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Anti-emetics
UVa med pharmacology block 2
| Question | Answer |
|---|---|
| Scopolamine | anti-motion sickness - muscarinic antagonist transdermal patch (4hrs before) or oral (1hr before) fx = sedation |
| Promethazine | Anti-motion sickness/drug nausea - H1 & muscarinic antag fx: sedation |
| Dimenhydrinate | anti-motion sickness - H1 & muscarinic antagonist fx: sedation |
| Ondansetron (& other -etron's) | Selective 5HT-3 antagonist - nausea from opiates, chemotherapy - action on vagal aff, NTS, area postrema fx: best tolerated, minor fx = headache, constipation, warmth, flushing |
| Metoclopramide | Prokinetic - 5HT3 antag @incr doses, D2 antag in CNS, decr nausea from emetic drugs, migraines axn @ Vagal aff, NTS, Area postrema fx: prokinetic fx, incr dose = akathisia/dystonia |
| Chlorpromazine/Prochlorperazine | Neuroleptic phenothiazines - DA receptor antags, post-op, radiation nausea - axn @ area postrema fx: extrapyramidal fx, antiACh fx, sedation |
| Dexamethasone | Glucocorticoid - tx acute emesis from emetic drugs, cancer tx (w/ondansetron) - long duration (36-72hrs) no immuno side fx |
| Lorazepam | Benzo - decr stress/anticipatory emesis pretx for chemo, adjunct for cancer chemo |
| Dronabionol (THC) | Cannabinoid - decr nausea from emetic drugs - agonist on cannab receptors (g-prot) fx: incr appetitite in aids/cancer px's |
| Aprepitant | Substance P receptor antag - chemo assoc'd nausea must be readministered after 2days new/expensive |
| What drugs are best for use of treating Motion Sickness? | - Muscarinic Antagonist (Scopolamine) - Mixed Histamine H1 / Muscarinic Antagonists (Dimenhydrinate aka Dramamine, Promethazine) *Transdermal Scopolamine is especially effective. |
| When must you take a Motion Sickness treatment for effectiveness? | If Oral pill, at least 1hr BEFORE nausea-inducing situation, 4hrs before for Transdermal. |
| Which Cannabinoid is mainly used for nausea and emesis treatment? | Dronabinol. Their most beneficial use is to stimulate appetite in AIDS patients, but they are moderately effective against nausea/emesis induced by low emetogenic drugs. |
| What are the clinical uses of Metoclopromide? | - Mainly used to treat Gastroparesis/GI Reflux (Has a Prokinetic effect on GI) - Can be used to treat Nausea from MILDLY emetic drugs. |
| Which Benzodiazapene is used as an adjunct treatment with cancer chemotherapy as an Anti-emetic? | Lorazepam *It reduces stress and therefore "Anticipatory emesis" |
| What are the side effects of Metoclopromide? | Extrapyramidal side-effects: Akathisia, Dystonia. |
| What is the therapeutic use for Scopolamine? | Treats Motion Sickness (Antimuscarinic) |
| What is the use of Dexamethasone? | - Greatly enhances effectiveness of other Anti-Emetics in cancer patients. - Used solo to treat post-op nausea. *Odansetron + Dexamethasone = Combo of choice to treat acute Emesis/Vomiting induced by highly emetogenic drugs. |
| What are side effects of Phenothiazines? | Anti-Ach effects, Sedation. Extrapyramidal side effects are most concerning, thus these drugs are a last resort. |
| Which drug is a "Substance P" receptor antagonist? | Aprepitant |
| What is the clinical use of Aprepitant? Why might it be limited? | It is used with 1st dose of Chemotherapy along with Odansetron and Dexamethasone. It is especially effective against delayed nausea. Its use may be limited as it is very expensive. |
| What is the clinical use of Odansetron? | Alleviates Post-op Nausea, Opiate-induced nausea, Cancer-chemotherapy-induced nausea. |
| What are side effects of Odansetron? | Headache, constipation, warmth, flushing. |
| What is the anti-emetic of choice to use along with SSRI's? | Odansetron |
| What is the anti-emetic of choice to use for a Migraine? | Metoclopromide |
| What is the anti-emetic of choice for severe pain? | Opiates |
| What are the sites of action of Odansetron (5HT-3 Antagonist)? | - Vagal Afferents - Nucleus of Solitary Tract - Area Postrema |
| What are side effects of Motion Sickness treatments? | - Sedation - Any low-dose Antimuscarinic effects (Dry mouth/eyes, Increased HR/BP, Mydriasis) |
| What are the Phenothiazines used for clinically? | Thay are DA receptor antagonists used for: - Post-op Nausea - Vomiting induced by Radiation/Opiates *In treatment of nausea due to cancer treatments, they are third-line agents ("Recsue Therapy" if other treatments are insufficient) |
| What are some physiological triggers for vomiting? | - Stimulation of Stretch/Chemo sensitive vagal afferents in Stomach and Upper GI (e.g. Hypomotility) - Stimulation of Area Postrema (Chemo-Trigger zone, e.g toxins). - Vestibular afferents (Motion Sickness) - Higher Cortical Centers (Conditioned Res) |
| Where is the autonomic control center for vomiting? | Medulla Oblongata - Synchronizes rythmic contractions of respiratory/abdominal muscles and gastric/esophageal constriction/relaxation. |
| Where is the site of action of Metoclopromide? | It is a Dopamine/5HT-3 Antagonist, 5HT-4 Agonist, at the Area Postrema, NTS, and Vagal afferents |
| What types of receptors does the Area Postrema express? | Muscarinic, Nicotinic, Opiate, Dopaminergic. It also projects to the Nucleus of the Solitary Tract (Which receives afferent input from many organs) |
Created by:
sam.mrosenfeld
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