Steroids complete lecture ppt

Anabolic steroids promote protein synthesis and increase muscle mass, resulting in weight gain.
Testosterone is secreted by the testis and is the main androgen in the plasma of men. In women, testosterone (in small amounts) is secreted by the ovary and adrenal glands. Many of the androgens are modified forms of testosterone
Kinetics: Absorbed orally and from of injection site and undergoes rapid first pass metabolism and quick metabolism respectively. In order to retard the rate of absorption, testosterone esters in oil are used which are less polar than the free steroid.

1. CASE DISCUSSION SESSION-4 # Clinical_PharmD_NURSING COMPLETE LECTURE ON STEROIDS D r . S P Srinivas Nayak , PharmD , R P h , ( M sc ), (PGDND) Assistant Professor, Dept. of Pharmacy Practice

2. INTRODUCTION STEROIDS 1. Androgens (Anabolic Steroids) 2. Corticosteroids 3. Oestrogens and Progestins .

3. Androgens (Anabolic Steroids) Examples include testosterone , testosterone esters ( propionate,enanthoate , and cypionate ), danazol , fluoxymesterone , methyltestosterone , Oxandrolone (oral), Nandrolone ( im ), Stanozolol (oral), ethylestrenol (oral ), oxymetholone , Methandrostenolone ( im , oral), mesterolone , and boldenone

4. A nabolic steroids Anabolic steroids promote protein synthesis and increase muscle mass, resulting in weight gain. Testosterone is secreted by the testis and is the main androgen in the plasma of men. In women, testosterone (in small amounts) is secreted by the ovary and adrenal glands. Many of the androgens are modified forms of testosterone Kinetics: Absorbed orally and from of injection site and undergoes rapid first pass metabolism and quick metabolism respectively. In order to retard the rate of absorption, testosterone esters in oil are used which are less polar than the free steroid . NOTE: Anabolic steroids enhance muscle strength and power; hence they are often misused by athletes. Their use by athletes is prohibited. They can be detected in the urine by antidoping investigations.

5. Adverse Effects Virilising effects : Results in masculinisation when taken by women , characterised by hirsutism , acne, deepening of the voice, menstrual irregularities, male pattern baldness , prominent musculature, and hypertrophy of clitoris. Feminising effects: Seen in men who receive androgens, and is characterised by gynaecomastia . This is because of conversion (by aromatisation ) of the androgen to oestrogen in extraglandular tissues

6. ■ Administration of anabolic steroids during gestation may result in masculinisation of the urogenital sinus and clitoral hypertrophy . Premature bone maturation and decreased birthweight have been reported . ■ Growing children may develop pre-mature fusion of the epiphyses of long bones, leading to permanent short stature . ■ Cystic acne, sebaceous cysts, furunculosis , and seborrheic dermatitis have occurred in persons using anabolic steroids

7. LONG TERM USE OR AT TOXIC DOSES Oedema —Retention of water and sodium chloride leads to weight gain and oedema . ■ Jaundice —Results from stasis and accumulation of bile in biliary capillaries, There is elevation of bilirubin , ALT, AST ■ CVS effects— Hypertension and thrombotic complications (stroke , myocardial infarction ). ■ Endocrine effects— Testicular atrophy, low sperm count, sterility , gynaecomastia . ■ Behavioural changes— Increased aggressiveness, iritability , psychosis .

8. Case.1 A 38 year old man k/c/o community aquired Pneumonia, DM2 and HTN. Comes the GP with joint Pains and wants to grow his Body. His treatment chart is followed with Rx Inj. Cefperazone 1g Once Tab. Azithromycin 500mg Tab. Glimepride 2mg Tab metformin 500mg tab,. Ramipril and Tab. Oxondrolone 10mg Inj. Pheniramine maleate 25mg Question: Can we proceed Oxondrolone here? Why?

9. 2. Corticosteroids Adrenal gland has cortex and medulla. Adrenal cortex secretes steroidal hormones; adrenal medulla secretes adrenaline and noradrenaline. Hormones of adrenal cortex are Mineralocorticoids and Glucocorticoids Dr spnayak

10. cosyntropin stimulation test or standard ACTH 1–24 stimulation test To evaluate the adrenal gland activity and its response to ACTH a synthetic form of ACTH called cosyntropin is administered intramuscularly or intravenously at a dose of 0.25 mg, and the plasma cortisol level is measured before and (30 minutes) after the test. An increase in cortisol level to greater than 20 mg/100 ml indicates normal response .

11. CLASSIFICATION OF GLUCOCORTICOIDS ( a) Short acting (8–12 hours) Hydrocortisone(cortisol) Cortisone Intermediate acting (12–36 hours) Prednisolone Prednisone methyl Prednisone Tri am cinolone Long acting (36–72 hours) (i) Bet am ethasone (IM,IV, ORAL) (ii) Dex am ethasone (IM, IV ORAL) Topical AND LOCAL: alclometasone , amcinonide, betamethasone , budesonide , clobetasol , clocortolone , cortisol , desonide , desoximetasone , dexamethasone, diflorasone , fluocinolone , fluocinonide , flurandrenolide , Fluticasone , halcinonide , hydrocortisone , loteprednol . Beclomethasone .

12. ACTIONS OF GLUCOCORTICOIDS LIPID METABOLISM: redistribution of body fat that is deposited over the neck, face, shoulder , etc. resulting in ‘moon face’, ‘ buffalo hump’ and ‘ fish mouth’ with thin limbs . PROTEIN METABOLISM: Muscle wasting, lympholysis , thinning of skin, osteoporosis, growth retardation ; wound healing inhibited .

13. Cardiovascular system Glucocorticoids have sodium and water retaining property and cause HTN and CCF. Calcium metabolism (anti-vitamin D action) Prolonged use may lead to osteoporosis and pathological fracture of vertebral bodies CNS: mental depression, irritability and even psychosis. On the other hand, euphoria , insomnia, restlessness and psychosis.

14. uses Acute and chronic adrenal insufficiency Rheumatoid arthritis Rheumatic fever Allergic diseases Bronchial asthma Collagen diseases Ocular diseases Skin diseases Organ transplantation contraindications Hypertension Epilepsy Diabetes mellitus Psychosis Peptic ulcer Congestive cardiac failure Tuberculosis Renal failure Herpes simplex keratitis Glaucoma Osteoporosis

15. Case.2 A 19-year-old man complains of anorexia, fatigue, dizziness, and weight loss of 8 months’ duration. The examining physician discovers postural hypotension and moderate vitiligo ( depigmented areas of skin) and obtains routine blood tests. She finds hyponatremia , hyperkalemia, and acidosis and suspects Addison’s disease. She performs a standard ACTH 1–24 stimulation test, which reveals an insufficient plasma cortisol response, compatible with primary adrenal insufficiency. The diagnosis of autoimmune Addison’s disease is made, and the patient must start replacement of the hormones he cannot produce himself. How should this patient be treated? What precautions should he take?

16. Answer for case.2 The patient should be placed on replacement oral hydrocortisone at 10 mg/m2/d and fludrocortisone at 75 mcg/d. He should be given a Medic Alert bracelet and instructions for minor and major stress glucocorticoid coverage at 2 times and 10 times replacement of hydrocortisone over 24 and 48 hours, respectively . Explanation: In primary adrenal insufficiency, about 20–30 mg of hydrocortisone must be given daily, with increased amounts during periods of stress . Although hydrocortisone has some mineralocorticoid activity, this must be supplemented by an appropriate amount of a saltretaining hormone such as fludrocortisone.

17. Oestrogens Oestrogens are hormones secreted primarily by the ovarian follicles and also by the adrenals, corpus luteum , placenta and testes. Oestrogens are readily absorbed through the skin and mucous membranes. Following intramuscular administration of aqueous suspensions or oil solutions, absorption begins promptly and continues for several days. Examples: oestradiol , ethinyl oestradiol , polyestradiol mestranol , quinestrol , estrone , equilin , equilenin .. diethylstilbestrol , dienestrol , bisphenol A, genistein .(non steroid molecules)

18. Uses : ■ Oral contraceptive. ■ Hormone replacement therapy (in post-menopausal women). ■ Treatment of ovarian dysgenesis (Turner’s syndrome).

19. Progestins Progestins are hormones naturally secreted by the ovary mainly from the corpus luteum during the second half of the menstrual cycle , from the placenta during pregnancy, and from adrenal glands in both sexes . Progestins are used for a number of purposes, including treatment of amenorrhoea , abnormal uterine bleeding, hypoventilation, contraception (routine, as well as emergency contraception) and management of bleeding during post-menopausal therapy . Progestins are used (with oestrogens ) for hormone replacement therapy in post-menopausal women, and ( with or without oestrogens ) for contraception.

20. Case.3 A 25-year-old woman with menarche at 13 years and menstrual periods until about 1 year ago complains of hot flushes, skin and vaginal dryness, weakness, poor sleep, and scanty and infrequent menstrual periods of a year’s duration. She visits her gynecologist, who obtains plasma levels of follicle-stimulating hormone and luteinizing hormone, both of which are moderately elevated. She is diagnosed with premature ovarian failure, and estrogen and progesterone replacement therapy is recommended. A dual-energy absorptiometry scan (DEXA) reveals a bone density t-score of 2.5 SD, ie , frank osteoporosis. How should the ovarian hormones she lacks be replaced? What extra measures should she take for her osteoporosis while receiving treatment?

21. answer The patient should be advised to start daily transdermal estradiol therapy (100 mcg/d) along with oral natural progesterone ( 200mg/d) for the last 12 days of each 28-day cycle. On this regimen, her symptoms should disappear and normal monthly uterine bleeding resume. She should also be advised to get adequate exercise and increase her calcium and vitamin D intake as treatment for her osteoporosis.

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