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77 Cards in this Set
- Front
- Back
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Erythromycin, Clindamycin,
Sulfamethoxazole, Trimethoprim, Tetracyclines, Chlorampenicol |
bacteriostatic
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Vancomycin, Fluoroquinolones, Penicillin, Aminoglycosides, Cephalosporins, Metronidazole
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bactericidal
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MOA of penicillin?
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1. bind penicillin-binding proteins
2. block transpeptidase cross-linking of cell wall 3. activate autolytic enzymes |
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often added to penicillin antibiotics to protect the antibiotic from destruction by beta-lactamase (penicillinase)
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beta-lactamase inhibitors
clavulanic acid, sulbactam, tazobactam |
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antipseudomonals?
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ticarcillin, carbenicillin, piperacillin
(+ clavulanic acid) |
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beta-lactam drugs that inhibit cell wall synthesis but are less susceptible to penicillinases. bactericidal
adverse effects? nephrotoxicity with what? disulfiram-like reaction with what? |
cephalosporins
SE: hypersensitivity reactions, vitamin K def nephrotoxicity w/ aminoglycosides disulfiram-like reaction with ethanol |
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used to treat meningitis, Lyme disease, gonorrhea
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ceftriaxone
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cephalosporin used to treat pseudomonas
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cetazidime
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a monobactam resistant to beta-lactamases.
inhibits cell wall (binds to PBP3) Synergistic with aminoglycosides. No cross-allergenicity with penicillins. |
Aztreonam
gram-negative rods only |
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always administered with cilastatin (inhibitor of renal dihydropeptidase I) to decrease inactivation of drug in renal tubules
SEs? |
Imipenem/cilastatin, Meropenem
SE: GI distress, skin rash, seizures |
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inhibits cell wall mucopeptide formation by binding D-ala D-ala portion of cell wall precursors. Bactericidal.
gram positive only SEs? |
Vancomycin
SE: Nephrotoxicity, ototoxicity, thrombophlebitis, diffuse flushing "red man syndrome" resistance possible with AA change of D-ala D-ala |
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what is the protocol for preventing extensive flushing seen with Vancomycin?
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pretreatment with antihistamines and slow infusion rate
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30S inhibitors
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aminoglycosides
tetracyclines |
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50S inhibitors
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chloramphenicol, clindamycin
erythromycin lincomycin linezolid |
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bactericidal.
inhibit formation of initiation complex and cause misreading of mRNA require O2 for uptake, thus ineffective against anaerobes gram-negative rods SEs? |
AMINOGLYCOSIDES
Gentamicin, Neomycin (bowel surgery) Amikacin, Tobramycin Streptomycin SEs: Nephrotoxicity (+cephalosporins) Ototoxicity (loop diuretics) Teratogen |
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bacteriostatic
bind to 30S and prevent attachment of aminoacyl-tRNA limited CNS penetration Must NOT take with milk, antacids, or iron-containing preps b/c divalent cations inhibit its absorption in the gut SEs? |
TETRACYCLINES
Tetracycline, doxycycline, demeoclocycline, minocycline used for Borrelia, H. pylori, M. pneum, Rickettsia, Chlamydia SEs: discoloration of teeth; inhibition of bone growth, photosensitivity, not during pregnancy |
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tetracycline that acts as a diuretic in SIADH
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Demeclocycline
ADH antagonist |
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inhibit protein synthesis by blocking translocation; bind to the 23S rRNA of the 50S ribosomal subunit. bacteriostatic
Atypical pneumonias SEs? |
MACROLIDES
Erythromycin, azithromycin, clarithromycin SEs: prolonged QT interval, GI discomfort increases concentration of theophyllines, oral anticoagulants resistance: methylation of 23S rRNA binding site |
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inhibits 50S peptidyltransferase activity.
bacteriostatic. Meningitis SEs? |
Chloramphenicol
SEs: Anemia (dose dependent) Aplastic anemia (dose INdependent) Gray baby syndrome (in premies b/c they lack liver UDP-glycuronyl transferase |
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blocks peptide bond formation at 50S ribosomal subunit. baceriostatic.
Anaerobic infections for aspiration pneumonia or lung abscesses SEs? |
Clindamycin
SE: pseudomembranous colitis (C. difficile overgrowth) treats anaerobes above diaphragm (v. metronidazole for below) |
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PABA antimetabolites inhibit dihydropteroate synthetase. bacteriostatic
SEs? |
SULFONAMIDES
Sulfamethoxazole (SMX), sulfisoxazole, sulfadiazine SEs: hypersensitivity reactions, hemolysis if G6PD deficient, nephrotoxicity (tubulointerstitial nephritis), photosensitivity, kernicterus in infants, displace other drugs from albumin (eg warfarin) |
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inhibit dihydrofolate reductase. bacteriostatic.
used with TMP-SMX to block folate synthesis; recurrent UTIs, Shigella, Salmonella, Pneumocystis jiroveci pneumonia SEs? |
trimethoprim, pyrimethamine
SEs: megaloblastic anemia, leukopenia, granulocytopenia |
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TMP SEs with bone marrow can be alleviated with supplemental ____________ (leucovorin rescue)
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folinic acid
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avoid thiazide diuretics, acetazolamide, furosemide, celecoxib, or probenecid because of?
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sulfa drug allergies
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Inhibit DNA gyrase (topoisomerase II) bactericidal.
must not be taken with antacids SEs? |
FLUOROQUINOLONES
Ciprofloxacin, norfloxacin, ofloxacin, sparfloxacin, moxifloxacin, gatifloxacin, enoxacin, nalidixic acid SEs: tendonitis, tendon ruptures, leg cramps, myalgias, damage to cartilage in pregnant women |
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forms free radical toxic metabolites in the bacterial cell that damage DNA. bactericidal, antiprotozoal.
anaerobic infection below diaphragm used in triple therapy against H. Pylori disulfiram-like reaction with? |
Metronidazole
disulfriam-like reaction with alcohol; headache, metallic taste |
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bind to cell membranes of bacteria and disrupt their osmotic properties.
are cationic, basic proteins that act like detergents. SEs? |
POLYMYXINS
Polymyxin B, colistimethate (polymyxin E) SEs: Neurotoxicity, acute renal tubular necrosis |
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Prophylaxis = isoniazid
Tx = Rifampin, Isoniazid, Pyrazinamide, Ethambutol |
M. tuberculosis
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Prophylaxis = Azithromycin
Tx = Azithromycin, rifampin, ethambutol, stretpomycin |
M. avium--intracellulare
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Prophylaxis = N/A
Tx = Dapsone, rifampin, clofazimine |
M. leprae
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effective in acidic pH of phagolysosomes, where TB engulfed by macrophages
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Pyrazinamide
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decreased carboydrate polymerization of mycobacterium cell wall by blocking arabinosyltransferase
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Ethambutol
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major side effect of this TB drug is red-green color blindness
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Ethambutol
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decreased synthesis of mycolic acids (in cell walls)
baceria catalzase-peroxidase needed to be converted to active form SEs? What supplement can prevent these? |
Isoniazid (INH)
M. TB SEs: neurotoxicity, hepatotoxicity, lupus prevent with B6 |
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TB drug that inhibits DNA-dependent RNA polymerase
delays resistance to dapsone when used for leprosy; meningoprophylaxis and chemoprophylaxis in H. influ |
Rifampin
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increased drug interactions, orange body fluids
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Rifampin
RNA polmerase inhibitor Revs up microsomal P-450 Red/orange body fluids Rapid resistance if used alone |
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Meningococcal infection prophylaxis?
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Rifampin,
minocycline |
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Gonorrhea prophylaxis?
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Ceftriaxone
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Syphilis prophylaxis?
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Benzathine penicillin G
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Hx of recurrent UTIs prophylaxis?
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TMP-SMX
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Pneumocystis jiroveci pneumonia prophylaxis?
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TMP-SMX,
aeorsolized pentamidine |
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Endocarditis with surgical or dental procedures prophylaxis?
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Penicillins
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Mycobacterium avium--intracellulare prophylaxis?
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Azithromycin
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MRSA treatment?
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Vancomycin
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VRE treatment?
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linezolid and streptogramins (quinupristin/dalfopristin)
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binds ergosterol (unique to fungi)
forms membrane pores that allow leakage of electrolytes; does not cross BBB systemic SEs? |
Amphotericin B
nephrotoxicity c/o increased DT permeability (tx w/ hydration) decreased K+ / arrhythmias decreased Mg2+ IV plebitis liposomal amphotericin reduces toxicity |
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tx for oral candidiasis, diaper rash or vaginal candidiasis
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Nystatin
topical form because too toxic for systemic use |
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inhibit fungal sterol (ergosterol) synthesis, by inhibiting the P-450 enzyme that converts lanosterol >> ergosterol
SEs? |
AZOLES
Fluconazole, ketoconazole, clotrimazole, miconazole, itraconazole, voriconazole Crytpococcal meningitis in AIDS (fluconazole) -- crosses BBB SEs: gynecomastia, liver disfunction, fever chills |
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inhibits DNA synthesis by conversion to 5-FU
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Flucytosine
Candida, Cryptococcus SE: N/V/D, BM suppression |
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inhibits cell wall synthesis by inhibiting synthesis of beta-glucan
used for invasive aspergillosis |
Caspofungin
SE: GI upset, flushing |
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inhibits the fungal enzyme squalene epoxidase
treat dematophytoses (especially onychomycosis) |
Terbinafine
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interferes with microtubule function; disrupts mitosis
deposits in keratin-containing tissues (eg nails) inhibit growth of dermatophytes |
Griseofulvin
tinea, ringworm SE: teratogenic, carcinogeic, confusion, headaches, increased P-450 and warfarin metabolism |
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selectively inhibits plasmodial dihydrofolate reductase (best for P. falciparum)
drug of choice for toxoplasmosis when combined with sulfadiazine |
Pyrimethamine
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inhibits enzymes infolved in energy metabolism (antiprotozoan)
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Suramin
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inhibits sulfhydryl groups in parasite enzymes. CNS involvement
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Melarsoprol
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Forms intracellular oxyden radicals (antiprotozoan)
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Nifurtimox
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Inhibits clycolysis at PFK reaction (antiprotozoan)
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Sodium stibogluconate
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blocks plasmodium heme polymerase, leading to accumulation of toxic hemoglobin breakdown products that destroy the organism
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chloroquine
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for chloroquine-resistant species when used in combination with pyrimethamine/sulfonamide
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Quinine
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inhibits glucose uptake and microtubule synthesis (antihelminthic)
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Mebendazole
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stimulates nicotinic receptors at neuromuscular junctions.
contraction occurs, followed by depolarization-induced paralysis. no effect on tapeworms or flukes |
Pyrantel pamoate
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intensifies GABA-mediated neurotransmission >> immobilization.
does not cross BBB |
Ivermectin
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increases membrane permeability to calcium >> contraction and paralysis of tapeworms and flukes
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Praziquantel
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blocks viral penetration/uncoating (M2 protein)
also causes the release of dopamine from intact nerve terminals used in influenza A and Parkinson's disease |
Amantadine
does not cross BBB ataxia, dizziness, slurred speech |
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inhibit influenza neuraminidase, decreasing the release of progeny virus
influenza A and B |
Zanamivir, oseltamivir
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inhibits synthesis of guanine nucleotides by competitively inhibiting IMP dehydrogenase
RSV, chronic hepatitis C |
Ribavirin
SE: hemolytic anemia, teratogen |
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monophosphorylated by HSV/VZV thymidine kinase. Guanosine analog
Triphosphate formed by cellular enzymes Preferentially inhibits viral DNA polymerase by chain termination HSV, VZV, EBV |
Acyclovir
resistance if there's a lack of viral thymidine kinase |
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5'-monophosphate formed by a CMV viral kinase or HSV/VZV thymidine kinase.
Guanosine analog. Triphosphate formed by cellular kinases. Preferentially inhibits viral DNA polymerase CMV SEs? |
Ganciclovir
SEs: Leukopenia, neutropenia, thrombocytopenia, renal toxicity. more toxic to host enzymes than acyclovir |
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Viral DNA polymerase inhibitor that binds to the pyrophosphate-binding site of the enzyme. Does not require activation by viral kinase
CMV retinitis when ganciclovir fails SE? |
Foscarnet (w/ cidofovir)
SE: Nephrotoxicity decreased Ca2+, Mg2+ >> seizures |
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HAART is initiated in AIDS PTs when?
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Highly active antiretroviral therapy
CD4 cell counts < 350 cells/mm^3 or high viral load either 2 NRTIs + 1 protease inhibitors or 2 NRTIs + 1non-NRTI |
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assembly of virions depends on HIV-1 protease (pol gene), which cleaves the polypeptide products of HIV mrNA into their functional parts
SEs? |
PROTEASE INHIBITORS
Saquinavir Ritonavir Indinavir Nelfinavir Amprenavir SE: hyperglycemia, N/D, lipodystrophy, thrombocytpenia (indinavir) |
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competitively inhibit nucleotide binding to reverse transcriptase and terminate the DNA chain (lack a 3'-OH group)
must be phosphorylated by thymidine kinase to be active used for prophylaxis in pregnancy |
NRTIs = nucleoside reverse transcriptase inhibitors
Aidovudine, Didanosine, Zalcitabine, Stavudine SE: BM suppression (reversed with G-CSF and erythropoietin) peripheral neuropaht, lactic acidosis, rash, megaloblastic anemia (ZDV) |
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bind to reverse transcriptase at site different from NRTIs.
do not require phosphorylation to be active or compete with nucleotides |
NNRTIs
Nevirapine Efavirenz Declaviridine SEs same as NRTIs |
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bind viral gp41 subunit; inhibit conformational change required for fusion with CD4 cells, blocking entry and replication
Used in patients with persistent viral replication despite antiretroviral therapy |
FUSION INHIBITORS
Enfuviritide SE: hypersensitivity reactions, reactions at subcutaneous injection site, increased risk of bacterial pneumonia |
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glycoproteins synthesized by virus-infected cells block replication of both RNA and DNA viruses
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Interferons
IFN-a -- chronic hepatitis B and C, Kaposi's IFN-b -- MS IFN-y -- NADPH oxidase deficiency SE: neutropenia |
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pregnant mothers should avoid
sulfonamides... aminoglycosides... fluoroquinolones... erythromycin... metronidazole... |
kernicterus
ototoxicity cartilage damage acute cholestatic hepatitis in mom; clarithromycin--embryotoxic mutagenesis |
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pregnant moms should avoid...
tetracyclines... ribavirin (antiviral)... griseofulvin (antifungal)... chloramphenicol... |
discolored teeth, inhibition of bone growth
teratogenic teratogenic "gray baby" syndrome |
