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1.
Artículo en Inglés | MEDLINE | ID: mdl-39229983

RESUMEN

BACKGROUND: Hypogalactia and agalactia in lactating mothers are the major causes of child malnutrition, mortality, morbidity, and overall ill health. The development of such treatments requires a well-designed preclinical study with suitable laboratory animals, which needs to be improved. Thus, a suitably designed study with a laboratory animal to analyse galactagogue activity, along with an assessment of the quality and quantity of milk, is required. OBJECTIVES: This study aimed to evaluate the potential of rabbits as an animal model for studying lactogenic activity. METHODS: The structural homology of prolactin, prolactin, and prolactin in humans, rabbits, and rats was studied using BLAST and PyMol to assess similarity in the lactogenic system. Daily and cumulative milk production and pre-treatment (control) and post-treatment (three drugs) in rabbits were recorded and evaluated by analysing protein, fat, lactose, solid non-fat, and ash values. All parameters were recorded on the 0th day and at the end of weeks 1, 2, and 3. Mammary gland histopathology was performed to evaluate the effects on mammary glands. RESULTS: Homology studies revealed that the sequences of the human and rabbit prolactin genes, receptors, and hormones had a high similarity index. Treatment with Domperidone, Metoclopramide, and Shatavari significantly enhanced milk production by enhancing prolactin secretion; only Shatavari increased milk nutrition. Enlargement of the tubuloalveolar ducts of the mammary glands was observed. CONCLUSION: Our findings suggest that rabbits are robust, reproducible, ethically superior, and preclinically relevant animals for assessing lactogenic activity.

2.
Vet Anaesth Analg ; 51(5): 500-509, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-39142985

RESUMEN

OBJECTIVE: To assess whether adding metoclopramide to a protocol of maropitant and pantoprazole would reduce incidence of ptyalism, vomiting and regurgitation in brachycephalic dogs undergoing thoracolumbar spinal surgery. STUDY DESIGN: Randomized blinded controlled trial. ANIMALS: A total of 43 brachycephalic dogs undergoing thoracolumbar spinal surgery. METHODS: In addition to a standardized anaesthetic regimen, dogs were randomized to be administered either a 2 mg kg-1 day-1 metoclopramide constant rate infusion (CRI) or a saline solution at an equivalent infusion rate, started after anaesthetic induction and discontinued 5 hours after tracheal extubation. The presence of vomiting, regurgitation and pytalism, and short form of the Glasgow Composite Pain Scale pain scores were assessed by a blinded observer hourly for 4 hours, starting 1 hour postextubation. RESULTS: Regurgitation occurred in six dogs postoperatively; three dogs were in the placebo group and three in the metoclopramide group. The odds ratio (OR) of regurgitation after surgery did not differ between groups [OR: 0.76, 95% confidence interval (CI): 0.13-4.3, p = 0.76]. The odds of observing ptyalism at 3 and 4 hours was approximately 15 times less than 1 hour postoperatively (both OR: 15.4, 95% CI: 1.8-130.7, p = 0.012) and did not differ based on the addition of metoclopramide (OR: 0.73, 95% CI: 0.07-8.0, p = 0.79). The odds of observing pain did not change over time and did not differ based on the addition of metoclopramide (OR: 0.71, 95% CI: 0.12-4.2, p = 0.71). Vomiting did not occur during the study (0.0%, 95% CI: 0.0-8.2%). No adverse effects were observed during the study period in either group. CONCLUSIONS AND CLINICAL RELEVANCE: The addition of a metoclopramide CRI to maropitant and pantoprazole did not result in a significant reduction in ptyalism or regurgitation in brachycephalic dogs undergoing thoracolumbar spinal surgery.


Asunto(s)
Antieméticos , Enfermedades de los Perros , Metoclopramida , Animales , Perros , Metoclopramida/administración & dosificación , Metoclopramida/uso terapéutico , Antieméticos/administración & dosificación , Antieméticos/uso terapéutico , Masculino , Femenino , Enfermedades de los Perros/cirugía , Enfermedades de los Perros/prevención & control , Craneosinostosis/cirugía , Craneosinostosis/veterinaria , Náusea y Vómito Posoperatorios/veterinaria , Náusea y Vómito Posoperatorios/prevención & control , Reflujo Laringofaríngeo/veterinaria , Reflujo Laringofaríngeo/prevención & control , Quinuclidinas/administración & dosificación , Quinuclidinas/uso terapéutico , Pantoprazol/administración & dosificación , Pantoprazol/uso terapéutico , Pantoprazol/farmacología
3.
Stroke ; 2024 Aug 12.
Artículo en Inglés | MEDLINE | ID: mdl-39129650

RESUMEN

BACKGROUND: A randomized trial suggested that treatment with metoclopramide reduces the risk of pneumonia in patients with acute stroke and a nasogastric tube. We assessed whether this finding could be replicated in a post hoc analysis of the randomized PRECIOUS trial (Prevention of Complications to Improve Outcome in Elderly Patients With Acute Stroke). METHODS: PRECIOUS was an international, 3×2 partial-factorial, randomized controlled, open-label clinical trial with blinded outcome assessment assessing preventive treatment with metoclopramide, paracetamol, and ceftriaxone in patients aged ≥66 years with acute ischemic stroke or intracerebral hemorrhage and a National Institutes of Health Stroke Scale score ≥6. In the present study, we analyzed patients who had a nasogastric tube within 24 hours after randomization. Patients who were allocated to metoclopramide (10 mg TID) were compared with patients who were not. Treatment was started within 24 hours after symptom onset and continued for 4 days or until discharge if earlier. The primary outcome was pneumonia in the first week after stroke. The score on the modified Rankin Scale after 90 days was a secondary outcome and analyzed with ordinal logistic regression. RESULTS: From April 2016 through June 2022, a total of 1493 patients were enrolled with 1376 included in this analysis, of whom 1185 (86%) had ischemic stroke and 191 (14%) had intracerebral hemorrhage. The first day after randomization, 329 (23.9%) patients had a nasogastric tube, of whom 156 were allocated to metoclopramide and 173 to standard care. Metoclopramide was not associated with a reduction of pneumonia (41.0% versus 35.8%; adjusted odds ratio, 1.35 [95% CI, 0.79-2.30]) or with poor functional outcome (adjusted odds ratio, 1.07 [95% CI, 0.71-1.61]). CONCLUSIONS: In patients with stroke who had a nasogastric tube shortly after stroke onset, metoclopramide for 4 days did not reduce pneumonia or have an effect on the functional outcome.

4.
Expert Opin Drug Saf ; : 1-7, 2024 Aug 08.
Artículo en Inglés | MEDLINE | ID: mdl-39086080

RESUMEN

BACKGROUND: This study evaluated the pharmacokinetic interactions of orally administered chloroquine and metoclopramide. METHODS: The study employed a randomized and two-phase cross-over design with 4-week washout plan. Twelve healthy male volunteers were shortlisted according to the set criteria and were administered with metoclopramide 10 mg PO and chloroquine (a total of 1500 mg) at different intervals which were (500 mg at 0, 6, and 24 h). The concentration of chloroquine and metoclopramide in the blood samples was estimated using a validated HPLC-UV technique to affirm the maximum concentration (Cmax), time to reach Cmax (Tmax), and area under the curve (AUC). RESULTS: Cmax, T1/2, and AUC of metoclopramide were increased up to 20, 10, and 47.8%, respectively, by the concomitantly administering Chloroquine. Chloroquine-treated phase showed increased values of Cmax (ng/ml), AUC (ng.h/ml), and T½ (h), i.e. 41.35 ± 1.61, 504.12 ± 66.25, and 5.72 ± 2.63, as compared to that reference phase i.e. 34.52 ± 4.92, 341.14 ± 112.8, and 5.19 ± 1.14, respectively. CONCLUSIONS: Chloroquine was found to attenuate CYP2D6 activity in healthy Pakistani male volunteers. Hence, patients that are prescribed with metoclopramide or other CYP2D6-substrate drugs require a dose adjustment when administered with chloroquine.

5.
Expert Rev Gastroenterol Hepatol ; 18(7): 389-395, 2024 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-38995209

RESUMEN

BACKGROUND: We aimed to examine the common adverse drug reactions (ADRs) of metoclopramide, FDA-approved for treating many gastrointestinal conditions including gastroparesis, and prucalopride, FDA-approved for treating chronic idiopathic constipation but used off-label for other gastrointestinal conditions including gastroparesis. RESEARCH DESIGN AND METHODS: The FDA Adverse Event Reporting System (FAERS) was analyzed from January 2013 to December 2023. ADR reports regarding use of only metoclopramide or prucalopride were analyzed following exclusion of reports indicating use for treatment of non-gastrointestinal conditions. RESULTS: Analysis of 1,085 reports on metoclopramide revealed tardive dyskinesia (n = 393, 36.2%) and dystonia (n = 170, 15.7%) among the most reported ADRs in addition to QTc prolongation (n = 16, 1.5%) with progression to Torsade de pointes (n = 5, 0.5%) and triggering of pheochromocytoma crisis (n = 24, 2.2%). Analysis of 865 reports on prucalopride revealed headache (n = 120, 13.9%), diarrhea (n = 116, 13.4%), and abdominal pain (n = 100, 11.6%) as the most common ADRs with 22 reports (2.5%) of dystonia with the use of prucalopride. CONCLUSIONS: This FAERS database analysis shows post-marketing reports of ADRs from metoclopramide most frequently include tardive dyskinesia, dystonia, and tremor in addition to potentially fatal arrhythmias such as Torsade de pointes. Consumers of prucalopride may also be at risk of dystonia and other ADRs.


Asunto(s)
Sistemas de Registro de Reacción Adversa a Medicamentos , Benzofuranos , Gastroparesia , Metoclopramida , United States Food and Drug Administration , Humanos , Metoclopramida/efectos adversos , Metoclopramida/uso terapéutico , Gastroparesia/tratamiento farmacológico , Gastroparesia/inducido químicamente , Estados Unidos , Benzofuranos/efectos adversos , Benzofuranos/uso terapéutico , Masculino , Femenino , Persona de Mediana Edad , Adulto , Anciano , Adulto Joven , Bases de Datos Factuales , Adolescente , Antagonistas de los Receptores de Dopamina D2/efectos adversos , Discinesia Tardía/inducido químicamente , Discinesia Tardía/tratamiento farmacológico
6.
Pharmaceutics ; 16(7)2024 Jul 19.
Artículo en Inglés | MEDLINE | ID: mdl-39065656

RESUMEN

New co-processed excipients comprising lactose (filler and sweetener), microcrystalline cellulose (MCC, filler), and low-substituted hydroxypropyl cellulose (L-HPC, disintegrant and binder) were developed via solvent evaporation for the preparation of metoclopramide orally disintegrating tablets (MCP ODTs). Single-factor and Box-Behnken experimental designs were employed to optimize the formulation. The optimized formulation ratios were water: MCC: lactose (g/g) = 17.26:2.79:4.54:1. The results demonstrated that particles formed by solvent evaporation had superior flowability and compressibility compared to the physical mixture. Tablets compressed with these co-processed excipients exhibited a significantly reduced disintegration time of less than 25 s and achieved complete dissolution within 5 min. Pharmacokinetic studies revealed that MCP ODTs significantly improved Cmax, which was 1.60-fold higher compared to conventional tablets. In summary, the lactose/L-HPC/MCC triple-based co-processed excipients developed in this study are promising and could be successfully utilized in orally disintegrating and fast-release tablets.

7.
Expert Opin Drug Metab Toxicol ; 20(6): 473-489, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38878283

RESUMEN

INTRODUCTION: Dopamine (D)2,3-receptor antagonists (RAs) were the first antiemetics used in the prophylaxis of chemotherapy-induced nausea and vomiting (CINV). AREAS COVERED: Eight D2,3-RAs, amisulpride, domperidone, droperidol, haloperidol, metoclopramide, metopimazine, olanzapine and prochlorperazine are reviewed focusing on pharmacokinetics, pharmacodynamics, antiemetic effect and side effects. EXPERT OPINION: Since the introduction of D2,3-RAs, antiemetics such as corticosteroids, 5-hydroxytryptamine (5-HT)3-RAs and neurokinin (NK)1-RAs have been developed. The classical D2,3-RAs are recommended in the prophylaxis of CINV from low emetic risk chemotherapy, but not as a fixed component of an antiemetic regimen for moderately or highly (HEC) emetic risk chemotherapy. D2,3-RAs are also used in patients with breakthrough nausea and vomiting. It should be emphasized, that most of these drugs are not selective for dopamine receptors.The multi-receptor targeting agent, olanzapine, is recommended in the prophylaxis of HEC-induced CINV as part of a four-drug antiemetic regimen, including a 5-HT3-RA, dexamethasone and a NK1-RA. Olanzapine is the most effective agent to prevent chemotherapy-induced nausea.Side effects differ among various D2,3-RAs. Metopimazine and domperidone possess a low risk of extrapyramidal side effects. Domperidone and metoclopramide are prokinetics, whereas metopimazine delays gastric emptying and haloperidol does not influence gastric motility. Many D2,3-RAs increase the risk of prolonged QTc interval; other side effects include sedation and orthostatic hypotension.


Asunto(s)
Antieméticos , Antineoplásicos , Antagonistas de Dopamina , Náusea , Vómitos , Humanos , Náusea/inducido químicamente , Náusea/prevención & control , Vómitos/inducido químicamente , Vómitos/prevención & control , Antieméticos/farmacología , Antieméticos/farmacocinética , Antieméticos/administración & dosificación , Antieméticos/efectos adversos , Antineoplásicos/efectos adversos , Antineoplásicos/farmacocinética , Antineoplásicos/administración & dosificación , Antagonistas de Dopamina/efectos adversos , Antagonistas de Dopamina/farmacología , Antagonistas de Dopamina/farmacocinética , Antagonistas de Dopamina/administración & dosificación , Animales , Antagonistas de los Receptores de Dopamina D2/efectos adversos , Antagonistas de los Receptores de Dopamina D2/farmacología , Receptores de Dopamina D3/antagonistas & inhibidores
8.
Saudi Pharm J ; 32(5): 102039, 2024 May.
Artículo en Inglés | MEDLINE | ID: mdl-38558884

RESUMEN

Background: Metoclopramide and domperidone are prokinetic agents commonly used to treat gastrointestinal dysmotility disorders. This study aimed to evaluate the safety and associated side effects of prolonged-use metoclopramide and domperidone as treatment for chronic gastrointestinal dysmotility disorders in patients with systemic sclerosis (SSc). Methods: A quantitative observational survey was conducted by interview questionnaire in rheumatology outpatients at a tertiary teaching hospital in Riyadh, Saudi Arabia. The study included all patients aged 25-80 years diagnosed with SSc. All patients were on metoclopramide or domperidone for the treatment of chronic gastrointestinal dysmotility symptoms over at least 12 weeks. Results: Eighteen eligible patients were included. Most study participants were diagnosed with SSc complicated by interstitial lung disease (n = 13; 72.2 %). The most frequently reported side effect that occurred while taking prokinetic drugs was shortness of breath (n = 12; 66.7 %). None of the participants reported experiencing depression, galactorrhea, or syncope. CNS side effects were reported in 5.6 %. There were no differences in side effects based on the type and dosage of prokinetic drug used. Conclusions: Use of metoclopramide and domperidone for the treatment of chronic gastrointestinal dysmotility in SSc patients for 12 weeks or longer was not associated with any troublesome side effects. Further studies with more participants are needed to confirm our findings.

9.
Sci Rep ; 14(1): 8765, 2024 04 16.
Artículo en Inglés | MEDLINE | ID: mdl-38627518

RESUMEN

Green spectrophotometric and HPLC methods have been developed for the quantification of metoclopramide. In the spectrophotometric method, it was determined by direct absorbance measurement at 273 nm wavelength using ultrapure water as solvent. The Extend C18 column was used for the HPLC method. The mobile phase system consisted of a combination of ethanol and formic acid solution (pH 2.0; 30:70 v/v). Isocratic elution was applied and the flow rate was set at 1.0 mL min-1. Metoclopramide was detected at 273 nm. The methods performed were economical, rapid, environmentally friendly, and simple, providing metoclopramide analysis within 5 min. The methods have been successfully applied in pharmaceutical products without matrix interference. The results of the application of the developed methods to pharmaceutical products were statistically compared and no significant difference was observed between the methods. In addition, the greenness assessment of the developed methods was performed using AGREE software. Our developed methods, based on the use of solvents such as ethanol and water, are proposed as a more environmentally and analyst-friendly option for the quantification of metoclopramide in pharmaceutical products than other methods currently in use.


Asunto(s)
Etanol , Metoclopramida , Cromatografía Líquida de Alta Presión/métodos , Metoclopramida/análisis , Agua , Preparaciones Farmacéuticas
10.
Expert Opin Pharmacother ; 25(5): 541-549, 2024 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-38629943

RESUMEN

INTRODUCTION: Gastroparesis is a chronic disorder characterized by decreased gastric emptying and presents with nausea, vomiting, and abdominal pain which impacts patients' quality of life greatly. The treatment modalities available for gastroparesis have been expanding over the past 2 decades. Currently, there are multiple options available for gastroparesis, albeit with only one FDA-approved medication until June 2021. AREAS COVERED: We review the different treatments available for gastroparesis and discuss the recently FDA-approved intranasal formulation of metoclopramide. This nasal spray guarantees metoclopramide absorption within 15 min of application bypassing first pass metabolism in the liver and overcoming the limitations of the oral formulation not passing into the small intestine for absorption because of a gastroparetic stomach or a patient unable to take the oral metoclopramide because of nausea and vomiting. EXPERT OPINION: We now find ourselves in an oasis after spending many years in a 'desert' regarding pharmacologic therapies available for gastroparesis. The expansion of the research involving dopamine receptor antagonists and delving into alternative mechanisms of alleviating gastroparesis symptoms has been crucial in the landscape of gastroparesis. This is especially true as our knowledge of gastroparesis has proven that simply improving gastric emptying does not necessarily translate to clinical improvement.


Asunto(s)
Vaciamiento Gástrico , Gastroparesia , Calidad de Vida , Humanos , Administración Intranasal , Antagonistas de Dopamina/uso terapéutico , Vaciamiento Gástrico/efectos de los fármacos , Fármacos Gastrointestinales/uso terapéutico , Fármacos Gastrointestinales/farmacología , Fármacos Gastrointestinales/administración & dosificación , Gastroparesia/tratamiento farmacológico , Gastroparesia/fisiopatología , Metoclopramida/uso terapéutico
11.
Life (Basel) ; 14(4)2024 Apr 19.
Artículo en Inglés | MEDLINE | ID: mdl-38672796

RESUMEN

BACKGROUND: Peptic ulcer disease (PUD) can cause upper gastrointestinal bleeding (UGIB), often needing esophagogastroduodenoscopy (EGD). Second-look endoscopies verify resolution, but cost concerns prompt research on metoclopramide's efficacy compared to erythromycin. METHODS: We analyzed the Diamond Network of TriNetX Research database, dividing UGIB patients with PUD undergoing EGD into three groups: metoclopramide, erythromycin, and no medication. Using 1:1 propensity score matching, we compared repeat EGD, post-EGD transfusion, and mortality within one month in two study arms. RESULTS: Out of 97,040 patients, 11.5% received metoclopramide, 3.9% received erythromycin, and 84.6% received no medication. Comparing metoclopramide to no medication showed no significant difference in repeat EGD (10.1% vs. 9.7%, p = 0.34), transfusion (0.78% vs. 0.86%, p = 0.5), or mortality (1.08% vs. 1.08%, p = 0.95). However, metoclopramide had a higher repeat EGD rate compared to erythromycin (9.4% vs. 7.5%, p = 0.003), with no significant difference in transfusion or mortality. CONCLUSIONS: The need to repeat EGD was not decreased with pre-EGD use of metoclopramide. If a prokinetic agent is to be used prior to EGD, erythromycin shows superior reduction in the need of repeat EGD as compared to metoclopramide.

12.
Sci Rep ; 14(1): 7598, 2024 03 31.
Artículo en Inglés | MEDLINE | ID: mdl-38556533

RESUMEN

Acute upper gastrointestinal hemorrhage (UGIH) is the most common emergency condition that requires rapid endoscopic treatment. This study aimed to evaluate the effects of pre-endoscopic intravenous metoclopramide on endoscopic mucosal visualization (EMV) in patients with acute UGIH. This was a multicenter, randomized, double-blind controlled trial of participants diagnosed with acute UGIH. All participants underwent esophagogastroduodenoscopy within 24 h. Participants were assigned to either the metoclopramide or placebo group. Modified Avgerinos scores were evaluated during endoscopy. In total, 284 out of 300 patients completed the per-protocol procedure. The mean age was 62.8 ± 14.3 years, and 67.6% were men. Metoclopramide group achieved a higher total EMV and gastric body EMV score than the other group (7.34 ± 1.1 vs 6.94 ± 1.6; P = 0.017 and 1.80 ± 0.4 vs 1.64 ± 0.6; P = 0.006, respectively). Success in identifying lesions was not different between the groups (96.5% in metoclopramide and 93.6% in placebo group; P = 0.26). In the metoclopramide group, those with active variceal bleeding compared with the control group demonstrated substantial improvements in gastric EMV (1.83 ± 0.4 vs 1.28 ± 0.8, P = 0.004), antral EMV (1.96 ± 0.2 vs 1.56 ± 0.6, P = 0.003), and total EMV score (7.48 ± 1.1 vs 6.2 ± 2.3, P = 0.02). Pre-endoscopic intravenous metoclopramide improved the quality of EMV in variceal etiologies of UGIH, which was especially prominent in those who had signs of active bleeding based on nasogastric tube assessment.Trial Registration: Trial was registered in Clinical Trials: TCTR 20210708004 (08/07/2021).


Asunto(s)
Várices Esofágicas y Gástricas , Hemorragia Gastrointestinal , Masculino , Humanos , Persona de Mediana Edad , Anciano , Femenino , Hemorragia Gastrointestinal/etiología , Metoclopramida/uso terapéutico , Várices Esofágicas y Gástricas/complicaciones , Endoscopía Gastrointestinal/efectos adversos , Administración Intravenosa , Método Doble Ciego
13.
Cureus ; 16(2): e53754, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-38327722

RESUMEN

Restless leg syndrome (RLS) is a chronic disorder characterized by a compulsive urge to move the legs, accompanied by various subjective symptoms and a distinctive nyctimeral pattern. A negligent entity is drug-induced RLS, which may be challenging to recognize by practitioners due to its rarity. Among various drugs that can induce or exacerbate RLS, metoclopramide is notable; however, the literature primarily describes cases related to its intravenous forms. In this case presentation, a 33-year-old male experienced drug-related gastrointestinal (GI) symptoms after starting semaglutide for weight loss. Semaglutide was discontinued, and oral metoclopramide was administered to manage the GI symptoms. Subsequently, he developed RLS-like symptoms, which resolved within 48 hours of stopping metoclopramide. His family history included chronic RLS. Laboratory tests were normal. The case highlights a potential link between drug administration and transient RLS symptoms. This case suggests that RLS can be a rare, reversible side effect of oral metoclopramide. It emphasizes the need for careful monitoring of RLS symptoms in patients using this drug and highlights the variability of side effects depending on the method of drug administration. The case serves as a reminder of the unpredictable nature of drug reactions and the importance of vigilance in pharmacotherapy.

14.
J Pain Symptom Manage ; 67(1): 20-26, 2024 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-37769820

RESUMEN

CONTEXT: Malignant bowel obstruction (MBO) is a common complication of intra-abdominal cancer, frequently seen in advanced gastrointestinal and gynecologic cancer. Management of MBO can be challenging, particularly if the patient is not a surgical candidate. No consensus exists on how best to manage these patients medically. Retrospective studies suggest that the combination of dexamethasone, octreotide and metoclopramide may lead to relief of obstruction and improvement in symptoms associated with the obstruction. OBJECTIVES: This study seeks to prospectively evaluate the combination of drug "triple therapy" dexamethasone 4 mg BID, metoclopramide 10 mg Q6 and octreotide 300 mcg TID to assess tolerability, safety, and effect on symptoms and deobstruction. METHODS: Adults admitted at Roswell Park Comprehensive Cancer Center with malignant bowel obstruction were eligible. Eligible patients who constented to the study were started on the triple therapy with close monitoring of symptoms and for adverse effects. RESULTS: A total of 15 patients enrolled in the study. Two patients experienced bradycardia as adverse effect and there was no incidence of bowel perforation. All patients who completed the study had complete resolution of their nausea, and improvement in other symptoms including pain, constipation, tolerance of oral intake and resumption of bowel movements. Only two of the 15 patients were alive to complete the six-month post study follow up. CONCLUSION: "Triple therapy" with dexamethasone, metoclopramide, and octreotide for management of nonsurgical MBO in this small sample size appears safe and well tolerated however a diagnosis of inoperable MBO remains associated with poor prognosis and death within months.


Asunto(s)
Obstrucción Intestinal , Neoplasias , Adulto , Humanos , Femenino , Metoclopramida/uso terapéutico , Octreótido/uso terapéutico , Fármacos Gastrointestinales/uso terapéutico , Estudios Retrospectivos , Estudios Prospectivos , Obstrucción Intestinal/terapia , Obstrucción Intestinal/complicaciones , Dexametasona/uso terapéutico , Cuidados Paliativos , Neoplasias/complicaciones
15.
J Pain Palliat Care Pharmacother ; 38(1): 38-44, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-37843383

RESUMEN

Symptoms of nausea and vomiting are common in palliative care and hospice patients. One of the many classes of medications used for the treatment of nausea and vomiting is dopamine receptor antagonists which are particularly helpful for treating nausea mediated by the chemoreceptor trigger zone (CTZ) and impaired gastrointestinal function. While dopamine antagonists can be very effective treatments for nausea they should be used with caution as they carry the risk of QTc prolongation, have a FDA black box warning for tardive dyskinesia (TD), and increased risk of precipitating psychosis and death in patients with dementia. This review will cover haloperidol, olanzapine, prochlorperazine, and metoclopramide for treatment of nausea and vomiting including evidence of efficacy, pharmacokinetics, and pharmacodynamics to improve safe and effective utilization in clinical practice. This includes medication receptor site affinities at histaminic, muscarinic, serotonergic, and alpha-adrenergic receptors which can help providers anticipate potential adverse effects and risk of extrapyramidal symptoms (EPS), TD, and QTc prolongation. This review also includes considerations for dose adjustments based on renal function, hepatic function, and age. Understanding the pharmacology of dopamine antagonists can help providers choose the best treatment for control of nausea and vomiting and subsequently improve patients' quality of life.


Asunto(s)
Antagonistas de Dopamina , Síndrome de QT Prolongado , Humanos , Cuidados Paliativos , Calidad de Vida , Vómitos/tratamiento farmacológico , Náusea/inducido químicamente , Náusea/tratamiento farmacológico
16.
Rev Recent Clin Trials ; 19(2): 143-149, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38099534

RESUMEN

BACKGROUND: Functional dyspepsia (FD) is felt as a discomfort or pain on the center line or upper abdomen. In this study, we aimed to compare the effects of Govarcin herbal capsule and Metoclopramide for alleviating gastrointestinal symptoms in patients with FD. METHODS: Totally, 106 patients enrolled in a double-blind, clinical trial study. The participants had FD and were divided into two groups receiving Govarcin and Metoclopramide by block randomization. The patients were treated for four weeks, taking one Govarcin capsule or Metoclopramide tablet after each meal. The rate of improvement in patients was assessed by mitigation of clinical symptoms, including epigastric pain, fullness, discomfort, nausea, vomiting and heartburn. Also, before and after intervention, we used Nepin questionnaire and ROME III. SPSS statistics 25 software was used for data analyzing. RESULTS: Clinical symptom score changes between Govarcin and Metoclopramide patients' groups showed that there was no significant difference in any of the clinical symptom scores (except for heartburn, p-value=0.012) between the study groups. Nepean score in Govarcin group before and after treatment were 19.3±4.8 and 8.9±2.8, respectively (p-value<0.001). For Metoclopramide group, these values were 19.8±3.5 and 9.4±2.1 respectively (p-value<0.001). No significant difference was found in terms of Nepean score between the Govarcin and Metoclopramide groups (p-value=0.995). CONCLUSION: Govarcin herbal capsule can be used to remedy symptoms in patients with FD. It seems that Govarcin is as effective as Metoclopramide in fighting symptoms of FD as no significant difference in efficacy has been demonstrated between them.


Asunto(s)
Dispepsia , Metoclopramida , Humanos , Metoclopramida/uso terapéutico , Método Doble Ciego , Dispepsia/tratamiento farmacológico , Masculino , Femenino , Adulto , Persona de Mediana Edad , Resultado del Tratamiento , Cápsulas , Medicamentos Herbarios Chinos/uso terapéutico
17.
J Cereb Blood Flow Metab ; 44(1): 142-152, 2024 01.
Artículo en Inglés | MEDLINE | ID: mdl-37728771

RESUMEN

The efflux transporter P-glycoprotein (P-gp) at the blood-brain barrier limits the cerebral uptake of various xenobiotics. To assess the sensitivity of [11C]metoclopramide to measure decreased cerebral P-gp function, we performed [11C]metoclopramide PET scans without (baseline) and with partial P-gp inhibition by tariquidar in wild-type, heterozygous Abcb1a/b(+/-) and homozygous Abcb1a/b(-/-) mice as models with controlled levels of cerebral P-gp expression. Brains were collected to quantify P-gp expression with immunohistochemistry. Brain uptake of [11C]metoclopramide was expressed as the area under the brain time-activity curve (AUCbrain) and compared with data previously obtained with (R)-[11C]verapamil and [11C]N-desmethyl-loperamide. Abcb1a/b(+/-) mice had intermediate P-gp expression compared to wild-type and Abcb1a/b(-/-) mice. In baseline scans, all three radiotracers were able to discriminate Abcb1a/b(-/-) from wild-type mice (2.5- to 4.6-fold increased AUCbrain, p ≤ 0.0001). However, only [11C]metoclopramide could discriminate Abcb1a/b(+/-) from wild-type mice (1.46-fold increased AUCbrain, p ≤ 0.001). After partial P-gp inhibition, differences in [11C]metoclopramide AUCbrain between Abcb1a/b(+/-) and wild-type mice (1.39-fold, p ≤ 0.001) remained comparable to baseline. There was a negative correlation between baseline [11C]metoclopramide AUCbrain and ex-vivo-measured P-gp immunofluorescence (r = -0.9875, p ≤ 0.0001). Our data suggest that [11C]metoclopramide is a sensitive radiotracer to measure moderate, but (patho-)physiologically relevant decreases in cerebral P-gp function without the need to co-administer a P-gp inhibitor.


Asunto(s)
Miembro 1 de la Subfamilia B de Casetes de Unión a ATP , Barrera Hematoencefálica , Ratones , Animales , Barrera Hematoencefálica/metabolismo , Miembro 1 de la Subfamilia B de Casetes de Unión a ATP/genética , Miembro 1 de la Subfamilia B de Casetes de Unión a ATP/metabolismo , Metoclopramida/metabolismo , Encéfalo/diagnóstico por imagen , Encéfalo/metabolismo , Subfamilia B de Transportador de Casetes de Unión a ATP/metabolismo , Tomografía de Emisión de Positrones
18.
Artículo en Alemán | MEDLINE | ID: mdl-37985511

RESUMEN

BACKGROUND: The presence of gastrointestinal dysfunction is an outcome-relevant complication in critically ill ICU patients. AIMS, MATERIALS AND METHODS: The following review aims to show the importance of gastrointestinal dysfunction. Multimodal therapy for gastroparesis and paralytic ileus is discussed. CONCLUSION: Erythromycin and metoclopramide are options for gastroparesis, while neostigmine is commonly used for paralytic ileus.

19.
Cureus ; 15(10): e47611, 2023 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-38022212

RESUMEN

Background Acute gastroenteritis (AGE) is a major health concern in pediatric populations because of its associated vomiting, which worsens dehydration and the severity of illness. Objective The purpose of the research was to compare the relative effectiveness of oral ondansetron in treating AGE in children's vomiting when compared to oral domperidone and oral metoclopramide. Methodology A clinical investigation involving 120 pediatric patients diagnosed with AGE was conducted in Pakistan from November 2022 to April 2023 using a single-blind randomized design and convenience sampling. The participants received oral suspensions of ondansetron, metoclopramide, and domperidone, with doses of 0.15 mg/kg, 0.1-0.2 mg/kg, and 0.5 mg/kg, respectively, adjusted according to their body weight. The outcome in different groups was analyzed using the Statistical Package for the Social Sciences (SPSS) (version 20.0; IBM SPSS Statistics for Windows, Armonk, NY). Results At six hours, vomiting cessation rates were 80.0% for ondansetron (n=32), 72.5% for domperidone (n=29), and 67.5% for metoclopramide (n=27; p=0.29). By 24 hours, ondansetron exhibited significantly higher efficacy (92.5%; n=37) compared to domperidone (82.5%; n=33) and metoclopramide (77.5%; n=31; p=0.03). Adverse effects were minimal and comparable across groups. Conclusion Oral ondansetron demonstrated superior efficacy in managing AGE-related vomiting in children within 24 hours compared to metoclopramide and domperidone.

20.
Int J Crit Illn Inj Sci ; 13(3): 92-96, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-38023576

RESUMEN

Background: Gastric content regurgitation and aspiration are the dreaded complications of securing the airway. Cricoid pressure hinders intubation and causes lower esophageal sphincter (LES) relaxation. A recent study suggests no added benefit of cricoid pressure in preventing pulmonary aspiration of gastric contents. Metoclopramide increases LES tone, prevents gastroesophageal reflux, and increases antral contractions. Hence, we wanted to study the efficacy of metoclopramide for preventing gastric regurgitation during endotracheal intubation (ETI) in patients presenting to the emergency department (ED). Methods: This study was a randomized controlled trial in patients requiring ETI in the ED. The study participants were randomized to receive either metoclopramide (intervention) 10 mg/2 ml intravenous (IV) bolus or a placebo of normal saline (placebo) 2 ml IV bolus 5 min before rapid sequence induction and intubation. The outcome of the study was the visualization of gastric regurgitation at the glottic opening during direct laryngoscopy at the time of intubation. Results: Seventy-four study participants were randomized and allocated to the metoclopramide group (n = 37) or placebo group (n = 37). Gastric regurgitation at the glottis was noted in three study participants (8%) in the metoclopramide group, and six (16%) in the placebo group (odds ratio [OR] - 0.456; 95% confidence interval [CI] of 0.105-1.981; P = 0.295). The study participants who were intubated in the first attempt had less gastric regurgitation compared to ≥2 attempts (OR 0.031; 95% CI of 0.002-0.511; P = 0.015). Conclusion: There was no decrease in regurgitation with metoclopramide as compared to placebo during ETI in study participants presenting to the ED.

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