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Pharmacology FINAL (2nd sem) > C15+16 > Flashcards

C15+16 Flashcards

1
Q

Macrolides

3

A
  • Clarithromycin
  • Azithromycin
  • Roxithromycin
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2
Q

Ketolides

A

Telithromycin

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3
Q

Macrolides MOA

A
  • bacterioSTATIC inhibitors of protein synth. (50s)

- block transpeptidation

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4
Q

macrolide structure?

A
  • cyclic lactone ring with sugars attatched
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5
Q

Clarithromycin Pharmacokinetics

A
  • administration : oral !
  • Bioavailability: good oral bioavailability
  • distribution: most body tissues
  • metabolism: hepatic
  • elimination: urinary excretion
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6
Q

Azithromycin pharmacokinetics

A
  • absorption: impeded by food (not good oral availability)
  • administration: I.V
  • distribution: levels in tissues & phagocytes > plasma
  • clearance: Hepatic
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7
Q

Antimicrobial activity of Azithromycin and Clarithromycin

A
  • CAP
  • Corynebacteria
  • Chlamydial infection
  • Pertussis
    (CCCP)
  • G+ cocci,
  • some G- organisms
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8
Q

G+ resistance mechanisms?

A
  • efflux pump

- production of a methylase –> adds a methyl to the ribosomal binding site

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9
Q

what is special indications of Azithromycin?

A

given IV

  • effective in gonorrhea (alternative to ceftriaxone)
  • effective in syphilis (alternative to penicillin G)
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10
Q

Macrolides clinical uses?

A
  • CAP (Chlamydophila pneumoniae, Legionella pneumophila, M. pneumoniae)
  • cornyebacteria
  • chlamydia
  • pertussis
  • G+ cocci (except PRSP)
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11
Q

special clinical uses of Azithromycin?

[ H&M ;) ]

A
  • H influenzae
  • Neisseria
  • Moraxella catarrhalis

also:
UGIs by: C.Trachomatis
(long 1/2 life –> single dose is given)

also:
CAP (4-d course)

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12
Q

special clinical uses of Clarithromycin

A
  • Prophylaxis treatment of Mycobacterium avium complex

- component of drug regimens for ulcers (by H pylori)

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13
Q

Macrolides Toxicity in general?

A
  • G.I. irritation (motolin rec. Stim)
  • Hepatic dysfunction
  • QT prolongation
  • CYP450 inhibition (NOT azithromycin)
  • skin rashes
  • eosinophilia
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14
Q

Clarithromycin toxicity?

A
  • inhibits several cyt.P450 –> increase the plasma levels of other drugs
    (ex. anticoagulants, carbamazepine, digoxin, theophylline)
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15
Q

Azithromycin Toxicity?

A
  • drug interactions are uncommon (does not inhibit hepatic cyt.P450)
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16
Q

about Telithromycin?

A

ketolide structurally related to macrolides

17
Q

Telithromycin MOA and spectrum

A

similar to Macrolides but narrower spectrum\

bind 50s subunit > inhibit protein syn
bacterioSTATIC

18
Q

why we use Telithromycin?

A
  • some macrolide-resistant strains are susceptible to Telithro
  • because it binds more tightly to ribosomes and is a TOO LARGE substrate for efflux pumps
19
Q

Telithromycin clinical uses?

A
  • used in CAP (including MDRs)
20
Q

Telithromycin pharmacokinetix

A

oral!

eliminated in the bile and the urine

21
Q

Telithromycin Toxicity?

A
  • hepatic dysfunction
  • QTc interval prolongation
  • inhibitor of the CYP3A4
22
Q

Clindamycin MOA

A
  • binds 50S ribosome> inhibits bacterial protein synth.
  • block transpeptidation

bacteriostatic

23
Q

Resistance to Clindamycin ?

A
  • binding site methylation on 50S
  • enzymatic inactivation
  • Clinda has poor penetration through the outer membrane of G- Aerobes!
24
Q

Clindamycin Pharmacokinetix

A

oral, IV

  • distribution: Good tissue penetration after oral abs
  • clearance: hepatic
  • Elimination: biliary & renal excretion (both intact drug + metabolites)
25
Q

Clindamycin uses?

A
  • skin, soft tissue infections
  • ANaerobic infection (ex. Bacteroides -severe-)
  • backup against G+ cocci (ex. MRSA)
  • prophylaxis of endocarditis in valvular disease (allergix to penicillin)
  • against P.jirovecii
26
Q

Clindamycin Toxicity?

A
  • G.I. upset
  • C.difficile colitis
  • skin rashes
  • NEUTROpenia
  • hepatic dysfunction
27
Q

Streptogramins?

A

Quinupristin-dalfopristin

bactericidal!!

28
Q

Quinupristin-dalfopristin MOA?

A
  • Bactericidal
  • 50S ribosomal subunit –> constricting the exit channel on the ribosome –> nascent polypeptides are extruded.
  • tRNA synthetase activity is inhibited –> decrease in free tRNA within the cell
29
Q

Quinupristin-dalfopristin activity?

A
  • staphylococci

* VRE. faecium

30
Q

Quinupristin-dalfopristin Spectrum?

A
  • PRSP
  • MRSA
  • VRSA
  • VRE.Faecium
31
Q

Quinupristin-dalfopristin administration?

A

I.V.

32
Q

Quinupristin-dalfopristin Toxicity?

A
  • pain
  • infusion related arthralgia-myalgia syndrome

inhibitors of CYP3A4 –> increase plasma levels of drugs
(cyclosporine, diazepam, NNRTI, warfarin)

33
Q

Oxazolidinones?

A

Linezolid

34
Q

Linezolid MOA?

A
  • bacterioSTATIC

- 50S –> Block tRNA-ribosome-mRNA ternary complex formation –> inhibit initiation

35
Q

Linezolid Spectrum?

A
  • against drug-resistant G+ cocci, including strains resistant to penicillins
  1. MRSA (skin &soft tissue infections)
  2. PRSP
  3. vancomycin (eg, VRE)
  • against L. monocytogenes and corynebacteria

indications kinda similar to streptogramins (quinapristin/dalfopristin )

36
Q

can linezolid be resisted?

A

RARE

37
Q

Linezolid formulation?

A

both Oral and I.V

38
Q

Linezolid Pharmacokinetix?

A

-oral, I.V

  • metabolism: hepatic
  • elimination half-life: 4–6 h
39
Q

Linezolid Toxicity?

A
  • dose-related ANEMIA
  • optic Neuropathy
  • in immunocompromised:
    Thrombocytopenia * Neutropenia

Pharmacology FINAL (2nd sem) (37 decks)

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