Candesartan; Uses, Dosage, Side Effects, Interactions, Pregnancy

Candesartan, Candesartan; Uses, Dosage, Side Effects, Interactions, Pregnancy, Rx Harun
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Candesartan is a synthetic, benzimidazole-derived angiotensin II receptor antagonist prodrug with antihypertensive activity. Candesartan selectively competes with angiotensin II for the binding of the angiotensin II receptor subtype 1 (AT1) in vascular smooth muscle, blocking angiotensin II-mediated vasoconstriction and inducing vasodilatation. In addition, antagonism of AT1 in the adrenal gland inhibits angiotensin II-stimulated aldosterone synthesis and secretion by the adrenal cortex; sodium and water excretion increase, followed by a reduction in plasma volume and blood pressure.

Candesartan is an angiotensin II receptor blocker used widely in the therapy of hypertension and heart failure. Candesartan is associated with a low rate of transient serum aminotransferase elevations and has been linked to rare instances of acute liver injury.

Candesartan lowers blood pressure by antagonizing the renin-angiotensin-aldosterone system (RAAS); it competes with angiotensin II for binding to the type-1 angiotensin II receptor (AT1) subtype and prevents the blood pressure increasing effects of angiotensin II. Unlike angiotensin-converting enzyme (ACE) inhibitors, ARBs do not have the adverse effect of a dry cough.

Mechanism of Action of Candesartan 

Candesartan selectively blocks the binding of angiotensin II to AT1 in many tissues including vascular smooth muscle and the adrenal glands. This inhibits the AT1-mediated vasoconstrictive and aldosterone-secreting effects of angiotensin II and results in an overall decrease in blood pressure. Candesartan is greater than 10,000 times more selective for AT1 than AT2. Inhibition of aldosterone secretion may increase sodium and water excretion while decreasing potassium excretion. Candesartan cilexetil is an ARB prodrug that is rapidly converted to candesartan, its active metabolite, during absorption from the gastrointestinal tract. Candesartan confers blood pressure lowering effects by antagonizing the hypertensive effects of angiotensin II via the RAAS. RAAS is a homeostatic mechanism for regulating hemodynamics, water, and electrolyte balance. During sympathetic stimulation or when renal blood pressure or blood flow is reduced, renin is released from granular cells of the juxtaglomerular apparatus in the kidneys. Renin cleaves circulating angiotensinogen to angiotensin I, which is cleaved by angiotensin converting enzyme (ACE) to angiotensin II. Angiotensin II increases blood pressure by increasing total peripheral resistance, increasing sodium and water reabsorption in the kidneys via aldosterone secretion, and altering the cardiovascular structure. Angiotensin II binds to two receptors: type-1 angiotensin II receptor (AT1) and type-2 angiotensin II receptor (AT2). AT1 is a G-protein coupled receptor (GPCR) that mediates the vasoconstrictive and aldosterone-secreting effects of angiotensin II.

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Angiotensin II is formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme (ACE, kininase II). 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. Its action is, therefore, independent of the pathways for angiotensin II synthesis. There is also an AT2 receptor found in many tissues, but AT2 is not known to be associated with cardiovascular homeostasis. Candesartan has a much greater affinity (>10,000-fold) for the ATI receptor than for the AT2 receptor. Blockade of the renin-angiotensin system with ACE inhibitors, which inhibit the biosynthesis of angiotensin II from angiotensin I, is widely used in the treatment of hypertension. ACE inhibitors also inhibit the degradation of bradykinin, a reaction also catalyzed by ACE. Because candesartan does not inhibit ACE (kininase II), it does not affect the response to bradykinin. Whether this difference has clinical relevance is not yet known. Candesartan does not bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation. Blockade of the angiotensin II receptor inhibits the negative regulatory feedback of angiotensin II on renin secretion, but the resulting increased plasma renin activity and angiotensin II circulating levels do not overcome the effect of candesartan on blood pressure.

Indications of Candesartan 

Conta Indications of Candesartan 

Dosage of Candesartan 

Strengths: 4 mg, 8 mg, 16 mg and 32 mg.

High Blood Pressure

  • Children 6 to <18 years of age: The recommended starting dose is 4mg once a day.
  • For patients weighing <50kg: In some patients whose blood pressure is not adequately controlled, your doctor may decide the dose needs to be increased to a maximum of 8mg once a day.
  • For patients weighing ≥50kg: In some patients whose blood pressure is not adequately controlled, your doctor may decide the dose needs to be increased to 8mg once a day or to 16mg once a day.
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Hypertension

  • Initial dose: 16 mg orally once a day
  • Maintenance dose: 8 to 32 mg/day orally in 1 to 2 divided doses
  • Maximum dose: 32 mg/day

Congestive Heart Failure

  • Initial dose: 4 mg orally once a day; double dose every 2 weeks, as tolerated, to target dose of 32 mg orally once a day

Pediatric Dose for Hypertension

1 to less than 6 years

  • Initial dose: 0.2 mg/kg/day orally in 1 to 2 divided doses
  • Maintenance dose: 0.05 to 0.4 mg/kg/day orally in 1 to 2 divided doses

6 to less than 17 years ,Less than 50 kg

  • Initial dose: 4 to 8 mg/day orally in 1 to 2 divided doses
  • Maintenance dose: 2 to 16 mg/day orally in 1 to 2 divided doses

Greater 50 kg

  • Initial dose: 8 to 16 mg/day orally in 1 to 2 divided doses
  • Maintenance dose: 4 to 32 mg/day orally in 1 to 2 divided doses

Side Effects of Candesartan 

The most common

Common

Rare

Drug Interactions of Candesartan 

Candesartan may interact with following drugs, supplements, & may change the efficacy of drugs

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Pregnancy & Lactation of Candesartan 

FDA Pregnancy Category D 

Pregnancy

Candesartan may cause severe harm to a fetus and should not be used during pregnancy. If you discover you are pregnant while taking this medication, stop taking it and tell your doctor at once. Women taking candesartan who are planning or trying to become pregnant should discuss other, more appropriate medications to control blood pressure with their doctor.

Lactation

It is not known if candesartan passes into breast milk. If you are a breastfeeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding.

The safety and effectiveness of using this medication have not been established for the treatment of hypertension in children less than 6 years of age and for the treatment of heart failure in children less than 18 years of age.

References

Candesartan, Candesartan; Uses, Dosage, Side Effects, Interactions, Pregnancy, Rx Harun

Candesartan, Candesartan; Uses, Dosage, Side Effects, Interactions, Pregnancy, Rx Harun

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