Cholestyramine is a member of the bile acid sequestrant class of cholesterol lowering medications, commonly marketed as Questran powder by Par Pharmaceutical.
Cholestyramine (Questran) is indicated as an addition to diet and lifestyle change for reducing excessively high total and low density lipoprotein (LDL) cholesterol in people with primary hypercholesterolemia (high blood cholesterol not caused by another disease).
Cholestyramine (Questran) might also be useful to lower high triglyceride levels, unlike its relative colestipol. However, cholestyramine should not be used when high triglyceride levels are the biggest problem.
Cholestyramine (Questran) also shouldn't be used for secondary hypercholesterolemia, which basically means high cholesterol caused by an outside factor like badly controlled diabetes, hypothyroidism, kidney disease, obstructive liver disease, other medications or alcoholism. They don't mention smoking as a cause of secondary high cholesterol levels, but it is.
Basically, the idea is to eliminate all other sources of high cholesterol before going on cholestyramine.
Cholestyramine (Questran) works by chemically binding the bile acids produced by the gall bladder.
The gallbladder synthesizes bile acids, used by the body in digestion, from cholesterol. Under normal circumstance, bile acids are secreted into the small intestine, where they break up fat and make it small enough for the intestines to absorb it into the blood. Then, at the end of the small intestine, the bile acids are reabsorbed and circulated back to the liver for re-use.
By binding these bile acids, cholestyramine prevents cholesterol from being broken down and absorbed through the small intestine. In addition, the bile acids aren't picked back up but get excreted from the body.
This makes the gallbladder have to burn up more cholesterol in order to produce more bile acids. Basically, you get two mechanisms of action in one medication.
In clinical studies cholestyramine has been show to reduce the rate of aggression and increase the rate of regression in coronary atherosclerosis, which makes it a good medication for anyone currently suffering hardening arteries.
Like other bile acid sequestrants, it's shown up to 10.4% reductions in LDL-C levels and a 19% reduction in coronary heart deaths and non-fatal heart attacks combined.
Like every other medication out there, Cholestyramine (Questran) has never been studied in pregnant or nursing women.
However, considering that it stays in the intestines instead of being absorbed into the blood, theory says that it would be pretty safe, if it weren't for the fact that developing children need cholesterol in order to grow properly.
That being a given, it might be an option for mothers who have extreme high cholesterol problems.
Cholestyramine (Questran) has been tested on children, unlike colestipol, and is both effective and relatively safe.
The biggest problem it's ever shown in kids is the tendency to create fecal impaction. When kids have a problem with constipation, they generally try to ignore it because it's painful. Ignoring constipation leads to fecal impaction.
If your child takes this medication, watch carefully for signs of constipation, and help the child as much as possible.
To date, two children have died due to fecal impaction while taking this medication. That's not statistically significant considering the thousands of children who have had no such problem, but you still want to be on the lookout for it.
In addition, people who suffer from complete biliary obstruction, a condition where bile is not being secreted at all into the intestine, should not take Cholestyramine (Questran), nor should anyone allergic to any component of the medicine itself.
It can take a bit to find the precise amount of cholestyramine needed to produce the effect you need. Because of this, frequent cholesterol testing for both LDL-C and triglyceride levels is important to adjust the dose properly.
After a steady dose is found, these tests should be done again every so often to make sure the medication is still working correctly.
It's always put into powder form, and should always be mixed with a prescribed amount of water before taking.
Do not ever take it dry, nasty things will result.
Cholestyramine really is one of the older medications out there, and as such is marketed under many names.
You'll find it as Questran, Questran Light, Cholybar, Locholest, Locholest Light, Novo-Cholamine, Novo-Cholamine Light, PMS Cholestyramine, and Prevalite.
In addition, many of the formulas have sugar added to improve the taste, which can really make a diabetic's day interesting.
Check the ingredients on whatever version of cholestyramine powder you get in order to make sure you're not allergic or sensitive to any given ingredient.
On the bright side, Cholestyramine (Questran) comes in either packets or a canister with a measured scoop. It's really easy to read on the packaging whether you got the right medication or not. If you didn't, call your pharmacy right away. We don't play April Fool's jokes in pharmacy practice and you shouldn't take prescription medication without a doctor's orders, especially if it is a pharmacy's mistake.
Cholestyramine does all its work in the intestines and does not travel into the bloodstream.
You should start seeing LDL-C levels dropping off within a month of starting to take it regularly.
However, cholestyramine is a treatment, not a cure. If you stop taking the medication, your LDL-C and triglyceride levels will return to what they were within a month.
Like other bile acid sequestrants, cholestyramine can reduce or delay the absorption of many medications, including anticoagulants such as anisindione, dicumarol, acenocoumarol and warfarin.
It's also been known to reduce phenylbutazone, thiazide, acidic diuretics, propanolol, tetracycline, penicillin G, phenobarbitol, thyroxine and thyroid preparations, oral contraceptives, digitalis-derived medications such as digoxin, and the statin class of cholesterol medications.
In addition, if you take cholestyramine with spironolactone, you increase your risks of acidosis and hyperkaliemia, which are two unpleasant metabolic problems you want to avoid.
It's particularly important with this and any other member of the bile sequestrant family to not just stop taking it if you've got any medication you're taking along with it. If another medication of yours, say warfarin, is adjusted to work with cholestyramine and you suddenly stop taking it without adjusting the warfarin dose, all of a sudden you'll have a warfarin overdose. Overdosing on anticoagulants leads to medication induced hemophilia. Apply this same philosophy to any medication you might be taking.
Many medications don't need adjusting as long as you space the two between one and four hours apart. That gives the intestinal tract enough time to work with one before the other comes through.
However, there are a few medications that still show interactions with cholestyramine (Questran) even when spaced out, so be sure to ask your doctor or pharmacist about the particular medications you take.
The biggest side effect associated with cholestyramine is constipation.
While this is usually not the worst side effect you could suffer, it can get pretty bad in a small number of cases.
Higher dietary fiber intake, higher water and stool softeners will generally take care of the problem.
However, if it gets too bad, you may need to discontinue the medication entirely.
In addition, constipation should be avoided at all costs in patients with coronary atherosclerosis, because it can cause one of the plaques to peel off and give a heart attack.
The other most common side effects are abdominal discomfort or pain, gastrointestinal upset, flatulence, nausea and vomiting.
The dosage should gradually be increased over time to minimize these side effects, rather than being jumped to the maximum all at once.
There have been rare reports of intestinal or fecal obstruction in people taking this medication, which can lead to death.
Again, if the side effects are interfering with your ability to go about your everyday life, talk to your doctor to find a solution.
Because cholestyramine interferes with your body's ability to digest and absorb fat, it can also interfere with fat-soluble vitamins like A, D, E and K.
If you can't absorb them from the fat they're suspended in, then you may start to suffer from deficiencies of these vitamins even though you're eating a healthy diet.
Effects of severe vitamin deficiencies include an increased tendency to bleed, bone problems, red blood cell problems, and skin problems to include fingernails and skin.
If you start to feel run down or under the weather, even though you're eating right and exercising, talk to your doctor about special vitamin supplements that are made in such a way as cholestyramine can't interfere with them.
And, last but not least, if you hold cholestyramine solution in your mouth for any length of time, it might lead to discoloration, decay or erosion of your tooth enamel. Therefore, drink it all down at once and remember to brush your teeth well.
There have been several cases of prolonged overdose of cholestyramine (Questran) reported, and no serious ill effects have yet cropped up.
The main potential problem with overdose is the same potential problem with side effects, which is to say the obstruction of the gastrointestinal tract.
If abdominal pain starts up after an overdose, get the person to a hospital and tell the staff what happened.
No matter what form it comes in, always store cholestyramine between 20 and 25 degrees C (68 to 77 degrees F). Excursions are permitted between 15 and 30 degrees C (59 to 86 degrees F). This means that unless you live in the Sudan or within the Arctic Circle, you can reasonably store this medication anywhere in the house as long as it's protected from light and excess moisture.
Cholestyramine is one of the oldest and relatively safest cholesterol lowering medications on the market today.
In addition, because it's been out so long and comes from so many companies, it's relatively cheap.
cholestyramine (Questran) can often be used as part of a combination therapy regimen to lower LDL-C levels, unlike many other medications today.
However, nothing works for everybody. Learn as much as you can about all your options, and make educated decisions for your particular circumstances, health, and quality of life.
Main Research and write by Loni Ice, Editing by Donald Urquhart