Ibuprofen

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Ibuprofen.jpg

[edit] MECHANISM OF ACTION

Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID) with analgesic, antipyretic and antirheumatic properties. Ibuprofen inhibits the enzyme, cyclooxygenase (COX), an early component of the arachidonic acid cascade, resulting in the reduced formation of prostaglandins and thromboxanes. Prostaglandins act as messenger molecules in the process of inflammation.

Single doses of 200 mg taken on an empty stomach by volunteers produced peak serum levels after approximately 45 minutes. When taken after food, absorption was slower, peak levels appearing at 1.5 to 3 hours.

Plasma half-life of ibuprofen is in the range 1.9 to 2.2 hours.

[edit] INDICATIONS

  • temporarily reduces fever
  • temporarily relieves minor aches and pains due to:
    • minor pain of arthritis (Rheumatoid arthritis, osteoarthritis, Juvenile rheumatoid arthritis)
    • muscular aches
    • backache
    • dysmenorrhea (menstrual cramps)
    • headache
    • toothache
    • Acute gout
    • the common cold

[edit] DOSAGE

  • IBUPROFEN 200 mg:
    • Adults and children 12 years and over: take 1 tablet every 4 to 6 hours while symptoms persist
    • if pain or fever does not respond to 1 tablet, 2 tablets may be used
    • do not exceed 6 tablets in 24 hours, unless directed by a doctor

Children: The daily dosage is 20 mg/kg of body weight in divided doses. In children weighing less than 30 kg the total dose given in 24 hours should not exceed 500 mg.

[edit] CONTRAINDICATIONS

  • Hypersensitivity to Ibuprofen or to any other NSAID
  • Right before or after heart surgery
  • Patients with severe heart failure.
  • Patients with severe liver failure.
  • Patients with severe renal failure (glomerular filtration below 30 mL/min).
  • Patients with conditions involving an increased tendency to bleeding
  • Patients with active, or a history of, ulcerative colitis, Crohn’s disease, recurrent peptic ulceration or gastrointestinal hemorrhage
  • Third trimester of pregnancy. (in the first 6 months of pregnancy, Ibuprofen should be avoided)

[edit] WARNINGS AND PRECAUTIONS

  • Severe Skin Reactions: NSAIDs may very rarely cause serious cutaneous adverse events such as exfoliative dermatitis, toxic epidermal necrolysis (TEN) and Stevens-Johnson syndrome (SJS), which can be fatal and occur without warning. These serious adverse events are idiosyncratic and are independent of dose or duration of use. Patients should be advised of the signs and symptoms of serious skin reactions and to consult their doctor at the first appearance of a skin rash or any other sign of hypersensitivity.
  • Stomach bleeding warning: NSAIDs may cause severe stomach bleeding, The chance is higher in: patients age 60 or older, history of stomach ulcers or bleeding problems, patients taking a blood thinning (anticoagulant) or steroid drug, patients taking another NSAIDs (aspirin, Naproxen, or others), patients drinking 3 or more alcoholic drinks every day while on Ibuprofen, patients taking Ibuprofen more or for a longer time than directed
  • Cardiovascular Risk: NSAIDs may cause an increased risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, which can be fatal. This risk may increase with duration of use. Patients with cardiovascular disease or risk factors for cardiovascular disease may be at greater risk
  • Hypertension: Use with caution in patients with hypertension (NSAIDs, can lead to onset of new hypertension or worsening of pre-existing hypertension)
  • Congestive Heart Failure and Edema: Fluid retention, edema, and peripheral edema have been observed in some patients taking NSAIDs. Ibuprofen should be used with caution in patients with fluid retention or heart failure.
  • NSAIDs should be used with caution in patients with a history of inflammatory bowel disease (ulcerative colitis, Crohn’s disease) as their condition may be exacerbated.
  • Asthma: Caution is required if ibuprofen is administered to patients suffering from, or with a previous history of, bronchial asthma since ibuprofen has been reported to cause bronchospasm in such patients.

[edit] INTERACTIONS

  • The use of an ACE inhibitor or angiotensin receptor antagonist, an antiinflammatory drug (NSAID or COX-2 inhibitor) and thiazide diuretic at the same time increases the risk of renal impairment. The combination of drugs from these three classes should be used with caution particularly in elderly patients or those with pre-existing renal impairment.
  • Anticoagulants (e.g. Warfarin): Caution is recommended since concomitant administration could increase the risk of bleeding.
  • Selective serotonin reuptake inhibitors (SSRIs): Concomitant administration of systemic NSAIDs and SSRIs may increase the risk of gastrointestinal bleeding.
  • Lithium carbonate: If used concomitantly, Ibuprofen may raise plasma concentrations of lithium. Lithium plasma concentrations should be monitored in patients on concurrent ibuprofen therapy.
  • Diuretics, ACE inhibitors or Beta blockers: concomitant use of Ibuprofen with diuretics or antihypertensive agents (e.g. beta blockers, angiotensin converting enzyme (ACE inhibitors)) may cause a decrease in their antihypertensive effect. Therefore, the combination should be administered with caution and patients, especially the elderly, should have their blood pressure periodically monitored. Diuretics can also increase the risk of nephrotoxicity of NSAIDs.
  • Cardiac glycosides (e.g. Digoxin): NSAIDs may exacerbate cardiac failure, reduce GFR (glomerular filtration rate) and increase plasma glycoside levels.
  • Aspirin, other systemic NSAIDs or Corticosteroids: Concomitant administration of Ibuprofen and other systemic NSAIDs or corticosteroids may increase the risk of gastrointestinal bleeding.
  • Herbal Extracts: Ginkgo biloba may potentiate the risk of bleeding with NSAIDs
  • Cyclosporine or Tacrolimus: Increased risk of nephrotoxicity when used with NSAIDs .
  • Quinolones: There have been isolated reports of convulsions which may have been due to concomitant use of quinolones and NSAIDs.
  • Methotrexate: NSAIDs inhibit tubular secretion of methotrexate in animals. As a result, reduction of clearance of methotrexate may occur. Use of high doses of methotrexate concomitant with NSAIDs should be avoided. At low doses of methotrexate caution should be used if ibuprofen is administered concomitantly.
  • CYP2C9 Inhibitors: Concomitant administration of ibuprofen with CYP2C9 inhibitors may increase the exposure to ibuprofen (CYP2C9 substrate). Reduction of the ibuprofen dose should be considered when potent CYP2C9 inhibitors are administered concomitantly, particularly when high-dose ibuprofen is administered with either voriconazole or fluconazole.

[edit] PREGNANCY AND LACTATION

Pregnancy Category C (US). During the first and second trimester of pregnancy, ibuprofen should not be given unless clearly necessary. If ibuprofen is used by a woman attempting to conceive, or during the first or second trimester of pregnancy, the dose should be kept as low and duration of treatment as short as possible.


Pregnancy Category D (US) (at ≥30 weeks of gestation) : Ibuprofen is contraindicated during the third trimester of pregnancy.
During the third trimester of pregnancy, all prostaglandin synthesis inhibitors may expose the foetus to:

  • Cardiopulmonary toxicity (with premature closure of the ductus arteriosus and pulmonary hypertension)
  • Renal dysfunction, which may progress to renal failure with oligohydramnios

At the end of pregnancy, prostaglandin synthesis inhibitors may expose the mother and the neonate to the following:

  • Possible prolongation of bleeding time
  • Inhibition of uterine contractions, which may result in delayed or prolonged labor.


Use in Lactation: Ibuprofen is not recommended for nursing mothers.

[edit] SIDE EFFECTS

Adverse effects may include:

  • gastrointestinal: dyspepsia, heartburn, nausea, loss of appetite, stomach pain, diarrhoea
  • central nervous system: dizziness, fatigue, headache, nervousness
  • hypersensitivity reactions: skin rashes and itching. Rarely exfoliative dermatitis andepidermal necrolysis have been reported with ibuprofen.
  • rare cases of photosensitivity
  • cardiovascular - fluid retention and in some cases oedema.
  • Allergic reactions such as skin rash, itching, swelling of the face or breathing difficulties may also occur. These are usually transient and reversible on cessation of treatment.

[edit] RELATED LINKS

NSAIDs: MOAs and Clinical Considerations

[edit] BIBLIOGRAPHY

[edit] REFERENCES

Non-steroidal anti-inflammatory drugs (NSAIDs)
Non-selective (COX-1 and COX-2 inhibitors) Aceclofenac   Acetylsalicylic acid   Benzydamine   Diclofenac   Flurbiprofen   Ibuprofen   Indometacin   Ketoprofen   Ketorolac   Ketorolac   Lornoxicam   Mefenamic acid   Morniflumate   Nabumetone   Naproxen   Niflumic acid   Piroxicam   Tenoxicam
Relatively COX-2 selective Meloxicam   Nimesulide
COX-2 selective inhibitors (Coxibs) Celecoxib   Etoricoxib   Parecoxib
Ophthalmic NSAIDs Bromfenac (ophthalmic)   Diclofenac (ophthalmic)   Flurbiprofen (ophthalmic)   Ketorolac (ophthalmic)   Nepafenac (ophthalmic)
Veterinary use Carprofen   Deracoxib   Firocoxib   Mavacoxib   Robenacoxib
Antimigraine preparations
5 HT1 agonists (Triptans) Almotriptan (Almogran, Axert)   Eletriptan (Relpax)   Frovatriptan (Frova, Migard, Menatriptan)   Rizatriptan (Maxalt)   Sumatriptan (Imigran)   Zolmitriptan (Zomig)
Ergot alkaloids Dihydroergotamine   Ergotamine
NSAIDs/ Analgesics Indometacin   Acetylsalicylic acid (Aspirin)   Diclofenac (Voltaren)   Ibuprofen (Advil, Brufen, Dolgit, Nurofen)   Ketorolac (Toradol)   Naproxen (Naprosyn, Aleve)   Nimesulide   Paracetamol (Efferalgan, Panadol...)
Prophylaxis Cinnarizine (Stugeron, Stugeron forte)   Flunarizine (Sibelium)   Nifedipine (Adalat)   Pizotifen   Propranolol (Inderal)   Topiramate (Topamax)