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Composition:


active ingredient: Cholestyramine resin, styrene and divinylbenzene copolymer with quaternary ammonium functional groups;


1 sachet of powder contains Cholestyramine rubber 4 g;


excipients: sucrose, citric acid anhydrous, colloidal silicon dioxide, yellow sunset FCF dye (E 110), D&C yellow dye No. 10 (Quinoline yellow E 104), d&c yellow dye No. 10 aluminum lacquer 15 % (Quinoline yellow E 104), propylene glycol alginate, orange flavor containing: orange flavor, maltodextrin, acacia (gum Arabic E 414), butylhydroxytoluene (e 321).


Dosage form. Powder for oral suspension.


Basic physical and chemical properties: fine powder of whitish or yellowish color with a faint smell of Orange. There are no particles of foreign material.


Pharmacotherapeutic group.


Lipid-lowering agents. Cholestyramine. ATX code C10A C01.


Pharmacological properties.


Pharmacodynamics.


Cholestyramine is an anion exchange resin with quaternary ammonium groups based on a polystyrene polymer framework. In the form of chloride, it binds bile acids in vivo and in vitro, exchanging the chloride ion for bile acid ions.


Pharmacokinetics.


The only precursor to bile acids in the body is cholesterol. During normal digestion, bile acids are released into the intestines. The main part of bile acids is absorbed from the intestines and returned to the liver through the intestinal-hepatic circulation system. The blood serum of healthy people contains only a fairly small amount of bile acids.


Cholestyramine in the intestine binds to bile acids to form an insoluble complex, which is excreted in the faeces. Thus, some of the bile acids do not return to the liver through the intestinal-hepatic circulation system.


As a result of the loss of a significant amount of bile acids in the feces when taking Cholestyramine, there is an increased oxidation of cholesterol with the formation of bile acids, while there is a decrease in the content of beta-lipoprotein or low-density lipoprotein in blood plasma, as well as a decrease in the content of cholesterol in the blood serum. Therefore, despite the increase in cholesterol synthesis in the liver, its content in blood plasma decreases.


Clinical characteristics.


Indications.


Cholestyramine is indicated as an adjuvant therapy (as an adjuvant to diet and exercise) to reduce elevated serum cholesterol in patients with primary Hypercholesterolemia in order to reduce the risk of atherosclerotic lesions of the coronary arteries and myocardial infarction.


Cholestyramine can be used as a means to reduce high cholesterol in patients with combined hypercholesterolemia and hypertriglyceridemia, but the drug is not indicated in cases where hypertriglyceridemia is the dominant pathology.


Cholestyramine can be used for the symptomatic treatment of bile acid-induced diarrhea in patients with short bowel syndrome, as well as to relieve pruritus in cholestasis due to partial biliary tract obstruction.


Contraindications.


Cholestyramine is contraindicated in complete obstruction of the biliary tract, when bile does not enter the intestines at all.


The drug is contraindicated in case of hypersensitivity to the active substance or to other components that make up the drug.


Interactions with other drugs and other types of interactions.


Cholestyramine as an ion exchanger has a pronounced affinity not only for bile acids, but also for other anions. It is difficult to predict a priori whether the use of Cholestyramine will affect the absorption of certain drugs from the intestine. It is potentially necessary to consider the possibility of such drug interactions with Cholestyramine, unless the absence of such interactions is proven by clinical studies.


Cholestyramine may reduce the absorption of oral medications such as thyroxine, warfarin, chlortiazide (acidic), phenylbutazone, tetracycline, penicillin G, digitalis. It should be borne in mind that when Cholestyramine is discontinued, toxic phenomena caused by Digitalis preparations may develop, if the dose of the latter was increased taking into account the decrease in its absorption under the influence of Cholestyramine. Cholestyramine may also affect the pharmacokinetics of drugs that undergo intestinal-hepatic recycling, such as estrogens.


Studies have been conducted on the interaction of Cholestyramine and various HMG-CoA reductase inhibitors. Although Cholestyramine reduces the bioavailability of these inhibitors, the clinical effects of cholesterol reduction with HMG-CoA reductase inhibitors and Cholestyramine appear to be additive.


It should be borne in mind that Cholestyramine can bind other drugs. Therefore, other medications should be taken no later than 1 hour before taking Cholestyramine and no earlier than 4-6 hours (and preferably even later) after taking Cholestyramine.


Application features.


The drug should not be used in dry form. The drug is intended only for use in the form of an aqueous suspension.


Before starting treatment with Cholestyramine, you should try other means to reduce cholesterol (diet therapy, weight loss). It is also necessary to treat major diseases such as hypothyroidism, diabetes mellitus, nephrotic syndrome, dysproteinemia, obstructive liver diseases that can cause hypercholesterolemia. It is also necessary to check whether the use of other medications leads to an increase in the content of low-density lipoprotein cholesterol. When using Cholestyramine, a positive trend towards lowering cholesterol levels is noted already during the first month of treatment. Taking the drug can be continued to consolidate the effect obtained.


There is a possibility that the use of Cholestyramine in the form of chloride can lead to hyperchloremic acidosis, which is especially likely in younger people, where the relative dose of the drug will be higher.


The use of Cholestyramine can lead to constipation or worsen pre-existing constipation. In this case, you should reduce the dose of the drug or even cancel the drug. It is also possible to exacerbate hemorrhoids due to constipation. In any case, it is advisable not to bring the patient to this state, especially in the presence of clinical symptoms of coronary artery damage.


Cholestyramine can potentially cause steatorrhea or worsen pre-existing steatorrhea. In such cases, it may be necessary to reduce the dose of the drug.


Effect on vitamin absorption: since Cholestyramine binds bile acids, it can interfere with the absorption of fat-soluble vitamins A, D and K. with prolonged use of Cholestyramine, parenteral forms of a mixture of vitamins A and D should be used. 


Vitamin K deficiency that develops with prolonged use of Cholestyramine can lead to hypoprothrombinemia and an increased risk of bleeding. With the development of such phenomena, parenteral forms of vitamin K1 should be used, and relapse prevention is also possible with oral administration of vitamin K1.


With prolonged use of Cholestyramine, it is also possible to reduce the content of folate in the blood serum or red blood cells. In such cases, it is necessary to take medications containing folic acid.


Laboratory tests. In the first months of using Cholestyramine, regular monitoring of serum cholesterol is required. Periodic monitoring is also necessary in the future. Periodically, it is necessary to monitor the content of triglycerides in the blood serum. 

Use in patients over 6 years of age.


Adequate studies on the effectiveness of Cholestyramine in people of different ages have not been conducted. However, in the elderly, gastrointestinal side effects are more likely.


Excipients.


The drug contains sucrose. If you have an established intolerance to certain sugars, consult your doctor before taking this medicine.


The drug contains the dye yellow sunset FCF (E 110), which can cause allergic reactions.


Use during pregnancy or lactation.


Since Cholestyramine is not absorbed in the intestine, theoretically it cannot negatively affect the fetus when taken at the recommended doses. However, no controlled clinical studies have been conducted on the use of the drug in pregnant women. In addition, Cholestyramine can interfere with the absorption of fat-soluble vitamins in the intestines, which can negatively affect fetal development.


The drug should be used with caution in women who are breast-feeding, as it can interfere with the absorption of vitamins in the intestines, which can lead to poor nutrition of the child.


Thus, the use of the drug in pregnant women and women who are breastfeeding is possible only in cases where the potential benefit of using the drug exceeds the potential risk to the fetus or child.


Ability to influence the reaction rate when driving vehicles or other mechanisms.


There are no data available, but you should consider the possibility of developing adverse reactions from the nervous system, such as dizziness, drowsiness, loss of consciousness.


Dosage and administration.


Cholestyramine should be administered orally.


In order to minimize possible side effects from the gastrointestinal tract, it is advisable to start therapy with one dose of the drug 1 time a day. Then, after 1-2 days, the dosage can be increased.


It is important to motivate the patient to follow the established treatment regimen, despite the side effects that occur from the gastrointestinal tract. For successful treatment, monitoring compliance with the drug regimen plays an important role.


The recommended dose for adults is 4 g of Cholestyramine 1 to 6 times a day. The dosage can be changed to best meet the individual needs of the patient.


The drug should not be taken in dry form, it is intended only for use in the form of an aqueous suspension.


Preparation of the drug for administration: the color of the drug may vary from series to series, which does not affect the quality of the drug itself.


To prepare the suspension, place the contents of 1 sachet in a glass with 120-180 ml of water or a drink that does not contain carbon dioxide (milk or fruit juice). After 1 minute, mix the powder intensively in the liquid. The powder can also be stirred into soup or juice with Pulp squeezed from fruit (apples or pineapples).


Children.


The safety and efficacy of Cholestyramine in children have not been established.


Overdose.


One case of overdose was described in a patient who took the drug for several weeks at a dose that was 150% of the maximum recommended daily dose. No significant phenomena were observed. The main consequence of overdose may be a violation of the patency of the gastrointestinal tract. The presence of such obstruction, the degree of its severity and determines the necessary symptomatic therapy.


Adverse reactions.


Most often, constipation is noted when using Cholestyramine, especially with a high dose of the drug and in elderly patients (from 60 years). In most cases, these side effects are removed by conventional therapy in such cases. In some cases, it may be necessary to temporarily reduce the dose or discontinue the drug.


Less often there are such side effects as a feeling of stretching of the stomach, flatulence, bloating, nausea, vomiting, diarrhea, steatorrhea, anorexia, heartburn, skin rashes, irritation of the skin, tongue, perianal zone, a tendency to bleeding due to hypoprothrombinemia (lack of vitamin K), deterioration of vision in the dark due to a lack of vitamin A, hyperchloremic acidosis in children, osteoporosis, manifestations of vitamin D deficiency.


Sometimes there was a compaction of the contents of the biliary tract, including compaction of the contents of the gallbladder, which may be a manifestation of liver disease, and is not associated with the use of the drug.


One patient had attacks of biliary colic at each dose of the drug. In another case, an acute abdominal symptom complex was noted, and the presence of a paste-like Mass was detected radiographically in the transverse colon.


Other adverse reactions have also been observed, not all of them can be directly caused by taking Cholestyramine. These are gastrointestinal and rectal bleeding, black bowel movements, hemorrhoidal bleeding, duodenal ulcer bleeding, dysphagia, hiccups, belching, rectal pain, exacerbation of peptic ulcer disease, sour taste sensation, exacerbation of pancreatitis, diverticulitis.


Changes in laboratory parameters: impaired liver function.


Hematological changes: changes in the value of prothrombin time (decrease or increase), ecchymosis, anemia, gum bleeding.


Musculoskeletal disorders: back pain, muscle pain, joint pain, arthritis.


Neurological changes: headache, dizziness, anxiety, increased fatigue, tinnitus, loss of consciousness, drowsiness, ishioneuralgia, paresthesia.


From the kidneys: hematuria, dysuria, burnt smell of urine, diuresis (increased urinary excretion).


From the side of the visual organs: uveitis.


Hypersensitivity reactions: urticaria, bronchial asthma, difficulty breathing, wheezing.


Other changes: decreased or increased body weight, increased libido, glandular edema, edema, tooth decay.

Tags: Cholestyramine