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| Clinical data | |
|---|---|
| Trade names | DynaCirc |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a693048 |
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| Routes of administration | Oral |
| ATC code | |
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| Pharmacokinetic data | |
| Bioavailability | 15-24% |
| Protein binding | 95% |
| Metabolism | 100% Hepatic |
| Eliminationhalf-life | 8 hours |
| Excretion | 70% Renal, 30% Fecal |
| Identifiers | |
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| CAS Number | |
| PubChemCID | |
| DrugBank |
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| ChemSpider |
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| UNII | |
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| ChEMBL | |
| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.158.721 |
| Chemical and physical data | |
| Formula | C19H21N3O5 |
| Molar mass | 371.393 g·mol−1 |
| 3D model (JSmol) | |
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Isradipine (tradenamesDynaCirc,Prescal) is acalcium channel blocker of thedihydropyridine class. It is usually prescribed for the treatment ofhigh blood pressure in order to reduce the risk ofstroke andheart attack.
It was patented in 1978 and approved for medical use in 1989.[1]
Isradipine is given as either a 2.5 mg or 5 mg capsule.[2]
Common side effects include:[3]
Serious side effects include:[3]
It is advised that those using isradipine not takedolasetron (Anzemet), as both agents can cause a dose-dependentPR interval andQRS complex prolongation.[4]
Itraconazole (Onmel/Sporanox) exhibits a negativeinotropic effect on theheart and thus could spur an additive effect when used concomitantly with isradipine. Itraconazole also inhibits an importantcytochromeliver enzyme (CYP 450 3A4) which is needed tometabolize isradipine and othercalcium channel blockers. This will increaseplasma levels of isradipine and could cause an unintentional overdose of the medication. Caution is advised when administering both agents together.[5]
Tizanidine demonstratesanti-hypertensive effects and should be avoided in patients taking isradipine due to the possibility of synergism between both medications.[6]
Theantibioticrifampin lowered plasma concentrations of isradipine to below detectable limits.[2]
Cimetidine increased isradipine mean peak plasma levels. A downward dose adjustment may be necessary with this particular instance ofpolypharmacy.[2]
Severehypotension was reported withfentanylanesthesia when it was combined with other calcium channel blockers. Even though isradipine, another calcium channel blocker, has not been used in conjunction with fentanyl anesthesia in any studies, caution is advised.[2]
Symptoms of an isradipine overdose include:[2]
Isradipine contains a stereocenter and consists of two enantiomers, more preciselyatropisomers. This is a racemate, i.e. a 1: 1 mixture of (R)- and the (S)-forms:[7]
| Enantiomers of Isradipine | |
|---|---|
-Isradipin_Structural_Formula_V1.svg) CAS-Nummer: 84260-63-9 | -Isradipin_Structural_Formula_V1.svg) CAS-Nummer: 84260-64-0 |
