DIHYDROERGOTAMINE MESYLATE spray

Држава: Сједињене Америчке Државе

Језик: Енглески

Извор: NLM (National Library of Medicine)

Активни састојак:

DIHYDROERGOTAMINE MESYLATE (UNII: 81AXN7R2QT) (DIHYDROERGOTAMINE - UNII:436O5HM03C)

Доступно од:

Hikma Pharmaceuticals USA Inc.

Пут администрације:

NASAL

Тип рецептора:

PRESCRIPTION DRUG

Терапеутске индикације:

Dihydroergotamine mesylate nasal spray is indicated for the acute treatment of migraine headaches with or without aura. Dihydroergotamine mesylate nasal spray is not intended for the prophylactic therapy of migraine or for the management of hemiplegic or basilar migraine. There have been a few reports of serious adverse events associated with the coadministration of dihydroergotamine and potent CYP 3A4 inhibitors, such as protease inhibitors and macrolide antibiotics, resulting in vasospasm that led to cerebral ischemia and/or ischemia of the extremities. The use of potent CYP 3A4 inhibitors (ritonavir, nelfinavir, indinavir, erythromycin, clarithromycin, troleandomycin, ketoconazole, itraconazole) with dihydroergotamine is, therefore contraindicated (see WARNINGS: CYP 3A4 Inhibitors ). Dihydroergotamine mesylate nasal spray should not be given to patients with ischemic heart disease (angina pectoris, history of myocardial infarction, or documented silent ischemia) or to patients who have clinical symptoms

Резиме производа:

Dihydroergotamine mesylate nasal spray is available (as a clear, colorless to light yellow aqueous solution) in 3.5 mL amber glass vials containing 4 mg of dihydroergotamine mesylate, USP. Dihydroergotamine mesylate nasal spray is provided as a package of 8 units, administration instruction sheet, and one package insert. Each unit consists of one vial and one sprayer. (NDC 24201-463-08) Store below 25°C (77°F). Do not refrigerate or freeze. Manufactured for: Hikma Pharmaceuticals USA Inc. Berkeley Heights, NJ 07922 Made in Italy 934035 USA Rev. 07/2022

Статус ауторизације:

Abbreviated New Drug Application

Карактеристике производа

DIHYDROERGOTAMINE MESYLATE- DIHYDROERGOTAMINE MESYLATE SPRAY
HIKMA PHARMACEUTICALS USA INC.
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DIHYDROERGOTAMINE MESYLATE NASAL SPRAY
THE SOLUTION USED IN DIHYDROERGOTAMINE MESYLATE NASAL SPRAY (4 MG/ML)
IS
INTENDED FOR INTRANASAL USE AND MUST NOT BE INJECTED.
RX ONLY
WARNING: PERIPHERAL ISCHEMIA FOLLOWING COADMINISTRATION
WITH POTENT CYP3A4 INHIBITORS
DESCRIPTION
Dihydroergotamine mesylate is ergotamine hydrogenated in the 9,10
position as the
mesylate salt. Dihydroergotamine mesylate is known chemically as
ergotaman-3', 6', 18-
trione, 9,10-dihydro-12'-hydroxy-2'-methyl-5'- (phenylmethyl)-,
(5'α)-, monomethane-
sulfonate. Its molecular weight is 679.78 and its empirical formula is
C
H
N O •CH O S.
The chemical structure is:
SERIOUS AND/OR LIFE-THREATENING PERIPHERAL ISCHEMIA HAS BEEN
ASSOCIATED WITH THE COADMINISTRATION OF DIHYDROERGOTAMINE WITH
POTENT CYP 3A4 INHIBITORS INCLUDING PROTEASE INHIBITORS AND
MACROLIDE ANTIBIOTICS. BECAUSE CYP 3A4 INHIBITION ELEVATES THE
SERUM LEVELS OF DIHYDROERGOTAMINE, THE RISK FOR VASOSPASM
LEADING TO CEREBRAL ISCHEMIA AND/OR ISCHEMIA OF THE EXTREMITIES IS
INCREASED. HENCE, CONCOMITANT USE OF THESE MEDICATIONS IS
CONTRAINDICATED.
(SEE ALSO _CONTRAINDICATIONS AND WARNINGS _SECTION)
33
37
5
5
4
3
Dihydroergotamine mesylate nasal spray is provided for intranasal
administration as a
clear, colorless to light yellow aqueous solution in an amber glass
vial containing:
Each milliliter contains
(equivalent to 3.43 mg dihydroergotamine)
CLINICAL PHARMACOLOGY
MECHANISM OF ACTION
Dihydroergotamine binds with high affinity to 5-HT1Dα and 5-HT1Dβ
receptors. It also
binds with high affinity to serotonin 5-HT1A, 5-HT2A, and 5-HT2C
receptors,
noradrenaline α2A, α2B and α1 receptors, and dopamine D2L and D3
receptors.
The therapeutic activity of dihydroergotamine in migraine is generally
attributed to the
agonist effect at 5-HT1D receptors. Two current theories have been
proposed to explain
the efficacy of 5-HT1D receptor agonists in migraine. One theory
suggests that
activation