Moxonitex pills 400mcg, 14pcs

Composition

Active ingredients:  

moxonidine 400 mcg;

Auxiliary substances:

lactose monohydrate,

povidone K 25,

crospovidone,

magnesium stearate.

Composition of the film shell:

opadray Y 1 7000 (titanium dioxide, hypromellose, macrogol 400), iron oxide red dye.

Pharmacological action

Moxonitex is a selective imidazoline receptor agonist. It is responsible for reflex control of the sympathetic nervous system (receptors are localized in the venter-lateral part of the medulla oblongata). Slightly binds to central_α2-adrenergic receptors, reduces systolic and diastolic blood pressure with a single and prolonged intake.

With prolonged use, it reduces left ventricular myocardial hypertrophy, eliminates signs of myocardial fibrosis and microarteriopathy, normalizes capillary blood supply to the myocardium, reduces OPSS, pulmonary vascular resistance, while cardiac output and heart rate do not change significantly.

During treatment, the activity of norepinephrine and epinephrine, renin, angiotensin II at rest and during exercise, atrial natriuretic peptide (during exercise) and plasma aldosterone decreases.

Reduces tissue resistance to insulin by 21% compared to placebo in obese patients and insulin-resistant patients with moderate arterial hypertension, stimulates the release of growth hormone. It does not affect the metabolism of glucose and lipids.

Duration of action – more than 12 hours

. PHARMACOKINETICS

Suction

After oral use, the absorption is 90%. Food intake does not affect the amount of absorption. With a single oral dose, the bioavailability is 88%. _Cmax in blood plasma is determined 30-180 minutes after oral use and is 1-3 ng / ml.

The interval between the achievement of_cmax and a marked decrease in blood pressure at rest differs by an average of 10%, with exercise-by 7.7%.

Distribution

Binding to plasma proteins is-7%. Vd – 1.4-3 l / kg. Penetrates through the BBB. Does not accumulate with prolonged use.

Elimination

T_1/2-2-3 hours. Excreted by the kidneys-90% (50-75% – unchanged,20% – in the form of metabolites).

Pharmacokinetics in special clinical cases

Moxonidine is excreted in small amounts during hemodialysis. No significant differences in pharmacokinetics were found in young and elderly patients.

In patients with renal failure of moderate severity (CC 30-60 ml/min) and severe (CC less than 30 ml/min) C_ss in the blood plasma and the final T_1/2 approximately 2 and 3 times (respectively) higher than in hypertensive patients with normal renal function (QC more than 90 ml/min). Therefore, in patients with moderate renal insufficiency, the drug should be prescribed with caution and its dose should be selected individually.

Indications

Arterial hypertension.

Contraindications

• a history of angioedema;
• SSSU or sinoatrial block;
• AV-block II and III degree,
• severe bradycardia (less than 50 beats/min at rest);
• severe heart rhythm disorders;
• congestive heart failure (III-IV functional class NYHA classification);
• unstable angina;
• severe hepatic impairment;
• renal failure severe (CC less than 30 ml/min, serum creatinine more than 160 µmol/l);
• the age of 18;
• lactation;
• galactose intolerance, lactase deficiency or malabsorption syndrome glucose-galactose;
• hypersensitivity to moxonidine or any other component of the drug.

With caution and under the supervision of a doctor, the drug should be used in patients after a recent myocardial infarction or with peripheral circulatory disorders (intermittent claudication, Raynaud’s syndrome); in patients with moderate renal impairment (creatinine clearance 30-60 ml/min; serum creatinine content 105-160 mmol/l), with impaired liver function, pregnancy, depression, glaucoma, epilepsy, Parkinson’s disease.

Side effects

From the cardiovascular system:  rarely-symptoms of vasodilation; sometimes-a marked decrease in blood pressure, syncopal states, Raynaud’s syndrome, peripheral edema.

From the central nervous system:  often – dizziness, headache, drowsiness, fatigue, sleep disorders; sometimes-paresthesia, depression, anxiety.

From the digestive system:  often – dryness of the oral mucosa, nausea, anorexia, constipation.

From the genitourinary system:  sometimes-urinary retention or incontinence, impotence and / or decreased libido.

From the side of the sensory organ:  sometimes-dry eyes that cause itching or burning sensation.

Allergic reactions:  sometimes – urticaria, pruritus, exanthema, angioedema.

Other services:  sometimes-gynecomastia, parotid gland soreness.

Interaction

When moxonidine is co-administered with other antihypertensive agents, the effect is mutually enhanced. Beta-blockers increase bradycardia, the severity of negative ino-and dromotropic effects. Moxonidine enhances the hypotensive effect of ethanol, sedatives, slow calcium channel blockers (dihydropyridine derivatives). Do not use moxonidine concomitantly with tricyclic antidepressants. TOlasoline dose-dependently reduces the hypotensive effect of moxonidine.

How to take, course of use and dosage

Inside, regardless of food intake, with a sufficient amount of liquid. The dosage regimen is selected individually.

In the absence of other prescriptions, Moxonitex should be prescribed in the following doses: as an initial dose,0.2 mg of the drug is prescribed in the morning. If the therapeutic effect is insufficient, the dose is increased after 3 weeks to 0.4 mg per day once or in 2 doses. The maximum daily dose is 0.6 mg; the maximum single dose is 0.4 mg.

In patients with moderate renal impairment (creatinine clearance 30-60 ml / min), a single dose should not exceed 0.2 mg, and the maximum daily dose should be 0.4 mg.

Overdose

Symptoms:  headache, marked decrease in blood pressure, bradycardia, palpitations, weakness, drowsiness, dryness of the oral mucosa; rarely-vomiting and epigastric pain. Paradoxical arterial hypertension and hyperglycemia are potentially possible.

Treatment:  symptomatic. There is no specific antidote. With a pronounced decrease in blood pressure, it is recommended to restore the BCC by introducing fluid. Alpha-adrenergic antagonists can reduce or eliminate transient arterial hypertension in case of overdose with moxonidine.

Special instructions

During treatment, regular monitoring of blood pressure, heart rate and ECG is required.

If it is necessary to cancel the simultaneous use of beta-blockers and Moxonitex, the beta-blockers are first canceled and only a few days later – Moxonitex. Stop taking Moxonitex gradually.

Influence on the ability to drive motor vehicles and manage mechanisms

The effect of Moxonitex on the ability to drive vehicles or operate machinery has not been studied. Taking into account the possible occurrence of dizziness and drowsiness, patients should exercise caution when engaging in potentially dangerous activities, such as driving vehicles or operating equipment that require increased concentration of attention.

Form of production

Tablets

Storage conditions

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

Indications

Hypertension