fisetin

Action and Spectrum

Actions and Spectrum:

It inhibits production of inflammatory cytokines and enzymes and thus reduces inflammation within the body. It exerts it effects on several signaling pathways such as PI3K/Akt, MAPK/ERK, and NF-κB which are involved in controlling many cell functions including growth, proliferation, differentiation and apoptosis.

Drug Interaction

Adverse Reaction

Adverse Reaction 

Vomiting

Diarrhea

Nausea

Black Box Warning

Black box warning:

None

Contraindication / Caution

Contraindications/caution:

Hepatic impairment

Pregnancy / Lactation

Pregnancy warnings:

Pregnancy Category: Insufficient data available

Lactation:

Excretion of the drug in human breast milk is unknown

Pregnancy Categories: 

• Category A: Satisfactory and well-controlled studies show no evidence of risk to the fetus in the 1^st trimester or in the 3^rd trimester.
• Category B: No evidence of risk to fetus found in animal reproduction studies and there are not enough studies on pregnant women.
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women.
• Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits.
• Category X: Drugs listed in this category clearly outweigh risks over benefits. These category drugs should be prohibited for pregnant women.
• Category N: There is no data available for the drug under this category.

Pharmacology

Pharmacology:

Fisetin is a flavonoid that is derived from fruits and vegetables and has a number of positive impacts on the body. It helps in protecting the cells from damage by free radicals through oxidative stress and also has anti-inflammatory properties. It also suppresses the secretion of pro-inflammatory cytokines as well as other enzymes involved in the inflammation process thus helps in handling inflammation related illnesses. The impact of fisetin on signaling networks involving PI3K/Akt, MAPK/ERK, and NF-κB proteins that controls cell growth, proliferation, differentiation and apoptosis has indicated. Thus, fisetin has been noted to possess neuroprotective properties and because neurons are vulnerable to oxidative stress and inflammation it may be of interest in neurodegenerative diseases. Further, it has been researched that it might affect cancer cells directly through pathways such as apoptosis and cancer cell division suppression.

Pharmacodynamics:

It works through the inhibition of BCL-2 related proteins, BCL-xL, HIF-α as well as the other molecules of the SCAP group.

Pharmacokinetics:

Absorption
The pharmacokinetics of fisetin shows that it is rapidly absorbed as seen in the biodistribution and time-concentration profile curves. In intraperitoneal, fisetin yield a peak plasma concentration of 2. 53 µg/mL at 15 min, after administering the dose of 223 mg/kg [28].

Distribution
After absorption, fisetin circulates in the body and gets incorporated in the target tissues and organs. This has been found in the plasma, brain, liver, kidney, and other tissues thus suggesting good tissue distribution.

Metabolism
Fisetin appears to be metabolized mainly through phase II reactions in the liver. One of these metabolic processes includes taking the substances through conjugation to form sulfates and glucuronides that are easy to be metabolized and expelled through urine.

Elimination/Excretion
The main metabolites of fisetin are the sulfate and glucuronide conjugates of the parent compound which are usually eliminated through the urine and the feces. Therefore, it may be expected that the rate constant and half-life of elimination in human are relatively high due to rapidly metabolism and excretion of the substance.

Adminstartion

Administration:

The route of administration is oral

Patient Information Leaflet

Patient information leaflet

Generic Name: fisetin

Why do we use fisetin?

Fisetin is an antioxidant that helps to prevent oxidative stress and oxidative injury to cells and maintain the well- being of the cells. They suppress pro-inflammatory cytokines and enzymes radically and may help to control the inflammatory processes. It protects neurons from oxidative stress and inflammation that are associated with conditions like Alzheimer’s disease and aids in mental health and cognitive abilities. They have been considered in numerous investigations concerning neurodegenerative disorders such as Alzheimer’s and Parkinson’s diseases.