MOKSOGAMMA
Active material: Moksonidin
When ATH: C02AC05
CCF: Selective imidazoline receptor agonist. Antihypertensive drugs
ICD-10 codes (testimony): I10
When CSF: 01.09.01.02
Manufacturer: Worwag PHARMA GmbH & Co. KG (Germany)
Pharmaceutical form, composition and packaging
Pills, Film-coated light pink, round.
1 tab. | |
moksonidin | 200 g |
Excipients: lactose bezvodnaya, povidone K25, krospovydon, magnesium stearate, Opadry Y-1-7000 (Titanium dioxide, gipromelloza, macrogol 400, iron oxide red).
10 PC. – blisters (3) – packs cardboard.
Pills, Film-coated Pink colour, round.
1 tab. | |
moksonidin | 300 g |
Excipients: lactose bezvodnaya, povidone K25, krospovydon, magnesium stearate, Opadry Y-1-7000 (Titanium dioxide, gipromelloza, macrogol 400, iron oxide red).
10 PC. – blisters (3) – packs cardboard.
Pills, Film-coated dark pink, round.
1 tab. | |
moksonidin | 400 g |
Excipients: lactose bezvodnaya, povidone K25, krospovydon, magnesium stearate, Opadry Y-1-7000 (Titanium dioxide, gipromelloza, macrogol 400, iron oxide red).
10 PC. – blisters (3) – packs cardboard.
Pharmacological action
Antihypertensive drugs, agonist selective imidazoline receptor I-, which are responsible for tonic and reflex control of the sympathetic nervous system (located in Venter-lateral medulla).
To a small extent associated with the central α2-adrenoreceptor, due to the interaction which is mediated dry mouth and sedation.
It reduces the resistance of tissues to insulin.
With a single and continuous moxonidine a reduction in systolic and diastolic blood pressure, due to the reduction of the pressor actions of the sympathetic system at the peripheral vessels, reduction in systemic vascular resistance, whereas cardiac output and heart rate did not significantly change.
Pharmacokinetics
Absorption
After oral administration absorption is 90%. Ingestion by an amount of absorption is not affected. Bioavailability – 88%. Cmax plasma is determined by 30-180 min after oral administration and is 1-3 ng / ml.
Distribution
Plasma protein binding is – 7%. Vd – 1.4-3 l / kg. It penetrates through the BBB. Not accumulates long-term use.
Deduction
T1/2 – 2-3 no. Report the news – 90% (70% – in unchanged form, 20% – as metabolites).
Pharmacokinetics in special clinical situations
No significant differences in the pharmacokinetics in patients younger and older age groups were found.
Testimony
- Arterial hypertension.
Dosage regimen
The drug is taken orally, regardless of the meal, drinking plenty of fluids.
In most cases the initial dose Moksogamma® is 200 mg / day 1 reception, preferably in the morning hours. When failure of the therapeutic effect of the dose can be increased through 3 weeks of therapy to 400 mg / day 1-2 admission.
The maximum daily dose, which should be divided into 2 admission (in the morning and in the evening), is 600 g. The maximum single dose – 400 g.
In elderly patients with normal renal function dosing recommendations such as, as for adult patients.
To patients with renal insufficiency (CC 30-60 ml / min) and patients, hemodialysis, The maximum single dose is 200 g, the maximum daily dose – 400 g.
Side effect
Determination of the frequency of adverse reactions: Often (more 1/10), often (more 1/100, less 1/10), sometimes (more 1/1000 less 1/100), rarely (less 1/1000, including isolated reports).
Frequently (especially early in treatment): dry mouth, headache, asthenia and sonlivosty. The intensity of the symptoms and the frequency of these reactions decreases with readmission.
From the central and peripheral nervous system: Often – drowsiness, headache, distraction, depression of consciousness; often – impaired ability to concentrate; sometimes – depression, alarm.
Cardio-vascular system: often – vasodilation; sometimes – decrease in blood pressure, orthostatic hypotension, limb paresthesia, Raynaud's syndrome, peripheral circulatory disorders.
From the digestive system: often – dry mouth, nausea, constipation, dyspeptic disorders; sometimes – anorexia; rarely – hepatitis, bile stasis.
From the urinary system: sometimes – delay or incontinence.
From the senses: sometimes – dry eyes, accompanied by itching or burning sensation.
On the part of the endocrine system: sometimes – gynecomastia, impotence, decreased libido.
Allergic reactions: sometimes – cutaneous manifestations, angioedema.
Other: often – asthenia; sometimes – swelling of various localization, weakness in the legs, fainting, fluid retention, pain in the parotid glands.
Contraindications
- SSS;
- Sinoatrialynaya blockade;
— AV-blockade II and III degrees;
- Vыrazhennaya bradycardia (HR less 50 u. / min);
- Chronic heart failure III and IV functional class (NYHA classification);
- A history of angioedema;
- Unstable angina;
- Severe hepatic impairment;
- Chronic renal failure (CC < 30 ml / min, sыvorotochchnыy creatinine > 160 mmol / l);
- Up to 18 years (efficacy and safety have not been established);
- Lactation (breast-feeding);
- Concomitant use of tricyclic antidepressants;
- Galactose intolerance, lactase deficiency, glucose-galactose malabsorption;
- Hypersensitivity to the drug.
FROM caution should use the drug in patients with Parkinson's disease (severe form), epilepsy, glaukomoj, depression, intermittent claudication, Raynaud's disease, AV block I degrees, chronic renal failure (CC > 30 ml / min, but < 60 ml / min), cerebrovascular diseases, after myocardial infarction, in chronic heart failure class I and II, mild to moderate hepatic insufficiency (due to lack of experience with), hemodialysis, Pregnancy.
Pregnancy and lactation
Precautions should use the drug during pregnancy. Clinical data on the negative impact of the drug on the course of pregnancy is not.
Use of the drug during lactation (breast-feeding) contraindicated.
Cautions
If you need to cancel at the same time received beta-blockers and Moksogammy® first cancel the beta-blockers and just a few days – Moksogammu®.
Not recommended to prescribe tricyclic antidepressants concurrently with moxonidine.
During treatment requires regular monitoring of blood pressure, Heart rate and ECG.
Moxonidine can be administered with thiazide diuretics, ACE inhibitors and calcium channel blockers slow.
Stop taking Moksogammy® should gradually.
Effects on ability to drive vehicles and management mechanisms
When using moxonidine possible drowsiness and dizziness, which should be considered when administering the drug to patients, whose activity is connected with the necessity of a high concentration of attention and psychomotor speed reatsky, incl. driving motor vehicles.
Overdose
Symptoms: headache, sedation, drowsiness, excessively pronounced decrease in blood pressure, dizziness, generalized weakness, bradycardia, dry mouth, vomiting, fatigue and pain in the stomach; It is also possible short-term increase in blood pressure, tachycardia, giperglikemiâ.
Treatment: As a specific antidote is administered idazoxan (imidazoline antagonist). Gastric lavage (immediately after receiving), administration of activated charcoal and laxatives. Symptomatic therapy.
In the case of reduction of blood pressure is recommended to restore the BCC by the introduction of liquid.
Bradycardia can be stopped by atropine.
Alpha-adrenoceptor antagonists can reduce or eliminate transient hypertension in overdose moxonidine.
Drug Interactions
The drug Moksogamma® can be administered in combination with thiazide diuretics and calcium channel blockers slow. In a joint application with these moxonidine and other antihypertensives mutual strengthening of action of moxonidine.
When moxonidine with hydrochlorothiazide, glibenclamide (gliʙuridom) or digoxin pharmacokinetic interaction is absent.
Tricyclic antidepressants may decrease the effectiveness of antihypertensive drugs of the central action.
Moksinidin moderately enhances cognitive decline in patients, taking lorazepam.
Moxonidine together with benzodiazepines may be accompanied by increased sedation past.
Moxonidine dampening effect on the central nervous system anxiolytics, barbiturates and ethanol.
When moxonidine together with moclobemide pharmacodynamic interaction is absent.
Beta-blockers increase bradycardia, the severity of the negative ino- and dromotropic action.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
List B. The drug should be stored out of reach of children, dry, protected from light, at a temperature no higher than 25 ° C. Shelf life – 2 year.