COMPOSITION:
Each film coated tablet contains 40mg or 80mg Valsartan.
MECHANISM OF ACTION:
Rennin, Angiotensin, Aldosteron – system (RAAS) is the most effective hormone that regulates hypertension in the body.
The active hormone of the RAAS is angiotensin II, which is formed from angiotensin I through ACE. Angiotensin II has two receptor subtypes AT1, AT2. AT1 receptors are located in vasculature, myocardium, kidney and adrenal glomerulosa. Their blocking produces vasodilation, loss of salt and water to decrease plasma volume, and decrease myogenic activity.
Dio Sartive is a potent and selective angiotensin II antagonist on receptors type AT1 (20000 fold greater affinity than AT2 receptors).
Valsartan does not bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation.
According to new studies on angiotensin II antagonists, it does not bind on angiotensin II receptors but on nearby receptors, so it cannot be moved by high concentrations of Angiotensin II, and that proves its long effect.
Valsartan does not lead to release of bradykinin which cause cough which is combined with ACE inhibitors taking.
INDICATIONS:
Treatment of hypertension and to improve survival following myocardial infarction in clinically stable patients with symptoms of left ventricular failure and/or left ventricular systolic dysfunction.
Valsartan may be used also as an alternative to ACE inhibitors in the management of heart failure.
DOSAGE:
Dio Sartive can be given either with or without food.
For most patients: The recommended dose of Dio Sartive is 80mg once daily. The antihypertensive effect is present within 2 weeks and maximal effects are seen after 4 weeks. In some patients whose blood pressure is not adequately controlled, the dose can either be increased to 160mg, or a greater decrease in blood pressure may be achieved by adding in a thiazide diuretic. Dio Sartive may also be administered with other antihypertensive agents.
Intravascular volume depletion: (e.g. patients those treated with high dose diuretics, who are unable to have their dose of diuretic reduced), a starting dose of 40mg is recommended.
In patients over 75 years: A lower starting dose of 40mg once daily is recommended.
In renal impairment: No initial dose adjustment is required in patients with mild renal impairment (i.e. creatinine clearance 20-50ml/min). For patients with moderate to severe renal impairment (i.e. creatinine clearance less than 20ml/min) or patients on dialysis, a lower starting dose of 40mg once daily is recommended.
In patients with mild to moderate hepatic impairment: Treatment should commence at a dose of 40mg once daily. A daily dose of 80 mg should not be exceeded.
Myocardial infarction: Therapy may be initiated as early as 12 hours after myocardial infarction, initially 20mg twice daily increased over several weeks to 160mg twice daily (consider lower dose in moderate hepatic impairment).
In children: The safety and efficacy of the product have not been established in children and adolescents (below the age of 18 years).
SIDE EFFECTS:
Adverse reactions have been reported as mild and transient in nature.
Occasionally (1–10%):
Body as whole: Body as whole fatigue. Blood and lymphatic system neutropenia. Elevation of serum potassium (but rarely was this of clinical significance and no patient discontinued for hyperkalaemia).
Rarely (0.001–1%):
Respiratory system: Respiratory system cough and epistaxis. Minor elevation of creatinine and bilirubin was seen in controlled trails. Valsartan was associated with decrease in haemoglobin, haematocrit and neutrophils. Elevation of liver function.
CONTRAINDICATIONS:
Hypersensitivity to the drug or to any of its contents, pregnancy, severe hepatic impairment, cirrhosis and biliary obstruction.
DRUG INTERACTIONS:
Compounds which have been studied in clinical trials include cimetidine, warfarin, furosemide, digoxin, atenolol, indometacin, hydrochlorothiazide, amlodipine, glibenclamide. When valsartan co-administered with Cimetidine, the systemic exposure of valsartan may be marginally increased. A co-administration with glibenclamide may cause decrease in the systemic exposure to valsartan. Concomitant use of potassium-sparing diuretics (e.g. spironolactone, triamterene, amiloride), potassium supplements, or salt substitutes containing potassium may lead to increases in serum potassium. Co-medication is not advisable.
PRECAUTIONS:
- Mild to moderate hepatic impairment and renal impairment, a lower dose is recommended.
- Monitoring of blood urea and serum creatinine is recommended as safety measure.
- Serum potassium should be monitored in renally impaired or elderly patients if they are also taking potassium supplement.
- In patients receiving high doses of diuretics, symptomatic hypotension may occur in rare cases after initiation of therapy with the product.
EFFECTS ON ABILITY TO DRIVE AND USE MACHINES:
There are no data to suggest that the product affects the ability to drive or use machines. When driving vehicles or operating machines, it should be recognized that occasionally dizziness or weariness may occur during treatment with any antihypertensive agent.
USE IN PREGNANCY OR LACTATION:
When using in pregnancy during the second and third trimesters drugs that act directly on the rennin-angiotensin system, they can cause injury and even death to the developing fetus, so when pregnancy is detected, valsartan should be discontinued as soon as possible.
Lactation: Valsartan should not be used in lactating mothers.
PHARMACOKINETIC PROPERTIES:
Absorption of valsartan after oral administration is rapid, the reduction of blood pressure is achieved within 4-6 hours. The antihypertensive effect persists over 24 hours after dosing. The maximum reduction in blood pressure is generally attained within 2-4 weeks.