DIHYDROERGOTAMINE (DHE), 1MG/ML LIQUID

Country: Canada

Language: English

Source: Health Canada

Active ingredient:

DIHYDROERGOTAMINE MESYLATE

Available from:

STERIMAX INC

ATC code:

N02CA01

INN (International Name):

DIHYDROERGOTAMINE

Dosage:

1MG

Pharmaceutical form:

LIQUID

Composition:

DIHYDROERGOTAMINE MESYLATE 1MG

Administration route:

INTRAMUSCULAR

Units in package:

1ML

Prescription type:

Prescription

Therapeutic area:

SYMPATHOLYTIC (ADRENERGIC BLOCKING) AGENTS

Product summary:

Active ingredient group (AIG) number: 0108813001; AHFS:

Authorization status:

APPROVED

Authorization date:

1997-08-01

Summary of Product characteristics

1
PRESCRIBING INFORMATION
PR
DIHYDROERGOTAMINE (DHE)
(dihydroergotamine mesylate injection USP)
Solution, 1 mg / mL for Subcutaneous, Intramuscular or Intravenous Use
USP
Migraine Therapy
SteriMax Inc.
2770 Portland Drive
Oakville ON
L6H 6R4
Date of Revision:
October 1, 2019
2
PRESCRIBING INFORMATION
PR
DIHYDROERGOTAMINE (DHE)
(dihydroergotamine mesylate injection USP)
Solution, 1 mg / mL
THERAPEUTIC CLASSIFICATION
Migraine Therapy
ACTIONS AND CLINICAL PHARMACOLOGY
Dihydroergotamine displays agonist activity at the 5-HT
1Da
and 5-HT
1Dß
receptors,
which, by reducing 5-HT neuronal function and/or contracting elements
of the cranial
vasculature and/or suppressing neurogenic inflammation, is believed to
underlie its anti-
migraine efficacy. It also displays affinity for the 5-HT
1A
and 5-HT
1C
receptors and
antagonistic activity at the 5-HT
2
subtype. Dihydroergotamine displays blocking actions
at alpha adrenoreceptors, with a direct stimulating effect on the
smooth muscle of
peripheral blood vessels. Its tonic effect on capacitance vessels
(veins) is particularly
pronounced, compared to its effects on resistance vessels
(arterioles). Dihydroergotamine
differs from ergotamine by being more potent with respect to its
adrenergic blocking
actions and less potent with respect to its capacity to produce
arterial vasoconstriction,
but it maintains a marked venoconstrictor effect. Dihydroergotamine
reduces the
incidence and degree of nausea, photophobia, and phonophobia.
Dihydroergotamine is 93% bound to plasma proteins. Its apparent volume
of distribution
is about 30 L/kg. The total body clearance is about 1.5 L/min.,
reflecting mainly the
3
hepatic clearance. Elimination from the plasma is biphasic with an
a-phase of 1.5 hours
and a ß-phase of 15 hours. The major route of excretion is via the
bile in the faeces.
Urinary excretion of parent substance and metabolites amounts to about
10% after
intravenous administration.
Pharmacokinetic interactions have been reported in patients treated
orally with other
ergot alkaloids