The drug 'Serdolect' - instructions for use, description and reviews

Pharmacodynamics and pharmacokinetics

Mebhydrolin contained in this drug is an antihistamine that blocks histamine H1 receptors. It significantly reduces the spasmogenic effect of histamine on the smooth muscles of the intestines and bronchi. It also affects vascular permeability . If we compare this drug with first-generation antihistamines, such as suprastin or diphenhydramine , then its sedative and hypnotic effects are much less pronounced.
Diazolin also has anesthetic properties, but they are weak. Absorption of the drug occurs very quickly, and after 15-30 minutes it begins to act. The maximum effect in patients is observed after 1-2 hours, while its duration is up to two days. It is excreted from the body through the kidneys.

Drug interactions

When Serdolect is used in combination with certain drugs/substances, the following effects may develop:

• drugs that prolong the QT interval or inhibit the metabolism of sertindole: increased risk of prolongation of the QT interval (combination of drugs is prohibited);
• macrolide antibiotics (erythromycin) and calcium channel blockers (diltiazem, verapamil): a slight increase in the plasma concentration of sertindole, the degree of increase may be greater in patients with weak CYP2D6 activity (the combination of drugs is prohibited);
• drugs that inhibit CYP2D6, including paroxetine, fluoxetine, quinidine: increased plasma concentrations of sertindole (maintenance doses may be reduced; an ECG is required before and after changes in doses of these drugs);
• rifampicin, phenytoin, carbamazepine, phenobarbital: increased metabolism of sertindole and, accordingly, a decrease in its plasma concentration (an increase in its dose may be required);
• some antihypertensives, antiarrhythmics, beta-blockers, a large number of antidepressants and antipsychotics: sertindole has a slight inhibitory effect on the activity of CYP2D6, by which these drugs are metabolized.

Which pharmacological group does Diazolin belong to?

The drug is classified as an antihistamine for systemic use.

The active substance of Diazolin (mebhydrolin) has an antihistamine effect, blocking H1 receptors for histamine in the body's immunocompetent cells. It also reduces the intensity of the spasmogenic effect of histamine on the smooth muscle fibers of the bronchi and intestines, and eliminates its effect on the permeability of vascular walls. It differs from other first-generation antiallergic drugs in that it has a mild hypnotic and sedative effect.

In the digestive tract, mebhydrolin is rapidly absorbed into the bloodstream. The percentage of bioavailability of the drug ranges from 40 to 60. Diazolin for allergies gives the first therapeutic effects ¼ hour after use, and maximum effectiveness is observed after 1-2 hours.

We suggest you familiarize yourself with Signs of sciatic nerve damage after injection || The medicine did not reach the muscle

Side effects

The use of Diazolin may cause the following side effects:

• Hematopoietic system: in rare cases - agranulocytosis, granulocytopenia.
• Central and peripheral nervous system: possible paresthesia, dizziness, tremor, fatigue, slow psychomotor reaction, drowsiness, anxiety (at night).
• Digestive system: rarely - dyspeptic symptoms as a result of irritation of the gastric mucosa (in particular, attacks of nausea, heartburn, pain in the epigastric region), dry mouth.
• Urinary system: in rare cases - dysuria.

Contraindications

Patients who are highly sensitive to the components of diazolin should not take the drug. The drug is not prescribed to people with exacerbation of gastric and duodenal ulcers or any other inflammatory diseases of the gastrointestinal tract. A contraindication to the use of Diazolin is pyloric stenosis.

This drug should be prescribed with extreme caution if the patient has severe liver and kidney failure. In this case, you need to individually adjust the dose of the drug, as well as the number of doses. It is not recommended to prescribe Diazolin for epilepsy , angle-closure glaucoma, or for various heart rhythm disorders.

Medicinal properties, indications for use and contraindications

Sertindole belongs to the category of antipsychotic drugs. The therapeutic effect of the antipsychotic is due to the selective blockade of specific neurons and inhibition of dopamine D2, alpha1-adrenergic, and serotonin 5-HT2 receptors.

Sertindole is rapidly absorbed from the gastrointestinal tract. The time of its maximum concentration in plasma is 10 hours. Metabolism of the substance occurs in the liver. Sertindole is excreted from the body mainly in feces, and partially in urine.

The indication for use of Serdolect is schizophrenia. The exceptions are acute psychotic disorders and intolerance to neuroleptics.

Contraindications:

• Pregnancy and lactation
• Hypomagnesemia
• Long QT syndrome
• Diseases of the heart and blood vessels
• Age up to 18 years
• Glucose-galactose malabsorption
• Liver failure.

The tablets should be taken with caution if there is a history of Parkinson's disease, liver disease, or an increased risk of stroke. Old age is considered a relative contraindication.

Diazolin for adults

It was said above why an adult should strictly follow the instructions for use and not self-medicate. Here we will talk about the nuances that you need to remember before taking Diazolin:

• firstly, about the sedative effect of the said drug. Although it is not as strong as that of first-generation antihistamines, the patient may fall asleep more often during the course of treatment, his attention may become more distracted, his behavior more passive, and his performance will decrease. That is, the usual daily routine will be disrupted. That is why a patient taking Diazolin should refuse work that requires a quick reaction or intellectual stress, as well as driving a vehicle or heavy equipment;
• secondly, that while providing a systemic effect on the allergy-affected body, Diazolin is not always successfully combined with other drugs. So, if the patient is taking medications that depress the central nervous system (hypnotics, sedatives, etc.), Diazolin will only worsen their effect. As a result, the patient becomes passive and lethargic. Also, medications that irritate the mucous membrane of the stomach and intestines should not be taken simultaneously with Diazolin. Ethanol and alcohol tinctures are incompatible with Diazolin, as they increase the symptoms of general intoxication of the body. By the way, for this reason it is recommended to avoid alcoholic beverages while taking Diazolin;
• thirdly, you need to be especially careful when handling Diazolin during pregnancy. This point should be discussed in more detail.

The question of whether you should take Diazolin if you are pregnant is of concern to many expectant mothers. Even if they received a prescription from the attending physician, they have doubts. After all, the instructions included with the drug list pregnancy as one of the contraindications. But here we must keep in mind that there are different cases. Allergies in the mother can negatively affect the health of the unborn child, so taking Diazolin is a lesser evil.

This drug is prescribed taking into account three factors: the health status of the expectant mother, the presence of concomitant diseases and the trimester of pregnancy.

During the first two trimesters, taking Diazolin, as well as any other drugs, is strictly prohibited. The fact is that Diazolin has a systemic effect on the body, easily penetrating into the blood of the unborn child. This can lead to pregnancy failure - spontaneous abortion or cessation of fetal development (frozen pregnancy), or the development of fetal pathologies.

After the twelfth week of pregnancy, the risks associated with the use of antihistamines decrease. In the third trimester (and in some cases also in the second), Diazolin can be prescribed. However, this drug is taken only under the strict supervision of the attending physician, who can determine how useful the drug is for the mother and child in a particular case. The course of treatment in this case does not exceed 3-5 days. At the same time, late toxicosis or the threat of premature birth are also contraindications to the use of the drug.

But it is best to simply avoid contact with a substance that causes an allergic reaction in the expectant mother.

The use of Diazolin during lactation is also unacceptable, since it passes into mother's milk and can negatively affect the health of the child. Instructions and doctors also warn about this.

Side effects

According to the annotation, the following side effects may occur while taking the drug.

In the digestive system: possible irritation of the mucous membranes of the gastrointestinal tract, dyspeptic symptoms - nausea, heartburn , pain in the epigastric region.

In the work of the central nervous system: possible dizziness, paresthesia , high level of fatigue, increased drowsiness, slow reaction, blurred visual perception.

Also, when taking the drug, you may experience dry mouth, problematic urination, and allergic reactions. Granulocytopenia and agranulocytosis occur very rarely . The risk of side effects increases significantly with an overdose.

Paradoxical reactions are possible when children take the drug: they may experience irritability, insomnia, and tremor .

Side effects

Taking Sirdalud in recommended therapeutic dosages for the treatment of muscle dysfunction in vertebrogenic pain syndromes rarely leads to side effects, they are expressed implicitly, and reducing doses leads to their disappearance. Among them are:

• Weakness.
• Drowsiness.
• Dizziness.
• Tendency to decrease pressure.
• Nausea.
• Increased activity of hepatic transaminases.
• Dry mucous membranes.

Taking large dosages for the treatment of spastic hypertonicity often leads to side effects, which, however, quickly go away when the dose is reduced or the drug is discontinued. Among them, sleep disturbances, bradycardia, sustained hypotension should be noted; extremely rarely, in high doses, the side effect of acute hepatitis can be observed.

What symptoms occur in case of an overdose of Diazolin?

In cases of overdose, there is an exacerbation of side effects from taking Diazolin. The patient experiences disruptions in the functioning of the digestive system, gastrointestinal tract, and central nervous system. Sometimes there is a feeling of dryness in the oral cavity, impaired urination, neutropenia, and agranulocytosis. Rarely does an exacerbation of allergic symptoms occur.

To combat the symptoms of a Diazolin overdose, you must:

• stop using Diazolin;
• carry out measures to detoxify the body (rinse the stomach, force diuresis);
• implement symptomatic therapy (in order to eliminate or alleviate signs of overdose).

Due to the use of Diazolin, the formation of certain side symptoms is possible. These include the occurrence of:

• disturbances in the functioning of the gastrointestinal tract and digestive system (heartburn, nausea, epigastric pain due to irritation of the mucous membranes with mebhydrolin);
• disturbances in the functioning of the central nervous system (dizziness, paresthesia, increased fatigue, drowsiness, blurred vision, slow reaction speed, tremor, anxiety);
• other disorders (dry mouth, urination problems, allergic reactions);
• quite rare: neutropenia, agranulocytosis;
• when used in pediatric therapy for increased agitation, tremor, sleep disturbances, irritability;
• headache;
• itching;
• rash;
• hives;
• Quincke's edema.

Instructions for use of Diazolin (Method and dosage)

Dragees and Diazolin tablets, instructions for use

The drug in tablets and dragees is used after meals.

How to take for adults? Children from twelve years of age, as well as adults, use the drug once or twice a day at a dose of 100-200 mg. The maximum single dose for adults should be 300 mg; adults can take 600 mg of Diazolin per day. Children five to twelve years old can take 50 mg two to three times daily. Children aged three to five years can take 50 mg of the drug 1-2 times a day. How long the treatment should last should be determined by a specialist in each specific case.

Instructions for use of Diazolin for children

Children's Diazolin is used as follows: 100 ml of warm boiled water is added to the bottle containing the granules. The contents must be mixed very thoroughly, for which you need to stir for several minutes. After this, the suspension is given to children in doses that can be easily determined using the supplied graduated glass. Dosages of children's Diazolin should be as follows: 2.5 ml - children 2-3 years old; 5 ml - children 4-6 years old; 7.5 ml – children 7-10 years old. The drug should be taken two or three times after meals for 5-7 days. The suspension must be shaken before use.

Release form and composition

The dosage form of Serdolect is film-coated tablets: biconvex, oval; color (4/12/16/20 mg respectively) – pale yellow, pale yellow-brownish, brownish pink or pale pink; on one side there is an inscription (corresponding to the dosage of the tablets) “S4”, “S12”, “S16” or “S20” (4 mg each: in blisters of 10 pcs., in cardboard packs of 2 or 3 blisters; 12, 16 and 20 each mg: in blisters of 14 pcs., in cardboard packs 1, 2 and 4 blisters).

Composition of 1 tablet:

• active ingredient: sertindole – 4, 12, 16 or 20 mg;
• additional components: lactose monohydrate, corn starch, hyprolose, microcrystalline cellulose, croscarmellose sodium, magnesium stearate;
• shell: hypromellose, macrogol 400, titanium dioxide (E171); additionally (depending on dosage): 4 mg – yellow iron oxide (E172); 12 mg – iron oxide red (E172), iron oxide yellow (E172); 16 mg – red iron oxide (E172); 20 mg – iron oxide red (E172), iron oxide black (E172), iron oxide yellow (E172).

pharmachologic effect

The active component of Diazolin (mebhydrolin) has a pronounced antiallergic effect and, by blocking H1-histamine receptors, helps reduce swelling of the mucous membranes.

A distinctive property of Diazolin compared to first generation antihistamines is the absence of pronounced hypnotic and sedative effects. At the same time, adult and children's Diazolin effectively affects the smooth muscles of the uterus, bronchi and intestines, and also reduces the severity of increased vascular permeability and lowering blood pressure.

The effect of Diazolin, according to the instructions, is observed half an hour after administration, and its duration can reach two days.

Serdolect®

The cardiovascular system

Clinical studies have shown that sertindole prolongs the QT interval to a greater extent than some other antipsychotics. The mean prolongation of the QT interval is greater at the upper end of the recommended dose range (20 mg and 24 mg). Prolongation of the QTc interval with certain drugs is associated with the possibility of torsades de pointes (TdP) (potentially fatal torsade de pointes) and sudden death. However, clinical and non-clinical trial data have failed to confirm whether sertindole is more arrhythmogenic than other antipsychotics. Therefore, sertindole should only be used in patients intolerant to at least one antipsychotic drug.

Doctors prescribing sertindole should observe the following safety precautions.

ECG monitoring:

— An ECG study must be performed before prescribing the drug Serdolect.

— When the QT interval exceeds 450 ms in men and 470 ms in women, the use of the drug Serdolect is contraindicated.

- An ECG study should be carried out before prescribing the drug, then when equilibrium concentration is reached approximately 3 weeks after the start of treatment or when the daily dose of 16 mg is reached, and also 3 months after the start of treatment.

— During maintenance therapy, an ECG study must be performed every 3 months.

- During maintenance therapy, an ECG study should be performed before and after any increase in the dose of sertindole.

— An ECG is recommended after adding/increasing the dose of a drug that can increase the concentration of sertindole in the blood (see section “Interaction with other drugs”).

— If the QTc interval prolongs beyond 500 ms, sertindole should be discontinued.

— If a patient develops symptoms such as palpitations, convulsions, fainting, which may indicate the possibility of developing arrhythmias, the attending physician should immediately begin examining the patient, including an ECG.

— It is preferable to conduct an ECG study in the morning; to calculate the QTc interval, it is preferable to use the Bazetta or Friederichia formulas.

The risk of QT prolongation is increased in patients receiving concomitant therapy with drugs that prolong the QTc interval or drugs that inhibit the metabolism of sertindole (see section "Contraindications").

In patients at risk of significant electrolyte imbalances, baseline plasma potassium and magnesium levels should be determined before initiating treatment with sertindole. Low potassium and magnesium levels should be corrected before starting treatment. Monitoring serum potassium levels is recommended for patients experiencing vomiting, diarrhea, patients taking potassium-sparing diuretics, or other electrolyte imbalances.

During the initial dose titration, due to the α1-blocking properties of sertindole, symptoms of postural hypotension may appear.

Antipsychotic drugs may inhibit the effects of dopamine agonists. Sertindole should be used with caution in patients with Parkinson's disease.

Some selective serotonin reuptake inhibitors (SSRIs), such as fluoxetine and paroxetine (potent CYP2D6 inhibitors), can increase plasma levels of sertindole by 2-3 times. Therefore, sertindole should only be used with these drugs with extreme caution and only if the potential benefits outweigh the risks. In this case, a lower maintenance dose of sertindole may be required; in addition, a thorough ECG study should be performed before and after any dose adjustment of these drugs (see Section “Interaction with other drugs”). Sertindole should be used with caution in patients with known low activity of the CYP2D6 isoenzyme (see section "Interaction with other drugs").

Very rare cases of hyperglycemia or exacerbation of existing diabetes have been reported during treatment with sertindole. It is advisable to establish appropriate clinical monitoring of patients with diabetes and patients with risk factors for developing diabetes.

Increased mortality among older people with dementia

Data from two large observational studies showed that older people with dementia taking antipsychotic drugs had a small increased risk of death compared with patients not taking antipsychotic drugs. There is no sufficient data to accurately assess the magnitude of the risk and the reasons for its increase. Sertindole is not registered for the treatment of behavioral disorders associated with dementia.

Risk of developing cerebrovascular adverse events

In randomized, placebo-controlled clinical trials of certain atypical antipsychotics in patients with dementia, a 3-fold increase in the risk of cerebrovascular adverse events was observed. The mechanism for this increased risk is unknown. An increased risk cannot be ruled out when using other antipsychotics in other groups of patients. Serdolect should be used with caution in patients at risk of stroke.

Given the increased risk of developing significant cardiovascular disease in the elderly, sertindole should be used with caution in patients over the age of 65 years. Treatment should be started only after a thorough examination of the cardiovascular system.

Venous thromboembolism (VTE)

Cases of venous thromboembolism (VTE) have been reported while taking antipsychotics. Due to the fact that patients treated with antipsychotics are often at risk for developing venous thromboembolism, all possible risk factors for developing venous thromboembolism should be identified before and during treatment with sertindole and precautions taken.

Decreased liver function

With a slight or moderate degree of liver dysfunction, careful monitoring of the patient's condition is necessary. Slower dosage titration and a lower maintenance dose are recommended.

Tardive dyskinesia

Tardive dyskinesia is thought to be caused by increased sensitivity of dopamine receptors in the basal ganglia as a result of chronic receptor blockade by antipsychotic drugs. In clinical studies, a low incidence (comparable to the placebo group) of extrapyramidal symptoms was observed during treatment with sertindole. However, long-term use of antipsychotic drugs, especially in high doses, is associated with the risk of developing tardive dyskinesia.

If symptoms appear while taking sertindole, you should consider reducing the dose or discontinuing the drug.

Seizures

Serdolect should be prescribed with caution in patients with a history of seizures.

Neuroleptic malignant syndrome (NMS)

The use of antipsychotic drugs has been reported to be associated with the development of a potentially fatal symptom complex called Neuroleptic Malignant Syndrome (NMS). Therapeutic tactics for managing patients with NMS should include immediate withdrawal of antipsychotic drugs.

Withdrawal syndrome

If antipsychotics are abruptly stopped, withdrawal symptoms may occur, including nausea, vomiting, increased sweating, and insomnia. The return of psychotic symptoms and the appearance of involuntary movement disorders (akathisia, dystonia, dyskinesia) are also possible. Therefore, gradual withdrawal of the drug is necessary.

Excipients
The tablets contain lactose monohydrate. Patients with rare hereditary galactose intolerance, lactase deficiency or impaired absorption of glucose and galactose should not be prescribed the drug.

Analogs

Structural analogues of Diazolin (based on the active substance) are Dialin, Mebhydron and Omeril.

The following drugs belong to the same pharmacological group (“Antihistamines for systemic action”) and are characterized by a similar mechanism of action: Aviamarin, Alerpriv, Allerfex, Gistafen, Gifast, Dezal, Desloratadine, Diacin, Dimebon, Dimedroquine, Dinox, Dramina, Kestin, Ketotifen, Clalergin, Clargotil, Claridol, Clarisens, Claritin, Clarifer, Clarotadine, Lomilan, LauraGexal, Loratadine, Lordestin, Lotharen, Nalorius, Peritol, Rapido, Rupafin, Semprex, Ciel, Telfast, Fexadin, Fexo, Fexofast, Fexofenadine, Fenkarol, Ezlor, Eliseus, Erius.

Diazolin price, where to buy

The price of Diazolin in tablets is 50 rubles for 10 pieces of 50 mg of active ingredient. The cost of the pills is 70 rubles for 10 pieces of 50 mg of mebhydrolin, and 80 rubles for 10 pieces of 100 mg.

How much do tablets cost in Kharkov? Around 5-10 UAH.

The price of children's Diazolin is about 95 rubles.

The ointment of this drug is not for sale.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine
• Online pharmacies in KazakhstanKazakhstan

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Diazolin - what are these tablets and what are they prescribed for?

Diazolin (Mebhydrolin) belongs to the first generation of antihistamines. Despite the fact that second and even third generation antihistamines have already appeared, Diazolin has not lost its relevance today.

Antihistamines are traditionally called drugs that can block the action of histamine. Histamine is a very active biological substance that is produced in the human body, both normally and under various pathological conditions. Histamine is most actively released during allergic reactions in the respiratory system, on the skin or in the eyes. In this case, characteristic allergy symptoms occur. Antihistamines prevent the development of allergic manifestations.

special instructions

During dose selection and before maintenance therapy, blood pressure should be monitored.

Serdolect is prescribed only if there is already intolerance to at least one antipsychotic, which is associated with precautions due to an increase in the QT interval.

The risk of QT prolongation (which can cause torsade de pointes (TdP) and, in some cases, sudden death) increases with higher daily doses of sertindole (20 to 24 mg).

An ECG is performed: before Serdolect is prescribed (if the QT interval is more than 470 ms in women and 450 ms in men, therapy is not prescribed); approximately 3 weeks after starting the drug or after reaching the daily dose of 16 mg; 3 months after the start of therapy; during maintenance treatment - every 3 months, as well as before/after increasing the dose or after adding/increasing the dose of a drug that can increase the plasma concentration of sertindole. If the QT interval prolongs above 500 ms, the drug is discontinued.

The reason for an immediate examination of the patient's condition, including an ECG, is the appearance of symptoms that indicate the possibility of arrhythmia (convulsions, palpitations, fainting). It is advisable to perform an ECG in the morning.

If there is a risk of severe electrolyte disturbances, serum concentrations of magnesium and potassium levels are measured before prescribing Serdolect. Hypokalemia and hypomagnesemia must be corrected before starting the drug. In case of vomiting and diarrhea, as well as during combination therapy with potassium-sparing diuretics or in the presence of other electrolyte disturbances, monitoring of plasma potassium concentration is required.

Long-term therapy with Serdolect, especially with high doses, increases the likelihood of developing tardive dyskinesia. If symptoms of this disorder appear, reduce the daily dose or discontinue the drug completely.

If neuroleptic malignant syndrome develops, immediate cessation of therapy is required.

Serdolect should be discontinued gradually, since abrupt withdrawal can lead to increased sweating, nausea, vomiting, insomnia, as well as the return of psychotic symptoms and the development of involuntary movement disorders (akathisia, dystonia, dyskinesia).

Serdolect does not have a sedative effect, but you should not drive vehicles or operate machinery until your individual tolerance to the drug is determined.