DIHYDROERGOTAMINE MESYLATE injection, solution

Maa: Yhdysvallat

Kieli: englanti

Lähde: NLM (National Library of Medicine)

Aktiivinen ainesosa:

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

Saatavilla:

Apollo Pharmaceuticals Inc.

Antoreitti:

INTRAVENOUS

Prescription tyyppi:

PRESCRIPTION DRUG

Käyttöaiheet:

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 a

Tuoteyhteenveto:

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 61990-0411-1) and 10 (NDC 61990-0411-2). Store at 20° to 25°C (68° to 77°F); excursions permitted between 15° to 30°C (59° to 86°F). 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.

Valtuutuksen tilan:

Abbreviated New Drug Application

Valmisteyhteenveto

DIHYDROERGOTAMINE MESYLATE- DIHYDROERGOTAMINE MESYLATE INJECTION,
SOLUTION
APOLLO PHARMACEUTICALS INC.
----------
DIHYDROERGOTAMINE MESYLATE INJECTION, USP
RX ONLY
WARNING
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).
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
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 efficacy of 5-HT
receptor agonists in mi