Alental (Aceclofenac) 100mg 20 tablets

Pharmacological action 

Pharm group: bone resorption inhibitor – biphosphonate.

Formdata: Alental – hormonal specific inhibitor osteoclastic bone resorption (from the group aminobisphosphonates – synthetic analogs of pyrophosphate that bind to the hydroxyapatite in bone) inhibits osteoclasts. 

Stimulates bone formation, restores a positive balance between resorption and bone reconstruction, progressively increases bone mineral density (regulates calcium and phosphorus metabolism), promotes formation of normal bone tissue with normal histological structure.

Pharmacokinetics: Absorption

The bioavailability of alendronova acid when taken in a dose of 70 mg on an empty stomach 2 hours before a meal is 0.64% (for women) and 0.6% (men); when taken on an empty stomach 1-1.5 hour before meals is reduced by 40%.

Coffee and orange juice reduces bioavailability by 60%.

Distribution

Average Vd in a state of equilibrium concentrations (with the exception of bone) in humans is at least 28 l.

The concentration of the drug in blood plasma after oral administration at the therapeutic dose is too small for analytical determination (< 5 ng/ml).

Linking blood plasma proteins is approximately 78%.

Metabolism

In the human body is not metabolized.

Excretion

Output unchanged. The elimination process is characterized by rapid. the decrease in the concentration of alendronova acid in the blood plasma and extremely slow release from the bones. When administered orally after 6 hours the plasma concentration is reduced by more than 95%. Absorbed, but not ustroivshis in the bone tissue

alendronate is rapidly excreted by the kidneys. After a single on/in the introduction of 10 mg of alendronate renal clearance is 71 ml/min, system – 200ml/min.

Testimony

• osteoporosis in postmenopausal women (prevention of bone fractures, including hip and spine);
• osteoporosis in men;
• Paget’s disease.

Contraindications

• hypocalcemia;
• inability of patient to stand or sit upright for at least 30 min;
• renal failure severe (KK less 35 ml/min);
• severe disorders of mineral metabolism;
• stricture or achalasia of the oesophagus and other conditions leading to difficulty.
• promotion of food through the esophagus;
• severe hypoparathyroidism;
• malabsorption of calcium;
• lactose intolerance;
• lactase deficiency;
• glucose-galactose malabsorption;
• pregnancy;
• lactation;
• the children’s age;
• hypersensitivity.

With caution in diseases of the gastrointestinal tract in the acute phase (dysphagia, esophagitis, gastritis, duodenitis, gastric ulcer and duodenal ulcer), a deficiency of vitamin D.

Special instructions

It is necessary to control the possibility of any symptoms of adverse reactions from the side of the esophagus. The patient should be informed about the necessity of discontinuation of the drug, Elental and seeking medical attention with the development of dysphagia, pain when swallowing, pain behind the breastbone, or heartburn.

It is necessary to inform the patient about the possible risk.damage to the mucosa of the esophagus failure to comply with the instructions for use.

In the presence of hypocalcemia it is necessary to conduct correction before treatment. Therapy should be combined with a diet enriched with calcium salts and vitamin D.

During treatment, a slight asymptomatic reduction in the concentration of calcium in blood serum and phosphate due to the positive effects of alendronova acid on mineral density of bone tissue, which is of particular importance for patients receiving glucocorticoid drugs, as they may experience reduced absorption of calcium.

It was reported on the pathological (i.e., when exposed to a small force and spontaneous) intertrochanteric fractures or fractures of the proximal femur diarise a small number of patients taking bisphosphonates. Some of the fractures were classified as stress (also known as stress fracture, March fracture, fracture of Deuscleaner), resulting in no injuries. Some patients for weeks or months before the occurrence of full fracture had experienced prodromal pain in the affected area, often associated with a characteristic radiographic picture of a stress fracture. The number of messages was very small, in addition, stress fractures with similar clinical features occur in patients not taking bisphosphonates. 

Patients with stress fractures should be evaluated with the assessment of known causes and risk factors (e.g. vitamin D deficiency, malabsorption, use of corticosteroids, stress fracture history of arthritis or fracture of the lower extremities, excessive or prolonged load, diabetes mellitus, chronic alcoholism) and to provide adequate orthopedic care. Pending the results of the survey should consider the suspension of acceptance of bisphosphonates in patients with stress fractures, based on the assessment of the benefit/risk in each case.

Effects on ability to drive vehicles and management mechanisms

Not affected.

Composition

1 tablet contains aceclofenac 100mg.

Method of application and doses

Inside.

While osteoporosis in postmenopausal women and men – 70 mg 1 time per week or 10 mg 1 times/day., with liquid, for 2 hours (but not less than 30 min) before the first meal, water or other drugs. Drink only plain water, 

because other beverages (including mineral water, coffee, tea, orange juice) reduce the absorption. The tablets should not be chewed or dissolve in the mouth.

Paget’s disease – 40 mg/day. during 6 months.

Dose adjustment in elderly patients is not required.

To reduce the irritating effect on the esophagus the drug Alental must be taken immediately as you Wake up with a full glass of water after taking should not lie down for 30 minutes (dangerous to use in the event of failure of the patient to stand or sit upright for 30 minutes).

Taking at bedtime or in a horizontal position increases the risk of developing esophagitis.

Accidental skipping of the drug in the dosage once a week should take 1 tablet in the morning, the nearest day. You should not take the pill one day, but in the future we must continue to take 1 tablet in the day of the week, which was selected to be used from the start of treatment.

Dose adjustment in patients with mild and moderate renal insufficiency (QC from 35 to 60 ml/min) is required.

Side effects

From the digestive system: dysphagia, esophagitis, abdominal pain, heartburn, dyspepsia, constipation, diarrhoea, flatulence. Rarely – nausea, vomiting, gastritis, melena, esophageal stricture, ulcers of the mucous membrane of the mouth and throat, ulcers of the esophagus, perforation of ulcer of esophagus with bleeding.

From the side of musculoskeletal system: pain in bones, muscles and joints.

CNS: headache

On the part of the organ of vision: uveitis, scleritis.

Allergic reactions: rare – urticaria, angioneurotic edema; reported sporadic occurrence of the syndrome Stevens-Johnson and Lyell.

Other: rash, itching, erythema, photodermatosis, symptomatic hypocalcemia; described the development of osteonecrosis of the upper and lower jaws, mainly in patients with cancer on the background of anticancer treatment, including bisphosphonates. Risk factors for the development of osteonecrosis are cancer, chemotherapy, radiation therapy, treatment with corticosteroids, inadequate oral hygiene, local infectious-inflammatory process, including osteomyelitis. In most described cases, the patients to the treatment with bisphosphonates was produced by extraction of teeth.

Laboratory data: a slight and transient of syrennialestrange of calcium and phosphate.

Typical symptoms at the beginning of treatment: myalgia, malaise and rarely, fever.

Drug interactions

The interval between doses of the drug, Elental and other drugs and nutritional supplements shall be not less than 1 h.

The combined use of alendronova acid (but not simultaneous use) of drugs for HRT (estrogen+Progestin) is not accompanied by a change in the safety profile and tolerability of each drug compared with their separate usage.

The use of alendronova acid and drugs for HRT (estrogen + progestin) privodit greater increase in bone mass compared with taking each preparatov separately.

The simultaneous use of calcium supplements and antacids reduce the absorption of alendronova acid.

Ranitidine increases the bioavailability of 2 times (clinical significance not determined). In clinical studies there was an increase in the incidence of side effects from the upper gastrointestinal tract in patients taking more than 10 mg of alendronate a day concurrently with medicinal products containing acetylsalicylic acid.

Alendronate sodium may be panacan patients taking NSAIDs. In a 3-year controlled clinical study (number of patients 2027) during which most of the patients were accepted as concomitant therapy of NSAIDs, the number of adverse events relating to the upper gastrointestinal tract was similar in patients receiving alendronate sodium in the dose of 5 and 10 mg/day, and patients receiving placebo. However, the use of NSAIDs is associated with irritation of the mucous membrane of the gastrointestinal tract, therefore, the use of NSAIDs together with alendronova acid should be careful.

Overdose

Symptoms: hypocalcemia, hypophosphatemia, adverse reactions from the upper gastrointestinal tract (heartburn, esophagitis, gastritis, ulcers).

Treatment: there is no specific treatment. We recommend taking milk and antacids. To avoid esophageal irritation, do not induce vomiting, the patient should be given a vertical position (standing or sitting).