Posts Tagged ‘LDL’
Zocor Heart- Pro (Simvastatin)
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.
Lopid (Gemfibrozil)
Lopid 300mg Capsules
Lopid 600mg Film-Coated Tablets
Gemfibrozil
1. What Lopid is and what it is used for
- Lopid belongs to a class of medicines called fibrates that control fats (lipids). It works by reducing fats (lipids) known as bad cholesterol (LDL) and triglycehdes in your blood while increasing good cholesterol (HDL).
- Lopid prevents the build-up of cholesterol and fats along the walls of your arteries (a process known as atherosclerosis) which causes blockage of your blood supply to vital organs. It decreases your chances of getting heart disease, angina (chest pain), strokes, and heart attacks. Lopid may be used to prevent heart attacks in men (who may not have ‘bad cholesterol’), in cases where other medicines (statins) cannot be used.
- Lopid should be used together with other means of lowering fats in the body such as exercise, dietary changes and weight reduction.
2. Before you take Lopid
Do not use Lopid if you have the following conditions:
- Hypersensitivity (allergy) to Gemfibrozil or other similar lipid regulating medicines or any of the other ingredients in Lopid.
- Liver disease.
- Severe kidney disease.
- History of gall stones, bile and gall bladder disease (biliary tract disease).
- Photoallergy or phototoxicity reaction ( allergic reaction triggered by exposure to sunlight) during treatment with fibrates.
- If you are currently taking a drug called repaglinide (a drug used to reduce blood sugar levels in diabetes).
Take special care with Lopid:
Tell your doctor if you have any of the following conditions to help him or her decide if Lopid is suitable for you:
- Mild or moderate kidney disease.
- Under-active thyroid.
- High risk of muscle breakdown (rhabdomyolysis): risk factors include kidney impairment; under-active thyroid; over 70 years; excessive use of alcohol; previous history of muscular pain and weakness (muscular toxicity) with another fibrate; a history of inherited muscular disorders.
- Diabetes.
- If you are taking or have recently taken any other medicines, even those not prescribed.
Taking other medicines:
Please tell your doctor or pharmacist if you are taking any of the following medication:
- Anti-diabetic medication particularly rosiglitazone or repaglinide (used to help reduce blood sugar levels).
- Anticoagulants like warfarin (used to thin the blood).
- Statins used to lower bad cholesterol and triglycerides, and increase good cholesterol such as atorvastatin, simavastatin, lovastatin, pravastatin, and rosuvastatin.
- Colestipol resin granules for the treatment of high levels of fat (cholesterol) in your blood.
- Bexarotene medication for the treatment of skin cancer.
Please tell your doctor or pharmacist if you are taking or have recently taken any other medicines, including medicines obtained without a prescription.
Pregnancy and breast-feeding
It is recommended that you do not take Lopid during pregnancy unless it is necessary. Tell your doctor if you are pregnant or trying to become pregnant.
It is recommended that you do not take Lopid while you breast-feed unless it is necessary. Ask your doctor or pharmacist for advice before taking any medicine while breast-feeding.
Driving and using machinery
In rare cases Lopid may cause dizziness and affect your eyesight, if this happens, do not drive or operate machinery. You can drive or operate machinery as long as you feel well.
3. How to take Lopid
Your blood lipid levels will be closely monitored and regularly assessed before and during your treatment with Lopid. If you are diabetic or have problems with your thyroid, your doctor will try to treat these conditions before you start treatment. Your doctor will also give you advice about eating the correct diet, exercising, giving up smoking, cutting down on alcohol and if necessary, losing weight.
Lopid should be taken orally. It is recommended that the capsules or tablets be swallowed with a glass of water as the tablets taste unpleasant if you break them.
- Adults and elderly
The usual starting dose is between 900mg and 1200mg daily. Your doctor will decide the best dose for you, follow the instructions given on the label.
If you are advised to take a 1200mg dose, one 600mg tablet will need to be taken, half an hour before your breakfast and a second 600mg tablet will need to be taken half an hour before your evening meal.
If you are advised to take a 900mg dose, you will need to take the dose (3 x 300mg capsules), half an hour before your evening meal.
- Adults with mild or moderate kidney disease
Your doctor will assess your condition before and during your treatment with Lopid. Your treatment will start at 900mg daily and may increase up to 1200mg or until you respond to treatment.
Lopid is not recommended for children
- If you take too many capsules or tablets
If you accidentally take too many capsules or tablets contact your doctor at once or go to the nearest hospital accident and emergency department. Always take the labelled medicine package with you, whether there is any Lopid left or not.
- If you forget to take a dose
If you forget to take a dose, do not worry. Simply miss that dose and take your next dose at the right time. Do not take two doses at the same time.
It is recommended that you follow all the advice given while you are taking Lopid so as to gain the full benefit of the treatment.
4. Possible side effects
Lopid can cause side effects although not everybody gets them. Although serious allergic reactions are very rare, you are advised to contact your doctor immediately if you get any of the following symptoms after taking Lopid:
- Any sudden wheeziness, difficulty in breathing or dizziness, swelling of the eyelids, face, lips or throat.
- Peeling and blistering of the skin, around the mouth, eyes and genitals.
- Rash affecting your whole body.
- Muscle weakness or weakness accompanied by dark urine, fever, rapid heart rate (palpitations), nausea, vomiting and facial swelling.
Other reported side effects include:
Common side effects (occurs in less than 1 in 10 patients)
- Indigestion.
- Sense of spinning or swaying (vertigo).
- Headache.
- Stomach pain.
- Diarrhoea. -Wind.
- Feeling sick.
- Being sick.
- Constipation.
- Rash (particularly an itchy or puffy rash).
- Tiredness.
Uncommon side effects (occurs in less than 1 in 100 patients)
- Irregular heartbeat.
Rare (occurs in less than 1 in 1,000 patients)
- Persistent lack of energy.
- Problems with bleeding and bruising.
- Dizziness.
- Sleepiness.
- Paraesthesia (loss of feeling and a tingling sensation).
- Depression.
- Decreased libido.
- Blurred vision.
- Pancreatitis.
- Jaundice (yellowing of the skin).
- Hair loss.
- Appendicitis.
- Painful joints.
- Muscle disease (myopathy), muscle weakness, painful muscles or muscle breakdown (rhabdomyolysis).
- Impotence and photosensitivity (a sensitivity to light that can cause skin discolouration or a rash).
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 Lopid
- The unopened packs should be stored in the original container until ready for use.
- Lopid 300mg Capsules: Store below 25°C, in the original package in order to protect from moisture.
- Lopid 600mg tablets: Store below 25°C.
- Keep out of the reach and sight of children.
- Lopid should not be used after the expiry date printed on the pack.
6. Further Information
- What Lopid contains
The active substance in Lopid capsules is 300mg of Gemfibrozil. The other ingredients are:
Polysorbate (E433), Colloidal silica, Maize starch, Gelatin, Titanium dioxide (E171), Indigo carmine (E132) Erythrosine (E127), Shellac glaze, Iron oxide black (E172), N-butyl alcohol, Propylene glycol, Isopropyl alcohol, Industrial Methylated spirit 740P, Purified water
The active substance in Lopid tablets is 600mg of Gemfibrozil. The other ingredients are:
Microcrystalline cellulose, Pregelatinized starch
Colloidal silica (anhydrous) (E551), Polysorbate 80 (E433),Sodium starch glycollate, Magnesium stearate, Hyproxypropylmethyl cellulose (E464), Titanium dioxide (E171), Talc(E553b), Polydimethyl siloxane, Polyethylene glycol 6000.
- What Lopid looks like and contents of the pack
Lopid 300mg capsules contains a fine white powder in a hard gelatin capsule with a white opaque body and maroon cap., It is packaged in aluminium foil blister strips containing 112capsules.
Lopid 600mg tablet is a white oval film-coated tablet. It is packaged in transparent PVC blister strips with an aluminium foil back in packs containing 56 tablets.
Ortho-Prefest: Another Choice for Relieving Symptoms of Menopause
Brand Name Drug: Ortho-Prefest
Active Ingredient Drug: 17(beta)-estradiol / norgestimate
Indication: Treatment of vasomotor symptoms associated with menopause, treatment of vulvar and vaginal atrophy, and prevention of osteoporosis
Company Name: Ortho-McNeil Pharmaceuticals
Availability: Approved for marketing in the US on October 22, 1999
Introduction
A variety of types of hormone replacement therapy (HRT) are available for women who are experiencing symptoms of menopause, particularly hot flashes and vaginal atrophy. HRT has also been shown to reduce the risk of osteoporosis and heart disease. Now a new form of HRT has been approved with a once-a-day dosing schedule that will enhance patient compliance: Ortho-Prefest. Manufactured by Ortho-McNeil Pharmaceutical, a division of Johnson & Johnson, Ortho-Prefest contains 17-beta-estradiol and norgestimate combined in a single tablet. The tablet containing 1.0 mg estradiol is taken on days 1-3 of therapy, and the tablet containing 1.0 mg estradiol plus 0.09 mg norgestimate is taken on days 4-6. The pattern is then repeated continuously to produce a constant estrogen/intermittent progestogen regimen. Ortho-Prefest is indicated for the treatment of vasomotor symptoms of menopause (hot flashes) and vulvar and vaginal atrophy, and for the prevention of osteoporosis.
How It Works
Estradiol is the principal intracellular human estrogen and is substantially more potent than its metabolites. Circulating estrogens modulate the pituitary secretion of gonadotropins, luteinizing hormone, and follicle stimulating hormone through a negative feedback mechanism, and estrogen replacement therapy acts to reduce the elevated levels of these hormones in postmenopausal women.
Norgestimate is a derivative of 19-nortestosterone and behaves similar to natural progesterone. Progestins counter estrogenic effects by decreasing the number of nuclear estradiol receptors and suppressing epithelial DNA synthesis in endometrial tissue.
Ortho-Prefest: Clinical Study Results
Ortho-Prefest was evaluated in two 12-month trials in 1,212 healthy postmenopausal women. The results showed that Ortho-Prefest reduced the mean number of daily hot flashes from 10.9 at baseline to 0.7 at week 12; the corresponding numbers for estrogen alone were 11.0 and 1.1, respectively. When assessed for its effect on vulvar and vaginal atrophy, Ortho-Prefest was associated with a 31.9% decrease in the percentage of parabasal cells, an increase of 16.7% in intermediate cells, and an increase of 15.2% in superficial cells; the corresponding values for estrogen alone were -22.4%, 7.2%, and 15.3%, respectively.
The incidence of endometrial hyperplasia in women treated with Ortho-Prefest was 0%, while 29% of women who receive estrogen alone have some degree of hyperplasia. The percentage of women with cumulative amenorrhea during the 12-month trial period ranged from 24% at baseline to 51% at 12 months; the corresponding values for estrogen alone were 39% and 63%, respectively. Finally, Ortho-Prefest was associated with a 1.9% reduction in total cholesterol, a 9.7% increase in HDL-cholesterol, a 1.2% increase in LDL-cholesterol, and a 9.4% increase in triglycerides; the corresponding values for estrogen alone were 1.2%, 12.0%, 1.7%, and 29.0%, respectively.
What the Patient Should Know
The most commonly reported adverse effects associated with Ortho-Prefest were headache, breast pain, and upper respiratory infection. Others included back pain, flu-like symptoms, and abdominal pain. Because hormone replacement therapy has been associated with cancers of the breast and endometrium, as well as venous thromboembolism and gallbladder disease, a woman should speak to her healthcare provider and carefully consider her medical history before embarking on hormone replacement therapy such as Ortho-Prefest.
Drug Welchol for Hypercholesterolemia
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.