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Kaplan
Endocrine Drugs
| Question | Answer |
|---|---|
| What are the Meal Insulin preparations for type 1 diabetes? (3) | 1. Lispro 2. Aspart 3. Glulisine No LAG —> they work fast but does not last long |
| What are the BASAL insulin preparations for type 1 diabetes? (3) | 1. Glargine 2. Determir 3. Degludec Have a slower onset but last all day >24hrs) |
| What is the “peak effect” of Glargine and to which receptor does it bind to? | - Glargine has NO PEAK (which decreases the risk of hypoglycemia) - binds to TRANSMEMBRANE receptors which activate TYROSINE KINASE to phosphorylation tissue specific substrates |
| What is METFORMIN used for and its MOA | METFORMIN is the #1 drug for type 2 diabetics. MOA: DECREASE hepatic gluconeogenesis (liver is primary target) |
| What is the difference between a drug that targets glucose vs insulin? | target GLUCOSE: NO RISK of hypoglycemia target INSULIN: HIGH RISK of hypoglycemia |
| What are the side effect of METFORMIN? (2) | 1. Rare: lactic acidosis (in pt with renal dysfunction 2. GI distress |
| What is ACARBOSE and MOA | Type 2 diabetic drug MOA: inhibits a- glucosidase in brush borders (of small intestine) which decreases the formation of absorbable carbohydrate —> decrease demand for insulin release. |
| Sulfonylureas and MOA | Sulfonylureas is a drug used in type 2 diabetics. MOA: block POTASSIUM channel —> pancreatic B cells depolarized —> INSULIN RELEASE |
| What are the second generation Sulfonylureas drugs (2) ? | 1. Glipizide 2. Glyburide |
| What is a major side effect of Sulfonylureas? | Weight gain Hypoglycemia (bc it work on insulin opposed to glucose) Confusion |
| What is the relationship between the status of the POTTASIUM channel and INSULIN RELEASE? | Potassium channel Open —> DECREASE insulin RELEASE(hyperpolarization) Closed —> INCREASE insulin RELEASE (depolarization) (I think of it as an inverse relationship) |
| Through which transporter does glucose enter the pancreatic beta cells? | GLUT-2 (But GLUT -4 in adipose and skeletal muscle which is the only insulin dependent glucose transporter) |
| Repaglinide MOA | Release insulin from pancreatic beta cells |
| What are the “-glitazones”/ Thiazolidinediones? (2) | Pioglitazone Rosiglitazone |
| What are the MOA of Thiazolidinediones/ “glitazones”? And side effect? | Binds to PPAR- gamma to SENSITIZE TISSUES TO INSULIN S/E weight gain and edema but less hypoglycemia than Sulfonylureas |
| What is a -Glutide and MOA | Liraglutide MOA: GLP-1 is an incretin, augments glucose dependent insulin secretion ( and inhibits glucagon release) |
| What is a -Gliptin and MOA | Sitagliptin MOA: inhibits dipeptidyl peptidase (DPP-4) —> inhibiting inactivation of GLP-1 “Gliptin DPP” DPP is an enzyme that breakdown incretin/GLP-1 |
| What’s a major side effect of “glutides” that makes them popular? | Promote weight loss and improves CV outcomes |
| What are the SGLT-2 inhibitors and their MOA? | “-Gliflozins” Canagliflozin MOA: Blocks SGLT-2 in proximal tubules —> increase glucose excretion |
| What is a common S/E of SGLT2 inhibitors? | Recurrent UTIs dt increase glucose in urine |
| What is Pramlintide and MOA? | Analogue of AMYLIN ( appetite depressor) MOA: slows down food absorption rate, decrease glucose production. Good for type 1 and 2 diabetics! |
| What is Fludrocortisone? | Aldosterone replacement therapy |
| Which drug is a good replacement for cortisol and aldosterone bc they have a 1:1 ratio? | Hydrocortisone |
| What are the adrenal steroid receptor antagonists ? (3) | 1. Spironolactone (- aldosterone) 2. Mifepristone ( - progesterone) 3. Ketoconazole ( - cortisol) |
| Mifepristone MOA | Blocks glucocorticoid and progestin receptors |
| Ketoconazole MOA | At high doses, ketoconazole can also inhibit human steroid synthesis (e.g., cortisol and testosterone) side effects like gynecomastia and decreased libido. This is due to inhibition of human CYP450 enzymes involved in steroidogenesis |
| Metyrapone MOA | Blocks 11 B hydroxylase |
| What is Premarin (conjugated equine estrogens)? | Most common estrogen replacement for post menopausal women |
| What is the most commonly used estrogen replacement overall? | Ethinyl estradiol |
| What are the 2 AROMATASE inhibitors ? (Aromatase = enzyme that converts androgen to estrogen) | 1. Anastrozole 2. Letrozole Decrease estrogen/estradiol |
| Where is estrogen synthesized in premenopausal and postmenopausal women? | Premenopausal: OVARIES Postmenopausal: Adisope tissue( that is why AROMATASE inhibitors are used in postmenopausal women found in adipose tissue) |
| What is the fertility pill? And it’s MOA | Clomiphene MOA: DECREASE feedback inhibition —> INCREASE FSH AND LH —> ovulation and pregnancy |
| What are the 2 SERMs (selective estrogen receptor modulators)? | 1. Tamoxifen 2. Raloxifene Both are partial agonists |
| Which of the 2 SERMs has the highest risk of Endometrial cancer? | Tamoxifen (bc it works as a agonist on the endometrium) Ta m = Ta Malo pso increase risk of endometrial cancer |
| On which organs do the SERMs work on and as what (agonist or antagonist) | They work on BONE, BREAST and ENDOMETRIUM Bone: agonist (esp in postmenopausal women) Breast: antagonist (good for ER+ breast cancer) Endometrium: varies They are partial agonist so in no estrogen agonist, in estrogen antagonist. |
| What is an progestin antagonist? And what is it used for? | Antagonist: MIFEPRISTONE and it is used as an abortificient w/ Mitoprostol ( an prostaglandin) |
| What are the primary progestins? (2) | 1. Norethindrone 2. Desogestrel |
| In combined oral contraceptive pills what is the role of each component (estrogen/progestin) ? | Estrogen: SUPPRESS FSH, assist in suppressing ovulation Progestin: BLOCK LH SURGE to inhibit ovulation |
| What are the 3 Androgen blockers/ antagonists? | 1. Flutamide 2. Leuprolide 3. Finasteride |
| Leuprolide MOA | GnRH analog. It is an agonist but given in a continuous format can become ANTAGONIST Same mechanism as GOSRELIN and other -relins |
| Finasteride MOA | 5 alpha reductase inhibitor (prevent testosterone to DHT) |
| What are the effects of DHT ? (2) | 1. Hairloss 2. Prostate enlargement |
| What drug is used with Leuprolide to prevent tumor flare (when treating androgen receptor positive prostate cancer)? | Flutamide (Blocks androgen receptor) |
| What are the drugs used to decrease BPH (2) ? | 1. Alpha 1 blocker (Tamsolusin or -zosins ) 2. Finasteride |
| What are the drugs used for baldness (2) ? | 1. Minoxidil 2. Finasteride |
| What are the drugs that inhibits Thyroid peroxidase (2)? | 1. Propylthiuracil 2. Methimazole They are THIOAMIDES |
| Drug induced AGRANULOCYTOSIS are (3): | 1. Propylthiouracil 2. Methimazole 3. Clozapine ( atypical antipsychotic) |
| What are the side effects of Thioamides (2)? | 1. Agranulocyrosis 2. Liver failure (especially PTU) |
| MOA of Iodine (Lugosi solution) | Proteolytic release of T3 T4 from thyroglobulin |
| Which drug inhibit T4 to T3 conversion in the peripheral tissues (2) ? | 1. PTU 2. Propranolol |
| What are the drug used in SIADH that blocks v2 receptors? (2) | -vaptan’s 2. Tolvaptan Demeclocycline (desensitize ADH to tubule) |
| Drug of choice of Lithium induced nephrogenic diabetes insipidus ? | Amiloride |
| What is a Dopmine analog and what is it used for? | CABERGOLINE used for HYPERPROLACTINEMIA |
| What is a Somatostatin analog and what is it used for? | Octreotide Used for almost all hormone secretion (inhibit hepatic bile secreting and gall bladder emptying) |
| What are the drugs used for treatment of OSTEOPOROSIS? (3) And their general moa | 1. Bisphosphonates 2. Teriparatide 3. Denosumab |
| What are the Bisphosphonates/ -dronates? (1) and MOA | Alendronate MOA: inhibit enzyme FARNESYL PYROPHOSPHATE (FPP) synthase in the mevalonate pathway. —> inhibit bone resorption |
| What is a side effect if Alendronate (a Bisphosphonates)? | Esophageal ulcer. After taken drink water and sit up for 30 minutes |
| Teriparatide MOA | Recombinant PTH ANALOG (PTH first activate osteoblast) |
| Which is the only osteoporosis pharmacotherapy that induce osteoblast formation and does not inhibit osteoclasts? | Teriparatide |
| Denosumab MOA | Inhibits RANK LIGAND ( protein that acts as the primary signal for bone removal) |
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