Ubretide - description of the drug, instructions for use, reviews

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Manufacturers: Nycomed Austria GmbH

Active ingredients

  • Distigmine bromide

Disease class

  • Dystonia
  • Myasthenia gravis and other neuromuscular junction disorders
  • Upper limb diplegia
  • Constipation
  • Megacolon, not elsewhere classified
  • Postoperative intestinal obstruction
  • Neurogenic bladder weakness, not elsewhere classified

Clinical and pharmacological group

  • Centrally acting cholinomimetics

Pharmacological action

  • Anticholinesterase

Pharmacological group

  • m-, n-cholinomimetics, incl. anticholinesterase drugs

Compound

Ritalin contains melifenidate and is available as regular tablets, film-coated tablets, extended-release tablets, and delayed-release capsules. The sale, transportation, storage or purchase of Ritalin on the territory of the Russian Federation is criminally punishable.

Methylphenidate is a piperidine derivative of amphetamine. In medications, the active substance is contained in the form of methylphenidate hydrochloride, an odorless white crystalline powder, easily soluble in water.

Mechanism of action

Ritalin is a powerful dopamine and norepinephrine reuptake inhibitor. Inhibiting the uptake of catecholamines by nerve cell terminals prevents their removal from the synaptic space.

Methylphenidate acts as an alpha and beta adrenergic receptor agonist:

  • at the presynaptic level enhances the release of norepinephrine and dopamine (indirect agonist)
  • at the postsynaptic level binds to adrenergic receptors (direct agonist)

Ritalin enhances the activity of the sympathetic nervous system by increasing the plasma concentration of norepinephrine. The drug increases the strength (positive inotropic effect) and frequency (positive chronotropic effect) of heart contractions, and also increases vascular tone. Systolic and diastolic blood pressure increase by an average of 5-20 mmHg.

Methylphenidate is well absorbed from the gastrointestinal tract. Already in the liver, the substance is actively metabolized; the bioavailability of the drug is 30%. Distribution in the central nervous system is largely due to passive diffusion. Methylphenidate is primarily removed by hydrolysis to ritalic acid. The half-life is approximately 3 hours. Metabolic products and unchanged active substance are excreted in the urine.

Publications in the media

(Distigmini bromidum) INN

Synonyms. Ubretid.

Composition and release form. Distigmine bromide tablets 0.5 mg; 0.05% solution in ampoules of 1 ml.

Indications. Prevention and treatment of postoperative intestinal atony and paralytic intestinal obstruction; atony of the bladder and ureters; atonic and hypotonic constipation; megacolon; peripheral skeletal muscle paralysis; myasthenia gravis. Pharmachologic effect. Distigmine bromide reversibly blocks acetylcholinesterase, an enzyme that destroys acetylcholine, which leads to the accumulation of acetylcholine in the endings of cholinergic nerves and an increase in its action. As a result, the tone and peristalsis of the gastrointestinal tract, bladder, and ureters increase; the tone and contraction of skeletal muscles increases.

Pharmacokinetics.

Side effects. Gastrointestinal spasms, bronchospasm, diarrhea, nausea, bradycardia, hypersalivation.

Contraindications. Hypersensitivity to the drug, hypersensitivity to bromine; bronchial asthma; thyrotoxicosis; hypervagotonia; hypertonicity of the intestines, biliary and urinary tracts; hypotension; epilepsy; stomach ulcer; chronic heart failure, post-infarction period; postoperative and hemodynamic shock; Parkinson's disease.

Adverse reactions when interacting with other drugs. The effect of the drug is reduced by m-cholinergic blockers, antihistamines, psychotropic drugs that have an anticholinergic component in the spectrum of action, corticosteroids and aminoglycoside antibiotics. When using cimetidine, the effect of distigmine bromide may be increased.

Information for the patient. The drug is prescribed orally at a dose of 5 mg per day in the morning 30-40 minutes before breakfast. For intramuscular administration, a single dose is 0.5 mg. Repeated administration of the drug should not be carried out earlier than after 24 hours. It is unacceptable to double the missed dose due to the risk of overdose. Signs of an overdose may include nausea, diarrhea, blurred vision, increased salivation and sweating, bronchospasm; in this case, it is necessary to administer atropine intravenously and subcutaneously at a dose of 0.5-1 mg. With functional amenorrhea, the drug can cause menstrual-like bleeding. During treatment you should refrain from driving a car, because distigmine bromide reduces the speed of physical and mental reactions.

Indications for use

Ritalin is used to treat attention deficit hyperactivity disorder (ADHD), narcolepsy, and primary hypersomnia. Methylphenidate should be prescribed for ADHD as part of complex therapy.

Lack of attention, hyperactivity and impulsivity are the three main signs of ADHD. This diagnosis is labor-intensive, complex and requires appropriate clinical experience. It involves an in-depth examination of the patient's medical history.

Symptoms must persist for more than 6 months and be observed for up to 7 years. The main diagnostic difficulty is based on the fact that symptoms are nonspecific and can have a variety of causes.

According to studies, the prevalence of ADHD is about 5% and narcolepsy is about 1%. ADHD is more common among younger men and those of low socioeconomic status. Symptoms of the disease are more common in adolescence and adulthood. Approximately 40-86% of men experience persistent symptoms of ADHD.

Available research suggests that methylphenidate can be meaningfully used for attention deficit hyperactivity disorder in children and adolescents, typically as part of multimodal therapy. A prerequisite is an adequate diagnosis of ADHD, narcolepsy or hypersomnia.

Ubretide instructions for use

INSTRUCTIONS for using the product

Ubretid

Release form

Tablets, ampoules

Pharmacological properties

Ubretide (distigmine bromide) is a long-acting inhibitor of acetylcholinesterase and pseudocholinesterase. Has a longer lasting effect than neostigmine. Ubretide has an indirect cholinomimetic effect due to reversible inhibition of cholinesterase and potentiation of the action of endogenous acetylcholine. Leads to the accumulation of acetylcholine in the synaptic cleft. Ubretide improves neuromuscular transmission, increases intestinal tone and motility, increases the tone of the bladder, bronchi, and the secretion of exocrine glands. Acts on the cardiovascular system: has a moderately pronounced vasodilator and negative chronotropic effect (causes bradycardia, lowers blood pressure). Ubretide increases the tone of skeletal muscles, especially in myasthenia gravis (a noticeable effect appears on the 1st–2nd day of administration). Constricts the pupil, lowers intraocular pressure, and causes a spasm of accommodation. Ubretide does not affect the neurotransmitter acetylcholine in the central nervous system. It also does not have a significant effect on the transmission of impulses in the ganglia of the autonomic nervous system. The clinical effect develops within 1–1.5 hours after oral administration. The increase in gastrointestinal tone reaches a maximum after 8–10 hours and persists for 20 hours.

Indications

Ubretide is recommended for use in the postoperative period for intestinal atony.

The medication is effective in the treatment of constipation caused by intestinal atony, megacolon and paralytic obstruction.

The high effectiveness of the drug is used for reduced tone and atony of the bladder, ureters, and functional abnormalities of the bladder sphincter.

Ubretide is indicated for myasthenia gravis and paralysis of the skeletal muscles of the limbs.

Contraindications

Ubretide should not be used by people allergic to bromine or the components of the drug.

The drug is contraindicated in case of increased tone of the intestines, biliary and urinary tracts, epilepsy, stomach and intestinal ulcers, enteritis, colitis, increased salivation, Parkinson's disease, increased acidity of gastric juice, arterial hypotension, bronchial asthma, bradycardia, myocardial infarction, circulatory disorders, thyrotoxicosis, iritis, myotonia and tetany.

Ubretide should not be used during the period of postoperative shock and intestinal obstruction of any etiology except paralytic.

Use during pregnancy and breastfeeding

Ubretide is strictly contraindicated during pregnancy and lactation.

Compound

The basis of the injection solution is distigmine bromide, the additional components are sodium chloride and water for injection.

Ubretide tablets are made on the basis of distigmine bromide using talc, corn starch, glucose and magnesium stearate.

Directions for use and doses

This drug Ubretide is used orally, on an empty stomach, 30 minutes before the morning meal.

The initial dosage is 1 tablet (5 mg) per day. If there is no reaction from the body, then you cannot take the drug on the same day, as this can cause uncontrolled cumulation.

Subsequent changes in dosage are determined by the attending physician, depending on the dynamics of treatment and the body’s response to the drug. If necessary, the dosage can be increased to 2 tablets per day or reduced to 1 tablet, which is taken every other day or every 3 days.

The duration of the treatment course is determined individually, depending on the severity of the disease and other indications of the body’s functioning.

Side effects

Side effects that may occur after taking this drug include:

- nausea, vomiting, diarrhea, intestinal spasms;

- increased gastric or intestinal motility;

- bronchospasms (if the patient suffers from bronchial asthma);

- bradycardia;

- constriction of the pupil;

- increased sweating;

- muscle spasms, tremors, muscle weakness;

- difficulty swallowing.

- vaginal bleeding.

Interaction with other drugs

The effect is weakened by anticholinergic (atropine), psychotropic, antihistamine, curare-like drugs, aminoglycosides (have a weak muscle relaxant effect).

Overdose

Symptoms associated with the cholinomimetic effect - nausea, vomiting, diarrhea, abdominal pain, bronchospasm, bradycardia, miosis, heavy sweating, etc. Treatment - atropine is administered intravenously or subcutaneously at a dose of 0.5–1 mg.

Storage conditions

In a place protected from light, at a temperature of 15–25 °C.

Best before date

No more than 5 years

Use as a drug

Being essentially a psychostimulant, methylphenidate is used among drug addicts to obtain euphoric sensations. To do this, the dosage of the drug is exceeded 2-3 times. In some ways, its effects are comparable to those of cocaine or methamphetamine, but are more reminiscent of Prozac or Zoloft. As the dosage increases, the likelihood of not only psychological but also physical addiction increases. Regular abuse is fraught with psychosis, insomnia and disruption of the functioning of all internal organs.

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** The Drug Directory is intended for informational purposes only. For more complete information, please refer to the manufacturer's instructions. Do not self-medicate; Before starting to use Ubretide, you should consult a doctor. EUROLAB is not responsible for the consequences caused by the use of information posted on the portal. Any information on the site does not replace medical advice and cannot serve as a guarantee of the positive effect of the drug.

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** Attention! The information presented in this medication guide is intended for medical professionals and should not be used as a basis for self-medication. The description of the drug Ubretide is provided for informational purposes and is not intended for prescribing treatment without the participation of a doctor. Patients need to consult a specialist!

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