Pharmacology Flashcards
Pirenzipine is obsolete for PUD but is a ___
M1+3 muscarinic receptor antagonist
PPIs block ___ on ___ NOT in ____
eg.s =
H+K+ATPase on apical membrane NOT in tuberovesicles
omeprazole
PGE1 analogue co-admined with NSAIDS to prevent PUD
Its effects =
misoprostol
decreases basal and stimulated secretion of acid
maintains/increases mucus and HCO3- secretion
Effect of COX-1 inhibitors on stomach
decrease PGE2 which increases acid secretion and causes PUD
eg. of H2 receptor antagonist
ranitidine
Drugs that inhibit gastric acid secretion are used to treat __(3)
GORD/dyspepsia
PUD
acid hypersecretion - by Zollinger-Ellison(gastrinoma)/Cushings (causes increased vagal tone)
mucosal strengtheners eg.s
Mechanism:
sucralfate
bismuth chealate
= bind to ulcer base and form gel with mucus, increase mucosal blood flow (^H+ removal), mucus, HCO3- and PG production
5-HT3 receptor antagonist eg.s
ondansetron, palonosetron
5-HT3 receptor antagonists are for ___
not ___
side effects:
For: chemo and radio acutely (long term add corticosteroid and (neurokinin) NK receptor ant.), Post op N+V
NOT motion sickness/dopaminergic v
constipation + headaches
5-HT3 receptor antagonists block receptors in __+_
peripheral (gut) and central (AP) receptors
muscarinic ACh receptor antagonist anti emetic eg.s
hyoscine, scopolamine
hyoscine and scopolamine (M antagonists) are used for
prophlaxis/treatment of motion sickness
can be given as a trans-dermal patch
side effects of M antagonist anti-emetics
para ANS = blurred vision, urinary retention, xerostomia
sedation
H1 receptor antagonist anti-emetic egs
cyclizine, cinnarizine
H1 rec. ant. antiemetics are used for ___
prophylaxis/treatment of motion sickness
acute labyrinthitis
stomach irritants
H1 rec ant.s block receptors in + and so may cause sedation. Not for emesis causes that directly affect ___
vestibular nuclei and NTS
not CTZ
anti-emetics: dopamine receptor antagonist eg.s
domperidone
metoclopramide
dopamine rec ant anti-emetics are for __
and not ___
drug induced and GI disorder causes of N+V
NOT motion sickness
mechanism of action of dopamine rec ant anti-emetics
block D2+3 in CTZ and have prokinetic effects on oeso, stomach and intestines
dopamine rec. ant.s are restricted in ___
metoclopramide/domperidone crosses the BBB and causes ___ side effects
children
metoclopramide
extra-pyramidal effects - eg. disorders of movement
Anti emetic used for severe vomiting with partial D2 blockade
Phenothiazines
NK1 receptor antagonist anti emetic eg. =
assumed to antagonise ____
aprepitant
substance P
aprepitant (NK1 r. ant) is used in combination with + in acute phase of chemo for anti-emesis
and with ___ in delayed phase
dexamethasone and 5-HT3 r. ant - eg. ondansetron
dexamethasone
CB1 (cannabinoid) r. ant anti-emetic eg.
nabilone
nabilone(CB1 r. ant) is used for ____ emesis
decreases emesis that is due to ___ stimulation
side effects =
cytotoxic chemo when others dont work
CTZ
drowsy, dizzy, xerostomia, mood changes
Anti-emetics used for motion sickness
Muscarinic r. ant.s - hyoscine/scopolamine
H1 r. ant.s - cyclizine/cinnarizine
Anti-emetics for chemo. emesis
5-HT3 r. ant (ondansetron) with NK1 r. ant (aprepitant) and dexamethasone
nabilone (CB1 r. ant.) if others don’t work
Slow acting laxatives =
bulk laxatives
methylcellulose, Ispaghula husk = indigestible polysaccharides
Fast acting laxatives =
osmotic laxatives
Mg sulfate/hydroxide, lactulose PO
Na citrate PR