Land: USA
Språk: engelska
Källa: NLM (National Library of Medicine)
DIHYDROERGOTAMINE MESYLATE (UNII: 81AXN7R2QT) (DIHYDROERGOTAMINE - UNII:436O5HM03C)
Hikma Pharmaceuticals USA Inc.
DIHYDROERGOTAMINE MESYLATE
DIHYDROERGOTAMINE MESYLATE 1 mg in 1 mL
INTRAMUSCULAR
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 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.
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.
Abbreviated New Drug Application
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 Läs hela dokumentet