Dopegit - instructions for use, reviews, analogs and forms of release (tablets of 250 mg) of the drug for the treatment of hypertension and pressure reduction in adults, children and pregnancy. Indications and contraindications

In this article, you can read the instructions for using the drug Dopegit. Comments of visitors of the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Dopegit in their practice are presented. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Dopegite in the presence of existing structural analogues.Use to treat hypertension and reduce blood pressure in adults, children, as well as during pregnancy and lactation. Indications and contraindications to taking the drug.

Dopegit - antihypertensive drug of central action. Metabolized with the formation of alpha-methylnoradrenaline, which has an antihypertensive effect through several mechanisms:

• decrease in sympathetic tone by stimulation of central inhibitory presynaptic alpha2 receptors;
• replacement of endogenous dopamine on dopaminergic nerve endings (as a false neurotransmitter);
• decreased plasma renin activity and decreased OPSS;
• suppression of norepinephrine synthesis, reduction of dopamine, serotonin, noradrenaline and epinephrine in tissues due to inhibition of dopa decarboxylase enzyme activity.

Methyldopa (the active substance of the preparation Dopegit) does not directly affect the function of the heart, does not reduce cardiac output, does not cause reflex tachycardia, nor does it reduce the glomerular filtration rate, renal blood flow, or the filtered fraction. In some cases, the heart rate decreases.Effectively reduces blood pressure in both a prone position and a standing position. Rarely causes postural hypotension.

After taking a single oral dose, the maximum effect develops within 4-6 hours and lasts approximately 12-24 hours. With repeated use of the drug, the maximum decrease in blood pressure is achieved on day 2-3. After discontinuation of therapy, the blood pressure level returns to the initial values ​​within 1-2 days.

Composition

Methyldopa sesquihydrate + auxiliary substances.

Pharmacokinetics

Absorption of methyldopa from the gastrointestinal tract is approximately 50%. After oral administration, the bioavailability of methyldopa is about 25%. Binding to plasma proteins is less than 20%. Methyldopa penetrates the placental barrier and is excreted in breast milk. Metabolism of methyldopa occurs intensively. Methyldopa is metabolized predominantly in the liver. Active metabolite of methyldopa - alpha-methylnoradrenaline, is formed in adrenergic neurons of the central nervous system. There are also some other methyldopa derivatives that are excreted from the body by the kidneys. Approximately two-thirds of the absorbed methyldopa is excreted from the body by the kidneys in unchanged form, as well as in the form of sulfate compounds.The rest of the drug is excreted through the intestine (also in the unmodified state). The active substance is completely eliminated from the body within 36 hours.

Indications

• arterial hypertension (to reduce pressure).

Forms of release

Tablets 250 mg.

Instructions for use and dosage

Tablets are taken orally before or after meals. The dosage regimen is set individually.

Adult patients

The recommended initial dose of Dopegit in the first 2 days of therapy is 250 mg 2-3 times a day. Then the dose can be gradually increased or decreased (depending on the degree of BP reduction). The duration of intervals between increasing and decreasing the dose of Dopegit should be at least 2 days. Since 2-3 days after the start of therapy, as well as with a subsequent increase in the dose, there may be an adverse sedative effect of the drug, it is recommended first to increase the evening dose of the drug.

The standard maintenance dose of Dopegit is 0.5-2 g per day. This dose is divided into 2-4 admission. The maximum daily dose of the drug should not exceed 3 g. In cases when against the background of taking the drug at a dose of 2 g per day there is not enough effective reduction in blood pressure,it is recommended to combine Dopegit with other antihypertensive drugs. After 2-3 months of therapy, tolerance to methyldopa may develop. Effective reduction in blood pressure can be achieved by increasing the dose of the drug or concomitant use of diuretics. 48 hours after the termination of therapy with Dopegit, the blood pressure usually returns to the baseline level. "Ricochet effect" is not observed.

The drug Dopegit can be prescribed to patients who are already receiving therapy with other antihypertensive drugs, subject to a gradual withdrawal of these drugs. In such cases, the initial dose of Dopegit should not exceed 500 mg per day. The dose is increased as needed, with intervals of at least 2 days.

When using Dopegit in addition to the previously prescribed antihypertensive therapy, in order to guarantee a smooth transition, it may be necessary to adjust the doses of antihypertensive drugs.

Side effect

• progression of angina pectoris
• myocarditis
• pericarditis
• congestive heart failure
• Orthostatic hypotension (a dose reduction is recommended)
• peripheral edema
• weight gain
• sinus bradycardia
• parkinsonism
• peripheral paralysis of the facial nerve (Bell's paralysis)
• intellectual decline
• symptoms of cerebral circulatory insufficiency (possibly as a consequence of hypotension)
• mental disorders, (including nightmares, usually reversible mild psychosis and depression)
• headache
• sedative effect (usually transient)
• general weakness
• increased fatigue
• dizziness
• paresthesia
• decreased libido
• nasal congestion
• pancreatitis
• colitis
• nausea, vomiting
• diarrhea
• inflammation of the salivary glands
• pain or dark staining of the tongue
• constipation
• bloating
• flatulence
• dryness of the oral mucosa
• jaundice
• toxic epidermal necrolysis
• eczema or a rash that resembles lichen
• slight pain in joints with or without edema
• myalgia
• hyperprolactinemia, gynecomastia, galactorrhea, amenorrhea
• vasculitis
• lupus syndrome
• drug fever
• eosinophilia
• positive Coombs test
• Hemolytic anemia, leukopenia, granulocytopenia, thrombocytopenia
• impotence
• violations of ejaculation.

Contraindications

• acute hepatitis, cirrhosis;
• liver disease in history (on the background of methyldopa);
• concomitant therapy with MAO inhibitors;
• depression;
• hemolytic anemia;
• acute myocardial infarction;
• pheochromocytoma;
• children's age up to 3 years (for the tablet form);
• hypersensitivity to the drug.

Application in pregnancy and lactation

According to the results of clinical studies after the application of Dopegit in the 2nd and 3rd trimesters of pregnancy, there were no signs of damage to the fetus or newborn. Since adequate and strictly controlled studies in the 3 trimester of pregnancy have not been conducted, the drug is recommended only after a careful comparison of the expected benefit of therapy for the mother and the potential risk to the fetus.

The study of children born to mothers who took Dopegit after the 26th week of pregnancy did not reveal any undesirable effects of the drug. In pregnant women who took the drug in the 3rd trimester, the condition of the fetus was better than in women who did not take the drug.

Methyldopa is excreted in breast milk, so it is recommended to prescribe the drug during lactation only after careful comparison of the expected benefit for the mother and the potential risk to the child.

Application in elderly patients

Elderly patients are prescribed a minimum initial dose, which should not exceed 250 mg per day. If necessary, the dose can be gradually increased. The duration of intervals between increasing the dose of the drug is at least 2 days. The maximum daily dose of Dopegit should not exceed 2 g.

Fainting is common in elderly patients. This may be due to increased susceptibility to the drug and pronounced atherosclerotic vascular lesions. The development of fainting can be avoided by reducing the dose of Dopegit.

Use in children

For children older than 3 years, the initial dose of the drug is 10 mg / kg of body weight per day. The daily dose is divided into 2-4 admission. If necessary, the dose can be gradually increased until the desired effect is achieved. Between the increase in the dose of the drug should be observed interval of at least 2 days. The maximum daily dose of Dopegit is 65 mg / kg of body weight per day, but not more than 3 grams per day.

Contraindicated in children under 3 years.

special instructions

In rare cases, patients taking methyldopa developed hemolytic anemia.When signs of anemia appear, it is necessary to determine the concentration of hemoglobin and hematocrit. If anemia is confirmed, the degree of hemolysis should be further assessed. In the case of hemolytic anemia, Dopegit should be discontinued. After discontinuation of therapy (with or without corticosteroids), it is usually possible to quickly achieve remission. However, in rare cases, lethal outcomes were observed. Dopegit is contraindicated in patients with hemolytic anemia, which has developed against the background of therapy with this drug.

In some patients who have been taking Dopegit for a long time, a positive Coombs test is determined. According to reports of various researchers, the prevalence of this reaction varies from 10 to 20%. A positive Coombs test is rarely seen during the first 6 months of therapy. If this phenomenon does not develop during the first 12 months of therapy, then its detection is unlikely in the future. The prevalence of a positive Coombs test is dose-dependent. Most rarely this phenomenon is observed in patients taking the drug at a dose of 1000 mg per day or less.The Coombs test, positive for methyldopa, becomes negative after a few weeks or months after discontinuation of therapy with the drug. Before starting treatment, and also at the 6th and 12th month of therapy, it is recommended to perform a general blood test and a direct Coombs test.

The identification of a positive Coombs test in the past or against the background of the therapy itself is not a contraindication to taking Dopegit. In cases where the positive direct Coombs test is detected against the background of the drug, it is necessary to exclude the presence of hemolytic anemia in the patient and to determine the clinical significance of this phenomenon.

Information on previous positive results from the Coombs test helps in assessing blood for cross-compatibility before transfusion. If in the treatment of a patient taking Dopegit, there is a need for transfusion, then before the blood transfusion it is necessary to perform both a direct and an indirect Coombs test. In the absence of hemolytic anemia, only the direct Coombs test is usually positive. Positive direct Coombs test does not affect the determination of the blood group and the result of the sample for cross-compatibility.If the indirect Coombs test is also positive, then there may be difficulties in assessing cross-compatibility. In such cases, a consultation of a hematologist or transfusiologist is necessary.

In rare cases, against the background of methyldopa therapy, reversible leukopenia and granulocytopenia were observed. After cessation of therapy, the amount of granulocytes returned to normal. In addition, patients who took methyldopa had rare cases of reversible thrombocytopenia.

Some patients experienced fever during the first three weeks of therapy with the drug, which was sometimes accompanied by eosinophilia or increased hepatic transaminase activity. In addition, the reception of methyldopa may be accompanied by the development of jaundice. Jaundice usually appears during the first 2-3 months of therapy. In some cases, against a background of jaundice, cholestasis was confirmed. Very rarely, patients developed fatal necrotizing hepatitis. A liver biopsy performed in several patients with impaired function of this organ showed microscopic focal necrosis, characteristic of drug hypersensitivity.Before starting Dopegit, at 6 and 12 weeks of treatment, as well as at any time when unexplained fever occurs, it is recommended to determine the activity of hepatic transaminases and an overall blood test with a leukocyte formula.

When fever, jaundice or increased activity of liver transaminases, taking Dopegit should be stopped immediately. If the appearance of these signs is associated with hypersensitivity to methyldopa, then after the drug is abolished the fever will disappear, and the functional liver tests will return to normal values. Renewal of the drug to such patients is not recommended. Patients with a history of liver disease in the history of therapy with Dopegit should be treated with extreme caution.

Patients taking Dopegit may need to reduce the dose of anesthetics. With the development of hypotension during general anesthesia, it is recommended to use vasopressor therapy. Adrenergic receptors do not lose their sensitivity against methyldopa therapy.

Some patients taking methyldopa develop peripheral edema, and body weight increases. These side effects can easily be eliminated with diuretics.With the growth of edema and the appearance of symptoms of heart failure, Dopegit should be discontinued.

Since methyldopa is removed from the body by dialysis, the blood pressure can increase after the session is over.

In patients with bilateral cerebral vascular lesions (cerebrovascular disease), methyldopa may be accompanied by involuntary choreoathetotic movements. In such cases, therapy with the drug should be discontinued.

The drug Dopegit must be used with great care in the treatment of patients with hepatic porphyria and their close relatives.

Dopegit therapy can affect the results of measuring the concentration of uric acid (using a phosphoric-tungsten reagent), creatinine (using alkaline picrate), and AST (calorimetric method) in blood serum. The effect of methyldopa therapy on the spectrophotometric analysis of the AST concentration was not reported.

Against the background of methyldopa therapy, false positive results can be obtained in determining the content of catecholamines in the urine by a fluorescent method, which complicates the diagnosis of pheochromocytoma.At the same time, methyldopa has no effect on the evaluation of the concentration of vanillylmandelic acid in the urine.

In rare cases in the air, the urine of patients taking methyldopa can darken. This effect is associated with the decomposition of methyldopa and its metabolites. Do not drink alcohol while taking Dopegit.

Impact on the ability to drive vehicles and manage mechanisms

Dopegit therapy may be accompanied by sedative effects, which are usually transient and develop at the beginning of treatment or with an increase in the dose of the drug. In the development of such effects, patients should not carry out activities that require increased attention, for example, to drive vehicles or mechanisms.

Drug Interactions

Dopegit can not be used concomitantly with MAO inhibitors.

Simultaneous use with the following medicines requires special care.

Drugs that reduce the antihypertensive effect of the drug Dopegit: sympathomimetics (enhance the pressor effect), tricyclic antidepressants, phenothiazines (at the same time they may have an additive antihypertensive effect),iron preparations for oral administration (they can reduce the bioavailability of methyldopa), non-steroidal anti-inflammatory drugs (NSAIDs), estrogen preparations.

Drugs that enhance the antihypertensive effect of the drug Dopegit: other antihypertensive drugs, beta-adrenoblockers (strengthening antihypertensive effect), levodopa + carbidopa (orthostatic hypotension may develop, in this case, patients after taking drugs should be in a horizontal position for 1-2 hours) , general anesthetics, anxiolytic drugs (tranquilizers).

Dopegit and the following drugs can change each other's effects: lithium (the danger of increasing lithium toxicity), levodopa (a decrease in the antiparkinsonic effect and an increase in undesirable effects on the central nervous system), ethanol (alcohol) and other drugs that depress the central nervous system (increased depression), anticoagulants effect, danger of bleeding), Bromocriptine (possibly an undesirable effect on the concentration of prolactin), Haloperidol (possibly disruption of cognitive functions - disorientation and confused state of consciousness).

Analogues of the drug Dopegit

Structural analogs for the active substance:

• Aldomet;
• Dopanol.

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