1. Analgesics
Drugs which relive pain by acting on the central nervous system
and reduce without loss of consciousness
They are of two types:
*Narcotic Analgesics
*Non-narcotic Analgesics.
Non-narcotic Analgesics: Don’t produce significant depression of
the central nervous system. e.g.salicylates and related compounds
Narcotic Analgesics: Produce depression of the central nervous
system.
Classified into
*Natural Analgesics e.g.morphine,codeine etc
*Synthetic Analgesics e.g. pethidine,methadone etc
2. NARCOTIC ANALGESICS
Naturally Occurring:
Morphine
opium alkaloid obtained from papaver somniferum
morphine is generally used as sulphate and hydrochloride
structure of morphine-isoquinoline alkaloid
solutions of morphine are sterilized at 98-100 for 30 min with
bactericide.
3. Analgesic action
powerful analgesic
relief from pain without altering the functions of the central nervous system.
does not lead to abnormal behavior.
large doses can relive all types of pain.
increases the threshold of the pain
does not remove pain completely but helps to tolerate the pain.
induces analgesia by acting on the receptors situated both in the higher
centers and spinal cord.
produces depression of respiration and miosis.
Uses
analgesic for reliving the pain
used to reduce pain in acute myocardial infraction, burns, fractures of bones,
pleurisy etc.
administered intravenously
used to reduce post operative pain.
it shows sedative effect
used as a premedication for surgery.
4. .
Disadvantage
invaluable in the treatment of pulmonary-edema
drug of addiction due to euphoriant effect
over dose causes poisoning
causes dryness of mouth, mental clouding, dysphoria, vomiting,
headache, fatigue, constipation etc.
5. Codeine
White crystalline powder
sparingly soluble in water
bitter in taste
less potent analgesic than morphine
better absorbed when administered orally
6. SYNTHETIC ANALGESICS
Some important synthetic morphine substitutes are:
1. Pethidine.
2. Methadone.
Pethidine
• White crystalline substance.
• Bitter taste.
• Forms salts with acid.
• Action is similar to Morphine.
• Powerful analgesic in short duration of action
• Used in respiratory depressant like morphine.
• For treatment of shock.
• Used in place of morphine as an analgesic in
myocardial infarction.
7. Methadone
Synthetic compound.
Slightly potent than morphine.
Available as Methadone Hydrochloride tablet doses 5 to 10mg.
Also available in ampoules in injection form.
Is a racemic mixture.
Used as a substitute for Morphine and Pethidine.
Gives relief from visceral pain.
As respiratory depressant.
8. Morphinan
.
syntheticanalgesics
example of morphinan compound is levorphanol
potent than morphine
well absorbed when administered orally
Benzomorphan
Potent than morphine
synthetic agent
used intramuscularly in the dose 2 to 3 mg
9. .
Salicyclic acid
The derivative of Salicyclic acid is analgesic and has antipyretic action.
The most important drugs are Aspirin, Sodium salicylate, salicin, etc.
10. .
Asprin
It’s also known as Acetyl salicyclic acid.
• Obtained by acetylation of Salicyclic acid.
• White crystalline, odorless powder.
• Sparingly soluble in water.
• Slight acid taste.
• In the presence of moisture, it gets hydrolyzed to
acetic acid & salicyclic acid.
• Stored in airtight containers.
• Stable in dry conditions.
• Used as analgesic in case of mild pain.
• Has antipyretic action.
• Used in headaches, cold, arthritis, toothache, etc.
• Used as anti-inflammatory agent.
• Reduces edema, tissue swelling, etc.
• Used as antirheumatic drug.
• Reliefs from signs and symptoms of inflammation.
• Has shown beneficial effect in radiation diarrhea.
11. Methyl salicylate
.
(Oil of winter green)
• Chemically it is O-hydroxy benzoate.
• Colourless pale yellow liquid.
• Slightly soluble in water.
• Has sweet taste and aromatic odor.
• Used for topical application.
• Methyl salicylate ointment is made in
white bees wax and hydrous wool fat.
• Flavoring agent.
• Used as analgesic in sciatica, rheumatic,
etc.
12. .
Sodium salicylate
Colourless small crystals or crystalline powder.
• Unpleasant taste
• Soluble in water.
• Taken in a mixture form with alkali.
• Used for integumental pain and acute rheumatic fever.
13. Salicin
• Obtained from bark of willows.
• Synthesized by the action of acetobromo-glucose and
Salicylaldehyde.
• Used in rheumatic pain and fever.
14. .
Diethylamine Salicylate
• It is a diethyl amine salt of salicylic acid.
• White crystalline substance.
• Topically used.
• Available as creams.
• Used in rheumatic and muscular pain.
15. .
The Para-aminophenol derivatives
Analgesic and antipyretic effects.
Not useful anti-inflammatory drugs.
Commonly used drugs are Phenacetin and para-acetamol.
Para acetamol
• Chemically it is 4-hydroxy Actanilide.
• White crystalline powder.
• Is odourless ans highly soluble in water.
• Daily dosage should not exceed 2.5% in adults.
• More potent antipyretic than Phenacetin.
• Used for relief of pain and fever.
• Shows adverse effect are sweating, nausea, vomiting, etc.
16. .
Phenacetin
• White odourless, crystalline powder.
• Sparingly bitter in taste.
• Prepared from p-nitrophenol.
• Used with aspirin for relief of integumental pain.
• Phenacetin is hydrolyzed to paracetamol and this is the cause for
antipyretic-analgesic action.
17. .
Indolyl and aryl acetic acid derivatives
Important drugs are Indomethacin and Sulindae
Indomethacin
• Chemically it is named as 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-3
indolylacetic acid.
• It is an indole acetic acid derivative.
• Brownish yellow crystalline powder.
• Insoluble in water.
• Soluble in organic solvents.
• Available as 25 mg capsules.
• Has an inflammatory, analgesic and antipyretic action.
• Effective in rheumatic disorders.
• Useful in treatment of gout.
• Some adverse effects are nausea, vomiting, skin rashes, diarrhea, etc.
18. Sulindae
• Chemically it is named as [5-fluoro-2 methyl-1 (4-methyl
sulphinyl-benzylidene) inden-3 yl] acetic acid.
• It is a fluorinated derivative of indomethacin.
• Yellow crystalline powder.
• Insoluble in water.
• Has longer duration of action than indomethacin.
• Used in the treatment of rheumatic and musculo-skeletal
disorders.