Module 4a Pharmaceutically Active Components
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Definition of Pharmacodynamics
The study of how a drug affects the organism/body
Definition of Pharmacokinetics
The study of how the organism/body affect the drug. The study of how absorption, distribution, metabolism, and excretion of drug from the body.
What does Pharmacodynamics include?
Site of Action Mechanism of Action Receptor Binding Post-receptor Effects Chemical Interactions
What can affect pharmacodynamics?
Disease/Disorder Age Drug-Drug Interactions
What are three receptor subtypes?
Enzymes Ion Channels Membrane Receptors
What are 4 chemical interactions involved with drug binding?
Electrostatic interaction (intermolecular forces) Hydrophobic Interactions Covalent Bonds Stereospecific Interactions (enantiomers)
What are 3 drug properties?
Affinity - how well the drug binds to the receptor Efficacy - how well the drug produces its desired effect Potency - term used to compare the relative affinity of competing drugs
What are two categories of drugs?
Agonist - bind and activates receptors Antagonist - bind, but do not activate receptors
What are two types of antagonist drugs?
Competitive - bind reversibly Non-competitive- either binds irreversibly or binds to create allosteric effects that diminish agonist’s ability to bind to a different receptor
___________ affects the ability of the drug to give its desired effect.
Concentration
What is Bioavailability?
How much of the administered drug is actually absorbed. Typically used for oral administration.
What are 8 factors affecting bioavailability?
• Molecular weight of the drug. • Drug Formulation • Drug Stability (pH sensitivity) • First Pass Metabolism (Liver) • Blood Flow • Gastric Emptying • Intestinal Motility • Drug Interactions
______________ properties help determine ability of drug to be distributed to the desired receptor site.
Drug Solubility
What are two common processes of metabolism?
Hydrolysis (esters, amides, nitriles) REDOX reactions (Cytochrome P450 enzymes in the liver)
What are 4 main routes for excretion?
• Kidneys (majority of drugs) • Feces (unabsorbed drugs from the bile) • Lungs (inhaled anesthetic drugs) • Sweat (not very common)
What is the Lipinski Rule of 5?
Describes drug potential for a new chemical entity (NCE). Used as a tool to measure a NCE’s potential bioavailability.
The Lipinski Rule of 5 is based on what four factors?
• Hydrogen bond donors (typically amine and alcohols) - no more than 5. • Hydrogen bond acceptors (total # of N, O, and F) - no more than 10 • Molecular Weight - less than 500 • Calculated Partition Coefficient (cLogP) - no more than 5 *Violation of more than one of these rule predicts NCE is not orally available.
Structural alerts of certain functional groups that have been linked to increase toxicity due to their metabolites. Name 5 examples listed in lecture.
• Aromatic anilines • Nitroaromatics • Aliphatic Halides • Polycyclic Aromatics Hydrocarbons- 3 or more rings together • Thiophenes