Antimicrobials Flashcards
bactericidal
Very Finely Proficient At Murder: Vancomycin, Fluoroquinolones, Penicillines, Aminoglycosides, Metronidazole (+ Nitrofurantoin)
bacteriostatic
ECSTTC: Erythromycin, Clindamycin, Sulfamethoxazole, Trimethoprim, Chloramphenicol
renal tubular reabsorption of Penicillin inhibited by
Probenecid
narrow-spectrum penicillins (Staph infections), resistant to inactivation by beta-lactamase
methicillin, nafcillin, oxacillin, cloxaciliin
extended spectrum penicillins; may cause pseudomembranous colitis
ampicillin/amoxicillin
antimicrobial coverage of extended spectrum penicillins
amoxicillin HELPS kill Enterococci (H. inf, E. coli, L. monocytogenes, P. mirabilis, Salmonella spp, Enterococci) + Moraxella
anti-pseudomonal penicillines
Takes Care of Pseudomonas: Ticarcillin, Carbenicillin, Piperacillin (also takes care of Klebsiella and Enterobacter)
penicillin with antiplatelet activities, hence risk for bleeding
Ticarcillin
1st gen cephalosporins microorganisms
Gram +, Proteus mirabilis, E. coli, K. pneumoniae (PEK frist)
mnemonic for 1st gen cephalosporins
FADer, help me FAZ my PHarma
2nd gen cephalosporins microorganisms
HEN PEKS, H. inf, Enterobacter, Neisseria spp., Proteus, E.Coli, Klebsiella, Serratia
mnemonic for 2nd gen cephalosporins
FAMily gathering, FOXy cousin wears a FUR coat drinking TEa. FAC! LORA the PROfessional AZhOLE is still on the FON
cephalosporins exhibiting disulfiram
cefamandole, cefotetan (2nd gen), cefoperazone (3rd gen)
3rd gen cephalosporins microorganisms
Pseudomonas, Bacteroides
mnemonic for 3rd gen cephalosporins
Fenge PO ng PERA to FIX my TTTTTv
anti-pseudomonal cephalosporins
ceftazidime, cefoperazone (3rd gen), cefepime (4th)
inhibits renal metabolism of imipenenm
cilastatin
silver bullet for gram negative (Klebsiella, Pseudomonas, Serratia)
Aztreonam
beta-lactamase inhibitors
clavulanic acid, tazobactam, sulbactam
inhibits cell wall synthesis by binding d-ala-d-ala terminus of nascent peptidoglycan
vancomycin/ teicoplanin
tx for redman syndrome
slow down infusion, antihistamine
interferes with late stage in cell wall synthesis of gram + organisms, reserved for topical use due to nephrotoxicity
bacitracin
blocks incorporation of d-ala in peptidoglycan, used for drug-resistant TB, SE: neurotoxicity
cycloserine
mnemonic for protein synthesis inhibitors
buy AT 30, CELLS at 50 (aminoglycosides, tetracycline, chloramphenicol, erythromycin, lincosamides, linezolid, streptogrammins)
idiosyncratic reaction of chloramphenicol
aplastic anemia
dec RBCs, cyanosis and CV collapse, ashen gray skin due to deficient glucoronosyltransferase and inability to metabolize chloramphenicol
Gray Baby Syndrome
tetracycline used for SIADH
demeclocycline
broadest spectrum tetracycline
tigecycline
tetracyclines must not be drank with
milk (decreased absorption)
blocks attachment of tRNA to acceptor site (A site)
tetracycline
macrolide which does not inhibit CYP450, also has highest Vd and slowest elimination
azithromycin
ketolide used for macrolide resistance
telithromycin
SE of macrolides
cholestatic hepatitis, QT prolongation
anaerobic infections above the diaphragm
clindamycin
anaerobic infections below the diaphragm
metronidazole
endocarditis prophylaxis (penicillin-allergy), PCP pneumonia, toxoplasmosis
lincosamide (clindamycin/lincomycin)
binds at 50S subunit, bactericidal, used for drug resistant gram + infections, SE: arthralgia-myalgia syndrome
streptogrammin(quinupristin-dalfopristin)
binds at 50S subunit, bacteriostatic, used for drug resistant gram + infections, Listeria and Corynebacteria, SE: serotonin syndrome, neuropathy, optic neuritis
linezolid
killing action continues even when plasma levels have declined, seen in aminoglycosides and fluoroquinolones
post-antibiotic effect
narrowest therapeutic window among aminoglycosides, resistant to enzymes that inactivate other aminoglycosides, 2nd line drug for MDR-TB
amikacin
bactericidal inhibitor of protein synthesis; ineffective against anaerobes
aminoglycoside
notable SE of aminoglycosides
reversible nephrotoxicity (ATN), irreversible ototoxicity, neuromuscular blockade
most vestibulotoxic and nephrotoxic aminoglycosides
gentamicin and tobramycin
Tx for Tularemia, Bubonic plague, Brucellosis; can cause congenital deafness
streptomycin
most ototoxic aminoglycoside
kanamycin, amikacin
aminoglycoside used for hepatic encephalopathy
kanamycin
aminoglycoside used for visceral leishmaniasis, also anti-protozoal (luminal amebicide)
paramomycin
aminoglycoside used for drug-resistant gonorrhea
spectinomycin
causes curare-like effect (non depolarizing neuromuscular block) reversible with calcium and neostigmine
aminoglycosides
mnemonic for aminoglycosides
mean GNATS canNOT kill anaerobes (genta, neomycin, amik, tobra, strepto) nephrotoxicity, ototoxicity, teratogen
have a common chemical nucleus resembling p-aminobenzoic acid
sulfonamides
solubility may be decreased in acidic urine; solution
sulfonamides; triple sulfa combination to reduce likelihood of precipitation
structurally similar to folic acid
trimethoprim
components of hepatic enceph tx
lactulose, neomycin, aminoleban
enzyme inhibited by sulfonamides
dihydropteroate synthase (found only in prokaryotes)
enzyme inhibited by trimethoprim
dihydrofolate reductase
TMP-SMX cidal/static?
bacteriostatic individually, cidal combined
similar drug to silver sulfadiazine with better eschar penetration
mafenide acetate
sulfonamides displace protein binding of_____ leading to _____
bilirubin; kernicterus
site of bilirubin deposition in kernicterus
subcortical nuclei, basal ganglia
interfere with topoisomerase II (DNA gyrase) for gram -, and topoisomerase IV for gram +
fluoroquinolones
2nd generation fluoroquinolones; coverage
ciprofloxacin, ofloxacin, norfloxacin; gram negative, gonococci, gram positive and Mycoplasma coverage (atypical pneumonia and 2nd line drug for TB)
notable SE of fluoroquinolones
tendinitis and tendon rupture (fluoroquinoLONES hurt your BONES), enhance toxicity of methylxanthines (theophyllines), avoid in children and pregnant women
macrolides
azithromycin, erythromycin, clarithromycin, telithromycin
3rd generation fluoroquinolones; coverage
levofloxacin, sparfloxacin, grepafloxacin (withdrawn due to cardiotoxicity); less gram -, more gram + (unlike cephalosporins), streptococci and enterococci
4th generation fluoroquinolones; coverage
moxifloxacin, trovafloxacin, gemifloxacin, gatifloxacin; gram +, gram -, anaerobes
fluoroquinolone with SE: DM; hepatotoxicity
gatifloxacin; trovafloxacin
reactive reduction by ferrodoxin forming free radicals that disrupt ETC; DOC for protozoal infections, vaginitis (Trichomonas, Gardnerella); SE: metallic taste, disulfiram
metronidazole/ tinidazole
forms multiple reactive intermediate acted upon by bacterial nitrofuran reductase; used for UTI (except Proteus and Pseudomonas); ok for pregnant pts; can also cause hemolysis in G6PD
nitrofurantoin/ nitrofuran
inhibits mycolic acid synthesis; bactericidal; mnemonic for side effects; coadminister with
isoniazid; affects neurons and hepatocytes; pyridoxine (vit B6)
inhibits DNA dependent RNA polymerase; bactericidal; also used as prophylaxis for meningococcal and staphylococcal carrier states, delays resistance to dapsone (leprosy); mnemonic
rifampicin (rifabutin, rifapentine); R=RNA polymerase inhibitor, red orange body fluids, rapid dev’t of resistance, revs up CYP450
inhibits arabinosyl transferases involved in synthesis of mycobacterial cell wall; bacteriostatic; SE
ethambutol; red green color blindness, retrobulbar neuritis, retinal damage
antimycobacterial with unknown MOA; static but cidal on actively dividing bacteria; SE
pyrazinamide; hyperuricemia, sterilizing agent, most hepatotoxic
hepatotoxicity of anti-TB drugs
PRI the liver! pyrazinamid>rifampicin>isoniazid
alternative antimycobacterial drug with no cross-resistance with INH; SE: severe GI irritation and neurotoxicity
ethionamide
alternative antimycobacterial drug rarely used because primary resistance is common; SE: GI irritation, hypersensitivity, effects on kidney, liver, thyroid
p-aminosalicylic acid (PAS)
alternative antimycobacterial drug; SE: ototoxicity, renal dysfuntion
capreomycin
dapsone, static/cidal; notable SE
bacteriostatic; methemoglobinemia
clofazimine, static/cidal; notable SE
bactericidal; GI irritation, skin discoloration
binds to ergosterol in fungal cell membranes (fungicidal); notable SE
amphotericin B (polyene); infusion reactions (give antihistamines), nephrotoxicity (RTA)
accumulates in fungal cells via permease; inhibits fungal thimidylate synthase, fungistatic
flucytosine
high systemic toxicity so used topically (for dermatophytosis); blocks ergosterol synthesis, fungistatic
ketoconazole
blocks ergosterol synthesis, fungistatic, can be used systemically for candidiasis, coccidiomycosis, cryptococcal meningitis
fluconazole
blocks ergosterol synthesis, fungistatic, can be used systemically for blastomycosis, sporotrichosis
itraconazole
echinocandin which inhibits B-glucan synthase decreasing fungal cell wall synthesis, fungistatic, salvage therapy for invasive aspergillosis
cASPofungin
interferes with microtubule formation, fungistatic, for dermatophytosis because it accumulates in keratin; CI in ____
griseofulvin; porphyria
inhibits squalene oxidase, fungicidal, for dermatophytosis because it accumulates in keratin
terbinafine
binds to ergosterol in fungal cell membranes (fungicidal); notable SE, swish and swallow preparation
nystatin
azole of choice for seborrheic dermatitis, pityriasis versicolor
clotrimazole
activated by viral thymidine kinase to forms that inhibit viral DNA polymerase, anti-herpes
acyclovir
activated by viral thymidine kinase to forms that inhibit viral DNA polymerase, anti-CMV
ganciclovir
inhibits viral DNA polymerase, active against strains with absent thymidine kinase; used for acyclovir and ganciclovir resistance, molluscum contagiosum
cifodovir
inhibits viral DNA polymerase, RNA polymerase and HIV reverse transcriptase, active against strains with absent thymidine kinase
foscarnet (pyroFOSphate analogue)
protease inhibitors mnemonic
NAVIR tease a PROTEASE
NRTI, requires phosphorlyation by cellular enzymes, incorporated in DNA chain; used for reversal of maternal-fetal HIV transmission; SE
zidovudine; BM suupression
inhibits HIV reverse transcriptase, no phosphorylation required; not incorporated in DNA chain; mnemonic
NNRTI (delavirdine, efavirenz, etravirine, nevirapine); never ever deliver, e trapik!
delavirdine, nevirapine SE
rash, increased AST, ALT
efavirenz SE
teratogenicity
etravirine
inc choles, TG, inhibitor and inducer of CYP450, cross-resistance with NNRTIs
protease inhibitor causing hyperbilirubinemia and nephrolithiasis
indinavir
binds to gp41 subunit preventing fusion of viral and cellular membranes, causes increased incidence of bacterial pneumonia; equivalent in HSV
enFUvirtide; doconasol
blocks HIV viral attachment via transmembrane chemokine receptor CCR5
maraviroc
anti-influenza A (prevents uncoating) and rubella, also used to treat Parkinsonism; can cause cerebellar dysfunction, livedo reticularis; mnemonic
Amantadine, Rimantidine; A man to dine takes off his coat; blocks influenza A and rubellA, causes problems with the cerebellA
anti-influenza which inhibits neuraminidase; SE
Oseltamivir (GI effects), Zanamivir (bronchospasm in asthmatics)
general SE for NRTI
lactic acidosis with hepatic steatosis
NRTI with SE: hypersensitivity
abacavir
NRTI with SE: pancreatitis
didanosine
NRTI with SE: peripheral neuropathy
stavudine, zalcitabine
general SE for protease
lipodystrophy, hyperglycemia (never tease)
degrades viral RNA via inactivation of host cell RNAase; used for HBV, HCV, Kaposi sarcoma, genital warts, also for hairy cell leukemia, CML and T cell lymphomas
interferon alpha
inhibits HBV DNA polymerase
lamivudine, entecavir, adefovir, telbivudine, tenofovir
inhibits RNA dependent RNA polymerase, prevents capping of viral mRNA; used for HCV, RSV, viral hemorrhagic fevers (West Nile, Ebola virus)
Ribavirin
prevents polymerization of heme into hemozoin; blood schizonticide, may precipitate porphyria
chloroquine
complexes with DNA to prevent strand separation; blood schizonticide; SE- to prevent, it is commonly used with ____ or ____, DOC for malaria in pregnant
quinine; QUInchonism (cinchonism-headache, tinnitus, vertigo), blackwater fever; doxycycline/clindamycin
anti-malarial with unknown MOA. blood schizonticide used as alternative to quinine, SE: cardiac conduction defects, psychosis
mefloquine
releases cellular oxidants. tissue schizonticide and gametocide; radical cure of P.vivax and ovale, should be used with blood schizontocide, also used for PCP pneumonia
primaquine
blood schizontocide-sporonticide combinations
atovaquone-proguanil (malarone), sulfadoxine-pyrimethamine
impairs progeny of malarial genes, blood schizonticide, used for chemophrophylaxis in multi-drug resistant malaria; SE
doxycycline; tooth enamel dysplacia/discoloration
DOC for uncomplicated falciparum malaria in the Phils, blood schizonticide
artemether-lumefantrine (CoArtem)
malaria chemoprophylaxis: choroquine sensitive
chloroquine 500mg/tab 1 tab weekly; 2-3 days before going, during stay and 4 weeks after
malaria chemoprophylaxis: choroquine resistant
mefloquine 250mg/tab 1 tab weekly or malarone 1 tab daily; 2-3 days before going, during stay and 4 weeks after
malaria chemoprophylaxis: multi-drug resistant
doxycycline 100mg/tab 1 tab daily; 2-3 days before going, during stay and 4 weeks after
2 types of amebicides
tissue (act on bowel wall and liver), and luminal (act on lumen)
DOC for asymptomatic intestinal amebiasis; back-up
diluxonide furoate; iodoquinol, paramomycin
DOC for mild to moderate intestinal amebiasis
metronidazole + luminal amebicide
DOC for severe intestinal amebiasis or hepatic abscess/extraintestinal; back-up drug (back-up only due to CV dysfunction)
metronidazole or tinidazole + luminal amebicide; emetine
luminal amebicide which can cause thyroid enlargement and neurotoxicity
iodoquinol
DOC for cryptosporidiosis, also anti-protozoal
nitazoxanide
DOC for pneumocystosis; back-up
TMP-SMX; pentamidine
DOC for toxoplasmosis
pyrimethamine-sulfadiazine (Fanzidar)
back-up drug for pneumocystosis, also used for hemolymphatic african sleeping sickness and visceral leishmaniasis (kala-azar), does not cross BBB
pentamidine
DOC for advanced West African sleeping sickness, inhibits ornithine decarboxylase, crosses BBB, less toxic than melarsoprol
eflornitihine
DOC for advanced East African sleeping sickness, inhibits enzyme sulfhydryl groups, causes reactive encephalopathy, usually administered with ____
melarsoprol; suramin
DOC for Chagas disease
nifurtimox
DOC for Leishmaniasis (except in India where Ampho B is given)
sodium stibogluconate
DOC for whipworm/ trichuris infections
mebendazole
inhibits microtubule synthesis, ovicidal; CI in pregnancy
mebendazole
inhibits microtubule assembly, larvicidal and ovicidal
albendazole
DOC for hydatid disease (Echinococcus)
albendazole
DOC for filiariasis
diethylcarbamazine
DOC for eye worm disease
diethylcarbamazine
DOC for hookworm and roundworm infections, in Phils, Enterobius vermicularis (pinworm)
pyrantel pamoate
DOC for trichinosis
thiabendazole
DOC for trematodes (Schistosoma, Paragonimus, Clonorchis, Opistorchis) and cestodes (Taenia, Diphyllobotrium) but contraindicated in____, used with ____ in neurocysticercosis
praziquantel; ocular cysticercosis (causes irreparable eye damage); corticosteroids
alternative drug for cestodes (Taenia, Diphyllobotrium), no effects on ova, avoid ethanol consumption
niclosamide