Antidiabetics Flashcards
1
Q
Insulin lispro, Insulin aspart, Insulin glulisine
A
Rapid acting insulins
2
Q
Regular insulin
A
Short acting insulin
3
Q
NPH, Isophane Insulin
A
Intermediate-acting insulin
4
Q
Insulin glargine, Insulin detemir
A
Long-acting insulin
5
Q
Glucagon
A
- Polypeptide hormone from pancreatic a-cells
- Regulates homeostasis of glucose/amino acids/possibly FFA. Inc blood glucose by mobilizing hepatic glycogen (when it is available).
- Juveniles respond less favorably than adults, not effective in pts w/reduced glycogen stores, potent inotropic and chronotropic effects on heart, profound relaxation of intestine.
- SC/IM/IV admin, gradual onset
6
Q
Diazoxide
A
- Non-diuretic thiazide, vasodilator, and hyperglycemic
- Produces dose related hyperglycemia by directly inhibiting insulin secretion or possibly dec peripheral glucose utilization or stimulating glucose production
- Tx in pts w/insulinoma
- Oral admin, long duration of action
- SE: closely watched for OD (hyperglycemia, DKA, non-ketotic hyperosmolar coma), Na/H2O retention, hypotension, GI irritation, Hyperuircemia, Thrombocytopenia, neutropenia, excessive hair growth (most often in children)
7
Q
Sulfonylureas
A
- Binds/blocks ATP sensitive K channel to depolarize membrane and inc Ca influx on B cells
- Primary mechanism is to stimulate insulin release from B cells, reduce serum glucagon, indirectly potentiate action of insulin on target tissues
- oral admin
- SE: hypoglycemia (longer t1/2 greater incidence), some GI effects, wt. gain
- CI: sever renal disease/hepatic dysfunction, sulfa allergies
8
Q
Tolbutamide, Chlorpropamide, Tolazamide
A
- First generation sulfonylureas
- Tolbutamide: t1/2 4-5 hrs, infrequent hypoglycemia, safest in elderly of 1st gen, rare toxic rxns, inexpensive
- Chlorpropamide: t1/2 32hrs, disulfiram like effect
9
Q
Glyburide, Glipizide, Glimepiride
A
- 2nd gen sulfonylureas
- Glyburide: effect lasts 24hrs, hypoglycemia possible (worst for 2nd gen), CI in hepatic impairment/renal insufficiency.
- Glipizide: t1/2 2-4hrs (least hypoglycemic), XR version is 24hrs
- Glimepiride: most potent sulfonylurea, once a day dosing, some cardioprotective effects, little hypoglycemia.
10
Q
Repaglinide, Nateglinide
A
- Meglitinides, not sulfonylureas-can be used in SA allergy
- Receptors on K channels-increase insulin release
- Tx: lower postprandial serum glucose
- rapid, short action, miics endogenous insulin patterns better
- lowers HbA1c glycosylation (Repaglinide more effective)
- not much wt gain - Oral, rapid acting (peak effect in 1 hr)
- short action
- liver metabolism (CYP3A4) - SE: Hypoglycemia
- CI: don’t combine w/sulfonylureas
- caution in liver impairment
- hypoglycemia
- pregnancy (class C) and breast feeding
11
Q
Metformin
A
- Biguanide, does not release insulin, DOC for type2 DM
- Increased glucose removal from blood
- slowing of glucose absorption from GI, inc lactate conversion by enterocytes
- Reduction of plasma glucagon levels
- Reduced gluconeogenesis - Tx: Reduction of glucose to a euglycemic state (normal pts not affected, lowers postprandial hyperglycemia)
- safe for kids >10
- DOC for DM2 because does not inc body wt, reduces macrovascular events. - Renal excretion, oral admin, t1/2 6hrs
- SE: Hypoglycemia if combined w/sulfonylurea or insulin
- Lactic acidosis
- Diarrhea/anorexia/nausea/vomitting
- Reduced B12 absoprtion - CI: Lactic acidosis conditions-
- Renal disease
- Hepatic disease
- Alcoholism
- Diseases predisposing to tissue hypoxia!!!!! (CHF, COPD)
- Pregnancy/breast feeding
12
Q
Pioglitazone, Rosiglitazone
A
- Thiazolidinediones (glitizones), insulin sensitizers
- Ligands of nuclear PPARy receptor which can cause post-receptor insulin mimetic action (inc glucose transporter synthesis in adipose, onset/offset can take weeks-months)
- do not stim insulin secretion - Tx: lowers insulin resistance
- Decreased triglycerides in long term use, slight inc in HDL
- potential reduction in development of DM2
- Improved glycemic control (reduced fasting glucose, modest reduction in HbA1c) - Oral 1-2x/day, wide variation in t1/2, liver metabolism
- SE: wt gain
- back pain, fatigue, HA
- hypoglycemia (slight)
- Edema (inc risk of HF in CHF)
- Rosiglitazone: black box warning for inc risk of MI/angina - CI: caution w/hepatic toxicity
- CHF!!!!!!
- Class C pregnancy
13
Q
Acarbose, Miglitol
A
- Alpha-glucosidase inhibitors, reduce glucose absorption, used as diet aide in DM1 and DM2
- Inhibit a-glucosidase in enterocytes, results in delayed carb digestion/absorption
- Tx: lower postprandial glucose alone or in combination
- minimal effects on fasting glucose/modest dec in HbA1c/potential dec in triglycerides
- no significant effects on weight - Admin oral, metabolism via digestive enzymes/intestinal microorganisms, t1/2 is 2hrs
- SE: Frequent GI effects (flatulence)
- elevated hepatic enzymes/jaundice - CI: Breast feeding
- GI disease/obstruction/IBD/hiatal hernia
- Hepatic disease
- Renal impairment
14
Q
Exenatide, Liraglutide, Dulaglutide
A
- Incretin Mimetics
- GLP-1 agonists, resistant to enzymatic degradation by DPP-IV
- Tx: lower postprandial and fasting glucose alone are in combination
-promotes better glycemic control, modest dec in HbA1c
-Potential inc B cell number and function
-Slows gastric emptying
-wt loss, at worst wt neutral - Exenatide: SC injections 60min before 2 main meals
Liraglutide: single daily SC injection
Dulaglutide: once/weekly SC injection - SE: GI disturbance, N/V/D
-hypoglycemia
-hypersensitivity rxns
-Exenatide may cause acute pancreatitis, inc risk of pancreatic and thyroid cancer - CI: slow GI problems, GI disease, oral meds that cannot be exposed too long, renal impairment, pregnancy class C
-Liraglutide Black Box warning of Thyroid cancer
15
Q
Sitagliptin, Saxagliptin, Linagliptin, Alogliptan
A
- DDP-IV inhibtors, “gliptans”
- Potentiates effects of incretin hormones by inhibiting their breakdown
- Tx: lower postprandial and fasting glucose alone or in combination, modest dec in HbA1c
- No significant effects on weight - Oral admin, 1/day
- SE: Hypersensitivity rxns,
- Sitagliptin may cause acute pancreatitis/pancreatic cancer - CI: Slow GI problems, renal impairment, Breast feeding/pregnancy (Class C)
