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Indications and Dosage
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).
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Renal Impairment
Severe (GFR <30 mL/min): Contraindicated. Moderate (GFR 30-60 mL/min): Max: 400 mcg daily (max 200 mcg per single dose).
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Administration
May be taken with or without food.
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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.
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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).
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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.
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Patient Counseling Information
This drug may cause somnolence and dizziness, if affected, do not drive or operate machinery.
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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.
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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.
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Food Interaction
May potentiate the sedative effect of alcohol.
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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. |
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Chemical Structure
 Source: National Center for Biotechnology Information. PubChem Database. Moxonidine, CID=4810, https://pubchem.ncbi.nlm.nih.gov/compound/Moxonidine (accessed on Jan. 23, 2020) |
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Storage
Store at or below 25°C.
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MIMS Class
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ATC Classification
C02AC05 - moxonidine ; Belongs to the class of imidazoline receptor agonists, centrally-acting antiadrenergic agents. Used in the treatment of hypertension.
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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.
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