Dolotral

Dolotral

tramadol

Manufacturer:

Stada

Distributor:

Croma Medic
Full Prescribing Info
Contents
Tramadol HCl.
Action
Pharmacology: Tramadol HCl is a cyclohexanol derivative with central analgesic and antitussive activities. Tramadol (and its active M1 metabolite) acts as an opiate agonist, apparently by selective activity at the mc-receptor. In addition to opiate agonist activity, tramadol inhibits reuptake of certain monoamine (norepinephrine, serotonin) which appears to contribute to its analgesic effect. Unlike morphine, tramadol has no respiratory depressant effect over a wide range of analgesic doses. It also does not affect gastrointestinal motility. Its effects on the cardiovascular system are relatively slight.
Pharmacokinetics: Following oral administration (100 mg), tramadol is rapidly and almost completely absorbed. The mean absolute bioavailability of tramadol after oral administration, irrespective of simultaneous food intake is 68%; following rectal administration it is 79%; and following IM administration 100%. The maximum first-pass effect after oral administration is 30% and after rectal administration 20%. Tramadol crosses the blood-brain barrier and the placental barrier. It is found in breast milk, together with its O-demethyl derivative in very low concentration (0.1% and 0.02% respectively, of the administered dose). The elimination half-life (t½), irrespective of the route of administration, is 5-7 hrs. This is slightly prolonged in patients >65 years. Tramadol and its metabolites are almost entirely excreted by the kidney. In the presence of disorders of hepatic and renal function, the half-lives are likely to be somewhat prolonged.
Indications/Uses
For moderate to severe pain.
Dosage/Direction for Use
The following dosage guidelines should be used unless otherwise prescribed by the physician.
Tramadol should not in any circumstances be used longer than therapeutically absolutely necessary. If the nature and severity of the disease makes more prolonged analgesic treatment with tramadol necessary, a regular, careful and frequent check should be carried out (possibly by the use of treatment-free intervals) to determine whether and to what extent a medical requirement still exists. Tramadol dosage should be adjusted to the severity of pain and the patient's individual sensitivity.
Adults and adolescents >14 years: For moderately severe pain, tramadol should be given according to the following dosages (single dose):
Capsule: 1-2 caps. Single oral doses of tramadol HCl ranging from 50-200 mg has provided relief of postoperative pain in patients who have undergone various types of surgery.
If a dose of 1 cap is not followed by adequate pain relief within 30-60 min, a 2nd single dose of 1 capsule may be given.
In severe pain, if clinical experience suggests that a higher analgesic dose is likely to be required, the initial dose may be 2 capsules. Tramadol tablet is not suitable for children weighing <25 kg and cannot usually be dosed individually for children <14 years. An oral solution and an injectable solution are available for this purpose.
IV/IM/SC: 1 ampoule tramadol equivalent to 100 mg tramadol HCl. For IV: Inject slowly or infuse diluted in an infusion solution.
If the analgesic effect is inadequate, a second single dose may be administered after 30-60 min. In severe pain, if clinical experience suggests that a higher analgesic requirement can be expected, the higher dose of tramadol may be used initially. For the treatment of severe postoperative pain, tramadol doses of up to 500 mg/4 hrs may be used in an on-demand analgesic system. This, however, requires monitoring facilities and special apparatus.
Children ≥1 year: Experience to date suggests that tramadol HCl may be used at doses of 1-2 mg/kg body weight.
The duration of action of tramadol HCl is on average 4-8 hrs, depending on the severity of pain when therapeutic doses are given.
Daily dose of up to 8 caps/4 ampoules of tramadol (400 mg) are generally adequate. When tramadol infusions are used intraoperatively, or in the treatment of tumor-induced pain, however, much higher daily doses have been used (150-400 mg daily in divided doses). The duration of action of tramadol may be prolonged in patients with disorders of renal or hepatic function. The need for dosage alterations in elderly patients is under discussion.
There is some evidence that elderly patients require lower doses of tramadol than younger patients. Creatinine clearance should be monitored and used as a determining factor for dosage adjustment. Age alone is not a sufficient criteria for dosage adjustment. While the usual oral tramadol HCl dosage of 50-100 mg every 4-6 hrs as needed can be used in geriatric patients ≥65 years with normal renal and hepatic function, it is recommended that dosage not exceed 300 mg daily in those >75 years. Dosage of tramadol HCl should be reduced in certain patients with renal or hepatic impairment by decreasing the frequency of administration.
Adults and children ≥16 years with creatinine clearance <30 mL/min: 50-100 mg every 12 hrs, not exceeding 200 mg daily. Since <10% of a dose of tramadol HCl is removed by hemodialysis, patients undergoing dialysis may receive their usual dosage on the day of dialysis.
Adults and children ≥16 years with hepatic cirrhosis: 50 mg every 12 hrs. The capsule should be taken with a little fluid, without relation to mealtimes.
Note: The recommended dosages are guidelines only. In principle, the lowest effective analgesic dose should be chosen. In the treatment of chronic pain, strict time-tabling of doses is preferred.
Overdosage
The following typical symptoms of overdosage have been observed: Disturbances of consciousness extending to coma; generalized epileptic fits, hypotension, tachycardia, constricted or dilated pupils, respiratory depression extending to respiratory arrest.
These effects can be abolished by administration of an opiate antagonist (eg, naloxone), which should be administered cautiously in repeated small doses, since its duration of action is shorter than that of tramadol. In addition, intensive care measures (particularly ventilation and incubation) should also be introduced. If fits occur, the use of benzodiazepines should be considered. In addition, measures to prevent heat loss and volume replacement therapy may be required. In oral intoxication with tramadol, gastric lavage may be useful. Some manifestations of overdose eg, seizures may not be reversible with an opiate antagonist eg, naloxone.
Contraindications
Dolotral must not be used in patients with: Hypersensitivity to tramadol; acute intoxication with alcohol, analgesics, sedatives or psychotropic drugs; patients receiving MAOI.
Special Precautions
Misuse and dependence are possible with tramadol. Tramadol is not suitable for drug substitution. If the recommended dosage is exceeded, as occasionally occurs particularly during general anesthesia, respiratory depression should be expected. Similarly, if the recommended dosage is exceeded and other central nervous depressant drugs are simultaneously used, respiratory suppression should be allowed for. The duration of action is prolonged in patients with disorders of hepatic or renal function. The dosage interval should therefore be prolonged in such cases, if necessary allowing for recurrence of pain. IV injections should be given slowly.
Caution should be taken in patients with previous hypersensitivity to morphine-like analgesic, patients with head injury and history of seizures. In patients with myxedema, hypothyroidism or hypoadrenalism, dose reduction may be required.
Dolotral should be used with caution in: Opiate dependence, disturbance of consciousness of unknown cause, disorders of function of the respiratory center, conditions with raised intracranial pressure, unless artificial ventilation is being given, children <1 year.
Effects on the Ability to Drive or Operate Machinery: Even when tramadol is used appropriately, the capacity to drive in traffic or operate machinery may be abolished.
Use in pregnancy & lactation: Tramadol crosses the placenta. No teratogenic effects of tramadol has been observed in animals. However, adequate systematic studies have not been carried out. Chronic treatment should be avoided throughout pregnancy. In neonates, tramadol may lead to changes in respiratory rate, which are usually of no importance. When given to breastfeeding mothers, tramadol is excreted in the breast milk at a concentration of approximately 0.1% of the maternal plasma concentration. With a single dose of tramadol, interruption of breastfeeding is usually unnecessary.
Use In Pregnancy & Lactation
Tramadol crosses the placenta. No teratogenic effects of tramadol has been observed in animals. However, adequate systematic studies have not been carried out. Chronic treatment should be avoided throughout pregnancy. In neonates, tramadol may lead to changes in respiratory rate, which are usually of no importance. When given to breastfeeding mothers, tramadol is excreted in the breast milk at a concentration of approximately 0.1% of the maternal plasma concentration. With a single dose of tramadol, interruption of breastfeeding is usually unnecessary.
Side Effects
Tramadol produces dose-dependent respiratory depression and sedation of varying degree (from mild fatigue to dizziness). Nausea, sweating, dry mouth, dizziness and giddiness may occasionally occur. Effects on the circulation (palpitations, tachycardia, faintness or circulatory collapse) are possible in rare cases. These adverse effects are particularly liable to occur when in the upright posture, when Dolotral is given IV or in patients undergoing physical stress.
In addition, headache, nausea, vomiting, constipation, gastrointestinal irritation (abdominal pressure, feeling of fullness) and skin reactions (eg, pruritus, rashes) may rarely occur. Very rare effects include muscular weakness, alterations in appetite and disturbances of micturition.
On very rare occasions, tramadol shows a variety of psychological side effects, varying in nature and intensity from individual to individual, depending on personality and duration of treatment. They include alterations in mood (usually elevated but sometimes in gloomy mood known as dysphoria), alterations in activity (usually suppression, sometimes intensification) and alteration in memory (eg, decision-taking, disturbances of perception). There have been few cases of cerebral convulsions. These however, almost always occurred following IV administration of high doses of tramadol with concomitant treatment with neuroleptic agents. Allergic reactions, extending to shock, cannot be reliably ruled out.
Skin diaphoresis has been reported in up to 20% of patients treated with oral/parenteral tramadol.
Drug Interactions
Simultaneous use of tramadol and other drugs with a central nervous inhibitory effect or alcohol can lead to potentiation of the central nervous side effects of tramadol, particularly respiratory depression. When concomitant medication with neuroleptic drugs is given, convulsions have been observed in a few cases.
The effect of treatment with cimetidine (a drug for the treatment of gastric ulcers and gastric mucosal irritation) on the excretion of tramadol is so slight that the alterations in analgesic effect attributable to this effect are insignificant.
When patients have been treated with MAO inhibitors (drugs for treatment of psychiatric disorders) within the last 14 days before opioid administration, life-threatening interactions affecting the central nervous system, respiratory and circulatory function have been observed with pethidine (another analgesic agent in the same group), and such effects cannot be excluded in the case of tramadol.
Increased incidence of seizures may occur with concomitant administration of tricyclic antidepressants eg, cyclobenzaprine, MAOI, Selective Serotonin Reuptake Inhibitors (SSRIs), neuroleptic agents and other drugs that lower the seizure threshold. Tramadol may potentiate the effects of other CNS depressants (alcohol, sedatives, hypnotic, other centrally acting analgesics, opiate agonists). The drug should be used with caution, and dosage of tramadol may need to be reduced in patients receiving such drugs.
Note: Tramadol possesses a potential for dependency. With long-term usage, tolerance, psychological and physical dependence may develop. There is cross-tolerance with other opioids.
Storage
Store at temperatures not exceeding 30°C. Keep dry.
ATC Classification
N02AX02 - tramadol ; Belongs to the class of other opioids. Used to relieve pain.
Presentation/Packing
Soln for inj (amp) 100 mg/2 mL x 5's.
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