Micronized Colestipol Hydrochloride - Indication, Dosage, Side Effects, Contraindications, Warnings, and Precautions

Overview:

Micronized Colestipol hydrochloride tablets contain one gram of Micronized Colestipol hydrochloride as the active ingredient, which is used to lower lipids when taken orally. FDA (Food and Drug Administration) approved Colestipol on May 25th, 2017. Colestipol is a light yellow, water-insoluble resin made of diethylenetriamine and 1-chloro-2,3-epoxypropane, functioning as a basic anion-exchange copolymer. Approximately one out of five amine nitrogens in Colestipol are protonated in the chloride form. These tablets are light yellow, tasteless, and odorless, composed of inactive ingredients such as cellulose acetate phthalate, glyceryl triacetate, carnauba wax, hypromellose, magnesium stearate, povidone, and silicon dioxide.

Available Doses and Dosage Forms:

Micronized Colestipol hydrochloride granules come in different packaging options:

• Boxes containing 30 or 90 foil packets.

• Bottles containing 300 or 500 grams of granules, with a scoop.

• Each packet or scoop contains five grams of Micronized Colestipol hydrochloride.

Flavored Micronized Colestipol hydrochloride granules are available in:

• Boxes containing 60 foil packets.

• Bottles containing 450 grams of granules, which is approximately 60 doses, with a scoop.

• Each packet or scoop contains approximately 7.5 grams of flavored Micronized Colestipol hydrochloride, which includes five grams of the active ingredient Colestipol hydrochloride.

• Remember to store these medications at room temperature between 20°C (degrees Celsius) to 25°C (68°F (degrees Fahrenheit) to 77°F).

For Patients:

What Are the Causes of High Cholesterol Levels?

• Drinking too much alcohol can raise the total cholesterol levels.

• Unhealthy cholesterol levels are more common in people over 40 because as they age, the liver becomes less efficient at removing LDL (low-density lipoprotein) cholesterol.

• Eating a lot of foods high in saturated fats, like fatty meats and dairy products, can increase bad LDL cholesterol levels. It is recommended that no more than 10 percent of the daily calories should come from saturated fats.

• Smoking can lower HDL (high-density lipoprotein) cholesterol, especially in women, and increase LDL cholesterol levels.

What Is the Dosage of Micronized Colestipol Hydrochloride?

Each dose of Micronized Colestipol hydrochloride granules contains five grams of the active ingredient, while each dose of flavored Micronized Colestipol hydrochloride granules contains approximately 7.5 grams, both containing the same amount of the active ingredient. For adults, the recommended daily dose is one to six packets or scoopfuls, taken once or divided throughout the day. Treatment usually starts with one dose once or twice a day, with the option to increase by one dose per day every one or two months until the desired effect is reached.

What Are the Things to Inform the Doctor Before Taking the Micronized Colestipol Hydrochloride?

• Let the doctor and pharmacist know if the person is allergic to Colestipol or any other medications or if the person has any allergies to the ingredients in Colestipol.

• Tell them about all the medications, vitamins, supplements, and herbal products they are taking or planning to take, including prescription and over-the-counter drugs. This includes specific medications like Amiodarone, antibiotics, blood thinners, heart medications, and others. The doctor may need to adjust the doses or monitor the person closely for side effects.

• Inform the doctor if the person has a history of unusual bleeding, thyroid issues, heart or intestinal problems, or if a person has hemorrhoids.

• If a person takes Gemfibrozil, make sure to take it either two hours before or two hours after taking Colestipol.

• If the person is pregnant, planning to become pregnant, or breastfeeding, inform the doctor. If they become pregnant while taking Colestipol, contact the doctor immediately.

How Is Micronized Colestipol Hydrochloride Administered?

• Other medications should be taken at least one hour before or four hours after taking Micronized Colestipol hydrochloride or flavored Micronized Colestipol hydrochloride to avoid any potential interference with their absorption.

• Before starting Micronized Colestipol hydrochloride or flavored Micronized Colestipol hydrochloride, identify the type of high cholesterol based on NCEP (National Center for Environmental Predictions) guidelines. Try changing the diet and losing weight first. Check the initial levels of total cholesterol, LDL cholesterol, and triglycerides in the blood.

• During Micronized Colestipol hydrochloride or flavored micronized Colestipol Hydrochloride use, monitor the patient closely, including checking cholesterol and triglyceride levels regularly.

• If cholesterol levels do not improve as expected, check if the patient is following the diet and taking the medication correctly. If they are, consider trying a different treatment. If triglyceride levels rise significantly, consider reducing the dose, stopping the medication, or trying a different treatment.

What Are the Side Effects of Micronized Colestipol Hydrochloride?

1. Gastrointestinal Side Effects: The most frequent problems associated with these medications affect the stomach and intestines. Doctors recommend gradually increasing the dosage to minimize stomach discomfort while still achieving the desired cholesterol-lowering effect. Constipation is the primary complaint and can sometimes be severe. Most cases are mild and short-lived, and can be managed with increased fluid intake and more fiber in the diet. Stool softeners may be necessary in some cases. Occasionally, patients may need to reduce their dosage or stop taking the medication altogether. These medications can also worsen hemorrhoids. Less common gastrointestinal issues include abdominal discomfort (pain and cramping), intestinal gas (bloating and flatulence), indigestion, heartburn, diarrhea, loose stools, nausea, and vomiting. Bleeding hemorrhoids and blood in the stool are reported infrequently. Rarely peptic ulcers, gallbladder inflammation, and gallstones may occur, but these are not necessarily caused by the medication.

2. Liver Enzyme Changes: Some patients may experience temporary increases in certain liver enzymes while taking these medications.

3. Cardiovascular: Chest pain, angina (chest pain due to reduced blood flow to the heart), and rapid heartbeat have been reported occasionally.

4. Hypersensitivity: Rash is reported infrequently. Urticaria (hives - causes skin infection with itchy welts) and dermatitis (swelling and irritation of the skin) are rare in patients taking these medications.

5. Musculoskeletal: Patients may experience muscle and joint pain, arthritis, and backache.

6. Neurological: Headaches, including migraine and sinus headaches, have been reported. Other occasional complaints include dizziness, feeling lightheaded, and difficulty sleeping (insomnia).

7. Miscellaneous: Some patients may experience loss of appetite (anorexia), fatigue, weakness, shortness of breath, and swelling in the hands or feet. These symptoms are infrequently reported.

Dietary Considerations:

• Mixing With Fluids: It is important to mix Micronized Colestipol hydrochloride and flavored Micronized Colestipol hydrochloride with water or another liquid before taking them to prevent any discomfort in the throat or lungs.

• With Beverages: Mix the prescribed amount of Micronized Colestipol hydrochloride or flavored Micronized Colestipol hydrochloride with at least three ounces of water or favorite beverage. Using thick or pulpy juices might help with consistency. Stir the mixture well until the medication is completely mixed. Micronized Colestipol hydrochloride and flavored Micronized Colestipol hydrochloride would not dissolve in the liquid. People can also mix them with carbonated beverages, but this might cause some stomach discomfort. Make sure to rinse the glass with a little more beverage to ensure complete intake of the medication. They have taken all the medication.

• With Cereals, Soups, and Fruits: A person can mix Micronized Colestipol hydrochloride and flavored Micronized Colestipol hydrochloride with milk in hot or regular breakfast cereals or even add them to soups that have a lot of liquid. They can also be added to pulpy fruits like crushed pineapple, pears, peaches, or fruit cocktails.

Missed Dose:

If a person misses a dose, they should take it as soon as they remember. But if it is almost time for the next dose, just skip the missed one and stick to the usual schedule. Do not take extra medication to make up for the missed dose.

Overdose:

Overdosing with Micronized Colestipol hydrochloride has not been reported, but if it does happen, the main risk would be a blockage in the digestive system. The treatment needed would depend on where the blockage is, how severe it is, and whether the person's gut is functioning normally.

Storage:

• Keep this medication in its original container, tightly closed, and out of reach of children.

• Store it at room temperature, away from excessive heat and moisture (do not keep it in the bathroom).

• Store all medications where children cannot see or reach them, as some containers are easy for them to open.

• To prevent accidental ingestion by children, always use safety caps and store medications in a secure place.

• Dispose of any unused medication properly to prevent accidental consumption by pets, children, or others.

• Do not flush this medication down the toilet. Instead, check if the community has a medicine take-back program. If not, consult the pharmacist or local waste management for safe disposal options.

For Doctors:

Indication:

• When choosing drugs for long-term use, it is important to carefully consider their purpose and any reasons why they might not be suitable.

• Micronized Colestipol hydrochloride granules and Flavoured Micronized Colestipol hydrochloride granules are meant to be used alongside changes in diet to help lower high levels of bad cholesterol (LDL) in people with a condition called primary hypercholesterolemia.

• Generally, these drugs do not have a significant effect on triglyceride levels, but in some cases, they might increase them.

• If a person is at high risk for heart disease because of high cholesterol, these drugs can be part of the treatment plan, but they should not be the only thing to do. They should also focus on changing their diet, as recommended by the NCEP guidelines.

• Before starting on these drugs, it is recommended to try intensive dietary therapy and counseling for at least six months. In some cases, if the LDL cholesterol is very high or if the patient already has heart disease, they might not have to wait that long.

• According to guidelines, the main goal of treatment is to lower bad cholesterol (LDL-C), and doctors should use LDL-C levels to decide if the treatment is working. If LDL-C levels are not available, total cholesterol levels can be used instead.

Dose:

Each dose of Colestipol hydrochloride granules contains five grams of the medication. Each dose of flavored Colestipol hydrochloride granules contains 7.5 grams of the granules, which contains five grams of Colestipol hydrochloride.

Dosing Considerations:

• For Pediatric Patients With Dyslipidemias: The dosage for Colestipol hydrochloride granules has not been established, but doses of 10 to 20 grams daily or 500 milligrams per kilogram daily, split into two to four doses, have been used. Lower doses, such as 125 to 250 milligrams per kilogram daily, have been used in some children with slightly elevated cholesterol levels after dietary changes.

• For Adults With Dyslipidemias: The initial dosage of Colestipol hydrochloride tablets is two grams once or twice daily, with the option to increase by two grams once or twice daily every one to two months. The typical daily dosage ranges from two to 16 grams, taken once or divided into multiple doses. If the desired effect is not achieved with the usual dosage and acceptable side effects, combined therapy or alternative treatments may be considered. If triglyceride levels rise significantly, adjust dosage or combine with other treatments.

• For Adults With Preexisting Constipation: Start with five grams of Colestipol hydrochloride granules once daily for five to seven days, then increase to five grams twice daily. Monitor constipation and cholesterol levels every four to six weeks, adjusting dosage as needed by increasing one dose per day monthly while monitoring cholesterol levels. If constipation worsens or the desired effect is not achieved with acceptable side effects, consider combined therapy or alternative treatments.

• For Patients With Heterozygous Familial Hypercholesterolemia: Use 30 grams of Colestipol hydrochloride granules daily in combination with Niacin.

What Are the Pharmacological Aspects of Micronized Colestipol Hydrochloride?

• Pharmacodynamics: Treatment with Colestipol hydrochloride typically leads to a decrease in serum cholesterol levels within one month. Discontinuation of treatment usually results in cholesterol levels returning to baseline within a month. Colestipol hydrochloride increases levels of lipoprotein LpAI, which is associated with removing cholesterol from cells and may have a protective effect against heart disease. When used alone, Colestipol hydrochloride may not achieve optimal cholesterol levels in some patients with familial hypercholesterolemia. Combining it with nicotinic acid has been shown to further reduce cholesterol and triglyceride levels while increasing HDL (high-density lipoprotein) cholesterol, potentially normalizing lipid values in these patients. Intensive lipid-lowering therapy, including Colestipol hydrochloride, has been shown to slow down or reverse the progression of artery blockages in patients with or at risk for coronary artery disease, compared to conventional measures like diet alone.

• Mechanism of Action: Colestipol hydrochloride binds to bile acids in the intestine, forming a complex that is then excreted in feces. This action reduces the reabsorption of bile acids, disrupting the enterohepatic circulation and preventing their recycling. By increasing the fecal loss of bile acids, Colestipol hydrochloride prompts the body to produce more bile acids from cholesterol. This process leads to increased uptake of LDL (low-density lipoprotein) cholesterol by the liver, resulting in lower LDL cholesterol levels in the bloodstream.

• Pharmacokinetics: Colestipol hydrochloride is hydrophilic (water-loving) but almost completely insoluble in water. It is not broken down by digestive enzymes and is not absorbed into the bloodstream. Only a tiny fraction (less than 0.17 percent) of an oral dose is excreted in urine.

What Are the Contraindications of Micronized Colestipol Hydrochloride?

Micronized Colestipol hydrochloride granules and flavored Micronized Colestipol hydrochloride granules should not be used by people who have had allergic reactions to any of the ingredients in these medications.

Warnings and Precautions:

• Do not take Micronized Colestipol hydrochloride or flavored Micronized Colestipol hydrochloride dry. Always mix them with water or another liquid before swallowing to avoid problems in the throat or lungs.

• Before starting these medications, doctors need to check if there are other reasons for high cholesterol, like diabetes, thyroid issues, or liver problems. They also need to check cholesterol levels.

• For some people with specific cholesterol levels, doctors can estimate LDL cholesterol using a formula. However, for higher triglyceride levels, a different method is needed.

• These medications can affect how the body absorbs certain vitamins like folic acid, as well as vitamins A, D, and K.

• Long-term use of these medications might lead to a lack of vitamin K, which can increase the risk of bleeding. This can be treated with vitamin K supplements.

• Doctors need to regularly check cholesterol and triglyceride levels to see how well the medication is working.

• These medications can cause or worsen constipation. Doctors should start with a low dose and gradually increase it to avoid problems.

• There is a small chance of developing thyroid problems or acidosis with long-term use of these medications.

Drug Interactions of Micronized Colestipol Hydrochloride

Colestipol hydrochloride is a type of resin that can bind to certain drugs, affecting their absorption. To minimize this interaction, it is recommended to take other medications at least one hour before or four hours after taking Micronized Colestipol hydrochloride or flavored Micronized Colestipol hydrochloride.

Specific Medications:

1. Taking Colestipol hydrochloride with Propranolol might slightly delay its absorption, but it does not affect the overall amount absorbed.

2. Chlorothiazide, Tetracycline, Furosemide, Penicillin G, Hydrochlorothiazide, and Gemfibrozil, taking these medications with Colestipol hydrochloride significantly reduces their absorption.

3. No significant interactions were found with Aspirin, Clindamycin, Clofibrate, Methyldopa, Nicotinic acid (Niacin), Tolbutamide, Phenytoin, or Warfarin.

4. There is uncertainty about the effect of Colestipol hydrochloride on the availability of these drugs, so caution is needed.

5. Phosphate supplements and Hydrocortisone may also have reduced absorption when taken with bile acid-binding resins like Colestipol hydrochloride.

6. Colestipol hydrochloride can reduce exposure to Mycophenolic acid, potentially affecting the effectiveness of Mycophenolate mofetil.

Specific Considerations:

1. Pregnancy: Colestipol hydrochloride is not absorbed much by the body, so it is unlikely to harm the fetus when taken during pregnancy in recommended doses. However, there have not been enough studies on pregnant women. Also, because it can interfere with the absorption of certain vitamins, there might be risks even with vitamin supplements. Doctors need to consider the potential benefits and risks before prescribing it to pregnant women or those planning to become pregnant.

2. Breastfeeding: It is important to be cautious when using Micronized Colestipol hydrochloride while breastfeeding. Since these medications might affect how vitamins are absorbed, it could impact nursing infants.

3. Pediatric Use: It has not been proven if Micronized Colestipol hydrochloride is safe or effective for children because there have not been enough studies in this population.