Chapter 189- Antihistamines Flashcards
First line therapy for chronic idiopathic and physical urticaria
H1 antihistamines
Useful adjunct therapy to H1 antihistamine therapy in refractory cases of chronic idiopathic urticaria/angioedema
H2 antihistamines
Histamine is metabolized by 2 major pathways (2)
Diamine oxidase
Histamine methyl transferase
Inverse agonists that reversibly bind and stabilize the inactive form of H1 receptor
H1 antihistamines
Second generation antihistamines have ___ lipophilicity and bind ___ hence have fewer CNS effects
Reduced
Selectively
Safe for those with hepatic impairment (5)
Cetirizine Levocetirizine Desloratadine Fexofenadine Levocabastine
Indications for treatment with H1 antihistamines (5)
Acute urticaria Chronic idiopathic urticaria Physical urticaria and dermographism Pruritus associated with histamine release Symptoms of mastocytosis
Most commonly reported problem with first generation H1 antihistamines
Sedation
All second generation antihistamines are less sedating except for (2)
Cetirizine
Levocetirizine
Anticholinergic side effects are common in ff groups of antihistamines
Ethanolamine
Phenothiazine
Piperazine
Most serious but rare side effects
Arrhythmias
2 second gen antihistamines removed due to risk of QT interval prolongation and torsades de pointes
Terfenadine
Astemizole
Contraindicated for patients receiving first generation H1 antihistamines
Monoamine oxidase inhibitors
Central depressive effects are observed when 2nd gen antihistamines are combined with alcohol.
True or False
False, 1st gen
Antihistamines are generally avoided during first trimester due to its association with
Cleft palate defects
Antihistamines requiring adjustment for renal (3)
Acrivastine
Ebastine
Fexofenadine
Antihistamines requiring adjustment for hepatic impairment (1)
Mizolastine
Major features of acute poisoning in children (5)
Hallucinations Ataxia Incoordination Athetosis Convulsions
First generation antihistamines are preferred for breastfeeding women.
True or False
False, second
Indications for treatment with H2 antihistamines (3)
Acute allergic reaction
Chronic urticaria
Systemic symptoms associated with mastocytosis
Requires dose adjustments in renal impairment (3)
Ranitidine
Famotidine
Nizatidine
Uncommon side effects of cimetidine (5)
Gynecomastia Galactorrhea Loss of libido Impotence Reduction of sperm counts
H2 atnihistamines that inhibit alcohol dehydrogenase activity (2)
Cimetidine
Ranitidine
Cimetidine is an inhibitor and should not be taken with
Dofetilide Warfarin Phenytoin BZD Metformin Sulfonylureas SSRIs
Uncommon side effect of H2 antihistamines to neonates
Necrotizing enterocolitis
H2 antihistamines are FDA Category
B
TCA most commonly used in dermatology
Doxepin 800 times more potent than diphenhydramine
MC adverse effect of oral and topical doxepin
Sedation
Oral doxepin is FDA Category
C
Doxepin is not safe to use for children less than ___ years of age
12
Benzocycloheptathiophene H1 antihistamine with mast cell and basophil stabilizing properties
Ketotifen