INTRODUCTION TO PHARMACOLOGY

PHARMACOLOGY
Pharmacology(Greek: Pharmacon-drug; poison in classic Greek; drug in modern
Greek and logos – discourse in) is a discipline that deals with the effects of drugs on
living system
•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.
•These substances may be chemicals administered to achieve a beneficial therapeutic
effect on some process within the patient or for their toxic effects on regulatory
processes in parasites infecting the patient.
Pharmacokinetics: (Greek: Kinesis-movement) the movement of the drug within the body. It
comprises the processes of absortption, distribution, metabolism and excretion. In a nut shell,
it means what the body does to the drug.
Pharmacodynamics: (Greek: dynamics-power) it is the study of drugs, the mechanism of
action, pharmacological actions and adverse effects. In summary, it covers all the aspects
relating to what the drug does to the body.
 Drug: WHO defines drug as “ any substance or product that is used or
intended to be used to modify or explore physiological systems or
pathological states for the benefit of the recipients.
•In the most general sense, a drug may be defined as any substance that
brings about a change in biologic function through its chemical actions. In
most cases, the drug molecule interacts as an agonist(activator) or
antagonist (inhibitor) with a specific molecule in the biologic system that
plays a regulatory role. This molecule is called a receptor
•Drugs may be synthesized within the body (e.g, hormones) or may be
chemicals not synthesized in the body (i.e, xenobiotics, from the Greek
xenos, meaning “stranger”).
Basics of Pharmacology
 History of Pharmacology
• Early in history a natural bond was formed between religion and use of drugs.
Priests, Shamans, Witches and holy persons were mediators between this
world and spiritual world. A concept then was prevalent that sickness is
caused by demons, and that these had to be cast out in order to restore health.
• In early periods religion dominated and divine intervention was called upon
for cure of ailments. As the knowledge of drugs and chemicals advanced the
divine intervention started to loose its importance and the treatment of disease
was taken over by the priests rather than gods. Advancement in the
knowledge of therapeutic value of natural products led to decrease in
dependence on supernatural powers and various gods.
• The priests gained experience by treating patients and the approach gradually
became more scientific. This was the foundation of practice of medicine and
use of drugs. Thus sequence of events started from magic to gods and priests
experience and culminated in scientific knowledge based on reasons and
logics
 Cultural Contribution
• The ancient Chinese wrote extensively on medical subjects as far as
2700 B.C. Egyptian medical papyri contain quite a number of
prescriptions. Greek observations on the medical effects, of various
natural substances are found in Thiad and Odyssey. The Greeks had
knowledge of toxic effects of drugs; they were interested in the poisonous
aspects of various plants. This led to the study of toxicological effects as
written by Plato which was an accurate description of the toxic properties
of the fruit of Hemlock, the sensory and motor nerve paralysis followed by
respiratory paralysis are the same as the actions of Conine a potent
alkaloid of hemlock.
• Almost parallel with old civilization Indian culture of Central and South
America developed drug usage. Indians treated patients with religious
rituals and herbal remedies, Rauwolfia serpentina was used to treat
insanity, and it was later that Vakil showed that it also had
antihypertensive properties.
• Early practitioners in Europe and America used herbs, plants, minerals,
even animals for medication, and often mixed them. The result of this at
times led to bad taste, smell and appearance, an attempt to make better
formulations led to the development of the field of pharmacy; which is
the science of preparing, compounding and dispensing medicines.
Galen floated the idea that he could combine different drugs to an
advantage for the patients; the term “galenicals” is based on that.
• The variation in the different effects of biological extracts was observed. It was
reasoned that to evaluate rational system of therapeutics, there had to be
standardization, uniformity and other aspects of medicinal agents.
• At the end of eighteenth century parallel development of disciplines of
Chemistry and Botany led to methods to isolate active principles from crude
drugs. For example Serturner purified morphine from Opium, quinine was
isolated from the tree of Cinchona bark. Other examples are strychnine from
Strychnos nuxvomica, emetine from Ipecachuana etc.
• Pharmacology became a separate and vital discipline, not only dealing with the
biological effects of chemical substances and their use, but also providing an
understanding between normal and abnormal human physiology through the
application of drugs as experimental tools.
 Branches of pharmacology
• Pharmacokinetics is the branch that deals with the routes of administration,
absorption, distribution, biotransformation, excretion and storage of drugs.
• Pharmacodynamics deals with the action of drugs that is the physiological
and biochemical changes brought about by drugs and deals with their
mechanism of action.
• Therapeutics is the branch which is concerned with the treatment of disease.
The various types of therapies are physiotherapy, psychotherapy,
pharmacotherapy & radiotherapy, etc.
• Pharmacotherapeutics is the branch of therapeutics that deals with the use
of drugs for treatment of disease.
• Toxicology is the discipline that deals with diagnosis, treatment and
prevention of the toxic effects of drugs and drug poisoning.
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•Experimental pharmacology is the branch of pharmacology that deals with
the effects of drugs in animals, human volunteers and living tissues.
•Clinical pharmacology deals with the use of drugs in patients. Measuring
the blood levels of drugs has important role in determining the dosage regimen
and the use of drugs in patients and individuals. It also includes the study of
side/undesirable toxic effects in patients and application of drugs in treatment
of disease. This field is gaining importance.
•Chemotherapy: it is the treatment of infectious diseases/cancer with
chemical compounds that have comparatively selective toxicity for infecting
organism or cancer cells
•There have been advancement in all scientific fields including pharmacology.
The advancements lead to new fields such as nuclear pharmacology, geriatric
pharmacology.
 Sources of drugs
Drugs can be obtained from: ­
– Natural sources.
– Prepared synthetically.
•Natural sources: ­
•Plant sources: - these can be the roots, stem, leaves, fruits and different seeds, e.g. atropine from root
of belladona, digoxin from leaf of digitalis, volatile oils from fruits and seeds.
•Animal sources: - e.g. insulin from cattle, cod liver oil from the fish cod and thyroxin from various
animal sources.
•Mineral sources: - e.g. iron, magnesium, calcium, etc.
•Synthetic sources are: ­
•These drugs are prepared in the laboratory, e-g Paracetamol, Cimetedine, and Pethidine. With the
advancement of research, most of the drugs used are synthetic in origin. Semi-synthetic, drugs are
prepared by altering the structure of drugs obtained from natural sources for e.g; Opioids. Semi-
synthetic penicillins, such as Ampicillin. Morphine derivatives such as Heroin.
 Classification of drugs
Drugs can be classified on different basis.
•Pharmacological effects and therapeutic uses, e.g.; analgesics,
antihypertensives, anaesthetics, diuretics, oxytocics, antibiotics etc.
•Based on mechanism of action at cellular level. e.g.; Enzyme inhibitors, ACE
inhibitors (captopril), carbonic anhydrase inhibitors (acetazolamide).
•Enhancing or blocking effects of neurotransmitters and mediators. e.g.; anti­
cholinesterases, dopaminergic drugs, Beta-blockers.
•Based on physiological effects. e.g.; vasodilators(sodium nitroprusside),
bronchodilators(aminophylline), anticoagulants(heparin).
•Drugs could be classified according to structure and molecular configuration,
such as alkaloids, anti histaminic, anti serotonin.
•According to the site of action, e.g.; loop diuretics, vasodilators.
•Another mode of classification, which is generally applied in teaching schedules,
is based on various systems of the body e.g., Drugs acting on Autonomic nervous
system. Drugs acting on Central Nervous system.
 Nomenclature of drugs
The names of drugs can be:
•Chemical, based on chemical formula.
•Generic, based on pharmacological action.
•Proprietary names. These are names given by a pharmaceutical company
and are commercial preparations.
 General Principles Of Pharmacology
• The Nature of Drugs: To interact chemically with its receptor, a drug molecule must
have the appropriate size, electrical charge and shape. A useful drug must have the
necessary properties to be transported from its site of administration to its site of action
• The Physical Nature of Drugs: Drugs may be solid at room temperature (eg, aspirin,
atropine), liquid (e.g, nicotine, ethanol), or gaseous (eg, nitrous oxide). These factors
often determine the best route of administration. A number of useful or dangerous
drugs are inorganic elements, eg, lithium, iron, and heavy metals. Many organic drugs
are weak acids or bases
• Drug Size: To have a good “fit” to only one type of receptor, a drug molecule must
be sufficiently unique in shape, charge, and other properties, to prevent its binding to
other receptors. To achieve such selective binding, it appears that a molecule should in
most cases be at least 100 MW units in size. Drugs much larger than MW 1000 do not
diffuse readily between compartments of the body. Therefore, very large drugs (usually
proteins) must often be administered directly into the compartment where they have
their effect
• Drug Reactivity and Drug-Receptor Bonds: Drugs interact with receptors by means of chemical
forces or bonds. These are of three major types: covalent, electrostatic and hydrophobic.
Electrostatic bonding is much more common than covalent bonding in drug-receptor interactions.
Thus, if we wished to design a highly selective short acting drug for a particular receptor, we would
avoid highly reactive molecules that form covalent bonds
• Drug Shape: The drug’s shape is complementary to that of the receptor site in the same way that a
key is complementary to a lock. Furthermore, the phenomenon of chirality (stereoisomerism) is so
common in biology that more than half of all useful drugs are chiral molecules; that is, they can exist
as enantiomeric pairs.
• Rational Drug Design: Rational design of drugs implies the ability to predict the appropriate
molecular structure of a drug on the basis of information about its biologic receptor. Previously,
drugs were developed through random testing of chemicals or modification of drugs already known
to have some effect. However, the characterization of many receptors during the past three decades
has changed this picture. Computer programs are now available that can optimize drug structures to
fit known receptors. As more becomes known about receptor structure, rational drug design will
become more common.