Tramadol Hydrochloride

What it is and how it works

Mechanism of Action Tramadol hydrochloride extended-release tablet contains tramadol, an opioid agonist and an inhibitor of reuptake of norepinephrine and serotonin. Although the mode of action of tramadol is not completely understood, the analgesic effect of tramadol is believed to be due to both binding to µ-opioid receptors and weak inhibition of reuptake of norepinephrine and serotonin. Opioid activity of tramadol is due to both low affinity binding of the parent compound and higher affinity binding of the O-desmethyl metabolite M1 to µ-opioid receptors. In animal models, M1 is up to 6 times more potent than tramadol in producing analgesia and 200 times more potent in µ-opioid binding.

Indications

Tramadol hydrochloride extended-release tablets are indicated for the management of pain severe enough to require daily, around-the-clock, long-term opioid treatment and for which alternative treatment options are inadequate. Limitations of Use • Because of the risks of addiction, abuse, and misuse with opioids, even at recommended doses, and because of the greater risks of overdose and death with extended-release opioid formulations , reserve tramadol hydrochloride extended-release tablets for use in patients for whom alternative treatment options (e.g., non-opioid analgesics or immediate-release opioids) are ineffective, not tolerated, or would be otherwise inadequate to provide sufficient management of pain. • Tramadol hydrochloride extended-release tablets are not indicated as an as-needed (prn) analgesic. Tramadol hydrochloride extended-release tablets are an opioid agonist indicated for the management of pain severe enough to require daily around-the-clock, long-term opioid treatment and for which alternative treatment options are inadequate.

Dosage and administration (summary)

• To be prescribed only by healthcare providers knowledgeable in use of potent opioids for management of chronic pain. • Use the lowest effective dosage for the shortest duration consistent with individual patient treatment goals . • Individualize dosing based on the severity of pain, patient response, prior analgesic experience, and risk factors for addiction, abuse, and misuse. • Do not exceed a daily dose of 300 mg tramadol. Do not use with other tramadol products. • For opioid-naÏve and opioid non-tolerant patients, initiate tramadol hydrochloride extended-release tablets at a dose of 100 mg once daily, then titrate up by 100 mg increments every 5 days according to need and tolerance.

Contraindications

Tramadol hydrochloride extended-release tablets are contraindicated for: • all children younger than 12 years of age • post-operative management in children younger than 18 years of age following tonsillectomy and/or adenoidectomy . Tramadol hydrochloride extended-release tablets are also contraindicated in patients with: • Significant respiratory depression • Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment • Known or suspected gastrointest…

Warnings and precautions

• Serotonin Syndrome with Concomitant Use of Serotonergic Drugs : Potentially life-threatening condition could result from concomitant serotonergic drug administration. Discontinue tramadol hydrochloride extended-release tablets if serotonin syndrome is suspected. • Risk of Seizure : Present within recommended dosage range.

Pregnancy

Pregnancy Risk Summary Prolonged use of opioid analgesics during pregnancy may cause neonatal opioid withdrawal syndrome . Available data with tramadol hydrochloride extended-release tablets in pregnant women are insufficient to inform a drug-associated risk for major birth defects and miscarriage.

Storage and supply

Tramadol hydrochloride extended-release tablets USP are supplied in the following package and dose strength forms: 200 mg tablets (white to off-white circular, biconvex, beveled edge, coated) imprinted with 'L011' on one side and plain on the other side.

Source: Tramadol Hydrochloride (Tramadol Hydrochloride) — US FDA prescribing information, 2022-11-01, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.