Dopegyt® [Methyldopa]

Brand Egis

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Clinical Pharmacology

Antihypertensive drug that affects the central mechanisms of regulation of blood pressure. Dopegyt penetrates through the BBB; metabolized with the formation of alpha-methylnoradrenaline, which has a hypotensive effect through several mechanisms:

decrease in sympathetic tone by stimulating central inhibitory presynaptic α2 receptors;
replacement of endogenous dopamine by dopaminergic nerve endings - as a false neurotransmitter;
reduction of plasma renin activity and OPS;
suppression of the enzyme dopa-decarboxylase, which leads to a decrease in the synthesis of norepinephrine, dopamine, serotonin and the concentration of norepinephrine and adrenaline in the tissues.

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Dosage and Administration

The drug Dopegyt requires individual dosing.
Dopegyt is prescribed for adults, orally, in the initial dosage of 250 mg in the evening (in the first two days). Over the next every two days, a single dose is increased by 250 mg until an optimal hypotensive effect is achieved (as a rule, it is noted when a daily dose of 1 g is reached, divided into 2-3 doses).
The first is recommended to increase the evening dose in order to reduce sedation.
The maximum daily dosage of the drug Dopegyt - 2 g. When combined therapy with other antihypertensive drugs, the maximum daily dose of Dopegyt®a should not exceed 500 mg.

The dose of the drug is gradually reduced after reaching a stable hypotensive effect to the level of the minimum effective dosage.
Patients with impaired renal function are advised to reduce a single dose of the drug. The initial daily dosage of Dopegyt®a for children is 10 mg / kg, divided into 2-4 doses. The maximum daily dosage of the drug Dopegyt for children should not exceed 65 mg / kg.
For elderly patients it is recommended to prescribe the initial dosage of the drug 125 mg once or twice a day. The maximum daily dose for elderly patients is 2 g, divided into 2 doses.

Adverse reactions

When using Dopegyt®a may appear:
- lethargy, drowsiness, lethargy, facial nerve paralysis, parkinsonism, paresthesia, spontaneous chorioathetoid movements, staggering when walking, dizziness, headache;
- orthostatic hypertension, peripheral edema, bradycardia, hyperemia of the upper half of the body, aggravation of the phenomena of heart failure, increased angina, in rare cases - pericarditis, myocarditis;
- glossalgia, dryness of the oral mucosa, vomiting, nausea, diarrhea, colitis, hepatotoxicity, pancreatitis, jaundice, increased activity of hepatic transaminases;
- leukopenia, hemolytic anemia, agranulocytosis, thrombocytopenia;
- arthralgia, myalgia;
- galactorrhea, gynecomastia, hyperprolactinemia;
- reduce libido, reduce potency, amenorrhea;
- fever, rash, rash, toxic epidermal necrolysis (Lyell syndrome);
- inflammation of the salivary glands, nasal congestion;
- positive direct Coombs test (when taking the drug for more than 6 months at a daily dosage> 1 g).

Contraindications

Dopegyt is contraindicated in patients with hemolytic anemia, hypersensitivity, acute hepatitis, renal failure, hepatic failure, hepatic cirrhosis, systemic connective tissue disorders, depression, parkinsonianism, pheochromocytoma, pronounced coronary atherosclerosis, acute myocardial infarction, in a pattern, pronounced coronary atherosclerosis, acute myocardial infarction, a syndrome, a pronounced coronary atherosclerosis, an acute myocardial infarction, a pattern, a pronounced coronary atherosclerosis, an acute myocardial infarction, a sympathetic heart disease and MAO inhibitors.
Caution should be exercised in the appointment of the drug Dopegyt during lactation and in patients with a history of hepatitis, diencephalic syndrome, acute left ventricular failure.

Drug interactions

The combination of the drug with MAO inhibitors can lead to increased side effects: hypotension or hypertensive crisis with psychomotor agitation.
The combination with tricyclic antidepressants can reduce the hypotensive effect of the drug and provoke the appearance of headaches, tachycardia, agitation.
Combined use with levodopa can lead to increased anti-Parkinsonian effect, which is caused by inhibition of peripheral decarboxylation of levodopa under the action of methyldopa and an increase in the concentration of levodopa in the central nervous system. In cases where inhibition of decarboxylation predominates in the central nervous system, a decrease in the anti-Parkinsonian effect of levodopa occurs.
The combination of Dopegyt®a with drugs that contain levodopa + carbidopa, can lead to the development of orthostatic hypotension. In such cases, patients are advised to be in a horizontal position for 1-2 hours after taking the drugs.

The combination of Dopegyt®a with haloperidol leads to an increased likelihood of developing dementia; a combination with digoxin in elderly patients may lead to an increased likelihood of developing SSS.
To increase the hypotensive effect of the drug, it is advisable to combine it with diuretics, hydralazine and nifedipine.
Simultaneous use of the drug with β-blockers may lead to the development of orthostatic hypotension.
Simultaneous administration with adrenergic agonists, indomethacin and other NSAIDs leads to a decrease in the severity of the hypotensive effect of the drug.
The combination of Dopegyt®a with anxiolytics (tranquilizers) enhances the hypotensive effect of the drug.
Alkalization of urine during the period of treatment with methyldopa leads to an increase in its action, acidification of urine to a decrease in action.
The drug should be stopped 7-10 days prior to general anesthesia in order to avoid the development of a collaptoid state. Medicines for general anesthesia (sodium thiopental or halothane) should be carefully prescribed to patients taking methyldopa. Use of diethyl ether is contraindicated.

Dopegyt increases the hepatotoxicity of oral contraceptives and lithium salts.
The drug is incompatible with reserpine.
Care should be taken when combining Dopegyt®a with quinidine, neuroleptics, acetazolamide and procainamide.

Pregnancy and Lactation

The results of clinical studies revealed no signs of damage to the newborn or fetus when using the drug in the second and third trimesters of pregnancy. However, it is recommended to prescribe the drug Dopegyt to pregnant women only under strict indications.

Overdosage

In case of an overdose of Dopegyt, the development of severe arterial hypotension, weakness, severe bradycardia, drowsiness, tremor, lethargy, dizziness, flatulence, constipation, diarrhea, vomiting, nausea, intestinal atony may occur.
Treatment of overdose: shortly after ingestion - flush the stomach and stimulate vomiting in order to reduce the amount of the drug absorbed. It is advisable to control the BCC, heart rate, electrolyte balance, the functions of the kidneys, intestines and brain. The introduction of sympathomimetics (epinephrine) is allowed if necessary.