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Moxonidine | CAS No: 75438-57-2 | GMP-certified suppliers
A medication that treats mild to moderate essential hypertension with effective blood pressure reduction and potential benefits for patients with insulin resistance syndrome.
Therapeutic categories
Primary indications
- For the treatment of mild to moderate essential or primary hypertension
- Effective as most first-line antihypertensives when used as monotherapy
Product Snapshot
- Moxonidine is an oral small molecule formulated as coated and film-coated tablets
- Its primary therapeutic use is for the treatment of mild to moderate essential or primary hypertension
- Moxonidine has approved and investigational status in key regulatory markets
Clinical Overview
Pharmacologically, moxonidine belongs to the halopyrimidine class, characterized by a halogenated pyrimidine ring structure. Its primary site of action is within the central nervous system, specifically targeting receptors in the rostral ventrolateral medulla (RSV). Moxonidine exerts its antihypertensive effect mainly through selective binding to imidazoline receptor subtype 1 (I1), with comparatively low affinity for central alpha-2 adrenergic receptors. This receptor profile leads to a reduction in sympathetic nervous system outflow, decreasing systemic vascular resistance and subsequently lowering arterial blood pressure. The selective receptor engagement distinguishes moxonidine from other centrally acting agents that typically cause sedation and dry mouth via stronger alpha-2 adrenergic receptor affinity.
Although detailed human absorption, distribution, metabolism, and excretion (ADME) parameters are not fully disclosed here, moxonidine’s clinical use reflects an acceptable pharmacokinetic and safety profile. Safety considerations revolve around its central sympatholytic activity; common adverse effects include dry mouth and dizziness, with sedation being less frequent than with older agents due to receptor selectivity. Clinical monitoring of blood pressure and renal function is advised during therapy.
Moxonidine is marketed under various brand names internationally and is classified under several pharmacotherapeutic categories including adrenergic agonists, antiadrenergic agents, and imidazoline receptor agonists. It is approved for antihypertensive use in multiple regulatory jurisdictions.
From an API sourcing perspective, quality considerations include rigorous adherence to specifications for purity, stereochemistry, and halopyrimidine integrity to ensure consistent pharmacological activity and safety. Suppliers should demonstrate compliance with Good Manufacturing Practices (GMP) and provide comprehensive analytical documentation to support regulatory submissions.
Identification & chemistry
| Generic name | Moxonidine |
|---|---|
| Molecule type | Small molecule |
| CAS | 75438-57-2 |
| UNII | CC6X0L40GW |
| DrugBank ID | DB09242 |
Pharmacology
| Summary | Moxonidine is an antihypertensive agent that acts centrally by selectively binding imidazoline I1 receptors and, to a lesser extent, alpha-2 adrenergic receptors in the rostral ventrolateral medulla. This interaction suppresses sympathetic nervous system activity, leading to reduced systemic vascular resistance and lowered arterial blood pressure. Compared to other centrally acting antihypertensives, moxonidine exhibits low affinity for alpha-2-adrenergic receptors, which may influence its side effect profile. |
|---|---|
| Mechanism of action | Stimulation of central alpha 2-adrenergic receptors is associated with sympathoadrenal suppression and subsequent reduction of blood pressure. As this class was further explored it was discovered that sympathoadrenal activity can also be suppressed by a second pathway with a newly discovered drug target specific to imidazolines . Specifically, moxonidine binds the imidazoline receptor subtype 1 (I1) and to a lesser extent αlpha-2-adrenoreceptors in the RSV causing a reduction of sympathetic activity, reducing systemic vascular resistance and thus arterial blood pressure. Moreover, since alpha-2-adrenergic receptors are considered the primary molecular target that facilitates the most common side effects of sedation and dry mouth that are elicited by most centrally acting antihypertensives, moxonidine differs from these other centrally acting antihypertensives by demonstrating only low affinity for central alpha-2-adrenoceptors compared to the aforementioned I1-imidazoline receptors. |
| Pharmacodynamics | Antihypertensive agent whose site of action is the Central Nervous System (CNS), specifically involving interactions with I1- imidazoline and alpha-2-adrenergic rececptors within the rostral ventrolateral medulla (RSV). |
Targets
| Target | Organism | Actions |
|---|---|---|
| Alpha-2A adrenergic receptor | Humans | agonist |
| Nischarin | Humans | agonist |
ADME / PK
| Absorption | 90% of an oral dose is absorbed with negligible interference from food intake or first pass metabolism, resulting in a high bioavailability of 88%. |
|---|---|
| Half-life | Plasma elimination half life is 2.2 - 2.3 hours while renal elimination half life is 2.6-2.8 hours. |
| Protein binding | About 10% of moxonidine is bound to plasma proteins. |
| Metabolism | Biotransformation is unimportant with 10-20% of moxonidine undergoing oxidation reactions to the primary 4,5-dehydromoxonidine metabolite and a guanidine derivative by opening of the imidazoline ring. The antihypertensive effects of these 4,5-dehydromoxonidine and guanidine metabolites are only 1/10 and 1/100 the effect of moxonidine. Oxidation on either the methyl group (pyrimidine ring) or on the imidazole ring of moxonidine results in the formation of the hydroxylmethyl moxonidine metabolite or the hydroxy moxonidine metabolite . The hydroxy moxonidine metabolite can be further oxidized to the dihydroxy metabolite or it can lose water to form the dehydrogenated moxonidine metabolite, which itself can be further oxidized to form an N-oxide . Aside from these Phase I metabolites, Phase II metabolism of moxonidine is also evident with the presence of a cysteine conjugate metabolite minus chlorine . Nevertheless, the identification of the hydroxy moxonidine metabolite with a high level of dehydrogenated moxonidine metabolite in human urine samples suggests that dehydrogenation from the hydroxy metabolite to the dehydrogenated moxonidine metabolite represents the primary metabolic pathway in humans . The cytochromes P450 responsible for the metabolism of moxonidine in humans have not yet been determined . Ultimately, the parent moxonidine compound was observed to be the most abundant component in different biological matrices of urinary excretion samples, verifying that metabolism only plays a modest role in the clearance of moxonidine in humans . |
| Route of elimination | Elimination is nearly entirely via the kidneys with a majority (50 -75%) of overall moxonidine being eliminated unchanged through renal excretion. Ultimately, more than 90% of a dose is eliminated by way of the kidneys within the first 24 hours after administration, with only approximately 1% being eliminiated via faeces. |
| Volume of distribution | 1.8±0.4L/kg. |
| Clearance | Administered twice daily due to short half life. However, lower dosage adjustments and close monitoring is necessary in elderly and renal impairment patients due to reduced clearance. In particular, the exposure AUC can increase by about 50% following a single dose and at steady state in elderly patients and moderately impaired renal function with GFR between 30-60 mL/min can cause AUC increases by 85% and decreases in clearence to 52 %. |
Formulation & handling
- Moxonidine is a small molecule suitable for oral administration in coated or film-coated tablet formulations.
- Low water solubility (0.114 g/L) suggests consideration of solubilization techniques to optimize bioavailability.
- Its halopyrimidine structure indicates potential chemical stability, but appropriate storage conditions should be maintained to preserve integrity.
Regulatory status
Safety
| Toxicity | * Contraindicated due to known hypersensitivity to an ingredient (Physiotens tablets contain lactose), heart failure, severe renal impairment, < 16 years old, >75 years old, bradycardia, severe bradyarrhythmia, sick sinus syndrome, second or third degree atrioventricular block, malignant arrhythmias. * Used with caution in patients with history of severe coronary artery disease (CAD), unstable angina, angioneurotic edema. * Pregnancy Category B3:Avoid use during pregnancy (inadequate data in pregnant woman) and lactation (maternal blood stream transfer to breast milk shown) unless benefit clearly justifies risk. * Lack of specific therapeutic experience in cases of intermittent claudication, Raynaud's disease, Parkinson's disease, epileptic disorders, gluacoma, and depression suggest moxonidine should not be used in such instances. * Carcinogenicity and genotoxicity does not appear significant. * Concurrent administration of other hypotensives or sedative and hypnotics can enhance the hypotensive effect and intensify sedation respectively. * Avoid concurrent Tricyclic Antidepressant (TCA) use to avoid reduction of monoxidine efficacy. * Generally well tolerated with dry mouth and headache the most common adverse effects * Symptoms of overdose correlate with pharmacodynamic properties:hypotension, sedation, orthostatic dysregulation, bradycardia, dry mouth with no specific counter-treatment known. |
|---|
- Contains lactose
- Contraindicated in individuals with known hypersensitivity to lactose or specific cardiovascular conditions including severe bradyarrhythmias and advanced atrioventricular block
- Use caution with concurrent administration of other hypotensive agents or sedatives due to potential for enhanced hypotensive and sedative effects
Moxonidine is a type of Antihypertensive agents
Antihypertensive agents are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) used to treat high blood pressure, also known as hypertension. These medications are designed to lower blood pressure and reduce the risk of associated cardiovascular complications.
Antihypertensive agents function by targeting various mechanisms involved in blood pressure regulation. Some common classes of antihypertensive agents include angiotensin-converting enzyme (ACE) inhibitors, angiotensin II receptor blockers (ARBs), beta-blockers, calcium channel blockers (CCBs), and diuretics.
ACE inhibitors work by inhibiting the enzyme responsible for converting angiotensin I to angiotensin II, a hormone that constricts blood vessels. ARBs, on the other hand, block the receptors to which angiotensin II binds, thereby preventing its vasoconstrictive effects.
Beta-blockers reduce blood pressure by blocking the effects of adrenaline and noradrenaline, which are responsible for increasing heart rate and constricting blood vessels. CCBs inhibit calcium from entering the smooth muscles of blood vessels, resulting in relaxation and vasodilation. Diuretics promote the elimination of excess fluid and sodium from the body, reducing blood volume and thereby lowering blood pressure.
Antihypertensive agents are typically prescribed based on the individual patient's condition and specific needs. They can be used alone or in combination to achieve optimal blood pressure control. It is important to note that antihypertensive agents should be taken regularly as prescribed by a healthcare professional and may require periodic monitoring to ensure their effectiveness and manage any potential side effects.
In summary, antihypertensive agents play a vital role in the management of hypertension by targeting various mechanisms involved in blood pressure regulation. These medications offer significant benefits in reducing the risk of cardiovascular complications associated with high blood pressure.
Moxonidine API manufacturers & distributors
Compare qualified Moxonidine API suppliers worldwide. We currently have 6 companies offering Moxonidine API, with manufacturing taking place in 4 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Arevipharma | Producer | Germany | Unknown | CEP, CoA, FDA | 25 products |
| Arshine Pharmaceutical Co... | Distributor | China | China | BSE/TSE, CEP, CoA, FDA, GMP, MSDS, USDMF | 176 products |
| Boehringer Ingelheim | Producer | Germany | Unknown | CEP, CoA, FDA, GMP | 35 products |
| Farmak | Producer | Czech Republic | Czech Republic | CEP, CoA, FDA, GMP | 19 products |
| Kinsy | Producer | Spain | Spain | CEP, CoA, GMP | 9 products |
| Nantong Jinghua | Producer | China | China | CoA, USDMF | 12 products |
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