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: Involved in cholesterol, fat, and protein metabolism Mineralocorticoids: Involved in regulating electrolyte and water balance Cortisol Principal adrenal steroid hormone Responsible for: Gluconeogenesis Protein catabolism Anti-inflammatory reactions Stimulation of fat deposition Sodium and water retention Corticosteroids Adrenal hormones excluding sex hormones Steroid production follows a circadian rhythm Properties of glucocorticosteroides used in clinics Anti-inflammatory Immune-depressive Anti-allergic Anti-shock Anti-toxic Anti-inflammatory action of GCS Nonspecific inflammation Auto-immune component Hyperergic character Therapy of despair Mechanism of anti-inflammatory action of GCS GCS activation of lipomoduline decreasing of activity of phospholipase А2 slowing down of arachidonic acid metabolites production (prostaglandins, leucotriens, thromboxan А2) stabilization of cellular and lyzosomal membranes depression of histamine, serotonin, bradykinine releasing decreasing of leucocytes’ migration processes, depression of phagocytes activity decreasing of capillaries’ wall permeability 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 Doses and terms of GCS therapy Situation Acute cases (shock, collapse, brain, lungs edema, septic shock, asthmatic condition etc.) Daily dose 200-500800-1000 mg i.v. Terms of treatment 1-3 days Subacute and acute attacks of 20-50 mg 4-6 weekschronic processes (rarely till 200 several (rheumatoid diseases, mg) months ulcerative colitis, bronchial asthma etc.) Primary and secondary 2,5-10 mg insufficiency of adrenal cortex life-long Corticosteroids Act as anti-inflammatory and immunosuppressive agents in treating diseases of different origins: Hematologic Allergic Inflammatory Neoplastic Autoimmune Addison’s Disease Life-threatening deficiency of glucocorticoids and mineralocorticoids Treated with daily corticosteroids Symptoms of Addison’s Disease Debilitating weakness Hyperkalemia Hyperpigmentation of skin Low levels of serum sodium and glucose Reduced blood pressure Weight loss 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 Reasons for Using Corticosteroids Inhibit inflammation Useful in treating asthma, rashes, and skin disorders Available in many different dosage forms Problems with Corticosteroids Lessen the ability of leukocytes to destroy infection which decreases fever, redness, and swelling Also may cause infection to spread Corticosteroid Dispensing Issues Warning! Take caution in patients with diabetes, uncontrolled hypertension, CHF, severe infection or altered immunity, or peptic ulcer disease with active GI bleeding 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 Adverse Effects of Glucocorticoids Cardiovascular effects Dermatologic effects Gastrointestinal effects Immune system effects Metabolic effects Musculoskeletal effects Neuropsychiatric effects Ophthalmic effects 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 Responsibilities of Testosterone Initiating sperm production Behavioral characteristics Libido Sexual potency Muscle mass and strength Fat distribution Bone mass Erythropoiesis Prevention of baldness 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 Androgen’s Side Effects Virilization Hirsutism Acne Hepatoxicity High levels of erythrocytes Oily skin Gynecomastia Priapism Male Impotence Failure to initiate or maintain an erection until ejaculation Causes: Testosterone deficiency Alcoholism Cigarette smoking Psychological factors Medications Drugs That May Cause Impotence Alcohol (most significant) Amphetamines Antihypertensives Corticosteroids Estrogens H2 blockers haloperidol lithium Opiates Some antidepressants Drug List Agents for Male Impotence alprostadil (Caverject, Edex, Muse) danazol (Danocrine) methyltestosterone (Android, Testred) oxymetholone (Anadrol) papaverine testosterone (Androderm, AndroGel, Striant, Testoderm) Drug List Agents for Male Impotence – Phosphodiesterase Inhibitors sildenafil (Viagra) tadalafil (Cialis) vardenafil (Levitra) sildenafil (Viagra) 1st oral therapy for impotence Allows an erection to occur naturally Take at least 1 hour before activity sildenafil Dispensing Issues Warning! Potentially lethal interaction with nitrates tadalafil (Cialis) Duration of action is 36 hours Faster onset and longer duration than others in this class tadalafil Dispensing Issues Warning! Potentially lethal interaction with nitrates Female Hormones Can prevent conception, ease symptoms of menopause, and help prevent osteoporosis 2 main female hormones: Estrogen Progesterone 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 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 Menopause As women reach menopause estrogen production decreases HRT can be used to supplement estrogen levels estrogens Dispensing Issues Warning! Patients should not smoke during therapy, whether birth control or HRT Estrogen’s Side Effects Nausea Vomiting Bloating Weight gain Breast tenderness Breakthrough bleeding Glucose intolerance HRT Reduces symptoms of menopause Decreases bone loss Lowers risk of cardiovascular disease Small risk of breast cancer 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) Drug List Estrogens estradiol-levonorgestrel (Climara Pro) estradiol-norethindrone (Activella, CombiPatch) estradiol-norgestimate (Ortho-Prefest) Drug List Estrogens estropipate (Ogen) ethinyl estradiol (Estinyl) ethinyl estradiol-norethindrone (Femhrt) estrogen-medroxyprogesterone (Premphase, Prempro) Provides estrogen and progesterone replacement Prevents uterine cancer Progestins Used primarily in birth control and to prevent uterine cancer Also used for menstrual dysfunction Progestin’s Side Effects Similar to pregnancy: Weight gain Depression Fatigue Acne Hirsutism Drug List Progestins levonorgestrel (Norplant II) medroxyprogesterone (Depo-Provera, Provera) norethindrone (Micronor) 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 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 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 Drug List Contraceptive Agents estradiol cypionate-medroxyprogesterone (Lunelle) ethinyl estradiol-desogestrel (Cyclessa, Desogen, Kariva, Mircette, Ortho-Cept) ethinyl estradiol-drospirenone (Yasmin) Drug List Contraceptive Agents estradiol cypionate-medroxyprogesterone (Lunelle) ethinyl estradiol-desogestrel (Cyclessa, Desogen, Kariva, Mircette, Ortho-Cept) ethinyl estradiol-drospirenone (Yasmin) Drug List Contraceptive Agents ethinyl estradiol-ethynodiol diacetate (Demulen) ethinyl estradiol-etonogestrel (NuvaRing) ethinyl estradiol-levonorgestrel (Levlen, Nordette, Seasonale, Tri-Levlen, Triphasil, Trivora-28) Drug List Contraceptive Agents ethinyl estradiol-norelgestromin (Ortho Evra) ethinyl estradiol-norethindrone (Estrostep Fe, Femhrt, Loestrin Fe, Ovcon) ethinyl estradiol-norgestimate (Ortho TriCyclen, Ortho Tri-Cylcen Lo) Drug List Contraceptive Agents ethinyl estradiol-norgestrel (Lo/Ovral, Low- Ogestrel, Ovral) ethinyl estradiol-desogestrel (Cyclessa, Desogen, Kariva, Mircette, OrthoCept) Inhibits ovulation Includes 2 days of placebo followed by 5 days of low-dose estrogen May be safer for smokers ethinyl estradiol-levonorgestrel (Seasonale) Taken for 3 months at a time Patient only has 4 menses per year Prevents egg release from the ovaries, increases mucus thickness, and thickness of the endometrial lining ethinyl estradiol-dropirenone (Yasmin) Drospirenone is related to spironolactone (a diuretic) Causes less bloating and less weight gain May cause weight loss due to excess water loss ethinyl estradiol-norelgestromin (Ortho-Evra) Transdermal contraceptive Suppresses gonadotropins A new patch is applied every 7 days for weeks then the 4th week is patch free 3 Some Oral Contraceptive Interactions Antibiotics Anticonvulsants Antifungals Benzodiazepines Bronchodilators Corticosteroids Lipid-lowering agents TCAs Emergency Contraception In great demand Patients want them to be available OTC Discussion What is one of the arguments for emergency contraceptives being OTC? Discussion What is one of the arguments for emergency contraceptives being OTC? Answer: After making a doctor’s appointment and then going to the get the prescription, sometimes it is too late to take the medication Drug List Contraceptive Agents Emergency Contraceptives levonorgestrel (Plan B) norgestrel (Ovrette) Home Pregnancy Tests Critical organ systems develop in the first month which is affected by Mother’s diet Environment (smoking) Medications Consumption of alcoholic beverages Home Pregnancy Tests Based on detecting human chorionic gonadotropin (HCG) Levels can be measured as early as 6-8 days after conception Results are given within 1-5 minutes Tests are better than 95% accurate Drugs Used at Birth Often no drugs are necessary for delivery, but in some cases they are To restart labor To decrease uncontrolled bleeding Drug List Drugs Used at Birth methylergonovine (Methergine) oxytocin (Pitocin) oxytocin (Pitocin) Natural hormone that stimulates uterine contractions Drug should be used as a last resort oxytocin’s Side Effects For the woman: For the child: Vomiting Bradycardia Irregular heart rate Arrhythmias Tachycardia Jaundice Postpartum bleeding Sexually Transmitted Disease the structural anatomy of the male and female genital systems Gonorrhea Most commonly reported STD Caused by Neisseria gonorrhoeae that attaches to mucosal cells in: Oropharyngeal area Eye Joints Rectum Male and female genitalia Gonorrhea If untreated, it can cause systemic infection including The heart, meninges, eyes, pharynx, and joints Eye infections occur most often in newborns and can cause blindness Syphilis Caused by Treponema pallidum Incubation averages three weeks Infection develops in 3 stages: Primary stage Secondary stage Tertiary stage Primary-Stage Infection Small, hard-based sore develops at site of infection May be painless and patient may be unaware Fluid in the sores is highly infectious Bacteria enters the bloodstream and lymphatic system Secondary-Stage Infection Produces skin rashes, patchy hair loss, malaise, and mild fever Symptoms subside after a few weeks and disease becomes latent After 2-4 years of latency, the disease is usually no longer infectious Tertiary-Stage Infection Occurs after an interval of at least 10 years Lesions appear as a rubbery mass in many organs and sometimes the skin May cause extensive damage Congenital Syphilis Crosses the placenta into the fetus Results in neurologic damage if pregnancy occurs during the tertiary stage Pregnancy during primary or secondary stage is likely to produce a stillborn child Genital Herpes Caused by herpes simplex virus Lesions appear after 1 week of incubation Infectious vesicles appear and heal within 2 weeks Virus becomes latent until reactivated Candidiasis Caused by Candida albicans Yeast-like fungal infection that can cause infection in genital area of men and women and the mouth (thrush) Can cause itching and a thick, yellow, cheesy discharge Vaginitis Caused by Gardnerella vaginitis Results from interaction between this organism and anaerobic bacterium in the vagina Symptoms: frothy discharge with fishy odor and vaginal pH of 5 to 6 Vaginitis May also be caused by Trichomonas vaginalis Normally found in both sexes, but causes infection if vaginal pH changes Causes profuse yellowish or cream-colored discharge with a disagreeable odor, irritation, and itching Drug List Agents for STDs acyclovir (Zovirax) azithromycin (Zithromax) ceftriaxone (Rocephin) clotrimazole (GyneLotrimin, Mycelex) doxycycline (Doryx, Vibramycin) Drug List Agents for STDs erythromycin fluconazole (Diflucan) ketoconazole (Nizoral) metronidazole (Flagyl) miconazole (Monistat) Drug List Agents for STDs penicillin G benzathine (Bicillin L-A) spectinomycin (Trobicin) tetracycline (Sumycin) tioconazole (Vagistat-1) valacyclovir (Valtrex)