Pagluferal-1
Pagluferal-1: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Pagluferalum-1
ATX code: N05CB02
Active ingredient: bromized (bromisoval) + calcium gluconate (calcium gluconate) + caffeine (caffeine) + papaverine (papaverine) + phenobarbital (phenobarbital)
Producer: Moscow pharmaceutical factory (Russia)
Description and photo update: 2018-21-11
Prices in pharmacies: from 63 rubles.
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Pagluferal-1 is a combined drug that has an antiepileptic, hypnotic effect.
Release form and composition
The dosage form of the release of the drug Pagluferal-1 - tablets: white, in the middle with a chamfer and a risk (in a cardboard box 2 blisters of 10 tablets each or 1 dark glass jar containing 40 tablets).
Active ingredients in 1 tablet:
- bromized - 0.1 g;
- phenobarbital - 0.025 g;
- caffeine sodium benzoate - 0.007 5 g;
- calcium gluconate - 0.25 g;
- papaverine hydrochloride - 0.015 g.
Additional components: potato starch, calcium stearate.
Pharmacological properties
Pharmacodynamics
Pagluferal-1 belongs to the antiepileptic combination drugs.
The effect of the drug is due to the properties of its active substances:
- papaverine hydrochloride: has an antispasmodic and hypotensive effect, promotes relaxation of smooth muscles and a decrease in the tone of internal vessels and organs;
- phenobarbital: has anticonvulsant, sedative, hypnotic and antispasmodic effects. Interacts with the barbiturate site of the benzodiazepine-GABA-receptor complex. Due to this, the sensitivity of GABA receptors to GABA (gamma-aminobutyric acid) increases, which causes the opening of neuronal channels for chlorine ions and leads to an increase in their entry into cells. With the use of phenobarbital, the development of the following effects is observed: suppression of the sensory zones of the cerebral cortex, a decrease in the excitability of neurons of the epileptogenic focus, a decrease in the spread of nerve impulses, the manifestation of antagonism with respect to some excitatory mediators (glutamate, etc.), a decrease in the tone of smooth muscles of the gastrointestinal tract, inhibition cerebral functions (including the respiratory center),decreased motor activity;
- calcium gluconate: helps to replenish the deficiency of calcium ions, which are involved in the transmission of nerve impulses;
- bromized: has mild hypnotic and sedative properties;
- caffeine: promotes excitation of the vasomotor and respiratory centers, an increase in the reflex excitability of the spinal cord, activation of metabolic processes in organs and tissues, including in the central nervous system and muscle tissues.
Pharmacokinetics
Caffeine
Caffeine is well absorbed throughout the intestine. The time to reach C max (maximum concentration of the substance) in blood plasma is in the range of 50–75 minutes. It is characterized by rapid distribution in all tissues and organs and penetration through the blood-brain barrier and placenta. Connection with blood proteins (albumin) - from 25 to 36%.
Metabolism occurs in the liver (more than 90% of caffeine, in children of the first years of life - up to 10-15%). Approximately 4%, 10% and 80% of the substance in adults is metabolized to theophylline, theobromine and paraxanthine, respectively. Subsequently, they are demethylated into monomethylxanthines, then into methylated uric acids. T 1/2 (half-life) in adults is 3.9-5.3 hours (sometimes up to 10 hours). Caffeine and its metabolites are excreted by the kidneys.
Phenobarbital
It is absorbed slowly and in full. C max in blood plasma is reached in 60–120 minutes, the connection with plasma proteins is approximately 50%. The metabolic process occurs in the liver, induces liver microsomal enzymes CYP3A4, CYP3A5, CYP3A7 (there is an increase in the rate of enzymatic reactions by about 10-12 times). Accumulates in the body. T 1/2 - in the range of 48–96 hours. It is excreted in the form of glucuronide by the kidneys, unchanged - about 25%. Penetrates through the placental barrier and into breast milk.
Calcium gluconate
1/5 to 1/3 of the dose is absorbed in the small intestine. Approximately 80% of the dose is removed with the intestinal contents (the most active process occurs in the wall of the terminal gastrointestinal tract), the rest is excreted by the kidneys.
Papaverine
The biological availability of papaverine averages 54%. The connection with plasma proteins is approximately 90%. It is well distributed, penetrates the histohematogenous barriers. The metabolic process takes place in the liver. T 1/2 - from 30 to 120 minutes (significant lengthening is possible). It is excreted by the kidneys in the form of metabolites.
Indications for use
According to the instructions, Pagluferal-1 is prescribed for the treatment of epilepsy.
Contraindications
- broncho-obstructive diseases;
- hypofunction of the adrenal glands;
- porphyria;
- severe anemia;
- hyperthyroidism;
- severe renal / hepatic impairment;
- depression;
- drug dependence (including a burdened history);
- myasthenia gravis;
- active alcoholism;
- diabetes;
- hyperkinesis;
- age up to 3 years;
- pregnancy and lactation;
- individual intolerance to the components of the drug.
In debilitated patients during the period of treatment with Pagluferal-1, medical monitoring of the condition is required, since even with therapy at usual doses there is an increased risk of paradoxical arousal, depression and confusion.
Instructions for use of Pagluferal-1: method and dosage
Pagluferal-1 is intended for oral administration.
Frequency rate - 2 times a day, preferably after meals.
The drug is prescribed in the following single doses:
- children over 14 years old and adults: 4 tablets;
- children 10-14 years old: 3 tablets;
- children 7-9 years old: 2 tablets;
- children 5–6 years old: 1.5 tablets;
- children 3-4 years old: 1 tablet.
Side effects
- nervous system: general weakness, paradoxical reaction, ataxia, dysarthria, dizziness, sleep disturbances, nystagmus, hallucinations;
- cardiovascular system: atrioventricular block, tachycardia, increase / decrease in blood pressure, arrhythmia (including extrasystole);
- hematopoietic system: agranulocytosis, megaloblastic anemia, thrombocytopenia;
- gastrointestinal tract: increased activity of hepatic transaminases, nausea, vomiting, diarrhea / constipation;
- others: allergic reactions; with a long course of use - drug dependence.
Overdose
In case of an overdose, the severity of side effects increases.
It is shown that symptomatic therapy is carried out, as well as measures aimed at reducing the absorption of active substances (intake of activated carbon, gastric lavage).
special instructions
Alcohol should not be consumed during therapy.
Against the background of a slight hypercalciuria, a decrease in glomerular filtration, a history of nephrolithiasis during therapy with Pagluferal-1, it is necessary to control the calcium content in the urine (due to the presence of calcium gluconate in the preparation).
Influence on the ability to drive vehicles and complex mechanisms
During the period of therapy with Pagluferal-1, patients should refrain from driving vehicles.
Application during pregnancy and lactation
Pagluferal-1 is contraindicated during pregnancy / breastfeeding.
Pediatric use
The appointment of Pagluferal-1 is contraindicated in newborns and children under 3 years of age.
With impaired renal function
It is contraindicated to use Pagluferal-1 in case of severe renal failure.
For violations of liver function
It is contraindicated to use Pagluferal-1 in case of severe hepatic insufficiency.
Drug interactions
- reserpine: the effectiveness of phenobarbital decreases;
- griseofulvin: the antifungal effect is reduced;
- valproate and phenytoin: serum phenobarbital in the blood increases;
- salicylates and oral contraceptives: the effectiveness of these drugs decreases;
- amitriptyline, diazepam, nialamide, chlordiazepoxide: the effectiveness of phenobarbital increases;
- ethanol, antipsychotics, muscle relaxants, narcotic analgesics, drugs with sedative and hypnotic effects: their effectiveness is enhanced;
- glucocorticosteroids, doxycycline, indirect anticoagulants, griseofulvin, estrogens and other drugs that are metabolized in the liver by oxidation: the content of these drugs in the blood decreases (associated with an acceleration of metabolism);
- sulfonamides, drugs with antibacterial action: the antibacterial activity of drugs decreases;
- acetazolamide: renal reabsorption of phenobarbital decreases, which leads to a weakening of its effectiveness (associated with urine alkalinization).
Analogs
Pagluferal-1 analogs are Pagluferal-2, Pagluferal-3.
Terms and conditions of storage
Store at a temperature not exceeding 25 ° C in a place protected from moisture and light. Keep out of the reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Pagluferal-1
According to reviews, Pagluferal-1 is an effective antiepileptic drug. They also indicate a positive trend in its use for the treatment of sleep disorders (frequent waking up, fears).
Pagluferal-1 is contraindicated for newborns, however, individual cases of the drug use are known, for example, with tremor at a dose of ¼ tablets 2 times a day.
Price for Pagluferal-1 in pharmacies
The price of Pagluferal-1 (20 pcs. In a package) is approximately 76–92 rubles.
Pagluferal-1: prices in online pharmacies
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Drug name Price Pharmacy |
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Pagluferal-1 tablets 20 pcs. RUB 63 Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
