Држава: Сједињене Америчке Државе
Језик: Енглески
Извор: NLM (National Library of Medicine)
Dihydroergotamine Mesylate (UNII: 81AXN7R2QT) (Dihydroergotamine - UNII:436O5HM03C)
Apollo Pharmaceuticals Inc.
INTRAVENOUS
PRESCRIPTION DRUG
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 a
Available as a clear, colorless, sterile solution in single 1 mL sterile ampules containing 1 mg of dihydroergotamine mesylate per mL, in packages of 5 (NDC 61990-0411-1) and 10 (NDC 61990-0411-2). Store at 20° to 25°C (68° to 77°F); excursions permitted between 15° to 30°C (59° to 86°F). 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.
Abbreviated New Drug Application
DIHYDROERGOTAMINE MESYLATE- DIHYDROERGOTAMINE MESYLATE INJECTION, SOLUTION APOLLO PHARMACEUTICALS INC. ---------- DIHYDROERGOTAMINE MESYLATE INJECTION, USP RX ONLY 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)_. 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; 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). 33 37 5 5 4 3 33 37 5 5 4 3 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 been proposed to explain the efficacy of 5-HT receptor agonists in mi Прочитајте комплетан документ