General Pharmacology

PH 1.1

 Competancy :

Define and describe the principles of

pharmacology & pharmacotherapeutics
 Learning Objective

At the end of the class student should be able to

undesrstand :
Basic principles in pharmacology
Naming of drugs
Essential drug Concept
Rational use of medecines
Pharmacology is one of the
oldest branches of medicine
 Ancient Egyptians  Medieval physicians
treated diseases prescribed opium and
with frog’s bile, gold as well as herbs.
 Patients in the 1600s
sour milk, lizard’s
blood, etc. were advised to eat
soap to cure hematuria
 The ancient
and to drink mercury
Egyptians applied in beer to cure
moldly bread to intestinal worms.
abrasions.
Two main divisions of pharmacology
y
og
ol
ac Pharmacodynamics - What the drug
does to the body?
m
Pharmacokinetics - What the body
r does to the drug?
ha
P
 Definitions

• Therapeutics
• Toxicology
• Pharmacoeconomics
• Pharmacogenetics
• Pharmacoepidemelogy
• Pharmacovigilance
• Chemotherapy
Definitions
CLINICAL PHARMACOLOGY:
It is the scientific study of drugs in man.

Clinical trials:
1. Phase I------Healthy volunteers
2. Phase II-----Small group of patients
3. Phase III----Large group
4. Phase I V ----Post marketing
 Sources of information
of drugs

Journals Websites CME

Text Books Library
 Sources of Drug Information
1. Pharmacopoeias :
IP,BP, USP, JP
useful – drug manufacturers, regulatory
authorities.
Information – molecular weight, physical
& chemical properties, solubility, purity,
storage, dosage forms of approved drugs
 Formularies

Information- dose, dosage forms, indications, CI,

precautions, ADR etc. for available
drugs.
FDC included
Beneficiary- prescribers
WHO model- 2002
BNF, NFI
 Martindale

* Complete reliable reference book

*Published by Royal Pharmaceutical Society of
Great Britain
* Updated compilation of unbiased information
on medecines all over the world
* Pharmaceutical, pharmacological, therapeutic
information on drugs.
 NOMENCLATURE OF DRUGS

Chemical Name:
A chemical name to a substance is given by
International Union of Pure and Applied
Chemistry(IUPAC) . It is usually very long and not
suitable for prescription.

International Nonproprietary Name (INN):-

This is also called as the generic name. this can be
either proposed (pINN) or recommended (r INN) by
WHO.
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Approved Names:-
These are some locally approved names in UK(British
Approved Name- BAN and USA( United States
Aproved Name- USAN).

Proprietary Name:-
This is also called as the brand name or the trade
name. it is given by the pharmaceutical company.

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 NOMENCLATURE OF DRUGS

 Chemical Name:-
• Describes drug chemically: Acetyl salicylic acid
Isopropyl amino naphthyl oxy propan-2-ol =
Propranolol !

 Non Proprietary name: [Approved name]

• Name approved by scientific body
Acetaminophen or Paracetamol
Pethidine or Meperidine

 Brand name [Proprietary name] :

• Name given by Mfr.
Paracetamol-”Crocin”
Chemical Name:
A chemical name to a substance is given by International
Union of Pure and Applied Chemistry(IUPAC) . It is
usually very long and not suitable for prescription.

International Nonproprietary Name (INN):-

This is also called as the generic name. this can be either
proposed (pINN) or recommended (r INN) by WHO.

16
Approved Names:-
These are some locally approved names in UK(British
Approved Name- BAN and USA( United States
Aproved Name- USAN).

Proprietary Name:-
This is also called as the brand name or the trade
name. it is given by the pharmaceutical company.

17
Essential drug [Medicine] concept

 WHO defined essential drugs as those that satisfy the

healthcare needs of majoritiy of population; Should be
available at all times in adequate amounts and required
dosage forms

 National list of essential medicines-

 2015 , 376 medicines
 Medicines in NLEM are listed with reference to the levels of
healthcare, namely, Primary (P), Secondary (S) and Tertiary (T).
 209 medicine formulations - all levels of health care (P, S, T)
Essential drug [Medicine] concept

 115 medicine formulations for secondary and tertiary levels (S,

T) and
 79 medicine formulations for the tertiary level (T).
 The NLEM 2015 has been prepared adhering to the basic
principles of Efficacy, Safety, Cost-Effectiveness; consideration
of diseases as public health problems in India.
 The list could be called as a Best-Fit List.
NATURE AND SOURCES OF
DRUGS
Many of these old sources are
still in use today
 Foxglove plant  Digitalis comes from the
foxglove plant and is used in
the treatment of CHF

 Colchicine is the drug of

 Meadow flower choice for treatment of gout
Colchicum  Insulin is used today to treat
autumnale diabetes and is derived from
the pancreas of beef or pork
or may be synthetically
 Beefor pork produced as well
pancreas
Origination of Drugs
Animals

Plants

Synthetically produced in
the laboratory
Drugs Derived from Plants
 Ephedrine is present in the leaves of a bushy
shrub (species name Ephedra), which, when
burned were used by the ancient Chinese to treat
respiratory ailments. Today, it is a
bronchodilator.
 Many estrogen hormone replacement therapy
drugs are derived from yams.
 The belladonna plant – source of atropine, which
is still used to dilate the pupils.
Drugs Derived from Animals
 Thyroid supplement
tablets are derived from
dried thyroid gland
tissue taken from
animals.
 Premarin is derived
from a pregnant mares’
urine. Premarin is used
to relieve the symptoms
of menopause.
 PLANTS ???  they produce
 Morphine
 Digoxin
 Quinine
 Atropine
 ANIMALS ??
 They give
 Insulin
 Thyroid extracts
 Gonadotropins
 Anti-toxic sera.
 MICROORGANISMS ??
 Bacteria
 Fungi
They produce
Antimicrobials…
 MINERALS ???
 L iquid paraffin
 Magnesium sulfate
 Magnesium trisilicate
 Kaolin
 SYNTHETIC DRUGS
 Drugs manufactured through well established
scientific methods.
 Analgesic
 Antipsychotics
 Synthetic derivatives of plants like belladona etc.
 GENETIC ENGINEERING
 Recombinant DNA technology
 Insulin
 Growth hormone.
 Uses of drugs
 To cure diseases. This can be for primary therapy
(Eg in bacterial infections) or for auxilary therapy
(anaesthetics, ergometrine and oxytocin in
obstetrics)

 It can be used continuously or intermittently to

maintain health without attaining cure ie for
suppression of disease or symptoms eg in
hypertension, diabetes.

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 Uses of drugs
 For prevention of disease. This can be either for
primary prevention as with vaccines or secondary
prevention Eg Aspirin for MI

 For diagnosis of disease eg contrast media,

dexamethasone suppression test .

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33
Introduction - ROUTES

 Various routes

 Drug

 Patient

 Feasibility

 Convenience
Factors affecting:

 Physical/ chemical properties

 Site of desired action
 Rate and extent of absorption
 Effect of digestive juices
 First pass metabolism
 Accuracy of dosage req.
 Patient condition
 CHANNELS OF
DRUG
ADMINISTRATIO
N

ENTERA PARENTERA TOPICA

L L L
ENTERAL

ORAL

SUBLINGUAL

BUCCAL

RECTA
L
 ORAL
ROUTE
 Oral refers to
two methods of administration:
 applying topically to the mouth
 swallowing for absorption along the gastrointestinal
(GI) tract into systemic circulation

 po (from the Latin per os) is the abbreviation used

to indicate oral route of medication
administration
 ORAL

 Advantages
 Convenient - can be self- administered, pain free,
easy to take
 Absorption - takes place along the whole length of
the GI tract
 Cheap - compared to most other parenteral routes
ORAL
 Disadvantages
 Sometimes inefficient - only part of the drug may
be absorbed
 First-pass effect - drugs absorbed orally are
initially transported to the liver via the portal
vein
 irritation to gastric mucosa - nausea and
vomiting
 ORAL
 Disadvantages cont.
 destruction of drugs by gastric acid and
digestive juices
 effect too slow for emergencies

 unpleasant taste of some drugs

 unable to use in unconscious patient

First-pass Effect

The first-pass effect is the term used for the

hepatic metabolism of a pharmacological
agent when it is absorbed from the gut and
delivered to the liver via the portal
circulation. The greater the first-pass effect,
the less the agent will reach the systemic
circulation when the agent is administered
orally
First-pass Effect
Oral Dosage Forms
 Common dose forms for oral administration
 tablets
 capsules
 liquids
 solutions
 suspensions
 syrups
 elixirs
 SUBLINGUAL ROUTE
 Sublingual administration
is where the dosage form is
placed under the tongue
 rapidlyabsorbed by
sublingual mucosa
SUBLINGUAL ROUTE
12

ADVANTAGES
 ECONOMICAL
 QUICK TERMINATION
 FIRST-PASS AVOIDED
 DRUG ABSORPTION IS QUICK

DISADVANTAGES
 UNPALATABLE & BITTER DRUGS
 IRRITATION OF ORAL MUCOSA
 LARGE QUANTITIES NOT GIVEN
 FEW DRUGS ARE ABSORBED
 BUCCAL ROUTE
 Buccal
administration is
where the dosage
form is placed
between gums and
inner lining of the
cheek (buccal
pouch)
absorbed by
buccal mucosa
BUCCAL ROUTE
ADVANTAGES
– Avoid first pass effect
– Rapid absorption
– Drug stability

DISADVANTAGES
– Inconvenience
– advantages lost if
swallowed
– Small dose limit
 RECTAL
ROUTE
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ADVANTAGE By Suppository or
S USED IN CHILDREN


 LITTLE OR NO FIRST PASS EFFECT

 Enema
USED IN – E.g. aspirin,
theophylline,
VOMITING/ UNCONSCIOUS
HIGHER CON CENTRATIONS RAPIDLY ACHIE VED


DISADVANTA
chlorpromazine
GES
 INCONVENIENT
 ABSORPTION IS SLOW AND ERRATIC
 IRRITATION OR INFLAMMATION OF RECTAL
MUCOSA CAN OCCUR
 SYSTEMIC-PARENTERAL
 Parenteral administration is
injection or infusion by means of
a needle or catheter inserted into
the body
 The term parenteral comes from
Greek words
 para, meaning outside

 enteron, meaning the intestine

 This route of administration

bypasses the alimentary canal
 SYSTEMIC-PARENTERAL
 INJECTABLES
I. INTRAVENOUS
II. INTRAMUSCULAR
III. SUBCUTANEOUS
IV. INTRA-ARTERIAL
V. INTRA-
ARTICULAR
VI.
VII. INTRATHECAL
INTRADERMAL

 INHALATION - Absorption through the lungs

 INTRAVENOUS
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ADVANTAGES

 Bioavailability 100%
 DISADVANTAGES
 Desired blood concentrations
achieved  Irritation & cellulitis
 Large quantities  Thrombophelebitis
 Repeated injections not
 Vomiting & diarrhea
 Always feasible
 Emergency situations
 Less safe
 First pass avoided
 Technical assistance
 Gastric manupalation
avoided required
 Danger of infection

 Expensive
 Less convenient and
painful
 INTRAMUSULAR
19
ROUTE
ADVANTAGES

 ABSORPTION
REASONABLY UNIFORM
 RAPID ONSET OF
ACTION
 MILD IRRITANTS CAN BE DISADVANTAGE
GIVEN S
 FIRST PASS AVOIDED  ONLY UPTO 10ML DRUG
 GASTRIC FACTORS CAN GIVEN
BE AVOIDED  LOCAL PAIN AND

ABCESS
 EXPENSIVE

 INFECTION

 NERVE DAMAGE
SUBCUTANEOUS

 Injected under the skin.

 Absorption is slow, so action is prolonged.

IMPLANT :a tablet or porous capsule is inserted into

the loose tissues by incision of the skin, which is
then stiched up.
example : certain hormonal drugs
INTRA-ARTERIAL
 Rarely used
 Anticancer drugs are given for localized effects
 Drugs used for diagnosis of peripheral vascular
diseases
INTRA-ARTICULAR
 injections of antibiotics
and corticosteroids are
administered in
inflammed joined
cavities by experts.
example: hydrocortisone
in rheumatoid arthritis
INTRADERMAL
 drug is given within skin
layers (dermis)
 Painful
 Mainly used for testing
sensitivity to drugs.
e.g. penicillin, ATS (anti tetanus
serum)

INOCULATION :administration of
vaccine (like small pox
vaccine )
Topical Routes of Administration

 Topical administration is the application of a

drug directly to the surface of the skin
 Includes administration of drugs to any

mucous membrane
 eye – vagina
 nose – urethra
 ears – colon
 lungs
Topical Dosage Forms

Dose forms for topical administration include:

 Skin:

 creams • Eye or ear:

 ointments – solutions
 lotions – suspensions
 gels – ointments
 transdermal patches • Nose and lungs:
 disks – sprays and powders
Advantages and Disadvantages of the
Topical Route
 Local therapeutic effects
 Not well absorbed into the deeper layers of
the skin or mucous membrane
 lower risk of side effects
 Transdermal route offers steady level of drug in
the system
 sprays for inhalation through the
nose may be for local or systemic
effects
 Transdermal

absorption of drug through skin (systemic action)

i. stable blood levels
ii. no first pass metabolism
iii. drug must be potent or patch
becomes too large
 Route for administration
-Time until effect-

Intravenous 30-60 seconds

Intraosseous 30-60 seconds
Endotracheal 2-3 minutes
Inhalation 2-3 minutes
Sublingual 3-5 minutes
Intramuscular 10-20 minutes
Subcutaneous 15-30 minutes
Rectal 5-30 minutes
Ingestion 30-90 minutes
Transdermal (topical) variable (minutes to hours)
 SELECTION OF TE
ROUTE
The ROA is determined by :

 The physical characteristics of the drug

 The speed which the drug is absorbed

and/ or released
 The need to bypass hepatic metabolism

 To achieve high conc. At particular sites

 Accuracy of dosage

 Condition of the patient