Generic
Moxonidine
2 brands available in the market
At a glance
Moxonidine is a centrally-acting antihypertensive used for high blood pressure. It stimulates central imidazoline receptors in the brainstem to reduce sympathetic tone and relax blood vessels, lowering blood pressure.
Description
Moxonidine is a centrally-acting antihypertensive. It acts in the brainstem through stimulation of central imidazoline receptors (I1) to reduce sympathetic tone. Moxonidine has low affinity for alpha2-adrenoceptors. It reduces systemic vascular resistance and arterial blood pressure.
Indications
- Hypertension (high blood pressure)
Therapeutic class
Anti-hypertensive
Pharmacological class
Centrally-acting Antihypertensive
Pharmacology
Moxonidine stimulates imidazoline receptors (I1) in the brainstem to reduce sympathetic nerve activity, decreasing systemic vascular resistance and arterial blood pressure. Low affinity for alpha2-adrenoceptors results in fewer sedation and dry mouth side effects.
Mechanism of action
Lowers blood pressure by reducing sympathetic tone and relaxing blood vessels.
Dosage
Adult Dose (Oral):
- Initial: 200 mcg in the morning
- After 3 weeks if needed: 400 mcg (single or divided dose)
- After further 3 weeks if needed: Up to 600 mcg (divided dose)
- Maximum dose: 600 mcg/day
Renal Dose:
- CrCl 30-60: Single dose not to exceed 200 mcg; max 400 mcg/day
- CrCl <30: Avoid use
Administration
- Swallow tablet whole; do not chew, crush or break
- May be taken with or without food
- Take at the same time each day
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Common Side Effects:
- Dry mouth
- Headache
- Dizziness
- Somnolence
- Weakness
- Nausea, vomiting
- Diarrhea
- Back pain
- Insomnia
- Vertigo
- Rash
Precautions & warnings
- Caution when driving or doing activities requiring concentration (may cause drowsiness and dizziness)
- Avoid alcohol (excessive drowsiness)
- May cause orthostatic hypotension; rise slowly
- Rebound hypertension may occur if stopped abruptly with beta-blockers; stop beta-blocker first
- Caution in renal impairment; dose adjustment needed
- Caution in severe liver disease
Contraindications
- Hypersensitivity
- Conduction disorders
- Bradycardia (resting HR <50/min)
- Severe arrhythmias
- Severe heart failure
- Severe ischaemic heart disease
- History of angioedema
- Severe renal or hepatic impairment
- Raynaud's syndrome
- Intermittent claudication
- Epilepsy
- Depression
- Parkinson's disease
- Glaucoma
- Pregnancy and lactation
Drug interactions
- Additive effects with other antihypertensives
- May increase sedative effects of benzodiazepines
- Effects may be antagonized by tricyclic antidepressants
Food interactions
Alcohol may cause excessive drowsiness.
Use in pregnancy
Use in Pregnancy: Moxonidine may be unsafe during pregnancy (Category B3); animal studies show evidence of fetal harm. Use only if clearly needed.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Moxonidine is secreted in breast milk; should not be used during breastfeeding.
Pediatric use
Safety and efficacy not established in children.
Geriatric use
Elderly may require dose adjustment.
Renal / hepatic impairment
Renal Impairment: Caution in kidney disease; dose adjustment needed (based on CrCl).
Hepatic Impairment: Caution in severe liver disease; dose adjustment may be needed.
Overdose effects
Overdose: Hypotension, bradycardia, dry mouth, somnolence, nausea; symptomatic treatment.
Storage conditions
Store below 25°C; protect from light and moisture; keep out of reach of children.
Chemical structure
Moxonidine