Moxonitex

Active ingredients: 

moxonidine 400 mcg; 

Excipients:

lactose monohydrate,

povidone K25,

crospovidone,

magnesium stearate.

Film casing composition :

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

Moxonitex is a selective agonist of imidazoline receptors. Responsible for reflex control over the sympathetic nervous system (receptors are located in the ventral-lateral part of the medulla oblongata). Slightly associated with central α ₂ -adrenergic receptors, reduces systolic and diastolic blood pressure with a single and long-term administration.

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

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

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

The duration of action is more than 12 hours.

PHARMACOKINETICS 

Suction

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

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

Distribution

Plasma protein binding is 7%. V _d  - 1.4-3 l / kg. Penetrates the BBB. Does not cumulate with prolonged use.

Withdrawal

T _1/2  - 2-3 hours. Excreted by the kidneys - 90% (50-75% - unchanged, 20% - in the form of metabolites).

Pharmacokinetics in special clinical situations

Moxonidine is excreted in small quantities during hemodialysis. There were no significant differences in pharmacokinetics in young and elderly patients.

In patients with moderate renal insufficiency (CC 30-60 ml / min) and severe (CC less than 30 ml / min) C _ss  in blood plasma and the final T _{1/2 are}  approximately 2 and 3 times (respectively) higher, than in hypertensive patients with normal renal function (CC more than 90 ml / min). Therefore, patients with moderate renal insufficiency should be prescribed the drug with caution and the dose should be selected individually.

Arterial hypertension.

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

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

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

From the side of the central nervous system: often - dizziness, headache, drowsiness, increased fatigue, sleep disturbance; 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 sense organ: sometimes - dry eyes, causing itching or burning.

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

Others: sometimes - gynecomastia, soreness of the parotid glands.

When moxonidine is co-administered with other antihypertensive drugs, the action is mutually reinforced.
Beta-blockers increase bradycardia, the severity of negative ino- and dromotropic action.
Moxonidine enhances the hypotensive effect of ethanol, sedatives, blockers of slow calcium channels (dihydropyridine derivatives).
Moxonidine should not be used concomitantly with tricyclic antidepressants.
Tolazoline dose-dependently reduces the hypotensive effect of moxonidine.

Inside, regardless of food intake, drinking plenty of fluids. The dose regimen is selected individually.

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

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

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 due to the introduction of fluid. Antagonists of α-adrenergic receptors can reduce or eliminate transient arterial hypertension in case of overdose with moxonidine.

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

If it is necessary to cancel the simultaneously taken beta-blockers and Moxonitex, beta-blockers are the first to cancel, and only a few days later - Moxonitex. Stop taking the drug Moxonitex gradually.

Influence on the ability to drive vehicles and use mechanisms

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