1. TOPICS TO DISCUSS
Pharmacokinetics
1. Penetration of drug molecules across cell membrane.
a) Mechanisms of penetration:
• lipid diffusion;
• aqueous diffusion;
• carrier-mediated transport;
• pinocytosis.
b) Dependence of drug penetration on lipid (water) solubility of drugs.
2. Penetration of weak acids and bases through cell membrane (dependence on the pH of the medium and the pKa).
3. Routes of drug administration. The main characteristics.
4. Drug absorption. Dependence of drug absorption on routes of administration and relative lipophilicity of drugs. Absorption of weak acids and weak bases in the gastrointestinal tract.
5. The main mechanisms of drug absorption after oral, intramuscular, and subcutaneous administration.
6. Bioavailability. Factors that influence bioavailability of drugs after oral administration (first-pass elimination etc). Determination of drug bioavail-ability.
7. Distribution of drugs in the body. Penetration through the blood-brain barrier. Difference between lipophilic and hydrophilic drugs.
8. Apparent volume of distribution. Drug distribution in the water compartments of the body (plasma, extracellular and intracellular fluids).
9. Accumulation of drugs in the body. Binding of drugs to tissue and plasma proteins.
10. Drug biotransformation (metabolism). Phase I and phase II reactions. The main changes in the properties of drugs caused by their metabolism (lipophilicity, hydrophilicity, activity and toxicity).
11. Excretion of drugs. Routes of excretion.
12. Excretion of drugs by the kidney. Difference between lipophilic and hydrophilic drugs. Excretion of weak acids and weak bases.
13. Enterohepatic circulation. Other routes of excretion.