BUTORPHANOL TARTRATE injection

Země: Spojené státy

Jazyk: angličtina

Zdroj: NLM (National Library of Medicine)

Aktivní složka:

BUTORPHANOL TARTRATE (UNII: 2L7I72RUHN) (BUTORPHANOL - UNII:QV897JC36D)

Dostupné s:

Cardinal Health

INN (Mezinárodní Name):

BUTORPHANOL TARTRATE

Složení:

BUTORPHANOL TARTRATE 1 mg in 1 mL

Druh předpisu:

PRESCRIPTION DRUG

Stav Autorizace:

Abbreviated New Drug Application

Charakteristika produktu

BUTORPHANOL TARTRATE- BUTORPHANOL TARTRATE INJECTION
CARDINAL HEALTH
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BUTORPHANOL TARTRATE INJECTION USP
RX ONLY.
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 477.56
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 USP 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 of
solution contains 3.3 mg of citric acid, 7.29 mg sodium citrate, and
6.4 mg sodium chloride, and 0.1 mg
benzethonium chloride (in multiple dose vial only) as a preservative.
The pH range is 3.5 to 5.0.
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 k-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 butorphanol tartrate required to
antagonize morphine analgesia by 50%
was similar to that for nalorphine, less than that for penta