img

Indometacin or Indomethacin

It is a nonsteroidal anti-inflammatory drug (NSAID) commonly used as a prescription medication to reduce fever, pain, stiffness, and swelling from inflammation. More

Sharing is caring, show love and share the thread with your friends.

Description

It is a nonsteroidal anti-inflammatory drug (NSAID) commonly used as a prescription medication to reduce fever, pain, stiffness, and swelling from inflammation.

Generic Name

Indometacin or Indomethacin

Chemical names

Indomethacin; Indometacin; Indocin; Indomethacine

Brand names

Artisid, Donica, Donica-SR, Ducain, Idicin, Indocap, Indocid, Indoflam, Indoflam EYE, Indoriv, Inmecin, Inmecin-P, Inmecin-R, Inocin, Lygacin, Microcid, Recticin

IUPAC name

2-[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]acetic acid

Pharmacokinetics

  • Bioavailability is approximately 100% following oral administration and 80–90% following rectal administration.
  • 97% protein binding
  • Hepatic metabolism

Actions

It is also known as cyclooxygenase or COX inhibitor (a prostaglandin G/H synthase)that acts on both prostaglandin G/H synthase 1 and 2 (COX-1 and -2). Prostaglandin G/H synthase catalyzes the conversion of arachidonic acid to a number of prostaglandins involved in fever, pain, swelling, inflammation, and platelet aggregation. The antipyretic, analgesic and anti-inflammatory activity of indomethacin occur as a result of decreased prostaglandin synthesis.

Dosage/Dosage form

  • PO- The recommended dose for adults is 50-200 mg per day in divided doses. 
  • Eye drops: As 0.5 or 1% solution: Instill 2 drops into the affected eyes.

Therapeutic uses

Treatment for osteoarthritis, ankylosing spondylitis, acute painful shoulder (bursitis and/or tendinitis) and acute gouty arthritis.

Adverse effects/Side effects

Renal failure, GI upsets, tinnitus, headache, dizziness, lightheadedness, psychiatric disturbances, depression, peripheral neuropathy, insomnia, blurred vision, confusion; hyperglycaemia, hyperkalaemia.

Interaction

  • Increased risk of hyperkalaemia when used with ACE inhibitors or potassium sparing diuretics; increased risk of nephrotoxicity with ACE inhibitors, ciclosporin and tacrolimus; increased risk of bleeding with warfarin and other NSAIDs.
  • Concurrent use with probenecid may cause indometacin toxicity.
  • Concurrent use may increase plasma concentration of digoxin, lithium and metrotrexate.
  • Concurrent use with diflunisal increases plasma concentrations of indometacin.
  • Rate of absorption delayed by food.
  •  Magnesium or aluminum containing antacids may delay absorption.

Contraindications

Active peptic ulcer; pregnancy (3rd trimester), hypersensitivity to aspirin and other NSAIDs; treatment of perioperative pain in CABG surgery; severe renal impairment; rectal admin in patients with proctitis and haemorrhoids; neonates with necrotizing enterocolitis, active bleeding, thrombocytopenia, coagulation defects and untreated infections.

Storage

Store below 30°C.

Information

Molecular weight

357.788

Molecular formula

C19H16ClNO4

CAS number

53-86-1

Precautions

  • Hypertension; congestive heart failure; fluid retention; epilepsy, Parkinsonism, psychiatric disorders; may affect performance of skilled tasks.
  • Monitor ophthalmologic, blood, electrolytes and renal function regularly; lactation.