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SEM3: PATH30210 Endocrine Health/Disease > Pharm 1 Type II Diabetes Pharmacology > Flashcards

Pharm 1 Type II Diabetes Pharmacology Flashcards

1
Q

4 Strategies for Prevention of Complications of Type II Diabetes?

A

Glycemic Management
Cardiorenal protection – glucose lowering agents
Cardiovascular Risk Factor Management
Weight Management

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2
Q

Target HbA1c for nonpregnant type II diabetic?

A

A reasonable HbA1c (Glycated hemoglobin, linked to a sugar) target is 53 mmol/mol (7%) or less

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3
Q

Normal, Prediabetes and Diabetes Thresholds of HbA1c Test

A
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4
Q

Primary cause of mortality in Diabetes?

A

Cardiovascular Disease

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5
Q

Reducing ______________ decreases the onset and progression of microvascular and macrovascular complications in diabtetes.

A

Reducing hyperglycemia decreases the onset and progression of microvascular and macrovascular complications.

Glucose control is a major focus in the management of patients with diabetes

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6
Q

When to consider dual therapy for Type II diabtes?

A

HbA1c (Glycosylated Hemoglobin) is ≥ 9%

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7
Q

First Line monotherapy for Type II diabetes?

Advantages of this drug?

A

Metformin (Biguanides): Targets Insulin Resistance so has a LOW risk of hypoglycemia (One of the biggest concerns of therapy)

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8
Q

MOA of Metformin?

  • Potent Activator of _______ => Improved Insulin _________
  • Reduces ________ absorption from the gut
  • Impedes ________ Signaling
  • Inhibits Hepatic ________
A
  • Potent Activator of AMPK => Improved Insulin Sensitivity
  • Reduces glucose absorption from the gut
  • Impedes Glucagon Signaling
  • Inhibits Hepatic Gluconeogenesis
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9
Q

_______________ activates muscle AMPK=> Improved Insulin Sensitivity

  • Improved ______________ Function
  • Improved ______________ Transport
  • Metabolic switch from fat __________ to fat ___________
A

Metformin (Type II Diabetes Drug) activates muscle AMPK=> Improved Insulin Sensitivity

  • Improved Insulin Receptor Function
  • Improved Glucose Transport
  • Metabolic switch from fat synthesis to fat oxidation
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10
Q

Side Effects/Contraindications for Metformin?

A

Lactic acidosis is primary side-effect (lack of lactate shuttling into gluconeogenesis pathway)

Vitamin B12 deficiency with long-term use can occur

NOT indicated in pnts with renal/hepatic insufficiency (Renal insufficiency => metformin accumulation = incr. risk of lactic acidosis)

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11
Q

Generations of Sulfonylurea?
Benefits of 2nd vs. 1st?

A

First generation: Tolbutamide (Short Acting) - safest for elderly

Second/Third generation: 200X potent w/ fewer adverse effects and drug interactions
* Glipizide (Fastest Acting)

  • Glyburide (Intermediate Acting)
  • Glimepiride (Long Acting) - avoid in elderly
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12
Q

MOA of Sulfonylureas?

A

Sulfonylureas close K+ channels of Pancreatic Beta Cells (mimicking the effect of glucose)
=> stimulates calcium influx
==> increased insulin release from the pancreas

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13
Q

Sulfonylurea that is well absorbed, rapidly metabolized and is the safest sulfonylurea in elderly patients due to its short half life.

A

Tolbutamide (Short Acting, First Gen)

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14
Q

Sulfonylurea with a half life of 32h. Prolonged hypoglycemia can result in the elderly.

A

Chlorpropamide (Long-Acting)

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15
Q

Sulphonyurea that achieves blood glucose lowering with the lowest dose of any sulfonylurea compound, only requiring once daily dosing.

A

Glimepiride (Long Acting)

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16
Q

When are Sulfonylureas Effective?

When Are they no longer Effective?

A

Useful to treat early stages of Type 2 diabetes when there is an insulin reserve

WILL NOT WORK IN T1D OR LATER STAGES OF T2D WHEN INSULIN RESERVE IS DEPLETED (Check C Peptide Levels)

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17
Q

Insulin Secretagogues with similar MOA to sulfonylureas but don’t contain Sulphur (2 binding sites in common)

A

Meglitinides (Repaglinide and Nateglinide) close K+ channels of Pancreatic Beta Cells (mimicking the effect of glucose)
=> stimulates calcium influx
==> increased insulin release from the pancreas

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18
Q

Insulin Secretagogue with the lowest risk of hypoglycemia of all the insulin that is also safe in those with reduced renal function?

A

Nateglinide: Does not induce insulin in the presence of normoglycemia

19
Q

Who are Thiazolidinediones (TZDs) well suited for?

A

Cohorts young, overweight individuals who are insulin resistant (Pioglitazone)

20
Q

MOA of Thiazolidinediones (TZDs)

A

Thiazolidinediones (TZDs) are potent insulin sensitizers that enhance the action of endogenous insulin

TZDs are ligands of peroxisome proliferator-activated receptor gamma (PPAR-gamma) in adipose, muscle cells => PPAR-gamma increases expression of genes involved in glucose/lipid metabolism (IRS-1, GLUT4)

21
Q

Side Effects/Contraindications of Thiazolidinediones (TZDs)

A

Pioglitazone-risk of bladder cancer at high doses

Rosiglitazone-Increased cardiovascular risk

Both:
Increased deposition of subcutaneous fat (Weight gain)
Fluid retention (Contra heart failure)

Contraindications:
Individuals at risk of heart failure
Breastfeeding/Pregnancy

22
Q

How to minimize side effects of Thiazolidinediones (TZDs)?

A

Risk of hypoglycemia minimal with monotherapy; increased risk with dual therapy

Side-effects can be mitigated by combining TZDs with other medications that promote weight loss (GLP1/SGLT2i).

23
Q

Ideal T2D Therapeutic for someone with hypertension/overweight comorbidities?

A

Sodium-Glucose Cotransporter 2 (SGLT2) Inhibitors (Empagliflozin/Dapagliflozin)

24
Q

MOA of SGLT2 inhibitors?

Other Associations?

A

Blocks glucose (and Na+) reabsorption from the proximal renal tubule in the kidney, thereby increasing urinary glucose excretion

Also associated with weight loss and reduced blood pressure without effects on heart rate.

25
Q

Major Side effects of SGLT2 inhibitors?

A

SGLT2 inhibitors (Empagliflozin/Dapagliflozin) can result in:

  • Urinary tract and genital infections
  • Increase in both LDL-C and HDL-C levels
  • risk of hypoglycemia minimal with monotherapy; increased risk with dual therapy
26
Q

T2D Therapeutic associated with a reduction in adverse cardiovascular events, overall CV death, reduction in risk of hospitalization for heart failure and reduction in risk of
kidney outcomes.

A

Sodium-Glucose Cotransporter 2 (SGLT2) Inhibitors (Empagliflozin/Dapagliflozin)

38% reduction in risk of death from cardiovascular causes!!

27
Q

MOA of Incretins in regulating Glucose Homeostasis?

A

**Incretins (GLP-1/GIP)(( regulate glucose homeostasis through effects on Islet Cell Function

Ingestion of food=> release of incretin hormones from gut:

  • Active GLP-1/GIP travel to Pancreatic BETA Cells=> Increase Insulin => Increase Glucose Uptake/Storage in Muscles/Adipose Tissue
  • Active GLP-1/GIP travel to Pancreatic ALPHA Cells => Decreased Glucagon=> Decreased glucose release into bloodstream by liver
  • GLP-1/GIP DEACTIVATED by DPP-4 Enzyme into inactive metabolites
28
Q

Two synthetic GLP-1 agonists?

A

Exenatide and Liraglutide

29
Q

MOA of GLP-1 (Incretin) agonists

A

Exenatide and Liraglutide decrease glucagon secretion, reduce appetite, slow gastric emptying, promote beta cell proliferation/prevent beta cell apoptosis

30
Q

Recent evidence suggests adding ________ to basal insulin treatment regimen can reduce the need for prandial insulin injections

A

Recent evidence suggests adding GLP1 to basal insulin treatment regimen can reduce the need for prandial insulin injections

31
Q

_____________________:
97% homology to native GLP1 but prolonged half-life
Once daily dosing; injectable; up to 1.8mg give daily
Currently given as a second line therapy with other oral hypoglycemic.

S/Es?

A

Liraglutide (Victoza) ($800 per month):
97% homology to native GLP1 but prolonged half-life
Once daily dosing; injectable; up to 1.8mg give daily
Currently given as a second line therapy with other oral hypoglycemic.

S/E’s: Headache, nausea, diarrhea, antibody formation, pancreatitis

32
Q

_______________________:
53% homology with native GLP1; has a glycine substitution to reduce degradation by DPP 4
Injectable duration of action 10h; twice (5-10mcg)daily 1h before main meals

S/Es?

A

Exenatide (BYETTA):
53% homology with native GLP1; has a glycine substitution to reduce degradation by DPP 4
Injectable duration of action 10h; twice (5-10mcg)daily 1h before main meals

S/Es nausea (44% of users), vomiting, diarrhea; rare hemorrhagic pancreatitis.

33
Q

T2D therapeutic that blocks natural endogenous GLP1 from being degraded?

A

Dipeptidyl Peptidase 4 (DPP4) Inhibitors:
Sitagliptin, saxagliptin, and linagliptin

Delivered orally & reduce HbA1c levels by 0.5-1% on average

34
Q

Dipeptidyl Peptidase 4 (DPP4) Inhibitor Side Effects?

A

Most common S/Es of this class are nausea and headache

Sitagliptin–Risk of pancreatitis and allergy

35
Q

Drug/MOA/MOD of Amylin Analogues?

A

Pramlinitide–synthetic analogue of amylin

MOD:
Injectable –given before meal in addition to insulin
Rapid acting insulin dose should be decreased by ~50% due to risk of hypoglycemia
Cannot be mixed with insulin for injection

MOA:
Suppresses glucagon, delays gastric emptying and has anorectic effects
Duration of action ~150mins

36
Q

Combining __________ with insulin results in similar reductions in HbA1c as traditional insulin regimen but prevents the adverse effects of insulin on weight gain.

A

Combining Liraglutide (97% GLP1 Homologue) with insulin results in similar reductions in HbA1c as traditional
insulin regimen but prevents the adverse effects of insulin on weight gain.

37
Q

Benefits of Incorporating GLP1 Agonists (Liraglutide) with Insulin?

A

Currently given as a second-line therapy with other oral hypoglycemic:

People on insulin alone require much higher doses than those injected w/ GLP1
Increased weight loss compared to lifestyle intervention
Improved glucose tolerance in both healthy and pre-diabetic individuals
Decreased rate of diabetes diagnosis

38
Q

Effects of medication on weight in Type 2 Diabetes

A

Weight loss: Metformin, SGLT2, GLP1 agonists, and amylin mimetics

Weight neutral: DPP inhibitors

Weight gain: TZDs and Insulin

39
Q

Strategies for Treating Diabetes (6)

A
  1. Give insulin to those lacking insulin –short-acting to long-acting insulin formulas
  2. Promote insulin sensitivity in those who are insulin resistant-TZDs, metformin
  3. Stimulate insulin secretion in those not producing enough insulin to compensate for insulin resistance –insulin secretagogues, GLP1-agonists, DPP-4 inhibitors
  4. Reduce glucose production –Metformin, amylin analog
  5. Reduce glucose absorption –alpha-glucosidase inhibitors, SGLT2 inhibitors
  6. Promote weight-loss –GLP-1 agonists, amylin analogue, SGLT2 inhibitors
40
Q

Therapeutics that promote insulin sensitivity in those who are insulin resistant?

A

TZDs (Rosiglitazone, Pioglitazone)

Biguanide (Metformin)

41
Q

Thereaputics that stimulate insulin secretion in those not producing enough insulin to compensate for insulin resistance?

A

Insulin Secretagogues (Sulfonylureas/Meglitinides)

GLP1-agonists (Liraglutide (Victoza))

DPP-4 inhibitors (Sitagliptin)

42
Q

Therapeutics that reduce glucose production?

A

Biguanide (Metformin)

Amylin analog (Pramlinitide)

43
Q

Therapeutics that reduce glucose absorption

A

SGLT2 inhibitors (Empagliflozin/Dapagliflozin)

Alpha-glucosidase inhibitors

44
Q

Therapeutics that promote weight loss

A

GLP 1 agonists (Liraglutide (Victoza), Exenatide (BYETTA))

Amylin analog (Pramlinitide)

SGLT2 inhibitors (Empagliflozin/Dapagliflozin)

SEM3: PATH30210 Endocrine Health/Disease (25 decks)

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