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GENERAL PHARMACOLOGY
Chapter-1
Table 1.1: Classification of different animal products used as drug and surgicals.
Drug Category Animal source
Insulin Hormone Pancreas of beef or pig
Thyroid extract/thyroxine Hormone Thyroid gland
Shark liver oil Vitamin A Livers of shark and allied species
Cod liver oil Vitamin A and D Livers of Gadus species
Antisnake venom Immune serum Blood of horse
Hyaluronidase Enzyme Testis of bull
Pepsin Enzyme Stomach of beef and pig
Surgical ligatures and sutures Used in surgery Intestinal tissues, tendons of animals.
Administration of drug in the form of intestinal juice (alkaline) only, which is useful
liquid into the rectum is called enema, which in:
may be soap water or glycerine-vegetable oil. z Preventing gastric irritation and alteration
It is used to remove the faecal matter and of the drug in the stomach.
flatus and is used in constipation. Certain z To get the desired concentration of the
drugs are administered rectally for produc- drug in intestine, and
ing systemic effects also (e.g. aminophylline, z To delay the absorption of the drug.
indomethacin, paraldehyde etc.)
Time Release/Sustained Release Capsules
Systemic Routes
It is a useful solid dosage form of drug,
The drug administered through systemic where the particles of the drug dissolve at
routes (orally or parenterally), is absorbed different time intervals.
into the blood, distributed along through the The advantages of time-release prepara-
circulation and produce their desired effects. tions are:
Oral Route z Reduction in the frequency of administra-
tion of drug.
This is the most commonly used route for
z Maintenance of therapeutic effect for
drug administration. It is also the safest, most
convenient and economical. But, there are longer time.
some limitation of this route: z To some extent decreased incidence of
undesired effects.
z Drug action is slow, thus not suitable for
z Appropriate for drugs with short half
emergencies.
lives (less than 4 hours).
z Incapability to absorb some drugs, due
to their physical characteristics i.e. Sublingual Administration
polarity of the drug. The highly lipid soluble and nonirritating
z Unpalatable and other irritant drugs can drugs (i.e. nitroglycerine, isoprenaline,
not be administered. methyltestosterone) in the form of tablets or
z Can not be used for unconscious and pellet is placed under the tongue, where they
uncooperative patient. rapidly dissolve and are absorbed quickly in
the general circulation. The advantage of this
z May not be useful in the presence of
routes are:
vomiting and diarrhoea.
z Rapid onset of action.
z Drugs, which can be destroyed by
z The degradation and metabolism of the
digestive juices (i.e. insulin, penicillin G)
drugs in the stomach and liver is avoided
or in liver (i.e. testosterone, nitroglycer-
ine) can not be administered orally. Parenteral Routes
z The absorption of certain drugs is negli- (par = beyond, enteral = intestinal)
gible e.g., streptomycin. The administration of drugs by injection
Enteric Coated Tablets directly into the tissue fluid or blood without
having to cross the intestinal mucosa.
The drugs which are destroyed by the gastric
The advantages of parenteral routes are:
juices in the stomach, are coated with keratin,
shellac and cellulose acid phosphate. These z Rapid action of drug.
substances are not dissolved by the acid juice z Can be employed in unconscious/unco-
of the stomach, but are dissolved in the operative patients.
6 Essentials of Pharmacology
z Drugs, which are modified by alimentary The rate of absorption is reasonably uni-
juices and liver can be given by this route. form and the onset of action is rapid.
z Drugs, which are not absorbed in small Intravenous
intestine or irritate the stomach can be
The drug is injected as a bolus or infused
administered by this route.
slowly directly into a vein to produce rapid
Disadvantages are: action. It is also useful for certain irritant and
z Less safe, more expensive. hypertonic solutions, as they are rapidly
z Inconvenient (painful) for the patient. diluted by the blood. Drugs in an oily vehicle
z Self medication is difficult. or those which precipitate blood constituents
z Chances of local injury at the site of or haemolyze erythrocytes should not be
injection. given by this route.
The important parenteral routes are: Intravenous route is the most rapidly
effective and the desired blood concentration
Subcutaneous can be obtained with a definite dose but at
The non-irritant substances can be injected the same time it is the most dangerous route
by this route. The rate of absorption of drug of administration. For once the drug is
is constant and slow to provide a sustained injected there is no retreat. So, intravenous
effect. The site of injection is usually the outer injection must usually be performed slowly
surface of the arm, or front of the thigh. Self and with constant monitoring of the patient.
medication (e.g. insulin) is possible because This route is usually reserved for emergencies
deep penetration is not needed. Other drugs when a rapid action is required and infusion
which are administered subcutaneously are of large amounts of fluids to overcome dehy-
adrenaline, morphine and certain hormonal dration or to supply nutrition to patients who
preparations. can not take food/fluids orally.
The other related subcutaneous routes Intradermal
are dermojet (by which, drug is projected from
The drug is injected into the skin raising a
a microfine orifice using a high velocity jet)
bleb. This route is employed for vaccination
and pellet implantation (which provides sus-
e.g. BCG vaccine and for testing the sensi-
tained release of the drug over weeks and
tivity e.g. penicillin injection.
months e.g. testosterone).
Intra-arterial
Intramuscular
This route is useful in diagnostic studies, by
The soluble substances, mild irritants and
which arterial blood sample may be with-
suspensions can be injected by this route in drawn for blood gas studies. Certain cyto-
the large skeletal muscles (deltoid, triceps, toxic compounds are administered by intra-
gluteus maximus, rectus femoris etc.). These arterial perfusion in localised malignancies.
muscles are less richly supplied with sensory
nerves and are more vascular, so irritant Intrathecal or Intraspinal
solutions can be injected. Small volumes (up For local and rapid effect of drugs on the
to 2 ml) are injected into the deltoid muscle, meninges or cerebrospinal axis, drugs are
and small or large volumes (up to 10 ml) are injected directly into the spinal subarachnoid
injected into the gluteal mass. space. This is also used to produce spinal
General Action of Drugs 7
anaesthesia, or for introduction of a radio- stabilizers are used in the treatment and
opaque contrast-medium into the subarach- prophylaxis of bronchial asthma i.e. salbuta-
noid space for visualising the spinal cord. mol (ASTHALIN) and sodium cromoglycate
Intramedullary (FINTAL) inhaler.
By this method, the drug is introduced into
TARGETED DRUG DELIVERY SYSTEMS
the bone marrow of the sternum or tibia.
Blood is occasionally given by this route. The targeted drug delivery system have
Intracardiac recently been developed with the objective
of patient compliance, drug delivery at the
In sudden cardiac arrest and other cardiac site where it required and having prolonged
emergencies, the adrenaline is directly injec- duration or action. It includes:
ted into the heart by a long needle in the left
fourth intercostal space close to the sternum. Transdermal patches
Intraperitoneal They are adhesive patches in which drug is
incorporated into a polymer which is usually
This route is a common laboratory procedure,
polyisobutylene. The drug is observed
but it is seldom employed clinically in infants
through percentaneous circulation and
for giving fluids like glucose saline, as the
provide smooth plasma concentration for a
peritoneum offers a large surface for
larger period of time. Clinically used
absorption.
transdermal patches are of nitroglycrine,
Intra-articular scopolamine, estradiol, ketorolac and
Certain drugs (i.e. glucocorticoids) can be clonidine etc.
administered directly into a joint space for Ocuserts
the treatment of local condition i.e. rheuma-
These are very thin elliptical microunits
toid arthritis.
which contains the active drug in a reservoir
Inhalation Route form and the drug is released by diffusion
The volatile liquids and gases are given by through a membrane at a steady rate.
inhalation route. The drugs may be given as Example are pilocerpine ocusert in glaucoma.
solid particles, as nebulized particles from Progestaserts
solutions or in the form of vapours. The It is intrauterine contraceptive containing
volatile substances include gaseous anaes- progesterone and to be inserted into the
thetics, amyl nitrite and vapours of liquid uterus where it releases progesterone at a
anaesthetics, gases like oxygen, carbon constant role for a specific period of time.
dioxide and helium.
Nonvolatile substances have to be broken DOSAGE FORMS
down into small particles, and then inhaled A dosage form is a medicated product
as aerosols. specially designed for administration to the
Drugs given by this route are quickly patient for the diagnosis and treatment of
absorbed, which takes place from the vast disease.
surface of alveoli and produce rapid action. The dosage form is broadly divided into
Various bronchodilators and mast cell solid dosage form, liquid dosage form and
8 Essentials of Pharmacology
inhalation which are used both internally as agent and then moistened to produce a
well as externally. cohernt mass which is then passes through a
Solid and liquid dosage forms includes sieve to form a granule.Granules are the
capsules, granules, effervescent granules, unusual means of administering drug that
powders, drops, solutions, syrups, tinctures, possess an unpleasant taste. Example: PAS
applications, creams, enema gargles, jellies, (Para-amino salicyclic acid) granules.
liniments, lotions, mouth washes, ointments, Effervascent granules: It is a mixture of
paints, paste, poultices etc. citric and tartaric acids with sodium
Inhalation forms include aerosols, sprays biocarbonate and usually some sweatening
etc. agents(saccharin or glucose) may be added.
The powder granules should be dissolved
DOSAGE FORMS AND ROUTES OF DRUG with a prescribed amount of water and taken
ADMINISTRATION when it produce effervascene. Example:
A dosage form is a medicated product ENO powder used for indigestion, flatulence
specially designed for administration and heartburn etc.
depending upon the routes to the patient for Powder: Powder are medicaments in
the diagnosis and treatment of disease. dried form. The powders are of different
The dosage form is broadly divided into types:
solid dosage form, liquid dosage form and - Simple or compound powder—The
inhalations which are used both internally simple powder containing just one active
as well as externally. inguedients (i.e. Acetylsalicylic acid
Solid Dosage Form: (Internal Use) powder) and compound powder con-
taining more than one active ingredients.
Capsules
- Powders enclosed in cachets (e.g.
These are small gelatin containes shells. ALCOPAR, ORS powder) and in capsules
Capsules are of two type—hard & soft (e.g. Ampicillin powder)
capsules.
- Effervascent Powder
Hard Capsules are used for powdered - Powder for external use—e.g. NEBA-
drugs i.e. capsules ampicillin, tetracycline. In SULF, Boric acid powder, Zinc oxide
hard capsules, certain sustained released powder, Talc etc. tooth powder may also
substance, which gradually release the drug
be classified under this group.
in the respiratory tract. (i.e. cap. theo-
phylline). - Powder with metal (e.g. Mercury with
chalk) used as purgative.
Soft Capsules are used for oils and
solution of active drugs i.e. cap. vitamins A, - Powder use after reconstitution e.g. Syr.
A & D, E, garlic pearls, seven seas etc. Ampicillin for paediatric use
Soft capsules are also used for semisolid Tablets
(ointment) i.e. eye aplicaps of chloromy- These are the most extensively used solid
cetein. dosage form containing granulated or
Granules: These are mixture of active powdered drugs that are compressed or
medicament, sugar and some flavouring moulded into different shapes. These are
General Action of Drugs 9
different types of tablets according to their nature and when applied on the skin (with
size, shape and uses: brush or rod) evaporates to the skin and
- Simple Tablets are disintegrated readily leaving a flexible, protective film. The film
e.g. Tab Aspirin. producing agent is pyroxylin (nitrocellulose)
- Soluble Tablets are dissolved in water to and for flexibility colour oil is added.
form solution for internal and external use It is generally used for small cuts and
(gargles) e.g. Tab Disprin, also used or abrasions.
parenteral administration called hypoder-
Dusting Powder are free flowing and
mic tablets e.g. Atropine sulphate tablets.
very fine in nature for external use.
- Scored Tablets may be easily divided if
smaller doses are required (e.g. Tab. Insufflations are dusting powder
Analgin) consisting medicaments that are blown by an
insufflator (Similar to automiser) into various
- Lozenges are solid preparation consisting
mainly of sugar and gum and ensures slow body cavities, nose, throat, ear etc., where it
release of medicaments and generally used would be difficult to apply the powder
for local action-cough remedies e.g. directly.
Strepcils, Vocacil. Suppositories are conical or ovoid shape
- Pastilles are solid medicated preparation solid preparation made up of fat (cocoa
intended to dissolve slowly in the mouth butter oil or theobroma oil), a wax or a
and softer than lozenges. glycerine-gelatin gelly. They are used for
- Chewable Tablets are chewed in the insertion into the rectum, where they melt,
mouth for systemic action e.g. Tab. Digene, dissolve and disperse and exert their action-
vitamin C (Suckcee), Mebendazole (for local as well as systemic.
peadiatric use) etc. Pessaries are the same as suppositories
- Buccal or Sublingual are chewed under for introduction into vagina. Pessaries are of
the tongue when it dissolved, tablets and two type:
extert their action e.g. Tab. Nitroglycerine. - Moulded passaries (as suppositories).
- Implants are tablets use for sustained - Compressed pessaries–in different shapes.
action and implented under the skin. e.g.
Deoxycortone acetone (for contraception) Bougies used for nasal and uretheral
administration.
- Depot Tablets are compressed tablets used
for sustained systemic action e.g. tab. Ear cone for ear administration.
Asmapax Depot for asthmatic patients. Plasters are solid adhesive (with cloth)
- Enteric-coated are coated keratin, cellulose preparation applied to the skin to protect
acetate phthalate, tablets which do not sooth and lessen pain e.g. Mustard plaster,
dissolve in the stomach and only dissolve Capsicum plaster.
in alkaline juice of the intestine where the
drug is liberated. e.g. Tab. Erythromycin. Semi Solid/Liquid dosage form (Internal
use)
Solid dosage form (Externally used) Aqua are aquous solution of volatile sub-
Collodions: These are the fluid preparation stance used as solvent in certain pharma-
intended for external use. The vehicle of ceutical preparation to mask the disagrable
collodion are volatile (e.g. ethyl alcohol) in taste of drug e.g peppermint water.
10 Essentials of Pharmacology
Cachets are providing a means of adminis- solution, bladder irrigation and certain
trating nauseous or disagreable powder dermatological solution intended for
in a tasteless form. application to broken surface.
Elixir are liquid, oral preparation of potent Syrups are the liquid oral preparation made
or nauseous medicaments, which are in concentrated sugar solution, mainly for
pleasantly flavoured and coloured with paediatric use and for drugs which are
suitable agents. unpleasant in taste.
Emulsions are suspensions of fats or oils in Tinctures are the concentrated alcoholic
water with the inclusion of an suitable preparation of vegetable drugs made by
emulsifying agent (e.g Gum acacia, Gum maceration process. (e.g. Tr. opium, Tr.
Tragacanth) e.g. Castor oil emulsion, Cod lemon) used in different pharmaceutical
liver oil emulsion for internal use. One preparation for oral use. Tr. Benzion Co.
such emulsion are also used externally— is used externally.
Benzyl Benzoate emulsion.
Gels are the aqueous colloidal suspension of SEMI SOLID/LIQUID DOSAGE FORM
insoluble medicaiments (e.g. Aluminium (EXTERNAL USE)
hydroxide as antacid – in Digene Gel). Applications are liquid or semi-liquid
Linctus are viscous, liquid oral preparation preparation to the skin, and are usually
containing high proportions of syrup emulsion or suspension in nature (e.g.
(sugar) and glycerin (for viscosity and its Antiparasitics application)
sweat nature) which produce a demuls-
Creams are semi solid preparation (usually
cent affect on the mucous membrane of
emulsion) for external use. They are oily
the throat.
and non-greasy in nature.
Mixture are liquid oral preparation, where
Ear/eye/nasal drops are solution of drugs
the medicaments are in solution or
suspension form. Mixture are generally that are instilled into a ear, eye and nose
not formulated for a long life and with a dropper. The eye drops are sterile
prepared freshly. solutions.
Paediatric Drops are liquid oral preparation Enema are solution, suspension or emulsion
of small dose giving by a calibrated (o/w type) of medicaiment intended for
dropper intended for paediatric use. rectal administration.
Solution are aquous solution containing one Gargels are aqueous solution used to prevent
or more drugs. They are divided into and treatment of throat infections.
different categories: Irrigators are medicated solution used to treat
Solution in dosage form for oral use/external urinary bladder, vagina and less often the
use. e.g. Strong iodine solution, Hydrogen nose infections. They are administering
peroxide solution. with a help of catheter (in bladder),
Parenteral Solution are sterile liquid or vulcanite (for vagina) which are made up
suspensions packaged in sterile containers, of thin, soft rubber or plastic tube. The
intended for parenteral administration. nose irrigator is made up of glass.
There are other type of solutions that are Jellies are transparent or translucent, non-
used for peritoneal dialysis, anticoagulant greasy medicated semi-solid preparation
General Action of Drugs 11