| Term 
 
        | Drug to treat growth failure, GH deficiency, wasting? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | What are some side effects of somatropin and somatrem? |  | Definition 
 
        | Leukemia, insulin resistance, arthralgia |  | 
        |  | 
        
        | Term 
 
        | Who is somatropin and somatrem cxdx in? |  | Definition 
 
        | Pediatric patients with closed epiphyses, active underlying cranial lesion, and must use caution in diabetics |  | 
        |  | 
        
        | Term 
 | Definition 
 | 
        |  | 
        
        | Term 
 
        | Drug used if defective GHRH release but normally functioning anterior pituitary somatotrophs? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | Drug to treat Laron Dwarfism (mutation of GH receptor)? |  | Definition 
 
        | Mecasermin “I put my dwarf in ME CASE”
 |  | 
        |  | 
        
        | Term 
 | Definition 
 | 
        |  | 
        
        | Term 
 
        | Drug to treat acromegaly? |  | Definition 
 | 
        |  | 
        
        | Term 
 | Definition 
 | 
        |  | 
        
        | Term 
 
        | Drug used to treat Carcinoid crisis (flushing, diarrhea)? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | Drug to treat refractory acromegaly? |  | Definition 
 | 
        |  | 
        
        | Term 
 | Definition 
 | 
        |  | 
        
        | Term 
 
        | Side effect of Pegvisomant? |  | Definition 
 
        | inc pituitary adenoma size (need yearly MRI); Elevated serum aminotransferase levels |  | 
        |  | 
        
        | Term 
 
        | Concentrated FSH/LH obtained from post menopausal woman’s urine? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | Concentrated FSH obtained from post menopausal woman’s urine? |  | Definition 
 | 
        |  | 
        
        | Term 
 | Definition 
 | 
        |  | 
        
        | Term 
 
        | LH agonist/Ovulation inducer? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | LH agonist that stimulates Leydig cells to produce testosterone? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | Drugs used to treat infertility/develop ovarian follicles? |  | Definition 
 
        | Menotropin/follitropin/urofollitropin |  | 
        |  | 
        
        | Term 
 
        | Synthetic human GnRH with a short half life? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | Drug used to diagnose hypogonadism? |  | Definition 
 
        | Gonadorelin with pulsatile release |  | 
        |  | 
        
        | Term 
 
        | What are Goserelin/Histrelin/Naferelin/Triptorelin? |  | Definition 
 
        | Synthetic analogs of GnRH used in sustained release and have longer half lives than native GnRH or gonadorelin |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Synthetic analog of GnRH used in sustained release and have longer half lives than native GnRH or gonadorelin |  | 
        |  | 
        
        | Term 
 
        | MOA of sustained release GnRH analogues? |  | Definition 
 
        | --inhibits the release of FSH and LH in both men and women --desensitizes GnRH receptors;
 --produces biphasic response*: first 7-10 days there is a transient flare* that increases gonadal hormones, which is followed by a long-lasting suppression of gonadotropins
 |  | 
        |  | 
        
        | Term 
 
        | Drug used during IVF to keep LH surge low in controlled ovarian hyperstimulation? |  | Definition 
 
        | Leuprolide, nafarelin (GnRH analogs – works in 7-10 days) Ganirelix and Cetrorelix (GnRH anatagonists-immediate effect)
 |  | 
        |  | 
        
        | Term 
 
        | Drug used to treat endometriosis & uterine fibroids? |  | Definition 
 
        | Leuprolide, nafarelin, goserelin |  | 
        |  | 
        
        | Term 
 
        | Drug used to suppress central precocious puberty? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | MOA of Ganirelix, Cetrorelix, and Abarelix? |  | Definition 
 
        | GnRH receptor antagonists (-relix = hormone-release inhibiting peptides)
 (-relin = hormone-release stimulating peptides)
 |  | 
        |  | 
        
        | Term 
 
        | GnRH antagonist used in metastatic prostate cancer in patients with extensive metastases or tumor encroaching on the spinal cord? |  | Definition 
 | 
        |  | 
        
        | Term 
 | Definition 
 | 
        |  | 
        
        | Term 
 
        | Drugs used to treat hyperprolactinema (amenorrhea, galactorrhea, infertility)? |  | Definition 
 
        | Bromocriptine and Cabergoline have high agonist affinity for D2 receptors and inhibit prolactin release |  | 
        |  | 
        
        | Term 
 
        | D2-agonist used to treat acromegaly? |  | Definition 
 
        | Bromocriptine (if pituitary tumor secretes both GH and prolactin); use in combination with Octreotide |  | 
        |  | 
        
        | Term 
 
        | Which D2 agonist causes the least nausea? |  | Definition 
 
        | Cabergoline -intravaginal administration can also reduce nausea
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Orthostatic hypotension, MI (bromocriptine and pergolide), pulmonary fibrosis and effusion (cabergoline) |  | 
        |  | 
        
        | Term 
 
        | Indications for estrogen in females? |  | Definition 
 
        | Vasomotor symptoms of menopause, vulvar/vaginal atrophy, hypoestrogenism secondary to hypogonadism, castration or POF, osteoporosis |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Vaginal adenocarcinoma in offspring |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Breast & Endometrial cancers, Cerebral vascular coronary artery disease, Benign or malignant liver tumors, Severe HTN, Pregnancy, Female smokers over 35 years of age, Thrombotic disorders |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Selective estrogen-receptor modulator – they are estrogen agonists in some tissues and antagonists in others |  | 
        |  | 
        
        | Term 
 
        | SERM used in prevention, palliative, or adjuvant therapy for breast cancer? |  | Definition 
 | 
        |  | 
        
        | Term 
 | Definition 
 
        | estrogen receptor antagonist in breast tissue (good); partial agonist in endometrium (bad); partial agonist in bone (good) |  | 
        |  | 
        
        | Term 
 
        | Why can Tamoxifen only be used for less than 5 years? |  | Definition 
 
        | It is assoc with 4-6 fold inc in incidence of endometrial cancer |  | 
        |  | 
        
        | Term 
 
        | SERM used to treat female infertility due to an ovulatory disorder? |  | Definition 
 | 
        |  | 
        
        | Term 
 | Definition 
 
        | An estrogen receptor antagonist in hypothalamus and pituitary gland, and partial agonist in ovaries; disinhibits GnRH release and increases the level of LH and FSH. The increased FSH stimulates follicle growth, LH surge and ovulation. |  | 
        |  | 
        
        | Term 
 
        | Why is clomiphene better than exogenous FSH for infertility? |  | Definition 
 
        | clomiphene is rarely assoc with Ovarian Hyperstimulation Syndrome |  | 
        |  | 
        
        | Term 
 
        | SERM used to for osteoporosis prevention and treatment? |  | Definition 
 | 
        |  | 
        
        | Term 
 | Definition 
 
        | E2 agonist in bone; E2 antagonist in uterus/breast (Decreases risk of invasive breast cancer in postmenopausal women with osteoporosis)
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | ER antagonist. Blocks action of estrogen on target tissues |  | 
        |  | 
        
        | Term 
 
        | Drug to treat ER positive metastatic breast cancer in postmenopausal women with dz progression following anti-estrogen therapy? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | MOA of Anastrozole and Letrozole? |  | Definition 
 
        | Competitive inhibitors of aromatase |  | 
        |  | 
        
        | Term 
 
        | MOA of Exemestane and Formestane |  | Definition 
 
        | Irreversible inhibitors of aromatase |  | 
        |  | 
        
        | Term 
 
        | Major SE of aromatase inhibitors? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | What are aromatase inhibitors used to treat? |  | Definition 
 
        | Treatment and prevention of estrogen receptor positive early-stage, locally advanced, and metastatic breast cancer (may be more effective than SERMs) |  | 
        |  | 
        
        | Term 
 | Definition 
 | 
        |  | 
        
        | Term 
 | Definition 
 | 
        |  | 
        
        | Term 
 
        | What is medroxyprogesterone acetate? |  | Definition 
 
        | Injectable progestin-only OCP given every 3 mos (Depo-Provera) |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Implant progestin-only OCP effective for 3 yrs (Nexplanon) |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Progestin-only OCP – used in Plan B (oral) and Mirena (IUD) |  | 
        |  | 
        
        | Term 
 
        | How do the MOAs differ for progestin-only OCP and COCs? |  | Definition 
 
        | Progestin-only/‘mini pills’ = alter frequency of GnrH pulse to dec ant pituitary responsiveness to GnRH. Prevent pregnancy by thickening cervical mucus and thinning the lining of the uterus. Some suppress ovulation but that’s not the main way they work. No placebo pills – every pill is ‘active’. Still get period because LH surge is not suppressed. COC = suppress GnRH as well as LH and FSH. Prevent pregnancy by thickening cervical mucus, thinning lining of uterus and suppressing ovulation.  21-24 days active pills/4-7 days placebo.
 |  | 
        |  | 
        
        | Term 
 
        | Would you prescribe a progestin-only pill or COC to a woman who was at risk for heart disease or stroke? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | Would you prescribe a progestin-only pill or COC to a woman who was a heavy smoker? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | Would you prescribe a progestin-only pill or COC to a woman who is breast-feeding? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | How do inhibins and activins regulate LH and FSH release? |  | Definition 
 
        | Inhibins inhibit the release of FSH, while Activin stimulates FSH release. Inhibins or Activin do NOT regulate LH release. |  | 
        |  | 
        
        | Term 
 
        | MOA of mifepristone used as abortifacient? |  | Definition 
 
        | Inhibits progesterone binding to receptor |  | 
        |  | 
        
        | Term 
 
        | MOA for levonorgestrol/morning after pill? |  | Definition 
 
        | Blocks LH surge, disrupting normal ovulation, produces endometrial change for implantation, and impairs sperm transport. |  | 
        |  | 
        
        | Term 
 
        | How does the risk of endometrial cancer and breast cancer change with HRT use over time? |  | Definition 
 
        | Endometrial Cancer: Estrogen alone assoc. w/ 5-8-fold risk (inclusion of progestin eliminates risk) Breast Cancer: Little or no risk w/ HRT < 5 years, Relative risk of ~ 1.3 for HRT of 10-15 years, good evidence that progestin contributes to risk
 |  | 
        |  | 
        
        | Term 
 
        | What are testosterone enanthate/testosterone cypionate used for? |  | Definition 
 
        | HRT with testosterone in hypogonadism |  | 
        |  | 
        
        | Term 
 
        | What is the best route for testosterone enanthate/testosterone cypionate? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | SE of testosterone enanthate/testosterone cypionate? |  | Definition 
 
        | Cholestatic jaundice syndrome, Liver carcinoma, Benign prostatic hyperplasia, Prostate cancer, Gynecomastia, Acne, Headache |  | 
        |  | 
        
        | Term 
 
        | Drug used to treat metastatic prostate cancer/BPH? |  | Definition 
 | 
        |  | 
        
        | Term 
 | Definition 
 
        | Competitive inhibition of DHT and testosterone binding to receptor |  | 
        |  | 
        
        | Term 
 | Definition 
 | 
        |  | 
        
        | Term 
 
        | Drug used to treat BPH/androgenic alopecia? |  | Definition 
 | 
        |  | 
        
        | Term 
 | Definition 
 
        | Inhibition of 5a-reductase |  | 
        |  | 
        
        | Term 
 | Definition 
 | 
        |  | 
        
        | Term 
 
        | What drugs are given as adjunct in prostate cancer? |  | Definition 
 
        | sustained release GnRH agonists =Leuprolide, goserelin, histrelin, triptorelin |  | 
        |  | 
        
        | Term 
 
        | What are the two MOA of spironolactone? |  | Definition 
 
        | Aldosterone receptor antagonist; androgen receptor antagonist |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | T4 replacement therapy for hypothyroidism, cretinism, or TSH suppression therapy for thyroid cancer patients/nontoxic goiter |  | 
        |  | 
        
        | Term 
 
        | What drugs have increased action when given with levothyroxine? |  | Definition 
 
        | warfarin, tricyclic antidepressants, amiodarone |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | T3 replacement therapy for myxedema coma and prep for radioactive iodine therapy of thyroid cancer. T3 has an immediate effect. |  | 
        |  | 
        
        | Term 
 
        | What is the combination T3/T4 drug called? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | What is the DOC for hyperthyroidism? |  | Definition 
 | 
        |  | 
        
        | Term 
 | Definition 
 
        | inhibits PTU – Peroxidase/Peripheral deiodination, Tyrosine iodination, Union (coupling) |  | 
        |  | 
        
        | Term 
 
        | What is a serious SE of both PTU and Methimazole? |  | Definition 
 
        | Agranulocytosis (not dose dependent in PTU) |  | 
        |  | 
        
        | Term 
 
        | Drug to treat thyroid storm? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | Drug given to hyperthyroid pts pre-op? |  | Definition 
 | 
        |  | 
        
        | Term 
 | Definition 
 
        | High iodide concentrations inhibit uptake of I- iodination and coupling of tyrosyl residues on TG. It also inhibits release of thyroid hormone |  | 
        |  | 
        
        | Term 
 
        | How do you permanently treat hyperthyroidism? |  | Definition 
 
        | Ablation therapy with radioactive iodide |  | 
        |  | 
        
        | Term 
 
        | What adjuvant therapy can be given for hyperthyroid pts during thyroid storm or with radioactive iodide treatment? |  | Definition 
 
        | B-blockers – decreases HR and contractility but ALSO inhibits deiodination (T4 to T3 conversion) |  | 
        |  | 
        
        | Term 
 
        | What drug can you giving nursing mothers with hyperthyroidism? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | Drug cxdx with radioactive iodide? |  | Definition 
 
        | Iodide makes it ineffective |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Stimulates gut absorption of Ca and PO4; Stimulates osteoclasts via RANKL resorption of bone |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Rickets, osteomalacia, hypoparathyroidism, osteoporosis |  | 
        |  | 
        
        | Term 
 
        | Vit D derivative that suppresses PTH synthesis and secretion/used in hypoparathyroidism? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | Vit D derivative used for renal osteodystrophy? (bone mineralization deficiency due to electrolyte and endocrine derangements) |  | Definition 
 
        | 1a-hydroxycholecalciferol |  | 
        |  | 
        
        | Term 
 
        | Vit D derivative used topically for psoriasis? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | Vit D derivative used iv for secondary hyperparathyroidism? |  | Definition 
 | 
        |  | 
        
        | Term 
 | Definition 
 | 
        |  | 
        
        | Term 
 | Definition 
 
        | Although PTH can increase bone resorption, once daily injections of teriparatide enhance bone deposition |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Paget’s dz, open epiphyses, prior radiation. |  | 
        |  | 
        
        | Term 
 
        | What drug is synergistic with teriparatide? |  | Definition 
 | 
        |  | 
        
        | Term 
 | Definition 
 
        | Possibly osteosarcoma, limit use <2years |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Dec gut calcium absorption, inc Ca and PO4 excretion, inhibits osteoclasts |  | 
        |  | 
        
        | Term 
 
        | Adverse effect of calcitonin? |  | Definition 
 
        | Quick loss of effectiveness |  | 
        |  | 
        
        | Term 
 
        | Drug used to treat Paget’s dz? |  | Definition 
 
        | First line - bisphosphonates Can also use Calcitonin – inhibits osteoclast activity, but not as powerful as bisphosphonates
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | adsorbed to bone crystal making it resistant to enzymatic hydrolysis |  | 
        |  | 
        
        | Term 
 
        | Drug interactions with bisphosphonates? |  | Definition 
 
        | Al(OH)3, antacids, Ca, Mg, Fe salts – reduce absorption, NSAIDs- inc GI ulcers; Pamidronate does not have drug interactions |  | 
        |  | 
        
        | Term 
 
        | Cxdx for bisphosphonates? |  | Definition 
 
        | Pregnancy/breastfeeding, GI ulcers |  | 
        |  | 
        
        | Term 
 
        | Drug for hypercalcemia of malignancy? |  | Definition 
 
        | Bisphosphonates – pamidronate is best Calcitonin
 Gallium nitrate
 Hydrocortisone
 |  | 
        |  | 
        
        | Term 
 
        | Drug to treat parathyroid carcinoma? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | Drug to treat secondary hyperparathyroidism? |  | Definition 
 
        | Cinacalcet Iv paricalcitol also used
 *Secondary hyperparathyroidism -- The PTH is elevated due to decreased levels of calcium or 1,25-dihydroxy-vitamin D3. It is usually seen in cases of chronic renal disease or defective calcium receptors on the surface of parathyroid glands.
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Mimics Ca++ on the Ca++ sensing receptors to inhibit PTH secretion by parathyroid |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Hypocalcemia, CYP450 interactions |  | 
        |  | 
        
        | Term 
 
        | Monoclonal Ab against RANKL? What is RANKL? |  | Definition 
 
        | Denosumab RANKL is the ligand on osteoblasts that activates RANK on osteoclasts
 |  | 
        |  | 
        
        | Term 
 | Definition 
 | 
        |  | 
        
        | Term 
 | Definition 
 
        | Hypocalcemia – check Ca and Vit D levels before starting |  | 
        |  | 
        
        | Term 
 
        | Drug used for hypercalcemia of sarcoidosis? |  | Definition 
 
        | Hydrocortisone -reduces serum calcium concentrations within two to five days by decreasing calcitriol production by the activated mononuclear cells in the lung and lymph nodes
 |  | 
        |  | 
        
        | Term 
 
        | Drug used for osteoporosis in menstruating women? |  | Definition 
 
        | Raloxifene – estrogen agonist in bone/estrogen antagonist in breast |  | 
        |  | 
        
        | Term 
 | Definition 
 | 
        |  | 
        
        | Term 
 
        | What are the short, intermediate and long-acting glucocorticoids? |  | Definition 
 
        | Short-acting (8-12 hours) = hydrocortisone/cortisol (active) and cortisone (inactive) Intermediate acting (12-36 hours) = fludrocortisone, prednisone, prednisolone, tramcinolone
 Long-acting (36-72 hours) = dexamethasone and beclamethasone
 |  | 
        |  | 
        
        | Term 
 
        | Does cortisol act on GR, MR or both? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | How is cortisone converted to the active cortisol? |  | Definition 
 
        | 11B-HSD1 expressed in the liver converts cortisone to cortisol |  | 
        |  | 
        
        | Term 
 
        | How is cortisol converted to inactive cortisone? |  | Definition 
 
        | 11B-HSD2 in the kidney, salivary glands and colon (aldosterone sensitive tissues) converts cortisol to cortisone. This prevents the more abundant cortisol from inappropriately activating MR in these tissues. |  | 
        |  | 
        
        | Term 
 
        | Does fludrocortisone act on GR, MR or both? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | Does prednisone act on GR, MR or both? |  | Definition 
 
        | Both, but GR potency is greater than MR |  | 
        |  | 
        
        | Term 
 
        | Does dexamethasone act on GR, MR or both? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | Is prednisone or prednisolone active? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | SE of glucocorticoid use? |  | Definition 
 
        | Abrupt withdrawal = Adrenal crisis; Chronic use = cushingoid symtoms, hyperglycemia/diabetes, risk of infection, edema, HTN/CVD, mania, bone loss, peptic ulcers.
 |  | 
        |  | 
        
        | Term 
 
        | Drugs to treat Addison’s Disease (primary adrenal insufficiency)? |  | Definition 
 
        | Hydrocortisone or dexamethasone for cortisol replacement plus fludrocortisones for aldosterone replacement |  | 
        |  | 
        
        | Term 
 
        | Drugs to treat secondary adrenal insufficiency? (eg. Exogenous GC use) |  | Definition 
 
        | Hydrocortisone or dexamethasone for cortisol replacement (ACTH does not act on zona glomerulosa where aldosterone is made so fludrocortisones is not necessary) |  | 
        |  | 
        
        | Term 
 
        | Prenatal treatment of congenital adrenal hyperplasia? |  | Definition 
 
        | In utero dexamethasone before 9 weeks gestation for females only (inhibits ACTH and CRH production and thereby decreases androgen synthesis) |  | 
        |  | 
        
        | Term 
 
        | Postnatal treatment of congenital adrenal hyperplasia? |  | Definition 
 
        | Lifelong hydroxycortisone and fludrocortisones to prevent adrenal crisis |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Prednisolone injections into joint - 11B-HSD1 not expressed in the joint |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Hydrocortisone or prednisolone - 11B-HSD1 is not expressed in the skin |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | An antifungal medication that also suppresses glucocorticoid synthesis by inhibiting CYP11A1 (conversion of cholesterol to pregnenolone-RLS) and CYP11B1 (final enzyme in cortisol biosynthesis) to decrease cortisol. Therefore, it is useful in treating Cushing’s Disease |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | A short-acting iv anesthetic used for induction of general anesthesia and sedation. It also suppresses glucocorticoid synthesis by inhibiting CYP11A1 (conversion of cholesterol to pregnenolone-RLS) and CYP11B1 (final enzyme in cortisol biosynthesis) to decrease cortisol. Therefore, it is useful in treating Cushing’s Disease |  | 
        |  | 
        
        | Term 
 
        | What drug is used to treat Cushing’s disease during pregnancy? |  | Definition 
 
        | Metyrapone MOA: inhibits CYP11B1 and CYP11B2 (aldosterone synthase) to decrease cortisol
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Mitotane -spares z glomerulosa but induces mitochondrial destruction of z fasciculata and z reticularis
 |  | 
        |  | 
        
        | Term 
 
        | Newly approved drug to treat refractory Cushing’s syndrome? |  | Definition 
 
        | Mifepristone = GR antagonist at high doses |  | 
        |  | 
        
        | Term 
 
        | Onset, peak and duration of Insulin aspart, Insulin lispro, Insulin glulisine? |  | Definition 
 
        | Onset – 5-15 min Peak – 45-75 min
 Duration – 2-4 hours
 |  | 
        |  | 
        
        | Term 
 
        | Onset, peak and duration of regular Insulin? |  | Definition 
 
        | Onset – 30-60 min Peak – 2-4 hours
 Duration – 6-8 hours
 |  | 
        |  | 
        
        | Term 
 
        | Onset, peak and duration of NPH Insulin? |  | Definition 
 
        | Onset – 1.5-2 hours Peak – 6-10 hours
 Duration – 16-24 hours
 |  | 
        |  | 
        
        | Term 
 
        | Onset, peak and duration of Insulin detemir, Insulin glargine? |  | Definition 
 
        | Onset – ~2 hours Peak – no peak
 Duration – 20-24 hours
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Acts through insulin plasma membrane cell surface tyrosine kinase receptor. -stimulates glucose uptake via upregulation of GLUT4 glucose transporter into liver, muscle, and adipose tissue
 -inhibits hepatic glucose production
 -promotes AA uptake and protein synthesis in muscle
 -inhibits lipolysis and promotes TG storage
 |  | 
        |  | 
        
        | Term 
 
        | Conventional insulin regimen for Type I diabetics? |  | Definition 
 
        | Twice daily injections of pre-mixed intermediate insulin (NPH) + regular insulin. Dose is typically 50-75% NPH + 25-50% regular/fast acting insulin |  | 
        |  | 
        
        | Term 
 
        | Intensive therapy regimen for Type I diabetics? |  | Definition 
 
        | Intensive therapy = 1-2x daily basal insulin (NPH or glargine) and pre-meal bolus of rapid/fast-acting. Intensive therapy recommended for majority of Type I diabetics |  | 
        |  | 
        
        | Term 
 
        | What are the glycemic goals for Type I diabetics? |  | Definition 
 
        | Fasting blood Glucose = 90-130 mg/dL 2 hr Postprandial BG = <180 mg/dL
 HbA1c = <7%
 |  | 
        |  | 
        
        | Term 
 
        | What two classes of drugs are insulin sensitizers? |  | Definition 
 
        | Biguanides (metformin) and Thiazolidinediones (pioglitazone and rosiglitazone) |  | 
        |  | 
        
        | Term 
 
        | DOC for type 2 diabetics? |  | Definition 
 
        | Metformin Lowers fasting plasma glucose by dec hepatic gluconeogenesis. Inc insulin sensitivity/glucose uptake. Lowers HbA1c by 1.5-2%. Does not cause hypoglycemia. Not assoc with weight gain. Improves lipid profile. Decreases risk of MI, diabetes-related death.
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Inhibits Complex I in the electron transfer chain of mitochondrion resulting in an increase in the cellular concentration of AMP that in turn: 1. Inhibits glucagon-induced hepatogluconeogenesis by inhibiting the glucagons-induced activation of adenylate cyclase
 2. Activates the AMP-dependent protein kinase (AMPK) which promotes glucose uptake in adipose and muscle tissue, inhibits hepatic glucose, cholesterol and TG production, promotes FA oxidation and reduces FFA that contribute toward the development of insulin resistance, and inhibits inhibitors of insulin signaling pathway, enhancing insulin signaling and preventing insulin resistance.
 |  | 
        |  | 
        
        | Term 
 
        | Rare but serious SE of metformin? |  | Definition 
 | 
        |  | 
        
        | Term 
 | Definition 
 
        | Pregnancy, 48 hr before iodinated contrast, renal/liver dz, CHF,  >80yo |  | 
        |  | 
        
        | Term 
 
        | MOA of pioglitazone and rosiglitazone? |  | Definition 
 
        | PPARg agonists which increases insulin sensitivity and decreases fasting plasma glucose by inc expression of GLUT4, increasing adiponectin (promotes insulin sensitivity), promotes FFA uptake (FFA promote insulin resistance) |  | 
        |  | 
        
        | Term 
 
        | SE of thiazolidinediones (pioglitazone and rosiglitazone)? |  | Definition 
 
        | Weight gain, CHF (black box warning), fracture, inc risk of bladder cancer |  | 
        |  | 
        
        | Term 
 
        | Cxdx for thiazolidinediones (pioglitazone and rosiglitazone)? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | What are Glimepiride, Glyburide, Glipizide? What is their MOA? |  | Definition 
 
        | Sulfonylureas(insulin secretagogues) MOA: stimulates insulin secretion in pancreatic B cells by inhibiting SUR1 subunit of K+channels. Cell depolarization triggers Ca2+ influx through VG-calcium channels and the secretion of insulin. Reduces fasting plasma glucose.
 |  | 
        |  | 
        
        | Term 
 
        | Which sulfonylurea should be used in pts with renal insufficiency and elderly? What is an alternative to this? |  | Definition 
 
        | Glipizide – shorter acting, inactive metabolite Alternative – repaglinide – 90% fecal elimination
 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Hypoglycemia in pts with impaired renal/hepatic function and elderly; subQ weight gain |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Sulfa allergy, pts with diabetes over 10 years (beta cells need to be functional), renal/liver failure, pregnant/lactating, elderly. Cannot be taken with salicylates, B-blockers, warfarin and fibrates because they displace sulfonylurea and inc the risk of hypoglycemia. |  | 
        |  | 
        
        | Term 
 
        | How do meglitinides differ from sulfonylureas? |  | Definition 
 
        | Meglitinides interact with a different region of SUR1 subunits of the beta cell K+/ATP channel. Meglitinides have a more rapid onset* and shorter duration*. Meglitinides are glucose-dependent*.
 Meglitinides are good for postprandial glucose control whereas sulfonylureas are good for fasting glucose control.
 |  | 
        |  | 
        
        | Term 
 
        | Which meglitinide affects both postprandial and fasting glucose? |  | Definition 
 | 
        |  | 
        
        | Term 
 | Definition 
 | 
        |  | 
        
        | Term 
 | Definition 
 | 
        |  | 
        
        | Term 
 | Definition 
 
        | DPP-IV inhibitor – blocks degradation of GLP-1 |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | DPP-IV inhibitor – blocks degradation of GLP-1 |  | 
        |  | 
        
        | Term 
 
        | Rare but serious SE of incretin mimetics (GLP-1 homologs and DPP-IV inhibitors) |  | Definition 
 | 
        |  | 
        
        | Term 
 | Definition 
 
        | Incretins are a group of GI hormones (eg. GLP-1 and gastric inhibitory peptide or GIP) that stimulate a decrease in blood glucose levels. Incretins increase insulin release from beta cells before blood glucose levels become elevated, reduce gastric emptying, and inhibit glucagon release. Both GLP-1 and GIP are rapidly inactivated by the enzyme dipeptidyl peptidase-4 (DPP-4) |  | 
        |  | 
        
        | Term 
 
        | Do incretin mimetics reduce fasting, postprandial glucose, or both? |  | Definition 
 | 
        |  | 
        
        | Term 
 | Definition 
 
        | Alpha-glucosidase inhibitor, brush border enzyme that hydrolyzes dietary carbohydrates, thus inhibiting the digestion of polysaccharides in the small intestine |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Alpha-glucosidase inhibitor, brush border enzyme that hydrolyzes dietary carbohydrates, thus inhibiting the digestion of polysaccharides in the small intestine |  | 
        |  | 
        
        | Term 
 
        | What are canagliflozin/dapagliflozin? |  | Definition 
 
        | SGLT2 inhibitor in the proximal tubule. Increase glucose excretion in the urine |  | 
        |  | 
        
        | Term 
 
        | How does bromocriptine help type 2 diabetics? |  | Definition 
 
        | Acts on the CNS to normalize the decreased AM dopamine secretions. Without dopamine, hepatic gluconeogenesis is increased, lipolysis/FFA are increased, and lipogenesis/TG are increased. |  | 
        |  | 
        
        | Term 
 
        | How does colesevelam help type 2 diabetics? |  | Definition 
 
        | Indirectly increase expression of GLP-1 by preventing absorption of bile acids. |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Synthetic amylin analogue useful in both type 1 AND 2 diabetics. It is normally co-secreted with insulin and reduces postprandial* glucose. |  | 
        |  | 
        
        | Term 
 | Definition 
 
        | Increase risk of severe hypoglycemia; insulin dose should be reduced by 50% |  | 
        |  | 
        
        | Term 
 
        | When should insulin be considered in type 2 diabetics? |  | Definition 
 
        | -decreased beta cell function -HbA1c > 8.5% (first line therapy is pts present with HbA1c > 10%)
 *use basal insulin therapy to lower FPG levels. If necessary, add rapid insulin to control postprandial glucose.
 *type 2 diabetics require more insulin compared to type 1
 |  | 
        |  | 
        
        | Term 
 
        | What is the least expensive/most common adjunct to metformin who glycemic goals are not met? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | What adjunct should not be added to metformin who glycemic goals are not met if a patient has an increased risk of CVD? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | What adjunct to metformin is good for overweight patients? |  | Definition 
 | 
        |  | 
        
        | Term 
 
        | What adjunct to metformin is good for patients with HbA1c >8.5%? |  | Definition 
 | 
        |  |