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Medication Safety Issues
Sound-alike/look-alike issues:
Claritin® may be confused with clarithromycin
Claritin® (loratadine) may be confused with Claritin™ Eye (ketotifen)
Pronunciation
(lor AT a deen)
U.S. Brand Names
Generic Available
Yes
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
Pregnancy Risk Factor
B
Pregnancy Considerations
Loratadine was not found to be teratogenic in animal studies. There are no adequate and well-controlled studies in pregnant woman; use during pregnancy only if clearly needed.
Lactation
Enters breast milk/not recommended (AAP rates “compatible”)
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.
Special populations:
• Pediatrics: Safety and efficacy have not been established in children <2 years of age.
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 (minor) of CYP2D6, 3A4; 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
Amphetamines: May diminish the sedative effect of Antihistamines. Risk C: Monitor therapy
Anticholinergics: May enhance the adverse/toxic effect of other Anticholinergics. Exceptions: Paliperidone. Risk C: Monitor therapy
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. Risk C: Monitor therapy
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
Ethanol/Nutrition/Herb Interactions
Ethanol: Avoid ethanol (although sedation is limited with loratadine, may increase risk of CNS depression).
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
Distribution: Significant amounts enter breast milk
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. Alavert® and Dimetapp® Children's ND contain phenylalanine 8.4 mg per 10 mg tablet. Claritin® Children's Allergy 5 mg contains phenylalanine 1.4 mg per tablet.
Patient Education
Take as directed; do not exceed recommended dose. Avoid use of other depressants, alcohol, or sleep-inducing medications unless approved by prescriber. You may experience drowsiness or dizziness (use caution when driving or engaging in tasks requiring alertness until response to drug is known); or dry mouth or nausea (small frequent meals, frequent mouth care, chewing gum, or sucking hard candy may help). Report persistent dizziness, sedation, or seizures; chest pain, rapid heartbeat, or palpitations; swelling of face, mouth, lips, or tongue; respiratory difficulty; changes in urinary pattern; yellowing of skin or eyes; dark urine or pale stool; or lack of improvement or worsening or condition. Breast-feeding precaution: Consult prescriber if breast-feeding.
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
Nursing: Physical Assessment/Monitoring
Assess effectiveness and interactions of other medications patient may be taking. Monitor effectiveness of therapy and adverse reactions at beginning of therapy and periodically with long-term use. Assess knowledge/teach patient appropriate use, interventions to reduce side effects, and adverse symptoms to report.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
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
Claritin® Hives Relief: 10 mg [DSC]
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:
Alavert® Allergy 24 Hour: 10 mg [dye free, gluten free, sucrose free; contains phenylalanine 8.4 mg/tablet; Citrus Burst™ and mint flavors]
Alavert® Children's Allergy: 10 mg [dye free, gluten free, sucrose free; contains phenylalanine 8.4 mg/tablet; bubblegum and Citrus Burst™ flavors]
Claritin® RediTabs® 24 Hour Allergy: 10 mg [mint flavor]
Dimetapp® ND Children's: 10 mg [contains phenylalanine 8.4 mg/tablet] [DSC]
Pricing: U.S. (www.drugstore.com)
Tablet, orally-disintegrating (Claritin Reditabs)
10 mg (10): $10.19
Tablets (Claritin)
10 mg (30): $29.99
Tablets (Loratadine)
10 mg (30): $21.99
References
“American Academy of Pediatrics Committee on Drugs. The Transfer of Drugs and Other Chemicals Into Human Milk,” Pediatrics, 2001, 108(3):776-89.
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 August 2009
Content last modified August 2009
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