Welchol
(colesevelam hydrochloride)Dosage & Administration
Tablets
Take 6 tablets once daily or 3 tablets twice daily with a meal and liquid.
For Oral Suspension
Take one packet once daily with a meal. To prepare, empty the entire contents of one packet into a glass or cup. Add 1 cup of water, fruit juice, or diet soft drinks. Stir well and drink.
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Welchol Prescribing Information
Primary Hyperlipidemia
WELCHOL is indicated as an adjunct to diet and exercise to reduce elevated low-density lipoprotein cholesterol (LDL-C) in adults with primary hyperlipidemia.
WELCHOL is indicated to reduce LDL-C levels in boys and postmenarchal girls, 10 to 17 years of age, with heterozygous familial hypercholesterolemia (HeFH) who are unable to reach LDL-C target levels despite an adequate trial of dietary therapy and lifestyle modification.
Type 2 Diabetes Mellitus
WELCHOL is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus .
Limitations of Use
- WELCHOL should not be used for the treatment of type 1 diabetes or for the treatment of diabetic ketoacidosis.
- WELCHOL has not been studied in Fredrickson Type I, III, IV, and V dyslipidemias.
Testing Prior to Initiation of WELCHOL
Obtain lipid parameters, including triglyceride (TG) levels, before starting WELCHOL. WELCHOL is contraindicated in patients with TG levels >500 mg/dL [see Contraindications (4)and Warnings and Precautions (5.1)] .
Recommended Dosage in Primary Hyperlipidemia and Type 2 Diabetes Mellitus
The recommended dosage of WELCHOL for adults and for boys and postmenarchal girls aged 10 to 17 years with primary hyperlipidemia is 3.75 grams daily. The recommended dosage of WELCHOL for adults with type 2 diabetes mellitus is 3.75 grams daily. WELCHOL should be taken as follows:
Tablets
Take 6 tablets once daily or 3 tablets twice daily. Due to tablet size, WELCHOL for oral suspension is recommended for use in the pediatric population.
For Oral Suspension
Take one packet once daily.
Important Dosing Information for Primary Hyperlipidemia
WELCHOL can be dosed at the same time as a statin, or WELCHOL and the statin can be dosed apart .Monitor lipid levels within 4 to 6 weeks after initiation of WELCHOL.
Administration Instructions
Tablets
Take WELCHOL tablets with a meal and liquid. For patients with difficulty swallowing tablets, use WELCHOL for oral suspension [see Warnings and Precautions (5.2)].
For Oral Suspension
To prepare, empty the entire contents of one packet into a glass or cup. Add 1 cup (8 ounces) of water, fruit juice, or diet soft drinks. Stir well and drink. Take WELCHOL oral suspension with meals. Do not take WELCHOL oral suspension in its dry form. Due to tablet size, WELCHOL for oral suspension is recommended for use in the pediatric population.
- Tablets: 625 mg tablets are off-white, oval, film-coated and imprinted with "Sankyo" and "C01" on one side.
- For Oral Suspension: 3.75 gram packet containing a white to pale yellow powder with yellow granules.
Pregnancy
Risk Summary
WELCHOL is not absorbed systemically following oral administration, and maternal use is not expected to result in fetal exposure to the drug. Limited available data on the use of WELCHOL are insufficient to determine a drug-associated risk of major congenital malformations or miscarriage. In animal reproduction studies, no evidence of either maternal or fetal toxicity was found in rats or rabbits exposed to colesevelam hydrochloride during the period of fetal organogenesis at 8 and 5 times, respectively, the maximum recommended human dose (MRHD) of 3.75 g/day, based on body surface area (mg/m 2). No adverse effects on offspring survival and development were observed in rats administered 5 times the MRHD (see Data). WELCHOL may decrease the absorption of fat-soluble vitamins [see Warnings and Precautions (5.3)]. There are no data available on the effect of colesevelam hydrochloride on the absorption of fat-soluble vitamins in pregnant women. If the patient becomes pregnant while taking WELCHOL, the patient should be advised of the lack of known clinical benefit with continued use during pregnancy.
The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the US general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.
Data
Human Data
There are no adequate and well-controlled studies of colesevelam hydrochloride use in pregnant women. In the postmarketing setting there have been infrequent reports of pregnancy with use of WELCHOL and a causal association with congenital anomalies has not been established.
Animal Data
In pregnant rats given dietary doses of 0.3, 1.0, 3.0 g/kg/day colesevelam hydrochloride from gestation days 7 through 17, no teratogenic effects were observed. Exposures at 3.0 g/kg/day were 8 times the human exposure at 3.75 g/day MRHD, based on body surface area (mg/m 2).
In pregnant rabbits given oral gavage doses of 0.1, 0.5, 1.0 g/kg/day colesevelam hydrochloride from gestation days 6 through 18, no teratogenic effects were observed. Exposures at 1.0 g/kg/day were 5 times the human exposure at 3.75 g/day MRHD, based on body surface area (mg/m 2).
In pregnant rats given oral gavage doses of 0.1, 0.3, 1.0 g/kg/day colesevelam hydrochloride from gestation day 6 through lactation day 21 (weaning), no adverse effects on survival and development were observed. Exposures at 1.0 g/kg/day were 5 times the human exposure at 3.75 g/day MRHD, based on body surface area (mg/m 2).
Lactation
Risk Summary
WELCHOL is not absorbed systemically by the mother following oral administration, and breastfeeding is not expected to result in exposure of the child to WELCHOL.
Females and Males of Reproductive Potential
Contraception
Use of WELCHOL may reduce the efficacy of oral contraceptives. Advise patients to take oral contraceptives at least 4 hours prior to taking WELCHOL [see Drug Interactions (7)].
Pediatric Use
Primary Hyperlipidemia
The safety and effectiveness of WELCHOL to reduce LDL-C levels in boys and postmenarchal girls 10 to 17 years of age with HeFH who are unable to reach LDL-C target levels despite an adequate trial of dietary therapy and lifestyle modification have been established. Use of WELCHOL for this indication is supported by a study in 129 WELCHOL-treated pediatric patients aged 10 to 17 years with HeFH [see Clinical Studies (14.1)] . Adverse reactions commonly observed in pediatric patients compared to placebo, but not in adults, included headache (3.9%), creatine phosphokinase increase (2.3%), and vomiting (2.3%) [see Adverse Reactions (6.1)] . There were no significant effects on fat-soluble vitamin levels or clotting factors in the adolescent boys or girls relative to placebo.
Due to WELCHOL tablet size, WELCHOL for oral suspension is recommended for use in the pediatric population [see Dosage and Administration (2.2, 2.4)] . The safety and effectiveness of WELCHOL in pediatric patients with HeFH less than 10 years of age or in premenarchal females have not been established.
Type 2 Diabetes Mellitus
The safety and effectiveness of WELCHOL to improve glycemic control in pediatric patients with type 2 diabetes mellitus have not been established. Effectiveness was not demonstrated in a 6-month, adequate and well-controlled study conducted in 141 WELCHOL-treated pediatric patients aged 10 to 17 years with type 2 diabetes mellitus.
Geriatric Use
Primary Hyperlipidemia
Of the 1350 patients enrolled in the hyperlipidemia clinical studies, 349 (26%) were ≥65 years old, and 58 (4%) were ≥75 years old. No overall differences in safety or effectiveness were observed between these subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.
Type 2 Diabetes Mellitus
Of the 2048 patients enrolled in the six diabetes studies, 397 (19%) were ≥65 years old, and 36 (2%) were ≥75 years old. In these trials, WELCHOL 3.8 g/day or placebo was added onto background anti-diabetic therapy. No overall differences in safety or effectiveness were observed between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.
Renal Impairment
Type 2 Diabetes Mellitus
Of the 2048 patients enrolled in the six diabetes studies, 807 (39%) had mild renal insufficiency (creatinine clearance [CrCl] 50-<80 mL/min), 61 (3%) had moderate renal insufficiency (CrCl 30-<50 mL/min), and none had severe renal insufficiency (CrCl <30 mL/min), as estimated from baseline serum creatinine using the Modification of Diet in Renal Disease (MDRD) equation. No overall differences in safety or effectiveness were observed between patients with CrCl <50 mL/min (n=53) and those with a CrCl ≥50 mL/min (n=1075) in the add-on to metformin, sulfonylureas, and insulin diabetes studies. In the monotherapy study and add-on to pioglitazone study, only 3 and 5 patients, respectively, had moderate renal insufficiency.
WELCHOL is contraindicated in patients with:
- Serum TG concentrations >500 mg/dL [see Warnings and Precautions (5.1)]
- History of hypertriglyceridemia-induced pancreatitis [see Warnings and Precautions (5.1)]
- A history of bowel obstruction [see Warnings and Precautions (5.2)]
Hypertriglyceridemia and Pancreatitis
WELCHOL, like other bile acid sequestrants, can increase serum TG concentrations. Hypertriglyceridemia can cause acute pancreatitis.
WELCHOL had effects on serum TG (median increase 5% compared to placebo) in trials of patients with primary hyperlipidemia.
In trials in patients with type 2 diabetes, greater increases in TG levels occurred when WELCHOL was used as monotherapy (median increase 9.7% compared to placebo) and when WELCHOL was used in combination with pioglitazone (median increase 11% compared to placebo in combination with pioglitazone), sulfonylureas (median increase 18% compared to placebo in combination with sulfonylureas), and insulin (median increase 22% compared to placebo in combination with insulin) [see Adverse Reactions (6.1)].
Obtain lipid parameters, including TG levels, before starting WELCHOL and periodically thereafter. WELCHOL is contraindicated in patients with TG levels >500 mg/dL or patients with a history of hypertriglyceridemia-induced pancreatitis [see Contraindications (4)] . Patients with TG levels greater than 300 mg/dL could have greater increases in serum TG levels with WELCHOL and may require additional TG monitoring. Instruct patients to discontinue WELCHOL and seek prompt medical attention if the symptoms of acute pancreatitis occur (e.g., severe abdominal pain with or without nausea and vomiting). Discontinue WELCHOL if TG levels exceed 500 mg/dL [see Adverse Reactions (6.1)] .
Gastrointestinal Obstruction
Postmarketing cases of bowel obstruction have occurred with WELCHOL [see Adverse Reactions (6.2)] . Because of its constipating effects, WELCHOL is not recommended in patients with gastroparesis, other gastrointestinal motility disorders, and in those who have had major gastrointestinal tract surgery and who may be at risk for bowel obstruction. WELCHOL is contraindicated in patients with a history of bowel obstruction [see Contraindications (4)] . Instruct patients to promptly discontinue WELCHOL and seek medical attention if severe abdominal pain or severe constipation occurs.
Because of the tablet size, WELCHOL tablets can cause dysphagia or esophageal obstruction. For patients with difficulty swallowing tablets, use WELCHOL for oral suspension.
Vitamin K or Fat-Soluble Vitamin Deficiencies
WELCHOL may decrease the absorption of fat-soluble vitamins A, D, E, and K. Patients with a susceptibility to deficiencies of vitamin K (e.g., patients on warfarin, patients with malabsorption syndromes) or other fat-soluble vitamins may be at increased risk when taking WELCHOL.
Patients on oral vitamin supplementation should take their vitamins at least 4 hours prior to WELCHOL [see Drug Interactions (7.1)].
Drug Interactions
WELCHOL reduces gastrointestinal absorption of some drugs. Administer drugs with a known interaction at least 4 hours prior to WELCHOL [see Drug Interactions (7)] .
Due to the potential for decreased absorption of other drugs that have not been tested for interaction, especially those with a narrow therapeutic index, consider administering at least 4 hours prior to WELCHOL [see Clinical Pharmacology (12.3)].
Risks in Patients with Phenylketonuria (PKU)
Phenylalanine can be harmful to patients with PKU. WELCHOL for oral suspension contains phenylalanine, a component of aspartame. Each 3.75 gram packet contains 27 mg of phenylalanine. Before prescribing WELCHOL for oral suspension to a patient with PKU, consider the combined daily amount of phenylalanine from all sources, including WELCHOL for oral suspension.