Physiotens tablets p / o 0.4mg, No. 28

Arterial hypertension.

It is taken internally. The initial dose is on average 200 mcg orally 1 time / day. The maximum single dose is 400 mcg. An individual correction of the daily dose is required depending on the tolerance of therapy. The maximum daily dose is 600 mcg in 2 divided doses.

For patients with moderate and severe renal insufficiency, as well as those on hemodialysis, the initial dose is 200 mcg / day. If necessary and with good tolerance, the daily dose can be increased to a maximum of 400 mcg.

White film-coated tablets , round, biconvex, without risks.

Active substance:

moxonidine

Severe bradycardia (less than 50 beats / min), SSSU, AV block II and III degree, acute and chronic heart failure, lactation (breastfeeding), children and adolescence up to 18 years, hypersensitivity to moxonidine.

pharmachologic effect

Antihypertensive agent. The mechanism of action of moxonidine is associated mainly with its effect on the central links of blood pressure regulation. Moxonidine is a predominantly imidazoline receptor agonist.

Exciting these receptors of the neurons of the solitary tract, moxonidine through the system of inhibitory interneurons helps to suppress the activity of the vasomotor center and thus to reduce the descending sympathetic influences on the cardiovascular system. BP (systolic and diastolic) decreases gradually. Moxonidine differs from other sympatholytic antihypertensive drugs in its lower affinity for ?2-adrenergic receptors, which explains the lower likelihood of developing a sedative effect and dry mouth.

Moxonidine increases the insulin sensitivity index (compared with placebo) by 21% in obese patients with insulin resistance and moderate hypertension.

Pharmacokinetics

After oral administration, moxonidine is rapidly and almost completely absorbed in the upper gastrointestinal tract. The absolute bioavailability is approximately 88%. The time to reach Cmax is about 1 hour. Food intake does not affect the pharmacokinetics of moxonidine. Plasma protein binding is 7.2%. The main metabolite of moxonidine is dehydrated moxonidine and guanidine derivatives. The pharmacodynamic activity of dehydrated moxonidine is about 10% compared to moxonidine.

T1 / 2 of moxonidine and metabolite is 2.5 and 5 hours, respectively. Within 24 hours, more than 90% of moxonidine is excreted by the kidneys (about 78% unchanged and 13% in the form of dehydriromoxonidine, other metabolites in urine do not exceed 8% of the dose taken). Less than 1% of the dose is excreted through the intestines.

Compared to healthy volunteers, patients with arterial hypertension did not show changes in the pharmacokinetics of moxonidine.

There were clinically insignificant changes in the pharmacokinetic parameters of moxonidine in elderly patients, probably due to a decrease in the intensity of its metabolism and / or a slightly higher bioavailability.

Excretion of moxonidine is largely correlated with CC. In patients with moderate renal insufficiency (CC 30-60 ml / min) Css in blood plasma and final T1 / 2 are approximately 2 and 1.5 times higher than in individuals with normal renal function (CC more than 90 ml / min). In patients with severe renal failure (CC less than 30 ml / min), Css in blood plasma and final T1 / 2 are 3 times higher than in patients with normal renal function. The use of moxonidine in multiple doses leads to predictable cumulation in the body in patients with moderate to severe renal failure. In patients with end-stage renal failure (CC less than 10 ml / min) on hemodialysis, Css in blood plasma and final T1 / 2, respectively, are 6 and 4 times higher than in patients with normal renal function.In all groups, Cmax of moxonidine in blood plasma is 1.5-2 times higher. In patients with impaired renal function, the dose should be selected individually. Moxonidine is excreted to a small extent during hemodialysis.

Indications of the active substances of the drug Moxonidin

Arterial hypertension.

Side effect

From the side of the central nervous system: often - headache, dizziness (vertigo), drowsiness; infrequently - fainting.

From the side of the cardiovascular system: infrequently - a marked decrease in blood pressure, orthostatic hypotension, bradycardia.

From the digestive system: very often - dry mouth; often - diarrhea, nausea, vomiting, dyspepsia.

On the part of the skin and subcutaneous tissues: often - skin rash, itching; infrequently - angioedema.

From the side of the psyche: often - insomnia; infrequently - nervousness.

On the part of the organ of hearing and labyrinthine disorders: infrequently - ringing in the ears.

From the musculoskeletal system: often - back pain; infrequently - neck pain.

From the side of the body as a whole: often - asthenia; infrequently - peripheral edema.

Contraindications for use

Severe bradycardia (less than 50 beats / min), SSSU, AV block II and III degree, acute and chronic heart failure, lactation (breastfeeding), children and adolescence up to 18 years, hypersensitivity to moxonidine.

Application during pregnancy and lactation

There have been no adequate and well-controlled studies of the safety of moxonidine during pregnancy, so it should not be used in this category of patients.

Should not be used during lactation, since moxonidine is excreted in breast milk. If it is necessary to use moxonidine during lactation, breastfeeding should be discontinued.

In the course of experimental studies on animals, the embryotoxic effect of the drug was established.

Application for violations of liver function

Contraindicated in severe liver dysfunctions.

Application for impaired renal function

Contraindicated in severe renal impairment.

Moxonidine is used with caution in patients with impaired renal function; in such cases, correction of the dosage regimen is required taking into account the CC values.

In the process of treating patients with impaired renal function, careful monitoring of their condition is required.

Application in children

Due to the lack of clinical experience, moxonidine should not be used in children and adolescents under the age of 16 years.

special instructions

Special care must be taken when using moxonidine in patients with grade I AV block (risk of bradycardia); severe coronary artery disease and unstable angina pectoris (experience of use is insufficient); renal failure.

If it is necessary to cancel simultaneously taken beta-blockers and moxonidine, first cancel beta-blockers and only after a few days - moxonidine.

Currently, there is no evidence that discontinuation of moxonidine leads to an increase in blood pressure. However, abrupt discontinuation of moxonidine is not recommended, the dose should be reduced gradually over 2 weeks.

Influence on the ability to drive vehicles and use mechanisms

During the period of treatment, patients should be careful if it is necessary to engage in potentially hazardous activities that require concentration of attention and high speed of psychomotor reactions.

Drug interactions

The combined use of moxonidine with other antihypertensive drugs leads to an additive effect.

Tricyclic antidepressants can reduce the effectiveness of centrally acting antihypertensive drugs, therefore, they are not recommended in conjunction with moxonidine.

Moxonidine can enhance the effect of tricyclic antidepressants, tranquilizers, ethanol, sedatives and hypnotics.

Moxonidine is able to moderately improve impaired cognitive function in patients receiving lorazepam.

Moxonidine can enhance the sedative effect of benzodiazepine derivatives when administered simultaneously.

Moxonidine is secreted by tubular secretion. Therefore, its interaction with other drugs released by tubular secretion is not excluded.