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pharmacology > pharmacotherapy of type 2 diabetes > Flashcards

pharmacotherapy of type 2 diabetes Flashcards

1
Q

criteria for diagnosing diabetes mellitus ?

A

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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2
Q

what is the goal in diabates mellitus

A

to keep hb1ac less than 6.5 percent

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3
Q

what are the ORAL drug groups available for diabetes ?

A

BIGUANIDES

SULFONYLUREAS

MEGLITINIDES

THIAZOLIDINEDIONE

ALPHA GLUCOSIDASE INHIBITORS

DIPEPTIDYL PEPTIDASE 4 INHIBITORS

SODIUM GLUCOSE CO TRANSPORTER 2 inhibotrs

DOPAMINE-2 AGONIST

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4
Q

what are the drugs in biguanide group ?

A

metformin

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5
Q

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

A

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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6
Q

what are the side effects and contraindications of biguanides ?

A

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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7
Q

what are the advanatges and cost of beguanides ?

A

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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8
Q

what are the sulfonylurease ?

A

GLIBENCLAMIDE
GLIPIZIDE
GLICLAZIDE
GLI’s

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9
Q

SULFONYLUREASE

pharmokinetics

mechanism of action

physiological action

A

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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10
Q

what are the side effects of sulfonylureases?

A 
hypoglycemia esp glibenclamide
weight gain 
vomitting -GI 
allergy 
(hematolgical) agranulocytosis and hemolytic anemia = RARE 
decrease of effect with time
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11
Q

what are the contraindications of sulfonylureas ?

A

except for GLIBENCLAMIDE =not in prgenacy and lactation

liver failure

severe renal failure

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12
Q

what are the advantages of sulfonylureas?

and cost ?

A

extensive usage
and decrease microvascular risk

cost is low

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13
Q

what are the MEGLITINIDES ?

A

repaglinide
nateglinide
-GLINIDES

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14
Q

for metglitinide what is it’s

PK

MECHANIMS OF ACTION

PHYSIOLOGICAL

SIDE EFFECTS

CONTRA

A

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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15
Q

what are the advntages of meglitinides ?

and cost ?

A

decrease in postprandil glucose
dosing flexibility

cost moderate

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16
Q

what are the THIAZOLIDINEDIONEs

A

PIOGLITAZONE

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17
Q

for THIAZOLIDINEDIONES

pk

mechanism of action

physiological

A

pk
liver metabolsim

mechanism of action
activation of nuclear transcription factor PPAR gamma

physiological
increase sensitivity to inuslin

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18
Q

side effects of thiazolidinediones ?

A 
weight gain by FLUID RETENSION
increased risk for myocardial infraction and heart failure 
anemia 
osteopenia
increased risk for bladder cancer
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19
Q

what are the contraindication of thiazolidinediones ?

A

pregnancy and lactation
liver failure
heart failure

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20
Q

what are the advanatgages of thiazolidinediones ?

cost ?

A

no hypoglycemia
long durability
increase HDL-C
decrease TG

cost = low

21
Q

what are the alpha glucosidase inhibitors ?

A

acarbose

22
Q

alpha glucosidase inhibitors is specifically given when ?

A

post prandil

23
Q

alpha glucosidase ihibitors

mechanism of action

physiological

side effects

contra

A

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

24
Q

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

A

dopamine 2 agonists =0.4-0.8 decrease

apha glucosidase inhibotrs = 0.5-0.8

25
Q

what are the advantages of alpha glucosidase ?

cost ?

A

no hypoglycemia
decrease postprandil glucose
non systemic

moderate

26
Q

what are the DDP-4 inhibitors ?

A

GLIPTINs

sitagliptin

27
Q

for DDP-4 inhibotrs

what is the mechanism of action

physiolgical

A

inhibtion of ddp-4 AND INCREASE POST PRANDIL INCRETIN

physiolgocal
increase insulin secretion
and glucagon secretion is decreased

28
Q

what are the side effcts of DDP-4 inhibitors ?

contra indications

A

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

29
Q

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

A

no hypoglycemia and well tolerated

cost = high

30
Q

what are the SGCT-2 inhibitors ?

A

dapagliflozin

-gliflozins

31
Q

physiological effect of SGCT-2 inhibitors? ?

A

blocks glucose resoprtionin the lidneys by increasing glucosurea

32
Q

whata re the side effcets to SGLT2 inhibtrs ?

A

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

33
Q

what are the contraindications of SGCT-2 inhibitors ?

A

renal failure
creatinin clearance even in 60ml/min

age over 70

children under 18 and pregnant women

34
Q

what are the advantages of SGCT-2?

A

no hypoglycemia
decrease weight
decrease blood pressure

35
Q

what are the dopamine agonist ?

A

bromocriptine

36
Q

for dopamine agonist
what is the pk

what is the physiological action

side effects

and contra

A

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
37
Q

what ara the advanatges and cost of dopamine agonist

A

no hypoglycemia

high cost

38
Q

WHAT ARE THE INJECTIBLE DRUG GROUPS for diabetes ?

A

glucagon like peptides 1 = glp-1

insulins

39
Q

what are the types of inulins

A

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

40
Q

what are the glucaon like peptides 1 ?

A

exanatide

1hr before meals

41
Q

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

A

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

42
Q

how is glucagon like peptide 1 exenatide administered ?

A

subcutaneous injection

43
Q

how is insulin administered ?

A

subcutaneous and IV

44
Q

what is the advanatges of GLP-1?

and its cost ?

A

no hypoglycemia
decrease weight
decrease post prandil glucose

cost is high

45
Q

which has the highest response to HB1A percentage lowering ?

A

insulin = 1.5-3.5 percent

46
Q

what are the physiological action and side effects of inuslin ?

A

increase uptake of glucose
decrease hepatic production of glucose

side effects 
hypoglycemia 
weight gain 
lipidystrophy at the injection site 
insulin resistance and allergy
47
Q

how do we treat diabetes melltius

A

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

48
Q

how do we use metformin ?

A

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

49
Q

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

A

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

pharmacology (7 decks)

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