Diabetez Drugz Flashcards
regular insulin
- -insulin lispro → rapid-acting
- –aspart (fast part)
- –glulisine (gasoline)
rapid & short-acting insulin
- clear solution → ok for IV
- contain Zn to ↑ stability and 1/2 life
- 5 min 1/2 life w/ uncomplicated diabetes
- DOC for ketoacidotic coma
NPH or isophane insulin
intermediate acting insulin
-unusable for IV admin
Insulin gLARGinE
insulin Determir
long-acting insulin
-unusable for IV
Glargine:
-at pH 4 in solution → precipitates in body (↑ duration)
Determir
-myristoylated → binds albumin (↑ 1/2 life)
Diazoxide
Non-diuretic thiazide, vasodilator, *hyperglycemic
–opens K channels → hyperpolarize → ↓ insulin ↑ glucose
-treat insulinoma
Adverse:
- hyperglycemia w/ ketoacidosis
- or non-ketotic hyperosmolar coma
- hyperuricemia
- Na & H2O retention
- thrombocytopenia & neutropenia
- excessive hair growth in children
Metformin
Biguanides–does not release insulin
AMPK
- ↑ glucose uptake (↑ insulin action at fat & muscle)
- ↓ glucose absorption from GI
- -↑ lactate conversion by enterocyte
- ↓ plasma glucagon
- ↓ gluconeogenesis
- **initial DOC for DM2
- -*no weight gain
- -↓ macrovascular events → *cardioprotective
- safe for children >10 yrs
- ↓ glucose levels to euglycemic state
- -not ↓ in normal subjects
- -↓ postprandial hyperglycemia
- ↓ plasma TG levels
Adverse:
- Lactic acidosis
- **Diarrhea (gets better w/ time)
CI:
- Lactic acidosis conditions
- -renal / hepatic / alcoholism
- -CHF, COPD (predisposing to tissue hypoxia)
Rapaglinide
–Nateglinide
Meglitinide
- receptors on K+ channels → ↑ insulin release
- -can be used in SA allergy
- take before meals
- -effectively ↓ postprandial serum glucose
- ↓ HbA1c
- rapid, short action → mimics endogenous insulin better
- not much effect on weight
CI:
- dont combine w/ Sulfonylureas
- liver impairment
- may cause hypoglycemia
- pregnancy
Tolbutamide
1st gen. Sulfonylurea
-1º mxn → stimulate insulin release
- safest in elderly *for 1st gen
- short 1/2 life → infrequent hypoglycemia (least overall)
- binds & blocks ATP-sensitive K channel → depolarize
- → ↑ Ca influx in B cells → ↑ insulin release
- -indirectly potentiates action of insulin on target tissues
Adverse:
- hypoglycemia (↑ risk w/ ↑ 1/2 life)
- **weight gain
- depress thyroid function
CI: severe renal disease or hepatic dysfunction
-allergy to sulfa drugs
–Chlorpropamide
1st gen. Sulfonylurea
-1/2 life 32 hours → WORST hypoglycemia
Glipizide
2nd gen. Sulfonylurea
- 2-4 hr 1/2 life → **least hypoglycemic effect of 2nd’s
- CI hepatic impairment & renal insufficiency
Glyburide
Glimepiride
2nd gen. Sulfonylurea
- effect lasts 24 hrs → may cause hypoglycemia
- -worst hypoglycemia of 2nd’s
- CI hepatic impairment & renal insufficiency
Glimepiride
- most potent (1/day dose)
- cardioprotective
- little hypoglycemic
Pioglitazone
- Rosiglitazone
- class?
Insulin sensitizers (Thiazolidinedione)
- ligands for PPAR → post-receptor insulin-mimetic action
- -↑ glucose transporter synthesis in adipose
- -onset & offset of action → week to months
- ↓ insulin resistance**
- ↓ TG in long term & small ↑ HDL
- potential reduce development of type 2 DM (prophylaxisis)
- improved glycemic control
Adverse:
- Edema → ↑ risk of heart failure in pre w/ CHF or who are prone to it
- weight gain (may be edema)
CI:
- hepatic disease
- CHF
- pregnancy (category C)
Acarbose
-Miglitol
Alpha-glucosidase inhibitors
- inhibit alpha glucosidases on enterocytes of SI
- -delayed CHO digestion & absorption
- ↓ postprandial glucose alone or in combo
- ↓ HbA1c
- NO sig effects on WEIGHT
Adverse:
-GI events → diarrhea, FLATULENCE
CI:
- GI disease
- breast feeding
- hepatic/renal impairment
Exenatide
- Liraglutide
- Dulaglutide
Incretin
- ↑ glucose dependent insulin release
- ↓ glucagon release → ↓ hepatic gluconeogenesis
- inactivated by DPP (these drugs are RESISTANT)
- ↓ postprandial & fasting serum glucose (alone or combo)
- potential ↑ β cell number & function
- slows gastric emptying →
- **weight LOSS / neutral
<>Exenatide<>: morn & evening SC inject 60 min before meal
- 1/week now available
- **can cause acute pancreatitis
- ↑ risk pancreatic & thyroid cancer
<>Liraglutide<>: single daily SC injection
-Thyroid cancer CI
<>Dulaglutide<>: once weekly SC injection
CI for slow GI problems, or drugs that can’t be in acid long
Sitagliptin potentiates effects
Sitagliptin
- -Saxagliptin
- -Linagliptin
- -Alogliptin
DPP-IV inhibitors
- ↑ effects of incretin hormones
- NO significant effect on WEIGHT
- orally active
-assoc. acute pancreatitis & pancreatic cancers
Pramlintide
pr-am(y)lin-tide
centrally acting Amylin analog
- only used as an adjunct to INSULIN therapy in DM 1 & 2
- regulates posprandial glucose [ ]
- -↓ gastric emptying w/o altering absorption
- -↓ postprandial glucagon
- -↓ appetite → ↓ calorie intake → WEIGHT LOSS
SC injection 3/day w/ meal bolus of insulin
