ebastine

Action and Spectrum

Actions and Spectrum: 

Actions: 

• ebastine is a selective histamine H1 receptor antagonist. It works by blocking the binding of histamine to H1 receptors on various cells and tissues in the body. 
• By inhibiting histamine-mediated signaling, ebastine helps alleviate the symptoms of allergies, including sneezing, runny or itchy nose, watery eyes, and itching of the throat or nose. 

Spectrum: 

• ebastine’s primary spectrum of activity is against histamine-mediated allergic responses. 
• It is particularly effective in relieving symptoms associated with allergic conditions, such as allergic rhinitis (including both seasonal and perennial allergies) and allergic conjunctivitis. 
• ebastine’s primary focus is on alleviating symptoms related to histamine release, and it is not typically used to treat other conditions like infections or non-allergic inflammatory disorders. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Tachycardia 

Palpitation 

Dry mouth 

Abdominal Pain 

Dyspepsia 

Nausea 

Vomiting 

Hepatitis 

Cholestasis 

Dizziness 

Insomnia 

Hepatobiliary disorders 

Menstrual disorders 

Sinusitis 

Epistaxis 

Pharyngitis 

Thoracic disorders 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity 
• Pregnancy  

Caution: 

• Breastfeeding 
• Liver impairment 
• Renal impairment 
• Elderly patients 
• Alcohol & CNS depressants 
• Driving & operating machinery 
• Interaction with other medications 

Pregnancy / Lactation

Pregnancy consideration:  

The drug should be used with caution during pregnancy. 

Breastfeeding warnings:  

The drug should be used with caution during lactation. 

Pregnancy category: 

Category A: Well-controlled and satisfactory studies show no risk to the fetus in the initial or later trimester. 

Category B: There was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: There was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence, these categories of drugs need to be avoided by pregnant women.    

Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology:  

ebastine exerts its pharmacological effects primarily through its antihistamine properties. It is a selective histamine H1 receptor antagonist. This means that it binds to and blocks the action of histamine at H1 receptors without significantly affecting other types of receptors. 

Histamine Receptors: Histamine is a naturally occurring chemical in the body that plays a role in various physiological processes, including regulating allergic reactions and inflammation. Histamine exerts its effects by binding to specific receptors, including H1 receptors. 

Pharmacodynamics: 

• Antihistamine Action: By blocking H1 receptors, ebastine inhibits the actions of histamine. It reduces the symptoms associated with histamine release, such as itching, sneezing, runny nose, and itchy or watery eyes. ebastine is particularly effective against allergies, including allergic rhinitis (hay fever) and allergic conjunctivitis. 
• Low Sedative Effects: Second-generation antihistamines like ebastine are often called “non-sedating” or “less-sedating” antihistamines. They are designed to have a reduced propensity to cause sedation or drowsiness compared to first-generation antihistamines. However, individual responses can vary; some may still experience mild drowsiness with ebastine. 

Pharmacokinetics: 

Absorption 

• ebastine is administered orally in tablets or other oral dosage forms. 
• It is well-absorbed from the gastrointestinal tract after oral administration. 
• Absorption of ebastine is relatively slow, with peak plasma concentrations (Cmax) typically reached within 3 to 4 hours. 

Distribution 

• Both ebastine and carebastine are distributed throughout the body, including various tissues and body fluids. 
• The active metabolite, carebastine, is highly lipophilic, contributing to its ability to cross cell membranes and distribute into tissues. 

Metabolism 

ebastine is metabolized primarily in the liver, where it undergoes hepatic biotransformation. 

The primary metabolic pathway involves the conversion of ebastine into its active metabolite, carebastine, primarily via the action of cytochrome P450 (CYP) enzymes, particularly CYP2J2 and CYP3A4. Carebastine is responsible for the antihistaminic effects. 

Elimination and Excretion 

• The elimination of ebastine and its metabolites primarily occurs through renal excretion (urine) and feces. 
• The elimination half-life of ebastine is relatively short, typically around 3 to 5 hours. 

Adminstartion

Administration: 

• Dosage: A healthcare provider usually prescribes ebastine dosage based on the type and severity of your allergic symptoms, age, and other factors. Always take the prescribed dose as directed. 
• Timing: ebastine is usually taken once daily. The specific time of day can vary, but it is often taken in the morning.  
• Empty Stomach: ebastine is typically more effectively absorbed when taken on an empty stomach, meaning about 1 hour before or 2 hours after a meal. However, if stomach upset occurs when taking ebastine on an empty stomach, it can be taken with food. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: ebastine 

Pronounced as: e-bas-teen 

Why do we use ebastine? 

ebastine is a medication primarily used to relieve allergy symptoms. It belongs to a class of drugs known as antihistamines, and its primary mode of action is to block the effects of histamine, a natural substance in the body that plays a crucial role in allergic reactions. Here are the main reasons why ebastine is used: 

• Allergic Rhinitis: ebastine is commonly used to treat the symptoms of allergic rhinitis, both seasonal and perennial.  
• Allergic Conjunctivitis: ebastine is effective in managing allergic conjunctivitis. Allergic conjunctivitis often accompanies allergic rhinitis, and ebastine can help relieve eye-related allergy symptoms. 
• Seasonal and Perennial Allergies: ebastine is suitable for both seasonal allergies (caused by specific allergens present during certain times of the year) and perennial allergies (caused by allergens that are present year-round, such as dust mites or pet dander). 
• Non-Sedating Antihistamine: ebastine is classified as a second-generation antihistamine, which means it is designed to have a reduced tendency to cause drowsiness or sedation compared to first-generation antihistamines like diphenhydramine. This makes it suitable for daytime use without causing significant impairment of alertness.