Allopathy
Prescription Required
DCGI (Drugs Controller General of India)
Schedule H
Levocabastine is an H1-Receptor Antihistamine.
It is used to treat Allergic rhinitis.
The Systemic availability is 60-80% (nasal); 30-60% (ocular).
The Protein-binding is 55%. Trace amounts detected in breast milk.
and get mainly excreted via urine (70% as unchanged drug, 10% as metabolites); via faeces (20% as unchanged drug). 35-40 hr (elimination half-life).
Levocabastine shows common side effects like Transient stinging and burning of the eyes, urticaria, dyspnoea, drowsiness and headache.
Levocabastine is available in the form of nasal solution.
Levocabastine is available in India, Germany, Canada, Italy.
Levocabastine is a potent, selective histamine H1-receptor antagonist. It works by competing with histamine for H1-receptor sites on effector cells. It thereby prevents, but does not reverse, responses mediated by histamine alone. Levocabastine does not block histamine release but, rather, prevents histamine binding and activity. Levocabastine also binds neurotensin receptors and serves as a neurotensin agonist. This can induce some degree of analgesia.
Levocabastine is available in the form of nasal solution.
Intranasal: Shake bottle well before each use. Prior to initial use, bottle should be primed until a fine spray is delivered. Instruct patients to blow nose and clear nasal passages before administering spray and to inhale nasally while spraying
It is used in to prevent and treat Anaphylaxis, Insomnia, it is also used to treat Angioedema, allergic (acute); Infusion- or transfusion-related reactions; Nausea and vomiting, pregnancy associated, severe or refractory; Scombroid (histamine) poisoning; Urticaria, new onset and chronic spontaneous; Vertigo, acute episodes
Levocabastine is a potent, selective histamine H1-receptor antagonist. It works by competing with histamine for H1-receptor sites on effector cells. It thereby prevents, but does not reverse, responses mediated by histamine alone. Levocabastine does not block histamine release but, rather, prevents histamine binding and activity. Levocabastine also binds neurotensin 2 receptors and serves as a neurotensin agonist. This can induce some degree of analgesia.
Levocabastine is approved for use in the following clinical indications
- Allergic rhinitis: Symptomatic treatment of allergic rhinitis in patients 12 years and older.
Nasal
Allergic rhinitis
Adult: Spray 0.05% suspension in each nostril bid; increase to 3-4 times daily if necessary.
Child: ≥9 yr: Spray 0.05% suspension in each nostril bid; increase to 3-4 times daily if necessary.
Ophthalmic
Allergic conjunctivitis
Adult: Instil 1 drop of 0.05% suspension in the affected eye(s) bid; increase to 3-4 times daily if necessary. Discontinue if there is no improvement within 3 days.
Child: ≥9 yr: Instil 1 drop of 0.05% suspension in the affected eye(s) bid; increase to 3-4 times daily if necessary. Discontinue if there is no improvement within 3 days.
Levocabastine is available in various strengths as 4ml, 10 ml
Levocabastine is available in the form of nasal solution.
Dosage Adjustment in Hepatic impairment Patient
- There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied); however, use caution in severe impairment due to the potential for altered pharmacokinetics.
Dosage Adjustment for Pediatric Patients
Allergic rhinitis: Children ≥12 years and Adolescents: Intranasal: Refer to adult dosing.
Hypersensitivity to Levocabastine , other structurally related antihistamines, or any component of the formulation; neonates or premature infants; breast-feeding
Additional contraindications: Parenteral: Use as a local anesthetic
OTC labeling: When used for self-medication, do not use in children <6 years, to make a child sleep, or with any other Levocabastine -containing products (including topical products)
Disease-related concerns:
- Renal impairment: Use caution; limited data available regarding use in this population.
Alcohol Warning
Levocabastine is only indicated for use in premature neonates.
Breast Feeding Warning
Following intranasal application, minute amounts of levocabastine have been detected in human breast milk. The manufacturer recommends that caution be exercised when administering levocabastine to nursing women.
Pregnancy Warning
Levocabastine is only indicated for use in premature neonates.
Food Warning
High-fat meal may decrease the rate but not the extent of absorption. Management: May administer with meals.
Common Adverse effects:
Transient stinging and burning of the eyes, urticaria, dyspnoea, drowsiness and headache.
The common side effects of Levocabastine include the following Transient stinging and burning of the eyes, urticaria, dyspnoea, drowsiness and headache.
Pharmacodynamic
Levocabastine is a selective histamine H1-receptor antagonist exerting inhibitory effects on the release of chemical mediators from mast cells and on the chemotaxis of polymorphonuclear leukocytes and eosinophils. Both histamine and antigens induced conjunctivitis can be inhibited by levocabastine. Levocabastine can also reduce symptoms of allergic rhinitis by preventing an increase in vascular permeability of nasal mucosa..
Pharmacokinetics
- Absorption: Systemic availability: 60-80% (nasal); 30-60% (ocular).
- Distribution: Protein-binding: 55%. Trace amounts detected in breast milk.
- Excretion: Mainly via urine (70% as unchanged drug, 10% as metabolites); via faeces (20% as unchanged drug). 35-40 hr (elimination half-life).
- https://clinicaltrials.gov/ct2/show/NCT04430790
- https://clinicaltrials.gov/ct2/show/NCT02820025
- https://pubmed.ncbi.nlm.nih.gov/27612991/
- https://clinicaltrials.gov/ct2/show/NCT03894189
- https://www.rxlist.com/dopram-drug.htm
- https://www.mims.com/india/drug/info/Levocabastine ?type=full&mtype=generic
- https://go.drugbank.com/drugs/DB00561
- https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7003846/
