Diclofenac- A Common Painkiller

By-Lovnish ThakurASU2014010100099INTEGRATED BIOTECH-4TH SEMBSBT-204(PHARMACEUTICAL SCIENCE)

Introduction

Diclofenac Sodium is NSAID, a phenyl acetic acid derivative

www.newdruginfo.com

NSAIDNon Steroidal

Anti Inflammatory

Drug

General Information

Name- Diclofenac Sodium Chemical Formula- C14H10Cl2NO2.Na Average Molecular Weight- 318.1Drug Category • Anti-Inflammatory Agents, Non-Steroidal • Inhibits cyclooxygenase-1 (COX-1) and COX-2s • Non steroidal Anti-inflammatory Agents

(NSAIDs)

Pharmacokinetics Profile

•Absorption•Distribution •Elimination

Absorption

Bioavailability:

• well absorbed • undergoes first-pass metabolism; only 50–60% of a dose reaches systemic circulation

as unchanged drug. • Peak plasma concentration usually attained within about 1 hour

• Onset: Single 50- or 100-mg doses of diclofenac potassium provide pain relief within 30 minutes.

• Duration: Pain relief lasts up to 8 hours following administration of single 50- or 100-mg doses of diclofenac sodium.

• Food: Food delays time to reach peak plasma concentration but do not affect extent of absorption following administration as conventional, delayed-release, or extended-release tablets.

Distribution

• Extent: Following oral administration, concentrations in synovial fluid may exceed those in plasma.

• Plasma Protein Binding: >99%

Elimination

• Metabolism: Metabolized in the liver via hydroxylation and

conjugation. Some metabolites may exhibit anti-inflammatory activity.

• Elimination Route: Excreted in urine (65%) and in feces via biliary elimination (35%) as metabolites

Half-life: • Oral preparations: 1–2 hours. • Diclofenac epolamine transdermal system: approximately 12

hours

Pharmacodynamic Profile

PharmacologyMechanism of Action

Adverse Reactions

Pharmacology

• Diclofenac has analgesic, antipyretic and anti-inflammatory activities.

• Its potency against cyclooxygenase-1 (COX-1) and COX-2s is substantially greater than that of several other NSAIDs.

Diclofenac is used to treat pain-:• ocular inflammation• osteoarthritis• rheumatoid arthritis• spondylitis

Mechanism of Action

Action by inhibition of prostaglandin synthesis by inhibition of cyclooxygenase (COX)

Prostaglandin-endoperoxide synthase

(PTGS), also known as cyclooxygenase (COX), is

the key enzyme in prostaglandin biosynthesis

Adverse Effects

Cardiovascular System: congestive heart failure, hypertension, tachycardia, syncope.

Digestive System: dry mouth, esophagitis, gastric/peptic ulcers, gastritis, jaundice.

Nervous System: anxiety, asthenia, confusion, depression, drowsiness, Insomnia, malaise, nervousness, tremors, vertigo.

Respiratory System: asthma, dyspnea.

Available Dosage Forms

• Tablet• Solution• Injections• Gels

Conclusion

Diclofenac is a potent drug for treating pain & Inflammation but it should not be taken

without prescription.

Reference

• Novartis. Voltaren (diclofenac sodium enteric-coated tablets) prescribing information. East Hanover, NJ; 2006 Jan.

• Todd PA, Sorkin EM. Diclofenac sodium: a reappraisal of its pharmacodynamic and pharmacokinetic properties, therapeutic efficacy. Drugs. 1988; 35:244-85. [IDIS 240385] [PubMed 3286213]

• www.drugbank.ca/drugs/DB00586• http://www.accessdata.fda.gov/drugsatfda_docs/

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