Summary Of Exposure |
A) USES: Colestipol is indicated as adjunctive therapy to diet for the reduction of elevated serum total and LDL-C in patients with primary hypercholesterolemia (elevated LDL-C) who do not respond adequately to diet.
B) PHARMACOLOGY: Colestipol hydrochloride, a lipid lowering agent, binds bile acids forming a complex that is then excreted in the feces. This action also results in partial removal of bile acids from the enterohepatic circulation which prevents its reabsorption.
C) EPIDEMIOLOGY: Overdose is rare.
D) WITH THERAPEUTIC USE
1) MOST COMMON: Constipation (can be severe). LESS FREQUENT: Nausea, vomiting, indigestion, heartburn, diarrhea, abdominal pain, flatulence. RARE: Chest pain, angina, tachycardia, rash, bleeding hemorrhoids, blood in the stool, peptic ulceration, cholecystitis, cholelithiasis, difficulty swallowing, transient esophageal obstruction, urticaria, dermatitis, elevated liver enzymes, musculoskeletal pain, aches, and pains in the extremities, joint pain, arthritis, backache, headache, dizziness, lightheadedness, insomnia, anorexia, fatigue, weakness, dyspnea, swelling of the hands or feet.
E) WITH POISONING/EXPOSURE
1) Overdose data are limited. In general, overdose effects are anticipated to be an extension of adverse effects at therapeutic doses. In the event of overdose, the chief potential harm would be obstruction of the gastrointestinal tract.
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Heent |
3.4.3) EYES
A) WITH THERAPEUTIC USE 1) ABNORMAL VISION: Isolated cases of diminution of visual acuity of a transient nature have been reported from colestipol therapy (Fellin et al, 1975). However, no eyeground changes were observed in ten patients after a one-year period with colestipol (Gross & Figueredo, 1973).
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Cardiovascular |
3.5.2) CLINICAL EFFECTS
A) CHEST PAIN 1) WITH THERAPEUTIC USE a) Chest pain, angina, and tachycardia have been reported infrequently during therapeutic use of colestipol (Prod Info Colestid(R) oral tablets, 2014).
B) TACHYCARDIA 1) WITH THERAPEUTIC USE a) Chest pain, angina and tachycardia have been reported infrequently during therapeutic use of colestipol (Prod Info Colestid(R) oral tablets, 2014).
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Respiratory |
3.6.2) CLINICAL EFFECTS
A) DYSPNEA 1) WITH THERAPEUTIC USE a) Shortness of breath has been reported infrequently during therapeutic use of colestipol (Prod Info Colestid(R) oral tablets, 2014).
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Neurologic |
3.7.2) CLINICAL EFFECTS
A) HEADACHE 1) WITH THERAPEUTIC USE a) Headache, including migraine and sinus headache, has occurred infrequently during therapeutic use (Prod Info Colestid(R) oral tablets, 2014).
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Gastrointestinal |
3.8.2) CLINICAL EFFECTS
A) CONSTIPATION 1) WITH THERAPEUTIC USE a) Constipation appears to be the most frequently occurring side effect of colestipol therapy and at times can be severe (Prod Info Colestid(R) oral tablets, 2014). Constipation is estimated to occur in approximately 10% of patients (Heel et al, 1980). Constipation cases are usually mild and transient in nature and can be controlled by traditional therapies. Increasing dietary fiber intake along with increasing daily fluid intake is the preferred initial treatment option for constipation. The addition of a stool softener may be warranted. In severe cases, some patients may require a decrease in the daily dose or a complete discontinuation of therapy (Prod Info Colestid(R) oral tablets, 2014).
B) DRUG-INDUCED GASTROINTESTINAL DISTURBANCE 1) WITH THERAPEUTIC USE a) Less frequent effects secondary to colestipol include: abdominal distention, vomiting, flatulence, diarrhea and perianal pruritus (Prod Info Colestid(R) oral tablets, 2014; Ryan et al, 1977). Bleeding hemorrhoids and blood in stool have been reported infrequently with therapeutic use (Prod Info Colestid(R) oral tablets, 2014).
b) INCIDENCE: Abdominal pain, vomiting and diarrhea have been reported in approximately 5% of patients (Heel et al, 1980a).
C) LOSS OF APPETITE 1) WITH THERAPEUTIC USE a) Anorexia has been reported infrequently during therapeutic use of colestipol (Prod Info Colestid(R) oral tablets, 2014).
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Hepatic |
3.9.2) CLINICAL EFFECTS
A) LIVER ENZYMES ABNORMAL 1) WITH THERAPEUTIC USE a) Transient and modest elevations of aspartate amino-transferase (AST, SGOT), alanine aminotransferase (ALT, SGPT) and alkaline phosphatase have been observed in colestipol patients (Prod Info Colestid(R) oral tablets, 2014).
b) CASE REPORT: A 65-year-old man with type IIa dyslipidemia developed asymptomatic hepatotoxicity (AST, ALT, and GGT were 10 times the normal value) after 3 months of therapy with colestipol granules. One week after discontinuing the therapy, serum transaminases fell quickly and all had returned to normal within 4 weeks of drug cessation. Rechallenge was not performed (Sirmans et al, 2001).
B) BILIARY CALCULUS 1) WITH THERAPEUTIC USE a) Cholelithiasis has been rarely reported with therapeutic colestipol use (Prod Info Colestid(R) oral tablets, 2014).
C) CHOLECYSTITIS 1) WITH THERAPEUTIC USE a) Cholecystitis has been rarely reported with therapeutic colestipol use (Prod Info Colestid(R) oral tablets, 2014).
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Acid-Base |
3.11.2) CLINICAL EFFECTS
A) ACIDOSIS 1) WITH THERAPEUTIC USE a) Colestipol hydrochloride is a chloride form of an anion exchange resin. Prolonged use of colestipol may lead to hyperchloremic acidosis (Prod Info Colestid(R) oral tablets, 2014). During this state, the kidneys reabsorb chloride in unusually large amounts, and serum chloride rises to preserve electroneutrality in the extracellular fluid; the unmeasured anion gap is normal (Isselbacher et al, 1994).
b) This form of metabolic acidosis has not been observed in some clinical trials (one long-term study up to 8 years) with either adults or children (Heel et al, 1980; Tsang et al, 1978; Ryan et al, 1977; Glueck et al, 1976).
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Hematologic |
3.13.2) CLINICAL EFFECTS
A) BLOOD COAGULATION DISORDER 1) WITH THERAPEUTIC USE a) Colestipol therapy can interfere with normal fat absorption and prevent the absorption of some fat-soluble vitamins such as vitamin K. Deficiency of vitamin K may increase bleeding tendencies due to hypoprothrombinemia. Hypoprothrombinemia due to vitamin K deficiency will respond promptly to parenteral vitamin K therapy, and recurrences can be prevented by oral administration of vitamin K (Prod Info Colestid(R) oral tablets, 2014).
b) Investigators reported no hematologic changes; the prolonged interference with absorption of vitamins A, D, E and K suggests that these vitamins be supplemented during long-term treatment (Cooper & Michel, 1975).
c) A temporary decrease in 25-hydroxy-vitamin D below normal limits was noted in 3 children after long-term use of colestipol (over 18 to 20 months of therapy). The levels appeared to return to baseline after 20 months without a change in the drug therapy (Tsang et al, 1978).
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Dermatologic |
3.14.2) CLINICAL EFFECTS
A) DERMATITIS 1) WITH THERAPEUTIC USE a) Dermatitis has been rarely reported in patients receiving colestipol granules (Prod Info Colestid(R) oral tablets, 2014). Dermatitis was reported in 3 patients receiving 30 grams/day of colestipol, and administration of vitamins A and E resolved the symptoms (Fellin et al, 1975). Dryness of the skin was also reported in 2 of 18 patients receiving 15 grams colestipol daily (Sachs & Wolfman, 1974).
B) ERUPTION 1) WITH THERAPEUTIC USE a) Rash has been infrequently reported with therapeutic use of colestipol. Urticaria has been rarely reported (Prod Info Colestid(R) oral tablets, 2014).
C) URTICARIA 1) WITH THERAPEUTIC USE a) Urticaria has been rarely reported with therapeutic use of colestipol (Prod Info Colestid(R) oral tablets, 2014).
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Endocrine |
3.16.2) CLINICAL EFFECTS
A) FINDING OF THYROID FUNCTION 1) WITH THERAPEUTIC USE a) Hypothyroidism especially in patients with limited thyroid reserve is theoretically possible (Prod Info Colestid(R) oral tablets, 2014).
b) Colestipol combined with niacin was implicated in the reduction of thyroxine-binding globulin levels. One hundred eighty-eight men received either colestipol (30 grams/day) plus niacin (3 to 6 grams/day) or an identical placebo. After 1 year, a significant difference in thyroid function between the drug and placebo groups was observed. The average reduction in T(4) was 1.5 micrograms/deciliter (mcg/dL). Nineteen percent of the drug-treated group experienced T(4) values less than the normal limit (4.5 mcg/dL). Colestipol alone and niacin alone have not significantly lowered thyroid function (Cashin-Hemphill et al, 1987).
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Reproductive |
3.20.1) SUMMARY
A) Based on its lack of absorption systemically (less than 0.17% of the dose), colestipol is not expected to cause fetal harm; however, due to its known interference with absorption of fat-soluble vitamins, its use may be detrimental during pregnancy even with vitamin supplementation. Administer during pregnancy only if the potential maternal benefit justifies the risk to the fetus.
3.20.3) EFFECTS IN PREGNANCY
A) RISK SUMMARY 1) Administer during pregnancy only if the potential maternal benefit justifies the risk to the fetus (Prod Info Colestid(R) oral tablets, 2014; Prod Info Flavored Colestid(R) oral suspension, 2014).
2) Based on its lack of absorption systemically (less than 0.17% of the dose), colestipol is not expected to cause fetal harm; however, due to its known interference with absorption of fat-soluble vitamins, its use may be detrimental during pregnancy even with vitamin supplementation (Prod Info Colestid(R) oral tablets, 2014; Prod Info Flavored Colestid(R) oral suspension, 2014).
3.20.4) EFFECTS DURING BREAST-FEEDING
A) BREAST MILK 1) Due to the possibility of inadequate vitamin absorption, exercise caution when administering colestipol to a lactating woman (Prod Info Colestid(R) oral tablets, 2014; Prod Info Flavored Colestid(R) oral suspension, 2014).
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