Hepatitis following the administration of trimethobenzamide hydrochloride.
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Benzamides↗
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Possible explanation for trimethobenzamide cross-reaction in immunoassays of amphetamine/methamphetamine.
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Amphetamine↗
Trimethobenzamide cross-reacts in immunoassays of amphetamine/methamphetamine.
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Amphetamine↗
Chin rub CRs may reflect conditioned sickness elicited by a lithium-paired sucrose solution.
Rats were given a single conditioning trial in which 20% sucrose solution was paired with an intraperitoneal (IP) injection of lithium chloride (127.2 mg/kg), d-amphetamine (3 mg/kg) or physiological saline. Thirty min before a subsequent 10-min taste reactivity (TR) test and a 1-h conditioned taste avoidance (CTA) test the rats were injected IP with either the antiemetic agent, trimethobenzamide (5 mg/kg) [corrected] or with physiological saline solution. The lithium-paired, but not the amphetamine- or saline-paired, sucrose solution elicited the aversive TR responses of chin rubs, paw pushes and gapes. Trimethobenzamide suppressed the aversive TR response of chin rubs in the lithium-conditioned group, but not in a group given unconditionally aversive quinine solution. The CTA test was not sensitive to the antiemetic properties of trimethobenzamide, although the drug enhanced sucrose preference overall. The results suggest that chin rub responses may measure conditioned sickness.
Animals↗
Effect of drug therapy on compensation from vestibular injury.
The influence of selected drugs on compensation from unilateral labyrinthectomy was studied in the cat. The drugs investigated included: a. amphetamine, b. diazepam, c. dimenhydrinate, d. scopolamine, and e. trimethobenzamide. The most beneficial drugs for improving recovery were a stimulant (amphetamine) and a general anti-emetic (trimethobenzamide). It is postulated they had this effect by improving the overall activity level with general exercise being a known positive influence. Conversely the other drugs either had little effect on recovery or hindered it, by presumably suppressing the sensory imbalance in the vestibular system that is essential stimulus to ultimate recovery.
Amphetamine↗
Effects of antiemetic drugs on glucose 6-phosphate dehydrogenase and some antioxidant enzymes.
The aim of this study was to investigate effect of antiemetics on G6PD and antioxidant enzymes. Antiemetics are currently being used to reduce or prevent nausea and vomiting in patients. This is the first study to show effect of antiemetics on glucose-6-phosphate dehydrogenase (G6PD) and antioxidant enzyme activities. For in vitro studies, G6PD was purified from human erythrocyte, 10, 26-fold in a yield of 51.3% by using ammonium sulphate precipitation and 2',5'-ADP-Sepharose 4B affinity gel. The purified enzyme showed a single band on sodium dodecyl sulfate-polyacrilamide gel electrophoresis (SDS-PAGE). The effects of four different antiemetics (granisetron hydrochloride, ondansetron hydrochloride, metoclopramide hydrochloride, trimethobenzamide hydrochloride) were investigated on the purified enzyme. Granisetron hydrochloride and ondansetron hydrochloride inhibited the enzyme activity (Ki values; 5.05 mM and 0.034 mM, I50 values; 3.9 mM and 0.036 mM, respectively). Metoclopramide hydrochloride, trimethobenzamide hydrochloride showed no inhibition effects. In addition, in vivo studies, effects of ondansetron hydrochloride on the G6PD, glutathione reductase (GR), glutathione peroxidase (GPx) and catalase (CAT) were examined in the rat erythrocytes. G6PD (49% of control), GR (55% of control), CAT (60% of control) activities in erythrocytes were significantly decreased whereas GPx (183% of control) was significantly increased. A marked alteration in these enzymes may be result of oxidative stress in the rats receiving ondansetron hydrochloride.
Animals↗
Intranasal apomorphine rescue therapy for parkinsonian "off" periods.
Eleven patients with levodopa-related motor fluctuations were scored before and after intranasal apomorphine monotherapy, and the motor responses were compared with those with levodopa/carbidopa in this openlabel study. Oral trimethobenzamide was used to prevent apomorphine-induced nausea. Three measures of motor performance were employed: (a) the Unified Parkinson's Disease Rating Scale (UPDRS) motor battery; (b) a timed hand-tapping test; and (c) the Webster's step-seconds test. The magnitude of the motor-score improvement after apomorphine administration was very similar to that after the usual doses of levodopa/carbidopa in the 10 patients completing the study; this was true for all three outcome measures. A major advantage of apomorphine was the rapid onset of clinical response, which typically occurred in < 10 min, as well as the ease of administration. Major side effects, beyond those experienced with levodopa/carbidopa, were limited to nausea and vomiting (three patients) and orthostatic hypotension (one patient); however, only a single patient dropped out of the study as a consequence. These results indicate that intranasal apomorphine is effective in rapidly relieving parkinsonian "off" states and that, for most patients, trimethobenzamide is an effective and well-tolerated antiemetic for use with apomorphine.
Administration, Intranasal↗
Stress modification of the toxicity of antimotion sickness drugs and aspirin.
The effect of environmental temperature on the toxicity of cyclizine, trimethobenzamide, and Aspirin were studied in mice. LD50s were compared at 30 degrees C (warm), 22 degrees C (normal), and 15 degrees C (cool). At 30 degrees C the toxicity of all three drugs increased, with that to aspirin being affected most. Cooling decreased the toxicity of cyclizine and had no significant effect on that of trimethobenzamide or Aspirin. These findings indicate that alterations in environmental temperature markedly affect drug toxicity. They emphasize that such alterations, and particularly increases in temperature, do not have to be particularly drastic, but that "mild' variations in the environment are effective in altering an animal's sensitivity to a drug.
Animals↗
A double-blind, placebo-controlled study of intranasal apomorphine spray as a rescue agent for off-states in Parkinson's disease.
Nine patients with advanced levodopa-responsive Parkinson's disease were enrolled in a double-blind, placebo-controlled crossover trial of intranasal apomorphine as rescue therapy for parkinsonian off-states. Patients were assigned in random order to each of four possible combinations of apomorphine, trimethobenzamide antiemetic, and their matched placebos and received detailed in-office motor scoring during each of the four study periods. Patients also completed diaries describing the effectiveness of the nasal spray for reversing off-states. A statistically significant reduction in the Unified Parkinson's Disease Rating Scale (UPDRS) motor score was seen following active apomorphine during in-office evaluation visits but not following placebo nasal spray. Patient diaries revealed that active apomorphine had a latency to onset of 11 minutes and a duration of 50 minutes. Significant nausea from apomorphine spray was seen in only one patient whereas nasal irritation was disabling in three and mild in two. We conclude that intranasal apomorphine is an effective rescue agent for parkinsonian off-states although nasal irritation is a limiting factor.
Administration, Intranasal↗
The attenuation of a specific cue-to-consequence association by antiemetic agents.
Previous research has been shown that rats develop a conditioned taste aversion after a single pairing of a distinct taste and subsequent toxicosis. The experiments reported here test the hypothesis that the expression of a taste aversion may reflect classically conditioned nausea mediated by activation of brainstem emetic centers by taste stimuli. Rats were allowed to drink a saccharin solution (1 g/l) and 10 min later were intubated with LiCl (180 mg/kg) to produce nausea. When control rats were posttested for saccharin preference they consumed less than 50% of their pretest intake. Experimental rats were injected with one of four pharmacologically distinct antiemetic drugs 30 min prior to their posttest with saccharin. Each drug significantly attenuated the aversion to saccharin at one dose level. The antiemetic drugs we used were scopolamine HBr, cyclizine, prochlorperazine dimaleate, and trimethobenzamide. These drugs had no effect on the conditioned fear of a noise that signaled foot shock or on a natural aversion to a bitter fluid (quinine monohydrochloride, 100 mg/l). Our data suggest that pharmacological suppression of the neural mechanisms of emesis selectively disrupts conditioned taste aversions, and that moderate dose levels are critical for obtaining this effect.
Animals↗
An evaluation of the teratogenicity of certain antinauseant drugs.
In a large, prospective, observational study of pregnancy and child development, the antinauseant drugs prescribed to gravides for nausea and vomiting in the first 84 days of pregnancy were evaluated for their teratogenic potential. The severe congenital anomaly rates per 100 liveborn children and ther perinatal death rates of this group did not differ from the rates of the group with untreated nausea and vomiting. There was no indication that the phenothiazine derivatives, specifically the prochlorperazine derivative, as well as meclizine, cylizine, and Bendectin were associated with teratogenicity. The trimethobenzamide drug gave a slight suggestion of an excess of severe congenital anomalies.
Abnormalities, Drug-Induced↗
RU 24969-induced emesis in the cat: 5-HT1 sites other than 5-HT1A, 5-HT1B or 5-HT1C implicated.
RU 24969 was administered s.c. to cats and found to elicit emesis with a maximally effective dose of 1.0 mg/kg. 5-Methoxytryptamine was found to have lower efficacy and to produce a higher incidence of non-specific effects while trifluoromethylphenylpiperizine (TFMPP) was devoid of emetic effects. The emesis elicited by 1.0 mg/kg of RU 24969 was not altered by pretreatment with phentolamine, haloperidol, yohimbine or (-)-propranolol, indicating that catecholamines played no role in this response. The emesis was prevented by metergoline and methysergide but not by ketanserin, cyproheptadine, mesulergine, ICS 205,930, methiothepin, trimethobenzamide or BMY 7378. An indirect argument is presented that implicates a role for 5-HT1D sites. This conclusion must remain tentative until drugs selective for this site are synthesized and tested. The emesis was also prevented by 8-hydroxy-2-(di-n-propylamine)tetralin (8-OH-DPAT), confirming that this drug has a general antiemetic effect in cats.
8-Hydroxy-2-(di-n-propylamino)tetralin↗
Does a learned taste aversion contribute to the anorectic effect of bacterial lipopolysaccharide?
The present study addressed the possible role of a conditioned taste aversion in the anorectic effect of bacterial lipopolysaccharide (LPS) in the rat. Pairing an intraperitoneal (IP) injection of LPS (100 micrograms/kg b.wt.) with the subsequent presentation of a familiar diet (FD) or of a novel-tasting saccharin diet (SD) for several hours did not affect FD or SD intake when the same diet was offered several days later after 12 h of food deprivation. However, food intake during the second presentation of SD was reduced when food was not withheld prior to the test. In a similarly designed experiment, the antipyretic and antiinflammatory drug indomethacin (5 mg/kg b.wt., IP) attenuated the anorectic effect of LPS during the initial pairing, but did not affect the inhibition of SD intake in LPS-pretreated rats during the second feeding test. The antiemetic trimethobenzamide (5 mg/kg b.wt., IP) failed to influence the anorectic effect of LPS. Lesion of the area postrema (AP) and the adjacent nucleus of the solitary tract (NST) was found to enhance the anorectic effect of LPS, but the development of tolerance to this effect remained unchanged in AP/NST-lesioned animals. In spite of the ability of LPS to induce a taste aversion that inhibits feeding under certain conditions (novel-tasting diet, no food deprivation prior to the feeding test), the findings indicate that a learned taste aversion is not the only contributor to the anorectic effect of LPS.
Animals↗
Effects of antiemetics on the acquisition and recall of radiation- and lithium chloride-induced conditioned taste aversions.
A series of experiments were run to evaluate the effect of antiemetics on the acquisition and recall of a conditioned taste aversion induced by exposure to ionizing radiation or by injection of lithium chloride. Groups of male rats were exposed to 100 rad gamma radiation or 3 mEq/kg lithium chloride following consumption of a 10% sucrose solution. They were then injected with saline or with one of three antiemetics (prochlorperazine, trimethobenzamide, or cyclizine) at dose levels that have been reported to be effective in attenuating a previously acquired lithium chloride-induced taste aversion. The pretreatments with antiemetics had no effect on the acquisition or recall of either the lithium chloride- or radiation-induced taste aversion. The data suggest that antiemetics do not disrupt lithium chloride-induced taste aversions as previously reported, nor do they effect radiation-induced taste aversion learning.
Animals↗
Neuroleptic-like properties of cholecystokinin analogs: distinctive mechanisms underlying similar behavioral profiles depending on the route of administration.
Rats were trained to discriminate vehicle injections from intraperitoneal injections of 3 micrograms/kg caerulein, a cholecystokinin (CCK) neuropeptide analog. The reward that reinforced correct choices was an electrical brain stimulation self-administered by bar pressing. Dose-response quantitative generalization was obtained by using 1 and 2 micrograms/kg caerulein. Qualitative generalization to the vehicle occurred after injecting 10, 20 and 200 micrograms/kg unsulfated CCK-8, 10, 20 and 200 micrograms/kg CCK-4, 5 micrograms/kg CCK-8 and 1 microgram/kg caerulein, neurotensin or bombesin and 200 micrograms/kg apomorphine or 320 micrograms/kg amphetamine. Total generalization to the caerulein cue was obtained with 20 micrograms/kg sulfated CCK-8 or gastrin 2-17, 25 micrograms/kg somatostatin, 50 micrograms/kg haloperidol and 2 mg/kg chlorpromazine. The previous 5 mg/kg injection of an antiemetic drug such as chlorhydrate of trimethobenzamide did not eliminate the discriminative properties of a subsequent injection of caerulein. Our data thus tend to show that IP injection of caerulein produces effects similar to those of IP neuroleptics.
Animals↗
Spectrophotometric determination of some pharmaceutical amides through charge-transfer complexation reactions.
A spectrophotometric method is described for the assay of fenpipramide hydrochloride, isopropamide iodide, trimethobenzamide hydrochloride, morphazinamide hydrochloride and tolazamide. The method is based on the formation of a charge-transfer complex between the drug as n-donor and iodine, a sigma-acceptor. The product exhibits absorption maxima at 295 and 365 nm; measurements are made at 365 nm for fenpipramide and at 295 nm for the other compounds. Beer's law is obeyed in a concentration range of 1-120 micrograms ml-1. The method is rapid, simple and sensitive and can be applied to the analysis of some commercial and laboratory prepared tablets without interference. A more detailed investigation of the complex was made with respect to its composition, association constant and free energy change.
Amides↗
Antiemetic inhibits conditioned taste aversion, but not the hypophagia induced by epinephrine.
It has been shown that relatively high doses of epinephrine (E) injected intraperitoneally (IP) produce hypophagia and conditioned taste aversion (CTA) in rats. We examined the possibility that E effects involve malaise. For this purpose, changes in saccharin preference induced by E injected IP (100 microg/kg) were determined after a previous administration of trimethobenzamide (TMB, 5 mg/kg), an antiemetic agent. E alone decreased saccharin preference by 54% (p < 0.01), but only by 16% (not significant) in the presence of TMB. In contrast, the injection of 75 or 100 microg/kg E reduced food intake by 50 and 85%, respectively (p < 0.01), regardless of previous injection of TMB. In conclusion, the results suggest that E-induced malaise is not the direct cause of the hypophagia it elicits.
Animals↗
Prescription medication use during pregnancy and risk of infant leukemia (United States).
OBJECTIVE: We explored whether maternal medication use during pregnancy may be an important etiologic area for investigation in studies of infant leukemia. METHODS: In this case-control study, associations were explored between specific medications as recorded in the medical records of 243 mothers of infants who were diagnosed with leukemia at < 18 months of age and 393 mothers ol infants without leukemia identified through random digit dialing. Cases included 157 acute lymphoblastic (ALL), 77 acute myeloid (AML), and nine other leukemias. A total of 27 different drugs that were prescribed for at least six women were analyzed. RESULTS: Overall, non-statistically significant negative associations (Odds ratios, OR < 0.5) were observed with amoxicillin, nystatin, clomiphene, levothyroxine, cefaclor, and trimethobenzamide HCL. When cases were restricted to either myeloid or lymphoblastic leukemia, cotrimoxazole was prescribed for five ALL case mothers and no matched controls; no association with cotrimoxazole was observed with AML. CONCLUSIONS: Given the number of comparisons, chance cannot be ruled out for any of the associations found here. However, a strength of this study is the lack of recall bias. The disparate data observed between AML and ALL in some instances may indicate areas of interest; they will be explored further in a case-control study of infant leukemia that is currently underway.
Case-Control Studies↗