Registration number
LP-002321
Dosage form
film-coated tablets
Compound
1 film-coated tablet contains:
dosage 0.2 mg g: active substance
: moxonidine 0.2 mg
excipients (core)
: croscarmellose sodium (primellose) - 3.0 mg; lactose monohydrate (lactopress) (milk sugar) -; 95.3 mg; colloidal silicon dioxide (aerosil) -; 0.5 mg; sodium stearyl fumarate -; 1.0 mg;
excipients (shell):
Opadry II (polyvinyl alcohol, partially hydrolyzed -; 1.32 mg; titanium dioxide E 171 -; 0.6027 mg; talc -; 0.6 mg; macrogol (polyethylene glycol 3350) -; 0.3705 mg; soy lecithin E 322 -; 0.105 mg; dye iron oxide (II) yellow -; 0.0003 mg; dye iron oxide (II) red -; 0.0015 mg).
dosage 0.3 mg: active substance
: moxonidine 0.3 mg
excipients (core)
: croscarmellose sodium (primellose);
3.0 mg; lactose monohydrate (lactopress) (milk sugar) -; 95.2 mg; colloidal silicon dioxide (aerosil) -; 0.5 mg; sodium stearyl fumarate; 1.0 mg;
excipients (shell):
Opadry II (polyvinyl alcohol, partially hydrolyzed -; 1.32 mg; titanium dioxide E 171 -; 0.6003 mg; talc -; 0.6 mg; macrogol (polyethylene glycol 3350) -; 0.3705 mg; soy lecithin E 322 -; 0.105 mg; aluminum varnish based on crimson dye [Ponceau 4R] -; 0.0039 mg; aluminum varnish based on sunset yellow dye 0.0003 mg).
dosage 0.4 mg g: active substance
: moxonidine 0.4 mg
excipients (core)
: croscarmellose sodium (primellose) -;
3.0 mg;
lactose monohydrate (lactopress) (milk sugar) -; 95.1 mg; colloidal silicon dioxide (aerosil) -; 0.5 mg; sodium stearyl fumarate -; 1.0 mg; excipients (shell):
Opadry II (polyvinyl alcohol, partially hydrolyzed -; 1.32 mg; titanium dioxide E 171 -; 0.5751 mg; talc -; 0.6 mg; macrogol (polyethylene glycol 3350) -; 0.3705 mg; soy lecithin E 322 -; 0.105 mg; aluminum varnish based on indigo carmine -; 0.0018 mg; aluminum varnish based on azorubine dye -; 0.0153 mg; aluminum varnish based on crimson dye [Ponceau 4R] -; 0. 0123 mg).
Description
Light pink, film-coated tablets, round, biconvex. Tablets with a break are white or almost white in color (dosage 0.2 mg). Tablets, film-coated, pink, round, biconvex. Tablets with a break are white or almost white (dosage 0.3 mg). Tablets, film-coated, dark pink, round, biconvex. Tablets with a break are white or almost white (dosage 0.4 mg).
ATX code
[C02AC05]
Pharmacological properties
Pharmacodynamics
Moxonidine is an antihypertensive drug with a central mechanism of action. In the brainstem structures (rostral layer of the lateral ventricles), moxonidine selectively stimulates imidazoline-sensitive receptors that take part in the tonic and reflex regulation of the sympathetic nervous system. Stimulation of imidazoline receptors reduces peripheral sympathetic activity and blood pressure (BP).
Moxonidine differs from other sympatholytic antihypertensive drugs in its lower affinity for α2-adrenergic receptors, which explains the lower likelihood of developing sedation and dry mouth.
Taking moxonidine leads to a decrease in systemic vascular resistance and blood pressure. Moxonidine improves the insulin sensitivity index by 21% (compared to placebo) in patients with obesity, insulin resistance and moderate hypertension.
Pharmacokinetics
Van suctions:
After oral administration, moxonidine is rapidly and almost completely absorbed into the
upper parts of the gastrointestinal tract. Absolute bioavailability is approximately 88%. Time to reach maximum concentration -; about 1 hour. Food intake does not affect the pharmacokinetics of the drug.
Distribution
The connection with blood plasma proteins is 7.2%.
Metabol Meas.
The main metabolite is; dehydrogenated moxonidine. Pharmacodynamic activity of dehydrogenated moxonidine -; about 10% compared to moxonidine.
Output
The half-life (T1/2) of moxonidine and metabolite is 2.5 and 5 hours, respectively. Within 24 hours, over 90% of moxonidine is excreted by the kidneys (about 78
% unchanged and 13% in the form of dehydri-romoxonidine, other metabolites in the urine do not exceed 8% of the dose taken). Less than 1% of the dose is excreted through the intestines.
Pharmacokinetics in patients with arterial hypertension:
Compared with healthy volunteers, patients with arterial hypertension show no changes in the pharmacokinetics of moxonidine.
Farmak okin etika in old age
Clinically insignificant changes in the pharmacokinetic parameters of moxonidine were noted in elderly patients, probably due to a decrease in the intensity of its metabolism and/or slightly higher bioavailability.
Farmak okinetics in children
Moxonidine is not recommended for use in patients under 18 years of age, and therefore pharmacokinetic studies have not been conducted in this group.
Pharmacokinetics for renal failure
Moxonidine excretion is significantly correlated with creatinine clearance (CC). In patients with moderate renal failure (creatinine clearance in the range of 30-60 ml/min), steady-state plasma concentrations and final T1/2 are approximately 2 and l.5 times higher than in patients with normal renal function (creatinine clearance more than 90 ml/min). min.).
In patients with severe renal failure (creatinine clearance less than 30 ml/min.), steady-state plasma concentrations and final T1/2 are 3 times higher than in patients with normal renal function. The administration of multiple doses of moxonidine leads to predictable accumulation in the body of patients with moderate and severe renal failure. In patients with end-stage renal failure (creatinine clearance less than 10 ml/min) on hemodialysis, steady-state plasma concentrations and final T1/2 are 6 and 4 times higher, respectively, than in patients with normal renal function. In all groups, the maximum concentration of moxonidine in blood plasma was 1.5 - 2 times higher. U
For patients with impaired renal function, the dosage should be adjusted individually. Moxonidine is excreted to a small extent during hemodialysis.
Indications for use
Arterial hypertension.
Contraindications
- hypersensitivity to the active substance and other components of the drug;
— sick sinus syndrome;
— severe bradycardia (resting heart rate less than 50 beats/min);
— atrioventricular block II and III degrees;
- severe heart rhythm disturbances;
— acute and chronic heart failure (III-IV functional class according to the NYHA classification);
- simultaneous use with tricyclic antidepressants (see section
“Interaction with other drugs”);
- severe renal failure (creatinine clearance less than 30 ml/min);
- hemodialysis;
- lactation period;
- hereditary lactose intolerance, lactase deficiency or glucose-galactose malabsorption;
— age over 75 years;
- age under 18 years (due to the lack of data on safety and effectiveness).
Particular caution should be exercised when using moxonidine in patients with
atrioventricular block of the first degree (risk of developing bradycardia); severe coronary artery disease, severe coronary heart disease or unstable angina (insufficient experience), chronic heart failure, severe liver failure, with impaired renal function (creatinine clearance more than 30 ml/min).
Pregnancy
There are no clinical data on the use of Moxonidine in pregnant women.
In animal studies, the embryotoxic effect of the drug was established. Moxonidine should be prescribed to pregnant women only after a careful assessment of the risk-benefit ratio, when the benefit to the mother outweighs the potential risk to the fetus.
Lactation period
Moxonidine passes into breast milk and should therefore not be given during breastfeeding. If it is necessary to use Moxonidine during lactation, breastfeeding should be stopped.
Directions for use and doses
Inside, regardless of food intake. In most cases, the initial dose of the drug
Moxonidine is 0.2 mg per day. The maximum single dose is 0.4 mg. The maximum daily dose, which should be divided into 2 doses, is 0.6 mg. Individual adjustment of the daily dose is necessary depending on the patient’s tolerance to the therapy. No dose adjustment is required for patients with hepatic impairment. The starting dose for patients with moderate or severe renal impairment is 0.2 mg/day. If necessary and if well tolerated, the daily dose can be increased to a maximum of 0.4 mg.
Side effect
The frequency of side effects listed below was determined accordingly
the following: very often (>1/10); often (>1/100, <1/10); uncommon (>1/1000, <1/100); including individual messages.
From the central nervous system:
Common: headache*, dizziness (vertigo), drowsiness. Uncommon: fainting*.
From the cardiovascular system:
Uncommon: marked decrease in blood pressure, orthostatic hypotension*, bradycardia.
From the gastrointestinal tract:
Very common: dry mouth. Common: diarrhea, nausea, vomiting, dyspepsia.
From the skin and subcutaneous tissues: Often: skin rash, itching.
Uncommon: angioedema.
Mental disorders:
Common: insomnia. Uncommon: nervousness.
Hearing and labyrinthine disorders: Uncommon: ringing in the ears.
Musculoskeletal and connective tissue disorders: Common: back pain.
Uncommon: neck pain.
General disorders and disorders at the injection site:
Often: asthenia.
Uncommon: peripheral edema.
(* - frequency comparable to placebo).
Overdose
There have been several reports of non-fatal overdoses when
Doses up to 19.6 mg were used simultaneously.
Symptoms:
headache, sedation, marked decrease in blood pressure, dizziness, asthenia, bradycardia, dry oral mucosa, vomiting, fatigue, pain in the epigastric region, respiratory depression and impaired consciousness. In addition, short-term increases in blood pressure, tachycardia and hyperglycemia are also possible, as shown in several high-dose animal studies.
Treatment
There is no specific antidote. In the case of a pronounced decrease in blood pressure, it may be necessary to restore the volume of circulating blood by introducing fluid and dopamine (injection).
Bradycardia can be stopped with atropine (injection).
In severe cases of overdose, it is recommended to carefully monitor disturbances of consciousness and avoid respiratory depression.
Alpha-adrenergic antagonists may reduce or eliminate the paradoxical hypertensive effects of moxonidine overdose.
Moxonidine is excreted to a small extent during hemodialysis.
Interaction with other drugs
The combined use of moxonidine with other antihypertensive drugs leads to an additive effect. Tricyclic antidepressants may reduce the effectiveness of centrally acting antihypertensive drugs, and therefore their use together with moxonidine is not recommended.
Moxonidine may enhance the effect of tricyclic antidepressants, tranquilizers, ethanol, sedatives and hypnotics.
Moxonidine may moderately improve impaired cognitive function in patients receiving lorazepam.
Moxonidine may enhance the sedative effect of benzodiazepine derivatives when administered simultaneously.
Moxonidine is released by tubular secretion. Therefore, its interaction with other drugs released by tubular secretion is not excluded. Beta-blockers increase bradycardia and the severity of negative ino- and dromotropic effects.
special instructions
If it is necessary to cancel beta-blockers and the drug Moxonidine taken simultaneously, first cancel the beta-blockers and only after a few days Moxonidine.
There is currently no evidence that stopping Moxonidine leads to an increase in blood pressure. However, it is not recommended to stop taking Moxonidine suddenly; instead, you should gradually reduce the dose of the drug over two weeks.
Avoid drinking alcohol during treatment.
During treatment, regular monitoring of heart rate and electrocardiography is necessary.
Impact on the ability to drive vehicles and operate machinery
The effect of Moxonidine on the ability to drive vehicles or operate machinery has not been studied. However, taking into account the possibility of dizziness and drowsiness, patients should be careful when engaging in potentially hazardous activities that require increased attention, such as driving a vehicle or operating equipment that requires increased concentration.
Release form
Film-coated tablets, 0.2 mg, 0.3 mg and 0.4 mg
10, 14 or 30 tablets per blister pack.
60 tablets in polymer jars or polymer bottles.
Each jar, bottle, 3 blister packs of 10 tablets, 1 or 2 blister packs of 14 tablets each, or 1 or 2 blister packs of 30 tablets, together with instructions for use, are placed in a cardboard box.
Best before date
3 years. Do not use after the expiration date stated on the packaging.
Storage conditions
In a dry place, protected from light, at a temperature not exceeding 25 C.
Keep out of the reach of children.
Vacation conditions
On prescription
Moxonidine-SZ 0.4 mg, 30 film-coated tablets
Registration Certificate Holder
NORTH STAR (Russia)
Dosage form
Medicine - Moxonidine-SZ
Description
Film-coated tablets
dark pink, round, biconvex; at the break - white or almost white.
1 tab.
moxonidine 0.4 mg
Excipients
: croscarmellose sodium (primellose) - 3 mg, lactose monohydrate (lactopress) (milk sugar) - 95.1 mg, colloidal silicon dioxide (Aerosil) - 0.5 mg, sodium stearyl fumarate - 1 mg.
Shell composition:
Opadry II (polyvinyl alcohol, partially hydrolyzed - 1.32 mg, titanium dioxide (E171) - 0.5751 mg, talc - 0.6 mg, macrogol (polyethylene glycol 3350) - 0.3705 mg, soy lecithin (E322) - 0.105 mg, indigo carmine-based aluminum varnish - 0.0018 mg, aluminum varnish based on azorubine dye - 0.0153 mg, aluminum varnish based on crimson dye [Ponceau 4R] - 0.0123 mg).
10 pieces. — cellular contour packages (3) — cardboard packs. 14 pcs. — cellular contour packages (1) — cardboard packs. 14 pcs. — contour cell packaging (2) — cardboard packs. 30 pcs. — cellular contour packages (1) — cardboard packs. 30 pcs. — contour cell packaging (2) — cardboard packs. 30 pcs. — cellular contour packages (3) — cardboard packs. 30 pcs. — contour cell packaging (4) — cardboard packs. 60 pcs. — polymer jars (1) — cardboard packs. 60 pcs. — polymer bottles (1) — cardboard packs.
Indications
- arterial hypertension.
Contraindications for use
- history of angioedema;
- severe liver failure;
- SSSU;
- sinoatrial block;
- severe bradycardia (resting heart rate less than 50 beats/min);
- AV block II and III degrees;
- acute and chronic heart failure;
- breastfeeding period;
- age under 18 years (due to lack of data on safety and effectiveness);
- hereditary lactose intolerance, lactase deficiency or glucose-galactose malabsorption;
- hypersensitivity to the active substance and other components of the drug.
Carefully:
1st degree AV block (risk of developing bradycardia); diseases of the coronary arteries (including ischemic heart disease, unstable angina, early post-infarction period); peripheral circulatory diseases (including intermittent claudication, Raynaud's syndrome); epilepsy; Parkinson's disease; depression; glaucoma; moderate renal failure (creatinine clearance 30-60 ml/min, serum creatinine 105-160 µmol/l); liver failure; pregnancy.
pharmachologic effect
Antihypertensive drug with a central mechanism of action. In the brain stem structures (rostral layer of the lateral ventricles), moxonidine selectively stimulates imidazoline-sensitive receptors that take part in the tonic and reflex regulation of the sympathetic nervous system. Stimulation of imidazoline receptors reduces peripheral sympathetic activity and blood pressure.
Moxonidine differs from other sympatholytic antihypertensive drugs in its lower affinity for α2-adrenergic receptors, which explains the lower likelihood of developing sedation and dry mouth. The use of moxonidine leads to a decrease in peripheral vascular resistance and blood pressure.
Moxonidine improves the insulin sensitivity index by 21% (compared to placebo) in patients with obesity, insulin resistance and moderate hypertension.
Drug interactions
The combined use of moxonidine with other antihypertensive drugs leads to an additive effect.
Tricyclic antidepressants may reduce the effectiveness of centrally acting antihypertensive drugs, and therefore their simultaneous use with moxonidine is not recommended.
Moxonidine may enhance the effect of tricyclic antidepressants, tranquilizers, ethanol, sedatives and hypnotics. Moxonidine may moderately improve impaired cognitive function in patients receiving lorazepam.
Moxonidine may enhance the sedative effect of benzodiazepine derivatives when used simultaneously.
Moxonidine is released by tubular secretion, so its interaction with other drugs released by tubular secretion is possible.
Dosage regimen
The drug is taken orally, regardless of food intake.
In most cases, the initial dose of Moxonidine-SZ is 0.2 mg/day. The maximum single dose is 0.4 mg. The maximum daily dose, which should be divided into 2 doses, is 0.6 mg. Individual adjustment of the daily dose is necessary depending on the patient’s tolerance to the therapy.
Dose adjustment for patients with liver failure
not required.
The starting dose for patients on hemodialysis
is 0.2 mg/day. If necessary and if well tolerated, the daily dose can be increased to a maximum of 0.4 mg.
Patients with renal failure
Careful dose selection is recommended, especially at the beginning of treatment.
The initial dose should be 0.2 mg/day. If necessary and if well tolerated, the daily dose of the drug can be increased to a maximum of 0.4 mg for patients with moderate renal failure (CR more than 30 ml/min, but less than 60 ml/min)
and 0.3 mg for
patients with severe renal failure (CR less than 30 ml/min)
.
Overdose
There have been reports of several cases of non-fatal overdose when doses up to 19.6 mg were used simultaneously.
Symptoms:
headache, sedation, drowsiness, excessive decrease in blood pressure, dizziness, asthenia, bradycardia, dry mouth, vomiting, fatigue, epigastric pain, respiratory depression and impaired consciousness. In addition, short-term increases in blood pressure, tachycardia and hyperglycemia are also possible, as has been shown in several studies examining the use of the drug in high doses in animals.
Treatment:
there is no specific antidote. In case of an excessive decrease in blood pressure, it may be necessary to restore bcc through the administration of fluid and dopamine (injection). Bradycardia can be stopped with atropine (injection). In severe cases of overdose, it is recommended to carefully monitor disturbances of consciousness and avoid respiratory depression. α-Adrenergic antagonists may reduce or eliminate the paradoxical hypertensive effects of moxonidine overdose.
Side effect
The most common side effects in patients taking moxonidine are dry mouth, dizziness, asthenia and drowsiness. These symptoms often improve after the first weeks of therapy.
The following side effects were observed in patients who participated in placebo-controlled clinical trials of moxonidine. The frequency of side effects was determined according to the following: very often (>1/10); often (>1/100, <1/10); uncommon (>1/1000, <1/100), including isolated reports.
From the nervous system:
often - headache*, dizziness (vertigo), drowsiness, insomnia; infrequently - fainting*, increased excitability.
Hearing and labyrinth disorders:
infrequently - ringing in the ears.
From the cardiovascular system:
uncommon - marked decrease in blood pressure, orthostatic hypotension*, bradycardia.
From the digestive system:
very often - dry mouth; often - diarrhea, nausea, vomiting, dyspepsia.
For the skin and subcutaneous tissues:
often - skin rash, itching.
Allergic reactions:
infrequently - angioedema.
From the musculoskeletal system:
often - back pain;
infrequently - pain in the neck. Other:
often - asthenia; infrequently - peripheral edema.
*Frequency comparable to placebo.
special instructions
During treatment, regular monitoring of blood pressure is necessary.
Post-marketing surveillance has documented cases of AV block of varying severity in patients taking moxonidine. A connection between taking Moxonidine-SZ and slowing AV conduction cannot be completely excluded. Therefore, caution is advised when treating patients likely to develop AV block.
If it is necessary to cancel simultaneously taken beta-blockers and the drug Moxonidine-SZ, first cancel the beta-blockers and only after a few days Moxonidine-SZ. There is currently no evidence that discontinuation of Moxonidine-SZ leads to an increase in blood pressure. However, it is not recommended to stop taking Moxonidine-SZ suddenly; instead, you should gradually reduce the dose of the drug over 2 weeks.
Elderly patients may have an increased risk of developing cardiovascular complications due to the use of antihypertensive drugs, therefore therapy with Moxonidine-SZ should be started with a minimum dose.
Effect on the ability to drive vehicles and operate machinery.
No studies have been conducted on the effect of the drug on the ability to drive a car or operate machinery. There have been reports of drowsiness and dizziness during treatment with moxonidine, which should be taken into account when performing the above actions.
Storage conditions
The drug should be stored out of the reach of children, protected from light at a temperature not exceeding 25°C.
Best before date
Shelf life: 3 years. Do not use after the expiration date stated on the package.
Use during pregnancy and breastfeeding
Restrictions during pregnancy - With caution. Restrictions when breastfeeding - Contraindicated.
There are no clinical data on the use of Moxonidine-SZ in pregnant women. In animal studies, the embryotoxic effect of the drug was established. Moxonidine-SZ should be prescribed to pregnant women only after a careful assessment of the risk-benefit ratio, when the expected benefit to the mother outweighs the potential risk to the fetus.
Moxonidine is excreted in breast milk, so the drug should not be administered during breastfeeding. If it is necessary to use the drug Moxonidine-SZ during lactation, breastfeeding should be stopped.
Use for renal impairment
Restrictions in case of impaired renal function - With caution. The drug should be prescribed with caution in case of moderate renal failure (creatinine clearance 30-60 ml/min, serum creatinine 105-160 µmol/l).
Use for liver dysfunction
Restrictions for liver dysfunction - With caution.
The drug should be prescribed with caution in case of liver failure.
The drug is contraindicated in severe liver failure.
Use in elderly patients
Restrictions for elderly patients - Use with caution.
Elderly patients may have an increased risk of developing cardiovascular complications due to the use of antihypertensive drugs, therefore therapy with Moxonidine-SZ should be started with a minimum dose.
Use in children
Restrictions for children - Contraindicated.
The use of the drug in patients under 18 years of age is contraindicated (due to the lack of data on safety and effectiveness).
Terms of sale
The drug is available with a prescription.
Contacts for inquiries
NORTH STAR NAO (Russia)
111524 Moscow st. Elektrodnaya, 2, building 34, room. 47 Tel./fax
