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Faculty of Pharmacy Department of Pharmacology pharmacology General Pharmacology 3rd year pharmacy students By  “Dr. Shimaa Elshazly”
What is pharmacology? The term pharmacology comes from the Greek words: •Pharmakon- drug or medicine •Logos- the truth about or a rational discussion             …………Truth about medicine • Pharmacology is the study of how drugs exert their effects on living systems. • More specifically it is the study of the interactions between a living organism and drugs that alter normal biochemical function.
History of Pharmacology Early pharmacology focused on natural substances, mainly plant extracts.
Modern approach ,[object Object],Foundational  Medicine Clinical Medicine Pharmacology Medicine Pharmacy Manufacture  of  Drugs Research  of  Drugs
……..Subdivisions of Pharmacology ,[object Object],application of pharmacodynamics and pharmacokinetics to human. •Toxicology -Study of harmful effects of drug •Posology- How medicines are dosed or calculation of dose •Pharmacognosy- Development of medicinal substances obtained from plants
Division of Pharmacology: ,[object Object],Pharmacokinetics: Study of the absorption, distribution, metabolism and excretion of drugs (ADME). ……………..what the body does to the drug B. Pharmacodynamics: Study of the molecular, biochemical and physiology effects of drugs on cellular systems and their mechanisms of action. ……………..what the drug does to the body
What Is a Drug? ,[object Object],In other meaning: ,[object Object],[object Object]
1- Natural:  Plant Origin: eg.Atropine from belladonna & Morphine from Opium.  b) Animal Origin: eg. Insulin, calcitonin etc.  2- Semisynthetic: ,[object Object],3- Purely synthetic: ,[object Object],[object Object]
Pharmacokinetics of drugs (ADME) ……………..what the body does to the drug Are studies of:  ,[object Object]
Distribution or Disposition
Metabolism
Excretion or Eliminationof drugs,[object Object]
Drug Absorption • Absorption is the movement of a drug from its site of application into the blood or lymphatic system without being chemically altered • Mathematically it is define in terms of Bioavailability (Rate and extent of absorption).
Bioavailability Definition: Rate and extent of absorption  i.e. Ka (Absorption constant)………. Rate of absorption.  Area under curve (AUC)………. extent of absorption. • for i.v.: 100% • for non i.v.: ranges from 0-100% e.g. lidocaine bioavailability is 35% due to destruction in gastric acid and liver metabolism
Process of Absorption In order for a drug to be absorbed, it must be able to pass through cell membranes (which is a lipid barrier) • Lipid soluble drugs would be ideal to pass through the membrane easily. • Drugs can be absorbed by 4 main ways : 1. Simple diffusion = passive diffusion.   2. Active transport.   3. Facilitated diffusion.   4. Pinocytosis (Endocytosis).
Cell membrane
Simple or passive diffusion ,[object Object]
 Lipid soluble drug (nonionized or non polar) is readily absorbed via cell membrane itself.,[object Object]
Simple diffusion Characters ,[object Object]
Occurs along concentration gradient. Non selective
 Not saturable
 Requires no energy
 No carrier is needed
Depends on lipid solubility.,[object Object]
Simple diffusion Drugs exist in two forms ionized (water soluble) & nonionized forms (lipid soluble) in equilibrium. Drug ionized + nonionized  Only nonionized form is absorbable.
Six things influence the rateof diffusion ,[object Object]
Size of molecule involved                      Large molecules slowdiffusion
Distance the molecule has to travelShort distance increase diffusion
TemperatureHigh temperatures increasediffusion
Solubility of the molecule
Surface area of the membrane over which the molecule can work.Large surface area increase diffusion,[object Object]
Occurs against concentration gradient.
Requires carrier and energy.
Specific
Saturable.
 Iron absorption.
Uptake of levodopa by brain.,[object Object]
Carrier-mediated Facilitated Diffusion ,[object Object]
Requires carriers
Selective.
Saturable.
No energy is required.
Selection is by size; shape; charge.
Common molecules entering/leaving cells this way include glucose and amino-acids.  ,[object Object]
Phagocytosis (Endocytosis & Exocytosis) Endocytosis: uptake of membrane-bound particles.  Exocytosis: expulsion of membrane-bound particles.  High molecular weight drugs   or  Highly lipid insoluble drugs
Factors which influence the rate of absorption: – Routes of drug administration – The physicochemical properties of the drug – Dosage forms – Circulation at the site of absorption – Concentration of the drug
Routes of drug administration Enteral 	 via gastrointestinal tract (GIT). Oral  Sublingual Rectal  Parenteral administration = injections. Topical application Inhalation
Oral administration
First pass Metabolism Metabolism of drug in the gut wall or portal circulation before reaching systemic circulation So the amount reaching system circulation is less than the amount absorbed Where ? ,[object Object]
 Gut  wall
 Gut LumenResult ? ,[object Object]
 Short duration of action (t ½).,[object Object]
Dosage forms             Capsules             Tablets              Syrup             Suspension Hard- gelatin capsule Soft- gelatin capsule Tablets Spansule

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