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27 Cards in this Set
- Front
- Back
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Distribution of histamine receptors H1, H2, and H3
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H1 = Smooth muscle; H2 = stomach, heart, mast cells; H3 = nerve endings, CNS
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Prototype antagonist of H1 and H2 receptors
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H1 = Diphenhydramine H2 = cimetidine
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1st generation antihistamine that is highly sedating
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Diphendydramine
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1st generation antihistamine that is least sedating
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Chlorpheniramine or cyclizine
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2nd generation antihistamines
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Fexofenadine, loratadine, and cetirizine
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Generation of antihistamine that has the most CNS effects
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First generation due to being more lipid-soluble
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Major indication for H1 receptor antagonist
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Use in IgE mediated allergic reaction
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Antihistamine that can be used for anxiety and insomnia and is not addictive
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hydroxyzine (Atarax)
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H1 antagonist used in motion sickness
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Dimenhydrinate, meclizine (1st gen)
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Most common side effect of 1st generation antihistamines
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Sedation
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Lethal arrhythmias resulting from concurrent therapy with azole fungals (metabolized by CYP 3A4) and these antihistamines which inhibit the 3A4 iso-enzyme.
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Terfenadine and astemizole (have been removed from the market)
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H2 blocker that causes the most interactions with other drugs
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Cimetidine
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Clinical use for H2 blockers
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Acid reflux disease, duodenal ulcer and peptic ulcer disease
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Peptide causing increased capillary permeability and edema
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Bradykinin and histamine
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Receptors for serotonin (5HT-1) are located where? Mechanism?
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Located mostly in the Brain. Mediate synaptic inhibition via increased K+ conductance
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5HT-1d agonist used for migraine headaches
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Sumatriptan, naratriptan, and rizatriptan
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Triptan available in parenteral and nasal formulation
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Sumatriptan
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H1 blocker that is also a serotonin antagonist
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Cyproheptadine
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Agents for reduction of postpartum bleeding
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Oxytocin, ergonovine and ergotamine
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Agents used in treatment of carcinoid tumor
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Ketanserin cyproheptadine, and phenoxybenzamine
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5ht-3 antagonist that has been associated with QRS and QTc prolongation and should not be used in patients with heart disease
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Dolasetron
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Drug used in ergot alkaloids overdose, ischemia and gangrene
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Nitroprusside
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Reason ergot alkaloids are contraindicated in pregnancy
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Uterine contractions
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SE of ergot alkaloids
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Hallucinations resembling psychosis
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Ergot alkaloid used as an illicit drug
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LSD
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Disease caused by excess ergot alkaloids
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St. Anthony's Fire
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Endogenous substances commonly interpreted as histamine, serotonin, prostaglandins, and vasoactive peptides
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Autocoids
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