Isradipine (tradenames DynaCirc, Prescal) is a calcium channel blocker of the dihydropyridine class. It is usually prescribed for the treatment of high blood pressure in order to reduce the risk of stroke and heart attack.
It was patented in 1978 and approved for medical use in 1989.[1]
Contents
1Medical uses
2Side effects
3Drug interactions
4Overdose
5Stereochemistry
6References
7Further reading
8External links
Medical uses
Isradipine is given as either a 2.5 mg or 5 mg capsule.[2]
Side effects
Common side effects include:[3]
Dizziness
Warmth, redness, or tingly feeling under your skin
Headache
Weakness, tired feeling
Nausea, vomiting, diarrhea, upset stomach
Skin rash or itching
Serious side effects include: [3]
Lightheadedness or fainting
Shortness of breath, especially from minimal physical activity
Swelling in the hands and feet
Rapid and/or heavy heartbeat
Chest pain
Drug interactions
It is advised that those using Isradipine not take Anzemet (Dolasetron), as both agents can cause a dose-dependent PR interval and QRS complex prolongation.[4]
Itraconazole exhibits a negative inotropic effect on the heart and thus could spur an additive effect when used concomitantly with Isradipine. Onmel/Sporanox also inhibits an important cytochrome liver enzyme (CYP 450 3A4) which is needed to metabolize Isradipine and other Calcium Channel Blockers. This will increase plasma levels of Isradipine and could cause an unintentional overdose of the medication. Caution is advised when administering both agents together.[5]
Tizanidine demonstrates anti-hypertensive effects and should be avoided in patients taking Isradipine due to the possibility of synergism between both medications.[6]
The anti-biotic Rifampin 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 of polypharmacy.[2]
Severe hypotension was reported with Fentanyl anesthesia 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]
Note: There was no significant interaction between Isradipine and Warfarin (Coumadin), Isradipine and Microzide Hydrochlorothiazide, Isradipine and Lanoxin (Digoxin), and Isradipine and Nitrostat (Nitroglycerin).
Overdose
Symptoms of an Isradipine overdose include:[2]
Lethargy
Sinus tachycardia
Transient hypotension
Stereochemistry
Isradipine contains a stereocenter and consists of two enantiomers, more precisely atropisomers. This is a racemate, i.e. a 1: 1 mixture of ( R ) - and the ( S ) - Form:[7]
Enantiomers of Isradipine
CAS-Nummer: 84260-63-9
CAS-Nummer: 84260-64-0
References
^Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 465. ISBN 9783527607495.
^ abcde"Isradipine: Brands, Medical Use, Clinical Data".
^ ab"Isradipine Side Effects".
^"Isradipine and Anzemet Drug Interactions".
^"Isradipine and Onmel Drug Interactions".
^"Isradipine and Zanaflex Drug Interactions".
^Rote Liste Service GmbH (Hrsg.): Rote Liste 2017 – Arzneimittelverzeichnis für Deutschland (einschließlich EU-Zulassungen und bestimmter Medizinprodukte). Rote Liste Service GmbH, Frankfurt/Main, 2017, Aufl. 57, ISBN 978-3-946057-10-9, S. 193.
Further reading
Hattori T, Wang P (2006). "Calcium antagonist isradipine-induced calcium influx through nonselective cation channels in human gingival fibroblasts". Eur J Med Res. 11 (3): 93–6. PMID 16751108.
Ganz M, Mokabberi R, Sica D (2005). "Comparison of blood pressure control with amlodipine and controlled-release isradipine: an open-label, drug substitution study". J Clin Hypertens (Greenwich). 7 (4 Suppl 1): 27–31. doi:10.1111/j.1524-6175.2005.04450.x. PMID 15858400.
Johnson B, Roache J, Ait-Daoud N, Wallace C, Wells L, Dawes M, Wang Y (2005). "Effects of isradipine, a dihydropyridine-class calcium-channel antagonist, on d-methamphetamine's subjective and reinforcing effects". Int J Neuropsychopharmacol. 8 (2): 203–13. doi:10.1017/S1461145704005036. PMID 15850499.
Fletcher H, Roberts G, Mullings A, Forrester T (1999). "An open trial comparing isradipine with hydralazine and methyl dopa in the treatment of patients with severe pre-eclampsia". J Obstet Gynaecol. 19 (3): 235–8. doi:10.1080/01443619964977. PMID 15512286.
Chan CS, Guzman JN, Ilijic E, Mercer JN, Rick C, Tkatch T, Meredith GE, Surmeier DJ (2007). "'Rejuvenation' protects neurons in mouse models of Parkinson's disease". Nature. 447 (3): 1081–1086. doi:10.1038/nature05865. PMID 17558391.
External links
MedlinePlus DrugInfo medmaster-a693048
DDB 30003
Drug offers hope for Parkinson's - BBC News, 11 June 2007.
[1] - Commentary of Chan et al. publication
[2] - ArsTechnica - Why neurons die in Parkinson's patients
…patients with PD , supporting further trials to study its possible neuroprotective effect in PD . Isradipine, a dihydropyridine calcium channel antagonist used for the treatment of hypertension, has neuroprotective…
…repair of aortic coarctation . Dihydropyridine calcium channel blockers, such as nicardipine and isradipine, are potent peripheral vasodilators and are effective in the treatment of neonatal hypertension …
…and also slow cardiac contractility and conduction . The dihydropyridines, including nifedipine, isradipine, felodipine, nicardipine, nisoldipine, lacidipine, and amlodipine, are potent vasodilators that…
…suggest oral isradipine or, for older children and adolescents, clonidine Isradipine can be compounded into a stable liquid formulation for administration to infants and toddlers. If isradipine or clonidine …
…cells. Dihydropyridines (including nifedipine, amlodipine, felodipine, nicardipine, nisoldipine, isradipine, and lacidipine) are potent vasodilators that have little negative effect upon cardiac contractility…
English Journal
Structural studies of calcium channel blockers used in the treatment of hypertension - 1 H and 13 C NMR characteristics of nifedipine analogues.
Adaptation of Quality by Design-Based Development of Isradipine Nanostructured-Lipid Carrier and Its Evaluation for In Vitro Gut Permeation and In Vivo Solubilization Fate.
Alam T1, Khan S1, Gaba B1, Haider MF1, Baboota S1, Ali J2.
Journal of pharmaceutical sciences.J Pharm Sci.2018 Aug 1. pii: S0022-3549(18)30456-8. doi: 10.1016/j.xphs.2018.07.021. [Epub ahead of print]
