Moxonidine
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Non-proprietary name | Moxonidine | |||||||||||||||||||||
other names |
4-chloro- N - (4,5-dihydro-1 H -imidazol-2-yl) -6-methoxy-2-methylpyrimidine-5-amine |
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Molecular formula | C 9 H 12 ClN 5 O | |||||||||||||||||||||
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Molar mass | 241.68 g · mol -1 | |||||||||||||||||||||
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As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . |
Moxonidine is a medicine used to treat essential hypertension ( high blood pressure ). It is an analogue of the blood pressure lowering agent clonidine and is one of the imidazoline derivatives . The patent granted to Beiersdorf AG in 1980 has expired and moxonidine is now available as a generic drug .
pharmacology
Mechanism of action
The active ingredient penetrates due to its lipophilicity fast in the central nervous system (CNS) before and acts as an agonist at the postsynaptic α 2 -adrenoceptors in the solitary tract nucleus , a switching of blood pressure regulation, whereby the sympathetic tone and thus the blood pressure is reduced. In addition, the peripheral presynaptic α 2 -adrenoceptors are stimulated, which leads to a reduced release of noradrenaline . The strongest effect, concerning the antihypertensive effect, follows from the effect as an agonist on the imidazoline receptor , u. a. in the ventrolateral medulla oblongata , which is much more pronounced in moxonidine than in clonidine, and which in turn inhibits sympathetic activity.
application
Moxonidine is mainly used to treat essential arterial hypertension without a known cause, for which the substance is also approved. It is also used as an antihypertensive agent to relieve the symptoms of opiate withdrawal .
Pharmacokinetics
The active ingredient is quickly absorbed and quickly transported to the site of action in the central nervous system. The plasma half-life is approx. 2-3 hours and the subsequent elimination takes place renally (via the kidneys).
Side effects
The decrease in sympathetic tone can lead to dry mouth , drowsiness, hypotension , libido and erectile dysfunction. The double effect on the α 2 - and imidazoline receptors is a retention of sodium - ions and thus a tendency for edema formation possible.
At the beginning of treatment there may be a sharp drop in blood pressure with dizziness and headache.
Sudden discontinuation must be avoided at all costs, as this can lead to a massive increase in blood pressure (blood pressure rebound ).
Interactions
The agonism of α 2 -adrenoceptors increases the effect of neuroleptics , hypnotics and alcohol .
Contraindications
Due to the complex mechanism of action, there are numerous basic contraindications (selection):
- malignant arrhythmias
- Heart failure NYHA II-IV
- unstable angina pectoris
- Angioedema
- Pregnancy and breastfeeding
There are also a number of recommendations where the drug should not be used due to a lack of therapeutic experience and a possible potential for interaction (selection):
- Intermittent claudication (peripheral arterial disease)
- Raynaud's disease
- Parkinson's disease
- epileptic diseases
- glaucoma
Potency and dosage
Moxonidine is available in strengths of 0.2–0.3 and 0.4 mg and is used as standard at 0.2–0.4 mg per day, whereby it must be ensured that the maximum single dose is 0.4 mg and the total daily dose does not exceed 0.6 mg.
Trade names
Cynt (D), Normohex (A), Physiotens (D, CH), numerous generics (D, A)
Individual evidence
- ↑ a b c d e f Mutschler, Geisslinger, Kroemer, Ruth, Schäfer-Korting: Mutschler drug effects: textbook of pharmacology and toxicology , Wissenschaftliche Verlagsges. 9th edition, 2008, ISBN 3-8047-1952-X .
- ↑ a b The Merck Index . An Encyclopaedia of Chemicals, Drugs and Biologicals. 14th edition, 2006, pp. 1087-1088, ISBN 978-0-911910-00-1 .
- ↑ a b Moxonidine ( Memento from October 31, 2016 in the Internet Archive )
- ↑ Data sheet MOXONIDINE CRS (PDF) at EDQM , accessed on July 28, 2008.
- ↑ a b c d e ABDA database (as of July 28, 2008).