Alenra

Alendra is a medicine that affects bone mineralization and structure.

Alendronate Na is a representative of the aminobisphosphonate category, an artificial analogue of natural pyrophosphate. The drug inhibits precipitation of phosphate Ca, blocks the process of its conversion into hydroxyapatite, and in addition slows down the aggregation of apatite crystals, forming larger crystals, and increases the rate of reverse dissolution of these crystals.

The selective effect is associated with a strong affinity observed in bisphosphonates to mineral bone elements. The drug has an effect as an effective (non-hormonal) specific substance that slows down osteoclast-mediated bone resorption. The final determination of the exact principle of the development of this process has so far failed

[1]

Indications Alenra

It is used to treat osteoporosis that develops during postmenopause. The drug reduces the likelihood of fractures in the hip bones, as well as the spine.

[2], [3], [4]

Release form

The release of therapeutic substance is implemented in tablets - 4 pieces inside the cell bundle. In the box - 1 such a pack.

Pharmacodynamics

The drug helps to establish a positive balance in relation to bone repair and resorption. It increases the mineral bone density in the pelvic region with the spine and helps to form bones that have a healthy histological structure.

Alendra prevents the occurrence of new bone fractures. Decreases serum Ca values, slowing bone resorption and reducing its volume, released from bone tissue.

Calcium-lowering effect of medication, mediated by the oppression of osteoclasts, develops after 1-2 days.

[5], [6], [7], [8], [9], [10]

Pharmacokinetics

Alendronate Na is 25% absorbed inside the gastrointestinal tract. The level of absolute bioavailability of tablets (within 5-10 mg), which are taken on an empty stomach 2 hours before meals, is 0.64% (for a woman) and 0.59% (for a man).

The bioavailability index decreases (approximately by 40%) in the case of the use of the drug 0.5-1 hour before the usual breakfast. The bioavailability values of the medicine will be low if taken with food or for 2 hours after eating food. The introduction of the drug together with any drinks (among them coffee, mineral water and orange juice) reduces the bioavailability value by 60%.

Tests with the participation of animals determined that after intravenous injection of the 1st mg / kg of alendronate Na, the substance is distributed for some time inside the soft tissues, but later it is rather quickly redistributed.

Half of the portion that was absorbed, in an unchanged state, is excreted mostly through the kidneys (for a period of 72 hours), the remainder cumulates inside the bone tissues for a long time. Its excretion is extremely slow - due to synthesis with bone tissue. The term half-life of bone medication lasts for several years.

About 78% of the substance is synthesized with intraplasma protein and does not participate in metabolic processes. Plasma values of the drug are quite low (below 5 ng / ml) and decrease by 95% in the period of 6 hours after the infusion.

With the 1-time use of 10 mg of the drug, the indicators of intrarenal clearance were 71 ml per minute; total clearance while making up a maximum of 0.2 liters per minute.

[11], [12], [13], [14], [15], [16], [17]

Dosing and administration

Apply the drug should be in portions of 70 mg (1 tablet), 1 time per week.

There is no optimal duration of the bisphosphonate therapy cycle for osteoporosis. The decision on the need to continue the course should be taken by the attending doctor, individually for each patient, taking into account the ratio of benefits and existing risks (especially after 5+ years of taking the medication).

A pill is swallowed, washed down with plain water, at least half an hour before the first use of food, drinks or other medicines. Other drinks (including mineral water), food and certain medicinal substances can lead to a decrease in the absorption of alendronate Na.

To simplify the passage of the drug inside the stomach, which will reduce its irritating effect on the mucous membranes of the oropharynx with the esophagus, you need to use the medicine, drinking down at least 0.2 liters of plain water (in the morning, after sleeping); chewing pills can not, because it can cause ulcers in the oropharynx. The first use of food per day should occur at least after half an hour from the moment of application of the 1st tablet. The patient should not lie within the minimum of half an hour after the introduction of the drug. It is forbidden to take medication in the evening before bedtime or when getting out of bed in the morning.

The interval between administration of Alendra and other medicinal substances (taken orally) should last at least half an hour.

Calciferol supplementation with Ca is required - in cases when an insufficient amount of these elements is supplied with food.

The medication must be consumed on the same day of the week. If the reception was accidentally missed, take a pill in the morning the next day. Further, the application continues in the usual way - a new pill is drunk on the day originally chosen for consumption.

[26], [27]

Use Alenra during pregnancy

You can not assign Alendra pregnant or lactating women.

Contraindications

Among the contraindications:

• severe intolerance associated with alendronate Na or another element of the drug;
• hypocalcemia;
• diseases affecting the esophagus (achalasia or stricture), in which there is a delay in removing its contents;
• the inability to stand or sit straight for at least half an hour;
• failure of renal function in severe (CC values - <35 ml per minute).

[18], [19], [20], [21]

Side effects Alenra

Main adverse symptoms:

• immune lesions: signs of intolerance, including allergy, urticaria and angioedema;
• disorders associated with the function of NA: dizziness or headaches, as well as a taste disorder (the appearance of an unusual or bitter taste after the use of drugs);
• visual disorders: episcleritis or scleritis, as well as uveitis;
• problems with the work of the auditory organs: osteonecrosis, affecting the external part of the auditory canal (a complication that often occurs when using bisphosphonates), and vertigo;
• signs associated with the work of the gastrointestinal tract: constipation, ulcers in the mouth, esophagus or pharynx, heartburn, pain in the abdomen, bloating, dysphagia and dyspepsia, and in addition to vomiting, erosion in the esophagus, tension of the peritoneal wall, nausea, esophagitis and regurgitation stomach contents. In addition, strictures may appear inside the esophagus, melena and perforations, bleeding or ulcers in the gastrointestinal area (oral cavity, stomach with esophagus and pharynx);
• lesions of the subcutaneous layers and the epidermis: erythema, alopecia, rashes, photosensitivity, pruritus and epidermal manifestations, among which are TEN and SJS;
• problems with the work of connective tissues and ODA: maxillary osteonecrosis, pain affecting the joints with bones or muscles, swelling in the joints and atypical fractures in the femur zone;
• metabolic disorders: hypocalcemia, which is accompanied by relevant clinical signs (usually associated with the presence of precipitating factors);
• systemic manifestations: temporary disturbances (malaise and muscle aches; occasionally, fever), often developing at the initial stage of therapy, and in addition, peripheral edema and asthenia;
• indications of laboratory tests: hypocalcemia or phosphatemia (in case of use 10 mg / kg alendronate per day).

[22], [23], [24], [25]

Overdose

In case of poisoning, hypophosphatemia and -calcemia develop, and in addition, negative manifestations affecting the upper part of the gastrointestinal tract (heartburn, gastric dysfunction, gastritis, esophagitis, or gastric ulcer).

To synthesize alendronate, you need to drink milk or use antacids. Due to the existing likelihood of irritation in the area of the esophagus, it is impossible to induce vomiting; In addition, the victim must be constantly upright.

[28]

Interactions with other drugs

Violation of the absorption of the drug can occur when taking it with drinks (also with mineral water), food, antacids, substances Ca (among them also food additives) and some other drugs for ingestion. The interval between the use of such substances should be at least half an hour.

The introduction of NSAIDs may be irritating to the gastrointestinal tract. Therefore, it is necessary to very carefully combine such medicines with Alendra.

[29], [30], [31], [32], [33], [34], [35]

Storage conditions

Alendra should be kept in a place closed to the penetration of small children. The temperature values are not more than 25 ° С.

[36]

Shelf life

Alendra can be used for a period of 3 years from the time the pharmaceutical product is manufactured.

Application for children

The drug is not used in pediatrics (under the age of 18).

Analogs

Analogs of drugs are drugs Londromax with Ostemax.

[37], [38], [39], [40], [41], [42], [43], [44]