GENERAL PHARMACOLOGY (Basic principles of pharmacology) Dhanasekaran Thangavel M.Pharm AUCMS 1. Pharmacological definitions 1.

Pharmacology: The science that deals with the origin, nature, chemistry, effects and uses of drugs, including pharmacognosy, pharmacokinetics, pharmacodynamics, pharmacotherapeutics and toxicology (From Greek pharmakon- drug and logia- study of) cont--2. Drug: A chemical substance of known structure, ( Other than a nutrient or an essential dietary ingredient) is used in the diagnosis, treatment, or prevention of disease or other than abnormal condition. Which is administered to a living organism for biological effect. cont--3.Phrmacokinetics: What the body does to the drug. The action of drugs in the body over a period of time, including the process of absorption, distribution, metabolism and excretion. cont--4. Pharmacodynamic: What the drug does to the body. The study of the biochemical and physiological effects of drugs on the body or on microorganisms or parasites within or on the body and the mechanisms of drug action and the relationship between drug concentration and effect. L+R = L . R where L=ligand (drug), R=receptor (attachment site)

cont--5. Distribution phase The phase (stage or period) of drug movement from the site of administration into the tissues 6. Elimination phase The phase of drug inactivation or removal from the body by metabolism or excretion cont--7.Endocytosis Absorption of materials across a cell membrane by phagocytosis and pinocytosis.

8.Zero-order elimination A constant amount of the drug is eliminated per unit time. 9.First order elimination A constant fraction of the drug is eliminated per unit time.

cont--10. Pharmacy The branch of the health sciences dealing with the preparation, storage, dispensing and proper utilization of drugs 11.Pharmacognocy The branch of pharmacology dealing with natural drugs and their constituents cont--12. Biotechnology. Biotechnology is the use of biological processes, organisms, or systems to manufacture products ( therapeutic proteins, diagnostics, genotyping, production of transgenic animals) intended to improve the quality of human life. cont--13. Pharmacogenetics. The study of genetic influences on responses to drugs (idiosyncratic drug reactions). or The study of the relationship between genetic (genes) factors and the nature of responses to drugs. cont--14. Pharmacogenomics The branch of pharmacology which deals with the influence of genetic variation on drug response in patients. 15. Genome: All of the genetic information, the entire genetic complement, all of the hereditary material possessed by an organism. cont--16. Pharmacoepidemiology. The study of drug effects at the population level. 17. Pharmacoeconomics. The branch of health economics aims to quantify in economic terms the cost and benefit of drugs used therapeutically. cont--18.Medical pharmacology The branch of pharmacology concerned with the use of chemicals in the prevention, diagnosis and treatment of disease especially in humans cont---

19. Toxicology The branch of pharmacology concerned with the undesirable effects of chemicals on biologic systems. 20. Chemotherapy Treatment of disease with a chemical agents 21. Pharmacotherapy Treatment of disease with medicines cont--22. Pharmacopeia A book containing an authoritative treatise (dissertation or discourse) on drugs and their preparations with descriptions, recipes(procedure or technique), strengths, standards of purity, and dosage forms for selected drugs.

cont--23. Formulary A collection of recipes, formulas and prescriptions 24. Absorption This is the movement of a drug from its site of administration into the blood 25. Bioavailability A fraction of an administered dose of unchanged drug that reaches the systemic circulation or target tissue

cont--26.Bioequivalence The relationship between two preparations of the same drug in the same dosage form that have a similar bioavailability 27. First pass effect or metabolism This is a phenomenon of drug metabolism, whereby the concentration of a drug is greatly reduced before it reaches the systemic circulation cont--28. Metabolism (from Greek"metabole- change or metabolismos- out throw) This is the set of chemical reactions that happen in living organisms to sustain life. These processes allow organisms to grow and reproduce, maintain their structures and respond to their environments. cont--Metabolism is usually divided into two categories. i)Catabolism breaks down organic matter, for example to harvest energy in cellular respiration. ii) Anabolism uses energy to construct components of cells such as proteins and nucleic acids

cont--29. Diffusion- wide spread 30.Passive diffusion The diffusion caused by neither spontaneous nor active process (not produced by active efforts) 31. Receptor A molecule on the surface or within a cell that recognizes and binds with specific molecules and producing a specific effect in the cell e.g., the cell-surface receptors for antigens or cytoplasmic receptors for steroid hormones. cont--32. Prescription A written directive for the preparation and administration of a remedy Inscription-part of a prescription containing the names and amount of the ingredients Subscription-part of a prescription giving directions for compounding the ingredients cont--Superscription-the heading of the prescription,i.e,the symbol R or the word receipe,meaning take Signature- permission to take the medicine from doctor 2. Drug Nomenclature A drug generally has three categories of names a) Chemical name -International Union of Pure and Applied Chemistry (IUPAC) name used most frequently in worldwide. - This is not suitable for use in prescription cont--b) Nonproprietary Name or Generic name An International Nonproprietary Name (INN, also known as recommended International Nonproprietary Name (rINN) or proposed International Nonproprietary Name (pINN) is the official nonproprietary or generic name, which has given to a pharmaceutical substance by the World Health Organization (WHO). - Generic drugs are labeled with the name of the manufacturer with nonproprietary name. cont---A generic drug must contain the same active ingredients like branded drugs

-According to the U.S. Food and Drug Administration (FDA), generic drugs should meet out all pharmacokinetic, pharmacological and pharmaceutical parameters like branded drugs

Prescription may be issued only with generic name rather than a manufacturer's name - These drugs can be marketed under its generic name without advertising.

cont--c) Proprietary or brand name

It is assigned by manufacturers as their property or trademark - One drug may have multiple proprietary names e.g, panadol, uphamol, para, paramax for paracetamol from different manufacturers Even same manufacturer may market the same drug under different brand names in different countries - This can be used in the prescription 3. Essential Drugs Concept The WHO has defined essential drugs as those that satisfy the priority healthcare needs of the population

These drugs are selected with due record to public health relevance, evidence on efficacy and safety and comparative cost effectiveness. cont--These drugs must be available at all times with - adequate amounts - appropriate dosage forms - assured quality - adequate information - a price the individual and community can afford Orphan drugs

These are drugs for diagnosis/treatment /prevention of a rare disease (orphan disease)or a more common disease (endemic in poor countries). 4. Routes of drug administration

-The choice of appropriate route depends both on drug as well as patient factors. - Mostly common sense considerations, feasibility and convenience dictate the route to be used Factors governing choice of route 1.Physical and chemical properties of the drug (solid/liquid/gas, solubility, stability,PH and irritability) 2. Site of desired action 3. Effect of digestive juices and first pass metabolism cont--4. Routine treatment or emergency 5. Accuracy of dosage required 6. Conditions of the patient (Unconsciousness and vomiting) a) Local Routes 1.Topical -External application of the drug for localized action - It is often more convenient for patients - Dosage forms: lotion, ointment, cream, powder, rinse, paints, drops, spray, lozenges, suppositories or pesseries, non absorbable drugs, inhalation of drugs, irrigating solutions/jellys.

note 1.Lotion:A liquid suspension, solution or emulsion for external application to the body Cont-2.Deeper tissues - Certain deep areas can be approached by using a syringe and needle - Systemic absorption is slow - e.g. intra- articular injection (Joint injection)-hydrocortisone acetate - intrathecal injection(Spinal canal) lidocaine - intrabulbar injection hydrocortisone acetate cont--3. Arterial supply - Close intra arterial injection in angiography - Anticancer drugs infused in femoral or brachial artery to localize the effect for limb malignancies 2. systemic routes The drug administered through systemic routes. 1.Oral -oldest and commonest mode of drug administration -It is safer, more convenient, does not need assistance, non-invasive, drug need not be sterile and cheaper with cost.

cont--2. Sublingual or buccal

The tablet or pellet containing the drug is placed under the tongue or crushed in the mouth

Only lipid soluble and non-irritating drugs can be administered - Can get rapid absorption and liver is bypassed -e.g. desamino-oxytocin cont--3.Rectal -Certain irritant and unpleasant drugs can be put in to rectum as suppositories or enema for systemic effect -Also used in patient having recurrent vomiting and unconsciousness -Bypass the liver -e.g. Diazepam cont--4. Cutaneous -Highly lipid soluble drugs can be applied over the skin for slow and prolonged absorption -The liver also bypassed -e.g. Transdermal devices cont--5.Inhalation -volatile liquids and gases are given by inhalation for systemic action (General anaesthetics) -The action is very rapid -Irritant vapours cause inflammation of respiratory tract and increase secretion cont--6. Nasal -The mucous membrane of the nose can readily absorb many drugs

The digestive juices and liver are bypassed E.g. Insulin

cont--7. Parenteral (Par-beyond, enteral-intestinal) -This refers to administration by injection which takes the drug directly into the tissues fluid or blood -This can be employed in unconsciousness, uncooperative or vomiting patient cont---

Subcutaneous a) Dermojet b) Pellet implantation c) Sialistic (nonbiodegradable) and biodegradable ii) Intramuscular iii)Intravenous iv) Intradermal injection