Valsartan
Drug Nomenclature
Pharmacopoeias. In US.
The United States Pharmacopeia 31, 2008, and Supplements 1 and 2 (Valsartan). Store in airtight containers at a temperature of 25°, excursions permitted between 15° and 30°.
Suspension. The US licensed product information provides the following method for making 160 mL of a suspension containing valsartan 4 mg/mL:
• add 80 mL of Ora-Plus (Paddock, USA) to an amber glass bottle containing eight 80-mg tablets (Diovan, Novartis) and shake for at least 2 minutes
• allow to stand for at least 1 hour then shake again for at least 1 minute
• add 80mL of Ora-Sweet SF (Paddock, US) to the bottle and shake for at least 10 seconds
The suspension can be stored for 30 days at or below 30° or for up to 75 days at 2° to 8°.
Adverse Effects and Precautions
As for Losartan Potassium. Valsartan should be used with caution in patients with hepatic impairment, cirrhosis, or biliary obstruction.
Interactions
As for Losartan Potassium.
Pharmacokinetics
Valsartan is rapidly absorbed after oral doses, with a bioavailability of about 23%. Peak plasma concentrations of valsartan occur 2 to 4 hours after an oral dose. It is between 94 and 97% bound to plasma proteins. Valsartan is not significantly metabolised and is excreted mainly via the bile as unchanged drug. The terminal elimination half-life is about 5 to 9 hours. Following an oral dose about 83% is excreted in the faeces and 13% in urine.
Uses and Administration
Valsartan is an angiotensin II receptor antagonist with actions similar to those of losartan. It is used in the management of hypertension, to reduce cardiovascular mortality in patients with left ventricular dysfunction after myocardial infarction, and in the management of heart failure (see under Losartan Potassium).
Valsartan is given orally. After a dose the hypotensive effect occurs within 2 hours, reaches a peak within 4 to 6 hours, and persists for over 24 hours. The maximum hypotensive effect is achieved within 2 to 4 weeks.
In hypertension, valsartan is given in an initial dose of 80 mg once daily. This may be increased, if necessary to 160 mg once daily; the maximum dose is 320 mg once daily. A lower initial dose of 40 mg once daily may be used in elderly patients over 75 years, and in those with intravascular volume depletion.
In heart failure, valsartan is given in an initial dose of 40 mg twice daily. The dose should be increased, as tolerated, to 160 mg twice daily. In patients who have had myocardial infarction, valsartan may be started as early as 12 hours after the infarction in clinically stable patients, in an initial dose of 20 mg twice daily; the dose may be doubled at intervals over the next few weeks up to 160 mg twice daily if tolerated.
Valsartan should be used with caution in patients with hepatic or renal impairment and dose reduction may be required (see below).
Administration in children. Valsartan may be used for hypertension in children aged 6 to 16 years. US licensed product information recommends an initial dose of 1.3 mg/kg once daily (up to a maximum of 40 mg). The dose should be adjusted according to response, but doses above 2.7 mg/kg daily have not been studied. A suspension formulation may be used (see Suspension, above) but exposure to valsartan may be higher with the suspension than with tablets. There is no experience with valsartan in children with renal impairment (creatinine clearance below 30 mL/minute per 1.73 m2) and it should therefore not be used in such children.
Administration in hepatic or renal impairment. The elimination of valsartan may be reduced in patients with hepatic impairment or biliary obstruction and it should be used with caution, if at all, in such patients; dose reductions may be required. In the UK, valsartan is contra-indicated in patients with severe hepatic impairment, cirrhosis, or biliary obstruction. In mild to moderate hepatic impairment an initial dose of 40 mg once daily and a maximum dose of 80 mg once daily is recommended for hypertension, and the dose after myocardial infarction should not generally exceed 80 mg twice daily.
Tower doses of valsartan may also be considered in patients with renal impairment. In the UK, an initial dose of 40 mg once daily is recommended for the treatment of hypertension in patients with moderate or severe renal impairment (creatinine clearance less than 20 mL/minute). Doses may need to be reduced in patients with heart failure or after myocardial infarction if renal function deteriorates.
Preparations
The United States Pharmacopeia 31, 2008, and Supplements 1 and 2: Valsartan and Hydrochlorothiazide Tablets.
Proprietary Preparations
Argentina: Alpertan; Diovan; Redutensill; Sarval; Simultan;
Austria: Angiosan; Diovan;
Belgium: Diovane;
Brazil: Diovan; Tareg †;
Canada: Diovan;
Chile: Tareg; Valaplex; Vartalan;
Czech Republic: Diovan; Sarton †; Valsacor;
Denmark: Diovan;
Finland: Diovan;
France: Nisis; Tareg;
Germany; Cordinate; Diovan; Provas;
Greece: Dalzad; Diovan;
Hong Kong; Diovan;
Hungary: Diovan; Varexan;
India: Diovan; Starval;
Indonesia: Diovan;
Ireland: Diovan;
Israel: Diovan;
Italy: Rixil; Tareg; Valpression;
Japan: Diovan;
Malaysia: Diovan;
Mexico: Diovan;
The Netherlands: Diovan;
Norway: Diovan;
Philippines: Diovan;
Poland: Diovan;
Portugal; Diovan; Tareg;
Russia: Diovan;
South Africa: Diovan; Tareg;
Singapore: Diovan;
Spain: Diovan; Kalpress; Miten; Vals;
Sweden: Diovan;
Switzerland: Diovan; Provas;
Thailand: Diovan;
Turkey: Diovan;
United Kingdom (UK): Diovan;
United States of America (US and USA): Diovan;
Venezuela: Alsart; Diovan; Vasaten.
MuIti-ingredient
Argentina: Diovan A; Diovan D; Diovan Triple; Simultan D;
Austria; Co-Angiosan; Co-Diovan; Valsartan/HCTZ †;
Belgium: Co-Diovane;
Brazil: Cotaregl; Diocomb SI; Diovan Amlo; Diovan HCT;
Canada: Diovan HCT;
Chile: Tareg-D; Valaplex-D; Vartalan D;
Czech Republic: Co-Diovan; Copalia; Dafiro; Exforge; Imprida;
Denmark: Diovan Comp;
Finland: Diovan Comp;
France: Cotareg; Nisisco;
Germany; Co-Diovan; Cordinate plus; Provas comp;
Greece: Co-Dalzad; Co-Diovan; Copalia; Dafiro; Exforge;
Hong Kong; Co-Diovan;
Hungary: Diovan HCT; Varexan HCT;
Indonesia: Co-Diovan;
Ireland: Co-Diovan;
Israel: Co-Diovan;
Italy: Combisartan; Corixil; Cotareg;
Malaysia: Co-Diovan;
Mexico: Co-Diovan;
The Netherlands: Co-Diovan; Cotareg;
Norway: Diovan Comp;
Philippines: Co-Diovan;
Poland: Co-Diovan;
Portugal: Co-Diovan; Co-Tareg; Copalia; Dafiro; Imprida;
Russia: Co-Diovan;
South Africa: Co-Diovan;
Singapore: Co-Diovan;
Spain: Co-Diovan; Co-Vals; Kalpress Plus; Miten Plus;
Sweden: Diovan Comp;
Switzerland: Co-Diovan; Provas comp; Provas maxx;
Thailand: Co-Diovan;
Turkey: Co-Diovan;
UK: Co-Diovan; Exforge;
USA: Diovan HCT; Exforge;
Venezuela: Diovan HCT; Diovan/Amlibon; Vasaten HCT
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