Gemfibrozil/Lopid

IMPORTANT: Gemfibrozil (Lopid) is contraindicated in combination with all statins. This combination significantly increases the risk of serious muscle damage (rhabdomyolysis) and must not be prescribed together. If you are currently taking any statin (including atorvastatin, simvastatin, rosuvastatin, pravastatin, or fluvastatin), you must inform your prescriber before starting gemfibrozil. Gemfibrozil is also contraindicated with repaglinide and selexipag. Your prescriber will carefully review your full medicines list before any prescription is considered.

Fibrate medicines play an important role in managing elevated triglycerides and certain mixed lipid disorders, particularly in patients where triglyceride reduction is the primary clinical need. Gemfibrozil tablets, available as Lopid 300 mg and 600 mg, are a prescription-only fibrate used in adults for hyperlipidaemia. Gemfibrozil has a distinct and important interaction profile that sets it apart from other fibrates, most notably its contraindication with statins. A prescription can only be issued following a clinical consultation.

Gemfibrozil is an oral prescription medicine belonging to the fibrate class of lipid-lowering medicines. The brand name Lopid is widely recognised for Gemfibrozil in the UK and internationally. Gemfibrozil is available in two tablet strengths: 300 mg and 600 mg. It is one of the older fibrate medicines, having been used clinically since the 1970s, and has a significant evidence base including the Helsinki Heart Study, which demonstrated cardiovascular benefit in men with dyslipidaemia.

Gemfibrozil is licensed in the UK for treatment of hyperlipidaemia of types IIa, IIb, III, IV, and V in adult patients who have not responded adequately to dietary measures. This covers primary hypercholesterolaemia, combined hyperlipidaemia, hypertriglyceridaemia, and mixed dyslipidaemia. Gemfibrozil is indicated for use when dietary and other non-pharmacological measures have not been sufficient.

An essential clinical feature of Gemfibrozil that distinguishes it from other fibrates is its contraindication with statins. Unlike fenofibrate and bezafibrate, which can be used alongside statins under careful monitoring, Gemfibrozil must not be prescribed together with any statin. This is due to its inhibition of the CYP2C8 enzyme and organic anion transporting polypeptides, which causes statin blood levels to rise dramatically, greatly increasing the risk of severe rhabdomyolysis.

Gemfibrozil lowers blood lipids through its action as a PPAR alpha agonist, the same fundamental mechanism as other fibrates, combined with several additional effects on lipoprotein metabolism.

PPAR Alpha Activation. Gemfibrozil activates PPAR alpha receptors in liver and muscle cells, regulating genes involved in fatty acid oxidation and lipoprotein metabolism. This activation increases lipoprotein lipase activity, breaking down triglyceride rich VLDL and chylomicron particles and producing a significant fall in plasma triglycerides. Gemfibrozil also reduces hepatic VLDL synthesis.

Effects on the Lipid Profile. Gemfibrozil's primary lipid effect is a substantial reduction in plasma triglycerides, typically 30 to 50 per cent from baseline. It also raises HDL cholesterol. The effect on LDL cholesterol varies: in hypertriglyceridaemia, LDL may rise modestly as VLDL is cleared; in mixed dyslipidaemia, LDL may fall modestly.

CYP2C8 and OATP Inhibition: Why Gemfibrozil Cannot Be Combined with Statins. Gemfibrozil and its glucuronide metabolite potently inhibit the CYP2C8 enzyme and organic anion transporting polypeptides, particularly OATP1B1 and OATP1B3, which are responsible for hepatic uptake and elimination of several statins. This causes statin plasma concentrations to increase dramatically — up to 3.5-fold for simvastatin acid and up to 7-fold for rosuvastatin — substantially increasing the risk of severe myopathy and potentially fatal rhabdomyolysis. This is the basis for the contraindication between Gemfibrozil and all statins.

Always take Gemfibrozil exactly as your prescriber instructs. Read the Patient Information Leaflet supplied with your medicine before starting treatment.

• Gemfibrozil is taken twice daily. The standard dose is 600 mg twice daily (morning and evening), taken 30 minutes before a meal.
• Take Gemfibrozil 30 minutes before your morning and evening meals.
• Swallow the tablet whole with a glass of water.

If you miss a dose, take it as soon as you remember before your next meal. If you only remember after eating, skip the missed dose and take your next scheduled dose 30 minutes before the following meal. Do not take two doses at once. Do not stop taking Gemfibrozil without speaking to your prescriber first.

Your prescriber will arrange blood tests to check your lipid levels before and during treatment. Liver function and kidney function may also be monitored.

Gemfibrozil 300 mg Tablets: Allows lower dose initiation or dose titration. A starting dose of 600 mg per day (two 300 mg tablets) once daily before breakfast may be used in some patients, with the possibility of increasing to the standard twice daily regimen. Also supports dose adjustment in patients with kidney impairment.

Gemfibrozil 600 mg Tablets: The standard strength for the recommended maintenance dose. The usual dose is 600 mg twice daily, taken 30 minutes before the morning and evening meals — a total daily dose of 1200 mg. The most commonly prescribed strength. All dose decisions are made by your prescriber.

Gemfibrozil can cause side effects.

Common Side Effects (may affect up to 1 in 10 people):

• Gastrointestinal effects including abdominal pain, dyspepsia, nausea, diarrhoea, and flatulence. Taking Gemfibrozil 30 minutes before meals helps reduce gastrointestinal discomfort.
• Muscle aches or weakness (myalgia). Contact your prescriber promptly if you experience unexplained muscle pain, tenderness, or weakness.

Uncommon Side Effects (may affect up to 1 in 100 people):

• Raised liver enzymes, monitored during treatment.
• Headache.
• Dizziness.
• Skin rash or itching.

Serious Side Effects — Seek Urgent Medical Attention: Go to your nearest accident and emergency department or call 999 immediately if you experience severe muscle pain, weakness, or cramps, particularly with dark, tea coloured urine (rhabdomyolysis — Gemfibrozil carries a higher risk than other fibrates); signs of significant liver problems such as yellowing of the skin or eyes, severe abdominal pain, or very dark urine; pancreatitis (severe upper abdominal pain radiating to the back); or signs of a severe allergic reaction such as sudden widespread rash, difficulty breathing, or swelling of the face, lips, tongue, or throat.

Gemfibrozil tablets may be suitable if you:

• Are an adult with hyperlipidaemia, hypertriglyceridaemia, or mixed dyslipidaemia that has not responded adequately to dietary measures.
• Are not currently taking any statin medicine and are not expected to require a statin alongside gemfibrozil.
• Are not taking repaglinide, selexipag, or other contraindicated medicines listed in the SmPC.
• Are already prescribed Gemfibrozil and require a repeat prescription through an online prescribing service.

Gemfibrozil tablets are contraindicated or not suitable if you:

• Are taking any statin. Gemfibrozil is contraindicated with all statins including atorvastatin, simvastatin, rosuvastatin, pravastatin, fluvastatin, and pitavastatin.
• Are taking repaglinide, due to a serious risk of severe hypoglycaemia.
• Are taking selexipag.
• Have significant liver disease or persistently abnormal liver function tests.
• Have severe kidney impairment.
• Have a history of gallbladder disease — contraindicated.
• Have a history of photoallergy or phototoxicity from fibrate medicines.
• Are pregnant or planning to become pregnant.
• Are breastfeeding.
• Are under 18 years of age.
• Have a known allergy or hypersensitivity to Gemfibrozil or any excipient listed in the SmPC.

Important Drug Interactions: All statins are contraindicated due to dramatically increased statin blood levels and rhabdomyolysis risk. Repaglinide is contraindicated due to life-threatening hypoglycaemia risk. Selexipag is contraindicated. Warfarin's anticoagulant effect is significantly enhanced — close INR monitoring needed, with likely dose reduction. Colchicine blood levels increase, raising toxicity risk. Ezetimibe levels increase, raising gallstone risk — combination generally not recommended. Antidiabetic medicines may have enhanced blood glucose lowering effects.

Gemfibrozil is a Prescription Only Medicine. The clinical consultation is the essential first step. A prescription will only be issued if a registered prescriber concludes, based on their individual assessment of your circumstances, that Gemfibrozil is clinically appropriate for you.

During your online consultation with Pharmacy Planet, a registered prescriber will review your lipid profile, triglyceride levels, complete medicines list, kidney and liver function where available, and other relevant medical history. Given the contraindication with statins and several other medicines, the prescriber will pay particular attention to your current and recent medicines before making any prescribing decision.

Not all consultations will result in a prescription. The prescriber may determine that a different fibrate is more appropriate for your circumstances, request blood test results, or advise that a GP review is needed.