Composition, form of production and packaging
Pagluferal В® -1
Tablets of white color with a facet and a risk in the middle.
1 tab.
phenobarbital 25 mg
brominated with 100 mg
caffeine sodium benzoate 7.5 mg
papaverine hydrochloride 15 mg
calcium gluconate 250 mg
Auxiliary substances: potato starch, calcium stearate.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
PagluferalВ® -2
Tablets of white color with a facet and a risk in the middle.
1 tab.
Phenobarbital 35 mg
brominated with 100 mg
caffeine sodium benzoate 7.5 mg
papaverine hydrochloride 15 mg
calcium gluconate 250 mg
Auxiliary substances: potato starch, calcium stearate.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
Pagluferal В® -3
Tablets of white color with a facet and a risk in the middle.
1 tab.
Phenobarbital 50 mg
brominated with 150 mg
caffeine sodium benzoate 10 mg
papaverine hydrochloride 20 mg
calcium gluconate 250 mg
Auxiliary substances: potato starch, calcium stearate.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2013.
PHARMACHOLOGIC EFFECT
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 chloride ions, which leads to an increase in their entry into the cell. Reduces excitability neurons of the epileptogenic focus and the spread of nerve impulses. It shows antagonism towards number of stimulating mediators (glutamate and others). Suppresses the sensory areas of the cerebral cortex, reduces motor activity, depresses the cerebral function, incl. respiratory center. Reduces the tone of smooth muscles of the gastrointestinal tract. Has anticonvulsant, sedative, hypnotic and antispasmodic effect.
Caffeine increases the reflex excitability of the spinal cord, excites the respiratory and vasomotor centers, stimulates metabolic processes in organs and tissues, incl. in muscle tissue and in the central nervous system.
Papaverine hydrochloride is an antispasmodic, has an antihypertensive effect. Reduces the tone and relaxes the smooth muscles of the internal organs and vessels.
Calcium gluconate replenishes the deficiency of calcium ions needed to carry out the process of transmission of nerve impulses.
Bromizoval has a sedative and moderate hypnotic effect.
PHARMACOKINETICS
Phenobarbital: absorbed slowly, completely. C max in blood plasma is determined after 1-2 hours, communication with plasma proteins - 50%. Metabolized in the liver, induces microsomal liver enzymes CYP3A4, CYP3A5, CYP3A7 (the rate of enzymatic reactions increases 10-12 times). Cumulates in the body. T 1/2 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 is good, occurs throughout the intestine. C max in blood plasma is achieved after 50-75 minutes. Rapidly distributed in all organs and tissues, it penetrates through the BBB and the placenta. Communication 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 dose of caffeine is metabolized and paraxanthin, about 10% - in theobromine and about 4% - in theophylline. These compounds are subsequently demethylated into monomethylxanthines, and then into methylated uric acids. T 1/2 in adults - 3.9-5.3 hours (sometimes up to 10 hours). The excretion of caffeine and its metabolites is carried out by the kidneys.
Papaverine: bioavailability on average - 54%. The connection with plasma proteins is 90%. It is well distributed, penetrates through histogemagic berries. Metabolised in the liver. T 1/2 - 0.5-2 hours (can extend up to 24 hours). It is excreted by the kidneys in the form of metabolites.
Calcium gluconate: approximately 1 / 5-1 / 3 part is absorbed into the small intestine. About 20% is excreted by the kidneys, the rest is removed from the intestinal contents (actively allocated by the wall of the terminal GIT).
INDICATIONS
- Epilepsy.
DOSING MODE
The drug is taken orally after a meal.
Paglyuferal В® -1 is prescribed for children aged 3-4 years - 1 tab. 2 times / day; children aged 5-6 years - 1.5 tab. 2 times / day; children aged 7-9 years - 2 tab. 2 times / day; children aged 10-14 years - 3 tab. 2 times / day; children from 14 years and adults - 4 tab. 2 times / day.
Paglyuferal В® -2 is prescribed for children aged 3-4 years - 1 tab. 2 times / day; children aged 5-6 years - 1.5 tab. 2 times / day; children aged 7-9 years - 2 tab. 2 times / day; children aged 10-14 years - 2.5 tab. 2 times / day; children from 14 years and adults - 4 tab. 2 times / day.
Paglyuferal В® -3 is prescribed for children aged 7-9 years - 1 tab. 2 times / day; children aged 10-14 years - 1.5 tab. 2 times / day; children from 14 years and adults - 2 tab. 2 times / day.
SIDE EFFECT
From the side of the nervous system: dizziness, general weakness, ataxia, dysarthria, nystagmus, paradoxical reaction (especially in elderly and weakened patients - agitation), hallucinations, sleep disturbances.
On the part of the digestive system: nausea, vomiting, constipation or diarrhea, increased activity of hepatic transaminases.
From the hematopoietic system: agranulocytosis, megaloblastic anemia, thrombocytopenia.
From the cardiovascular system: a decrease or increase in blood pressure, tachycardia, arrhythmia (including extrasystole), AV-blockade.
Other: allergic reactions, with prolonged use - drug dependence.
CONTRAINDICATIONS
- marked hepatic and / or renal insufficiency;
- drug dependence (including in history);
- hyperkinesis;
- Myasthenia gravis;
- severe anemia;
- porphyria;
- diabetes;
hypofunction of the adrenal glands;
- hyperthyroidism;
- Depression;
- bronchoobstructive diseases;
- active alcoholism;
- Pregnancy;
- lactation period;
- hypersensitivity to any of the components of the drug.
This dosage form is not used in children under 3 years of age.
With caution should be used in patients with weakened patients (high risk of paradoxical arousal, depression and confusion even when prescribed in usual doses).
PREGNANCY AND LACTATION
The drug is contraindicated for use in pregnancy and lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in severe renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe hepatic insufficiency.
APPLICATION FOR CHILDREN
This dosage form is not used in children under 3 years of age.
SPECIAL INSTRUCTIONS
Patients with minor hypercalciuria, reduced glomerular filtration, or with nephrolithiasis in the history of the drug should be administered under the control of calcium in the urine, which is due to the presence of calcium gluconate in the drug.
Against therapy, alcohol is not recommended.
Impact on the ability to drive vehicles and manage mechanisms
During treatment should refrain from performing work that requires speed of psychomotor reactions (including driving).
OVERDOSE
Symptoms: increased severity of side effects.
Treatment: gastric lavage, reception of activated charcoal, symptomatic therapy.
DRUG INTERACTION
Phenytoin and valproate increase the content of phenobarbital in the blood serum.
The effect of phenobarbital decreases with simultaneous administration with reserpine, increases when combined with amitriptyline, nialamide, diazepam, chlordiazepoxide.
Reduces the effectiveness of oral contraceptives and salicylates.
Reduces the blood levels of indirect anticoagulants, GCS, griseofulvin, doxycycline, estrogens and other drugs metabolized in the liver along the oxidation pathway (speeds up their metabolism).
Strengthens the action of ethanol, neuroleptics, narcotic analgesics, muscle relaxants, sedatives and hypnotics.
Acetazolamide, alkalinizing urine, reduces the reabsorption of phenobarbital in the kidneys and weakens its effect.
Reduces antibacterial activity of antibiotics and sulfonamides, antifungal action of griseofulvin.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored in a dry, protected from light and out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 2 years.
