DIHYDROERGOTAMINE MESYLATE injection, solution

Land: USA

Språk: engelsk

Kilde: NLM (National Library of Medicine)

Aktiv ingrediens:

Dihydroergotamine Mesylate (UNII: 81AXN7R2QT) (Dihydroergotamine - UNII:436O5HM03C)

Tilgjengelig fra:

Provepharm Inc.

Administreringsrute:

INTRAVENOUS

Resept typen:

PRESCRIPTION DRUG

Indikasjoner:

Dihydroergotamine Mesylate Injection, USP is indicated for the acute treatment of migraine headaches with or without aura and the acute treatment of cluster headache episodes. There have been a few reports of serious adverse events associated with the coadministration of dihydroergotamine and potent CYP3A4 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 CYP3A4 inhibitors (i.e., ritonavir, nelfinavir, indinavir, erythromycin, clarithromycin, troleandomycin, ketoconazole, itraconazole) with dihydroergotamine is, therefore, contraindicated (see WARNINGS, CYP3A4 Inhibitors). Dihydroergotamine Mesylate Injection, USP should not be given to patients with ischemic heart disease (e.g., angina pectoris, history of myocardial infarction, or documented silent ischemia) or to patients who have clinical symptoms or findings consistent with coronary artery vasospasm including Prinzmetal's variant an

Produkt oppsummering:

Available as a clear, colorless, sterile solution in single 1 mL sterile ampules containing 1 mg of dihydroergotamine mesylate per mL, in packages of 5 (NDC 81284-411-05) and 10 (NDC 81284-411-10). Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature]. Use carton to protect contents from light until used. Do not refrigerate or freeze. To assure constant potency, protect the ampules from light and heat. Administer only if clear and colorless. *Trademark of PDR Network, LLC Manufactured for: Provepharm SAS Distributed by: Provepharm, Inc. Collegeville, PA 19426 Made in France Revised: 11/2022

Autorisasjon status:

Abbreviated New Drug Application

Preparatomtale

DIHYDROERGOTAMINE MESYLATE- DIHYDROERGOTAMINE MESYLATE INJECTION,
SOLUTION
PROVEPHARM INC.
----------
DIHYDROERGOTAMINE MESYLATE INJECTION, USP
RX ONLY
WARNING: PERIPHERAL ISCHEMIA FOLLOWING COADMINISTRATION WITH POTENT
CYP3A4
INHIBITORS
SERIOUS AND/OR LIFE-THREATENING PERIPHERAL ISCHEMIA HAS BEEN
ASSOCIATED WITH THE
COADMINISTRATION OF DIHYDROERGOTAMINE WITH POTENT CYP3A4 INHIBITORS
INCLUDING PROTEASE
INHIBITORS AND MACROLIDE ANTIBIOTICS. BECAUSE CYP3A4 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).
DESCRIPTION
Dihydroergotamine Mesylate Injection, USP is ergotamine hydrogenated
in the 9, 10 position as the mesylate
salt. Dihydroergotamine Mesylate Injection, USP is known chemically as
ergotaman-3´,6´,18-trione,9,10-
dihydro-12´-hydroxy-2´-methyl-5´-(phenylmethyl)-,(5´α)-,
monomethanesulfonate. Its molecular weight is
679.80 and its empirical formula is C
H
N O •CH O S.
The chemical structure is:
Dihydroergotamine mesylate
C
H
N O •CH O S Mol. Wt. 679.80
Dihydroergotamine Mesylate Injection, USP is a clear, colorless
solution supplied in sterile ampules for
intravenous, intramuscular, or subcutaneous administration. Each mL
contains 1 mg Dihydroergotamine
Mesylate, USP; Alcohol, USP 6.1% by volume; Glycerin, USP 15% by
weight; Water for Injection, USP;
Methanesulfonic Acid and/or Sodium Hydroxide for pH adjustment (pH
range is 3.4 to 4.9).
CLINICAL PHARMACOLOGY
MECHANISM OF ACTION
Dihydroergotamine binds with high affinity to 5-HT
α and 5-HT
β 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 migraine is generally
attributed to the agonist effect at 5-
HT
receptors. Two current theories have been proposed to explain the
effic