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neurology/psychiatry > ergots > Flashcards

ergots Flashcards

1
Q

what is ergot?

A

a spur
dark brown horn shaped peg that projects from ripening ears of rye in place of rye grains

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2
Q

ergot contains ___

A

ergotoxine

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3
Q

2 types of ergotism

A

gangrenous (caused by ergotoxine)
convulsive or spasmotic (not caused by ergotoxine)

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4
Q

epidemic outbreaks of gangrenous ergotism resulted from ____

A

consumption of ergotised rye

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5
Q

describe what gangrenous ergotism is

A

primarily due to effects of ergotoxine, produces vigorous and prolonged occlusion of the arterioles, food/leg becomes inflamed/hot alternating with sensations of cold (this is called St. Anthony’s Fire), numbness, dry gangrene, painless loss of limb

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6
Q

structure of ergot alkaloid

A

ergoline ring structure; 4 rings

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7
Q

_______ is used to prepare ergonovine and ergotamine

A

lysergic acid

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8
Q

3 classes of ergot alkyloids

A

clavines
ergopeptines
ergoamides

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9
Q

which sites do ergot alkaloids act on

A

5HT1A, 5HT1B, 5HT1D, dopamine D2, and norepinephrine receptors

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10
Q

examples of 5HT1B and 5HT1D agonist drugs

A

triptans and ergots

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11
Q

examples of 5HT3 antagonist drugs

A

setron antiemetics

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12
Q

effects of ergots on blood vessels

A

a significant and prolonged vasoconstriction that may result in ischemia and gangrene

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13
Q

effects of ergots on the uterus

A

direct uterine smooth muscle stimulation (alpha adrenergic and 5HT receptors) that will potentially result in abortion or miscarriage in a pregnant uterus

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14
Q

when might ergots be used for their uterine effects?

A

AFTER THE DELIVERY OF THE PLACENTA to prevent hemorrhage/blood loss

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15
Q

CNS effects of ergots

A

hallucinations
inhibit prolactin secretion (useful to treat hyperprolactinemia)

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16
Q

which ergots may be used as oxytocics after delivery of the placenta?

A

ergonovine, methylergonovine

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17
Q

indications for ergnovine and methylergonovine

A

following delivery of the placenta for management of uterine atony, hemorrhage, subinvolution
administered only after placental expulsion because prior administration may result in ENTRAPMENT of the placenta

18
Q

ergot contraindications

A

CYP3A4 inhibitors/inducers
pregnancy- category x- risk of spontaneous abortion
induction of labor- risk of stillbirth

19
Q

acronym for migraine

A

POUND
Pulsatile
One day duration (4-72h)
Unilateral location
Nausea, vomiting, photophobia, phonophobia
Disabling intensity

20
Q

which ergots are used for migraines

A

ergotamine
dihydroergotamine

21
Q

structure of ergotamine and dihydroergotamine

A

peptide alkaloids- Alanine-Proline-Phenylalanine

22
Q

depolarization theory for migraine pathogenesis

A

wave or neuronal and glial cell activity- trigeminovascular system activated- release of CGRP by trigeminal afferents- inflammatory mediators released- meningeal inflammation- cortical sensitization

23
Q

indications for ergotamine and dihydroergotamine

A

ACUTE therapy of vascular headaches: migraine and migraine variants, cluster headaches

NOT RECOMMENDED FOR CHRONIC PROPHYLAXIS

24
Q

MOA for ergots in migraines

A

agonist at 5HT1B and 5HT1D receptors (like triptans) but also partial agonist at 5HT2, alpha adrenergic, and dopamine D2 receptors

25
Q

onset/duration of dihydroergotamine

A

onset in 15-30 minutes
duration 3-4 hours

26
Q

what are other effects of ergotamine/dihydroergotamine to look out for when treating migraine?

A

potent emetic effect (via stimulation of CTZ)
uterine stimulant

27
Q

what is cafergot

A

oral ergotamine tartrate + caffeine
works together to reduce dilation of cranial blood vessels
less effective than triptans

28
Q

triptan MOA

A

selective for 5HT1B, 5HT1D

29
Q

triptans are ____ selective than ergots, resulting in _____

A

more selective, resulting in fewer side effects

30
Q

adverse effects of ergotamine and dihydroergotamine at a therapeutic dose vs overdose

A

therapeutic dose: nausea, vomiting, weakness, paresthesias, myalgias

overdose: severe vasoconstriction, peripheral ischemia, fingers/toes, numbness/tingling/cold, endarteritis, acute arterial occlusion, gangrene of the extremities

31
Q

how much ergotamine leads to overdose

A

> 15 mg/24h or 40 mg in 2-3 days

32
Q

treatment of ergotamine overdose

A

ACEi such as captopril 50 mg TID
can also use anticoagulants, nitroprusside etc

33
Q

what are the warnings that come along with ergot use

A

pregnancy category x
FDA boxed warning: concomitant use with strong CYP3A4 inhibitors can result in life threatening ergot toxicity
avoid prolonged administration or excessive dosage
rebound headache: patients taking the drug for extended periods of time may experience withdrawal symptoms

34
Q

which ergots may be used for inhibition of prolactin secretion or glycemic control in T2DM

A

bromocriptine
cabergoline

35
Q

bromocriptine and cabergoline MOA

A

potent D2 receptor agonist

36
Q

indications for bromocriptine

A

hyperprolactinemia associated dysfunctions (amenorrhea, prolactin-secreting adenomas), acromegaly, treatment of T2DM as adjunct to diet & exercise

37
Q

indications for cabergoline

A

hyperprolactinemia, prolactin-secreting tumors, reduce breast milk production

38
Q

ergots for parkinson’s disease

A

NO!!! not effective

39
Q

agents that are effective in treatment of parkinson’s disease

A

ropinirole
pramipexole
rasagiline

40
Q

rapid withdrawal is serious for which drugs

A

D2 agonists

41
Q

which drugs are D2 agonists

A

ropinirole and pramipexole

42
Q

which drug is MAO-B inhibitor

A

rasagiline

neurology/psychiatry (22 decks)

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