Pharmacology1 Flashcards by A B

Penicillins

- Mechanism of Actions ?

c.w. synthesis inhibition

(stage 3) bactericidal

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Prototype

- drugs ?

Penicillin G

Penicillin V [103]

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Pharmacokinetics ?

Penicillin G
Penicillin V [103]

G: IM/IV (poor oral), renal excretion (almost all)
V: good oral, acid stable, renal excretion (almost all)

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Penicillins

- Pharmacokinetics ?

renal excretion (almost all)

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Penicillins

- Adverse Reactions?

anaphylaxis (Type I, rare)
Prototype convulsions (very high doses)

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Penicillinase-resistant

-drug?

Dicloxacillin,

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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)

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Extended Spectrum

- drugs ?

(Amoxicillin [4], Ampicillin)

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(Amoxicillin [4], Ampicillin)

- Pharmacokinetics ?

good oral

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(Amoxicillin [4], Ampicillin)

- Adverse Reactions?

diarrhea (less with amoxicillin)

superinfection (CDAD) possible

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Antipseudomonal

- drugs?

Piperacillin

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Piperacillin

- Pharmacokinetics ?

IV only

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Cephalosporins

- Mechanism of Actions ?

c.w. synthesis inhibition

(stage 3) bactericidal

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Cephalosporins

- - Pharmacokinetics ?

renal excretion (almost all)

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Cephalosporins

- Adverse Reactions?

allergy, less severe than penicillins

(some cross sensitivity - ∼ 1-5%)

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Cephalosporins - 1st Generation

- drug?

Cephalexin [23]

(Cefazolin)

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Cephalosporins - 2nd Generation

- drug?

Cefaclor,

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Cephalosporins - 3rd Generation

- drug?

Ceftriaxone, Ceftazidine

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Cephalexin

- Pharmacokinetics ?

good oral

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(Cefazolin)

- Pharmacokinetics ?

IV/IM only

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Cephalexin, Cefazolin

- Adverse Reactions?

diarrhea

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Cefuroxime

- Pharmacokinetics ?

good oral

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Cefuroxime

- Adverse Reactions?

DDI: enhancement of warfarin
anticoagulant activity possible
superinfection (CDAD) possible

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Ceftriaxone [IV, IM]) Ceftazidine

- - Pharmacokinetics ?

good CNS penetration

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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 ?

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