Candesartan

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[edit] BRAND NAMES

[edit] STRUCTURE

Candesartan.jpg

[edit] MECHANISM OF ACTION

Candesartan is an angiotensin II receptor antagonist.

Angiotensin II is formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme (ACE). Angiotensin II is the principal pressor agent of the renin-angiotensin system, with effects that include vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium.

Candesartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in many tissues, such as vascular smooth muscle and the adrenal gland.

[edit] INDICATIONS

  • Treatment of hypertension, alone or concomitantly with thiazide diuretics
  • Treatment of heart failure (NYHA Class II-IV) in adult patients who are receiving treatment with angiotensin converting enzyme (ACE) inhibitors or who cannot be given ACE inhibitors. (ACE inhibitors are considered first-line therapy in heart failure)

[edit] DOSAGE

  • Hypertension: In adults, the starting dose is 16 mg (when used as monotherapy) once daily with or without food. Dosage range is 8-32 mg once daily.
    Most of the antihypertensive effect is apparent within 2 weeks and maximal reduction is generally attained after 4 weeks.
  • Heart Failure: The usual recommended initial dose for treating heart failure is 4 mg once daily. The target dose is 32 mg once daily which is achieved by doubling the dose at approximately 2 week intervals, as tolerated by the patient. Candesartan can be administered with other heart failure treatments including ACE inhibitors, beta-blockers, diuretics, digoxin, and/or spironolactone.

[edit] DOSAGE FORMS AND STRENGTHS

Tablets: 4 mg, 8 mg, 16 mg, 32 mg.

[edit] CONTRAINDICATIONS

  • Known hypersensitivity (e.g., anaphylaxis or angioedema) to Candesartan
  • Contraindicated in patients with severe hepatic impairment.
  • Pregnancy; Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus
  • Do not co-administer Aliskiren with Candesartan in patients with diabetes

[edit] PRECAUTIONS

[edit] INTERACTIONS

  • Lithium clearance may be reduced. Serum lithium levels should be monitored carefully.
  • [[NSAIDS]]: Caution is advised if non steroidal antiinflammatory drugs NSAIDs are prescribed with angiotensin II receptor antagonists, including Candesartan. (Concomitant use of NSAIDS may result in decreased angiotensin II receptor antagonists effectiveness). In some patients with compromised renal function who are being treated with NSAIDS, the co-administration of angiotensin II receptor antagonists may result in further deterioration of renal function. Cases of acute renal failure, usually reversible, have also been reported.
  • Do not co-administer aliskiren with Candesartan in patients with diabetes
  • Drugs that inhibit the renin-angiotensin system can cause hyperkaliemia. Potassium-sparing diuretics and potassium supplements may have an additive effect on potassium retention, resulting in hyperkalemia.

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category D (US). Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus, thus Candesartan should not be used during pregnancy or in women planning to become pregnant and is not advisable to use in breast-feeding mothers. If pregnancy is detected during therapy, Candesartan should be discontinued as soon as possible.
  • Nursing Mothers: Choose to discontinue nursing or drug

[edit] SIDE EFFECTS

Common side effects are: Dizziness, Headache, Worsening of the kidney function (especially in patients with existing kidney problems or heart failure), Hypotension, Upper respiratory tract infection, Hyperkalemia (High levels of potassium in the blood) and back pain.

[edit] RELATED LINKS

[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)