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ETC / RX - Cardiovascular system - OPEVALSART 40, 80, 160

COMPOSITION: Each film coated tablet contains:

Active ingredient:

Valsartan…… 40 mg/80 mg/160 mg.

Excipients: Microcrystalline cellulose, crospovidone, colloidal anhydrous silica, magnesium stearate, iron oxide red, opadry II white.


PHARMACODYNAMICS:

Valsartan is an orally active, potent, and specific angiotensin II receptor antagonist. It acts selectively on the AT1 receptor subtype, which is responsible for the known actions of angiotensin II. The increased plasma levels of angiotensin II following AT1 receptor blockade with valsartan may stimulate the unblocked AT2 receptor, which appears to counterbalance the effect of the AT1 receptor. Valsartan does not exhibit any partial agonist activity at the AT1 receptor and has much greater affinity for the AT1 receptor than for the AT2 receptor.

Valsartan does not inhibit ACE (also known as kininase II), which converts angiotensin I to angiotensin II and degrades bradykinin.


PHARMACOKINETICS:

Valsartan is rapidly absorbed after oral. Peak plasma concentrations of valsartan are reached in 2–4 hours. Mean absolute bioavailability is 23%. Valsartan is highly bound to serum proteins (94–97%), mainly serum albumin. Valsartan does not undergo extensive biotransformation. Only approximately 25% of absorbed drug is metabolised. About 70% of dose is eliminated in faeces and about 30% of dose is eliminated in urine, mainly as unchanged drug.


INDICATIONS:

  • Opevalsart is indicated for the treatment of hypertension, heart failure.
  • Opevalsart is indicated for the treatment of post-myocardial infarction. In clinically stable patients with left ventricular failure or left ventricular dysfunction following myocardial infarction.

ADMINISTRATION AND DOSAGE: Oral route.

Adult:

Hypertension: Start: 80-160 mg once a day if on monotherapy, use lower dose if on diuretic. The maximum dose is 320 mg/day.

Heart failure: Start: 40 mg twice a day; the dose may be increased to 80-160 mg twice daily, use lower dose if on diuretic. The maximum dose is 320 mg/day.

Post-myocardial infarction: Valsartan may be initiated as early as 12 hours after a myocardial infarction. The recommended starting dose of Valsartan is 20 mg twice daily. Patients may be uptitrated within 7 days to 40 mg twice daily, with subsequent titrations to a target maintenance dose of 160 mg twice daily, as tolerated by the patient.

Elderly:

No dose adjustment is required in elderly patients.

Renal impairment:

No dosage adjustment is required for patients with a creatinine clearance above 10 ml/min.

Hepatic impairment:

In patients with mild to moderate hepatic impairment without cholestasis, the dose of valsartan should not exceed 80 mg. Valsartan is contraindicated in patients with severe hepatic impairment and in patients with cholestasis.

Children:

Valsartan is not recommended for use in children below the age of 18 years due to a lack of data on safety and efficacy.


CONTRAINDICATIONS:

  • Hypersensitivity to valsartan or any component of the formulation.
  • Severe hepatic impairment, biliary cirrhosis and cholestasis.
  • Second and third trimester of pregnancy.

WARNINGS AND PRECAUTIONS:

  • Hyperkalemia: Concomitant use with potassium supplements, potassium-sparing diuretics, salt substitutes containing potassium, or other agents that may increase potassium levels (heparin, etc.) is not recommended.
  • Patients with intravascular volume depletion (e.g those taking high-dose diuretics).
  • Renal artery stenosis, severe renal impairment.
  • Kidney transplantation: There is currently no data on the safe use of valsartan in patients who have recently undergone kidney transplantation.
  • Primary hyperaldosteronism: Should not be treated with valsartan as their renin-angiotensin system is not activated.
  • Hepatic impairment: In patients with mild to moderate hepatic impairment without cholestasis, valsartan should be used with caution.
  • Myocardial infarction: The combination of valsartan with an ACE inhibitor is not recommended due to the risk for adverse events increased.
  • Heart Failure: The triple combination of an ACE inhibitor, a beta blocker and valsartan is not recommended due to the risk for adverse events increased.
  • Pregnancy: The use of Angiotensin II Receptor Antagonists is not recommended during pregnancy.
  • Lactation: Because no information is available regarding the use of valsartan during breastfeeding, valsartan is not recommended to be use during this period.
  • Driving vehicles or operating machinery.

SIDE EFFECTS:

Dizziness, headache, abdominal pain, back pain, sore throat, fatigue, upper respiratory infections, hypotension, hyperkalemia, myalgia, GI disturbances, dry cough, sinusitis, nausea, edema, arthralgia, palpitations, pruritus, rash, diarrhea, constipation, dry mouth, dyspepsia, flatulenceanxiety, insomnia, dyspnea, vertigo.

Rare: Angioedema, thrombocytopenia, hepatitis, rhabdomyolysis.

In case of an unexpected reaction, consult your physician.


INTERACTIONS:

  • Lithium: Reversible increases in serum lithium concentrations and toxicity have been reported during concurrent use of ACE inhibitors. Due to the lack of experience with concomitant use of valsartan and lithium, this combination is not recommended.
  • Potassium-sparing diuretics, potassium supplements, salt substitutes containing potassium  may increase potassium levels.
  • Concomitant use of valsartan and NSAIDs may lead to an increased risk of worsening of renal function and an increase in serum potassium.

OVERDOSAGE:

Overdose with valsartan may result in marked hypotension. If the ingestion is recent, vomiting should be induced. Otherwise, the usual treatment would be IV infusion of normal saline solution. Valsartan is unlikely to be removed by hemodialysis.

 


PRESENTATION:

Box of 3 blisters x 10 film coated tablets.

Storage: Store at temperature from 150C to 300C, in a dry place, protect from light.

Shelf-life: 36 months from the manufacturing date. Do not use after expiry date.