Br Pharmacology: Histamine, Serotonin, Ergot Alkaloids

Front 1

what is the precursor for histamine? How is it metabolized? What is breakdown product?

Back 1

1) histadine
2) MAO
3) imidazoleacetic acid in urine

Front 2

Which two histamine receptors mediate most peripheral actions? What is their function?

Back 2

1) H1 = Smooth muscle, Gq, increase IP3 and DAG
2) H2 = stomach, heart, mast cells, Gs, increase cAMP

Front 3

What histamine receptor is on the heart? What is its action? what is the effect on mast cells?

Back 3

1) H2
2) cardiac stimulant
3) reduces histamine release from mast cells via negative feedback

Front 4

What type of receptor is H3? Where is it found?

Back 4

1) Gi, decreases cAMP
2) nerve endings and CNS

Front 5

What type of receptor is H4? Where is it found?

Back 5

1) leukocytes and mast cell chemotaxis
2) Gi, decrease cAMP

Front 6

What is the prototype first gen H1 blocker? What are other effects? What are sub-group first gen H1 blockers?

Back 6

1) diphenhydramine
2) highly sedative and autonomic blocker
3) Chlorpheniramine and cyclizine

Front 7

What are second gen H1 blockers?

Back 7

1) fexofendandine
2) loratadine
3) cetirizine
Note: less sedating and autonomic effects

Front 8

What do H1 blockers have major applications in

Back 8

1) Type I hypersensitivity

Front 9

Which H1 blocker can be used for antimotion sickness?

Back 9

1) meclizine, also diphenhydramine, dimenhydramine, cyclazine

Front 10

Which H1 blocker can be used for chemo-therapy induced vomitting?

Back 10

diphenhydramine

Front 11

which H1 blockers is sedation most common with?

Back 11

1) diphenhydramine
2) promethazine

Front 12

Alpha-blocking actions are strongest with which H1 blocker? What can it cause?

Back 12

1) promethazine
Note: may cause orthostatic hypotension

Front 13

Where is 5-HT1D found? What is its function?

Back 13

1) brain
2) Gi, decreases cAMP
3) synaptic inhibition via increased K+ conductance

Front 14

Where is 5-HT2 found? What is its function?

Back 14

1) smooth muscle, platelets
2) Gq, increases IP3 and DAG
3) relaxation of smooth muscle

Front 15

Where is 5-HT3 found? What is its function?

Back 15

1) area postrema, sensory and enteric nerves
2) ligand gated Ca channel

Front 16

Where is 5-HT4 found? What is its function?

Back 16

1) presynaptic nerve terminals in enteric nervous system
2) Gs, increases cAMP
3) increases GI motility

Front 17

What are the H2 blockers?

Back 17

1) cimetidine
2) ranitidine
3) famotidine
4) nizatidine

Front 18

What effects do H2 blockers have?

Back 18

1) used only for reducing gastric acid secretion
2) accelerate healing and prevent recurrence of ulcers

Front 19

What are the side-effects of cimetidine?

Back 19

1) inhibitor of hepatic drug metabolizing enzymes
2) significant anti-androgen effects

Front 20

what is serotonin made from? where is it stored? How is it metabolized? What metabolite can be detected?

Back 20

1) tryptophan
2) enterochromaffin cells in gut and neurons CNS and ENS and platelets
3) MAO
4) 5-hydroxyindoleacetic acid (5-HIAA)

Front 21

What is the MOA of sumatriptan? What is another drug of this class? What are they effective against?

Back 21

1) 5-HT1D agonist
2) Naratriptan
3) acute migraine and cluster HA

Front 22

What is the MOA of tegaserod? What is it used for?

Back 22

1) 5-HT4 partial agonist
2) chronic constipation
Note: it is restricted because of cariactoxicity

Front 23

What is the MOA of dexfenfluramine? what was it used for? What was it combined with?

Back 23

1) Serotonin reuptake inhibitor
2) appetite reducer
3) phentermine an amphetamine anorexant

Front 24

Which drugs are 5-HT2 blockers?

Back 24

1) ketaserin
2) phenoxybenzamine (irreversible)
3) cyprohepatadine

Front 25

Which drugs are 5-HT3 blockers? What are they used for?

Back 25

1) ondansetron
2) granisetron
3) dolasetron
Note: these three are effective as antiemetics
4) alosetron

Front 26

The 5-HT2 blockers are poorly selective. Where else do they act?

Back 26

1) alpha blockers = ketanserin, phenoxybenzamine
2) H1 blockers = cyproheptadine

Front 27

which drugs are used to treat carcinoid tumor? What symptoms are present?

Back 27

1) 5-HT2 blockers
2) diarrhea, bronchoconstriction, flushing

Front 28

Which drug is most effective in post chemo vomiting?

Back 28

ondansetron

Front 29

Alosteron is used to treat what condition?

Back 29

irritable bowel syndrome associated with diarrhea

Front 30

What is a specific side effect of dolasetron and who is it contraindicated in?

Back 30

1) QRS and QT prolongation
2) heart disease

Front 31

What are toxic effects of alosteron?

Back 31

1) significant constipation
2) fatal bowel complications

Front 32

Which ergot alkaloid effects blood vessels? What receptor is used? What is main drug?

Back 32

1) vasoconstriction
2) alpha agonist
3) ergotamine

Front 33

Which drug can lead to ischemia and gangrene? How is it reversed?

Back 33

1) ergotamine
2) nitroprusside

Front 34

Which ergot alkaloids can contract the uterus?

Back 34

1) ergonovine (#1)
2) ergotamine

Front 35

Which drugs are useful to slow uterine blood flow after pregnancy?

Back 35

1) ergonovine (#1)
2) ergotamine

Front 36

What is the MOA of LSD?

Back 36

1) 5-HT2 blocker in peripheral tissues
2) dopamine agonist in CNS

Front 37

Which ergot alkaloids are D2 agonists?

Back 37

1) bromocriptine
2) pergolide

Front 38

1st Jew in the Senate

Back 38

Benjamin

Front 39

How do ergot derivatives affect connective tissues?

Back 39

fibroplasia in:
1) retroperitoneal
2) retropleural
3) subendocardial

Front 40

What are organs in the body can be damaged from taking ergot derivatives?

Back 40

1) kidney = hydronephrosis
2) heart = valve and conduction system malfunction

Front 41

What are GI effects of erogot alkaloids?

Back 41

1) N/V
2) diarrhea

Front 42

A woman is pregnant and suddenly has an abortion. She has a history of migraines. What drug was she taking?

Back 42

1) ergonovine
2) ergotamine

Front 43

Disease caused by excess ergot alkaloids

Back 43

St. Anthony's Fire

Front 44

Endogenous substances commonly interpreted as histamine, serotonin, prostaglandins, and vasoactive peptides

Back 44

Autocoids

Front 45

Generation of antihistamine that has the most CNS effects

Back 45

First generation due to being more lipid-soluble

Front 46

Antihistamine that can be used for anxiety and insomnia and is not addictive

Back 46

hydroxyzine (Atarax)

Front 47

Most common side effect of 1st generation antihistamines

Back 47

Sedation

Front 48

Lethal arrhythmias resulting from concurrent therapy with azole fungals (metabolized by CYP 3A4) and these antihistamines which inhibit the 3A4 iso-enzyme.

Back 48

Terfenadine and astemizole (have been removed from the market)

Front 49

"
5HT-1d agonist used for migraine headaches "

Back 49

Sumatriptan, naratriptan, and rizatriptan

Front 50

Triptan available in parenteral and nasal formulation

Back 50

Sumatriptan

Front 51

H1 blocker that is also a serotonin antagonist

Back 51

Cyproheptadine

Front 52

Dopamine agonist used in hyperprolactinemia

Back 52

Bromocriptine

Front 53

Peptide causing increased capillary permeability and edema

Back 53

Bradykinin and histamine

Front 54

Ergot alkaloid that is a partial agonist at D2 receptors in the brain, used for patients who are refractory or cannot tolerate levodopa, causes erythromelalgia

Back 54

Bromocriptine
Note:erythromelalgia = neurovascular peripheral pain disorder in which blood vessels, usually in the lower extremities (or hands), are episodically blocked (frequently on and off daily), then become hyperemic and inflamed. There is severe burning pain (in the small fiber sensory nerves) and skin redness

Front 55

Non ergot agents used as first-line therapy in the initial management of Parkinson's

Back 55

Pramipexole and ropinirole

Front 56

Agent with long duration of action and is most likely to cause histamine release

Back 56

Tubocurarine