Moxonidine

4-chloro- N- (4,5- dihydro- 1H -imidazol-2 -yl) -6-methoxy - 2- methyl-pyrimidin- 5-amine

• 75438-57-2 (free base)
• 75438-58-3 (hydrochloride)

C02AC05

• Antihypertensives
• Antisympathotonics

• Agonist at pre-and post-synaptic α2 -adrenoceptors
• Agonist to imidazoline receptors

• 217-219 ° C ( free base)
• 189 ° C (hydrochloride)

130 mg · kg -1 ( LD50, rat, oral)

Template: Infobox chemical / molecular formula search available

Moxonidine is a drug used for the treatment of hypertension (high blood pressure). He is an analogue of the well -hypertensive drug clonidine and is one of the imidazoline derivatives. Moxonidine was patented in 1980 by Beiersdorf AG and is available as a generic in the trade.

Pharmacology

Mechanism of Action

The active ingredient penetrates due to its lipophilicity quickly into the central nervous system (CNS ) in front, where it acts as an agonist at postsynaptic α2 -adrenoceptors in the nucleus tractus solitarius, a switching blood pressure regulation, whereby the sympathetic tone and thus the blood pressure is lowered. In addition, the peripheral presynaptic α2 -adrenoceptors are stimulated, leading to a decreased release of noradrenaline. The most powerful effect of the antihypertensive effect relating follows, by acting as an agonist at imidazoline receptor, including in the ventrolateral medulla oblongata, which is much more pronounced when moxonidine than with clonidine, and which in turn leads to an inhibition of the sympathetic activity.

Application

Moxonidine is mainly used for the treatment of essential arterial hypertension with no known cause, for which the substance is also permitted. It is also used as an antihypertensive agent for the relief of opiate withdrawal.

Pharmacokinetics

The drug is rapidly absorbed and quickly transported to the site of action in the central nervous system. The plasma half -life is approximately 2-3 hours and the subsequent elimination was renal ( via the kidneys ).

Side effects

Because of the reduction of the sympathetic tone may cause dry mouth, dizziness, hypotension, libido and impotence. By the double- effect on the α2 - receptors and imidazoline a retention of sodium ions, and hence a tendency for edema formation is possible.

At the beginning of treatment may lead to a sharp drop in blood pressure with dizziness and headache.

Abrupt discontinuation should be avoided at, because it can lead to a massive increase in blood pressure (blood pressure rebound) come.

Interactions

By agonism at α2 -adrenoceptors, the effects of neuroleptics, hypnotics and alcohol is enhanced.

Contraindications

Justified by the complex mechanism of action, there are numerous basic contraindications ( selection):

• Malignant arrhythmias
• NYHA functional class II -IV
• Unstable angina pectoris
• Angioedema
• Pregnancy and lactation

There are also a number of recommendations on where the drug due to lack of experience of therapy and a possible interaction potential should not be used (selection):

• Intermittent claudication ( peripheral arterial disease )
• Raynaud's Disease
• Parkinson's disease
• Epileptic disorders
• Glaucoma

Different strengths and dosage

Moxonidine is available in dosage strengths 0.2-0.3 and 0.4 mg available and is used by default with 0.2-0.4 mg per day, which is to ensure that the maximum single dose 0.4 mg and the total daily dose not exceed 0.6 mg.

Trade names

CYNT (D), Normohex (A), Physiotens (D, CH ), numerous generics (D, A)