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27 Cards in this Set

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