Niftholide

Niftholide - General Information

An antiandrogen with about the same potency as cyproterone in rodent and canine species.

Pharmacology of Niftholide

Niftholide 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.

Niftholide for patients

Patients should be informed that EULEXIN Capsules and the drug used for medical castration should be administered concomitantly, and that they should not interrupt their dosing or stop taking these medications without consulting their physician.

Niftholide Interactions

Increases in prothrombin time have been noted in patients receiving long- term warfarin therapy after flutamide was initiated. Therefore, close monitoring of prothrombin time is recommended and adjustment of the anticoagulant dose may be necessary when EULEXIN Capsules are administered concomitantly with warfarin.

Niftholide Contraindications

EULEXIN Capsules are contraindicated in patients who are hypersensitive to flutamide or any component of this preparation.

EULEXIN Capsules are contraindicated in patients with severe hepatic impairment (baseline hepatic enzymes should be evaluated prior to treatment.

Additional information about Niftholide

Niftholide Indication: For the management of locally confined Stage B2-C and Stage D2 metastatic carcinoma of the prostate
Mechanism Of Action: Niftholide is a nonsteroidal antiandrogen that blocks the action of both endogenous and exogenous testosterone by binding to the androgen receptor. In addition Niftholide is a potent inhibitor of testosterone-stimulated prostatic DNA synthesis. Moreover, it is capable of inhibiting prostatic nuclear uptake of androgen.
Drug Interactions: Anisindione Niftholide increases the anticoagulant effect
Dicumarol Niftholide increases the anticoagulant effect
Acenocoumarol Niftholide increases the anticoagulant effect
Warfarin Niftholide increases the anticoagulant effect
Food Interactions: Take without regard to meals.
Generic Name: Flutamide
Synonyms: FTA; Flutamide USP25
Drug Category: Androgen Antagonists; Antineoplastic Agents, Hormonal
Drug Type: Small Molecule; Approved

Other Brand Names containing Flutamide: Cebatrol; Eulexin; Niftholide; Niftolide;
Absorption: Rapidly and completely absorbed.
Toxicity (Overdose): In animal studies with flutamide alone, signs of overdose included hypoactivity, piloerection, slow respiration, ataxia, and/or lacrimation, anorexia, tranquilization, emesis, and methemoglobinemia.
Protein Binding: 94-96%
Biotransformation: Flutamide is rapidly and extensively metabolized, with flutamide comprising only 2.5% of plasma radioactivity 1 hour after administration.
Half Life: The plasma half-life for the alpha-hydroxylated metabolite of flutamide (an active metabolite) is approximately 6 hours.
Dosage Forms of Niftholide: Tablet Oral
Chemical IUPAC Name: 2-methyl-N-[4-nitro-3-(trifluoromethyl)phenyl]propanamide
Chemical Formula: C11H11F3N2O3
Flutamide on Wikipedia: https://en.wikipedia.org/wiki/Flutamide
Organisms Affected: Humans and other mammals