Bupraxon
Bupraxon: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Bupraxon
ATX code: N02AE01
Active ingredient: naloxone (Naloxone) + buprenorphine (Buprenorphine)
Manufacturer: FSUE "Moscow Endocrine Plant" (Russia)
Description and photo update: 2019-11-07
Bupraxone is a combined sublingual analgesic drug.
Release form and composition
Dosage form - sublingual tablets: white, biconvex, round (in a cardboard box 1 or 2 blister packs of 10 tablets and instructions for use of Bupraxone).
Composition for 1 tablet:
- active substances: buprenorphine - 0.2 mg (buprenorphine hydrochloride - 0.216 mg); naloxone 0.2 mg (naloxone hydrochloride 0.222 mg);
- auxiliary components: colloidal silicon dioxide - 0.6 mg; lactose monohydrate - 27.729 mg; potato starch - 9 mg; mannitol (mannitol) - 18 mg; crospovidone - 1.8 mg; low molecular weight polyvinylpyrrolidone medical povidone - 1.233 mg; magnesium stearate - 0.6 mg; citric acid monohydrate (or citric acid in terms of citric acid monohydrate) - 0.6 mg.
Pharmacological properties
Pharmacodynamics
Bupraxone is a combination drug that contains buprenorphine and naloxone. The pharmacological action in sublingual administration is determined by the properties of buprenorphine.
After sublingual use of Bupraxone, the effect of buprenorphine takes about 30 minutes. The maximum effect develops after 3 hours. The duration of the analgesic effect is up to five hours.
Buprenorphine
Buprenorphine belongs to the group of opioid analgesics - semi-synthetic derivatives of thebaine, is a partial antagonist of κ-opioid receptors and a partial agonist of the β-opioid receptor subtype.
In terms of the severity of the analgesic effect when used in equivalent doses, buprenorphine is similar to morphine. As a partial agonist of opioid receptors, it causes respiratory depression and has an effect on smooth muscles, although to a lesser extent than morphine and other opiates. In comparison with them, it has less potential for physical dependence. At the same time, a certain addictive potential of a substance is associated with the activation of µ-opioid receptors.
Naloxone
Naloxone is an opioid receptor antagonist that effectively attenuates / eliminates the effects of opioids and opiates. Its action is aimed at restoring breathing, reducing sedative and euphorizing effects. May lead to the development of opiate withdrawal syndrome when they are previously administered for pain relief or in patients with drug addiction and using opioid analgesics.
Pharmacological effects occur only in the case of parenteral (intravenous, intramuscular, subcutaneous) administration. If naloxone is applied sublingually, then it hardly enters the systemic circulation and has no pharmacodynamic effect.
The substance, when taken orally, practically does not show pharmacological activity, when administered orally and parenterally, the ratio of the effectiveness of naloxone is 1 ÷ 50.
Pharmacokinetics
Buprenorphine
Buprenorphine is well absorbed after sublingual administration. Systemic bioavailability is approximately 50–55%. After taking a dose of 0.4 mg, C max (maximum concentration) of the substance in the blood plasma averages 1.13 ng / ml and is reached in 2 hours.
The substance penetrates well through the blood-brain barrier. It binds to blood plasma proteins at a level of 96%, mainly with α- and β-globulins. V d (volume of distribution) is 2.5 liters, which confirms its active capture by tissues and organs.
Buprenorphine metabolism occurs in the liver by N-dealkylation, with the formation of norbuprenorphine (with the participation of the isoenzyme CYP3A4), then glucuronidation and the formation of conjugates with glucuronic acid. The main metabolite is norbuprenorphine, which is also glucuronidated. It does not possess significant analgesic activity.
T 1/2 (half-life) of a substance from blood plasma is in the range from 24 to 42 hours. Metabolites are excreted by the kidneys and bile (30 and 69%, respectively). Only about 1% of buprenorphine is excreted unchanged.
Naloxone
Naloxone with the sublingual route of administration is practically not absorbed. Systemic bioavailability is less than 5%. Plasma concentration in blood is not significant. The substance binds to blood plasma proteins at a level of 45%, binding occurs mainly with albumin.
It has been established that naloxone, when administered sublingually, has a low bioavailability (within 9 ± 6%). The absorbed small amount of naloxone does not create therapeutic concentrations in blood plasma and does not affect the effects and metabolism of buprenorphine.
The substance undergoes rapid metabolism in the liver and direct glucuronization to naloxone-3-glucuronide, as well as reduction (6-oxo group) and N-dealkylation.
T 1/2 of naloxone is within 2-12 hours. Excretion of metabolites is carried out mainly by the kidneys.
Indications for use
- postoperative pain syndrome (moderate to severe intensity);
- pain syndrome caused by burns and injuries;
- preparation and implementation of diagnostic procedures.
Contraindications
Absolute:
- conditions that are accompanied by pronounced depression of the central nervous system or depression of the respiratory center, or in which the development of breathing disorders is possible;
- combined use with monoamine oxidase inhibitors, both throughout the entire period of use of these drugs, and for another 14 days after their withdrawal;
- mucositis, stomatitis, lesions of the oral mucosa of ulcerative-necrotic and inflammatory nature;
- drug dependence, including opioid;
- decompensated cor pulmonale;
- traumatic brain injury;
- paralytic ileus;
- status asthmaticus, bronchial asthma;
- convulsive conditions;
- acute alcohol intoxication;
- cardiac arrhythmias, including supraventricular and ventricular paroxysmal tachycardia, atrial fibrillation, extrasystole;
- lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
- acute surgical diseases of the abdominal organs (use is contraindicated until a diagnosis is established);
- pregnancy and lactation;
- age up to 18 years;
- individual intolerance to the components of the drug.
Relative (Bupraxon tablets are prescribed under medical supervision):
- renal / hepatic impairment;
- myxedema;
- depression of the central nervous system;
- hypothyroidism;
- hyperplasia of the prostate;
- toxic psychosis;
- alcoholism;
- respiratory and adrenal insufficiency;
- strictures of the urethra;
- elderly and senile age.
Bupraxon, instructions for use: method and dosage
Bupraxone is intended for sublingual administration. The tablets must be kept under the tongue until they are completely absorbed.
The dose of the drug and the duration of therapy are selected by the doctor individually.
Single dose - 1 or 2 tablets (maximum). During the day, it is possible to reapply Bupraxone at the same dose every 6–8 hours (maximum 8 tablets per day).
A reduction in the dose of Bupraxone is required for elderly patients, patients with hypovolemic conditions, the risk of surgical pathology, as well as when combined with sedatives and other narcotic analgesics.
To avoid excessive suppression of the activity of the respiratory center and depression of the central nervous system, Bupraxone should be used in reduced doses against the background of the action of hypnotics, general anesthetics, anxiolytics, antipsychotics and antidepressants.
Side effects
Adverse events that occur during the use of Bupraxone are due to the pharmacological action of the active component of buprenorphine.
Possible side effects [> 10% - very common; (> 1% and 0.1% and 0.01% and <0.1%) - rarely; <0.01% - very rare)]:
- sense organs: often - blurred vision, miosis, diplopia; very rarely - conjunctivitis;
- digestive system: often - nausea; rarely - constipation, vomiting, xerostomia;
- nervous system: very often - sedation; often - weakness, headache, dizziness; rarely - tinnitus, fatigue / weakness, lethargy, confusion, drowsiness, nervousness, psychosis, depression, slurred speech, slowing down of the speed of motor and mental reactions, euphoria, paresthesia; with prolonged use - the occurrence of opioid dependence and addiction;
- urinary system: rarely - urinary retention;
- skin: rarely - itching, cyanosis;
- metabolism: rarely - sweating;
- cardiovascular system: often - increased blood pressure; rarely - hot flushes, bradycardia, tachycardia, coldness / chills;
- respiratory system: rarely - shortness of breath, depression of the respiratory center, hypoventilation;
- allergic reactions: rarely - urticaria, rash.
Overdose
The main symptoms of a bupraxone overdose are associated with the buprenorphine it contains. They manifest as sedation, nausea, vomiting, drowsiness, respiratory depression, and miosis.
Therapy: verbal and physical stimulation of the patient, symptomatic treatment, including infusion therapy, the use of oxygen, parenteral administration of naloxone (a single intramuscular or intravenous administration is recommended at a dose of 0.4–2 mg with repeated administration after 2–3 minutes to a total dose of 10 mg and more). Due to the high affinity of buprenorphine for opioid receptors, higher doses of naloxone should be used than in cases of morphine and other full opioid agonist poisoning. Sometimes assisted and artificial ventilation is prescribed.
special instructions
Naloxone is included in Bupraxone to increase drug abuse safety. In cases of non-medical use of the drug, naloxone will block the effects of buprenorphine, which interferes with the action that is pursued by drug abuse. With physical dependence on opioids, this can lead to withdrawal symptoms.
With impaired liver function, the duration and intensity of the action of Bupraxone may vary, therefore, the use of the drug in such patients should be carried out under the supervision of a specialist.
Nicotine helps to reduce the pharmacological activity of Bupraxone.
In case of accidental / deliberate administration of the drug in children, respiratory depression may develop, which can lead to death.
Influence on the ability to drive vehicles and complex mechanisms
Driving during therapy with Bupraxone should be abandoned.
Application during pregnancy and lactation
Bupraxone is not prescribed during pregnancy / lactation.
The potential risk of the drug to humans is unknown. No controlled studies have been conducted in pregnant women.
Buprenorphine, even when used briefly at the end of pregnancy, can cause respiratory depression in the newborn. Long-term therapy during the last three months of pregnancy can cause withdrawal symptoms in newborns (including hypertension, tremors, neonatal agitation, seizures, or myoclonus). Most often, the postpartum syndrome lasts from several hours to several days.
There is no evidence to support or disprove that naloxone is excreted in breast milk. Buprenorphine and its metabolites are excreted from the body through breast milk.
In studies on rats, it was found that buprenorphine inhibits lactation. Also, studies have shown inhibition of female fertility, when taken in doses that are many times higher than the average daily dose for humans.
Pediatric use
Bupraxone is not prescribed for patients under 18 years of age.
With impaired renal function
Bupraxone for renal failure should be used under medical supervision.
For violations of liver function
Bupraxone for liver failure should be used under medical supervision.
Use in the elderly
For elderly / senile patients, Bupraxone tablets are prescribed with caution.
Drug interactions
- ethanol, anxiolytics, general anesthetics, sedatives, hypnotics, antihistamines, antipsychotics, benzodiazepines, phenothiazines and other tranquilizers: Bupraxone potentiates their action;
- monoamine oxidase inhibitors: against the background of combined use, arterial hypertension, convulsions, malignant hyperthermia, coma may occur;
- full opioid agonists: possible development of an opiate withdrawal syndrome;
- valproic acid / sodium valproate: there is an increase in the inhibitory effect on the central nervous system;
- other analgesics: an increase in cerebrospinal fluid pressure is likely, and therefore the use of Bupraxone requires caution in cases where the cerebrospinal fluid pressure can be increased, since buprenorphine can lead to a change in the level of consciousness and miosis;
- drugs that inhibit the activity of the CYP3A4 isoenzyme (macrolides, ketoconazole, erythromycin, and others), HIV protease inhibitors (ritonavir): with simultaneous use, the effects of buprenorphine may increase and their duration may be increased, while dose adjustment of one or both drugs is necessary;
- inducers of the CYP3A4 isoenzyme (including rifampicin, phenobarbital, phenytoin, carbamazepine): the plasma concentration of buprenorphine in the blood may decrease; the interaction of buprenorphine with all inducers of the CYP3A4 isoenzyme has not been studied, therefore, it is recommended to monitor the condition of patients for symptoms and signs of withdrawal;
- herbal medicines: may affect the pharmacological activity of buprenorphine; when combined with St. John's wort (is an inducer of the isoenzyme CYP3A4), a decrease in the plasma concentration of buprenorphine in the blood is likely;
- ethanol: against the background of simultaneous use, there is an increase in the inhibition of the central nervous system by buprenorphine, during the period of therapy, alcohol should be discarded.
Analogs
Bupraxone analogs are Transtek, Bupranal, Nurofen Plus, Santoperalgin, Pentalgin-ICN, Sedal-M, Targin, Sedalgin-Neo.
Terms and conditions of storage
Store in a place protected from light at temperatures up to 25 ° C. Keep out of the reach of children.
Shelf life is 4 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Bupraxone
There are practically no reviews about Bupraxone, the drug is included in the list of narcotic and psychotropic drugs, the circulation of which in the Russian Federation is limited.
Price for Bupraxone in pharmacies
Since the drug is not available in pharmacies, the price of Bupraxone is unknown.
The approximate cost of analogues: Nurofen Plus (12 tablets) - 359 rubles, Sedal-M (20 tablets) - 250 rubles.
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
