Forose - instructions for use, doses, side effects, contraindications

Excipients: cellulose microcrystalline 261.250 mg; silicon dioxide colloidal anhydrous 3,500 mg; croscarmellose sodium 1,280 mg; magnesium stearate 2,620 mg.

Shell: Luster Clear LC 103 7,000 mg (microcrystalline cellulose -44%, carrageenan-18%, macrogol 8000 - 38%).

Description:

White round, biconvex tablets, film-coated, engraved "ALN 70 "on one side.

Pharmacotherapeutic group:Bone resorption inhibitor-bisphosphonate

ATX: & nbsp

M.05.B.A.04 Alendronic acid

Pharmacodynamics:Non-hormonal specific inhibitor of osteoclastic bone resorption. Stimulates osteogenesis, restores a positive balance between resorption and bone restoration, increases bone mineral density (regulates phosphorus-calcium metabolism), promotes the formation of bone tissue with a normal histological structure.

Pharmacokinetics:

Absorption.

Bioavailability alendronic acid in a dose of 70 mg for fasting for 2 hours before a standard breakfast is 0.64% in women, 0.59% in men. If you take 1 hour or half an hour before breakfast, bioavailability alendronic acid decreases to 0.46 % and 0.39%, respectively. In clinical trials confirmed the effectiveness alendronic acid when applied at least 30 minutes before the first meal or drinks, with the use of alendronic acid simultaneously with food or within 2 hours after eating, the absorption of the drug is sharply reduced, the bioavailability of alendronic acid becomes insignificant.When combined with coffee or orange juice, the bioavailability of the drug is reduced by approximately 60%.

Distribution.

Alendronovaya acid after intravenous administration at a dose of 1 mg / kg is temporarily distributed into soft tissues and then quickly redistributed into bone tissue or removed from the urine. Average volume distribution in the equilibrium state, not counting bone tissue, in humans is about 28 liters. The concentration of the drug in the blood plasma is negligible (less than 5 ng / ml). The connection with plasma proteins is about 78%.

Metabolism.

No data, confirming that alendronic acid is metabolized in the human body.

Excretion.

After a single intravenous administration alendronic acid labeled with carbon atoms [¹⁴C], for about 72 hours about 50% of the substance is secreted by the kidneys and a small amount - through the intestine.

The final half-life is more than 10 years, reflecting the release of alendronic acids from bone tissue.

Pharmacokinetics in specific patient groups

Floor: The bioavailability of alendronic acid does not differ significantly between men and women.

Elderly age: Bioavailability and excretion of alendronic acid are similar in elderly and younger patients.

Race: Pharmacokinetic differences on the basis of race were not studied.

Impaired renal function: Have healthy volunteers alendronic acid, not accumulates in the bone tissue, quickly excreted in the urine. Controlled pharmacokinetic studies on the use of alendronic acid in renal there was no failure, but in patients with marked renal dysfunction, alendronic acid elimination is likely to be reduced. Therefore, a somewhat greater accumulation of alendronic acid in the bone tissue of patients with impaired renal function can be expected. With the clearance of creatinine (CK) from 35 to 60 ml / min, dose adjustment is not required. Use of alendronic acid in patients with SC less than 35 ml / min is not recommended due to the lack of such experience.

In patients with hepatic dysfunction There is no need to adjust the dose of alendronic acid, since she does not metabolized and not excreted with bile.

Indications:

- Treatment of osteoporosis in postmenopausal women, including to reduce the risk of compression fractures of the spine and hip fractures;

- treatment of osteoporosis in men to prevent fractures;

- Treatment of osteoporosis caused by prolonged use of glucocorticosteroid drugs.

Contraindications:

- Hypersensitivity to alendronate or other components of the drug;

- strictures of the esophagus, achalasia of the cardia and other conditions leading to dysphagia and slowing of the food movement along the esophagus;

- vitamin deficiency D;

- the patient's inability to stand or sit for 30 minutes;

- severe renal failure (creatinine clearance less than 35 ml / min);

- severe disturbances in mineral metabolism (hypocalcemia);

- pregnancy, the period of breastfeeding;

- children's age (efficacy and safety not established).

Carefully:

It should be used with caution in patients with diseases of the gastrointestinal tract, such as dysphagia, gastritis, duodenitis, peptic ulcer disease, active gastrointestinal bleeding or surgery on the upper gastrointestinal tract in history, hypovitaminosis D.

Pregnancy and lactation:

The drug Forosa® is contraindicated in pregnancy and during breastfeeding.

There is no data on the use of alendronic acid in pregnant women,However, animal studies have revealed a violation of the formation of fetal bone tissue when using high doses of alendronic acid and dysfunction of labor related to hypocalcemia. Do not use the drug during pregnancy.

It is not known whether the alendronic acid in breast milk, so the use of the drug during breastfeeding is contraindicated.

Dosing and Administration:

Inside.

The drug should be used to ensure daily intake of calcium and vitamin D.

The optimal duration of the drug is not established. The need for continued therapy with biophosphonates should evaluated on a regular basis, especially after 5 or more years of use.

To ensure the proper absorption of the drug, Forosa® Tablets should be taken in the morning on an empty stomach, at least 30 minutes before the first meal, drinks or other medications, with a glass of ordinary water (at least 200 ml). Other beverages (including mineral water) can reduce absorption of the drug.

To reduce the risk of esophageal irritation: 1) the preparation of Forosa® should be taken only after full awakening and getting up from bed; 2) swallow tablets whole (do not chew, dissolve or dissolve them in the mouth due to the possible formation of ulcers in the mouth and throat, 3) do not take a horizontal position before the first meal (the first meal - no earlier than 30 minutes after taking the drug); 4) You must not take the drug before going to bed or before going to bed early.

The recommended dose is 70 mg (1 tablet) once a week.

For elderly patients and patients with violation of the function liver, moderate renal dysfunction (QC more than 35 ml / min) dose adjustment is not required.

In patients with marked impairment of kidney function (SC less than 35 ml / min) apply the drug is not recommended because there is no experience application in a given population.

Side effects:

In a one-year study conducted among postmenopausal women with osteoporosis, general safety profiles of alendronic acid once a week at a dose of 70 mg (n = 519) and at a dose of 10 mg / day (n = 370) were similar.

In two three-year studies of almost identical design conducted among postmenopausal women (alendronic acid 10 mg: n = 196; placebo: n = 397), common profiles safety of alendronic acid 10 mg / day and placebo were similar.

Side effects noted by the investigators as possibly related to alendronate, probably related and precisely conditioned by the action of the drug, are presented below. The incidence of side effects was> 1% in one of the therapeutic groups in the 1-year study or> 1% in one of the 3-year studies with 10 mg alendronate daily and above the incidence of side effects among patients receiving placebo:

	1-year		3-year
	study		research
	Alendronate 70 mg 1 time per	Alendronate 10	Alendronat10	Placebo
	week,	mg, daily	mg, daily
	(n = 519)	(n = 370)	(n = 196)	(n = 397)
	%	%	%	%
Gastrointestinal tract
stomach ache	3,7	3,0	6,6	4,8
dyspepsia	2,7	2,2	3,6	3,5
acid regurgitation	1,9	2,4	2,0	4,3
nausea	1,9	2,4	3,6	4,0
bloating	1,0	1,4	1,0	0,8
constipation	0,8	1,6	3,1	1,8
diarrhea	0,6	0,5	3,1	1,8
dysphagia	0,4	0,5	1,0	0,0
flatulence	0,4	1,6	2,6	0,5
gastritis	0,2	1,1	0,5	1,3
gastric ulcer	0,0	1,1	0,0	0,0
oesophageal ulcer	0,0	0,0	1,5	0,0
Musculoskeletal system
Musculoskeletal (bones, muscles or joints) pain	2,9	3,2	4,1	2,5
muscle spasms	0,2	1,1	0,0	1,0
Nervous system
headache	0,4	0,3	2,6	1,5

In a broad clinical practice (including clinical trial data and data postmarketing application), the following undesirable effects, which are classified according to their frequency of development (WHO classification): very often (≥1 / 10); often (≥1 / 100, <1/10), infrequently (≥1 / 1000, <1/100), rarely (≥1 / 10000, <1/1000) and very rarely (<1/10000), the frequency is unknown - according to available data, it was not possible to establish the frequency of occurrence.

From the immune system rarely: reactions Hypersensitivity (including flushing of skin, urticaria, angioedema, edema).

From the side of metabolism and nutrition rarely: symptomatic hypocalcemia (often associated with conditions predisposing to it); rarely: asymptomatic transitional hypophosphatemia.

Co the sides of the nervous system often: dizziness, headache; infrequently: perversion of taste; frequency is unknown: irritability.

From the side of the organ of vision infrequently: scleritis, uveitis (inflammation of the choroid of the eye), and episcleritis (inflammation connective tissue between sclera and conjunctiva).

On the part of the ruffian of hearing and labyrinthine disorders often: vertigo (dizziness).

Co side of the gastrointestinal tract often: abdominal pain, dyspeptic disorders (constipation or diarrhea, flatulence), dysphagia, heartburn; infrequently: nausea, vomiting, esophagitis, gastritis, ulceration of the mucosa esophagus membranes, melena; rarely: stricture of the esophagus, ulceration of the mucous membrane of the mouth, throat, stomach and duodenum, bleeding from the upper sections of the gastrointestinal tract, perforation of the esophagus.

From the skin and subcutaneous tissues often: alopecia, itchy skin integuments; infrequently: rash, redness of the skin; rarely: increased photosensitivity, severe skin reactions, including Stevens-Johnson syndrome (malignant exudative erythema) and Lyell's syndrome (toxic epidermal necrolysis).

From the musculoskeletal and connective tissue Often: pain in muscles, bones, joints; often: severe pain in muscles, bones and joints, swelling joints; rarely: osteonecrosis of the jaw (see section "Special instructions"), atypical fractures proximal diaphysis of the femur.

General disorders and disorders at the site of administration often: asthenia, peripheral edema; infrequently: transient influenza-like symptoms (muscle pain, fatigue, rarely fever), usually occurring at the beginning of therapy.

Overdose:

Against the background of an overdose of the drug may develop hypocalcemia, hypophosphatemia, as well as symptoms such as abdominal pain, dyspeptic disorders, dysphagia, heartburn, esophagitis, gastritis, ulceration of the mucous membrane of the gastrointestinal tract. Treatment: symptomatic. The use of milk and antacid preparations for the binding of alendronate is shown. Due to the risk of esophageal injury, Vomiting should be caused, the patient should be in an upright position.

Interaction:

Simultaneous application calcium preparations (including food additives) and antacids worsen the absorption of alendronic acid. Concerning It is recommended to take other medications no earlier than 30 minutes after using the drug Forosa®. Non-steroidal anti-inflammatory drugs (including acetylsalicylic acid) can increase the side effects of alendronic acid on the mucosa of the gastrointestinal tract.

Despite,that special studies on drug interaction have not been conducted, the use of alendronate in clinical studies with a large number of widely used drugs has not been accompanied development of clinically relevant interaction.

In clinical studies in patients taking estrogen preparations (intravaginally, transdermally or inward) simultaneously with alendronate, there was no clinically significant interaction.

Special instructions:

Use only ordinary water to take Porose ® tablets, as other beverages (including mineral water, tea, coffee, fruit juices) worsen absorption of the drug. Taking alendronic acid before bedtime or in a horizontal position increases the risk of developing esophagitis.

If symptoms of esophageal irritation, such as dysphagia, chest pain, or the appearance / deterioration of an existing heartburn patients should consult a doctor to assess the possibility of continuing therapy.

The risk of serious adverse effects from esophagus is higher in patients, taking alendron acid with violation of this instruction and / or continuing its reception after the onset of symptoms, indicative of irritation of the esophagus. It is important to explain in detail the patient the rules of taking the drug and make sure that he understood them. Patients should be aware of the increased risk of adverse events on the part of the esophagus in the event of deviation from the instructions.

Before the start of therapy with the drug Froza^® correction of hypocalcaemia and other metabolic disorders (such as vitamin deficiency D). In connection with the increase in the background of therapy with alendronic acid, bone mineral density is possible insignificant clinically asymptomatic decrease in serum calcium and phosphate levels, especially in patients receiving

glucocorticosteroids, in which calcium absorption can be reduced. It is therefore important to ensure sufficient the amount of calcium and vitamin D in the body, which is especially important in patients receiving glucocorticosteroids.

Patients should be warned that if they miss a dose of the drug once a week, they should take 1 tablet in the morning of the next day (it is unacceptable to take 2 tablets in one day).In the future should continue to take 1 tablet on the day of the week, which was selected at the beginning of therapy.

There is also evidence of osteonecrosis of the jaw in patients with osteoporosis receiving oral bisphosphonates. Prior to the appointment of bisphosphonate therapy to patients with concomitant risk factors (eg, cancer, chemotherapy, radiation therapy, glucocorticosteroids, inadequate oral hygiene, anemia, coagulopathy, infection, gum disease) it is necessary to undergo dental examination with appropriate preventive treatment of teeth.

During treatment, these patients should avoid invasive dental intervention whenever possible. For patients who developed osteonecrosis of the jaw during the treatment with bisphosphonates, the operative dental interventions can lead to worsening of the condition.

Data on possible risk reduction osteonecrosis of the jaw after discontinuation of bisphosphonates in patients who require dental intervention are not available.

Low-energy fractures (also known as fatigue fractures) of the proximal femoral diaphysis can occur in patients taking alendronic acid for a long time.Fractures can occur after minimal or no trauma, some patients may experience hip pain, often with external signs of stress fractures in a few weeks / months before full fracture of the femur. Low-energy fractures of the proximal femoral diaphysis were often bilateral, so patients with a long-term fracture of the femoral diaphysis receiving bisphosphonates should be examined for the opposite thigh. Discontinuation of bisphosphonate in patients with stress fractures It is advisable to carry out after assessing their condition on the basis of an individual assessment risk / benefit ratio.

The decision to perform treatment should be taken individually for each patient after a thorough assessment of the risk / benefit ratio, especially for patients with Barrett's esophagus.

Effect on the ability to drive transp. cf. and fur:Studies on effect of alendronic acid on the ability to control vehicles and work with mechanisms, was not carried out. However, since the development of dandruff is possible with alendronic acid, as well as other side effects, care should be taken when managing transport means and work with mechanisms, and refrain from performing these activities in case of side effects.

Form release / dosage:

Tablets, film-coated, 70 mg.

Packaging:

2 or 4 tablets per blister of aluminum / aluminum.

For 1, 2, 3, 4 or 6 blisters together with instructions for use are placed in a cardboard box.

Storage conditions:

In dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-007906/08

Date of registration:07.10.2008

The owner of the registration certificate: Lek dd Lek dd Slovenia

Manufacturer: & nbsp

LEK d.d. Slovenia

Representation: & nbspSANDOZ SANDOZ Switzerland

Information update date: & nbsp18.09.2015

Illustrated instructions

Instructions

Forosa® (Forosa®)