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Pharmacology 2 > Exam II- DM, Hormones, Thyroid > Flashcards

Exam II- DM, Hormones, Thyroid Flashcards

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1
Q

Raloxifene/ Evista

A

Class: SERM
MOA: modulates estrogen receptors, inc BD, dec cholesterol without increased risk of E2 cancers
Significantly reduces BCa incidence
PO once daily dosing
SE: hot flashes, arthralgias, myalgias, edema, pruritis, increased risk of DVT
***CI: pregnancy, lactation, Hx of DVT, PE, stroke, retinal vein thrombosis

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2
Q

Calcitonin/ Miacalcin

A

Produced by parafollicular C cells in thyroid
decreases osteoclasts can activity
Decreases risk spinal fx, possibly hip fx too
Class: synthetic hormone
MOA: increases serum Ca
Indic: osteoporosis Tx
SE: nose bleeds, sinusitis, HA, dizziness, edema, anorexia, diarrhea, rashes
IV and nasal spray routes available

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3
Q

Teriparatide/ Forteo

A 
Class: synthetic PTH analog
Indic: females with osteoporosis
MOA: activates bone turnover with osteoblasts activation
Char: SQ, once daily, up to 24 months
SE: nausea, leg cramps, dizziness

Benefits continue after discontinuation
chronic high PTH–> inc risk fx; but daily low dose PTH –> dec risk fx

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4
Q

Denosumab/ Prolia

A

Monoclonal antibodies, anti-TNF agent
Indic: osteoporosis tx, bone metastasis, RA, MMyeloma, giant cell bone carcinoma
MOA: targets RANK Ligand (usu primary signal for bone remodeling)
Char: SQ q6months
SE: increased susceptibility of infx

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5
Q

Sitagliptin/ Januvia

A

Class: dipeptidyl peptidase-4 inhibitor (DDP-4)
MOA: prevents DDP-4 breakdown of GLP-1/GIP–> increased insulin, decreased glucagon postparandially
Tends to normalize insulin without risk of hypoglycemia
Approved as monotx or with Met/Sulfonly/TZDs but not with insulin
25/50/100 mg tabs available
100mg once daily
$200-400/ month

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6
Q

T2DM medications and their MOAs

A

Biguinides (metformin): inhibits liver glucose production
Sulfonylureas: increase insulin secretion
Meglitinides: increased insulin secretion
Alpha- glucoidase inhibitors: delays intestinal glucose absorption
TZDs: decreased insulin resistance
DPP-4 inhibitors: increased postparandial insulin release

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7
Q

Metformin/ glucophage / fortamet

A

Class: biguanide
MOA: decreases hepatic glucose production, increases skeletal musc insulin sensitivity
when used alone, generally won’t cause hypoglycemia
Similar effects on hba1c as sulfonlureas with modest weight loss
SE: wt loss, abd cramping, nausea (decreased in ExR form), metallic taste, increased risk of B12 deficiency (supplementation recommended), LACTIC ACIDOSIS
CI in pts with renal impairment (creative >1.4/1.5)
500/800/1000mg BID or QD if ExR; $55-100/ month

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8
Q

Alendronate/ Fosamax

A

Class: bisphosphates
MOA: inhibits osteoclasts
Indic: primary drug to treat osteoporosis (postmenopausal and post corticosteroid tx)
SE: upset stomach, esophageal irritation/erosion, esophagitis, atypical femur fractures, osteonecrosis of jaw, myalgia,
low bioavailability
**Take away from meals! Prevent esophageal Sxs by standing upright for 30-60mins after taking PO. D/c after 5yrs increases risk vertebral fx **

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9
Q

Glipizide/ glyburide/ glimepiride (chlorpropamide, tolbutamide 1st generations)

A

Class: sulfonlureas
MOA: stimulate beta cells to inc insulin production (partially blocks ATP sensitive K channels, increasing the insulin release stage)
Second generations preferred
SE: hypoglycemia, weight gain
Generally ineffective after 5-10 years of use
Avoid in pts with sulfa allergy**
Glyburide has an increased risk of hypoglycemic events
Char: one AM dose, $4-50/month

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10
Q

Nateglinide (Starlix)

Repaglinide (Prandin)

A

Class: Meglitinide (non-sulfonylurea secretagogue)
MOA: increased insulin secretion, binds ATP dependent K channels
Prandin better than Starlix, Prandin is equal to sulfonlureas in activity
SE: hypoglycemia, weight gain
Approved for use with metformin, Sulfonylurea
Rapid,y absorbed in GI
TID-QID dosing before each meal, do not take if meals are skipped
No generic available $150-300/month

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11
Q

Rosiglitazone (Avandia)

Pioglitazone (ACTOS)

A

Class: thiazolidinediones (TZDs)/ glitazones
MOA: increase insulin sensitivity in skeletal muscle, decrease liver glucose production
Dosed once daily, may take 6-14 wks to have effect. Approved as mono therapy or with Sulfonylurea/ metformin
Only ACTOS is approved with insulin
SE: inc risk CHF, MI, dec BMD, inc risk fx, weight gain
*monitor lv fxn tests at 1 month and q3months
$125-200/month

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12
Q

Acarbose (precose)

Miglitol (Glyset)

A

Class: alpha-glucosidase inhibitors
MOA: inhibits brunch border alpha glucosidase in SI –> inhibited carbohydrate hydrolysis–> delayed glucose abs
Must be taken with each meal
No hypoglycemic risk alone, but inc risk with sulfonylurea/ insulin use
TID-QID $90-125/month
SE: abd pain, diarrhea, flatulence, inc transaminases, hepatic failure (acarbose)
CI: chronic intestinal dz, IBD, colonic ulceration, intestinal obstruction
*incase of hypoglycemia, give GLUCOSE, not sucrose

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13
Q

Pramlintide/ Symlin

A

Class: synthetic amylin (usu produced with insulin in beta cells)
Indic: Type 1 and 2 diabetics who use insulin
Allows put to use less insulin
Cannot be injected in same vial/syringe as insulin
1st drug for type 1 diabetics since insulin!
Inject at meal times
SE: modest weight loss, nausea (improves with optimal dose)

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14
Q

Exenatide/ Byetta

A

Class: incretin mimetics, synthetic exedin-4 hormone
Isolated from the Gila monster
Increases insulin secretion
Does not inc risk of hypoglycemia on its own, but can if taken with sulfonylureas

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15
Q

Sildenafil citrate / viagra
Tadalafil/ Cialis
Vardenafil/ Levitra

A

Class: phosphodiesterase type 5 inhibitor
MOA: increases cyclic GMP in smooth muscle–> inc blood in c.cavernosum
Indic: ED, pulmonary hypertension
SE: cyanopsia, photophobia, HA, flushing, hypotension, glaucoma, stroke, priapism
No erection without stimulation
25/50/100mg tabs available
Take 30mins to 4hrs prior to intercourse, no more than 1 tab qd
CI: nitrites, nitrates, NO, nitroglycerin…. Liver/renal impairment, hypotension, degenerative retinal disorders

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16
Q

Doxazosin (Cardura)
Terazosin (Hytrin)
Tamsulosin (Flomax/Urimax)
Silodosin (Urief)

A

Alpha blockers
Indic: BPH
All equally effective
SE: weakness, orthostatic hypotension, nasal congestion

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17
Q

Finasteride/ Proscar

A

Class: type 2 5-a-reductive inhibitor
MOA: decs DHT conversion, anti-androgen if
Indic: BPH, male pattern baldness, prostate CA
SE: dec libido, ED, impotency, depression, breast tenderness, breast swelling
PREGNANT FEMALES SHOULD NOT HANDLE

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18
Q

Leuprolide/ Lupron

A

Anti- androgenic, anti-estrogen if
Indic: prostate ca, precocious puberty, endometriosis, uterine fibroids, some IVF protocols
GnRH synthetic analog, interrupts T and E2 production
SE: dec libido, impotence, N/V, hot flashes, night sweats, arthralgias, myalgias, osteoporosis

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19
Q

Clomiphene/ Clomid

A

Class: SERM
Indic: infertility, amenorrhea
MOA: binds estrogen receptor sites –> inc GnRH –> inc LH, FSH –> ovulation stimulation
SE: multiple gestations, vaginal dryness, anxiety, hot flashes

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20
Q

Usual etiology for primary vs secondary vs tertiary hypothyroidism

A

Primary: autoimmune thyroiditis, iodine deficiency, malnutrition, surgery/ ablation
Secondary: pituitary dysfunction
Tertiary: hypothalamic dysfunction

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21
Q

1 grain equivalent doses for
Armor thyroid
Synthroid
Cytomel

A

1g= 60mg Armour Thyroid= 100mcg of T4 (Synthroid)= 25mcg of T3 (Cytomel)

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22
Q

Mifepristone/ Mifeprex

A

synthetic steroid, abortifacient within first 2 mo of Pgx
MOA: progestin antagonist, decreases hCG
85% effective in abortion within the first trimester
often used with Cytotec (prostaglandin E1 analog)
SE: abd pain, cramping, vag bleeding for 9-16 days, N/V, diarrhea, dizziness, fatigue, fever, excessive uterine bleeding
CI: IUD, ectopic pregnancy, Prednisone Tx, hemorrhagic d/o, anticoagulation Tx

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23
Q

Morning after pill

A

1 dose 1.5mg Levonorgestrel (progestin)
or 2 doses 750microgm q12hrs
Prevents implantation, can obtain same effect by taking multiple OCPs

OR

Ulipristal acetate (Ella)
Class: SPRM
given within 5 days of unprotected sex, inhibits ovulation

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24
Q

Skyla

A

IUD with 13.5mg Levonorgestrel at implantation
14 mcg/day released
FDA approves 3yrs continued use

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25
Liletta
IUD with 52mg Levonorgestrel 20mcg/day released 5yrs continued use approved
26
Mirena
IUD with 52mg Levonorgestrel 20mcg/day released 5yrs continued use approved
27
Paragard
copper, non-hormonal IUD MOA: impairs sperm mobility, ongoing inflammation decreases implantation approved for 10 years
28
Nuvaring
Low dose progestin and E2 release inserted for 3wks, then removed for 2wk for withdrawal bleed. decreased efficacy if removed for 3 hours. If removed for 3+ hours, use back-up contraception for 7 days. SE: vaginitis, HA, leucorrhea, nausea, weight gain CI in Hx of blood clots or in pt at inc risk of clotting
29
Ortho Evra
transdermal contraceptive patch inner adhesive layer, norelgestromin and ethanol estradiol middle layer, outer protective layer applied week for 3 weeks if patch detaches, replace w/in 48 hours with no effect on contraceptive efficacy. 2x risk of blood clots compared to oral contraception dt higher E2 exposure!
30
Implantable Contraceptives
Levonorgestrel (Norplant) no longer available Implanon (also a progestin implant) approved for up to 3 years, then must be removed
31
Medroxyprogesterone acetate/ Depro-provera IM
150mg aqueous suspension required 4x per year to maintain contraceptive efficacy high dose progesterone inhibits follicular development, decs GnRH ---> dec FSH, LH decreased risk of endometrial Ca SE: irregular menses, abd discomfort, weight changes, HA2yrs due to osteoporosis risk**
32
Drospirenone
``` Synthetic progestin (Yaz/Yasmin) closest pharmacology to natural progesterone, non-androgenic, a-mineralocorticoid properties ``` 6-7x the risk of thromboembolism to placebo 2x the risk of thromboembolism to levonorgestrel
33
What drugs can interact with BCPs/ Oral contraceptives?
Penicillin, amoxicillin, tetracycline, cephalosporins, sulfa drugs, seizure drugs, St Johns wort!
34
What is the most commonly used oral contraceptive formulation? What is the efficacy?
containing both estrogen (prevents ovulation) and progestin (prevents implantation) MC estrogen: ethanol estradiol MC progestin: norgestrel ~97-98% effective
35
Medroxyprogesterone/ Provera
Class: synthetic progesteron variant Indic: contraceptive, HRT
36
Progestins were added to Premarin/HRT in order to:
prevent endometrial hyperplasia
37
Premarin
Conjugated estrogen (estrone, equillon) Indic: P/Tx osteoporosis, post-menopause Sxs MOA: alters gene expression PO/topical creams available progesterone should be added in any female without a Hx of hysterectomy SE: vaginal bleeding, breast tenderness, increased DVT risk, inc atherosclerosis, CVD, increased risk of uterine, breast Ca, palpitations, fever, hives, SOB, weight gain CI: Hx of DVT, thromboembolism, Breast/Uterine/Ovarian Ca
38
BiEst/ TriEst
Bioidentical Hormones, PO and topical applications BiEst: 80:20 Estriol: Estradiol TriEst: 80:10:10 Estriol:Estradiol:Estrone
39
Some Pros/Cons of HRT (estrogen only)
PROS: reduced vasoconstrictive events (hot flashes, night sweats, etc). Prevention/Tx of postmenopausal vaginal atrophy, increased sleep quality, dec bone resorption, osteoporosis prevention CONS: increased stroke risk, blood clot risk, ovarian Ca, endometrial Ca, breast Ca [Note: Estrogen and progesterone formulations have an increased risk of DVT/PE/Stroke/Breast Ca but a decreased risk of Fx, colorectal Ca relative to estrogen only formulations]
40
Hypoglycemia Tx
Glucagon stimulates glucagon receptors --> breakdown of hepatic glycogen made from recombinant DNA IV/IM/SQ 1mg doses
41
Insulin Side Effects
weight gain, hypoglycemia, seizures, coma, death, hypokalemia, fibrotic injection sites, musc/fat atrophy at injection site
42
Long Acting Insulin Therapy onset/peak/duration
Glargine (Lantus) Onset: 4-6 hours Peak: none Duration: 24 hours
43
intermediate acting insulin therapy onset/peak/duration timing
NPH (humulin N) Onset: 1-3 hours Peak: 6-10 hours Duration: 10-18 hours
44
Short acting insulin therapy onset/peak/duration timing
Regular/ Humulin R Onset: 0.5-1 hour Peak: 2-4 hour Duration 4-12 hours
45
Rapid acting insulin therapy onset/peak/duration timing
SQ/IM/IV only Lispro/Aspart Humulog/Novalog Onset:
46
Exubera
nasal insulin | withdrawn in 2007 dt lack of acceptance by the market
47
Insulin MOA overview
anabolic hormone that promotes energy storage, stimulates glucose movement into cells, activates gene transcription --> increased cell growth and differentiation Promotes: glycogen productions, FA synthesis, Triglyceride storage Inhibits: hepatic ketogenesis, gluconeogenesis, glycogenesis
48
Dr. Miller preferences for DM treatment
newer drugs are no more effective, no safer, are more expensive than older Rxs Stick to metformin and sulfonylureas metformin alone is 1st choice
49
Troglitazone (Rezulin)
Class: TZD/ Glitazone succesful in DB-RCT studies, but found lethal SEs later. removed from market in 2000
50
DM Diagnostic Criteria
``` Fasting glucose >126mg/dl OR Non-fasting glucose >200mg/dl in patient with Sxs of DM OR OGTT >200mg/dl at 2 hours postprandial ```
51
Ipriflavone
synthetic isoflavone | may conserve bone loss but evidence is conflicting
52
Types of phytoestrogens and food sources
Isoflavones (genistein, diadzein, glyceitein, equol, eg): from soy beans, chickpeas, legumes Lignans (enterolactone, enterodiol, eg): oilseeds, flaxseeds, cereal bran, legumes, alcohol Coumestrans (coumestrol, eg): alfalfa, clover
53
Lovastatin (Mevacor) | Simvastatin (Zocor)
HMG-CoA reductase inhibitors (statins) | may decrease risk of hip fracture, increase BMD but not confirmed
54
Estrogen/ HRT for osteoporosis
reduces bone loss, incs BMD, dec risk fx Indic: prevention of osteoporosis in females PO/patch 0.625 mg/day E2+P decreases risk of endometrial Ca (Prempro) SE: vaginal bleeding, breast tenderness, venous blog clots, inc risk gall bladder dz Premarin: inc risk stroke Prempro: inc risk stroke, MI, Breast Ca ***Transdermal E2 does not affect clotting!**
55
Risk Factors for osteoporosis
``` Gender Age Size Ethnicity Family Hx Diet low in Ca, Vit D Sex hormones (estrogen) inactive lifestyle smoking, alcohol use glucocorticoid, anticonvulsant meds ```
56
Magnesium supplementation
300-1000 mg/day to help minimize bone loss with concurrent Ca/D supplementation SE: diarrhea at high doses
57
Vitamin D for osteoporosis
increases absorption of Ca in GI 70yo: 800 IU or higher Calcitriol/Rocaltrol: Rx D Derivative to inc bone mass, dec fx SE: elevated serum Ca- requires frequent monitoring
58
Calcium supplementation
50yo: 1200-1500 mg qd Breastfeeding: 2000 mg qd Ca citrate better absorbed that other salts Ca from oyster shells may have lead contamination effects of dietary Ca unclear (may increase risk?) *may not provide benefit in patients with Hx of osteoporosis related fx already*
59
Strontium supplementation
absorbed as Ca, increases osteoblastic activity Protos/ Strontium Ranelate is available in Europe may dec risk vertebral fx in postmenopausal females 500mg-1000mg qd in existing osteoporosis SE: generally well tolerated, mild diarrhea/GI upset >2gm may increase risk of fx- use caution!!
60
Radioactive iodine (131 I)
Radioactive Iodine Ablation (CATEGORY X) Indic: definitive hyperthyroid Tx, Thyroid Ca PO, radioactivity gone in 3-5 days (but postpone pregnancy 6-12 months) thyroid cell destruction goes on the wks SE: minimal systemic SEs, tenderness, swelling, N/V, bone marrow depression, acute leukemia possible, decreased sperm count (consider sperm banking) patient needs to be euthyroid prior to Tx no evidence of increased risk of malignancy lifelong T3/T4 supplementation required after procedure
61
Iodine/ SSKI
Class: elemental Iodine Indications: hyperthyroidism, thyroid storm MOA: large 1 dose inhibits thyroxine release PO/IV SE: rash, fever, 2-3 wks of benefit
62
Propranolol/ Inderal
Class: Non-selective B-blocker Indic: adrenergic block, hyperthyroidism, tachycardia, anxiety, thyroid storm MOA: B1/B2 block PO/IV SE: fatigue, sedation, impotency, depression
63
Propylthiouracil (PTU)
Class: Thionamide CATEGORY D (safer than methimazole) Indic: hyperthyroidism (Graves), used to control Sxs before surgery/ablation MOA: inhibits conversion of inorganic to organic **Blocks peripheral T3-T4 conversion** PO, qd NOT used for thyroid storm SE: hypothyroidism, rash, edema, arthralgia, agranulocytosis
64
Methimazole/ Tapazole
Class: Thionamide Indic: hyperthyroidism, Graves, may control Sxs until thyroid ablation MOA: inhibits transformation to organic iodine --> blocked thyroxine, dec T3/T4 formation PO qd dosing, NOT for thyroid storm CI IN PREGNANCY AND LONG-TERM USE SE: hypothyroidism, rash, edema, arthralgia, agranulocytosis
65
Hyperthyroidism common causes and Sxs:
autoimmune (Graves), thyroiditis, thyroiditis factitia Sis: nervousness, tachycardia, weight loss, heat intolerance, sweating, diarrhea, generalized weakness, increased risk of osteoporosis, CVD, goiter, exophthalmos, pretrial myxedema
66
Liothyronine/ Cytomel
synthetic T3 Indications: hypothyroidism not improving with T4, myxedema coma, Wilsons syndrome PO- 100% absorption, rapid absorption, half life of several hours SE: higher peaks/troughs and high CVD/Osteoporosis risk
67
Thyroid USP/ Armour
Porcine desiccated thyroid gland 0.2% Iodine standardized, PO 60mg= 1 grain= 38mcg T4/ 9mcg T3 SE: angina, palpitations, tachycardia, heat intolerance, anxiety, may accelerate CVD/osteoporosis
68
Levothyroxine/ Synthroid
Synthetic T4 Indic: hypothyroidism, TSH suppression with thyroid nodules and thyroid cancer PO/IV, once daily dosing, ramp up dose slowly, reduce if pt complains of angina SE: palpitations, tachycardia, heat intolerance, anxiety, may accelerate CVD/osteoporosis in the long term ***replace cortisol first in Addisons before replacing thyroid***
69
Clinical Findings in Hypothyroidism
fatigue, generalized weakness, cold intolerance, constipation, thinning hair, bradycardia, poor concentration respiratory depression, hypothermia, coma (myxedema coma), death
70
Thyroid Storm Sxs and Tx
Sxs: high fever, irritability, delirium, vomiting, diarrhea, dehydration, hypotension, vascular collapse, coma, death Tx: Beta blockers, IV-Iodine to "stun" thyroid *(can occur in septic hyperthyroid pts)

Pharmacology 2 (8 decks)

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