Moxonidin-SZ
Moxonidin-SZ: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Moxonidine-SZ
ATX code: C02AC05
Active ingredient: moxonidine (Moxonidine)
Manufacturer: CJSC "SEVERNAYA ZVEZDA" (Russia)
Description and photo update: 09.10.2019
Prices in pharmacies: from 112 rubles.
Buy
Moxonidin-SZ is an antihypertensive drug. Refers to selective agonists of imidazoline receptors.
Release form and composition
Moxonidin-SZ is available in the form of film-coated tablets:
- tablets with a dosage of 0.2 mg: biconvex, round, light pink, white or almost white at a break;
- tablets with a dosage of 0.3 mg: biconvex, round, pink, white or almost white at a break;
- tablets with a dosage of 0.4 mg: biconvex, round, dark pink, white or almost white at a break.
Regardless of the dosage, the tablets are packed in blisters of 10, 14 and 30 pcs. or in polymer bottles / polymer cans of 60 pcs. Secondary packaging - cardboard packs in which 3 blisters with 10 tablets in each are put, 1 or 2 blisters with 14 tablets in each, 1, 2, 3 or 4 blisters with 30 tablets in each, 1 can or 1 bottle and instructions for use of Moxonidin-SZ.
Composition for 1 film-coated tablet:
- active substance: moxonidine - 0.2; 0.3 or 0.4 mg;
- auxiliary components of the tablet core: milk sugar, sodium stearyl fumarate, croscarmellose sodium, colloidal silicon dioxide;
- auxiliary components of the shell: Opadray II [titanium dioxide, partially hydrolyzed polyvinyl alcohol, soy lecithin, talc, macrogol and dyes (for tablets with a dosage of 0.2 mg - iron oxide red, iron oxide yellow; for tablets with a dosage of 0.3 mg - solar dye sunset yellow, crimson dye Ponso 4R; for tablets with a dosage of 0.4 mg - azorubin, indigo carmine, crimson dye Ponso 4R)].
Pharmacological properties
Pharmacodynamics
Moxonidine is an antihypertensive substance with a central mechanism of action. It selectively stimulates imidazoline-sensitive receptors located in the brain stem structures and involved in the reflex and tonic regulation of the sympathetic nervous system. As a result of stimulation of imidazoline receptors, peripheral sympathetic activity decreases and blood pressure (blood pressure) decreases.
The affinity of moxonidine for α 2 -adrenergic receptors is lower compared to other sympatholytic antihypertensive drugs, so the likelihood of dry mouth and the risk of sedation is less.
As a result of the use of moxonidine, blood pressure decreases and systemic vascular resistance decreases.
Moxonidine-SZ improves the insulin sensitivity index by 21% (compared to placebo) in patients with insulin resistance, obesity and moderate arterial hypertension.
Pharmacokinetics
Moxonidine is rapidly absorbed in the upper GI tract (gastrointestinal tract). The absorption of the drug is almost 100%. Absolute bioavailability is about 88%. It takes about 1 hour to reach the maximum concentration in the blood plasma. Food intake does not affect the pharmacokinetic parameters of Moxonidine-SZ. No more than 7.2% of the drug binds to plasma proteins.
The main metabolite is dehydrated moxonidine. Its pharmacological activity is about 10% compared to the original substance. The half-life of moxonidine and its main metabolite is 2.5 hours and 5 hours, respectively. More than 90% of the drug is excreted by the kidneys within 24 hours (78% - in unchanged form, 13% - in the form of dehydrated moxonidine and no more than 8% - in the form of other metabolites). Less than 1% of the dose is excreted through the intestines.
In patients with arterial hypertension, the pharmacokinetics of moxonidine does not differ from that in healthy volunteers.
In the elderly, pharmacokinetic parameters change slightly, which is probably due to its slightly higher bioavailability and / or a decrease in the intensity of moxonidine metabolism.
Pharmacokinetic studies of the drug in children and adolescents under 18 years of age have not been conducted.
Excretion of Moxonidine-C3 correlates with CC (creatinine clearance). With moderate renal failure (CC from 30 to 60 ml / min), equilibrium plasma concentrations and the final half-life are almost 2 and 1.5 times higher than those in individuals with normal renal function. In patients with severe renal impairment (CC 90 ml / min). With repeated administration of the drug, predictable accumulation of moxonidine in the blood plasma is observed in patients with severe and moderate renal failure. In persons with end-stage renal failure (CC <10 ml / min) who are on hemodialysis, equilibrium plasma concentrations are 6 times higher, and the terminal half-life is 4 times higher than in patients with normal renal function. In all of these groups, the maximum plasma concentration of the drug was 1.5–2 times higher,therefore, the dosage of moxonidine is selected individually for such patients. With hemodialysis, the elimination of the drug is negligible.
Indications for use
Moxonidine-SZ is used for arterial hypertension in order to reduce high blood pressure.
Contraindications
Absolute:
- severe heart rhythm disturbances;
- SSSU (sick sinus syndrome);
- AV (atrioventricular) blockade II – III degree;
- a significant decrease in heart rate (less than 50 beats / min at rest);
- chronic and acute heart failure (NYHA functional classes III and IV);
- severe renal failure (including patients on hemodialysis);
- lactase deficiency, glucose-galactose malabsorption syndrome, hereditary lactose intolerance (since the tablets contain lactose);
- co-administration with tricyclic antidepressants;
- children and adolescents up to 18 years old;
- advanced age over 75;
- period of breastfeeding;
- hypersensitivity to the main or auxiliary components of the drug.
Relative (Moxonidin-SZ tablets are used with caution):
- unstable angina pectoris, severe ischemic heart disease or severe coronary artery disease (since there is no sufficient experience of use);
- AV blockade of the I degree (due to the risk of developing bradycardia);
- chronic heart failure;
- impaired renal function (CC> 30 ml / min);
- severe liver failure.
Moxonidin-SZ, instructions for use: method and dosage
Moxonidin-SZ tablets are taken orally, regardless of food.
As a rule, the initial dose of the drug is 0.2 mg once a day. The maximum single dose is 0.4 mg, and the maximum daily dose is 0.6 mg (in two divided doses). The daily dose is adjusted if necessary and depending on the tolerability of the treatment.
In hepatic impairment, dose adjustment is not required.
For patients with moderate renal impairment, the initial daily dose should not exceed 0.2 mg. If Moxonidine-SZ is well tolerated and there is a need for a more pronounced therapeutic effect, the dose can be increased to a maximum of 0.4 mg.
Side effects
- digestive system: very often - dryness of the oral mucosa; often - nausea, vomiting, dyspeptic disorders, diarrhea;
- central nervous system and psyche: often - dizziness (vertigo), insomnia, headache, drowsiness; infrequently - nervousness, fainting;
- sense organs: infrequently - ringing in the ears;
- cardiovascular system: infrequently - bradycardia, orthostatic hypotension, marked decrease in blood pressure;
- musculoskeletal system: often - back pain; infrequently - pain in the neck;
- skin and subcutaneous fat: often - itching, rash on the skin; infrequently - Quincke's edema;
- other reactions: often - asthenic state; infrequently - peripheral edema.
Overdose
There are isolated reports of non-fatal overdose of moxonidine, when doses of the drug up to 19.6 mg were used once.
Intoxication symptoms: marked decrease in blood pressure, dryness of the mucous membranes of the oral cavity, headache, increased fatigue, sedation, slowing heart rate (heart rate), vomiting, pain in the epigastric region, dizziness, respiratory depression, asthenia, impaired consciousness. It is also possible a short-term increase in blood pressure, hyperglycemia and tachycardia (such reactions have been shown when studying the effect of high doses of the drug in animal studies).
There is no specific antidote for moxonidine. With a pronounced decrease in blood pressure, an injection of dopamine and liquid may be required to restore the volume of circulating blood. Bradycardia is controlled by parenteral administration of atropine. In severe cases, it is necessary to monitor the patient's condition, especially in cases of impaired consciousness, and prevent respiratory depression.
It is possible to use alpha-adrenergic receptor antagonists, which can eliminate or reduce the hypotensive effects caused by an overdose of the drug. Hemodialysis is ineffective.
special instructions
If beta-blockers are used simultaneously with Moxonidin-C3 and they must be canceled, it is the beta-blockers that are first canceled and only after a few days you can stop taking moxonidine.
To date, there is no reliable evidence that blood pressure rises with abrupt withdrawal of the drug. Despite this, it is recommended to stop treatment with Moxonidine-SZ gradually, gradually reducing the dose over two weeks.
Alcohol should not be consumed during therapy.
Throughout the course of treatment, it is necessary to regularly monitor the heart rate and conduct electrocardiography.
Influence on the ability to drive vehicles and complex mechanisms
The effect of Moxonidine-SZ on the ability to drive vehicles and other complex equipment has not been studied. Given the likelihood of side effects such as drowsiness and dizziness, before establishing an individual response to the drug, you should refrain from work associated with increased concentration of attention and require a quick reaction, or be especially careful when performing them.
Application during pregnancy and lactation
In animal studies, it has been established that moxonidine is embryotoxic. There are no data on the use of the drug during pregnancy, therefore, if necessary, its use should carefully assess the possible risk to the fetus and the expected benefit to the mother.
Moxonidin-SZ is secreted in breast milk. During lactation, its use is contraindicated.
Pediatric use
There are no data on the efficacy and safety of Moxonidine-SZ for children and adolescents under 18 years of age. In this regard, the drug is not used in this age group.
With impaired renal function
The drug should not be administered to patients with severe renal impairment (CC <30 ml / min). In case of impaired renal function of mild and moderate severity, Moxonidine-SZ is used with caution (at an initial dose of no more than 0.2 mg per day).
For violations of liver function
In patients with severe hepatic impairment, the use of Moxonidine-SZ is possible, but requires caution. There is no need for dose adjustment.
Use in the elderly
Moxonidin-SZ is not prescribed to persons over 75 years old.
Drug interactions
Other antihypertensive drugs enhance the action of Moxonidin-SZ (an additive effect is observed).
It is not recommended to use moxonidine simultaneously with tricyclic antidepressants, since the latter can reduce the effectiveness of antihypertensive drugs.
Moxonidine-SZ can enhance the therapeutic effect of ethanol, tranquilizers, hypnotics and sedatives, and tricyclic antidepressants.
In patients receiving lorazepam, Moxonidine-SZ may moderately improve cognitive function.
With simultaneous use with benzodiazepine derivatives, their sedative properties may be enhanced.
Since moxonidine is excreted by tubular secretion, the possibility of its interaction with other drugs excreted by secretion in the renal tubules cannot be excluded.
Beta-blockers increase the severity of negative dromotropic and inotropic effects, and also increase bradycardia.
Analogs
Moxonidin-SZ analogs are Moxonidin, Moxonidin Canon, Moxarel, Moxonitex, Physiotens, Tenzotran, etc.
Terms and conditions of storage
Store in a dark place, out of the reach of children, at a temperature not exceeding 25 ° C.
The shelf life of the tablets is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Moxonidine-SZ
According to reviews, Moxonidin-SZ quickly and effectively reduces high blood pressure. The tablets are easy and convenient to take. The cost of the drug is low compared to some of the more expensive analogues.
At the same time, users note that Moxonidine-SZ should be used with caution, since it is possible to develop persistent bradycardia. It should also be borne in mind that when using moxonidine simultaneously with hypnotics, coordination of movements may be impaired. Some patients developed dry mouth after taking the pills.
Price for Moxonidin-SZ in pharmacies
Approximate prices for Moxonidin-SZ, film-coated tablets, depend on the dosage and the number of tablets in the package:
- dosage 0.2 mg: 14 pcs. in the package - 70–80 rubles; 28 pcs. in the package - 150–160 rubles; 60 pcs. in the package - 250-280 rubles; 90 pcs. in the package - 400–410 rubles;
- dosage 0.3 mg, 28 pcs. in the package - 140–150 rubles;
- dosage 0.4 mg, 14 pcs. in the package - 110–120 rubles; 28 pcs. in the package - 200-250 rubles; 60 pcs. in the package - 380-420 rubles; 90 pcs. in the package - 600-610 rubles.
Moxonidin-SZ: prices in online pharmacies
|
Drug name Price Pharmacy |
|
Moxonidin-SZ tablets p.o. 0.2mg 14 pcs. 112 RUB Buy |
|
Moxonidin-SZ tablets p.o. 0.4mg 14 pcs. 120 RUB Buy |
|
Moxonidin-SZ tablets p.o. 0.3mg 28 pcs. RUB 145 Buy |
|
Moxonidin-SZ tablets p.o. 0.2mg 28 pcs. 232 RUB Buy |
|
Moxonidin-SZ tablets p.o. 0.2mg 60 pcs. 279 r Buy |
|
Moxonidin-SZ tablets p.o. 0.2mg 90 pcs. 347 r Buy |
|
Moxonidin-SZ 200 mcg tablets 90 pcs. 347 r Buy |
|
Moxonidin-SZ tablets p.o. 0.4mg 28 pcs. 353 r Buy |
|
Moxonidin-SZ tablets p.o. 0.4mg 60 pcs. 401 RUB Buy |
|
Moxonidin-SZ tablets p.o. 0.4mg 90 pcs. 572 r Buy |
| See all offers from pharmacies |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
