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86 Cards in this Set
- Front
- Back
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MOA of Benzimidazoles |
Binds free tubulin and inhibits tubulin polymerization |
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The only Benzimidazole in the US |
Albendazole (Albenza) |
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Indications for Albendazole |
cysticercosis and neurocysticercosis (tapeworm) |
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Metabolism of Albendazole |
Hepatically metabolized to albendazole sulfoxide (active) |
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Brand name for Ivermectin |
Stromectol |
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Indications for Ivermectin |
Head lice, scabies, and other infections including Stronglyloides stercoralis (roundworm) and intestinal nematodes |
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Describe the MOA and dosing for Ivermectin |
Binds to glutamate gated chloride channels which increases permeability of chloride to enter the cells which causes hyperpolarization of nerve and muscle cells of the parasite. Paralysis and death results.
Oral (single dose) and topical |
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Adverse effects of Ivermectin |
Generally well tolerated since it is a single dose. Mazzotti type reaction- HA, dizziness, weakness due to inflammatory or allergic responses to dying microfilariae. |
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MOA of Praziquantel |
Increases permeability of parasite cell membrane to calcium which causes strong contraction and paralysis of the worm. There is detachment of suckers from the blood vessel walls and dislodgement of the parasite.
Schistosoma and fluke infections. |
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Brand name for Praziquantel |
Biltricide |
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Brand name for Iodoquinol |
Yodoxin |
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Use for Iodoquinol |
Used to treat amebiasis (amoebic dysentery) |
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Adverse effects of Iodoquinol |
Optic atrophy leading to blindness
Enlarged thyroid (iodines in structure) |
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Adverse effects of Paromomycin (Humatin) |
Aminoglycoside antibiotic effective against amebiasis
Oral administration with GI side effects |
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3 Rapid Acting Insulins |
Lispro (Humalog) Aspart (Novolog) Glulisine (Apidra) |
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Brand name of short acting (regular) insulin |
Humulin R and Novolin R |
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Intermediate acting insulin (NPH) |
Humulin N and Novolin N |
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2 Long Acting Insulins |
Glargine (Lantus) Detemir (Levemir) |
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List the routes of administration for regular insulin |
IV, IM, SQ 30-60 minutes before a meal |
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Explain the metabolism of regular insulin |
Metabolized by the liver and kidney by insulin protease |
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Pharmacokinetics for regular insulin |
Onset: 1/2-1 hours Peak: 2-3 hours Duration: 4-6 hours |
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Adverse effects of regular insulin |
hypoglycemia |
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Interaction of regular insulin |
Enhanced hypoglycemia: thiazides and beta-blockers
Decreased hypoglycemia: loop diuretics and systemic steroids |
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What effect does adding protamine and zinc to insulin preparations have? |
Increases the duration of action |
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Describe the route of administration and pharmacokinetics of NPH insulin |
Administered subcutaneously
Onset: 2-4 hours Peak: 4-8 hours Duration: 18-28 hours |
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Structural modification of Lispro (Humalog) |
B28 (Pro > Lys) B29 (Lys > Pro)
"Lys-Pro" |
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Structural modification of Aspart (Novolog) |
B28 (Pro > Aspartic Acid) |
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Structural modification of Glulisine (Apidra) |
B3 (Asp > Lys) B29 (Lys > Glutamic Acid) |
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How are rapid acting insulins administered? |
Subcutaneous |
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Pharmacokinetics of rapid acting insulins |
Onset: 5-15 min Peak: 45-75 min Duration: 2-4 hours |
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Structural modification of Glargine (Lantus) |
A21 (Asp > Glycine) 2 Arginines are added to C-terminus of the B chain |
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Structural modification of Detemir (Levemir) |
Myristic acid is covalently bound to lysine at B29 B30 threonine is missing Fatty acid acylation enhances affinity to albumin allowing for delayed absorption |
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Pharmacokinetics of Glargine (Lantus) |
Onset: 2 hours Peak: n/a Duration: 22-24 hours |
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Pharmacokinetics of Detemir (Levemir) |
Onset: 2 hours Peak: n/a Duration: 6-24 hours (dose dependent) |
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2 classes of insulin secretagogues |
Sulfonylureas Meglitinides |
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MOA of sulfonylureas |
Receptors are part of the ATP dependent channels in pancreatic beta cells. The channels close, which alters the resting potential of the cell. Calcium influx causes stimulation of insulin secretion from the cell. |
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1st generation sulfonylureas |
chlorpropamide (24-72 hours) tolbutamide (14-16 hours) |
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2nd generation sulfonylureas |
Glipizide (Glucotrol) Glyburide (DiaBeta, Glynase PresTab, Micronase) Glimepiride (Amaryl) |
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Explain the dosing differences between the 1st and 2nd generation sulfonylureas |
2nd generation sulfonylureas can be given at lower doses |
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Uses of sulfonylureas |
Monotherapy or combination with other hypoglycemic drugs or insulin
Lower blood glucose levels by ~20% and A1C by 1-2% |
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Metabolism of chlorpropamide |
CYP2C9 |
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Metabolism of tolbutamide |
CYP2C9 to an active and inactive metabolite |
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Metabolism of glipizide |
CYP2C9 to inactive metabolites |
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Metabolism of glyburide |
hepatic |
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Metabolism of glimepiride |
CYP2C9 |
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Elimination of sulfonylureas |
Urine
Glyburide and Glimepiride (Urine & Feces) |
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Adverse effects of sulfonylureas |
usually well tolerated
hypoglycemia
AE more common with long acting sulfonylureas
Nausea, skin reactions, abnormal liver function tests
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MOA meglitinides |
Regulates ATP dependent potassium channels in beta-cells to increase insulin secretion |
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Brand and generic of meglitinides |
Repaglinide (Prandin) Nateglinide (Starlix)
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Adverse effects of meglitinides |
Hypoglycemia |
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Uses for meglitinides |
Type 2 DM as monotherapy or combination with metformin |
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Metabolism of meglitinides |
Repaglinide: CYP3A4 Nateglinide: CYP2C9 and CYP3A4 |
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Elimination of meglitinides |
Repaglinide: feces Nateglinide: urine
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MOA of biguanides |
Inhibits gluconeogenesis decreasing hepatic glucose production (accumulates in the liver cell and inhibits mitochondrial respiratory chain complex) Decreases intestinal absorption of glucose Increases peripheral glucose uptake (improves insulin sensitivity) |
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Adverse effects of biguanides |
Severe diarrhea |
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One biguanide available in the US |
Metformin |
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Uses of Metformin |
Type 2 DM can be used in patients who are obese and/or insulin resistant; can result in weight loss
Monotherapy or in combination |
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Metabolism of Metformin |
No metabolism |
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Elimination of Metformin |
Kidneys |
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MOA of thiazolidinediones |
Enhance action of insulin at target tissue (administered with insulin). Binds to PPAR gamma, a transcription factor. This results in gene expression to result in increased FA uptake and storage in adipose tissue instead of skeletal muscle or the liver. The decrease in muscle and liver fat content enables tissues to be more sensitive to insulin and glucose production in liver is suppressed. |
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2 thiazolidinediones currently available in the US |
Rosiglitazone (Avandia) Pioglitazone (Actos) |
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Metabolism of thiazolidinediones |
CYP2C8 (Pioglitazone has active metabolites) |
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Elimination of thiazolidinediones |
Urine and feces |
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Adverse effects of thiazolidinediones |
Weight gain, fluid retention, heart failure, risk of bone fracture |
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Uses of thiazolidinediones |
Combination therapy with sulfonylurea, metformin, or insulin
Monotherapy |
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MOA of alpha-glucosidase inhibitors |
Inhibits the upper GI enzymes and the small intestines (alpha-glucosidases) that convert complex polysaccharides into monosaccharides in a dose dependent fashion. These drugs slow the absorption of glucose and delay carbohydrate digestion.
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2 alpha-glucosidase inhibitors |
Acarbose (Precose) Miglitol (Glyset) |
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Metabolism of alpha-glucosidase inhibitors |
Acarbose metabolized by the intestinal bacteria and digestive enzymes
Miglitol is not metabolized |
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Elimination of alpha-glucosidase inhibitors |
Urine |
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Adverse effects of alpha-glucosidase inhibitors |
No effect on weight, GI effects (gas, flatulence), hypoglycemia does not occur even with overdosing |
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MOA of amylin mimetic |
Co-secreted with insulin: affects glucose control, slows gastric emptying, regulates postprandial glucose, reduce food intake, inhibits inappropriate glucagon secretion, slows gastric emptying, promotes satiety (does not cause weight gain), suppresses the abnormal postprandial rise of glucose |
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Brand and generic of amylin mimetic |
Pramlintide (Symlin, SymlinPen) |
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Explain the use of Pramlintide |
Type I and insulin treated Type II DM |
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Adverse effects of Pramlintide |
Nausea, hypoglycemia (dose low and titrate up; drop insulin dose ~50%) |
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Interactions of Pramlintide |
Slows gastric emptying and may delay the rate of absorption of oral medications
CI: patients with gastroparesis should not use drug |
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List the indications for DPP-IV inhibitors |
Not for Type I DM Not initial therapy with Type 2 DM Monotherapy in patients intolerant or have CI to other drugs such as metformin, sulfonylureas, or thiazolidinediones Add on therapy for patients inadequately controlled by metformin, sulfonylureas, or thiazolidinediones |
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MOA of DPP-IV inhibitors |
Increases incretin hormones (GIP, GLP-1), which stimulate insulin release in response to meals |
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Explain why DPP-IV inhibitors are a good therapeutic target in terms of its function |
Involved in glucose-dependent stimulation of insulin secretion, reduction of gastric emptying, reduction of inappropriate glucagon secretion |
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Brand and generic names of DPP-IV inhibitors |
Sitagliptin (Januvia) Saxagliptin (Onglyza) Linagliptin (Tradjenta) Alogliptin (Nesina) |
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Adverse effects of DPP-IV inhibitors |
Hypoglycemia, HA, nasopharyngitis, upper respiratory infection, pancreatitis |
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Explain the function of GLP-1 proteins |
Involved in glucose-dependent stimulation of insulin secretion Reduction of gastric emptying Reduction of inappropriate glucagon secretion Weight loss (reduce food intake; decreases appetite) |
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GLP-1 like proteins (Brand and Generic) |
Exenatide (Bydureon) Liraglutide (Victoza) |
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Adverse effects of GLP-1 like proteins |
GI (nausea) Hypoglycemia when given with a sulfonylurea Acute renal failure Pancreatitis Black Box Warning: Thyroid C cell tumors (CI in patients with family history of thyroid tumors) |
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Modification to the structure of liraglutide that extends its 1/2 life |
Modified with a lipid side chain allowing it to bind to albumin. Results in slower degradation and once-daily dosing. |
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Adverse effects of liraglutide |
Nausea, vomiting, diarrhea, pancreatitis, small risk of hypoglycemia, significant weight loss (Do NOT use during pregnancy!) |
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Benefits of liraglutide |
Monotherapy as an adjunct to diet and exercise or in combination with oral agents in adults with Type 2 DM Not a first line drug Relatively stable against DPP IV inhibitors |
