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INDOMETHACIN

by: Hedy Mae Bautista and Ana Francesca Jacinto

NSAID Nonsteroidal Anti-inflammatory Drugs

Introduced in 1963 as an indole derivative


Potent, nonselective COX inhibitor and may also inhibit phospholipase A and C. Well absorbed after oral administration.

Prostaglandin Biosynthesis
Phospholipid
Phospholipase A2 COX-1 constitutive enzyme

Arachidonic Acid

COX-2 inducible enzyme

Prostaglandins
Indomethacin blocks here

Prostaglandins

Physiology

Pathology

Popular Local Brand Names of Indomethacin


Indocid Infree

Indomethacin is indicated for:


Severe pain, tenderness, swelling, and stiffness caused by

osteoarthritis, rheumatoid arthritis, ankylosing spondylitis.


Extra-articular inflammatory conditions such as pericarditis,

pleurisy and in Bartters syndrome.


Pain in the shoulder caused by bursitis and tendinitis. Immediate-release capsules, suspension and suppositories are

also indicated for the pain, swelling caused by acute gouty arthritis.

Off-Label Use of Indomethacin


Management of patent ductus arteriosus (PDA) in premature infants.
The ductus arteriosus is a blood vessel that allows blood to go around

the baby's lungs before birth. Soon after the infant is born and the lungs fill with air, the ductus arteriosus is no longer needed. It usually closes in a couple of days after birth.
PDA leads to abnormal blood flow between the aorta and pulmonary

artery, two major blood vessels that carry blood from the heart.
This structure is kept patent in the fetus by continuous production of

prostaglandins, closure can be accelerated by intravenous infusion of this drug.

Adverse Reactions of Indomethacin


Although Indomethacin is able to reduce pain and fever, it is not routinely used for these effects due to its potential for toxicity:

Severe frontal headache CNS Effects: Dizziness, Vertigo, Confusion, Seizures and Psychiatric changes such as depression and psychosis. Mild GI reactions: Nausea and Vomiting, Indigestions More severe GI effects: Ulceration with perforation, hemmorrhage Hematologic reactions: Neutropenia, Thrombocytopenia, aplastic anemia,

Drug Interactions:
1. May decrease the antihypertensive effects of beta-

blockers, ACE inhibitors, angiotensin II antagonists and hydralazine


2. Antagonizes the natriuretic and hypertensive effects

of furosemide and thiazides


3. May increase serum Potassium when used with

Potassium-sparing diuretics

Drug Interactions:
4. Probenecid may increase the serum concentration

of indomethacin
5. Concurrent use with other NSAIDs may increase GI

adverse effects
6. May increase the nephrotoxicity of Cyclosporine 7. May increase the serum concentrations of Digoxin,

Methotrexate, Lithium and Aminoglycosides

Identification and Chemical/Color reactions:


1. Indomethacin + Water + NaOH + Sodium nitrite + HCl

Result: Green color

2. Indomethacin + Water + NaOH


Result: strong yellow color is produced which fades rapidly.

References:
Basic and Clinical Pharmacology Katzung Pharmacology for Nursing Care Richard A. Lehne (5th Edition) USP 24 Philippine National Drug Formulary Volume II (3rd Edition) http://www.nlm.nih.gov/medlineplus/druginfo/meds/a681027.

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