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56 Cards in this Set

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what is the precursor for histamine? How is it metabolized? What is breakdown product?
1) histadine
2) MAO
3) imidazoleacetic acid in urine
Which two histamine receptors mediate most peripheral actions? What is their function?
1) H1 = Smooth muscle, Gq, increase IP3 and DAG
2) H2 = stomach, heart, mast cells, Gs, increase cAMP
What histamine receptor is on the heart? What is its action? what is the effect on mast cells?
1) H2
2) cardiac stimulant
3) reduces histamine release from mast cells via negative feedback
What type of receptor is H3? Where is it found?
1) Gi, decreases cAMP
2) nerve endings and CNS
What type of receptor is H4? Where is it found?
1) leukocytes and mast cell chemotaxis
2) Gi, decrease cAMP
What is the prototype first gen H1 blocker? What are other effects? What are sub-group first gen H1 blockers?
1) diphenhydramine
2) highly sedative and autonomic blocker
3) Chlorpheniramine and cyclizine
What are second gen H1 blockers?
1) fexofendandine
2) loratadine
3) cetirizine
Note: less sedating and autonomic effects
What do H1 blockers have major applications in
1) Type I hypersensitivity
Which H1 blocker can be used for antimotion sickness?
1) meclizine, also diphenhydramine, dimenhydramine, cyclazine
Which H1 blocker can be used for chemo-therapy induced vomitting?
diphenhydramine
which H1 blockers is sedation most common with?
1) diphenhydramine
2) promethazine
Alpha-blocking actions are strongest with which H1 blocker? What can it cause?
1) promethazine
Note: may cause orthostatic hypotension
Where is 5-HT1D found? What is its function?
1) brain
2) Gi, decreases cAMP
3) synaptic inhibition via increased K+ conductance
Where is 5-HT2 found? What is its function?
1) smooth muscle, platelets
2) Gq, increases IP3 and DAG
3) relaxation of smooth muscle
Where is 5-HT3 found? What is its function?
1) area postrema, sensory and enteric nerves
2) ligand gated Ca channel
Where is 5-HT4 found? What is its function?
1) presynaptic nerve terminals in enteric nervous system
2) Gs, increases cAMP
3) increases GI motility
What are the H2 blockers?
1) cimetidine
2) ranitidine
3) famotidine
4) nizatidine
What effects do H2 blockers have?
1) used only for reducing gastric acid secretion
2) accelerate healing and prevent recurrence of ulcers
What are the side-effects of cimetidine?
1) inhibitor of hepatic drug metabolizing enzymes
2) significant anti-androgen effects
what is serotonin made from? where is it stored? How is it metabolized? What metabolite can be detected?
1) tryptophan
2) enterochromaffin cells in gut and neurons CNS and ENS and platelets
3) MAO
4) 5-hydroxyindoleacetic acid (5-HIAA)
What is the MOA of sumatriptan? What is another drug of this class? What are they effective against?
1) 5-HT1D agonist
2) Naratriptan
3) acute migraine and cluster HA
What is the MOA of tegaserod? What is it used for?
1) 5-HT4 partial agonist
2) chronic constipation
Note: it is restricted because of cariactoxicity
What is the MOA of dexfenfluramine? what was it used for? What was it combined with?
1) Serotonin reuptake inhibitor
2) appetite reducer
3) phentermine an amphetamine anorexant
Which drugs are 5-HT2 blockers?
1) ketaserin
2) phenoxybenzamine (irreversible)
3) cyprohepatadine
Which drugs are 5-HT3 blockers? What are they used for?
1) ondansetron
2) granisetron
3) dolasetron
Note: these three are effective as antiemetics
4) alosetron
The 5-HT2 blockers are poorly selective. Where else do they act?
1) alpha blockers = ketanserin, phenoxybenzamine
2) H1 blockers = cyproheptadine
which drugs are used to treat carcinoid tumor? What symptoms are present?
1) 5-HT2 blockers
2) diarrhea, bronchoconstriction, flushing
Which drug is most effective in post chemo vomiting?
ondansetron
Alosteron is used to treat what condition?
irritable bowel syndrome associated with diarrhea
What is a specific side effect of dolasetron and who is it contraindicated in?
1) QRS and QT prolongation
2) heart disease
What are toxic effects of alosteron?
1) significant constipation
2) fatal bowel complications
Which ergot alkaloid effects blood vessels? What receptor is used? What is main drug?
1) vasoconstriction
2) alpha agonist
3) ergotamine
Which drug can lead to ischemia and gangrene? How is it reversed?
1) ergotamine
2) nitroprusside
Which ergot alkaloids can contract the uterus?
1) ergonovine (#1)
2) ergotamine
Which drugs are useful to slow uterine blood flow after pregnancy?
1) ergonovine (#1)
2) ergotamine
What is the MOA of LSD?
1) 5-HT2 blocker in peripheral tissues
2) dopamine agonist in CNS
Which ergot alkaloids are D2 agonists?
1) bromocriptine
2) pergolide
1st Jew in the Senate
Benjamin
How do ergot derivatives affect connective tissues?
fibroplasia in:
1) retroperitoneal
2) retropleural
3) subendocardial
What are organs in the body can be damaged from taking ergot derivatives?
1) kidney = hydronephrosis
2) heart = valve and conduction system malfunction
What are GI effects of erogot alkaloids?
1) N/V
2) diarrhea
A woman is pregnant and suddenly has an abortion. She has a history of migraines. What drug was she taking?
1) ergonovine
2) ergotamine
Disease caused by excess ergot alkaloids
St. Anthony's Fire
Endogenous substances commonly interpreted as histamine, serotonin, prostaglandins, and vasoactive peptides
Autocoids
Generation of antihistamine that has the most CNS effects
First generation due to being more lipid-soluble
Antihistamine that can be used for anxiety and insomnia and is not addictive
hydroxyzine (Atarax)
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)
"
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
Dopamine agonist used in hyperprolactinemia
Bromocriptine
Peptide causing increased capillary permeability and edema
Bradykinin and histamine
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
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
Non ergot agents used as first-line therapy in the initial management of Parkinson's
Pramipexole and ropinirole
Agent with long duration of action and is most likely to cause histamine release
Tubocurarine