Lendrate
Lendrate Uses, Dosage, Side Effects, Food Interaction and all others data.
Lendrate inhibits osteoclast-mediated bone-resorption. Like all bisphosphonates, it is chemically related to inorganic pyrophosphate, the endogenous regulator of bone turnover. But while pyrophosphate inhibits both osteoclastic bone resorption and the mineralization of the bone newly formed by osteoblasts, alendronate specifically inhibits bone resorption without any effect on mineralization at pharmacologically achievable doses. Its inhibition of bone-resorption is dose-dependent and approximately 1,000 times stronger than the equimolar effect of the first bisphosphonate drug, etidronate. Under therapy, normal bone tissue develops, and alendronate is deposited in the bone-matrix in a pharmacologically inactive form. For optimal action, enough calcium and vitamin D are needed in the body in order to promote normal bone development. Hypocalcemia should, therefore, be corrected before starting therapy.
Lendrate tablets have a very low oral bioavialability. After administration it distributes into soft tissue and bone or is excreted in the urine. Lendrate does not undergo metabolism.
| Trade Name | Lendrate |
| Generic | Alendronic acid |
| Alendronic acid Other Names | ABDP, Acide Alendronique, Acido Alendronico, Acidum Alendronicum, Alendronate, Alendronic acid |
| Type | |
| Formula | C4H13NO7P2 |
| Weight | Average: 249.096 Monoisotopic: 249.016724799 |
| Protein binding | 78%. Studies in rats show that plasma protein binding increases with decreasing alendronic acid plasma concentration and increasing pH. |
| Groups | Approved |
| Therapeutic Class | Bisphosphonate preparations |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Lendrate is used for the-
- Treatment and prevention of osteoporosis in post-menopausal women
- Treatment of osteoporosis, Lendrate increases bone mass and reduces the incidence of fractures, including those of the hip and spine (vertebral compression fractures)
- Prevention of osteoporosis, Lendrate may be considered in postmenopausal women who are at risk of developing osteoporosis and for whom the desired clinical outcome is to maintain bone mass and to reduce the risk of future fracture
- Treatment toincrease bone mass in men with osteoporosis
- Treatment of glucocorticoid-induced osteoporosis in men and women receiving glucocorticoids in a daily dosage equivalent to 7.5 mg or greater of prednisone and who have low bone mineral density. Patients treated with glucocorticoids should receive adequate amounts of calcium and vitamin D
- Treatment of Paget’s disease of bone in men and women
Lendrate is also used to associated treatment for these conditions: Osteogenesis Imperfecta (OI), Osteoporosis, Osteoporosis caused by glucocorticoid, Paget’s Disease
How Lendrate works
Lendrate binds to bone hydroxyapatite. Bone resorption causes local acidification, releasing alendronic acid which is that taken into osteoclasts by fluid-phase endocytosis. Endocytic vesicles are acidified, releasing alendronic acid to the cytosol of osteoclasts where they induce apoptosis. Inhibition of osteoclasts results in decreased bone resorption which is shown through decreased urinary calcium, deoxypyridinoline and cross-linked N-telopeptidases of type I collagen.
Dosage
Lendrate dosage
Treatment of osteoporosis in post-menopausal women: The recommended dose is one Lendrate 70 mg once weekly or 10 mg once daily.
Treatment to increase bone mass in men with osteoporosis:The recommended dose is one Lendrate tablet 10 mg once daily. Alternatively, one Lendrate 70 mg once weekly may be considered.
Prevention of osteoporosis in post-menopausal women: The recommended dose is 35 mg once weekly or 5 mg once daily. The safety of treatment and prevention of osteoporosis with Lendrate has been studied for up to 7 years.
Use for elderly patients: No dosage adjustment is required for elderly patients. Because in clinical study there was no evidence of age related differences in the efficacy or safety profiles of Lendrate.
Treatment of glucocorticoid-induced osteoporosis in men and women: The recommended dose is 5 mg once daily, except for post-menopausal women not receiving oestrogen, for whom the recommended dose is 10 mg once daily.
Paget’s disease of bone in men and women: The recommended treatment regimen is 40 mg once a day for six months.
Side Effects
The commonest symptomatic side effects are constipation, diarrhoea, oesophageal ulcer, flatulence, dysphagia, musculoskeletal pain, headache, rarely rash, erythema, transient decrease in serum calcium and phosphate, nausea, vomiting, peptic ulceration, hypersensitivity reactions including urticaria and angio-oedema.
Toxicity
In clinical studies, ≥3% of patients experience abdominal pain, acid regurgitation, constipation, diarrhea, dyspepsia, musculoskeletal pain, and nausea.
No information for treatment of overdose is available, however patients should be given milk or antacids to bind alendronic acid and vomiting should not be induced. Patients may experience hypocalcemia, hypophosphatemia, and upper gastrointestinal events..
There are currently no studies for safety and efficacy in pregnancy, though studies in pregnant rats show fetal and maternal complications at 4 times the clinical dose and pregnant rabbits do not show complications at as high as 10 times the clincal dose.
Excretion in breast milk, and therefore safety in lactation, is unknown.
Lendrate has been studied for use in pediatric patients. The oral bioavailability is similar to that in adult patients, but an increase in the portion of patients experiencing vomiting.
There is no significant difference in efficacy or safety of alendronic acid in geriatric populations, though there is potential for even greater sensitivity in patients at a further advanced age than those in the study.
Lendrate is not recommended for patients with creatinine clearance Label.
Interaction
The incidence of upper gastrointestinal side effects are increased with the concomitant use of non-steroidal anti-inflammatory agents and aspirin. Absorption of Alendronate is reduced in the presence of antacids and calcium supplements.
Food Interaction
- Administer vitamin supplements. Patients may require supplemental vitamin D.
- Avoid multivalent ions. Calcium, antacids, and divalent ions may interfere with the absorption of this medication.
- Take before a meal. Take 30-60 minutes before breakfast.
- Take with a full glass of water.
Volume of Distribution
28L.
Elimination Route
Mean oral bioavailability of alendronic acid in women is 0.64% and in men is 0.59%. Bioavailability of alendronic acid decreases by up to 40% if it is taken within an hour of a meal.
Half Life
Due to alendronic acid being incorporated into the skeleton, the terminal half life is estimated to be over 10 years.
Clearance
71mL/min.
Elimination Route
Administration of radiolabeled alendronic acid results in 50% recovery in urine within 72 hours. No alendronic acid is recovered in the feces. Men excrete less alendronic acid than women, though race and advanced age do not affect elimination.
Pregnancy & Breastfeeding use
Lendrate should not be given to pregnant women or nursing mother.
Contraindication
Hypocalcaemia; Renal impairment; Vitamin D deficiency; Active gastrointestinal problem such as dysphagia, oesophago-duodenitis or ulcer; and Hypersensitivity to any components of the tablet.
Special Warning
Children: Not recommended.
Innovators Monograph
You find simplified version here Lendrate
Lendrate contains Alendronic acid see full prescribing information from innovator Lendrate Monograph, Lendrate MSDS, Lendrate FDA label
FAQ
What is Lendrate used for?
Lendrate is a bisphosphonate medication used to treat osteoporosis and Paget's disease of bone. Taking Lendrate can help if you have, or are at risk of developing, osteoporosis. This is a condition that causes your bones to get weaker and be more likely to break.
How safe is Lendrate?
This evidence shows Lendrate to be safe and effective; it should be considered the nonhormonal therapy of choice for treating osteoporosis in postmenopausal women at risk for hip and vertebral fractures.
How does Lendrate work?
Lendrate works by slowing down the production of the cells that wear down bone (osteoclasts). This helps to improve bone strength and makes the bone less fragile.
What are the common side effects of Lendrate?
Some people may have serious side effects when taking Lendrate. These include heartburn (or heartburn that gets worse), problems or pain when swallowing, or chest pain. These may be signs of ulcers in your food pipe (oesophagus). If this happens, stop taking Lendrate and speak to a doctor.
Is Lendrate safe during pregnancy?
Lendrate should not be used during pregnancy.
Is Lendrate safe during breastfeeding?
It is not known whether Lendrate is excreted into human breast milk. Given the indication, Lendrate tablet should not be used by breast-feeding women.
Can I drink alcohol with Lendrate?
Yes, you can drink alcohol while taking Lendrate. However, drinking a lot of alcohol affects the strength of your bones and can increase your risk of breaks (fractures).
Can I drive after taking Lendrate?
Lendrate may make you feel dizzy. It can also cause blurred vision, and bone, muscle or joint pain. If this happens to you, do not drive, cycle or use any machinery or tools until the effects have worn off.
When should be taken of Lendrate?
Take Lendrate first thing in the morning, before you have anything to eat or drink and before you take any other medicines. Stay sitting or standing for 30 minutes so the medicine does not irritate your food pipe (oesophagus).
How many time can I take Lendrate daily?
The usual dose of Lendrate for adults is 70mg taken once a week. There is also a 10mg tablet you take once a day. You will usually take Lendrate once a week: as a standard tablet.
How often should Lendrate be taken?
Lendrate is taken either once daily or once per week. Follow your doctor's dosing instructions very carefully.
How long does Lendrate take to work?
Lendrate usually starts to work after 1 month.
How long does Lendrate stay in my system?
You'll usually take Lendrate long term, for at least 3 to 5 years. The longer you take the medicine, the longer the effects will last.
Who should not take Lendrate?
Lendrate should not be given to children and adolescents. You may suffer from a stomach upset, heartburn, inflammation of the gullet or stomach, muscle and stomach cramps, spasms, weakness and fits.
What happen If I stop taking Lendrate?
Once you stop taking Lendrate, the effects of the medicine will gradually wear off. Your bones may continue to benefit for up to 5 years afterwards. The longer you take the medicine, the longer the effects will last.
What happen If I missed Lendrate?
Patients should be instructed that if they miss a dose of Lendrate once weekly tablet, they should take one tablet on the morning after they remember. They should not take two tablets on the same day but should return to taking one tablet once a week, as originally scheduled on their chosen day.
What happen if I overdose on Lendrate?
Hypocalcaemia, hypophosphataemia and upper gastro-intestinal adverse events, such as upset stomach, heartburn, oesophagitis, gastritis, or ulcer, may result from oral overdosage. No specific information is available on the treatment of overdosage with Lendrate.
Will Lendrate affect my fertility?
There's no evidence to suggest that taking Lendrate will reduce fertility in either men or women.
Can Lendrate affect my kidneys?
Lendrate was found to be safe and effective for the treatment of osteoporosis in women with decreased renal function.
Can Lendrate affects my liver?
Lendrate treatment has also been considered as a potential hepatotoxic agent, as high serum liver enzyme concentrations and hepatitis have occasionally been reported in a few patients while receiving Lendrate.
