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Pronunciation
(lor AT a deen)
Generic Available (U.S.)
Yes
U.S. Brand Names
Canadian Brand Names
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Relief of nasal and non-nasal symptoms of seasonal allergic rhinitis; treatment of chronic idiopathic urticaria
Contraindications
Hypersensitivity to loratadine or any component of the formulation
Warnings/Precautions
Disease-related concerns:
• Hepatic impairment: Use with caution in patients with hepatic impairment; dosage adjustment recommended.
• Renal impairment: Use with caution in patients with renal impairment; dosage adjustment recommended.
Dosage form specific issues:
• Phenylalanine: Some products may contain phenylalanine.
Adverse Reactions
Adults:
Central nervous system: Headache (12%), somnolence (8%), fatigue (4%)
Gastrointestinal: Xerostomia (3%)
Children:
Central nervous system: Nervousness (4% ages 6-12 years), fatigue (3% ages 6-12 years, 2% to 3% ages 2-5 years), malaise (2% ages 6-12 years)
Dermatologic: Rash (2% to 3% ages 2-5 years)
Gastrointestinal: Abdominal pain (2% ages 6-12 years), stomatitis (2% to 3% ages 2-5 years)
Neuromuscular & skeletal: Hyperkinesia (3% ages 6-12 years)
Ocular: Conjunctivitis (2% ages 6-12 years)
Respiratory: Wheezing (4% ages 6-12 years), dysphonia (2% ages 6-12 years), upper respiratory infection (2% ages 6-12 years), epistaxis (2% to 3% ages 2-5 years), pharyngitis (2% to 3% ages 2-5 years)
Miscellaneous: Flu-like syndrome (2% to 3% ages 2-5 years), viral infection (2% to 3% ages 2-5 years)
Adults and Children: <2%: Agitation, altered lacrimation, altered micturition, altered salivation, altered taste, amnesia, angioneurotic edema, anorexia, anxiety, appetite increased, arthralgia, back pain, blepharospasm, blurred vision, breast pain, bronchitis, bronchospasm, chest pain, confusion, constipation, cough, depression, dermatitis, diaphoresis increased, diarrhea, dizziness, dry hair, dry skin, dysmenorrhea, dyspepsia, dysphonia, dyspnea, earache, eye pain, flatulence, flushing, gastritis, hemoptysis, hiccup, hypertension, hypertonia, hypoesthesia, hypotension, impaired concentration, impotence, insomnia, irritability, laryngitis, leg cramps, libido decreased, loose stools, malaise, menorrhagia, migraine, myalgia, nasal dryness, nausea, palpitation, paresthesia, paroniria, photosensitivity, pruritus, purpura, rigors, sinusitis, sneezing, supraventricular tachyarrhythmia, syncope, tachycardia, thirst, tinnitus, tremor, urinary discoloration, urinary incontinence, urinary retention, urticaria, vaginitis, vertigo, vomiting, weakness, weight gain
Postmarketing and/or case reports: Abnormal hepatic function, alopecia, anaphylaxis, breast enlargement, erythema multiforme, hepatitis, hepatic necrosis, jaundice, peripheral edema, seizure, thrombocytopenia
Metabolism/Transport Effects
Substrate of CYP2D6 (minor), CYP3A4 (minor), P-glycoprotein; Inhibits CYP2C8 (weak), 2C19 (moderate), 2D6 (weak)
Drug Interactions
Acetylcholinesterase Inhibitors (Central): Anticholinergics may diminish the therapeutic effect of Acetylcholinesterase Inhibitors (Central). Acetylcholinesterase Inhibitors (Central) may diminish the therapeutic effect of Anticholinergics. If the anticholinergic action is a side effect of the agent, the result may be beneficial. Risk C: Monitor therapy
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Amiodarone: May increase the serum concentration of Loratadine. Management: Due to reported QT interval prolongation and Torsades de Pointes with this combination, consider an alternative to loratadine when possible. Risk D: Consider therapy modification
Amphetamines: May diminish the sedative effect of Antihistamines. Risk C: Monitor therapy
Anticholinergics: May enhance the adverse/toxic effect of other Anticholinergics. Exceptions: Levocabastine (Nasal); Paliperidone. Risk C: Monitor therapy
Benzylpenicilloyl Polylysine: Antihistamines may diminish the diagnostic effect of Benzylpenicilloyl Polylysine. Management: Suspend systemic H1 antagonists for benzylpenicilloyl-polylysine skin testing and delay testing until systemic antihistaminic effects have dissipated. A histamine skin test may be used to assess persistent antihistaminic effects. Risk D: Consider therapy modification
Betahistine: Antihistamines may diminish the therapeutic effect of Betahistine. Risk C: Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Exceptions: Levocabastine (Nasal). Risk C: Monitor therapy
Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Management: Upon completion/discontinuation of conivaptan, allow at least 7 days before initiating therapy with drugs that are CYP3A4 substrates. Risk D: Consider therapy modification
Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use. Risk D: Consider therapy modification
HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Management: For patients being treated with hydroxyzine, a reduction in the dose of any other CNS depressants that are to be used in combination is recommended. With concurrent use, monitor patients closely for excessive response to the combination. Risk D: Consider therapy modification
Peginterferon Alfa-2b: May decrease the serum concentration of CYP2D6 Substrates. Risk C: Monitor therapy
P-Glycoprotein Inducers: May decrease the serum concentration of P-Glycoprotein Substrates. P-glycoprotein inducers may also further limit the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Risk C: Monitor therapy
P-Glycoprotein Inhibitors: May increase the serum concentration of P-Glycoprotein Substrates. P-glycoprotein inhibitors may also enhance the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Risk C: Monitor therapy
Pramlintide: May enhance the anticholinergic effect of Anticholinergics. These effects are specific to the GI tract. Risk D: Consider therapy modification
Selective Serotonin Reuptake Inhibitors: CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. Risk C: Monitor therapy
Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Ethanol: May increase CNS depression; monitor for increased effects with coadministration. Caution patients about effects.
Food: Increases bioavailability and delays peak.
Herb/Nutraceutical: St John's wort may decrease loratadine levels.
Storage
Store at 2°C to 25°C (36°F to 77°F).
Rapidly-disintegrating tablets: Use within 6 months of opening foil pouch, and immediately after opening individual tablet blister. Store in a dry place.
Mechanism of Action
Long-acting tricyclic antihistamine with selective peripheral histamine H1-receptor antagonistic properties
Pharmacodynamics/Kinetics
Onset of action: 1-3 hours
Peak effect: 8-12 hours
Duration: >24 hours
Absorption: Rapid
Metabolism: Extensively hepatic via CYP2D6 and 3A4 to active metabolite
Half-life elimination: 12-15 hours
Excretion: Urine (40%) and feces (40%) as metabolites
Dosage
Oral: Seasonal allergic rhinitis, chronic idiopathic urticaria:
Children 2-5 years: 5 mg once daily
Children ≥6 years and Adults: 10 mg once daily
Elderly: Peak plasma levels are increased; elimination half-life is slightly increased; specific dosing adjustments are not available
Dosage adjustment in renal impairment: Clcr ≤30 mL/minute:
Children 2-5 years: 5 mg every other day
Children ≥6 years and Adults: 10 mg every other day
Dosage adjustment in hepatic impairment: Elimination half-life increases with severity of disease
Children 2-5 years: 5 mg every other day
Children ≥6 years and Adults: 10 mg every other day
Administration: Oral
Administer on an empty stomach.
Dietary Considerations
Take on an empty stomach. Some products may contain phenylalanine and/or sodium.
Patient Education
Avoid use of alcohol. You may experience drowsiness, dizziness, dry mouth, or nausea. Report persistent dizziness or sedation; swelling of face, mouth, lips, or tongue; respiratory difficulty; lack of improvement; or worsening of condition.
Rapidly-disintegrating tablets: Place tablet on tongue; it dissolves rapidly. May be used with or without water. Use within 6 months of opening foil pouch and immediately after opening individual tablet blister.
Geriatric Considerations
Loratadine is a nonsedating antihistamines; because of its low incidence of side effects, it seems to be a good choice in the elderly. However, there is a wide variation in loratadine half-life reported in the elderly and this should be kept in mind when initiating dosing. Because of its new OTC status, patients should be advised of appropriate use.
Cardiovascular Considerations
At recommended doses, loratadine has not been associated with clinically relevant QT prolongation or ventricular arrhythmias (eg, torsade de pointes). Loratadine has been associated with supraventricular tachyarrhythmia.
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation) and stomatitis in children (2-5 years).
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
Drowsiness is common; may cause anxiety or depression
Mental Health: Effects on Psychiatric Treatment
None reported
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, liquid gel, oral:
Claritin® Liqui-Gels® 24 Hour Allergy: 10 mg
Solution, oral: 5 mg/5 mL (120 mL)
Syrup, oral: 5 mg/5 mL (120 mL)
Claritin® Children's Allergy: 5 mg/5 mL (60 mL, 120 mL) [dye free, ethanol free; contains propylene glycol, sodium benzoate; fruit flavor]
Claritin® Children's Allergy: 5 mg/5 mL (60 mL, 120 mL) [dye free, ethanol free, sugar free; contains propylene glycol, sodium 6 mg/5 mL, sodium benzoate; grape flavor]
Tablet, oral: 10 mg
Alavert® Allergy 24 Hour: 10 mg [dye free, gluten free, sucrose free]
Claritin® 24 Hour Allergy: 10 mg
Loradamed: 10 mg
Tavist® ND Allergy: 10 mg
Tablet, chewable, oral:
Claritin® Children's Allergy: 5 mg [contains phenylalanine 1.4 mg/tablet; grape flavor]
Tablet, orally disintegrating, oral: 10 mg
Alavert® Allergy 24 Hour: 10 mg [dye free, gluten free, sucrose free; contains phenylalanine 8.4 mg/tablet; Citrus Burst™ flavor]
Alavert® Allergy 24 Hour: 10 mg [dye free, gluten free, sucrose free; contains phenylalanine 8.4 mg/tablet; mint flavor]
Alavert® Children's Allergy: 10 mg [dye free, gluten free, sucrose free; contains phenylalanine 8.4 mg/tablet; Citrus Burst™ flavor]
Alavert® Children's Allergy: 10 mg [dye free, gluten free, sucrose free; contains phenylalanine 8.4 mg/tablet; bubblegum flavor]
Claritin® RediTabs® 24 Hour Allergy: 10 mg [mint flavor]
Pricing: U.S. (www.drugstore.com)
Tablet, orally-disintegrating (Claritin Reditabs)
10 mg (10): $20.99
Tablets (Claritin)
10 mg (30): $30.99
10 mg (30): $35.99
Tablets (Loratadine)
10 mg (30): $21.99
References
Clissold SP, Sorkin EM, and Goa KL, “Loratadine: A Preliminary Review of Its Pharmacodynamic Properties and Therapeutic Efficacy,” Drugs, 1989, 37(1):42-57.
Crumb WJ, “Loratadine Blockade of K(+) Channels in Human Heart: Comparison With Terfenadine Under Physiological Conditions,” J Pharmacol Exp Ther, 2000, 292(1):261-4.
Crumb WJ, “Rate-Dependent Blockade of a Potassium Current in Human Atrium by the Antihistamine Loratadine,” Br J Pharmacol, 1999, 126(3):575-80.
Delpon E, Valenzuela C, Gay P, et al, “Block of Human Cardiac Kv1.5 Channels by Loratadine: Voltage-, Time-, and Use-Dependent Block at Concentrations Above Therapeutic Levels,” Cardiovasc Res, 1997, 35(2):341-50.
Lin CC, Radwanski E, Affrime M, et al, “Pharmacokinetics of Loratadine in Pediatric Subjects,” Am J Ther, 1995, 2:504-8.
Luck JC and Evrard HM, “Atrial Fibrillation Associated With Loratadine Use,” J Allergy Clin Immunol, 1995, 95(2):282.
Lutsky BN, Klose P, Melon J, et al, “A Comparative Study of the Efficacy and Safety of Loratadine Syrup and Terfenadine Suspension in the Treatment of 3 to 6 Year Old Children With Seasonal Allergic Rhinitis,” Clin Ther, 1993, 15(5):855-65.
Simons FE, “Loratadine, a Nonsedating H1-Receptor Antagonist (Antihistamine),” Ann Allergy, 1989, 63(4):266-8.
International Brand Names
Lexi-Comp.com
Last full review/revision May 2011
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