Difference between revisions of "Ondansetron"
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{{Infobox drug reference | {{Infobox drug reference | ||
| trade_names = | | trade_names = Zofran | ||
| drug_class = | | drug_class = Antiemetic | ||
| drug_class_color = | | drug_class_color = | ||
| uses = | | uses = Prevention and treatment of postoperative nausea and vomiting | ||
| contraindications = | | contraindications = Prolonged QT interval | ||
| routes = | Patients taking apomorphine | ||
| routes = PO, IM, IV | |||
| dosage = | | dosage = | ||
| dosage_calculation = ondansetron | |||
| mechanism = 5HT3 antagonist | |||
| adverse_effects = Cardiac arrhythmias, cardiac arrest, constipation, headaches | |||
| duration = | |||
| metabolism = Liver oxidation followed by glucuronidation and sulfate conjugation | |||
| halflife_elimination = 4 hours | |||
}} | }} | ||
'''Ondansetron''' is a 5HT<sub>3</sub> receptor antagonist that is commonly used for the prevention and treatment of postoperative nausea and vomiting. | |||
== Uses<!-- Describe uses of the drug. If appropriate, add subsections for each indication. --> == | == Uses<!-- Describe uses of the drug. If appropriate, add subsections for each indication. --> == | ||
* Prevention and treatment of postoperative nausea and vomiting | |||
* Commonly used to treat many other causes of nausea and vomiting<ref name=":0">{{Citation|last=Griddine|first=Alexandria|title=Ondansetron|date=2022|url=http://www.ncbi.nlm.nih.gov/books/NBK499839/|work=StatPearls|place=Treasure Island (FL)|publisher=StatPearls Publishing|pmid=29763014|access-date=2023-01-05|last2=Bush|first2=Jeffrey S.}}</ref> | |||
== Contraindications<!-- List contraindications and precautions for use of the drug. --> == | == Contraindications<!-- List contraindications and precautions for use of the drug. --> == | ||
=== Absolute contraindications<!-- List absolute contraindications for use of the drug. If none, this section may be removed. --> === | === Absolute contraindications<!-- List absolute contraindications for use of the drug. If none, this section may be removed. --> === | ||
* Prolonged QT intervals | |||
* Patients taking apomorphine <ref name=":0" /> as it can cause hypotension and loss of consciousness | |||
=== Precautions<!-- List precautions for use of the drug. If none, this section may be removed. --> === | === Precautions<!-- List precautions for use of the drug. If none, this section may be removed. --> === | ||
* Maximum dose of 16 mg IV due to risk of QT prolongation and arrhythmias | |||
* Maximum dose decreased to 8 mg IV or 8 mg PO in severe hepatic impairment | |||
* Dissolving tablets formulations contain phenylalanine which can lead to irreversible neurological damage in phenylketonuria (PKU)<ref name=":0" /> | |||
== Pharmacology == | == Pharmacology == | ||
| Line 24: | Line 41: | ||
==== Mechanism of action<!-- Describe the mechanism of action for the primary uses of the drug. --> ==== | ==== Mechanism of action<!-- Describe the mechanism of action for the primary uses of the drug. --> ==== | ||
* Antagonism of the 5HT<sub>3</sub> receptors | |||
* Centrally, ondansetron antagonizes the 5HT<sub>3</sub> receptors in the area postrema <ref name=":0" /> | |||
* Peripherally, ondansetron antagonizes the 5HT<sub>3</sub> receptors on the vagus nerve within the GI tracts which forms synapses within the nucleus tracts solitarius <ref name=":0" /> | |||
** Predominant mechanism for its anti-emetic effect | |||
==== Adverse effects<!-- Describe any potential adverse effects of the drug. --> ==== | ==== Adverse effects<!-- Describe any potential adverse effects of the drug. --> ==== | ||
* Cardiac arrhythmia | |||
* Cardiac arrest | |||
* Constipation | |||
* Headache | |||
* dry mouth | |||
* malaise | |||
* drowsiness | |||
* sedation | |||
* pruritus | |||
* transient elevation in liver function test | |||
=== Pharmacokinetics<!-- Describe the pharmacokinetics of the drug. --> === | === Pharmacokinetics<!-- Describe the pharmacokinetics of the drug. --> === | ||
* Peak plasma concentration about 1.5 hours after an 8 mg PO dose | |||
* Plasma half life is approximately 4 hours<ref name=":1">{{Citation|last=Zabirowicz|first=Eric S.|title=Pharmacology of Postoperative Nausea and Vomiting|date=2019|url=http://dx.doi.org/10.1016/b978-0-323-48110-6.00034-x|work=Pharmacology and Physiology for Anesthesia|pages=671–692|publisher=Elsevier|access-date=2023-01-05|last2=Gan|first2=Tong J.}}</ref> | |||
*Metabolized by CYP2D6, CYP3A4, CYP2E1, CYP1A2 initially with oxidation followed by glucuronide and sulfate conjugations <ref name=":0" /> | |||
** Many polymorphisms with four different phenotypes | |||
*** Poor metabolizer (no functional allele) | |||
*** Intermediate metabolizer (less activity than one functional allele) | |||
*** Extensive metabolizer (two functional allele, most common phenotype) | |||
*** Ultrarapid metabolizer (three functional allele) | |||
== Chemistry and formulation<!-- Describe the chemistry and formulation of the drug. --> == | == Chemistry and formulation<!-- Describe the chemistry and formulation of the drug. --> == | ||
Available in PO, intramuscular (IM), and intravenous (IV). | |||
== History<!-- Describe the historical development of the drug. --> == | == History<!-- Describe the historical development of the drug. --> == | ||
== References == | == References == | ||
[[Category:Drug reference]] | [[Category:Drug reference]] | ||
<references /> | |||
[[Category:Antiemetics]] | |||
Latest revision as of 13:36, 8 January 2023
Ondansetron
| Trade names |
Zofran |
|---|---|
| Clinical data | |
| Drug class |
Antiemetic |
| Uses |
Prevention and treatment of postoperative nausea and vomiting |
| Contraindications |
Prolonged QT interval Patients taking apomorphine |
| Routes of administration |
PO, IM, IV |
| Dosage | |
| Pharmacodynamics | |
| Mechanism of action |
5HT3 antagonist |
| Adverse effects |
Cardiac arrhythmias, cardiac arrest, constipation, headaches |
| Pharmacokinetics | |
| Metabolism |
Liver oxidation followed by glucuronidation and sulfate conjugation |
| Elimination half-life |
4 hours |
| Physical and chemical data | |
| Article quality | |
| Editor rating | |
| User likes | 0 |
Ondansetron is a 5HT3 receptor antagonist that is commonly used for the prevention and treatment of postoperative nausea and vomiting.
Uses
- Prevention and treatment of postoperative nausea and vomiting
- Commonly used to treat many other causes of nausea and vomiting[1]
Contraindications
Absolute contraindications
- Prolonged QT intervals
- Patients taking apomorphine [1] as it can cause hypotension and loss of consciousness
Precautions
- Maximum dose of 16 mg IV due to risk of QT prolongation and arrhythmias
- Maximum dose decreased to 8 mg IV or 8 mg PO in severe hepatic impairment
- Dissolving tablets formulations contain phenylalanine which can lead to irreversible neurological damage in phenylketonuria (PKU)[1]
Pharmacology
Pharmacodynamics
Mechanism of action
- Antagonism of the 5HT3 receptors
- Centrally, ondansetron antagonizes the 5HT3 receptors in the area postrema [1]
- Peripherally, ondansetron antagonizes the 5HT3 receptors on the vagus nerve within the GI tracts which forms synapses within the nucleus tracts solitarius [1]
- Predominant mechanism for its anti-emetic effect
Adverse effects
- Cardiac arrhythmia
- Cardiac arrest
- Constipation
- Headache
- dry mouth
- malaise
- drowsiness
- sedation
- pruritus
- transient elevation in liver function test
Pharmacokinetics
- Peak plasma concentration about 1.5 hours after an 8 mg PO dose
- Plasma half life is approximately 4 hours[2]
- Metabolized by CYP2D6, CYP3A4, CYP2E1, CYP1A2 initially with oxidation followed by glucuronide and sulfate conjugations [1]
- Many polymorphisms with four different phenotypes
- Poor metabolizer (no functional allele)
- Intermediate metabolizer (less activity than one functional allele)
- Extensive metabolizer (two functional allele, most common phenotype)
- Ultrarapid metabolizer (three functional allele)
- Many polymorphisms with four different phenotypes
Chemistry and formulation
Available in PO, intramuscular (IM), and intravenous (IV).
History
References
- ↑ 1.0 1.1 1.2 1.3 1.4 1.5 Griddine, Alexandria; Bush, Jeffrey S. (2022), "Ondansetron", StatPearls, Treasure Island (FL): StatPearls Publishing, PMID 29763014, retrieved 2023-01-05
- ↑ Zabirowicz, Eric S.; Gan, Tong J. (2019), "Pharmacology of Postoperative Nausea and Vomiting", Pharmacology and Physiology for Anesthesia, Elsevier, pp. 671–692, retrieved 2023-01-05
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