Tramadol STADA - instructions for use, dose, side effects, contraindications

contents of the capsule: calcium hydrophosphate dihydrate - 97.0 mg, magnesium stearate - 5.5 mg, colloidal anhydrous silicon (silicon dioxide colloidal anhydrous) - 2.5 mg;

capsule shell: gelatin 39.2 mg, titanium dioxide (E 171) 0.8 mg.

Description:Hard gelatinous opaque white capsules with a size of 4. The contents of the capsule are a white powder.

Pharmacotherapeutic group:An analgesic with a mixed mechanism of action.

ATX: & nbsp

N.02.A.X.02 Tramadol

Pharmacodynamics:

Opioid synthetic analgesic, which has a central effect and action on the spinal cord (contributes to the discovery of potassium and calcium channels, causes hyperpolarization of membranes and inhibits pain impulses), enhances the action of sedatives. Activates opioid receptors (mu, delta, kappa) on the pre- and postsynaptic membranes of the afferent fibers of the nociceptive system in the brain and gastrointestinal tract. Slows down the destruction of catecholamines, stabilizes their concentration in the central nervous system.

It is a racemic mixture of 2 enantiomers - dextrorotatory (+) and levorotatory (-), each of which exhibits a different receptor affinity:

(+)Tramadol is a selective agonist of mu-opioid receptors, and selectively inhibits reverse neuronal seizure of serotonin;

(-)Tramadol inhibits the reverse neuronal seizure of norepinephrine. Mono-O-desmethyltramadol (Ml metabolite) also selectively stimulates mu-opioid receptors. The affinity of tramadol for opioid receptors is ten times weaker than that of codeine, and 6000 times weaker than morphine. Expression of analgesic action is 5-10 times weaker than morphine.

The analgesic effect is due to a decrease in nociceptive activity and an increase in the antinociceptive systems of the body.

In therapeutic doses, it does not significantly affect haemodynamics and breathing, does not change the pressure in the pulmonary artery, slightly slows down the intestinal motility without causing constipation. Has some antitussive and sedative effect. Oppresses the respiratory center, excites the start zone of the vomiting center, the nucleus of the oculomotor nerve.

With prolonged use, the development of tolerance is possible. Analgesic effect develops 15-30 minutes after ingestion and lasts up to 6 hours.

Pharmacokinetics:

Absorption - 90%; bioavailability - 68% when taken orally (increases with repeated use). Time to reach a maximum concentration of 2 hours.Penetrates through the blood-brain barrier and the placenta, 0.1% excreted in breast milk. In the liver, it is metabolized by N- and O-demethylation followed by conjugation with glucuronic acid. 11 metabolites have been identified, of which mono-O-desmethyltramadol (Ml) has pharmacological activity. The half-life in the second phase is -6h (tramadol), 7.9 hours (mono-O-desmethyltramadol); in patients older than 75 years - 7.4 h (tramadol); with cirrhosis of the liver - 13.3 ± 4.9 h (tramadol), 18.5 ± 9.4 h (mono-O-desmethyltramadol), in severe cases - 22.3 h and 36 h, respectively; with chronic renal failure (creatinine clearance less than 5 ml / min) - 11 ± 3.2 h (tramadol), 16.9 ± 3 h (mono-O-desmethyltramadol), in severe cases - 19.5 h and 43.2 h respectively.

It is excreted by the kidneys (25-35% unchanged), the average cumulative index of renal excretion is 94%.

Indications:Moderate and strong pain syndrome of various etiology (postoperative period, trauma, pain in cancer patients, with diagnostic and therapeutic manipulations).

Contraindications:Hypersensitivity to the components of the drug and other opioids; conditions accompanied by respiratory depression or severe depression of the central nervous system (intoxication with alcohol, hypnotic drugs, opioid analgesics,psychotropic drugs); simultaneous use of monoamine oxidase inhibitors (and two weeks after their withdrawal); severe hepatic and / or renal insufficiency (creatinine clearance less than 10 ml / min); pharmacovirus-resistant epilepsy; use of tramadol as a drug for the treatment of the syndrome of "withdrawal" of drugs; propensity to suicide, substance abuse; pregnancy, the period of breastfeeding; children's age (up to 14 years).

Carefully:With caution and under the supervision of a doctor, the drug should be used in patients with impaired renal and hepatic function, with craniocerebral trauma, with disorders of consciousness of various genesis, convulsions, intracranial hypertension, epilepsy, persons with drug dependence (especially narcotic and alcohol), in patients against a background of abdominal pain of an unknown genesis ("acute" abdomen), with renal failure (creatinine clearance from 10 to 30 ml / min). When used simultaneously with selective serotonin reuptake inhibitors (some antidepressants and drugs that reduce appetite), tricyclic antidepressants,other tricyclic compounds (for example, promethazine), antimigraine drugs (tryptans), opioid analgesics, neuroleptics and other drugs that reduce the threshold of convulsive readiness.

Pregnancy and lactation:

The safety of tramadol during pregnancy is not established. Avoid use because of the risk of developing addiction in the fetus and the occurrence of the syndrome of "cancellation" in the neonatal period.

If it is necessary to use during breastfeeding, consider stopping breastfeeding (the drug is excreted in breast milk).

Dosing and Administration:

Tramadol Stada® is used according to the doctor's prescription, the dosage regimen is selected individually depending on the severity of the pain syndrome and the patient's sensitivity. Duration of treatment is determined individually, do not prescribe the drug beyond the term justified from a therapeutic point of view. In the absence of other regulations Tramadol Stade® should be given in the following doses: For adults and children over 14 years of age, the usual initial dose is 1 capsule (50 mg) orally with a small amount of liquid, regardless of meal time.If there is no effect for 30-60 minutes, you can take another 1 capsule. With severe pain, a single dose can immediately be 100 mg (2 capsules). If necessary, the drug is prescribed repeatedly, but not earlier than 6-8 hours. The maximum daily dose is 400 mg (8 capsules).

In elderly patients (at the age of 65 to 75 years) due to the possibility of delayed excretion, the interval between injections of the drug can be increased in accordance with individual characteristics. Patients over the age of 75 are recommended to reduce the daily dose to 300 mg.

In patients with renal and hepatic insufficiency it is recommended to reduce the dose or increase the interval between doses of single doses. In patients with creatinine clearance less than 30 ml / min or 0.5 ml / s, a doubling of the interval between doses is recommended at the beginning of the treatment.

Tramadol Stada® should not be administered for longer than it is therapeutically necessary.

Side effects:

The most frequent side effects of the drug Tramadol Stada®, capsules are nausea and dizziness.

From the nervous system: increased sweating, dizziness,headache, weakness, fatigue, inhibition, anxiety, anorexia, paradoxical stimulation of the central nervous system (nervousness, agitation, anxiety, tremor, muscle spasms, euphoria, emotional lability, hallucinations), drowsiness, sleep disorders, confusion, coordination disorders , convulsions of the central genesis (with the simultaneous administration of antipsychotic drugs (antipsychotics)), depression, amnesia, cognitive impairment, paresthesia, unsteadiness of gait, violation of concentration, asthenia.

From the digestive system: dry mouth, nausea, vomiting, flatulence, indigestion, abdominal pain, constipation or diarrhea, difficulty in swallowing.

From the side of the cardiovascular system: manifestations of vasodilation - tachycardia, orthostatic hypotension, fainting, collapse, increased blood pressure, palpitation.

From the side of the musculoskeletal system, increase of muscle tone. Allergic reactions: urticaria, itching, exanthema, rash, including bullous, angioedema.

From the urinary system: difficulty urinating, dysuria, urinary retention.

From the sense organs: a violation of visual acuity, sometimes mydriasis, a violation of taste.

From the respiratory system: dyspnoea, pulmonary edema.

Other: weight loss, violation of the menstrual cycle. With prolonged use - drug dependence.

With a sharp cancellation - the syndrome of "withdrawal" (possible symptoms: panic attacks, anxiety, hallucinations, parasthesia, ringing in the ears, paradoxical symptoms from the central nervous system (depersonalization, derealization, paranoia)). In the case of a significant excess of the recommended dose or with the simultaneous use of other drugs that have an effect on the central nervous system, respiratory depression can be observed. Epileptiform seizures can mainly occur after application of high doses of tramadol or with simultaneous use of drugs that reduce the threshold of convulsive readiness.

Overdose:

Symptoms: mydriasis, miosis, vomiting, collapse, impaired consciousness (up to coma), cramps, respiratory center depression, apnea, lowering of blood pressure, tachycardia.

Treatment: ensuring airway patency, maintaining breathing and cardiovascular activity. Opiate-like effects can be stopped with naloxone, convulsions with benzodiazepine. Hemodialysis or hemofiltration is ineffective.

Interaction:

Strengthens the effect of drugs that depress the central nervous system, and ethanol Microsomal oxidation inductors (incl. carbamazepine, barbiturates) reduce the severity of the analgesic effect and the duration of the action. Long-term use of opioid analgesics or barbiturates stimulates the development of cross tolerance.

Anxiolytics increase the severity of the analgesic effect; The duration of anesthesia increases with combination with barbiturates.

Naloxone activates breathing, eliminating analgesia after the use of opioid analgesics.

Quinidine increases the plasma concentration of tramadol and decreases the metabolite Ml due to competitive inhibition of the CYP2D6 isoenzyme. Inhibitors of the CYP2D6 isoenzyme (such as fluoxetine, paroxetine and amitriptyline) reduce the metabolism of tramadol.Pre- or postoperative use of anti-vomiting medication ondansetron (an antagonist of 5-HTZ-serotonin receptors) increased the need for tramadol in patients with postoperative pain syndrome.

With the simultaneous use of tramadol and indirect anticoagulants - coumarin derivatives (eg, warfarin) - careful monitoring of patients is necessary, as some of them increase prothrombin time with the development of bleeding and subcutaneous hemorrhage.

Selective serotonin reuptake inhibitors (some antidepressants and drugs that reduce appetite), tricyclic antidepressants, other tricyclic compounds (for example, promethazine), antimigraine medicines (triptans), opioid analgesics, monoamine oxidase inhibitors, neuroleptics and other drugs that reduce the threshold of convulsive readiness, increase the risk of seizures.

Selective serotonin reuptake inhibitors, serotonin reuptake inhibitors and norepinephrine, tricyclic antidepressants, monoamine oxidase inhibitors,antimigraine drugs (triptans) and drugs that disrupt the metabolism of tramadol (inhibitors of isoenzymes CYP2D6 and CYP3A4), when combined with tramadol can cause serotonin syndrome. Symptoms of serotonin syndrome: confusion, agitation, hyperthermia, sweating, ataxia, hyperreflexia, myoclonus and diarrhea. The abolition of serotonergic drugs causes rapid relief of symptoms.

Special instructions:

Do not use for the treatment of the syndrome of "withdrawal" of opioids.

It should not be used simultaneously with the use of tramadol ethanol.

The drug should be avoided Tramadol Stada® patients with drug dependence (including dependence on opioids, alcohol).

The use of tramadol drugs increases the risk of suicide in patients with suicidal tendencies.

Effect on the ability to drive transp. cf. and fur:When using the drug Tramadol Stada®, capsules, it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Capsules 50 mg.

Packaging:10 capsules per blister of aluminum foil and polyvinyl chloride film. For 1, 2, 3 or 5 blisters together with instructions for medical use of the drug is placed in a cardboard box.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

The drug belongs to the list of 1 potent substances of the Standing Committee on Drug Control of the Ministry of Health and Social Development of the Russian Federation.

Shelf life:5 years. Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N015510 / 01

Date of registration:30.12.2010

Date of cancellation:2017-09-26

The owner of the registration certificate:SHTADA Artznajmittel AGSHTADA Artznajmittel AG Germany

Manufacturer: & nbsp

SHTADA Artznajmittel AG

Representation: & nbspNizhpharm, JSCNizhpharm, JSCRussia

Information update date: & nbsp26.09.2017

Illustrated instructions

Instructions

Tramadol STADA® (Tramadol Stada®)