Ibuprofen

A nonsteroidal anti-inflammatory drug (NSAID) class that is used for treating pain, fever, and inflammation,

painful menstrual periods, migraines, and rheumatoid arthritis, to close a patent ductus in a premature baby.

Works, as other NSAIDs, by inhibiting the cyclooxygenase (COX) enzymes, which convert arachidonic acid to prostaglandin H2 (PGH2).

PGH2, in turn, is converted by other enzymes to several other prostaglandins, mediating of pain, inflammation, and fever, and to thromboxane A2 which stimulates platelet aggregation, leading to the formation of blood clots.

Ibuprofen is a nonselective COX inhibitor, inhibiting two isoforms of cyclooxygenase, COX-1 and COX-2.

The analgesic, antipyretic, and anti-inflammatory activity of NSAIDs appears to operate mainly through inhibition of COX-2.

Routes of administration by mouth, rectal, topical, and intravenous.

Onset of activity is typically within an hour.

Trade names Advil, Motrin

Pregnancy category US: C (Risk not ruled out)

Category D (US) at ≥30 weeks of gestation, due to the potential for premature closure of the ductus arteriosus

Bioavailability 80–100% (by mouth), 87% (rectal).

Protein binding 98%.

Metabolism by liver -CYP2C

After oral administration, peak serum concentration is reached after 1–2 hours and up to 99% of the drug is bound to plasma proteins.

The majority of ibuprofen is metabolized and eliminated within 24 hours in the urine.

1% of the unchanged drug is removed through biliary excretion.

Onset of action 30 minutes.

Elimination half-life 2–4 hours.

Excretion in Urine (95%)

Common side effects include heartburn and a rash.

Compared to other NSAIDs, it may have fewer side effects such as gastrointestinal bleeding.

Inhibition of COX-1 is responsible for unwanted effects on the gastrointestinal tract.

It increases the risk of heart failure, kidney failure, and liver failure.

At low doses does not appear to increase the risk of heart attack; however, at higher doses it may.

Can worsen asthma, sometimes fatally.

Harmful in late pregnancy,and use is nit recommended.

Works by inhibiting the production of prostaglandins by decreasing the activity of the enzyme cyclooxygenase.

Might be a weaker anti-inflammatory agent than other NSAIDs.

Used primarily to treat fever, mild to moderate pain, painful menstruation, osteoarthritis, dental pain, headaches, pain from kidney stones, inflammatory diseases such as juvenile idiopathic arthritis and rheumatoid arthritis, pericarditis and patent ductus arteriosus.

Its antipyretic effects may be due to action on the hypothalamus, causing an increased peripheral blood flow, vasodilation, and subsequent heat dissipation.

About 60% of people respond to any NSAID; those who do not respond well to a particular one may respond to another.

Ibuprofen lysine is approved for closure of patent ductus arteriosus in premature infants weighing between 500 and 1,500 grams who are no more than 32 weeks gestational age when usual medical management is not effective.

Adverse effects include: nausea, dyspepsia, diarrhea, constipation, gastrointestinal ulceration/bleeding, headache, dizziness, rash, salt and fluid retention, and high blood pressure.

Infrequent adverse effects include esophageal ulceration, heart failure, high blood levels of potassium, kidney impairment, confusion, and bronchospasm.

Ibuprofen levels maybe measured in blood, plasma, or serum to demonstrate the presence of the drug in a person having experienced an anaphylactic reaction, confirm a diagnosis of poisoning, or assist in a medicolegal death investigation.

As with several other NSAIDs, chronic ibuprofen use has been correlates with risk of hypertension and myocardial infarction, especially at high dose.

Sometimes used for the treatment of acne because of its anti-inflammatory properties, and may be useful in the treatment of severe orthostatic hypotension.

It has been found to be effective chemoprophylaxis of acute mountain illness but is slightly inferior to acetazolomide.

Associated with the onset of bullous pemphigoid or pemphigoid-like blistering, photosensitization of the skin as is an extremely rare cause of the autoimmune disease Stevens–Johnson syndrome and toxic epidermal necrolysis.

Concurrent consumption of alcohol may increase the risk of stomach bleeding.

Can interfere with the antiplatelet effect of low-dose aspirin, potentially rendering aspirin less effective when used for cardioprotection and stroke prevention.

Most symptoms of overdose include abdominal pain, nausea, vomiting, drowsiness, dizziness, headache, ear ringing, and nystagmus.

Rarely, in overdose gastrointestinal bleeding, seizures, metabolic acidosis, hyperkalemia, hypotension, slow heart rate, fast heart rate, atrial fibrillation, coma, liver dysfunction, acute kidney failure, cyanosis, respiratory depression, and cardiac arrest have been reported.

The symptoms with an overdose of ibuprofen are similar to the symptoms caused by overdoses of other NSAIDs.

Therapy for overdose is largely symptomatic.

Early presentation of overdose can be managed with decontamination of the stomach using activated charcoal.

Gastric lavage can be considered if the amount ingested is potentially life-threatening, and it can be performed within 60 minutes of ingestion.

Measures to maintain urine are employed and kidney function is monitored.

Studies are variable as to the effects of NSAIDs on miscarriage rates in pregnant women.

Has been associated with a lower risk of Parkinson’s disease, and may delay or prevent it.