Generic Name

Tramadol Hydrochloride

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Classification

FDA Approved Indications

• Moderate to severe pain in adults

Mechanism of Action

Tramadol is a centrally acting synthetic opioid that binds to mu-opioid receptors and inhibits reuptake of norepinephrine and serotonin, enhancing descending inhibitory pain pathways.

Dosage and Administration

Adult: Start with 25 mg to 50 mg every 4 to 6 hours as needed. Max dose is 400 mg per day.

Pediatric: Not recommended for children under 12 years.

Geriatric: Start at lower end of dosing range; monitor closely, especially in patients over 75.

Renal Impairment: Use with caution; consider dose reduction in severe impairment.

Hepatic Impairment: Use with caution; may require dose adjustment and close monitoring.

Pharmacokinetics

Absorption: Well-absorbed orally, with peak plasma concentrations in 2 hours (immediate-release) and up to 4 hours (extended-release).

Distribution: Widely distributed; crosses the blood-brain barrier and placenta.

Metabolism: Extensively metabolized in the liver via CYP2D6 and CYP3A4 to active and inactive metabolites.

Excretion: Primarily renal; approximately 30-40% of unchanged drug excreted in urine.

Half Life: Approximately 6 hours for immediate-release; longer for extended-release formulations.

Contraindications

• Hypersensitivity to tramadol or opioids.
• Use in patients with respiratory depression.
• Use within 14 days of monoamine oxidase inhibitors (MAOIs).

Precautions

• History of substance abuse, seizures, increased intracranial pressure, hepatic impairment, and in elderly patients. Caution in pregnancy and lactation.

Adverse Reactions - Common

• Nausea (Common)
• Dizziness (Common)
• Constipation (Common)
• Headache (Common)

Adverse Reactions - Serious

• Serotonin syndrome (Rare)
• Breathing difficulties or respiratory depression (Rare)
• Seizures (Rare, increased in those with seizure disorder or with dose escalation)
• Allergic reactions including rash, angioedema, anaphylaxis (Rare)

Drug-Drug Interactions

• Other serotonergic drugs (SSRIs, SNRIs, triptans), other opioids, benzodiazepines, CYP2D6 inhibitors, CNS depressants.

Drug-Food Interactions

• No significant food interactions identified.

Drug-Herb Interactions

• Caution with herbal products affecting CYP enzymes or serotonergic activity.

Nursing Implications

Patient/Family Teaching

• Take medication exactly as prescribed.
• Do not exceed the recommended dose.
• Be aware of potential side effects, including dizziness and nausea.
• Use caution when performing tasks requiring alertness.
• Avoid alcohol and other CNS depressants.
• Seek medical attention for signs of severe reactions, including difficulty breathing or seizures.

Special Considerations

Black Box Warnings:

• Risks of respiratory depression, addiction, adverse cognitive effects, and accidental ingestion.
• Serious adverse reactions can occur with concomitant use of serotonergic drugs, risking serotonin syndrome.

Genetic Factors: Patients with CYP2D6 ultrarapid metabolizer genotype may experience increased effects and side effects.

Lab Test Interference: May affect certain hepatic function tests due to hepatic metabolism.

Overdose Management

Signs/Symptoms: Respiratory depression, sedation, miosis, seizures, hypotension, coma.

Treatment: Supportive care, including airway management, naloxone administration for respiratory depression, seizure control with anticonvulsants, and monitoring in an intensive setting.

Storage and Handling

Storage: Store at room temperature away from moisture, heat, and light.

Stability: Stable under recommended storage conditions for the duration of the product's shelf life.