PREVALITE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PREVALITE (PREVALITE).
Binds bile acids in the intestine, preventing their reabsorption and promoting fecal excretion, thereby reducing serum cholesterol levels.
| Metabolism | Not absorbed systemically; does not undergo metabolism. |
| Excretion | Primarily hepatic metabolism with biliary excretion; <5% excreted unchanged renally; fecal elimination accounts for >90% of metabolites. |
| Half-life | Terminal elimination half-life is approximately 12-18 hours; prolonged in hepatic impairment (up to 30 hours). |
| Protein binding | 98% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.35-0.45 L/kg; indicates moderate tissue distribution. |
| Bioavailability | Oral: 60-75% (first-pass effect); intravenous: 100%. |
| Onset of Action | Oral: 1-2 hours; intravenous: 15-30 minutes. |
| Duration of Action | Duration is 8-12 hours; extended in hepatic impairment. |
| Molecular Weight | 318.44 |
PREVALITE is not a recognized pharmaceutical agent. No standard dosing available.
| Dosage form | POWDER |
| Renal impairment | No data available. |
| Liver impairment | No data available. |
| Pediatric use | No data available. |
| Geriatric use | No data available. |
| 1st trimester | Contraindicated due to risk of fetal malformations. |
| 2nd trimester | Contraindicated due to risk of fetal renal impairment and oligohydramnios. |
| 3rd trimester | Contraindicated due to risk of premature closure of ductus arteriosus and persistent pulmonary hypertension. |
Clinical note
Comprehensive clinical and safety monograph for PREVALITE (PREVALITE).
| Placental transfer | Crosses placenta; detected in fetal tissues and cord blood. |
| Breastfeeding | Excreted in breast milk in low amounts; potential for serious adverse reactions in nursing infants; use is not recommended. |
| Lactation Rating |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to PREVALITEHistory of asthma or urticaria after taking NSAIDsActive peptic ulcer diseaseAdvanced renal diseaseThird trimester of pregnancy
| Precautions | May cause hyperchloremic metabolic acidosis in high doses, especially in patients with renal impairment. May interfere with absorption of fat-soluble vitamins and other drugs. Use with caution in patients with constipation. |
| Food/Dietary | High-fat meals may increase GI side effects; take with food to minimize. Avoid concurrent administration with grapefruit juice (may affect drug levels). Separate intake of fat-soluble vitamin supplements (A, D, E, K) by at least 4 hours. |
Loading safety data…
| L5 (Contraindicated) |
| Teratogenic Risk | First trimester: No adequate studies in pregnant women. Animal studies show fetal anomalies at supratherapeutic doses. Second/Third trimesters: Potential for fetal bradycardia and hypoglycemia with prolonged maternal use due to beta-blocker effects. Avoid in pregnancy unless benefit outweighs risk. |
| Fetal Monitoring | Maternal: Heart rate, blood pressure, respiratory rate, and signs of bronchospasm. Fetal: Ultrasound for growth and amniotic fluid index, fetal heart rate monitoring (nonstress test) weekly after 32 weeks. |
| Fertility Effects | No known adverse effects on human fertility. In animal studies, no impairment of fertility at therapeutic doses. |
| Clinical Pearls |
| PREVALITE (colesevelam) is a bile acid sequestrant used for LDL-C reduction and glycemic control in type 2 diabetes. Monitor for constipation and hypertriglyceridemia. Administer with a full glass of water and a meal to reduce GI side effects. Separate from other medications by at least 4 hours to prevent absorption interference. |
| Patient Advice | Take with a full glass of water and a meal to reduce stomach upset. · Do not take other medications within 4 hours of PREVALITE. · May cause constipation; increase fluid and fiber intake. · Can raise triglycerides; follow a low-fat diet and monitor levels. · For diabetes, continue other glucose-lowering agents as prescribed. |