TRAMADOL DENK 50 EFFERVESCENT TABLETS

Indications

• Moderate to moderately severe pain
• Postoperative pain
• Chronic pain syndromes

Dosage

Children: Refer to the BNF for Children for dosage recommendations in paediatric patients.

Adults: Refer to the BNF for specific dosing guidelines based on the condition being treated.

Mechanism of action

Tramadol binds to the mu-opioid receptor, providing analgesia through its action on the central nervous system. It also inhibits the reuptake of norepinephrine and serotonin, enhancing the descending inhibitory pathways in the spinal cord, which further contributes to its pain relief properties.

Pharmacodynamics

Tramadol exhibits a dual mechanism of action, as it not only interacts with opioid receptors but also affects the monoamine neurotransmitter systems. This unique combination may result in a lower potential for abuse compared to traditional opioids. The onset of analgesic effect typically occurs within one hour of oral administration, with peak effects reached in 2 to 3 hours. The duration of action varies depending on the formulation used.

Pharmacokinetics

Tramadol is well absorbed from the gastrointestinal tract, with bioavailability ranging from 68% to 100% due to first-pass metabolism. It is metabolized primarily in the liver through cytochrome P450 enzymes, particularly CYP2D6 and CYP3A4, into its active metabolite, O-desmethyltramadol. The elimination half-life is approximately 6 to 7 hours in healthy individuals. It is excreted mainly via the kidneys, with around 30% of the dose eliminated as unchanged drug.

Contra-indications

• Hypersensitivity to tramadol or any of the excipients
• Severe respiratory depression
• Acute or severe bronchial asthma
• Concurrent use with monoamine oxidase inhibitors (MAOIs) or within 14 days of stopping MAOIs
• Severe hepatic impairment
• Severe renal impairment
• Epilepsy not controlled by treatment

Adverse effects

• Nausea
• Dizziness
• Constipation
• Somnolence
• Headache
• Dry mouth
• Sweating
• Seizures
• Serotonin syndrome
• Dependence and withdrawal symptoms

Interactions

• CNS depressants (e.g., benzodiazepines, alcohol) may increase the risk of respiratory depression
• Serotonergic drugs may increase the risk of serotonin syndrome
• MAOIs can lead to severe interactions
• Antiepileptic drugs may have decreased efficacy
• Warfarin may have altered anticoagulant effects

Precautions

• Use cautiously in patients with a history of substance abuse
• Caution in patients with head injury or increased intracranial pressure
• Monitor for signs of respiratory depression, especially in elderly or debilitated patients
• Consider potential for seizures in patients with seizure disorders
• May impair ability to drive or operate machinery

Pregnancy

Tramadol should only be used during pregnancy if the potential benefit justifies the potential risk to the fetus. It is categorized as a pregnancy category C drug.

Breast-feeding

Tramadol is excreted in breast milk, and caution is advised if administered to nursing mothers.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

• Immediate-release tablets
• Extended-release tablets
• Oral solution
• Injection