STALEVO 150

Clinical safety rating: caution

Comprehensive clinical and safety monograph for STALEVO 150 (STALEVO 150).

How it works

Stalevo 150 is a combination of carbidopa, levodopa, and entacapone. Levodopa is converted to dopamine in the brain, replenishing striatal dopamine levels. Carbidopa inhibits peripheral decarboxylation of levodopa, increasing its bioavailability. Entacapone is a selective and reversible inhibitor of catechol-O-methyltransferase (COMT), reducing peripheral metabolism of levodopa to 3-O-methyldopa.

What the body does with it

Metabolism	Levodopa is metabolized by aromatic L-amino acid decarboxylase (AADC) and COMT. Carbidopa inhibits AADC peripherally. Entacapone inhibits COMT primarily in the periphery. Levodopa metabolites are excreted in urine; entacapone is metabolized via glucuronidation (UGT1A9 and UGT2B7) and to a minor extent by CYP450.
Excretion	Carbidopa and levodopa are primarily excreted renally. Levodopa: ~70-80% renal, with metabolites including 3-O-methyldopa. Carbidopa: ~50-70% renal, with ~30% fecal. Entacapone: ~90% fecal (mainly as metabolites), ~10% renal.
Half-life	Levodopa (with carbidopa): ~1.5-2 hours. Carbidopa: ~1-2 hours. Entacapone: ~0.4-0.7 hours (short half-life; not primary determinant of dosing interval). Clinically, levodopa half-life determines dosing frequency for motor fluctuations.
Protein binding	Levodopa: ~30% bound (mainly to albumin). Carbidopa: ~36% bound. Entacapone: ~98% bound (albumin).
Volume of Distribution	Levodopa: ~0.9-1.6 L/kg. Carbidopa: ~0.5 L/kg. Entacapone: ~0.3 L/kg. Large Vd indicates extensive tissue distribution, including CNS.
Bioavailability	Oral: Levodopa bioavailability ~30-40% with carbidopa (vs 10% without); carbidopa ~50-60%; entacapone ~30-35% (high first-pass metabolism).
Onset of Action	Oral: Levodopa effect begins within 30 minutes; peak effect at 1-2 hours.
Duration of Action	Oral: 3-5 hours for levodopa motor response; entacapone prolongs levodopa duration by ~20-30%.

Classification & Brands

Dosing & administration

One tablet orally three times daily. Each tablet contains 150 mg levodopa, 37.5 mg carbidopa, and 200 mg entacapone.

Dosage form	TABLET
Renal impairment	Contraindicated in severe renal impairment (eGFR <30 mL/min/1.73 m²). No adjustment required for mild to moderate impairment (eGFR 30-89 mL/min/1.73 m²).
Liver impairment	Contraindicated in severe hepatic impairment (Child-Pugh class C). No data for mild to moderate impairment; use with caution.
Pediatric use	Not indicated for pediatric patients. Safety and efficacy not established.
Geriatric use	Initiate at lower doses (e.g., one tablet twice daily) with careful titration due to increased risk of adverse effects (dyskinesia, hallucinations, hypotension).

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for STALEVO 150 (STALEVO 150).

Breastfeeding	Excreted in human milk. M/P ratio not established. Avoid breastfeeding due to potential for adverse effects in the infant, including bradycardia and hypotension.
Teratogenic Risk	Pregnancy Category C. First trimester: No adequate studies in humans; animal studies show fetal abnormalities at high doses. Second and third trimesters: Potential for fetal bradycardia and reduced placental perfusion due to carbidopa/levodopa; risk of congenital malformations not well established.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

None explicitly required per FDA labeling. However, levodopa/carbidopa may cause sudden onset of sleep during daily activities, including driving, without warning signs.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Concomitant use with nonselective monoamine oxidase (MAO) inhibitors (MAOIs) (e.g., phenelzine, tranylcypromine)","History of hypersensitivity to any component of the formulation (carbidopa, levodopa, entacapone)","Narrow-angle glaucoma","Suspicious undiagnosed skin lesions or history of melanoma (because levodopa may activate malignant melanoma)"]

Clinical Precautions

Precautions

["May cause falling asleep during activities of daily living, including driving","May cause or exacerbate dyskinesias","May cause hypotension, especially orthostatic","May cause hallucinations and psychotic-like behavior","May cause impulse control disorders (e.g., compulsive gambling, hypersexuality)","May cause hyperpyrexia and confusion in patients withdrawing from levodopa","Entacapone may cause diarrhea, often severe, and may cause brownish-orange discoloration of urine","Not recommended for patients with G6PD deficiency due to risk of hemolytic anemia","Avoid abrupt discontinuation; taper gradually"]

Clinical Tips & Counseling

Drug interactions

Loading safety data…

STALEVO 150

Clinical safety rating: caution

Comprehensive clinical and safety monograph for STALEVO 150 (STALEVO 150).

How it works

What the body does with it

Metabolism	Levodopa is metabolized by aromatic L-amino acid decarboxylase (AADC) and COMT. Carbidopa inhibits AADC peripherally. Entacapone inhibits COMT primarily in the periphery. Levodopa metabolites are excreted in urine; entacapone is metabolized via glucuronidation (UGT1A9 and UGT2B7) and to a minor extent by CYP450.
Excretion	Carbidopa and levodopa are primarily excreted renally. Levodopa: ~70-80% renal, with metabolites including 3-O-methyldopa. Carbidopa: ~50-70% renal, with ~30% fecal. Entacapone: ~90% fecal (mainly as metabolites), ~10% renal.
Half-life	Levodopa (with carbidopa): ~1.5-2 hours. Carbidopa: ~1-2 hours. Entacapone: ~0.4-0.7 hours (short half-life; not primary determinant of dosing interval). Clinically, levodopa half-life determines dosing frequency for motor fluctuations.
Protein binding	Levodopa: ~30% bound (mainly to albumin). Carbidopa: ~36% bound. Entacapone: ~98% bound (albumin).
Volume of Distribution	Levodopa: ~0.9-1.6 L/kg. Carbidopa: ~0.5 L/kg. Entacapone: ~0.3 L/kg. Large Vd indicates extensive tissue distribution, including CNS.
Bioavailability	Oral: Levodopa bioavailability ~30-40% with carbidopa (vs 10% without); carbidopa ~50-60%; entacapone ~30-35% (high first-pass metabolism).
Onset of Action	Oral: Levodopa effect begins within 30 minutes; peak effect at 1-2 hours.
Duration of Action	Oral: 3-5 hours for levodopa motor response; entacapone prolongs levodopa duration by ~20-30%.

Classification & Brands

Dosing & administration

One tablet orally three times daily. Each tablet contains 150 mg levodopa, 37.5 mg carbidopa, and 200 mg entacapone.

Dosage form	TABLET
Renal impairment	Contraindicated in severe renal impairment (eGFR <30 mL/min/1.73 m²). No adjustment required for mild to moderate impairment (eGFR 30-89 mL/min/1.73 m²).
Liver impairment	Contraindicated in severe hepatic impairment (Child-Pugh class C). No data for mild to moderate impairment; use with caution.
Pediatric use	Not indicated for pediatric patients. Safety and efficacy not established.
Geriatric use	Initiate at lower doses (e.g., one tablet twice daily) with careful titration due to increased risk of adverse effects (dyskinesia, hallucinations, hypotension).

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for STALEVO 150 (STALEVO 150).

Breastfeeding	Excreted in human milk. M/P ratio not established. Avoid breastfeeding due to potential for adverse effects in the infant, including bradycardia and hypotension.
Teratogenic Risk	Pregnancy Category C. First trimester: No adequate studies in humans; animal studies show fetal abnormalities at high doses. Second and third trimesters: Potential for fetal bradycardia and reduced placental perfusion due to carbidopa/levodopa; risk of congenital malformations not well established.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

None explicitly required per FDA labeling. However, levodopa/carbidopa may cause sudden onset of sleep during daily activities, including driving, without warning signs.