Grisetin

Grisetin Uses, Dosage, Side Effects, Food Interaction and all others data.

Grisetin is a nonsteroidal 'pure' antiandrogen which acts directly on the target tissues either by blocking androgen uptake or by inhibiting cytoplasmic and nuclear binding of androgen.

Grisetin is a nonsteroidal antiandrogen. In animal studies, flutamide demonstrates potent antiandrogenic effects. It exerts its antiandrogenic action by inhibiting androgen uptake and/or by inhibiting nuclear binding of androgen in target tissues or both. Prostatic carcinoma is known to be androgen-sensitive and responds to treatment that counteracts the effect of androgen and/or removes the source of androgen, e.g. castration. Elevations of plasma testosterone and estradiol levels have been noted following flutamide administration.

Grisetin
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Grisetin
Availability	Prescription only
Generic	Flutamide
Flutamide Other Names	Flutamid, Flutamida, Flutamide, Flutamidum, NFBA, Niftolid, Niftolide
Related Drugs	spironolactone, estradiol, Premarin, Aldactone, Xtandi, Casodex, Zytiga, Lynparza, Vaniqa, Eulexin
Type
Formula	C₁₁H₁₁F₃N₂O₃
Weight	Average: 276.2118 Monoisotopic: 276.072176843
Protein binding	94-96%
Groups	Approved, Investigational
Therapeutic Class	Hormonal Chemotherapy
Manufacturer
Available Country	Spain
Last Updated:	September 19, 2023 at 7:00 am

Uses

Grisetin is used for use in combination with LHRH agonists for the management of locally confined Stage B2-C and Stage D2 metastatic carcinoma of the prostate.

Stage B2-C Prostatic Carcinoma: Treatment with Grisetin and the LHRH agonist should start 8 weeks prior to initiating radiation therapy and continue during radiation therapy.

Stage D2 Metastatic Carcinoma: To achieve benefit from treatment, Grisetin should be initiated with the LHRH agonist and continued until progression.

Grisetin is also used to associated treatment for these conditions: Acne Vulgaris, C Prostatic Carcinoma, Idiopathic Hirsutism, Stage B2 Prostatic Carcinoma, Stage D2 Prostatic carcinoma

How Grisetin works

Grisetin is a nonsteroidal antiandrogen that blocks the action of both endogenous and exogenous testosterone by binding to the androgen receptor. In addition Grisetin is a potent inhibitor of testosterone-stimulated prostatic DNA synthesis. Moreover, it is capable of inhibiting prostatic nuclear uptake of androgen.

Dosage

Grisetin dosage

Oral (Adult)-

Palliative treatment of prostatic carcinoma: 250 mg tid preferably at least 3 days before gonadorelin analogue treatment. May be taken with or without food.

Side Effects

Hot flushes, loss of libido, impotence, gynaecomastia, nausea, vomiting, diarrhoea, increased appetite, sleep disturbances, skin reactions, anaemias, headache, dizziness, malaise, anxiety, hypertension, gastric and chest pain, oedema, blurred vision, hepatitis, jaundice, rash, thirst, pruritus, SLE-like syndrome, drowsiness, confusion, depression, nervousness.

Toxicity

In animal studies with flutamide alone, signs of overdose included hypoactivity, piloerection, slow respiration, ataxia, and/or lacrimation, anorexia, tranquilization, emesis, and methemoglobinemia.

Precaution

Perform liver function tests before starting treatment and at regular intervals. Treatment is not recommended in patients whose ALT values exceed twice the upper limit of normal. Regular assessment of prostate specific antigen level may help to monitor disease progression. Advise patient against discontinuing drug on their own. Exercise caution in patients with cardiac disease.

Interaction

Increased prothrombin time in patients on long-term warfarin treatment.

Food Interaction

Take with or without food. The absorption is unaffected by food.

Grisetin Drug Interaction

Major: sotalol, sotalolModerate: lithium, lithiumUnknown: amoxicillin / clavulanate, amoxicillin / clavulanate, duloxetine, duloxetine, heparin, heparin, leuprolide, leuprolide, metoprolol, metoprolol, acetaminophen, acetaminophen, vitamin a topical, vitamin a topical, bioflavonoids, bioflavonoids

Grisetin Disease Interaction

Major: hepatic dysfunctionModerate: hemolysis

Elimination Route

Rapidly and completely absorbed.

Half Life

The plasma half-life for the alpha-hydroxylated metabolite of flutamide (an active metabolite) is approximately 6 hours.

Elimination Route

Grisetin and its metabolites are excreted mainly in the urine with only 4.2% of a single dose excreted in the feces over 72 hours.

Pregnancy & Breastfeeding use

Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).