Bupralal® (Bupranal)

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: & nbsp
    injection
    Composition:
    1 ml of the solution contains:
    Active substance:
    Buprenorphine hydrochloride 0.324 mg
    (in terms of buprenorphine) 0.3 mg
    Excipients:
    dextrose monohydrate (in terms of anhydrous) - 50.00 mg
    water for injection - up to 1 ml
    Description:Transparent colorless or slightly colored liquid.
    Pharmacotherapeutic group:Analgesic drug: an opioid receptor agonist-antagonist
    ATX: & nbsp

    N.07.B.C.01   Buprenorphine

    Pharmacodynamics:Narcotic analgesic, a partial (partial) agonist of mu-opioid receptors that binds firmly to them, and a partial antagonist of kappa-opioid receptors. The pharmacological effect exceeds morphine (0.3 mg of buprenorphine is equivalent to 10 mg of morphine). Activates the antinociceptive system and, thus, disrupts the interneuronal transmission of pain impulses at various levels of the central nervous system, and also changes the emotional color of the pain, affecting the higher parts of the brain. Has low narcogenic potential.
    It inhibits conditioned reflexes, causes euphoria,has a mild hypnotic effect, a central antitussive effect, excites a vomiting center, by the ability to depress respiration is equal to morphine, causes a narrowing of the pupil due to activation of the oculomotor nerve, increases the tone of the center of the vagus nerve, bronchi and smooth muscle sphincters of internal organs (intestine, bile ducts, bladder) , weakens the peristalsis of the intestine, inhibits the secretory activity of the glands of the gastrointestinal tract. In terms of development of drug dependence for long-term use is less dangerous than morphine.
    The onset of action after intravenous administration is 15 minutes, after intramuscular injection, 30 minutes. The maximum effect develops after 1-2 hours. The duration of analgesic action is 6-8 hours (more than morphine).
    Pharmacokinetics:96% of buprenorphine binds to blood plasma proteins (predominantly with alpha and beta globulins). Evenly distributed in tissues, it penetrates the blood-brain barrier.
    Metabolised in the liver by N-dealkylation with the participation of the CYP3A4 isoenzyme to form a pharmacologically active metabolite - norbuprenorphine.Part unaltered buprenorphine and active metabolite undergoes glucuronidation. The half-life is 3-6 hours.
    Excreted in the bile 69% (33% - unchanged - 5% as glucuronide; 21% - as norbuprenorfina and 2% - as its glucuronide) and kidneys 30% (1% - unchanged and 9 4% - as glucuronide; 2.7% - in the form norbuprenorfina and 11% - as its glucuronide).
    Indications:
    It is used as an anesthetic in patients with severe pain syndrome traumatic origin, burns, preoperative, operative and postoperative periods, in myocardial infarction, severe attacks of angina, pain at malignancies and other conditions involving severe pain.
    Contraindications:
    - Hypersensitivity to the drug,
    - drug dependence, including opioid dependence,
    - conditions accompanied by respiratory depression or severe depression of the central nervous system,
    - convulsive conditions,
    - craniocerebral injury,
    - Acute alcohol intoxication,
    - bronchial asthma, asthmatic status,
    - pulmonary heart failure,
    - cardiac arrhythmias (paroxysmal tachycardia, suprarenal, ventricular, atrial fibrillation and flutter, ventricular fibrillation and flutter, extrasystoles),
    - paralytic ileus,
    - acute surgical diseases of the abdominal cavity until diagnosis,
    - age to 18 years,
    - Do not apply Bupralal® against treatment with monoamine oxidase inhibitors and for another 14 days after they are discontinued.
    Carefully:
    - respiratory insufficiency,
    - hepatic and / or renal failure,
    - myxedema,
    - hypothyroidism,
    - adrenal insufficiency,
    - depression of the central nervous system,
    - Toxic psychosis,
    - hyperplasia of the prostate,
    - strictures of the urethra,
    - alcoholism,
    - elderly and senile age.
    Pregnancy and lactation:
    Contraindicated the use of Bupralal® during pregnancy and during breastfeeding.
    Dosing and Administration:The drug Bupranal® 0.3 mg / ml in syringe tubes is injected intramuscularly, in ampoules intramuscularly or intravenously slowly in 1-2 ml. If necessary, repeat the drug every 6-8 hours. The highest daily dose is 2.4 mg.
    Under careful supervision and in reduced doses, Bupranal® should be used against the background of agents for general anesthesia, hypnotics, anxiolytics, antidepressants and antipsychotics to avoid excessive central nervous system depression and inhibition of respiratory center activity.
    The dose of the drug should be reduced in older patients, with hypovolemic conditions, at the risk of surgical pathology, while using sedatives and other narcotic analgesics.
    Duration of treatment and dosage are determined by the doctor individually for each patient, depending on the type, causes and characteristics of the pain syndrome.
    Side effects:
    From the nervous system: sedation, dizziness; headache; confusion, inhibition, euphoria, weakness, nervousness, depression, agitation, anxiety, drowsiness, slowing of the speed of mental and motor reactions.
    From the cardiovascular system: lowering blood pressure; increased blood pressure, tachycardia, bradycardia.
    From the respiratory system: hypoventilation, dyspnea, oppression of the respiratory center.
    From the gastrointestinal tract: nausea; vomiting, dry mouth, constipation.
    From the genitourinary system: delayed urination, decreased erection.
    Allergic reactions: skin rash, itching.
    Other: sweating, miosis; diplopia, a feeling of heat, chills.
    With long-term use of the drug Bupranal®, it is possible to develop addiction (weakening of the analgesic effect) and opioid dependence.
    Overdose:Symptoms: nausea, vomiting, drowsiness, pronounced miosis (with significant hypoxia - mydriasis), lowering of arterial pressure, hypothermia, respiratory depression (until it stops), stupor, coma.
    Treatment: naloxone in a dose of 0.4-2 mg. If the application in this dose does not bring the expected effect, the administration in the same dose is repeated after 2-3 minutes. The introduction of naloxone, even in high doses, does not always lead to the restoration of adequate breathing, in this regard, carry out activities aimed at maintaining adequate pulmonary ventilation and cardiovascular activity. If necessary, conduct symptomatic therapy.
    Interaction:Strengthens the depressing effect on the central nervous system and the breathing of other narcotic analgesics, means for general anesthesia, hypnotics, sedatives, antipsychotic, bloggers H1-gistaminovyh receptors with the central component of the action, anxiolytics, antidepressants, ethanol, monoamine oxidase inhibitors. Simultaneous use with monoamine-sidase inhibitors is contraindicated.
    Naloxone prevents the inhibitory effect of Bupralan® on breathing, but does not always effectively eliminate the already developed effect, even at high doses.
    The drug should not be combined with narcotic analgesics from the agonist group (morphine, trimeridine, fentanyl) and antagonist agonists (nalboufine, butorphanol) opioid receptors because of the danger of weakening analgesia and the possibility of provoking a withdrawal syndrome in patients with opioid dependence.
    May cause abstinence syndrome in patients with drug dependence to complete agonists of mu-opioid receptors (morphine, heroin, trimeridine, fentanyl).
    Inhibitors of the isoenzyme CYP3A4 (ritonavir, fluconazole and others) increase the activity of buprenorphine. Inductors of the isoenzyme CYP3A4 (ketoconazole, loperamide and others) reduce the pharmacological activity of the drug.
    Special instructions:

    For anesthesia during childbirth is not used because of the low effectiveness of naloxone in the case of respiratory depression in the newborn.
    It is not recommended to apply for short (less than 3 hours) surgical interventions.
    During the treatment period, one should refrain from driving motor vehicles and practicing other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
    Care should be taken when prescribing the drug to patients with craniocerebral trauma accompanied by cerebrospinal hypertension; with increased intracranial pressure; with violation of respiratory function; with severe pulmonary insufficiency; impaired liver and kidney function; myxedema or hypothyroidism; adrenal insufficiency; depression of the central nervous system. Individual dose selection is also necessary in patients with prostatic hypertrophy, urethral stricture.

    Form release / dosage:
    Solution for injection 0.3 mg / ml in ampoules of 1 ml.
    Solution for injection 0.3 mg / ml in syringe tubes of 1 ml (cm3).
    Packaging:Ampoules:
    5 ampoules per circuit cell packaging made of polyvinylchloride film and aluminum foil; 1 or 2 contour squares with instructions for use, a scarifier or a knife ampoule in a pack of cardboard.
    20, 50 or 100 contour mesh packages, with instructions for use (by the number of contoured cell packs), scarifiers or knives, ampoule into carton boxes or corrugated cardboard boxes (for hospitals).
    When packing ampoules with notches, rings, break points, scarifiers or ampoule knives do not.
    Syringe Tubes:
    By 20, 50, 100 syringes-tubes with instruction on the use of the preparation and instruction on the use of a syringe-tube in a box of cardboard (for completing first-aid kits of servicemen of the Armed Forces, MES, MIA).
    Storage conditions:
    List II "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 for the drug in ampoules, in a dark place at a temperature of no higher than 15 ° C for the drug in syringe tubes.
    Keep out of the reach of children.
    Shelf life:
    4 years (for the drug in ampoules).
    2 years (for the drug in syringe tubes).
    Terms of leave from pharmacies:On prescription
    Registration number:P N002817 / 01
    Date of registration:14.08.2008 / 02.02.2017
    Expiration Date:Unlimited
    The owner of the registration certificate:MOSCOW ENDOCRINE FACTORY, FSUE MOSCOW ENDOCRINE FACTORY, FSUE Russia
    Manufacturer: & nbsp
    Information update date: & nbsp12.03.2017
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