Generic
Candesartan Cilexetil
4 brands available in the market
At a glance
Candesartan Cilexetil is an angiotensin receptor blocker (ARB) used in the treatment of hypertension and heart failure. It blocks angiotensin II AT1 receptors, dilating blood vessels and lowering blood pressure, which helps prevent heart attack and stroke.
Description
Candesartan Cilexetil is an ester prodrug that is hydrolysed in the body to the active form Candesartan during absorption from the gastrointestinal tract. Candesartan is an angiotensin II receptor (type AT1) antagonist. It 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 (e.g., vascular smooth muscle, adrenal gland).
Candesartan Cilexetil is indicated for hypertension, heart failure with impaired left ventricular systolic function, and prevention of diabetic nephropathy. It lowers blood pressure and reduces the risk of heart attack and stroke.
Indications
- Hypertension
- Heart failure (with impaired left ventricular systolic function)
- Prevention of diabetic nephropathy
Therapeutic class
Angiotensin-ll receptor blocker
Pharmacological class
Angiotensin II Receptor Blocker (ARB)
Pharmacology
Candesartan Cilexetil is a prodrug that is converted to active Candesartan after absorption. Candesartan acts as an AT1 receptor antagonist, blocking the vasoconstrictive and aldosterone-secreting effects of angiotensin II. It reduces peripheral vascular resistance to lower blood pressure and improves heart failure symptoms by reducing preload and afterload.
Mechanism of action
Candesartan selectively blocks AT1 receptors, preventing the vasoconstrictive effects of angiotensin II, thereby dilating blood vessels, lowering blood pressure, and reducing cardiac workload.
Dosage
Hypertension: Initially 8 mg once daily (2 mg for hepatic impairment, 4 mg for renal impairment or intravascular volume depletion). May increase every 4 weeks to max 32 mg/day. Usual maintenance dose: 8 mg once daily.
Heart failure: Initially 4 mg once daily; increase at intervals of at least 2 weeks to target dose of 32 mg once daily or max tolerated dose.
Children (1-6 years, <50 kg): 4-16 mg/day; adjust to 4-32 mg/day as needed.
Children (6-17 years): 8-16 mg/day; adjust to 4-32 mg/day as needed.
Hepatic impairment: Mild-moderate: Initially 4 mg/day; Severe: Contraindicated.
Renal impairment: Mild: No dose adjustment; Moderate: Initiate at lower dose.
Administration
May be taken with or without food, preferably at a fixed time each day. Swallow tablets whole; do not chew, crush, or break. Follow the dose and duration as advised by your physician.
Missed dose
If you miss a dose, skip it and continue with your normal schedule. Do not double the dose.
Side effects
Common side effects: Dizziness (especially with intravascular volume depletion), back pain, upper respiratory tract infection, sore throat, nasal congestion, vertigo, headache.
Uncommon: Hyperkalemia (occasionally), angioedema (rare), hepatitis, blood disorders, hyponatremia, arthralgia, myalgia, rash, urticaria, pruritus.
Side effects are usually mild.
Precautions & warnings
- Caution in renal artery stenosis, aortic or mitral valve stenosis, and obstructive hypertrophic cardiomyopathy.
- Monitor plasma-potassium concentration, especially in elderly and patients with renal impairment; lower initial doses may be appropriate.
- May cause dizziness for the first few days; rise slowly from sitting or lying position.
- Do not use during pregnancy (2nd and 3rd trimester) due to fetal harm.
- Do not stop suddenly (may cause rebound hypertension).
- Avoid anti-inflammatory drugs such as ibuprofen without consulting your doctor.
Contraindications
- Hypersensitivity to any component
- Pregnancy (2nd and 3rd trimester)
- Lactation
- Cholestasis
Drug interactions
- NSAIDs: May reduce antihypertensive effect and cause deterioration of renal function (including acute renal failure).
- Lithium: May increase serum lithium concentration.
- Potassium-sparing diuretics, potassium supplements, or salt substitutes containing potassium: Increased risk of hyperkalemia.
- Aliskiren (in diabetic patients): Increased risk of renal impairment, hypotension, and hyperkalemia (potentially fatal).
- Candesartan is not metabolized by CYP450, so interactions with CYP450 inhibitors or substrates are not expected.
Food interactions
Alcohol consumption is unsafe (increases risk of hypotension and dizziness).
Use in pregnancy
Unsafe during pregnancy (Category D). Definite evidence of risk to the developing baby (2nd and 3rd trimester). Discontinue as soon as pregnancy is detected. May be used in life-threatening situations if benefits outweigh risks.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Use in lactation
Probably safe during breastfeeding (if prescribed). Limited human data suggests the drug does not pose significant risk to the baby. However, caution is advised.
Pediatric use
Safety and efficacy in pediatric patients have not been established (under 18 years). Children 1-6 years: 4-16 mg/day (max 32 mg/day); Children 6-17 years: 8-16 mg/day (max 32 mg/day).
Geriatric use
Elderly patients may require lower initial doses; monitor plasma-potassium concentration.
Renal / hepatic impairment
Hepatic impairment: Mild-moderate: Initially 4 mg/day; Severe: Contraindicated.
Overdose effects
Overdose symptoms: Severe hypotension, dizziness, tachycardia, hyperkalemia, renal failure. Treatment: Gastric lavage, IV fluids, vasopressors, electrolyte monitoring. Hemodialysis is not effective. Consult your doctor immediately if overdose is suspected.
Storage conditions
Store in a cool and dry place, protected from light and moisture. Keep out of reach of children.
Chemical structure
Candesartan Cilexetil