Unit 1 General Action of Drugs-I: Structure
Unit 1 General Action of Drugs-I: Structure
Unit 1 General Action of Drugs-I: Structure
1.1 Introduction
Objectives
1.2 Introduction to Pharmacology
1.3 Sources of Drugs
Plant Origin
Animal Sources
From Human Being
From Microorganisms
1.4 Routes of Drug Administration
Local Routes
Systemic Routes
Parenteral Routes
Inhalation route
1.5 Dosage Forms
1.6 Dosage Forms and Routes of Drug Administration
Solid Dosage Form (Internal Use)
Solid Dosage Form (Externally used)
Semisolid/Liquid Dosage Form (Internal Use)
Semisolid/Liquid Dosage Form (External use)
Inhalation Form
1.7 Summary
1.8 Terminal Questions
1.9 Answers
1.1 INTRODUCTION
Objectives
Pharmacokinetics deals with the alterations of the drug by the body which
includes absorption, distribution, binding/storage, biotransformation and
excretion of drugs.
Toxicology deals with the side/adverse effects and other poisonous effects of
drugs, since the same drug can be a poison, depending on the dose.
Pharmacognosy deals with the study of the sources of drugs derived from
plants and animal origin.
Materia-medica: This is an older term and deals with the source, description
(physical and chemical properties) and preparation of drugs.
‘Drug’ is derived from French word ‘drogue’ means a dry herb. Drugs are
obtained mainly from plants, animals, microbes and mineral sources, but a
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majority of them that are used therapeutically are from synthetic or semi- General Action of
synthetic products. Drugs-I
ii) Glycosides are ether like organic structure combined with sugars, the non-
sugar component called aglycone or genin. The important glycosides are:
Digitalis.
iii) Oils
a) Fixed oils are glycerides of oleic, palmitic and stearic acids. Mostly
fixed oils are edible and used for cooking. The fixed oils used as drug
are: castor oil, olive oil, cocoa butter , cod liver oil and shark liver oil.
iv) Resins are produced by oxidation and polymerization of volatile oils. The
different types of resins are: Oleoresins, gum resins, oleo gum resin and
balsams.
The different animal products after purification in a suitable dosage form for
the treatment of disease are listed in Table 1.1. 7
General Pharmacology Table 1.1: Classification of different animal products used as drug and
surgicals
There are certain products which are obtained from human being e.g.
SAQ 1
The dosage forms applied locally to the skin are powders, paste, lotions,
ointments, creams, plasters and jellies. They are used for their antiseptic,
antipruritic, analgesic, local anaesthetic and other related effects.
On the skin, drug is applied in the form of ointment, cream, lotion, paste,
plaster, powder etc.
The topical application is also used on the mucous membranes i.e. nose, throat,
eye, ear, bronchi, rectum, urethra, vagina and rectum.
In case of mouth and pharynx, the drug is used in the form of throat paints,
lozenges, gargles or mouth washes.
In case of corneal application (in the form of ointments, drops), the drug may
penetrate the anterior chamber and affect the ciliary muscle. The nasal mucosa
is treated with drug solution in the form of spray or irrigation.
The bronchial mucosa and lungs are treated with inhalations, aerosols (in the
form of fine powder with the help of nebulizer) e.g. salbutamol (ASTHALIN)
inhaler.
Drugs may also be administered locally in the form of bougies, jellies for
urethra, pessaries, vaginal tablets, creams and douches for vagina and
suppositories for rectal administration.
Due to the rich blood and lymph supply to rectum the unionized and lipid
soluble substances are readily absorbed from the rectum. The advantages of
this route are that gastric irritation is avoided and easy administration by the
patient himself. Administration of drug in the form of liquid into the rectum is
called enema, which may be soap water or glycerine-vegetable oil. It is used to
remove the faecal matter. Certain drugs are administered rectally for producing
systemic effects also (e.g. aminophylline, indomethacin, paraldehyde etc.).
Oral Route
This is the most commonly used route for drug administration. It is also the
safest, most convenient and economical.
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General Pharmacology Enteric Coated Tablets
The drugs which are destroyed by the gastric juices in the stomach are coated
with keratin, shellac and cellulose acid phosphate. These substances are not
dissolved by the acid juice of the stomach, but are dissolved in the intestinal
juice (alkaline) only, which is useful in:
It is a useful solid dosage form of drug, where the particles of the drug dissolve
at different time intervals.
Sublingual Administration
The administration of drugs by injection directly into the tissue fluid or blood
without having to cross the intestinal mucosa. The advantages of parenteral
routes are:
Subcutaneous
The non-irritant substances can be injected by this route. The site of injection is
usually the outer surface of the arm, or front of the thigh. Self medication (e.g.
insulin) is possible because deep penetration is not needed. Other drugs which
are administered subcutaneously are adrenaline, morphine and certain
hormonal preparations.
The other related subcutaneous routes are dermojet (by which, drug is
projected from a microfine orifice using a high velocity jet) and pellet
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implantation (which provides sustained release of the drug over weeks and General Action of
months e.g. testosterone). Drugs-I
Intramuscular
The soluble substances, mild irritants and suspensions can be injected by this
route in the large skeletal muscles (deltoid, triceps, gluteus maximus, rectus
femoris etc.). These muscles are less richly supplied with sensory nerves and
are more vascular, so irritant solutions can be injected. Small volumes (up to 2
ml) are injected into the deltoid muscle, and small or large volumes (up to 10
ml) are injected into the gluteal mass.
The rate of absorption is reasonably uniform and the onset of action is rapid.
Intravenous
The drug is injected as a bolus or infused slowly directly into a vein to produce
rapid action. It is also useful for certain irritant and hypertonic solutions, as
they are rapidly diluted by the blood. Drugs in an oily vehicle or those which
precipitate blood constituents or haemolyze erythrocytes should not be given
by this route.
Intravenous route is the most rapidly effective and the desired blood
concentration can be obtained with a definite dose but at the same time it is the
most dangerous route of administration. For once the drug is injected there is
no retreat. So, intravenous injection must usually be performed slowly and with
constant monitoring of the patient. This route is usually reserved for
emergencies when a rapid action is required.
Intradermal
The drug is injected into the skin raising a bleb. This route is employed for
vaccination e.g. BCG vaccine and for testing the sensitivity e.g. penicillin
injection.
Intra-arterial
This route is useful in diagnostic studies, by which arterial blood sample may
be withdrawn for blood gas studies. Certain cytotoxic compounds are
administered by intra-arterial perfusion in localised malignancies.
Intrathecal or Intraspinal
For local and rapid effect of drugs on the meninges or cerebrospinal axis, drugs
are injected directly into the spinal subarachnoid space. This is also used to
produce spinal anaesthesia, or for introduction of a radio-opaque contrast-
medium into the subarachnoid space for visualising the spinal cord.
Intramedullary
By this method, the drug is introduced into the bone marrow of the sternum or
tibia. Blood is occasionally given by this route.
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General Pharmacology Intracardiac
Intraperitoneal
Intra-articular
The volatile liquids and gases are given by inhalation route. The drugs may be
given as solid particles, as nebulized particles from solutions or in the form of
vapours. The volatile substances include gaseous anaesthetics, amyl nitrite and
vapours of liquid anaesthetics, gases like oxygen, carbon dioxide and helium.
Nonvolatile substances have to be broken down into small particles, and then
inhaled as aerosols.
Drugs given by this route are quickly absorbed, which takes place from the vast
surface of alveoli and produce rapid action. Various bronchodilators and mast
cell stabilizers are used in the treatment and prophylaxis of bronchial asthma
i.e. salbutamol (ASTHALIN) and sodium cromoglycate (FINTAL) inhaler.
SAQ 2
The dosage form is broadly divided into solid dosage form, liquid dosage form
and inhalation which are used both internally as well as externally.
The dosage form is broadly divided into solid dosage form, liquid dosage form
and inhalations which are used both internally as well as externally.
Capsules: These are small gelatin contains shells. Capsules are of two types –
hard & soft capsules.
Hard capsules are used for powdered drugs e.g. capsules ampicillin,
tetracycline. In hard capsules, certain sustained released substance, which
gradually release the drug in the respiratory tract (e.g. cap. theophylline).
Soft capsules are used for oils and solution of active drugs e.g. cap. vitamins
A, A & D, E, garlic pearls, seven seas etc.
Soft capsules are also used for semisolid (ointment) e.g. eye applicaps of
chloromycetin.
Granules: These are mixture of active medicament, sugar and some flavouring
agent and then moistened to produce a coherent mass which is then passed
through a sieve to form a granule. Granules are the unusual means of
administering drug that possess an unpleasant taste e.g. PAS (para-amino
salicylic acid) granules.
Powder: Powder are medicaments in dried form. The powders are of different
types:
• Effervescent powder. 13
General Pharmacology • Powder for external use e.g. NEBASULF, boric acid powder, zinc oxide
powder, talc etc. Tooth powder may also be classified under this group.
• Powder with metal (e.g. mercury with chalk) used as purgative.
• Powder use after reconstitution e.g. syr. ampicillin for paediatric use.
Tablets: These are the most extensively used solid dosage form containing
granulated or powdered drugs that are compressed or moulded into different
shapes. These are different types of tablets according to their size, shape and
uses:
Collodions: These are the fluid preparation intended for external use. It is
generally used for small cuts and abrasions.
Dusting powder are free flowing and very fine in nature for external use.
Plasters are solid adhesive (with cloth) preparation applied to the skin to
protect, soothe and lessen pain e.g. Mustard plaster, Capsicum plaster.
Mixture are liquid oral preparation, where the medicaments are in solution or
suspension form. Mixture are generally not formulated for a long life and
prepared freshly.
Solutions are aqueous solution containing one or more drugs. They are divided
into different categories:
• Solution in dosage forms for oral use/external use e.g. strong iodine
solution, hydrogen peroxide solution.
• Parenteral solution are sterile liquid or suspensions packaged in sterile
containers, intended for parenteral administration.
There are other type of solutions that are used for peritoneal dialysis,
anticoagulant solution, bladder irrigation and certain dermatological solution
intended for application to broken surface.
Syrups are the liquid oral preparation made in concentrated sugar solution,
mainly for paediatric use and for drugs which are unpleasant in taste.
Creams are semisolid preparation (usually emulsion) for external use. They
are oily and non-greasy in nature.
Ear/eye/nasal drops are solution of drugs that are instilled into a ear, eye and
nose with a dropper. The eye drops are sterile solutions.
Gargles are aqueous solution used to prevent and for treatment of throat
infections.
Irrigators are medicated solution used to treat urinary bladder, vagina and less
often the nose infections. They are administered with a help of catheter (in
bladder), vulcanite (for vagina) which are made up of thin, soft rubber or
plastic tube. The nose irrigator is made up of glass.
Lotions are liquid preparation applied to skin without friction. Lotions are used
for soothing, astringent and antipruritic affects e.g. calamine lotion.
Mouth washes are liquid preparation similar to gargles but are use for oral
hygiene.
Ointments are semi-solid greasy preparation for local application to the skin,
rectum and mucous membrane also. The ointment base is usually anhydrous
and contains the medicaments in solution or suspension. Ointments are used for
its soothing, astringent, antiseptic and other selected actions e.g. chloromycetin
eye ointment.
Throat paints are more viscous in nature (due to the high proportion of
glycerine) which being sticky and adhere to the affected site and prolongs the
action of the drug.
Pastes are semi-solid preparation for external application that differs from
similar products (i.e. ointment) in containing a high proportion of finely
powdered medicaments. They afford greater protection and are more
16 absorptive. The base may be anhydrous or water soluble e.g. zinc oxide paste.
1.6.5 Inhalation Form General Action of
Drugs-I
Aerosols are suspension of fine, solid or liquid particles in a medium like air or
oxygen and administered with the help of nebulizers. They are used to apply
drugs to the respiratory tract in asthmatic patients e.g. ASTHALIN
(salbutamol) inhaler, FINTAL (sodium cromoglycate) inhaler.
SAQ 3
1.7 SUMMARY
4. What are the different dosage forms available for oral administration of
drugs?
1.9 ANSWERS
Terminal Questions
1. Drugs are obtained mainly from plants, animals, microbes and mineral
sources, but a majority of them that are used therapeutically are from
synthetic or semi-synthetic products.
Plant Origin
ii) Glycosides are ether like organic structure combined with sugars, the
non-sugar component called aglycone or genin. The important
glycosides are: Digitalis.
iii) Oils
a) Fixed oils are glycerides of oleic, palmitic and stearic acids. Mostly
fixed oils are edible and used for cooking. The fixed oils used as
drug are: castor oil, olive oil, cocoa butter, cod liver oil and shark
liver oil.
b) Volatile oil or essential oil contains the hydrocarbon terpene. The
important volatile oils are: Turpentine oil, from species of pines,
used as a counter-irritant, lemon oil used as flavouring agent,
peppermint, cardamom and fennel used as carminative and
flavouring agent and oil of clove useful in relieving pain in
toothache.
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iv) Resins are produced by oxidation and polymerization of volatile oils. The General Action of
different types of resins are: Oleoresins, gum resins, oleo gum resin and Drugs-I
balsams.
Animal Sources
From Microorganisms
Disadvantages are:
4. The various dosage forms available for oral administration of drugs are as
follows:
Capsules: These are small gelatin contains shells. Capsules are of two
types – hard & soft capsules.
Granules: These are mixture of active medicament, sugar and some
flavouring agent and then moistened to produce a coherent mass which is
then passed through a sieve to form a granule. Granules are the unusual
means of administering drug that possess an unpleasant taste e.g. PAS
(para-amino salicylic acid) granules.
Effervescent granules: It is a mixture of citric and tartaric acids with
sodium bicarbonate and usually some sweetening agents (saccharin or
glucose) may be added. The powder granules should be dissolved with a
prescribed amount of water and taken when it produce effervescence e.g.
ENO powder used for indigestion, flatulence and heartburn etc.
Powder: Powder are medicaments in dried form. The powders are of
different types:
Tablets: These are the most extensively used solid dosage form containing
granulated or powdered drugs that are compressed or moulded into
different shapes.
Elixir are liquid, oral preparation of potent or nauseous medicaments,
which are pleasantly flavoured and coloured with suitable agents.
Mixture are liquid oral preparation, where the medicaments are in solution
or suspension form. Mixture are generally not formulated for a long life
and prepared freshly.
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