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DRUGS & SUPPLEMENTS
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Dutimelan
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Dutimelan uses
Dutimelan consists of Cortisone Acetate, Prednisolone, Prednisolone Acetate.Cortisone Acetate:
- Indications and usage:
- Contraindications:
- Warnings:
- Precautions:
- Adverse reactions:
- Overdosage:
- Dosage and administration:
- How supplied:
INDICATIONS AND USAGE:
- Endocrine Disorders
Primary or secondary adrenocortical insufficiency (hydrocortisone or Dutimelan (Cortisone Acetate) is the first choice; synthetic analogs may be used in conjunction with mineralocorticoids where applicable; in infancy mineralocorticoid supplementation is of particular importance).
Congenital adrenal hyperplasia
Nonsuppurative thyroiditis
Hypercalcemia associated with cancer
- Rheumatic Disorders
As adjunctive therapy for short-term administration (to tide the patient over an acute episode or exacerbation) in:
Psoriatic arthritis
Rheumatoid arthritis, including juvenile rheumatoid arthritis (selected cases may require low-dose maintenance therapy)
Ankylosing spondylitis
Acute and subacute bursitis
Acute nonspecific tenosynovitis
Acute gouty arthritis
Post-traumatic osteoarthritis
Synovitis of osteoarthritis
Epicondylitis
- Collagen Diseases
During an exacerbation or as maintenance therapy in selected cases of:
Systemic lupus erythematosus
Acute rheumatic carditis
Systemic dermatomyositis (polymyositis)
- Dermatologic Diseases
Pemphigus
Bullous dermatitis herpetiformis
Severe erythema multiforme (Stevens-Johnson syndrome)
Exfoliative dermatitis
Mycosis fungoides
Severe psoriasis
Severe seborrheic dermatitis
- Allergic States
Control of severe or incapacitating allergic conditions intractable to adequate trials of conventional treatment:
Seasonal or perennial allergic rhinitis
Bronchial asthma
Contact dermatitis
Atopic dermatitis
Serum sickness
Drug hypersensitivity reactions
- Ophthalmic Diseases
Severe acute and chronic allergic and inflammatory processes involving the eye and its adnexa, such as:
Allergic conjunctivitis
Keratitis
Allergic corneal marginal ulcers
Herpes zoster ophthalmicus
Iritis and iridocyclitis
Chorioretinitis
Anterior segment inflammation
Diffuse posterior uveitis and choroiditis
Optic neuritis
Sympathetic ophthalmia
- Respiratory Diseases
Symptomatic sarcoidosis
Loeffler's syndrome not manageable by other means
Berylliosis
Fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate antituberculosis chemotherapy
Aspiration pneumonitis
- Hematologic Disorders
Idiopathic thrombocytopenic purpura in adults
Secondary thrombocytopenia in adults
Acquired (autoimmune) hemolytic anemia
Erythroblastopenia (RBC anemia)
Congenital (erythroid) hypoplastic anemia
- Neoplastic Diseases
For palliative management of:
Leukemias and lymphomas in adults
Acute leukemia of childhood
- Edematous States
To induce a diuresis or remission of proteinuria in the nephrotic syndrome, without uremia, of the idiopathic type or that due to lupus erythematosus
- Gastrointestinal Diseases
To tide the patient over a critical period of the disease in:
Ulcerative colitis
Regional enteritis
- Miscellaneous
Tuberculous meningitis with subarachnoid block or impending block when used concurrently with appropriate antituberculous chemotherapy
Trichinosis with neurologic or myocardial involvement
CONTRAINDICATIONS:
- Systemic fungal infections
- Hypersensitivity to this product
WARNINGS:
In patients on corticosteroid therapy subjected to unusual stress, increased dosage of rapidly acting corticosteroids before, during, and after the stressful situation is indicated.
Drug-induced secondary adrenocortical insufficiency may result from too rapid withdrawal of corticosteroids and may be minimized by gradual reduction of dosage. This type of relative insufficiency may persist for months after discontinuation of therapy; therefore, in any situation of stress occurring during that period, hormone therapy should be reinstituted. If the patient is receiving steroids already, dosage may have to be increased. Since mineralocorticoid secretion may be impaired, salt and/or a mineralocorticoid should be administered concurrently.
Corticosteroids may mask some signs of infection, and new infections may appear during their use. There may be decreased resistance and inability to localize infection when corticosteroids are used. Moreover, corticosteroids may affect the nitroblue-tetrazolium test for bacterial infection and produce false negative results.
In cerebral malaria, a double-blind trial has shown that the use of corticosteroids is associated with prolongation of coma and a higher incidence of pneumonia and gastrointestinal bleeding.
Corticosteroids may activate latent amebiasis. Therefore, it is recommended that latent or active amebiasis be ruled out before initiating corticosteroid therapy in any patient who has time in the tropics or any patient with unexplained diarrhea.
Prolonged use of corticosteroids may produce posterior subsapsular cataracts, glaucoma with possible damage to the optic nerves, and may enhance the establishment of secondary ocular infections due to fungi or viruses.
Average and large doses of hydrocortisone or Dutimelan can cause elevation of blood pressure, salt and water retention, and increased excretion of potassium. These effects are less likely to occur with the synthetic derivatives except when used in large doses. Dietary salt restriction and potassium supplementation may be necessary. All corticosteroids increase calcium excretion.
Administration of live virus vaccines, including smallpox, is contraindicated in individuals receiving immunosuppressive doses of corticosteroids. If inactivated viral or bacterial vaccines are administered to individuals receiving immunosuppressive doses of corticosteroids, the expected serum antibody response may not be obtained. However, immunization procedures may be undertaken in patients who are receiving corticosteroids as replacement therapy, e.g., for Addison's disease.
Persons who are on drugs which suppress the immune system are more susceptible to infections than healthy individuals. Chickenpox and measles, for example, can have more serious or even fatal course in non-immune children or adults on corticosteroids. In such children or adults who have not had these diseases, particular care should be taken to avoid exposure. How the dose, route and duration of corticosteroid administration affects the risk of developing a disseminated infection is not known. The contribution of the underlying disease and/or prior corticosteroid treatment to the risk is also not known. If exposed to chickenpox, prophylaxis with varicella zoster immune globulin (VZIG) may be indicated. If exposed to measles, prophylaxis with pooled intramuscular immunoglobulin (IG) may be indicated.. If chickenpox develops, treatment with antiviral agents may be considered.
The use of Dutimelan (Cortisone Acetate) acetate tablets in active tuberculosis should be restricted to those cases of fulminating or disseminated tuberculosis in which the corticosteroid is used for the management of the disease in conjunction with an appropriate antituberculous regimen.
If corticosteroids are indicated in patients with latent tuberculosis or tuberculin reactivity, close observation is necessary as reactivation of the disease may occur. During prolonged corticosteroid therapy, these patients should receive chemoprophylaxis.
Literature reports suggest an apparent association between use of corticosteroids and left ventricular free wall rupture after a recent myocardial infarction; therefore, therapy with corticosteroids should be used with great caution in these patients.
Usage in Pregnancy
Since adequate human reproduction studies have not been done with corticosteroids, use of these drugs in pregnancy or in women of childbearing potential requires that the anticipated benefits be weighed against the possible hazards to the mother and embryo or fetus. Infants born of mothers who have received substantial doses of corticosteroids during pregnancy should be carefully observed for signs of hypoadrenalism.
Corticosteroids appear in breast milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other unwanted effects. Mothers taking pharmacologic doses of corticosteroids should be advised not to nurse.
PRECAUTIONS:
General
Following prolonged therapy, withdrawal of corticosteroids may result in symptoms of the corticosteroid withdrawal syndrome including fever, myalgia, arthralgia, and malaise. This may occur in patients even without evidence of adrenal insufficiency.
There is an enhanced effect of corticosteroids in patients with hypothyroidism and in those with cirrhosis.
Corticosteroids should be used cautiously in patients with ocular herpes simplex because of possible corneal perforation.
The lowest possible dose of corticosteroid should be used to control the condition under treatment, and when reduction in dosage is possible, the reduction should be gradual.
Psychic derangements may appear when corticosteroids are used, ranging from euphoria, insomnia, mood swings, personality changes, and severe depression, to frank psychotic manifestations. Also, existing emotional instability or psychotic tendencies may be aggravated by corticosteroids.
Aspirin should be used cautiously in conjunction with corticosteroids in hypoprothrombinemia.
Steroids should be used with caution in nonspecific ulcerative colitis, if there is a probability of impending perforation, abscess, or other pyogenic infection, diverticulitis, fresh intestinal anastomoses, active or latent peptic ulcer, renal insufficiency, hypertension, osteoporosis, and myasthenia gravis. Signs of peritoneal irritation following gastrointestinal perforation in patients receiving large doses of corticosteroids may be minimal or absent. Fat embolism has been reported as a possible complication of hypercortisonism.
When large doses are given, some authorities advise that corticosteroids be taken with meals and antacids taken between meals to help to prevent peptic ulcer.
Growth and development of infants and children on prolonged corticosteroid therapy should be carefully observed.
Steroids may increase or decrease motility and number of spermatozoa in some patients.
Phenytoin, phenobarbital, ephedrine, and rifampin may enhance the metabolic clearance of corticosteroids, resulting in decreased blood levels and lessened physiologic activity, thus requiring adjustment in corticosteroid dosage.
The prothrombin time should be checked frequently in patients who are receiving corticosteroids and coumarin anticoagulants at the same time because of reports that corticosteroids have altered the response to these anticoagulants. Studies have shown that the usual effect produced by adding corticosteroids is inhibition of response to coumarins, although there have been some conflicting reports of potentiation not substantiated by studies.
When corticosteroids are administered concomitantly with potassium-depleting diuretics, patients should be observed closely for development of hypokalemia.
Information for Patients
Persons who are on immunosuppressant doses of corticosteroids should be warned to avoid exposure to chickenpox or measles. Patients should also be advised that if they are exposed, medical advice should be sought without delay.
ADVERSE REACTIONS:
Fluid and Electrolyte Disturbances
- Sodium retention
- Fluid retention
- Congestive heart failure in susceptible patients
- Potassium loss
- Hypokalemic alkalosis
- Hypertension
Musculoskeletal
- Muscle weakness
- Steroid myopathy
- Loss of muscle mass
- Osteoporosis
- Vertebral compression fractures
- Aseptic necrosis of femoral and humeral heads
- Pathologic fracture of long bones
- Tendon rupture
Gastrointestinal
- Peptic ulcer with possible perforation and hemorrhage
- Perforation of the small and large bowel, particularly in patients with inflammatory bowel disease
- Pancreatitis
- Abdominal distention
- Ulcerative esophagitis
Dermatologic
- Impaired wound healing
- Thin fragile skin
- Petechiae and ecchymoses
- Erythema
- Increased sweating
- May suppress reactions to skin tests
- Other cutaneous reactions, such as allergic dermatitis, urticaria, angioneurotic edema
Neurologic
- Convulsions
- Increased intracranial pressure with papilledema (pseudotumor cerbri) usually after treatment
- Vertigo
- Headache
- Psychic disturbances
Endocrine
- Menstrual irregularities
- Development of cushingoid state
- Suppression of growth in children
- Secondary adrenocortical and pituitary unresponsiveness, particularly in times of stress, as in trauma, surgery, or illness
- Decreased carbohydrate tolerance
- Manifestations of latent diabetes mellitus
- Increased requirements for insulin or oral hypoglycemic agents in diabetics
- Hirsutism
Ophthalmic
- Posterior subcapsular cataracts
- Increased intraocular pressure
- Glaucoma
- Exophthalmos
Metabolic
- Negative nitrogen balance due to protein catabolism
Cardiovascular
- Myocardial rupture following recent myocardial infarctions (see WARNINGS ).
Other
- Hypersensitivity
- Thromboembolism
- Weight gain
- Increased appetite
- Nausea
- Malaise
OVERDOSAGE:
Reports of acute toxicity and/or death following overdosage of glucocorticoids are rare. In the event of overdosage, no specific antidote is available; treatment is supportive and symptomatic.
The intraperitoneal LD50 of Dutimelan (Cortisone Acetate) acetate in female mice was 1405 mg/kg.
DOSAGE AND ADMINISTRATION:
For Oral Administration
DOSAGE REQUIREMENTS ARE VARIABLE AND MUST BE INDIVIDUALIZED ON THE BASIS OF THE DISEASE AND THE RESPONSE OF THE PATIENT.
The initial dosage varies from 25 to 300 mg a day depending on the disease being treated. In less severe diseases doses lower than 25 mg may suffice, while in severe diseases doses higher than 300 mg may be required. The initial dosage should be maintained or adjusted until the patient's response is satisfactory. If satisfactory clinical response does not occur after a reasonable period of time, discontinue Dutimelan (Cortisone Acetate) acetate tablets and transfer the patient to other therapy.
After a favorable initial response, the proper maintenance dosage should be determined by decreasing the initial dosage in small amounts to the lowest dosage that maintains an adequate clinical response.
Patients should be observed closely for signs that might require dosage adjustment, including changes in clinical status resulting from remissions or exacerbations of the disease, individual drug responsiveness, and the effect of stress (e.g., surgery, infection, trauma). During stress it may be necessary to increase dosage temporarily.
If the drug is to be stopped after more than a few days of treatment, it usually should be withdrawn gradually.
HOW SUPPLIED:
Dutimelan (Cortisone Acetate) Acetate Tablets USP 25 mg: White, Round, Scored Tablet; Imprinted "West-ward 202."
- Bottles of 100 tablets.
Store at 20-25°C (68-77°F). Protect from light and moisture.
Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.
Manufactured by:
West-ward Pharmaceutical Corp.
Eatontown, N.J. 07724
Revised July 2009
Prednisolone:
Pharmacological action
Dutimelan is a glucocorticosteroid (GCS). This medication inhibits the function of leukocytes and tissue macrophages. Dutimelan (Prednisolone) restricts the migration of leukocytes in the area of inflammation. This drug violates the ability of macrophages to phagocytosis and the formation of interleukin-1. Dutimelan (Prednisolone) contributes to the stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in inflammation. This medicine decreases capillary permeability caused by histamine release. Dutimelan (Prednisolone) inhibits the activity of fibroblasts and collagen formation.
Dutimelan (Prednisolone) inhibits the activity of phospholipase A2 which leads to suppression of the synthesis of prostaglandins and leukotrienes. This medication inhibits the release of COX (especially COX-2), which also helps reduce the production of prostaglandins.
Dutimelan (Prednisolone) reduces the number of circulating lymphocytes (T-and B-cells), monocytes, eosinophils and basophils as a result of their displacement from the bloodstream into lymphoid tissue; suppresses the formation of antibodies.
Dutimelan (Prednisolone) inhibits the release of pituitary ACTH and beta-lipotropina but it does not reduces the level of circulating beta-endorphin. This drug also inhibits the secretion of TSH and FSH.
Dutimelan (Prednisolone) has a vasoconstrictor effect with direct application to the vessels.
Dutimelan (Prednisolone) has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats. It stimulates gluconeogenesis, amino acid contributes to the capture of the liver and kidneys and increases the activity of enzymes of gluconeogenesis. In the liver, Dutimelan (Prednisolone) enhances the deposition of glycogen by stimulating the activity of glikogensintetazy and synthesis of glucose from the products of protein metabolism. This medicine increases blood glucose activates the secretion of insulin.
Dutimelan (Prednisolone) inhibits glucose uptake by fat cells that leads to the activation of lipolysis. However, due to an increase in insulin secretion is stimulated lipogenesis which contributes to the accumulation of fat.
Dutimelan (Prednisolone) also has catabolic effects in lymphoid and connective tissue, muscle, adipose tissue, skin, bone tissue. To a lesser extent than hydrocortisone Dutimelan (Prednisolone) affects the processes of water and electrolyte metabolism: promotes the excretion of potassium and calcium, delay in the body of sodium and water. Osteoporosis and Itsenko-Cushing's syndrome are the main factors limiting the long-term therapy with corticosteroids. As a result of the catabolic actions it may suppress growth in children.
In high doses prednisone can increase the excitability of brain tissue and contributes to lowering the threshold of convulsive readiness. This medication stimulates the excessive production of hydrochloric acid and pepsin in the stomach which leads to the development of peptic ulcers.
When systemic use the therapeutic activity of Dutimelan (Prednisolone) is due to anti-inflammatory, antiallergic, immunosuppressive and antiproliferative action.
For external and local application the therapeutic activity of Dutimelan (Prednisolone) is due to anti-inflammatory, antiallergic and antiexudative (due to vasoconstrictor effect) effect.
As compared with hydrocortisone the anti-inflammatory activity of Dutimelan (Prednisolone) is 4 times greater, the mineralocorticoid activity is 0.6 times smaller.
Pharmacokinetics
After oral administration Dutimelan (Prednisolone) is well absorbed from the gastrointestinal tract. Cmax in plasma observed after 90 min. In plasma most of Dutimelan (Prednisolone) is associated with transcortin (cortisol binding globulin). This drug metabolized primarily in the liver.
T1/2 is about 200 minutes.
Why is Dutimelan prescribed?
For oral and parenteral use: rheumatism; rheumatoid arthritis, dermatomyositis, periarteritis nodosa, scleroderma, ankylosing spondylitis, asthma, asthmatic status, acute and chronic allergic diseases, anaphylaxis, Addison's disease, acute adrenal insufficiency, adrenogenital syndrome; hepatitis, hepatic coma, hypoglycemic states, lipid nephrosis; agranulocytosis, various forms of leukemia, lymphoma, thrombocytopenic purpura, hemolytic anemia; chorea; pemphigus, eczema, pruritus, exfoliative dermatitis, psoriasis, pruritus, seborrheic dermatitis, SLE, erythroderma, alopecia.
For intra-articular administration: chronic arthritis, post-traumatic arthritis, osteoarthritis of large joints, rheumatic destruction of individual joints, arthritis.
For the introduction of infiltration in the tissue: epicondylitis, tenosynovitis, bursitis, frozen shoulder, keloids, sciatica, Dupuytren's contracture, rheumatism and similar lesions of joints and various tissues.
For use in ophthalmology: allergies, chronic and atypical conjunctivitis and blepharitis; inflammation of the cornea with intact mucosa; acute and chronic inflammation of the anterior segment of the choroid, sclera and episcleritis; sympathetic inflammation of the eyeball; after injuries and operations during prolonged stimulation of eyeballs.
Dosage and administration
When Dutimelan administered orally for replacement therapy in adults the initial dose is 20-30 mg, maintenance dose is 10.5 mg / day. If necessary, the initial dose is may be 15-100 mg / day, the maintenance one is 5-15 mg / day. The daily dose should be reduced gradually. For children the starting dose is 1-2 mg / kg in 4-6 receptions, the maintenance one is 300-600 mg / kg / day.
For IM or IV dose administration the multiplicity and duration of application are determined individually.
When intra-articular administration in large joints it used a dose of 25-50 mg, for medium-sized joints - 10-25 mg for small joints - 5-10 mg. For the introduction of infiltration into the tissues depending on disease severity and magnitude of the defeat use doses from 5 mg to 50 mg.
Dutimelan (Prednisolone) used topically in ophthalmology 3 times / day, course of treatment is no more than 14 days; in dermatology - 1-3 times / day.
Dutimelan (Prednisolone) side effects, adverse reactions
Endocrine system: menstrual irregularities, suppression of adrenal function, Itsenko-Cushing's syndrome, suppression of pituitary-adrenal system, reduced tolerance to carbohydrates, steroid diabetes, or a manifestation of latent diabetes, growth retardation in children, delayed sexual development in children.
Digestive system: nausea, vomiting, steroid ulcer and duodenal ulcer, pancreatitis, esophagitis, bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, flatulence, hiccups. In rare cases - elevated liver transaminases and alkaline phosphatase.
Metabolism: the negative nitrogen balance due to protein catabolism, increased excretion of calcium from the body, hypocalcemia, weight gain, increased sweating.
Cardiovascular system: the loss of potassium, hypokalemic alkalosis, arrhythmia, bradycardia (up to cardiac arrest); steroid myopathy, heart failure (the development or worsening of symptoms), ECG changes typical of hypokalemia, increased blood pressure, hypercoagulability, thrombosis. In patients with acute myocardial infarction - the spread of necrosis, slowing the formation of scar tissue that can lead to rupture of the heart muscle.
Musculoskeletal system: slowing growth and ossification processes in children (premature closure of epiphyseal growth zones) and osteoporosis (very rarely - pathological fractures, aseptic necrosis of the humeral head and femoral), rupture of tendons of muscles, muscle weakness, steroid myopathy, loss of muscle mass (atrophy).
CNS: headache, increased intracranial pressure, delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, nervousness or anxiety, insomnia, dizziness, vertigo, pseudotumor cerebellum, and seizures.
Vision: the rear subcapsular cataracts, increased intraocular pressure (with the possible damage to the optic nerve), trophic changes of the cornea, exophthalmos, the propensity to develop secondary infections (bacterial, fungal, viral).
Dermatological reactions: petechiae, ecchymosis, thinning and fragility of the skin, hyper- or hypopigmentation, acne, stretch marks, susceptibility to the development of pyoderma and candidiasis.
Reactions due to immunosuppressive effect: slow process of regeneration, reduced resistance to infections.
For parenteral administration: in rare cases of anaphylactic and allergic reactions, hyper- or hypopigmentation, atrophy of skin and subcutaneous tissue, exacerbation after intrasinovialnogo applications such as Charcot arthropathy, sterile abscesses, when injected into pockets on the head - blindness.
Dutimelan contraindications
For short-term use for health reasons - increased sensitivity to Dutimelan (Prednisolone).
For intra-articular injection and injection directly into the lesion: previous arthroplasty, abnormal bleeding (endogenous or caused by the use of anticoagulants), intra-articular fracture, infection (sepsis) inflammation in the joints and periarticular infections (including in history), as well as general infectious disease marked juxta-articular osteoporosis, lack of signs of inflammation in the joints ("dry" joint, such as osteoarthritis without synovitis), severe bone destruction and deformity of the joint (a sharp narrowing of joint space, ankylosis), the instability of the joint as a result of arthritis, aseptic necrosis of the epiphyses of bones forming the joint.
For external use only: bacterial, viral, fungal skin diseases, tuberculosis, skin, cutaneous manifestations of syphilis, skin tumors, post-vaccination period, violation of the integrity of the skin (ulcers, wounds), children's age (up to 2 years, with itching in the anal area - up to 12 years), rosacea, acne vulgaris, perioral dermatitis.
For use in ophthalmology: bacterial, viral, fungal eye diseases, tuberculosis eye disease, trachoma, violating the integrity of ocular epithelium.
Using during pregnancy and breastfeeding
During pregnancy Dutimelan (Prednisolone) is used only for health reasons. If necessary use of Dutimelan (Prednisolone) during lactation should carefully weigh the potential benefits of treatment for both mother and child at risk.
Special instructions
With care use for parasitic and infectious diseases of viral, fungal or bacterial origin - herpes simplex, herpes zoster (viraemic phase), chicken pox, measles, amoebiasis, strongyloidiasis, systemic mycosis, active and latent tuberculosis.
Be wary of up to 8 weeks before and 2 weeks after vaccination, and lymphadenitis after BCG, with immunodeficiency (including AIDS or HIV infection).
Be wary of diseases in gastrointestinal tract: gastric ulcers and duodenal ulcers, esophagitis, gastritis, acute or latent peptic ulcer, the newly created anastomosis intestinal ulcerative colitis with the threat of perforation or abstsedirovaniya, diverticulitis. Be wary of Dutimelan (Prednisolone) use in diseases of the cardiovascular system, including after recent myocardial infarction, with decompensated congestive heart failure, hypertension, hyperlipidemia, with endocrine diseases - diabetes mellitus, hyperthyroidism, hypothyroidism, pituitary basophilia, with severe chronic renal and / or liver failure, nefrourolitiaze, with hypoalbuminemia, with systemic osteoporosis, myasthenia gravis, acute psychosis, obesity III-IV stage, in poliomyelitis, open- and closed-angle glaucoma.
If necessary, intra-articular injection with caution in patients with severe general condition, failure (or brevity) of the 2 previous injections (with regard to individual properties apply GCS). During treatment (especially long-term) it needed to monitor at eye specialist, blood pressure control and water-electrolyte balance, and the pattern of peripheral blood glucose levels; to reduce the side effects can be assigned anabolic steroids, antibiotics, and increase the flow of potassium in the body (diet, potassium containing medications).
It is recommended to clarify the need for injection of ACTH after treatment with prednisone (after a skin test).
When Addison's disease should avoid the simultaneous use of barbiturates.
After cessation of treatment it may be experience a withdrawal syndrome, adrenal insufficiency and exacerbation of the disease, about which he was appointed Dutimelan (Prednisolone) Rotexmedica.
When intercurrent infections, septic conditions, and tuberculosis, must be simultaneous antibiotic therapy.
The children in the period of growth GCS should be used only if absolutely indicated and under close medical supervision.
Externally Dutimelan (Prednisolone) should not be used for more than 14 days. In case of application for ordinary or pink acne perhaps exacerbation.
Dutimelan drug interactions
Simultaneous administration of Dutimelan (Prednisolone) with:
Dutimelan in case of emergency / overdose
Risk of overdose increases with prolonged use of prednisone, particularly in large doses.
Symptoms: increased blood pressure, peripheral edema, increased side effects of the drug.
Treatment of acute overdose: an immediate gastric lavage or induction of vomiting, specific antidote is not found.
Treatment of chronic overdose: should reduce the dose of the drug.
Prednisolone Acetate:
Pharmacological action
Dutimelan is a glucocorticosteroid (GCS). This medication inhibits the function of leukocytes and tissue macrophages. Dutimelan (Prednisolone Acetate) restricts the migration of leukocytes in the area of inflammation. This drug violates the ability of macrophages to phagocytosis and the formation of interleukin-1. Dutimelan (Prednisolone Acetate) contributes to the stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in inflammation. This medicine decreases capillary permeability caused by histamine release. Dutimelan (Prednisolone Acetate) inhibits the activity of fibroblasts and collagen formation.
Dutimelan (Prednisolone Acetate) inhibits the activity of phospholipase A2 which leads to suppression of the synthesis of prostaglandins and leukotrienes. This medication inhibits the release of COX (especially COX-2), which also helps reduce the production of prostaglandins.
Dutimelan (Prednisolone Acetate) reduces the number of circulating lymphocytes (T-and B-cells), monocytes, eosinophils and basophils as a result of their displacement from the bloodstream into lymphoid tissue; suppresses the formation of antibodies.
Dutimelan (Prednisolone Acetate) inhibits the release of pituitary ACTH and beta-lipotropina but it does not reduces the level of circulating beta-endorphin. This drug also inhibits the secretion of TSH and FSH.
Dutimelan (Prednisolone Acetate) has a vasoconstrictor effect with direct application to the vessels.
Dutimelan (Prednisolone Acetate) has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats. It stimulates gluconeogenesis, amino acid contributes to the capture of the liver and kidneys and increases the activity of enzymes of gluconeogenesis. In the liver, Dutimelan (Prednisolone Acetate) enhances the deposition of glycogen by stimulating the activity of glikogensintetazy and synthesis of glucose from the products of protein metabolism. This medicine increases blood glucose activates the secretion of insulin.
Dutimelan (Prednisolone Acetate) inhibits glucose uptake by fat cells that leads to the activation of lipolysis. However, due to an increase in insulin secretion is stimulated lipogenesis which contributes to the accumulation of fat.
Dutimelan (Prednisolone Acetate) also has catabolic effects in lymphoid and connective tissue, muscle, adipose tissue, skin, bone tissue. To a lesser extent than hydrocortisone Dutimelan (Prednisolone Acetate) affects the processes of water and electrolyte metabolism: promotes the excretion of potassium and calcium, delay in the body of sodium and water. Osteoporosis and Itsenko-Cushing's syndrome are the main factors limiting the long-term therapy with corticosteroids. As a result of the catabolic actions it may suppress growth in children.
In high doses prednisone can increase the excitability of brain tissue and contributes to lowering the threshold of convulsive readiness. This medication stimulates the excessive production of hydrochloric acid and pepsin in the stomach which leads to the development of peptic ulcers.
When systemic use the therapeutic activity of Dutimelan (Prednisolone Acetate) is due to anti-inflammatory, antiallergic, immunosuppressive and antiproliferative action.
For external and local application the therapeutic activity of Dutimelan (Prednisolone Acetate) is due to anti-inflammatory, antiallergic and antiexudative (due to vasoconstrictor effect) effect.
As compared with hydrocortisone the anti-inflammatory activity of Dutimelan (Prednisolone Acetate) is 4 times greater, the mineralocorticoid activity is 0.6 times smaller.
Pharmacokinetics
After oral administration Dutimelan (Prednisolone Acetate) is well absorbed from the gastrointestinal tract. Cmax in plasma observed after 90 min. In plasma most of Dutimelan (Prednisolone Acetate) is associated with transcortin (cortisol binding globulin). This drug metabolized primarily in the liver.
T1/2 is about 200 minutes.
Why is Dutimelan prescribed?
For oral and parenteral use: rheumatism; rheumatoid arthritis, dermatomyositis, periarteritis nodosa, scleroderma, ankylosing spondylitis, asthma, asthmatic status, acute and chronic allergic diseases, anaphylaxis, Addison's disease, acute adrenal insufficiency, adrenogenital syndrome; hepatitis, hepatic coma, hypoglycemic states, lipid nephrosis; agranulocytosis, various forms of leukemia, lymphoma, thrombocytopenic purpura, hemolytic anemia; chorea; pemphigus, eczema, pruritus, exfoliative dermatitis, psoriasis, pruritus, seborrheic dermatitis, SLE, erythroderma, alopecia.
For intra-articular administration: chronic arthritis, post-traumatic arthritis, osteoarthritis of large joints, rheumatic destruction of individual joints, arthritis.
For the introduction of infiltration in the tissue: epicondylitis, tenosynovitis, bursitis, frozen shoulder, keloids, sciatica, Dupuytren's contracture, rheumatism and similar lesions of joints and various tissues.
For use in ophthalmology: allergies, chronic and atypical conjunctivitis and blepharitis; inflammation of the cornea with intact mucosa; acute and chronic inflammation of the anterior segment of the choroid, sclera and episcleritis; sympathetic inflammation of the eyeball; after injuries and operations during prolonged stimulation of eyeballs.
Dosage and administration
When Dutimelan administered orally for replacement therapy in adults the initial dose is 20-30 mg, maintenance dose is 10.5 mg / day. If necessary, the initial dose is may be 15-100 mg / day, the maintenance one is 5-15 mg / day. The daily dose should be reduced gradually. For children the starting dose is 1-2 mg / kg in 4-6 receptions, the maintenance one is 300-600 mg / kg / day.
For IM or IV dose administration the multiplicity and duration of application are determined individually.
When intra-articular administration in large joints it used a dose of 25-50 mg, for medium-sized joints - 10-25 mg for small joints - 5-10 mg. For the introduction of infiltration into the tissues depending on disease severity and magnitude of the defeat use doses from 5 mg to 50 mg.
Dutimelan (Prednisolone Acetate) used topically in ophthalmology 3 times / day, course of treatment is no more than 14 days; in dermatology - 1-3 times / day.
Dutimelan (Prednisolone Acetate) side effects, adverse reactions
Endocrine system: menstrual irregularities, suppression of adrenal function, Itsenko-Cushing's syndrome, suppression of pituitary-adrenal system, reduced tolerance to carbohydrates, steroid diabetes, or a manifestation of latent diabetes, growth retardation in children, delayed sexual development in children.
Digestive system: nausea, vomiting, steroid ulcer and duodenal ulcer, pancreatitis, esophagitis, bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, flatulence, hiccups. In rare cases - elevated liver transaminases and alkaline phosphatase.
Metabolism: the negative nitrogen balance due to protein catabolism, increased excretion of calcium from the body, hypocalcemia, weight gain, increased sweating.
Cardiovascular system: the loss of potassium, hypokalemic alkalosis, arrhythmia, bradycardia (up to cardiac arrest); steroid myopathy, heart failure (the development or worsening of symptoms), ECG changes typical of hypokalemia, increased blood pressure, hypercoagulability, thrombosis. In patients with acute myocardial infarction - the spread of necrosis, slowing the formation of scar tissue that can lead to rupture of the heart muscle.
Musculoskeletal system: slowing growth and ossification processes in children (premature closure of epiphyseal growth zones) and osteoporosis (very rarely - pathological fractures, aseptic necrosis of the humeral head and femoral), rupture of tendons of muscles, muscle weakness, steroid myopathy, loss of muscle mass (atrophy).
CNS: headache, increased intracranial pressure, delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, nervousness or anxiety, insomnia, dizziness, vertigo, pseudotumor cerebellum, and seizures.
Vision: the rear subcapsular cataracts, increased intraocular pressure (with the possible damage to the optic nerve), trophic changes of the cornea, exophthalmos, the propensity to develop secondary infections (bacterial, fungal, viral).
Dermatological reactions: petechiae, ecchymosis, thinning and fragility of the skin, hyper- or hypopigmentation, acne, stretch marks, susceptibility to the development of pyoderma and candidiasis.
Reactions due to immunosuppressive effect: slow process of regeneration, reduced resistance to infections.
For parenteral administration: in rare cases of anaphylactic and allergic reactions, hyper- or hypopigmentation, atrophy of skin and subcutaneous tissue, exacerbation after intrasinovialnogo applications such as Charcot arthropathy, sterile abscesses, when injected into pockets on the head - blindness.
Dutimelan contraindications
For short-term use for health reasons - increased sensitivity to Dutimelan (Prednisolone Acetate).
For intra-articular injection and injection directly into the lesion: previous arthroplasty, abnormal bleeding (endogenous or caused by the use of anticoagulants), intra-articular fracture, infection (sepsis) inflammation in the joints and periarticular infections (including in history), as well as general infectious disease marked juxta-articular osteoporosis, lack of signs of inflammation in the joints ("dry" joint, such as osteoarthritis without synovitis), severe bone destruction and deformity of the joint (a sharp narrowing of joint space, ankylosis), the instability of the joint as a result of arthritis, aseptic necrosis of the epiphyses of bones forming the joint.
For external use only: bacterial, viral, fungal skin diseases, tuberculosis, skin, cutaneous manifestations of syphilis, skin tumors, post-vaccination period, violation of the integrity of the skin (ulcers, wounds), children's age (up to 2 years, with itching in the anal area - up to 12 years), rosacea, acne vulgaris, perioral dermatitis.
For use in ophthalmology: bacterial, viral, fungal eye diseases, tuberculosis eye disease, trachoma, violating the integrity of ocular epithelium.
Using during pregnancy and breastfeeding
During pregnancy Dutimelan (Prednisolone Acetate) is used only for health reasons. If necessary use of Dutimelan (Prednisolone Acetate) during lactation should carefully weigh the potential benefits of treatment for both mother and child at risk.
Special instructions
With care use for parasitic and infectious diseases of viral, fungal or bacterial origin - herpes simplex, herpes zoster (viraemic phase), chicken pox, measles, amoebiasis, strongyloidiasis, systemic mycosis, active and latent tuberculosis.
Be wary of up to 8 weeks before and 2 weeks after vaccination, and lymphadenitis after BCG, with immunodeficiency (including AIDS or HIV infection).
Be wary of diseases in gastrointestinal tract: gastric ulcers and duodenal ulcers, esophagitis, gastritis, acute or latent peptic ulcer, the newly created anastomosis intestinal ulcerative colitis with the threat of perforation or abstsedirovaniya, diverticulitis. Be wary of Dutimelan (Prednisolone Acetate) use in diseases of the cardiovascular system, including after recent myocardial infarction, with decompensated congestive heart failure, hypertension, hyperlipidemia, with endocrine diseases - diabetes mellitus, hyperthyroidism, hypothyroidism, pituitary basophilia, with severe chronic renal and / or liver failure, nefrourolitiaze, with hypoalbuminemia, with systemic osteoporosis, myasthenia gravis, acute psychosis, obesity III-IV stage, in poliomyelitis, open- and closed-angle glaucoma.
If necessary, intra-articular injection with caution in patients with severe general condition, failure (or brevity) of the 2 previous injections (with regard to individual properties apply GCS). During treatment (especially long-term) it needed to monitor at eye specialist, blood pressure control and water-electrolyte balance, and the pattern of peripheral blood glucose levels; to reduce the side effects can be assigned anabolic steroids, antibiotics, and increase the flow of potassium in the body (diet, potassium containing medications).
It is recommended to clarify the need for injection of ACTH after treatment with prednisone (after a skin test).
When Addison's disease should avoid the simultaneous use of barbiturates.
After cessation of treatment it may be experience a withdrawal syndrome, adrenal insufficiency and exacerbation of the disease, about which he was appointed Dutimelan (Prednisolone Acetate) Rotexmedica.
When intercurrent infections, septic conditions, and tuberculosis, must be simultaneous antibiotic therapy.
The children in the period of growth GCS should be used only if absolutely indicated and under close medical supervision.
Externally Dutimelan (Prednisolone Acetate) should not be used for more than 14 days. In case of application for ordinary or pink acne perhaps exacerbation.
Dutimelan drug interactions
Simultaneous administration of Dutimelan (Prednisolone Acetate) with:
Dutimelan in case of emergency / overdose
Risk of overdose increases with prolonged use of prednisone, particularly in large doses.
Symptoms: increased blood pressure, peripheral edema, increased side effects of the drug.
Treatment of acute overdose: an immediate gastric lavage or induction of vomiting, specific antidote is not found.
Treatment of chronic overdose: should reduce the dose of the drug.
Dutimelan pharmaceutical active ingredients containing related brand and generic drugs:
Dutimelan available forms, composition, doses:
Composition is the list of ingredients which combinedly form a medicine. Both active ingredients and inactive ingredients form the composition. The active ingredient gives the desired therapeutic effect whereas the inactive ingredient helps in making the medicine stable.
Doses are various strengths of the medicine like 10mg, 20mg, 30mg and so on. Each medicine comes in various doses which is decided by the manufacturer, that is, pharmaceutical company. The dose is decided on the severity of the symptom or disease.