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ANTI INFLAMMATORY
DRUGS
Dr.s.Vinodhini
Department of Pharmacology
Perception of painful stimulus Nociception (termed by
Sherrington)
consciousness
CYCLOOXYGENASE PATHWAY
Classification
A) Non selective COX inhibitors/ conventional NSAIDS
1) Salicylates - Aspirin* , Diflumisal
Sensitise Afferent N
Pain
Pyrogens +IL
Interferons+ INF-α
Fever
3) Anti inflammatory action
NSAID inhibits
PG secretion
ECAM-1 ICAM-1
Selectins & Integrins
4) Antithrombotic activity
NSAIDS TXA2 Proaggregatory
PGI2 Antiaggregatory
6) Dysmenorrhoea
2) Bleeding
3) Limitation of renal blood flow
Tubular reabs
6) Hepatic damage
NSAIDS raises transaminase hepatic failure
7) CNS Manifestations
Headache, mental confusion, behavioural disturbances, seizures
precipitation
Aspirin
Pharmacological action
1) Analgesic, antipyretic, anti-inflammatory, antiplatelet
3) Respiratory failure
- At anti-inflammatory doses Resp. stimulated
- At higher doses Resp. depression Resp. failure
6) GIT
Nausea vomitting & epigastric distress (irritation & CTZ)
Back diffussion of gastric acid
Occult blood loss
7) Urate excretion
• Elimination = urine
Adverse Effects
1) Gastric mucosal damage & peptic ulceration
2) Hypersensitivity and idiosyncrasy
3) At Anti inflammatory dose (3-6 gm/day)
- Salicylism syndrome
- Liver Damage
4) Reye’s syndrome = Hepatic encephalopathy in children having
viral infection
5) Acute salicylate poisoning
- Dose in adults 15-30 gm
- Serious toxicity at serum levels > 50 mg / dl
Manifestations
- Vomiting, Dehydration
- Hallucination
- Hyperpyrexia
- Convulsions
Treatment
Symptomatic and supportive
- External cooling
- Maintain electrolyte balance = i.v. fluid with Na+ K+ HCO3-
and glucose
- Gastric Lavage
- Forced alkaline diuresis or hemodialysis
- Blood Transfusion and Vit K (if bleeding occurs)
• SYMPTOMS OF ASPIRIN SENSITIVITY
Precautions and Contraindications
- Prolonged labour
- blood loss
1) Analgesic(0.3-1.5 g)
2) Antipyretic
5) Rheumatoid arthritis
6) Osteoarthritis
7) To delay labour
Diclofenac Na
Has good tissue permeability & conc in synovial fluid is high
chondroprotictive action.
• Dose- 100 mg BD
Drugs Pharmacokinetic Adverse Uses
s Effects
t ½ - 2-5 hrs
Paracetamol
Good antipyretic and analgesic action but poor anti-
inflammatory action (0.5-1g tds)
Pharmacokinetics
• Excretion = Urine
• Adverse Effects = GI Irritation rare
Necrosis
Rx
Induce emesis
Gastric Lavage
Specific antidote: N-acetyl cysteine 150 mg/kg i.v. followed
by same dose iv over next 20 hrs.
• Infertility– reversible
• Paracetamol --Asthma
intracranial hemorrhage
Selection of NSAID
• Paracetamol
Mild/moderate pain • Low dose ibuprofen
Pregnancy • Paracetamol
45
THANK YOU