Anti Diabetics Flashcards

1
Q

Insulin secretion mechanism

A

Glucose in blood increases –> cell depolarizes –> Ca+ triggers insulin secretion

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2
Q

Insulin receptor

A

a subunit for recognition

b subunit tyrosine kinase and phosphorylates tyrosine

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3
Q

Insulin inhibits

A

gluconeogenesis

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4
Q

Insulin causes

A
  • glucose entry in muscle and adipose tissue
  • glycogen synthesis in liver and muscle
  • fatty acid synthesis and storage
  • amino acid uptake
  • glycolysis
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5
Q

Rapid acting insulin is

A

fast onset, short duration

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6
Q

Short acting insulin is

A

rapid onset

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7
Q

Long acting insulin is

A

slow onset, long duration

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8
Q

Rapid acting insulin analogs

A

Insulin Lispro
Insulin Aspart
Insulin Glulisine

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9
Q

Rapid acting insulin analogs mimic ___

A

prandial release of insulin
usually given with long acting insulin
given 15 min before meal

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10
Q

Short acting insulin __

A

soluble crystalline zinc insulin

given 30 minutes before meal

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11
Q

Intermediate acting insulin ___

A

Neutral protamine Hagedorn (NPH)
aka. Isophane insulin

Crystalline zinc + protamine
used for basal control

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12
Q

Long acting insulin analogs

A

Insulin Glargine
Insulin Degludec
Insulin Detemir

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13
Q

Rapid and long acting insulin do?

A
  • improve HbA1C levels

- reduce hypoglycemia

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14
Q

Standard mode of insulin therapy is

A

SC injection

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15
Q

IV insulin is used in

A
  • pt with ketoacidosis
  • perioperative period
  • labor and delivery
  • ICU
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16
Q

Inhaled insulin AE and CI

A
  • cough, throat pain, hypoglycemia

CI:

  • copd
  • asthma
  • smokers
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17
Q

Insulin regimen goals?

A

replace basal insulin and pradnsial insulin

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18
Q

2 methods of insulin release

A
  1. basal bolus insulin regimens

2. insulin pump therapy

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19
Q

Basal bolus insulin regime

A
  • one shot of long acting insulin when fasting

- doses of rapid acting around mealtimes

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20
Q

Insulin pump therapy

A

best way to mimic normal insulin secretion

  • glulisine, lispro, or insulin aspart is used in the insulin pump
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21
Q

The biggest AE of insulin

A

hypoglycemia

  • less risk with rapid than regular
  • less risk with long than NPH
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22
Q

If you have mild hypoglycemia?

A

drink OJ, or have sugar

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23
Q

If you have severe hypoglycemia?

A

IV glucose infusion

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24
Q

Drugs that cause hypoglycemia

A

Ethanol
B blockers
Salicylates

25
Drugs that cause hyperglycemia
* Epinephrine * Glucocorticoids * Atypical antipsychotics * HIV protease inhibitors * Phenytoin * Clonidine * Ca2+-channel blockers * Diuretics
26
NON- insulin antidiabetic agents
- Insulin secretagogues - Biguanides - Thiazolidinediones - A glucosidase inhibitors - Incretin analogues - Inhibitors of DPP-IV - Amylin analogs - Bile-acid sequestrants - SGLT2 inhibitiors
27
Insulin secretagogues
Sulfonyureas | Meglitinides
28
Sulfonyureas
1st gen and 2nd gen reduce fasting plasma glucose and HBA1C - stimulate insulin release from B cells by binding to SUR1 subunit and blocking K channels AE: - hypoglycemia - weight gain
29
First gen sulfonylureas
Chlorpropamide AE: - hypoglycemia - hyperemic flush when alcohol ingested due to inhibitiono f aldehyde dehydrogenase - SIADH CI: - old ppl
30
Second gen sulfonylureas
Glyburide Glipizide Glimepiride - more potent than 1st gen AE: - hypoglycemia - weight gain
31
Meglitinides
Repaglinide Nateglinide - not as effective as sulfonylureas - rapid onset, short duration - postprandial glucose regulators - take before each meal AE: - weight gain CI: - pt with sulfur allergy
32
Biguanides
Metformin
33
Metformin
AE: - GI - impaired B12 absorption - lactic acidosis CI: - renal, hepatic disease - hypoxia - alcoholism first line of therapy in type 2 diabetes
34
TZDs
promote glucose uptake in adipose tissue ➢ Pioglitazone ➢ Rosiglitazone slow onset ``` MOA: gene regulation AE: - fluid retention, edema - weight gain - CHF ``` CI: - heart failure liver function monitoring required
35
a-Glucosidase Inhibitors
Acarbose
36
Acarbose
MOA: - reduces postprandial digestion of starch - reduces absorption - drop HBA1C and FPG lvl AE: - GI effects - hepatic. enzyme elevation CI: - IBS liver function monitoring required
37
Incretin analogs
Exenatide (injectable)
38
Exenatide
analog of Glucagon like polypeptide 1 agonist of GLP-1 receptor resistant to dipeptidyl peptidase IV (DPP-IV) MOA: • Enhances glucose-dependent insulin secretion. • Suppresses postprandial glucagon release. • Slows gastric emptying. • Decreases appetite. • May stimulate β-cell proliferation AE: - nausea, vomiting - acute pancreatitis CI: - pt with gasteroparesis
39
Inhibitors of DPP-IV
Sitagliptin
40
Sitagliptin
MOA: - inhibitor of DPP-IV - increase GLP1 and insulin AE: - pancreatitis - hypersensitivity reactions
41
Amylin analogs
Pramlintide
42
Pramlintide
MOA: - analog of amylin - inhibits food intake, gastric emptying and glucagon secretion
43
BIle acid sequestrants
Colesevelam
44
Colesevelam
MOA: lower LDL cholesterol used for type 2 DM
45
SGL2 inhibitors
Canagliflozin
46
Canagliflozin
MOA: - blocks glucose reabsorption - increased glucose excretion and decreased blood glucose lvls AE: - UTI - hyperkalemia, hypermagnesmia CI: - pt with GFR < 45
47
type 2 DM inital drug therapy
metformin monotherapy reduce HBA1C by 1%
48
Dual combination therapy
after 3 months if monotherpay doesnt help add second oral agent GLP1 agonist or insulin
49
Triple combination therapy
if 2 drug doesnt help add 3rd agent might need to get --> insulin if HBA1C > 8.5%
50
GLP1 receptor agonist vs. Insulin
GLP1 RA is better injectable option because minimize hypoglycemia and weight gain
51
When is insulin initial therapy for type 2 DM
- ongoing catabolism (weight loss) - hyperglycemic syndromes - ketonuria - HbA1C > 10% - random glucose > 300
52
Gestational DM (preganancy)
NPH insulin single dose and id postprandial glucose control needed then add insulin lispro or aspart
53
DM with CVD
- ACEI/ARB - Statins - Aspirin
54
DM with nephropathy
- ACEI/ARB
55
DM with gastroparesis
prokinetic agents: metoclopramide or erythromycin
56
DM with erectile dysfunction
phosphodiesterase type 5 inhibitors
57
Glucagon
secreated by pacreatic a cells increases: glycogen degradation, gluconeogenesis, fatty acid oxiziation, insulin release decreases: glycolysis
58
Glucagon uses:
- severe hypoglycemia - radiology of bowel - B blocker poisoning - C peptide test