Antiemetic
Encyclopedia
An antiemetic is a drug
that is effective against vomiting and nausea
. Antiemetics are typically used to treat motion sickness
and the side effects
of opioid
analgesic
s, general anaesthetic
s, and chemotherapy
directed against cancer
.
Anti-emetics are also used for morning sickness
, but there is little information about the effect on the fetus, and doctors prefer not to use them unless it is strictly necessary.
Medication
A pharmaceutical drug, also referred to as medicine, medication or medicament, can be loosely defined as any chemical substance intended for use in the medical diagnosis, cure, treatment, or prevention of disease.- Classification :...
that is effective against vomiting and nausea
Nausea
Nausea , is a sensation of unease and discomfort in the upper stomach with an involuntary urge to vomit. It often, but not always, precedes vomiting...
. Antiemetics are typically used to treat motion sickness
Motion sickness
Motion sickness or kinetosis, also known as travel sickness, is a condition in which a disagreement exists between visually perceived movement and the vestibular system's sense of movement...
and the side effects
Adverse effect (medicine)
In medicine, an adverse effect is a harmful and undesired effect resulting from a medication or other intervention such as surgery.An adverse effect may be termed a "side effect", when judged to be secondary to a main or therapeutic effect. If it results from an unsuitable or incorrect dosage or...
of opioid
Opioid
An opioid is a psychoactive chemical that works by binding to opioid receptors, which are found principally in the central and peripheral nervous system and the gastrointestinal tract...
analgesic
Analgesic
An analgesic is any member of the group of drugs used to relieve pain . The word analgesic derives from Greek an- and algos ....
s, general anaesthetic
General anaesthetic
A general anaesthetic is a drug that brings about a reversible loss of consciousness. These drugs are generally administered by an anaesthesia provider to induce or maintain general anaesthesia to facilitate surgery...
s, and chemotherapy
Chemotherapy
Chemotherapy is the treatment of cancer with an antineoplastic drug or with a combination of such drugs into a standardized treatment regimen....
directed against cancer
Cancer
Cancer , known medically as a malignant neoplasm, is a large group of different diseases, all involving unregulated cell growth. In cancer, cells divide and grow uncontrollably, forming malignant tumors, and invade nearby parts of the body. The cancer may also spread to more distant parts of the...
.
Anti-emetics are also used for morning sickness
Morning sickness
Morning sickness, also called nausea gravidarum, nausea, vomiting of pregnancy , or pregnancy sickness is a condition that affects more than half of all pregnant women. Related to increased oestrogen levels, a similar form of nausea is also seen in some women who use hormonal contraception or...
, but there is little information about the effect on the fetus, and doctors prefer not to use them unless it is strictly necessary.
Types of antiemetics
Antiemetics include:- 5-HT3 receptor antagonists5-HT3 antagonistThe 5-HT3 antagonists are a class of medications that act as receptor antagonists at the 5-HT3 receptor, a subtype of serotonin receptor found in terminals of the vagus nerve and in certain areas of the brain....
– these block serotoninSerotoninSerotonin or 5-hydroxytryptamine is a monoamine neurotransmitter. Biochemically derived from tryptophan, serotonin is primarily found in the gastrointestinal tract, platelets, and in the central nervous system of animals including humans...
receptors in the central nervous systemCentral nervous systemThe central nervous system is the part of the nervous system that integrates the information that it receives from, and coordinates the activity of, all parts of the bodies of bilaterian animals—that is, all multicellular animals except sponges and radially symmetric animals such as jellyfish...
and gastrointestinal tractGastrointestinal tractThe human gastrointestinal tract refers to the stomach and intestine, and sometimes to all the structures from the mouth to the anus. ....
. As such, they can be used to treat post-operative and cytotoxic drug nausea & vomiting. However, they can also cause ConstipationConstipationConstipation refers to bowel movements that are infrequent or hard to pass. Constipation is a common cause of painful defecation...
, DiarrheaDiarrheaDiarrhea , also spelled diarrhoea, is the condition of having three or more loose or liquid bowel movements per day. It is a common cause of death in developing countries and the second most common cause of infant deaths worldwide. The loss of fluids through diarrhea can cause dehydration and...
, Drymouth, and Fatigue.- DolasetronDolasetronDolasetron is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. It does not have much antiemetic effect when...
(Anzemet) - can be administered in tablet form or in an injection. - GranisetronGranisetronGranisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. It does not have much effect...
(Kytril, Sancuso) - can be administered in tablet (Kytril), oral solution (Kytril), or in a single transdermal patch to the upper arm (SANCUSO). - OndansetronOndansetronOndansetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic , often following chemotherapy. Its effects are thought to be on both peripheral and central nerves...
(Zofran) - administered in an oral tablet form, oral dissolving tablet form, or in an injection. - TropisetronTropisetronTropisetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic to treat nausea and vomiting following chemotherapy, although it has been used experimentally as an analgesic in cases of fibromyalgia. The drug is available in a 5 mg oral preparation or in 2 mg...
(Navoban) - can be administered in oral capsules or in injection form. - PalonosetronPalonosetronPalonosetron is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting...
(Aloxi) - can be administered in an injection or in oral capsules. - MirtazapineMirtazapineMirtazapine is a tetracyclic antidepressant used primarily in the treatment of depression. It is also sometimes used as a hypnotic, antiemetic, and appetite stimulant, and for the treatment of anxiety, among other indications...
(Remeron), an antidepressantAntidepressantAn antidepressant is a psychiatric medication used to alleviate mood disorders, such as major depression and dysthymia and anxiety disorders such as social anxiety disorder. According to Gelder, Mayou &*Geddes people with a depressive illness will experience a therapeutic effect to their mood;...
that also has antiemetic effects.
- Dolasetron
- Dopamine antagonistDopamine antagonistA dopamine antagonist is a drug which blocks dopamine receptors by receptor antagonism. There are five known types of dopamine receptors in the human body; they are found in the brain, peripheral nervous system, blood vessels, gastrointestinal tract and the kidney.-Uses and examples:* Used as...
s act in the brain and are used to treat nausea and vomiting associated with neoplastic disease, radiation sickness, opioids, cytotoxic drugs and general anaesthetics. Side effects include Muscle Spasms and RestlessnessPsychomotor agitationPsychomotor agitation is a series of unintentional and purposeless motions that stem from mental tension and anxiety of an individual. This includes pacing around a room, wringing one's hands, pulling off clothing and putting it back on and other similar actions...
.- DomperidoneDomperidoneDomperidone is an antidopaminergic drug, developed by Janssen Pharmaceutica, and used orally, rectally or intravenously, generally to suppress nausea and vomiting, or as a prokinetic agent...
- OlanzapineOlanzapineOlanzapine is an atypical antipsychotic, approved by the FDA for the treatment of schizophrenia and bipolar disorder...
- DroperidolDroperidolDroperidol is an antidopaminergic drug used as an antiemetic and antipsychotic...
, haloperidolHaloperidolHaloperidol is a typical antipsychotic. It is in the butyrophenone class of antipsychotic medications and has pharmacological effects similar to the phenothiazines....
, chlorpromazineChlorpromazineChlorpromazine is a typical antipsychotic...
, promethazinePromethazinePromethazine is a first-generation antihistamine of the phenothiazine family. The drug has anti-motion sickness, antiemetic, and anticholinergic effects, as well as a strong sedative effect and in some countries is prescribed for insomnia when benzodiazepines are contraindicated...
, prochlorperazineProchlorperazineProchlorperazine is a dopamine receptor antagonist that belongs to the phenothiazine class of antipsychotic agents that are used for the antiemetic treatment of nausea and vertigo. It is also a highly-potent typical antipsychotic, 10-20x more potent than chlorpromazine...
. Some of these drugs are limited in their usefulness by their extra-pyramidalExtrapyramidal systemIn human anatomy, the extrapyramidal system is a neural network located in the brain that is part of the motor system involved in the coordination of movement. The system is called "extrapyramidal" to distinguish it from the tracts of the motor cortex that reach their targets by traveling through...
and sedative side-effects. - MetoclopramideMetoclopramideMetoclopramide is an antiemetic and gastroprokinetic agent. It is commonly used to treat nausea and vomiting, to facilitate gastric emptying in people with gastroparesis, and as a treatment for the gastric stasis often associated with migraine headaches.-Medical uses:Metoclopramide is commonly...
(Reglan) also acts on the GI tract as a pro-kinetic, and is thus useful in gastrointestinal disease; however, it is poor in cytotoxic or post-op vomiting. - AlizaprideAlizaprideAlizapride is a dopamine antagonist with prokinetic and antiemetic effects used in the treatment of nausea and vomiting, including postoperative nausea and vomiting. It is structurally related to metoclopramide and other benzamides.- See also :* Antiemetic* BenzamideAnon., Drugs Future 1981, 6, 11....
- ProchlorperazineProchlorperazineProchlorperazine is a dopamine receptor antagonist that belongs to the phenothiazine class of antipsychotic agents that are used for the antiemetic treatment of nausea and vertigo. It is also a highly-potent typical antipsychotic, 10-20x more potent than chlorpromazine...
(Compazine, Stemzine, Buccastem, Stemetil, Phenotil)
- Domperidone
- NK1 receptor antagonistNK1 receptor antagonistNeurokinin 1 antagonists are a novel class of medications that possesses unique antidepressant, anxiolytic, and antiemetic properties. The discovery of neurokinin 1 receptor antagonists was a turning point in the prevention of nausea and vomiting associated with cancer chemotherapy.An example of...
- AprepitantAprepitantAprepitant is an antiemetic chemical compound that belongs to a class of drugs called substance P antagonists . It mediates its effect by blocking the neurokinin 1 receptor.Aprepitant is manufactured by Merck & Co...
(Emend) Commercially available NK1 Receptor antagonist - CasopitantCasopitantCasopitant is an neurokinin 1 receptor antagonist undergoing research for the treatment of chemotherapy-induced nausea and vomiting . It is currently under development by GlaxoSmithKline ....
Investigational NK1 receptor antagonist
- Aprepitant
- AntihistamineAntihistamineAn H1 antagonist is a histamine antagonist of the H1 receptor that serves to reduce or eliminate effects mediated by histamine, an endogenous chemical mediator released during allergic reactions...
s (H1 histamine receptorHistamine receptorThe histamine receptors are a class of G protein-coupled receptors with histamine as their endogenous ligand.There are four known histamine receptors:*H1 receptor*H2 receptor*H3 receptor*H4 receptor-Comparison:...
antagonists), effective in many conditions, including motion sickness, morning sickness in pregnancy, and to combat opioidOpioidAn opioid is a psychoactive chemical that works by binding to opioid receptors, which are found principally in the central and peripheral nervous system and the gastrointestinal tract...
nausea.- CyclizineCyclizineCyclizine is an antihistamine drug used to treat nausea, vomiting and dizziness associated with motion sickness, vertigo and post-operatively following administration of general anaesthesia and opioids.-Indications:...
- DiphenhydramineDiphenhydramineDiphenhydramine hydrochloride is a first-generation antihistamine possessing anticholinergic, antitussive, antiemetic, and sedative properties which is mainly used to treat allergies. Like most other first-generation antihistamines, the drug also has a powerful hypnotic effect, and for this reason...
(Benadryl) - DimenhydrinateDimenhydrinateDimenhydrinate is an over-the-counter drug used to prevent nausea and motion sickness...
(Gravol, Dramamine) - MeclozineMeclozineMeclozine is an antihistamine considered to be an antiemetic. It is sold under the brand names Bonine, Bonamine, Antivert, Postafen, Sea Legs, and Dramamine . Emesafene is a combination of meclozine and pyridoxine...
(Bonine, Antivert) - PromethazinePromethazinePromethazine is a first-generation antihistamine of the phenothiazine family. The drug has anti-motion sickness, antiemetic, and anticholinergic effects, as well as a strong sedative effect and in some countries is prescribed for insomnia when benzodiazepines are contraindicated...
(Pentazine, Phenergan, Promacot) Promethazine can be administered via a rectal suppository for adults and children over 2 years of age. - HydroxyzineHydroxyzineHydroxyzine is a first-generation antihistamine of the diphenylmethane and piperazine classes. It was first synthesized by Union Chimique Belge in 1956 and was marketed by Pfizer in the United States later the same year, and is still in widespread use today....
- Cyclizine
- Cannabinoids are used in patients with cachexiaCachexiaCachexia or wasting syndrome is loss of weight, muscle atrophy, fatigue, weakness, and significant loss of appetite in someone who is not actively trying to lose weight...
, cytotoxic nausea, and vomiting, or who are unresponsive to other agents. These may cause changes in perception, dizziness, and loss of coordination.- CannabisMedical cannabisMedical cannabis refers to the use of parts of the herb cannabis as a physician-recommended form of medicine or herbal therapy, or to synthetic forms of specific cannabinoids such as THC as a physician-recommended form of medicine...
- Medical marijuana, in the U.S., it is a Schedule I drug. - Dronabinol (Marinol) - a Schedule III drug in the U.S.
- Some synthetic cannabinoids such as NabiloneNabiloneNabilone is a synthetic cannabinoid with therapeutic use as an antiemetic and as an adjunct analgesic for neuropathic pain. It is a synthetic cannabinoid, which mimics the main ingredient of cannabis...
(Cesamet) or the JWH series. - SativexSativexNabiximols is a cannabinoid oromucosal mouth spray developed by the UK company GW Pharmaceuticals for multiple sclerosis patients, who can use it to alleviate neuropathic pain, spasticity, overactive bladder, and other symptoms. Nabiximols is also being developed in Phase III trials as a...
is an oral spray containing THC and CBD. It is currently legal in Canada and a few countries in Europe but not legal in the U.S.
- Cannabis
- Benzodiazepines
- MidazolamMidazolamMidazolam is a short-acting drug in the benzodiazepine class developed by Hoffmann-La Roche in the 1970s. The drug is used for treatment of acute seizures, moderate to severe insomnia, and for inducing sedation and amnesia before medical procedures. It possesses profoundly potent anxiolytic,...
given at the onset of anesthesia has been shown in recent trials to be as effective as ondansetronOndansetronOndansetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic , often following chemotherapy. Its effects are thought to be on both peripheral and central nerves...
.
- Midazolam
-
- LorazepamLorazepamLorazepam is a high-potency short-to-intermediate-acting 3-hydroxy benzodiazepine drug that has all five intrinsic benzodiazepine effects: anxiolytic, amnesic, sedative/hypnotic, anticonvulsant, antiemetic and muscle relaxant...
said to be very good as an adjunct treatment for nausea along with first line medications such as Compazine or Zofran.
- Lorazepam
- AnticholinergicAnticholinergicAn anticholinergic agent is a substance that blocks the neurotransmitter acetylcholine in the central and the peripheral nervous system. An example of an anticholinergic is dicycloverine, and the classic example is atropine....
s- Hyoscine (also known as scopolamineScopolamineScopolamine, also known as levo-duboisine, and hyoscine, is a tropane alkaloid drug with muscarinic antagonist effects. It is among the secondary metabolites of plants from Solanaceae family of plants, such as henbane, jimson weed and Angel's Trumpets , and corkwood...
)
- Hyoscine (also known as scopolamine
- SteroidSteroidA steroid is a type of organic compound that contains a characteristic arrangement of four cycloalkane rings that are joined to each other. Examples of steroids include the dietary fat cholesterol, the sex hormones estradiol and testosterone, and the anti-inflammatory drug dexamethasone.The core...
s- DexamethasoneDexamethasoneDexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs. It acts as an anti-inflammatory and immunosuppressant...
given in low dose at the onset of a general anaesthetic is an effective anti-emetic. The specific mechanism of action is not fully understood.
- Dexamethasone
- Other
- TrimethobenzamideTrimethobenzamideTrimethobenzamide is an antiemetic used to prevent nausea and vomiting. It is often prescribed for patients with gastroenteritis, medication-induced nausea, and other illnesses...
; thought to work on the CTZChemoreceptor trigger zoneThe chemoreceptor trigger zone , is an area of the medulla that receives inputs from blood-borne drugs or hormones, and communicates with the vomiting center, to initiate vomiting. The CTZ is close to the area postrema on the floor of the fourth ventricle and is outside of the blood-brain barrier... - GingerGingerGinger is the rhizome of the plant Zingiber officinale, consumed as a delicacy, medicine, or spice. It lends its name to its genus and family . Other notable members of this plant family are turmeric, cardamom, and galangal....
- contains 5HT3 antagonists gingerols and shogaols. - EmetrolEmetrolEmetrol is the brand name of an over-the-counter upset stomach medicine taken to relieve nausea and vomiting. Made by WellSpring Pharmaceutical Corporation, it was formerly distributed by McNeil Consumer Healthcare....
also claimed to be an effective antiemetic. - PropofolPropofolPropofol is a short-acting, intravenously administered hypnotic agent. Its uses include the induction and maintenance of general anesthesia, sedation for mechanically ventilated adults, and procedural sedation. Propofol is also commonly used in veterinary medicine...
given intravenously. It has been used in an acute care setting in hospital as a rescue therapy for emesis. - PeppermintPeppermintPeppermint is a hybrid mint, a cross between the watermint and spearmint . The plant, indigenous to Europe, is now widespread in cultivation throughout all regions of the world...
claimed to help nausea or stomach pain when added into a tea or peppermint candies. - MuscimolMuscimolMuscimol is the major psychoactive alkaloid present in many mushrooms of the Amanita genus. Unlike psilocin , which is a serotonergic psychedelic and agonist for the 5-HT2A receptor set, muscimol is a potent, selective agonist for the GABAA receptor set and is a deliriant as a opposed...
purported as such. - AjwainAjwainTrachyspermum ammi, commonly known as ajowan, bishop's weed, ajwain, ajowan caraway, carom seeds, or thymol seeds, is a plant of India and the Near East whose seeds are used as a spice.-Characteristics:...
purported to be antiemetic. It is a popular spice in IndiaIndiaIndia , officially the Republic of India , is a country in South Asia. It is the seventh-largest country by geographical area, the second-most populous country with over 1.2 billion people, and the most populous democracy in the world...
, EthiopiaEthiopiaEthiopia , officially known as the Federal Democratic Republic of Ethiopia, is a country located in the Horn of Africa. It is the second-most populous nation in Africa, with over 82 million inhabitants, and the tenth-largest by area, occupying 1,100,000 km2...
and EritreaEritreaEritrea , officially the State of Eritrea, is a country in the Horn of Africa. Eritrea derives it's name from the Greek word Erethria, meaning 'red land'. The capital is Asmara. It is bordered by Sudan in the west, Ethiopia in the south, and Djibouti in the southeast...
.
- Trimethobenzamide
- Non-pharmaceutical therapies with some evidence of efficacy include acupunctureAcupunctureAcupuncture is a type of alternative medicine that treats patients by insertion and manipulation of solid, generally thin needles in the body....
and hypnosisHypnosisHypnosis is "a trance state characterized by extreme suggestibility, relaxation and heightened imagination."It is a mental state or imaginative role-enactment . It is usually induced by a procedure known as a hypnotic induction, which is commonly composed of a long series of preliminary...
.
See also
- Emetic
- Hyperemesis gravidarumHyperemesis gravidarumHyperemesis gravidarum is a severe form of morning sickness, with "unrelenting, excessive pregnancy-related nausea and/or vomiting that prevents adequate intake of food and fluids." Hyperemesis is considered a rare complication of pregnancy but, because nausea and vomiting during pregnancy exist...
- ChemotherapyChemotherapyChemotherapy is the treatment of cancer with an antineoplastic drug or with a combination of such drugs into a standardized treatment regimen....