Pharm 6 Diabetes Flashcards

1
Q

2 methods of insulin secretion

A
  • Pulsatile pacemaker B cells open Ca channels

- Glucose through GLUT2 -> ATP -> block KIR channel -> Ca opens

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2
Q

Insulin molecule

A

A + B chain, C-peptide is cleaved

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3
Q

Insulin metabolism

A

50% degraded in liver, 50% in other target tissues

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4
Q

Insulin receptor MOA (GLUT4)

A

Tetramer

-Insulin binds to a-subunits -> b-subunits autophosphorylate -> tyrosine kinase

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5
Q

Insulin receptor MOA (mitogen)

A

MAP-kinase phosphorylation

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6
Q

Insulin in liver

A
  • Glycogen/triglyceride synthesis

- Inhibit glycogenolysis/gluconeogenesis

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7
Q

Insulin in fat

A
  • Glucose uptake, triglyceride storage

- Inhibit lipolysis

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8
Q

Insulin in general

A

Promote anabolism, inhibit catabolism

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9
Q

Insulin deficiency acidosis mechanism

A

Increase lipolysis -> ketoacids -> acidosis

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10
Q

Glucose intolerance with onset during pregnancy

A

GDM - Gestational Diabetes Mellitus

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11
Q

Instant type I diabetes cause

A

Total pancreatectomy

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12
Q

Drug therapy provoking chronic hyperglycemia

A

Steroid therapy

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13
Q

Rate limiting step for insulin absorption

A

Subcutaneous dissociation from hexamers into dimers and then monomers

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14
Q

-Lispro-

A

Lysine-Proline switched, can’t form aggregates

  • Ultra fast
  • Take after starting meal
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15
Q

-Aspart-

A

Proline replaced with aspartic acid, can’t form aggregates

-Ultra fast

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16
Q

-Insulin-

A

Can be given IV

-Fast

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17
Q

-NPH insulin-

A

Regular plus protamine zinc insulin (positively charged)

-Intermediate

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18
Q

-Glargine-

A

Ultra slow, peakless

-Single bedtime dose

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19
Q

-Determir-

A

Binds to albumin

-Ultra slow

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20
Q

Insulin pump benefit

A

Controls “dawn phenomenon”

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21
Q

Injection to accelerate insulin absorption

A
  • Intramuscular
  • Heat (exercise)
  • Abdomen or buttock (blood flow)
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22
Q

Compromised renal function effect on insulin

A

Reduced clearance, prolonged effectiveness

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23
Q

-Pramlintide-

A

Amylin analog

  • Slows postprandial glucose levels
    • Slow stomach, inhibit glucagon
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24
Q

-Pramlintide-
Contraindications
Adverse Effects

A
  • Gastroparesis

- Delayed onset of action of oral drugs

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25
-Exenatide- MOA indication
Incretin mimetic - Stimulate Insulin, inhibit Glucagon - Suppress postprandial hyperglycemia - From lizard
26
GLUT4 recruiting without insulin
5'AMP-K | -From exercise
27
Sulfonylurea MOA
Directly inhibit KIR -> Insulin secretion | -(normally inhibited by GLUT2 glucose)
28
2 Sulfonylurea drugs
Glipizide | Glyburide
29
Sulfonylurea binding site
SUR1 on inwardly-rectifying potassium channel
30
Sulfonylurea effect
Raise insulin secretion -> correct hyperglycemia - Increase insulin sensitivity - Improve B-cell responsiveness
31
Exenetide, Pramlintide main purpose
Suppress postprandial hyperglycemia
32
-Glipizide-
Fastish Sulfonylurea | -Bind KIR
33
-Glyburide-
Slower Sulfonylurea - Bind KIR - Doesn't cross placenta
34
Glipizide, Glyburide | -Preferred drugs for what
Renal dysfunction | -(2nd gen are fecal excretion)
35
Glipizide, Glyburide | -Bad drugs for what
Type I DM
36
Drug for pregnancy
Glyburide
37
Sulfonylurea Adverse effects
- Severe Hypoglycemia (overdose) | - Weight gain
38
Drug to use for surgery, severe infections, severe stress or trauma, severe hepatic or renal failure
Insulin ONLY
39
The Glinides
Repa and Nate
40
Repaglinide, Nateglinide class
Meglitinides
41
Repaglinide, Nateglinide MOA
Inhibit KIR, rapid insulin release
42
Repaglinide, Nateglinide indication
Tx postprandial hyperglycemia | -Reduced risk of long-lasting hypoglycemia
43
Biguanide drug
Metformin
44
-Metformin- good for
Rarely produces lactic acidosis
45
-Metformin- | MOA
Induces 5'AMPK - no effect on insulin - no hypoglycemia
46
-Metformin- | indication
Obese diabetics, prediabetics | -(weight loss, beneficial effect on lipids)
47
-Metformin- | also good for
Polycystic ovarian syndrome | -Hyperandrogenism insulin resistance
48
Thiazolidinedione drugs
Glitazone - Pioglitazone - Rosiglitazone
49
-Pioglitazone, Rosiglitazone- | MOA
PPARy ligand | -(peroxisome proliferator-activated receptor) nuclear hormone
50
-Pioglitazone, Rosiglitazone- | target genes
GLUT4 and GLUT1 increase | -Increase insulin sensitivity
51
-Rosiglitazone, Pioglitazone- | AE
Black Box for heart failure | -Rosiglitazone - angina, MI
52
-Acarbose, Miglitol- | MOA
a glucosidase inhibitors | -Delay carb digestion, absorption
53
-Acarbose, Miglitol- | administration
taken with first bite of meal
54
-SitaGLIPTIN, SaxaGLIPTIN- | MOA
DPP-4 inhibitors | -slow stomach emptying
55
-Diazoxide- | MOA
Hyperglycemic agent - opposite effect of sulfonylureas (KIR) - inhibits insulin release, not synthesis
56
Sulfonylurea drugs
Glipizide | Glyburide
57
-Diazoxide- | indication
Insulinomas
58
-Glucagon- | MOA
G-protein -> liver glycogenolysis, gluconeogenesis
59
-Glucagon- | indication
Severe hypoglycemia due to DM Tx
60
-Orlistat- | MOA
Inhibit GI lipases and TG hydrolysis | -inhibit fat absorption
61
-Pramlintine, Exenetide- | MOA
Slow gastric emptying