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1.
Saudi Med J ; 44(11): 1127-1131, 2023 Nov.
Article in English | MEDLINE | ID: mdl-37926456

ABSTRACT

OBJECTIVES: To determine the impact of implementing a new pediatric inpatient structure - the clinical teaching unit (CTU) - on length of stay (LOS) and other patient care outcomes. METHODS: A retrospective study was carried out on children admitted to the General Pediatric Inpatient Service at King Abdullah Specialized Children's Hospital, Riyadh, Saudi Arabia, between July 2015 and December 2018. The main outcome measures were median and mean LOS before and after CTU implementation. Other outcomes measured were the proportion of patients discharged on weekends, during daytime, and within 24 hours of admission, and the proportion of patients readmitted within 7 days of discharge. RESULTS: Median LOS decreased from 2.80 to 2.63 days after CTU implementation (p<0.0001). The proportion of weekend discharges significantly increased after CTU implementation from 18% to 21.5% (p<0.0243) and daytime discharges significantly increased from 6.9% to 25.6% (p<0.0001) after CTU implementation. The improvements in LOS were sustained in the years after CTU implementation, with median LOS decreasing from 2.71 to 2.60 days during 2016-2018 (p<0.001) and mean LOS decreasing from 5.03 to 3.92 days (p=0.0031). During the same period, readmission rates remained stable at 3.5-4%. CONCLUSION: The implementation of a new pediatric inpatient team structure led to significant improvements in many patient care outcomes, including decreased LOS.


Subject(s)
Hospitalization , Inpatients , Humans , Child , Length of Stay , Retrospective Studies , Patient Discharge , Patient Readmission
2.
Saudi Med J ; 43(9): 1007-1012, 2022 Sep.
Article in English | MEDLINE | ID: mdl-36104056

ABSTRACT

OBJECTIVES: To determine the prevalence and risk factors of serious bacterial infections (SBIs) in infants 90 days and younger with a confirmed respiratory tract infection (RTI). METHODS: A retrospective cross-sectional study was carried out of infants 90 days and younger who were admitted to King Abdullah Specialized Children's Hospital, Riyadh, Saudi Arabia, from January 2019 to December 2020, with polymerase chain reaction (PCR)-proven RTI. Cultures from the urine, blood, and cerebrospinal fluid were reviewed with the patients' demographic information and clinical presentation. RESULTS: Of 322 patients with a viral RTI, 21 (6.5%) had a concurrent urinary tract infection (UTI), and no patients had bacteremia or bacterial meningitis. The risk of a concurrent SBI was 4 times higher in neonates (odds ratio [OR]=4.66, 95% confidence interval [CI]: [1.32-16.47]). Previously healthy infants were at lower risk to have a SBI in comparison to those with chronic diseases or renal abnormalities (OR=0.23, 95% CI: [0.09-0.61]). In addition, male gender (OR=3.49, 95% CI: [1.07-11.38]) and abnormal urinalysis (OR=4.12, 95% CI: [1.48-11.42]) were predictors of SBIs. There was no statistically significant association between the number or type of detected viruses and SBIs. CONCLUSION: No cases of invasive bacterial infections were found in infants with PCR-proven viral RTIs. There is a risk of having a concurrent UTI in this cohort of patients. Neonates had a higher risk of UTIs as compared to older infants.


Subject(s)
Bacterial Infections , Respiratory Tract Infections , Urinary Tract Infections , Bacterial Infections/epidemiology , Child , Cross-Sectional Studies , Fever/epidemiology , Humans , Infant , Infant, Newborn , Male , Prevalence , Respiratory Tract Infections/epidemiology , Retrospective Studies , Risk Factors , Urinary Tract Infections/epidemiology , Urinary Tract Infections/microbiology
3.
J Taibah Univ Med Sci ; 16(5): 695-699, 2021 Oct.
Article in English | MEDLINE | ID: mdl-34690649

ABSTRACT

OBJECTIVES: Recent studies have highlighted an increasing prevalence of depression and sleep problems among physicians during their residency training in the medical field. The study aims to explore the prevalence of depressive symptoms and sleepiness among the residents of different medical specialties in the two regions of KSA and describe the factors that potentially cause depression and sleepiness. METHODS: A survey was distributed to the residents of King Abdulaziz Medical City in the Riyadh province, and to the residents of King Fahad Specialist Hospital Buraidah and Maternity and Children's Hospital Buraidah in the Qassim province. The Patients' Health Questionnaire-2 was used to determine the prevalence of depression and the Epworth Sleepiness Scale was used to measure sleepiness. RESULTS: One hundred and eighty-one residents completed the survey. While depressive symptoms were prevalent among 93% of the residents, 49% of the residents reported excessive daytime sleepiness. Depressive symptoms were more common in the residents of King Abdulaziz Medical City, with the prevalence being 94.5%. There was a significant association between depressive symptoms and excessive sleepiness (p = 0.046). CONCLUSION: Depressive symptoms and excessive sleepiness are highly prevalent in postgraduate trainees. Residents with depression were found to be sleepier during their work. Given the negative effect on patient safety, the high prevalence of both depressive symptoms and sleepiness is alarming. There is an urgent need to improve residents' wellness through well-structured well-being programs.

4.
Surg Laparosc Endosc Percutan Tech ; 30(6): 511-517, 2020 Dec.
Article in English | MEDLINE | ID: mdl-32694403

ABSTRACT

BACKGROUND: This study primarily aimed to assess the impact of prolonged neoadjuvant treatment-surgery interval (PNSI) on histopathologic and postoperative outcomes. Impacts of the mode of neoadjuvant treatment (NT) and surgery on the outcomes were also evaluated in the same patient population. PATIENTS AND METHODS: Between February 2011 and December 2017, patients who underwent NT and total mesorectal excision for locally advanced rectal cancer were included. PNSI was defined as >4 and >8 weeks after short-course and long-course NT modalities, respectively. RESULTS: A total of 44 (27%) patients received short-course NT (standard interval: n=28; PNSI: n=16) and 122 (73%) patients received long-course NT (standard interval: n=39; PNSI: n=83). Postoperative morbidity was similar between the standard interval and PNSI in patients undergoing short-course [n=3 (11%) vs. n=3 (19%), P=0.455] and long-course [n=6 (15%) vs. n=16 (19%), P=0.602] NT. PNSI was associated with increased complete pathologic response in patients receiving short-course NT [0 vs. n=5 (31%), P=0.002]. Compared with short-course NT, long-course NT was superior in terms of tumor response based on the Mandard [Mandard 1 to 2: n=6 (21%) vs. 6 (38%), P=0.012] and the College of American Pathologists (CAP) [CAP 0 to 1: n=13 (46%) vs. n=8 (50%), P=0.009] scores. Postoperative morbidity was similar after open, laparoscopic, and robotic total mesorectal excision [n=1 (14.2%) vs. n=21 (21%) vs. n=6 (12.5%), P=0.455] irrespective of the interval time to surgery and the type of NT. CONCLUSIONS: PNSI can be considered in patients undergoing short-course NT due to its potential oncological benefits. The mode of surgery performed at tertiary centers has no impact on postoperative morbidity after both NT modalities.


Subject(s)
Laparoscopy , Rectal Neoplasms , Humans , Neoadjuvant Therapy , Rectal Neoplasms/surgery , Rectum/surgery , Retrospective Studies , Treatment Outcome
5.
J Laparoendosc Adv Surg Tech A ; 29(5): 671-676, 2019 May.
Article in English | MEDLINE | ID: mdl-30807257

ABSTRACT

Background: Robotic technique has been proposed to overcome the limitations of laparoscopic surgery. In this study, we aimed at determining whether robotic complete mesocolic excision (CME) for right-sided colon cancer can be safe and effective as conventional laparoscopic right hemicolectomy (CLRH). Materials and Methods: Between February 2015 and September 2017, patients undergoing robotic right CME and CLRH with curative intent for right-sided colon cancer were included. Patient characteristics, short-term and histopathological outcomes were compared between the groups. Results: Ninety-six patients (robotic, n = 35) were included in this study. The operative time (286 ± 77 versus 132 ± 40 minutes, P = .0001) was significantly longer in the robotic group. There were no conversions in either group. No significant differences existed between the groups regarding the mean estimated blood loss, time to first flatus, length of hospital stay (6 ± 3 versus 6 ± 3 days, P = .64), and follow-up times (robotic 15 ± 8 versus laparoscopic 16 ± 10 months P = .11). Overall complication rates (n = 10 [29%] versus n = 15 [25%], P = .67) were similar. In the robotic group, vascular injury occurred in 2 patients, and both were repaired robotically. The mean number of harvested lymph nodes was significantly higher (41 ± 12 versus 33 ± 10, P = .04) and length between the vascular tie and colonic wall was longer (13 ± 3.5 versus 11 ± 3, P = .02) in the robotic group. Conclusion: Although robotic right CME seems equally safe to CLRH in terms of short-term morbidity, future prospective randomized trials are needed to define its role for treatment of right colectomy.


Subject(s)
Colectomy/methods , Colonic Neoplasms/surgery , Laparoscopy/methods , Mesocolon/surgery , Robotic Surgical Procedures/methods , Adult , Aged , Female , Humans , Length of Stay , Lymph Nodes/pathology , Male , Mesocolon/pathology , Middle Aged , Operative Time
6.
Neurologist ; 19(4): 101-3, 2015 Apr.
Article in English | MEDLINE | ID: mdl-25888197

ABSTRACT

INTRODUCTION: POEMS syndrome is a rare, atypical plasma cell proliferative disorder. Predominantly motor chronic demyelinating polyneuropathy and monoclonal plasma cell disease are the major clinical features of POEMS syndrome. Demyelinating lesions of the central nervous system have been reported only in 2 patients with POEMS syndrome up to now. CASE REPORT: A 71-year-old man was investigated for numbness, burning sensation, and weakness of the lower extremities. He was found to have hypertrichosis, white nails, and multiple hemangiomas in the lower extremities. Neurological examination revealed decreased strength of the proximal and distal muscles of the lower extremities and absence of deep tendon reflexes. There was a marked impairment of temperature, position, and vibration senses in the lower extremities. Romberg test was positive. Nerve conduction was markedly reduced in all extremities and needle electromyography showed denervation pattern. Cerebrospinal fluid was clear, colorless, and had no oligoclonal band. IgM kappa monoclonal gammopathy was identified in serum immunofixation electrophoresis. In bone marrow aspirate plasma cells were counted as being <2%, with normal morphology. Brain magnetic resonance imaging revealed hyperintense lesions in the regions of periventricular and subcortical white matter and thalamus. Normal TSH, T4, and T3 levels and elevated levels of antitiroglobulin antibody and antithyroid peroxydase antibody were found in the laboratory tests. Our patient was diagnosed with POEMS syndrome and treated with intermittent courses of melphalan and prednisone. CONCLUSIONS: POEMS syndrome should also be considered in differential diagnosis of patients with demyelinating brain lesions, accompanied by peripheral neuropathy. Diagnostic evaluation of patients with demyelinating polyneuropathy should include brain magnetic resonance imaging.


Subject(s)
Brain/pathology , Demyelinating Diseases/diagnosis , POEMS Syndrome/pathology , Aged , Central Nervous System/pathology , Humans , Male , Neural Conduction , Sural Nerve/pathology , Sural Nerve/physiopathology
7.
Adv Clin Exp Med ; 23(5): 691-8, 2014.
Article in English | MEDLINE | ID: mdl-25491681

ABSTRACT

BACKGROUND: Antiepileptic drugs (AED) which are used to treat seizures in pregnant women, infants, and young children may cause cognitive impairment or other uncertain injury. However, the precise mechanisms responsible for the negative effects of new AEDs like lamotrigine (LTG) and topiramate (TPM) in the developing brain are still unclear. OBJECTIVES: To investigate the GFAP, NCAM and S100B levels in the whole brain of newborn rats on postnatal 1 day and in the hippocampus of adult rats to find out the effect of TPM and LTG on cognitive impairment and brain maturation. MATERIAL AND METHODS: Twenty eight pregnant rats were randomly divided into 7 groups with 4 animals in each group. The first group, receiving no drugs, was assigned as the control group. The study groups received intraperitoneal TPM or LTG injections in each trimester. Western blot analysis of the GFAP, NCAM and S100B was performed in the offspring. Behavioral tests were performed at postnatal day 75. RESULTS: The rats in the TPM-I and TPM-III groups had a significant impairment in escape latency on the 5th day as compared to the control rats in a Morris water maze test. In addition, in the expression of astrocyte derived markers, GFAP was upregulated, whereas S100ß and NCAM were downregulated in the whole brain on postnatal day 1, in offspring exposed to LTG and TPM in utero. CONCLUSIONS: The detrimental effects of TPM and LTG appear to be confined particularly to the early stages of brain development. And TPM seems to have a partial role in the cognitive impairment.

8.
Drug Res (Stuttg) ; 63(9): 439-44, 2013 Sep.
Article in English | MEDLINE | ID: mdl-23804250

ABSTRACT

UNLABELLED: The effects of 50% Drink of Myrica rubra (MRD) on the cardiovascular system of the rat and on the platelets aggregation of rats and guinea pigs were studied. METHOD: Different groups of male Wistar rats were treated either with 50% Myrica rubra drink as drinking vehicle (4 weeks) or water. The animals were then prepared for the measurement of arterial blood pressure and heart rate, ECG, sensitivity of the baroreceptors, platelets' aggregation, blood clotting time and cardiac parasympathetic ganglia. The mechanism of action of any induced effect was elucidated using different receptor blockers. RESULTS: Treatment induced a significant decrease in the arterial blood pressure and heart rate on Wistar rats, but no significant changes in the ECG were observed. Pretreatment of rats with MRD 10 or 20 ml/kg (i. p.) significantly suppressed vagal electrical stimulation to the heart and nicotine-induced bradycardia, via decreasing phenylephrine-induced rise in the arterial blood pressure and the reflexly-induced bradycardia. It significantly suppressed the Baroreceptor Sensitivity Index (BSI). The treatment also significantly suppressed ADP-induced platelets aggregation in rats and arachidonic acid-induced aggregation in guinea pigs.All these actions seemed to be mediated by the MRD constituents such as proanthocyanidins, polyphenols and flavonoids. The decreases in the heart rate and BSI were probably caused by an inherent ability to block the parasympathetic ganglia. CONCLUSION: The results of this study regarding the effects of MRD actions on the cardiovascular system and platelets qualify the drink to be classified as a functional food.


Subject(s)
Blood Platelets/drug effects , Cardiovascular System/drug effects , Myrica , Animals , Blood Platelets/physiology , Blood Pressure/drug effects , Electrocardiography/drug effects , Functional Food , Heart Rate/drug effects , Male , Phenylephrine/pharmacology , Platelet Aggregation/drug effects , Pressoreceptors/drug effects , Rats , Rats, Wistar
9.
Drug Res (Stuttg) ; 63(9): 484-8, 2013 Sep.
Article in English | MEDLINE | ID: mdl-23780497

ABSTRACT

The present study reports Gas chromatographic mass analysis (GC-MS) as well as important biological activities of Cymbopogon proximus essential oil. The chemical composition of the essential oil of Cymbopogon proximus was investigated by GC-MS. Furthermore, the effects of Cymbopogon proximus essential oil on the cardiac parasympathetic ganglia in rats, the intra-tracheal pressure in guinea-pigs and on carrageenan-induced inflammation in the rats paw, were studied. The GC-MS study led to the identification of 22 components with Piperitone representing (73.81%), Elemol (9.32%), alpha-Eudesmol (5.21%) and alpha-Terpineol (3.01%) of the oils composition. The percentage protective effect of the oil on the vagus-induced bradycardia in rats was 90.1±3.1%, which represents a significant protection. As for the effect of Cymbopogon oil on bronchoconstrictors-induced increase in intra-tracheal pressure in guinea-pigs, the oil antagonized the actions of 5-HT and histamine by 80±3.7 and 93±8.3%, respectively. Pharmacological investigations using Cymbopogon oil revealed its inherent ability to possess a bronchodilator activity mediated via blockade of both histamine and serotonin receptors. It possessed a significant ganglionic blocking action and a limited anti-inflammatory activity that seemed to involve blockade of histamine and serotonin receptors in the rats' paws.


Subject(s)
Cymbopogon/chemistry , Gas Chromatography-Mass Spectrometry/methods , Oils, Volatile/analysis , Animals , Guinea Pigs , Heart Rate/drug effects , Male , Oils, Volatile/pharmacology , Rats , Serotonin/pharmacology
10.
Int Ophthalmol ; 32(4): 383-6, 2012 Aug.
Article in English | MEDLINE | ID: mdl-22450560

ABSTRACT

The purpose is to report a case of Candida interface infection after deep anterior lamellar keratoplasty (DALK). A 23-year-old female patient underwent DALK surgery in the left eye for keratoconus. Four weeks after the surgery, she presented with asymptomatic white-cream colored deposits at the graft-host interface. Epithelial ingrowth was our first possible diagnosis because there were no symptoms or signs of inflammation. However, progression of the lesion under steroid treatment and the appearance of inflammation signs after tapering the steroid treatment raised suspicion of fungal keratitis. Anterior segment optical coherence tomography (OCT), ultrasound biomicroscopy, confocal microscopy and microbiologic examinations of the cornea were performed to evaluate the lesion. Anterior segment OCT and ultrasound biomicroscopy confirmed the lesion to be at the interface. The confocal scan disclosed hyper-reflective deposits and surrounding inflammatory cells but there were no hyphae-like structures. While taking a specimen from the lesion, the Descemet's membrane ruptured so a penetrating keratoplasty was performed. The microbiologic examination revealed Candida infection. Candida interface keratitis is a rare infection seen after DALK. The asymptomatic clinical picture and the similarity to epithelial ingrowth may postpone the diagnosis and consequently the treatment. Therefore, in cases of interface deposits seen after lamellar surgery, one should consider Candida interface keratitis.


Subject(s)
Candidiasis/diagnosis , Corneal Transplantation/adverse effects , Keratitis/diagnosis , Keratoconus/surgery , Surgical Wound Infection/diagnosis , Female , Humans , Keratitis/microbiology , Keratoconus/drug therapy , Opportunistic Infections/diagnosis , Opportunistic Infections/microbiology , Steroids/adverse effects , Surgical Wound Infection/microbiology , Young Adult
11.
Rheumatol Int ; 32(2): 525-8, 2012 Feb.
Article in English | MEDLINE | ID: mdl-21258800

ABSTRACT

Diabetic muscular infarct (DMI) is a rare condition, which begins with acute onset of extremity pain and swelling. Patients usually have long-standing disease and poorly controlled diabetes mellitus (DM). Thigh muscle group is the most commonly involved side, while lower leg involvement is rare. We represent herein a 22-year-old patient with type I DM who admitted to our outpatient clinic due to painful swelling of the left leg. In physical examination, anterior left leg was painful and firm on palpation; there was diffuse swelling extending to the knee and ankle with mild local fever and redness. T2-weighted MRI demonstrated hyperintensity in left leg muscles. A biopsy confirmed the diagnosis of DMI. She was treated with glucose regulation, analgesics, antiplatelet treatment and rest. At her 6 months, recurrence of DMI was observed. DMI should be considered in diabetic patients with extremity pain and swelling. Treatment plan should include the regulation of the blood glucose and evaluation of end-organ complications, analgesia, and bed rest.


Subject(s)
Diabetes Complications/pathology , Infarction/etiology , Muscle, Skeletal/pathology , Muscular Diseases/etiology , Musculoskeletal Pain/etiology , Diabetes Complications/metabolism , Female , Humans , Infarction/pathology , Magnetic Resonance Imaging , Muscle, Skeletal/blood supply , Muscular Diseases/pathology , Young Adult
12.
Drugs Exp Clin Res ; 30(5-6): 213-20, 2004.
Article in English | MEDLINE | ID: mdl-15702514

ABSTRACT

The hepatoprotective activity of an ethanolic extract of Commiphora opobalsamum ("Balessan") was investigated in rats by inducing hepatotoxicity with carbon tetrachloride:liquid paraffin (1:1). This extract has been shown to possess significant protective effect by lowering serum transaminase levels (serum glutamate oxaloacetate transaminase and serum glutamate pyruvate transaminase), alkaline phosphatase and bilirubin. Pretreatment with an extract of Balessan prevented the prolongation of the barbiturate sleeping time associated with carbon tetrachloride-induced liver damage in mice. On the other hand, CCl4-induced low-level nonprotein sulfhydryl concentration in the liver was replenished by the Balessan extract. These data suggest that the plant C. opobalsamum may act as an antioxidant agent and may have a hepatoprotective effect.


Subject(s)
Commiphora , Liver Diseases/pathology , Liver Diseases/prevention & control , Medicine, Traditional , Plants, Medicinal , Animals , Carbon Tetrachloride/toxicity , Chemical and Drug Induced Liver Injury , Female , Male , Mice , Plant Components, Aerial , Plant Extracts/isolation & purification , Plant Extracts/therapeutic use , Rats , Rats, Wistar , Saudi Arabia
13.
Can J Infect Dis ; 13(4): 253-8, 2002 Jul.
Article in English | MEDLINE | ID: mdl-18159398

ABSTRACT

OBJECTIVE: It is a widely accepted practice that children with anaphylaxis from penicillins should avoid cephalosporins. The purpose of the present study was to determine whether there is evidence in the literature to support this practice. DATA SOURCES: MEDLINE, EMBASE, Toxline, International Pharmaceutical Abstracts and PubMed were used to search the literature published from 1966 to 2001. The Canadian Medical Protective Association, Health Canada and the Boston Collaborative Drug Surveillance Program were also contacted to determine whether there were any unpublished cases of cross-reactivity between penicillins and cephalosporins. DATA EXTRACTION: Cases describing the use of cephalosporins in adults and children with positive penicillin skin tests or anaphylaxis from penicillin were evaluated. Case reports of anaphylaxis from cephalosporins in paediatric patients were identified. DATA SYNTHESIS: There have been five reported cases of serious reactions from cephalosporins in patients with a history of anaphylaxis from penicillins. All cases occurred in adults; three developed anaphylaxis from the older, first-generation cephalosporins, cephalothin and cephaloridine; one developed anaphylaxis from cefamandole; and one developed anaphylaxis from cefaclor. There have been 12 other published reports of anaphylaxis from cephalosporins in adults with a history of penicillin allergy or a positive penicillin skin test, but with no history of anaphylaxis from penicillin. In seven studies, in which a total of 158 patients with positive penicillin skin tests were administered cephalosporins, seven had apparent immunoglobulin E-mediated reactions when they were given a cephalosporin. When the class of cephalosporin was able to be determined, none of the reports of reactions from cephalosporins in patients with allergies to penicillin involved third-generation cephalosporins. There have been 13 case reports of anaphylaxis from cephalosporins in paediatric patients. CONCLUSION: There are no published case reports of anaphylaxis from cephalosporins in children with anaphylaxis from penicillin, and there are only a small number of such reports in adults. Anaphylaxis from cephalosporins appears to be incredibly rare in children. There is minimal evidence in the literature to support the avoidance of cephalosporins in children with anaphylaxis from penicillins.

14.
Int J Epidemiol ; 31(6): 1201-7, 2002 Dec.
Article in English | MEDLINE | ID: mdl-12540723

ABSTRACT

BACKGROUND: There are few studies reporting depression in the postnatal period in developing countries. In this study our objective was to evaluate women from eastern Turkey in the postnatal one-year period in order to analyse the risk factors for depression. METHODS: In this cross-sectional, multi-centre study, we selected a study sample from five eastern provinces. Among 2602 randomly selected women who gave birth within the last year, we included 2514 women in our analysis. The Edinburgh Postnatal Depression Scale was used for the evaluation of depression. RESULTS: The percentage of women with high depression scores was 27.2%. Excess risk of depression was associated with several factors including unemployment, low education, poverty, poor family relations, low marital age, lack of medical services, and mental health problems. CONCLUSIONS: Depression in postnatal women is an important public health problem in the less developed eastern part of Turkey.


Subject(s)
Depression, Postpartum/etiology , Adolescent , Adult , Age Factors , Cross-Sectional Studies , Depression, Postpartum/epidemiology , Developing Countries , Educational Status , Family Relations , Female , Health Services Accessibility , Humans , Middle Aged , Poverty , Psychiatric Status Rating Scales , Risk Factors , Turkey/epidemiology , Unemployment/psychology
17.
Gen Pharmacol ; 33(1): 17-22, 1999 Jul.
Article in English | MEDLINE | ID: mdl-10428011

ABSTRACT

The influence and mechanisms of action of N-ethyl- and N-benzyl-1,2-diphenylethanolamines (compounds E and B, respectively) on the arterial blood pressure and the heart rate of the rat together with their effects on CaCl2-induced arrhythmias in the rat were investigated. Both E and B in doses of (1.5-12 micromol/kg IV) decreased the arterial blood pressure and the heart rate in a dose-dependent manner. Studies with various receptor blockers, enzyme inhibitors and CaCl2 revealed that E-induced cardiovascular depressant effects were mainly due to CaCl2 channel blocking action and activation of cyclic guanylyl cyclase or release of NO whereas the cardiovascular effects of B seemed to involve both blockade of Ca2+ channels and activation of parasympathetic ganglia. Both compounds (12-14.5 micromol/kg) completely protected the rat against CaCl2 (60 mg kg(-1))-induced tachyarrhythmias. The B compound seemed to be several times more potent than the E compound in its cardiovascular depressant actions. The results suggest the potential usefulness of both compounds in the treatment of hypertension and supraventricular arrhythmias.


Subject(s)
Cardiovascular Agents/pharmacology , Ethanolamines/pharmacology , Animals , Arrhythmias, Cardiac/prevention & control , Blood Pressure/drug effects , Calcium Chloride/pharmacology , Cardiovascular Diseases/physiopathology , Cardiovascular Diseases/prevention & control , Cyclooxygenase Inhibitors/pharmacology , Dose-Response Relationship, Drug , Heart Rate/drug effects , Histamine H1 Antagonists/pharmacology , Histamine H2 Antagonists/pharmacology , Indomethacin/pharmacology , Male , Pyrilamine/pharmacology , Ranitidine/pharmacology , Rats , Rats, Wistar
18.
Pharmacol Res ; 39(6): 463-70, 1999 Jun.
Article in English | MEDLINE | ID: mdl-10373239

ABSTRACT

The influence of N -ethyl- and N -benzyl-1,2-diphenyl ethanolamines (compounds E and B, respectively) was examined on the spontaneously contracting rabbit jejunum and the rat uterus together with their influence on the contractions induced by some spasmogens in the guinea-pig ileum and oxytocics and CaCl2in the pregnant rat uterus. Both E and B inhibited the spontaneous contractions of the rabbit jejunum with ID50values of 0.13 and 0.03 micromol ml-1. Their inhibitory activities were not antagonized by alpha- or beta-adrenoceptor blockers but significantly reversed by CaCl2(0.015 micromol ml-1). The compounds also antagonized nicotine, ACh-, histamine-, 5-HT- and CaCl2-induced contractions by 44-100%. Compound E seemed to be several times more potent than B in inhibiting the spontaneous uterine contractions with an ID50of (7 nmol ml-1). Their inhibitory effects were not antagonized by beta2-adrenoceptor or H2-receptor blocking drugs. Both compounds (40 nmol ml-1) antagonized in a competitive manner CaCl2-induced contractions in the K+-depolarised uterus and PGE2and oxytocin-induced uterine contractions. The ID50values were in the range of 1.6-10.7 nmol ml-1. The results suggest that E and B compounds may be considered as putative L-Ca2+channel blockers with certain selectivities. The E compound seemed to be more selective against uterine L-Ca2+channels and the B compound against intestinal smooth muscles. Thus, the compounds may be of potential value in treatment of some colics, the irritant bowel syndrome, dysmenorrhoea and premature deliveries.


Subject(s)
Ethanolamines/pharmacology , Parasympatholytics/pharmacology , Uterine Contraction/drug effects , Uterus/drug effects , Adrenergic alpha-Antagonists/pharmacology , Animals , Blinking/drug effects , Calcium Chloride/pharmacology , Dinoprostone/pharmacology , Dose-Response Relationship, Drug , Ethanolamines/chemistry , Female , Guinea Pigs , Ileum/drug effects , Ileum/physiology , In Vitro Techniques , Jejunum/drug effects , Jejunum/physiology , Male , Muscle Contraction/drug effects , Oxytocics/pharmacology , Oxytocin/pharmacology , Potassium/pharmacology , Prazosin/pharmacology , Pregnancy , Rabbits , Rats , Rats, Wistar , Uterus/physiology , Vasodilator Agents/pharmacology
20.
Boll Chim Farm ; 136(11): 691-5, 1997 Dec.
Article in English | MEDLINE | ID: mdl-9534266

ABSTRACT

A series of 1H-1,4-benzothiazineylides was synthesized and characterized. The influence of this series of compounds 1-7 was examined on the cardiovascular system of the rat, the isolated jejunum of the rabbit, the guinea-pig ileum and the isolated uteri of late pregnant rats. The results of the present study revealed the bradicardiogenic effect of the ethyl, propyl and isobutyl derivatives when tested in the dose range of (10-53 mumole Kg-1). Furthermore, the isobutyl derivative also exhibited an ability to decrease the arterial blood pressure. All the test compounds exhibited non-spasmolytic activity against ACh, histamine and BaCl2. The butyl, isobutyl and isopropyl derivatives were found to be the most potent. The results direct the attention to a new potential group of cardiovascular depressant and spasmolytic agents.


Subject(s)
Cardiovascular Agents/chemical synthesis , Hemodynamics/drug effects , Muscle, Smooth, Vascular/drug effects , Thiazines/chemical synthesis , Animals , Cardiovascular Agents/pharmacology , Female , Guinea Pigs , In Vitro Techniques , Male , Pregnancy , Rabbits , Rats , Thiazines/pharmacology
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