Moxonidine Canon pills 0.4mg, 14pcs

Composition

Active ingredient:

moxonidine 0.4 mg.

Auxiliary substances:

microcrystalline cellulose,

aerosil A-380,

polyvinylpyrrolidone,

magnesium stearate,

hydroxypropylcellulose (klucel),

castor oil,

twin-80.

Pharmacological action

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

By stimulating these receptors of neurons in the solitary tract, moxonidine, through the system of inhibitory interneurons, helps to inhibit the activity of the vasomotor center and thus reduce the descending sympathetic effects on the cardiovascular system. Blood pressure (systolic and diastolic) decreases gradually. Moxonidine differs from other sympatholytic antihypertensive agents in its lower affinity for α2-adrenergic receptors, which explains the lower likelihood of sedation and dry mouth.

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

Pharmacokinetics

After oral use, moxonidine is rapidly and almost completely absorbed in the upper gastrointestinal tract. Absolute bioavailability is approximately 88%. The time to reach Cmax is about 1 h. Food intake does not affect the pharmacokinetics of moxonidine. Binding to plasma proteins is 7.2%. The main metabolite of moxonidine is dehydrogenated moxonidine and guanidine derivatives. The pharmacodynamic activity of dehydrogenated moxonidine is about 10% compared to moxonidine.

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

Compared with healthy volunteers, patients with arterial hypertension showed no changes in the pharmacokinetics of moxonidine.

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

Moxonidine elimination is strongly correlated with creatinine clearance. In patients with moderate renal insufficiency (creatinine clearance 30-60 ml/min), Css in blood plasma and final T1/2 are approximately 2 and 1.5 times higher than in those with normal renal function (creatinine clearance more than 90 ml/min). In patients with severe renal insufficiency (creatinine clearance 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 accumulation in the body in patients with moderate to severe renal insufficiency. In patients with end-stage renal insufficiency (creatinine clearance less than 10 ml/min) on hemodialysis, Css in blood plasma and final T1 / 2, respectively, is 6 and 4 times higher than in patients with normal renal function. In all groups, the 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 slightly eliminated during hemodialysis.

Indications

Arterial hypertension

Contraindications

Severe bradycardia (less than 50 beats / min), SSR, grade II and III AV block, acute and chronic heart failure, lactation (breastfeeding), children and adolescents under 18 years of age, hypersensitivity to moxonidine.

Side effects

Especially at the beginning of therapy, the most common side effects were: dry mouth, headache, dizziness, asthenia, peripheral edema, allergic reactions, nausea, constipation, drowsiness. Their intensity and frequency decrease with repeated use. Cases of anorexia, parotid gland pain, urinary retention or incontinence, dry eye, orthostatic hypotension, Raynaud’s syndrome, endocrine disorders, and gallstone disease have been reported.

Interaction

Moxonidine can be given with thiazide diuretics and slow calcium channel blockers. When moxonidine is co-administered with these and other antihypertensive agents, the effect of moxonidine is mutually enhanced. When moxonidine is administered with hydrochlorothiazide, glibenclamide (glyburide) or digoxin, there is no pharmacokinetic interaction.

Tricyclic antidepressants may reduce the effectiveness of centrally acting antihypertensive drugs.

Beta-blockers increase bradycardia, the severity of the negative ino-and dromotropic effects of moxonidine.

Moxinidine modestly enhances cognitive decline in patients taking lorazepam.

The use of moxonidine together with benzodiazepines may be accompanied by an increase in the sedative effect of the latter.

When moxonidine is co-administered with moclobemide, there is no pharmacodynamic interaction.

How to take, course of use and dosage

Inside, regardless of food intake, with a sufficient amount of liquid. In most cases, the initial dose of moxonidine is 0.2 mg per day, in one dose, preferably in the morning. If the therapeutic effect is insufficient, the dose can be increased after 3 weeks of therapy to 0.4 mg per day in 2 doses or once. The maximum daily dose, which should be divided into 2 doses (morning and evening), is 0.6 mg. The maximum single dose is 0.4 mg.

In elderly patients with normal renal function, the dosage recommendations are the same as for adult patients.

In patients with renal insufficiency (cretinin clearance 30-60 ml per minute) and patients undergoing hemodialysis, a single dose should not exceed 0.2 mg, the maximum daily dose is 0.4 mg.

Overdose

Symptoms:  headache, sedation, drowsiness, excessive decrease in blood pressure, dizziness, general weakness, bradycardia, dry mouth, vomiting, fatigue, stomach pain. A short-term increase in blood pressure, tachycardia, and hyperglycemia are also potentially possible.

Treatment:  symptomatic. Gastric lavage (immediately after use), use of activated charcoal and laxatives, symptomatic therapy. In the case of a decrease in blood pressure, it is recommended to restore the volume of circulating blood by introducing fluid. Bradycardia can be treated with atropine. Alpha-adrenergic antagonists may reduce or eliminate transient hypertension in the case of moxonidine overdose. As a specific antidote, idazoxan (an imidazoline antagonist) is administered.

Special instructions

If it is necessary to cancel simultaneously taking beta-blockers and moxonidine, first cancel beta-blockers and, only after a few days, moxonidine. It is not recommended to prescribe tricyclic antidepressants simultaneously with moxonidine. During treatment, alcohol consumption is excluded. During treatment, regular monitoring of blood pressure, heart rate and ECG is necessary.

Moxonidine can be given with thiazide diuretics, ACE inhibitors, and slow calcium channel blockers. Stop taking moxonidine gradually.

Shelf life

2 years

Active ingredient

Moxonidine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Description

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

Indications

Hypertension