- Drug habituation and physical dependence
- withdrawal syndrome ( withdrawal syndrome) phenobarbital
- Interaction of phenobarbital with other drugs. Phenobarbital and caffeine
The site provides reference information for informational purposes only. Diagnosis and treatment of diseases should be carried out under the supervision of a specialist. All drugs have contraindications. Expert advice is required!
What is phenobarbital? Pharmacological group and mechanism of action of the drug
Phenobarbital – synthetic drug from the group barbiturates, which is currently used as an antiepileptic drug. The drug was released in 1912 in Germany under the trade name Luminal. At the time of its discovery, the drug was used as a hypnotic and sedative ( sedative) remedy, while today, due to the large number of side effects, it is practically not used for these purposes.Phenobarbital is available and effective drug. It has many beneficial effects in different situations. It is part of such popular drugs as valocordin and corvalol. However, along with all the benefits, it disrupts memory, concentration, and is also addictive with prolonged use. Therefore, today the use of this drug is gradually abandoned.
The active substance of the drug is phenobarbital. Mechanism of action. The main effects of the drug
Phenobarbital is a white, odorless, crystalline powder with a bitter taste. It is practically insoluble in cold water, so it is not used in powder form. The drug is used in the form of tablets with a small dosage. The drug acts directly on receptors in the central nervous system, which is why the use of phenobarbital in large doses is very dangerous.The active substance of the drug interacts with gamma-aminobutyric acid receptors ( GABA) in the central nervous system. This substance is the main inhibitory neurotransmitter of the nervous system ( information carrier molecule). The action of GABA is to interrupt the nerve impulse of any nature ( motor, psycho-emotional). Falling asleep, blocking negative emotions, reducing stress levels - all these processes are controlled by this neurotransmitter. Phenobarbital increases the sensitivity of cell membrane receptors to GABA in the central nervous system, and also prolongs its action.
The main effects of the drug, due to the effect on GABA receptors, include:
- sedative action. The drug inhibits almost all processes in the brain. Decreased reaction rate, motor activity. When it is used, the sensory areas of the cerebral cortex are suppressed. This also manifests itself in minor analgesia ( decreased response to pain stimulus). This effect is manifested in a decrease in irritability, excitement, as well as the appearance of drowsiness.
- Sleeping action. It is caused by inhibition of cells of the brain stem, nuclei of the thalamus and their interaction with the cerebral cortex. Despite the fact that the hypnotic effect of this drug is quite pronounced, the sleep achieved as a result of its use differs from the physiological one. It is less deep, and, accordingly, restores the energy reserves of a person worse.
- Anticonvulsant action. The drug is one of the main treatments for epilepsy. This disease occurs due to the appearance of abnormal nerve impulses in various areas of the nervous system, which lead to uncontrolled motor activity ( convulsions). Barbiturates reduce the excitability of neurons and block the emergence and propagation of nerve impulses.
The effect of phenobarbital on the liver ( normalization of bilirubin levels)
Phenobarbital is an inducer ( accelerator) microsomal oxidation enzymes in the liver. This means that the processes of oxidation, reduction and transformation of various substances in the liver occur faster. As a result, the elimination of toxins and medicinal substances through the liver is accelerated. Therefore, when using various drugs in conjunction with phenobarbital, their activity may decrease. After 3-5 days of using the drug, the rate of enzymatic changes can increase by 10-12 times.Bilirubin is one of the derivatives of hemoglobin that appears in the blood after the destruction of red blood cells. For a number of diseases including hemolytic jaundice of newborns) increases the amount of bilirubin in the blood. Phenobarbital speeds up metabolism ( metabolism) in relation to bilirubin and quickly remove it from the body.
The effect of the drug on the cardiovascular system
In normal doses, the drug does not have a specific effect on the cardiovascular system. However, it is believed that it can be effective in neurovegetative vascular disorders, as it can relieve spasm of vascular smooth muscles. This effect is not the main effect of the drug, when using it, the patient will inevitably feel drowsiness and sedation from the drug. Despite this, such recognized drugs as Corvalol and Valocordin, containing phenobarbital, have gained popularity precisely as drugs that alleviate the state of the cardiovascular system.In high doses, the drug depresses the vasomotor center, which reduces blood pressure and heart rate. The use of the drug in large doses is fraught with respiratory arrest and heartbeat, therefore, when taking it, it is necessary to carefully monitor the amount of medication taken.
The release form of the drug ( tablets 5 mg, 50 mg and 100 mg)
The drug is produced exclusively in the form of tablets with an active ingredient content of 5, 50 or 100 mg. The dosage of the drug in 5 mg is intended for use in childhood. The drug is packed in cardboard boxes with 6 or 10 tablets each. The tablet has a flat-cylindrical shape with a risk for accurate division in half.Phenobarbital tablets also contain excipients that help maintain the desired form of the drug for a long shelf life. These include sucrose, starch, talc, stearic acid. The shelf life of the tablets is 5 years when stored at a temperature not exceeding 25 degrees ( at room temperature).
How does the drug enter the bloodstream and is excreted from the body?
The drug is used for oral administration. After taking the tablet, it is completely but slowly absorbed in the small intestine. The intestinal wall is rich in blood vessels, so immediately after this the drug is in the blood. Therapeutic drug concentration ( for epilepsy and seizures) should be 10 - 40 mcg / ml of blood. After that, it is distributed to all organs and tissues and enters the brain, passing through the blood-brain barrier. The drug is stored in the body for a very long time. Middle period its half-life ( the time it takes for the plasma concentration of a drug to be halved) in adults is 80 hours, and in children - 110 hours. Thus, the drug is excreted from the body for a very long time even with optimally functioning liver and kidneys, so it is used in small doses. In addition, the drug is prone to cumulative effect, which means that when it is used again, the effect of previous applications is added.The drug is excreted by the kidneys unchanged ( about 50%), as well as in the form of specific compounds. They are biologically inactive, formed in the liver after a series of chemical transformations. With prolonged use of the drug, the enzymes of the liver cells are activated, which accelerates its excretion from the body. Despite this, it still takes quite a long time. That is why a person can feel the effect of the drug for a long time after taking just one tablet.
Is phenobarbital a drug? Determination of phenobarbital in urine
Phenobarbital can indeed cause hallucinations, impaired consciousness and various mental reactions. Its long-term use leads to addiction, as a result of which the circulation of this drug has been limited. Today it can only be purchased with a doctor's prescription. In 2013, it was included in the list of narcotic and psychotropic drugs subject to control in Russian Federation. Also, the drug is banned for import in a number of countries, for example, in the USA. Therefore, when using phenobarbital, as well as combined preparations with its content ( primarily, Corvalol and Valocordin) must be responsible for all risks associated with its use.The test for the presence of phenobarbital in the urine is sometimes used by narcologists to confirm the state of drug intoxication. This testing is performed only by appropriate medical personnel for good reasons ( e.g. being involved in a traffic accident while intoxicated). However, it should be borne in mind that phenobarbital can be in the urine and with the usual use of drugs containing this substance ( pentalgin, corvalol) for their intended purpose. In any case, when using phenobarbital, you need to carefully control your actions ( the drug can change the perception of reality, impair memory and attention).
Phenobarbital analogues
Currently, there are many analogues of this drug, which have quite large advantages over phenobarbital. Today, you can choose a more effective and safer analogue of this drug with respect to any of its effects. There are very good hypnotics, anti-epileptics and sedatives that do not have the side effects of this drug and are more effective.From modern sleeping pills, such drugs as zolpidem, methaqualone, nitrazepam should be preferred. Their advantage is due to selectivity ( selectivity) actions, they act only on the processes associated with brain activity during sleep. At the same time, the use of phenobarbital as a sleeping pill leads to a large number of side effects due to the lack of selective action. Sleep caused by barbiturates is different from natural and does not give the desired recuperation.
It is not recommended to use phenobarbital as a sedative, it is better to resort to herbal preparations ( preparation of valerian, motherwort, mint). Phenobarbital may have a better temporary effect, but its long-term use is addictive and can lead to depression or mental disorders.
Finally, among antiepileptic drugs, phenobarbital still has not lost its relevance, despite the fact that it is no longer considered a first-line drug. It has been proven that its use in children can lead to mental retardation, disrupt memory, attention, school performance. Today, topiramate, gabapentin, carbamazepine and some other drugs are used as anticonvulsants.
Phenazepam and phenobarbital
Phenazepam is similar to phenobarbital in its mechanism of action, it also increases the inhibitory effect of GABA on the nervous system. Therefore, the indications for their use are largely the same. However, phenazepam belongs to the group of tranquilizers, its effect on the nervous system is several times stronger than that of phenobarbital. It is used for severe psychoses, obsessions, phobias, neurotic conditions, that is, in much more severe cases. At the same time, this drug is more difficult to tolerate than phenobarbital. Therefore, in cases where the use of phenobarbital can be dispensed with, this drug should be preferred.Preparations containing phenobarbital ( valocordin, corvalol, andipal, pentalgin, bellataminal). Interaction of phenobarbital with paracetamol
This drug is very often used as part of combined preparations, since it can reduce the symptoms of almost any disease, due to the sedative and vasodilating effect. The hypnotic effect helps to immerse a person in sleep, which favorably affects the cure. On the other hand, today phenobarbital is recognized as a psychotropic drug, which is why its distribution has become limited. Therefore, today it is less and less often included in the composition of combined preparations.Phenobarbital is part of the following medicines:
- Valocordin and Corvalol. These preparations contain about 20 mg of phenobarbital in 1 ml of solution. They are taken for tachycardia, functional disorders of the cardiovascular system. They also make it easier to fall asleep. As additional active substances, they use peppermint oil ( has a vasodilating effect) and ethyl bromoisovalerianate ( sedative).
- Andipal. The drug is used as an antispasmodic for migraine and mild forms of hypertension. It additionally includes painkillers ( analgin) and antispasmodics ( dibazole, papaverine).
- Pentalgin, trialgin, tetralgin and other painkillers. This substance is used in a number of painkillers. Thanks to additional components, these drugs have anti-inflammatory, antipyretic and tonic effects. The use of phenobarbital together with paracetamol enhances its analgesic effect, since it is achieved at two levels, in the region of peripheral receptors and at the level of the central nervous system. However, phenobarbital increases the rate of elimination of paracetamol from the body, which may reduce its effectiveness.
- Bellataminal. This substance contains belladonna alkaloids, ergotamine and phenobarbital. The drug is used for neurosis, insomnia, during menopause in women. It reduces the excitability of many receptors and has a sedative and hypnotic effect.
Indications for the use of phenobarbital
Phenobarbital can be used to achieve various effects. Today, the only real use of the drug remains as an antiepileptic agent. It helps to cope with cramps and muscle spasms. However, it remains possible to use phenobarbital as a hypnotic, with psycho-emotional arousal and in some other cases. The drug is indicated for use in the following cases:
- epilepsy;
- chorea;
- cramps and muscle spasm;
- excitement, anxiety, tension, fear;
- sleep disturbance;
- hyperbilirubinemia ( hemolytic disease of the newborn, Gilbert's syndrome).
epilepsy and phenobarbital
Epilepsy is a chronic neurological disease characterized by sudden seizures. They occur due to an increase in the activity of certain neurons in certain areas of the cerebral cortex, which is why they generate an unusually large number of nerve impulses. They are manifested by increased uncontrolled motor activity ( epileptic fit). In addition, with epilepsy, changes in the human psyche can occur ( fear, sadness, increased irritability and aggressiveness).This substance remains one of the main drugs in the treatment of epilepsy, since it acts on the cause of the disease. Phenobarbital reduces the excitability of the motor centers of the brain, which is why epileptic seizures occur very rarely or completely stop. The daily dose of the drug depends on the frequency of seizures, however, in any case, the treatment of epilepsy with phenobarbital is very long. Today, the use of this drug in children for the treatment of epilepsy is being tried to be limited, since it inevitably slows down the mental and mental development of the child.
Phenobarbital for seizures and muscle spasm
Cramps are involuntary muscle contractions that can be accompanied by pain. There are spasms of skeletal muscles and smooth muscles ( blood vessels, bronchial walls, intestines). There are many causes of seizures other than epilepsy. They can occur with meningitis, eclampsia, the action of certain toxins and poisons ( e.g. strychnine). Muscle twitches can also be caused by electrolyte imbalance ( magnesium deficiency). In most cases, the use of phenobarbital helps to relieve muscle spasm and stop cramps.Chorea is a disease characterized by erratic, uncontrolled, jerky movements. It occurs due to a violation of nerve transmission in the region of the nuclei of the brain stem, as well as an increase in the sensitivity of receptors to dopamine. The frequency and amplitude of choreic movements can be reduced by taking anticonvulsants, including phenobarbital.
The anticonvulsant effect of the drug is due to the inhibition of the motor areas of the cerebral cortex. Taking phenobarbital tablets for seizures may be done to relieve symptoms rather than as part of a course. There are special blends for example, a mixture of Sereysky), which are used both for the treatment of epilepsy and for the temporary relief of seizures.
Use of phenobarbital for eclampsia
Eclampsia is an abnormal condition of the mother during pregnancy or in the postpartum period, which is characterized by seizures and an abnormal increase in the mother's blood pressure. This condition threatens the life of a pregnant woman and her fetus. The reasons for this phenomenon are not clear. Eclampsia is manifested by convulsions with loss of consciousness, cessation of breathing. Phenobarbital in this condition allows not only to reduce contractions of skeletal muscles ( convulsions), but also relieve spasm of blood vessels and bronchi. Thus, the use of the drug in eclampsia reduces blood pressure and makes breathing easier.The use of the drug for insomnia as a sleeping pill. The effect of the drug on sleep
Sleep is a physiological oppression of consciousness, during which the energy reserves of the body are restored. The sleep process is based on the physiological processes of the nervous system, which are expressed in an increase in the activity of certain ( so-called hypnogenic, responsible for sleep) areas of the brain and a decrease in the activity of other structures. Phenobarbital does indeed have a pronounced effect on sleep. Its reception causes drowsiness and can be used for various sleep disorders. For a long time, barbiturates were the only sleeping pills. The action of the drug develops 20-30 minutes after administration and lasts about 7-8 hours.Today it is known that sleep is an alternation of two phases ( fast and slow sleep ). Both phases are necessary, but the most important is REM sleep, which eliminates fatigue and reduces stress levels. The entire cycle lasts about an hour and a half. Both phases are necessary for full sleep, while the use of barbiturates shortens the REM phase and changes the duration of the cycles. Therefore, when using phenobarbital, a person wakes up broken, tired, drowsiness persists. There may be a decrease in performance and a deterioration in mood. With prolonged use, addiction, physical and mental dependence occurs. Thus, the use of this drug adversely affects sleep, and today it is less and less recommended for use as a sleeping pill.
The use of the drug in hyperbilirubinemia ( Gilbert's syndrome, hemolytic disease of the newborn)
Hyperbilirubinemia is a condition in which the amount of bilirubin in the blood rises. This pigment has a yellow color, therefore, with an increase in its content in the blood, the skin sometimes turns yellow ( jaundice sets in). The level of bilirubin in the blood can increase in various diseases of the liver and biliary tract or in physiological conditions, such as Gilbert's syndrome and hemolytic disease of the newborn. Phenobarbital can be used for both conditions, as it speeds up the excretion of bilirubin from the body.Gilbert's syndrome is a congenital feature of the body, which is characterized by the accumulation of bilirubin in tissues, a change in skin color due to a violation of its metabolism. This benign disease can be passed from parents to children. It practically does not affect the state of health and quality of life, except for changes in skin color ( may have varying degrees of manifestation).
Hemolytic disease of the newborn is one of the causes of jaundice in newborns. It is observed as a result of the Rh conflict between the mother and the fetus, resulting in a massive destruction of red blood cells and the release of hemoglobin. Hemoglobin is one of the main sources of bilirubin, which is why this condition is accompanied by severe jaundice. Bilirubin in high concentrations becomes toxic, so phenobarbital is used to treat this disease, which helps to remove it from the body.
Phenobarbital increases the enzymatic activity of liver cells, due to which bilirubin is captured from the blood and excreted faster and almost completely. Due to this, the level of bilirubin decreases, and the yellowness of the skin disappears. It should be noted that the drug is effective only if there are no organic diseases of the liver and biliary tract ( e.g. hepatitis, cholecystitis). With Gilbert's syndrome, the drug is taken at night in an amount of 50 mg, which allows it to be used for a long time.
Contraindications to the use of phenobarbital
Phenobarbital, despite the large number of side effects, has a rather limited list of contraindications. This is due to the fact that the drug, acting on the nervous system, interacts very limitedly with other metabolic processes. However, in any case, before using the drug, you should make sure that there are indications and the absence of contraindications to its use. The drug is contraindicated in the following diseases and conditions:
- Hypersensitivity and allergic reactions to barbiturates. Allergy to the drug is a logical contraindication. Repeated use of the drug can cause such serious reactions as anaphylactic shock, Quincke's edema. They threaten a person's life and may require urgent assistance.
- Porfiry. Porphyria is a hereditary disorder of pigment metabolism, which can be aggravated in case of taking phenobarbital. This is due to the fact that the drug activates enzymes that synthesize porphyrin ( pigment, the content of which is increased in this disease).
- Severe anemia. When using the drug, blood pressure decreases. Anemia ( reduced number of red blood cells) is almost always compensated by increased pressure to maintain oxygen supply to organs and systems. The use of the drug violates this compensatory mechanism.
- Severe respiratory failure and shortness of breath. Phenobarbital suppresses the respiratory center, which reduces the frequency of breathing. As a result, the human body can suffer from a lack of oxygen, which can lead to serious disruption of its work.
- Liver or kidney failure. In severe disorders of renal or hepatic activity, the effect of the drug is markedly prolonged, it becomes toxic. The effect of inhibition of the central nervous system can last more than a day, which is unacceptable.
- Myasthenia. This drug depresses the motor areas of the cerebral cortex, so its use in muscle weakness can significantly worsen the condition.
- Alcoholism, as well as other drug or drug addiction. The drug is a psychotropic substance, so its use in a group of patients suffering from any addiction is strictly prohibited. This drug may be habit-forming.
In what cases should the use of the drug be limited?
There are a number of conditions that are not direct contraindications, but in which you need to be careful in using this drug. If available, you should use analogues or take this medicine only after consulting a doctor or pharmacist. This is because such conditions create an increased risk of side effects.The drug should be used with caution in the presence of the following conditions or diseases:
- Depression, sudden mood changes, suicidal tendencies. The drug can affect a person's mental health in the most unexpected way, most often negatively. With psychological instability, the risk of this phenomenon increases.
- History of liver and kidney disease. Any violation of these organs can theoretically reduce the rate of excretion of a substance from the body.
- Hyperthyroidism. Barbiturates are transported by plasma proteins, as are thyroid hormones ( thyroxine). Taking phenobarbital displaces thyroxine from its association with blood plasma proteins, which may cause symptoms of intoxication with this substance to suddenly appear.
- Hypofunction of the adrenal glands. When using phenobarbital, the systemic action of adrenal hormones decreases, which worsens the course of this disease.
- The presence of acute or chronic pain. The drug does not eliminate the source of pain, it changes its perception by the central nervous system. Thus, important symptoms of the disease can be hidden or time is lost in which the underlying disease will progress.
Phenobarbital for diabetes
The use of this drug in diabetes is not prohibited, but should be done with caution. The drug affects the synthesis of cortisol - one of the hormones of the adrenal glands. This hormone regulates blood sugar levels. Taking the drug can reduce the level of cortisol, respectively, with this, the level of sugar in the blood decreases. Against the background of taking insulin, this can lead to hypoglycemia - a condition in which the amount of glucose in the blood is significantly lower than normal. Hypoglycemia is characterized by dizziness, nausea, weakness, disorientation in space. Taking the drug against the background of diabetes is allowed only for those patients who independently monitor the level of glucose in the blood.Can the drug be used during pregnancy? Does the drug pass into breast milk?
The drug is strictly not recommended for use during pregnancy. It has been proven that in the case of use in the first trimester of pregnancy, the development of various anomalies in the fetus is possible. The drug passes through the placental barrier, distributed throughout all tissues of the fetus ( the highest concentration is found in the liver and brain). When used in the third trimester of pregnancy, the development of physical dependence in the fetus and withdrawal syndrome after birth is possible.The drug can lead to a violation of blood clotting in a child ( due to a deficiency of vitamin K, which is synthesized in the liver), as well as respiratory problems. The drug also passes into breast milk, therefore, at the time of breastfeeding, the mother should stop taking the drug. Its use during pregnancy or lactation is possible only if there are strict indications, when the potential benefit outweighs the risk.
Can the drug be used in children?
There is a special medicinal dose of the drug ( tablets 5 mg) intended for the treatment of children. However, today the drug is practically not used in childhood. This is due to the fact that it has a large number of side effects, slows down the processes of mental and physical development. To date, the relevance of its use in children only as an antiepileptic agent remains, but there are safer analogues that have replaced phenobarbital in this area. It is worth noting that this drug at a dosage of 5 mg for children is still used in antiepileptic hospitals, but it is rarely sold in pharmacies.Instructions for using the drug. Applicable dosages
Phenobarbital is a potent drug that has a depressant effect on the central nervous system. Even when used correctly, its use can cause a large number of side effects. That is why it is important to observe the dosage, as well as to take it in accordance with the instructions. The effectiveness of treatment and the overall impression of the patient from the drug depends on this. The dose and route of administration are selected individually depending on the goals of treatment, as well as the age and anthropometric data of patients.
However, standard doses are usually used for adults, and several times smaller for children. On sale there are three types of tablets of the drug with different contents of the active substance. This makes it easier to use. Long-term use of the drug should be carried out only under the supervision of a physician.
Taking the drug as a sleeping pill
When using the drug as a sleeping pill, it is prescribed to adults at a dosage of 100 mg 1 hour before bedtime. The tablet should be washed down with water, taking the drug does not have to be associated with food intake. For children, a dose of 5 mg is also provided, but today doctors do not recommend the use of this sleeping pill in children. The drug can be used every day for no more than a week, otherwise there may be various side effects ranging from mood disorders to addiction.Taking the drug in the form of a sedative and antispasmodic ( relieves muscle spasm)
As a sedative and antispasmodic, phenobarbital is used only in adults. To achieve this effect, the drug can be taken 2-3 times a day. Its dosage in this case is from 20 to 30 mg, that is, half a tablet with an active ingredient content of 50 mg. It is in this amount that the drug is found in most combined drugs ( valocordin, corvalol, pentalgin), since it is included in their composition to achieve similar effects. It goes well with vasodilators, antispasmodics for various neurovegetative disorders. In case of violations of this nature, the drug is used as a symptomatic agent, its administration is stopped after the symptoms have been eliminated.Taking the drug in the form of an antiepileptic drug
As an antiepileptic drug, the drug is used in adults and children with seizures. Treatment begins with a daily dose of 50 mg, divided into 1 to 3 doses. Increasing the dose of the drug should be gradual. If necessary, increase the dose until the seizures stop ( usually 200 mg 2 to 3 times a day is sufficient). Treatment with the drug is long-term, and also involves maintaining therapeutic doses even after the disappearance of the symptoms of the disease. Stopping phenobarbital should be gradual, as abrupt interruption of its use can lead to an epileptic seizure or even status epilepticus ( the most dangerous manifestation of the disease).For children, much smaller doses are used. Usually they are determined at the rate of 3 - 5 mg / kg of body weight per day. This dose is divided into three doses. It may take about half an hour to achieve the effect of the drug. When calculating dosages, it is very important not to exceed the allowable daily and single doses, as this can lead to overdose, respiratory depression, palpitations, low blood pressure and other dangerous phenomena.
The highest single and daily dose of the drug ( WFD and VSD)
For potent and toxic drugs in medicine, the concepts of the highest single and daily dose have been established. They establish the maximum allowable amount of a medicinal substance that a patient can take at a time and during the day. Their excess poses a threat to the health of the patient. Doctors rarely prescribe higher doses, most often they use average therapeutic doses, 2 or more times less than the highest doses. Knowledge of the highest single and daily doses is within the competence of doctors and pharmacists, but it is also useful for the patient as a person interested in maintaining his health.The highest single oral dose for phenobarbital is 200 mg. The highest daily dose of the drug is 500 mg. These values are indicated for adults, while for children they are several times less. If a patient is prescribed a drug in excess of the highest daily or single dose, it is necessary to double-check the doctor's prescription and clarify the prescription.
Can I drive machinery, including a car, after taking the drug?
The drug significantly affects mental activity, as well as concentration. It inhibits the transmission of nerve impulses, which reduces the reaction rate. That is why driving a car, as well as any work that requires increased concentration of attention, is impossible when using this drug. However, with prolonged use of this drug, during course therapy, the body adapts to some extent to its constant presence in the body, due to which memory, attention and reaction speed are restored to a large extent. Thus, restrictions on the control of mechanisms are partially removed. However, it should be noted that epilepsy, which is often treated with phenobarbital, is a medical contraindication to driving in the Russian Federation.How should the drug be stored?
The drug belongs to potent and toxic substances, therefore, when storing it, special precautions must be observed. It should not fall into the hands of children or random people who might use it. Proper storage of the drug involves its being in a cool, dry place, protected from direct sunlight. The storage temperature of the drug is room temperature, from 15 to 25 degrees. With proper storage, you can guarantee its safety during the entire shelf life.Expiry date of the drug
The shelf life of the drug in the form of tablets is 5 years from the date of packaging. It is possible that the drug remains active for a longer period, since the shelf life of the drug in the form of a powder ( not released today) was 10 years. However, it should be borne in mind that during transportation, the storage conditions of the drug may not be ideal, so you should not take the drug with an expired shelf life. It can be dangerous to health and ineffective in treatment.Side effects of the drug. Psychotropic effect of phenobarbital. Addictive effect and drug withdrawal syndrome
Phenobarbital is considered a potent and rather dangerous substance due to the fact that it affects the receptors of the nervous system. It is included in the list of psychotropic substances, since its long-term use can be addictive. In addition to affecting the psyche, it can affect various systems and organs at the time of their admission. However, most often, patients report side effects associated with disorders of the nervous system and sensory organs. Side effects of phenobarbital are expressed in violation of the following organs and systems:
- Nervous system. The drug can cause hallucinations, nightmares, headache, nervousness, anxiety, irritability. The drug leaves an aftereffect - fatigue, fatigue, decreased memory and concentration. Paradoxical reactions are sometimes noted, especially in children - unusual arousal and insomnia.
- The musculoskeletal system. The drug causes muscle weakness, and with prolonged use affects the development of bones in children, can lead to rickets.
- The hematopoietic system. Rarely, the drug leads to a decrease in the production of red blood cells, platelets, white blood cells in the bone marrow, however, such cases have still been noted.
- Respiratory system. The drug can cause difficulty in breathing, as it depresses the respiratory center.
- The cardiovascular system. Phenobarbital leads to a drop in blood pressure, for hypotensive patients such a decrease can become critical.
- Digestive system. The drug can cause vomiting, constipation. Prolonged use depletes the resources of the liver, may cause yellowness of the eyes and skin.
- Allergic reactions. Rarely, this drug can become a source of allergies. In this case, develop various manifestations allergies, skin rashes ( hives) to anaphylactic shock. These reactions are especially likely if the patient has bronchial asthma or other allergic diseases.
Drug habituation and physical dependence
Drug addiction is one of the main problems for the widespread use of phenobarbital. It has been proven that the use of the drug in high doses leads to the development of physical dependence in 75% of cases. At the same time, the use of the drug as part of a course therapy, even at medium doses, can be addictive. This property in barbiturates is even more pronounced than in alcohol.The risk of addiction increases with the use of large doses of phenobarbital and an increase in the duration of administration. Also, patients with any other drug or alcohol dependence may develop addiction to phenobarbital with a high probability. Dependence on phenobarbital is physical in nature. This means that over time, tolerance to the active substance increases, and when it is canceled, a complex of negative symptoms appears, which is called the withdrawal syndrome.
withdrawal syndrome ( withdrawal syndrome) phenobarbital
Withdrawal syndrome is a group of symptoms that occurs when the use of the drug is stopped or the dose is sharply reduced. This symptom is characteristic of many psychotropic substances, including phenobarbital. Withdrawal syndrome is one of the manifestations of drug dependence. The withdrawal syndrome in the case of this drug develops 8 to 12 hours after its final administration. To prevent it during long-term treatment with phenobarbital, it is recommended to gradually reduce the dose until it is completely discontinued.Withdrawal syndrome of phenobarbital is accompanied by the following symptoms:
- anxiety;
- muscle twitches ( hand tremor);
- weakness;
- dizziness;
- nausea and vomiting;
- convulsions.
Interaction of phenobarbital with other drugs. Phenobarbital and caffeine
This drug enhances the activity of the liver in the biotransformation of many drugs. Because of this, their elimination is accelerated and their effectiveness is reduced. This applies to anticoagulants, corticosteroids, antidepressants, antibacterial drugs, anti-inflammatory drugs ( paracetamol). The drug significantly reduces the effect of the antifungal drug griseofulvin.The drug does not combine well with most anticonvulsants, since it can either increase or decrease their concentration in the blood. In addition, an additional inhibitory effect on the nervous system is possible when combined. The action of phenobarbital is prolonged by the use of monoamine oxidase inhibitors, which counteract its enzymatic breakdown in the liver.
Phenobarbital and caffeine are opposite to each other in action. Caffeine tones the body and stimulates nervous processes, eliminating drowsiness. That is why the use of caffeine reduces the hypnotic effect of phenobarbital. However, caffeine can be used to eliminate residual effects after taking phenobarbital.
Can I take phenobarbital with alcohol?
Alcohol is prohibited for use with this drug. This is due to the fact that when they are used together, the depression of the central nervous system increases and the risk of side effects increases. Residual effects after using the drug in this case last longer. In addition, when they are used together, the risk of addiction and the appearance of a withdrawal syndrome after stopping the use of phenobarbital increases several times.Phenobarbital poisoning. Antidote for poisoning
Symptoms of drug poisoning appear a few hours after ingestion. The toxic dose in case of poisoning can vary significantly and is individual. Usually, 1 gram of the active substance is enough for poisoning. Phenobarbital poisoning is characterized by severe impairment of consciousness up to its loss, dizziness, weakening or absence of reflexes. In case of poisoning with this substance, pressure drops, breathing worsens, and the heart rate decreases. In the worst case, coma and death occur.There is no specific antidote for phenobarbital, therefore, in case of overdose and poisoning, it is necessary to accelerate its excretion from the body as quickly as possible. It is necessary to induce a gag reflex, and also give the patient activated charcoal or other sorbents. You can do gastric lavage. The patient is given diuretics, as well as a large amount of fluid to restore water and electrolyte balance. If necessary, carry out artificial ventilation of the lungs and correction of blood pressure levels.
What is the lethal dose of phenobarbital?
A lethal outcome can occur with a single dose of more than 2 grams of the substance. In order to prevent an overdose, it is necessary to monitor the integrity of the package and the amount of the substance taken with each use of the drug. It is important to store it in such a way as to prevent accidental ingestion by children or others. When treating with this drug, you must very strictly follow the doctor's recommendations and follow the doses indicated in the instructions.Prices for phenobarbital in various cities
The drug is relatively cheap and available for purchase. The price of the drug may differ depending on the city, region, as well as the average price level. However, in recent years, its prevalence in pharmacies has significantly decreased due to the inclusion of the drug in the list of psychotropic substances. That is why the sale of phenobarbital in pharmacies is currently significantly limited, far from all pharmacies today you can find this drug. The cost of the drug phenobarbital in the cities of Russia
City | Price of different dosages of phenobarbital |
||
Tablets 5 mg, 10 pieces | Tablets 50 mg, 10 pieces | Tablets 100 mg, 10 pieces |
|
Moscow | |||
Saint Petersburg | |||
Ekaterinburg | |||
Chelyabinsk | |||
Novosibirsk
| |||
Ufa | |||
Ulyanovsk | |||
Tver | |||
Penza | |||
Tambov | |||
Do I need a prescription to buy a drug at a pharmacy?
The active substance of the drug is recognized as a psychotropic substance. For these reasons, it is released in pharmacies only with a prescription. You will also need a prescription to buy combination drugs that include phenobarbital. Patients with epilepsy receive it, as a rule, in specialized dispensaries. That is why it is quite difficult to find the drug in free sale even with a prescription.Phenobarbital - medicinal product used in medicine as an anticonvulsant and hypnotic.
The active substance of the drug is phenobarbital - an odorless powder with a bitter taste. Reduces the level of motor activity, stops convulsive muscle contractions. When taking the drug, the smooth muscles of the gastrointestinal tract decrease.
In this article, we will look at why doctors prescribe Phenobarbital, including instructions for use, analogues and prices for this drug in pharmacies. Real REVIEWS of people who have already used Phenobarbital can be read in the comments.
Composition and form of release
The drug is sold in tablets and as a solution of 0.2%. In addition, there is such a form of release as a powder.
- one tablet contains: active substance: phenobarbital - 100 mg;
- excipients: sugar, calcium stearate, talc, potato starch.
Clinico-pharmacological group: hypnotic and sedative drug. Anticonvulsant.
Indications for use
Instructions for use indicate that Phenobarbital is used in the treatment of the following ailments and conditions:
- Hyperbilirubinemia;
- Chorea;
- spastic paralysis;
- sleep disorders;
- Adjuvant therapy in the treatment of tetanus;
- Emergency therapy aimed at relieving seizures caused by eclampsia, meningitis or epilepsy;
- Treatment of epilepsy (for the relief of generalized tonic-clonic seizures or focal seizures).
It is also prescribed for nervous exhaustion (used as a sedative to get rid of feelings of fear, constant anxiety and tension).
pharmachologic effect
Phenobarbital is a derivative of barbituric acid. It has a pronounced anticonvulsant effect, reduces the excitability of epileptic neurons, acts as an enzyme inducer, and increases the activity of the monooxygenase enzyme system.
Has a hypnotic effect. It inhibits the activity of the motor areas of the cortex and subcortex of the brain. Increases the content of the endogenous inhibitory mediator GABA in the central nervous system, reduces the excitatory effect on the central nervous system of amino acids.
Instructions for use
- sleep disorders: 0.1-0.2 g 0.5-1 hour before sleep.
- as a sedative drug: 0.05 g 2-3 times a day.
- as an anticonvulsant: 0.05-0.1 g 2 times a day. With a decrease in liver function, it should be prescribed in smaller doses.
With prolonged use of the drug, drug dependence may occur.
Contraindications
Among the restrictions for taking the medicine, it is worth noting:
- myasthenia gravis;
- depression;
- diabetes;
- porphyria;
- alcohol and drug addiction;
- children's age (due to the impossibility of accurate dosing);
- hypersensitivity (also to a different kind of barbiturates);
- severe liver and kidney failure;
- pregnancy and lactation;
- hyperkinesis.
Side effects
Judging by the reviews of Phenobarbital, the drug often causes a paradoxical reaction (unusual excitement) in debilitated patients, as well as in children. In some cases, prolonged use of the drug can cause nausea, constipation, vomiting, asthenia, weakness, dizziness.
Rarely - fainting, ataxia, depression, hallucinations, allergic reactions, hemolytic disorders. Prolonged use of the drug often leads to a violation of osteogenesis and contributes to the development of rickets.
In the case of toxic poisoning, symptoms may not appear for several hours. Ingestion of 1 g can lead to serious poisoning in adults. In turn, taking 2-10 g leads to death.
Phenobarbital's analogs
Structural analogues for the active substance:
- Luminal;
- Phenobarbital tablets for children.
Attention: the use of analogues must be agreed with the attending physician.
Phenobarbital is an antiepileptic drug that has a muscle relaxant, antispasmodic, sedative and hypnotic effect.
Release form and composition
Phenobarbital is available in the following dosage forms:
- tablets for children 5 mg: flat-cylindrical, white shade, have a chamfer (10 pieces in a blister pack, in a cardboard bundle 1, 2 or 1000 packs);
- tablets for children 50 mg: flat-cylindrical, white, have a chamfer and a risk (10 pcs in a blister pack, in a carton pack of 1, 2 or 1000 packs, in a carton box of 500 packs; 6 pcs in a blister pack , in a cardboard box 1000 packs);
- tablets 100 mg: flat-cylindrical, white, chamfered (6, 10 or 12 pcs. in a blister pack, in a carton pack of 1, 2, 3, 180 or 300 packs, in a carton box of 150 or 1000 packs; 10 pcs in a blister pack, in a carton pack 1, 2 or 3 packs, in a carton box 500 packs, 12 pcs in a strip, in a carton pack 1 strip).
1 Phenobarbital tablet contains:
- active substance: phenobarbital - 5/50/100 mg;
- auxiliary components: sucrose - 42.2 / 14.8 / 8 mg, potato starch - 11.3 / 32.3 / 40 mg, calcium stearate (for tablets 5 and 50 mg) - 1.5 / 2.9 mg, stearic acid (for 100 mg tablets) - 0.9 mg, talc (for 100 mg tablets) - 1.1 mg.
Indications for use
For adults:
- epilepsy (all types of seizures, excluding absences);
- spastic paralysis;
- convulsions of non-epileptic origin;
- chorea;
- increased anxiety, fear;
- psychomotor agitation;
- sleep disorders.
For children:
- partial and large epileptic seizures;
- insomnia;
- premedication;
- hyperbilirubinemia in chronic cholestasis and in newborns.
Contraindications
Absolute:
- severe renal and / or hepatic insufficiency;
- myasthenia gravis;
- acute mixed or intermittent porphyria (including a history of the disease);
- anemia with severe symptoms;
- respiratory diseases accompanied by shortness of breath and obstructive syndrome;
- drug or drug addiction, alcoholism (including history);
- diabetes;
- I trimester of pregnancy (possibly teratogenic effects on the fetus);
- lactation period;
- children's age (for tablets 100 mg);
- hypersensitivity to any of the components of the drug.
Relative:
- dysfunction of the liver and / or kidneys;
- hypofunction of the adrenal glands associated with a weakening of the systemic action of hydrocortisone of endogenous and exogenous origin when taking phenobarbital;
- acute and/or chronic pain syndrome;
- hyperkinesis;
- thyrotoxicosis (possibly increased signs of the disease);
- depression and/or suicidal tendencies;
- bronchial asthma in history;
- children's age (for tablets 5 and 50 mg);
- II and III trimesters of pregnancy.
Method of application and dosage
Phenobarbital is taken orally. The dosage is determined strictly individually, depending on age, individual sensitivity to the components of the drug, diagnosis, characteristics of the course of the disease, and so on. Treatment begins with the minimum effective dose, which is suitable for a particular form of pathology. In elderly patients, with reduced immunity, liver and / or kidney dysfunctions, therapy should be started with the lowest possible doses.
Depending on the diagnosis, Phenobarbital is prescribed for adults according to the following scheme:
- epilepsy, chorea, spastic paralysis, convulsions of non-epileptic origin: the initial dosage is 50-100 mg 2 times a day, then the daily dose is gradually increased until the seizures completely stop (the maximum daily dose is 500 mg), after which it is gradually reduced;
- sleep disorders: 100-200 mg 30-60 minutes before going to bed;
- fear, increased anxiety, psychomotor agitation: 30-50 mg 2-3 times a day.
The maximum daily dose for adult patients is 500 mg, the maximum single dose is 200 mg.
For children, the drug is prescribed in smaller doses in accordance with the age category. Do not exceed the maximum daily and single doses. The use of Phenobarbital requires a long course of therapy. With epilepsy, the drug is discontinued gradually, since a sudden cessation of its use can provoke a seizure and even cause status epilepticus. Phenobarbital is often an element of combination drug therapy. Typically, such combinations are selected individually depending on the general condition of the patient.
The dose for children is determined individually depending on the body weight and age of the child. The drug is taken on an empty stomach, 30-40 minutes before meals 2 times a day. Single and daily doses for patients childhood are respectively:
- children under 6 months: 5 and 10 mg;
- children 6 months to 1 year: 10 and 20 mg;
- children 1–2 years: 20 and 40 mg;
- children 3-4 years: 30 and 60 mg;
- children 5–6 years: 40 and 80 mg;
- children 7–9 years: 50 and 100 mg;
- children 10–14 years: 75 and 150 mg.
With depressed liver function, doses are reduced. As a hypnotic, Phenobarbital is prescribed to children at a dose of 5–7.5 mg in accordance with the age category. Long-term use of the drug as a sedative and hypnotic should be avoided due to its possible cumulation and drug dependence.
With hyperbilirubinemia in children, the drug is prescribed as follows:
- children under 12 years old: daily dose - 3-8 mg / kg, divided into 2-3 doses; if necessary, the dose is increased to 12 mg / kg; duration of therapy - 3-5 days;
- children over 12 years old: daily dose - 90-180 mg / kg, divided into 2-3 doses.
For premedication for children older than 6 months, the drug is prescribed at a dose of 1-3 mg / kg 1-1.5 hours before surgery.
When Phenobarbital is taken by children under 3 years of age, the required number of tablets must be ground to a powder, dissolved in a small amount of water and used as a suspension.
Side effects
- cardiovascular system: bradycardia, arterial hypotension;
- hematopoietic system: thrombocytopenia, megaloblastic anemia (with long-term treatment), agranulocytosis;
- nervous system and sensory organs: aftereffect (expressed in a decrease in concentration of attention and a slowdown in psychomotor reactions, a feeling of lethargy and weakness, asthenia), a violation of the thinking process, drowsiness, sleep disorders, anxiety, nervousness, dizziness, hyperkinesia (in children), ataxia, depression of the respiratory center, nystagmus, loss of consciousness, paradoxical reaction (especially in debilitated patients and elderly patients - agitation), nightmares, irritability, lethargy, depression, hallucinations, hand tremor, headache;
- digestive system: nausea, vomiting, constipation; with prolonged use - liver dysfunction;
- musculoskeletal system: development of rickets and osteogenesis disorders (with long-term therapy);
- allergic reactions: in rare cases, death is possible, Stevens-Johnson syndrome (exudative malignant erythema), shortness of breath, exfoliative dermatitis, local swelling (mainly lips, eyelids or cheeks), urticaria, skin rashes;
- other: withdrawal syndrome [minor symptoms (appear within 8-12 hours after discontinuation of the drug) - orthostatic hypotension, anxiety, nightmares, sleep disturbances, muscle twitches, restlessness, trembling in the hands, nausea, vomiting, dizziness, weakness, disorders vision; the main symptoms (manifest for 16 hours and last up to 5 days) - hallucinations, convulsions]; impotence, libido disorders.
To prevent the development of a withdrawal syndrome, the course of treatment with the drug should be completed gradually.
special instructions
The use of Phenobarbital during pregnancy is allowed only for strict medical reasons, if it is impossible to use other drugs. Taking this drug by pregnant women greatly increases the risk of fetal abnormalities.
With prolonged intrauterine exposure to Phenobarbital in newborns whose mothers took the drug in the third trimester of pregnancy, manifestations of physical dependence and acute withdrawal syndrome are possible, expressed in increased excitability and epileptic seizures immediately after childbirth or for 14 days after them.
The use of Phenobarbital for the treatment of seizures during pregnancy can cause clotting disorders in newborns due to a lack of vitamin K and often leads to bleeding in the neonatal period (usually within the first days after birth). The use of the drug during childbirth can lead to depression of the respiratory center in newborns, especially in premature infants, which is associated with underdevelopment of hepatic function.
At the moment, Phenobarbital is practically not used as a sleeping pill. If dermatological complications occur, the drug is canceled. Hypersensitivity reactions to the components of the drug are more common with a history of angioedema, urticaria, bronchial asthma, etc.
During therapy, regular checks of the complete blood count, liver and kidney function are necessary.
In debilitated and elderly patients, the appointment of Phenobarbital in normal doses can provoke confusion, depression or marked arousal. In children, taking the drug is sometimes accompanied by hyperactivity, irritability, and unusual arousal.
The risk of developing dependence is significantly higher when taking large doses of Phenobarbital and with an increase in the duration of therapy, as well as in patients with a history of alcohol and drug dependence. Regular use of the drug in doses 3-4 times higher than therapeutic leads to physical dependence in 75% of patients. Cancel Phenobarbital gradually, constantly reducing the dose for a long time, in order to avoid the manifestation of "recoil" and withdrawal syndromes. Sudden discontinuation of a drug for epilepsy may trigger a seizure or status epilepticus.
When using Phenobarbital in the course of treatment of epilepsy, it is desirable to control its content in the blood. With long-term therapy, it is recommended to periodically check the function of the liver and kidneys, the picture of peripheral blood, the content of folate in the blood.
If the drug must be used during childbirth, they should be taken with prepared resuscitation equipment.
The drug is forbidden to be used during work by drivers of vehicles, as well as people whose occupation requires increased concentration and immediate mental and physical reactions.
drug interaction
While taking Phenobarbital with other drugs, the following effects may be observed:
- valproic acid, phenytoin: an increase in the concentration of phenobarbital in the blood serum;
- griseofulvin, sulfonamides, antibiotics: a decrease in the effectiveness of the effects on the body of the latter;
- reserpine: decrease in the anticonvulsant effect of phenobarbital;
- psychostimulant drugs, analeptics, atropine, nicotinic acid, thiamine, dextrose, belladonna extract: reduction of the hypnotic effect of phenobarbital;
- chlordiazepoxide, amitriptyline, diazepam, nialamide: an increase in the anticonvulsant effect of the drug;
- salicylates, oral contraceptives: decreased effectiveness of the latter;
- acetazolamide: weakening the effect of phenobarbital;
- hypnotics and sedatives, alcohol, muscle relaxants, narcotic analgesics, neuroleptics: increased action of the latter;
- estrogens, indirect anticoagulants, doxycycline, glucocorticosteroids and other drugs metabolized in the liver using cytochrome P450 isoenzymes (including the CYP3A4 isoenzyme): a decrease in the concentration in the blood of the latter.
Analogues
Analogues of Phenobarbital are: Luminal, Barbital, Dormiral.
Terms and conditions of storage
Store in a dry dark place at a temperature not exceeding 25 °C. Keep out of reach of children.
Shelf life - 5 years.
Terms of dispensing from pharmacies
Released by prescription.
Found a mistake in the text? Select it and press Ctrl + Enter.
Prohibited during pregnancy
Prohibited while breastfeeding
Allowed for children
Has restrictions for the elderly
Forbidden for liver problems
Forbidden for kidney problems
Phenobarbital is a drug that has long been the main drug for the treatment of epilepsy. But due to the pronounced hypnotic effect and a large number of side effects, modern medicine no longer classifies this drug as a first-line drug.
Despite this, Phenobarbital is a vital drug for people with status epilepticus and, according to the instructions for use, is widely used to relieve seizures of various etiologies. At the moment, the active ingredient phenobarbital is the basis of many medicines, including the popular Corvalol, but is often supplemented with other components to minimize negative impact on the body.
General information about the drug
The drug is a derivative of barbiturates and belongs to the list of drugs that have a narcotic and psychotropic effect on the human body, and is subject to special quantitative control by the state.
Drug group, INN, scope
Phenobarbital (INN - Phenobarbital) belongs to the pharmacological group of antiepileptic drugs. The drug selectively inhibits the excitatory activity of the central nervous system, thereby preventing the occurrence of convulsive seizures of various etiologies, eliminates spasm of peripheral vessels and has a sedative effect, causing drowsiness.
Due to the pronounced inhibitory activity on the motor areas of the cerebral cortex, the drug is used for the symptomatic treatment of epilepsy and seizures of various etiologies, and also helps to fight insomnia.
Forms of release and prices for the drug, average in Russia
The drug is produced in the form of round white tablets placed in blisters. One carton of the drug may contain 6, 10, 12, 50 or 100 tablets.
It is important to understand that Phenobarbital is a drug from the group of barbiturates, therefore it is released exclusively on prescription.
On the territory of the Russian Federation, Phenobarbital is sold under the trade name Luminal, but most often pharmacies offer other medicines based on this substance.
Composition and pharmacological properties
The basis of the drug is the active substance of the same name - phenobarbital. One tablet may contain 5, 50 and 100 mg of the active ingredient. As additional and formative components, calcium, gelatin, starch (potato), lactose and croscarmellose sodium are involved.
The anticonvulsant mechanism of action of the substance is based on the inhibition of the transmission of an excitable impulse to neurons and an increase in the concentration of the inhibitory mediator GABA in the CNS. Also, the drug reduces the activity of the motor areas of the brain and reduces the stimulating effect of the effects of glutamate and aspartate (amino acids) on the central nervous system. Causes drowsiness.
Almost 80% of the substance is absorbed from the digestive tract and is evenly distributed throughout all tissues and body media. The drug is slowly absorbed and excreted from the body, begins to act only after 30-60 minutes after ingestion, and the half-life can take from 2 to 4 days in an adult and 10 days in an infant. The medicine has a cumulative effect.
Communication with blood proteins is about 45%. The process of splitting the substance into metabolites occurs under the influence of liver enzymes, excreted by the kidneys. 25% of the substance is excreted from the body unchanged.
Indications and contraindications
Due to the tendency of the drug to accumulate, it should not be used for too long a time in order to avoid the development of drug dependence.
Indications for the use of the drug are:
- paralysis (spastic);
- epileptic status;
- chorea;
- eclampsia;
- spasm of peripheral arteries;
- insomnia;
- hemolytic disease of the newborn.
The drug is contraindicated in case of allergy to one of the components of the drug, as well as in concomitant diseases and conditions:
- increased blood pressure;
- myocardial infarction (in the acute stage);
- kidney and liver dysfunction;
- diabetes;
- porphyria;
- myasthenia gravis;
- depression with a tendency to suicidal thoughts and intentions;
- SARS, complicated by shortness of breath and inflammation of the lower respiratory tract;
- chronic alcoholism, drug or drug addiction in history;
- lactose intolerance or Lapp lactase deficiency.
Bronchial asthma, depressed adrenal function, heart failure, acute and chronic pain syndrome, hyperkinesis, hyperthyroidism and intoxication of the body with other drugs are diseases in which Phenobarbital is prescribed with extreme caution.
Side effects of taking phenobarbital during pregnancy
The appointment of Phenobarbital is prohibited during pregnancy, since taking during the first three months of pregnancy can lead to the development of congenital malformations in the fetus or its death. Admission to recent weeks childbearing leads to the development of withdrawal syndrome in the newborn, which manifests itself in the form of seizures, bleeding disorders and increased excitability.
A significant part of Phenobarbital falls into breast milk women, in view of this, during treatment with the drug, it is necessary to abandon breastfeeding. The drug is approved for use from the first days of a person's life in recommended dosages.
Instructions for use
According to the instructions, Phenobarbital should be taken orally only after meals. The daily therapeutic dose of the drug is set gradually and adjusted only by the attending physician, based on the severity of the disease and age group sick.
A single dose for adults can range from 50 to 200 mg. During therapy, the dose can be slowly increased at intervals of every 5-7 days for one tablet per day.
The daily dose of the drug for children of different ages differs by approximately 10-20 mg / day and is:
- up to 6 months - 10 mg;
- up to 12 months - 20 mg;
- 1-3 years - 40 mg;
- 3-4 years - 60 mg;
- 4-7 years - 80 mg;
- 7-9 years - 100 mg;
- 9-14 years - 150 mg.
The daily dose of the drug must be divided into several doses. Children younger three years of age you can take the drug in the form of a suspension. To do this, crush the tablet into a powder and mix it with water.
The course of therapy depends on the nature of the disease. The first 2 weeks of therapy increased the risk of developing Lyell's and Steven-Johnson's syndromes. With a sharp rejection of the drug, the development of a withdrawal syndrome is possible, which is characterized by an increase in the signs of the underlying disease. Therefore, it is necessary to stop treatment with Phenobarbital slowly, gradually reducing the daily dosage, once a week.
The drug has a pronounced hypnotic effect, for this reason, during the period of treatment, it is worth giving up driving and work that requires increased attention and quick response. As a rule, after 2 weeks of therapy, the hypnotic effect of the drug begins to decrease.
The drug reduces the protective effectiveness of oral contraceptives. Concurrent use of NSAIDs can lead to the formation of ulcers on the gastric mucosa and duodenum, as well as internal bleeding.
Possible side effects and overdose
Long-term use of the drug has undesirable effects on the body, causing a number of complications, in the form of a lack of folate, impotence, nervousness, rickets and drug dependence. In addition, Phenobarbital can provoke the appearance of such adverse reactions:
With a significant increase in a single or daily dose (1 g or more), Phenobarbital poisoning develops.
An overdose of the drug is manifested by the following symptoms:
- Nausea with retching.
- Headache.
- Ataxia.
- Hypotension, up to collapse.
- Hypotension of peripheral vessels.
- Pneumonia.
- Difficulty breathing with the risk of its complete stop.
- General weakness of the body.
- Arrhythmia.
- Bradycardia.
- A sharp drop in body temperature (skin becomes cold and clammy to the touch).
- Slow diuresis.
- No reflexes.
- Coma.
Taking from 2 to 10 g of a substance, as a rule, leads to the biological death of a person. Detoxification in case of an overdose is carried out in a hospital under the control of all body functions, especially respiratory rate, heart rate and blood pressure.
There is no special antidote, so treatment is based on symptomatic therapy and reducing the amount of phenobarbital in the body by gastric lavage and forced diuresis using alkaline solutions. In case of severe kidney damage and difficulty breathing, a hemodialysis procedure is prescribed, and the patient is connected to a ventilator.
Analogues
All analogues of Phenobarbital, in addition to Pagluferal, are developed on the basis of other active substances that have an antiepileptic effect, since this substance is prohibited for use in many countries of the world.
In addition to complete analogues, there is a rather extensive list of medicines that contain phenobarbital in combination with other substances and at the same time have a completely different scope. Let's take a closer look at which drugs still contain phenobarbital:
- Corvalol.
- Valocordin.
- Lavocordin.
These medicines contain a small dose of phenobarbital and are widely used as sleeping pills or sedatives.
Latin name: Phenobarbitalum
ATX code: N03A A02
Active substance:
Manufacturer: Aspharma, Pharmstandard
- Leksredstv, Dalchimpharm, Tatkhimpharmpreparaty,
Usolye-Sibirsky KhPZ (RF)
Vacation from the pharmacy: on prescription
Storage conditions: at temperatures up to 25°C
Best before date: 5 l.
The drug Phenobarbital is a tablet with an antiepileptic, sedative and slight hypnotic effect based on the barbituric acid derivative of the same name. Reduces the activity of neurons in the area of epileptic excitation. In small doses, it is used as a sedative and hypnotic.
Phenobarbital is designed for use in:
- Epilepsy
- Convulsive conditions of non-epileptic origin
- Chorea
- Spasms of peripheral arteries
- spastic paralysis
- Eclampsia
- Sleep disorders
- Increased arousal, anxiety, inexplicable fear.
Composition, form of release, dosage
For the first time, the drug was released on the pharmaceutical market at the beginning of the last century - in 1912 under the trade name Luminal. It is the second name of phenobarbital. Anticonvulsant drugs are produced in tablets for children and adults.
- Active: 0.05 or 0.1 g of phenobarbital (for adults) or 5 mg (for children)
- Auxiliary: sucrose, potato starch, talc, stearic acid.
Drugs in the form of pills of a flat-cylindrical shape with a dividing strip and bevelled edges. Luminal tablets are packaged in non-cell or cell contour packs of 6, 10, or 12 pieces. It enters the pharmacy network in packs of cardboard or without it. The cardboard package contains 1, 5 or 10 Phenobarbital plates, description-instruction.
Medicinal properties
Medication with anticonvulsant, sedative and hypnotic effects.
The therapeutic effect of the drug is due to the properties of its main component - phenobarbital. It is a long acting barbiturate. It is assumed that the therapeutic effect of the substance is provided by its ability to enhance the properties of the endogenous GM mediator - gamma-aminobutyric acid (GABA), which provides inhibition of internal processes, or imitate its functions. Also, the mechanism of action of phenobarbital as a sedative and hypnotic is its effect on certain sensory areas of the cerebral cortex, resulting in a decrease in motor activity and changes in brain functions.
All processes triggered by drugs containing phenobarbital have not yet been fully studied. It is assumed that it is able, through its effect on the thalamus, to prevent neurotransmission to the cerebral cortex.
The anticonvulsant effect is achieved by suppressing mono- and polysynaptic transmission to the central nervous system.
During therapy with phenobarbital, it must be taken into account that it negatively affects respiratory activity, as it reduces sensitivity to carbon dioxide. The intensity of action is dose-dependent.
By acting on liver enzymes, it can change the metabolic transformations of other drugs, as well as have a relaxing effect on the smooth muscles of the gastrointestinal tract.
After ingestion, it is absorbed almost completely. Distribution in the body proceeds at a slower pace compared to other drugs included in the same pharmacological group together with phenobarbital. Peak levels of plasma concentration are formed in 1-2 days.
Forms metabolites in the liver. Able to accumulate in the body. The half-life from the body takes from 2 to 4 days: ¾ of the amount taken is in the form of metabolites, the rest is unchanged.
Phenobarbital is able to penetrate into milk and through the placenta.
Mode of application
The treatment regimen is determined individually for each patient in accordance with the severity of the diagnosis, age and condition of the body. Use of Phenobarbital for adults, according to the instructions for use:
- As a hypnotic: 0.1-0.2 g of drugs 30-60 minutes before going to bed
- As a sedative: 0.03-0.05 g x 2-3 r./d
- As an antispasmodic: 0.01-0.05 g x
- Epilepsy therapy: 0.05-0.1 g x 2 r./d.
The highest single dosage for adults is 200 mg, the daily dose is 500 mg.
Children
The drug is taken orally twice a day 30-40 minutes before meals. The recommended amount of Phenobarbital for a single dosage:
- (Up to 6 mo): 5 mg
- (6-12 mo): 10 mg
- (1-2 g): 20 mg
- (3-4 years): 30 mg
- (5-6 liters): 40 mg
- (7-9 l.): 50 mg
- (10-14 l.): 75 mg.
Use during pregnancy and lactation
The drug is forbidden to be taken in the 1st trimester, since its active substance has a teratogenic effect. Use during the period of bearing a child is possible in exceptional cases according to strict indications, when there is no alternative to the medicine, and the benefit to the mother is obvious.
The results of studies of the properties of the drug showed that the consequences of taking barbiturates by pregnant women are anomalies in the development of the fetus.
Babies whose mothers were treated with Phenobarbital during the last three months of gestation developed drug dependence and, after birth, a withdrawal syndrome. In addition to the usual symptoms after drug withdrawal in children, extremely high excitability and epileptic seizures were observed in the first two weeks of life.
There is also evidence that after the use of Phenobrabital for the treatment of convulsive conditions during gestation, it led to impaired blood clotting in children (due to a lack of vitamin K in the body), which contributed to the development of bleeding and death in the neonatal period.
For children, Phenobarbital is also dangerous because it can inhibit respiratory activity. Especially often, breathing problems develop in babies born prematurely.
In the case of the use of the drug during childbirth, resuscitation is required to provide timely assistance to the child.
Nursing women are also contraindicated to be treated with Phenobarbital, since the substance is excreted in milk and can suppress the central nervous system. At the time of therapy, lactation should be canceled.
Contraindications and precautions
Price: 100 mg (12 tablets) - from 20 rubles.
The use of the drug Phenobarbital can not be used for therapy with:
- Individual hypersensitivity to the active ingredient or auxiliary
- Porphyritic disease (in a mixed form, acute intermittent or in the presence of a history)
- Severe forms of liver and / or kidney pathologies
- Arterial hypotension in a pronounced form
- myasthenia gravis
- Acute form of MI
- Hyperkinesis
- Depression and depression with suicidal tendencies
- Severe anemia
- Adrenal insufficiency
- Pregnancy (1, 3 trimesters), lactation
- Alcoholism, drug addiction, drug addiction
- Respiratory diseases, bronchopulmonary pathologies with concomitant apnea
Phenobarbital and alcohol
Moreover, the consequences of such a combination can develop according to several scenarios. In alcoholics and heavy drinkers, the medicine may take a short time to work. In patients who rarely drink alcohol, after drinking during treatment, the therapeutic effect of the drug may occur with a significant delay.
Phenobarbital: drug or not?
One of the dangerous side effects of the drug is its ability to be addictive, the formation of physical and mental dependence. In 2013, phenobarbital was added to the list of narcotic and psychotropic substances.
Therefore, the drug is prohibited for use in patients with an existing addiction.
special instructions
If during therapy with Phenobarbital dermatological reactions develop, then you need to consult a doctor and stop the medicine. It is also worth considering that skin lesions are more common in patients who have a history of asthma, urticaria, angioedema.
Elderly patients, people with a weakened body are most susceptible to CNS depression: increased arousal or depression, clouding of consciousness.
Barbiturates in children often provoke hyperactivity, hyperexcitation, increased irascibility.
Phenobarbital should be used with particular caution in the treatment of elderly patients suffering from depression, since the drug can aggravate the course of the disease.
The risk of dependence increases with the use of the drug in large doses and with a long course, as well as in the treatment of patients with dependence on drugs and alcohol in the past. Frequent use of the drug at a dosage 3-4 times higher than the therapeutic one contributes to the formation of physical dependence in most patients (75-80%).
During the treatment of epilepsy, it is necessary to constantly monitor the level of concentration in the blood of phenobarbital and folate, the state of the liver and kidneys, and monitor peripheral circulation.
How to cancel Phenobarbital
In order not to provoke withdrawal and rebound syndromes, drug withdrawal should be carried out gradually, with a gradual decrease in dosage over a long period of time. The withdrawal state occurs, as a rule, 8-12 hours after drug withdrawal and manifests itself with varying degrees of intensity. First, there is anxiety, uncontrolled muscle twitches, hand tremors, increasing weakness, dizziness, decreased vision, nausea, vomiting, insomnia, orthostatic hypotension (dizziness, fainting, loss of consciousness).
With a severe pathology, adverse symptoms appear after about 16 hours and can persist for 5 days after drug withdrawal. Convulsions and delirium are the most common, with the latter sign being fatal if Phenobarbital has been used for a long time in an addicted patient. In addition, the sudden withdrawal of the drug can provoke epileptic seizures or status epilepticus.
Cross-drug interactions
During therapy with phenobarbital, one must take into account its ability to influence the therapeutic and side effects of other medications:
- Reduces the effect of antibiotic drugs, sulfonamides, Grisofulvin.
- Reduces the effect of indirect anticoagulants, corticosteroids, estrogen-containing drugs, as well as drugs whose metabolism is carried out in the liver.
- The hypnotic effect of phenobarbital decreases when combined with atropine, drugs based on belladonna extract substances, as well as when combined with dextrose, analeptics, nicotinic acid, and NS stimulants.
- When combined with reserpine, the antiepileptic activity of phenobarbital decreases, and under the influence of diazepam, amitriptyline, chlordiazepoxide, it increases.
Side effects and overdose
Like any drug, Phenobarbital can provoke a negative reaction of the body, which manifests itself in the form of various disorders from the internal systems:
- NS: asthenia, general weakness, dizziness, pre- and syncope, motor coordination disorder, nystagmus, hallucinations, paradoxical excitement (especially in children, debilitated and elderly patients), depression, nightmares, insomnia
- Locomotor system: with a long course - damage to bone tissue, rickets
- Digestive organs: nausea, bouts of vomiting, difficulty in emptying the intestines, with long-term therapy - liver dysfunction
- Hematopoietic system: agranulocytosis, B12 deficiency anemia, thrombocytopenia
- CCC: pressure reduction
- Allergy manifestations: skin rash, urticaria, swelling of the face and eyelids, depressed breathing, in some patients - Ritter dermatitis, Stevens-Johnson syndrome
- Other effects: addiction and dependence on phenobarbital.
If these or other unnamed side effects occur, you should contact your healthcare professional.
Intentional or unintentional ingestion of large amounts of Phenobarbital provokes an overdose. In addition to the acute form of intoxication after a single use of overdoses, the oversaturation of the body with the active substance also occurs with a long treatment course.
The characteristic signs of acute toxicity are manifested in the form of:
- nystagmus
- Headache
- dizziness
- Ataxia
- Inhibition of reactions
- Slurred speech
- General weakness
- Impaired or absent reflexes
- Changes in body temperature (decrease or increase)
- Drowsiness
- Apnea
- nervous excitement
- Decrease in blood pressure
- midriaza
- Decreased urine output
- Brady and tachycardia
- Respiratory depression
- cyanosis
- Rash in the form of hemorrhage into the dermis (hemorrhages) in pressure zones
- clouding of consciousness
- Absence of brain electrical activity
- Pulmonary edema
- Coma
- pneumonia
- heart failure
- Loss of self-criticism
- Increased irritability.
During therapy, the prescribed therapy regimen must be carefully observed, since an unauthorized change in the dose of the drug can provoke fatal consequences. The lethal dose of phenobarbital is the intake of 2 to 10 g of drugs.
There is no specific antidote for the substance yet. If the patient is conscious, then vomiting is stimulated, if he is fainting or induction of the gag reflex is contraindicated, gastric lavage should be done. To speed up the cleansing of the body from the absorbed substance, forced diuresis is prescribed (with normal condition kidneys), saline laxative drugs.
In addition to detoxification treatment, phenobarbital poisoning is stopped by symptomatic therapy. During the correction of the condition, measures are required that support the functions of vital organs.
Chronic intoxication manifests itself in the form of:
- Enduring irritability
- Weakening of self-criticism
- Insomnia or drowsiness
- apathetic state
- General weakness
- Impaired sense of balance
- inconsistent speech
- dizziness
- Severe disturbance of consciousness
- hallucinations
- convulsions
- Nervous excitement
- Dysfunctions of the gastrointestinal tract, cardiovascular system, liver, kidneys.
Elimination of chronic intoxication requires a gradual reduction in dosage so as not to provoke a withdrawal syndrome. Simultaneously, symptomatic and psychiatric treatment is carried out.
Analogues
Only the attending specialist can replace Phenoabarbital with analogues. Drugs with a similar effect: Antelepsin, Apilepsin, Acediprol, Benzonal, Valparin, Vetoin, Hexamidin, etc.
Medicines containing phenobarbital: Andipal, Barboval, Bellataminal, Valocordin, Valoserdin, Corvaldin, Corvalol, Pagluferal, Pentabufen, Pentalgin, Piralgin, Santoperalgin, Santotitralgin, Sedal-m, Sedalgin-neo, Teofedrin-n, Tetralgin.
Sun Pharmaceutical Industries (India)
Price: tab. 200 mg (30 pcs.) - 84 rubles, 400 mg (30 pcs.) - 106 rubles.
An antiepileptic drug based on carbamazepine. It is used for the treatment and prevention of epilepsy, seizures, as well as trigeminal neuralgia, acute forms of manic states, alcohol withdrawal, psychotic disorders, migraine.
Produced in tablets with a prolonged effect. The dosage regimen and duration of therapy is determined by the attending specialist.
Pros:
- Effective remedy
- Prevents seizures
- available remedy.
Minuses:
- accumulates in the body.
