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Pharmacology (Winter) > Diabetes Drugs - Part 2 > Flashcards

Diabetes Drugs - Part 2 Flashcards

1
Q

Insulin releasing agents:

A

Sulfonylureas & meglitinides

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2
Q

Weight reducing agents (AMPK activator):

A

Biguanides (metformin; 1st line therapy)

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3
Q

Insulin sensitivity enhancers:

A

Glitazones
- Rosiglitazone; Pioglitazone

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4
Q

Glucosidase inhibitors:

A

Acarbose

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5
Q

Incretin-related molecules:

A

GLP-1 analogues

DPP-4 inhibitors

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6
Q

Sodium-glucose transport protein-2 (SGLT2) inhibitors:

A

Dapaglifozin

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7
Q

Sulfonylureas:

A

Glimepiride; Glyburide; Glipizide

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8
Q

Sulfonylureas MOA:

A
  • Over 60 yrs of use (1st gen)
  • Release insulin form pancreatic beta cells
  • Reduce serum glucagon levels
  • Potentiate the action of insulin on its target tissues

Target SUR1 to block the KATP channel
- KIR6.2 (4 subuits)
- ATP binding blocks pore
- SUR1 (4 subunits) – binds MgADP/ATP at nucleotide binding sites
- Causes pore opening
- High affinity on SUR1
- Low affinity on KIR6.2 (not relevant in pts)
- Partial antagonists

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9
Q

Sulfonylureas AE’s:
- Glimepiride; Glyburide; Glipizide

A
  • Hypoglycemia (glyburide worse)
  • Weight gain
  • Aggravation of myocardial ischemia
    CI: in pts w/ CV disease & elderly (hypoglycemia more serious) & in pts w/ hepatic impairment &/or renal insufficiency

(not 1st DOC b/c can cause most of these things that come up w/ pts that have diabetes)

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10
Q

Meglitinides MOA:
- Repaglinide; Nateglinide
(Meglitinide analogs)

A
  • Structurally diff from sulfonylureas
  • Bind to SUR1 & KIR6.2
  • Rapidly absorbed w/ a short half life (4-7 hrs)
  • MUST be taken 15-30 mins prior to meals
  • Fast onset of action (1 hr peak)
  • Can be combined w/ Metformin
  • Repaglinide CAN BE USED in pts w/ renal impairment & in the elderly
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11
Q

Biguanides MOA:
- Metformin (GlucophageR) – 1st line therapy

A
  • Not fully understood
  • No effect on insulin secretion
  • *Activates cyclic AMP-activated protein kinase (AMPK) – regulator of hepatic glucose production & improves insulin resistance
  • Dose 1500-2000 mg/day (divided)
  • Euglycemic agent (benefit)
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12
Q

Biguanides Benefits:
- Metformin (GlucophageR) – 1st line therapy

A
  • *Euglycemic rather than hypoglycemia – i.e. lowers BG after food, but not fasting levels in steady state
  • Increase glycolysis & insulin binding
  • Inhibits gluconeogenesis in liver & glucose absorption from the gut
  • Reduce plasma glucagon levels
  • *Mild weight loss
  • METFORMIN is not metabolized
  • Excreted by the kidneys in the active form
  • Half life 1.5-3 hours
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13
Q

Biguanides AE’s:
- Metformin (GlucophageR) – 1st line therapy

A
  • Lactic acidosis – impaired liver metabolism of lactate
  • Range of GI effects
  • B12 deficiency
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14
Q

Glitazones – Thiazolidinedione (TZD) compounds MOA:
- Rosiglitazone; Pioglitazone

A
  • Decreases insulin resistance by binding to nuclear r’s which regulate genes responsible for lipid metabolism
  • Peroxisome proliferator-activated r. (PPAR)-g agonists
  • Decreases gluconeogenesis, glucose output & triglyceride synthesis in the liver
  • Increases glucose uptake in skeletal muscle & adipose tissues
  • Has no effect on insulin secretion

(by driving expression of these proteins, you turn on these pathways which help to decrease hyperglycemia)

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15
Q

Glitazones – Thiazolidinedione (TZD) compounds Metabolism:
- Rosiglitazone; Pioglitazone

A
  • Absorption better when taken w/ food
  • Plasma level peaks in 3 hr, & half-life 16-34 hr
  • Metabolized in the liver by CYP3A4
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16
Q

Glitazones – Thiazolidinedione (TZD) compounds Use:
- Rosiglitazone; Pioglitazone

A
  • Used for T2D pts who need more than 30 units of insulin daily & have HbA1C > 8.5%
  • Max effect may require 12 wks of tx
  • Should be taken orally once a day

Benefits:
- Tighter control of glucose
- HbA1C decreased by 0.6-1.6%
- No lactic acidosis observed
- Pioglitazone – lowers TG’s & raises HDL cholesterol
- Rosiglitazone – raises HDL cholesterol
(therefore both do have some benefits)

17
Q

Glitazones – Thiazolidinedione (TZD) compounds AE’s:
- Rosiglitazone; Pioglitazone

A
  • Rosiglitazone – myocardial infraction (use stopped in Europe)
    CI: in pts w/ renal failure & liver impairment
  • Edema
  • Macular edema
  • Loss of bone density
  • Weight gain
  • Pioglitazone – bladder cancer
    *Consequently, these drugs are used less & less
18
Q

Glucosidase Inhibitors MOA:
- Acarbose; Miglitol

A
  • Acts only in the gut, slows carbohydrate breakdown
  • Competitive inhibitors of a-glucosidase enzymes
  • Lowers post-prandial rise in BG
  • Lowers HbA1C levels
19
Q

Glucosidase Inhibitors Use:
- Acarbose; Miglitol

A

Approved for T2D

20
Q

Glucosidase Inhibitors SE’s:
- Acarbose; Miglitol

A

Dose dependent abd. bloating, flatulence, which is reduced in 3 months (not really serious)

21
Q

Incretin-related molecules:

A
  • Meal ingestion leads to secretion of GLP-1 (glucagon-like peptide-1) & gastric inhibitory peptide (GIP) from the gut
    • These agents increase insulin synthesis & release, & also decrease glucagon (from a-cells of pancreas)

GLP-1 analogues
DPP-4 inhibitors

22
Q

Incretins – DPP-4 Inhibitors:
- Sitagliptin-PO4
- Saxagliptin

A
  • Dipeptidyl peptidase-4 inhibitors
  • Orally active
  • Peak at 1-4 hr – half life of 12 hr (3 hr for sax)
23
Q

Incretins – DPP-4 Inhibitors: AE’s:
- Sitagliptin-PO4
- Saxagliptin

A
  • Respiratory infections
  • May produce pancreatitis (sitagliptin)
  • Hypersensitivity rxns – anaphylaxis
24
Q

GLP-1 Analogues:
- Exenatide
- Liraglutide

A

GLP-1 Analogues:
- Enhances glucose-dependent insulin secretion from pancreatic b cells
- Restores 1st-phase insulin response
- Suppresses glucagon secretion from pancreatic a cells under conditions of hyperglycemia, which leads to a reduction in glucose output from the liver
- Reduces food intake – weight loss
- Slows gastric emptying, allowing for timely absorption not nutrients

25
Q

Exenatide:

A
  • Used for T2D w/ either metformin or sulfonylurea
  • It is a synthetic version of a intestinal hormone (Extendin-4)
  • Euglycemic on its own
  • Injected 2x/day*
  • Peak at 2hr – lasts 10 hrs
  • Consider potential risks of pancreatitis, renal dysfunction
  • Nausea
26
Q

Sodium-glucose transport protein-2 (SGLT2 inhibitors:

A

Dapagliflozin
- Competitive inhibitor of SGLT2
- Functions in the proximal tubule of kidney (transporter)
- Prevents re-absorption of glucose (glucose is flushed out in urine & therefore decrease BGL’s)

27
Q

Sodium-glucose transport protein-2 (SGLT2 inhibitors: SE’s

A
  • Excessive glycosuria – hypotension
  • Urinary tract & bladder infection
28
Q

Other drugs – Pramlintide:

A
  • Synthetic analog of Amylin, which is more soluble & dose not readily aggregate like amylin
  • Amylin is a hormone co-secreted w/ insulin from b cells in response to glucose
29
Q

Other drugs – Pramlintide MOA:

A
  • Suppresses glucagon secretion
  • Rate of glucose absorption from the gut is slowed down
  • Fructosamine is a surrogate marker which reflects average glucose [ ]’s over 2-3 wks prior to testing
  • Pramlintide decreased fructosamine by 60%
30
Q

Other drugs – Pramlintide Use:

A
  • Pramlintide can be mixed w/ regular or NPH insulin just prior to injecting
  • Found to be useful for both T1D & T2D
31
Q

T1D:

A

control BG w/ insulin & diet as best as possible

32
Q

T2D:

A
  • exercise, weight reduction & diet control
  • if mild then add anti-diabetic agents - metformin
  • oral combo therapy & diet
  • add insulin
  • reduce hypertension*

Future mode of therapy may include:
- CGM + insulin pump; beta islet cell transplantation

33
Q

Diabetes in the elderly (oral agents):

A

in elderly people, sulfonylureas should be used w/ caution b/c the risk of hypoglycemia increases exponentially w/ age

in general, initial doses should be half those for younger people, & doses should be increased more slowly

Pharmacology (Winter) (23 decks)

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