pharmacotherapy of type 2 diabetes Flashcards by Janet Jincy

criteria for diagnosing diabetes mellitus ?

normal glucose levels more than 11.1mmol/l

fasting plasma glucose more than 7 mmol/l

and there is 75g of oral glucose intake after 2 hours measures more than 11.1mmol/l

hemoglobin more than 6.5 percent

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what is the goal in diabates mellitus

to keep hb1ac less than 6.5 percent

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what are the ORAL drug groups available for diabetes ?

BIGUANIDES

SULFONYLUREAS

MEGLITINIDES

THIAZOLIDINEDIONE

ALPHA GLUCOSIDASE INHIBITORS

DIPEPTIDYL PEPTIDASE 4 INHIBITORS

SODIUM GLUCOSE CO TRANSPORTER 2 inhibotrs

DOPAMINE-2 AGONIST

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what are the drugs in biguanide group ?

metformin

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what is the mechansim of action and physiological actions in biguanide ?

mechanism of action
activation of AMP- kinase and reduce heptic glucose production

physiological 
decrease gluconeogenesis 
increase insulin release 
decreases insulin reistsnace 
decrease glucose absoprtion in the GIT 
suppression of appetitie 
decrease LDL and VLDL

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what are the side effects and contraindications of biguanides ?

GI = anorexia , diarrhea , metallic taste
vitb12deficiency
rarely lactic acidosis and coma

contraindications
renal failure =
decrease dose if if creatining clearance less than 60ml/min
stop if 30

predisposing disease to hypoxia such as cardiopulmonary diseases

radiographic contrast media

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what are the advanatges and cost of beguanides ?

extensive use
improves lipid profile
good cardiovascular benefits
no metabolic changes = weight neutral or weight loss
can be used as prevention in people who are obese

cost = low

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what are the sulfonylurease ?

GLIBENCLAMIDE
GLIPIZIDE
GLICLAZIDE
GLI’s

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SULFONYLUREASE

pharmokinetics

mechanism of action

physiological action

PK
binds to plasma porteins
CYP2C9 liver metabolism
long half life

mechansim
closing of potassium atp channels in the b cells’s membrane

physioloigical
increase insulin secretion

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what are the side effects of sulfonylureases?

hypoglycemia esp glibenclamide
weight gain 
vomitting -GI 
allergy 
(hematolgical) agranulocytosis and hemolytic anemia = RARE 
decrease of effect with time

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what are the contraindications of sulfonylureas ?

except for GLIBENCLAMIDE =not in prgenacy and lactation

liver failure

severe renal failure

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what are the advantages of sulfonylureas?

and cost ?

extensive usage
and decrease microvascular risk

cost is low

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what are the MEGLITINIDES ?

repaglinide
nateglinide
-GLINIDES

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for metglitinide what is it’s

MECHANIMS OF ACTION

PHYSIOLOGICAL

SIDE EFFECTS

CONTRA

pk
liver metabolism, renal excretion (10 percent) and short half life

mechansim of action
like sulfonylureas

physiolgocal action
like sulfonylurease

side effects
hypoglycemia but compared to sulfonylureas its better
weight gain
bone fractures

contra
in pregenancy and lactation
liver failure
renal failure

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what are the advntages of meglitinides ?

and cost ?

decrease in postprandil glucose
dosing flexibility

cost moderate

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what are the THIAZOLIDINEDIONEs

PIOGLITAZONE

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for THIAZOLIDINEDIONES

mechanism of action

physiological

pk
liver metabolsim

mechanism of action
activation of nuclear transcription factor PPAR gamma

physiological
increase sensitivity to inuslin

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side effects of thiazolidinediones ?

weight gain by FLUID RETENSION
increased risk for myocardial infraction and heart failure 
anemia 
osteopenia
increased risk for bladder cancer

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what are the contraindication of thiazolidinediones ?

pregnancy and lactation
liver failure
heart failure

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what are the advanatgages of thiazolidinediones ?

cost ?

no hypoglycemia
long durability
increase HDL-C
decrease TG

cost = low

what are the alpha glucosidase inhibitors ?

acarbose

alpha glucosidase inhibitors is specifically given when ?

post prandil

alpha glucosidase ihibitors

mechanism of action

physiological

side effects

contra

inhibitio of eneteral alpha glucosidase

phsyiological
slows intestinal carbohydrate absorption and digestion

side effects
flatulance , diarrhea , abdominal pain

contra
large hernia
stenosisi and ulceration of the intestines

what are the diabetic drugs that has the lowest reduction of HB1AC

dopamine 2 agonists =0.4-0.8 decrease

apha glucosidase inhibotrs = 0.5-0.8

what are the advantages of alpha glucosidase ? cost ?

no hypoglycemia decrease postprandil glucose non systemic moderate

what are the DDP-4 inhibitors ?

GLIPTINs | sitagliptin

for DDP-4 inhibotrs what is the mechanism of action physiolgical

inhibtion of ddp-4 AND INCREASE POST PRANDIL INCRETIN physiolgocal increase insulin secretion and glucagon secretion is decreased

what are the side effcts of DDP-4 inhibitors ? contra indications

infection of the upper respirtory tract acute pancreatitis increase liver enzymes allergy = angioedema urticaria , skin problems contra moderate and severe renal impairment = adjust dose children under 18 and pregnant

what are the advanatges and cost for DDP-4 inhibitors ?

no hypoglycemia and well tolerated cost = high

what are the SGCT-2 inhibitors ?

dapagliflozin | -gliflozins

physiological effect of SGCT-2 inhibitors? ?

blocks glucose resoprtionin the lidneys by increasing glucosurea

whata re the side effcets to SGLT2 inhibtrs ?

do not use it in combination with sulfonylurease and inuslin because in only then hypoglycemia genitrourinary infection dysuria polyuria = HYPOTENSIONN = DIZZINESS rare ketoacidosisi bone fractures risk of breast cancer and bladder cancer INCREASE LDL-C increase creatinin

what are the contraindications of SGCT-2 inhibitors ?

renal failure creatinin clearance even in 60ml/min age over 70 children under 18 and pregnant women

what are the advantages of SGCT-2?

no hypoglycemia decrease weight decrease blood pressure

what are the dopamine agonist ?

bromocriptine

for dopamine agonist what is the pk what is the physiological action side effects and contra

first pass metabolism in CYP3A4 excretion predominantly in bile physio action increase inuslin sensitivity modulates hypothalamic control of metabolism side effects syncope and dissiness = hypotnesion rhinitis ``` contra renal and hepatic failure psychosis syncopal migraines nursing women = prevent lactation ```

what ara the advanatges and cost of dopamine agonist

no hypoglycemia high cost

WHAT ARE THE INJECTIBLE DRUG GROUPS for diabetes ?

glucagon like peptides 1 = glp-1 insulins

what are the types of inulins

1) rapid and short acting human insulin = actrapid insulin analogues lispro and aspart SOLUBLE INSULIN INJECTION 2) intermediate insulin mixtures - humulin insulin protamine SUSPENSION INJECTION 3) long acting insulin analgoues glargine detemir

what are the glucaon like peptides 1 ?

exanatide | 1hr before meals

what is the physiological action ? side effects ? contraindication of GLP-1 ?

increase insulin secretion glucagon secretion decreased slows gastric emptying increase satiety side vomitting diarrhea allergic acute pancreatitis contra severe renal failure children under 18 and pregnant women

how is glucagon like peptide 1 exenatide administered ?

subcutaneous injection

how is insulin administered ?

subcutaneous and IV

what is the advanatges of GLP-1? | and its cost ?

no hypoglycemia decrease weight decrease post prandil glucose cost is high

which has the highest response to HB1A percentage lowering ?

insulin = 1.5-3.5 percent

what are the physiological action and side effects of inuslin ?

increase uptake of glucose decrease hepatic production of glucose ``` side effects hypoglycemia weight gain lipidystrophy at the injection site insulin resistance and allergy ```

how do we treat diabetes melltius

start with monotherapy of metformin always if hb1ac has not reached target levels in 3 months then add one of the other groups if the patient has irregular meals meglitinides is used instead of sulfonylurease due to late post prandil hypoglycemia dual therapy must begin with metformin plus another class if the hb1ac is over 9 percent or equal to it initial inuslin injection therapy when bood glucose is over 16.7 mmol.l and hb1ac is over or equal to 10 percent = because this leads to weight loss and ketoacidosis

how do we use metformin ?

take it with meals , low dose first 500mg after 5-7 days if no gastroinetsinal sympotms can raise it up to 850mg or two 500mg

what are teh complication of diabetes mellitus and how can we treat it

proteinurea = acei and arb = renal portective bp control any diabetic patient over 40 = take statin existing cardiovascular porblems target LDL <1.8mmol/l LDL-C less than 2.6mmol/l HDL-C more than 1.1mmol/l men and 1.38 women