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. More recent research in animal models suggests that isradipine may have potential uses for treating Parkinson’s disease Chan et al. 2007.
Isradipine is given as either a 2.5mg or 5mg capsule. [1]
Side effects
Common side effects include: [2]
- 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: [2]
- Lightheadedness or fainting
- Shortness of breath, especially from minimal physical activity
- Swelling in the hands and feet
- Rapid and/or heavy heartbeat
- Chest pain
If you experience one or more of these serious side effects, contact your health care provider immediately.
Significant drug interactions
There are other interactions beyond those listed below. Make sure to speak with a Pharmacist or Doctor if you have any concerns.
Three major interactions are listed below.
1. It is advised that those using Isradipine not take Anzemet (Dolasetron), as both agents can cause a dose-dependent PR intervaland QRS complex prolongation. [3]
2. Onmel/Sporanox (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. [4]
3. Zanaflex (Tizanidine) demonstrates anti-hypertensive effects and should be avoided in patients taking Isradipine due to the possibility of synergism between both medications. [5]
4. The anti-biotic Rifadin (Rifampin) lowered plasma concentrations of Isradipine to below detectable limits. [1]
5. Tagamet (Cimetidine) increased Isradipine mean peak plasma levels. A downward dose adjustment may be necessary with this particular instance of polypharmacy. [1]
6. Severe hypotension was reported with Duragesic (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. [1]
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: [1]
- Lethargy
- Sinus tachycardia
- Transient hypotension
US 4466972
http://www.google.com.na/patents/US4466972
Further reading and references
- “”Isradipine: Brands, Medical Use, Clinical Data””.
- “Isradipine Side Effects”.
- “”Isradipine and Anzemet Drug Interactions””.
- “”Isradipine and Onmel Drug Interactions””.
- “”Isradipine and Zanaflex Drug Interactions””.
- 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.
synthesis………..will be updated
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
…………
References: Dihydropyridine calcium channel blocker. Prepn: P. Neumann, DE 2949491; idem, US 4466972 (1980, 1984 both to Sandoz). Prepn of enantiomers: A. Vogel, DE 3320616 (1983 to Sandoz), C.A. 101, 7162s (1984). Comparative study of in vitro effects on human and canine cerebral arteries: E. Müller-Schweinitzer, P. Neumann, J. Cereb. Blood Flow Metab.3, 354 (1983). Effect on a-adrenoceptor mediated vasoconstriction in rats: K. Jie et al., Arch. Int. Pharmacodyn. 278, 72 (1985). Pharmacokinetics: F. L. S. Tee, J. M. Jaffe, Eur. J. Clin. Pharmacol. 32, 361 (1987). Clinical evaluation in angina and coronary artery disease: C. E. Handler, E. Sowton, ibid. 27, 415 (1984); in hypertension: E. B. Nelson et al., Clin. Pharmacol. Ther. 40, 694 (1986). Comparison of hemodynamic effects of enantiomers: R. P. Hof et al., J. Cardiovasc. Pharmacol. 8, 221 (1986). Series of articles on pharmacology and clinical use: Am. J. Med. 86, 1-146 (1989).
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| Systematic (IUPAC) name | |
|---|---|
| 3-methyl 5-propan-2-yl 4-(2,1,3-benzoxadiazol-4-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate | |
| Clinical data | |
| Trade names | DynaCirc |
| AHFS/Drugs.com | monograph |
| MedlinePlus | a693048 |
|
|
| Legal status | |
| Routes | Oral |
| Pharmacokinetic data | |
| Bioavailability | 15-24% |
| Protein binding | 95% |
| Metabolism | 100% Hepatic |
| Half-life | 8 hours |
| Excretion | 70% Renal, 30% Fecal |
| Identifiers | |
| CAS number | 75695-93-1  |
| ATC code | C08CA03 |
| PubChem | CID 3784 |
| DrugBank | DB00270 |
| ChemSpider | 3652 |
| UNII | YO1UK1S598 |
| KEGG | D00349 |
| ChEMBL | CHEMBL1648 |
| Chemical data | |
| Formula | C19H21N3O5 |
| Molecular mass | 371.387 g/mol |
Filed under: GENERIC DRUG Tagged: isradipine
