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| | Moxonidine Chemical Properties |
| Melting point | 217-219° (dec) | | Boiling point | 364.7±52.0 °C(Predicted) | | density | 1.52±0.1 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | Very slightly soluble in water, sparingly soluble in methanol, slightly soluble in methylene chloride, very slightly soluble in acetonitrile. | | form | neat | | pka | 7.11±0.10(Predicted) | | color | White to Almost white | | Water Solubility | 800.3mg/L(temperature not stated) | | Merck | 14,6293 | | InChIKey | WPNJAUFVNXKLIM-UHFFFAOYSA-N | | CAS DataBase Reference | 75438-57-2(CAS DataBase Reference) |
| RIDADR | UN 2811 6.1/PG III | | WGK Germany | 3 | | RTECS | UV6260290 | | HS Code | 2933.99.5300 | | HazardClass | 6.1 | | PackingGroup | III |
| | Moxonidine Usage And Synthesis |
| 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 | Moxonidine is an antihypertensive agent. | | Uses | Antihypertensive;Imidazoline receptor agonist | | 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 |
| | Moxonidine Preparation Products And Raw materials |
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