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| Clinical data | |
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| Trade names | Plendil |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a692016 |
| Routes of administration | Oral |
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| Pharmacokinetic data | |
| Bioavailability | 15% |
| Metabolism | Hepatic |
| Onset of action | 2.5–5 hours |
| Eliminationhalf-life | 25 hours[1] |
| Excretion | Renal |
| Identifiers | |
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| CAS Number | |
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| DrugBank |
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| ChemSpider |
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| UNII | |
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| ChEBI | |
| ChEMBL | |
| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.149.305 |
| Chemical and physical data | |
| Formula | C18H19Cl2NO4 |
| Molar mass | 384.25 g·mol−1 |
| 3D model (JSmol) | |
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Felodipine is a medication of thecalcium channel blocker type that is used to treathigh blood pressure.
It was patented in 1978, and approved for medical use in 1988.[2]
Felodipine is used to treathigh blood pressure and stableangina.[1][3]
It should not be used for people who are pregnant, haveacute heart failure, are having aheart attack, have anobstructed heart valve, or have obstructions that blockbloodflow out of the heart.[1]
For people withliver failure the dose needs to be lowered, because felodipine is cleared by the liver.[1]
The only very common side effect, occurring in more than 1/10 people, ispain and swelling in the arms and legs.[1]
Common side effects, occurring in between 1% and 10% of people, include flushing, headache,heart palpitations, dizziness and fatigue.[1]
Felodipine can exacerbategingivitis.[1]
Felodipine is metabolized bycytochrome P450 3A4, so substances that inhibit or activate CYP3A4 can strongly effect how much felodipine is present.[1]
CYP3A4 inhibitors, which increase the amount of felodipine available per dose, includecimetidine,erythromycin,itraconazole,ketoconazole,HIV protease inhibitors, andgrapefruit juice.[1][4]
CYP3A4 activators, which decrease the amount of felodipine available per dose, includephenytoin,carbamazepine,rifampicin,barbiturates,efavirenz,nevirapine, andSaint John's wort.[1]
Felodipine is acalcium channel blocker.[1] Felodipine has additionally been found to act as anantagonist of themineralocorticoid receptor, or as anantimineralocorticoid.[5]
Different calcium channels are present in vascular tissue and cardiac tissue; anin vitro study on human vascular and cardiac tissues comparing how selective various calcium channel blockers are for vascular compared to cardiac tissue found the following vascular/cardiac tissue ratios:mibefradil 41, felodipine 12;nifedipine 7,amlodipine 5, andverapamil 0.2.[6]: 172
Felodipine is a member of the 1,4-dihydropyridine class of calcium channel blockers.[6]: 20–21 It is a racemic mixture, and is insoluble in water but is soluble in dichloromethane and ethanol.[6]: 25
The Swedish company Hässle, a division ofAstra AB,discovered felodipine;[7] it filed a patent application in 1979 claiming felodipine as an antihypertensive drug.[8][9] Astra partnered this drug and others withMerck & Co. in the US under a 1982 agreement between the companies.[7] The drug was approved by the FDA in 1991 after a three-and-a-half-year review; the drug entered a very crowded market to included the other calcium channel blockersnifedipine,verapamil,nicardipine, andisradipine.[7] The FDA gave the drug a 1C rating, meaning that it found little difference between felodipine and the drugs already approved for the same use.[7]
In 1994 Astra AB and Merck changed their partnership to ajoint venture called Astra Merck,[10] and in 1998 Astra (by that time,AstraZeneca) bought out Merck's rights in the joint venture.[11]
The first generics became available in Sweden in 2003[12] and in the US in 2004.[13]: 155
In April 2016, AstraZeneca announced that they were selling the right to market felodipine in China to China Medical System Holdings for $310 million; AZ would continue to manufacture the drug.[14]
As of 2016, felodipine was marketed under many brand names worldwide: Auronal, Cardioplen, Catrazil, Dewei, Dilahex, Enfelo, Erding, Fedil, Fedisyn, Feldil, Felicipin, Felo, Felocard, Felocor, Feloday, Felodil, Felodin, Felodip, Felodipin, Felodipina, Felodipine, Felodipino, Felodistad, Felogard, Felohexal, Felop, Felopine, Felostad, Feloten, Felotens, Felpin, Flodicar, Flodil, Keliping, Keydipin, Lodistad, Modip, Munobal, Nirmadil, Parmid, Penedil, Perfudal, Phelop, Phenodical, Plendil, Plentopine, Polo, Presid, Preslow, Prevex, Renedil, Sistar, Splendil, Stapin, Topidil, Vascalpha, Versant, and XiaoDing.[15]
The combination of felodipine andcandesartan was marketed as Atacand.[15]
The combination of felodipine andramipril was marketed as Delmuno, Tazko, Triacor, Triapin, Triasyn, Tri-Plen, Unimax, and Unitens.[15]
The combination of felodipine andenalapril was marketed as Lexxel.[15]
The combination of felodipine andmetoprolol was marketed as Logimat, Logimax, and Mobloc.[15]
