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The main ingredient of this product is valsartan.
Chemical name: (S) -N-valeryl-N-{[2 '-(1H-5-tetrazolyl) -4-diphenyl] -methyl} -valine.
Chemical Structure:

Dal (valsartan dispersible tablet), the indication is for the treatment of mild to moderate essential hypertension.

Drug Name

Dale

Drug type

Prescription drugs, medicines for medical workers' injuries

Use classification

Angiotensin receptor antagonist

Dara Ingredients

The main ingredient of this product is valsartan.
Chemical name: (S) -N-valeryl-N-{[2 '-(1H-5-tetrazolyl) -4-diphenyl] -methyl} -valine.
Chemical Structure:

Molecular formula: C ₂₄ H ₂₉ N ₅ O ₃
Molecular weight: 435.5

Dahlia traits

This product is a white tablet.

Dallas indication

Treatment of mild to moderate essential hypertension.

Dallas specifications

80mg

Dala usage dosage

Recommended dosage: This product is 80mg once a day. The dose has nothing to do with race, age, or sex. Can be taken with meals or on an empty stomach (see Absorption). It is recommended to take the medicine at the same time every day (such as in the morning). The exact antihypertensive effect was achieved within 2 weeks, and the maximum effect was achieved after 4 weeks. When the antihypertensive effect is not satisfactory, the daily dose can be increased to 160mg, or a diuretic can be added. Patients with renal insufficiency (severe renal failure are contraindicated) and non-biliary-derived, cholestatic liver dysfunction do not need to adjust the dose.

Valsartan can be used in combination with other antihypertensive drugs.

Dale adverse reactions

A placebo-controlled trial of 2316 patients comprehensively compared the side effects of this product with placebo. The following table shows the adverse reactions reported in 10 placebo-controlled trials, with patients taking valsartan 10-320 mg / day for up to 12 weeks. Of the 2316 patients, 1281 and 660 took 80mg and 160mg, respectively. The incidence of adverse reactions has nothing to do with the dosage and duration of medication. Therefore, the adverse reactions occurring at various doses are combined for statistics. The incidence of adverse reactions was not related to gender, age, or race. All adverse reactions with an incidence of 1% are listed in the table below (whether or not related to the drug under study).

Other adverse reactions with a incidence of less than 1% are: edema, weakness, insomnia, rash, and decreased libido. Whether these adverse reactions are causally related to valsartan treatment is unknown. After the product was put on the market, there were some rare reports, including: angioedema, rash, pruritus, and other hypersensitivity reactions such as allergic reactions such as serum disease and vasculitis.

Laboratory research results

Rarely, valsartan causes a decrease in hemoglobin and hematocrit. Clinical controlled trials found that hemoglobin and hematocrit were significantly reduced (20%) in the valsartan treatment groups by 0.8% and 0.4%, respectively. The placebo group was 0.1%.

Clinically controlled trials found that neutropenia was seen in 1.9% of valsartan-treated patients and 1.6% of ACEI-treated patients. Serum creatinine, potassium, and total bilirubin significantly increased in the valsartan group were 0.8%, 4.4%, and 6%, respectively, and in the ACEI group were 1.6%, 6.4%, and 12.9%. Occasionally elevated liver function indicators. Patients with essential hypertension do not need to monitor special laboratory indicators when receiving valsartan.

Dare taboo

People who are allergic to any ingredients.

Pregnancy (see Pregnancy and breastfeeding).

There is no experience with this product in patients with severe renal failure (creatinine clearance [10ml / min).

Dale Note

Low sodium and / or hypovolemia

In rare cases, patients with severe sodium deficiency and / or hypovolemia (such as: high-dose diuretics) may have symptomatic hypotension at the beginning of treatment with this product. Hyponatremia and / or hypovolemia should be corrected or diuretics should be reduced before medication. If hypotension occurs, the patient should lie supine, with intravenous saline if necessary. After stable blood pressure, resume the treatment of this product.

Renal artery stenosis

Twelve patients with secondary renal vascular hypertension due to unilateral renal artery stenosis who took this product for 4 days did not cause significant changes in renal hemodynamics, creatinine, and urea nitrogen (BUN). Because other drugs that act on RAAS may increase BUN and creatinine in patients with unilateral or bilateral renal artery stenosis, monitoring is recommended to ensure safety.

Renal insufficiency

Patients with renal insufficiency do not need to adjust the dose.

Liver dysfunction

Patients with liver dysfunction do not need to adjust the dose.

The dose of valsartan in patients with mild to moderate liver dysfunction should not exceed 80 mg / day.

Valsartan is mainly excreted from the bile as a prototype, and excretion is reduced in patients with biliary obstruction (see Pharmacokinetics). Valsartan should be used with particular care in such patients.

As with other antihypertensive drugs, patients should take care when driving and operating machines.

Drugs for pregnant women and lactating women

Early (first trimester of pregnancy): pregnancy type B

Animal experiments show no harm to the fetus

Mid and late (2nd, 3rd and 3rd trimesters of pregnancy): pregnancy type D

There is evidence of harm to human fetuses, but the benefits outweigh the disadvantages in terms of the treatment benefits the mother receives.

Given the mechanism of action of angiotensin II receptor antagonists, harm to the fetus cannot be ruled out.

The use of drugs that directly affect RAAS in the middle and late stages of pregnancy can cause fetal harm or death. The fetus begins to undergo renal perfusion from the second trimester of pregnancy, which depends on the development of the RAAS system. Therefore, the use of this product in the middle and late pregnancy increases the risk.

Similar to other drugs that directly affect RAAS, this product should not be used during pregnancy. If pregnancy is found during medication, valsartan should be discontinued as soon as possible.

All newborns who have been in contact with the drug in the uterus should be closely observed to ensure adequate urine output, prevent hyperkalemia, and monitor blood pressure. If necessary, use appropriate treatment measures (such as rehydration) to remove the drug.

Valsartan can be excreted from the milk of rabbits. At present, no studies have been conducted on lactating women, so this product is not suitable for lactating.

Dhaler medication for children

There are no related studies on the effectiveness and safety of this product in children. No child medication experience.

Dala medication for the elderly

Although the systemic exposure of elderly people after valsartan is slightly higher than that of young people, it has no clinical significance.

Dara drug interactions

No obvious drug interaction was found clinically. The following drugs have been studied: cimetidine, warfarin, furazomib, digoxin, atenolol, indomethacin, hydrochlorothiazide, amlodipine, and glibenclamide.
Since valsartan is hardly metabolized, it has not been clinically found to interact with drugs that induce or inhibit the cytochrome P450 system.
Although valsartan mostly binds to plasma proteins, in vitro experiments have not found that it interacts with other plasma protein-binding drugs (such as diclofenac, furosemide, warfarin) at this level.
When used in combination with potassium-sparing diuretics (such as spironolactone, ampicillin, amiloride), potassium supplementation or the use of potassium-containing preparations can lead to an increase in blood potassium concentration. Therefore, care should be taken when using the combination.
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Daluo overdose

Although there is no experience in the diagnosis and treatment of this product, its main symptom may be obvious hypotension. If the medication is not taken for a long time, vomiting treatment should be used, otherwise the normal treatment is given intravenous saline infusion. Hemodialysis cannot clear valsartan.

Daluo Pharmacology and Toxicology

Mechanism

The activator of the renin-angiotensin-aldosterone system (RAAS) is angiotensin II, which is formed by angiotensin I under the action of angiotensin converting enzyme (ACE). Angiotensin II binds to specific receptors on various tissue cell membranes. It has a variety of physiological effects, including direct or indirect involvement in blood pressure regulation. Angiotensin is a potent vasoconstrictor substance, which has a direct pressure-increasing effect, and can also promote sodium reabsorption and stimulate aldosterone secretion.

Valsartan is an orally effective specific angiotensin (AT) II receptor antagonist that selectively acts on the AT ₁ receptor subtype and produces all known effects. The AT ₂ receptor subtype is not associated with cardiovascular effects. Valsartan does not have any partial agonist activity at the AT ₁ receptor. Valsartan has a 20,000-fold stronger affinity for the AT ₁ receptor than the AT ₂ receptor.

ACE converts angiotensin I to angiotensin II and degrades bradykinin. Angiotensin II receptor antagonist valsartan has no inhibitory effect on ACE and does not cause retention of bradykinin or substance P, so it does not cause cough. Clinical trials comparing valsartan with ACE inhibitors confirmed that the incidence of dry cough (2.6%) in the valsartan group was significantly lower than that in the ACE inhibitor group (7.9%) (P [0.05). A clinical trial of patients with dry cough symptoms after receiving ACE inhibitors found that 19.5%, 19.0%, and 68.5% of patients in the valsartan group, diuretic group, and ACEI group had cough (P [0.05 ). Valsartan has no effect on other hormone receptors or ion channels known to play important roles in cardiovascular regulation.

Medicinal effect

Valsartan lowers elevated blood pressure without affecting heart rate.

For most patients, a single dose of antihypertensive effect occurs within 2 hours of oral administration, and the peak effect is reached within 4-6 hours. The maximum antihypertensive effect is achieved after 2-4 weeks of treatment, and the effect is maintained during long-term treatment. Combining with thiazide diuretics can further enhance the antihypertensive effect.

Sudden termination of valsartan treatment does not cause hypertension "bounce" or other side effects.

Valsartan does not affect total cholesterol, triglycerides, blood glucose, and uric acid levels in patients with hypertension.

Dara pharmacokinetics

absorb

Valsartan is absorbed rapidly after oral administration, and its absorption varies widely. The average absolute bioavailability is 23% (23 ± 7). The pharmacokinetic curve is linear within the dose range studied. Valsartan rarely causes accumulation when taken once daily, and plasma concentrations are similar in men and women.

Taking valsartan with meals reduced the AUC by 48% and the peak blood concentration ( _Cmax ) by 59%. Regardless of whether it was taken with a meal or not, blood levels after 8 hours were similar. The reduction of AUC or C _max has no significant effect on clinical efficacy.

distributed

Most of valsartan (94-97%) bound to serum proteins (mainly albumin) and reached steady state within 1 week. The steady-state distribution volume is about 17 liters, and plasma clearance is relatively slow (about 2 liters / hour) compared with liver blood flow (30 liters / hour).

Clear

Valsartan is metabolized in multiple exponential decay kinetics (alpha phase half-life [1 hour, terminal half-life approximately 9 hours).

Valsartan is mainly excreted as a prototype, with 70% excreted in feces and 30% excreted in urine.

Pharmacokinetics in special clinical situations

Seniors

Compared with young volunteers, the body tissue concentration of valsartan in some elderly (65 years) is slightly higher, but it has no clinical significance.

Patients with renal insufficiency

Since only 30% of valsartan is excreted from the kidney, there is no clear correlation between renal function and valsartan tissue concentration. Therefore, patients with renal insufficiency do not have to adjust the dose (for severe renal failure, see contraindications). Studies on dialysis patients have not been seen, but given the high binding of valsartan to serum proteins, it is unlikely to be cleared by dialysis.

Liver dysfunction

Approximately 70% of valsartan is excreted by the bile as a prototype, and valsartan is not biotransformed. Therefore, valsartan systemic tissue concentration is not related to liver dysfunction. For patients with non-biliary origin and cholestatic liver dysfunction, no dose adjustment is necessary. In patients with biliary cirrhosis or biliary obstruction, the AUC of valsartan is approximately doubled (see Precautions).

Dale storage

Store in a sealed, dry place (not exceeding 30 ° C).

Dallas Packaging

(1) Aluminum-plastic packaging, 7 pieces / board × 1 board / box;
(2) Aluminum-plastic packaging, 7 pieces / board × 2 plates / box.

Dale validity period

24 months.

Dallas Executive Standard

WS _1- (X-003) -2009Z

Dale Approval Number

National Medicine Standard H20050508

Dale Production Enterprise

Hainan Huanglong Pharmaceutical Factory Co., Ltd.

Dale approval date

August 29, 2006

Dale Revision Date

April 07, 2009 November 03, 2009