GI 1 (Vomiting) Flashcards
Acute Chemotherapy/Cytotoxic Drug Induced Vomiting
- Pharmacology
5-HT/5HT3 Receptor Signaling (0-24 hrs)
Delayed Chemotherapy/Cytotoxic Drug Induced Vomiting
- Pharmacology
SP/NK1 Receptor Signaling (>24 hrs)
Ondansetron
- Drug Class?
5-HT(3) Receptor Antagonists
Granisetron
- Drug Class?
5-HT(3) Receptor Antagonists
Alosetron
- Drug Class?
5-HT(3) Receptor Antagonists
- Ischemic Colitis
Palonosetron
- Drug Class?
5-HT(3) Receptor Antagonists
5-HT(3) Receptor
- Mechanism of Action
Ligand Gated Ion Channel
Antagonist targets CTZ and blocks 5-HT(3) receptors from sensitizing spinal sensory neurons and blocks vagal signaling of nausea
- Slows down intestinal movement and secretions
Chlorpromazine
- Drug Class?
Dopamine Receptor 2 (D2) Antagonist
- Sedation
Perphenazine
- Drug Class?
Dopamine Receptor 2 (D2) Antagonist
Prochlorperazine
- Drug Class?
Dopamine Receptor 2 (D2) Antagonist
Trifluoperazine
- Drug Class?
Dopamine Receptor 2 (D2) Antagonist
Dopamine Receptor 2 (D2)
- MOA
G-Protein Coupled Receptor (Gq)
- Causes activation of PLC leading to an increase of IP3 and DAG levels
D2 Antagonist Targets D2 Receptors in CTZ and prevents activation
Dopamine Receptor 2 (D2)
- Adverse Effects
Involuntary Movements:
- Extrapyramidal Syndrome
- Dystonia
- Tardive Dyskinesia
Hyperprolactinemia (D2 is supposed to inhibit prolactin)
- Excessive lactation
- Men lactate
Metoclopramide
- Drug Class?
Dopamine Receptor 2 (D2) Antagonist
- Acts primarily on CTZ
- Also acts on GI (Increases Motility)
- Blocks Histamine and Muscarinic Receptors too
Metoclopramide
- Adverse Effects
Involuntary Movement:
- Spasmodic Torticollis (Neck)
- Oculogyric Crises (Eye)
Hyperprolactinemia
Domperidone
- Drug Class?
Dopamine Receptor 2 (D2) Antagonist
- Does not penetrate BBB, less CNS effect
- Risk of cardiac arrest
Haloperidol
D2 Receptor Antagonists
- Treats Acute Chemotherapy Emesis
Droperidol
D2 Receptor Antagonists
- Treats Acute Chemotherapy Emesis
Levomepromazine
D2 Receptor Antagonists
- Treats Acute Chemotherapy Emesis
Cinnarizine
- Drug Class?
Histamine H1 Receptor Antagonist
Cyclizine
- Drug Class?
Histamine H1 Receptor Antagonist
Promethazine
- Drug Class?
Histamine H1 Receptor Antagonist
Histamine H1 Receptor
- MOA
G-Protein Coupled Receptor (Gq)
- H1 Antagonist manages motion sickness and pregnancy morning sickness
- Does not act on CTZ
Adverse Effects:
- Drowsiness
Hyoscine (Scopolamine)
- Drug Class?
Muscarinic Receptor Antagonist
Muscarinic Antagonist
- Treats?
- Adverse?
M Antagonist is used to prevent and treat motion sickness
- Adverse Effects
–> Dry mouth / Blurred vision
–> Drowsiness
Aprepitant
- Drug Class?
Substance P Antagonist (Neurokinin-1 Receptors)
- Targets CTZ for delayed chemotherapy emesis
Fosaprepitant
- Drug Class?
Inactive Prodrug for Substance P Antagonist (Neurokinin-1 Receptors)
Nabilone
- Drug Class?
Synthetic Cannabinol
- Treats vomiting
- Can be reversed by naloxone through opioid receptors
Dexamethasone
- Drug Class?
Glucocorticoid
- Last Resort Treatment
- High doses are used to prevent vomiting caused by cytotoxic drugs