Sinusitis

What is Dopegit taken for? Dopegit - rules of use for different ages

High blood pressure is observed in a large part of the population, and one of the predisposing factors is pregnancy, for which Dopegit is often prescribed. Hypertension is accompanied by nausea, dizziness, weakness and other characteristic symptoms that are relieved by the drug. “Dopegit” for blood pressure during pregnancy is prescribed in 70% of cases, since the drug has a minimum number of side effects and contraindications for the mother and fetus.

Release form and dosage composition

“Dopegit” for high blood pressure is taken in the form of tablets; they have a characteristic inscription on one side. There is a smell, but it is elusive to humans. Sold in darkened glass bottles of 50 pcs. The cardboard package contains 1 bottle.

Each tablet consists of:

active ingredient: methyldopa 250 mg;
additional substances: corn starch (45 mg), ethylcellulose (8.8 mg), talc (6 mg), sodium carboxymethyl starch (3.5 mg), stearin acid (3 mg), magnesium stearate (1 mg).

Indications for use

The drug is prescribed when hypertension occurs. Mainly used in II and III degrees of severity. "Dopegit" can be used during pregnancy.

The components of the medication have a calming effect on the central nervous system, reduce blood pressure and keep it in a normal state for a long time.

Contraindications

Among the obvious contraindications to the drug "Dopegit" for blood pressure include:

depression;
anemia of hemolytic origin;
acute form of myocardial infarction;
pheochromocytoma;
acute forms of liver pathology;
concurrent treatment with monoamine oxidase inhibitors;
children under 3 years of age;
excessive sensitivity to the drug or components.

Dopegit anti-pressure tablets for pregnant women are prescribed based on an assessment of the degree of risk and expected health benefits. For children, the drug can be prescribed only from 3 years of age and with extreme caution. It is also recommended for elderly people, patients with diencephalic syndrome and kidney failure to take precautions.

Directions for use

"Dopegit" is indicated for oral use before or after meals. The dosage is selected individually according to health indicators.

Use during pregnancy and breastfeeding

According to the research results, no signs of the drug’s effect on the child were established. The drug has no effect in any trimester of treatment. But doctors recommend using “Dopegit” blood pressure pills during pregnancy only under strict indications.

Adverse reactions and overdose

Potential adverse reactions include:

the onset of daytime drowsiness, lethargy, reactions become inhibited. The onset of headaches and dizziness is often noted. Sometimes there is severe paralysis of the nerves of the face, deviation in coordination;

Sharp decrease in blood pressure

orthostatic hypertension, edema in peripheral vessels, decreased heart rate, redness of the chest and face, aggravation of the condition in heart failure, angina pectoris. Myocarditis and pericarditis are less common;
glossalgia, nausea with vomiting, drying of the oral mucosa, diarrhea, pancreatitis, jaundice of the skin, colitis, increased renal transaminase function;
myalgia, arthralgia;
decreased libido, deterioration of potency, amenorrhea;
hemolytic anemia, thrombocytopenia, leukopenia, and agranulocytosis;
fever, rash, Lyell's syndrome, exanthema;
gynecomastia, galactorrhea, hyperprolactinemia;
inflammatory processes in the salivary glands and blockage of the nasal sinuses.

In case of an overdose, the following symptoms may occur:

severe hypotension;
weakness, drowsiness, lethargy;
severe slowing of heart rate;
tremor;
dizziness;
flatulence;
diarrhea alternating with constipation;
nausea developing into vomiting, intestinal atony.

General weakness

Interaction of the drug with other drugs

Concomitant use with certain medications should be done with caution:

1 tablet contains 250 mg of the active substance methyldopa (in the form of methyldopa sesquihydrate).

Additional components are: ethylcellulose, talc, magnesium stearate, starch, sodium carboxymethyl starch, stearic acid.

Release form

Dopegit is available in tablet dosage form.

Pharmacological action

Central alpha-2 agonist.

Pharmacodynamics and pharmacokinetics

The active component is . The drug reduces heart rate and IOC, providing a hypotensive effect and reducing peripheral vascular resistance. In the central nervous system, a metabolite of the drug is formed - alpha-methylnorepinephrine, under the influence of which vascular tone decreases and slows down sympathetic impulse . The medication moderately suppresses activity, causes orthostatic hypotension, reduces peripheral vascular resistance, and reduces tissue concentration , dopamine, . Dopegit does not have a significant effect on renal blood flow and IOC, but increases plasma volume. Long-term therapy leads to regression of the size of the hypertrophied left ventricle, an increase is observed in the myocardium collagen .

Taking the first dose leads to short-term hypertension. During periods of intense physical activity, the severity decreases. hypotensive effect . The drug promotes the retention of water and sodium ions in the body, slows down the sinus rhythm, increases the activity of baroreceptors, which leads to the possible development of refractoriness with long-term therapy (1-1.5 months). The medicine is characterized by withdrawal syndrome . Dopegit can cause sedation, the severity of which decreases 2-3 weeks after the start of therapy.

The maximum drop in blood pressure is recorded after 4-6 hours, the effect lasts 1-2 days. The severity of the hypotensive effect increases gradually. With intravenous infusion of the drug, a drop is recorded after 2-3 hours, a peak is noted after 3-5 hours, the effect lasts 6-10 hours. The drug increases renal blood flow.

Indications for use

Contraindications

Dopegit is not used for acute hepatitis , intolerance to methyldopa, in acute, systemic connective tissue diseases, severe pathology of the liver and renal system, pheochromocytoma , depression, cerebral vessels , at hemolytic anemia , simultaneous therapy with levodopa and MAO inhibitors, with severe coronary atherosclerosis .

In case of diencephalic syndrome, acute left ventricular failure, or a history of hepatitis, the medication is prescribed with caution.

Side effects

Nervous system: spontaneous choreoathetoid movements of the limbs, parkinsonism, lethargy, dizziness, staggering when walking, headaches, facial paralysis , lethargy and drowsiness.

Cardiovascular system: pericarditis , hyperemia of the skin of the upper body, peripheral edema, bradycardia, orthostatic hypotension , myocarditis, worsening heart failure.

Digestive tract: jaundice, hepatotoxicity, increased liver enzymes, vomiting, diarrhea, dry mouth, nausea.

Blood-forming organs: thrombocytopenia, agranulocytosis , hemolytic anemia, leukopenia.

Musculoskeletal system: development of arthralgia, myalgia.

Endocrine system: decreased libido, amenorrhea, decreased potency.

Combined therapy with beta-blockers causes orthostatic hypotension and may increase blood pressure.

An increase in the hypotensive effect is observed when prescribing diuretic medications and hydralazine .

Simultaneous therapy with adrenergic stimulants and NSAIDs leads to a decrease in the severity of the hypotensive effect.

Tranquilizers (anxiolytics) can enhance the hypotensive effect. When the urine becomes acidic while taking methyldopa, its effect decreases; when it becomes alkalized, it increases. Patients receiving methyldopa during general anesthesia may develop collaptoid states Therefore, the drug is discontinued 7-10 days before the proposed surgery.

Dopegit is prescribed with caution to patients receiving and other medications for general anesthesia. Ethyl ether contraindicated.

The drug is incompatible with procainamide, quinidine , neuroleptics.

Dopegit can enhance hepatotoxicity oral contraceptives; increase the toxicity of lithium salts.

Dopegit during pregnancy

According to the instructions, the tablets are not recommended for use during pregnancy, since there is an assumption that the drug may be harmful to the child, although there is no clinical evidence of this, and reviews of Dopegyt during pregnancy also do not contain information about the harmful effects of the drug.

The active substance penetrates the placental barrier. Dopegyt can pass into mother's milk during breastfeeding.

If the medicine has been prescribed, it should be taken under the strict supervision of a doctor.

Thus, a drug can only be prescribed if the potential benefit to the mother is greater than the potential harm to the baby.

Analogs

Analogues can be called drugs Dopanol And Aldomet .

Dopegyt is a drug used to eliminate hypertension, high blood pressure (BP).

Dopegit is the proprietary name of the drug. The active ingredient in it is Methyldopa.

This substance from the class of phenylethylamines is a white or white-yellow crystalline powder, highly soluble in water.

Chemical formula: C 10 H 13 NO 4.

Names: (-)3-(3,4-Dioxyphenyl)-2-methylalanine, or 3-hydroxy-a-methyl L-tyrosine.

Mechanism of action

Dopegit is an antihypertensive drug with a central mechanism of action. It affects the vasomotor center of the medulla oblongata by stimulating alpha-2 adrenergic receptors. Typically, stimulation of sympathetic neurons of the vasomotor center leads to spasm of arterial vessels and an increase in blood pressure.

The transmission of nerve impulses through the contacts between these neurons (synapses) is ensured by the transmitter norepinephrine. Alpha-2 adrenergic receptors are located on the membrane of the presynaptic (located in front of the synapse) neuron.

The effect of norepinephrine on these receptors leads to a decrease in the amount of norepinephrine and to difficulty in conducting sympathetic nerve impulses in the vasomotor center. It turns out that norepinephrine itself inhibits its release.

Apparently, this physiological mechanism, called a negative feedback loop, is created by nature to regulate blood pressure and prevent the development of uncontrolled hypertension.

Thus, activation of alpha-2 adrenergic receptors on the presynaptic membrane by Dopegyt according to the principle of negative feedback leads to a decrease in the amount of norepinephrine.

The conduction of nerve impulses in the vasomotor center is hampered, and vascular spasm is eliminated. But this is not the only way Dopegit influences blood pressure.

The bottom line is that the propagation of nerve impulses along sympathetic fibers in the central nervous system, in addition to norepinephrine, is also ensured by other neurotransmitters - adrenaline, dopamine, serotonin.

Dopegyt inhibits the synthesis of these mediators. This is achieved by inhibiting the specific enzyme dopa decarboxylase. In addition, Dopegite, acting as a false neurotransmitter, binds to dopaminergic receptors, and in this way interferes with the action of dopamine as a neurotransmitter.

All these central effects are provided not by Dopegite itself, but by its metabolite, alpha-methylnorepinephrine, which is formed in the liver and then penetrates the BBB - the blood-brain barrier.

The peripheral effect of Dopegyt manifests itself in improving renal blood flow and enhancing glomerular filtration. Renin secretion by the kidneys, on the contrary, decreases.

Renin is an enzyme that plays a key role in the RAAS (renin-angiotensin-aldosterone system). Under the influence of the components of the RAAS, the main mechanisms of hypertension are triggered - vasoconstriction (vascular spasm), retention of water and sodium salts in the body.

Thus, the central and peripheral action of Dopegit is aimed at hypotension. Hypotension in this case is achieved by reducing TPR (total peripheral resistance) as a result of expansion of the lumen of small arteries (arterioles).

The drug has virtually no effect on the contractile function of the myocardium. However, a decrease in OPS and blood pressure can reflexively lead to a decrease in heart rate and a decrease in the strength of heart contractions. This is manifested by a decrease in cardiac output - the volume of blood pushed by the myocardium through the blood vessels.

In addition, it has been established that Dopegit, with long-term use, reduces the collagen content in the muscle fibers of the heart. Clinically, this is manifested by the elimination of myocardial hypertrophy and cardiosclerosis - the main structural changes in cardiovascular pathology.

The central action of Dopegit, aimed at reducing the activity of neurotransmitters, in addition to hypotension, is often manifested by sedation. The sedative effect is manifested by calming, eliminating feelings of anxiety and fear.

However, with long-term use of Dopegyt, resistance and addiction occur. Resistance is due to activation of baroreceptors. These receptors are located on the inner vascular wall. They respond to changes in intravascular pressure.

Pressure increases - baroreceptors trigger the process of vasodilation; pressure decreases - blood vessels spasm. Dopegit is characterized by a withdrawal syndrome - worsening hypertension when taking the drug abruptly. Another negative point: Dopegit promotes sodium and water retention in the body. This is manifested by edema syndrome and hypertension.

History of creation

The drug was synthesized and began to be produced in the 60s of the twentieth century. in Hungary by the pharmaceutical plant Egis. Currently, this company is better known as Egis Pharmaceutical Plant OJSC or “Egis” Pharmaceutical Ltd. Over these decades, Dopegit as an effective antihypertensive agent has been widely used in Russia and in many other countries.

Synthesis technology

Methyldopa, like other phenylephrines, is obtained through organic synthesis reactions. One of the methods is the reductive amination of ammonia compounds in the presence of a nickel catalyst.

Release form

Tablets 250 mg.

Dopegit, produced by EGIS, does not have generics. However, in clinical practice, along with Dopegit, other centrally acting antihypertensive drugs are also used.

These are Moxonidine (Physiotens, Tenzotran), Rilmenidine (Albarel), Clonidine (Clonidine, Gemiton). These medicines contain other active substances. Their mechanism of action is similar to that of Methyldopa, but may differ slightly from it.

Indications

The drug is prescribed for arterial hypertension.

Dosages

This dose is divided into 2-4 doses. Given the sedative effect of the drug, it is recommended to start increasing the dose with an evening dose. The tablets are taken whole, not chewed, before or after meals. The maximum daily dose of the drug is 2 g.

Elderly patients are recommended to start taking Dopegite at a daily dose of 250 mg (1 tablet). In the future, if there is no desired effect, the dosage can be increased, but not more than 250 mg over 2 days. In children, the average daily dose of the drug is determined at the rate of 10 mg/kg body weight, which is divided into 2-4 doses.

If necessary, the daily dose can be increased, but not more than 65 mg/kg body weight. Given that the drug is excreted by the kidneys, in case of renal failure its elimination may be slowed down. Therefore, patients with renal failure should observe certain time intervals between doses.

The duration of these intervals depends on the degree of renal failure. With a mild degree it is 8 hours, with a moderate degree – 8-12 hours, with a severe degree – 12-24 hours.

With long-term use of Dopegyt, tolerance develops. This manifests itself in a weakening of the hypotensive effect after 2-3 months of regular use of the medicine. In these cases, it is recommended to increase the dose, or combine Dopegit with other antihypertensive and diuretics, in particular with Hypothiazide.

In addition, Dopegit is used with other antihypertensive drugs with their smooth gradual withdrawal. In these cases, the daily dose of Dopegit should not exceed 500 mg.

Pharmacodynamics

About 50% (according to various sources - from 8 to 62%) of the drug taken orally is absorbed into the gastrointestinal tract. Less than 20% of absorbed Methyldopa is bound to plasma proteins.

In the liver, 10% of methyldopa taken orally is metabolized first to form alpha-methyldopamine and then alpha-methylnorepinephrine. It is this active metabolite, alpha-norepinephrine, that crosses the BBB. The hypotensive effect reaches its maximum 4-6 hours after administration and lasts 12-24 hours. When used again, it lasts for 2-3 days.

The drug accumulates in the body. The majority (70%) is excreted in the urine in the form of Methyldopa and metabolites, the rest is excreted in the feces in the form of Methyldopa. The half-life is 1.7 hours.

It is completely eliminated within the next 36 hours. Alkalinization of urine increases the duration of action of Methyldopa, and acidification, on the contrary, reduces it. In patients with insufficient renal function, the elimination time of Methyldopa may be significantly prolonged. After completely stopping the drug, blood pressure returns to its original values within 1-2 days.

Side effects

CNS: headache, dizziness, general weakness, fatigue, paresthesia. Rarely – parkinsonism, peripheral facial palsy, cerebrovascular insufficiency, mental changes, decreased intelligence.
Cardiovascular system: hypotension, bradycardia, edema syndrome, due to edema - increased body weight. Rarely: myocarditis, pericarditis, increased frequency of angina attacks, congestive heart failure.
Gastrointestinal tract: nausea, vomiting, bloating, abdominal pain, flatulence, diarrhea, colitis, pancreatitis, cholestatic jaundice, inflammation of the salivary glands, dry mouth.
Respiratory system: nasal congestion.
Skin: exanthema, toxic epidermal necrolysis, eczema.
Immune system: vasculitis due to fever, lupus syndrome.
Endocrine system: gynecomastia, galactorrhea, hyperprolactinemia.
Musculoskeletal system: arthralgia, myalgia.
Reproductive system: decreased libido, in men - erectile dysfunction, difficulty ejaculating, in women - amenorrhea.
Blood: eosinophilia, lupus cells, positive rheumatoid factor, increased levels of liver transaminases, urea, bilirubin. Sometimes there is insufficiency of bone marrow function, and, as a consequence, inhibition of the synthesis of all blood elements, anemia, leukopenia, agranulocytopenia, thrombocytopenia. Immunity decreases and the risk of spontaneous bleeding increases.

Contraindications

Individual intolerance to the drug;
Acute myocardial infarction;
Acute hepatitis;
Cirrhosis;
Depressive states;
Hemolytic anemia;
Pheochromocytoma;
Concomitant use of MAO inhibitors (monoamine oxidase);
Children under 3 years old.

The drug is prescribed with caution to elderly patients, children over 3 years of age, as well as persons with renal failure and diencephalic syndrome. Given the sedative effect, taking Dopegit is not recommended while driving vehicles or working with complex and potentially dangerous machines and mechanisms.

Interaction with other drugs

MAO inhibitors – uncontrolled hypotension, or vice versa, hypertensive crisis, psychomotor agitation;
Tricyclic antidepressants – decreased hypotensive effect, tachycardia, agitation, headache;
Levodopa – increased hypotensive and decreased antiparkinsonian effect, toxic effect on the central nervous system;
Sympathomimetics, iron supplements, estrogens, NSAIDs – decreased hypotensive effect;
Diuretics, antihypertensive drugs of other groups, including beta-blockers, as well as tranquilizers and anesthetics - enhance the hypotensive effect;
Ethyl alcohol – central nervous system depression, increased depression;
Lithium salts, contraceptives - increased toxicity of these drugs, liver damage;
Anticoagulants - the likelihood of spontaneous bleeding increases;
Haloperidol – impaired consciousness, cognitive disorders, dementia;
Digoxin - increases the risk of developing sick sinus syndrome.

Pregnancy and lactation

Methyldopa penetrates the placental barrier. However, no negative changes in the fetus were detected. However, Dopegit, especially in the third trimester of pregnancy, is prescribed according to strict indications.

Sometimes Dopegit is used to relieve hypertensive conditions in pregnant women and to prevent severe gestosis and eclampsia associated with these conditions. With the help of Dopegit, it is possible to reduce blood pressure in pregnant women by 10-20% of the original level.

Dopegyt passes into breast milk. Therefore, during lactation it is prescribed only in exceptional cases. It is recommended to stop breastfeeding.

Storage

Store at temperatures from 15 to 25 0 C. Shelf life – 5 years. The drug is available with a doctor's prescription.

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Dear visitors of the Farmamir website. This article does not constitute medical advice and should not serve as a substitute for consultation with a physician.

Active ingredient

Methyldopa (methyldopa)

Release form, composition and packaging

Pills white or greyish-white, round, flat, chamfered, engraved with "DOPEGYT" on one side, odorless or almost odorless.

Excipients: ethylcellulose - 8.8 mg, magnesium stearate - 1 mg, corn starch - 45.7 mg, stearic acid - 3 mg, sodium carboxymethyl starch - 3.5 mg, talc - 6 mg.

50 pcs. - brown glass bottles with a PE cap, with first opening control and an accordion shock absorber (1) - cardboard packs.

Pharmacological action

Centrally acting antihypertensive drug. Metabolized to form alpha-methylnorepinephrine, which has a hypotensive effect through several mechanisms:

- reduction of sympathetic tone by stimulation of central inhibitory presynaptic α 2 receptors;

- replacement of endogenous at dopaminergic nerve endings (as a false neurotransmitter);

- decrease in plasma renin activity and decrease in peripheral vascular resistance;

- suppression of norepinephrine synthesis, reduction in the concentration of dopamine, norepinephrine and adrenaline in tissues due to inhibition of the activity of the dopa decarboxylase enzyme.

Methyldopa does not have a direct effect on cardiac function, does not reduce output, does not cause reflex tachycardia, and does not reduce the glomerular filtration rate, renal blood flow, or filtered fraction. In some cases, heart rate decreases. Effectively reduces blood pressure both in the supine and standing positions. 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 reduction in blood pressure is achieved on days 2-3. After cessation of therapy, blood pressure levels return to initial values within 1-2 days.

Pharmacokinetics

Suction

Absorption of methyldopa from the gastrointestinal tract is approximately 50%. After oral administration, the bioavailability of methyldopa is about 25%. Cmax in the blood is reached after 2-3 hours.

Distribution

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

Metabolism

Metabolism of methyldopa occurs intensively. Methyldopa is metabolized primarily in the liver. The active metabolite of methyldopa, alpha-methylnorepinephrine, is formed in adrenergic neurons of the central nervous system. There are also some other methyldopa derivatives that are excreted by the kidneys.

Removal

Approximately two-thirds of absorbed methyldopa is excreted from the body by the kidneys unchanged and also in the form of sulfate compounds. The rest of the drug is excreted through the intestines (also unchanged). The elimination of methyldopa is biphasic. With preserved renal function, T1/2 of the drug is 1.8±0.2 hours. The active substance is completely eliminated from the body within 36 hours. Methyldopa is removed from the body by dialysis. A six-hour hemodialysis session removes approximately 60% of the absorbed dose, while 20-30 hours of peritoneal dialysis removes approximately 22-39% of the drug.

Pharmacokinetics in special clinical situations

If nocturnal function is impaired, the elimination of methyldopa slows down in proportion to the severity of renal failure. In severe renal failure (without hemodialysis), T1/2 of the drug increases approximately 10 times.

Indications

- arterial hypertension.

Contraindications

- acute hepatitis, cirrhosis of the liver;

- history of liver disease (while taking methyldopa);

- concomitant therapy with MAO inhibitors;

- depression;

- hemolytic anemia;

- acute myocardial infarction;

- pheochromocytoma;

- children under 3 years of age (for this dosage form);

- hypersensitivity to the drug.

WITH caution the drug should be prescribed for renal failure (dose adjustment required), diencephalic syndrome, elderly patients and children over 3 years of age.

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 blood pressure reduction). The duration of the intervals between increasing and decreasing the dose of Dopegit should be at least 2 days. Since side sedative effects of the drug may be observed within 2-3 days after the start of therapy, as well as with subsequent increases in the dose, it is recommended to first increase the evening dose of the drug.

The standard maintenance dose of Dopegit is 0.5-2 g/day. This dose is divided into 2-4 doses. The maximum daily dose of the drug should not exceed 3 g. In cases where, while taking the drug at a dose of 2 g/day, there is an insufficiently 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 of blood pressure can be achieved by increasing the dose of the drug or concomitant use of diuretics. 48 hours after stopping therapy with Dopegit, blood pressure usually returns to its original level. There is no “rebound effect” observed.

Dopegit can be prescribed to patients who are already receiving therapy with other antihypertensive drugs, provided that these drugs are gradually withdrawn. In such cases, the initial dose of Dopegit should not exceed 500 mg/day. The dose is increased as needed, at intervals of at least 2 days.

When using Dopegit in addition to previously prescribed antihypertensive therapy, dose adjustment of antihypertensive drugs may be required to ensure a smooth transition.

Elderly patients

Children over 3 years old

For children

Renal dysfunction

Up to 8-12 hours, and at < 30 мл/мин/1.73 м 2) - up to 12-24 hours

Side effects

At the beginning of therapy with Dopegit, as well as with increasing doses of the drug, transient sedative effects, headache, general weakness and increased fatigue may be observed.

Classification of adverse reactions depending on the frequency of occurrence: very often (>1/10), often (from >1/100 to<1/10), нечасто (от >1/1000 to<1/100), редко (от >1/10,000 to< 1/1000), очень редко (<1/10 000), отдельные случаи.

In each of these categories, adverse effects are presented in descending order of severity.

From the cardiovascular system: very rarely - progression of angina pectoris, myocarditis, pericarditis; isolated cases - congestive heart failure, prolonged hypersensitivity of the carotid sinus, orthostatic hypotension (reducing the dose of the drug is recommended), peripheral edema, weight gain, sinus bradycardia.

Peripheral edema and weight gain usually regress with diuretic therapy. If swelling increases or signs of heart failure appear, the drug should be discontinued.

From the side of the central nervous system: very rarely - parkinsonism; isolated cases - peripheral paralysis of the facial nerve (Bell's palsy), decreased intelligence, involuntary choreoathetotic motor activity, symptoms of cerebrovascular insufficiency (possibly as a result of hypotension), mental disorders (including nightmares, usually reversible mild psychosis and depression), headache , sedation (usually transient), general weakness or increased fatigue, dizziness, paresthesia, decreased libido.

From the respiratory system: isolated cases - nasal congestion.

From the digestive system: very rarely - pancreatitis; isolated cases - colitis, vomiting, diarrhea, inflammation of the salivary glands, pain or dark discoloration of the tongue, nausea, constipation, bloating, flatulence, dry mouth, hepatitis, necrotizing hepatitis; cholestasis, jaundice.

From the skin: isolated cases - toxic epidermal necrolysis, eczema or a rash resembling lichen.

From the musculoskeletal system: isolated cases - mild joint pain with or without swelling, myalgia.

From the endocrine system: isolated cases - hyperprolactinemia, gynecomastia, galactorrhea, amenorrhea.

From the immune system: isolated cases - vasculitis, lupus syndrome, drug fever, eosinophilia.

Laboratory indicators: very often - a positive Coombs test; rarely - hemolytic anemia, leukopenia, granulocytopenia, thrombocytopenia; isolated cases - suppression of bone marrow function, positive test results for antinuclear antibodies, LE cells and rheumatoid factor, increased activity of liver transaminases, increased urea concentration in the blood.

Others: individual cases - impotence, ejaculation disorders.

Overdose

Symptoms: marked decrease in blood pressure, dizziness, severe drowsiness, weakness, bradycardia, lethargy, tremor, intestinal atony, constipation, bloating, flatulence, diarrhea, nausea, vomiting.

Treatment: gastric lavage and stimulation of vomiting can reduce the amount of absorbed drug. It is necessary to monitor heart rate, blood volume, water and electrolyte balance, intestinal and kidney function, as well as the brain. If necessary, sympathomimetics (eg, epinephrine) can be administered. There is no specific antidote.

Drug interactions

Dopegit should not be used simultaneously with MAO inhibitors.

Concomitant use with the following medicinal products requires extreme caution.

Drugs, reducing antihypertensive effect of the drug Dopegit: sympathomimetics (increase the pressor effect), tricyclic antidepressants, phenothiazines (at the same time, they may have an additive antihypertensive effect), oral iron preparations (they can reduce the bioavailability of methyldopa), NSAIDs, estrogen drugs.

Drugs, reinforcing antihypertensive effect of the drug Dopegit: other antihypertensive drugs, beta-blockers (increased antihypertensive effect), (orthostatic hypotension may develop, in this case, after taking the drugs, patients should be in a horizontal position for 1-2 hours), general anesthetics, anxiolytic drugs drugs (tranquilizers).

Methyldopa and the following drugs may change effects of each other: lithium (risk of increased lithium toxicity), levodopa (reduced antiparkinsonian effect and increased undesirable effects on the central nervous system), ethanol and other drugs that depress the central nervous system (increased depression), anticoagulants (increased anticoagulant effect, risk of bleeding), bromocriptine (possibly undesirable effect on prolactin concentration), haloperidol (possible impairment of cognitive functions - disorientation and confused state of consciousness).

Special instructions

In rare cases, hemolytic anemia has developed in patients taking methyldopa. If signs of anemia appear, it is necessary to determine the hemoglobin concentration and hematocrit. If anemia is confirmed, the degree of hemolysis should be further assessed. If hemolytic anemia develops, therapy with Dopegit should be discontinued. After cessation of therapy (with or without corticosteroids), remission is usually achieved quickly. However, in rare cases, deaths have been observed. Taking the drug Dopegit is contraindicated in patients with hemolytic anemia that developed during therapy with this drug.

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

Detection of a positive Coombs test in the past or during ongoing therapy is not in itself a contraindication to taking the drug Dopegit. In cases where 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.

Knowledge of previous positive Coombs test results is helpful in assessing blood for crossmatch before transfusion. If, when treating a patient taking the drug Dopegyt, there is a need for a transfusion, then before blood transfusion it is necessary to perform both a direct and indirect Coombs test. In the absence of hemolytic anemia, only the direct Coombs test is usually positive. A positive direct Coombs test does not affect the determination of blood group and the result of the cross-match test. If the indirect Coombs test is also positive, then difficulties may arise in assessing cross-compatibility. In such cases, consultation with a hematologist or transfusiologist is necessary.

In rare cases, the development of reversible leukopenia and granulocytopenia has been observed during methyldopa therapy. After cessation of therapy, the granulocyte count returned to normal. In addition, rare cases of reversible thrombocytopenia have been reported in patients taking methyldopa.

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

If fever, jaundice or increased activity of liver transaminases occurs, the drug Dopegit should be stopped immediately. If the appearance of these signs is associated with hypersensitivity to methyldopa, then after discontinuation of the drug, the fever will disappear and liver function tests will return to normal values. It is not recommended to restart the drug in such patients. Patients with a history of liver pathology should be treated with Dopegit with extreme caution.

Patients taking Dopegyt may require a reduction in anesthetic doses. If hypotension develops during general anesthesia, it is recommended to use vasopressor therapy. Adrenergic receptors do not lose their sensitivity during methyldopa therapy.

Some patients taking methyldopa experience peripheral edema and weight gain. These side effects can be easily managed with diuretics. If edema increases and symptoms of heart failure appear, therapy with Dopegit should be discontinued.

Since methyldopa is removed from the body by dialysis, an increase in blood pressure levels may occur after the session is completed.

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

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

Therapy with Dopegit may affect the results of measuring the concentration of uric acid (using a phosphorus-tungsten reagent), creatinine (using alkaline picrate) and AST (colorimetric method) in blood serum. The effect of methyldopa therapy on spectrophotometric analysis of AST concentrations has not been reported.

During methyldopa therapy, false-positive results may be obtained for determining the content of catecholamines in urine using the fluorescent method, which complicates the diagnosis of pheochromocytoma. At the same time, methyldopa does not affect the assessment of the concentration of vanillylmandelic acid in the urine.

In rare cases, the urine of patients taking methyldopa may darken when exposed to air. This effect is due to the degradation of methyldopa and its metabolites. While taking Dopegit, you should not drink alcoholic beverages.

Impact on the ability to drive vehicles and operate machinery

Therapy with Dopegit may be accompanied by sedative effects, which are usually transient and develop at the beginning of treatment or when the dose of the drug is increased. If such effects develop, patients should not engage in activities that require increased attention, such as operating vehicles or machinery.

Pregnancy and lactation

According to the results of clinical studies after the use of methyldopa in the second and third trimesters of pregnancy, no signs of damage to the fetus or newborn were identified. Since adequate and strictly controlled studies have not been conducted in the third trimester of pregnancy, it is recommended to use the drug only after careful comparison of the expected benefits of therapy for the mother and the potential risk to the fetus.

A study of children born to mothers taking methyldopa after the 26th week of pregnancy found no adverse effects from the drug. In pregnant women who took the drug in the third 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 for the child.

Use in childhood

Children over 3 years old

For children The initial dose of the drug is 10 mg/kg body weight/day. The daily dose is divided into 2-4 doses. If necessary, the dose can be gradually increased until the desired effect is achieved. An interval of at least 2 days must be maintained between increasing the dose of the drug. The maximum daily dose of Dopegit is 65 mg/kg body weight/day, but not more than 3 g/day.

Contraindicated for children under 3 years of age.

For impaired renal function

Methyldopa is excreted primarily by the kidneys, therefore, when treating patients with impaired renal function, the dose of Dopegit must be reduced. At mild renal failure (glomerular filtration rate - 60-89 ml/min/1.73 m2) It is recommended to increase the interval between doses of the drug to 8 hours, with moderate renal failure (glomerular filtration rate - 30-59 ml/min/1.73 m2)- up to 8-12 hours, and when severe renal failure (glomerular filtration rate -< 30 мл/мин/1.73 м 2) - up to 12-24 hours

Methyldopa is removed from the body during dialysis, so it is recommended to use an additional dose of the drug 250 mg to prevent an increase in blood pressure after a hemodialysis session.

For liver dysfunction

Contraindicated in acute hepatitis, liver cirrhosis, and in patients with a history of liver disease that developed while taking methyldopa.

Patients with a history of liver disease or dysfunction should use this drug with extreme caution.

Use in old age

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

Older patients are more likely to experience fainting. This may be due to increased susceptibility to the drug and severe atherosclerotic vascular damage. The development of fainting can be avoided by reducing the dose of Dopegit.

Conditions for dispensing from pharmacies

The drug is available with a prescription.

Storage conditions and periods

The drug should be stored out of the reach of children at a temperature of 15° to 25°C. Shelf life - 5 years.

In this article you can read the instructions for use of the drug Dopegit. Reviews of site visitors - consumers of this medicine, as well as the opinions of specialist doctors on the use of Dopegyt in their practice are presented. We kindly ask you to actively add your reviews about the drug: whether the medicine helped or did not help get rid of the disease, what complications and side effects were observed, perhaps not stated by the manufacturer in the annotation. Analogues of Dopegit in the presence of existing structural analogues. Use for the treatment of arterial hypertension and blood pressure reduction in adults, children, as well as during pregnancy and lactation. Indications and contraindications for taking the drug.

Dopegit- a centrally acting antihypertensive drug. Metabolized to form alpha-methylnorepinephrine, which has a hypotensive effect through several mechanisms:

reduction of sympathetic tone by stimulation of central inhibitory presynaptic alpha2 receptors;
replacement of endogenous dopamine at dopaminergic nerve endings (as a false neurotransmitter);
decrease in plasma renin activity and decrease in peripheral vascular resistance;
suppression of norepinephrine synthesis, reduction in the concentration of dopamine, serotonin, norepinephrine and adrenaline in tissues due to inhibition of the activity of the dopa decarboxylase enzyme.

Methyldopa (the active ingredient of the drug Dopegit) does not have a direct effect on cardiac function, does not reduce cardiac output, does not cause reflex tachycardia, and does not reduce the glomerular filtration rate, renal blood flow, or filterable fraction. In some cases, heart rate decreases. Effectively reduces blood pressure both in the supine and standing positions. Rarely causes postural hypotension.

Compound

Methyldopa sesquihydrate + excipients.

Pharmacokinetics

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

Indications

arterial hypertension (to reduce blood pressure).

Release forms

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 standard maintenance dose of Dopegit is 0.5-2 g per day. This dose is divided into 2-4 doses. The maximum daily dose of the drug should not exceed 3 g. In cases where, while taking the drug at a dose of 2 g per day, an insufficiently effective reduction in blood pressure is observed, it is recommended to combine Dopegit with other antihypertensive drugs. After 2-3 months of therapy, tolerance to methyldopa may develop. Effective reduction of blood pressure can be achieved by increasing the dose of the drug or concomitant use of diuretics. 48 hours after stopping therapy with Dopegit, blood pressure usually returns to its original level. There is no “rebound effect” observed.

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

When using Dopegit in addition to previously prescribed antihypertensive therapy, dose adjustment of antihypertensive drugs may be required to ensure a smooth transition.

Side effect

progression of angina
myocarditis
pericarditis
congestive heart failure
orthostatic hypotension (dose reduction is recommended)
peripheral edema
weight gain
sinus bradycardia
parkinsonism
peripheral facial palsy (Bell's palsy)
decreased intelligence
symptoms of cerebrovascular insufficiency (possibly as a consequence of hypotension)
mental disorders (including nightmares, usually reversible, mild psychosis and depression)
headache
sedation (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 discoloration of the tongue
constipation
bloating
flatulence
dry mouth
jaundice
toxic epidermal necrolysis
eczema or ringworm-like rash
mild joint pain with or without swelling
myalgia
hyperprolactinemia, gynecomastia, galactorrhea, amenorrhea
vasculitis
lupus syndrome
drug fever
eosinophilia
positive Coombs test
hemolytic anemia, leukopenia, granulocytopenia, thrombocytopenia
impotence
ejaculation disorders.

Contraindications

acute hepatitis, liver cirrhosis;
history of liver disease (while taking methyldopa);
concomitant therapy with MAO inhibitors;
depression;
hemolytic anemia;
acute myocardial infarction;
pheochromocytoma;
children under 3 years of age (for tablet form);
hypersensitivity to the drug.

Use during pregnancy and breastfeeding

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

A study of children born to mothers who took Dopegyt 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.

Use in elderly patients

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

Use in children

For children over 3 years of age, the initial dose of the drug is 10 mg/kg body weight per day. The daily dose is divided into 2-4 doses. If necessary, the dose can be gradually increased until the desired effect is achieved. An interval of at least 2 days must be maintained between increasing the dose of the drug. The maximum daily dose of Dopegit is 65 mg/kg body weight per day, but not more than 3 g per day.

Contraindicated for children under 3 years of age.

Special instructions

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

Since methyldopa is removed from the body by dialysis, an increase in blood pressure levels may occur after the session is completed.

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

Impact on the ability to drive vehicles and operate machinery

Drug interactions

Dopegit should not be used simultaneously with MAO inhibitors.

Concomitant use with the following medicinal products requires extreme caution.

Drugs that reduce the antihypertensive effect of Dopegit: sympathomimetics (increase the pressor effect), tricyclic antidepressants, phenothiazines (at the same time, they may have an additive antihypertensive effect), oral iron supplements (they can reduce the bioavailability of methyldopa), nonsteroidal anti-inflammatory drugs (NSAIDs) ), estrogen drugs.

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

Dopegit and the following drugs may alter the effects of each other: lithium (risk of increased lithium toxicity), levodopa (reduced antiparkinsonian effect and increased undesirable effects on the central nervous system), ethanol (alcohol) and other drugs that depress the central nervous system (increased depression), anticoagulants (increased anticoagulant effect, risk of bleeding), bromocriptine (possibly undesirable effect on prolactin concentration), haloperidol (possible cognitive impairment - disorientation and confusion).

Analogues of the drug Dopegit

Structural analogues of the active substance:

Aldomet;
Dopanol.

If there are no analogues of the drug for the active substance, you can follow the links below to the diseases for which the corresponding drug helps, and look at the available analogues for the therapeutic effect.