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Ketoprofen information from DrugsUpdate  

See Available Brands of Ketoprofen in India

P - Caution when used during pregnancy
L - Caution when used during lactation

Ketoprofen, (RS)2-(3-benzoylphenyl)-propionic acid (chemical formula C16H14O3) is one of the propionic acid class of non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic effects. It acts by inhibiting the body's production of prostaglandin.

Pharmacodynamics

Ketoprofen is a racemate with only the S enantiomer possessing pharmacological activity. The enantiomers have similar concentration time curves and do not appear to interact with one another. An analgesic effect-concentration relationship for Ketoprofen was established in an oral surgery pain study with Ketoprofen immediate-release capsules. The effect-site rate constant (Ke0) was estimated to be 0.9 hour-1 (95% confidence limits: 0 to 2.1), and the concentration (Ce50) of Ketoprofen that produced one-half the maximum PID (pain intensity difference) was 0.3 mcg/mL (95% confidence limits: 0.1 to 0.5). Thirty-three (33) to 68% of patients had an onset of action (as measured by reporting some pain relief) within 30 minutes following a single oral dose in postoperative pain and dysmenorrhea studies. Pain relief (as measured by remedication) persisted for up to 6 hours in 26 to 72% of patients in these studies.

Pharmacokinetics

Ketoprofen exhibits anti-inflammatory, analgesic and antipyretic activities. It potently inhibits the enzyme cyclooxygenase resulting in prostaglandin synthesis inhibition. It also prevents formation of thromboxane A2 by platelet aggregation.


Absorption Readily absorbed from the GI tract (oral); reduced absorption with food. Peak plasma concentrations after 0.5-2 hr. Well absorbed (IM, rectal); minimal (topical).


Distribution Synovial fluid (substantial concentrations). Protein-binding: 99%.


Metabolism Hepatic via conjugation with glucuronic acid.


Excretion Urine (as glucuronide conjugates); 1.5-4 hr (elimination half-life).

Ketoprofen Indications / Ketoprofen Uses

Information Not Available

Ketoprofen Adverse Reactions / Ketoprofen Side Effects

Acute interstitial nephritis, reversible decline in renal function; GI symptoms e.g. discomfort, nausea, diarrhoea; pain and tissue damage at inj site (IM). Potentially Fatal: Rarely, idiosyncrasy, anaphylaxis; very rarely GI haemorrhage.

Precautions

Information Not Available

Special Precautions

Pregnancy, lactation. Renal or hepatic impairment. Elderly. Heart failure.

Other Drug Interactions

Risk of nephrotoxicity increased with ACE inhibitors, ciclosporin, tacrolimus or diuretics. Increased risk of hyperkalaemia with ACE inhibitors and potassium-sparing diuretics. Reduces effects of antihypertensives (e.g. ACE inhibitors, β-blockers). Increased risk of convulsions with quinolones. Increased risk of adverse effects with aspirin. Increased risk of GI bleeding and ulceration with corticosteroids, SSRIs, clopidogrel and ticlopidine. Increased risk of haematotoxicity with zidovudine. May alter the efficacy of mifepristone. Increased plasma levels with probenecid. Potentially Fatal: Enhances effects of oral anticoagulants, phenytoin and sulfonylureas. Increases plasma concentrations of lithium, methotrexate and cardiac glycosides.

Other Interactions

Information Not Available

Dosage

Oral Rheumatic disorders Adult: 100-200 mg/day in 2-4 divided doses. As modified-release formulation: Administer dose once daily. Max: 300 mg daily in divided doses. Elderly: >75 yr: Reduce initial dose. Renal impairment: Max dose: Mild impairment: 150 mg daily; severe impairment: 100 mg daily. Hepatic impairment: Max dose: 100 mg daily if serum albumin <3.5 g/dL. Oral Pain and inflammation Adult: 25-50 mg every 6-8 hr. Max: 300 mg daily in divided doses. Elderly: >75 yr: Reduce initial dose. Renal impairment: Max dose: Mild impairment: 150 mg daily; severe impairment: 100 mg daily. Hepatic impairment: Max dose: 100 mg daily if serum albumin <3.5 g/dL. Intramuscular Acute exacerbations of musculoskeletal, joint, periarticular and soft-tissue disorders Adult: 50-100 mg by deep inj into the gluteal muscle every 4 hr. Max: 200 mg in 24 hr for up to 3 days. Intramuscular Pain following orthopaedic surgery Adult: 50-100 mg by deep inj into the gluteal muscle every 4 hr. Max: 200 mg in 24 hr for up to 3 days. Rectal Rheumatic disorders Adult: 100 mg at night or bid. Recommended total (including oral and rectal forms): Not to exceed 200 mg daily. Topical/Cutaneous Local pain relief Adult: Apply 2.5% gel onto affected areas 2-4 times daily for up to 10 days.

Food(before/after)

Should be taken with food. (Preferably taken w/ or after meals.)

List of Contraindications

Ketoprofen and Pregnancy

Caution when used during pregnancy. Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters). In 3rd trimester or near delivery: Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).

Ketoprofen and Lactation

Caution when used during lactation

Ketoprofen and Children

Safety and efficacy not established

Ketoprofen and Geriatic

Increased risk of adverse reactions

Ketoprofen and Other Contraindications

Acute or history of peptic ulcer or dyspepsia. Hypersensitivity to aspirin or other NSAIDs or those suffering from bronchial asthma, angioedema, urticaria or rhinitis. Severe renal insufficiency.

Storage

Intramuscular Store below 30 ℃. Oral Store at room temperature 15-30 ℃ (59-86 ° F). Rectal Store below 25 ℃ Topical/Cutaneous Store below 25 ℃

Lab interference

Intramuscular Store below 30 ℃. Oral Store at room temperature 15-30 ℃ (59-86 ° F). Rectal Store below 25 ℃ Topical/Cutaneous Store below 25 ℃

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