Chemotherapy Pharmacology

Flashcards based on lecture notes about Chemotherapy Pharmacology, including classifications, mechanisms of action, and pharmacokinetics of antimicrobial drugs.

What are Antimicrobial Agents?

Antibacterial, Antifungal and Antiviral drugs.

What are Anti-parasitic Agents?

Anti-helminthic and Anti-protozoal drugs.

What do Beta-lactam Antibacterials do?

Bind to Penicillin-Binding Proteins (PBPs), inhibit late steps in synthesis, and produce autolysins enzymes.

How do Aminoglycosides inhibit protein synthesis?

Enter cell by Oxygen dependent system and Binds to 30 S, causing Disruption of polysomes/ Misreading of genetic code.

How do Tetracyclines inhibit protein synthesis?

Binds to 30 S and Blocking access of tRNA

How does Chloramphenicol inhibit protein synthesis?

Inhibits peptidyl transferase [transpeptidation].

How do Clindamycin, Macrolides, Streptogramins, and Linezolid inhibit protein synthesis?

Bind 50 S or Bind 30 S to inhibit Translocation

What effects do Bactericidal antibiotics have?

Kill the microorganisms e.g. penicillin & aminoglycosides.

What effects do Bacteriostatic antibiotics have?

Stop growth of microorganisms with the need for the body defense mechanisms to eradicate the infection.

What is the significance of Post antibiotic effect (PAE)?

Persistence of antibiotic effect for a period of time after its level falls below the minimum inhibitory concentration (MIC).

What are examples of Concentration – Dependent Antibiotics With PAE?

Aminoglycosides and Quinolones

What are examples of Time- Dependent Antibiotics With minimal or no PAE?

β-lactams and Vancomycin

What are maximization administration approaches for Concentration –Dependent antibiotics?

Maximize drug Conc. with Large infrequent doses (Once/day).

What are maximization administration approaches for Time-Dependent antibiotics?

Maximize duration of exposure to drug with Small frequent doses & IV infusions

Name narrow sprectrum Beta Lactam Antibiotics

Penicillin V

Name B-Lactamase Resistant Antibiotics that are orally administered

Oxacillin, Cloxacillin, Flucloxacillin, Nafcillin

Name long acting Penicillin Antibiotics

Procaine Penicillin and Benzathine Penicillin

Name Broad-spectrum Penicillin Antibiotics

Ampicillin and Amoxicillin

Name Antipseudomonal Penicillin Antibiotics

Ticarcillin, Piperacillin, Carbenicillin oral

Why is Probenecid used with Penicillin?

Inhibits the secretion of penicillins by competing for active tubular secretion, thus prolonging its duration.

What are some adverse effects of Penicillin?

Hypersensitivity and Diarrhea with ampicillin

Name first generation Cephalosporins

Cephadroxil, Cephalexin and Cefazolin

Name second generation Cephalosporins

Cefaclor, Cefuroxime, Cefoxitine and Cefotetan

Name third generation Cephalosporins

Cefotaxime, Ceftazidime, Ceftriaxone and Cefoperazone

Name fourth generation Cephalosporins

Cefepime

Name fifth generation Cephalosporins

Ceftaroline

For what is Cefazoline used?

Surgical prophylaxis

For what is Ceftriaxone used?

Gonorrhea, Typhoid fever and meningitis

What is specific adverse effect of CefoPerazone?

Platelet dysfunction, ↓Prothrombin Alcohol intolerance

What is specific advantages of the usage of Cefoperazone & ceftriaxone?

Excreted mainly in bile, thus can be used in biliary infection or renal dysfunction.

What are some adverse effects of Cephalosporins?

Allergy and cross allergy with penicillin [10 %], Nephrotoxicity and Alcohol intolerance (Disulfiram like)

What is combined with Imipenem and why?

Cilastatin, to ↓ its nephrotoxicity and prevent inactivation

Name a Monobactam Antibiotic

Aztreonam

Name B-Lactamase Inhibitors

Clavulenic, Sulbactam and Tazobactam

Why are Penicillins and aminoglycosides combined?

Synergistic effects: Because cell wall synthesis inhibitors alter the permeability of bacterial cells, these drugs can facilitate the entry of aminoglycosides