PL 309

General
Pharmacology
 Course Lecturers

• Prof. Dr. Safaa El Reweny

• Prof. Dr. Inas Darwish
• Dr. Mennatallah Ahmed Ismail (course
coordinator)- Office hours (C416):
Wednesday 12:30-2:30
 Course Teacher assistants and
Demonstrators
• Ph Fady Awad
• Ph Yara Samy
 Recommended Textbooks

• 1- Richard A. Harvey, Michelle A Clark,

Richard Finkel, Jose A. Rey, Karen
Whalen - Lippincott Williams & Wilkins
Illustrated Pharmacology 6th ed (2015)
• 2- Betram G. Katzung, Bertram
Katzung, Susan Masters, Anthony
Trevor - Basic and Clinical
Pharmacology 12th Ed (2011).
 Pharmacology I course

• This is the first of a series of courses

that are intended to cover the subject
of Pharmacology to Pharmacy
students.
• Prerequisite course: Physiology
(PL105)
 Pharmacology I course

• The aim of the course is to teach the students

the basic general principles of Pharmacology,
the pharmacology of the Autonomic Nervous
System (sympathetic and parasympathetic
nervous systems) and the pharmacology of
autacoids (local mediators)
• These are very essential in pharmaceutical
career and acquiring basic knowledge about
drugs used in various diseases
 Aim of the course

1-Explain the principles of pharmacodynamics.

2- Discuss the processes of drug absorption,
distribution, metabolism and excretion.
3- Discuss the pharmacology of the autonomic
nervous system (cholinomimetics, anticholinergics,
adrenergic agonists, sympatholytics and drugs
acting on autonomic ganglia).
4- Identify the pharmacology of autacoids
(histamine, serotonin, prostanoids, nitric oxide).
 Intended Learning Outcomes
of the course
A. Knowledge and Understanding
1- Define the terms "Pharmacology, pharmacokinetics pharmacdynamics, potency,
efficacy, second messengers, therapeutic index, agonists and antagonists.
2- Define the different sources of drugs, different routes of drug
administration,factors affecting the dosage of drug and its choice, different
mechanisms by which drugs can produce their effects&the pharmacokinetics of
drugs.
3- Define different types of pharmacokinetic and pharmacodynamic drug
interactions.
4- Identify the basic principles of the autonomic nervous system with emphasis on
the neurotransmitters, their receptors and the localization of those receptors and
the effects of their activation on different organs and tissues.
5- List the most important drugs which act on different types of adrenergic receptors
(activators and blockers), their pharmacokinetics and their effects on different
organs and tissues.
6- Describe the different chemical classes of autacoids, their localization, synthetic
and degradative pathways, physiological and pharmacological effects and clinical
significance.
 Intended Learning Outcomes
of the course
B- Intellectual Skills
1- Differentiate between pharmacokinetics & pharmacodynamics of drugs.
2- Compare between different processes by which drugs can pass across cell membranes.
3- Determine the concept of plasma steady state, compare between zero-order and first-order
kinetics&compare between phase I and phase II metabolic reactions.
4- Differentiate between different routes for drug excretion&distinguish between types of
adverse drug reactions.
5- Classify cholinergic receptors & drugs acting on them.
6- Differentiate between the antimuscarinic drugs (atropine & hyoscine) in pharmacological
actions, side effects and therapeutic uses.&differentiate between synthetic atropine substitutes.
7- Compare the different drugs in the classes of sympathomimetic and sympatholytic drugs as
to their side effects and therapeutic uses.
8- Differentiate between "autocrine", "paracrine" and "endocrine" control systems.&analyse the
physiological roles of different autacoids in health and disease.
9- Compare the nonsteroidal anti-inflammatory drugs in their mechanism of action, side effects
and toxicity &analyze the role of angiotensin II, bradykinin and nitric oxide in the control of blood
pressure.
10- Compare between different generations of antihistamines&compare between mechanisms
of drugs interfering with 5-HT.
 Intended Learning Outcomes
of the course
C. Professional Skills
1- Explain guidelines for animal experimentation and laboratory safety.
2- Construct plasma concentration-time curves for some drugs under different
conditions.
3- Infer the sleeping time in male and female rats to study the effect of gender on
drug metabolism.
4- Explain the effect of directly acting stimulant and depressant drugs and
autonomic drugs on intestinal contraction.
5- Perform experiments for the identification of an unknown stimulant drug using the
isolated toad’s intestine.
6- Explain the effect of some autonomic drugs using in-vivo experiments.
7- Construct a dose-response curve for acetylcholine using the isolated rectus
abdominis muscle of the frog.
8- Perform an experiment for the identification of an unknown drug acting on the
isolated rectus abdominis muscle of the frog.
9- Analyze the obtained data and tabulate the results.
 Intended Learning Outcomes
of the course

D. General Skills
1- Label scientific topics clearly
2- Qualify skills of communication
3- Qualify skills of planning, observation and organization
4- Qualify skills of working independently and in teams.
5- Qualify the ability to think critically and analytically.
 Course Assessment

• Total marks = 300

• Midterm written exam (10%) = 30 marks.
• Final written exam (50%) = 150 marks.
• Oral exam (10%) = 30 marls
• Practical exams, interactive learning &
assignments (30%)= 90 marks.
 Course Assessment
Grades:
The practical course is assigned 50 marks (out of 300).
20 marks interactive learning will take place in the
lectures and 20 marks assignments.

There will be continuous assessment on weekly basis

during the practical sessions. Students will be notified
about the timing of any exam
General Pharmacology
Introduction
 Introduction

Pharmacology is the science, which deals with the

effect of drugs on the body system.
It is the study of substances that interact with living
systems through chemical processes, especially by
binding to regulatory molecules and activating or
inhibiting normal body processes.
 Introduction

Main subdivisions:
A. Pharmacodynamics: which gives an
indication on what the drug does to the body.
B. Pharmacokinetics: which gives an information
on what the body does to the drug.
 Introduction

Pharmacogenomics (or pharmacogenetics) is the

study of the genetic variations that cause
differences in drug response among individuals or
populations.
 Introduction

The goal of drug therapy is to prevent, cure, or control

various disease states.

To interact chemically with its receptor, a drug molecule

must have the appropriate size, electrical charge, shape,
and atomic composition.
Furthermore, a drug is often administered at a location
distant from its intended site of action, therefore, a drug
must be transported from its site of administration to its site
of action. Finally, a practical drug should be inactivated or
excreted from the body at a reasonable rate so that its
actions will be of appropriate duration.
 Sources of the drugs
1. Natural:
a) Plant origin: eg. Atropine from belladonna & Morphine from
Opium.
b) Animal Origin: eg. Insulin, calcitonin, heparin etc.
2. Semisynthetic: these are compounds that are obtained from
natural source and subjected to chemical modification eg.Penicillins
and heroin (prepared by acetylation of morphine).

3. Purely synthetic: are purely chemically synthesized. eg. The

majority of drugs.

4. Mineral origin eg. Iodine, magnesium sulphate.

5. Genetic engineering:
a) Gene therapy.
b) Recombinant DNA as the production of human insulin from
bacterial origin.
 Pharmacokinetics

The onset of drug action, the

intensity of the drug's effect, and the
duration of drug action are controlled
by four fundamental pathways of drug
movement and modification in the body.
• Absorption
• Distribution
• Biotransformation (metabolism)
• Excretion of drugs
These determine the route of
administration for a specific drug, the
dose and frequency, and the duration of
the treatment.
 Routes of Administration

The route of administration is determined primarily by:

• The properties of the drug (for example, water or lipid
solubility, ionization, physical nature, etc.)
• The therapeutic objectives (for example, the desirability
of a rapid onset of action or the need for long-term
administration or restriction of delivery to a local site).
 Routes of Administration

There are two major routes of drug administration, enteral

and parenteral.
A. Enteral
1. Oral
2. Sublingual

B. Parenteral
1. Intravenous (IV)
2. Intramuscular (IM)
3. Subcutaneous (SC)
 Routes of Administration

C. Other
1. Inhalation
2. Intranasal
3. Intrathecal/ intraventricular
4. Topical
5. Transdermal
6. Rectal
 Enteral Route
1- Oral Administration

Drugs are swallowed orally for systemic

effect.
Advantages:
1. Highly acceptable as it is easily self-
administered.
2. Cheaper than other routes.
3. Prolongation of the drug action could
be possible by using extended-release
formulations (ER).
4. Toxicities or overdose by the oral route
may be overcome with antidotes such
as activated charcoal.
 1- Oral Administration
Disadvantages:
1. Unsuitable in emergencies.
2. Some drugs may be inactivated by gastric juice and
enzymes eg. insulin ; oxytocin
3. Some drugs could irritate the gastric mucosa e.g. aspirin.
N.B. Enteric coating of a drug protects it from the acidic
environment; the coating may prevent gastric irritation, and
depending on the formulation, the release of the drug may be
prolonged, producing a sustained-release effect
4. Some drugs are not absorbed by the GIT. eg.
Gentamicin, heparin.
5. Presence of food may hinder the absorption of the drug.
6. The tablet or capsule may be lodged in the esophagus.
7. Most drugs absorbed from the GI tract encounter first-
pass metabolism.
 First-pass Metabolism

Orally administered drugs

travel to the peripheral
venous circulation almost
exclusively by way of the
hepatic portal system. Thus
the absorbed drug is
exposed first to the liver &
may be extensively
metabolized. This
phenomenon is called the
‘FIRST – PASS EFFCT’
& can significantly decrease
systemic bioavailability.
 2- Sublingual/buccal Administration
Drugs are given sublingually or buccally.
Placement under the tongue allows a drug to diffuse into
the capillary network and, therefore, to enter the
systemic circulation directly.
Advantages:
1. Convenience of administration
2. Can produce rapid effect & with smaller doses because:
• Oral mucosa has a good blood supply.
• Not subjected to first by pass in the liver.
3. Not susceptible to inactivation in the GIT
4. Lower incidence of infection than parenteral
 2- Sublingual Administration

Disadvantages:
1. May be irritant to the mucus membrane.
2. Salivation may produce swallowing so losing the
advantage of this route.
3. Only suitable for a small number of drugs.
 Parenteral Route

The parenteral route introduces drugs directly into the

systemic circulation or other vascular tissue.
Parenteral administration is used for:
• Drugs that are poorly absorbed from the GI tract, e.g.
heparin
• Agents that are unstable in the GI tract, e.g. insulin
• Treatment of unconscious patients
In addition, these routes have the highest bioavailability and
are not subject to first-pass metabolism.

However, these routes are irreversible and may cause pain,

fear, local tissue damage and infections
 Parenteral Route
1- Intravenous (IV)
The drug is injected right into the venous
blood.
Advantages:
1. Immediate effect.
2. Suitable for drugs not absorbed by the gut.
3. Rapidly destroyed drugs, short t½ can be
infused continuously to provide a steady
state of plasma concentration
.
 Parenteral Route
1- Intravenous (IV)
Disadvantages :
1. Dangerous if given rapidly and cannot be
recalled by strategies such as emesis or by
binding to activated charcoal.
2. Prolonged infusion of irritant drugs lead to
venous thrombosis.
3. Susceptibility to infection if not using
aseptic conditions.
 Parenteral Route
2- Intramuscular (IM)
 Parenteral Route
2- Intramuscular (IM)
Injection is made into a large muscle
Advantages:
1. Reliable & produces more rapid
absorption than SC.
2. Could be used for irritant drugs.
3. Could be used for depot preparations (a
suspension of drug in a nonaqueous
vehicle such as polyethylene glycol) eg.
Long acting penicillins and
medroxyprogesterone
Disadvantages:
1. It is painful.
2. Not accepted as self-administration.
3. Risk of infection & formation of abscess.
 Parenteral Route
3- Subcutaneous ( SC)
• Suitable only for non irritant drugs to
avoid severe pain and necrosis.
• Large volume may be painful.
• Provides even & slow absorption to
obtain sustained drug effect eg.
Insulin.
• Vasoconstrictors such as
adrenaline greatly decrease the rate
of absorption.

4- Intradermal
5- Intrarterial
6- Intrathecal: amphotericin B is used
in treating cryptococcal meningitis. To avoid
the delay or the prevention of the drug
delivery to the CNS by the BBB
 Rectal Administration

• Used to produce
either systemic or
local effect.
• Suppositories or
enema are used.
 Rectal Administration

Advantages:
1. Ideal in unconscious pts.
2. Good for drugs with bad taste or smell.
3. Is not destructed of the drug by intestinal
enzymes or by low pH in the stomach.
4. Suitable in cases of vomiting.
5. Suitable for pts that cannot swallow.
6. Good for children.
7. Suppositories used for local effects.
 Rectal Administration

Disadvantages:
1. Irregular absorption (erratic and
incomplete)
2. Rectal inflammation or irritation may be
caused with repeated use.
 Topical Administration

• Is the application of the

drug on the body surfaces
e.g ointments, creams,
lotions powders, eye or ear
drops..etc.
• Topical application is used
when a local effect of the
drug is desired.
• Clotrimazole for the
treatment of fungal
infections
 Transdermal Delivery System (TDS )

• TDS is a method by which

the drug is released and
absorbed through the skin
for systemic absorption.

• Advantages:
1. Lead to more stable drug
level in the blood.
2. Avoid inactivation by first
hepatic bypass eg.
Nitroglycerine
3. Minimal side effects.
 Inhalational Administration

• Both oral and nasal

• Drugs given by this
method are in the form of
gases, aerosols &
powder.
• This method is used
when local (anti –
asthmatic) or systemic
(anesthesia) effect is
required.
 Inhalational Administration

Advantages:
1. Gaseous drugs can be rapidly taken up & eliminated.
2. Aerosols can produce high local concentration at the
site of application especially convenient for patients
with respiratory complaints.
3. Minimizing systemic effect when intended for local
action. eg. Corticosteroids
4. Easily administered eg. Aerosols.
 Inhalational Administration

Disadvantages:
1. Needs special apparatus and some patients have
difficulty regulating the dose.
2. Drugs may irritate the mucus membrane.
3. The presence of mucus plugs in the bronchi, for
example, hinders treatment, if used in bronchial
asthma.
4. Most addictive route (drug can enter the brain quickly)