Controlling Drugs PHARMACOLOGY. Questions. Basics. An Introduction to. Categorizing Drugs. Naming Drugs. Drugs can be categorized by
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1 Basics An Introduction to PHARMACOLOGY A drug is a chemical substance that alters a body function, Drugs work at the cellular level, Drugs are distributed to ALL parts of the body via blood, not just the to target organ, therefore, All drugs have side effects Categorizing Drugs Birth control Naming Drugs Drugs can be categorized by 1. body system, 2. effect, 3. composition genitourinary Estrogen Chemical Name ( ie, proprionic acid) Proprietary, brand, trade name (Motrin) Protected for 17 years Generic Name (ibuprofen) Name given by U.S. Adopted Names Council Questions Controlling Drugs Below is the brand name and the generic name for the same drug. Which is which and how do you know? Tequin gatifloxacin FDA (Federal dministration) measures safety and effectiveness, determines if OTC or prescribed, how to advertise DEA (drug enforcement agency) controls drugs have abuse potential, 1
2 HEADING BODY CLOSING superscription Amoxicillin 500 mg. PRESCRIBING Inscription DRUGS Disp: 4 tabs Subscription Sig: Take all tabs 1 hr before dental appt. Transcription Scheduled Drugs Drugs are categorized 1,2,3,4 or 5, with 1 having most abuse potential, 5 least 1=no medical use 2 =written Rx needed, no refills 3 and 4=verbal Rx OK, 5 refills allowed 5=OTC in some states Pharmocokinetics Absorption getting drug into bloodstream Distribution getting drug to target organs and other sites Effect (stimulate or inhibit cells) Metabolism (biotransformation)- changing drug for elimination Elimination removal of drug from body Intraveneous (Quickest route) Inhalation (Controlled effects) Oral (easy) Intramuscular (modifies irritating drugs) Questions -Absorption-Sublingual (quick and easy) Topical Routes of (locally Administration effective) -absorption- Drug must pass thru biologic membrane to reach circulation Which of the previous routes are parenteral? Which of the previous routes bypass absorption? 2
3 -absorption- Drug must pass thru biologic membrane to reach circulation water soluble Lipid soluble Water pour Mostly lipid nonionized Water pour Mostly lipid ionized Biologic Membrane What determines the amount of ionized vs nonionized drug? The ph of the water and whether the drug is an acid or a base If drug is an acid, More drug is nonionized when water is acidic,(ph < 7.0) More drug is ionized when water is basic Therefore acidic drugs work better in an acidic environment If drug is a base, More drug is nonionized when water is basic (ph > 7.0) More drug is ionized when water is acidic Therefore more basic drugs work better in a basic environment Oral Administration LIVER Nontarget organ Target organ First Pass Effect Oral medications pass through liver first, Certain amount metabolized and is ineffective, Therefore some drugs not given orally (morphine) LIVER -Distribution Protein Binding Unbound drug effective Blood Vessel protein Why are some people more effected by a drug than others? 3
4 -Effect Potency -Effect Efficacy Drug B Drug B More potent (Smaller doses needed) more effective because it attaches to more sites Drug B nontarget -Effect Drug Interactions Metabolism (biotransformation) Most drugs metabolized in liver by cytochrome P450 enzymes Some drugs metabolized by enzymes in plasma Oral administered experience first pass effect Rate of metabolism measured in half lives A drug s Half Life The time it takes for half of the drug in the circulation system to be metabilized Half life varies, long acting drug has a longer half life After 5 half lives, drug is considered ineffective 100% -50% - 25% % % - 3% Excretion Most drugs excreted by kidneys, but also in feces, saliva, sweat Kidney disease can lead to toxic amounts of drug retained 4
5 Adverse Reactions Toxic Reaction Side effects Predictable Toxic reaction ( target organ overreaction) Idiocyncratic reaction (genetic related abnormal reaction) Allergic reaction If liver busy metabolizing drug A and drug B metabolized by same process, toxic levels of drug B may develop B A LIVER Allergic Response Allergic Response Type I anaphylaxis (histamine release) Type II Cytotoxic (Rh factor) Type III immune complex (Serum sickness) Type VI (cell mediated) (contact dermatitis) Common side effects with oral implications Xerostomia Gingival hyperplasia Bleeding Nausea, vomiting, Mucositis Dysgeusia Therapeutic Index Measures the safety of a drug Numerator is the dose that kills 50% of test animals - LD50 (lethal dose for 50%) Denominator is dose that produces desired effect in 50% of test animals - ED50 (effective dose in 50%) Drugs with index less than 10 are dangerous Ex. - LD50 of 100 mg / ED50 of 5 mg =TI of 20 5
6 -Summary- Drug Effectiveness Patient size - Redistribution and binding to non target tissue decreases effect Liver function Oral drugs pass thru liver before target organ (first pass effect), Nutrition Drug binds to protein in blood Acidity If tissue acidic, drug will be ionized, won t pass cell membrane easily 6
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