Diclofenac

Diclofenac- NSAID and its pharmacology

Diclofenac is a type of Non-steroidal anti-inflammatory drugs prescribed for musculoskeletal pain. NSAIDs are a collective class of compounds widely used in several different indications. The drugs under this class have effects ranging from analgesic, antipyretic, anti-inflammatory, cardio-protection, with varying effectiveness levels. Some are also being used for cancer chemoprevention. These are some of the most commonly available OTC (over the counter) drugs.

The most common of them include paracetamol, diclofenac, and aspirin. They are sometimes, also referred to as non-narcotic, non-opioid, or aspirin-like analgesics.

ParametersDetails
Category of DrugDiclofenac is an Analgesics, Antipyretics, Non-Steroidal Anti-Inflammatory Drugs
Mechanism of ActionDiclofenac inhibits cyclooxygenase (COX-1 and COX-2). Diclofenac is a potent inhibitor (1)of prostaglandin synthesis in vitro. Prostaglandins are mediators of inflammation.
Indications Diclofenac is used for
1. Acute musculoskeletal pain
2. Arthritis
3. Gout
4. Spondylitis
5. Migraine
6. Post-operative pain.
Well Known
Pharmaceutical Brands
DYNAPAR- TROIKAA PHARMA
VOVERAN-NOVARTIS
DICLOTAL- BLUE CROSS
DOLOKIND AQ- MANKIND
Products & Services | Wholesaler from Lucknow
StructureThumb
Molecular details Weight: 296.149
Chemical Formula- C14H11Cl2NO2
IUPAC Name2-[2-(2,6-dichloroanilino)phenyl]acetic acid
Available dosage forms1. TABLETS
2. CAPSULES
3. INJECTION
4. EYE/EAR DROP
5. SUPPOSITORIES
6. GEL
Storage conditions Store protected from light
Dose100 to 150 mg daily in 2 to 3 divided doses, (max 150 mg/day) maintenance by 50 to 100 mg in divided doses
Contraindications1.  Porphyria
2. Avoid injections containing benzyl alcohol in neonates
3. History of gastric ulcers,
4. Bleeding or perforation.
Pharmacokinetic properties 1. Absorption- completely absorbed from the GI tract 
2. Vd- 5-10 L or 0.1-0.2 L/kg
3. 99.7% bound to serum proteins
4. The primary metabolite is 4′-hydroxy diclofenac
5. 60-70% is eliminated in the urine
6. half-life – 2 h approx.
7. plasma clearance- 16 L/h
Precautions 1. NSAIDs should be used with caution in the elderly
2. Interactions
3. Pregnancy
4. Patients with coagulation disorders
5. Hepatic, renal and cardiac impairment
6. History of gastrointestinal lesions
Adverse Effects 1. Injection site reactions
2. Transient epigastric pain
3. Risk of thrombotic events
4. Toxic epidermal necrolysis
5. Abnormality in kidney function.
Pregnancy Category B

References:

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