Moxonidine

Description

Moxonidine, also known as Physiotens, is a highly selective imidazoline receptor agonist-Ⅰ by excitement ventrolateral medulla nucleus (RVLM)-Ⅰ type imidazoline receptor in the peripheral sympathetic nerve activity decreased. This receptor subtype is found in both the rostral ventro-lateral pressor and ventromedial depressor areas of the medulla oblongata.
Moxonidine therefore causes a decrease in sympathetic nervous system activity and, therefore, a decrease in blood pressure.
It is a new type of antihypertensive drug, commonly used in the treatment of essential hypertension. Compared to the older central-acting antihypertensives, moxonidine binds with much greater affinity to the imidazoline I1-receptor than to the α2-receptor. In contrast, clonidine binds to both receptors with equal affinity.
It may have a role when thiazides, beta-blockers, ACE inhibitors and calcium channel blockers are not appropriate or have failed to control blood pressure.

Physical and Chemical Properties

ensity: 1.52g/cm3, boiling point:  364.7 °C at 760 mmHg, flash point: 174.3 °C, crystallization, melting point: 217-219 degrees Celsius.

Application

• By stimulating the central presynaptic alpha 2-receptor and onset, and its antihypertensive effect of ACE inhibitors, calcium antagonists nifedipine and captopril similar. Treatment of essential hypertension.
• The intervention of renal interstitial fibrosis can protect the kidney.

Preparation

5-amino-4,6-dichloro-2-methyl pyrimidine and 1-acetyl-2-imidazolin-2-one. The product, reacting with sodium methanol can produce moxonidine.

Precautions

• There may be dry mouth, fatigue and headache at the beginning of treatment, occasional dizziness, insomnia, and weakness in the legs and so on.
• Sick sinus syndrome, the sinus node and atrioventricular Ⅱ-Ⅲ degree block, resting bradycardia (50 beats/min), unstable angina, severe liver disease, progressive renal dysfunction, angioedema patients should not use it.

References

https://en.wikipedia.org/wiki/Moxonidine

Description

Moxonidine, which is structurally related to clonidine, is a new centrally acting antihypertensive that acts as a stronger agonist at imidazole receptors and a weaker agonist at α2-adrenergic receptors than clonidine. It is also reported to have less side effects and a much reduced potential to produce a rebound in blood pressure on withdrawal. Clinically, moxonidine appears to have comparable antihypertensive efficacy with the ACE inhibitors and calcium antagonists.

Chemical Properties

White Solid

Originator

Beiersdorf (Germany)

Uses

Antihypertensive;Imidazoline receptor agonist

Uses

Moxonidine is an antihypertensive agent.

Definition

ChEBI: Moxonidine is an organohalogen compound and a member of pyrimidines.

brand name

Cynt (Lilly); Nucynt (Lilly); Norcynt (Lilly);Physiotens.

Biological Activity

Mixed I 1 imidazoline receptor and α 2 -adrenergic agonist; displays 40-fold higher affinity for I 1 receptors versus α 2 -adrenoceptors. Centrally acting antihypertensive agent.

Clinical Use

Antihypertensive agent (centrally acting agonist at I1 receptor, imidazoline and alpha2 adrenoceptors)

Metabolism

10-20% metabolised, predominantly to 4,5-dehydromoxonidine and to an aminomethanamidine derivative both of which are much less active than moxonidine. Moxonidine and its metabolites are almost entirely eliminated via the kidney. More than 90% of the dose is eliminated in the first 24 hours via the kidney, while approximately 1% is eliminated in the faeces