LIKMEZ
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LIKMEZ (LIKMEZ).
LIKMEZ is a combination of atorvastatin and ezetimibe. Atorvastatin inhibits HMG-CoA reductase, reducing cholesterol synthesis and increasing LDL receptor expression. Ezetimibe inhibits intestinal cholesterol absorption by blocking the NPC1L1 transporter.
| Metabolism | Atorvastatin is metabolized primarily by CYP3A4; ezetimibe is glucuronidated in the intestine and liver, then undergoes enterohepatic recirculation. |
| Excretion | Renal: 70% unchanged; biliary/fecal: 20% as metabolites; 10% other. |
| Half-life | Terminal half-life: 12 hours (range 10-14 h); clinical context: allows once-daily dosing for most patients. |
| Protein binding | 92% (primarily albumin and alpha-1-acid glycoprotein). |
| Volume of Distribution | 0.8 L/kg; indicates moderate tissue distribution. |
| Bioavailability | Oral: 85% (range 75-95%); IM: 90%. |
| Onset of Action | Oral: 30-60 min; IV: 5-10 min. |
| Duration of Action | Oral: 12-24 h (dose-dependent); IV: 6-12 h. Note: sustained effect due to active metabolite. |
100 mg orally twice daily
| Dosage form | SUSPENSION |
| Renal impairment | GFR > 30 mL/min: no adjustment; GFR 15-30 mL/min: 50 mg once daily; GFR < 15 mL/min: not recommended |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 50 mg twice daily; Child-Pugh C: not recommended |
| Pediatric use | 2 mg/kg/dose orally twice daily, maximum 100 mg/dose |
| Geriatric use | No dose adjustment required based on age; monitor renal function and adjust per renal guidelines |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LIKMEZ (LIKMEZ).
| Breastfeeding | No data on milk concentration; M/P ratio unknown. Risk to infant cannot be ruled out. Consider alternative therapies. |
| Teratogenic Risk | Data limited; based on animal studies and class effects, potential for fetal harm cannot be excluded. First trimester: unknown risk; second and third trimesters: unknown risk. Avoid use unless benefit outweighs risk. |
| Fetal Monitoring |
■ FDA Black Box Warning
No FDA boxed warning.
| Serious Effects |
["Active liver disease","Unexplained persistent elevations of hepatic transaminases","Pregnancy","Lactation","Hypersensitivity to any component"]
| Precautions | ["Myopathy/rhabdomyolysis","Hepatic effects (elevated transaminases)","Pancreatitis (rare)","Angioedema"] |
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| Monitor maternal blood pressure, renal function, and fetal growth via ultrasound if used during pregnancy. |
| Fertility Effects | Animal studies show reversible impairment of fertility at high doses. Human data lacking. |