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BASIC PRINCIPLES IN

PHARMACOLOGY
Learning Objectives for the course
•Purpose
• This course aims to prepare students to understand the foundations
of pharmacology.

• It also provides concepts of toxicology and ways to diagnose forms


of poisoning in an individual and the environment. The students
shall be guided to identify and manage poisoning as well as to think
critically about ways of avoiding poisoning in the environment and
the general population.

GitauSC, PhD
Learning Objectives for the course
• Expected Learning Outcomes
1. Explain various terminologies used in pharmaceutical and medical
sciences
2. Discuss the pharmacodynamics, pharmacokinetic, ADR and interactions of
drugs acting on various systems
3. Explain the cellular and molecular mechanisms underlying adverse drug
reactions
4. Describe the various types of drug interactions
5. Define terms used in toxicology and diagnostics
6. Describe causes and mechanisms of various types of poisoning
7. Describe the clinical signs / symptoms, diagnosis and management of
various types of poisoning
8. Describe types of air pollutants, their causes, mechanism of action and
general management

GitauSC, PhD
Core Texts
1. D, Buxton L. Goodman & Gilman’s Manual of pharmacology and
Therapeutics. McGraw Hill Medical, USA.

2. Tripathi KD (2013). Essential of medical pharmacology 7th Ed.


Jaypee brothers’ medical publishers (P) Ltd.

3. Lippincott’s Illustrated Reviews: Pharmacology 6th edition.


Lippincott Williams and Wilkins
4. Casarret and Duoll’s Textbook Of Toxicology; The Basic Science
of Poisons 8th edition; Curtis D Klaassen and John B Watkins III
5. Oxford handbook of clinical medicine 9th edition eds : Murray
Longmore, Ian Wilkinson, Andrew Baldwin, Elizabeth Wallin;
Oxford University Press
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Lesson 1
Definition: Pharmacology,
Pharmacodynamics,
Pharmacokinetics,

Drug discovery
Therapeutic Goal of medicine

To achieve drug concentrations…


at the site of action (target tissue)…
that are sufficiently high enough…
to produce the intended effect…
without producing adverse drug reactions.
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What is pharmacology

Pharmacology is the branch of science


concerned with the study of drugs and
how they affect living organisms.
Pharmacology is the science of
drugs (Greek: Pharmacon—drug;
logos—discourse in)
 Scientific study of the interactions
between drugs and the body.
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What is drug?
 Drug (French: Drogue—a dry herb)

 The WHO (1966) has given a more comprehensive


definition—“Drug is any substance or product that is
used or is intended to be used to modify or explore
physiological systems or pathological states for the
benefit of the recipient.”

 A chemical which is utilized for the diagnosis,


prevention and cure of an unwanted health condition
(definition by FDA)

 Pharmacy and poison act ( KENYA):

 Drug-includes any medicine, medicinal preparation or therapeutic


substance GitauSC, PhD
What is Medicine?
 Pharmacy and poison act ( KENYA):

 Medicine-any medicament or curative or


preventive substance, whether proprietary
or in the form of a preparation

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Other terms
 Pharmacotherapeutics

 It is the application of pharmacological


information together with knowledge of the
disease for its prevention, mitigation or cure

 Selection of the most appropriate drug, dosage


and duration of treatment taking into account the
specific features of a patient are a part of
pharmacotherapeutics

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Other terms
 Clinical pharmacology
 Scientific study of drugs in man.

 Includes pharmacodynamic & pharmacokinetic


investigation in healthy volunteers & in patients;
evaluation of efficacy and safety of drugs and
comparative trials with other forms of treatment;
surveillance of patterns of drug use, adverse effects.

 Chemotherapy

 Treatment of systemic infection/malignancy with


specific drugs that have selective toxicity for the
infecting organism/ malignant cell with no/minimal
effects on the host cells
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Pharmacy
 It is the art & science of compounding & dispensing
drugs or preparing suitable dosage forms for
administration of drugs to man or animals.

 It includes collection, identification, purification,


isolation, synthesis, standardization & quality
control of medicinal substances. The large scale
manufacture of drugs is called Pharmaceutics. It is
primarily a technological science
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Toxicology

 It is the study of poisonous effect of drugs & other


chemicals (household, environmental pollutant,
industrial, agricultural, homicidal) with emphasis on
detection, prevention & treatment of poisonings.

 It also includes the study of adverse effects of drugs,


since the same substance can be a drug or a poison,
depending on the dose

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DRUG NOMENCLATURE
 A drug generally has three categories of names:
i. Chemical name: It describes the substance chemically,
e.g. 1-(Isopropylamino)-3-(1-naphthyloxy) propan-2-ol for
propranolol. This is cumbersome and not suitable for use in
prescribing. A code name, e.g. RO 15-1788 (later named
flumazenil) may be assigned by the manufacturer for
convenience & simplicity before an approved name is
coined.

ii. Non-proprietary name: It is the name accepted by a


competent scientific body/authority, e.g. the United States
Adopted Name (USAN) by the USAN council. Similarly,
there is the British Approved name (BAN) of a drug.
GitauSC, PhD
DRUG NOMENCLATURE
 A drug generally has three categories of names:

ii. Non-proprietary name:


 The nonproprietary names of newer drugs are kept
uniform by an agreement to use the Recommended
International Nonproprietary Name (rINN) in all
member countries of the WHO. The BAN of older
drugs as well has now been modified to be
commensurate with rINN.

 NB:

 Many older drugs still have more than one non-


proprietary names, e.g. ‘meperidine’ and ‘pethidine’
or ‘lidocaine’ and ‘lignocaine’ for the same drugs
GitauSC, PhD
DRUG NOMENCLATURE
 A drug generally has three categories of names:

ii. Non-proprietary name:

a) generic name is used in place of nonproprietary name

iii. Proprietary (Brand) name: It is the name assigned by the


manufacturer(s) and is his property or trade mark.

• There are many arguments for using the nonproprietary


name in prescribing: uniformity, convenience, economy
& better comprehension

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Naming of a Drug

HO NHCOCH3

Chemical : N-acetyl-p-amino-phenol
Generic : Paracetamol (BP)
Acetaminophen (USP)
Trade : Panadol (500)
Tylenol (300)
Calpol etc.

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Medicine vs. Drugs

medicines
common everyday chemicals

a variety of man-made or natural


illegal substances of abuse
environmental toxins.
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Source of drugs
Modern
 Active principles of natural products
 Artificial synthetics
interferon
─ Full synthetic
─ Semi synthetic
─ Biological engineering

Steroid nucleus

Willow bark aspirin Glucocorticoids


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Yam
vaccine
What do we must know

1. Drug action
2. Mechanism of action
3. Major adverse drug reaction
4. Clinically important pharmacokinetics
5. Clinical application

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Drug-Body Interaction

Pharmacokinetics
Drug Administration
Absorption
Drug in Tissues Drug Drug
of Distribution Concentration in Metabolism or
Systemic Excreted
Circulation
Distribution Elimination
Drug Concentration at
Site of Action

Pharmacodynamics
Pharmacological Effect

Clinical Response

Toxicity Efficacy
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Why do we need to know PK?

Optimize drug therapy to obtain a


predictable response!
1. Drug of choice
2. How much
3. How often
4. For how long

The dose makes medicine


–Paracelsus 1538
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Missions of pharmacology

1. Explore the pharmacokinetic and


pharmacodynamic features of drugs
2. Probe the mystery of life process
3. Find and develop new drugs

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A brief History of
Pharmacology
• The birth date of pharmacology is not as clear-cut

• History of Pharmacology, Knowledge of drugs & their use in


disease is as old as history of mankind

• Primitive men gathered the knowledge of healing & medicine


by observing the nature, noticing animals while ill & by
personal experiences after consuming certain herbs & berries
as remedies
GitauSC, PhD
A brief History of Pharmacology
• As old as the history of human being

• As old as the age of pain an sufferings

• So, PAIN & sufferings were the 1st sensed alarm reactions that drew the
attention of human being

• Thus, surge was focused on how to combat with theseleading symptoms

• By experience, the analgesic power of certain plants was explored


accidentally first

• Hippocrates (460B.C.-377B.C. “The Father of Medicine” was the 1st to


attempt to separate the practice of medicine from religion & superstition ,
developed his pledge of proper conduct for doctors

GitauSC, PhD
A brief History of Pharmacology
• Ebers papyrus describes more than 700 drugs in extensive
pharmacopeia of that civilization. Included in this are: beer,
turpentine, berries, poppy, lead, salt & crushed precious stones
etc.(Egyptian remedies)
• Dhanvantari : an early Indian medical practitioner & one of the
world’s 1st surgeons., regarded as the source of Ayurveda. He
perfected many herbal based cures & natural remedies & was
credited with the discovery of the antiseptic properties of turmeric &
the preservative properties of salt which he incorporated in his cures.
• Susruta Ancient Hindu Medical Text Describes 760 herbs
• Charka Samhita describes more than 65O drugs of animal, plant &
mineral origins are used.
• Chinese remedies

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Some Historical landmarks
• Morphine : Friedrich Serturner (1805)
• Atropine : Grieger & Hessie (1833)
• Histamine : Vogt (1907)
• Sulfanilamide : P. Gleno (1908)
• Oxytocin : Abel (1919)
• Insulin: Banting & Best (1922)
• Penicillins : A. Flemming (1928)
• Sulfonamides : Domagk (1932)
• Cortisone: Edward C.Kendall
• Streptomycin : Waksman (1944)
• Chloramphenicol : Bartz (1948)
• Tetracycline: Duggar (1948)
• Lithium : Cade (1950)
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"I have been trying to point out that in our lives
chance may have an astonishing influence and, if I
may offer advice to the young laboratory worker, it
would be this - never to neglect an extraordinary
appearance or happening.”

Alexander Fleming

??? And/or comments

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Institute of Clinical Pharmacology

www.csupharmacol.com
GitauSC, PhD
Some Pharmacologists in History

• William Withering, 1741-1799 (digitalis)

• Claude Bernard 1813-1878 (d-tubo curare)

• Friedrich Sertürner 1783--1841 (morphine)

• Rudolf Buchheim 1820-1879 (1st Pharmacology Laboratory, University of


Dorpat (now Tartu, Estonia)

• Oswald Schmiedeberg 1838-1921 (Strassburg, now Strasbourg, trained many


pharmacologists)

• John Langley 1852--1926 (Receptor concept)

• Paul Ehrlich 1854-1915 (Receptor concept)

• Otto Loewi, Henry Dale (Neurotransmission)


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