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Endo Dynamics Exam 1
| Question | Answer |
|---|---|
| What is the brand name of Epoetin? | Epogen (EPO) |
| What type of molecule is Epoetin? | Recombinant Human Protein |
| What is the MOA of Epoetin? | Erythropoietin Receptor Activation |
| What is the most common use of Epoetin? Dosing? | Increase Erythrocyte Count (given 3 x week s.c.) |
| What is the brand name of Darbepoetin? | Aranesp |
| What type of molecule is Epoetin? | Glycosylated Engineered Protein |
| What is the MOA of Darbepoetin? | Erythropoietin Receptor Activation |
| What is the most common use of Darbepoetin? Dosing? | Increase Erythrocyte Count (given weekly s.c.) |
| What is the brand name of Methoxy-Polyethylene Glycol Epoetin Beta? | Micera |
| What type of molecule is Methoxy-Polyethylene Glycol Epoetin Beta? | Pegylated protein |
| What is the MOA of Methoxy-Polyethylene Glycol Epoetin Beta? | Erythropoietin Receptor Activation |
| What is the most common use of Methoxy-Polyethylene Glycol Epoetin Beta? Dosing? | Increase Erythrocyte Count (given monthly or every 2 weeks s.c.) |
| What is the brand name of Peginesatide? | Omontys |
| What type of molecule is Peginesatide? | Synthetic, Pegylated, Dimeric Peptide |
| What is the MOA of Peginesatide? | Erythropoietin Receptor Activation |
| What is the most common use of Peginesatide? Dosing? | Increase Erythrocyte Count (given monthly s.c) --> Discontinued 2019 |
| Regarding pharmacokinetics, what is different about Peginesatide from the other erythropoietin receptor activators? | Not Metabolized |
| What is the brand name of Sargramostim? | Leukine |
| What type of molecule is Sargramostim? | Recombinant Human Glycoprotein |
| What is the MOA of Sargramostim? | GM-CSF Receptor Activation |
| What is the most common use of Sargramostim? Dosing? | Stimulates Progenitor Cells to Differentiate into Neutrophils, Monocytes, and Macrophages (given iv over 4 or 24 hours depending on indication or s.c. once daily) |
| What is the brand name of Filgrastim? | Neupogen |
| What type of molecule is Filgrastim? | Recombinant Human Protein |
| What is the MOA of Filgrastim? | G-CSF receptor activation |
| What is the most common use of Filgrastim? | Increase Neutrophil Count |
| What is the brand name of Pegfilgrastim? | Neulasta |
| What type of molecule is Pegfilgrastim? | Pegylated Recombinant Human Protein |
| What is the MOA of Pegfilgrastim? | G-CSF receptor activation |
| What is the most common use of Pegfilgrastim? | Increase Neutrophil Count |
| What is the brand name of Romiplostim? | Nplate |
| What type of molecule is Romiplostim? | Fc-peptide fusion protein (peptibody) |
| What is the MOA of Romiplostim? | Thrombopoietin Receptor Activation |
| What is the most common use of Romiplostim? Dosing? | Increases Platelet Count (once weekly) |
| Romiplostim and Eltrombopag are both thrombopoietin receptor activators, however, only Eltrombopag carries a black box warning. What is the black box warning for Eltrombopag? | Risk of hepatic decompensation (acute liver failure) in patients with chronic hepatitis and risk of hepatotoxicity |
| What is the brand name of Eltrombopag? | Promacta |
| What type of molecule is Eltrombopag? | Small Organic Molecule |
| What is the MOA of Eltrombopag? | Thrombopoietin Receptor Activation |
| What is the most common use of Eltrombopag? Dosing? | Increases platelet count (given po daily) |
| Erythropoiesis stimulating agents, such as Epoetin and Darbepoetin, carry a black box warning. What is the black box warning? | Myocardial Infarction; Stroke; Venous Thrombosis; Tumor Progression or Recurrence |
| Changes (increase or decrease) in __________ lack behind dosage changes by __________ due to __________ and __________. | hematocrit; 2-6 weeks; the time needed for erythropoiesis; erythrocyte half-life |
| Do Sargramostim, Filgrastim, and Pegfilgrastim have a black box warning? | No |
| What is another name for Iron (II)? How is Iron (II) given? | Ferrous Iron (2+); given orally |
| How is Iron (II) intake related to absorption? | Absorption into circulation is not proportional to oral intake |
| What is another name for Iron (III)? How is Iron (III) given? | Ferric Iron (Fe3+); given IV |
| When would Iron (III) be given? | When oral iron supplements are not tolerated |
| What is Deferoxamine used to treat? | Chronic iron overload or acute iron poisonings |
| What is the MOA of Deferoxamine? | Binds tightly to iron and blocks its oxidation properties |
| What is the most common use of oral Vitamin B12? | Nutritional vitamin B12 deficiency |
| What is the most common use of Vitamin B12 injection or nasal spray? | Vitamin B12 deficiency secondary to intrinsic factor deficiency or poor vitamin B12 absorption in the GI tract |
| Vitamin B12 contains a porphyrin ring contain what metal? | Cobalt |
| What is Vitamin B12 used for in the body? | Coenzyme needed for DNA synthesis and thus for cell replication |
| What is another name for folic acid? | Folacin |
| What is the most common use of folic acid? | Reduces risk of neuronal tube defects |
| What is folic acid used for in the body? | Needed for amino acid metabolism, DNA synthesis and cell replication |
| What is Pernicious Anemia? | Deficiency of gastric intrinsic factors leading to vitamin B12 deficiency even if the diet provides enough vitamin B12 |
| What is another name for Vitamin D2? | Ergocalciferol |
| How is Ergocalciferol (Vitamin D2) produced? | From ergosterol found in plants and fungi when they are exposed to UV radiation; obtained by humans through diet or foods enriched with |
| How is another name for Vitamin D3? | Cholecalciferol |
| How is Cholecalciferol (Vitamin D3) produced? | formed when 7-dehydrocholesterol, a form of pre-vitamin D3 in animal skins is stimulated by UV radiation; obtained by humans through eating animal products |
| What is the active form of Vitamin D called? | Calcitriol 1,25(OH)2D3 |
| When taking Vitamin D, what other serum concentrations will change? | Increased Calcium & Phosphate |
| What is the brand name of Teriparatide? | Forteo |
| What type of molecule is Teriparatide and Abaloparatide? | Recombinant DNA peptide |
| What is the MOA of Teriparatide and Abaloparatide? | Binds to the PTH receptor leading to G-protein coupled signaling |
| What is the brand name of Abaloparatide? | Tymlos |
| What are Teriparatide and Abaloparatide use to treat? How? | Osteoporosis; Increase Serum Calcium |
| What is the brand name of Calcitonin? | Miacalcin |
| What type of molecule is Calcitonin? | Synthetic human peptide or animal derived sequence (SALMON) |
| What is the MOA of Calcitonin? | Binds CT receptor leading to G-protein coupled signaling |
| What is Calcitonin used to treat? How? | Osteoporosis, Hypercalcemia; Decrease Serum Calcium and Phosphate |
| What is the brand name of Anti-FGF23 (burosumab-twza)? | Crysvita |
| What is Anti-FGF23 used to treat? | Hypophosphatemia caused by a genetic defect that causes increased FGF23 activity |
| What is the black box warning for Teriparatide and Abaloparatide? | Increase in osteosarcoma due to the intracellular cellular signaling initiated by PTH (increased serum calcium does not cause cancer) |
| What is the brand name of Alendronate? | Fosamax |
| What drug class is Alendronate part of? | Biphosphonates |
| What is the MOA of Alendronate? | Reduce osteoclast activity by inhibiting farnesyl pyrophosphate synthesis which reduces bone resorption (movement of calcium to circulation) |
| What is Alendronate used to treat? | Osteoporosis; Paget Disease |
| What is the brand name of Raloxifene? | Evista |
| What drug class is Raloxifene part of? | SERMs |
| What is the MOA of Raloxifene? | Binds estrogen receptors which reduces bone resorption (movement of calcium to circulation) without bread or endometrial cancer risk |
| What is Raloxifene used to treat? | Osteoporosis |
| What is the MOA of Denosumab? | Binds RANKL and blocks activation of RANK which reduces bone resorption (movement of calcium to circulation) |
| What is Denosumab used to treat? | Osteoporosis from bone-related cancers |
| What is the MOA of Romosozumab? | Binds sclerotin stimulating bone deposition |
| What is Romosozumab used to treat? | Osteoporosis |
| What happens when a patient takes Abaloparatide? | Serum Ca2+ goes up |
| What can be the effect of no skin exposure to sun light? | Low calcitriol |
| Formation of calcitriol involves which organs? | Skin, Liver, Kidney |
| How is intrinsic factor related to Vitamin B12? | Intrinsic factor is needed for B12 uptake |
| Define Type I Diabetes. | Beta-cell destruction, progressive, usually leading to absolute insulin deficiency |
| Define Type II Diabetes. | May range from predominantly insulin resistant with relative insulin deficiency to a predominantly secretory defect with insulin resistance |
| Define Type IV Diabetes. | Gestational Diabetes Mellitus |
| What is considered a normal fasting plasma glucose? | less than 100 mg/dL |
| What is considered a normal blood glucose following an oral glucose tolerance test? | less than 140 mg/dL |
| What is considered a normal A1C? | less than 5.7% |
| What is considered a diabetic A1C? | greater than or equal to 6.5% |
| What does A1C measure? | long-term (3 month) average measure of glucose control |
| Where is insulin produced? | Beta-Cells of the Islets of Langerhans |
| Where is glucagon produced? | Alpha-Cells of the Islets of Langerhans |
| What does insulin do? | decreases blood glucose levels |
| What does glucagon do? | increases blood glucose levels |
| What does somatostatin do to insulin and glucagon? | suppresses insulin and glucagon secretion |
| What does somatostatin do to the pituitary gland? | inhibits the pituitary gland's secretion of growth hormone and thyroid stimulating hormone |
| What organs take up glucose independently of insulin? | Brain and red blood cells (greatest affinity); pancreas, liver, kidney, gut, placenta |
| What tissues are dependent on insulin stimulation? Which glucose transporter? | muscle and adipose tissue; GLUT4 |
| What glucose transporter is insulin dependent? | GLUT4 |
| Which glucose transporter has the greatest affinity? | GLUT1 |
| What are the two gastrointestinal incretin hormones? How do they affect insulin? | GLP-1 and GIP are potent inducers of insulin secretion from the pancreas |
| What is the non-pharmacological treatment of hyperinsulinemia? | Lifestyle changes (food & exercise) |
| What is the brand name of diazoxide? | Proglycem |
| What is the MOA of diazoxide? | keeps ATP-dependent K-channel open, preventing hyperpolarization of the cell which would trigger Ca2+ influx and insulin release --> PREVENTS INSULIN RELEASE |
| What is the brand name of Octreotide? | Sandostatin |
| What is the MOA of Octreotide? | Somatostatin receptor agonist that alters the balance between insulin, glucagon, and growth hormone secretion --> LOWERS INSULIN SECRETION |
| What is the brand name of Nifedipine? | Procardia; Adalat |
| What is the MOA of Nifedipine? | Block Ca2+ influx and thus block subsequent exocytosis of insulin loaded vesicles --> Monitor for HYPERglycemia |
| Example(s) of Biguanides drug class. | Metformin |
| What drug class does Metformin belong to? | Biguanides |
| What is the MOA of Metformin? | reduction of gluconeogenesis in the liver |
| Does Metformin cause hypoglycemia? | anti-hyperglycemic, not hypoglycemic; has little effect in normoglycemic persons |
| What is the most common first line treatment of Type II Diabetes? | Metformin |
| What is the brand name of Metformin? | Glucophage |
| What are the Black Box Warnings for Metformin? | Lactic Acidosis; can also cause vitamin B12 deficiency or hypoglycemia with concomitant use of insulin and insulin secretagogues |
| Example(s) of Sulfonylurea drug class. | First Generation (Not Commonly Used Anymore): Tolbutamide, Tolazamide, Chlorpropamide Second Generation: Glyburide, Glipizide, Glimpiride |
| Second generation Sulfonylureas are _____ times more potent than first generation. | 100 |
| What is the brand name of Glyburide? | Micronase; Diabeta |
| What is the brand name of Glipizide? | Glucotrol |
| What is the brand name of Glimepiride? | Amaryl |
| What is the MOA of Sulfonylureas? | Binds to SUR1 and blocks ATP-sensitive K-channel in beta-cells causing depolarization, followed by Ca2+ influx and insulin release --> INCREASES RELEASE OF INSULIN |
| What is the binding site of Sulfonylureas and Meglitinides? | SUR1 |
| Do Sulfonylureas cause hypoglycemia? | Hypoglycemic reactions including coma are possible |
| Can Glipizide, a Sulfonylurea, be used during pregnancy? | Cannot be used during pregnancy or lactation (drug class C) |
| Example(s) of Meglitinides (Glinides) drug class. | Repaglinide; Nateglinide |
| What is the brand name of Repaglinide? | Prandin |
| What is the brand name of Nateglinide? | Starlix |
| Meglitinides have the same binding site as Sulfonylureas but do not have a urea or sulfonyl chemical group, meaning, a patient with an _________ to Sulfonylureas could take a Meglitinide. | allergy |
| Do Meglitinides cause hypoglycemia? | yes, however, the risk is lower with Nateglinide (Starlix) than other secretagogues |
| The drug class Thiazolidinediones are also called what? | Glitazones or TZDs |
| Example(s) of Thiazolidinediones drug class. | Pioglitazone; Rosiglitazone |
| What is the brand name of Pioglitazone? | Actos |
| What is the brand name of Rosiglitazone? | Avandia |
| What is the MOA of Thiazolidinediones? | selective agonists for PPAR gamma (nuclear peroxisome proliferator-activated receptor-gamma) |
| What is the major site of action for Thiazolidinediones? | adipose tissue |
| Thiazolidinediones require __________ to be present for their action. | insulin --> act as insulin boosters |
| Pioglitazone and Rosiglitazone, both Thiazolidinediones, can take how long to become effective? | 6-12 weeks |
| What is the Black Box Warning for Pioglitazone? | Congestive Heart Failure |
| Example(s) of DPP-4 Inhibitors. | Sitagliptin; Saxagliptin; Linagliptin; Alogliptin |
| What is the MOA of DPP-4 Inhibitors? | Block DPP-4 enzyme which is responsible for inactivating incretins (GLP-1/GIP), thereby increasing the available amount of incretins |
| What is the brand name of Sitagliptin? | Januvia |
| Example(s) of Alpha-Glucosidase Inhibitors. | Acarbose; Miglitol |
| What is the brand name of Acarbose? | Precose |
| What is the brand name of Miglitol? | Glyset |
| What is the MOA of Acarbose and Miglitol? | reduce activity of intestinal alpha-glucosidases (predominantly glucoamylase and sucrase), which break down starch, dextrin and sucrose, |
| Example(s) of SGLT2 Inhibitors? | Canaglifozin; Dapagliflozin; Empagliflozin |
| What is the brand name of Canaglifozin? | Invokana |
| What is the brand name of Dapagliflozin: | Farxiga |
| What is the brand name of Empagliflozin? | Jardiance |
| What is the MOA of SGLT2 inhibitors? | located in the proximal part of the renal tubule, it is a high affinity, low capacity transporter for glucose and when inhibited more glucose is allowed to pass into the urine --> lowers blood glucose concentrations |
| What is a common adverse effect of SGLT2 inhibitors? | Urinary tract infections due to the increase glucose concentration in the urine |
| Example(s) of Bile Acid Sequestrant. | Colesevelam |
| What is the brand name of Colesevelam? | Welchol |
| What is the MOA of Colesevelam? | no clearly defined molecular structure with high binding affinity for bile acid molecules; mechanism for lowering glucose is not understood |
| Example(s) of Dopamine Receptor Agonist. | Bromocriptine mesylate |
| What is the brand name of Bromocriptine Mesylate? | Cycloset |
| What is the MOA of Bromocriptine Mesylate? | Unknown, does not increase plasma insulin concentrations |
| What is the brand name of Dulaglutide? | Trulicity |
| What is the brand name of Exenatide? | Byetta & Byduron (Extended Release) |
| What is the brand name of Liraglutide? | Victoza |
| What is the brand name of injectable Semaglutide? | Ozempic |
| What is the brand name of oral Semaglutide? | Rybelsus |
| What is the brand name of Albiglutide? | Tanzeum |
| What is the brand name of Lixisenatide? | Adlyxin |
| Which two GLP1 drugs do not carry a boxed warning? What is the boxed warning for all other GLP1 drugs and GIP drugs? | Exenatide (Byetta Only) & Lixisenatide (Adlyxin); the boxed warning for all other GLP1 drugs is may cause Thyroid C-Cell Tumor |
| What is the brand name of Tirzepatide? | Mounjaro |
| What is the brand name of Pramlintide? | Symlin |
| What is the brand name of Glucagon? | GlucaGen |
| What is the Black Box Warning for Pramlintide? | Severe Hypoglycemia |
| What is the MOA of Pramlintide? | amylin analog; lowers postprandial blood glucose, moderates appetite, delays gastric emptying, suppresses glucagon release |
| Example(s) of short-acting insulin. | Regular Insulin (Humulin R; Novolin R) |
| Example(s) of rapid acting inhaled insulin. | Afrezza |
| What is the Black Box Warning for Afrezza? | Bronchospasm |
| Example(s) of rapid acting insulin. | Insulin Aspart; Insulin Glulisine; Insulin Lispro |
| What is the brand name of Insulin Aspart? | Novolog; Flexpen; Fiasp |
| What is the brand name of Insulin Glulisine? | Apidra |
| What is the brand name of Insulin Lispro? | Humalog |
| Example(s) of intermediate-acting insulin. | Insulin Isophane (NPH Insulin); Humulin N, Novolin N |
| Example(s) of long-acting insulin? | Insulin Degludec; Insulin Detemir; Insulin Glargine --> Insulin DDG |
| What is the brand name of Insulin Degludec? | Tresiba |
| What is the brand name of Insulin Detemir? | Levemir |
| What is the brand name of Insulin Glargine? | Lantus; Toujeo |
| What is the most common adverse reaction of insulin therapy? | Hypoglycemia |
| What is the therapeutic use of glucagon? | to treat hypoglycemia |
| Which diabetes drug classes have a risk of hypoglycemia? | Sulfonylureas (Moderate to Severe); Meglitinides (Mild); Insulin (Moderate to Severe) |
| Which diabetes drug classes show weight loss? | Metformin (Slight Loss); GLP1 (Loss); SGLT2 (Loss); Pramlintide (Loss) |
| Which diabetes drug classes show weight gain? | TZDs (Gain); Sulfonylureas (Gain); Meglitinides (Gain); Insulin (Gain) |
| What are common side effects of DPP-4 inhibitors? | Severe Joint Pain; Pancreatitis |
| What medication is the most effective at lower A1C and the most cost effective? | Metformin |
| Are diabetes combination drugs additive or synergistic? | Synergistic |
| What is basal insulin? In a Type I Diabetic what percentage of TDD should be basal insulin? | controls glucose production between meals and overnight, near constant levels; 40-50% TDD |
| What is bolus insulin? In a Type I Diabetic what percentage of TDD should be bolus insulin? | limits hyperglycemia after meals, immediate rise and sharp peak at 1 hour post-meal; 60-50% TDD |
| What oral diabetes medications could "possibly" be used in pregnancy? | Metformin, Glyburide or Sitagliptin |
| What injectable diabetes medications are recommended during pregnancy? | Regular insulin, NPH and Insulin Lispro |
| What oral diabetes medication cross the placenta? | Metformin & Glyburide |
| Does injectable insulin cross the placenta? | No |
| What is the indication for Teplizumab-mzwv (TZIELD)? | to delay onset of stage 3 T1D in adults and children older than 8 years with stage 2 T1D |
| What is the MOA of Teplizumab-mzwv? | deactivation of pancreatic beta cell auto reactive T lymphocytes - extend beta cell destruction |
| A patient is diagnosed with auto-antibodies against intrinsic factor but has no signs of anemia. How should the patient be treated? | Injections of vitamin B12 |
| Nitrogen containing biphosphonates differ from biphosphonates that do not contain a nitrogen in what way? | N-containing biphosphonates are more potent |
| Deferoxamine is used to treat what acute condition? | Accidental iron poisoning; High serum iron concentrations |
| Vitamin D3 is hydroxylated in two separate enzymatic steps to form calcitriol. These biochemical reactions occur in which organs? | Liver and Kidney |
| True or False. ACTOS is a PPAR-gamma antagonist. | False. Actos is a PPAR-gamma agonist. |
| What is the molecular target of Invokana? | SGLT2 |
| True or False. Alendronate is usually administered by weekly s.c. injections. | False. Given po. |
| True or False. Diazoxide can be used to treat pre-diabetes. | False. Diazoxide is used to treat hyperinsulinemia by keeping ATP-dependent K-channel open, preventing hyperpolarization of the cell which would trigger Ca2+ influx and insulin release --> PREVENTS INSULIN RELEASE |
| The molecular target of diazoxide is? | ATP-dependent K-channel |
| Does a drug combination of Sulfonylurea and Meglitinides make sense? | No, they have the same MOA. Meglitinides can be used in patients with sulfonyl or urea allergies. |
| What is the binding site of Sulfonylureas and Meglitinides? | SUR1 |
| What is the molecular target of Sulfonylureas? | ATP-dependent potassium channel |
| Sulfonylureas are used in Type _____ diabetes. | II (2) |
| Example(s) of GLP1 analogs. | Exenatide, Lixisenatide, Liraglutide, Dulaglutide, Albiglutide, Semaglutide (ELLDAS) |
| What modification was made to the GLP1 analog Exenatide? Half-life? | Altered sequence; 2.4 hours |
| What modification was made to the GLP1 analog Lixisenatide? Half-life? | Altered sequence with poly-Lys tail; 3 hours |
| What modification was made to the GLP1 analog Dulaglutide? Half-life? | N-terminal fusion to Fc-fragment; 5 days |
| What modification was made to the GLP1 analog Albiglutide? Half-life? | Minor sequence change + fusion to ALBumin; 5 days |
| What modification was made to the GLP1 analog Liraglutide? Half-life? | Altered sequence + C16 acylation (lipid tail); 13 hours |
| What modification was made to the GLP1 analog Semaglutide? Half-life? | Altered sequence + hydrophobic space + C18 acylation (lipid tail); 1 week |
| Explain in a single sentence why metformin should be used carefully by nursing mothers. | Metformin is secreted into breast milk. |
| Explain in a few words the molecular mechanism of diabetes medications in the sulfonylurea drug class. | Sulfonylurea diabetes drugs bind to the ATP-dependent potassium channel in pancreatic beta-cells and favor the closed state of the channel. |
| Explain in a few words the molecular mechanism of WELCHOL (Colesevelam) as a diabetes medication. | The mechanism by which WELCHOL leads to a reduction in A1c is unknown. |
| Explain in a few words why the therapeutic use of insulin can lead to body weight gain. | Insulin enhances the up-take of blood glucose into fat tissues. In adipocytes (fat cells) the glucose is converted into fat and stored as such. |
| Explain in a few words why the therapeutic use of SGLT2 inhibitors can lead to body weight loss. | SGLT2 inhibitor drugs result in glucose elimination from the body. Thus, the glucose that entered the blood stream is partially lost in the urine and only a fraction can be stored as fat. |
| Which physiological stimulus triggers an increase in serum GLP1? | food intake; a meal |
| The activity of GLUT4 is regulated by insulin. Name two tissues that express GLUT4. | muscle and fat tissue |
| Describe the effect of diazoxide binding to the ATP-dependent potassium channel in pancreatic beta-cells. | Diazoxide keeps the potassium channel preferentially in the open state. Thus, the membrane potential is maintained, the calcium channel doesn't open as much and less insulin is released. |
| What is the route of administration of Miacalcin? | Nasal spray; Miacalcin is salmon calcitonin |
| What condition is Miacalcin used to treat? | Hypercalcemia; Osteoporosis; Paget Disease |
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