Isradipine

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Isradipine.jpg

[edit] MECHANISM OF ACTION

Isradipine is a potent dihydropyridine calcium channel blocker. It inhibits the influx of extra cellular calcium across the peripheral arterial smooth muscle cell membranes by binding directly to inactive L-type calcium channels, stabilizing their inactive conformation.

The decrease in intracellular calcium inhibits the contractile processes of the systemic arteries smooth muscle cells, and thus, decreases total peripheral resistance and systemic blood pressure.

[edit] INDICATIONS

Treatment of hypertension

[edit] DOSAGE

The recommended dosage in mild to moderate hypertension is one 5 mg Modified Release Capsule (SRO) If 5 mg once a day is not sufficiently effective after at least 4 weeks of treatment, the addition of another antihypertensive agent is recommended (preferably a thiazide diuretic, ACE inhibitor or beta-blocker). Isradipine can also be added to existing antihypertensive treatment

[edit] CONTRAINDICATIONS

  • Known hypersensitivity to isradipine or to other calcium channel blockers of the dihydropyridine type
  • Cardiogenic shock
  • Unstable angina
  • During or within one month after myocardial infarction

[edit] WARNINGS AND PRECAUTIONS

  • Isradipine may lead to reflex tachycardia which, particularly in patients with severe obstructive coronary artery disease, may precipitate angina pectoris

[edit] INTERACTIONS

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US). Isradipine should be used during pregnancy only if clinically indicated and only if the expected benefit outweighs the potential risk to the fetus.
  • Nursing: It is unknown whether Isradipine is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when isradipine is administered to a breastfeeding woman.

[edit] SIDE EFFECTS

  • Most common: dizziness, headache, flushing, tachycardia, Skin rash or itching, palpitations and localised peripheral edema of non-cardiac origin (local arterial dilatation seems to be involved rather than fluid retention). These tend to disappear or to decrease as treatment continues.
  • Anaphylactic reactions (Very rare)

[edit] RELATED LINKS

Calcium Channel Blockers Pharmacology

[edit] BIBLIOGRAPHY

[edit] REFERENCES

Antihypertensives
ACE inhibitors Benazepril (Lotensin)   Captopril (Capoten)   Cilazapril   Delapril   Enalapril (Renitec, Vasotec)   Fosinopril (Monopril)  Lisinopril (Prinivil, Zestril)   Moexipril (Univasc)  Perindopril (Aceon)  Quinapril (Accupril)  Ramipril (Altace, Triatec)   Trandolapril (Mavik)  Zofenopril (Bifril, Zopranol)
Angiotensin II receptor antagonist Azilsartan (Edarbi)   Candesartan (Atacand)   Eprosartan (Teveten)   Irbesartan (Aprovel, Avapro, Karvea)   Losartan (Cozaar)   Olmesartan (Benicar, Olmetec)   Telmisartan (Micadis)   Valsartan (Diovan, Tareg)
Renin inhibitors Aliskiren (Rasilez, Tekturna)
Alpha-1 blockers Doxazosin (Cardura)   Prazosin (Minipress)   Terazosin (Hytrin)
Alpha-2 agonists (centrally acting) Clonidine (Oral route)   Clonidine (Transdermal) (Catapresan)   Guanfacine (Tenex)   Methyldopa (Aldomet)
Calcium channel blockers Dihydropyridines‎ Amlodipine (Norvasc)   Barnidipine (Vasexten)   Felodipine (Plendil)   Isradipine (Dynacirc)   Lacidipine (Lacipil, Motens)   Lercanidipine (Zanidip)   Manidipine   Nicardipine   Nifedipine (Adalat)   Nisoldipine   Nitrendipine
Benzothiazepine‎ Diltiazem (Cardizem, Taztia XT, Tiazac, Tildiem)
Phenylalkylamine‎ Gallopamil   Verapamil (Calan)
Beta blockers Beta1 selective (cardioselective) Acebutolol (Sectral)   Atenolol (Tenormin)   Betaxolol (Kerlon)   Bisoprolol (Concor)   Celiprolol (Cordiax)   Metoprolol (Betaloc, Lopressor, Toprol-XL)   Nebivolol (Bystolic, Lobivon, Nebilox)
Nonselective (Beta1 and Beta2 blockers) Oxprenolol (Trasitensin)   Propranolol (Inderal)   Timolol (Blocadren)
Nonselective (Beta1, Beta2 and Alpha1 blockers) Carvedilol (Dilatrend)   Labetalol (Trandate)
Beta blocker with intrinsic sympathomimetic activity (ISA) Acebutolol (Sectral)   Celiprolol (Cordiax)
Lipophilic Beta blockers Propranolol (Inderal)   Metoprolol (Betaloc, Lopressor, Toprol-XL)   Oxprenolol (Trasitensin)
Diuretics Carbonic anhydrase inhibitors Acetazolamide (Diamox)
Loop diuretics Bumetanide   Etacrynic acid   Furosemide (Lasix)   Piretanide   Torasemide (Demadex)
Thiazide diuretics Chlorothiazide (Diuril)   Hydrochlorothiazide (Esidrex)
Thiazide-like diuretics Chlortalidone (Hygroton)   Indapamide (Lozol, Lozide)   Metolazone
Potassium-sparing diuretics Epithelial sodium channel blockers: Amiloride (Midamor)   Triamterene (Dyrenium)
Aldosterone receptor antagonists: Potassium canrenoate   Eplerenone (Inspra)   Spironolactone (Aldactone)
Osmotic diuretics Mannitol
Combination therapy Amiloride/Hydrochlorothiazide (Moduretic)   Spironolactone/Hydrochlorothiazide (Aldactazide)