Probucol (Oral)

Probucol is prescribed by doctors to lower cholesterol in the bloodstream and prevent diseases associated with an elevated level of fat in the arteries.

Overview

What is Probucol?

Probucol, before it was removed from the market in the US in 1995 for safety reasons, was prescribed to reduce the level of artery-clogging cholesterol found to be too high in some patients, putting them at risk for multiple health conditions. While Probucol is effective on LDL and HDL cholesterol, serum-triglyceride cholesterol, also known as VLDL, doesn't seem to be affected.

Probucol was sold under the name Lorelco and was available in tablet form. It was removed from the market for safety reasons, after it proved too effective and underbalanced the cholesterol levels in the blood to the point it was deemed unsafe for some patients. Probucol is a completely synthetic substance and is only found in the bloodstream of individuals who have taken the drug itself.

How does Probucol work?

By increasing LDL elimination along with inhibiting cholesterol being absorbed from the foods eaten by the patient, Probucol effectively lowered the blood cholesterol by 10 to 20% in some patients, thereby controlling conditions of elevated levels. Some patients who have not responded to diet or exercise changes or other drugs have been successfully treated with Probucol to lower their blood cholesterol.

It is recommended, however, that patients follow a low fat, low sodium, low cholesterol diet prior to and during treatment with Probucol. Following a healthy diet and exercise plan can help the drug work better in lowering dangerous cholesterol levels before they become harmful to patient health.

What is cholesterol?

Cholesterol is found in the bloodstream of all people and plays an important part in cellular functions that aid in digestion and other vital processes. Too much cholesterol can increase a person's risk of contracting circulatory diseases, heart disease and stroke.

The two main forms of cholesterol are low-density lipoprotein and high-density lipoprotein or LDL and HDL. These are often referred to as bad cholesterol and good cholesterol respectively. Both types must be in balance, however, for the healthy functioning of the body's cells. Without drugs such as Probucol, patients who cannot control their cholesterol levels through diet alone had no choice but to face the health risks associated with imbalanced cholesterol.

Conditions Treated

High cholesterol

Type Of Medicine

Anticholesteremic agent

Side Effects

Unwanted health symptoms may occur in some patients with use of Probucol to lower the blood cholesterol. The following symptoms, should they appear, should be communicated to your doctor right away to prevent any long-term health issues:

  • Fainting
  • Dizziness
  • Rapid, irregular heart rhythm
  • Swollen face or mouth, hands or feet
  • Bleeding or bruising of an unusual nature
  • Fatigue or weakness that is unexpected

Other side effects will typically go away as the patient becomes adjusted to the medication. Check with your doctor if you experience the following:

  • Diarrhea
  • Vomiting
  • Nausea
  • Bloated stomach
  • Pain in stomach
  • Headache
  • Numb or tingling face, toes or fingers

Your doctor may be able to provide you with information on how to lessen any side effects you experience. Check with your healthcare provider should you experience any unwanted health effects while taking Probucol.

Dosage

Your doctor has written your prescription with your specific health in mind. For this reason, it is vitally important to follow all instructions given to you by your physician. Read all prescription information including the leaflet provided and ask any questions needed to make absolutely certain you understand all aspects of treatment with Probucol.

Do your best to take this medication at the same time every day as your doctor directs. Remember that Probucol doesn't cure your high cholesterol, but it does continuously work to keep your levels in check and needs to remain in your system to do so.

Your doctor will most likely give you a special diet that will assist Probucol in its effectiveness, so be sure to follow this diet. In fact, before prescribing you this medication, your doctor may put you on a low sugar, low cholesterol and low fat diet to see if diet alone can control your condition. If you are prescribed this medication, it is best to take Probucol with meals so that the absorption of the drug is maximized.

People who are very obese may not experience any benefit from treatment with Probucol and therefore may have to reduce their weight through diet and exercise prior to treatment with this drug. Follow your doctor's recommendation with regard to a special diet.

The tablet form of Probucol is most often prescribed in a 500-milligram dose twice daily with morning and evening meals for adults. Use of Probucol in children and infants is to be determined by their health care provider.

Do not miss a dose of Probucol; taking care to have a consistent routine in taking this drug ensures maximum safety and effectiveness. Should you miss a dose, do not double up if it is close to your regular schedule in taking the next dose. Skip the missing dose and resume your dosage routine as soon as possible.

Interactions

Patients who have previously demonstrated an adverse reaction to other medications or even foods, additives, dyes, preservatives or animals should alert their health care provider in case they are prone to allergic reactions. Disclose any other medications you may be taking to your physician before being prescribed Probucol and be certain to include any vitamin, holistic, herbal or over-the-counter medications you take as well, whether currently or in the past.

If you are on the following medications, it is not recommended that you be treated with Probucol as the combination of the drugs could put your health at risk. Alert your doctor if you are taking:

  • Amisulpride
  • Amifampridine
  • Cisapride
  • Bepridil
  • Foscarnet
  • Dronedarone
  • Mesoridazine
  • Levomethadyl
  • Piperaquine
  • Pimozide
  • Terfenadine
  • Sparfloxacin
  • Ziprasidone
  • Thioridazine

The drugs listed below may interact negatively with Probucol, but both drugs may be necessary as treatment to continue your health regimen. Your physician must determine if dosage should be adjusted for Probucol or other drugs if you are taking:

  • Acecainide
  • Amiodarone
  • Ajmaline
  • Aprindine
  • Anagrelide
  • Arsenic Trioxide
  • Aripiprazole
  • Azimilide
  • Astemizole
  • Buserelin
  • Bretylium
  • Chloroquine
  • Chloral Hydrate
  • Crizotinib
  • Chlorpromazine
  • Clarithromycin
  • Degarelix
  • Dabrafenib
  • Deslorelin
  • Delamanid
  • Dofetilide
  • Disopyramide
  • Domperidone
  • Dolasetron
  • Droperidol
  • Donepezil
  • Enflurane
  • Efavirenz
  • Escitalopram
  • Erythromycin
  • Flecainide
  • Fingolimod
  • Fluoxetine
  • Fluconazole
  • Gonadorelin
  • Gemifloxacin
  • Halofantrine
  • Goserelin
  • Halothane
  • Haloperidol
  • Hydroquinidine
  • Histrelin
  • Hydroxyzine
  • Hydroxychloroquine
  • Isoflurane
  • Ibutilide
  • Ivabradine
  • Isradipine
  • Leuprolide
  • Ketoconazole
  • Lidoflazine
  • Levofloxacin
  • Mefloquine
  • Lorcainide
  • Moxifloxacin
  • Metronidazole
  • Octreotide
  • Nafarelin
  • Panobinostat
  • Ondansetron
  • Pazopanib
  • Pasireotide
  • Pimavanserin
  • Pentamidine
  • Prajmaline
  • Pirmenol
  • Pitolisant
  • Prochlorperazine
  • Procainamide
  • Quetiapine
  • Propafenone
  • Risperidone
  • Quinidine
  • Sertindole
  • Sematilide
  • Sotalol
  • Sevoflurane
  • Sulfamethoxazole
  • Spiramycin
  • Sultopride
  • Sulpiride
  • Tedisamil
  • Tacrolimus
  • Trimethoprim
  • Telithromycin
  • Trifluoperazine
  • Vandetanib
  • Triptorelin
  • Vemurafenib
  • Vasopressin
  • Zolmitriptan
  • Vinflunine
  • Zuclopenthixol
  • Zotepine

Finally, patients who are taking the drug Cyclosporine should use caution and alert their physician that they are taking it, as the combination of drugs could cause unwanted effects on your health.

Your physician should be alerted if you are a regular user of tobacco products, alcoholic beverages or illegal drugs, as these substances can adversely interact with Probucol, causing risks to your overall health and wellbeing.

Patients who have the following diseases should make them known to their health care provider, as these conditions could become worse with use of Probucol:

  • Gallstones or disease of the gallbladder
  • Heart disease
  • Liver dysfunction
  • Kidney dysfunction

Your overall medical history should be communicated to your physician before being treated with Probucol for health reasons.

Warnings

No specific data has been collected with regard to use of Probucol in pediatric patients, so caution is advised in children older than the age of two. Children younger than two years old should not have their blood cholesterol adjusted with any drug, as this substance is necessary for health growth and development.

Geriatric patients have not been studied to determine if Probucol has the same effectiveness for them as it does in younger patients. As older patients have more overall health conditions, caution is advised with regard to any pre-existing health concerns in geriatric patients who are being considered for treatment with Probucol.

Pregnant women and those who are breastfeeding have not been studied with regard to risks they may pass on to their fetus or infants if they are being treated with Probucol. Risks and benefits must be assessed by your health care provider with regard to treatment with this drug if you are pregnant or breastfeeding.

Your physician will check the progress of Probucol in lowering your blood cholesterol levels during regular office visits. It will be determined at this time whether to continue treatment with Probucol. Long QT syndrome has been reported in some patients, which is accompanied by racing heart rhythm, fainting or dizziness. Symptoms such as this should be reported to your physician immediately.

As Probucol does not prevent the condition of high blood cholesterol and merely controls it, stopping this medication without advisement of your doctor is not safe and may increase your blood cholesterol levels to dangerous heights, putting you at risk for developing a number of cardiovascular diseases and conditions.

It is advised that you heed the diet and exercise recommendations passed on to you by your health care provider, as these instructions will assist in the work Probucol does to regulate your cholesterol levels. Patients who have experienced success with treatment of Probucol have followed a low fat, low cholesterol diet as well as following their doctor prescribed medication.

Storage

Probucol should be stored out of sight and reach of children and pets and is safe to store at room temperature. Do not allow this medication to be exposed to excess heat, moisture or light and do not allow it to freeze. Expired or unused Probucol should be disposed of safely according to the instructions given to you by your physician or pharmacist.

Summary

Though discontinued for regular prescription since 1995, Probucol was very effective and largely safe for doctors to prescribe in the treatment of patients with high blood cholesterol. Discontinued due to safety after some patients experienced out-of-balance cholesterol levels, Probucol may have a new life with a small number of patients who have not responded to other therapies including diet changes.

Considered an antihyperlipidemic class of drug, Probucol is prescribed in tablet form in a 500 milligram twice daily dose during meals in the morning and evening. It is not recommended that Probucol is prescribed for pediatric patients or for nursing mothers and pregnant women, as the lipid-lowering effects have been proven to negatively affect the health of infants and young children.

Probucol interacts with several drugs and may adversely affect pre-existing health conditions. For this reason, it is recommended that patients disclose their full medical history including any drugs they take to their health care provider, taking care to include any over-the-counter, vitamin or herbal supplements as well.

Probucol may not be effective in patients who are very obese and could build up to dangerous levels in patients who do not have full kidney or liver function. Patients with gallstones or diseases involving the gallbladder or those who have heart conditions are not candidates for treatment with this drug.

Patients are urged to maintain their treatment schedule as far as dosing and size of dose are concerned; this will assure a constant level of Probucol in the blood, which helps effectively regulate cholesterol levels. Do not miss a dose if you can help it and be sure to take the drug at the same times every day. Store this medication in a safe, secure place where it will not be exposed to extreme temperatures or moisture.