seasonal allergies: antihistamines & the future jacquelyn covarrubias chem 5389 april 24, 2007

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Seasonal Allergies: Seasonal Allergies: Antihistamines & Antihistamines & the Future the Future Jacquelyn Covarrubias Jacquelyn Covarrubias CHEM 5389 CHEM 5389 April 24, 2007 April 24, 2007

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Page 1: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

Seasonal Allergies:Seasonal Allergies:Antihistamines &Antihistamines &

the Futurethe Future

Jacquelyn CovarrubiasJacquelyn Covarrubias

CHEM 5389CHEM 5389

April 24, 2007April 24, 2007

Page 2: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

OutlineOutline

1.1. What is an Allergy?What is an Allergy?2.2. AllergensAllergens3.3. Allergic RhinitisAllergic Rhinitis4.4. Histamine and Mast CellsHistamine and Mast Cells5.5. Symptoms Symptoms 6.6. Common Structures of AntihistaminesCommon Structures of Antihistamines7.7. TreatmentsTreatments8.8. Future Ideas for Dealing with AllergiesFuture Ideas for Dealing with Allergies

Page 3: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

What is an allergy?What is an allergy? Allergies are caused by an over-sensitive immune response. Allergies are caused by an over-sensitive immune response.

The immune system normally protects the body against The immune system normally protects the body against harmful substances. Allergy symptoms occurs when the harmful substances. Allergy symptoms occurs when the immune system reacts to allergens that are generally immune system reacts to allergens that are generally harmless and in most people do not cause an immune harmless and in most people do not cause an immune response.response.

When a person with allergies breathes in an allergen such as When a person with allergies breathes in an allergen such as pollen or dust, antibodies are produced. Immunoglobulin E is a pollen or dust, antibodies are produced. Immunoglobulin E is a class of immunoglobulins that includes the antibodies elicited class of immunoglobulins that includes the antibodies elicited by an allergen. A person who has an allergy usually has by an allergen. A person who has an allergy usually has elevated blood levels of IgE. IgE antibodies attack and engage elevated blood levels of IgE. IgE antibodies attack and engage the invading army of allergens. the invading army of allergens.

When the antibodies are stimulated by pollen and dust, When the antibodies are stimulated by pollen and dust, histamine and other chemicals are released. This causes histamine and other chemicals are released. This causes itching, swelling, and mucus production. Symptoms vary from itching, swelling, and mucus production. Symptoms vary from person to person.person to person.

Page 4: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

Common AllergensCommon Allergens Airborne particles (hay Airborne particles (hay

fever) fever) – Grass, weeds, Grass, weeds,

timothy grass, birch timothy grass, birch trees, and Mold trees, and Mold sporesspores

Drugs Drugs – Penicillin, sulfonamides, Penicillin, sulfonamides,

salicylates, local salicylates, local anesthetics, and latex anesthetics, and latex

Insect stings Insect stings – bee sting venom and bee sting venom and

wasp sting venom wasp sting venom Animal products Animal products

(animal allergy) (animal allergy) – Animal hair and Animal hair and

dander, cockroach dander, cockroach calyx, and dust mite calyx, and dust mite excretionexcretion

Foods (food allergy) Foods (food allergy) – Peanuts, nuts, sesame, Peanuts, nuts, sesame,

pittster fruit, seafood pittster fruit, seafood eggs, peas, beans, eggs, peas, beans, soybeans, celery, soy, soybeans, celery, soy, milk, wheat, and cornmilk, wheat, and corn

Page 5: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

Allergic RhinitisAllergic Rhinitis

Allergic rhinitis is the fifth most Allergic rhinitis is the fifth most prevalent chronic disease in the United prevalent chronic disease in the United States, affecting up to 40 million States, affecting up to 40 million adults and children each year. adults and children each year.

Allergic rhinitis costs the nation Allergic rhinitis costs the nation approximately $5.3 billion in direct approximately $5.3 billion in direct and indirect costs (including time lost and indirect costs (including time lost from work and school) and accounts from work and school) and accounts for about 10,000 absences from for about 10,000 absences from school. school.

Page 6: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

Histamine and Mast CellsHistamine and Mast Cells When you are exposed to When you are exposed to

an allergen, a specific type an allergen, a specific type of white blood cell called the of white blood cell called the mast cell, which is located mast cell, which is located in the membrane lining the in the membrane lining the nose and sinuses, releases a nose and sinuses, releases a chemical called histamine. chemical called histamine. Histamine attaches to its Histamine attaches to its site of action called site of action called receptors on nearby blood receptors on nearby blood vessels, causing them to vessels, causing them to dilate or enlarge, leading to dilate or enlarge, leading to redness, swelling, itching, redness, swelling, itching, and changes in the and changes in the secretions. secretions.

Page 7: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

Histamine and Mast CellsHistamine and Mast CellsHistamine:Histamine:

Mast Cells:Mast Cells:

Page 8: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

SymptomsSymptoms Nose: swelling of the Nose: swelling of the

nasal nasal mucosa (allergic mucosa (allergic rhinitis) rhinitis)

Eyes: redness and itching Eyes: redness and itching (allergic (allergic

conjunctivitis) conjunctivitis) Airways: Airways:

bronchoconstriction, bronchoconstriction, wheezing, itchy or wheezing, itchy or sore throat, post nasal sore throat, post nasal drip, and cough drip, and cough

Ears: feeling of fullness, Ears: feeling of fullness, possibly pain, and possibly pain, and impaired hearing impaired hearing

due due to the lack of to the lack of eustachian tube eustachian tube drainage. drainage.

Page 9: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

Common Structures of AntihistaminesCommon Structures of Antihistamines

Amino alkyl ethers Amino alkyl ethers BromodiphenhydramineBromodiphenhydramine

::Diphenhydramine Diphenhydramine

hydrochloridehydrochloride:Carbinoxamine:Carbinoxamine:

Benadryl (diphenhydramine hydrochloride) will be discussed later.

Page 10: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

Common Structures of AntihistaminesCommon Structures of Antihistamines

Substituted alkylaminesSubstituted alkylaminesBrompheniraminBrompheniramin

e:e:Chlorphenamine:Chlorphenamine:Pheniramine maleatePheniramine maleate:

These antihistamines will not be discussed These antihistamines will not be discussed later.later.

Page 11: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

Common Structures of AntihistaminesCommon Structures of Antihistamines

Substituted ethylene diaminesSubstituted ethylene diamines

Methapyrilene:Methapyrilene: Chloropyramine:Chloropyramine: Pyribenzamine:Pyribenzamine:

These first generation antihistamines are These first generation antihistamines are hardly used anymore and will not be hardly used anymore and will not be

discussed further.discussed further.

Page 12: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

Common Structures of AntihistaminesCommon Structures of Antihistamines

Phenothiazine derivativesPhenothiazine derivatives

Mequitazine:Mequitazine: Methdilazine:Methdilazine: Promethazine:Promethazine:

These antihistamines will not be discussed later.These antihistamines will not be discussed later.

Page 13: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

Common Structures of AntihistaminesCommon Structures of Antihistamines

Piperazine derivativesPiperazine derivativesCetirizine hydrochloride:Cetirizine hydrochloride: Niaprazine:Niaprazine:

Buclizine:Buclizine:

Zyrtec (cetirizine hydrochloride) will Zyrtec (cetirizine hydrochloride) will be discussed later.be discussed later.

Page 14: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

Common Structures of AntihistaminesCommon Structures of AntihistaminesTricyclic derivativesTricyclic derivatives

Desloratadine:Desloratadine: Loratadine:Loratadine: Ketotifen:Ketotifen:

Clarinex (desloratadine) and Claritin (loratadine) will be Clarinex (desloratadine) and Claritin (loratadine) will be discussed later.discussed later.

Page 15: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

Common Structures of AntihistaminesCommon Structures of Antihistamines

Antiallergic agents excluding corticosteroidsAntiallergic agents excluding corticosteroids

Antazoline:Antazoline:

Azelastine hydrochloride:Azelastine hydrochloride:Fexofenadine hydrochloride:Fexofenadine hydrochloride:

Astelin (azelastine hydrochloride) and Astelin (azelastine hydrochloride) and Allegra (fexofenadine hydrochloride) Allegra (fexofenadine hydrochloride)

will be discussed later.will be discussed later.

Page 16: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

Treatments: BenadrylTreatments: Benadryl Diphenhydramine is a first Diphenhydramine is a first

generation antihistamine drug.generation antihistamine drug. It works by blocking the effect of It works by blocking the effect of

histamine at H1 receptor sites. histamine at H1 receptor sites. This results in effects such as the This results in effects such as the reduction of smooth muscle reduction of smooth muscle contraction, making contraction, making diphenhydramine a popular diphenhydramine a popular choice for treatment of the choice for treatment of the symptoms of allergic rhinitis, symptoms of allergic rhinitis, hives, motion sickness, and insect hives, motion sickness, and insect bites and stings.bites and stings.

Side effects include: drowsiness, Side effects include: drowsiness, possibilities of motor impairment, possibilities of motor impairment, dry mouth and throat, flushed dry mouth and throat, flushed skin, rapid or irregular heartbeat, skin, rapid or irregular heartbeat, blurred vision at near point, blurred vision at near point, abnormal sensitivity to bright abnormal sensitivity to bright light, pupil dilatation, urinary light, pupil dilatation, urinary retention, constipation, difficulty retention, constipation, difficulty concentrating, short-term concentrating, short-term memory loss, visual disturbances, memory loss, visual disturbances, hallucinations, confusion, erectile hallucinations, confusion, erectile dysfunction, and delirium. dysfunction, and delirium.

Diphenhydramine Diphenhydramine hydrochloridehydrochloride:

Page 17: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

Treatments: AllegraTreatments: Allegra

• Fexofenadine hydrochloride is Fexofenadine hydrochloride is a second-generation a second-generation antihistamine, which does not antihistamine, which does not cross the blood-brain barrier, cross the blood-brain barrier, and so causes less drowsiness and so causes less drowsiness than first-generation than first-generation histamine-receptor histamine-receptor antagonists.antagonists.

Fexofenadine hydrochloride is Fexofenadine hydrochloride is a histamine H1-receptor a histamine H1-receptor antagonist.antagonist.

Treats sneezing, rhinorrhea, Treats sneezing, rhinorrhea, itchy nose/palate/throat, and itchy nose/palate/throat, and itchy/watery/red eyes.itchy/watery/red eyes.

Common side effects: nausea, Common side effects: nausea, vomiting, weakness, vomiting, weakness, drowsiness, sleepiness, and drowsiness, sleepiness, and depression depression

Fexofenadine hydrochloride:Fexofenadine hydrochloride:

Page 18: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

Treatments: ClarinexTreatments: Clarinex Desloratadine is a tricyclic Desloratadine is a tricyclic

antihistamine, which has a antihistamine, which has a selective and peripheral H1-selective and peripheral H1-antagonist action. It has a long-antagonist action. It has a long-lasting effect and does not lasting effect and does not cause drowsiness because it cause drowsiness because it does not readily enter the does not readily enter the central nervous system.central nervous system.

Clarinex treats sneezing, runny Clarinex treats sneezing, runny nose, itching and watering of nose, itching and watering of the eyes, and other allergic the eyes, and other allergic symptoms. symptoms.

Common Side Effects: sore Common Side Effects: sore throat, dry mouth, drowsiness, throat, dry mouth, drowsiness, fatigue, headache, and fatigue, headache, and gastrointestinal disturbances.gastrointestinal disturbances.

Desloratadine:Desloratadine:

Page 19: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

Treatments: ClaritinTreatments: Claritin Loratadine is a tricyclic Loratadine is a tricyclic

antihistamine, which has a antihistamine, which has a selective and peripheral H1-selective and peripheral H1-antagonist action. It has a antagonist action. It has a long-lasting effect and does long-lasting effect and does not normally cause not normally cause drowsiness because it does drowsiness because it does not readily enter the central not readily enter the central nervous system. nervous system.

Loratadine treats watery Loratadine treats watery eyes, runny nose, itching eyes, runny nose, itching eyes, and sneezing. It may eyes, and sneezing. It may also be used to treat hives. also be used to treat hives.

Common Side Effects: dry Common Side Effects: dry mouth, headache and mouth, headache and gastrointestinal gastrointestinal disturbances. disturbances.

Loratadine:Loratadine:

Page 20: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

Treatments: ZyrtecTreatments: Zyrtec Cetirizine hydrochloride Cetirizine hydrochloride

is a racemic selective is a racemic selective H1 receptor antagonist.H1 receptor antagonist.

Cetirizine hydrochloride Cetirizine hydrochloride treats itchy, red, and treats itchy, red, and watery eyes, sneezing, watery eyes, sneezing, runny, and itchy nose, runny, and itchy nose, postnasal drip and postnasal drip and itching from hives.itching from hives.

Common side effects: Common side effects: sleepiness, fatigue, or sleepiness, fatigue, or dizziness, headache, dizziness, headache, and dry mouth.and dry mouth.

Cetirizine hydrochloride:Cetirizine hydrochloride:

Page 21: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

Treatments: AstelinTreatments: Astelin Azelastine hydrochloride is the only Azelastine hydrochloride is the only

prescription antihistamine approved prescription antihistamine approved to treat nasal congestion. to treat nasal congestion.

It is a steroid free and It is a steroid free and pseudoephedrine free pseudoephedrine free antihistamine antihistamine nasal spray which provides relief from nasal spray which provides relief from congestion, itchy or runny nose, congestion, itchy or runny nose, sneezing, and postnasal drip. Astelin, sneezing, and postnasal drip. Astelin, the Azelastine hydrochloride brand the Azelastine hydrochloride brand name, blocks the effects of histamine. name, blocks the effects of histamine.

The medicine is a nasal spray which The medicine is a nasal spray which enables quicker relief from allergy enables quicker relief from allergy symptoms. symptoms.

Astelin is unique because it treats Astelin is unique because it treats symptoms caused by both allergens symptoms caused by both allergens and irritants.and irritants.

Because Astelin does not contain a Because Astelin does not contain a topical vasoconstrictor like other topical vasoconstrictor like other nasal decongestants, it does not nasal decongestants, it does not cause chronic nasal stuffiness. cause chronic nasal stuffiness.

Common side effects: bitter taste, Common side effects: bitter taste, headache, nasal inflammation or headache, nasal inflammation or burning, and drowsiness. burning, and drowsiness.

Azelastine hydrochloride:Azelastine hydrochloride:

Page 22: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

Future IdeasFuture Ideas According to the According to the

American Academy of American Academy of Allergy, Asthma and Allergy, Asthma and Immunology, 30 million Immunology, 30 million Americans suffer from Americans suffer from some form of cat some form of cat allergy. allergy.

Allerca has produced Allerca has produced the world's first hypo-the world's first hypo-allergenic cats. They allergenic cats. They allow people with feline allow people with feline allergies to enjoy allergies to enjoy having a pet without having a pet without having allergic having allergic symptoms. symptoms.

Page 23: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

Allerca CatsAllerca Cats The hypo-allergenic cats are The hypo-allergenic cats are

made by focusing in on the made by focusing in on the cat allergen that causes the cat allergen that causes the symptoms. symptoms.

Normally, the cat allergen can Normally, the cat allergen can remain airborne for several remain airborne for several months and is ten times months and is ten times smaller than pollen or dust smaller than pollen or dust particles. particles.

There is a glycoprotein There is a glycoprotein secreted by the cat's skin and secreted by the cat's skin and salivary glands whose salivary glands whose production depends on the Fel production depends on the Fel d 1 gene. d 1 gene.

The company altered the The company altered the protein to allow the cat to protein to allow the cat to secrete a genetic divergent secrete a genetic divergent Fel d 1 that does not trigger Fel d 1 that does not trigger symptoms of allergies and is symptoms of allergies and is not harmful to the cat. The not harmful to the cat. The cats were tested on people cats were tested on people with cat allergies and proved with cat allergies and proved that these new cats did not that these new cats did not cause any symptoms. cause any symptoms.

Page 24: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

Only $9895!!Only $9895!!

ALLERCA began deliveries of ALLERCA began deliveries of GD kittens to eager GD kittens to eager customers at the end of 2006.customers at the end of 2006.

You too can now own an You too can now own an ALLERCA GD kitten. The price ALLERCA GD kitten. The price is is $6950 $6950 per kitten. Orders per kitten. Orders made on or before May 1, made on or before May 1, 2007 qualify for the initial 2007 qualify for the initial price of $3950. price of $3950.

A processing and A processing and transportation fee of transportation fee of $995$995 is is due eight weeks prior to due eight weeks prior to delivery. delivery.

The Premium Placement fee is The Premium Placement fee is $$1,9501,950 to guarantee your to guarantee your delivery in 1 year rather than delivery in 1 year rather than 2 years.2 years.

Page 25: Seasonal Allergies: Antihistamines & the Future Jacquelyn Covarrubias CHEM 5389 April 24, 2007

OverviewOverview

How Allergies Occur:How Allergies Occur: How to treat Allergies according to How to treat Allergies according to symptoms:symptoms: