Serotonin antagonists are a class of prescription drugs used in the treatment and prevention of nausea and vomiting. This class is sometimes referred to as 5-HT3 receptor antagonists or serotoninblockers. 5-HT3 stands for 5-hydroxytryptamine, the chemical structure and name for serotonin. This class is used in cases of nausea and vomiting specifically related to chemotherapy treatment, radiation, and postoperative effects. Nausea and vomiting related to these conditions can be severe and further impact the health and safety of the patient, so effective treatment for nausea and vomiting in these cases is very important.
Drug name | Learn more | See SingleCare price |
---|---|---|
Ondansetron | ondansetron details | ondansetron price |
Zofran | zofran details | zofran price |
Sancuso | sancuso details | sancuso price |
Granisetron Hcl | granisetron-hcl details | granisetron-hcl price |
Aloxi | aloxi details | aloxi price |
Palonosetron Hcl | palonosetron-hcl details | palonosetron-hcl price |
Anzemet | anzemet details | anzemet price |
Zuplenz | zuplenz details | zuplenz price |
Sustol | sustol details | sustol price |
Zofran | zofran details | zofran price |
Kytril (granisetron)
Granisol (granisetron)
Serotonin receptor antagonists are a class of medications known as antiemetics available by prescription only for the treatment of nausea and vomiting, particularly cases related to chemotherapy and radiation therapy, and postoperative treatment. Serotonin antagonists are also used for prophylaxis (prevention) of nausea and vomiting in these patients. There are different formulation types available within the class including oral tablets, dissolvable tablets, and intravenous solutions.
You may be thinking of serotonin as one of the many neurotransmitters which affect your mood and energy. It is! Serotonin plays a key role in mood and energy along with dopamine, norepinephrine, histamine, and other neurotransmitters. What you may not realize is that there are many serotonin receptors in your gastrointestinal tract which have other effects as well.
Chemotherapy and radiation cause the release of serotonin from the tissue lining the gastrointestinal tract when it is damaged by the treatment. This now free serotonin interacts with nerve receptors in the stomach that send signals through the central nervous system (CNS) to the portion of the brain which triggers the vomit reflex. By blocking serotonin from interacting with those receptors, the signal is not sent and the likelihood of nausea and vomiting is reduced. It is not understood exactly how serotonin antagonists alleviate postoperative or other types of nausea, though it is presumed to be due to the same CNS signal inhibition.
Nausea and vomiting
Chemotherapy-induced nausea and vomiting
Postoperative nausea and vomiting
Radiation-induced nausea and vomiting
These were the first serotonin receptor antagonists developed. They are available in oral tablets, orally disintegrating tablets, and injectable solutions. The first generation does have an affinity for other serotonin receptors in the body not related to the vomiting reflex. The clinical implications of these affinities are not understood.
Examples: Zofran and Zofran ODT (ondansetron), Sancuso (granisetron), and Anzemet (dolasetron)
There is only one second-generation serotonin antagonist. It has a much greater affinity for 5HT3 receptors and little to no affinity for any other serotonin receptor. This increases the duration of action for this second generation, making it useful in both acute and delayed nausea and vomiting related to chemotherapy.
Example: Aloxi (palonosetron)
Men with no previous history of sensitivity to serotonin antagonists and who have healthy liver function can take serotonin antagonists for nausea and vomiting.
Women may also take serotonin antagonists as long as there is no previous history of sensitivity to serotonin antagonists and healthy liver function has been established.
Ondansetron is the serotonin antagonist utilized most frequently in pregnant patients. Valuable safety data is limited, though there have been suggestions that cleft palate and other malformations have occurred in babies born to mothers who used ondansetron. That incidence appears to be higher when it is taken in the first trimester. The American College of Obstetricians and Gynecologists (ACOG) considers the overall risk very low. In cases of severe or refractory nausea and emesis in pregnancy, the risk may outweigh the risks associated with dehydration due to vomiting.
Children can take serotonin antagonists, though they are generally not recommended for younger children under the age of 4.
Seniors can take serotonin antagonists, though if they have impaired hepatic function, they may not be a good candidate for treatment with these drugs.
Serotonin antagonists should not be used in patients with a known sensitivity to this class of drugs.
Serotonin antagonists are extensively metabolized in the liver. Increased serum plasma levels may occur in patients with hepatitis, hepatic disease, or elevated hepatic enzymes. This can lead to toxicity.
The use of serotonin antagonists may mask more serious gastrointestinal diseases such as adynamic ileus, GI obstruction, or distention after abdominal surgery. Ongoing gastrointestinal symptoms should be investigated to ensure it is nothing more serious.
Serotonin syndrome can occur when a patient is taking one or more serotonergic medications. Serotonin syndrome is characterized by confusion, headache, high blood pressure, and diarrhea. Combining a serotonin antagonist with antidepressants like selective serotonin reuptake inhibitors (SSRIs) may increase the risk of serotonin syndrome.
Serotonin antagonists can cause QT prolongation, a type of arrhythmia. SSRIs like fluoxetine or antipsychotics like chlorpromazine can cause this as well. Combined treatment with two drugs that have this arrhythmia potential increases the likelihood it can happen.
No, serotonin antagonists are not controlled substances.
Headache
Constipation
QT prolongation
Weakness
Pruritus
Bradycardia
Anxiety
Urinary retention
Tinnitus
Thrombocytopenia
Rash
Insomnia
Hypotension
Hypertension
Hypersalivation
Hyperglycemia
Hiccups
Flatulence
Edema
Diarrhea
Dizziness
Aloxi, the only second-generation serotonin antagonist, can be expensive if it is not covered by your insurance. It can cost up to $630. The generic version, palonosetron, is significantly cheaper, and a coupon from SingleCare can lower the price to less than $20.
Zofran, a common first-generation serotonin antagonist, can cost up to $300 without coverage. Thankfully, a coupon from SingleCare can give you significant savings, lowering the cost to less than $7 at participating pharmacies.
Kristi C. Torres, Pharm.D., is a 2005 graduate of The University of Texas at Austin. Her professional background includes academic teaching roles, district-level management for a nationwide pharmacy chain, and clinic-based pharmacy management. Dr. Torres has a wide range of experience in pharmacy operations and has traveled to many states to open and convert clinic-based pharmacies for one of the largest healthcare systems in the nation.
Currently, she works for Tarrytown Expocare Pharmacy in Austin, Texas, serving the intellectual and developmental disability community. There, she leads the order entry team, overseeing orders from across the country.
Dr. Torres began working in pharmacy at the age of 16 in a small East Texas town. She currently resides in Round Rock, Texas, with her daughter and a Shih-Tzu puppy.
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