Forsteo solution for subcutaneous injection 250mcg/ml cartridges in syringe pens, 2.4ml

Composition

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1 ml of solution for subcutaneous use contains:

Active ingredient:

teriparatide 250 mcg,

excipients:

acetic acid ice – 0.41 mg,

sodium acetate anhydrous – 0.1 mg,

mannitol – 45.4 mg,

metacresol – 3 mg,

hydrochloric acid solution 10% and/or sodium hydroxide solution 10% – q. s.,

water d/and – q. s. to 1 ml of

Pharmacological action

Pharm group:

parathyroid hormone analog.

Pharmaceutical action:

Forsteo is an analog of parathyroid hormone. Recombinant human parathyroid hormone (PTH) produced using a strain of Escherichia coli (using DNA recombination technology). Endogenous PTH, which is a sequence of 84 amino acid residues, is the main regulator of calcium and phosphorus metabolism in bones and kidneys. Forsteo® (recombinant human PTH (1-34)) is an active fragment of endogenous human PTH. The physiological effect of PTH is to stimulate the formation of bone tissue by directly affecting osteoblasts. PTH indirectly increases intestinal absorption and tubular reabsorption of calcium, as well as phosphate excretion by the kidneys.

The biological effect of PTH is achieved by binding to specific PTH receptors on the cell surface. Teriparatide binds to the same receptors and has the same effect on bones and kidneys as PTH. A single daily use of teriparatide stimulates the formation of new bone tissue on the trabecular and cortical (periosteal and/or endosteal) surfaces of bones with a predominant stimulation of osteoblast activity in relation to osteoclast activity. This is confirmed by an increase in the content of markers of bone formation in the blood serum: bone-specific ALP and procollagen-I carboxytherminal propeptide (PICP). An increase in the content of bone formation markers is accompanied by a secondary increase in the level of bone resorption markers in the urine: N-telopeptide (NTX) and deoxypyridinoline (DPD), which reflects the physiological interaction of bone formation and resorption processes in skeletal remodeling.

2 hours after use of teriparatide, there is a short-term increase in the concentration of serum calcium, which reaches maximum values in 4-6 hours and returns to the initial values within 16-24 hours. In addition, transient phosphaturia and a slight short-term decrease in the content of phosphorus in the blood serum can be observed.

When treated with teriparatide, bone mineral density (BMD) of the entire body increases by 5-10% (including in the lumbar spine, femoral neck and femur).

Mineralization processes occur without signs of toxic effects on bone tissue cells, and the bone tissue formed under the influence of teriparatide has a normal structure (without the formation of reticulofibrous bone tissue and bone marrow fibrosis). Teriparatide reduces the risk of fractures regardless of age, baseline bone metabolism or BMD (relative reduction in the risk of new fractures is 65%).

Pharmacokinetics:  

Teriparatide is well absorbed by subcutaneous use. The absolute bioavailability of the drug is approximately 95%. Cmax of teriparatide is reached 30 minutes after subcutaneous use of the drug at a dose of 20 mcg and exceeds 4-5 times the ULN of the PTH level, followed by a decrease in the concentration to undetectable values within 3 hours

. Vd is approximately 1.7 l/kg.

Like endogenous PTH, teriparatide does not accumulate in bones or other tissues.

T1 / 2 of teriparatide with subcutaneous use is about 1 hour, which reflects the time required for absorption.

Peripheral PTH metabolism occurs primarily in the liver through non-specific enzymatic mechanisms, followed by renal excretion.

Pharmacokinetics in special clinical cases:

No effect of age (age group from 31 to 85 years) on the pharmacokinetics of teriparatide was observed.

In patients with mild or moderate renal insufficiency (creatinine clearance from 30 to 72 ml / min), the pharmacokinetics of the drug do not change.

Indications

Treatment of osteoporosis in postmenopausal women; treatment of primary or hypogonadal osteoporosis in men.

Use during pregnancy and lactation

The effect of teriparatide treatment on human fetal development has not been studied.

Do not prescribe the drug during pregnancy.

No clinical studies have been conducted to determine whether teriparatide is excreted in breast milk.

Teriparatide should not be administered to nursing mothers.

Contraindications

• prior hypercalcemia;
• severe renal failure;
• metabolic bone disease, with the exception of primary osteoporosis (including hyperparathyroidism and Paget’s disease);
• increased activity of alkaline phosphatase of unknown origin;
• prior radiation therapy of the skeleton’s bones;
• metastases to bone or bone tumors in history;
• pregnancy;
• lactation;
• age to 18 years;
• hypersensitivity to the drug Forteo.

With caution:

• in patients with acute urolithiasis or who have recently had it, due to possible deterioration of the condition; urinary calcium excretion should be monitored;
• in patients with moderate renal impairment;
• hypovitaminosis D, clinically significant hypocalcemia.

Side effects

Musculoskeletal disorders: very often (≥ 10%) – pain in the extremities; often (≥1%,

From the hematopoietic system: frequently (≥1%,

From the side of metabolism: frequently (≥1%,

Nervous system disorders: frequently (≥1%,

From the side of the psyche: frequently (≥1%,

Cardiovascular system: frequently (≥1%,

Respiratory system disorders: frequently (≥1%,

From the digestive system: frequently (≥1%,

Skin and subcutaneous tissue disorders: frequently (≥1%,

From the urinary system: rarely (≥ 0.1%,

Allergic reactions are very rare (

General reactions: frequently (≥1%,

Local reactions: rare (≥ 0.1%,

Interaction

There were no clinically significant interactions with hydrochlorothiazide, furosemide, digoxin, atenolol, or delayed – release drugs such as diltiazem, nifidipine, felodipine, or nisoldipine.

Co-use of teriparatide with raloxifene or hormone replacement therapy does not affect the content of calcium in the blood serum and urine.

A single use of teriparatide does not affect the Pharmacodynamics of digoxin.

Hypercalcemia is a predisposing factor to the development of digitalis intoxication, so teriparatide should be used with caution in patients taking digitalis preparations.

How to take, course of use and dosage

The drug Forsteo is prescribed for adults. The dose does not depend on the patient’s age.

The recommended dose of Forsteo is 20 mcg, administered once a day subcutaneously in the thigh or abdomen.

The maximum duration of treatment with Forsteo is 18 months. In the event of a break in treatment with Forsteo, patients can continue treatment with other drugs.

Additional calcium and vitamin D supplements are recommended if they are not available in sufficient quantities.

The patient should be trained in the technique of drug use (see “Instructions for using the pen”).

Rules for using a syringe pen

Forsteo is a solution in a syringe pen designed for individual use. A new sterile needle is required for each injection. Each Forsteo package contains a “Patient’s Guide”, which describes in detail the rules for handling the syringe pen.

Injection needles are not included. The pen can be used with insulin pen needles (Becton Dickinson). The drug should be administered immediately after the pen is removed from the refrigerator. After each injection, the pen should be placed in the refrigerator.

Overdose

Symptoms: overdose may be manifested by prolonged hypercalcemia and the development of orthostatic collapse. Nausea, vomiting, dizziness, and headache are also possible.

Treatment: There is no specific antidote. If an overdose is suspected, discontinuation of Forsteo, monitoring of serum calcium levels, and symptomatic therapy are recommended.

Special instructions

The effect of teriparatide in patients with hypercalcemia has not been studied, so the drug should not be prescribed to such patients due to the possibility of exacerbation of hypercalcemia.

Hypercalcemia should be excluded before starting treatment with teriparatide, however, regular monitoring of serum calcium concentrations is not required.

The effect of teriparatide in patients with active urolithiasis has not been studied. In patients with urolithiasis (acute course or recent exacerbation), teriparatide should not be used because of the risk of exacerbation of this disease.

Blood sampling to determine the calcium content in the blood should be performed no earlier than 16 hours after the last use of Forsteo, since there may be a short-term increase in serum calcium content after teriparatide injection. Constant monitoring of calcium concentrations during treatment is not required.

When taking the drug Forsteo, rare episodes of short-term orthostatic hypotension may occur, which occur within 4 hours after use of the drug and pass independently within a few minutes to several hours when the patient is placed in a supine position and are not a contraindication to further treatment.

Due to insufficient clinical data for long-term treatment with teriparatide, the recommended treatment period should not exceed 18 months.

Forsteo should not be used if the solution in the syringe pen is cloudy, colored or contains foreign particles.

Use in pediatrics

The effect of teriparatide in paediatric patients has not been studied. Teriparatide should not be used in children, adolescents, or young adults with open epiphyseal growth zones.

Form of production

Solution for subcutaneous use

Storage conditions

At a temperature of 2-8 °C (do not freeze)

Shelf life

2 years

Active ingredient

Teriparatide

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection

Purpose

For adults as directed by your doctor

Indications

Osteoporosis