Prochlorperazine
Nausea
Betahistine
Granisetron
Ondansetron
Chlorpromazine
Granisetron (Kytril) suppresses methotrexate-induced nausea and vomiting among patients with inflammatory arthritis and is superior to prochlorperazine (Stemetil). (1/51)
OBJECTIVE: Methotrexate (MTX) is an increasingly popular anti-rheumatic drug with its usefulness limited by toxicity, most commonly gastrointestinal (GI). The aim of the study was to study the effectiveness of the 5-HT3 receptor antagonist granisetron (GR) in the therapy of MTX-induced nausea. METHODS: A single-blind 8 week pilot study with random allocation to either GR 1 mg or prochlorperazine (Stemetil; PCh) 10 mg was undertaken in 13 patients who were taking or had taken MTX for either rheumatoid arthritis (10) or psoriatic arthritis (3). RESULTS: One in six patients treated with PCh completed the 8 week study compared to 7/7 treated with GR. After switching of symptomatic patients, 11 completed the study on GR and median improvement was by two grades (P < 0.001) with a significantly better visual analogue scale score for patient satisfaction compared to PCh. CONCLUSION: Treatment with GR may be useful in establishing and maintaining some patients on MTX where GI toxicity would have precluded such therapy. (+info)Modification of the pharmacokinetics of high-dose cyclophosphamide and cisplatin by antiemetics. (2/51)
Interpatient variability in exposure to certain chemotherapy agents can influence patient outcome, particularly with high-dose chemotherapy. We evaluated the possibility of a pharmacokinetic (PK) drug-drug interaction between the antiemetic agents and high-dose cyclophosphamide, cisplatin and BCNU (CPA/cDDP/BCNU). Twenty-three self-selected patients treated with high-dose CPA/cDDP/BCNU followed by autologous hematopoietic progenitor cell support (AHPCS) received ondansetron, lorazepam and diphenhydramine as antiemetics. PK parameters for each chemotherapeutic drug in the regimen were compared with those of 129 patients who received exactly the same chemotherapy but an antiemetic regimen substituting prochlorperazine for ondansetron. In addition, we performed a review of the English literature for reported drug-drug interactions between antiemetics and chemotherapy agents that led to modifications in any PK parameters of the chemotherapy agent. Our retrospective study showed that the mean area under the curve (AUC) for both cyclophosphamide (76,600 vs 90,600 microg/ml/min, P=0.001) and cisplatin (525 vs 648 microg/ml/min, P = 0.01) were significantly lower in the ondansetron group when compared with the prochlorperazine group. The AUC for BCNU was not significantly different in both groups (544 vs 677, P = 0.43). We found only one report of modifications of the PK parameters of high-dose chemotherapy agents due to drug-drug interactions with the most commonly used antiemetics in a review of the English literature between 1966 and 1995. We concluded that the AUC of high-dose cyclophosphamide and cisplatin are significantly lower when ondansetron, as opposed to prochlorperazine, is used as the antiemetic. The small sample size and heterogeneity of this group of patients precludes any outcome analysis of pharmacodynamic endpoints such as toxicity or antitumor effect. Nevertheless, the potential for interactions between antiemetics and chemotherapy agents should be taken into account when using different high-dose chemotherapy regimens. (+info)Synergistic effect of prochlorperazine and dipyridamole on the cellular retention and cytotoxicity of doxorubicin. (3/51)
Incubation of drug-resistant human tumor cells with a combination of prochlorperazine and dipyridamole has additive/synergistic effect on the cellular retention and cytotoxicity of doxorubicin. In patients administered a fixed dose of doxorubicin and prochlorperazine with escalating doses of dipyridamole, mean plasma levels of dipyridamole and prochlorperazine achieved were as high as 3.01 +/- 0.41 microm and 0.94 +/- 0.09 microm, respectively. Plasma samples from patients were analyzed in an in vitro assay to monitor the effect on the cellular retention of tritium-labeled daunorubicin in MDR1-transfected P388 cells. In 22 of 49 of the plasma samples analyzed, the daunorubicin in efflux blocking activity was one-half or greater than that of cells incubated with 12.5 microM verapamil, a well-known efflux blocker. These observations suggest that a combination of prochlorperazine and dipyridamole may enhance cellular doxorubicin retention by blocking efflux while reducing normal tissue toxicity and unwanted side effects in vivo. (+info)Oral granisetron for the prevention of acute late onset nausea and vomiting in patients treated with moderately emetogenic chemotherapy. (4/51)
PURPOSE: To demonstrate the efficacy of oral granisetron 1 mg twice daily for the prevention of late onset nausea and vomiting after moderately emetogenic chemotherapy that includes cyclophosphamide, carboplatin, or doxorubicin. METHODS: Prior to chemotherapy, patients were stratified by gender and randomized to receive oral granisetron (1 mg tablet twice daily) or prochlorperazine (10 mg sustained release capsule twice daily). Study agents were administered 1 h prior to and 12 h after chemotherapy. Antiemetics were administered for seven consecutive days. Efficacy variables were assessed 48 and 72 h after administration of chemotherapy, and included no emesis, no nausea, no moderate or severe nausea, and no antiemetic rescue. Safety analysis included all patients who received medication. RESULTS: A total of 230 patients were included in the intent-to-treat analysis; 119 patients received granisetron and 111 patients received prochlorperazine. Females, and all patients combined, who received granisetron had significantly higher no-emesis rates at 48 h (p =.010 and p =.016, respectively) than patients who received prochlorperazine. No-nausea rates at 48 h were numerically higher for all patients combined and females who received granisetron rather than prochlorperazine. Response rates for no nausea or mild nausea were also numerically higher in females treated with granisetron, compared to prochlorperazine, at 48 h. Significantly more patients (p <.001) and females (p <.001) in the granisetron group than in the prochlorperazine group did not require rescue antiemetics at 48 h. At 72 h, efficacy results were comparable for granisetron and prochlorperazine. CONCLUSION: Oral granisetron is well tolerated and more effective than prochlorperazine in preventing nausea and vomiting for up to 48 h following treatment with moderately emetogenic chemotherapy. (+info)ANTI-EMETIC ACTIVITY OF PHENOTHIAZINES IN RELATION TO THEIR CHEMICAL STRUCTURE. (5/51)
Twelve phenothiazine derivatives have been studied for anti-emetic potency in dogs against emesis induced by apomorphine. The PD(50)s of all the compounds were determined and the activities compared with chlorpromazine hydrochloride as standard. Thioproperazine methanesulphonate was 300 times more active than chlorpromazine hydrochloride and twice as active as perphenazine sodium citrate. The anti-emetic activity of the compounds has been correlated with their chemical structure. (+info)TRANQUILLIZING AND HYPOTENSIVE ACTIVITIES OF TWELVE PHENOTHIAZINES. (6/51)
Twelve phenothiazine derivatives have been compared in relation to their central sedative, tranquillizing and hypotensive activities. The ED50's of the compounds to suppress the conditioned response, unconditioned response and forced locomotor activity were determined. Suppressions of the conditioned and unconditioned responses were taken as criteria for tranquillizing and central sedative activities respectively. The "tranquillizing ratio" (ED50 for unconditioned response/ED50 for conditioned response) was used as the criterion of tranquillizing activity in relation to sedative activity and for purposes of comparison this ratio was assigned a value of unity for chlorpromazine. Perphenazine was the most potent drug in suppressing the conditioned and unconditioned responses whereas fluopromazine had the maximal "tranquillizing index" activity. Six compounds had great, three moderate and three mild hypotensive activity when doses of 1 mg/kg were injected intravenously into dogs. The relationship of the chemical structure to the central sedative activity is discussed. (+info)THE EFFECT OF SOME PHENOTHIAZINE TRANQUILLIZERS ON THE OESTROUS CYCLE OF ALBINO MICE. (7/51)
The effects of reserpine and of nine phenothiazine compounds on the oestrous cycle of albino mice were tested. With the exception of promethazine (which is not a tranquillizer) all the phenothiazine compounds and reserpine prolonged the oestrous cycle. The mechanism by which these tranquillizers interfere with the oestrous cycle is discussed. (+info)PROMAZINE AND MEPERIDINE (SPARIDOL 50), AN EFFICIENT COMBINATION FOR PREOPERATIVE MEDICATION. (8/51)
A number of elderly patients undergoing intraocular surgery were premedicated with a combination of promazine 50 mg. and meperidine 50 mg. Superior sedation and a smoother postoperative course were noted as compared to a control group premedicated with the usual high dosages of opiates and barbiturates. The incidence of nausea and vomiting, urinary retention, and postoperative disorientation was less than 20%. Hypotension was not a problem.Promazine was found to potentiate the action of opiates and barbiturates given in smaller dosages, thus permitting surgical procedures to be carried out with safety in an older population prone to the complications of opiate and barbiturate administration. This finding confirms reports noted in the obstetrical literature. (+info)Prochlorperazine is an antipsychotic drug, specifically a phenothiazine derivative. It works by blocking dopamine receptors in the brain, which helps to reduce psychotic symptoms such as hallucinations and delusions, and also has antiemetic (anti-nausea and vomiting) effects.
Prochlorperazine is used to treat various conditions, including:
* Schizophrenia and other psychotic disorders
* Nausea and vomiting, including motion sickness and postoperative nausea and vomiting
* Severe anxiety or agitation
* Tension headaches
The drug can be administered orally, intramuscularly, or rectally, depending on the formulation. Common side effects of prochlorperazine include drowsiness, dry mouth, blurred vision, and constipation. More serious side effects can include neurological symptoms such as tardive dyskinesia (involuntary movements), neuroleptic malignant syndrome (a life-threatening condition characterized by fever, muscle rigidity, and autonomic dysfunction), and seizures. Prochlorperazine should be used with caution in elderly patients, those with a history of seizures or cardiovascular disease, and those taking other medications that may interact with it.
Antiemetics are a class of medications that are used to prevent and treat nausea and vomiting. They work by blocking or reducing the activity of dopamine, serotonin, and other neurotransmitters in the brain that can trigger these symptoms. Antiemetics can be prescribed for a variety of conditions, including motion sickness, chemotherapy-induced nausea and vomiting, postoperative nausea and vomiting, and pregnancy-related morning sickness. Some common examples of antiemetic medications include ondansetron (Zofran), promethazine (Phenergan), and metoclopramide (Reglan).
Phenothiazines are a class of heterocyclic organic compounds that contain a phenothiazine nucleus, which consists of a pair of benzene rings fused to a thiazine ring. They have been widely used in medicine as antipsychotic drugs for the treatment of various mental disorders such as schizophrenia and bipolar disorder.
Phenothiazines work by blocking dopamine receptors in the brain, which helps to reduce the symptoms of psychosis such as hallucinations, delusions, and disordered thinking. They also have sedative and antiemetic (anti-nausea) effects. However, they can cause a range of side effects including extrapyramidal symptoms (involuntary muscle movements), tardive dyskinesia (irreversible movement disorder), and neuroleptic malignant syndrome (a rare but potentially fatal reaction to antipsychotic drugs).
Examples of phenothiazine drugs include chlorpromazine, thioridazine, and promethazine. While they have been largely replaced by newer atypical antipsychotics, phenothiazines are still used in some cases due to their lower cost and effectiveness in treating certain symptoms.
Nausea is a subjective, unpleasant sensation of discomfort in the stomach and upper gastrointestinal tract that may precede vomiting. It's often described as a feeling of queasiness or the need to vomit. Nausea can be caused by various factors, including motion sickness, pregnancy, gastrointestinal disorders, infections, certain medications, and emotional stress. While nausea is not a disease itself, it can be a symptom of an underlying medical condition that requires attention and treatment.
Betahistine is a medication that is primarily used to treat symptoms associated with Ménière's disease, which is an inner ear disorder that can cause vertigo (dizziness), tinnitus (ringing in the ears), and hearing loss. Betahistine is thought to work by improving blood flow in the inner ear and reducing the pressure in the fluid-filled compartments of the ear.
Betahistine is a histamine analogue, which means that it has a similar chemical structure to histamine, a naturally occurring compound in the body that plays a role in various physiological processes, including the regulation of blood flow and inflammation. Betahistine acts as an agonist at H1 and H3 histamine receptors and as an antagonist at H2 receptors, which leads to its therapeutic effects on the inner ear.
The medication is available in tablet form and is typically taken two or three times a day, with or without food. The dosage may vary depending on the individual's response to treatment and any underlying medical conditions. Common side effects of betahistine include gastrointestinal symptoms such as nausea, vomiting, and diarrhea, as well as headache, dizziness, and dry mouth.
It is important to note that betahistine may interact with other medications, including certain antidepressants, antihistamines, and sedatives, so it is essential to inform your healthcare provider of all the medications you are taking before starting treatment with betahistine. Additionally, individuals with asthma or a history of peptic ulcers should use caution when taking this medication, as it may exacerbate these conditions.
Vomiting is defined in medical terms as the forceful expulsion of stomach contents through the mouth. It is a violent, involuntary act that is usually accompanied by strong contractions of the abdominal muscles and retching. The body's vomiting reflex is typically triggered when the brain receives signals from the digestive system that something is amiss.
There are many potential causes of vomiting, including gastrointestinal infections, food poisoning, motion sickness, pregnancy, alcohol consumption, and certain medications or medical conditions. In some cases, vomiting can be a symptom of a more serious underlying condition, such as a brain injury, concussion, or chemical imbalance in the body.
Vomiting is generally not considered a serious medical emergency on its own, but it can lead to dehydration and other complications if left untreated. If vomiting persists for an extended period of time, or if it is accompanied by other concerning symptoms such as severe abdominal pain, fever, or difficulty breathing, it is important to seek medical attention promptly.
Granisetron is a medication that is primarily used to prevent nausea and vomiting caused by chemotherapy, radiation therapy, or surgery. It belongs to a class of drugs known as serotonin antagonists, which work by blocking the action of serotonin, a chemical in the brain that can trigger nausea and vomiting.
Granisetron is available in several forms, including oral tablets, oral solution, and injectable solutions. It is usually taken or administered about an hour before chemotherapy or radiation therapy, or shortly before surgery. The medication may also be given as needed to manage nausea and vomiting that occur after these treatments.
Common side effects of granisetron include headache, constipation, dizziness, and tiredness. In rare cases, it can cause more serious side effects such as irregular heartbeat, seizures, or allergic reactions. It is important to follow the dosage instructions carefully and inform your healthcare provider if you experience any unusual symptoms while taking granisetron.
Ondansetron is a medication that is primarily used to prevent nausea and vomiting caused by chemotherapy, radiation therapy, or surgery. It is a selective antagonist of 5-HT3 receptors, which are found in the brain and gut and play a role in triggering the vomiting reflex. By blocking these receptors, ondansetron helps to reduce the frequency and severity of nausea and vomiting.
The drug is available in various forms, including tablets, oral solution, and injection, and is typically administered 30 minutes before chemotherapy or surgery, and then every 8 to 12 hours as needed. Common side effects of ondansetron include headache, constipation, and diarrhea.
It's important to note that ondansetron should be used under the supervision of a healthcare provider, and its use may be contraindicated in certain individuals, such as those with a history of allergic reactions to the drug or who have certain heart conditions.
Metoclopramide is a medication that is primarily used to manage gastrointestinal disorders. It is classified as a dopamine antagonist and a prokinetic agent, which means it works by blocking the action of dopamine, a chemical in the brain that can slow down stomach and intestine function.
The medical definition of Metoclopramide is:
A synthetic congener of procainamide, used as an antiemetic and to increase gastrointestinal motility. It has a antidopaminergic action, binding to D2 receptors in the chemoreceptor trigger zone and stomach, and it may also block 5HT3 receptors at intrapyloric and central levels. Its actions on the gut smooth muscle are mediated via cholinergic muscarinic receptors. (Source: Dorland's Medical Dictionary)
Metoclopramide is commonly used to treat conditions such as gastroesophageal reflux disease (GERD), gastritis, and gastroparesis, which is a condition that affects the normal movement of food through the digestive tract. It can also be used to prevent nausea and vomiting caused by chemotherapy or radiation therapy.
Like any medication, Metoclopramide can have side effects, including drowsiness, restlessness, and muscle spasms. In some cases, it may cause more serious side effects such as tardive dyskinesia, a condition characterized by involuntary movements of the face, tongue, or limbs. It is important to use Metoclopramide only under the supervision of a healthcare provider and to follow their instructions carefully.
Chlorpromazine is a type of antipsychotic medication, also known as a phenothiazine. It works by blocking dopamine receptors in the brain, which helps to reduce the symptoms of psychosis such as hallucinations, delusions, and disordered thinking. Chlorpromazine is used to treat various mental health conditions including schizophrenia, bipolar disorder, and severe behavioral problems in children. It may also be used for the short-term management of severe anxiety or agitation, and to control nausea and vomiting.
Like all medications, chlorpromazine can have side effects, which can include drowsiness, dry mouth, blurred vision, constipation, weight gain, and sexual dysfunction. More serious side effects may include neurological symptoms such as tremors, rigidity, or abnormal movements, as well as cardiovascular problems such as low blood pressure or irregular heart rhythms. It is important for patients to be monitored closely by their healthcare provider while taking chlorpromazine, and to report any unusual symptoms or side effects promptly.