Product Information
Registration Status: ActiveFASTUM GEL MAX 2.5% is approved to be sold in Singapore with effective from 2018-07-11. It is marketed by A. MENARINI SINGAPORE PTE LTD, with the registration number of SIN15511P.
This product contains Ketoprofen 2.5g/100g in the form of GEL. It is approved for TOPICAL use.
This product is manufactured by A. Menarini Manufacturing Logistics and Services S.R.L. in ITALY.
It is an Over-the-counter Medicine that can be freely obtained from any retailer
Description
Ketoprofen, a propionic acid derivative, is a nonsteroidal anti-inflammatory agent (NSAIA) with analgesic and antipyretic properties.
Indication
For symptomatic treatment of acute and chronic rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, primary dysmenorrhea and mild to moderate pain associated with musculotendinous trauma (sprains and strains), postoperative (including dental surgery) or postpartum pain.
Mechanism of Action
The anti-inflammatory effects of ketoprofen are believed to be due to inhibition cylooxygenase-2 (COX-2), an enzyme involved in prostaglandin synthesis via the arachidonic acid pathway. This results in decreased levels of prostaglandins that mediate pain, fever and inflammation. Ketoprofen is a non-specific cyclooxygenase inhibitor and inhibition of COX-1 is thought to confer some of its side effects, such as GI upset and ulceration. Ketoprofen is thought to have anti-bradykinin activity, as well as lysosomal membrane-stabilizing action. Antipyretic effects may be due to action on the hypothalamus, resulting in an increased peripheral blood flow, vasodilation, and subsequent heat dissipation.
Pharmacokinetics
- Absorption
- Ketoprofen is rapidly and well-absorbed orally, with peak plasma levels occurring within 0.5 to 2 hours.
- Distribution
- Metabolism
- Rapidly and extensively metabolized in the liver, primarily via conjugation to glucuronic acid. No active metabolites have been identified.
- Elimination
Clearance
* Oral-dose cl=6.9 +/- 0.8 L/h [Ketoprofen Immediate-release capsules (4 × 50 mg)] * Oral-dose cl=6.8 +/- 1.8 L/h [Ketoprofen Extended-release capsules (1 × 200 mg)] * 0.08 L/kg/h * 0.7 L/kg/h [alcoholic cirrhosis patients]
Toxicity
LD50=62.4 mg/kg (rat, oral).
Symptoms of overdose include drowsiness, vomiting and abdominal pain.
Side effects are usually mild and mainly involved the GI tract. Most common adverse GI effect is dyspepsia (11% of patients). May cause nausea, diarrhea, abdominal pain, constipation and flatulence in greater than 3% of patients.
Active Ingredient/Synonyms
2-(3-Benzoylphenyl)propionic acid | 3-Benzoyl-alpha-methylbenzeneacetic acid | 3-Benzoyl-α-methylbenzeneacetic acid | 3-Benzoylhydratropic acid | Ketoprofen | L'Acide (benzoyl-3-phenyl)-2-propionique | m-Benzoylhydratropic acid | Orudis (tn) | Ketoprofen |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.