GIT Flashcards
meclizine
1st gen antihistamine (H1)
minimal anticholinergic an sedating
Vomiting centre
in lateral medullary reticular formation
receptors: H1, M1, NK1, 5HT3
5HT3 antagonists
ondansetron, dolasetron (long QT), palonesetron (long half life)
post op nausea and post chemo (no effect on delayed nausea)
Aprepitant
NK1 antagonist, central blockade CRTZ
chemo related vmiting in combo 5HT and steroid
Steroids in post chemo
with 5HT3 antag to help with delayed nausea
CRTZ
outside BBB 4th vent
blood and CSF
D2 receptors and opioid receptors
Domperidone
D2 antagonist
Doesn’t cross BBB so EPSEs rare
Contraindications D2 antagnists
e.g. metoclopromide, domperidone
phaeochromocytoma, previous EPSE, parkinsons, porphyria
Loratadine
2nd gen antihistamine H1
high vD, does not cross BBB
inc QTc
1st gen antihistamines
all sedating and anticholinergic ecept meclizine
diphenhydramine, promethazine
Loperamide
opioid agonist doesn’t cross BBB
Diphenoxylate
opioid agonist for diarrhoea
analgesic at high dose, contains atropine to stop OD
Bulk forming laxative
psyllium, methylcellulose
SE bloating and flatus
Softener laxative
docusate, glycerin suppository, mineral oil
mineral oil - aspiration pneumonitis and de absorption ADEK
Stimulant laxatives
aloe, senna, cascara, bisacodyl
SE colonic dilation and atony
except bisacodyl cause brown pigmentation colon (melanosis coli)
Osmotic laxatives
lactulos, magnesim hydroxicol,
high volume liquid stool
polyethylene glycol - pre endoscopy, isotonic and balanced with electrolytes
Methylnaltrexone
opioid induced constipation
Antacids
sodium bicarb - belching and metabolic alkalosis
calcium carbonate - less belching, milk alkali syndrome
Mg - osmotic diarrhoea
Aluminium - constipation
Mg +Al renally filtered - not for CRF
H2 antagonist PK
A: F0.5 significent 1st pass
D: T1/2 1-4h, VD1L/KG, 70%PB
M: hepatic
E: glomerular filtration, tubular secretion
Most and least potent H2 antagonists
cimetidine least 400mg BD
Famotidine most 20mg BD
Effect of H2 antagonists
block 60-70% total acid
more effective inhibiting nocturnal acid secretion
SE cimetidine
diarrhoea, headache fatigue
mental state change
gynecomastia and galactorrhoea
brady with rapid IV
PPI drug type
prodrugs, irreversible H/K atpase inhibitors
pka 4-5 weak bases
lipophilic
inhibit 90-98% daily acid
PPI bioavailability
bioavailability decreased by food
omeprazole 0.4-0.65
lansoprazole >0.8
PK PPIs
A: PO/IV
D: Onset 05-2h, duration 1d, highly protein bound, small vD
M: p450 liver
E: renal
SE PPIs
diarrhoea
interstitial nephritis
malabsorption B12, mg and Ca
hip #
risk C diff and other GI bugs + resp
Sulfacrate
paste that binds GI ulcers 6h
SE constipation (contains aluminium)
Bismuth compounds
coast GI ulcers
dark stool and tongue
prostaglandin analogue GI
misoprostyl (PGE1)
dec H2 stimulated cAMP and therefore acid
inc mucous and bicarb
Electrolyte abnormalities sodium phosphate enema
Hypicalcaemia and kalaemia
Hypernatraemia
Metabolic acidosis