Introduction
Keto-A Suppository 100 mg, a propionic acid derivative, is a nonsteroidal anti-inflammatory agent (NSAIA) with analgesic and antipyretic properties.
Uses
Keto-A Suppository 100 mg is an NSAID used to treat rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, dysmenorrhea, mild to moderate muscle pain, postoperative pain, and postpartum pain.
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.
Associated Conditions
Pharmacodynamics
Keto-A Suppository 100 mg is a nonsteroidal anti-inflammatory agent (NSAIA) with analgesic and antipyretic properties. Keto-A Suppository 100 mg has pharmacologic actions similar to those of other prototypical NSAIDs, which inhibit prostaglandin synthesis. Keto-A Suppository 100 mg is used to treat rheumatoid arthritis, osteoarthritis, dysmenorrhea, and alleviate moderate 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. Keto-A Suppository 100 mg 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. Keto-A Suppository 100 mg 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.
Absorption
Keto-A Suppository 100 mg is rapidly and well-absorbed orally, with peak plasma levels occurring within 0.5 to 2 hours.
Protein Binding
99% bound, primarily to albumin
Route of Elimination
In a 24 hour period, approximately 80% of an administered dose of ketoprofen is excreted in the urine, primarily as the glucuronide metabolite.
Half Life
Conventional capsules: 1.1-4 hours
Extended release capsules: 5.4 hours due to delayed absorption (intrinsic clearance is same as conventional capsules)
Clearance
- Oral-dose cl=6.9 +/- 0.8 L/h [Keto-A Suppository 100 mg Immediate-release capsules (4 × 50 mg)]
- Oral-dose cl=6.8 +/- 1.8 L/h [Keto-A Suppository 100 mg 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.
Food Interactions
- Avoid alcohol.
- Take with food. Food reduces irritation.
Dosage
Cattle:
- For deep intramuscular or intravenous use. 1 ml/33 kg body weight (3 mg/kg body weight) once daily for 3 days.
- For musculoskeletal disorder: 1 ml/45 kg body weight (2.2 mg /kg) by intravenous injection once daily
- for 3 to 5 days.
- For equine colic: 1 ml/45 kg body weight (2.2 mg/kg) by intravenous injection. A second injection may be given if colic recurs.
- Cattle: 1 bolus per 100 kg body weight (4 mg/kg) orally daily for upto 3 days. Or As directed by the Veterinary physician.