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Drugs And Infectious Diseases > Protein synthesis inhibitors > Flashcards

Protein synthesis inhibitors Flashcards

1
Q

Macrolides

A
  • have macrocyclic lactone rings

- Erythromycin, Clarithromycin, Azithromycin

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2
Q

Macrolide spectrum

A

G(+) including MRDA (not first choice), S. pneumoniae (PEN susceptible), strep
G(-): H. influenzae, shigella, Neisseria
Atypical: Legionella, chlamydia
H. pylori (clarithromycin)

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3
Q

clinical uses of macrolides

A

penicillin substitute for strep or pneumnococcal infections in pts with hypersensitivity. Respiratory, skin and STIs

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4
Q

MoA of macrolides

A

Mainly bacteriostatic.
high affinity pocket of the peptidlytransferase site on 50s ribosomal subunit. blocks protein progression by stopping elongation.

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5
Q

Absorption/elimination of erythromycin

A

excellent tissue penetration -> cross placental barrier
half life 1-3hr.
hepatic metabolism
greater activity at high pH

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6
Q

Absorption/elimination of clarithromycin

A 
T1/2=3-5h
improved bioavailability than erythromycin. 
high concentration in phagocytes
hepatic and renal metabolism
kidney and biliary excretion
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7
Q

Absorption/elimination of azithromycin

A

VERY LONG half life 48-96h
high concentration in phagocytes and fibroblast
biliary clearance so no hepatic adjustment

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8
Q

AE erythromycin, clarithromycin and azithromycin

A

RARE: CV effects (palpitations, arrhythmias)
Ototoxicity (renal insufficient, AIDS)
Serious: cholestatic hepatits

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9
Q

Special considerations: erythromycin

A
  • metabolized by CYP450 in liver
  • acts reversible inhibitor of CYP3A4, 1A2, 2C9
  • highly concentrated in bile
  • no adjustment or renal impairment
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10
Q

Special considerations: clairthromycin

A
  • metabolized to nitrosalkane metabolite
  • inactive complex with CYP3A
  • 14 OH metabolite = abx activity
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11
Q

Special considerations: Azithromycin

A
  • lots of tissue distribution
  • lots of drug within cells
  • lots of protein binding at low plasma concentration
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12
Q

Chloramphenicol spectrum

A
  • bacteriostatic against H. influenzae, S. pneumoniae, N. meningitis
  • anaerobic bacteria & aerobic +/-
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13
Q

Clinical uses of chloramphenicol

A

Treat CNS infections (bacterial meningitis, brain abscess) in pts with allergies to B-lactams.
when other medications don’t work for anaerobic.
Rickettsial disease (tetracycline is 1st) for rocky mountain fever or typus.
Also for typhoid.

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14
Q

MoA for chloramphenicol

A

Binds to hydrophobic acyl site on 50s ribosomal subunit. prevents tRNA from binding to P-site. stops the transition state during peptide bond formation.

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15
Q

absorption/ elimination of chloramphenicol

A

absorbed in GI. widely distributed in body fluids -> goes to CSF and crosses placenta.
long half life 4h.
50% bound to plasma proteins
eliminated through hepatic metabolism

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16
Q

AE of chloramphenicol

A

Serious: Hematological effects - blood (anemia..ect) & bone marrow. Gray baby syndrome. decreased visual acuity. increased chance of childhood leukemia.

17
Q

special considerations: chloramphenicol

A

inhibits CYP3A4 and CYP2C19
involved in: tylenol, cyclosporine (inc. levels), phenobarb. (dec chloramphenicol), phenytoin toxicity, warfarin (enhanced anticoagulation).

18
Q

Clindamycin MoA

A

Bacteriostatic:

Prevents bacterial protein synthesis by binding to 50s

19
Q

Clinical application of clindamycin

A

skin and soft tissue infection. anaerobic infections and some G(+) like strep, S. pneumoniae, MSSA/MRSA. NO GRAM (-) action. Gangrene, Toxic shock syndrome, prophylactic for neuro surgery.

20
Q

PK for clindamycin

A

Hepatic clearance and metabolism CYP3A4. widely spread through body fluids and tissues but not CSF.

21
Q

AE of clindamycin

A

Serious: C. difficile colitis
Rare: Neuromuscular block (combo with relaxants)

22
Q

Streptogramins

A

Quinupristin, dalfoprostin

: against G(+) aerobic and various anaerobic

23
Q

Streptogramins MoA

A

prevents bacterial protein synthesis by binding to 50s subunit. Alone the 2 drugs are bacteriostatic but in combination they are bactericidal. Dalfoprostin directly interferes with polypeptide chain formation

24
Q

Clinical applications of Streptogramins

A

serious infections that are vancomycin resistant (E. faccium). complicated skin infections by staph. (aureus and pyrogenes). don’t use with other CYP3A4 (they inhibit it).

25
Q

PK of Streptogramins

A

IV. CYP450 inhibitor (not metabolized by this). hepatic clearance. short half life.

26
Q

AE of Streptogramins

A

severe infusion related myalgia and arthaglias. abnormal liver enzymes and billirubin.

27
Q

Linezolid spectrum

A

G(+)

28
Q

Linezolid clinical use

A

infections from MRSA, vancomycin resistant enterococci, nosocomial & community pneumonia

29
Q

Linezolid MoA

A

Bacteriostatic: prevents protein synthesis by binding to peptide site on 50s (prevents complex formation)

30
Q

PK Linezolid

A

Hepatic clearance, long half life (6h).

31
Q

AE Linezolid

A

Bone marrow suppression, neuropathy, optic neuritis. potentiate effects of SSRI -> serotonin syndrome

Drugs And Infectious Diseases (4 decks)

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