Adrenocorticosteroids

Dr. Meera Ababneh, Pharm.D, PhD Click to edit Master subtitle style

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Adrenal Cortex

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Adrenocorticosteroids

Glucocorticoids (cortisol)

important effects on intermediary metabolism and immune function salt-retaining activity

Mineralocorticoids (aldosterone)

androgenic or estrogenic

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Glucocorticoids; Cortisol

Involved in stress response, immune response and regulation of inflammation, carbohydrate metabolism, protein catabolism, and cardiovascular function. The half-life of cortisol in the circulation is normally about 6090 min
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Pharmacological effects
Metabolic effects 1) Carbohydrate
serum glucose metabolism glucogen in liver & muscle Protein metabolism in liver but in lymphoid, connective synthesis
2)

tissue, muscle, fat and skin serum aa , urea nitrogen 3) Fat metabolism lipogenesisserum fatty acids & lipolysis, cholesterol Electrolyte & water Na+ retention , K+
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, Ca2+

& water excretion

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Pharmacological effects
Permissive effects Glucocorticoids enhances the effects of other hormones such as catecholamine, ACTH, and growth hormone Anti-inflammatory effects

Characteris tics: 1) Strong

2) 3) 4) No antibacterial effect Advantage: 5) A two sides sword Disadvantage: delaying

wound healing 7/18/12 88

Early: alleviating swelling, redness, pain Nonselective Later: limiting conglutination, scar Whole process formation of inflammation

Pharmacological

effects
Immunosuppressive effects & anti-anaphylaxis effects 1) Immunosuppressive effects Mechanisms Inhibits macrophages & other antigen-presenting cells function; Decreases circulating lymphocyte number; Low dose mainly inhibits cellular immunity, and high dose inhibits humoral immunity 2) Anti-anaphylaxis effects Inhibits histamine release by basophils / mast
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cells

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Pharmacological effects Anti shock effect

Mechanisms

Decreases inflammatory factors release; Increases body resistance to the bacterial endotoxin; Contracts blood vessel dilated & increases myocardial contractibility Decreases vascular sensitivity to some vasoconstrictors Decreases myocardial depressant factor generation because of stabilizing lysosome membrane.
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Pharmacological effects

Hematic effects
1)

Stimulation of hematopoiesis in bone marrow red cells, hemoglobin ; platelets , fibrinogen (in high dose); neutrophils increases in number, but decreases in function

2) Lymphatolysis lymphocytes in blood

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Pharmacological effects Gastrointestinal effects gastric acid , pepsin peptic ulcer Central nervous exciting effects Euphoria, excitation, insomnia; High dose induces convulsion in chidren.
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Stress and The Adrenal Glands

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Glucocorticoid Analogues

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Uses of Corticosteroids
Use to treat a number of different disorders especially inflammatory or immunologic disorders Arthritis Dermatitis Allergic reactions Asthma Hepatitis Lupus erythematosus Inflammatory bowel disease: ulcerative colitis and Crohns disease 7/18/12 Uveitis inflammation of eye

Uses of Corticosteroids
Adrenocortical insufficiency Addisons disease, anteriorhypopituitarism , postsubtotal bilateral adrenalectomy . Acute serious infections: adjuvant Bacteria infection: fulminant dysentery, bacterial meningitis, toxic pneumonia, heavy typhoid, acute miliary tuberculosis, scarlatina, septicemia Virus infection: heavy infectious hepatitis, epidemic parotitis, measles, Japanese encephalitis Sequelae of some inflammation: pyogenic meningitis, encephalitis, pericarditis, rheumatic heart disease, traumatic arthritis, testitis, 7/18/12

Autoimmunity diseases & allergic diseases Autoimmunity diseases : rheumatic fever, rheumatic myocarditis, rheumatic arthritis rheumatoid arthritis, systemic lupus erythematosus , polyarteritis nodosa, dermatomyositis, nephrotic syndrome, etc. Organ transplantation rejection Allergic diseases: urticaria, pollenosis, serum sickness, angioneurotic edema, allergic rhinitis, asthma, etc. Shocks 1) Septic shock: early, short, large dose. 2) Anaphylactic shock: the support drugs 3) Cardiogenic shock 4) Hypovolemic shock

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Hematic diseases: acute lymphoblastic leukemia, aplastic anemia, granulocytopenia, thrombocytopenia, allergic purpura syndrome Local use on skin: contact dermatitis, eczema, anus tickle, psoriasis, neurodermatitis
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Pharmacological Actions

For most clinical purposes, synthetic glucocorticoids are used because they have a higher affinity for the receptor, are less activated and have little or no salt-retaining properties. Hydrocortisone used for: orally for replacement therapy, i.v. for shock and asthma, topically for eczema (ointment) and enemas (ulcerative colitis).
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Prednisolone the most widely used

Pharmacological Actions

Betamethasone and dexamethasone: very potent, w/o salt-retaining properties; thus, very useful for highdose therapies (e.g., cerebral edemas). Beclometasone, diproprionate, budesonide: pass membranes poorly; more active when applied topically (severe eczema for local antiinflammatory effects) than orally; used in asthma, (aerosol). Triamcinolone: used for severe

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Tapering of Steroids
Very important concept when we give steroid to a patient the higher plasma levels effectively shuts down the bodies production of the drug naturally this is a drug that cannot be abruptly stopped needs to be tapered.

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When not to use Corticosteroids

Fungal infections Patients who are high risk for infection Diabetes Peptic ulcer Hypertension CHF

Renal Failure 7/18/12

How Administered

Topical skin rashes - hydrocortisone Eye drops / ear drops: cortisone ear drops or ophthalmic suspension Nasal Nasonex Tablet or liquid form prednisone, Decadron IV methyl prednisone or Solumedrol Inhaled - asthmatic or COPD

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Goals of Therapy

To reduce symptoms to a tolerable level Total suppression of symptoms may require excessive dosages Avoid serious side effects

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Clinical Pearl

Whenever possible the physician / nurse practitioner will prescribe a topical, nasal spray, eye drops or inhaled dosage before going to an oral route or intravenous route. Oral and intravenous routes are usually higher dosages and more likely to have side effects.

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Effects on the Body

Carbohydrates increased blood glucose levels Protein increase breakdown of protein Increased in blood pressure Decrease in natural cortisol production by the body

Decrease in bodies inflammatory response 7/18/12

Administration of PO Prednisone
Take with meal or snack to decrease intestinal tract upset If once a day dosing take in am before 9am If more than once daily be sure to evenly space time medication is taken In long term usage may need to take every other day in the morning so natural production is not totally 7/18/12 suppressed

Adverse Effects
Complications during chronic uses Cushings syndromes: body obesity, rounded face, increased fat around the neck, thinning arms & legs, acne, hirsutism, edema, hypokalemia, hypertension, diabetes.
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Side Effects

Moon face, buffalo hump, obese trunk (love handles), acne, hirsutism, weight gain Impaired healing or bruising CNS: nervousness, insomnia, depression, aggravation of pre-existing mental disorders Musculoskeletal: long term use can cause osteoporosis, muscle weakness and atrophy GI: peptic ulcer, increased appetite Cardiovascular: fluid retention

Ocular: increased intraocular pressure, glaucoma, cataracts 7/18/12

Moon Face

High-dose corticosteroid therapy produces a characteristic moon face appearance.

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Before and After

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Inhaled Corticosteroids

Used in asthma and COPD Provided as an inhaled medication Take daily in am Rinse and spit after treatment to prevent thrush in mouth Rinse mouth piece after use

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Oral Thrush

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