TRAMADOL (Capsules)

Active material: Tramadol
When ATH: N02AX02
CCF: Opioid analgesic with a mixed mechanism of action
When CSF: 03.01.04
Manufacturer: HEMOFARM A.D. (Serbia)

Pharmaceutical form, composition and packaging

Capsules hard gelatin, size №4, kryshecka capsules case and opaque, yellow color; contents of capsules – powder from white to almost white.

Excipients: microcrystalline cellulose, sodium carboxymethyl, magnesium stearate.

Ingredients of the capsule shell: gelatin, Titanium dioxide, Dyes (Sunset yellow, kvinolin yellow).

10 PC. – blisters (2) – packs cardboard.

DESCRIPTION OF ACTIVE SUBSTANCES

Pharmacological action

Opioid analgesic, cyclohexanol derivative. Neselektivnыy mu agonist, delta- and kappa receptors in the CNS. Is a racemic mixture (+) and (-) isomers (by 50%), who in various ways are involved in obezbolivaûŝem effects. Isomer(+) is a pure opioid receptor agonist, has low tropism and does not have the pronounced selectivity towards different subtypes of receptors. Isomer(-), oppressing neironalny hostage norarenalina, activates the descending noradrenergic effects. Thanks to this broken transmission of pain impulses in the gelatinous substance of spinal cord.

Causes sedation. In therapeutic doses does not practically oppressing breathing. Provides protivokashlevoe action.

Pharmacokinetics

Once inside quickly and almost completely absorbed from the gastrointestinal tract (about 90%). C_max plasma achieved through 2 hours after ingestion. Bioavailability of the one-time admission is 68% and increases when multiple application.

Plasma protein binding – 20%. Tramadol is widely distributed in the tissues. V_d Once inside, and on/in the introduction is 306 and l 203 l, respectively. Penetrates through the placental barrier in concentration, equal to the concentration of the active substance in plasma. 0.1% excreted in breast milk.

Metabolised by demethylation and conjugation to 11 metabolites, of which only 1 It is active.

Report the news – 90% and through the intestine – 10%.

Testimony

Moderate and strong pain syndrome different Genesis (incl. in malignant tumors, acute myocardial infarction, neuralgia, injuries). Carrying out painful diagnostic or therapeutic procedures.

Dosage regimen

Adults and children over 14 years dose administered – 50 mg, rectally – 100 mg, in/in slowly or/m – 50-100 mg. When injecting efficiency is insufficient, then after 20-30 min possible ingestion dose 50 mg.

Children aged 1 to 14 years dose set based 1-2 mg / kg.

The duration of treatment is determined individually.

The maximum dose: adults and children over 14 regardless of the method of introduction – 400 mg / day.

Side effect

CNS: dizziness, weakness, drowsiness, confusion; in some cases – convulsions cerebral Genesis (the on/in the introduction or in high doses, while appointing Neuroleptics).

Cardio-vascular system: tachycardia, orthostatic hypotension, collapse.

From the digestive system: dry mouth, nausea, vomiting.

Metabolism: increased sweating.

On the part of the musculoskeletal system: mioz.

Contraindications

Acute intoxication with alcohol and drugs, have a depressing effect on the central nervous system, Children up to age 1 year, hypersensitivity to tramadolu.

Pregnancy and lactation

If pregnancy should avoid prolonged use of tramadol because of risk of fetal habituation and the emergence of the syndrome in the neonatal period.

If necessary, the use of lactation (breast-feeding) must be considered, What is tramadol a small number out of breast milk.

Cautions

The caution should be applied to convulsions Central origin, drug dependence, twisted minds, in patients with the human kidney and liver, as well as in case of hypersensitivity to other opioid receptor agonist.

Tramadol should not be applied for any longer time period, justified with a therapeutic perspective. In the event of prolonged treatment not to exclude the possibility of drug dependence.

Not recommended for the treatment of the syndrome of drugs.

You should avoid combination with MAO inhibitors.

During treatment, avoid alcohol.

Tramadol in the form of dosage forms prolonged action should not be used in children under the age of 14 years.

Effects on ability to drive vehicles and management mechanisms

During the period of tramadol is not recommended to engage in activities, require attention, high speed psychomotor reactions.

Drug Interactions

In an application with drugs, have a depressing effect on the central nervous system, with ethanol may increase the oppressive influence on the central nervous system.

Together with the use of MAO inhibitors, there is a risk of developing serotonin syndrome.

Together with the use of serotonin reuptake inhibitors, tricyclic antidepressants, antipsychotic drug, by other means, lowering the seizure threshold, increases the risk of seizures.

Together with the use of amplified antikoagulyannetary effect of warfarin and fenprokumona.

Together with the use of carbamazepine decreases the concentration of tramadol in plasma and its analgesic effect.

Together with the use of paroxetine describes cases of serotonin syndrome, seizures.

Together with the application sertralinom, Fluoxetine are the cases of serotonin syndrome development.

In an application is likely reduce the analgesic effect of opioid analgesics. Long-term use of opioids or barbiturates stimulate the development of cross-tolerance.

Naloxone activates breath, eliminating analgesia after administration of opioid analgesics.