undefined. [Audio] Hi! Today we will be discussing a second gen antihistamine namely Ebastine. We will discuss its pharmacokinetics dynamics as well as dose along with its side effects..
Ebastine was manufactured in the laboratories of Almirall S.A. This drug belongs to Anti-histaminic class. It provides relief from allergies without causing drowsiness. It works excellently against allergic rhinitis and chronic idiopathic urticaria, conditions that make the simple act of breathing a challenge for many. In 1990, after years of trials and improvements, Ebastine was ready to step into the world as a beacon of hope for those suffering from allergies..
[Audio] Pharmacokinetics Administration Taken Orally It is absorbed in the gastrointestinal tract Half Life 1.5 to 4 hours Protein Binding = >95% Distribution Distributed throughout the body (90 to 143L) Elimination Rectal and Fecal Elimination E Half Life: Single dose (10 milligrams) = 10.3 to 19 hrs Multiple dose(10 milligrams) = 19hrs.
Carebastine is an active metabolite of ebastineand a histamine H1 receptor antagonist..
[Audio] Pharmacodynamics H1 receptor antagonists work by binding to the H1 receptors on cells and preventing histamine from attaching to these receptors. Thus blocking the histamine-mediated allergic response and helps alleviate symptoms associated with allergies. H1 receptor antagonists are commonly used to treat allergic conditions such as hay fever allergic rhinitis hives and allergic conjunctivitis. They can also be used to manage symptoms of non-allergic conditions like motion sickness and insomnia..
[Audio] Mode Of Action We Can See That The Anti Histamine Gets Attached With H1 Receptor Blocking Binding Of Histamine With The Receptor Resulting In Antagonsim Of All Actions Of Histamine.
[Audio] Interactions Cytochrome P450 3A4 inducers Examples: Acetaminophen Betamethasone Corticotropin Tocilizumab Effects: These inducers can decrease the plasma level of ebastine by increasing its metabolism potentially reducing its efficacy. Cytochrome P450 3A4 inhibitors Examples: Abametapir Bromocriptine Patupilone Zafirlukast Zimelidine. Effects: These inhibitors can increase plasma levels of ebastine and its active metabolite carebastine by reducing their metabolism. This can enhance the effects and side effects of ebastine potentially leading to increased risk of adverse reactions..
[Audio] Drug-Condition Interactions Cardiovascular Conditions QT Prolongation Ebastine can prolong the QT interval so it should be used with caution in patients with pre-existing cardiovascular conditions or those taking other drugs known to prolong the QT interval. Hepatic Impairment: Since ebastine is metabolized in the liver patients with liver impairment may have increased plasma levels of the drug and its metabolite requiring dose adjustments..
[Audio] Contraindications Hypersensitivity: Known Allergy: Ebastine is contraindicated in individuals with a known hypersensitivity or allergy to ebastine or any of the excipients in the formulation. Hypersensitivity reactions may include rash itching swelling or severe allergic reactions such as anaphylaxis. Severe Hepatic Impairment: Patients with severe hepatic impairment should not take ebastine. This is due to the fact that ebastine is extensively metabolized in the liver and severe hepatic dysfunction can lead to significantly altered drug metabolism and increased risk of adverse effects. QT Interval Prolongation: Ebastine is contraindicated in patients with a known history of QT interval prolongation or those who have conditions that predispose them to QT prolongation such as congenital long QT syndrome. This contraindication is crucial because ebastine can prolong the QT interval increasing the risk of potentially fatal arrhythmias like Torsades de Pointes..
[Audio] Contraindications Severe Renal Impairment Kidney Function While not always a strict contraindication caution is advised and dose adjustments may be necessary in patients with severe renal impairment due to potential accumulation of the drug and its metabolites. Pregnancy and Lactation Although not absolute contraindications ebastine should be used during pregnancy and lactation only if the potential benefits outweigh the risks. Consultation with a healthcare provider is essential..
[Audio] Adverse Effects Common Adverse Effects 1. Headache 2. Drowsiness (though less common compared to other antihistamines) 3. Dry Mouth 4. Pharyngitis (sore throat) Nausea Less Common Adverse Effects: 1. Dizziness 2. Abdominal Pain 3. Dyspepsia (indigestion) 4. Insomnia 5. Rhinitis (nasal inflammation) Rare Adverse Effects 1. QT Interval Prolongation 2. Hypersensitivity Reactions 3. Hepatic Dysfunction 4. Tachycardia (fast heart rate) 5. Palpitations Very Rare Adverse Effects: 1. Anaphylaxis (a severe potentially life-threatening allergic reaction) 2. Severe Skin Reactions (such as Stevens-Johnson syndrome) 3. Liver Toxicity.
[Audio] Children age restrictions The safety and efficacy of ebastine in children under a certain age (usually below 12 years) have not been established so it should be used with caution or avoided in this population unless specifically indicated and supervised by a healthcare provider. Dosing Oral Adults: 10-20 milligrams once daily Child >6 years: 5 milligrams once daily..
[Audio] Clinical Uses Seasonal Allergic Rhinitis (Hay Fever) Perennial Allergic Rhinitis Chronic Idiopathic Urticaria Allergic Conjunctivitis Dermographism (Dermatographic Urticaria) Atopic Dermatitis (as an adjunct to other treatments) Cold Urticaria Physical Urticarias (for example cholinergic urticaria delayed pressure urticaria) Insect Bite Allergies Food Allergies Drug Allergies Mastocytosis Nasal Polyps.
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