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43 Cards in this Set

  • Front
  • Back
common feature of autacoids?
the ability to be formed by certain tissues, and then act on those SAME tissues
Histamine is found in all tissues, especially high [ ] in?
1) lung
2) skin
3) intestinal mucosa
histamine is synthesized from ?
histamine is stored intracellularly in vesicles with?
storage sites of histamine?
1) mast cells & basophills
2) GI mucosa
3) nerve endings in certain areas of the brain
4) cells of rapidly growing or regenerating tissue
release of histamine is caused by?
1) allergic reactions
2) cellular injury
3) drugs (opioids, sux, contrast, vanc, anti-protozoal)
activation of H1 receptor causes?
constriction of bronchi and gut
H2 receptor ?
gastric acid secretion
H1 and H2 receptors?
vascular dilation
H3 receptor?
inhibition of histamine release and synthesis (like autoreceptor)
circulatory effects of histamine?
1) increased capillary permeability
2) vasodilation
3) triple response of Lewis
triple response of Lewis?
1) red spot
2) wheal
3) flare or red flush
hyposecretion of histamine?
1) pernicious anemia
2) gastric carcinoma
3) atropic gastritis
hypersecretion of histamine?
1) diodenal ulcer
2) Zollinger-Ellison syndrome
clinical use of histamine for diagnosis?
Histalog (histamine analog Betazole) = less H1 receptor activity (H2:H1 = 10:1)
investigational drug
greater H2 selectivity
(H2:H1 = 10,000:1)
1st generation antihistamines
1) Alkylamines
2) Ethanolamines
3) Ethylenediamines
4) Phenothiazines
5) Piperazines
6) Piperidines
7) Phthalazinone
1) Alkylamines
1) Brompheniramine (in Dimetane)
2) Chlorpheniramine (Chlor-Trimeton)
3) Dexchlorpheniramine (Polaramine)
4) Triprolidine (Actifed)
Alkylamines have marked potential for producing?
2) Ethanolamines
1) Carbinoxamine (Rondec)
2) Clemastine (Tavist)
3) Dimenhydrinate (Dramamine)
4) Diphenhydramine (Benadryl)
5) Doxylamine (Unisom)
Clemastine (Tavist) also blocks?
at muscarinic receptors
Dimenhydrinate (Dramamine) is used to treat?
motion sickness
Dephenhydramine (Benadryl) is active metabolite of?
1) sedation
2) motion sickness
3) anticholinergic
Doxylamine (Unisom) is used as ?
OTC sleep aid
3) Ethylenediamines
1) Tripelennamine (PBZ)
2) Pyrilamine (in cold medecine)
4) Phenothiazines
1) Promethazine (Phenergan)
Phenergan also blocks at?
alpha adrenergic receptors
5) Piperazines
1) Hydroxyzine (Vistaril, Atarax)
2) Meclizine (Bonine OTC, Antivert)
Meclizine is used to treat?
1) motion sickness
2) vertigo
3) Meniere's syndrome
6) Piperidines
antihistaminic / antiserotogenic
1) Cyproheptadine (Periactin)
SE of Cyprohepatidine?
increase appetite and wt gain
7) Phthalazinone
1) Azelastine (Astelin)
- 1st antihistamine nasal spray
- for seasonal allergic rhinitis
2nd generation antihistamines
1) Loratadine (Claritine)
2) Desloratadine (Clarinex)
3) Cetirizine (Zyrtec)
4) Fexofenadine (Allegra)
benefit of 2nd generation antihistamines?
primary active metabolite of Claritin?
desloratadine (Clarinex)
Are H1 antagonists effective in severe hypersensitivity reactions?
No. b/c hypotension is cauused by histamine acting at both H1 and H2 receptors
antihistamine and MAOI?
MAOI can prolong and intensify their anticholinergic effects
episodes of syncope in pts with H1 antagonists?
Discontinue H1 antagonists.
SE = severe arrhythmia
H2 receptor antagonists
1) Cimetidine (Tagamet)
2) Ranitidine (Zantac)
3) Famotidine (Pepcid)
4) Nizatidine (Axid)
H2 receptor antagonists inhibit?
action of histamine at parietal cell H2 receptors = decrease in acid secretion
SE of Cimetidine?
1) gynecomastia
Cimetidine decreases metabolism of?
1) Warfarin
2) Phenytoin
3) Theophyllin