Product Overview
[Drug Name]
Generic Name: Levoamlodipine Maleate Tablets
Trade Name: Xuanning
English Name: Levoamlodipine Maleate Tablets
Chinese Pinyin: Ma Lai Suan Zuo Xuan An Lv Di Ping Pian
[Ingredients]
The main ingredient of this product is levamlodipine.
[Properties]
This product is a white or off-white tablet.
[Indications]
1. Hypertension. This product can be used alone or in combination with other antihypertensive drugs. 2. Chronic stable angina and variant angina. This product can be used alone or in combination with other antianginal drugs.
[Dosage and Administration]
1. The initial dose for the treatment of hypertension is 2.5 mg (1 tablet) once daily; the maximum dose is 5 mg (2 tablets) once daily. The initial dose for frail or elderly patients, or those with hepatic insufficiency, is 1.25 mg (half a tablet) once daily. This dose may also be added to other antihypertensive drugs. Dose adjustments should be made based on individual patient response. Generally, dose adjustments should be initiated after 7–14 days. If clinically indicated, dose adjustments may be initiated sooner, provided the patient is under close observation.
2. The initial dose for the treatment of angina pectoris is 2.5–5 mg (1–2 tablets) once daily. Lower doses are recommended for elderly patients and those with hepatic impairment; the effective dose for most patients is 5 mg (2 tablets) daily.
[Adverse Reactions]
Common adverse reactions: 1. Autonomic nervous system: flushing. 2. General: fatigue. 3. Cardiovascular, general: edema. 4. Central and peripheral nervous system: dizziness, headache. 5. Gastrointestinal: abdominal pain, nausea. 6. Heart rate/rhythm: palpitations. 7. Psychological: drowsiness. No clinical laboratory abnormalities associated with this product were observed in clinical trials. Less common adverse reactions observed post-marketing include: 1. Autonomic nervous system: dry mouth, increased sweating. 2. General: Weakness, back pain, malaise, pain, weight gain/loss. 3. Cardiovascular, General: Hypotension, syncope. 4. Central and Peripheral Nervous System: Hypertonia, hypoesthesia/paresthesia, peripheral neuropathy, tremor. 5. Endocrine: Breast hyperplasia. 6. Gastrointestinal: Changes in bowel habits, dyspepsia (including gastritis), gingival hyperplasia, pancreatitis, vomiting. 7. Metabolic/Nutritional: Hyperglycemia. 8. Musculoskeletal: Arthralgia, muscle cramps, myalgia. 9. Platelets/Hemorrhage/Coagulation: Purpura, thrombocytopenic purpura. 10. Psychological: Impotence, insomnia, change in attitude. 11. Respiratory: Cough, dyspnea. 12. Skin/Appendages: Hair loss, skin discoloration. 13. Special Senses: Taste disturbances, tinnitus. 14. Urinary: Frequent urination. 15. Vascular (Extracardiac): Vasculitis. 16. Vision: Visual impairment. 17. Leukocyte/Reticuloendothelial System: Leukopenia. Hypersensitivity reactions are rare and include pruritus, rash, vasogenic edema, and erythema multiforme. There have been very rare reports of hepatitis, jaundice, and elevated transaminases (usually consistent with cholestasis). Severe cases requiring hospitalization have been reported in association with amlodipine use, but in most cases, a causal relationship has not been established. Similar to other calcium channel blockers, the following adverse reactions have been reported rarely, but these events are difficult to distinguish from the natural history of the underlying disease: myocardial infarction, arrhythmias (including bradycardia, ventricular tachycardia, and atrial fibrillation), and chest pain.
[Contraindications]
This product is contraindicated in patients with hypersensitivity to dihydropyridines or any of its components.
[Precautions]
1. Warning: A very small number of patients, particularly those with severe coronary artery obstructive disease, may experience increased frequency, prolonged duration, and/or worsening of angina pectoris, or acute myocardial infarction, when initiating or increasing the dose of calcium channel blockers. The mechanism of action is currently unknown. 2. Because the vasodilatory effect of this drug is gradual, rare cases of acute hypotension have been reported following administration of this drug. However, caution should be exercised when using this drug in combination with other peripheral vasodilators in patients with severe aortic stenosis. 3. Use in Patients with Heart Failure: Calcium channel blockers should be used with caution in patients with congestive heart failure. In a long-term, placebo-controlled study (PRAISE-2) in patients with non-ischemic heart failure (NYHA Class IV), although the incidence of worsening heart failure was not significantly different compared with placebo, there was an increase in reports of pulmonary edema associated with amlodipine. 4. Use in Patients with Impaired Hepatic Function: As with all calcium channel blockers, the half-life of this drug is prolonged in patients with impaired hepatic function. However, a recommended dose has not yet been established, so this drug should be used with caution. 5. Use in Patients with Renal Failure: Changes in amlodipine plasma concentrations are not correlated with the degree of renal impairment, so a normal dose can be used. This product cannot be dialyzed.
[Use in Special Populations]
Precautions for Pediatric Patients:
There are no data available for the use of this product in children.
Precautions for Pregnancy and Lactation:
There is a lack of research data on its use in pregnant women, but based on animal studies, this product should only be used in pregnant women when absolutely necessary. It is unknown whether this product is excreted in breast milk; lactating women taking this product should discontinue breastfeeding.
Precautions for the Elderly:
The time to peak plasma concentration of this product is similar in elderly and younger patients. Increased area under the curve (AUC) and prolonged elimination half-life in elderly patients result in a decreased elimination rate. Elderly patients have been reported to tolerate similar doses of amlodipine as well as younger patients. Therefore, a normal dose can be used in elderly patients. However, it is advisable to start with a lower dose and then gradually increase the dose.
[Drug Interactions]
Amlodipine is safe to be coadministered with the following medications: thiazide diuretics, α-adrenergic receptor blockers, β-adrenergic receptor blockers, angiotensin-converting enzyme inhibitors, long-acting nitrates, sublingual nitroglycerin, nonsteroidal anti-inflammatory drugs, antibiotics, and oral hypoglycemic agents. In vitro data from human plasma indicate that amlodipine does not affect the plasma protein binding of digoxin, phenytoin, warfarin, or indomethacin. Effects of Other Drugs on Amlodipine: Cimetidine: Coadministration with cimetidine did not alter the pharmacokinetics of amlodipine. Grapefruit Juice: Concomitant administration of 240 ml of grapefruit juice and 10 mg of amlodipine to 20 healthy volunteers did not significantly affect the pharmacokinetics of amlodipine. Aluminum/Magnesium (Antacids): Concomitant administration of aluminum/magnesium antacids with a single dose of amlodipine did not significantly affect the pharmacokinetics of amlodipine. Sildenafil (Viagra): A single 100 mg dose of sildenafil did not affect the pharmacokinetics of amlodipine in patients with essential hypertension. When the two drugs are used together, each drug exerts its antihypertensive effect independently. Effects of Amlodipine on Other Drugs: Atorvastatin: Coadministration of 10 mg of amlodipine and 80 mg of atorvastatin did not significantly alter the steady-state pharmacokinetic parameters of atorvastatin. Digoxin: Coadministration of amlodipine and digoxin did not alter plasma digoxin concentrations or renal clearance in normal volunteers. Ethanol: Single or multiple doses of 10 mg of amlodipine had no effect on the pharmacokinetics of ethanol. Warfarin: Coadministration of amlodipine and warfarin did not alter the prothrombin reaction time of warfarin. Cyclosporine: Pharmacokinetic studies have shown that amlodipine does not significantly alter the pharmacokinetics of cyclosporine. Drug/Laboratory Test Interactions: Unknown.
[Pharmacological Actions]
Pharmacological Action: Amlodipine is a calcium channel blocker (also known as a slow-channel blocker or calcium ion antagonist), which blocks the transmembrane entry of calcium ions into myocardial and vascular smooth muscle cells. Its antihypertensive mechanism is direct relaxation of vascular smooth muscle. The exact mechanism of angina relief is not fully determined, but it can dilate peripheral arterioles and coronary arteries, reduce total peripheral vascular resistance, and relieve coronary artery spasm. It reduces cardiac afterload, energy consumption, and oxygen demand, thereby relieving angina. Carcinogenicity, Mutagenicity, and Teratogenicity: Amlodipine was not shown to be carcinogenic in rats and mice when administered daily for two years at doses of 0.5, 1.25, and 2.5 mg/kg. The highest dose reached the maximum tolerated dose in mice, but not in rats (calculated based on the maximum recommended clinical dose of 10 mg in mg/m²). No drug-related mutagenicity was observed at the genomic or chromosomal levels. Amlodipine administration at a daily dose of 10 mg/kg (8 times the maximum recommended human dose) to male rats starting 64 days before mating and to female rats starting 14 days before mating did not affect reproductive capacity. No teratogenicity or other embryotoxic effects were observed in pregnant rats and rabbits given 10 mg/kg of amlodipine (8 and 23 times the maximum recommended human dose) during the period of major organogenesis. However, administration of 10 mg/kg of amlodipine to rats, starting 14 days before mating and continuing throughout the mating period and gestation, resulted in a significant decrease in litter size (approximately 50%), a significant increase in intrauterine mortality (approximately 5-fold), and prolonged gestation and delivery. Toxicity: Single doses of amlodipine up to 40 mg/kg and 100 mg/kg, respectively, can cause lethality in mice and rats. Single doses of 4 mg/kg or higher in dogs cause significant peripheral vasodilation and hypotension.
[Storage] Store in a dark, airtight container.
[Strength] 2.5mg (calculated as levamlodipine)
[Packaging] Aluminum-aluminum blister pack, 14 tablets/box.
[Expiry Date] 60 months.
[Approval Number] National Medicine Standard H20030690
[Manufacturer] CSPC Pharmaceutical Group Ouyi Pharmaceutical Co., Ltd.
