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

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Dosage form: & nbsptablative hyoid

Composition:On one tablet.

Active substances: buprenorphine hydrochloride - 0.216 mg, equivalent to 0.200 mg buprenorphine; naloxone hydrochloride - 0.222 mg, equivalent to 0.200 mg of naloxone

Excipients: lactose monohydrate 27.729 mg mannitol 18,000 mg, potato starch 9,000 mg povidone low molecular weight polyvinylpyrrolidone 1,233 mg crospovidone polyplasdone XL - 10) - 1,800 mg, citric acid monohydrate (or citric acid in terms of citric acid monohydrate) - 0.600 mg, magnesium stearate - 0.600 mg, silicon dioxide colloid (aerosil) - 0.600 mg.

Description:Round, biconvex tablets of white color.

Pharmacotherapeutic group:Analgesic narcotic drug

ATX: & nbsp

Buprenorphine

Pharmacodynamics:

Combined drug containing buprenorphine and naloxone. In sublingual administration, the pharmacological action is determined by the buprenorphine included in the formulation.

Buprenorphine

Buprenorphine is an opioid analgesic, a semisynthetic derivative of thebaine. It refers to partial agonists of the p-opioid receptor subtype and partial antagonists of c-opioid receptors. By the expression of analgesic action in equivalent doses is similar to morphine. As a partial agonist opioid receptor inhibits breathing, affects smooth muscle, although to a lesser extent than morphine and other opiates, has a lower potential for the development of physical dependence than it. At the same time, the activation of the μ-opioid receptors determines a certain addictive potential of the drug.

Naloxone

Naloxone is an antagonist of opioid receptors. Effectively eliminates or reduces the effects of opiates and opioids. Restores breathing, reduces sedative and euphoric effects. Can cause the "withdrawal" syndrome of opiates with their preliminary administration for analgesia or in addicted people using opioid analgesics. Pharmacological action develops only with parenteral (intravenous, intramuscular, subcutaneous) route of administration. With the sublingual route of administration, practically does not enter the systemic circulation and does not have an effect.

Pharmacodynamic effects are absent. Naloxone practically does not show pharmacological activity when taken orally, the ratio of the effectiveness of naloxone for oral and parenteral administration is 1:50.

The onset of buprenorphine after sublingual use of the drug Bupraxon occurs 30 minutes later. The maximum effect is observed after 3 hours.The duration of the analgesic action is 5 hours.

Pharmacokinetics:

Suction

Buprenorphine

With sublingual admission buprenorphine well absorbed. Systemic bioavailability is about 50-55%. The maximum concentration (C_mOh) in the blood plasma after taking 0.4 mg buprenorphine is achieved after 2 hours and averages 1.13 ng / ml.

Naloxone

With sublingual admission naloxone almost not absorbed. Systemic bioavailability is less than 5%. Concentrations in the blood plasma are not significant.

Distribution

Buprenorphine

Buprenorphine penetrates well through the blood-brain barrier. 96% bind to blood plasma proteins, primarily with α- and β-globulins. Volume of distribution (V_d) buprenorphine is 2.5 liters, which indicates its active capture by the organs of the body.

Naloxone

Naloxone binds to blood plasma proteins, mainly with albumin, by 45%.

Metabolism

Buprenorphine

Buprenorphine undergoes liver metabolism by N-dealkylation with the formation of norbuprenorphine with the participation of the CYP3A4 isoenzyme, followed by glucuronation, to form conjugates with glucuronic acid.The main metabolite, norbuprenorphine, does not have significant analgesic activity and is also subject to glucuronidation.

Naloxone

According to clinical studies naloxone has a low bioavailability (9 ± 6%) with sublingual administration. Absorbed insignificant amounts of naloxone included in Bupraxone® do not create therapeutic concentrations in the blood plasma and do not affect the effects and metabolism of buprenorphine.

Naloxone is rapidly metabolized in the liver, undergoing direct glucuronization to naloxone-3-glucuronide, and N-dealkylation and reduction (for the 6-oxo group).

Excretion

Buprenorphine

The half-life (T_1/2) of buprenorphine from the blood plasma is 24-42 hours. Excretion of metabolites is carried out by the kidneys (30%) and bile (69%). Only about 1% of the drug is excreted unchanged.

Naloxone

(T_1/2) of naloxone is 2-12 hours. Metabolites are excreted mainly by the kidneys.

Indications:

In patients with postoperative pain syndrome (strong and medium intensity), pain syndrome caused by trauma and burns, during diagnostic procedures.

Contraindications:

- Hypersensitivity to buprenorphine, naloxone and other components of the drug;

- conditions that can lead to a violation of breathing, or are already accompanied by depression of the respiratory center or severe depression of the central nervous system;

- simultaneous use with monoamine oxidase (MAO) inhibitors, both during the entire period of application of MAO inhibitors, and within 14 days after their cancellation (see the section "Interaction with other drugs");

- stomatitis and mucositis, ulcerative-necrotic and inflammatory lesions of the mucous membrane of the oral cavity;

- drug dependence, including opioid dependence;

- convulsive conditions;

- craniocerebral trauma;

- acute alcohol intoxication;

- bronchial asthma, asthmatic status;

- pulmonary heart failure;

- heart rhythm disturbances (supraventricular and ventricular paroxysmal tachycardia, atrial fibrillation and flutter, ventricular fibrillation and flutter, extrasystole);

- paralytic ileus;

- acute surgical diseases of the abdominal cavity before diagnosis;

- use during pregnancy and during breastfeeding;

- age to 18 years;

- lactose intolerance, lactase deficiency, glucose-galactose malabsorption (see section "Special instructions").

Carefully:

- Respiratory failure,

- hepatic and / or renal failure,

- myxedema,

- hypothyroidism,

- adrenal insufficiency,

- oppression of the central nervous system,

- toxic psychosis,

- hyperplasia of the prostate,

- stricture of the urethra,

- alcoholism,

- elderly and senile age.

Pregnancy and lactation:

The drug is contraindicated for use during pregnancy and during breastfeeding. Controlled studies of the use of sublingual Bupraxone® tablets were not performed. The potential risk to humans is unknown.

When using the drug at the end of pregnancy buprenorphine can cause respiratory depression in the newborn, even after a short period of use. Long-term use of buprenorphine during the last three months of pregnancy can cause abstinence syndrome in newborns (including hypertension, tremor, neonatal agitation, myoclonus, or convulsions). The syndrome, as a rule, can proceed from several hours to several days after childbirth.

Breast-feeding

It is not known whether the blood is excreted naloxone with breast milk. Buprenorphine and its metabolites are excreted from the body through the mother's milk.

In an animal study, in rats, buprenorphine was found to inhibit lactation. Therefore, breastfeeding should be discontinued for the duration of treatment with Bupraxone®.

Fertility

Studies in animals have shown a reduction in female fertility in doses many times greater than the average daily dose for humans.

Dosing and Administration:

The drug Bupraxone ® is applied sublingually. The tablets are held under the tongue until complete resorption.

The dose is selected individually. Duration of treatment and dose should be determined by a doctor.

A single dose for adults is 1 or 2 tablets. Repeated use of the drug in a similar dose is possible every 6-8 hours.

The maximum single dose is 2 tablets, the maximum daily dose is 8 tablets.

The dose of Bupraxone ® should be reduced in elderly patients, with hypovolemic conditions, at a risk of surgical pathology, while using sedatives and other narcotic analgesics.

The drug Bupraxone® in reduced doses should be used against the background of funds for general anesthesia, hypnotics, anxiolytics, antidepressants and antipsychotics to avoid excessive central nervous system depression and inhibition of respiratory center activity.

Side effects:

Information on the incidence of side effects is presented on the basis of data obtained during clinical trials and literature data.

Very Frequent	- 1/10 appointments	(≥ 10%)
Frequent	- 1/100 appointments	(≥ 1% but <10%)
Infrequent	- 1/1000 appointments	(≥ 0.1% but <1%)
Rare	- 1/10000 appointments	(≥ 0.01%, but <0.1%)
Very rare	- less than 1 / 10,000 assignments	(<0,01%)

Side effects of Bupraxone® are determined by the buprenorphine entering into it.

Allergic reactions: rarely: rash, hives.

From the central nervous system (CNS): very often sedation, often - weakness; rarely - confusion, drowsiness, weakness / fatigue, inhibition, slowing of the speed of mental and motor reactions, slurred speech, paresthesia, euphoria, nervousness, depression, psychosis.

With prolonged use, it is possible to develop addiction and opioid dependence.

From the nervous system: often - dizziness, headache; rarely - noise in the ears.

From the skin: rarely - cyanosis, itching.

From the urinary system: rarely - urinary retention.

From the side of metabolism: rarely - sweating.

From the digestive system: often - nausea; rarely - vomiting, dry mouth, constipation.

From the respiratory system: rarely - oppression of the respiratory center, dyspnea, hypoventilation.

From the sense organs: often - miosis, blurred vision, diplopia; very rarely - conjunctivitis.

From the side of the cardiovascular system: often - increased blood pressure, rarely - tachycardia, bradycardia, chills / sensation of cold, "hot flashes" of blood.

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

Overdose Symptoms are determined by the buprenorphine component. Symptoms: nausea, vomiting, sedation, drowsiness, miosis, respiratory depression.

Treatment: physical and verbal stimulation of the patient, symptomatic therapy.

Symptomatic therapy: oxygen, infusion therapy, parenteral administration of naloxone (a single intravenous or intramuscular injection of naloxone is recommended in a dose of 0.4-2 mg with repeats in 2-3 minutes, up to a total dose of 10 mg or more).Due to the high affinity of buprenorphine for opioid receptors, doses of naloxone are used that are higher than for morphine and other "complete opioid agonists". If necessary, auxiliary and artificial ventilation (IVL).

Interaction:

Potentiates the action of neuroleptics, benzodiazepines, phenothiazines, as well as other tranquilizers; anxiolytics, sedatives, hypnotics, general anesthetics, antihistamines, ethanol.

When combined with MAO inhibitors, malignant hyperthermia, convulsions, coma, arterial hypertension can develop.

When Buprakson ® is combined with "complete opioid agonists," the "opiate withdrawal" syndrome may develop.

When used with valproic acid / sodium valproate, the inhibitory effect on the central nervous system increases.

When taking other analgesics, the pressure of the cerebrospinal fluid may increase, so Bupraxone® should be used with caution in cases where the pressure of the cerebrospinal fluid can be increased, since buprenorphine can lead to miosis and a change in the level of consciousness.

Drugs that inhibit isoenzyme activity CYP3A4 (ketoconazole, macrolides, erythromycin and others) or HIV protease inhibitors (ritonavir) can enhance the effects and duration of buprenorphine, which will require a dose adjustment of one or both drugs.

When combined with isoenzyme inducers CYP3A4 (incl. phenobarbital, carbamazepine, phenytoin, rifampicin) the concentration of buprenorphine in the blood plasma can decrease. Since the interaction of buprenorphine with all isoenzyme inducers CYP3A4 has not been studied, it is recommended to monitor the condition of patients receiving Bupraxone®, sublingual tablets, for signs and symptoms of withdrawal syndrome.

Phytopreparations can influence the pharmacological activity of buprenorphine. Hypericum perforated, as isoenzyme inducer CYP3A4, is able to reduce the concentration of buprenorphine in the blood plasma.

Ethanol increases CNS depression by buprenorphine. For the period of treatment it is necessary to refuse alcoholic beverages.

Special instructions:

The inclusion of naloxone in the drug Buprakson ® is made with the goal of increasing narcological safety when using the latter.In the case of non-medical use of the tablets of Bupraxone® (due to the presence of a narcotic analgesic), naloxone will block the effects of buprenorphine and will not lead to an action, the achievement of which is pursued in the abuse of buprenorphine. In persons with physical dependence on opioids, this can lead to the development of the "withdrawal" syndrome.

Patients with hepatic insufficiency

Buprenorphine is metabolized in the liver. In patients with impaired liver function, the intensity and duration of action of the drug may vary. The use of sublingual tablets Bupraxone® in such patients should be controlled by a specialist.

Patients with renal insufficiency

The pharmacokinetics of buprenorphine in renal failure does not change.

Nicotine-dependent patients

It is necessary to warn patients that nicotine reduces the pharmacological activity of the drug.

Medicinal preparation Buprakson® in the auxiliaries contains lactose, which can have a clinically significant effect on persons with intolerance, having lactase deficiency, glucose-galactose malabsorption.

Keep out of the reach of children.In the event of accidental or deliberate admission, respiratory depression may occur in children, which can lead to death.

Effect on the ability to drive transp. cf. and fur:

During the treatment period it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Tablets sublingual.

Packaging:

10 tablets per contour cell pack.

1 or 2 contour packs with instructions for use in a pack of cardboard.

For 100, 200, 400 contour mesh packages together with an equal number of instructions for use in a cardboard box or in a box of corrugated cardboard (for hospital).

Storage conditions:

In accordance with the rules for the storage of narcotic drugs listed in List II of the List of Narcotic Drugs, Psychotropic Substances and Their Precursors Subject to Control in the Russian Federation.

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

4 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-003748

Date of registration:21.07.2016

Expiration Date:21.07.2021

The owner of the registration certificate:MOSCOW ENDOCRINE FACTORY, FSUE MOSCOW ENDOCRINE FACTORY, FSUE Russia

Manufacturer: & nbsp

MOSCOW ENDOCRINE FACTORY, FSUE Russia

Representation: & nbspMOSCOW ENDOCRINE FACTORY FGUP MOSCOW ENDOCRINE FACTORY FGUP Russia

Information update date: & nbsp12.03.2017

Illustrated instructions

Instructions

Bupraxon (Bupracson)