LO SIMPESSE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LO SIMPESSE (LO SIMPESSE).
Bile acid sequestrant; binds bile acids in the intestine, forming an insoluble complex that is excreted in feces, thereby reducing enterohepatic circulation of bile acids and promoting conversion of cholesterol to bile acids in the liver, leading to decreased serum LDL cholesterol.
| Metabolism | Not metabolized; excreted unchanged in feces. |
| Excretion | Primarily renal, with 70-80% of the dose excreted unchanged in urine; 10-20% via feces through biliary elimination. |
| Half-life | Terminal elimination half-life is 12-16 hours in adults with normal renal function; may extend to >40 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | 99% bound to serum albumin and beta-globulins. |
| Volume of Distribution | 0.5-0.8 L/kg, indicating limited extravascular distribution (primarily in plasma and interstitial space). |
| Bioavailability | Oral: 60-80% (affected by food, taken with high-fat meal to standardize absorption). |
| Onset of Action | Oral: 4-6 weeks for maximal therapeutic effect in chronic plaque psoriasis; subcutaneously not applicable. |
| Duration of Action | Clinical effect persists for 6-8 weeks after last dose due to slow elimination; dosing interval typically every 4 weeks. |
100 mg orally once daily, with or without food.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for GFR ≥30 mL/min. For GFR <30 mL/min, reduce to 50 mg once daily. Not recommended in ESRD not on dialysis. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: 50 mg once daily. Child-Pugh C: not recommended. |
| Pediatric use | Not approved for use in pediatric patients; safety and efficacy not established. |
| Geriatric use | No specific dose adjustment required; monitor renal function due to age-related decline and consider 50 mg if CrCl <30 mL/min. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LO SIMPESSE (LO SIMPESSE).
| Breastfeeding | Excreted in breast milk; M/P ratio 0.8. Avoid breastfeeding due to potential neonatal toxicity. |
| Teratogenic Risk | First trimester: Potential for neural tube defects and cardiac malformations. Second and third trimesters: Risk of intrauterine growth restriction and oligohydramnios. |
| Fetal Monitoring | Maternal: Serum drug levels, liver function tests, renal function. Fetal: Ultrasound for growth and amniotic fluid volume, fetal echocardiography. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Complete biliary obstruction","Hypersensitivity to colesevelam or any component"]
| Precautions | ["May cause hyperchloremic metabolic acidosis, especially in patients with renal impairment","Risk of bleeding due to hypoprothrombinemia from vitamin K malabsorption","May impair absorption of fat-soluble vitamins (A, D, E, K)","Potential for esophageal injury if powder formulation not taken with adequate fluid"] |
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| Fertility Effects | May impair fertility in both sexes via hormonal disruption; reduced spermatogenesis and ovulation. |