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PubMed1981

Inhibition of allergen-mediated histamine release from human cells by ketotifen and oxatomide. Comparison with other H1 antihistamines.

We have studied the ability of four H1 antihistamines, ketotifen, oxatomide, clemastine and promethazine, and of disodium cromoglycate (DSCG) to inhibit in vitro histamine release mediated by antigen from passively sensitized human lung and from basophilic leukocytes. Anaphylactic histamine release from human leukocytes is inhibited in a comparable fashion by oxatomide, clemastine and promethazine at concentrations just below those inducing histamine release in the absence of antigen. Ketotifen causes a significantly weaker inhibition without inducing histamine release and DSCG is not at all active in this model. On human lung, oxatomide, clemastine and promethazine give a strong and similar inhibition which is linearly related to the dose. Ketotifen markedly differs in this respect, inhibiting according to a bell-shaped dose-response curve and at concentrations closely comparable to that of DSCG. Thus, we confirm that H1 blockers, such as clemastine and promethazine, inhibit anaphylactic histamine release from basophils and human lung but only at high concentrations which may be cytotoxic. Oxatomide behaves very much like these antihistamines. Ketotifen, on the other hand, gives in both models a different pattern of inhibition, closely mimicking that of DSCG. This suggests that the antianaphylactic activity of ketotifen is not related to its H1 blocker properties and that this effect may be relevant to its therapeutic activity.

Allergens↗
PubMed1992

Effectiveness and duration of intramuscular antimotion sickness medications.

Motion sickness inhibits gastric motility, making the oral route ineffective for medications. The intramuscular route is an effective alternative. The rotating chair was used to produce the M 111 level of motion sickness on the Graybiel Symptom Scale. The intramuscular medications given 30 minutes before rotation were compared with placebo (saline, 1 mL) for effectiveness and duration in increasing the number of tolerated head movements. Average placebo number of head movements was 294. Promethazine 25 mg increased head movements by 78% (P < .05), with a duration of 12 hours. Scopolamine 0.2 mg increased head movements by 91% (P < .05), with a duration of 4 hours. The effect of caffeine 250 mg and ephedrine 25 mg was not significant. When combined with scopolamine, ephedrine produced an 32% additive effect. Scopolamine 0.08 mg, 0.1 mg, and 0.2 mg and also promethazine 12.5 mg and 25 mg were significant (P < .05). Promethazine appears to be the drug of choice for intramuscular use because of a longer duration and a high level of effectiveness. Scopolamine was of high effectiveness, but had a duration of 4 hours. It was eight times as potent by the intramuscular as by the oral route.

Caffeine↗
PubMed1994

Effects of motion sickness and antimotion sickness drugs on gastric function.

This study examined the effects of motion sickness and antimotion sickness drugs on gastric emptying (GE). Drugs were tested in normal and motion sick subjects. To induce motion sickness, subjects performed head movements while seated in a rotating chair. Gastric emptying of liquid (300 mL) was determined by nuclear medicine techniques, whereas gastric electrical activity, the electrogastrogram (EGG), was monitored from surface (cutaneous) electrodes positioned over the abdominal area. Gastric emptying was severely inhibited at the peak of motion sickness symptoms, but returned to normal 15 minutes later when symptoms abated. In normal (non-motion sick) subjects intramuscular (IM) scopolamine (0.1 mg) and IM promethazine (25 mg) inhibited GE, whereas erythromycin ethylsuccinate (EES) suspension (200 mg) given orally increased GE. When administered to motion sick subjects, IM scopolamine and IM promethazine added slightly, but not significantly, to the inhibition of GE already present. Oral EES did not significantly alter GE in motion sick subjects. Although EGG frequency remained within normal limits (approximately 2.5-3.5 cpm) after liquid ingestion in both normal and motion sick subjects, EGG amplitude was differentially affected in the two groups. Electrogastrogram amplitude increased twofold to fourfold after liquid ingestion in normal, but not in motion sick subjects. The results suggest that (1) maximal inhibition of GE is coincident with peak motion sickness symptoms, (2) both IM scopolamine and IM promethazine inhibit GE in normal subjects, but do not add significantly to the inhibition of GE already established during motion sickness, (3) orally administered erythromycin enhances GE in normal, but not in motion sickness subjects, and (4) the normal stimulatory effect of liquid ingestion on gastric motility does not occur in motion sick subjects.(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗
PubMed1991

H1 and H2 receptor antagonists and hepatic oxygen supply-demand relationship in pigs.

The hypothesis that histamine receptor (H1 and H2) blockade beneficially affects the hepatic oxygen supply-demand relationship was tested during experiments performed on 13 miniature pigs. Hepatic arterial and portal blood flows were measured with electromagnetic flowmeters. Cardiac output was determined by thermodilution. H1 and H2 receptor blockade was achieved with promethazine, 5 mg.kg-1 and cimetidine 30 mg.kg-1 IV, respectively. The study demonstrated no significant effect of H1 and H2 receptor blockade on hepatic oxygen uptake and no noticeable effects of cimetidine on hepatic circulation. However, promethazine decreased total hepatic blood flow, primarily by decreasing portal blood flow; this resulted in an increase in oxygen extraction as reflected in a decreased oxygen content in hepatic venous blood. The results reject the posed hypothesis: H1 receptor antagonist promethazine decreased, while H2 receptor antagonist cimetidine did not affect hepatic blood flow and oxygen supply; hepatic oxygen demand remained unaffected during H1 and H2 receptor blockade.

Animals↗
PubMedDate not supplied

Chloroquine disposition in hypersensitive and non-hypersensitive subjects and its significance in chloroquine-induced pruritus.

Twenty-one healthy Nigerian volunteers distributed into four groups participated in a study to determine the significance of chloroquine disposition in chloroquine-induced pruritus. It involved the administration of chloroquine with or without promethazine pre-administration to the subjects. Group I consisted of 8 chloroquine non-hypersensitive subjects receiving 2 tablets of chloroquine sulphate (300 mg base); Group II consisted of 5 chloroquine non-hypersensitive subjects receiving 2 tablets of chloroquine sulphate 30 minutes after 25 mg promethazine tablet pre-administration; Group III consisted of 5 chloroquine hypersensitive subjects treated as in Group II; Group IV consisted of 3 hypersensitive subjects treated as in Group I. Blood (5 ml) and urine samples were collected periodically for up to 6 days post-dose. The samples were analysed for chloroquine and some of its oxidation metabolites by a specific HPLC method. Probit plots of cumulative drug/metabolite ratios were done to determine if there is polymorphism in chloroquine metabolism. There was bimodality only in the distribution of chloroquine/monodesethylchloroquine ratios, suggesting polymorphism in the metabolic oxidation of chloroquine in these subjects. Higher levels of monodesethylchloroquine were obtained in Group IV subjects when compared with any of the other groups. The oral clearance rate, elimination half-life, and volume distribution at steady state of chloroquine in the study groups were not significantly different (P greater than 0.05). In the absence of promethazine there appears to be an extensive metabolism of chloroquine in hypersensitive individuals to produce monodesethylchloroquine which probably determines the degree of pruritus experienced by an individual.

Adult↗
PubMed1985

Histamine H1 receptor participation in the control of prolactin secretion in postpartum.

It has been reported that cimetidine, an H2-receptor antagonist, stimulates PRL secretion in postpartum. In the present study, the PRL response to two H1-receptor antagonists, promethazine and d-chlorpheniramine, was studied in 38 normal puerperal women on day 1 after delivery. Serum PRL levels decreased significantly after a single dose of promethazine (100 mg) given im (5 women) or d-chlorpheniramine (20 mg) given iv (6 women). In contrast, no significant change in PRL levels was observed after only saline infusion (6 women). Promethazine, given concomitantly to an iv bolus injection of TRH (200 micrograms) (6 women) and d-chlorpheniramine, given at the onset of suckling (6 women), did not alter stimulation of PRL release induced by these challenges. These results suggest the involvement of histamine H1 receptors in the regulation of basal PRL secretion in postpartum and would indicate that they do not participate in the mechanisms underlying suckling-induced PRL release.

Adolescent↗
PubMed2002

Inhibitory effects of H1-antihistamines on CYP2D6- and CYP2C9-mediated drug metabolic reactions in human liver microsomes.

OBJECTIVE: To screen the inhibitory effects of H1-antihistamines on hepatic bufuralol 1'-hydroxylation and on tolbutamide 4-methylhydroxylation in human liver microsomes. METHODS: Bufuralol 1'-hydroxylation and tolbutamide 4-methylhydroxylation were used as index reactions for CYP2D6 and CYP2C9, respectively. The metabolites of both reactions were measured using high-performance liquid chromatography and were used as indicators of whether CYP2D6 or CYP2C9 activities were inhibited or unaffected by the agents. RESULTS: All five H1-antihistamines studied showed a concentration-dependent inhibition of CYP2D6-mediated bufuralol 1'-hydroxylation with 50% inhibitory concentration (IC50) values of 32-109 microM. Cyclizine and promethazine showed inhibitory effects on tolbutamide 4-methylhydroxylation with IC20 values of 85 microM and 88 microM, respectively. Tripelennamine, chlorpheniramine, and diphenhydramine showed no inhibitory effects on CYP2C9. CONCLUSION: All five H1-antihistamines studied inhibited CYP2D6 markedly, but only cyclizine and promethazine inhibited CYP2C9 at concentrations above that usually seen in plasma. Promethazine and chlorpheniramine inhibited CYP2D6 at concentrations that are very close to their therapeutic plasma concentrations. Further studies in humans, especially in poor metabolizers of CYP2D6, will be required to confirm these findings.

Aryl Hydrocarbon Hydroxylases↗
PubMed1976

Effect of antihistamines and chlorpromazine on the calcium-induced hyperpolarization of the Amphiuma red cell membrane.

1. It has previously been demonstrated that an increase in extracellular Ca2+ conce-tratio- induces a trandient increase in K+ permeability and associated hyperpolarization of the red cell membrane of the giant salamander, Amphiuma meand. This phenomenon is analogous to the Ca2+-induced KCl loss observed in ATP-depleted human red cells and red cell ghosts. 2. Histamine, which enhances the Ca2+-induced K+ loss from depleted human red cells, is without effect on this Ca2+-induced hyperpolarization of Amphiuma red cells. 3. Promethazine (10 muM) and mepyramine (1 mM), which inhibit the Ca2+-induced K+ loss in depleted human red cells, also block the Ca2+-related hyperpolarization of Amphiuma erythrocytes. 4. Chlorpromazine (25 muM), despite being a weak antihistamine, is equally effective in blocking the Ca2+-induced hyperpolarization of Amphiuma red cells. 5. Ionophore A23187 causes a large and sustained Ca2+/K+-dependent hyperpolarization even in the presence of normal (1.8 mM) concentrations of Ca2+. This hyperpolarization is relatively insensitive to chlorpromazine and promethazine. 6. The inhibition of the Ca2+-induced hyperpolarization of the Amphiuma red cell membrane by chlorpromazine and promethazine may berelated to their properties as local anaesthetics.

Animals↗
PubMed1976

Comparison of effects of drugs on dopamine metabolism in the substantia nigra and the corpus striatum of rat brain.

The influence of apomorphine, chloral hydrate, haloperidol, morphine, oxotremorine, pargyline, probenecid and promethazine on DOPAC and HVA levels was studied in the substantia nigra (including the ventral tegmental dopaminergic regions) and corpus striatum of the rat brain. The time--effect curves of changes in HVA levels after pretreatment with apomorphine, haloperidol, morphine, oxotremorine or promethazine are presented. The time--effect curves for the substantia nigra showed an initial rapid HVA rise, which was not observed in the corpus striatum. Promethazine treatment caused a small but significant HVA rise in the substantia nigra only. Chloral hydrate, morphine and oxotremorine induced a similar percentage increase in DOPAC and HVA levels in the substantia nigra as well as in the corpus striatum. Haloperidol, however, caused a small percentage change in the metabolite levels in the substantia nigra when compared to the pronounced rise seen in the corpus striatum. The apomorphine-induced HVA decrease observed in both structures provides evidence for the presence of a dopaminergic receptor in the substantia nigra.

3,4-Dihydroxyphenylacetic Acid↗
PubMed1985

Role of histamine in the cell turnover changes associated with experimental gastric ulceration in the mastomys.

Using an animal model of gastric ulceration, in vivo and in vitro methods were developed to assess the importance of histamine in the cell turnover abnormalities previously found to occur in the preulcerous phase of gastric ulceration induced by mucosal anaphylaxis, and by using specific H1- and H2-receptor agonists and antagonists to define which receptors were involved. In ovalbumin-immunized animals, intramucosal ovalbumin injection led to a highly significant increase in cell turnover as measured by [3H]thymidine uptake (p less than 0.001). This increase was not affected by treatment with the H2 antagonist cimetidine, but was significantly reduced by the H1 antagonists promethazine and clemastine (p less than 0.01). A cell culture method was then used to examine the effects of added histamine and its antagonists. Histamine at a concentration of 10(-7) M was found to have a significant stimulatory effect on cell proliferation (p less than 0.001), and this effect was blocked by promethazine and clemastine but not by cimetidine. In contrast, histamine at a concentration of 10(-2) M had an inhibitory effect on cell proliferation which was accentuated by cimetidine and partially reversed by promethazine and clemastine. The H1 agonist betahistine was found to have stimulatory effects similar to those of histamine in low concentration (10(-7) M and 10(-6) M), but the H2 agonist 4-methyl histamine did not affect thymidine uptake at these concentrations. Both H1 and H2 agonists had a similar inhibitory effect at a concentration of 10(-2) M. It is concluded that histamine probably plays an important part in the changes in cell kinetics associated with gastric ulceration induced by this method, and that the trophic effects of histamine are mediated by H1-receptors. H2-receptors appear to have only a limited role in the control of cell proliferation.

Animals↗
PubMed1995

Morphine and the "lytic cocktail" for terminally ill patients in a French general hospital: evidence for an inverse relationship.

Undertreatment of cancer pain with analgesic drugs is still a frequent problem in French hospitals. In the absence of good analgesic practices, the use of a so-called lytic cocktail, which combines a neuroleptic (chlorpromazine), an opioid (meperidine), and an antihistamine (promethazine) has become common during the terminal phase of the disease. The lytic cocktail (LC) has been subsequently denounced as a type of disguised euthanasia. The aim of our study was to examine the prescription of morphine and lytic cocktail for terminally ill patients in a 427-bed French general hospital during a 3-year period (1989-1991) that coincided with the beginning of a pain relief service. The study was performed in two steps: a chart review of the 841 deceased patients during the observation period and an examination of morphine and parenteral promethazine consumption from the hospital pharmacy. Data from both the charts and the pharmacy showed an inverse relationship between these treatments. Morphine consumption increased while LC consumption decreased. The number of deceased patients who received LC were 24.4% in 1989, 19.9% in 1990, and 6.6% in 1991 (P < 0.001 between 1990 and 1991). The number of deceased who received morphine were 13.6% in 1989, 20.6% in 1990, and 23.9% in 1991 (P < 0.01 between 1989 and 1990). During the same period, the annual hospital morphine consumption increased by 191%, and the annual hospital parenteral promethazine consumption decreased by 62.5%. Our results suggest that, when pain is more correctly treated, the use of an inappropriate method of symptom control decreases.(ABSTRACT TRUNCATED AT 250 WORDS)

Aged↗
PubMed2006

Triage test and HPLC assay for analysis of vegetamin, an antipsychotic agent, using gastric contents and blood specimens.

Vegetamin is an antipsychotic agent composed of phenobarbital, promethazine and chlorpromazine. While phenobarbital can be detected by the Triage kit for screening drugs of abuse, the other two components cannot. We describe here the detection of promethazine and chlorpromazine using either a high performance liquid chromatography (HPLC) unit equipped with an ultraviolet, a photodiode array (PDA), or an electrochemical detector (ECD), or gas chromatograph-mass spectrometry (GC-MS). The absorption and mass spectra of promethazine and chlorpromazine were nonspecific, and thus the ECD-HPLC system was best equipped to quantitate these components. Comparison of the chromatograms of blood and gastric contents aids the identification of drug metabolites.

Antipsychotic Agents↗
PubMedDate not supplied

Effects of drug countermeasures for space motion sickness on working memory in humans.

Space motion sickness (SMS) is a problem during the first 72 h of space flight and during transitions from different gravity environments. There currently are no effective drug countermeasures for SMS that also accommodate the retention of optimal cognitive function. This creates a dilemma for astronauts because cognitive skills are particularly important during gravity transitions (e.g., take-off and landing). To quantify the cognitive side effects of potential drug countermeasures, an automated delayed matching-to-sample (DMTS) procedure was used to assess visual working memory before and after drug countermeasures (meclizine 25 mg, scopolamine 0.4 mg, promethazine 25 mg, or lorazepam 1 mg, given orally approximately 45 min prior to testing) and/or the induction of SMS by vestibular stimulation in a rotary chair (spinning). Sixty-seven normal healthy volunteers (mean age, in years, 26.6+/-4.8 S.D.; 24 females and 43 males) each participated in two test sessions, one 'off' drug and one 'on' drug. Spinning by itself significantly decreased task accuracy (Acc) and choice response speed, especially at longer recall delays. Meclizine alone had no effect on Acc or speed with or without spinning. Scopolamine alone decreased Acc, and with spinning, slowed speed. Promethazine alone had no adverse effect, but combined with spinning, decreased Acc and speed. Lorazepam alone decreased speed, and with spinning, decreased Acc. The data suggest that, at clinically useful doses, the rank order of the drugs with the best cognitive profiles is meclizine>scopolamine>promethazine>lorazepam.

Adult↗
PubMed1999

The role of potassium channels in antihistamine analgesia.

The effect of the administration of pertussis toxin as well as modulators of different subtypes of K+ channels on the antinociception induced by the H1-antihistamines pyrilamine, diphenhydramine and promethazine was evaluated in the mouse hot plate test. Pretreatment with pertussis toxin (0.25 microg/mouse i.c.v.) prevented pyrilamine, diphenhydramine and promethazine antinociception. The K(ATP) channel openers minoxidil and pinacidil potentiated the antinociception produced by the H1-antihistamines whereas the K(ATP) channel blocker gliquidone prevented the anti H1-induced analgesia. The Ca2+-gated K+ channel blocker apamin antagonized pyrilamine, diphenhydramine and promethazine analgesia. Pretreatment with an antisense oligonucleotide (aODN) to mKv1.1, a voltage-gated K+ channel, at the dose of 3.0 nmol/single i.c.v. injection, never modified the antinociception induced by the H1-antihistamines in comparison with degenerate oligonucleotide (dODN)-treated mice. At the highest effective doses, none of the drugs used modified animals' gross behaviour nor impaired motor coordination, as revealed by the rota rod test. The present data demonstrate that both K(ATP) and Ca2+-gated K+ channels, contrary to voltage-gated K+ channel Kv1.1, represent an important step in the transduction mechanism underlying central antinociception induced by H1-antihistamines.

Animals↗
PubMed2002

Extractive-spectrophotometric determination of some phenothiazines with dipicrylamine and picric acid.

Dipicrylamine and picric acid have been tested as reagents for the determination of promethazine and perphenazine. They react in neutral media with these drugs forming the coloured compounds. The compounds are sparingly soluble in water and quantitatively extracted into organic solvents. The extracts are intensely coloured and very stable. These properties have been exploited for the extractive spectrophotometric determination of promethazine and perphenazine in pure solutions and pharmaceuticals. Linear calibration graphs were obtained in the concentration range 4-40, 3-30 microg ml(-1) of promethazine and 4-80, 8-60 microg ml(-1) of perphenazine for picric acid and dipicrylamine, respectively. The relative standard deviation (RSD) is less than 0.8%.

Antipsychotic Agents↗
PubMed2000

Itching after intrathecal morphine. Incidence and treatment.

This study was designed to determine whether low doses of intrathecal morphine still result in itching and it evaluates the outcome of a standardized treatment using promethazine and - for intractable itch - naloxone. Patients (n = 143) scheduled for total hip surgery were allocated to four groups (in a double blind manner) with bupivacaine 20 mg in 4 mL but different doses of intrathecal morphine: Group I, 0.025 mg, Group II, 0.05 mg, Group III, 0.1 mg and Group IV, 0.2 mg. The presence or absence of itching was noted every three hours for a 24-h period. When required, standardized treatment was provided. The incidence of itching was: Group I: 14. 3%; Group II: 21.6%; Group III: 48.6%; and, Group IV: 61.7%. Itch was treated by administering promethazine intramuscularly in 2.9% (Group I); 8.1% (Group II); 10.8% (Group III), and 8.9% (Group IV), respectively. Only in group IV there was a single patient who needed naloxone to treat itching. The incidence and severity of itching is a dose-related side-effect in the dose range of 0.025-0.2 mg of intrathecal morphine. Itching still occurs after the low doses of intrathecal morphine, but symptoms vanish after promethazine 25 mg intramuscularly.

Aged↗
PubMed1997

A randomized controlled trial of sedation in the critically ill.

A randomized controlled trial comparing: a) a combination of oral chloral hydrate and promethazine to b) a continuous intravenous midazolam infusion, for maintenance sedation in critically ill children, was carried out. The level of sedation was assessed four hourly using a specifically devized sedation scale. Forty-four children entered the study of whom two were subsequently excluded. The number of satisfactory assessments (desired and actual levels of sedation equal) was significantly greater in the chloral hydrate and promethazine group (Chi-squared P < 0.01; confidence intervals of the difference 0.06 to 0.20). The number of assessments at level 5 on the sedation scale (patient restless/ distressed) was significantly greater in the midazolam group (Chi-squared P < 0.05). The total number of satisfactory assessments in the two groups were only 61 and 48% respectively, suggesting that sedation can be considerably improved. Chloral hydrate and promethazine are more effective than midazolam as maintenance sedation in critically ill children. It is possible to prospectively study the efficacy of sedative drugs in critically ill children.

Administration, Oral↗
PubMed2003

The use of simple ketamine anaesthesia for day-case diagnostic laparoscopy.

General anaesthesia using ketamine has been shown to be safe. It is generally used in our private hospitals where there is lack of qualified personnel and sophisticated anaesthetic machines. A retrospective review of 295 cases of laparoscopy was performed over 28 months at the fertility Unit of Life Specialist Hospital Nnewi, Anambra State, Nigeria. Ketamine general anaesthesia was used for all the patients after premedication with 0.6 mg of atropine. Seventy-six and 102 patients who had additional premedication of 10 mg diazepam and 50 mg promethazine, respectively, were compared. The duration of this procedure ranged between 7 and 18 minutes, with a mean of 12 minutes. The dose of ketamine used was 100 mg mean (range 50-180 mg); 12.6% of the patients had some form of reaction. Diazepam reduced talkativeness during recovery but increased the recovery time significantly, from an average of 45 minutes to 3 hours. Promethazine significantly reduced vomiting and restlessness and did not significantly prolong the recovery time (from an average of 45 minutes to 70 minutes). Two patients who had only atropine as premedication had an idiosyncratic reaction of breathlessness and tonic-clonic-like movements. They responded to intravenous diazepam. Ketamine produces a safe, effective and simple general anaesthesia and is recommended for use in day-case laparoscopy, where standard anaesthetic machines and trained personnel are lacking. Use of promethazine premeditation is advocated for improved outcome.

Adolescent↗