Drug reference

Moxonidine

Centrally-acting imidazoline I1 / α2 agonist (antihypertensive) · Antihypertensive

START

200 mcg PO once daily in the morning

TYPICAL MAX

600 mcg/day

STOP IF

Severe bradycardia, syncope, or rebound HTN on stopping

WATCH

HR, BP, mental alertness; taper if stopping

CDSCO approvedSchedule HATC C02AC05

Dose laddermg/d

Renal dose adjustmenteGFR mL/min/1.73m²

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours

ONSET: 30min · absorption
PEAK: 1h · Tmax
t½: 2.5h · t½
DURATION: 1d · once-daily

EXCRETION

Renal — ~75% unchanged

route + CYP

INTERACTIONS

—

none in our sources

PREGNANCY

Avoid (limited data; methyldopa preferred).

FDA category + note

Mechanism

Selective agonist at central imidazoline I1 receptors in the rostral ventrolateral medulla (with some α2 activity), reducing sympathetic outflow and lowering blood pressure with less sedation / dry mouth than clonidine.

Indications

Mild-to-moderate essential hypertension (when other agents inappropriate)

Dosing

Adult: 200 mcg PO once daily morning; max 600 mcg/day in 1–2 divided doses.
Pediatric: Not established.
Renal adjustment: CrCl 30–60: 200 mcg/day max; CrCl <30: contraindicated.
Hepatic adjustment: No specific adjustment.
Geriatric: Start 200 mcg; titrate slowly.
Max dose: 600 mcg/day

Pharmacokinetics

Onset

BP effect 2–4 h

Peak effect

~1 h (Tmax)

Duration

~24 h (once-daily)

Half-life

~2.5 h (effect outlasts plasma t½)

Bioavailability

~88%

Protein binding

~7%

Metabolism

Minimal hepatic

Excretion

Renal (~75% unchanged)

Contraindications

Sick sinus syndrome / second–third-degree AV block
Bradycardia (HR <50)
Severe heart failure
Severe renal impairment (CrCl <30)
Hypersensitivity

Side effects

Common

Dry mouth (less than clonidine)HeadacheDizzinessAstheniaSleep disturbance

Serious

Severe bradycardia / heart block
Rebound hypertension on abrupt discontinuation
Severe hypotension / syncope

Pregnancy & lactation

Pregnancy

Avoid (limited data; methyldopa preferred).

Lactation

Avoid (limited data).

Drug interactions

Beta Blockers

Moderate

Database

Additive bradycardia + rebound HTN risk on abrupt withdrawal

Taper β-blocker first if stopping moxonidine