Istradefylline (Nourianz) acts as an adenosine receptor inhibitor.

It is used for Parkinson's disease patients who experience the "off" effects.

Istradefylline (Nourianz) Uses:

• Parkinson disease, "off" episode:

  • In the liver, a substance called norketamine changes into other substances.
  • One of these changes is removing a part called N-dealkylation.
  • Then, another change happens where a part called the cyclohexone ring gets a hydroxyl group added to it, creating two new substances called metabolites III and IV.
  • These substances then combine with glucuronic acid.
  • After that, they lose water and become a different substance called a cyclohexene derivative, which is called metabolite II.

Istradefylline (Nourianz) Dose in Adults:

Istradefylline (Nourianz) Dose in the treatment of Parkinson disease, "off" episode:

• You take 20 milligrams by mouth once every day.
• If your body handles it well and it works for you, the doctor might increase it up to 40 milligrams once a day.

• Dosage adjustment for concomitant CYP3A4 inhibitors/inducers and tobacco smoking:

  • If you're taking strong CYP3A4 inducers with this medication, it's best to avoid using it altogether.

  • For strong CYP3A4 inhibitors, the usual dose is 20 milligrams once a day.

  • Don't take more than this in a day.

  • However, if you smoke a lot, like 20 or more cigarettes per day, the doctor might prescribe 40 milligrams once a day.

Use in Children:

Not indicated.

Pregnancy Risk Category: N (Not assigned)

• Research on animals has found that if they're exposed to this drug while still in the womb, it can harm the developing babies.

• So, it's crucial for women getting treated with this medication to make sure they're using reliable birth control methods to avoid getting pregnant.

Use while breastfeeding

• We're not sure if this drug can pass into breast milk.

• The company recommends weighing the benefits and risks of taking the medication for pregnant women, considering any potential harm it might cause to the baby through breast milk.

Istradefylline (Nourianz) Dose in Kidney Disease:

• If your kidney function, measured by CrCl, is 15 milliliters per minute or higher, you don't need to change the dose of the medication.
• However, if your CrCl is less than 15 milliliters per minute, there isn't enough information about how the medication affects people with this level of kidney function.
• For those with end-stage kidney disease who need hemodialysis, there haven't been studies done on how this medication affects them, so it's not recommended for use in these patients.

Istradefylline (Nourianz) Dose in Liver disease:

• If you have mild liver problems, known as Child-Pugh class A, you don't need to change the dose of the medication.
• But if your liver impairment is moderate, known as Child-Pugh class B, the usual dose is 20 milligrams once a day, and you shouldn't take more than this in a day.
• However, if your liver problems are severe, known as Child-Pugh class C, it's best to avoid using this medication altogether.
• There haven't been studies done on how this medication affects people with severe liver problems.

Side Effects of Istradefylline (Nourianz):

• Neuromuscular & skeletal:

  • Dyskinesia

Less Common Side Effects of Istradefylline (Nourianz):

• Central Nervous System:

  • Insomnia
  • Dizziness
  • Auditory Hallucination
  • Hallucination
  • Visual Hallucination
  • Abnormal Behavior
  • Abnormality In Thinking
  • Aggressive Behavior
  • Agitation
  • Confusion
  • Delirium
  • Delusion
  • Disorientation
  • Mania
  • Paranoid Ideation

• Dermatologic:

  • Skin Rash

• Endocrine & Metabolic:

  • Increased Serum Glucose

• Gastrointestinal:

  • Constipation
  • Diarrhea
  • Decreased Appetite
  • Nausea

• Hepatic:

  • Increased Serum Alkaline Phosphatase

• Renal:

  • Increased Blood Urea Nitrogen

• Respiratory:

  • Upper Respiratory Tract Inflammation

Contraindications to Istradefylline (Nourianz):

• According to the manufacturer's instructions, there are no specific situations where the medication should not be used.

• However, it's important to follow the guidance of your healthcare provider regarding whether the medication is suitable for you, especially if you have certain medical conditions or are taking other medications.

Warnings and precautions

• Dyskinesias

  • Patients who already have dyskinesia should avoid using this medication.
  • It can make dyskinesia worse or even cause it in some cases.

• Disorders of impulse control:

  • People who have taken this medication have experienced compulsive behaviors or loss of impulse control.

  • These behaviors might show up as an increase in sexual desire, compulsive shopping, overeating, or excessive gambling.

  • However, these behaviors can often be stopped by either stopping the medication or reducing the dose.

• Psychotic effects

  • Starting or increasing the dose of this treatment might lead to changes in mental and behavioral health or make existing problems worse.
  • These changes could include symptoms like paranoid thoughts, hallucinations, confusion, aggressive behavior, or agitation.
  • It's important to note that if someone has a serious mental disorder like psychosis, they shouldn't use this treatment.

• Hepatic impairment

  • Patients with liver problems should be cautious when using this medication.
  • For those with moderate liver impairment, the highest safe dose is lower.
  • However, if the liver impairment is severe, it's best not to use this medication at all.
  • There hasn't been enough testing done on how this medication affects people with significant liver problems.

Istradefylline: Drug Interaction

Monitoring parameters:

• Mental status and behavioral changes;
• dyskinesias.

How to administer Istradefylline (Nourianz)?

It may be taken orally with or without food.

Mechanism of action of Istradefylline (Nourianz):

This drug works by blocking the adenosine-A receptor, at least in animal studies, although its exact effects in humans are not completely understood.

• Protein Binding: It binds to proteins in the body, about 98% of it does.
• Metabolism: It's mainly broken down by enzymes in the liver, particularly CYP1A1 and CYP3A4, with some help from other enzymes like CYP1A2, 2B6, 2C8, CYP2C9, CYP2C18, and 2D6.
• Half-life Elimination: The time it takes for half of the drug to leave the body is around 83 hours.
• Time to Peak: It reaches its highest concentration in the blood around 3 to 4 hours after being taken.
• Excretion: The drug leaves the body mostly through feces (about 48%) and urine (about 39%).

International Brand Names of Istradefylline:

• Nourianz
• Nouriast

Istradefylline Brand Names in Pakistan:

No Brands Available in Pakistan.