VI - Topnotch Pharma Flash Cards - Endocrine Drugs
Recombinant Growth hormone
Somatropin (TOPNOTCH)
Increases release of IGF-1 in the liver and carilage, stimulates skeletal muscle growth, amino acid transport, protein synthesis and cell proliferation
Somatropin (TOPNOTCH)
Recombinant IGF-1
Mecasermin (TOPNOTCH)
Somatostatin analog
Octreotide, Lanreotide (TOPNOTCH)
suppresses the release of growth hormones, glucagon, insulin, gastrin, IGF-1, serotonin and gastrointestinal peptides
Octreotide, Lanreotide (TOPNOTCH)
For Acromegaly, pituitary adenoma, carcinoid, gastrinoma, glucagonoma, variceal bleeding
Octreotide, Lanreotide (TOPNOTCH)
GH receptor antagonist ; For acromegaly
Pegvisomant (TOPNOTCH)
Gonadotropin analog (FSH analog) ; For Controlled ovarian hyperstimulation, infertility due to hypogonadism in men
Follitropin alfa, Follitropin beta, Urofollitropin (TOPNOTCH)
Gonadotropin analog (LH analog)
For Controlled ovarian hyperstimulation (ovulation induction), hypogonadotripic hypogonadism (TOPNOTCH)
SE: Headache, depression, edema, ovarian hyperstimulation syndrome, multiple pregnancies in women, gynecomastia in men
FHS and LH analogs (TOPNOTCH)
GnRH analog
Leuprolide, Gonadorelin, Goserelin, Histrelin, Nafarelin, Triptorelin (TOPNOTCH)
For Controlled ovarian hyperstimulation, endometriosis, myoma uteri, precocious puberty, postate CA
Leuprolide, Gonadorelin, Goserelin, Histrelin, Nafarelin, Triptorelin (TOPNOTCH)
there is exacerbation of symptoms in males with prostate CA and children with precocious puberty during the first few weeks of therapy
GnRH analog (TOPNOTCH)
For GnRH analogs: increased LH and FSH secretion with ________ administration , reduced LH and FSH secretion with ________ administration
intermittent ; prolonged continuous (TOPNOTCH)
GnRH antagonist
Ganirelix, Cetrorelix, Degarelix (TOPNOTCH)
For Controlled ovarian hyperstimulation (prevents premature LH surge), advanced prostate CA
Ganirelix, Cetrorelix, Degarelix (TOPNOTCH)
Does NOT cause tumor flare-up whe used for treatment of advanced prostate cancer
Ganirelix, Cetrorelix, Degarelix (TOPNOTCH)
_____ is used for prostate CA while _____ prevent LH surge in controlled ovulation
Degarelix ; Ganirelix (TOPNOTCH)
Dopamine agonist, partial agonist at dopamine D2 receptors in brain ; For Hyperprolactinemia, Pituitary adenoma, acromegaly, Parkinson’s disease
Bromocriptine, Carbegoline (TOPNOTCH)
Activates oxytocin receptors stimulates uterine contraction and labor, stimulates mammary glands, lactation and milk let-down
Oxytocin (TOPNOTCH)
For Labor induction, labor augmentation, control of uterine hemorrhage post-delivery
Oxytocin (TOPNOTCH)
oxytocin antagonist used in preterm labor
ATOSIBAN (TOPNOTCH)
ADH agonist, Vasopressin V2 receptor agonist
Desmopressin (TOPNOTCH)
For Central DI, Hemphilia A, von Willebrand’s disease, Variceal bleeding, primary nocturnal seizures
Desmopressin (TOPNOTCH)
SE: Fetal distress, placental abruption, uterine rupture, fluid retention, hyponatremia, heart failure, seizures, hypotension
Oxytocin (TOPNOTCH)
ADH antagonist, Antagonist at V1a and V2 receptors
Conivaptan, Tolvaptan (TOPNOTCH)
_____ may occur with rapid correction of hyponatremia
Central pontine myelinolysis (TOPNOTCH)
Which is more selective for V2 receptors, Conivaptan or Tolvaptan?
tolvaptan (TOPNOTCH)
Thryoid hormone ; For Hypothyroidism, myxedema coma
Levothyroxine (T4), Liothyronine (T3) (TOPNOTCH)
T or F: Liothyronine has a faster onset but shorter half-life
TRUE (TOPNOTCH)
Inhibits thyroid peroxidase reactions, blocks iodine organification, inhibits peripheral conversion of T4 into T3
Propylthiouracil (PTU) (TOPNOTCH)
Drug of choice for pregnant hyperthyroid patients
Propylthiouracil (PTU) (TOPNOTCH)
Inhibits thyroid peroxidase reactions, blocks iodine organification
Methimazole, Carbimazole (TOPNOTCH)
Inhibit iodine organification and hormone release leading to reduced size and vascularity of thyroid gland
Lugol Solution (Iodine in Potssium Iodide), Potassium Iodide (TOPNOTCH)
onset is more rapid (2-7 days) but effect is transient ; Should not be used alone (escape in 2-8 weeks); prevents radiation induced thryoid damage; prenatal exposure causes fetal goiter
Lugol Solution (Iodine in Potssium Iodide), Potassium Iodide (TOPNOTCH)
Beta blocker control HR and other cardiac abnormalities of severe thyrotoxicosis, slows pacemaker activity; inhibits peripheral conversion of T4 into T3
Propranolol, Esmolol, Metoprolol, Atenolol (TOPNOTCH)
_____ may be used to treat thyrotoxicosis-related arrhythmias
Esmolol (TOPNOTCH)
Iodide, emits beta rays causing destruction of thyroid parenchyma
Radioactive Iodine (TOPNOTCH)
For hyperthyroidism, permanent cure of thyrotoxicosis without surgery and no effect on other tissues
Radioactive Iodine (TOPNOTCH)
Preferred treatment for most patients due to ease of administration, effectiveness, low expense and absence of pain; contraindicated in pregnant women or nursing mothers
Radioactive Iodine (TOPNOTCH)
Low Potency Glucocorticoid (GC)
Desonide (TOPNOTCH)
Medium Potency GC
Fluticasone, Mometasone (TOPNOTCH)
High Potency GC
Desoximetasone, Clobetasol (TOPNOTCH)
Effects: stimulate gluconeogenesis, increased fat deposition, protein catabolism, inhibit cell-mediated immunologic functions, lymphotoxic, increased neutrophils, decreased lymphocytes, eosinpphils, basophils and monocytes, inhibit leukocyte migration, inhibit PLA2
Glucocorticoids (TOPNOTCH)
_____ is the active metabolite of prednisone
prednisolone (TOPNOTCH)
SE: Adrenal suppression, growth inhibition, muscle wasting, osteoporosis, salt retention, glucose intolerance, behavioral changes (psychosis)
Glucocorticoids (TOPNOTCH)
For supressession of inflammation and immune response, hematopoeitic cancers, transplant rejection, collagen and rheumatic disease, lung maturation in preterm labor
Glucocorticoids (TOPNOTCH)
strong agonist of mineralocorticoid receptors and moderate activation of glucorticoid receptors
Mineralocorticoid (TOPNOTCH)
Increases Na reabsorption, K and H excretion ; For Chronic adrenal insufficiency (Addison’s disease), Congenital adrenal hyperplasia, adrenal replacement therapy post-adrenalectomy
Mineralocorticoid (TOPNOTCH)
Mineralocorticoid
Fludrocortisone, Deoxycorticosterone (TOPNOTCH)
Additive hypokalemia with loop diurectics and thiazides
Fludrocortisone, Deoxycorticosterone (TOPNOTCH)
Glucorticoid synthesis inhibitor, inhibits desmolase activity, blocking conversion of cholesterol to pregnenolone
Aminoglutethimide (TOPNOTCH)
Glucorticoid synthesis inhibitor, inhibits cholesterol side chain cleavage, cytochrome P450 enzymes and other enzymes necessary for synthesis of all steroids
Ketoconazole (TOPNOTCH)
Ketoconazole is CYP450 inhibitor or inducer?
Inhibitor (TOPNOTCH)
Glucorticoid synthesis inhibitor, selective inhibitor of steroid-11 hydroxylation
Metyrapone (TOPNOTCH)
DOC for pregnant patients with Cushing’s syndrome
Metyrapone (TOPNOTCH)
competitive inhibitor at the GC receptor as well as progesterone receptor ; For Cushing’s syndrome
Mifepristone (RU486) (TOPNOTCH)
also used as an approved abortifacient for medical abortion (usually together with misoprostol)
Mifepristone (RU486) (TOPNOTCH)
Activates etrogen receptors, leads to changes in rates of trasncription of estrogen-regulated genes
Estrogens: Ethinyl Estradiol, Mestranol, Estradiol cypionate, Premarin (TOPNOTCH)
Synthetic estrogen (nonsteroid); activates estrogen receptors; leads to changes in rates of transcription of estrogen-regulated genes ; For Atrophic vaginitis, hormone replacement therapy, prevention of adverse pregnancy outcomes, metastatic prostate CA
Diethylstilbestrol (TOPNOTCH)
associated with Infertility, ectopic pregnancy, clear cell vaginal adenocarcinoma in daughters of women who used this drug
Diethylstilbestrol (TOPNOTCH)
activates progesterone receptors, change rates of transcription of progesterone-regulated genes ; For Hormone replacement therapy, contraception, assisted reproduction, anovulation induction
Progestins: Norgestrel, Medroxyprogesterone, Norethindrone, Norgestimate, Desogestrel,Megestrol (TOPNOTCH)
IM depot preparation
Medroxyprogesterone Acetate (TOPNOTCH)
Must be taken within 72 hours of unprotected sexual intercourse
Levonorgestrel (TOPNOTCH)
Estrogen antagonist actions in breast tissue and CNS, Estrogen agonist effects in uterus, liver and bone
Tamoxifen, Torimefene (TOPNOTCH)
Estrogen antagonist actions in breast tissue, uterus, and CNS, Estrogen agonist effects in liver and bone
Raloxifene (TOPNOTCH)
Partial agonist in pituitary, reduces negative feedback by estradiol, increases FSH and LH output, For Induction of ovulation
Clomiphene (TOPNOTCH)
Reduces estrogen synthesisby inhibiting aromatase ; For breast CA, precocious puberty
Anastrozole, Letrozole, Exemestane (TOPNOTCH)
Ovarian inhibitor, weak cytochrome P450 inhibitor and partial agonist of progestin and androgen receptors ; For Endometriosis, Fibrocystic disease, Hemophilia, Angioneurotic edema
Danazol (TOPNOTCH)
Activates androgen receptors, promotes development of male characteristics, increases body muscle bulk and RBC production
Androgens: Testosterone, Fluoxymesterone, Methyltestosterone (TOPNOTCH)
Effects: induces secretory changes in the endometrium, stabilize the endometrium, affect carbohydrate metabolism and stimulate deposition of fat, high doses suppress FSH and LH secretion
progesterone (TOPNOTCH)
Effects: secondary sexual characteristics, fertility and libido, male pattern baldness, increases muscle mass, increased RBC production, decreased urea nitrogen excretion
Androgens: Testosterone, Fluoxymesterone, Methyltestosterone (TOPNOTCH)
anabolic steroids
Oxandrolone, Stanozolol, Nandrolone (TOPNOTCH)
Competitive antagonist at androgen receptor ; For Prostate CA, surgical castration
Flutamide, Bicalutamide, Nilutamide (TOPNOTCH)
Antagonist at androgen receptor. Marked progestational effect that suppresses the feedback enhancement of LH and FSH
Cyproterone (TOPNOTCH)
Androgen synthesis inhibitor, inhibits 5a reducase enzyme that converts testosterone to dihydrotestosterone ; For BPH, Male pattern baldness. Hirsutism
Finasteride, Dutasteride (TOPNOTCH)
Activates a Tyrosine Kinase typer of receptorsleading to a reducting of circulating glucose: promotes glucose transport and oxidation; glycogen, lipid, protein synthesis and regulation of gene expression
Insulin (TOPNOTCH)
Rapid Acting Insulin
Lispro, Aspart, Glulisine (TOPNOTCH)
Short Acting Insulin
Regular Insulin (TOPNOTCH)
Intermediate Acting Insulin
NPH, Lente (TOPNOTCH)
Long Acting Insulin
Detemir, Glargine, Ultralente, Lantus (TOPNOTCH)
peakless insulins
Long Acting Insulin (TOPNOTCH)
acts as an insulin secretagogue, increases insulin secretion from pancreatic beta cells by closing ATP sensitive K+ channels leading to depolarization of the B cell
Sulfonylureas (TOPNOTCH)
2nd generation sulfonylurea
Glipizide, Glibenclamide, Glimepiride, Gliclazide, Glyburide (TOPNOTCH)
1st generation sulfonylurea
Tolazamide, Tolbutamide, Chlorpropamide (TOPNOTCH)
T or F: 1st gen SUs have less hypoglycemia than 2nd gen
FALSE (TOPNOTCH)
Insulin Secretagogue, similar to sulfonylureas with some overlap in binding sites, reduces circulating glucose, increases glycogen, fat and protein formation and gene regulation
Meglitinides (TOPNOTCH)
Meglitinides
Repaglinide, Nateglinide (TOPNOTCH)
Least hypoglycemia among OHAs
Meglitinides (TOPNOTCH)
Reduced hepatic and renal gluconeogenesis with decreased endogenous glucose production, activates AMP-stimulated protein kinase leading to inhibition of gluconeogenesis
Biguanides (TOPNOTCH)
Biguanides
Metformin (TOPNOTCH)
DOC for obese diabetics
Metformin (TOPNOTCH)
Inhibits intestinal alpha-glucosidases , reduces conversion of starch and disacchardies to monosaccharidea, reduces post prandial hyperglycemia
Alpha Glucosidase Inhibitors (TOPNOTCH)
Alpha Glucosidase Inhibitors
Acarbose, Miglitol (TOPNOTCH)
Regulates gene expression by binding to PPAR-gamma and PPAR-alpha which increases tissue sensitivity, increases glucose uptake in muscle and adipose tissue, inhibits hepatic gluconeogenesis, effects on lipid metabolism and distribution of body fat, control of fasting and postprandial glucose, decreased risk of DM in high-risk patients
Thiazolidinediones (TOPNOTCH)
Thiazolidinediones
Pioglitazone, Rosiglitazone (TOPNOTCH)
binds to PPAR-gamma and PPAR-alpha
Pioglitazone (TOPNOTCH)
binds to PPAR-gamma ONLY
Rosiglitazone (TOPNOTCH)
SE: Fluid retention, weight gain, congestive heart failure, fractures esp in women, cardiovascular events, hepatotoxicity, macular edema, dyslipidemia, increased risk of MI
Thiazolidinediones (TOPNOTCH)
Analog of GLP-1, Binds to GLP-1 receptors which leads to reducetion of post-meal glucose excursions, increases glucose-mediated insulin release, lowers glucagon levels, slows gastric emptying time, produces satiety
Exenatide (TOPNOTCH)
Dipeptidyl Peptidase-4 Inhibitors, blocks degradation of GLP-1, raises circulating GLP-1 levels, reduces post-meal glucose excursions, increases glucose mediated insulin release, lowers glucagon levels, slows gastric emptying time, decreases appetite
Sitagliptin, Linagliptin (TOPNOTCH)
Analog of amylin, Binds to amylin receptors, reduce post-meal glucose excursions, lowers glucagon levels, slows gastric emptying, decreases appetite
Pramlintide (TOPNOTCH)
Bile acid binder, lowers glucose through unknown mechanisms
Colesevelam hydrochloride (TOPNOTCH)
INACTIVE Vitamin D
Cholecalciferol, Ergocalciferol (TOPNOTCH)
ACTIVE Vitamin D
Calcitriol, Doxercalciferol, Paricalcitol, Calcipotriene (TOPNOTCH)
Suppress the activity of osteoclasts in part via inhibition of farnesyl pyrophosphate synthesis, inhibit resorption and formation of bone by acting on the basic hydroxyapatite crystal structure
Bisphosphonates (TOPNOTCH)
Bisphosphonates
Alendronate, Risedronate, Ibandronate, Pamidronate, Zoledronate, Etidronate, Tiludronate, Zoledronic acid (TOPNOTCH)
Recombinant PTH, Acts via cognate G protein coupled receptors, stimulates bone formation when given in low intermittent doses
Teriparatide (TOPNOTCH)
Acts via cognate G protein coupled receptors; suppresses bone resorption ; For Paget’s disease of the bone, hypercalcemia, osteoporosis, tumor marker for thyroid CA
Calcitonin (TOPNOTCH)
Interacts selectively with estrogen receptors, inhibits PTH-stimulated bone resorption without stimulating breast or endometrial hyperplasia, delay bone loss in post-menopausal women
Raloxifene (TOPNOTCH)
Monoclonal antibody, binds to RANKL and prevents it from stimulating osteoclast differentiation and function, blocks bone resorption
Denosumab (TOPNOTCH)
Activates the calcium sensing receptors in the parathyroid gland, inhibits PTH secretion
Calcium Receptor Antagonist: Cinacalcet (TOPNOTCH)