Insulin and Oral Hypoglycemic Agents Flashcards
Type I diabetes
Insulin dependent
Little to no insulin production
Type II diabetes
Non-insulin dependent
Insulin resistance
What is insulin?
What does it do?
Mech?
Central control for metabolism of glc
Protein hormone secreted from B cells of islets of Langerhans (pancreas)
Anabolic hormone-increase storage and uptake of nutrients
Glc and AA, etc.
In absence of insulin we have tissue breakdown into glc
Mech: binds to cell surface receptor + increase glc cell uptake
Muscle and fat cells
Effects of diabetes
General
- Decrease insulin→ decrease glc uptake
Short term
- Polyuria-increase urine output
- Due to glc in urine (brings H2O w/ it)
- Polydipsia-increase thirst
- Polyphagia-increase appetit
Long term
- Glycosylation of proteins
- Altered signal pathways and cell death
- Cardio dysfunctions
- Compromised circ→organ death
- Atherosclerosis
- Diabetic neuropathy
- Leading cause of kidney failure
- Vision changes
- Diabetic retinopathy–blood vv in eye damaged
- Ocular edema
- Glaucoma, cataracts, etc.
- Peripheral neuropathy-neurons lack energy
- Infections–bacterial overgrowth b/c glc so available
- Kidney
- Bladder
What’s the most important factor to control diabetes?
_*DIET*_
This will be on the exam
We also use insulin injections
and other agents
What does crystal size matter w/ regards to insulin?
What is used to increase size?
Duration of action proportional to size
Larger crystals=longer to dissolve
Protamine increases size in protamine insulin
Lispro
Tx: Diabetes
Designer insulin
Short acting (2-5 hrs)
Regular human insulin
Tx: Diabetes
Designer insulin
Short acting (2-5 hrs)
Afrezza is the inhaled form
Aspart
Tx: Diabetes
Designer insulin
Short acting (2-5 hrs)
Glulisine
Tx: Diabetes
Designer insulin
Short acting (2-5 hrs)
Detemir
Tx: Diabetes
Designer insulin
Long acting (24+ hrs)
Determined to get large (that a long time)
Detemir +glargine=long acting insulins
Glargine
Tx: Diabetes
Designer insulin
Short acting (24+ hrs)
Determined to get large (that a long time)
Detemir +glargine=long acting insulins
Isophane
Tx: Diabetes
Designer insulin
Protamine insulin
Intermediate acting
What are the short acting designer insulins?
Regular human insulin
Lispro
Aspart
Glulisine
2-5 hrs
What are the long acting designer insulins?
Detemir
Glargine
Tolbutamide
Tx: Diabetes
Oral hypoglycemic agents
First gen sulphonylureas
Mech: K channel blockers
Block K channels on B cells →Increase Ca→Insulin secretion
Duration: 6-12 hrs
Contra/Indications:
- Do not use if you have renal or hepatic damage
- Not overweight
- Have some islet fxn
SE:
- Hypoglycemia and hypoglycemia coma
- More common in drugs w/ longer duration
- Can be teratogenic
- Can increase death due to cardiovascular problems
Tolazamide
Tx: Diabetes
Oral hypoglycemic agents
First gen sulphonylureas
Mech: K channel blockers
Block K channels on B cells →Increase Ca→Insulin secretion
Duration: 12-60 hrs
Contra/Indications:
- Do not use if you have renal or hepatic damage
- Not overweight
- Have some islet fxn
SE:
- Hypoglycemia and hypoglycemia coma
- More common in drugs w/ longer duration
- Can be teratogenic
- Can increase death due to cardiovascular problems
Chlorpropamide
Tx: Diabetes
Oral hypoglycemic agents
First gen sulphonylureas
Mech: K channel blockers
Block K channels on B cells →Increase Ca→Insulin secretion
Duration: 60+ hrs
Contra/Indications:
- Do not use if you have renal or hepatic damage
- Not overweight
- Have some islet fxn
SE:
- Hypoglycemia and hypoglycemia coma
- More common in drugs w/ longer duration
- Can be teratogenic
- Can increase death due to cardiovascular problems
Gli–ide
or
Gly–ide
Glipizide
Glyburide
**Glimepiride **(most potent)
Tx: Diabetes
Oral hypoglycemic agents
Second gen sulphonylureas
More rapid onset and longer duration
Mech: K channel blockers
Block K channels on B cells →Increase Ca→Insulin secretion
Contra/Indications:
- Do not use if you have renal or hepatic damage
- Not overweight
- Have some islet fxn
SE: Less than 1st gen
- Hypoglycemia and hypoglycemia coma
- More common in drugs w/ longer duration
- Can be teratogenic
- Can increase death due to cardiovascular problems
-glinide
Repaglinide
Nateglinide
Tx: Diabetes
Oral hypoglycemic agents
Sulphonylurea-like agents
Rapid onset, short duration
Mech: K channel blockers
Bind diff site on K channel
Block K channels on B cells →Increase Ca→Insulin secretion
Contra/Indications:
- Do not use if you have renal or hepatic damage
- Not overweight
- Have some islet fxn
SE:
- Hypoglycemia and hypoglycemia coma
- More common in drugs w/ longer duration
- Can be teratogenic
- Can increase death due to cardiovascular problems
Exenatide
Tx: Diabetes
Incretin enhancer
Mech: Bind to and activate receptors on B cell
Analog of GLP-1 (incretin)
Not broken down by DPP-4
Injection 2x/day
SE:
- Pancreatitis
-glutide
**Liraglutide **(Inj 1x/day)
Albiglutide (Inj. 1x/week)
Tx: Diabetes
Incretin enhancer
Mech: Bind to and activate receptors on B cell
Incretin analog
SE:
- Thyroid tumor
- I want my glutes to be as hard as concrete*
- -glutide to be as hard as incretin*
-gliptin
or
-glyptin
Sitagliptin
Saxagliptin
Linaglyptin
Alogliptin
Tx: Diabetes
Incretin enhancer
Mech: Inh DPP-4 Enzyme →prevent incretin metab
Orally
Often used in combo w/ other drugs
- Put a lip of dip in (oral). Dip comes in a tin*
- G-_LIP_-TIN are DPP inh. Taken orally.*
Metformin
Tx: Diabetes
Insulin enhancers
Mech: Act. protein kinase→
Increased glc abs. by muscle
Decreased glc production by liver
SE:
- Lactic acidosis (potentially fatal)
- Weight loss due to anorexia
- George Foreman was an American Professional (Kick)boxer *
- Metformin Activates Protein Kinase*
- He worked out so hard he had lactic acidosis and had to be anorexic to make his weight class*
-glitazone
Rosiglitazone
Pioglitazone
Tx: Diabetes
Insulin enhancers
Mech: Act. PPAR→
Increased insulin receptor response
Increased # insulin receptors
Increased glc uptake by cells
SE:
- Wt gain
- Edema
- Fractures of arms and legs
- Macular edema
- Cardio problems
- MI
Acarbose
Tx: Diabetes
Glucose abs. delayers
Mech: Inh. alpha glucosidase
Prevents breakdown of complex carbs in gut
SE:
- Unabsorbed carbs ferment in gut
- Cramps
- Diarrhea
- Flatulence
- A-carb-ose*
- No-carb-abs.*
Miglitol
Tx: Diabetes
Glucose abs. delayers
Mech: Inh. alpha glucosidase
Prevents breakdown of complex carbs in gut
SE:
- Unabsorbed carbs ferment in gut
- Cramps
- Diarrhea
- Flatulence
Mig--litol
_Midg_ets (Mack) are little b/c they don’t absorb any carbs
Pramlintide
Tx: Diabetes
Amylin analogs
Mech: Activate amylin receptor→
Decrease gastric emptying
Decrease appetite
Route: SubQ before meals
SE:
- Severe hypoglycemia
- prAMLINtide=AMyLIN analog*
-gliflozin
Canagliflozin
Dapagliflozin
Empagliflozin
Tx: Diabetes
Inh. of glc resorption by kidney
**Mech: **Inh. SGLT2 (Na-glc cotransporter)
in PCT–allows kidney to eliminate blood glc
SE:
- Hypotension
- Hypokalemia
- Due to increased urine output
- Gential fungal inf
- Urine loaded w/ glc