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Anti-microbials
1. MoA 2. Use 3. Side Effects, 4. Interactions
64
Pharmacology
Professional
04/14/2012

Additional Pharmacology Flashcards

 


 

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Term
acyclovir
Definition
1. guanosine analog viral DNA Pol inhibitor; must be activated by viral TK
2. HSV, VZV, EBV
3. nephrotoxic
Term
ganciclovir
Definition
1. guanosine analog viral DNA pol inhibitor
2. CMV
3. neutropenia, thrombocytopenia, leukopenia (all esp if with AZT), renal toxic; potential mutagen/carcinogen
Term
foscarnet
Definition
1. PPi analog vial DNA pol inhibitor - does NOT need activating!
2. CMV retinitis if gancyclovir fails
3. Metabolic disturbances esp HypoCalcemia (=CNS stuff), nephrotoxic
Term
amantadine
Definition
1. blocks M2 pore, inhibits viral uncoating
2. just Influenza A tx and prophylaxis, Parkinsons (bc also Incr dopamine)
3. CNS effects, >90% resistant now
Term
oseltamivir
Definition
1. blocks neuraminidase & viral release
2. Influenza A and B within 48hrs
3. kidney elimination; FDA says possible behvioural/suicide problems
Term
ribavirin
Definition
1. competative inhibitor of IMPDH, which decreases synthesis of guanosine nucleotides
2. RSV, chronic Hep C
3. Teratogen! hemolytic anemia (it concentrates in RBCs)
Term
zidovudine
Definition
1. (aka AZT) NRTI-nucleoside COMPETATIVE reverse transcriptase inhibitor but must be activated by TK; lipophilic=can cross BBB
2. HIV; during and prophylaxis of pregnancy HIV
3. granulocytopenia, lactic acidosis, hepatotoxic
4. lots!
Term
nevirapine
Definition
1. NNRTI - non nucleoside analog; NONcompetative of HIV-RT inhibitor & does NOT need activating
2. HIV
3. rash, bone marrow supression
Term
indinavir
Definition
1. Viral protease inhibitor
2. HIV
3. HYPERGLYCEMIA, nephrolithiasis, thrombocytopenia, buffalo hump, GI
4. "f" impaired with high fat meal; metabolized by CYP3A4
Term
penicillin G
Definition
1. original Lactam; bind PBPs & inhibit cell wall synthesis - bacteriocidal; some GABA Antagonism effect
2. syphilis, anthrax; Gram+ like S. pneumo and pyogenes, and Gram- N. meningitidis
3. (All Lactams=) Allergy, GI, nephrotoxic potential, colitis super infection
Term
amoxicillin
Definition
1. amino penecillin; better oral availability than amp.
2. more Gram- spectrum; empiric sepsis & meningitis (ecoli, h. influenza, salmonella, listeria)
3. Rash
Term
ampicillin
Definition
1. amino penecillin;
2. more Gram- spectrum; empiric sepsis & meningitis (ecoli, h. influenza, salmonella, listeria)
3. Rash
Term
nafcillin
Definition
1. beta lactamase-resistant Lactam
2. MSSA
3. metabolized in LIVER/BILE, not kidney
Term
piperacillin
Definition
1. binds PBPs to inhibit cell wall synthesis
2.Anti-pseudomonal
3. inhibit platelet aggregation in the very ill
Term
imipenem/cilastatin
Definition
1. beta lactamase-resistant Lactams
2. BROAD spectrum
3. dizziness/headache, superinfection colitis
Term
cefazolin
Definition
1. 1st generation cephalosporin Lactam; binds PBPs
2. proteus, Ecoli, Klebsiella
3. toxic to renal tubules, Vit K deficiency = bleeding problems
4. disulfiram-like rxn with ETOH
Term
cefotaxime
Definition
1. 3rd generation cephalosporin Lactam; binds PBPs
2. serious gram neg infections
3. toxic to renal tubules, Vit K deficiency = bleeding problems
4. disulfiram-like rxn with ETOH
Term
ceftriaxone
Definition
1. 3rd generation cephalosporin Lactam; binds PBPs
2.meningitis, gonorrhea; can get to CNS
3. biliary sludging! toxic to renal tubules, Vit K deficiency = bleeding problems
4. disulfiram-like rxn with ETOH
Term
ceftazidime
Definition
1. 3rd generation cephalosporin Lactam; binds PBPs
2. pseudomonas; can get to CNS
3. toxic to renal tubules, Vit K deficiency = bleeding problems
4. disulfiram-like rxn with ETOH
Term
aztreonam
Definition
1. Monobactam
2. Gram Neg Rods ONLY! in Penecillin hypersensitivity pts bc won't form hapten
Term
amoxicillin/clavulanic acid
Definition
Augmentin - includes beta-lactamase inhibitor
Term
piperacillin/tazobactam
Definition
Zosyn - includes beta-lactamase inhibitor
Term
ciprofloxacin
Definition
1. 2nd Gen FluoroQuinolone; inhibit DNA gyrase(Topo 2) in Gram-, Topo 4 in Gram+; BacterioCIDAL
2. Pseudomonas, Gram Neg Rods, UTIs & PNA, anthrax
3. CYP Inhibitor; CONTRA to pregnancy and kids(cartilage damage)
4. Don't give with Antacids; Metals Chelate this
Term
levofloxacin
Definition
1. 3rd Gen FluoroQuinolone; inhibit DNA gyrase(Topo 2) in Gram-, Topo 4 in Gram+; BacterioCIDAL
2. Pseudomonas, Gram Neg Rods, UTIs & PNA
3. CYP Inhibitor; CONTRA to pregnancy and kids(cartilage damage)
4. Don't give with Antacids; Metals Chelate this
Term
sulfamethoxazole
Definition
1. reversibly inhibit dihydropteroate synthase (DHPS) = block formation of DHF
2. UTIs, Toxoplasm, Nocardia; combo tx TMP-SMX
3. CONTRA to preg/infants bc bili-displacement; hemolysis and more risk of allergy in G6PD deficiency; precipitates in Urine
Term
TMP/SMX
Definition
1. together become bacterioCIDAL; TMP inhibits bacterial DHFR
2. Opportunisitic AIDS infections like PCP!; recurrent UTIs, septicemia, GI infections, chronic bronchitis, bLactam-resistant ear infection
3. offset toxicity with leucovorin; sulfonomide rxns + bone marrow supression of antifolates
Term
azithromycin (-thro)
Definition
1. inhibit mRNA translocation on 50S - bacteriostatic;
2. Atypical pneumonias & Gram+; Legionella
3. HEPATIC Toxcity! Prolonged QT, GI (stim motilin receptors); Resistance via methylating 23SrRNA target
4. Dont Take with any Food!
Term
clarithromycin (-thro)
Definition
1. inhibit mRNA translocation on 50S - bacteriostatic
2. Atypical pneumonias & Gram+, Legionella
3. HEPATIC Toxcity! Prolonged QT, LESS GI (stim motilin receptors); Resistance via methylating 23SrRNA target
4. Dont Take with any Food!
Term
erythromycin (-thro)
Definition
1. inhibit mRNA translocation on 50S - bacteriostatic
2. Atypical pneumonias & Gram+, Legionella
3. HEPATIC Toxcity! Prolonged QT, GI (stim motilin receptors); Resistance via methylating 23SrRNA target
4. Dont Take with any Food!
Term
doxycycline
Definition
1. a very Lipid Soluble tetracycline, bacteriostatic; binds 30S A-site =prevents tRNA from binding; must be pumped IN cell
2. borrelia, Hpylori, intracellulars-Rickettsia, Chlamydia - And Protozoa!
3. photosensitivity; caution to preg/kids/Liver probs, discolors teeth, impairs bone growth
4. antacids (chelates!)
Term
chloramphenicol
Definition
1. binds 50S and blocks peptidyltransferase; bacteriostatic
2. Brain Abscess, sepsis & meningitis
3. dose-dependent anemia, dose-independent aplastic anemia, Gray Baby syndrome (affects host mitochond.); CONTRA to preg.
4. anatag to Erythro & Clindamycin (similar site of action)
Term
clindamycin
Definition
1. bacteriostatic; binds 50S and blocks translocation
2. ANAEROBICs ex- bacteroides, clostridium in lung (but doesn't go to CNS)
3. big one for Pseudomembranous Colitis!
Term
gentamicin
Definition
1. aminoglycoside; inhibits initiation complex at 30S; only PRO-synth-inhib to be bacterioCIDAL; Needs O2 to get thru porin!
2. gram neg rods - aerobic; TB, Psuedomon, gonorrhea; synergy in Vivo with bLactams
3. ototoxic, nephrotoxic, TERATOGEN; high dose NMJ Blockade!
4. Loop diuretics Incr ototoxicity
Term
streptomycin
Definition
1. aminoglycoside; inhibits initiation complex at 30S; only PRO-synth-inhib to be bacterioCIDAL; Needs O2 to get thru porin!
2. gram neg rods - aerobic; TB, Psuedomon, gonorrhea; synergy in Vivo with bLactams
3. ototoxic, nephrotoxic, TERATOGEN; high dose NMJ Blockade!
4. Loop diuretics Incr ototoxicity
Term
neomycin
Definition
1. aminoglycoside; inhibits initiation complex at 30S; only PRO-synth-inhib to be bacterioCIDAL; Needs O2 to get thru porin!
2. gram neg rods - aerobic; TB, Psuedomon, gonorrhea; synergy in Vivo with bLactams
3. ototoxic, nephrotoxic, TERATOGEN; high dose NMJ Blockade!
4. Loop diuretics Incr ototoxicity
Term
tobramycin
Definition
1. aminoglycoside; inhibits initiation complex at 30S; only PRO-synth-inhib to be bacterioCIDAL; Needs O2 to get thru porin!
2. gram neg rods - aerobic; TB, Psuedomon, gonorrhea; synergy in Vivo with bLactams
3. ototoxic, nephrotoxic, TERATOGEN; high dose NMJ Blockade!
4. Loop diuretics Incr ototoxicity
Term
dapsone
Definition
1. antifolate, inhibits DHPS
2. m. leprae
Term
isoniazid
Definition
1. inhibit mycolic acid of TB cell wall; needs catalase-peroxidase to get active metabolite
2. prophylaxis or combo tx of TB
3. G6PD hemolysis, INH = Injures Neurons & Hepatocytes; can induce B6 Deficiency = neurotoxicity; have slow and rapid acetylators
Term
metronidazole
Definition
1. Undergoes reductive metabolism by bug to produce free radicals; gets in to CNS
2. Anaerobes; Pseudomebranous Colitis! Helicobacter, bacteroides, Anaerobic Protozoa: Giardia, Entaboeba, Trichomonas
3 - Safe to give to Kids!
4. Disuliram effect with ETOH; metallic taste
Term
polymyxin B & E
Definition
1. detergent-like, cyclic peptide+hydrophobic tail = disrupt cellular membranes; CIDAL
2. GramNeg drug-resistant bugs; B-topical eye and ear, E- last resort for ear, pseudo, acinetobacter
3. Highly neuro and nephrotoxic with oral forms
Term
rifampin
Definition
1. inhibits DNA-dependent RNA pol to block transcription
2. leprosy, TB; meningococcal & H.Influenza prophylaxis, ETEC, M.Avium
3. orange body fluids; CYP450 inducer
Term
vancomycin
Definition
1. Non-Lactam that inhibits cell wall synthesis by binding D-Ala D-Ala of petidoglycan precursors
2. Gram POS only; MRSA& MRSE, enterococci, 2nd line tx C. diff, penecillin-resistant s.pneumo
3. Red Man Syndrome from histamine, ototoxic, nephrotoxic
Resistance - Change target to D-Lactate via VanA plasmid genes
Term
caspofungin
Definition
1. inhibits synthesis of b-Glucans needed for fungal cell walls
2. invasive aspergillosis and cadidiasis
3. hepatic elimination
Term
amphotericin B
Definition
1. binds ergosterol in fungal cell walls and forms pores
2. DOC for crypto-meningitis; serious mycoses, protozoa; LONG 1/2 life!
3. infusion rxns, NEPHROtoxic
Term
terbinafine
Definition
1. inhibit fungal squalene epoxidase
2. dermatophytoses, esp onychomycosis
3. CONTRA to preg.
4. Take with Non-Acidic Foods
Term
fluconazole
Definition
1. inhibit 14a demethylase, final step in making erogosterol; only azole to cross BBB
2. cryptococcus meningitis, candida; NOT aspergillus
3. inhibits CYP450's (incld hydroxylases of adrenals) = gynocomastia, liver dysfx
Term
itraconazole
Definition
1. inhibit 14a demethylase, final step in making erogosterol
2. Broad Spectrum; aspergilosis...
3. CONTRA to CHF pts; inhibits CYP450's (incld hydroxylases of adrenals) = gynocomastia, liver dysfx
Term
flucytosine
Definition
1. cytosine analog pro-drug; fungal deaminase converts to 5-FU; inhibits DNA (via TS-block) and RNA (via incorporation) synthesis, but pump needed to take up drug
2. with AmphoB for cryptococcus meningitisl systemic mycoses
3. anticancer-like side effects: bone marrow supression
Term
griseofulvin
Definition
1. binds and interferes with MicroTubules to inhibit mitosis
2. oral tx for dermatophytes - distributes to keratin areas, "ringworm"
3. Teratogenic, carcinogenic, CYP450 inducer
Term
pentamidine
Definition
1. unknown
2. alternative for PCP; leishmaniasis, African trypanosomiasis hemolyphatic stage
3. Monitor all labs! nephrotoxic, cardiotoxic, hypoglycemia (inhalation less toxic)
Term
chloroquine
Definition
1. binds heme being eaten by parasite, block heme polymerase = toxic Hb metabolites accum. & bug dies in own waste
2. Malaria prophylaxis & tx if not resistant
3. CONTRA to epilepsy, myasthenia, psoriasis, or G6PD deficiency
4. Resistance widespread in S. America, Africa...
Term
quinine/quinine gluconate
Definition
1. (also an antiarrhythmic) inhibit heme polymerase
2. Used in combo with Doxycyclin for chloroquine-resistant and SEVERE malaria ( vivax or falciparum have this potential resistance)
3. CONTRA to Optic neuritis or tinnitus, epilepsy, myasthenia, or G6PD deficiency; "cinchonism" aka anti muscarinic and alpha receptors
Term
atovaquone & proguanil combo
Definition
1. parasite Cyt-bc1 inhibitor = block bug's respiration! & enhance mitoch. collapse + DHFR-i
2. p. falciparum; also Toxo and Pneumocystis
3. contra to renal dysfx
Term
primaquine
Definition
1.
2. only one to work on LIVER maleria hypnozites (relapsing malaria pts - ovale and vivax)
3. Quinine effects; Hemolysis in G6PD defeciency
Term
sulfadiazine + pyrimethamine
Definition
1. pyri inhibits plasmodial DHFR (Sulf = DHPS-i)
2. DOC in toxoplasmosis! p. falciparum
3. sulfa = allergy, pyri = BM supression; supplement with leucovorin to help
Substitute with Clindamycin if allergic = inhibits their apicoplast!
Term
sodium stibogluconate
Definition
1. interfere with trypanothione antioxidant system
2. leishmaniasis
(alt choice - Ampho B)
Term
nifurtimox
Definition
1. forms intracellular free radicals
2. Chagas Disease (t. cruzi of S.America; in combo to work on African sleeping sickness (t. brucei)
Term
suramin
Definition
1. inhibits enzymes involved in energy metabolism; NO CNS involvement
2. African Sleeping Sickness (t. brucei) in hemolyphatic stage
Term
melarsoprol
Definition
1. "Arsenic in Antifreeze" - Inhibits sulfhydryl groups in parasite enzymes; HAS CNS involvement
2. CHRONIC stage of t. brucei
3. KILLS 10% aka a last resort drug
Term
mebendazole
Definition
1. inhibits glucose uptake and Microtubule synthesis; poorly absorbed = gets to GI worms
2. Nematodes/Roundwords; DOC in pinworms
Term
pyrantel pamoate
Definition
1. nicotinic receptor agonist at NMJ = depolarizing blockade
2. Anti-Helminth: ASCARIS, hookworm, pinworm
[NOT for tapeworms of flukes]
Term
ivermectin
Definition
1. induces worm paralysis via Glutamate-gated Cl-channel of larva; also effects GABA receptors
2. nematodes esp filariae causing river blindness
3. Don't give if HOST BBB is compromised, could get anti GABA effects
Term
praziquantel
Definition
1. increase membrane permeability to Ca++ = spastic paralysis & tegument damage
2. tapeworms & flatworms/flukes
3. CONTRA to ocular cysticercosis (larvae in eye)
Term
enfuvirtide
Definition
1. binds viral gp41 & blocks fusion with CD4 cell
2. HIV
3. incr risk of bacterial PNA
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