Anti-Diabetic Agents Flashcards

1
Q

alpha secretes:

A

glucagon

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2
Q

beta secretes:

A

insulin and amylin

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3
Q

delta secretes:

A

somatostatin

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4
Q

G-cell secretes:

A

gastrin

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5
Q

F-cell secretes:

A

pancreatic polypeptide

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6
Q

Insulin

  • type of hormone?
  • process to make?
A
  • peptide hormone

- made as pre-pro-inslin –> cleaved to pro-insulin –> maturation that cleaves C-peptide leaving just insulin

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7
Q

*positive regulation of insulin release:

A
  • glucose (substrate)
  • amino acids (substrate)
  • incretins (hormones)
  • Epi/Beta2 stim (hormone)
  • vagus stim (neuronal)
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8
Q

*Negative regulation of insulin release:

A
  • NE/alpha2 stim (neuronal)

- amylin (hormone feedback)

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9
Q

Insulin secretion is dependent on? Process?

A
  • Calcium - vesicles and docking and stuff
  • ATP sensitive K channel closes when ratio of ATP/ADP is high bc of high glucose levels=making ATP –> depolarization –> CA influx)
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10
Q

Insulin receptor and effect on cell upon binding:

A

bunch of stuff but upreg of GLUT4 transporter on membrane (MUSCLE AND ADIPOSE TISSUE)

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11
Q

GLUT4 is on what tissue? regulated by what?

A

Muscle and adipose - insulin mediated uptake of glucose

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12
Q

Insulin effects on Liver, muscle and adipose.

A

1) liver = mediates storage of glucose as glycogen (NOT HEPATIC UPTAKE OF GLUCOSE)
2) adipose= stimulates uptake of glucose (GLUT4)
- uptake and conversion of fatty acids into storage triglycerides
3) Muscle=stimulates uptake of glucose (GLUT4)
- uptake and storage of amino acids into proteins

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13
Q

Type 1 Diabetes

A
  • insulin-dependent diabetes mellitus
  • juvenile-onset
  • 1a=immune mediated (most)
  • 1b=idiopathic

-beta cell destruction = absolute deficiency

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14
Q

Type 2 diabetes

A
  • adult-onset
  • non-insulin dependent diabetes
  • resistance to insulin and then get insulin secretory deficiency (body tries to inc insulin production to keep up with sugar levels)

-obesity/genetics/nutrition/physical activity

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15
Q

Gestational diabetes

A
  • glucose intolerance in 2nd or 3rd trimester
  • 4% get this
  • return to normal immediately post delivery
  • 40% who get will develop diabetes in next 10 years
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16
Q

type 1 diabetes - signs and symptoms:

A

1) polyuria/nocturnal enuresis- osmotic diuresis:loss of glucose, electrolytes and water
2) Thirst- hyperosmolar state
3) blurred vision-hyperosmolar state
4) WL/polyphagia
- acute=depletion of water, glycogen, triglyc stores
- chronic=loss of muscle mass as amino acids are used for gucose and ketone bodies
5) Weakness/Dizziness-postural hypertension, potassium loss and muscle catabolism
6) Paresthesias - temporary Periph sensory nerve dysf
7) level of consciousness - depends on level of hyperosmolarity
- slow insulin def = minimal signs but fast deficiency shows fruity breath, ketoacidosis, dehydration, coma,…

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17
Q

Type 2 diabetes- signs and symptoms

A

1) asymptomatic initially
2) infections - glucose available as E source for microorganisms - skin and candidal vag
3) neuropathy - retinopathy and peripheral neuropathy
4) classic severe insulin deficiency signs - polyuria,thrirst, blurred vision, fatigue, weakness
5) obesity & metabolic syndrome - dyslipidemia, HTN, CAD

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18
Q

Fasting blood glucose levels should be around?

A

100mg/dL

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19
Q

insulin therapy is required for whcih diabetes?

A
  • type 1

- also used for type2 with declining insulin production/secretion

20
Q

Whats the point of synthetic insulins pharmakokinetics wise?

A

We change around a few amino acids of the sequence = different kinetics = how much the insulin sticks to itself (determines length of action)

21
Q

Rapid acting insulin drugs & duration*

A
  • insulin lispro
  • insulin aspart
  • insulin glulisine
  • inhaled insulin

-3-5 hrs

22
Q

short acting insulin drugs & duration*

A
  • regular insulin

- 4-12 hrs

23
Q

Intermediate acting insulin drugs & duration*

A
  • NPH

- 10-20hrs

24
Q

Long acting insulin drugs & duration*

A
  • insulin Glargine 12-20 hrs

- insulin detemir 22-24hrs

25
Q

Rapid acting insulin-

  • key feature
  • peak period?
A
  • amino acid alteration in C-terminal tail of the B peptide preventing insulin complex formation
  • peak=30min-3hrs
  • insulin lispro
  • insulin aspart
  • insulin glulisine
  • inhaled insulin
26
Q

Short-acting insulin-

  • key feature
  • peak period?
A
  • identical to human insulin

- peak=2.5-5hrs

27
Q

Intermediate acting insulin

  • key feature
  • peak period?
A
  • protamine-insulin complex

- peak=4-8hrs

28
Q

Long acting insulin

  • key feature
  • peak period?
A

-amino acid subs that result in PPT formation at neutral pH

  • insulin Glargine 12-20 hrs PEAK=flat
  • insulin detemir 22-24hrs PEAK=NONE
29
Q

insulin pumps use which insulin?

A

short acting - the pump is constantly infusing some insulin

30
Q

Adverse effect of insulin therapy:

A
  • hypoglycemia**
  • hypersensitiviy-rare-immune response to non-insulin protein contaminants
  • resistance-rare - antiinsulin antibodies
  • lipohypertrophy-fat deposition at injection site
  • lipoatrophy-fat loss at injection site
31
Q

If diabetic get hypoglycemia and is conscious vs unconscious?

A
conscious=food, sugar tablet
unconscious=glucose or glucagon
32
Q

symptoms of hypoglycemia

A
  • tachycardia
  • sweating
  • tremors
  • nausea
  • hungry
  • neurologic symptoms (irritability, confusion, headache, speech difficulty…)
33
Q

Glucagon

  • type?
  • MOA?
  • administration?
  • AE?
A
  • peptide
  • catabolism of stored glycogen
  • subcu injection
  • safe- nausea, vomit
34
Q

Metformin

  • type?
  • MOA
  • AE?
  • benefit to use?
A

1) biguanides
2) -decrease hepatic glucose output
- inc peripheral glucose use
- activation of hepatic enzyme AMP-activated protein kinase (AMPK)
3) GI issues
- Vit b12 deficiency
4) no hypoglycemia

35
Q

first line oral antidiabetic agent for type 2 diabetic

A

metformin

36
Q

Which oral anti-diabetic drug is not dependent on beta cell fucntion

A

metformin

37
Q

Sulfonylureas - name the drugs?

A

oral antidiabetic drugs

  • glimepiride
  • glipizide
  • glyburide
38
Q

Meglitinide-name the drugs?

A

oral antidiabetic drugs

  • repaglinide
  • nateglinide
39
Q

Sulfonylureas and meglitinides

  • MOA?
  • AE?
A
  • oral antidiabetic drug
  • inh ATP-sensitive potassium channel of beta cell=insulin release
  • weight gain
  • hypoglycemia
40
Q

Glucosidase inh -

  • name the drugs?
  • MOA?
  • AE?
A
  • oral antidiabetic drug
  • acarbose and miglitol
  • inh brush border glucosidase enzyme = no absorptio of glucose
  • abdominal pain, diarrhea, flatulence bc unabs carbs
41
Q

COntraindications for glucosides inh?

A

acarbose and miglitol

-not ok for people with GI disease

42
Q

Thiazolidinediones (TZDs)

  • drugs?
  • MOA?
  • AE?
A

-oral antidiabetic drug
-pioglitazone - rosiglitazone
-dec perpheral resistance by activating peroxisome proliferator activated receptor gamme
-effect on glucose metabolism and insulin signaling
AE=periph edema; weight gain; hep tox; bone fractures; hypoglycemia; cardiovascular

43
Q

Thiazolidineddones - contracindications?

A

people with heart problems

44
Q

Prmlintide

  • type?
  • MOA?
  • admin?
  • AE?
A

-amylinomimetic - oral antidiabetic
-inh glucagon release
-inh gastric emptying
-anorectic effect
-synthetic pepetide=injection
-AE=N, V,anorexia, hypoglycemia
delayed drug absorption

45
Q

Exenatide & Liraglutide

  • type?
  • MOA?
  • admin?
  • AE?
A
  • incretins-oral anti-diabetic drugs
  • potentiate insulin secretion
  • inh glucagon release
  • inh gastric emptyng
  • anorectic effect
  • INJECTION-peptide
  • N
  • V
  • diarrhea
  • -acute pancreatitis*
  • delayed drug absorption
  • hypoglycemia
46
Q

Sitagliptin, Saxagliptin, Linagliptin

  • type?
  • MOA?
  • admin?
  • AE?
A
  • dipeptidyl peptidase (DPP) inhibitors
  • inh integrin degredation
  • oral admin
  • acute/hemorrhagic/necrotizing pancreatitis
  • upper respiratory inf