DOLOREX- butorphanol tartrate injection

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

Butorphanol Tartrate (UNII: 2L7I72RUHN) (Butorphanol - UNII:QV897JC36D)

Available from:

Merck Sharp & Dohme Corp.

INN (International Name):

Butorphanol Tartrate

Composition:

Butorphanol 10 mg in 1 mL

Administration route:

INTRAVENOUS

Prescription type:

PRESCRIPTION

Therapeutic indications:

DOLOREX (butorphanol tartrate) is indicated for the relief of pain associated with colic in adult horses and yearlings. Clinical studies in the horse have shown that butorphanol tartrate alleviates abdominal pain associated with torsion, impaction, intussusception, spasmodic and tympanic colic, and postpartum pain.

Product summary:

DOLOREX is supplied in 50 mL vials (Order Code No. 017070). Store at or below 25°C (77°F).

Authorization status:

Abbreviated New Animal Drug Application

Summary of Product characteristics

DOLOREX- BUTORPHANOL TARTRATE INJECTION
MERCK SHARP & DOHME CORP.
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DOLOREX
(BUTORPHANOL TARTRATE)
CIV
CAUTION
Federal law restricts this drug to use by or on the order of a
licensed veterinarian.
DESCRIPTION
DOLOREX (butorphanol tartrate) is a totally synthetic, centrally
acting, narcotic agonist-antagonist
analgesic with potent antitussive activity. It is a member of the
phenanthrene series. The chemical name
is Morphinan-3, 14-diol, 17-(cyclobutylmethyl)-, (-)-, (S- (R*, R*))-
2, 3- dihydroxybutanedioate (1:1)
(salt). It is a white crystalline, water soluble substance having a
molecular weight of 477.55; its
molecular formula is C
H NO C H O .
Each mL of DOLOREX contains 10 mg butorphanol base (as butorphanol
tartrate, USP), 3.3 mg citric
acid, Ph.Eur., 6.4 mg sodium citrate, Ph.Eur., 4.7 mg sodium chloride,
Ph.Eur., and 0.1 mg benzethonium
chloride, Ph.Eur., q.s. with water for injection, Ph.Eur.
COMPARATIVE PHARMACOLOGY
In animals, butorphanol has been demonstrated to be 4 to 30 times more
potent than morphine and
pentazocine (Talwin -V) respectively.
In humans, butorphanol has been shown to have 5 to 7 times the
analgesic activity of morphine and 20 times that of pentazocine.
Butorphanol has 15 to 20 times the
oral antitussive activity of codeine or dextromethorphan in dogs and
guinea pigs.
As an antagonist, butorphanol is approximately equivalent to
nalorphine and 30 times more potent than
pentazocine.
Cardiopulmonary depressant effects are minimal after treatment with
butorphanol as demonstrated in
dogs , humans
and horses.
Unlike classical narcotic agonist analgesics which are associated with
decreases in blood pressure, reduction in heart rate, and concomitant
release of histamine, butorphanol
does not cause histamine release.
Furthermore, the cardiopulmonary effects of butorphanol are not
distinctly dosage related but rather reach a ceiling effect beyond
which further dosage increases result
in relatively lesser effects.
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