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Transcript
Pharmacology Introduction Terminology • Drug – Pure chemical compound with specific chemical structure • Biological effects • Chemical effects • Therapeutic Effect – Intended effect of a drug • Drug Indication – Therapeutic use of a drug • Contraindication – Situation when a particular drug should NOT be used Undesired Effects of Drugs • Side Effects – Nuisance more than dangerous • E.g. dry mouth, sedation, • Adverse Effects – May be harmful • E.g. darrhea, vomitting, CNS disturbances • Toxic Effects – Drug poisoning • Most drugs exhibit all effects depending on dose Basic Concepts • Site of Action – Location within the body where the drug exerts its therapeutic effect • E.g. aspirin acts at the hypothalamus to reduce fever • Mechanism of Action – How a drug produces its effects • Anesthetic produce loss of pain by interrupting sensory nerve conduction • Receptor Site – Drug usually exerts action once binding to specific cell in the body • Often site of binding is a specific receptor • Receptor site is usually synonymous with Site of Action • E.g. morphine binds to opiod receptors in the brain to reduce pain – Same receptors as endorphins in exercise or fight of flight • Agonists and Antogonists • Drugs that bind to specific receptors and produce a drug action are termed Agonists • Drugs that bind to specific receptors but do not produce any drug action are termed Antagonists – Antagonists are used as blocking drugs • Naloxone is an antogonist to morphine receptor • Used for treatment in morphine overdose Dose-Response Curve • Dose is the exact amount of a drug that is administered in order to produce and effect – The graph of the response versus a given dose is the dose-response curve – The response is often proportional to the dose • Not always • May hit a ceiling above which no therapeutic effect is observed, but adverse effects may be • ED50 – Effective dose that elicits 50% of maximal response – Measure of potency Agonist Dose Response Curves Full agonist Partial agonist Response Dose Relative Potency hydromorphone morphine codeine Analgesia aspirin Dose Effectiveness, toxicity, lethality • ED50 - Median Effective Dose 50; the dose at which 50 percent of the population or sample manifests a given effect; used with quantal dr curves • TD50 - Median Toxic Dose 50 - dose at which 50 percent of the population manifests a given toxic effect • LD50 - Median Toxic Dose 50 - dose which kills 50 percent of the subjects Quantification of drug safety Therapeutic Index = TD50 or LD50 ED50 Drug A 100 sleep death Percent 50 Responding 0 ED50 LD50 dose Drug B 100 Percent Responding sleep death 50 0 ED50 dose LD50 Time-Response Curve • Relationship of drug response and duration of the action Drug Safety • All drugs will act as poisons if taken in excess • Therapeutic effect is distinguished from toxic effect by dose • Factors such as route of administration, absorption, and drug metabolism will influence amount of drug reaching site of action Nomenclature • All drugs typically have three names – Chemical • Gives the chemical structure of the compound – Generic • Often abbreviated form of chemical name – Trade • Name given by manufacturer to drug Drug Schedules • Schedule 1 – High abuse potential- no accepted medical use • E.g. heroin, not to be prescribed • Schedule 2 – High abuse potential – accepted medical use • E.g. morphine, cocaine, no refills without new prescription • Schedule 3 – Moderate abuse potential – accepted medical use • E.g. codeine plus another drug, can be refilled 5 x in 6 months • Schedule 4 – Low abuse potential – accepted medical use • E.g. valium, phenobarbital, can be refilled 5 x in 6 months • Schedule 5 – Limited abuse potential – accepted medical use No limitations on refill of prescription