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diltiazem (diltiazam, Aptalis / diltiazem, SURECAPS)

✓ Approved

Adare Pharma Solutions · CACNA1C · Small Molecule

What is diltiazem?

diltiazem is a small molecule developed by Adare Pharma Solutions. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand Namesdiltiazam, Aptalis, diltiazem, SURECAPS
CompanyAdare Pharma Solutions
Drug ClassSmall Molecule
Molecular TargetCACNA1C
RouteOral (PO)
StatusApproved
Sources: ClinicalTrials.gov, Adare Pharma Solutions

Mechanism of Action

Molecular Targets

diltiazem acts on 1 molecular target:

CACNA1Ccalcium voltage-gated channel subunit alpha1 C (CACNL1A1, CACNA1C-IT2)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

diltiazem is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Cardiac disordersAngina pectoris✓ Approved

Related Research Articles

PubMedImmunobiology2026-08-28

Luhong formula attenuates cardiomyocyte hypoxia/reoxygenation injury in vitro through SLC7A11-mediated ferroptosis.

Zhang Saiwen S, Zhou Dan D, Zhou Yaozhong Y, Cai Wan W

This study investigates whether Luhong Formula (LHF) inhibits hypoxia/reoxygenation (H/R)-induced ferroptosis in cardiomyocytes and the underlying mechanism. H9c2 cells were subjected to H/R injury and treated with LHF extract, diltiazem (positive control), or Fer-1 (ferroptosis inhibitor). CCK-8, colorimetric assays, and transmission electron microscopy showed that LHF significantly increased cell viability, reduced LDH release, restored SOD activity and GSH content, and alleviated mitochondrial damage. FerOrange staining and C11-BODIPY flow cytometry revealed that LHF decreased intracellular Fe2+ levels and lipid ROS accumulation. Immunofluorescence and Western blot demonstrated that LHF up-regulated GPX4 expression, showing effects comparable to those of Fer-1 and diltiazem in this in vitro system. Using SLC7A11-overexpressing and -silencing stable cell lines, we found that SLC7A11 overexpression mimicked LHF's protective effects, while SLC7A11 silencing partially reversed them. Co-immunoprecipitation confirmed that H/R increased SLC7A11 ubiquitination, whereas LHF reduced this modification, thereby stabilizing SLC7A11 protein. Collectively, LHF is associated with reduced SLC7A11 ubiquitination, which correlates with up-regulated GPX4 and blocked ferroptosis, alleviating H/R injury in cardiomyocytes. These findings provide preliminary evidence for a potential regulatory effect of LHF on SLC7A11 protein stability, although direct measurements of protein half-life and detailed ubiquitin topology require further investigation. These findings suggest that LHF inhibits H/R-induced ferroptosis in H9c2 cells, at least in part, through the SLC7A11/GPX4 pathway, which may contribute to its cardioprotective effect.

PMID 42664531
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PubMedJournal of veterinary internal medicine2026-08-27

Effect of amiodarone, diltiazem, or both to achieve strict heart rate control in dogs with atrial fibrillation.

Tjostheim Sonja S SS, Kellihan Heidi B HB, Stepien Rebecca L RL

Dogs with atrial fibrillation (AF) live longer if heart rate is strictly controlled (SHRC, 24-h mean heart rate ≤ 125 beats per minute [bpm]). Amiodarone and diltiazem are used to lower ventricular response rate (VRR) in dogs with AF, but information about their relative efficacy for achieving SHRC is lacking. Describe heart rate response with sequential escalation of amiodarone or diltiazem monotherapy to combination therapy. Thirteen client-owned dogs with AF. Prospective cohort study with an adaptive treatment protocol. Dogs with AF with mean daily heart rate (MDHR) > 125 bpm (baseline, 24-h Holter) were randomized to receive amiodarone or diltiazem at standard doses. Dogs were reassessed 21 days later, and the other drug (amiodarone or diltiazem) was added if SHRC was not achieved. Dogs were then reassessed at 42 and 63-147 days after starting treatment. If MDHR >125 bpm at any repeat assessment, the second drug was added. Timing of final assessment was dependent on whether treatment was escalated. Monotherapy with amiodarone and diltiazem was initially used in 7 and 6 dogs, respectively. SHRC was achieved in 3 dogs (amiodarone, n = 2; diltiazem, n = 1) at first follow-up. At last follow-up, 11 of 13 dogs were receiving both drugs (median [range] 50 [20-153] days). Combination therapy of amiodarone and diltiazem did not result in SHRC (139 [94-160] bpm) in most dogs (7/11, 64%). Monotherapy with amiodarone or diltiazem or combination therapy of amiodarone/diltiazem did not achieve SHRC in most dogs in this study.

PMID 42658783
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PubMedNeurological sciences : official journal of the Italian Neurological Society and of the Italian Society of Clinical Neurophysiology2026-08-25

A novel CACNA1S variant associated with diltiazem-related worsening of hypokalemic periodic paralysis: a case report.

Sugiura Hidenori H, Watanabe Kazuki K, Furuhashi Kai K, Kawano Tatsuhiro T et al.

Hypokalemic periodic paralysis (HypoPP) is a skeletal muscle channelopathy characterized by recurrent episodes of transient paralysis associated with hypokalemia. Most cases are caused by heterozygous missense variants in CACNA1S, which encodes the α1 subunit of the skeletal muscle L-type calcium channel (CaV1.1). Known triggers include excessive carbohydrate intake, rest after strenuous exercise, and emotional stress; however, worsening potentially associated with the use of L-type calcium channel blockers (LTCCBs) has not been well documented. A 68-year-old man with HypoPP and a five-generation family history of the disease developed increased frequency of paralytic attacks and progressive muscle weakness after initiation of LTCCBs (nifedipine and diltiazem) for vasospastic angina. Exome sequencing and segregation analysis identified a novel heterozygous CACNA1S variant (NM_000069.3:c.4097T > G, p.(Met1366Arg)), which co-segregated with disease among genotyped affected family members and was classified as likely pathogenic. Despite continued nifedipine therapy, paralytic episodes ceased following discontinuation of diltiazem, and muscle strength improved. The p.(Met1366Arg) variant is located in the S6 segment of CaV1.1, outside the canonical S4 arginine residues implicated in most cases of CACNA1S-related HypoPP; nevertheless, strong intrafamilial segregation evidence supports its pathogenicity. Furthermore, its proximity to the diltiazem-binding site raises the possibility of altered drug-channel interactions. The observed diltiazem-associated worsening of HypoPP may be variant-specific rather than a class effect of LTCCBs. Nevertheless, careful monitoring may be warranted when prescribing these agents to patients with HypoPP.

PMID 42637926
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PubMedBMJ open2026-08-20

Potentially inappropriate prescribing in Iranian elderly population: a nationwide claims-based analysis.

Kharaghani Mohammad Amin MA, Kianipour Reza R, Ataei Seyed Mohammad-Navid SM, Ebrahimpour Sholeh S et al.

Potentially inappropriate prescribing (PIP) in the elderly is associated with adverse outcomes and increased healthcare use. We aimed to estimate its prevalence and pattern among the elderly population of Iran using the Screening Tool of Older Persons' Prescriptions (STOPP) criteria. Retrospective, population-based observational study. Nationwide data of Iran Health Insurance Organization (IHIO) prescription claims from 24 provinces (21 March 2014 to 19 March 2017). Adults aged ≥60 years with at least one prescription in the dataset were included. The study comprised 2 696 300 older adults who received 28 575 400 prescriptions. Not applicable. Using a two-stage curation process, we selected STOPP version 3 criteria that could be operationalised from dispensing data alone (age, Anatomical Therapeutic Chemical code, dose, duration and concurrent use). For each criterion, we calculated prescription and patient level PIP prevalence overall and among at-risk prescriptions. Across the curated STOPP criteria, 313 315 prescriptions issued to 131 012 patients met at least one PIP criterion. The most frequent PIPs were concurrent beta blocker and diltiazem use (99 027 prescriptions; 1.26% of patients), benzodiazepine therapy ≥4 weeks (89 240 prescriptions; 1.60% of patients), ≥2 anticholinergic drugs (47 079 prescriptions; 0.78% of patients) and concomitant non-steroidal anti-inflammatory drug plus anticoagulant (25 685 prescriptions; 0.38% of patients). PIPs involving acetylcholinesterase inhibitors, ticlopidine, clonidine and methyldopa were rare. In this nationwide claims-based study, about 5% of elderly Iranians were exposed to PIPs, particularly chronic benzodiazepine use, excessive anticholinergic burden and high-risk cardiovascular and antithrombotic combinations. Our findings provide concrete targets for claims-based surveillance and interventions to improve prescribing safety in Iran's ageing population.

PMID 42624577
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PubMedCritical care explorations2026-08-01

Severe Diltiazem Poisoning Managed With CytoSorb Hemoadsorption and Supportive Therapies: A Case Report.

Cox Juul M JM, Verwaaijen Julia A M JAM, Hendriks Ruben M F RMF, Smeets Dorien D et al.

Severe intoxication with nondihydropyridine calcium channel blockers, such as diltiazem, is associated with high morbidity and mortality. Evidence supporting extracorporeal treatment strategies remains limited. This case integrates serial toxicokinetic measurements with adjunctive hemoadsorption in sustained-release diltiazem poisoning. A 73-year-old man presented with coma, complete atrioventricular block, refractory hypotension, and severe lactic acidosis. Despite optimized supportive therapy including vasopressors, calcium supplementation, hyperinsulinemic-euglycemic therapy, and continuous renal replacement therapy, he remained hemodynamically unstable. CytoSorb hemoadsorption was initiated 6 hours after ICU admission. Shortly thereafter, sinus rhythm was restored, serum lactate rapidly declined, and vasopressor and insulin requirements were progressively reduced, allowing discontinuation of extracorporeal support. The patient recovered and was discharged home. Retrospective analysis demonstrated elevated diltiazem concentrations with delayed, capacity-limited elimination. This case supports considering hemoadsorption in unstable patients with severe diltiazem poisoning despite conventional measures and highlights the need for systematic pharmacokinetic evaluation in future studies.

PMID 42538738
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PubMedJACC. Case reports2026-07-30

AVNRT With Intermittent Aberrancy-Mimicking Ventricular Tachycardia: One Tachycardia, Two QRS Morphologies.

Madishetty Vineet V, Sojitra Badal B, Sachs Vincent V, Xiang Kun K

Regular wide-complex tachycardia often prompts concern for ventricular tachycardia, yet supraventricular tachycardia with aberrancy is a frequent mimic. A 36-year-old male presented with palpitations, dizziness, and presyncope after ambulatory monitoring documented tachycardia >200 beats/min. Telemetry showed recurrent regular tachycardia with alternating narrow and wide QRS morphologies at a similar cycle length. Vagal maneuvers, adenosine, and diltiazem transiently slowed/terminated the rhythm, but it recurred, necessitating cardioversion. Electrophysiology study induced typical atrioventricular nodal re-entrant tachycardia with rate-dependent aberrancy; slow-pathway ablation rendered the tachycardia noninducible. Unchanged cycle length during narrow-to-wide transitions supports a single supraventricular tachycardia mechanism with a functional bundle branch block. When QRS morphology alternates without cycle-length change, suspect supraventricular tachycardia with aberrancy and confirm with electrophysiology testing.

PMID 42530209
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