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Endo & Reproduction
Pharmacology: Endocrine and Reproduction
Question | Answer |
---|---|
Sulfonylureas mechanism of action? | block K+ channels on pancreatic β cells leading to cell depolarization and insulin release |
Mechanism of action of Acarbose, miglitol | inhibits α-glucosidase in brush borders of small intestine → ↓ absorbable carbohydrate in intestine |
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 |
Mechanism of action of exenatide | GLP-1 analog that stiulates release of insulin from pancreatic β-islet cells |
How does octreotide effect insulin levels? | long-acting somatostatin analog that decreases insulin secretion |
How does Diazoxide effect insulin levels? | diazoxide activates K+ channels leading to pancreatic cell membrane hyperpolarization which decreases insulin release |
What is the primary tissue thiazolidinediones act on? | adipose tissue (contains the highest level of PPAR-γ) |
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 |
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 |
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 |
Repaglinide mechanism of action | Meglitinide class. Blocks pancreatic β-cell K+ channel → cell depolarization and insulin release. |
1. Competitive dipeptidyl peptidase IV inhibitor 2. Irreversible dipeptidyl peptidase IV inhibitor 3. Synthetic amylin | 1. Sitagliptin 2. Saxagliptin 3. Pramlintide |
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 |
Metyrapone 1. Mechanism of action 2. treatment usage | 1. inhibits steroid 11β-hydroxylase 2. used to treat Cushings syndrome |
Finasteride 1. Mechanism of action 2. Usage | 1. 5α-reductase inhibitor 2. BPH, male pattern baldness (androgenic alopecia) |
1. androgen receptor antagonist used in prostate cancer 2. GnRH analog | 1. Flutamide 2. Leuprolide, Goserelin |
What is the mechanism of action of the oral contraceptives? | suppresses gonadotropins, especially midcycle LH surge |
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 |
Synthetic insulins: 1. rapid acting (3) 2. intermediate acting 3. long-acting | 1. regular insulin, lispro, aspart 2. NPH 3. glargine |
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 |
1. Main side effect of metformin? 2. Why is this seen? | 1. lactic acidoss 2. metformin ↓ gluconeogenesis so lactic acid cannot be degraded |
1. Which receptor does insulin act through? 2. Which receptor does IGF-1 act through? | 1. receptor tyrosine kinase 2. G-protein adenylate cyclase |
Why should nonselective β-blockers be avoided in diabetic patients? | blockade of β2-adrenergic receptors inhibits hepatic gluconeogenesis, glycogenolysis and lipolysis |
Which diabetes drug increases adiponectin? | thiazolidinediones through ↑PPARγ → ↑ fat → ↑ adiponectin |
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. |
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) |
1. Drug that can increase release of vWF from platelets 2. ADH antagonist used in SIADH | 1. desmopressin 2. demeclocycline |
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 |
What is the treatment for thyroid storm? | β1-blocker and propylthiouracil |
1. Treatment for central diabetes insipidus 2. Treatment for nephrogenic diabetes insipidus | 1. desmopressin (intranasal) 2. hydrochlorothiazide, indomethacin or amiloride |
Which antisiezure medication is given for prevention and treatment of eclampsia? | magnesium sulfate |
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 |
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 |
Clomiphene 1. Mechanism of action 2. Clinical use? | 1. partial agonist at estrogen receptors in hypothalamus 2. infertility, Polycystic ovary (increase LH/FSH release) |
How does Tamoxifen effect estrogen receptors on: 1. Bone 2. Breast 3. Endometrium | 1. Agonist 2. Antagonist 3. Agonist |
How does Raloxifen effect estrogen receptors on: 1. Bone 2. Breast 3. Endometrium | 1. Agonist 2. Antagonist 3. Antagonist |
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 |
1. α1-antagonist that is selective for receptors in prostate versus the vasculature 2. non-selective α1 receptor antagonist | 1. Tamsulosin 2. terazosin, prazosin |
1. PGE2 analog causing cervical dilation and uterine contraction 2. β2-agonist that relaxes uterus and reduces premature contractions | 1. dinoprostone 2. Ritodrine/terbutaline |
Mechanism of action of Sildenafil | inhibit cGMP phosphodiesterase |
Naturally occuring substance used to inhibit bone resorption in Paget's disease of bone | calcitonin |
What is the treatment for myxedema coma? | free T4 |
Does glucocorticoid usage lead to potassium ion imbalance? | yes; possess mineralocorticoid acitivity which can lead to hypokalemia |
Treatment of choice for hyperthyroidism during pregnancy | propylthiouracil is more protein bound which reduces its crossing of the placenta |
Progesterone receptor inhibitor used to terminate pregnancy | Mifepristone |
How do the following effect insulin release: 1. β2 receptors 3. α1 receptors | 1. block insulin secretion 2. stimulates insulin secretion |