Therapeutic effect of Exforge 5/80mg

Exforge 5/80 is a commonly prescribed medication for chronic conditions in the elderly. What is Exforge and what are the therapeutic effects of Exforge 5/80mg?

1. What is Exforge 5/80 mg medication?

Exforge 5/80mg comprises Amlodipine 5mg and Valsartan 80mg. This 5/80mg formulation is presented as dark yellow, round, film-coated tablets with biconvex surfaces and beveled edges. For identification purposes, the tablets are debossed with "NVR" on one side and "NV" on the other.

2. Therapeutic effect of Exforge 5/80mg

Exforge 5/80mg is indicated for use in the treatment of essential hypertension. Exforge 5/80mg is a combination of two antihypertensive compounds with complementary mechanisms of action, providing enhanced blood pressure control in patients with essential hypertension. Amlodipine acts as a calcium channel blocker, and Valsartan is an angiotensin II receptor antagonist. The combined action of these two active substances provides a synergistic effect on blood pressure reduction, leading to a more pronounced decrease in blood pressure compared to monotherapy with either component.
The Amlodipine component of Exforge 5/80mg exerts its effect by inhibiting the transmembrane influx of calcium ions into both cardiac myocytes and vascular smooth muscle cells, relaxed vascular smooth muscle, resulting in a reduction of peripheral vascular resistance and a subsequent decrease in blood pressure. Preclinical data demonstrate that Amlodipine exhibits binding affinity for both dihydropyridine (DHP) and non-dihydropyridine (non-DHP).
Valsartan is a potent and specific, orally active angiotensin II receptor antagonist, it selectively blocks the AT1 receptor subtype, which is responsible for the known actions of angiotensin II. Plasma angiotensin II concentrations are increased following AT1 receptor blockade by Valsartan.
Pharmacokinetics of Individual Components:

• Amlodipine: Following oral administration, amlodipine as a single agent reaches peak plasma concentrations within 6-12 hours, with an absolute bioavailability estimated to be between 64% - 80%. Amlodipine crosses the placenta and is excreted in breast milk. Amlodipine undergoes extensive hepatic metabolism (90%) to inactive metabolites. The elimination half-life of amlodipine is 30-50 hours, with 60% of amlodipine metabolites eliminated via urine.
• Valsartan: Following oral administration, valsartan as a single agent reaches peak plasma concentrations within 2-4 hours, with an average absolute bioavailability of 23%. Valsartan does not distribute extensively into tissues but exhibits high binding to serum proteins (97%), primarily to serum albumin. Valsartan is primarily eliminated unchanged in feces (83%) and in urine (13%), with an elimination half-life of 6 hours.

Pharmacokinetics of the Valsartan/Amlodipine Combination: Following oral administration of Exforge 5/80 mg, peak plasma concentrations of valsartan are attained within 3 hours, while peak plasma concentrations of amlodipine are attained within 6-8 hours. The rate and extent of absorption of Exforge 5/80 mg are equivalent to the bioavailability of valsartan and amlodipine when administered as separate tablets.
 

3. Dosage and Administration of Exforge 5/80mg

Exforge 5/80 mg is administered orally. It should be taken with some water and can be taken with or without food. The recommended dose of Exforge is one tablet once daily. Exforge 5/80 mg may be used in patients whose blood pressure is not adequately controlled with amlodipine 5 mg or valsartan 80 mg monotherapy.
No dosage adjustment of Exforge 5/80 mg is necessary for patients with mild to moderate renal impairment; however, monitoring of potassium and creatinine levels is recommended in patients with moderate renal impairment during treatment.
In patients with mild to moderate hepatic impairment without cholestasis, the maximum recommended dose of valsartan is 80 mg, when hypertensive patients with hepatic impairment are eligible for amlodipine or Exforge, the lowest available dose of amlodipine monotherapy or the corresponding amlodipine component should be used.
Elderly patients (65 years and older): When hypertensive elderly patients are eligible for amlodipine or Exforge, the lowest effective dose of amlodipine monotherapy or the corresponding amlodipine component should be used.
Note: The above information regarding Exforge 5/80 mg dosage is for reference only. The actual dosage depends on the patient's condition and disease progression. Patients should consult their physician for the most accurate dosage regimen.

4. Management of Exforge 5/80mg Overdose

Overdosage of Exforge 5/80mg can result in pronounced hypotension, necessitating aggressive cardiovascular support, Vasopressor agents may be beneficial in restoring vascular tone and blood pressure if not contraindicated. In cases of recent ingestion, emesis or gastric lavage may be considered, administration of activated charcoal immediately or up to 2 hours post-amlodipine ingestion can significantly reduce amlodipine absorption. Intravenous administration of calcium gluconate may reverse the effects of calcium channel blockade.

5. Adverse Drug Reactions of Exforge 5/80mg

When receiving Exforge 5/80mg, Patients may experience the following adverse drug reactions:

• Common Adverse Reactions of Exforge 5/80mg : Nasopharyngitis, influenza, headache, edema, facial flushing, asthenia.
• Less Common Adverse Reactions of Exforge 5/80mg : Dizziness, somnolence, postural dizziness, paresthesia, vertigo, tachycardia, palpitations, orthostatic hypotension, cough, pharyngolaryngeal pain, diarrhea, nausea, abdominal pain, constipation, dry mouth, rash, erythema.

6. Contraindications of Exforge 5/80mg

Exforge 5/80mg is contraindicated in the following conditions:

• Hypersensitivity to amlodipine, valsartan, dihydropyridine derivatives, or any of the excipients listed in the excipient composition section.
• Severe hepatic impairment, cirrhosis, or cholestasis.
• Concomitant use of Exforge 5/80mg with aliskiren-containing products in patients with diabetes mellitus or renal impairment (glomerular filtration rate [GFR] < 60 mL/min/1.73m²).  
• Second and third trimesters of pregnancy.  
• Severe hypotension
• Shock (including cardiogenic shock).
• Left ventricular outflow tract obstruction.
• Hemodynamically unstable heart failure post-acute myocardial infarction.

7. Precautions for Exforge 5/80mg Use

Caution should be exercised when using Exforge 5/80mg in the following patient populations:

• Patients with sodium depletion or hypovolemia.
• If excessive hypotension occurs during Exforge 5/80mg therapy, the patient should be placed in a supine position, and if necessary, intravenous infusion of isotonic saline solution may be administered. Treatment should be continued once blood pressure has stabilized.
• Hyperkalemia: Caution is warranted with concomitant use of Exforge 5/80mg with potassium supplements, potassium-sparing diuretics, potassium-containing salt substitutes, or other drugs that may increase potassium concentrations. Frequent monitoring of serum potassium is recommended.  
• Patients with renal artery stenosis: Caution should be exercised when using Exforge 5/80mg for the treatment of hypertension in patients with unilateral or bilateral renal artery stenosis or renal artery stenosis in a solitary kidney.
• Patients with renal impairment: Data on the use of Exforge 5/80mg in severe renal impairment (creatinine clearance < 10 mL/min) are limited; therefore, caution is advised.
• Patients with hepatic impairment: Caution should be exercised when using Exforge 5/80mg in patients with mild to moderate hepatic impairment or biliary obstructive disorders.
• Angioedema: Exforge 5/80mg should be discontinued immediately in patients who develop angioedema. Re-administration of Exforge is contraindicated.
  Patients with heart failure/post-myocardial infarction: Caution should be exercised when using calcium channel blockers, including amlodipine as in Exforge 5/80mg, in patients with congestive heart failure due to a potential increased risk of future cardiovascular events and mortality.
• Patients with acute myocardial infarction: Caution should be exercised when using amlodipine in patients with aortic stenosis, mitral stenosis, or hypertrophic obstructive cardiomyopathy.
• Primary aldosteronism: Patients with primary aldosteronism should not be treated with valsartan.
• Dual blockade of the renin-angiotensin-aldosterone system (RAAS): Dual blockade of the RAAS through the combined use of angiotensin-converting enzyme inhibitors, angiotensin receptor blockers, or aliskiren is not recommended due to an increased risk of hypotension, hyperkalemia, and impaired renal function.
  Pregnancy: Like other agents that directly affect the renin-angiotensin-aldosterone system, Exforge 5/80mg should not be used during pregnancy.
• Lactation: It is unknown whether valsartan is excreted in human milk, but amlodipine has been reported to be excreted in human milk with unknown effects on the infant. Exforge 5/80mg is not recommended during breastfeeding.
   

8. Drug interactions of Exforge 5/80mg

Interaction of Exforge 5/80mg with other antihypertensive agents: Other antihypertensive agents (alpha-blockers, diuretics) and medications that may cause hypotension as adverse effects (such as tricyclic antidepressants, alpha-blockers for benign prostatic hyperplasia) may potentiate the hypotensive effect when used with Exforge 5/80mg.
Concomitant use of amlodipine with strong or moderate CYP3A4 inhibitors (protease inhibitors, azole antifungals, macrolide antibiotics, verapamil, or diltiazem) may significantly increase amlodipine concentrations.  
Concomitant use of angiotensin receptor blockers with agents acting on the renin-angiotensin system increases the incidence of hypotension, hyperkalemia, and changes in renal function compared to monotherapy.  
Caution is advised when using Exforge 5/80mg concomitantly with potassium supplements, potassium-sparing diuretics, potassium-containing salt substitutes, or other drugs that may increase potassium levels (e.g., heparin). Frequent monitoring of serum potassium is recommended.  
Exforge 5/80mg contains amlodipine 5mg and valsartan 80mg. It is indicated for the treatment of essential hypertension. To ensure effective use and avoid unwanted adverse effects, patients should strictly adhere to their physician's instructions.

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