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Chemical
nameBenzeneacetic acid, a -
methyl - 4 - (2 - methylpropyl), (±).
CategoryAntirheumatic; Analgesic; Antigout agent;
Antipyretic; Antidysmenorrheal; Vascular headache prophylactic; Vascular
headache suppressant.
Mechanism of
action
Ibuprofen inhibits the activity of the enzyme cyclo -
oxygenase, resulting in decreased formation of precursors of
prostaglandins and thromboxanes from arachidonic acid. Analgesic -
Ibuprofen may block pain impulse generation via a peripheral action that
may involve reduction of the prostaglandins, and possibly inhibition of
the synthesis or actions of other substances that sensitize pain receptors
to mechanical or chemical stimulation. Antipyretic - Ibuprofen probably
produces antipyresis by acting centraIly on the hypothalamic heat -
regulating center to produce peripheral vasodilation, resulting in
increased blood flow through the skin, sweating, and heat loss. The
central action probably involves reduction of prostaglandin activity in
the hypothalamus.
Indications
Indicated for rheumatoid arthritis, osteoarthritis,
juvenile arthritis, and psoriatic arthritis; pain; gouty arthritis or
calcium pyrophosphate deposition disease (pseudogout); fever; and
dysmenorrhea. May also be used for prophylaxis and treatment of vascular
headaches.
Precautions to
consider
Risk - benefit should be considered when the foIlowing
medical problems exist: Allergic reaction, mild, such as aIlergic
rhinitis, urticaria, or skin rash, induced by aspirin or other NSAIDs,
history of (possibility of cross- sensitivity); anemia; asthma;
hypertension; renal or hepatic function impairment or failure; edema;
congestive heart disease; inflammatory or ulcerative disease of the upper
or lower gastrointestinal tract, including crohn's disease,
diverticulitis, peptic ulcer disease, or ulcerative colitis, active or
history of; hemophilia or other bleeding problems; alcoholism; diabetes
meIlitus; systemic lupus erythematosus; edema; stomatitis.
PregnancyTeratogenic effects in animals have not been
shown. Adequate and well - controlled studies in humans have not been
done.
Breast -
feedingMethodology capable
of detecting 1 mcg/mL failed to show that ibuprofen is distributed into
breast milk.
Drug
interactions
ln addition to the interactions listed below, the
possibility should be considered that additive or multiple effects leading
to impaired blood clotting and / or increased risk of bleeding may occur
if any NSAID is used concurrently with any medication having a significant
potential for causing hypoprothrombinemia , thrombocytopenia , or
gastrointestinal ulceration or hemorrhage. Cyclosporine - Gold
compounds - Digoxin - Lithium - Probenecid - Acetaminophen -
Anticoagulants - Potassium supplements - Antihypertensives - Diuretics
such as triamterene - Salicylates - Alcohol - Corticosteroids - Valproic
acid - Antidiabetic agents.
Side / Adverse
effects
Hypersensitivity reactions such as: Rhinosinusitis /
asthma or angioedema / urticaria; anaphylaxis. In addition, a syndrome
of fever and chills, nausea, vomiting, and abdominal pain has been
reported with ibuprofen, and a serum sickness- or influenza-like syndrome
that may consist of troubled breathing, arthralgias, fever and chills,
fatigue, pruritus, and / or skin rash or other cutaneous manifestations,
has been reported with ibuprofen. Gastrointestinal problems; headache;
renal and hepatic function impairment; CNS effects; edema; hyperkalemia;
hearing problems.
Administration and
dosage
Usual adult and adolescent dose : Antirheumatic
(nonsteroidal anti -inflammatory): Oral, 1200 to 3200 mg a day in 3 or 4
divided doses. After a satisfactory response has been obtained, dosage
should be reduced to the lowest maintenance dose that provides continuing
control of symptoms. Note: Higher doses generally are required in
rheumatoid arthritis than in osteoarthritis. Analgesic (mild to
moderate pain); antipyretic; antidysmenorrheal - Oral, 200 to 400 mg every
4 to 6 hours as needed. Usual adult prescribing limits
: Antirheumatic (nonsteroidal anti - inflammatory) -Up to 3600 mg per
day. The maximum dosage should be used only if the clinical benefit is
increased sufficiently to offset the higher risk of adverse effects.
Analgesic; antipyretic; antidysmenorrheal - for patient self - medication
(over - the - counter use): Not to exceed 1200 mg per day. Usual pediatric
dose: Antirheumatic (nonsteroidal anti -inflammatory) - Children 6
months to 12 years of age: Oral, initially 30 to 40 mg per kg of body
weight a day in 3 or 4 divided doses, although 20 mg per kg of body weight
per day may be sufficient for patients with mild disease. After a
satisfactory response has been achieved, dosage should be reduced to the
lowest dose needed to control disease activity. Antipyretic - Children
6 months to 12 years of age: Oral, 5 mg per kg of body weight for fevers
lessthan 39.17°C (102.5°F) and 10 mg per kg of body weight for higher
fevers. Dosage may be repeated, if necessary, at intervals of 4 to 6 hours
or more. Usual pediatric prescribing limits: Antirheumatic - Oral,
50 mg per kg of body weight per day. Antipyretic - Oral, 40 mg per kg
of body weight per day.
How
supplied1 - Tablets: Box of
100 coated tablets. Each coated tablet contains 200 mg ibuprofen. 2 -
Tablets: Box of 100 coated tablets. Each coated tablet contains 400 mg
ibuprofen.
StorageStore below 30° C, protect from light and
moisture.
References1 -USP DI Vol: 1 (1997). Pages: 379
-399. 2 -Drug facts and comparisons (1994). 3 -USP 23 page: 785.
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