Methovate-R

Approved Indications:

• Otolaryngologic use (ear, nose, throat):
• Symptomatic relief of nasal congestion, inflammation, and pain in rhinitis, sinusitis, and nasopharyngitis.
• Supportive treatment for otitis externa and otitis media (with or without tympanostomy tubes) to relieve inflammation, swelling, and pain.

Topical and ENT Combination Use:

• Treatment of allergic or inflammatory nasal conditions requiring a combination of corticosteroid (anti-inflammatory), decongestant (vasoconstrictor), and anesthetic (pain reliever) action.

Clinically Accepted Off-label Uses:

• Adjunctive therapy in procedural nasal preparation before minor ENT procedures (e.g., nasal endoscopy).
• Relief of symptoms in post-nasal surgery recovery where inflammation and pain management are needed.

Route of Administration: Intranasal (nasal drops or spray), Otic (ear drops), Topical ENT use.

Adults:

• Nasal Use: 2-3 drops or sprays into each nostril 2-3 times daily.
• Otic Use: 2-4 drops in the affected ear 2-3 times daily.

Pediatrics (Above 2 years):

• Nasal Use: 1-2 drops or sprays in each nostril 2-3 times daily under supervision.
• Otic Use: 2-3 drops in the ear canal 2-3 times daily.

Elderly:

• Same adult dosing; monitor for cardiovascular sensitivity to phenylephrine.

Renal/Hepatic Impairment:

• No dose adjustment typically required for localized use, but use with caution.

Duration:

• Typically used for short courses (up to 7 days); prolonged use not recommended due to risk of rebound congestion or corticosteroid-related adverse effects.

• Betamethasone is a potent glucocorticoid that binds to intracellular corticosteroid receptors, modulating gene expression to inhibit pro-inflammatory cytokines and mediators, resulting in reduced swelling, erythema, and exudation.
• Phenylephrine is a selective α1-adrenergic receptor agonist that causes vasoconstriction in the nasal and mucosal blood vessels, decreasing nasal edema and congestion.
• Lignocaine (Lidocaine) is a local amide-type anesthetic that blocks voltage-gated sodium channels in neuronal membranes, preventing the initiation and propagation of nerve impulses, thereby producing local anesthesia and rapid pain relief.

Betamethasone (Local Use):

• Absorption: Minimal systemic absorption with topical use; increased with prolonged or extensive application.
• Distribution: Widely distributed if absorbed systemically.
• Metabolism: Hepatic via CYP3A4.
• Elimination: Renal.

Phenylephrine (Topical Use):

• Absorption: Rapid mucosal absorption; systemic absorption is possible but low when used topically.
• Onset: 15–30 minutes.
• Duration: 2–4 hours.
• Metabolism: MAO-mediated metabolism in liver and gut.
• Elimination: Mainly renal.

Lignocaine (Topical Use):

• Absorption: Rapid from mucous membranes.
• Onset: Within minutes.
• Duration: 30–60 minutes.
• Metabolism: Hepatic via CYP1A2 and CYP3A4.
• Elimination: Renal (as metabolites).

Pregnancy:

• Betamethasone: Category C – Risk cannot be ruled out; avoid prolonged or extensive application during pregnancy.
• Phenylephrine: Caution advised due to possible systemic vasoconstriction and reduced uterine blood flow.
• Lignocaine: Category B – Generally considered safe in limited local use.

Lactation:

• No significant data on excretion in breast milk for this combination. Topical use is considered low risk if applied in limited amounts; avoid application near the breast area.
• Caution advised, especially in neonates and premature infants.

• Combination Preparation:
• Betamethasone: Corticosteroid (Anti-inflammatory)
• Phenylephrine: Sympathomimetic (Nasal decongestant)
• Lignocaine: Local anesthetic (Amide class)

• Hypersensitivity to betamethasone, phenylephrine, lignocaine, or formulation excipients.
• Viral, fungal, or tubercular infections of the ear/nose.
• Perforated tympanic membrane (for otic use).
• Severe hypertension or coronary artery disease (due to phenylephrine).
• Use in children under 2 years unless specifically directed by a physician.

• Prolonged use may lead to rebound nasal congestion or mucosal atrophy.
• Use with caution in:
• Patients with hypertension, cardiac disease, hyperthyroidism, or diabetes (due to phenylephrine).
• Patients with glaucoma or systemic infections.
• Avoid ocular exposure; may cause eye irritation.
• Clinical monitoring is advised in long-term users for adrenal suppression or local irritation.
• Discontinue if symptoms worsen or no improvement within 7 days.

Common:

• Nasal irritation, dryness or burning sensation
• Transient stinging or bitter taste
• Headache, dizziness (rarely)

Less Common / Serious:

• Rebound congestion (rhinitis medicamentosa)
• Mucosal ulceration or atrophy with prolonged use
• Systemic corticosteroid effects (rare, with long-term use)
• Allergic reactions: rash, itching, swelling

Dose-dependence: Most side effects are local and dose-frequency related.

• Phenylephrine:
• May interact with MAO inhibitors (hypertensive crisis risk).
• Use cautiously with beta-blockers, tricyclic antidepressants, or antihypertensives.
• Lignocaine:
• May enhance effects of antiarrhythmics, cimetidine, or other local anesthetics.
• CYP1A2/CYP3A4 inhibitors may increase systemic lignocaine levels (rare with topical use).
• Betamethasone:
• Additive systemic corticosteroid effects with other corticosteroids.
• May reduce response to vaccines.

• Combination preparations with phenylephrine are being reevaluated in some jurisdictions due to the limited effectiveness of oral phenylephrine. However, intranasal formulations remain widely accepted.
• No significant changes in international guidelines recently regarding this combination.
• Safety emphasis increased on limiting treatment duration (not exceeding 7 days) to prevent rebound congestion and steroid overuse.

• Store below 25°C in a dry place.
• Protect from light and moisture.
• Do not freeze.
• Shake well before use if suspension.
• Keep container tightly closed and out of reach of children.