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178 Cards in this Set

  • Front
  • Back
Penicillin, ampicillin, ticarcillin, piperacillin, imipenem, aztreonam, cephalosporins

MOA
Block cell wall synth by inhibiting peptidoglycan cross linking
Bacitracin, Vancomycin

MOA
Block peptidoglycan synth
Polymyxins

MOA
Disrupt bacterial cell membranes
Sulfonamindes
Trimethoprim

MOA
block nucleotide synth
Fluroquinolones

MOA
Block DNA topoisomerase
Rifampin

MOA
block mRNA synth
Chloraemphenicol, macrolides, clindamycin, streptogramins (quinupristin, dalfopristin), linezolid

MOA
block protein synth at 50s ribosome
Aminoglycosides, tetracyclines

MOA
block protein synth at 30s ribosome
Bacteriostatics
we're ECSTaTiC about bacteriostatics

Erythromycin
Clindamycin
Sulfamethoxazole
Trimethprim
Tetracycline
Chloramphenicol
Batcericidials
Very Finely Proficient At Cell Murder

Vancomycin
Fluoroquinolones
Penicillin
Aminoglycosides
Cephalosporins
Metronidazole
prototype for b-lactams

(2)
penicillin G (IV), pen V (oral)
Drug that is bactericidal for
-S. pneumo
-S. pyogenes
-N. meningitides
-Treponema pallidum (syphillis)
-Pasteurella multocida
-Listeria
-Actinomyces israelii

a. drug?
b. MOA
c. toxicity
a. penicillin G (IV), V (oral)
b. binds and blocks transpeptidase cross linking, activates autolytic enzymes
c allergy (bronchospasm, rash, shock), rash, Pseudomembranous colitis (C. diff)
Drug I would use for a patient with strep throat caused by S. pyogenes
Penicillin V
3 Penicillinase-resistant penicillins

what makes them penicillinase-resistant
METhicillin, NAfcillin, diclOXacillin

I MET a NAsty OX

bulkier R group
Infection with S. aureus (but not MRSA)

a. drug to treat
b. toxicity
a. penicillinase-resistant penicillins (methicillin, nafcillin, dicloxacillin)

b. hypersensitivity
methcillin - interstitial nephritis
What makes MRSA methicillin-resistant
altered penicilllin binding protein (transpeptidase) binding site
What would I use for an s. aureus infection causing
-cellulitis
-endocarditis
-sepsis
nafcillin

"use NAF for STAPH"
spectrum compared to pen G
a. penicilinase-resistant pens
b. aminopens
c. antipseudomonals
a. narrower
b. wider
c. wider
2 aminopenicillins

how do they compare in general with penicillins regarding coverage
ampicillin (IV) , amoxicillin (oral)

better coverage of gram negs
class of drug used to treat
-H. influenzae
-E. coli
-Listeria
-Proteus
-Salmonella
-Enterococci

a. 2 drugs
b. toxicity
ampicillin (IV), amOxacillin (Oral)

hypersensitivity, ampicillin rash, pseudomembranous colitis
Drug I would use for outpatient bronchitis, otitis media, sinusitis, or Listeria infection

what makes it good as an outpatient drug
amoxacillin

oral
drug combined with gentamycin to provide broad gram neg. coverage
ampicillin
Aminopenicillins

a. sensitive to penicilinase?

b. how can you enhance their spectrum
a. yes

b. give clauvulanic acid, protects against penicillinase destruction
Triple therapy for H. pylori infection involving an aminopenicllin
amoxacilin, bismuth, metronidazole
3 antipseudomonals
ticarcillin, carbenicillin, piperacillin

James Bond uses 3 tools to kill the nasty pseudomonas
1. TICk
2. CAR
3. PIPE bomb
Treatment for pseudomonas and gram negative rods

a. what should you use it with to extend the spectrum
b. toxicity
ticarcillin, carbenicillin, piperacillin

a. give with clauvulanic acid (sensitive to penicillinase)

b. hypersensitivity
3 beta lactamase inhibitors
Clauvulanic Acid
Sulbactam
Tazobactam

CAST
First generation cephalosporins
CePHalexin
CeFAZolin

they all have PH except ceFAZolin, so don't get "FAZed" by this
drug to treat gram positive cocci (staph or strep when patient is allergic to penicillin, or before surgery to prevent skin infection)
-Proteus
-E.Coli
-Klebsiella

a. adverse efects
1st gen cephalosporins (cefazolin, cephalexin)
-treat gram pos cocci + PEcK

a. Hypersensitivity, delayed rash, c. difficile
Drug that treats gram pos. cocci +
-H. influenzae
-Enterboacter
-Neisseria
-Proteus
-E. Coli
-Klebsiella
-Serratia
2nd gen cephalosporins (Cefoxitin, Cefaclor, Cefuroxime)

treat HEN PEcKS
If your patient has pneumonia, but you don't know what is causing it, what is a good agent to give broad coverage of the most likely pathogens
Cefuroxime (2nd gen cephalosporin)

provides coverage of both S. pneumo and H. influenzae
2nd gen cephalosporin good for anaerobes
cefoxitin
3 second gen cephalosporins

toxicities (5)
ceFOXitin, ceFAclor, ceFURoxime (FOX FAmily wears FUR)

1. hypersensitivity
2. C. diff
3. increases nephrotixicity of aminoglycosides
4. if ceph has a MMT sidechain, can interfere with alcohol metabolism --> buildup of acetaldehyde
5. vit K deficiency
3 third gen cephalosporins

what are they good for in general
cefTRIaxone, cefoTaxime, cefTazidime

good for serious gram neg infections resisant to other b-lactams
patient has meningitis/gonorrheae that is resistant to other b-lactams

what should I try?
ceftriaxone - good CSF penetration
3rd gen cephalosporin used for pseudomonas
ceftazidime
Cephalosporins

5 adverse side effects
1. hypersensitivty
2. cross-hypersensitivity with penicillins
3. nephrotoxic with aminoglycosides
4. if MTT side chain --> disulfride-like rxn with ethanol (nausea and vomiting from buildup of acetaldehyde)
5. vit K def
cephalosporin good for pseudomonas and gram pos.
cefepime (4th gen)
two cephalosporins that work against pseudomonas
ceftazidime (3rd), cefepime (4th)
Drug that is a magic bullet for gram negative rods, aerobic organisms in patients who are
-pen allergic
-cannot tolerate aminoglycosides because they are pen allergic

how should you take these to increase spectrum?
aztreonam


used with a gram pos. killer like vancomycin or clindamycin
aztreonam
a. mechanism
b. toxicity
c. use
a. monobactam (resists b-lactamase) that binds to PBP3 and inhibits cell wall synth

b. non-toxic, little cross reactivity with pens

c. gram neg rods, used synergistically with aminoglycosides
Drug with the broadest spectrum
-gram pos cocci
-gram neg rods (+pseudomonas)
-anaerobes

but it cannot cover MRSA

drug?
newer drug that is better?
imipenem/cilastatin

meroprenem - don't need cilastatin b/c it is stable to dihydropeptidase
imipenem

what do you give with it to increase its lifespan and why
cilastatin

b/c imipenem is broken down by dihydropeptidase (in kidney)
Drug that you can give in a trauma for the best overall general coverage (known as 'decerebrate antiobiotic')

negative side effects
carbapenem class

1. GI distress
2. skin rash
3. seizures
beta lactams that are
a. resistant to beta lactamase (4)
b. susceptible to beta lactamase (3)
a. impinem, aztreonam, cephalosporins, pen-resistant pens

b. Penicillin, aminopenicillins, antipseudomonals
Drug that is used only for serious gram positive infections
-MRSA
-C. diff
-enterococci

a. mechanism
b. toxicity (4)
a. inhibits cell wall peptidoglycan by binding D-ala D-ala side chain --> bacteriocidal

b. Nephrotoxic, Ototoxic, Thrombophlebitis, flushing

generally NOT many problems
A bacteria has an amino acid change from D-ala D-ala to D-ala D-lac in its peptidoglycan

it is now resistant to what drug
vancomycin
Why should you pre-treat with antihistamines and give a slow infusion rate of vancomycin
prevent diffuse flushing (red man syndrome)
30s inhibitors

static or cidal?
AT

aminoglycosides (cidal)
tetracycline (static)
50s inhibitors
CCELL

Chlomramphenicol (static)
Clindamycin (static)
Erythromycin (static)
Lincomycin (static)
Linezolin (variable)
Only anti-ribosomal antibiotic that cannot be absorbed orally
aminoglycosides
Drug that has wide spectrum activity (gram pos, gram neg, anaerobes), used specifically with

-bacterial meningitis if patient is pen and cephalosporin allergic
-Rickettsial infection (rocky mtn spotted fever) if patient is pregnant or a child
Chloramphenicol

very wide spectrum - good overall coverage, but toxic, so only use if other drugs are contraindicated

can't use tetracycline for rickettsia in a child or pregnant woman
Drug used to treat pen/cephalosporin-resistant meningitis

a. MOA
b. toxicity
chloramphenicol

a. inhibits 50s peptidyltransferase, bacteriostatic

b. anemia (dose dep.), aplastic anemia (dose indep.), gray baby syndrome (baby lacks UDP-glucoronyl transferase)
Bacteria obtains a plasmid-encoded acetyltransferase

what drug is it resistant to now
chloramphenicol

this drug inhibits peptidyltransferase in 50s ribosome (bacteriostatic)
Patient with poor dentition presents with
-wt loss
-chronic fever
-night sweats
-foul-smelling sputum

imaging shows lung abscess
treat?
clindamycin

in general, used for anaerobic infections above the diaphragm
Treatment of bacteroides or c. perfringens infection --> aspiration pneumonia or lung abscess

a. MOA
b. toxicity
clindamycin

MOA: blocks peptide bond formation at 50s subunit (static)

Tox: pseudomembranous colitis, fever, diarrhea
treats anaerobic infections
a. above diaphragm

b. below diaphargm
a. clindamycin

b. metronidazole
aminoglycosides - which one is used for
a. added with penicillin for in-hospital infections
b. pseudomonas
c. broadest spectrum, good for resistant nosocomial infections
d. broadest spectrum but lots of toxicity, topically for skin, bowel surgery
a. gentamycin
b. tobramycin
c. amikacin
d. neomycin
Drug that is used with b-lactams to kill aerobic gram negative rods of the GI tract (like e.coli)

why use b-lactam
aminoglycosides
-MEAN GNATS canNOT kill anaerobes

Gentamycin, neomycin, amikacin, tobramycin, streptomycin

these need to cross the cell wall to act, so beta lactams help by breaking down wall
a bacteria develops a transferase enzyme that allows it to acetylate, phosphorylate, or adenylate a drug

what drug is it now resistant to?

what is its MOA?

Toxicity?
aminoglycosides

inhibits initiation complex formation on 30s (cidal), but needs Oxygen for uptake

Nephrotoxic (esp w/cephalosporins), Ototoxic (esp w/ loop diuretics), Teratogen

MEAN GNATS canNOT kill anaerobes
Drug used for
-Chlamydial VD
-Mycoplasma pneumoniae
-Rickettisia
-H. pylori
-Borrelia burgdorgeri

4 types
Tetracycline, doxycycline, demeclocyline, minocycline

Picture a solider in the TET offensive: he has chlamydia from prostitutes, rickettsia from ticks, 'walking' pneumonia
Contraindications for tetracycline
-pregnancy
-don't take with milk, antacids, or Fe-containing preps (chlates divalent cations --> inhibits absorption in the gut)
Tetracyclines

which tetracycline works better than the rest with food because it is a poor chelator of divalent cations

how is it eliminated and why is this important
doxycylcine

fecally eliminatd, can take in renal failure
Tetracycline

which can work as a diuretic in SIADH and why
demeclocycline - ADH antagonist
Alternative drug to erythromycin for treating walking pneumonia from mycoplasma pneumoniae

MOA?
adverse?
tetracycline

prevents attachment of aminoacyl-tRNA to 30s ribosome (static), limited CNS penetration

GI distress, discolored teeth, inhibits bone growth in kids, photosensitivity (phototoxic dermatitis), renal and hepatotoxic

(picture soldier in TET offensive who is irritable (GI), has yellow teeth, works in the dark (photosensitive), has shrapnel in kidney and liver, and breaks kids' bones)
MOA of tetracycline

resistance conferred when...
prevents aminoacyl-tRNA attachment to 30s ribosome (Static)

resistance when bacteria gets plasmid-encoded efflux pumps that decrease uptake into cells or increase efflux out of cells
Rickettisial infection - treat

a. adults
b. kids/pregnant women
a. tetracycline (can accumulate intracellularly)

b. chloramphenicol (can't use tetracycline with kids and pregnant people)
Drug that treats
-atypical pneumonias (mycoplasma, chlamydia, legionella)
-Legionairre's disease
-gram positives (strep infections in paitents allergic to pen)
-URIs - otitis, sinusitis, bronchitis
-STDs
-Neisseria
Macrolides: erythromycin, azithromycin, clarithromycin

(Picture cross (gram pos.) over a wreat (erythromycin) that commemorates a french legionnaire (legionella))
Patient has Legionairre's disease

go to drug?

MOA?

Tox?
Macrolide - erythromycin, clarithromycin, azithromycin

MOA: blocks translocation on 50s ribosome - inhibits protein synth (static)

Tox:
-long QT (avoid if arrhythmias)
-GI discomfort (peristalsis)
-acute cholestatic hepatitis (blocked bile duct)
-eiosinophilia, skin rash
-increases serum conc. of theophyllines, oral anticoags
Bacteria has a methylated 23s binding site

what drug is it resistant to
Macrolides - eryth, azith, clarithromycin

these drugs bind to 23s subunit of 50s ribosome, inhibit translocation of growing polypeptide
Drug to that treats UTIs that you should NEVER use with warfarin

why
TMP-SMX

displaces warfarin from albumin --> increases serum warfarin --> high risk of bleeding
3 sulfonamide drugs

MOA
sulfamethoxazole, sulfisoxazole, sufladizine

Inhibits Dihydropteroate synthetase --> inhibits THF production -> can't make purines, thymine, or proteins
Hypersensitivity
Hemolysis (if G6PD deficient)
Tubulointerstitial nephritis
Photosensitivity
Kernicterus in infants
Warfarin interaction

which drug?

what does it treat?
sulfonamides

Gram pos, gram neg, nocardia, chlamydia
Bacteria gets altered dihydropteroate synthetase or upregulates PABA synthesis

what drug is it resistant to
sulfonamides
Trimethoprim

MOA
TOX
inhibits bacterial DHF reductase

megaloblastic anemia, leukopenia, granulocytopenia

(can help by giving folic acid)
Drug that treats
-Strep pneumo or h. influenza induced otitis, bronchitis, sinusitis, pneumonia

-Shigella, salmonella, e.coli induced diarrhea

-Enterics (e.coli) induced UTI, urethritis, prostatitis

-PCP, toxoplasmosis, Isospora syndromes in AIDS patients
TMP-Smx

T - (respiratory) Tree -
M - mouth (GI)
P - pee (GU)
S - systemic (AIDS)
I have a sulfa allergy

which 8 drugs must I avoid
-sulfonamindes
-sulfasalazine
-sulfonylurea
-thiazide diuretics
-acetazolamide
-furosemide
-celecoxib
-probenicid
Drug that covers
-pseudomonas in CF patients
-aerobic enterics (ETEC, slamonella, shigella, campylobacter)
-complicated UTIs (enterobacteriae)
-pneumonia from intracellular organisms (Legionella, mycobact, salmonella)
-s.aureus chronic osteomyelitis
fluroquinolones

cipro, noro, oflo, sparflo, moxi, gat "floxacins"

nalidixic acid
patient with CF has pseudomonas infection


drug?
MOA?
toxicity?
fluroquinolones - cipro

inhibits DNA gyrase (cidal)

-GI upset
-C. diff colitis
-pregnant and children - cartilage damage
-tendon rupture
-myalgias in kids
patient has chronic s. aureus osteomyelitis

drug?

when is it contraindicated?
what should you avoid taking it with?
fluorquinolones

contra in pregnancy and children (cartilage damage, tendon damage, myalgias)
"fluorquinoLONES hurt attachments to BONES"

Don't take with antacids
bact has point mutation in DNA gyrase

what drug is it resistant to
fluoroquinolones
How do moxifloxacin and gatfloxacin differ from ciprofloxacin
fluoroquinolones

moxi and gati have more anaerobic coverage, strep pneumo coverage
Drug good for aeorbic enterics, complicated UTIs, community acquired pneumonia from legionella or mycobact.
fluoroquinolones
Drug that treats
-Giardia
-Entamoeba
-Trichomonas
-Gardnerella vaginalis
-Anaerobes (below diaphragm)
-h. Pylori

MOA
adverse?
Metronidazole (GET GAP)

Forms free radical toxic metabolite--> damages DNA (cidal)

Disulfiram-like rxn with alcohol
headache
metallic taste
teratogen
Drug to use in resistant gram negative infections that bind to cell membranes and disrupt their osmotic properties

2Toxicity
Polymyxins (polymyxin B, colistimethate)

-Neurotoxic
-acute renal tubular necrosis
M. tuberculosis
a. prophylaxis
b. treatment
a. isoniazid
b. RIPE = rifampin, isoniazid, pyrazinamide, ethambutol
T. avium-intracellulare
a. prophylaxis
b. treat
a. azithromycin
b. azithromycin, rifampin, ethambutol, streptomycin
mycobacterium leprae

treatment?
dapsone, rifampin, clofazimine
Patient has TB
a. first line therapy
b. second line therapy
a. Isoniazid (INH), Streptomycin, Pyrazinamide, Rifampin, Ethambutol (RIPES)

b. cycloserine
Ethambutol

MOA

Side effect
MOA = decreases carb polymerazation of myocobact. cell wall by blocking arabinosyltransferase

side effect: optic neuropathy (red green color blindness)
Pyrazinamide
use?
MOA?
use: first line TB

Effective in acidic pH of phagolysosomes, where mycobact engulfed by macrophages live
If active TB

treatments and how long
1. 4 for 2 (RIPE for 2 months)

2. 2 for 4 (RI for 4 months)

If potts or meningitis from TB, treat longer!
Only agent used for solo prophylaxis for TB

MOA?
Toxicity?
Isoniazid

Decreases synth of mycolic acids, but needs to be converted to active form by bacterial catalase peroxidase
-inhibits Cyp 450
-different half lives for fast and slow acetylators!


-Neurotox (peripheral neuropathy), lupus - give B6 to prevent these
-Hepatototoxic
Drug used for
-first line TB
-given with dapsone in leprosy to delay resistance
-meningococcal prophylaxis and chemoprophylaxis in contacts of children w/ H. influenzae B

Mechanism?
Tox
Rifampin

Inhibits DNA-dependent RNA Pol

Drug interaction (increases activity of P450), orange body fluids (non toxic)
4 Rs of rifampin
RNA polymerase in hibitor
Revs up P450
Red/orange body fluids
Rapid resistance if used alone
Drug interactions with rifampin
upregulates P450, so it decreases effect of these drugs

-coumadin (blood thinner)
-oral contraceptives
-oral hypoglycemics, corticosteroids
-anti-seizure (phenytoin)
Nonsurgical antimicrobial prophylaxis

Meningococcal infection
rifampin (first choice)
minocycline
Nonsurgical antimicrobial prophylaxis

Gonorrhea
ceftriaxone
Nonsurgical antimicrobial prophylaxis

Syphilis
Benzathine, pen G
Nonsurgical antimicrobial prophylaxis

History of recurrent UTIs
TMP-SMX
Nonsurgical antimicrobial prophylaxis

PCP
TMP-SMX (first)
aerosolized pentamidine
Nonsurgical antimicrobial prophylaxis

Endocarditis with surgical or dental procedures
Penicillins
Nonsurgical antimicrobial prophylaxis

Mycobacterium avium-intracellulare
Azithromycin
Treat MRSA
Vancomycin
Treat VRE
Linezolid and streptogramins (quinupristin/dalfoprisitne)
Antifungals

2 drugs that disrupt membrane by forming artificial pores
amphtericin
nystatin
Antifungals

drug for serious, systemic mycoses
-crypto, blasto, coccidioides, aspergillus, histoplasma, candida, mucormycoses

MOA
amphotericin B

Binds to ergosterol, forms pores that allow electrolytes to leak (amphotericin TEARS membrane)
Fungal meningitis

drug? how is it given?
amphotericin B

give intrathecally because it does not cross BBB
Patient has systemic aspergillus infection

drug?

toxicity?

how can you reduce toxicity
amphotericin B

-Fever/chills (shake and bake)
-Nephrotoxicity (keep track of BUN, Cr)
-Hypotension
-Arrhythmias
-Anemias
-IV phlebitis (inflamm of vein)

hydration to reduce nephrotoxicity, liposomal amphotericin reduces toxicity
drug for
-oral candidiasis
-diaper rash
-vaginal candidiasis

MOA?
Nystatin

same as amphotericin B, but too toxic so only use topically
Drug for cryptococcal meningitis in AIDS, candida infections

MOA
Fluconazole (can cross BBB)

Inhibits P450 that converts lanosterol to ergosterol --> cannot make ergosterol --> cannot make fungal membrane
Drug for systemic infections of (less serious?)
-blastomyces
-coccidioides
-histoplasma
-candida
-hypercortisolism

Toxicity?
Ketoconazole

-inhibits hormone synth (gynecomastia)
-liver dysfunction (inhibits P450)
-fever, chills
Drugs for topical fungal infections that can cause gyencomastia and liver dysfunction
ketoconazole
Drug used in systemic fungal infections, combined to amphotericin B

MOS?
tox?
flucytosine

converted to 5-FU --> inhibits thymidylate synthase --> inhibits DNA synth

-bone marrow suppression
-nausea, vomiting, diarrhea

(effects rapidly dividing GI and Bone marrow cells)
Drug for invasive aspergillosis

MOA
Tox
Caspofungin

Inhibits b-glucan --> inhibits fungal cell wall synth

GI upset, flushing
Drug to treat onychomycosis (fungal infection of finger or toe nails)

MOA
terbinafine

inhibits fungal enzyme squalene epoxidase --> can't make ergosterol
drug that is oral treatment for superficial fungal infections

also inhibits growth of dermatophytes (tinea, ringworm)

MOA

Tox
Griseofulvin

MOA: interferes with microtubule formation, disrupts mitosis; deposits in keratin containing tissues

Tox: teratogen, carcinogen, confusion, headache, increases P450 and warfarin metabolism
Patient with HIV was cleaning cat litter, presents with 1 month of
-LN enlargement, fever, aches

dx?
What drug should you use with sufladiazine?

MOA of drug?
Toxoplasmosis

Pyrimethamine

Inhibits plasmodial DHF reductase
Patient in Africa has constant, irregular episodes of
-extreme fever, shaking and chills
-drenching sweats
-hepatosplenomegaly
0brain, lung, kidney damage

dx?
treat?
MOA of drug?
malaria from p. falciparum (constant, irregular episodes differentiate from other bugs that cause malaria)

pyrimethamine

selectively inhibits DHF reductase of plasmodiaum falciparum
Patient bitten by a Tse Tse fly has
-fever, headache, joint pain, itching
-swollen LN at back of neck (Winterbottom's sign)
-anemia

dx?
treat?
MOA?
Sleeping sickness from a Trypanosoma infection (hemolymphatic stage)

Treat with suramin

Inhibits enzymes involved in energy metabolism
Drug used to treat African sleeping sickness

limitations of this drug
suramin - inhibits enzymes involved in energy metabolism

no CNS involvement
Patient bitten by a Tse Tse fly had
-fever, headache, winterbottom's sign

now has
-altered sleep cycle
-confusion

treat?

MOA
african sleeping sickness from trypanosoma (neuro phase)

melarsoprol, which inhibits sulfhydryl groups in parasite enzymes

Has CNS involvment
African sleeping sickness treatment
a. hemolymphatic stage
b. neuro stage
a. suramin

b. melarsoprol
Patient in S. America has
-dilated cardiomyopathy
-magacolon
-megaesophagus

on blood smear, you see motile trypomastigotes

a. dx
b. bug
c. treat
d. MOA of treat
Chigas disease

Tyrpanosoma Cruzi

Nifurtimox

Forms intracellular oxygen radicals, which are toxic to organism
Patient is bitten by a sandfly, has
-spiking fevers
-hepatosplenogmegaly
-pancytopenia

macrophages show up containing amastigotes (lacking flagella)

a. dx
b. bug
c. treat
d. MOA of treat
a. Visceral leishmaniasis

b. leishmania donovani

c. Sodium stiogluconate

d. inhibits glycolysis at PFK reaction
Antiprotozoan drug that is a prophylaxis for P. falciparum and p. malarieae

used with primaquine for P. vivax and P. ovale

MOA
Chloroquine

Blocks plasmodium heme polymerase --> accumulation of toxic Hb breakdown products --> destroys plasmodium
A first line prophylaxis for malaria and treatment for acute malaria (P. falciparum) resistant to chloroquine
mefloquine
Treatment for chloroquine-resistant species of p. falciparum when used in combo with pyrimethamine/sulfonamide
Quinine
Treatment for intestinal nematodes

MOA
MeBENDazole (worms are BENDy)

Inhibit glucose uptake and microtubule synth
Alternative to mebendazole for ascaris, necator (hookworm), and enterobius (pinworm)

MOA
Pyrantel pamoate

stimulates nicotnic receptors at NMJ --> contraction --> depolarization-induced paralysis

(does not affect tapeworms or flukes)
Treatment of choice for onchocerca volvulus (river blindness) and intestinal nematodes

MOA

effect on humans
Ivermectin

Intensifies GABA neuroransmission --> immobilization

Does not cross BBB --> no effect on humans
Drug used for
1. extra-intestinal nematodes
(wucheria bancroti, brugia malayi, loa loa, oncocercia (2nd line))

2. toxocariasis (visceral larval migrans)

3. tropical pulmonary eosinophilia
Diethylcarbamazine
Drug for
1. trematodes (flukes) - schistosomes
2. Cestodes (tapeworms) - Teania and diphyllobatum, latum
3. Taenia solium (cysticercosis)

MOA
Praziquantel

Increases membrane permeability to Ca --> contraction and paralysis of tapeworms and flukes
Drug for HSV, VZV, EBV

BUT NOT CMV

why not CMV?
acyclovir

needs to be monphosphorylated by thymidine kinase, which CMV does not have
Drug used for
-HSV - mucocutaneous and genital lesions, encephalitis
-VZV infection involving eye
-prophylaxis in immunocompromised patients

a. drug
b. structure of drug
c. MOA of drug
d. toxicity
a. acyclovir

b. guanosine analog

c. monphosphorylated by thymidine kinase --> triphosphate form made --> inhibits viral DNA polymerase by chain termination

d. well tolerated
A virus that lacks thymidine kinase is resistant to...

one example
acyclovir

CMV
Drug used for
1. CMV infection in AIDS patients
-retinitis
-pneumonitis
-esophagitis

2. CMV pneumonitis in bone marrow transplant patients

MOA
Ganciclovir

5' monophosphate form by CMV viral kinase or VZV/HSV thymidine kinase --> triphosphate form of guanosine analog --> inhibits viral DNA pol
Ganciclovir

Toxicity
Leukopenia, neutropenia, thrombocytopenia
renal toxicity (more toxic than acyclovir)
A CMV has mutated DNA polymerase or lacks viral kinase

what drug is it resistant to
ganciclovir
Drug for CMV retinitis when gancicovir fails or acyclovir-resistant HSV

MOA

Toxicity
Foscarnet

Binds to viral DNA pol pyrophosphate binding site, inhibits (does not need viral thymidine kinase)

Nephrotoxic
Foscarnet resistance
Mutated DNA pol
When should HAART therapy be initiated in AIDS patient?
CD4 < 350 or high viral lode or AIDS-defining illness
What does the HAART regimen consist of (2)
1. 2 NRTIs + 1 protease inhibitor

2. 2 NRTIs + 1 NNRTI
HAART

5 protease inhibitors
SaquiNAVIR
Ritonavir
Indinavir
Nelfinavir
Amprenavir

NAVIR TEASE a proTEASE
HAART

4 NRTIs
Zidovudine (ZDV)
Didanosine (ddI)
Zacitabine (ddC)
Stavudine (d4T)


"have YOU DINED (zidovUDINE) with my NUCLEAR (nucleosides) family?"
HAART

3 NNRTIs
Nevirapine
Efavirenz
Declaviridine

Never Ever Deliver nucleosides
HAART

1 fusion inhibitor
EnFUvirtide

FUsion inibitior
HAART

Mechanism of protease inhibitors
prevent maturation of new viruses by preventing HIV-1 protease (pol) from cleaving HIV polypeptides into functional proteins
Drugs that inhibit viral penetration
gamma globulins
Drugs that inhibit viral uncoating
amantadine
Drugs that inhibit viral nucleic acid synth
purin and pyrimdine analogs

Reverse transcriptase inhibitors
Drugs that block late protein synth and processing (viral
protease inhibitors
Drugs that block viral protein packaging and assembly
rifampin (vaccine()
Drug that is used for treatment of influenza A, Parkinson's disease

MOA
toxicity
Amantadine

Blocks viral penetration, unCOATing (M2), release of dopamine from nerve terminals
(picture A MAN getting ready TO DINE by taking off his COAT)

Ataxia, dizziness, slurred speech
"Amantadine causes problems with the cerebellA"
a virus has a mutated M2 protein

What drug does it resist
amantadine
Drug with fewer CNS side effects than amantadine, used for influenza A only
Rimantadine
Drug for both Influenza A and B

MOA
Zanamavir, Oseltamivir

Inhibits influenza neuraminidase --> decreases release of progeny virus
Drug to treat RSV, chronic Hep C

MOA
tox
Ribavirin

Competitively inhibits IMP dehydrogenase --> disrupts guanine nucleotide synth

Hemolytic anemia, teratogen
Saquinavir
Ritonavir
Indinavir
Nelfinavir
Amprenavir

class?
use?
toxicity?
protease inhibitors

HAART

Hyperglycemia
GI intolerance
Lipdystrophy
Thrombodytopenia (indinavir)
Zidovudine (ZDV)
Didanosine (ddI)
Zacitabine (ddC)
Stavdine (d4T)

class?
use?
MOA?
NRTI

HAART, prophylaxis in pregnancy (ZDV)

when phosphorylated by viral thymidine kinase, they competitively inhibit nucleotide binding to reverse transcriptase -> chain termination (they lack a 3'OH group)
Zidovudine (ZDV)
Didanosine (ddI)
Zacitabine (ddC)
Stavdine (d4T)

adverse
-bone marrow suppression (reversed by G-CSF and erythropoietin)
-peripheral neuropathy (ddI, ddC, d4T)
-lactic acidosis (nucelosides)
-rash (non-nucleosides)
-megaloblastic anemia (ZDV)
Nevirapine
Efavirenz
Declaviridine

class?
use?
MOA
NNRTI

HAART

Bind to reverse transcriptase (at a different site than NRTIs, do not require phosphorylation)
NNRTI

adverse
same as NRTI
Enfuviritide

class?

use?

adverse?
fusion inhibitor - binds gp41 and inhibits fusion with CD4 T cells

HAART - used in patients with persistent viral replication desite antiretroviral therapy

-Hypersensitivity at injetion site
-increased risk of bacterial pneumonia
Interferons

MOA

adverse
Induce the production of glycoproteins by virus infected cells that block replication of virus

Neutropenia
Drug for chronic hepatitis B and C, Kaposi's sarcoma
IFN-alfa
Drug for MS
IFN-beta
Drug for NADPH oxidase deficiency
IFN-gamma
combo therapy to treat hep C
ribavirin + IFN-a
Antibiotics to avoid in pregnancy

(mnemonic) (8)
SAFE Moms Take Really Good Care
Sulfonamides
Aminoglycosides
Fluoroquinolones
Erythromycin
Metrnidazole
Tetracycline
Ribavirin
Griseofulvin
Chloramphenicol
Antibiotics to avoid in pregnancy

causes kernicterus (damage to baby brain caused by unconjugated bilirubin)
Sulfonamides
Antibiotics to avoid in pregnancy


Causes ototoxicity
Aminoglycosides
Antibiotics to avoid in pregnancy

Cartilage damage
Fluoroquinolones
Drug that causes

Acute cholestatic hepatitis
Macrolide
Antibiotics to avoid in pregnancy

Mutagenesis
Metronidazole
Antibiotics to avoid in pregnancy

Discolored teeth, inhibits bone growth
tetracycline
Antibiotics to avoid in pregnancy


Teratogenic (2)
Ribavirin (antiviral)
Griseofulvin (anti-fungal)
Antibiotics to avoid in pregnancy

gray baby
chloremphenicol