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Pharmacology > Antidiabetics II > Flashcards

Antidiabetics II Flashcards

1
Q

Insulin Secretagogues

A

Sulfonylureas & Meglitinides

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2
Q

Sulfonylureas are effective at reducing ___ and ___

A

Sulfonylureas are effective at reducing fasting plasma glucose and HbA1C

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3
Q

Sulfonylureas bind to ____ subunit and block the ATP-sensitive ___ channel in the B cell membrane stimulating ___ release

A

Sulfonylureas bind to SUR1 subunit and block the ATP-sensitive K+ channel in the B cell membrane stimulating insulin release

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4
Q

sulfonylureas end in “__”

A

“ide”

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5
Q

1st generation Sulfonylurea

A

Chlorpropamide

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6
Q

Chlorpropamide has a ___ half life

AE’s?

A
  • Long half-life
  • Hypoglycemia, particularly in elderly
    • Contraindicated in elderly patients
  • Hyperemic flush with alcohol
    • d/t inhibition of aldehyde dehydrogenase
  • may potentiate vasopressin
    • ​elicit an apparent SIADH
    • ​hyponatremia
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7
Q

list 2nd generation Sulfonylureas

compare them to Chlorpropamide

A
  • Glyburide (Glibenclamide)
  • Glipizide
  • Glimepiride
  • much more potent than 1st gen drugs
  • lack some of the adverse effects and drug interactions of 1st gen drugs
  • replaced 1st gen drugs
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8
Q

compare hypoglycemic actions between 2nd gen sulfonylureas

A

Glimepiride < Glipizide < Glyburide

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9
Q

Sulfonylurea & Meglitinide AEs

A
  • Hypoglycemia
  • Weight gain
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10
Q

list Meglitinides

Glinides have the same MOA as ___

A
  • Repaglinide, Nateglinide
  • same MOA as Sulfonylureas
    • stimulate insulin release by binding to SUR1 and inhibiting ATP-sensitive K+ channel
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11
Q

Sulfonylureas vs. Meglitinides

  • effect
  • onset and duration of action
A

Sulfonylureas = more effective in reducing FPG and HbA1C levels

Meglitinides = more rapid onset and shorter DOA

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12
Q

Glinides are ____ glucose regulators.

Must be taken ____; if the meal is missed the drug must be omitted

A

Glinides are postprandial glucose regulators

Must be taken before each meal; if the meal is missed the drug must be omitted

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13
Q

Comparing the Meglitinides, ___ has a less risk of hypoglycemia than ___

A

Comparing the Meglitinides, Nateglinide has a less risk of hypoglycemia than Repaglinide

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14
Q

Biguanides

A

Metformin

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15
Q

Metformin does not cause ____

does not cause ___ (even in large doses)

___ efficacy to sulfonylureas in reducing FPG and HbA1C levels

A

Metformin does not cause insulin secretion

does not cause hypoglycemia (even in large doses)

Equal efficacy to sulfonylureas in reducing FPG and HbA1C levels

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16
Q

Metformin reduces glucose levels primarily by inhibiting ___ by reducing ____ of gluconeogenic enzymes

A

Metformin reduces glucose levels primarily by inhibiting gluconeogenesis by reducing gene expression of gluconeogenic enzymes

  • increases insulin-mediated glucose utilization in muscle and liver
  • As a result of the improvement in glycemic control, serum insulin concentrations decline slightly
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17
Q

Metformin actions are mediated by activation of ____

A

Metformin actions are mediated by activation of AMPK

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18
Q

other effects of metformin

A
  • Reduces plasma TG by 15-20%
  • weight LOSS

(sulfonylureas / glinides = weight gain)

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19
Q

1st line agent for treating T2 DM

A

Metformin

  • high insulin sensitivity
  • associated w/ weight loss
  • rarely causes hypoglycemia
  • does not depend on B-cells
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20
Q

Metformin AE and contraindications

A
  • Largely GI: anorexia, nausea, vomiting, abdominal discomfort, diarrhea
  • Long term use: B12 deficiency
  • Fatal lactic acidosis
  • Contraindicated: renal disease, hepatic disease, hypoxia, alcoholism
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21
Q

list the TZDs

A
  • Pioglitazone
  • Rosiglitazone
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22
Q

Pioglitazone and Rosiglitazone decrease insulin ____

___ agonist found in muscle, fat and liver

A

Pioglitazone and Rosiglitazone decrease insulin resistance

Peroxisome proliferator-activated receptor-y (PPAR-y) agonist found in muscle, fat and liver

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23
Q

Glitazones promote glucose uptake and utilization in adipose tissue by ___

__ effective than Sulfonylureas/Metformin in decreasing FPG and HbA1C

MOA involves ___

A

Glitazones promote glucose uptake and utilization in adipose tissue by increasing insulin sensitization

Less effective than Sulfonylureas/Metformin in decreasing FPG and HbA1C

MOA involves gene regulation

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24
Q

Glitazones have a slow onset and offset of activity taking ____

A

Glitazones have a slow onset and offset of activity taking weeks to months

25
Q

____ effects on lipids are more favourable than ___

associated with significant improvements in:

A

pioglitazone effects on lipids are more favourable than rosiglitazone

pioglitazone is associated with significant improvements in: HDL, TG, LDL particle concentration, LDL particle size

26
Q

TZD AE’s

A
  • fluid retention, weight gain, edema
  • cause or exacerbate CHF
  • contraindicated: Class III or IV heart failure
  • Troglitazone: 1st TZD approved, caused severe hepatotoxicity → withdrawn
    • FDA requires monitoring of liver function with TZD
    • so far pioglitazone or rosiglitazone have not been associated with hepatotoxicity
27
Q

a-Glucosidase Inhibitors

A

Acarbose

28
Q

Acarbose: MOA

A
  • competitive inhibitor of intestinal a-glucosidases
  • reduces postprandial digestion of starch and disaccharides
  • minimizes upper intestinal carb absorption and defers absorption to distal SI
    • decreases postprandial hyperglycemia and hyperinsulinemia
  • modest drop in HbA1C and FPG levels
29
Q

Acarbose AEs

A
  • Flatulence, diarrhea, abdominal pain
  • Contraindicated in IBS or any intestinal condition worsened by gas and distension
  • associated with reversible hepatic enzyme elevation
  • Periodical liver function monitoring is required with acarbose therapy
30
Q

Incretin Analog: ____

DDP-4 inhibitor: ____

both ___ insulin secretion

A

GLP-1 analog: Exenatide

DDP-4 inhibitor: Sitagliptin (oral)

both increase insulin secretion

31
Q

Incretin secretion & action on the B cell

A
32
Q

Exenatide effects

A
  • Resistant to dipeptidyl peptidase IV (DPP-IV)
  • increases insulin secretion
  • Suppresses postprandial glucagon release
  • Slows gastric emptying
  • Decreases appetite
  • May stimulate β-cell proliferation
33
Q

Exenatide and Sitagliptin AEs

A
  • Both: Pancreatitis
  • Exenatide
    • GI: Nausea, vomiting and diarrhea
    • not used in patients w/ gastroparesis
  • Sitagliptin
    • urticaria, angioedema, anaphylaxis, skin reactions (Stevens-Johnson syndrome)
34
Q

Amylin Analog

A
  • Pramlintide
  • Peptide co-secreted with insulin from pancreatic β-cells
  • Inhibits food intake, gastric emptying, and glucagon secretion
35
Q

Bile-acid Sequestrants and Use

A

Colesevelam

used to lower LDL cholesterol

Approved for treatment of type 2 DM

Mechanism unclear.

Given orally

36
Q

SGLT2 Inhibitor

A
  • “-Gliflozin” (canagliflozin)
  • blocked SGLT2 leads to decreased glucose reabsorption in proximal tubule, increased glucose excretion, and decreased blood glucose levels
  • Given orally
37
Q

-gliflozin AE

A
  • Increased risk of genital and urinary tract infections
  • osmotic diuresis: volume depletion, increased serum creatinine levels, hyperkalemia, hypermagnesemia, hyperphosphatemia and hypotension
  • Contraindicated in patients with renal insufficiency
38
Q
A
39
Q
A
40
Q

INITIAL DRUG THERAPY FOR T2 DM

____ is the preferred first agent if lifestyle intervention does not achieve HbA1c goals

A

INITIAL DRUG THERAPY FOR T2 DM

Metformin is the preferred first agent if lifestyle intervention does not achieve HbA1c goals

41
Q

Patients with HbA1c ≥9.0% are unlikely to achieve HbA1c goals with ____

what do we give them?

A

Patients with HbA1c ≥9.0% are unlikely to achieve HbA1c goals with monotherapy

combination of 2 noninsulin agents or with insulin itself

42
Q

If monotherapy does not achieve HbA1C goal over∼3 months, the next step is to add a second agent:

A

oral agent, exenatide or insulin (the higher the HbA1C, the more likely insulin will be required)

43
Q

If 2-drug combination fails to achieve the glycemic target a third agent can be added - many patients will eventually need to be on ___

when HbA1c ≥ 8.5% we should transition to ___

A

If 2-drug combination fails to achieve the glycemic target a third agent can be added - many patients will eventually need to be on insulin

when HbA1c ≥ 8.5% we should transition to insulin

44
Q

Describe Insulin Therapy

A
  1. Begins with a single low dose injection of basal insulin
    • NPH, Glargine, Detemir
  2. Dose is then uptitrated
  3. If there is postprandial hyperglycemia, add prandial insulin
    • lispro, aspart, glulisine
45
Q

___ is the most effective of diabetes medications in lowering glycemia

A

Insulin is the most effective of diabetes medications in lowering glycemia

  • decreases any level of elevated HbA1C to therapeutic goal
  • no maximum dose of insulin beyond which a therapeutic effect will not occur
  • Large doses of insulin may be necessary to overcome the insulin resistance of type 2 diabetes
46
Q

when is insulin warranted as initial therapy for patients with type 2 diabetes?

A
  • severe hyperglycemia
    • Significant hyperglycemic symptoms
    • Ketonuria
    • HbA1c > 10%
    • random glucose > 300 mg/dL
47
Q

what is the preferred drug for Gestational DM?

A

Insulin (does not cross the placenta)

  • start with a single dose of bedtime NPH insulin
  • If postprandial glucose control is required injections of lispro or aspart can be added
48
Q

which insulin drugs should not be given in Pregnancy

A

Glulisine, Glargine, Degludec (Category C)

49
Q

DM + HTN should be given:

A

ACEi (pril) or ARB (sartan)

50
Q

what should be monitored in a patient on an ACEi?

A

K+ and creatinine

51
Q

DM + Dyslipidemia should be given…

Potential AE of this drug?

A

Statins

AE: AST/ALT elevations, rhabdomyolysis

  • With overt CVD
  • Aged < 40 yr with CVD risk factors
  • Aged > 40 yr with or without CVD risk factors
52
Q

DM + increased CV risk should be given…

A

Aspirin (antiplatelet agent) - 1° prevention strategy

53
Q

DM + Albuminuria patients should be given….

A

ACE inhibitors or ARBs

54
Q

Drugs used for neuropathic pain

A
  • Imipramine
  • Amitriptyline
  • Pregabalin
  • Gabapentin
  • Duloxetine
  • Venlafaxine
  • Valproate
  • Opioids
55
Q

Diabetic gastroparesis (2)

A

Metoclopramide or Erythromycin (prokinetic agents)

Potential AE of Metoclopramide: Parkinsonism

56
Q

Contraindicated in a patient with gastroparesis?

A

Exenatide, Sitagliptin, Pramlintide

57
Q

DM neuropathy + erectile dysfunction

A

Phosphodiesterase-5 inhibitor: Sildenafil

58
Q

____ is used to treat severe hypoglycemia in diabetic patients treated with insulin

A

Glucagon is used to treat severe hypoglycemia in diabetic patients treated with insulin

Also used for:

  • Radiology of bowel (relaxes intestine)
  • B-blocker overdose
  • Glucagon C-peptide Test (tests for residual β-cell function in diabetes)

Pharmacology (19 decks)

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