INTRODUCTION

Mankind owes much to chemistry. The main aim of chemistry has

been to improve the quality of human life. Organic compounds
are so closely elated with our everyday life activities that in their
absence, the survival is not possible. For example, clothes
(cotton, wool, terylence, silk, nylon, etc.) we wear, carbohydrates.
Proteins, oils and fats (essential constituents of food) we eat,
soaps and detergent we use for washing and bathing purpose,
etc. are all organic compounds Futher these organic compounds
are used in various fields of human effort such as agriculture,
textiles, medicines and durgs, plastics, dyes, photography power
and transportation, etc. So, we can safely say that Life without
chemistry would have not been possible.. In this unit, we shall
briefly study the chemistry of organic compounds which are
widely used in our everyday life.
9.1

INTRODUCING

TO

MEDICINES

OR

DRUGS

AND

CHEMOTHERAPY
Chemical substances used for the cure or treatment of diseases
(in man or other animals) and reducing suffering from pain are
called medicines or drugs.
Drugs and Medicines
All drugs are medicines and all medicines are drugs. But a drug
may be habit forming causing addiction while a medicine is safe
to us and does not cause addiction.

Drugs may be a single chemical substance or a combination of

two or more different substance. An ideal drug should satisfy the
following requirements:
(i)

When administrated to the ailing individual or host, its

action should be localized at the site where it is desired to
act. In actual practice. There is no drug which behaves in

the manner.
(ii)
It should act on system with efficiency and safety.
(iii) It should have minimum side effects.
(iv) It should not injure host tissues or physiological processes.
(v) The cells should not acquire resistance to the drug after
sometime.
Very few days satisfy all the above requirements. Each
drug has an optimum dose, below which it has no action
and above this level it becomes a poison.
The term chemotherapy, which literally means chemical
therapy or chemical treatment was coined in 1913 by Paul
Ehrlich, the father of modern chemotherapy. He defined
chemotherapy as the sue of chemicals (drugs) to injure or
destroy infections micro- organisms without causing any
injure to the host. According to Ehrlich, Chemotherapeutic
agents are chemical substance which have selective
toxicity, being harmful as much as possible to the
invading or infectious organization but harmless to the
host. Chemotherapy has developed into a vast

subject

today and efforts are being continuously made to search

new drug as to free human beings from various types of

diseases. Chemicals (drugs) used in chemotherapy are

usually classified according to their action Examples are,
9.2 ANTIPYRETICS
Chemical substance which are used to bring down the
body temperature in high fevers and called antipyretics.
This causes body to lose heat and the person gets a lot of
perspiration Some

common antipyretics are aspirin,

phenacetin, paracetamol, analgin (novalgin, methacetin,

and butazlolidine, etc.
Aspirin is absorded from gastrointestinal tract. The
stomach acid causes a partial hydrolysis of the ester. The
ester circulated in the blood and further hydrolysis occurs
into salicylic and which is the active component. It causes
several side effects. It may cause minute ulcers in the
stomach and cause persons are allergic to aspirin. The
usual allergic reaction is rashes on skin, lowering of blood
pressure, profuse sweating intense thirst,

nausea and

vomiting. Calcium and sodium salts of aspirin are more

soluble and less harmful.
Because of these shortcomings in aspirin, the other
analgesics like ibuprofen, naproxen, diclofenac sodium or
potassium find use as alternatives.
The derivatives of p- aminophenol

are

used

as

antipyretics. The main limi9tation of these derivatives is

that they may act on red blood cells and thus, they may
be harmful in moderate doses. The important derivatives
are:

9.2 ANALGESICS
Medicines used for relieving pain in the body by acting on
the central nervous system, are called analgesics. These
are of two types:(i)
Narcotic (addictive) drugs: These are mainly opium
alkaloids and its products such as morphine, codeine,
marijuance and heroin (morphine dilacerate these
produce analgesia and sleep and in high doses cause
unconsciousness

(super

coma),

convulsions

and

ultimately leading to death. These narcotics are also

referred to as opiates because they are obtained
from the opium poppy. They are very potent drugs
and their chronic use leads to addiction. These
analgesics

are

mainly

used

for

the

relief

in

postoperative pains, cardiac pain and pain related to

(ii)

child birth and terminal cancer.

Non- narcotic (non- addictive) drugs: These are
the drugs which are not potent and do not cause
addiction.

Common

paracetamol,

drugs

novalgin,

are

aspirin,

butazolidin,

analgin,
(phenyl

butazone,) brufen (ibuprofen ) and naproxen, etc.

These drugs also have antipyretic properties. Aspirin,
novalgin and phenacetin act both as antipyretic as
well as analgetic. They are quite effective and give
immediate relief from pain and fever. Now, aspirin
also finds use in the prevention of heat attacks and
as reliever of pain in angina because it has anti-

blood clotting action. However, overdoses and empty

stomach aspirin is supposed to be toxic to the liver. It
gets hydrolysed in stomach giving salicylic acid
which sometimes cause bleeding in stomach Calcium
and sodium salts of aspirin are m ore soluble and less
harmful.
9.4 ANTI- MALARIALS
Medicines used to bring down the body temperature during
malaria fever are called anti- malarias. Originally quinine (an
alkaloid) was the only drug know to be effective against malaria.
Malaria is highly widespread infections disease, caused by
protozoa of genus Plasmodium. It is characterized clinically by
periodic fever, anemia and enlargement of liver and spleen. The
four species, Plasmodium vivax, Plasmodium malaria, Plasmodium
ovule and Plasmodium falciparum are responsible for malaria in
humans. Thus, there are four types of malaria:
Protozoa

Malaria Caused

Plasmodium vivax

Fever on altermate days

PlasmodiumMalariae

Fever once in three days

Plasmodium ovale

Fever once in three days

Plasmodium Falciparum

Fever once in four days

Choice of an anti- malarial drug depends on the point of its action

on the life cycle of the malarial parasite. Various drugs used are:

1. Primaquine

: It destroys sporozited in theliver. It is

too toxic,
and its long term use is not
advisable.
2. Chloroquine, proquanil and pyrimethamine:
These kill the parasites in blood.
9.5 TRANQUILLIZERS OR HYPNOTICS
The drugs which act on the Central Nervous System (CNS) and
help

in

reducing

anxiety

and

mental

tension

are

called

tranquilizers. They produce a more calm outlook grossly altering

the level of consciousness. They are used for the treatment of
mental disease and hence, are called psychotherapeutic drugs.
There are various type of tranquilizers and they work by
different mechanisms. For example, noradrenaline is one of the
several neurothransmitters that plays an important role in mood
changes. If the level of noradrenalin in the body is low due to
certain reasons then the signal sending activity of the hormore
becomes slow and the person suffers from depression. In such
cases, the patient needs antidepressant drugs and these drugs
inhibit

the

enzymes

which

catalyse

the

degradation

of

noradrenalne.
The two important commonly used antidepressant drugs are
iproniazid and phenelzine (Nardil).

Two

powerful

drugs

called

reserpine

(an

alkaloid

and

chlorpromazine were introduced simultancously for getting reliet

from hypertension. The other drugs in common use are barbituric
acid and its 5,5 disubstituted. Derivatives (barbiturate ) such as
veronal, amytal, luminal, seconal etc.
Chlorodiazepoxide and meprohamate are relatively and relatively
mild tranquilizers suitable for relieving tension. Equanil is used in
controlling depression and hypertension. Another

important

tranquilizers are diazepam (valium, calmpose) and serotonin.

9.6 ANTISEPTICS AND DISINFECTANTS
The chemicals used for sterilizations are classified under two
headings: (i) Antiseptics and (ii) Disinfections.
(i)

Antiseptics : Chemical substances which prevent growth

to micro- organism or kill them but are not harmful to the
living human tissues are called antiseptics.
The term septic is derived from the Greek word
skeptics which means putrify or rot. In medicine, it
indicated the sate of being infected with pus forming
organism. Anti- infective agents which are applied locally,
i.e, applied directly to the wounds, cuts, ulcers, and
diseased skin surfaces, etc. are known as antiseptics.
There are also sued to reduce odours casued by bacterial,
decomposition of the body or in the mouth. They are
therefore, mixed with deodorants, face powders and

breath purifiers, soframycin and forcing, etc are familiar

antiseptic creams.
Some common examples of antispctics are Dettol, savlon,
acriflavin,gentian violet, mercurochrome, boric acid, chloraminesT, tincture of iodine (an alcohol- water solution containing 2-3%
iodine), iodofor, hydrogen, peroxide, potassium permanganate,
soframycin and furacine, etc.
(ii)

Disinfectants: Chemical substances which kill microorganisum or stop their growth but are harmful to the
human tissue are called disinfectants.
These substances kill the bacteria immediately. These are
used for sterilization of inanimate objects like instruments,
utensils,

toilets,

drains,

floors,

sanitary

fittings

and

excreta. These are harmful to living tissues and cannot be

used on the skin. The chlorine, bleaching powder, sulphur
dioxide, etc.
The same substance can act as antiseptic or disinfectant
depending upon the concentration of the substance in
solution. In smaller concentrations, it is and antiseptic in
solution. In smaller concentrations, It is and antiseptic
while in higher concentration it becomes disinfectant.
0.2% solution of phenol acts as an antiseptic and its 1%
solution is a disinfectant.
Some common examples are:
(a)
Chlorine (C12) is used to disinfect drinking water. It
is

used

as

0.2

to

concentrated solution.)

0.4

ppm

(parts

per

million

(b)

Hexachlorohene is mainly used in soaps, creams,

dusting poweders and emulusions.

(c)
Thymol a natural derivative of phenol is a powerful
disinfectant.
(d)
Amyl meta cresol (5- methyl-2 pently phenol) is
used as antiseptic in mouth wash or gargles in
infections of the mouth and throat.
(e)
Bithional is used as an antiseptic in medicated
soaps. Such soaps are used to reduce undesirable
odours due to bacterial action on skin surface.
(f) Dettol is one of the most commonly used antiseptic in the
world. It is a mixture of chloroxylenol and
a

suitable

solvent.

Chloroxylenol

- terpeeol in

antiseptic

and

disinfectant. p- Chlorometaxylenol is also used as a body

deodorant.
(g) Gention violer and methylene blue are organic dyes but
are also used as effective antiseptics.
9.7 ANTIMICROBIALS
Chemical substances used to cure diseases caused by bacteria,
fungi and viruses are called antimicrobials. These include
antibacterial, antifungal and antiviral agents.
Discovery

of

antibacterial.

In

the

year

1908,

German

bacteriologist Paul Ehrlich developed the first antimicrobial drug

known as salvarsan which destroys the bacteria spirochete
responsible for syphilis which is common skin disease. For this
discovery, Paul Ehrlich got Noble prize for medicine. At the same

time, he was also working on the different azo dyes which are
coloured in nature and noticed the similarities in structures of
salvarsan and azo dyes. Whereas similarities in structure of
salvarsan and azo dyes. Where as_______________________The
tissues are selectively coloured by the azo dyes. In 1932, he
synthesized the first effective antibacterial agent known as
Prontosil which resembles in structure to salvarsn.

Antibacterial; Some important examples of antibacterial drugs are

sulpha, drugs, antibiotics, quinonlones, etc.
(a)

Sulpha drugs A group of drugs which are derivatives of

p-amino benzene sulphonaide (sulphanilamide) are called

sulpha drugs, which showed antibacterial activity (a part of
protosil.)
These were the first effective chemotherapeutic agents to be
widely used against disease (such as dysentery. Pneumonia,
tuberculosis, infections, etc.) caused by cocciinfectiosn. They
have also been found to be active against gram- positive and
gram-

negative

cocci,

bacilli

and

protozoa.

At

present

sulphanilamides have been largely replaced by antibiotics for the

treatment of most of the largely replace by antibiotics for the
treatment of most of the bacterial diseases. Some successful
sulphanilamides are given below:

(b)

Antibiotics: Chemical substances which are produced by

micro- organism (such as bacteria, fungi and moulds) and

can be used to kill other micro- organisms are called
antibiotics.
The first antibiotic. Discovered by Alexander Flemming in
1929 from the mould pencillium notanu, was penicillin. In
1938, Ernst chain and Howard Florey isolated penicillin in
pure from and proved its effectiveness as an antibiotic. It
was introduced into medical practice in 1941. Penicnllin is
used against large number of infections caused by various
cocci, gram- positive bacteria, etc. In is an effective drug for
pneumonia, bronchits, sore throat and abcesses.
Several naturally occurring penicillin have been isolated All
of these have the empirical formula, C9H11 O4SN2R.
In penicillin, a four membered ring is fused to another five
membered ring. Strutures of individual penicillins are given
in the table. Penicillin- G is the most commonly used.
The penicillins are only sparingly soluble in water. However,
their sodium or potassium salts are soluble in water.
Penicillins are found to b e active against gram- positive
stains. However, these are ineffective aganst resistance to
penicillins.

Penicillins

generally

have

low

toxicity

in

comparison to sulpha drugs. However, in some cases allergic

reactions may result in. Penicillin in thus, given after a test
prick.
The antibiotics which control the microbial diseases can
either be bactericidal or bacteriostatic. Examples are,

Bactredical: The durgs which kill the organism in the body.

For example. Pencillin, ofloxacin, aminoglycosiders.
Bacteriostatic: The drugs which inhibits or check the growth
of the organism in the body. For example, Tetracycline.
Chloramphenicol and crythromycin.
Scientists have discovered a number of other antibioties.
These have proved to be as effective as penicillin but some
of these are broad spectrum and are more effective.
Broad spectrum antibiotic: The complete range of
micro- organisms which can be killed by a particular
antibiotic is called its spectrum. Antibiotics which are
effective against several different types of

harmful micro-

organism and thus, Capable of curing several infections are

called broad spectrum, antibiotics. Amongst these are
chloramphenicol, tetracyclines, oxloxacin and vancomycin,
or a mixture of different antibiotics. Penicillin has a narrow
spectrum.
Ampicillin and amoxicillin are semisynthetic modification of
penicillin.

In

Inida

pencillin

in

smanufactured

at

the

Hindustan antibiotics in Pimpri and at Indian Drugs and

Pharmaceuticals Limited (IDPL), Rishikesh and In

private

sector of Industry.
(h)
Streptomycin: It was discovered in 1944 by
Waksman. It is effective against tuberculosis. It is also
used for other common infections like throat, lungs,
ears and Kidney. It is very effective in the treatment of
meaningitis and pneumonia.

(i) Streptomycin is an amino base and forms salts that are

very soluble in water. The sulphate and calcium chloride
double

salts

are

white

amorphous

powders.

The

molecule contains two strongly basiuc quandioa groups

and a weakly basic methylamino group.
Streptomycin is rapidly absorbed after an intramscullar
injection. Oral administration of streptomycin is of no
value in the treatment.
PAS (p- amino salicyclic acid) and INH (iso- nicotin
hydrazine or iso niazid) are also, used for the treatment of
tuberculosis.
(ii) Chloramphenicol: It is a broad spectrum antibiotic. It
was first isolated from a species of streptomyces. It has
been produced synthetically on commercial basis. It is
white or greyish white needle like crystalline substance . It
has a bitter taste. One gram of chloramphenicol is soluble
in about 400 ml. of water, It is frelly soluble in alcohol.
It is effective against certain gram- positive and gramnegative bacteria, some rickettsiae and viruses. It is very
effective in the treatment of typhoid. Fever, para- typhoid
fevers, diarrhea and dysentery. It is also specific for
influenza, meningitis, pneumonia, whooping, cough and
urinary tract infection.

Chloraphenicol may cause serious complications and

hence. It should not be used indiscriminately or for minor
infections. Chloraphenicol in high concentrations inhibits
the growth of animal and plant cells.
(iii) Tetracyclines:

The

hydronaphthacene

Tetrachylines

skeleton

as

the

contain

characteristic

structural unit. The structures of tetracyclines are given

as follow:Tetracyclines are broad spectrum antibiotics and are effective
against a number of types of bacteria, larger viruses, protozoa,
parasites and typhus fever. These can be given orally.
(c)

Quinolones: Other important class of antibacterial drugs

which are neither sulpha drugs nor antibiotics, are the

derivatives of quinines such as ciprofloxacin and norfloxacin,
These are widely used for urinary tract infections.
9.8 Anti- Fertility Drugs
Chemical substances used to check progeny in women are
called

anti-

fertility

drugs

or

birth

control

drugs

or

oral

contraceptives.
Oral contraceptives (or pills or oral pills) belong to the class
of natural products known as steroids. It control the female
menstrual cycle and ovulation. A number of oral pills (POP), postoctal pill, long acting (once- a month) pill and male pill. These
anti-

fertility

drugs

contain

chemicals

and

progesterone

(progestin), which are more potent than the natural hormones.

For

example,

common

brand

name

Enovid

contains

Norethindrone (a progesting) and Mestranol (or Ethynylestradiol,

an estrogen). Mifepristone is a synthetic steroid that blocks the
effects of progesterone and is used as a morning after pill in
many countries.
Ormeloxifene

(centchroman,

saheli

has

also

been

developed and tested at the CDRI (Central Drug Research

Institute) Lucknow as an effective anti- fertility drug to certain
extent.
All such drugs are expected to have side effects and hence
should be used only under proper medical advice.
9.9 ANTIHSTAMINES
These

drugs

are

also

called

anti-

allergy

drugs.

Antihistamines are amines which are amines which are used

as drugs to control the allergy. Effects produced by
histamines. Antigens from environment and food create
allergic reactions to our body. In this situation histamines are
relapsed from certain cells in our body and is produced by
the decarboxylation of histidine which is an amino acid
present in the body.
Anthistamines are the drugs which diminiosh or abolish the
effects of histamine (a chemical realized by most cells during
allergic recations.)

Synthetic drugs such as bromopheniramine (Dimetapp) and

terfenadine (seldane) are used an antihistamines and they
neutralize the effect of histamine in the body.
Thus, antihistamines are widely used for treatment of skin
rashes, conjunctivitis (inflammation of eyes), hay fever,
nasal discharges itching of ENT (eyes, nose and throat)
motion sickness (air, road and sea,) nausea in pregnancy
and post operative vomiting, mild asthma,insect bites, cold,
etc. Some other commonly used antishistances are:
i.
Disphenydramine (Benadryl)
ii.
Pheniramine maleate (Avil and cough syrups)
iii. Chlorpheniramine maleate (zeet)
iv. Triprolidine (Acididil)
v.
Phenonthiazine, Promethazine (Phenargan)
vi. Dimethindene (Foristal)
vii. Antazoline (Antistine)
viii. Chlorotheopyllinate salt (Avomine)
ix. Cetrizine
9.10 ANTACIDS
The substances which reduce of neutralize gastric acidity and
raise the Ph to appropriate level

in stomach are called

antacids. Intestine is acidic due to the formation of HCI during

digestion. Excessive acidity in the intestine creates problem o f
intestinal ulcer, gastric rrefluc and oesophagitis. The commonly
used antacids are discussed below:
(i) Baking soda containing NaHCO3 and KHCO3
(ii) MgO, Mg (OH)2, MgCo3 and magnesium trislicate
(iii) CaCo3
(IV)AI (OH)3, AIPO4 and aluminium amino acetate.

In recent years, Omeprazole and Lansoprazole are also,

marketed as antacid as they prevent the formation of acid in the
stomach. Rantitidine (Zantac) and Cimitidine (Tegamet) are used
in the treatment of peptic ulcers. Some other antacids are:
digene, gelusil, aciguard, acidin, acifix, acinil, metadrate, alucino,
etc.
9.11 ANAESTHETICS
Anaesthetics may be defined as those drugs which produce
insensibility to the vital functions of all type of cells especially of
nervous system. The effect produced by anesthetic is reversible.
i.e. affected organs return to the normal state as soon as the
concentration of the an aesthetic is decreased. Thus, anesthetic
produces temporary insensibility to pain or feeling in the whole
body or a particular organ. Anaesthetics may be classified into
two groups on the basis of their applications.
(i)

General anesthetics: These depress the central nervous

system to such an extent that all sensitivity to pain or feeling is

lost, i.e., they produce unconsciousness all over the body. These
are used for major surgical operations, Chloroform, diethylether
and viny ethers, etc are general anaesthetics. These any be used
in the form of a gas, e.g., nitrous oxide, cyclopropane, ethylene,
ether or may be given in the injection form , e.g, sodium
pentothal.