Lovastatin with Itraconazole Interaction Details
Brand Names Associated with Lovastatin
- Altocor®
- Altoprev®
- Lovastatin
- Mevacor®
Brand Names Associated with Itraconazole
- Itraconazole
- Onmel®
- Sporanox®
- Tolsura®
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Nov 15, 2023
Interaction Effect
An increased risk of myopathy and rhabdomyolysis
Interaction Summary
Coadministration of itraconazole and lovastatin, as well as use for up to 2 weeks following itraconazole discontinuation, is contraindicated as this may increase lovastatin exposure and the risk of serious adverse events, including myopathy .
Severity
Contraindicated
Onset
Delayed
Evidence
Probable
How To Manage Interaction
Coadministration of itraconazole and lovastatin, as well as use for up to 2 weeks following itraconazole discontinuation, is contraindicated as this may increase lovastatin exposure and the risk of serious adverse events, including myopathy .
Mechanism Of Interaction
Inhibition of CYP3A4-mediated metabolism of lovastatin by itraconazole
Literature Reports
A) In a double-blind, randomized, two-phase crossover study, 12 healthy volunteers were given either 200 mg itraconazole or placebo orally every day for four days. On day 4, each subject received a single 40 mg dose of lovastatin. For the next 24 hours, plasma concentrations of lovastatin, lovastatin acid, itraconazole, hydroxyitraconazole, and creatine kinase were determined. Itraconazole increased the Cmax and AUC of lovastatin more than 20-fold. In addition, itraconazole increased the mean Cmax and the AUC of the active metabolite , lovastatin acid, by 13-fold and 20-fold, respectively. During the itraconazole phase and within 24 hours of lovastatin administration, the plasma creatine kinase was increased 10-fold in one subject .
B) In one case report, a 74-year-old man was given itraconazole 200 mg for fungal toenails. He had been taking simvastatin 40 mg daily, lisinopril, and aspirin for hypertension and type IIa hyperlipidemia. After 3 weeks of therapy, he experienced pain in the lower and upper extremities and neck, muscle tenderness, and brown urine. Abnormal lab values on examination included creatine kinase (22,800,000 units/L), aldolase (423,600 units/L), lactate dehydrogenase (927,000 units/L), aspartate aminotransferase (990,000 units/L), and alanine aminotransferase (446,000 units/L). The patient was diagnosed with rhabdomyolysis .
C) A 63-year-old woman with familial hypercholesterolemia and previous myocardial infarction with bypass was treated with 80 mg of lovastatin and 3 g of niacin daily for 10 years without indications of toxicity. She was also taking timolol maleate and aspirin. Two weeks after itraconazole 100 mg twice daily was added for tinea corporis, the patient developed weakness, pain on motion, and tenderness to touch in her arms, back, and legs. This was later diagnosed as drug-induced rhabdomyolysis and hepatotoxicity. Eighteen days after termination of lovastatin, niacin, and itraconazole therapy, and initiation of ubiquinone 210 mg daily, the symptoms had disappeared .
D) Ten healthy volunteers received itraconazole 100 mg daily or matching placebo for four days in a randomized, cross-over study. Lovastatin 40 mg was administered one hour after the itraconazole or placebo dose on day 4. Cmax of lovastatin increased from 4.0 ng/mL during the placebo phase to 50.3 ng/mL in the itraconazole phase. Likewise, the Cmax of lovastatin acid, the active drug component, increased from 5.3 ng/mL to 51.5 ng/mL. AUC of lovastatin and lovastatin acid rose from less than 15 to 222 ng/mL/hr and from 34.0 to 291 ng/mL/hr, respectively, in the presence of itraconazole. The study demonstrated that even a relatively low daily dose of itraconazole can result in a clinically significant risk of interaction with lovastatin .
Lovastatin Overview
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Lovastatin is used together with diet, weight-loss, and exercise to reduce the risk of heart attack and stroke and to decrease the chance that heart surgery will be needed in people who have heart disease or who are at risk of developing heart disease. Lovastatin is also used to decrease the amount of cholesterol (a fat-like substance) and other fatty substances in the blood. Lovastatin is in a class of medications called HMG CoA reductase inhibitors (statins). It works by slowing the production of cholesterol in the body to decrease the amount of cholesterol that may build up on the walls of the arteries and block blood flow to the heart, brain, and other parts of the body.
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Accumulation of cholesterol and fats along the walls of your arteries (a process known as atherosclerosis) decreases blood flow and, therefore, the oxygen supply to your heart, brain, and other parts of your body. Lowering your blood level of cholesterol and fats with lovastatin may help prevent heart disease, angina (chest pain), strokes, and heart attacks.
Itraconazole Overview
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Itraconazole capsules (Sporanox, Tolsura) are used to treat fungal infections in the lungs that can spread throughout the body. Itraconazole capsules (Sporanox) are also used to treat fungal infections of the fingernails and toenails. Itraconazole oral solution (liquid) is used to treat yeast infections of the mouth and throat or of the esophagus (tube that connects the throat to the stomach). Itraconazole is in a class of antifungals called triazoles. It works by slowing the growth of fungi that cause infection.
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Definitions
Severity Categories
Contraindicated
These drugs, generally, should not be used together simultaneously due to the high risk of severe adverse effects. Combining these medications can lead to dangerous health outcomes and should be strictly avoided unless otherwise instructed by your provider.
Major
This interaction could result in very serious and potentially life-threatening consequences. If you are taking this drug combination, it is very important to be under close medical supervision to minimize severe side effects and ensure your safety. It may be necessary to change a medication or dosage to prevent harm.
Moderate
This interaction has the potential to worsen your medical condition or alter the effectiveness of your treatment. It's important that you are monitored closely and you potentially may need to make adjustments in your treatment plan or drug dosage to maintain optimal health.
Minor
While this interaction is unlikely to cause significant problems, it could intensify side effects or reduce the effectiveness of one or both medications. Monitoring for changes in symptoms and your condition is recommended, and adjustments may be made if needed to manage any increased or more pronounced side effects.
Onset
Rapid: Onset of drug interaction typically occurs within 24 hours of co-administration.
Delayed: Onset of drug interaction typically occurs more than 24 hours after co-administration.
Evidence
Level of documentation of the interaction.
Established: The interaction is documented and substantiated in peer-reviewed medical literature.
Theoretical: This interaction is not fully supported by current medical evidence or well-documented sources, but it is based on known drug mechanisms, drug effects, and other relevant information.
How To Manage The Interaction
Provides a detailed discussion on how patients and clinicians can approach the identified drug interaction as well as offers guidance on what to expect and strategies to potentially mitigate the effects of the interaction. This may include recommendations on adjusting medication dosages, altering the timing of drug administration, or closely monitoring for specific symptoms.
It's important to note that all medical situations are unique, and management approaches should be tailored to individual circumstances. Patients should always consult their healthcare provider for personalized advice and guidance on managing drug interactions effectively.
Mechanism Of Interaction
The theorized or clinically determined reason (i.e., mechanism) why the drug-drug interaction occurs.
Disclaimer: The information provided on this page is for informational purposes only and should not be considered medical advice. Always consult with a qualified healthcare professional regarding your specific circumstances and medical conditions.
Where Does Our Information Come From?
Information for our drug interactions is compiled from several drug compendia, including:
The prescribing information for each drug, as published on DailyMED, is also used.
Individual drug-drug interaction detail pages contain references specific to that interaction. You can click on the reference number within brackets '[]' to see what reference was utilized.
The information posted is fact-checked by HelloPharmacist clinicians and reviewed quarterly.