Loratadine
Pronouncation: (lore-AT-uh-DEEN)Class: Piperidine, peripherally selective
Trade Names:
Alavert
- Tablets, orally disintegrating 10 mg
Trade Names:
Children's Loratadine
- Syrup 5 mg per 5 mL
Trade Names:
Claritin
- Tablets 10 mg
- Syrup 1 mg/mL
Trade Names:
Claritin Hives Relief
- Tablets 10 mg
Trade Names:
Claritin Non-Drowsy Allergy
- Tablets 10 mg
Trade Names:
Claritin RediTabs
- Tablets, rapidly disintegrating 5 mg
Trade Names:
Clear-Atadine
- Tablets 10 mg
Trade Names:
Non-Drowsy Allergy Relief for Kids
- Syrup 5 mg per 5 mL
Trade Names:
Tavist ND
- Tablets 10 mg
Claritin Kids (Canada)
Pharmacology
Competitively antagonizes histamine at the H 1 -receptor site.
Pharmacokinetics
Absorption
Rapidly absorbed following oral administration. T max is 1.3 h for loratadine and 2.5 h for its metabolite. Food increases bioavailability (AUC) about 40%; however, T max is delayed 1 h. Steady state is reached by about the fifth dosing day.
Distribution
97% protein bound.
Metabolism
Metabolite is descarboethoxyloratadine. Metabolized by CYP-450 3A4 and P450 2D6. Undergoes extensive first-pass metabolism.
Elimination
About 80% equally distributed between urine and feces in the form of metabolic products within 10 days. The t ½ for loratadine is 8.4 h (3 to 20 h). The t ½ for descarboethoxyloratadine is 28 h (8.8 to 92ߙh).
Onset
Rapid.
Special Populations
Renal Function ImpairmentWith CrCl less than 30 mL/min, AUC and C max are increased approximately 73% for loratadine and 120% for its metabolite.
Hepatic Function ImpairmentAUC and C max doubled for loratadine; t ½ is 24 h (loratadine) and 37 h (metabolite).
ElderlyAUC and C max are increased approximately 50%, and t ½ ranged from 6.7 to 37 h.
Indications and Usage
Temporarily relieves symptoms caused by hay fever or other upper respiratory allergies (runny nose, sneezing, itchy/watery eyes, itching of the nose or throat); treatment of chronic idiopathic urticaria.
Contraindications
Standard considerations.
Dosage and Administration
Adults and children 6 yr of age and olderPO 10 mg/day.
Children 2 to 5 yr of agePO 5 mg (syrup, 5 mL) daily.
Hepatic ImpairmentAdults and children 6 yr of age and older
PO Start with 10 mg every other day.
Children 2 to 5 yr of agePO 5 mg (syrup, 5 mL) every other day.
Renal Impairment (Glomerular Filtration Rate Less Than 30ߙmL/min)Adults and children 6 yr of age and older
PO Start with 10 mg every other day.
Children 2 to 5 yr of agePO 5 mg (syrup, 5 mL) every other day.
General Advice
- Do not administer orally-disintegrating tablet to patient with phenylketonuria without first discussing with health care provider.
- Administer without regard to meals. Administer with food if GI upset occurs.
- Measure and administer prescribed dose of syrup using dosing syringe, dosing spoon, or dosing cup.
- Remove orally- or rapidly-disintegrating tablet from blister just before administration. Have patient place on tongue and allow tablet to dissolve. May administer with or without water.
Storage/Stability
Store tablets between 36° and 86°F. Store orally-disintegrating tablets at controlled room temperature (68° to 77°F). Store syrup and rapidly-disintegrating tablets between 36° and 77°F. Do not remove orally-disintegrating or rapidly-disintegrating tablet from blister until just prior to administration.
Drug Interactions
Alcohol, CNS depressantsAdditive CNS depressant effects.
Azole antifungals (eg, ketoconazole, itraconazole)Use of these agents with similar antihistamines has resulted in serious cardiac toxicity, including death.
CimetidineConcomitant use may increase plasma levels of loratadine.
ErythromycinLoratadine plasma levels, including metabolite, may be increased.
FoodMay increase absorption of loratadine.
Laboratory Test Interactions
May prevent or diminish otherwise positive reactions to dermal reactivity indicators.
Adverse Reactions
Cardiovascular
Hypotension; hypertension; palpitations; tachycardia; syncope.
CNS
Headache (12%); somnolence (8%); fatigue, nervousness (4%); hyperkinesia (3%); paresthesia; dizziness; migraine; tremor; vertigo; impaired concentration; depression; agitation; anxiety; confusion; insomnia; seizures (postmarketing).
Dermatologic
Dermatitis; dry hair; dry skin; urticaria; rash; pruritus; purpura; photosensitivity; increased sweating; alopecia, erythema multiforme (postmarketing).
EENT
Conjunctivitis, dysphonia (2%); blurred vision; earache; eye pain; blepharospasm; altered taste.
GI
Dry mouth (3%); abdominal pain (2%); anorexia; increased appetite and weight gain; nausea; vomiting; diarrhea; constipation; flatulence; gastritis; dyspepsia; thirst; hiccough; stomatitis.
Genitourinary
Urinary discoloration; altered micturition; menstrual irregularities; impotence; vaginitis; urinary retention; urinary incontinence; breast enlargement (postmarketing).
Hepatic
Abnormal hepatic function, including jaundice, hepatitis, hepatic necrosis (postmarketing).
Respiratory
Wheezing (4%); upper respiratory tract infection (2%); nasal dryness; pharyngitis; epistaxis; nasal congestion; dyspnea; coughing; rhinitis; hemoptysis; sinusitis; sneezing; bronchospasm; bronchitis; laryngitis.
Miscellaneous
Breast pain; arthralgia; myalgia; malaise; chest pain; leg cramps; asthenia; back pain; fever; peripheral edema (postmarketing).
Precautions
Pregnancy
Category B .
Lactation
Excreted in breast milk.
Children
Safety and efficacy not established in children younger than 6 yr of age (tablets) or younger than 2 yr of age (syrup).
Hypersensitivity
Hypersensitivity may occur.
Renal Function
Use drug with caution in patients with renal impairment.
Hepatic Function
Use drug with caution in patients with hepatic renal impairment.
Special Risk Patients
Use with caution in patients with a predisposition to urinary retention, history of bronchial asthma, increased IOP, hyperthyroidism, CV disease, or hypertension.
Overdosage
Symptoms
Somnolence, tachycardia, headache, extrapyramidal signs, palpitations.
Patient Information
- Warn patient not to increase dose to obtain quicker relief of symptoms.
- If patient is to have allergy skin testing, advise to avoid taking medication for 4 days before test.
- Tell patient that drug may be used alone for symptoms of sneezing and runny nose with slight nasal congestion.
- Instruct patient to maintain fluid intake of 1.5 to 2 qt/day to decrease viscosity of secretions.
- Caution patient to avoid exposure to sunlight and to use sunscreen or wear protective clothing to avoid photosensitivity reaction.
- Instruct patient to avoid intake of alcoholic beverages or other CNS depressants (eg, sedatives, hypnotics, tranquilizers).
- Advise patient that drug may cause drowsiness and to use caution while driving or performing other tasks requiring mental alertness until response to medication is known.
- Explain that rapidly-disintegrating tablet will disintegrate on the tongue and may be administered with or without water.
- Advise patient to take frequent sips of water, suck on ice chips or sugarless hard candy, or chew sugarless gum if dry mouth occurs.
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More Loratadine resources:
Loratadine - Includes detailed dosage instructions.
