Sinakten Depot® (Synacthen depot®)

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Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceTetracosactideTetracosactide
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  • Sinakten Depot®
    suspension w / m 
    QuestCor Limited     Ireland
    • Dosage form: & nbspsuspension for intramuscular injection
    Composition:

    1 ml of suspension for injection (1 ampoule) contains: active substance - tetracosactide 1 mg (equivalent to 1,123 mg of tetracosactide hexaacetate); Excipients: zinc chloride anhydrous 5, 218 mg, benzyl alcohol 10,000 mg, sodium chloride 2,000 mg, sodium hydrogen phosphate dihydrate 1,050 mg, hydrochloric acid (sufficient amount), sodium hydroxide (sufficient amount), water for injection (up to 1 ml).

    Description:milky white suspension.
    Pharmacotherapeutic group:adrenocorticotropic hormone
    ATX: & nbsp

    H.01.A.A   ACTH

    H.01.A.A.02   Tetracosactide

    Pharmacodynamics:Tetrakosaktid consists of the first 24 amino acids that make up the natural adrenocorticotropic hormone (ACTH). As well as ACTH, tetracosactide stimulates the production of adrenal cortex glucocorticosteroids and mineralocorticosteroids, and, to a lesser extent, androgens. All this explains the therapeutic effect of the drug in diseases usually treated with glucocorticosteroids. Tetracosactide has anti-inflammatory, antiallergic and immunosuppressive action, inhibits the development of connective tissue, affects carbohydrate, fat, protein, mineral metabolism.

    Pharmacological activity of the drug can not be compared with the activity of glucocorticosteroids, since under the influence of ACGH, in contrast to treatment alone glucocorticosteroids, fabrics are subjected to the action of the physiological spectrum of corticosteroids.

    Increase in the dose of the drug Sinakten Depot " not increases the pharmacodynamic response, but only lengthens its duration actions. A longer the use of the drug, according to the results of studies, minimally suppresses the hypothalamic-pituitary-suprarenal system with long-term therapy glucocorticosteroids.

    ACTH binds to a specific receptor membranes of cortical cells adrenal glands. The resulting hormone-receptor complex activates adenylate cyclase, which is involved in the formation of cyclic adenosine monophosphate (AMP), which, in turn, activates protein kinase, which provides the synthesis of pregnenolone from enzymatic reactions from pregnenolone synthesized a variety of corticosteroids.

    After 1 mg of Synakten Depot® is used, the concentration of cortisol increases, and its highest values ​​are recorded within 8-12 hours after the injection. Elevated cortisol concentrations persist for up to 24 hours and return to baseline after approximately 36-48 hours.

    Slowed down release tetrakozaktida from the drug provides a long-term effect of the drug. Thus, an increase in the concentration of cortisol in the plasma after intramuscular (IM) administration of 1 mg of the drug persists for 24-32 hours.

    Pharmacokinetics:

    After an intravenous injection of 1 mg of the preparation, the concentrations of tetracosactide in plasma varied from 200 to 300 pg / ml and were maintained for 12 hours. The delayed release of the active substance from the injection site is provided by adsorption of tetracosactide on zinc phosphate.

    The apparent volume of distribution of tetracosactide is about 0.4 l / kg.

    In the blood plasma tetracosactide fast disintegrates under the action of enzymatic hydrolysis first on Inactive oligopeptides, then on free amino acids. Period terminal phase of the half-life of tetracosactide isabout 3 hours. Tetracosactide is excreted mainly by the kidneys. Tetrakozaktid does not penetrate the placental barrier. The possibility of penetration of tetracosactide into breast milk has not been studied.
    Indications:

    Neurological diseases

    Multiple sclerosis (exacerbation). Vesta Syndrome (infantile myoclonic encephalopathy with gypsarhythmia).

    Rheumatic diseases

    Short-term therapy of diseases and states in which glucocorticosteroids; patients with diseases of the gastrointestinal pathways that tolerate poor reception glucocorticosteroids inside; cases, when the use of conventional doses glucocorticosteroids does not lead to adequate effect.

    Skin diseases

    Long-term treatment of skin diseases, usually responding to therapy glucocorticosteroids - incl. bladder, chronic eczema severe flow, erythrodermic or pustular forms of psoriasis.

    Diseases of the gastrointestinal tract

    Ulcerative colitis. Regional enteritis.

    Oncological diseases

    As an additional method of treatment to improve the tolerability of chemotherapy.

    Diagnostic application for the determination of adrenal cortex function deficiency

    A five-hour test can be conducted with application of preparation of Synakten Depot "in those cases where a thirty minute test from drug (intramuscularly / intravenously) gave a dubious result, and also with the purpose of determining the functional reserve of the adrenal cortex.

    Contraindications:

    ■ Increased sensitivity to tetracosactide and / or ACTH and the components of the preparation.

    ■ Acute psychosis.

    ■ Infectious diseases.

    ■ Stomach ulcer and duodenal ulcer in the phase of exacerbation.

    ■ Refractory cardiac failure.

    ■ Syndrome Itenko-Cushing.

    ■ Primary insufficiency treatment cortical insufficiency adrenal glands.

    ■ Adrenogenital syndrome.

    ■ Pregnancy and the period breastfeeding.

    ■ Systemic fungal infections.

    ■ Simultaneous use of live or diluted vaccines with immunosuppressive doses of the drug Synakten Depot ®.

    Due to the increased risk anaphylactic reactions drug Sinakten Depo® should not be used for treatment of bronchial asthma or other allergic diseases.

    As Sinakten Depo® contains benzyl alcohol, application of of the drug is contraindicated in children under 3 years in view of high risk toxic and allergic reactions, up to a lethal outcome.

    Carefully:

    If you have one of these diseases, always consult a doctor before using the drug.

    The potential risk associated with the use of the drug and the expected benefit of therapy for prescribing patients with the following diseases should be compared: ulcerative colitis, diverticulitis, newly established intestinal anastomosis, renal failure, arterial hypertension, predisposition to thromboembolism, osteoporosis, myasthenia gravis.

    Care should be taken when using the drug Synakten Depot in patients suffering from eye damage with herpes simplex, as it is possible to develop corneal perforation. The drug Sinakten Depot can activate latent amoebiasis. In this regard, it is recommended to exclude latent or active amoebiasis before starting therapy.

    In cases where the drug Sinakten Depot is indicated to patients with latent tuberculosis or a positive reaction to tuberculin, careful observation is necessary, since the development of clinical manifestations of the disease is possible.During prolonged therapy, such patients should receive preventive chemotherapy.

    During treatment with the drug Sinakten Depot should not be vaccinated against smallpox. Care should be taken when carrying out any procedure for immunization, as against the background of drug therapy, the formation of antibodies is reduced.

    Dosing and Administration:

    Therapeutic application

    Treatment begins with a daily application of the preparation Synakten Depot ®.

    After about 3 days, treatment continue in the intermittent mode. The drug is administered intramuscularly (w / m). Before use the ampoule to shake.

    Adults and children over 15 years of age, the drug is administered at an initial dose of 1 mg daily. In acute cases and oncologic practice, treatment can be started with a dose of 1 mg, applied every 12 hours. After the disappearance of acute symptoms of the disease, the drug is usually administered at a dose of 1 mg every 2-3 days. In those cases, when there is a good effect, the dose can be reduced to a minimum of 0.5 mg every 2-3 days or 1 mg once a week.

    For young children (from 3 to 6 years), the initial dose is 0.25 - 0.5 mg daily; the maintenance dose is 0.25-0.5 mg every 2-8 days.

    For children of school age (from 6 to 15 years) the initial dose is 0.25 -1 mg daily; the maintenance dose is 0.25-1 mg every 2-8 days. Ampoule before use shake.

    Use in patients with impaired renal function

    Research the patients in violation of function kidneys not carried out.

    Use in patients with impaired liver function

    Research the patients in violation of function liver not was conducted.

    Elderly patients (> 65 years old)

    Data for the need for dose adjustment in the elderly (65 years and older) is not received.

    Diagnostic application

    5 hour test. The concentration of cortisol is measured immediately before and 0.5; 1; 2; 3; 4 and 5 hours after the injection of Sinakten Depo ®.

    If the adrenal function is normal, the basal concentrations of tetracosactide (> 200 nmol / L) are doubled within the first hour and then slowly increase according to the following pattern:

    Concentrations of cortisol

    Time The index (nmol / l)

    1 hour 600-1250 nmol / l

    2 hour 750-1500 nmol / l

    3 hour 800-1550 nmol / l

    4 hours 950-1650 nmol / l

    5 hours 1000-1800 nmol / l

    If the cortisol concentrations increase more slowly than those listed in the table, this may indicate the following diseases: Addison's disease,secondary insufficiency of the function of the adrenal cortex due to disorders functions hypothalamic-pituitary systems or an overdose of glucocorticosteroids.

    For differential diagnosis of primary and secondary adrenal hypofunction, a 3-day test should be performed. All plasma samples should be stored in the refrigerator prior to determination concentrations cortisol plasma.

    Side effects:

    Side effects can be caused by tetrakozaktidom, gasoline alcohol, which is part of the drug, as well as increased secretion of glucocorticosteroids and mineralocorticosteroids during the period of treatment with the drug Synakten Depot ®.

    Adverse effects due to tetracosactide

    At the postmarketing stage, the following side effects were reported based on spontaneous cases and literature data.

    Immune system disorders

    Gyne Sensitivity

    Disorders from the endocrine system

    Hemorrhages in the adrenal glands.

    Side effects caused by benzyl alcohol

    Gasoline alcohol included in the composition preparation as a filler, can cause toxic and allergic reactions in children under the age of 3 years.

    Side effects associated with effects of glucocorticosteroids and mineralocorticoids

    These side effects are unlikely when using Synakten Depot ® with a diagnostic purpose, however can occur when applied to therapeutic indications.

    Infectious and parasitic diseases: increased susceptibility to infections, abscess.

    Violations from the blood and lymphatic system: leukocytosis.

    Disorders from the endocrine system: irregular menstrual cycle, syndrome Itenko-Cushing (violations of protein, carbohydrate, fatty and water-electrolyte exchange); secondary bark failure adrenal gland and pituitary gland, especially in time of stress, for example, after an injury, surgical interventions or diseases; reduced tolerance to tolerance to carbohydrates, hyperglycemia, development of clinical manifestations latent diabetes mellitus; hirsutism.

    Disorders from the metabolism and nutrition: increased appetite, weight gain, hypokalemia, disorders calcium exchange of (steroidal osteoporosis), delay sodium, water retention.

    Disorders of the psyche: mental disorder. During treatment with tetracosactide, develop violations by psychic sphere (for example, euphoria, insomnia, mood swings, personality changes, severe depression and even obvious psychotic phenomena). It is possible to strengthen existing ones the patient emotional instability or psychotic phenomena.

    Impaired nervous system: headache, dizziness, convulsions; insignificant increased intracranial pressure with edema of the nipple of the optic nerve (usually after the end of treatment).

    Disorders from the side of the organ of vision: subcapsular cataract, rise intraocular pressure, glaucoma, exophthalmos.

    Vascular disorders: thromboembolism, necrotizing angiitis, increase in blood pressure.

    Heart Disease: chronic heart failure.

    AT individual cases in children up to 5 lay down with prolonged treatment with the drug in large doses, reversible hypertrophy of the myocardium can develop.

    Disturbances from the gastrointestinal tract: peptic ulcer with possible perforation and bleeding, pancreatitis, bloating, ulcerative esophagitis.

    Violations from skin and subcutaneous tissues: skin atrophy, petechiae and ecchymosis, erythema, hyperhidrosis, acne, hyperpigmentation of the skin. Violations from skeletal-muscular system and connective tissue: osteoporosis, muscle weakness, myopathy, muscular atrophy, compression fractures of the vertebrae, aseptic necrosis of femoral and humerus head, pathological fractures of long (tubular) bones, rupture of tendons.

    Other: reactions increased sensitivity, deceleration rate of growth in children, negative nitrous balance due to protein catabolism, impaired wound healing, suppression of skin reactions when conducting tests, fever, decreased vision, nausea, vomiting.

    If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

    Interaction:

    Interaction, which leads to the restriction of the combined application With the simultaneous use of the drug Synakten Depot ® and valproate in children with severe jaundice. Their joint application should be avoided.

    Joint application of the preparation Synakten Depot ® and other anticonvulsants drugs (eg, phenytoin, clonazepam, nitrazepam, phenobarbital, primidon) may increase the risk of liver damage, thus Sinakten Depot ® in combination therapy should be used at the lowest possible dose and for a minimum time. Endogenous and synthetic estrogens can call rise concentration of total cortisol and, thus, it is considered appropriate to apply alternative methods (eg, salivary cortisol, free cortisol index, free plasma cortisol) to assess function hypothalamic-gynophyseal-adrenal system.

    Special instructions:

    The drug Sinakten Depo ® should be used only under medical supervision. The drug Sinakten Depo® can not be administered intravenously.

    Special instructions associated with tetracosactide

    Hypersensitivity reactions

    Patients who are prone to allergic reactions (including those suffering from bronchial asthma) should not be treated with the drug Sinakten Depo®.

    Before the appointment of the drug Sinakten Depo®, the doctor should find out whether the patient is inclined to allergic reactions, whether he suffers from bronchial asthma.It is also important to determine whether the patient was previously treated with ACTH drugs, and if treated, then clarify whether the treatment did not cause treatment reactions increased sensitivity.

    If during or after an injection develop local or systemic allergic reactions (eg, severe erythema and tenderness at the injection site, hives, itching, heat, severe weakness or shortness of breath), treatment with Sinakten Depot® should be discontinued, and in the future should be avoided applications any drugs ACTH.

    Hypersensitivity reactions (if they occur at all) tend to develop within 30 minutes after the injection. Therefore, during this time, the patient must remain under medical supervision. In case of serious anaphylactic reaction, 0.1% solution of epinephrine (0.4-1 ml IM or 0.1-0.2 ml in 10 ml of 0.9% sodium chloride solution intravenously slow) and glucocorticosteroids intravenously in large doses, if necessary, repeat them.

    Insufficient diagnostic accuracy

    In some clinical situations, due to a change in the concentration of cortisol-binding globulins, monitoring the plasma cortisol concentration in a test with the Synakten depot ® can give erroneous results.These include the use in patients receiving oral contraceptives, patients after surgery, in critical condition, patients with severe liver damage, nephrotic syndrome. In these states, alternative parameters (cortisol saliva, free cortisol index, free plasma cortisol) can be used to evaluate the functioning of the hypothalamic-pituitary-adrenal system.

    Special instructions related to glucocorticosteroid and mineralocorticosteroid effects

    Delayed sodium and water arising in response to the administration of the drug Synakten Depot ®, can in many cases be avoided when prescribing a low-salt diet. With prolonged treatment, it may sometimes be necessary to administer additional potassium.

    In the event that a fluid retention (weight gain) or a syndrome develops Itenko-Cushing, preparation Synakten Depot ® should be canceled for a while or prescribed in a smaller dose (either by reducing the daily dose by half, or by prolonging intervals between injections, for example, up to 5-7 days).
    The effect of the drug may be enhanced in patients with hypothyroidism or cirrhosis of the liver. Long-term therapy with Sinakten Depot® may be accompanied by the development of posterior subcapsular cataract and glaucoma. Therefore, it is necessary to observe the oculist. Patients, suffered injury or surgery during treatment with Sinakten Depo® or within one year after the end of treatment, the dose should be increased or resume treatment with this drug. In some cases, an additional application of glucocorticosteroids fast action. When carrying out therapy with the drug Synakten Depot ® the minimum effective dose should be applied. Reduce the dose should be done gradually. Prolonged use of the drug leads to a relative insufficiency of the "pituitary-adrenal" system, which can persist for several months after discontinuation of treatment. In these cases, the question of the appropriate steroid therapy should be decided.

    During the period of treatment with the drug Sinakten Depot ® should not be immunization with live vaccines, as these patients are decrease in the antibody response.

    Use in children aged 3 years and older

    It is unlikely that the drug Sinakten Depo®, assigned individually selected doses will lead to growth disorders in children. Nevertheless, the children who undergo long-term therapy need regular monitoring growth.

    Young children should regularly conduct echocardiography, since during prolonged therapy high doses can develop reversible hypertrophy of the myocardium.

    Effect on the ability to drive transp. cf. and fur:

    As a drug Sinakten Depot® can affect the central nervous system, patients should comply with caution in managing vehicles or working with mechanisms.

    Form release / dosage:

    Suspension for intramuscular injection 1 mg / ml.

    Packaging:1 ml per ampoule of colorless glass. 1 or 10 ampoules together with instructions for use in a cardboard box.
    Storage conditions:

    At a temperature of 2 to 8 ° C in a dark place.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:П N013438 / 01
    Date of registration:23.12.2011 / 10.03.2015
    Expiration Date:Unlimited
    Date of cancellation:2017-01-13
    The owner of the registration certificate:QuestCor LimitedQuestCor Limited Ireland
    Manufacturer: & nbsp
    Representation: & nbspInfarma, LLCInfarma, LLCRussia
    Information update date: & nbsp13.01.2017
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