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PHAR 230 > M4 L3: Insulin and Anti-diabetic Agents > Flashcards

M4 L3: Insulin and Anti-diabetic Agents Flashcards

1
Q

treatment of diabetes

A

diet control, antidiabetic agents, treatment of complications

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2
Q

what are 2 types of antidiabetic agents

A
  1. insulin
  2. oral hypoglycemic agents (T2D)
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3
Q

indications of insulin therapy

A
  1. type 1 diabetes
  2. type 2 diabetes
  3. gestational diabetes
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4
Q

when can you not take oral hypoglycemic agents

A

during pregnancy, gestational diabetes

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5
Q

administration of insulin

A

injection: IV, IM, SC
alternative methods: pump

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6
Q

onset peak and duration of fast (rapid) insulin

A

onset: 5-15 min
peak: 3/4-1 hr
duration: 2-4 hr

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7
Q

onset peak and duration of short insulin

A

onset: 0.5-1 hr
peak: 2-3 hr
duration: 5-8 hr

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8
Q

onset peak and duration of intermediate insulin

A

onset: 1-2 hr
peak: 4-12 hr
duration: 10-20 hr

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9
Q

onset peak and duration of long insulin

A

onset: 1-2 hr
peak: minimal
duration: 18-24 hr

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10
Q

onset peak and duration of ultra long insulin

A

onset: 1-2 hr
peak: minimal
duration: >24 hr

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11
Q

insulin preparations for fast-acting

A

lispro-aspart

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12
Q

insulin preparations for short-acting

A

regular (crystalline) insulin

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13
Q

insulin preparations for intermediate-acting

A

NPH (neutral protamine hagedorn)

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14
Q

insulin preparations for long-acting

A

detemir-glargine

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15
Q

insulin preparations for ultra-long

A

degludec

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16
Q

insulin preparations for mixed types

A

(combinations)

rapid onset + prolonged duration
ex: NPH/regular 70/30

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17
Q

what is conventional therapy for insulin regimens

A
  • 1-2 injections/day
  • daily self monitoring of glucose
  • lower risk of hypoglycemia
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18
Q

what is intensive therapy for insulin regimens

A
  • multiple daily injections
  • daily self monitoring of glucose and dose adjustment
  • reduction in retinopathy, nephropathy, and neuropathy
  • higher risk of hypoglycemia (3- fold more than conventional)
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19
Q

what does a daily insulin schedule for fast/short type 1 diabetes

A
  • injection time before breakfast (BF)
  • major affect BF->lunch
  • end effect before lunch
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20
Q

what does a daily insulin schedule for fast/short type 1 diabetes

A
  • injection time before breakfast
  • major effect lunch -> dinner
  • end effect before dinner
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21
Q

what does a daily insulin schedule for fast/short type 2 diabetes

A
  • injection time before dinner
  • major effect dinner -> bed snack
  • end effect before bed snack
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22
Q

what does a daily insulin schedule for NPH/long type 2 diabetes

A
  • injection time before dinner
  • major effect overnight
  • end of effect before breakfast the next day
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23
Q

absorption of SC insulin

A
  • highly variable: inter (diff from one person to another based on their metabolism and so on)/intraindividual (some conditions will be associated with high rate of absorption.

factors affecting absorption:
- site of injection
- blood flow to site of injection
- depth of injection
- exercise increases absorption
- massage of the area increases absorption

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24
Q

what are alternatives to insulin injections?

A
  • insulin pumps, insulin pens (most common)
  • transdermal: jet injection, patches
  • inhaled insulin (afrezza)
  • oral formulas (under investigation)
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25
systemic complications of insulin therapy
- hypoglycemia -> most dangerous - insulin allergy -> rare w human insulin - insulin resistance
26
what are local complications of insulin therapy
- lipoatrophy - hypertrophy (change the site of injection)
27
ex of oral hypoglycemic agents
- sulfonylureas (insulin secretagogues) - meglitinides (insulin secretagogues) - biguanides - thiazolidinediones (TZDs, glitazones) - alpha-glucosidase inhibitor
28
how is insulin stimulated by beta cell (inulin secretagogues)
they inhibit potassium on the beta-cell, which causes depolarization, resulting in increased calcium entry, and increased insulin release
29
what causes increased receptor sensitivity for insulin (sulfonylureas)
potentiate insulin action in different tissues - they require functional beta-cells to work, and are only useful for type 2 NOT type 1 diabetes
30
alpha cells secrete...
glucagon
31
beta cells secrete...
insulin
32
what are endocrine glands
- form clusters called pancreatic islets - secrete hormones
33
what are the effects of insulin
1. accelerates glucose uptake and utilization 2. stim glycogen formation 3. stim triglyceride formation in adipose tissue 4. stim amino acid absorption and protein synthesis
34
sulfonylureas pharmacokinetics
- bind to plasma proteins - metabolized in the liver - excreted through kidneys - exaggerated effects in elderly and renal or liver disease - cross the placenta -> teratogenic effect contraindicated during pregnancy**
35
what are sulfonylureas drugs that increase hypoglycemic effects
- NSAIDs, warfarin, MAO inhibitors, alcohol, some antibacterials (ex: sulfonamides) - microsomal enzyme inhibitors
36
what are sulfonylureas drugs that decrease hypoglycemic effects
- microsomal enzyme inducers (ex: rifampicin) - phenytoin (inhibits insulin release)
37
what sulfonylureas drugs mask the symptoms of hypoglycemia
beta blockers
38
sulfonylureas preparations for 1st gen examples
tolbutamide, chlorpropamide
39
sulfonylureas preparations for 2nd gen examples
glipizide, glibenclamide, gliclazide
40
sulfonylureas preparations for 3rd gen examples
glimepiride
41
duration of tolbutamide & glipizide (sulfonylurea agents)
6-10 hrs dose frequency: BID-TID
42
duration of glibenclamide & gliclazide (sulfonylurea agents)
12-16 hrs dose frequency: OD-BID
43
duration of glimepiride & chlorpropamide (sulfonylurea agents)
24-72 hrs dose frequency: OD
44
sulfonylureas adverse effects
- hypoglycemia - GI disturbances - hepatic toxicity - allergic skin reactions
45
biguanides mech of action
- decreased gluconeogenesis in liver - increased glucose uptake by skeletal muscles
46
biguanides indications
- 1st choice for obese patients with type 2 - can be combined with sulfonylurea or insulin
47
what is the advantage of biguanides
- do not cause hypoglycemia as they do not alter insulin levels
48
biguanides side effects
- anorexia - nausea, diarrhea, metallic taste - lactic acidosis
49
what is metformin
(only available biguanide on the market so far) - 2 tablet forms: glucophage, glucophage XR
50
what are meglitinides
- short acting insulin secretagogues - action is similar to sulfonylureas - short acting, half life is 1hr
51
indications of meglitinides
type 2 DM - can be combined w metformin
52
adverse effects of meglitinides
hypoglycemia (rare)
53
examples of meglitinides
repaglinide, nateglinide
54
mech of action for thiazolidinediones (TZDs)
- activate a transcription regulator PPARy - this improved glucose uptake in skeletal muscles - decreased hepatic glucose production - modulate lipogenesis in adipocytes - reverse insulin resistance
55
what are the indications of thiazolidinediones
- T2D - alone or combined w metformin, sulfonylurea
56
thiazolidinedione adverse effects
congestive heart failure and myocardial ischemia - may cause hepatic injury (monitor liver function)
57
what are ex. of thiazolidinediones
rosiglitazone, pioglitazone
58
what are alpha-glucosidase inhibitors
- inhibits alpha-glucosidases in intestine -> reduces absorption of carbs - not absorbed from intestine - control post-prandial glucose levels not adequately controlled by diet and sulfonylureas
59
side effects of alpha-glucosidase inhibitors
GI upset and flatulence
60
name an example of a alpha-glucosidase inhibitor
acarbose
61
recent antidiabetic agents
- glucagon-like peptide-1 (GLP-1) agonists - DPP-4 inhibitors (gliptins) - amylin analogues - gliflozins
62
what are glucagon-like peptide-1 (GLP-1) agonists
- group of GIT hormones called "incretins" - adjunct treatment in T2D - SC injection
63
example of glucagon-like peptide-1 (GLP-1) agonists
exenatide
64
what are incretins
GIT hormones stim insulin release and inhibit glucagon. Includes GLP-1 and GIP (gastric inhibitory peptide)
65
mech of action for glucagon-like peptide-1 (GLP-1) agonists
- increase insulin release (insulin secretagogues) - decrease glucagon release
66
mech of action for DPP-4 inhibitors (gliptins)
- decreased DPP-4 enzyme -> increased incretins - is the adjunct treatment in type 2 - take them orally
67
what are the adverse effects of DPP-4 inhibitors (gliptins)
- joint pain - HF - pancreatitis - ? pancreatic cancer
68
ex of DPP-4 inhibitors (gliptins)
sitagliptin, saxagliptin
69
what is amylin
- a hormone made by the beta cells of the pancreas (not just insulin!) made in a 99:1 ratio (larger being insulin)
70
mech of action for amylin analogues
- slows gastric emptying - decrease postprandial glucagon release
71
what is amylin analogues for, how is it administered
- adjunct treatment for T1D, and T2D - SC injection
72
what is an example of amylin analogues
pramlintide (only product available)
73
what do glifolzins do
decrease SGLT-2 (sodium-glucose cotransporter 2) -> decrease renal glucose reabsorption -> glycosuria
74
what is gliflozins used for and how is it administered
- T2D (alone or in combo) - orally
75
adverse effects of gliflozins
- hypoglycemia - ketoacidosis - UTI
76
gliflozins example
canagliflozin

PHAR 230 (31 decks)

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