Moxonitex, 0.4 mg 14 pcs

Moxonitex is a selective imidazoline receptor agonist. It is responsible for reflex control of the sympathetic nervous system (receptors are localized in the ventero-lateral part of the medulla oblongata). Slightly binds to central α₂-adrenoreceptors, reduces systolic and diastolic BP with single and prolonged use.

Long-term use decreases myocardial hypertrophy of the left ventricle, levels the signs of myocardial fibrosis microarteriopathy, normalizes myocardial capillary blood supply, decreases PPS, pulmonary vascular resistance, while cardiac output and HR do not change significantly.

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

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

The duration of action is more than 12 hours.

Pharmacokinetics

Intake

After oral administration the absorption is 90%. The absorption is not influenced by food intake. With a single oral administration the bioavailability is 88%. C_max in plasma is determined 30-180 min after oral administration and is 1-3 ng/ml.

The interval between reaching C_max and a marked decrease in BP at rest differs on average by 10%, at load by 7.7%.

Distribution

The binding to plasma proteins is – 7%. V_d – 1.4-3 l/kg. It penetrates through the barrier membrane. It does not cumulate with prolonged use.

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

Pharmacokinetics in special clinical cases

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

In patients with moderate renal impairment (CK 30-60 ml/min) and severe renal impairment (CK less than 30 ml/min), plasma C_ss and terminal T_1/2 is approximately 2 and 3 times (respectively) higher than in patients with arterial hypertension with normal renal function (CK greater than 90 mL/min). Therefore, in patients with moderate renal insufficiency, the drug should be prescribed with caution and its dose should be adjusted individually.

Indications

Arterial hypertension.

Active ingredient

Composition

Active substances:

moxonidine 400 mcg;

Associates:

Lactose monohydrate,

povidone K25,

crosspovidone,

Magnesium stearate.

Composition of the film coating:

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

How to take, the dosage

Overly, regardless of meals, with plenty of fluid. The dosage regimen is adjusted individually.

In the absence of other prescriptions, Moxonitex should be prescribed in the following doses: 0.2 mg of the drug in the morning as an initial dose. If the therapeutic effect is insufficient, the dose is increased after 3 weeks to 0.4 mg daily 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 function impairment (creatinine Cl 30-60 ml/min), the single dose should not exceed 0.2 mg and the maximum daily dose 0.4 mg.

Interaction

When co-administration of moxonidine with other hypotensive agents there is a mutual enhancement of action.
Beta-adrenoblockers increase bradycardia, the severity of negative and drootropic action.
Moxonidine increases hypotensive effect of ethanol, sedatives, slow calcium channel blockers (dihydropyridine derivatives).
Moxonidine should not be used simultaneously with tricyclic antidepressants.
Tolazoline dose-dependently reduces hypotensive effect of moxonidine.

Special Instructions

Regular monitoring of BP, HR and ECG is required during treatment.

If it is necessary to withdraw beta-adrenoblockers and Moxonitex taken simultaneously, the beta-adrenoblockers should be withdrawn first and Moxonitex only after a few days. Moxonitex should be stopped gradually.

The effect of Moxonitex on driving and operating machinery has not been studied. As dizziness and drowsiness may occur, patients should be cautious when engaged in potentially dangerous activities such as driving or operating machinery requiring increased concentration.

Contraindications

Side effects

Cardiovascular system disorders: rare – symptoms of vasodilation; sometimes – marked BP decrease, syncopal states, Raynaud’s syndrome, peripheral edema.

CNS disorders: frequently – dizziness, headache, somnolence, fatigue, sleep disturbance; sometimes – paraesthesia, depression, anxiety.

Digestive system disorders: often – dry mouth, nausea, anorexia, constipation.

Urogenital system disorders: sometimes – urinary retention or incontinence, impotence and/or decreased libido.

Senses: sometimes – dry eyes, causing itching or burning sensation.

Allergic reactions: sometimes – hives, skin itching, exanthema, angioedema.

Others: sometimes – gynecomastia, painful parotid glands.

Overdose

Symptoms: headache, marked BP decrease, bradycardia, palpitations, weakness, drowsiness, dry mouth; rarely, vomiting and epigastric pain. Paradoxical arterial hypertension and hyperglycemia are potentially possible.

Treatment: symptomatic. There is no specific antidote. In marked BP decrease it is recommended to restore the blood pressure by fluid administration. α-adrenoreceptor antagonists can reduce or eliminate transient arterial hypertension in moxonidine overdose.

Similarities