DIHYDROERGOTAMINE MESYLATE injection

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

Hikma Pharmaceuticals USA Inc.

Administration route:

INTRAMUSCULAR

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

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 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 angina

Product summary:

Dihydroergotamine Mesylate Injection, USP Available as a clear, colorless, sterile solution in single 1 mL sterile vials containing 1 mg of dihydroergotamine mesylate per mL, in packages of 10 (NDC 0143-9151-10). Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15° to 30ºC (59º to 86ºF) [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 vials from light and heat. Administer only if clear and colorless.

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

DIHYDROERGOTAMINE MESYLATE- DIHYDROERGOTAMINE MESYLATE INJECTION
HIKMA PHARMACEUTICALS USA INC.
----------
DIHYDROERGOTAMINE MESYLATE INJECTION, USP
RX ONLY
BOXED WARNING
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 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 STRUCTURAL FORMULA
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
vials 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).
33
37
5
5
4
3
33
37
5
5
4
3
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 α2A, α2B and α1 receptors, and dopamine D and D
receptors.
The therapeutic activity of dihydroergotamine in migraine is generally
attributed to the
agonist e