Final Final Combined In Pharm

Front 1

examples of systemic fungal infections

Back 1

Soft tissue infection, UTI, Pneumonia, Meningitis, Septicemia (Aspergillus, Blastomyces , Candida, Coccidioides, Cryptococcus, Histoplasma);

Front 2

how do viruses replicate?

Back 2

Entry into host cell
Uncoating of viral nucleic acid
Synthesis of early reg. proteins
i.e. nucleic acid polymerases
Synthesis of RNA and DNA
Synthesis of structural proteins
Assembly of viral particles
Release from cell

Front 3

examples of subcutaneous fungal infections

Back 3

Puncture wounds- pseudallescheriasis , sporotrichosis

Front 4

describe malaria and how it is infected ect

Back 4

Plasmodium sporozoites enter the liver, form tissue schizonts, and undergo exoerythrocytic schizogony (blocked by primaquine) to produce merozoitesreleased from the liver invade erythrocytes and form trophozoites that undergo erythrocytic schizogony (antimalarial drugs). Some trophozoites develop into male and female gametocytes, which must subsequently pass back into a mosquito before they can develop into sporozoites

Front 5

albendazole

Back 5

A benzimidazole carbamate

Anti-helmithic
INHIBITS microtubule synthesis (specific for B-tubulin in nematodes).
ORAL
Nematode infections: Ascariasis
Trichuriasis, Hookworm, Pinworm , Teratogenic,
Side effects (well tolerated): Mild GI discomfort, Const/diarrhea Active metabolite (albendazole sulfoxide) made in liver.

Bioavailability increases if taken w/a FATTY MEAL.

Front 6

examples of superficial fungal infections

Back 6

Nails, Skin, Mucous membranes Epidermophyton, Microsporum , Trichophyton , Candida albicans (yeast)

Front 7

Diethylcar-bamazine

Back 7

Anti-helminthic Immobilizes microfilariae, displacing them from tissue; then are taken out by host defenses.
ORAL
Filariasis (W. bancrofti), Loiasis
Tropical eosinophilia
--
Excreted in urine.
Plasma t1/2=2-3 hrs in acidic urine.
Plasma t1/2=10 hrs in alkaline urine.

Front 8

nucleoside analogues

Back 8

prodrugs first synthesized by viral thymidine (selective for infected cells)-->host kinases activate; competitively inhibit viral DNA polymerase preventing synthesis of viral DNA
resistant when tyrosine kinase (TK) activity is lost

Front 9

ivermectin

Back 9

Semi-synthetic macrocyclic lactone

Anti-helminthic
Activates glutamate-gated Cl- ion channels; enhances GABA transmission of signals in peripheral nerves of nematodes; Cl influx; hyperpolerization; FLACCID paralysis. --
Strongyloidiasis (when isolated to intestines)
Onchocerciasis (microfilaria causing river blindness)
Mazzotti Reaction:
Hypersensitivity to dying microfilariae: fever, pruritis, arthralgia, HA.

Tx w/corticosteroids. Excreted in feces.
t1/2=16 hrs

Commonly used.

Disseminated Strongyloidiasis = THIABENDAZOLE

Front 10

name the polyene antibiotics

Back 10

amphotericin B and nystatin

Front 11

mebendazole

Back 11

A synthetic benzimidazole.

Anti-helminthic
INHIBITS microtubule synthesis (specific for B-tubulin in nematodes).
ORAL
Nematode infections: Ascariasis, Trichuriasis, Hookworm, Pinworm
Teratogenic

Side effects (well tolerated):
Mild GI discomfort
Const/diarrhea

Front 12

what are nematodes?

Back 12

roundworms, most common

Front 13

praziquantal

Back 13

Synthetic isoquinolone pyrazine

Anti-helminthic
Increases Ca2+ permeability leading to SPASTIC paralysis; dislodged and expelled.
ORAL
All schistosomes (liver flukes), trematodes, and cestodes Does NOT treat NEMATODES
Side effects: Abdominal pain, Nausea , HA
CONTRAINDICATION:
Not for ocular cysticercosis: Permanent eye damage!! T1/2= < 2 hrs

Front 14

amphotericin B

Back 14

Parenteral formulation, Extensive hepatic metabolism-Slowly excreted in the urine, Renal toxicity in 80% of patients, Lipid-based formulation reduces renal concentrations and subsequent toxicity; Poor CNS accumulation
MOA: Selectively binds ergosterol in fungal membranes--Results in inc membrane permeability and subsequent release of cytoplasmic components; used for a wide variety of fungi=used in resistance

Front 15

pyrantel pamoate

Back 15

A tetrahydro-pyrimidine derivative

Anti-helminthic
A neuromuscular blocking agent that causes ACh release, and inhibition of cholinesterase; Paralysis and expulsion. ORAL
Broad spectrum: Pinworm, Ascaris
Hookworm NOT effective against trichuriasis or strongyloides Alternate tx option for albendazole and mebendazole

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acyclovir

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HSV >> VZV > EBV > CMV ; oral F=22%
Nucleoside analogue Phosphorylated by viral thymidine kinase, then converted to active metabolite by host kinase; Competitively inhibits DNA polymerase (no synthesis).
Additionally: incorporated into nascent viral DNA and terminates elongation.
ORAL, IV and topical

HSV: 1st episode suppression, recurrent; Oral therapy: Labialis, genitalis, proctitis; IV: Severe HSV, herpes encephalitis, neonatal herpes (varicella in immunocomprimized and zoster in immunocomprimised)
Topical: genitalis, mild labialis
VZV: (less effective for shingles than vala or fam)
Varicella: chicken pox
NO CMV TX.
prophylaxis for CMV
Resistance when viral thymidine kinase activity is lost (drug is not activated). All nucleoside analogues: Prevents viral replication and shedding; shortens time to heal.
DOES NOT ELIMINATE virus.
Renal excretion.
(Gancyclovir is more effective for CMV)

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oxamiquine

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shistoome mansoni

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nystatin

Back 18

Structurally and functionally similar to amphotericin B, Useful only for candidiasis, MOA--Selectively binds ergosterol in fungal membranes, Results in inc membrane permeability and subsequent release of cytoplasmic components

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niclosamine

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cestode infections

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Tissue schizonticides

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Eliminate developing or dormant liver forms (primaquine)

Front 21

permethrin

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Anti-ectoparasite
Blocks Na+ currents, slowing the opening; paralysis.
Liquid prep (lice), Cream (mites)
DOC Lice (pediculosis)
DOC Mites (scabies) Resistance is an issue.

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what do azoles do?

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Inhibit 14-α-demethylase, Prevent conversion of lanosterol to ergosterol, Disrupts integrity of the cell membrane; accum of 14-α-demethylsterols, Impairs membrane-bound enzyme systems, ATPase , Enzymes of the electron transport system; rely on intact membrane to do job

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malathion

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Anti-ectoparasite
Inhibits cholinesterase in most eukaryotes; prevents neurons from returning to resting state --> perpetual activation; paralysis. --
Lice (pediculosis)
Mites (scabies)
Overdose can cause neuron paralysis in patient.

Front 24

valacyclovir

Back 24

HSV >> VZV > EBV > CMV
oral F=55%; prodrug of acyclovir
Nucleoside analogue

Phosphorylated by viral thymidine kinase, then converted to active metabolite by host kinase; Competitively inhibits DNA polymerase.
ORAL
1st episode suppress recurrent HSV: labialis, genitalis, proctitis
VZV: (shingles)
Prophylaxis CMV
Resistance when viral thymidine kinase activity is lost (drug is not activated). All nucleoside analogues: Prevents viral replication and shedding; shortens time to heal.

(Gancyclovir is more effective for CMV)
Less frequent dosing than acyclovir so better compliance.
does not eliminate virus

Front 25

Which of these agents increases GABA activation at the neuromuscular junction in nematodes?

Albendazole, (B) Suramin, (C) Iodoquinol (D) Ivermectin, (E) Pyrimethamine

Back 25

ivermectin--Treatment of intestinal strongyloidiasis and nchocerciasis;
Thiabendazole is used for disseminated strongyloides

Albendazole-Treatment of hookworm and pinworm infections; inhibits microtubule synthesis

(B) Suramin,-First line treatment of EAST African trypanosomiasis
(without CNS involvement)

(C) Iodoquinol -Mechanism unknown; luminal amebicide used to treat E. histolytica


(E) Pyrimethamine-Treatment of erythrocytic schizonts (malaria)

Front 26

what do polyene antibiotics do?

Back 26

Selectively binds ergosterol in fungal membranes--Results in inc membrane permeability and subsequent release of cytoplasmic components;

Front 27

thiabendazole

Back 27

disseminated strogyloides

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alkylating agents

Back 28

Transfer alkyl group to various tumor cell targets (replicating cells are most susceptible), Primarily the N7 position of guanine within DNA , Single strand or both strands (cross-linking);

Drug resistance----Increased DNA repair, Decreased permeability to drug, Increased glutathione production , (or GSH-S-transferase), (conjugates and inactivates alkylating agent)

Front 29

Which of the following is the drug of choice for treatment of most major schistosome infections?
Mebendazole, Thiabendazole,
Pyrantel pamoate, Praziquantel

Back 29

Mebendazole-nematode infections like ascariasis and trichuriasis; toxic—GI distress and dizziness

Thiabendazole-Disseminated strongyloides

Pyrantel pamoate-Alternate for albendazole and mebendazole (nematode infections like ascariasis, pinworm and hookworm

***Praziquantel-Trematode infections; increases calcium permeability leading to paralysis; adverse effects include GI distress and headache

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itraconazole

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Oral preparation, Capsule, Absorbed best in the fed state; Solution, Absorbed best in the fasting state
Metabolized by CYP3A4 isoenzyme system, Many drug interactions, DOC blastomycosis (lung infection), Also indicated for onychomycosis (nail infection)=very popular used a lot
-Inhibit 14-α-demethylase, Prevent conversion of lanosterol to ergosterol, Disrupts integrity of the cell membrane; accum of 14-α-demethylsterols, Impairs membrane-bound enzyme systems, ATPase , Enzymes of the electron transport system; rely on intact membrane to do job

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DOC for filariasis

Back 31

w. bancrofti is diethycarbamazine

Front 32

famiciclovir

Back 32

HSV >> VZV > EBV > CMV
oral F=80%-->penciclovir after absorption
Nucleoside analogue
Phosphorylated by viral thymidine kinase, then converted to active metabolite by host kinase; Competitively inhibits DNA polymerase
ORAL (Most bioavailable at 80%)
HSV: labialis, genitalis, proctitis
VZV: (shingles)
NO CMV at all
Resistance when viral thymidine kinase activity is lost. All nucleoside analogues: Prevents viral replication and shedding; shortens time to heal.

Renal AND fecal excretion.
Converts to penciclovir
Less frequent dosing than acyclovir so better compliance

Front 33

drug that causes mazzotti reaction

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ivermectin

Front 34

fluconazole

Back 34

Absorption is not affected by food or gastric acidity, > 90% renal elimination, Excellent BBB penetration; Uses-Prevention of cryptococcal meningitis in AIDS patients, Candidiasis, Esophagus, urinary tract and vagina
-Inhibit 14-α-demethylase, Prevent conversion of lanosterol to ergosterol, Disrupts integrity of the cell membrane; accum of 14-α-demethylsterols, Impairs membrane-bound enzyme systems, ATPase , Enzymes of the electron transport system; rely on intact membrane to do job

Front 35

drug causing flaccid paralysis

Back 35

activates glutamate, enhance GABA, cl influx hyperpolarizaiton
ivermectin

Front 36

Blood schizonticides

Back 36

Act on erythrocytic parasites chloroquine, quinine, mefloquine, pyrimethamine, proguanil

Front 37

drug that causes spastic paralysis

Back 37

inc Ca permeability
praziquantal

Front 38

ketoconazole

Back 38

largely phased out b/c of more drug intx, less BBB penetration, lower activity
-Inhibit 14-α-demethylase, Prevent conversion of lanosterol to ergosterol, Disrupts integrity of the cell membrane; accum of 14-α-demethylsterols, Impairs membrane-bound enzyme systems, ATPase , Enzymes of the electron transport system; rely on intact membrane to do job
***SE are nasea rash hepatic injury and hematopoietic toxicity

Front 39

DOC strongyloidiasis in the intestines

Back 39

ivermectin

Front 40

penciclovir

Back 40

Nucleoside analogue (The active metabolite of famciclovir)
Phosphorylated by viral thymidine kinase, then converted to active metabolite by host kinase; Competitively inhibits DNA polymerase
Topical
HSV: recurrent labialis --
All nucleoside analogues: Prevents viral replication and shedding; shortens time to heal.

Front 41

DOC disseminated strongyloidiasis

Back 41

thiabendazole

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voriconazole

Back 42

-“second-generation”, Enhanced activity against Aspergillus and Candida species, 60-100 times more potent than fluconazole against Candida (Yet fluconazole still listed as primary and voriconazole as alt.); primary adverse affect is PHOTOPHOBIA AND CHROMATOPSIA; -Inhibit 14-α-demethylase, Prevent conversion of lanosterol to ergosterol, Disrupts integrity of the cell membrane; accum of 14-α-demethylsterols, Impairs membrane-bound enzyme systems, ATPase , Enzymes of the electron transport system; rely on intact membrane to do job

Front 43

Drugs that inhibit microtubule synthesis

Back 43

albendazole and mebendazole and thiabendazole

Front 44

what are trematodes

Back 44

flukes

Front 45

DOC lice and mites

Back 45

permethrin

Front 46

posaconazole

Back 46

specifically indicated for prophylaxis in immunocomprimised individuals
-Inhibit 14-α-demethylase, Prevent conversion of lanosterol to ergosterol, Disrupts integrity of the cell membrane; accum of 14-α-demethylsterols, Impairs membrane-bound enzyme systems, ATPase , Enzymes of the electron transport system; rely on intact membrane to do job

Front 47

alternate for lice and mties

Back 47

malathion

Front 48

2 drugs more effective against shingles

Back 48

valacyclovir and famiciclovir

Front 49

SE is paralysis in patient

Back 49

malathion inhibits cholinesterase-->paralysis

Front 50

clotimazole

Back 50

Topical formulation, Candida, Mouth, Throat, Vagina, Vulva; Dermatophyte infections of the skin--Athlete’s foot, Jock itch, not effective against infections of SCALP OR NAILS
-Inhibit 14-α-demethylase, Prevent conversion of lanosterol to ergosterol, Disrupts integrity of the cell membrane; accum of 14-α-demethylsterols, Impairs membrane-bound enzyme systems, ATPase , Enzymes of the electron transport system; rely on intact membrane to do job

Front 51

suramin

Back 51

mech unknown sulfated napthylamine; IV
early EAST african trypanosomiasis
does not enter CNS-->not effective in advanced disease
---sure is nice to sleep

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Gametocides

Back 52

: Kill sexual stages and prevent transmission to mosquitoes, primaquine

Front 53

melarsoprol

Back 53

melatonin helps to sleep

reacts w/ sulfhydryl groups of trypanothione. inhibits pyruvate kinase dec ATP;
IV
CNS advanced EAST african trypanosomiaisis
ENTERS CNS

Front 54

naftifine

Back 54

Topical treatment of superficial dermatophyte infections

Inhibit squalene monooxygenase (instrumental in conversion of squalene to lanosterol), Results in reduced ergosterol biosynthesis

Front 55

early and late stage tx for east african trypanosome

Back 55

suramin, melarsoprol

Front 56

nucleoside analogue eliminated by? exception?

Back 56

renal excretion
famiciclovir--renal and fecal excretion

Front 57

pentamidine

Back 57

MOA unknown
IV
early stage west african trypanosomiasis

***best know to treat pneumocystis jirrovecii

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terbinafine

Back 58

Oral treatment of onychomycosis, Accumulates in nails, skin and fat; used a lot;

Inhibit squalene monooxygenase (instrumental in conversion of squalene to lanosterol), Results in reduced ergosterol biosynthesis

Front 59

eflornithine

Back 59

selective irrev inhib ornithin decarboxylase; disrupts prod of nucleic acid and prot synthesis
advanced stage west african trypanosomiasis---crosses BBB
IV
SE diarrhea anemia leukopenia
less toxic than melarsoprol

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bacteriocidal

Back 60

Bactericidal typically has more rapid effect and less likely to induce resistance (tend to target cell wall or activate autolytic enzymes; i.e., penicillins
irreversible inhibitors are usually bactericidal (streptomycin)

Front 61

treatment for west african trypanosomiasis early and late

Back 61

pentamidine, eflornithine

Front 62

allylamines

Back 62

naftifine and terbinafines

Front 63

nifurtimox

Back 63

nitroaromatic compount O2 radicals toxic (no catalase)
ox (oxidizing stress)
american trypanosomiasis (chaga's disease)
GI distress
IFN gamma helps shorten acut ephase

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2 drugs for prophylaxis of CMV

Back 64

valacyclvir and acylovir

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drug for trypanozomiasis american

Back 65

nifutimox

Front 66

what is the MOA of allyamines?

Back 66

Inhibit squalene monooxygenase (instrumental in conversion of squalene to lanosterol), Results in reduced ergosterol biosynthesis

Front 67

sodium stibgluconate

Back 67

MOA unknown poss dec glycolysis and FA syn
ORAL
cut and visceral leishmaniasis mostly cutanoeus
---sand fly in macs

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primaquine

Back 68

Anti-malarial (8-aminoquinoline) Unknown mechanism. NOT effective in erythrocytic forms; eliminate liver forms; kill sexual stages prevent transmission ot mosquitoes; pre erythrocytic prevents preleapse due to vivax
Tissue schizonticide and gametocide
ORAL
NOT effective on erythrocytic forms.
Side effects: Well tolerated, except:
AVOID IN: G6PD-deficient pts-hemolysis, Myelosuppressed
, Pregnancy
Max [plasma]=1-2 hrs (FASTEST)
T 1/2 = 3-8 hrs.
Urine excretion

Front 69

miltefosine

Back 69

alkylphosphocholine analog; not in US
treats visceral leishmaniaissis only (sandfly)
oral

Front 70

griseofulvin

Back 70

Very lipophilic, Absorption is increased when taken with fatty meal, Induces P450 CYP3A4 , accumulates in keratin precursor cells of skin, hair and nails, Interacts with polymerized microtubules and disrupts their function, Binding sites are distinct from those of colchicine and vinca alkaloids (anti-inflammatory/gout and antineoplastic drugs respectively), Prevents mitosis of dermatophytes; inhibits MT synthesis and function

Front 71

treat for leishmanisis

Back 71

sodium stibogluconate
miltefosine (visceral but not in US)

Front 72

trifluridine

Back 72

Nucleoside analogue
Phosphorylated by viral thymidine kinase, then converted to active metabolite by host kinase; Competitively inhibits DNA polymerase
Topical ocular
HSV: keratoconjunctivitis
Well tolerated.
-- All nucleoside analogues: Prevents viral replication and shedding; shortens time to heal.

Front 73

MOA of griseofulvin

Back 73

inhibits MT synthesis and function

Front 74

what are cestodes?

Back 74

tapeworms

Front 75

flucocystine

Back 75

Fluorinated pyrimidine analog, Accumulated by fungal cells, Converted to 5-fluorouracil (5-FU) by cytosine deaminase , Subsequent metabolites are Incorporates into fungal RNA and disrupts subsequent protein synthesis, Another metabolite, 5-fluorodeoxyuridylic acid potently inhibits thymidylate synthetase resulting in impaired DNA synthesis, Human cells lack cytosine deaminase
**inhibits cytosine deaminase (only fungus cells) blocks pyrimidine and protein synthesis; impairs RNA synthesis;
SE are bm suppression; tx: symstemic fungus
***used more commonly in combo w/ an AZOLE

Front 76

what drug treats chicken pox?

Back 76

acylcovir

Front 77

echinocandins

Back 77

caspofungin, anidulafungin,

Front 78

chloroquine

Back 78

CQ Anti-malarial (4-aminoquinoline)
Concentrates in the food vacuole; prevents polymeration of heme into hemozoin. (Parasite eats Hb for nutrients, but heme is toxic to it, so it converts it to hemozoin); lysis of parasite and RBC.
**Blood schizonticide -->erythrocytic paracites
ORAL
Malaria (DOC for tx AND prophylaxis)
Used alone for P.falciparum and P.malariae; w/combo of primaquine for P. vivax or P. ovale.
***Increasing drug resistance
***GI distress, N/V
CONTRAINDICATIONS: Psoriasis or porphyria, Retinal abnormalities
, Myopathy
Don't take w/Kaolin or Ca2+/Mg antacids → reduce absorption
Max [plasma]=3 hrs. t1/2 = 1-2 months (LONGEST)
Urine excretion
****Safe in pregnancy and kids

Front 79

caspofungin

Back 79

IV preparation; Inhibits the β(1,3)-D-glucan synthase enzyme complex-Prevents formation of β(1,3)-D-glucans in the fungal cell wall; Excellent activity against Candida species, Particularly azole-resistant infections

Front 80

topical drug for recurrent labialis HSV

Back 80

penciclovir

Front 81

anidulafungin

Back 81

-also inhibits glucan synthase, indicated for intra-abdominal abscess caused by Candida species and esophageal candidiasis (same mech but diff target)

Front 82

cyclophosphamide

Back 82

Alkylating agent A bis(chloroethyl)amine ***must be activated by P450 system; transfer of alkyl group to tumor cell targets; causes PHYSICAL cross-linking of DNA by binding to guanine; prevents transcription and replication (All alkylating agents).
ORAL or IV
Cell-cycle nonspecific treatment of neoplastic cells (broad spectrum).
CLL Nonenzymatic conversion to cytoxic form in non-hepatic tissue.
Resistance (for ALL alkylating agents):
Increased DNA repair (repairs
drug's damage)
Dec'd. permeability to drug
Inc'd. glutathione production
or GSH-S-transferase;
conjugates and inactivates
drug --

Front 83

ganciclovir

Back 83

Nucleoside analogue Same as valacyclovir.
ORAL and IV
DOC for CMV (oral for prophylaxis; IV or oral for CMV maintenance)
CMV retinitis w/ IV; oral-CMV prophylaxis, retintis
Leukopenia
Thrombocytopenia 100x more active against CMV than acyclovir.
All nucleoside analogues: Prevents viral replication and shedding; shortens time to heal.

****Ganciclovir is phosphorylated by a viral kinase in CMV infected cells; Competitively inhibits viral DNA polymerase; 100X more active against CMV than ACV

Front 84

pre erythrocytic malarial drug

Back 84

primaquine

Front 85

cidofovir

Back 85

Nucleoside analogue Activated independent of viral enzymes.
alternate b/c of more sideeffects
IV
CMV: (alternate choice after gan)
Maintenance, CMV retinitis ind and malt?
CONTRAINDICATION: renal insufficiency and when taking aminoglycosides or Amphotericin B (due to add'n of renal toxicity)
Nephrotoxicity
Neutropenia
Metabolic acidosis -- All nucleoside analogues: Prevents viral replication and shedding; shortens time to heal.

Front 86

most common parasitic infections ww?

Back 86

ascaris>hookworms>trichuris>filaris>enterobius ALL are nematodes
>shistosomes (trematodes)>tapeworms>strongyloides and trichinella

Front 87

foscarnet

Back 87

Nucleoside analogue (a pyrophosphate derivative) Activated independent of viral enzymes OR host kinases. Blocks pyrophosphate-binding sites on viral DNA polymerase (no attachment of nucleoside precursors to DNA) IV HSV: acyclovir-resistant
herpes genitalis
VZV: acyclovir-resistant
shingles
CMV: 2nd line
maintenance
(If gan-resistant
or if pt. had
severe
neutropenia rxn
to gan) Renal toxicity
Cardiac arrhythmias PREHYDRATION is a must due to renal toxicity.

All nucleoside analogues: Prevents viral replication and shedding; shortens time to heal.

***still distrupts replication

Front 88

fastest malrial drug

Back 88

primaquine; 1-2 hours lasts 3-8 hours

Front 89

DOC for CMV

Back 89

ganciclovir

Front 90

bacteriostatic

Back 90

Bacteriostatic relies heavily on competent immune response (tend to target metabolic pathways; i.e., sulfonamides); Also, reversible inhibitors of protein synthesis are often bacteriostatic (tetracyclines)

Front 91

what to use for CMV if resistant to primary drugs

Back 91

foscarnet

Front 92

drugs that causes G6PD deficient pts hemolysis

Back 92

primaquine

Front 93

what to use for HSV/VZV if resistant to acylovir

Back 93

foscarnet

Front 94

albendazole

Back 94

A benzimidazole carbamate

Anti-helmithic
INHIBITS microtubule synthesis (specific for B-tubulin in nematodes).
ORAL
Nematode infections: Ascariasis
Trichuriasis, Hookworm, Pinworm , Teratogenic,
Side effects (well tolerated): Mild GI discomfort, Const/diarrhea Active metabolite (albendazole sulfoxide) made in liver.

Bioavailability increases if taken w/a FATTY MEAL.

Front 95

NNRI

Back 95

nucleoside reverse transcriptase inhibitor
Synthetic derivatives of nucleosides
Converted to active triphosphate metabolite (nucleotide) by host kinases
Compete for entry into viral DNA (rxn which is catalyzed by reverse transcriptase)
Cause DNA chain termination
given in combination-->single drug therapy inc resistance

Front 96

DOC for malarial treatment an dprophylaxis

Back 96

chlorquine ---P. falciparum P malariae
combo of primauqine for vivax and ovale

Front 97

purine cogener NRTI

Back 97

didanosine

Front 98

carmustine

Back 98

Alkylating Agent
A nitrosurea; req's nonenzymatic conversion to active form; see above. --
Cell-cycle nonspecific treatment of gliomas. Non-resistant with other alkylating agents.
Resistance (for ALL alkylating agents):
Increased DNA repair (repairs
drug's damage)
Dec'd. permeability to drug
Inc'd. glutathione production
or GSH-S-transferase;
conjugates and inactivates
drug
**Crosses BBB

Front 99

name 4 pyrimidine cogeners of NRTIs

Back 99

lamivudine, stavudine, emtiricitabine, zidovudine (AZT)

Front 100

quinine

Back 100

used for severe malaria
Anti-malarial. From the bark of a cinchona tree
Unknown mechanism.
Blood schizonticide -->NOT active against liver schinzonts.
(all 4 species) Gametocidal (P.vivax & P.ovale)
ORAL
Esp. P.falciparum
Give w/doxycycline or other Ab. to reduce duration to 3 day max.
NOT for prophylaxis (too much toxicity) NOT active on liver stage parasites.
"Cinchonism":- Tinnitus, HA, Nausea/dizziness, flushing, Visual disturbances
Caution w/cardiac =****QT prolongation is common
CONTRAINDICATION: anyone taking or recently took mefloquine (cardiac arrest and convulsions) Max [plasma]=1-3 hrs.
T1/2 = 18 hours
--higher rate in infected pts. due to increased protein binding
Liver metabolism;
urine excretion
2nd choice w/Ab for treatment of malaria. (combine w/any of the following: tetracycline, doxycycline, clindamycine, azithromycin)

Front 101

didanosine

Back 101

Nucleoside Reverse Transcriptase Inhibitor (NRTI)
--Purine cogener- Synthetic nucleoside  nucleotide by host kinases; nucleotide competes w/endogenous nucleoside triphospates for entry into viral DNA (rxn catalized by reverse transcriptase); DNA chain termination ORAL (in combo) HIV
Combo of different classes prevents resistance (2 NRTIs are often combined w/ NNRTI or a protease inhibitor)

Pancreatitis
Peripheral neuropathy (All NRTI) crosses BBB
Renal excretion

If adverse effects occur, pull back on dose, don't have to stop tx.

Front 102

Diethylcar-bamazine

Back 102

Anti-helminthic Immobilizes microfilariae, displacing them from tissue; then are taken out by host defenses.
ORAL
Filariasis (W. bancrofti), Loiasis
Tropical eosinophilia
--
Excreted in urine.
Plasma t1/2=2-3 hrs in acidic urine.
Plasma t1/2=10 hrs in alkaline urine.

Front 103

most common side effect of NNRTI

Back 103

rash

Front 104

quinidine

Back 104

not used much due to shorter 1/2 life
Anti-malarial. From the bark of a cinchona tree Unknown mechanism.
Blood schizonticide (all 4 species)
Gametocidal (P.vivax & P.ovale) ORAL Esp. P.falciparum
Give w/doxycycline or other Ab. to reduce duration to 3 day max.
NOT for prophylaxis (too much toxicity) NOT active on liver stage parasites.
"Cinchonism": Tinnitus, HA, Nausea/dizziness, Flushing, Visual disturbances
Caution w/cardiac =QT prolongation is common
CONTRAINDICATION: anyone taking or recently took mefloquine (cardiac arrest and convulsions) Max [plasma]=1-3 hrs.
T1/2 = 18 hours
--higher rate in infected pts. due to increased protein binding
Liver metabolism;
urine excretion
2nd choice w/Ab for treatment of malaria. (combine w/any of the following: tetracycline, doxycycline, clindamycine, azithromycin)

Front 105

side effect of didanosine

Back 105

pancreatitis and peripheral neuropathy

Front 106

MIC

Back 106

MIC (minimal inhibitory concentration-used most frequently): Concentration of drug required to inhibit growth of the pathogen.
--inc concentration the time to inhibit is decreased ---concentration dependent

Front 107

NRTI you can't combine!

Back 107

stavudine and zidovudine (antagonistic)

Front 108

mefloquine

Back 108

MQ
Anti-malarial (synthetic 4-quinoline methanol) Unknown mechanism.
Blood schizonticide
ORAL-->local irritation
Tx. of Chloroquine-resistant P.falciparum (last choice for tx)
Prophylaxis for malaria
Not for severe infections; (quinine preferred d/t more rapid activity and less resistance)
NOT for use WITH quinine or quinidine.
Side effects: N/V, dizziness,
Sleep & behavioral disturbances
CONTRAINDICATIONS: epilepsy, phychiatric disorders, cardiac conditions
G6PD deficiency (hemolysis d/t decreased NADPH and GSH) Max [plasma]=18 hrs.
(SLOWEST)
T1/2=20 days (weekly dosing)

Front 109

oral drug that treats Hep B

Back 109

lamivudine

Front 110

ivermectin

Back 110

Semi-synthetic macrocyclic lactone

Anti-helminthic
Activates glutamate-gated Cl- ion channels; enhances GABA transmission of signals in peripheral nerves of nematodes; Cl influx; hyperpolerization; FLACCID paralysis. --
Strongyloidiasis (when isolated to intestines)
Onchocerciasis (microfilaria causing river blindness)
Mazzotti Reaction:
Hypersensitivity to dying microfilariae: fever, pruritis, arthralgia, HA.

Tx w/corticosteroids. Excreted in feces.
t1/2=16 hrs

Commonly used.

Disseminated Strongyloidiasis = THIABENDAZOLE

Front 111

NRTI that can be IV

Back 111

zidoviudine

Front 112

pyrimethamine

Back 112

Folate reductase inhibitor Inhibition of plasmodial dihydrofolate reductase.
Blood schizonticide--> all four species
***also treats toxoplasmosis
Chemoprophylaxis (in combo w/chloroquine) for malaria -- T 1/2=3.5 days (LONG)

Front 113

side effects of zidoviudine

Back 113

bone marrow suppression, anemia, neutropenia

Front 114

procarbazine

Back 114

Alkylating Agent A
methylhydrazine derivative that inhibits synthesis of DNA, RNA and protein; additionally, azoprocarbazine and H2O2 generated and may cause DNA strand breaks. --
Cell-cycle nonspecific treatment of Hodgkin's lymphoma. Resistance (for ALL alkylating agents):
Increased DNA repair (repairs
drug's damage)
Dec'd. permeability to drug
Inc'd. glutathione production
or GSH-S-transferase;
conjugates and inactivates
drug

Front 115

lamivudine

Back 115

Nucleoside Reverse Transcriptase Inhibitor (NRTI)
--Pyrimidine cogener-- Synthetic nucleoside -->nucleotide by host kinases; nucleotide competes w/endogenous nucleoside triphospates for entry into viral DNA (rxn catalized by reverse transcriptase); DNA chain termination
ORAL (in combo)
HIV Hep B
Combo of different classes prevents resistance (2 NRTIs are often combined w/ NNRTI or a protease inhibitor)
SE: Lactic acidosis, Hepatic steatosis
(All NRTI) crosses BBB
Renal excretion

Front 116

proguanil

Back 116

Folate reductase inhibitor Inhibition of plasmodial dihydrofolate reductase.
Blood schizonticide-->treats all four species
Chemoprophylaxis (in combo w/chloroquine) for malaria -- T 1/2= 16 hrs. (SHORT)

Front 117

stavudine

Back 117

Nucleoside Reverse Transcriptase Inhibitor (NRTI)
--Pyrimidine cogener--
Synthetic nucleoside --> nucleotide by host kinases; nucleotide competes w/endogenous nucleoside triphospates for entry into viral DNA (rxn catalized by reverse transcriptase); DNA chain termination
ORAL (in combo)
HIV
Combo of different classes prevents resistance (2 NRTIs are often combined w/ NNRTI or a protease inhibitor)

CAN NOT combo with zidovudine –antagonistic effect
SE-Pancreatitis
(All NRTI) crosses BBB
Renal excretion
Can be used in lieu of zidovudine, if rxn.

Front 118

mebendazole

Back 118

A synthetic benzimidazole.

Anti-helminthic
INHIBITS microtubule synthesis (specific for B-tubulin in nematodes).
ORAL
Nematode infections: Ascariasis, Trichuriasis, Hookworm, Pinworm
Teratogenic

Side effects (well tolerated):
Mild GI discomfort
Const/diarrhea

Front 119

Emtricitabine

Back 119

Nucleoside Reverse Transcriptase Inhibitor (NRTI)
--Pyrimidine cogener--
Synthetic nucleoside --> nucleotide by host kinases; nucleotide competes w/endogenous nucleoside triphospates for entry into viral DNA (rxn catalized by reverse transcriptase); DNA chain termination
ORAL (in combo)
HIV
Combo of different classes prevents resistance (2 NRTIs are often combined w/ NNRTI or a protease inhibitor)
(All NRTI) crosses BBB
Renal excretion

Front 120

antibodies for malaria?

Back 120

tetracycline, doxylcine, clindamycin, azithromycin

--erythrocyte shizonts all 4 species

Front 121

zidovudine

Back 121

AZT; Nucleoside Reverse Transcriptase Inhibitor (NRTI)
--Pyrimidine cogener--
Synthetic nucleoside -->nucleotide by host kinases; nucleotide competes w/endogenous nucleoside triphospates for entry into viral DNA (rxn catalized by reverse transcriptase); DNA chain termination
ORAL (in combo) and IV
HIV
combo of different classes prevents resistance (2 NRTIs are often combined w/ NNRTI or a protease inhibitor)
CAN NOT combo with stavudine –antagonistic effect
SE: Bone marrow suppression,
Anemia, Neutropenia
(All NRTI) crosses BBB
Renal excretion

Front 122

MBC

Back 122

MBC (minimal bactericidal concentration): Concentration required to kill the pathogen

Front 123

efavirenz

Back 123

Nonnucleoside Reverse Transcriptase Inhibitor (NNRTI) Direct inhibition of reverse transcriptase (no activation req’d); disrupts catalytic site. ORAL HIV Combo req'd.
Interact'n with protease inhib.
Rash
CONTRAINDICATION: Pregnancy (teratogenic) Crosses BBB
Renal AND fecal excretion
Most POTENT NNRTI (once a day dosing)

Front 124

atovaquone

Back 124

inhibits mitochondrial E transport dec ATP synthesis....for malaria????

Front 125

nevirapine

Back 125

Nonnucleoside Reverse Transcriptase Inhibitor (NNRTI) Direct inhibition of reverse transcriptase (no activation req’d); disrupts catalytic site. ORAL HIV Combo req'd.

Rash; hepatotoxicity
Induces P450 system  drug interactions (including ↓ effect of protease inhibitors) Crosses BBB
Renal AND fecal excretion

Front 126

praziquantal

Back 126

Synthetic isoquinolone pyrazine

Anti-helminthic
Increases Ca2+ permeability leading to SPASTIC paralysis; dislodged and expelled.
ORAL
All schistosomes (liver flukes), trematodes, and cestodes Does NOT treat NEMATODES
Side effects: Abdominal pain, Nausea , HA
CONTRAINDICATION:
Not for ocular cysticercosis: Permanent eye damage!! T1/2= < 2 hrs

Front 127

atazanavir

Back 127

Protease Inhibitor Binds active site of HIV protease; production of immature, noninfectious viral particles. ORAL HIV Combo of different classes prevents resistance (2 NRTIs are often combined w/a protease inhibitor)
Interaction with NNRTI
(in book: hyperbilirubinemia, PR interval prolongation)

SE: breast hypertrophy, central adiposity, hyperlipidemia and insulin resistance---All protease inhibitors can cause disruption of lipid and CHO metabolism

Front 128

malarone

Back 128

Folate reductase inhibitor Inhibition of plasmodial dihydrofolate reductase + inhibits nucleic acid and ATP in parasite by messing up transport.
Blood schizonticide -- Chloroquine-resistant malaria (Treatment or prophylaxis) -- A combo drug of proguanil + atovaquone

Front 129

Lopinavir

Back 129

Protease Inhibitor Binds active site of HIV protease; production of immature, noninfectious viral particles. ORAL HIV (Combo req'd.)
Interaction with NNRTI (in book: GI intolerance)

SE: breast hypertrophy, central adiposity, hyperlipidemia and insulin resistance---All protease inhibitors can cause disruption of lipid and CHO metabolism

Front 130

cisplatin

Back 130

Alkylating Agent
Inorganic platinum complex; causes PHYSICAL cross-linking of DNA by binding to guanine; prevents transcription and replication (All alkylating agents).
IV
Testicular cancer
Ovarian cancer
Bladder cancer Nephrotoxic

Adverse effect: SEVERE nausea

Resistance (for ALL alkylating agents):
Increased DNA repair (repairs
drug's damage)
Dec'd. permeability to drug
Inc'd. glutathione production
or GSH-S-transferase;
conjugates and inactivates
drug IV hydration or diuretics REQ'D to reduce nephrotoxicity.

NOTE: Carboplatin is 2nd generation w/less renal toxicity;
Oxaliplatin is 3rd generation -- cells resistant to 1st and 2nd gens are typ. NOT resistant to this one.

Front 131

Ritonavir

Back 131

Inhibitor of Protease Inhibitor Inhibits metabolism of protease inhibitors; increases ½ life of other protease inhibitors. ORAL HIV (in book: GI intolerance, hepatitis, inhibition of other drugs: antiarrythmics, opioids, tricyclic antidepressants) Ritonavir + Lopinavir are combo of choice


SE: breast hypertrophy, central adiposity, hyperlipidemia and insulin resistance---All protease inhibitors can cause disruption of lipid and CHO metabolism

Front 132

2 gametocidal drugs for malaria

Back 132

primaquine and quinine (only vavax ovale)

Front 133

enfuvirtide

Back 133

Fusion Inhibitor Inhibits fusion of HIV with host cell. Specifically binds gp41, blocking viral entry. SubQ injection (2x daily) HIV (in book: injection site rxns, hypersensitivity rxns) Good alternative when resistance or intolerance occurs w/other drug classes.

Front 134

pyrantel pamoate

Back 134

A tetrahydro-pyrimidine derivative

Anti-helminthic
A neuromuscular blocking agent that causes ACh release, and inhibition of cholinesterase; Paralysis and expulsion. ORAL
Broad spectrum: Pinworm, Ascaris
Hookworm NOT effective against trichuriasis or strongyloides Alternate tx option for albendazole and mebendazole

Front 135

amantidine

Back 135

Synthetic tricycylic amine compound Prevents uncoating (inhibits viral M2 proton selective ion channel-This channel is needed for acidification and subsequent uncoating and nucleic acid transfer from the endosome into the host cell cytoplasm ) of influenza A particles after cell entry.
ORAL (also liquid preps for kids) Influenza A
Not effective against Influenza B
REDUCE dose in renal insufficiency.
Crosses BBB, so more negative
CNS effects. Give w/in 48 hrs: Reduces severity and duration.

Front 136

2 drugs that can cause hemolysis w/ G6PD def?

Back 136

mefloquine and primaquine

Front 137

rimantadine

Back 137

Synthetic tricycylic amine compound Prevents uncoating (inhibits viral M2 proton selective ion channel--This channel is needed for acidification and subsequent uncoating and nucleic acid transfer from the endosome into the host cell cytoplasm
) of influenza A particles after cell entry.
ORAL (also liquid preps for kids)
Influenza A (DOC)
Not effective against Influenza B
REDUCE dose in renal insufficiency.
DOES NOT cross BBB, so less
side effects.Give w/in 48 hrs: Reduces severity and duration.

Front 138

susceptibility testing

Back 138

-In vitro testing to confirm susceptibility to antimicrobial agents, ideally, to a narrow spectrum drug

Front 139

oseltamivir

Back 139

Neuraminidase inhibitor
Inhibit neuraminidase so that virions can not be released from surface of infected cell.
ORAL
Influenza A and B
(prophylaxis and
treatment)
Dose reduction NOT necessary in renal insufficiency
Give w/in 48 hrs: Reduces severity and duration.
Viral neuraminidase inactivates mucus by breaking linkages. The inhibitor allows our mucus to be active against the virus.

Front 140

what is cinochonism?

Back 140

tinnitius HA nausea/dizzy, flush, visual distubances in quinine malarial drug

Front 141

zanamivir

Back 141

Neuraminidase inhibitor Inhibit neuraminidase so that virions can not be released from surface of infected cell.
NASAL
Influenza A and B
Dose reduction NOT necessary in renal insufficiency
Viral neuraminidase inactivates mucus by breaking linkages. The inhibitor allows our mucus to be active against the virus.

Front 142

oxamiquine

Back 142

shistoome mansoni

Front 143

ribavirin

Back 143

Guanosine analog
Inhibits synthesis of viral nucleic acid d/t reduced guanosine triphosphate levels; Inhibits host cell nucleic acid synthesis.
Aerosol (RSV)
IV (HCV)
RSV , Hep C (in combo with IFN-α2b drugs)
(In book: Teratogenic)

****Alone for RSV; combo with IFNalpha2b for hepatitis C;
IFN alone for hepatitis B
Recall lamivudine is also effective against Hep B

Front 144

do not take MQ w/ ?

Back 144

quinine or quinidine

Front 145

interferon a

Back 145

Interferon
A DNA recombinant; Signals immune pathways; induction of antiviral proteins in the host cells. (Boosts hosts immune response)
SubQ or IM
Hep B, Hep C (in combo w/
ribavirin)
(in book: also papillomaviruses, Kaposi's sarcoma, hairy cell leukemia, genital warts, CML, mal. melanoma, multiple myeloma, renal ca.) --
Recall that lamivudine (an NRTI) also treats Hep B.

Front 146

carboplatin

Back 146

2nd generation platinum compound with less renal toxicity

Alkylating Agent
Inorganic platinum complex; causes PHYSICAL cross-linking of DNA by binding to guanine; prevents transcription and replication (All alkylating agents).
IV
Testicular cancer
Ovarian cancer
Bladder cancer Nephrotoxic

Adverse effect: SEVERE nausea

Resistance (for ALL alkylating agents):
Increased DNA repair (repairs
drug's damage)
Dec'd. permeability to drug
Inc'd. glutathione production
or GSH-S-transferase;
conjugates and inactivates
drug IV hydration or diuretics REQ'D to reduce nephrotoxicity.

Front 147

2 things effective against hep B

Back 147

lamivudine and interferon alpha

Front 148

drug for CQ resistant P falciparum?

Back 148

MQ

Front 149

how to treat hep C

Back 149

ribavirin and IFN-a2b drugs

Front 150

niclosamine

Back 150

cestode infections

Front 151

subQ injection for HIV

Back 151

enfurvirtide

Front 152

2 drugs folate reductase inhibitors?

Back 152

pyrimehtamine, proguanil

Front 153

DOC for influenza A

Back 153

rimantadine

Front 154

PAE

Back 154

Post-antibiotic effect (PAE)- give drug, after it is taken away then inhibition cont for a time; time required for the bacteria to return to log growth following drug withdrawal

The PAE in vivo is considerably longer than in vitro due presumably to post-antibiotic leukocyte enhancement (PALE) and exposure of bacteria to subinhibitory drug concentrations. Aminoglycosides and quinolones (once-daily) . have concentration-dependent PAE. For instance, aminoglycosides remain effective for some time after serum levels of the drug drop below the MIC of a given organism.

Front 155

amantadine does/not cross BBB?

Back 155

it does

Front 156

permethrin

Back 156

Anti-ectoparasite
Blocks Na+ currents, slowing the opening; paralysis.
Liquid prep (lice), Cream (mites)
DOC Lice (pediculosis)
DOC Mites (scabies) Resistance is an issue.

Front 157

rimantadine does/not cross BBB

Back 157

does not so less side effects

Front 158

oxaliplatin

Back 158

3rd generation agent; cells resistant to cisplatin and carboplatin are typically not resistant to this drug.

Alkylating Agent
Inorganic platinum complex; causes PHYSICAL cross-linking of DNA by binding to guanine; prevents transcription and replication (All alkylating agents).
IV
Testicular cancer
Ovarian cancer
Bladder cancer Nephrotoxic

Adverse effect: SEVERE nausea

Resistance (for ALL alkylating agents):
Increased DNA repair (repairs
drug's damage)
Dec'd. permeability to drug
Inc'd. glutathione production
or GSH-S-transferase;
conjugates and inactivates
drug IV hydration or diuretics REQ'D to reduce nephrotoxicity.

Front 159

oral drug treats influenza A and B

Back 159

oseltamivir

Front 160

malathion

Back 160

Anti-ectoparasite
Inhibits cholinesterase in most eukaryotes; prevents neurons from returning to resting state --> perpetual activation; paralysis. --
Lice (pediculosis)
Mites (scabies)
Overdose can cause neuron paralysis in patient.

Front 161

nasal drug treats influenza A and B

Back 161

zanamivir

Front 162

why would you give IV antibiotics?

Back 162

critically ill, bacterial meningitis, endocarditis, N/V, gastrectomy

pharmacokinetics are pretty much the same orally or parenterally

Front 163

drugs that treats RSV

Back 163

ribavirin

Front 164

Which of these agents increases GABA activation at the neuromuscular junction in nematodes?

Albendazole, (B) Suramin, (C) Iodoquinol (D) Ivermectin, (E) Pyrimethamine

Back 164

ivermectin--Treatment of intestinal strongyloidiasis and nchocerciasis;
Thiabendazole is used for disseminated strongyloides

Albendazole-Treatment of hookworm and pinworm infections; inhibits microtubule synthesis

(B) Suramin,-First line treatment of EAST African trypanosomiasis
(without CNS involvement)

(C) Iodoquinol -Mechanism unknown; luminal amebicide used to treat E. histolytica


(E) Pyrimethamine-Treatment of erythrocytic schizonts (malaria)

Front 165

NNRTI

Back 165

NNTRI-Do not require metabolic activation, Directly inhibit reverse transcriptase, Single-drug therapy increases risk of resistance, Rash is most common side effect; cross the BBB, renal and fecal excretion

Front 166

antimetabolites

Back 166

Methotrexate
Mercaptopurine (6-MP)
Cladribine
Fluorouracil
Capecitabine
Cytarabine

Front 167

Protease inhibitor

Back 167

Protease Inhibitors-Bind to the active site of HIV protease, Results in the production of immature, noninfectious viral particles;

SE: breast hypertrophy, central adiposity, hyperlipidemia and insulin resistance---All protease inhibitors can cause disruption of lipid and CHO metabolism

Front 168

thiabendazole

Back 168

disseminated strogyloides

Front 169

fusion inhibitor

Back 169

Inhibits fusion of HIV with host cell, gp120 directs virus to host cell, gp41 fascilitates viral entry

Front 170

pharmacokinetics or oral vs parenteral antibiotics

Back 170

they are similar no matter what. a few exceptions for IV

Front 171

drug that is a fusion inhibitor

Back 171

enfurvirtide

Front 172

Which of the following is the drug of choice for treatment of most major schistosome infections?
Mebendazole, Thiabendazole,
Pyrantel pamoate, Praziquantel

Back 172

Mebendazole-nematode infections like ascariasis and trichuriasis; toxic—GI distress and dizziness

Thiabendazole-Disseminated strongyloides

Pyrantel pamoate-Alternate for albendazole and mebendazole (nematode infections like ascariasis, pinworm and hookworm

***Praziquantel-Trematode infections; increases calcium permeability leading to paralysis; adverse effects include GI distress and headache

Front 173

Influenza A and B are effectively treated with oseltamivir and zanamivir. The mechanism of action for these antiviral agents is inhibition of
DNA polymerase,
Reverse transcriptase,
Thymidine kinase,
Neuraminidase,
Viral protease

Back 173

neuramidase---This enzyme on the lipid envelope prevents viral clumping and binding to already infected cells. This interference disrupts infectivity.

DNA polym-acyclovir, famciclovir, valacyclovir, ganciclovir and cidofovir
reverse transcriptase--didanosine, lamivudine, stavudine, zidovudine, efavirenz and nevirapine
TK-Activates several antivirals (i.e., acyclovir, famciclovir, valacyclovir
viral protease--Anti-HIV agents are protease inhibitors

Front 174

MTX

Back 174

Antimetabolite -- Folic acid antagonist Binds catalytic site of dihydrofolate reductase (enzyme); interferes w/ DNA, RNA and prot. synthesis; enters the cell ACTIVATED. ORAL or IV Broad spectrum; esp choriocarcinoma, ALL and meningial metastases. Side effects: myelosuppression (dose limiting due to suppressing good cells as well) and oral ulcers.

Resistance:
↓ drug transport (req's an active process to enter cell)
↓ polyglutamate formation (won't stay IN the cell)
↑ DHFR synthesis
Reduced affinity of DHFR for MTX Polyglutamates are retained in tumor cells --> Longer period of activity.

Leukovorin rescue: to correct overdose; an active folate molecule that bypasses the step "you screwed up".

Front 175

drugs that inhibit DNA polymerase

Back 175

acyclovir, famciclovir, valacyclovir, ganciclovir and cidofovir

Front 176

DOC for filariasis

Back 176

w. bancrofti is diethycarbamazine

Front 177

drugs that inhibit reverse transcriptase

Back 177

didanosine, lamivudine, stavudine, zidovudine, efavirenz and nevirapine

Front 178

when are pharmacokinetics altered? what patients?

Back 178

Renal or hepatic insufficiency, Burns, CF, Elderly, neonates, pregnancy; may need to alter dosing but don’t necessarily HAVE to change

Front 179

thymidine kinase activates?

Back 179

Activates several antivirals (i.e., acyclovir, famciclovir, valacyclovir

Front 180

drug that causes mazzotti reaction

Back 180

ivermectin

Front 181

The most common mechanism of HSV resistance to acyclovir is

Structural change in viral TK,
Mutation in DNA pol gene,
Loss of ability to produce TK,
Structural change in reverse transcriptase



Mutation in gene that encodes for phosphotransferase

Back 181

usually very few have structural changes or mut DNA polymerase

most lose the ability to synthesize TK
Viral specific thymidine kinase needed to activate acyclovir, which inhibits DNA polymerase.

Front 182

leukovorin rescue

Back 182

for MTX
to correct overdose; an active folate molecule that bypasses the step "you screwed up".

Front 183

An AIDS patient is being treated with a combination of the drugs listed below. Which of these is most likely to cause breast hypertrophy, central adiposity, hyperlipidemia and insulin resistance?

Zidovudine
Atazanavir
Ketoconazole
Sulfamethoxazole
Trimethoprim

Back 183

atazanavir---All protease inhibitors can cause disruption of lipid and CHO metabolism

zidovudine--Bone marrow suppression, anemia and neutropenia
ketoconazole-Antifungal; nausea, rash, hepatic injury and hematopoetic toxicity
SMX--Antibacterial; nausea, rashes, headache and hematologic disorders
TMP--Antibacterial; nausea, rashes, hematologic disorders

Front 184

drug causing flaccid paralysis

Back 184

activates glutamate, enhance GABA, cl influx hyperpolarizaiton
ivermectin

Front 185

side effect of PI

Back 185

SE: breast hypertrophy, central adiposity, hyperlipidemia and insulin resistance---All protease inhibitors can cause disruption of lipid and CHO metabolism

Front 186

what happens when vancomycin and penecillins are given with an aminoglycoside?

Back 186

synergystic effect instead of just bacteriostatic also bacteriocidal

Front 187

drug that causes spastic paralysis

Back 187

inc Ca permeability
praziquantal

Front 188

mercaptopurine

Back 188

Antimetabolite -- Purine Antagonist Req's activation by HGPRT to nucleotide form; inhibits several enzymes in purine nucleotide pathway ORAL Primarily to maintain remission of ALL; also to treat AML and CML Side effects:
Hyperuricemia assoc. w/ cell lysis.

Resistance:
Due to decreased HGPRT activity. Metabolized by xanthine oxidase.

Allopurinol (xanthine oxidase inhibitor) treats the acute gout and prevents nephrotoxicity.
MP6 + allopurinol = decreased dose of MP6 (since XO usually prevents toxicity of MP6)

Front 189

DOC strongyloidiasis in the intestines

Back 189

ivermectin

Front 190

name the cell wall synthesis inhibitors

Back 190

Penicillins, β-lactamase inhibitors*, Cephalosporins, Monobactams, Carbapenems

Front 191

DOC disseminated strongyloidiasis

Back 191

thiabendazole

Front 192

cladribine

Back 192

Antimetabolite -- Purine Antagonist Phos by a kinase; resistant to adenosine daminase, so reaches high intracellular concentrations (accumulation of toxic deoxynucleotide); incorporates into DNA causing strand breaks. -- Hairy cell leukemia; other lymphomas and leukemias.

Front 193

Drugs that inhibit microtubule synthesis

Back 193

albendazole and mebendazole and thiabendazole

Front 194

PBP

Back 194

Penicillin-binding proteins (PBP); NOT static; collective term for bacterial enzymes responsible for assembly, maintenance and regulation of the peptidoglycan portion of the cell wall, β-lactam Abs covalently bind PBP, Inhibition of PBP-1 prevents cross-linking of peptidoglycan, whereas, inhibition of PBP-2 results in loss of rod shape

Front 195

DOC lice and mites

Back 195

permethrin

Front 196

5-FU

Back 196

fluorouricil
Pyrimadine antagonist 3 active metabolites:
FdUMP: complexes with thymidylate synthase to inhibit DNA synthesis. thymidylate is not synthesize so DNA synthesis is inhibited.
FdUTP: incorporates into DNA to inhibit DNA synthesis
FUTP: interferes with RNA processing. no RNA or mRNA for translation
In short: 2 DNA, 1 RNA --
Colorectal cancer

Front 197

alternate for lice and mties

Back 197

malathion

Front 198

peptidoglycan

Back 198

-Linear strands of two alternating amino sugars which are crosslinked by a peptide chain.; Linkage is catalyzed by a transpeptidase, Penicillin irreversibly binds at the active site of the transpeptidase , It mimics the residues that would normally bind to this site.
it gives rigid support, portects aginst osmotic pressure

Front 199

SE is paralysis in patient

Back 199

palation inhibits cholinesterase-->paralysis

Front 200

capecitabine

Back 200

Pyrimadine antagonist Enters the tumor, converted to fluorouracil by thymidine phosphorylase. (then same mechanism as fluorouracil-->3 active metabolites: FdUMP: complexes with thymidylate synthase to inhibit DNA synthesis. thymidylate is not synthesize so DNA synthesis is inhibited. FdUTP: incorporates into DNA to inhibit DNA synthesis. FUTP: interferes with RNA processing. no RNA or mRNA for translation
In short: 2 DNA, 1 RNA ----
Solid tumors:
Metastatic breast cancer

fluropyrimidine carbamate prodrug

Front 201

pharmacokinetics of penicillins

Back 201

some are acid stable others are acid labile; Widely distributed, except not typically found in brain, prostatic secretions or intraocular secretion. Enter the CNS when meninges are inflammed.
they rely on the kidney for GFR and RTA; probenicid used to prolong HL

Front 202

Cytarabine
Aka: cytosine arabinoside
Aka: ara-C

Back 202

Pyrimidine antagonist Active agent is AraCTP,
an S-phase-specific antimetabolite that inhibits DNA polymerase, and interferes with chain elongation of DNA and RNA. --
Acute myelogenous leukemia
highly schedule dependent

Front 203

penecillins can NOT be used in what dysfunction/disease

Back 203

renal dysfunction

Front 204

Typically, cells are most resistant to chemotherapeutic agents during which phase of the cell cycle?

G0, G1, G2, M, S

Back 204

G0 Most agents are more effective when cells are proliferating, synthesizing DNA or undergoing mitosis

Non-cell-cycle-specific agents include alkylating agents (cyclophosphamide) and some anti-tumor antibiotics like dactinomycin and doxorubicin.

Front 205

what is used to prolong HL in penicillins?

Back 205

probenecid

Front 206

An adult female with choriocarcinoma is treated with high dose methotrexate (MTX). What agent should be administered to reduce host cell toxicity?

Back 206

Leucovorin rescue

MTX is a folic acid analog (antimetabolite) which inhibits dihydrofolate reductase (enzyme needed for optimal nucleic acid synthesis). MTX is not taken up well by cancer cells so high doses are used to “drive” it into the cells.

Leucovorin enters normal cells well, bypasses the MTX block and spares metabolism. Cancer cells are not spared because they do not readily take up leucovorin.

Front 207

name 2 long acting penecillins for IM

Back 207

Procaine penicillin G and benzathine penicillin G

Front 208

While reading your charts you notice you have another patient on MTX. However, this patient is cancer free and the dose of MTX is relatively low. Do you recall why you are treating this patient with MTX?

Back 208

Yes, Rheumatoid arthritis (or maybe psoriasis)

Front 209

side effects of penicillin

Back 209

Hypersensitivity-Degradation products of penicillin combine with protein to form antigenic compounds; IgE mediated response
Rash , Nephritis, Serum sickness, Anaphylactic shock

Front 210

Concurrent treatment with allopurinol will most likely increase the toxicity of which of the agents? Why?

Bleomycin
Cisplatin
Cyclophoshamide
Doxorubicin
Mercaptopurine

Back 210

Allopurinol inhibits XO
XO metabolizes mercaptopurine

Front 211

why are cephalosporins better than penicillins?

Back 211

More stable than penicillins (highly resistant to penicillinase) and less likely to cause hypersensitivity reactions,
Renal excretion-Except ceftriaxone which is excreted in bile; dose modification in renal dysfucntion

Front 212

plant alkaloids

Back 212

Vinblastine
Vincristine
Etoposide
Topotecan
Paclitaxel

Front 213

Divided into 4 generations based on antimicrobial spectrum cephalosporins

Back 213

1st primarily active against most gram-positive cocci (not MRSA or enterococci) and some gram-negative organisms; 2nd-4th increased activity against Gram-negative bacilli

; as inc generation inc effect and strength against bugs

Front 214

vinca alkaloids

Back 214

bind tubulin, block polymerizaiton of MT; no assembly

Front 215

cephalosporin Cross-sensitivity w/ penicillins

Back 215

-If mild reaction to penicillin then cephalosporins usually tolerable, If severe reaction to penicillin then cephalosporins contraindicated

Front 216

taxanes

Back 216

block dissassembly
binds MT to enhance polymerizations

Front 217

how do bacteria get resistance to B lactams?

Back 217

structural differences in PBPs, recombination of PBP genes of different species resulting in PBPs with low affinity for antibiotic; Efflux pumps; ↓ entry of the drug into bacteria through the outer membrane porins-In gram-negative bacteria the PBP are very near the cell surface thus more readily accessible , In gram-negative bacteria the outer membrane is often an impenetrable barrier to some antibiotics. However, hydrophilic antibiotics diffuse through aqueous channels created by proteins called porins.
P aeruginosa is intrinsically resisitant to many antibiotic b/c of a relatively low number of hightly-perimeable porins

Front 218

vinblastine

Back 218

Vinca alkaloid Binds tubulin to block polymerization of microtubules;
Mitotic arrest in metaphase. -- Hodgkin’s
Non-Hodgkin’s
lymphoma
Breast cancer -- MYELOSUPPRESSIVE

Front 219

penicillin G

Back 219

Narrow Spectrum Penicillin Cell wall synthesis inhibitor; IRREVERSIBLY binds the active site of transpeptidase Acid-stable in large doses (oral)
Think Gram (+); CNS when meninges inflamed
Use with 3rd gen. cephalosporin or vancomycin until sure of PCN-sensitivity.

Hypersensitivity: degradation products of PCN combine w/protein = IgE mediated response w/rash, nephritis, serum sickness, Anaphylactic shock Elimination=kidneys

Used in elderly due to lower acid content
treats: Syphilis (Treponema pallidum) spirochete ; Meningitis (Meningococci) (-); Pneumonia (Pneumococci) (+)

Front 220

vincristin

Back 220

Vinca alkaloid Block polymerization of microtubules -- KIDS:
ALL
Ewing’s sarcoma
Wilm’s tumor

Blood malignancies (H and non-H) -- NEUROTOXIC
--numbness/tingling in extremities

Front 221

penicillin V

Back 221

Narrow Spectrum Penicillin Cell wall synthesis inhibitor;
IRREVERSIBLY binds the active site of transpeptidase Acid-stable (oral) Think Gram (+)
CNS when meninges inflamed Hypersensitivity reaction Elimination=kidneys
treats: Pharyngitis (Streptococcus pyogenes) (+)

Front 222

paclitaxel

Back 222

Taxane Binds microtubules to enhance polymerization (good tubules that don’t break apart, and also makes faulty microtubules) -- Solid tumors (Note: NOT leukemias) Side effect: neutropenia Liver metabolization
Excreted in feces

Front 223

procaine Penicillin G

Back 223

Long-acting combination; penicillin; Cell wall synthesis inhibitor;
IRREVERSIBLY binds the active site of transpeptidase; Combined with Probenecid; competes w/ penillin for organic acid transporter IM
treat: Think Gram (+);
CNS when meninges inflamed Hypersensitivity reaction Elimination=kidneys

Front 224

etoposide

Back 224

Taxane Cell cycle specific: late S-G2 phase;
Inhibits topoisomerase II  DNA strand breakage -- Variety:
Germ cell cancer
Lung cancer
Hematologic malignancies
Gastric cancer Relies on P-glycoprotein; increase efflux is mode of resistance.

Side effects: nephrotoxic (reduce dose in renal insuff)
Leukopenia is dose limiting. No CNS.

Front 225

benzathine penicillin G

Back 225

Long-acting combination Penicillin Cell wall synthesis inhibitor; IRREVERSIBLY binds the active site of transpeptidase; Combined with Probenecid; competes w/ penillin for organic acid transporter IM
tx: Think Gram (+);
CNS when meninges inflamed Hypersensitivity reaction Elimination=kidneys

Front 226

topotecan

Back 226

Taxane Inhibits topoisomerase I so that DNA is not cut or re-ligated. -- Ovarian cancer (when platinum agents fail: cisplatin, carboplatin, oxaloplatin) -- Renal excretion

Front 227

diclocillin

Back 227

Penicillinase resistant Penicillin IRREVERSIBLY binds the active site of transpeptidase; Acid stable (ORAL)
tx: Think Gram (+);
Osteomyelitis (Staphylococci);
Endocarditis (Staphylococci);
Skin/soft tissue infections (Staphylococci) Less effective than other PCNs; Use ONLY if bugs make penicillinase (PCN-resistant; MRSA)
Hypersensitivity reaction Elimination=kidneys;
Vancomycin is DOC for PCN-resistant bugs;
NOT for GRAM (-)

Front 228

antineoplastic antibiotics

Back 228

Doxorubicin
Daunorubicin
Dactinomycin
Mitomycin
Bleomycin

Front 229

nafcillin

Back 229

Penicillinase resistant Penicillin IRREVERSIBLY binds the active site of transpeptidase; PARENTERAL (IV) acid labile
tx: Think Gram (+);
Osteomyelitis (Staphylococci);
Endocarditis (Staphylococci);
Skin/soft tissue infections (Staphylococci) Less effective than other PCNs
Use ONLY if bugs make penicillinase (PCN-resistant; MRSA);
Hypersensitivity reaction Elimination=kidneys and BILE;
Vancomycin is DOC for PCN-resistant bugs; NOT for GRAM (-)

Front 230

doxorubicin

Back 230

Antibiotic 4 Mechanisms:
Inhibition of Topoisomerase II
Bind DNA/inhibits synthesis
Bind cell membrane/alters
fluidity and ion transport
Generation of ROS
(bold items differentiate this from etoposide) -- Broad spectrum:
Hematologic malignancies
Solid tumors (Breast, endometrium, cervical)

Front 231

amoxicillin

Back 231

Aminopenicillin; Extended spectrum Penicillin IRREVERSIBLY binds the active site of transpeptidase; Acid stable (oral) Otitis;
Upper Respiratory Tract infection
(S. pneumoniae and
H. influenza) MOST ACTIVE oral β-lactam against PCN-resistant S. pneumonia;
Hypersensitivity reaction Elimination=kidneys

Front 232

daunoribicin

Back 232

Antibiotic 4 Mechanisms:
Inhibition of Topoisomerase II
Bind DNA/inhibits synthesis
Bind cell membrane/alters
fluidity and ion transport
Generation of ROS
(bold items differentiate this from etoposide) -- Acute myeloid leukemia

Front 233

ampicillin

Back 233

Aminopenicillin; Extended spectrum Penicillin; IRREVERSIBLY binds the active site of transpeptidase; ORAL
tx: Meningitis (L. monocytogenes in immunocompro-mised)
NOTE: When caused by S.pneumonieae (like in kids), tx. requires a cocktail. Hypersensitivity reaction Elimination=kidneys and BILE

Given in cocktail with vancomycin and 3rd gen. cephalosporin.

If a rash appears with tx, think MONO.

Front 234

dactinomycin

Back 234

Antibiotic Binds DNA to inhibit RNA synthesis -- KIDS:
Rhabdomyosarcoma
Wilm’s tumor

Front 235

piperacillin

Back 235

Anti-pseudomonal; Extended spectrum Penicillin; IRREVERSIBLY binds the active site of transpeptidase Acid labile (parenteral)
tx: GRAM (-) BUGS, Lyme disease; Nosocomial pneumonia (P.aeruginosa); Bite wounds (often combined w/β-lactamase inhibitor like clavulanate, sulbactam, tazobactam)
Hypersensitivity reaction Elimination=kidneys

Front 236

mitomycin

Back 236

Antibiotic Metabolized to an alkylating agent w/crosslinking of DNA -- Hypoxic tumor stem cell: oral cavity (lip, mouth, etc.), pharynx, GI and bladder.
***says breat cancer combo vincristine only??!?!?!

Front 237

ticarcillin

Back 237

Extended spectrum Penicillin; IRREVERSIBLY binds the active site of transpeptidase; Acid labile (parenteral)
Hypersensitivity reaction Elimination=kidneys

tx gram - bugs mainly Pseudomonas

Front 238

bleomycin

Back 238

Antibiotic Cell cycle specific: G2
Peptide w/DNA binding region and IRON binding domain; iron becomes oxidized leading to damage to DNA and proteins. -- Broad spectrum Renal excretion so decrease dose in renal insuff.

Front 239

clavulanate

Back 239

β-lactamase inhibitor Irreversibly bind β-lactamases to inactivate them.
Amoxicillin + clavulanate= augmentin inc effectiveness

Do not mix w/ cephalosporins???
---these agents irrev bind B lactam prod by wide range of bact. Active against plasmid encoded BMS including the extended spectrum BLMs that hydrolyze ceftazidime and ceftaxime (3rd gen.), Inactive against type I chromosomal BLMs induced in Enterobacter, Acinetobacter and Citrobacter by 2nd & 3rd gen. cephalosporins.

Front 240

tamoxifen

Back 240

Hormonal agent: Antisteroid agent Binds estrogen receptor of estrogen-dependent tumors; estrogen stimulates the cytokine, TGF-β which has an autocrine fxn on tumor cells (this drug blocks this process) -- Breast cancer NOTE: endogenous estrogens must be ablated Works best for post-menopausal women.

***less affinity than estrodial so must ablate estrogen

Front 241

sulbactam

Back 241

β-lactamase inhibitor Ampicillin + sulbactam
Irreversibly bind β-lactamases to inactivate them. inc effectiveness
Do not mix w/ cephalosporins???
---these agents irrev bind B lactam prod by wide range of bact. Active against plasmid encoded BMS including the extended spectrum BLMs that hydrolyze ceftazidime and ceftaxime (3rd gen.), Inactive against type I chromosomal BLMs induced in Enterobacter, Acinetobacter and Citrobacter by 2nd & 3rd gen. cephalosporins.

Front 242

flutamide

Back 242

Hormonal agent: Antisteroid agent A nonsteroidal agent that binds androgen receptor for antiandrogen effects; prevents translocation of receptor from cytosol to the nucleus; so no transcription factor activity. -- Prostate cancer

Front 243

tazobactam

Back 243

Piperacillin + tazobactam
Irreversibly bind β-lactamases to inactivate them.
Do not mix w/ cephalosporins???
---these agents irrev bind B lactam prod by wide range of bact. Active against plasmid encoded BMS including the extended spectrum BLMs that hydrolyze ceftazidime and ceftaxime (3rd gen.), Inactive against type I chromosomal BLMs induced in Enterobacter, Acinetobacter and Citrobacter by 2nd & 3rd gen. cephalosporins.

Front 244

leuprolide

Back 244

Hormone agonist Analog of GnRH; initial increase of LH and FSH leading to desensitization of the receptor and decreased testosterone synthesis results. -- Androgen-receptor positive tumors (prostate)

Front 245

amikacin

Back 245

Aminoglycoside; bacteriocidal
Inhibitor protein synthesis via 30S ribosomal subunit; LOCKS the 2 subunits in place at the start codon = causes misreading of mRNA so premature termination of translation or incorporation of incorrect amino acids.
Parenteral
tx: Aerobic Gram (-) Bacilli;
Used when infection is resistant to other aminoglycosides.
resistant to enzyme inact
Adjust dosing based on creatinine clearance levels;
Blocked by low pH.
Resistant to acetylase, adenylase and phosphorylase.
NEPHROTOXIC: Accumulates in prox. tubules resulting in acute necrosis.
OTOTOXIC: Accumulation in labyrinth and hair cells of cochlea.
Elimination=kidneys
Long post-antibiotic effect.
Does not enter CNS or host cells.
Poorly absorbed.
“A = aerobic”

Front 246

anastrole

Back 246

Hormonal agent: Aromatase inhibitors Nonsteroidal inhibits aromatase; blocks conversion of androgens to estrogen. -- Metastatic breast cancer in post menopausal women Preferred aromatase inhibitor d/t less side effects (a nonsteroidal)

Front 247

gentamicin

Back 247

Aminoglycoside; bacteriocidal
Inhibitor protein synthesis via 30S ribosomal subunit; LOCKS the 2 subunits in place at the start codon = causes misreading of mRNA so premature termination of translation or incorporation of incorrect amino acids.
Parenteral or Topical
tx: Aerobic Gram (-) Bacilli; Most active against Enterobacteriaceae species.
Adjust dosing based on creatinine clearance levels;
Blocked by low pH.
Inactivated by acetylase, adenylase and phosphorylase.
NEPHROTOXIC: Accumulates in prox. tubules resulting in acute necrosis.
OTOTOXIC: Accumulation in labyrinth and hair cells of cochlea.
Elimination=kidneys
Long post-antibiotic effect.
Does not enter CNS or host cells.
Poorly absorbed.
“A = aerobic”

Front 248

Which of the following is the most likely adverse effect of vincristine?

Nephrotoxicity or renal dysfunction
Neutropenia
Peripheral neuropathy
Pulmonary damage
Bleeding

Back 248

Vincristine is rather unique in that it does not cause bone marrow suppression (Vinblastine and vinorelbine do)

Neuropathies
sensory: parathesias, hearing loss
motor: muscle weakness and obtunded reflexes

Front 249

neomycin

Back 249

Aminoglycoside; bacteriocidal
Inhibitor protein synthesis via 30S ribosomal subunit; LOCKS the 2 subunits in place at the start codon = causes misreading of mRNA so premature termination of translation or incorporation of incorrect amino acids.
TOPICAL only most nephrotoxic
tx: Aerobic Gram (-) Bacilli;
Limited to TOPICAL treatments.
Adjust dosing based on creatinine clearance levels; Blocked by low pH. Inactivated by acetylase, adenylase and phosphorylase.
NEPHROTOXIC: Accumulates in prox. tubules resulting in acute necrosis. OTOTOXIC: accumulation in labyrinth and hair cells of cochlea.
Elimination=kidneys
Long post-antibiotic effect.
Does not enter CNS or host cells.
“A = aerobic”

Front 250

Which of the following is most likely to cause irreversible cardiomyopathy as a result of toxicity?

Bleomycin
Cisplatin
Cyclophoshamide
Doxorubicin
Vincristine

Back 250

doxorubicin

Cisplatin- renal toxicity
Bleomycin- pulmonary toxicity
Cyclophosphamide- toxic to bone marrow, gut mucosa and hair follicles
Vincristine- peripheral nerve damage

Front 251

streptomycin

Back 251

Aminoglycoside; bacteriocidal
Inhibitor protein synthesis via 30S ribosomal subunit; LOCKS the 2 subunits in place at the start codon = causes misreading of mRNA so premature termination of translation or incorporation of incorrect amino acids.
IM
tx: Aerobic Gram (-) Bacilli;
Least active against Pseudomonas aeruginosa; Multi-drug resistant tuberculosis, plague (Yersinia pestis), and tularemia (Francisella tularensis); “RABBIT HUNTERS”
Adjust dosing based on creatinine clearance levels; Blocked by low pH. Inactivated by acetylase, adenylase and phosphorylase.
NEPHROTOXIC: Accumulates in prox. tubules resulting in acute necrosis. OTOTOXIC: Accumulation in labyrinth and hair cells of cochlea.
Elimination=kidneys
Long post-antibiotic effect.
Does not enter CNS or host cells.
Poorly absorbed.
LEAST toxic of the aminoglycosides
“A = aerobic”

Front 252

exemestane

Back 252

Hormonal agent: Aromatase inhibitors Steroid IRREVERSIBLY inhibits aromatase; -- -- Decrease dose in renal insufficiency.
More steroidal-type side effects.

Front 253

tobramycin

Back 253

Aminoglycoside; bacteriocidal
Inhibitor protein synthesis via 30S ribosomal subunit; LOCKS the 2 subunits in place at the start codon = causes misreading of mRNA so premature termination of translation or incorporation of incorrect amino acids.
Parenteral or topical
tx: Aerobic Gram (-) Bacilli;
Most active against PSEUDOMONUS aeruginosa
Adjust dosing based on creatinine clearance levels; Blocked by low pH. Inactivated by acetylase, adenylase and phosphorylase.
NEPHROTOXIC: Accumulates in prox. tubules resulting in acute necrosis. OTOTOXIC: Accumulation in labyrinth and hair cells of cochlea. Elimination=kidneys
Long post-antibiotic effect.
Does not enter CNS or host cells.
Poorly absorbed.
“A = aerobic”

Front 254

imatinib

Back 254

Other Inhibits the oncoprotein tyrosine kinases that normally promote proliferation and block apoptosis.
High affinity for kinase IN the tumor schedule. -- CML (Bcr-Abl)
GI stromal tumor
(c-kit)

Front 255

tetracycline

Back 255

Tetracycline; bacteriostatic
Inhibitor of protein synthesis via 30S ribosomal subunit; PhYSICALLY BINDS to prevent access of aminoacyl-tRNA to the A site.
Parenteral or oral
tx: Broad spectrum; DOC for Rocky Mtn. Spotted fever (Rickettsia) and Lyme Disease.
Also, Peptic ulcers (H.pylori) Bioavailability is reduced in certain foods (binds divalent cations…Ca, Al and Fe and is deactivated)
DO NOT take w/antacids or Iron supplements, dairy products, etc.
Discoloration of teeth;
Photosensitivity (absorbs UV and looks like sunburn)
Nephrotoxicity; Hepatotoxicity Elimination=kidneys and bile
“T = ticks”

Front 256

asparginase

Back 256

Other Bacterial derived enzyme hydrolyzes L-asparginine; prevents tumor cell from utilizing the asparginine. -- KIDS:
ALL

many tumor cells lack asparagine synthase and require exogenous asparagine-->dec portein synthesis

Front 257

doxycycline

Back 257

Tetracycline; bacteriostatic
Inhibitor of protein synthesis via 30S ribosomal subunit; PhYSICALLY BINDS to prevent access of aminoacyl-tRNA to the A site.
Parenteral or oral
Broad spectrum; DOC for Rocky Mtn. Spotted fever (Rickettsia) and Lyme Disease. Also, Genital infections (Chlamydia) Bioavailability is reduced in certain foods (binds divalent cations…Ca, Al and Fe and is deactivated)
DO NOT take w/antacids or Iron supplements, dairy products, etc.
Discoloration of teeth;
Photosensitivity (absorbs UV and looks like sunburn)
Nephrotoxicity; Hepatotoxicity Elimination=kidneys and bile
NOTE: NOT DEPT ON RENAL EXCRETION!!! (USE in pts with renal dysfxn.)
“T = ticks”

Front 258

sorafenib

Back 258

Mulitkinase inhibitor Inhibits kinases involved in angiogenesis and intracellular signaling. No tumor growth. -- Renal cell carcinoma -- NEW drug

Front 259

minocycline

Back 259

Tetracycline; bacteriostatic
Inhibitor of protein synthesis via 30S ribosomal subunit; PYSICALLY BINDS to prevent access of aminoacyl-tRNA to the A site. Parenteral or oral
Broad spectrum; DOC for Rocky Mtn. Spotted fever (Rickettsia) and Lyme Disease.
Also, acne vulgaris
Effective in CNS and penetrates skin well. Bioavailability is reduced in certain foods (binds divalent cations…Ca, Al and Fe and is deactivated)
DO NOT take w/antacids or Iron supplements, dairy products, etc.
Discoloration of teeth;
Photosensitivity (absorbs UV and looks like sunburn)
Nephrotoxicity; Hepatotoxicity Elimination=kidneys and bile
“T = ticks”

Front 260

nelarabine

Back 260

Prodrug of ara-G; metabolized to ara-GTP; disrupts DNA synthesis and induces apoptosis. -- Lymphoblastic leukemia -- NEW drug

Front 261

what do the inhibitors of protein synthesis do?

Back 261

These agents selectively disrupt bacterial protein synthesis; Differences in bacterial ribosome structure; Differences in bacterial ribosome function
either 30s or 50s
do not directly alter enzyme instead bind to 30 or 50 to prevent appropriate interaction
prevent translocation from A to P site prevents tRNA binding to ribosome

Front 262

lenalidomide

Back 262

Thalidomide analog Anti-angiogenic, anti-inflammatory; enhances T cells and NK cells. -- Myelodysplastic syndromes -- NEW drug

Front 263

are tetracyclines bacteriocidal or static?

Back 263

bacteriostatic

Front 264

immunosuppresive agents

Back 264

Glucocorticoids
Cyclosporine
Tacrolimus
Sirolimus
Interferons
Azathioprine
Antibodies

Front 265

are aminoglycosides bacteriocidal or static?

Back 265

bacteriocidal

Front 266

what are the 30S ribosombal binding drugs?

Back 266

aminoglycosides and tetracyclines

Front 267

what are the 50s ribosomal binding drugs?

Back 267

chloramphenicol, clindamycin, macrolides, mupirocin, streptogramins

CCMMS

Front 268

name the protein synthesis inhibitors

Back 268

aminoglycosides, cholormaphenicol, clindamycin, macrolides, mupirocin, streptogramins, tetracyclines

Front 269

describe aminoglycosidal function

Back 269

glycosidic bond, poorly absorbed in gut, postantibiotic effect, elim in kidneys NOT met in liver;
do not cross CNS

Front 270

adverse effects of aminoglycosides

Back 270

nephrotoxic-prox tubules necrosis
ototoxic

Front 271

tetracycline function

Back 271

bind 30s, prevent tRNA access to A site, bacteriostatic; broad spec; high oral availability unless taken w/ metals or antacids, iron, dairy

Front 272

side effects of tetracyclines

Back 272

discoloration of teeth, photosn (accum under skin and absorbs UV), nephrotoxicity and hepatotoxicity

Front 273

tetracycline that is not dependent on renal

Back 273

doxycylcine

Front 274

tetracycline that can penetrate the CNS and skin

Back 274

minocycline

Front 275

If someone is immunocomprimised what does the drug need to be?

Back 275

bacteriocidal

Front 276

do not take tetracyclines w/ what?

Back 276

trace metals Fe, Ca, Al
antacids, dairy ect

Front 277

Which of the following agents is most active against Pseudomonas aeruginosa? Ampicillin, Penicillin G, Penicillin V, Nafcillin, Piperacillin

Back 277

piperacillin

Front 278

An adult female is admitted to the hospital with endocarditis caused by a penicillinase-producing Staphylococcus aureus infection and requires parenteral therapy. Which of the following agents is indicated? Ampicillin, Amoxicillin , Dicloxacillin, Nafcillin, Penicillin G

Back 278

nafcillin---parenteral
other choice but oral is dicloxacillin

Front 279

what are b lactamases

Back 279

kill penicillins they are enzymes against them even destroy extended specrum like amoxicillin

penicillinase is a specific B lactamase

use clavulonate, sulbactam and lazobactam to be a BLI!!!

Front 280

Drugs that affect the 50S Ribosomal Subunit

Back 280

Drugs that affect the 50S Ribosomal Subunit--Macrolides , Ketolides , Chloramphenicol , Clindamycin , Quinupristin-Dalfopristin
Linezolid

Front 281

macrolides

Back 281

50S ribosomal subunit and prevent TRANSLOCATION of the nascent peptide from the A site (aminoacyl site) to the P site (peptidyl site). This blockade inhibits binding of the next aminoacyl tRNA to the ribosome.
ORAL
Absorption and activity of erythromycin is reduced by gastric acid.
--Azythromycin and clarithromycin are more readily absorbed, have a longer t1/2 and achieve higher tissue concentrations. These two drugs are less likely to cause GI distress
Excretion-Bile and urine;

Front 282

azithromycin

Back 282

Macrolide Inhibitor of protein synthesis via 50S ribosomal subunit; prevents translocation of nascent peptide from A to P site. Incoming tRNA can’t bind.
Oral
URTi and pneumonia, esp: Chlamydia, H. influenza, *otitis media, *sinusitis; M. pneumonia
L. pneumonia; Generally for all macrolides: Streptococci
Pneumococci; BORDATELLA DOC!!!!
Little effect on CYP3A4 Elimination=Kidney and bile;
More readily absorbed, longer ½ life, higher tissue concentrations.

**less GI distress DOC if P450 drug intx

Front 283

clarithromycin

Back 283

Macrolide
Inhibitor of protein synthesis via 50S ribosomal subunit; prevents translocation of nascent peptide from A to P site. Incoming tRNA can’t bind.
Oral
URTi and pneumonia, esp:
****DOC H. pylori ; Generally for all macrolides: Streptococci, Pneumococci
CYP3A4 inhibition = possible toxicity of other drugs (esp. statins) Elimination=Kidney and bile;
****More readily absorbed, longer ½ life, higher tissue concentrations.

Front 284

erythromycin

Back 284

Macrolide Inhibitor of protein synthesis via 50S ribosomal subunit; prevents translocation of nascent peptide from A to P site. Incoming tRNA can’t bind.
Oral
URTi and pneumonia:
neonatal chalmydia eye drops, DOC legionella
Streptococci, Pneumococci Absorption reduced by gastric acid = gastric distress;
CYP3A4 inhibition = possible toxicity of other drugs (esp. statins)
Elimination=Kidney and bile

Front 285

telithromycin

Back 285

Ketolide
Similar to macrolides; 2 separate binding sites on 50S subunit.
Oral w/o regard to food
Acute sinusitis, acute exacerbations of chronic bronchitis by S. pneumonia and H. influenza
Adverse effects: Nausea, diarrhea, prolonged Q/T interval, impairs visual accomodation
CONTRAINDICATION: don’t take with antiarrythmics

More stable to stomach acid; don’t have to take w/food. Long ½ life (10 h); Less susceptible to bacterial export pumps.

METHYLASE DOES NOT INACTIVATE!!!

Front 286

which macrolide has reduced absorption?

Back 286

erythromycin

Front 287

which 2 macrolides have CYP3A4 inhibition?

Back 287

clarithromycin and erythromycin

Front 288

route of preparation for macrolides

Back 288

oral

Front 289

clindamycin

Back 289

Inhibitor of protein synthesis via 50S ribosomal subunit by binding peptidyltransferase site and preventing transpeptidation; incoming tRNA can’t bind (same as macrolide) Parenteral,
Topical or Oral
Penicillin-resistant Streptococci
Anaerobic bacteria:
Bacteriodes fragilis
Clostridium perfringens High risk of GI SUPERINFECTION (Clostridium dificile growth enhanced…fatal diarrhea) – stop tx and give metronidazole or vancomycin
Pseudomembranous colitis Elimination=kidney and bile

DOES not enter CNS

Front 290

chloramphenicol

Back 290

Inhibitor of protein synthesis via 50S ribosomal subunit (MOA same as clindamycin) Parenteral,
Topical or Oral
Broad spectrum of meningitis:
Pneumococci
Meningococci
H. influenzae Neonates deficient in glucuronosyl-transferase so DECREASE dosage;
Anemia d/t inhibition of iron incorporation into heme.
Gray baby syndrome Elimination=kidney (after glucuronate conjugation)
Enters CNS

Front 291

quinupristin-dalfopristin

Back 291

Streptogramin Inhibitor of protein synthesis via 50S ribosomal subunit.
Synergistic effect: Q inhibits synthesis of tRNA (prevention of add’n to new peptide chain), and D inhibits peptidyl transferase (blocks formation of peptide bond). Parenteral NASTY BUGS (but not CNS)
Vancomycin-resistant organisms or if pt. has red-man syndrome. Inflammation of veins;
Arthralgia;
Myalgia;
Diarrhea

Think “vancomycin-resistant”

Front 292

linezolid

Back 292

Oxazolidine-diones Inhibitor of protein synthesis by binding the 23S ribosomal RNA of the 50S ribosomal subunit. (Prevents formation of 70S initiation complex) Parenteral or oral NASTY BUGS
Aerobic Gram (+):
Vancomycin-resistant E. faecium
MRSA Cross-resistance with other drugs unlikely due to unique MOA. Oral bioavailability is 100%; 30% excreted in urine unchanged.

Front 293

mupirocin

Back 293

Inhibitor of protein synthesis via 50S ribosomal subunit. Side chain mimics isoleucine so competes for isoleucine tRNA synthetase. Topical Most Staphylococci
First effective topical tx. for impetigo (staphylococci or streptococci) Cross-resistance with other drugs unlikely due to unique MOA.

Front 294

what infection can clindamycin CAUSE?

Back 294

C. diff

Front 295

what metabolizes chloramphenicol?

Back 295

glucuronosyl-transferase

Front 296

what treats vancomycin-resistant organisms?

Back 296

quinupristin dalfopristin

Front 297

topical drug for staph and strep?

Back 297

mupirocin

Front 298

. inactivation of aminoglycosides by

Back 298

by acetylase, adenylase and phosphorylases,

Front 299

fluroquinolones and rxns to other molecules

Back 299

Chelate divalent and trivalent cations, Inhibit the metabolism of caffeine, Reduce caffeine intake to reduce CNS stimulation

Front 300

mycobacterial infections describe and name

Back 300

Obligate aerobes, Thrive in oxygen rich tissues (i.e., lung); Intracellular pathogens-macrophage, Hydrophobic with high lipid (mycolic acid) content in the cell wall, Tuberculosis-Mycobacterium tuberculosis( risk of infection is particularly high in immunocomprimised pt); Atypical -mycobacterial infections, Mycobacterium kansasii, Mycobacterium avium-intracellular complex (MAC) –prophylaxis in AIDS pts; Leprosy-Mycobacterium leprae

Front 301

isoniazid

Back 301

Nicotinic acid derivative, Oral preparation, widely distributed following absorption, Extensively metabolized, Key metabolizing enzyme is acetyltransferase (japanese fast, middle eastern slow, US-50/50), Rate of activity is genetically determined
Antimycobacterial Activity-M. tuberculosis-Newly diagnosed (isoniazid will be included in treatment), Exposed neonates or children (isoniazid alone, 3 mo), Latent tuberculosis in TST positive patients that meet one of the following criteria: (isoniazid alone, 9 mo)
HIV+, Chest x-ray indicates non-progressive tuberculosis, IV drug user, Diabetes, Immunocompromised; Active TB: Isoniazid, rifampin, ethambutol and pyrazinamide (with PZA therapy can be reduced to 6 months); INH is effective against some strains of M kansaii NOT MAI or M leprae
Mechanism of Action-Inhibits synthesis of mycolic acid , Mycobacterial cell wall component, Isoniazid is activated by mycobacterial catalase-peroxide (encoded by the katG gene), An isoniazid-enzyme complex is formed which subsequently inhibits enoyl reductase
Enoyl reductase is instrumental in mycolic acid synthesis; Resistance-Mutation in katG; Adverse effects-Hepatitis (risk increases with age), Monitor serum transaminase levels ; Peripheral neuritis-Parathesias Numbness in fingers and toes, Due to drug induced inactivation of vitamin B6 (pyridoxine), Prevent with vitamin supplements

Front 302

what does the mutation in isonizid do?

Back 302

kat G inhibits catalyase to prevent activation so can't inhibit enoyl reductase

Front 303

key metablizing enzyme in isoniazid

Back 303

acetyltransferase

Front 304

what are some side effects of isoniazid?

Back 304

hepatitis, peripheral neuritis (vit B6), hemolysis in G6PD

Front 305

isoniazid

Back 305

First line anitmycobacterial for TB Inhibits synthesis of mycolic acid (cell wall component); Activated by mycobacterial catalase-peroxide forming a complex that inhibits enoyl reductase. Oral M. tuberculosis
-Newly diagnosed
-Exposed neonates or kids (prophylaxis)
-Latent TB in tuberculin skin test (+) pt w/one of the following:
HIV, (+) chest xray, IV drug user, DM, immunocompromised.
Some M. kansasii
KEY: CHRONIC ds; reqs extended tx. Resistance: mutation in katG gene (encodes catalse-peroxide)

Hepatitis (risk increases w/age)
Peripheral neuritis (paresthesias, numbness due to inactivation of Vit. B6

Given as the essential ingredient of a COCKTAIL. Nicotinic acid derivative

Key metabolizing enzyme: acetyltransferase
(Note: rate is genetically determined)

NOT M. avian-int OR M. leprae

9 mo-1 drug for prophylaxis; B6 prevents neuropathy; fast acetylator clears faster
hemolysis in G6PD

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ethambutol

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First line anitmycobacterial for TB Two targets: Inhibits RNA synthesis and arabinosyl transferase (necessary for cell wall synthesis) Oral Tuberculous meningitis
(M. tuberculosis and M.avium-intracellulare Optic neuritis;
Impaired red/green discrimination  CONTRAINDICATED in kids <5;
Gout
Thrombocytopenia
Used as a COCKTAIL. Butanol derivative
CNS penetration
80% absorbed in the gut; 75% of that excreted unchanged in urine;
Doesn’t req. activation

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pyrazinamide

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First line anitmycobacterial for TB Converted to pyrazinoic acid (the active form) by pyrazinamidase, reducing the pH. (Disrupts mb. energetics and transport fxns.) Oral Tx of M. tuberculosis Gout
Hematologic toxicity
Hepatitis
Elevated Serum Iron
Myalgia, phototoxicity, rash
COCKTAIL w/other first line drugs Nicotinamide derivative
CNS penetration

THINK: “P=pH”

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rifampin

Back 308

First line anitmycobacterial for TB Active metabolite is deacetylrifampin; Binds DNA-dependent RNA polymerase. Result is inhibition of DNA transcription. Oral Broad spectrum; ALL 4!
M. tuberculosis, M.avium-intercellulare, M.kansasii, and M.leprae Hepatotoxicity, flu-like illness, red-orange discoloration of fluids.
Resistance d/t dec’d affinity of enzyme for drug;
COCKTAIL w/other first line drugs;
Significant drug interactions d/t inducing hepatic enzymes (Ex. OC, anti-HIV drugs, digoxin, halothane, corticosteroids, propanalol, oral anticoagulants.) Elimination = kidney and bile.
Significant enterohepatic recycling Converted to active metabolite in the liver.
Crosses BBB

THINK: “R=RNA polymerase”
INDUCES P450

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name the combo treatment for TB

Back 309

Isoniazid, rifampin, ethambutol and pyrazinamide (with PZA therapy can be reduced to 6 months)

Front 310

MOA of isonizid

Back 310

inhibits mycolic acid but needs to be activated by catalyse
enoyl reductase assists w/ forming complex

Front 311

adverse effects of isoniazid

Back 311

Hepatitis (risk increases with age), Monitor serum transaminase levels ; Peripheral neuritis-Parathesias Numbness in fingers and toes, Due to drug induced inactivation of vitamin B6 (pyridoxine), Prevent with vitamin supplements

Front 312

ethambutol treats vs isonizid?

Back 312

tuberculous meningitis (M Tb, and MAC) vs TB and some M. kansasaii

Front 313

drug that induces P450

Back 313

rifampin

Front 314

bacteria that rifampin treats

Back 314

all 4!!! M tb, MAC, m kansaii, and M leprae

Front 315

rifabutin

Back 315

Second line anitmycobacterial for TB Similar to Rifampin; Inhibits DNA-dependent RNA polymerase -- Tx of TB in HIV-positive or immunosuppressed pts.

Front 316

cycloserine

Back 316

Second line anitmycobacterial for TB Inhibits cell wall synthesis

Front 317

capreomycin

Back 317

Second line anitmycobacterial for TB Peptide that disrupts protein synthesis  abnormal protein products alter mycobacterial cell wall fxn. Parenteral -- Nephrotoxicity
Ototoxicity
Requires close monitoring

Front 318

ethionamide

Back 318

Second line anitmycobacterial for TB Inhibits acetylation of isoniazid
-- Enhance isoniazid fxn. -- Isoniazid analog

Front 319

dapsone

Back 319

Inhibits folic acid synthesis (similar to sulfonamides) -- Tx of Leprosy (M.leprae) Used in COCKTAIL with RIFAMPIN;
Hemolytic anemia common in G6PD deficient pt.

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clofazimine

Back 320

Preferentially binds mycobacterial DNA, disrupts DNA replication

Slowly bactericidal to M. leprae
Anti-inflammatory properties prevent erythema nodosum leprosum (a Type II H.S. rxn) GI irritation
Photosensitivity, Skin discoloration
Hepatitis Elimination=feces (unchanged)
Does NOT enter CNS
Very LONG ½ life: 70 days

Front 321

combo treatment for MAC

Back 321

Azithromycin (or Clarithro-mycin) + ethambutol + rifabutin

Front 322

combo prophylaxis for MAC

Back 322

Azithromycin (weekly) or Clarithromycin daily

Front 323

name the 2nd line TB drugs

Back 323

rifabutin, cycloserine, capreomycin, ethionamide,
FLUORQUINOLONES

Front 324

Aminosalicylic acid

Back 324

Inhibits folate biosynthesis by competitively inhibiting p-aminobenzoic acid (PABA)
Poorly tolerated, infrequently used

Front 325

with rifampin or isoniazid resistance in TB what replaces them?

Back 325

fluoroquinolone

Front 326

Mycobacterium tuberculosis

Back 326

First-line drugs—Isoniazid, Ethambutol, Pyrazinamide, Rifampin, 2nd line—rifabutin, fluroquinolones, cycloseirne, capreomycin, ehtionamide, aminosalysylic acid w/ rifampin restiance—isoniazid, pyrazinamide, ethambutol, fluorquinolone; w/ isoniazid resistance rifampin, pyrazinamide, ethambutol, fluorquinolone;

Isoniazid + rifampin + pyrazinamide + ethambutol

Front 327

Mycobacterium avium intracellulare

Back 327

Prophylaxis-azithromycin-weekly; clarithromycin daily; tx-azithromycin + ehtambutol + rifabutin

Front 328

Mycobacterium leprae

Back 328

Tubuculoid-dapsone + rifampin; lepromatous-dapsone +rifampin + clofazimine

Front 329

Which antimalarial drug may cause hemolytic anemia in persons with low levels of glucose-6-phosphate dehydrogenase?

didanosine, nifurtimox, chloroquine, primaquine, doxycycline

Back 329

primaquine--Hemolysis is an issue with this drug; effective against liver forms and is gametocidal
chloroquine--GI distress
didanosine-NTRI used to treat HIV infection; pancreatitis and peripheral neuropathy
nifurtimox--Treatment of Chagas’ disease (American trypanosomiasis); Gi distress
doxyclycline---erythrocytic malaria

Front 330

Which drug inhibits exo-erythrocytic (pre-erythrocytic) schizogony and prevents relapse of malaria due to Plasmodium vivax?

primaquine, chloroquine, mefloquine, pyrimethamine, tetracycline

Back 330

primaquine---Active against liver forms and gametocytes; prevent reemergence of organisms from liver

CQ-Drug of choice for prophylaxis, but a blood schizonticide
mefloquine-Used in chloroquine-resistance
pyrimethamine--A folate reductase inhibitor also used to treat toxoplasmosis
tetracycline--blood schizonticide, as are doxycycline, clindamycin and azithromycin

Front 331

CQ resistant drugs for treatment

Back 331

malarone, MQ or doxycycline

Front 332

prophylaxis for malaria

Back 332

CQ or malarone (atovaquone-proguanil)....alt doxy or MQ

Front 333

amebiasis

Back 333

Amebiasis (protozoan): Infection with Entamoeba histolytica, Asymptomatic intestinal infection, Mild to moderate colitis, Severe intestinal infection (dysentery); Liver abscess
--ingest cysts, -->form trophozoites (treat w/ luminal amebasides diloxanide furoate, todoquinol, paromomycin sulfate)-->penetrate intestinal wall-->multipicaiton of trophozoites in colon wall (tx w/ systemic amebiacides chloroquine, dehydroemetine, emetine)-->systemic invasion esp liver-->cysts discard in feces

metronidazole does mixed intestinal and systemic activity

Front 334

Giardiasis treat w/

Back 334

Nitazoxanide
Tinidazole

Front 335

trypansomiasis treat w/

Back 335

Suramin, Melarsoprol, Pentamidine
Eflornithine, Nifurtimox

Front 336

Leishmaniasis treat w/

Back 336

Sodium Stibogluconate

Front 337

Following a field-trip to a small village in Mexico, a 20-yr-old pre-medical student presents with persistent diarrhea. A fecal sample is collected and is positive for Entamoeba histolytica. There is no indication of amebic liver abscess. What is the recommended treatment?

Back 337

Metronidazole (or tinidazole) followed by paromomycin or iodoquinol.

Metronidazole and tinidazole are tissue amebicides (others are luminal)

Front 338

A 2-yr-old child presents at a Brazilian clinic with a swollen left eye, fever and tachycardia. The doctor suspects Chagas disease given the history of recent childhood infections in this region. Blood culture confirms the diagnosis as Trypanosoma cruz is detected. Which of the following is indicated in this patient?

Melarsoprol, Metronidazole, Nifurtimox, Pentamidine, Quinine

Back 338

nifurtimox--generates ROS which are toxic to parasite which lacks catalase
pentamidien-First line therapy for early stages of WEST African trypanosomiasis
quinine-Anti-malarial, very toxic
metronidazole-Treatment of E. histolytica
melarsoprol-First line therapy for advanced EAST African trypanosomiasis

Front 339

diloxanide furoate

Back 339

Luminal amebicide --
ORAL
Ameobiasis (asymptomatic intestinal infection) --
Not used much.... replaced by iodoquinol and paromomycin

Front 340

iodoquinol

Back 340

Halogenated hydroxyquinoline (Luminal amebicide) Unknown.

Kills the CYSTS.
ORAL
Ameobiasis -- alone for
asymptomatic
intestinal infection;
-- combo w/
metronidazole for
dysentery or liver
abscess) -- 90% excreted in feces; 10% in circulation.

Front 341

paromomycin sulfate

Back 341

Aminoglycoside antibiotic
(Luminal amebicide)
Unknown MOA
Kills the CYSTS.
ORAL
Ameobiasis
-- alone for
asymptomatic
intestinal infection;
-- combo w/
metronidazole for
dysentery or liver
abscess) Not w/ another aminoglycoside --> renal toxic Not significantly absorbed (less toxic than diloxanide furoate)

Front 342

metronidazole (+ luminal amebicine)

Back 342

Nitroimidazole
(Tissue amebicide)
Protozoal enzymes reduce the nitro group; produces toxic, nitro free-radicals that damage DNA and protein.
Kills trophozoites, but NOT cysts
ORAL or IV
Ameobiasis (Amebic colitis & extraintestinal infections) ---E. histolyticsa
Plasma clearance ↓ with impaired liver fxn. Also DOC for trichomoniasis and giardiasis.

Excreted in urine.
Newer, similar drug = TINIDAZOLE (treats giardia)
---HL 7.5 hours

Front 343

drug similar to metronidazole? what does it treat?

Back 343

tinidazole; giardia

Front 344

nitazoxanine

Back 344

Anti-protozoal
A nitrothiazol-salicylamide prodrug that is activated to TIZOXANIDE; inhibits a pyruvate pathway that is critical for anaerobic energy metabolism in protozoa.
-- Giardiasis by G. lamblia in KIDS.
Also used against Cryptosporidium parvum in KIDS. -- Infection by contaminated food and water. (Nasty lakes and rivers)
Common intestinal parasite in US

Front 345

suramin

Back 345

Antiprotozoal for Trypanosoma Mechanism unknown.
A sulfated naphthylamine
IV
Early stage EAST African trypanosomiasis FIRST LINE
Does NOT enter CNS --> NOT effective in advanced disease.

Front 346

melarsoprol

Back 346

Antiprotozoal for Trypanosoma Reacts w/sulfhydryl groups of trypanothione (a reducing agent in the parasite); result is inhibition of pyruvate kinase (and glycolysis) so ↓ ATP synthesis.
IV
ADVANCED CNS progressed EAST African trypanosomiasis -- ENTERS CNS.

Front 347

pentamidine

Back 347

Antiprotozoal for Trypanosoma -- IV
Early stage WEST African trypanosomiasis
MOA unknown
1st line for african trypansome
best known as tx of pneumocytis jirovecii in immunocompromised individuals

Front 348

eflornithine

Back 348

Antiprotozoal for Trypanosoma Selectively, irreversibly inhibits ornithine decarboxylase; disrupts production of nuc. acid and protein synthesis.
IV
ADVANCED stage WEST African trypanosomiasis
Side effects: GI distress!!!! Diarrhea, Anemia, Leukopenia

Front 349

nifurtimox

Back 349

Antiprotozoal for Trypanosoma Nitroaromatic compound generates O2 radicals that are toxic to parasite (Lack catalase; we have catalase so avoid toxicity....selectivity) -- American trypanozomiasis (Chagas' disease) -- In combo with interferon gamma shortens acute phase.

Front 350

sodium stibogluconate

Back 350

Anti-protozoal for Leishmania Mechanism unknown...but thought to ↓ glycolysis and fatty acid synthesis (no ATP or GTP) ORAL Tx of both types: cutaneous and visceral leishmaniasis (MOSTLY cutaneous) -- Leishmania is transmitted by sand fly; infiltrates macrophages

Front 351

miltefosine

Back 351

Anti-protozoal for Leishmania An alkylphosphocholine analog; mechanism unknown. ORAL Tx of visceral leishmaniasis (aka Kala azar) ONLY -- Leishmania is transmitted by sand fly; infiltrates macrophages

Front 352

american trypanosomiasis

Back 352

Trypanosomiasis summarized: AMERICAN type (by Trypanosoma cruzi) Insect feces contaminate eye or break in skin--> cardiomyopathy; TX: NIFURTIMOX

Front 353

west african trypansoma

Back 353

AFRICAN types (x2): Tsetse fly bite
--Type 1: by Trypanosoma brucei gambiense-->WEST AFRICAN sleeping sickness; slowly enters CNS; Early Tx: PENTAMIDINE;
Advanced Tx: EFLORNITHINE

Front 354

east african trypanosomiasis

Back 354

tsetse fly bite
--Type 2: by Trypanosoma brucei rhodensiense--> EAST AFRICAN sleeping sickness; quickly enters CNS, fatal; Early

Tx: SURAMIN;
CNS-progressed Tx: MELARSOPROL

Front 355

tx cutaneous leishmaniasis

Back 355

sodium stibogluconate

Front 356

what treats visceral leishmaniasis

Back 356

miltefosine, sodium stibogluconate

Front 357

treats luminal ameobia

Back 357

metronidazole

Front 358

DOC trichomoniasis and giardiasis

Back 358

metronidazole???

Front 359

antibiotics to avoid in pregnancy

Back 359

SAFE Moms TAke Really Good Care
sulfonamides (kericterus)
aminoglycosides (nephro/ototox)
fluoroquinolones (bone, cartilage damage)
erythromycin (acute cholestatic hepatitis in mom and clarithromycin is embryotoxic
metronidazole---mutagenasis
tetracyclines--discolored teeth, inhib bone growth
ribavirn --teratogenic
griseofulvin--teratogenic
chloramphenicol--gray baby

Front 360

DOC giardia

Back 360

metronidazole

Front 361

DOC trichomonas

Back 361

metronidazole

Front 362

giardia in kids treatment

Back 362

nitazoxanide

Front 363

2 parasidic drugs inhibit cholinesterase

Back 363

malathion (overdose paralysis in pt) and pyrantel pamoate (pin worm, hook worm, ascaris)

Front 364

drug and alternate drug for pinworm

Back 364

pyrantel pamoate and albendazole/mebendazole

Front 365

2 drugs for strongyloides

Back 365

ivermectin and thiobendazole

Front 366

teratogenic paracidic drug

Back 366

albendazole and mebendazole

Front 367

treatment for schistosomes

Back 367

praziquantel

Front 368

3 combo for organ transplant

Back 368

daclizumab, cyclosporine and corticosteroid

Front 369

migraines 1/2 phase

Back 369

1st phase is VC; 2nd phase is VD

Front 370

prevention for migraines

Back 370

dec VC-->anticonvulsants, antidepressants, CCB, NSAIDs, 5HT blockers

Front 371

abort migraines

Back 371

DHE, ergotamine, isometheptene, NSAIDs, tramadol, triptans

Front 372

phenelzine

Back 372

MAOI antidepressents prevention for HA

Front 373

fluoxetine

Back 373

prozac antidepressent prevents migriane

Front 374

amitriptyline

Back 374

depression and rpevent migraine

Front 375

gabapentin

Back 375

seizure prevent migraine

Front 376

methysergide

Back 376

prevent migraines; serotonin 5HT antag and for carcionid tumors

Front 377

verapamil

Back 377

CCB prevent migraines

Front 378

nimodipine

Back 378

CCB prevent migiraines

Front 379

propranolol

Back 379

BB prevent migrianes

Front 380

naproxen

Back 380

NSAIDs for prevention and aborting migraines

Front 381

sumatriptan

Back 381

seratonin agonist 5HT B/D vasoconstrictl for cluster and migraines
2nd phase of migraines
SE: paresthesias
CI: angina, MI, CAD, HTN
NOT IN PT WITH HEART PROBLEMS

Front 382

triptans

Back 382

abort migraine HA

seratonin agonist 5HT B/D vasoconstrictl for cluster and migraines
2nd phase of migraines
SE: paresthesias
CI: angina, MI, CAD, HTN
NOT IN PT WITH HEART PROBLEMS

Front 383

prochlorperazine

Back 383

antipycotic, IV, abort migraine

Front 384

butorphanol

Back 384

opiod, open K channel aborting migraine

Front 385

serotonin agonist vs antagonsit

Back 385

agonist-VC abort migraines, triptans

antag--methylsergide antimigraine prophylaxis and carcinoid tumor 5HT A/C

Front 386

DHE

Back 386

ergots, migraines
ergotism (VC) leading to gangrene bowel infarction
NOT in heart problems like CAD or perpheral vascular disease
CI--CV, pychosis, collagen disease
VC!!! migraine orgrt

Front 387

ergotamine

Back 387

abort migriane; acute
VC-may cuase ergotism gangrene
CI heart diseaes

Front 388

estradiol **

Back 388

NOT GIVEN ORALLY! natual estrogen; postmenopausal HRT, osteoprosis; continuous
may causes THROMBOEMBOLISM, GB DISEASE, HTN
WITH A HYTERECTOMY YOU CAN USE ESTROGEN ALONE

Front 389

estrone

Back 389

IM, natural estrogen, postmeno HRT, osteoperosis

Front 390

estradiol valerate

Back 390

IM, oil suspension, weeks of effect
post meno HRT, osteoperosis

Front 391

estradiol cypionate

Back 391

oil suspention IM, weeks of effect
post menopausal HRT, osteoprosis

Front 392

estrone and equilin

Back 392

conjugated estrogen; hydrolysed
premarin and cenestin
post menopausal HRT, osteoperosis

Front 393

medroxyprogesterone acetate + estrogen ****

Back 393

MPA, addition of progesterone limits endomedtrial hyperplasial; conjugated estrogen

Front 394

ethinyl estradiol

Back 394

oral potency, synthetic STEROID
OCPs

Front 395

mestranol

Back 395

synthetic STEROID; oral
OCPs

Front 396

diethylstilbestrol

Back 396

DES, synthetic NONSTEROID
limited in inoperable breast and prostatic cancer
may cause inc risk of vaginal and cervical cancer

Front 397

raloxifene ***

Back 397

SERM, osteoperosis; dec bone resorption an dremodeling
hot flashes only