DIHYDROERGOTAMINE MESYLATE NASAL spray, metered

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

Exelan Pharmaceuticals, Inc.

Administration route:

NASAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

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 or

Product summary:

Dihydroergotamine mesylate nasal spray is available (as a clear, colorless to faintly yellow solution) in 3.5 mL amber glass vials containing 4 mg of dihydroergotamine mesylate. 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 76282-680-43). Each carton contains eight such units. (NDC 76282-680-44). Store below 25°C (77°F). Do not refrigerate or freeze.             Disclaimer: Other brands listed are the registered trademarks of their respective owners and are not trademarks of Exelan Pharmaceuticals, Inc. Manufactured by: Mipharm, S.p.A. Milan, Italy Manufactured for: Exelan Pharmaceutical Inc., Boca Raton, FL 33432 Issued: 06/2020

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

DIHYDROERGOTAMINE MESYLATE NASAL- DIHYDROERGOTAMINE MESYLATE NASAL
SPRAY,
METERED
EXELAN PHARMACEUTICALS, INC.
----------
DIHYDROERTOTAMINE MESYLATE NASAL SPRAY, 4 MG/ML
THE SOLUTION USED IN DIHYDROERGOTAMINE MESYLATE NASAL SPRAY (4 MG/ML)
IS INTENDED FOR
INTRANASAL USE AND MUST NOT BE INJECTED.
Rx Only
WARNING
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)_
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:
Dihydroergotamine mesylate nasal spray is provided for intranasal
administration as a clear, colorless
to faintly yellow solution in an amber glass vial containing:
dihydroergotamine mesylate……………4 mg
caffeine, anhydrous……………………. 10 mg
33
37
5
5
4
3
dextrose, anhydrous…………………… 50 mg
carbon dioxide………………………….qs
purified water ………………………….qs 1 mL
Each milliliter contains
Dihydroergotamine mesylate……4 mg
(equivalent to 3.43 mg dihydroergotamine)
CLINICAL PHARMACOLOGY
MECHANISM OF ACTION
Dihydroergotamine binds with high affinity to 5-HT
and 5-HT
receptors. It also binds with high
affinity to serotonin 5-HT
, 5-HT
, and 5-HT
receptors, noradrenaline α
, α
and α receptors,
and dopamine D and D receptors.
The therapeutic activity of dihydroergotamine in migrain