Velneperit: Difference between revisions

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'''Velneperit''' is a [[drug]] candidate that was developed by [[Shionogi]] for the treatment of [[obesity]]. It is a selective [[neuropeptide Y]] receptor antagonist, specifically targeting the Y4 subtype.
{{DISPLAYTITLE:Velneperit}}


== History ==
==Overview==
'''Velneperit''' is a pharmaceutical compound that acts as a [[peripherally acting mu-opioid receptor antagonist]] (PAMORA). It is primarily used in the management of [[opioid-induced constipation]] (OIC), a common side effect of opioid medications. Velneperit works by blocking the action of opioids on the mu-opioid receptors in the gastrointestinal tract without affecting the central nervous system.


Velneperit was first synthesized by Shionogi, a Japanese pharmaceutical company, in the early 2000s. The drug was developed as part of a larger effort to find effective treatments for obesity, a growing global health concern.  
==Mechanism of Action==
Velneperit selectively targets the mu-opioid receptors located in the [[gastrointestinal tract]]. By antagonizing these receptors, it mitigates the constipating effects of opioids, which are often prescribed for [[pain management]]. Unlike other opioid antagonists, Velneperit does not cross the [[blood-brain barrier]], thus preserving the analgesic effects of opioids.


== Mechanism of Action ==
==Clinical Use==
Velneperit is indicated for patients who experience constipation as a result of chronic opioid therapy. It is particularly beneficial for individuals who do not respond adequately to traditional laxatives. The drug is administered orally and is typically well-tolerated.


Velneperit works by blocking the Y4 subtype of the neuropeptide Y receptor. [[Neuropeptide Y]] is a neurotransmitter that is involved in a variety of physiological processes, including appetite regulation. By blocking the Y4 receptor, Velneperit is thought to reduce appetite and promote weight loss.
==Side Effects==
Common side effects of Velneperit include abdominal pain, diarrhea, and flatulence. These effects are generally mild and transient. Serious adverse effects are rare but may include severe gastrointestinal symptoms.


== Clinical Trials ==
==Pharmacokinetics==
Velneperit is absorbed in the gastrointestinal tract and undergoes minimal systemic absorption, which limits its action to the periphery. It is metabolized in the liver and excreted primarily in the feces.


Velneperit has undergone several phases of [[clinical trials]]. In early trials, the drug showed promise in reducing body weight in obese patients. However, later trials revealed potential side effects, including nausea and abdominal discomfort. As of now, the drug has not been approved for use by any major regulatory bodies.
==Development and Approval==
Velneperit was developed as part of a class of drugs aimed at addressing the side effects of opioid therapy. It has been approved for use in several countries and is subject to ongoing research to explore its full potential and safety profile.


== Potential Applications ==
==Related pages==
* [[Opioid-induced constipation]]
* [[Mu-opioid receptor]]
* [[Peripherally acting mu-opioid receptor antagonist]]
* [[Pain management]]


If approved, Velneperit could be used as a treatment for obesity. The drug could also potentially be used in the treatment of other conditions related to appetite regulation, such as [[eating disorders]].
==Gallery==
[[File:Velneperit.svg|thumb|right|Chemical structure of Velneperit]]


== See Also ==
[[Category:Pharmacology]]
 
[[Category:Opioid antagonists]]
* [[Obesity]]
[[Category:Gastroenterology]]
* [[Neuropeptide Y]]
* [[Clinical trials]]
* [[Shionogi]]
 
[[Category:Drugs]]
[[Category:Obesity]]
[[Category:Pharmaceuticals]]
{{Pharma-stub}}

Latest revision as of 03:46, 13 February 2025


Overview[edit]

Velneperit is a pharmaceutical compound that acts as a peripherally acting mu-opioid receptor antagonist (PAMORA). It is primarily used in the management of opioid-induced constipation (OIC), a common side effect of opioid medications. Velneperit works by blocking the action of opioids on the mu-opioid receptors in the gastrointestinal tract without affecting the central nervous system.

Mechanism of Action[edit]

Velneperit selectively targets the mu-opioid receptors located in the gastrointestinal tract. By antagonizing these receptors, it mitigates the constipating effects of opioids, which are often prescribed for pain management. Unlike other opioid antagonists, Velneperit does not cross the blood-brain barrier, thus preserving the analgesic effects of opioids.

Clinical Use[edit]

Velneperit is indicated for patients who experience constipation as a result of chronic opioid therapy. It is particularly beneficial for individuals who do not respond adequately to traditional laxatives. The drug is administered orally and is typically well-tolerated.

Side Effects[edit]

Common side effects of Velneperit include abdominal pain, diarrhea, and flatulence. These effects are generally mild and transient. Serious adverse effects are rare but may include severe gastrointestinal symptoms.

Pharmacokinetics[edit]

Velneperit is absorbed in the gastrointestinal tract and undergoes minimal systemic absorption, which limits its action to the periphery. It is metabolized in the liver and excreted primarily in the feces.

Development and Approval[edit]

Velneperit was developed as part of a class of drugs aimed at addressing the side effects of opioid therapy. It has been approved for use in several countries and is subject to ongoing research to explore its full potential and safety profile.

Related pages[edit]

Gallery[edit]

Chemical structure of Velneperit