Maa: Yhdysvallat
Kieli: englanti
Lähde: NLM (National Library of Medicine)
Dihydroergotamine Mesylate (UNII: 81AXN7R2QT) (Dihydroergotamine - UNII:436O5HM03C)
Bausch Health US, LLC
Dihydroergotamine Mesylate
Dihydroergotamine Mesylate 1 mg in 1 mL
INTRAVENOUS
PRESCRIPTION DRUG
D.H.E. 45 (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 ). D.H.E. 45 (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 includi
Available as a clear, colorless, sterile solution in single 1 mL sterile ampuls containing 1 mg of dihydroergotamine mesylate per mL, in packages of 10 (NDC 66490-041-01). 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]. Use carton to protect contents from light until used. Do not refrigerate or freeze. To assure constant potency, protect the ampuls from light and heat. Administer only if clear and colorless.
New Drug Application
D.H.E. 45- DIHYDROERGOTAMINE MESYLATE INJECTION, SOLUTION BAUSCH HEALTH US, LLC ---------- D.H.E. 45® (DIHYDROERGOTAMINE MESYLATE) INJECTION, USP WARNING: PERIPHERAL ISCHEMIA FOLLOWING COADMINISTRATION WITH POTENT CYP3A4 INHIBITORS DESCRIPTION D.H.E. 45 is ergotamine hydrogenated in the 9, 10 position as the mesylate salt. D.H.E. 45 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 D.H.E. 45 (dihydroergotamine mesylate) Injection, USP is a clear, colorless solution supplied in sterile ampuls 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 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. 33 37 5 5 4 3 33 37 5 5 4 3 1D 1D 1A 2A 2C 2A 2B 1 2L 3 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 arteriovenous anastomoses, leads to vasoconstriction, which correlates with the relief of migraine headache. The alternative hypothesis suggests that activation of 5-HT receptors on sensory nerve endings of the trigeminal system results in the inhibition of pro-inflammatory neuropeptide release. In addition, dihydroergotamine possess Lue koko asiakirja