Pharm 16

Front 1

where are mast cells especially rich

Back 1

sites of potential injury like mouth, nose, feet, internal body surfaces, and blood vessels (P points and bifurcations)

Front 2

histamine release negative feedback occurs where (H2 receptors)

Back 2

skin and blood vessels; NOT lungs

Front 3

histamine receptors

Back 3

H1 to 4; all coupled to G proteins

Front 4

brain histamine receptors

Back 4

H1 and 2 mostly postsynaptic and H3 presynaptic

Front 5

H2 receptors in gastic mucosa, cardiac muscle cells, and some immune cells intracellular effect

Back 5

increase cAMP via Gs

Front 6

H4 receptor are mostly found where

Back 6

leukocytes in bone marrow and circulating blood; important chemotaxic effects on eosinophils and mast cells

Front 7

histamine and nervoud system

Back 7

powerful stimulant of sensory nerve endings, especially pain and itching

Front 8

H3 agonists reduce the release of what in brain and peripheral nerves

Back 8

acetylcholine, amine, and peptide transmitters

Front 9

H1 distribution

Back 9

smooth muscle, endothelium, brain; Gq, increases IP3 and DAG

Front 10

H2 distribution

Back 10

gastric mucosa, cardiac muscle, mast cells, brain; Gs, increases cAMP

Front 11

H3 distribution

Back 11

presynaptic brain, myenteric plexus, other neurons; Gi, decreases cAMP

Front 12

H4 distribution

Back 12

eosinophils, neutrophils, CD4 T cells; Gi, decrease cAMP

Front 13

what can cardiovascular effects of histamine (small amounts) be blocked by

Back 13

H1-receptor antagonists alone

Front 14

what causes histamine-induced edema

Back 14

action on H1 receptor in vessels of microcirculation

Front 15

histamine in stomach

Back 15

gastric acid stimulant along with gastric pepsin and intrinsic factor; via increased adenylyl cyclase and cAMP and Ca2+

Front 16

3 separate cell types causing red spot, edema, and flare response of intradermal histamine

Back 16

smooth muscle in microcirculation, capillary/venular endothelium, and sensory nerve endings

Front 17

release inhibitors

Back 17

reduce degranulation of mast cells that results from immunologic triggering by anti-IgE interaction; eg cromolyn and nedocromil

Front 18

first gen H1-receptor antagonists

Back 18

strong sedative effects; more likely to block autonomic receptors; enter CNS readily

Front 19

antiparkinsonism effects and histamine

Back 19

H1 antagonists (like diphenhydramine) have significant acute suppressant effects on extrapyramidal symptoms associated with some antipsychotic drugs

Front 20

potent H1-blocking agent that also strongly blocks serotonin receptors

Back 20

cyproheptadine

Front 21

H1 antagonists that block sodium channels in excitable membranes

Back 21

diphenhydramine and promethazine

Front 22

antihistaminic drugs most effective in motion sickness

Back 22

diphenhydramine and promethazine; piperazines (cyclizine and meclizine)=less sedating

Front 23

OD of antihistamines

Back 23

resemble atropine OD and treated same way

Front 24

what blocks CYP3A4 and causes significant increases in blood concentration of antihistamines

Back 24

ketoconazole, itraconazole, macrolide antibiotics (erythromycin)

Front 25

H3 receptor blockers potential uses

Back 25

sleep disorders, obesity, cognitive and psychiatric disorders

Front 26

H4 receptor blocker potential uses

Back 26

chronic inflammatory conditions like asthma; pruritus

Front 27

carcinoid syndrome

Back 27

neoplasn of enterochromaffin cells that secrete serotonin

Front 28

what is blocked by reserpine

Back 28

vesicle-associated transporter (VAT) = depletes serotonin, and catecholamines from vesicles

Front 29

measure of serotonin synthesis

Back 29

urine 5-HIAA

Front 30

serotonin receptors

Back 30

7 families of 5-HT-receptor subtypes; 6 involve G protein coupled and one is ligand-gated channel (5-HT3)

Front 31

5-HT3

Back 31

member of nicotinic/GABAa family of Na+, K+ channel proteins; area postrema, sensory, and enteric nerves

Front 32

serotonin is a precursor to

Back 32

melatonin in pineal gland

Front 33

chemoreceptor reflex (Bezold-Jarisch reflex)

Back 33

activation of 5-HT3 receptors on afferent vagal nerve endings; marked bradycardia and hypotension

Front 34

melatonin receptor MT1

Back 34

activation results in sleepiness

Front 35

melatonin receptor MT2

Back 35

light-dark synchronization

Front 36

ramelteon

Back 36

selective MT1 and 2 agonist zpproved for insomnia; no addiction liability

Front 37

cardiovascular system and serotonin

Back 37

direct contraction of vascular smooth muscle via 5-HT2; dilates vessels in skeletal muscle and heart; reflex bradycardia via 5-HT3

Front 38

triphasic BP response to serotonin

Back 38

1) decrease HR, CO, and BP via chemoreceptor 2) increase due to vasoconstriction 3) decrease due to vasodilation to vessels supplying skeletal muscle

Front 39

serotonin and platelet aggregation

Back 39

5-HT2

Front 40

GI and serotonin

Back 40

stimulant of smooth muscle (tone and facilitating peristalsis) via 5-HT2; 5-HT4 in enteric NS motility-enhancing (increase acetylcholine)

Front 41

serotonin syndrome

Back 41

skeletal muscle contractions precipitated when MOA inhibitors given with serotonin agonists (especially SSRIs)=hyperthemia

Front 42

buspirone

Back 42

5-HT1a agonist; anti-anxiety agent

Front 43

appetite suppression

Back 43

5-HT2c in CNS agonists

Front 44

triptans

Back 44

5-HT1d/1b agonists; migraine headaches; eg sumatriptan

Front 45

triptans are contraindicated in

Back 45

coronary artery disease (can cause vasospasm) and angina

Front 46

ondansetron

Back 46

prototypical 5-HT3 antagonist; prevention of nausea and vomiting associated with surgery and cancer chemotherapy

Front 47

ergotism (ergot poisoning)

Back 47

dementia with florid hallucinations, prolonged vasospasm-may result in gangrene; stimulation of uterine smooth muscle

Front 48

ergot derivatives bromocriptine, cabergoline, and pergolide on pituitary dopamine receptos

Back 48

directly suppress prolactin secretion by activating regulatory dopamine receptors

Front 49

ergotamine and alpha receptors

Back 49

partial agonist; dissociates slowly-long-lasting and atagonist effects; little/no B adrenoceptor effect

Front 50

ergots and uterine smooth muscle

Back 50

stimulant due to combined alpha agonist, serotonin, and other effects; ergonovine used in obstetrical applications (post-delivery bleeding)

Front 51

ergots used in migraine

Back 51

ergotamine traditional; also dihydroergotamine IV for intractable migraine

Front 52

what can treat ergot vasospasm

Back 52

refractory to most; large doses of nitroprusside or nitroglycerin can be successful

Front 53

contraindications for ergots

Back 53

obstructive vascular diseases and collagen diseases

Front 54

chronic use of methysergide caused

Back 54

CT proliferation in retroperitoneal space, pleural cavity, and endocardial tissue causing hydronephrosis or cardiac murmur