Diabetes Meds Flashcards
MOA of acarbose and miglitol
inhibit intestinal alpha-glucosidase which prevent uptake of glucose
MOA of insulin replacement therapy
- activate insulin receptor
- regular insulin is short acting
- NPH insulin and lente insulin (zinc crystal) are intermediate acting
- insulin lispro (humalog), insulin aspart (novolog), insulin glulisine (apidra) are all rapid acting with faster onset of action and shorter onset of action than regular insulin and don’t form hexamers.
- insulin glargine and insulin detemir are both long acting with slow absorption.
- inhaled insulin–exubera
- insulin pump-esp good for young children
What is ketoacidosis and how do you treat it?
- caused by low insulin. You have incresed release of Fatty acids that vause increased ketone bodies –> acidosis.
- you also get hyperglycemia d/t hepatic gluconeogenesis
- tx with insulin
What is hypoglycemic coma and how do you treat it?
- caused by insulin overdose
- so common that all comatose pts are given glucose first while glucose being measured!!
- tx is with glucose!
What is normal hbA1c levels?
What are early symptoms of hypoglycemia?
- confused, dizzy, shaky, hungry, headache, irritable
- heart pounding/racing pulse, pale skin, sweaty, trembling, weak, anxious
What are severe symptoms of hypoglycemia?
- headache, irritable, poor coordination and concentration
- nubness in mouth and tongue, pass out, nightmares, coma
MOA of sulfonylureas and drug examples
- Increase insulin secretion from pancreatic beta cells by closing ATP sensitive K channels causing depolarization
- increase insulin sensitivity by enhancing the effect of insulin on glucose uptake
- examples include glyburide, glipizide, glizlazide, & glimepiride
- These have intermediate duration of action.
MOA of meglitinides and drug examples
- increase insulin secretion from pancreatic beta cells by closing ATP sensitive K channels causing depolarization
- drug examples include repaglinide and nateglinide
- these are fast acting insulin secretagogues
Problem with long term use of sulfonylureas?
-Initially increase insulin release but with long term tx, may decrease insulin metabolism by liver
What are the side effects of the insulin secretagogues like sulfanylureas and meglitides??
hypoglycemia and weight gain
MOA Of biguanides and drug examples
- decrease endogenous glucose production by acting on AMP kinase; does not affect insulin secretion so doesn’t cause hypoglycemia
- metformin and phenformin. phenformin is more potent than metformin so it has been withdrawn d/t lactic acidosis.
Side effects of biguanides?
GI disturbances, lactic acidosis (don’t give to alcohol abusers)
MOA of thiazolidinediones and examples of drugs
- bind to PPARy (peroxisome proliferator-activated reciptor-y)
- INCREASE INSULIN SENSITIVITY
- Increase glucose transport into muscle and adipose tissue
- rosiglitazone, pioglitazone, troglitazone (this one withdrawn d/t severe liver toxicity)
Side effects of thiazolidinediones?
- fluid retention, edema, weight gain, anemia, bone fx in women,
- may worsen heart dz and increase risk of MI
MOA of acarbose and miglitol?
Inhibit intestinal alpha-glucosidase
- reduce uptake of carb and reduce post prandial glucose rise
- used in combo with other hypoglycemics and/or insulin
Function of Somatostatin and examples of drugs
- inhibit release of TSH and GH from pituitary
- inhibit release of insulin AND glucagon from pancreas
- octreotide is a long acting somatostatin analogue used in glucagonomas. It’s also used to controle xcess secretion of GH (acromegaly)
What drug is used to treat inoperable insulinomas and its MOA?
- diazoxide which is an antihypertensive antidiuretic with potent hyperglycemic actions
- inhibits insulin secretion but not insulin synthesis so insulin builds up in beta cells.
Function of GLP-1
- increase glucose dependent insulin secetion
- inhibit glucagon stimulated glycogenolysis
- slows gastric emptying
- decrease glucagon secretion
- all these decrease postprandial blood glucose
MOA of incretin-based drugs and examples of drugs
- exanatide, liraglutide, dulaglutide- analog of GLP-1 and activates GLP-1 receptors
- sitagliptin, saxagliptin, linagliptin- inhibitor of the dipeptidyl peptidase-4 (DPP4) that degrades GLP-1 and other incretins
- inhibits glucagon-stimulated glycogenolysis in the liver and may preserve or increase production of new beta-cells in the pancreas.
**Exanatide was isolated from Gila monster venom
Amylin analog MOA and examples of drugs
- activate amylin receptors
- pramlintide, symlin
- amylin is released by beta cells of pancreas along with insulin after a meal. it is deficient like insulin in T1DM.
- augments endogenous amylin and aids in the absorption of glucose by slowing gastric emptying, promote satiety via hypothalamic recepors, and inhibiting inappropriate secretion of glucagon
- tx results in weight loss yay
Cinagliflozin (Invokana) MOA
- SGLT2 (sodium dependent glucose cotransporter) inhibitor. These glucose transporters are found in intestinal mucosal cells SGLT1 and the proximal tubule of nephron SGLT2
- 100% OF filtered glucose must be reabsorbed through prox tubules. In t1dm, glucose is excreted in urine because SGLT is saturated.
**- Decrease reabsorption of glucose in kidney but does not stimulate secretion **
Side effects of SGLT2 inhibitors?
- hypotension, hyperkalemia, hypoglycemia, increases LDL cholesterol
Contraindications for SGLT2 inhibitors:
- severe renal impairment, ESRD, patients on dialysis
Colesevelam hydrochloride MOA and side effects
- bile acid sequestrant that was developed to lower blood cholesterol
- lowers HbA1C 0.5% and lowers LDL cholesterol 15%
- interrupts enterohepatic cycling and lower Farnesoid X receptor activation
- SIde effects: GI
