Pocket Drug Guide

Posts Tagged ‘HDL’

Zocor Heart- Pro

Simvastatin

1 What the medicine is for

Zocor Heart-Pro is a medicine which is used to reduce the risk of a first heart attack in people who have a moderate risk of coronary heart disease (heart disease caused by a build up of plaques in the coronary arteries). Moderate risk means that your chances of having a heart attack in the next 10 years are at least 1 in 10 (10%). The tablets contain simvastatin, which belongs to a group of medicines known as statins. Statins significantly reduce the amount of cholesterol in your blood.

You will need to take these tablets regularly for a long period of time to get the maximum benefit from them.

Who is at moderate risk of coronary heart disease?

■  You are likely to be at moderate risk if you are a man aged 55 or over.

■  You are also likely to be at moderate risk if you are a man aged between 45 and 54 or a woman aged 55 or over and you answer yes to one or more of the questions below:

■  Do you have a parent, brother or sister who suffered a heart attack younger than 55 for men or 65 for women?

■  Do you smoke or have you smoked within the last 5 years?

■  Are you overweight?

This means you have a body mass index (BMI) over 25kg/m² (this is your weight in kilos divided by your height in metres squared), OR

■  Men – your waist is greater than 40 inches or 102cm OR

■  Women -your waist is greater than 35 inches or 88cm

Your pharmacist can help you answer this question if you are in any doubt.

■  Are you of South Asian origin (from the Indian subcontinent that includes Bangladesh, India, Pakistan or Sri Lanka)?

■  In addition, if you take no physical exercise other than normal daily activities, your risk of heart attack is further increased.

How does the medicine work?

Zocor Heart-Pro works by reducing the level of LDL (bad) cholesterol and fatty substances called triglycerides in your blood and raises HDL (good) cholesterol.

LDL (bad) cholesterol clogs your coronary arteries.

HDL (good) cholesterol helps to protect against heart disease.

How LDL (bad) Cholesterol can cause a heart attack

If too much cholesterol in your blood builds up in the walls of the coronary arteries, then plaques will form. This leads to narrowing of the coronary arteries, just like hard water furs up a water pipe. Heart attacks can then happen when a blood clot forms in a narrowed coronary artery.

How this medicine can help reduce the likelihood of a heart attack

By taking these tablets you can significantly reduce LDL (bad) cholesterol levels and help reduce the build up of artery-narrowing plaques.

2 Before taking this medicine

This medicine is suitable for most adults, but a few people should not use it. If you are in any doubt, talk to your doctor or pharmacist.

Do not use this medicine.

■  If you have ever had a bad reaction to statins or any of the ingredients in this medicine.

■  If you have liver disease or have been told that you have abnormal liver function blood tests.

■  If you are already taking prescription drugs to lower your cholesterol (such as gemfibrozil, bezafibrate).

■  If you are pregnant, planning to become pregnant or think you may be pregnant, or if you are breast-feeding.

■  If you discover you are pregnant while taking Zocor Heart-Pro. In this case you should stop taking the tablets immediately and contact your doctor.

■  If you have had muscle problems in the past after taking a cholesterol lowering medicine.

■  If you are taking any of the following medicines:

■  Oral antifungal medicines (drugs taken by mouth which are used to treat fungal infections such as itraconazole or ketoconazole).

Erythromyrin, Telithromycin and Clarithromyrin (these are a type of antibiotic medicine).

■  Protease inhibitors (drugs used to treat HIV infections such as indinavir, nelfinavir, ritonavir or saquinavir). Nefazodone (a drug used to treat depression).

If any of these apply to you, get advice from a doctor or pharmacist without using Zocor Heart-Pro.

Talk to your doctor or pharmacist before taking this medicine.

■  If you have an under active thyroid gland (hypothyroidism).

■  If you have kidney problems.

■  If you have a family history of muscle disorders.

■  If you already have angina or have had a heart attack.

■  If you have diabetes.

■  If you have had a stroke.

■  If you have disease of the arteries of your legs or neck (peripheral vascular disease).

■  If you have inherited very high blood cholesterol levels.

■  If you have high blood pressure.

■  If you are aged over 70.

■  If you drink more than 4 units of alcohol a day (for men) or 3 units a day (for women). One unit is Yi pint of lager, a small glass of wine or one short.

■  If you eat grapefruit or drink grapefruit juice.

■  If you are taking any other medicines, including:

■  Anti-coagulants (drugs that thin the blood, such as warfarin).

■  High doses of niacin or nicotinic acid (more than 1000 mg a day) for poor blood flow to the hands and feet.

■  Cidosporin (an immunosuppressant medicine).

■ Danazol (a steroid often used to treat endometriosis).

■ Fusidic acid (an antibiotic used to treat bacterial infections).

If you are not sure about any of the medicines you are taking, show the bottle or pack to your pharmacist.

■  If your doctor prescribes a new medicine while you are taking this medicine, you should mention that you are taking Zocor Heart-Pro.

If any of these bullets apply to you now or in the past, talk to a doctor or pharmacist.

If you have your cholesterol levels checked and you find that you have a fasting LDL cholesterol measurement greater than 5.5 mmol/l, you should talk to your doctor because you may need more than Zocor Heart-Pro to reduce your cholesterol levels.

If you are pregnant or breast-feeding

■  Do not take this medicine if you are pregnant, think you may be pregnant, trying to become pregnant or breast-feeding.

Some of the ingredients can cause problems

■  This product contains lactose. If you have been told by your doctor that you have an intolerance to some sugars, contact your doctor before taking this medicine.

Special warnings about this medicine

■  This medicine can cause dizziness. If affected, do not drive or operate machinery.

■  Do not drink grapefruit juice while you are taking these tablets.

3 How to take this medicine

Check the table below to see how much medicine to take.

■  For oral use only.

■  Do not use more than the stated dose shown in the table.

■  Do not give to children.

■  Swallow the tablet whole with a drink of water.

■  Zocor Heart-Pro should betaken regularly and on a long term basis in order to gain the full benefits of treatment.

Children (under 18 years):

This medicine is not recommended for children under 18 years of age.

Adults and the elderly:

Age                                 Dose

Adults and the elderly.   Take one tablet in the evening.

■  Do not take more than one tablet in any 24 hour period. ■  Ask your doctor or pharmacist if you are not sure about anything.

Special warnings whilst taking Zocor Heart-Pro

■  Very rarely these tablets can affect the muscles. Symptoms of this are generalised muscle pain, tenderness or weakness unless clearly related to the flu, unaccustomed exercise or recent injury or strains. If you develop these symptoms you should stop taking your tablets immediately and contact your doctor.

■  The chances of getting the muscle disorder mentioned above are greater if you drink grapefruit juice, have kidney problems or are taking tidosporin, danazol or prescription drugs to lower your cholesterol. If you are in any doubt whether to take the medicine or whether any symptoms you have are related to the medicine you should talk to your doctor or pharmacist.

■  if you are going into hospital for major surgery, you should tell your doctor you are taking these tablets, as you will need to stop taking them a few days beforehand.

■  if your cholesterol is checked whilst you are taking these tablets and your fasting LDL-cholesterol is above 5.5 mmol/lyou should talk to your doctor as it may mean that you need more than 10 mg of Zocor Heart-Pro to reduce your cholesterol.

If anyone has too much of the medicine

If anyone has taken too many Zocor Heart-Pro tablets, contact a doctor or your nearest Accident and Emergency Department (Casualty) taking this post and pack with you.

If you forget to take the medicine

You should only take this medicine as required following the dosage instructions above carefully. If you forget to take a dose, take one tablet the next evening you remember. Do not take a double dose to make up.

4 Possible side-effects

Zocor Heart-Pro tablets can have side-effects, like all medicines, although these don’t affect everyone and are usually mild.

If you experience any of the following, stop using the medicine and seek immediate medical help:

■  Allergic reactions such as swelling of the face or neck, muscle and joint pains, joint and blood vessel inflammation, itchy, lumpy rash (hives, nettle rash), a high temperature, sensitivity to light, flushing, difficulty in breathing or tiredness.

■  Muscle aches and pains, cramps, tenderness or weakness which can be severe (see section 3 Special warnings while you are taking Zocor Heart-Pro).

■  Yellowing of the skin or the whites of the eyes, dark coloured urine. This may mean you have a problem with your liver.

■  Abdominal pain felt just behind the ribs and spreading through to your back which may be due to pancreatitis (inflammation of the pancreas).

If you experience any of the following stop using the medicine and talk to your doctor:

■  Tiredness, faintness or breathlessness that may be due to anaemia (not enough red blood cells).

■  Tingling and numbness, dizziness, painful heavy pins and needles.

■  Rash, itching, hair loss.

■  Abnormal blood test results for liver or muscle function.

Other effects which occur are listed below:

■  Commonly stomach pain, wind, constipation, weakness, indigestion and headache.

■  Diarrhoea, feeling sick or being sick.

If you experience any side-effects not included in this leaflet or are not sure about anything, talk to your doctor or pharmacist.

5 Storing this medicine

Keep the product out of the reach and sight of children.

Do not store above 30°C.

Do not put them in another container as they might get mixed up.

Do not use your medicine if the pack is damaged, or after the expiry date on the packaging.

6 Further information

What’s in this medicine?

The active ingredient in Zocor Heart-Pro is: 10 mg simvastatin.

Other ingredients are: Ascorbic acid (E300), Butylated hydroxyanisole (E320), Citric acid monohydrate (E330), Lactose,

Magnesium stearate (E572), Microcrystalline cellulose (E460), Pregelatinised maize starch, Hydroxypropylcellulose (E463),

Methylhydroxy-propylcellulose (E464), Talc (E553b), Titanium dioxide (E171), Red iron oxide (E172), Yellow iron oxide (E172).

What the medicine looks like

Zocor Heart-Pro are peach coloured, oval shaped film coated tablets marked “MSD-735″. They are available in packs of

28 tablets.

7 What you can do to help reduce your risk of heart attack

At the same time as taking Zocor Heart-Pro tablets, try to reduce your risk of coronary heart disease by doing the following:

■  Stop smoking – there is strong evidence to link cigarette smoking with heart disease. The risks increase with the number of cigarettes you smoke each day, but risks still exist even if you smoke as little as five a day. It is better to stop smoking altogether rather than just cut down on how much you smoke. Your pharmacist can advise you on a suitable programme to help you stop smoking.

■  Eat a healthy diet – this will not only help towards preventing coronary heart disease, but has also been shown to reduce the risk of stroke and a number of cancers. Try to increase the amount of fruit and vegetables in your diet and reduce the amount of sugar, salt and fat.

■  Lose weight – being overweight can cause a rise in your blood pressure, increase your risk of developing diabetes and increase the risk of developing heart disease due to high cholesterol levels. Try to change your diet as described above and take more exercise.

■  Exercise – a brisk walk to the shops can help. Swimming is a good all round exercise that you could do as it is something you can gradually build up without overdoing it to start with. You could try adding the following to your daily routine: vigorous housework, walk upstairs more often and gardening.

If you would like to receive other advice and information on a healthy lifestyle and reducing your risk of a heart attack, register on the Healthy Heart Programme. This is a free on line service designed to help you understand your heart attack risk, lower it and keep it low.

 

 

Lipantil Micro 67 mg capsules

(Fenofibrate)

1. WHAT LIPANTIL MICRO IS AND WHAT IT IS USED FOR

Lipantil Micro 67 belongs to a group of medicines known as fibrates. These alter the levels of lipids or fats in the blood. Lipantil Micro is given to reduce the levels of cholesterol and triglycerides (types of fat) in the blood, when a low-fat diet and other measures (such as weight reduction or exercise) have failed.

Lipantil Micro can often also increase the amount of a “good” type of cholesterol, called HDL or high density lipoprotein cholesterol.

It is always essential to continue a low-fat diet during treatment with Lipantil Micro.

2.  BEFORE YOU TAKE LIPANTIL MICRO

Do not take Lipantil Micro if:

•  You are allergic (hypersensitive) to fenofibrate, or any of the other ingredients of Lipantil Micro 67 mg.

•   You suffer from liver or kidney disease or gallbladder disease.

•   Sunlight or UV light have caused an allergic reaction (photoallergy) or skin damage while you were taking fibrates or an anti-inflammatory drug called ketoprofen in the past.

•   You are pregnant, breast-feeding, or planning to get pregnant.

•  You suffer from pancreatitis (inflammation of the pancreas leading to abdominal pain) unless it is caused by high levels of fat in the blood (hypertriglyceridemia).

Take special care with Lipantil Micro

Tell your doctor before you start to take this medicine:

•  If you have any kidney problems.

•    If you suffer from an under active thyroid gland (hypothyroidism).

•  If you have diabetes, especially Type 2 diabetes, that is not well controlled.

•  If you have liver problems.

•  If you have problems with certain proteins in your blood

•  If you have an alcohol problem.

•  You are taking other medicines.

•  If you or your family have had muscle problems

•  If you are over 70 years of age

(some of the above conditions can lead to high levels of lipids in your blood and need to be corrected before you start therapy with fenofibrate).

Your doctor might want to test your blood or urine to check if Lipantil Micro is working properly and also if your kidneys, muscles and liver are working properly.

Important advice regarding muscle effects:

Contact your doctor quickly if you experience unexplained muscle pain, tenderness or weakness. This is because on rare occasions, there is a risk of muscle problems which may be serious, including muscle breakdown which can cause kidney damage. Your doctor may perform a blood test to check the condition of your muscles before and after starting treatment.

The risk of muscle breakdown is greater in certain patients. Tell your doctor if any of the following applies to you:

•  You have any kidney problems.

•  You have an under active thyroid.

•  You often drink large amounts of alcohol.

•  You have ever had muscle problems during treatment with

cholesterol lowering medicines called “statins” (such as simvastatin, atorvastatin, pravastatin, rosuvastatin or fluvastatin) or fibrates (such as fenofibrate, bezafibrate or gemfibrozil).

•  You or close family members have a hereditary muscle disorder.

The risk of muscle problems can be greater if Lipantil Micro is taken with cholesterol lowering medicines called “statins” (such as simvastatin, atorvastatin, pravastatin, rosuvastatin, fluvastatin). Tell your doctor if you are taking any of these medicines.

Taking other medicines

Please tell your doctor if you are taking or have recently taken any other medicines, including medicines obtained without a prescription.

In particular please let your doctor know if you already take:

•  Anticoagulants to thin your blood (for example, warfarin).

•  Other drugs to control lipid (fat) levels in the blood (for example, drugs known as “statins” or “fibrates”). Taking a “statin” (e.g. simvastatin, atorvastatin) at the same time as Lipantil Micro can increase the risk of muscle problems.

•  Ciclosporin (an immunosuppressant).

Pregnancy and breast-feeding Pregnancy

Tell your doctor if you are, you think you might be or are planning to become pregnant. Lipantil Micro must not be taken if you are pregnant.

Breast-feeding

You must not use Lipantil Micro if you are breast-feeding or if you are planning to breastfeed your baby.

Driving and using machines

This medicine should not affect your ability to drive or use machines.

Important information about some of the ingredients of Lipantil Micro

This medicine contains lactose which is a type of sugar. If you have been told by your doctor that you  have a intolerance to some sugars, contact your doctor before taking this medicinal product.

3.  HOW TO TAKE LIPANTIL MICRO

Always take Lipantil Micro exactly as your doctor has told you. Also, please read the label on the packet. You should check with your doctor if you are not sure.

Swallow the capsule with a glass of water. It is important to take the capsule with food, as it will not work as well if your stomach is empty.

The usual dose for adults is one capsule of Lipantil Micro 67 three times a day, taken at mealtimes. The usual dose for children is one capsule of Lipantil Micro 67 per 20kg bodyweight per day. Your doctor will work out the dose that is required.

• If you take more Lipantil Micro than you should

If you accidentally take more Lipantil Micro than you should or if someone else has taken your medicine, contact your nearest hospital casualty department or tell your doctor immediately.

• If you forget to take Lipantil Micro

Do not take a double dose to make up for a forgotten capsule. Take the next dose with your next meal and then carry on taking your capsules as usual. If you are worried about this talk to your doctor.

• If you stop taking Lipantil Micro

Do not stop taking the medicine unless your doctor tells you to, or your medicine makes you feel unwell. This is because raised cholesterol levels need treating for a long period of time. Remember you should also continue with a low-fat diet whilst taking Lipantil Micro. If your doctor stops your medicine, do not keep any left over capsules unless your doctor tells you to. If you have any further questions on the use of this product, ask your doctor.

4.  POSSIBLE SIDE EFFECTS

Like all medicines, Lipantil Micro can cause side effects, although not everybody gets them. Some patients have experienced the following side effects whilst taking fenofibrate:

Common side effects:

-  Stomach pain, being sick, feeling sick, diarrhoea and wind (flatulence)

- Reactions such as rashes, itching, red patches on the skin or increased sensitivity   to sunlight, sun lamps and sunbeds

-  Headache, fatigue, vertigo

Uncommon side effects:

-   Pancreatitis (inflammation of the pancreas leading to abdominal pain)

- Blood clot in the lung causing chest pain and breathlessness (pulmonary embolism); blood clot in the leg causing pain, redness or swelling (deep vein thrombosis)

-  Gallstones

Rare side effects:

-  Raised levels of various liver enzymes in the blood

-  Slight increases in blood levels of substances normally excreted by the kidneys (urea and creatinine)

-  Reduced sex drive

-  Hair loss

-   Muscle pain, muscle inflammation, muscle cramps and weakness

-   Decrease in haemoglobin (oxygen carrying pigment in blood) and decrease in white blood cells

Very rare side effects:

-  Hepatitis (inflammation of the liver), symptoms of which may be mild jaundice (yellowing of the skin and whites of the eyes), stomach pain and itching

-  Muscle breakdown

-  Chronic disease of the lung tissues

If you develop any unusual discomfort, tell your doctor as soon as possible.

If any of the side effects gets serious, or if you notice any side effects not listed in this leaflet, please tell your doctor.

5. HOW TO STORE LIPANTIL MICRO

Keep this  medicine in the original  package  in  order to protect from moisture. Do not store above 30°C Keep out of the reach and sight of children.

On the carton and the blister pack after EXR The expiry date refers to the last day of that month.

Lipantil Micro should not be disposed of via wastewater or household waste. Ask your pharmacist how to dispose of medicines no longer required. These measures will help to protect the environment.

6. FURTHER INFORMATION

What Lipantil Micro contains

Each Lipantil Micro 67 capsule contains the active ingredient:

67 miligrams (mg) of fenofibrate.

Each capsule also contains the following inactive ingredients:

lactose    monohydrate,    magnesium    stearate,    sodium laurilsulfate, pregelatinised starch and crospovidone.

The capsule is made of gelatin, titanium dioxide (E171), quinoline yellow (E104) and erythrosine (E127).

 

Brand Name Drug: Targretin
Active Ingredient Drug: bexarotene
Indication: Treatment of cutaneous manifestations of early and advanced cutaneous T-cell lymphoma in patients refractory to at least one prior systemic therapy
Company Name: Ligand Pharmaceuticals Incorporated
Availability: Approved by FDA December 29, 1999

Introduction

Cutaneous T-cell lymphoma (CTCL) is a cancer of the T lymphocytes and afflicts between 16,000 and 20,000 people in the U.S. The cancer ordinarily manifests itself in the skin, but over time may progress to involve other organs. Skin lesions in CTCL patients can become deforming and culminate in ulceration, with secondary infection. Many treatments for cutaneous T-cell lymphoma have been external, such as UV light therapy and electron beam therapy.

Now a new drug manufactured by Ligand Pharmaceuticals Incorporated offers CTCL patients a more convenient form of treatment: Targretin (bexarotene). Targretin is an oral retinoid drug that can be taken once daily and has been shown to help some patients by reducing the severity of skin lesions. It is available in gelatin capsule form, with a recommended dosage of 300 mg/day per square meter of body surface area, to be taken with food. A gel form of Targretin is currently under review by the FDA.

How It Works

Targretin selectively binds to and activates retinoid X receptors (RXRs), which play an important role in cellular differentiation and proliferation. Targretin inhibits the growth in vitro of some tumor cell lines of hematopoietic and squamous cell origin, and has also induced tumor regression in animal studies. The exact mechanism of action of Targretin in the treatment of cutaneous T-cell lymphoma is unknown.

Targretin: Clinical Study Results

Two multicenter, open-label clinical studies were conducted in the U.S., Canada, Europe, and Australia to evaluate Targretin in 152 patients with advanced and early stage cutaneous T-cell lymphoma. Of this group, 102 were found to have been refractory to at least two prior therapies – one of them systemic – including 90 patients with advanced disease and 12 with early disease. Patients had an

Patients were treated with 300 mg/m(2)/day, a dosage that could be increased to 400 mg if no response was seen after 8 or more weeks of therapy and the patient could tolerate the drug. Tumor response was assessed using a Composite Assessment of Index Lesion Disease Severity, with a partial response defined as an improvement of at least 50% of the index lesions without worsening of lesions or development of new ones. A complete clinical response required complete disappearance of all manifestations of disease.

At the 300 mg dose, 1.6% of patients had a complete tumor response and 30% had a partial response. The rate of relapse in the patients who had a tumor response was 30% over a median observation period of 21 weeks. Responses were observed as early as 4 weeks and new responses continued to be seen at later visits.

What the Patient Should Know

Several mild to moderate events were observed in association with Targretin, and were essentially reversible. These included elevated blood triglycerides and cholesterol and decreased HDL cholesterol, acute pancreatitis associated with the triglyceride increase, leukopenia and neutropenia, hypothyroidism, headache, asthenia, rash, anemia, nausea, infection, peripheral edema, abdominal pain, diarrhea, fatigue/lethargy, and dry skin. Adverse events were dose-dependent, being most common in patients treated at a dose higher than 300 mg/m(2)/day.

Because Targretin is a retinoid – a class of drugs that has been associated with birth defects – Targretin must not be taken by women who are pregnant or intend to become pregnant. Targretin should be used with caution in patients with renal or hepatic impairment. Ketoconazole, itraconazole, erythromycin, gemfibrozil, grapefruit juice, and other inhibitors of cytochrome P450 may cause increased plasma Targretin levels, while rifampin, phenytoin, phenobarbital, and cytochrome p450 inducers may decrease plasma Targretin levels; patients taking these drugs should inform their physicians. Targretin should also be used with caution in patients taking antidiabetic medication, since Targretin may enhance their effects and result in hypoglycemia.

Patients are also advised to limit vitamin A intake to no more than 15,000 IU/day, and to provide themselves with adequate sun protection, since Targretin and other retinoids may increase photosensitivity.

Brand Name Drug: Welchol
Active Ingredient Drug: colesevelam hydrochloride
Indication: For the reduction of elevated low-density lipoprotein cholesterol in patients with primary hypercholesterolemia, as an adjunct to diet and exercise
Company Name: GelTex Pharmaceuticals, Inc.
Availability: Approved by FDA on May 26, 2000

Introduction

An estimated 52 million people in the US have at least mild hypercholesterolemia and would benefit from lipid-lowering therapy. Bile acid sequestrants are a class of lipid-lowering agents that work nonsystemically and therefore are an attractive treatment option for certain patients with elevated LDL cholesterol levels, particularly young adults with familial hypercholesterolemia. Bile acid sequestrants work without entering the bloodstream and are generally regarded as safer than absorbed agents such as statins, which require frequent liver function tests. In fact, the National Cholesterol Education Program recommends that physicians prescribe bile acid sequestrants as first-line cholesterol-lowering therapy. They may be used as monotherapy or in combination with other drugs such as the HMG-CoA reductase inhibitors (statins).

The biggest drawback to bile acid sequestrants, however, has been gastrointestinal side effects, including a high incidence of constipation as well as bloating, flatulence, and cramping. Welchol (colesevelam hydrochloride) is a new bile acid sequestrant manufactured by GelTex Pharmaceuticals, Inc. Welchol (formerly known as Cholestagel) is a nonabsorbed polymer (water-absorbing hydrogel) that has been specifically engineered to bind to bile acids. On May 26, 2000, the FDA approved Welchol for the reduction of elevated low-density lipoprotein cholesterol in patients with primary hypercholesterolemia.

Each Welchol tablet contains 625 mg of colesevelam. The recommended starting dose of Welchol as monotherapy is 3 tablets taken twice per day with meals or 6 tablets taken once a day with a meal. The Welchol dose can be increased up to 7 tablets, if necessary. When administered with an HMG-CoA reductase inhibitor, Welchol at doses of 4-6 tablets per day has been shown to be safe and effective when taken at the same time as the HMG-CoA reductase inhibitor or when the two drugs are taken at different times. The recommended dose of Welchol in combination with an HMG-CoA reductase inhibitor is 3 tablets twice daily or 6 tablets once daily, taken with a meal.

How It Works

Bile acids are synthesized by the liver from cholesterol and secreted into the intestines to aid digestion of fats. Bile acid sequestrants such as Welchol bind to bile acids in the intestinal tract and increase their excretion from the body. To replenish the bile acid pool, the liver draws cholesterol from the bloodstream, resulting in a reduction in blood cholesterol levels.

Welchol (colesevelam hydrochloride) has been found to have a high affinity for both trihydroxy and dihydroxy bile acids in the intestine, leading to increased fecal bile acid excretion. Preliminary in vivo and in vitro studies suggest that Welchol has superior bile acid binding efficacy compared with cholestyramine. Furthermore, since Welchol is not absorbed in the gastrointestinal tract, there is minimal potential for toxic effects. Its water-retaining ability creates a soft, gelatinous-like material that minimizes the potential for gastrointestinal irritation.

Welchol (colesevelam hydrochloride): Clinical Study Results

The efficacy of Welchol for lowering LDL cholesterol was demonstrated in eight clinical trials involving approximately 1,400 patients who were treated for 4-50 weeks. Welchol was found to be effective as initial monotherapy for patients with mild-to-moderate hypercholesterolemia.

One clinical study compared various doses of Welchol (1.5, 2.25, 3.0, or 3.75 g/d) to placebo in 137 patients with hypercholesterolemia (LDL cholesterol level greater than 160 mg/dL) who took Welchol or placebo with their morning and evening meals for 6 weeks. LDL cholesterol concentrations decreased in a dose-dependent manner by 4.2 mg/dL (1.8%) in the 1.5-g/d Welchol treatment group and up to 39 mg/dL (19.1%) in the 3.75-g/d Welchol treatment group. LDL cholesterol concentrations at the end of treatment were significantly reduced from baseline levels in the 3.0-g/d and 3.75-g/d Welchol treatment groups.

Total cholesterol levels demonstrated a similar response to Welchol treatment, with an 8.1% decrease from baseline in the 3.75-g/d treatment group. High-density lipoprotein cholesterol levels rose significantly in the 3.0-g/d and 3.75-g/d Welchol treatment groups, by 11.2% and 8.1%, respectively. Median triglyceride levels did not change from baseline, nor were there any significant differences between treatment groups.

In a study in patients with LDL cholesterol of 130-220 mg/dL, Welchol was given for 24 weeks in divided doses with the morning and evening meals. Mean LDL cholesterol reductions were 15% and 18% for the 3.8 g and 4.5 g doses, respectively, with respective mean total cholesterol reductions of 7% and 10%. HDL cholesterol increased by 3% with both doses of Welchol.

Co-administration of Welchol with an HMG-CoA reductase inhibitor (atorvastatin, lovastatin, or simvastatin) demonstrated additive reduction of LDL cholesterol in three clinical trials. Welchol at doses of 2.3 g/d and 3.8 g/d resulted in additional 8% and 16% reductions in LDL cholesterol, respectively, above that seen with the HMG-CoA reductase inhibitor alone.

What the Patient Should Know

The most common side effects reported by patients in clinical trials of Welchol were flatulence (12% for Welchol vs. 14% for placebo) and constipation (11% for Welchol vs. 7% for placebo). The incidence of gastrointestinal side effects was less than that associated with other drugs in its class; constipation, for example, occurs in up to 39% of patients taking conventional bile acid sequestrants.

Welchol (colesevelam hydrochloride) should not be taken by patients with bowel obstruction and those who have shown a hypersensitivity to any of its components.