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Deflazacort 6/30 mg
TRAINING MANUAL
Hormones secreted by Adrenal Gland: The cells of the adrenal cortex secrete a variety of steroid hormones known as CORTICOSTEROIDS. These steroids can be of 3 types: 1. Mineralocorticoids (e.g., Aldosterone) which are mainly responsible for maintaining water and electrolyte balance. 2. Glucocorticoids (e.g., Cortisol) which are mainly responsible for metabolism of glucose and proteins. 3. Gonadocorticoids (e.g., Testosterone), they are also known as sex hormones. The cells of medulla secret Adrenaline and Noradrenaline.
Functions of Glucocorticoids in our body: The glucocorticoids get their name from their effect of raising the level of blood sugar (glucose). The most abundant glucocorticoid found in our body is cortisol (also called hydrocortisone).
Glucocorticoids have a potent anti-inflammatory effect. They depress the immune response. For this reason they are widely used in therapy to reduce the inflammatory destruction of rheumatoid arthritis and other autoimmune diseases to prevent the rejection of transplanted organs to control asthma & allergic disorders Used to treat wide range of autoimmune and inflammatory diseases like conditions: Anaphylaxis, asthma, COPD, severe hypersensitivity reactions Rheumatoid arthritis, juvenile chronic arthritis Systemic lupus erythematosus Skin conditions, such as eczema and psoriasis Ulcerative colitis, Crohn's disease Uveitis, optic neuritis Autoimmune haemolytic anaemia, Idiopathic thrombocytopenia Acute and lymphatic leukaemia, malignant lymphoma, multiple myeloma. Immune suppression in transplantation.
Classification Of Glucocorticoids (based on their half life) Duration of Action Short Acting (t< 12 hrs) Intermediate acting (t 12 to 36 hrs) Long acting (t > 36 hours) Compound Hydrocortisone, Cortisone, Deflazacort Predisolone ,Methyl prednisolone Triamcinolone Paramethasone, Dexamethasone Betamethasone
Autoimmune Disorders
1. Chronic obstructive pulmonary disease (COPD) COPD is a disease state characterized by airflow limitation that is not fully reversible. The airflow limitation is usually both progressive and associated with an abnormal inflammatory response of the lungs to noxious particles or gases.
2. Asthma Asthma is a chronic disease of the respiratory system in which the airway occasionally constricts, becomes inflamed, and is lined with excessive amounts of mucus, often in response to one or more triggers. These episodes may be triggered by exposure to an environmental stimulant (or allergen), cold air, warm air, moist air, exercise or exertion, or emotional stress.
Some undesirable effects of Oral Glucocorticoids: Elevated pressure in the eyes (glaucoma) Cataracts Fluid retention, weight gain & fat Increased blood pressure Mood swings High blood sugar, which can trigger or worsen diabetes Increased risk of infections Loss of calcium from bones, which can lead to osteoporosis and fractures Menstrual irregularities Suppressed adrenal gland hormone production Thin skin, easy bruising and slower wound healing
DEFLAZEN
Deflazacort 6mg/30 mg Introduction: Deflazacort is a synthetic glucocorticoid and is used to suppress inflammation. It has been proven to having a lower risk of side effects such as bone loss, glucose intolerance or Cushings syndrome than other available steroids.
Mode of Action: Glucocorticoids (GC) are widely used for the suppression of inflammation in chronic inflammatory diseases such as asthma, R.A., inflammatory bowel disease and autoimmune diseases, all with increased expression of inflammatory genes. GC bind to GR in the cytoplasm which then translocate to the nucleus, where they bind to GC response elements (GRE) on GC-responsive genes, resulting in increased transcription for genes coding for anti-inflammatory proteins
GC increase the syntesis of lipocortin-1, that has inhibitory effect on phospholipas A2 and therefore inhibit the production of inflammatory mediators as well as inhbit genes coding for COX-2.
Inhibition of the synthesis of inflammatory Mediators as well as genes helping in the synthesis of COX-2.
Finally GCs reduce inflammatory mediators (eosinophils, T-lymphocytes, IL-8, TNF-, iNOS & COX-2)
Pharmacokinetic Parameters: Absorption: Metabolism: T max: Protein binding: T : Elimination: Rapid Through (enzymes) esterases to the pharmacologically active metabolite (D 21 OH). 1.5 to 2 hours 40% 1.1 1.9 hours Urine (70%) & Feces (30%)
Drug interaction: It is recommended to increase the maintenance dose of deflazacort if drugs, which are liver enzyme inducers, are co-administered, e.g. rifampicin, rifabutin, carbamazepine, phenobarbitone, phenytoin, primidone and aminoglutethimide. For drugs, which inhibit liver enzymes, e.g. ketoconazole, it may be possible to reduce the maintenance dose of deflazacort. The desired effects of hypoglycaemic agents (including insulin), antihypertensives and diuretics are antagonised by corticosteroids and the hypokalaemic effects of acetazolamide, loop diuretics, thiazide diuretics and carbenoxolone are enhanced. The efficacy of coumarin anticoagulants may be enhanced by concurrent corticosteroid therapy. The renal clearance of salicylates is increased by corticosteroids and steroid withdrawal may result in salicylate intoxication. As glucocorticoids can suppress the normal responses of the body to attack by microorganisms, it is important to ensure that any anti-infective therapy is effective and it is recommended to monitor patients closely. Concurrent use of glucocorticoids and oral contraceptives should be closely monitored as plasma levels of glucocorticoids may be increased. Antacids may reduce bioavailability; leave at least 2 hours between administration of deflazacort and antacids. Special warnings and precautions: Hereditary problems of galactose intolerance Cardiac disease Gastritis or oesophagitis, ulcerative colitis if there is probability of impending perforation, active or latent peptic ulcer Diabetes mellitus or a family history, Osteoporosis Renal insufficiency. Liver failure. Previous corticosteroid-induced myopathy. Hypothyroidism
Contraindications: Systemic infection unless specific anti-infective therapy is employed. Hypersensitivity to deflazacort or any of the ingredients. Patients receiving live virus immunization.
Adverse Effects: Nausea / Vomiting Gastritis / heartburn However the overall adverse events in deflazacort treated patients was lower than that in prednisolone & methylprednisolone recipients. Cushingoid syndrome
Indications: Chronic Obstructive Pulmonary Disease Bronchial Asthma Rheumatoid Arthritis Juvenile chronic arthritis Dosage: Adults For acute disorders, up to 120 mg/day deflazacort may need to be given initially. Maintenance doses in most conditions are within the range 3 - 18 mg/day. The following regimens are for guidance only. Rheumatoid arthritis: The maintenance dose is usually within the range 3 18 mg/day. The smallest effective dose should be used and increased if necessary. Bronchial asthma: In the treatment of an acute attack, high doses of 48 72 mg/day may be needed depending on severity and gradually reduced once the attack has been controlled. For maintenance in chronic asthma, doses should be titrated to the lowest dose that controls symptoms. Children: There has been limited exposure of children to deflazacort in clinical trials. In children, the indications for glucocorticoids are the same as for adults, but it is important that the lowest effective dosage is used. Doses of deflazacort usually lie in the range 0.25 - 1.5 mg/kg/day. Juvenile chronic arthritis: The usual maintenance dose is between 0.25 1.0 mg/kg/day. Bronchial asthma: The initial dose should be between 0.25 - 1.0 mg/kg deflazacort on alternate days.
Dosage Adjustment: Hepatic Impairment In patients with hepatic impairment, blood levels of deflazacort may be increased. Therefore the dose of deflazacort should be carefully monitored and adjusted to the minimum effective dose. Renal Impairment: No special precautions Elderly: No special precautions Pregnancy and lactation: The ability of corticosteroids to cross the placenta varies between individual drugs, however, deflazacort does cross the placenta. Corticosteroids are excreted in breast milk, although no data are available for deflazacort. Doses of up to 50 mg daily of deflazacort are unlikely to cause systemic effects in the infant. Conventional Glucocorticoids: Conventional glucocorticoids exert a negative influence on calcium balance, and longterm treatment with these agents leads to osteoporosis. It is well known that long-term use of steroids plays a decisive role in the development of glucose intolerance and diabetes mellitus (DM). Longer term side effects of prolonged treatment high dose prednisone can include the child becoming cushingoid. (The term refers to a typical appearance of a round face. Such a child fails to grow normally, the bones can become thin and the skin bruises easily; very occasionally the blood pressure goes up). Another rare problem is the formation of cataract in the eye. USPs: Novel Glucocorticoid Deflazacort: Deflazacort is an oxazoline derivative of prednisolone provides: Calcium-sparing properties , improves on osteoporosis and vertebral collapse Ameliorate glucose intolerance & DM. Deflazacort treatment in Progressive diaphyseal dysplasia (PDD), a rare disorder of bones, resulted in clinical and radiological improvement within 12 months with no side effects. A safer alternative in case of severe systemic juvenile chronic (rheumatoid) arthritis, does not make children so round faced, and may also allow them to continue to grow more normally.