ก F
scope
1.Anti-emetics drugs; ก ก F
2.Agents for treatment of peptic ulcer : ก
3.Antidiarrheal drugs : ก ก F F
4.Anticonstip...
1.Anti-emetics drugs; ก ก F
ก F
ก ก F ก ก
F F ก ก ก F ก F ก
2 F ˈ ก2 F ˈ ก
: F( F ) / /
ก ก ก F
Cerebral cortex(higher center)
NK1,GABA
Pain,smell,sight,taste→ ←Memory,fear,
hearing,stress,
thinking
Vomit cente...
F( F ) ก F ก ก N/V
Vomitting center ( F ) กก F
ก F( F ) F
1.Cerebral cortex (higher center) กF1.Cerebral cortex (higher ce...
F( F ) ก F ก ก N/V
2.Chemoreceptor trigger zone (CTZ)
area postrema F Medulla ( F
Blood Brain Barrier) F กBlood Brain Barr...
F( F ) ก F ก ก F
3.Vestibular system ( ก F F )
vestibular F F ก
acetylcholine histamine F vomitting center Facetylcholine ...
4.Stomach,small intestine F vagus nerve
F nucleus tractus solitarius (NTS) ก nucleus
F fibers F vomitting center
e.g.Cytot...
5.Glossopharyngeal nerve Trigerminal nerve
F F nucleus tractus
solitarius (NTS) F F F vomitting center
F( F ) ก F ก ก F
so...
ก F ก N/V
(neurotransmitters)
(receptor)
1.Acetylcholine
2.Dopamine
1.MuscarinicM1 receptor
2.Dopaminergic receptor (dopam...
F ก F
F ...
Dystonia :
ก F ก F F ก ก
F F F F ˁ
Extrapyramidal side effect (EPS)
F F F F ˁ
1.http://www.youtube.com/watch?v=VHGzUxnuvwQ...
Extrapyramidal side effect (EPS)
Parkinsonism:
ก ก F ก ก F / F
ก F (posture) กก F (posture) ก
http://www.youtube.com/watch...
Tardive dyskinesia :
ก F ก F F
F ˁ ก ก ก F ˈ
Extrapyramidal side effect (EPS)
F ˁ ก ก ก F ˈ
F F F F ก ก/
F กF
Extrapyramidal side effect (EPS)
Tardive dyskinesia :
ก ก ก ก ก
ʾ ก ก F ก กʾ ก ก F ก ก
ก ก 2 F
http://www.youtube.com/watc...
Anticipatory CINV
(Anticipatory chemo therapy-induced nausea and vomiting)
ˈ ก กF ก F
ก ก ก ก ก N/V กก ก ก ก ก N/V ก
กF F
...
Nausea and vomiting ก
Acute nausea and vomiting:
ก 24 F
ก ก 24ก ก 24
Nausea and vomiting ก
Delayed nausea and vomiting :
ก F F ก F 24 hr
F F 5-7 FF F 5-7 F
Anti-emetics drugs
1. Muscarinic M1 antagonist
2. Dopamine D2 antagonist
3. Histamine H1 antagonists
ʽ ก
(receptor) ก F F ...
1)Anti-emetics drugs ;Muscarinic M1 antagonist
e.g.Scopolamine (hyoscine)
ก ก : ʽ ก muscarinic M1 receptor
Common ADR: ADR...
2)Anti-emetics drugs;Dopamine D2 antagonist
e.g. Domperidone(Motilium®),Metoclopramide(Plasil®),
(Chlorpromazine,Perphenaz...
2)Anti-emetics drugs;Dopamine D2 antagonist
2. ʽ ก 5 HT3 receptors GI ,
e.g.Metoclopramide (high dose)
3. F Fก
ก / F (gast...
2)Anti-emetics drugs;Dopamine D2 antagonist
ADR: F ก F ก ก ก F
Domperidone/metoclopramide
↑ก prolactin hyperprolactinemia-...
2)Anti-emetics drugs;Dopamine D2 antagonist
Domperidone /metoclopramide ;
Take the tablets 30 minutes before each meal and...
3)Anti-emetics drugs;Histamine H1 antagonists
e.g.Dimenhydrinate(Dramamine®)(+antimuscarinics)
,Diphenhydramine(Benadryl®)...
4)Anti-emetics drugs;5-HT3 antagonist :
e.g.Ondansetron(Onsia®),Granisetron,Dolasetron,Tropisetron
ก ก:
ʽ ก 5-HT3 receptor...
4)Anti-emetics drugs;5-HT3 antagonist :
F ondansetron
first dose :30 minutes before the start of chemotherapy
1 to 2 hours...
5)Anti-emetics drugs;Substance P antagonist ; NK1 receptor antagonist:
e.g.aprepitant
ก ก :
ʽ ก F F substance P ก F NK1 re...
6)Anti-emetics drugs;Others; Pyridoxine (Vit B6)
ก ก:
B6 ˈ coenzyme F Glutamic decarboxylase
ก ก Glutamic acid ˈ GABAก ก G...
7)Anti-emetics drugs ;Others;Benzodiazepines
e.g. lorazepam (Ativan®)
ก ก:
ก benzodiazepine GABAA-receptor ionorphoreก ben...
8)Anti-emetics drugs;Others;Steroids
e.g.Dexamethasone, Methylprednisolone
ก ก :
ก F 5-HT F กก F 5-HT F ก
Common ADR:
GI i...
8)Anti-emetics drugs;Others;Steroids
F dexamethasone
Acute nausea and vomiting
/ กF F/ กF F
Delayed nausea and vomiting
: ...
ก ก F ก ก F
ก ก F
1.Motion
sickness ˆ ก
HistamineH1 antagonists:
e.g.dimenhydrinate,meclizine
Effective if take before ½ h...
ก ก F ก ก F
ก ก F
2.Morning
sickness
N/V in pregnancy
Select safety to fetus
Vitamin
B6 +doxylamine (firstsickness Select ...
ก ก F
3.Postoperative
N/V (PONV)
N/V after surgery
opioid:relief pain
opioid:(+)CTZ
5-HT3 antagonists (all.gold
standard)
...
ก ก F ก ก F
ก ก F
4.Radiotherapy-
inducedN/V
(RINV)
Mechanism ~ cytotoxic D2 antagonists
e.g.metoclopramide
5-HT antagonis...
ก ก F ก ก F
ก ก F
5.Chemo
therapy-
induced
cytotoxic
1.CTZ
2. F ก
5-HT3 antagonist(all.acute/delayed)
gold standard
D anta...
ก ก F ก ก F
ก ก F
5.Chemo
therapy-induced
N/V(CINV)
*NK1 receptor antagonist(acute /delayed)
e.g.Aprepitant
N/V(CINV)
(*) ...
ก ก F ก ก F
ก ก F
6.Combine tx
for Acute CINV
- 5-HT3antagonist+steroid(best treatment)
effective than single drug and low...
ก ก F ก ก F
ก ก F
7.Gastroenteritis
( F ก )
- D2 antagonists
e.g. metoclopramide( F ก ) e.g. metoclopramide
8.Gastroparesi...
ก
Agents for treatment of peptic ulcer
Antacid
Anti-secretory drug
Mucosal resistance(Cytoprotective)Mucosal resistance(Cy...
Parietal cells mucosa ก
Receptor ( ) ก F ก ก ก
F ก ก F ก ก F
ก ก
F ก ก F ก ก F
receptor
Second messenger
F H+/K+ ATPase or...
ก F F ก ก ก
Receptor ก F ก
ก F (Receptor)
Histamine-2 receptor HistamineHistamine-2 receptor
(H2 receptor)
Histamine
Musca...
F ก F
1.Second messenger
ก F F กก ก F
Second messenger กF F ก กSecond messenger กF F ก ก
F
Second messenger F ก
ก ก กก ก F
F ก F
2.Phosphate Binders
F ก phosphate
F phosphate form ˈ insolubleF phosphate form ˈ insoluble
compound ก ก
ก กก ก
1. receptor
2. F ก secondary messengers
Cyclic AMP (cAMP)Cyclic AMP (cAMP)
Calcium
ก กก ก
Histamine:
(+) F adenylate cyclase (ATP cAMP)
Gastrin ,acetylcholine:
ก calcium ก F cell
↑calcium cell
(+) F adenyl...
ก กก ก
3.cAMP ↑, calcium ↑ (+) H+/K+ ATPase at
parietal cell membrane
4. F ก ก ก hydrogen ion4. F ก ก ก hydrogen ion
ก ก (...
ก กก ก ก parietal cell
: F hydrogen/potassium adenosine triphosphate (H+/K+ ATPase gastric proton pump )
Gastric pH <3 ( ˈ ก ก) ก ก F
1. ก gastrin
ก กก ก ก
2.Prostaglandin (PGE2 ) histamine ก
ก F adenylate cyclase
(peptic ulcer)
Peptic ulcer
ก/ ก ก / F ก F F +
ก ก กก ก ก
ˈ ก aggressive factor -defensive factor
imbalance
ˆ F ก ก peptic ulcer
Aggressive factor Defensive factor
ก parietal cell
mass
ก ก /bicarbonate
mass
ก
ก
F
mucosa (mucosa
ก ...
ˆ F ก ก peptic ulcer
Aggressive factor Defensive factor
ก F prostaglandin
inhibitor
ก
epithelial cell (cellinhibitor
(e.g....
ก Peptic ulcer
F ʾˉ F ˈ ก
Duration : day/wk
ก ก ˈ F ก
ก ก DU/GU
F ก F
ก ( F )
ก ก ˈ F ก
ก Peptic ulcer
F ก (Duodenal ulcer;DU)
ก ก F F F
กF กกF ก
Relief : / F ก
ก (Gastric ulcer;GU)
ก ก F F F 1-3
F ก ก
ก
F
ก ก ˈก ก ˈ
ก ก F ก ˈ
e.g.haemorrhage ,obstruction ( ก scar),perforation
ก
Agents for treatment of peptic ulcer
Antacid
Anti-secretory drug
Mucosal resistanceMucosal resistance
Misc.
-Rebamipide
...
1.Antacids ( ก )
e.g. aluminium salt , magnesium salt, sodium bicarbonate
ก ก:
1.ก ก (acid neutralizing effects)1.ก ก (aci...
1.Antacids ( ก )
F ก F F F
rapid onset : within 5-15 min
duration : 15 min-1 hrduration : 15 min-1 hr
F ก
F F F
ก F F ก F ...
1.Antacids ( ก )
ADR : Aluminium salt ( F ก), Magnesium salt
( F )
Drug interaction (DI) :Drug interaction (DI) :
↓ absorp...
1.Antacids ( ก )
antacid (aluminium salt) ก phosphate ก
phosphate F ˈ phosphate binder F ˁ
Drug interaction (DI) :
phospha...
2.1 H2 receptor antagonist (H2RA)
2.2 Proton pump inhibitor (PPI)
2.Anti-secretory drugs ; ก ก
2.1 H2 receptor antagonist (H2RA)
e.g.ranitidine, famotidine, nizatidine, cimetidine
ก ก
F histamine ก ก H receptorF hista...
cimetidine ranitidine nizatidine famotidine
1 4-10 4-10 20-50
Dose of
treatment
400 bid
800 hs
150 bid
300 hs
150 bid
300 ...
2.1 H2 receptor antagonist (H2RA)
food : not affect to absorption
Treatment
DU : 6-8 wk if not cure F F ก 2-4 wkDU : 6-8 w...
ADR:
F F / F ก F
F F F
2.1 H2 receptor antagonist (H2RA)
F F F
cimetidine (antiandrogen effect) in men/high dose
/long ter...
2.1 H2 receptor antagonist (H2RA)
Drug interaction (DI)
antacid , sucralfate : ↓ absorption of H2RA
F antacid/sucralfate F...
2.2 Proton pump inhibitor (PPI)
e.g.omeprazole(Losec®),lansoprazole(Prevacid®),
pantoprazole(Controloc®),rabeprazole(Parie...
ก / ก F H2RA
Food delays absorption
ADR :
2.2 Proton pump inhibitor (PPI)
ADR :
F F F ˁ F F F F F F ก
F
2.2 Proton pump inhibitor (PPI)
Drug interaction (DI)
PPIs ก metabolize ก Cytochrome
P450 enzyme (CYP450)
ก ก metabolize F...
ก F PPI (enteric coated tablet) F ˁ F NG tube
NG tube (Nasogastric tube )
ก F F ก
F กF ก
F
F / กF F ˁ F
F ก
Enteric coated tablet/granules
F ก F ก F ก
ก ก (capsule) ก กก ก (capsule) ก ก
Enteric coating ก F F F
F ก
ก granules ก F ก...
omeprazole (miracid® )
delayed-release capsule/multiple unit granules system
enteric-coated granules
ก F PPI (enteric coat...
rabeprazole (pariet®)
delayed-release tablet or enteric-coated tablet
drug is absorbed in the intestine
ก F PPI (enteric c...
Omeprazole
1. ก capsule
2. granules NG F
Gastric : ˈ ก
ก F PPI (enteric coated tablet) F ˁ F NG tube
Gastric : ˈ ก (protec...
Mucosal resistance ;Cytoprotective
ก ก ˂ ก F F ก
ก F
Cytoprotective agents :Cytoprotective agents :
Sucralfate
Bismuth pre...
Sucralfate
ก ก:
1.sucralfate กก (viscous substance)
ก กก ก
ก ˂ ก ก ก
Sucralfate
2.ก F endogenous prostaglandin
ก PGE2 F
- F ก ˂ ก- F ก ˂ ก
- gastric mucus secretion F ก F
3. F F F ก ก
Sucralfate
ADR:
sucralfate ก ก F F ก ก F
systemic F ก F F กF F ก Fsystemic F ก F F กF F ก F
F F ก F ˈ ก F
F
Sucralfate
Drug interaction:
ก
F sucralfate F F (กFF sucralfate F F (กF
1 )
Bismuth preparation
e.g.bismuth subsalicylate (GASTRO-BISMOL®),
ranitidine bismuth citrate
ก กก ก
1. ก bismuth ก ก
ก F F ˈ...
Bismuth preparation
2.ก F ก F prostaglandin, bicarb, ก
3.ก ก H.pylori
4. F neutralize ก4. F neutralize ก
ADR ;
- ˆ
-bismut...
Prostaglandin analogues
e.g.Prostaglandin E analogues (misoprostol;cytotec®)
ก ก:
ก prostaglandin receptor parietal cellก ...
Prostaglandin analogues
ADR;
F F (4-38%)
F F N/VF F N/V
ก F F F F
(FDA pregnancy category X )
Prostaglandin analogues;misoprostol;cytotec®
ก F off-label
F F
F กF ก
ก ก (postpartum hemorrhage)
F off-label F ก ก ก F F ก
Misc. ;Rebamipide (mucosta®):
ก ก ( / ):
↑ PGE2 ก F ก
↑ ก/ ก ก
↑ก ก ก↑ก ก ก
F ก F ก
F ก F F ก/ F ก
ก F interleukin-8 (IL-8...
Misc.; Rebamipide (mucosta®):
ADR;
leukopenia ( ก F ก ) ,
thrombocytopenia ( ก )thrombocytopenia ( ก )
hepatic dysfunction...
Combination treatment
Single (2-3 wk)+eradicate risk factors not cure
combine
ก (Eradication) H.pylori (HP)
Helicobacter pylori :
ก ก
F F ก ก กF F ก ก ก
(urease enz.) F urea ammonia+CO2
ammonia : ก ก ...
ก (Eradication) H.pylori (HP)
ก H. pylori
( )
PPI-based triple therapy
PPI bid + amoxicillin 1 g bid + clarithromycin 500
...
ก (Eradication) H.pylori (HP)
ก H. pylori
( )
Bismuth-basedquadruple therapy
PPI bid + bismuth 240-525 mg bid +
14
PPI bid...
ก (Eradication) H.pylori (HP)
ก H. pylori
( )
Sequentialtherapy
PPI bid + amoxicillin 1 g bid ˈ 5 F F
10
PPI bid + amoxici...
ก (Eradication) H.pylori (HP)
ก H. pylori
( )
Levofloxacin-basedtriple therapy 10Levofloxacin-basedtriple therapy
PPI bid ...
ก (Eradication) H.pylori (HP)
ก H. pylori
( )
Concomitanttherapy 10Concomitanttherapy
PPI bid + amoxicillin1 g bid + clari...
ก (Eradication) H.pylori (HP)
PPI-based triple therapy sequential therapy
Bismuth-based quadruple therapy
Levofloxacin-bas...
NSAIDs-induced peptic ulcer
ก กก ก NSAIDs-induced peptic ulcer
ก F prostaglandin
- F mucosal blood flow- F mucosal blood flow
-mucus secretion , HCO3 ...
NSAIDs-induced peptic ulcer
ก ˂ ก (prophylaxis)
F ˈ F Fก ˂ ก F ˁ
F NSAIDs กF NSAIDs ก
NSAIDs-induced peptic ulcer
ˆ (High risk)
> 60 ʾ
ก F
ก/ ก ก /ก/ ก ก /
F NSAIDs F ก corticosteroids
F NSAIDs ก F ก F
NSAIDs กก F 1 F ก
F F ก anticoagul...
NSAIDs induced peptic ulcer
ก ก (Treatment)
1. NSAIDs : H2RA ∼ PPIs
2. F NSAIDs F : Drugs of choice :PPIs2. F NSAIDs F : D...
ก ก F F (antidiarrheal drugs)
ก F F (diarrhea)
F F ˈ กก F
3 /
F ก F F 1
24
F F (diarrhea)
1. F
2. F F ก กก F
antibiotic (eg.clindamycin,tetracycline),antibiotic (eg.clindamycin,tetracycline),
ก
ก F...
ก ก ก F F
1. ก F กF
ก F ( ˁ / )
F IV :F IV :
ORS (oral rehydration salt) :
(Electrolyte=Na,K,Cl,HCO3) + ก
ก ก ก F F
F F
F F
F FF F
ก F F
ก ก ก F F
2.ก ก ก F F กก
2.1 F F ก (toxigenic diarrhea)
ก epithelial cell F F ก Fก epithelial cell F F ก F
enterotoxin ก
ก...
ก ก ก F F
2.2 F F กก ก F F
(invasive diarrhea)
ก ก ก Fก ก ก F
ก e.g.shigella, salmonella, E.coli
ก ก ก F F
F ก ˈ
Shigella ( F )
e.g.TMP/SMX (bactrim®),norfloxacin,ciprofloxacine.g.TMP/SMX (bactrim®),norfloxacin,ciproflo...
ก ก ก F F
3. ก ก ก F F
ก F / ก F F F
3.1 ก F3.1 ก F
3.2 F ก ก
3.3 Intraluminal agents
3.4 Bulk forming agents
3.5 Bile aci...
3.1 ก F
Opioid derivatives -Loperamide; Imodium®
-Diphenoxylate+atropine;Lomotil®
ก ก :ก F opioid receptors Fก ก :ก F opio...
3.1 ก F
Diphenoxylate ก atropine ˂ ก ก
F
Atropine : ก atropinism
e.g. F F F
F
3.1 ก F
ADR:
opioid F / F F
FF
F loperamide ก F ก F ก F
Diphenoxylate
3.1 ก F
ก F F F
ก F F
2 F ก F2 F ก F
F ˁ ก F กก invasive diarrhea
F F F
F ก ก F F
F ก F Fก F
3.2 F ก ก
Activated charcoal
Kaolin-pectin (Kaolin and pectin®)
Diosmectite (Smecta®)
3.2 F ก ก
ก ก : F ก F F ก
F F F
ˈ ก F F Fˈ ก F F F
ก F
ADR : F ก F F F
ก ˈ F F ก F
3.3 Intraluminal agents
e.g.Bismuth subsalicylates (GASTRO-BISMOL®)
ก ก : ก ก F
ADRADR
salicylism ( )
N/V
/
3.4 Bulk forming agents
e.g.Psylium(AGIOLAX®,METAMUCIL®,FYBOGEL®)
F F/ ก ก ก F
F กF ก
ก ก : F ˈ กF F
ADR F F F ก F
3.5 Bile acid binder
e.g.Cholestyramine (Questran®)
ก ก : ก ก toxin (clostridium
difficile toxin)difficile toxin)
F ก anti...
Cholestyramine ก bile acid
ก F F ก F F ก
ก bile acid ก
ก ก ก F ก F bile acid
3.5 Bile acid binder
ก ก ก F ก F bile acid
(c...
F ก F
Catabolism :
ก ก F
ก ก ˈ ก กก ก ˈ ก ก
ˈ F ก F / F F F
F
Antibiotic associated diarrhea
ก ก ก F F F
ก ก F F ก
F F ก F
Antibiotic associated diarrhea
F ก diarrhea F ก ก e.g.
1. Osmotic diarrhea
2. Bile salt diarrhea2. Bile salt diarrhea
3. ↑...
1.Osmotic diarrhea
↓ (non absorbable carbohydrate) F F
F F non absorbable carbohydrate FF F non absorbable carbohydrate F
...
2. Bile salt diarrhea
↓ F F( )
F bile salt F F
↑ bile salt↑ bile salt
ก F ก colonic fluid ก
F
3. ↑↑↑↑Small intestine motility
F e.g. erythromycin
ก F motilin receptor F กก F motilin receptor F ก
F ก
F
4. Microorganism infection
e.g. Clostridium perfrigen type A
Clostridium difficile
Antibiotic associated diarrhea
Cause
Drug : ampicilln,amoxycilln,cefixime,
fluoroquinolone(1-2%) bactrim (<1%)fluoroquinol...
ก ก Clostridium difficile diarrhea
ก F : +supportive tx
ก :metronidazole (oral) 10-14
*If not relieve ,no tolerance to dru...
ก ก F ก ก F F
ก
F opioid derivative (eg.+atropine) :serious S/E
F F ก / กF F ก / ก
: F ก ก + ก
/
/ ก F e.g. ORS
ก ก F ก ก F F
F
:
FF
loperamide (limited safety information)
diphenoxylate ( ก )
Anticonstipation ; กF ก F ก->laxatives/cathartics
ก F ก (constipation)
ก F ˁ
F F F ( F ก F 3 F F)
ˈ F Fˈ F F
F ก F F F
F ก F ก
ก ก
1. ก / F
ก ก ก F
ก กก กก กก ก
F ก (aluminium hydroxide)
ก F ʽˉ (tramadol,morphine,codeine,
fentanyl), bismuth , trihex...
ก ก
2. ก
ก ก : F ก
กก
ก กก ก F
ก ก
3.ก F
Bulk forming laxatives
LubricantLubricant
Stool softeners /emollient laxatives
Stimulant laxatives
Osmotic laxat...
Bulk -forming laxatives
F ˈ กF ก ก e.g.
ก ก ก
FF
ก ก (Ispaghula seed ,Plantago,
Psyllium) ;AGIOLAX®,METAMUCIL®,FYBOGEL®
F
...
ก ก
F ก F / F ก GI
ก F F ˈ ก
Bulk -forming laxatives
ก F F ˈ ก
F ˈ กF F F
ก F ก F F F
F F F
F F 1 wk
Fก ก F ก F F F
Bulk -forming laxatives
ADR;
fiber F ( F) gas
F F F
Bulk -forming laxatives
F F F
fiber + F F
Drug interaction ; ก ก
F ก 2 hr
** ก ก ก F ก F/ **
Lubricant laxatives
F ˈ ก e.g.
Mineral oil (synonym)
F (synonym)F (synonym)
liquid paraffin (synonym)
ELP(Emulsion of liqu...
ก ก ;
F F F ก
F F
Lubricant laxatives
F F
ก ก F F F ก ˈ ก
ก ˈ ก F F
ADR;
lipoid pneumonia ( ก ) ก ก
F
Lubricant laxatives
F
- F F กF
- F F กF F ˁ F F
- ก F : ก ก/ F ˁ / F ˁ
ก ก F ˀˊ
F F
F F F ( ;drug interaction)
Lubricant laxatives
F F F ( ;drug interaction)
Drug interaction;
ก F
(vit D def. F...
Stool softeners /emollient laxatives
e.g. Docusate
ก ก
F F F FF F F F
กF F F F
ก ก F
** F F F F ก ; F/
**
ADR ; F ก F
F F F
Stool softeners /emollient laxatives
Drug interaction;
ก F mineral,phenolpthalein
Toxic of mineral oil, ...
e.g. ก(senna) , bisacodyl (dulcolax®),phenolpthalein,
F (castor oil), dehydrocholic acid(Decholin® )
ก ก;
Stimulant laxati...
ADR;
Bisacodyl e.g. F F
Phenolpthalein e.g. ˆ ˈ
Stimulant laxatives
Phenolpthalein e.g. ˆ ˈ
Castor oil ( F ) e.g. ก ** F F...
Drug interaction; e.g.
bisacodyl (enteric coated tablet F ก F F)
F ก
Stimulant laxatives
F ก
ก / F
F ก F ก ก /
ก F ก F F 1
F
F F F ก > 1 wk
ก F ˈ ʾ F ก F
Stimulant laxatives
ก F ˈ ʾ F ก F
/ ก cathartic colon
(ก F ) F F F ก F F
F
enteric coated tablet F / ˂ ก ก ก
ก ( ก F F)
Stimulant laxatives
ก ( ก F F)
F ก F
Osmotic laxatives
ˈ ก e.g.
ก F ก
-Magnesium sulfate, citrate, hydroxide-Magnesium sulfate, citrate, hydroxide
(M.O.M/milk ...
Osmotic laxatives
Glycerine
Sorbitol
LactuloseLactulose
Lactitol
Osmotic laxatives
ก ก; ( ก F F F ก GI)
F F F F ก
(osmotic action) F ก ก ก(osmotic action) F ก ก ก
F
ADR; e.g. N/V, F ˂ F F...
Osmotic laxatives
Drug interation ;
ก F ก F F ก ˆ F ก
FF
Osmotic laxatives
F
ก F ก : F ˁ ก ก
- F ˁ- F ˁ
-
-
- ก F
Osmotic laxatives
F ก F ก F F
ก ก F ก electrolyte
imbalance ก F M.O.M F Fimbalance ก F M.O.M F F
ก F lactulose F ˁ
ˈ galac...
Hepatic encephalopathy
ก
ก
↓
↓
ก F F
↓
ก ก ˆ
F
ก metabolize ˈ
Hepatic encephalopathy
eg. cirrhosis
↓
ก metabolize ˈ
↓
↓
↓
Hepatic encephalopathy
ก hepatic encephalopathy
ก ก F F F
FF
ก F ก ก
ก F lactulose ก hepatic encephalopathy
Others ; ก (enemas)
e.g.
(tap water)
ก =NaCl = eg.unison enemaก =NaCl = eg.unison enema
sorbitol
F (soap solution)
ก ก; ก ...
ก ก F
:
bulk forming agents + life modification
(ก ก กก ก ʿกก F ˈ ) F F ∆ laxatives(ก ก กก ก ʿกก F ˈ ) F F ∆ laxatives
F ก...
ก ก F
F ˁ ก ก ก F
bulk forming agents
ก ก F ก ก Fก ก F ก ก F
lubricant/stool softener F ก F bulk forming agents
F ก ก e.g....
ก ก F
F ˁ / F
bulk forming agents F F bisacodyl
/senna/M.O.M/(lactulose;low dose) F F F F F/senna/M.O.M/(lactulose;low dos...
ก ก F
ก ก ก ก :
ก ก e.g.glycerin
suppo/ กsuppo/ ก
F F F F F F ; M.O.M./senna
F ˁ F ก :
saline laxatives e.g.magnesium sulf...
ก F ˂ (antiflatulants)
ก F ˂ (flatulence)
ก F ก F F F
กF
e.g.e.g.
F ก F
/ F ก F e.g. peptic ulcer
ก F ˂ (antiflatulants)
ก F (volatile oils)
ก F F ก ก (defoaming agent)
ก F (volatile oils)
e.g. pepermint oil , fennel oil ,cinnamon oil,
Cardamom, (stomachica mixture),
ก F ˂ (antiflatulants)
...
ก F (volatile oils)
ก ก
F F ก F
ก F ˂ (antiflatulants)
F กF F ก F
F ก กF ก
:ก F
F ก
ก F ˂ (antiflatulants)
F F Mixture Carminative Fก
ก F ก Alcohol ก
F F 8.8 F กF F 8.8 F ก
ก F F F ก
F กF ก
ก F F ก ก (defoaming agent)
e.g.Simeticone tab,susp.
Trade name :AIR-X , Belcid compound
ก F ˂ (antiflatulants)
Trade name...
F ˂ ก ก F ˂
ก ก F ก กF e.g.
F
F FF F
F
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  1. 1. ก F
  2. 2. scope 1.Anti-emetics drugs; ก ก F 2.Agents for treatment of peptic ulcer : ก 3.Antidiarrheal drugs : ก ก F F 4.Anticonstipation ; กF ก F ก -> laxatives and cathartics 5.Antiflatulants ; ก F ˂
  3. 3. 1.Anti-emetics drugs; ก ก F
  4. 4. ก F ก ก F ก ก F F ก ก ก F ก F ก 2 F ˈ ก2 F ˈ ก : F( F ) / /
  5. 5. ก ก ก F Cerebral cortex(higher center) NK1,GABA Pain,smell,sight,taste→ ←Memory,fear, hearing,stress, thinking Vomit center H1,5-HT3,D2,M1 CTZ area postrema D2,NK1, 5-HT3,M1,H1,opioid Cytotoxic,opioid→ Cardiac glycoside Nucleus tractus solitarius Stomach Small intestine 5-HT3,D2,NK1, opioid Gastric irritation Infect at GI,Ipecac cytotoxic,radiation Nucleus tractus solitarius (NTS) 5-HT3,D2,M1,H1,NK1 Glossopharyngeal nerve Trigerminal nerve F Vestibular system H1,M1 (motion sickness) Vomiting reflex Neuronal pathways Factors cause N/V
  6. 6. F( F ) ก F ก ก N/V Vomitting center ( F ) กก F ก F( F ) F 1.Cerebral cortex (higher center) กF1.Cerebral cortex (higher center) กF Stimulants N/V: ก ก F ก ก
  7. 7. F( F ) ก F ก ก N/V 2.Chemoreceptor trigger zone (CTZ) area postrema F Medulla ( F Blood Brain Barrier) F กBlood Brain Barrier) F ก CTZ Stimulants N/V: opioid ,cardiac glycosides ,cytotoxic
  8. 8. F( F ) ก F ก ก F 3.Vestibular system ( ก F F ) vestibular F F ก acetylcholine histamine F vomitting center Facetylcholine histamine F vomitting center F ก Stimulants N/V :ก (motion sickness)
  9. 9. 4.Stomach,small intestine F vagus nerve F nucleus tractus solitarius (NTS) ก nucleus F fibers F vomitting center e.g.Cytotoxic ก serotonin ก F( F ) ก F ก ก F e.g.Cytotoxic ก serotonin ก Enterochromaffin like cell F ก (+) 5-HT3 receptors F vagus nerve N/V Stimulants N/V : cytotoxics , gastric irritation , ipecac, ก GI, ก (radiation)
  10. 10. 5.Glossopharyngeal nerve Trigerminal nerve F F nucleus tractus solitarius (NTS) F F F vomitting center F( F ) ก F ก ก F solitarius (NTS) F F F vomitting center
  11. 11. ก F ก N/V (neurotransmitters) (receptor) 1.Acetylcholine 2.Dopamine 1.MuscarinicM1 receptor 2.Dopaminergic receptor (dopamine D2.Dopamine 3.Histamine 4.Serotonin (5-HT) 5.Substance P (SP) 2.Dopaminergic receptor (dopamine D2 receptor) 3.Histaminergic receptor (histamine H1 receptor) 4.5-HT receptor (5-HT3 receptor) 5.Neurokinin-1(NK1 receptor)
  12. 12. F ก F F ...
  13. 13. Dystonia : ก F ก F F ก ก F F F F ˁ Extrapyramidal side effect (EPS) F F F F ˁ 1.http://www.youtube.com/watch?v=VHGzUxnuvwQ 2.http://www.youtube.com/watch?v=N_daWx-qcaw
  14. 14. Extrapyramidal side effect (EPS) Parkinsonism: ก ก F ก ก F / F ก F (posture) กก F (posture) ก http://www.youtube.com/watch?v=j86omOwx0Hk
  15. 15. Tardive dyskinesia : ก F ก F F F ˁ ก ก ก F ˈ Extrapyramidal side effect (EPS) F ˁ ก ก ก F ˈ F F F F ก ก/ F กF
  16. 16. Extrapyramidal side effect (EPS) Tardive dyskinesia : ก ก ก ก ก ʾ ก ก F ก กʾ ก ก F ก ก ก ก 2 F http://www.youtube.com/watch?v=FUr8ltXh1Pc
  17. 17. Anticipatory CINV (Anticipatory chemo therapy-induced nausea and vomiting) ˈ ก กF ก F ก ก ก ก ก N/V กก ก ก ก ก N/V ก กF F Stimulants : ก F ก ก ก ก ก ก F กF
  18. 18. Nausea and vomiting ก Acute nausea and vomiting: ก 24 F ก ก 24ก ก 24
  19. 19. Nausea and vomiting ก Delayed nausea and vomiting : ก F F ก F 24 hr F F 5-7 FF F 5-7 F
  20. 20. Anti-emetics drugs 1. Muscarinic M1 antagonist 2. Dopamine D2 antagonist 3. Histamine H1 antagonists ʽ ก (receptor) ก F F F Histamine H1 antagonists 4. 5-HT3 antagonist 5. Substance P antagonist 6. Pyridoxine (Vit B6) 7. Benzodiazepines 8. Steroids
  21. 21. 1)Anti-emetics drugs ;Muscarinic M1 antagonist e.g.Scopolamine (hyoscine) ก ก : ʽ ก muscarinic M1 receptor Common ADR: ADR ˈ ก antimuscarinicCommon ADR: ADR ˈ ก antimuscarinic effect F ก F F F F ก
  22. 22. 2)Anti-emetics drugs;Dopamine D2 antagonist e.g. Domperidone(Motilium®),Metoclopramide(Plasil®), (Chlorpromazine,Perphenazine,Haloperidol,Droperidol) ก ก : 1. ʽ ก dopamine D receptor CTZ NTS ก ก : 1. ʽ ก dopamine D2 receptor CTZ NTS ( ก F domperidone F F Blood brain barrier ; BBB) F F CTZ F )
  23. 23. 2)Anti-emetics drugs;Dopamine D2 antagonist 2. ʽ ก 5 HT3 receptors GI , e.g.Metoclopramide (high dose) 3. F Fก ก / F (gastroprokinetic) e.g.Domperidone , Metoclopramide
  24. 24. 2)Anti-emetics drugs;Dopamine D2 antagonist ADR: F ก F ก ก ก F Domperidone/metoclopramide ↑ก prolactin hyperprolactinemia-related side effects F gynecomastia galactorrhea ↑ก prolactin hyperprolactinemia-related side effects F gynecomastia galactorrhea ก F domperidone ......... Metoclopramide ( Fdomperidone < F BBB;<EPS) Extrapyramidal side effect (EPS) F F esp. F ˁ (cause.tardive dyskinesia )
  25. 25. 2)Anti-emetics drugs;Dopamine D2 antagonist Domperidone /metoclopramide ; Take the tablets 30 minutes before each meal and bedtimebedtime
  26. 26. 3)Anti-emetics drugs;Histamine H1 antagonists e.g.Dimenhydrinate(Dramamine®)(+antimuscarinics) ,Diphenhydramine(Benadryl®), promethazine,meclizine ก ก:ก ก: ʽ ก histamine H1 receptor F vestibular system /vomitting center Common ADR: F ก F F ก
  27. 27. 4)Anti-emetics drugs;5-HT3 antagonist : e.g.Ondansetron(Onsia®),Granisetron,Dolasetron,Tropisetron ก ก: ʽ ก 5-HT3 receptor F ก (CTZ, NTS)ʽ ก 5-HT3 receptor F ก (CTZ, NTS) visceral afferent vagus nerve Common ADR: F / F ก F Serious ADR : QT prolong ( F ˁ ก ˂ ก ) cardiac arrhythmia
  28. 28. 4)Anti-emetics drugs;5-HT3 antagonist : F ondansetron first dose :30 minutes before the start of chemotherapy 1 to 2 hours before the start of radiation therapy1 to 2 hours before the start of radiation therapy 1 hour before surgery. Additional doses are sometimes taken one to three times a day during chemotherapy or radiation therapy and for 1 to 2 days after the end of treatment.
  29. 29. 5)Anti-emetics drugs;Substance P antagonist ; NK1 receptor antagonist: e.g.aprepitant ก ก : ʽ ก F F substance P ก F NK1 receptor NTSʽ ก F F substance P ก F NK1 receptor NTS ก cerebral cortex ก F vomitting center Common ADR : F F
  30. 30. 6)Anti-emetics drugs;Others; Pyridoxine (Vit B6) ก ก: B6 ˈ coenzyme F Glutamic decarboxylase ก ก Glutamic acid ˈ GABAก ก Glutamic acid ˈ GABA Glutamic acid((+)N/V) -------------------> GABA ((-)N/V) ADR : F F if ≥2000 mg/day Glutamic decarboxylase/B6
  31. 31. 7)Anti-emetics drugs ;Others;Benzodiazepines e.g. lorazepam (Ativan®) ก ก: ก benzodiazepine GABAA-receptor ionorphoreก benzodiazepine GABAA-receptor ionorphore complex F GABA F GABAA receptor ก F ˂ ก Anticipatory CINV amnestic antianxiety effects Common ADR : F (amnesia)
  32. 32. 8)Anti-emetics drugs;Others;Steroids e.g.Dexamethasone, Methylprednisolone ก ก : ก F 5-HT F กก F 5-HT F ก Common ADR: GI irritate, F , กก
  33. 33. 8)Anti-emetics drugs;Others;Steroids F dexamethasone Acute nausea and vomiting / กF F/ กF F Delayed nausea and vomiting : 2 3-4 ก F ก F 24
  34. 34. ก ก F ก ก F ก ก F 1.Motion sickness ˆ ก HistamineH1 antagonists: e.g.dimenhydrinate,meclizine Effective if take before ½ hr travel ( receptor M1,H1) Effective if take before ½ hr travel MuscarinicM1 antagonists : e.g.scopolamine ( F Effective if take 4 hrs before travel Effective : 3days
  35. 35. ก ก F ก ก F ก ก F 2.Morning sickness N/V in pregnancy Select safety to fetus Vitamin B6 +doxylamine (firstsickness Select safety to fetus B6 +doxylamine (first line) or vit B6 only H1 antagonists e.g.dimenhydrinate D2 antagonist e.g.metoclopramide
  36. 36. ก ก F 3.Postoperative N/V (PONV) N/V after surgery opioid:relief pain opioid:(+)CTZ 5-HT3 antagonists (all.gold standard) D antagonists ก ก F ก ก F opioid:(+)CTZ D2 antagonists e.g.metoclopramide,droperidol M1 antagonists e.g.scopolamine H1 antagonist e.g.promethazine
  37. 37. ก ก F ก ก F ก ก F 4.Radiotherapy- inducedN/V (RINV) Mechanism ~ cytotoxic D2 antagonists e.g.metoclopramide 5-HT antagonists(all.)(RINV) 5-HT3 antagonists(all.)
  38. 38. ก ก F ก ก F ก ก F 5.Chemo therapy- induced cytotoxic 1.CTZ 2. F ก 5-HT3 antagonist(all.acute/delayed) gold standard D antagonists (acute type)induced N/V(CINV) 2. F ก D2 antagonists (acute type) e.g.metoclopramide *Steroids (acute/delayed) e.g.dexamethasone,methylprednisolone *Benzodiazepines (anticipatoryCINV) e.g.lorazepam
  39. 39. ก ก F ก ก F ก ก F 5.Chemo therapy-induced N/V(CINV) *NK1 receptor antagonist(acute /delayed) e.g.Aprepitant N/V(CINV) (*) ก F ˈ F F ก 5-HT3 metoclopramide
  40. 40. ก ก F ก ก F ก ก F 6.Combine tx for Acute CINV - 5-HT3antagonist+steroid(best treatment) effective than single drug and lower S/E than metoclopramide+steroid and others for Acute CINV effective than single drug and lower S/E than metoclopramide+steroid and others
  41. 41. ก ก F ก ก F ก ก F 7.Gastroenteritis ( F ก ) - D2 antagonists e.g. metoclopramide( F ก ) e.g. metoclopramide 8.Gastroparesis (ก F ก F ) - D2 antagonists e.g. metoclopramide ,domperidone
  42. 42. ก Agents for treatment of peptic ulcer Antacid Anti-secretory drug Mucosal resistance(Cytoprotective)Mucosal resistance(Cytoprotective) Misc. -Rebamipide - ก (Eradication) H.pylori NSAIDs-induced peptic ulcer
  43. 43. Parietal cells mucosa ก Receptor ( ) ก F ก ก ก F ก ก F ก ก F ก ก F ก ก F ก ก F receptor Second messenger F H+/K+ ATPase or gastric proton pump
  44. 44. ก F F ก ก ก Receptor ก F ก ก F (Receptor) Histamine-2 receptor HistamineHistamine-2 receptor (H2 receptor) Histamine Muscarinic -3 receptor Acetylcholine CCK2 receptor Gastrin
  45. 45. F ก F 1.Second messenger ก F F กก ก F Second messenger กF F ก กSecond messenger กF F ก ก F Second messenger F ก ก ก กก ก F
  46. 46. F ก F 2.Phosphate Binders F ก phosphate F phosphate form ˈ insolubleF phosphate form ˈ insoluble compound ก ก
  47. 47. ก กก ก 1. receptor 2. F ก secondary messengers Cyclic AMP (cAMP)Cyclic AMP (cAMP) Calcium
  48. 48. ก กก ก Histamine: (+) F adenylate cyclase (ATP cAMP) Gastrin ,acetylcholine: ก calcium ก F cell ↑calcium cell (+) F adenylate cyclase (ATP cAMP) ↑cAMP
  49. 49. ก กก ก 3.cAMP ↑, calcium ↑ (+) H+/K+ ATPase at parietal cell membrane 4. F ก ก ก hydrogen ion4. F ก ก ก hydrogen ion ก ก (H+) ก F parietal cell ก F canaliculi ก ก (K+) F F cell
  50. 50. ก กก ก ก parietal cell : F hydrogen/potassium adenosine triphosphate (H+/K+ ATPase gastric proton pump )
  51. 51. Gastric pH <3 ( ˈ ก ก) ก ก F 1. ก gastrin ก กก ก ก 2.Prostaglandin (PGE2 ) histamine ก ก F adenylate cyclase
  52. 52. (peptic ulcer) Peptic ulcer ก/ ก ก / F ก F F + ก ก กก ก ก ˈ ก aggressive factor -defensive factor imbalance
  53. 53. ˆ F ก ก peptic ulcer Aggressive factor Defensive factor ก parietal cell mass ก ก /bicarbonate mass ก ก F mucosa (mucosa ก ˈ ก F ก )
  54. 54. ˆ F ก ก peptic ulcer Aggressive factor Defensive factor ก F prostaglandin inhibitor ก epithelial cell (cellinhibitor (e.g.NSAIDs protective prostaglandin) epithelial cell (cell ก ) ก ก H.pylori Prostaglandin E2 (PGE2)
  55. 55. ก Peptic ulcer F ʾˉ F ˈ ก Duration : day/wk ก ก ˈ F ก ก ก DU/GU F ก F ก ( F ) ก ก ˈ F ก
  56. 56. ก Peptic ulcer F ก (Duodenal ulcer;DU) ก ก F F F กF กกF ก Relief : / F ก ก (Gastric ulcer;GU) ก ก F F F 1-3
  57. 57. F ก ก ก F ก ก ˈก ก ˈ ก ก F ก ˈ e.g.haemorrhage ,obstruction ( ก scar),perforation
  58. 58. ก Agents for treatment of peptic ulcer Antacid Anti-secretory drug Mucosal resistanceMucosal resistance Misc. -Rebamipide - ก (Eradication) H.pylori (HP) NSAIDs-induced peptic ulcer
  59. 59. 1.Antacids ( ก ) e.g. aluminium salt , magnesium salt, sodium bicarbonate ก ก: 1.ก ก (acid neutralizing effects)1.ก ก (acid neutralizing effects) 2.ก ก F ก ก 2.1 ∆ pepsinogen pepsin 2.2 ก ก H.pylori
  60. 60. 1.Antacids ( ก ) F ก F F F rapid onset : within 5-15 min duration : 15 min-1 hrduration : 15 min-1 hr F ก F F F ก F F ก F ก ก F F
  61. 61. 1.Antacids ( ก ) ADR : Aluminium salt ( F ก), Magnesium salt ( F ) Drug interaction (DI) :Drug interaction (DI) : ↓ absorption F F (absorption & dissolution depend on acid) enteric coated F กF ก
  62. 62. 1.Antacids ( ก ) antacid (aluminium salt) ก phosphate ก phosphate F ˈ phosphate binder F ˁ Drug interaction (DI) : phosphate F ˈ phosphate binder F ˁ ก sucralfate ก gastric mucosa
  63. 63. 2.1 H2 receptor antagonist (H2RA) 2.2 Proton pump inhibitor (PPI) 2.Anti-secretory drugs ; ก ก
  64. 64. 2.1 H2 receptor antagonist (H2RA) e.g.ranitidine, famotidine, nizatidine, cimetidine ก ก F histamine ก ก H receptorF histamine ก ก H2receptor competitive/reversible ก F cyclic AMP
  65. 65. cimetidine ranitidine nizatidine famotidine 1 4-10 4-10 20-50 Dose of treatment 400 bid 800 hs 150 bid 300 hs 150 bid 300 hs 40 hs 2.1 H2 receptor antagonist (H2RA) treatment (mg) 400 bid 800 hs 150 bid 300 hs 150 bid 300 hs 40 hs Dose of recurrent prophylaxis* (at least 1 ʾ) 400 hs 150 hs 150 hs 20 hs
  66. 66. 2.1 H2 receptor antagonist (H2RA) food : not affect to absorption Treatment DU : 6-8 wk if not cure F F ก 2-4 wkDU : 6-8 wk if not cure F F ก 2-4 wk GU : 8 wk if large ulcer F 12 wk * if recurrent > 3 / ʾ
  67. 67. ADR: F F / F ก F F F F 2.1 H2 receptor antagonist (H2RA) F F F cimetidine (antiandrogen effect) in men/high dose /long term ก gynecomastia/impotence
  68. 68. 2.1 H2 receptor antagonist (H2RA) Drug interaction (DI) antacid , sucralfate : ↓ absorption of H2RA F antacid/sucralfate F ก H RA F FF antacid/sucralfate F ก H2RA F F 2 hr
  69. 69. 2.2 Proton pump inhibitor (PPI) e.g.omeprazole(Losec®),lansoprazole(Prevacid®), pantoprazole(Controloc®),rabeprazole(Pariet®), esomeprazole (Nexium®)esomeprazole (Nexium ) ก ก parent compound(not active)-------->active metabolites F ก H+/K+ATPase non-competitive /irriversible ( ; ก F F F) can use once daily before meal ~ 1/2 hr ACID CONDITION
  70. 70. ก / ก F H2RA Food delays absorption ADR : 2.2 Proton pump inhibitor (PPI) ADR : F F F ˁ F F F F F F ก F
  71. 71. 2.2 Proton pump inhibitor (PPI) Drug interaction (DI) PPIs ก metabolize ก Cytochrome P450 enzyme (CYP450) ก ก metabolize F CYP450 P450 enzyme (CYP450) ก ก metabolize F CYP450 F ก F ↑warfarin,phenytoin level - monitor response phenytoin - maybe adjust dose of warfarin/monitor INR,PT
  72. 72. ก F PPI (enteric coated tablet) F ˁ F NG tube NG tube (Nasogastric tube ) ก F F ก F กF ก F F / กF F ˁ F F ก
  73. 73. Enteric coated tablet/granules F ก F ก F ก ก ก (capsule) ก กก ก (capsule) ก ก Enteric coating ก F F F F ก ก granules ก F ก กF ก F ก+ ก
  74. 74. omeprazole (miracid® ) delayed-release capsule/multiple unit granules system enteric-coated granules ก F PPI (enteric coated tablet) F ˁ F NG tube enteric-coated granules Capsule :dissolves in gastric acid Granules :base-labile coating dissolves in small intestine
  75. 75. rabeprazole (pariet®) delayed-release tablet or enteric-coated tablet drug is absorbed in the intestine ก F PPI (enteric coated tablet) F ˁ F NG tube drug is absorbed in the intestine ** F / rabeprazole F NG tube** Coated ; ก ก
  76. 76. Omeprazole 1. ก capsule 2. granules NG F Gastric : ˈ ก ก F PPI (enteric coated tablet) F ˁ F NG tube Gastric : ˈ ก (protect the base-labile granules) e.g. F F flush ก F Small intestine : ˈ F ( F ก ) e.g.8.4%NaHCO3 F flush F ก F
  77. 77. Mucosal resistance ;Cytoprotective ก ก ˂ ก F F ก ก F Cytoprotective agents :Cytoprotective agents : Sucralfate Bismuth preparation Prostaglandin analogues
  78. 78. Sucralfate ก ก: 1.sucralfate กก (viscous substance) ก กก ก ก ˂ ก ก ก
  79. 79. Sucralfate 2.ก F endogenous prostaglandin ก PGE2 F - F ก ˂ ก- F ก ˂ ก - gastric mucus secretion F ก F 3. F F F ก ก
  80. 80. Sucralfate ADR: sucralfate ก ก F F ก ก F systemic F ก F F กF F ก Fsystemic F ก F F กF F ก F F F ก F ˈ ก F F
  81. 81. Sucralfate Drug interaction: ก F sucralfate F F (กFF sucralfate F F (กF 1 )
  82. 82. Bismuth preparation e.g.bismuth subsalicylate (GASTRO-BISMOL®), ranitidine bismuth citrate ก กก ก 1. ก bismuth ก ก ก F F ˈ ก local gastroprotective effect
  83. 83. Bismuth preparation 2.ก F ก F prostaglandin, bicarb, ก 3.ก ก H.pylori 4. F neutralize ก4. F neutralize ก ADR ; - ˆ -bismuth accumulate neurotoxic :not for recurrent prophylaxis;long time
  84. 84. Prostaglandin analogues e.g.Prostaglandin E analogues (misoprostol;cytotec®) ก ก: ก prostaglandin receptor parietal cellก prostaglandin receptor parietal cell - ก ก - (mucosa) -ก F ก bicarb - ก mucosa
  85. 85. Prostaglandin analogues ADR; F F (4-38%) F F N/VF F N/V ก F F F F (FDA pregnancy category X )
  86. 86. Prostaglandin analogues;misoprostol;cytotec® ก F off-label F F F กF ก ก ก (postpartum hemorrhage) F off-label F ก ก ก F F ก
  87. 87. Misc. ;Rebamipide (mucosta®): ก ก ( / ): ↑ PGE2 ก F ก ↑ ก/ ก ก ↑ก ก ก↑ก ก ก F ก F ก F ก F F ก/ F ก ก F interleukin-8 (IL-8) ก ก Helicobacter pylori F (IL-8- inflammation)
  88. 88. Misc.; Rebamipide (mucosta®): ADR; leukopenia ( ก F ก ) , thrombocytopenia ( ก )thrombocytopenia ( ก ) hepatic dysfunction and jaundice (↑AST,ALT) rash constipation, diarrhea , N/V heartburn
  89. 89. Combination treatment Single (2-3 wk)+eradicate risk factors not cure combine
  90. 90. ก (Eradication) H.pylori (HP) Helicobacter pylori : ก ก F F ก ก กF F ก ก ก (urease enz.) F urea ammonia+CO2 ammonia : ก ก , ก acid hypersecretion , F ก gastric atrophy ก ˈ cancer cell F
  91. 91. ก (Eradication) H.pylori (HP) ก H. pylori ( ) PPI-based triple therapy PPI bid + amoxicillin 1 g bid + clarithromycin 500 7-14PPI-based triple therapy PPI bid + amoxicillin 1 g bid + clarithromycin 500 mg bid PPI bid + metronidazole400 mg bid + clarithromycin500 mg bid PPI bid + amoxicillin1 g bid + metronidazole400 mg bid 7-14
  92. 92. ก (Eradication) H.pylori (HP) ก H. pylori ( ) Bismuth-basedquadruple therapy PPI bid + bismuth 240-525 mg bid + 14 PPI bid + bismuth 240-525 mg bid + metronidazole400 mg bid or tid + tetracycline500 mg qid PPI bid + bismuth 240-525 mg bid +metronidazole 400 mg bid or tid + clarithromycin500 mg bid
  93. 93. ก (Eradication) H.pylori (HP) ก H. pylori ( ) Sequentialtherapy PPI bid + amoxicillin 1 g bid ˈ 5 F F 10 PPI bid + amoxicillin 1 g bid ˈ 5 F F PPI bid + metronidazole400-500 mg bid + clarithromycin 1000 mg od 500 mg bid ˈ 5
  94. 94. ก (Eradication) H.pylori (HP) ก H. pylori ( ) Levofloxacin-basedtriple therapy 10Levofloxacin-basedtriple therapy PPI bid + levofloxacin250 mg (or 500 mg) bid + amoxicillin1 g bid 10 Rifabutin-basedtriple therapy: 7-10 days PPI bid + rifabutin 150 mg bid + amoxicillin1 g bid 10
  95. 95. ก (Eradication) H.pylori (HP) ก H. pylori ( ) Concomitanttherapy 10Concomitanttherapy PPI bid + amoxicillin1 g bid + clarithromycin500 mg bid + metronidazole 400 mg tid 10 * ก ก ก ก * * ก F ˁ ก ก ก ก ˈ ก*
  96. 96. ก (Eradication) H.pylori (HP) PPI-based triple therapy sequential therapy Bismuth-based quadruple therapy Levofloxacin-based triple therapy ก F F or Levofloxacin-based triple therapy Rifabutin-based triple therapy Concomitant therapy or or or
  97. 97. NSAIDs-induced peptic ulcer
  98. 98. ก กก ก NSAIDs-induced peptic ulcer ก F prostaglandin - F mucosal blood flow- F mucosal blood flow -mucus secretion , HCO3 secretion ก /pepsin/NSAIDs : ก ก
  99. 99. NSAIDs-induced peptic ulcer ก ˂ ก (prophylaxis) F ˈ F Fก ˂ ก F ˁ F NSAIDs กF NSAIDs ก
  100. 100. NSAIDs-induced peptic ulcer
  101. 101. ˆ (High risk) > 60 ʾ ก F ก/ ก ก /ก/ ก ก / F NSAIDs F ก corticosteroids F NSAIDs ก F ก F NSAIDs กก F 1 F ก F F ก anticoagulants eg. warfarin
  102. 102. NSAIDs induced peptic ulcer ก ก (Treatment) 1. NSAIDs : H2RA ∼ PPIs 2. F NSAIDs F : Drugs of choice :PPIs2. F NSAIDs F : Drugs of choice :PPIs Drugs of choice ; ก F ˈ ก ก ก ก F F F F
  103. 103. ก ก F F (antidiarrheal drugs)
  104. 104. ก F F (diarrhea) F F ˈ กก F 3 / F ก F F 1 24
  105. 105. F F (diarrhea) 1. F 2. F F ก กก F antibiotic (eg.clindamycin,tetracycline),antibiotic (eg.clindamycin,tetracycline), ก ก F ก F กก F F colon cancer, hyperthyroidism
  106. 106. ก ก ก F F 1. ก F กF ก F ( ˁ / ) F IV :F IV : ORS (oral rehydration salt) : (Electrolyte=Na,K,Cl,HCO3) + ก
  107. 107. ก ก ก F F F F F F F FF F ก F F
  108. 108. ก ก ก F F 2.ก ก ก F F กก 2.1 F F ก (toxigenic diarrhea) ก epithelial cell F F ก Fก epithelial cell F F ก F enterotoxin ก ก e.g.Vibrio cholerae ,E.Coli F F ˁ F ˈ ก *Enterotoxin :toxin ก F F F ก ก F *
  109. 109. ก ก ก F F 2.2 F F กก ก F F (invasive diarrhea) ก ก ก Fก ก ก F ก e.g.shigella, salmonella, E.coli
  110. 110. ก ก ก F F F ก ˈ Shigella ( F ) e.g.TMP/SMX (bactrim®),norfloxacin,ciprofloxacine.g.TMP/SMX (bactrim®),norfloxacin,ciprofloxacin Salmonella typhi ( F ก F F F ) e.g.TMP/SMX (bactrim®),ceftriaxone,ciprofloxacin Vibrio cholerae( ก ) e.g.TMP/SMX(bactrim®),doxycycline,norfloxacin
  111. 111. ก ก ก F F 3. ก ก ก F F ก F / ก F F F 3.1 ก F3.1 ก F 3.2 F ก ก 3.3 Intraluminal agents 3.4 Bulk forming agents 3.5 Bile acid binder
  112. 112. 3.1 ก F Opioid derivatives -Loperamide; Imodium® -Diphenoxylate+atropine;Lomotil® ก ก :ก F opioid receptors Fก ก :ก F opioid receptors F ก ก F ก F ก ก F F /
  113. 113. 3.1 ก F Diphenoxylate ก atropine ˂ ก ก F Atropine : ก atropinism e.g. F F F F
  114. 114. 3.1 ก F ADR: opioid F / F F FF F loperamide ก F ก F ก F Diphenoxylate
  115. 115. 3.1 ก F ก F F F ก F F 2 F ก F2 F ก F F ˁ ก F กก invasive diarrhea F F F F ก ก F F F ก F Fก F
  116. 116. 3.2 F ก ก Activated charcoal Kaolin-pectin (Kaolin and pectin®) Diosmectite (Smecta®)
  117. 117. 3.2 F ก ก ก ก : F ก F F ก F F F ˈ ก F F Fˈ ก F F F ก F ADR : F ก F F F ก ˈ F F ก F
  118. 118. 3.3 Intraluminal agents e.g.Bismuth subsalicylates (GASTRO-BISMOL®) ก ก : ก ก F ADRADR salicylism ( ) N/V /
  119. 119. 3.4 Bulk forming agents e.g.Psylium(AGIOLAX®,METAMUCIL®,FYBOGEL®) F F/ ก ก ก F F กF ก ก ก : F ˈ กF F ADR F F F ก F
  120. 120. 3.5 Bile acid binder e.g.Cholestyramine (Questran®) ก ก : ก ก toxin (clostridium difficile toxin)difficile toxin) F ก antibiotic associated diarrhea F F ก ก F ADR: F ก F ก
  121. 121. Cholestyramine ก bile acid ก F F ก F F ก ก bile acid ก ก ก ก F ก F bile acid 3.5 Bile acid binder ก ก ก F ก F bile acid (cholesterol ˈ ) ↓cholesterol ก ↑LDL receptor ↑ ก catabolism LDL ↓ LDL ก
  122. 122. F ก F Catabolism : ก ก F ก ก ˈ ก กก ก ˈ ก ก ˈ F ก F / F F F F
  123. 123. Antibiotic associated diarrhea ก ก ก F F F ก ก F F ก F F ก F
  124. 124. Antibiotic associated diarrhea F ก diarrhea F ก ก e.g. 1. Osmotic diarrhea 2. Bile salt diarrhea2. Bile salt diarrhea 3. ↑Small intestine motility 4. Microorganism infection
  125. 125. 1.Osmotic diarrhea ↓ (non absorbable carbohydrate) F F F F non absorbable carbohydrate FF F non absorbable carbohydrate F osmotic diarrhea
  126. 126. 2. Bile salt diarrhea ↓ F F( ) F bile salt F F ↑ bile salt↑ bile salt ก F ก colonic fluid ก F
  127. 127. 3. ↑↑↑↑Small intestine motility F e.g. erythromycin ก F motilin receptor F กก F motilin receptor F ก F ก F
  128. 128. 4. Microorganism infection e.g. Clostridium perfrigen type A Clostridium difficile
  129. 129. Antibiotic associated diarrhea Cause Drug : ampicilln,amoxycilln,cefixime, fluoroquinolone(1-2%) bactrim (<1%)fluoroquinolone(1-2%) bactrim (<1%) Organism : Clostridium difficle infection *10% of total.cause but serious complication then Death ก F Clostridium difficile diarrhea*
  130. 130. ก ก Clostridium difficile diarrhea ก F : +supportive tx ก :metronidazole (oral) 10-14 *If not relieve ,no tolerance to drug ,pregnancy,*If not relieve ,no tolerance to drug ,pregnancy, <10 years old , severe colitis* vancomycin (oral) 10-14
  131. 131. ก ก F ก ก F F ก F opioid derivative (eg.+atropine) :serious S/E F F ก / กF F ก / ก : F ก ก + ก / / ก F e.g. ORS
  132. 132. ก ก F ก ก F F F : FF loperamide (limited safety information) diphenoxylate ( ก )
  133. 133. Anticonstipation ; กF ก F ก->laxatives/cathartics
  134. 134. ก F ก (constipation) ก F ˁ F F F ( F ก F 3 F F) ˈ F Fˈ F F F ก F F F F ก F ก
  135. 135. ก ก 1. ก / F ก ก ก F ก กก กก กก ก F ก (aluminium hydroxide) ก F ʽˉ (tramadol,morphine,codeine, fentanyl), bismuth , trihexyphenidyl Pregnancy, Hypothyroidism, DM
  136. 136. ก ก 2. ก ก ก : F ก กก ก กก ก F
  137. 137. ก ก 3.ก F Bulk forming laxatives LubricantLubricant Stool softeners /emollient laxatives Stimulant laxatives Osmotic laxatives Others ; ก (enemas)
  138. 138. Bulk -forming laxatives F ˈ กF ก ก e.g. ก ก ก FF ก ก (Ispaghula seed ,Plantago, Psyllium) ;AGIOLAX®,METAMUCIL®,FYBOGEL® F ก F F methylcellulose
  139. 139. ก ก F ก F / F ก GI ก F F ˈ ก Bulk -forming laxatives ก F F ˈ ก F ˈ กF F F ก F ก F F F F F F
  140. 140. F F 1 wk Fก ก F ก F F F Bulk -forming laxatives
  141. 141. ADR; fiber F ( F) gas F F F Bulk -forming laxatives F F F fiber + F F Drug interaction ; ก ก F ก 2 hr ** ก ก ก F ก F/ **
  142. 142. Lubricant laxatives F ˈ ก e.g. Mineral oil (synonym) F (synonym)F (synonym) liquid paraffin (synonym) ELP(Emulsion of liquid paraffin) (synonym)
  143. 143. ก ก ; F F F ก F F Lubricant laxatives F F ก ก F F F ก ˈ ก ก ˈ ก F F
  144. 144. ADR; lipoid pneumonia ( ก ) ก ก F Lubricant laxatives F - F F กF - F F กF F ˁ F F - ก F : ก ก/ F ˁ / F ˁ
  145. 145. ก ก F ˀˊ F F F F F ( ;drug interaction) Lubricant laxatives F F F ( ;drug interaction) Drug interaction; ก F (vit D def. F ก ) F F
  146. 146. Stool softeners /emollient laxatives e.g. Docusate ก ก F F F FF F F F กF F F F ก ก F ** F F F F ก ; F/ **
  147. 147. ADR ; F ก F F F F Stool softeners /emollient laxatives Drug interaction; ก F mineral,phenolpthalein Toxic of mineral oil, phenolpthalein
  148. 148. e.g. ก(senna) , bisacodyl (dulcolax®),phenolpthalein, F (castor oil), dehydrocholic acid(Decholin® ) ก ก; Stimulant laxatives ก ก; ก F ก F F ก ก ก F ก / F ก ก / ก F F ก ก
  149. 149. ADR; Bisacodyl e.g. F F Phenolpthalein e.g. ˆ ˈ Stimulant laxatives Phenolpthalein e.g. ˆ ˈ Castor oil ( F ) e.g. ก ** F F F F F F** ก dehydrocholic acid e.g. F
  150. 150. Drug interaction; e.g. bisacodyl (enteric coated tablet F ก F F) F ก Stimulant laxatives F ก ก / F F ก F ก ก / ก F ก F F 1
  151. 151. F F F F ก > 1 wk ก F ˈ ʾ F ก F Stimulant laxatives ก F ˈ ʾ F ก F / ก cathartic colon (ก F ) F F F ก F F
  152. 152. F enteric coated tablet F / ˂ ก ก ก ก ( ก F F) Stimulant laxatives ก ( ก F F) F ก F
  153. 153. Osmotic laxatives ˈ ก e.g. ก F ก -Magnesium sulfate, citrate, hydroxide-Magnesium sulfate, citrate, hydroxide (M.O.M/milk of magnesia) -Sodium phosphate (xubil®;Monobasic Na phosphate, dibasic Na phosphate)
  154. 154. Osmotic laxatives Glycerine Sorbitol LactuloseLactulose Lactitol
  155. 155. Osmotic laxatives ก ก; ( ก F F F ก GI) F F F F ก (osmotic action) F ก ก ก(osmotic action) F ก ก ก F ADR; e.g. N/V, F ˂ F F F
  156. 156. Osmotic laxatives Drug interation ; ก F ก F F ก ˆ F ก FF
  157. 157. Osmotic laxatives F ก F ก : F ˁ ก ก - F ˁ- F ˁ - - - ก F
  158. 158. Osmotic laxatives F ก F ก F F ก ก F ก electrolyte imbalance ก F M.O.M F Fimbalance ก F M.O.M F F ก F lactulose F ˁ ˈ galactose F
  159. 159. Hepatic encephalopathy ก ก ↓ ↓ ก F F ↓ ก ก ˆ F ก metabolize ˈ
  160. 160. Hepatic encephalopathy eg. cirrhosis ↓ ก metabolize ˈ ↓ ↓ ↓ Hepatic encephalopathy
  161. 161. ก hepatic encephalopathy ก ก F F F FF ก F ก ก
  162. 162. ก F lactulose ก hepatic encephalopathy
  163. 163. Others ; ก (enemas) e.g. (tap water) ก =NaCl = eg.unison enemaก =NaCl = eg.unison enema sorbitol F (soap solution) ก ก; ก ก F ก F ก F ก 15-30
  164. 164. ก ก F : bulk forming agents + life modification (ก ก กก ก ʿกก F ˈ ) F F ∆ laxatives(ก ก กก ก ʿกก F ˈ ) F F ∆ laxatives F ก : / ก F F bisacodyl /senna /M.O.M >1 wk F F ก F
  165. 165. ก ก F F ˁ ก ก ก F bulk forming agents ก ก F ก ก Fก ก F ก ก F lubricant/stool softener F ก F bulk forming agents F ก ก e.g. F F saline laxatives (high dose)
  166. 166. ก ก F F ˁ / F bulk forming agents F F bisacodyl /senna/M.O.M/(lactulose;low dose) F F F F F/senna/M.O.M/(lactulose;low dose) F F F F F F ( F F F F ก ) docusate/bulk forming agent **stimulant laxatives use if necessary but not use Castor oil**
  167. 167. ก ก F ก ก ก ก : ก ก e.g.glycerin suppo/ กsuppo/ ก F F F F F F ; M.O.M./senna F ˁ F ก : saline laxatives e.g.magnesium sulfate,osmotic laxatives
  168. 168. ก F ˂ (antiflatulants)
  169. 169. ก F ˂ (flatulence) ก F ก F F F กF e.g.e.g. F ก F / F ก F e.g. peptic ulcer
  170. 170. ก F ˂ (antiflatulants) ก F (volatile oils) ก F F ก ก (defoaming agent)
  171. 171. ก F (volatile oils) e.g. pepermint oil , fennel oil ,cinnamon oil, Cardamom, (stomachica mixture), ก F ˂ (antiflatulants) Cardamom, (stomachica mixture), F F (carminative mixture)
  172. 172. ก F (volatile oils) ก ก F F ก F ก F ˂ (antiflatulants) F กF F ก F F ก กF ก :ก F F ก
  173. 173. ก F ˂ (antiflatulants) F F Mixture Carminative Fก ก F ก Alcohol ก F F 8.8 F กF F 8.8 F ก ก F F F ก F กF ก
  174. 174. ก F F ก ก (defoaming agent) e.g.Simeticone tab,susp. Trade name :AIR-X , Belcid compound ก F ˂ (antiflatulants) Trade name :AIR-X , Belcid compound ก ก : กF F ก กF : F กF ก
  175. 175. F ˂ ก ก F ˂ ก ก F ก กF e.g. F F FF F F

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