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Isradipine

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Isradipine
Clinical data
Trade namesDynaCirc
AHFS/Drugs.comMonograph
MedlinePlusa693048
Pregnancy
category
  • C
Routes of
administration		Oral
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability15-24%
Protein binding95%
Metabolism100% Hepatic
Elimination half-life8 hours
Excretion70% Renal, 30% Fecal
Identifiers
  • 3-methyl 5-propan-2-yl 4-(2,1,3-benzoxadiazol-4-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.158.721 Edit this at Wikidata
Chemical and physical data
FormulaC19H21N3O5
Molar mass371.387 g/mol g·mol−1
3D model (JSmol)
  • O=C(OC)\C3=C(\N\C(=C(\C(=O)OC(C)C)C3c1cccc2nonc12)C)C
  • InChI=1S/C19H21N3O5/c1-9(2)26-19(24)15-11(4)20-10(3)14(18(23)25-5)16(15)12-7-6-8-13-17(12)22-27-21-13/h6-9,16,20H,1-5H3 checkY
  • Key:HMJIYCCIJYRONP-UHFFFAOYSA-N checkY
  (verify)

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.

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

Significant Drug Interactions

1. 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. [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

Further Reading and References

  1. ^ a b c d e ""Isradipine: Brands, Medical Use, Clinical Data"".
  2. ^ a b "Isradipine Side Effects".
  3. ^ ""Isradipine and Anzemet Drug Interactions"".
  4. ^ ""Isradipine and Onmel Drug Interactions"".
  5. ^ ""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.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  • 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.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  • 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.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  • 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.{{cite journal}}: CS1 maint: multiple names: authors list (link)
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