Pelzont

laropiprant / nicotinic acid

This is a summary of the European public assessment report (EPAR). It explains how the Committee for Medicinal Products for Human Use (CHMP) assessed the studies performed, to reach their recommendations on how to use the medicine.
If you need more information about your medical condition or your treatment, read the package leaflet (also part of the EPAR) or contact your doctor or pharmacist. If you want more information on the basis of the CHMP recommendations, read the scientific discussion (also part of the EPAR).

What is Pelzont?

Pelzont is a medicine containing two active substances: nicotinic acid (also known as niacin or vitamin B3) and laropiprant. It is available as modified-release tablets. ‘Modified-release’ means that the two active substances are released at different rates from the tablet over a few hours.

What is Pelzont used for?

Pelzont is used in addition to diet and exercise in patients with dyslipidaemia (abnormally high levels of fat in the blood), particularly ‘combined mixed dyslipidaemia’ and ‘primary hypercholesterolaemia’. Patients with combined mixed dyslipidaemia have high blood levels of ‘bad’ LDL cholesterol and triglycerides (a type of fat), and low levels of ‘good’ HDL cholesterol. Primary hypercholesterolaemia is when the levels of cholesterol in the blood are high. Primary means that the hypercholesterolaemia does not have any identifiable cause.

Pelzont is normally given together with a statin (the standard medicine used to reduce cholesterol) when the effectiveness of a statin taken alone is inadequate. Pelzont is used on its own only in patients who cannot take statins.

The medicine can only be obtained with a prescription.

How is Pelzont used?

The starting dose of Pelzont is one tablet once a day for four weeks, after which the dose is increased to two tablets once a day. It is taken by mouth, with food, in the evening or before going to bed. The tablets must be swallowed whole, and should not be split, broken, crushed or chewed.

Pelzont is not recommended for use in children under 18 years of age because of a lack of information on its safety and effectiveness in this group. It should be used with caution in patients who have problems with their kidneys and should not be used in patients with liver problems.

How does Pelzont work?

The two active substances in Pelzont, nicotinic acid and laropiprant, have different modes of action.

Nicotinic acid is a naturally occurring substance that is used in low doses as a vitamin. In higher doses, it reduces the levels of fat in the blood via a mechanism that is not fully understood. It was first used as a medicine to modify blood fat levels in the mid-1950s, but its use has been limited because of its side effects, particularly flushing (reddening of the skin).

Flushing due to nicotinic acid is thought to occur because of the release of a substance called ‘prostaglandin D2’ (PGD2) from cells in the skin, which dilates (widens) the blood vessels in the skin. Laropiprant blocks the receptors to which PGD2 normally attaches. When the receptors are blocked, PGD2 cannot dilate the vessels in the skin, reducing the frequency and intensity of flushing.

In Pelzont tablets, laropiprant is in one of the layers, and the other layer contains nicotinic acid. When the patient takes the tablet, laropiprant is released first into the bloodstream and blocks the PGD2 receptors. The nicotinic acid is released more slowly from the other layer and has its effect as a fat-modifying agent.

How has Pelzont been studied?

The effects of Pelzont were first tested in experimental models before being studied in humans.

Pelzont was studied in four main studies in patients with hypercholesterolaemia or mixed dyslipidaemia.

Two studies looked at the effectiveness of Pelzont in modifying blood fat levels. The first study compared the effectiveness of Pelzont with that of nicotinic acid alone or placebo (a dummy treatment) in reducing the levels of LDL cholesterol in a total of 1,613 patients. This study also looked at the symptoms of flushing using a specially designed questionnaire.

The second study compared the combination of Pelzont and simvastatin (a statin) with Pelzont alone or simvastatin alone in 1,398 patients. The main measure of effectiveness was the change in the blood levels of LDL cholesterol after 12 weeks.

The third and fourth studies looked at the effectiveness of laropiprant in reducing the flushing caused by nicotinic acid. They included a total of 2,349 patients who were taking either Pelzont or nicotinic acid. Flushing was measured using the flushing symptom questionnaire.

What benefit has Pelzont shown during the studies?

Pelzont was effective in reducing the blood levels of LDL cholesterol. In the first study, LDL cholesterol levels were reduced by 19% in patients taking Pelzont, compared with 1% in those taking placebo. The second study showed that the LDL cholesterol levels were further reduced when Pelzont was taken with simvastatin (48% reduction), compared with Pelzont alone (17% reduction) or simvastatin alone (37% reduction).

Adding laropiprant to nicotinic acid reduced the symptoms of flushing caused by nicotinic acid. In the first and third studies, fewer patients taking Pelzont reported moderate, severe or extreme flushing than patients taking nicotinic acid alone. In the fourth study, flushing was seen on fewer days in patients taking Pelzont than in those taking nicotinic acid alone.

What is the risk associated with Pelzont?

The most common side effect with Pelzont (seen in more than 1 patient in 10) is flushing. For the full list of all side effects reported with Pelzont, see the package leaflet.

Pelzont should not be used in people who may be hypersensitive (allergic) to nicotinic acid, laropiprant or any of the other ingredients. It should also not be used in patients who have problems with their liver, an active stomach ulcer or bleeding from an artery.

Why has Pelzont been approved?

The Committee for Medicinal Products for Human Use (CHMP) decided that Pelzont’s benefits are greater than its risks for the treatment of dyslipidaemia, particularly in patients with combined mixed dyslipidaemia and in patients with primary hypercholesterolaemia. The Committee recommended that Pelzont be given marketing authorisation.

Other information about Pelzont

The European Commission granted a marketing authorisation valid throughout the European Union for Pelzont to Merck Sharp & Dohme Ltd. on 3 July 2008.

This EPAR was last updated on 02/02/2012 .

More detail is available in the summary of product characteristics

Product details

Publication details

Product information

24/08/2011  Pelzont -EMEA/H/C/000903 -WS/0123

Contents

• Annex I - Summary of product characteristics
• Annex IIA - Manufacturing-authorisation holder responsible for batch release
• Annex IIB - Conditions of the marketing authorisation
• Annex IIIA - Labelling
• Annex IIIB - Package leaflet

Please note that the size of the above document can exceed 50 pages.

You are therefore advised to be selective about which sections or pages you wish to print.

Pharmacotherapeutic group

Lipid modifying agents

Therapeutic indication

Pelzont is indicated for the treatment of dyslipidaemia, particularly in patients with combined mixed dyslipidaemia (characterised by elevated levels of LDL-cholesterol and triglycerides and low HDL-cholesterol) and in patients with primary hypercholesterolaemia (heterozygous familial and non-familial).
Pelzont should be used in patients in combination with HMG-CoA reductase inhibitors (statins), when the cholesterol lowering effect of HMG-CoA reductase inhibitor monotherapy is inadequate. It can be used as monotherapy only in patients in whom HMG-CoA reductase inhibitors are considered inappropriate or not tolerated. Diet and other non-pharmacological treatments (e.g. exercise, weight reduction) should be continued during therapy with Pelzont.

Changes since initial authorisation of medicine

Initial marketing-authorisation documents