Nouriast
Nouriast Uses, Dosage, Side Effects, Food Interaction and all others data.
Nouriast, 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, Nouriast targets adenosine A2A receptors in the basal ganglia. This region of the brain is highly involved in motor control.
Nouriast 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. Nouriast was granted FDA approval on 27 August 2019.
| Trade Name | Nouriast |
| Availability | Prescription only |
| Generic | Istradefylline |
| Istradefylline Other Names | Istradefylline |
| Related Drugs | Gocovri, Rytary, Sinemet, Sinemet CR, ropinirole, pramipexole, benztropine, carbidopa / levodopa, Exelon |
| Type | |
| 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 | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Nouriast is a selective adenoside A2A receptor antagonist indicated in adjunct to levodopa and carbidopa for the treatment of Parkinson's Disease.
Nouriast is indicated in adjunct to levodopa and carbidopa in the treatment of Parkinson's disease.
Nouriast is also used to associated treatment for these conditions: Parkinson's Disease (PD)
How Nouriast works
Nouriast is a selective adenosine A2A 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. A2A receptors are also expressed on GABAergic medium spiny neurons within the indirect striato-pallidal pathway. The GABAergic action of this pathway is thereby reduced. Nouriast has 56 times the affinity for A2A 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.
Nouriast 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
Nouriast reaches a Cmax of 181.1ng/mL with a Tmax of 2.0h and an AUC of 11,100ng*h/mL. M1, the primary active metabolite, reaches a Cmax of 4.34ng/mL with a Tmax of 3.5h. The M8 metabolite reaches a Cmax of 12.6ng/mL with a Tmax 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.
Innovators Monograph
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