Drug Response & Interactions PDF
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San Lorenzo Ruiz College of Ormoc, Inc.
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Summary
This document discusses various aspects of drug response and interactions, including idiosyncratic responses, hypersensitivity reactions, and different types of antagonism. It explains the concepts of tolerance, tachyphylaxis, receptor alterations, and desensitization. Examples of drug interactions and classifications are also provided.
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Idiosyncrasy - Unusual drug Response caused by genetic differences in metabolism of the drug or by immunologic mechanisms, including allergic reactions. Hyporeactivity - the intensity of effect of a given dose of drug is diminished Hyperreactivity- the intensity of effect of a given dose of...
Idiosyncrasy - Unusual drug Response caused by genetic differences in metabolism of the drug or by immunologic mechanisms, including allergic reactions. Hyporeactivity - the intensity of effect of a given dose of drug is diminished Hyperreactivity- the intensity of effect of a given dose of drug is increased in comparison to the effect seen in most individuals. Hypersensitivity -refers to allergic or other immunologic responses to drugs TYPE OTHER NAM NAMES MES I Allergyy (Immediate) (Immediate) II Cytotoxic, Cytotoxxic, Antibody dependent dep pendent III Immune ne Complex Immun Complex Disease e IV Delayed-Type Hy Hypersensitivity ypersensitivity V Autoimmune Aut Disease toimmune Dis sease Tolerance - it refers to a decreased responsiveness to the drug a consequence of continued drug administration Tachyphylaxis- This refers to rapidly acting tolerance Responsiveness diminishes rapidly after administration of a drug Alterations in Number or Function of Receptors Down-regulation of receptors it is caused by continuous prolonged exposure of receptors to drugs that disrupt the homeostatic equilibrium and result in altered levels of the receptors. Desensitization It is the result of down-regulation. The target cells become desensitized, and the effect of subsequent exposure to the same concentration of the drug is reduced. Classification of drugs according to receptor interaction 1. AGONIST Able to bind (with affinity) With intrinsic activity 1.1 Full agonist Full response Stimulate all different variant of receptors even the new receptors 1.2 Partial agonist Less than the expected response 2. ANTAGONIST With affinity but no intrinsic activity It prevents the binding of agonist Antagonist Antago onist Recept Receptor tor Antagonist-Receptor Antagon nist-Recepto or DENIED! DENIED!! Complex Comple ex PHARMACOLOGIC ANTAGONIST utilizes the same receptor produce an effect opposite of agonist by binding to the same receptor Beta blocker and Beta agonist (Propranolol) (epinephrine) PHYSIOLOGIC ANTAGONIST - occurs when the drugs act independently at different receptor sites, often yielding opposing actions. e.g. HISTAMINE + EPINEPHRINE CHEMICAL ANTAGONIST no receptor is involved occurs when two drugs bind with each other to form an inactive compound. Protamine SO4 + Heparin SO4 o forms a complex devoid of action Protamine- (+) charged at physiologic pH Heparin ± (-) charged at physiologic pH Chelating agents Deferoxamine ± Iron (Fe) It depends on whether or not they reversibly compete with agonists for binding to receptors Competitive antagonist- Effects of Antagonist can be overcome/reversed by increasing the concentration of agonist NO RESPONSE NON-COMPETITIVE ANTAGONISM it is also known as irreversible antagonism 1. ADDITION A drug effect that is equal in the magnitude to the sum of the individual effects of two drugs. Two different drugs with the same effect are given together. 1 +1=2 Alcohol + Sedative hypnotic drug 2. SYNERGISM The effect of two drugs is greater in magnitude than the sum of the individual effects of the two drugs. Two drugs with same effect are given together. 1 +1=3 Sulfamethoxazole + Trimethoprim 3. POTENTIATION Occurs when one drug, lacking an effect of its own, increases the effect of another drug that is active. 1 + 0 = 2 Tyramine-containing Foods + MAOI