Medicines

­           Introduction, short hystory of medicins and drug discovery. Fundamental conceptions in medicinal chemistry. Rules of drug research and production: preclinical and clinical development, GLP, GMP, role of FDA and other offices.

­           Biological molecules: amino acids, peptides and proteins, carbohydrates, lipids, nucleic acids.

­           Routes of drug administration: methods of extravascular and intravascular administration. Methods to influence of the duration of biological effect (retardation, special methods).

­           The pharmacokinetic phase: role of adsorption, distribution, metabolism and elimination (ADME) properties in drug action.

­           Dose/biological effect relations: single oral dose, repeated oral doses. Calculation of safety parameters of drugs (ED50, LD50, TI, CSF, SSM). Selectivities of biologically active compounds, effects and side effects.

­           Time dependent exchange of bilogical effects of drugs: habituation, addiction, sensitivity and allergic reactions. Drug-drug interactions: synergism, antagonism.

­           Absorption and distribution of drugs: diffusion, carrier aided absorption, biological pump mechanisms. Determination of drug distribution.

­           Effects of the drugs on the human body: drugs with physical or physico-cemical effects. Type of chemical bonds between a drug and the biological target molecule: reversible and irreversible connections. Affinity and specific activity. Multipoint interactions: role of stereochemistry in drug action.

­           Drug metabolism: phase I metabolitic reactions (oxidation, reduction, hydrolysis, hydration) and phase II reactions (conjugations).

­           Drug metabolism and drug design (prodrugs, active metabolites, etc).

­           Elimination of drugs and metabolites. Renal elimination, role of the liver in elimination. (Enterohepatic cycle, reabsorption in kidney).

­           An introduction to drug discovery: solubility and drug design. Hansch parameter, electronic and steric effects. QSAR approaches, computer aided drug design, methods for preparation molecular libraries and HTS methods.

­           Selected examples of drug action at some common target areas: 

Antibacterial and antifungal agents. Antiinflammatory agents (steroids and nonsteroid type antiinflammatory agents). Opioid type analgesics.