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17 recordsLinked to original sources
PubMed1978

Thiethylperazine; clinical antipsychotic efficacy and correlation with potency in predictive systems.

A one-to-one relationship between clinical antipsychotic potency and pharmacologic dopaminergic antagonism is implicit in the dopamine hypothesis of neuroleptic action. Thiethylperazine maleate, a classical antiemetic phenothiazine, displays dopaminergic antagonism in behavioral, neurochemical, and neuroendocrine systems, but is paradoxical insofar as it is thought not to possess clinical neuroleptic activity. In three tests of dopaminergic antagonism--elevation of levels of CSF homovanillic acid in monkeys, striatal dihydroxyphenylacetic acid in rats, and prolactin in man--as well as in a clinical trial of neuroleptic efficacy in schizophrenics, thiethylperazine was fully active and approximately three times as potent as chlorpromazine. Differences in efficacy between this and earlier clinical studies can be accounted for on the basis of dosage.

3,4-Dihydroxyphenylacetic Acid↗
PubMed1978

A comparative study of the effects of cinnarizine, sulpiride and thiethylperazine on vestibular nystagmus in rabbits.

The effects of cinnarizine, sulpiride, thiethylperazine and a placebo on vestibular nystagmus in rabbits were investigated. The nystagmus was provoked by means of a torsion swing. A suppressive effect was shown by all drugs and not by the placebo. A fast and strong effect was seen after the administration of sulpiride, however this effect decreased after 1 h. The onset of the effect of cinnarizine was slower but the effect lasted longer. Thiethylperazine had a clear suppressive effect but less strong and shorter than that of the other two drugs.

Animals↗
PubMed1978

Comparative investigation between thiethylperazine and meclizine in vertigo of different genesis.

Forty patients suffering from vertigo of different genesis received thiethylperazine 6.5 mg or meclizine 25 mg, 2 capsules a day for 5 days, according to double-blind, cross-over methodology in randomized order. It appeared that the effect on the symptoms vertigo, gait disturbance and nausea does not differ significantly for the two preparations. On the other hand, an almost significant effect on vertigo, and, to a smaller degree, on gait disturbances, was obtained during the second period of treatment, independent of administered preparation. Side-effects in the form of fatigue and headache occur to the same extent after both preparations. Meclizine should be an alternative to thiethylperazine in the treatment of vertigo, especially in patients who might risk chronic dyskinesia in long-term treatment.

Adult↗
PubMed1979

Control of radiation-induced emesis with promethazine, cimetidine, thiethylperazine, or naloxone.

Promethazine (2 mg/kg), cimetidine (4 mg/kg), thiethylperazine (0.86 mg/kg), and naloxone (0.08 mg/kg) were each evaluated for their ability to increase the threshold of radiation-induced emesis in the dog. Each dog was fed a can of dog food (ca 0.4 kg) and then injected IM with the appropriate drug 1 hour before being irradiated by a 60Co teletherapy unit. The total radiation dose given an individual dog was determined by an up-and-down exposure schedule. Dogs were then observed continuously for 10 hours while the number, time of onset, and duration of each emetic episode were monitored. The dose of radiation causing emesis in 50% (ED50 +/- SEM) of control dogs was 170 +/- 38.5 rad. The ED50 +/- SEM was increased to 402 +/- 18.6 rad by promethazine, to 331 +/- 27.3 rad by cimetidine, and to 320 +/- 38.5 rad by thiethylperazine. This increased tolerance was significant at P less than 0.05 for each drug. The ED50 for naloxone was 262.5 +/- 92.9 rad, which was not a statistically significant increase in threshold.

Animals↗
PubMed1977

The interaction between clonidine and various neuroleptic agents and some benzodiazepine tranquillizers.

The central hypotensive action of clonidine, infused into the vertebral artery of chloralose-anaesthetized cats was antagonized by several phenothiazine-neuroleptics (chlorpromazine, promazine, promethazine, thiethylperazine, thioridazine), by chlorprothixene and to a limited extent by haloperidol administered via the same route. Pimozide and some benzodiazepines (chlordiazepoxide, diazepam and flurazepam) hardly influenced the central hypotensive response to clonidine. The antagonism between clonidine and the psychotropic drugs is probably associated with central alpha-adrenoceptors, clonidine being the agonist and the neuroleptic agents the antagonists at these receptors. Virtually the same type of antagonism was observed in conscious, spontaneously hypertensive rats where both clonidine and the neuroleptic drugs were injected intravenously. The phenothiazines and also piperoxane effectively diminished the centrally induced hypotensive response to clonidine, whereas the initial pressor effect to clonidine was not reduced.

Anesthesia↗
PubMedDate not supplied

Migraine and drug absorption.

The majority of migraine attacks are associated with gastrointestinal symptoms which add considerably to the distress and inconvenience caused by the headache. When salicylate absorption from effervescent aspirin tablets was studied during migraine, the rate of absorption was found to be reduced relative to that found in non-migrainous volunteers and in the same patients when headache-free. There is evidence that this reduced rate of absorption is caused by gastrointestinal stasis and reduced rate of gastric emptying. Patients in whom aspirin absorption was delayed were more likely to take longer to respond and to require additional treatment. Metoclopramide, which increases gastric emptying rate, has been shown to improve the rate of absorption of aspirin during migraine and also increase the rate of recovery from the attack and avoid the need for additional treatment; effects which were not shown by thiethylperazine. It is likely that delayed absorption during migraine affects some drugs other than aspirin, such as ergotamine, and it is therefore recommended that the most rapidly absorbable formulation should be used. If such treatment is ineffective, metoclopramide may be a useful addition and should be tried before resorting to other routes of administration.

Aspirin↗
PubMed1975

Phenothiazine drugs: structure-activity relationships explained by a conformation that mimics dopamine.

The antischizophrenic activity of phenothiazine drugs and their tendency to elicit extrapyramidal symptoms are thought to involve blockade of synaptic dopamine receptors in the brain. Space filling molecular models show how favorable Van der Waal's interactions between the side chain amino of phenothiazines and the 2-substituent on ring A can promote a conformation mimicking dopamine. These Van der Waal's attractive forces can expain (i) the greater potency of drugs with trifluoromethyl rather than chlorine as a 2-substituent; (ii) the enhanced activity of phenothiazines with piperazine instead of alkylamino side chains; (iii) the increased potency associated with hydroxyethylpiperazines as contrasted to piperazine side chains; (iv) the greater potency of cis rather than trans thioxanthenes; and (v) the crucial location of the ring A substituent at carbon no. 2. Potential energy calculations support the observations with molecular models and suggest an active conformation for the phenothiazines.

Antipsychotic Agents↗
PubMed1975

Dopamine receptor blockade and the neuroleptics, a crystallographic study.

The X-ray structures of 12 drugs of the tricyclic class having varying pharmacological profiles have been examined in detail in an attempt to rationalize the known structure-activity relations of neuroleptic drugs with respect to their ability to block dopamine receptors in the brain. Further evidence is presented in support of the theory that the neuroleptics are able to block dopamine receptors because of a conformational complementarity between certain portions of these drugs and dopamine.

Chlorpromazine↗
PubMed1979

The effects of some drugs on the caloric induced nystagmus.

A striking difference between the two anticholinergic drugs was observed. Atropine only modified the eye speed of the slow phase (mes), whereas scopolamine modified both parameters measured, mes and duration. Amphetamine and caffeine prolonged the duration, leaving the mes unchanged. All antiemetic drugs inhibited both parameters. It is concluded that the effect of a drug on the caloric reaction gives insufficient information in the preclinical evaluation of vestibulo-suppressive drugs.

Amphetamine↗