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Loratadine

Pronunciation

Pronunciation: lore-AT-uh-DEEN
Class: Piperidine, peripherally selective

For Professionals Side Effects Interactions More...

Trade Names

Alavert
- Tablets, orally disintegrating 10 mg

Children's Loratadine
- Syrup 5 mg per 5 mL

Claritin
- Tablets 10 mg
- Syrup 1 mg/mL

Claritin Hives Relief
- Tablets 10 mg

Claritin Non-Drowsy Allergy
- Tablets 10 mg

Claritin Non-Drowsy Liqui-Gels
- Capsules, liquid-filled 10 mg

Claritin RediTabs
- Tablets, rapidly disintegrating 5 mg

Loratadine Hives Relief
- Solution, oral 5 mg

Non-Drowsy Allergy
- Tablets 10 mg

Non-Drowsy Allergy Relief for Kids
- Syrup 5 mg per 5 mL

Apo-Loratadine (Canada)
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) approximately 40%; however, T _max is delayed 1 h. Steady state is reached by approximately 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

Approximately 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 92 h).

Onset

Rapid.

Special Populations

Renal Function Impairment

With CrCl less than 30 mL/min, AUC and C _max are increased approximately 73% for loratadine and 120% for its metabolite.

Hepatic Function Impairment

AUC and C _max doubled for loratadine; t _½ is 24 h (loratadine) and 37 h (metabolite).

Elderly

AUC 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 urticaria and chronic idiopathic urticaria.

Contraindications

None well documented.

Dosage and Administration

Adults and children 6 y of age and older

PO 10 mg (syrup, 10 mL) daily (max, 10 mg/day).

Children 2 to 5 y of age

PO 5 mg (syrup, 5 mL) daily.

Hepatic Impairment
Adults and children 6 y of age and older

PO Start with 10 mg (syrup, 10 mL) every other day.

Children 2 to 5 y of age

PO Start with 5 mg (syrup, 5 mL) every other day.

Renal Impairment (Glomerular Filtration Rate Less Than 30 mL/min)
Adults and children 6 y of age and older

PO Start with 10 mg (syrup, 10 mL) every other day.

Children 2 to 5 y of age

PO Start with 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 and liquid-filled capsules at 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 depressants

Additive CNS depressant effects.

Azole antifungals (eg, ketoconazole, itraconazole)

Use of these agents with similar antihistamines has resulted in serious cardiac toxicity, including death.

Cimetidine

Concomitant use may increase plasma levels of loratadine.

Erythromycin

Loratadine plasma levels, including metabolite, may be increased.

Food

May 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 y of age (tablets) or younger than 2 y 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.