Pruritus cholestyramine

Biliary obstruction (cholestyramine only) Relief of pruritus associated with partial biliary obstruction. 

Cholestyramine (Questran/ Questran Light Prevalite) [AntilipemiC/ Bile Acid Sequestrant] Uses Hypercholesterolemia Rx pruritus associated w/ partial biliary obst D associated w/ excess fecal bile acids ... 

Therapeutic uses The bile acid binding resins are the drugs of choice (often in combination with diet or niacin) in treating Type lla and lib hyperlipidemias. [Note In those rare individuals who are homozygous for Type lla, that is, for whom functional LDL receptors are totally lacking, these drugs have little effect on plasma LDL levels.] Cholestyramine can also relieve pruritus caused by accumulation of bile acids in patients with biliary obstruction. 

Treatment of icteric episodes with phenobarbital (3 x 20-60 mg/day) together with phototherapy (430-470 nm, 8-12 hr/day) and/or plasmapheresis is indicated. Cholestyramine (3x4 g/day) or cholestipol (3x5 g/day) may be used to treat pruritus. Qther recommended effective antipruritics are naloxone (2-3 x 0.4 mg/day, i.v.) or naltrexone (2-4 x 25-50 mg/day), which act as opi-oidergic neurotransmitters. (69) It is also possible to use the 5-HT3 antagonist ondansetron (3 x 4.8 mg/day, i.v. or orally). (64) Refractory cholestasis pruritus has recently been treated successfully with dronabinol (50) and also with sertraline. Administration of ursodeoxycholic acid (22, 53), medium-chain fatty acids, PUFA (65) and fat-soluble vitamins (especially vitamin K) is recommended. (s. pp 6, 47) (s. tab. 13.11)... 

Cholestyramine may prove necessary for severe pruritus due to a cholestatic course of disease (4-8 g prior to breakfast) - if antihistamines were unsuccessful. With such a cholestatic course of disease, the application of ursodeoxycholic acid (2-3 x 250 mg) is most suitable. (166) In some cases with a fulminant course, interferon alpha has been successfully used. Special diets , glucocorticoids or other medication are not necessary. 

Cholestyramine may be advisable in cases of pronounced pruritus as a result of a cholestatic course of disease (4-8 g before breakfast). 

Treatment of intrahepatic biliary atresia is symptomatic, with intramuscular replacement of vitamins A, D, and E. Medium chain triglycerides that do not need bile acids for absorption provide calories in patients with partial atresia. Cholestyramine may relieve pruritus. Ursodeoxychofic acid reduces serum enzyme activities and refieves pruritus in some patients. 

Cholestyramine is indicated as adjunctive therapy to diet for the reduction of elevated serum cholesterol in patients with primary hypercholesterolemia (elevated low-density lipoprotein [LDL] cholesterol) who do not respond adequately to diet. Similarly, it is indicated for the relief of pruritus associated with partial biliary obstruction. Cholestyramine is not absorbed but binds to bile acids in the intestine, whereupon it is eliminated. To replenish the lost bile acid, cholesterol is then converted to bile acid, and this lowers the level of cholesterol (see Figure 34). Cholestyramine has also been used in the treatment of cholestasis to control the intense pruritis. It reduces the LDL level in 4 to 7 days, and the maximum effect is seen in 14 days. 

Cholestyramine resin also is helpful for the relief of pruritus associated with partial biliary obstruction and in conditions such as primary biliary cirrhosis. Cholestyramine increases fecal excretion of bile acids and reduces circulating and eventually systemic levels with relief of pruritus in -1-3 weeks. 

Cholestasis-associated pruritus may respond to cholestyramine (Questran, others see Chapter 35), ursodeoxycholic acid (achgall, others see Chapter 37), ondansetron (zofran see Chapter 37), or rifampin (see Chapter 47). Recently, nalmefene (revex) (20 mg twice per day) has been shown to be effective in cholestatic pruritus. 

Cholestyramine was originally developed in the 1960s to treat pruritus secondary to elevated plasma concentrations of bile acids in patients with cholestasis. Its ability to bihd (i.e., to hold or to sequester) bile acids and to increase their fecal eliminafion was subsequently shown to produce beneficial effects in lowering serum cholesterol levels. In 1973, cholestyramine was approved for fhe treatment of hypercholesterolemia ih patiehts who do hot respond to dietary modifications. Colestipol and colesevelam, which retain the key structural features required to bind bile acids, were approved in 1977 and 2000, respectively (7,15). 

Bile acid sequestrants are indicated for the treatment of hypercholesterolemia in patients who do not adequately respond to dietary modifications. They may be used either alone or in combination with HMGRIs or niacin. These combinations often can achieve a 50% reduction in plasma LDL levels. Cholestyramine, but neither colestipol nor colesevelam, also is approved for the relief of pruritus associated with partial biliary obstruction. Bile acid sequestrants should not be used to treat hypertriglyceridemias or mixed hyperlipoproteinemias in which hypertriglyceridemia is the primary concern. These compounds also are contraindicated in patients with cholelithiasis or complete biliary obstruction because of the impaired secretion of bile acids caused by these conditions. Finally, cholestyramine and colestipol are contraindicated in patients with primary biliary cirrhosis, because this can further raise serum cholesterol (7,15,21). 

A nonabsorbable strongly basic anion exchange resin which binds bile salts in the intestinal lumen, thereby removing them from the enterohepatic circulation for excretion in the feces, will relieve pruritus in patients who do not have complete biliary obstruction. When serum bile salt concentrations are measured serially at frequent intervals during cholestyramine feeding, it can be shown that concentrations reach near normal levels before pruritus stops, and when cholestyramine is withheld, high serum concentrations are reached before pruritus starts. This lag period, which may be a day or more, may represent the period of time required for concentrations of bile salts sufficient to induce pruritus to accumulate in or leave the skin (57). 

The type of pruritus occurring during pregnancy which is caused by increased concentrations of bile salts in the blood and skin is readily relieved by cholestyramine this is discussed in Section XXVIII. 

Serum lithocholate concentrations can be lowered with either neomycin or cholestyramine, as can the serum concentrations of the other bile salts if they are elevated. This is often associated with a similar decline in serum bilirubin concentrations, alkaline phosphatase activity, and BSP retention (7,95,105,106). This response has been interpreted as at least one piece of evidence that high serum bile salt concentrations, especially of lithocholate, may be injurious to the liver. In three jaundiced children with a paucity of intrahepatic bile ducts and pruritus, lowering of the serum bile salt concentrations to normal values with cholestyramine was accompanied by a return to normal of all previously abnormal liver chemistries except alkaline phosphatase, and the patients growth curves returned to normal (95). 

Cholestyramin is a basic anion exchange resin which is used to ameliorate watery diarrhea in cases of ileal dysfunction, ileal resection, and vagotomy. It is also used to relieve pruritus due to elevated serum and skin levels of bile salts in patients with intrahepatic cholestasis and to lower cholesterol levels in familial hypercholes-... 

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