Sie sind auf Seite 1von 3

Drugs used in management of DIABETES MELLITUS

HUMAN INSULIN PREPARATIONS


DRUG ULTRA- SHORT SHORT ACTING INTERMEDIATE ACTING LONG ACTING
CHEMISTRY Insulin Lispro (IL)
Human insulin analog - same
except for inversion of
proline(28)-lysine(29) a.a.
sequence on B chain more
rapid asorption! faster onset
" shorter duration of axn
compared to regular insulin
#lear appearance
$o added protein
%hosphate uffer
Insulin Aspart
&nalogue of human
insulin is an insulin pen
($ovo'apid(lex%en).
%roline is replaced at
position 28 y aspartate
on the B chain

Regular insulin
MECHANISM
OF ACTION
ABSORPTION )xerts effect *+in ,-min of s+c
'.&. /ery rapid! can give
given immediately efore a
meal
0anufactured y recominant 1$& tech
%lasma 2-,+2 3 ,4min
'.&s5
,. 6+c
2. 70
8. 7/ 9 insulin only: 6%H " lente are suspensions $.2 given 7/
;. 7% 9 used in end-stage renal failure pts on amulatory peritoneal dialysis " are diaetic. &sored into 7% mem. #os of shrin<age of renal tissue! less <ny meta of insulin! can
give less insulin
-. 7nsulin aerosol 9 ne* route. 7nsulin asored y lung capillaries
%rolems5
a. (actitious hypoglycaemia (inappropriate ta<ing of insulin)
. Hypoglycemia5 .1 of insulin in a diaetic. #an go into coma! may get #$6 sequelae even if recover. 2each diaetic to recogni=e " deal *ith hypoglycaemia
c. >ipodystrophy5 lipoatrophy " lipohypertrophy
7ncreased glucose levels result in &2% levels in the eta cell. 2his causes &2%- sensitive potassium channels to close! thus depolarising the cell memrane. 7nflux of calcium occurs as a result
of the opening of voltage- gated calcium channels. 2he increased intracellular calcium in turn triggers secretion of insulin.
7nsulin receptors5
- #irculating insulin inds to specialised receptors on the memranes of most tissues! particularly the liver! muscle and adipose tissues
- 2he insulin receptor consists of 2 heterodimers! each containing an extracellular alpha su- unit (*hich is the recognition site) and a eta suunit (containing the en=yme! tyrosine
<inase) *hich spans the cell memrane.
DRUG ULTRA- SHORT SHORT ACTING INTERMEDIATE ACTING LONG ACTING
soon after meals
;--x+d inconvenient
%ea<5 84-94 min after admin
(earlier than regular insulin)
7mm action on post-prandial
glucose increase
1uration of axn5 ?-hrs
DISTRIBUTION
METABOLISM 2 STEPS: (in liver & renal !"!le#$
%& Re'!(ive (leava)e *+
'i#!l,-i'e "*n'# ". in#!lina#e
()l!a-i*ne in#!lin
ran#-.'r*)ena#e$
2& Pr*e*l.#i# *+ ,e,i'e (-ain# ".
,e,i'a#e#
ELIMINATION
CLINICAL USES Re#erve' +*r a(ive in'ivi'!al#
(.*!n)er ,e*,le$ /-* 0a. "e 0!li1
a#2in) an' 0a. re0e0"er * a2e
-eir 0eal# re)!larl.
AD3ERSE
DRUG
REACTIONS
,. &llergy!
2. >ipodystrophy!
8. Hypoglycaemia!
;. &normal la tests.
6light change in amino acid position ma<es it antigenic
DISAD3ANTAG
ES
0ore expensive (higher unit
cost) than regular insulin
0ore freq in@ections needed
cos of ultra-short duration of
axn 9 adds to cost

Das könnte Ihnen auch gefallen