Farmakoloji Flashcards
Prokinetic agents function
Agents that
• increase lower esophageal sphincter pressures may be useful for GERD
• improve gastric emptying may be helpful for gastroparesis and postsurgical gastric emptying delay.
• stimulate the intestine function may be beneficial for postoperative ileus or chronic intestinal pseudoobstruction.
• enhance colonic transit may be useful in the treatment of constipation.
Cholinomimetic agents
Betanecol
Neotigmin
• Muscarinic M3 receptor agonist on muscle cells and at myenteric plexus synapses
• Used in treatment of GERD and gastroparesis - seldomly used now
Betanecol
– (The acetylcholinesterase inhibitor) • Enhance gastric, small intestine, and colonic emptying
• Used for the treatment of hospitalized patients with acute large bowel distention (known as acute colonic pseudo-obstruction or Ogilvie’s syndrome).
• Adverse cholinergic effects include excessive salivation, nausea, vomiting, diarrhea, and bradycardia.
Neostigmin
Metoclopramide
Domperidone
Dopamine D2- Receptor antagonists
• Normally activation of dopamine receptors inhibits cholinergic smooth muscle stimulation- blockage of this affect- Potentiate prokinetic effect
• Increase esophageal peristaltic amplitude, increase lower esophageal sphincter pressure, and enhance gastric emptying - no effect on intestine
• Used in therapy of Gastroesophageal reflux disease, impaired gastric emptying due to postsurgical disorders (vagotomy, antrectomy) and diabetic gastroparesis
• Effective in dyspepsia via acceleration of gastric emptying
• Prevention of vomiting
Adverse effect
• neuropsychiatric side effects, restlessness, drowsiness, insomnia, anxiety, and agitation , extrapyramidal disorders (dystonias, akathisia, parkinsonian features), increased prolactin related side effects; galactorrhea, gynecomastia, impotence, and menstrual disorders.
Metoclopramide
Domperidone
• Directly stimulate motilin receptors on gastrointestinal smooth muscle. • Motillin increase gastric emptying and gastric motor activity
• Intravenous erythromycin
• used in gastroparesis and
• acute upper gastrointestinal hemorrhage to promote gastric emptying of blood before endoscopy.
Macrolides
Eritromycin etc
1-Stimulation of 5-HT receptors on the presynaptic terminal of submucosal intrinsic primary afferent nerves
2- enhances the release of their neurotransmitters, including calcitonin gene-related peptide, Ach
3- stimulates second-order enteric neurons 4- promote the peristaltic reflex
Serotonin 5-HT4- receptor agonists
Seratonin agonists
Cisapride
Tegaserod
Prucalopride- Velusetrag
DRUGS that are used in intestinal motility dysfunction
Regularly colonic movements are important properly evacuation of bowel . If this movements are slown down, patient can get a constipation, at the opposite condition cause a diarrhea
Laxatives promotes empty the bowel, make defecation easier
Laxatives
Laxatives types
- Bulk- forming laxatives
- Stool surfactant agents (softener)
- Osmotic laxatives
- Magnesium citrate, magnesium hydroxide, sodium phosphate
• indigestible, hydrophilic colloids that absorb water, forming a bulky, emollient gel that distends the colon and promotes peristalsis.
• Treatment of constipation
• natural plant products (psyllium, methylcellulose)
• synthetic fibers (polycarbophil)
• Adverse effect: Bloating and flatulence
Bulk formin laxatives
• These agents soften stool material, permitting water and lipids to penetrate • Docusate (oral or enema) and glycerin suppository.
• Considered safed in pregnacy after the childbirth and surgery
Stool surfactant agents (softener)
• High doses of osmotically active agents produce prompt bowel evacuation within 1–3 hours.
• Used to cleanse the bowel prior to colonoscopy.
• Sodium phosphate –orally, rectally
• Require adequate hydration for effect
• Electrolyteabnormalities-shouldnotbeusedinpatientswhoarefrailorelderly,haverenal insufficiency, have significant cardiac disease
Magnesium citrate
Magnesium hydroxide
Sodium phosphate
• Used for complete colonic cleansing before gastrointestinal colonoscopic procedures.
• As a perioperative colon periparation- For optimal bowel cleansing, 4 L of solution should be ingested rapidly (over 2-4 hours) on the evening before the procedure
Lactulose
Balanced polyethylene (PEG) solutions