DIHYDROERGOTAMINE MESYLATE injection, solution

Negara: Amerika Serikat

Bahasa: Inggris

Sumber: NLM (National Library of Medicine)

Bahan aktif:

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

Tersedia dari:

Paddock Laboratories, LLC.

Rute administrasi :

SUBCUTANEOUS

Jenis Resep:

PRESCRIPTION DRUG

Indikasi Terapi:

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. (Se

Ringkasan produk:

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 0574-0851-05         Packages of 10: NDC 0574-0851-10 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 otorisasi:

Abbreviated New Drug Application

Karakteristik produk

DIHYDROERGOTAMINE MESYLATE- DIHYDROERGOTAMINE MESYLATE INJECTION,
SOLUTION
PADDOCK LABORATORIES, LLC.
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DIHYDROERGOTAMINE MESYLATE INJECTION, USP
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'a)-,monomethanesullonate. Its
molecular weight is 679.80 and
its molecular formula is C
H N 0 •CH 0 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.
CLINICAL PHARMACOLOGY
MECHANISM OF ACTION
33
37
5
5
4
3
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 art