This presentation is as per ER 2020 for Diploma in Pharmacy Students

1. Analgesic and Anti-
inflammatory Agent
Prepared By Ms. Gunjegaonkar Manjushree B.
Lecture, SJVPM’S Rasiklal M. Dhariwal College of Pharmacy, Chinchwad

2. LEARNING OBJECTIVES
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After completing the chapter, students will be able to:
• To gain basic knowledge about analgesic acid anti-inflammatory
agents.
• To learn pharmaceutical formulations, market preparations, uses and
storage conditions of drugs.

3. Pain
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Pain is the first manifestation of injury to tissue and indicates the onset
or result of disease.
In man, most common forms of pain are headache, neuralgia, chronic
arthritis, dysmenorrhea, labour pain, pain of cardiac muscle, visceral
pain, pressure origin pain etc. Visceral pain (e.g. appendicitis, spasm,
coronary thrombosis, peptic ulcer etc.) is not well localized but somatic
pain (e.g. pain in muscle, joints, ligaments, tendon, skin etc.) is better
localized.
Hence, analgesics are used to get relief from pain.

4. Pain
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Analgesics can be categorized as:
1. True analgesics or narcotic analgesics or opioid analgesics,
2. Antipyretic analgesics or non-narcotic analgesics or febrifuges.
The drugs which decrease sensitivity (awareness) of pain by depressing
of consciousness are called analgesics (true analgesics).

5. Pain
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• These drugs increase the capacity to tolerate pain i.e. increase pain
threshold.
• As these drugs induce sleep (which does not resemble natural sleep)
i.e. produce narcosis along with analgesic effect, they are called
narcotic analgesics (The word 'narcotic' is derived from Greek word
'narkoun' which means drowsiness).
• The first narcotic analgesic discovered was morphine, an alkaloid,
which was isolated from opium.
Hence, analgesics are also called opioids or opiate analgesics.

6. Narcotic analgesics are classified as
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A. Naturally occurring:
1. Morphine & its analogues: e.g. morhine, codiene.
B. Totally synthetic drugs:
1. Morphinan analogues: e.g. levorphanol.
2. Benzomorphan analogues: e.g. pentazocin
3. 4-phenylpiperidine analogues: e.g. pethidine
4. Phenylpropylamine analogues: e.g. methadone,
dextropropoxyphene

7. Narcotic analgesics are classified as
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Narcotic analgesics are mainly used to relieve moderate to severe
pain.
They are also used to suppress non-productive cough (antitussive), to
induce sleep in the presence of pain, to control diarrhoea.
Their use is limited due to
(i) Addictive property.
(ii) Respiratory depression.
(iii) Decrease in gastro-intestinal motility leading to constipation

8. Narcotic analgesics are classified as
8
Narcotic analgesics are mainly used to relieve moderate to severe
pain.
They are also used to suppress non-productive cough (antitussive), to
induce sleep in the presence of pain, to control diarrhoea.
Their use is limited due to
(i) Addictive property.
(ii) Respiratory depression.
(iii) Decrease in gastro-intestinal motility leading to constipation

9. Antipyretics-analgesics or febrifuges
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Pyrexia is a condition where body temperature has been raised above normal.
Antipyretics: the drugs which lower the raised temperature & bring it to
normal are called antipyretics.
They differ from narcotic features:
(1) They have low activity in normal dose.
(2) Their large dose will not relieve severe or prolonged pain.

10. Antipyretics-analgesics or febrifuges
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Analgesics can be categorized as :
1. True analgesics or narcotic analgesics or opioid analgesics.
2. Antipyretic analgesics or non-narcotic analgesics or febrifuges.
True analgesics: the drugs which decrease sensitivity (awareness) of pain by
depressing CNS without loss of consciousness are called analgesics (true
analgesics).
Narcotic analgesics: the drugs which induce sleep (does not resembles to
natural sleep) i.e. produces narcosis along with analgesic effect are called
as narcotic analgesics.

11. Antipyretics-analgesics or febrifuges
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Analgesics can be categorized as :
1. True analgesics or narcotic analgesics or opioid analgesics.
2. Antipyretic analgesics or non-narcotic analgesics or febrifuges.
True analgesics: the drugs which decrease sensitivity (awareness) of pain by
depressing CNS without loss of consciousness are called analgesics (true
analgesics).
Narcotic analgesics: the drugs which induce sleep (does not resembles to
natural sleep) i.e. produces narcosis along with analgesic effect are called
as narcotic analgesics.

12. Antipyretics-analgesics classification
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Antipyretic analgesics may be classified on the basis of their chemical
Structure
1. Aniline and p-aminophenol derivatives. e.g. Acetanilide, Paracetamol
2. Salicylic acid derivatives e.g. Aspirin.
3. Pyrazole derivatives e.g. Analgin, Antipyrine

13. Morphine Sulphate
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It is the principal alkaloid obtained from opium ( the partly dried latex from
incised unripe seed capsules of papaver somniferum). It belongs to
phenanthrene class of alkaloid. It contains morphinan heterocycle.
Stability & storage:
affected by light. Hence stored in well-closed, light-resistant containers.

14. Morphine Sulphate
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Uses :
1. For control of moderate to severe, acute & chronic pain associated with
neoplasm.
2. As a premedication prior to surgery (due to claiming & sedative
property).
3. To suppress responses to intra-operative surgical stimuli.
4. To treat diarrhoea (to reduce G.I. peristaltic activity).
5. To suppress cough.
6. To relieve dyspnea of left ventricular failure & of pulmonary oedema.
7. As a hypnotic when insomnia is due to pain.
8. To alleviate (relieve) anxiety due to pain.
9. As an adjunct to anaesthetics for pain relief & to allay (reduce) anxiety.

15. Morphine Sulphate
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Pharmaceutical formulation:
i. Morphine Injection
ii. Morphine & atropine Injection
iii. Morphine & ammonium chloride mixture
iv. Morphine & ipecacuanha mixture
v. Morphine & kaolin mixture
vi. Morphine & hydrochloride solution
vii. Morphine suppositories.
Brand names: zephrol, cherana, Morcotin, Rilimorf,
Duramorph, Astramorph, Inumorph

16. Morphine Sulphate
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Pharmaceutical formulation:
i. Morphine Injection
ii. Morphine & atropine Injection
iii. Morphine & ammonium chloride mixture
iv. Morphine & ipecacuanha mixture
v. Morphine & kaolin mixture
vi. Morphine & hydrochloride solution
vii. Morphine suppositories.
Brand names: zephrol, cherana, Morcotin, Rilimorf, Duramorph,
Astramorph, Inumorph

17. Codeine
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It is also isolated from opium. It differs from morphine in having methoxy
group instead of hydroxy group at position 3
Stability & storage:
It effloresces slowly in dry air & is affected by light.
Uses :
1. To suppress cough
2. To treat diarrhoea
3. To suppress mild to moderate pain
4. As a sedative & hypnotic
5. Commonly used in combination with aspirin.

18. Codeine
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Dosage forms:
1. Codeine phosphate tablets
2. Codeine & paracetamol tablets
3. Codeine & aspirin tablets
4. Codeine phosphate syrup
5. Codeine phosphate linctus
6. A.P.C tablet (B.P.)
Brand names:
glycodin terp vasaka, cosaka, powerin, kefex.

19. Codeine
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Dosage forms:
1. Codeine phosphate tablets
2. Codeine & paracetamol tablets
3. Codeine & aspirin tablets
4. Codeine phosphate syrup
5. Codeine phosphate linctus
6. A.P.C tablet (B.P.)

20. NARCOTIC ANTAGONISTS
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• Narcotic antagonists are the class of drugs which block the euphoric effects
of opiates by attaching to the opioid receptor.
• The examples of narcotic antagonists are nalorphine, maloxone, naltrexone
and endorphin.
• These are used therapeutically as antidote to treat verdose associated with
opioid analgesics.

21. Naltrexone Hydrochloride
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• It is a narcotic antagonist that is effective orally, longer lasting and more
potent than naloxone, and has been proposed for the treatment of heroin
addiction.
• Storage: Store protected from light and moisture.

22. Naltrexone Hydrochloride
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Uses:
• Used in following conditions:
• (i)Alcohol Dependency
• (ii) Cholestatic pruritus
• (iii) Obesity (Disorder)
• (iv) Opioid Dependence
• (v) Severe Pain

23. Naltrexone Hydrochloride
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Pharmaceutical Formulations:
(i) Naltrexone Hydrochloride Tablets.
(ii) Naltrexone Tablets LP.
(iii) Naltrexone Implantable Pellet.
Brand Name:
Contrave, Embeda, Vivitrol, Naltima, Antaxone, Nalorex, Revia, Vivitrol,
Adepend

24. Non steroidal Anti-inflammatory Agents (NSAIDS)
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The drugs which are used to reduce inflammation, & pain arising from it are
called as anti-inflammatory agents.

25. Non steroidal Anti-inflammatory Agents (NSAIDS)
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Classification:
1. Salicylic acid derivative: e.g. aspirin
2. N-aryl anthranilic acid derivative or fenamates: e.g. mefenamic acid
3. Indolyl or aryl acetic acid derivatives: e.g. indomethacin (indole
derivative), ibuprofen (aryl acetic acid derivative)
4. Pyrazole derivatives:
a) 5-pyrazolone (3-pyrazolin-5-one) derivative: e.g. analgin
b) Pyrazolidine-3-5 dione: e.g. phenylbutazone, oxyphenbutazone.

26. Aspirin (acetyl salicylic acid)
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Structure:
Chemical name: o-acetoxy benzoic acid.

27. Aspirin (acetyl salicylic acid)
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Stability & storage:
stable in air but is slowly hydrolyzed in presence of moisture. Hence stored in
tightly-closed containers.
Uses :
1. For relief of mild to moderate pain like headache, toothache, myalgia.
2. As an antipyretic.
3. In chronic disease accompanied by pain & inflammation e.g. rheumatoid
arthritis.
4. To treat gout
5. In high doses, to reduce risk of myocardial infarction.

28. Aspirin (acetyl salicylic acid)
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Dosage forms:
1. Aspirin tablets
2. Soluble aspirin tablets
3. Aspirin & caffeine tablets
4. Dispersible aspirin & caffeine tablets
Brand name:
Aspro, anacin, coldarin, mejoral, powerin, codopyrin.

29. Paracetamol ( acetaminophen):
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Structure:
Chemical name: p-hydroxy acetanilide or p-acetamido phenol or N-acetyl, p-
aminophenol.

30. Paracetamol ( acetaminophen)
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Stability & storage: stored in well-closed, light-resistant containers.
Uses :
1. As antipyretic
2. As an analgesic for relief of pain such as headache, toothache, neuralgia,
rheumatism, etc.
Dosage forms:
Tablets, Elixirs, Pediatric syrup, Infusion, Pediatric oral Suspension

31. Paracetamol ( acetaminophen)
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Brand names: Crocin, Metacin, Calpol, Paramol, Ibuplus

32. Diclofenac Sodium
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 Diclofenac is associated with a hepatotoxicity risk, particularly when used
in high doses.
 Diclofenac can be administered topically, as well as orally.
 The risk of hepatotoxicity f topical formulations is lower since first pass
extraction into the liver is avoided.
 Diclofenac are slightly less potent than indomethacin.
 Transdermal formulations diclofenac sodium Analgesics and Anti
Inflammatory Agents are applied directly, to arthritic and/or inflammed
joints.
 Ophthalmic solutions of diclofenac sodium are available,

33. Diclofenac Sodium
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Storage:
It is stored in well-closed containers protected from moisture and light.
Uses:
(i) For short- and long term treatment of rheumatoid arthritis.
(ii) It is used in the treatment of osteo arthritis and ankylosing spondylitis.
(iii) To treat postoperative ocular inflammation or ocular pain.
(iv) Diclofenac is among the most extensively used NSAID; employed in
toothache, dysmenorrhoea,
(v) To treat renal colic, posttraumatic and postoperative inflammatory
conditions.
(vi) To afford quick relief of pain and wound edema.

34. Diclofenac Sodium
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Pharmaceutical Formulations :
(i) Diclofenac prolong release tablets I.P.
(ii) Diclofenac gastro resistant tablet I.P.
(iii) Diclofenac gel I.P.
(iv) Diclofenac injection I.P.
Brand Name:
Voltaren, Voltaflam, Cataflam, Arthrotec, Voveran,
Diclonac, Movonac, Diclomax and

35. Aceclofenac
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Aceclofenac potently inhibits the cyclo-oxygenase enzyme (COX) that is
involved synthesis of prostaglandins, which are inflammatory mediators that
cause pain,inflammation, and fever.
A moderately COX-2 selective congener of diclofenac similar properties.
Uses :Used to treat
(i) Ankylosing Spondylitis (AS)
(ii) Osteoarthritis (OA)
(iii) Rheumatoid Arthritis

36. Aceclofenac
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Pharmaceutical Formulations :
(i) Aceclofenac tablet I.P.
(ii) Aceclofenac SR tablet.
Brand Names:
Aceclo, Dolokind and Clanza.

37. Ibuprofen
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Structure:
Chemical Name : (RS)-2-(4-isobutyl phenyl) propionic acid.

38. Ibuprofen
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Storage:
It is stored in well-closed containers protected from moisture and light at
temperature
Uses:
1. Rheumatoid arthritis
2. Oestoarthritis
3. Ankylosing spondylitis
4. Dysmenorrhoea
5. Acute musculo-skeletal disorders such as fibrositis, lumbago, neck pain,
myalgia, etc.

39. Ibuprofen
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Pharmaceutical Formulations :
Ibuprofen tablets I.P.
Ibuprofen gel I.P.
Ibuprofen cream I.P.
Brand Names:
Brufen, ibugesic, Acife, Emflam,
Ibular, Genpril

40. Piroxicam
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Piroxicam is the most widely used oxicam because of its once-daily dosing
schedule.
Oxicams, are first-generation NSAIDs that lack a free carboxylic acid side
chain.
Piroxicam and meloxicam have nearly identical structural features but also have
at least a nine fold difference in selectivity for meloxicam to COX-2 isozyme
and an even larger difference in their relative risks for GI complications (i.e.,
Piroxicam has the highest risk among NSAIDs, whereas meloxicam has very
little or no such side effects

41. Piroxicam
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Uses :
(i) Used as analgesic and antipyretic.
(ii) Used as long-term anti-inflammatory drug in rheumatoid.
(iii) It has also been used for acute gout.
(iv) It is used in the treatment of musculoskeletal injuries and in dentistry.
Pharmaceutical Formulations :
(i) Piroxicam Tablets I.P.
(ii) Piroxicam Capsules I.P.
(iii) Piroxicam Injections
(iv) Piroxicam Gel

42. Piroxicam
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Brand Names:
Feldene, Piricam, Dolonex, Pirox, Minicam and Movon.

43. Celecoxib
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• It exerts anti-inflammatory, analgesic and antipyretic actions, with low
ulcerogenic potential into the market for use in the treatment of RA, OA,
acute pain, and menstrual pain.
• The real benefit is that it has caused fewer GI complications, when compared
with other conventional NSAIDs.
• Analgesics and Anti-Inflammatory Agents of pain medications, especially for
arthritic patients who are at higher risk of serious GI complications.
Storage:
• It is stored in well-closed containers protected from moisture and light

44. Celecoxib
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• Uses:
(i)Celecoxib's primary use is as an anti-inflammatory agent in osteo and
rheumatoid arthritis,
(ii) It is used for celecoxib in the prevention of lung and colorectal cancers.
(iii) Celecoxib is not a substitute for aspirin for cardiovascular event prophylaxis.
(iv) It may also be used to treat acute pain from various sources, juvenile
rheumatoid arthritis in childrens
(v) It is used to treat ankylosing spondylitis and primary dysmenorrhea
Pharmaceutical Formulations :Celecoxib Capsule.

45. Celecoxib
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Brand Names:
• Celebrex,
• Celecap,
• Celedol,
• Celact,
• Revibra and
• Colcibra

46. Mefenamic Acid
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• Mefenamic acid, an anthranilic acid derivative, is a member of the fenamate
group of non-steroidal anti-inflammatory drugs (NSAIDs).
• It exhibits anti-inflammatory, analgesic, and antipyretic activities.
• Similar to other NSAIDs, Mefenamic acid inhibits prostaglandin synthetase.
• Storage: Affected by light. So store in closed container at room temperature.
It is kept away from heat, light and Moisture.

47. Mefenamic Acid
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• Uses : For the treatment of:
• (i) Rheumatoid arthritis.
• (ii) Osteoarthritis.
• (iii) Inflammation and fever.
• (iv) For mild to moderate pain and for primary dysmenorrhea.
• Pharmaceutical Formulations :Mefenamic Acid Capsules.
• Brand Names: Ponstel, Ponstan and Mefenamic, Bipas, Dotra-M.

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