Nourianz

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

Nourianz, or KW6002, was developed by Kyowa Hakko Kirin in Japan for the treatment of Parkinson's disease as an adjunct to standard therapy. Unlike standard dopaminergic therapies for Parkinson's, Nourianz targets adenosine A2A receptors in the basal ganglia. This region of the brain is highly involved in motor control.

Nourianz is indicated as an adjunct treatment to levodopa and carbidopa for Parkinson's disease.

This drug was first approved in Japan on 25 March 2013. Nourianz was granted FDA approval on 27 August 2019.

Nourianz
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	Nourianz
Availability	Prescription only
Generic	Istradefylline
Istradefylline Other Names	Istradefylline
Related Drugs	Gocovri, Rytary, Sinemet, Sinemet CR, ropinirole, pramipexole, benztropine, carbidopa / levodopa, Exelon
Weight	20mg, 40mg,
Type	Oral tablet
Formula	C₂₀H₂₄N₄O₄
Weight	Average: 384.436 Monoisotopic: 384.179755269
Protein binding	Istradefylline is approximately 98% protein bound in plasma, mostly to serum albumin and alpha-1-acid glycoprotein.
Groups	Approved, Investigational
Therapeutic Class
Manufacturer
Available Country	United States,
Last Updated:	September 19, 2023 at 7:00 am

Uses

Nourianz is a selective adenoside A2A receptor antagonist indicated in adjunct to levodopa and carbidopa for the treatment of Parkinson's Disease.

Nourianz is indicated in adjunct to levodopa and carbidopa in the treatment of Parkinson's disease.

Nourianz is also used to associated treatment for these conditions: Parkinson's Disease (PD)

How Nourianz works

Nourianz is a selective adenosine A_2A receptor inhibitor. These receptors are found in the basal ganglia, a region of the brain that suffers degeneration in Parkinson's disease, and is also significantly involved in motor control. A_2A receptors are also expressed on GABAergic medium spiny neurons within the indirect striato-pallidal pathway. The GABAergic action of this pathway is thereby reduced. Nourianz has 56 times the affinity for A_2A receptors than A₁ receptors.

Toxicity

The oral LD₅₀ in mice is >300mg/kg.

Patients experiencing an overdose may present with hallucinations, agitation, and dyskinesia. Treat patients by discontinuing istradefylline and administering supportive treatment.

Food Interaction

Avoid St. John's Wort. St. John's Wort decreases istradefylline concentrations.
Take at the same time every day.
Take with or without food.

[Moderate] ADJUST DOSE: Smoking tobacco may decrease the steady-state systemic exposure of istradefylline by 38% to 54%.

MANAGEMENT: The possibility of reduced therapeutic effects of istradefylline should be considered in smokers.

The manufacturer recommends an istradefylline dosage of 40 mg once daily in patients who smoke 20 or more cigarettes (or the equivalent amount of another tobacco product) per day.

Nourianz Disease Interaction

Major: severe hepatic impairmentModerate: end stage renal disease, psychotic disorders, smoking

Volume of Distribution

The apparent volume of distribution of istradefylline is 448-557L.

Elimination Route

Nourianz reaches a C_max of 181.1ng/mL with a T_max of 2.0h and an AUC of 11,100ng*h/mL. M1, the primary active metabolite, reaches a C_max of 4.34ng/mL with a T_max of 3.5h. The M8 metabolite reaches a C_max of 12.6ng/mL with a T_max of 3.0h and an AUC of 610ng*h/mL.

Half Life

The terminal elimination half life of istradefylline was 64-69 hours.

Clearance

The apparent clearance of istradefylline is 4.1-6.0L/h.

Elimination Route

A 3mg/kg oral dose given to male rats was 17.6% elminated in the urine and 68.3% eliminated in the feces. In urine, 5.31% of the total dose was the M3 metabolite and 1.96% of the total dose was the M1 metabolite. In feces, 30.60% of the total dose was the M3 metabolite, 9.34% of the total dose was the M1 metabolite, 8.33% of the total dose was the M10 metabolite, and 1.62% of the total dose was unchanged istradefylline.