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Indomethacin

Generic Name
Indomethacin
Brand Names
Indocin, Tivorbex
Drug Type
Small Molecule
Chemical Formula
C19H16ClNO4
CAS Number
53-86-1
Unique Ingredient Identifier
XXE1CET956

Overview

Indometacin, or indomethacin, is a non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic properties. NSAIDs consist of agents that are structurally unrelated; the NSAID chemical classification of indometacin is an indole-acetic acid derivative with the chemical name 1- (p-chlorobenzoyl)25-methoxy-2-methylindole-3-acetic acid. The pharmacological effect of indometacin is not fully understood, however, it is thought to be mediated through potent and nonselective inhibition of the enzyme cyclooxygenase (COX), which is the main enzyme responsible for catalyzes the rate-limiting step in prostaglandin and thromboxane biosynthesis via the arachidonic acid (AA) pathway. Indometacin was first discovered in 1963 and it was first approved for use in the U.S. by the Food and Drug Administration in 1965, along with other acetic acid derivatives such as diclofenac and sulindac that were also developed during the 1960s. Since then, indometacin has been extensively studied in clinical trials as one of the most potent NSAIDs in blocking prostaglandin synthesis and was among the first NSAIDs to be used in the symptomatic treatment of migraine and for headaches that eventually became known as “indomethacin-responsive” headache disorders. Most commonly used in rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, acute shoulder pains, and acute gouty arthritis, indometacin is currently available as oral capsules as well as other methods of administration, including rectal and intravenous formulations. Intravenous indometacin is administered to close a hemodynamically significant patent ductus arteriosus, as indicated by clinical evidence, in premature infants. Ophthalmic indometacin has been studied and used in the symptomatic treatment of postoperative ocular inflammation and pain and/or complications after cataract surgery. Although deemed effective in reducing ocular inflammation in clinical studies, topical NSAIDs were also associated with a potential reduction in corneal sensitivity accompanied by an increased risk of superficial punctate keratitis and subjective symptoms of discomfort, including pain, burning or pricking, or a tingling sensation after instillation into the cul‐de‐sac.

Background

Indometacin, or indomethacin, is a non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic properties. NSAIDs consist of agents that are structurally unrelated; the NSAID chemical classification of indometacin is an indole-acetic acid derivative with the chemical name 1- (p-chlorobenzoyl)25-methoxy-2-methylindole-3-acetic acid. The pharmacological effect of indometacin is not fully understood, however, it is thought to be mediated through potent and nonselective inhibition of the enzyme cyclooxygenase (COX), which is the main enzyme responsible for catalyzes the rate-limiting step in prostaglandin and thromboxane biosynthesis via the arachidonic acid (AA) pathway. Indometacin was first discovered in 1963 and it was first approved for use in the U.S. by the Food and Drug Administration in 1965, along with other acetic acid derivatives such as diclofenac and sulindac that were also developed during the 1960s. Since then, indometacin has been extensively studied in clinical trials as one of the most potent NSAIDs in blocking prostaglandin synthesis and was among the first NSAIDs to be used in the symptomatic treatment of migraine and for headaches that eventually became known as “indomethacin-responsive” headache disorders. Most commonly used in rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, acute shoulder pains, and acute gouty arthritis, indometacin is currently available as oral capsules as well as other methods of administration, including rectal and intravenous formulations. Intravenous indometacin is administered to close a hemodynamically significant patent ductus arteriosus, as indicated by clinical evidence, in premature infants. Ophthalmic indometacin has been studied and used in the symptomatic treatment of postoperative ocular inflammation and pain and/or complications after cataract surgery. Although deemed effective in reducing ocular inflammation in clinical studies, topical NSAIDs were also associated with a potential reduction in corneal sensitivity accompanied by an increased risk of superficial punctate keratitis and subjective symptoms of discomfort, including pain, burning or pricking, or a tingling sensation after instillation into the cul‐de‐sac.

Indication

Oral indometacin is indicated for symptomatic management of moderate to severe rheumatoid arthritis including acute flares of chronic disease, moderate to severe ankylosing spondylitis, moderate to severe osteoarthritis, acute painful shoulder (bursitis and/or tendinitis) and acute gouty arthritis. Intravenous indometacin is indicated to induce closure of a hemodynamically significant patent ductus arteriosus in premature infants weighing between 500 and 1750 g when after 48 hours usual medical management (e.g., fluid restriction, diuretics, digitalis, respiratory support, etc.) is ineffective.

Associated Conditions

  • Acute Gouty Arthritis
  • Joint Pain
  • Moderate to Severe Osteoarthritis
  • Moderate to Severe Rheumatoid Arthritis
  • Moderate to severe ankylosing spondylitis
  • Myalgia
  • Patent Ductus Arteriosus (PDA)
  • Acute Shoulder Pain

Clinical Trials

FDA Approved Products

Indomethacin
Manufacturer:A-S Medication Solutions
Route:ORAL
Strength:50 mg in 1 1
Approved: 2021/03/15
NDC:50090-2987
Indomethacin
Manufacturer:A-S Medication Solutions
Route:ORAL
Strength:25 mg in 1 1
Approved: 2021/03/15
NDC:50090-0054
Indomethacin
Manufacturer:Proficient Rx LP
Route:ORAL
Strength:75 mg in 1 1
Approved: 2023/07/28
NDC:71205-822
Indomethacin
Manufacturer:RedPharm Drug, Inc.
Route:ORAL
Strength:25 mg in 1 1
Approved: 2023/02/05
NDC:67296-1525
INDOMETHACIN
Manufacturer:DIRECT RX
Route:ORAL
Strength:50 mg in 1 1
Approved: 2023/04/11
NDC:61919-130

Singapore Approved Products

INDO CAPSULES 25 mg
Manufacturer:BEACONS PHARMACEUTICALS PTE LTD
Form:CAPSULE
Strength:25 mg
Online:Yes
Approved: 1991/01/29
Approval:SIN05375P
INDOMEN CAPSULE 25 mg
Manufacturer:Y S P INDUSTRIES (M) SDN BHD
Form:CAPSULE
Strength:25 mg
Online:Yes
Approved: 1996/03/26
Approval:SIN08624P
HD-METHACIN CAPSULE 25 mg
Manufacturer:HOVID BHD, HOVID Bhd.
Form:CAPSULE
Strength:25.00MG
Online:Yes
Approved: 1998/04/06
Approval:SIN09699P

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