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PubMed1994

[Absolute bioavailability of chlorpromazine, promazine and promethazine].

The absolute bioavailability of the three phenothiazine neuroleptics, promazine (Sinophenin, CAS 58-40-2), chlorpromazine (Propaphenin, CAS 50-53-3) and promethazine (Prothazin, CAS 60-87-7) was tested in three single-dose cross-over studies. In each trial 12 to 14 healthy volunteers were enrolled. The single doses for promazine, promethazine and chlorpromazine were 100, 75 and 150 mg (orally) and 20, 50 and 50 mg (intravenously), resp. The serum concentrations of the three neuroleptics were measured by means of a selective HPLC-method. the distribution-free confidence intervals for the absolute bioavailability of the three phenothiazines were within 10.5 to 24.7% for chlorpromazine, 7.8 to 24.9% for promazine and 12.3 to 40% for promethazine. Promazine and chlorpromazine are pharmacokinetically very similar and differ substantially from promethazine.

Administration, Oral↗
PubMed1997

Interactions between promazine and antidepressants at the level of cellular distribution.

The pharmacokinetic interactions in clinical combinations of a phenothiazine neuroleptic and antidepressants at the level of cellular distribution were investigated. Uptake experiments were performed on slices of various rat tissues as a system with intact lysosomes. Promazine and antidepressants (imipramine, amitriptyline, sertraline, fluoxetine) were incubated separately or jointly with tissue slices for 1 hr. Initial concentration of each drug was 5 microM. The interaction studies were carried out in the absence and presence of ammonium chloride (20 mM), a lysosomotropic compound which increases the internal pH value of lysosomes. All the tissues known for their abundance of lysosomes (the lungs, liver, kidneys) were the site of an interaction between promazine and antidepressants. The neuroleptic and antidepressants mutually inhibited their tissue uptake. The potency of interference of each antidepressant with the lysosomal uptake of promazine was similar. The interactions did not occur in the presence of ammonium chloride, which indicates involvement of the lysosomal trapping. Carbamazepine, a lipophilic but non-lysosomotropic drug, did not interfere with the promazine uptake, and the adipose tissue containing very few lysosomes was never the site of interaction in our experiment. Distribution interactions were also observed in the brain and in some cases in muscles (the tissues less abundant of lysosomes), the effect of the inhibitory drug being usually more potent than that of ammonium chloride. Most of the interactions occurring in these two tissues were also observed in the presence of ammonium chloride. Most of the interactions occurring in these two tissues were also observed in the presence of ammonium chloride, which suggests involvement, at least partially, of a non-lysosomal trapping mechanism. The consequences of the observed distributive interactions at the level of lysosomal trapping in vitro are diminished intralysosomal concentration of the basic lipophilic psychotropic and its increase in cell membranes and fluids. In vivo, a shift from the organs or tissues rich in lysosomes to those less abundant in these organella, and an increase in the free drug concentration in body fluids may be expected. In conclusion, the obtained results show that, regardless of the previously known metabolic interactions between psychotropics, interactions at the levels of cellular and body distribution are also feasible.

1-Naphthylamine↗
PubMed1978

Effect of phenobarbitone and propionyl-promazine on serum enzymes in carbon-tetrachloride hepatotoxicity.

The influence of phenobarbitone givenin ten repeated doses simultaneously with small doses of CCl4 on serum enzymes was investigated in albino rats. The same experiment was repeated to investigate the influence of propionyl-promazine (phenothiazine derivative). The results proved that SGPT is a more specific and sensitive index than SGOT of hepato-cellular injury. The activity ratio between serum GOT and GPT in the normal control group was 2.44. The activity of SGPT increased nearly 6.1 fold after CCl4 administration and thus the activity ratio between GOT and GPT is sharply reduced to 0.56. The activity of serum GPT when CCl4 and phenobarbitone were administered together showed value of about 1/2 of the value when CCl4 was administered alone, while it remained high when CCl4 administration was combined with propionyl-promazine. Serum GOT and alkaline phosphatase increased significantly in all the groups. Regarding the pathological examination of the liver it was found that marked fatty necrosis could be demonstrated when high values of SGPT was found, which is not the case with serum GOT. It is concluded that in the present experimental conditions phenobarbitone protected the liver from the hepatotoxic effect of CCl4, while propionyl-promazine did not.

Alanine Transaminase↗
PubMed1983

Maternal and fetal cardiovascular indices during fetal hypoxia due to cord compression in chronically cannulated sheep. II. Responses to promazine.

Promazine (Sparine) administered to chronically cannulated pregnant ewes caused significant maternal and fetal tachycardia and hypotension, depressed uterine blood flow and fetal Pao2, and increased fetal Paco2. When the drug was given before brief compression of the umbilical cord, uterine flow was more depressed than by compression alone, the fetal pressor response was attenuated, and fetal posthypoxia tachycardia was augmented. We conclude that promazine taken by a mother could have especially deleterious effects on her fetus when the latter's oxygenation is already depressed (e.g., by cord compression), and suggest that the use of promazine during labor be reevaluated.

Animals↗
PubMed1987

Photosensitization of SV 40 DNA mediated by promazine derivatives and 4'-hydroxymethyl-4,5',8-trimethylpsoralen. Inhibition of the in vitro transcription.

In vitro transcription by E. coli RNA polymerase was carried out on SV40 DNA photoreacted with various promazine derivatives. Inhibition of the template activity was recorded with increasing irradiation times in the presence of promazine derivatives. Promazine covalent adducts on guanine did not terminate RNA synthesis and seemed to be bypassed by the enzyme. HMT (4'-hydroxymethyl-4,5',8-trimethylpsoralen) photoreaction with DNA was carried out under two conditions: irradiation with lambda greater than 395 nm favouring monoadduction on pyrimidine residues and irradiation at 360 nm inducing a maximum of interstrand diadducts. Both adducts were able to terminate RNA synthesis on the phototreated SV40 DNA and using the O-methyl-nucleotide sequencing procedure, the termination sites were precisely mapped. Monoadducts on the coding strand and cross-links induced termination two bases away from the covalent adduct, but monoadducts on the noncoding strand did not half RNA polymerase.

Base Sequence↗
PubMedDate not supplied

Spectrophotometric determination of promazine with an oxidative column in FIA manifolds.

A simple flow-injection spectrophotometric method for the determination of promazine is described. The two proposed procedures are based on the oxidation of analyte with a manganese dioxide column. Concentrations of promazine in the ranges 2-20 and 1-6 are determined with a relative standard deviation of 1.0%. The injection rates are 62 and 80 samples h-1, respectively. The influence of foreign species and the determination of promazine in a pharmaceutical formulation are also reported.

Calibration↗
PubMed2001

Simultaneous quantification of promazine hydrochloride and its sulfoxide in pharmaceutical preparations.

The use of derivative UV-spectrophotometry is proposed for the simultaneous quantification of promazine hydrochloride in the presence of sulfoxide, and vice versa. For this purpose, mathematical parameters were established for generating derivative spectra of analytes. The determination of promazine was made using the first-order derivative (deltalambda = 10 nm, second polynomial degree) at 268 nm. The quantification of sulfoxide was achieved by applying third-derivative spectra (deltalambda = 14 nm, sixth polynomial degree) based on measurements of the amplitude at 342 - 344 nm. An elaborated method was successfully used to determine analytes in commercial promazine pharmaceuticals. The obtained results agreed well with those obtained by the HPLC method.

Antipsychotic Agents↗
PubMed1991

Influence of aprotinin and promazine on survival of isolated pancreatic acinar cells.

Aprotinin, a protease inhibitor, and promazine, an inhibitor of phospholipase A2, were tested for possible inhibition of pancreatic acinar cell (PAC) decline induced by uncoupling of oxidative phosphorylation with 2,4-dinitrophenol (DNP) or by temporary anoxia/reoxygenation. In incubates of acinar cells isolated from rat pancreas the presence of aprotinin did not influence the survival of cells treated with these noxae. This finding excludes that extracellulary acting trypsin, possibly released from damaged cells, contributes to further cell death. While promazine at concentrations of 15 to 20 nmol.(10(6) cells)-1 was well tolerated by untreated PAC, higher concentrations caused a clear reduction of cell viability. At optimum concentration promazine was without influence on DNP-treated cells, but it had a beneficial effect on survival and morphology of anoxia-treated PAC (p less than or equal to 0.05). Therefore, it can be assumed that after anoxia/reoxygenation the membrane phospholipase A2 becomes stimulated and causes phospholipid depletion with final death of the cells. It is suggested that such a mechanism may contribute to the initial cell damage in the pathogenesis of acute pancreatitis, too.

Acute Disease↗
PubMed1990

Provocation of convulsive activity in the EEG by promazine-HCl-induced sleep in children.

The authors report on the convulsive activity provoking effect of Promazine as shown on EEG during sleep. It has successfully been used in infants and children who do not tolerate sleep deprivation. Promazine had smaller effect on the EEG-pattern than other related compounds or barbiturates. The greatest efficacy could be reached in generalised epilepsy, but the method was also helpful in other epilepsies. It is emphasized that in cases of acute neurological symptoms of not epileptical origin the compound is helpful to exclude epilepsy since Promazine induced sleep was never associated with convulsive activity on EEG in these cases.

Adolescent↗
PubMed1984

Termination sites of the in vitro DNA synthesis on single-stranded DNA photosensitized by promazines.

Bacteriophage phi X174 and M13 mp9 single-stranded DNA molecules were primed either with restriction fragments or synthetic primers and irradiated with near UV light in the presence of promazine derivatives. These DNAs were used as template for in vitro complementary chain synthesis by Escherichia coli DNA polymerase I large fragment. Chain terminations were observed by denaturing polyacrylamide gel electrophoresis of the synthesis products and localized by comparison with a standard dideoxy sequencing pattern. More than 90% of the chain terminations were mapped exactly one nucleotide before a guanine residue. In addition, photoreaction was shown to occur more predominantly with guanine residues localized in single-stranded parts of the genome. The same guanine residues could also be damaged when the reaction was performed, in the dark, in the presence of the artificially generated promazine cation radicals. Using the BamHI-SmaI adaptor (5'GATCCCCGGG-3'), it was shown that the guanine alteration was a covalent addition of the promazine, or of a cation radical photodegradation product, on the guanine moiety. Kinetics of chlorpromazine photoaddition on single-stranded and double-stranded DNAs were determined.

Acepromazine↗
PubMed1976

Effects of d-amphetamine, pentobarbital, chlorpromazine and promazine on electric shock postponement responding by the pigeon.

The effects of d-amphetamine, pentobarbital, chlorpromazine and promazine on responding under schedules of electric shock postponement were studied in pigeons. Responding was maintained by three different response-shock intervals (10, 20 and 60 seconds). Low doses (0.3-3 mg/kg) of d-amphetamine increased response rates without decreasing shock rates under all three response-shock intervals. The highest dose (10 mg/kg) of d-amphetamine increased the shock rates under all response-shock intervals and decreased the high response rate under the 10-second response-shock interval but did not decrease the lower rates of responding under the 20- and 60-second response-shock intervals. Pentobarbital decreased the high rate of responding maintained under the 10-second response-shock interval at lower dose (10 mg/kg) than the lower rates of under the 20- and 60-second response-shock intervals. The high dose (17.5 mg/kg) of pentobarbital decreased responding and the low doses (1-3 mg/kg) had no effect under all three response-shock intervals. Chlorpromazine (3-100 mg/kg) did not affect the average rate of responding under all response-shock intervals and only slightly increased shock rates under the 20- and 60-second response-shock intervals. Promazine (3-30 mg/kg) increased the rates of responding and decreased shock rates under all three response-shock intervals. Analysis of the temporal patterns of responding within the response-shock interval showed that d-amphetamine tended to induce the animals to respond earlier than they normally would in the response-shock interval while otherwise maintaining the temporal pattern of responding, pentobarbital decreased the probability of responses late in the response-shock interval, and chlorpromazine and promazine increased the probability of responses in the middle of the response-shock interval, producing a lessening of the temporal patterning of responding within the response-shock interval.

Animals↗
PubMed1978

Pentobarbital, promazine, d-amphetamine, and scopolamine effects on behavior under multiple and primed schedules of reinforcement.

Pigeons responded under compound fixed-interval (FI) fixed-ratio (FR) schedules of food presentation. Distinctive discrimininative stimuli were either continuously present during each component schedule (multiple FI FR) or were present only for a brief period at the beginning of each component (primed FI FR). Similar rates and patterns of responding were maintained under the multiple and primed schedules. Pentobarbital, scopolamine, and d-amphetamine decreased FR responding, but promazine had little effect at the doses studied. d-Amphetamine and promazine increased FI responding at certain doses, pentobarbital had little effect, and scopolamine decreased responding. There were no systematic differences in the effects of drugs under the multiple and primed schedules, in spite of the differences in discriminative stimuli under the conditions.

Animals↗
PubMed1983

Effects of chlorpromazine and promazine on the visual aftereffects of tilt and movement.

The effects of chlorpromazine (CPZ) and promazine on the visual aftereffects of tilt and motion were measured. CPZ markedly reduced the strength of both aftereffects, while promazine produced a smaller and not always significant reduction. Control experiments suggested that the effects were produced in the central visual system rather than by several possible peripheral artefacts or by drowsiness. The effects are discussed with reference to the pharmacological activity of the drugs and their influence on the strength of inhibition in the visual cortex, both in normal subjects and in schizophrenic illness.

Adaptation, Ocular↗
PubMed1986

Termini generated at the site of the DNA breakage mediated by photoexcited promazines.

Promazine derivatives are known to be able to photoinduce, in vitro, direct single-strand breaks into DNA (Decuyper et al., Biochem. Pharmac. 33, 4025-4031 (1984]. Using [32P]end labeled DNA fragments, it is demonstrated that this DNA breakage occurs almost regardless of the nucleotide sequence of the DNA. Using 3'-[32P]end or 5'-[32P]end labeled oligonucleotide and enzymatic digestion of the fragments generated, it is demonstrated that the termini generated at the site of the breakage are 5'-phosphate, 3'-phosphate and 3'-termini which are presumed to be 3'-phosphoglycolate. This is consistent with an attack of the sugar moeity of the sugar-phosphate backbone of the DNA by the reactives species generated upon near-u.v. irradiation of promazine derivatives.

DNA↗
PubMed1987

Interaction of promazine with human ceruloplasmin.

Promazine is enzymically oxidized by ceruloplasmin without reduction of the 610 nm absorption band of the enzyme. Fluoride inhibited the reaction in a non-competitive manner. The ceruloplasmin oxidase activity is markedly enhanced when promazine is added in the presence of NADH; possibly through a change in enzyme conformation.

Ceruloplasmin↗
PubMed1979

[Clinico-physiological sleep- and hangover-spectra from pentobarbital, promazin and their combination, as reflected by self-ratings of young and elderly subjects (author's transl)].

A sample of 8 young and 8 elderly subjects was examined in a 2x2x2 factorial design, whether and how promazine interacts with pentobarbital as a hypnotic agent. Analyses of self-reports led to the following conclusions: 1. Young subjects and not experience any significant effects from either the single components (pentobarbital, promazine) and/or their combination. 2. Elderly subjects experienced positive effects in sleep and hangover parameters under the single components as well as under the combination. Consequences for research in clincal psychopharmacology are discussed.

Adult↗
PubMed1985

Hemodynamic and acid-base effects of promazine on unanesthetized pregnant sheep and fetus.

Although promazine has been used in obstetrics for over 20 years, its effects upon hemodynamic and acid-base conditions of steady-state pregnant sheep and fetus has not been sufficiently investigated. To study these effects, 10 experiments were performed in 5 ewes and their fetuses. Promazine (1 mg/kg/4 min) was administered intravenously to the ewes. Significant maternal changes included: reduction in hemoglobin from 9.1 +/- 0.43 to 8.4 +/- 0.43 g/100 ml at 120 min, O2 content from 12.1 +/- 0.61 to 10.8 +/- 0.59 vol% at 90 min, O2 saturation from 9.7 +/- 2.58 to 95.4 +/- 2.80% at 15 min, and blood pressure from 86.1 +/- 4.94 to 74.1 +/- 2.55 mm Hg at 45 min. The heart rate increased from 84 +/- 2.64 to 100 +/- 5.03 beats/min at 120 min. The uterine blood flow remained unchanged. The fetus developed mild metabolic acidosis as manifested by the reduction in pH from 7.375 +/- 0.008 to 7.35 +/- 0.005 at 45 min. No other fetal hemodynamic changes were observed. The significance of these findings is discussed.

Acid-Base Equilibrium↗
PubMed1982

Oral administration of diazepam and promazine hydrochloride to immobilize pronghorn.

Oral tranquilizers were mixed with a grain bait and fed to pronghorn (Antilocapra americana) in an attempt to immobilize and thus facilitate their capture. Diazepam, administered at 6 mg/kg body weight immobilized a tame pronghorn fawn within 30 min. Tranquilization was still apparent after 8 h. A minimum dose of 23 mg/kg body weight was necessary to immobilize a wild adult pronghorn. Immobilization occurred after 60 min and tranquilization was apparent 24 h post ingestion. Excitement severely impeded the effect of the drug and although easily captured, the animal struggled wildly when handled. Wild pronghorn fawns showed moderate tranquilization when administered diazepam at 23 mg/kg body weight but were unapproachable. Doses of diazepam between 13 and 23 mg/kg body weight were used to capture tame yearling and adult pronghorn held in a 132 ha enclosure. A dose of 23 mg/kg body weight was excessive in that the animals did not recover for 48 to 54 h post ingestion and had difficulty maintaining a sternal bedding position. Diazepam at 13 mg/kg body weight failed to tranquilize the animals sufficiently for easy capture. Promazine hydrochloride at doses of 2 to 17 mg/kg body weight, given orally to wild pronghorn fawns and an adult, did not produce visible signs of tranquilization. Animals refused to eat bait containing doses of promazine hydrochloride greater than 17 mg/kg body weight.

Administration, Oral↗