Composition, form of production and packaging
The tablets covered with a film cover of light pink color, round.
1 tab.
moxonidine 200 Ојg
[PRING] lactose monohydrate - 94.5 mg, povidone (K25) - 2 mg, crospovidone - 3 mg, magnesium stearate - 0.3 mg.
The composition of the shell: opadray Y-1-7000 (titanium dioxide - 1.093 mg, hypromellose - 2.186 mg, macrogol 400 - 0.219 mg) - 3.498 mg, iron-oxide red oxide - 0.002 mg.
14 pcs. - blisters (1) - packs of cardboard.
14 pcs. - blisters (2) - packs of cardboard.
14 pcs. - blisters (3) - packs of cardboard.
The tablets covered with a film cover of dark pink color, round.
1 tab.
moxonidine 400 Ојg
[PRING] lactose monohydrate - 94.3 mg, povidone (K25) - 2 mg, crospovidone - 3 mg, magnesium stearate - 0.3 mg.
The composition of the shell: opadray Y-1-7000 (titanium dioxide - 1.083 mg, hypromellose - 2.165 mg, macrogol 400 - 0.217 mg) - 3.465 mg, iron oxide red oxide - 0.035 mg.
14 pcs. - blisters (1) - packs of cardboard.
14 pcs. - blisters (2) - packs of cardboard.
14 pcs. - blisters (3) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2017.
PHARMACHOLOGIC EFFECT
Selective agonist imidazoline receptors responsible for the reflex regulation of the sympathetic nervous system (localized in the ventro-lateral region of the medulla oblongata). Has a low affinity for the central? 2- adrenoreceptors, due to interaction with which the sedative effect and dryness of the mucous membrane of the oral cavity are mediated.
Moxonidine increases the insulin sensitivity index by 21% compared with placebo in patients with obesity, insulin resistance with a moderate degree of hypertension.
Influence on hemodynamics: a decrease in systolic and diastolic blood pressure with a single and prolonged administration of moxonidine is associated with a decrease in the pressor effect of the sympathetic nervous system on peripheral vessels, a decrease in OPSS, while cardiac output and heart rate do not change significantly.
PHARMACOKINETICS
Suction and distribution
After oral administration, moxonidine rapidly and almost completely absorbed from the upper gastrointestinal tract. Tmax is approximately 1 hour. Absolute bioavailability is approximately 88%. To an insignificant degree is exposed to a metabolism at "the first passage" through a liver. Eating does not affect the pharmacokinetics of the drug.
Binding to plasma proteins is 7.2%. Moxonidine penetrates the BBB.
Metabolism
The main metabolite is deoxidized moxonidine, whose pharmacodynamic activity is about 1/10 of the activity of moxonidine.
Excretion
T 1/2 of moxonidine and metabolites is 2.5 and 5 hours, respectively. Within 24 hours, more than 90% of moxonidine is excreted by the kidneys: approximately 78% in unchanged form, and 13% in the form of dehydrated moxonidine. Other metabolites in the urine account for approximately 8% of the dose. Less than 1% of the dose is excreted through the intestine.
Pharmacokinetics in specific patient groups
The excretion of moxonidine largely correlates with QC. In patients with moderate renal insufficiency (CK 30-60 ml / min), C ss in the blood plasma and final T 1/2 areapproximately 2 and 1.5 times higher than in patients with arterial hypertension with normal renal function (KC more than 90 ml / min.). In patients with severe renal insufficiency (CC less than 30 ml / min), C ss in plasma and final T 1/2 are 3 times higher than in patients with normal renal function. The use of moxonidine in multiple doses does not lead to cumulation in the body of patients with moderate and severe renal insufficiency. In patients with terminal renal failure (CC less than 10 ml / min) on hemodialysis, C ss in the blood plasma and final T 1/2 are respectively 6 and 4 times higher than in patients with normal renal function. In patients with impaired renal function, the dose should be selected individually. Moxonidine is slightly excreted in hemodialysis.
INDICATIONS
- arterial hypertension.
DOSING MODE
The drug is administered orally, regardless of food intake. Tablets should be washed down with a sufficient amount of liquid.
In most cases, the initial dose of Tenzotran is 200 Ојg / day in 1 dose, preferably in the morning hours. If the therapeutic effect is inadequate, the dose can be increased after 3 weeks of therapy to 400 mcg / day in 2 divided doses (morning and evening) or in 1 morning (in the morning). The maximum daily dose, which should be divided into 2 divided doses (morning and evening), is 600 mcg. The maximum single dose is 400 Ојg.
In elderly patients with normal renal function, the recommendations for the dosing regimen are the same as for adult patients.
In patients with renal insufficiency (QC 30-60 ml / min) and patients on hemodialysis , a single dose should not exceed 200 mcg. The maximum daily dose is 400 mcg.
SIDE EFFECT
The most frequent adverse reactions, especially at the beginning of therapy, were dry mouth, headache, asthenia and drowsiness. The intensity of their manifestation and frequency decrease upon repeated admission.
The incidence of adverse reactions is determined as follows: very often (> 1/10), often (> 1/100, <1/10), sometimes (> 1/1000 and <1/100), very rarely (<1/1000 , including individual messages).
From the side of the central nervous system: often - increased fatigue, drowsiness, headache, dizziness; sometimes - insomnia, asthenia.
From the cardiovascular system: often - vasodilation; sometimes - excessive reduction of blood pressure, orthostatic hypotension, paresthesia, Raynaud's syndrome, peripheral microcirculation disorders.
From the digestive tract: very often - dryness of the mucous membrane of the oral cavity; often - nausea, constipation and other abnormalities of the gastrointestinal function; very rarely - hepatitis, cholestasis.
From the genitourinary system: sometimes - urine retention or incontinence, impotence, decreased libido.
Allergic reactions: sometimes - skin manifestations, angioedema.
From the side of the eye: sometimes - dry eyes, causing itching or burning sensation.
Other: sometimes - edema of different localization, weakness in the legs, fainting, fluid retention, anorexia, pain in the parotid glands, gynecomastia.
CONTRAINDICATIONS
- SSSU;
- Sinoatrial blockade;
- AV blockade II and III degree;
- pronounced bradycardia (heart rate less than 50 beats per minute);
- chronic cardiac insufficiency III and IV of the functional class according to NYHA classification;
- unstable angina;
- angioedema in history;
- marked hepatic insufficiency (more than 9 points on the Child-Pugh scale);
- chronic renal failure (CC <30 ml / min, serum creatinine content> 160 Ојmol / l);
- age under 18 years (effectiveness and safety not established);
- lactation period;
- Galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome;
- Hypersensitivity to moxonidine and other components of the drug.
With caution should be used in Parkinson's disease (severe form), epilepsy, glaucoma, depression, intermittent claudication, Raynaud's disease, AV blockade of I degree, chronic renal failure (CK> 30 ml / min, but <60 ml / min), expressed cerebrovascular disorders, after myocardial infarction, chronic cardiac insufficiency of I and II functional class, violations of liver function, hemodialysis, during pregnancy.
PREGNANCY AND LACTATION
There are no clinical data on the negative effect on the course of pregnancy. However, it should be prescribed to pregnant women only if the intended benefit to the mother exceeds the potential risk to the fetus.
Moxonidine is excreted in breast milk. During the period of treatment it is recommended to stop breastfeeding or to cancel the drug.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated use in chronic renal failure (CC <30 ml / min, serum creatinine content> 160 Ојmol / l).
Caution should be used for chronic renal failure (CK> 30 ml / min, but <60 ml / min).
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated use in severe hepatic insufficiency (more than 9 points on the scale Child-Pugh).
With caution should apply the drug for violations of liver function.
APPLICATION FOR CHILDREN
Contraindicated in children and adolescents under 18 years of age (efficiency and safety not established).
APPLICATION IN ELDERLY PATIENTS
In elderly patients with normal renal function, the recommendations for the dosing regimen are the same as for adult patients.
SPECIAL INSTRUCTIONS
If it is necessary to cancel simultaneously taken beta-blockers and Tenzotran, first abolish beta-blockers and only after a few days - Tenzotran.
Stop taking Tenzotrana should be gradual.
It is not recommended to prescribe tricyclic antidepressants simultaneously with Tenzotran.
During treatment, regular monitoring of blood pressure, heart rate and ECG is necessary.
Moxonidine can be prescribed with thiazide diuretics, ACE inhibitors and slow calcium channel blockers.
Patients with a rare hereditary pathology of galactose intolerance, lactase deficiency, or glucose-galactose malabsorption syndrome should not take Tenzotran.
Impact on the ability to drive vehicles and manage mechanisms
Data on the adverse effects of moxonidine on the ability to drive vehicles and to manage mechanisms are absent. There are reports of the development of drowsiness and dizziness during treatment with moxonidine. This should be taken into account when prescribing the drug to patients who engage in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
OVERDOSE
There are reports of several cases of overdose without a lethal outcome, when doses up to 19.6 mg per dose were applied.
Symptoms: headache, sedation, drowsiness, marked decrease in blood pressure, dizziness, asthenia, bradycardia, dry mouth, vomiting and stomach pain, increased fatigue. Potential short-term increases in blood pressure, tachycardia, hyperglycemia are possible.
Treatment: there is no specific antidote. Gastric lavage, intake of activated carbon and laxatives, symptomatic therapy. In the case of a marked decrease in blood pressure, it is recommended to introduce a fluid for the recovery of bcc and the introduction of dopamine. Bradycardia can be stopped with atropine. Antagonists? -adrenoceptors are able to reduce or eliminate transient hypertension in case of an overdose of moxonidine.
DRUG INTERACTION
Moxonidine can be administered with thiazide diuretics, slow calcium channel blockers, and other antihypertensive agents. The combined use of moxonidine with these and other antihypertensive agents leads to an additive effect and an increase in the hypotensive effect.
When moxonidine is administered with hydrochlorothiazide, glibenclamide (glyburide), or digoxin, there is no pharmacokinetic interaction.
Tricyclic antidepressants can reduce the effectiveness of antihypertensive agents of central action, therefore it is not recommended to prescribe tricyclic antidepressants concomitantly with moxonidine.
Moxonidine moderately increases the reduced cognitive ability in patients taking lorazepam.
The administration of moxonidine together with benzodiazepines may be accompanied by an increase in the sedative effect of the latter.
Moxonidine is able to potentiate the effect of ethanol when used together.
When moxonidine is administered together with moclobemide, pharmacodynamic interaction is absent.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TENO-RU-00003-DOC-PHARM
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children at a temperature of no higher than 30 В° C. Shelf life for tablets 200 Ојg - 2 years; for tablets 400 mcg - 3 years.
