DIHYDROERGOTAMINE MESYLATE injection, solution

Quốc gia: Hoa Kỳ

Ngôn ngữ: Tiếng Anh

Nguồn: NLM (National Library of Medicine)

Thành phần hoạt chất:

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

Sẵn có từ:

Padagis US LLC

INN (Tên quốc tế):

Dihydroergotamine Mesylate

Thành phần:

Dihydroergotamine Mesylate 1 mg in 1 mL

Tuyến hành chính:

SUBCUTANEOUS

Loại thuốc theo toa:

PRESCRIPTION DRUG

Chỉ dẫn điều trị:

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

Tóm tắt sản phẩm:

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.         Packages of 5 (NDC 0574-0850-05)         Packages of 10 (NDC 0574-0850-10) 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]. 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.

Tình trạng ủy quyền:

Abbreviated New Drug Application

Đặc tính sản phẩm

DIHYDROERGOTAMINE MESYLATE- DIHYDROERGOTAMINE MESYLATE INJECTION,
SOLUTION
PADAGIS US LLC
----------
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 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 empirical
formula is
C
H
N O •CH O S.
The chemical structure is:
33
37
5
5
4
3
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
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
recep