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Rupatadine

Second-generation H1 antihistamine with PAF antagonism · Antiallergic

Also known as Rupatadine fumarate

START
10 mg PO once daily
TYPICAL MAX
10 mg/day
STOP IF
Severe hypersensitivity (rare)
WATCH
Sedation (mild); QT-prolonging co-meds in at-risk patients
CDSCO approvedSchedule HATC R06AX28
Dose laddermg/d
2.5child low5child mid10adult/day
Renal dose adjustmenteGFR mL/min/1.73m²
FULLNo fixed adjustment; caution if severe90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
30minONSET45minPEAK6h1dDURATION
ONSET
30min · absorption
PEAK
45min · Tmax
6h ·
DURATION
1d · once-daily
EXCRETION
Mainly faecal; minor renal
route + CYP
INTERACTIONS
none in our sources
PREGNANCY
Limited data; use only if benefit outweighs risk.
FDA category + note

Mechanism

Selective peripheral H1-receptor antagonist with concurrent platelet-activating factor (PAF) receptor blockade — provides anti-allergic and anti-inflammatory effects; minimal CNS sedation at therapeutic doses.

Indications

Seasonal / perennial allergic rhinitis (≥2 y)Chronic urticaria (≥2 y)

Dosing

Adult
10 mg PO once daily.
Pediatric
≥2 y: 2.5 mg/day (10–24 kg); 5 mg/day (25–49 kg); 10 mg/day (≥50 kg) — once daily.
Renal adjustment
Limited data in significant impairment; caution.
Hepatic adjustment
Limited data in significant impairment; caution.
Geriatric
No specific adjustment; rare sedation.
Max dose
10 mg/day

Pharmacokinetics

Onset
~30 min (symptom relief)
Peak effect
~45 min (Tmax)
Duration
~24 h
Half-life
~6 h (active metabolites longer)
Bioavailability
Well absorbed orally
Protein binding
~98%
Metabolism
Hepatic CYP3A4 (desloratadine is an active metabolite)
Excretion
Mainly faecal; minor renal

Contraindications

  • Hypersensitivity
  • Caution: QT prolongation risk factors (less than older antihistamines)

Side effects

Common
HeadacheSomnolence (mild)FatigueDry mouthNausea
Serious
  • QT prolongation (theoretical, not seen at therapeutic doses)
  • Severe hypersensitivity

Pregnancy & lactation

Pregnancy

Limited data; use only if benefit outweighs risk.

Lactation

Limited data; caution.

Drug interactions

Qt Prolonging Drugs
Moderate
Database

Additive QT effect (theoretical)

Caution in at-risk patients

Source: Kimi deep-research + Cla

Strong Cyp3a4 Inhibitors
Moderate
Database

Increased rupatadine exposure

Monitor; avoid if possible

Source: Kimi deep-research + Cla

Alcohol
Mild
Database

Possible additive sedation

Counsel

Source: Kimi deep-research + Cla

Cns Depressants
Mild
Database

Possible additive sedation

Avoid stacking

Source: Kimi deep-research + Cla

Grapefruit Juice
Mild
Database

Gut CYP3A4 inhibition

Avoid grapefruit (precaution)

Source: Kimi deep-research + Cla

Related guidelines

Ask House about Rupatadine

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: KD Tripathi 7e, BNF·Verified: 2026-05-20 · House clinical team·Cockpit curated: 2026-05-20