BUTORPHANOL TARTRATE injection solution

Država: Združene države Amerike

Jezik: angleščina

Source: NLM (National Library of Medicine)

Aktivna sestavina:

butorphanol tartrate (UNII: 2L7I72RUHN) (butorphanol - UNII:QV897JC36D)

Dostopno od:

Apotex Inc.

INN (mednarodno ime):

butorphanol tartrate

Sestava:

2 mg in 1 mL

Tip zastaranja:

PRESCRIPTION DRUG

Lastnosti izdelka

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