Losartan Potassium Tablets

1. Mechanism of action Angiotensin II is the main active substance of the renin-angiotensin system. It is a potent vasoconstrictor and plays a major role in the pathophysiological process of hypertension. Angiotensin II binds to AT1 receptors in various tissues (such as vascular smooth muscle, adrenal glands, kidneys and heart), producing a variety of important biological effects including vasoconstriction and aldosterone release. At the same time, it can also stimulate smooth muscle cell proliferation. It has been confirmed that another angiotensin II receptor subtype is AT2, but its role in the functional homeostasis of the cardiovascular system is still unclear. Losartan is a synthetic, potent orally active drug. Binding tests and pharmacological biological assays have shown that it can selectively bind to AT1 receptors. In vitro and in vivo studies have shown that losartan and its pharmacologically active carboxylic acid metabolite (E?3174) can block the corresponding physiological effects of angiotensin II synthesized from any source or any route. Compared with other peptide angiotensin II antagonists, losartan has no agonist effect. Losartan selectively acts on AT1 receptors, does not affect the functions of other hormone receptors or important ion channels in the cardiovascular system, and does not inhibit angiotensin converting enzyme (kininase II) that degrades bradykinin. Therefore, effects that are not directly related to blocking AT1 receptors, such as bradykinin-mediated effects or edema (losartan 1.7% placebo 1.9%), are not related to losartan. 2. Toxicology studies The LD50 of losartan potassium in male mice orally administered is 2248 mg/Kg (6744 mg/m3) (1124 times the recommended maximum daily dose for adults). The significant minimum lethal dose of this product in mice and rats orally administered is 1000 mg/Kg (3000 mg/m3) and 2000 mg/Kg (11800 mg/m3), respectively, which are 500 times and 1000 times the recommended maximum daily dose for adults (calculated based on a body weight of 50 kg). The potential toxicity of losartan potassium was evaluated by a series of toxicity tests with multiple oral administrations for three months in monkeys and one year in rats and dogs, and no toxicity was found to prevent the use of the drug at therapeutic dose levels. When rats and mice were given the maximum tolerated dose of this product, the observation time was up to 105 weeks and 92 weeks, respectively, and no carcinogenic effect of losartan potassium was found. In vitro alkaline elution tests and chromosome aberration tests showed that the use of losartan potassium at a maximum plasma concentration equivalent to 1700 times the recommended therapeutic dose for humans had no direct mutagenic effect. Male and female rats were given losartan potassium 150 and 300 mg/kg orally every day, respectively, and no effect on reproductive capacity was found. Losartan potassium can cause adverse reactions to rat embryos and newborns, including weight loss, death and/or nephrotoxicity. In addition, the concentrations of losartan potassium and its active metabolites in the milk of rats taking the drug were high.

The main ingredient of this product is losartan potassium. Chemical name: 2-butyl-4-chloro-1-[[2-(1H-tetrazolyl-5-yl)[1,1′-biphenyl]-4-yl]methyl]-H-imidazole-5-methanol monopotassium salt Molecular weight: C22H22ClKN6O

This product is a film-coated tablet, which appears white or off-white after removing the coating.

This product is suitable for the treatment of essential hypertension.

For most patients, the usual starting and maintenance dose is 50 mg once a day. The maximum antihypertensive effect can be achieved after 3 to 6 weeks of treatment. (See instructions for details)

Other adverse reactions reported after the product was marketed include: 1. Allergic reactions: Angioedema (including swelling of the larynx and glottis leading to airway obstruction, and/or swelling of the face, lips, pharynx and/or tongue) has been reported in a very small number of patients treated with losartan. Some of these patients had previously experienced angioedema due to taking other drugs, including ACE inhibitors. Vasculitis, including Henoch-Schönlein purpura, has been rarely reported. 2. Gastrointestinal reactions: Hepatitis (rarely reported), abnormal liver function, vomiting. 3. General disorders and administration site conditions: discomfort. 4. Blood system: anemia, thrombocytopenia (rarely reported). 5. Musculoskeletal system: myalgia, arthralgia. 6. Nervous/psychiatric system: migraine, grand mal seizures, taste disorders. 7. Reproductive system disorders: erectile dysfunction/impotence. 8. Respiratory system: cough. 9. Skin: urticaria, itching, erythroderma. Photosensitivity. 10. Hyperkalemia and hyponatremia have been reported.

It is contraindicated for those who are allergic to any ingredient of this product.

Precautions for children: The safety and effectiveness of the drug in children have not been established. Precautions for pregnancy and lactation: 1. Pregnant women use drugs that directly act on the renin-angiotensin system can cause damage to the developing fetus or even death when pregnant women use the drug in the middle and late stages of pregnancy. When pregnancy is discovered, this product should be discontinued as soon as possible. Although there is no experience of pregnant women using this product, animal studies using losartan potassium have demonstrated fetal and neonatal damage and death, and the mechanism is believed to be due to drug-mediated effects on the renin-angiotensin system. Renal perfusion of human fetuses from the middle of pregnancy depends on the development of the renin-angiotensin system. Therefore, if this product is used in the middle and late stages of pregnancy, the risk to the fetus will increase. 2. Precautions for lactating women: It is not known whether losartan is secreted in human milk. Since many drugs can be secreted in human milk and have adverse effects on breastfeeding infants, it is not known whether losartan is secreted in human milk. Precautions for the elderly: There is no age difference in the effectiveness and safety of this product in clinical studies.

In clinical pharmacokinetic studies, it has been confirmed that there are no clinically significant drug interactions with hydrochlorothiazide, digoxin, warfarin, cimetidine, phenobarbital, ketoconazole and erythromycin. Rifampicin and fluconazole have been reported to reduce the levels of active metabolites. The clinical consequences of these interactions have not been evaluated. 1. Like other drugs that inhibit angiotensin II and its effects, this product can cause increased serum potassium when used in combination with potassium-sparing diuretics (such as spironolactone, triamterene, amiloride), potassium supplements, or potassium-containing salt substitutes. 2. Like other drugs that affect sodium excretion, lithium excretion may be reduced. Therefore, if lithium salts are used in combination with angiotensin II receptor antagonists, serum lithium levels should be carefully monitored. 3. Nonsteroidal anti-inflammatory drugs (NSAIDs) include

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0.1g

36 months

Yangtze River Pharmaceutical Group Sichuan Hairong Pharmaceutical Co., Ltd.

• Founded in:

  2001-08-17

• Address:

  No. 802, South Section of Rainbow Avenue, Dujiangyan City, Chengdu City, Sichuan Province

• Tax NO.:

  91510181730231740X

• Registered Funds:

  50 million yuan

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