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How does colesevelam work in treatment of DM? Bromocriptine? - ANS ✓Colesevelam—bile acid sequestrant used to lower cholesterol and helps lower blood glucose Many with diabetes also have high cholesterol so 2 birds-1 stone o Bromocriptine—adjunct to diet and exercise (0.5% reduction) Injectables: o Amylin memetics? - ANS ✓Pramlintide Side effects—hypoglycemia when used with insulin Drug/Drug—insulin o GLP-1 receptor agonists (or incretin mimetics) Can cause medullary thyroid cancer What is treatment of diabetic ketoacidosis (DKA)? Hypoglycemia? - ANS ✓o Insulin replacement, reverse acidosis with bicarbonate, replace water, sodium, potassium, normalize glucose levels o Hypoglycemia—IV glucose, glucagon is glucose
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How does colesevelam work in treatment of DM? Bromocriptine? - ANS ✓Colesevelam—bile acid sequestrant used to lower cholesterol and helps lower blood glucose Many with diabetes also have high cholesterol so 2 birds-1 stone o Bromocriptine—adjunct to diet and exercise (0.5% reduction) Injectables: o Amylin memetics? - ANS ✓Pramlintide Side effects—hypoglycemia when used with insulin Drug/Drug—insulin o GLP-1 receptor agonists (or incretin mimetics) Can cause medullary thyroid cancer What is treatment of diabetic ketoacidosis (DKA)? Hypoglycemia? - ANS ✓o Insulin replacement, reverse acidosis with bicarbonate, replace water, sodium, potassium, normalize glucose levels o Hypoglycemia—IV glucose, glucagon is glucose not available What is hyperosmolar hyperglycemia state (HHS)?
o When does this occur?
o Treatment? - ANS ✓o Large amount of glucose excreted in the urine and results in dehydration and loss of blood volume o Increases blood concentration of electrolytes and nonelectrolytes, particularly glucose and hematocrit
Most frequently with type 2 diabetics with acute infection or illness or other stressors
Correcting hyperglycemia and dehydration with IV insulin, fluids, and electrolytes What effect does iodine have on thyroid? - ANS ✓o When iodine availability is low production of thyroid hormones decrease Why is normal thyroid function important in first trimester of pregnancy? How much does requirement unusually increase in pregnant women taking thyroid supplements? - ANS ✓o Fetus is unable to produce its own hormones, without can result in permanent neuropsychologic deficits o Usually increases as much as 50% When is fetal thyroid gland full functional? - ANS ✓o 16 weeks If not treated, what does hypothyroidism cause in an infant? - ANS ✓o Large protruding tongue, potbelly, and dwarfish stature o The development of the nervous system, bones, and teeth is impaired
Catecholamines—increase cardiac responses Increase requirements of insulin and digoxin How is this dosed? How does dosage differ for someone over 50? 65 and older? Someone with heart disease? Overweight? Underweight? - ANS ✓1.6-1. mcg/kg/day Obese—go by ideal body weight Underweight—actual weight Older patients with CAD—start with 12.5-25 mcg Elderly—start low and go slow Younger than 3 months—10 to 15 mcg/kg/day Children (3-5 months)—8 to 10 mcg/kg/day Children (6-11 months)—6 to 8 mcg/kg/day Children 1-5 years—5 to 6 mcg/kg/day Children 6- 12 —4 to 5 mcg/kg/day Liotrix—a mixture of synthetic T4 plus synthetic T3 in a 4:1 fixed ratio - ANS ✓o Because levothyroxine alone produces the same ratio of T4 to T3, Liotrix offers no advantage over levothyroxine for most indications Armour—consists of desiccated animal thyroid glands. - ANS ✓o Standardization is based on content of iodine, levothyroxine, and liothyronine. o The ratio of levothyroxine to lipthyronine is not less than 5: o Thyroid is available in tablets (15-300 mg) Methimazole—used in hyperthyroidism - ANS ✓o Cell form of therapy for Graves' disease o Adjunct to radiation therapy until the effects of radiation become manifested
o Suppresses the thyroid hormone synthesis in preparation for thyroid gland surgery o Thyrotoxic crisis Propylthiouracil - ANS ✓o Inhibits thyroid hormone synthesis o Second line for graves o Short half-life o Full benefits—6 to 12 months o Uses—graves', adjunct therapy to radiation, preparation for thyroid gland surgery, thyrotoxic crisis o Adverse effects—agranulocytosis, severe liver damage o Pregnancy? Crosses the placenta less and concentrations in breastmilk are lower than methimazole Radioactive Iodine 131 (lugol solution) - ANS ✓o Effect on the thyroid is destruction of thyroid tissue by emission of beta particles o Advantages—low cost; spared the risk, discomfort, and experience of thyroid surgery; death is extremely rare; no tissue other than thyroid is injured o Disadvantages—treatment is delated, taking several months to become maximal; treatment is associated with significant incidents of delayed hypothyroidism from destruction of thyroid tissue (need levothyroxine) o Diagnostic uses? Hyperthyroidism, hypothyroidism, and goiter o Pregnancy—contraindicated o What are indications for Lugol solution?
o Affect glucose homeostasis Increase insulin sensitivity and promote glucose uptake Adverse effects of estrogen? - ANS ✓o Endometrial hyperplasia and carcinoma o Increase cardiovascular events, N/V, gallbladder disease, jaundice, headache and chloasma Therapeutic uses of Estrogen? - ANS ✓o Menopausal hormone o Female hypogonadism o Acne SERMS—Selective estrogen receptor modulators - ANS ✓o drugs that activate estrogen receptors in some tissues and block them in others Why were these developed? - ANS ✓Provide the benefits of estrogen protection against vaginal atrophy Reduction of LDL cholesterol, but avoiding the drawbacks What is Duavee? - ANS ✓Conjugated estrogens with bazedoxifene Combine estrogen with an estrogen agonist or antagonist Used for treatment of vasomotor symptoms and osteoporosis in postmenopausal women Bazedoxifene—reduces the risk of excessive growth of the uterine lining that is posed by the estrogen component What are noncontraceptive uses for progesterone? - ANS ✓o Postmenopausal hormone therapy o Dysfunctional uterine bleeding o Amenorrhea
o Infertility o Prematurity prevention o Endometrial carcinoma and hyperplasia When is estrogen therapy (ET) alone indicated? Estrogen/Progesterone (EPT)? - ANS ✓o Estrogen alone—women who have had a hysterectomy o EPT—all other women What are benefits? Risks? - ANS ✓o Benefits Relief of vasomotor symptoms Management of urogenital atrophy Prevention of osteoporosis and related fractures Cardioprotection Prevention of colorectal cancer Positive effect on wound healing Tooth retention Glycemic control Physiologic doses of estrogen (with or without progestin) Taken to manage symptoms caused by loss of estrogen in menopause Hot flashes, sleep disturbances, urogenital atrophy, bone loss, altered lipid metabolism Use of hormone replacement therapy (HRT) has declined sharply o Risks Cardiovascular events: Myocardial infarction, stroke, pulmonary embolism, and deep vein thrombosis Endometrial cancer Breast cancer Ovarian cancer Gallbladder disease
o MOA—inhibit ovulation o What are categories? Subgroups? - ANS ✓Classification (two main categories) Combination oral contraceptives (OCs) Estrogen and progestin Progestin-only OCs ("mini-pills") Three major subgroups of combination OCs Monophasic Biphasic Triphasic What are 3 estrogens in OCPs? Progesterone? 1st gen? 2nd gen? 3rd gen? 4th gen? - ANS ✓Estrogens—ethinyl, estradiol, estriol and estradiol valerate Progesterone—4 generations 1 st generation—ethynodiol diacetate and norethindrone 2 nd gen—levonorgestrel and norgestrel 3 rd gen—desogestrel and norgestimate 4 th gen—dienogest and drospirenone Combination Ocs o Adverse effects? o Noncontraceptive uses? o What drugs reduce the effects? o What drugs effects are decreased by OCs? o What are drugs whose effects are increased by Ocs?
o What are unique properties of Beyaz and Safyral? Natazia? - ANS ✓Thyrombolytic disorders Increase risk—heavy smoking, a history of thrombo embolism, thrombophilias Hypertension Cancer Stroke in patients with migraine Teratogenic effects Abnormal uterine bleeding Use in pregnancy and lactation Benign hepatic adenoma Glucose intolerance
Decrease risks of ovarian cancer, endometrial cancer, ovarian cysts, pelvic inflammatory disease, benign breast disease, iron deficiency anemia, and acne Favorable effect on menstrual cycles Diminished cramps; lighter, shorter, more predictable flow
Rifampin Ritonavir Antiepileptic drugs St. John's wort
Warfarin Insulin Oral hypoglycemics
Several agents, including theophylline, tricyclic antidepressants, diazepam, and chlordiazepoxide
Long-acting contraceptives - ANS ✓o Implants—irregular bleeding, can stop period all together o Depot medroxyprogesterone acetate Side effects? Menstrual irregularities Bone loss How often are injections given? Every 3 months o IUDs What are the different types and how long can they remain in place? Copper T 380A [ParaGard] - 10 years Levonorgestrel-releasing intrauterine system [Mirena] - 5 years o Spermicides—Chemical surfactants that kill sperm by destroying their cell membrane What are drugs used for medical abortion? - ANS ✓o Mifepristone (RU 486) with misoprostol What is Plan B? - ANS ✓o Single high dose tablet, 1.5 mg of levonorgestrel o Must be taken within 72 hours of unprotected intercourse What are the indications of prostaglandins? - ANS ✓o Induction of abortion for cervical ripening before induction of labor o Control of postpartum hemorrhage What are the therapeutic uses of testosterone? - ANS ✓o Male hypogonadism o Replacement therapy o Delayed puberty o Replacement therapy in menopausal women
o Wasting in patients with acquired immunodeficiency syndrome (AIDS) o Anemias What are adverse effects of Testosterone? - ANS ✓o Virilization in women, girls, and boys o Premature epiphyseal closure o Hepatotoxicity o Effects on cholesterol levels o Use in pregnancy o Prostate cancer o Edema o Abuse potential (athletic performance) What are the preparations? Instructions on use? - ANS ✓o Preparations Oral androgens: Fluoxymesterone and methyltestosterone Intramuscular testosterone esters Transdermal testosterone patches Transdermal testosterone gels Transdermal testosterone under arms Implantable subcutaneous testosterone pellets Testosterone buccal tablets o Topical Applications Pick the location for application Avoid skin-to-skin contact transfer Wash hands with soap and water after every application Cover application site with clothing once gel is dry Women and children: Avoid contact Swimming and showering—5 to 6 hours after application
o Alpha1-adrenergic antagonists (dynamic obstruction) - ANS ✓Terazosin [Hytrin] Doxazosin [Cardura] Tamsulosin [Flomax] Alfuzosin [Uroxatral] Silodosin [Rapaflo] MOA Blockade of alpha1 receptors relaxes smooth muscle in the bladder neck (trigone and sphincter) Side effects - ANS ✓Tamsulosin [Flomax] and alfuzosin [Uroxatral] o Less likely to cause the effects of terazosin and doxazosin o Tamsulosin can cause abnormal ejaculation Terazosin [Hytrin] and doxazosin [Cardura] o Hypotension, fainting, dizziness, somnolence, and nasal congestion These drugs do not decrease PSA levels Drug Interactions? - ANS ✓Exercise caution with other medications that lower blood pressure o Organic nitrates, antihypertensive drugs, PDE-5 inhibitors used for ED o Inhibitors of CYP3A Cataract surgery: "Floppy-iris syndrome" Overactive bladder - ANS ✓o Tolteridine o Oxybutynin o Solifenacin o Tolterodine
o Trospium o Botulinum toxin What does activation of H1 receptors cause? - ANS ✓o Dilation of small blood vessels What are the actions of H2 receptors? - ANS ✓o Regulate the secretion of gastric acid H1 antagonists - ANS ✓o First generation (sedating)—Benadryl MOA Block the actions of histamine at H1 receptors Do not block H2 receptors Some bind to muscarinic receptors Therapeutic uses? - ANS ✓Mild allergy Severe allergy—used in adjunct with other treatments Motion sickness (promethazine and dimenhydrinate) Insomnia (Diphenhydramine) Adverse effects - ANS ✓Sedation GI effects Dizziness Fatigue Coordination problems Confusion Anticholinergic effects—dry mouth, constipation, etc. Severe respiratory depression Severe local tissue injury
Use with caution in patients with significant hepatic and renal impairment Desloratadine [Clarinex] Uses: Seasonal allergic rhinitis, perennial allergic rhinitis, and chronic idiopathic urticaria Allergic Rhinitis - ANS ✓o Inflammatory disorder of the upper airway, lower airway, and eyes o Seasonal and perennial o Triggered by airborne allergens o Allergens bind to immunoglobulin E (IgE) on mast cells o Triggers release of inflammatory mediators Histamine, leukotrienes, prostaglandins o Drug Classes used to treat Intranasal glucocorticoids First choice Side effects o Drying of nasal mucosa or sore throat o Epistaxis (nosebleed) o Headache o Rarely, systemic effects (adrenal suppression and slowing of linear pediatric growth) Intranasal and oral antihistamines—Azelastine and Olopatadine Best used prophylactically For children over 12 and adults 1 - 2 weeks to take affects Side effects o Systemic absorption can be sufficient to cause somnolence o Nosebleeds
o Anticholinergic effects o Unpleasant taste Intranasal and oral sympathomimetics Reduce nasal congestion (do not reduce rhinorrhea, sneezing or itching) Activate alpha1-adrenergic receptors on nasal blood vessels Adverse effects o Rebound congestion o CNS stimulation o Cardiovascular effects and stroke o Abuse Factors in topical administration o Should not be used longer than 5 consecutive days o Drops or sprays Comparison: Oral versus Nasal o Topical agents act more quickly than oral agents and are usually more effective o Oral agents act longer than topical preparations o Systemic effects occur primarily with oral agents; topical agents usually elicit these responses only when dosage is higher than recommended o Rebound congestion is common with prolonged use of topical agents but rare with oral agents o Montelukast - ANS ✓Benefits derive from blocking binding of leukotrienes to their receptors o Omalizumab - ANS ✓Is a monoclonal antibody directed against IgE, an immunoglobulin (antibody) that plays a central role in the allergic release of inflammatory mediators from