Levocetirizine; Uses, Dosage, Side Effects, Drug Interactions

Levocetirizine is a third generation, non-sedating, selective histamine H1 receptor antagonist, with an antihistamine, anti-inflammatory, and potential anti-angiogenic activities. Levocetirizine competes with endogenous histamine for binding at peripheral H1-receptor sites on the effector cell surface. This prevents the negative symptoms associated with histamine release and an allergic reaction. In addition, as histamine plays an important role in angiogenesis during an allergic inflammatory reaction, blocking the action of histamine may modulate the expression of proangiogenic factors and thus may prevent angiogenesis. As a third-generation histamine H1 receptor antagonist, levocetirizine has fewer side effects than most second-generation antihistamines.

Levocetirizine is a third-generation non-sedative antihistamine indicated for the relief of symptoms associated with seasonal and perennial allergic rhinitis and uncomplicated skin manifestations of chronic idiopathic urticaria. It was developed from the second-generation antihistamine cetirizine. Levocetirizine is the R-enantiomer of the cetirizine racemate. Levocetirizine is an inverse agonist that decreases activity at histamine H1 receptors. This, in turn, prevents the release of other allergy chemicals and increased blood supply to the area, and provides relief from the typical symptoms of hay fever.

Mechanism of action of Levocetirizine

Levocetirizine, the active enantiomer of cetirizine, is an antihistamine; its principal effects are mediated via selective inhibition of H1 receptors. The antihistaminic activity of levocetirizine has been documented in a variety of animal and human models. In vitro binding studies revealed that levocetirizine has an affinity for the human H1-receptor 2-fold higher than that of cetirizine (Ki = 3 nmol/L vs. 6 nmol/L, respectively). This increased affinity has unknown clinical relevance.

Indications of Levocetirizine

• Chronic idiopathic urticaria
• Perennial allergic rhinitis
• Seasonal allergic rhinitis
• Urticaria
• Allergies
• Allergic rhinitis
• Perennial allergic rhinitis
• Pollen allergy
• Sneezing
• Runny nose
• Itchy or watery eyes
• Itchy throat or nose
• Upper respiratory tract hypersensitivity reaction, site unspecified
• Rhinorrhea
• Postnasal discharge,
• Nasal pruritus,
• Ocular pruritus & tearing

Contra-Indications of Levocetirizine

• End-Stage Renal Disease
• enlarged prostate with urination problem
• Cannot Empty Bladder
• moderate to severe kidney impairment
• Hemodialysis with High-Flux Membrane

Allergies to

• Antihistamines
• Antihistamines – Piperazine

Dosages of Levocetirizine

Strengths: 2.5 mg; 5 mg; 0.5 mg/mL

Urticaria

• 5 mg orally once a day in the evening

Allergic Rhinitis

Seasonal Allergic Rhinitis (OTC)

• 5 mg orally once a day in the evening; some patients may be adequately controlled on 2.5 mg once a day

Pediatric Dose for Allergic Rhinitis

Perennial Allergic Rhinitis

• 6 months to 2 years: 1.25 mg orally once a day in the evening

Seasonal Allergic Rhinitis (OTC)

• 6 to 11 years: 2.5 mg orally once a day in the evening
• 12 years or older: 5 mg orally once a day in the evening; some patients may be adequately controlled on 2.5 mg once a day.

Urticaria

• 6 months to 5 years: 1.25 mg orally once a day in the evening
• 6 to 11 years: 2.5 mg orally once a day in the evening
• 12 years or older: 5 mg orally once a day in the evening; some patients may be adequately controlled on 2.5 mg once a day

Side Effects of Levocetirizine

The most common

• headache,
• drowsiness,
• fatigue
• dry mouth.
• Sleepiness
• Stomach pain
• Headache
•  Diarrhea
• An opposite reaction in which you feel excited, jittery, or nervous, known as paradoxical CNS stimulation instead of drowsy or sleepy

More common

• headache
• fast, pounding, or uneven heartbeat;
• fever, flu symptoms;
• seizure (convulsions)
• jaundice (yellowing of the skin or eyes).
• dry mouth, sore throat, cough;
• muscle pain;
• drowsiness, tired feeling;
• nausea,
• fever, flu symptoms;
• seizure (convulsions); or
• jaundice (yellowing of the skin or eyes).

Less common

• Dizziness
• dry mouth
• dysmenorrhea, such as, difficult or painful menstruation
• dyspepsia, such as acid or sour stomach, belching, heartburn, indigestion, stomach discomfort , upset or pain,
• fatigue, such as unusual tiredness or weakness
• myalgia, such as joint pain, swollen joints, muscle aching or cramping, muscle pains or stiffness, difficulty in moving
• pharyngitis, such as, body aches or pain, congestion, cough, dryness or soreness of throat, fever, hoarseness, runny nose, tender swollen glands in the neck, trouble in swallowing, voice changes.
• somnolence, such as sleepiness or unusual drowsiness
• nausea
• liver damage or inflammation
• tightness in the chest or breathing tube
• passing out or fainting
• seizures

Drug Interactions of Levocetirizine

Levocetirizine may interact with following drugs, supplement & may change the efficacy of drugs

Tell your doctor or pharmacist if you are taking other products that cause drowsiness such as opioid pain or cough relievers (such as codeine, hydrocodone), alcohol, marijuana, drugs for sleep or anxiety (such as alprazolam, lorazepam, zolpidem), muscle relaxants (such as carisoprodol, cyclobenzaprine), or other antihistamines (such as diphenhydramine, promethazine).

Check the labels on all your medicines (such as allergy or cough-and-cold products) because they may contain ingredients that cause drowsiness. Ask your pharmacist about using those products safely.

Do not use with any other antihistamines applied to the skin (such as diphenhydramine cream, ointment, spray) because increased side effects may occur.

Levocetirizine is very similar to hydroxyzine and cetirizine. Do not use these medications while using levocetirizine.

This medication may interfere with certain laboratory tests (including allergy skin testing), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.

Pregnancy and Lactation of Levocetirizine

FDA Pregnancy category B

Pregnancy

People Also Reading

Cetirizine; Uses, Dosage, Side Effects, Drug Interactions Ketotifen; Uses, Dosage, Side Effects, Drug Interactions Montelukast; Uses, Dosage, Side Effects, Drug Interactions Folinic Acid; Uses, Dosage, Side Effects, Drug Interactions Hydroxyzine; Uses, Dosage, Side Effects, Drug Interactions Simvastatin; Uses, Dosage, Side Effects, Drug Interactions Zafirlukast; Uses, Dosage, Side Effects, Drug Interactions Famotidine; Uses, Dosage, Side effects, Drug Interactions Lansoprazole; Uses, ,Dosage, Side Effects, Drug Interactions Oxtriphylline; Uses, Dosage, Side Effects, Drug Interactions Fluvastatin; Uses, Dosage, Side Effects, Drug Interactions Desipramine; Uses, Dosage, Side Effects, Drug Interactions