receptors in the central nervous system play
important roles in extrapyramidal motor control and the
regulation of pituitary prolactin release.
dopamine receptors
have the
highest selectivity for the pituitary dopamine receptors.
These drugs directly suppress prolactin secretion from
pituitary cells by activating regulatory dopamine
receptors.
Bromocriptine, cabergoline, and pergolide
In humans, (blank) and similar
compounds constrict most vessels in nanomolar
concentrations. The vasospasm is prolonged.
This response is partially blocked by
conventional a- blocking agents.
ergotamine
all have partial agonist effects at
5-HT 2 vascular receptors. The remarkably
specific antimigraine action of the ergot
derivatives was originally thought to be related
to their actions on vascular serotonin receptors.
Ergotamine, ergonovine, and
methysergide
After overdosage with ergotamine and similar
agents, vasospasm is (blank).
This vasospasm is not easily reversed by a
antagonists, serotonin antagonists, or
combinations of both.
severe and prolonged
is typical of the ergot alkaloids that
have a strong vasoconstrictor spectrum of
action.
Ergotamine
The stimulant action of ergot alkaloids on the
uterus, as on vascular smooth muscle, appears
to combine a
agonist, serotonin agonist, and
other effects.
Furthermore, the sensitivity of the uterus to the
stimulant effects of ergot increases dramatically
during pregnancy, perhaps because of
increasing dominance of (blank) as
pregnancy progresses. As a result, the uterus at
term is more sensitive to ergot than earlier in
pregnancy and far more sensitive than the
nonpregnant organ.
a 1 receptors
these drugs induce
powerful and prolonged contracture.
At higher concentrations,
is more selective than other ergot
alkaloids in affecting the uterus and is the agent
of choice in obstetric applications of the ergot drugs
Ergonovine
Ergonovine is more selective than other ergot
alkaloids in affecting the uterus and is the agent
of choice in obstetric applications of the ergot drugs although (blank), the peptide hormone,
is preferred in most cases.
oxytocin
little or no significant effect on bronchiolar
or urinary smooth muscle.
ergot alkaloids
The (blank), on the other
hand, is quite sensitive. Nausea, vomiting,
and diarrhea may be induced even by low
doses in some patients.
gastrointestinal tract
The effect is (blank) with action on the
central nervous system emetic center and
on gastrointestinal serotonin receptors.
consistent
Ergot derivatives are highly specific for
migraine pain
is available for oral,
sublingual, rectal suppository, and inhaler use.
Ergotamine tartrate
It is often combined with (blank) to
facilitate absorption of the ergot alkaloid.
caffeine (
how many mg of
caffeine for each 1 mg ergotamine tartrate
100 mg
The vasoconstriction induced by ergotamine is
long-lasting and cumulative when the drug is
taken repeatedly, as in a
severe migraine attack
Therefore, patients must be carefully informed
that no more than (blank) of the oral preparation
may be taken for each attack and no more than
(blank) per week.
6 mg, 10 mg