Name: Blue Illustrative Innovations in Medicine Presentation
Uploaded: 2024-06-01
Duration: 7 min 39 s
Description: 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..

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.. 

Scene 1

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.. 

Scene 2

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.

Kestine'10mg
(Ebastine)
Laboratorios Almirall S.A.
Non-Sedating
10 Film Coated Tablets
Allergy Relief Medicine

[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. 

Scene 3

Taken Orally  It is absorbed in the gastrointestinal tract

Distributed throughout the body (90 to 143L)

Rectal and Fecal Elimination
 E. Half Life: Single dose (10mg) = 10.3 to 19 hrs Multiple dose(10mg) = 19hrs

Carebastine is an active metabolite of ebastineand a histamine H1 receptor antagonist.. 

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Carebastine is an active metabolite of ebastineand a histamine H1 receptor antagonist.

It is formed from ebastine by the cytochrome P450 (CYP) isoform CYP3A4.2

Carebastine inhibits histamine-induced contraction of isolated guinea pig trachea. It is  used at concentrations ranging from 30 to 100 µM.

EBASTINE
4. CHEMISTRY
H3C
HYDROXYLATION
(CYP2J2)
o
CAREBASTINE
HYDROXYEBASTINE
OH

[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.. 

Scene 5

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. 

Scene 6

MODE OF ac.T10N
EBASTINE
NH2
HISTAMINE
BLOCKING HI RECEPTOR
ANTIHISTAMINE
ANTAGONISE ALL ACTIONS OF HISTAMINE
NO RESPONSE

[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.. 

Scene 7

[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.. 

Scene 8

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.

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.. 

Scene 9

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.. 

Scene 10

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.

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.

[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. 

Scene 11

1.    Headache  2.    Drowsiness (though less common compared to other antihistamines)  3.    Dry Mouth  4.    Pharyngitis (sore throat) Nausea

1.    Dizziness 2.    Abdominal Pain 3.    Dyspepsia (indigestion) 4.    Insomnia 5.    Rhinitis (nasal inflammation)

1.    QT Interval Prolongation  2.    Hypersensitivity Reactions  3.    Hepatic Dysfunction   4.    Tachycardia (fast heart rate) 5.    Palpitations

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.. 

Scene 12

Oral Adults: 10-20 mg once daily Child >6 years: 5 mg once daily.

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.

[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. 

Scene 13

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 (e.g., cholinergic urticaria, delayed pressure urticaria)  Insect Bite Allergies Food Allergies  Drug Allergies  Mastocytosis Nasal Polyps

[Audio] Thank you for your attention
We Hope You Get The Most Benefit Out Of This Video
Meet You In Another Video
Goodbye. 

Scene 14

Blue Illustrative Innovations in Medicine Presentation

Scene 0

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.

avatar

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

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.

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

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.

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.

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.

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.

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

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.

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

Thank you for your attention
We Hope You Get The Most Benefit Out Of This Video
Meet You In Another Video
Goodbye