Physiotens pills 0.2mg, 14pcs

Composition

1 coated tablet contains: Active ingredients: moxonidine 0.2 mg; Excipients: lactose monohydrate — of 95.8 mg;povidone — 0.7 mg;crospovidone — 3 mg;magnesium stearate — 0.3 mg;hypromellose 1.3 mg;ethyl cellulose — 4 mg;macrogol 6000 — 0.25 mg;talc — 0,9975 mg;iron oxide red (E 172) — 0,0025 mg;titanium dioxide (E 171) — 1.25 mg.

Pharmacological action of

Selectively interacting with imidazoline I₁-receptors located in the brain stem, reduces sympathetic activity.

Moxonidine has a high affinity for imidazoline I1-receptors and only slightly binds to central alpha_-2-adrenergic receptors due to interaction with which dry mouth and sedation are explained.

Reduces the resistance of tissues to insulin.

Effect on hemodynamics: a decrease in systolic and diastolic blood pressure with a single and prolonged use of moxonidine is associated with a decrease in the pressor effect of the sympathetic system on peripheral vessels, a decrease in peripheral vascular resistance, while cardiac output and heart rate do not change significantly.

Pharmacokinetics

Suction

Absorption — 90%. _Cmax in blood plasma (after taking a tablet containing 0.2 mg of moxonidine) is 1.4-3 ng / ml and is reached in 60 minutes. Bioavailability-88% (food intake does not affect the pharmacokinetics).

Distribution

The volume of distribution is 1.4-3 l / kg. Penetrates through the BBB. Binding to plasma proteins — 7.2%.

Metabolism

Main metabolites: 4,5-dihydromoxonidine and guanidine derivatives.

Elimination

of T_1/2 moxonidine and its metabolites is 2.5 and 5 hours, respectively. Within 24 hours, more than 90% of moxonidine is excreted by the kidneys, approximately 78% unchanged and 13% as a dehydrogenated derivative. Less than 1% is excreted in the faeces. Does not accumulate with prolonged use.

Pharmacokinetics in the elderly

There are age-related changes in pharmacokinetics, probably associated with slightly higher bioavailability and / or reduced metabolic activity. However, these changes are not clinically significant.

Pharmacokinetics in patients with renal insufficiency

Moxonidine clearance is strongly correlated with creatinine clearance. In patients with moderate renal insufficiency (creatinine clearance in the range of 30-60 ml/min), steady-state plasma concentrations and final T_1/2 are approximately 2 and 1.5 times higher than in patients with arterial hypertension with normal renal function (creatinine clearance >90 ml/min). In patients with severe renal insufficiency (creatinine clearance) is 3 times higher than in those with normal renal function.

use of multiple doses of the drug does not lead to accumulation in the body of patients with moderate renal insufficiency. In late stages, patients with extremely severe renal insufficiency (creatinine clearance) are 6 and 4 times higher, respectively, than in patients with normal renal function. In patients with impaired renal function, the dosage should be selected individually. Moxonidine is slightly eliminated during hemodialysis.

Indications

Arterial hypertension.

Use during pregnancy and lactation

Pregnancy: There are no clinical data on the use of Fiziotenz® in pregnant women. In the course of animal studies, the embryotoxic effect of the drug was established. Fiziotenz® should be prescribed to pregnant women only after careful assessment of the risk-benefit ratio, when the benefit to the mother exceeds the potential risk to the fetus.

Breast-feeding period: moxonidine is excreted in breast milk and should therefore not be administered during breast-feeding. If it is necessary to use the drug Fiziotenz® during lactation, breastfeeding should be discontinued.

Contraindications

• hypersensitivity to the Active ingredient and other components of the drug;
• a history of angioedema;
• the syndrome of weakness of the sinus node or sinoatrial block;
• severe hepatic impairment;
• severe bradycardia (heart rate (HR) of rest of less than 50 beats/min);
• atrioventricular block II and III degree
• acute and chronic heart failure;
• breastfeeding;
• hereditary galactose intolerance, lactase deficiency or malabsorption of glucose-galactose;
• the age of 18 (due to the lack of data on safety and efficacy.

Side effects

From the central nervous system: dizziness, headache, drowsiness, sleep disturbance.

From the cardiovascular system: excessive decrease in blood pressure, orthostatic hypotension.

From the gastrointestinal tract: dry mouth, nausea.

Skin and subcutaneous fat disorders: skin rash, pruritus, angioedema.

Common: asthenia.

These symptoms usually gradually decrease during the first weeks of treatment.

Interaction

It can be co-administered with thiazide diuretics, ACE inhibitors and slow calcium channel blockers. There is a mutual strengthening of the action when combined with these and other antihypertensive agents.

There is no pharmacokinetic interaction with hydrochlorothiazide (possible co-use), glibenclamide( glyburide), digoxin. Tricyclic antidepressants may reduce the effectiveness of centrally acting antihypertensive drugs (co-use is not recommended). Moderately enhances cognitive decline in patients taking lorazepam. Increases the sedative effect of benzodiazepines. There is no pharmacodynamic interaction when co-administered with moclobemide.

How to take, course of use and dosage

Inside, regardless of food intake, the initial dose (in most cases) — 0.2 mg per day; the maximum daily dose is 0.6 mg (divided into 2 doses); the maximum single dose is 0.4 mg;

in renal insufficiency (creatinine clearance 30-60 ml / min) and in patients on hemodialysis, a single dose is 0.2 mg, the maximum daily dose is 0.4 mg.

Overdose

Several cases of non-fatal overdose have been reported with simultaneous doses of up to 19.6 mg. There is no specific antidote.

Description

Film-coated tablets of pale pink color, round, biconvex, with the inscription “0,2” on one side; on the break – white color.

Special instructions

In post-marketing follow-up, cases of atrioventricular block of varying severity were recorded in patients taking moxonidine. An association between Fiziotenz and atrioventricular conduction retardation cannot be completely excluded. Therefore, caution is recommended when treating patients with a possible predisposition to the development of atrioventricular block.

If it is necessary to cancel the simultaneous use of beta-blockers and Fiziotenz®, first cancel beta-blockers and only after a few days Fiziotenz®.

Currently, there is no evidence that discontinuation of Fiziotenz® leads to an increase in blood pressure. However, it is not recommended to stop taking Fiziotenz® abruptly, instead gradually reduce the dose of the drug over two weeks

Form of production

Film-coated tablets

Storage conditions

Store in a dark place, at a temperature not exceeding 25°C.

Shelf life

2 years

Active ingredient

Moxonidine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Description

For adults as prescribed by a doctor, for pregnant women as prescribed by a doctor

Indications

Hypertension