Colestyramine

C10A - Cholesterol and triglyceride regulating preparations ATC C10AC01 Unknown approved 1973 Oral

JFDA label: Colestyramine Rubio

Mechanism of Action

Sequestering Agent of Bile acids — Bile acids sequestering agent

Target	Action	Gene / class
Bile acids efficacy	SEQUESTERING AGENT

Indications

Off-label

Chronic diarrhea due to bile acid malabsorption
Enhance elimination of digoxin when non-life-threatening toxicity occurs
Hyperthyroidism (Graves’ disease) (adjunctive therapy)

Contraindications

Source: Lexicomp

Hypersensitivity to bile acid sequestering resins or any component of the formulation Absolute
complete biliary obstruction Absolute

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Cardiac disorders (2)

Not Known Edema · syncope

Nervous system disorders (8)

Not Known Anxiety · dizziness · drowsiness · fatigue · headache · neuralgia · paresthesia · vertigo

Hepatobiliary disorders (1)

Not Known Abnormal hepatic function tests

Renal and urinary disorders (3)

Not Known Diuresis · dysuria · hematuria

Blood and lymphatic system disorders (7)

Not Known Adenopathy · anemia · bruise · hemorrhage · hypoprothrombinemia · prolonged prothrombin time · rectal hemorrhage

Metabolism and nutrition disorders (4)

Not Known Hyperchloremic metabolic acidosis (children) · increased libido · weight gain · weight loss

Gastrointestinal disorders (28)

Not Known Abdominal pain · anorexia · biliary colic · constipation · dental bleeding · dental caries · dental discoloration · diarrhea · diverticulitis · duodenal ulcer with hemorrhage · dysgeusia · dysphagia · eructation · flatulence · gallbladder calcification · gastric ulcer · gastrointestinal hemorrhage · hemorrhoidal bleeding · hiccups · intestinal obstruction (rare) · melena · nausea · pancreatitis · rectal pain · steatorrhea · tongue irritation · tooth enamel damage (dental erosion) · vomiting

Skin and subcutaneous tissue disorders (4)

Not Known Perianal skin irritation · skin irritation · skin rash · urticaria

Musculoskeletal and connective tissue disorders (5)

Not Known Arthralgia · arthritis · back pain · myalgia · osteoporosis

Eye disorders (2)

Not Known Nocturnal amblyopia (rare) · uveitis

Ear and labyrinth disorders (1)

Not Known Tinnitus

Respiratory, thoracic and mediastinal disorders (3)

Not Known Asthma · dyspnea · wheezing

Dosing

Source: Lexicomp

Dosages are expressed in terms of anhydrous resin: Dyslipidemia: Oral: Initial: 4 g 1 to 2 times/day; increase gradually over ≥1-month intervals; maintenance: 8 to 16 g/day divided in 2 doses; maximum: 24 g/day Chronic diarrhea due to bile acid malabsorption (off-label use): Oral: Initial: 4 g once daily; increase by 4 g at weekly intervals in 1 to 4 divided doses; maximum: 36 g/day (Wilcox 2014). Additional data may be needed to further define the role of cholestyramine resin in this condition. Hyperthyroidism (Graves’ disease) (adjunctive therapy) (off-label use): Oral: 4 g twice daily (Tsai 2005) or 4 g 3 times daily (Mercado 1996). Note: Use in combination with an antithyroid drug (eg, methimazole or propylthiouracil) and propranolol.

(For additional information see "Cholestyramine resin: Pediatric drug information") Dosages are expressed in terms of anhydrous resin: Dyslipidemia (off-label use): Oral: 240 mg/kg/day in 2 to 3 divided doses; titrate dose to response and tolerance; maximum: 8 g/day

Refer to adult dosing.

There are no dosage adjustments provided in the manufacturer's labeling; however, use with caution in renal impairment; may cause hyperchloremic acidosis.

No dosage adjustment necessary; not absorbed from the gastrointestinal tract.

Warnings & Precautions

Source: Lexicomp

Bleeding

Chronic use may be associated with bleeding problems (especially in high doses); may be prevented with use of oral vitamin K therapy.

Constipation

May produce or exacerbate constipation problems; initiate therapy at a reduced dose in patients with a history of constipation. Hemorrhoids may be worsened. Disease-related concerns:

Hypertriglyceridemia

Bile acid sequestrants should not be used in patients with baseline fasting triglyceride levels ≥300 mg/dL or type III hyperlipoproteinemia since severe triglyceride elevations may occur. Use bile acid sequestrants with caution in patients with triglyceride levels 250 to 299 mg/dL and evaluate a fasting lipid panel in 4 to 6 weeks after initiation; discontinue use if triglycerides are >400 mg/dL (Stone 2013).

Renal impairment

Use caution in patients with renal impairment. Concurrent drug therapy issues:

Decreased absorption (orally administered drugs)

Not to be taken simultaneously with many other medicines (decreased absorption).

Patients susceptible to fat-soluble vitamin deficiencies

Use with caution in patients susceptible to fat-soluble vitamin deficiencies. Absorption of fat soluble vitamins A, D, E, and K and folic acid may be decreased; patients should take vitamins ≥4 hours before cholestyramine. Dosage form specific issues:

Phenylalanine

Some products may contain phenylalanine. Other warnings/precautions:

Hyperlipidemia

Secondary causes of hyperlipidemia should be ruled out prior to therapy.

Pregnancy & Lactation

Pregnancy

FDA category C

Lipid concentrations increase during pregnancy as required for normal fetal development. When increases are greater than expected, supervised dietary intervention should be initiated. Bile acid sequestrants are recommended when treatment is needed (Avis 2009; Jacobson 2015). Cholestyramine is not absorbed systemically, but may interfere with maternal vitamin absorption; therefore, regular prenatal supplementation may not be adequate.

Lactation

Due to lack of systemic absorption, cholestyramine is not expected to be present in breast milk. When treatment for hypercholesterolemia in breastfeeding women is needed, therapy with bile acid sequestrants may be considered (Jacobson 2015; NICE 2008). However, because use may interfere with maternal vitamin absorption, the manufacturer recommends caution be used if administered to breastfeeding women.

Monitoring

Clinical pearl	Fasting lipid profile before initiating treatment, 3 months after initiation (within 4 to 6 weeks if baseline fasting triglycerides of 250 to 299 mg/dL), and every 6 to 12 months thereafter (Stone 2013)

Biology & Pharmacokinetics

Pharmacokinetics

Drug–drug interactions (57, DDInter)

Interacting drug	Severity	Management
Mycophenolic acid	major
Teriflunomide	major
Acetohexamide	moderate
Budesonide	moderate
Calcifediol	moderate
Calcitriol	moderate
Chenodeoxycholic acid	moderate
Chlorpropamide	moderate
Cholecalciferol	moderate
Cholic Acid	moderate
Deferasirox	moderate
Deflazacort	moderate
Dexamethasone	moderate
Dicoumarol	moderate
Diethylstilbestrol	moderate
Dihydrotachysterol	moderate
Doxercalciferol	moderate
Ergocalciferol	moderate
Ethinylestradiol	moderate
Fludrocortisone	moderate
Folic acid	moderate
Glimepiride	moderate
Glipizide	moderate
Glyburide	moderate
Hydrocortisone	moderate
Leflunomide	moderate
Levothyroxine	moderate
Liothyronine	moderate
Medroxyprogesterone acetate	moderate
Megestrol acetate	moderate
Methylprednisolone	moderate
Metronidazole	moderate
Obeticholic acid	moderate
Paricalcitol	moderate
Phylloquinone	moderate
Prednisolone	moderate
Prednisone	moderate
Simvastatin	moderate
Sirolimus	moderate
Temsirolimus	moderate

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Registered Products (1)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
Colestyramine Rubio	Sachet 4 g	50 sachet	Al-Omawai Drug Store	25.710