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Ebastine Indications Contraindications, Warning

Ebastine Indications Contraindications/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

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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, c ough, dryness or soreness of throat, fever, hoarseness, runny nose, tender swollen glands in neck, trouble in swallowing, voice changes.
somnolence, such as, sleepiness or unusual drowsiness
nausea

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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

Pregnancy & Lactation

FDA pregnancy category C

Pregnancy

Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.

Lactation

Betamethasone has not been well studied during breastfeeding after systemic or topical use. Systemic betamethasone is best avoided in favor of one of the shorter-acting and better studied alternatives because of its potency and low protein binding which would favor its passage into milk.