Tirilazad: Difference between revisions

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'''Tirilazad''' is a [[steroid]]-based [[drug]] that was developed for the treatment of [[stroke]] and [[neurotrauma]]. It functions as an inhibitor of [[lipid peroxidation]], a process that can lead to cell damage in the brain. Despite promising results in animal studies, clinical trials in humans have not shown significant benefits.
{{Short description|An article about the drug Tirilazad}}
{{Drugbox
| verifiedfields = changed
| verifiedrevid = 477002123
| image = Tirilazad.svg
| image_size = 200px
| image_alt = Chemical structure of Tirilazad
}}


== History ==
'''Tirilazad''' is a synthetic steroid derivative that acts as a potent inhibitor of lipid peroxidation. It is primarily investigated for its neuroprotective properties in the treatment of acute neurological injuries such as [[subarachnoid hemorrhage]] and [[spinal cord injury]].


Tirilazad was developed by [[Pharmacia & Upjohn]], a pharmaceutical company based in the United States. The drug was initially designed to treat [[ischemic stroke]], a condition caused by a blockage in the blood vessels supplying the brain. It was also tested for use in neurotrauma, specifically [[spinal cord injury]] and [[traumatic brain injury]].
==Mechanism of Action==
Tirilazad functions by inhibiting the peroxidation of lipids in cell membranes, a process that can lead to cell damage and death. This is particularly important in the context of [[central nervous system]] injuries, where oxidative stress plays a significant role in secondary injury mechanisms. By reducing lipid peroxidation, Tirilazad helps to preserve cellular integrity and function.


== Mechanism of Action ==
==Clinical Applications==
Tirilazad has been studied in various clinical settings, particularly in the management of subarachnoid hemorrhage and spinal cord injury. In these conditions, the drug is thought to mitigate the effects of oxidative stress and inflammation, potentially improving neurological outcomes.


Tirilazad belongs to a class of drugs known as [[21-aminosteroids]]. These drugs are designed to inhibit lipid peroxidation, a chemical process that can lead to cell damage. Lipid peroxidation occurs when free radicals steal electrons from the lipids in cell membranes, resulting in cell damage. By inhibiting this process, Tirilazad was intended to protect brain cells from damage following a stroke or injury.
===Subarachnoid Hemorrhage===
In patients with subarachnoid hemorrhage, Tirilazad has been evaluated for its ability to reduce the incidence of [[vasospasm]], a common and serious complication. While early studies showed promise, subsequent trials have yielded mixed results, and its use in this context remains controversial.


== Clinical Trials ==
===Spinal Cord Injury===
Tirilazad has also been investigated for its potential to improve outcomes following spinal cord injury. The drug's ability to limit oxidative damage and inflammation is thought to contribute to neuroprotection and functional recovery.


Despite promising results in animal studies, clinical trials of Tirilazad in humans have not shown significant benefits. In trials for ischemic stroke, the drug did not improve survival rates or functional outcomes. Similarly, in trials for neurotrauma, Tirilazad did not show a significant benefit in terms of improved neurological function or reduced mortality.
==Pharmacokinetics==
Tirilazad is administered intravenously, and its pharmacokinetic profile is characterized by rapid distribution and metabolism. The drug is metabolized primarily in the liver and excreted in the urine. Its half-life and clearance rates can vary depending on the patient's condition and other factors.


== Current Status ==
==Side Effects==
The use of Tirilazad can be associated with several side effects, including [[gastrointestinal]] disturbances, [[hypotension]], and [[allergic reactions]]. Careful monitoring is required to manage these potential adverse effects.


As of now, Tirilazad is not approved for use in any country. The lack of efficacy in clinical trials has led to its discontinuation. However, research into the potential benefits of 21-aminosteroids and other inhibitors of lipid peroxidation continues.
==Research and Development==
Despite initial enthusiasm, the development of Tirilazad has faced challenges due to inconsistent clinical trial results. Research continues to explore its potential benefits and limitations in various neurological conditions.


== See Also ==
==Related pages==
 
* [[Neuroprotection]]
* [[Stroke]]
* [[Oxidative stress]]
* [[Neurotrauma]]
* [[Lipid peroxidation]]
* [[Lipid peroxidation]]
* [[21-Aminosteroids]]
* [[Subarachnoid hemorrhage]]
* [[Spinal cord injury]]


[[Category:Drugs]]
[[Category:Neuroprotective agents]]
[[Category:Stroke]]
[[Category:Steroids]]
[[Category:Neurotrauma]]
{{medicine-stub}}

Revision as of 03:39, 13 February 2025

An article about the drug Tirilazad


Tirilazad
INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
Excretion
Legal status
CAS Number
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KEGG


Tirilazad is a synthetic steroid derivative that acts as a potent inhibitor of lipid peroxidation. It is primarily investigated for its neuroprotective properties in the treatment of acute neurological injuries such as subarachnoid hemorrhage and spinal cord injury.

Mechanism of Action

Tirilazad functions by inhibiting the peroxidation of lipids in cell membranes, a process that can lead to cell damage and death. This is particularly important in the context of central nervous system injuries, where oxidative stress plays a significant role in secondary injury mechanisms. By reducing lipid peroxidation, Tirilazad helps to preserve cellular integrity and function.

Clinical Applications

Tirilazad has been studied in various clinical settings, particularly in the management of subarachnoid hemorrhage and spinal cord injury. In these conditions, the drug is thought to mitigate the effects of oxidative stress and inflammation, potentially improving neurological outcomes.

Subarachnoid Hemorrhage

In patients with subarachnoid hemorrhage, Tirilazad has been evaluated for its ability to reduce the incidence of vasospasm, a common and serious complication. While early studies showed promise, subsequent trials have yielded mixed results, and its use in this context remains controversial.

Spinal Cord Injury

Tirilazad has also been investigated for its potential to improve outcomes following spinal cord injury. The drug's ability to limit oxidative damage and inflammation is thought to contribute to neuroprotection and functional recovery.

Pharmacokinetics

Tirilazad is administered intravenously, and its pharmacokinetic profile is characterized by rapid distribution and metabolism. The drug is metabolized primarily in the liver and excreted in the urine. Its half-life and clearance rates can vary depending on the patient's condition and other factors.

Side Effects

The use of Tirilazad can be associated with several side effects, including gastrointestinal disturbances, hypotension, and allergic reactions. Careful monitoring is required to manage these potential adverse effects.

Research and Development

Despite initial enthusiasm, the development of Tirilazad has faced challenges due to inconsistent clinical trial results. Research continues to explore its potential benefits and limitations in various neurological conditions.

Related pages