14 - GI Pharmacology II Flashcards
What are the common neurotransmitters that affect gastric motility?
- Serotonin (inc.)
- Dopamine (dec.)
- Acetylcholine (inc.)
- Motilin (inc.)
How does serotonin induce gastric motility?
By inducing the
release of acetylcholine by neurons onto gastrointestinal smooth muscle (contraction of gastric smooth muscle)
How does dopamine affect gastric motility?
By activating presynaptic receptors to decrease the firing of ENS neurons, therefore decreasing gastric motility
How does acetylcholine affect gastric motility?
By activating muscarinic receptors to induce contraction of gastrointestinal smooth muscle
How does motilin affect gastric motility?
Promotes gastric motility through activation of motilin receptors located on gastrointestinal smooth muscle
What are the four prokinetic agents used to increase gastric motility?
1 - Metoclopramide
2 - Bethanechol
3 - Neostigmine
4 - Erythromycin
What is the mechanism of action and use of metoclopramide?
- D2 antagonist (blocks the dopamine receptor - remember dopamine slows down gastric motility)
- Used to treat GERD, impaired gastric emptying, dyspepsia and is used as an antiemetic
What are the adverse effects of metoclopramide?
- CNS (restlessness, drowsiness, insomnia, anxiety)
- Altered motor function (Parkinsonian symptoms - because it can cross the BBB)
What is the mechanism of action and use of bethanechol?
- M3 anonist (stimulates ACh receptor
- Used to treat GERD and gastroparesis
What are the adverse effects of bethanechol?
- Cholinergic side effects
What is the mechinism of action and use of neostigmine?
- AChE inhibitor
- Used to treat non-obstructive urinary retention and abdominal distention
What are the adverse effects of neostigmine?
- Cholinergic side effects
What is the mechanism of action and use of erythromycin?
- Motilin receptor agonist (increases the effects of motilin)
- Used to treat gastroparesis
What are the adverse effects of erythromycin?
- Erythromycin mediated side effects
- Antibiotic use can cause diarrhea
What are laxatives commonly used to treat?
- Constipation (infrequent evacuation of the feces)
- Minimizing strain during defecation following cardiothoracic surgery
- Clear GI tract before endoscopy
What are the main causes of constipation?
- Hormone secreting tumors that decrease motility
- Presence of toxins
- Various disease states
- Diet, stress, exercise, etc.
There are 8 laxatives you need to know about, which can be grouped into either physical-induced laxatives (4) and receptor-induced laxatives (4)
Physical-induced laxatives
- Methylcellulose (bulk-forming)
- Glycerin (surfactant)
- Lactulose (osmotic)
- Senna (stimulant)
Receptor-induced laxatives
- Tegaserod (serotonin agonist)
- Lubiprostone (chloride channel activator)
- Methylnaltrexone (mu-opioid receptor antagonist)
- Alvimopan (mu-opioid receptor antagonist)
For the physical-induced laxatives, how good is the absorption?
Poor
For the physical-induced laxatives, what is the use?
- Constipation
- Minimize straining
- Prior to surgical or endoscopic procedure