Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
109 Cards in this Set
- Front
- Back
|
Penicillin G
|
Class: Penicillin
Disease: Gram+ cocci, Gram- cocci (meningococci), Gram+ rods (anthrax, diptheria), Gram- rods (bacteriodes), syphilis, recurrent rheumatic fever, H. flu, enterococcal endocarditis, leptospirosis Mechanism:inhibits transpwpdidation that results in cross-linking of cell wall; activates autolytic enzymes Route:IV, oral Side effect: procaine syndrome, convulsions Contraindication:allergy Resistance:inactivated by beta lactamases |
|
|
Penicillin V
|
Class: penicillin
Disease:same as PCN G Mechanism: inhibits transpepdidation that results in cross-linking of cell wall; activates autolytic enzymes Route:oral Side effect: Contraindication: allergy Resistance:inactivated by beta lactamase |
|
|
Amoxicillin
(+ clavulanic acid = augmentin) |
Class: penicillin
Disease: Hemophilus, gonorrhea Mechanism:inhibits transpepdidation that results in cross-linking of cell wall; activates autolytic enzymes Route:oral Side effect: nausea, vomiting, diarrhea Contraindication: allergy Resistance: inactivated by beta lactamase |
|
|
Ampicillin
|
Class: penicillin
Disease: Gram+ rod (listeria), Gram- rod (H. pylori) Mechanism: inhibits transpepdidation that results in cross-linking of cell wall; activates autolytic enzymes Route: oral Side effect: nausea, vomiting, diarrhea, skin rashes Contraindication: allergy Resistance: inactivated by beta lactamases |
|
|
Ticarcillin
|
Class: penicillin
Disease: Gram- rods, especially pseudomonas Mechanism: inhibits tranpeptidation that results in cross-linking of cell wall; activates autolytic enzymes Route: not oral Side effect: Contraindication: allergy Resistance: inactivated by beta lactamase |
|
|
Nafcillin
|
Class: penicillin
Disease: staph Mechanism: inhibits transpeptidase which results in cross-linking of cell wall; activates autolytic enzymes Route: IV Side effect: Contraindication: allergy Resistance: penicillinase resistant |
|
|
`Clavulanic Acid
|
Class: Beta-lactamase inhibitor
Disease: used with amoxicillin Mechanism: inhibits beta lactamase Route: Side effect: Contraindication: Resistance: |
|
|
Sulbactam
|
Class: beta lactamase inhibitor
Disease: Mechanism: Route: Side effect: Contraindication: Resistance: |
|
|
Tazobactam
|
Class: beta lactamase inhibitor
Disease: Mechanism: Route: Side effect: Contraindication: Resistance: |
|
|
Sulfamethoxazole
|
Class: sulfa
Disease: UTI, Nocardia, drug-resistant malaria & toxoplasmosis, recurrent rheumatic fever Mechanism: competes with PABA for enzyme dihydropteroate synthestase and blocks folate synthesis Route: oral, slow IV Side effect: toxicity-bone marrow depression, cyralluria, agranulocytosis, aplastic anemia, kernicterus, Stevens-Johnson syndrome Contraindication: pregnancy, anticoagulants (displaces them from albumin), synergistic effect with sulfonyl urea causing hypoglycemia, G6PD deficiency causes hemolytic anemia Resistance: |
|
|
Trimethoprim
|
Class:
Disease: acute UTI Mechanism: inhibits folate reduction (inhibits DHFR) Route: oral Side effect: toxicity-bone marrow depression, crystalluria, agranulcytosis & aplastic anemia, kernicterus, Stevens-Johnson syndrome Contraindication: pregnancy, anticoagulants Resistance: |
|
|
Co-Trimoxazole
(sulfamethoxazole + trimethoprim) |
Class:
Disease: Pneumocystic carinii, Shigella & Salmonella, UTI, otitis media, respiratory tract infection, gonococcal urethritis, oralphayngeal gonorrhea Mechanism: synergistic effect Route: oral Side effect: fever, rash, leukoplakia, folate deficiency, hepatitis Contraindication: pregnancy Resistance: |
|
|
Cefalexin
|
Class: 1st gen. cephalosporin
Disease: gram+ cocci Mechanism: inhibits transpepdidation that results in cross-linking, inactive against MRSA & enterococci Route: oral Side effect: same a PCN Contraindication: Resistance: inactivated by beta-lactamases |
|
|
Cefazolin
|
Class: 1st gen Cephalosporin
Disease: gram+ cocci, E. coli, Klebsiella, Proteus Mechanism: inhibits transpepdidation that results in cross-linking; inactiave against MRSA or enterococci Route: Side effect: same as PCN Contraindication: Resistance: inactivated by beta lactamase |
|
|
Cefuroxime
|
Class: 2nd gen. Cephalosporin
Disease: gram-, meningitis Mechanism: inhibits transpepdidation that results in cross linking Route: Side effect: same as PCN Contraindication: Resistance: inactivated by beta-lactamase |
|
|
Cefotetan
|
Class: 2nd gen Cephalosporin
Disease: Gram-, B. fragilis Mechanism: inhibits transpepdidation that results in cross-linking Route: Side effect:same as PCN Contraindication: Resistance:inactivated by beta lactamase |
|
|
Ceftriaxone
|
Class: 3rd gen Cephalosporin
Disease: huge gram- coverage, meningitis, Haemophilius, Pseudomonas Mechanism: inhibits transpepdidation that results in cross-linking Route: Side effect: PCN like Contraindication: Resistance: inactivated by beta lacatamase |
|
|
Cefotaxime
|
Class: 3rd gen Cephalosporin
Disease: huge gram- coverage, meningitis, Haemophilus, Neisseria Mechanism: inhibits transpepdidation that results in cross-linking Route: Side effect: same as PCN Contraindication: Resistance: inactivated by beta lactamase |
|
|
Ceftazidime
|
Class: 3rd gen Cephalosporin
Disease: huge gram- covrage, meningitis, pseudomonas Mechanism: inhibits transpepdidation that results in cross-linking Route: Side effect: same as PCN Contraindication: Resistance: inactivated by beta lactamase |
|
|
Cefepime
|
Class: 4th gen Cephalosporin
Disease: P. aeruginosa, Enterobacteria, S. aureus, S. pneumoniae, Haemophilus, Neisseria Mechanism: inhibit transpeptidation that results in cross-linking Route: Side effect: same as PCN Contraindication: Resistance: inactivated by beta lactamase |
|
|
Aztreonam
|
Class: Penems & Monobactams
Disease: substitute for amino-glucosides, Klebsiella, P. aeruginosa, Serratia Mechanism: bind to PBP & inhibit cell wall synthesis; synergistic with aminoglycosides Route: IM/IV Side effect: no renal toxicity Contraindication: PCN allergy pts CAN tolerate Resistance: resistant to beta lactamase |
|
|
Imipenem
|
Class: Penems & Monobactams
Disease: Enterobacter, Staph, B. fragillis, P. aeruginosa Mechanism: Route: Side effect: nausea, vomiting, diarrhea, skin rash, seizure with toxicity Contraindication: PCN allergy Resistance: resistant to most beta lactamase |
|
|
Cliastatin
|
Class: Penems & Monobactams
Disease: use with imipenem Mechanism: NOT an antibiotic; inhibits renal dihydropeptidase I and thus prevents penem degradation Route: Side effect: Contraindication: Resistance: |
|
|
Tetracycline
|
Class:
Disease: Chlamydia, Vibrio cholera, Plague, Lyme, protozoa, prophylax meningococcal meningitis Mechanism: binds to 30S subunit and blocks binding of tRNA to A site on ribosome; bacteriostatic; bacteria have TC-uptake system and can concentrate TCs Route: oral Side effect: very toxic-retard growth in bones, suprainfection, hapatic dysfunction, renal toxicity Contraindication: pregnancy Resistance: efflux of tetracyclines out of bacteria; plasmid mediated; wide-spread |
|
|
Doxycycline
|
Class:
Disease: prophylax for traveler's diarrhea, prostate infections, prophylax for malaria Mechanism: Route: Side effect: photo-sensitization Contraindication: Resistance: |
|
|
Streptomycin
|
Class: Aminoglycosides
Disease: severe infections only - endocarditis caused by enterococci or virdans, TB Mechanism: binds to P12 receptor protein on 30S subunit; blocks formation of mRNA+formyl methionine+tRNA complex; mRNA is misread; wrong AA inserted Route: IM Side effect: nephrotoxic, neuromuscular blockade, ototoxicity, Contraindication: myasthenia gravis Resistance: deletion of P12 gene; plasmid dependent production of destructive enzymes; mutant porins; mutant 30S ribosome |
|
|
Neomycin
|
Class: Aminoglycoside
Disease: Severe infection only , gram- enteric, in combo with beta-lactams, pseudomonas, chronic UTI, E. coli, Klebsiella Mechanism: binds to P12 receptor protein on 30 S subunit; blocks formation of mRNA+formyl methionine+tRNA complex; mRNA is misread; wrong AA inserted Route: IM Side effect: nephrotoxic, neuromuscular blockade, ototoxicity Contraindication: myasthenia gravis Resistance: deletion of P12 gene; plasmid-dependent production of destructive enzymes; mutant porins; mutant 30S ribosome |
|
|
Gentaminicin
|
Class: Aminoglycoside
Disease: Severe infections only; gram- enteric; in combo with beta-lactams; pseudomonas; chronic UTI; E. coli, Klebsiella Mechanism: binds P12 receptor protein on 30s subunit; blocks formation of mRNA+formyl methionine+tRNA complex; mRNA misread; wrong AA inserted Route: IM Side effect: nephrotoxic, neuromuscular blockade, ototoxicity Contraindication: myasthenia gravis Resistance: deletion of P12 gens; plasmid dependent production of destructive enzymes; mutant porins; mutant 30S ribosome |
|
|
Tobramycin
|
Class: aminoglycoside
Disease: severe infections only; gram- enteric; in combo with beta lactams; pseudomonas; chronic UTI; E. coli, Klebsiella Mechanism: binds to P12 receptor protein on 30S subunit; inhibits formation of mRNA+formyl methionine+tRNA complex; mRNA misread; wrong AA inserted Route: IM Side effect: nephrotoxic, neuromuscular blockade, ototoxicity Contraindication: myasthenia gravis Resistance: deletion of P12 gene; plasmid-dependent production of destructive enzymes; mutant porins; mutant 30S ribosome |
|
|
Chloramphenicol
|
Class:
Disease: meningitis, TC disease, typhoid, brain abscess caused by anaerobes, eye infections Mechanism: bins to 50S ribosome and inhibit transpeptidation Route: Side effect: pancytopenia, bone marrow distrubances, Gray Baby syndrome, death Contraindication: G6PD deficiency Resistance: chloramphenicol acetyl transferase (from plasmid gene) inactivates drug |
|
|
Vancomycin
|
Class:
Disease: Only gram+; meningitis caused by staph; MRSA; C. diff suprainfection Mechanism: prevents peptidoglycan construction (inhibits cell wall mucopeptide formation) Route: Side effect: nephrotoxicity, ototoxicity, thrombophlebitis, diffuse flushing Contraindication: Resistance: |
|
|
Bacitracin
|
Class:
Disease: gram+ cocci; eye and skin infections Mechanism: interferes with regeneration of lipid carrier in peptidoglycan synthesis by blocking its dephosphorylation Route: Side effect: Contraindication: Resistance: |
|
|
Ciprofloxacin
|
Class: Quinolone
Disease: multi-drug resistant UTI, Pseudomonas, Shigella, Salmonella, E coli, Helicobacter, infection of soft tissue, bones, joints, intrabdominal & respiratory tract infections, gonococcal, chlamydia, prophylax travelers diarrhea Mechanism: inhibits DNA gyrase Route: oral Side effect: GI problems, suprainfection with strep and candida Contraindication: pts <18 Resistance: |
|
|
Norfloxacin
|
Class: Quinolone
Disease: multi-drug resistant UTI, Pseudomonas, Shigella, Salmonella, E coli, Helicobacter, infection of soft tissue, bones, joints, intrabdominal & respiratory tract infections, gonococcal, chlamydia, prophylax travelers diarrhea Mechanism: inhibits DNA gyrase Route: oral Side effect: GI problems, suprainfection with strep and candida Contraindication: pts <18 Resistance: |
|
|
Oflaxacin
|
Class: Quinolone
Disease: multi-drug resistant UTI, Pseudomonas, Shigella, Salmonella, E coli, Helicobacter, infection of soft tissue, bones, joints, intrabdominal & respiratory tract infections, gonococcal, chlamydia, prophylax travelers diarrhea Mechanism: inhibits DNA gyrase Route: oral Side effect: GI problems, suprainfection with strep and candida Contraindication: pts <18 Resistance: |
|
|
Erythromycin
|
Class: macrolide
Disease: PCN allergic pts, Mycoplasma pneumoia, Chlamydia, Legionella, Helicobacter, Listeria, Neisseria, Bordetella pertussis, Treponema, Campylobacter, Gram+ Mechanism: binds to 50S ribosome; inhibits aminoacyl translocation Route: Side effect: Contraindication: Resistance: plamid-mediated gene encodes alternate protein on 50S ribosome |
|
|
Azithromycin
|
Class: macrolilde
Disease: Chlamydia, H.flu, Mechanism: Route: Side effect: Contraindication: Resistance: |
|
|
Clarithromycin
|
Class: macrolide
Disease: H.pylori, H.flu Mechanism: Route: Side effect: Contraindication: Resistance: |
|
|
Clindamycin
|
Class:
Disease: B. fragilis Mechanism: inhibits protein synthesis Route: Side effect: suprainfection with C.diff, hepatotoxicity Contraindication: Resistance: |
|
|
Metronidazole
|
Class:
Disease: Bacteroides, Clostridia, Pseudomembranous colitis Mechanism: inhibits DNA synthesis, bactericidal Route: oral, IV Side effect: minor GI, minor CNS, interferes with ETOH metabolism Contraindication: Resistance: |
|
|
Polymyxins
|
Class:
Disease: topical for eye & ear (with bacitracin or neomycin) Mechanism: binds to phosphotidyl enthanolamine, disrupts transport; detergent-like action Route: Side effect: Contraindication: Resistance: |
|
|
Zidovudine
(AZT) |
Class: NRTI
Disease: AIDS; reduces incidence of opportunistic infections, stailize weight, reduces dementia, delays AIDS onset, reduces transplacental transmission, prophylaxis Mechanism: analogue of pyrimidine thymidine; inhibits reverse trancriptase Route: IV, oral Side effect: anemia, neutropenia, GI, skin rash, paresthesia, fever, headache, abn liver function, myopathy Contraindication: Resistance: point mutation in reverse transcriptase leads to reduced drug sensitivity, response wanes with long-term use |
|
|
Zalcitabine
(ddC) |
Class: NRTI
Disease: AIDS; used in combination with AZT Mechanism: inhibits reverse transcriptase; activated in T cells by different phosphorylation pathway than AZT Route: oral Side effect: neuropathy, GI, headache, mouth ulcers, nail changes, edema, malaise Contraindication: Resistance: |
|
|
Lamivudine (3TC)
|
Class: NRTI
Disease: AIDS; used in combination with AZT Mechanism: a dideoxynucloside, terminates synthesis of proviral DNA chain, inhibits reverse trancriptase Route: oral Side effect: pancreatitis Contraindication: Resistance: resistance to AZT develops more slowly when given in combo with 3TC |
|
|
Didanosine
(ddI) |
Class: NRTI
Disease: AIDS; switching to ddI after AZT therapy shown to be beneficial Mechanism: chain terminator, inhibits reverse transcriptase Route: oral Side effect: peripheral neuropathy, pancreatitis, headache, GI, skin rash, bone marrow depression, altered liver function Contraindication: Resistance: resistance with long-term use, but less so than with AZT |
|
|
Tenofovir
|
Class: NtRTI
Disease: AIDS; used in combination with other antiretrovirals Mechanism: does not require phosphorylation or other modification for activation, inhibit reverse transcriptase Route: Side effect: renal failure, Fanconi syndrome, proteinuria, tubular necrosis Contraindication: Resistance: |
|
|
Nevirapine
|
Class: NNRTI
Disease: AIDS; treatment AIDS and related symptoms, prevention of transplacental transmission Mechanism: do no require phosphorylation for activation; bind to lipophilic pocket of reverse transciptase distinct from substrate binding site; inhibit P-450 system, so decrease protease inhibitors; act synergistically with NRTI Route: Side effect: rash, fever, headache, fatigue, nausea Contraindication: Resistance: rapid resistance if given alone |
|
|
Delavirdine
|
Class: NNRTI
Disease: AIDS Mechanism: do not require phosphorylation for activation; bind to lipophilic pocket of reverse transcriptase distinct from substrate binding site; inhibit P-450 system, so decrease metabolism of protease inhibitors; act synergistically with NRTI Route: Side effect: rash Contraindication: Resistance: rapid if given alone |
|
|
Efavirenz
|
Class: NNRTI
Disease: AIDS Mechanism: do not require phosphorylation for activation; bind to lipophilic pocket of reverse transcriptase distinct from substrate binding site; inhibit P450 system, so decrease metabolism of protease inhibitors; act synergistically with NRTI Route: Side effect: CNS effects: dizziness, drowsiness, insomnia, headache, confusion, amnesia, agitation, depression, nightmares; induces metabolic enzyme CYP3ZA4, which reduces plasma methodone and serum levels of other antiviral Contraindication: Resistance: |
|
|
Indinavir
|
Class: protease inhibitor
Disease: AIDS Mechanism: inhibition of HIV-1 protease (cleaves precursor protein to generate viral proteins essential for final stage of viral formation) Route: Side effect: increased bilirubin, nephrolithiasis Contraindication: Resistance: rapid at low dose |
|
|
Nelfinavir
|
Class: protease inhibitor
Disease: AIDS Mechanism: inhibition of HIV-1 protease (cleaves precursor protein to generate viral proteins essential for final stage of viral formation) Route: Side effect: diarrhea, asthenia, headache, moderate hypertension Contraindication: Resistance: |
|
|
Ritonavir
|
Class: protease inhibitor
Disease: AIDS Mechanism: inhibition of HIV-1 protease (cleaves precursor protein to generate viral proteins essential for final stage of viral formation) Route: Side effect: GI, elevated aminotransferasea and triglyceride Contraindication: Resistance: |
|
|
Saquinavir
|
Class: protease inhibitor
Disease: AIDS Mechanism: inhibition of HIV-1 protease (cleaves precursor protein to generate viral proteins essential for final stage of viral formation) Route: Side effect: mild diarrhea, abd discomfort, nausea, Contraindication: Resistance: after about 1 year due to single amino acid mutation |
|
|
Lopinavir/Ritonavir
|
Class: protease inhibitor
Disease: AIDS; sub-therapeutic dose of ritonavir inhibits CYP3A-mediated metabolism thereby increasing lepinavir concentration Mechanism: inhibition of HIV-1 protease (cleaves precursor protein to generate viral proteins essential for final stage of viral formation) Route: Side effect: Contraindication: Resistance: low due to combination |
|
|
Enfuvirtide
|
Class: fusion inhibitor
Disease: AIDS; pts with persistant HIV-1 replication despite tx with other antivirals Mechanism: mimics HR2 region of gp41 viral glycoprotein and binds to gp41, block entry into cell Route: Side effect: Contraindication: Resistance: no cross-resistance found |
|
|
Acyclovir
|
Class:
Disease: HSV; shingles, chicken pox, Herpes simpled Mechanism: converted 1st to a monophosphate by viral thymidine kinase, then to a triphosphate by mammalian kinase: acyclovir-triphosphate inhibits viral DNA polyerase Route: oral, IV Side effects: local inflammation, renal dysfunction, nausea, headache Contraindications: Resistance: mutations in viral genes for thymidine kinase or DNA polymerase lead to resistance |
|
|
Valacyclovir
|
Class:
Disease: HSV; shingles, chicken pox, herpes simplex Mechanism: an L-valyl ester of acyclovir; almost completely metabolize to acyclovir, but higher bioavailability Route: oral Side effects: similar to acyclovir, generally well tolerated Contraindications: Resistance: |
|
|
Vidarabine
|
Class:
Disease: HSV; Herpes simplex in neonates, herpes associated encephalitis, Varicella-zoster in AIDS pts Mechanism: phosphorylated to triphosphate which inhibits DNA polymerase Route: IV, topical Side effects: GI, neurotoxicity, bone marrow disturbance, carcinogenic Contraindications: Resistance: |
|
|
Idoxuridine
|
Class:
Disease: HSV; Herpes simplex and varicella-zoster infections of the eye Mechanism: phosphorylated by cellular kinases and incorporated into both viral and host DNA Route: topically (dissolved in dimethy-sulfoxide) Side effects: irritations/contact dermatitis Contraindications: Resistance: |
|
|
Ganciclovir
|
Class:
Disease: CMV; life or sight threatening CMV, phophylaxis in transplant pts Mechanism: guanosine analogue; phosphorylated 1st by viral protein kinase, then by host kinase to form triphosphate, which competes with guanosine triphosphate for incorporation into viral DNA Route: IV Side effects: bone marrow suppression; severe myelosuppression; potentially carcinogenic Contraindications: Resistance: |
|
|
Foscarnet
|
Class:
Disease: CMV; 2nd line for CMV eye infections Mechanism: pyrophosphate analogue; binds to pyrophosphate binding site and inhibits viral DNA polymerase Route: IV Side effects: serious nephrotoxicity Contraindications: Resistance: some reported |
|
|
Ribavirin
|
Class:
Disease: early stages of Lassa fever; RSV Mechanism: adenosine/guanosine analogue; alters viral DNA and mRNA synthesis Route: IV, oral, aerosol Side effects: teratogenic, embryotoxic, oncogenic, anemia Contraindications: Resistance: |
|
|
interferon alpha2b
|
Class:
Disease: HBV, Kaposi sarcoma, Hairy cell leukoplakia Mechanism: induce host enzymes that inhibit translation of viral mRNA; IFN receptors (gangliosides) inhibit viral replication Route: Side effects: fever, headache, lassitude, myalgia, bone marrow suppression, CV changes, rash, alopecia, altered thyroid and renal function, exacerbate autoimmune disease, hearing loss or tinnitus Contraindications: Resistance: |
|
|
interferon alpha2b and Ribavirin
|
Class:
Disease: HCV Mechanism: induce host enzymes that inhibit translation of viral mRNA; IFN receptors (gangliosides) inhibit viral replication Route: Side effects: fever, headache, lassitude, myalgia, bone marrow suppression, CV changes, rash, alopecia, altered thyroid and renal function, exacerbate autoimmune disease, hearing loss or tinnitus Contraindications: Resistance: |
|
|
Oseltamivir
|
Class:
Disease: tx and prevention of flu Mechanism: inhibition of viral neuraminidase; alteration of virus particle aggregation and release Route: oral Side effects: renal impairment Contraindications: Resistance: associated with changes in AA sequence |
|
|
Zanamivir
|
influenza
|
|
|
Amphotericin B
|
Class: anti-fungal
Disease: fungal meningitis, balstomyces, coccidioides, histoplasma, candida, cryptococcus neoformans, aspergillus, mucor Mechanism: binds to fungal membrane ergosterol and alters selective permeability Route: intrahecal injection Side effects: very toxic, fever, chills, headache, nausea, vomiting, abd pain, anorexia, renal hypokalemia, thrombocytopenia, leukopenia, anemia Contraindications: Resistance: |
|
|
Griseofulvin
|
Class: anti-fungal
Disease: superficial ringworm, microsporum, tricophyton, epidermophyton Mechanism: binds to fungal microtubules; interferes with spindle formation and inhibits cell division Route: oral Side effects: GI, hepatoxicity, rash, leukopenia, aluminuria Contraindications: phenobarbital-decreases levels of GF by interfering with absorption; anticoagulants-GF diminishes activity of coumarins by increasing rate of metabolism; pregnancy; lupus Resistance: via decrease in drug uptake |
|
|
Nystatin
|
Class: anti-fungal
Disease: superficial candida Mechanism: binds to fungal membrane ergosterol and alters selective permeability Route: oral, topical Side effects: Contraindications: Resistance: |
|
|
Flucytosine
|
Class: anti-fungal
Disease: subcutaneous & systemic candida, cryptococcus Mechanism: converted to 5-flurouracil, which inhibits thymidylate synthetase, which inhibits DNA & RNA synthesis; never used alone, use with Amphotericin B for synergism Route: oral Side effects: epigastric distress, hematology problems, bone marrow depression, Steven-Johnson syndrome Contraindications: Resistance: |
|
|
Ketoconazole
|
Class: anti-fungal
Disease: subcutaneous, systemic and superficial candida vaginitis, cutaneous dermatophyte infection Mechanism: inhibits synthesis of ergosterol; increases permeability of membrane Route: oral Side effects: Contraindications: Resistance: |
|
|
Clotrimazole
|
Class: anti-fungal
Disease: superficial dermatophytic tinea, candida Mechanism: inhibits synthesis of ergosterol; increases permeability of membrane Route: topical Side effects: Contraindications: Resistance: |
|
|
Miconazole
|
Class: anti-fungal
Disease: subcutaneous, systemic and superficial athletes foot Mechanism: inhibits synthesis of ergosterol; increases permeability of membrane Route: topical Side effects: severe GI disturbances Contraindications: Resistance: |
|
|
Tolnaftate
|
Class: anti-fungal
Disease: athletes foot Mechanism: unknown Route: topical Side effects: Contraindications: Resistance: |
|
|
Dapsone
|
Class: anti-mycobacterial
Disease: leprosy Mechanism: inhibition of folate synthesis Route: oral Side effects: hemolysis of RBC, methemoglobinemia, anorexia, nausea, vomiting, allergic dermatitis, fever Contraindications: Resistance: increase, so combination therapy used |
|
|
Clofazimine
|
Class: anti-mycobacterial
Disease: lepromatous leprosy Mechanism: binds DNA, may interfere with DNA replication; alternative to dapsone Route: oral Side effects: skin discoloration, GI intolerance Contraindications: Resistance: |
|
|
Isoniazid
|
Class: anti-mycobacterial
Disease: tuberculosis Mechanism: bacteriostatic against resting bacteria; bacteriocidal against dividing bacteria; effective on intracellular bacteria; pro-drug activated by catalase-peroxidase enzyme; inhibits mycolic acid Route: oral, parental injection Side effects: drug-induced hepatitis, allergic skin eruptions, fever, hepatotoxicity, arthritic symptoms, pyroxidine deficiency - B6 dificiency Contraindications: decreases metabolism of antiepileptic drugs Resistance: decreased penetration into infected cell; mutations leading to overexpression of inhA or ahpC; mutations of KatG |
|
|
Rifampin
|
Class: anti-mycobacterial
Disease: tuberculosis, leprosy Mechanism: inhibits DNA dependent RNA polymerase in prokaryotic cells; effective on intracellular, gram+ and gram- bacteria; good penetration into tissue and macrophages Route: oral Side effects: orange saliva, tears, sweat; fever; GI; skin eruptions; induces hepatic enzymes Contraindications: pts on warfarin, glucocorticoids, narcotic analgesics, or estrogen Resistance: mutations in DNA-dependent RNA polymerase - reduced affinity of drug binding |
|
|
Ethambutal
|
Class: anti-mycobacterial
Disease: tuberculosis Mechanism: inhibits synthesis of arabinogalactin (cell wall component) Route: oral Side effects: optic neuritis, GI, malaise, fever Contraindications: Resistance: resistance occurs rapidly if given alone, mutations leading to overexpression of emb gene |
|
|
Pyrazinamide
|
Class: anti-mycobacterial
Disease: tuberculosis Mechanism: active at acid pH only, effective against intracellular bacteria in macrophages Route: oral, injections Side effects: hepatotoxicity, nausea, vomiting, fever, hyperuricemia Contraindications: Resistance: rapidly developed |
|
|
Streptomycin
|
Class: anti-mycobacterial
Disease: tuberculosis Mechanism: irreversibly binds to 30S ribosome; extracellular bacteria only; used for life threatening TB+meningitis Route: IV Side effects: vertigo, hearing loss, 8th nerve toxicity Contraindications: Resistance: enzymatic deactivation of aminoglycoside; change in permeability; mutation of 30S ribosome |
|
|
Doxycycline
|
Class: anti-protozoal
Disease: malaria prophylax in Chloroquine-resistant areas Mechanism: inhibits protein synthesis Route: Side effects: photosensitivity, GI, vaginitis Contraindications: not to be taken with antacids or iron Resistance: |
|
|
Chloroquine
|
Class: anti-protozoal
Disease: malaria; prophylax travel to N. Africa, Carribean, temperate S America, most of Central America, part of Middle East; treatment of erythrocytic stage Mechanism: inhibits parasite hydrolysis of hemoglobin, leading to accumulation of toxic heme by-products and lysis of cell membrane; binds to DNA; fragments parasite RNA Route: Side effects: GI, visual disturbances, headache, CV changes, ototoxicity, renal impairment, skin eruptions Contraindications: Resistance: caused by increase efflux; decreased uptake; increased metabolism |
|
|
Mefloquine
|
Class: anti-protozoal
Disease: malaria; DOC for treatment of Chlorquine-resistant strains; Mechanism: similar to chlorquine Route: Side effects: GI, dysphoria, dizziness, CNS signs, visual and auditory disturbance Contraindications: hx of epilepsy or psychiatric dx, hypersenstivity, pregnancy Resistance: |
|
|
Atrovaquone and proguanil
|
Class: anti-protozoal
Disease: malaria; active against erythrocytic AND exoerythrocytic stages Mechanism: Atovaquone-inhibits parasite mitochondrial transport; Progunil - metabolizes to a dihydrofolate reductase inhibitor, which disrupts deoxythymidylate synthesis Route: Side effects: headache, GI, mouth ulcers Contraindications: Resistance: |
|
|
Primaquine
|
Class: anti-protozoan
Disease: malaria; prevent relapse, tx of hepatic stages Mechanism: generation of active oxidations products Route: Side effects: Contraindications: G6PD deficient pts - causes hemolytic anemia Resistance: |
|
|
Pyrimethamine
|
Class: anti-protozoan
Disease: malaria; treatment of erythrocytic stage Mechanism: inhibit folate pathway-inhibition of DNA synthesis Route: Side effects: skin rash, megaloblastic anemia, severe-fatal cutaneous rxn Contraindications: Resistance: |
|
|
Pyrimethamine-Sufadoxine (Fansidar)
|
Class: anti-protozoan
Disease: malaria; treatment of erythrocyctic stage Mechanism: 2 drugs inhibit different steps in folate pathway - synergistic inhibition of DNA synthesis Route: Side effects: skin rash, megaloblastic anemia, severe-fatal cutaneous rxn Contraindications: Resistance: wide-spread resistance due to overuse |
|
|
Quinine
|
Class: anti-protozoan
Disease: malaria; used only for Chloroquine-resistant and multidrug resistant P. falciparum Mechanism: similar to Chloroquine, but more toxic and less effective Route: Side effects: "cinchonism," disturbed vision, dysrrhythmias hypotension, hypoglycemia Contraindications: hypersensitivity Resistance: |
|
|
Melarsopol
|
Class: anti-protozoan
Disease: african trypanosomiasis w/ CNS involvement Mechanism: arsenic compound; binds to sulfhydryl groups on proteins, inactivating enzymes Route: Side effects: very toxic; local rxn; fever, encephalopathy, HTN, myocardial damage; vomiting; abd colic Contraindications: Resistance: |
|
|
Pentamindine isethionate
|
Class: anti-protozoal
Disease: african trypanosomiasis w/o CNS involvement; 2nd line for Leishmania, P. carinii Mechanism: inhibition of adenosine uptake; DNA binding and topoisomerase inhibition Route: IM or IV Side effects: too many to list Contraindications: Resistance: |
|
|
Suramin
|
Class: anti-protozaon
Disease: African Trypanosomiasis w/o CNS involvement Mechanism: inhibits parasite energy production Route: Side Effect: nausea, vomiting, shock, loss of consciousness, optic atrophy, adrenal insufficiency, skin rash, hemolytic anemia Contraindications: Resistance: |
|
|
Nifurtimox
|
Class: anti-protozoan
Disease: acute T. cruzi infections Mechanism: coverted to free radicals Route: Side Effect: GI, weight loss, peripheral neuropathy, CNS excitability, suppression of cell-mediated immune rxn Contraindications: Resistance: |
|
|
Benznidazole
|
Class: anti-protozoan
Disease: 2nd line for T. cruzi Mechanism: free radical formation, like metronidazole Route: Side Effect: similar to metronidazole Contraindications: Resistance: |
|
|
Diloxanide furoate
|
Class: anti-protozoan
Disease: amebiasis Mechanism: luminal amebicide - active only against intestinal form of amoeba Route: Side Effect: well tolerated Contraindications: pregnancy Resistance: |
|
|
Metronidazole
|
Class: anti-protozoan
Disease: amebiasis, Trichomonas vaginalis, E. histolytica, Girardia Mechanism: mixed amebicide - active against amebas in both GI lumen and systemic tissues; selective toxicity for anaerobic and microaerophilic microoranisms; accepts electrons from flavoproteins, creating free radicals Side Effects: headache, nausea, dry mouth, metallic tast, disulfirum-like rxn (interferes with ethanol metabolism), CNS and peripheral effects Contraindications: concomitant CNS disease, safe at therapeutic doses in pregnancy Resistance: |
|
|
Paromomycin
|
Class: anti-protozoan
Disease: amebiasis Mechanism: luminal amebicide; an aminoglycoside; binds 30S ribosome & inhibits protein synthesis Route: Side Effect: GI, diarrhea Contraindications: Resistance: |
|
|
Iodoquinol
|
Class: anti-protozoan
Disease: Amebiasis Mechanism: Route: Side Effect: Contraindications: Resistance: |
|
|
Quinacrine
|
Class: anti-protozoan
Disease: giardia Mechanism: intercarlates into DNA; flavoenzyme inhibitions Route: Side Effect: headache, dizziness, vomiting, yellow skin, black and blue nails, toxic psychosis at high doses Contraindications: exacerbates psoriasis Resistance:` |
|
|
Nebupent
|
Class: anti-protozoan
Disease: Mechanism: areosol form of pentamidine isethionate Route: Side Effect: Contraindications: Resistance: |
|
|
Pyrimethamine-sulfadoxine
|
Class: anti-protozoan
Disease: toxoplasmosis Mechanism: Route: Side Effect: Contraindications: Resistance: |
|
|
Trimethoprim-sulfamethoxazole
|
Class: anti-protozoan
Disease: P. carinii Mechanism: Route: Side Effect: Contraindications: Resistance: |
|
|
Mebendazole
|
Class: anti-helminth
Disease: roundworms (nematodes); Ascaris, intestinal capillariasis, enterobiasis, Trichuria, Hookworms Mechanism: bind selectively to worm beta-tubulin and inhibit microtubule polymerization; uncouple oxidative phosphorylations Route:oral Side Effect: Contraindications: Resistance: |
|
|
Albendazole
|
Class: anti-helminthic
Disease: roundworms (nematodes); Ascaris, Trichuria, hookworms Mechanism: binds selectively to worm beta-tubulin and inhibit polyerization; uncouple oxidative phosphylations Route: Side Effect: Contraindications: pregnancy Resistance: |
|
|
Pyrantel
Pamoate |
Class: anti-helminth
Disease: roundworms (nematodes); Ascaris, Enteribiasis, Ancylostoma, N. Americanus, Trichostongulus Mechanism: selectively active against GI parasites; activates nicotinic receptors and inhibits cholinesterase; depolarizing neuromuscular blocker-parasite spasm and paralysis Route: oral Side Effect: GI, headach, fever, rash, dizziness Contraindications: Resistance: |
|
|
Piperazine
|
Class: anti-helminth
Disease: roundworm (nematodes); 2nd line for roundworms and pinworms Mechanism: paralysis of parasite skeletal muscle; parasite expelled alive Route: Side Effect: lethal at high doses Contraindications: Resistance: |
|
|
Ivermectin
|
Class: anti-helminth
Disease: roundworms (nematode); Onchoceriasis, Nematodes Mechanism: induces tonic paralysis of musculature; activates invertebrate GABA or glutamate-gates Cl channels Route: Side Effect: fever, headache, rash, muscle and joint pain Contraindications: children <5, pregnancy, meningitis pts Resistance: |
|
|
Niclosamide
|
Class: anti-helminth
Disease: Flatworm (cestodes); tapeworms Mechanism: inhibition of oxidative phosphorylations; stimulation of ATPase; leads to depletion of ATP Route: Side Effect: mild Contraindications: Resistance: |
|
|
Praziquantel
|
Class: anti-helminth
Disease: flukes (trematodes); schistosomiasis, liver flukes, other cestodes and fluke Mechanism: causes increased muscular activity by contraction & spastic paralysis by increasing calcium permeability; high doses cause tegumental damage which activates host immune system Route: Side Effect: GI, headache, muscle and joint pain Contraindications: children <4, pregnancy, ocular cysticercosis Resistance:` |
