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Exforge 5/80 is a drug commonly found in prescriptions for the treatment of chronic diseases of the elderly. So what is Exforge and what is the use of Exforge 5/80mg?
1. What is Exforge 5/80 mg?
Exforge 5/80mg drug contains Amlodipine 5mg and Valsartan 80mg ingredients. The drug 5/80mg is formulated as a dark yellow, round, oblique film coated tablet, engraved with the word "NVR" on one side and the word "NV" on the other side.
2. Uses of Exforge 5/80mg
Exforge 5/80mg is indicated for use in the treatment of essential hypertension. Exforge 5/80mg is a combination of 2 antihypertensive compounds with an adjunctive mechanism to help control blood pressure in patients with essential hypertension. Amlodipine is an active ingredient in the group of calcium antagonists, and Valsartan is an active ingredient in the treatment of hypertension that belongs to the class of angiotensin II receptor antagonists. The combination of these two active ingredients has an additive effect on the treatment of hypertension, reducing blood pressure more strongly than when using each ingredient alone. The Amlodipine component of exforge 5/80mg acts by blocking the passage of calcium ions into the myocardium and vascular smooth muscle, directly relaxing vascular smooth muscle, reducing peripheral vascular resistance and hypotension. Experimental data show that Amlodipine binds to both dihydropyridine and non-dihydropyridine binding sites. Valsartan is a potent and specific oral angiotensin II receptor antagonist that selectively acts on the AT1 receptor responsible for the known effects of angiotensin II. The plasma concentration of angiotensin II is increased after the AT1 receptor is inhibited by the active substance valsartan.
Pharmacokinetics of each active ingredient:
Amlodipine: After oral administration, Amlodipine alone with therapeutic doses will reach peak concentrations after 6 - 12 hours, absolute bioavailability is calculated as 64 - 80 %. Amlodipine crosses the placenta and is likely to be excreted in human milk. Amlodipine is extensively (90%) metabolized in the liver to inactive metabolites. The half-life of Amlodipine is 30-50 hours, 60% of Amlodipine's metabolites are excreted in the urine. Valsartan: Following oral administration, valsartan alone will reach peak plasma concentrations in 2-4 hours, with a mean absolute bioavailability of 23%. Valsartan is not widely distributed into tissues but is strongly bound to serum proteins (97%), mainly to serum albumin. Valsartan is mainly excreted unchanged in the faeces (83%) and in the urine (13%), the half-life of Valsartan is 6 hours. Pharmacokinetics of the 2 active ingredients Valsartan/Amlodipine: Following oral administration of Exforge 5/80 mg, peak plasma concentrations of valsartan were reached 3 hours after dosing, peak plasma concentrations of amlodipine were achieved. achieved after using the drug after 6 - 8 hours. The rate and extent of absorption of Exforge 8/50 mg are comparable to the bioavailability of Valsartan and Amlodipine when administered as individual tablets.
3. Dosage of Exforge 5/80mg
Exforge 5/80mg is taken orally, should be taken with a little water, with or without food. The recommended dose of Exforge is 1 tablet per day. Exforge 5/80mg may be used in patients whose blood pressure is not adequately controlled with Amlodipine 5mg or Valsartan 80mg alone.
No dose adjustment of Exforge 5/80mg is necessary for patients with mild to moderate renal impairment, potassium and creatinine levels should be monitored in patients with moderate renal impairment during use.
In patients with mild to moderate hepatic impairment without cholestasis, the maximum recommended dose for valsartan is 80 mg; when hypertensive liver failure patients are eligible for Amlodipine or Exforge, a low dose should be used. most effective of Amlodipine monotherapy or of the corresponding Amlodipine component.
Elderly patients (65 years of age and older): when hypertensive liver failure patients are eligible for Amlodipine or Exforge, the lowest effective dose of Amlodipine monotherapy or of the corresponding Amlodipine component should be used. .
Note: The dose of Exforge 5/80mg above is for reference only, the dose depends on the condition and progression of the disease, to get the most accurate dose, the patient needs to consult the doctor. treating doctor.
4. What to do when using an overdose of Exforge 5/80mg?
Overdosage of Exforge 5/80mg causes hypotension, requiring active cardiovascular support for patients, vasoconstrictor drugs can be helpful in restoring vascular tone and blood pressure if there are no contraindications. use. If new to the drug may consider induction of vomiting or gastric lavage, use of activated charcoal immediately or use up to 2 hours after administration of Amlodipine significantly reduces the absorption of amlodipine. Intravenous calcium gluconate can reverse the effects of calcium channel blockade.
5. Exforge 5/80mg . side effects
When using Exforge 5/80mg drug, patients may experience undesirable effects of the drug:
Common side effects of Exforge 5/80mg drug: nasopharyngitis, flu, headache, edema, red hot flushing, weakness. Uncommon side effects of Exforge 5/80mg: Dizziness, somnolence, postural dizziness, paresthesia, dizziness, tachycardia, palpitations, orthostatic hypotension, cough, sore throat - bar management, diarrhea, nausea, abdominal pain, constipation, dry mouth, rash, erythema.
6. Contraindications of Exforge 5/80mg
Exforge 5/80mg is contraindicated in the following cases:
Hypersensitivity to the active ingredient Amlodipine, Valsartan, dihydropyridine derivatives or any of the excipients listed in the excipients section; Severe liver failure, cirrhosis or cholestasis; Use of Exforge 5/80mg concurrently with aliskiren-containing products in patients with diabetes mellitus or renal failure (glomerular filtration rate GFR < 60ml/min/1.73m2); Pregnant women in the second and third trimesters; Severe hypotension; Shock (including cardiogenic shock); Obstruction of the left ventricular outflow tract; Hemodynamically unstable heart failure after acute myocardial infarction.
7. Be careful when using Exforge 5/80mg
Be careful when using Exforge 5/80mg with the following subjects:
Patients with hyponatremia or volume depletion; If excessive hypotension occurs when taking Exforge 5/80mg, the patient should be placed in the supine position and, if necessary, intravenous isotonic saline solution, continuing treatment when blood pressure has stabilized; Hyperkalemia: Caution should be exercised when Exforge 5/80 mg is co-administered with potassium supplements, potassium-sparing diuretics, salt substitutes containing potassium or other drugs that may increase potassium levels. regular monitoring of potassium levels; Patients with renal artery stenosis: Exforge 5/80mg should be used with caution in the treatment of hypertension in patients with unilateral or bilateral renal artery stenosis, renal artery stenosis in a single kidney; Patients with renal impairment: There are no data on the use of Exforge 5/80mg for severe cases (creatinine clearance < 10ml/min), so it should be used with caution; Patients with hepatic impairment: Exforge 5/80mg should be used with caution in patients with mild to moderate hepatic impairment or with biliary obstruction; Angioedema: Exforge 5/80mg should be discontinued immediately in patients who develop angioedema; Exforge should not be reintroduced; Heart Failure/Post-Myocardial Infarction Patients: Care should be taken when using calcium channel blockers including Amlodipine such as Exforge 5/80mg in patients with congestive heart failure because of possible increased risk of cardiovascular events. and future mortality; Patients with acute myocardial infarction: Amlodipine should be used with caution in patients with aortic or mitral stenosis, obstructive hypertrophic cardiomyopathy; Primary hyperaldosteronism: patients with primary hyperaldosteronism should not be treated with Valsartan; Dual blockade of the renin-angiotensin-aldosterone system: Dual blockade of the renin-angiotensin-aldosterone system is not recommended through the combined use of angiotensin-converting enzyme inhibitors, angiotensin receptor blockers or aliskiren because of the increased risk of hypotension. blood pressure, hyperkalemia , impaired kidney function; Pregnancy: any other drugs that act directly on the renin-angiotensin-aldosterone system should not be used in pregnancy, including Exforge 5/80mg. Lactation: It is not known whether Valsartan is excreted in human milk but Amlodipine has been reported to be excreted in human milk with effects on the neonate of unknown; Exforge 5/80 mg is not recommended for use in breast milk. women who are breastfeeding.
8. Drug interactions of Exforge 5/80mg
Interactions of Exforge 5/80mg with other antihypertensive drugs: Antihypertensive drugs (alpha blockers, diuretics) and drugs that can cause adverse effects to lower blood pressure (drugs) Tricyclic antidepressants, alpha blockers in benign prostatic hyperplasia) may increase the antihypertensive effect when used with Exforge 5/80mg.
Concomitant use of amlodipine with strong or moderate inhibitors of CYP3A4 (protease inhibitors, azole antifungals, macrolide antibiotics, verapamil or diltiazem) may significantly increase amlodipine exposure. .
Concomitant use of angiotensin receptor blockers with drugs acting on the renin-angiotensin system increases the incidence of hypotension, hyperkalemia, and changes in renal function compared with monotherapy.
Caution should be taken when administering Exforge 5/80mg concurrently with potassium supplements, potassium-sparing diuretics, salt substitutes containing potassium or other drugs that may increase potassium levels (such as heparin), monitor regular potassium levels.
Exforge 5/80mg drug contains Amlodipine 5mg and Valsartan 80mg ingredients. The drug is indicated for use in the treatment of essential hypertension. To ensure effective use and avoid unwanted side effects, users need to strictly follow the instructions of the doctor.
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