Phenobarbital use. Phenobarbital: instructions for use. Cross-drug interactions

Instructions for use:

Phenobarbital – antiepileptic medicinal product.

Medicines Dormiral, Barbinal, Luminal are analogues of Phenobarbital in action.

Composition and release form of Phenobarbital

According to the instructions, Phenobarbital is produced in the form of tablets of 0.005 g (for children), 0.05 g and 0.1 g (for adults), as well as in powder form. Phenobarbital is the active ingredient of the drug. Auxiliary components: stearic acid, potato starch, talc, sucrose.

Pharmacological action of Phenobarbital

According to the instructions, Phenobarbital has antihyperbilirubinemic, hypnotic, anticonvulsant, muscle relaxant and antispasmodic effects. Phenobarbital suppresses the sensory area of the cerebral cortex, reduces motor activity. The principle of action of Phenobarbital has not been fully established, but there is an assumption that the drug suppresses ascending conduction in the reticular formation and blocks the transmission of impulses to the cerebral cortex.

Reviews of Phenobarbital indicate that this drug significantly enhances the neutralizing function of the liver and is often used to combat various intoxications of the body.

Judging by the reviews of Phenobarbital, small doses of the drug have a calming effect, so the drug is often used in complex therapy with other medications (vasodilators, antispasmodics) in the treatment of neurovegetative disorders.

The direct inhibitory effect of Phenobarbital on the respiratory center has been proven. The drug significantly reduces the tone of smooth muscles of the gastrointestinal tract, slightly reduces the intensity metabolic processes with hypnotic effects.

Indications for use of Phenobarbital

According to the instructions, there are the following indications for the use of Phenobarbital:

epilepsy;
hyperbilirubinemia;
spasms of peripheral arteries and spastic paralysis;
congenital non-hemolytic unconjugated hyperbilirubinemia;
chronic intrahepatic cholestasis;
insomnia, tension, anxiety, fear, agitation, convulsions of various origins, tremor;
alcohol withdrawal;
encephalitis caused by influenza, measles, rubella, chickenpox, whooping cough and mononucleosis;
neurovegetative disorders;
generalized tonic-clonic seizures;
focal seizures in children and adults.

Contraindications to the use of Phenobarbital

severe renal and/or liver failure;
hypersensitivity to the active substance of the drug;
porphyria;
chronic alcoholism;
myasthenia gravis;
drug addiction;
thyrotoxicosis;
first and second trimesters of pregnancy;
lactation period;
severe anemia;
hyperkinesis;
broncho-obstructive pulmonary diseases.

Side effects

Judging by the reviews of Phenobarbital, the medication often causes a paradoxical reaction (unusual agitation) in weakened patients, as well as in children. In some cases, long-term use of the medicine can cause nausea, constipation, vomiting, asthenia, weakness, and dizziness. Rarely - fainting, ataxia, depression, hallucinations, allergic reactions, hemolytic disorders. Long-term use of the drug often leads to disruption of osteogenesis and contributes to the development of rickets.

How to use Phenobarbital

as a sedative - 30-50 mg three times a day;
as a sleeping pill – 100-200 mg an hour before bedtime;
for epilepsy, you should take 50-100 mg of the drug twice a day;
as an antispasmodic - 10-50 mg two to three times a day.

According to the instructions, children should take Phenobarbital half an hour before meals, twice a day. Recommended single doses of the drug depending on the age of the child:

up to six months – 5 mg;
from six months to one year – 10 mg;
from one year to two years – 20 mg;
at three to four years – 30 mg;
at five to six years – 40 mg;
at seven to nine years old – 50 mg;
at ten to fourteen years – 75 mg of the drug.

Overdose

With a single dose of one gram of the drug Phenobarbital, the following symptoms are observed: lethargy, nystagmus, dizziness, headache, decrease or increase in body temperature, blurred speech, irritability, loss or weakening of reflexes, sleep disturbances, difficulty and slowing of breathing, coma, ataxia, decreased blood pressure , brady- or tachycardia, pneumonia, confusion, pulmonary edema, oliguria, constriction of the pupils. In these cases, symptomatic therapy is necessary.

When taking from 2 to 10 g of the drug Phenobarbital, it is fatal.

Phenobarbital interaction

The drug reduces the antimicrobial activity of sulfonamides and antibiotics, as well as the antifungal effect of griseofulvin; reduces the effectiveness of doxycycline, estrogens, corticosteroids, accelerating their destruction in the liver.

Simultaneous administration of Phenobarbital with atropine, belladonna extract, dextrose, thiamine, nicotinic acid, analeptics and psychostimulants medicines leads to a decrease in the hypnotic effect of the drug. The use of Phenobarbital in complex therapy with reserpine leads to a decrease in the anticonvulsant effect of the drug and an increase in the same effect under the influence of nialamide, diazepam, amitriptyline, and chlordiazepoxide.

Nowadays, few people know what phenobarbital is, although this substance is included in many popular drugs. Many people have been taking Corvalol or Valocordin for years without knowing what ingredients these drugs contain. After all, phenobarbital was recently classified as a dangerous narcotic substance and banned in some countries. And products based on it began to gradually disappear from sale. Now the drug "Phenobarbital" and its analogues are used only as prescribed by a doctor. After all, it is one of the most effective anticonvulsants and sedatives.

What is phenobarbital

This substance is from the group of barbiturates. It reduces the excitability of brain neurons and the propagation of nerve impulses in epilepsy. When exposed to it, the flow of calcium ions into the cell increases, which helps to reduce motor activity and decrease the tone of smooth muscles.

This substance was first obtained at the beginning of the 20th century in Germany. Phenobarbital appeared on sale under the name "Luminal". It was the most popular sleeping pill until drugs from the benzodiazepine group appeared. IN last years Many countries have banned the production of phenobarbital. In Russia, drugs based on it are on sale, but only with a doctor’s prescription.

Nowadays, Phenobarbital is mainly used in the treatment of epilepsy. Its analogues and products containing this substance in small quantities can be prescribed for less serious conditions, for example, overexcitation or insomnia.

The narcotic effect of this substance is special: it does not cause euphoria, only drowsiness and apathy. In addition, taking phenobarbital leads to very strong dependence. But its unhealthy popularity as a drug is explained by its cheapness and availability.

Preparations based on phenobarbital

The medicine with this name is mainly familiar to patients with seizures or severe sleep disorders. But you can buy drugs that contain phenobarbital. The most famous are Corvalol and Valocorin. They are inexpensive and very popular as a sleeping pill and sedative, especially among the older generation.

Less popular drugs are:

Features of the action

Preparations based on phenobarital have been used in medicine for a long time. They are even prescribed to children, as they have unique properties. In some pathologies, only with their help can the patient be helped. The effect of phenobarbital extends only to smooth muscles and neurons, without affecting the cardiovascular system. After taking such drugs orally, the following effects are observed:

the intensity of metabolic processes decreases slightly;
motor activity decreases;
the tone of the smooth muscles of the gastrointestinal tract decreases;
the detoxification function of the liver increases;
The concentration of bilirubin in the blood decreases.

Phenobarbital is widely used in medicine due to the fact that it has anticonvulsant, sedative, hypnotic and antispasmodic effects. It is used in emergency cases, as it is highly addictive when taken for a long time.

Phenobarbital: indications for use

Now drugs based on it are used only in serious cases. They are no longer prescribed for ordinary insomnia. Indications for the use of this remedy are the following conditions:

Contraindications

Despite the fact that Phenobarital has very serious indications, not all patients can receive such treatment. Taking medications based on this substance is contraindicated in the following cases:

Side effects

Preparations containing phenobarbital are classified as narcotic substances. In addition to the fact that they are highly addictive, even with short-term use there may be side effects:

general weakness, dizziness, asthenia;
lethargy, speech impairment;
hallucinations, nightmares;
depression;
sleep disorders;
decreased visual acuity;
dry mouth, nausea, vomiting, intestinal dysfunction;
thrombocytopenia, anemia;
rapid heartbeat, heart failure;
decline blood pressure;
rash, swelling, dermatitis, itching;
labored breathing.

Instructions for use

Phenobarbital and drugs similar in composition are available in the form of tablets of 100 and 50 mg for adults and 5 mg for children. Depending on the indications and regimen, the doctor prescribes different dosages. As a rule, you need to drink 100 mg an hour before bedtime. If Phenobarbital was prescribed for regular use by a patient with epilepsy, he is recommended to take 50-100 mg twice a day. As a sedative, drugs based on this substance are taken in a dosage of 50 mg 2-3 times a day. It is recommended to reduce the dose for elderly people, as well as patients with impaired liver and kidney function.

Phenoarital is prescribed to children according to strict indications. The dosage is determined by the doctor depending on the age and condition of the patient. Prescribe the drug half an hour before meals 2 times a day. The dosage is usually as follows: up to 6 months 5 mg, up to a year - 10 mg, 1-2 years - 20 mg, up to 4 years - 30 mg, up to 7 years - 40 mg, 7-10 years - 50 mg, up to 14 years - 75 mg. After this age, the dosage of the drug is already adult.

If taken regularly, it is necessary to stop treatment gradually. When phenobarbital-based drugs are abruptly discontinued, depression, insomnia, and headaches often develop. Dependence develops after two weeks of regular use, so it is not recommended to use it as a sleeping pill and sedative for more than 10 days.

Special instructions for use

Many people do not know what phenobarbital is, but they calmly take drugs based on it. Some of them are sold without a doctor's prescription, and people do not even know what a serious drug they are using. Therefore, it is advisable to always study the composition and instructions before using each drug. When using drugs containing phenobarbital, it is advisable to take into account the following features:

Analogues of the drug

Few people know what Phenobarbital tablets are. Analogues of this remedy are most often used. The most famous of them has long been “Luminal”. But in Lately it is used less and less. The following methods are now more common:

Navigation

At the beginning of the 20th century, the pharmaceutical company Bayer launched the potent sleeping pill and sedative Luminal on the market. For forty years, the product remained a leader in its pharmacological group until benzodiazepines appeared. Today, consumers are more familiar with the trade name “Phenobarbital”, which comes from the name of the active ingredient. Despite the abundance and variety of analogues, the synthetic drug is still actively used to relieve convulsive syndromes. Doctors warn that only if you follow the instructions for using Phenobarbital can you count on a therapeutic effect with minimal risks.

Compound

The main active ingredient of the drug is phenobarbital. It is a white powder with a crystalline structure with a slight bitter taste and no odor. It is almost insoluble in ordinary water, poorly in boiling water, well in alkalis and alcohol. Depending on the dosage form, there are additional components that give the product the desired structure, physical properties. Phenobarbital is part of such common drugs as Corvalol and Valocordin.

Release form

Manufacturers offer a variety of formulations of Phenobarbital. Recently, the circulation of the drug has been limited, but it is possible to replace one medicinal type of composition with another only with the permission of the doctor and according to the scheme developed by him.

In pharmacies you can find:

tablets - round, white, flat elements of 50 or 100 mg of active substance for adults. For children, Phenobarbital is available in 5 mg tablets with a high sucrose content;
solution – transparent, colorless composition of 0.2% concentration in ampoules of 1 ml;
powder is a pure substance that is used only in a hospital setting.

Working with each of the above dosage forms accompanied by its own specifics. The rules for using the products must be established by the attending physician, taking into account the conditions given in the instructions from the manufacturer.

pharmachologic effect

"Phenobarbital" is included in pharmacological group antiepileptic, sedative and hypnotic drugs. It belongs to the long-acting barbiturates.

The chemical and biological properties of the product make it possible not to officially classify it as a drug, unlike some intermediate or short-acting barbiturates. The synthetic composition is actively used to combat sleep disorders, manifestations of intoxication of the body, and seizures of various etiologies.

Pharmacodynamics and pharmacokinetics

The mechanism of action of the drug can be traced at the cellular level. The component causes stimulation of the receptors of the nervous system, changing the principles of the flow of metabolic processes, chemical reactions. The result is a decrease in the excitability of cell membranes, inhibition of nervous activity, and inhibition of impulse transmission between neurons.

The body's reaction to the use of the drug "Phenobarbital":

relieving convulsive syndrome by blocking the appearance and propagation of nerve impulses;
a decrease in the volume of free bilirubin in the blood against the background of changes in enzyme activity. This feature of the product allows you to stimulate the “cleaning” properties of the liver and improve the quality of its work during intoxication;
weak analgesic effect, but an increased reaction to the stimulus is not excluded;
reduction of nervous tension, feeling of calm, sleep. Achieved by suppressing sensory activity of areas of the cerebral cortex. Such sleep differs from physiological sleep in the shortening of some phases of the process. It occurs within 30-60 minutes, lasting on average 6-8 hours. When taken regularly, the therapeutic benefit of the product decreases after 10-14 days;
sedative effect when using small doses of the drug;
dulling the severity of signs of neurovegetative disorders when using the composition in combination with antispasmodics and/or vasodilators;
an overdose of the active component provokes depression of the respiratory center in the brain, dulls its sensitivity to carbon dioxide, and reduces tidal volume;
lowering blood pressure when using large doses;
relieving increased tone of the smooth muscles of the digestive organs;
slowing down the rate of metabolic processes;
slight drop in body temperature.

After oral administration, the main component is absorbed in the small intestine, its maximum concentration in the blood is observed after 1-2 hours. The product is evenly distributed throughout the body; in the brain tissue its volume is minimal.

Bioavailability is 80%, binding to blood proteins in an adult reaches 50%, in a newborn – up to 40%. The drug penetrates the placenta well, breast milk.

Elimination of the product takes several days, which creates a risk of accumulation of the substance or its metabolites in tissues. The half-life averages from 2 to 4 days for adults, up to 7 days for newborns. If kidney function is impaired, the substance stays in the body longer, which must be taken into account when selecting doses and drawing up a therapy schedule. The medicine is processed by liver tissue with the formation of inactive breakdown products. Up to 50% of the composition is excreted from the body unchanged, the rest is excreted in the urine.

Indications for use

The multidisciplinary effect of the drug on the body allows it to be used for a wide variety of pathologies. Increased chemical activity, which occurs in combination with other drugs, increases the effectiveness of a number of integrated approaches. The instructions for use of Phenobarbital or Luminal provide basic information on the product. The final decision on the appropriateness of the approach is made by the doctor.

Indications for use of the drug:

epileptic seizures different types, frequency, severity. The exception is absence seizures;
seizures not associated with epilepsy;
spastic type muscle paralysis;
pathological agitation, especially accompanied by anxiety and/or fear;
hemolytic disease of newborns;
chorea;
disturbance of sleep patterns and/or quality;
the need for premedication;
increased concentration of bilirubin in the blood in chronic cholestasis, pathological or physiological conditions of newborns;
infectious diseases (measles, smallpox, whooping cough and others) - as part of complex therapy.

In narcology, through the use of Phenobarbital, patients are helped to cope with the manifestations of withdrawal syndrome due to alcohol dependence. The combination of alcoholic beverages with medication is associated with serious risks, so such therapy is carried out strictly under the supervision of medical professionals.

Contraindications

The manufacturer cites a lot of conditions in which it is better to refrain from using the product. If the patient has relative inhibitions, therapy is recommended to be carried out under the supervision of a physician. If possible, with any restrictions, the drug is replaced with an analogue from the corresponding therapeutic group.

List of absolute contraindications to the use of the medicine:

violent reaction of the body to the main component, increased sensitivity to any barbiturates;
severe decreased performance of the kidneys and/or liver;
metabolic problems, for example, diabetes, damage to the thyroid gland, adrenal glands;
first trimester of pregnancy – there is a high risk of impaired embryo development;
breast-feeding;
myasthenia gravis of any severity;
porphyria in medical history;
chronic alcoholism, drug addiction in the active phase or history;
severe anemia;
respiratory diseases, which are accompanied by shortness of breath and bronchial obstruction.

Separately, there are a number of conditions in which treatment requires special care. Persons with depression, a history of suicide attempts, bronchial asthma, and hyperkinesis need increased attention from doctors. A decrease in kidney and/or liver function should be accompanied by dosage adjustments. Pregnant women (II and III trimesters) and children of any age are usually treated under the supervision of medical personnel. The medication is not recommended for patients with persistent or acute pain.

Side effects

The use of Phenobarbital is often accompanied by drowsiness, decreased activity and attention. If the phenomena do not cause significant discomfort, they are considered a variant of the norm.

Otherwise, treatment should be stopped and the patient should be given a less aggressive drug. Almost all side effects that may occur during treatment become an indication to stop taking the drug. The final decision in each specific case is made by the attending physician, based on the severity of symptoms and the presence of signs of positive dynamics.

Possible side effects therapy:

neurological - severe drowsiness, up to pathologically prolonged sleep. Dizziness, coordination problems, headache, lethargy, depression. Sometimes, instead of a hypnotic effect, insomnia occurs, and the patient is tormented by nightmares. In elderly and weakened patients, a paradoxical reaction in the form of an extreme degree of agitation cannot be ruled out. With long-term use of the drug, hallucinations, tremors of the limbs, and decreased intelligence are possible;
dyspeptic – nausea or vomiting, stool retention. Long-term use may result in deterioration of liver function;
rheological – decrease in the number of platelets, leukocytes and/or red blood cells in the blood;
cardiovascular - slow heart rate, slow decrease or sharp drop in blood pressure;
immune - an allergic response in the form of hives, breathing problems, swelling of certain parts of the face. In rare cases, malignant exudative erythema develops, and the patient may die;
from the senses - involuntary vibrations of the eyeballs;
from the musculoskeletal system - changes in the chemical and structural composition of bones, rickets.

With prolonged use of the medication, its active substance begins to accumulate in the tissues, and drug dependence develops. If you then exit therapy incorrectly, the patient will develop withdrawal syndrome.

During the first 12 hours, anxiety, muscle twitching, hand tremors, and dizziness appear. Weakness, nausea and vomiting may occur, problems with sleep appear, and the patient is tormented by nightmares. Next, the main symptoms arise in the form of hallucinations and seizures. There are often signs of mental drug dependence, which are accompanied by a decrease in libido. To prevent such negative consequences, drug withdrawal is carried out gradually, the regimen is selected by the attending physician.

Instructions for use of Phenobarbital: method and dosage

The annotation for the product states detailed information on the principles of therapy. Despite this, drug dosages should be selected by a doctor. They depend on the patient's age, his physical condition, physiological characteristics, diagnosis, expected results. Typically, the starting daily dose is the therapeutic minimum suitable for a particular case. It is increased only if there are no signs of positive dynamics.

Basic principles of using the medicine:

for epilepsy - adults are given 50 mg twice a day. The dose is gradually increased until a volume that relieves seizures is established. The same schedule is provided for children, but doses are selected according to age. One-time volume for a baby less than 6 months. – 5 mg, up to one year – 10 mg, up to 2 years – 20 mg, up to 4 years – 30 mg, up to 6 years – 40 mg, up to 9 years – 50 mg, up to 14 years – 75 mg;
The composition is taken orally 30-40 minutes before meals;
Abrupt withdrawal from the drug for epilepsy threatens not only withdrawal syndrome, but also the development of status epilepticus and an increase in seizures;
the maximum single dose of the drug for an adult is 200 mg, daily – 500 mg;
for children under 3 years of age, the tablets are crushed into powder, which is diluted with a small amount of water to form a suspension;
for problems with sleep, the drug is given to adults at a single dose of 100-200 mg 30-60 minutes before going to bed. The pediatric dose is selected according to age, starting from 5 mg;
if there is an increased level of bilirubin in the blood, children under 12 years of age are given medicine at a rate of 3 to 8 mg per 1 kg of body weight per day for 3-5 days. Children over 12 years of age are prescribed 90-180 mg of the active ingredient. The therapeutic volume is divided into 2-3 approaches;
as a premedication, the composition is given to patients older than 6 months, 1-3 mg per 1 kg of weight 60-90 minutes before manipulation.

For young children, the drug is often given in the form of a 0.2% solution for oral administration. In this case, you can ignore the meal schedule. In this case, standard dosages are used, unless otherwise provided by the treatment regimen.

Phenobarbital overdose

Addiction and withdrawal symptoms are not the only dangers of barbiturate. When taking it, there is a possibility of developing chronic toxic poisoning or acute overdose. If 1 g of the active substance enters the body, serious negative consequences are possible. For an adult, 2 g of the drug is a potentially lethal dose.

The acute condition is characterized by ataxia, confusion, headache, severe weakness and drowsiness or extreme agitation. The patient experiences oliguria, decreased blood pressure, a drop in body temperature, slow pulse, and cyanosis. In the absence of timely medical care the pupils narrow, reflexes weaken or disappear, the pulse weakens, and bruises appear at pressure points on the skin. Severe poisoning leads to apnea, collapse, coma, and death due to cardiac or respiratory arrest.

Intoxication due to a barbiturate overdose can take the form clinical death, which is explained by the suppression of electrical activity in the brain. In this case, it is important to make a correct diagnosis. If not much time has passed since the development of the emergency condition, and hypoxia has not led to irreversible changes in the brain matter, then the phenomenon is completely reversible.

Chronic Phenobarbital poisoning is characterized by bad mood, apathy, irritability, sleep problems, and decreased intelligence. Victims often complain of dizziness, problems with coordination, poor balance, general weakness, confusion of speech, and drowsiness. In advanced cases, convulsions, hallucinations, and malfunctions of the digestive tract, heart, blood vessels, and kidneys occur.

There is no special antidote that neutralizes the effect of the drug. As first aid in case of acute overdose, it is necessary to remove Phenobarbital from the body as quickly as possible. Additionally, symptomatic therapy is provided according to indications. After performing manipulations aimed at stabilizing the vital functions of the body, the victim is transported to the hospital.

Principles of treating a patient with an overdose of Phenobarbital:

preventing further absorption of the active substance by inducing vomiting and gastric lavage;
reception activated carbon, laxative saline and alkaline solutions, forced diuresis;
normalization of blood pressure, prevention of airway blockage, oxygen supply if necessary;
carrying out anti-shock measures in severe condition of the patient;
preventing oversaturation of the body with sodium or fluid;
hemodialysis for life-threatening intoxication.

After the patient is brought out of critical condition, the activities are not completed. An overdose of barbiturate can cause congestive heart failure, pneumonia, kidney problems, and heart rhythm disturbances. Chronic drug poisoning is treated by gradually eliminating the product. If necessary, symptomatic therapy is carried out.

Interaction

The increased chemical activity of the product requires caution when including it in complex therapy. Any drug combinations in this case should be monitored by the attending physician.

The description of the drug indicates a number of features:

caffeine inhibits the hypnotic properties of the product;
MAO inhibitors and Methylphenidate increase the toxicity of the main substance and its inhibitory effect on the nervous system by increasing the concentration in the blood plasma;
an extensive list of drugs begins to act more intensely or weakly under the influence of phenobarbital (some contraceptives, xanthines, antidepressants, anticoagulants);
in combination with acetazolamide, the composition provokes the development of rickets and osteomalacia;
valproic acid stimulates the sedative effect of the product, up to lethargy;
the effect of some calcium channel blockers is inhibited due to a decrease in their concentration in the blood plasma;
phenobarbital reduces the effectiveness of paracetamol, while creating a toxic effect on the liver;
active substances in psychotropic drugs and sedatives under the influence of the drug can provoke respiratory depression.

These are just the basic points, which are highlighted separately due to the high frequency of use of products in such combinations. The use of barbiturates should be treated with caution against the background of antibacterial therapy, the use of antifungals, analeptics and many other compounds.

special instructions

Phenobarbital affects the central nervous system and affects the activity of liver enzymes. It is perceived differently by people and has a particular impact on the elderly and children. There are several points that must be taken into account to obtain the maximum effect from therapy with minimal risks.

for liver problems, the drug is prescribed in reduced doses;
for the treatment of insomnia, the drug is used less and less, replacing it with less aggressive analogues;
the occurrence of a skin reaction is an indication for discontinuation of the product;
a history of urticaria, angioedema, or bronchial asthma significantly increases the likelihood of developing intolerance to the main component;
A course of Phenobarbital should be accompanied by regular assessment of the functioning of the liver, kidneys, and blood composition;
clinical manifestations of depression may increase under the influence of medication;
children often react to taking barbiturates with signs of irritability, hyperactivity, and unhealthy agitation;
Pregnant women can take the drug only if there are strict indications and it is impossible to choose a less dangerous analogue. Even if all precautions are followed, such manipulations can lead to abnormalities in the child’s development. Used on later barbiturates can provoke drug dependence in newborns;
Taking the drug during pregnancy in the later stages or during childbirth can only be carried out if resuscitation equipment is within walking distance.

Even a single dose of Phenobarbital leads to a decrease in concentration and the development of drowsiness. During the period of treatment, it is better to refrain from driving vehicles or working in hazardous industries.

Terms of sale

The product cannot be purchased at a pharmacy without a prescription written by your doctor.

Storage conditions

The drug should be kept out of the reach of children, in a dark, cool, dry place.

Best before date

The product must be used within 5 years from the date of manufacture, unless otherwise indicated on the packaging.

Newborns

The use of Phenobarbital by children is indicated for hemolytic disease. The drug, increasing the detoxification properties of the liver, reduces the concentration of bilirubin in the serum and weakens the clinical picture. For newborns, tablets with a minimum concentration of the substance are provided, and gentle treatment regimens have been developed. Treatment is carried out in a hospital; at the same time, the baby’s vital signs are monitored.

Phenobarbital and alcohol

The simultaneous use of the drug and alcoholic beverages is dangerous to human health and life. The harm to the body is due to the double inhibitory effect on the central nervous system. You should avoid alcohol in any form for the entire period of therapy. Otherwise, the consequences will be unpredictable, even fatal.

Hypnotic and sedative drug. Anticonvulsant

Active substance

Phenobarbital

Release form, composition and packaging

6 pcs. - cellless contour packages.
10 pieces. - contour cellular packaging (1) - cardboard packs.
10 pieces. - contour cell packaging (2) - cardboard packs.
6 pcs. - cellless contour packaging (1000) - cardboard boxes.

pharmachologic effect

Belongs to the group of barbiturates. It interacts with the barbiturate portion 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 neurons in the epileptogenic focus and the propagation of nerve impulses. Shows antagonism towards a number of excitatory mediators (glutamate and others). Suppresses the sensory zones of the cerebral cortex, reduces motor activity, inhibits cerebral functions, incl. respiratory center. Does not have a significant effect on the cardiovascular system. Reduces the tone of the smooth muscles of the gastrointestinal tract. In small doses, it somewhat reduces the intensity of metabolic processes, which may manifest itself as slight hypothermia.

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

Pharmacokinetics

When taken orally, it is absorbed slowly and completely. Cmax in the blood 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. 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.

Indications

epilepsy (all types of seizures except absences), seizures of non-epileptic origin;
chorea;
spastic paralysis;
sleep disorders;
excitation;
anxiety;
fear.

Contraindications

pronounced hepatic and/or;
drug dependence (including a history);
hyperkinesis;
myasthenia gravis;
severe anemia;
porphyria;
diabetes;
adrenal hypofunction;
hyperthyroidism;
depression;
broncho-obstructive diseases;
active alcoholism;
pregnancy;
lactation period;
this dosage is not used in children due to the impossibility of precise dosing (for children, tablets containing 5 mg or 50 mg of phenobarbital are used);
hypersensitivity to any of the components of the drug.

Carefully: in weakened patients (high risk of paradoxical agitation, depression and confusion, even when prescribed normal doses).

Dosage

For adults:

violations sleep: 100-200 mg 0.5-1 hour before bedtime.
as a sedative: 50 mg 2-3 times/day.
as an anticonvulsant: 50-100 mg 2 times/day.

At decreased liver function should be prescribed in smaller doses.

Side effects

From the nervous system: asthenia, dizziness, general weakness, ataxia, nystagmus, paradoxical reaction (especially in elderly and weakened patients - agitation), hallucinations, depression, nightmares, sleep disturbances, syncope.

From the musculoskeletal system: with long-term use - a violation of osteogenesis and the development of rickets.

From the outside digestive system: nausea, vomiting, constipation, with prolonged use - impaired liver function.

From the hematopoietic organs: agranulocytosis, megaloblastic anemia, thrombocytopenia.

From the cardiovascular system: decrease in blood pressure.

Allergic reactions: skin rash, hives, swelling of the eyelids, face and lips, difficulty breathing; rarely - exfoliative dermatitis, malignant exudative erythema (Stevens-Johnson syndrome).

Others: with long-term use - drug dependence.

Overdose

Symptoms: nystagmus, ataxia, dizziness, headache, retardation, slurred speech, severe weakness, decreased or loss of reflexes, severe drowsiness or agitation, increased or decreased body temperature, respiratory depression, shortness of breath, decreased blood pressure, constriction of the pupils (alternating with paralytic dilation), oliguria, tachy- or bradycardia, cyanosis, confusion, cessation of electrical activity of the brain, pulmonary edema, coma, later pneumonia, arrhythmias, failure; when taking 2-10 g - death; with chronic toxicity - irritability, weakened ability to critically evaluate, sleep disturbances, confusion.

Treatment: there is no specific antidote. Gastric lavage, taking activated charcoal, detoxification therapy, symptomatic treatment, maintaining vital functions of the body.

Drug interactions

Phenytoin and valproate increase the content of phenobarbital in the blood serum.

The anticonvulsant effect of phenobarbital decreases when taken simultaneously with reserpine, increases when combined with nialamide, diazepam, chlordiazepoxide.

Reduces the effectiveness of oral contraceptives and salicylates.

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

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

The hypnotic effect of phenobarbital is reduced when taken simultaneously with atropine, dextrose, thiamine, nicotinic acid, analeptics and psychostimulants.

Reduces the antibacterial activity of antibiotics and sulfonamides, the antifungal effect of griseofulvin.

Phenobarbital is a drug that has an antiepileptic effect. Available in the form of tablets and powder substance.

Pharmacological action of Phenobarbital

The active ingredient of the drug in all forms of release is phenobarbital.

In accordance with the instructions, Phenobarbital has sedative, hypnotic, antispasmodic, muscle relaxant and anticonvulsant properties. The medicine is a long-acting barbiturate.

When used, Phenobarbital changes the functional state and suppresses the sensory zone of the cerebral cortex, and also inhibits motor activity. The drug helps reduce the excitability of neurons in the epileptogenic focus and reduces the spread of nerve impulses.

The anticonvulsant effect of Phenobarbital is due to blunting of mono- and polysynaptic transmission in the central nervous system. The drug reduces the tone of smooth muscles of the gastrointestinal tract. In small doses, it reduces the intensity of metabolic processes, which manifests itself in the form of slight hypothermia.

Phenobarbital is an inducer of microsomal oxidation enzymes in the liver, thereby increasing its detoxification function and reducing the concentration of bilirubin in the blood serum.

When administered orally, Phenobarbital is absorbed slowly. Reaches maximum concentration in plasma after 1-2 hours, binds well to blood proteins. Metabolized in the liver. Active substance accumulates in the body. It is excreted through the kidneys in the form of glucuronide. The period of complete elimination is 4-8 days. Penetrates through the placental barrier and into breast milk.

Indications for use of Phenobarbital

According to the instructions, Phenobarbital is prescribed for the treatment of:

Focal seizures in adults and children;
Generalized tonic-clonic seizures;
Neurovegetative disorders;
Encephalitis caused by mononucleosis, whooping cough, chickenpox, rubella, measles or influenza;
Alcohol withdrawal;
Tremors, convulsions of various origins, agitation, fear, anxiety, tension, insomnia;
Chronic intrahepatic cholestasis;
Hyperbilirubinemia, including congenital non-hemolytic conjugated;
Spasms of peripheral arteries and spastic paralysis;
Epilepsy.

Methods of using Phenobarbital and dosage

As a sedative, Phenobarbital is taken at a dose of 30-50 mg 3 times a day.

For epilepsy, the medicine is prescribed 50-100 mg 2 times a day.

For sleep disorders, the daily dose is 150-300 mg, divided into 3 doses.

Children should take the drug 2 times a day 30-40 minutes before meals. A single dosage is prescribed depending on the age of the child:

Up to 6 months – 5 mg;
From 6 months to 1 year – 10 mg;
From 1 to 2 years – 20 mg;
From 3 to 4 years – 30 mg;
From 5 to 6 years – 40 mg;
From 7 to 9 years – 50 mg;
From 10 to 14 years – 75 mg.

Side effects of Phenobarbital

According to reviews, side effects from the body may occur during therapy with Phenobarbital:

Cardiovascular system: arterial hypotension;
Hematopoietic organs: thrombocytopenia, megaloblastic anemia, agranulocytosis;
Gastrointestinal tract: nausea, constipation, vomiting, with prolonged use – liver dysfunction;
Musculoskeletal system: with long-term treatment – osteogenesis disorders and the development of rickets;
Central nervous system: syncope, depression, hallucinations, nystagmus, ataxia, weakness, dizziness, asthenia;
Allergic reactions: difficulty breathing, swelling of the face, urticaria, skin rash, rarely - malignant exudative erythema.

Reviews of Phenobarbital report that with prolonged use the drug causes drug dependence.

Contraindications to the use of Phenobarbital

Contraindications to Phenobarbital according to the instructions are:

Broncho-obstructive pulmonary diseases;
Hyperkinesis;
Severe anemia;
Pregnancy;
Thyrotoxicosis;
Lactation;
Drug addiction;
Myasthenia;
Chronic alcoholism;
Porphyria;
Hypersensitivity to the components of the drug;
Severe liver or kidney failure.

Phenobarbital overdose

When used in large quantities side effects Phenobarbital may cause: pulmonary edema, disorder of electrical activity of the brain, confusion, cyanosis, oliguria, constriction of the pupils, decreased blood pressure, respiratory depression, drowsiness or agitation, loss of reflexes, weakness, lethargy, headaches, dizziness, ataxia, nystagmus. Treatment is symptomatic.

According to reviews, Phenobarbital in a dose of more than 2 g is fatal.

Phenobarbital analogues

In terms of pharmacological action, analogues of Phenobarbital are Luminal, Barbital and Dormiral.

Additional Information

With long-term use of Phenobarbital, liver damage is possible.

During treatment with the drug, alcohol consumption is contraindicated.

The medicine affects the speed of psychomotor reactions, which is important to take into account for people whose activities involve driving heavy machinery and vehicles.

The instructions for Phenobarbital indicate that the product should be stored in a dark, dry place out of reach of children.

Dispensed from pharmacies with a doctor's prescription.

Shelf life – 5 years.