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Flashcards in Autacoids Deck (39):
1

what drugs can displace histamine from the heparin-protein complex within cells

morphine and tubocurarine

2

H1 and H2 -- who has the higher affinity for histamine and its significance

H1 -- rapid response but short lived
H2 -- slowly develops response but sustained

3

what does activation of H1 and H2 lead to

H1 -- works on endothelial cells so leads to production of NO
H2 - works on vascular SM so leads to vasodilation, in heart leads to increased contractility

4

histamine agonist and its clinical use

histamine
pulmonary function testing (test nonspecific bronchial hyperactivity)

5

toxicity of histamine

flushing, hypotension, tachycardia, headache, wheals (area of skin that is raised and itchy), GI upset, bronchial constriction

6

who do you not give histamine to

asthmatics, those with acute ulcer disease, GI bleeding

7

physiological antagonist of histamine

epinephrine

8

release inhibitors of histamine

cromolyn and nedocromil (use to treat asthma)
beta 2 agonists as well

9

what are the first generation H1 receptor antagonist

chlorpheniramine, cyclizine, dimenhydrinate, diphenhydramine, meclizine, promethazine, hydroxyzine

CD2 MPH

10

what are the second generation H1 receptor antagonist

cetirizine, fexofenadine, loratadine, astemizole, terfenadine

C-FLAT

11

why were astemizole and terfenadine removed from US market

induced potentially fatal arrhythmias called torsades de pointes

this occurred especially in the presence of CYP3A4 inhibitors leaving these two drugs in circulation longer than they are supposed to be

12

actions of H1 receptor antagonist

-inverse agonist
-blocks histamine induced contraction of GI and bronchial
-bind to cholinergic, alpha adrenergic, serotonin, and local anesthetic receptor sites

13

what are H1 receptor antagonists used for

-allergies caused by antigens acting on IgE antibody sensitized mast cells so like allergic rhinitis and urticaria
-not good at treating bronchial asthma because histamine is only one of the several mediators
-motion sickness and nausea (with scopolamine)
-insomnia

14

which antihistamine is used as a somnifacients aka tx for insomnia

diphenhydramine

15

which antihistamine is used as a tx for motion sickness and nausea

diphenhydramine, dimenhydrinate, promethazine

16

adverse reaction of H1 blocker

sedation and dry mouth

17

why is driving and operating heavy machinery cautioned against in H1 blockers

some H1 blockers cause sedation especially if taken with drugs that cause CNS depression

18

adverse effects if overdosed on H1 blockers

hallucinations, excitement, ataxia, and convulsion

19

what are H2 receptor antagonists

Famotidine, Ranitidine, Nizatidne, Cimetidine

FRaNC

20

clinical use of H2 receptor antagonist

inhibit gastric acid secretion (induced by histamine or gastrin)
so used for the treatment of peptic ulcer, acute stress ulcers, GERD

21

adverse effects of H2 blocker (we'll talk about cimetidine in a diff flash card)

headache, diarrhea, muscular pain, constipation
-mental status changes
-blood dyscriasis
-bradycardia and hypertension

22

adverse effects of cimetidine an H2 blocker

-inhibits CYP450 and slows metabolism of certain drugs
-binds to androgen receptors and has antiandrogenic effects like gynecomastia in men and galactorrhea in women

23

what are the serotonin agonists

serotonin, sumatriptan, metoclopramide, cisapride

24

what is sumatripan used to treat

migraine headache (first line therapy for acute migraine)

25

who do you not prescribe sumatripan to and why

person with coronary heart disease because of their vasoconstrictive action

26

what is metoclopramide given for

prokinetic agent - enhance GI motility by coordinating contractions that enhance transit

27

adverse effects of metoclopramide

somnolence, nervousness, dystonic reactions
extrapyramidal effects and tardive dyskinesia

28

use of cisapride

prokinetic agent - enhance GI motility for pts with gastroesophageal reflux and gastroparesis

29

why is cisapride no longer widely used in US

because of its cardiac effects

30

what is the serotonin 5-HT2 antagonist

cyproheptadine

31

action of cyproheptadine

prevents smooth muscle effects of serotonin and histamine

32

uses of cyproheptadine

perennial and seasonal allergic rhinitis
vasomotor rhinitis
allergic conjuctivitis due to inhalant allergens and foods
cold urticaria
dermatographism
serotonin syndrome (hyperthermia, muscle rigidity, and myoclonus)

33

what is the serotonin 5-HT3 antagonist

ondansetron

34

use of ondansetron

nausea and vomiting that occurs with cancer chemotherapy

35

what are the ergoid alkaloids (also serotonin antagonist)

MEED CB

methylergonovine, ergonovine, ergotamine, dihydroergotamine, cabergoline, bromocriptine

36

ergoid alkaloid used to treat migraine

ergotamine

37

ergoid alkaloid used for hyperprolactinemia

bromocriptine and cabergoline

38

ergoid alkaloid used for postpartum hemorrhage

ergonovine and methylergonovine

39

what is used to diagnose variant angina (also do you remember what type of drugs you don't use on pt with variant angina)

ergonovine to diagnose

do not use beta blockers on variant angina!

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