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99 Cards in this Set

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Sulfonamide affects what enzyme
dihydropteroate synthase

(competitive inhibition)

(PABA --> DHF)
Tremothoprim enzyme affected
inhibit DHF --> THF

block FA synth
Quinolones enzyme affected
inhibit DNA gyrase (topoisomerase)
What drugs affect folic acid synthesis
Sulfonamides (PABA --> DHF)
Trimethoprim (DHF--> THF)
Trimethoprim AE
AE
same as for sulfonamides plus
HEMATOPOIETIC: LEUKOPENIA, MEGALOBLASTIC ANEMIA
sulfonamides moa
analog of PABA inhibit dihydropteroate synthase

PABA --> DHF

cant make purines
sulfonamide spectrum
gram pos
gram neg
chlamydia
nocardia
sulfonamide topical drugs
silver sulfadiazine
sulfacetamide
triple sulfa
Silver sulfadiazine
burns
sulfacetamide
ocular infections:
conjunctivitis, corneal ulcer
Triple sulfa
vaginitis
(hemophilius vaginitis)
Oral Sulfonamides
Sulfamethoxazole
Sulfisoxazole
Sulfadoxine/pyramethamine
Sulfadiazine/pyramethamine
Sulfasalazine
Dapsone
Sulfamethoxazole and Sulfisoxazole used for
previously untreated UTI
Sulfonamide AE effect (topical)
irritation, stinging, burning
Sulfonamide AE effect (oral)
Systemic AE:

-Steven Johnson syndrome (fever,rash)
-cross-sens w/ other sulfa drugs (sulfa, thiazide, sulfonyl urea)
-crystalluria

-HEMOLYTIC ANEMIA IF G6PD

-kernicterus (newborn)
Hemolytic anemia in g6pd
AE of sulfonamide
sulfa containing drugs
-sulfa
-thiazide
-sulfonyl urea
Sulfonamide resistance
1) overproduction of PABA
2)change enzyme dihydropteroate synthase
3) decrease permeability
Sulfonamide - general
-bacteriostatic
-inhibits purine synthesis
-gram neg,pos, chlamydia,nocardia
-topical and oral
Trimethoprim spectrum
gram neg
gram pos
chlamydia
nocardia
Sulfonamide Pharmokinetics
-rapid GI absorption
-readily distrib (incl CSF)
-acetylated at liver (product still toxic but not antimicrobial)
Trimethaprim Pharmokinetics
-rapid GI absorption
-readily distrib (incl CSF)
-most excreted uncahnged into urine
-some transformed to inactive prods
Trimethaprim is usually used w/...
usu used in combo with SULFONAMIDE --> SYNERGY
Trimethaprim used alone
Oral - UTI
Trimethoprim + Sulfamethoxazole
SYNERGY!!!

ORAL

1) pneumonia: pneumocystis carinii

2) GI infections: Shigella

3) Systemic infections: nocardia, salmonella

4) UTI and resp infection:
H.influenza , strep pneum


IV
pneumonia : pneumocystis carinii
Sulfadoxine/pyramethamine
malaria (long acting)


- - SULFONAMIDE
Sulfadiazine/pyramethamine
toxoplasmosis

- - SULFONAMIDE
Sulfasalazine
Inflammatory bowel disease

-not absorbed
-active ingred = 5 amino salicylic acid

- - SULFONAMIDE
Dapsone
leprosy

- - SULFONAMIDE
Trimethoprim AE
same like sulfonamide PLUS LEUKOPENIA, MEGALOBLASTIC ANEMIA
synergistic combo of sulfonamide plus trimethaprim
sulfamethoxazole + trimethaprim
Quinolones
-synthetic flourinated

-inhibit dna gyrase (cant unwind and replicate or transcribe)

-doesnt affect our enzyme much
Quinolones Group 1

group 2
Group 1 = more on Gram neg

Ciprofloxacin
Norfloxacin
enoxacin
lomefloxacin
ofloxacin

Group 2 = more on gram pos

Levofloxacin
Moxifloxacin
Topical Quinolone
Ciprofloxacin / Ofloxacin

-superficial ocular infection
conjntivitis, corneal ulcer
Superficial ocular infection drugs
Sulfacetamide

Ciprofloxacin/ofloxacin
Oral Quinolone
all group 1 quinolones

Previously untreated UTI

Bone, skin suture infection

Infectious diarrhea

typhoid fever

STD - neisseria

Anthrax
Quinolone Pharmokinetics
-well absorbed orally
(lowest = norfloxacin)

-antacids containing Al or Ca salts delay absorp

-small amt biotransformed in liver
-most elim in urine
Group 2 Quinolones
levofloxacin
moxifloxacin

-respiratory tract infections including community acquired pneumonia

(methicillin sens. staph, s. pneumonia)
Quinolones AE
local - irritation, burn

Systemic:

-CONTRAIND FOR PREGNANCY (damage growing cartilage)

-some PROLONG QT INTERVAL
avoid if taking anti-arrythmic or drugs that prolong QT interval (erythromycin, tricycic antidepressant)

-nausea, diarrhea, rash, CNS distub, tendonitis
IV Quinolone
Ciprofloxacin
ofloxacin
Quinolones - general
-inhibit dna gyrase
-2 groups
- gram negative/ poitive, chlamydia
Quinolones resistance
1) microb mod of DNA gyrase
2) change permeability to drug
-floxacin
quinolone
Antivirals

BLOCK VIRAL UNCOATING
(TRICYCLIC AMINES)
AMANTADINE
RIMANTADINE

-inhibit m2 proton channel in viral envelope
antivirals

DECREASE VIRAL RELEASE
ZANAMIVIR
OSELTAMIVIR

-neuraminidase inhibitors
antivirals

MIXED ACTING
RIBAVARIN

guanosine nucleoside analogue

-inhibits viral RNA Pol
-inhibits GTP synth
-blocks mRNA capping
antivirals

INHIBIT GENOME REPLICATION
ACYCLOVIR
TRIFLURIDINE
GANCICLOVIR
CIDOFOVIR
FOSCARNET

-inhibit DNA pol
antivirals

INHIBIT TRANSLATION OF VIRAL mRNA
INTERFERONS

-glycoprotein encoded by host cell acts on neighbor cells to inhibit rep, degrade mrna, and inhib peptide elong

FOMIVIRSEN

-anti mrna nucleotide (cant make important protein for rep)
Rimantadine/Amantadine

tricyclic amines
Influenza A

-work best prophylactically
-can treat w/vaccine simult (wont suppress Ab production)

Amantadine also initial therapy for Parkinsons (DA)
Amantadine Pharmokinetics / other
-oral
-excreted unchanged into urine (need dosage adjustment for renal impairment)

-crosses BBB --> DA release

-CNS EFFECTS!!!
Rimantadine Pharmokinetics / other
-oral
-extensively metabolized (dont need dosage adjustment unless if creatine clearance really low)

-less CNS effects than Amantadine
Zanamivir/Oseltamivir
INFLUENZA A AND B

neuraminidase inhibitors (sialic acid not removed so binds hemaglutinin --> aggregation --> less viral release)

-use early
-good prophylactically, not approved
-decreases flu complication
Zanamivir info
-inhaled as dry powder
-poor bioavailability

AE:
bronchospasm in asthma

(flu A and b....neuram inhib)
Oseltamivir info
-prodrug
-well absorbed
-nausea, vomit, headache

-BIRD FLU

(flu a and b...neuram inhib)
Ribavarin
INFLUENZA A AND B

RESP SYNCYTIAL VIRUS

VIRAL HEPATITIS (w. interferon)
Ribavarin MOA
nucleoside analogue (guanosine)

MIXED

1)inhibits viral RNA Pol (competes w/ GTP and ATP)

2)Inhibits GTP Synth (inhibits IMP dehydrogenase)

3)blocks mRNA capping (inhibits N7 methyl transferase)

lots of mechs --> less resistance
Ribavarin Use
Aerosol:
-Flu A and B
-resp synctial virus

Oral:
-Viral Hepatitis w/ IFN
SYNERGY
Ribavarin AE
When used ORAL: (w. IFN for hepatitis)
hemolytic anemia
Acyclovir
Trifluridine
Ganciclovir

MOA
get phosph by VIRAL THYMIDINE KINASE

(acyclovir --> acyclovir monophosph)

then acyclovir monophosph --> acyclovir triphosph via cellular kinase

1) inhibit DNA pol
2) incorp into DNA, terminate elongation
Acyclovir USE
low dose: Herpes 1 and 2

High: Herpes, other trains

Herpes encephalitis

Herpes keratitis

Mucocutaneous infections (immunocomp) IV

Varicella zoster (immunocomp)
Acyclovir Pharmokin/ AE / Resistance
IV
topical
oral (bad bioavail)

AE:

1% encepholopath

nephrotoxicity

Resistance:
alter thymidine kinase
Trifluridine USE
topical

HERPES KERATITIS (DOC)

-use if acyclovir resistant
Ganciclovir structure/pharmokinetics
-like acyclovir + CH2OH

IV @ acute
oral @ maintenance
Ganciclovir USE
CMV RETINITIS (serious only)

PNEUMONIA DUE TO CMV - KIDNEY TRANSPLANT PATIENTS
(with anti-CMV antibody)
Ganciclovir AE
bone marrow suppression
Ganciclovir General
CMV RETINITIS (serious bc TOXIC)

:o( - bone marrow suppression
Ribavarin
Flu A and B
Resp syncytial virus

oral -
viral hepatitis (w. IFN)
:O( - causes hemolytic anemia
Cidofovir
nuceloside analogue - cytosine
(dont need viral kinase for phosph)

USE:
CMV RETINITIS (ganciclovir resistance)

-IV (w. probenicid)

AE:
bone marrow supp
renal toxicity
Foscarnet MOA
Pyrophosphate analogue

-interact w/ PPi binding site --> inhibit DNA pol, reverse transcriptase

CMV RETINITIS (ganciclovir resistance)

AE: decrease renal function
CMV RETINITIS
GANCICLOVIR (serious only bc toxic)

-bone marrow supp, some CNS

CIDOFOVIR

-bone marrow supp, renal tox

FOSCARNET

-decrease renal func

FOMIVIRSEN

-2nd line CMV retinitis (intravitreally)
INTERFERONS MOA
1) kinase inhibits rep (inactivates IF)

2) endonuclease degrades viral mRNA

3) phosphodiesterase degrades tRNA --> inhib peptide elong
INTERFERONS pharmokin
proteins so admin'd

IM
subQ
topical
INTERFERONS use
Chronic Hepatitis B and C (w. ribavarin --> SYNERGY)

HAIRY CELL LEUKEMIA

AIDS RELATED KAPOSI SARCOMA

GENITAL WARTS (condyloma acuminatum)

HERPES ZOSTER (given early prevent dissemination in cancer pts)

HERPES KERATOCONJUNCTIVITIS
INTERFERONS AE
AE:

neutropenia --> flu like symptoms

-when used with ribavarin --> hemolytic anemia

(no synergy of side effects)
FOMIVIRSEN MOA
antisense oligonucleotide
against mRNA for protein needed for viral rep
FOMIVIRSEN use
CMV RETINIS (2nd line)

-intravitreally
antifungal

FORM LYTIC ION CHANNEL
Polyene Macrolide:

AMPHOTERICIN B

NYSTATIN

(bind sterol in PM, esp ergosterol, form cytotoxic pores) (lysis, decreased ATP)
most antifungal drugs target:
cell membrane (have ergosterol)
antifungal

DISRUPT NUCLEIC ACID SYNTHESIS
FLUCYTOSINE
-antimetabolite

-converted by fungi to active metab (FU)
- inhibits RNA/DNA synthesis
antifungal

INHIBITS MITOSIS VIA DISRUPT. CYTOSKELETON
GRISEOFULVIN

-inhibits microtubules
-binds keratin

-fungistatic!!
antifungal

INHIBITS ERGOSTEROL SYNTHESIS
selectively inhibits fungal P450 enzyme

-IMIDAZOLE

KETACONAZOLE
MICONAZOLE
CLOTRIMAZOLE

(-triazole) inhibits more selectively

ITRACONAZOLE
FLUCONAZOLE
VORICONAZOLE
antifungal

INHIBITS SQUALENE OXIDASE
NAFTIFINE
TERBINAFINE

-inhibits SO, increase is toxic decreases ergosterol
antifungal

INHIBITS CELL WALL FORMATION
CASPOFUNGIN

-inhibits Beta 1,3 D- glucan synth (cell wall)
Amphotericin B USE
-broadest spectrum

LIFE THREATENING SYSTEMIC INFECTIONS (doc)

invasive Apergillus (w. itraconazole)

crypto meningitis (w. flucocystine)

histoplasosis

dermatophytic mucocutaneous infections
Amphotericin B

info
AE
-given as IV liposome
-bad absorption

AE:

RENAL IMPAIRMENT

hypokalemia

fairly toxic, binds cholesterol
Nystatin USE
local dermal/oropharyngeal infection

vaginal candidiasis

-too toxic for systemic (unlike amphotericin B)
just local topical
Flucocystine USE / AE
oral combos (so decrease resistance and toxicity)

CRYPTO. MENINGITIS (w. ampho B)

BLASTOMYCOSES (w. itraconazole)

AE: narrow ther. window (bc FU metabolite)

BONE MARROW TOXICITY!!
Griseofulvin USE
dermaphytosis (nail infection)

extd. treatment after triazoles

athletes foot, ringworm
Ketoconazole USE

AE
mucocutaenous candidiases

coccidiomycosis (non-meningeal)- not CNS

shampoo - seborr dermatitis

AE

interferes w/ adrenal/gonadal synthesis
interfere w/ human p450 enzymes

(use to decrease adrenal steroids in Cushings disease)
Miconazole/Clotrimazole USE
topical antifungal

vulvovaginal candidiases

dermatophytic infections

oropharyngeal thrush - candidiases
(clotrimazole - oral) alt to nystatin
Itraconazole USE

AE
MOST POTENT AZOLE FOR SYSTEMIC INFECTION

PERSISTENT DERMATOPHYTOSIS (doc)

EFFECTIVE AGAINST ALL APERGILLUS

PREFERRED FOR ENDEMIC HISTOPLASMOSIS

AE

drug intx (w. non sedating histamine)

no effect on steroid synth

variable on human p450
Fluconazole USE

AE
CRYPTO. MENINGITIS (doc)
--good CSF
-if life threatening --> ampho B

mucocutaneous candidiasis

prophylactic for bone marrow transplants - AIDS

AE

widest therapeutic window :O)
Naftidine/Terbinafine
cutaneous mycoses (topical)

NAIL INFECTIONS - TERBINAFINE!

-not affective against candida
Caspofungin USE
invasive candidiasis

apergillosis (alt to ampho B)

-not affective against cryptococcus
Voriconazole USE

AE
invasive Aspergillus (doc)

candida (even if resistant to fluconazole)

meningitis (good CSF)

AE

visual disturbances
hepatotoxity
inhibit p450
fungus

DERMATOPHYTE doc
ITRACONAZOLE
fungus

CANDIDA doc
FLUCONAZOLE

(if resistant --> voriconazole)
fungus

CRYPTOCOCCUS doc
FLUCONAZOLE (wide ther. window)

also:

Flucocystine + Ampho B
fungus

ASPERGILLUS doc
VORICONAZOLE

also:

ampho B w. itraconazole(all asp)