Pharmacology1 Flashcards

1
Q

Penicillins

- Mechanism of Actions ?

A

c.w. synthesis inhibition

(stage 3) bactericidal

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2
Q

Prototype

- drugs ?

A

Penicillin G

Penicillin V [103]

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3
Q

Pharmacokinetics ?

  • Penicillin G
  • Penicillin V [103]
A

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

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4
Q

Penicillins

- Pharmacokinetics ?

A

renal excretion (almost all)

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5
Q

Penicillins

- Adverse Reactions?

A
anaphylaxis (Type I, rare)
Prototype convulsions (very high doses)
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6
Q

Penicillinase-resistant

-drug?

A

Dicloxacillin,

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7
Q

Dicloxacillin

- Pharmacokinetics ?

A
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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8
Q

Extended Spectrum

- drugs ?

A

(Amoxicillin [4], Ampicillin)

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9
Q

(Amoxicillin [4], Ampicillin)

- Pharmacokinetics ?

A

good oral

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10
Q

(Amoxicillin [4], Ampicillin)

- Adverse Reactions?

A

diarrhea (less with amoxicillin)

superinfection (CDAD) possible

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11
Q

Antipseudomonal

- drugs?

A

Piperacillin

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12
Q

Piperacillin

- Pharmacokinetics ?

A

IV only

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13
Q

Cephalosporins

- Mechanism of Actions ?

A

c.w. synthesis inhibition

(stage 3) bactericidal

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14
Q

Cephalosporins

- - Pharmacokinetics ?

A

renal excretion (almost all)

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15
Q

Cephalosporins

- Adverse Reactions?

A

allergy, less severe than penicillins

(some cross sensitivity - ∼ 1-5%)

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16
Q

Cephalosporins - 1st Generation

- drug?

A

Cephalexin [23]

(Cefazolin)

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17
Q

Cephalosporins - 2nd Generation

- drug?

A

Cefaclor,

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18
Q

Cephalosporins - 3rd Generation

- drug?

A

Ceftriaxone, Ceftazidine

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19
Q

Cephalexin

- Pharmacokinetics ?

A

good oral

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20
Q

(Cefazolin)

- Pharmacokinetics ?

A

IV/IM only

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21
Q

Cephalexin, Cefazolin

- Adverse Reactions?

A

diarrhea

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22
Q

Cefuroxime

- Pharmacokinetics ?

A

good oral

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23
Q

Cefuroxime

- Adverse Reactions?

A

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

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24
Q

Ceftriaxone [IV, IM]) Ceftazidine

- - Pharmacokinetics ?

A

good CNS penetration

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25
Q

Ceftriaxone [IV, IM]) Ceftazidine

- Adverse Reactions

A

superinfection (CDAD) possible

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26
Q

Cephalosporins - 4th generation

- drug?

A

Cefepime

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27
Q

Cefepime

- Adverse Reaction?

A

superinfection (CDAD) possible

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28
Q

Vancomycin

- Mechanism of Actions ?

A

c.w. synthesis inhibition

(stage 2) bactericidal

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29
Q

Vancomycin

- Pharmacokinetics ?

A

poor oral absorption

renal excretion

30
Q

Vancomycin

- Adverse Reactions?

A

infusion related: chills / fever / rash
ototoxicity, renal toxicity
routine monitoring of Cp levels

31
Q

Carbapenems

- Mechanism of actions?

A

c.w. synthesis inhibition

m (stage 3) bactericidal

32
Q

Carbapenems

- Pharmacokinetics ?

A

IV

33
Q

Carbapenems - Doripenem , Meropenem, Ertapenem imipenem-cilastatin
-Adverse Reactions

A

nausea/vomiting, diarrhea

seizures possible at highest doses

34
Q

Doripenem , Meropenem

- - Pharmacokinetics ?

A

renal excretion

35
Q

Ertapenem imipenem-cilastatin

- Pharmacokinetics ?

A

once daily with Ertapenem

36
Q

Carbapenems

- drugs?

A

Doripenem , Meropenem

Ertapenem imipenem-cilastatin

37
Q

Macrolides

- Mechanism of actions?

A

protein synthesis inhibition (50S)

bacteriostatic

38
Q

Macrolides

- drugs?

A

Erythromycin
Azithromycin [7]
Clarithromycin

39
Q

Macrolides

- Pharmacokinetics ?

A
good oral (also IV)
concentrates in lungs
40
Q

Macrolides

- Adverse Reaction

A
GI disturbances (n/v, diarrhea)
DD interactions due to inhibition of P450 metabolism (NOT AZI)
41
Q

Erythromycin

- Pharmacokinetics ?

A

QID - liver metabolism

42
Q

Azithromycin [7]

- Pharmacokinetics ?

A

QD - biliary

43
Q

Clarithromycin

- Pharmacokinetics ?

A

BID - metabolism to active

metabolite

44
Q

Tetracyclines

- Mechanism of action?

A

protein synthesis inhibition (30S)

bacteriostatic

45
Q

Tetracyclines

- drugs?

A

Tetracycline
Doxycycline
Minocycline

46
Q

Tetracycline

- Pharmacokinetics?

A

po, renal excretion

47
Q

Doxycycline

- Pharmacokinetics?

A

po, biliary (non-renal excretion)

48
Q

Minocycline

- Pharmacokinetics?

A

????

49
Q

Tetracyclines

- Adverse Reactions, DDI

A

abnormal bone/tooth development
(avoid in pregnancy, < 8y/o)
n/v/diarrhea, fungal superinfection

DD interactions with metal cations (antacids / dairy / iron) in stomach

50
Q

Clindamycin

- Mechanism of Action

A

protein synthesis inhibition (50S) g

bacteriostatic

51
Q

Clindamycin

- Pharmacokinetics

A
good po (also IV)
penetrates into bone
hepatobiliary elimination
52
Q

Clindamycin

- Adverse Reactions?

A

severe diarrhea

pseudomembranous colitis

53
Q

Aminoglycoside

- Mechanism of action?

A

protein synthesis inhibition (30S)

bactericidal

54
Q

Aminoglycoside

- Pharmacokinetics?

A

poor oral absorption (IV/IM)
distributed in extracellular fluid
accumulates in kidney / inner ear
renal excretion

55
Q

Aminoglycoside

- Adverse Reactions?

A

vestibular and auditory toxicity
nephrotoxicity
routine monitoring of Cp levels

56
Q

Chloramphenicol

- Mechanism of action?

A

protein synthesis inhibition (50S)

bacteriostatic

57
Q

Chloramphenicol

-Pharmacokinetics?

A

good po (also IV)
distributes to CNS / CSF
metabolized by glucuronidation

58
Q

Chloramphenicol

- Adverse reaction?

A

bone marrow toxicity
gray baby syndrome, GI upset
toxicity limits use in US

59
Q

Fluoroquinolones

- Mechanism of Action?

A

inhibition of DNA gyrase

bactericidal

60
Q

Fluoroquinolones

- Adverse Reaction?

A

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)

61
Q

Fluoroquinolones

- drugs?

A

Ciprofloxacin
Levofloxacin
Moxifloxacin

62
Q

Fluoroquinolones

- Pharmacokinetics?

A

good oral (also IV)

63
Q

Mechanism of actions?

  • Ciprofloxacin [37]
  • Levofloxacin [51]
  • Moxifloxacin
A

[2nd generation]
[3rd generation-respiratory FQ]
[4th generation-respiratory FQ]

64
Q

Pharmacokinetics?

  • Ciprofloxacin [37]
  • Levofloxacin [51]
  • Moxifloxacin
A

primarily renal excretion
primarily renal excretion
primarily hepatic (20% renal)

65
Q

Fluoroquinolones

- adverse reactions?

A
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)
66
Q

Nitrofurantoin

- Mechanism of Action

A

reduced in cell to intermediates that damage bacterial DNA bactericida

67
Q

Nitrofurantoin

- Pharmacokinetics

A

rapid, complete GI absorption but rapid excretion via kidneys, thus acts as urinary antiseptic

68
Q

Nitrofurantoin

- Adverse Reactions

A

GI side effects, macrocrystalline

forms better tolerated

69
Q

Metronidazole [

- Mechanism of Action

A

reduced intracellularly to active form; interference with DNA fxn bactericidal

70
Q

Metronidazole [

- Pharmacokinetics

A

good oral bioavailability

hepatic metabolism

71
Q

Metronidazole [

- Adverse Reactions

A

nausea, headache, GI distress
Antabuse®-like reaction
occasional candidal superinfections