Moxonidine


Concise Prescribing Info
Indications/Uses
HTN.
Dosage/Direction for Use
Adult : PO Initial: 200 mcg once daily, up to 400 mcg/day in 1-2 divided doses if needed after 3 wk. May further increase to max of 600 mcg/day in 2 divided doses after another 3 wk (max 400 mcg/single dose).
Dosage Details
Oral
Hypertension
Adult: Initially, 200 mcg once daily in the morning, increase if necessary after 3 wk to 400 mcg daily as single or in 2 divided doses. If necessary, after a further 3 wk, increase to a max of 600 mcg daily in 2 divided doses (max 400 mcg per single dose).
Renal Impairment
Severe (GFR <30 mL/min): Contraindicated. Moderate (GFR 30-60 mL/min): Max: 400 mcg daily (max 200 mcg per single dose).
Administration
May be taken with or without food.
Contraindications
Sick sinus syndrome or sino-atrial block, 2nd or 3rd degree AV block, bradycardia (<50 beats/min at rest), severe heart failure, severe ischaemic heart disease, Raynaud’s disease, Parkinson’s disease, epilepsy, glaucoma, depression. Severe renal impairment (GFR <30 mL/min). Lactation.
Special Precautions
1st degree AV block, moderate heart failure, severe coronary artery disease, unstable angina, history of angioneurotic oedema. Avoid abrupt withdrawal. Moderate renal impairment (GFR 30-60 mL/min).
Adverse Reactions
Bradycardia, tinnitus, headache, dizziness, somnolence, syncope, hypotension, diarrhoea, dry mouth, nausea, vomiting, dyspepsia, pruritus, angioedema, asthenia, oedema, back or neck pain, insomnia, nervousness.
Patient Counseling Information
This drug may cause somnolence and dizziness, if affected, do not drive or operate machinery.
Overdosage
Symptoms: Headache, sedation, somnolence, hypotension, dizziness, asthenia, bradycardia, dry mouth, vomiting, fatigue, upper abdominal pain. Management: May consider admin of IV fluids and dopamine for hypotension, atropine for bradycardia, or α-receptor antagonists for paradoxal hypertensive effects.
Drug Interactions
Additive effects w/ other antihypertensives. May enhance the sedative effects of benzodiazepines, TCAs, tranquilisers, sedatives and hypnotics. TCAs may reduce the effect of moxonidine.
Food Interaction
May potentiate the sedative effect of alcohol.
Action
Description: Moxonidine is a centrally-acting antihypertensive. It acts in the brainstem through stimulation of central imidazoline receptors to reduce sympathetic tone. It also has a low affinity for α2-adrenoceptors.
Pharmacokinetics:
Absorption: Well absorbed from the GI tract. Bioavailability: Approx 88%. Time to peak plasma concentration: 0.5-3 hr.
Distribution: Enters breast milk. Plasma protein binding: Approx 7%.
Metabolism: Metabolised via opening of the imidazoline ring, mainly to 4,5-dehydromoxonidine and to a guanidine derivative.
Excretion: Via urine (approx 50-75% as unchanged drug). Plasma elimination half-life: 2-3 hr.
Chemical Structure

Chemical Structure Image
Moxonidine

Source: National Center for Biotechnology Information. PubChem Database. Moxonidine, CID=4810, https://pubchem.ncbi.nlm.nih.gov/compound/Moxonidine (accessed on Jan. 23, 2020)

Storage
Store at or below 25°C.
ATC Classification
C02AC05 - moxonidine ; Belongs to the class of imidazoline receptor agonists, centrally-acting antiadrenergic agents. Used in the treatment of hypertension.
References
Buckingham R (ed). Moxonidine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 22/07/2016.

Joint Formulary Committee. Moxonidine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 22/07/2016.

Disclaimer: This information is independently developed by MIMS based on Moxonidine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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