1
Q
Calcium Carbonate
A
- Most common oral source of calcium
- most concentrated
- Need HCl to be absorbed
- More GI effects than other supplements
- Milk Alkali Syndrome: Excessiv Ca plus absorbable alkali from milk
2
Q
Calcium Citrate
A
- Oral tablets
- More soluble (doesn’t require HCl)
3
Q
Calcium Gluconate
A
- Oral or IV
- -NOT IM route
- Drug of choice for IV therapy in acute hypocalcemic tetany b/c less irritating to veins (infuse slowly arrhythmias)
4
Q
Calcium Gluceptate
A
-IV or IM (only IM)
5
Q
Cholecalciferol
A
-Oral tablets of pure D3
6
Q
Ergocalciferol
A
- Pure D2 (used in milk and other foods)
- can be prescribed and therefore reimbursed
- Tablets, capsules, oral solution, and IM injection
7
Q
Dihydrotachysterol
A
- 1-OH Vitamin D analog so doesn’t require renal hydroxylation (good for renal failure and hyperparathyroidism secondary to renal failure)
- orally effective as tablets capsules and solutions
8
Q
Calcifediol
A
- 25-OH-D3 so no liver hydroxylation required
- Patients with liver disease
- Oral capsules
9
Q
Calcitriol
A
- the final hormone form
- neither kidney or liver activation required
- oral or injection
- Too strong for most patients
10
Q
calcitonin
A
- Peptide hormone
- promote Ca and phosphate secretion
- Decrease Bone turnover; inhibits osteoclasts, Paget’s disease
- Few side effects
11
Q
Salmon Calcitonin
A
- More potent and longer duration than human form
- Peptide drug (SC or IM)
12
Q
Bisphosphonates
A
- Bind to bone matrix and inhibit osteoclasts to decrease bone turnover
- Hypercalcemia, osteoporosis, Paget’s disease
- Poorly absorbed with food
- Excreted in kidney without metabolism (avoid in kidney disease)
13
Q
Newer Bisphosphonates
A
-Esophageal ulcers: take overnight while standing up with copious amounts of water, no food for 30 minutes, and remain standing for 30 minutes
-SIde effects:
Ab pain, nausea and vomiting
Osteonecrosis of Jaw (cancer patients)
Femur fractures w/ long term use (atypical fractures)
14
Q
Alendronate
A
- Osteoporosis and Pagets
- Oral, effervescent prep available
15
Q
Ibandronate
A
- Postmenopausal osteoporosis
- Oral tablets (daily or monthly)
- IV injection every 3 months
16
Q
Zoledronate
A
- IV use for osteoporosis
- Prevention and treatment
- Paget’s (recommended Tx) and hypercalcemia of malignancy
- AVOID IN RENAL DISEASE
17
Q
Teriparatide
A
- PTH hormone analog (short)
- Acts on GPCR to increase cAMP
- Increases resorbtion of Ca and Phosphate (bone)
- Increases reabsorption of Ca and stim vit D activation (Kidney)
- Increases absorption of Ca and phosphate (GI tract)
- Daily SC injection
- stimulates bone formation because of short duration of action and low levels
- Tx of Osteoporosis
- Anabolic as opposed to anti-resorptive effects of calcitonin and bisphos
- Increase risk of bone cancer: Paget’s, incr. alk phos, and open bone epiphysis
18
Q
Denosumab
A
- Monoclonal antibody against Rank-L which is usually suppressed by estrogen
- Rank-L activates osteoclasts
- Injection (2/yr)
- Postmenopausal women with osteoporosis w/ Hx of fracture risk
- Cancer Pts to treat bone break down from metastasis, men w/ prostate cancer (androgen deprivation)
- Suppression of bone remodeling –> ONJ, incr fracture risk, delayed fracture healing
- Hypocalcemia
19
Q
Estradiol
A
- Orally –> rapid first pass metabolism
- Slow release depot forms
- Topical preps (vaginal creams, vaginal rings, transdermal patches, transdermal spray, microionized oral prep.)
- Used mainly for HRT and hypogonadism
20
Q
Conjugated Estrogens
A
- Natural estrogen preparations
- Conjugates and salts of estrone and estriol
- Premarin
- Oral, IV, IM, and vaginal
- Mainly used for HRT
21
Q
Ethinyl Estradiol
A
- Ethinyl group slows degradation
- Increases potency, oral effectiveness, and duration of action
- Oral contraceptives
22
Q
HRT treats:
A
- Vasomotor (hotflashes palpitations) good response
- Urogenital atrophy: (incontinence dyspareunia, and UTI)
- Psychological Disturbances: Mood changes, depression
- Osteoporosis: Bone loss increased fracture, major indication for therapy. Alter cytokine synthesis and inhibit osteoclasts
- Women who have lost gonadal function
23
Q
Cancer in HRT
A
- Estrogens alone increase risk of CA
- Adding progestin greatly reduces this risk
- Estrogens and progesterone increase breast cancer risk
24
Q
Heart Disease in HRT
A
- Estrogens alone decrease myocardial risk
- Progesterones with estrogens reverse risk reduction
25
HRT preps
- Conjugate estrogens commonly used
- Ethinyl estradiol becoming more common
- preps with estradiol itself becoming more popular (medroxyprogesterone)
26
Women's health Initiative
- Reduce hip fracture
- Red. Colorectal cancer
- Incr. in coronary artery disease, strokes, and PE
- Incr risk of breast & lung cancer
- Treat menopausal symptoms (short term) is probably okay
27
Selective Estrogen Response Modifiers
- Steroid analogs with mixed agonist-antagonist properties
- Some tissues full agonist while full antagonist in other tissues
- Agonism vs. antagonism determined by position stabilized by analog
28
2 SERMs currently available
- Tamoxifen and Raloxifene
- Tamoxifen: Bad at Uterus cancer, clotting factors/stroke, and menopausal symptoms
- Raloxifene: Bad at Clotting factors/stroke, and menopausal symptoms
29
Tamoxifen
- Orally effective
- Used as anti-estrogen in breast cancer but agonist in other tissues
- Breast cancer preventative therapy (good)
- May decrease osteoporosis and improve blood lipid panels
- Uterine cancer incr risk, incr. risk of thrombosis, cause hot flashes
30
Raloxifene
- Orally effective
- agonist on bone (OSTEOPOROSIS only use)
- Antagonist for breast cancer prevention (no increase risk)
- Improves lipid profile
- Causes hot flashes and increases stroke/clot risk
31
Oral Contraceptive pills
- All contain ethanol estradiol and and 19-nor progestin
- Traditionally active pill for 21 day and 7 day non-active
- Inhibit ovulation by disrupting cyclical release of gonadotropins (Feedback suppressive therapy)
- Decrease likelihood of fertilization if ovulation happens due to changes in cervical mucous, endometrium, and fallopian tube secretions
- Endometrial changes that decrease likelihood of successful implantation
- Onset of menstruation at end of pill cycle
32
Norethindrone and Levonorgestrel
-Androgenic and anabolic
33
Norethynodrel
-Estrogenic, not androgenic
34
Norgestimate
-not androgenic or estrogenic (pure progesterone)
35
Drospirenone
-anti-androgenic and anti-mineralocorticoid activity
36
-Etonogestrel
-Used in several unique preparations
37
Drugs that decrease efficacy of OCPs
- Antibiotics (enterohepatic recirc and induce liver enzymes)
- Anti-epileptic drugs induce liver enzymes
38
Mini Pill
- Only oral progesterone
- Norethindrone and Norgestrel
- Not as effective
- Taken Daily, not cyclically
- Lack of regular menstruation and occurrence of irregular bleeding (6-8 wks w/o blood = pregnancy test)
- Ovulation still occurs but fertilization and implantation are prevented
39
Medroxyprogesterone
- Depo-Provera
- IM injection every 3 months
- Possible toxicity (don't use on woman who may want kids later)
40
Etonogestrel
- Single rod implant effective for 3 yrs
- Irregular bleeding
- 4% complications with 2% causing removal
41
Emergency post-coital contraceptives
- Estrogen, progestin or estrogen plus progestin taken after intercourse to prevent pregnancy
- Inhibit ovulation if it hasn't occurred
- inhibit fertilization and/or implantation
- Lead to menstruation when pills are stopped
- Reasonably effective
42
Plan B
Levonorgestrel only
- 2 pills within 72 hrs
- One step = 1 pill available OTC to girls 15 yrs older
43
Next Choice
Levonorgestrel only
| -2 pills 12 hrs apart within 72 hrs
44
Ella
- Ulipristal
- Agonist/antagonist progesterone receptors
- Structurally related to mifepristone
- Up to 5 days after intercourse
- Prescription
- Inhibit gonadatropin release and prevent maintenance
45
Mifepristone
- Progesterone receptor antagonist whihc disrupts maintenance of the endometrium
- Increases PG synthesis -> stimulation of uterine contractility for expulsion of fetus
46
Methotrexate plus misoprostol
- Another abortion approach
- Methotrexate is folic acid antagonist = cytotoxic to trophoblast
- Mistoprostol -> uterine contraction
47
Bromocriptine
- Dopamine agonist
- Inhibits prolactin secretion
- Use if prolactinemia is cause
48
Danazol
- Weak androgen used in endometriosis is problem
| - Androgen -> inhibition of gonadotropin secretion -> decrease estrogen synthesis
49
Clomiphene
- Non-steriodal estrogen partial agonist
- Anti estrogen blocks estrogen feedback inhibition of gonadotropin release, functional pituitary is required for the function of this drug
Pharm
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