Drugs and their Classification :- Drugs are chemicals of low molecular masses (~100 – 500u). These interact with macromolecular targets and produce a biological response. When the biological response is therapeutic and useful, these chemicals are called medicines and are used in diagnosis, prevention and treatment of diseases. Use of chemicals for therapeutic effect is called chemotherapy .
Classification of Drugs:- (a) On the basis of pharmacological effect :- Analgesics have pain killing effect . Antiseptics kill or arrest the growth of microorganisms. Antipyretic reduce body temperature.
(b) On the basis of drug action:-based on the action of a drug on a particular biochemical process.
All Antihistamines inhibit the action of the compound, histamine which causes inflammation in the body.
(c) On the basis of chemical structure-sulphonamides have common structural feature,
(d) On the basis of molecular targets:-
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.
Substrates bind to the active site of the enzyme through a variety of interactions such as ionic bonding, hydrogen bonding, van der Waals interaction or dipole-dipole interaction .
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The second function of an enzyme is to provide functional groups that will attack the substrate and carry out chemical reaction.
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.
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Some drugs do not bind to the enzyme’s active site. These bind to a different site of enzyme which is called allosteric site. This binding of inhibitor at allosteric site changes the shape of the active site in such a way that substrate cannot recognise it.
Receptors as Drug Targets :-Receptors are proteins that are crucial to body’s communication process. Majority of these are embedded in cell membranes.
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.
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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.
Antacids :-Until 1970, only treatment for acidity was administration of antacids, such as sodium hydrogencarbonate or a mixture of aluminium and magnesium hydroxide. However, excessive hydrogencarbonate can make the stomach alkaline and trigger the production of even more acid.
Histamine, stimulates the secretion of pepsin and hydrochloric acid in the stomach . The drug cimetidine (Tegamet), was designed to prevent the interaction of histamine with the receptors present in the stomach wall. This resulted in release of lesser amount of acid. The importance of the drug was so much that it remained the largest selling drug in the world until another drug, ranitidine (Zantac), was discovered.
Antihistamines :-Histamine is a potent vasodilator. It has various functions. It contracts
the smooth muscles in the bronchi and gut and relaxes other muscles, such as those in the walls of fine blood vessels. Histamine is also responsible for the nasal congestion associated with common cold and allergic response to pollen .
Synthetic drugs, brompheniramine (Dimetapp) and terfenadine (Seldane),act as
antihistamines. They interfere with the natural actionof histamine by competing with histamine for binding sites of receptor where histamine exerts its effect.
Tranquilizers :-Tranquilizers and analgesics are neurologically active drugs. These affect the message transfer mechanism from nerve to receptor.
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Tranquilizers are a class of chemical compounds used for the treatment of stress, and mild or even severe mental diseases. These relieve anxiety, stress, irritability or excitement by inducing a sense of well-being. They form an essential component of sleeping pills.
There are various types of tranquilizers:-
a) Noradrenaline is one of the neurotransmitters that plays a role in mood changes. If the level of noradrenaline is low for some reason, then the signal-sending activity becomes low, and the person suffers from depression . In such situations, antidepressant drugs are required. These drugs inhibit the enzymes which catalyse the degradation of noradrenaline .These drugs inhibit the enzymes which catalyse the degradation of noradrenaline.Iproniazid and Phenelzine are two such drugs.
b) Some tranquilizers namely, chlordiazepoxide and meprobamate, are relatively mild
tranquilizers suitable for relieving tension. Equanil is used in controlling depression and hypertension.
c) Derivatives of barbituric acid viz., veronal, amytal, nembutal, luminal and seconal constitute an important class of tranquilizers. These derivatives are called Barbiturates. Barbiturates are hypnotic, i.e., sleep producing agents. Some other substances used as tranquilizers are valium and serotonin.
Analgesics:-Analgesics reduce or abolish pain without causing impairment of consciousness,
mental confusion, incoordination or paralysis or some other disturbances of nervous system. These are classified as follows: (i) 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.
(ii) Narcotic drugs :-Morphine and many of its homologues, when administered in medicinal doses, relieve pain and produce sleep. In poisonous doses, these produce stupor, coma, convulsions and ultimately death.
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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.
Antimicrobials :-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 (antiparasitic drugs) selectively.
Antibiotics, antiseptics and disinfectants are antimicrobial drugs.
(a) Antibiotics:-Initially antibiotics were classified as chemical substances produced by
microorganisms (bacteria, fungi and molds) that inhibit the growth or even destroy microorganisms.
Some purely synthetic compounds have antibacterial activity, and therefore, definition of antibiotic has been modified.
An antibiotic now refers to a substance produced wholly or partly by chemical synthesis,
which in low concentrations inhibits the growth or destroys microorganisms by intervening in their metabolic processes.
Sulpha drugs or sulphanilamide were discovered by Paul Ehrlich. A large range of
sulphonamide analogues was synthesised.
Antibiotics have either cidal (killing) effect or a static (inhibitory) effect on microbes. A few examples of the two types of antibiotics are as follows:-
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Antibiotics which kill or inhibit a wide range of Gram-positive and Gram-negative bacteria are said to be broad spectrum antibiotics. Those effective mainly against Gram-positive or Gram- negative bacteria are narrow spectrumantibiotics. Penicillin G has a narrow spectrum. Ampicillin and Amoxycillin are synthetic modifications of penicillins. These have broad spectrum.
(b) Antiseptics and disinfectants :-Antiseptics are applied to the living tissues such as wounds, cuts, ulcers and diseased skin surfaces. Examples are furacine, soframicine, etc. These are not ingested like antibiotics.
Commonly used antiseptic, dettol is a mixture of chloroxylenol and terpineol. Bithionol
(the compound is also called bithional) is added to soaps to impart antiseptic properties.
Iodine is a powerful antiseptic. Its 2-3 per cent solution in alcohol water mixture is known as Tincture of iodine. It is applied on wounds. Iodoform is also used as an antiseptic for wounds.
Boric acid in dilute aqueous solution is weak antiseptic for eyes.
Disinfectants are applied to inanimate objects such as floors, drainage system, instruments, etc. Same substances can act as an antiseptic as well as disinfectant by varying the concentration. For example, 0.2 per cent solution of phenol is an antiseptic while its one percent solution is disinfectant. Chlorine in the concentration of 0.2 to 0.4 ppm in aqueous solution and sulphur dioxide in very low concentrations, are disinfectants.
Antifertility Drugs :- Birth control pills essentially contain a mixture of synthetic estrogen and progesterone derivatives. Both of these compounds are hormones. It is known that progesterone suppresses ovulation.
Synthetic progesterone derivatives are more potent than progesterone. Norethindrone is an
example of synthetic progesterone derivative most widely used as antifertility drug.
The estrogen derivative which is used in combination with progesterone derivative is
ethynylestradiol (novestrol).
Chemicals in Food Chemicals are added to food for (i) their preservation, (ii) enhancing their appeal, and (iii) adding nutritive value in them. Main categories of food additives are as follows: (i) Food colours (ii) Flavours and sweeteners
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(iii) Fat emulsifiers and stabilising agents
(iv) Flour improvers - antistaling agents and bleaches (v) Antioxidants (vi) Preservatives (vii) Nutritional supplements such as minerals, vitamins and amino acids. Artificial Sweetening Agents :- Ortho-sulphobenzimide, also called saccharin, is the first popular artificial sweetening agent. It is about 550 times as sweet as cane sugar.
Aspartame is the most successful and widely used artificial sweetener. It is roughly 100 times as sweet as cane sugar.. Use of aspartame is limited to cold foods and soft drinks because it is unstable at cooking temperature.
Alitame is high potency sweetener, although it is more stable than aspartame, the control of sweetness of food is difficult while using it.
Sucralose is trichloro derivative of sucrose. Its appearance and taste are like sugar. It is stable at cooking temperature. It does not provide calories.
Food Preservatives :-The most commonly used preservatives include table salt, sugar, vegetable oils and sodium benzoate, C6H5COONa. Sodium benzoate is used in limited quantities and is metabolised in the body. Salts of sorbic acid and propanoic acid are also used as preservatives.
Nitarte and Nitite—Meat product.
BHA and BHT---Anti-Oxidants in food.
Cleansing Agents SOAP :-Soaps are the detergents used since long. Soaps used for cleaning purpose are sodium or potassium salts of long chain fatty acids, e.g., stearic, oleic and palmitic acids. Soaps containing sodium salts are formed by heating fat (i.e., glyceryl ester of fatty acid) with aqueous sodium hydroxide solution. This reaction is known as saponification.
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Only sodium and potassium soaps are soluble in water and are used for cleaning purposes. Generally potassium soaps are soft to the skin than sodium soaps .
In medicated soaps, substances of medicinal value are added. In some soaps, deodorants are added. Shaving soaps contain glycerol to prevent rapid drying. A gum called, rosin is added while making them. It forms sodium rosinate which lathers well. Laundry soaps contain fillers like sodium rosinate, sodium silicate, borax and sodium carbonate.
Why do soaps not work in hard water?
Hard water contains calcium and magnesium ions. These ions form insoluble calcium and magnesium soaps respectively when sodium or potassium soaps are dissolved in hard water.
These insoluble soaps separate as scum in water and are useless as cleansing agent. In fact these are hinderance to good washing, because the precipitate adheres onto the fibre of the cloth as gummy mass. Hair washed with hard water looks dull because of this sticky precipitate.
Synthetic Detergents :- Synthetic detergents are cleansing agents which have all the propertiesof soaps, but which actually do not contain any soap. These can be used both in soft and hard water as they give foam even in hard water.
Synthetic detergents are mainly classified into three categories: (i) Anionic detergents (ii) Cationic detergents and (iii) Non-ionic detergents
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Anionic Detergents: Anionic detergents are sodium salts of sulphonated long chain alcohols or hydrocarbons. Alkyl hydrogensulphates formed by treating long chain alcohols with concentrated sulphuric acid are neutralised with alkali to form anionic detergents. In anionic detergents, the anionic part of the molecule is involved in the cleansing action. Sodium salts of alkylbenzenesulphonates are an important class of anionic detergents. They are mostly used for household work. Anionic detergents are also used in toothpastes.
Cationic Detergents: Cationic detergents are quarternary ammonium salts of amines with acetates, chlorides or bromides as anions. Cationic part possess a long hydrocarbon chain and a positive charge on nitrogen atom. Hence, these are called cationic detergents. Cetyltrimethylammonium bromide is a popular cationic detergent and is used in hair conditioners.
Cationic detergents have germicidal properties and are expensive, therefore, these are of limited use.
Non-ionic Detergents: Non-ionic detergents do not contain any ion in their constitution. One such detergent is formed when stearic acid reacts with polyethyleneglycol.
Main problem that appears in the use of detergents is that if their hydrocarbon chain is highly branched, then bacteria cannot degrade . Slow degradation of detergents leads to their accumulation. Effluents containing such detergents reach the rivers, ponds, etc.They persist in water even after sewage treatment and cause foaming in rivers, ponds and streams and their water gets polluted.
