Felodipine (Plendil)
Dihydropyridine calcium channel blocker for hypertension and angina. Undergoes extensive first-pass hepatic metabolism via CYP3A4, resulting in low oral bioavailability. Highly susceptible to grapefruit-drug interactions. Available as extended-release tablets for once-daily dosing.
Projected serum levels — 5 mg, once daily
Maintenance schedule: 5 mg once daily (oral).
Loading schedule: 10.3 mg on day 1, then 5 mg once daily — reaching therapeutic levels sooner.
Modeled steady state after ~3 days: peak ≈ 1.4 mg, trough ≈ 0.78 mg body load. Population-based estimate over 15 days for a 5 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.
Key facts
- Category
- Calcium Channel Blocker
- Route modeled
- Oral
- Model confidence
- inferred
- Half-life
- 25 h
- Common dose
- 5 mg
- Suggested maximum
- 10 mg/day
- Reference dose range
- 2.5–10 mg (single dose)
- Suggested cadence
- once daily
- Validated against
- 10 mg oral — Cmax 0.014 mg/L at 3.5 h
Documented interactions
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contraindicated
Carbamazepine (Tegretol) + Felodipine (Plendil)
Carbamazepine (Tegretol) inducer of CYP3A4 predicted to change Felodipine (Plendil) AUC by ~0.20x
-
contraindicated
Clarithromycin (Biaxin) + Felodipine (Plendil)
Clarithromycin (Biaxin) mechanism_based of CYP3A4 predicted to change Felodipine (Plendil) AUC by ~10.00x
-
contraindicated
Dasatinib (Sprycel) + Felodipine (Plendil)
Dasatinib (Sprycel) time_dependent_inhibitor of CYP3A4 predicted to change Felodipine (Plendil) AUC by ~5.00x
-
contraindicated
Diltiazem + Felodipine (Plendil)
Diltiazem mechanism_based of CYP3A4 predicted to change Felodipine (Plendil) AUC by ~10.00x
-
contraindicated
Efavirenz (Sustiva) + Felodipine (Plendil)
Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Felodipine (Plendil) AUC by ~0.12x
-
contraindicated
Grapefruit (whole fruit) + Felodipine (Plendil)
Grapefruit (whole fruit) mechanism_based of CYP3A4 predicted to change Felodipine (Plendil) AUC by ~10.00x
Serum checks 222 modeled interaction pairings for felodipine (plendil) across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.
Research behind this entry
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Interaction of citrus juices with felodipine and nifedipine
Landmark study demonstrating that grapefruit juice increases felodipine bioavailability 2.8-fold, establishing the original grapefruit-drug interaction (mean 284% of control, range 164-469%).
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Grapefruit juice increases felodipine oral availability in humans by decreasing intestinal CYP3A protein expression
Mechanistic study showing grapefruit-mediated 62% reduction in intestinal CYP3A4 protein, explaining the dramatic increase in felodipine systemic exposure.
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Pharmacokinetic analysis of felodipine-grapefruit juice interaction based on an irreversible enzyme inhibition model
Quantitative PK modeling of grapefruit-felodipine interaction demonstrating mechanism-based intestinal CYP3A4 inhibition by furanocoumarins.
3 published studies referenced in the app, each with a plain-language summary.