Introduction to Pharmacology Lecture 1 - PDF

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The British University in Egypt

Dr. Nesreen Elgayar

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pharmacology pharmacokinetics drug absorption medicine

Summary

Lecture notes covering Introduction to Pharmacology, with a focus on pharmacokinetics and the factors affecting drug absorption. The lecture touches on drug properties, formulations, and clinical significance. It is from the British University in Egypt.

Full Transcript

Introduction to Pharmacology Pharmacokinetic 1 Dr. Nesreen Elgayar Pharmacodynamic Body Drug Pharmacokinetic Outlines Introduction about Pharmacology. Pharmacokinetics. Absorption of Drug. Factors Affecting Absorption...

Introduction to Pharmacology Pharmacokinetic 1 Dr. Nesreen Elgayar Pharmacodynamic Body Drug Pharmacokinetic Outlines Introduction about Pharmacology. Pharmacokinetics. Absorption of Drug. Factors Affecting Absorption of Drug. Drug Properties. Drug Formulation. Pharmacokinetics Pharmacokinetics It is a quantitative study of drug Absorption Distribution ADME Metabolism Excretion Absorption Absorption is the passage of a drug from site of administration to reach Blood Factors affecting Drug Absorption ? I- Drug Factors Drug properties Drug Formulation II- Patient Factors I. Drug properties MW ↓ MW → ↑ Absorption ↑ MW → ↓ Absorption e.g. procaine penicillin (PP) Lipophilicity Solubility Non-ionized drug is lipid-soluble and diffusible. Ionized drug is water-soluble and non-diffusible..Ionization is pH-dependent Solubility In solution, Drugs are ionized to different degrees depending on : -pH of the solution (Body fluid) and -pKa of the drug. pKa (Dissociation or Ionization Constant) It is the pH of the medium at which drug (PH=PKa) 50% 50% Ionized Nonionized Acidic Drug Basic Drug Acidic Basic Ionization Hydrophilic Nonionized Execreted Nonionized Lipid soluble( )Absorped )Lipid soluble( Absorped Clinical Significance of pKa 1. GIT Aspirin: (weak acid; pKa 3.5) is non-ionized in stomach → crosses cell membrane → gastric mucosal cells → trapped inside these cells (aspirin trap) → death of cells → peptic ulceration Clinical Significance of pKa 2. Kidney Drug ionization →↑ renal excretion. So…. Alkalinization of urine in Acidic drug Toxicity e.g. Aspirin Acidification of urine in Basic drug Toxicity e.g. Amphetamine II. Drug Formulation Active Drug + Vehicle Vehicle: Aqueous (cream) > absorbable Oily (ointment) Tablet Disintegration Particles Dissolution Molecules + Ions Fragments Absorbed.Slow release tab. & sustained release cap (Spansules) Long Acting Less Frequent administration Less Adverse Effects (Low Good Compliance peak Level) How to prolong Action of Drug? ↑ MW Use Oily Prep. Use Spansules Add VC to local anesthesia

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