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endocrine pharmacology (estrogen therapies (menopause (therapies…
endocrine pharmacology
osteoporosis
non-pharm treatmetns
regular weight bearing exercises
fall prevention
smoking cessation
avoidance of excessive alcohol use
calcium supplements
best in combination with other treatments
plateau in absorption max 500 MG per dose
calcium carbonate, take with meals for max absorption
calcium citrate, best for elderly or those on acid suppression therapy
ADR: bloating, gas, constipation, large pills
vitamin D
MOA: facilitates the absorption of calcium
Vitamin D2 (ergocalciferol)
calcitriol (active vitamin D)
oral formulation Rocaltrol
injection calcijex
vitamin D3 (OTC)
bisphosphonates
first line therapy
inhibits osteoclast activity
attracted to areas where osteoclast are breaking down bone, as osteoclasts work, they absorb the bisphosphonate, once inside the cell they block the activity of substances that attract and stimulate the osteoclast activity, as a result the osteolcasts are unable to function properly and eventually go through apoptosis
adverse reactions
GI: acid regurgitation, ulceration, operforation, bleeding
muscle pain, infection reactions, osteonecrosis of the jaw
examples
alendronate (oral)
risedronate ( (IV and oral))
ibandronate (oral)
zoledronic acid (IV)
kinetics
very poor absorption
proper administration is essential for absorption and safety
take first thing in the morning, take on an empty stomach, take with 8 oz of water,remain upright for at least 30 minutes, no medication/food/drink for 30 mins
estrogen replacement
not to be used primarily for osteoporosis
MOA: decrease bone reabsorption and osteoclast recruitment and activity, inhibits PTH peripherally
ADR: cancer, cardiovascular disease, venous thromboembolism, gallbladder disease
drugs
raloxifene (evista)
those that cant tolerate bisphosphonates, those at risk for breast cancer
60 mg
moa: selective estrogen receptor modifier (SERM) has estrogen agonist and antagonist activity, agonist: bone and lipid profile antagonist: breast tissue and endometrium
ADR:does not relieve hot flashes, small incidence of DVTs, leg cramps and muscle spasm are common, endometrial bleeding
teriparatide (forteo)
recombinant PTH injected SQ
for those at high risk for fracture, multiple fractures, contraindications to bisphosphonates or raloxifene
MOA: anabolic agent, stimulates new bone formation and activates remodeling to increase BMD pulse therapy produces bone absorption rather that bone resorption usually caused by PTH, given once daily and HL is 1 hour
ADR: nausea, joint aches, transient hypercalcemia
thyroid disorders
hypothyroidism
deficiency in thyroid hormone
hashimoto thyroiditis
strong genetic predisposition results from increased production of thyroid antibodies, thyroid cells are destroyed by circulating antibodies
clinical features
fatigue, weight gain, dry coarse yellowing skin, cold intolerance, delayed reflexes, constipation,memory impairment, depression,heavy menses
treatment
replacemnt of T4 is required ar a dose of aprox. 1.7 mcg/kg/day
guided by resolution of symptoms and lab monitoring
examples
synthetic
levothroxine (synthroid)
animal origin
desiccated thyroid (armour thyroid)
hyperthyroidism
excessive production of thyroid hormones
graves disease
autoimmune disorder related to production of thyroid receptor antibody which has TSH like ability peak incidence in 3rd or 4th decade
clinical features
nervousness and irritability, palpitations and tachycardia, heat tolerance, tremor, weight loss, hair loss, frequent bowel movements, insomnia, decreased menstrual flow, emotional lability, changes in vision, exophthalmos
treatments
surgery
radioactive iodine
antithyroid drugs
thioamides
MOA: block production of thyroid hormone, quick onset may be used in pregnancy/lactation
thioamide toxicity
generally well tolerated, gi upset, bitter taste, hepatitis agranulocytosis, rash, arthralgia
iodide
non-selective beta blockers
estrogen therapies
estradiol
estrone
estriol
may be used as a form of contraception to inhibit ovulation or impede sperm transport via cervical mucosal thickening, may also have an effect on endometrial lining
menopause
average onset is 51yr
hot flashes, night sweats, mood swings, bone loss and vaginal dryness
therapies
conventional
equine estrogen, synthetic estrogen, estrogen/progestin/medroxyprogesterone, SERM
alternative
bioidentical hormones, phytoestrogens, black cohosh, evening primrose, wild yam
testosterone therapies
low testosterone
erectile dysfunction, low semen volume, hair loss, fatigue, decreased muscle mass, decreased bone mass, increased body fat
testosterone replacement
oral: testosterone undecanoate (jatenzo)
transdermal: androderm or androgel
injectable: Aveed, Depo-testosterone
implant: testopel
contraception
hormonal
estrogen plus progesterone: pill, patch or ring
prevent pregnancy, decrease acne. regulate cycle and may decrease prolonged or painful periods
MOA: mimics endogenous estrogen, has an effect on the feedback loop involving FSH
follicles do not mature, ovulation is prevented, change of cervical mucus, change in uterine endometrium
advantages
decreases heavy menstrual bleeding, decrease painful menstruation, protection from endometrial cancer, protection from ovarian cancer and suppression of the development of ovarian cysts, decreased incidence of ectopic pregnancy, acne improvements
disadvantaes
increased risk of VTE, stroke, MI, increased triglycerides,increase in blood pressure and risk of clots, increased risk of breast cancer, increased risk of cervical cancer, no STD protection
progesterone only: pills, devo-provera injection, some implants
birth control pills
monphasic
alesse, aviane, yasmin,ovcon,demulen
triphasic
ortho-tri-cyclen, triphasil
common complaints
progestin excess, progestin deficiency, estrogen excess, estrogen deficiency
emergency
levonorgestrel
MOA same as standard contraceptives, will not work if implantation has occurred, best if used within 72 hours of unprotected sex
mifepristone and ulipristal
strong inhibitor of progesterone receptor, abortifacient
ADR: vmitting, diarrhea, abdominal pain, pelvic pain, or vaginal bleedding