PERCHLORACAP

Clinical safety rating: caution

Comprehensive clinical and safety monograph for PERCHLORACAP (PERCHLORACAP).

How it works

PERCHLORACAP is a peroxisome proliferator-activated receptor gamma (PPARγ) agonist that enhances insulin sensitivity, reduces hepatic glucose production, and increases peripheral glucose uptake. It also modulates lipid metabolism by activating PPARα, leading to decreased triglyceride levels.

What the body does with it

Metabolism	Primarily metabolized by cytochrome P450 2C8 (CYP2C8) and to a lesser extent by CYP3A4
Excretion	Perchloracap is primarily excreted unchanged in urine (approx. 75–85%), with approximately 10–15% eliminated via bile/feces. Renal clearance accounts for the majority of systemic elimination, with minimal metabolism.
Half-life	The terminal elimination half-life is approximately 6.2 hours (range 5.0–8.1 hours) in adults with normal hepatic and renal function. This half-life supports twice-daily dosing in most clinical scenarios.
Protein binding	Approximately 94% bound to plasma proteins, primarily albumin.
Volume of Distribution	Volume of distribution is 0.55 L/kg (range 0.4–0.7 L/kg). This moderate Vd indicates distribution into total body water with some tissue binding.
Bioavailability	Oral bioavailability is 72% (±12%) due to first-pass metabolism; absorption is rapid and nearly complete (>90%).
Onset of Action	Intravenous: 2–5 minutes; Oral: 30–60 minutes on an empty stomach, delayed by food.
Duration of Action	Intravenous: 4–6 hours; Oral: 6–8 hours. Duration is dose-dependent; higher doses may prolong analgesic effect up to 12 hours.

Classification & Brands

Dosing & administration

1 mg orally once daily.

Dosage form	CAPSULE
Renal impairment	GFR 30-59 mL/min: 0.5 mg once daily. GFR 15-29 mL/min: 0.25 mg once daily. GFR <15 mL/min: not recommended.
Liver impairment	Child-Pugh A: no adjustment. Child-Pugh B: 0.5 mg once daily. Child-Pugh C: not recommended.
Pediatric use	0.02 mg/kg orally once daily; maximum 1 mg. Not recommended for weight <10 kg.
Geriatric use	Initial dose 0.5 mg orally once daily; titrate based on tolerability.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for PERCHLORACAP (PERCHLORACAP).

Breastfeeding	Excreted into human milk; M/P ratio not established. Potential for adverse effects in nursing infant (e.g., neurotoxicity). Contraindicated during breastfeeding.
Teratogenic Risk	First trimester: Increased risk of major congenital malformations (neural tube defects, cardiac anomalies) based on animal studies and limited human data. Second and third trimesters: Potential for fetal growth restriction and neurodevelopmental toxicity. Avoid use during pregnancy unless benefit outweighs risk.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

WARNING: CONGESTIVE HEART FAILURE. PERCHLORACAP may cause or exacerbate congestive heart failure in patients with NYHA Class III or IV heart failure. PERCHLORACAP is contraindicated in these patients. If used in patients with NYHA Class I or II heart failure, monitor closely for signs and symptoms of heart failure. Discontinue PERCHLORACAP if worsening heart failure occurs.

Side Effect Profile

Serious Effects

Absolute Contraindications

NYHA Class III or IV heart failure. History of a serious hypersensitivity reaction to PERCHLORACAP or any of its components. Diabetic ketoacidosis. Active bladder cancer (due to increased risk in animal studies). Severe hepatic impairment (Child-Pugh Class C).

Clinical Precautions

Precautions

May cause fluid retention leading to or exacerbating heart failure; monitor for signs of heart failure. Risk of bone fractures, particularly in female patients. Risk of hypoglycemia when used in combination with insulin or other insulin secretagogues. Can cause weight gain. Macular edema reported; consider ophthalmic evaluation if visual disturbances occur. Dose-dependent elevation of serum creatinine and decrease in estimated glomerular filtration rate (eGFR) observed.

Clinical Tips & Counseling

Drug interactions

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PERCHLORACAP

Clinical safety rating: caution

Comprehensive clinical and safety monograph for PERCHLORACAP (PERCHLORACAP).

How it works

What the body does with it

Metabolism	Primarily metabolized by cytochrome P450 2C8 (CYP2C8) and to a lesser extent by CYP3A4
Excretion	Perchloracap is primarily excreted unchanged in urine (approx. 75–85%), with approximately 10–15% eliminated via bile/feces. Renal clearance accounts for the majority of systemic elimination, with minimal metabolism.
Half-life	The terminal elimination half-life is approximately 6.2 hours (range 5.0–8.1 hours) in adults with normal hepatic and renal function. This half-life supports twice-daily dosing in most clinical scenarios.
Protein binding	Approximately 94% bound to plasma proteins, primarily albumin.
Volume of Distribution	Volume of distribution is 0.55 L/kg (range 0.4–0.7 L/kg). This moderate Vd indicates distribution into total body water with some tissue binding.
Bioavailability	Oral bioavailability is 72% (±12%) due to first-pass metabolism; absorption is rapid and nearly complete (>90%).
Onset of Action	Intravenous: 2–5 minutes; Oral: 30–60 minutes on an empty stomach, delayed by food.
Duration of Action	Intravenous: 4–6 hours; Oral: 6–8 hours. Duration is dose-dependent; higher doses may prolong analgesic effect up to 12 hours.

Classification & Brands

Dosing & administration

1 mg orally once daily.

Dosage form	CAPSULE
Renal impairment	GFR 30-59 mL/min: 0.5 mg once daily. GFR 15-29 mL/min: 0.25 mg once daily. GFR <15 mL/min: not recommended.
Liver impairment	Child-Pugh A: no adjustment. Child-Pugh B: 0.5 mg once daily. Child-Pugh C: not recommended.
Pediatric use	0.02 mg/kg orally once daily; maximum 1 mg. Not recommended for weight <10 kg.
Geriatric use	Initial dose 0.5 mg orally once daily; titrate based on tolerability.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for PERCHLORACAP (PERCHLORACAP).

Breastfeeding	Excreted into human milk; M/P ratio not established. Potential for adverse effects in nursing infant (e.g., neurotoxicity). Contraindicated during breastfeeding.
Teratogenic Risk	First trimester: Increased risk of major congenital malformations (neural tube defects, cardiac anomalies) based on animal studies and limited human data. Second and third trimesters: Potential for fetal growth restriction and neurodevelopmental toxicity. Avoid use during pregnancy unless benefit outweighs risk.
Fetal Monitoring