Diabetes medications: Difference between revisions
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Suppresses liver glucose production | Suppresses liver glucose production | ||
===Dose=== | ===Dose=== | ||
Metformin 500mg PO BID is first-line agent for type II diabetics | [[Metformin]] 500mg PO BID is first-line agent for type II diabetics | ||
*Do not prescribe if | *Do not prescribe if creatinine > 1.4 (GFR <40), CHF, hepatic insufficiency, ETOH abuse | ||
*Should be withheld for 48hr after IV contrast | *Should be withheld for 48hr after IV contrast | ||
===Side Effects=== | ===Side Effects=== | ||
Line 28: | Line 28: | ||
==Sulfonylureas== | ==Sulfonylureas== | ||
* | *[[Glipizide]], [[glyburide]] | ||
*Hypoglycemia is the major adverse effect ( | *Increase insulin secretion | ||
*[[Hypoglycemia]] is the major adverse effect (especially with glyburide) | |||
==Alpha Glucosidase Inhibitors== | ==Alpha Glucosidase Inhibitors== | ||
* | *Acarbose, miglitol, voglibose | ||
* | *Competitively and reversibly inhibit alpha glucosidase brush border hydrolase enzyme- makes postprandial decrease in carbohydrate absorption since complex polysaccharides not broken down into absorbable monosaccharides. Does not affect lactose absorption | ||
*Taken with first bite of each meal | |||
* | *Since limited absorption, stays in gut and side effects mostly GI- bloating, gas, [[diarrhea]] | ||
**acarbose- can cause transaminitis/ liver inj | |||
* | *Contraindications- [[cirrhosis]], [[IBD]], malabsorption syndrome | ||
* | *Do not cause [[hypoglycemia]] when used as monotherapy | ||
* | **If [[hypoglycemia|hypoglycemic]]- sucrose/ table sugar will ''not'' work- use glucose- PO or IV | ||
* | *Since minimal absorption- systemic toxicity from OD unlikely | ||
* | |||
==Thiazolidinediones== | ==Thiazolidinediones== | ||
* | *Rosiglitazone and poiglitazone | ||
* | *Enhance insulin effect on muscle, fat, liver without increasing pancreatic insulin secretion | ||
* | *Protein bound and hepatic metabolism - avoid in patients with liver disease | ||
* | *Side effects- induces ovulation, decreases effectiveness of OCP's, increases plasma volume (bad if CHF) | ||
==Benzoic Acid Derivatives== | ==Benzoic Acid Derivatives== | ||
* | *Repaglinide- monotherapy or combined with metformin | ||
*binds to | *binds to ATP dependent potassium channel like sulfonyls but at different site. | ||
*Unlike sulfonyls, it decreases insulin | *Unlike sulfonyls, it ''decreases'' insulin levels | ||
*Dose 30 min before meal to decrease | *Dose 30 min before meal to decrease postprandial hyperglycemia | ||
==[[GLP-1 agonists]]== | |||
*Exanatide (Byetta and Bydureon), Liraglutide (Victoza) | |||
*Synthetic glucagon-like peptide-1 (GLP-1) receptor agonists | |||
*Stimulates insulin release from pancreatic islet cells | |||
*May promote weight loss by slowing gastric emptying and increasing satiety | |||
==[[DPP-4 inhibitors]]== | |||
*Sitagliptin, saxagliptin, linagliptin, alogliptin | |||
*Block DPP-4, which leads to increased activity of incretins, which inhibit glucagon release, which in turn increase insulin secretion and slow gastric emptying, ultimately decreasing blood glucose levels | |||
*Potential serious adverse events include acute [[pancreatitis]], [[anaphylaxis]]/[[angioedema]], [[SJS]] | |||
==[[SGLT-2 inhibitors]]== | |||
*Canagliflozin (Invokana), Dapagliflozin (Farxiga), Empagliflozin (Jardiance) | |||
*Inhibit sodium-glucose cotransporter 2, decreasing glucose reabsorption in the proximal tubule | |||
*Potential serious adverse event: euglycemic [[DKA]] | |||
==See Also== | ==See Also== | ||
Line 59: | Line 75: | ||
==References== | ==References== | ||
<references/> | |||
[[Category:Endocrinology]] | [[Category:Endocrinology]] | ||
[[Category:Pharmacology]] | [[Category:Pharmacology]] |
Latest revision as of 15:44, 28 September 2019
Background
- Hypoglycemics
- Sulfonylureas
- Benzoic acid derivatives
- Antihyperglycemics
- Biguanides
- Alpha glucosidase inhibitors
- Thiazolidinediones
Common Anti-hyperglycemic Drugs and Pharmacology
Drug | Pharmacology | ||
---|---|---|---|
Onset | Peak | Duration | |
Rapid-acting insulin
|
15-30min | 1-2h | 3-5h |
Short-acting insulin
|
30-60min | 2-4h | 6-10h |
Intermediate-acting insulin
|
1-3h | 4-12h | 18-24h |
Long-acting insulin
|
2-4h | None | 24h |
Sulfonylurea
|
– | 2-6h | 12-24h |
See also GLP-1 agonists
Insulin
Biguanides (Metformin)
Suppresses liver glucose production
Dose
Metformin 500mg PO BID is first-line agent for type II diabetics
- Do not prescribe if creatinine > 1.4 (GFR <40), CHF, hepatic insufficiency, ETOH abuse
- Should be withheld for 48hr after IV contrast
Side Effects
- Lactic acidosis (due to increased lactate production)
- Seen almost exclusively in patients with renal failure
- Nausea, diarrhea, crampy abdominal pain
Toxicity
- Almost never causes hypoglycemia when taken alone, but can exacerbate hypoglycemia when taken in combination with hypoglycemic agents
- Toxic dose unknown
- Management: Supportive care
Sulfonylureas
- Glipizide, glyburide
- Increase insulin secretion
- Hypoglycemia is the major adverse effect (especially with glyburide)
Alpha Glucosidase Inhibitors
- Acarbose, miglitol, voglibose
- Competitively and reversibly inhibit alpha glucosidase brush border hydrolase enzyme- makes postprandial decrease in carbohydrate absorption since complex polysaccharides not broken down into absorbable monosaccharides. Does not affect lactose absorption
- Taken with first bite of each meal
- Since limited absorption, stays in gut and side effects mostly GI- bloating, gas, diarrhea
- acarbose- can cause transaminitis/ liver inj
- Contraindications- cirrhosis, IBD, malabsorption syndrome
- Do not cause hypoglycemia when used as monotherapy
- If hypoglycemic- sucrose/ table sugar will not work- use glucose- PO or IV
- Since minimal absorption- systemic toxicity from OD unlikely
Thiazolidinediones
- Rosiglitazone and poiglitazone
- Enhance insulin effect on muscle, fat, liver without increasing pancreatic insulin secretion
- Protein bound and hepatic metabolism - avoid in patients with liver disease
- Side effects- induces ovulation, decreases effectiveness of OCP's, increases plasma volume (bad if CHF)
Benzoic Acid Derivatives
- Repaglinide- monotherapy or combined with metformin
- binds to ATP dependent potassium channel like sulfonyls but at different site.
- Unlike sulfonyls, it decreases insulin levels
- Dose 30 min before meal to decrease postprandial hyperglycemia
GLP-1 agonists
- Exanatide (Byetta and Bydureon), Liraglutide (Victoza)
- Synthetic glucagon-like peptide-1 (GLP-1) receptor agonists
- Stimulates insulin release from pancreatic islet cells
- May promote weight loss by slowing gastric emptying and increasing satiety
DPP-4 inhibitors
- Sitagliptin, saxagliptin, linagliptin, alogliptin
- Block DPP-4, which leads to increased activity of incretins, which inhibit glucagon release, which in turn increase insulin secretion and slow gastric emptying, ultimately decreasing blood glucose levels
- Potential serious adverse events include acute pancreatitis, anaphylaxis/angioedema, SJS
SGLT-2 inhibitors
- Canagliflozin (Invokana), Dapagliflozin (Farxiga), Empagliflozin (Jardiance)
- Inhibit sodium-glucose cotransporter 2, decreasing glucose reabsorption in the proximal tubule
- Potential serious adverse event: euglycemic DKA