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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
Spectrum of Clindamycin/Lincomycin
Extended: → gram +ve → gram -ve → Antifungal → Antiprotozoal
25
A.D.M.E of Clindamycin/Lincomycin
E: excreted both in kidneys and bile
26
Indications of Clindamycin/Lincomycin
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
Properties of Chloramphenicol
bacteriostatic, but against H. influenza & N. gonorrhea, it is bactericidal
28
RoA of Chloramphenicol
* IV * eye drop
29
Spectrum of Chloramphenicol
Broad: → gram +ve → gram -ve
30
Adverse Effects of Chloramphenicol
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
Properties of Tetracyclines
their structure is composed of 4 adjacent rings
32
MoA of Tetracyclines
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
Spectrum of Tetracyclines
Extended: → gram +ve → gram -ve → Antiprotozoal
34
A.D.M.E of Tetracyclines
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
Adverse Effects of Tetracyclines
* 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
RoA of Tetracycline
* IV * Oral
37
Indications of Tetracycline
Quadruple therapy for Peptic ulcer → H. pylori - Tetracycline + Amoxiclav + Clarithromycin + PPIs or Bismuth
38
RoA of Doxycycline & Minocycline
* IV * Oral
39
Indications of Doxycycline & Minocycline
1. Acne → Cutibacterium acnes 2. Cholera → V. cholera 3. Amebiasis → Entamoeba histolytica
40
RoA of Tigecycline
IV,very long half-life of 36 hours
41
Indications of Tigecycline
Reserved for Tetracycline-resistant bacteria; as it is not affected by the common resistance mechanisms
42
State the Oxazolidinones
Linezolid Tedizolid
43
Properties of Oxazolidinones
reserved drugs for life-threatening situations due to their unique MoA
44
RoA of Oxazolidinones
Oral
45
MoA of Oxazolidinones
They inhibit the formation of the mRNA-Ribosome Complex
46
Spectrum of Linezolid
Broad: → gram +ve → gram-ve
47
Spectrum of Tedizolid
Narrow: → MRSA
48
A.D.M.E of Linezolid
A: it has 100% bioavailability even if it is oral
49
A.D.M.E of Tedizolid
M: given as a prodrug Tedizolid phosphate which gets metabolized into the active form
50
Indications of Linezolid
1. Vancomycin-resistant Enterococci (VRE) 2. Nosocomial pneumonia 3. Anaerobic soft tissue infections
51
Indications of Tedizolid
Skin and soft tissue MRSA infections → S. aureus
52
Drugs of Aminoglycosides
Streptomycin Neomycin Kanamycin Amikacin Gentamycin Tobramycin Sisomicin
53
Properties of Aminoglycosides
* they are the most used antibiotics after #1 Penicillins & #2 Cephalosporins * have Post-Antibiotic Effect (PAE)
54
RoA of Aminoglycosides
* Oral * IV * eye drop * Inhalation
55
MoA of Aminoglycosides
FIRST, they enter through pores made by the associated β-lactams, THEN, they irreversibly bind to the 30S subunit
56
Spectrum of Aminoglycosides
Narrow: → Aerobic gram -ve
57
A.D.M.E of Aminoglycosides
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
Adverse Effects of Aminoglycosides
→ 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
What is Creatinine Clearance (ClCr)?
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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