Description
Pharmacological action
An antihypertensive drug with a central mechanism of action. In the brain stem structures (the rostral layer of the lateral ventricles), moxonidine selectively stimulates the imidazoline-sensitive receptors involved 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 agents in a lower affinity for ОІ2-adrenergic receptors, which explains the lower likelihood of developing a sedative effect and dry mouth. The use of moxonidine leads to a decrease in OPSS and blood pressure.
Moxonidine improves the insulin sensitivity index (compared with placebo) by 21% in patients with obesity, insulin resistance, and moderate arterial hypertension.
Indications
arterial hypertension.
Contraindications
severe renal failure (CC less than 30 ml / min)
severe cardiac arrhythmias
SSSL
severe bradycardia (resting heart rate less than 50 beats. / min)
AV block II and III degree
acute and chronic heart failure (NYHA class III-IV functional class)
simultaneous use with tricyclic antidepressants
hemodialysis
lactation period
age over 75 years old
age up to 18 years (in due to the lack of safety and efficacy data)
hereditary lactose intolerance, lactase deficiency or malabsorption of glucose-galactose
hypersensitivity to the active substance and other components of the drug.
Caution
Special care must be taken when using moxonidine in patients with degree I AV block (risk of developing bradycardia), severe coronary artery disease, severe coronary artery disease, or unstable angina (insufficient experience), chronic heart failure, severe liver failure, impaired renal function (CC more than 30 ml / min).
Recommendations for use
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. An individual correction of the daily dose is necessary depending on the patient’s tolerance of the therapy.
Dose adjustment for patients with hepatic insufficiency is not required.
The initial dose for patients with moderate to severe renal failure is 0.2 mg / day. If necessary and with good tolerance, the daily dose can be increased to a maximum of 0.4 mg.
Composition
Tablets, film-coated, dark pink, round, biconvex at a 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, azorubine dye based aluminum varnish – 0.0153 mg, dye based aluminum varnish crimson [Ponceau 4R] – 0.0123 mg).
Side effects
The frequency of side effects below was determined according to the following: very often (> 1/10) often (> 1/100, <1/10) infrequently (> 1/1000, <1/100) including individual messages. From the side of the central nervous system: often – headache *, dizziness (vertigo), drowsiness infrequently – fainting *. Mental disorders: often – insomnia infrequently – nervousness. On the part of the hearing organ and labyrinth disorders: infrequently – ringing in the ears. From the cardiovascular system: infrequently – a marked decrease in blood pressure, orthostatic hypotension *, bradycardia. From the digestive system: very often – dryness of the oral mucosa often – diarrhea, nausea, vomiting, dyspepsia. From the skin and subcutaneous tissues: often – skin rash, itching. From the musculoskeletal system: often – back pain infrequently – pain in the neck. Allergic reactions: infrequently – angioedema. General disorders and disorders at the injection site: often – asthenia infrequently – peripheral edema. * – the frequency is comparable to placebo. Overdose There are reports of several cases of overdose without fatal outcome, when doses up to 19.6 mg were used simultaneously. Symptoms: headache, sedation, excessive decrease in blood pressure, dizziness, asthenia, bradycardia, dry oral mucosa, vomiting, fatigue, pain in the epigastric region, respiratory depression and impaired consciousness. In addition, a short-term increase in blood pressure, tachycardia and hyperglycemia are also possible, as has been shown in several studies on the use of the drug in high doses in animals. Treatment: There is no specific antidote. In the case of an excessive decrease in blood pressure, it may be necessary to restore the BCC due to the introduction of fluid and dopamine (injection). Bradycardia can be stopped with atropine (injection). In severe cases of overdose, it is recommended to carefully monitor impaired consciousness and prevent respiratory depression. Antagonists of β-adrenergic receptors can reduce or eliminate the paradoxical hypertensive effects of an overdose of moxonidine. Moxonidine is slightly excreted during hemodialysis. Active ingredient moxonidine lekarstvennaja form tablets
