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Endocrine - Pharmacology > Non-Insulin Drugs to Treat Diabetes > Flashcards

Non-Insulin Drugs to Treat Diabetes Flashcards

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1
Q

Sulfonylureas are used in the treatment of diabetes?
• 1st generation?
• 2nd Generation?

A

Sulfonylureas:

  • *1st Chlorpropamide, tolbutamide**
  • *2nd Glyburide, glipizide, glimepiride – the “G-ides”**
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2
Q

Chorapropamide
MOA
T1DM/T2DM?
Metabolism

A

Sulfonylureas: 1st Chlorpropamide, tolbutamide; 2nd Glyburide, glipizide, glimepiride – the “G-ides”

**TD2M tx only…Requires Islet cell function**

MOA:
These block the ATP-dependent potassium channel in ß-cells leading to depolarization, opening of Ca2+ channels, and release of insulin vesicles.

Metabolism:
These are extensively protein bound, metabolized by the liver and excreted by the kidney

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3
Q

Chlorapropamide
Side Effects
Contraindications
Administration

A

Sulfonylureas: 1st Chlorpropamide, tolbutamide; 2nd Glyburide, glipizide, glimepiride – the “G-ides”

**TD2M tx only…Requires Islet cell function**

Side Effects:
Hypoglycemia, Renal failure, first generations (chloropropamide, and tolbutamide) have disulfram-like effects.

Contraindications:
NSAIDs cause increased likelihood of hypoglycemic events

Administration:
Oral

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4
Q

Tolbutamide
MOA
T1DM/T2DM?
Metabolism

A

Sulfonylureas: 1st Chlorpropamide, tolbutamide; 2nd Glyburide, glipizide, glimepiride – the “G-ides”

**TD2M tx only…Requires Islet cell function**
MOA:

These block the ATP-dependent potassium channel in ß-cells leading to depolarization, opening of Ca2+ channels, and release of insulin vesicles.

Metabolism:
These are extensively protein bound, metabolized by the liver and excreted by the kidney

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5
Q

Tolbutamide
Side Effects
Contraindications
Administration

A

Sulfonylureas: 1st Chlorpropamide, tolbutamide; 2nd Glyburide, glipizide, glimepiride – the “G-ides”

**TD2M tx only…Requires Islet cell function**

Side Effects:
Hypoglycemia, Renal failure, first generations (chloropropamide, and tolbutamide) have disulfram-like effects.

Contraindications:
NSAIDs cause increased likelihood of hypoglycemic events

Administration:
Oral

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6
Q

Glyburide
MOA
T1DM/T2DM?
Metabolism

A

Sulfonylureas: 1st Chlorpropamide, tolbutamide; 2nd Glyburide, glipizide, glimepiride – the “G-ides”

**TD2M tx only…Requires Islet cell function**
MOA:

These block the ATP-dependent potassium channel in ß-cells leading to depolarization, opening of Ca2+ channels, and release of insulin vesicles.

Metabolism:
These are extensively protein bound, metabolized by the liver and excreted by the kidney

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7
Q

Glyburide
Side Effects
Contraindications
Administration

A

Sulfonylureas: 1st Chlorpropamide, tolbutamide; 2nd Glyburide, glipizide, glimepiride – the “G-ides”

**TD2M tx only…Requires Islet cell function**

Side Effects:
Hypoglycemia, Renal failure, first generations (chloropropamide, and tolbutamide) have disulfram-like effects.

Contraindications:
NSAIDs cause increased likelihood of hypoglycemic events

Administration:
Oral

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8
Q

Glipizide
MOA
T1DM/T2DM?
Metabolism

A

Sulfonylureas: 1st Chlorpropamide, tolbutamide; 2nd Glyburide, glipizide, glimepiride – the “G-ides”

**TD2M tx only…Requires Islet cell function**
MOA:

These block the ATP-dependent potassium channel in ß-cells leading to depolarization, opening of Ca2+ channels, and release of insulin vesicles.

Metabolism:
These are extensively protein bound, metabolized by the liver and excreted by the kidney

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9
Q

Glipizide
Side Effects
Contraindications
Administration

A

Sulfonylureas: 1st Chlorpropamide, tolbutamide; 2nd Glyburide, glipizide, glimepiride – the “G-ides”

**TD2M tx only…Requires Islet cell function**

Side Effects:
Hypoglycemia, Renal failure, first generations (chloropropamide, and tolbutamide) have disulfram-like effects.

Contraindications:
NSAIDs cause increased likelihood of hypoglycemic events

Administration:
Oral

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10
Q

Glimpiride
MOA
T1DM/T2DM?
Metabolism

A

Sulfonylureas: 1st Chlorpropamide, tolbutamide; 2nd Glyburide, glipizide, glimepiride – the “G-ides”

**TD2M tx only…Requires Islet cell function**
MOA:

These block the ATP-dependent potassium channel in ß-cells leading to depolarization, opening of Ca2+ channels, and release of insulin vesicles.

Metabolism:
These are extensively protein bound, metabolized by the liver and excreted by the kidney

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11
Q

Glimepiride
Side Effects
Contraindications
Administration

A

Sulfonylureas: 1st Chlorpropamide, tolbutamide; 2nd Glyburide, glipizide, glimepiride – the “G-ides”

**TD2M tx only…Requires Islet cell function**

Side Effects:
Hypoglycemia, Renal failure, first generations (chloropropamide, and tolbutamide) have disulfram-like effects.

Contraindications:
NSAIDs cause increased likelihood of hypoglycemic events

Administration:
Oral

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12
Q

What Meglintinides are used in the treatment of Diabetes?

A

Meglitinides: repaglinide, nateglinide – the “glinides”

*Similar function to sulfonureas, but different structure

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13
Q

Repaglinide
MOA
Metabolism
T1DM/T2DM?

A
  • *Meglitinides** repaglinide, nateglinide – the “glinides”
  • **TD2M tx only…Requires Islet cell function***

MOA:
These block the ATP-dependent potassium channel in ß-cells leading to depolarization, opening of Ca2+ channels, and release of insulin vesicles.
***Structurally unrelated to sulfonureas***

Metabolism:
Taken before meals; metabolized by the liver; Short half-life

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14
Q

Repgalinide
Side Effects
Contraindications
Administration

A

Meglitinides repaglinide, nateglinide – the “glinides”

Side Effects:
Hypoglycemia – more likely to see this with meglitinides than with sulfonureas

Containdications:
None mentioned

Administration:
Oral

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15
Q

Nateglinide
MOA
Metabolism
T1DM/T2DM?

A

Meglitinides repaglinide, nateglinide – the “glinides”
**TD2M tx only…Requires Islet cell function**
MOA:

These block the ATP-dependent potassium channel in ß-cells leading to depolarization, opening of Ca2+ channels, and release of insulin vesicles.
***Structurally unrelated to sulfonureas***

Metabolism:
Taken before meals; metabolized by the liver; Short half-life

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16
Q

Nateglinide
Side Effects
Contraindications

A

Meglitinides repaglinide, nateglinide – the “glinides”

Side Effects:
Hypoglycemia – more likely to see this with meglitinides than with sulfonureas

Containdications:
None mentioned

Administration:
Oral

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17
Q

What biguanides are used in the treatment of DM?

A

Biguanides: Phenformin (no longer used), Metformin – the “formins”

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18
Q

Metformin
MOA
Metabolism

A

Biguanides: Phenformin (no longer used), Metformin – the “formins”
****First-line therapy in T2DM*****CAN be used in T1DM
MOA:
These work by increasing AMP kinase activity that is typically activated in times of low ATP so it phosphorylates enzymes used in glycolysis an others that leads to lowering of blood glucose. (decreases gluconeogenesis, increases glycolysis, and increases peripheral glucose uptake.

Metabolism:
not mentioned

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19
Q

Metformin
Side Effects
Contraindications
Administration

A
  • *Biguanides:** Phenformin (no longer used), Metformin – the “formins”
  • ****First-line therapy in T2DM*****CAN be used in T1DM*

Side Effects:
LACTIC ACIDOSIS, GI upset

Lactic acidosis makes sense because metformin increases glycolysis and may overwhelm the ox-phos pathway

Containdications:
Renal Insufficiency – because of the risk of lactic acidosis

Administration:

Oral

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20
Q

That thiazolidindiones are used in the treatment of DM?
• how do they work?

A

Thiazolidindiones: troglitazone, rosiglitazone, pioglitazone, rosiglitazone + metformin – the “azones”

MOA:
Binds to Peroxisome Proliferator-Activated Receptor-gamma (PPAR-gamma) – a nuclear transcription regulator. This leads to increased insulin sensitivity peripherally. Ultimately this leads to increased glucose transport into muscles and adipose tissue.

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21
Q

Troglitazone
MOA
Metabolism

A

Thiazolidindiones: troglitazone, rosiglitazone, pioglitazone, rosiglitazone + metformin – the “azones”

MOA:
Binds to Peroxisome Proliferator-Activated Receptor-gamma (PPAR-gamma) – a nuclear transcription regulator. This leads to increased insulin sensitivity peripherally. Ultimately this leads to increased glucose transport into muscles and adipose tissue.

Metabolism:
Absorbed from GI tract, little metabolism

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22
Q

Troglitazone
Side Effects
Contraindications
Administration

A

Thiazolidindiones: troglitazone, rosiglitazone, pioglitazone, rosiglitazone + metformin – the “azones”

Side Effects:
Increased risk of fractures, Hepatotoxicity, weight gain, edema

Containdications:
safe even with renal impairment

Administration:

Oral

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23
Q

Rosaglitazone
MOA
Metabolism

A

Thiazolidindiones: troglitazone, rosiglitazone, pioglitazone, rosiglitazone + metformin – the “azones”

MOA:
Binds to Peroxisome Proliferator-Activated Receptor-gamma (PPAR-gamma) – a nuclear transcription regulator. This leads to increased insulin sensitivity peripherally. Ultimately this leads to increased glucose transport into muscles and adipose tissue.

Metabolism:
Absorbed from GI tract, little metabolism

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24
Q

Rosaglitazone
Side Effects
Contraindications
Administration

Study These Flashcards
A

Thiazolidindiones: troglitazone, rosiglitazone, pioglitazone, rosiglitazone + metformin – the “azones”

Side Effects:

Increased risk of fractures, Hepatotoxicity, weight gain, edema

Containdications:
safe even with renal impairment

Administration:

Oral

25
What alpha glucosidase inhibitors are used in the treatment of DM?
**Alpha-glucosidase inhibitors:** acarbose, miglitol
26
Acarbose MOA Metabolism
**Alpha-glucosidase inhibitors**: acarbose, miglitol MOA: **Inhibition of intestinal brush-border alpha-glucosidases** – remember glucose must be in its monomeric form to be absorbed so this allows it to move through the GI tract – this *decreases the rise in post-prandial glucose* Metabolism: not mentioned
27
Acarbose Side Effects Contraindications Administration
**Alpha-glucosidase inhibitors**: acarbose, miglitol ``` Side Effects: GI disturbances (flatulence) are common because more sugar makes it to your colonic flora ``` Containdications: none mentioned Administration: Oral – typically used as a combination drug
28
Miglitol MOA Metabolism
**Alpha-glucosidase inhibitors**: acarbose, miglitol MOA: **Inhibition of intestinal brush-border alpha-glucosidases** – remember glucose must be in its monomeric form to be absorbed so this allows it to move through the GI tract – this *decreases the rise in post-prandial glucose* Metabolism: not mentioned
29
Miglitol Side Effects Contraindications Administration
**Alpha-glucosidase inhibitors**: acarbose, miglitol ``` Side Effects: GI disturbances (flatulence) are common because more sugar makes it to your colonic flora ``` Containdications: none mentioned Administration: Oral – typically used as a combination drug
30
What GLP-1 analogs are used to treat DM?
Incretins – GLP-1 agonists: **Exentatide, Ilraglutide – the “tides”**
31
Exentatide MOA T1DM or T2DM?
**Incretins – GLP-1 agonists:** Exentatide, Ilraglutide – the “tides” \*\*\*These drugs will only be useful in T2DM\*\*\* MOA: GLP-1 is secreted by the L-cells in the distal ileum and colon and **increases glucose dependent insulin secretion, decreases glucagon release, decreases gastric emptying, and increases satiety –** *all of these actions decrease postprandial glucose –* THIS DRUG ACTS ON THE GLP-1 RECEPTOR
32
Extentatide
**Incretins – GLP-1 agonists:** Exentatide, Ilraglutide – the “tides” Side Effects: Nausea, vomiting, **pancreatitis, weight loss** (both of these make sense based on the MOA, you’re activating pancreatic cells)
33
Liraglutide MOA T1DM or T2DM? Administration
**Incretins – GLP-1 agonists:** Exentatide, Ilraglutide – the “tides” \*\*\*These drugs will only be useful in T2DM\*\*\* MOA: GLP-1 is secreted by the L-cells in the distal ileum and colon and **increases glucose dependent insulin secretion, decreases glucagon release, decreases gastric emptying, and increases satiety –** *all of these actions decrease postprandial glucose –* THIS DRUG ACTS ON THE GLP-1 RECEPTOR \*\*LIRAGLUTIDE must be injected SC
34
Liraglutide Side effects
**Incretins – GLP-1 agonists:** Exentatide, Ilraglutide – the “tides” Side Effects: Nausea, vomiting, **pancreatitis, weight loss** (both of these make sense based on the MOA, you’re activating pancreatic cells)
35
What DPP-4 inhibitors are used in the treatment of DM?
**Incretins – DPP-4 anatagonists:** Sitagliptin, saxaglipitin, linagliptin, vildaglipitin – the “liptins
36
Linaliptin MOA T1DM or T2DM?
**Incretins – DPP-4 anatagonists:** Sitagliptin, saxaglipitin, linagliptin, vildaglipitin – the “liptins” \*\*\*These drugs will only be useful in T2DM\*\*\* MOA: GLP-1 is secreted by the L-cells in the distal ileum and colon and **increases glucose dependent insulin secretion, decreases glucagon release, decreases gastric emptying, and increases satiety –** *all of these actions decrease postprandial glucose –* **THIS DRUG ACTS TO BLOCK DIPEPTIDYL PEPTIDASE-4 (DPP-4) that BREAKS DOWN GLP-1.**
37
Linagliptin Side Effects
**Incretins – DPP-4 anatagonists:** Sitagliptin, saxaglipitin, linagliptin, vildaglipitin – the “liptins” \*\*\*These drugs will only be useful in T2DM\*\*\* Side Effects: Mild Urinary or Respiratory infections; weight neutral
38
saxagliptin MOA T1DM or T2DM?
**Incretins – DPP-4 anatagonists:** Sitagliptin, saxaglipitin, linagliptin, vildaglipitin – the “liptins” \*\*\*These drugs will only be useful in T2DM\*\*\* MOA: GLP-1 is secreted by the L-cells in the distal ileum and colon and **increases glucose dependent insulin secretion, decreases glucagon release, decreases gastric emptying, and increases satiety –** *all of these actions decrease postprandial glucose –* **THIS DRUG ACTS TO BLOCK DIPEPTIDYL PEPTIDASE-4 (DPP-4) that BREAKS DOWN GLP-1.**
39
Saxagliptin Side Effects
**Incretins – DPP-4 anatagonists:** Sitagliptin, saxaglipitin, linagliptin, vildaglipitin – the “liptins” \*\*\*These drugs will only be useful in T2DM\*\*\* Side Effects: Mild Urinary or Respiratory infections; weight neutral
40
sitagliptin MOA T1DM or T2DM?
**Incretins – DPP-4 anatagonists:** Sitagliptin, saxaglipitin, linagliptin, vildaglipitin – the “liptins” \*\*\*These drugs will only be useful in T2DM\*\*\* MOA: GLP-1 is secreted by the L-cells in the distal ileum and colon and **increases glucose dependent insulin secretion, decreases glucagon release, decreases gastric emptying, and increases satiety –** *all of these actions decrease postprandial glucose –* **THIS DRUG ACTS TO BLOCK DIPEPTIDYL PEPTIDASE-4 (DPP-4) that BREAKS DOWN GLP-1.**
41
Sitagliptin Side Effects
**Incretins – DPP-4 anatagonists:** Sitagliptin, saxaglipitin, linagliptin, vildaglipitin – the “liptins” \*\*\*These drugs will only be useful in T2DM\*\*\* Side Effects: Mild Urinary or Respiratory infections; weight neutral
42
Vildagliptin MOA T1DM or T2DM?
**Incretins – DPP-4 anatagonists:** Sitagliptin, saxaglipitin, linagliptin, vildaglipitin – the “liptins” \*\*\*These drugs will only be useful in T2DM\*\*\* MOA: GLP-1 is secreted by the L-cells in the distal ileum and colon and **increases glucose dependent insulin secretion, decreases glucagon release, decreases gastric emptying, and increases satiety –** *all of these actions decrease postprandial glucose –* **THIS DRUG ACTS TO BLOCK DIPEPTIDYL PEPTIDASE-4 (DPP-4) that BREAKS DOWN GLP-1.**
43
Vildagliptin Side Effects
**Incretins – DPP-4 anatagonists:** Sitagliptin, saxaglipitin, linagliptin, vildaglipitin – the “liptins” \*\*\*These drugs will only be useful in T2DM\*\*\* Side Effects: Mild Urinary or Respiratory infections; weight neutral
44
What Amylin analogs are used in the treatment of DM? T1DM or T2DM?
* *Amylin Analogues** - Pramlinitide * *T1 AND T2 DM**.
45
Pramlinitide MOA
**Amylin Analogues** - Pramlinitide MOA: Amylin is a physiological compound released from the ß-cells in the pancreas. It **Lowers glucagon**, **decreases gastric emptying, and acts on HYPOTHALMUS to promote satiety** (satiety is important in preventing people from eating more and causing an even greater rise in post-prandial glucose)
46
Pramlinitide Side Effects Administration
**Amylin Analogues** - Pramlinitide Side Effects: Hypoglycemia Administration: **SC**
47
What bile-acid sequestrants are used in the treatment of DM?
**Bile-acid sequestrants** – Colesevelam hydrochloride
48
Diazoxide MOA Indication
**Diazoxide** MOA: Anti-hypertensive diuretic that has potent hyperglycemic action by preventing insulin secretion (not synthesis) Indication: Used to treat inoperable insulinomas
49
Octreotide MOA Indication
**Octreotide** MOA: Somatostatin analog – remember somatostatin decreases release of GH, TSH, insulin, and glucagon Indication: Tumors that cause increased release of GH, TSH, insulin, or glucagon
50
What two drugs are used in the treatment of insulin secreting tumors?
**Octreotide** MOA: Somatostatin analog – remember somatostatin decreases release of GH, TSH, insulin, and glucagon Indication: Tumors that cause increased release of GH, TSH, insulin, or glucagon
51
What SGLT2 inhibitors are used in the treatment of DM? T1DM or T2DM?
SGLT2 Inhibitors: **Cingaflozin, Dapagliflozin, Empagliflozin - the "flozins"** T2DM only
52
Canaglifozin MOA
**SGLT2 Inhibitors:** Cingaflozin, Dapagliflozin, Empagliflozin MOA: **Sodium Dependent Glucose Transporters that normally cause 100% glucose reabsorption in the PROXIMAL CONVOLUTED TUBULES of the kidney are inhibited.** This leads to more glucose in the urine (it does not stimulate secretion of glucose in the kidney – this never happens)
53
Canaglifozin Side Effects Contraindications
**SGLT2 Inhibitors:** Cingaflozin, Dapagliflozin, Empagliflozin Side Effects: **INCREASED SERUM KETONE BODIES – LESS GLYCOLYSIS, MORE LIPOLYSIS GLUCOSURIA -\> MORE UTIS, YEAST INFECTIONS, HYPERKALEMIA, AND DEHYDRATION** Containdications: **severe renal impairment, end stage renal disease, patients on dialysis**
54
Dapagliflozin MOA
**SGLT2 Inhibitors:** Cingaflozin, Dapagliflozin, Empagliflozin MOA: **Sodium Dependent Glucose Transporters that normally cause 100% glucose reabsorption in the PROXIMAL CONVOLUTED TUBULES of the kidney are inhibited.** This leads to more glucose in the urine (it does not stimulate secretion of glucose in the kidney – this never happens)
55
Dapagliflozin Side Effects ​Contraindications
**SGLT2 Inhibitors:** Cingaflozin, Dapagliflozin, Empagliflozin Side Effects: **INCREASED SERUM KETONE BODIES – LESS GLYCOLYSIS, MORE LIPOLYSIS GLUCOSURIA -\> MORE UTIS, YEAST INFECTIONS, HYPERKALEMIA, AND DEHYDRATION** Containdications: **severe renal impairment, end stage renal disease, patients on dialysis**
56
Empaglifozin MOA
**SGLT2 Inhibitors:** Cingaflozin, Dapagliflozin, Empagliflozin MOA: **Sodium Dependent Glucose Transporters that normally cause 100% glucose reabsorption in the PROXIMAL CONVOLUTED TUBULES of the kidney are inhibited.** This leads to more glucose in the urine (it does not stimulate secretion of glucose in the kidney – this never happens)
57
Empagliflozin Side Effects ​Contraindications
**SGLT2 Inhibitors:** Cingaflozin, Dapagliflozin, Empagliflozin Side Effects: **INCREASED SERUM KETONE BODIES – LESS GLYCOLYSIS, MORE LIPOLYSIS GLUCOSURIA -\> MORE UTIS, YEAST INFECTIONS, HYPERKALEMIA, AND DEHYDRATION** Containdications: **severe renal impairment, end stage renal disease, patients on dialysis**
58

Endocrine - Pharmacology (5 decks)

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