Pagluferal-2
Pagluferal-2: 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-2
ATX code: N03AX
Active ingredient: phenobarbital (phenobarbitalum), bromizoval (bromisoval), caffeine (caffeine), papaverine hydrochloride (papaverine hydrochloride), calcium gluconate (calcium gluconate)
Manufacturer: CJSC "Moscow Pharmaceutical Factory" (Russia)
Description and photo update: 28.11.2018
Prices in pharmacies: from 78 rubles.
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Pagluferal-2 is an antiepileptic drug.
Release form and composition
Dosage form - tablets: white, chamfered and scored (10 pcs. In blister / non-cell packs, 2 packs in a cardboard box; 40 pcs. In orange glass jars, 1 can in a cardboard box and instructions for using Pagluferal -2).
Active ingredients in 1 tablet:
- calcium gluconate - 250 mg;
- bromized - 100 mg;
- phenobarbital - 35 mg;
- papaverine hydrochloride - 15 mg;
- caffeine sodium benzoate - 7.5 mg.
Auxiliary components in Pagluferal-2: potato starch, calcium stearate.
Pharmacological properties
Pharmacodynamics
Pagluferal-2 is a combined antiepileptic agent, the action of which is due to the properties of its active components:
- calcium gluconate: makes up for the lack of calcium ions necessary for the transmission of nerve impulses;
- bromized: has a moderate hypnotic and sedative effect;
- phenobarbital: interacts with the "barbiturate" site of the benzodiazepine-GABA-receptor complex, thereby increasing the sensitivity of GABA-receptors to GABA (gamma-aminobutyric acid), facilitates the opening of neuronal channels for chlorine ions and, as a result, increases their entry into the cell. Shows antagonism in relation to a number of excitatory mediators (for example, glutamate), reduces the tone of smooth muscles of the gastrointestinal tract, reduces the spread of nerve impulses and the excitability of neurons of the epileptogenic focus. It inhibits cerebral functions (including the respiratory center), suppresses the sensory areas of the cerebral cortex, and reduces motor activity. It has an anticonvulsant, antispasmodic, sedative and hypnotic effect;
- papaverine hydrochloride: has an antispasmodic and hypotensive effect, reduces tone and relaxes the smooth muscles of internal organs and blood vessels;
- caffeine-sodium benzoate: stimulates the respiratory and vasomotor centers, increases the reflex excitability of the spinal cord, stimulates metabolic processes in organs and tissues (including the central nervous system and muscle tissue).
Pharmacokinetics
- calcium gluconate: 1/5 to 1/3 part is absorbed in the small intestine. Approximately 20% of the substance is excreted by the kidneys, the rest is excreted through the intestine (actively excreted by the wall of the terminal section of the gastrointestinal tract);
- phenobarbital: absorbed completely, but slowly. The maximum plasma concentration reaches within 1–2 hours, it binds to plasma proteins by 50%. It undergoes metabolization in the liver, is an inducer of microsomal enzymes CYP3A4, CYP3A5 and CYP3A7 (the rate of enzymatic reactions increases 10-12 times). Has the ability to accumulate in the body. The half-life is 2-4 days. It is excreted by the kidneys (about 25% unchanged, the rest in the form of glucuronide). Penetrates through the placental barrier and into breast milk;
- papaverine hydrochloride: the connection with plasma proteins is about 90%, bioavailability is 54%. It is well distributed in the body, penetrates the histohematogenous barriers. It is metabolized in the liver. It is excreted in the form of metabolites by the kidneys. The half-life is 0.5–2 hours (it can be extended up to 24 hours);
- caffeine: characterized by good absorption throughout the intestine. The maximum plasma concentration reaches within 50–75 minutes. It is quickly distributed in all tissues and organs, crosses the placenta and the blood-brain barrier. With blood proteins (mainly albumin), 25–36% binds. It is metabolized in the liver: in adults - more than 90% of the dose, in children of the first years of life - no more than 15%. In an adult patient, about 80% of the dose of caffeine received is metabolized into paraxanthine, about 10% into theobromine, and about 4% into theophylline. Subsequently, these compounds are demethylated to monomethylxanthines, then to methylated uric acids. Caffeine and its metabolites are excreted by the kidneys. The half-life is 3.9-5.3 hours (in some cases, up to 10 hours).
Indications for use
Pagluferal-2 is used to treat epilepsy.
Contraindications
- drug dependence (including a history);
- depression;
- hyperkinesis;
- broncho-obstructive diseases;
- diabetes;
- porphyria;
- myasthenia gravis;
- hyperthyroidism;
- hypofunction of the adrenal glands;
- severe anemia;
- severe hepatic and / or renal failure;
- active alcoholism;
- age up to 3 years;
- period of pregnancy and lactation;
- hypersensitivity to any component in Pagluferal-2.
Pagluferal-2 is used with caution in debilitated patients (this is due to the high risk of depression, confusion, paradoxical agitation, even when the drug is prescribed in standard therapeutic doses).
Pagluferal-2, instructions for use: method and dosage
Pagluferal-2 tablets are taken orally, after meals.
Recommended single doses:
- adults and adolescents from 14 years old: 4 tablets;
- children 10-14 years old: 2.5 tablets;
- children 7-9 years old: 2 tablets;
- children 5–6 years old: 1.5 tablets;
- children 3-4 years old: 1 tablet.
Frequency rate of admission during the day - 2 times.
Side effects
Possible side effects of Pagluferal-2:
- from the central nervous system: general weakness, sleep disturbances, nystagmus, dysarthria, ataxia, dizziness, hallucinations, paradoxical reactions (especially in debilitated patients and elderly patients);
- from the digestive system: constipation or diarrhea, nausea, vomiting, increased activity of hepatic transaminases;
- on the part of the cardiovascular system: increase or decrease in blood pressure, arrhythmias (including extrasystole), tachycardia, atrioventricular block;
- from the hematopoietic system: thrombocytopenia, megaloblastic anemia, agranulocytosis;
- others: allergic reactions; with long-term use - drug dependence.
Overdose
Overdose usually intensifies the reactions described in the side effects.
It is recommended to flush the stomach and take activated charcoal. Then symptomatic therapy is carried out.
special instructions
With a slight hypercalciuria, decreased glomerular filtration, history of nephrolithiasis, Pagluferal-2 should be used with caution, under constant control of the level of calcium in the urine (due to the presence of calcium gluconate in the tablets).
During treatment, it is recommended to refrain from drinking alcoholic beverages.
Influence on the ability to drive vehicles and complex mechanisms
Given the specifics of the disease and the risk of developing reactions from the central nervous system, during the period of therapy, it is worth refraining from any activities that require the speed of psychomotor reactions, including driving.
Application during pregnancy and lactation
The anticonvulsant drug Pagluferal-2 is contraindicated for use in pregnant and breastfeeding women.
Pediatric use
Due to the solid dosage form, Pagluferal-2 is not used to treat children under 3 years of age.
With impaired renal function
With severe renal failure, it is contraindicated to take Pagluferal-2.
For violations of liver function
In case of severe hepatic insufficiency, it is contraindicated to take Pagluferal-2.
Drug interactions
- valproate, phenytoin: the level of phenobarbital in the blood serum increases;
- salicylates, oral contraceptives: their effectiveness decreases;
- acetazolamide: the reabsorption of phenobarbital (due to urine alkalinization) decreases and, as a result, its effect;
- sedatives and hypnotics, muscle relaxants, narcotic analgesics, neuroleptics, ethanol: their effects are enhanced;
- doxycycline, griseofulvin, estrogens, glucocorticosteroids, indirect anticoagulants and other drugs metabolized in the liver by oxidation: their concentration in the blood decreases (due to increased metabolism);
- antibiotics, sulfonamides: their antibacterial activity decreases;
- griseofulvin: the severity of its antifungal action decreases;
- reserpine: the effect of phenobarbital decreases;
- amitriptyline, chlordiazepoxide, diazepam, nialamide: the effect of phenobarbital is enhanced.
Analogs
Analogs of Pagluferal-2 are: Briviak, Valproic acid, Depakin, Difenin, Convilept, Konvuleks, Lamictal, Lamotrigine, Pagluferal, Pagluferal-3, Pregabalin, Replica, Ropimat, Phenobarbital, Epiterra, etc.
Terms and conditions of storage
Keep out of the reach of children, protected from light and moisture, at temperatures up to 25 ° C.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Pagluferal-2
There are few reviews about Pagluferal-2 on medical websites and specialized forums, but they are mostly positive. The drug has a pronounced anticonvulsant effect, but it is potent, therefore it should be used strictly as directed by a doctor.
Price for Pagluferal-2 in pharmacies
The approximate price for Pagluferal-2 is 97–105 rubles per pack of 20 tablets.
Pagluferal-2: prices in online pharmacies
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Drug name Price Pharmacy |
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Pagluferal-2 tablets 20 pcs. RUB 78 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!
