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Moxonidine

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2019-09-19
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Clinical Pharmacology

Moxonidine is a hypotensive agent with a central mechanism of action. In the brain stem structures (rostral layer of the lateral ventricles), moxonidine selectively stimulates imidazolin-sensitive receptors involved in the tonic and reflex regulation of the sympathetic nervous system. Stimulation of the imidazoline receptor decreases peripheral sympathetic activity and blood pressure.

Moxonidine differs from other adrenergic antihypertensive drugs by its lower affinity for α.1-adrenoreceptors, which explains the lower likelihood of developing a sedative effect and dryness of the oral mucosa.

Acceptance of moxonidine leads to a decrease in systemic vascular resistance and blood pressure.

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 GI tract. Absolute bioavailability is approximately 88%. Tmax - about 1 h. Eating does not affect the pharmacokinetics of the drug.

Distribution. Communication with plasma proteins is 7.2%.

Metabolism. The main metabolite is dehydrated moxonidine. The pharmacodynamic activity of dehydrated moxonidine is about 10% compared with moxonidine.

Derivation. T1/2 moxonidine and the metabolite are 2.5 and 5 h, respectively. Within 24 hours, more than 90% of moxonidine is excreted by the kidneys (about 78% unchanged and 13% as dehydromoxonidine, other metabolites in the urine do not exceed 8% of the accepted dose). Less than 1% of the dose is eliminated through the intestines.

Special patient groups

Elderly patients. Clinically insignificant changes in the pharmacokinetic parameters of moxonidine in elderly patients are noted, probably due to a decrease in the intensity of its metabolism and / or slightly higher bioavailability.

Children. Moxonidine is not recommended for use in patients younger than 18 years, and therefore in this group pharmacokinetic studies have not been conducted.

Impaired renal function. Moxonidine clearance largely correlates with creatinine clearance. In patients with moderate renal insufficiency (Cl creatinine 30–60 ml / min) Css in plasma and end T1/2 approximately 2 and 1.5 times higher than in patients with normal renal function (Cl creatinine more than 90 ml / min). In patients with severe renal insufficiency (Cl creatinine less than 30 ml / min) Css in plasma and end T1/2 3 times higher than in patients with normal renal function. The administration of multiple doses of moxonidine leads to predictable cumulation in the body of patients with moderate to severe renal failure. In patients with end-stage renal disease (Cl creatinine less than 10 ml / min) on hemodialysis, Css in plasma and end T1/2respectively, 6 and 4 times higher than in patients with normal renal function.

In all groups, the maximum plasma concentration of moxonidine is 1.5–2 times higher. In patients with impaired renal function, the dosage should be adjusted individually. Moxonidine is slightly excreted during hemodialysis.

Indications

Arterial hypertension.

Composition

1 tablet contains:

Active substance: moxonidine;

Excipients: lactose monohydrate; MCC; colloidal silicon dioxide; Povidone K30; croscarmellose sodium; magnesium stearate.

Moxonidine is marketed under different brands and generic names, and comes in different dosage forms:

Brand nameManufacturerCountryDosage form
Moxonitex Sandoz Switzerland pills
Moxonidine-SZ North Star Russia pills
Moxonidine-SZ pills
Moxonidine Canonpharma Russia pills
Physiotens Abbott USA pills
Moxarel Vertex Russia pills
Moxonidine Pharmaceutical NPC Russia pills
Tensotran Perrigo Israel Pharmaceuticals Ltd Israel pills

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Moxonidine

Dosage and Administration

Inside, regardless of the meal.

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. An individual adjustment of the daily dose depending on the patient's tolerance of the therapy being performed is required.

Dose adjustment for patients with liver failure is not required. The initial dose for patients with moderate or severe renal insufficiency is 0.2 mg / day.

If necessary and with good tolerance, the daily dose may be increased to a maximum of 0.4 mg.

Adverse reactions

The frequency of the side effects listed below was determined according to the following: very often (> 1/10); often (> 1/100, <1/10); infrequently (> 1/1000, <1/100); including individual posts.

From the side of the central nervous system:

Often: headache *, dizziness (vertigo), drowsiness.

Infrequently: faint *.

Since the cardiovascular system:

Infrequently: pronounced decrease in blood pressure, orthostatic hypotension *, bradycardia.

From the gastrointestinal tract:

Very often: dryness of the oral mucosa.

Often: diarrhea, nausea, vomiting, dyspepsia.

Skin and Subcutaneous Tissues:

Often: skin rash, itching.

Infrequently: angioedema.

Mental Disorders:

Often: insomnia.

Infrequently: nervousness.

On the part of the organ of hearing and labyrinth disorders:

Infrequently: ringing in the ears.

From the musculoskeletal and connective tissue:

Often: back pain.

Infrequently: pain in the neck.

General disorders and disorders at the site of administration:

Often: asthenia.

Infrequently: peripheral edema.

(* - the frequency is comparable to placebo).

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;

- pronounced cardiac arrhythmias;

- acute and chronic heart failure (NYHA class III-IV functional class);

- simultaneous use with tricyclic antidepressants (see the section "Interaction with Other Medicines");

- severe renal failure (CC less than 30 ml / min);

- hemodialysis;

- lactation period;

- hereditary lactose intolerance, lactase deficiency or glucose-galactose malabsorption;

- age over 75 years;

- age up to 18 years (due to the lack of data on safety and efficacy).

Carefully:

Special care should be taken when applying moxonidine in patients with atrioventricular block I degree (risk of developing bradycardia); severe coronary vascular disease, severe coronary heart disease or unstable angina (insufficient use of experience), chronic heart failure, severe liver failure, with impaired renal function (CC more than 30 ml / min).

Drug interactions

The combined use of moxonidine with other antihypertensive drugs leads to an additive effect.

Tricyclic antidepressants can reduce the effectiveness of centrally acting antihypertensive drugs, and therefore they are not recommended in conjunction with moxonidine.

Moxonidine can enhance the action of tricyclic antidepressants, tranquilizers, ethanol, sedatives and hypnotics.

Moxonidine can moderately improve impaired cognitive function in patients receiving lorazepam.

Moxonidine may enhance the sedative effect of benzodiazepine derivatives when administered concurrently.

Moxonidine is secreted by tubular secretion. Therefore, its interaction with other drugs secreted by tubular secretion is not excluded.

Beta-blockers enhance bradycardia, the severity of negative insomnia and dromotropic action.

Pregnancy and Lactation

Pregnancy

Clinical data on the use of Moxonidine in pregnant women are not available. In animal studies, the embryotoxic effect of the drug was established.

Moxonidine should be prescribed to pregnant women only after a thorough assessment of the risk-benefit ratio, when the benefit to the mother outweighs the potential risk to the fetus.

Lactation period

Moxonidine penetrates into breast milk and therefore should not be administered during breastfeeding.

If necessary, the use of Moxonidine during lactation, breastfeeding should be stopped.

Special instructions

If it is necessary to cancel simultaneously taken beta-blockers and the drug Moxonidine-C3, first remove the beta-blockers and only a few days later Moxonidine-C3.

Currently there is no evidence that discontinuation of the drug Moxonidine leads to an increase in blood pressure. However, it is not recommended to stop taking the drug Moxonidine abruptly, instead, you should gradually reduce the dose of the drug within two weeks.

During treatment, exclude alcohol.

During treatment, regular monitoring of heart rate and electrocardiography is necessary.

Impact on the ability to drive trans. Wed and fur .:

The effect of Moxonidine on the ability to drive vehicles or control technology 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 controlling equipment that requires increased concentration.

Overdosage

There are reports of several cases of overdose without death, when doses of up to 19.6 mg were applied simultaneously.

Symptoms: headache, sedation, marked decrease in blood pressure, dizziness, asthenia, bradycardia, dryness of the 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 has been shown in several high-dose studies in animals.

Treatment

There is no specific antidote. In the case of a pronounced decrease in blood pressure, it may be necessary to restore the circulating blood volume by injecting fluid and dopamine (injection).

Bradycardia can be stopped by atropine (injectable).

In severe cases of overdose, it is recommended to carefully monitor impairment of consciousness and to prevent respiratory depression.

Alpha-adrenoreceptor antagonists can reduce or eliminate the paradoxical hypertensive effects of moxonidine overdose.

Moxonidine is slightly excreted during hemodialysis.

  • Brand name: Moxonitex
  • Active ingredient: Moxonidine
  • Manufacturer: Sandoz

Studies and clinical trials of Moxonidine (Click to expand)

  1. Randomized clinical trial of moxonidine in patients undergoing major vascular surgery
  2. Synthesis of triple [14C]-labeled moxonidine
  3. Determination of moxonidine (BDF 5895) in plasma by gas chromatography—negative ion chemical ionization mass spectrometry
  4. Determination of moxonidine in human plasma by liquid chromatography–electrospray ionisation–mass spectrometry
  5. Population pharmacokinetic-pharmacodynamic modeling of moxonidine using 24-hour ambulatory blood pressure measurements
  6. Pharmacodynamic models for the cardiovascular effects of moxonidine in patients with congestive heart failure
  7. Quinidine does not affect the renal clearance of moxonidine
  8. Central nervous system effects of moxonidine experimental sustained release formulation in patients with mild to moderate essential hypertension
  9. Metabolic effects of moxonidine and other centrally acting antihypertensives
  10. A novel approach to treatment of hypertension in diabetic patients – a multicenter, double-blind, randomized study comparing the efficacy of combination therapy of Eprosartan versus Ramipril with low-dose Hydrochlorothiazide and Moxonidine on blood pressure levels in patients with hypertension and associated diabetes mellitus type 2 – rationale and design [ISRCTN55725285]
  11. Adjunctive treatment with moxonidine versus nitrendipine for hypertensive patients with advanced renal failure: a cost-effectiveness analysis
  12. Drug withdrawal and rebound hypertension: Differential action of the central antihypertensive drugs moxonidine and clonidine
  13. Hemodynamic and neurohumoral effects of moxonidine in patients with essential hypertension
  14. Presynaptic imidazoline receptors and α2-adrenoceptors in the human heart: discrimination by clonidine and moxonidine
  15. Effect of moxonidine on urinary electrolyte excretion and renal haemodynamics in man
  16. Crossover comparison of moxonidine and clonidine in mild to moderate hypertension
  17. Intraindividual comparison of moxonidine and prazosin in hypertensive patients
  18. A novel mechanism of action for hypertension control: Moxonidine as a selective I1-imidazoline agonist
  19. Clinical experience with moxonidine
  20. Lack of pharmacokinetic interaction between moxonidine and hydrochlorothiazide
  21. Influence of different dietary salts on the cardiovascular and renal effects of moxonidine in spontaneously hypertensive rats
  22. Analysis of the receptor involved in the central hypotensive effect of rilmenidine and moxonidine
  23. Site of action of moxonidine in the rat nephron
  24. Moxonidine and cognitive function: interactions with moclobemide and lorazepam

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