Major indication:Mild to moderate primary hypertension.
Strength:80mg×7 Capsules/box, 80mg×10 Capsules/box
Dosage and Administration:orally, 1 capsule 1 times daily
Product Features :
Selectivity--- A direct role in AT, receptors, without the side effect of dry cough, antihypertensive does not rebound
Effectiveness---Effect for 24 hours
Safety--- The clinical side effects are similar to placebo
Protective--- Play a protective role of the heart, brain, kidneys and other organs
- Product details
Commom Name：Valsartan Capsules
English Name：Valsartan Capsules
Chinese Name：Xieshatan Jiaonang
Chemical Name：N-(1-oxopentyl)-N-[[2´-(1H-tetrazol-5-yl) [1,1´-biphenyl]-4-yl] methyl]-L-valine
【Description】This product is hard capsule, the contents of white particles and powder.
【Indications】Mild to moderate primary hypertension.
【Dosage and Administration】
Recommended dose of 80 mg, once a day. The dose has nothing to do with race, age
and gender. Take on table or an empty stomach. Suggest taking medicine at the
same time per day (such as the morning). Reach the exact antihypertensive effect
within two weeks, after four weeks can reach the best efficacy. Not satisfied
with the antihypertensive effect, the daily dose can be increased to 160 mg or
plus diuretics. Patients with renal insufficiency (serious renal failure see
taboo), non-duct-derived and without cholestatic of hepatic insufficiency don’t
need to adjust the dose. This product can be combined use with other
The literature shows that the adverse reactions of valsartan are mild, similar to placebo; Compared with the angiotensin converting enzyme (ACE) inhibitors, this product seldom cause cough. The drug's main side effects are headaches, dizziness, virus infection, upper respiratory tract infection, diarrhea, fatigue, dizziness etc., rare reports including angioneurotic edema, rash, itching and other hypersensitivity diseases such as serum sickness, vasculitis and other allergies reactions; Laboratory examination showed that very few patients with hemoglobin and hematocrit are reduced, neutrophil reduced, occasionally see serum creatinine, serum potassium, total bilirubin and the index of liver function increased.
【Contraindications】People are allergic to the components of this product; Patients with serious renal failure (creatinine clearance <10 ml / min).
1、Low sodium and / or hypovolemia: In very rare cases, patients with serious shortage of sodium and / or hypovolemia (such as: large doses of using diuretics), thestart treatment of using valsartan may appear symptomatic hypotension. Should correct the low sodium and / or hypovolemia before the use of drugs, or reduce the decrement of diuretics. If hypotension occurs, patients should be allowed to prostration, if necessary, venoclysis of physiological saline. Recover the treatment of valsartan after the stability of blood pressure.
2、Renal artery stenosis: Patients with renovascular hypertension which caused by unilateralrenal artery stenosis used valsartan for short-term, found no renal hemodynamics, creatinine, urea nitrogen (BUN) had statistical significance changes. Because other drugs act on RAAS may increase BUN and creatinine in patients with unilateral or bilateral renal artery stenosis, suggestion of monitoring to ensure safety.
3、Renal failure: Mild to moderate renal insufficiency patients do not need to adjust dosage.
4、Liver dysfunction: Liver failure patients do not need to adjust dose; The dose of valsartan in patients with mild to moderate liver failure should not exceed 80 mg / day; valsartan mainly excrete from bile by original shape, the excretion of patients with biliary obstruction is reduced (see Pharmacokinetics), to such patients should be particularly careful in the use of valsartan.
5、The same as other anti-hypertension drugs, patients in medication should be careful when driving or operating machines.
【Pregnancy and Lactation】
Fetus from the mid trimester of pregnancy began to appear renal perfusion, the latter depends on the development of RAAS system. The drugs application act directly on RAAS for pregnant women can cause fetus harm or death, so the pregnant women are prohibited from using valsartan. If found pregnancy during using the drugs, drugs should be stopped as soon as possible. All the newborns in utero had contact with drugs should be closely observed to ensure that sufficient amount of urine, preventing hyperkalemia and monitoringblood pressure, if necessary, take appropriate therapeutic measures to eliminate drugs. Valsartan can be excreted from the milk of rabbits. There is no research for breast-feeding women, so breast-feeding women are prohibited from using valsartan.
【Drug Used In Children】This product used for children's safety and efficacy has not yet been established.
【Drug Used In the Elderly】Although valsartan on the systemic impact on the elderly more than young people, but there is no clinical significance.
Clinical found no significant drug interactions. Now the following drugs has been researched: cimetidine, warfarin, furosemide, digoxin, atenolol, indomethacin, hydrochlorothiazide, amlodipine and glibenclamide. Because valsartan almost didn’t elapse metabolism, clinical research found no mutual influence between relevant drugs and this product on inducing or inhibiting the cytochrome P450 system. Although the majority of valsartan combines with plasma protein, but in vitro did not find at this level it has mutual influence with other plasma protein combined drugs (such as diclofenac, furosemide, warfarin).When combined application with potassium-sparing diuretic drugs (such as spironolactone, triamterene, amiloride), supplying potassium or using potassium preparation can lead serum potassium concentration increased. Therefore, the combined need extra attention.
Data of human drug overdose is limited, the main symptoms of excessive valsartan may be hypotension and tachycardia, bradycardia may appear stimulated by parasympathetic nerve. If appears symptom such as hypotension, support treatment should be processed. Valsartan can not be cleared by dialysis.
【Pharmacology and Toxicology】
1、Pharmacological effects：① valsartan is an orally effective, specific angiotensin Ⅱ (AT1)receptor antagonists, it selectively act on the AT1 receptor subtypes, blocking AngⅡ combined with AT1 receptor (the effect of specific antagonize AT1 receptor is more than AT2receptor about 20 times), thereby inhibiting vasoconstriction and the release of aldosterone, producing hypotensive effect. The drug is not in the role of angiotensin-converting enzyme (ACE), renin and other receptors, and do not inhibit the ion channels that related to blood pressure and the balance of sodium; This product doesn’t have inhibit effect on the angiotensin-converting enzyme, doesnot affect the level of Bradykinin in vivo, so the side effects which lead to cough less than angiotensin-converting enzyme inhibitors.② Valsartan reduces elevated blood pressure, does not affect heart rate simultaneously.③ For most patients, single-dose orally within two hours can cause the antihypertensive effect, four to six hours of peak effect, the effect of antihypertensive can maintain to 24 hours or more after dosing. Two to four weeks after the treatment will get the largest antihypertensive effect and maintain the effect during long-term treatment period. Combined with thiazide diuretic could further enhance the effect of antihypertensive.④ Suddenly terminate treatment of valsartan, not cause hypertension "Anti-jump" or other side effects.⑤ Valsartan does not affect the level of the total cholesterol, triglycerides, blood sugar and uric acid in patients with hypertension.
2、Toxicologic study:：① The toxicity of repeat administration: rats fed with valsartan monthly, dose were 60, 200, 600 mg / kg, three consecutive months, high-dose rats group, thewater intake and urine output slightly Increased, male rats mild glomerular proliferation and basophil cell increased, female rats glomerular afferent arteriole hypertrophy. After the recovery period not see unusual. Valsartan in rats fed with the highest dose of 200 mg / kg / day. For consecutive 12 months (some animals6 months), the highest orally dose of valsartan of a monkey is 120 mg / kg / day, had no adverse reactions.② Genetic toxicity: the results of the reverse mutation assay with microbestrains (Ames test),Chinese hamster V79cell gene mutation test, Chinese hamster ovary cells and rat chromosome test and rat cells cytogenetics test were negative.③ Reproductive toxicity: Pregnant rats or mice were for the orally dose of 600 mg / kg / day, pregnant rabbits orally dose get to 10 mg / kg / day, with no teratogenic effect. But rats in the formation of organs or late pregnancy and lactation period were given the dose of this product 600 mg / kg / day, it is clear that the weight of fetal rats dropped, fetal survival rate decreased, fetal development delayed. The rabbit fetal toxicity (absorbed fetus, litter size reduction, abortion and weight reduction) are related to the toxicity generated by mother-in-dose 5 mg / kg / day, 10 mg / kg / day. When mice were given 2200 and 600 mg / kg / day, rats and rabbits were given one of the largest 0.1, 6, 9 times of the recommended dose (expressed in patients with 60 kg weight, the dose of 320 mg / kg / day), don’t observe the adverse reactions.④ Carcinogenic: mice and rats were given this product of 160 and 200 mg / kg / day for successive two years, when respectively the largest recommended human dose (expressed in patients with60 kg weight, the dose of 320 mg / kg / day) of 2.6 and 6 times , no carcinogenic effect.
Valsartan was rapidly absorbed after oral, the plasma concentration get to the peak two tofour hours after administration, Valsartan Capsules absolute bioavailability of an average of 25 percent (10% -25%). Medication during the dinner can make the area under the curve (AUC) of valsartan decreased 40%, the peak plasma concentration (Cmax) reduced by 50%. In clinical dose of medication, the AUC and Cmax of valsartan increased with the dose linearly. Duplication in administration, no significant accumulation of plasma valsartan. Steady-state distribution volume of 17 liters of Valsartan after intravenous injection with, explains that the drug not widely distributed into the organizations. The combination rate of Valsartan and serum protein (mainly albumin) is very high (95 percent). Valsartan mainly excreted by the form of feces (dose of 83 percent) and urine (dose of 13 percent), the majority of prototype drugs, 20 percent for metabolites. The main metabolites for vaferyl 4-hydroxy valsartan, accounting for 9 percent of the administration. The plasma clearance rate of Valsartan is about 2 L / hour, renal clearance rate is 0.62 L / hour. Valsartan metabolized by multiple index decay dynamics, T1 / 2 α <1 hour, T1 / 2 β about nine hours. Under special clinic condition of the pharmacokinetics: ① The elderly: Compared with young people, elderly patients (> 65) the AUC of valsartan increased 70%, T1/2 extended 35 percent, but dose adjustment is not needed. ② Gender: gender had no effect on the pharmacokinetics of valsartan. ③ Patients with renal insufficiency: As only 30 percent of valsartan excreted from the kidney, and without a clear corelation between kidney function and the tissue concentration of valsartan. Therefore, the mild to moderate renal insufficiency patients do not have to adjust dosage (for serious renal failure patients, see taboo). Have not been study in serious renal dysfunction patients (creatinine clearance <10 ml / min), valsartan can not be cleared by dialysis, so serious kidney disease patients should pay attention to the dose. ④ Patients with liver dysfunction: about 70 percent valsartan excreted from bile by prototype, valsartan not elapse biotransformation, therefore, the whole body tissue concentration of valsartan has nothing to do with liver dysfunction. To non-duct-derived, without cholestatic liver failure patients do not have to adjust dosage. Biliary cirrhosis or biliary obstruction patients, the AUC of valsartan increased about 1 times (see notes).
【Storage】Preserved closeness, cool (not more than 20 ℃) and dry place.
【Package】Aluminum-plastic blister package, 7 granules / board / box, 10 granules / board / box.
【Perform Standard】《Chinese Pharmacopoeia》2010 Version 2.
【Approval Document Number】H.M.L.N. H20030035
Enterprise Name：Yung Shin Pharm.Ind.(Kunshan) Co.,Ltd.
Production Address：No.191 West Jin Yang Road, Lujia Town, Kunshan, Jiangsu 215331 Peoples Republic Of China