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Pharmacology of antihistamines and drugs for the treatment of allergic rhinitis

Histamine is produced by Mast cells, basophils, and paracrine cells, CNS neurotransmitter
Histidine is converted to histamine by Enzyme L-histidine decarboxylase
Histamine is stored in granules and released from mast cells when IgE reacts to cause degranulation
How can morphine and tubocurarine cause histamine release? My stimulating IP3 and DAG which releases Ca+ and stimulates mast cell degranulation
Histamine can be inactivated by (2 ways) 1. Methylation from methyltransferease enzyme or 2. Oxidation from diamine oxidase
All histamine receptors are GCPR
Which histamine receptors are involved in allergic reactions? H1
Which histamine receptors are involved in gastric acid production and some allergies? H2
What do H3 receptors do? Used as a feedback mechanism in the brain to inhibit histamine production and release
Antihistamines are agonists for which receptors H1 or H2
1st generation H1 antihistamines cause Sedation because they cross the BBB
2nd generation H1 antihistamines are usually preferred because They do not cross the BBB to cause sedation
H1 antihistamines are most effectively when taken Prophylatically
Most antihistamines are metabolized by the Liver
Which two antihistamines are not metabolized by the liver? Hydroxyzine and ceftrizine
First generation antihistamines are often used to treat Nausea, vertigo and for sedation
Meclizine is used for Motion sickness because it is an anitemetic and non-sedating
Which drug is used to treat the symptoms of allergic rhinitis? Azelastine
First line treatment of acute allergies Antihistamines
Antihistamines are used for Acute allergies that are mediated by mast cell-derived histamine but not continuous exposure
Which generation of antihistamines has a longer duration? 2nd
Pseudoephedrine does what Decongestant (but a mild stimulant), used with antihistamines
Leukotriene modifier mechanism Treats pro-inflammatory mediators
Leukotriene modifiers Zileuton, zafirlukast, montelukast
Nasal cromyln does what? Stabilizes mast cells and mediates pro-inflammatory mediatiors
Most effective treatment for moderate to severe AR Intranasal corticosteroids
Intranasal corticosteroids Fluticasone, triamcinolone, flunisolide, budesonide, mometasone, ciclesonide
Patients should start intranasal corticosteroids One week prior to allergy season
Intranasal corticosteroids mechanism of action Decreased nasal eosinophilia, mast cell numbers, and cytokine expression
Intranasal corticosteroid Side effects Local irritation, dryness, and epitaxis
Most effective drug to treat allergic rhinitis Corticosteroids
First generation antihistamine Diphenhydramine
Second generation antihistamines Loratadine and fexofenadine
2nd generation antihistamine with a short half life Fexofenadine
Does intranasal azelastine cause drowsiness? Yes
What does an acute poisoning with 1st gen antihistamines present as Anticholinergic toxicity ("dryness")
Leukotriene modifier mechanism of action Competitive inhibitor of cysteinyl leukotrienes for CysLT1 receptor binding to inhibit early and late phases of bronchoconstriction induced by antigen challenge
Churg-Strauss syndrome Allergic granulomatous vasculitis due to leukotriene antagoists/modifiers in patients being withdrawn from glucocoricoid therapy
Ipratroprium bromide mechanism of action blocks the muscarinic acetylcholine receptors in the smooth muscles of the bronchi in the lungs, opening the bronchi, also has anticholinergic effects in the nose to relieve rhinorrhea but not congestion
Rhinitis medicoamentosa is due to Down regulation of the alpha receptors by continual use of phenylephrine
Created by: mcasto