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US Approved Rx

2

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Primary Target

Delta opioid receptor

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Kappa opioid receptor

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Mu opioid receptor

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Highest Phase

Approved

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Approval Year

1978

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Pain

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Palliative

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CNS Activity

CNS Active

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Originator

Monkovic, I.

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Chemical

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CAS

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ChEMBL

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DEA NO.

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OPIOIDS

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ATC Level 4

Morphinan derivatives

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Salts, Hydrates, Esters, etc.

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BUTORPHANOL

QV897JC36D

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Status:

US Approved Rx (1997)

First approved in 1978

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Kappa opioid receptor

Mu opioid receptor

Delta opioid receptor

Conditions:

Butorphanol is a synthetic opioid agonist-antagonist analgesic with a pharmacological and therapeutic profile that has been well established since its launch as a parenteral formulation in 1978. The introduction of a transnasal formulation of butorph...

anol represents a new and noninvasive presentation of an analgesic for moderate to severe pain. This route of administration bypasses the gastrointestinal tract, and this is an advantage for a drug such as butorphanol that undergoes significant first-pass metabolism after oral administration. The onset of action and systemic bioavailability of butorphanol following transnasal delivery are similar to those after parenteral administration. Butorphanol blocks pain impulses at specific sites in the brain and spinal cord. Butorphanol has agonistic activity at the κ-receptor and antagonistic activity at the μ-receptor. It also exhibits partial agonistic activity at the σ-receptor.

BUTORPHANOL TARTRATE

2L7I72RUHN

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Status:

US Approved Rx (1997)

First approved in 1978

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Kappa opioid receptor

Mu opioid receptor

Delta opioid receptor

Conditions:

Butorphanol is a synthetic opioid agonist-antagonist analgesic with a pharmacological and therapeutic profile that has been well established since its launch as a parenteral formulation in 1978. The introduction of a transnasal formulation of butorph...

anol represents a new and noninvasive presentation of an analgesic for moderate to severe pain. This route of administration bypasses the gastrointestinal tract, and this is an advantage for a drug such as butorphanol that undergoes significant first-pass metabolism after oral administration. The onset of action and systemic bioavailability of butorphanol following transnasal delivery are similar to those after parenteral administration. Butorphanol blocks pain impulses at specific sites in the brain and spinal cord. Butorphanol has agonistic activity at the κ-receptor and antagonistic activity at the μ-receptor. It also exhibits partial agonistic activity at the σ-receptor.

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