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Drugs and Their Classification
Drugs and Their Classification
ACKNOWLEDEMENT
ABHINAV RITURAJ
1.1.1
1.1.2
1.1.3
common
structural
features
and
often
have
similar
DRUG-TARGET INTERACTION
Macromolecules of biological origin perform various functions in the body.
For example, proteins which perform the role of biological catalysts in the
body are called enzymes, those which are crucial to communication
system in the body are called receptors. Carrier proteins carry polar
molecules across the cell membrane. Nucleic acids have coded genetic
information for the cell. Lipids and carbohydrates are structural parts of
the cell membrane. We shall explain the drug-target interaction with the
examples of enzymes and receptors.
1.2.1
1.2.1.1
1.2.1.2
Drug-Enzyme Interaction
Drugs inhibit any of the above mentioned activities of enzymes. These
can block the binding site of the enzyme and prevent the binding of
substrate, or can inhibit the catalytic activity of the enzyme. Such drugs
are called enzyme inhibitors. Drugs inhibit the attachment of substrate on
active site of enzymes in two different ways :
Drugs compete with the natural substrate for their attachment on the
active sites of enzymes. Such drugs are called competitive inhibitors
(Fig. 16.2).
Some drugs do not bind to the enzymes active site. These bind to a
different site of enzyme which is called allosteric site. This binding of
inhibitor at allosteric site (Fig.16.3) changes the shape of the active
site in such a way that substrate cannot recognise it. If the bond
formed between an enzyme and an inhibitor is a strong covalent
bond and cannot be broken easily, then the enzyme is blocked
permanently. The body then degrades the enzyme-inhibitor complex
and synthesises the new enzyme.
1.2.2
In the body, message between two neurons and that between neurons to
muscles is communicated through certain chemicals. These chemicals,
known as chemical messengers are received at the binding sites of
receptor proteins. To accommodate a messenger, shape of the receptor
site changes. This brings about the transfer of message into the cell.
Thus, chemical messenger gives message to the cell without entering the
cell (Fig. 16.5).
There are a large number of different receptors in the body that interact
with different chemical messengers. These receptors show selectivity for
one chemical messenger over the other because their binding sites have
different shape, structure and amino acid composition. Drugs that bind to
the receptor site and inhibit its natural function are called antagonists.
These are useful when blocking of message is required. There are other
types of drugs that mimic the natural messenger by switching on the
receptor, these are called agonists. These are useful when there is lack of
natural chemical messenger.
1.3
1.3.1
Antacids
An antacid is any substance, generally a base or basic salt, which
neutralizes stomach acidity. They are used to relieve acid indigestion,
upset stomach, sour stomach, and heartburn.
Antacids perform a neutralization reaction, i.e. they buffer gastric acid,
raising the pH to reduce acidity in the stomach. When gastric hydrochloric
acid reaches the nerves in the gastrointestinal mucosa, they signal pain to
the central nervous system. This happens when these nerves are
exposed, as in peptic ulcers. The gastric acid may also reach ulcers in the
esophagus or the duodenum.
Hyperacidity or acid dyspepsia simply means increase of acidity in the
stomach. The human stomach secretes hydrochloric acid which is
necessary for the digestion of food. When the stomach contains an
excessive amount of hydrochloric acid, then the condition is called as
hyperacidity. Sometimes, hyperacidity is confused for a simple bellyache.
This is because people with hyperacidity generally get pains in their
stomach with similar symptoms as bellyaches. This confusion is more
rampant in children who cannot differentiate between different kinds of
stomach ailments. However, hyperacidity can be found out with the sour
belching and after taste of the already eaten food in the mouth.
Bismuth subsalicylate
Histamine
Cimetidine
Ranitidine
Omeprazole
Lansoprazole
OMEPRAZOLE
1.3.2
Antihistamines
When body comes into contact with whatever the allergic trigger is -pollen, ragweed, pet dander, dust mites, for example -- it makes
taking
decongestant.
Some
drugs
combine
an
Allegra (fexofenadine)
Benadryl (diphenhydramine)
Dimetane (brompheniramine)
Claritin, Alavert (loratadine)
Tavist (clemastine)
Chlor-Trimeton (chlorpheniramine)
Zyrtec (certirizine)
Eyedrops likes Emadine and Livostin treat symptoms of eye allergies,
including itchy, watery eyes. Some medications, like Allegra-D, Claritin-D,
and Zyrtec-D, combine an antihistamine and a decongestant to relieve
congestion.
Side Effects of Antihistamines
Antihistamines can cause side effects, and some cause more side effects
than others. Drugs such as Benadryl, Chlor-Trimeton, and Tavist and
belong to an older group known as "first-generation" antihistamines. They
tend to cause more side effects, particularly drowsiness.
Newer-generation antihistamines such as Allegra, Clarinex, and Zyrtec
and have fewer side effects, so they may be a better choice for some
people.
Some of the main side effects of antihistamines include:
Dry mouth
Drowsiness
Dizziness
Nausea and vomiting
Restlessness or moodiness (in some children)
ALLERGA-D
1.3.3
1.3.3.1
Tranquilizers
Tranquilizers and analgesics are neurologically active drugs. These affect
the message transfer mechanism from nerve to receptor. Tranquilizer is a
drug that acts on the central nervous system and is used to calm,
decrease anxiety, or help a person to sleep. Often called depressants
because they suppress the central nervous system and slow the body
down, they are used to treat mental illness as well as common anxiety
and sleeplessness.
MEPROBAMATE
PHENELZINE (NARDIL)
IPRONIAZID
1.3.3.2
VALIUM
VERONAL
Analgesics
Analgesics reduce or abolish pain without causing impairment of
consciousness, mental confusion, in coordination or paralysis or some
other disturbances of nervous system.
These are classified as follows:
Non-narcotic (non-addictive) analgesics
Aspirin and paracetamol belong to the class of non-narcotic
analgesics. Aspirin is the most familiar example. Aspirin inhibits the
synthesis of chemicals known as prostaglandins which stimulate
inflammation in the tissue and cause pain. These drugs are effective
in relieving skeletal pain such as that due to arthritis. These drugs
have many other effects such as reducing fever (antipyretic) and
preventing platelet coagulation. Because of its anti blood clotting
action, aspirin finds use in prevention of heart attacks.
ASPIRIN
Narcotic drugs
Morphine and many of its homologues like heroin, codeine, when
administered in medicinal doses, relieve pain and produce sleep. In
poisonous doses, these produce stupor, coma, convulsions and
ultimately death. Morphine narcotics are sometimes referred to as
opiates, since they are obtained from the opium poppy. These
analgesics are chiefly used for the relief of postoperative pain,
cardiac pain and pains of terminal cancer, and in child birth.
1.3.4
Antimicrobials
Diseases in human beings and animals may be caused by a variety of
microorganisms such as bacteria, virus, fungi and other pathogens. An
antimicrobial tends to destroy/prevent development or inhibit the
pathogenic action of microbes such as bacteria (antibacterial drugs), fungi
(antifungal
agents),
virus
(antiviral
agents),
or
other
parasites
Antibiotics
Antibiotics are used as drugs to treat infections because of their low
toxicity for humans and animals. Initially antibiotics were classified as
chemical substances produced by microorganisms (bacteria, fungi and
molds) that inhibit the growth or even destroy microorganisms. The
development of synthetic methods has helped in synthesising some of the
compounds
that
microorganisms.
were
Also,
originally
some
purely
discovered
synthetic
as
products
compounds
of
have
The search for chemicals that would adversely affect invading bacteria but
not the host began in the nineteenth century. Paul Ehrlich, a German
bacteriologist, conceived this idea. He investigated arsenic based
structures in order to produce less toxic substances for the treatment of
syphilis. He developed the medicine, arsphenamine, known as salvarsan.
Paul Ehrlich got Nobel prize for Medicine in 1908 for this discovery. It was
the first effective treatment discovered for syphilis. Although salvarsan is
toxic to human beings, its effect on the bacteria, spirochete, which causes
syphilis is much greater than on human beings. At the same time, Ehrlich
was working on azodyes also. He noted that there is similarity in
structures of salvarsan and azodyes. The As = As linkage present in
arsphenamine resembles the N = N linkage present in azodyes in the
sense that arsenic atom is present in place of nitrogen. He also noted
tissues getting coloured by dyes selectively. Therefore, Ehrlich began to
search for the compounds which resemble in structure to azodyes and
selectively bind to bacteria. In 1932, he succeeded in preparing the first
effective antibacterial agent, prontosil, which resembles in structure to the
compound, salvarsan. Soon it was discovered that in the body prontosil is
converted to a compound called sulphanilamide, which is the real active
compound. Thus the sulpha drugs were discovered. A large range of
sulphonamide analogues was synthesised. One of the most effective is
sulphapyridine.
SALVARSAN
PRONTOSIL
SULPHANILAMIDE
AZODYE
Bacteriostatic
Penicillin
Erythromycin
Aminoglycosides
Tetracycline
Ofloxacin
Chloramphenicol
PENCILLIN
CHLORAMPHENICOL
ofloxacin
1.3.4.2
like antibiotics.
Some common antiseptics are
A wide range of different substances are used as disinfectants, including alcohols (also used
as antiseptics), aldehydes, such as ortho-phthalaldehyde, bleaches based on chlorine
compounds, hydrogen peroxide and also iodine (also another traditional antiseptic) and
potassium permanganate solution. Phenolic compounds also have anti-bacterial activity and
are often used in disinfectants bought for use in the home, and in disinfectant hand-washes
and soaps.
Different disinfectants work in different ways. Hydrogen peroxide, which reacts to produce
free oxygen radicals and bleaches that are based on chlorine compounds are very powerful
oxidising agents. They oxidise the complex molecules present on the surface of bacteria,
causing their cell walls and cell membranes to disrupt. The proteins on the surface become
irreversibly damaged and start to stick together forming clumps. This happens very quickly
a strong solution of sodium hypochlorite solution that is used to disinfect a toilet, for
example, kills bacteria within seconds. The bacterial cell cannot respond to the damage
quickly enough and the whole cell simply splits open and dies.
CHLOROXYLENOL
1.3.5
TERPINEOL
BITHIONOL
Antifertility Drugs
Antibiotic revolution has provided long and healthy life to people. The life
expectancy has almost doubled. The increased population has caused
many social problems in terms of food resources, environmental issues,
employment, etc. To control these problems, population is required to be
controlled. This has lead to the concept of family planning. Antifertility
drugs are of use in this direction.
The basic aim of antifertility drugs is to prevent conception or fertilization.
These control the female menstrual cycle and ovulation. The birth control
pills are essentially a mixture of synthetic esterogen and progesterone
derivatives which are more potent than the natural hormones.
It
is
known
progesterone
that
progesterone
derivatives
are
suppresses
more
potent
ovulation.
than
Synthetic
progesterone.
NORETHINDRONE
Mifepristone is
ETHYNYLESTRADIOL (NOVESTROL)
synthetic
steroid
which
blocks
the
effects
MIFEPRISTONE
of