Universal reference book for medicines
Product name: PALEXIA (PALEXIA)

Active substance: tapentadol

Type: Opioid analgesic with mixed mechanism of action.
The drug of prolonged action
Manufacturer: GRUNENTHAL (Germany) manufactured by FARMACEUTICI FORMENTI (Italy)
Composition, form of production and packaging
Long-acting tablets covered with a film shell of
white color, oblong, on one side the engraving is the Grünenthal logo, on the other side is the engraving "H1".

1 tab.

tapentadol hydrochloride 58.24 mg,

which corresponds to the content of tapentadol 50 mg

Auxiliary substances: hypromellose 100000 mPa? S - 100 mg, microcrystalline silicified cellulose (98% microcrystalline cellulose, 2% silicon colloidal dioxide) - 363.76 mg, magnesium stearate - 3 mg.

The composition of the film shell: Opaprai II white 33G28488 - 15 mg, including hypromellose 6 mPa? S - 6.164 mg, lactose monohydrate - 3.185 mg, talc - 2.055 mg, macrogol 6000 - 1.541 mg, propylene glycol 0.514 mg, titanium dioxide - 1.541 mg.

10 pieces.
- packings cellular planimetric (2) - packs cardboard.
10 pieces.
- packings cellular planimetric (6) - packs cardboard.
The tablets of prolonged action, covered with a film shell of pale yellow color, oblong, on one side the engraving - the Grünenthal logo, on the other side the engraving "H2".

1 tab.

tapentadol hydrochloride 116.48 mg,

which corresponds to the content of tapentadol 100 mg

Auxiliary substances: hypromellose 100000 mPa s - 100 mg, microcrystalline silicified cellulose (98% cellulose microcrystalline, 2% silicon colloidal dioxide) - 305.52 mg, magnesium stearate - 3 mg.

Composition of the film coat: Opadrai II yellow 33G32826 - 15 mg, including hypromellose 6 mPa? S - 6.164 mg, lactose monohydrate 3.185 mg, talc 2.055 mg, macrogol 6000 1.541 mg, propylene glycol 0.514 mg, titanium dioxide - 1.461 mg, iron oxide yellow - 0.08 mg.

10 pieces.
- packings cellular planimetric (2) - packs cardboard.
10 pieces.
- packings cellular planimetric (6) - packs cardboard.
The tablets of prolonged action, covered with a film membrane of pale pink color, oblong, on one side the engraving - the Grünenthal logo, on the other side the engraving "H3".

1 tab.

tapentadol hydrochloride 174.72 mg,

which corresponds to the content of tapentadol 150 mg

Auxiliary substances: hypromellose 100000 mPa s - 100 mg, cellulose microcrystalline silicified (98% cellulose microcrystalline, 2% silicon dioxide colloid) - 247.28 mg, magnesium stearate - 3 mg.

The composition of the film coat: Opaprai II pink 33G34210 - 15 mg, including hypromellose 6 mPa? S - 6.164 mg, lactose monohydrate - 3.185 mg, talc - 2.055 mg, macrogol 6000 - 1.541 mg, propylene glycol 0.514 mg, titanium dioxide - 1.52 mg, iron oxide yellow - 0.008 mg, iron oxide red - 0.014 mg.

10 pieces.
- packings cellular planimetric (2) - packs cardboard.
10 pieces.
- packings cellular planimetric (6) - packs cardboard.
Tablets of prolonged action, covered with a film shell of pale orange color, oblong, on one side engraving - the Grünenthal logo, on the other side the engraving "H4".

1 tab.

tapentadol hydrochloride 232.96 mg,

which corresponds to the content of tapentadol 200 mg

Auxiliary substances: hypromellose 100000 mPa? S - 100 mg, microcrystalline silicified cellulose (98% cellulose microcrystalline, 2% silicon colloidal dioxide) - 363.04 mg, magnesium stearate - 4 mg.

The composition of the film shell: Opaprai II orange 33G23931 - 15 mg, including hypromellose 6 mPa? S - 6.164 mg, lactose monohydrate - 3.185 mg, talc - 2.055 mg, macrogol 6000 - 1.541 mg, propylene glycol 0.514 mg, titanium dioxide - 1.156 mg, iron oxide yellow - 0.362 mg, iron oxide red - 0.024 mg.

10 pieces.
- packings cellular planimetric (2) - packs cardboard.
10 pieces.
- packings cellular planimetric (6) - packs cardboard.
Long-acting tablets covered with a film coating of brownish-red color, oblong, on one side engraving - the Grünenthal logo, on the other side the engraving "H5";
on the cross section, the core is white or almost white in color and the film shell.
1 tab.

tapentadol hydrochloride 232.96 mg,

which corresponds to the content of tapentadol 250 mg

Auxiliary substances: hypromellose 100000 mPa s - 100 mg, microcrystalline silicified cellulose (98% cellulose microcrystalline, 2% silicon colloidal dioxide) - 304.8 mg, magnesium stearate - 4 mg.

The composition of the film shell: Opaprai II orange 33G35200 - 15 mg, including hypromellose 6 mPa? S - 6.164 mg, lactose monohydrate - 3.185 mg, talc - 2.055 mg, macrogol 6000 - 1.541 mg, propylene glycol 0.514 mg, titanium dioxide - 1.114 mg, iron oxide yellow - 0.001 mg, iron oxide red - 0.386 mg, iron oxide black - 0.041 mg.

10 pieces.
- packings cellular planimetric (2) - packs cardboard.
10 pieces.
- packings cellular planimetric (6) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2015.

PHARMACHOLOGIC EFFECT

Tapentadol is a potent analgesic that is an agonist of mu-opioid receptors and an inhibitor of norepinephrine reuptake.
Tapentadol directly has an analgesic effect without the involvement of pharmacologically active metabolites.
Tapentadol has been shown to be effective in the pain of nociceptive, neuropathic, visceral genesis and pain caused by the inflammatory process.
In the course of clinical studies of the drug with pain in the back, okologicheskih and neonkologicheskih pain was confirmed the analgesic effectiveness of tapentadol. Effects on the cardiovascular system: with a careful study of the QT interval, no effect from taking therapeutic and exceeding the therapeutic doses of tapentadol with respect to the QT interval has been established. Tapentadol had no significant effects on other ECG parameters (heart rate, PR interval, QRS complex, T and U tooth morphology).
PHARMACOKINETICS

Suction

The average absolute bioavailability of tapentadol after ingestion of a single dose on an empty stomach in sustained-release tablets coated with a film coat is approximately 32% due to intensive pre-systemic metabolism.
Maximum concentrations of tapentadol in the blood plasma are observed between 3 and 6 hours after ingestion of long-acting tablets coated with a film coat. Proportional to the dose of AUC (the area under the concentration-time curve, the most significant parameter for long-acting dosage forms) was noted after taking long-acting tablets within the therapeutic range of doses.
The long-term administration of tapentadol twice daily at doses of 86 mg and 172 mg in prolonged-release tablets showed that the accumulation factor is approximately 1.5, which was mainly determined by the dosing interval and the half-life of tapentadol.
The equilibrium concentration of tapentadol in the blood plasma is reached on the second day after the start of taking oral tablets of prolonged action, coated with a film membrane.
Effect of food

AUC and C max of tapentadol increased by 8% and 18%, respectively, with long-acting tablets taken after taking fatty high-calorie food.
The time to reach C max isdelayed by 1.5 hours with high-calorie food. This was considered clinically insignificant. The drug Palexia can be taken orally both before and after meals.
Distribution

Tapentadol has a large volume of distribution.
After intravenous administration of tapentadol, the volume of distribution in the terminal elimination phase (Vd) is 540 ± 98 liters. Binding to plasma proteins is low and does not exceed 20%.
Metabolism

Tapentadol undergoes a pronounced metabolism.
About 97% of the compound is metabolized. The main way of metabolism of tapentadol is conjugation with glucuronic acid. After oral administration, approximately 70% of the dose is excreted into the urine in the form of conjugated forms (55% glucuronide and 15% tapentadol sulfate). Uridine diphosphate glucuronyltransferase (CGT) is the main enzyme involved in the glucuronation process (mainly isoenzymes UGT1A6, UGT1A9 and UGT2B7). A total of 3% of tapentadol is excreted into the urine unchanged. Tapentadol is also metabolized to N-desmethyltapentadol (13%) by the action of the CYP2C9 and CYP2C19 isoenzymes and to hydroxy-tentadol (2%) under the action of the CYP2D6 isoenzyme, which are further subjected to conjugation. For this reason, the metabolism of tapentadol mediated through the cytochrome P450 isoenzyme system is less important than glucuronidation.
None of the metabolites of tapentadol has an analgesic effect.

Excretion

Tapentadol and its metabolites are excreted almost completely (99%) by the kidneys.
The total clearance after intravenous administration is 1530 ± 177 ml / min. The final half-life after taking tapentadol inside long-acting tablets coated with a film coating, averagely 5-6 hours.
Special categories of patients

Elderly patients

AUC of tapentadol is similar in the elderly (65-78 years) and in middle-aged patients (19-43 years), while in elderly patients the average C max is 16% lower than in middle-aged patients.

Impaired renal function

AUC and C max of tapentadol are comparable in patients with varying degrees of functional kidney activity (from normal to severe disability).
Conversely, with an increase in the severity of renal failure, there was an increase in the area under the concentration-time curve (AUC) of tapentadol-O-glucuronide. In patients with mild, moderate and severe renal dysfunction, an increase in the AUC of tapentadol-O-glucuronide was observed at 1.5, 2.5, and 5.5 times compared with patients with normal renal function, respectively.
Impaired liver function

In patients with impaired hepatic function, the intake of tapentadol by mouth was characterized by a higher AUC and serum concentration compared to patients with normal liver function.
The ratios of pharmacokinetic indexes of tapentadol for groups of patients with mild and moderate hepatic insufficiency, when compared with the group of patients with normal liver function, were 1.7 and 4.2, respectively, for AUC; 1.4 and 2.5, respectively, for C max ; and 1,2 and 1,4 respectively for the half-life. The rate of formation of tapentadol-O-glucuronide in patients with more severe impairment of liver function is lower.
Pharmacokinetic interactions

Tapentadol is mainly metabolized by 2-phase (glucuronidation), and only a small amount is metabolized through the oxidation processes of the 1 phase.
Since glucuronidation is a high-potency system with low affinity, any clinically meaningful interaction associated with glucuronation is unlikely. This is confirmed by the experience of simultaneous application of tapentadol with naproxen and probenecid, the growth of Tupentadol AUC was 17% and 57%, respectively. With simultaneous use with paracetamol and acetylsalicylic acid, no changes in the pharmacokinetic index of tapentadol were observed.
When studying the possible effects of metoclopramide and omeprazole on the absorption of tapentadol, there was no clinically significant effect on the concentration of tapentadol in blood plasma.

TAPENTADOL is not an inducer or inhibitor of cytochrome P450 isoenzymes.
Therefore, clinically significant interactions mediated through the cytochrome P450 isoenzyme system are unlikely.
The binding of tapentadol to plasma proteins is low (approximately 20%).
For this reason, the probability of pharmacokinetic interactions due to substitution from the connection with plasma proteins is small.
INDICATIONS

- chronic pain syndrome of medium and high severity.
The drug is used only for pain syndrome of medium and high intensity, requiring the appointment of opioid analgesics.
DOSING MODE

As with other analgesics with a central mechanism of action, the dose of the drug should be selected individually in accordance with the severity of the pain syndrome, previously conducted therapy and the possibility of monitoring the patient.
The drug Palexia in prolonged-action tablets coated with a film coat, should be taken twice a day, approximately every 12 hours, regardless of food intake. The tablet should be taken with a sufficient amount of liquid, without chewing, not breaking and not dissolving.
Start treatment

a) patients who do not take narcotic analgesics:

You should start therapy with a dose of 50 mg of tapentadol twice a day.

b) patients taking narcotic analgesics:

When switching from other narcotic analgesics to the preparation of Palexia and choosing the initial dose, one should take into account the characteristics of the previously prescribed drug, the frequency of its administration and the average daily dose.

Dose selection and maintenance therapy

After the beginning of treatment, under the careful supervision of the doctor, the dose should be selected individually before adequate anesthesia is achieved with a minimum of side effects.
Experience shows that the dose selection regime with an increase of 50 mg of tapentadol twice a day every 3 days in most patients is sufficient to achieve adequate pain control.
A daily dose of tapentadol in excess of 500 mg in prolonged-action tablets coated with a film coat was not prescribed, therefore, in such doses, the drug should not be used.

End of treatment

With the simultaneous discontinuation of taking tapentadol, the syndrome of "cancellation" is possible.
It is recommended to gradually reduce the dose of the drug before complete cancellation in order to prevent the development of the "withdrawal" syndrome.
Adults with chronic diseases

Impaired renal function

Dose adjustments in patients with mild or moderate renal failure are not required.
The experience of application in patients with severe renal dysfunction is not, therefore, the use of the drug in this group of patients is contraindicated.
Impaired liver function

Dose adjustment in patients with mild hepatic insufficiency is not required.
Care must be taken when administering Palexia to patients with moderate hepatic impairment. Treatment of such patients should start with 50 mg of tapentadol in prolonged-action tablets coated with a film coat, not more often than once a day.Further therapy should be aimed at maintaining the analgesic effect with an acceptable level of tolerance. Experience in patients with severe impairment of liver function is not, therefore, the use in this group of patients is contraindicated.
Elderly patients (65 years and over)

In general, the recommended doses for elderly patients with normal liver and kidney function are the same as for middle-aged patients with normal kidney and liver function.
Because elderly patients are more likely to have decreased kidney and liver function, care should be taken when choosing a dose and not exceeding recommended.
Use in children

The drug Palexia is contraindicated for use in patients under the age of 18 due to insufficient data on efficacy and safety.

SIDE EFFECT

Approximately 60% of patients taking the drug Palexia in prolonged-action tablets coated with a film coat, side effects, mainly of mild or moderate intensity, were observed.
The most frequent of these were disorders of the gastrointestinal tract and central nervous system (nausea, dizziness, constipation, headache and drowsiness).
The table below shows the side effects of the drug Palexia, identified during its use.
They are represented by classes and frequency: very frequent (? 1/10); frequent (? 1/100, <1/10); infrequent (? 1/1 000, <1/100); rare (? 1/10 000, <1/1 000); very rare (<1/10 000).
System-Organ Classes Very Frequent (? 1/10) Frequent (from? 1/100 to <1/10) Infrequent (from? 1/1 000, to <1/100);
Rare (from? 1/10 000, to <1/1 000)
Disturbances from the immune system Hypersensitivity to the drug (including angioedema)

Disorders from the metabolism and nutrition Decreased appetite Decreased body weight

Disorders of the psyche Sleep disturbances, anxiety, depressed mood, increased excitability, anxiety Unusual dreams, impaired perception, disorientation in place and in time, psychomotor agitation, confusion, euphoria Drug dependence, pathological thinking

Disturbances of the nervous system Dizziness, headache, drowsiness Involuntary muscle contractions, tremor, attention disorders Paresthesia, hypoesthesia, imbalance, sedation, syncope, memory impairment, cognitive impairment, depression, dysarthria Coordination disorders, pre-syncope, convulsions

Impaired vision

Violations from the heart and blood vessels "Tides" Increase in heart rate, decreased heart rate, palpitations, decreased blood pressure

Disturbances from the respiratory system, chest and mediastinal organs Shortness of breath Respiratory depression

Disturbances from the gastrointestinal tract Nausea, constipation Vomiting, diarrhea, dyspepsia Discomfort in the abdomen Disruption of evacuation of stomach contents

Disturbances from the skin and subcutaneous tissues. Itching, hyperhidrosis, rash. Hives

Disorders from the kidneys and urinary tract Pollakuria, difficulty urinating

Disorders from the reproductive system and breast cancer Sexual dysfunction

General disorders and disorders at the injection site Fatigue, dryness of the mucous membrane (mouth, eyes and throat), asthenia, sensation of changes in body temperature, swelling Syndrome of "withdrawal", irritability, unusual sensations Feeling of intoxication, feeling of relaxation

When taking the drug Palexia inside the tablets of prolonged action, covered with a film coat, duration of up to 1 year, there are cases of mild "withdrawal" syndrome with sudden interruption of therapy, in severity they were classified as lungs.
However, doctors should take into account the possibility of the occurrence of the "withdrawal" syndrome and provide the necessary treatment in case of its occurrence.
The risk of suicidal thoughts higher in patients suffering from chronic pain. In addition, drugs with a pronounced effect on the mono-nergicheskuyu system increase the risk of suicidal behavior in patients suffering from depression, especially early in treatment. Clinical studies and post-marketing experience with tapentadola found no evidence of increased risk. If you experience these side effects in the instructions, or seen the other side effects not mentioned in the instructions, tell your doctor.
CONTRAINDICATIONS

- tapentadolu or hypersensitivity to any of the excipients included in the formulation;
- in situations where drugs are contraindicated agonists of mu-opioid receptors, ie, in patients with significant respiratory depression (if you can not observe or the absence of resuscitative equipment), as well as in patients with acute exacerbation, or severe bronchial asthma or hypercapnia;
- the presence or suspected paralytic ileus;
- acute intoxication with alcohol, hypnotic drugs, centrally acting analgesics and psychotropic drugs;
- in patients receiving monoamine oxidase inhibitors (MAOIs), or taking them in the last 14 days;
- severe renal insufficiency;

- severe hepatic impairment;
- the age of 18;
- Lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

Carefully

Paleksiya drug should be used with caution:
- with an increased risk of misuse or abuse of the drug;
- in violation of the respiratory function;
- in patients with traumatic brain injury and depression of consciousness;
- in patients with convulsive disorders or a history of any conditions that increase the risk of seizures;
- in patients with hepatic insufficiency of moderate severity;
- in patients with biliary tract disorders, and acute pancreatitis;
- in patients with low blood pressure.
It recommended a gradual reduction in the dose of the drug Paleksiya before complete abolition. Care should be taken while applying Paleksiya drug with serotonergic medications.
PREGNANCY AND LACTATION

Pregnancy

Data on the use tapentadola during pregnancy is limited. In animal studies, teratogenic effects associated with tapentadolom not found. However, at doses higher than the upper limit of therapeutic, revealed embryonic retardation and embryotoxicity (CNS effects associated with agonism in mu-opioid receptor). It has been revealed effects on postnatal development of offspring in the appointment tapentadola at doses that do not cause adverse effects in pregnant females.
Use of the drug during pregnancy Paleksiya is permissible only if the potential benefit to the mother outweighs the potential risk to the fetus.
birth
The impact of the application of tapentadola not known at the time of delivery. Apply tapentadol during childbirth and immediately before birth is not recommended.Due tapentadola affinity for mu-opioid receptors, newborns whose mothers took tapentadol should be monitored closely due to the possibility of respiratory depression.
Lactation

Information on tapentadola excretion in breast milk is limited. Physico-chemical and pharmacodynamic / toxicological data on tapentadolu point to excretion in breast milk, so the risk of exposure to the breast-fed child can not be excluded. Paleksiya The drug should not be administered during breast-feeding.
APPLICATION FOR FUNCTIONS OF THE LIVER

Dose adjustment for patients with mild or moderate renal impairment is required. Experience with patients with severe, so there is no use of kidney function in the group of the drug contraindicated patients.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Dose adjustment in patients with mild hepatic impairment is not required. Care should be taken when appointing Paleksiya drug to patients with moderate hepatic insufficiency. Treatment of such patients should be started with 50 mg tapentadola tablets prolonged action, film-coated, not more than once per day. Further treatment should be aimed at maintaining analgesia with acceptable tolerability. Experience with patients with severe, so there is no use of liver function in the group contraindicated patients.
APPLICATION FOR CHILDREN

Paleksiya drug is contraindicated for use in patients under the age of 18 years due to lack of efficacy and safety data.
APPLICATION IN ELDERLY PATIENTS

In general, the recommended dose for elderly patients with normal liver function and kidney are the same as for the middle-aged patients with normal renal function and liver. Since elderly patients are more likely to decline in kidney function and liver, caution should be exercised in the selection and dose not exceed recommended.
SPECIAL INSTRUCTIONS

Possible abuse of medication
There is a potential risk of abuse of the drug Paleksiya. This should be considered when administering the drug in situations where there is danger of improper use, abuse of the drug or the drug transmission to others.
All patients treated with drugs - agonists of the mu-opioid receptor, are subject to rigorous control in relation to drug abuse and dependence.
respiratory depression
In high doses and in patients with increased sensitivity to agonists of mu-opioid receptor tapentadol can induce dose-dependent respiratory depression. For this reason, patients with impaired respiratory function Paleksiya drug should be administered with caution. Should consider the possibility of using analgesics, non-agonist of mu-opioid receptors, and the drug Paleksiya in these patients should only be used under close medical supervision and in the lowest effective doses. When respiratory depression must be treated as in the case of respiratory depression against application of any other agonist of the mu-opioid receptors.
Traumatic brain injury and increased intracranial pressure
As with other drugs - agonists of mu-opioid receptor, tapentadol should not be administered to patients who may be especially sensitive to the pathophysiological reactions, developing with increasing partial pressure of carbon dioxide in the intracranial vessels and brain tissue, for example, increased intracranial pressure, inhibition of of consciousness or coma. Analgesics, characterized by an affinity for the mu-opioid receptor may mask clinical manifestations of traumatic brain injury. Paleksiya drug should be used with caution in patients with traumatic brain injury and brain tumors.
convulsions
Tapentadola systematic study in patients with convulsive disorders have been conducted. Nevertheless, like other analgesics with affinity for the mu-opioid receptor Paleksiya drug must be administered with caution to patients with history of convulsive disorders, or any conditions which expose patients to the risk of seizures.
Liver failure

Patients with mild to moderate hepatic impairment identified respectively 2-fold and 4.5-fold increase in systemic exposure compared to patients with normal liver function. Paleksiya drug should be used with caution in patients with moderate hepatic insufficiency. Paleksiya drug in patients with severe hepatic dysfunction has not been studied and therefore contraindicated in these patients.
Application in the pathology of the pancreas and bile ducts
Formulations having an affinity for the mu-opioid receptor, can cause spasm of the sphincter of Oddi. Paleksiya drug should be used with caution in patients with biliary tract disorders, and acute pancreatitis.
"Cancellation" syndrome
When you single-step termination receiving tapentadola may develop the syndrome of "cancellation". You may experience the following symptoms: anxiety, sweating, insomnia, chills, pain, nausea, tremors, diarrhea, upper respiratory tract symptoms, piloerection, and rarely, hallucinations. It recommended a gradual reduction in dose to the complete abolition of the purposes of the prevention of "cancellation" syndrome.
Blood Pressure Reducing
drug Paleksiya may cause a significant decrease in blood pressure particularly in patients with hypovolemia or simultaneously with tapentadolom receiving drugs that reduce peripheral vascular tone (e.g., phenothiazine derivatives, agents for anesthesia).
serotonin syndrome
There are reports of life-threatening serotonin syndrome with concomitant use tapentadola even at therapeutic doses with serotonergic drugs: selective serotonin reuptake inhibitors (SSRIs), serotonin reuptake inhibitors and norepinephrine, tricyclic antidepressants, triptans, drugs affecting the serotonergic transmission in the central nervous system (e.g. mirtazapine, trazodone and tramadol), and formulations disruptor serotonin metabolism (e.g., ingibi proof operation MAO). Possible symptoms of serotonin syndrome may be, for example, confusion, agitation, coma, tachycardia, fever, incoordination, nausea, vomiting and diarrhea.
Tapentadol should be used with caution in patients with adrenocortical insufficiency (eg Addison's disease), patients with delirium tremens, toxic psychosis in patients with myxedema and hypothyroidism, as well as hypertrophy of the prostate and urethral strictures.
Effects on ability to drive vehicles, machinery
As with other drugs - agonists of the mu-opioid receptor, Paleksiya may adversely affect the ability to road management and complex mechanisms, as It affects the central nervous system. Very often such action possible at the beginning of treatment, at any change in dose, while taking tranquilizers or alcohol. Patients should refrain from driving and classes of potentially hazardous activities.
OVERDOSE

Data on overdose is very limited.
Symptoms can be expected inherent in all preparations having central analgesic activity and characterized by an affinity for the mu-opioid receptor symptoms - cramps, vomiting, collapse, depression of consciousness until coma, convulsions and respiratory depression, with its stop.
Urgent care:treatment of an overdose should be focused on eliminating symptoms stimulation of mu-opioid receptors. In case of suspected overdose tapentadola emphasis should be given to recovery of the airway and application managed or controlled ventilation. Full opioid receptor antagonists, such as naloxone, are specific antidotes against respiratory depression associated with an overdose of the narcotic analgesics. Respiratory depression after an overdose may exceed the duration of the opioid receptor antagonist. Appointment of an opioid receptor antagonist does not replace the continuous monitoring of airway status, monitoring violations of breathing and blood circulation, which developed as a result of an overdose of narcotic analgesics.If the response to the administration of antagonists or insufficient short-opioid receptor may further administering an opioid receptor antagonist.
Purification of the gastrointestinal tract can be carried out in order to remove not absorb tapentadola. The use of activated charcoal or gastric lavage may be performed within 2 hours after ingestion. Before cleaning the digestive tract need to protect the respiratory tract.
DRUG INTERACTION

Concomitant use of tapentadola with benzodiazepines, barbiturates and opioids (analgesics, antitussives and for the treatment of the syndrome of "cancellation") may increase the risk of respiratory depression. Drugs that suppress the activity of the CNS (benzodiazepines, neuroleptics, blockers of H 1 histamine receptors, opioids, alcohol), may enhance tapentadola sedation and central nervous system depression. If the combination tapentadola and preparations causing respiratory depression and central nervous system, it is necessary to determine whether or dose reduction.
Agonists, opioid receptor antagonists.Caution must be exercised while the use tapentadola agonist-antagonists, mu-opioid receptor (e.g., pentazocine, nalbuphine) or partial agonists at the mu-opioid receptor antagonists (e.g., buprenorphine). While the use of buprenorphine has been noted the need to increase doses of agonists of mu-opioid receptor, and in these circumstances requires careful monitoring of side effects such as respiratory depression.
There are few reports of development of serotonin syndrome, coincides in time with simultaneous application tapentadola and serotonergic drugs such as selective serotonin reuptake inhibitors (SSRIs). Possible symptoms of serotonin syndrome may be, for example, confusion, agitation, a rise in body temperature, sweating, ataxia, hyperreflexia, myoclonus and diarrhea. Cancel serotonergic drugs typically resulted in a rapid disappearance of symptoms. Treatment depends on the nature and severity of symptoms.
Since the main route of metabolism is tapentadola conjugation with glucuronic acid isoenzymes involving UGT1A6, UGT1A9 and UGT2B7, simultaneous application of potent inhibitors of these isoenzymes (such as ketoconazole, fluconazole, meclofenamic acid) can increase the systemic exposure tapentadola.
Patients under treatment tapentadolom, caution should be exercised at the beginning and at the end of the simultaneous use of powerful enzymatic inducers liver systems (e.g., rifampin, phenobarbital, Hypericum preparations), as this may lead respectively to decreased efficiency or risk of side effects.
Tapentadol is contraindicated in patients receiving MAO inhibitors or takes them past 14 days, as possibly elevated levels of norepinephrine, which can cause side effects to the cardiovascular system, such as a hypertensive crisis.
TERMS OF RELEASE FROM PHARMACY

Let go on prescription.

TERMS AND CONDITIONS OF STORAGE

At a temperature of not higher than 30 ° C. Keep out of reach
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