Dopegit

Dopegyt (methyldopa) is a medicine used to treat high blood pressure (hypertension). It belongs to a class of drugs called antihypertensives, which help lower blood pressure.

Methyldopa works by converting to dopamine in the body. Dopamine, in turn, is a neurotransmitter that is involved in the regulation of blood pressure. It acts on receptors in the brain, which leads to a decrease in sympathetic activity and, as a result, to a decrease in vascular resistance and blood pressure.

It is important to remember that Dopegit (methyldopa) should only be used as prescribed by a doctor, as each patient may have their own optimal dosage and reaction to the drug. Like other medications, Dopegit has its own side effects, including drowsiness, dizziness, gastrointestinal disturbances, changes in the blood, and others. Therefore, it is important to discuss any symptoms or questions with your doctor.

Indications Dopegita

1. Hypertension (high blood pressure): This is the main indication for Dopegyt. It is used to lower blood pressure in patients with hypertension.
2. Preeclampsia and eclampsia during pregnancy: Methyldopa may be used to control blood pressure in pregnant women with preeclampsia (high blood pressure during pregnancy) or eclampsia (a serious complication of preeclampsia characterized by seizures and coma).
3. Pheochromocytoma: This is a rare tumor that can cause high blood pressure. Methyldopa can be used to lower blood pressure in patients with pheochromocytoma.
4. Migraine: Methyldopa may sometimes be used to prevent migraines in patients for whom other medications are ineffective or unsuitable.

Release form

Methyldopa, known under the trade name Dopegit, is most often available in tablet form. Tablets can have different dosages of the active substance, for example, 250 mg or 500 mg.

Pharmacodynamics

Methyldopa works by converting it into alpha-methylnorepinephrine in neurons of the brain's intermediate zone. This agent, in turn, is converted into norepinephrine and epinephrine, neurotransmitters that control blood pressure and heart rate.

The pharmacodynamic action of Dopegit is as follows:

1. Lowering Blood Pressure: The mechanism of lowering blood pressure is due to the fact that alpha-methylnorepinephrine, formed from methyldopa, acts as an alpha-adrenergic receptor antagonist. This leads to vasodilation and a decrease in peripheral resistance, which in turn lowers blood pressure.
2. Central action: Methyldopa also has an effect on the central nervous system, decreasing sympathetic activity, which also helps to lower blood pressure.
3. Decreased catecholamine formation: Methyldopa inhibits the conversion of tyrosine to dopa and hence the formation of norepinephrine and epinephrine.
4. Prevention of hypertensive crisis: Due to its long-acting and blood pressure stabilizing properties, methyldopa can also be used to prevent hypertensive crisis.

Pharmacokinetics

1. Absorption: Methyldopa is generally well absorbed from the gastrointestinal tract after oral administration.
2. Metabolism: After absorption, methyldopa undergoes metabolism in the liver. It is primarily metabolized to alpha-methylnorepinephrine, which is the active metabolite. This metabolite is largely responsible for the antihypertensive effect of methyldopa.
3. Elimination: Methyldopa and its metabolites are excreted primarily via the kidneys. Elimination occurs both unchanged and as metabolites.
4. Half-life: The half-life of methyldopa varies from patient to patient, but is typically around 1-2 hours. However, the drug's effects may last longer due to its metabolites.
5. Protein binding: Methyldopa is extensively bound to plasma proteins, meaning that only a small fraction of the drug remains in free form and is available for tissue distribution.
6. Influencing factors: The pharmacokinetics of methyldopa may be altered in patients with impaired liver or kidney function. It is also important to consider possible interactions with other drugs that may affect its metabolism or elimination.

Dosing and administration

Directions for use:

1. Oral use: Methyldopa is usually taken orally in tablet form.
2. Intravenous administration: If necessary, such as in severe hypertension, methyldopa can be administered intravenously.

Dosage:

• Initial Dose: The usual starting dose is 250 mg two or three times daily. The effectiveness and tolerability of the dose should be assessed by a physician.
• Maintenance dose: The maintenance dose may range from 500 mg to 2 g per day, divided into several doses.
• Maximum Dose: The maximum daily dose should not exceed 3 g.

Status control:

• It is important to regularly monitor the patient's blood pressure to assess the effectiveness of treatment and possible dose adjustments.
• During treatment with methyldopa, periodic blood tests, including liver function tests, should be performed, especially at the beginning of therapy.

Features of application:

• Methyldopa may cause drowsiness or dizziness, so it is important to assess the patient's ability to drive vehicles and operate machinery.
• Patients should avoid abruptly discontinuing the drug, as this may result in a sharp increase in blood pressure.

Use Dopegita during pregnancy

Methyldopa (Dopegyt) is generally considered safe for use during pregnancy and is widely used to treat hypertension in pregnant women. Here are the key points from the research:

1. Safety and Efficacy: Methyldopa is considered a safe and effective option for the treatment of hypertension during pregnancy. It not only controls blood pressure but also reduces the risk of serious complications such as preeclampsia. The results of the study show that methyldopa does not increase the risk of having babies with birth defects or spontaneous abortions and may improve perinatal outcomes when hypertension is adequately controlled (Hoeltzenbein et al., 2017).
2. Risk of hepatotoxicity: Despite the widespread use of methyldopa, there are reports of hepatotoxicity associated with its use. In rare cases, methyldopa can cause acute hepatitis, which requires careful monitoring of liver function during treatment. If liver toxicity develops, methyldopa treatment should be discontinued immediately (Slim et al., 2010).

Before starting treatment with methyldopa or any other medication during pregnancy, it is important to talk to your doctor to help you evaluate all the potential risks and benefits of therapy.

Contraindications

1. Allergic reaction: People with a known allergy to methyldopa or any other component of the drug should avoid using it.
2. Liver problems: Patients with severe liver dysfunction or liver failure should use methyldopa with caution because it may affect liver function.
3. Kidney problems: People with severe kidney problems or kidney failure should also use methyldopa with caution because it may affect kidney function.
4. Depression: Methyldopa may increase symptoms of depression, so its use is not recommended in patients with depression without consulting a doctor.
5. Drug interactions: There are multiple drug interactions with methyldopa, so patients taking other medications should discuss this with their doctor to avoid unwanted effects.
6. Heart and blood vessel problems: Methyldopa may affect heart function and circulation, so its use requires caution in patients with cardiovascular disease.

Side effects Dopegita

1. General symptoms:

   • Drowsiness or fatigue
   • Headache
   • Dizziness, especially when standing up from a sitting or lying position (orthostatic hypotension)

2. Digestive system:

   • Dry mouth
   • Nausea or vomiting
   • Constipation or diarrhea
   • Possible liver dysfunction, which may manifest as jaundice

3. Hematopoietic system:

   • Anemia
   • Leukopenia (decrease in the number of white blood cells)
   • Thrombocytopenia (decreased platelet count)

4. Nervous system:

   • Paresthesia (burning or tingling sensation)
   • Cramps
   • Depressive states

5. Immune system:

   • Allergic reactions including fever, rash, angioedema

6. Cardiovascular system:

   • Rapid heartbeat
   • Edema

7. Other rare but serious effects:

   • Parkinsonism or extrapyramidal disorders (less common)
   • Hyperprolactinemia (elevated prolactin levels), which can lead to gynecomastia in men or galactorrhea in women

Overdose

1. A severe drop in blood pressure: This may manifest itself as dizziness, fainting, weakness, and a feeling of depression.
2. Bradycardia: A decrease in heart rate, which can lead to decreased blood flow and hypoxia.
3. Drowsiness and sleep: This may be related to the central actions of methyldopa.
4. Bradypnea: Decreased breathing rate.
5. Unconsciousness: In severe cases of overdose, unconsciousness and coma may occur.

Interactions with other drugs

1. Monoamine oxidase inhibitors (MAOIs): The interaction of methyldopa with MAOIs may result in an increase in its hypotensive effect, which may cause a severe drop in blood pressure.
2. Alpha-blockers: The combination of methyldopa with alpha-blockers may enhance the hypotensive effect, which may result in blood pressure that is too low.
3. Tricyclic antidepressants (TCAs): Methyldopa may enhance the cardiotoxic effects of TCAs such as cardiac arrhythmias.
4. MAO inhibitors: The use of methyldopa with MAO inhibitors may enhance the hypotensive effect and cause acute hypotension.
5. Drugs that increase sympathetic nervous system activity: Drugs such as epinephrine or norepinephrine may reduce the hypotensive effect of methyldopa.
6. Sympathetic nervous system depressants: The use of methyldopa with drugs such as beta-blockers or central antihypertensive agents may enhance the hypotensive effect and increase the risk of hypotension.