CHAPTER 24: DIABETES DRUGS Flashcards
Amylin
- what is it
- actions
hormone co secreted w insulin from pancreatic beta cells
ACTION: delays gastric emptying, dec postprandial (after meal) glucagon secretion, improve satiety
Pramlintide
- synthetic form of amylin
- SC before major meal
- combo with insulin and oral agents
Pramlintide: Adverse effects
nausea, vomiting, anorexia, hypoglycemia
CANNOT be mixed in same syringe with insulin
Incretin Mimetics/GLP-1 Agonists
- incretin effect
- how does gut regulate it
Incretin effect reduced in type 2 diabetes
- gut releases incretin hormones, GLP-1, and GIP, in response to a meal, which are responsible for insulin secretion
Incretin mimetics/GLP-1 receptor agonists: 2 drugs
exenatide and liraglutide
Incretin Mimetics: MOA and route
mimic incretin hormones (GLP-1 receptor agonists)
- polypeptides–> SC route before meals
Incretin Mimetics: Actions/effects
- improves glucose dep insulin secretion
- slow gastric emptying time
- reduce food intake by inc satiety
- dec postprandial glucagon secretion
- promote Beta cell proliferation—> post prand hyperglycemia is reduced, HbA1c dec, weight loss
Incretin Mimetics: adverse effects
GI: nausea, vomit, diarrhea, constipation
- pancreatitis
-thyroid C-cell tumor (only liraglutide)
Oral Agents
- 3 types of PTs that need oral agents
- PT w type 2 diabetes not controlled w diet
- PT who develop diabetes after age 40, had it for less than 5 yrs
- PT with long-standing disease need combo or oral agents to control hyperglycemia
DPP-4 Inhibitors
- name the drugs
- MOA
- Alogliptin, linagliptin, saxagliptin, sitagliptin
MOA: inhibit DPP-4 enzyme that inactivates incretin hormone (GLP-1)–> increases insulin release in response to meal
DDP-4 is what inactives GLP-1 and GIP
DPP-4 Inhibitors: adverse effects
- nasopharyngitis
- headache
- pancreatitis
- dose adjust for renal dysfunction (drug is heavily metab by liver) except linagliptin
DPP-4 Inhibitors: drug-drug interactions
Strong liver enzyme inhibitors (antivirus/bacterial drugs) may INCREASE levels of saxagliptin
Sulfonylureas
- names
- use
- glyburide, glipizide, glimepiride
- insulin secretagogues: they promote insulin release from the B cells of pancreas
Sulfonylureas: MOA
- stim insulin release from B cells of pancreas—> block ATP dep K+ channels—> depolarize, influx Ca2+, insulin exocytosis
- may REDUCE hepatic glucose production and INC peripheral insulin sensitivity
Sulfonylureas: Adverse Effects
- hyperinsulinemia and hypoglycemia (imbalanced levels gluc and insulin)
- weight gain
- Gi distress (nausea, vomit, anorexia)
Glyburide: minimal placenta transfer
which sulfonylurea is best for pregnant patients?
glyburide bc it has minimal transfer across the placenta, a better insulin alternative
Sulfonylureas: Contraindications and cautions
- diabetes w/ fever, severe infection, trauma, major surgery, ketoacidosis, renal/hepatic disease
- contraindicate for use in type 1 diabetes
- pregnancy/lactation
- not safe/efficient in children
Glinides
- names
- actions
- taken when?
- repaglinide, nateglinide
actions: stimulate insulin secretion by blocking ATP dep K+ channels in B cells
take before meal
- rapid onset, short half life
why can’t you use glinides in combo with sulfonylureas?
due to the overlapping of MOA
Glinides: adverse effects
- hypoglycemia and weight gain
- liver enzyme inducers (ex: barbiturates) may reduce effect
- liver enzyme inhibitors (ex: antibiotics) may enhance repaglinide gluc lowering effect
Glinides: contraindications and cautions
caution in PT with hepatic impairment
Biguanides: METFORMIN
- actions
- reduce hepatic gluconeogenesis
- slow intestinal absorption of sugars
- improve peripheral gluc uptake/utilization
- weight loss may occur (loss of appetite)
Biguanides: METFORMIN
- therapeutic uses
- anti-diabetic APPROVED FOR CHILDREN 10 yrs and older
- off label for PCOS
Biguanides: METFORMIN
- adverse effects
- lactic acidosis
- GI distress (nausea/vomit)
- Hypoglycemia if taken w insulin/other agents
- LONG TERM USE–> b12 deficiency
why is hyperinsulinemia not a problem for those taking metformin?
bc this drug does NOT affect insulin release, its focus is on reducing liver making glucose
Biguanides: METFORMIN
- contraindications and cautions
- renal dysfunc bc of acidosis
- discontinue if acute MI or worsening HF occurs
Thiazolidinediones
- names
- MOA
- insulin sensitizer?
- pioglitazone, rosiglitazone
MOA: dec insulin resistance acting as agonists for PPAR gamma receptors—> transcription of insulin responsive genes–> inc insulin sensitivity in adipose, liver, and skeletal muscle
insulin sensitizers INC glucose uptake (no hyperinsulinemia)
Thiazolidinediones: adverse effects
- liver toxicity
- inc SC fat, cause fluid retention–> weight gain
- fluid retention–> avoid in PT with HF!!!
- osteopenia, inc fracture risk in women
pio–> inc bladder cancer risk
rosi–> inc MI and angina risk
Alpha Glucosidase Inhibitors
- names
- MOA
- acarbose, miglitol
MOA: inhibit a-glucosidase (enz breaks down carbs into gluc that can be absorbed)
- delay digestion of carbs–> lower postprandial glucose levels
USE IN COMBO w sulfonylureas, metformin, insulin, at start of meal
Alpha Glucosidase Inhibitors
- adverse effects and contraindications
AE: GI distress
Contraindications:
- PT w bowel disease, colonic ulceration, intestinal obstruction should NOT use these drugs
