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	~~'''~~Nepicastat~~''' is a potent and selective inhibitor of~~ [~~[dopamine beta~~-hydroxylase]], an enzyme that catalyzes the conversion of [[dopamine]] to [[norepinephrine]]. It was developed by [[Roche]] and is currently in clinical trials for the treatment of [[cocaine dependence]] and [[heart failure]].		{{Short description\|An article about the drug Nepicastat}}
			{{Drugbox
			\| verifiedfields = changed
			\| verifiedrevid = 477002123
			\| IUPAC_name = 2-[(2S)-2-hydroxy-2-phenylethyl]hydrazinecarboximidamide
			\| image = Nepicastat_Structure.svg
			\| image_size = 200px
			}}

	~~==Pharmacology==~~		'''Nepicastat''' is a [[pharmacological]] agent that acts as a selective inhibitor of the enzyme [[dopamine beta-hydroxylase]] (DBH). This enzyme is responsible for the conversion of [[dopamine]] to [[norepinephrine]], a key neurotransmitter in the [[sympathetic nervous system]].
	Nepicastat ~~works by inhibiting~~ the enzyme dopamine beta-hydroxylase~~, which~~ is responsible for the conversion of dopamine to norepinephrine~~. This results in a decrease in the levels of norepinephrine~~, a neurotransmitter ~~that plays a key role~~ in the ~~reward pathway of the brain. By reducing the levels of norepinephrine, nepicastat may help to reduce the cravings and withdrawal symptoms associated with cocaine dependence~~.

	==~~Clinical Trials~~==		==Mechanism of Action==
	Nepicastat ~~has been tested in several clinical trials for its potential use in~~ the ~~treatment~~ of ~~cocaine dependence and heart failure. In a phase II trial, nepicastat was found to be safe and well~~-~~tolerated in patients with cocaine dependence. However~~, the ~~results~~ of ~~the trial did not show a significant difference~~ in ~~cocaine use between the nepicastat and placebo groups~~.		Nepicastat inhibits the activity of dopamine beta-hydroxylase, thereby reducing the synthesis of norepinephrine. This reduction in norepinephrine levels can lead to decreased [[sympathetic nervous system]] activity, which may be beneficial in conditions characterized by excessive sympathetic activity.

	~~In a separate trial, nepicastat was tested~~ in ~~patients with heart failure. The results of this trial showed that nepicastat was able to improve cardiac function and reduce~~ the ~~symptoms~~ of ~~heart failure.~~		==Therapeutic Uses==
			Nepicastat has been investigated for its potential use in the treatment of various conditions, including:

	~~==Potential Uses==~~		* [[Congestive heart failure]]
	~~While the results of the clinical trials have been mixed, nepicastat still holds promise for the treatment of cocaine dependence and~~ heart failure~~. Further research is needed to fully understand the potential benefits and risks of this drug.~~		* [[Post-traumatic stress disorder]] (PTSD)
			* [[Hypertension]]

	==~~See Also~~==		By modulating norepinephrine levels, Nepicastat may help alleviate symptoms associated with these conditions.

			==Pharmacokinetics==
			Nepicastat is administered orally and undergoes hepatic metabolism. The pharmacokinetic profile of Nepicastat includes its absorption, distribution, metabolism, and excretion, which are important for determining the appropriate dosing regimen.

			==Side Effects==
			Common side effects of Nepicastat may include:

			* [[Dizziness]]
			* [[Fatigue]]
			* [[Nausea]]

			These side effects are generally mild and may diminish with continued use.

			==Research and Development==
			Research into Nepicastat is ongoing, with studies focusing on its efficacy and safety in various clinical settings. The drug's ability to modulate norepinephrine levels makes it a promising candidate for further investigation.

			==Related pages==
	* [[Dopamine beta-hydroxylase]]		* [[Dopamine beta-hydroxylase]]
	* [[~~Cocaine dependence~~]]		* [[Norepinephrine]]
	* [[~~Heart failure~~]]		* [[Sympathetic nervous system]]

	[[Category:Drugs]]		[[Category:Drugs]]
	[[Category:~~Pharmacology~~]]		[[Category:Enzyme inhibitors]]
	[[Category:~~Clinical trials~~]]		[[Category:Sympatholytics]]
	~~[[Category:Roche]]~~

	~~{{stub}}~~

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2024-02-25T22:27:00Z

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'''Nepicastat''' is a potent and selective inhibitor of [[dopamine beta-hydroxylase]], an enzyme that catalyzes the conversion of [[dopamine]] to [[norepinephrine]]. It was developed by [[Roche]] and is currently in clinical trials for the treatment of [[cocaine dependence]] and [[heart failure]].

==Pharmacology==
Nepicastat works by inhibiting the enzyme dopamine beta-hydroxylase, which is responsible for the conversion of dopamine to norepinephrine. This results in a decrease in the levels of norepinephrine, a neurotransmitter that plays a key role in the reward pathway of the brain. By reducing the levels of norepinephrine, nepicastat may help to reduce the cravings and withdrawal symptoms associated with cocaine dependence.

==Clinical Trials==
Nepicastat has been tested in several clinical trials for its potential use in the treatment of cocaine dependence and heart failure. In a phase II trial, nepicastat was found to be safe and well-tolerated in patients with cocaine dependence. However, the results of the trial did not show a significant difference in cocaine use between the nepicastat and placebo groups.

In a separate trial, nepicastat was tested in patients with heart failure. The results of this trial showed that nepicastat was able to improve cardiac function and reduce the symptoms of heart failure.

==Potential Uses==
While the results of the clinical trials have been mixed, nepicastat still holds promise for the treatment of cocaine dependence and heart failure. Further research is needed to fully understand the potential benefits and risks of this drug.

==See Also==
* [[Dopamine beta-hydroxylase]]
* [[Cocaine dependence]]
* [[Heart failure]]

[[Category:Drugs]]
[[Category:Pharmacology]]
[[Category:Clinical trials]]
[[Category:Roche]]

{{stub}}

Nepicastat - Revision history

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