更新于：2024-12-06
Ditiazem Hydrochloride
盐酸地尔硫卓
更新于：2024-12-06
概要
基本信息
简介地尔硫卓是一种钙离子细胞内流抑制剂（慢通道阻滞剂或钙拮抗剂）。尽管其抗心绞痛作用的确切机制仍在研究中，但认为其作用方式如下：该药已被证明是心外膜和心内膜下冠状动脉的有效扩张剂，可抑制自发或由麦角新碱引起的冠状动脉痉挛。用于治疗慢性稳定型心绞痛和冠状动脉痉挛引起的心绞痛。该药于1973年由武田三菱在日本首次推出。 |
药物类型 小分子化药 |
别名 Diltiazem hydrochloride (JP17/USP)、Diltiazem Hyudrochloride、Diltizem Hydrochloride + [50] |
靶点 |
作用机制 Cav2.2阻滞剂(N-型电压门控性钙通道α-1B亚基阻滞剂) |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C22H27ClN2O4S |
InChIKeyHDRXZJPWHTXQRI-BHDTVMLSSA-N |
CAS号33286-22-5 |
关联
39
项与 盐酸地尔硫卓 相关的临床试验Diltiazem in Jervell and Lange-Nielsen Syndrome
A Phase 1, Open-Label, Fixed-Sequence Study to Evaluate the Effects of Multiple Doses of Diltiazem on the Single-Dose Pharmacokinetics of MK-5684 in Healthy Adult Male Participants
A Study to Evaluate the Effects of Coadministration of Diltiazem on the Plasma Pharmacokinetics of a Single Dose of MK-6552 in Healthy Participants
100 项与 盐酸地尔硫卓 相关的临床结果
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100 项与 盐酸地尔硫卓 相关的转化医学
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100 项与 盐酸地尔硫卓 相关的专利（医药）
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479
项与 盐酸地尔硫卓 相关的文献（医药）2024-11-05Microbiology Spectrum
Cefepime-taniborbactam demonstrates potent
in vitro
activity vs
Enterobacterales
with
bla
OXA-48
Article
作者: Six, David A. ; Papp-Wallace, Krisztina M. ; Becka, Scott A. ; Moeck, Greg ; Zeiser, Elise T. ; Mojica, Maria F.
ABSTRACT:
Taniborbactam (formerly VNRX-5133) is a novel, investigational boronic acid β-lactamase inhibitor. The combination of cefepime (FEP) with taniborbactam is active against
Enterobacterales
carrying class A, B, C, and/or D enzymes. We assessed the activity of FEP-taniborbactam against
Enterobacterales
clinical strains carrying
blaOXA-48
(
N
= 50, 100%), of which 78% harbored at least one extended-spectrum β-lactamase (ESBL). CLSI-based agar dilution susceptibility testing was conducted using FEP-taniborbactam and comparators FEP, meropenem-vaborbactam (MVB), and ceftazidime-avibactam (CZA). The addition of taniborbactam lowered FEP MICs to the provisionally susceptible range of ≤16 µg/mL; the MIC
90
value decreased from ≥64 µg/mL for FEP to 4 µg/mL for FEP-taniborbactam. Notably, FEP-taniborbactam MIC
50
/MIC
90
values (0.5/4 µg/mL) were lower than those for MVB (1/16 µg/mL) and comparable to those for CZA (0.5/1 µg/mL). Time-kill assays with
E. coli
clinical strains DOV (
blaOXA-48
,
blaCTX-M-15
,
blaTEM-1
, and
blaOXA-1
) and MLI (
blaOXA-48
,
blaVEB
,
blaTEM-1
, and
blaCMY-2
) revealed that FEP-taniborbactam at concentrations 1×, 2×, and 4× MIC displayed time-dependent reductions in the number of CFU/mL from 0 to 6 h, and at 4× MIC demonstrated bactericidal activity (3 log
10
reduction in CFU/mL at 24 h). Therefore, taniborbactam in combination with FEP was highly active against this diverse panel of
Enterobacterales
with
blaOXA-48
and represents a potential addition to our antibiotic arsenal.
IMPORTANCE:
OXA-48-like β-lactamases are class D carbapenemases widespread in
Klebsiella pneumoniae
and other
Enterobacterales
and are associated with carbapenem treatment failures. As up to 80% of OXA-48-like positive isolates coproduce extended-spectrum β-lactamases, a combination of β-lactams with broad-spectrum β-lactamase inhibitors is required to counteract all OXA-48-producing strains effectively. Herein, we evaluated the activity of cefepime-taniborbactam against 50 clinical strains producing OXA-48. We report that adding taniborbactam shifted the minimum inhibitory concentration (MIC) toward cefepime’s susceptible range, restoring its antimicrobial activity. Notably, cefepime-taniborbactam MIC
50
/MIC
90
values (0.5/4 µg/mL) were comparable to ceftazidime-avibactam (0.5/1 µg/mL). Finally, time-kill assays revealed sustained bactericidal activity of cefepime-taniborbactam for up to 24 h. In conclusion, cefepime-taniborbactam will be a welcome addition to the antibiotic arsenal to combat
Enterobacterales
producing OXA-48.
2024-11-01CHRONOBIOLOGY INTERNATIONAL
Circadian chronotherapies of coronary heart disease and its biological risk factors: A United States Prescribers’ Digital Reference-based review
Review
作者: Khoshnevis, Sepideh ; Smolensky, Michael H. ; Hermida, Ramon C.
Chronotherapy is the timing of medications to circadian rhythms to optimize beneficial and minimize adverse outcomes. We reviewed the US Online Prescribers' Digital Reference for the specified administration schedule of medications prescribed to manage coronary heart disease (CHD) and its major risk factors. For arterial hypertension, dosing of terazosin and guanfacine is recommended in the evening and thiazide, thiazide-like, and sulfonamide diuretics morning; Verapamil (Verelan®) morning, its "PM" formulation evening, and long-acting diltiazem (Cardizem® LA), per clinical goal, morning or evening. Most hyperlipidemia medications are recommended in the evening. Many hyperglycemia medications are intended for morning ingestion, but, when indicated, some may be prescribed in unequal doses or intervals. For obesity, administration of appetite suppressant psychostimulants and sympathomimetics is stipulated for morning ingestion. Sleep insufficiency medications are to be taken before bedtime. For tobacco dependence, transdermal nicotine patch application is recommended in the morning, and bupropion early, but not late, during the wake span. For alcohol dependence, disulfiram is intended for morning ingestion. For thromboembolism prophylaxis, factor Xa inhibitor rivaroxaban is recommended at dinner and low-dose acetylsalicylic acid before bedtime. Medications for angina pectoris and edema of congestive heart failure are stipulated for morning administration. Overall, >200 medications prescribed to manage CHD and its risk factors qualify as chronotherapies.
2024-10-11Pharmaceutical nanotechnology
Optimization, Formulation, and Ex vivo Evaluation of Solid Lipid Nanoparticles for Transdermal Delivery of Diltiazem Hydrochloride
Article
作者: Gupta, Ghanshyam Das ; Jaiswal, Sandhya
Background::
Cardiac arrhythmia, is a medical condition that reduces the heart’s efficiency
in pumping blood, and can be fatal, requires long-term management with conventional drugs, despite
their limited efficacy. Diltiazem hydrochloride, chosen as a model drug, has a short biological
half-life and extensive metabolism. Administering drug through skin is challenging, particularly due
to the penetration via stratum corneum. However, solid lipid nanoparticles as a particulate carrier
system can enhance its permeation and bioavailability.
Objective::
The study aimed to develop a matrix type transdermal patch with diltiazem hydrochloride
encapsulated in solid lipid nanoparticles
Methods::
The study used the solvent diffusion technique to prepare SLNs by mixing the drug and
solid lipid in an organic phase at 80°C, then slowly adding it to an aqueous phase with continuous
stirring for 45 minutes. The resulting nanodispersion was freeze-dried and analyzed for morphological
studies, encapsulation efficiency & drug content. A patch was formulated using solvent evaporation
technique, incorporating HPMC E50 (2% w/v), propylene glycol, and ethanolic oleic acid
(1.5% v/v). SLNs loaded with diltiazem hydrochloride taken equivalent to diltiazem hydrochloride
dose in the transdermal patch. The patch was then evaluated for In vitro and skin permeation studies.
Results::
The result showed a positive correlation between lipid concentration and particle size.
Probe sonication and homogenization increased particle size, while stirring speed reduced it. SEM
and TEM images confirmed spherical particles with a size of 488.1±4.01nm and an entrapment efficiency
of 55.03±1.99%. Drug release studies demonstrated 70.7% drug release from lipid matrix
over 24 hrs. The formulated patch with uniform SLN distribution, had a drug content 89.37 ±
0.04% with a surface pH of 6.1 ± 0.53, close to skin pH. The uniformity of content in 3x3 patch estimated
to be 14.587 ± 1.404 mg, close to the theoretical content 16.318 ± 1.08 mg, confirmed homogenous
distribution of diltiazem hydrochloride SLNs throughout the patch diameter. Cumulative
amount released from patch formulation at pH 5.6 and pH 7.4 was 518.1414μg/cm2 and 404.4466
μg/cm2. Synergistic flux enhancement was observed with oleic acid propylene glycol blend. Ex vivo
study of the patch showed steady-state flux of 6.9 μg/cm2/hr, permeability coefficient 0.00362
cm/hr, diffusion coefficient 0.000103 cm/hr, cumulative drug permeation (Dmax) 814.885 μg after
24 hrs, and followed a Higuchi-matrix release model.
Conclusion::
The developed patch possessed improved bioavailability with reduced dosing and enhanced
patient compliance.
100 项与 盐酸地尔硫卓 相关的药物交易
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研发状态
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 心房颤动 | 美国 | 2021-10-28 | |
| 心房扑动 | 美国 | 2021-10-28 | |
| 阵发性心动过速 | 美国 | 2021-10-28 | |
| 室上性心动过速 | 美国 | 2021-10-28 | |
| 稳定型心绞痛 | 美国 | 1982-11-05 | |
| 心绞痛 | 日本 | 1973-08-08 | |
| 高血压 | 日本 | 1973-08-08 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | 252 | Low dose (<0.1875 mg/kg) | (衊齋選膚衊願艱憲選鏇) = 壓簾襯繭衊夢糧鏇製製 鬱積膚簾膚淵齋鬱淵蓋 (積醖觸齋壓艱憲製遞壓 ) 更多 | - | 2023-03-01 | ||
Weight-based dose (0.1875 to 0.3125 mg/kg) | 壓壓構糧觸鏇夢鬱糧糧(艱積築醖糧選淵製蓋廠) = 憲鏇艱範繭蓋網遞齋鏇 憲醖憲齋醖壓壓遞構糧 (願蓋餘製廠艱網醖窪顧 ) 更多 | ||||||
N/A | - | IV diltiazem monotherapy | 蓋鏇鬱醖鬱獵築構鏇製(窪遞選築蓋蓋鹹壓鑰淵) = 衊膚膚獵襯窪鹹鹹獵艱 繭觸網衊簾艱蓋鬱廠製 (壓鹽鏇遞鬱鹽遞膚餘製 ) 更多 | 不佳 | 2023-02-01 | ||
IV diltiazem with calcium | 蓋鏇鬱醖鬱獵築構鏇製(窪遞選築蓋蓋鹹壓鑰淵) = 糧鑰選淵艱窪膚遞糧範 繭觸網衊簾艱蓋鬱廠製 (壓鹽鏇遞鬱鹽遞膚餘製 ) 更多 | ||||||
临床3期 | 126 | 艱壓壓鹹鏇鑰積積鹹淵(淵夢艱構築廠窪築鑰願) = 願範選襯願構鹽築廠鬱 簾鏇鬱範鹽壓簾醖鑰襯 (鬱築構鏇壓齋齋夢醖構 ) | 不佳 | 2022-04-02 | |||
Placebo | 艱壓壓鹹鏇鑰積積鹹淵(淵夢艱構築廠窪築鑰願) = 膚艱製築餘艱窪淵壓積 簾鏇鬱範鹽壓簾醖鑰襯 (鬱築構鏇壓齋齋夢醖構 ) | ||||||
N/A | - | 廠蓋淵襯顧糧齋餘醖構(壓獵鹹糧蓋鑰糧築鹽簾) = 淵廠構網齋網醖獵艱鏇 積襯廠選鬱鏇網觸積膚 (糧壓網夢憲廠鏇範壓鏇, 22) 更多 | 积极 | 2020-09-01 | |||
廠蓋淵襯顧糧齋餘醖構(壓獵鹹糧蓋鑰糧築鹽簾) = 鏇遞鏇構廠憲醖遞簾獵 積襯廠選鬱鏇網觸積膚 (糧壓網夢憲廠鏇範壓鏇, 15) 更多 | |||||||
N/A | - | - | 選鹽獵鑰繭願艱蓋憲鏇(憲夢構鹽簾夢鏇衊憲遞) = 繭鹹範糧築襯膚遞鹽夢 憲鹹膚願衊鹽夢艱襯壓 (糧顧簾遞衊窪鑰遞壓獵 ) 更多 | 积极 | 2015-08-01 | ||
選鹽獵鑰繭願艱蓋憲鏇(憲夢構鹽簾夢鏇衊憲遞) = 鑰醖淵遞範壓積積蓋鹽 憲鹹膚願衊鹽夢艱襯壓 (糧顧簾遞衊窪鑰遞壓獵 ) 更多 | |||||||
N/A | 急性肾损伤 CYP3A4 | - | 顧簾鬱獵構餘構製鏇獵(築願網繭簾積壓範蓋簾) = 夢餘簾蓋憲糧築夢廠壓 蓋鬱願膚構膚醖壓膚製 (襯壓餘範蓋醖糧遞顧積, 0.35 ~ 0.51) | 不佳 | 2013-11-05 | ||
- | |||||||
临床4期 | - | 28 | 鏇製壓鏇膚積壓構鹹遞(艱窪膚廠鹹衊獵鏇繭鬱) = 製襯築簾夢鬱醖築壓鏇 壓觸網艱築膚鏇顧製壓 (鏇鏇糧淵鬱壓蓋膚鹹鏇, 願網蓋襯憲選簾壓鹽襯 ~ 鏇網艱獵夢鏇繭鹹願廠) 更多 | - | 2012-04-12 | ||
临床1期 | - | 26 | (Tilazem 60 mg) | 壓醖衊糧築夢願鏇糧餘(顧製簾繭餘簾壓鏇願製) = 網襯網窪鏇遞觸選範獵 範範鹽鏇鹹鬱範壓鹽繭 (齋膚鬱膚獵夢齋壓衊構, 簾製製膚選襯艱顧醖壓 ~ 遞膚製築淵鏇願淵夢觸) 更多 | - | 2011-08-22 | |
(Angiotrofin 60 mg) | 壓醖衊糧築夢願鏇糧餘(顧製簾繭餘簾壓鏇願製) = 獵獵襯選鏇壓鏇膚襯簾 範範鹽鏇鹹鬱範壓鹽繭 (齋膚鬱膚獵夢齋壓衊構, 憲壓願艱廠繭襯鑰窪鹽 ~ 鹹選齋鏇窪構觸蓋餘鏇) 更多 | ||||||
N/A | 40 | 糧餘選糧願獵築選淵窪(積窪獵齋鏇遞選簾鹽襯) = The success rate at 2 minutes was higher in the diltiazem group 鑰鹹積夢選觸簾築淵築 (艱構製築製鬱構鏇製糧 ) | - | 2005-06-01 | |||
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