Zotarolimus: Difference between revisions

From WikiMD's Wellness Encyclopedia

CSV import
 
CSV import
 
Line 1: Line 1:
'''Zotarolimus''' is a semi-synthetic derivative of [[rapamycin]]. It was developed by [[Abbott Laboratories]] and is used primarily in drug-eluting stents to prevent restenosis, a complication that can occur after [[angioplasty]] procedures. Zotarolimus works by inhibiting the proliferation of smooth muscle cells in the arterial wall, a key factor in the development of restenosis.
== Zotarolimus ==


== History ==
[[File:Zotarolimus.svg|thumb|right|Chemical structure of Zotarolimus]]


Zotarolimus was developed by [[Abbott Laboratories]] in the early 2000s as a new type of drug for use in [[drug-eluting stents]]. The drug was designed to be more lipophilic than its parent compound, [[rapamycin]], in order to improve its distribution within the arterial wall.
'''Zotarolimus''' is a [[macrolide]] [[immunosuppressant]] drug that is primarily used in [[drug-eluting stents]] to prevent [[coronary artery disease|coronary artery]] restenosis. It is a derivative of [[sirolimus]], also known as rapamycin, and functions by inhibiting the [[mammalian target of rapamycin]] (mTOR), a key regulatory kinase involved in cell proliferation.


== Pharmacology ==
== Mechanism of Action ==


Zotarolimus is a semi-synthetic derivative of [[rapamycin]], a naturally occurring compound produced by the bacterium ''[[Streptomyces hygroscopicus]]''. Like rapamycin, zotarolimus works by binding to the protein [[FKBP12]], which then inhibits the [[mTOR]] pathway. This inhibition prevents the proliferation of smooth muscle cells in the arterial wall, a key factor in the development of restenosis.
Zotarolimus works by binding to the intracellular protein [[FKBP12]] (FK506-binding protein 12). This complex then inhibits the mTOR pathway, which is crucial for cell cycle progression. By blocking mTOR, zotarolimus effectively reduces the proliferation of [[smooth muscle cells]] in the arterial wall, thereby preventing restenosis.


== Clinical use ==
== Clinical Use ==


Zotarolimus is used primarily in [[drug-eluting stents]], which are used in [[angioplasty]] procedures to treat [[coronary artery disease]]. The drug is released slowly from the stent over time, helping to prevent the development of restenosis.
Zotarolimus is primarily used in [[drug-eluting stents]] (DES), which are implanted in patients with [[coronary artery disease]] to keep the arteries open. The drug is released slowly from the stent to prevent the growth of scar tissue and restenosis, which is the re-narrowing of the artery.


== Side effects ==
== Pharmacokinetics ==


As with any drug, zotarolimus can have side effects. These can include [[hypotension]], [[bradycardia]], and [[peripheral edema]]. However, these side effects are generally rare and the drug is considered to be well-tolerated.
Zotarolimus is designed to be released locally from the stent over a period of time, allowing for targeted action at the site of the stent placement. This local delivery minimizes systemic exposure and reduces the risk of systemic side effects.


== See also ==
== Side Effects ==


* [[Rapamycin]]
As with other mTOR inhibitors, potential side effects of zotarolimus include [[immunosuppression]], which can increase the risk of infections. Other side effects may include delayed wound healing and [[thrombocytopenia]].
 
== Related Pages ==
 
* [[Sirolimus]]
* [[Drug-eluting stent]]
* [[Drug-eluting stent]]
* [[Restenosis]]
* [[Coronary artery disease]]
* [[Angioplasty]]
* [[Mammalian target of rapamycin]]


[[Category:Drugs]]
[[Category:Immunosuppressants]]
[[Category:Macrolides]]
[[Category:Pharmacology]]
[[Category:Pharmacology]]
[[Category:Cardiology]]
{{stub}}

Latest revision as of 04:00, 13 February 2025

Zotarolimus[edit]

Chemical structure of Zotarolimus

Zotarolimus is a macrolide immunosuppressant drug that is primarily used in drug-eluting stents to prevent coronary artery restenosis. It is a derivative of sirolimus, also known as rapamycin, and functions by inhibiting the mammalian target of rapamycin (mTOR), a key regulatory kinase involved in cell proliferation.

Mechanism of Action[edit]

Zotarolimus works by binding to the intracellular protein FKBP12 (FK506-binding protein 12). This complex then inhibits the mTOR pathway, which is crucial for cell cycle progression. By blocking mTOR, zotarolimus effectively reduces the proliferation of smooth muscle cells in the arterial wall, thereby preventing restenosis.

Clinical Use[edit]

Zotarolimus is primarily used in drug-eluting stents (DES), which are implanted in patients with coronary artery disease to keep the arteries open. The drug is released slowly from the stent to prevent the growth of scar tissue and restenosis, which is the re-narrowing of the artery.

Pharmacokinetics[edit]

Zotarolimus is designed to be released locally from the stent over a period of time, allowing for targeted action at the site of the stent placement. This local delivery minimizes systemic exposure and reduces the risk of systemic side effects.

Side Effects[edit]

As with other mTOR inhibitors, potential side effects of zotarolimus include immunosuppression, which can increase the risk of infections. Other side effects may include delayed wound healing and thrombocytopenia.

Related Pages[edit]