Endocrinology Flashcards by Mike Mah

Rapid acting insulins

Insulin (short acting)
Lispro
Aspart
Glulisine

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Intermediate acting insulin

NPH

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Long acting insulin

Glargine

Detemir

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Biguanides: Metformin

bypass insulin receptors
Mech: activates PPAR
Use: 1st line therapy for DM2
Tox: GI upset, lactic acidosis (C/I in renal failure)

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Sulfonylureas: First generation
Tolbutamide
Chlorpropamide

Stimulates insulin release
Mech: Close K+ channel in β-cell membrane => cell depolarizes & triggers insulin release via Ca2+ influx.
Use: DM2, useless in DM1.
Tox: Hypoglycemia in renal failure, disulfiram-like effects.

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Sulfonylureas: Second generation:
Glyburide
Glimepiride
Glipizide

Stimulates insulin release
Mech: Close K+ channel in β-cell membrane => cell depolarizes & triggers insulin release via Ca2+ influx.
Use: DM2, useless in DM1.
Tox: Hypoglycemia.

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Glitazones/thiazolidinediones:
Pioglitazone
Rosiglitazone

bypass insulin receptors
Mech: activates PPAR
Use: DM2
Tox: Weight gain, edema, hepatotoxicity, heart failure.

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α-glucosidase inhibitors:
Acarbose
Miglitol

dec. postprandial hyperglycemia.
Use: DM2
Tox: GI disturbance

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Amylin analogs:

Pramlintide

dec. gastric emptying, dec. glucagon.
Use: DM1 & 2
Tox: Hypoglycemia, nausea, diarrhea.

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GLP-1 analogs:
Exenatide
Liraglutide

inc. insulin prod.
Mech: stimulating beta-cells to prod. insulin
Use: DM2
Tox: Nausea, vomiting, pancreatitis.

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DPP-4 inhibitors:
Linagliptin
Saxagliptin
Sitagliptin

inc. insulin prod.
Mech: inhibiting DPP-4 from digesting GLP-1
Use: DM2
Tox: Mild urinary or respiratory infections.

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Sulfonylureas: First generation

Tolbutamide

Chlorpropamide

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Sulfonylureas: Second generation:

Glyburide
Glimepiride
Glipizide

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Glitazones/thiazolidinediones:

Pioglitazone

Rosiglitazone

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α-glucosidase inhibitors:

Acarbose

Miglitol

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Amylin analogs:

Pramlintide

GLP-1 analogs:

Exenatide

Liraglutide

DPP-4 inhibitors:

Linagliptin
Saxagliptin
Sitagliptin

Mifepristone (RU-486)

Comp. inhibitor of progestins at progesterone receptors.
Use: Abortion (w/misoprostol).
Tox: Heavy bleeding, GI effects, abdominal pain.

Ketoconazole

Inhibits steroid synthesis (inhibits 17,20-desmolase).
Use: Polycystic ovarian syndrome to prevent hirsutism.
Tox: gynecomastia, amenorrhea.

*also anti-fungal. Its the gynecomastia w/athletes foot drug.

Spironolactone

Inhibits steroid binding, 17α-hydroxylase, and 17,20-desmolase.
Use: Polycystic ovarian syndrome to prevent hirsutism.
Tox: gynecomastia, amenorrhea.

Estrogens:
ethinyl estradiol
Diethylstilbestrol (DES)
mestranol

*“est” in the name

-Estrogen analog
-Use:
Female hypogodanism (ie. Turners)
HRT in menopause (w/progestrins)
Contraception
Etc.
-Tox: endometrial hyperplasia/carcinoma, bleeding in postmenopausal women, clear cell adenocarcinoma (DES only), inc. risk of thrombi,

Anastrozole, exemestane

aromatase inhibitors

- Use: Estrogen-dependent postmenopausal breast cancer.

Clomiphene

Stimulates ovulation. “Fertility pill”.
Mech: ER antagonist prevents normal E feedback to hypoT, inc. FSH and LH, causes ovulation.
Causes LH/FSH surge.
Use: infertility due to anovulation (ie. PCOS)
Tox: hot flashes, ovarian enlargement, multiple simultaneous pregnancies, and visual disturbances.

Raloxifene

- SERM: ER agonist on bone; antagonist at uterus. - Use: prophylaxis of post-meno. osteoporosis - Tox: thrombi formation

Tamoxifen

- SERM: Antagonist @ breast; agonist @ uterus, bone. - Use: Treat and prevent recurrence of ER pos. breast cancer. - Tox: Endometrial cancer, thrombus formation.

Progestrins

- Thicken cervical mucus, inhibit endometrial prolif., also E & P have neg. feedback on LH & FSH. - Use: Oral contraceptives. - Tox: C/I in smokers => thrombus formation. *OCP => liver adenoma

Flutamide

- androgen receptor antagonist | - Use: prostate carcinoma

Leuprolide

- GnRH analog: - -agonist: pulsatile doses - -antagonist: continuous dose - Use: - -pulsatile (agonist): infertility, - -cont. (antagonist): prostate cancer, uterine fibroids (leiomyoma), precocious puberty. - Tox: Antiandrogen, nausea, vomiting.

Propylthiouracil

- blocks thyroid peroxidase & 5′-deiodinase. - Use: Hyperthyroidism - Tox: Skin rash, agranulocytosis (rare), aplastic anemia, hepatotoxicity.

methimazole

- blocks thyroid peroxidase - Use: Hyperthyroidism - Tox: Skin rash, agranulocytosis (rare), aplastic anemia, hepatotoxicity, possible teratogen (causing aplasia cutis).

bromocriptine, capergoline

- dopamine analog - PRL inhibitor - Use: hyperprolactinemia - Tox: dyskinesia, nausea, vomitting, psychosis

Bisphosphonates | *-dronates

- Dec. bone resorption by inhibiting osteoclasts. - Use: Paget disease, Osteoporosis, hypercalcemia - Tox: Corrosive esophagitis, osteonecrosis of the jaw.

Teriparatide

- Inc. bone density/mass. - Mech:PTH analog. Stimulates osteoblast activity, inc. GI absorption of Ca., inc. renal resorption of Ca. - Use: osteoporosis - Tox: never use more than 2 yrs due to inc. risk of osteosarcoma (cancer of osteoblasts). *intermittent PTH stimulates bone formation whereas continuous PTH stimulates bone resorption.

pegvisomant

GH receptor antagonist