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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
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.
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.
.




    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.
Codeine



   White crystalline powder
   sparingly soluble in water
   bitter in taste
   less potent analgesic than morphine
   better absorbed when administered orally
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.
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.
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
.




                              Salicyclic acid
       The derivative of Salicyclic acid is analgesic and has antipyretic action.
    The most important drugs are Aspirin, Sodium salicylate, salicin, etc.
.




                             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.
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.
.




                        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.
Salicin

• Obtained from bark of willows.
• Synthesized by the action of acetobromo-glucose and
  Salicylaldehyde.
• Used in rheumatic pain and fever.
.




                             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.
.




                    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.
.




    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.
.




    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.
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.

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Analgesics

  • 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.