- active ingredient: tramadol;
- 1 ml solution contains tramadol hydrochloride 50 mg;
- auxiliary substances: sodium acetate, trihydrate; water for injection.
- Medicinal form. Solution for injection.
- The main physical and chemical properties: a transparent colorless liquid.
- Pharmacotherapeutic group. Analgesics. Opioids. Tramadol. ATX code N02A X02.
- Pharmacological properties.
Tramadol dosage – central active opioid analgesic. Has a mixed mechanism of action. It is a non-selective pure opioid μ-, d- and ?-receptor agonist with maximum affinity for μ-receptors. Other mechanisms involved in providing tramadol analgesic effect are inhibition of noradrenaline reverse capture in neurons and serotonergic response enhancement. Tramadol also has an anti coughing effect. In contrast to morphine, tramadol analgesic doses over a wide range do not inhibit respiration. The motor of the digestive tract is also less inhibited. The effect on the cardiovascular system is usually weak. The activity of tramadol is estimated in the range from 1/10 to 1/6 of morphine activity.
Pharmacokinetics. Absorption at intramuscular injection – 100%. Time to reach maximum concentration in plasma after intramuscular injection – 45 minutes. Absolute bioavailability – almost 70%. Binding to blood proteins is approximately 20%. It penetrates through hematoencephalic and placental barriers. 0.1% of the drug penetrates breast milk. It is metabolized in the liver. The half-life period is 6 hours. Tramadol and its metabolites are excreted by kidneys (25-35 %) in unchanged form. Approximately 7 % is eliminated by hemodialysis.
Treatment of moderate to severe pain Ultram Contraindications
Hypersensitivity to tramadol or other components of the drug. Acute alcohol intoxication; acute poisoning with sleeping pills, analgesic, opioid or psychotropic drugs; severe hepatic/renal insufficiency (creatinine clearance less than 10 ml/min); simultaneous use of MAO inhibitors (and 2 weeks after their withdrawal); epilepsy uncontrolled by treatment; drug withdrawal syndrome. Interaction with other drugs and other types of interactions Tramadol ultram, a solution for injection, should not be used together with MAO inhibitors. Life threatening reactions affecting the central nervous, respiratory and cardiovascular systems were observed in patients receiving MAO inhibitors for 14 days before opioid pethidine was administered. Similar interactions with MAO inhibitors cannot be ruled out when tramadol is used.
Simultaneous use of tramadol and medications depressing the central nervous system (CNS), including alcohol, may increase their effect on the CNS. Pharmacokinetic studies have shown that concomitant or preliminary use of cimetidine (an enzyme inhibitor) is unlikely to result in clinically significant interactions. Simultaneous or preliminary application of carbamazepine (enzyme inhibitor) may reduce analgesic effect and shorten the duration of the drug action. A combination of mixed agonists/antagonists (e.g. buprenorphine, nalbufin, pentazocin) and tramadol is not recommended, since with such a combination https://reference.medscape.com/drug/ultram-er-tramadol-343324, the analgesic effect of a pure agonist may theoretically be reduced.