What is Fosamax?
Pharmacological action
Inhibitor of bone resorption. Refers to group of a medicine which is localized in areas of active bone resorption, by osteoclasts, inhibit the process of bone resorption caused by osteoclasts, without exerting direct influence on the formation of new bone tissue. Because bone resorption and the appearance of new bone tissue are interconnected, the formation of bone also decreases, but to a lesser extent than the resorption, which leads to a progressive increase in bone mass. During treatment with alendronate formed by normal bone tissue, which is embedded in the matrix alendronate, remaining pharmacologically inactive. In therapeutic doses of alendronate did not cause osteomalacia.
Osteoporosis in postmenopausal women
Osteoporosis is characterized by reduced bone mass and, consequently, increased risk of fractures, particularly of the spine, hips and wrists. It occurs as men and women, but particularly common in women after menopause, when the rate of bone resorption exceeds the rate of its formation, which leads to loss of bone mass. Daily intake of alendronate in postmenopausal women causes biochemical changes, indicating a dose-dependent suppression of bone resorption, including lowering the level of calcium in the urine and markers of bone collagen dissolution (hydroxyproline and cross-linked N-telopeptide of collagen type I) in urine. These biochemical parameters returned to their original values within 3 weeks after discontinuation of alendronate, despite the fact that the drug is stored in the long bones of the skeleton. Long-term (up to 5 years) treatment of osteoporosis, FOSAMAX 10 mg / reduces urinary excretion of bone resorption markers and cross-linked N-telopeptide type I collagen by approximately 50% and 70%, respectively, to levels observed in healthy women before the onset of menopause.
The rate of bone resorption begins to decline already in the first month of treatment, reaches a constant value at 3-6 months of therapy and maintained on the achieved values throughout the treatment FOSAMAX. It is also noted lower levels of markers of bone formation – osteocalcin and alkaline phosphatase approximately 50%, and total alkaline phosphatase by approximately 25-30%, reaching a plateau after 6-12 months of therapy. When prophylactic FOSAMAX 5 mg / there is a reduction levels of osteocalcin and alkaline phosphatase by approximately 40% and 15% respectively. This decrease in the rate of bone metabolism occurs when receiving FOSAMAX in a dose of 70 mg 1 time per week for one year.
Treatment of postmenopausal osteoporosis
Effect on bone mineral density. FOSAMAX 10 mg / postmenopausal in patients with osteoporosis increases bone mineral density (BMD) of lumbar spine, femoral neck and greater trochanter femur after 3 years of therapy compared with placebo by an average of 8.82%, 5.9% and 7.81% respectively. Total IPC also significantly increased, and this indicates that the increase in bone mass in the lumbar spine and femur is not at the expense of other parts of the skeleton. The increase in bone mass observed after 3 months after taking the drug and lasts for 3 years. When extending the deadline for receiving up to 5 years of lumbar spine BMD and femoral greater trochanter continued to increase and additional increases between 3 and 5 year of therapy is 0.94% and 0.88% respectively. Thus, FOSAMAX is the opposite of osteoporosis. Efficiency FOSAMAX is not dependent on age, race, and baseline rate of bone metabolism, renal function and application of a wide range of drugs. Cancel FOSAMAX after 1-2 years of receiving a dose of 10 mg is accompanied by a gradual return of the intensity of bone metabolism to the original values, the IPC does not increase, but the accelerated loss of bone mass is observed. Therefore, therapy FOSAMAX should be prolonged to ensure a gradual increase in bone mass. In a study in women with osteoporosis postmenopausal it was shown that a dose of FOSAMAX 70 mg 1 time per week therapeutically equivalent FOSAMAX 10 mg / Thus, the average increase in lumbar spine BMD in the first year of receiving a dose of FOSAMAX 70 mg 1 time per week and FOSAMAX 10 mg 1 time / is 5.1% and 5.4% respectively. The degree of increase in the IPC was also comparable between the treatment groups and for other parts of skeleton. These data support the view that a dose of FOSAMAX 70 mg, taken 1 time per week, is also effective in reducing the incidence of fractures as FOSAMAX 10 mg daily at the reception. Influence on the incidence of bone fractures. Found that among women with osteoporosis postmenopausal taking FOSAMAX for 3 years, statistically significant at the 48% reduces the proportion of patients who came by one or more vertebral fractures (3.2% versus 6.2% for placebo). Moreover, those patients who received FOSAMAX and suffered fractures of the spine, reducing the growth was not as great as in the placebo group (5.9 mm and 23.3 mm respectively), owing to a decrease in the number and severity of fractures. When you receive FOSAMAX for 2-3 years at doses> 2.5 mg / decrease the frequency of vnepozvonochnyh fractures by 29% (9.0% versus 12.6% in the placebo group). Thus, FOSAMAX effectively reduces the frequency of fractures, including spine and hip, that is, sites of the skeleton, the most vulnerable to the development of osteoporosis and its complications.
Histology of bone tissue. Histologically in postmenopausal women with osteoporosis who received FOSAMAX at doses of 1 to 20 mg for 1, 2 or 3 years, it was found that bone tissue has a normal structure and mineralization, but also registered a decline rate of bone metabolism compared with placebo .
Application men
Although osteoporosis in men does not occur as frequently as in postmenopausal women, a significant portion of fractures associated with osteoporosis are men. The prevalence of spinal deformity associated with osteoporosis, the same for men and women. Application of FOSAMAX 10 mg 1 time / men for 2 years reduced urinary excretion of cross-linked N-telopeptide type I collagen by approximately 60% and kostespetsificheskoy alkaline phosphatase by approximately 40%. Similar results were observed when receiving FOSAMAX in a dose of 70 mg 1 time per week for 1 year. Increased MEC in the lumbar spine was 5.3% in the femoral neck – 2.6%, in a big spit – 3.1%, the overall IPC – 1.6% compared with placebo. In the application of FOSAMAX 10 mg / men there is a declining rate of new vertebral fractures, which is 0.8% compared with 7.1% for placebo. Also, a decline of magnitude reduction of growth, which is 0.6 mm while taking FOSAMAX compared to 2.4 mm for placebo. When applying a dose of FOSAMAX 70 mg 1 time per week for 1 year is an increase in BMD at the lumbar spine by 2.8% in the femoral neck – by 1.9% in the femur – 2%, in other parts of the body – 1.2% compared with placebo. How to stop taking fosamax is effective in men regardless of age, the function of sexual glands and the initial BMD at the femoral neck and lumbar spine.
Prevention of osteoporosis in postmenopausal women
In women aged 40-60 years old, started taking FOSAMAX 5 mg / at least 6 months after menopause, the average increase in IPC compared to baseline at the lumbar spine, femoral neck, greater trochanter, and in general in the bones of the skeleton after 2 years of therapy is 3.46%, 1.27%, 2.98% and 0.67% respectively, after 3 years – 2.89%, 1.10%, 2.71% and 0.32% respectively. In addition, FOSAMAX 5 mg / decreases the rate of bone loss in the bones of the forearm by approximately half compared to placebo and is effective regardless of age, menopause, race and baseline rate of bone metabolism. After 3 years of taking the drug histological examination reveals normal structure of bone tissue.
Interactions with estrogen / hormone replacement therapy
In the conduct of combined therapy a significant increase or trend towards an increase in BMD at the femur as a whole, as well as in the femoral neck and greater trochanter compared with the isolated HRT and where can i buy fosamax with no prescription buy paypal.
Osteoporosis due to glucocorticoid
Prolonged glucocorticoid is associated with the development of osteoporosis and fractures in men and women at any age and sever reactions to fosomax. FOSAMAX decreases the level of biochemical markers of bone resorption and causes a significant increase in BMD at the lumbar spine, femoral neck, greater trochanter femur, regardless of dose and duration of glucocorticoid. In applying the drug at a dose of 10 mg 1 time / 1-year histological examination reveals a normal picture of the bone tissue.
Bone Paget’s disease
In Paget’s disease of bone FOSAMAX decreases the rate of bone resorption, accompanied by a decrease in bone formation. Use of the drug in a dose of 40 mg 1 time / 6 months causes a significant reduction in serum alkaline phosphatase, which is an objective indicator of disease severity. In addition, receiving FOSAMAX leads to the formation of normal lamellar bone in place disorganized bone tissue, while not breaking the mineralization of bone. Histological data confirm that under the influence of FOSAMAX are not indicated violations of mineralization and formed normal bone tissue.
Pharmacokinetics
FOSAMAX absorption
After oral doses of 5-70 mg on an empty stomach, not later than 2 h before a standardized breakfast bioavailability of alendronate was 0.64% for women and 0.6% – men. After receiving alendronate fasting for 1-1.5 h before a standardized breakfast reduced bioavailability by approximately 40%. Patients with osteoporosis and Paget’s disease of bone FOSAMAX is effective in applying an empty stomach, not later than 30 minutes before the first intake of food or liquid. Bioavailability of alendronate is insignificant in his appointment in conjunction with meals, fda warning to doctors about fosomax or within 2 hours after meals. Simultaneous treatment with coffee or orange juice reduced bioavailability by approximately 60%. When receiving prednisolone 20 mg 3 to 5 days there is no clinically significant changes in the bioavailability of alendronate.
Distribution
The average Vd alendronate in the equilibrium state (with the exception of bone tissue) is at least 28 liters. When receiving therapeutic doses of the drug concentration in plasma is negligible (less than 5 ng / ml). Alendronate binding to plasma proteins is approximately 78%.
Metabolism
There is no evidence that alendronate undergoes metabolism in humans or animals.
FOSAMAX withdrawal
After a single in / to the introduction of alendronate, 14C-labeled carbon atoms, approximately 50% of the drug is excreted in the urine within 72 h, excretion of the labeled drug in the faeces was low or not determined. After a single in / to the introduction of alendronate in a dose of 10 mg of its renal clearance is 71 ml / min. In 6 hours plasma concentration in blood is decreased by more than 95%. Final T1 / 2 more than 10 years, reflecting the release of drug from bone tissue. Alendronate does not violate the excretion of drugs through the acidic and basic transport systems of the kidneys; I want to use paypal to buy fosamax. Somewhat greater accumulation of the drug in the bone tissue can be expected in patients with impaired renal function.
Indications
- Treatment of osteoporosis in postmenopausal women with a view to preventing the development of fractures, including hip fractures and compression fractures of the spine;
- Prevention of osteoporosis in the presence of the risk of its development in postmenopausal women to reduce the likelihood of fractures;
- Treatment of osteoporosis in men to prevent fractures;
- Treatment and prevention of osteoporosis induced by glucocorticoids, in men and women;
- Treatment of Paget’s disease of bone in men and women.
FOSAMAX dosage regimen
FOSAMAX must be taken, at least 30 minutes before the first meal, fluid or drugs, drinking just plain water. Other beverages (including mineral water), food and some medicines may reduce the absorption of FOSAMAX. To reduce the risk of esophageal irritation FOSAMAX should be taken, following these rules: take the morning immediately after rising from fosamax studies, with a full glass of water to facilitate the receipt tablets in the stomach, do not chew the tablets or dissolve them in the mouth because of the possible formation of ulcers in the mouth cavity and pharynx, patients should not lie down until the first meal fosamax warning, which should produce at least 30 minutes after taking FOSAMAX, fosamax plus mexico should not be taken at bedtime or before getting out of bed. Patients should take extra calcium preparations and vitamin D, if the intake of these substances with food is not enough herbal alternatives for fosomax. Treatment of osteoporosis in postmenopausal women and men: The recommended dosage – 1 tablet 70 mg 1 time per week, or 1 tablet 10 mg 1 time. Prevention of osteoporosis in postmenopausal women: 5 mg once. Treatment and prevention of osteoporosis caused by glucocorticoid, men and women: 5 mg 1 time / in postmenopausal women who receive estrogen, the recommended dose is 10 mg of fosamax onj once. Bone Paget’s disease in men and women: 40 mg 1 time / within 6 months. Repeated treatment of bone Paget’s disease can be carried out within 6 months after 1 course in the case of patients developed a disease from which diagnosis is based on increasing levels of alkaline phosphatase. Repeated treatment may also be performed in patients whose alkaline phosphatase level is not returned to normal after an initial course of therapy. For elderly patients and patients with renal insufficiency of mild and moderate degree (Page 35 to 60 ml / min) dose adjustment is required evista like fosomax. FOSAMAX is not recommended to be considered in patients with severe renal insufficiency (CC <35 ml / min) due to lack of application in these patients.
FOSAMAX side effects
From the digestive system:> 1% – abdominal pain, dyspepsia, dysphagia, flatulence, constipation, diarrhea, sour belching, nausea, gastritis, gastric ulcer, including stomach ulcer complicated by hemorrhage (melena); possible erosion or ulceration of the esophagus, nausea, vomiting, gastritis, melena, esophagitis, esophageal stricture, perforation, oropharyngeal ulcers, rarely – gastric and duodenal ulcers (although the link with the drug has not been established).
On the part of the musculoskeletal system: > 1% – myalgia, bone pain, joint pain, muscle cramps; possible myalgia, bone pain, joint pain (rare – heavy flow).
Dermatological reactions: possible skin rash, erythema, photosensitivity, pruritus. Allergic reactions: urticaria possible; rare – angioedema, transient symptoms of acute phase response in early treatment (myalgia, malaise, rarely – fever), severe skin reactions including Stevens-Johnson syndrome and toxic epidermal necrolysis. On the part of metabolism: rarely – hypocalcemia where can i buy fosamax with no prescription. From the sense organs adverse reaction from fosomax occurs: rarely – uveitis, scleritis, episcleritis. From the laboratory parameters: reduction of calcium and phosphate in the blood serum (usually slight, asymptomatic and transient) by 18% and 10% respectively. FOSAMAX was generally well tolerated, side effects are usually light and do not require discontinuation of the drug. The safety and tolerability of FOSAMAX in the form of tablets, 10 mg and 70 mg are comparable.
FOSAMAX contraindications
- Esophageal disease, slowing its emptying (eg stricture or achalasia);
- Inability to sit or stand upright for 30 minutes;
- Hypocalcemia;
- Hypersensitivity to the ingredients.
Be used with caution during exacerbation of upper gastrointestinal disorders such as dysphagia, esophageal disease, gastritis, duodenitis or gastric ulcer fda and fosomax. FOSAMAX is not recommended to be considered in patients with impaired renal function with CC <35 ml / min in the case of susceptibility to hypocalcemia (gipoparatireoidizm, vitamin D, calcium malabsorption). Application during pregnancy and breastfeeding improves fosomax side effects. FOSAMAX should not be given during pregnancy and lactation (breastfeeding).
FOSAMAX use in renal impairment
For older patients tail bone fosamax, patients with renal insufficiency mild or moderate severity (QC from 35 to 60 ml / min) dose adjustment is required. Application of FOSAMAX in patients with severe renal insufficiency (CC less than 35 ml / min) is not recommended due to the lack of clinical observations.
Fosomax cautions
FOSAMAX, like other bisphosphonates, may cause local irritation of the mucous membrane of upper gastrointestinal. Patients receiving treatment FOSAMAX, observed adverse reactions such as esophagitis, esophageal ulcer and erosion of the esophagus, occasionally giving rise to stricture or perforation of the esophagus. In some cases of fosamax migraine, these undesirable effects can be severe and require hospitalization, and therefore should be especially careful to control any symptoms suggestive of possible violations of the esophagus. Patients should be warned of the tim o’brien fosamax need to stop taking FOSAMAX and seek medical advice in case of dysphagia, pain when swallowing or behind the substitutes for fosamax breastbone, new or worsening heartburn. The risk of severe adverse events from the esophagus is higher in patients who violate the guidelines for receiving the drug and / or continue to take it when symptoms of irritation of the esophagus. It is particularly important that the patient had a recommendation on the admission of the drug, understood them and was informed that the risk of injury of the esophagus is increasing in the event of failure of these recommendations. Known rare cases how long for fosamax to work the appearance of gastric ulcers and duodenal ulcers, some severe and complicated (a causal link with taking this medication is not installed). FOSAMAX should be used with caution in patients with exacerbations of diseases of the upper gastrointestinal tract, such as dysphagia, esophageal disease, gastritis, duodenitis and ulcers because of possible irritant effect of the drug on the mucous membrane of upper gastrointestinal and the worsening of the underlying disease. Patients should be warned that if you accidentally missed doses fosomax 1 times a week, they should take one tablet in the morning next day. Do not take two doses in one day, but later must return to receive the medication 1 time a week on the day of the week, which was selected at the beginning of treatment. You should take into account other causes of osteoporosis other than estrogen deficiency, age and treatment with glucocorticoids. In presence of hypocalcemia level of calcium in the blood normalize before treatment FOSAMAX. Other violations of mineral metabolism (eg, deficiency of vitamin D) should also be eliminated. Patients with these disorders need to control the content of calcium in the blood and symptoms of hypocalcemia. As FOSAMAX increases mineral content in bones, a mild asymptomatic decrease in calcium and phosphate in the blood serum, especially in Paget’s disease of bone, with the initially significantly increased rate of bone tissue metabolism, as well as in patients receiving glucocorticoids, which is accompanied by a possible decrease in absorption calcium. It is particularly important to ensure adequate intake of calcium and vitamin D in these patients with side effects from fosamax. In rare cases, hypocalcemia may be severe, usually in patients with a predisposition to this complication (gipoparatireoidizm, vitamin D, calcium malabsorption).
FOSAMAX use in pediatrics what schedule is fosamax. FOSAMAX studies in children have been conducted, so the drug should not be used in pediatrics.
Effects on ability to drive vehicles and management mechanisms have not been proved. There is no evidence that FOSAMAX affect the ability to drive or work with mechanisms.
FOSAMAX overdose is novacaine ineffective if you have been taking fosamax. Symptoms: hypocalcemia, hypophosphatemia, adverse effects from the upper part of the digestive tract, including dipepsiya, heartburn, esophagitis, gastritis, side effects of fosomax, gastric ulcer and esophagus. Treatment: the patient should take milk or antacids to bind alendronate. To prevent irritation of the esophagus should not induce vomiting. Patients should remain upright. Data on the specific therapy is not available.
FOSAMAX Interactions
In an application with calcium supplementation, antacids and other means for possible violation of the oral absorption of alendronate. In this regard, the interval between taking to buy FOSOMAX and other medicines taken by mouth should be at least 30 minutes. In joint application FOSAMAX and HRT (estrogen ± progestin) safety and tolerability of paypal fosamax combination therapy correspond to those in the application of each of these drugs individually. In clinical studies FOSAMAX in men, postmenopausal women and patients taking glucocorticoids, have been identified clinically significant drug interactions with regard to fosamax martha rosenberg effects on protein binding, renal excretion and metabolism. The frequency of adverse events from the upper gastrointestinal increases when combined with a dose of FOSAMAX 10 mg / s preparations containing acetylsalicylic acid. However, this effect was not observed when receiving fosamax jaw problems in a dose of 70 mg 1 time / week.
