diabetes Flashcards
Metformin’s effect on weight
weight loss 2-5kg
Metformin’s effect on Hgb H1ac
decrease 1.5 to 2.6 %
Metformin’s effect on women
pcos treatment
Metformin’s effect on TG
decrease by 16%
Metformins effect on lipid level
lower by 8%
Metformins effect on HDL and total cholesterol
increase HDL by 2% and increase total cholesterol by 5%
Metformins effect on fibrinolysis, inflammatory marker, endothelial function
improvement
what is metformin’s drug class?
biguanides
what is the role of metformin
insulin sensitizer
metformin peak level
1-3hr
metformin half life
5hrs
metformin metabolism site
liver and kidneys
metformin preparations
500, 750, 850, 1000mg
metformin maximum daily dosage
2000mg
metformin adverse effect:
GI side effect and anorexia
when do you eat metformin?
after meals
Clinical use of metformin
diet failed DM2 especially in overweight, failure to meet treatment goals in SU, IGT, PCOS.
how is metformin used with other drugs or solo?
monotherapy or combo with SU, glinides, AGIs, glitazones, and insulins
Metformin contraindication in women
pregnancy and breastfeeding
metformin renal dysfunction
creatinine >1.5mg/dl (males), >1.4mg/dl(females)
metformin liver dysfunction
hepatic dyfunction = lactate metabolism
metformin electrolyte problem
acute or chronic lactic acidosis
metformin lifestyle contra
hx of alcoholism
metformin no nos
any condition with renal dysfunction or hypoxic conditions (cvd, severe infection, use iodinated contrast, trauma, major operation)
metformin additional iotragenic problem
hold metformin: prevent contrast induced nephropathy
increase insulin secretion regardless of blood glucose level.
sulfonylureas and meglinitides
sulfonylurea and meglinitides side effect
hypoglycemia, stimulate appetite weight gain, nausea, fullness, heartburn. Rash, swelling
contraindication of sulfonylurea and meglinitides
type 1 dm, pregnancy, breast feeding
stimulating insulin secretion by the pancreat beta cells
sulfonylureas
A1c effect
reduction 1-2%
sulfonylurea treatment method
monotherapy or in combo with others
sulfony urea is unaffected by food except
glipizide
metabolized in urine
chlorpropamide
metabolized in biliary
glipzide
adverse effect on SU
hypoglycemia and weight gain
blood effect on Su
agranulocytosis, thrombocytopenia, BM aplasia, RBC aplasia, hemolytic anemia
skin effect on Su
rashes, pruritis, erythema nodosum, erythema multiforme, Steven Johnson syndrome, exfoliative dermatitis, purpura photosensitivity
GIT effect on Su
N/V, heartburn
Liver effect on Su
abnormal function test, jaundice, cholestasis, granulomatous hepatitis
Good candidate for SU treatment
Recently dx DM2, mild to moderate fasting hyperglycemia (
Bad candidate for SU treatment
type 1 dm, pregnancy, breast feeding, Major surgery (NPO), severe infection, stress, trauma (prone to hypoglycemia), severe adverse reaction, Liver or kidney disease (delayed clearance)
works similar to sulfonylurea but with a more rapid onset and shorter duration of action
Meglitinides
Insulin effect on Meglitinide
Insulin secretion is stimulated to a greater extent immediately after administration
When is good time to take it
before meals
improves insulin sensitivity in muscle, adipose tissue and liver, reduce glucose output from liver, change fat distribution by decreasing visceral fat and increasing peripheral fat
thiazolidinediones
Side effects of Thiazo
weight gain, fluid retention, headache, decrease hemoglobin, fracture in women, bladder Ca in men
contraindication of thiazo
liver disease, heart failure or history of heart disease, pregnancy and breast feeding
when is it not contraindicated
renal insufficiency
possible advantage of thiazo
potential benefits of pioglitazone, reduce levels of LDL-C, increase levels of HDL-C
Thiazo actions depends on?
presence of endogenous or exogenous insulin and insulin resistance
Thiazo effect on HbA1c
decrease 0.5 to 1.3%
dosing frequency of Thiazo
once or twice daily
metabolism site of TZD-Pio
liver and kidneys
adverse effect of TZD
weight gain, edema, dilutional anemia
contraindicated of TZD
congenital heart failure
adverse effect on plasma
plasma volume expansion: reduction in hemoglobin, hematocrit, neutrophil count
what NYHA class to be avoided by tzd
class 3 and class 4
Pioglitazone names
actos, prialta, piozone, glucozone, glitaz, PPAR, zolid
slow digestion of sucrose and starch and delays absorption. Slow post meal rise of blood glucose
alpha glucosidase inhibitor
must to do list for alpha glucosidase inhibitor
must be taken just before a meal or within first bite wtf
what other drugs will cause hypoglycemia if alpha glucosidase inhibitor is used
sulphonylurea- so as remedy use glucose
contraindication of alpha glucosidase inhibitor
intestinal disease -Crohn’s, autonomic neuropathy affecting the gastrointestinal tract
side effect of alpha glucosidase inhibitor
flatulence, ab discomfort, diarrhea, NO hypoglycemia used as monotherapy
inhibits pancreatic alpha amylases that hydrolyzes complex starches to oligosaccharides in the lumen of small intestines, reduces the rate of digestion and subsequent delayed intestinal absorption glucose
alpha glucosidase inhibitor
Starch blocker
alpha glucosidase inhibitor
another name for alpha glucosidase inhibitor
acarbose
GI absorption of acarbose is
very minimal and metabolism happens in intestinal bacteria and digestive enzymes
maximum dose of alpha glucosidase inhibitor or acarbose
100mg TID
GLP 1 another name is
Incretin Mimetic Agent
action of GLP 1
improve responsiveness of beta cell to increase glucose levels, decrease glucagon secretion, slow gastric emptying
side effect of GLP 1
nausea, weight loss, diahrrea, risk of hypoglycemia when used with sulphonylurea
contraindication of GLP1
end stage kidney disease or renal impairment, pregnancy, severe GI disease
how is GLP1 administered
must be injected subcutaneously once or twice a day depending on medication before meals. Results in a feeling of fullness before a meal
GUT derived factor that increase glucose stimulating insulin secretion
Incretin Mimetic Agent
2 incretin molecules
glucagon like peptide 1(GLP 1) and Gastric Inhibitory Peptide or glucose dependent insulinotropic peptide (GIP)
increatin molecule is inactivated y
both molecule rapidly inactivated by enzyme Dipeptidyl Peptidase 4 (DDP 4)
what lymphocyte cell surface protein of DDP 4
CD 26
DDP4 role on GLP1
DPP4 rapidly inactivates GLP1
Inhibition of DPP4 enhances what
activity of GLP 1 and other bioactive peptides (GIP, GRP)
This inibition of DPP4 creates what
Stimulates release of insulin, reduces secretion of glucagon
two types of incretin modulator
incretin mimetics (GLP 1 analogs) and incretin enhancers (DPP 4 inhibitors)
GLP1 actions and location
stimulates insulin release from beta cells and may increase beta cells mass/regeneration in ileum and colon
GIP action
releases from K cells in duodenum
medication in combo examples
Su + metformin, pioglitazone + metformin, DPP 4 inhibitor + metformin, SU + pioglitazone
examples of sodium glucose transport (SGLT 2) inhibitors
Canagliflozin (Invokana), Sergliflozin, Remogliflozin, Dapagliflozin (Forxica)
Insulin secretagogues MOA and location
increase insulin production in pancreas
biguanides MOA and location
reduce glucose production in liver and cell evel
thiazolidinediones MOA and location
reduce insulin resistance in cell level and liver
alpha glucosidase inhibitor MOA and location
slow absorption of sucrose and starch in GIT
GLP 1 (incretin) MOA and location
increase response of beta cells to circulating glucose levels in pancrease and brain
DPP4 inhibitors MOA
increase effects of incretin
action of Colesevelam
bile acid sequestrant
indication of colesevelam
adjunt to diet and exercise to reduce elevated low density lipoprotein cholesterol (LDL-C) in patient with primary hyperlipidemia and to improve glycemic control in adults with T2DM
action of pramlintide
analogue of amylin, small peptide hormones that is released into bloodstream by beta cells of pancreas along with insulin. Like insulin, amylin is completely absent in individuals with type 1 dm
effect of pramilintide
by augmenting endogenous amylin, pramlintide aids in the absorption of glucose by slowing gastric emptying, promoting satiety via hypothalamic receptors (different receptors than GLP 1) and inhibiting inappropriate secretion of glucagon, a catabolic hormone that opposes the effects of insulin and amylin. Also has effects in raising the acute first phase insulin response threshold following a meal
