1st Lec Pharma
1st Lec Pharma
1st Lec Pharma
BABYLONIA
ANCIENT CHINA
The ancient man
learned from instinct,
from observation
of birds and beasts.
Hippocrates
Egypt: Imhotep
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
❖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
➢Absorption
➢Distribution
➢Biotransformation (metabolism)
➢Elimination (Excretion)
❖ Pharmacokinetics
➢Absorption
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
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
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
✓ 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
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
➢Drug structure
Small lipophilic molecules will be able to distribute to more
compartments than will large polar molecules
Reference to read