Lovastatin and Itraconazole: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Itraconazole
Lovastatin
How we grade severity & evidence
Severity levels
- Contraindicated: These should generally not be used together.
- Major: Potentially serious — often needs a change or close monitoring.
- Moderate: Can be significant — usually manageable with monitoring.
- Minor: Usually limited clinical impact.
Evidence grades
- Established: Well documented — supported by controlled studies or strong clinical data.
- Probable: Good supporting evidence, though not definitively proven.
- Suspected: Some evidence suggests this interaction, but it is not well established.
- Possible: Limited or conflicting evidence; the interaction may occur.
- Theoretical: Predicted from the drugs' pharmacology; not yet confirmed in people.
Ratings come from the documented interaction literature and are reviewed by a pharmacist. They describe the documented risk of the combination, not what will necessarily happen to you — your dose, timing, and health picture all matter.
What happens
Increased lovastatin exposure and an increased risk of lovastatin-related adverse effects, such as an increased risk of myopathy and rhabdomyolysis
Interaction Deep Dive
Coadministration of itraconazole (strong CYP3A4 inhibitor) and lovastatin, as well as use for up to 2 weeks following itraconazole discontinuation, is contraindicated. Coadministration of itraconazole and lovastatin may increase lovastatin exposure and the risk of serious adverse events23, including myopathy and rhabdomyolysis, particularly at high lovastatin doses. If treatment with itraconazole is unavoidable, suspend lovastatin during the course of itraconazole treatment. In a drug interaction study, coadministration of itraconazole and lovastatin increased lovastatin AUC and Cmax by 14.8-fold and 14.5-fold, respectively 1.
Why it happens (mechanism)
Inhibition of CYP3A4-mediated metabolism of lovastatin by itraconazole
Literature reports
5 reports — tap to read
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 4.
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 5.
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 6.
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 7.
e) In a drug interaction study, coadministration of itraconazole (strong CYP3A4 inhibitor) and lovastatin increased lovastatin AUC and Cmax by 14.8-fold and 14.5-fold, respectively 1.
Common questions
Can I take Lovastatin and Itraconazole together?
Increased lovastatin exposure and an increased risk of lovastatin-related adverse effects, such as an increased risk of myopathy and rhabdomyolysis Always confirm with your pharmacist or prescriber before making any change.
How serious is the Lovastatin and Itraconazole interaction?
It is rated contraindicated. These should generally not be used together.
How quickly could this interaction happen?
The documented onset is "delayed". Effects tend to build up gradually over days to weeks.
How strong is the evidence for this interaction?
The evidence is graded "probable". Good supporting evidence, though not definitively proven.
From our Q&A
Real reader questions about these medications, each personally answered by our pharmacist:
Questions for your pharmacist
- Does my dose of Lovastatin or Itraconazole need adjusting while I take them together?
- What symptoms should prompt me to call you or my prescriber right away?
- Does the timing of my doses matter for this combination?
- Is there a safer alternative to one of these medications for me?
References (7)
- Product Information: ALTOPREV(R) oral extended-release tablets, lovastatin oral extended-release tablets. Covis Pharma (per FDA), King of Prussia, PA, 2024. DailyMed
- Product Information: SPORANOX(R) oral capsules, itraconazole oral capsules. Janssen Pharmaceuticals Inc (per FDA), Titusville, NJ, 2024. DailyMed
- Product Information: SPORANOX(R) oral solution, itraconazole oral solution. Janssen Pharmaceuticals Inc (per FDA), Titusville, NJ, 2024. DailyMed
- Neuvonen PJ & Jalava KM: Itraconazole drastically increases plasma concentrations of lovastatin and lovastatin acid. Clin Pharmacol Ther 1996; 60:54-61. PubMed
- Horn M: Coadministration of itraconazole with hypolipidemic agents may induce rhabdomyolysis in healthy individuals. Arch Dermatol 1996; 132:1254. DOI
- Lees RS & Lees AM: Rhabdomyolysis from the coadministration of lovastatin and the antifungal agent itraconazole (letter). N Eng J Med 1995; 333:664-665. PubMed
- Kivisto KT, Kantola T, & Neuvonen PJ: Different effects of itraconazole on the pharmacokinetics of fluvastatin and lovastatin. Br J Clin Pharmacol 1998; 46:49-53. PubMed
Keep reading about Itraconazole
Keep reading about Lovastatin
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Prescription drugs aren't the whole picture — herbal and dietary supplements can interact with them too. From the evidence-graded Natural Medicines database:
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