antidiabetic agents II Flashcards
List the Meglitinides
- Repaglinide
- Nateglinide
MOA of Meglitinides
- bind and block ATP-sensitive K+ channel to cause membrane depolarization and increase Ca2+ influx on B cells
which Antidiabetic Agents can be used in sulfa allergy
Meglitinides
therapeutic effects of Meglitinides
- decrease postprandial serum glucose
- decrease HbA1c
route of administration and onset of action of meglitinides
- oral, preprandially
- rapid action; peak effect at 1 hour
MOA of Metformin (Glucophage)
- increase glucost uptake (muscle and adipose tissue)
- decrease glucose absorption from GI
- decrease glucagon
- decrease gluconeogenesis
drug of choice for Type 2 diabetics
-
Metformin
- does not increase body weight
- Reduces CV problems
theraputic effects of Metformin (Glucophage)? is glucose lowered in normal subjects
- overall effect: decrease glucose levels
- glucose is not lowered in normal subjects
- decreases postprandial hyperglycemia
can metformin be used in children
safe for use in children > 10 years old
adverse effects of metformin
- lactic acidosis
- diarrhea
contraindications to taking metformin
- lactic acidosis conditions
- renal disease
- hepatic disease
- alcoholism
- disease predisposing to tissue hypoxia (CHF, COPD)
List the Thiazolidinediones
- Pioglitazone
- Rosiglitazone
MOA of Thiazolidinediones
- “insulin sensitizers”-> increase insulin sensitivity
- ligands of the nuclear PPARy receptor -> post receptor insulin-mimetic action
theraputic effects of Thiazolidinediones
- lowers insulin resistance
- reduces the development of type 2 DM -> prophylatic use
adverse effects of Thiazolidinediones
- weight gain
- edema: increase in risk of heart failure in CHF patients
- rosiglitazone black lavel warning for increased incidence of MI and angina
contraindications to taking Thiazolidinediones
- hepatic disease
- CHF
List the alpha-glucosidase inhibitors
- Acarbose
- Miglitol
MOA of alpha-glucosidase inhibitors
delayed carbohydrate digestion and absorption
theraputic effects of alpha-glucosidase inhibitors
- Effectively lower postprandial serum glucose
- Has minimal effects on fasting glucose
- Modest decreases in HbA1c glycosylation
- No significant effects on weight
adverse effects of alpha-glucosidase inhibitors
- flatulence
oral glucose stimulates release of the incretins:
- glucagon-like peptide (GLP-1)
- glucose dependent insulinotropic peptide (GIP)
function of GLP-1 and GIP
- increase release of insulin
- GLP-1 inhibits glucagon release -> decreased hepatic gluconeogenesis
List the GLP-1 Incretin Mimetics
- Exenatide
- Liraglutide
- Dulaglutide
- Albiglutide
incretin mimetics are resistant to enzymatic degradation by
DPP-IV
route of administration of GLP-1 mimetics
S.C.
theraputic effects of incretic mimetics
- lowers postprandial and fasting serum glucose
- potential increased B cell number and function
- weight loss
adverse effects of Incretin mimetics
- acute pancreatitis
contraindications to taking Incretin mimetics: Liraglutide
- thyroid CA -> black box warning
list the Dipeptidyl-peptidase-IV (DPP-IV) inhibitors
- Sitagliptin
- Saxagliptin
- Linagliptin
- Alogliptin
MOA of Dipeptidyl-peptidase-IV (DPP-IV) inhibitors
- potentiates the effects of incretin hormones, by inhibiting thier breakdown by DPP-IV
theraputic effects of Dipeptidyl-peptidase-IV (DPP-IV) inhibitors
- lowers postprandial and fasting serum glucose
- has no significant effects on weight
how are Dipeptidyl-peptidase-IV (DPP-IV) inhibitors administered
orally, once a day
adverse effects of Dipeptidyl-peptidase-IV (DPP-IV) inhibitors
- acute pancreatitis
- pancreatic CA
MOA and use of Pramlintide
-
synthetic analog of amylin, a hormone co-secreted with insulin
- used as an adjuct to insulin therapy in type 1 and type 2 DM
-
regulates postprandial glucose by
- decrease gastric empyting
- centrally mediated modulation of appetite
theraputic effects of Pramlintide
weight loss
MOA of Bromocriptine
- Dopamine agonist
- reduction in postmeal plasma glucose levels due to enhanced suppression of hepatic glucose production
therapeutic effects of Bromocriptine
- no AM glucose surge
- decrease fasting and postprandial free fatty acid and triglyceride levels
- reduces the cardiovascular end point problems in diabetics
MOA of Colesevelam
- bile acid binding resin
- MOA unknown
adverse effects of Colesevelam
- constipation and bloating
List the SGLT2 inhibitors
- Canagliflozin
- Dapagliflozin
- Empagliflozin
MOA of SGLT2 inhibitors
- Inhibits the sodium-glucose co-transporter 2 (SGLT2) in the kidney
- Blocks the reabsorption of glucose by the kidney, which results in increased glucose excretion and lower blood glucose concentrations in patients with type 2 diabetes mellitus
adverse effects of SGLT2 inhibitors
- female genital mycotic infections, UTIs and increased urinary frequency
which antidiabetic drugs cause episodes of hypoglycemia
- sulfonylureas
- meglitinides
which antidiabetic drugs cause episodes of hyperinsulinemia
- sulfonylureas
- meglitinides
Which of the Antidiabetic drugs cause weight gain
- sulfonylureas
- thiazolidinediones
Which of the Antidiabetic drugs causes weight loss
- incretin mimetics
- pramlintide