Ibuprofen; Uses, Dosage, Side Effects, Interactions

Ibuprofen
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Ibuprofen is a nonsteroidal anti-inflammatory agent with analgesic properties used in the therapy of rheumatism and arthritis. Ibuprofen is a propionic acid derivate and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic effects. Ibuprofen inhibits the activity of cyclo-oxygenase I and II, resulting in a decreased formation of precursors of prostaglandins and thromboxanes. This leads to decreased prostaglandin synthesis, by prostaglandin synthase, the main physiologic effect of ibuprofen. Ibuprofen also causes a decrease in the formation of thromboxane A2 synthesis, by thromboxane synthase, thereby inhibiting platelet aggregation. (NCI05)
Ibuprofen is a commonly used nonsteroidal anti-inflammatory (NSAID) drug which is available both by prescription and over-the-counter. Ibuprofen is considered to be among the safest NSAIDs and is generally well tolerated but can, nevertheless, rarely cause clinically apparent and serious acute liver injury.

Mechanism of Action of Ibuprofen

The exact mechanism of action of ibuprofen is unknown. 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 to inhibition cyclooxygenase-2 (COX-2) which decrease the synthesis of prostaglandins involved in mediating inflammation, pain, fever, and swelling. Antipyretic effects may be due to action on the hypothalamus, resulting in increased peripheral blood flow, vasodilation, and subsequent heat dissipation. Inhibition of COX-1 is thought to cause some of the side effects of ibuprofen including GI ulceration. Ibuprofen is administered as a racemic mixture. The R-enantiomer undergoes extensive interconversion to the S-enantiomer in vivo. The S-enantiomer is believed to be the more pharmacologically active enantiomer.

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We previously showed the non-steroidal anti-inflammatory drug (NSAID) ibuprofen suppresses inflammation and amyloid in the APPsw (Tg2576) Tg2576 transgenic mouse. The mechanism for these effects and the impact on behavior are unknown. We now show ibuprofen’s effects were not mediated by alterations in amyloid precursor protein (APP) expression or oxidative damage (carbonyls). Six months of ibuprofen treatment in Tg+ females caused a decrease in open field behavior (p < 0.05), restoring values similar to Tg- mice. Reduced caspase activation per plaque provided further evidence for a neuroprotective action of ibuprofen. The impact of a shorter 3-month duration ibuprofen trial, beginning at a later age (from 14 to 17 months), was also investigated. Repeated measures ANOVA of Abeta levels (soluble and insoluble) demonstrated a significant ibuprofen treatment effect (p < 0.05). Post-hoc analysis showed that ibuprofen-dependent reductions of both soluble Abeta and Abeta42 were most marked in the entorhinal cortex (p < 0.05). Although interleukin-1beta and insoluble Abeta were more effectively reduced with longer treatment, the magnitude of the effect on soluble Abeta was not dependent on treatment duration.

Indications of Ibuprofen

IbuprofenTablet is used for the treatment, control, prevention, & improvement of the following diseases, conditions, and symptoms

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Temporarily relieves minor aches and pains due to

Therapeutic Indications of Ibuprofen

Contra-Indications of Ibuprofen

Dosage of Ibuprofen

Strengths:50 mg; 100 mg;  200 mg; 300 mg; 400 mg; 800 mg; 200 mg;100 mg/5 mL;

Dysmenorrhea

  • 200 to 400 mg orally every 4 to 6 hours as needed.

Osteoarthritis

  • Initial dose: 400 to 800 mg orally every 6 to 8 hours.
  • Maintenance dose: May be increased to a maximum daily dose of 3200 mg based on patient response and tolerance.

Rheumatoid Arthritis

  • Initial dose: 400 to 800 mg orally every 6 to 8 hours.
  • Maintenance dose: May be increased to a maximum daily dose of 3200 mg based on patient response and tolerance.
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Headache

  • 600 mg orally 90 minutes prior to the initial ECT session

Pain

  • 200 to 400 mg orally every 4 to 6 hours as needed. Doses greater than 400 mg have not been proven to provide greater efficacy.
  • IV: (Patients should be well hydrated before IV ibuprofen administration):
  • Pain: 400 to 800 mg intravenously over 30 minutes every 6 hours as needed.

Fever

  • 200 to 400 mg orally every 4 to 6 hours as needed.
  • IV: (Patients should be well hydrated before IV ibuprofen administration):
  • Fever: Initial: 400 mg intravenously over 30 minutes
  • Maintenance: 400 mg every 4 to 6 hours or 100 to 200 mg every 4 hours as needed.

Pediatric Dose for Fever

Greater than 6 months to 12 years

  • 5 mg/kg/dose for temperature less than 102.5 degrees F (39.2 degrees C) orally every 6 to 8 hours as needed.
  • 10 mg/kg/dose for temperature greater than or equal to 102.5 degrees F (39.2 degrees C) orally every 6 to 8 hours as needed.
  • The recommended maximum daily dose is 40 mg/kg.
  • OTC pediatric labeling (analgesic, antipyretic): 6 months to 11 years: 7.5 mg/kg/dose every 6 to 8 hours; Maximum daily dose: 30 mg/kg

Pediatric Dose for Pain

  • Infants and Children: 4 to 10 mg/kg orally every 6 to 8 hours as needed.
  • The recommended maximum daily dose is 40 mg/kg.
  • OTC pediatric labeling (analgesic, antipyretic): 6 months to 11 years: 7.5 mg/kg/dose every 6 to 8 hours; Maximum daily dose: 30 mg/kg

Pediatric Dose for Rheumatoid Arthritis

6 months to 12 years

  • Usual: 30 to 40 mg/kg/day in 3 to 4 divided doses; start at lower end of dosing range and titrate; patients with milder disease may be treated with 20 mg/kg/day; doses greater than 40 mg/kg/day may increase risk of serious adverse effects; doses greater than 50 mg/kg/day have not been studied and are not recommended.
  • Maximum dose: 2.4 g/day

Side Effects of Ibuprofen

The most common

More common

Rare

Drug Interactions of Ibuprofen

Ibuprofen may interact with following drugs, supplyments & may change the efficacy of drugs

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Pregnancy Category of Ibuprofen

FDA pregnancy category: C

Pregnancy

Animal studies have revealed evidence of increased risk of miscarriage, cardiac malformation, and gastroschisis following use of prostaglandin synthesis inhibitors in early pregnancy. Administration of nonsteroidal anti-inflammatory drugs (NSAIDs) during the third trimester of pregnancy may cause significant adverse effects, including premature closure of the fetal ductus arteriosus, oligohydramnios, fetal renal impairment, pulmonary hypertension, and prolongation of bleeding time. There are no controlled data in human pregnancy.

Lactation

Not recommended during last trimester of pregnancy. Prior to 30 weeks gestation: Use only if potential benefit justifies the potential risk to the fetus. Avoid use during third trimester as it may cause premature closure of the ductus arteriosus.

Tips

  • Take with food or milk if stomach disturbances (such as indigestion) occur with use. See a doctor if these persist.
  • Always use the lowest effective dose for the shortest duration consistent with the condition being treated.
  • If you are taking ibuprofen and find it is not working very well for you, you may like to try a different NSAID.
  • Response to different NSAIDs can vary so switching types (for example, from ibuprofen to naproxen) may improve response.
  • See a doctor immediately if you experience any difficulty with breathing, unexplained sickness or fatigue, loss of appetite, vision changes, fluid retention or abnormal bleeding.
  • NSAIDs should not be used in the last 3 months of pregnancy; ask your doctor before using any medication during pregnancy.
  • Avoid ibuprofen if you have a history of asthma or hives due to aspirin use or other NSAIDs, like naproxen.
  • Do not use this medicine if you have just had heart bypass surgery (also called coronary artery bypass graft, or CABG).

References

  1. https://pubchem.ncbi.nlm.nih.gov

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