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| Pronunciation | /mɒkˈsɒnɪdiːn/ |
| Trade names | Physiotens, Moxon |
| AHFS/Drugs.com | International Drug Names |
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| Routes of administration | Oral (tablets) |
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| Pharmacokinetic data | |
| Bioavailability | 88% (Tmax = 1 hour) |
| Protein binding | 7.2–10%[1][2] |
| Metabolism | Liver (10–20%)[2] |
| Metabolites | Dehydrogenated moxonidine (major), hydroxymethyl-moxonidine, hydroxy-moxonidine, dihydroxy-moxonidine[3] |
| Eliminationhalf-life | ~2.2–2.8 hours |
| Excretion | Renal (90%),[4] feces (~1%)[2] |
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| ECHA InfoCard | 100.158.061 |
| Chemical and physical data | |
| Formula | C9H12ClN5O |
| Molar mass | 241.68 g·mol−1 |
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Moxonidine (INN) is a new-generation alpha-2/imidazoline receptor agonistantihypertensive drug licensed for the treatment of mild to moderateessential hypertension.[5][6] It may have a role whenthiazides,beta-blockers,ACE inhibitors, andcalcium channel blockers are not appropriate or have failed to control blood pressure. In addition, it demonstrates favourable effects on parameters of theinsulin resistance syndrome, apparently independent of blood pressure reduction. It is also agrowth hormone releaser.[7] It is manufactured bySolvay Pharmaceuticals (acquired byAbbott in 2009) under the brand namePhysiotens and Moxon.
Moxonidine is a selectiveagonist at theimidazoline receptor subtype 1 (I1).[5] This receptor subtype is found in both the rostral ventro-lateral pressor and ventromedial depressor areas of themedulla oblongata. Moxonidine therefore causes a decrease insympathetic nervous system activity and, therefore, a decrease inblood pressure.
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 near equal affinity. Moxonidine has an affinity for I1 that is 33 times greater than α2, compared to clonidine which is only four times greater.[8]
In addition, moxonidine may also promotesodium excretion, improve insulin resistance andglucose tolerance and protect against hypertensive target organ damage, such askidney disease andcardiachypertrophy.
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In all animal models of insulin resistance, moxonidine had striking effects on the development of insulin resistance, hyperinsulinaemia and impaired glucose homeostasis. Given the importance of insulin resistance as a risk factor for cardiovascular disease, it is of considerable relevance that it has been shown to improve insulin sensitivity.
It is contraindicated if there has been a past history ofangioedema; heart conduction disorders (e.g.sick sinus syndrome, second- or third-degreeheart block);bradycardia; severeheart failure orcoronary artery disease. Also:Raynaud's syndrome,intermittent claudication,epilepsy, depression,Parkinson's disease,glaucoma. Use in pregnancy is discouraged. Moxonidine passes into breast milk.
Moxonidine should be avoided in patients with moderate to severe renal impairment. Abrupt discontinuation of the drug should also be avoided. If concomitant treatment with a beta blocker has to be stopped, the beta blocker should be discontinued first, then moxonidine after a few days. Alcohol may potentiate the hypotensive effects of Moxonidine.[medical citation needed]
Excess mortality has been seen in patients with symptomaticheart failure in the MOXCON study.[9] However, the MOXCON trial utilised a very high dose of 3.0 mg daily which is well above the normal dose of 0.2–0.6 mg daily.
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Noteworthyside effects include dry mouth, headache, fatigue, dizziness, intermittent facial oedema, nausea, sleep disturbances (rarely sedation),asthenia, vasodilatation, and rarely, skin reactions.
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Routine toxicology studies have provided no evidence that moxonidine has any teratogenic, mutagenic or carcinogenic potential. No evidence has been found of serious adverse effects on organs or organ systems, and the drug has not been shown to have deleterious effects on perinatal or postnatal growth and development.
Concomitant administration of moxonidine and a thiazide diuretic such ashydrochlorothiazide gave a synergistic antihypertensive effect.[10]
Media related toMoxonidine at Wikimedia Commons