Ibuprofen

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Ibuprofen

Ibuprofen, a propionic acid derivative, is a prototypical nonsteroidal anti-inflammatory agent (NSAID) with analgesic and antipyretic properties. Ibuprofen is indicated for the treatment of primary dysmenorrhea, osteoarthritis, rheumatoid arthritis, and for the relief of mild to moderate pain. It works by inhibition of cyclooxygenase enzyme (COX-2) which decreases the synthesis of prostaglandins involved in causing inflammation, pain, fever and swelling.

Introduction

Ibuprofen, a propionic acid derivative, is a prototypical nonsteroidal anti-inflammatory agent (NSAID) with analgesic and antipyretic properties. Ibuprofen is indicated for the treatment of primary dysmenorrhea, osteoarthritis, rheumatoid arthritis, and for the relief of mild to moderate pain. It works by inhibition of cyclooxygenase enzyme (COX-2) which decreases the synthesis of prostaglandins involved in causing inflammation, pain, fever and swelling.

Pharmacological class: NSAID

Indications

  • Pain
  • Primary dysmenorrhea
  • Rheumatoid arthritis
  • Osteoarthritis
  • Headache
  • Toothache
  • Premenstrual pain
  • Back pain

Pharamcological Action

Ibuprofen is a non-selective inhibitor of cyclooxygenase, an enzyme involved in prostaglandin synthesis via the arachidonic acid pathway. Its pharmacological effects are believed to be due inhibition of inflammatory mediators, thus acts by reducing inflammation, pain, fever and swelling. Antipyretic effects may be due to action on the hypothalamus, resulting in an increased peripheral blood flow, vasodilation, and subsequent heat dissipation. It is a racemic mixture and S-form is believed to be more pharmacologically active.

Dosage

Dysmenorrhea: 200 to 400 mg orally every 4 to 6 hours

Osteoarthritis: 1200 to 3200 mg orally per day in divided doses

Rheumatoid Arthritis: 1200 to 3200 mg orally per day in divided doses

Pain: 400 to 800 mg IV every 6 hours

Fever: 200 mg orally every 4 to 6 hours

Pharmacokinetics

Ibuprofen is readily absorbed from GI tract (80%). Ibuprofen is a racemic mixture of R and S isomers; the R isomer (thought to be inactive) is slowly and incompletely (~60%) converted to the S isomer (active) in adults; the amount of conversion in children is not known, but it is thought to be similar to adults; a study in preterm neonates estimated the conversion to be 61% after prophylactic ibuprofen use and 86% after curative treatment (Gregoire 2004). Urine (primarily as metabolites (45% to 80%); ~1% as unchanged drug and 14% as conjugated; 1% as unchanged drug); some feces.

Contraindications

  • Contraindicated in patients with hypersensitivity to ibuprofen.
  • Contraindicated in patients with asthma or utricaria as allergic-type reactions may take place after consuming aspirin
  • Contraindicated for treatment of peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery

Drug Interactions

  • Concomitant use of ibuprofen and aspirin may reduce the effectiveness of aspirin to prevent heart attacks or strokes.
  • Ibuprofen when administered together with danaparoid can increase the risk of bleeding.
  • Lomitapide when taken concomitantly with ibuprofen may increase the risk of liver problems.
  • Concomitant use of methotrexate and ibuprofen may result in increase of the blood levels and side effects of methotrexate specially if the person is having liver disease.
  • Rivaroxaban together with ibuprofen may increase bleeding risk, including severe and sometimes fatal hemorrhage.
  • Tenofovir together with ibuprofen may increase the risk of kidney problems.

Side effects

Common (affecting between 1 in10 to 1 in 100)

  • Rash
  • Dizziness
  • Throwing Up Feel
  • Heartburn
  • Stomach Cramps

Uncommon (affecting 1 in 100 to 1 in 1000)

  • Itching
  • Ringing in Ears
  • Visible Water Retention
  • Water Retention
  • Conditions of Excess Stomach Acid Secretion
  • Diarrhea
  • Easily Angered or Annoyed
  • Gas
  • Head Pain
  • Incomplete or Infrequent Bowel Movements
  • Indigestion
  • Loss of Appetite
  • Nervous
  • Throwing Up

Very rare (affecting less than 1 in 10,000)

  • A Rupture in the Wall of Stomach/Intestine
  • Abnormal Heart Rhythm
  • Abnormal Liver Function Tests
  • Acquired Decrease of All Cells in the Blood
  • Acute Inflammation of Pancreas
  • Allergic Reaction causing Serum Sickness
  • Altered Mental Status

Precautions

  • Avoid in patients who are allergic to ibuprofen.
  • Avoid in patients who have or ever had asthma.
  • Avoid in pregnant women or women who is breastfeeding.
  • Avoid in patients having Phenylketonuria (inborn disease).
  • Never recommended in patients having surgery,including dental surgery.

Clinic Evidence

A study of 15 young women with primary dysmenorrhea was carried out to assess the prophylactic administration of ibuprofen for the treatment of severe and disabling primary dysmenorrhea. The study lasted for six months. The treatment schedule included 400 mg of ibuprofen every 8 hours, starting 24 hours before the menstrual cycle during 4 days of menstruation for six consecutive cycles. Results showed that the mean of initial intensity of menstrual cramp experienced in the cycle before treatment (control) was 9.47 +/- 0.5. During prophylactic treatment, the means of initial intensity of pain were significantly lower, between 7.84 +/- 0.37 and 7.21 +/- 0.52. A statistically significant progressive decrease of pain was recorded during the duration of treatment. After 48 hours of treatment, intensity of pain was recorded as three (mild). Results from study proves that prophylactic administration of ibuprofen is an effective treatment for selected women experiencing severe and disabling primary dysmenorrhea.1

References

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