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Levocetirizine is a third generation, non-sedating, selective histamine H1 receptor antagonist, with an antihistamine, infection, or irritation, often causing pain, swelling, heat, or redness. সহজ বাংলা: শরীরের প্রদাহ; ব্যথা, ফোলা বা লালভাব হতে পারে।" data-rx-term="inflammation" data-rx-definition="Inflammation is the body’s response to injury, infection, or irritation, often causing pain, swelling, heat, or redness. সহজ বাংলা: শরীরের প্রদাহ; ব্যথা, ফোলা বা লালভাব হতে পারে।">inflammation, pain, or swelling. সহজ বাংলা: প্রদাহ/ফোলা/ব্যথা কমায়।" data-rx-term="anti-inflammatory" data-rx-definition="Anti-inflammatory means reducing inflammation, pain, or swelling. সহজ বাংলা: প্রদাহ/ফোলা/ব্যথা কমায়।">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 infection, or irritation, often causing pain, swelling, heat, or redness. সহজ বাংলা: শরীরের প্রদাহ; ব্যথা, ফোলা বা লালভাব হতে পারে।" data-rx-term="inflammation" data-rx-definition="Inflammation is the body’s response to injury, infection, or irritation, often causing pain, swelling, heat, or redness. সহজ বাংলা: শরীরের প্রদাহ; ব্যথা, ফোলা বা লালভাব হতে পারে।">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
Very rare clinical data on exposed pregnancies are available. Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/fetal development, parturition or postnatal development. Caution should be exercised when prescribing to pregnant or breastfeeding women because levocetirizine passes into breast milk.
Lactation
Levocetirizine is the R-enantiomer of cetirizine. Small occasional doses of levocetirizine are probably acceptable during breastfeeding. Larger doses or more prolonged use may cause drowsiness and other effects in the infant or decrease the milk supply, particularly in combination with a sympathomimetic such as pseudoephedrine or before lactation is well established.
References
