DIHYDROERGOTAMINE MESYLATE injection

מדינה: ארצות הברית

שפה: אנגלית

מקור: NLM (National Library of Medicine)

מרכיב פעיל:

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

זמין מ:

Hikma Pharmaceuticals USA Inc.

INN (שם בינלאומי):

DIHYDROERGOTAMINE MESYLATE

הרכב:

DIHYDROERGOTAMINE MESYLATE 1 mg in 1 mL

מסלול נתינה (של תרופות):

INTRAMUSCULAR

סוג מרשם:

PRESCRIPTION DRUG

סממני תרפויטית:

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. (See WARNINGS). Because dihydroergotamine mesylate injection may increase blood pressure, it should not be given to patients with uncontrolled hypertension. Dihydroergotamine mesylate injection, 5-HT1 agonists (e.g., sumatriptan), ergotamine-containing or ergot-type medications or methysergide should not be used within 24 hours of each other. Dihydroergotamine mesylate injection should not be administered to patients with hemiplegic or basilar migraine. In addition to those conditions mentioned above, dihydroergotamine mesylate injection is also contraindicated in patients with known peripheral arterial disease, sepsis, following vascular surgery and severely impaired hepatic or renal function. Dihydroergotamine mesylate injection is contraindicated in patients who have previously shown hypersensitivity to ergot alkaloids. Dihydroergotamine mesylate should not be used with peripheral and central vasoconstrictors because the combination may result in additive or synergistic elevation of blood pressure.   Currently available data have not demonstrated drug abuse or psychological dependence with dihydroergotamine. However, cases of drug abuse and psychological dependence in patients on other forms of ergot therapy have been reported. Thus, due to the chronicity of vascular headaches, it is imperative that patients be advised not to exceed recommended dosages.

leaflet_short:

Dihydroergotamine Mesylate Injection, USP Available as a clear, colorless, sterile solution in single 1 mL sterile ampules containing 1 mg of dihydroergotamine mesylate per mL, in packages of 10 (NDC 0143-9273-10). 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 ampules from light and heat. Administer only if clear and colorless.

מצב אישור:

Abbreviated New Drug Application

מאפייני מוצר

DIHYDROERGOTAMINE MESYLATE- DIHYDROERGOTAMINE MESYLATE INJECTION
HIKMA PHARMACEUTICALS USA 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_
_ 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;
33
37
5
5
4
3
33
37
5
5
4
3
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 be