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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
Finasteride
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
Sprinolactone
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
Flutamide
MOA: - Anti-androgen - Competitive AR antagonist Indications: - Hormonal therapy for prostate cancer - Hirsutism (rarely) Adverse effects: -Hepatotoxicity
28
Cinacalcet
MOA: CaSR agnonist = Suppresses abnormal/unwanted PTH secretion Uses: o Parathyroid carcinoma o Secondary hyperparathyroidism due to ESRD/HD
29
Loop diuretics (Furosemide)
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
Thiazide diuretics (hydrochlorothiazide)
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
Estrogen
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
Raloxifene
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
Alendronate
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
Risedronate
MOA: Bisphosphonate Efficacy: Same as Alendronate Side effects: Same as Alendronate
35
Ibandronate
MOA: Bisphosphonate Dosed orally monthly or IV every 3 months Efficacy: Antifracture efficacy only shown for vertebral fractures Side effects: Same as Alendronate
36
Zoledronic Acid
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
Calcitonin
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
Denosumab
``` 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
Teriparatide
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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