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colestipol (Colestid)

 

Classes: Bile Acid Sequestrants

Dosing and uses of Colestid (colestipol)

 

Adult dosage forms and strengths

granules, bottle

  • 5g

granules, packets

  • 5g

tablet

  • 1g

 

Hyperlipidemia

Tablets: 2 g PO qDay or q12hr; increases of 2 g should occur at 1- or 2-month intervals; titrate not to exceed 16 g/day

Granules: 5 g PO qDay; increases of 5 g should occur at 1- or 2-month intervals; titrate not to exceed 30 g/day

 

Overdose Management

Generally considered safe in acute overdose although not formally studied

Adverse drug reactions in overdose may include peripheral neuropathy, diarrhea, increase K+, myopathy , rhabdomyolysis, acute renal failure, elevated liver function tests, eye lens opacities)

Check renal function tests, urine myoglobin, CPK, LFT's

 

Administration

Mix dry form in water/fluids to avoid inhalation or esophageal distress

Mix granules in fluids or food; take before meals

Do not crush, chew, or cut tablets

Take 1 tablet at a time; swallow with water or other fluids

 

Other Information

Monitor: Serum cholesterol, triglycerides

 

Other Indications & Uses

Used in relief of pruritus associated with elevated levels of bile

Used to decrease plasma half-life of digoxin in toxicity

Hypercholesterolemia (adjunct to diet for Type IIa & IIb hyperlipidemia)

 

Pediatric dosage forms and strengths

Safety & efficacy not established

 

Geriatric dosage forms and strengths

Tablets: 2 g PO qDay or q12hr; increases of 2 g should occur at 1- or 2-month intervals; titrate not to exceed 16 g/day

Granules: 5 g PO qDay; increases of 5 g should occur at 1- or 2-month intervals; titrate not to exceed 30 g/day

 

Colestid (colestipol) adverse (side) effects

>10%

Gastrointestinal (mostly)

Constipation

 

1-10%

Stomach pain

Belching

Nausea/vomiting

Flatulance

Diarrhea

Dizziness

Anxiety

Vertigo

Fatigue

Drowsiness

 

Frequency not defined

Heartburn

Steatorrhea

Malabsorption of fat-soluble vitamins

Gallstones

Dysphagia

GI bleeding

Cholecystitis

Peptic ulceration

Transient esophageal obstruction

 

Warnings

Contraindications

Hypersensitivity to colestipoL

Bowel obstruction

 

Cautions

Increased risk of bleeding due to hypoprothrombinemia from vitamin K deficiency

May interfere with fat absorption, and decrease absorption of fat-soluble vitamins (A, D, E, K)

May worsen pre-existing constipation

Take other medications 1 hr before or 4 hr after colestipoL

If significant increase in triglycerides, consider dose reduction, discontinuation or alternatives

 

Pregnancy and lactation

Pregnancy category: C

Lactation: use caution; may interfere with vitamin absorption in infants

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Colestid (colestipol)

Mechanism of action

Forms a soluble complex after binding to bile acid, increasing fecal loss of bile acid-bound low-density lipoprotein cholesteroL

 

Pharmacokinetics

Onset: initial effect: 24-48 hr; max effect: 1 wk

Bioavailability: Not absorbed

Metabolism: Not metabolized

Excretion: feces 100%