Transtec (Transtec®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceBuprenorphineBuprenorphine
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  • Bupralal®
    solution for injections 
    MOSCOW ENDOCRINE FACTORY, FSUE     Russia
  • Transtec
    patch through. 
    Grünenthal GmbH     Germany
    • Dosage form: & nbspTransdermal patch.
    Composition:Transtec 35 microgram / hour transdermal patch:
    One transdermal patch contains the active substance buprenorphine 20 mg. Surface containing the active substance: 25 cm2.
    The size of the transdermal patch: 72x72 mm ± 2 mm.
    Nominal release rate: 35 micrograms of buprenorphine per hour (for 96 hours).
    Excipients: oleyl oleate 30 mg, povidone K 90 20 mg, levulinic acid 20 mg.
    Adhesive matrix: poly [acrylic acid-co-butyl acrylate-co- (2-ethylhexyl) acrylate-co-vinyl acetate], cross-linked (Durotak 387-2054) 110 mg.

    Transtec 52.5 microgram / hour transdermal patch:
    One transdermal patch contains the active substance - buprenorphine 30 mg. Surface containing the active substance: 37.5 cm2.
    The size of the transdermal patch: 72x97 mm ± 2 mm.
    Nominal release rate: 52.5 micrograms of buprenorphine per hour (for 96 hours).
    Excipients: oleyl oleate 45 mg, povidone K 90 30 mg, levulinic acid 30 mg.
    Adhesive matrix: poly [acrylic acid-co-butyl acrylate-co- (2-ethylhexyl) acrylate-co-vinyl acetate], cross-linked (Durotak 387-2054) 165 mg.
    Transtec 70 microgram / hour transdermal patch:
    One transdermal patch contains the active substance - buprenorphine 40 mg. Surface containing active substance: 50 cm2.
    The size of the transdermal patch: 72x122 mm ± 2 mm.
    Nominal release rate: 70 micrograms of buprenorphine per hour (for 96 hours).
    Excipients: oleyl oleate 60 mg, povidone K 90 40 mg, levulinic acid 40 mg.
    Adhesive matrix: poly [acrylic acid-co-butyl acrylate-co- (2-ethylhexyl) acrylate-co-vinyl acetate], cross-linked (Durotak 387-2054) 220 mg.
    Description:Rectangular plaster with rounded corners on an aluminized rigid removable protective layer with a solid color base. In the center there is a reservoir - the matrix of the drug.
    The appearance of the matrix containing the active substance is a light brown sticky mass applied to the tissue base of the patch.
    Pharmacotherapeutic group:An analgesic opioid: an opioid receptor agonist-antagonist
    ATX: & nbsp

    N.07.B.C.01   Buprenorphine

    Pharmacodynamics:

    Buprenorphine is a strong opioid analgesic, acts as a μ-opioid receptor agonist and an antagonist of c-opioid receptors.
    Buprenorphine is similar to morphine, but has certain clinical and pharmacological features.

    The ratio of analgesic activity of buprenorphine to morphine is determined as follows:

    Morphine is orally correlated with buprenorphine in the transdermal patch as 1: 75 - 115 (with repeated use in patients with chronic pain syndrome).

    In addition, to compare the analgesic effect, factors such as the route of administration of the drug, the indication by which the drug is used, the clinical state of the patient and interindividual variability should be considered.

    Side effects are similar to other opioid analgesics. In buprenorphine, the risk of dependence is lower than with morphine.
    Pharmacokinetics:Binding to plasma proteins is about 96%. Metabolized in the liver to N-dezalkylbuprenorphine (norbuprenorphine) and glucuronated metabolites. 2/3 of the active substance is released unchanged through the intestine and 1/3 is excreted by the kidneys as conjugates of unchanged or dealkylated buprenorphine. There may be enteric-liver recirculation.
    After the application of transdermal Transtec, buprenorphine absorbed through the skin.Constant inflow of active substance into the body is provided by an adhesive polymer matrix system.
    At the first application the concentration of buprenorphine in the blood plasma gradually increases and after 12-24 hours reaches the minimum effective 100 pg / ml. From studies of transdermal Transtec plaster 35 microgram / h it is known that the average maximum concentration of Stax = 200-300 pg / ml is observed with an average time of reaching a maximum concentration of tmax = 60-80 hours.
    After removing Transtec transdermal patch, the buprenorphine concentration in the plasma gradually decreases with an approximate half-life of 30 hours (22 to 36 hours). Due to the continued absorption of buprenorphine from the subcutaneous tissue, buprenorphine is displayed more slowly than with intravenous administration. Buprenorphine penetrates through the blood-brain and placental barrier. In experiments on pregnant and nonpregnant rats it was revealed that the concentration of buprenorphine in the brain, where only the unchanged buprenorphine, after parenteral application is 2-3 times higher than when administered orally.After intramuscular or oral administration, the fetus has an accumulation of buprenorphine in the lumen of the digestive tract, probably due to excretion of bile and underdevelopment of the mechanism of enterohepatic circulation.
    Indications:Pain syndrome of medium and high intensity in cancer diseases; pain syndrome of high intensity, with ineffectiveness of non-narcotic analgesics. Transtec is not indicated for acute pain.
    Contraindications:- hypersensitivity to buprenorphine, adhesive or excipients of the drug (see section "Composition"),
    - use in patients with opioid dependence, as well as for the treatment of opioid withdrawal syndrome,
    - conditions that may entail or are already accompanied by violations of breathing or depression of the respiratory center,
    - combined use with monoamine oxidase (MAO) inhibitors, and within two weeks after the abolition of MAO inhibitors (see "Interaction with other drugs"),
    - Myasthenia gravis,
    - alcoholic delirium,
    - age under 18 years (no data),
    - pregnancy and lactation period (see p.section "Application in pregnancy and lactation")
    Carefully:- Acute alcohol intoxication,
    - convulsive syndrome,
    - craniocerebral injury,
    - state of shock,
    - a disorder of unclear genesis, intracranial hypertension of unknown origin,
    - together with drugs that depress the breath (see the section "Interaction with other medicinal products"),
    - in patients suspected of drug abuse,
    - for violations of liver function (see section "Special instructions"),
    - in patients with high body temperature, or subjected to overheating in conditions of high ambient temperature (see section "Special instructions").
    Pregnancy and lactation:The use of Transtec during pregnancy and during breastfeeding is contraindicated.
    Data on the use of Transtec during pregnancy are absent. In the course of animal studies, reproductive toxicity was identified. Possible risks for humans are not defined.
    In late pregnancy, high doses of buprenorphine can cause respiratory depression in the newborn even after short-term use.Long-term use of buprenorphine during the last trimester of pregnancy can lead to the development of symptoms of "cancellation" in a newborn.
    Lactation
    Buprenorphine penetrates into breast milk. In studies on rats, it was found that buprenorphine can suppress lactation.
    Transtec should not be given during breastfeeding.
    Dosing and Administration:Dosing regimen
    Patients over 18 years of age
    The dose of Transtec is selected in accordance with the patient's condition (depending on the severity of the pain syndrome and the response to ongoing therapy). The lowest effective dose should be selected. To optimize the therapy, three doses of buprenorphine in the transdermal patch are possible: Transtec 35 micrograms per hour, Transtec 52.5 micrograms per hour and Transtec 70 micrograms per hour.

    Choice of initial dose
    Patients who had not previously received analgesics should begin therapy with a minimum dosage of Transtec transdermal patch 35 μg / h. Patients who received previous stage I (non-opioid analgesics) according to the recommendations of the World Health Organization (WHO) or stage II analgesics (weak opioids) should also receive Transtec at a dosage of 35 micrograms / hour.According to WHO recommendations, simultaneous use with non-narcotic analgesics is possible depending on the general condition of the patient.
    When switching from analgesics of stage III (strong opioids) to Transtec and choosing the initial dosage of the transdermal patch, the class, route of administration and the average daily dose of the drug of the previous therapy should be taken into account in order to avoid relapse of the pain syndrome. The dose is selected individually, starting with the minimum (Transtec 35 micrograms / h). Clinical experience has shown that patients who received previously high doses of strong opioids (approximately corresponding to ingestion of 120 mg of morphine) should begin therapy with a higher dose of buprenorphine in the transdermal patch (also see the section "Pharmacodynamics").
    In order to quickly and correctly choose the optimal dose, in the period of its selection, immediate release analgesics should be additionally applied in sufficient quantities.
    The dose of Transtec is determined individually and should be monitored regularly.
    After the first application of Transdermal Transtec transdermal patch, the concentration of buprenorphine in serum increases slowly, regardless of whether the patient has previously taken analgesics or not.Therefore, the first evaluation of the analgesic effect should be performed no earlier than 24 hours later.
    Formulations of previous therapy (with the exception of transdermal opioids) should be administered in the same doses within the first 12 hours after transition to Transtec, and also if necessary within the next 12 hours.
    Selection of maintenance therapy dose
    Transtek transdermal patch should be replaced not later than 96 hours (4 days). For convenience, the transdermal patch can be changed twice a week at regular intervals, for example, always on Mondays in the morning and on Thursdays in the evening. The dose can be increased before the onset of adequate analgesia. If, at the end of the dose selection period, a sufficient level of analgesia is not obtained, the dose can be increased either by applying an additional transdermal patch of the same dosage or by switching to the next highest dosage of the transdermal patch.
    Before switching to the next largest dose of Transtec, it is necessary to review the amount of opioids that the patient took in addition to the previous dosage of the transdermal patchand adjust the amount of opioid supplementary therapy in accordance with the new Transtec dosage. Patients in need of additional pain relief (for example, in case of temporary pain) can receive 1-2 buprenorphine tablets 0.2 mg sublingually every 24 hours in addition to transdermal patch therapy. If the amount of additional analgesics reaches 0.4-0.6 mg in terms of buprenorphine sublingually, it is necessary to transfer the patient to the next dosage of the transdermal patch.
    Patients under 18 years of age
    Since the use of Transtec in patients under the age of 18 years has not been studied, the drug is not used in this category of patients.
    Elderly patients
    There is no need to adjust the dose of Transtec for elderly patients.
    Patients with renal insufficiency
    There are no special instructions (see section "Special instructions").
    Patients with hepatic insufficiency
    The effectiveness and duration of analgesia may vary (see section "Special instructions").
    Mode of application
    Transtek is glued to a clean, even, non-inflamed skin without hair, and there should be no large scars on the surface of the skin.Preferred is the application in the upper part of the body: the upper back or the surface of the chest below the clavicle. Hair must be removed with scissors (do not shave). If necessary place the application of the transdermal patch can be washed with water. It is not recommended to use soap or other detergents. Also, skin care products that can affect the adhesion of Transtec transdermal patch should be avoided.
    The transdermal patch should be stuck on completely dry skin. Transtec should be used immediately after extraction from the sachet. After removing the protective film, the transdermal patch should be strongly pressed to the skin with the palm for about 30 seconds. Transdermal patch is not damaged during washing or swimming. However, it should not be subjected to excessive heating (for example, a sauna or infrared radiation).
    You can not wear Transtek continuously for more than 4 days. After removing the previous transdermal patch, the next is glued to another area of ​​the skin. At the same place transdermal patch can be pasted not earlier than one week.
    Duration of Transdermal Transtec Transplant Trim
    Transtek transdermal patch should be used only if absolutely necessary. If the disease and its severity require long-term use, it is necessary to ensure regular and thorough monitoring, possibly with interruptions in treatment, and a reassessment of the need for further use of the drug and the duration of its use.
    Termination of transdermal Transtek transplant application
    After removing the Transtec transdermal patch, the serum buprenorphine concentration decreases gradually, and thus the analgesic effect is maintained for a certain time. This should be taken into account when prescribing other opioids after Transtec therapy. As a rule, subsequent therapy with opioids should not begin earlier than 24 hours after Transtec removal. At the moment, there is insufficient information on the starting doses of other opioids used after the discontinuation of Transtec.
    Side effects:The following side effects have been reported.
    To assess the incidence of side effects, the following gradation is used:
    Very often: (> 1/10)
    Often: (≥ 1/100, <1/10)
    Infrequently: (≥ 1/1000, <1/100)
    Rarely: (≥ 1/10000, <1/1000)
    Very rarely: (≤ 1/10000)
    Insufficient data: on the basis of available data it is impossible to estimate frequency.
    A) The most frequent systemic side effects are nausea and vomiting.
    The most frequent side effects in the place of application are erythema and itchy skin.
    B) From the immune system.
    Very rarely: serious allergic reactions *.

    From the side of metabolism and nutrition.
    Rarely: loss of appetite.
    Disorders of the psyche.
    Infrequently: confusion, sleep disturbance, anxiety.
    Rarely: psychotomimetic effects (for example, hallucinations, anxiety, nightmares), decreased libido.
    Very rarely: drug dependence, mood change.
    From the nervous system.
    Often: dizziness, headache.
    Infrequent: sedation, drowsiness.
    Rarely: impaired concentration, speech impairment, numbness, imbalance, paresthesia (eg, tingling sensation or burning sensation of the skin).
    Very rarely: fasciculation, changing the perception of taste.
    From the side of the organ of sight.
    Rarely: impaired vision, blurred vision, swelling of the eyelids.
    Very rarely: miosis.
    From the side of the organ of hearing.
    Very rarely: pain in the ear.
    From the cardiovascular system.
    Infrequent: impaired blood circulation (arterial hypotension, less often collapse). Rarely: "hot flushes".
    From the respiratory system.
    Often: shortness of breath.
    Rarely: respiratory depression.
    Very rarely: hyperventilation, hiccough.
    From the digestive system.
    Very often: nausea.
    Often: vomiting, constipation.
    Infrequent: dry mouth.
    Rarely: heartburn.
    Very rarely: the urge to vomit.
    From the skin and subcutaneous tissues.
    Very often: redness, itching.
    Often: exanthema, increased sweating.
    Infrequent: rash.
    Rarely: urticaria.
    Very rarely: pustular and vesicular rash.
    From the genitourinary system.
    Infrequent: urinary retention, impaired urination.
    Rarely: an erection disorder.
    General disorders and local reactions.
    Often: swelling, fatigue.
    Uncommon: exhaustion.
    Rarely: withdrawal syndrome *, skin reactions at the site of application. Very rarely: chest pain.
    * See section B below.
    B) In some cases, delayed allergic reactions develop with marked signs of inflammation. In such cases, the use of Transtec should be discontinued.
    Buprenorphine is characterized by a low risk of dependence. After the withdrawal of the drug manifestation of the syndrome of "cancellation" is unlikely.This is due to the very slow dissociation of buprenorphine with opioid receptors and a gradual decrease in the concentration of the substance in the blood serum (usually within 30 hours after removal of the last transdermal patch). However, after long-term use of Transtec, it is impossible to completely exclude the possibility of developing symptoms similar to the "withdrawal" of opioids. Such symptoms include: anxiety, agitation, nervousness, insomnia, hyperkinesia, tremor and gastrointestinal disorders.
    If any of the following side effects occur, or if any other side effects are noted that are not listed in the instructions, tell your doctor.

    Overdose:Buprenorphine has a wide therapeutic range. Due to the constant intake rate of small amounts of buprenorphine from the transdermal patch to the total blood flow, the probability of toxic concentrations of buprenorphine is very low. The maximum concentration of buprenorphine in the blood serum after the application of transdermal Transtache patch is 70 micrograms / hour approximately six times less than when intravenously administered a therapeutic dose of buprenorphine equal to 0.3 mg.

    Symptoms
    With an overdose of buprenorphine, the same symptoms are possible as in the case of an overdose of other analgesics of the central action, for example: respiratory depression, sedation, drowsiness, nausea, vomiting, cardiovascular collapse, pronounced miosis.
    Treatment
    General first aid measures should be carried out. Ensure airway patency (possible aspiration!), Simtomatic correction of respiratory and circulatory disorders. Naloxone has a limited effect on respiratory depression caused by buprenorphine. High doses of naloxone are required, which can be administered by repeated bolus injections, or infusion (for example, starting with a bolus intravenous injection of 1-2 mg, after achieving a sufficient antagonistic action, it is recommended to infuse naloxone to maintain a constant concentration of the substance in the blood plasma). Adequate ventilation should be provided.
    Interaction:In patients who took MAO inhibitors for 14 days before using pethidine opioid, life-threatening reactions from the central nervous system (CNS), cardiovascular system,violation of breathing. It is impossible to exclude a similar interaction of MAO inhibitors with buprenorphine (see "Contraindications"),
    The use of Transtec together with other opioids, anesthetics, hypnotics and sedatives, antidepressants, neuroleptics and any other drugs that depress respiration and central nervous system function potentiates the effect of these drugs on the CNS. This also applies to alcohol.
    When combined with inhibitors or inductors of the CYP isoenzyme ZA4, Transtec's effectiveness can accordingly increase (inhibit) or decrease (inducers).
    Special instructions:Because the buprenorphine can cause respiratory depression, caution should be exercised in the treatment of patients with suspected respiratory failure or receiving drugs that can depress respiration.
    Buprenorphine, compared with pure opioid agonists, has a much lower potential for drug dependence. In studies conducted on patients and healthy volunteers, no reactions were recorded for the abolition of buprenorphine.However, after prolonged use of Transtec, the possibility of developing symptoms similar to the symptoms of "withdrawal" of opioids (see "Side Effects") can not be completely ruled out.
    In patients who abuse opioids, buprenorphine therapy can affect the development of withdrawal symptoms of opioids. In this case, there is the possibility of abuse of buprenorphine, caution should be exercised in prescribing patients with addiction to drug dependence.
    Patients with hepatic insufficiency
    Buprenorphine is metabolized in the liver. In patients with impaired liver function, the intensity and duration of the effect of the drug may vary. The use of Transtec in such patients should be controlled by a specialist.
    Patients with renal insufficiency
    Since the pharmacokinetics of buprenorphine in renal insufficiency does not change, the drug can be used in patients with renal insufficiency, including those on dialysis.
    Since the use of Transtec in patients under the age of 18 years has not been studied, the drug is not used in this category of patients.
    Patients with fever or undergoing overheating in conditions of elevated temperature
    Fever and heating from external heat sources can enhance skin permeability. Theoretically, in such a situation, after application of Transdermal Transtec patch, an increased concentration of buprenorphine in the blood serum can be observed, therefore, when using the drug in patients with fever or elevated body temperature, for other reasons, possible opioid reactions should be closely monitored.
    Effect on the ability to drive transp. cf. and fur:Buprenorphine has a pronounced effect on the ability to drive and work with machinery.
    Even application in accordance with the instructions for use can affect the speed of psychomotor reactions, reducing the safety of driving and the ability to work with mechanisms. This effect is especially pronounced at the beginning of treatment, with any dose changes or with other central action substances, including alcohol, tranquilizers, sedatives and hypnotics.
    If there is dizziness, drowsiness, or visual impairment, the patient should not drive the car or moving machinery during the Transtech period and not earlier than 24 hours after removing the transdermal patch.
    These restrictions may not apply to patients who consistently take a constant dose of the drug and in the absence of the above symptoms, but should consult with a medical specialist.
    Form release / dosage:Transdermal patch 35, 52.5 and 70 μg / h.
    Packaging:1 patch transdermal in the sachet.
    For 3, 5 or 10 sachets, along with instructions for use in a cardboard bundle.
    Storage conditions:At a temperature of no higher than 25 ° C.
    Inaccessible to children!
    List II. In accordance with the Federal Law of the Russian Federation "On Narcotic Drugs and Psychotropic Substances".

    SPECIAL PRECAUTIONS IN DESTROYING
    Patients should be informed that the used transdermal patch must be rolled up with the sticky side inward and returned to the doctor for destruction. Patients should also return unused transdermal patches to the doctor.
    Shelf life:3 years.
    Do not use after the expiry date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:П N015004 / 01-2003
    Date of registration:04.04.2008
    The owner of the registration certificate:Grünenthal GmbHGrünenthal GmbH Germany
    Manufacturer: & nbsp
    Representation: & nbspSTADA CISASTADA CISARussia
    Information update date: & nbsp2015-12-03
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