Inxight Drugs

Showing 1 - 10 of 11 results

Status:

US Approved Rx (1997)

First approved in 1978

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

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...

NALOXONE

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36B82AMQ7N

Status:

US Approved Rx (2022)

First approved in 1971

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Naloxone, sold under the brand name Narcan among others, is a medication used to block the effects of opioids, especially in overdose. Naloxone has an extremely high affinity for μ-opioid receptors in the central nervous system (CNS). Naloxone is a μ...

-opioid receptor (MOR) inverse agonist, and its rapid blockade of those receptors often produces rapid onset of withdrawal symptoms. Naloxone also has an antagonist action, though with a lower affinity, at κ- (KOR) and δ-opioid receptors (DOR). If administered in the absence of concomitant opioid use, no functional pharmacological activity occurs (except the inability for the body to combat pain naturally). In contrast to direct opiate agonists, which elicit opiate withdrawal symptoms when discontinued in opiate-tolerant people, no evidence indicates the development of tolerance or dependence on naloxone. The mechanism of action is not completely understood, but studies suggest it functions to produce withdrawal symptoms by competing for opiate receptor sites within the CNS (a competitive antagonist, not a direct agonist), thereby preventing the action of both endogenous and xenobiotic opiates on these receptors without directly producing any effects itself. When administered parenterally (e.g. intravenously or by injection), as is most common, naloxone has a rapid distribution throughout the body. The mean serum half-life has been shown to range from 30 to 81 minutes, shorter than the average half-life of some opiates, necessitating repeat dosing if opioid receptors must be stopped from triggering for an extended period. Naloxone is primarily metabolized by the liver. Its major metabolite is naloxone-3-glucuronide, which is excreted in the urine. Naloxone is useful both in acute opioid overdose and in reducing respiratory or mental depression due to opioids. Whether it is useful in those in cardiac arrest due to an opioid overdose is unclear. Naloxone is poorly absorbed when taken by mouth, so it is commonly combined with a number of oral opioid preparations, including buprenorphine and pentazocine, so that when taken orally, just the opioid has an effect, but if misused by injecting, the naloxone blocks the effect of the opioid. In a meta-analysis of people with shock, including septic, cardiogenic, hemorrhagic, or spinal shock, those who received naloxone had improved blood flow. Naloxone is also experimentally used in the treatment for congenital insensitivity to pain with anhidrosis, an extremely rare disorder (one in 125 million) that renders one unable to feel pain or differentiate temperatures. Naloxone can also be used as an antidote in overdose of clonidine, a medication that lowers blood pressure.

PENTAZOCINE

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RP4A60D26L

Status:

US Approved Rx (1997)

First approved in 1967

Class (Stereo):

CHEMICAL (MIXED)

Targets:

Conditions:

Development Status

Primary Target

Highest Phase

Approval Year

Condition

Treatment Modality

CNS Activity

Originator

Substance Class

Code System

ATC Level 1

ATC Level 2

ATC Level 3

ATC Level 4

Substance Form

BUTORPHANOL

QV897JC36D

NALOXONE

36B82AMQ7N

PENTAZOCINE

RP4A60D26L

BUTORPHANOL TARTRATE

2L7I72RUHN

DINALOXONE PAMOATE

P7WJA2YB2Y

NALOXONE PAMOATE

Q33JU1X13B

NALOXONE HYDROCHLORIDE

F850569PQR

NALOXONE HYDROCHLORIDE DIHYDRATE

5Q187997EE

PENTAZOCINE HYDROCHLORIDE

A36BXO4PPX

PENTAZOCINE LACTATE

1P2XIB510O