2. Chemistry has played an important role in providing newer chemicals of synthetic origin which can be
used for treatment of diseases. Substances used for the treatment of diseases, for alleviating pain and
controlling fever are called medicines or chemotherapeutic drugs. There are large number of synthetic and
natural drugs that chemist have given to medicine. Predominant among these are sulphadrugs, analgesics,
antipyretics, antimalarials, antibiotics.
INTRODUCTION TO PHARMACOLOGY•
The study of drugs or chemicals and the effects theyhave on living animals is called pharmacology.It
explains what drugs are, what they do to body functionsand what the body does to them.It also explains why
a person may experience side effectswhen they take drugs and why there is such a widespectrum of
differences between drug actions in differentpeople.
Any substance or combination of substances presented as having properties fortreating or preventing
disease in human beings and/or animals
WHAT IS A DRUG?A drug is any substance (other than food that providesnutritional support) that,when
inhaled, injected, smoked, consumed, absorbed via a patch on the skin, or dissolved under the tongue causes
a temporary physiological (and often psychological) change in the body.
A pharmaceutical drug, also called a medication or medicine, isa chemical substance used to treat, cure,
prevent,or diagnose a disease or to promote well-being.Once these chemicals are absorbed into the
systemiccirculation they bind with certain proteins and this changes thefunctioning of the cell
slightly.Example: anticancer drugs bind to proteins on the surface of cancer cells this stimulates the cells to
die. In this case cell death is the physiological action of the drug.
3. The chemical in the drug that affects physiologicalfunctioning is the active ingredient of the drug. For most
drugs, the amount of chemical needed to cause an effect is very small, often as small as 5 micrograms; this
is 0.005%of a gram.
Along with this, inactive substances are also packed with itso that its not vulnerable to loss. Examples of
inactive ingredients are lactose and gluten.
.
?
4. Our bodies are largely controlled by proteins.
Proteins exist in many different forms in the body andhave many different functions.
Each protein has a specific function and is quite specific tothe cell type that it acts on.
For example, there are specific types of proteins called receptors.
Receptors are embedded on the cell surfaces, there are different receptors for different types of cells. A liver
cell will have different receptors than a cardiac cell. The receptor binds to other proteins and chemicals on the
outside of the cell and this in turn creates a change in the functioning of the cell
HOW DO DRUGSWORK?
5. Drugs and their Classification. Drugs used as medicines may be :
(i) natural drugs or
(ii) synthetic drugs.
(i) Natural drugs. In Aryurveda, a large number of substances are obtained from plants which can be used to
cure diseases. For example, morphine which is an important pain killer is obtained from opium. Quinine is
obtained from cinchona (bark of a tree) and is an important antimalarial. Also Reserpine is used as
antihypertensive and is obtained from rauwolfia serpentina.
ii) Synthetic drugs. A very large number of synthetic (organic) drugs are synthesised in the laboratory.The
official synthetic drugs are listed in the pharmacopoea.
Classification. Drugs have been classified as below:
a) Antibacterial drugs. Such drugs are used against disease producing bacteria, called pathogens
B]Antiviral drugs. Such drugs are used for the treatment of diseases caused by
viruses.
(c) Antiseptics and Analgesics. These are used to lower the body temperature and to get relief from pain.
(d) Central nervous system drugs. Such drugs are used against nervous diseases.
7. 1. ANTIPYRETICS
These are fever killing drugs and bring down the body temperature. Doses of an antipyretic cause excessive
sweating and thereby bring down the body temperature. The antipyretic action and the analgesic actions are
usually found together in the same drug.
Paracetamol (N-acetyl-p-amino phenol). Synthesis. It can be synthesised from p-nitrophenol as described below :
8.
9. 2. ANALGESICS
These are the drugs which decrease pain or give full relief.They can be narcotics or non- narcotics.
(i) Narcotics.These include Morphine, Codein, Heroin which are opium products Regular doses cause
addiction.They cause sleep or unconciousness depending upon the dose. These are more effective in their
analgesic properties. The structural formulae of Morphine and Codein are:
They contain the phenanthrene nucleus.
ii) Non-narcotics. Regular doses of these drugs do not cause addiction. Some common drugs of this
type are analgin and aspirin.These have anti-pyretic properties also. The structural formula of
analgin is
10. Some of the drugs which act both as analgesic and antipyretic
are:
(i) Aspirin
(ii) Analgin
(iii) Para-acetamol etc.
11. (I) ASPIRIN:it is prepared by the acetylating salicylic acid and with acetic anhydride.
Itis a common remedy for the relief of headache, muscular pain and toothache. Its use in children is not
recommended. The toxic side effect of aspirin-therapy is gastric irritation leading to ulceration. Thus, it
should not be taken empty stomach.
The calcium salt of aspirin which is soluble in water is better than simple aspirin as it has few side
effects. A familiar example of soluble aspirin is Disprin. Disprin contains calcium carbonate and
anhydrous citric acid besides aspirin and this renders aspirin, water soluble
12.
13. 3. Antimalarials
Malaria is caused by the bites of female mosquitos of genes Anopheles.
Earlier malaria was treated with Cinchona, the bark of a tree. Later, quinine (extracted
from cinchona) was used for a long time as a specific drug for malaria. Now more effective
synthetic drugs have almost replaced quinine. Antimalarials are the drugs used for supression
and treatment of the tropical disease malaria. Some important antimalarials which are used
these days are:
(a) Chloroquine. It is a much more effective antimalarial than quinine. Its synthesis from m-chloroaniline (2
mole) is outlined given
14. b) PAMAQUIN (PLASMOQUIN).
Its chemical name is 8- (4'-diethylamino-3-methyl butyl amino)-6-methoxy
quinoline. It is synthesised by the condensation reaction between 4-bromo-1-
diethyl-aminopentane and 8-amino-6-methoxy quinoline. It may be noted that 8-
amino-6-methoxy quinoline is prepared from 4-amino-3-nitroanisol by means of
the skraup synthesis.
15. USES: Chloroquine is more effective drug and is more potent. It does not stain the eyes or skin.Thus, it is a drug
of choice for the treatment of malaria. It is very effective in acute attacks of vivax malaria.
Choice of antimalarial drug depends upon the point of its action on the life cycle of the malarial parasite.
Supressive drug like chloroquine kill the parasites in the blood and donot permit the cycle to continue. Parasites
continue, being present in the liver but as red cell cycle is discontinued, the patient does not suffer from fever.
16. RANITIDINE ; ANTACID:-
Over production of hydrochloric acid in the stomach causes irritation and pain. In severe cases ulcers
are produced in the stomach.The substances which neutralise the excess acid raise the pH to an
appropriate level in stomach are called antiacid. Most commonly used antacids are NaHCO3,
Mg(OH)2,Al(OH)3 gel, aluminium phosphate etc.
Excess of sod. bicarbonate can make the stomach alkaline and trigger the production of even more
acid. But with these substances, patients cannot be treated permanently. In advanced stages, ulcers
can be caused which are life threatening.
Ranitidine is the largest selling antacid to control acidity.The use of Ranitidine prevents the formation
of acid in the stomach.
Ranitidine is used to treat ulcers of the stomach and intestines and prevent them from deturning after
treatment. It gives relief from heart burn, It is a therapy of gastric and duodenal ulcers, etc.
17.
18. An antibiotic is a substance produced by micro organisms, that is capable of inhibiting destroying the
growth of other micro-organisms at low concentration. Antibiotics are much ог more potent than
sulphonamides, as antibacterial substances have substantially replaced sulphonamides as anti-
infective agents.
An antibiotic compound produced by one micro organism is toxic to another organisms. Penicillin is
the most widely used antibiotic in the world. Fleming (1929) discovered a mould of the penicillium
species which inhibited the growth of certain bacteria. The observation was investigated later by a
number of workers which resulted in the isolation of the active principal Penicillin.
Penicillin, cephalosporin, tetracycline are the important types ofantibiotics.
It can be taken orally as a pill or liquid, or can be injected. It is produced from the bacteria and
molds.
It fights diseases caused by bacteria.
19. PENICILLIN.Penicillin can not be taken orally. The compound is quite unstable and undergoes
rearrangement to an inactive derivative in the stomach (pH slightly more than seven). Also some
kind of bacteria develop resistance to penicillin by developing the enzyme penicillinase which
breaks down the antibiotic.To persons who are allergic, it can cause fatal coma. A large number of
other antibiotics were later discovered which destroy infectious micro-organisms.
Of all the natural penicillins, benzyl penicillin (Penicillin G) is still the best. It has been found that
different types of penicillins are produced by Penicillium chrysogenum when the cultural
conditions are changed. Penicillin is narrow spectrum antibiotic.
20.
21. 2. STREPTOMYCIN: It is very effective in the treatment of tuberculosis, meningitis and pneumonia. It is
laevorotatory. It is also used for other common infections like throat, lungs, etc. Its structure is composed of the
three units:
(i) streptose
(ii) N-methyl-L-glucosamine
(iii) streptidine.
ITS STRUCTURE IS:
22. 3. TETRACYCLINES:Aureomycin was isolated from cultures of streptomyces aureofaciens. It is used in
the treatment of typhoid fever. Terramycin was isolated from cultures of streptomyces rimosus.
Chlorotetracycline was also called aureomycin and Terramycin is named as oxytetracycline.
Tetracyclines are broad spectrum antibiotics and are effective against a number of types of bacteria, viruses,
protezos, parasites etc. Unlike Penicillin and streptomycin, they can be given orally because these are absorbed
from the gastrointestinal tract. Due to this property, streptomycin is largely replaced by tetracyclins.
23. MEDICINAL USES OF CURCUMIN, AZADIRACHTIN,
VITAMIN C:-
(a) Curcumin (Haldi)
It is used in mustard and to colour butter and cheese. Turmeric has been
used in both Ayurvedic and chinese medicine as an anti-inflammatory to treat
digestive and liver problems, skin diseases and wounds. Curcumin is also a
powerful antioxident.
It is the main active ingredient in turmeric. The curcumin content of
turmeric is not that high. It is around 3% by weight.
It is used to heal many health disorders like liver problems, digestive
disorders
(b) Azadirachtin (Neem)
Neem leaf is used for leprosy, eye disorders, bloody nose,
intestinal worms, stomach upset, loss of apetite, skin ulters, diseases of heart and
blood vessels (cardiovascular disease), fever, diabetes, gum disease (gingivitis) and
liver problems.
The leaf is also used for birth control and to cause abortions.
Neem flowers can be used to treat anorexia, nausea, belching and intestinal worms.
Ayurveda suggests neem leaves are good for the eyes and useful in treating skin
disease and headaches. They are used in aromatherapy because of their calming
effect.
24. (C) VITAMIN-C (I-ASCORBIC ACID):
We need Vitamin-C for the growth and repair of tissues in all parts of our body. It
helps the body make collagen, an important protein used to make skin, cartilage,
tendons, ligaments and blood vessels.
Vitamin C is needed for healing wounds and for reparing and maintaining bones and
teeth.
The benefits of vitamin C include protection against immune system
deficiencies, cardiovascular disease etc.
Vitamin-C is used for skin injuries.Vitamin C supplementation is also used to treat
ulcers, burns and injurities because of its ability to stimulate collagen formation.
The cooking of food at low temperatures and for short-times is important to keep
vitamin-C preserved and beneficial in the food.
25. Pharmaceuticals have contributed to improvements in life expectancy and
quality of life of many patients. Medicines can cure, relieve symptoms, delay the
onset of disease and prevent complications.They often offer good value for
money.
However, recent trends raise a number of concerns. The launch prices of new
drugs have been increasing in some therapeutic categories, sometimes without
commensurate health gains. At the same time, new effective medicines are not
always affordable to all patients who need them and put a high pressure on
healthcare budgets.
These trends raise questions about incentives at work in the pharmaceutical
sector and the sustainability of current pricing models