DROMELATE- dihydroergotamine mesylate injection, solution

Kraj: Stany Zjednoczone

Język: angielski

Źródło: NLM (National Library of Medicine)

Składnik aktywny:

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

Dostępny od:

IT3 Medical LLC

Droga podania:

SUBCUTANEOUS

Typ recepty:

PRESCRIPTION DRUG

Wskazania:

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 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 Injection, USP 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 findings consistent with coronary artery vasospasm including Prinzmetal's variant angina. (See

Podsumowanie produktu:

Available as a clear, colorless, sterile solution in single 1 mL sterile ampules containing 1 mg of dihydroergotamine mesylate per mL.         Packages of 5: NDC 0574-0850-05         Packages of 10: NDC 0574-0850-10 Store at 20 to 25°C (68 to 77°F). Excursions permitted between 15 to 30°C (59 to 86°F) [See USP Controlled Room Temperature]. Do not refrigerate or freeze. To assure constant potency, protect the ampules from light and heat. Use carton to protect contents from light until used. Administer only if clear and colorless.

Status autoryzacji:

Abbreviated New Drug Application

Charakterystyka produktu

DROMELATE- DIHYDROERGOTAMINE MESYLATE INJECTION, SOLUTION
IT3 MEDICAL LLC
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DROMELATE INJECTION SYSTEM
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_ SECTIONS_)
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)-,
monomethanesulfonate. Its molecular weight is 679.80 and its molecular
formula is
C
H
N O •CH O S.
The chemical structure is:
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 - 4.9.
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 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 migraine. One theory suggests that
activation of 5-HT
receptors located on intracranial blood vessels, including those on
arterio-venous anastomoses, leads to vas