KETESSE 25MG

Indications

• Pain and inflammation in musculoskeletal disorders
• Pain and inflammation in osteoarthritis
• Pain and inflammation in rheumatoid arthritis
• Pain relief in other mild to moderate pain conditions

Dosage

Children: Refer to BNF for Children for appropriate dosing information.

Adults: Adult: 12.5 mg every 4–6 hours, alternatively 25 mg every 8 hours; maximum 75 mg per day.

Mechanism of action

Dexketoprofen exerts its effects by reducing prostaglandin synthesis through the inhibition of the cyclooxygenase pathway, specifically targeting both COX-1 and COX-2 enzymes. This leads to decreased inflammation and pain signaling in the body.

Pharmacodynamics

As an isomer of ketoprofen, dexketoprofen is recognized for its analgesic and anti-inflammatory effects. It is classified as a propionic acid derivative, which means it shares similar properties with other drugs in this class, providing effective pain relief and reducing inflammation.

Pharmacokinetics

Dexketoprofen is rapidly absorbed after oral administration, with peak plasma concentrations typically occurring within 1-2 hours. It has a half-life of approximately 1-2 hours, allowing for relatively frequent dosing to maintain therapeutic effects. The drug is primarily metabolized in the liver and excreted via the kidneys, and dose adjustments may be necessary in patients with hepatic or renal impairment.

Contra-indications

• History of hypersensitivity to aspirin or any other NSAID
• Active gastrointestinal bleeding
• Active gastrointestinal ulceration
• Cerebrovascular disease
• Inflammatory bowel disease
• Ischaemic heart disease
• Mild to severe heart failure
• Peripheral arterial disease

Adverse effects

• Gastrointestinal discomfort
• Nausea
• Drowsiness
• Fluid retention
• Skin reactions
• Chest pain
• Myocardial infarction
• Depression
• Conjunctivitis
• Constipation

Interactions

• Concurrent use of fluconazole may require dose adjustment
• Risk of renal impairment with other NSAIDs or in patients with renal insufficiency

Precautions

• Use caution in patients with hepatic impairment
• Monitor blood pressure before and during treatment
• Long-term use may reduce female fertility, reversible on stopping treatment

Pregnancy

Avoid, as it is teratogenic in animal studies.

Breast-feeding

Avoid, as it is present in milk in animal studies.

Storage

Store at room temperature, away from moisture and heat.

Formulations

• 100 mg capsules
• 25 mg and 12.5 mg capsules

Indications

• Moderate to severe pain
• Postoperative pain
• Pain due to injury or trauma
• Chronic pain conditions

Dosage

Children: Refer to the BNF for Children for appropriate pediatric dosing guidelines.

Adults: Refer to the BNF for specific dosing information. Generally, initial dosing may vary based on the severity of pain and individual patient factors.

Mechanism of action

Trametamol is thought to exert its analgesic effects through two main pathways: it inhibits the reuptake of serotonin and norepinephrine in the central nervous system, which contributes to its pain-relieving properties. Additionally, trametamol is metabolized to O-desmethyltramadol, an active metabolite that binds to μ-opioid receptors, further enhancing its analgesic effects.

Pharmacodynamics

Trametamol provides analgesia primarily by modulating pain pathways in the brain and spinal cord. The inhibition of serotonin and norepinephrine reuptake enhances descending inhibitory pathways, reducing pain perception. Its action on opioid receptors contributes to its efficacy in pain management. The combination of these actions results in effective pain relief with a potentially lower risk of opioid-related side effects compared to stronger opioids.

Pharmacokinetics

Trametamol is well absorbed from the gastrointestinal tract, with peak plasma concentrations typically occurring within 1 to 2 hours after oral administration. It undergoes extensive metabolism in the liver, primarily through cytochrome P450 enzymes, leading to the formation of O-desmethyltramadol. The elimination half-life is generally around 6 to 8 hours. The drug and its metabolites are excreted mainly via the kidneys, thus renal function can affect clearance.

Contra-indications

• Hypersensitivity to trametamol or any of its components
• Severe respiratory depression
• Acute or severe bronchial asthma
• Severe hepatic impairment
• Concurrent use with monoamine oxidase inhibitors (MAOIs) or within 14 days of stopping such treatment

Adverse effects

• Nausea
• Vomiting
• Constipation
• Dizziness
• Drowsiness
• Headache
• Rash
• Allergic reactions
• Dependence potential with prolonged use

Interactions

• Caution with other central nervous system depressants, including alcohol, benzodiazepines, and opioids due to additive effects
• May enhance the anticoagulant effects of warfarin and other anticoagulants
• Potential interaction with serotonergic drugs, increasing the risk of serotonin syndrome

Precautions

• Use with caution in patients with a history of drug dependence or abuse
• Monitor renal and hepatic function in long-term users
• Caution in elderly patients and those with pre-existing respiratory conditions
• Avoid abrupt withdrawal after prolonged use to prevent withdrawal symptoms

Pregnancy

Trametamol should only be used in pregnancy if the potential benefit justifies the potential risk to the fetus. Limited data is available on its safety during pregnancy.

Breast-feeding

Trametamol is excreted in breast milk. Caution is advised when administered to nursing mothers, and it should only be used if necessary.

Storage

Store in a cool, dry place away from direct sunlight. Keep out of reach of children. Do not use after the expiry date.

Formulations

• Oral tablets
• Oral solution
• Injectable forms

Mechanism of action

It is a non-steroidal anti-inflammatory drug (NSAID) that reduces prostaglandin synthesis via inhibition of cyclooxygenase pathway (both COX-1 and COX-2) activity.

Pharmacodynamics

This drug is an isomer of ketoprofen. Dexketoprofen a propionic acid derivative with analgesic, anti-inflammatory, and antipyretic properties.