ANALGESIC AND ANTI-INFLAMMATORY AGENTS.pptx

ANALGESIC AND ANTI-
INFLAMMATORY AGENTS
PHARMACEUTICAL CHEMISTRY
D. Pharm 1st year
2022-2023
MISS NIKITA J. BHUTE
Assistant professor
Nagpur college of Pharmacy, Wanadogari,
Higna road, Nagpur 441 110

INDEX
A. Morphine Analogues
1. Morphine
2. Codeine
3. Diamorphine
B. Narcotic Analogues
1. Nalorphine
2. Naloxone
3. Naltrexone
C. Non-steroidal anti-inflammatory agents (NSAIDs)
• Classification
• Chemical name, Chemical structure (compounds marked
with*) Uses, Stability and storage conditions, different types of
formulations and their popular brand names of:
1. Aspirin * 5. Celecoxib
2. Diclofenac 6. Mefenamic Acid
3. Ibuprofen * 7. Paracetamol *
4. Piroxicam 8. Aceclofenac *

Analgesic and anti-inflammatory
agents
• Analgesic and anti-inflammatory agents are the medications used for the
treatment of pain and inflammation.
• Hyperalgesia refers to the enhancement in sensitivity to pain caused by
nociceptors or peripheral nerves. Analgesics are the agents which relieve
the pain by acting selectively on the CNS and peripheral pain mediators
without changing consciousness. Analgesics may be narcotic or non-
narcotic.
• Inflammation is a complex biological response which occurs when the
body is exposed to infective agents or to physical or chemical injury.
Inflammation is of two types such as acute and chronic. Acute
inflammation is short lived and is considered as a positive, protective,
healing and renewing mechanism. On the other hand, chronic
inflammation is not beneficial.

• Morphine analogues are closely related to morphine
structure and are even synthesized from it.
Agonists
(e.g.. morphine,
dimorphine
(heroin), and
codeine)
Partial
agonists
(e.g., nalorphine
and levorphan)
Antagonists
(e.g., naloxone)

1. Morphine
• Chemical name:
(4R, 4aR, 7S, 7aR, 12bS)-3-methyl-2, 4, 4a, 7, 7a, 13-hexahydro-1H-4, 12-
methanobenzofuro[3,2-e] isoquinoline-7,9-diol
• Uses:
1) It is used to relieve moderate to severe pain.
2) It acts on the central nervous system to relieve pain.
• Stability and Storage Conditions:
1) It is stored at room temperature in order to avoid precipitation at low
temperatures and water evaporation at higher temperature.
2) Its exposure to light accelerates decomposition. When exposed to air,
morphine sulfate gradually loses water of hydration. It darkens on
prolonged exposure to light. So, it should be stored in a tightly closed
container at controlled room temperature and protected from freezing and
light.

• Type of Formulation:
1) extended-release oral capsules and tablets
2) Solution
3) Tablets
4) Suppositories
5) injection
• Popular Brand Names:
1) Duramorph
2) Astramorph
3) Infumorph

2. Codeine
• Chemical name:
(5α, 6α)-7, 8-didehydro-4, 5-epoxy-3-methoxy-17- methylmorphinan-6-ol.
• Uses:
1) It is used as an analgesic, antitussive and antidiarrheal agent.
2) It is used to relieve mild to moderately severe pain.
• It effloresces in dry air and is affected by light. So, it should be stored in a
tightly closed container at controlled room temperature and protected from
freezing and light.
1) Each tablet contains 15, 30, or 60 mg of codeine sulfate. The recommended
dose of codeine for pain relief for adults and children over 12 years of age is
15 mg to 60 mg every 4 to 6 hours. The recommended adult dose of codeine
as a cough suppressant is 15 mg to 30 mg every 6 to 8 hours.
1) Codistar
2) Corex

3. Diamorphine
• Chemical name:
(5α,6α)-7,8-didehydro-4,5- epoxy-17-methylmorphinan-3,6-diol diacetate.
• Uses:
1) Used for the treatment of severe pain.
2) It produces it action by binding to opioid receptors in the central nervous
system.
• It is stored in a tightly closed container at controlled room temperature and
protected from light.
1) For acute pain, 5 mg is administered and repeated every four hours if
necessary. In case of chronic pain, 5-10 mg is administered regularly every
four hours by subcutaneous or intramuscular injection. The dose may be
increased according to patient needs.
1) Diagesil
2) Udidyne

B. Narcotic Analogues
• 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,
naloxone, naltrexone and endorphin.

1. Nalorphine
• Chemical name:
(4R,4aR,7S,7aR,12bS)-3-prop-2-enyl-2,4,4a,7,7a,13-hexahydro-1H-4,12-
methanobenzofuro[3,2-e] isoquinoline-7,9-diol.
• Uses:
1) It is used as an antidote to reverse the opioid overdose.
1) It slowly darkens on prolonged exposure to light and air.
2) It is stored in a tightly closed container at controlled room temperature and
protected from light.
1) It is administered through intravenous route with dose of 5 mg twice at three
times intervals.
1) Lethidrone
2) Nalline

2. Naloxone
• Chemical name:
(4R, 4aS, 7aR, 12bS)-4 a ,9-dihydroxy-3-prop-2-enyl-2, 4, 5, 6, 7a, 13-
hexahydro-1H-4, 12-methanobenzofuro[3,2-e]isoquinolin-7-one
• Uses:
1) Used to block or reverse the effects of opioid drugs.
2) It binds to mu-opioid receptors with a high affinity, and a lesser degree to
kappa- and gamma-opioid receptors in the CNS.
1) It is stored at 20 to 25°C and protected from light.
2) It is stored in a tightly closed container.
1) Naloxone Hydrochloride with dose of 400 microgram/ml solution is available
for injection/infusion.
1) Narcan
2) Narcotan
3) Evzio

3. Naltrexone
• Chemical name:
(4R,4aS,7aR,12bS)-3- (cyclopropylmethyl)-4a,9-dihydroxy-2,4,5,6,7a,13-
hexahydro-1H-4,12-methano-benzofur[3,2-e]isoquinolin-7-one.
• Uses:
1) It is prescribed for management of alcoholism and addiction to opioid drugs.
So, it is used to help narcotic dependents who have stopped taking narcotics
to stay drug-free.
1) It is relatively stable at low pH. It is stored at room temperature away from
light and moisture.
1) It is available in scored film-coated tablet containing 50 mg of naltrexone
hydrochloride.
1) Adepend 4)Nalorex
2) Antaxone 5)ReVia
3) Celupan 6)Vivitrol

C. Non-steroidal anti-inflammatory agents
(NSAIDs)
• Non-steroidal anti-inflammatory drugs (NSAIDs) are the
medications that are used to relieve pain, reduce
inflammation and also lower the elevated body temperature.
Membrane phospholipid
COX-2 Selective
NSAIDs
Prostaglandin H₂ (PGH₂)
Peroxidase activity
Prostaglandin G₂ (PGG₂)
Arachidonic acid
Phospholipase A2
COX-2 Non-
selective NSAIDS
PGD ₂ PGE ₂ PGF ₂ α PGI ₂ TXA ₂
COX 2
COX 2
COX 1

Classification of NSAIDs
Class Name of Drugs
(a) Non-selective COX inhibitor Salicylates Aspirin, Diflunisal, Salsalate, Sodium
Salicylate, Salol,Salicylamide,
Benorilate, Choline salicylate.
Anthranillic acid derivatives Mefenamic acid
Aryl acetic acid derivative Diclofenac, Aceclofenac
Propionic acid derivative Ibuprofen
Oxicam derivative Piroxicam, Tenoxicam
Pyrozolone derivative Phenyl butazone, Oxyphenbutazone
Indole Derivatives Indomethacin, Sulindac
Pyrrolo-Pyrrole Derivatives Ketorolac
(b) Preferential COX-2
inhibitors
Nimesulide, Meloxicam, Nabumetone
(c) Selective COX-2 inhibitors Celecoxib, Etoricoxib, Rofecoxib,
Valdecoxib
(d) Analgesic and anti-pyretic Para-amino phenol Paracetamol (Acetaminophen)
Pyrozolone derivative Metamizol (Dipyrone),
Propiphenazone
Benzoxazocine derivative Nefopam

1. Aspirin
• Structure:
• Chemical name:
2-acetoxybenzoic acid
• Uses:
1) Aspirin is used to treat fevers and mild to moderate discomfort associated
with muscle aches, toothaches, the common cold, and headaches.
2) It can also be used to treat pain and swelling associated with arthritis.
3) It reduces pain and swelling by blocking a particular natural chemical in the
body.
4) It is also used to treat Kawasaki disease, pericarditis, and rheumatic fever.
5) Aspirin given shortly after a heart attack to decreases the risk of death.

1) It is stable in dry air but gradually hydrolyzed in contact with moisture to
acetic acid and salicylic acid.
2) It is stored in a cool, dry place at room temperature (20°C to 25°C) in a
sealed container.
3) It is kept away from direct sunlight and moisture.
• Formulations:
1) It is available as tablet with dose of 81mg, 325mg or 500mg. The usual
doses of aspirin for mild to moderate pain are 350 or 650 mg every 4 hours
or 500 mg every 6 hours. The recommended doses for rheumatoid arthritis
include 500 mg every 4-6 hours,650 mg every 4 hours or 1000 mg every 4-6
hours.
• Popular brand names:
1) Asatab 6) Bufferin 11) Vazalore
2) Durlaza 7) Durlaza 12) Arthritis Pain
3) Ecosprin 8) Ecotrin 13) Aspir 81
4) Zorprin 9) Ecpirin 14) Aspi-Cor
5) Bayer Plus 10) Miniprin 15) Aspir-Low

2. Diclofenac
• Chemical name:
2-[2-(2,6-dichloroanilino) phenyl) acetic acid.
• Uses:
1) It is used for the treatment of pain and inflammatory diseases such as arthritis.
2) Rheumatoid and osteoarthritis
3) Bursitis
4) Ankylosing spondylitis
5) Dysmenorrhea
6) Post-traumatic inflammatory conditions
7) Post-operative inflammatory conditions
1) It is stored in a tightly closed container at room temperature away from light
and moisture.
2) Ora-Blend was used to as a suspending and flavoring agent in diclofenac
sodium (10 mg/mL) suspension that is produced from commercially available
diclofenac sodium tablets. This suspension should be stored at room temperature
(23°C) or under refrigeration (5°C) in 60-mL amber PVC prescription bottles.

1) It is administered orally, rectally in a suppository and also used by injection
or applied to the skin.
2) Diclofenac sodium extended-release tablets: 100 mg orally once a day
3) Diclofenac sodium enteric-coated and delayed-release tablets: 25 mg orally
4 times a day.
4) Diclofenac potassium immediate-release tablets: 50 mg orally 3 or 4 times a
day.
5) Diclofenac sodium enteric-coated and delayed-release tablets: 50 mg orally
3 to 4times a day or 75 mg orally twice a day.
6) Parenteral: 37.5 mg IV bolus over 15 seconds every 6 hours as needed for
pain.
7) Capsule
8) Powder
1) Arthrotec 5) Cambia 8) Voltaren-XR
2) Voltaren 6) Voltaren 9) Zipsor
3) Voveran 7) Cataflam 10) Zorvolex
4) Zorvolex

3. Ibuprofen
• Structure:
• Chemical Name:
(RS)-2-(4-(2-methylpropyl) phenyl) propanoic acid.
• Uses:
1) It is used to treat rheumatoid arthritis, juvenile rheumatoid arthritis, and
osteoarthritis symptoms.
2) It can be used to treat mild to severe pain as well as control dysmenorrhea.
3) It can be used as anti-pyretic.
4) It has been used to treat ankylosing spondylitis, gout, and psoriatic arthritis.
5) It may help in reducing pericarditis discomfort, fever, and inflammation.

6) It can be given intravenously with opiates to treat moderate to severe
pain.
7) Ibuprofen lysine can be given intravenously to preterm infants with
patent ductus arteriosus (PDA).
1) It is stored in well closed, light resistant container at 15-30°C
2) It should be kept away from light, moisture and bathroom.
• Types of Formulations:
1) It is available as oral capsule (200 mg)
2) oral suspension (100 mg/5 ml; 50 mg/1.25 ml)
3) oral tablet (100 mg; 200 mg: 400 mg: 600 mg: 800 mg)
4) oral tablet, chewable (100 mg: 50 mg).
1) Advil 4)Motrin
2) Genpril 5) IBU
3) Ibular 6) Motrin IB

4. Piroxicam
• Chemical name:
4-hydroxyl-2-methyl-N-2- pyridinyl-2H-1,2,-benzothiazine-3-
carboxamide-1,1-dioxide.
• Uses:
1) It is used to reduce pain, swelling, tenderness and joint stiffness caused by
Osteoarthritis and rheumatoid arthritis.
1) It is stored in a closed container under dry place below 25°C and is kept
away from light, heat and moisture.
1) For the relief of rheumatoid arthritis and osteoarthritis, the dosage of
piroxicam is 20 mg which is given orally once per day.
2) Capsules
• Popular Brand Names;
1) Axicam
2) Feldene
3) Piroflam

5. Celecoxib
• Chemical name:
4-[5-(4-methylphenyl)-3- (trifluoromethyl)pyrazol-1-yl]benzene
sulfonamide.
• Uses:
1) It is used to relief of the signs and symptoms of osteoarthritis and
rheumatoid arthritis in adults.
2) It is also been allowed to help people with familial adenomatous
polyposis reduce the number of polyps in their intestines.
3) It is also used in:
a) Acute pain and primary dysmenorrhea,
b) Osteoarthritis,
c) Rheumatoid arthritis,
d) Ankylosing spondylitis,
e) Juvenile idiopathic arthritis,
f) Acute pain and dysmenorrhea.

• Stability and Storage Conditions :
1) Store at room temperature between 20°C and 25°C (68°F and 77°F);
excursions between 15°C and 30°C (59°F and 86°F).
2) It is kept away from light and moisture.
1) Adult dose for osteoarthritis: 200 mg orally once daily or 100 mg orally
twice daily.
2) Adult dose for rheumatoid arthritis: 100 to 200 mg orally twice daily.
3) Adult Dose for Ankylosing Spondylitis: 200 mg orally once daily or 100
mg orally twice daily.
4) Capsule
• Popular Brand Names;
1) Celebrex
2) Celecap
3) Celedol
4) Elyxyb

6. Mefenamic Acid
• Chemical name:
2-(2,3-dimethylphenyl) aminobenzoic acid
• Uses:
1) It is used to relieve mild to moderate pain caused by a variety of
disorders in the short term.
2) It can also be used to reduce menstruation pain and blood loss.
3) It is a nonsteroidal anti-inflammatory medication (NSAID).
1) It darkens on prolonged exposure to light.
2) It should be stored between 68°F and 77°F (20°C and 25°C) at room
temperature.
3) It should not be kept in a moist or damp environment, such as a
bathroom.
4) It is kept away from heat, light and moisture.

1) Capsules
2) Tablets
3) Adult initial dose for pain: 500 mg orally once daily.
1) Biospas
2) Dotra-M
3) Lenagesic
4) Ponstel
5) Mefenamic

7. Paracetamol
• Structure:
• Chemical name:
N-(4-hydroxyphenyl) acetamide or N-acetyl-p-aminophenol.
• Uses:
1) It is an over-the-counter analgesic and antipyretic used extensively.
2) It is a traditional remedy for headaches and other mild aches and pains,
and a key element in many cold and flu cures.
3) It can be used in combination with opioid analgesics to treat more severe
pain, like post-surgical pain and palliative care in advanced cancer
patients.

1) It is stored in a cool, dry place, away from direct sunlight.
2) When the temperature is raised from 25 to 45°C, paracetamol tablets
exhibit an increase in disintegration time ranging from 9.1 to 65.5 % (200
mg tablets) and 1.2 to 150.0% (500 mg tablets) (75% RH).
• Formulations:
1) It is available as tablet or syrup.
2) Usual adult paracetamol dose for fever: 500 mg tablets orally every 4 to 6
hours.
3) Usual pediatric dose for fever. Age < 1 month: 10 to 15 mg/kg/dose every
6 to 8 hours and age >1 month to 12 years: 10 to 15 mg/kg/dose every 4 to
6 hours as needed(Maximum: 5 doses in 24 hours).
1) Albimol 5)Cofamol
2) Calpol 6)Panadol
3) Cipmol 7)Tylenol
4) Excedrin

8. Aceclofenac
• Structure:
• Chemical name:
2-[(2-(2-[(2,6-dichlorophenyl)amino]phenyl)acetyl)oxy]acetic acid
• Uses:
1) It is an anti-inflammatory drug that is used to treat pain. Therefore it
is used in rheumatoid arthritis, ankylosing spondylitis, and
osteoarthritis to reduce pain and inflammation.
2) It is an NSAID (Non-Steroidal Anti-Inflammatory Drug).

1) It should be stored in a cool and dry place in an airtight container.
2) It should be kept away from the sunlight and children's reach and sight.
• Formulations:
1) The usual dose of aceclofenac is 100 mg tablet twice daily, taken
preferably morning and evening time.
1) Acerap
2) Aceact
3) Aceroc
4) Acent
5) Abate
6) Abdal
7) Aclonac-SR
8) Acec

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