LOM Pharmacology Notes

CHAPTER 2: PHARMACOLOGY

INTRODUCTION

Pharmacology is the science that deals with the study of drugs and
their interaction with the living systems. The word pharmacology is derived from
Greek word Pharmacon means drug and logos means study.

It also deals with the discovery, chemistry, composition,

identification, biological/physiological effects and uses and manufacture of drugs.

Pharmaceuticals are substances with medicinal properties that aim to

treat, cure, prevent, or recognise disease and relieve pain through their application.

SUBDIVISIONS

Pharmacology is a broad medical specialty and contains many sub divisions

of study such as
1. Behavioral pharmacology
2. Cardiovascular pharmacology
3. Biochemical and cellular Pharmacology
4. Chemotherapy
5. Clinical pharmacology
6. Endocrine Pharmacology
7. Neuropharmacology
8. Molecular pharmacology
9. Systems and integrative pharmacology
10. Toxicology
11. Veterinary pharmacology
12. Drug Discovery, Drug Development and Regulatory Affairs

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DRUGS

A drug is chemical /biological substance used in the treatment, cure,

prevention, or diagnosis of a disease or used to enhance physical or mental well-
being in living organisms.

NOMENCLATURE

1. Chemical name
It is given based on the drugs chemical composition and molecular
structure.
E.g.: (+/-) 2 (p-isobutylphneyl) proponic acids
2. Generic name (Non proprietary name) is the universally accepted name given by
the United States Adopted Name Council
E.g.: ibuprofen
3. Trade name (Brand name/ Proprietary name) is a registered trademark for a drug
and its use of the name is restricted by the drug owner.
E.g.: Mortin

PRINCIPLES
Pharmacologic principles are defined as an understanding of the
molecular mechanism of action of a drug and its dose-response characteristics
 DRUG ACTION
 DRUG EFFECT
 PHARMACOGNOSY

 DRUG ACTION
The action of a drug is the biochemical physiological mechanism by which the
chemical produces a response in living organisms
It is classified in to following way
1. Pharmaceutics is the study of how various drug types influence Pharmacokinetics
and pharmacodynamic activities. This includes disintegration and dissolution of
drugs.
2. Pharmacokinetics is the study of how the body breaks down a drug after it is
administered.
It includes the following steps
Absorption
Distribution

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Metabolism
Excretion /elimination
3. Pharmacodynamics is the study of how drugs act at target sites of action in the
body, i.e. the mechanism of drug action in living tissues

 DRUG EFFECT
Drug effect is the ability of the drug to produce the desired result. It
contains the following term
Pharmacotherapeutics is the study of the use of drugs and their clinical
indications to prevent and treat disease

 PHARMACOGNOSY

Pharmacognosy is the study of natural (plant & animal) drug sources

DRUG TARGETS
Drug targets are key molecules involved in a particular metabolic or signaling
pathway that is specific to a disease condition or pathology.
Important drug targets:
1. Enzymes – protein that act as catalysts.
2. Receptors – protein that are crucial for the body's communication process.
3. Carrier proteins – transport important polar molecules across the cell wall.
4. Structural proteins – include tubulin in humans, cellulose in plants and collagen in
animals.
5. Nucleic acids – targets for several important drugs, including various antimicrobial
and anticancer agents.
6. Lipids – cell membranes consist of phospholipids bilayer, which act as a
hydrophobic barrier
7. Carbohydrates – cell surface carbohydrates are promising drug targets.

DRUG TOXICITY

Drug toxicity may occur with over dosage of a medication,

accumulation of the drug in the body over time, or the inability of the patient's body to
eliminate the drug. This is the poisonous and potentially dangerous effect of some drugs.

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Idiosyncrasy - It is a genetically determined abnormal reaction to a drug. It is an

example of an unpredictable type of drug toxicity
Iatrogenic -Disorder can occur as a result of mistakes in drug use or of individual
sensitivity of a given agent.
Side effects – Side effects are unwanted effects of a drug that are extensions of
pharmacological effects and are seen with the therapeutic dose of the drug. They are
predictable, common and can occur in all people.
Contraindication –These are factors in a patient's condition that make the use of a drug
dangerous and ill advised.

ROUTES OF DRUG ADMINISTRATIONS

A drugs route of administration affects the rate and extent of

absorption of the drug.
The routes can be broadly divided in to
1.Enteral
2.Parenteral
3.Topical

Enteral
Drugs can be administered in the following ways:
A) Taken by mouth (orally) eg : Acetaminophen
B) Placed under the tongue (sublingually) eg: Nitroglycin
C) Through the rectum(rectally) or vagina (vaginally) eg: Progestin

Parenteral Route
Drug can be given by injecting in the following ways:
1. Intravenous – In to a vein
2.Intramuscular –In to a muscle
3.Subcutaneous-Beneath the skin
4.Intrathecal – In to the space around the spinal cord

Topical
Topically applied drugs can be given by the following methods:
1.Ocular route – Instilled in the eye e.g. betaxolol
2.Nasal route – Sprayed in to the nose and absorbed through the nasal membranes e.g.
calcitonin

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3.Inhalation in to the lungs – Usually through the mouth E.g. budamate

4.Cutaneously – Applied to the skin for local or body wide effect. E.g phenytoin
5.Trans dermal – deliverd through the skin by patch for a systemic effect.e.g.fentanyl
MAJOR CLASSIFICATION

 ANALGESICS
An analgesic a drug that lessens pain. Mild analgesics relieve mild to moderate
pain, such as myalgias, headaches, and toothaches. More potent analgesics are narcotics
or opioids, which are derived from opium. These drugs may induce stupor (a condition of
near-unconsciousness and reduced mental and physical activity). They are used only to
relieve severe pain because they may produce dependence.
Some non-narcotic analgesics reduce fever, pain, and inflammation and are used for
joint disorders , painful menstruation, and acutepain due to minor injuries or infection
These agents are not steroid hormones (such as cortisone) and are known as nonsteroidal
anti-inflammatory drugs

e.g
Narcotic NSAID’s
morphine diclofenac sodium (Voltaren)

tramadol (Ultram) ketorolac (Toradol)

.
 ANESTHETICS

Anesthetics are agents that bring about reversible loss of sensation. They may be
general or local.

 General anesthesia
General anesthetics are drugs that bring about reversible loss of sensation and
consciousness.
E.g. Diazepam, Nitrous oxide

 Local anesthesia
Local anesthetics are drugs that block nerve conduction when applied locally
to nerve tissue in appropriate concentrations. Their action completely reversible.
E.g. lignocaine

 ANTIBIOTICS

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An antibiotic is a chemical substance produced by a microorganism (bacterium,

yeast, or mold) that inhibits (bacteriostatic) or kills (bactericidal) bacteria, fungi, or
parasites The use of antibiotics (penicillin was first in general use in 1945) has made it
possible to cure many conditions such as pneumonia, urinary tract infection, and
streptococcal pharyngitis.

Caution about the use of antibiotics is warranted because they are powerful agents. Like
all drugs, they have side effects. Also, with indiscriminate use of antibiotics, bacteria and
fungi can develop resistance to a particular agent. Infections caused by these resistant
bacteria can spread and may be difficult or impossible to cure.

e.g. azithromycin (Zithromax)

clarithromycin (Biaxin)

 ANTICOAGULANTS
Anticoagulants prevent clotting (coagulation) of blood. They prevent formation of clots or
break up clots in blood vessels in conditions such as thrombosis and embolism. They also
are used to prevent coagulation in preserved blood used for transfusions. Heparin is a
natural anticoagulant. A more easily administered form of heparin called low-molecular-
weight heparin (Fragmin, Lovenox) is self-injected on a daily basis and requires no
monitoring of blood clotting ability, as is done with regular heparin.

 ANTIPLATELETS
Antiplatelet drugs reduce the tendency of platelets to stick together. Aspirin is an
example of an antiplatelet drug; daily aspirin prophylaxis is recommended for patients
with coronary artery disease and for those who have had heart attacks.
e.g. clopidogrel bisulfate

 ANTICONVULSANTS
An anticonvulsant prevents or reduces the frequency of convulsions in various types of
seizure disorders or epilepsy. Ideally, anticonvulsants depress abnormal spontaneous
activity of the brain arising from areas of scar or tumor, without affecting normal
brain function.
e.g. gabapentin (Neurontin)
 ANTIDEPRESSANTS
Antidepressants treat symptoms of depression. They can elevate mood, increase
physical activity and mental alertness, and improve appetite and sleep patterns. Many

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antidepressants also are mild sedatives and treat mild forms of depression associated
with anxiety.
e.g. escitalopram (Lexapro)

 ANTIDIABETICS
A substance that helps a person with diabetes control their level of glucose (sugar) in
the blood. Antidiabetic agents include insulin and the oral hypoglycemic agents.
E.g. glimepiride, metformin, Actrapid
Rapid-acting insulins start working in 15 to 30 minutes and last 3 to 5 hours. Short-
acting insulin begins working within 30 minutes to an hour and lasts 5 to 8 hours. Long-
acting insulins have a time to onset of 1 to 3 hours and last between 24 and 36 hours.

 ANTIHISTAMINES
Drugs that combat the histamine released during an allergic
reaction by blocking the action of the histamine on the tissue. Antihistamines do not
stop the formation of histamine nor do they stop the conflict between the IgE and
antigen. Therefore, antihistamines do not stop the allergic reaction but protect tissues
from some of its effects
e.g. Cetirizine (Zyrtec)
diphenhydramine (Benadryl)

 CARDIOVASCULAR DRUGS

 ANGIOTENSIN- CONVERTING ENZYME (ACE) INHIBITORS

Angiotensin-converting enzyme (ACE) inhibitors dilate
blood vessels to lower blood pressure, improve the performance of the heartand reduce
its workload. They preventthe conversion of angiotensin I into angiotensin II, which is a
powerful vasopressor (vasoconstrictor). ACE inhibitors reduce the risk of heart attack,
stroke, and death even if a patient is not hypertensive.
e.g. benazepril (Lotensin)
ramipril (Altace)

 ANTIARRHYTHMIC
Antiarrhythmics reverse abnormal heart rhythms. They
slow the response of heart muscle to nervous system stimulation or slow the rate
at which nervous system impulses are carried through the heart.

e.g. Amioadarone (Cordarone)

Procainamide(Procanbid)

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 CARDIOVASCULAR DRUGS

 BETA-BLOCKERS
Beta-blockers decrease muscular tone in blood vessels
(leading to vasodilation),slow heart rate, decrease output of the heart, and reduce blood
pressure by blocking the action of epinephrine at receptor sites in the heart muscle
and in blood vessels. Beta-blockers are prescribed for angina, hypertension,
arrhythmias (such as fibrillation), and prevention of a second heart attack.

e.g. Propranalol,acebutolol

 CALCIUMCHANNEL BLOCKERS
Calcium channel blockers dilate blood vessels and lower blood
pressure and are used to treat angina and arrhythmias. They inhibit the entry of calcium
(necessary for blood vessel contraction) into the muscles of the heart and blood vessels

e.g. verapamil,diltiazem

 CARDIOVASCULAR DRUGS

 DIURETICS
Diuretics reduce the volume of blood in the body by promoting the kidney to remove water
and salt through urine. They treat hypertension (high blood pressure) and congestive
heart failure.
E.g. chlorothiazide
metolazone

 ENDOCRINE DRUGS
Endocrine preparations act in much the same manner as the naturally occurring
(endogenous) hormones.

Androgens
Androgens normally made by the testes and adrenal glands, are used for male
hormone replacement and to treat endometriosis and anemia.

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E.g. fluoxymesterone (Halotestin)

methyltestosterone (Virilon)

Antiandrogens
Antiantrogens interfere with the production of androgens or with their
binding in tissues. They are prescribed for prostate cancer.

E.g. abiraterone (Zytiga)

flutamide (Eulexin)
goserelin (Zoladex)

 ENDOCRINE DRUGS

Estrogens
Estrogens are female hormones, normally produced by the ovaries,that are used
for symptoms associated with menopause (estrogen replacement therapy) and to prevent
postmenopausal osteoporosis.

E.g. estrogens (Premarin, Prempro)

Aromatase inhibitors
Aromatase inhibitors also reduce the amount of estrogen (estradiol)
in the blood and are effective against breast cancer.

E. g. anastrozole (Arimidex)
exemestane (Aromasin)

 ENDOCRINE DRUGS

Selective estrogen receptor modulators (SERMs)

Selective estrogen receptor modulators (SERMs) have estrogen-
like effects on bone (increase in bone density) and on lipid metabolism (decrease in
cholesterol levels). However, they lack estrogenic effects on uterus and breast tissue.
SERMs are used to treat postmenopausal osteoporosis and breast cancer.

E.g. Tamoxifen and raloxifene are SERMs.

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Progestins
Progestins are prescribed for abnormal uterine bleeding caused by hormonal
imbalance and, together with estrogen, in hormone replacement therapy and oral
contraceptives.

E.g. medroxyprogesterone acetate (Cycrin, Provera)

megestrol (Megace)

 ENDOCRINE DRUGS

Thyroid hormone
Thyroid hormone is administered when there is a low output of hormone
from the thyroid gland. Calcitonin (a thyroid hormone) is used to treat osteoporosis. It
increases calcium in the blood and promotes bone deposition.

E.g. calcitonin (Cibacalcin)

levothyroxine (Levothroid, Levoxyl, Synthroid)

Glucocorticoids (adrenal corticosteroids)

Glucocorticoids are prescribed for reduction of inflammation and a wide
range of other disorders, including arthritis, severe skin and allergic conditions,
respiratory and blood disorders, gastrointestinal ailments, and malignant conditions.

E.g. dexamethasone (Decadron)

prednisone (Deltasone)

 ENDOCRINE DRUGS

Parathyroid hormone (PTH)

A fragment of human parathyroid hormone (PTH) has been
approved for osteoporosis treatment. This agent stimulates new bone formation.

E.g. teriparatide (Forteo)

Growth hormone release–inhibiting factor

Growth hormone release–inhibiting factor (somatostatin) can be
manufactured and given to treat gastrointestinal symptoms associated with acromegaly
and other tumors. It inhibits the production of natural growth hormone.

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e.g. octreotide (Sandostatin)

 GASTROINTESTINAL DRUGS

Gastrointestinal drugs often are used to relieve uncomfortable and

potentially dangerous symptoms, rather than as cures for specific diseases.

Antacids neutralize the hydrochloric acid in the stomach to relieve symptoms of peptic
ulcer, esophagitis, and reflux.
E.g. aluminum and magnesium antacid (Gaviscon)

Antiulcer drugs block secretion of acid by cells in the lining of the stomach and are
prescribed for patients with gastric and duodenal ulcers and gastroesophageal reflux
disease (GERD).
E.g. omeprazole (Prilosec)

 GASTROINTESTINAL DRUGS

Antidiarrheal drugs relieve diarrhea and decrease the rapid movement (peristalsis) in the
muscular walls of the colon. Cathartics relieve constipation and promote defecation for
diagnostic and operative procedures and are used to treat disorders of the
gastrointestinal tract. Some cathartics increase the intestinal salt content to cause fluid
to fill the intestines; others increase the bulk of the feces to promote peristalsis.
Another type of cathartic lubricates the intestinal tract to produce soft stools. Laxatives
are mild cathartics, and purgatives are strong cathartics.
E.g. loperamide (Imodium)

Antiemetics relieve nausea and vomiting and overcome vertigo, dizziness, motion
sickness, and similar symptoms due to labyrinthitis
E.g. ondansetron (Zofran)

RESPIRATORY DRUGS

Bronchodilators open bronchial tubes and are administered by injection or aerosol inhalers.
E.g. epinephrine (Primatene), theophylline (Theo-Dar)

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Steroid drugs are inhaled or given intravenously and orally to reduce chronic inflammation
in respiratory passageways.
E.g. fluticasone propionate (Flovent), mometasone (Asmanex)
Leukotriene modifiers are recent additions to the anti-inflammatory therapy of asthma.
They prevent asthma attacks by blocking leukotriene (a bronchoconstrictor) from binding
to receptors in respiratory tissues.
E.g. dexamethasone (Decadron), methylprednisolone (Medrol)

 SEDATIVES – HYPNOTICS
A sedative is a drug that produces a calming or quietening
effect and reduces excitement. It may induce drowsiness. Hypnotics is a drug that induces
sleep resembling natural sleep.
E.g. Barbiturates and benzodiazepines

 STIMULANTS
Stimulants are drugs that act on the brain to speed up vital
processes (heart and respiration) in cases of shock and collapse. They also increase
alertness and inhibit hyperactive behavior in children. High doses can produce
restlessness, insomnia, and hypertension.

E.g. caffeine
dextroamphetamine sulfate (Dexedrine)

 TRANQUILIZERS
Tranquilizers are useful for controlling anxiety. Minor tranquilizers
(benzodiazepines) control minor symptoms of anxiety. Major tranquilizers (phenothiazines)
control more severe disturbances of behavior.

E.g. lorazepam (Ativan)

olanzapine (Zyprexa)

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