Dexamethasone (injection solution 0.4 %)
Dexamethasonesolutio pro injeсtionibus
International nonproprietary name (INN)
Dexamethasone
Pharmacotherapeutic group
Glucocorticoids for systemic dosing.
Composition
Active ingredient – dexamethasone sodium phosphate (calculated on dexamethasone phosphate) – 4.0 g;
Auxiliary substances: glycerol, sodium phosphate bisubstituted dihydrous or sodium phosphate bisubstituted 12-hydrous, disodium ethylene diamine salt -N, N, N', N'- tetraacetic acid dihydrous, injection water.
Pharmacologicaleffect
Pharmacodynamics
Interaction with specific cytoplasmatic receptors and formation of complex penetrating cell nucleus and stimulating synthesis of mRNA; the latter induces protein formation meditating cellular activity, inclusive lipocortin that inhibits phospholipase A2, inhibits liberation of arachidonic acid and biosynthesis of endoperoxides, PG, leukotriene, provoking inflammatory process, allergy and others. It hampers liberation of mediators of inflammation from eosinophils and labrocytes It inhibits the activity of hyaluronidase, collagenase and protease, normalizes intracellular matrix of cartilaginous tissue and bone tissue functions. It reduces vascular permeability, stabilizes cell membranes, inclusive lysosomal ones, inhibits liberation of cytokines (interleukine and gamma-interferon) from lymphocytes and macrophages, induces involution of lymphoid tissue. It compensates sensitivity of adrenoreceptors to catecholamine. It accelerates protein catabolism, reduces glucose consumption by peripheral tissues and stimulates hepatic gluconeogenesis. It reduces absorption and increases calcium excretion retaining sodium (and water) secretion of ACTH.
Pharmacokinetics
I.v. injection: the drug is bound with specific protein-carrier transcoritin by 70-80%; in higher doses drug binding with protein is reduced to 60-70% due to transcoritin saturation. It easily penetrates histohematogenous barriers, either blood-brain and placental one. It is readily absorbed mainly in proximal section of small intestine, absorption in distal section is about half of that of proximal. Смахis reached in 1-2 h. Liver biotransformation mainly by conjugation with glucuronic and sulfuric acids to inactive metabolites. Blood half-decomposition Т1/2 is 3-5 h., biological period of half-excretion is 36-54 h. In parenteral dosing it metabolizes more rapidly, and pharmacological action is less-term. It is mainly urine-excreted (less by lactation glands) as 17-ketosteroids, glucuroids, sulphates. Urine-excretedabout 15% oforiginaldexamethasone. After skin application the absorption depends on many factors (integrity of skin surface, occlusive dressing, dosage form, etc.) and is highly variable.
Indicationsforusage
Addison's disease, congenital hypoplastic adrenal glands, adrenal gland insufficiency (usually with mineralocorticoids), adrenogenital syndrome, thyroiditis (acute, subacute), hypothyroidism, tumor hypercalcemia, shock (anaphylactic, posttraumatic, postoperative, cardiogenic, posttransfusion and others), rheumatoid in acute condition, acute rheumatic carditis, collagenosis (rheumatic disease, disseminated lupus erythematosus and others), inflammatory and degenerative joint diseases (arthritis, tendovaginitis, bursitis, epicondylitis, styloiditis, osteochondrosis, osteoarthritis, Bechterew's disease and others), myositis, infection-allergic bronchial asthma, asthmatic status, anaphylactogenic factor, either drug one, brain edema (tumor, craniocerebral injury, neurosurgical intervention, cerebral hemorrhage, encephalitis, meningitis, lung radiation damage), non-specific ulcer colitis, hepatitis, sarcoidosis, berylliosis, disseminated tuberculosis (only in combination with antituberculosis drugs), Leffler disease and other severe respiratory diseases, anemia (autoimmune, hemolytic, congential, hypoplastic, idiopathic, erythroblastopenia), idiopathic thrombocytopenic purpura (in adults), secondary thrombocytopenia, lymphoma (Hodgkin's lymphoma, non-Hodgkin's lymphoma), leukemia, lymphatic leukemia (acutem chronic), agarnulocytisis, plasmoma and other blood diseases; nephrotic syndrome; severe infections (with antibiotics only), severe inflammation after eye trauma and intervention.
Administrationanddosage
i.v., i.m., i.art., retrobulbar injections. In adults with acute and urgent state inject slowly i.v., by jet or drop ore i.m. 4-20 mg 3-4 time a day. Max.single dose is 80 mg. sustaining dose is 0.2-9 mg daily. Course of treatment is 3-4 days with further oral dosing of dexamethasone. In children i.m. dose 0.02776-0.16665 mg/kg every 12-24 h. Intra-articular (focus of damage) ir peri-articular (smooth tissues) injection for adults and teenagers 0.2-6 mg (2-8 mg), refresh in 3 days to 3 months interval subject to the case, max.adult dose 80 mg daily. In shock, for adults i.v. 20 mg single dose, further 3 mg/kg during 24 h. As discontinuous infusion or i.v. single dose 2-6 mg/kg or i.v. 40 mg every 2-6 h. in brain edema (adults) 10 mg i.v., then i.m. 4 mg every 6 h. till elimination of symptoms; decrease the dose in 2-4 days and gradually during 5-7 days calcel the treatment. In adrenocortical insufficiency (children) i.m. 0.0233 mg/kg (0.67/mg2) daily in 3 injections every third day or daily 0.00776-0.01165 mg/kg (0.233-0.335 mg/m2) daily.
Specialindications
Limitation of usage under: peptic ulcer of gastrointestinal tract, gastric and duodena ulcer, esophagitis, gastritis, intestinal anastomosis (the latest anamnesis), congestive heart failure, arterial hypertensia, thrombosis, diabetes, osteoporosis, Cushing's syndrome, acute hepatic and/or renal insufficiency, psychosis, convulsions, myasthenia, open-angle glaucoma, AIDS, pregnancy, breast feeding.
Administration in pregnancy and lactation
Pregnancy: possible dosing in pregnancy) if therapeutic effect is higher than the risk for fetus. Cancel lactation for the period of treatment.
Dosageform
Ampul of neutral glass 1 or 2 ml.
