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GLUCOCORTICOIDS AND MINERALOCORTICOIDS

GLUCOCORTICOIDS AND MINERALOCORTICOIDS. Corticosteroids. Adrenal glands produce glucocorticoids and mineralocorticoids Glucocorticoids: Involved in cholesterol, fat, and protein metabolism. Corticosteroids. Adrenal glands produce glucocorticoids and mineralocorticoids Glucocorticoids:

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GLUCOCORTICOIDS AND MINERALOCORTICOIDS

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  1. GLUCOCORTICOIDS AND MINERALOCORTICOIDS

  2. Corticosteroids • Adrenal glands produce glucocorticoids and mineralocorticoids • Glucocorticoids: • Involved in cholesterol, fat, and protein metabolism

  3. Corticosteroids • Adrenal glands produce glucocorticoids and mineralocorticoids • Glucocorticoids: • Involved in cholesterol, fat, and protein metabolism • Mineralocorticoids: • Involved in regulating electrolyte and water balance

  4. Cortisol • Principal adrenal steroid hormone • Responsible for: • Gluconeogenesis • Protein catabolism • Anti-inflammatory reactions • Stimulation of fat deposition • Sodium and water retention

  5. Corticosteroids • Adrenal hormones excluding sex hormones • Steroid production follows a circadian rhythm

  6. Properties of glucocorticosteroides used in clinics • Anti-inflammatory • Immune-depressive • Anti-allergic • Anti-shock • Anti-toxic

  7. Anti-inflammatory action of GCS • Nonspecific inflammation • Auto-immune component • Hyperergic character • Therapy of despair

  8. Mechanism of anti-inflammatory action of GCS GCS activation of lipomoduline decreasing of activity of phospholipaseА2 slowing down of arachidonic acid metabolites production (prostaglandins, leucotriens, thromboxanА2) stabilization of cellular and lyzosomal membranes decreasing of capillaries’ wall permeability decreasing of leucocytes’ migration processes, depression of phagocytes activity depression of histamine, serotonin, bradykinine releasing

  9. Indications for administration of GCS • Insufficiency of adrenal cortex • Rheumatoid illnesses (rheumatoid arthritis, rheumatism, system red lupus etc.) • Chronic active hepatitis • Bronchial asthma • Ulcerative colitis • Nephritic syndrome • Auto-immune hemolytic anemia • Shock and collapse of any etiology • Brain, lungs, larynx edema • Acute allergic reactions • Transfusion reactions • Heavy infections (hiding behind the etiotropic drugs!) • Liver disesaes

  10. Doses and terms of GCS therapy

  11. Corticosteroids • Act as anti-inflammatory and immunosuppressive agents in treating diseases of different origins: • Hematologic • Allergic • Inflammatory • Neoplastic • Autoimmune

  12. Addison’s Disease • Life-threatening deficiency of glucocorticoids and mineralocorticoids • Treated with daily corticosteroids

  13. Symptoms of Addison’s Disease • Debilitating weakness • Hyperkalemia • Hyperpigmentation of skin • Low levels of serum sodium and glucose • Reduced blood pressure • Weight loss

  14. Cushing’s Disease • Caused by an overproduction of steroids or excessive administration of corticosteroids • Symptoms: • Protruding abdomen; round, puffy face; fat over the shoulder blades

  15. Reasons for Using Corticosteroids • Inhibit inflammation • Useful in treating asthma, rashes, and skin disorders • Available in many different dosage forms

  16. Problems with Corticosteroids • Lessen the ability of leukocytes to destroy infection which decreases fever, redness, and swelling • Also may cause infection to spread

  17. Corticosteroid Dispensing Issues • Take caution in patients with diabetes, uncontrolled hypertension, CHF, severe infection or altered immunity, or peptic ulcer disease with active GI bleeding Warning!

  18. Corticosteroids • Usage must be tapered off, not abruptly stopped • May cause withdrawal symptoms • Anorexia, nausea, vomiting, myalgia, arthralgia, lethargy, headache, sluggishness, weight loss, postural hypotension, fever and depression • Doses should be given in the morning

  19. Adverse Effects of Glucocorticoids • Cardiovascular effects • Dermatologic effects • Gastrointestinal effects • Immune system effects • Metabolic effects • Musculoskeletal effects • Neuropsychiatric effects • Ophthalmic effects

  20. Adrenal Sex Hormones • Androgens are produced by: • The testes • The ovaries • Adrenals • Peripheral fat tissue • Most important male hormone is testosterone which is produced by the testes

  21. Responsibilities of Testosterone • Initiating sperm production • Behavioral characteristics • Libido • Sexual potency • Muscle mass and strength • Fat distribution • Bone mass • Erythropoiesis • Prevention of baldness

  22. Hypogonadism • Deficient hormone production and secretion • Androgens must be replaced by medications • May cause virilization, muscle building, and hematologic stimulation of erythropoiesis • Can be used to treat anemia, breast cancer, or endometriosis

  23. Androgen’s Side Effects • Virilization • Hirsutism • Acne • Hepatoxicity • High levels of erythrocytes • Oily skin • Gynecomastia • Priapism

  24. Male Impotence • Failure to initiate or maintain an erection until ejaculation • Causes: • Testosterone deficiency • Alcoholism • Cigarette smoking • Psychological factors • Medications

  25. Alcohol (most significant) Amphetamines Antihypertensives Corticosteroids Estrogens H2 blockers haloperidol lithium Opiates Some antidepressants Drugs That May Cause Impotence

  26. Drug List Agents for Male Impotence • alprostadil (Caverject, Edex, Muse) • danazol (Danocrine) • methyltestosterone (Android, Testred) • oxymetholone (Anadrol) • papaverine • testosterone (Androderm, AndroGel, Striant, Testoderm)

  27. Drug List Agents for Male Impotence – Phosphodiesterase Inhibitors • sildenafil (Viagra) • tadalafil (Cialis) • vardenafil (Levitra)

  28. sildenafil (Viagra) • 1st oral therapy for impotence • Allows an erection to occur naturally • Take at least 1 hour before activity

  29. sildenafil Dispensing Issues • Potentially lethal interaction with nitrates Warning!

  30. tadalafil (Cialis) • Duration of action is 36 hours • Faster onset and longer duration than others in this class

  31. tadalafil Dispensing Issues • Potentially lethal interaction with nitrates Warning!

  32. Female Hormones • Can prevent conception, ease symptoms of menopause, and help prevent osteoporosis • 2 main female hormones: • Estrogen • Progesterone

  33. Estrogen • Formed in the ovaries when FSH is released • Responsible for: • Endometrial growth • Increased cervical mucus • Cornification of vaginal mucosa • Growth of breast tissue • Increased epiphyseal closure • Sodium retention • Carbohydrate metabolism • Calcium utilization

  34. Estrogen Deficiency Symptoms • Irregular bleeding and cycles • “hot flashes” that start in the face and move down through the body • Atrophic vulvovaginitis, excessive dryness • Dyspareunia • Frequent infections

  35. Menopause • As women reach menopause estrogen production decreases • HRT can be used to supplement estrogen levels

  36. estrogens Dispensing Issues • Patients should not smoke during therapy, whether birth control or HRT Warning!

  37. Estrogen’s Side Effects • Nausea • Vomiting • Bloating • Weight gain • Breast tenderness • Breakthrough bleeding • Glucose intolerance

  38. HRT • Reduces symptoms of menopause • Decreases bone loss • Lowers risk of cardiovascular disease • Small risk of breast cancer

  39. Drug List Estrogens • conjugated estrogen (Enjuvia,Premarin) • conjugated estrogen-medroxyprogesterone (Premphase, Prempro) • estradiol (Alora, Climara, Esclim, Estrace, Estraderm, Estrasorb, Estring, Femring, Menostar, Vivelle, Vivelle Dot)

  40. Drug List Estrogens • estradiol-levonorgestrel (Climara Pro) • estradiol-norethindrone (Activella, CombiPatch) • estradiol-norgestimate (Ortho-Prefest)

  41. Drug List Estrogens • estropipate (Ogen) • ethinyl estradiol (Estinyl) • ethinyl estradiol-norethindrone (Femhrt)

  42. estrogen-medroxyprogesterone (Premphase, Prempro) • Provides estrogen and progesterone replacement • Prevents uterine cancer

  43. Progestins • Used primarily in birth control and to prevent uterine cancer • Also used for menstrual dysfunction

  44. Progestin’s Side Effects Similar to pregnancy: • Weight gain • Depression • Fatigue • Acne • Hirsutism

  45. Drug List Progestins • levonorgestrel (Norplant II) • medroxyprogesterone (Depo-Provera, Provera) • norethindrone (Micronor)

  46. Contraceptives • Most OCs are combinations of estrogen and progestin • Interfere with hormones responsible for regulation of the menstrual cycle • Change the consistency of cervical mucus • Alter the endometrial lining

  47. Benefits of OCs • Prevention of pregnancy • Regulates menstrual cycle • Reduces menstrual flow • Lessens severe menstrual cramps and pain • Protects against ovarian and endometrial cancer, benign breast disease, ectopic pregnancy, fibroadenomas, and ovarian cysts

  48. Oral Contraceptives • There are different combinations of estrogen and progestin as well as differing strengths • Tricycling – taking meds for 3 - 21 day cycles without a pill-free interval

  49. Drug List Contraceptive Agents • estradiol cypionate-medroxyprogesterone (Lunelle) • ethinyl estradiol-desogestrel (Cyclessa, Desogen, Kariva, Mircette, Ortho-Cept) • ethinyl estradiol-drospirenone (Yasmin)

  50. Drug List Contraceptive Agents • estradiol cypionate-medroxyprogesterone (Lunelle) • ethinyl estradiol-desogestrel (Cyclessa, Desogen, Kariva, Mircette, Ortho-Cept) • ethinyl estradiol-drospirenone (Yasmin)

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