Estulic® [Guanfacin]

Pharmacological properties

Antihypertensive drug of central action. its hypotensive effect is mainly due to stimulation of α2-adrenergic receptors in the brain stem, which leads to a decrease in central sympathetic impulse and, accordingly, to a decrease in heart rate and peripheral vascular resistance both at rest and during exercise.

The drug is rapidly and completely absorbed in the digestive tract. The maximum concentration of guanfacin in blood plasma is achieved 1-4 hours after ingestion. Binding to plasma proteins - up to 64%. The average elimination half-life is on average 17 hours (12–23 hours). Guanfacin metabolism occurs mainly in the liver. More than 80% of the dose taken is excreted in the urine, and about 30% is unchanged.

Indications

Ag, especially essential and renal.

Application

Usually, the initial dose is 0.5–1 mg once daily at bedtime. if necessary, the daily dose can be increased by 0.5–1 mg / day for a week until the desired effect is achieved - lowering hell. the maximum daily dose is 3 mg.

Contraindications

Hypersensitivity to guanfacin or other components of the drug; cerebrovascular disease; coronary insufficiency; recent myocardial infarction; chronic impaired liver function; history of depression; During pregnancy and breastfeeding; childhood.

Side effects

Drowsiness, dry mouth, dizziness, constipation, headache, nausea, vomiting, sleep disturbance, fatigue or weakness, conjunctivitis, decreased sexual function, confusion, depression are possible.

special instructions

Caution must be exercised in the treatment of patients with cardiovascular or coronary insufficiency, impaired cardiac conduction, with cerebrovascular disease, a history of stroke or myocardial infarction. Patients with impaired liver or kidney function, history of depression should be under the constant supervision of a doctor. elderly patients may be more sensitive to the hypotensive and sedative effect of guanfacin, therefore, such patients are prescribed the drug with caution.

The drug should be discontinued gradually, since with the sudden cessation of drug treatment, withdrawal syndrome is possible.

In patients with severe renal failure, the daily dose should be reduced.

The concentration of catecholamines in the urine and excretion of vanillyl mindic acid in the urine can be reduced, but with the sudden cancellation of Estulic they can increase.

During the entire course of treatment with Estulic, you should not drink alcoholic beverages.

Patients taking the drug should refrain from all potentially dangerous activities that require increased attention and speed of response due to possible drowsiness.

Interactions

Estulic should not be used in combination with blockers of α2-adrenergic receptors (phentolamine, yohimbine), since they reduce its effect.

With caution, the drug should be used in conjunction with sympathomimetics (reduce its effect); β-adrenoreceptor blockers (bradycardia may develop); antipsychotics (enhance Estulics sedative effect).

Some β-adrenoreceptor blockers (e.g. pindolol, okprenolol) can be safely used in combination with Estulic.

With simultaneous use with drugs that cause central nervous system depression, it is possible to increase central nervous system depression.

With simultaneous use with NSAIDs, the activity of guanfacin may be weakened.

When using Estulic in combination with other antihypertensive agents, the antihypertensive effect may be enhanced.

When using Estulic along with estrogens, blood pressure may increase due to fluid retention due to the action of estrogen.

Overdose

Symptoms: drowsiness, dizziness, arterial hypotension, bradycardia, arrhythmia, in severe cases - coma.

Treatment: symptomatic; gastric lavage, careful monitoring of the functions of the cardiovascular system should be ensured. If necessary, iv administration of isadrine. Dialysis is ineffective.

Storage conditions

At a temperature of 15–25 ° C.