Oradin

Approved Indications:

• Seasonal allergic rhinitis (hay fever): Relief of nasal and ocular symptoms such as sneezing, rhinorrhea, nasal congestion, itchy nose, and itchy/watery eyes.
• Perennial allergic rhinitis: Management of chronic allergic symptoms throughout the year.
• Chronic idiopathic urticaria: Relief of itching and the reduction in the number and size of hives.

Clinically Accepted Off-Label Uses:

• Allergic conjunctivitis (supportive treatment)
• Cold-induced urticaria
• Atopic dermatitis (mild cases): For pruritus relief
• Insect bite reactions: As adjunctive therapy to reduce itching and inflammation

Adults and Adolescents ≥12 years:

• Tablet or Syrup: 10 mg once daily (oral)

Children 6 to 11 years:

• Tablet (if swallowable): 10 mg once daily
• Syrup: 10 mL once daily (5 mg/5 mL = 10 mg total)

Children 2 to 5 years:

• Syrup only: 5 mL once daily (5 mg total)

Children <2 years:

• Use not routinely recommended. Use only if prescribed by a physician with weight-based dosing.

Elderly:

• No routine dose adjustment; monitor for increased sensitivity.

Renal Impairment (Severe):

• 10 mg every other day.

Hepatic Impairment:

• 10 mg every other day due to prolonged elimination half-life.

Route of Administration:

• Oral (tablet, syrup, or dispersible tablet)
• May be taken with or without food.

Loratadine is a long-acting, non-sedating, second-generation H1-antihistamine. It selectively inhibits peripheral histamine H1 receptors, thereby blocking histamine-mediated allergic reactions such as vasodilation, increased vascular permeability, and sensory nerve stimulation. Because it does not easily cross the blood-brain barrier, Loratadine has minimal sedative effects. Its active metabolite, desloratadine, contributes to its sustained antihistaminic activity.

• Absorption: Rapid and nearly complete after oral administration
• Bioavailability: Approximately 40% due to first-pass metabolism
• Time to Peak Concentration (Tmax): 1 to 2 hours (Loratadine), 3 to 4 hours (Desloratadine)
• Protein Binding: Loratadine ~97%; Desloratadine ~73%
• Metabolism: Hepatic via CYP3A4 and CYP2D6 into active metabolite (desloratadine)
• Half-life:
• Loratadine: ~8 hours
• Desloratadine: ~27 hours
• Elimination:
• Primarily via urine and feces as metabolites

Pregnancy:

• FDA Pregnancy Category B
• No evidence of fetal harm in animal studies; limited human data suggest relative safety. Use if clearly needed.

Lactation:

• Loratadine is excreted in breast milk in small amounts.
• Generally considered safe during breastfeeding, but caution is advised, especially in preterm or neonatal infants.

Summary: Safe for use in pregnancy and lactation when clinically indicated.

• Primary Class: Antihistamine
• Subclass: Second-generation H1-receptor antagonist
• Generation: Non-sedating

• Known hypersensitivity to Loratadine or any component of the formulation
• Severe hepatic impairment (unless adjusted dosage is used)
• Children under 2 years (unless specifically prescribed and monitored)

• Hepatic impairment: Use lower or alternate-day dosing due to reduced clearance
• Renal impairment: Caution in severe renal dysfunction; dose adjustment recommended
• CNS effects: Although non-sedating, mild drowsiness may occur in sensitive individuals
• Seizure disorders: Rare reports of seizures; use with caution in predisposed patients
• Use with alcohol or CNS depressants: May enhance sedative effects, although uncommon with Loratadine

Common:

• Nervous system: Headache, drowsiness (less frequent than first-generation antihistamines), fatigue
• Gastrointestinal: Dry mouth, nausea

Less Common:

• Abdominal discomfort
• Nervousness or restlessness (especially in children)

Serious/Rare:

• Hypersensitivity reactions (e.g., rash, urticaria, anaphylaxis – extremely rare)
• Tachycardia or palpitations
• Seizures (rare and typically dose-related or in predisposed individuals)

Onset & Severity:

• Usually mild and transient; side effects often appear within a few hours to a few days after initiation.

Major Interactions:

• CYP3A4 and CYP2D6 inhibitors (e.g., ketoconazole, erythromycin, cimetidine): May increase Loratadine levels
• Other antihistamines: Concomitant use not recommended due to risk of duplication
• Alcohol/CNS depressants: Minimal interaction expected, but caution advised in sensitive individuals

Food Interactions:

• Food may slightly delay absorption, but does not affect efficacy.

• Loratadine continues to be recommended as a first-line therapy for allergic rhinitis and chronic urticaria in international guidelines (ARIA, EAACI, AAAAI).
• Desloratadine, its active metabolite, is sometimes preferred due to longer half-life but both are considered clinically effective and interchangeable based on patient response.
• Pediatric use (≥2 years) confirmed as safe and effective in global guidelines.

• Temperature: Store at 20°C to 25°C (68°F to 77°F)
• Light: Protect from direct light
• Humidity: Store in a dry place
• Handling Instructions:
• Keep out of reach of children
• Shake syrup well before each use
• Use dispersible tablets immediately after reconstitution
• Do not freeze liquid preparations