Pharmacology1 Flashcards
Penicillins
- Mechanism of Actions ?
c.w. synthesis inhibition
(stage 3) bactericidal
Prototype
- drugs ?
Penicillin G
Penicillin V [103]
Pharmacokinetics ?
- Penicillin G
- Penicillin V [103]
G: IM/IV (poor oral), renal excretion (almost all)
V: good oral, acid stable, renal excretion (almost all)
Penicillins
- Pharmacokinetics ?
renal excretion (almost all)
Penicillins
- Adverse Reactions?
anaphylaxis (Type I, rare) Prototype convulsions (very high doses)
Penicillinase-resistant
-drug?
Dicloxacillin,
Dicloxacillin
- Pharmacokinetics ?
good oral (not methicillin or nafcillin) NOTE: All other PCN classes are penicillinase (β-lactamase) susceptible; unless combined w/β-lactamase inhibitor (amoxicillin-clavulanate [34] or piperacillin/tazobactam)
Extended Spectrum
- drugs ?
(Amoxicillin [4], Ampicillin)
(Amoxicillin [4], Ampicillin)
- Pharmacokinetics ?
good oral
(Amoxicillin [4], Ampicillin)
- Adverse Reactions?
diarrhea (less with amoxicillin)
superinfection (CDAD) possible
Antipseudomonal
- drugs?
Piperacillin
Piperacillin
- Pharmacokinetics ?
IV only
Cephalosporins
- Mechanism of Actions ?
c.w. synthesis inhibition
(stage 3) bactericidal
Cephalosporins
- - Pharmacokinetics ?
renal excretion (almost all)
Cephalosporins
- Adverse Reactions?
allergy, less severe than penicillins
(some cross sensitivity - ∼ 1-5%)
Cephalosporins - 1st Generation
- drug?
Cephalexin [23]
(Cefazolin)
Cephalosporins - 2nd Generation
- drug?
Cefaclor,
Cephalosporins - 3rd Generation
- drug?
Ceftriaxone, Ceftazidine
Cephalexin
- Pharmacokinetics ?
good oral
(Cefazolin)
- Pharmacokinetics ?
IV/IM only
Cephalexin, Cefazolin
- Adverse Reactions?
diarrhea
Cefuroxime
- Pharmacokinetics ?
good oral
Cefuroxime
- Adverse Reactions?
DDI: enhancement of warfarin
anticoagulant activity possible
superinfection (CDAD) possible
Ceftriaxone [IV, IM]) Ceftazidine
- - Pharmacokinetics ?
good CNS penetration
Ceftriaxone [IV, IM]) Ceftazidine
- Adverse Reactions
superinfection (CDAD) possible
Cephalosporins - 4th generation
- drug?
Cefepime
Cefepime
- Adverse Reaction?
superinfection (CDAD) possible
Vancomycin
- Mechanism of Actions ?
c.w. synthesis inhibition
(stage 2) bactericidal
Vancomycin
- Pharmacokinetics ?
poor oral absorption
renal excretion
Vancomycin
- Adverse Reactions?
infusion related: chills / fever / rash
ototoxicity, renal toxicity
routine monitoring of Cp levels
Carbapenems
- Mechanism of actions?
c.w. synthesis inhibition
m (stage 3) bactericidal
Carbapenems
- Pharmacokinetics ?
IV
Carbapenems - Doripenem , Meropenem, Ertapenem imipenem-cilastatin
-Adverse Reactions
nausea/vomiting, diarrhea
seizures possible at highest doses
Doripenem , Meropenem
- - Pharmacokinetics ?
renal excretion
Ertapenem imipenem-cilastatin
- Pharmacokinetics ?
once daily with Ertapenem
Carbapenems
- drugs?
Doripenem , Meropenem
Ertapenem imipenem-cilastatin
Macrolides
- Mechanism of actions?
protein synthesis inhibition (50S)
bacteriostatic
Macrolides
- drugs?
Erythromycin
Azithromycin [7]
Clarithromycin
Macrolides
- Pharmacokinetics ?
good oral (also IV) concentrates in lungs
Macrolides
- Adverse Reaction
GI disturbances (n/v, diarrhea) DD interactions due to inhibition of P450 metabolism (NOT AZI)
Erythromycin
- Pharmacokinetics ?
QID - liver metabolism
Azithromycin [7]
- Pharmacokinetics ?
QD - biliary
Clarithromycin
- Pharmacokinetics ?
BID - metabolism to active
metabolite
Tetracyclines
- Mechanism of action?
protein synthesis inhibition (30S)
bacteriostatic
Tetracyclines
- drugs?
Tetracycline
Doxycycline
Minocycline
Tetracycline
- Pharmacokinetics?
po, renal excretion
Doxycycline
- Pharmacokinetics?
po, biliary (non-renal excretion)
Minocycline
- Pharmacokinetics?
????
Tetracyclines
- Adverse Reactions, DDI
abnormal bone/tooth development
(avoid in pregnancy, < 8y/o)
n/v/diarrhea, fungal superinfection
DD interactions with metal cations (antacids / dairy / iron) in stomach
Clindamycin
- Mechanism of Action
protein synthesis inhibition (50S) g
bacteriostatic
Clindamycin
- Pharmacokinetics
good po (also IV) penetrates into bone hepatobiliary elimination
Clindamycin
- Adverse Reactions?
severe diarrhea
pseudomembranous colitis
Aminoglycoside
- Mechanism of action?
protein synthesis inhibition (30S)
bactericidal
Aminoglycoside
- Pharmacokinetics?
poor oral absorption (IV/IM)
distributed in extracellular fluid
accumulates in kidney / inner ear
renal excretion
Aminoglycoside
- Adverse Reactions?
vestibular and auditory toxicity
nephrotoxicity
routine monitoring of Cp levels
Chloramphenicol
- Mechanism of action?
protein synthesis inhibition (50S)
bacteriostatic
Chloramphenicol
-Pharmacokinetics?
good po (also IV)
distributes to CNS / CSF
metabolized by glucuronidation
Chloramphenicol
- Adverse reaction?
bone marrow toxicity
gray baby syndrome, GI upset
toxicity limits use in US
Fluoroquinolones
- Mechanism of Action?
inhibition of DNA gyrase
bactericidal
Fluoroquinolones
- Adverse Reaction?
well tolerated, some GI upset,
superinfections (CDAD) possible
DDI w/theophylline (↓ metabolism) and antacids (↓ FQ absorption)
Rare: CNS disorders, ↑ QT interval NOT 1st choice in children (potential arthalgias)
Fluoroquinolones
- drugs?
Ciprofloxacin
Levofloxacin
Moxifloxacin
Fluoroquinolones
- Pharmacokinetics?
good oral (also IV)
Mechanism of actions?
- Ciprofloxacin [37]
- Levofloxacin [51]
- Moxifloxacin
[2nd generation]
[3rd generation-respiratory FQ]
[4th generation-respiratory FQ]
Pharmacokinetics?
- Ciprofloxacin [37]
- Levofloxacin [51]
- Moxifloxacin
primarily renal excretion
primarily renal excretion
primarily hepatic (20% renal)
Fluoroquinolones
- adverse reactions?
well tolerated, some GI upset superinfections (CDAD) possible DDI w/theophylline (↓ metabolism) and antacids (↓ FQ absorption) Rare: CNS disorders, ↑ QT interval NOT 1st choice in children (potential arthalgias)
Nitrofurantoin
- Mechanism of Action
reduced in cell to intermediates that damage bacterial DNA bactericida
Nitrofurantoin
- Pharmacokinetics
rapid, complete GI absorption but rapid excretion via kidneys, thus acts as urinary antiseptic
Nitrofurantoin
- Adverse Reactions
GI side effects, macrocrystalline
forms better tolerated
Metronidazole [
- Mechanism of Action
reduced intracellularly to active form; interference with DNA fxn bactericidal
Metronidazole [
- Pharmacokinetics
good oral bioavailability
hepatic metabolism
Metronidazole [
- Adverse Reactions
nausea, headache, GI distress
Antabuse®-like reaction
occasional candidal superinfections