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Background: Presently available antiepileptic drugs are effective in controlling seizures in more than half of patients of all epilepsy but use is often limited by adverse effects. H1 receptor antagonists, have a controversial status in patients of epilepsy. Both pro and antiepileptic effect has been documented in various animal studies. Hence, this study was designed to see the effect of promethazine, an H1 antihistaminic drug and its interactions with antiepileptic drugs lorazepam and sodium valproate in rats.Methods: The effect of promethazine (10 mg/kg) and its interactions with antiepileptic drugs lorazepam and sodium valproate was assessed by using maximal electroshock seizures (MES) and chemoshock pentylenetetrazol (PTZ) method.Results: Promethazine along with lorazepam and sodium valproate in subtherapeutic doses exerted significant protection against MES induced seizures whereas no such protection was observed with PTZ method rather the seizure threshold was reduced.Conclusions: Subtherapeutic doses of promethazine alone and in combination with lorazepam and sodium valproate showed protection against seizures in MES method. However, proconvulsant effect was seen with PTZ method. This shows dual behavior of promethazine on MES and PTZ induced seizures.
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Purpose: Hyperemesis gravidarum is one of the leading causes of hospitalization during pregnancy. This randomized study wasaimed to compare and evaluate the efficacy of granisetron and promethazine in controlling nausea and vomiting in pregnancy.Materials and Methods: This study was done in the Department of Obstetrics and Gynaecology, Nalanda Medical College andHospital, Patna, Bihar, over a period of 6 months from February 2019 to July 2019. The included patients were administeredgranisetron and promethazine randomly and evaluated for nausea and vomiting by senior gynecologist blinded to designated drugs.Results: This study showed that granisetron was more effective than promethazine in controlling nausea and vomiting inpregnant patients. Greater patient satisfaction and less adverse drug reaction were observed in women receiving granisetron.Conclusion: Hyperemesis gravidarum is a health-related problem with social, economic, and psychological dimensions.All efforts, especially simple outpatient strategies, can reduce the severity of this condition and will help pregnant women tocontinue her pregnancy with satisfaction.
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Background: Current antiepileptic drugs (AEDs) are effective in controlling seizures in about 70% patients but use is often limited by adverse effects. Promethazine, H1 receptor antagonist, has a controversial status in patients of epilepsy. Both pro and antiepileptic effect has been documented in various animal studies. Hence, this study was designed to see the effect of promethazine, an H1 antihistaminic drug and its interactions with antiepileptic drugs in rats.Methods: The effect of promethazine (10mg/kg) and its interactions with antiepileptic drugs diazepam and phenytoin was assessed by using maximal electroshock seizures (MES) and chemoshock (PTZ) method.Results: Promethazine along with diazepam in subtherapeutic doses exerted significant protection against MES induced seizures whereas no such protection was observed with PTZ method rather the seizure threshold was reduced.Conclusions: Subtherapeutic doses of Promethazine alone and in combination with diazepam showed protection against seizures in MES method. However, proconvulsant effect was seen with PTZ method suggesting histamine plays a protective role in development of seizures. This shows dual behavior of promethazine on MES and PTZ induced seizures.
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Objective To observe the clinical efficacy of acupoint injection at Fenglong (ST 40) with Promethazine in treating posterior circulation ischemic vertigo (PCIV) due to turbid phlegm obstructing the middle.Method Sixty-two patients with PCIV due to turbid phlegm obstructing the middle were randomized into a treatment group and a control group, 31 cases each. The two groups both received intravenous infusion of Vinpocetine injection, based on which, the treatment group was intervened by injection at Fenglong (ST 40) with Promethazine, while the control group was given gluteal intramuscular injection of Promethazine. The traditional Chinese medicine (TCM) syndrome score and Dizziness Handicap Inventory (DHI) were observed for the two groups before and after the treatment, and the clinical efficacies were also compared.Result The TCM syndrome and DHI scores were significant changed after the intervention in both groups (P<0.05). After the treatment, the TCM syndrome and DHI scores in the treatment group were significantly different from those in the control group (P<0.05). The total effective rate was 93.5％ in the treatment group versus 80.6％ in the control group, and the between-group difference was statistically significant (P<0.05).Conclusion Injection at Fenglong (ST 40) with Promethazine is an effective method in treating PCIV due to turbid phlegm obstructing the middle.
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Objective To study the absorption characteristics of promethazine hydrochloride in different parts of rat intestine, provide evidence for the development of new preparation. Methods Rat single-pass intestinal perfusion model was established. By using high performance liquid chromatography (HPLC), 25, 50, 100 μgmL-1 promethazine hydrochloride concentration changing in different parts of the intestine was detected. Through the relevant calculation, the absorption rate constant ( Ka ) , and the apparent absorption coefficient ( Papp ) were obtained. Results With the concentration increase of promethazine hydrochloride in duodenal and ileal segments, the Ka and Papp increased significantly in the same part. Ka was (28.00±0.02)×10-2min-1 and Papp was (9.64±0.22) in the jejunum were the highest when the promethazine hydrochloride concentration was 50 μgmL-1 . As the concentration increased in colon, there were no significant changes in Ka and Papp . Conclusion Promethazine hydrochloride is absorbed in various intestinal segments, most obviously in duodenum and ileum, the absorption order is duodenum>ileum>jejunum>colon. Promethazine hydrochloride is absorbed most in the small intestine, in line with the intestinal absorption characteristics.
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Objective To study the absorption characteristics of promethazine hydrochloride in different parts of rat intestine, provide evidence for the development of new preparation. Methods Rat single-pass intestinal perfusion model was established. By using high performance liquid chromatography (HPLC), 25, 50, 100 μgmL-1 promethazine hydrochloride concentration changing in different parts of the intestine was detected. Through the relevant calculation, the absorption rate constant ( Ka ) , and the apparent absorption coefficient ( Papp ) were obtained. Results With the concentration increase of promethazine hydrochloride in duodenal and ileal segments, the Ka and Papp increased significantly in the same part. Ka was (28.00±0.02)×10-2min-1 and Papp was (9.64±0.22) in the jejunum were the highest when the promethazine hydrochloride concentration was 50 μgmL-1 . As the concentration increased in colon, there were no significant changes in Ka and Papp . Conclusion Promethazine hydrochloride is absorbed in various intestinal segments, most obviously in duodenum and ileum, the absorption order is duodenum>ileum>jejunum>colon. Promethazine hydrochloride is absorbed most in the small intestine, in line with the intestinal absorption characteristics.
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AIM To establish an HPLC-DAD method for the simultaneous content determination of four constituents in Compound Kendir Leaves Tablets Ⅰ (Apocyni veneti Folium,Chrysanthemi indici Flos,Stephaniae tetrandrae Radix,etc.).METHODS The analysis of 50％ methanol extract of this drug was performed on a 35 ℃ thermostatic Shimadzu VP-ODS column (250 mm × 4.6 mm,5 μm),with the mobile phase comprising of methanol-0.5％ phosphoric acid flowing at 1.0 mL/min in a gradient elution manner,and the detection wavelengths were set at 260 nm and 325 nm.RESULTS Chlorogenic acid,hydrochlorothiazide,buddleodide and promethazine hydrochloride showed good linear relationships within the ranges of 24.91-498.2 ng (r =0.999 9),286.33-5 726.7 ng (r =0.999 9),10.04-200.9 ng (r =0.999 9) and 154.80-3 096.1 ng (r =0.999 9),whose average recoveries were 98.3％ (RSD =1.3％),99.1％ (RSD =0.6％),98.5％ (RSD =1.0％) and 99.3％ (RSD =1.2％),respectively.CONCLUSION This simple,accurate and reliable method can be used for the quality control of Compound Kendir Leaves Tablets Ⅰ.
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Objective To develop a high performance liquid chromatography (HPLC) method for determining the content and dissolution of promethazine hydrochloride and caffeine tablets. Methods Agilent TC C18 column (250 mm×4.6 mm, 5 μm) was used. The mobile phase was methanol-3‰ triethylamine solution (adjusted to pH2.3 with phosphoric acid) (50: 50, v/v) with a flow rate 1.0 ml/min, and the detection wavelengths were set at 250 nm and 272 nm, respectively. The column temperature was 30°C and the injection volume was 20 μl (injection volume of 10 μl for dissolution). Dissolution of tablets was determined by paddle method and the temperature was 37°C, 900 ml pH 1.2 hydrochloric acid solution, acetic acid buffer (pH 4.5), phosphoric acid buffer (pH 6.8) and water were used as dissolution medie at the rotation speed of 50, 75 r/min for selecting dissolution condition. Results The calibration curves were linear within the range of 0.5-100 μg/ml (r=1) for promethazine hydrochloride, and forcaffeine 4-400 μg/ml (r=0.9999), respectively. The detection limit and quantification limit of promethazine hydrochloride were 15 and 40 ng/ml, and caffeine 2 and 10 ng/ ml, respectively. The recoveries of promethazine hydrochloridum and caffeine were (100.04±1.39) % (n=9) and (99.42±1.07) % (n= 9), respectively. And the stability of working solutions was acceptable in 12 h. The method of dissolution tests for the tablet was established with 900 ml pH 1.2 hydrochloric acid solution as dissolution medium, paddle rotation speed of 50 r/min, and dissolution time 30 min. Conclusion The method is convenient, fast, sensitive and reproducible, with good precision, specificity and accuracy. So it can be used for simultaneous determination and dissolution of promethazine hydrochloride and caffeine tablet.
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Objective To investigate the efficacy and safety of using various sedative regimens during transcatheter arterial chemoembolization (TACE) for hepatocellular carcinoma (HCC).Methods 156 HCC patients were randomly divided into four groups.The control group (n =30):intramuscular injection of 10 ml saline;The diazepam group (n =42):intramuscular injection of 10 mg of diazepam;The promethazine group (n =42):intramuscular injection of promethazine 25 mg;and The combined group (n =42):intramuscular injection of 10 mg of diazepam and promethazine 25 mg.Results The blood pressure and heart rate of the control group was significantly higher than the other three groups,while the combined group was significantly lower than the diazepam and the promethazine groups.The sedative rating:Grade 0 of the four groups were:30,11,18,0 patients respectively;Grade 1 of the four groups were:0,21,15,24 patients respectively;Grade 2 of the four groups were:0,10,9,18 patients respectively;No patients were in grades 3 and 4.The anxiety score of the control group was significantly higher than the other three groups.There was no significant difference in complications among the four groups.Conclusion Diazepam and/or promethazine could be used effectively and safely during TACE,and they could reduce stress response of HCC patients during TACE,and improved tolerance of TACE.
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Objective:To establish an HPLC method for the determination of promethazine hydrochloride and glycyrrhizic acid in compound promethazine and glycyrrhizae oral solution. Methods:A Thermo BDS C18 column(250 mm × 4. 6 mm,5μm)was used with methanol-glacial acetic acid-0. 2 mol·L-1 ammonium acetate solution (58: 1: 41)as the mobile phase. The flow rate was 1. 0 ml· min-1 and the detection wavelength was 250 nm. The column temperature was ambient and the injection volume was 10 μl. Results:There was a good linear relationship within the concentration range of 0. 079 4-0. 317 6 mg · ml-1 ( r =0. 999 9 ) for promethazine hydrochloride and 0. 060 3-0. 241 1 mg · ml-1 ( r =0. 999 9 ) for glycyrrhizic acid. The average recovery was 99. 61% ( RSD =0. 32%, n=9) and 99. 30% (RSD=0. 59%, n=9), respectively. Conclusion: The method is simple, accurate and repeatable, which can be used to control the quality of the preparation.
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Objective:To establish a method for the simultaneous determination of content and uniformity of hydrochlorothiazide and promethazine hydrochloride in compound kendir leaves tablets I. Methods:An HPLC-UV wavelength switching method was adopt-ed. The separation was carried out on a YMC-Pack Pro-C18(250 mm × 4. 6 mm,5 μm)column with 0. 06 mol·L-1 potassium phos-phate monobasic solution(adjusting pH to 3. 0 with phosphoric acid )-methanol as the mobile phase with gradient elution. The flow rate was 1. 0 ml·min-1 , the column temperature was set at 35℃. During 0 to13 min, the detection wavelength was 271 nm, and during 13 to 25 min, the detection wavelength was 251nm. The injection volume was 10μl for content determination and 20μl for content uni-formity. Results:The linear range of hydrochlorothiazide and promethazine hydrochloride was 0. 255 9 ~2. 558 9 μg (r=0. 999 9) and 0. 175 1~1. 751 4 μg (r=0. 999 9) with the average recovery of 98. 06%(RSD=0. 64%, n=9)and 99. 61%(RSD=0. 53%, n=9), respectively. Conclusion:The method is simple, rapid, accurate and reproducible, which can provide a scientific basis for the quality control of compound kendir leaves tablets I.
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OBJECTIVE To explore the effect and underlying mechanism of promethazine(PMZ) on proarrhythmia in guinea pigs. METHODS ① InvivoECG recordings were made to analyze effects of jugular intravenous(iv)injection of PMZ on ECG in guinea pigs. PMZ was injected in this order:3.83→7.67→15.33→38.33 mg·kg-1 cumulatively. ② In vitroECG recordings were made to analyze effects of PMZ on ECG in isolated hearts of guinea pigs. PMZ was perfused in such order:0. 1 → 1 → 10 →50 μmol·L-1 . ③ L-type Ca2+ currents from ventricular myocytes in guinea pigs were recorded to investi-gate the PMZ's blocking effect. PMZ was perfused in such order:0.1→1→10→50 μmol·L-1→washout.④ hNav1.5 and hERG currents were recorded to investigate the PMZ's blocking effects. PMZ-perfused in such order:1→3→10→30 μmol·L-1 for hNav1.5 current analysis,and 0.3→1→3→10 μmol·L-1 for hERG current analysis. RESULTS ① PMZ(15.33 mg·kg-1 )significantly prolonged QRS intervals in guinea pigs invivoECG(P﹤0.05). PMZ(38.33 mg·kg-1 )prolonged QRS,QTc,and P-R intervals but reduced the heart rate( P﹤0.05). PMZ(10 μmol·L-1 )reduced the heart rate of isolated guinea pig hearts. PMZ 50 μmol·L-1 prolonged QRS and QTc intervals and further reduced the heart rate(P﹤0.05).③ PMZ inhibited the L-type Ca2+ current from ventricular myocytes in guinea pigs in a concentration-dependent manner with the lC50 of(8.9±1.0)μmol·L-1 . ④ PMZ inhibited the hNav1.5 and hERG currents in a concentration-dependent manner with the lC50 of 6.1±1.5 and(1.6±0.2)μmol·L-1 ,respectively. CONCLUSION PMZ might cause arrhythmia at overdoses and incombination with other drugs which have potential blocking effect on /Na ,Ca2+ and /kr currents. The proarrhythmic effect of PMZ might be mediated by the blocking effect on /Na ,Ca2+ and /kr currents.
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A new, sensitive, rapid, simple, specific and economical procedure has been developed for determination Promethazine HCl in phosphate buffer saline pH 7.4. The purpose of this analytical validation procedure is to determine a process of assessment and to validate it by laboratory experiments to prove that the method meets the minimum standard for laboratory use. This analytical method for the determination of Promethazine HCl in phosphate buffer saline pH 7.4 can be used to estimate the amount of promethazine HCl penetrated and dissolved in the blood vessels in vitro by penetration study. The method is based on the ultraviolet light absorbance at 251 nm which is the maximum wavelength of the concerned drug. This method can be succesfully applied for determination of drug in phosphate buffer saline pH 7.4 . The results of the analysis have been validated statistically and by recovery studies.
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Náusea e vômitos (NV) são os sintomas mais comuns durante a gravidez, geralmente iniciando-se entre a 6ª e a 8ª semana, atingindo a intensidade máxima em torno da 9ª semana e resolvendo-se até a 12ª semana. Embora sua etiologia seja, provavelmente, multifatorial, seu curso clínico se correlaciona com as concentrações plasmáticas da gonadotrofina coriônica humana. Por comprometerem a qualidade de vida, NV devem ser abordados com modificações dietéticas que incluem dieta fracionada e redução do consumo de alimentos gordurosos, entre outras. O uso de piridoxina pode melhorar a náusea de intensidade leve, embora não diminua significantemente os episódios de vômitos. Os anti-histamínicos são os medicamentos mais utilizados como terapia medicamentosa de primeira linha e têm sua segurança comprovada; dentre eles, o dimenidrinato determina início de ação mais rápido e menor sedação que a meclizina. Entre os antagonistas dopaminérgicos, a prometazina e a metoclopramida podem ser utilizadas, mas apresentam como desvantagem o potencial de eventos adversos maternos. O antagonista dos receptores 5-HT3, ondansetrona, pode ser considerado quando outros medicamentos não foram efetivos no tratamento de NV de intensidade grave. Do mesmo modo, os corticosteroides devem ter seu uso reservado para casos não responsivos a outros medicamentos e preferencialmente após a 10ª semana de gestação...
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Dimenhydrinate , Pregnancy , Meclizine , Nausea , Ondansetron , Pyridoxine , Promethazine , VomitingABSTRACT
A new, sensitive, rapid, simple, specific and economical procedure has been developed for determination Promethazine HCl in phosphate buffer saline pH 7.4. The purpose of this analytical validation procedure is to determine a process of assessment and to validate it by laboratory experiments to prove that the method meets the minimum standard for laboratory use. This analytical method for the determination of Promethazine HCl in phosphate buffer saline pH 7.4 can be used to estimate the amount of promethazine HCl penetrated and dissolved in the blood vessels in vitro by penetration study. The method is based on the ultraviolet light absorbance at 251 nm which is the maximum wavelength of the concerned drug. This method can be succesfully applied for determination of drug in phosphate buffer saline pH 7.4 . The results of the analysis have been validated statistically and by recovery studies.
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The objective of this study was to compare the efficacy and safety of cough mixture containing pholcodeine and promethazine - Tixylix (CS1) to a cough mixture which has noscapine, ammonium chloride, and sodium citrate (CS2) as its constituents in treatment of children suffering from dry cough. A total of 208 patients were enrolled at 4 sites. Of these, 179 (94 receiving CS1 and 99 receiving CS2) completed the study. Results of this study suggest that both the cough mixtures were comparable as per evaluation of their primary parameters. According to global assessment for efficacy and tolerability by parents on Day 7, Group CS1 performed better than CS2. It was also observed that no AE was reported in Group CS1 as compared to 2 AEs in Group CS2. To conclude, cough mixture combination of pholcodeine and promethazine - Tixylix exhibited efficacy and safety that was comparable with cough mixture which has noscapine, ammonium chloride, and sodium citrate. It was proven to be efficacious, safe and well tolerated in the select population.
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Ammonium Chloride/pharmacology , Ammonium Chloride/therapeutic use , Antitussive Agents/therapeutic use , Child , Child, Preschool , Citrates/analogs & derivatives , Citrates/pharmacology , Citrates/therapeutic use , Codeine/analogs & derivatives , Codeine/pharmacology , Codeine/therapeutic use , Cough/drug effects , Cough/drug therapy , Drug Combinations , Female , Humans , Male , Morpholines/analogs & derivatives , Morpholines/pharmacology , Morpholines/therapeutic use , Multicenter Studies as Topic , Noscapine/pharmacology , Noscapine/therapeutic use , Promethazine/analogs & derivatives , Promethazine/pharmacology , Promethazine/therapeutic use , Randomized Controlled Trials as Topic , Treatment OutcomeABSTRACT
Objectives To explore the brain white matter integrity among the patients with buprenorphine tables,scopolamine and promethazine solution(BSP) dependence after abstinence.Methods BSP-dependent patients( n=16)and age/eduction-matched healthy control subjects ( n=18) were assessed by diffusion tensor imaging (DTI) after 3 days,1 month and 2 months of abstinence.White matter (WM) integrity was measured with DTI as fractional anisotropy ( FA),an index of intravoxel orientational coherence of white matter fibers.Results Compared with health controls,FA values were significantly lower in frontal,parietal,temporal and corpus callosum in the BSP addicts after 3-day withdrawal (P＜0.001,uncorrected).Increased FA values in left superior frontal cortex,right medial frontal gyms and fight inferior parietal gyrus were found in BSP users after 2 months of abstinence (P ＜0.001,uncorrected).However,no significant difference was found between these BSP addicts after 1-month abstince.Compared with health controls,BSP dependent subjects still exhibited significantly lower FA in the corpus callosum,frontal,parietal and temporal WM after 2-month withdrawal (P ＜ 0.001,uncorrected ).Conclusion The abnormalities showed less recovery in BSP dependent individuals with abstinence in white matter that suggests that rehabilitation time should be further prolonged for BSP addicts and emphasis cognitive-behavioral therapy to assist BSP abusers rebuild social functions.
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Aim To observe the effects of promethazine on the analgesia,hypnosis,amnesia and therapeutic index of isoflurane.Methods The experiments were designed to study promethazine on the analgesic effect of isoflurane by hot-plate test and writhing test,and to study the effect of promethazine on the sleeping time of isoflurane by the method of righting reflex,and the amnesia of isoflurane by Morris water maze,and the ED_(50),LD_(50) by sequential method in mice.Results The result of hot-plate test and writhing test indicated that promethazine could enhance the analgesic effect of isoflurane(P＜0.05 or P＜0.01);through the experiment of righting reflex, sleeping time of isoflurane in mice was extended by promethazine(P＜0.01);in Morris water maze experiment, the average latency in the combination of promethazine and isoflurane was longer than that of the promethazine group or isoflurane group(P＜0.05 or P＜0.01), while aiming to the residence time, the combination of the two was shorter than that in the third quadrant(P＜0.01 or P＜0.05),the TCPP of the group of isoflurance was more than that of the combination group;promethazine could decrease the ED_(50) of isoflurance(P＜0.01),but it did not obviously affect its LD_(50)(P＞0.05).Conclusion Promethazine can not only reinforce the effect of isoflurance on analgesia,hypnosis and amnesia, but also boost the therapeutic index of isoflurance.
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The present study investigated a novel extended release system of promethazine hydrochloride (PHC) with acrylic polymers Eudragit RL100 and Eudragit S100 in different weight ratios (1:1 and 1: 5), and in combination (0.5+1.5), using freeze-drying and spray-drying techniques. Solid dispersions were characterized by Fourier-transformed infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), Powder X-ray diffractometry (PXRD), Nuclear magnetic resonance (NMR), Scanning electron microscopy (SEM), as well as solubility and in vitro dissolution studies in 0.1 N HCl (pH 1.2), double-distilled water and phosphate buffer (pH 7.4). Adsorption tests from drug solution to solid polymers were also performed. A selected solid dispersion system was developed into capsule dosage form and evaluated for in vitro dissolution studies. The progressive disappearance of drug peaks in thermotropic profiles of spray-dried dispersions were related to increasing amount of polymers, while SEM studies suggested homogenous dispersion of drug in polymer. Eudragit RL100 had a greater adsorptive capacity than Eudragit S100, and thus its combination in (0.5+1.5) for S100 and RL 100 exhibited a higher dissolution rate with 97.14 percent drug release for twelve hours. Among different formulations, capsules prepared by combination of acrylic polymers using spray-drying (1:0.5 + 1.5) displayed extended release of drug for twelve hours with 96.87 percent release followed by zero order kinetics (r²= 0.9986).
O presente trabalho compreendeu estudo de um novo sistema de liberação prolongada de cloridrato de prometazina (PHC) com polímeros acrílicos Eudragit RL100 e Eudragit S100 em diferentes proporções em massa (1:1 e 1:5) e em combinação (0,5+1,5), utilizando técnicas de liofilização e de secagem por aspersão As dispersões sólidas foram caracterizadas por espectrofotometria no infravermelho por transformada de Fourier (FT-IR), calorimetria diferencial de varredura (DSC), difratometria de raios X (PXRD), Ressonância Magnética Nuclear (RMN), microscopia eletrônica de varredura (SEM) e, também, por estudos de solubilidade e de dissolução in vitro em HCl 0,1 N (pH 1,2), água bidestilada e tampão fosfato (pH 7,4). Realizaram-se, também, testes de adsorção da solução do fármaco nos polímeros sólidos. Desenvolveu-se sistema de dispersão sólida exclusiva dentro das cápsulas, que foi avaliado por meio de estudos de dissolução in vitro. Relacionou-se o desaparecimento progressivo de picos do fármaco em perfis termotrópicos de dispersões secas por spray à quantidade aumentada de polímero, enquanto os estudos de SEM sugeriram dispersão homogênea do fármaco no polímero. O Eudragit RL100 apresentou maior capacidade de adsorção do que o Eudragit S100 e, dessa forma, a combinação de (0,5+1,5) para S100 e para RL100 mostrou taxa de dissolução maior, com liberação de 94,17 por cento de fármaco em 12 horas. Entre as várias formulações, as cápsulas preparadas pela combinação de polímeros acrílicos utilizando secagem por aspersão (0,5+1,5) apresentou liberação prolongada do fármaco em 12 horas, com 96,78 por cento de liberação, seguindo cinética de ordem zero (r² = 0,9986).
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Hydrochloric Acid/pharmacokinetics , Chemistry, Pharmaceutical , Delayed-Action Preparations , Polymers/pharmacokinetics , Organic Chemistry Phenomena , Promethazine/pharmacokinetics , Drug Evaluation , Freeze Drying , Pharmaceutical PreparationsABSTRACT
OBJETIVO: A tranquilização farmacológica rápida e segura de episódios de agitação/agressividade é muitas vezes inevitável. Esta revisão investiga a efetividade da combinação haloperidol e prometazina intramuscular, muito utilizada no Brasil. MÉTODO: Através de busca nos registros do Cochrane Schizophrenia Group, foram incluídos todos os ensaios clínicos nos quais a combinação haloperidol e prometazina foi avaliada em pacientes agressivos com psicose. Todos os estudos relevantes foram avaliados quanto à qualidade e tiveram seus dados extraídos de forma confiável. RESULTADOS: Foram identificados quatro estudos relevantes de alta qualidade. A combinação haloperidol e prometazina foi comparada com midazolam, lorazepam, haloperidol isolado e olanzapina, todos administrados por via intramuscular. No Brasil, a combinação foi efetiva, com mais de 2/3 dos pacientes tranquilos em 30 minutos, mas midazolam foi mais rápido. Na Índia, comparado a lorazepam, a combinação haloperidol e prometazina foi mais efetiva. Após as primeiras horas, as diferenças foram negligenciáveis. O uso de haloperidol isolado acarretou maior incidência de efeitos adversos. Olanzapina promove tranquilização tão rapidamente quanto a combinação, mas não tem efeito tão duradouro e mais pessoas necessitaram medicação adicional nas quatro horas subseqüentes. CONCLUSÃO: Todos os medicamentos avaliados são eficazes, mas esta revisão demonstra vantagens no uso da combinação haloperidol e prometazina.
OBJECTIVE: Rapid and safe tranquillisation is sometimes unavoidable. We conducted this systematic review to determine the value of the combination haloperidol plus promethazine, frequently used in Brazil. METHOD: We searched the Cochrane Schizophrenia Group's Register and included all randomised clinical trials involving aggressive people with psychosis for which haloperidol plus promethazine was being used. We reliably selected, quality assessed and extracted data from all relevant studies. RESULTS: We identified four relevant high quality studies. The combination haloperidol plus promethazine mix was compared with midazolam, lorazepam, haloperidol alone and olanzapine Intramuscular. In Brazil, haloperidol plus promethazine was effective with over 2/3 of people being tranquil by 30 minutes, but midazolam was more swift and in India, compared with lorazepam, the combination was more effective. Over the next few hours reported differences are negligible. Haloperidol given without promethazine in this situation causes frequent serious adverse effects. Olanzapine is as rapidly tranquillising as haloperidol plus promethazine, but did not have an enduring effect and more people needed additional drugs within 4 hours. CONCLUSION: All treatments evaluated are effective, but this review provides compelling evidence as to clear advantages of the haloperidol plus promethazine combination.