Hextrofen

Uses

Hextrofen is used for musculoskeletal and joint disorders such as ankylosing spondylitis, osteoarthritis, and rheumatoid arthritis, in periarticular disorders such as bursitis and tendinitis, in mild to moderate pain such as dysmenorrhoea or postoperative pain, and in other painful and inflammatory conditions such as acute gout or soft tissue disorders.

Hextrofen is used for symptomatic relief of mild to moderate pain, such as postoperative (including that associated with dental surgery) postpartum and orthopedic (including musculoskeletal strains or sprains) pain and visceral pain associated with cancer.

Hextrofen IM injection is used for management of acute exacerbations of: Rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, periarticular conditions such as fibrositis, bursitis, capsulitis, tendinitis, and tenosynovitis, low back pain of musculoskeletal origin, sciatica, other musculoskeletal conditions, acute gout and control of pain and inflammation following orthopaedic surgery.

Hextrofen 2.5% Gel is an anti-inflammatory and analgesic preparation to be applied topically to the painful area. It is used for a short-term treatment for traumatic lessions (sprains, tendinitis, edema, bruises) and pain.

Hextrofen is also used to associated treatment for these conditions: Ankylosing Spondylitis (AS), Migraine, Osteoarthritis (OA), Pain, Postpartum pain, Primary Dysmenorrhoea, Rheumatoid Arthritis

How Hextrofen works

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. Hextrofen 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. Hextrofen 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.

Dosage

Hextrofen dosage

Hextrofen Tablet: Oral treatment with Hextrofen is 50-100 mg daily, taken with food to minimize gastrointestinal disturbance. For rheumatic disease, 100-200 mg daily in 2-4 divided doses with food. For pain and dysmenorrhoea, 50 mg up to 3 times daily.

Hextrofen SR Capsule: 100-200 mg once daily, depending on patient’s weight and on severity of symptomsHextrofen IM injection:

• Adults: 50 to 100 mg every four hours, repeated up to a maximum of 200 mg in twenty-four hours for up to 3 days. Following a satisfactory response oral therapy should be instituted with Hextrofen tablet. It is recommended that the injection should not normally be continued for longer than three days.
• Elderly: As with other medications it is generally advisable in the elderly to begin ketoprofen therapy at the lower end of the dose range and to maintain such patients on the lowest effective dosage.
• Paediatric dosage: Not established for intramuscular use. It is not used as intravenous injection.

Hextrofen 2.5% Gel: Thisis to be applied to the painful area twice daily.The gel can be used with an occlusive dressing. Rub gently into the skin to ensure penetration.

For children: There is no contraindication to the use of this drug in children, but the appropriate dosage has not yet been established. Dosage of Hextrofen must be carefully adjusted according to individual requirements and response, using the lower possible effective dosage. Dosage exceeding 300 mg daily has not been adequately studied and are not recommended.

Suppository: 1 suppository (100 mg) late at night supplemented as required with Hextrofen capsules during daytime. Hextrofen suppositories are especially appropriate for controlling overnight symptoms (severity of night and morning pain; duration and severity of morning stiffness). Suppositoriesadministered late at night provide more consistent effective control of overnight symptoms than oral medication.

Side Effects

Adverse reactions to Hextrofen are usually mild and mainly involve the GI tract, particularly upper GI tract. Most Hextrofen-induced adverse effects occur during the first month of treatment, and the frequency of adverse effects generally decreases with continued therapy.

Adverse reactions involving digestive system are dyspepsia, nausea, abdominal pain, diarrhoea, constipation, flatulence, anorexia, vomiting, stomatitis and that involving nervous system are headache, dizziness, malaise, depression, nervousness, dreams, etc. Other reactions are tinnitus, visual disturbance, rash, impairment of renal function, signs or symptoms of urinary-tract irritation.

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.

Precaution

Hextrofen should be used with caution in patients who may be adversely affected by a prolongation of bleeding time (e.g. patients receiving anticoagulant therapy), since the drug may inhibit platelet function.

Hextrofen should be used with caution in patients with heart failure, hypertension, or other conditions associated with fluid retention, since peripheral edema has been observed in some patients receiving the drug.

Liver function should be monitored periodically during long-term Hextrofen therapy.

Hextrofen injection must not be given intravenously.

Hextrofen gel should not be applied to patients who have allergy toketoprofen, other anti-inflammatory agents and aspirin.

Interaction

As Hextrofen may cause GI bleeding, inhibit platelet aggregation and prolong bleeding time, the drug should be used with caution and the patient should be carefully observed if the drug is used concomitantly with any anticoagulant or thrombolytic agent. Concomitant administration of Hextrofen and hydrochlorothiazide has resulted in decreased urinary excretion of potassium and chloride compared with hydrochlorothiazide alone. Hextrofen and salicylates appear to interact in a complex manner and they should not be used concomitantly. Concomitant use of Hextrofen and probenecid is also not recommended. Hextrofen should be avoided in patients receiving methotrexate.

Food Interaction

• Avoid alcohol.
• Take with food. Food reduces irritation.

Hextrofen Alcohol interaction

[Moderate] GENERALLY AVOID:

The concurrent use of aspirin or nonsteroidal anti-inflammatory drugs (NSAIDs) and ethanol may lead to gastrointestinal (GI) blood loss.

The mechanism may be due to a combined local effect as well as inhibition of prostaglandins leading to decreased integrity of the GI lining.

Patients should be counseled on this potential interaction and advised to refrain from alcohol consumption while taking aspirin or NSAIDs.

Hextrofen Hypertension interaction

[Major] Fluid retention and edema have been reported in association with the use of nonsteroidal anti-inflammatory drugs (NSAIDs).

Therapy with NSAIDs should be administered cautiously in patients with preexisting fluid retention, hypertension, or a history of heart failure.

Blood pressure and cardiovascular status should be monitored closely during the initiation of NSAID treatment and throughout the course of therapy.

[Moderate] Nonsteroidal anti-inflammatory drugs (NSAIDs), including topicals, can lead to new onset of hypertension or worsening of preexisting hypertension, either of which can contribute to the increased incidence of cardiovascular events.

NSAIDs should be used with caution in patients with hypertension.

Blood pressure should be monitored closely during the initiation of NSAID therapy and throughout the course of therapy.

Hextrofen Drug Interaction

Moderate: aspirin, aspirin, duloxetine, duloxetine, escitalopram, escitalopramUnknown: zolpidem, zolpidem, pregabalin, pregabalin, esomeprazole, esomeprazole, acetaminophen, acetaminophen, acetaminophen, acetaminophen, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol

Hextrofen Disease Interaction

Major: asthma, fluid retention, GI toxicity, rash, renal toxicities, thrombosisModerate: anemia, heart failure, hepatotoxicity, hyperkalemia, hypertension, platelet aggregation inhibition

Elimination Route

Hextrofen is rapidly and well-absorbed orally, with peak plasma levels occurring within 0.5 to 2 hours.

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 [Hextrofen Immediate-release capsules (4 × 50 mg)]
• Oral-dose cl=6.8 +/- 1.8 L/h [Hextrofen Extended-release capsules (1 × 200 mg)]
• 0.08 L/kg/h
• 0.7 L/kg/h [alcoholic cirrhosis patients]

Elimination Route

In a 24 hour period, approximately 80% of an administered dose of ketoprofen is excreted in the urine, primarily as the glucuronide metabolite.

Pregnancy & Breastfeeding use

Embryopathic effects have not been recorded with Hextrofen, but it is recommended to avoid medication during pregnancy. Trace amounts of the drug appear in breast milk and it should not be used during breast feeding unless unavoidable.

Contraindication

Hextrofen is contraindicated in patients with known hypersensitivity to the drug. Hextrofen is contraindicated in patients in whom asthma, urticaria, or other sensitivity reaction is precipitated by aspirins or other NSAIDs, since severe, rarely fatal, anaphylactic reactions to Hextrofen have been reported in these patients.

The risk of potentially serious adverse GI effects should be considered in patients receiving Hextrofen, particularly in patients receiving chronic therapy with the drug. Hextrofen should be used in patients with GI bleeding or active peptic ulceration only when the potential benefits justify the possible risks.

Storage Condition

Store at cool and dry place, protect from light and moisture. Keep out of the children’s reach.

Innovators Monograph

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