M2 receptor antagonists(Muscarinic acetylcholine receptor M2 antagonists), Potassium channel blockers, VDCCs blockers(Voltage-gated calcium channel blockers)

Therapeutic Areas

Cardiovascular Diseases

Active Indication

Ventricular ArrhythmiaArrhythmias, Cardiac

Inactive Indication-

Originator Organization

Pfizer Inc.

Active Organization

Dainippon Pharmaceutical Co., Ltd.

Sumitomo Pharma Co., Ltd.

Pfizer Japan, Inc.

Inactive Organization-

License Organization-

Drug Highest PhaseApproved

First Approval Date

Japan (01 Jan 1994),

Arrhythmias, Cardiac

Regulation-

Structure/Sequence

Molecular FormulaC22H31ClN2O

InChIKeyHFIHPVIVQSWZBV-ROSXHPEZSA-N

CAS Registry61477-94-9

View All Structures (2)

100 Clinical Results associated with Pirmenol Hydrochloride Hydrate

100 Translational Medicine associated with Pirmenol Hydrochloride Hydrate

100 Patents (Medical) associated with Pirmenol Hydrochloride Hydrate

170

Literatures (Medical) associated with Pirmenol Hydrochloride Hydrate

21 Feb 2025·Biological and Pharmaceutical Bulletin

<i>α</i><sub>1</sub>-Adrenoceptor Blockade by Class I Antiarrhythmic Drugs in Guinea Pig Thoracic Aorta as Revealed by Mechanical and Fluorescence Displacement Analysis

Article

Author: Tanaka, Hikaru ; Igarashi, Hiro ; Namekata, Iyuki ; Shirai, Kuniaki ; Kawazoe, Ayaka ; Tsukada, Kohei ; Seki, Maika ; Hamaguchi, Shogo ; Miyahara, Marina

The effects of thirteen Vaughn Williams class I antiarrhythmic drugs on the α₁-adrenergic receptor-mediated contraction were examined in thoracic aorta tissue preparations isolated from the guinea pig. Cibenzoline, quinidine, aprindine, and ranolazine, as well as prazosin, inhibited the phenylephrine-induced contraction with pA₂ values of 5.64, 5.59, 5.61, 5.08, and 8.50, respectively, but not prostaglandin F_2α-induced. These drugs reduced the staining of the smooth muscle layer by fluorescent prazosin. Propafenone inhibited the phenylephrine-induced contraction with an apparent pA₂ value of 5.31 and reduced the staining by fluorescent prazosin, but also inhibited the prostaglandin F_2α-induced contraction. Other class I antiarrhythmic drugs, disopyramide, pirmenol, procainamide, lidocaine, mexiletine, flecainide, pilsicainide, and GS-458967, affected neither the contraction by phenylephrine nor the fluorescent staining by prazosin. These results indicate that among the class I antiarrhythmic drugs, cibenzoline, aprindine, and propafenone, as well as quinidine and ranolazine, have α₁-adrenoceptor-blocking activity at therapeutically relevant concentrations.

01 Jan 2022·Journal of Clinical Pharmacy and TherapeuticsQ4 · MEDICINE

Detecting drug‐drug interactions that increase the incidence of long QT syndrome using a spontaneous reporting system

Q4 · MEDICINE

Article

Author: Matsuo, Jun ; Yamaori, Satoshi

WHAT IS KNOWN AND OBJECTIVEDrug-induced long QT syndrome (diLQTS) is a rare but serious adverse drug reaction. Drug-drug interaction (DDI) is one of the risk factors for the development of diLQTS. However, the combinations of drugs that increase the risk of diLQTS have not been extensively investigated. This study was performed to analyse the potential DDIs that elevate the incidence of diLQTS using a spontaneous reporting system.METHODSThe Japanese Adverse Drug Event Report database from April 2004 to January 2020 was used to assess adverse event reports. We calculated the reporting odds ratio and 95% confidence interval for signal detection.RESULTS AND DISCUSSIONSignals for concomitant use risk were detected in 31 drug combinations. Combinations of antipsychotics and antidepressants were the most common (olanzapine & fluvoxamine, olanzapine & trazodone, quetiapine & paroxetine, sulpiride & fluvoxamine, sulpiride & trazodone). Sixteen, 17 and 21 combinations were designated as requiring precaution for concomitant use in at least one of the package inserts in Japan, the United States and the United Kingdom, respectively, although no such precautions were described for the remaining combinations. On the contrary, a combination of bepridil & clarithromycin was categorized as "X (avoid combination)" and two combinations (chlorpromazine & haloperidol, amiodarone & metildigoxin) were classified as "D (modify regimen)" in the Lexicomp^® risk rating.WHAT IS NEW AND CONCLUSIONThis study identified 31 combinations of drugs that may elevate the risk of diLQTS. The use of these drug combinations should be monitored more carefully in future.

01 Jun 2021·Drug Metabolism and PharmacokineticsQ4 · MEDICINE

Estimation of absolute oral bioavailability without performing an intravenous clinical study

Q4 · MEDICINE

Article

Author: Akiyoshi, Takeshi ; Ohtani, Hisakazu ; Iwata, Risa ; Imaoka, Ayuko

The absolute oral bioavailability (BA) of drugs are yet to be determined, and intravenous pharmacokinetic studies are currently considered indispensable for determining the BA values of oral drugs. The aim of this study was to develop and validate a novel approach to estimating BA values without intravenous pharmacokinetic data. Based on the drug inclusion criteria, such as exhibiting a urinary recovery rate of (R_u) of ≥20% in a clinical study, 13 drugs were included in the present study, and pharmacokinetic data for them were collected from the literature. The fraction excreted unchanged into urine (f_e) was calculated for healthy subjects by dividing the R_u value by the total recovery rate. The contribution of renal excretion to total clearance from the systemic circulation (R_ren) was estimated by subjecting oral clearance and creatinine clearance to regression in subjects with normal and impaired renal function. BA was estimated as f_e/R_ren and compared with the observed BA (BA_obs). The predicted BA values for 9 drugs fell within ±20% of their BA_obs. The examined approach makes it possible to estimate BA values for drugs with mean renal excretion values in healthy subjects and oral clearance in subjects with various renal function, without intravenous pharmacokinetic data.

100 Deals associated with Pirmenol Hydrochloride Hydrate

External Link

KEGG	Wiki	ATC	Drug Bank
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R&D Status

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Indication	Country/Location	Organization	Date
Ventricular Arrhythmia	Japan	Pfizer Japan, Inc.	05 Oct 1994
Arrhythmias, Cardiac	Japan	Sumitomo Pharma Co., Ltd.	01 Jan 1994

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