Palexia - instructions for use, dose, side effects, contraindications

Active substanceTAPENTADOLTAPENTADOL

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Palexia

pills inwards

Grünenthal GmbH Germany

Palexia

pills inwards

Grünenthal GmbH Germany

Dosage form: & nbsp

Tablets of prolonged action, covered with a film membrane.

Composition:

Each tablet of prolonged action, film-coated, 50 mg contains:

Core tablet: active ingredient - tapentadol hydrochloride 58,24 mg in terms of tapentadol 50.00 mg.

Excipients: hypromellose 100,000 mPa-s 100.00 mg, cellulose microcrystalline silicate (98% cellulose microcrystalline, 2% silicon colloidal dioxide) 363.76 mg, magnesium stearate 3.00 mg;

White film shell (Opadrai® II white 33G28488) 15 mg. Ingredients: hypromellose 6 mPa with 6.164 mg, lactose monohydrate 3,185 mg, talc 2,055 mg, macrogol 6000 1.541 mg, propylene glycol 0.514 mg, titanium dioxide (E171) 1.541 mg.

Each tablet of prolonged action, film-coated, 100 mg contains:

Tablet core: active ingredient - tapentadol hydrochloride 116, .48 mg in terms of tapentadol 100.00 mg.

Excipients: hypromellose 100,000 mPa-s 100.00 mg, microcrystalline silicate cellulose (98% microcrystalline cellulose, 2% silicon colloidal dioxide) 305.52 mg, magnesium stearate 3.00 mg;

Yellow film membrane (Opadrai® II yellow 33G32826) 15 mg.Ingredients: hypromellose 6 mPa with 6.164 mg, lactose monohydrate 3.185 mg, talc 2.055 mg, macrogol 6000 1.541 mg, propylene glycol 0.514 mg, titanium dioxide (EI71) 1.461 mg, iron oxide yellow (13172) 0.080 mg.

Each tablet of prolonged action, film-coated, 150 mg contains:

Core tablet: active ingredient - tapentadol hydrochloride 174.72 mg in terms of tapentadol 150.00 mg.

Excipients: hypromellose 100,000 mPa-s 100.00 mg, cellulose microcrystalline silicate (98% cellulose microcrystalline, 2% silicon dioxide colloid) 247.28 mg, magnesium stearate 3.00 mg;

Pink film shell (Opadrai® II pink 33G34210) 15 mg. Composition: 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 (E171) 1.520 mg, iron oxide yellow (E172) 0.008 mg, iron oxide red (E172) 0.014 mg.

Each tablet of prolonged action, film-coated, 200 mg contains:

Tablet core: active ingredient - tapentadol hydrochloride 232.96 mg in terms of tapentadol 200.00 mg.

Excipients: hypromellose 100,000 mPa-s 100.00 mg, cellulose microcrystalline silicate (98% cellulose microcrystalline, 2% silicon colloidal dioxide) 363.04 mg, magnesium stearate 4.00 mg;

Orange film membrane (Opadrai® II orange 33G23931) 15 mg. Ingredients: 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 (E171) 1.156 mg, iron oxide yellow (E172) 0.362 mg, iron oxide red (E172 ) 0.024 mg.

Each tablet of prolonged action, film-coated, 250 mg contains:

Core tablet: active ingredient - tapentadol hydrochloride 291.20 mg in terms of tapentadol 250.00 mg.

Excipients: hypromellose 100,000 mPa-s 100.00 mg, cellulose microcrystalline silicate (98% cellulose microcrystalline, 2% silicon colloidal dioxide) 304.80 mg, magnesium stearate 4.00 mg;

Red film shell (Opadrai® II red 33G35200) 15 mg. Composition: 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 (E171) 1.114 mg, iron oxide yellow (E172) 0.001 mg, iron oxide red (E172) 0.386 mg, iron oxide black (E172) 0.041 mg.

Description:

The tablets of the prolonged action, covered with a film membrane, 50 mg. White oblong film-coated tablets, on one side of the engraving - the Grünenthal logo, on the other side of the engraving "H1".

Extended-release tablets, film-coated, 100 mg. Pale yellow oblong tablets covered with a film membrane, on one side the engraving is the Grünenthal logo, on the other side is the engraving "H2".

Extended-release tablets, film-coated, 150 mg. Pale pink oblong tablets covered with a film membrane, on one side the engraving is the Grünenthal logo, on the other side is the engraving "H3".

Extended-release tablets, film-coated, 200 mg. Pale orange oblong tablets covered with a film membrane, on one side the engraving is the Grünenthal logo, on the other side is the engraving "N4".

Extended-release tablets, film-coated, 250 mg. Brown-red oblong film-coated tablets, 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, covered with a very thin coat of white, pale yellow, pale pink, pale orange or brown-red for tablets of 50 mg, 100 mg, 150 mg, 200 mg and 250 mg respectively.

Pharmacotherapeutic group:Analgesic narcotic drug

ATX: & nbsp

N.02.A.X.06 TAPENTADOL

Pharmacodynamics:

Tapentadol is a potent analgesic that is an agonist of mu-opioid receptors and an inhibitor of norepinephrine reuptake. TAPENTADOL directly exerts an analgesic effect without the participation 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 for back pain, oncological and non-oncological pains, the analgesic effectiveness of tapentadol was confirmed.

Action on the cardiovascular system: with a careful study of the interval QT, no effects from taking therapeutic and exceeding therapeutic doses tapentadol with respect to the interval QT was not established. TAPENTADOL did not provide significant effects and other parameters of the ECG (heart rate, interval PR, complex QRS, morphology of the T wave and U).

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 membrane,is approximately 32% because of intensive pre-systemic metabolism.

Maximum concentrations of tapentadol in blood plasma are observed between 3 and 6 hours after ingestion of prolonged-action tablets coated with a film membrane.

Proportional dose growth AUC (the area under the concentration-time curve, the most significant parameter for long-acting dosage forms) was noted after long-acting tablets were taken within the therapeutic range of doses.

Long-term administration of tapentadol twice daily at doses of 86 mg and 172 mg in prolonged-release tablets showed that the accumulation coefficient is about 1.5, which was mainly determined by the dosage interval and the half-life of tapentadol. The equilibrium concentration of tapentadol in the blood plasma is reached on the second day after the beginning of the intake of long-acting tablets coated with a film membrane.

Effect of food

AUC and C_m_Oh (maximum concentration) of tapentadol increased by 8% and 18%, respectively, with the intake of long-acting tablets after taking fatty high-calorie food. Time to reach C_m_Oh is postponed for 1.5 hours with the intake of high-calorie food.This was considered clinically insignificant. The drug Palexia can be taken orally both before and after eating.

Distribution

Tapentadol has a large volume of distribution. After intravenous administration of tapentadol, the volume of distribution in the terminal phase of elimination (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 ingestion, approximately 70% of the dose is excreted into the urine in the form of conjugated forms (55% glucuronide and 15% tapentadol sulfate). Uridindifosfatglyukuroniltransferase (UGT) is the main enzyme involved in the glucuronation process (mainly isoenzymes UGT1A6, UGT1A9 and UGT2B7). In total, 3% of the tapentadol is excreted into the urine unchanged. TAPENTADOL also metabolized to N-desmethyltapentadol (13%) by the action of isoenzymes CYP2C9 and CYP2C19 and to hydroxy-tentadol (2%) under the action of isoenzyme CYP2D6. 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 in long-acting tablets coated with a film membrane, an average of 5-6 hours.

Special categories of patients

Elderly patients

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

Impaired renal function

AUC and C_m_Oh tapentadol are comparable in patients with varying degrees of functional kidney function (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) tapentadol-O-glucuronide. In patients with mild, moderate and severe renal dysfunction, there was an increase AUC tapentadol-O-glucuronide in 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, tapentadol intake was characterized by a higher AUC and serum concentration in comparison with patients with normal liver function. The ratios of pharmacokinetic indexes of tapentadol for groups of patients with mild to moderate hepatic insufficiency, when compared with the group of patients with normal liver function, were 1.7 and 4.2, respectively AUC; 1.4 and 2.5, respectively, for CmOh; 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.The ego is confirmed by the experience of simultaneous application of tapentadol with naproxen and probenecid, growth AUC tapentadol by 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.

Contraindications:

- hypersensitivity to tapentadol or any of the excipients included in the formulation;

- in situations where agonist drugs of mu-opioid receptors are contraindicated, i.e. in patients with significant respiratory depression (with the impossibility of observation or absence of resuscitation equipment), as well as in patients with exacerbation or severe bronchial asthma or hypercapnia;

- presence or suspicion of paralytic ileus;

- acute intoxication with alcohol, sleeping pills, central analgesics and psychotropic drugs;

- in patients receiving monoamine oxidase (MAO) inhibitors or taking them within the last 14 days;

- severe renal insufficiency;

- severe hepatic impairment;

- age to 18 years;

- deficiency of lactase, lactose intolerance, glucose-galactose malabsorption.

Carefully:Palladium should be used with caution:

- at increased risk of misuse or abuse of the drug;

- when the respiratory function is impaired;

- in patients with craniocerebral trauma and oppression of consciousness;

- in patients with a history of convulsive syndrome or any conditions that increase the risk of seizures;

- in patients with hepatic insufficiency of moderate severity;

- in patients with pathology of the bile duct and acute pancreatitis;

- in patients with low blood pressure.

It is recommended that the dose of Palexia is gradually reduced before complete cancellation. Caution is necessary when using the drug Palexia with serotonergic drugs at the same time.

Pregnancy and lactation:

Pregnancy

Data on the use of tapentadol during pregnancy are limited. In studies on animals teratogenic effects associated with tapentadol, it was not found. but in doses exceeding the upper limit of the therapeutic, delayed embryonic development and embryotoxicity (effects on the central nervous system associated with atomism to mu-opioid receptors) were detected. Influence on postnatal development of offspring was revealed with the appointment of tapentadol in doses that did not cause undesirable phenomena in pregnant females.

The use of the drug Palexia during pregnancy is permissible only if the potential benefit to the mother exceeds the potential risk to the fetus.

Childbirth

The effect of tapentadol when administered during labor is unknown. Use tapentadol during labor and immediately before childbirth is not recommended. Due to the affinity of tapentadol for mu-opioid receptors, newborns whose mothers took tapentadolshould be carefully observed in connection with the possibility of respiratory depression.

Lactation

Information on the excretion of tapentadol in breast milk is limited. Physico-chemical and pharmacodynamic / toxicological data on tapentadol indicate excretion into breast milk, so the risk of exposure to a child being fed can not be ruled out. The drug Palexia should not be prescribed during breastfeeding.

Dosing and Administration: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 the tablets of prolonged action, film-coated, 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, not 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.

The daily dose of tapentadol over 500 mg in prolonged-action tablets coated with a film membrane, ns was prescribed, therefore, in such doses, the drug is not recommended.

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 adjustment in patients with mild or moderate renal failure is not required. The experience of application in patients with severe renal dysfunction is not, therefore, the use of the drug and this group of patients is contraindicated.

Impaired liver function

Correction of doses in patients with mild hepatic impairment is not required. Care must be taken when prescribing Palexia to patients with moderate hepatic impairment. Treatment of such patients should begin with 50 mg of tapentadol in prolonged-action tablets coated with a film membrane, 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. Since 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 lack of data but efficiency and safety.

Side effects:

Approximately 60% of patients who took the drug Palexia in prolonged-action tablets coated with a film coat, side effects, mostly 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).

SIDE EFFECTS

System-Organ Classes	Frequency
System-Organ Classes	very frequent (≥1 / 10)	frequent (≥1/100, <1/10)	infrequent (≥1/1 000, <1/100)	rare (≥1/10 000, <1/1 000)
Violations from the nominal system			Hypersensitivity *
Disorders from the metabolism and nutrition		Decreased appetite	Weight loss
Disorders of the psyche		Sleep disorders, anxiety, depressed mood, increased excitability, anxiety	Unusual dreams, impaired perception, disorientation in place and in time, psychomotor agitation, confusion, euphoria	Drug addiction, pathological thinking
Disturbances from the nervous system	Dizziness, headache, drowsiness	Involuntary muscle contractions, tremors, attention disorders	Paresthesia, kinesthesia, imbalance, sedation, syncope, memory impairment, cognitive impairment, oppression of consciousness, dysarthria	Disturbances in coordination, pre-syncope, convulsions
Disturbances on the part of the organ of sight			Visual impairment
Violations from the heart and blood vessels		"Tides"	Increase heart rate, decrease heart rate, palpitations, lower blood pressure
Violations from hand respiratory system, thoracic cells and the mediastinum		Dyspnea		Oppression breathing
Violations from hand gastrointestinal tract	Nausea, constipation	Vomiting, diarrhea, indigestion	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 urination
Disorders from the reproductive system and breast			Sexual dysfunction
Are common disorders and disorders at the site of administration		Fatigue, dryness of the mucous membrane (mouth, eyes and throat), asthenia, sensation of changes in body temperature, edema	The "withdrawal" syndrome, irritability, unusual sensations	Feeling intoxication, feeling relaxation

* Note: In the postmarketing use of the drug, rare cases of angioedema, anaphylaxis and anaphylactic shock.

When taking the drug Palexia inward in the tablets of prolonged action, covered with a film membrane, up to 1 year, there are cases of a mild "withdrawal" syndrome with a sharp interruption of therapy, but they were classified as light.Nevertheless, 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 is higher in patients suffering from chronic pain. In addition, drugs with a pronounced effect on the monoaminergic system increase the risk of suicidal behavior in patients suffering from depression, especially at the beginning of treatment. Clinical studies and post-marketing experience with tapentadol have not revealed evidence of increased risk.

If any of the following side effects occur, or if there are other side effects not indicated in the instructions, tell your doctor.

Overdose:Data on overdose are very limited.

Symptoms: it is necessary to expect inherent in all drugs with central analgesic effect and characterized by affinity for mu-opioid receptors of symptoms - miosis, vomiting, collapse, depression of consciousness down to coma, convulsions and respiratory depression with the possibility of stopping it.

Urgent care: treatment of overdose should be focused on eliminating the symptoms of stimulation of mu-opioid receptors.If suspicion of an overdose of tapentadol, attention should be focused on restoring airway patency and the use of controlled or controlled ventilation of the lungs. Complete opioid receptor antagonists, such as naloxone, are specific antidotes for respiratory depression associated with an overdose of narcotic analgesics. Respiratory depression after an overdose may exceed the duration of the opioid receptor antagonist. The appointment of an opioid receptor antagonist does not replace the continuous monitoring of the airway, the control of breathing disorders and blood circulation that have developed as a result of an overdose of narcotic analgesics. If the response to the introduction of opioid receptor antagonists is insufficient or short-term, an additional administration of an opioid receptor antagonist is possible.

Purification of the gastrointestinal tract can be performed to remove ns absorbed tapentadol. The use of activated carbon or gastric lavage can be performed within 2 hours after ingestion.Before cleaning the gastrointestinal tract, it is necessary to protect the respiratory tract.

Interaction:

The simultaneous use of tapentadol with benzodiazepines, barbiturates and opioids (analgesic, antitussives and remedies for withdrawal) may increase the risk of respiratory depression. Drugs that depress the central nervous system (CNS) (benzodiazepines, antipsychotics, blockers H₁-gistaminovyh receptors, opioids, alcohol), can enhance the sedative effect of tapentadol and CNS depression. If a combination of tapentadol and drugs that cause respiratory depression or CNS is necessary, it is necessary to solve the question of reducing the dose of drugs.

Agonists-antagonists of opioid receptors. Caution should be exercised with the simultaneous use of tapentadol with agonist antagonists of mu-opioid receptors (eg, pentazocine, nalboufine) or partial agonists of mu-opioid receptors (for example, buprenorphine). With simultaneous use with buprenorphine, there was a need to increase the dose of agonists of the mu-opioid receptors, and in these circumstances careful monitoring of side effects such as respiratory depression is necessary.

There are isolated reports of the development of serotonin syndrome, but the timing coincided with the simultaneous use of tapentadol and serotonergic drugs, for example, selective serotonin reuptake inhibitors (SSRIs). Possible symptoms of serotonin syndrome may be, for example: confusion, agitation, fever, increased sweating, ataxia, hyperreflexia, myoclonia and diarrhea. The abolition of serotonergic drugs usually led to the rapid disappearance of symptoms. Therapy is determined by the nature and severity of the symptoms.

Since the main way of metabolism of tapentadol is conjugation with glucuronic acid with the participation of isoenzymes UGT1A6, UGT1A9 and UGT2B7, simultaneous use with potent inhibitors of these isoenzymes (such as ketoconazole, fluconazole, meclofenamic acid) can increase the systemic exposure of tapentadol.

Patients in the treatment of tapentadol should be careful at the beginning and at the end of simultaneous use of powerful inducers of liver enzyme systems (for example, rifampicin, phenobarbital, preparations of St. John's wort),because the ego can lead to a decrease in effectiveness or a risk of side effects, respectively.

Tapentadol is contraindicated in patients receiving monoamine oxidase inhibitors (MAO) or taking them for the last 14 days, it is possible to increase the content of noradrenaline, which can cause side effects from the cardiovascular system, such as hypertensive crisis.

Special instructions:

Possible abuse of the drug

There is a potential risk of abuse of the drug Palexia. This should be taken into account when prescribing the drug in situations where there is a risk of misuse, abuse of the drug or transfer of the drug to others.

All patients treated with mu-opioid receptor agonist drugs are closely monitored for drug abuse and dependence.

Inhibition of breathing

In high doses and in patients with hypersensitivity to agonists of mu-opioid receptors tapentadol can provoke a dose-dependent respiratory depression. For this reason, patients with respiratory function impairment drug Palexia should be administered with caution.Consider the possibility of using analgesics other than agonists of mu-opioid receptors, and Palexia in these patients should be used only under close medical supervision and in minimal effective doses. In respiratory depression, treatment should be performed as in the case of respiratory depression when any other agonist of mu-opioid receptors is used.

Craniocerebral injury and increased intracranial pressure

As with the use of other drugs - agonists of mu-opioid receptors, tapentadol should not be given to patients who may be particularly sensitive to pathophysiological reactions developing with increasing partial pressure of carbon dioxide in the intracranial vessels and brain tissue, for example, with increased intracranial pressure, oppression or coma. Analgesics, characterized by their affinity for mu-opioid receptors, can mask the clinical manifestations of craniocerebral trauma. The drug Palexia should be used with caution in patients with craniocerebral trauma and brain tumors.

Convulsions

A systematic study of tapentadol in patients with convulsive syndrome was not performed. Nevertheless, like other analgesics with an affinity for mu-opioid receptors, the preparation Palexia should be administered with caution to patients with a history of convulsive syndrome or any conditions that put the patient at risk for seizures.

Liver failure

In patients with mild and moderate hepatic insufficiency, respectively, a 2-fold and 4.5-fold increase in systemic exposure compared with patients with normal liver function. The drug Palexia should be used with caution in patients with moderate hepatic impairment. The drug Palexia in patients with severe impairment of liver function has not been studied and therefore it is contraindicated for use in this group of patients.

Use in the pathology of the pancreas and bile ducts

Drugs that have an affinity for mu-opioid receptors can cause spasm of the sphincter of Oddi. The drug Palexia should be used with caution in patients with pathology of the bile duct and acute pancreatitis.

The "cancellation" syndrome

With the simultaneous discontinuation of taking tapentadol, the syndrome of "cancellation" is possible. The following symptoms may occur: anxiety, increased sweating, insomnia, chills, pain, nausea, tremors, diarrhea, symptoms from the upper respiratory tract, piloerection and, rarely, hallucinations. In order to prevent the syndrome of "withdrawal", it is recommended that the dose of the drug be gradually reduced before complete cancellation.

Reduction of blood pressure

The drug Palexia can cause a significant reduction in blood pressure especially in patients with hypovolemia or taking concomitantly with tapentadol drugs that reduce the tone of peripheral vessels (eg, phenothiazine derivatives, anesthesia products).

Serotonin syndrome

There are reports of the development of a life-threatening serotonin syndrome with the simultaneous use of tapentadol even in therapeutic doses with serotonergic drugs: selective serotonin reuptake inhibitors (SSRIs), serotonin and noradrenaline reuptake inhibitors, tricyclic antidepressants, tryptanes, drugs that affect serotonergic transmission in the central nervous system (for example, mirtazapine, trazodone and tramadol), and drugs that interfere with the metabolism of serotonin (eg, MAO inhibitors). Possible symptoms of serotonin syndrome may be, for example: confusion, agitation, coma, tachycardia, increased body temperature, impaired coordination of movements, nausea, vomiting and diarrhea.

Tapentadol should be used with caution in patients with adrenocortical insufficiency (eg, in Addison's disease), in patients with alcoholic delirium, toxic psychosis, in patients with myxedema and hypothyroidism, as well as in prostatic hypertrophy and urethral strictures.

Effect on the ability to drive transp. cf. and fur:Like other agonist drugs of mu-opioid receptors, Palexia may be negative to influence the ability to manage motor transport and complex mechanisms, because has an effect on the central nervous system. Especially often this effect is possible at the beginning of treatment, with any changes in the dose of the drug, while taking with tranquilizers or alcohol. Patients should refrain from driving a car and engaging in potentially hazardous activities.

Form release / dosage:Extended-release tablets, film-coated, 50 mg, 100 mg, 150 mg, 200 mg, 250 mg.

Packaging:For 10 tablets of prolonged action, film-coated, in a contiguous cell pack of PVC / PVDC / paper / PET / aluminum. For 2 or 6 contour packagings together with instructions for use in a cardboard bundle.

Storage conditions:

At a temperature of no higher than 30 ° C. Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-002631

Date of registration:22.09.2014

The owner of the registration certificate:Grünenthal GmbHGrünenthal GmbH Germany

Manufacturer: & nbsp

FARMACEUTICI FORMENTI, S.p.A. Italy

Representation: & nbspNizhpharm, JSCNizhpharm, JSCRussia

Information update date: & nbsp28.10.2015

Illustrated instructions

Instructions

Palexia (Palexia)