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.
- 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.
5-amino-4,6-dichloro-2-methyl pyrimidine and 1-acetyl-2-imidazolin-2-one. The product, reacting with sodium methanol can produce moxonidine.
- 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.
https://en.wikipedia.org/wiki/Moxonidine
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.
Antihypertensive;Imidazoline receptor agonist
Moxonidine is an antihypertensive agent.
ChEBI: Moxonidine is an organohalogen compound and a member of pyrimidines.
Cynt (Lilly); Nucynt (Lilly); Norcynt (Lilly);Physiotens.
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.
Antihypertensive agent (centrally acting agonist at I1
receptor, imidazoline and alpha2
adrenoceptors)
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
