Moxonidine
Moxonidine: 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. Use in the elderly
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Moxonidine
ATX code: C02AC05
Active ingredient: Moxonidine (Moxonidine)
Manufacturer: Atoll, LLC (Russia), Farmzashchita, NPC (Russia), Severnaya Zvezda, CJSC (Russia)
Description and photo update: 2018-25-10
Prices in pharmacies: from 83 rubles.
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Moxonidine is a centrally acting antihypertensive drug.
Release form and composition
Film-coated tablets: round, biconvex, from pink to pale pink; 2 layers are visible in the cross section - a film shell and an almost white core (7, 10 and 14 pcs. in blisters, in a cardboard box 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 packages; 10, 20, 30, 40, 50, 60 and 100 pcs. in polyethylene terephthalate or polymer cans, in a cardboard box 1 can).
Composition of 1 tablet:
- active substance: moxonidine - 0.2 or 0.4 mg;
- excipients (core): magnesium stearate, croscarmellose sodium, povidone-K25, lactose monohydrate (milk sugar);
- excipients (shell): titanium dioxide, macrogol-4000, hypromellose, iron dye red oxide.
Pharmacological properties
Pharmacodynamics
Moxonidine - the active substance of the drug - a selective agonist of imidazoline receptors, which reduces sympathetic activity, selectively interacts with imidazoline I 1 receptors, which are located in the brain stem.
Decrease in diastolic and systolic blood pressure with the use of moxonidine (single or long-term) is due to its ability to reduce the pressor effect of the sympathetic system on peripheral vessels and reduce peripheral vascular resistance, without significantly affecting cardiac output and heart rate.
The maximum antihypertensive effect is achieved 2.5-7 hours after oral administration of the drug.
Moxonidine has a high affinity for imidazoline I 1 receptors. It binds to central alpha 2 -adrenergic receptors only slightly, which explains the sedative effect and dryness of the oral mucosa.
The drug stimulates the release of growth hormone, reduces tissue resistance to insulin.
Pharmacokinetics
Moxonidine absorption is 90%. The maximum plasma concentration after taking 0.2 mg of the drug is reached after 30-180 minutes and is 1.4-3 ng / ml.
The bioavailability of the substance is 88%. Food intake does not affect its pharmacokinetics.
The volume of distribution is 1.8 ± 0.4 l / kg. It binds to blood plasma proteins by about 10%.
Penetrates the blood-brain barrier.
It is metabolized to form metabolites, mainly derivatives of guanidine and 4,5-dihydromoxonidine. The pharmacodynamic activity of the latter is about 10% compared to moxonidine.
The half-life (T 1/2) of moxonidine is 2.5 hours, metabolites is 5 hours.
The average final T 1/2 of moxonidine in the blood plasma is 2.2–2.3 hours, the average end renal T 1/2 is 2.6–2.8 hours.
Moxonidine is excreted mainly by the kidneys: within a day after administration - more than 90%, of which 50-75% - unchanged, 13% - in the form of a dehydrogenated derivative. In a small amount (no more than 1%) it is excreted through the intestines.
With prolonged use, moxonidine does not cumulate.
Changes in pharmacokinetic parameters are observed in patients of different ages, which is presumably associated with a higher bioavailability of moxonidine and / or a reduced metabolic activity. However, these changes have no clinical significance.
Excretion of moxonidine is highly correlated with creatinine clearance (CC).
In moderate renal failure (CC 30-60 ml / minute), equilibrium plasma concentrations and final T 1/2 are approximately 2 and 1.5 times higher, respectively, and in severe renal failure (CC 90 ml / minute).
With prolonged use, moxonidine does not accumulate in the body of patients with moderate renal failure.
In end-stage renal failure (CC <10 ml / min) in patients on hemodialysis, equilibrium plasma concentrations and final T 1/2, respectively, are 6 and 4 times higher than in patients with normal night function.
Moxonidine is excreted in small quantities during hemodialysis.
Indications for use
The drug is used for arterial hypertension.
Contraindications
- severe renal failure (CC less than 30 ml / min, plasma creatinine more than 160 μmol / l);
- hemodynamically significant heart rhythm disturbances;
- severe chronic heart failure III – IV functional class in accordance with the NYHA classification;
- severe bradycardia (heart rate less than 50 beats / minute);
- severe bradyarrhythmia, including sick sinus syndrome, atrioventricular block II and III degree;
- lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
- age under 18 and over 75;
- simultaneous use of tricyclic antidepressants;
- hypersensitivity to drug components.
Due to the lack of experience in the use of Moxonidine, it is not recommended to prescribe for the following diseases: Parkinson's disease, depression, glaucoma, epilepsy, Raynaud's disease, intermittent claudication.
The drug should be used with caution in the following cases:
- a history of angioedema;
- severe ischemic heart disease;
- bradycardia;
- unstable angina;
- severe coronary artery disease;
- chronic heart failure I – II functional class according to NYHA classification;
- atrioventricular block I degree;
- chronic renal failure (CC 30-60 ml / min);
- advanced age (from 60 to 75 years).
Instructions for the use of Moxonidine: method and dosage
Moxonidine is taken orally with a sufficient amount of liquid. Time of meals does not matter.
The starting dose is usually 0.2 mg in the morning. If the therapeutic effect after 3 weeks is not pronounced enough, you can increase the daily dose to 0.4 mg in 1 or 2 doses. If the therapeutic effect after 3 weeks is unsatisfactory, you can increase the daily dose to 0.6 mg in 2 divided doses - in the morning and in the evening.
The maximum allowable doses: single - 0.4 mg, daily - 0.6 mg.
Patients with renal insufficiency (CC 30-60 ml / minute) are prescribed 0.2 mg at the beginning of therapy. If the effect is not enough, you can increase the dose to 0.4 mg per day (only if the drug is well tolerated).
Side effects
- from the digestive system: very often (≥ 1/10) - dryness of the oral mucosa; often (≥ 1/100 to <1/10) - diarrhea, nausea, vomiting, dyspepsia; infrequently (≥ 1/1000 to <1/100) - anorexia;
- on the part of the organ of vision: infrequently - a burning sensation in the eyes, dry eyes;
- on the part of the organ of hearing: infrequently - tinnitus;
- on the part of the cardiovascular system: often - vasodilation; infrequently - impaired peripheral circulation, a marked decrease in blood pressure (including orthostatic hypotension);
- from the genitourinary system: infrequently - decreased libido and / or impotence;
- from the endocrine system: infrequently - gynecomastia;
- from the musculoskeletal system: often - back pain; infrequently - neck pain;
- from the central nervous system: often - sleep disturbance, drowsiness, headache, vertigo, increased fatigue; infrequently - paresthesia, fainting;
- mental disorders: often - impaired cognitive functions, insomnia; infrequently - anxiety, nervousness;
- allergic reactions: often - itching, skin rash; infrequently - angioedema;
- others: often - asthenia; infrequently - soreness in the parotid glands, weakness in the legs, peripheral edema.
Overdose
Symptoms: dryness of the oral mucosa, fatigue, drowsiness, headache, increased asthenia, sedation, dizziness, marked decrease in blood pressure, bradycardia; rarely - pain in the upper abdomen, vomiting. Also, presumably, hyperglycemia, tachycardia, paradoxical arterial hypertension are possible.
There is no specific antidote to moxonidine. Overdose treatment is aimed at eliminating the symptoms that have arisen. If a little time has passed since the moment of administration, it is recommended to rinse the stomach, take activated charcoal and a laxative to reduce the absorption of the drug. With bradycardia, the introduction of atropine is indicated, with a pronounced decrease in blood pressure - the restoration of the volume of circulating blood by the introduction of fluid and dopamine. Antagonists of α-adrenergic receptors help to eliminate or reduce paradoxical antihypertensive effects.
special instructions
Blood pressure, heart rate, and electrocardiogram should be monitored regularly during treatment.
Moxonidine should be discontinued gradually, reducing the dose within 2 weeks.
With the concomitant use of beta-blockers, if it is necessary to cancel both drugs, beta-blockers should be canceled first, and after a few days - Moxonidine.
During the period of therapy, you must refrain from drinking alcohol.
Influence on the ability to drive vehicles and complex mechanisms
Due to the risk of drowsiness and dizziness when using the drug, it is recommended to refrain from performing potentially hazardous activities that require speed of reactions and increased attention, including driving.
Application during pregnancy and lactation
There is no experience with moxonidine during pregnancy, so the drug can only be used in exceptional cases when the expected benefits outweigh the potential risks.
Moxonidine is excreted in breast milk, therefore, it is not prescribed during lactation, or breastfeeding should be stopped.
Pediatric use
Pharmacokinetic studies on the use of the drug in patients under 18 years of age have not been conducted, therefore it is not used in pediatrics.
With impaired renal function
According to the instructions, Moxonidine is contraindicated in severe renal failure (CC less than 30 ml / min, plasma creatinine more than 160 μmol / L).
For patients with impaired renal function, the dosage of the drug should be selected individually.
Use in the elderly
Moxonidine should be used with caution when treating elderly patients. Dosage recommendations are similar to those for adult patients with normal renal function. Treatment should be started with a minimum dose, the subsequent increase should be carried out under close medical supervision.
The drug is contraindicated in elderly people - over 75 years old.
Drug interactions
- tricyclic antidepressants: a decrease in the hypotensive effect of moxonidine is possible;
- antihypertensive drugs: the antihypertensive effect is mutually enhanced;
- anxiolytics, barbiturates, ethanol: their depressing effect on the central nervous system is enhanced;
- beta-blockers: increased bradycardia, negative dromo- and inotropic effects of moxonidine;
- derivatives of benzodiazepine: it is possible to enhance their sedative effect;
- tolazoline: the antihypertensive effect of moxonidine decreases (the degree of reduction depends on the dose of tolazoline);
- lorazepam: Moderately enhanced cognitive decline in patients.
There is no pharmacokinetic interaction of moxonidine with hydrochlorothiazide, digoxin and glibenclamide.
Analogs
Moxonidin analogs are: Moxarel, Moxonidin Canon, Moxonidin C3, Moxonitex, Tenzotran, Physiotens.
Terms and conditions of storage
The shelf life is 3 years.
Storage conditions: inaccessible to children, protected from light, temperature - up to 25 ° C.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Moxonidine
According to reviews, Moxonidine is an effective antihypertensive agent that reduces high blood pressure both with a single dose and with prolonged use.
Price for Moxonidine in pharmacies
Average prices for Moxonidine, depending on dosage and packaging:
- tablets 0.2 mg, 14 pcs. in the package - 100 rubles;
- tablets 0.2 mg, 20 pcs. in the package - 141 rubles;
- tablets 0.2 mg, 28 pcs. in the package - 183 rubles;
- tablets 0.4 mg, 14 pcs. in the package - 161 rubles;
- tablets 0.4 mg, 28 pcs. in the package - 225 rubles;
- tablets 0.4 mg, 30 pcs. in the package - 234 rubles.
Moxonidine: prices in online pharmacies
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Drug name Price Pharmacy |
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Moxonidine 0.2 mg film-coated tablets 14 pcs. 83 rbl. Buy |
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Moxonidine 200 mcg film-coated tablets 14 pcs. RUB 99 Buy |
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Moxonidin Canon 0.2 mg film-coated tablets 14 pcs. RUB 103 Buy |
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Moxonidin Canon 0.2 mg film-coated tablets 28 pcs. 108 RUB Buy |
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Reviews Moxonidine Canon 108 RUB Buy |
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Moxonidine tablets p.o. 200μg 14 pcs. 117 RUB Buy |
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Moxonidine Canon tablets p.o. 0.2mg 28 pcs. 117 RUB Buy |
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Moxonidine 0.4 mg film-coated tablets 14 pcs. 117 RUB Buy |
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Moxonidine 200 mcg film-coated tablets 20 pcs. 124 RUB Buy |
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Moxonidine tab. p / o 200mkg No. 20 135 RUB Buy |
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Moxonidine Canon tablets p.o. 0.4mg 14 pcs. 139 RUB Buy |
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Moxonidine Canon 0.4 mg film-coated tablets 14 pcs. 139 RUB Buy |
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Moxonidine 200 mcg film-coated tablets 28 pcs. RUB 160 Buy |
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Moxonidin Canon 0.4 mg film-coated tablets 28 pcs. 171 r Buy |
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Moxonidine tablets p.o. 0.4mg 14 pcs. 172 r Buy |
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Moxonidine 400 mcg film-coated tablets 28 pcs. 178 r Buy |
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Moxonidine Canon tablets p.o. 0.4mg 28 pcs. RUB 180 Buy |
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Moxonidin Avexima tablets p.p. 0.2mg 30 pcs 183 r Buy |
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Moxonidine 400 mcg film-coated tablets 30 pcs. 199 RUB Buy |
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Moxonidin Canon tablets p.p. 0.2mg 60pcs RUB 200 Buy |
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Moxonidine Canon 0.2 mg film-coated tablets 60 pcs. RUB 200 Buy |
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Moxonidine tablets p.o. 400μg 30 pcs. 241 RUB Buy |
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Moxonidin Avexima tablets p.p. 0.4mg 30 pcs 268 r Buy |
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Moxonidin tablets p.p. 400 mcg 28 pcs. RUB 300 Buy |
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Moxonidin Avexima tablets p.p. 0.2mg 60 pcs 303 RUB Buy |
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Moxonidin Canon 0.4 mg film-coated tablets 60 pcs. 313 r Buy |
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Moxonidin Canon tablets p.p. 0.4mg 60pcs 316 RUB Buy |
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Moxonidine Avexima tablets p.p. 0.4mg 60 pcs 409 r Buy |
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Moxonidine 400 mcg tablets 90 pcs. 549 r Buy |
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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!
