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Current heart failure treatment regimens require a combination of multiple drug classes to reduce the risk of death and hospital admission. One of them is a combination of Sacubitril and Valsartan such as Uperio 50mg. So how does Uperio 50mg work?
1. What is Uperio 50mg?
Drug Uperio 50mg is a medicinal product of Novartis Singapore Company, active ingredients include Sacubitril and Valsartan.
Uperio 50mg is produced as a film-coated tablet, the identification features of which include a light purple color, biconvex with beveled edges, one side engraved with the word "NVR" and the other side with the word "LZ".
2. What is the use of Uperio 50mg?
Uperio 50mg is indicated in the treatment of symptomatic heart failure in patients with systolic dysfunction. Uperio 50mg has been shown to reduce cardiovascular mortality and heart failure hospitalizations when compared with Enalapril (an angiotensin-converting enzyme inhibitor). Therefore, Uperio 50mg is often used in combination with other heart failure drugs and as an alternative to ACE inhibitors or receptor blockers (ARBs).3. Pharmacological characteristics of Uperio 50mg
Uperio 50mg works by both inhibiting Neprilysin via sacubitril (the active metabolite of sacubitril) and inhibiting the angiotensin II (AT1) receptor by the action of valsartan. Inhibition of Neprilysin stimulates increased concentrations of diuretic peptides (Natridiuretic peptides), thereby activating the membrane-bound Guanylyl cyclase receptor, leading to increased levels of Guanosin monophosphate (cGMP) and resulting in a range of beneficial effects. benefits such as:Vasodilation; Increased sodium and diuretic excretion; Increases glomerular filtration rate, increases blood flow through the kidneys; Inhibits renin and aldosterone release; Decreased sympathetic activity; Anti ventricular hypertrophy, anti fibrosis. In addition, the active ingredient Valsartan in Uperio 50mg inhibits the adverse cardiovascular and renal effects of angiotensin II through selective inhibition of the AT1 receptor, and also inhibits angiotensin II-dependent aldosterone release.
Pharmacokinetic characteristics of Uperio 50mg:
Absorption: After taking Uperio 50mg, the active ingredient Sacubitril will be converted into Sacubitrilat. Both sacubitril, sacubitrilat and valsartan reached peak plasma concentrations after 0.5 h, 2 h and 1.5 h, respectively. Food can reduce the concentration of valsartan in the blood but does not reduce the clinical effect; Distribution: Uperio 50mg is strongly bound to plasma proteins (about 94% - 97%); Metabolism: Sacubitril is converted to dacubitrilat by esterase, whereas only about 20% of a dose of Valsartan is metabolized. Uperio 50mg is poorly metabolized by CYP450; Elimination: After oral administration, 52-68% of sacubitril (mainly as sacubitril) and about 13% of valsartan are excreted in the urine, with the remainder excreted in the feces. Sacubitril, sacubitrilat and valsartan have half-lives of approximately 1.43 hours, respectively; 11.48 hours and 9.90 hours.
4. Dosage of the drug Uperio 50mg
Patients need to take the entire tablet of Upio 50mg with water, either before or after meals.
Dosage of Uperio 50mg in adults:
The starting dose of Uperio 50mg is 2 tablets/time (100mg) x 2 times/day. Then double the dose after 2-4 weeks to the target dose of 4 tablets/time (200mg) x 2 times/day depending on the patient's tolerance level; In case of problems with tolerability of Uperio 50mg (eg, systolic blood pressure less than 95 mmHg, symptomatic hypotension, hyperkalemia or renal dysfunction) the dose of the combination drug should be adjusted, the dose reduced temporarily. time or stop using Uperio 50mg; Uperio 50mg can be combined with other heart failure therapies, as an alternative to ACE inhibitors or angiotensin II receptor blockers (ARBs); Patients should start with 1 tablet once (50 mg) twice daily, then adjust the dose gradually (doubling after 3 to 4 weeks) if the patient has not previously taken an ACE inhibitor. (ACE) or angiotensin II receptor blocker (ARB) or use these drugs in low doses. Dosage of Uperio 50mg in some special subjects:
Renal failure: Depending on the degree of renal failure, the dose of Uperio 50mg should be adjusted accordingly, specifically as follows: Mild renal impairment (eGFR 60 - 90 ml/min/1.73) m2): No dose adjustment is required; Moderate or severe renal impairment (eGFR < 30 - 60ml/min/1.73m2): Initially 1 tablet/time x 2 times/day; End stage renal failure: Uperio 50mg is not recommended; Hepatic impairment: Adjust dose of Uperio 50mg according to the degree of liver failure: Mild hepatic impairment (Child-Pugh A): No need to adjust the dose of Uperio 50mg; Moderate hepatic impairment (Child-Pugh B) or liver enzymes AST/ALT above 2 times the upper limit: Initially 1 tablet x 2 times/day; Severe liver failure, cirrhosis or cholestasis (Child-Pugh C): Contraindicated with Uperio 50mg; Elderly: Adjust the dose of Uperio 50mg according to renal function; Children: Uperio 50mg is not recommended for children under 18 years of age.
5. Side effects of the drug Uperio 50mg
When using Uperio 50mg, patients may experience some unwanted side effects, the most common of which are the following:
Anemia; Hyper/hypokalemia; Hypoglycemia ; Uperio 50mg may cause dizziness, headache, fainting or postural dizziness; Orthostatic hypotension; A cough; Uperio 50mg may cause digestive disorders such as diarrhea, nausea or gastritis; CKD. Some other less common effects of Uperio 50mg:
Allergic or hypersensitivity; Skin itching, rash or angioedema.
6. Contraindications of Uperio 50mg
Hypersensitivity to Sacubitril, Valsartan or any of the ingredients in Uperio 50mg; Contraindicated use of Uperio 50mg concurrently or within 36 hours after stopping treatment with ACE inhibitors; History of angioedema due to ACE inhibitor or angiotensin II receptor blocker; Patients with a history of hereditary or idiopathic angioedema; Concomitant use of Uperio 50mg with Aliskiren is contraindicated in patients with diabetes mellitus or renal failure (eGFR less than 60 ml/min/1.73m2); Severe liver failure, cirrhosis or cholestasis; Uperio 50mg is not indicated in pregnant patients.
7. Precautions while using Uperio 50mg
Dual blockade of the Renin-Angiotensin-Aldosterone System (RAAS):
Do not use Uperio 50mg concurrently with an ACE inhibitor due to the increased risk of angioedema, and do not start this drug within 36 hours of the last dose of ACE inhibitors and vice versa; Caution should be exercised when administering Uperio 50mg with a direct renin inhibitor (such as Aliskiren); Concomitant use of Uperio 50mg with angiotensin receptor blockers is contraindicated due to the inclusion of valsartan in the composition of the drug. Risk of hypotension due to Uperio 50mg:
Treatment with Uperio 50mg should only be initiated when the patient has a systolic blood pressure above 100mmHg. Cases of systolic blood pressure less than 100 mmHg have not been studied using this drug; Uperio 50mg may cause symptomatic hypotension, especially in people over 65 years of age, with kidney disease or low systolic blood pressure (less than 112 mmHg); When initiating or adjusting the dose of Uperio 50 mg, the patient's blood pressure should be monitored regularly. If hypotension occurs, the dose may be temporarily reduced or Uperio 50 mg discontinued, and the dose adjustment of other heart failure drugs should be considered and the possible cause of the hypotension (eg, volume depletion) should be considered. due to diuretics, low salt diet, diarrhea or vomiting). Uperio 50mg and renal dysfunction:
Patients should be monitored for renal function regularly while taking Uperio 50mg. It should be remembered that the degree of renal failure is directly proportional to the possibility of lowering blood pressure; Uperio 50mg may cause decreased renal function, especially in patients with dehydration or concomitant use of non-steroidal anti-inflammatory drugs (NSAIDs). Uperio 50mg and hyperkalemia:
Do not initiate therapy and consider discontinuing Uperio 50mg if serum potassium is above 5.4 mmol/L because the drug can cause hyperkalemia (sometimes hypokalemia); Monitor blood potassium regularly during treatment with Uperio 50mg, especially in high-risk patients such as renal failure, diabetes mellitus, high potassium diet or taking anti-mineralocorticoid drugs; Patients with clinically significant hyperkalemia require a dose adjustment of concomitant medications or a temporary dose reduction or discontinuation of Uperio 50 mg. Uperio 50mg drug causes angioedema:
Patients with angioedema when taking Uperio 50mg should stop taking the drug immediately, and monitor and treat until the symptoms disappear and absolutely do not use Uperio 50mg again. Use of Uperio 50mg in patients with renal artery stenosis:
Uperio 50mg may increase blood urea and creatinine in patients with renal artery stenosis, so caution and regular monitoring of renal function is required. Use of Uperio 50mg in patients with NYHA class IV heart failure: Caution is advised when prescribing Uperio 50mg to this population due to limited clinical experience.
Uperio 50mg may cause dizziness and fatigue, so use caution when driving or operating machinery.
Use of Uperio 50mg during pregnancy: There have been reports of the effects of Uperio 50mg on fetal development, including spontaneous abortion, oligohydramnios, and neonatal renal dysfunction. mainly related to the active ingredient valsartan. Patients being treated with Uperio 50mg should stop as soon as pregnancy is detected and promptly notify their doctor.
Use of Uperio 50mg during lactation: It is not known whether Uperio 50mg is excreted in breast milk. Therefore, it is best not to prescribe this product to patients who are breastfeeding. However, breast-feeding may be discontinued if the use of Uperio 50mg is important to the mother.
8. Drug interactions of Uperio 50mg
Some contraindicated interactions of Uperio 50mg:
Angiotensin-converting enzyme (ACE) inhibitors increase the risk of angioedema; Aliskiren is contraindicated for the concomitant use of Uperio 50 mg in patients with type II diabetes. Drug interactions that do not recommend using the combination of Uperio 50mg:
Angiotensin II receptor blocker (ARB); Aliskiren if the patient has renal failure (glomerular filtration rate less than 60 ml/min/1.73 m2). Interactions to consider when combining Uperio 50mg:
Statins: In vitro, the active ingredient Sacubitril inhibits the transport proteins OATP1B1 and OATP1B3, resulting in increased plasma concentrations of statins. Therefore, the concomitant use of Uperio 50mg with Statins requires caution; PDE5 Inhibitors (Including Sildenafil): Caution should be exercised because of the risk of a stronger hypotension than single-drug therapy; Potassium: Using Uperio 50mg concurrently with potassium-sparing diuretics, mineralocorticoid receptor antagonists (Spironolactone, Eplerenone), potassium supplements... can increase blood potassium and creatinine levels; Non-steroidal anti-inflammatory drugs (NSAIDs): Concomitant use of Uperio 50mg increases the risk of progressive decline in renal function in elderly patients, with concomitant hypovolemia or pre-existing renal impairment; Lithium: Uperio 50mg can increase blood lithium levels and lead to toxicity, especially when combined with a diuretic; OATP and MRP2 transporters: Sacubitrilat) and Valsartan are substrates of OATP1B1, OATP1B3 and OAT3, and Valsartan is also an MRP2 substrate. Therefore, concomitant use of Uperio 50mg with OATP1B1, OATP1B3, OAT3 inhibitors (such as Rifampin, Cyclosporin) or MRP2 (such as Ritonavir) may increase the concentration of Sacubitrilat or Valsartan; Metformin: Uperio 50mg reduces the Cmax and AUC of Metformin when combined.
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