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WELCOME TO
DEPARTMENT OF
PHARMACOLOGY,
NEIGRIHMS
Dr. D. K. Br ahma MD (Phar ma)
Asstt. Pr ofessor and in-char ge
Depar tme...
PHARMACOLOGY

AN INTRODUCTION
History
Pioneers of Medicine and
Pharmacology:
• Hippocrates (450 B.C.)
• Francois Magendie (1783 - 1855)
• Claude Bernerd...
What is Pharmacology ?
• From the Greek Pharmacon (drug), logos (a
discourse or treatise)
• Broadly defined as how chemica...
…contd.
• The medicinal/organic chemists may
create the candidate compound
(sometimes referred to as a new chemical
entity...
What is a Drug?
• French: Drogue – a dry herb
• A single active chemical entity present in a
medicine that is used for dia...
…contd.
• Pharmacology studies the effects of drugs
and how they exert their effects:

• Paracetamol can reduce body tempe...
Pharmacology is the unique
combination of several
Biomedical Sciences!
Ph
ys
iol
og
y

ch
o
Bi

try
is
em

Pharmacology
tr...
Recommended Text
Books
Text Book

Author

Edition

The Pharmacological
Basis of Therapeutics

Goodman
Gillman

11th
Editio...
Branches
of
Pharmacology

• TWO MAIN BRANCHES - Pharmacokinetics
& Pharmacodynamics
Pharmacokinetics:
(What Body does to D...
Relationship – Dynamics
and Kinetics
Dosage Regimen

Absorption
Distribution
Metabolism
Excretion

Pharmacokinetics

Conce...
Branches of
Pharmacology
Pharmacotherapeut
ics:
Use of Drugs for prevention
and cure of diseases –
clinical management of
...
Pharmacy and Clinical
Pharmacy
Definitions

• It is the art and science of compounding
and dispensing drugs or preparing
s...
Some Other Definitions
• Pharmacoepidemiology: Study of effect of
Drugs on populations
• Pharmacoeconomics: Study of cost
...
Definitions – contd.
• Chemotherapy: It is the branch of therapeutics
which is concerned with the effects of drugs upon
mi...
Definitions – contd.
• Pharmacopoeia: It is
an official code
containing a selected
list of the established
drugs and medic...
Definitions – contd.
• National Formulary: It is the book
published as product information on
drugs available to prescribe...
Definitions – contd.
• Martindale The Extra Pharmacopoeia: It is
a voluminous database published
periodically by The Pharm...
Essential Medicines
• WHO defines – “Essential Medicines are
those that satisfy the priority healthcare
needs of the popul...
Orphan Drugs
• These are the drugs or biological products
for diagnosis, prevention and treatment of
a rare disease or a m...
Drug Nomenclature
1. Chemical Name – Chemical name
and code name
• Describe substances chemically
• For example - paraacet...
Drug Nomenclature –
contd.
1. Chemical Name –
•
•

Describe substances chemically
For example - paraacetylaminophenol …!

...
Drug Nomenclature –
contd.
•

Chemical Name – “N-(4-Nitro-2phenoxyphenyl) methanesulfonamide”
[International union of Pure...
Drug Nomenclature –
New drug being
developed

1. Chemical Name or Code name
– RO 15-17288
2. Non-proprietary Name:
Flumaze...
Sources of Drugs
• Plant sources – Morphine, digoxin, quinine,
atropine, reserpine , vinca alkaloids and paclitaxel.
• Ani...
Plant Sources
• Alkaloids: Water soluble salts of water insoluble
nitrogenous compounds e.g. Atropine
• Glycosides: Ether-...
Opium Alkaloid
Extraction
Routes of Drug Administration
Choices of Routes of
Drugs
• Drugs may be acidic, basic, or neutral and come in
a variety of chemical forms such as small ...
Local Routes
1.

2.

3.

Topical – External application of the drug
to the surface for localized action, e.g.
lotion, oint...
Routes - Enemata
• Application of medicaments into rectum
• Two types:
• Evacuant enema: Mainly liquid form for
local acti...
Systemic Routes –
1.Oral (enteral)
ADVANTAGES:

DISADVANTAGES:

•
•

•

• Self medication
possible – no
assistance require...
Oral Route – contd.
• Enteric coated: with acetate-pthalate,
glutean and anionic polymers of
methacrylic acid and its este...
2. Sublingual
• Kept under the tongue or crushed and spread over
the buccal mucosa
• Advantages:
•
•
•
•

rapid absorption...
3. Rectal
• Irritant and unpleasant drugs as
suppositories or retention enema
• Can be used in presence of vomiting
and un...
4. Inhalation
• Very rapid absorption due to vast
surface area of lungs
• General anesthetics – gases and liquids
• Pressu...
5. Nasal
• Absorbed by mucous membrane
of the nose
• Hepatic first pass metabolism
and gastric juices are bypassed
(GnRH a...
6. Parenteral (Par –
beyond, enteral – intestine)
Advantages:

• Unconscious and
uncooperative patient
• In presence of vo...
Parenteral Route –
contd.
•
•
•
•
•
•

Intradermal
Subcutaneous
Intramuscular
Intravenous
Intrathecal
Intraperitoneal
Intradermal and
Subcutaneous
Intradermal:
BCG and sensitivity Tests
Subcutaneous:
• Non-irritant substances
• Small amount...
Intramuscular
• Soluble substances, mild
irritants, suspensions and
colloids
• Sites of Injection – buttock,
deltoid muscl...
Intravenous route
Advantages

Disadvantages

• Quick action – ideal for
emergency
• Desired concentration
can be obtained
...
Transcutaneous Routes
• Innunction: Nitroglycerin in angina pectoris
• Iontophoresis: Galvanic current is for penetration
...
Transcutaneous images

Inuncti
on

Transdermal
Dermojet
Special Drug Delivery
System
• Ocusert: Pilocarpine, progestsert
• Prodrug: Examples
• levodopa to dopamine
• Chlorampheni...
Remember
• Drug Nomenclature
• Sources of Drugs with examples of each
• Active pharmacological components of
plants
• Rout...
Thank You

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An Introduction to Pharmacology
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An Introduction to Pharmacology

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An Introductory lecture on General Pharmacology suitable for medical undergraduate students.

Published in: Health & Medicine, Business

An Introduction to Pharmacology

  1. 1. WELCOME TO DEPARTMENT OF PHARMACOLOGY, NEIGRIHMS Dr. D. K. Br ahma MD (Phar ma) Asstt. Pr ofessor and in-char ge Depar tment of Phar macology NEIGRIHMS
  2. 2. PHARMACOLOGY AN INTRODUCTION
  3. 3. History Pioneers of Medicine and Pharmacology: • Hippocrates (450 B.C.) • Francois Magendie (1783 - 1855) • Claude Bernerd (1813 - 1878) • Rudolf Buchheim (1820 to 1879)
  4. 4. What is Pharmacology ? • From the Greek Pharmacon (drug), logos (a discourse or treatise) • Broadly defined as how chemical agents affect living processes: • • • • • Hormones Neurotransmitters Growth factors Drugs (pharmaceuticals) Toxic agents in the environment
  5. 5. …contd. • The medicinal/organic chemists may create the candidate compound (sometimes referred to as a new chemical entity, (NCE), it is the pharmacologist who is responsible for testing it for pharmacological activity. • Ultimately will lead to the discovery of novel drugs for therapeutic intervention
  6. 6. What is a Drug? • French: Drogue – a dry herb • A single active chemical entity present in a medicine that is used for diagnosis, prevention and treatment of diseases • WHO – in 1966 – “ Drug is any substance or product which is used or intended to be used to modify or explore physiological systems or pathological states for the benefit of the recipient.” • Therapeutic or diagnostic or preventive benefits Must …
  7. 7. …contd. • Pharmacology studies the effects of drugs and how they exert their effects: • Paracetamol can reduce body temperature in case of fever by inhibiting an enzyme known as cyclooxygenase in CNS, which is responsible for the synthesis of a number of inflammatory mediators. • Penicillin cures certain bacterial infections by disrupting the synthesis of bacterial cell walls by inhibiting a key enzyme.
  8. 8. Pharmacology is the unique combination of several Biomedical Sciences! Ph ys iol og y ch o Bi try is em Pharmacology try s mi he C M ed ici n e
  9. 9. Recommended Text Books Text Book Author Edition The Pharmacological Basis of Therapeutics Goodman Gillman 11th Edition Basic and Clinical Pharmacology Bertram G Katzung 7th Edition Essentials of Medical Pharmacology K. D. Tripathi Pharmacology and Pharmacotherapeutics Satoskar and Bhandarkar 6th edition, 2008 20th Edition
  10. 10. Branches of Pharmacology • TWO MAIN BRANCHES - Pharmacokinetics & Pharmacodynamics Pharmacokinetics: (What Body does to Drugs?) • Study the FATE of drugs once ingested and the variability of drug response in varying patient population • Includes absorption, distribution, metabolism and excretion of Drugs Pharmacodynamics: (What Drugs do to the Body?) • Study the mechanisms by which Drugs act? • Also study endogenous agents
  11. 11. Relationship – Dynamics and Kinetics Dosage Regimen Absorption Distribution Metabolism Excretion Pharmacokinetics Concentration in Plasma Pharmacodynamics Concentration at the site of action Effect
  12. 12. Branches of Pharmacology Pharmacotherapeut ics: Use of Drugs for prevention and cure of diseases – clinical management of diseases
  13. 13. Pharmacy and Clinical Pharmacy Definitions • It is the art and science of compounding and dispensing drugs or preparing suitable dosage forms for administration of drugs in man and animals. It also includes identification, selection, collection, purification, isolation, standardization and quality control of medicinal substances. • Clinical pharmacy is a health science discipline in which pharmacists provide patient care that optimizes medication therapy and promotes health, wellness, and disease prevention
  14. 14. Some Other Definitions • Pharmacoepidemiology: Study of effect of Drugs on populations • Pharmacoeconomics: Study of cost effectiveness of drug treatment; the cost of medications is of worldwide concern, particularly among certain groups such as elderly and AIDS patients
  15. 15. Definitions – contd. • Chemotherapy: It is the branch of therapeutics which is concerned with the effects of drugs upon microorganisms and parasites, living or multiplying in a living organism. It also includes the drugs used in malignancy • Pharmacognosy: is the science of identification of drugs • Toxicology: is the science of poisons which includes detection and measurement of poisons as well as treatment of poisoning. Poisons are the substances causing harmful, dangerous or fatal symptoms in man and animals.
  16. 16. Definitions – contd. • Pharmacopoeia: It is an official code containing a selected list of the established drugs and medicinal preparations with descriptions of their physical properties and tests for their identity, purity and potency. Define the standards of preparations. Examples- BP, USP, IP an EP
  17. 17. Definitions – contd. • National Formulary: It is the book published as product information on drugs available to prescribers in respective countries Examples – National formulary – BNF by BMA and PSGB National Formulary of India is published by Govt. of India.
  18. 18. Definitions – contd. • Martindale The Extra Pharmacopoeia: It is a voluminous database published periodically by The Pharmaceutical Press for Council of Royal Pharmaceutical Society of Great Britain • It contains concise reports on action and uses of drugs available in most of the world.
  19. 19. Essential Medicines • WHO defines – “Essential Medicines are those that satisfy the priority healthcare needs of the population. Essential medicines are intended to be available within the context of functioning health systems at all times and in adequate amounts, in appropriate dosage forms, with assured quality and adequate information, and at a price the individual and the community can afford.” • 1977 – 1996 – 2003
  20. 20. Orphan Drugs • These are the drugs or biological products for diagnosis, prevention and treatment of a rare disease or a more common disease (endemic only in poor countries) for which there is no reasonable expectation that the cost of developing and marketing will be recovered from the sale of these medicines. • Examples: Rifabutin, Succimer, Fomepizole and liposomal amphotericin B etc.
  21. 21. Drug Nomenclature 1. Chemical Name – Chemical name and code name • Describe substances chemically • For example - paraacetylaminophenol 1. Non-proprietary Name – USAN, BAN, rINN, generic name. 2. Proprietary Name (Brand Name) Manufacturer
  22. 22. Drug Nomenclature – contd. 1. Chemical Name – • • Describe substances chemically For example - paraacetylaminophenol …! 1. Non-proprietary Name – (USAN and BAN) • PARACETAMOL 1. Proprietary Name – • Crocin, Calpol and …….. (Similarly for aspirin …..)
  23. 23. Drug Nomenclature – contd. • Chemical Name – “N-(4-Nitro-2phenoxyphenyl) methanesulfonamide” [International union of Pure and Applied chemistry (IUPAC)] • • Non-proprietary Name – Nimesulide Proprietary Name – Nise, Nimulid …. etc.
  24. 24. Drug Nomenclature – New drug being developed 1. Chemical Name or Code name – RO 15-17288 2. Non-proprietary Name: Flumazenil (BAN, USAN and rINN) – approved name/official name 3. Proprietary name: Anexate, Lanexat, Mazicon, Romazicon
  25. 25. Sources of Drugs • Plant sources – Morphine, digoxin, quinine, atropine, reserpine , vinca alkaloids and paclitaxel. • Animal sources – Insulin, Thyroid extract, heparin, gonadotrophins and antitoxic sera. • Minerals – Liquid paraffin, magnesium sulfate, magnesium trisilicate, ferrous sulfate and kaolin. • Micro – organisms – Bacteria and fungi – Penicillin, Streptomycin • Synthetic – Analgesics, hypnotics, anticancer drugs and antimicrobials • Genetic Engineering – Human insulin, growth hormone genes • Hybridoma technique – monoclonal antibodies origin
  26. 26. Plant Sources • Alkaloids: Water soluble salts of water insoluble nitrogenous compounds e.g. Atropine • Glycosides: Ether-like combination of sugar with other organic acids. Acid hydrolysis separates sugar from non-sugar moiety • Oils: Glycerides of oleic, palmitic or stearic acids • Fixed oils: Peanut oil, coconut oil and castor oil • Volatile oils: Peppermint oil, ginger, eucalyptus oil etc. • Resins: Oxidized or polymerized volatile oils • Oleoresins: Mixture of volatile oils and resins • Gums: Secretory products of plants
  27. 27. Opium Alkaloid Extraction
  28. 28. Routes of Drug Administration
  29. 29. Choices of Routes of Drugs • Drugs may be acidic, basic, or neutral and come in a variety of chemical forms such as small organic molecules, large polymers such as proteins, carbohydrates and other compounds with complex chemistries • Physical and chemical properties of drug – solid/gas/liquid or solubility, pH etc. • Site of desired action – localized or generalized • Effect of digestive juices and first pass metabolism of drug • Accuracy of dosage required • Condition of the patient – unconscious, vomiting etc.
  30. 30. Local Routes 1. 2. 3. Topical – External application of the drug to the surface for localized action, e.g. lotion, ointment, cream, powder, paints, and spray etc. Deeper tissues – Certain deep areas can be approached by syringe and needle, e.g. intra-articular, intra-medullarly, intralesional injection, intrathecal and infiltration Arterial supply – Closed intra arterial injection, e.g. angiography and anticancer drugs.
  31. 31. Routes - Enemata • Application of medicaments into rectum • Two types: • Evacuant enema: Mainly liquid form for local action e.g., soap water enema • Quantity of fluid 600 ml • Retention enema: Mainly solid form meant for systemic action e.g., prednisolone enema
  32. 32. Systemic Routes – 1.Oral (enteral) ADVANTAGES: DISADVANTAGES: • • • • Self medication possible – no assistance required • • Vast area of absorption Simplicity of procedure – no extra cost Slow in action and hence safe with some risky drugs Both solid and liquid dosage forms can be given • • • • • • Onset of action is tardy Irritant and unpalatable drugs cannot be administered Absorption is irregular with some drugs e.g. aminoglycosdes May induce nausea and vomiting Not useful in presence of vomiting and diarrhoea Can be destroyed by gastric juice – penicillin G, insulin Cannot be used in unconscious and uncooperative patient.
  33. 33. Oral Route – contd. • Enteric coated: with acetate-pthalate, glutean and anionic polymers of methacrylic acid and its esters. • To prevent gastric irritation and alteration of drug in stomach. • To achieve desired concentration of drug in small intestine • To retard the absorption of drug • Controlled release (CR): Timsules/Spansules • To provide uniform medication for prolonged period
  34. 34. 2. Sublingual • Kept under the tongue or crushed and spread over the buccal mucosa • Advantages: • • • • rapid absorption – action in 1 minute liver is bypassed – directly in systemic circulation can spit out the drug Unconscious patients • Disadvantages: • Only lipid soluble drugs • Uncooperative patients • Irritation of mucosa Drugs: GTN (Glyceryl trinitrate), Buprenorphine (Nifedepine)
  35. 35. 3. Rectal • Irritant and unpleasant drugs as suppositories or retention enema • Can be used in presence of vomiting and unconsciousness • Absorbed by external hemorrhoid veins – bypasses liver Drugs – Diazepam, Indomethacin and Aminophylline etc.
  36. 36. 4. Inhalation • Very rapid absorption due to vast surface area of lungs • General anesthetics – gases and liquids • Pressurized metered dose aerosols - MDI • Dry powder inhalation - Rotahalers
  37. 37. 5. Nasal • Absorbed by mucous membrane of the nose • Hepatic first pass metabolism and gastric juices are bypassed (GnRH agonists like Leuprolide, dDAVP and calcitonin)
  38. 38. 6. Parenteral (Par – beyond, enteral – intestine) Advantages: • Unconscious and uncooperative patient • In presence of vomiting and diarrhea • Irritant drugs • By pass alimentary juice and 1st pass metabolism • Rapid action and accuracy of dose Disadvantages: • Costly and painful • Self medication is difficult • Less safe and chance of infection • Injury to nerves and arteries • Risky
  39. 39. Parenteral Route – contd. • • • • • • Intradermal Subcutaneous Intramuscular Intravenous Intrathecal Intraperitoneal
  40. 40. Intradermal and Subcutaneous Intradermal: BCG and sensitivity Tests Subcutaneous: • Non-irritant substances • Small amount as less vascular • Self injection is possible • Avoid in shock • Repository depot preparations – aqueous suspensions Best example – Insulin Hypodermoclysis
  41. 41. Intramuscular • Soluble substances, mild irritants, suspensions and colloids • Sites of Injection – buttock, deltoid muscle • No IM injection to child before walking
  42. 42. Intravenous route Advantages Disadvantages • Quick action – ideal for emergency • Desired concentration can be obtained • No hepatic first pass metabolism • Can be used in unconscious and uncooperative patients • • • • • • Costly – special apparatus required Thrombophlebitis and local irritation Self medication not possible Action cannot be halted Extravasation may cause severe irritation Aseptic and antiseptic measures to be maintained
  43. 43. Transcutaneous Routes • Innunction: Nitroglycerin in angina pectoris • Iontophoresis: Galvanic current is for penetration of drugs to deeper tissues – anode and cathode iontophoresis e.g., salicylates • Jet injection: Painless injection – high velocity jet produced through a microfine orifice • Transdermal therapeutic system (Novel drug delivery): Examples – GTN, Nicotine and Estrdiol • Scopolamine patch • Implants: Biodegradable and non-biodegradable. Example - Norplants
  44. 44. Transcutaneous images Inuncti on Transdermal Dermojet
  45. 45. Special Drug Delivery System • Ocusert: Pilocarpine, progestsert • Prodrug: Examples • levodopa to dopamine • Chloramphenicol palmitate • Targeted delivery: Monoclonal antibodies • Liposomes: daunorubicin, doxorubicin nd amphotericin B etc.
  46. 46. Remember • Drug Nomenclature • Sources of Drugs with examples of each • Active pharmacological components of plants • Routes of administration of Drugs with examples • Advantages and Disadvantages of different routes • Special drug delivery systems
  47. 47. Thank You Montoux test

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