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8/18/2019 2. DM Drugs
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Diabetes Complications Treatment
Hypoglycemia
- Sweating, tremor, tachycardia, anxiety, hunger- MOA: dec. blood glucose (+ !pi- "ost#prandial (low blood glucose a$ter lunch- %asting (impro&es w' sugar
nsulinoma Hyperinsulinism: benign insulin#producingtumor
- serum insulin ) ug'm* blood glucose - mg'd*(inappropriate high insulin despite low blood glucose
- ele&ated plasma insulin and insulin:glucose- ele&ated proinsulin and / peptide
%actitious Hyperinsulinism: sel$#ingestion o$ insulin(0*"12!
- 3riad o$ Hypoglycemia + Antibodies + Suppressed
plasma / peptide- ele&ated plasma insulin and insulin:glucose ratio
0lucagon:Use:
- Hypoglycemia- Severe hypoglycemia (1mg IV)- n!ocrine !iagnosis- 4eta#bloc5er O2 (inc" c#$% in heart)
increase! ins&lin release Hypoglycemia- 'a!iology o boel (rela*es intestine)
2extrose: Use: Hypoglycemia+ D,#
2ia6oxide: To*icity: hyperglycemia+ etoacitosis
$ patient is conscious (78 40* oral
glucose
$ patient is unconscious (- 40*
0lucagon
Surgery: remove ins&linoma
2iabetic 9etoacidosis 2M type
- nc. plasma glucose (- mg'd*, H+, 5etones, 9+- 2ec. H/O, ntracellular 9+
- "recipitated by: insu;cient insulin therapy, in$ection,emotional stress, excess alcohol use- "resents w' $ruity odor o$ acetone on breath
< regular insulin
< =uids
2extrose
4alance electrolytes, 9+
Hyperosmolar coma' Hyperosmolar Hyperglycemic >on#9etotic Syndrome (HH>S 2M type
- "recipitated by: in$ections, stro5es, M, elderly, 2M- 2iagnosis: blood glucose 7? mg'd*, high serum osmolality, high 4@>, no 5etosis- 2ue to 2ecreased nsulin ncreased 0lucagon
0lut beta cell
- Higher 9m (lower a;nity allows the muscles to utili6ed glucose
Brst.o >eed high amount o$ glucose to stimulate
0lut - muscle cells
- *ower 9m (higher a;nity allows muscles to utili6e any small
amount o$ glucose.
0lucose 0*@3 enters beta cell glucose metabolism inside
cell inc. A3" closure o$ 9+ channels inc. 9+ inside cell
depolari6ation stimulation' opening o$ /a++ channels /a++ into beta cell degranulation
release insulin into circulation
- CD'D >"H'regular insulin
- ED'ED >"*'*ispro insulin
- CED'ED >"*'*ispro insulin
- CD'D >"A'Aspart insulin
Note: insulin glargine and detemir must be gi&en as
separate inFections.
nsulin indications:- 2M (?' gestational 2rug o$ choice $or
0estational- 29A
- Hyperglycemia ' >on#9etotic /oma
How do you gi&e the insulin shotG $ u want to gi&e
units' day you ha&e to gi&e ' o$ the daily dose in the morning and gi&e the remaining ?' at
night. 3his is to a&oid hypoglycemia which could be caused by inc. acti&ity and $ood during the day
Dr&g &se! to treat
8/18/2019 2. DM Drugs
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Type II D$ Dr&gs:
8/18/2019 2. DM Drugs
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1st gen.
Sulfonylurease
(not used
clinically due to
A!
Tobl&tami!e Short t1./" In!icate! . el!erly an!
renal !ys&nction
MOA: 4loc5 9+ channels
beta cells cell
depolari6ation /a+ in=ux
nsulin granule release
@se: 3ype 2M (need wor5ing4eta cell
/ontraindication: hepatic
renal insu;ciency
A!: hypoglycemia w' long#
acting drugs, weight gain,
rashes, hypersensiti&ityIx nteractions: inc.
hypoglycemia w' /imetidine,
nsulin, Salicylates,
Sul$onamides
Tol0ami!e Short t1./
Chlorproprami!e ong !&ration (23h)
#: Dis&l4ram-lie r*n5 SI#DH+
6a&n!ice+ le&copenia+ 7
thrombocytopenia
2nd gen.
Sulfonylurease0lipi6ide Short-acting
Sa$e w' mild to mod. renal
dys$unctionDec" !ose in hepatic !ys&nction
0lyburide ong-actingSa$e w' mild#mod. hepatic
dys$unction
Dec" !ose in renal !ys&nction
0limepiride ong-acting+ once.!aily !ose
Meglitinides
(may be ta5en
alone or w'
biguanides
Iepaglinide
>ateglinide (D-phenylalanine)
$8#: Same as Sul$onylureas but mainly stimulates the Brst phase
o$ insulin secretion
Use: %ost-pran!ial hyperglycemia in type / D$" In!icate! in pt" . s&l&r
allergy
9ateglini!e: sae in renal ins&ciency+ loer ris o hypoglycemia
Insulin
sensitizers
4iguanide:
Met$ormin
;&glycemic '* (!oes
not ca&se
hypoglycemia)
;9o eight gain
$8#: (-phosphate DH (-)
gl&cose o&tp&t rom liverUse: !ec" ins&lin resistance in obese type / !iabetics
#: anorexia, nausea, &omiting, diarrhea+ lactic aci!osis (anion gap)+
vit" ?1/ !e4ciency
Contrain!ications: alcoholism+ renal 7 hepatic !isease+ chronic
car!iop&lmonary !isease+ ra!iographic contrast+ aci!osis
3hia6olidinedion
es:
"ioglita6one'osiglita0one
(#,# =IT#@89S)
$8#: bind ""AI#gamma in nucleus !ec" ins&lin resistance inc"
gl&cose &ptae !ec T= levels
#: =uid retention, edema+ inc" ris o HA (especially 'osiglita0one)+
weight gain+ !ec" bone mineral !ensity+ bone ract&res in omen+
hepato!o*iticy
'* interactions: !ec" ecacy o 8C b.c is metaboli0e! by cyt pB3
Alpha-
glucosidaseinhibitors
Acarbose
Miglitol
$8#: (# J#glucosidase in 03 !ec" gl&cose absorption !ec"
!eman! or ins&linUse: control post-pran!ial hyperglycemia
#: =I !iscomort+ at&lence+ !iarrhea+ hepatoto*icity
D-!
inhibitorsSitagliptin
Saxagliptin
$8#: (# 2""- (# 0*"? inacti&ation inc" =%1 action inc"
gl&cose-me!iate! ins&lin secretion 7 !ec" gl&cagon lvls
#: naso-pharyngitis+ &pper respiratory inections+ hea!aches+
hypoglycemia+ ac&te pancreatitis+ Foint pain
"#-1 agonist !xenatide (IV)
*iraglutide (IV)
$8#: (