Pagluferal 2, pills, 20pcs

Composition

Composition per tablet

Pharmacological action

Combined antiepileptic drug. Phenobarbital interacts with the “barbiturate” site of the benzodiazepine-GABA receptor complex, thereby increasing the sensitivity of GABA receptors to GABA, leading to the opening of neuronal channels for chlorine ions, which leads to an increase in their entry into the cell. Reduces the excitability of epileptogenic focus neurons and the spread of nerve impulses. It shows antagonism towards a number of excitatory mediators (glutamate, etc. ). It suppresses the sensory areas of the cerebral cortex, reduces motor activity, and inhibits cerebral functions, including the respiratory center. Reduces the smooth muscle tone of the gastrointestinal tract. It has anticonvulsant, sedative, hypnotic and antispasmodic effects. Caffeine-increases the reflex excitability of the spinal cord, excites the respiratory and vasomotor centers, and stimulates metabolic processes in organs and tissues, including muscle tissue and the central nervous system. Papaverine hydrochloride is an antispasmodic agent that has a hypotensive effect. Reduces the tone and relaxes the smooth muscles of internal organs and blood vessels. Calcium gluconate-makes up for the lack of calcium ions necessary for the transmission of nerve impulses. Bromizoval has a sedative and moderate hypnotic effect. Pharmacokinetics of Phenobarbital:  it is absorbed slowly and completely. The maximum concentration in the blood plasma is determined after 1-2 hours, the connection with plasma proteins is 50%. It is metabolized in the liver, induces microsomal liver enzymes CYP3A4, CYP3A5, and CYP3A7 (the rate of enzymatic reactions increases 10-12 times). It accumulates in the body. The elimination half-life is 2-4 days. It is excreted by the kidneys in the form of glucuronide, about 25% – unchanged. Penetrates into breast milk and through the placental barrier. Caffeine:  absorption – good, occurs throughout the intestine. The maximum concentration in the blood plasma is reached after 50-75 minutes. It is rapidly distributed in all organs and tissues, penetrates the blood-brain barrier and the placenta. The relationship with blood proteins (albumins) is 25-36%. Metabolism in the liver is more than 90%, in children of the first years of life up to 10-15%. In adults, about 80% of the caffeine dose is metabolized to paraxanthin, about 10% to theobromine, and about 4% to theophylline. These compounds are subsequently demethylated to monomethylxanthines, and then to methylated uric acids. The half-life in adults is 3.9-5.3 hours (sometimes up to 10 hours). The elimination of caffeine and its metabolites is carried out by the kidneys. Papaverine:  the average bioavailability is 54%. Plasma protein binding is 90%. It is well distributed and penetrates through histohematic barriers. It is metabolized in the liver. The half-life is 0.5-2 hours (can be extended up to 24 hours). It is excreted by the kidneys in the form of metabolites. Calcium Gluconate:  approximately 1/5-1/3 of it is absorbed in the small intestine. About 20% is excreted by the kidneys, the remaining amount is removed with the contents of the intestine (actively released by the wall of the terminal gastrointestinal tract).

Indications

Epilepsy.

Contraindications

Hypersensitivity to any of the components of the drug, severe hepatic and/or renal insufficiency, drug dependence (including in the anamnesis), hyperkinesis, myasthenia gravis, severe anemia, porphyria, diabetes mellitus, adrenal hypofunction, hyperthyroidism, depression, bronchial obstructive diseases, active alcoholism, pregnancy, lactation.

This dosage form is not used in children under 3 years of age.

With caution:  in debilitated patients (high risk of paradoxical arousal, depression, and confusion, even at normal doses).

Side effects

Dizziness, general weakness, ataxia, dysarthria, nystagmus, paradoxical reaction (especially in elderly and debilitated patients – agitation), hallucinations, sleep disorders, nausea, vomiting, constipation or diarrhea, increased activity of hepatic transaminases, agranulocytosis, megaloblastic anemia, thrombocytopenia, decreased or increased blood pressure, tachycardia, arrhythmia (including extrasystole), atrioventricular arrhythmia blockade, allergic reactions, with prolonged use – drug dependence.

Interaction

Phenytoin and valproates increase the content of phenobarbital in the blood serum. The effect of phenobarbital decreases when taken simultaneously with reserpine, increases when combined with amitriptyline, nialamide, diazepam, chlordiazepoxide. Reduces the effectiveness of oral contraceptives and salicylates. Reduces the blood content of indirect anticoagulants, glucocorticosteroids, griseofulvin, doxycycline, estrogens and other drugs that are metabolized in the liver by oxidation (accelerates their metabolism). Increases the effect of alcohol, neuroleptics, narcotic analgesics, muscle relaxants, sedatives and sleeping pills. Acetazolamide, by alkalizing the urine, reduces the reabsorption of phenobarbital in the kidneys and weakens its effect. Reduces the antibacterial activity of antibiotics and sulfonamides, the antifungal effect of griseofulvin.

How to take, course of use and dosage

Inside after eating. Children: 3-4 years – 1 tablet 2 times a day,5-6 years-1.5 tablets 2 times a day,7-9 years-2 tablets 2 times a day,10-14 years-2.5 tablets 2 times a day. Children from 14 years of age and adults: 4 tablets 2 times a day.

Overdose

Symptoms: increased severity of side effects. Treatment: gastric lavage, taking activated charcoal, symptomatic therapy.

Special instructions

Patients with minor hypercalciuria, reduced glomerular filtration rate, or a history of nephrolithiasis should be prescribed the drug under the control of the content of calcium in the urine, which is due to the presence of calcium gluconate in the drug. During treatment, you should refrain from performing work that requires rapid psychomotor reactions (including driving a car). Alcohol consumption is not recommended during therapy.

Storage conditions

List B. Store in a dry place protected from light and out of reach of children at temperatures above 25 °C. Keep out of reach of children

Shelf

life is 2 years.

Active ingredients

: Calcium Gluconate, Bromizoval, Caffeine, Papaverine, Phenobarbital

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Description

For adults as prescribed by a doctor, Children over 3 years of age, Children as prescribed by a doctor

Indications

Epilepsy