U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Status:
First marketed in 1827

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Morphine is one of the most important and widely used opioid for the treatment of chronic and acute pain: the very wide interindividual variability in the patients’ response to the drug may have genetic derivations. Sulphate salt of morphine sold under the many brand names, one of them, DURAMORPH, which is indicated for the management of pain severe enough to require use of an opioid analgesic by intravenous administration, and for which alternative treatments are not expected to be adequate. In addition for the epidural or intrathecal management of pain without attendant loss of motor, sensory, or sympathetic function. Morphine is a full opioid agonist and is relatively selective for the mu-opioid receptor, although it can bind to other opioid receptors at higher doses. The principal therapeutic action of morphine is analgesia. Like all full opioid agonists, there is no ceiling effect for analgesia with morphine. The precise mechanism of the analgesic action is unknown. However, specific CNS opioid receptors for endogenous compounds with opioid-like activity have been identified throughout the brain and spinal cord and are thought to play a role in the analgesic effects of this drug. Morphine has a high potential for addiction and abuse. Common side effects include drowsiness, vomiting, and constipation. Caution is advised when used during pregnancy or breast-feeding, as morphine will affect the baby.
Status:
Investigational
Source:
INN:oxilorphan
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Oxilorphan (also known as levo-BC-2605) was developed as a long-acting, narcotic antagonist that has agonist properties. Oxilorphan is a partial agonist at the kappa-opioid receptor and antagonist of the mu-opioid receptor. During clinical trials, oxilorphan had led to dysphoria, which combined with its hallucinogenic effects, serves to limit its clinical usefulness. As a result, many patients who experienced these side effects refused to take additional doses in clinical trials.
Status:
Investigational
Source:
INN:oxilorphan
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Oxilorphan (also known as levo-BC-2605) was developed as a long-acting, narcotic antagonist that has agonist properties. Oxilorphan is a partial agonist at the kappa-opioid receptor and antagonist of the mu-opioid receptor. During clinical trials, oxilorphan had led to dysphoria, which combined with its hallucinogenic effects, serves to limit its clinical usefulness. As a result, many patients who experienced these side effects refused to take additional doses in clinical trials.
Levallorphan (brand name Lorfan), is an opiate antagonist of morphine family. Levallorphan was formerly used in general anesthesia, mainly to reverse the respiratory depression produced by opioid analgesics and barbiturates used for induction of surgical anaesthesia whilst maintaining a degree of analgesia. Levallorphan was also used in combination with opioid analgesics to reduce their side effects, mainly in obstetrics. The combination of levallorphan with pethidine was used so frequently, a standardized formulation was made available, known as Pethilorfan, by Roche Products Ltd in later 1950s. Is known to be used for narcotic overdose. Levallorphan is similar to naloxone but differs from naloxone in that it also possesses some agonist properties. It acts as an antagonist and partial agonist of the mu opioid receptor (MOR). Levallorphan can produce severe mental reactions at sufficient doses including hallucinations, dissociation, and other psychotomimetic effects, dysphoria, anxiety, confusion, dizziness, disorientation, derealization, feelings of drunkenness, and bizarre, unusual, or disturbing dreams.