Moksarel Tab n / a film about 0.4mg 30 pc

Description

Composition
Active substance:
1 tablet contains: moxonidine – 0.2 mg; 0.3 mg or 0.4 mg.
Excipients:
Lactose monohydrate, microcrystalline cellulose, colloidal silica, povidone K-30, sodium croscarmellose, magnesium stearate.
Film coating: [hypromellose, talc, titanium dioxide, macrogol 4000 (polyethylene glycol 4000), yellow iron oxide (iron oxide)] or [the dry mixture to a film coating containing hypromellose (60%), talcum (20%), titanium dioxide ( 10.33%), macrogol 4000 (polyethylene glycol 4000) (9%), yellow iron oxide (ferric oxide) (0.67%)] or [the dry film coating mixture comprising hypromellose (60%), talc (20% ), titanium dioxide (11%), macrogol 4000 (polyethylene glycol 4000) (9%)].
Description:
Round biconvex tablets, film-coated white or nearly white (dosage 0.2 mg), pink (dosage 0.3 mg) or yellow (dosage 0.4 mg).
The cross-sectional core of a white or nearly white.
Product form:
Tablets, film-coated, 0.2 mg, 0.3 mg or 0.4 mg. 10, 14, 15 or 30 tablets in blisters of PVC film and aluminum foil. 1, 2 or 3 blisters with 10 tablets 1, 2 or 4 blisters 14 tablets 1, 2 or 4 blisters 15 tablets, 1 or 2 blisters of 30 tablets together with instructions for use in the stack of cardboard.
Contraindications
Hypersensitivity to the active substance, other components of the formulation; The expressed disturbances of heart rhythm; sick sinus syndrome; atrioventricular block II and III degree; bradycardia (heart rate (HR) of less than 50 beats / min); acute and chronic heart failure (III-IV NYHA functional class classifying); simultaneous application of tricyclic antidepressants (see “Interaction with other drugs.”); severe renal impairment (creatinine clearance less than 30 mL / min), including patients on hemodialysis; age over 75 years; age 18 years (effectiveness and safety have not been established moxonidine); breastfeeding; lactose intolerance, lactase deficiency, glucose-galactose malabsorption.
Precautions renal dysfunction (creatinine clearance of more than 30 ml / min); severe liver failure (more than 9 points on the Child-Pugh classification); I degree atrioventricular block; severe coronary artery disease; severe coronary heart disease or unstable angina (application experience is insufficient); chronic heart failure.
Dosage
0.4 mg
Indications
Arterial hypertension.
Interaction with other drugs
The combined use of Moxonidine with other antihypertensives leads to additive effect.
Tricyclic antidepressants may reduce the effectiveness of centrally acting antihypertensive agents, and therefore is not suitable for taking them together with moxonidine.
Moxonidine may exacerbate the effects of tricyclic antidepressants, tranquilizers, ethanol, sedatives and hypnotics.
Moxonidine is able to moderately improve cognitive impairment in patients receiving lorazepam.
Moxonidine in conjunction with benzodiazepines may be accompanied by increased sedative effect of the latter.
Concomitant use of moxonidine with beta-blockers leads to increased bradycardia, severity of foreign-and dromotropic action.
In conjunction with moxonidine moclobemide pharmacodynamic interaction is absent.
Moxonidine by tubular secretion is released, so it is possible its interaction with other drugs, was isolated by tubular secretion.
Overdose
symptoms
Headache, sedation, drowsiness, and marked reduction in blood pressure, dizziness, fatigue, asthenia, bradycardia, dryness of the oral mucosa, vomiting, epigastric pain, respiratory depression, disturbance of consciousness. Potentially also possible transient increase in blood pressure, tachycardia, hyperglycemia.
Treatment
There is no specific antidote. In case of significant decrease in blood pressure is recommended for the introduction of liquid recovery circulating blood volume and dopamine. Bradycardia atropine may be cropped. Alpha-adrenergic antagonists may reduce or eliminate paradoxical hypertensive effects in overdose moxonidine.
In severe cases of overdose it is recommended to carefully monitor the human consciousness and to prevent respiratory depression.
Moxonidine slightly displayed during hemodialysis.
pharmachologic effect
Pharmacological group:
Centrally acting antihypertensive agent.
Pharmacodynamics:
Moxonidine is a antihypertensive agent with a central mechanism of action. The structures of the brain stem (rostral layer lateral ventricles) moxonidine selectively stimulates imidazolin-sensitive receptors involved in tonic reflex and regulation of the sympathetic nervous system. Stimulation of imidazoline receptors reduces peripheral sympathetic activity and blood pressure (BP).
Moxonidine differs from other sympatholytic antihypertensives lower affinity to the alpha 1-adrenoceptors, which explains the lower probability of sedation and dryness of the mucous membrane of the oral cavity.
Receiving moxonidine leads to a reduction in systemic vascular resistance and BP.
Moxonidine improves insulin sensitivity index in patients with obesity, insulin resistance, and moderate hypertension.
Pharmacokinetics:
Suction
After oral administration moxonidine is rapidly and almost completely absorbed in the upper gastrointestinal tract. The absolute bioavailability is about 88%. Time to maximum concentration-about 1 hour. Food intake has no effect on the pharmacokinetics of the drug.
Distribution
Communication plasma protein is 7.2%.
Metabolism
The main metabolit- dehydrogenated moxonidine. Pharmacodynamic Activity dehydrogenated moxonidine-about 10% compared with moxonidine.
breeding
The half-life (T1 / 2) of moxonidine and metabolite of 2.5 and 5 hours, respectively. Within 24 hours over 90% moxonidine excreted by the kidneys (approximately 78% unchanged and 13% as a degidromoksonidina, other metabolites in urine do not exceed 8% of the dose). Less than 1% of the dose is excreted through the intestines.
Pharmacokinetics in elderly patients
It is noted clinically insignificant change in pharmacokinetic parameters moxonidine in elderly patients, probably due to decrease in the intensity of its metabolism and / or somewhat higher bioavailability.
Pharmacokinetics in children
Moxonidine is not recommended for use in patients younger than 18 years, and therefore in this group pharmacokinetic studies have not been conducted.
Pharmacokinetics in renal failure
Excretion Moxonidine largely correlates with creatinine clearance (CC). In patients with moderate renal impairment (creatinine clearance in the range of 30-60 ml / min) the equilibrium concentration in the blood plasma and the end of T1 / 2 of approximately 2 and 1.5 times higher than those with normal renal function of patients (creatinine clearance greater than 90 mL / min).
In patients with severe renal failure (creatinine clearance less than 30 mL / min) the equilibrium concentration in the blood plasma and the final T1 / 2 to 3 times higher than in patients with normal renal function. Assigning multiple doses of moxonidine leads to a predictable accumulation in the body of patients with moderate and severe renal insufficiency. Patients with end-stage renal failure (creatinine clearance less than 10 mL / min) on hemodialysis, the equilibrium concentration in the blood and the end of T1 / 2, respectively, in the plasma 4 and 6 times higher than in patients with normal renal function.
In all groups, the maximum concentration of moxonidine in plasma is higher in 1,5-2 times. In patients with renal function impairment, the dosage should be individualized.
Moxonidine slightly displayed during hemodialysis.
Pregnancy and breast-feeding
Clinical data on the treatment of pregnant drug Moksarel® absent.
Appoint Moksarel® pregnant with caution only after careful evaluation of the risk-benefit ratio when the benefit to the mother outweighs the potential risk to the fetus.
Moxonidine passes into breast milk. Lactating women during the period of treatment is recommended to stop breast-feeding or stop the drug.
Conditions of supply of pharmacies
Prescription.
side effects
The frequency of side effects listed below, was determined according to the following: very frequency not less than 10%; often – at least 1% but less than 10%; infrequently, not less than 0.1% but less than 1%; rarely, not less than 0.01% but less than 0.1%; rarely -less 0.01% (including sporadic cases).
Central nervous system: often -Head pain, dizziness (vertigo), somnolence; -obmorok infrequently.
Cardio-vascular system: Infrequent -vyrazhennoe decrease in blood pressure, orthostatic hypotension, bradycardia.
From the gastrointestinal tract: very often -suhost oral mucosa; -toshnota often, diarrhea, vomiting, dyspepsia.
Skin and subcutaneous tissue disorders: often -kozhnaya rash, itching; infrequently-angioedema.
Mental disorders: often, insomnia; infrequently-nervousness.
On the part of the ear and labyrinth disorders: rarely, ringing in the ears.
On the part of the musculoskeletal and connective tissue disorders: often, back pain; infrequently, the pain in the neck.
General disorders and the site of injection: often, asthenia; infrequently-peripheral edema.
special instructions
There is currently no evidence that discontinuation Moksarel® leads to increased blood pressure. However, do not stop taking the drug abruptly Moksarel® instead should gradually reduce the dose of the drug for two weeks.
If necessary, cancel the concomitant beta-blockers and drug Moksarel® first override beta-blockers, and only after a few days moxonidine.
During treatment requires regular monitoring of blood pressure, heart rate and recording electrocardiography (ECG). Moksarel® stop taking the drug should be gradually.
During treatment Moksarel® should exclude alcohol.
Effects on ability to drive vehicles and mechanisms
Moksarel® influence of the drug on the ability to drive vehicles or operate machinery has not been studied. However, taking into account the possible occurrence of dizziness and drowsiness, patients should be careful during the occupation of potentially hazardous activities that require attention, such as driving a vehicle or control technique, which requires high concentration of attention.
Storage conditions
In the dark place at a temperature not higher than 25 C.
Keep out of the reach of children.
Dosing and Administration
Inside, regardless of the meal.
In most cases the initial dose Moksarel® drug is 0.2 mg per day. The maximum single dose is 0.4 mg. The maximum daily dose to be divided into 2 doses is 0.6 mg.
The starting dose for patients with moderate or severe renal insufficiency, and also for patients on hemodialysis was 0.2 mg / day. If necessary and if tolerated daily dose may be increased to 0.4 mg.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist