Product Overview
Generic name: Alendronate Sodium Vitamin D3 Tablets
Chinese Pinyin: ALunLinSuanNaWeiD3Pian
English name: Alendronate Sodium and Vitamin D3 Tablets
Product name: Formica
Ingredients: This product is a compound preparation, and its components are alendronate sodium and vitamin D3.
Properties: This product is white or off-white shaped tablets.
Indications: This product is suitable for:
1. Treat postmenopausal women with osteoporosis to increase bone mass and reduce the incidence of fractures, including hip and vertebral fractures (vertebral compression fractures).
2. Treat male osteoporosis to increase bone mass.
Specification: 70mg/2800IU*1 tablet
Dosage: This product must be taken with white water at least half an hour before eating, drinking or applying other medications for the first time each day (see Note: Adverse reactions in the upper gastrointestinal tract), because other beverages (including mineral water) , Food and some drugs may reduce the absorption of thiram (see note: adverse reactions in the upper gastrointestinal tract). Waiting for less than 30 minutes, or taking it with food, beverages (not white water) or other medicines will reduce the effect of alendronate due to reduced absorption. In order to deliver the medicine to the stomach as soon as possible and reduce the irritation to the esophagus, Formica should be taken with a full glass of white water (175-250ml) in the early morning, and at least 30 minutes after taking the medicine and before the first meal of the day, Patients should avoid lying down, and Fomega should not be taken at bedtime and before getting up early in the morning. Otherwise it will increase the risk of esophageal adverse events (see precautions for upper gastrointestinal adverse reactions).
If the dietary calcium intake is insufficient, the patient can supplement calcium supplements (see note: mineral metabolism).
For high-risk patients with vitamin D deficiency (such as those who are older than 70 years, breastfeeding or chronic diseases), in addition to taking formica, it may be necessary to increase the amount of vitamin D supplementation. For patients with gastrointestinal malabsorption syndrome, higher doses of vitamin D may be needed, and 25-hydroxyvitamin D levels may be considered. The recommended intake of vitamin D is 400IU-800IU/day. The purpose of alendronate vitamin D3 tablet is to provide the equivalent of 400IU of vitamin D per day when applied one tablet per week.
For the elderly or patients with mild to moderate renal insufficiency (creatinine clearance rate 35-60ml/min), dose adjustment is not required. Due to lack of relevant medication experience, it is not recommended to use alendronate sodium vitamin D3 tablets in patients with more severe renal insufficiency (creatinine clearance <35ml/min).
The recommended dosage for treating osteoporosis in postmenopausal women is thiram once a week, one tablet each time.
The recommended dose for treatment of male osteoporosis to increase bone mass is thiram, one tablet at a time.
Adverse reactions: A five-year clinical study of alendronate (FOSAMAX) has shown that adverse events related to alendronate (FOSAMAX) are generally mild and usually do not need to stop treatment.
Systemic reactions: allergic reactions, including urticaria and rare angioedema. Transient myalgia, discomfort and fatigue symptoms have been reported after taking alendronate, and fever is rare, usually related to initial treatment. In the presence of triggering conditions, rare hypocalcemia can occur. Peripheral edema is rare.
Gastrointestinal tract: nausea, vomiting, esophagitis, esophageal erosion, esophageal ulcer, rare esophageal stricture or perforation, and oropharyngeal ulcer. There have been reports of gastric or duodenal ulcers, some of which are more serious with complications.
There are occasional reports of localized osteonecrosis of the jaw, which may be related to delayed healing of tooth extraction and/or local infection (including osteomyelitis) (see [Precautions] Osteonecrosis of the jaw).
Musculoskeletal: bone, joint and/or muscle pain, rarely serious and/or disabling (see [Precautions]); joint swelling, musculoskeletal pain.
Nervous system: dizziness, vertigo, dysgeusia.
Skin: rash (occasionally with photosensitivity), itching, and hair loss. Rare and serious skin reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis.
Special sensation: rare uveitis, scleritis or episcleritis.
Contraindications: 1. Esophageal abnormalities that lead to delayed esophageal emptying, such as stenosis or flaccidity
2. Those who cannot stand or sit upright for at least 3 minutes · Hypocalcemia (see Notes on Mineral Metabolism)
3. Those who are allergic to any ingredient of this product.
Matters needing attention: mineral metabolism
Alendronate
Before starting treatment with this product, hypocalcemia must be corrected (see [Contraindications]). Other diseases that can affect mineral metabolism (such as vitamin D deficiency) should be effectively treated. For these patients, during the treatment with this product, serum calcium and symptoms of hypocalcemia should be monitored.
It is speculated that it may be due to the effect of alendronate sodium to increase bone density, and a mild asymptomatic decrease in serum calcium and phosphorus levels may occur.
Vitamin D3
This product should not be used alone to treat vitamin D deficiency (usually defined as 25-hydroxyvitamin D levels below 9 ng/mL). Patients at high risk of vitamin D deficiency may require a higher dose of vitamin D supplementation. For patients with gastrointestinal malabsorption syndrome, higher doses of vitamin D may be needed, and 25-hydroxyvitamin D levels should be considered.
For patients with diseases related to overproduction of 1,25 dihydroxyvitamin D (such as leukemia, lymphoma, sarcoidosis), supplementation of vitamin D3 may aggravate hypercalcemia and/or hypercalciuria. In these patients, blood calcium and urine calcium levels should be monitored.
Musculoskeletal pain
According to post-marketing experience reports, in patients using bisphosphonates (approved for the prevention and treatment of osteoporosis), severe bone, joint and/or muscle pain has occasionally occurred (see [Adverse Reactions]). Among these drugs is Alendronate (FOSAMAX). Most patients are postmenopausal women. The time from the application of the drug to the onset of symptoms varies from one day to several months. If severe symptoms occur, it should be stopped. Symptoms relieved in most patients after stopping the drug. After reusing the same drug or other bisphosphonates, some patients may experience symptoms again.
In a small number of patients receiving long-term bisphosphonate treatment (usually more than three years), low-energy fractures of the femur and proximal femoral shaft have been reported. Some are non-traumatic stress fractures (some reports are also called incomplete fractures). Several weeks to months before the occurrence of a complete fracture, some patients develop prodromal pain in the affected area, often accompanied by imaging features of stress fractures. Approximately one-third of patients have bilateral fractures, so patients who have experienced a stress fracture of the femoral shaft should examine the contralateral femur. Stress fractures with similar clinical features also occur in patients not receiving bisphosphonate treatment. Patients suspected of having a stress fracture should be evaluated, including evaluation of known causes and risk factors (such as vitamin D deficiency, malabsorption, glucocorticoid use, previous stress fractures, arthritis or fractures of the lower extremities, excessive activity or activity Increased volume, diabetes, long-term alcohol abuse), and need to receive appropriate corrective treatment. For patients with stress fractures, before the assessment is confirmed, based on individual benefit/risk assessment, the interruption of bisphosphonate therapy should be carefully considered.
Notice for missed dose
This product should be used in the morning on a fixed day of the week. Patients should be told that if a weekly dose is missed, one tablet should be taken the morning after remembering. Do not take two tablets on the same day. Instead, you should still take one tablet per week according to the original plan.
Renal insufficiency
It is not recommended to use this product in patients with renal insufficiency (creatinine clearance <35 mL/min).
Drug interactions: 1. Calcium supplements/antacids
Calcium supplements, antacids, and certain oral medications are likely to interfere with the absorption of alendronate. Therefore, patients must take at least one and a half hours after taking this product before taking any other oral drugs.
2. Aspirin
In clinical studies, the incidence of adverse events in the upper gastrointestinal tract increased in patients who used alendronate sodium (FOSAMAX) (daily dose higher than 10 mg) and aspirin-containing drugs.
3. Non-steroidal anti-inflammatory drugs (NSAIDs)
Patients who are taking non-steroidal anti-inflammatory drugs can use compound alendronate sodium. In a 3-year controlled clinical study (n=2027), most patients were concomitantly taking non-steroidal anti-inflammatory drugs, and patients taking alendronate (FOSAMAX) 5 or 10 mg/day had upper gastrointestinal dysfunction The events were similar to those of patients taking placebo. However, because the use of non-steroidal anti-inflammatory drugs is related to gastrointestinal irritation, warnings must be given during the concomitant use of this product.
4. Since non-steroidal anti-inflammatory drugs can cause gastrointestinal irritation, caution should be exercised when using it with alendronate.
Drugs that can interfere with vitamin D3 absorption
Olestra (fat substitute), mineral oil, orlistat, and bile acid sequestrants (for example, cholestyramine, colestipol) can interfere with the absorption of vitamin D. Vitamin D supplementation should be considered at this time.
Drugs that can increase the catabolism of vitamin D3
Anticonvulsants, cimetidine and thiazides can increase the catabolism of vitamin D. Vitamin D supplementation should be considered at this time.
Pharmacology and Toxicology: 1. Alendronate
Animal studies have found that this product has the following modes of action. At the cellular level, alendronate has an affinity for osteoclast-mediated sites. Under normal circumstances, osteoclasts adhere to the bone surface but lack folds, and the edges of folds are a sign of active bone resorption. Alendronate does not affect the aggregation or adhesion of osteoclasts, but it does inhibit the activity of osteoclasts. Studies on the site of action of radioactive [3H]alendronate in mice in mice showed that the surface intake of osteoclasts was 10 times that of osteoblasts. [3H] Alendronate labeled with radioactivity was administered to rats for 6 days and mice for 49 days. Bone tissue was examined and it was found that normal bone was formed on alendronate, which was not combined with the matrix. It has pharmacological activity again, therefore, alendronate must be taken continuously to inhibit the newly formed osteoclasts on the absorption surface. Histomorphometry of baboons and rats shows that alendronate can reduce bone turnover (ie, the number of bone reconstruction sites), and at these reconstruction sites, bone formation exceeds bone resorption, resulting in a gradual increase in bone mass.
2. Vitamin D3
Vitamin D3 is photochemically converted from 7-dehydrocholesterol to the precursor of vitamin D3 by the skin under the action of ultraviolet rays, and then non-enzymatic isomerization to produce vitamin D3. In the absence of adequate sunlight, vitamin D3 mainly comes from nutrients in the diet. Vitamin D3 in the skin and diet (absorbed into chylomicrons) is converted into 25-hydroxyvitamin D3 in the liver, and under the stimulation of parathyroid hormone and hypophosphatemia, it is further converted into calcium-regulating activity by the kidneys. -Dihydroxy vitamin D3 (calcitriol). The basic role of 1,25-dihydroxyvitamin D3 is to increase the intestinal reabsorption of calcium and phosphorus, and to regulate serum calcium, renal calcium and phosphorus excretion, bone formation and bone absorption.
Vitamin D3 is required for normal bone formation. Lack of sun exposure or malnutrition can cause vitamin D deficiency. Insufficient vitamin D is associated with negative calcium balance, bone loss, and increased fracture risk. In severe cases, vitamin D deficiency can cause secondary hyperparathyroidism, hypophosphatemia, proximal muscle weakness, and osteomalacia, further increasing the risk of falls and fractures in patients with osteoporosis.
Medication for pregnant women and lactating women: Prohibited for pregnant women.
Medication for elderly patients: In the Fracture Intervention Trial (FIT), among patients treated with alendronate (FOSAMAX), 71% (n=2302) were aged ≥65 years, and 17 were aged ≥75 years. %(n=550). In the United States and many countries in the treatment of female osteoporosis and the treatment of male osteoporosis [see clinical trials], patients 65 years of age or older who received alendronate (FOSAMAX) treatment were 45% and 54 respectively %. There is no overall difference in efficacy and safety observed between these patients and younger patients, but it cannot be ruled out that some older individuals are more sensitive. The elderly have an increased demand for vitamin D3 in food.
Storage: Keep away from moisture, light and airtight at 30℃.
Packing: Aluminum-plastic board, 1 piece per box.
Validity period: 18 months
Approval number: National Medicine Standard J20140022
Company Name: Hangzhou Merck Pharmaceutical Co., Ltd.
