Drugs for Diabetes Konorev Flashcards

1
Q

What are the rapid acting Insulins?

A
  • Aspart
  • Lispro
  • Glulisine
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2
Q

Short acting insulins?

A

Regular insulin

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3
Q

Intermediate acting insulin

A

NPH

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4
Q

Long acting insulin

A

Detemir and Glargine

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5
Q

Insulin Secretagogues GLP-1 agonists?

A
  • Exenatide
  • Liraglutide
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6
Q

Insulin Secretagogues Dipeptidyl Peptidase 4 inhibitors?

A
  • Sitagliptin
  • Linagliptin
  • Saxagliptin
  • Alogliptin
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7
Q

First generation Katp channel blockers

A
  • Chlorpropamide
  • Tolbutamide
  • Tolazamide
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8
Q

Katp channel blocker Sulfonylurea Second gens?

A
  • Glipizide
  • Glyburide
  • Glimepride
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9
Q

Katp channel blockers Meglitinides?

A
  • Nateglinide
  • Repaglinide
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10
Q

Biguanides?

A

Metformin

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11
Q

Thiazolidinediones?

A

Pioglitazone and Rosiglitazone

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12
Q

SGLT2 inhibitors?

A
  • Canagliflozin
  • Dapagliflozin
  • Empagliflozin
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13
Q

Alpha glycosidase inhibitors?

A

Acarbose

Miglitol

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14
Q

What hormones increase blood glucose?

A
  • Glucagon
  • T3 and T4
  • Epinephrine
  • GLucocorticoids
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15
Q

Which of the following actions contributes to antihyperglycemic effect of insulin?

  • Activation of gluconeogenesis
  • Suppression of lgycolysis
  • Activation of glycogenolysis
  • Suppression of glucose transport into cells
  • Activation of glycogen synthesis
A
  • Activation of glycogen ssynthesis
  • rest incr. production of glucose
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16
Q

What does insulin do to gluconeogenesis and glycogenolysis?

A

Inhibits them

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17
Q

What are rapid acting insulins used for?

A

Postprandial hyperglycemia → taken before a meal as sc injections

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18
Q

What is short acting regular insulin used for?

A
  • basal insulin maintenance
  • overnight coverage
  • 45 minutes before a meal
  • Can be given IV in urgent situations
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19
Q

What is NPH?

A
  • complex of protamine with zinc insulin
  • used for basal insulin maintenance and or overnight coverage
  • use is declining being replaced by long acting insulins
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20
Q

What is Detemir?

A
  • long acting insulin rapidly absorbed into blood but binds strongly to albumin, allows slow release
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21
Q

What is Glargine?

A
  • long acting insulin made by changing amino acids iin both A and B chains, changing the pKa of insulin
  • used for basal insulin maintenance
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22
Q

What is an unexpected indication for insulin?

A
  • Severe hyperkalemia
    • Insulin + glu + furosemide
    • IV insulin activates Na/K ATPase to shift K from extracellular fluid into cells
    • K is then eliminated using loop diuretics
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23
Q

24 yo woman wants to tighten control of her diabetes to improve long term prognosis. Which regimen is most appropriate?

  • morning insulin injections mixed insulin lispro and insulin aspart
  • injections of mixed regular insulin and insulin glargine before bed
  • morning and evening injections of regular insulin supplemented by small amounts of NPH at meals
  • Morning injections of insulin glargine supplemented by insulin lispro at meal times
A
  • Morning injections of insulin glargine supplemented by insulin lispro at meal times
    • glargine is long acting used for basal coverage
    • lispro is rapid acting used for post prandiol control
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24
Q

what are the ways insulin can be delivered?

A
  • Standard by subQ injection with disposable needles
  • Portable pen injectors
  • Continuous subQ infusion devices
    • pumps
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25
Q

Adverse effect of Insulin?

A
  • Hypoglycemia
  • Lipodistrophy
  • Resistance
  • Allergic rxn
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26
Q

Most common complication of insulin therapy?

A
  • hypoglycemia
    • caued by delayed or missed meal
    • exercise
    • overdose
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27
Q

Signs of hypoglycemia? Tx?

A
  • Confusion, bizarre behavior seizure coma
  • tachycardia, palpitation, sweat, tremor
  • hunger nausea
  • Glucose or sucrose
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28
Q

Hypokalemia is a side effect of insulin that occurs due to?

  • inc. elimination of K in urine
  • inc. secretion of K in bile
  • inc. transport of K from ECF to cells
  • dec. absorption of K from GI tract
A
  • Inc. transport of K from extracell fluid into cells
29
Q

What is Amylin and its uses?

A
  • pancreatic hm made by beta cells
  • enhances action of insulin through
    • inhibiting glucagon
    • dec. gastric emptying → slows intestinal glucose absorption
    • causes feeling of satiety
30
Q

What is Pramlintide?

A
  • amylin analog drug
  • used in patients with absolute insulin deficiency
    • all type 1 and advanced type 2
  • inject before meals as adjunct to insulin therapy to control postprandial hyperglycemia
31
Q

Pramlintide AE? Drug interaction?

A
  • N/V, diarrhea, anorexia
  • severe hypoglycemia if used with insulin
  • enhances effects of anticholinergic drugs on GI tract → constipation
32
Q

Which of the following regarding Pramlintide as adjunct to insulin therapy is correct?

  • used primarily for T2DM patients
  • given orally
  • taken before bed
  • manage postprandial hyperglycemia
  • can cause hyperlgycemia
A

manage postprandial hyperglycemia

33
Q
A
34
Q
A

Isoproterenol a non selective Beta agonist

35
Q

How do incretin mimetics work?

A
  • activates GLP-1 receptor or boosts endogenous GLP-1 levels
36
Q

What are incretins? Example?

A
  • group of GI hormones that caue decrease in glucose levels
    • GLP-1:
      • promotes Beta cell proliferation and insulin gene expression
      • inhibits glucagon secretion
      • causing satiety and inhibits gastric emptying
      • NOT AN EFFECTIVE DRUG → very short half life
37
Q

What are two types of incretin mimetics?

A
  • Long acting GLP-1 receptor agonists
  • Dipeptidyl peptidase 4 inhibitors
38
Q

What are the long acting GLP1 agonsits?

A
  • Exenatide
    • AA subs make it less susceptible to hydrolysis of DPP4
    • 2.5 half life
  • Liraglutide
    • rapidly absorbed but binds albumin
    • half life 11-15 hrs
39
Q

Clinical use for GLP-1 receptor agonists?

A
  • Approved for T2DM patients who are not controlled by metformin/sulfonylurea/thiazolidinediones
  • other anti diabetic meds should be reduced to avoid hypoglycemia
40
Q

GLP-1 agonist AE’s?

A

n/v diarrhea anorexia

hypoglycemia

41
Q

What are the DPP 4 inhibitors?

A
  • “gliptins”
  • Sitagliptin
  • LInagliptin
  • Saxagliptin
  • Alogliptin
42
Q

DPP-4 MOA and indications??

A
  • Increase levels of GLP-1 to enhance its interactions with cognate receptor
  • given PO, as adjunct therapy to diet and exercise in those with T2DM
  • can be used monotherapy or combo with metformin/sulfonylurea/TZDs
43
Q

First gen vs second gen sulfonylureas?

A
44
Q

Katp channel blocker MOA?

A
  • Binds SUR1 blocking K current through an inwardly rectifying K channel
45
Q

Sulfonylureas use? AE’s?

A
  • T2DM as monotherapy or in combo with insulin or other anti diabetic drugs
  • Hypoglycemia
  • weight gain
  • secondary failure leading to hyperglycemia
46
Q

Sulfonylurea drug interactions?

A

Enhancing hypoglycemic effects:

  • Ethanol
  • Inhbits CYP enzymes: azoles, gemfibrozil, cimetidine
  • salicylates and other NSAIDs

Decrease glucose lowering effect:

  • inhibit insulin secretion → Beta blockers and CCBs
  • inducing hepatic CYP enzymes phenytoin griseofulvin rifampin
47
Q

Meglitinides? use? MOA?

A
  • Repaglinide and Nateglinide
  • Katp channel inhibition similar to sulfonylureas
  • use to control post prandial hyperglucemia T2
    • PO before meal
  • used alone or combo
48
Q
A
  • Glyburide and aspirin
49
Q

Metformin MOA?

A

Activation of AMP activated protein kinase

50
Q

Advantages to using Metformin?

A
  • Superior glu lowering efficacy compared to other oral meds
  • Doesn’t cause hypoglycemia or weight gain
  • oral
  • alone or combo use
  • dec risk of macro and microvascualr complications
51
Q

Pharmacokinetics meetformin?

A

Not bound to plasma proteins not metabolized, decreases drug interactions

52
Q

AE and contraindications of Metformin?

A
  • anorexia, n/v, diarrhea
  • lactic acidosis if renal and hepatic insufficiency
  • contraindicated in conditions predisposed to hypoxia
    • COPD, renal failure, alcoholism, cirrhosis
53
Q

What are the thiazolidinediones?

A
  • Pioglitazone and Rosiglitazone
  • Ligands of peroxisome proliferatior activated receptor gamma, a nuclear receptor expressed in fat, mm, liver and endothelium
    • increase glut4 in sk mm, adipocytes
    • dec PEPCK
54
Q

Pharmacokinetics of Thiazolidinediones?

A
  • orally once a day
  • delayed onset → 1-3 month and effects persist after drugs are eliminated
  • half life reduced by CPY inducing drugs such as rifampin
  • half life prolonged by CYP inhibitor ssuch as gemfibrosil
  • safe for patients with renal fialure
55
Q

TZD AE’s?

A
  • Weight gain
  • Edema:
    • incr vascular permeability
    • inc exprssion of ENaC increased sodium and water reabsorption in collecting duct
  • exacerbate heart failure
  • osteoporosis
56
Q

Which of the following is euglycemic?

  • insulin
  • glimepiride
  • pioglitazone
  • repaglinide
  • tolazamide
A
  • Pioglitazone
57
Q

Other effects of SGLT2?

A
  • osmotic diuresis
  • weight loss
  • dec BP
  • reeduce plasma uric acid
  • don’t cause hypoglycemia
58
Q

SGLT2 use?

A

T2DM in combo, orally before first meal

59
Q

SGLT2 AE’s?

A
  • hypotension
  • hypovolemia
    • orthostatic hypotension, dizziness, syncope
  • UTI
  • hypoglycemia if combined with insulin
60
Q

alpha glycosidase inhibitors?

A
  • competitive inhibition of alpha glycosidases
  • lowers postprandiol hyperglycemia to create an insulin sparing effect
  • Acarbose and Miglitol are the drugs
61
Q

alpha glycosidase inhibtor uses?

A
  • T2DM as monotherapy or combo
  • taken orally at meal time
  • no weight gain and no hypoglycemia when used alone
62
Q

Which stimulates insulin secretion by beta cells?

  • metformin
  • rosiglitazone
  • pramlintide
  • repaglinide
  • miglitol
A
  • repaglinide
63
Q

Which drugs can increase risk of hypoglycemia?

A
  • sulfonylurea (highest risk)
  • SGLT 2 Inhibitors (lower risk)
  • DPP4 inhibitors (lower risk)
64
Q

Which drugs cause increase in weight gain?

A

Sulfonylureas and TZD

65
Q

Which class of drugs causes weight loss

A

GLP 1 analogs

66
Q

Which classes can be used in CKD?

A

DPP4 inhibitors and TZD

67
Q

Which classes can be used in HF?

A
  • SUlfonylurea
  • SGLT2 inhibitors
  • GLP 1 analogs
68
Q

Contraindications for HF?

A

DPP4 and TZD

69
Q

COntrainidcations for CKD

A
  • Sulfonylurea
  • SGLT2
  • GLP1