Difference between revisions of "Diabetes medications"

(Thiazolidinediones)
 
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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 creatinine > 1.4 (GFR <40), CHF, hepatic insufficiency, ETOH abuse
 
*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
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==Sulfonylureas==
 
==Sulfonylureas==
*Increases insulin secretion (glipizide, glyburide)
+
*[[Glipizide]], [[glyburide]]
*[[Hypoglycemia]] is the major adverse effect (esp with glyburide)
+
*Increase insulin secretion
 +
*[[Hypoglycemia]] is the major adverse effect (especially with glyburide)
  
 
==Alpha Glucosidase Inhibitors==
 
==Alpha Glucosidase Inhibitors==
*acarbose, miglitol, voglibose
+
*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
+
*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
*does not affect lactose absorption
+
*Taken with first bite of each meal  
*if hypoG- sucrose/ table sugar will not work- use glucose- PO or IV
+
*Since limited absorption, stays in gut and side effects mostly GI- bloating, gas, [[diarrhea]]
*taken with first bite of each meal  
+
**acarbose- can cause transaminitis/ liver inj
*since limited absorption, stays in gut and side effects mostly GI- bloating, gas, diarrhea
+
*Contraindications- [[cirrhosis]], [[IBD]], malabsorption syndrome
*contraindications- cirrhosis, IBD, malabsorption synd
+
*Do not cause [[hypoglycemia]] when used as monotherapy
*alpha glucs do not cause hypoG when used as monotreatment
+
**If [[hypoglycemia|hypoglycemic]]- sucrose/ table sugar will ''not'' work- use glucose- PO or IV
*acarbose- can cause transaminitis/ liver inj
+
*Since minimal absorption- systemic toxicity from OD unlikely
*since minimal absorption- systemic toxicity from OD unlikely
 
  
 
==Thiazolidinediones==
 
==Thiazolidinediones==
*rosiglitazone and poiglitazone
+
*Rosiglitazone and poiglitazone
*enhance insulin effect on muscle, fat, liver without increasing pancreatic insulin secretion
+
*Enhance insulin effect on muscle, fat, liver without increasing pancreatic insulin secretion
*protein bound and hepatic metabolism - avoid in patients with liver disease
+
*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)
+
*Side effects- induces ovulation, decreases effectiveness of OCP's, increases plasma volume (bad if CHF)
  
 
==Benzoic Acid Derivatives==
 
==Benzoic Acid Derivatives==
*repaglinide- mono or combined with metformin
+
*Repaglinide- monotherapy or combined with metformin
 
*binds to ATP dependent potassium channel like sulfonyls but at different site.
 
*binds to ATP dependent potassium channel like sulfonyls but at different site.
*Unlike sulfonyls, it decreases insulin lvls
+
*Unlike sulfonyls, it ''decreases'' insulin levels
*Dose 30 min before meal to decrease post prandial hyperglycemia
+
*Dose 30 min before meal to decrease postprandial hyperglycemia
  
 
==[[GLP-1 agonists]]==
 
==[[GLP-1 agonists]]==
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==[[DPP-4 inhibitors]]==
 
==[[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]]==
 
==[[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==

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

  • Aspart (Novolog)
  • Lispro (Humalog)
15-30min 1-2h 3-5h
Short-acting insulin

  • Regular
30-60min 2-4h 6-10h
Intermediate-acting insulin

  • NPH (Humulin, Novolin)
1-3h 4-12h 18-24h
Long-acting insulin

  • Glargine (Lantus)
2-4h None 24h
Sulfonylurea

  • Glimepiride
  • Glipizide (Glucotrol)
  • Glyburide (Glycron, Micronase)
2-6h 12-24h

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

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

See Also

References