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USMLE1 MicroBio Pharm
N/A
110
Medical
Graduate
04/04/2011

Additional Medical Flashcards

 


 

Cards

Term
Antibiotics
Mechanism of action:
Block cell wall synthesis by inhibition of peptidoglycan cross-linking
Definition
Penicillin, ampicillin, ticarcillin, piperacillin, imipenem, aztreonam, cephalosporins
Term
ABx
Mech
Block peptidoglycan synthesis
Definition
Bacitracin, Vancomycin
Term
Abx
Mech
Disrupt bacterial cell membranes (detergent)
Definition
polymyxins
Term
Abx
Mech
Block nucleotide synthesis (folate pathway)
Definition
sulfonamides (ex. sulfamethoxazole), trimethoprim
Term
Abx
Mech
Block topoisomerases
Definition
fluoroquinalones
Term
Abx
Mech
block mRNA synthesis
Definition
rifampin
Term
Abx
Mech
block protein synthesis at 50S subunit
Definition
chloramphenicol, macrolides, clindamycin, streptogramins (quinupristin, dalfopristin), linezolid
Term
Abx
Mech
Block protein synth at 30S subunit
Definition
aminoglycosides, tetracyclines
Term
Abx Mech Free radical generation, cause DNA breaks
Definition
metronidazole, nitrofurantion
Term
Bacteriostatic antibiotics
Definition
ECSTaTIC
Erythromycin, Clindamycin, Sulfamethoxazole, Trimethoprim, Tetracyclines, Cloramphenicol
(generally, stop protein or DNA synth)
Term
Bacteriocidal Abx
Definition
Very Finely Proficient At Neat Cell Murder Vancomycin, Fluoroquinolones, Penicillin, Aminoglycosides, Nitrofurantoin, Cephalosporins, Metronidazole (any that damage DNA or cell wall, EXCEPT aminoglycosides - weird ones that are cidal anyway)
Term
Penicillin
Mech
Uses
Tox
Definition
bind PBPs, block transpeptidase cross-linking of cell wall, activate autolytic enzymes
Gram-positive organisms and spirochetes.
Hypersensitivity, hemolytic anemia.
Term
Penicillinase-resistant penicillins Mech Uses Tox
Definition
Methicillin, nafcillin, oxacillin, cloxacillin, dicloxacillin Same as penicillin, bulkier R group gives resistance. S. aureus, except MRSA (altered target site) Hypersensitivity. Methicillin: interstitial nephritis.
Term
Aminopenicillins
Mech
Uses
Tox
Definition
Ampicillin, amoxicillin
Same as penicillin. Wide spectrum but penicillinase sensitive. Combine with beta-lactamase inhibitors.
AmOxicillin has greater Oral bioavail.
Gram-positive and some gram-negs (Hflu, Ecoli, Listeria, Proteus, Salmonella, enterococci) HELPS
Hypersensitivity, ampicillin rash, pseudomem. colitis.
Term
Antipseudomonals
Mech
Uses
Tox
Definition
Ticarcillin, carbenicillin, piperacillin (TCP: takes care of pseudomonas)
Same as penicillin, extd. spectrum. Need beta-lactamase inhibitor.
Pseudomonas spp. and other gram negs.
Hypersensitivity.
Term
Beta-lactamase inhibitors
Mech
Uses
Tox
Definition
Clavulanic acid, sulbactam, tazobactam
Inhibit beta-lactamase (penicillinase).
Use with sensitive penicillin Abx.
Term
Cephalosporins: 1st gen
Mech
Uses
Tox
Definition
Cefazolin, cephalexin
same as penicillin, b-lactamase resistant. Cidal.
gram-pos cocci, Proteus mirabilis, E. coli, Klebsiella (PEcK)
Hypersensitivity (cross with penicillin in 5-10%), vit. K deficiency, increased nephrotoxicity with aminoglycosides.
Term
Cephalosporins: 2nd gen
Mech
Uses
Tox
Definition
Cefotoxin, Cefaclor, Cefuroxime
same as penicillin, b-lactamase resistant. Cidal.
gram pos cocci, H flu, Enterobacter, Neisseria, Proteus, Ecoli, Klebsiella, Serratia (HEN PEcKS).
Hypersensitivity (cross with penicillin in 5-10%), vit. K deficiency, increased nephrotoxicity with aminoglycosides. Disulfram-like effect.
Term
Cephalosporins: 3rd gen Mech Uses Tox
Definition

Ceftriaxone, Cefotaxime, Ceftazidime. Same as penicillin, b-lactamase resistant.

Better CSF distribution than previous gens.

Serious gram neg infxns.

Ceftriaxone: meningitis, gonorrhea

Ceftazidime: Pseudomonas.

Hypersensitivity (cross with penicillin in 5-10%), vit. K deficiency, increased nephrotoxicity with aminoglycosides.

Term
Cephalosporins: 4th gen
Mech
Uses
Tox
Definition
Cefepime
Same as penicillins, b-lactamase resistant. Cidal.
IV only. Good CSF dist. More lactamase resistant.
Better activity against Pseudomonas.
Term
Aztreonam
Mech
Uses
Tox
Definition
Monobactam. Similar to penicillin. B-lactamase resistant.
Gram Neg Aerobes Only.
Less toxic. For renal failure pts. No cross-rxn with penicillins/cephalosporins.
Term
Meropenem
Mech
Uses
Tox
Definition
A carbapenem. Same as penicillins. B-lactamase resistant.
IV only. Broad-spec, CSF penetration with inflammed meninges. Tox = last resort.
GI distress, skin rash, CNS probs/seizures.
Term
Imipenem
Mech
Use
Tox
Definition
A carbapenem. Same as penicillins. B-lactamase resistant.
IV only. Broad-spec, CSF penetration with inflammed meninges. Tox = last resort.
ALWAYS GIVE with Cilastatin: prevent inactivation in renal tubules by renal dihydropeptidase I.
GI distress, skin rash, CNS probs/seizures.
Term
Vancomycin
Mech
Use
Tox
Definition
Bind D-ala D-ala portion of cell wall precursors. Resistance: change to D-ala D-lac
Gram positive only. Multidrug resistant organisms. No CSF distribution.
Nephrotoxicity, Ototoxicity, Thrombophlebitis. Flushing: "red man" - prevent with antihistamines.
Term
Aminoglycosides
Mech
Use
Tox
Resistance
Definition
Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin (GNATS)
Inhibit formation of initiation complex (30S), cause mRNA misreads. Require O2. Cidal.
Gram-neg aerobes only: Pseudomoas, Enterobacter, Klebsiella. Synergy with b-lactams. Neomycin for bowel surgery. Endocarditis.
Nephrotoxicity (esp. w/ cephalosporins), Ototoxicity (esp. w/ loop diuretics). Teratogen. Acute muscle paralysis.
Enzymatic alteration of drug: acetylation, phosphorylation, adenylation. Ribosomal alteration. Biofilm formation.
Term
Gentamicin
class?
Definition
Aminoglycoside
Term
Neomycin
class?
special uses?
Tox?
Definition
Aminoglycoside
Topical mostly (neosporin), not absorbed from GI tract.
Can be used to clear bowels (e.g. bowel surg prep).
Very nephro and ototoxic
Term
Amikacin
class?
special use?
special resistance?
Definition
Aminoglycoside
most broad spectrum
sterically blocks enzymatic alteration (adenylation, acetylation, phosphorylation)
Term
Tobramycin
class?
special use?
Definition
aminoglycoside
may be better against Pseudomonas
Term
Streptomycin
Class?
Special use?
Definition
Aminoglycoside
First TB drug, but monotherapy --> resistance.
Term
Linezolid
Mech
Use
Tox
Definition
Blocks formation of initiation complex (30S + 50S). Static.
Backup for MDROs.
Headache, hematologic toxicity, serotonergic toxicity, peripheral or optic neuropathy.
Term
Tetracyclines
Mech
Use
Tox
Resist
Definition
Tetracycline, doxycycline, demeclocycline, minocycline.
Bind 30S and precent tRNA attachment. Little CSF. Static.
Cannot take with milk, antacids, or iron: bind divalent cations and inhibit gut absorption.
Borrelia, H. pylori, Mycoplasma. Broad spec. Has intracellular penetration: Rickettsia, Chlamydia.
GI distress, discoloration of teeth, inhibition of bone growth, photosensitivity, CI for pregnancy.
Resistance by efflux.
Term
Doxycycline
class?
special use?
Definition
Tetracycline
Hepatic elimination - OK for renal failure
For Rickettsial disease
Term
Demeclocycline
class?
special use?
Definition
Tetracycline
ADH antagonist - use as diuretic in SIADH.
Term

Macrolides

Mech Use Tox Resist

Definition

Erythromycin, Azithromycin, Clarithromycin (ACE) Bind 23s rRNA of 50S subunit. Static.

STDs, URIs, Atypical pneunomia (USA!) gram+ cocci, Neisseria.

Prolonged QT interval (esp. Eryth), GI discomfort, acute cholestatic hepatitis, eosinophilia, skin rashes. P450 inhibition (esp. Eryth).

Methylation of 23S rRNA binding site.

Term
Erythromycin
class?
special use?
special toxicity?
special resistance?
Definition
Macrolide
can be used as motillin analog.
Prolonged QT interval, P450 inhibition, severe GI distress.
Efflux resistance, in addition to 50S methylation.
Term
Cloramphenicol
Mech
Use
Tox
Resist
Definition
Inhibits 50S peptidyltransferase. Static.
Hepatic metabolism.
Meningitis (Hflu, Neisseria, S. pneumo). Mycoplasma, chlamydia.
Severe: anemia, aplastic anemia, "gray baby" (undeveloped UDP-glucuronyl transferase).
Plasmid encoded acetyltransferase
Term
Clindamycin Mech Use Tox Resist
Definition

Binds 50S subunit. Static. Anaerobes (B. fragilis, C. perfringens) in aspiration pneumonia/lung abscess (anaerobes above diaphragm). No good for gram-neg anaerobes, UTIs.

Psedomem. colitis, fever, diarrhea. Neuromuscular block (Myasthenia Gravis CI).

50S methylation (like macrolides).

Term
Daptomycin
Mech
Use
Tox
Definition
Binds membranes in calcium depd. manner, depolarizes. Sialyc acid (human) repels.
IV only. Cidal. For MDROs. No CSF entry.
GI irritation, despite IV! Elevated creatinine, muscle weakness)
Term
Sulfonamides Mech Use Tox Resist
Definition

Sulfamethoxazole (SMX), Sulfisoxazole, Sulfadiazine

PABA analog, comp. inhibit dihydropteroate synthetase.

Gram+or-, Nocardia, Chlamydia. Simple UTIs.

Hypersensitivity, *hemolysis with G6PD def., nephrotoxicity, *photosensitivity, kernicterus, *displacement from albumin (e.g. Warfarin), P450 inhibition.

Altered enzyme, increased PABA synth, low uptake.

Term
Trimethoprim
Mech
Use
Tox
Definition
Trimethoprim (TMP)
Inhibits bacteria DHFR. Static.
Synergy with SMX. Recurrent UTIs, Shigella, Salmonella, *PCP pneumonia prophylaxis.
Megaloblastic anemia, leukopenia, granulocytopenia. Rescue with leucovorin (folinic acid).
Term
Sulfa allergy drugs?
Definition
SULFA? Not for FAT Pro Celeb!
Sulfonamides
sulfasalazine
sulfonylureas
furosemide
acetazolamide
thiazide diuretics
probenecid
celecoxib
Term
Nitrofurantoin
Mech
Use
Tox
Definition
Reduction in bacteria makes reactive metabolites, DNA damage. Cidal.
Tx or prophylaxis of UTIs.
GI disturbance, G6PD deficient --> anemia, Pulmonary rxns, hypersensitivity, headache, vertigo, neuropathies.
Term
Fluoroquinolones
Mech
Use
Tox
Resist
Definition
Ciprofloxacin, Norfloxacin, Ofloxacin, Sparfloxacin, Moxifloxacin, Gatifloxacin, Enoxacin, nalidixic acid (a quinolone).
Inhibit DNA topoisomerase II - dsDNA breaks. Cidal.
Cannot take with mild/antacids/iron: divalent cations inhibit absorption (like tetracyclines).
Gram-and+, intracellular. Not for anaerobes. UTIs, resp. infxn, diarrhea, osteomyelitis. Pseudomonas, Neisseria.
GI upset, superinfections, skin rash, headache, dizziness. *Damage to cartilage, tendons: CI in pregnancy and children.
Mutation in DNA topoisomerase II.
Term
Ciprofloxacin
class?
special use?
Definition
fluoroquinolone
excellent lung tissue penetration -> resp. infxns.
Term
Metronidazole Mech Use Tox
Definition
Free radical toxic metabolites, damage DNA. Cidal. *Anti-protozoal. Giardia, Entamoeba, Trichomonas, Gardnerella vaginalis, Anaerobes, H. pylori (GET GAP). Disulfiram rxn with EtOH, metallic taste, headache. (Inhibits P450?)
Term
Polymixins
Mech
Use
Tox
Definition
Polymixin B, colistimethate (polymixin E)
Detergents, disrupt cell membrane.
Resistant gram-neg infxn.
Neurotoxicity, acute renal tubular necrosis.
Term
M. tuberculosis
Prophylaxis?
Tx?
Definition
Pro: INH
Tx: Rifampin, INH, Pyrazinamide, Ethambutol, Streptomycin (RIPES)
Term
M. avium-intracellulare
Prophylaxis?
Tx?
Definition
Pro: Azithromycin
Tx: Azithromycin, rifampin, ethambutol, streptomycin
Term
M. leprae
Tx?
Definition
Dapsone, rifampin, clofazimine
Term
Isoniazid Mech Use Tox
Definition

Inhibit mycolic acid synthesis.

Bacterial catalase-peroxidase needed to activate.

N-acetylated: bimodal half-life.

M. tuberculosis only - Tx and prophylaxis. Neurotoxicity, hepatotoxicity, drug-induced lupus, inhibits P450.

Depletes B6 - pyridoxine (B6) can prevent neurotoxicity, lupus.

Term
Rifampin Mech Use Tox
Definition
Inhibits DNA-dependent RNA polymerase. M. tuberculosis with other drugs, M. leprae to delay resistance to dapsone. Meningoccocal prophylaxis, H. flu prophylaxis for contacts. Minor hepatotoxicity; induces P450; red/orange bodyfluids (4Rs: RNA polymerase inhibitor, Ramps up P450, Red/orange body fluids, Rapid resistance if used alone)
Term
Prophylaxis for meningococcal infection?
Definition
Rifampin, minocycline
Term
Prophylaxis for gonorrhea?
Definition
Ceftriaxone
Term
Prophylaxis for syphilis?
Definition
Benzathine penicillin G
Term
Prophylaxis for recurrent UTIs?
Definition
TMP-SMX
Term
Prophylaxis for Pneumocystis pneumonia in AIDS?
Definition
TMP-SMX (1st choice), aerosolized pentamidine
Term
Prophylaxis for endocarditis with surgical/dental procedures? (controversial?)
Definition
Penicillins
Term
Prophylaxis for Mycobacterium avium-intracellulare?
Definition
Azithromycin
Term
Treatment for MRSA?
Definition
Vancomycin
Term
Treatment for VRE?
Definition
linezolid, streptogramins (quinupristin/dalfopristin)
Term
Amphotericin B
Mech
Use
Tox
Definition
Binds ergosterol; forms membrane pores.
Serious, systemic mycoses. Does not enter CSF; can use intrathecally for fungal meningitis.
Fever/chills, hypoTN, nephrotox (increased distal tubule permeability, increased serum K and Mg), arrythmias, anemia, IV phlebitis. Hydration to reduce nephrotoxicity. Liposomal amphotericin to reduce overall toxicity.
Term
Nystatin
Mech
Use
Definition
Same as amphotericin B
Topical only - too toxic! Can use for GI tract too, not absorbed. Oral candidiasis, vaginal candidiasis, diaper rash.
Term
Azoles
Mech
Use
Tox
Definition
Fluconazole, ketoconazole, clotrimazole, miconazole, itraconazole, voriconazole
Inhibit ergosterol synthesis, by inhibiting P450 enzyme: lanosterol-->ergosterol.
Systemic mycoses.
Hormone synthesis inhibition (gynecomastia), P450 inhibition, fever/chills.
Term
Fluconazole
Class?
Use?
Definition
Azole
Cryptococcal meningitis in AIDS (enters CSF), candidal infections.
Term
Ketoconazole
Class?
Uses?
Tox?
Definition
Azole
Blastomyces, Coccidiodes, Histoplasma (environmental mycoses), Candida. Also use for hypercortisolism: inhibits steroid hmn synth.
Gynecomastia is particular toxicity.
Term
Clotrimazole and miconazole
Class?
Use?
Definition
Azoles
Topical fungal infections
Term
Flucytosine
Mech?
Use?
Tox?
Definition
Inhibits DNA synth by conversion to 5-FU.
Systemic fungal infections along with Amphotericin B.
Nausea, vomiting, diarrhea, *bone marrow suppression.
Term
Caspofungin Mech? Use? Tox?
Definition

Inhibits beta-glucan synthesis, a cell wall carbohydate.

Invasive aspergillosis

GI upset, flushing

Term

Terbinafine

Mech?

Use?

Definition
Inhibit fungal squalene epoxidase, ultimately inhibiting ergosterol synthesis. Use for dermatophytoses, esp. onychomycosis (finger or toenail infxn)
Term
Griseofulvin Mech? Use? Tox?
Definition
Interfere with microtubule formation; disrupt mitosis. Deposits in keratin containing tissue (e.g. nails). Oral drug for superficial infections; inhibits growth of dermatophytes (tinea, "ringworm"). Teratogenic, carcinogenic, confusion, headaches. P450 inducer.
Term
Which Abx classes *generally* have good intracellular activity?
Definition
Macrolides
Fluoroquinolones
Chloramphenicol
Term
Which drugs/classes *generally* have good activity against anaerobes?
Definition
Clindamycin
Metronidazole
Carbapenems
Term
Which drugs/classes are effective against aerobes only?
Definition
Aminoglycosides
Aztreonam
~Fluoroquinolones (not great against anaerobes)
Term
Which drugs generally work against gram + only?
Definition
Penicillins
Macrolides
~Clindamycin (not effective on Gram - aerobes [E. coli])
Early generation Cephalosporins
Term
Which drugs generally work against gram - only?
Definition
Aztreonam
Aminoglycosides
Term
Which drugs enter CSF well?
Definition
Later gen. Cephalosporins
Carbapenems (when meninges inflammed)
Linezolid
Sulfonamides
Trimethoprim
Acyclovir/Ganciclovir
Anti-tuberculosis
Fluconazole
Zidovudine
Nevirapine
Term
Pyrimethamine
Use?
Mechanism?
Tox?
Definition
Anti-protozoan; best for P. falciparum, toxoplasmosis with sulfadiazine.
Inhibits plasmodial DHFR.
Not for pregnant women; give with folinic acid.
Term

Suramin

Use?

Mechanism?

Definition

Antiprotozoan (sleeping sickness)

no CNS entry (S = serum only)

Inhibits energy metabolism enzymes.

Term
Melarsoprol Use? Mechanism?
Definition

Antiprotozoan; (sleeping sickness)

+CSF entry (like MELAtonin)

Inhibits sulfhydryl groups in parasite enzymes.

Term
Nifurtimox Use? Mechanism?
Definition

Antiprotozoan (Chagas dz)

Forms oxygen free radicals

Term
Sodium stibogluconate Use? Mechanism?
Definition

Antiprotozoan (Leishmaniasis)

Inhibits glycolysis at PFK reaction

Term
Chloroquine
Use?
Mechanism?
Definition
Antiprotozoan; Chloroquine sensitive malaria.
Blocks plasmodium heme polymerase, accumulation of toxic hemoglobin breakdown products.
Term
Primaquine
Use?
Mechanism?
Definition
Antiprotozoan; kills latent malaria parasites in hepatocytes (vivax, ovale), prevents reactivation.
Same as chlorquine - use with chloroquine or quinine plus doxycycline for vivax, ovale.
Term
Mebendazole/Albendazole
Use?
Mechanism?
Definition
Antihelminthic
All intestinal helminths (trichonosis, strongyloides, nematodes, tapeworms/cestodes)
Inhibit glucose uptake and microtuble synth
Term
Pyrantel pamoate
Use?
Mechanism?
Definition
Antihelminthic; *No effect on tapeworms or flukes.
Stimulates nicotinic receptors --> contraction --> depolarization paralysis.
Term
Ivermectin
Use?
Mechanism?
Definition
Antihelminthic; "filarial" infections: lymphatic filariasis, onchocerciasis, loa loa
Intensifies GABA neurotransmission, immobilizes. No CNS entry, no effect on humans.
Term
Praziquantel
Use?
Mechanism?
Definition
Antihelminthic; tapeworms and flukes.
Increases membrane permeability to calcium, causing contraction and paralysis.
Term
Amantidine/Rimantidine
Mech
Use
Tox
Resist
Definition
Blocks M2 ion channel; virus can not decoat in vesicle.
Amantidine: Prophylaxis and tx for Influenza A only. Parkinson's Dz (affects catechol synth). Rimantidine does not cross BBB, fewer CNS SEs.
Ataxia, dizziness, slurred speech.
Mutated M2 protein, 90% of influenza A now resistant (rarely used anymore.)
Term
Zanamivir, Oseltamivir, Pirimivir Mech Use Tox Resist
Definition

Inhibit neuraminidase, progeny virus can't release.

Influenza A and B, prevention and shorten course.

Zanam: bronchospasm, CI asthma, COPD.

Oseltam: mild GI.

Mutation of neuraminidase resists Oseltamivir, not Zanamivir currently. Strain dependent.

Term
Ribavirin
Mech
Use
Tox
Definition
Guanine analog, comp. inhibits IMP dehydrogenase.
RSV, chronic HepC
No selectivity for viral enzyme! Hemolytic anemia, severe teratogen. Rarely used.
Term
Acyclovir, Valacyclovir, Famciclovir
Mech
Use
Tox
Resist
Definition
Guanosine analog. Monophosphorylated by viral thymidine kinase. Triphosphate formed by cell enzymes. Pref. inhibits viral DNA polymerase by chain termination. Valacyclovir is valine ester prodrug. Famciclovir is topical form.
HSV, VZV, EBV. HSV lesions and encephalitis. No effect on latent HSV and VZV.
Some nephrotoxicity (precipitation): hydrate!
Mutation/lack in viral thymidine kinase/DNA pol.
Term
Ganciclovir
Mech
Use
Tox
Resist
Definition
Guanosine analog. Phosphorylated by viral kinase. Less selectivity for viral DNA polymerase than acyclovir.
CMV, esp. immunocompromised pts.
Bone marrow: leukopenia, neutropenia, thrombocytopenia. Renal toxicity.
Mutated polymerase, mutated/lack kinase.
Term
Foscarnet
Mech
Use
Tox
Resist
Definition
Pyrophosphate analog. Binds viral DNA polymerase. No activation needed.
CMV retinitis in immunocomp pts when ganciclovir fails; acyclovir-resistant HSV.
Nephrotoxicity. Calcium chelation, low Ca, Mg, seizures.
Mutated DNA polymerase.
Term
Cidofovir
Mech
Use
Definition
Nucleotide analog of cytosine monophosphate. Inhibits viral DNA polymerase. Does not require viral kinase activation.
Use Cidofovir or Foscarnet in kinase-deficient viruses (acyclovir/ganciclovir resistant)
Term
What constitutes a HAART regimen?
Definition
3 drugs (prevent resistance):
2 NucleosideRTIs + 1 Protease inhib.
2 NucleosideRTIs + 1 Non-NucleosideRTI
Term
Protease Inhibitors
Mechanism
Use
Toxicity
Definition
"-navir": Saquinavir, Ritonavir, Indinavir, Nelfinavir, Amprenavir
Inhibit protase (pol gene), cleaves HIV proteins into functional parts.
HIV, can be part of HAART.
Inhibit P450. Hyperglycemia, GI, lipodystrophy, thrombocytopenia (indinavir).
Term
Nucleoside Reverse Transcriptase Inhibitors Mech Use Tox
Definition

NRTIs: Zidovudine (ZDV or AZT), Didanosine (ddI), Zalcitabine (ddC), Stavudine (d4T), Lamudivine, Abacavir.

Chain termination (no 3'-OH). Need activation by host cell thymidine kinases. Selective for viral reverse transcriptase.

2 are always needed as part of HAART! ZDV for prophylaxis, during pregnancy to prevent vertical trans.

Bone marrow suppression, periph neuropathy, lactic acidosis (except abacavir), rash, megaloblastic anemia, lipoatrophy, GI intolerance (ZDV only).

Term
Non-Nucleoside Reverse Transcriptase Inhibitors
Mech
Use
Tox
Definition
Nevirapine, Efavirenz, Declaviridine (Never Ever Deliver nucleosides).
Bind reverse transcriptase, non-competitive inhibition. No kinase activation needed.
HIV, can be part of HAART.
Hypersensitivity (Stevens-Johnson), hepatotoxic, GI. Nevirapine can induce P450.
Term

Zidovudine

Class?

Special use?

Special toxicity?

Definition

Nucleoside Reverse Transcriptase Inhibitor

Prophylaxis: general or during pregnancy

Megaloblastic anemia, GI upset

Term
Enfuvirtide
Mech
Use
Tox
Definition
Fusion inhibitor. Binds gp41 subunit, prevents fusion with CD4 cells.
Used for HIV failure on HAART.
*Injection site irritation. Hypersensitivity (peptide drug). Increased bacterial pneumonia risk (mech?)
Term
Maraviroc
Mech
Use
Tox
Definition
Non-competitive inhibitor of CCR5, prevents HIV entry.
Used for HIV failure on HAART.
*Hepatotoxicity.
Term
Raltegravir
Mech
Use
Tox
Definition
Inhibits viral integrase, can't insert HIV DNA into genome.
Failure on HAART.
Few toxicities.
Term
Interferons
Mech
Uses
Tox
Definition
IFN-alpha, beta, gamma
Block replication of RNA and DNA viruses.
IFN-a: HepB, HepC, Kaposi's sarcoma (HHV8)
IFN-b: MS
IFN-g: NADPH oxidase def. (CGD)
Neutropenia.
Term
Interferons
Mech
Uses
Tox
Definition
IFN-alpha, beta, gamma
Block replication of RNA and DNA viruses.
IFN-a: HepB, HepC, Kaposi's sarcoma (HHV8)
IFN-b: MS
IFN-g: NADPH oxidase def. (CGD)
Neutropenia.
Term
Antibiotics to avoid during pregnancy?
Toxicity?
Definition
SAFE Moms Take Really Good Care
Sulfonamides - kernicterus
Aminoglycosides - ototoxicity
Fluoroquinolones - cartilage damage
Erythromycin - acute cholestatic hepatitis in mom
(and Clarithromycin - embryotoxic)
Metronidazole - mutagenesis
Tetracyclines - discolored teeth, bone growth inhibition
Ribavirin - teratogenic
Griseofulvin - teratogenic
Chloramphenicol - "gray baby"
Term
Anti-bacterials OK for pregnancy?
Definition

Penicillins, Cephalosporins, Azithromycin, Nitrofurantoin

(Pregnancy CAN!)

Term
Pyrazinamide
Mech
Use
Tox
Definition
Converted to pyrazinoic acid by mycobacterial enzyme pyrazinamidase, lowering pH inside bacterium
Anti-tuberculosis
hepatotoxicity
Term
Ethambutol
Mech
Use
Tox
Definition
Inhibit arabinosyl transferase, inhibiting synthesis of mycobacterial cell wall.
Anti-TB
Red/Green colorblindness, optic neuropathy, hepatic toxicity
Term
Streptogramins
Definition

think "pristin"

Quinupristin, Dalfopristin, Pristinamycin

Block translation at 50S subunit

VRE and VRSA

Arthralgias/myalgias, N/V, diarrhea, rash, headache, phlebitis, jaundice. P450 inhibition.

MLS resistance (methylation)

 

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