Ergot Alkaloids - Therapeutic Uses Flashcards
What are the therapeutic uses of ergots?
1 - Migraine headache 2 - treatment of postpartum hemorrhage 3 - treatment of hyperprolactemia 4 - treatment of Parkinson's disease 5 - diagnosis of variant angina 6 - senile cerebral insufficiency
Which ergots are used to treat migraine headaches?
- Ergotamine: for early stages, 5HT1a/1b/1d and 5HT-2 partial agonist, also D2. Better absorbed rectally but if used orally it is usually complexed with caffeine (Cafergot). Long lasting vasoconstriction which can be a problem
- Metoclopramide is given with ergotamine to enhance gastric emptying and as an anti-emetic
- Dihydroergotamine (DHE) for patients with long-lasting attacks of greater than 48 hours (status migraines)
- Methysergide (Sansert): for migraine prophylaxis only (before), Inhibits NO, serotonin and histamine release
What is a major problem with ergotamine?
Ergotamine -induced headache and rebound headache associated with frequent use
Which is the only parenterally formulated ergot?
Dihydroergotamine (DHE). Used IV, IM, SC, nasally.
Since Dihydroergotamine (DHE) is also a D2 receptor agonist, what do you give with it to avoid vomiting?
D2 blocker
Treatment with Methysergide (Sansert) must not exceed?
Six continuous months. You must have a 3 to 4 week drug-free interval due to risk of retroperitoneal fibrosis, pulmonary fibrosis, thickening of the aortic and mitral valves because its metabolite is a very potent 5HT-2D agonist.
Which ergot has behavioral changes reminiscent of mild LSD reaction as a side effect?
Methysergide (Sansert)
Which ergots are used to treat postpartum hemorrhage?
Ergonovine and methyergonovine (the ones with “no” in the name)
Which ergots are used in the treatment of hyperprolactemia?
Bromocriptine mesylate (Parlodel) and Pergolide (Permax) because they are D2 agonists.
Breast-feeding mothers who want to stop lactating should not use bromocriptine because of what risk?
Increased risk of stroke
Which ergots are used in the treatment of Parkinson’s disease?
Bromocriptine as monotherapy or as an adjunct to LDOPA.
Orthostatic hypotension is a side effect of what ergot?
Bromocriptine
Which ergots are used in the diagnosis of variant angina?
Ergonovine which produces a diagnostic vasoconstriction of coronary arteries that are prone to vassal spasms as in variant angina. Administered IV.
Which ergots are used to treat senile cerebral insufficiency?
Dihydroergotoxine (Hydergine). It is a mixture of dihydroergocryptine and three similar by hydrogenated peptide ergot alkaloids.
What are some acute side effects of ergot alkaloids?
- Nausea and vomiting
- abdominal pain and cramping
- paresthesias
- swollen fingers
- leg cramps
- tremor
- diarrhea
- confusion
- unconsciousness
- myocardial infarction
- cerebral vasospasms
