Bellataminal, tablets 30 pcs

Migraine, Headache

Indications

In the complex therapy of vegetative-vascular dystonia, accompanied by increased irritability, insomnia, headache, including menopausal syndrome; to relieve itching in neurodermatitis.

Pharmacological effect

Pharmacotherapeutic group: Sedative

ATC: N05CB02 Barbiturates in combination with other drugs
Pharmacodynamics:

Bellataminal® is a combination drug. It has α-adrenergic blocking, m-anticholinergic and sedative effects, and has antispasmodic properties. The drug reduces the excitability of the central and peripheral adrenergic and cholinergic systems of the body, has a calming effect on the central nervous system (CNS), and has some antispasmodic effects.

The pharmacological properties of the drug are determined by the action of the components included in its composition.

Belladonna’s sum of alkaloids (alkaloids of the atropine group) has an m-anticholinergic and antispasmodic effect. Interferes with the stimulating effect of acetylcholine; reduces the secretion of salivary, gastric, bronchial, lacrimal, sweat glands, exocrine function of the pancreas. Reduces the tone of the muscles of the gastrointestinal tract, bile ducts and gallbladder, but increases the tone of the sphincters; causes tachycardia, improves atrioventricular conduction. Dilates the pupils, impedes the outflow of intraocular fluid, increases intraocular pressure, causes paralysis of accommodation, etc.

Phenobarbital belongs to the group of barbiturates. It interacts with the barbiturate site of the benzodiazepine-γ-aminobutyric acid receptor complex, thereby increasing the sensitivity of γ-aminobutyric acid receptors to γ-aminobutyric acid, leading to the opening of neuronal channels for chloride ions, which leads to an increase in their entry into the cell.

Suppresses the sensory zones of the cerebral cortex, reduces motor activity, and inhibits cerebral functions, including the respiratory center. Reduces the tone of the smooth muscles of the gastrointestinal tract. Has a sedative effect.

Ergotamine is an ergot alkaloid. Affects various organs and systems of the body, incl. on the central nervous system; increases the tone of the uterus. It has been established that ergotamine is characterized by α-adrenergic blocking activity in combination with a pronounced direct vasoconstrictor effect on the smooth muscles of peripheral and cerebral vessels.

In this regard, against the background of the action of ergotamine, despite its α-adrenergic blocking activity, the tonic effect on peripheral vessels and cerebral vessels predominates. It has a direct stimulating effect on the smooth muscles of the vessels of the skull, causing their constriction due to binding to 5-HT1-serotonin receptors, which leads to their activation.

Pharmacokinetics:

Pharmacokinetic studies of the combination drug have not been conducted.

Belladonna, the sum of alkaloids, contains a complex of biologically active substances, and therefore pharmacokinetic studies are not possible.

When taken orally, phenobarbital is completely, but relatively slowly, absorbed. The maximum concentration in the blood is observed 1-2 hours after administration. About 50% binds to plasma proteins. Phenobarbital is evenly distributed in different organs and tissues; lower concentrations are found in brain tissue.

Metabolized in the liver, induces microsomal liver enzymes: isoenzymes CYP3A4, CYP3A5, CYP3A7 (the rate of enzymatic reactions increases 10-12 times), increases the detoxification function of the liver.

Cumulates in the body. The half-life (T1/2) is 2-4 days.

It is excreted by the kidneys in the form of glucuronide, 25% unchanged. Penetrates well into breast milk and through the placental barrier.

Ergotamine after oral administration is slightly absorbed from the gastrointestinal tract. Bioavailability is low due to intensive metabolism during the “first pass” through the liver. The maximum concentration of ergotamine in the blood plasma is achieved 50-70 minutes after oral administration, 90% of ergotamine is metabolized in the liver. T1/2 is 2 hours. The main metabolites (some of them are active) are excreted in the bile. About 4% is excreted unchanged by the kidneys.

Special instructions

The drug should not be used for more than 4 weeks without a doctor’s recommendation due to the risk of developing drug dependence on phenobarbital.

Impact on the ability to drive vehicles. Wed and fur.:

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Active ingredient

Belladonna alkaloids, Phenobarbital, Ergotamine

Composition

Active substances:
Belladonna total alkaloids – 0.0001 g (calculated as 100% substance)
Phenobarbital – 0.0200 g
Ergotamine tartrate – 0.0003 g (calculated as 100% substance)
Excipients (core):
Sucrose – 0.0535 g (refined sugar or granulated sugar)
Potato starch – 0.0244 g based on 97% substance
Povidone – 0.0007 g (polyvinylpyrrolidone) low molecular weight medical 12600 ± 2700
Calcium stearate – 0.0 010 g
Tablet core weight – 0.1 g

Excipients (shell):
Sucrose – 0.0605831 g (refined sugar or granulated sugar)
Colloidal silicon dioxide – 0.000620 g (Aerosil A-380)
Magnesium hydroxycarbonate – 0.010900 g (magnesium carbonate main)
Titanium dioxide – 0.000620 g (titanium dioxide)
Gelatin – 0.000274 g
Beeswax – 0.000030 g
Tropeolin 0 – 0.0000029 g
Weight of coated tablet – 0.173 g

Contraindications

Hypersensitivity to the components of the drug. Angina and other severe manifestations of atherosclerosis, spasm of peripheral arteries, angle-closure glaucoma, pregnancy, breastfeeding, childbirth, age under 18 years.

Side Effects

Allergic reactions, dry mouth, drowsiness, accommodation paresis.

Interaction

The effect of the drug is enhanced by alpha and beta adrenergic stimulants and nicotine.

Overdose

Symptoms of overdose: dizziness, lethargy, drowsiness, tachycardia, dilated pupils, impaired accommodation, difficulty urinating, intestinal atony, convulsions, in severe cases, stupor, coma.

First aid: gastric lavage, taking activated carbon, carrying out symptomatic therapy.

Storage conditions

In a dry place, at a temperature not exceeding 25 °C. List B.

Keep out of the reach of children.

Shelf life

5 years. Do not use after expiration date.

Manufacturer

Pharmcenter VILAR JSC, Russia