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163 Cards in this Set

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non-insulin medications for DM



3 main categories

1-oral for DM -II



2-injectable for DM II



3-injectable for DM I

oral medications for DM II


categories # 7

1-Biguanide = metformin



2-insulin secretagogous


((SFU / non-SFU))



3-DPP-IV



4-TZDs = pioglitazone



5-a-glucosidase inhibitors



6-bile acid sequestrant



7-dopamine receptors agonist

biguainide

metformin

SFUs secretagogues

(4)

Gly/i

(Glyb)uride / (gli)penclimide
(Glip)izde
(Glim)epride
(Glic)lazide

non-SFUs secretagogues
(3)

glinide

Nate(glinide)
Repa(glinide)
Miti(glinide)

a-glucosidase inhibitors

acarbose
voglibose
miglitol

thia-zolidin-diones

zone

pio-glita-zone

DPP-4

Di-peptidyl peptidase-4 inhibitors

gliptin

sita-gliptin
saxa-gliptin
vilda-gliptin
lina-gliptin

bile acid sequestrant

cole-seve-lam

dopamine receptor agonist

bromocriptine mesylate

2-injectable for DM II

GLP agonist

Liraglutide

exenatide

2-injectable for DM II + I

amylin analog

pramlinitide

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Biguanide



example

metformin

metformin



doses forms / tab

500



850



1000

metformin



dose / day



start by 500-850 once



increase every days - wks



start



500 X2



850 X1

meformin extended release

Glucophage XR



500 X1 then increase up to 2000/d

metformin



max dose

max 2000 mg / day



? 200 - 2550

metformin



mechanism of action

1-inhibits hepatic glucose output


 


2-decrease GI glucose absorption


 


2-stimulate periphral glucose uptake/ sensitivity

1-inhibits hepatic glucose output



2-decrease GI glucose absorption



2-stimulate periphral glucose uptake/ sensitivity

metformin



advantages

wt loss



no hypoglycemia

metformin



administration

with food

metformin



side effects

1-GI



2-lactic acidosis



3-asthenia /weakness

metformin



contraindications

1-CHF



2-M.acidosis



3-DKA



4-cr > 1.5 male / > 1.4 fem



5-contrast within 48 hrs before / after



6-lactation



7-shock



metformin



when to D/C during hospitalization

-trauma



-fever



-stress



-avoid with alcohol



-infection

metformin



pregnancy

B

metformin



uses /

montherapy / 1st line



as combination

meformin



brand names

-glucopahge


 


-Diamet


 


-formit


 


-metforal


 


-Mystro

-glucopahge



-Diamet



-formit



-metforal



-Mystro

metformin combination available

meformin + Glmepride



metformin + glibenclimide



metformin + vildagliptin



metformin + sitagliptin



metformin + saxaglibtin


_____________________



metformin + pioglitazone



metformin + glimepride

amaryl M


 


500 / 2

amaryl M



500 / 2

metformin + glibenclimide

Glucovance


 


500 / 2.5


 


500 / 5

Glucovance



500 / 2.5



500 / 5

metformin + vildagliptin

Galvusmet 


 


1000 / 50


 


850 / 50

Galvusmet



1000 / 50



850 / 50

metformin + sitagliptin

janumet


 


500 / 50


 


1000 / 50


 


1000 / 100 (ER)

janumet



500 / 50



1000 / 50



1000 / 100 (ER)

metformin + saxaglibtin

metformin + saxaglibtin

kombiglyza XR


 


500 / 5


 


1000 / 2.5


 


1000 / 5

kombiglyza XR



500 / 5



1000 / 2.5



1000 / 5

1

1

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1

1111

1

1

DDP-IV ???

dipeptidyl peptidase 4 inhib



=gliptins

DDP-IV



mechanism of action

1-L-cells in intestine


 


2-L-cells secreates the enzyme DPP-IV 


 


3-DPP4 breaks down GLP


 


4-GLP is an (incretin) that secraeted from L-cells


 


5-GLP act  ti inhibit glucagon and stimulate insulin

1-L-cells in intestine



2-L-cells secreates the enzyme DPP-IV



3-DPP4 breaks down GLP



4-GLP is an (incretin) that secraeted from L-cells



5-GLP act ti inhibit glucagon and stimulate insulin

GLP = incretin

GLP = incretin

GLP ??

Glucagon-like-peptide



is an incretin

incretin ??

group of gastrointestinal hormones that stimulate a decrease in blood glucose levels by :


1-inhibiting glucagon


2-stimulating insulin



incretin examples ??

only 2 :


______________________


1-GLP : glucagon-like-peptide


 


2-GIP :gastric inhibitory peptide

only 2 :


______________________


1-GLP : glucagon-like-peptide



2-GIP :gastric inhibitory peptide

DPP- IV


??

is the enzyme that inhibits incretin and breaks them

DPP-IV



side effects

-pancreatitis مهم مهم مهم / نادر



-angioedema



-Steven Johnson synd

DPP-IV



Examples #4

1-sitagliptin = jinuvea



2-saxagliptin = Ongelyza



3-linagliptin



4-vildaglibtin =

Sitagliptin



generic name



JANUVIA 

JANUVIA

Sitagliptin



administration

once daily

Sitagliptin



dose

100 mg



Sitagliptin



renal impairment

renal elimenation



if GFR < 50



dose 50 mg

Saxagliptin



generic name


Onglyza

Onglyza

Saxagliptin



dose

once daily



2.5 mg



5 mg

Saxagliptin



renal imparment

renal elimination


 


2.5 mg / day

renal elimination



2.5 mg / day

Saxagliptin



side effects

urticaria



angioedema

Vildagliptin



generic name

Galvus

Galvus

Vildagliptin



dose

once daily



50


100 mg

Vildagliptin


renal impairment

not approved

linagliptin



dose

once daily



5 mg

linagliptin




renal imparment

fecal excreation



no adjustment

1

1

1

1

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1

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a-glucosidase inhibitors



mechanism of action

acts by inhibition of :


-polusaccharides


 


-disacchardides


breakdown to glucose so decreasing postprandial hyperglycemia

acts by inhibition of :


-polusaccharides



-disacchardides


breakdown to glucose so decreasing postprandial hyperglycemia

a-glucosidase inhibitors



administration

with meals

a-glucosidase inhibitors



examples

1-Acarbose



2-Miglitol

a-glucosidase inhibitors



dose / initial



max

300 mg / day

a-glucosidase inhibitors



main side effect

GI 25 - 50 %


____________________


bloating


cramps


diarrhea


flatulance

a-glucosidase inhibitors




HbA1c reduction

modest



0.4 - 0.7 %

a-glucosidase inhibitors



risk of hypoglycemia

no

a-glucosidase inhibitors


acarbose


 


 

a-glucosidase inhibitors


acarbose



1

1

a-glucosidase inhibitors



acarbose



specific side effect

elevated liver enzymes

a-glucosidase inhibitors



if hypoglycemia while in regimen

treat with glucose not sucrose

*****

***

***

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***

TZDs ??

thia-zolidine-diones

TZDs


thia-zolidine-diones




mechanism of action??

increased insulin sensitivity in :


-,uscles


 


-adipose


 


-liver

increased insulin sensitivity in :


-,uscles



-adipose



-liver

TZDs


thia-zolidine-diones



examples

only one :


_____________________



Pioglitazone

TZDs


thia-zolidine-diones



pioglitazone



brand name

Actos

Actos

TZDs


thia-zolidine-diones



pioglitazone



use

as single agent



in combination



in pt early in DM , still have endogenous insulin

TZDs


thia-zolidine-diones



pioglitazone


frequency of use

once daily

TZDs


thia-zolidine-diones



pioglitazone


dose

15 - 30 mg daily


 


up to 45 /day

15 - 30 mg daily



up to 45 /day

TZDs


thia-zolidine-diones



pioglitazone


max dose

45 mg daily



30 mg daily if used with insulin

TZDs


thia-zolidine-diones



pioglitazone


contraindications

combromized heart function NYHA III-IV



every pt must be assessed regarding cardiac function



active bladder CA

TZDs


thia-zolidine-diones



pioglitazone


side effects

- edema / CHF



-hepatotoxicity - rare



-bladder CA ?? still



-subclinical BM suppression


(((with possible pancytopenia due to volume expansion))



-inhib. osteoblast : risk of fx in females



-ovulation in women with anovulatory cycles



-interactions / cyto-p450

TZDs


thia-zolidine-diones



pioglitazone


risk factors for precipitating heart failure

-previous CHF


-IHD


-HTN


-long-standing DM


-left vent. hypertropthy


-pre-existing edema


-edema after TZDs therapy


-insulin therapy


-aging


-renal failure


-aortic stenosis


-mitral valve disease

actos


u have to monitor >>>>

liver enzemes

actos and bladder CA ??

still under-study

****

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dopamin rec agonist

bromocriptin

22

22

2222

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Bile acid sequestrant



example



mech. of action

Cole-Sevelam hydrochloride

Cole-Sevelam hydrochloride

Cole-Sevelam hydrochloride



use

as monotherapy



combination

Cole-Sevelam hydrochloride



dose

3 tabs X 2


 


((625 mg X2))

3 tabs X 2



((625 mg X2))

Cole-Sevelam hydrochloride



administration

empty stomach



not with other medications / not to interfere with their absorptions

Cole-Sevelam hydrochloride



HbAic lowering effect

0.4 - 0.8 %

Cole-Sevelam hydrochloride



other benefit

LDL lowering effect



can be used in pregnancy



can be used in renal + hepatic disease

Cole-Sevelam hydrochloride



side effects

constipation



Increases TG : triglecyrides

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insulin secretagogus



SFU



mechanism of action

- increasing insulin secreation by binding to specific receptor at B-cells

- increasing insulin secreation by binding to specific receptor at B-cells

SFUs



administration

before meals by 30-60 min



never to fasting

SFU



frequency of pills

once ( esp. lomg acting)



twice daily

SFUs


main side effects

-hypoglycemia\\wt gain

SFUs



examples #4

1-Gli(b)enclimide = Daonil= Glibil



2-Gli(m)epride = Amaryl / Glemax



3-Gli(c)lazide = Dimicron



4-Gli(p)izide

Glibenclamide



other name

Glyburide

Glibenclamide




trade name

Daonil


 


Glibil

Daonil



Glibil

Glibenclamide



dose

1.25 - 20



5 mg X2



10 mg X2 max

Glibenclamide




renal impairment

avoid



also in elderly



high risk of hypoglycemia

Glibenclimide + metformin



brand name

Glucovance



Diamet

11

11

11

11111111

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11

Glipizide

short action 2-3 X


once if ling acting

1111

11

1111

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Gli(M)epride



administration


longest duration



once daily

Gli(M)epride



brand name

Amaryl


 


Glemax

Amaryl



Glemax

Gli(M)epride




doses

1 mg >>>>> 8 mg

Gli(M)epride + glucophage



brand

Amaryl M

Amaryl M

11

11

11

11

Gli(c)lazide


brand name

Di-mi(c)ron


 


dimicron

Di-mi(c)ron



dimicron

11

11111

1111

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non-SFUs segreatagogus



examples ((-glinide grop))

-meglitinide



-Repaglitinide



-nateglitinid



_________________________________-


X3 with meals

meglitinide



??

short acting secretagogus



5-20 X 3 (meals)

Repaglitinide



short action / half life



within 30 min before meals



0.5 - 4 mg X 3 (meals)



hypoglycemia / wt.gain

Natiglinide

D-phenylalanine derevatives



within 10 mino of meals



low hypoglycemia risk



to control postprandial hyperglycemia




18- - 320 X 3

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1

injectable drugs for Type 2 DM

GLP agonist

GLP agonist



mechanism

similar to endogenous GLP 1 = incretin



resistant to degradation by DPP-IV enzyme

GLP agonist


administration

SC



GLP agonist



advantages

- improved satiety



-wt loss

GLP agonist



examples

Exenatide




Liraglutide

GLP agonist



Exenatide



doses/admin

-daily doses (X3 meals)



-weekly dose

GLP agonist



Exenatide



daily dose

5 - 10 micg X3

GLP agonist



Exenatide



weekly dose

2 mg / wk

GLP agonist



Exenatide



side effects

-pancreatitis



-renal impairment

GLP agonist



Exenatide



advantages


wt


HbA1c

-wt loss = 4 Kgg



-Hba1c 0.6 - 1.2 %

GLP agonist



leraglutide

SC



Once daily



0.6 ..... 1.2......1.6

GLP agonist



leraglutide



side effects

-nausea



-vomitting



-dizziness



-headach

GLP agonist



leraglutide



possible side effects in animal models

increased calcitonin and thyrois]d medullary cancer

injectable medication for type 1+2

Amylin analogues

amylin analogue



mechanism

blunting postprandial BG

blunting postprandial BG

amylin analogue



example

pram-lintide


 


SC


 


15 - 120 mic


 


before meals

pram-lintide



SC



15 - 120 mic



before meals