Block 3 Drugs Flashcards
Atropine
Classification: muscarinic antagonist
Main clinical applications: preanesthetic to prevent respiratory secretions; sinus bradycardia, blockade of excessive muscarinic receptor activation
- *Pharmacodynamics:** Mechanisms/Sites of Action
- heart: high doses can result in tachycardia
- lungs: bronchodilation; decreased secretion
- GI tract: decreased motility
- glands: decreased salivation and sweating
Adverse Effects: dry mouth, urinary retention, tachycardia. Contraindicated in glaucoma, prostatic hypertrophy, heart disease.
Buspirone
Classification: 5-HT1A partial agonist
Main clinical applications: used for treatment of functional dyspepsia with impaired accommodation; CNS application - used as an anxiolytic for the treatment of anxiety disorders
- *Pharmacodynamics: Mechanisms/Sites of action**
- induces relaxation of the proximal stomach; alleviates dyspeptic symptoms, and is associated with and enhancement of accommodation to a meal
Adverse Effects: dizziness, headache, nausea (infrequent)
Cimetidine
Classification: histamine H2 receptor antagonist
Main clinical applications: used for duodenal/gastric ulcer, hypersecretion of acid, GERD
- *Pharmacodynamics: Mechanisms/Sites of Action**
- histamine H2 receptor antagonist that inhibits acid secretion into stomach
Adverse Effects: diarrhea, dizziness, rash, headache, confusion
Relevant Pharmacokinetics: it is a known inhibitor of many isozymes of the cytochrome P450 enzyme system (eg CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4)
Erythromycin
Classification: macrolide antibiotic
motilin agonist
Main clinical aplications: treat respiratory tract and soft tissue infections; used for treatment of gastroparesis due to its pro-motility effects
- *Pharmacodynamics: Mechanism/Sites of action**
- binds to the 50 s ribosomal subunit, inhibiting bacterial protein synthesis
- useful in treating gastroparesis
- considered a motilin receptor agonist able to stimulate gastrointestinal motility by a combination of direct muscular and indirect neurotransmitter effects
Adverse Effects: GI upset
Fluoxetine
Classification: SSRI antidepressent
Main clinical applications: used for treatment of depression, obsessive compuslive disorder, bulimia nervosa
- *Pharmacodynamics: Mechanism/Sites of action**
- selective serotonin reuptake inhibitor that blocks the uptake of serotonin at all SERT sites, both in the CNS and PNS
Adverse Effects: GI discomfort, nausea, headache, nervousness, insomnia, anxiety or diarrhea
Metoclopramide
Classification: prokinetic drug
Main clinical applications: used for treatment of reflux esophagitis, pre-op gastric emptying, reduces chemotherapy - induced nausea; used for its antiemetic and prokinetic properties
- *Pharmacodynamics: Mechanism/Sites of action**
- acts as a 5-HT3 antagonist and a 5-HT4 agonist. Indirectly effects increases in ACh release in gut. Dopamine D2 receptor antagonist in CNS and PNS.
Adverse Effects: diarrhea, drowsiness, depression
Misoprostol
Classification: a synthetic, oral prostaglandin E1 analog
Main clinical applications: used for and is commonly believed to be effective for prevention of gastric and duodenal ulcers secondary to use of nonsteroidal antiinflammatory drugs (NSAIDs) although currently it is indicated only for the prevention of gastric ulcers
- *Pharmacodynamics: Mechanism/Sites of action**
- exerts a mucosal protectant effect that may contribute to its effectiveness in treating ulcers. It has been suggested that the cytoprotective effect is secondary to mucus and bicarbonate secretion, prevention of mucus bilayer disruption, reduction of backflow of hydrogen ions and regulation of mucosal blood flow
Adverse Effects: diarrhea, abdominal pain, dyspepsia
Neostigmine
Classification: carbamate-type peripheral cholinesterase inhibitor
Main clinical applications: myasthenia gravis diagnosis and treatment, paralytic ileus (increases gastric motility), lack of bladder tone, reversal of neuromuscular blockade following anesthesia
- *Pharmacodynamics: Mechanism/Sites of action**
- carbamate type acetylcholinesterase inhibitor in the periphery
Adverse Effects: bowel craps, diarrhea
Octreotide
Classification: synthetic analog of somatostatin
Main clinical applications: used for treatment of diarrhea and other symptoms of abdominal illness; also for other medical conditions such as intestinal tumors vasoactive intestinal peptide tumors, metastatic carcinoid tumors, acromegaly, variceal bleeding, orthostatic hypotension
- *Pharmacodynamics: Mechanism/Sites of action**
- antidiarrheal
- mimics somatostatin pharmacologically; inhibits gastric acid and pepsin secretion; reduces gastrointestinal motility and inhibits contraction of the gallbladder and bile flow; reduces liver blood flow
Adverse Effects: abdominal cramps and nausea common
Omeprazole
Classification: proton pump inhibitor (PPI)
other PPIs: lansoprazole, rabeprazole, pantoprazole, esomeprazole
Main clinical applications: used for gastroesophageal reflux disease, duodenal ulcer, hypersecretory states (Zollinger-Ellison syndrome)
- *Pharmacodynamic: Mechanism/Site of action**
- blocks secretion of acid by irreversibly inhibiting the H+/K+ ATPase in the parietal cell
Adverse effects: few side effects, constipation
Ondansetron
Classification: 5-HT3 antagonist (same as granisetron)
Main clinical applications: prophylactic administration used for treatment of vomiting and nausea following chemotherapy; also for vomiting postoperatively
- *Pharmacodynamics: Mechanism/Sites of action**
- 5-HT3 receptor antagonist; its effect both in periphery and chemotrigger zone (CTZ) - an area of the brain which receives inputs from blood-borne drugs or hormones
Adverse Effects: headache, constipation
Ranitidine
Classification: histamine H2 receptor antagonist
Main clinical applications: used for treatment of duodenal/gastric ulcer, hypersecretion of acid, GERD
- *Pharmacodynamics: Mechanism/Sites of action:**
- histamine H2 receptor antagonist that inhibits secretion of acid in the stomach; more potent that cimetidine
Adverse Effects: diarrhea, dizziness, rash, headache, confusion; fewer side effects than cimetidine
Sumatriptan
Classification: 5-HT1B/1D agonist and an agonist at 5-HT1P receptors
Main clinical applications: used for treatment of functional dyspepsia with impaired accommodation; acute migraine, cluster headache attacks
- *Pharmacodynamics: Mechanism/Sites of action**
- its peripheral actions include fundal relaxation and reductions in antral motility; as a 5-HT1B/1D agonist it causes vasoconstriction
Adverse Effects: may initially cause flushing, dizziness, weakness, nausea, drowsiness, stiffness, or feelings of tingling
Sucralfate
Classification: cytoprotectant; mucosal coating agent
Main clinical applications: treatment of gastric, duodenal, stress ulcers
- *Pharmacodynamics: Mechanism/Sites of action**
- acts locally (not systematically) to complex with proteins at ulcer site; forms a protective, viscous, adhesive barrier on the surface of intact mucosa of stomach and duodenum; inhibits pepsin activity
Adverse Effects: constipation
Antacids
Classification: (Al)OH3, Mg(OH)2, CaCO3; Alka-Seltzer (acetylsalicylic acid, sodium bicarbondate (NaHCO3), and citric acid) also simethicone
Main clinical applications: antacids neutralize acid in stomach
Pharmacodynamics: Mechanism/Sites of action
- Neutralization by acid-base interactions or binding of H+
often included in these preparations - simethicone: antiflatulent agent/ surfactant that may reduce flatulence or belching by decreasing foaming (change in surface tension of gas bubbles which otherwise quickly coalesce)
Adverse Effects: constipation