Antinausea drugs
Definition
Antinausea drugs are medicines that control nausea—a feeling of sickness or queasiness in the stomach with an urge to vomit. These drugs also prevent or stop vomiting. Drugs that control vomiting are called antiemetic drugs.
| Brand Name (Generic Name) | Possible Common Side Effects Include: |
| Compazine (phochlorperazine) | Involuntary muscle spasms, dizziness, jitteriness, puckering of the mouth |
| Phenergan (promethazine hydrochloride) | Dizziness, dry mouth, nausea and vomiting, rash |
| Reglan (metoclopramide hydrochloride) | Fatigue, drowsiness, restlessness |
| Tigan (trimethobenzamide hydrochloride) | Blurred vision, diarrhea, cramps, headache |
| Zofan (ondansetron hydrochloride) | Constipation, headache, fatigue, abdominal pain |
Purpose
Prochlorperazine (Compazine), the medication described in detail in this entry, controls both nausea and vomiting. Prochlorperazine is also sometimes prescribed for symptoms of mental disorders, such as schizophrenia. Prochlorperazine may be used to control the nausea and vomiting that occur during recovery from the general anesthetics used in surgery.
Some antihistamines such as dimenhydrinate (Dramamine) and meclizine (Antivert, Bonine) are useful for treatment of the nausea and vomiting associated with motion sickness.
A group of drugs called the 5HT3 inhibitors, ondansetron (Zofran) and granisetron (Kytril), are used to control the nausea and vomiting associated with anticancer drugs. Ondansetron and granisetron are also valuable for controlling nausea and vomiting following surgery.
Corticosteroid hormones such as dexamethasone (Decadron, Hexdrol) may also be used as antiemetics.
Description
Prochlorperazine is available only with a physician's prescription. It is sold in syrup, capsule, tablet, injection, and suppository forms.
Recommended dosage
To control nausea and vomiting in adults, the usual dose is:
- Tablets: one 5-mg or 10-mg tablet three to four times a day
- Extended-release capsules: one 15-mg capsule first thing in the morning or one 10-mg capsule every 12 hours
- Suppository: 25 mg, twice a day
- Syrup: 5–10 mg three to four times a day
- Injection: 5–10 mg injected into a muscle three to four times a day
Doses for children must be determined by a physician.
Precautions
Prochlorperazine may cause a movement disorder called tardive dyskinesia. Signs of this disorder are involuntary twitches and muscle spasms in the face and body and jutting or rolling movements of the tongue. The condition may be permanent. Older people, especially women, are particularly at risk of developing this problem when they take prochlorperazine.
Some people feel drowsy, dizzy, lightheaded, or less alert when using this medicine. The drug may also cause blurred vision, and movement problems. For these reasons, people who take this drug should not drive, use machines, or do anything else that might be dangerous until they have found out how the drug affects them.
Prochlorperazine makes some people sweat less, which can allow the body to overheat. The drug may also make the skin and eyes more sensitive to the sun. People who are taking prochlorperazine should try to avoid extreme heat and exposure to the sun. When going outdoors, they should wear protective clothing, a hat, a sunscreen with a skin protection factor (SPF) of at least 15, and sunglasses that block ultraviolet (UV) light. Saunas, sunlamps, tanning booths, tanning beds, hot baths, and hot tubs should be avoided while taking this medicine. Anyone who must be exposed to extreme heat while taking the drug should check with his or her physician.
This medicine adds to the effects of alcohol and other drugs that slow down the central nervous system, such as antihistamines, cold and flu medicines, tranquilizers, sleep aids, anesthetics, some pain medicines, and muscle relaxants . People taking prochlorperazine should not drink alcohol, and should check with the physician who prescribed the drug before combining it with any other medicines.
Patients should not stop taking this medicine without checking with the physician who prescribed it. Stopping the drug suddenly can dizziness, nausea, vomiting, tremors, and other side effects. When stopping the medicine, it may be necessary to taper the dose gradually.
Prochlorperazine may cause false pregnancy tests.
Women who are pregnant (or planning to become pregnant) or are breastfeeding should check with their physicians before using this medicine.
Before using prochlorperazine, people with any of these medical problems should make sure their physicians are aware of their conditions:
- previous sensitivity or allergic reaction to prochlorperazine
- heart disease
- glaucoma
- brain tumor
- intestinal blockage
- abnormal blood conditions, such as leukemia
- exposure to pesticides
Side effects
Many side effects are possible with this drug, including, but not limited to, constipation, dizziness, drowsiness, decreased sweating, dry mouth, stuffy nose, movement problems, changes in menstrual period, increased sensitivity to sun, and swelling or pain in breasts. Anyone who has unusual or troublesome symptoms after taking prochlorperazine should contact his or her physician.
Interactions
Prochlorperazine may interact with other medicines. When this happens, the effects of one or both of the drugs may change or the risk of side effects may be greater. Among the drugs that may interact with prochlorperazine are antiseizure drugs such as phenytoin (Dilantin) and carbamazepine (Tegretol), anticoagulants such as warfarin (Coumadin), and drugs that slow the central nervous system such as alprazolam (Xanax), diazepam (Valium), and secobarbital (Seconal). Not every drug that interacts with prochlorperazine is listed here, and all patients should consult with a physician or pharmacist before taking any other prescription or nonprescription (over-the-counter) drug with prochlorperazine.
Resources
books
Brody, T. M., J. Larner, K. P. Minneman, and H. C. Neu. Human Pharmacology: Molecular to Clinical, 2nd ed. St. Louis: Mosby Year-Book, 1998.
Griffith, H. W., and S. Moore. 2001 Complete Guide to Prescription and Nonprescription Drugs. New York: Berkely Publishing Group, 2001.
other
"Anticholinergics/Antispasmodics." Medline Plus Drug Information. [cited June 25 2003] http://www.nlm.nih.gov/medlineplus/druginfo/uspdi/202049.html .
"Antihistamines (Systemic)." Medline Plus Drug Information. [cited June 25 2003] <http://www.nlm.nih.gov/medline plus/druginfo/uspdi/202060.html> .
"Ondansetron." Medline Plus Drug Information. [cited June 25 2003] http://www.nlm.nih.gov/medlineplus/druginfo/medmaster/a601209.html .
"Prochlorperazine." Medline Plus Drug Information. [cited June 25, 2003] < http://www.nlm.nih.gov/medlineplus/druginfo/medmaster/a682116.html> .
Nancy Ross-Flanigan Sam Uretsky, PharmD
Stemetil suppresses activity in the trigger zones of the vomiting center by "paralyzing the gastrointestinal tract" which governs the vomiting reflex, which can exacerbate dismotility. Stemetil is widely distributed into body tissues and fluids. Stemetil undergoes metabolism in the gastric mucosa and on first pass through the liver where it enters the enterohepatic circulation and is excreted chiefly in the feces.
The antiemetic action of Stemetil may mask the signs and symptoms of drug overdosage from other drugs and may obscure the diagnosis and treatment of other conditions. Prochlorperazine intoxication or poisoning can cause deep physiologic depression that resembles and can also mimic brain death.
Phenothiazine compounds should not be used in patients receiving large doses of hypnotics (opioids), due to the possibility of potentiation.
Stemetil can lead to changes in the blood-brain barrier (BBB), allowing an infectious agent to gain entry to the brain and produce lethal central nervous system (CNS) brain and spinal cord infection. The scientific literature describe two bacterial factors specific to the meningitis pathogen that thwart the normal protective role of the blood-brain barrier, leading to serious infection by invasion of the CNS. Further, sugar solution in IV which can lead to hyperglycemia creates gaps in the blood- brain barrier allowing chemicals such as Stemetil to enter which can serve to shuttle infectious matter directly into the brain and CNS. Blood-brain barrier (BBB) disruption is usually accompanied by cerebral edema.
Notably, antiemetic/antipsychotic drugs, such as Stemetil (prochlorperazine), can cross the blood-brain barrier taking with it purulent exhudates in the presence of bacterial infection. Purulent exhudates is a medical term for "pus-producing bacteria", usually the result of serious infection. The most common manifestations are meningitis and brain abscess. Atypical antipsychotic medications can also trigger diabetes.
Once across the blood-brain barrier, the infection enters neural cells, with resultant disruption in cell functioning, perivascular congestion, hemorrhage, and inflammatory response diffusely affecting gray matter disproportionately to white matter. CAVEAT: Blood borne infection in the blood lyse easily. It seems logical to assume that Stemetil would be contraindicated to serious infection for this reason. Increased sedation is ALSO a serious side effect of this type of agent.