Kraj: Stany Zjednoczone
Język: angielski
Źródło: NLM (National Library of Medicine)
butorphanol tartrate (UNII: 2L7I72RUHN) (butorphanol - UNII:QV897JC36D)
Apotex Inc.
butorphanol tartrate
2 mg in 1 mL
PRESCRIPTION DRUG
BUTORPHANOL TARTRATE- BUTORPHANOL TARTRATE INJECTION, SOLUTION APOTEX INC. ---------- BUTORPHANOL TARTATE INJECTION USP RX ONLY CIV DESCRIPTION Butorphanol tartrate is a synthetically derived opioid agonist-antagonist analgesic of the phenanthrene series. The chemical name is ( – )-17-(cyclobutylmethyl)morphinan-3,14-diol D- ( – ) - tartrate (1:1) (salt). The molecular formula is C H NO •C H O , which corresponds to a molecular weight of 477.55 and the following structural formula: Butorphanol tartrate is a white crystalline substance. The dose is expressed as the tartrate salt. One milligram of the salt is equivalent to 0.68 mg of the free base. The n-octanol/ aqueous buffer partition coefficient of butorphanol is 180:1 at pH 7.5. Butorphanol tartrate injection is a sterile, parenteral, aqueous solution of butorphanol tartrate for intravenous or intramuscular administration. In addition to 1 or 2 mg of butorphanol tartrate, each mL contains 3.3 mg of citric acid, 7.29 mg sodium citrate dihydrate (equivalent to 6.4 mg sodium citrate, anhydrous), and 6.4 mg of sodium chloride, and 0.1 mg benzethonium chloride (in multiple dose vial only) as a preservative. The pH range is 3.0 to 5.5. CLINICAL PHARMACOLOGY GENERAL PHARMACOLOGY AND MECHANISM OF ACTION Butorphanol is a mixed agonist-antagonist with low intrinsic activity at receptors of the µ-opioid type (morphine-like). It is also an agonist at κ-opioid receptors. Its interactions with these receptors in the central nervous system apparently mediate most of its pharmacologic effects, including analgesia. In addition to analgesia, CNS effects include depression of spontaneous respiratory activity and cough, stimulation of the emetic center, miosis and sedation. Effects possibly mediated by non-CNS mechanisms include alteration in cardiovascular resistance and capacitance, bronchomotor tone, gastrointestinal secretory and motor activity and bladder sphincter activity. In an animal model, the dose of the butorphanol tartrate required to antagonize morphine anal Przeczytaj cały dokument