Gall Stones Pharmacology 3
rd
-stage
1 |
P a g e
Treatment of Gall Stones:
Cholesterol solubilized in aqueous bile by combine effects of bile salt & lecithin,
all together form micelle. When cholesterol is secreted in excess to lecithin & bile
salt acid their crystals precipitate & may coalesce cholesterol gall stones that
caused by
1- Impair bile salt secretion.
2- Excess cholesterol secretion.
3- Combine effects of both 1&2.
Treatment include:-
1-CHENODIOL: which is a primary bile acid in man & URSODIOL is a 7β
epimer of chenodiol, both are effective in dissolving cholesterol stones in some
patient by expanding bile salt pool by inhibiting rate-timing enzyme of
conversion of bile salt into cholesterol [HMG-CoA reductase] this end in
increasing bile salt secretion & decrease cholesterol secretion. . They able to
dissolve a stone less than 5 mm, floating stone in functional gall bladder. a high
recurrence rate after stopping therapy so long life therapy may be consider in
patient who response well to initial therapy . their dose 10-15 mg/kg as daily
single dose at bedtime or divide doses depending on stone size , treatment
continue to 3 months after dissolving the stones . their side effects include
[diarrhea ,pruritis , raising level of aspartate transaminase in plasma ( ursodiol of
less causing such effects so of preferable in uses ) . their contra-indication are
[pregnancy , chronic liver disease , inflammatory disease of intestine & colon ].
2-METHYL-TERT-BUTYL-ETHER: can dissolve cholesterol stones in gall
bladder & bile duct when infuse into bile duct or gall bladder via catheter directly ,
ether of boiling point of 52.2c
0
so remain liquor at body temperature , excellent
dissolving of cholesterol stones within hours . Can be use for non-operative
patients.
3-MONOCTANOIN [GLYCERYL1-1MONOOCTANOATE] other agent
infuse into common bile duct via catheter or T tube cause complete dissolving of
stone or reduce its size to be sufficient for subsequent removal
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Treatment of pancreatic insufficiency (pancreatic supplement):
Pancreatic enzyme supplement is indicated as pancreatic enzymes are deficient or
absent as in cystic fibrosis, chronic pancreatitis, pancreatectomy, gastrointestinal
bypass surgery, ductal obstruction from neoplasm .Also this preparation used to
Gall Stones Pharmacology 3
rd
-stage
2 |
P a g e
treat a condition like statorrhea associated with postgastrectomy syndrome &
bowel resection. Other uses as diagnosis test for pancreatic insufficiency.
1-Pancrelipase: it is an agent derived from porcine pancreatic enzyme & contain
lipase, amylase & protease which capable of digest fate, starches & protein
respectively. It is a 12 times the lipolytic activity, 4 times the proteolytic activity
& 4 times the amylolytic activity of second form of pancreatic supplement that
called pancreatin . pancrelipase act as : following activation in alkaline pH of
duodenum it release high level of lipase , amylase & protease which facilitate the
hydrolysis of fat into glycerol & fatty acid, starches into dextrins & sugar ,
protein into proteoses . Factor influence the effectiveness of pancrelipase are dose,
gastrointestinal pH, & microshere size of products. It is not absorbed via GIT so it
exert its effect locally. its preparation of two types 1- that contain enteric-coated
microsphere of pancrelipase to inhibit gastric inactivation /2- free of enteric
coating enzyme need to be administrated with H2 antagonist , omperazole ,
misoprostol , NaCO3 , Al(OH)3 . It is excreted in feces. Its dose as 8000 USP
units of lipase /17 g of dietary fat orally (for adult 1-3 tablets /day & 1-2 tablets
for children as powder 0.7 g , as capsule 1-2 with meals or before it ).
Contraindicated in breast feeding, pancreatitis, porcine hypersensitivity &
pregnancy. Their adverse effects include [most often reported adverse effects is
skin rashes, sneezing & lacrimation. GIT at usual dose nausea vomiting,
abdominal pain & diarrhea, at higher dose hyperuricosuria & hyperuricemia. If
retain drug in the mouth it cuase mucosal ulceration & stomatitis] their powder is
irritable for nasal mucosa & respiratory tract. So it may induce sneezing &
bronchospasm & may precipitate attach of asthma.
2- Pancreatin: it is less potent than pancrelipase. Can be use in acute pancreatitis.
it is of no side effects on respiratory system .
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