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Pharmacology Second > Protein Synthesis Inhibitors > Flashcards

Protein Synthesis Inhibitors Flashcards

1
Q

RoA of Erythromycin

A
  • IV
  • Oral
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1
Q

State all macrolides

A

Erythromycin
Clarithromycin
Azithromycin
Fidaxomicin

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2
Q

MoA of Macrolides / Lincosamides / Chloramphenicol

A

They bind to and inhibit the 50S subunit, which are near
the Peptidyl transferase enzyme, resulting in inhibition
of the elongation of the polypeptide chain

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3
Q

Spectrum of Erythromycin

A

Extended:
- gram +ve
- gram -ve
- Atypical:
Mycoplasma Chlamydia Legionella

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4
Q

A.D.M.E of Erythromycin

A

A: has large MW & very lipophilic; increase absorption
D: it cannot cross BBB but it can cross the
placenta to the fetus
E: excreted in the bile

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5
Q

Indications of Erythromycin

A
  1. Erythrasma (groin skin infection) → C. minutissimum
  2. Trachoma (eyelid infection) → C. trachomatis
  3. Preoperative colon prophylaxis (Hemorrhoids)
  4. Atypical CAP → M. Pneumonia & L. pneumophilia
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6
Q

Properties of Clarithromycin

A
  • patients complain
    from metallic taste after administering Clarithromycin
  • it is well tolerated in GI than Erythromycin
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7
Q

RoA of Clarithromycin

A
  • Oral
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8
Q

Spectrum of Clarithromycin

A

Extended:
→ gram +ve
→ gram -ve
→ Atypical:
Mycoplasma
Mycobacteria

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9
Q

A.D.M.E of Clarithromycin

A

M: metabolized in the liver to 12-hydroxy clarithromycin, which is also antibacterial
E: excreted in kidneys, and dose should me reduced when ClCr < 30 mL/min

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10
Q

Indications of Clarithromycin

A
  1. HIV disseminated infections
    → Mycobacterium Avium Complex (MAC)
  2. Triple therapy for Peptic ulcer → H. pylori - Amoxiclav + Clarithromycin + PPIs or Bismuth
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11
Q

Properties of Azithromycin

A

very potent drug; 1g of Azithromycin is as effective as 7-days Doxycycline course

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12
Q

RoA of Azithromycin

A
  • IV
  • Oral
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13
Q

Spectrum of Azithromycin

A

Extended:
→ gram -ve
→ Atypical:
Chlamydia

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14
Q

A.D.M.E of Azithromycin

A

D: it can penetrate phagocytes to target the intracellular bacteria

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15
Q

Indications of Azithromycin

A
  1. CAP → H. influenza
  2. Cervicitis and Urethritis → C. trachomatis
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16
Q

Properties of Fidaxomicin

A

very expensive drug; 1 pill costs $250

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17
Q

RoA of Fidaxomycin

A

Oral

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18
Q

Spectrum of Fidaxomycin

A

Narrow: C. difficile

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19
Q

A.D.M.E of Fidaxomycin

A

A: bad oral absorption, although given orally to work locally in GIT

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20
Q

Indications of Fidaxomycin

A

Pseudomembranous colitis → C. difficile

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21
Q

Adverse Effects of Macrolides

A
  • Acute cholestatic hepatitis
    → the liver toxicity that can progress to liver failure if not treated within 3 days
  • CYT P450 inhibition
    → this will increase serum conc. of most drugs, especially those with low TI like Warfarin
  • Torsades de Pontes (TdP)
    → TdP is the QT-interval prolongation induced by
    drugs due to inhibition of K+ channels
    → using these drugs, especially Azithromycin, increases the risks of arrhythmia
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22
Q

Properties of Clindamycin/Lincomycin

A

They are basically the same drug, but Clindamycin has an extra (Cl) atom

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23
Q

RoA of Clindamycin/Lincomycin

A
  • IV
  • Oral
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24
Q

Spectrum of Clindamycin/Lincomycin

A

Extended:
→ gram +ve
→ gram -ve
→ Antifungal
→ Antiprotozoal

25
Q

A.D.M.E of Clindamycin/Lincomycin

A

E: excreted both in kidneys and bile

26
Q

Indications of Clindamycin/Lincomycin

A
  1. Anaerobic abdominal infection → B. fragilis
  2. Pneumocystis pneumonia (PCP) → Pneumocystis carinii
  3. HIV-related cerebral toxoplasmosis → Toxoplasma gondii
  4. Soft tissue infections → C. perfringens & S. pyogenes
    (Clindamycin with Penicillin G)
  5. Prophylaxis for IE in patients with prosthetic valve and penicillin allergy undergoing dental surgery
27
Q

Properties of Chloramphenicol

A

bacteriostatic, but against H. influenza & N. gonorrhea, it is bactericidal

28
Q

RoA of Chloramphenicol

A
  • IV
  • eye drop
29
Q

Spectrum of Chloramphenicol

A

Broad:
→ gram +ve
→ gram -ve

30
Q

Adverse Effects of Chloramphenicol

A

Gray baby syndrome
→ because liver enzymes in neonates are inactive,
chloramphenicol will accumulate in the blood - this results in lethargy, hypothermia, and shock - can be avoided by giving a dose < 50 mg/kg/day

31
Q

Properties of Tetracyclines

A

their structure is composed of 4 adjacent rings

32
Q

MoA of Tetracyclines

A

They reversibly bind to 30S
subunit, blocking the
binding of tRNA to the
acceptor site on the mRNA-
ribosome complex and
prevent addition of new AAs

33
Q

Spectrum of Tetracyclines

A

Extended:
→ gram +ve
→ gram -ve
→ Antiprotozoal

34
Q

A.D.M.E of Tetracyclines

A

A: absorption is impaired by food containing divalent or trivalent cations. Exception is Doxycycline and Minocycline
D: it cannot cross BBB but it can cross the placenta to the fetus
E: excreted in urine and breast milk. Exception is Tigecycline; excreted in the bile

35
Q

Adverse Effects of Tetracyclines

A
  • Bone and teeth deformation
    → tetracyclines highly accumulate in calcium-rich
    growing tissues like bones and teeth
    → contraindicated in pregnancy (Category D) and
    in children younger than 8 years
  • High conc. affect mammalian ribosomes
36
Q

RoA of Tetracycline

A
  • IV
  • Oral
37
Q

Indications of Tetracycline

A

Quadruple therapy for Peptic ulcer → H. pylori
- Tetracycline + Amoxiclav + Clarithromycin + PPIs or Bismuth

38
Q

RoA of Doxycycline & Minocycline

A
  • IV
  • Oral
39
Q

Indications of Doxycycline & Minocycline

A
  1. Acne → Cutibacterium acnes
  2. Cholera → V. cholera
  3. Amebiasis → Entamoeba histolytica
40
Q

RoA of Tigecycline

A

IV,very long half-life of 36 hours

41
Q

Indications of Tigecycline

A

Reserved for Tetracycline-resistant bacteria; as it is not affected by the common resistance mechanisms

42
Q

State the Oxazolidinones

A

Linezolid
Tedizolid

43
Q

Properties of Oxazolidinones

A

reserved drugs for life-threatening situations due to their unique MoA

44
Q

RoA of Oxazolidinones

A

Oral

45
Q

MoA of Oxazolidinones

A

They inhibit the
formation of the
mRNA-Ribosome
Complex

46
Q

Spectrum of Linezolid

A

Broad:
→ gram +ve
→ gram-ve

47
Q

Spectrum of Tedizolid

A

Narrow:
→ MRSA

48
Q

A.D.M.E of Linezolid

A

A: it has 100% bioavailability even if it is oral

49
Q

A.D.M.E of Tedizolid

A

M: given as a prodrug Tedizolid phosphate which gets metabolized into the active form

50
Q

Indications of Linezolid

A
  1. Vancomycin-resistant Enterococci (VRE)
  2. Nosocomial pneumonia
  3. Anaerobic soft tissue infections
51
Q

Indications of Tedizolid

A

Skin and soft tissue MRSA infections → S. aureus

52
Q

Drugs of Aminoglycosides

A

Streptomycin
Neomycin
Kanamycin
Amikacin
Gentamycin
Tobramycin
Sisomicin

53
Q

Properties of Aminoglycosides

A
  • they are the most used antibiotics after #1 Penicillins & #2 Cephalosporins
  • have Post-Antibiotic Effect (PAE)
54
Q

RoA of Aminoglycosides

A
  • Oral
  • IV
  • eye drop
  • Inhalation
55
Q

MoA of Aminoglycosides

A

FIRST, they enter through
pores made by the
associated β-lactams,
THEN, they irreversibly
bind to the 30S subunit

56
Q

Spectrum of Aminoglycosides

A

Narrow:
→ Aerobic gram -ve

57
Q

A.D.M.E of Aminoglycosides

A

A: they don’t get absorbed orally; as they are intended to act locally in the GIT
E: when given orally, they are eliminated by feces, other RoAs are eliminated in urine

58
Q

Adverse Effects of Aminoglycosides

A

→ Ototoxicity [Neomycin]
- due to the Vestibulocochlear nerve damage
(CN - VIII), even in pregnancy (Category D)
→ NMJ paralysis (Curare-like effect)
- associated with rapid/bolus administration
- reversible by giving Calcium Gluconate with
aminoglycosides
→ Nephrotoxicity [Neomycin]
→ Hypersensitivity [Neomycin]

59
Q

What is Creatinine Clearance (ClCr)?

A

A measure used to determine the efficiency of kidney excretion, it is the gold-standard test to determine the GFR (Glomerular Filtration Rate)
→ Normal value in males is 120 mL/min and in females is 100 mL/min

Pharmacology Second (14 decks)

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