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1.
BMC Anesthesiol ; 24(1): 155, 2024 Apr 23.
Artigo em Inglês | MEDLINE | ID: mdl-38654209

RESUMO

BACKGROUND: This study aimed to determine the median effective dose (ED50) and 95% effective dose (ED95) of nicardipine for treating pituitrin-induced hypertension during laparoscopic myomectomy, providing guidance for the management of intraoperative blood pressure in such patients. METHODS: Among the initial 40 participants assessed, 24 underwent elective laparoscopic myomectomy. A sequential up-and-down method was employed to ascertain the ED50 of nicardipine based on its antihypertensive efficacy. Nicardipine was initially administered at 6 µg/kg following the diagnosis of pituitrin-induced hypertension in the first patient. Dosing adjustments were made to achieve the desired antihypertensive effect, restoring systolic blood pressure and heart rate to within ± 20% of baseline within 120 s. The dosing increment or reduction was set at 0.5 µg/kg for effective or ineffective responses, respectively. The ED50 and ED95 of nicardipine were calculated using Probit regression by Maximum Likelihood Estimation (MLE) to establish dose-response curves and confidence intervals. RESULTS: 24 patients were included for analysis finally. The ED50 and ED95 of nicardipine for blood pressure control after pituitrin injection were determined. The study found that the ED50 of nicardipine for treating pituitrin-induced hypertension was 4.839 µg/kg (95% CI: 4.569-5.099 µg/kg), and the ED95 was estimated at 5.308 µg/kg (95% CI: 5.065-6.496 µg/kg). Nicardipine effectively mitigated the hypertensive response caused by pituitrin without inducing significant tachycardia or hypotension. CONCLUSIONS: Nicardipine effectively controlled blood pressure after pituitrin injection during laparoscopic myomectomy, with ED50 and ED95 values established. This research highlights the potential utility of nicardipine in addressing hypertensive responses induced by pituitrin, particularly in clinical settings where pituitrin is routinely administered.


Assuntos
Anti-Hipertensivos , Relação Dose-Resposta a Droga , Hipertensão , Laparoscopia , Nicardipino , Miomectomia Uterina , Humanos , Nicardipino/administração & dosagem , Feminino , Adulto , Hipertensão/tratamento farmacológico , Laparoscopia/métodos , Miomectomia Uterina/métodos , Anti-Hipertensivos/administração & dosagem , Anestesia Intravenosa/métodos , Hormônio Liberador de Gonadotropina , Pressão Sanguínea/efeitos dos fármacos
2.
Int J Impot Res ; 36(2): 107-109, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38218956

RESUMO

Treatment options for Peyronie's disease (PD) remain limited. Topical H100 gel, (Hybrid Medical, Edina, USA), which contains nicardipine, super oxide dismutase and emu oil showed safety and efficacy in a previous small double-blind placebo-controlled pilot study. The present study evaluates if topically applied H100 gel applied to the penile shaft infiltrates the tunica albuginea. Nicardipine is a key active ingredient in H100 and serves as a surrogate marker. Three men already scheduled to undergo a planned surgical procedure for PD applied commercially available H100 gel twice daily to the penile shaft for up to 30 days prior to the procedure. Tunica albuginea samples were obtained at surgery. Nicardipine evaluation was performed using isotope dilution technique via liquid-chromatograph-mass spectrometry (LCMS). All three patients tolerated H100 gel application without side effects. All three tunica albuginea specimens showed detectable nicardipine in the tunical tissue. Transdermal application of commercially available H100 gel is able to penetrate the tunica albuginea tissue and is detectable in men with acute and chronic PD. This finding may support the encouraging results found in the prior H100 pilot study.


Assuntos
Induração Peniana , Masculino , Humanos , Induração Peniana/tratamento farmacológico , Induração Peniana/cirurgia , Nicardipino/análise , Nicardipino/uso terapêutico , Projetos Piloto , Pênis/cirurgia , Superóxido Dismutase , Ensaios Clínicos Controlados Aleatórios como Assunto
3.
Am J Emerg Med ; 77: 233.e5-233.e7, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38155033

RESUMO

Naphazoline, a nonspecific alpha-adrenoceptor stimulant, is a potent vasoconstrictor used in nasal sprays, eye drops, and over-the-counter antiseptics. Naphazoline intoxication increases afterload by constricting the peripheral arteries, which can lead to complications including multiple organ failure. Although phentolamine, a nonselective alpha-adrenoceptor antagonist, and nicardipine, a calcium channel blocker, are used for the treatment of naphazoline intoxication, no established administration protocols currently exist. We present the case of a 32-year-old male with depression who ingested 150 mL of an antiseptic containing 0.1% naphazoline (equivalent to 150 mg of naphazoline). Five hours after ingestion, the patient was admitted to hospital exhibiting signs of naphazoline intoxication, such as bradycardia (46 beats/min), blood pressure of 166/122 mmHg, and peripheral cyanosis. We used the FloTrac™/EV1000™ system (Edwards Lifesciences, Irvine, CA, USA), a minimally invasive cardiac output monitoring system, to monitor systemic vascular resistance. The systemic vascular resistance index (SVRI) was elevated (4457 dyne.s/cm5/m2; nomal range: 1970-2390 dyne.s/cm5/m2) upon admission and initial treatment with continuous intravenous infusion of phentolamine led to SVRI normalization within 2 h. With the goal of maintaining SVRI normalization, continuous infusion with nicardipine was then started. At 10 h after treatment initiation, the nicardipine dose peaked at 9 mg/h (1.9 µg/kg/min). Treatment was discontinued 8 h later, and the patient was discharged on the fourth day without sequelae. In conclusion, the use of a minimally invasive cardiac output monitoring system to track vascular resistance can effectively guide the dosing of phentolamine or nicardipine in the treatment of naphazoline intoxication.


Assuntos
Nafazolina , Nicardipino , Masculino , Humanos , Adulto , Fentolamina , Débito Cardíaco , Receptores Adrenérgicos
5.
Medicine (Baltimore) ; 102(27): e34272, 2023 Jul 07.
Artigo em Inglês | MEDLINE | ID: mdl-37417597

RESUMO

BACKGROUND: We evaluated heart rate (HR) and blood pressure (BP) trends when nicardipine (NCD) was co-administered during dexmedetomidine (DEX) sedation after spinal anesthesia. METHODS: Sixty patients aged 19 to 65 were randomly assigned to the DEX or DEX-NCD groups. Five minutes after infusion of the loading dose of DEX, the NCD was administered intravenously at a rate of 5 µg/kg for 5 minutes in the DEX-NCD group. The study starting point was set at 0 minute when the DEX loading dose was initiated. The primary outcomes were the differences in HR and BP between the 2 groups during the study drug administration. Secondary outcomes included the number of patients whose HR was < 50 beats per minute (bpm) after the DEX loading dose infusion, and associated factors were evaluated. The incidence of hypotension in the postanesthesia care unit, postanesthesia care unit length of stay, postoperative nausea and vomiting, postoperative urinary retention, time to first urination after spinal anesthesia, acute kidney injury, and postoperative hospital length of stay were evaluated. RESULTS: The HR was significantly higher at 14 minutes, and the mean BP was significantly lower at 10 minutes in the DEX-NCD group than in the DEX group. The number of patients with an HR < 50 bpm during surgery was significantly higher in the DEX group than in the DEX-NCD group at 12, 16, 24, 26, and 30 minutes. The DEX group and a low initial HR were independently associated with the occurrence of an HR < 50 bpm after DEX loading dose infusion. Postoperative outcomes were not significantly different between the 2 groups. CONCLUSIONS: Simultaneous administration of NCD during the administration of a loading dose of DEX prevented severe bradycardia. Co-administration of NCD may be considered in patients with a low initial HR when severe bradycardia is expected during the DEX loading dose infusion. NCD and DEX may be safely infused simultaneously without affecting postoperative complications (see Figure S1, Supplemental Digital Content, http://links.lww.com/MD/J241 , Graphical abstract).


Assuntos
Raquianestesia , Dexmedetomidina , Doenças não Transmissíveis , Humanos , Hipnóticos e Sedativos/efeitos adversos , Nicardipino , Bradicardia , Frequência Cardíaca , Náusea e Vômito Pós-Operatórios , Método Duplo-Cego
6.
Br J Cancer ; 129(5): 884-894, 2023 09.
Artigo em Inglês | MEDLINE | ID: mdl-37474721

RESUMO

BACKGROUND: It is imperative to develop novel therapeutics to overcome chemoresistance, a significant obstacle in the clinical management of prostate cancer (PCa) and other cancers. METHODS: A phenotypic screen was performed to identify novel inhibitors of chemoresistant PCa cells. The mechanism of action of potential candidate(s) was investigated using in silico docking, and molecular and cellular assays in chemoresistant PCa cells. The in vivo efficacy was evaluated in mouse xenograft models of chemoresistant PCa. RESULTS: Nicardipine exhibited high selectivity and potency against chemoresistant PCa cells via inducing apoptosis and cell cycle arrest. Computational, molecular, and cellular studies identified nicardipine as a putative inhibitor of embryonic ectoderm development (EED) protein, and the results are consistent with a proposed mechanism of action that nicardipine destabilised enhancer of zeste homologue 2 (EZH2) and inhibited key components of noncanonical EZH2 signalling, including transducer and activator of transcription 3, S-phase kinase-associated protein 2, ATP binding cassette B1, and survivin. As a monotherapy, nicardipine effectively inhibited the skeletal growth of chemoresistant C4-2B-TaxR tumours. As a combination regimen, nicardipine synergistically enhanced the in vivo efficacy of docetaxel against C4-2 xenografts. CONCLUSION: Our findings provided the first preclinical evidence supporting nicardipine as a novel EED inhibitor that has the potential to be promptly tested in PCa patients to overcome chemoresistance and improve clinical outcomes.


Assuntos
Nicardipino , Neoplasias da Próstata , Animais , Humanos , Masculino , Camundongos , Apoptose , Linhagem Celular Tumoral , Docetaxel/farmacologia , Docetaxel/uso terapêutico , Nicardipino/farmacologia , Nicardipino/uso terapêutico , Complexo Repressor Polycomb 2 , Neoplasias da Próstata/tratamento farmacológico
7.
Fundam Clin Pharmacol ; 37(5): 1006-1010, 2023 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-37125685

RESUMO

There is a paucity of clinical data about whether sugammadex forms precipitates with other medications. This laboratory experimental study was performed to determine the drugs that produce precipitates with sugammadex. Samples of 1 ml of sugammadex were prepared in transparent cylinders, to which 1 ml of test drugs (rocuronium, neostigmine, glycopyrrolate, atropine, nitroglycerin, dobutamine, dopamine, epinephrine, vasopressin, norepinephrine, phenylephrine, ephedrine, esmolol, nicardipine, and labetalol) was added. The precipitation reaction was observed visually and via light microscope. The pH of each drugs before and after mixing with sugammadex was measured. White crystals were formed when sugammadex was mixed with nicardipine or labetalol. Sugammadex formed precipitate when mixed with nicardipine or labetalol. Sufficient fluid flushing is required between injections of each drug to prevent these reactions.


Assuntos
Labetalol , Bloqueio Neuromuscular , Fármacos Neuromusculares não Despolarizantes , Sugammadex , Nicardipino , Labetalol/uso terapêutico , Pesquisa
8.
Anal Methods ; 15(17): 2073-2081, 2023 05 04.
Artigo em Inglês | MEDLINE | ID: mdl-37070706

RESUMO

A HPLC-UV method for the determination of nimodipine and nicardipine in breast milk using restricted access polypyrrole as an adsorbent in pipette-tip solid-phase extraction (PT-SPE) has been developed. The chromatographic conditions were a C18 column (150 mm × 4.60 mm, 5 µm) using methanol : acetonitrile : ultrapure water (55 : 30 : 15, v/v/v) at a flow rate of 1.0 mL min-1 and detection at 236 nm. The adsorbents have been synthesized and characterized by using Fourier-transform infrared spectroscopy, scanning electron microscopy, thermogravimetric analysis, surface analysis, wettability and point zero charge, and were then applied in sample preparation. The main parameters that affect analyte recovery from breast milk by PT-SPE were optimized and the analytical method showed recoveries around 100%, linearity from 3 to 3000 ng mL-1, and correlation coefficients (r) ≥ 0.99 for the two analytes, in addition to adequate precision, accuracy and robustness. Finally, the validated method has been successfully applied in analyses of breast milk from volunteers.


Assuntos
Leite Humano , Polímeros , Feminino , Humanos , Polímeros/química , Pirróis/química , Nimodipina , Nicardipino , Extração em Fase Sólida/métodos
9.
Clin Neurol Neurosurg ; 227: 107644, 2023 04.
Artigo em Inglês | MEDLINE | ID: mdl-36842290

RESUMO

PURPOSE: The term "cerebrovascular diseases (CVDs)" refers to a broad category of diseases that affect the brain's blood vessels and cerebral circulation. Controlling acute hypertension (HTN) by antihypertensive drugs such as clevidipine and nicardipine can be a highly efficient method of lowering the incidence of CVDs. METHODS: This is a systematic review and meta-analysis study. The PubMed, Scopus, and Web of Science online databases and a gray literature search were performed to identify potentially eligible studies. The included studies were observational studies that compared adult patients receiving clevidipine or nicardipine for controlling HTN in the setting of CVD. RESULTS: We reviewed 5 final included articles, including 546 patients. The pooled standardized mean difference (SMD) for time to goal SBP was - 0.04 (95 % CI: [-0.66; 0.58], p-value: 0.86, I2: 79.0 %, pooled MD: -12.90 min), meaning that the clevidipine group had a shorter time to goal systolic blood pressure (SBP) than the nicardipine group. The pooled SMD for total volume infusion was - 0.52 (95 % CI: [-0.93; -0.12], p-value: 0.03, I2: 0.0 %, pooled MD: -1118.81 mL), showing a notably lower total volume infused into patients in the clevidipine group. CONCLUSIONS: We found that clevidipine reaches the SBP goal faster than nicardipine; however, there was no statistically significant difference between the two drugs. The total volume infused to achieve the goal SBP was significantly lower in the clevidipine group. Further prospective studies are needed to compare clevidipine and nicardipine in CVD patients on a large scale.


Assuntos
Transtornos Cerebrovasculares , Hipertensão , Adulto , Humanos , Nicardipino/uso terapêutico , Bloqueadores dos Canais de Cálcio/uso terapêutico , Bloqueadores dos Canais de Cálcio/farmacologia , Anti-Hipertensivos/uso terapêutico , Transtornos Cerebrovasculares/tratamento farmacológico , Transtornos Cerebrovasculares/complicações , Pressão Sanguínea
10.
J Pharm Pract ; 36(3): 501-507, 2023 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-34693825

RESUMO

Objective: The primary objective of this study was to compare the efficacy of clevidipine to nicardipine in the treatment of perioperative acute hypertension in patients undergoing cardiac surgery. Methods: This was a single-center retrospective study which included patients who received either clevidipine or nicardipine. Patients were followed for the duration of study drug infusion or for a maximum of 48 hours. Outcomes assessed included the percent of time spent within patient specific goal blood pressure, incidence of hypertensive events per patient, safety outcomes, and cost of medication treatment. Results: There were 201 cardiac surgeries performed between August 2018-January 2019 and July 2019-February 2020. Sixty-seven patients met our inclusion criteria of receiving either clevidipine (n = 29) or nicardipine (n = 38). The median percent of time spent within goal blood pressure range for clevidipine was 55.2% compared to 36.4% for nicardipine treatment (P = .036). The median number of hypertensive episodes per patient was 3 for clevidipine and 2 for nicardipine (P = .211). There were no identified differences in safety outcomes such as hypotension, vasopressor use, serum creatinine elevation, tachycardia, and atrial fibrillation. The median cost of treatment required for the observed 48-hour period with clevidipine was $128.58 compared to $55.74 for nicardipine (P < .001). Conclusion: Our findings suggest that patients undergoing cardiac surgery on clevidipine had better perioperative blood pressure control compared to nicardipine, with a negligible increase in cost, and no observed difference in safety.


Assuntos
Procedimentos Cirúrgicos Cardíacos , Hipertensão , Humanos , Nicardipino/uso terapêutico , Bloqueadores dos Canais de Cálcio/efeitos adversos , Estudos Retrospectivos , Hipertensão/tratamento farmacológico , Hipertensão/epidemiologia , Pressão Sanguínea , Procedimentos Cirúrgicos Cardíacos/efeitos adversos , Anti-Hipertensivos/efeitos adversos
11.
Intern Med ; 62(9): 1365-1369, 2023 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-36171133

RESUMO

A 67-year-old man was admitted to our hospital with a high fever. Laboratory tests revealed leukopenia, thrombocytopenia, liver dysfunction, rhabdomyolysis, and hyperferritinemia. He was diagnosed with severe fever with thrombocytopenia syndrome (SFTS) complicated by hemophagocytic lymphohistiocytosis and treated with steroid therapy, intravenous calcium channel blocker (CCB), and supportive care, without favipiravir. Serum levels of ferritin and soluble interleukin 2 receptor (sIL2R) were markedly elevated on Day 3 after admission and decreased thereafter, while an SFTS viral load of 6.8×104 copies/µL was detected on Day 2, increasing to 2.9×105 copies/µL on Day 6. Serum ferritin and sIL2R levels may be better indicators of mortality than the SFTS viral load, and CCBs may have a therapeutic effect.


Assuntos
Linfo-Histiocitose Hemofagocítica , Phlebovirus , Febre Grave com Síndrome de Trombocitopenia , Trombocitopenia , Masculino , Humanos , Idoso , Febre Grave com Síndrome de Trombocitopenia/complicações , Bloqueadores dos Canais de Cálcio/uso terapêutico , Nicardipino , Linfo-Histiocitose Hemofagocítica/complicações , Linfo-Histiocitose Hemofagocítica/tratamento farmacológico , Linfo-Histiocitose Hemofagocítica/diagnóstico , Trombocitopenia/complicações , Trombocitopenia/tratamento farmacológico , Ferritinas
12.
Neurocrit Care ; 37(2): 487-496, 2022 10.
Artigo em Inglês | MEDLINE | ID: mdl-35513751

RESUMO

BACKGROUND: On the basis of increased mortality associated with hyperchloremia among critically ill patients, we investigated the effect of occurrence of early hyperchloremia on death or disability at 90 days in patients with intracerebral hemorrhage (ICH). METHODS: We analyzed the data from Antihypertensive Treatment of Cerebral Hemorrhage 2 trial, which recruited patients with spontaneous ICH within 4.5 h of symptom onset. Patients with increased serum chloride levels (110 mmol/L or greater) at either baseline or 24, 48, or 72 h after randomization were identified. We further graded hyperchloremia into one occurrence or two or more occurrences within the first 72 h. Two logistic regression analyses were performed to determine the effects of hyperchloremia on (1) death within 90 days and (2) death or disability at 90 days after adjustment for potential confounders. RESULTS: Among the total of 1,000 patients analyzed, hyperchloremia within 72 h was seen in 114 patients with one occurrence and in 154 patients with two or more occurrences. Patients with one occurrence of hyperchloremia (odds ratio [OR] 2.5, 95% confidence interval [CI] 1.1-5.5) and those with two or more occurrences (OR 2.6, 95% CI 1.3-5.0) had significantly higher odds of death within 90 days after adjustment for age, race and ethnicity, National Institutes of Health Stroke Scale score strata, hematoma volume, presence or absence of intraventricular hemorrhage, cigarette smoking, previous stroke, and maximum hourly dose of nicardipine. Patients with two or more occurrences of hyperchloremia (OR 3.4, 95% CI 2.1-5.6) had significantly higher odds of death or disability at 90 days compared with patients without hyperchloremia after adjustment for the abovementioned potential confounders. CONCLUSIONS: The independent association between hyperchloremia and death or disability at 90 days suggests that avoidance of hyperchloremia may reduce the observed death or disability in patients with ICH. CLINICAL TRIAL REGISTRATION: ClinicalTrials.gov: NCT01176565.


Assuntos
Nicardipino , Acidente Vascular Cerebral , Anti-Hipertensivos/uso terapêutico , Hemorragia Cerebral , Cloretos/uso terapêutico , Humanos , Nicardipino/uso terapêutico
13.
Int J Cardiol ; 356: 1-5, 2022 06 01.
Artigo em Inglês | MEDLINE | ID: mdl-35395290

RESUMO

BACKGROUND: Administration of intracoronary (IC) adenosine allows an easily feasible, inexpensive, and more rapid alternative method for fractional flow reserve (FFR). It is common practice in many centers worldwide. Nicardipine is a strong coronary vasodilator but its efficacy and safety for assessing FFR is not established. The purpose of present study was to compare the efficacy and safety of IC nicardipine and adenosine for assessing FFR. METHODS: One hundred and fifty-nine patients with a total of 193 vessels undergoing clinically indicated FFR assessment of intermediate coronary stenoses were included. For the initial assessment of FFR, hyperemia was induced by an IC adenosine. After a washout period of 3 min, FFR was reassessed using 200 µg of IC nicardipine. RESULTS: Hyperemic efficacy among two different stimuli was compared. The mean FFR with IC adenosine was 0.83 ± 0.09 and that with an IC nicardipine was 0.84 ± 0.09. The median FFR with an IC adenosine was 0.83 (0.78-0.91) and that with an IC nicardipine was 0.85 (0.79-0.91) (p-value 0.246). Both FFR values showed an excellent correlation (R2 = 0.982, p < 0.001). Nicardipine produced fewer changes in heart rate, less chest pain and less flushing than adenosine. Transient atrioventricular block occurred in 29 patients with IC adenosine and none with IC nicardipine. CONCLUSIONS: IC bolus injection of nicardipine could be introduced as a safe and practical alternative method of inducing hyperemia during FFR measurements. Compared to IC adenosine, IC nicardipine has a similar hyperemic efficacy and excellent side-effect profile.


Assuntos
Estenose Coronária , Reserva Fracionada de Fluxo Miocárdico , Hiperemia , Adenosina , Cateterismo Cardíaco , Angiografia Coronária/métodos , Estenose Coronária/diagnóstico , Estenose Coronária/tratamento farmacológico , Vasos Coronários , Reserva Fracionada de Fluxo Miocárdico/fisiologia , Humanos , Hiperemia/induzido quimicamente , Nicardipino/efeitos adversos , Índice de Gravidade de Doença , Vasodilatadores
14.
World J Pediatr Congenit Heart Surg ; 13(3): 341-345, 2022 05.
Artigo em Inglês | MEDLINE | ID: mdl-35446217

RESUMO

OBJECTIVE: The use of nicardipine in congenital cardiac surgery has been guarded given the calcium sensitivity of immature myocardium and paucity of clinical data. Reports of nicardipine use have excluded neonates with single ventricles. The goal of this study was to compare the use of nicardipine and sodium nitroprusside for postoperative blood pressure control in young patients recovering from cardiac surgery. METHODS: All neonates (<30 days) and young infants (31-180 days) who received either sodium nitroprusside or nicardipine as first-line therapy for blood pressure control were retrospectively reviewed. Some patients had multiple index operations and each index operation was counted separately regarding treatment with sodium nitroprusside or nicardipine. RESULTS: A total of 59 patients underwent 70 procedures (24 as neonates and 46 as infants). Nicardipine was administered as initial therapy following 33 procedures (n = 28 patients), and sodium nitroprusside was administered as initial therapy following 37 index procedures (n = 31 patients). The duration of treatment was longer (P = .025) when sodium nitroprusside was the initial treatment. Five (15%) patients that received nicardipine required a second blood pressure management agent, and seven (19%) patients that received sodium nitroprusside required a second agent (P = .66). No adverse events related to titratable antihypertensive therapy were recorded in any treatment group. The use of nicardipine resulted in significant medication cost reduction. Based on average wholesale price, patient costs for sodium nitroprusside use were $182,952 ($5,544/pt), while costs for nicardipine were only $24,960 ($780/pt). CONCLUSIONS: Nicardipine can be safely used as a first-line antihypertensive in infants. The use of nicardipine as initial antihypertensive therapy rather than sodium nitroprusside can lead to a significant reduction in medication costs without jeopardizing clinical outcomes.


Assuntos
Procedimentos Cirúrgicos Cardíacos , Hipertensão , Anti-Hipertensivos/uso terapêutico , Pressão Sanguínea , Análise Custo-Benefício , Humanos , Hipertensão/tratamento farmacológico , Lactente , Recém-Nascido , Nicardipino/efeitos adversos , Nitroprussiato/farmacologia , Nitroprussiato/uso terapêutico , Estudos Retrospectivos
15.
Anal Chim Acta ; 1199: 339567, 2022 Mar 22.
Artigo em Inglês | MEDLINE | ID: mdl-35227379

RESUMO

Electrically conductive polymer nanomaterials signify a promising class of sensing platforms in the field of electrochemistry, but their applications as electrocatalysts are commonly limited by their poor colloidal stability in aqueous media and large particle sizes. Inspired by biomineralization approaches for integrating nanoscale materials, herein, a gadolinium (Gd)-integrated polypyrrole (PPy) electrocatalyst (namely, BSA@PPy-Gd) was successfully prepared by choosing bovine serum albumin (BSA) as a stabilizer for biomimetic mineralization and polymerization in a "one-step" manner. BSA@PPy-Gd possesses outstanding water dispersibility, nanoscale morphology, and improved electrical conductivity. The electrocatalytic competency of the electrochemical (EC) sensing platform fabricated for the sensitive detection of nicardipine (NCD) was assessed. The synergy of remarkable conductivity, superior active surface area, and electrostatic interactions stimulated by the combination of BSA with the NH group of PPy on BSA@PPy-Gd and Gd increases the fast electron transfer at the analyte-electrode junction. The fabricated EC sensor, BSA@PPy-Gd/glassy carbon electrode (GCE), exhibits a current intensity greater than that of PPy/GCE, BSA/GCE, and bare GCE in terms of peak height at a pH of 7.0 in phosphate buffer solution. The newly fabricated EC sensing platform shows excellent electrocatalytic activities for the electroreduction of NCD in terms of a low detection limit (2 nM), good sensitivity, linear dynamic detection ranges (0.01-575 µM), operational stability, and repeatability and was also tested on rat and human serum specimens.


Assuntos
Polímeros , Pirróis , Animais , Biomimética , Eletrodos , Gadolínio , Nicardipino , Ratos
16.
Neurocrit Care ; 36(3): 983-992, 2022 06.
Artigo em Inglês | MEDLINE | ID: mdl-34904214

RESUMO

BACKGROUND: Intracranial hemorrhage is associated with high mortality and morbidity. Lowering systolic blood pressure (SBP) with an intravenous antihypertensive, such as nicardipine or clevidipine, may reduce the risk of hematoma expansion and rebleeding. Previous studies comparing nicardipine and clevidipine in patients with stroke found no significant difference in blood pressure management. The inclusion of patients with ischemic stroke limited those studies because of convoluted results related to faster door-to-needle times. The purpose of this study was to compare clevidipine with nicardipine in time to goal SBP in hemorrhagic stroke. METHODS: This single-center retrospective observational cohort study evaluated adult hemorrhagic patients with stroke who received clevidipine or nicardipine from January 1, 2015, to December 31, 2020. Patients were excluded if they had trauma-related hemorrhage, received concurrent continuous intravenous antihypertensives, received the study drug for less than 1-h duration, had a less than 24-h washout period between agents, required any dialysis, were pregnant, or were incarcerated. The primary outcome was time to goal SBP. Secondary outcomes included need for additional antihypertensives, percentage of time at goal SBP, all-cause mortality, 30-day readmission, rebleeding, total volume of antihypertensive infusion, hematoma expansion, intensive care unit length of stay (LOS), hospital LOS, and cost of infusion. Safety outcomes included hypotension, severe hypotension, rebound hypertension, bradycardia, tachycardia, onset of atrial fibrillation, and acute kidney injury. RESULTS: Of 89 patients included in this study, 60 received nicardipine and 29 received clevidipine. There was no significant difference between nicardipine and clevidipine in time to goal SBP in the unmatched cohort (30 vs. 45 min; p = 0.73) or the propensity-score-matched cohort (30 vs. 45 min; p = 0.47). Results were not affected by potential confounders in the multiple linear regression. The nicardipine group had a higher total volume from infusion compared with the clevidipine group (1410 vs. 330 mL; p < 0.0001) but significantly lower cost ($99.6 vs. $497.4; p < 0.0001). There were no significant differences in need for additional antihypertensives, percentage of time at goal SBP, all-cause mortality, 30-day readmission, rebleeding, hematoma expansion, intensive care unit LOS, and hospital LOS. Compared with the clevidipine group, the nicardipine group had less rebound hypertension (40% vs. 75.9%; p = 0.0017) and less bradycardia (23.3% vs. 44.8%; p = 0.05). There were no significant differences in hypotension, severe hypotension, tachycardia, and acute kidney injury. CONCLUSIONS: In patients with hemorrhagic stroke, nicardipine appeared to have similar efficacy as clevidipine in SBP reduction, with a more likely reduction of rebound hypertension and drug cost. This retrospective study was underpowered, which may limit these implications. Further prospective studies are warranted to confirm these results.


Assuntos
Injúria Renal Aguda , Acidente Vascular Cerebral Hemorrágico , Hipertensão , Hipotensão , Acidente Vascular Cerebral , Adulto , Anti-Hipertensivos/efeitos adversos , Pressão Sanguínea/fisiologia , Bradicardia , Hematoma/complicações , Humanos , Hipotensão/tratamento farmacológico , Nicardipino/farmacologia , Nicardipino/uso terapêutico , Piridinas , Estudos Retrospectivos , Resultado do Tratamento
17.
Aging (Albany NY) ; 13(5): 6820-6831, 2021 02 17.
Artigo em Inglês | MEDLINE | ID: mdl-33621205

RESUMO

Glioblastoma multiforme (GBM) is the most invasive malignant central nervous system tumor with poor prognosis. Nicardipine, a dihydropyridine calcium channel antagonist, has been used as an adjuvant to enhance sensitivity to chemotherapeutic drugs. However, whether glioma stem cells (GSCs) can be sensitized to chemotherapy via combined treatment with temozolomide (TMZ) and nicardipine is unclear. In this study, surgical specimen derived GSCs SU4 and SU5 were applied to explore the sensitization effect of nicardipine on temozolomide against GSCs, and further explore the relevant molecular mechanisms. Our results showed that nicardipine can enhance the toxic effect of temozolomide against GSCs, promote apoptosis of GSCs, and inhibit autophagy of GSCs. The relevant mechanisms were related to activation of mTOR, and selective inhibition of mTOR by rapamycin could weaken the sensitization of nicardipine to temozolomide, which suggest that nicardipine can be applied as an adjuvant to inhibit autophagy in GSCs, and enhance apoptosis-promoting effect of temozolomide in GSCs as well. Nicardipine can inhibit autophagy by activating expression of mTOR, thus play tumor inhibition roles both in vitro and in vivo. Repurposing of nicardipine can help to improving therapeutic effect of TMZ against GBM, which deserves further clinical investigations.


Assuntos
Apoptose/efeitos dos fármacos , Autofagia/efeitos dos fármacos , Glioma/patologia , Células-Tronco Neoplásicas/efeitos dos fármacos , Nicardipino/farmacologia , Temozolomida/farmacologia , Antineoplásicos Alquilantes/farmacologia , Neoplasias Encefálicas/patologia , Bloqueadores dos Canais de Cálcio/farmacologia , Humanos , Células Tumorais Cultivadas
19.
J Card Surg ; 35(5): 1021-1028, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-32176355

RESUMO

BACKGROUND: Vasoactive medications are commonly administered for afterload reduction and arterial hypertension treatment in patients after cardiac surgery. A systematic review and meta-analysis were conducted to determine the effects of sodium nitroprusside and nicardipine on hemodynamics and cardiac performance in this population. METHODS: A systematic review of published manuscripts was performed to identify studies of patients who received sodium nitroprusside and nicardipine as part of the treatment for arterial hypertension or afterload reduction after cardiac surgery. A meta-analysis was then conducted to determine the effects of sodium nitroprusside and nicardipine on hemodynamics and cardiac performance. The following parameters were captured: blood pressure, heart rate, right atrial pressure, systemic vascular resistance, and stroke volume. RESULTS: In total, five studies with 571 patients were pooled for these analyses. Systolic blood pressure, diastolic blood pressure, and mean arterial blood pressure were similar in both groups. The cardiac index was greater with nicardipine while mean pulmonary artery pressure was lower with sodium nitroprusside. CONCLUSION: Nicardipine and sodium nitroprusside have similar abilities in reducing afterload in the postoperative cardiac population. Statistically significant differences were found in pulmonary artery pressure and cardiac index. It may be beneficial to consider nicardipine for afterload reduction in patients with a low cardiac index.


Assuntos
Procedimentos Cirúrgicos Cardíacos , Hipertensão/tratamento farmacológico , Nicardipino/uso terapêutico , Nitroprussiato/uso terapêutico , Complicações Pós-Operatórias/tratamento farmacológico , Adulto , Idoso , Pressão Arterial , Pressão Sanguínea , Feminino , Hemodinâmica , Humanos , Hipertensão/fisiopatologia , Masculino , Pessoa de Meia-Idade , Complicações Pós-Operatórias/fisiopatologia , Artéria Pulmonar , Volume Sistólico , Resistência Vascular
20.
J Neurointerv Surg ; 12(8): 774-776, 2020 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-32034105

RESUMO

OBJECTIVE: To develop a nicardipine prolonged-release implant (NPRI) to prevent cerebral vasospasm in patients with subarachnoid hemorrhage in 1999, which may be used during craniotomy, and report the results of our recent 12-year single critical care center experience. METHODS: Of 432 patients with aneurysmal subarachnoid hemorrhage treated between 2007 and 2019, 291 were enrolled. 97 Patients were aged >70 years (33%), 194 were female (67%), 138 were World Federation of Neurological Societies grades 1, 2, and 3 (47%), 218 were Fisher group 3 (75%), and 243 had an anterior circulation aneurysm (84%). Using a propensity score matching method for these five factors, the severity of cerebral vasospasm, occurrence of delayed cerebral infarction, and modified Rankin Scale (mRS) score at discharge were analyzed. RESULTS: One hundred patients each with or without NPRI were selected, and the ratios of coil/clip were 0/100 and 88/12, respectively. Cerebral vasospasm and delayed cerebral infarction were both significantly less common in the NPRI group (p=0.004, OR=0.412 (95% CI 0.223 to 0.760) and p=0.005, OR=0.272 (95% CI 0.103 to 0.714, respectively); a significant difference was seen in the mRS score at discharge by Fisher's exact test (p=0.0025). A mRS score of 6 (dead) was less common in the group with NPRI, and mRS scores of 0 and 1 were also less common. No side effects were seen. CONCLUSIONS: NPRIs significantly reduced the occurrence of cerebral vasospasm and delayed cerebral infraction without any side effects. The NPRI and non-NPRI groups showed different patterns of short-term outcomes in the single critical care center, which might have been due to selection bias and patient characteristics. Differences in outcomes may become clear in comparisons with patients treated by craniotomy.


Assuntos
Nicardipino/uso terapêutico , Hemorragia Subaracnóidea , Adulto , Idoso , Idoso de 80 Anos ou mais , Infarto Cerebral , Cuidados Críticos , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Pontuação de Propensão , Próteses e Implantes , Resultado do Tratamento , Vasoespasmo Intracraniano/tratamento farmacológico , Vasoespasmo Intracraniano/prevenção & controle
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