DOPEGYT instructions for use, description of the drug DOPEGYT: contraindications, side effects, dosages, composition

Release form and composition

Dopegyt is produced in the form of tablets: grayish-white or white, round, flat, with a bevel and the inscription “DOPEGYT” on one side, odorless or almost odorless (50 pieces in brown glass bottles, 1 bottle in a cardboard box ).

1 tablet contains:

Active substance: methyldopa – 250 mg (in the form of methyldopa sesquihydrate – 282 mg);
Auxiliary components: talc – 6 mg; stearic acid – 3 mg; corn starch – 45.7 mg; sodium carboxymethyl starch – 3.5 mg; ethylcellulose – 8.8 mg; Magnesium stearate – 1 mg.

Undesirable consequences

Unexpected events are possible at the very beginning of the course of therapy or after dose titration. Side symptoms can be recognized by headache, loss of energy, slow reaction time, and deterioration in sleep quality. After adaptation or dose reduction, the condition normalizes on its own. The list of signs of side effects can be supplemented:

Arthralgia, myalgia;
Parkinson's disease, paresthesia;
Epidermal necrolysis;
Hyperprolactinemia, amenorrhea, gynecomastia;
Drug fever;
Pancreatitis, vasculitis;
Dyspeptic disorders;
Disorders of defecation rhythm;
Cholestasis, jaundice;
Pericarditis, progression of coronary heart disease;
Myocarditis, CHF.

After a long course, tests may show a positive reaction to humoral immunity, which indicates immune hemolytic anemia.

Contraindications

Hemolytic anemia;
Depression;
Pheochromocytoma;
Acute myocardial infarction;
Liver cirrhosis, acute hepatitis;
History of liver disease (when taking methyldopa);
Concomitant therapy with monoamine oxidase inhibitors;
Age up to 3 years;
Hypersensitivity to the components of the drug.

Lactating and pregnant women can take Dopegit only after assessing the benefit/risk ratio for the health of the mother and child.

Dopegit should be taken with caution by children over 3 years of age, elderly patients, as well as patients with renal failure (dose adjustment required) and diencephalic syndrome.

Pharmacokinetics

Suction

After oral administration, approximately 50% of alpha-methyldopa is absorbed.

Distribution

Slightly (less than 20%) binds to blood plasma proteins. Methyldopa crosses the placental barrier and is excreted in breast milk.

Metabolism

Metabolized in the liver to form an active metabolite - alpha-methylnorepinephrine and other metabolites.

Removal

It is excreted mainly in the urine. About 70% of the absorbed active substance is excreted in the urine in the form of methyldopa and its sulfoconjugates, the rest is excreted in the feces in the form of methyldopa.

With normal renal function, T1/2 is 1.7 hours. The active component of the drug is completely eliminated from the body within 36 hours.

Pharmacokinetics in special clinical situations

In renal failure, the elimination of methyldopa slows down according to the degree of renal dysfunction. In case of severe renal impairment (without hemodialysis), T1/2 of methyldopa increases 10 times.

Methyldopa is eliminated during hemodialysis. 6-hour hemodialysis can remove 60% of the absorbed dose of methyldopa from the circulating blood, peritoneal dialysis for 20-30 hours removes approximately 22-39%.

Directions for use and dosage

Dopegit should be taken orally; the drug can be taken before or after meals.

The doctor sets the dosage regimen individually.

Pharmacological characteristics

Dopegin is a centrally acting drug with antihypertensive properties. After oral administration, central inhibitory presynaptic alpha2 receptors are stimulated, helping to reduce sympathetic tone. Under the influence of the medication, the performance of renin in the blood is inhibited, and the peripheral vascular resistance is also reduced.

The active component of the drug inhibits the synthesis of norepinephrine, reduces the level of serotonin and adrenaline. Methyldopa does not directly affect the myocardium and does not contribute to the appearance of tachycardia, as is often the case with other antihypertensive medications. With long-term use of the drug, blood pressure is normalized, and the achieved level is maintained both without physical activity and with adequate muscle loads.

After consuming the tablet, it is quickly absorbed into the tissue. The maximum concentration of the active component is observed after 6 hours and is maintained for 12-24 hours.

Side effects

At the beginning of treatment, as well as with an increase in the dose of Dopegyt, headache, transient sedative effects, increased fatigue and general weakness may be observed.

Also, when using the drug, it is possible to develop disorders of certain body systems, which manifest themselves with varying frequencies:

Central nervous system: very rarely – parkinsonism; in some cases - Bell's palsy (peripheral paralysis of the facial nerve), involuntary choreoathetotic motor activity, decreased intelligence, decreased libido, mental disorders (including nightmares, depression and mild psychosis), paresthesia, symptoms of cerebrovascular insufficiency, headache, dizziness, sedation, increased fatigue or general weakness;
Cardiovascular system: very rarely - pericarditis, myocarditis, progression of angina pectoris; in some cases - prolonged hypersensitivity of the carotid sinus, congestive heart failure, orthostatic hypotension (reducing the dose of Dopegyt is recommended), weight gain, peripheral edema, sinus bradycardia (as a rule, weight gain and peripheral edema regress with diuretic therapy. When signs appear heart failure or if edema increases, the drug should be stopped);
Digestive system: very rarely - pancreatitis; in some cases - vomiting, colitis, inflammation of the salivary glands, diarrhea, constipation, nausea, bloating, dry mouth, flatulence, necrotizing hepatitis, hepatitis, jaundice, cholestasis, dark coloration of the tongue or pain;
Respiratory system: in some cases – nasal congestion;
Endocrine system: in some cases - gynecomastia, hyperprolactinemia, amenorrhea, galactorrhea;
Musculoskeletal system: in some cases - myalgia, mild joint pain with or without swelling;
Immune system: in some cases - lupus syndrome, vasculitis, eosinophilia, drug fever;
Skin: in some cases - a rash resembling lichen, toxic epidermal necrolysis or eczema;
Laboratory indicators: very often - positive Coombs test; rarely – leukopenia, hemolytic anemia, thrombocytopenia, granulocytopenia; in some cases - increased activity of liver transaminases, suppression of bone marrow function, LE cells and rheumatoid factor, increased concentration of urea in the blood, positive test results for antinuclear antibodies;
Other: in some cases - ejaculation disorders, impotence.

Overdose

Symptoms:

severe arterial hypotension, severe bradycardia, weakness, drowsiness, lethargy, tremor, dizziness, constipation, flatulence, diarrhea, nausea, vomiting, intestinal atony.

Treatment:

Gastric lavage and induction of vomiting, taken soon after taking the drug, can reduce the amount of absorbed drug. It is necessary to monitor heart rate, blood volume, electrolyte balance, intestinal and kidney function, as well as the brain. If necessary, sympathomimetics (eg, epinephrine) can be administered.

special instructions

In some cases, hemolytic anemia may develop during therapy. When symptoms of the disease appear, the hematocrit and hemoglobin concentration must be determined. When confirming the diagnosis, it is necessary to further evaluate the degree of hemolysis. If hemolytic anemia develops, stop taking Dopegit.

With prolonged therapy, a positive Coombs test may be detected. If this phenomenon does not occur during the first year of taking Dopegyt, its detection in the future is unlikely. This disorder is most rarely observed in patients taking the drug in a daily dose of less than 1 g. If a positive direct Coombs test is detected while taking the drug, it is necessary to exclude the presence of hemolytic anemia in the patient and determine the clinical significance of this phenomenon.

In rare cases, when using Dopegyt, reversible leukopenia and granulocytopenia may occur. As a rule, after stopping treatment, the granulocyte count returns to normal.

Some patients develop fever during the first 21 days of therapy, which in rare cases is accompanied by eosinophilia or increased liver transaminase activity. In addition, the use of Dopegit may be accompanied by the development of jaundice, which appears during the first 2-3 months of therapy. In some cases, cholestasis and fatal necrotizing hepatitis may develop. If unexplained fever occurs, it is recommended to determine the activity of liver transaminases and a complete blood count with a leukocyte formula.

If jaundice, fever or increased activity of liver transaminases develop, therapy should be stopped immediately. If the appearance of these symptoms is associated with hypersensitivity to the active substance of the drug, then after discontinuation of Dopegit, the fever disappears, and liver function tests return to normal values. It is not recommended to restart therapy in such patients. Patients with a history of liver pathology should take Dopegit with extreme caution.

Some patients experience peripheral edema and weight gain during therapy. Such side effects are easily eliminated with the help of diuretics. If symptoms of heart failure and swelling increase, therapy should be discontinued.

Patients taking Dopegyt may require lower doses of anesthetics. If hypotension develops during general anesthesia, vasopressor therapy should be used.

With bilateral damage to the cerebral vessels (cerebrovascular disease), taking Dopegit may be accompanied by involuntary choreoathetotic movements. In this case, therapy is stopped.

The drug should be used with great caution when treating patients with hepatic porphyria and their close relatives.

Dopegyt may interfere with measurements of serum uric acid, creatinine and aspartate aminotransferase concentrations. It is also possible to obtain false-positive results for determining the content of catecholamines in urine using the fluorescent method, which can complicate the diagnosis of pheochromocytoma.

During therapy you should not drink alcoholic beverages.

Taking Dopegit may be accompanied by sedative effects, which, as a rule, are transient and develop at the beginning of therapy or with an increase in the dose taken. In this case, patients should not perform work that requires increased attention, for example, driving vehicles or machinery.

Is Dopegit safe for pregnant women?

Clinical studies of the effect of the drug on the body of pregnant women did not reveal complications when using Dopegyt in the 2-3rd trimesters of pregnancy. But in any case, the responsibility for choosing a medication during the gestational period lies with the doctor, who evaluates the benefits and potential risks for the woman and child.

The results of a study of pregnant women over 26 weeks show a complete absence of adverse events after taking Doppegit.

Residues of Dopegyt were detected in breast milk, so it is advisable to switch the baby to alternative nutrition options during treatment while breastfeeding.

Drug interactions

The simultaneous use of Dopegit with the following drugs requires special caution:

Sympathomimetics, tricyclic antidepressants, phenothiazines, oral iron preparations, estrogenic drugs, non-steroidal anti-inflammatory drugs: decreased antihypertensive effect of Dopegyt;
Other antihypertensive drugs, general anesthetics, anxiolytic drugs, beta-blockers, levodopa with carbidopa: increased antihypertensive effect of Dopegyt;
Levodopa, lithium, anticoagulants, ethanol and other drugs that depress the central nervous system, haloperidol, bromocriptine: changes in the effects of these drugs and Dopegyt.

Dopegit cannot be used simultaneously with monoamine oxidase inhibitors.

Interactions with other medicinal drugs and other types of interactions

With special care, it is necessary to take Dopegit® in combination with any of the following drugs:

sympathomimetics (can enhance the vasopressor effect);
tricyclic antidepressants;
phenothiazines;
drugs for oral administration (the bioavailability of methyldopa may be reduced);
non-steroidal anti-inflammatory drugs;
estrogen.

The antihypertensive effect of methyldopa is enhanced when combined with other antihypertensive drugs and anesthetics.

If you take one-hour treatment with antihypertensive medications, you can avoid idiosyncrasy.

Methyldopa and lower-prescribed drugs may alter the effect of either:

lithium (may increase the toxicity of lithium);
levodopa [change in antiparkinsonian effect, strengthening of unpleasant influx on the central nervous system (CNS)];
alcohol and drugs that depress the central nervous system (increasingly depressant effect on the central nervous system);
anticoagulants (the anticoagulant effect is developing, the risk of bleeding);
bromocriptine (may have an adverse effect on prolactin concentration).

Overdose

Symptoms

: marked arterial hypotension, marked drowsiness, weakness, bradycardia, confusion, constipation, bloating, flatulence, diarrhea, boredom, vomiting.

Likuvannya

: immediately after overdosing - rinsing the tube; Induction of vomiting may change the amount of drug absorbed. If the drug has already been soaked, it can be removed from the section by taking an internal infusion. Necessary monitoring of heart rate, blood volume, electrolyte balance, bowel function, neuronal function and brain function. Likuvannya is more symptomatic.

Features of good stagnation

Before treatment with methyldopa, it is necessary to perform a blood test, and after the first 6–10 years of treatment, perform a Coombs test, which must be repeated through the skin 0.5–1 times during daily treatment. 10–20% of patients who were exposed to methyldopa had a positive Coombs test, especially if they took more than 1 g of methyldopa per 0.5–1 dose dose.

Single episodes of hemolytic anemia become more frequent during treatment with methyldopa. Once symptoms of anemia appear, it is necessary to measure the level of hemoglobin and hematocrit. Once the presence of anemia is confirmed, further investigations should be carried out to determine the stage of hemolysis. If hemolytic anemia is detected, take the drug Dopegit.

After taking the drug, hemolytic anemia disappeared. In some episodes, treatment with steroids was necessary. Administered treatment with methyldopa (with or without the addition of a corticosteroid) should lead to a rapid remission. However, lethal attacks were dealt with one by one. This also accounts for the possibility of other causes for the development of hemolytic anemia. If hemolytic anemia was caused by methyldopa, taking the drug as a precaution. A positive Coombs test becomes negative for several years or months after methyldopa treatment.

A positive Coombs test is not a contraindication for methyldopa therapy. If a positive Coombs test is detected during treatment with methyldopa, the physician must exclude the possibility of hemolytic anemia or determine whether a positive Coombs test has any clinical significance. A problem may arise if the patient requires a blood transfusion. In this case, it is necessary to conduct a direct and indirect Coombs test. If hemolytic anemia is present, the direct Coombs test will be positive. If the indirect Coombs test is also positive, there may be problems. In this case, assistance from a blood transfusion specialist or hematologist is required.

In the first 6–12 years of age, or in cases of uneasy walking, it is necessary to investigate the function of the liver. To be wary of changes in the liver enzyme system or hypersensitivity, avoid a hypersensitivity reaction that can cause cholestasis, hepatocellular damage or hepatitis. It is very rare that liver necrosis and lethal consequences can occur. If you are concerned about changes in the enzyme system of the liver or liver failure, dosage with methyldopa should be taken immediately. These patients are not at all to blame for taking methyldopa again. If body temperature and indicators of liver function, impaired by methyldopa, returned to normal after administration of the drug, methyldopa should no longer be prescribed to these patients.

Patients with a history of liver disease or impaired liver function require special care when treated with methyldopa.

Granulocytopenia and thrombocytopenia can develop very rarely. The stench begins to fade away when you take a bath with methyldopa.

Some patients treated with methyldopa may experience swelling or an increase in body weight that can be treated with additional sechoginic treatment. Do not continue the methyldopa bath, otherwise the swelling will increase or symptoms of heart failure will develop.

Methyldopa is available for additional dialysis. Therefore, after this procedure, arterial hypertension may recur (see also section “Method of administration and dosage”).

Methyldopa fragments fluoresce at the same time as catecholamines, and a large number of catecholamines may be detected in the sample, which indicates the development of pheochromocytoma. It is important to recognize this phenomenon before a patient with a possible pheochromocytoma undergoes surgery. Treatment of patients with catecholamine-secreting tumors such as pheochromocytoma or paraganglioma is contraindicated.

However, methyldopa does not interfere with the absorption of vanillyl mygdalic acid (VMA).

Patients treated with methyldopa should be prescribed lower doses of anesthetics. If arterial hypotension develops during the hour of anesthesia, it is possible to control the stagnation of vasodilatory functions. Adrenergic receptors are deprived of the sensitive traction of methyldopa treatment (see also section “Interactions with other drugs and other types of interactions”).

Patients with severe bilateral cerebrovascular diseases can rarely avoid fleeting pathological changes in the body. If you are afraid of the appearance of pathological ruins, it is important to take methyldopa.

Methyldopa should be administered with special care to patients whose close relatives suffer from hepatic porphyria.

Before drinking methyldopa, it is necessary to avoid intoxication with alcoholic drinks.

When taking methyldopa, you may be wary of reversal leukopenia and fever.

Also beware of changes in laboratory tests, such as darkening of the section due to the breakdown of methyldopium or its metabolites.

Methyldopa may interfere with the measured concentrations of sechoic acid in the phosphotungstate method, creatinine in blood serum using the medicinal acid method, and aspartate aminotransferase (AST (SGOT)) in the colorimetric method.

There was no evidence of infusion of methyldope into AST (SGOT) values in spectrophotometric methods.

Suspension during pregnancy or breastfeeding.

Treatment of arterial hypertension in pregnant women with methyldopa must be carried out under the watchful eye of a doctor.

During the treatment with the drug in pregnant women or women who are breastfeeding, there was no evidence of excessive flow into the fetus or newborn.

In published reports about methyldopa treatment in all trimesters of pregnancy, there is information about the effectiveness of a long-term, slow infusion of the drug into the pregnancy.

Methyldopa penetrates the placental barrier, breast milk and umbilical cord blood.

Although no information about teratogenic influx was found in the pregnancy, the influx risk should not be turned off. Medicinal intake can be prescribed to pregnant women or women who are planning to become pregnant, as well as women who are breastfeeding, in which case the crust outweighs the potency.

This is due to the fluidity of the reaction during treatment with vehicles or other mechanisms.

During the hour of treatment with the drug, it is necessary to avoid the use of vehicles and potentially unsafe types of activities that require concentration of attention.