1st Lec Pharma

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Pharmacology

Dr. Yassir Al-Zubaidi 1st Lecture


Objectives:

❖Introduction to the general aspects of


pharmacology and principle of drug

❖Be familiar with the drug administration


and pharmacokinetic (absorption and
distribution)
Historical review

BABYLONIA
ANCIENT CHINA
The ancient man
learned from instinct,
from observation
of birds and beasts.
Hippocrates

Egypt: Imhotep

Father of Medicine 460 - 370 BC


Father of Modern Medicine

Avicenna
Galenus 980 –1037
Paracelsus
1493–1541 Swiss
129 –216 philosopher, physician, introduced chemistry
medical theory and practice Pharmacologist to medicine
Greek and scientist
in the Roman Empire

801–873 demonstrates the


application of mathematics to
medicine, particularly in the field
of pharmacology.
Introduction
❖The word pharmacology is derived
from the Greek words pharmacon
(drug or poison) and logos (science).

Pharmacology deals with the fate


and actions of drugs at various
levels (molecular, cellular,
organ, and whole body)
Introduction

➢ Pharmacology is the base of Pharmacotherapeutics


(the treatment of diseases with drugs). It overlaps extensively
with pharmacy (the science of drug production).

➢Drug: can be defined as a natural or synthetic substance


that can affect a function or a structure of a living body. It can
be used in diagnosing, treating, and/or preventing a disease
or discomfort situation.

Receptor: a specialized target macromolecule present on


the cell surface or within the cell.
Objectives of drug usage
1- To cure a disease as primary therapy such as
bacterial and parasitic infections.
2- To suppress disease or symptoms of diseases such
as hypertension and diabetes.
3- To prevent diseases such as vaccination.
Sources of drugs
1- Plants such as morphine and atropine.
2-Animals such as insulin and heparin from pork or beef.
3-Minerals such as iron and calcium salts.
4- Microorganisms such as antibiotics produced from yeast and
bacteria ( penicillin).
5-Synthetic: most drugs today are synthetic (chemical) such as
paracetamol.
6-Semisynthetic: They are partially synthetic and partially natural
such as heroin.
7- Genetic engineering technology: It is produced by the insertion
of the human gene in the plasmid of bacteria such as human insulin.
Classification of drugs according to
methods of their dispensing
1- Controlled drugs(CD)

They are regulated drugs because of their high potential


for abuse and addiction. For prescribing these drugs,
certain official forms are used. These drugs can be
classified according to their severity into three classes:

A- Class A e.g morphine and heroin


B- Class B e.g amphetamine and barbiturates
C- Class C e.g benzodiazepines
• When these drugs are prescribed to be taken at home,
the nurse provides patient and family education about
the drug.
2- Prescription Only Medicines (POM)
Drugs that are dispensed by prescription. Most drugs are
POM because many drugs are dangerous (have side effects
and interactions) and must be supervised by a doctor. e.g
hormones and antibiotics.

3- Over the counter drug (OTC)


They are available and you can buy them without a
prescription. They are safe and effective when you follow
the directions on the label. They can be used to relieve
annoying symptoms and to cure some diseases simply and
without the cost of seeing a doctor. e.g drugs for headaches,
colds, constipation, skin creams, ointments……etc.
Factors modifying drug action

The individual variation in drug response may be due to:

1-Body weight. Thin, or obese patients have to receive


special doses.
2- Age. Children have immature liver or kidneys, in old
patients, a disease in the liver or kidney may cause a delay in
absorption or metabolism.
3- Disease states. Kidney, liver, or heart diseases may affect
the distribution and absorption of the drug.
4- Immune factors. Some drugs cause hypersensitivity in
some patients.
Patients at particular risks

1- Children. Doses should be calculated by age, weight, or body


surface area by using specific rules.

2-Elderly. Doses should be reduced because these people may


have kidney or liver failure, in addition, they usually used more
than one drug.

3-Pregnant women. Most drugs should be avoided because of


their teratogenic or toxic effects on the fetus.

4- Breastfeeding. Some drugs pass into the milk, are ingested by


the baby, and may cause toxic effects on the baby.

5-Liver and kidney diseases. Certain drugs should be avoided and


some require dose reduction.
Subdivisions of Pharmacology

❖Pharmacokinetics
describes “what the body does to the drug.” This includes topics such as
absorption, distribution, metabolism, and excretion of drugs.

❖Pharmacodynamics
describes “what the drug does to the body.” Specifically, it deals with the
biochemical and physiological effects of drugs and their mechanisms of
action

❖Pharmacotherapeuties
describes the use of drugs for the prevention, diagnosis, and treatment
of disease.

❖Toxicology
describes the undesirable effects of therapeutic agents, poisons, and
pollutants on biologic systems.
❖ Pharmacokinetics

Pharmacokinetics describes actions of the


body on drugs, including the principles of drug

➢Absorption
➢Distribution
➢Biotransformation (metabolism)
➢Elimination (Excretion)
❖ Pharmacokinetics

➢Absorption

Absorption is the rate at which extent a drug


moves from its site of administration to the
bloodstream.
❖ Rate of absorption depends on:

1. Route of administration
The intravenous route is most effective.

2. Blood flow
Highly vascularized organs such as the small intestine have the greatest
absorbing ability

3. Surface area available


Absorption of a drug is directly proportional to the surface area available

4. Solubility of a drug
The ratio of hydrophilic to lipophilic properties (partition coefficient) that a drug
has will determine whether the drug an permeate cell membranes

5. Drug-drug interactions
When given in combination, drugs can either enhance or inhibit one another's
absorption
6. pH
A drug's acidity or alkalinity affects its charge, which affects absorption
Routes of drug administration

❖Alimentary
❖Parenteral
❖Inhalation
❖Topical
❖Transdermal
❖Alimentary (Gastrointestinal tract)

1. Oral
commonest route. Advantage compliance and the utilization of the
small intestine, which is specialized for absorption because of its large
surface area

2. Buccal (between gum and cheeks).


Advantage: Allows direct absorption into the venous circulation

3. Sublingual (under the tongue}


Nitroglycerin is often given by this route. Advantage: Allows the drug to
drain into the superior vena cava, thus bypassing hepatic first-pass
metabolism

4, Rectal (suppository)
Useful when the oral route is unavailable due to vomiting or loss of
consciousness. Advantage: Approximately 50% of drug absorbed from
the rectum will bypass the liver
❖Parenteral (injection)
1. Intravenous (IV)
direct injection into the vascular system, Advantage: Most
rapid and potent mode of administration, because 100% of
drug enters the circulation

2. Intramuscular (IM)
Advantages: Usually more rapid and complete absorption
than with oral Minimizes hazards of intravascular injection.

3. Subcutaneous
This route allows drugs such as insulin and heparin
to be absorbed slowly over a period of time

4. Intrathecal
Advantage: In cases of acute CNS infections or spinal anesthesia, drugs
can be more effective if injected directly into the spinal subarachnoid space.

5. Intraperitoneal (IP)
the injection of a substance into the peritoneum (body cavity)
❖Inhalation
Pulmonary agents (vaporization)

❖Topical
Usually for treatment of localized disease eye infection
and acne

❖Transdermal
For sustained release of a drug —for example nicotine
patches
Bioavailability

❖ Bioavailability is the rate and extent to which an


administered drug reaches the systemic circulation.

For example, if 100 mg of a drug is administered orally


and 70 mg is absorbed, the bioavailability is 70%.

❖ Determining bioavailability is important for


calculating drug dosages for non-intravenous routes
of administration.

Factors that influence bioavailability:

✓ First-pass hepatic metabolism: When a drug is absorbed from the GI


tract, it enters the portal circulation before entering the systemic
circulation. If the drug is rapidly metabolized in the liver during this initial
passage, the amount of unchanged drug entering the systemic circulation
is decreased. This is referred to as first-pass metabolism.
Bioavailability

✓ Solubility of the drug: Very hydrophilic and extremely lipophilic drugs


are poorly absorbed. The very hydrophilic drugs are unable to cross
lipid-rich cell membranes, and the extremely lipophilic drugs are totally
insoluble in aqueous body fluids and, therefore, cannot gain access to
the surface of cells.
• For a drug to be readily absorbed, it must be lipophilic, yet have some
solubility in aqueous solutions.

✓ Chemical instability: Some drugs, such as penicillin G, are unstable in


the pH of the gastric contents. Others, such as insulin, are destroyed in
the GI tract by degradative enzymes.

✓ Nature of the drug formulation: factors such as particle size, salt form,
crystal polymorphism, enteric coatings, and the presence of excipients
can influence the ease of dissolution and, therefore, alter the rate of
absorption.
➢Distribution

The process by which a drug leaves the bloodstream and enters the
cells of the tissues, biochemical mechanisms are drugs absorbed into
cells.

1. Passive diffusion
Controlled by a concentration gradient across a membrane, which
makes a drug move from an area of high concentration to one of
low concentration. It is the most common mode of drug transport

2. Transport by special carrier proteins


A form of passive diffusion that is facilitated by a carrier protein

3. Active transport
Transport against a concentration gradient. The energy comes from
the dephosphorylation of adenosine triphosphate,
Distribution depends on:

➢Blood flow

➢Capillary permeability
The structure of capillaries varies depending on the organ, for
example, in the brain the junction between cells is very tight. In the
liver and spleen, the junction between endothelial cells is wide, which
allows large molecules to pass through

➢Binding to plasma proteins


Such as albumin—This will limit access to cellular compartments

➢Drug structure
Small lipophilic molecules will be able to distribute to more
compartments than will large polar molecules
Reference to read

• Pharmacology for dentistry 2nd Edition


• Lippincott's Illustrated Reviews Pharmacology 7th
Edition
Thanks

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