Phenobarbital - instructions for use, dose, side effects, contraindications

Excipients: potato starch 33.8 mg, povidone (polyvinylpyrrolidone low molecular weight medical 12600 ± 2700 or type K-17) 1.0 mg, sucrose (sugar) 8.1 mg, crospovidone (polyplasdone XL-10) 2.3 mg, stearic acid 1.5 mg, talc 3.3 mg.

Description:Tablets are white, flat-cylindrical with a facet and a risk.

Pharmacotherapeutic group:antiepileptic agent

ATX: & nbsp

N.03.A.A.02 Phenobarbital

Pharmacodynamics:

PHENOBARBITAL belongs to the barbiturate group.It interacts with the barbiturate site of benzodiazepine-gamma-aminobutyric acid-the receptor complex, thereby increasing the sensitivity of gamma-aminobutyric acid receptors to gamma-aminobutyric acid, leading to the opening of neuronal channels for chloride ions, which leads to an increase in their entry into the cell. Reduces the excitability of neurons in the epileptogenic focus and the spread of nerve impulses. It shows antagonism against a number of exciting mediators (glutamate). Suppresses the sensory areas of the cerebral cortex, reduces motor activity, depresses the cerebral functions, including the respiratory center. Has no significant effect on the cardiovascular system. Reduces the tone of the smooth muscles of the gastrointestinal tract. In small doses, the intensity of metabolic processes decreases somewhat, which can be manifested by a slight hypothermia.

It has anticonvulsant, sedative (in small doses), hypnotic, antihyperbilirubinemic, myorelaxing and spasmolytic action. Being an inducer of enzymes of microsomal oxidation in the liver, it increases its detoxification function,reduces the concentration of bilirubin in the blood serum.

Pharmacokinetics:

When ingested slowly absorbed, completely.

The maximum concentration in the blood plasma is determined after 1-2 hours, the connection with plasma proteins is 50%, in newborns 30-40%. Metabolized in the liver, induces microsomal liver enzymes CYP3A4, CYP3A5, CYP3A7 (the rate of enzymatic reactions increases 10-12 times). Cumulates in the body. The 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.

Indications:

- Epilepsy (all types of seizures except for absences), seizures of non-epileptic genesis;

- chorea;

- spastic paralysis;

- sleep disturbances, agitation, anxiety, fear.

Contraindications:

- Hypersensitivity to any of the components of the drug;

- deficiency of sugar / isomaltase, intolerance to fructose, glucose-galactose malabsorption;

- marked hepatic and / or renal insufficiency;

- drug dependence (including in history);

- porphyria;

- active alcoholism;

- drug addiction;

- Myasthenia gravis;

- severe anemia;

- diabetes;

- hyperkinesis;

hypofunction of the adrenal glands;

- hyperthyroidism;

- Depression;

- bronchoobstructive diseases;

- Pregnancy;

- lactation period;

- Children's age (due to the impossibility of accurate dosing).

Carefully:

Asthmatic status, dyspnea, suicide, acute and / or chronic pain syndrome.

Weakened patients (high risk of paradoxical arousal, depression and confusion, even with normal doses).

Dosing and Administration:

Inside.

For adults, the following dosing regimens are recommended:

Sleep Disorders: 100-200 mg for 0.5-1 h before bedtime.

As a sedative drug: 50 mg 2-3 times a day.

As an anticonvulsant: 50-100 mg 2 times a day.

For individuals suffering from a decrease in liver function, doses should be lower than for patients with normal hepatic function, and adapted to the condition of the patient.

Side effects:

From the nervous system: asthenia, dizziness, general weakness, ataxia, nystagmus, paradoxical reaction (especially in elderly and weakened patients - excitement), agitation, inhibition,irritability, headache, hand tremors, drowsiness, hallucinations, depression, nightmarish dreams, sleep disorders, syncope.

From the side of the musculoskeletal system: with prolonged use - violation of osteogenesis and development of rickets.

From the digestive system: nausea, vomiting, constipation, with prolonged use - a violation of liver function.

From the hematopoiesis: agranulocytosis, megaloblastic anemia, thrombocytopenia.

From the side of the cardiovascular system: lowering of blood pressure.

Allergic reactions: skin rash, urticaria, puffiness of the eyelids, face and lips, shortness of breath, rarely - exfoliative dermatitis, malignant exudative erythema (Stevens-Johnson syndrome).

Other: "withdrawal" syndrome: minor symptoms (within 8-12 hours after stopping the use of the drug) - anxiety, motor anxiety, muscle twitching, hand trembling, weakness, dizziness, blurred vision, nausea, vomiting, sleep disturbance, "nightmarish" dreams, orthostatic hypotension; the main symptoms (within 16 hours and lasts up to 5 days) - convulsions, hallucinations; with prolonged use - drug dependence.

To avoid the development of the syndrome of "withdrawal" (headaches, "nightmarish" dreams, drowsiness and / or insomnia), treatment should be discontinued gradually.

Overdose:

Symptoms: nystagmus, ataxia, dizziness, headache, blockage, blurred speech, severe weakness, decreased or loss of reflexes, pronounced drowsiness or agitation, increased or decreased body temperature, respiratory depression, dyspnea, lowering of blood pressure, narrowing of the pupils (alternating with paralytic enlargement), oliguria, tachi or bradycardia, cyanosis, confusion, cessation of brain electrical activity, pulmonary edema, coma, later pneumonia, arrhythmias, heart failure; when taking 2-10 g - a lethal outcome; with chronic toxicity - irritability, weakened ability to critical evaluation, sleep disorders, confusion.

Treatment: there is no specific antidote. Gastric lavage, reception of activated charcoal, conduct of detoxification therapy, symptomatic treatment, maintenance of vital body functions.

Interaction:

Phenytoin and valproic acid increase the content of phenobarbital in the blood serum.

Anticonvulsant effect of phenobarbital decreases with simultaneous reception with reserpine, increases when combined with amitriptyline, nialamide, diazepam, chlordiazepoxide.

Reduces the effectiveness of oral contraceptives and salicylates.

Reduces the blood in the blood of indirect anticoagulants, glucocorticosteroids, griseofulvin, doxycycline, estrogens and other drugs metabolized in the liver along the oxidation path (speeds up their destruction).

Strengthens the effect of alcohol, neuroleptics, narcotic analgesics, muscle relaxants, sedatives and hypnotics.

Acetazolamide, alkalinizing urine, reduces the reabsorption of phenobarbital in the kidneys and weakens its effect.

The hypnotic effect of phenobarbital decreases with simultaneous administration of atropine, belladonna extract, dextrose, thiamine, nicotinic acid, analeptics and psychostimulating drugs.

Reduces antibacterial activity of antibiotics and sulfonamides, antifungal action of griseofulvin.

Special instructions:

Avoid prolonged use of the drug due to the possibility of its cumulation in the body and the development of addiction.

To avoid the development of the syndrome of "withdrawal" (headaches, "nightmarish" dreams, drowsiness and / or insomnia), treatment should be discontinued gradually.

Effect on the ability to drive transp. cf. and fur:

During the treatment period it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets, 100 mg.

Packaging:

For 6 or 10 tablets in a contour non-jawed package.

1 or 2 contour non-jawed packages of 6 tablets or 1 contour non-jawed package of 10 tablets together with instructions for use in a pack of cardboard.

180 contour non-jawed packages of 10 tablets or 300 contour non-jawed packages of 6 tablets (1800 tablets) with an equal number of instructions for use in a cardboard box or boxes of corrugated cardboard (for inpatient).

10 tablets per contour cell pack. 1 or 2 contourcell packs with instructions for use in a pack of cardboard.

Storage conditions:

In accordance with the rules for storage of psychotropic substances listed in List III of the "List of narcotic drugs, psychotropic substances and their precursors subject to control in the Russian Federation".

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N002444 / 01

Date of registration:06.06.2008

The owner of the registration certificate:MOSCOW ENDOCRINE FACTORY, FSUE MOSCOW ENDOCRINE FACTORY, FSUE Russia

Manufacturer: & nbsp

MOSCOW ENDOCRINE FACTORY, FSUE Russia

Representation: & nbspMOSCOW ENDOCRINE FACTORY FGUP MOSCOW ENDOCRINE FACTORY FGUP Russia

Information update date: & nbsp20.09.2015

Illustrated instructions

Instructions

Phenobarbital (Phenobarbital)