Difference between revisions of "Diabetes medications"

(Biguanides (Metformin))
 
(21 intermediate revisions by 8 users not shown)
Line 1: Line 1:
 
==Background==
 
==Background==
#Hypoglycemics
+
*Hypoglycemics
##Sulfonylureas
+
**Sulfonylureas
##Benzoic acid derivatives
+
**Benzoic acid derivatives
#Antihyperglycemics
+
*Antihyperglycemics
##Biguanides
+
**Biguanides
##Alpha glucosidase inhibitors
+
**Alpha glucosidase inhibitors
##Thiazolidinediones
+
**Thiazolidinediones
 +
 
 +
{{Common Anti-hyperglycemic Drugs and Pharmacology}}
  
 
==[[Insulin]]==
 
==[[Insulin]]==
  
 
==Biguanides (Metformin)==
 
==Biguanides (Metformin)==
#Suppresses liver glucose production
+
Suppresses liver glucose production
#Metformin 500mg PO BID is first-line agent for type II diabetics
+
===Dose===
##Do not prescribe if Cr > 1.4 (GFR <40), CHF, hepatic insufficiency, ETOH abuse
+
[[Metformin]] 500mg PO BID is first-line agent for type II diabetics
##Should be withheld for 48hr after IV contrast
+
*Do not prescribe if creatinine > 1.4 (GFR <40), CHF, hepatic insufficiency, ETOH abuse
#Side Effects
+
*Should be withheld for 48hr after IV contrast
##Lactic acidosis (due to increased lactate production)
+
===Side Effects===
###Seen almost exclusively in pts with renal failure
+
*Lactic acidosis (due to increased lactate production)
###Signs of lactic acidosis: nausea/vomiting, abd pain, tachypnea, lethargy
+
**Seen almost exclusively in patients with renal failure
##Nausea, diarrhea, crampy abdominal pain
+
*Nausea, diarrhea, crampy abdominal pain
#Toxicity
+
===Toxicity===
##Almost never causes hypoglycemia when taken alone, but can exacerbate hypoglycemia when taken in combination with hypoglycemic agents
+
*Almost never causes hypoglycemia when taken alone, but can exacerbate hypoglycemia when taken in combination with hypoglycemic agents
##Toxic dose unknown
+
*Toxic dose unknown
##Management: Supportive care
+
*Management: Supportive care
  
 
==Sulfonylureas==
 
==Sulfonylureas==
#Increases insulin secretion (glipizide, glyburide)
+
*[[Glipizide]], [[glyburide]]
#Hypoglycemia is the major adverse effect (esp w/ 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]]
#take these meds with each meal with first bite
+
**acarbose- can cause transaminitis/ liver inj
#since limited aborption, 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 monotx
+
**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 min absorption- systemic tox from OD unlikely
 
  
 
==Thiazolidinediones==
 
==Thiazolidinediones==
#rosiglitazone and poiglitazone
+
*Rosiglitazone and poiglitazone
#enhance insulin effect on muscle, fat, liver without increasing panc insulin secretion
+
*Enhance insulin effect on muscle, fat, liver without increasing pancreatic insulin secretion
#protein bound and hep metab- not good if liver dz
+
*Protein bound and hepatic metabolism - avoid in patients with liver disease
#side effects- induce ovulation, increase plasma vol bad if CHF, decrease effectiveness of OCP's
+
*Side effects- induces ovulation, decreases effectiveness of OCP's, increases plasma volume (bad if CHF)
  
 
==Benzoic Acid Derivatives==
 
==Benzoic Acid Derivatives==
#repaglinide- mono or combo tx c 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]]==
 +
*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==
 
*[[Diabetes Mellitus (Main)]]
 
*[[Diabetes Mellitus (Main)]]
  
==Source ==
+
==References==
Tintinalli
+
<references/>
  
[[Category:Endo]]
+
[[Category:Endocrinology]]
[[Category:Drugs]]
+
[[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

  • 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