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Endocrine Physiology > Endocrine Drugs > Flashcards

Endocrine Drugs Flashcards

1
Q

Short Acting Insulin

A

Lispro (Commonly in pumps)
Aspart (Commonly in pumps)
Glulisine
Regular

Uses:
Bolus or mealtime insulin; taken to match CHO intake

Onset: 5-15 min
Peaks: 45-75 min
Duration: 2-4 hr
(For Regular): IV infusion in hospital (30 min onset; duration 5-8 hours)

Adverse effects:

  • Hypoglycemia
  • Local injection reactions
  • Weight gain
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2
Q

Intermediate/ Long-Acting Insulin

A

NPH (Neutral Protamine Hagedorn)
Glargine
Detemir

Used as basal insulin; taken independent of food intake

NPH: 2x/day dosing → produces peak (6-10 hours)
Glargine : 1x/day dosing (duration 20 - >24 hr; no peak)
Detemir : 2x/day dosing (duration 6-24 hr; no peak)

Adverse effects:

  • Hypoglycemia
  • Local injection reactions
  • Weight gain
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3
Q

Sulfonylureas

A

Glipizide
Glyburide
Glimepiride

MOA:
Bind to sulfonylurea receptor (SUR1) → closes ATP-dependent K+ channel Kir6.2 on beta cells → depolarizes cell → increased insulin secretion
Decrease in A1c ~1-2%

Treat Type 2 DM
Dosed orally 1-2x/day

Adverse effects:

  • Hypoglycemia
  • Weight gain
  • Caution in elderly; with renal and liver failure
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4
Q

Meglitinides

A

Nateglinide
Repaglinide

MOA:
Similar to Sulfonylureas but shorter acting
Decrease in A1c ~0.5-1.5%

Treat Type 2 DM

  • Short acting
  • Dose orally with each meal

Adverse effects:

  • Hypoglycemia (mild)
  • Weight gain (mild)
  • Caution with renal and liver failure
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5
Q

Biguanides

A

Metformin

MOA:
-Not well understood
-Increased insulin sensitivity (esp at liver)
-Decreased hepatic glucose production 
Decrease in A1c ~1-2%

Uses:
1st line drug in obese patients with Type 2 DM
-Weight loss or weight neutral
-Does not cause hypoglycemia

Adverse effects:

  • GI symptoms (metallic taste, nausea, diarrhea)
  • Lactic acidosis (rare)

Contraindications:

  • Renal insufficiency (Cr >1.4-1.5 mg/dL)
  • Liver disease, alcohol abuse
  • Heart failure
  • Serious acute illness
  • Age >80 years
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6
Q

Thiazolidinediones

A

Rosiglitazone
Pioglitazone

MOA:
PPARγ = peroxisome proliferator activated receptor gamma (member of nuclear receptor superfamily)
-Agonist of PPARγ receptor = sensitizes skeletal muscle to insulin → increased glucose uptake
-Decreases hepatic glucose production
Decrease in A1c ~0.5-1.4%

Uses:
Does not cause hypoglycemia
Pioglitazone improves lipid profile

Delayed onset of action = may take 6-12 weeks for peak effect

Adverse effects:

  • Weight gain
  • Edema/Fluid retention
  • Increased risk osteoporosis/ Fractures
  • Contraindicated in heart failure; caution in liver failure
  • Rosiglitizone may be associated with increased risk of CVD events (MI, stroke) so restricted use
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7
Q

α-Glucosidase Inhibitors

A

Acarbose

MOA:
α-Glucosidase (enzyme in intestinal wall) = converts CHO into monosaccharides
-Inhibits α-Glucosidase → delays CHO digestion and absorption → lowers blood glucose
Decrease in A1c ~0.5-0.8%

Adverse effects:
-Flatulence, diarrhea

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8
Q

Incretin Mimetics

A

Exenatide
Liraglutide

MOA:
Incretins = hormones made by GI tract to regulate blood glucose
-Agonists at incretin GLP-1 receptor
-Promotes glucose-mediated insulin secretion (glucose must be present)
-Decreases hepatic glucose production
-Slows gastric emptying
-Mimetics = longer ½ life than GLP-1 since less degradation by DPP-4
Decrease in A1c ~0.5-1%

Uses:

  • Reduces appetite and improves satiety → weight loss
  • Does not cause hypoglycemia
  • May support beta cell mass/survival
  • Injected subcutaneously
  • Dosing ranges: 1x/day – 1x/week

Adverse Effects:

  • GI symptoms (nausea, vomiting)
  • Caution in renal insufficiency
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9
Q

Dipeptidyl Peptidase 4 (DPP-4) Inhibitors

A

Sitagliptin
Saxagliptin

MOA:
Inhibits dipeptidyl peptidase 4 (degrades GLP-1) → increases circulating GLP-1 levels & insulin secretion
Decrease in A1c ~0.5-0.8%

Adverse Effects:
None significant

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10
Q

Glucagon

A

MOA:
Stimulates adenylate cyclase → increased cAMP → promotes hepatic GNG and glycogenolysis → increased blood glucose

Uses:
Hypoglycemia (when oral intake not possible)

Adverse Effects:
None significant

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11
Q

Luprolide

GnRH agonists

A

MOA:
Pulsatile secretion:
FSH → folliculogenesis & spermatogenesis
LH → ovulation, ovarian & testicular steroidgenesis
Long-acting/continuous:
Initially stimulates FSH/LH (Flare effect); then inhibition (hypogonadotropic hypogonadism)

Indications:
Testing:
-Evaluate precocious and delayed puberty (single dose “LHRH” test)
Pulsatile GnRH:
-Hypogonadotropic hypogonadism (ex: Kallmann syndrome)
Non-pulsatile:
-Children: suppress central precocious puberty
-Women: treat endometriosis, fibroids, fertility tx
-Men: androgen deprivation for prostate cancer

Adverse effects:
Hypogonadism sx:
-Hot flashes
-Low libido
-Amenorrhea, infertility 
(all of above = reversible)
-Bone loss = limiting factor
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12
Q

GnRH antagonists

A

MOA:
Immediate FSH/LH inhibition (no flare)

Indications:
Same as for non-pulsatile GnRH agonist

Adverse effects:

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13
Q

Recombinant FSH and hCG

A

MOA:
-Exogenous hCG is homologous to LH (same α-subunit) but longer ½-life

Indications:
Fertility tx and endocrine support:
-Daily FSH injections → stimulates ovarian follicle development or sperm production
-hCG (can be used in place of LH): stimulates LH surge (ovulation and progesterone production from CL); enhances spermatogenesis and testosterone secretion

Adverse effects:

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14
Q

Bromocriptine, cabergoline

A

MOA:
Dopamine receptor agonists → inhibits prolactin production

Indications:
Hyperprolactinemia/ prolactinoma

Adverse effects:
Nausea, hypotension, dizziness

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15
Q

Estradiol and other estrogens

A 
Indications:
Premature ovarian failure
Menopause
Prevention & tx of osteoporosis 
Contraception

Adverse effects:

  • Nausea & vomiting
  • Breast tenderness
  • Endometrial hyperplasia & increased risk of endometrial carcinoma if unopposed by progestin
  • Increased risk of thrombosis and thromboembolic events (smoking increases risk)
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16
Q

Clomiphene

A

MOA:
SERM
-Acts as antagonist
-Inhibits estrogen binding in hypothalamus and Ant. Pit.
-Prevents negative feedback of estrogen → increased GnRH secretion and gonadotropins → ovarian follicle development

Indications:
Ovulation induction

Adverse effects:

  • Multiple births
  • Hot flashes
  • Thick mucous and thin endometrium
17
Q

Tamoxifen

A

MOA:
SERM
-Estrogen antagonist in breast tissue
-Weak agonist in endometrium and bone

Indications:
Treat ER+ breast cancer

Adverse effects:

  • Endometrial hyperplasia/carcinoma
  • Hot flashes
  • Thromboembolic events
  • Can stimulate ovary → multiple births
18
Q

Raloxifene

A 
MOA:
SERM
-Estrogen agonist in bone
-Estrogen antagonist in breast tissue
NO action in endometrium

Indications:

  • Prevent and treat post-menopausal osteoporosis
  • Also decreases risk of ER+ breast cancer

Adverse effects:

  • Hot flashes
  • Thromboembolic events
19
Q

Anastrozole

A

MOA:
-Reversible aromatase inhibitor = inhibits androgen to estrogen conversion →lowers estrogen levels

Indications:

  • ER+ breast cancer
  • Ovulation induction (non-FDA approved use)

Adverse effects:

  • Hot flashes
  • Bone loss
20
Q

Letrozole

A

MOA:
-Reversible aromatase inhibitor = inhibits androgen to estrogen conversion →lowers estrogen levels

Indications:

  • ER+ breast cancer
  • Ovulation induction (non-FDA approved use)

Adverse effects:

  • Hot flashes
  • Bone loss
21
Q

Exemestane

A

MOA:
-Irreversible aromatase inhibitor

Indications:
-ER+ breast cancer

Adverse effects:

  • Hot flashes
  • Bone loss
22
Q

Progesterone and other progestins

A 
Indications:
Progesterone:
Pregnancy maintenance
Progestin:
Hormone replacement therapy; part of combined contraceptives

Adverse effects:
Weight gain
Edema
Menstrual disorders

23
Q

Mifipristone

A

MOA:

  • Progesterone antagonist → breakdown of endometrium → detachment of blastocyte & decrease in hCG
  • Glucocorticoid receptor antagonist

Indications:

  • Termination of pregnancy
  • Treat Cushing’s Syndrome

Adverse effects:

  • Vaginal bleeding
  • Prevention/termination of pregnancy
  • Adrenal insufficiency (high doses)
24
Q

Testosterone

A

MOA:

  • Cannot be given orally (inactivated in liver)
  • Needs to be given IM, gel, or patch

Indications:

  • Replacement in males with testosterone deficiency
  • NOT help with fertility

Adverse effects:

  • Same as endogenous testosterone
  • Need to monitor: hematocrit (erythrocytosis); PSA (occult prostate cancer)
25
Q

Finasteride

A

MOA:

  • Anti-androgen
  • Inhibits 5α-reductase (converts testosterone to DHT)

Indications:

  • Symptoms of benign prostatic hypertrophy
  • Male-pattern baldness and hirsutism

Adverse effects:
-Hepatotoxicity

26
Q

Sprinolactone

A

MOA:

  • Anti-androgen
  • Weak blocker of AR & weak inhibitor of testosterone synthesis
  • Blocks mineralocorticoid receptor
  • Weak agonist activity at progesterone receptor

Indications:

  • Hirsutism in women
  • HT and CHF
  • Primary hyperaldosteronism

Adverse effects:

  • Hyperkalemia
  • Irregular menses
  • Gynecomastic in men
27
Q

Flutamide

A

MOA:

  • Anti-androgen
  • Competitive AR antagonist

Indications:

  • Hormonal therapy for prostate cancer
  • Hirsutism (rarely)

Adverse effects:
-Hepatotoxicity

28
Q

Cinacalcet

A

MOA:
CaSR agnonist = Suppresses abnormal/unwanted PTH secretion

Uses:
o Parathyroid carcinoma
o Secondary hyperparathyroidism due to ESRD/HD

29
Q

Loop diuretics (Furosemide)

A

MOA:
Blocks Na/K/Cl transport –> blocks Ca2+ reabsorption in thick ascending limb

Uses:
-Treat severe hypercalcemia (only after adequate volume expansion with saline since volume contraction from diuretic can impair renal function and limit Ca2+-excretion capability)

30
Q

Thiazide diuretics (hydrochlorothiazide)

A

MOA:
Block Na/Cl cotransporter in distal convoluted tubule –> decreased movement of Cl- into cell –> opens voltage-gated Ca2+ channel –> Ca2+ able to be reabsorbed

Uses:
Treat hypercalciuria (increased risk of kidney stones)
31
Q

Estrogen

A

MOA:
Antiresorptive
-Stimulates osteoblast maturation & prolongs lifespan
-Inhibits osteoclast maturation & shortens lifespan
-Inhibits RANKL expression → decreases osteoclast activity
Net effect: supports bone formation; suppresses bone resorption

Efficacy:
(Women’s Health Initiative) Small improvements in BMD; prevents fractures

Side effects:

  • CHD
  • Stroke
  • Breast Cancer
32
Q

Raloxifene

A

MOA:
Antiresorptive = SERM
-Bone: estrogen-like = improves bone density, prevents further loss
-Breast: anti-estrogen = decreases breast cancer risk
-Endometrium = neutral (no risk endometrial hyperplasia)

Efficacy:

  • Decreases risk of vertebral fracture by 30-50%
  • No proven effect on hip or other fractures

Side effects:
-Increased hot flashes and risk of thromboembolic disease

33
Q

Alendronate

A

MOA:
Bisphosphonate
For all bisphosphonates:
-Incorporated into bone matrix = reabsorbed by osteoclasts → impair function and induce apoptosis
-Result: small improvement in bone density, prevents further bone loss

Efficacy:
For all bisphosphonates:
-Preventing bone loss; small gains in bone density in clinical trials
-Decreases fracture risk ~50%

Side effects:
For all bisphosphonates:
-Oral form = upper GI symptoms/heartburn (so take on empty stomach, 8oz water, upright for 30 min)
-Osteonecrosis of the jaw (very rare)
-Atypical femoral fractures: very rare, “slightly less rare” on bisphosphonates = not alter the overall risk/benefit ratio which strongly favors overall fracture prevention in patients at risk

34
Q

Risedronate

A

MOA:
Bisphosphonate

Efficacy:
Same as Alendronate

Side effects:
Same as Alendronate

35
Q

Ibandronate

A

MOA:
Bisphosphonate
Dosed orally monthly or IV every 3 months

Efficacy:
Antifracture efficacy only shown for vertebral fractures

Side effects:
Same as Alendronate

36
Q

Zoledronic Acid

A

MOA:
Bisphosphonate
IV form, Dosed yearly (osteoporosis) or every 2 years (prevention)

Efficacy:

  • Most potent bisphosphonate
  • Antifracture efficacy at all sites
  • Decreases vertebral fracture by 70%

Side effects:

  • No GI side effects
  • Up to 1/3 have acute phase reaction to 1st infusion (fever, myalgias)
37
Q

Calcitonin

A

MOA:
Antiresorptive
-Produce by thyroid parafollicular cells
-No role in Ca2+ balance in humans; so use salmon-derived calcitonin pharmacologically
-Decreases Ca2+ levels acutely in severe hypercalcemia (short-lived effect)

Efficacy:

  • Some small vertebral fracture prevention data
  • Some supporting data for pain control in acute vertebral compression fracture

Side effects:

  • None significant
  • Recent data = possible link to increase in cancer risk
38
Q

Denosumab

A 
MOA:
Antiresorptive
-Monoclonal Ab to RANKL (functions like OPG)
-Decreases osteoclast activation 
-Subcutaneous injection every 6 months

Efficacy:

  • Antifracture efficacy at all sites
  • Vertebral fractures decreased 70%

Side effects:
-Possible increased risk of infections (RANKL signaling in immune cells)

39
Q

Teriparatide

A

MOA:

  • Anabolic agent
  • Short-acting recombinant PTH 1-34
  • Pulsatile PTH → stimulates osteoblasts more than osteoclasts → net gains in bone density
  • Dosed: daily injection for up to 2 years

Efficacy:

  • Significant gains in BMD (5-15%)
  • Decreases vertebral fractures ~65%; non-vertebral fractures ~50%

Side effects:

  • Mild (nausea, dizziness, weakness)
  • In rats = osteosarcoma; not shown in humans
  • Quickly lose bone gains when stop drug; so must follow treatment with anti-resorptive to maintain improvements

Endocrine Physiology (5 decks)

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