Pharmacology: Endocrine and Reproduction
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| Sulfonylureas mechanism of action? | block K+ channels on pancreatic β cells leading to cell depolarization and insulin release
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| Mechanism of action of Acarbose, miglitol | inhibits α-glucosidase in brush borders of small intestine → ↓ absorbable carbohydrate in intestine
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| Mechanism of action of Pioglitazone on peripheral and liver tissues. | Thiazolidinedione class
1. sensitization of tissues to insulin
- binds PPAR-γ and ↑ gene expression of proteins that facilitate the action of insulin
2. ↑ insulin receptor numbers
3. ↓ hepatic gluconeogenesis
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| Mechanism of action of exenatide | GLP-1 analog that stiulates release of insulin from pancreatic β-islet cells
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| How does octreotide effect insulin levels? | long-acting somatostatin analog that decreases insulin secretion
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| How does Diazoxide effect insulin levels? | diazoxide activates K+ channels leading to pancreatic cell membrane hyperpolarization which decreases insulin release
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| What is the primary tissue thiazolidinediones act on? | adipose tissue (contains the highest level of PPAR-γ)
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| Which diabetes drug is associated with: 1. fluid retention & weight gain 2. hypoglycemia 3. GI distress 4. lactic acidosis 5. pancreatitis 6. hepatotoxicity | 1. thiazolidinediones
2. sulfonylurea
3. acarbose, miglitol
4. metformin
5. exenatide (GLP-1 analog)
6. thiazolidinediones
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| Which diabetes medications: 1. enhance glucose uptake in adipose 2. increase insulin release from pancreas 3. inhibit liver production of glucose | 1. thiazolidinediones, metformin
2. sulfonylureas, meglitinide
3. thiazolidinediones, metformin
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| 1. Peptide hormone that is secretes with insulin by pancreatic β cells and decreases α-cell glucagon secretion 2. Mechanism of action of demeclocycline | 1. amylin
2. ADH antagonist
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| Repaglinide mechanism of action | Meglitinide class. Blocks pancreatic β-cell K+ channel → cell depolarization and insulin release.
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| 1. Competitive dipeptidyl peptidase IV inhibitor 2. Irreversible dipeptidyl peptidase IV inhibitor 3. Synthetic amylin | 1. Sitagliptin
2. Saxagliptin
3. Pramlintide
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| How are dipeptidyl peptidase IV (DPP-4) inhibitors useful in controlling diabetes? | 1. DPP-4 degrades incretins
2. incretins enhance insulin secretion
3. thus DPP-4 inhibitors enhance insulin secretions
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| Metyrapone 1. Mechanism of action 2. treatment usage | 1. inhibits steroid 11β-hydroxylase
2. used to treat Cushings syndrome
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| Finasteride 1. Mechanism of action 2. Usage | 1. 5α-reductase inhibitor
2. BPH, male pattern baldness (androgenic alopecia)
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| 1. androgen receptor antagonist used in prostate cancer 2. GnRH analog | 1. Flutamide
2. Leuprolide, Goserelin
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| What is the mechanism of action of the oral contraceptives? | suppresses gonadotropins, especially midcycle LH surge
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| 1. Propylthiouracil & methimazole mechanism of action 2. Which action does propylthiouracil have that methimazole does not? | 1. inhibit organification of I- to I2 and coupling of thyroid hormone synthesis
2. ↓ peripheral conversion of T4 to T3
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| Synthetic insulins: 1. rapid acting (3) 2. intermediate acting 3. long-acting | 1. regular insulin, lispro, aspart
2. NPH
3. glargine
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| 1. Which diabetes drug is contraindicated in renal failure? 2. Drug used in gestational diabetes 3. Type of insulin preferred to acutely treat diabetic ketoacidosis | 1. metformin
2. insulin
3. regular insulin
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| 1. Main side effect of metformin? 2. Why is this seen? | 1. lactic acidoss
2. metformin ↓ gluconeogenesis so lactic acid cannot be degraded
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| 1. Which receptor does insulin act through? 2. Which receptor does IGF-1 act through? | 1. receptor tyrosine kinase
2. G-protein adenylate cyclase
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| Why should nonselective β-blockers be avoided in diabetic patients? | blockade of β2-adrenergic receptors inhibits hepatic gluconeogenesis, glycogenolysis and lipolysis
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| Which diabetes drug increases adiponectin? | thiazolidinediones through ↑PPARγ → ↑ fat → ↑ adiponectin
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| 1. How may potassium perchlorate be used to treat hyperthyroidism? 2. Propanolol's effect in hyperthyroidism | 1. is competes with iodine for uptake into the follicular cell by the sodium/iodine transporter
2. ↓ sympathetic outflow; ↓ peripheral conversion of T4 to T31.
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| 1. Thyroxine replacement therapy 2. Drug used to treat hyperprolactinemia 3. Drug used to treat acromegaly | 1. Levothyroxine
2. bromocriptine (DA agonist)
3. octreotide (somatostatin)
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| 1. Drug that can increase release of vWF from platelets 2. ADH antagonist used in SIADH | 1. desmopressin
2. demeclocycline
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| What effect does prednisone have on: 1. WBC's 2. lipolysis 3. gluconeogenesis | 1. acutely ↑ neutrophils; ↓ all other WBC's
2. blocks insulin to favor lipolysis
3. ↑ gluconeogenesis
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| What is the treatment for thyroid storm? | β1-blocker and propylthiouracil
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| 1. Treatment for central diabetes insipidus 2. Treatment for nephrogenic diabetes insipidus | 1. desmopressin (intranasal)
2. hydrochlorothiazide, indomethacin or amiloride
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| Which antisiezure medication is given for prevention and treatment of eclampsia? | magnesium sulfate
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| 1. 5α-reductase inhibitor 2. Why is this an effective treatment for BPH? | 1. finasteride
2. inhibits conversion of testosterone to DHT; DHT is responsible for prostate growth
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| What frequency must GnRH (or leuprolide) be given to treat: 1. infertility 2. prostate cancer | 1. pulsatile - causes LH/FSH release
2. continuous - inhibits LH/FSH release
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| Clomiphene 1. Mechanism of action 2. Clinical use? | 1. partial agonist at estrogen receptors in hypothalamus
2. infertility, Polycystic ovary (increase LH/FSH release)
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| How does Tamoxifen effect estrogen receptors on: 1. Bone 2. Breast 3. Endometrium | 1. Agonist
2. Antagonist
3. Agonist
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| How does Raloxifen effect estrogen receptors on: 1. Bone 2. Breast 3. Endometrium | 1. Agonist
2. Antagonist
3. Antagonist
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| 1. Anastrozole mechanism of action 2. Why is it beneficial in postmenopausal women with breast cancer? | 1. Aromatase ihibitor
2. the primary source of estrogen in postmenopausal women is the conversion of androstenedione from the adrenal glands to estrogen via aromatase in adipocytes
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| 1. α1-antagonist that is selective for receptors in prostate versus the vasculature 2. non-selective α1 receptor antagonist | 1. Tamsulosin
2. terazosin, prazosin
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| 1. PGE2 analog causing cervical dilation and uterine contraction 2. β2-agonist that relaxes uterus and reduces premature contractions | 1. dinoprostone
2. Ritodrine/terbutaline
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| Mechanism of action of Sildenafil | inhibit cGMP phosphodiesterase
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| Naturally occuring substance used to inhibit bone resorption in Paget's disease of bone | calcitonin
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| What is the treatment for myxedema coma? | free T4
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| Does glucocorticoid usage lead to potassium ion imbalance? | yes; possess mineralocorticoid acitivity which can lead to hypokalemia
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| Treatment of choice for hyperthyroidism during pregnancy | propylthiouracil is more protein bound which reduces its crossing of the placenta
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| Progesterone receptor inhibitor used to terminate pregnancy | Mifepristone
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| How do the following effect insulin release: 1. β2 receptors 3. α1 receptors | 1. block insulin secretion
2. stimulates insulin secretion
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