Neuroleptic drug treatment
P. J. McKenna in Schizophrenia and Related Syndromes, 2007
As recounted by Caldwell (1970), the story of how schizophrenia became a treatable illness began with a French surgeon, Laborit. In the course of testing the usefulness of various compounds for combating the adverse autonomic and psychological consequences of surgery, he observed that an antihistamine, promethazine, tended to induce a state of calm, quiet, relaxation in volunteers. His attempts to maximise this effect by pharmacological manipulation resulted in the synthesis of chlorpromazine, a drug that reliably produced ‘not any loss of consciousness, not any change in the patient’s mentality, but a slight tendency to sleep and, above all, disinterest for all that goes on around him’ (Laborit et al., 1952). Laborit immediately recognised the potential of this effect and managed to persuade some reluctant psychiatric colleagues to try it on psychotic patients. Successes in individual cases were quickly followed by the now classic report on a small series of patients by Delay et al. (1952).
Neuroregulators and Pain
Barry Stimmel in Pain and Its Relief Without Addiction, 1997
The major tranquilizers, antipsychotic, or neuroleptic drugs are utilized mainly in the treatment of psychoses. The absorption of these drugs from the gastrointestinal tract is influenced by many factors, including individual variability, dose, presence of food in the stomach, and simultaneous use of antacids. The phenothiazines affect all areas of the central nervous system through their ability to block postsynaptic dopamine receptors interfering with dopamine-mediated neurotransmission. The ability of phenothiazines to serve as effective alpha blockers assumes importance in the treatment of chlorpromazine-induced hypotension. Methotrimeprazine is a phenothiazine derivative specifically marketed as an injectable analgesic for moderate to severe pain. The phenothiazines may induce the hepatic endoplasmic reticulum, affecting metabolism of other drugs detoxified by this system. The neuroleptics, with the exception of methothimeprazine have consistently not been found to be primary analgesics. Promethazine can enhance morphine analgesia, relieve anxiety, and diminish postoperative nausea. It is therefore prescribed with opioids in surgical patients.
Histamine and antihistamines
Alan Galbraith, Shane Bullock, Elizabeth Manias, Barry Hunt, Ann Richards in Fundamentals of Pharmacology, 2007
Injection of the antihistamines chlorphenamine (chlorpheniramine) or promethazine is used as an adjunct to adrenaline to stop further histaminic action. Corticosteroids are often given to stabilise the immunologic cells causing the problem (see Chapter 58). Corticosteroids take at least 30 minutes to produce an effect and several hours to reach maximum activity and so are given last and help to prevent delayed reactions.
The risk of fractures, acute myocardial infarction, atrial fibrillation and ventricular arrhythmia in geriatric patients exposed to promethazine
Published in Expert Opinion on Drug Safety, 2020
Maurizio Sessa, Annamaria Mascolo, Kim Peder Dalhoff, Morten Andersen
Objectives: This study aimed to compare the risk of fractures, acute myocardial infarction, atrial fibrillation, and ventricular arrhythmia among Danish citizens aged ≥ 65 which were new users of promethazine or domperidone, triazolam, loratadine, and betahistine. Secondly, the study aimed to perform a risk stratification to identify the most relevant predictors for the study outcomes. Methods: The study period was 01/01/2015 to 31/12/2016. The data sources were the Danish registers. Each patient was followed for 90 days. A logistic regression model was used to compute the unadjusted and adjusted odds ratios (OR), and a conditional inference tree was used to identify the most relevant predictors for the study outcomes. Results: Promethazine had a higher risk of hospitalization for atrial fibrillation than loratadine and betahistine (OR 1.58; 95% CI 1.07–2.63 and OR 3.22; 95% CI 1.69–7.14, respectively). For fractures, acute myocardial infarction, and ventricular arrhythmia hospitalizations, no statistically significant differences were found among drugs under investigation. The medical history of cardiac arrhythmia (OR 4.14; 95% CI 2.94–5.78, p
Chronic promethazine misuse and the possibility of dependence: a brief review of antihistamine abuse and dependence
Published in Journal of Substance Use, 2013
Stephen D. Parker, Angelo De Gioannis, Colin Page
Objective: Misuse of centrally acting antihistamines is potentially a significant under-recognised issue contributing to problems of abuse and dependence, with the potential to complicate management of other mental disorders. This article considers this problem with the aim of increasing practitioner awareness. Method: This article considers the literature relating to abuse of centrally acting antihistamines and presents a unique case, with features suggesting of psychological and physiological dependence following prolonged misuse of promethazine. Results: Increased understanding of the potential problem of centrally acting antihistamine abuse and consideration of the possibility of a dependence syndrome associated with promethazine. Conclusions: The need for vigilance for abuse potential of promethazine and other centrally acting antihistamines by doctors and pharmacists is emphasised.
A Validated HPLC Method for Separation and Determination of Promethazine Enantiomers in Pharmaceutical Formulations
Published in Drug Development and Industrial Pharmacy, 2009
Ola A. Saleh, Aida A. El-Azzouny, Hassan Y. Aboul-Enein, Amr M. Badawy
A simple, rapid, and validated method for separation and determination of promethazine enantiomers was developed. Promethazine was separated and quantitated on a Vancomycin Chirobiotic V column (250 × 4.6 mm), using a mixture of methanol, acetic acid, and triethylamine (100:0.1:0.1%, by volume) as a mobile phase at 20°C and at a flow rate of 1 mL/min. The UV-detector was set to 254 nm. Acetyl salicylic acid (Aspirin®) was used as an internal standard. The applied HPLC method allowed separation and quantification of promethazine enantiomers with good linearity (r > .999) in the studied range. The relative standard deviations (RSD) were 0.29 and 0.36 for the promethazine enantiomers with accuracy of 100.06 and 100.08. The limit of detection and limit of quantification of promethazine enantiomers were found to be 0.04 and 0.07 μg/mL, respectively. The method was validated through the parameters of linearity, accuracy, precision, and robustness. The HPLC method was applied for the quantitative determination of promethazine in pharmaceutical formulations.
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