Indications
This medication is prescribed for:
- Reducing Cardiovascular Risk: Decreases the risk of cardiovascular death and hospitalizations for heart failure in patients with chronic heart failure (NYHA Class II-IV) and reduced ejection fraction.
- Pediatric Heart Failure: Treats symptomatic heart failure with systemic left ventricular systolic dysfunction in children aged one year and older.
- Combination Therapy: Used alongside other heart failure treatments, replacing angiotensin-converting enzyme inhibitors (ACEi) or other angiotensin receptor blockers (ARBs).
Pharmacology
This tablet combines two key components:
- Sacubitril: A neprilysin inhibitor, which increases levels of peptides like natriuretic peptides by inhibiting neprilysin via its active metabolite, LBQ657.
- Valsartan: An angiotensin receptor blocker (ARB) that selectively blocks the AT1 receptor, counteracting the effects of angiotensin II and reducing aldosterone release.
Dosage & Administration
- Adults with Heart Failure: Start with 49/51 mg twice daily, increasing to 97/103 mg twice daily after 2-4 weeks if tolerated.
- Patients with Specific Conditions: Reduce starting dose to 24/26 mg twice daily for those not previously on ACEi/ARB, with severe renal impairment, or moderate hepatic impairment.
- Pediatric Heart Failure: Doses are adjusted based on weight. Follow specific dosing guidelines for children aged one year and older.
Interaction
- Avoid Combination: Do not use with ACE inhibitors, aliskiren in diabetic patients, or other ARBs.
- Potassium-Sparing Diuretics: May increase serum potassium levels.
- NSAIDs: Risk of renal impairment may be elevated.
- Lithium: Increased risk of toxicity.
Contraindications
- Hypersensitivity: Contraindicated in patients allergic to any component.
- History of Angioedema: Not suitable for those with a history of angioedema from ACE inhibitors or ARBs.
- Concomitant Use: Avoid use with ACE inhibitors or aliskiren in diabetic patients.
Side Effects
- Common: Angioedema, hypotension, impaired renal function, hyperkalemia, cough, dizziness.
- Rare: Hepatic issues, anemia, blurred vision, increased pancreatic enzymes.
Pregnancy & Lactation
- Pregnancy: Safety not established; limited studies available.
- Lactation: Avoid use during breastfeeding due to minimal drug levels in milk.
Precautions & Warnings
- Angioedema: Monitor closely; avoid if there’s a history of angioedema.
- Hypotension: Monitor blood pressure and renal function; adjust dosage as needed.
- Hyperkalemia: Periodically check serum potassium levels, especially in at-risk patients.
Use in Special Populations
- Pediatric: Safety and effectiveness not established in children under one year.
- Geriatric: No significant pharmacokinetic differences observed in elderly patients.
- Renal Impairment: Adjust starting dose for severe renal impairment.
- Hepatic Impairment: No dose adjustment needed for mild hepatic impairment; not recommended for severe hepatic impairment.
Overdose Effects
- Symptoms: Likely to cause hypotension. Symptomatic treatment is recommended.
- Hemodialysis: Unlikely to remove due to high protein binding.
Storage Conditions
- Store: Keep in a dry place, below 30°C. Protect from moisture and keep out of reach of children.
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