Ibuprofen

Overview

Ibuprofen is a non-steroidal analgesic, antipyretic and antinflammatory agent. It was the first propionic acid derivative to be used in most countries. Chemically Ibuprofen is (+/-)2-(4-Isobutylphenyl) propionic acid. It reduces inflammation, fever and relieves pain. Ibuprofen is equivalent to aspirin in its antinflammatory effects, but Ibuprofen is more effective analgesic than aspirin or acetaminophen. Ibuprofen is prepared chemically and marketed as racemic mixture of its two enantiomers. Ibuprofen is available in combination with codeine, acetaminophen ans pseudoephedrine. Ibuprofen is available for oral and topical administration.

Category:

Primary Characterstics

Molecular Structure of Ibuprofen
. It is of Synthetic origin and belongs to Propionic Acid. It belongs to Cyclo-oxygenase inhibitor pharmacological group on the basis of mechanism of action and also classified in Analgesics and Anti-inflammatory Agents and NSAIDs pharmacological group.The Molecular Weight of Ibuprofen is 206.30.
Its pKa is 4.4, 5.2.

Pharmacokinetics

Oral absorption of Ibuprofen is found to be 97% ±2. Volume of distribution is found to be 0.1 l/kg and plasma protien binding is 99%. and metabolism is reported extensive by liver. Renal Excretion accounts for >90%. Also excreted in bile and feces and plasma half life is 2-4 hr.

Indications

Contraindications

Ibuprofen is contraindicated in conditions like Hypertension,Peptic ulcer,Bronchospasm,Renal failure,Hypersensitivity,GI bleeding.

Drug Interactions

Ibuprofen is known to interact with other drugs, the details of drug interactions is as follows:

DrugDetailsSeverityOnsetManagement
AspirinIbuprofen bind reversibly at the active site of platelet cyclogenase and thus competitively inhibit this enzyme but because this binding is reversible so it cause temporary rather than sustained depression of thromboxane formation an thus antagonize the anti-platelet and cardioprotective effect of low-dose aspirin.MajorTake medication with food and immediately report sign and symptoms of GI ulceration and bleeding.
Chlorthalidone
DiazoxideHypotensive effect of when diazoxide antagonised by Ibuprofen.
Interferon Beta
MethotrexateIbuprofen increases the plasma concentration of methotrexate by interfering with renal elimination results in increased toxicity and pharmacological effects.MajorClosely monitor for signs of bone marrow suppression and nephrotoxicity. Avoid any other over-the-counter NSAID product.
Moclobemide
OxaliplatinYou should inform your doctor before using this combination.Do not start or stop any medicine without doctor or pharmacist approval.
PemetrexedIbuprofen (400 mg four times a day) can decrease the clearance of pemetrexed.Caution should be used when administering ibuprofen concurrently with Pemetrexedto patients with mild to moderate renal insufficiency
StreptomycinConcurrent use may cause toxicities to the kidneys.
TorasemideIbuprofen, a strong CYP2C9 inhibitor, may increase the serum concentration of Torasemide, a CYP2C9 substrate, by decreasing Torasemide metabolism and clearance. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Torasemide if Ibuprofen is initiated, discontinued or dose changed.

These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Interference in Pathology

No data regarding the pathological interferences produced by Ibuprofen is available.

Side Effects

The severe or irreversible adverse effects of Ibuprofen, which give rise to further complications include Thrombocytopenia.

Ibuprofen produces potentially life-threatening effects which include Vomiting, Peptic ulceration, Hematemesis, Severe gastric pain. which are responsible for the discontinuation of Ibuprofen therapy.

The signs and symptoms that are produced after the acute overdosage of Ibuprofen include Hypotension, Nausea, Vomiting, Cardiac arrhythmias, Coma, Seizures, Acidosis, Ataxia, Headache, Renal failure, Epigastric pain, Hyperkalemia, GI bleeding, Renal and Hepatic dysfunction.

The symptomatic adverse reactions produced by Ibuprofen are more or less tolerable and if they become severe, they can be treated symptomatically, these include Flatulence, Dizziness, Headache, Diarrhea, Constipation, Tinnitus, Blurred vision, Rashes, Pruritus, Gastritis, Depression, Elevation of liver enzymes, Fluid retention, SomnolenceX, Hearing loss, Hypersensitivity reactions, Blood dyscrasias, Vision disturbances, Aseptic maningitis.

Available Brands

Click on the appropriate strength of the dosage form to view its available brands.

Single Ingredient

Syrup: 100 mg/5ml,
Susp: 100 mg, 100 mg/5ml,
Oral Soln: 100 mg,
Cream: 10 %w/w,
Gel: 10 %w/w,
Tabs: 200 mg, 400 mg, 600 mg,
Tabs SR: 800 mg,
Caps: 200 mg, 400 mg,
Powder: 100 mg,

Multi ingredient

Syrup: 100 mg/5ml,
Susp: 100 mg, 100 mg/5ml,
Gel: 10 %w/w,
Tabs: 200 mg, 400 mg,

Dosage

Ibuprofen's dosage details are as follows:
Dose Single Dose Frequency Route Instructions

Adult Dosage

200 to 600 mg400 (400)8 hourlyPOMaximum dose 1.2 g

Paedriatic Dosage ( 20 Kg. )

5 to 10 mg/kg7.5 (7.5)8 hourlyOralMaximum dose: 40 mg/kg

Neonatal Dosage ( 3 Kg. )

No data regarding the neonatal dosage details of Ibuprofen is available.

High Risk Groups

Drug should not be given to Neonates.

If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.

Warning / Precautions

Ibuprofen should be used with caution in patients with intrinsic coagulation defects and those on anticoagulant therapy. It should be used with caution in patients with compromised cardiac function, hypertension other condition predisposing to fluid retention. It should be used with extra care in the presence of existing uncontrolled infection. Perform periodic auditory (hearing) function test during chronic therapy. Discontinue drug if skin reaction occurred.

Storage Conditions

Tab

Store Below 40°C. Protect from Sunlight and Moisture.

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