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Samidorphan (INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name) is an opioid antagonist that in the form of olanzapine/samidorphan (sold as Lybalvi) is used in the treatment of schizophrenia and bipolar disorder. Samidorphan reduces the weight gain associated with olanzapine. Samidorphan is taken by mouth.
Samidorphan was under development as a standalone medication for various indications but has been discontinued. Buprenorphine/samidorphan for the treatment of major depressive disorder was rejected by the US Food and Drug Administration (FDA) due to insufficient evidence of effectiveness, but remains in preregistration as of September 2021. Development of baclofen/samidorphan has also been discontinued.




Development


Samidorphan has been investigated for the treatment of alcoholism and cocaine addiction by its developer, Alkermes, showing similar efficacy to naltrexone, but possibly with reduced side effects.
It has attracted much more attention as part of the combination product (buprenorphine/samidorphan), where samidorphan is combined with the mixed μ-opioid receptor (MOR) weak partial agonist and κ-opioid receptor (KOR) antagonist buprenorphine, as an antidepressant. Buprenorphine has shown antidepressant effects in some human studies, thought to be because of its antagonist effects at the KOR, but has not been further developed for this application because of its MOR agonist effects and consequent abuse potential. By combining buprenorphine with samidorphan to block the MOR agonist effects, the combination acts more like a selective KOR antagonist, and produces only antidepressant effects, without typical MOR effects such as euphoria or substance dependence being evident.
Samidorphan was also studied in combination with olanzapine, (olanzapine/samidorphan), for use in schizophrenia. A Phase III study found that the addition of samidorphan to olanzapine significantly reduced weight gain compared to olanzapine alone, and the combination was approved for the treatment of schizophrenia and bipolar disorder by the FDA in May 2021, under the brand name Lybalvi.




Side effects


Side effects of samidorphan include somnolence and gastrointestinal disturbances among others.




Pharmacology






= Pharmacodynamics

=

Samidorphan acts primarily as an antagonist or very weak partial agonist of the μ-opioid receptor (MOR) and to a lesser extent as a partial agonist of the κ-opioid receptor (KOR) and δ-opioid receptor (DOR). In accordance with this profile, samidorphan has been observed to produce some side effects that are potentially consistent with activation of the KOR such as somnolence, sedation, dizziness, and hallucinations in some patients in clinical trials.




= Pharmacokinetics

=
The elimination half-life of samidorphan is 7 to 9 hours.




Chemistry


Samidorphan has its origins in academia where 8-carboxamidocyclazocine and naltrexone were utilized in its design and synthesis.




References






See also






External links


Buprenorphine/samidorphan (ALKS-5461 - AdisInsight
Olanzapine/samidorphan (ALKS-3831) - AdisInsight

Kata Kunci Pencarian:

• Samidorphan
• Olanzapine/samidorphan
• Buprenorphine/samidorphan
• Buprenorphine
• Atypical antidepressant
• Opioid antagonist
• Black tar heroin
• Μ-opioid receptor
• Buprenorphine/naltrexone
• Laudanum

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Daftar Isi

• Samidorphan - Wikipedia
• A Review of Samidorphan: A Novel Opioid Antagonist - PMC
• Lybalvi: Uses, Dosage, Side Effects, Warnings - Drugs.com
• Samidorphan: Uses, Interactions, Mechanism of Action ...
• Home page for LYBALVI® (olanzapine and samidorphan ...
• Olanzapine and Samidorphan: MedlinePlus Drug Information
• Olanzapine/samidorphan - Wikipedia
• Samidorphan/olanzapine combination therapy for schizophrenia ...
• MEDICATION FACT SHEET Olanzapine/Samidorphan
• Samidorphan | C21H26N2O4 | CID 11667832 - PubChem

Samidorphan - Wikipedia

Samidorphan (INN Tooltip International Nonproprietary Name, USAN Tooltip United States Adopted Name) is an opioid antagonist that in the form of olanzapine/samidorphan (sold as Lybalvi) is used in the treatment of schizophrenia and bipolar disorder.

A Review of Samidorphan: A Novel Opioid Antagonist - PMC

Opioid modulators have been explored as a treatment option for psychiatric disorders, but their use has been limited due to their abuse potential. Samidorphan (SAM), a μ-opioid receptor antagonist, has gained interest due to its favorable pharmacokinetic and …

Lybalvi: Uses, Dosage, Side Effects, Warnings - Drugs.com

Feb 12, 2025 · Lybalvi (olanzapine and samidorphan) is a combination antipsychotic/opioid antagonist prescription medicine that may be used to treat adults with manic or mixed episodes associated with bipolar I disorder (either alone or in combination with valproate or lithium) or adults with schizophrenia.

Samidorphan: Uses, Interactions, Mechanism of Action ...

Oct 20, 2016 · Samidorphan is a novel opioid-system modulator, similar to naltrexone, that functions primarily as a μ-opioid receptor antagonist in vivo and is used primarily in combination with antipsychotics to reduce their metabolic dysfunction-associated adverse effects.

Home page for LYBALVI® (olanzapine and samidorphan ...

LYBALVI is a prescription medicine which contains 2 medicines (olanzapine and samidorphan) used in adults: to treat schizophrenia alone for short-term (acute) or maintenance treatment of manic or mixed episodes that happen with bipolar I disorder

Olanzapine and Samidorphan: MedlinePlus Drug Information

The combination of olanzapine and samidorphan is used to treat the symptoms of schizophrenia (a mental illness that causes disturbed or unusual thinking, loss of interest in life, and strong or inappropriate emotions) in adults.

Olanzapine/samidorphan - Wikipedia

Olanzapine/samidorphan, sold under the brand name Lybalvi, is a fixed-dose combination medication for the treatment of schizophrenia and bipolar I disorder. [1] It contains olanzapine, an atypical antipsychotic, and samidorphan, an opioid antagonist.

Samidorphan/olanzapine combination therapy for schizophrenia ...

The potential of samidorphan in mimicking the efficacy of olanzapine while mitigating olanzapine-induced weight gain makes it a promising regimen for improving symptoms and health outcomes in schizophrenic patients.

MEDICATION FACT SHEET Olanzapine/Samidorphan

Olanzapine/samidorphan is a medication that works in the brain to treat schizophrenia. Olanzapine is also known as a second generation antipsychotic (SGA) or atypical antipsychotic.

Samidorphan | C21H26N2O4 | CID 11667832 - PubChem

Samidorphan is a novel opioid antagonist structurally related to [naltrexone], with a higher affinity for opioid receptors, more potent μ-opioid receptor antagonism, higher oral bioavailability, and a longer half-life, making it an attractive candidate for oral dosing.