Steroids and anabolic steroids

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STEROIDS &

ANABOLIC STEROIDSBy: Mrs. Kalaivani Sathish,

Asst Professor,PIMS - Panipat

INTRODUCTION

• Corticosteroids are a class of steroid hormones that are produced in the adrenal cortex.

• Corticosteroids includes natural glucocorticoids and mineralocorticoids, and their synthetic analogues.

Functions of Steroids

• Stress response• Immune response• Regulation of inflammation• Carbohydrate metabolism• Protein catabolism• Blood electrolyte level maintenance• Control of behavior

Biosynthesis• Synthesis of steroids are from adrenal cortical

cells from cholesterol.• Adrenal cortex is divided into three zones

– Zona glomerulosa – mineralocorticoids such as aldosterone, which regulates sodium and water are produced.

– Zona fasiculata – glucocorticoids such as hydrocortisone and corticosterone, which regulates carbohydrate and protein metabolism and Na+ & H20 balance are produced.

Biosynthesis (Cont..)– Zona reticularis– involved in the biosynthesis of

androgens.

STEROIDS CLASSIFICATIONSMineralocorticoids (Cortisone,

Fludrocortisone)Glucocorticoids (Betamethasone,

Methylprednisolone)Sex Steroids (Estrogen, Progestins)

MECHANISM OF ACTION• Steroids in blood binds to transcortin

• Glucocorticods molecules binds to cytoplasmic receptor protein

• Structural changes occurs in receptor steroid Complex

• Migration of steroid complex into nucleus

MECHANISM OF ACTION

• Binding of glucocorticoid response elements on the chromatin.

• Suppression of genes

• Genes inhibition contributes to their anti-inflammatory & Immunosuppressive

action.

PHARMACOLOGIC ACTION• Carbohydrate and Protein Metabolism• Fat Metabolism – promotes lipolysis• Calcium metabolism & water excretion• Cardiovascular – permissive effects• Skeletal muscles – weakness in case of hypo

and hypercorticism• CNS – Precipitates seizure in epileptic patients.• Stomach – increased secretion of gastric acid

and pepsin.

PHARMACOLOGIC ACTION• Hemopoitic System - se in number of

RBC’s & Platelets, but decrease in lymphocytes, eosinophills and basophils.

• Inflammatory Response– reduction of phagocytic activity.

• Immunologic and allergic response – Suppresses all types of allergic phenomenon and hypersensitization.

Pharmacokinetics• Absorption – effective in oral route, acts rapidly by

IV / IM.• Bioavailability – oral bioavailability of synthetic

corticosteroids are high.• Plasma protein binding is 90 %.• Metabolism by hepatic microsomal enzymes.• Excretion – urine• Distribution – widely distributed – 10L/Kg• Plasma t ½ - 66 minutes.

Preparations & Doses

• Synthetic steroids have largely replaced the natural compounds in therapeutic use because they are potent, longer acting and more selective for glucocorticoid / mineralocorticoid actions.

Preparations & Doses(Glucocorticoids)

Category Compound

Short Acting (t1/2 <12h) Hydrocortisone (cortisol)

Intermediate acting (t1/2 12 – 36 h) PrednisoloneMethylprednisolone

Long acting (t1/2 > 36 h) DexamethasoneBetamethasone

Doses & Routes(Glucocorticoids)

Category Compound

Short Acting (t1/2 <12h) Hydrocortisone (cortisol) 20 mg, 100 mgOral, IV

Intermediate acting (t1/2 12 – 36 h) Prednisolone 5 – 60 mg / day oral, IMMethylprednisolone 4 – 32 mg, Oral, IV

Long acting (t1/2 > 36 h) Dexamethasone 0.5 – 5 mg / day oral, IV, IMBetamethasone 0.5 – 5 mg / day oral, IV, IM

Doses & Routes(Mineralocorticoids)

Category Compound

Mineralocorticoids Desoxycortisone 2 – 5 mg once or twice weekly, sublingual, IM

Aldosterone

(Aldosterone is not used clinically)

Indications

– Replacement Therapy: Acute adrenal insufficiency,

Chronic adrenal insufficiency and congenital adrenal

hyperplasia.

– Pharmacotherapy: Collagen disease, Arthritis, Severe

allergic reactions, Autoimmune disease, Bronchial asthma,

Infective diseases, Eye diseases, Skin diseases, intestinal

diseases, cerebral edema, Malignancies, Organ

transplantation and skin alograft, septic shock, thyroid

storm.

CONTRA INDICATIONS

ABSOLUTE• Hypersensitivity• Cushing syndrome• Herpes Ocular Infections

RELATIVE• Peptic ulcer• DM and HTN• Viral and fungal infections• TB• Osteoporosis• Psychosis• Epilepsy• CHF• Renal failure

ADVERSE EFFECTS• Occurs usually with prolonged therapy

• Mineralocorticoids • Na and water retention, edema,

hypokalemic alkalosis and HTN.• Glucocorticoids

• Cushing habitus – Characterized by moon like face, accumulation of fat in the truncal region.

ADVERSE EFFECTS• Glucocorticoids

• Hyperglycemia and Glycosuria• Myopathy & Muscle• Susceptibility to infections• Peptic ulceration• Osteoporosis• Glaucoma • Growth retardation in children• Fetal abnormality (IUGR)

NURSES ROLE• Check vital signs, lung sounds, BP and

weight.• Conduct MSE, to assess for depression,

withdrawal, Insomnia and anorexia.• Advise regular opthalmic examination• Check stool for occult blood periodically.• Administer suitable antibiotics as prescribed. •

ANABOLIC STEROIDS

DEFINITION• These are androgens with anabolic

properties and are rarely prescribed., but are commonly abused by athletes in an

attempt to enhance performance.• They are developed in replace of androgens.

MECHANISM OF ACTION• Testosterone is converted to active metabolite

dihydrotestosterone

• Increased synthesis of RNA & Cellular protein

• Stimulate growth of muscle, bone, skin and hair and accelerate closure of epiphyses at ends

of long bones. (ed the RBC production)

• Indications – Growth and development retardation.– Ulcerative colitis– Osteoporosis– Aplastic anemia– After trauma & surgery– Prolonged immobilization

• Contra Indications• Pregnancy, Lactation, CHF, Renal failure,

Liver failure and prostate enlargement.

• Adverse Effects• Hepatotoxicity

• Hepatitis B & C• Abusers of anabolic steroids use same needles so risk of

HIV / AIDS.• Nurses Role

• Do not administer for more than 90 days.• Assess the client for Liver function edema, weight gain

and skin changes• Evaluate the client for signs of depression.

• Warm and shake vials before administer to prevent crystals. Administer in deep into gluteal muscles