MOXONIDINE

Possibly Marketed Outside US

Details

Stereochemistry	ACHIRAL
Molecular Formula	C9H12ClN5O
Molecular Weight	241.677
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COC1=C(NC2=NCCN2)C(Cl)=NC(C)=N1

InChI

InChIKey=WPNJAUFVNXKLIM-UHFFFAOYSA-N

InChI=1S/C9H12ClN5O/c1-5-13-7(10)6(8(14-5)16-2)15-9-11-3-4-12-9/h3-4H2,1-2H3,(H2,11,12,15)

HIDE SMILES / InChI

Molecular Formula	C9H12ClN5O
Molecular Weight	241.677
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://gp2u.com.au/static/pdf/P/PHYSIOTENS-PI.pdf | https://www.ncbi.nlm.nih.gov/pubmed/16597164

Moxonidine is a second-generation, centrally acting antihypertensive drug with a distinctive mode of action. Moxonidine activates I1-imidazoline receptors (I1-receptors). Imidazoline I1-receptor agonism represents a new mode of antihypertensive action to inhibit peripheral alpha-adrenergic tone by a central mechanism. Adrenaline, noradrenaline and renin levels are reduced, a finding consistent with central inhibition of sympathetic tone. Moxonidine acts centrally to reduce peripheral sympathetic activity, thus decreasing peripheral vascular resistance. In patients with mild to moderate hypertension, moxonidine reduces blood pressure (BP) as effectively as most first-line antihypertensives when used as monotherapy and is also an effective adjunctive therapy in combination with other antihypertensive agents. It improves the metabolic profile in patients with hypertension and diabetes mellitus or impaired glucose tolerance, is well tolerated, has a low potential for drug interactions and may be administered once daily in most patients. Moxonidine is a good option in the treatment of patients with mild to moderate hypertension, particularly as adjunctive therapy in patients with the metabolic syndrome.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Nischarin 7 Target ID: Q9Y2I1\|\|\|Q9UFW3 Gene ID: 11188.0 Gene Symbol: NISCH Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/8380858	Agonist 2752

Conditions

Condition	Modality	Highest Phase	Product
Hypertension 575 Sources: https://gp2u.com.au/static/pdf/P/PHYSIOTENS-PI.pdf	Primary	Phase IV 63	PHYSIOTENS Approved Use Physiotens is indicated for the treatment of hypertension.
Obesity 206 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15269705	Palliative	Phase IV 63	Unknown Approved Use Unknown
Metabolic syndrome 34 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15269705	Palliative	Phase IV 63	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
1.5 ng/mL REVIEW https://journals.lww.com/cardiovascularpharm/Abstract/1992/20004/Clinical_Pharmacokinetics_of_Moxonidine.8.aspx	0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered:	MOXONIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
3.97 ng/mL REVIEW https://journals.lww.com/cardiovascularpharm/Abstract/1992/20004/Clinical_Pharmacokinetics_of_Moxonidine.8.aspx	0.2 mg single, intravenous dose: 0.2 mg route of administration: Intravenous experiment type: SINGLE co-administered:	MOXONIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.29 ng/mL REVIEW https://journals.lww.com/cardiovascularpharm/Abstract/1992/20004/Clinical_Pharmacokinetics_of_Moxonidine.8.aspx	0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered:	MOXONIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.33 ng/mL REVIEW https://journals.lww.com/cardiovascularpharm/Abstract/1992/20004/Clinical_Pharmacokinetics_of_Moxonidine.8.aspx	0.2 mg 2 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered:	MOXONIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.04 ng/mL REVIEW https://journals.lww.com/cardiovascularpharm/Abstract/1992/20004/Clinical_Pharmacokinetics_of_Moxonidine.8.aspx	0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered:	MOXONIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.89 ng/mL REVIEW https://journals.lww.com/cardiovascularpharm/Abstract/1992/20004/Clinical_Pharmacokinetics_of_Moxonidine.8.aspx	0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered:	MOXONIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
2319 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1686975/	0.4 mg single, oral dose: 0.4 mg route of administration: Oral experiment type: SINGLE co-administered:	MOXONIDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
3.67 ng × h/mL REVIEW https://journals.lww.com/cardiovascularpharm/Abstract/1992/20004/Clinical_Pharmacokinetics_of_Moxonidine.8.aspx	0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered:	MOXONIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
4.2 ng × h/mL REVIEW https://journals.lww.com/cardiovascularpharm/Abstract/1992/20004/Clinical_Pharmacokinetics_of_Moxonidine.8.aspx	0.2 mg single, intravenous dose: 0.2 mg route of administration: Intravenous experiment type: SINGLE co-administered:	MOXONIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
4.18 ng × h/mL REVIEW https://journals.lww.com/cardiovascularpharm/Abstract/1992/20004/Clinical_Pharmacokinetics_of_Moxonidine.8.aspx	0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered:	MOXONIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
4.02 ng × h/mL REVIEW https://journals.lww.com/cardiovascularpharm/Abstract/1992/20004/Clinical_Pharmacokinetics_of_Moxonidine.8.aspx	0.2 mg 2 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered:	MOXONIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
3.45 ng × h/mL REVIEW https://journals.lww.com/cardiovascularpharm/Abstract/1992/20004/Clinical_Pharmacokinetics_of_Moxonidine.8.aspx	0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered:	MOXONIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3.23 ng × h/mL REVIEW https://journals.lww.com/cardiovascularpharm/Abstract/1992/20004/Clinical_Pharmacokinetics_of_Moxonidine.8.aspx	0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered:	MOXONIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
5107 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1686975/	0.4 mg single, oral dose: 0.4 mg route of administration: Oral experiment type: SINGLE co-administered:	MOXONIDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
1.98 h REVIEW https://journals.lww.com/cardiovascularpharm/Abstract/1992/20004/Clinical_Pharmacokinetics_of_Moxonidine.8.aspx	0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered:	MOXONIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.18 h REVIEW https://journals.lww.com/cardiovascularpharm/Abstract/1992/20004/Clinical_Pharmacokinetics_of_Moxonidine.8.aspx	0.2 mg single, intravenous dose: 0.2 mg route of administration: Intravenous experiment type: SINGLE co-administered:	MOXONIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.12 h REVIEW https://journals.lww.com/cardiovascularpharm/Abstract/1992/20004/Clinical_Pharmacokinetics_of_Moxonidine.8.aspx	0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered:	MOXONIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.97 h REVIEW https://journals.lww.com/cardiovascularpharm/Abstract/1992/20004/Clinical_Pharmacokinetics_of_Moxonidine.8.aspx	0.2 mg 2 times / day multiple, oral dose: 0.2 mg route of administration: Oral experiment type: MULTIPLE co-administered:	MOXONIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.85 h REVIEW https://journals.lww.com/cardiovascularpharm/Abstract/1992/20004/Clinical_Pharmacokinetics_of_Moxonidine.8.aspx	0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered:	MOXONIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.1 h REVIEW https://journals.lww.com/cardiovascularpharm/Abstract/1992/20004/Clinical_Pharmacokinetics_of_Moxonidine.8.aspx	0.2 mg single, oral dose: 0.2 mg route of administration: Oral experiment type: SINGLE co-administered:	MOXONIDINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
1.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1686975/	0.4 mg single, oral dose: 0.4 mg route of administration: Oral experiment type: SINGLE co-administered:	MOXONIDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
2.5 h REVIEW https://pubmed.ncbi.nlm.nih.gov/8872298/	0.4 mg 1 times / day unknown, oral dose: 0.4 mg route of administration: Oral experiment type: UNKNOWN co-administered:	MOXONIDINE unknown	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
1 mg 2 times / day multiple, oral Highest studied dose Dose: 1 mg, 2 times / day Route: oral Route: multiple Dose: 1 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/3316304/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/3316304/	Disc. AE: Vertigo... Other AEs: Dry mouth, Tiredness... AEs leading to discontinuation/dose reduction: Vertigo (0.8%) Other AEs: Dry mouth (19.7%) Tiredness (13.1%) Headache (0.8%) Weakness of limbs (0.8%) Orthostatic dysregulation (0.8%) Edema (0.8%) Flushed face (0.8%) Nervousness (1.6%) Diarrhea (0.8%) Sources: https://pubmed.ncbi.nlm.nih.gov/3316304/

AEs

AE	Significance	Dose	Population
Diarrhea	0.8%	1 mg 2 times / day multiple, oral Highest studied dose Dose: 1 mg, 2 times / day Route: oral Route: multiple Dose: 1 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/3316304/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/3316304/
Edema	0.8%	1 mg 2 times / day multiple, oral Highest studied dose Dose: 1 mg, 2 times / day Route: oral Route: multiple Dose: 1 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/3316304/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/3316304/
Flushed face	0.8%	1 mg 2 times / day multiple, oral Highest studied dose Dose: 1 mg, 2 times / day Route: oral Route: multiple Dose: 1 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/3316304/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/3316304/
Headache	0.8%	1 mg 2 times / day multiple, oral Highest studied dose Dose: 1 mg, 2 times / day Route: oral Route: multiple Dose: 1 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/3316304/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/3316304/
Orthostatic dysregulation	0.8%	1 mg 2 times / day multiple, oral Highest studied dose Dose: 1 mg, 2 times / day Route: oral Route: multiple Dose: 1 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/3316304/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/3316304/
Weakness of limbs	0.8%	1 mg 2 times / day multiple, oral Highest studied dose Dose: 1 mg, 2 times / day Route: oral Route: multiple Dose: 1 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/3316304/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/3316304/
Vertigo	0.8% Disc. AE	1 mg 2 times / day multiple, oral Highest studied dose Dose: 1 mg, 2 times / day Route: oral Route: multiple Dose: 1 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/3316304/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/3316304/
Nervousness	1.6%	1 mg 2 times / day multiple, oral Highest studied dose Dose: 1 mg, 2 times / day Route: oral Route: multiple Dose: 1 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/3316304/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/3316304/
Tiredness	13.1%	1 mg 2 times / day multiple, oral Highest studied dose Dose: 1 mg, 2 times / day Route: oral Route: multiple Dose: 1 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/3316304/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/3316304/
Dry mouth	19.7%	1 mg 2 times / day multiple, oral Highest studied dose Dose: 1 mg, 2 times / day Route: oral Route: multiple Dose: 1 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/3316304/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/3316304/

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 2252 inducer 1087	inhibitor 2438	inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2E1 1060 CYP2C19 2057 CYP2A6 879 CYP19A1 429 CYP1A2 2153	P-gp 2052

Drug as perpetrator

Target	Modality	Activity
CYP19A1 430	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/4810#section=BioAssay-Results Page: 357.0	inconclusive
CYP2C19 2141	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNjIyIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDE5MjM2In19	no [IC50 39.8107 uM]
CYP1A2 2333	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzMzU2IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDE5MjM2In19	no [IC50 >10 uM]
CYP2A6 911	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw1MjgyIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDE5MjM2In19	no [IC50 >10 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzMzk3IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDE5MjM2In19	no [IC50 >10 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwyODkiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMMTkyMzYifX0=	no [IC50 >10 uM]
CYP2E1 1146	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw1MjgxIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDE5MjM2In19	no [IC50 >10 uM]
CYP3A4 2633	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNDAiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMMTkyMzYifX0=	no [IC50 >10 uM]
CYP3A4 2633	inducer 1966 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/4810#section=BioAssay-Results Page: 412.0	no

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
P-gp 2052	substrate 4014 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/4810#section=BioAssay-Results Page: 383 \| 391	no

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwyNDAiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMMTkyMzYifX0=

PubMed

Title	Date	PubMed
Imidazoline receptors but not alpha 2-adrenoceptors are regulated in spontaneously hypertensive rat heart by chronic moxonidine treatment.	2004-08	15075383
Augmentation of moxonidine-induced increase in ANP release by atrial hypertrophy.	2004-07	14975931
The I1-imidazoline agonist moxonidine decreases sympathetic tone under physical and mental stress.	2004-05	15089806
Effect of i1 imidazoline receptor agonist, moxonidine, in nitric oxide-deficient hypertension in pregnant rats.	2004-05	15071362
Selective imidazoline agonist moxonidine plus the ACE inhibitor ramipril in hypertensive patients with impaired insulin sensitivity: partners in a successful MARRIAGE?	2004-03	15025845
Pharmacological therapy can increase capillary density in post-infarction remodeled rat hearts.	2004-02-15	14962492
The effects of imidazoline agents on the aggregation of human platelets.	2004-02	15005880
Moxonidine, an antihypertensive agent, is permissive to alpha1-adrenergic receptor pathway in the rat-tail artery.	2004-02	14716222
Elevated sympathetic activity may promote insulin resistance syndrome by activating alpha-1 adrenergic receptors on adipocytes.	2004	15082116
Moxonidine and central alpha2 adrenergic receptors in sodium intake.	2003-12-12	14642844
Moxonidine, a mixed alpha(2)-adrenergic and imidazoline receptor agonist, identifies a novel adrenergic target for spinal analgesia.	2003-12	15028616
Apparent absence of direct renal effect of imidazoline receptor agonists.	2003-12	15028602
Normalization of up-regulated cardiac imidazoline I(1)-receptors and natriuretic peptides by chronic treatment with moxonidine in spontaneously hypertensive rats.	2003-12	15028599
Norepinephrine release is reduced by I(1)-receptors in addition to alpha(2)-adrenoceptors.	2003-12	15028598
Moxonidine displays a presynaptic alpha-2-adrenoceptor-dependent synergistic sympathoinhibitory action at imidazoline-1 receptors.	2003-12	15028597
Involvement of forebrain imidazoline and alpha(2)-adrenergic receptors in the antidipsogenic response to moxonidine.	2003-12	15028596
The role of I(1)-imidazoline receptors and alpha(2)-adrenergic receptors in the modulation of glucose and lipid metabolism in the SHROB model of metabolic syndrome X.	2003-12	15028595
Cardiac effects of moxonidine in spontaneously hypertensive obese rats.	2003-12	15028594
Identification and pharmacological characterization of a specific agmatine transport system in human tumor cell lines.	2003-12	15028572
Electrophysiological responses to imidazoline/alpha2-receptor agonists in rabbit sinoatrial node pacemaker cells.	2003-12	14653947
Contrasting metabolic effects of antihypertensive agents.	2003-12	14557373
Central moxonidine on salivary gland blood flow and cardiovascular responses to pilocarpine.	2003-10-17	14499959
Adverse mortality effect of central sympathetic inhibition with sustained-release moxonidine in patients with heart failure (MOXCON).	2003-10	14607206
Moxonidine treatment of hypertensive patients with advanced renal failure.	2003-09	12923404
Antihypertensive efficacy of moxonidine in primary care: a 'real-life' study.	2003-08-16	12918886
The I(1)-imidazoline receptor in PC12 pheochromocytoma cells reverses NGF-induced ERK activation and induces MKP-2 phosphatase.	2003-08-01	12865160
Effects of moxonidine and metoprolol in penile circulation in hypertensive men with erectile dysfunction: results of a pilot study.	2003-08	12934058
The role of I(1)-imidazoline and alpha(2)-adrenergic receptors in the modulation of glucose metabolism in the spontaneously hypertensive obese rat model of metabolic syndrome X.	2003-08	12756274
[Study examines prescriptions for hypertension. Physicians adhering to guidelines very well].	2003-06-19	12891855
Experimental approach to differentiation of the effects mediated by imidazole receptors and alpha2-adrenoceptors on platelets.	2003-06	12937676
Central nervous system effects of moxonidine experimental sustained release formulation in patients with mild to moderate essential hypertension.	2003-06	12814444
[Ambulatory monitoring of blood pressure in regular dialysis therapy].	2003-04	12793047
Dual effect of agmatine in the bisected rat vas deferens.	2003-03	12724044
Modification of noradrenaline release in pithed spontaneously hypertensive rats by I1-binding sites in addition to alpha2-adrenoceptors.	2003-03	12604683
Metabolism and disposition of the antihypertensive agent moxonidine in humans.	2003-03	12584161
Non-adrenergic exploratory behavior induced by moxonidine at mildly hypotensive doses.	2003-02-21	12573508
Central alpha(2) adrenergic receptors and cholinergic-induced salivation in rats.	2003-01-30	12507689
[Moxonidine is advantageous for hypertensive type 2 diabetic patients. Therapy of hypertension also lowers HbA1c].	2003-01-16	12638449
Importance of imidazoline-preferring receptors in the cardiovascular actions of chronically administered moxonidine, rilmenidine and clonidine in conscious rabbits.	2003-01	12544449
[Effect of imidazoline receptor agonist moxonidine on the state of microcirculation and renal function in patients with hypertension and diabetes mellitus type 2].	2003	14682297
[Current views on migraine and anti-migraine preparations].	2003	14598505
[The use of moxonidine in patients with essential hypertension combined with metabolic syndrome].	2003	12913980
Plasma catecholamines and chronic congestive heart failure.	2002-12-17	12485972
Pharmacological evidence of a role for prejunctional imidazoline (I(1)) receptors in ocular function.	2002-11	12658545
[Obesity and hypertension. A dangerous liaison].	2002-10-24	12534023
[Clinical assessment of prolonged therapy of patients with hypertension and diabetes with imidazoline receptor agonist moxonidine].	2002	12494208
[Moxomidine effectiveness in women with arterial hypertension associated with metabolic syndrome in initially high heart rate].	2002	12494035
[Pathogenetic role of moxonidine in the treatment of hypertension in postmenopausal women].	2002	12494033
[Comparison of the antihypertensive efficacy of and tolerance to 2 imidazoline receptor agonists: moxonidine and rilmenidine in monotherapy].	2001-04	12555509
Centrally acting imidazoline I1-receptor agonists: do they have a place in the management of hypertension?	2001	14728014

Patents

Sample Use Guides

In Vivo Use Guide

Treatment should be started with 0.2 mg Physiotens in the morning. The dose may be titrated after two weeks to 0.4 mg given as one dose or as divided doses (morning and evening) until a satisfactory response is achieved. If the response is still unsatisfactory after a further 2 weeks treatment, the dosage can be increased up to a maximum of 0.6 mg in divided doses (morning and evening). A single daily dose of 0.4 mg and a divided daily dose of 0.6 mg of Physiotens should not be exceeded. Physiotens may be taken with or without food.

Route of Administration: Oral

In Vitro Use Guide

It was investigate the effects of moxonidine on neurons in the rostral ventrolateral medulla (RVLM) with electrophysiological properties similar to premotor sympathetic neurons in vivo. Moxonidine (2-10 microM) was applied to the perfusate on 4 irregularly firing neurons, and 2 regularly firing neurons. Moxonidine (2 microM) produced only minor depolarization in 2 of these neurons. However, on 4 tested neurons, moxonidine (10 microM) elicited a profound inhibitory effect with hyperpolarization (near -20 mV); these neurons practically ceased firing. These changes were partially reversible. The results would indicate that neurons in the RVLM, recorded in vitro and with similar electrophysiological characteristics to a group of neurons previously identified in vivo in the same bulbar region as barosensitive premotor sympathetic neurons, can be modulated by imidazoline-derivative adrenergic agonists. These results could help to understand the hypotensive effects of moxonidine.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:08:24 GMT 2025` Edited by `admin` on `Mon Mar 31 18:08:24 GMT 2025`
Record UNII	CC6X0L40GW
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

MOXONIDINE

Official Name

English

CYNT

Preferred Name

English

MOXONIDINE [MART.]

Common Name

English

BE5895

Code

English

BE-5895

Code

English

LY326869

Code

English

5-PYRIMIDINAMINE, 4-CHLORO-N-(4,5-DIHYDRO-1H-IMIDAZOL-2-YL)-6-METHOXY-2-METHYL-

Systematic Name

English

LY-326869

Code

English

Moxonidine [WHO-DD]

Common Name

English

BDF-5896

Code

English

4-Chloro-5-(2-imidazolidinyldeneamino)-6-methoxy-2-methylpyrimidine

Common Name

English

moxonidine [INN]

Common Name

English

MOXONIDINE [USAN]

Common Name

English

MOXONIDINE [MI]

Common Name

English

MOXONIDINE [EP MONOGRAPH]

Common Name

English

BDF5896

Code

English

Classification Tree Code System Code

WHO-ATC

C02LC05