Tramadol (Tramadol)

Trade name drugs: tramadol

International Nonproprietary Name: tramadol (tramadol)

Chemical name: (RR, SS0-2-(dimetilaminometil) -1 – (3-methoxyphenyl) cyclohexanol hydrochloride

Dosage form: tablets

Ingredients:

1 tablet contains 50 mg of tramadol hydrochloride.

Excipients:
Lactose, microcrystalline cellulose, magnesium stearate, crospovidone, macrogol 4000, saccharin sodium, colloidal silicon dioxide, flavor.

Description: white or almost white, round biconvex tablets with a notch on one side and a characteristic smell of strawberries.

Pharmacological properties:

Pharmacotherapeutic group: opioid with mixed mechanism of action. N02AH02

Pharmacodynamics:
Refers to the means of the central analgesic action. Has anesthetic effect.
Nonselective antagonist of opioid mu, delta and kappa receptors in the CNS with the highest affinity for mu receptors. Inhibits neuronal capture of noradrenaline and enhances the release of serotonin. Has also antibechic action does not violate the motility of the gastro – intestinal tract. Duration – approximately 4-8 hours.

Pharmacokinetics:
Suction: After receiving tramadol fast and almost completely absorbed from the gastro – intestinal tract (90%). Maximum concentration in plasma determined after approximately 2 hours. The value of the biological availability is about 70%, independent of food intake and increases with repeated application of the drug.
Distribution: Plasma protein binding is about 20%. Tramadol crosses the blood-entsefallichesky and placental barriers. Approximately 0.1% is excreted in breast milk.
Metabolism: metabolized by demethylation and conjugation to 11 metabolites, only one of which (O-demetiltramadol) has marked pharmacological activity (2-4 times greater activity than tramadol).
Derivation: Tramadol and its metabolites are primarily renally (90%) and through the intestine (about 10%). The half-life, regardless of the route is about 6 hours.
Patients in the elderly, with liver cirrhosis and renal failure half-life value increases.

Indications:

Pain syndrome secondary to severe intensity of various etiology (postoperative period, trauma, pain in cancer patients).
To analgesia during painful diagnostic or
therapeutic manipulation.

Contraindications:

Increased sensitivity to the drug.
States, accompanied by respiratory depression or marked depression of the central nervous system (alcohol poisoning, sleeping pills, narcotic analgesics, psychotropic drugs). The simultaneous use of MAO inhibitors (and two weeks after their withdrawal). Pregnancy and Lactation (application is possible only for health reasons).
Age 14 years.

Pregnancy and lactation:
In pregnancy, should avoid prolonged use of tramadol because the risk of addiction in the fetus and the emergence of withdrawal syndrome in the neonatal period.
If necessary, admission to the lactation period should take into account that tramadol in small amounts excreted in breast milk.

Dosage and administration:

Dose podbiraetsya physician individually depending on the intensity and nature of pain.
Adults and adolescents older than 14 years:
Typically, the initial dose – 1 tablet (50 mg) orally with a small amount
fluid, regardless of meal times, with no effect during 30 – 60 minutes can take 1 more pill with a single dose of strong pain may soon reach 100 mg (2 tablets). The effect, depending on the degree of pain persists for 4-8 hours. Do not exceed the daily dose of tramadol 400 mg (8 tablets).
Children: Do not take this dosage form for children weighing less than 25 kg and aged less than 14 years.
Older patients, patients with impaired hepatic function and kidney: If you want to receive should increase the interval between doses of the drug.
The duration and pattern of use are determined by the attending physician
Tablets can be swallowed without chewing, washing down the necessary quantity of liquid, with or without food or pre-dissolved in 1 / 2 cup water.

Side effects:

The most characteristic dizziness, nausea, constipation, headache, drowsiness
(these side effects occur in 30 – 15% of patients receiving tramadol), vomiting, skin itching, symptoms of psychostimulant action, asthenia, sweating, dyspepsia, dry mouth, diarrhea (there are 15 – 5% of patients).
With a frequency of less than 5% of their weight loss, hypotension and tachycardia, paresthesia, hallucinations, tremors, abdominal pain, blurred vision, urinary retention.
The frequency of adverse effects increases with duration of dosing. With prolonged use at high doses can not exclude the possibility of drug dependence.
On all the side effects, including those not listed above, should be reported
doctor.

Overdose (intoxication) drug. The most dangerous effects of overdose of tramadol are pupillary constriction, vomiting, respiratory depression and convulsions. If you suspect a poisoning should immediately seek medical help.
First aid for poisoning – the maintenance of adequate pulmonary ventilation and symptomatic therapy in a specialized department. In mild cases enough gastric lavage. Application of naloxone is not critical, since does not resolve all the symptoms of poisoning and can cause convulsions. Hemodialysis is ineffective. In convulsions appropriate intravenous diazepam.

Special instructions:

With increased time intervals used tramadol in elderly patients. With caution and under the supervision of a physician should use the drug to patients with impaired renal function and liver in cases of cranial trauma, increased intracranial pressure, patients with epilepsy, as well as individuals with drug addiction to opioids.
Under close medical supervision and in small doses should be applied against the background of tramadol of action for narcosis, hypnotics and psychotropic drugs. The drug should not be combined with narcotic analgesics because of the poor predictability of the effect of interaction.
Against the background of the prolonged use of carbamazepine effect of tramadol may be weaker.
Avoid drinking alcohol in the treatment of tramadol.
In applying Tramadol should not drive or perform other work that requires increased attention.

Interaction with other medication:

In an application with tramadol drugs, providing a depressing effect on the central nervous system, as well as with ethanol, may increase their actions.
In an application trmadola with carbamazepine and other inducers of metabolic enzymes may weaken analgesic action of tramadol.
When systematic admission of barbiturates, especially phenobarbital, is likely to reduce the analgesic action of opioid analgesics. Prolonged use of opioid analgesics, or barbiturates stimulate the development of cross-tolerance.
Naloxone activates respiration, eliminating analgesia after application of opioid analgesics.

Method of issuance:

10 tablets containing 50 mg of tramadol d / x in blisters of PVC (or polypropylene) / aluminum.
At 1, 2, 3 or 5 blisters together with instructions for use in a carton.

Expiration:

Shelf life is 5 years.
You should not use the medicine after the expiration on the package shelf life.

Storage:

List B. Store at temperatures above 25 C in the reach of children.

Conditions of supply of pharmacies:

Dispensed from pharmacies by prescription.