Schedule H

Oral

• Tablets: 0.2 mg, 0.3 mg, 0.4 mg

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

Essential Hypertension (Mild to Moderate)

Parameter Details

Starting dose 0.2 mg orally once daily (preferably in the morning)

Titration After 2–3 weeks, may increase by 0.2 mg/day increments based on BP response and tolerability

Usual maintenance dose 0.2–0.4 mg/day (once daily or divided twice daily)

Maximum dose 0.6 mg/day (if ≥0.4 mg/day, divide into two doses)

Dosing by Clinical Scenario:

Clinical Scenario Starting Dose Titration Maximum Dose Notes

Mild hypertension (Grade 1) 0.2 mg once daily Increase by 0.2 mg after 3 weeks if needed 0.4 mg/day Monotherapy may suffice

Moderate hypertension (Grade 2) 0.2 mg once daily Increase to 0.4 mg/day after 2–3 weeks 0.6 mg/day in divided doses Usually requires combination therapy

Add-on therapy to existing regimen 0.2 mg once daily Titrate cautiously; adjust other agents as needed 0.4 mg/day Monitor for additive hypotension

High sympathetic tone (tachycardia, anxiety) 0.2 mg once daily Titrate based on HR and BP response 0.6 mg/day Particularly useful in this phenotype

Elderly patients (>65 years) 0.2 mg once daily Slower titration over 3–4 weeks 0.4 mg/day Higher risk of orthostatic hypotension

Renal impairment (eGFR 30–60) 0.2 mg once daily Titrate cautiously every 3–4 weeks 0.4 mg/day Monitor renal function

Renal impairment (eGFR <30) 0.2 mg once daily Generally avoid titration 0.2 mg/day Close monitoring required

Clinical Notes:

• Consistent timing of administration improves adherence — morning dosing preferred

• May be taken with or without food

• Avoid abrupt cessation — taper over 1–2 weeks to prevent rebound hypertension

• Not first-line in Indian hypertension guidelines — reserve for resistant hypertension or patients intolerant to first-line agents

• Particularly useful in patients with metabolic syndrome or high sympathetic activity

Secondary Indications — Adults Only (Off-label)

Indication Dose Duration Specialist Required Evidence Basis

Resistant hypertension — OFF-LABEL 0.2–0.6 mg/day; titrate as per primary use Long-term Yes (Cardiologist/Nephrologist) European observational studies; limited India-specific data; useful as add-on in multidrug regimens

Hypertension with metabolic syndrome — OFF-LABEL 0.2–0.4 mg/day Long-term Yes Some RCT evidence of favourable metabolic profile; reduces sympathetic overdrive

Diabetic nephropathy with hypertension — OFF-LABEL 0.2–0.4 mg/day Chronic use; monitor renal parameters Yes (Nephrologist) Small European RCTs; presumed benefits via sympatholysis; not in standard Indian nephrology guidelines

PAEDIATRIC DOSING (Specialist Only)

Primary Indications

Not applicable — Moxonidine is NOT approved for paediatric use.

Secondary Indications — Paediatric (Off-label)

Not applicable — No established paediatric indications.

⚠️ Not recommended in children and adolescents below 18 years of age. Safety and efficacy not established. No paediatric formulations available in India. Use only in exceptional circumstances (refractory hypertension) under specialist supervision with documented justification.

60 0.2 mg once daily 0.6 mg/day Standard BP monitoring No dose adjustment required

30–60 0.2 mg once daily 0.4 mg/day BP, renal function every 2–4 weeks initially Titrate cautiously; slower increments

<30 0.2 mg once daily 0.2 mg/day Close BP and renal monitoring weekly initially Avoid titration; use with caution

Haemodialysis 0.2 mg once daily 0.2 mg/day Post-dialysis BP monitoring Not significantly removed by dialysis; administer after dialysis session

Peritoneal dialysis 0.2 mg once daily 0.2 mg/day Regular BP monitoring Use with caution; limited data

Note: Moxonidine is primarily renally excreted (~90%); dose reduction essential in renal impairment to avoid accumulation and excessive hypotension.

• Sinus bradycardia (heart rate <50 bpm)

• Sick sinus syndrome (without pacemaker)

• Second-degree or third-degree AV block (without pacemaker)

• Severe heart failure (NYHA Class III–IV)

• Unstable angina or acute coronary syndrome

• Recent myocardial infarction (within 3 months)

• Severe arrhythmias

• Known hypersensitivity to moxonidine or any excipient

• Severe depression with suicidal ideation

• Concurrent use with clonidine (risk of rebound hypertension)

• Mild to moderate heart failure (NYHA Class I–II) — risk of bradycardia or haemodynamic deterioration

• First-degree AV block — monitor ECG

• History of depression or mood disorders — may worsen; monitor mental status

• Moderate renal impairment — requires dose adjustment

• Elderly patients — increased sensitivity to hypotensive and CNS effects

• Raynaud's phenomenon or peripheral vascular disease

• Concurrent use with other centrally acting antihypertensives (additive effects)

• Concurrent use with beta-blockers — additive bradycardia risk; avoid abrupt withdrawal of either drug

• Risk of sedation and dizziness — advise caution with driving or operating machinery

• Abrupt discontinuation — risk of rebound hypertension; always taper

Parameter Details

Safety Category Not well classified in India; limited human data; generally avoided

Preferred alternatives Labetalol, nifedipine (extended-release), methyldopa — as per Indian obstetric guidelines

When to use Only if potential benefit justifies risk and preferred alternatives are contraindicated or ineffective; specialist (Obstetrician/Cardiologist) supervision required

Monitoring Maternal blood pressure; fetal heart rate; fetal growth monitoring

Parameter Details

Compatibility Not recommended — moxonidine is excreted in breastmilk

Drug levels in milk Unknown; potential for significant transfer

Preferred alternatives Methyldopa, labetalol, nifedipine — preferred antihypertensives during lactation per Indian practice

Infant monitoring If used despite recommendation, monitor infant for sedation, poor feeding, lethargy, hypotension

Parameter Recommendation

Starting dose 0.2 mg once daily

Titration Slower titration over 3–4 weeks; increase by 0.2 mg only if well tolerated

Maximum dose 0.4 mg/day (avoid higher doses unless essential)

Special considerations Increased sensitivity to hypotensive and CNS effects; higher risk of orthostatic hypotension; assess renal function before initiation

Additional risks Falls risk due to dizziness and postural hypotension; bradycardia; confusion; syncope

Drug Mechanism Clinical Effect Recommendation

Clonidine Both are centrally acting antihypertensives Additive hypotension; severe rebound hypertension if either discontinued abruptly Avoid concurrent use

Beta-blockers Additive negative chronotropic effect Significant bradycardia; AV block; enhanced rebound hypertension if abruptly stopped Use with caution; avoid abrupt withdrawal of either drug; monitor HR and ECG

Tricyclic antidepressants (amitriptyline, imipramine) Antagonise central antihypertensive effect Reduced moxonidine efficacy Avoid combination; consider alternative antidepressants

Digoxin Additive AV nodal depression Enhanced risk of bradycardia and AV block Monitor ECG; use with caution

MAO inhibitors Potential for hypertensive crisis or enhanced hypotension Unpredictable BP effects Avoid concurrent use

Drug Interaction Recommendation

Other antihypertensives (ACE inhibitors, ARBs, CCBs, diuretics) Additive hypotensive effect Monitor BP closely; adjust doses as needed

Benzodiazepines, Opioids, Sedatives Additive CNS depression Monitor for excessive sedation; use caution

Alcohol Enhanced hypotensive and sedative effects Counsel to limit alcohol intake

NSAIDs (ibuprofen, diclofenac, naproxen) May attenuate antihypertensive effect Regular BP monitoring; consider dose adjustment

Diuretics (thiazides, loop diuretics) Enhanced hypotension; electrolyte imbalance Monitor BP and electrolytes

Alpha-blockers (prazosin, tamsulosin) Additive hypotension; orthostatic effects Use with caution; monitor for postural symptoms

Verapamil, Diltiazem Additive bradycardia and AV nodal depression Monitor HR and ECG

• Dry mouth (most common; dose-related)

• Dizziness

• Headache

• Fatigue/asthenia

• Somnolence/sedation

• Nausea

• Insomnia (paradoxical)

• Peripheral oedema (mild)

• Rebound hypertension — with abrupt discontinuation; may be severe; always taper

• Significant bradycardia — may require dose reduction or discontinuation

• AV block — monitor ECG in at-risk patients

• Severe hypotension/Syncope — dose-related; more common in elderly or with drug interactions

• Depression worsening — monitor mood; discontinue if significant mood changes occur

• Angioedema — rare; discontinue immediately

• Heart failure exacerbation — avoid in NYHA III–IV; use cautiously in NYHA I–II

Phase Parameters

Baseline Blood pressure (supine and standing); heart rate; ECG (especially in elderly or cardiac patients); renal function (serum creatinine, eGFR); mood/depression screening

After initiation/dose change BP and HR weekly for first month; assess for orthostatic hypotension; monitor for dizziness, sedation, dry mouth

Long-term BP and HR every 3–6 months; renal function annually (or more frequently if impaired); periodic mood assessment; ECG if symptomatic

• Physiotens® (Abbott/Solvay)

• Moxovas® (Lupin)

• Moxcent® (Centaur)

• Clonivel® (Micro Labs)

• Moxibest® (Zydus)

• Moxicard® (Torrent)

0.2 mg tablet ₹4–8 per tablet

0.3 mg tablet ₹6–10 per tablet

0.4 mg tablet ₹8–12 per tablet

Note: Not included in NLEM 2022; not NPPA price-controlled; available only in private market.

• Not first-line: Moxonidine is not first-line therapy per Indian hypertension guidelines (ISH-India) — reserve for resistant hypertension, intolerance to first-line agents, or as add-on therapy

• Sympathetic overdrive phenotype: Particularly useful in patients with high sympathetic tone (resting tachycardia, anxiety, metabolic syndrome) — provides both BP control and heart rate reduction

• Metabolic advantages: Unlike beta-blockers, moxonidine has neutral to favourable effects on glucose and lipid metabolism — consider in hypertensive patients with metabolic syndrome or diabetes

• Taper before stopping: Never discontinue abruptly — rebound hypertension can occur; taper over 1–2 weeks

• Less sedation than clonidine: Better tolerated than clonidine with lower incidence of sedation and dry mouth — preferred centrally acting agent when this class is indicated

• Bradycardia caution: Monitor HR regularly, especially when combined with beta-blockers, digoxin, or non-dihydropyridine CCBs

moxonidine; hypertension; imidazoline agonist; centrally acting antihypertensive; resistant hypertension; sympatholytic; renal-adjust; elderly-caution; bradycardia-risk; rebound-hypertension; Schedule H; India

RxIndia v1.0 — 06 Apr 2025

• CDSCO approved product labelling and inserts

• Indian Pharmacopoeia/NFI 2021

• API Textbook of Medicine 2022

• Indian Society of Hypertension Guidelines (ISH-India) 2020

• AIIMS Drug Formulary

• Goodman & Gilman's The Pharmacological Basis of Therapeutics

• Harrison's Principles of Internal Medicine

• Indian clinical practice inputs (resistant hypertension management)