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92 Cards in this Set
- Front
- Back
Cephalexin (Keflex)
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Indications: alt to PCN; Gram + cocci; resistant to staph penicillinase
MOA: inhibits cross-linkage of cell wall peptidoglycans Adverse effects: Cross-sensitivity; hypersensitivity; broader spectrum can lead to opportunistic infections (candidiasis) Class: 1st gen cephalosporin |
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Antibiotics
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Substances produced by the natural metabolic processes of some bugs that can inhibit or destroy other bugs.
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Semisynthetic
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Drugs which are chemically modified in the lab after being isolated from natural sources.
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Synthetic
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The use of chemical rxns to synthesize antimicrobial compounds in the laboratory
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Narrow spectrum
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Effective against a limited number of bugs
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Broad spectrum
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Effective against a wide variety of bugs
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What are the steps involved in choosing the right drug?
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1. ID bug/its sensitivity
2. Be aware of drug interactions/combinations 3. ID site of infection 4. Know the toxicity of the drug 5. Know pt factors 6. Cost |
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What is imipenem/cilastatin?
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A broad spectrum abx
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What is MIC?
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Minimum inhibitory concentration. This is the lowest concentration that inhibits growth in broth.
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What are the pharmacokinetics of the BBB?
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Tight junctions prevent passage so drugs often must be administered intrathecally.
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What are the pharmacokinetics of the prostate?
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It has an acidic environment that favors bases
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What do abx do to kidney fxn?
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Most abx are excreted by the kidneys; this may allow amino glycosides to reach toxic levels
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When is chloramphenicol used?
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For life threatening illness because it is very toxic
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What are the mechanisms of resistance?
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1. DNA mutations or DNA transfer
2. Modification of target 3. Decreased permeability/increased efflux 4. Inactivation of the drug |
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What are the ways bugs can transfer DNA to one another?
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1. Conjugation
2. Transformation 3. Transduction |
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What are the sites of action of abxs?
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1. Cell wall synthesis
2. Metabolism 3. Protein synthesis 4. Nucleic acid synthesis and fxn |
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Which abxs are inhibitors of cell wall synthesis?
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1. B-lactams
2. Vancomycin |
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Which abxs are inhibitors of protein synthesis?
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1. Tetracyclines
2. Aminoglycosides 3. Macrolides 4. Clindamycin 5. Chloramphenicol |
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Which abxs are inhibitors of metabolism?
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1. Sulfas
2. Trimethoprim |
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Which abxs are inhibitors of nucleic acid synthesis and fxn?
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1. Fluoroquinolones
2. Rifampin |
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PCN
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Indications: inf due to: Gram + cocci, Gram + bacilli, Gram - cocci, anaerobes which are B-lactamase negative, spirochetes
MOA: inhibits cross-linkage of cell wall peptidoglycans Adverse effects: occasional hypersensitivity Resistance: B-lactamase |
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Amoxicillin
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Indications: sim to PCN but more Gram - organisms; w/clavulanante, extends spectrum to S. aureus; UTI, sinusitis, otitis, lower resp tract infections
MOA: same as PCN Adverse effects: same as PCN Resistance: sim to PCN; reduced uptake, altered PBP |
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Cephalexin (Keflex)
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Indications: Alt to PCN; resists staph penicillinase
MOA: same as PCN Adverse effects: cross-sensitivity w/ PCN, hypersensitivity; opportunistic infections Class: 1st gen cephalosporin |
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Cefaclor (Ceclor)
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Indications: More Gram -, less Gram +; H. flu
MOA: PCN Adverse effects: hypersensetivity rxns, renal tox Info: po, excreted by kidney, inhib aldehyde dehydrogenase Class: 2nd gen cephalosporin |
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Cefotaxime (Claforan)
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Indications: More Gram +, less Gram -; specific for meningitis
MOA: PCN SE: hypersensetivity rxns, renal tox Info: IM, IV, penetrates CNS, inhib aldehyde hydrogenase Class: 3rd gen cephalosporin |
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Cefepime (Maxipime)
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Indications: meningitis, P. aeruginosa
MOA: PCN; very broad Adverse effects: inc risk of superinfection; renal toxicity; inhibition of aldehyde dehydrogenase Class: 4th gen cephalosporin |
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Carbapenems
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Indications: broadest B-lactam; staph (not MRSA), strep, neisseria, klebsiella, haemophilius, proteus, pseudomonas, bacteroides, anaerobes (except c diff)
MOA: imipenem inhibits cell wall synthesis; cilastatin inhibits renal dihydropeptidase I, which prevents imipenem metabolism Adverse effects: PCN allergy cross reactivity; sz noted w/imipenem |
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Aztreonam
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Indications: aerobic Gram - rods (H. flu, N. gonorrhea, E. coli, Klebseilla, Proteus, Pseudomonas)
MOA: inhibits cell wall synthesis Adverse effects: low cross allergenicity; Gram + superinfections |
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Vancomycin
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Indications: MRSA
MOA: inhibition of peptidoglycan synthesis Adverse effects: fever, chills, redman, shock Resistance: reduced targets |
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What type of inhibition is bacteriostatic?
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Reversible
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What type of inhibition is bacteriocidal?
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Irreversible
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Tetracycline
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Indications: broad; effective against intracellular organisms; Mycoplasma pneumonae, Chlamidae, Rickettsiae
MOA: binds to 30s ribosomal subunit, blocking tRNA access, therefore protein synthesis Adverse Effects: GI, bones, teeth, kidney, liver, photosensitivity Resistance: Decreased influx, increased efflux, decreased binding to 30s subunit, enzymatic inactivation of drug Class: tetracycline |
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Erythromycin
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Indications: diptheria, chlamydial inf, CAP
MOA: binds 50s subunit Adverse Effects: GI, liver Resistance: reduce uptake, increased efflux, enzymatic hydrolysis of drug, altered 50s subunit Class: macrolide |
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Streptomycin
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Indications: Gram - enteric bacteria; used w/B-lactams; plague, tularemia; 2nd line for TB
MOA: inhibits protein synthesis CI: pregnancy SE: oto & nephrotox, vertigo Info: IV, IM, doesn't enter CNS, eye or cells, cleared by kidney, used in combo w/β-lactam ab Resistance: dec influx, inactivation, altered target Class: aminoglycoside |
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Ciproflaxcin (Cipro)
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Indications: Prostatitis, MRSA, P. aeruginosa, UTI, bacterial diarrhea; Gram - aerobic bacteria, Gram +
MOA: inhibitions of DNA gyrase (inhibits nucleic acid synthesis/fxn) Adverse Effects: GI, dizziness, HA, insomnia, hepatitis Resistance: point mutations in DNA gyrase Class: fluoroquinolone |
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Rifampin
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Indications: TB, meningitis, h. flu; Mycobacteria, Gram+/Gram-
MOA: inhibits DNA dependent RNA polymerase of some Gram +/- TB and N. meningitidis Adverse Effects: free of toxicity; orange poop; stigmata Resistance: dec affinity of the polymerase; develops rapidly-use in combination w/ other drugs Class: semisynthetic macrocyclic |
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Sulfisoxazole
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Indications: UTIs, pneumocystis carinii
MOA: inhibits folate metabolism; PO Adverse Effects: hypersensitivity, SJS, precipitates in pee Resistance: utilization of exogenous folate, overproduction of PABA, loss of target affinity Class: sulfas |
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How is TB spread?
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By airborne droplets from 1-5 microns in size
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Why is TB hard to kill w/abx?
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-Slow growing
-Possess a fortified cell wall -Grows within cell -Very good at developing resistance to single agents |
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What is the standard combination therapy for TB?
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RIPE
1. Rifampin 2. Isoniazid 3. Pyrazinamide 4. Ethambutol |
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Isoniazid
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Indications: TB
MOA: prevents synthesis of mycolic acids; bactericidal for growing cells and bacteriostatic for resting cells Adverse Effects: allergic rxns, hepatitis, peripheral neruopathy, jaundice, peripheral neuritis Resistance: aletred mycolic acid synthesis proteins Class: antimycobacterial |
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Rifampicin
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Indications: TB; prophylaxis against meningcoccus, staph inf
MOA: inhibits DNA dependent RNA polymerase Adverse Effects: Resistance: target alteration Class: rifamycins |
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Ethambutol
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Indications: TB
MOA: inhibits arabinosyl transferases-cell wall synthesis Adverse Effects: dose dependent diminished visual acuity |
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Pyrazinamide
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Indications: TB
MOA: inhibits FA synthase I gene Adverse effects: hepatotoxicity, hyperuricemia, gout -Bactericidal at weak pH, where TB is found in macrophages |
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What are the considerations for treating fungal diseases?
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1. Fungi/human cells have the same size large ribosomal subunit while bacteria have a smaller one
2. Fungi are slower growing and larger than bacteria 3. Locations of infection 4. Toxicity associated w/long term therapy 5. Fungi have a chitinous cell wall w/B-glucans 6. Fungi use ergosterol instead of cholesterol 7. Antimetabolites |
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What are the types of fungal infections?
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Superficial/Subcutaneous
Systemic |
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What subtypes are associated with systemic infections?
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-Exogenous
-Opportunistic |
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Caspofungin
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Indications: oropharyngeal/esophageal candidiasis; invasive aspergillosis
MOA: inhibits B-(1,3)-glucan synthase-inhibits cell wall synthesis Adverse Effects: HA, fever, phebitis at site; IV only |
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Amphotericin B
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Indications: systemic fungal infections
MOA: binds to ergosterol; increases permeability of cell membrane Adverse Effects: hypokalemia, acidosis, glomerular damage, renal tubule degeneration, fevers, HA, NVD, anemia, thrombophlebitis Resistance: occurs w/altered sterols |
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Nystatin
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Indications: tx of candida
MOA: binds to cell membrane sterols Info: cream, ointment & powder → mucocutaneous, lozenges → oral candidiasis, PO tabs & suspensions → intestinal candidiasis |
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Clotrimazole (Lotrimin)
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Indications: oral, skin, vaginal infxns; topical: dermatophytes, candidiasis, cryptococcus, tinea (not scalp or nails)
MOA: alters cell membrane permeability Adverse Effects: induction of liver enzymes |
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Miconazole (Monistat)
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Indications: vulvovaginitis
MOA: disrupts cell membrane Adverse Effects: itching, burning, cramps, HA |
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Ketoconazole
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Indications: dermatophytes, mucosal infections, seborrbeic dermatitis; systemic infections
MOA: disrupts cell membranes Adverse Effects: N/V Resistance: Class: |
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Fluconazole
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Indications: thrush, esophageal/systemic candidiasis, cryptococcal meningitis
MOA: disrupts cell membrane Adverse Effects: elevated liver enzymes Resistance: increased efflux through altered demethylase Class: |
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Itraconazole
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Indications: blastomycosis, histoplasmosis, onychomycosis
MOA: disrupts cell membrane |
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Voriconazole
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Indications: invasive aspergillosis, invasive nonalbicans candidiasis
MOA: disrupts cell membrane SE: visual disturbances, altered perception of light, chromatopsia, phytophobia, may ↑ hepatic enzymes (transitory but death possible) Info: po availability 96% vs IV |
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5-Fluorocytosine
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Indications: Candida, Aspergillus, Cryptococcus; prophylaxis w/ AIDS (w/amphotecerine B)
MOA: inhibits DNA/RNA synthesis Adverse Effects: neutropenia, BMD Resistance: transport, cytosine deaminase, anabolism Info: PO, CSF, low protein binding, no metabolism, renal filtration, neutropenia, BMD, combo w/AZT |
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Griseofulvin
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Indications: dermatophytes
MOA: inhibits microtubules; fungicidal/fungistatic Adverse effects: CYT3A4 induction-reduces wafarin, BCPs |
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Amantadine
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Indications: tx/prevent flu A; parkinson's
MOA: inhibits viral uncoating |
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Oseltamivir
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Indications: flu A/B
MOA: neurominidase SE: |
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Acyclovir
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Indications: HSV 1/2; chickenpox
MOA: inhibits DNA synthesis SE: GI and HA, rare nephrotox w/IV; alteration of VTK causes resistance |
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Ganciclovir
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Indications: CMV
MOA: inhibts DNA synthesis SE: myelosuppresion; MOA same as acyclovir |
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Zidovudine
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Indications: HAART
MOA: NRTI SE: myelosuppresion |
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Nevirapine
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Indications: HAART; can be prophylactic for delivery
MOA: NNRTI, binds and inhibits HIV-1rtase SE: SJS (7%) |
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Ritonavir
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Indications: HAART
MOA: protease-inhibitors; inhibits proteolytic cleavage of GAG-POL polyprotein SE: induces lipodystrophy |
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Protease Inhibitors
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Indications:
MOA: HAART SE: induces lipodystrophy |
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Interferons
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Indications: HepB, HepC
MOA: suppresses cell proliferation & inhibits viral replication SE: severe depression, SI/SA, flu-like s/sx |
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Ribavirin
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Indications: RSV, flu, HepC
MOA: selective viral RNA & DNA synthesis |
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PIs
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Indications: HIV
MOA: protease inhibitor; inhibits proteolytic cleavage of gag-pol polyprotein SE: Induces lipodystrophy; resistance to monotherapy |
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Choloroquine
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Indications: clinical cure (all forms), prophylaxis for sensitive organisms, radical cure (P. falciparum & P. malariae)
SE: rash, puritis, lupus-like syndromes, retinal/corneal toxicity, ototoxicity w/high doses CI: porphyria, poriasis |
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Quinine/Quinidine
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Indications: malaria-RBC forms; DOC for chloroquine-resistant plasmodia
SE: may increase uterine contractions, hemolysis/hemoglobinuria, skeletal muscle relaxation from mild NM blockade; PO/IV |
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Mefloquine
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Indications: prophylaxis against all chloroquine-resistant P. vivax (RBC forms)
SE: GI upset, myocardium depression, sz, possible teratogen; PO; sleep/behavior disturbances, elicit latent psych issues |
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Pyrimethamine/Sulfadoxine
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Indications: malaria; presumptive tx; mainly RBC form, some effect on sporozites/pre-RBCs, some effect on 2nd tissue forms
SE: sulfa drug |
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Primiquine
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Indications: malaria; exoerythrocyte and gametocytes; radical cure of p.vivax and p. ovale; won't suppress dz once developed; only drug available for tissue/late stage tx
SE: GI upset, HA, dizziness, |
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Metronidazole
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Indications: E. histolytica, G. lamblia, T. vaginalis; anaerobic bacteria: Bacteroides fragilis & Clostridum difficile
SE: GI irritation, metallic taste, reddish urine, disulfiram-like effect (avoid -OH), carcinogenic in animals, rarely: HA, ataxia, seizures, neuropathies, neutropenia, pregnancy- avoid 1st trimester Info:distributes widely (inc CSF), kills amoeba in GI lumen (mixed amebicide), po & parenteral |
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Paromomycin
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Indications: luminal trophozoites & cysts of E. histolytica, T. vaginalis, tapeworm; combo w/metronidazole for ambebiasis or w/o for asymptomatic amebiasis
SE: SE: GI upset- potential for oto and nephrotox w/paren (aminoglycoside AB) Info: poorly abs from GI tract |
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Sulfatrim
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Indications: pneumocytosis, useful for toxicoplasmosis, porphylaxis
SE: rash, pruritis, cytopenias & transaminase elevation |
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Mebendazole
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Indications: roundworm, whipworm, hookworm, pinworm, trichinosis (w/corticosteriod), may work for some tapeworms
MOA: binds to tubulin, interferes w/protein fxn SE: GI discomfort & diarrhea Info: 10% abs from GI (↓ system tox), caution in preg- may be teratogenic |
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Pyrantel pamoate
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Indications: roundworm, pinworm, hookworm; 2nd DOC for mebendazole
MOA: cholinesterase inhibitor; depolarizing NM blockage in worm SE: dizziness, HA, drowsiness |
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Ivermectin
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Indications: DoC for filaria infestation & onchocerciasis (O. volvulus -> river blindness), also for threadworm, roundworm & cutaneous larva migrans
MOA: alters Cl- permeability/paralyzes parasite SE: puritis, tender lymph nodes, fever; CI w/BBB compromise, don't use w/ drugs that act on the GABA receptor |
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Thiabendazole
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Indications: strongyloidiasis (threadworm), useful for larva migrans and effective in trichinosis and visceral larva migrans
MOA: interferes w/microtubule aggregation SE: anorexia, N/V, diarrhea, pruritus, HA, dizz, visual & neuropsychiatric disturbances, potential for allergic rxns Info: has anti-inflamm properties |
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Niclosamide
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Indications: most tapeworms
MOA: inhbibits anaerobic oxidative phosphorylation SE: HA, skin rashes, pruritis (antigenic material from worms), loose stools abdominal discomfort Info: single dose = cure, not abs not effective against cysticercosis (use laxatives for T. solium) |
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Praziquantel
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Indications: shistosomes, many cestodes, trematodes, cysticercosis
MOA: increases Ca2+ permeability, causes contractions then paralysis SE: low tox, N/V, abdominal discomfort from release of dead worm protein Info: well absorbed, good for systemic infections, little effect on human muscle |
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What causes Pneumocystosis
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Pneumocystis carinii (Pneumocystis jiroveci)
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What causes Toxoplasmosis
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Toxoplasma gondii
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What causes Trichomoniasis
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Trichomonas vaginalis
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What treats E. histolytica?
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Flagyl, paromomycin (cysts)
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What causes amebiasis?
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E. histolytica
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What treats toxicoplasmosis?
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Sulfatrim, pryimethamine+sulfadiazine (DOC)
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What treats giardiasis?
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Flagyl
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What treats triachomonoasis?
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Flagyl
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What treats pneumocystosis?
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Sulfa-trim (DOC)
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