PHARMACOLOGY I

PHA 2103

Dr.Taita T. Lee., M.P.S.,Bpharm-MUST.

OBJECTIVES
 By the end of this lecture, students should able to;
Define pharmacology, pharmacokinetics and
pharmacodynamics.
Describe the history of pharmacology.
Define the terms; drug, prodrug, prototype, placebo,
pharmaco-economics, and therapeutics.
Classify the routes of drug administration.
Discuss the advantages and disadvantages of the various
routes of drug administration.
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INTRODUCTION
 Pharmacology comes from two Greek words pharmacon
(meaning drug) and logos (meaning- discourse in/study).
 Pharmacology can therefore be defined as the science that
deals with the study of drugs and their interaction with living
systems.
Two major branches of Pharmacology:
 Pharmacokinetics (Greek: kinesis- movement)- refers to the
absorption, distribution, metabolism and excretion of drugs i.e.
what the body does to the drug.

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 Pharmacodynamics (Greek: dynamis- power)- refers to
molecular, biological and physiological effects of drugs,
including their mechanism of action at organ system or
subcellular or macromolecular levels i.e. what the drug does
to the body.

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HISTORY OF PHARMACOLOGY
 Man knew useful and toxic effects of many plant and animal
products even in ancient times.
 In ancient times, there was a close relationship between
religion and treatment of diseases i.e. the knowledge of use
of drugs often rested the holy man (priest).
 Cultures like Greek, Chinese, Indian, Persian, Roman and
others contributed a great deal to the development medicine
in early times. Drug prescriptions included preparations from
herbs, animals and minerals.

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 The earliest writings of drugs are the Egyptian medical papyrus
(1600 BC) and the largest of them known as Ebers papyrus
(1550 BC) lists some 800 preparations.
 Various traditional systems of medicine were practiced in
different parts of the world like Ayurveda, Homeopathy, Unani,
Siddha and Allopathy.
 Ayurveda – the science of life; Allopathy – the other suffering;
Homeopathy – similar suffering, ‘like cures like’ and ‘dilution
increases potency of drugs’.

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 By the 17th century the importance of experimentation and
observation and scientific methods became more clear.
Development of other branches of science like botany,
zoology, chemistry and physiology helped in better
understanding of pharmacology.
 The last century has seen rapid growth in pharmacology with
several new drugs. We now know more about receptors and
molecular mechanisms and most diseases are now curable.

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OTHER BRANCHES OF PHARMACOLOGY
Pharmacotherapeutics
 It is the application of pharmacological information together
with the knowledge of the disease for it’s prevention, mitigation
or cure.
Chemotherapy:
 It is the treatment of systemic infection/malignancy with
specific drugs that have selective toxicity for infecting organism
or malignant cell with no/minimal effects on the host cell.

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Pharmacy
 Is the art and science of analyzing, standardizing,
compounding and dispensing of drugs so as to make them fit
for administration to man or animals.

Toxicology
 It is the study of the poisonous effects of drugs and other
chemicals (household, environmental pollutant, industrial,
agricultural, homicidal) with emphasis on detection,
prevention and treatment of poisonings.

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Clinical Pharmacology
 It is the scientific study of drugs in man. It includes
pharmacodynamics and pharmacokinetic investigation in healthy
volunteers and in patients; evaluation of safety and efficacy of
drugs and comparative trials with other forms of treatment;
surveillance of patterns of use, adverse effects etc.

Pharmacogenonomics
 The science of understanding the correlation between an
individual patient’s genetic make-up (genotype) and their
response to drug treatment.
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TERMINOLOGIES
 Drug- “Any substance/product that is used or intended to be
used to modify/explore physiological systems or pathological
states for the benefit of the recipient”.-WHO.
or
It can also be defined as a substance or mixture of substances
used in the diagnosis, treatment, investigation or prevention of
disease or for modification of physiological function of humans
and animals and is incorporated in the official list.
Therapeutics
 It is the branch of medicine concerned with the cure of disease
or relief of symptoms.
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Prodrugs
 Compounds which on administration must undergo chemical
conversion by metabolic processes before becoming an active
pharmacological agent (drug). E.g. Methyldopa, an
antihypertensive, is first converted into α-methyl
norepinephrine to produce pharmacological effects.

Placebo
 It refers to inactive substance given to satisfy the patients
symbolic need (phychic need) for drug therapy and also used
in controlled studies to determine the safety (efficacy) of
medicinal substances.
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Prototype
 A prototype drug (lead agent) is an individual drug that
represents a class of drugs having similar chemical structures,
mechanism of action and mode of action and it is typically the
first developed drug within the class, and used as a reference for
assessing new drugs. E.g. propranolol is a prototype of beta
blockers.

Medicine
 It is a science and an art of maintenance of health and the
prevention and treatment of disease.
 Medicine can also refer to a substance or preparation used in
the prevention and treatment of disease.
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 Medicine can also refer to a discipline of study, e.g. Bachelor of
Medicine and Surgery.

Pharmacopoeia
 Is a book published by a recognized authority of any country
containing description of the chemical nature, molecular weight,
physical and chemical characteristics, solubility, chemical and assay
methods, standards of purity, storage conditions and dosage forms
of officially approved drugs in a country. E.g. British
pharmacopoeia (BP) , Indian pharmacopoeia (IP), European
Pharmacopoeia (EP) etc.

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Dose
 It refers to the quantity of a drug, or dosage form,
administered to a subject at a given time, e.g. the dose of
Aspirin ranges between 300 – 600mg.

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BRANCHES OF PHARMACOLOGY
 Pharmacokinetics.
 Pharmacodynamics.
 Pharmacotherapeutics.
 Pharmacognosy.
 Toxicology.
 Pharmacy.
 Chemotherapy.
 Pharmacogenetics.

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PHARMACOKINETICS
 Pharmacokinetics refers to the absorption, distribution,
metabolism (biotransformation), and elimination (ADME) of
drugs.
Most drugs :
enter the body (by mouth or injection or…) - must cross
barriers to entry (skin, gut wall, alveolar membrane…..)
are distributed by the blood to the site of action - intra- or
extra- cellular - cross barriers to distribution (capillaries, cell
wall….) - distribution affects concentration at site of action and
sites of excretion and biotransformation

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are biotransformed perhaps to several different compounds
by enzymes evolved to cope with natural materials - this may
increase, decrease or change drug actions
are excreted (by kidney or …….) which removes them
and/or their metabolites from the body.
Pharmacokinetics is the quantification of these
processes

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ROUTES OF DRUG ADMINISTRATRATION

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CLASSIFICATION OF ROUTES OF DRUG ADMINISTRATION
1. Local routes 2. Systemic routes
I. Topical route- skin surface, I. Oral.
oropharyngeal/nasal mucosa, II. Sublingual and buccal.
eyes, ear canal, vaginal and
anal canal. III. Rectal.
II. Deeper tissues IV. Transdermal.
Intra-articular injection. V. Inhalation.
Intrathecal injection. VI. Parenteral
Retrobulbar (behind the - IV
eyeball). - IM
III. Arterial supply - SC
Intra-arterial injection
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Factors determining choice of the route of
drug administration
 Condition of the patient (conscious, vomiting).
 Physicochemical properties of the drug (solid/liquid/gas,
solubility, pH, stability).
 Rapidity with which response is desired (routine/emergency).
 Accuracy of the dosage required (iv and inhalation can
provide fine tuning).
 Effect of digestive juices and first pass metabolism on the
drug.

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 Site of desired action i.e. localized and approachable or
generalized and unapproachable.
 Bioavailability from different routes.

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1. ENTERAL ROUTE (oral, sublingual)

 It is the safest and most common, convenient, and

economical method of drug administration.
 A drug may be swallowed allowing oral delivery or
administered sublingually (placed under the tongue) leading
to absorption into the blood stream.

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Advantages of oral route of drug administration
Simple, convenient.
Oral drugs are easily self-administered and, compared to drugs
given parenterally.
Have a low risk of systemic infections that could complicate
treatment.
Toxicities and overdose by the oral route may be overcome
with antidotes, such as activated charcoal.

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Disadvantages of the oral route

Limited absorption of some drugs.

Food may affect absorption.
Patient compliance is necessary.
Drugs may be metabolized before systemic absorption (first-
pass effect).
Limitations when patient is unconscious, vomiting or in pre-
/post-operative patients.

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Sublingual route
Drugs are placed under the tongue allows them to diffuse into
the capillary network. It has several advantages:
Rapid absorption.
Convenience of administration.
Low incidence of infection.
Bypass of the harsh gastrointestinal environment, and
avoidance of first-pass metabolism.

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Sublingual route

Advantages Disadvantages
Bypasses first-pass effect. Limited to certain types of
Bypasses destruction by drugs.
stomach acid. Limited to drugs that can be
Drug stability maintained taken in small doses.
because the pH of saliva
relatively neutral. May lose part of the drug dose if
swallowed.
May cause immediate
pharmacological effects.

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Parenteral route
Introduces drugs directly across the body’s barrier
defenses into the systemic circulation.
3 major parenteral routes:
 Intravenous (IV) route.
 Intramuscular (IM) route.
 Subcutaneous (SC) route.

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Intravenous (IV) route
 Most common parenteral route.
 Route of choice for drugs not absorbed orally e.g. atracurium
(neuromuscular blocker).
 A drug can be injected as a bolus where the full amount of a
drug is delivered to the systemic circulation almost
immediately or administered as an IV infusion over a longer
time, resulting in a decrease in the peak plasma
concentration and an increase in the time the drug is present
in the circulation.

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Advantages of the IV route
Can have immediate effects.
Ideal if dosed in large volumes.
Suitable for irritating substances and complex mixtures.
Valuable in emergency situations.
Dosage titration permissible.
Ideal for high-molecular-weight proteins and peptide drugs.

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Disadvantages of the IV route
Unsuitable for oily or poorly absorbed substances.
Bolus injection may result in adverse effects.
Most substances must be slowly injected.
Strict aseptic techniques needed.

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Intramuscular (IM) route
 Drugs administered via this route can be in aqueous
solutions, which are absorbed rapidly or in specialized
depot preparations, which are absorbed slowly.
 Depot preparations often consist of a suspension of
the drug in a non-aqueous vehicle such as
polyethylene glycol (PEG). As the vehicle diffuses out
of the muscle, the drug precipitates at the site of
injection.
 The drug then dissolves slowly, providing a sustained
dose over an extended period of time. Examples of
sustained-release drugs are haloperidol (neuroleptic)
and depot medroxyprogesterone (depo povera,
contraceptive).
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Advantages of IM route
Suitable if drug volume is moderate.
Suitable for oily vehicles and certain irritating substances.
Preferable to intravenous if patient must self administer.

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Disadvantages of IM route
Affects certain lab tests (creatine kinase).
Pain at the site of injection.
Can cause intramuscular hemorrhage.

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Subcutaneous (SC) route
 Like IM injection, requires absorption via simple diffusion and
is somewhat slower than the IV route.
 SC injection minimizes the risks of hemolysis or thrombosis
associated with IV injection and may provide constant, slow,
and sustained effects.
 This route should not be used with drugs that cause tissue
irritation, because severe pain and necrosis may occur.

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SC route.

Advantages Disadvantages
Suitable for slow-release drugs. Pain or necrosis if drug is
Ideal for some poorly soluble irritating.
suspensions. Unsuitable for drugs
administered in
large volumes.

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Transdermal route (Diffusion thru the
skin).
 Achieves systemic effects by application of drugs to the skin,
usually via a transdermal patch.
 The rate of absorption can vary markedly, depending on the
physical characteristics of the skin at the site of application as
well as the lipid solubility of the drug.
 Most often used for the sustained delivery of drugs, such as
the antianginal drug nitroglycerin, the antiemetic
scopolamine, and nicotine transdermal patches, which are
used to facilitate smoking cessation.

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Transdermal route

Advantages Disadvantages
Bypasses the first-pass effect. Some patients are allergic to
patches, which can cause irritation.
Convenient and painless.
Drug must be highly lipophilic.
Ideal for drugs that are
lipophilic, thus requiring May cause delayed delivery of drug
prolonged administration. to pharmacological site of action.
Ideal for drugs that are quickly Limited to drugs that can be
taken in small daily doses.
eliminated from the body.

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Rectal route
 50% of the drainage of the rectal region bypasses the portal
circulation, therefore, first-pass effect of drugs by the liver is
minimized with rectal administration.
Advantages
Disadvantages
 Partially bypasses first-pass effect.
 Drugs may irritate the rectal
 Bypasses destruction by stomach
mucosa.
acid.
 Not a well-accepted route.
 Ideal if drug causes vomiting.
 Ideal in patients who are vomiting,
or comatose.

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INHALATION ROUTE (oral & nasal)
a) Oral inhalation:
 Both oral and nasal inhalation routes provide rapid delivery of a
drug across the large surface area of the mucous membranes of
the respiratory tract and pulmonary epithelium, producing an
effect almost as rapidly as does IV injection.
 Used for drugs that are gases e.g. some anesthetics and those that
can be dispersed in an aerosol.
 Convenient for patients with respiratory complaints e.g. asthma or
chronic obstructive pulmonary disease, because the drug is
delivered directly to the site of action, thereby minimizing
systemic side effects.
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 Examples of drugs administered via oral inhalation include
bronchodilators, e.g. albuterol, and corticosteroids, such as
fluticasone.

b) Nasal inhalation:
 Involves administration of drugs directly into the nose.
 Agents include nasal decongestants e.g. oxymetazoline, and
anti-inflammatory corticosteroids such as mometasone
furoate. Desmopressin is administered intra-nasally in the
treatment of diabetes insipidus. Salmon calcitonin, a peptide
hormone used in the treatment of osteoporosis, is also available
as a nasal spray.

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Inhalation route
Advantages Disadvantages
Absorption is rapid; can have Most addictive route (drug can
immediate effects. enter the brain quickly).
Ideal for gases. Patient may have difficulty
Effective for patients with regulating dose.
respiratory problems. Some patients may have
Dose can be titrated. difficulty using inhalers.
Localized effect to target lungs:
lower doses used compared to that
with oral or parental administration.
Fewer systemic side effects.
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Intrathecal/intraventricular route.
 The blood-brain barrier and the blood-cerebrospinal
fluid (CSF) barrier often preclude or slow the
entrance of drugs into the CNS.
 Therefore, when local and rapid effects of drugs on
the meninges or cerebrospinal axis are desired, as in
spinal anesthesia or treatment of acute CNS
infections, drugs sometimes are injected directly into
the spinal subarachnoid space.
 E.g. intrathecal amphotericin B is used in treating
cryptococcal meningitis.

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Intra-articular Injection

Into Synovial Joint Fluid.

Local Effect.
Example- Cortisone, Antibiotic in
Rx of arthritis.

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Topical route
 Involves drugs are applied to the skin for local action as
ointment, powder paste, gel, cream etc.
 Drugs may also be applied in the mucous membranes as in
the eyes, ears and nose as ointments, drops and sprays.
 Used when a local effect of the drug is desired.
 E.g. clotrimazole is applied as a cream directly to the skin in
the treatment of dermatophytosis.

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Topical route

Advantages Disadvantages
May be adopted to provide a Some dosage forms used for topical
localized effect. administration require particular
patient advice to ensure safe and
When route used to provide appropriate drug administration.
systemic effect, first-pass effect is Local reactions may occur as side-
reduced. effects.
When systemic absorption is
required, lipid solubility of drugs is a
required characteristic.

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Vaginal route

Advantages Disadvantages
May be used to treat local Inconvenient and not well
infections. accepted by patients.
Allows for local application of
hormone replacement therapy.

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THE END