Product Overview
[Drug Name]
Generic Name: Valsartan Capsules
Trade Name: Jiafei
English Name: Valsartan Capsules
Chinese Pinyin: Valsartan Capsules
[Ingredients]
The active ingredient of this product is valsartan.
[Properties]
This product consists of white or off-white granules and powder.
[Indications]
It is indicated for mild to moderate essential hypertension.
[Dosage and Administration]
Recommended dose: 80 mg once daily. The dose is not affected by race, age, or gender. It can be taken with or without food (see Absorption). It is recommended to take the drug at the same time each day (e.g., morning).
A definitive antihypertensive effect is achieved within 2 weeks of treatment, and maximum efficacy is achieved after 4 weeks. If the antihypertensive effect is unsatisfactory, the daily dose can be increased to 160 mg or a diuretic can be added. No dose adjustment is required for patients with renal insufficiency (contraindications are for severe renal failure) or non-biliary, non-choledostatic hepatic insufficiency.
Valsartan can be used in combination with other antihypertensive drugs.
[Adverse Reactions]
In a placebo- and Diovan-controlled trial in 2,316 hypertensive patients, the overall incidence of adverse events (AEs) in the Diovan group was similar to that in the placebo group. In a 6-month, open-label extension trial of 320 mg of valsartan in 642 hypertensive patients, the overall incidence of adverse events was similar to that observed in the placebo-controlled trials. The table below shows the incidence of adverse reactions reported in 10 placebo-controlled trials in which patients received 10 to 320 mg of valsartan daily for up to 12 weeks. Of the 2,316 patients, 1,281 received 80 mg and 660 received 160 mg, respectively. The incidence of adverse reactions observed was independent of dose and duration of treatment; therefore, adverse reactions occurring at all doses were combined. The incidence of adverse reactions was not associated with gender, age, or race. All adverse reactions with an incidence rate (≥1%) are listed in the table below (regardless of whether they are related to the drug under study). This product also includes adverse drug reactions reported in patients with hypertension after marketing. The incidence is defined as follows: very common (≤1/10); common (≤1/100, 1/1000); uncommon (≤1/1000, 1/100); rare (≤1/10000, 1/1000); very rare (1/10000). Infections Common: Viral infections Uncommon: Upper respiratory tract infection, pharyngitis, sinusitis Very rare: Rhinitis Blood and lymphatic system disorders Common: Neutropenia Very rare: Thrombocytopenia Immune system disorders Very rare: Hypersensitivity reactions, including serum sickness Psychiatric disorders: Uncommon: Insomnia, decreased libido Ear and inner ear labyrinth disorders Uncommon: Vertigo Vascular disorders Very rare: Vasculitis Respiratory, chest and mediastinal disorders Uncommon: Cough Gastrointestinal disorders Uncommon: Diarrhea, abdominal pain Skin and subcutaneous tissue disorders Very rare: Rash, pruritus Musculoskeletal and connective tissue disorders Uncommon: Back pain Very rare: Arthralgia, myalgia Systemic disorders and administration site reactions Uncommon: Fatigue, asthenia, edema Laboratory findings: Valsartan rarely causes decreases in hemoglobin and hematocrit. In controlled clinical trials, 0.8% and 0.4% of patients treated with valsartan experienced significant decreases in hematocrit and hemoglobin (20%), respectively. In contrast, only 0.1% of patients treated with placebo experienced decreases in hematocrit and hemoglobin. In controlled clinical trials, neutropenia was observed in 1.9% of patients treated with valsartan and 1.6% of patients treated with ACE inhibitors. Significant increases in serum creatinine, potassium, and total bilirubin were observed in 0.8%, 4.4%, and 6% of patients treated with valsartan, respectively, and in 1.6%, 6.4%, and 12.9% of patients treated with ACE inhibitors, respectively. Elevated liver function tests may occasionally occur. No specific laboratory monitoring is required for patients with essential hypertension receiving valsartan.
[Contraindications]
Hypersensitivity to valsartan or any of the other excipients in this product. Pregnancy (see [Use in Pregnant and Lactating Women]).
[Precautions]
Hyponatremia and/or hypovolemia: Rarely, patients with severe sodium deficiency and/or hypovolemia (e.g., those taking high-dose diuretics) may experience symptomatic hypotension when starting treatment with this product. Correction of hyponatremia and/or hypovolemia, or reduction of the diuretic dose, should be performed before starting treatment. If hypotension occurs, the patient should be placed in a supine position and, if necessary, intravenous saline infusion should be administered. Treatment with this product should be resumed after blood pressure stabilizes. Renal Artery Stenosis: Short-term use of this drug in 12 patients with secondary renovascular hypertension caused by unilateral renal artery stenosis did not cause significant changes in renal hemodynamics, creatinine, and urea nitrogen (BUN). Since other drugs that act on RAAS may increase BUN and creatinine in patients with unilateral or bilateral renal artery stenosis, it is recommended to monitor BUN and creatinine as a safety measure. Renal insufficiency: No dose adjustment is required for patients with renal insufficiency. However, since there is no data on severe cases (creatinine clearance 10ml/min), caution is required when using this drug. Hepatic insufficiency: No dose adjustment is required for patients with hepatic insufficiency. Valsartan is mainly excreted in the bile in its original form, and excretion is reduced in patients with biliary obstruction (see [Pharmacokinetics]). Particular caution should be exercised when using valsartan in such patients. Effects on driving and operating machines: As with other antihypertensive drugs, patients taking this medication should exercise caution when driving or operating machinery.
[Use in Special Populations]
Precautions for Children:
The efficacy and safety of this product in children and adolescents (under 18 years of age) have not been studied.
Precautions for Pregnancy and Lactation:
Pregnancy: Given the mechanism of action of angiotensin II antagonists, harm to the fetus cannot be ruled out. There have been reports that angiotensin-converting enzyme inhibitors (a specific class of drugs that act on the RAAS) administered in utero during the second and third trimesters of pregnancy can cause damage to the developing fetus or lead to fetal death. In addition, retrospective data have shown a potential risk of birth defects when angiotensin-converting enzyme inhibitors are used during the first trimester of pregnancy. There have been reports of spontaneous abortion, oligohydramnios, and neonatal renal insufficiency when pregnant women inadvertently take valsartan. Similar to other drugs that act directly on the RAAS, this product should not be used by pregnant women (see Contraindications). For women of childbearing potential, physicians should inform them of the potential risks of this class of drugs during pregnancy when prescribing drugs that act on the RAAS. If pregnancy is discovered during medication, valsartan should be discontinued as soon as possible. Breastfeeding: It is unknown whether valsartan is excreted in human milk. Valsartan is excreted in the milk of lactating rats. Therefore, this product should not be used during lactation.
[Precautions for Elderly Patients]
Although systemic exposure to valsartan in the elderly is slightly higher than in younger individuals, this is not clinically significant.
[Drug Interactions]
No significant drug interactions have been observed clinically. The following drugs have been studied: cimetidine, warfarin, furosemide, digoxin, atenolol, indomethacin, hydrochlorothiazide, amlodipine, and glyburide. Because valsartan is largely metabolized, no clinical drug interactions have been observed with drugs that induce or inhibit the cytochrome P450 system. Although valsartan is largely bound to plasma proteins, in vitro studies have not shown interactions at this level with other plasma protein-bound drugs (such as diclofenac, furosemide, and warfarin). When used in combination with potassium-sparing diuretics (such as spironolactone, triamterene, and amiloride), potassium supplementation or the use of potassium-containing preparations may lead to elevated serum potassium levels. Therefore, caution is required when using these drugs together.
[Pharmacological Actions]
Mechanism of Action: Angiotensin II is an activator of the renin-angiotensin-aldosterone system (RAAS). It is formed by angiotensin I in response to angiotensin-converting enzyme (ACE). Angiotensin II binds to specific receptors on the cell membranes of various tissues. It has numerous physiological effects, including direct and indirect involvement in blood pressure regulation. Angiotensin II is a potent vasoconstrictor that exerts a direct pressor effect, promotes sodium reabsorption, and stimulates aldosterone secretion. Valsartan is an orally active, specific angiotensin (AT) II receptor antagonist. It selectively targets the AT1 receptor subtype, which is responsible for all known effects of angiotensin II. The AT2 receptor subtype is not associated with cardiovascular effects. Valsartan does not exhibit any partial agonist activity at the AT1 receptor. Valsartan has a 20,000-fold stronger affinity for the AT1 receptor than for the AT2 receptor. ACE converts angiotensin I to angiotensin II and degrades bradykinin. The angiotensin II receptor antagonist, valsartan, has no inhibitory effect on ACE and does not cause retention of bradykinin or substance P, thus not causing cough. Clinical trials comparing valsartan with ACE inhibitors demonstrated a significantly lower incidence of dry cough in the valsartan group (2.6%) compared with the ACE inhibitor group (7.9%) (P < 0.05). In a clinical trial of patients who developed dry cough after receiving ACE inhibitors, cough was reported in 19.5% of the valsartan group, 19.0% of the diuretic group, and 68.5% of the ACE inhibitor group (P < 0.05). Valsartan has no effect on other hormone receptors or ion channels known to play an important role in cardiovascular regulation. Efficacy: Valsartan lowers elevated blood pressure without affecting heart rate. In most patients, a single oral dose produces a blood pressure-lowering effect within 2 hours, reaching peak effect within 4-6 hours, and maintaining the antihypertensive effect for at least 24 hours after dosing. Maximum antihypertensive efficacy is achieved after 2-4 weeks of treatment and is maintained during long-term treatment. Combination with thiazide diuretics can further significantly enhance the antihypertensive effect. Abrupt discontinuation of valsartan treatment does not result in rebound hypertension or other clinical adverse events. In multiple-dose studies in hypertensive patients, valsartan had no significant effects on total cholesterol, fasting triglycerides, fasting blood glucose, or uric acid levels. Preclinical safety information: Preclinical safety studies in several animal models revealed no evidence of systemic or target organ toxicity, except for fetal toxicity in rabbits. In rats, administration of 600 mg/kg of valsartan during the last trimester of gestation and lactation resulted in slightly reduced survival and developmental delay in offspring (see Use in Pregnant and Lactating Women). The primary preclinical safety findings are due to the drug's pharmacological effects and are not clinically significant. No evidence of mutagenicity, clastogenicity, or carcinogenicity was found in mice and rats.
Storage: Keep sealed in a dark place.
Strength: 80 mg
Packaging: Plastic packaging, 80 mg x 14 tablets per box
Shelf life: 18 months.
Approval number: National Medicine Standard H20030035
Manufacturer: Dequan Pharmaceutical (Jiangsu) Co., Ltd. (formerly known as Yongxin Pharmaceutical Industry (Kunshan) Co., Ltd.)
