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Transcript
Chapter 2 Basic Concepts of Pharmacology Chapter 2 Topics • • • • Receptors Mechanisms of Drug Action Pharmacokinetics Drug Effects Learning Objectives • Understand receptors and their function in mechanisms of drug actions. • Be aware of the pharmacokinetics involved in developing and testing drugs. • Understand that some drug effects are beneficial whereas others can be harmful. • Be familiar with the common terms used to describe drug interactions. Receptors • A receptor is a protein molecule on the surface of or within a cell that recognizes and binds with specific molecules, thereby producing some effect within the cell. Receptors • A receptor is a protein molecule on the surface of or within a cell that recognizes and binds with specific molecules, thereby producing some effect within the cell. – receptor site may have specificity – the affinity is the strength by which a particular chemical messenger binds to its receptor site or cell Mechanisms of Drug Action Agonist An agonist is a drug that binds to a particular receptor site and triggers the cell’s response in a manner similar to the action of the body’s own chemical messenger. Mechanisms of Drug Action Antagonist An antagonist is a drug that binds to a receptor site and blocks the action of the endogenous messenger or other drugs. Pharmacokinetics • Activity of a drug within the body over a period of time. • Includes ADME Pharmacokinetics • Activity of a drug within the body over a period of time • Includes ADME – – – – absorption distribution metabolism elimination Pharmacokinetics Absorption Process whereby the drug enters the circulatory system Pharmacokinetics Distribution Process by which a drug moves from the blood into other body fluids and tissues and ultimately to its sites of action Blood flow is the rate-limiting factor. Pharmacokinetics Metabolism Process by which drugs are chemically converted to compounds and then excreted through metabolic pathways. Induction Inhibition Pharmacokinetics Elimination Clearance is the rate at which a drug is eliminated from a specific volume of blood per unit of time. Discussion What are the primary sites of elimination in the body? Discussion What are the primary sites of elimination in the body? Answer: The kidney and the liver, but can also be exhaled by the lungs or excreted in perspiration. Pharmacokinetics Dose-Response Curve Pharmacokinetics Therapeutic Range Pharmacokinetics Duration of Action Discussion How is a drug’s volume of distribution, clearance, and half-life used in dosing drugs? Discussion How is a drug’s volume of distribution, clearance, and half-life used in dosing drugs? Answer: Volume of distribution is important for calculating the loading dose, clearance for calculating the maintenance dose, and half-life for determining the dosing interval. Pharmacokinetics Pharmacokinetic Modeling Method of describing the process of ADME of a drug within the body Drug Effects Beneficial Responses Drug Effects Beneficial Responses – Therapeutic Effect The action for which the drug is prescribed Drug Effects Beneficial Responses – Therapeutic Effect The action for which the drug is prescribed – Local Effect Confined to a specific part of the body Drug Effects Beneficial Responses – Therapeutic Effect The action for which the drug is prescribed – Local Effect Confined to a specific part of the body – Systemic Effect Generalized, all-inclusive effect on entire body Discussion What are some of the issues a healthcare practitioner considers when selecting a drug for an individual patient? Drug Effects When choosing a drug for a patient, a healthcare practitioner considers: Indications The diseases, symptoms, and conditions for which the drug is known to be of benefit Contraindications The diseases, symptoms, and conditions for which the drug will not be beneficial and may do harm Drug Effects Side Effects Secondary responses to a drug other than the primary therapeutic effect for which the drug was intended • Allergic responses • Drug dependence, addiction, abuse, and tolerance Common Drug Relationships Addition Antagonism The combined effect of two drugs. It is equal to the sum of the effects of each drug taken alone. The action of one drug negates the action of a second drug. Common Drug Relationships Potentiation Synergism An effect that occurs when a drug increases or prolongs the action of another drug, and the total effect is greater than the sum of the effects of each drug used alone. Joint action of drugs in which their combined effect is more intense or longer in duration than the sum of their individual effects. Discussion Name a common food-drug interaction. Discussion Name a common drug-food interaction. Answer: Grapefruit juice can affect drugs for up to a day following ingestion. Discussion Why is it important for the pharmacy to have a complete list of all of the prescription drugs, OTC medications, vitamins, and herbal remedies that a patient is taking? Discussion Why is it important for the pharmacy to have a complete list of all of the prescription drugs, OTC medications, vitamins, and herbal remedies that a patient is taking? Answer: Such a list will help healthcare professionals identify potential drug interactions.