Ebastine; Uses, Dosage, Side Effects, Interactions

Ebastine is a non-sedating H1 antihistamine. It does not penetrate the blood-brain barrier and thus allows an effective block of the H1 receptor in peripheral tissue without a central side effect, i. e not causing sedation or drowsiness. The basic patent for ebastine in Europe is EP-B-134124. It is often provided in the micronized form, due to poor water solubility. CYP2J2, an arachidonic acid epoxygenase, is recognized for its role in the first-pass metabolism of astemizole and ebastine. Ebastine is under investigation for the treatment of Irritable Bowel Syndrome (IBS). Ebastine has been investigated for the treatment of Urticaria.

This compound belongs to the class of organic compounds known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.

Mechanism of Action of Ebastine

Ebastine, a piperidine derivative, is a long-acting, nonsedating, second-generation histamine receptor antagonist that binds preferentially to peripheral H₁ receptors. It is metabolized to the active metabolite, carebastine. It has antihistaminic, antiallergic activity and prevents histamine-induced bronchoconstriction. It does not have significant sedative or antimuscarinic actions.

Indications of Ebastine

• Allergic rhinitis
• Seasonal allergic conditions
• Chronic idiopathic urticaria
• Chronic itching
• Asthma
• Ebastine may also be used for purposes not listed here.
• Conjunctivitis,
• Both seasonal and perennial (nasal discharge, nasal itching, eye itching, weeping, sneezing, etc.),
• Chronic urticaria
• Allergic dermatitis.
• Inflammatory dermatoses
• Pruritis
• Allergic symptoms like urticaria,
• Rhinorrhea,
• Sneezing and itching
• Skin itching
• Itching of the skin
• Itching skin
• Runny nose
• Sneezing

Ebast (Ebastine) is indicated for hay fever (perennial or seasonal allergic rhinitis), idiopathic chronic urticaria (hives) and atopic dermatitis (a type of eczema). In addition to this, some people have used it for asthma or certain autoimmune diseases. This medicine is a type of second-generation H1 antihistamine which is considered to be non-drowsy. When ingested, it is converted into carebastine, its active metabolite. It works by inhibiting histamine, which in turn helps to provide relief from allergies and symptoms of the conditions listed here

Contra-Indications of Ebastine

• Cardiac arrhythmias.
• Hypersensitivity
• Stomach Cancer
• Porphyria
• Liver Problems
• Kidney disease witha reduction in kidney function
•  AllergiesHistamine H2 Inhibitors

Dosages of Ebastine

Strengths : Tabs: 10 mg, 20 mg, 120 mg,

Caps: 10 mg,

Syrup: 5 mg/5ml,

Allergic conditions

• Adult: 10-20 mg once daily.
• Child: >6 yr: 5 mg once daily.

Children older than 12 years 

• Kestine 10mg tablet or 10 ml (2 teaspoonfuls) Kestine Syrup once daily. In severe symptoms Kestine 20mg tablet or 20 ml Kestine Syrup (4 teaspoonfuls) once daily.

Children from 6 to 11 years old

• One 5 ml dose (equivalent to Ebastine 5 mg) once daily.

Children from 2 to 5 years old

• One 2.5 ml dose (equivalent to Ebastine 2.5 mg) once daily.

Side Effects of Ebastine

The most common

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

More common

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

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 ofthroat, fever, hoarseness, runny nose, tender swollen glands in neck, trouble in swallowing, voice changes.
• somnolence, such as, sleepiness or unusual drowsiness
• nausea

Drug Interactions of Ebastine

• amiodarone
• antihistamines (e.g,. cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
• antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine,risperidone)
• “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
• barbiturates (e.g., butalbital, pentobarbital phenobarbital)
• benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
• general anesthetics (medications used to put people to sleep before surgery)
• ipratropium
• ketotifen
• mirabegron
• mirtazapine
• muscle relaxants (e.g., cyclobenzaprine, methocarbamol, orphenadrine)
• narcotic pain relievers (e.g., codeine, fentanyl, morphine, oxycodone)
• seizure medications (e.g., clobazam, ethosuximide, felbamate, levetiracetam, phenobarbital, phenytoin, primidone, topiramate, valproic acid, zonisamide)
• selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine, fluoxetine,paroxetine, sertraline)
• sleeping medications (e.g., zolpidem, zopiclone)
• tapentadol
• thiazide diuretics (water pills; e.g., hydrochlorothiazide, indapamide, metolazone)
• tiotropium
• tolterodine
• tramadol
• tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
• fluconazole
• fluvastatin
• irbesartan
• losartan
• omeprazole
• phenytoin
• tocilizumab
• trimethoprim
• zafirlukast