A Review of Structure Activity Relationship of Amiodarone and Its Derivatives

Siddiqui, Moiz A.; Khan, Asif; Zaka, Mehreen

doi:10.4236/ojmc.2016.62003

Cited by 3 publications

(1 citation statement)

References 19 publications

(6 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…In addition, this can sometimes cause serious adverse reactions in all organs [ 27 , 28 ]. Thus, the two iodine atoms in the central benzene ring, which give it a structure similar to triiodothyronine, are responsible for thyroid gland disorders and hypo- and hyperthyroidism [ 29 ] by inhibiting iodine transport into the thyroid gland [ 30 ].…”

Section: Results Case Studies In Different Pharmacological Classesmentioning

confidence: 99%

Drugs Associated with Adverse Effects in Vulnerable Groups of Patients

Ștefan,

Nechita,

Dragostin

et al. 2024

Clinics and Practice

View full text Add to dashboard Cite

In recent years, a series of recommendations have been issued regarding the administration of drugs because of awareness of the serious side effects associated with certain classes of drugs, especially in vulnerable patients. Taking into account the obligation of the continuous improvement of professionals in the medical fields and the fact that we are in the midst of a “malpractice accusations pandemic”, through this work, we propose to carry out a “radiography” of the scientific literature regarding adverse effects that may occur as a result of the interaction of drugs with the physiopathological particularities of patients. The literature reports various cases regarding different classes of drugs administration associated with adverse effects in the elderly people, such as fluoroquinolones, which can cause torsade de pointes or tendinopathy, or diuretics, which can cause hypokalemia followed by torsade de pointes and cardiorespiratory arrest. Also, children are more prone to the development of adverse reactions due to their physiological particularities, while for pregnant women, some drugs can interfere with the normal development of the fetus, and for psychiatric patients, the use of neuroleptics can cause agranulocytosis. Considering the physiopathological particularities of each patient, the drug doses must be adjusted or even completely removed from the treatment scheme, thus requiring the mandatory active participation both of clinician pharmacists and specialists in the activity of medical-pharmaceutical analysis laboratories within the structure of hospitals.

show abstract

Section: Results Case Studies In Different Pharmacological Classesmentioning

confidence: 99%

Drugs Associated with Adverse Effects in Vulnerable Groups of Patients

Ștefan,

Nechita,

Dragostin

et al. 2024

Clinics and Practice

View full text Add to dashboard Cite

show abstract

Photoredox‐Catalyzed Decarboxylative Oxidation of Arylacetic Acids

Sakakibara

Cooper

Murakami

et al. 2018

Chemistry An Asian Journal

View full text Add to dashboard Cite

show abstract

Inhibition of Clostridioides difficile toxins TcdA and TcdB by the amiodarone derivative dronedarone

Matylitsky,

Krieg,

Schumacher

et al. 2024

Naunyn-Schmiedeberg's Arch Pharmacol

View full text Add to dashboard Cite

The dreaded nosocomial pathogen Clostridioides difficile causes diarrhea and severe inflammation of the colon, especially after the use of certain antibiotics. The bacterium releases two deleterious toxins, TcdA and TcdB, into the gut, which are mainly responsible for the symptoms of C. difficile-associated diseases (CDADs). Both toxins are capable of entering independently into various host cells, e.g., intestinal epithelial cells, where they mono-O-glucosylate and inactivate Rho and/or Ras GTPases, important molecular switches for various cellular functions. We have shown recently that the cellular uptake of the Clostridioides difficile toxins TcdA and TcdB (TcdA/B) is inhibited by the licensed class III antiarrhythmic drug amiodarone (Schumacher et al. in Gut Microbes 15(2):2256695, 2023). Mechanistically, amiodarone delays the cellular uptake of both toxins into target cells most likely by lowering membrane cholesterol levels and by interfering with membrane insertion and/or pore formation of TcdA/B. However, serious side effects, such as thyroid dysfunction and severe pulmonary fibrosis, limit the clinical use of amiodarone in patients with C. difficile infection (CDI). For that reason, we aimed to test whether dronedarone, an amiodarone derivative with a more favorable side effect profile, is also capable of inhibiting TcdA/B. To this end, we tested in vitro with various methods the impact of dronedarone on the intoxication of Vero and CaCo-2 cells with TcdA/B. Importantly, preincubation of both cell lines with dronedarone for 1 h at concentrations in the low micromolar range rendered the cells less sensitive toward TcdA/B-induced Rac1 glucosylation, collapse of the actin cytoskeleton, cell rounding, and cytopathic effects, respectively. Our study points toward the possibility of repurposing the already approved drug dronedarone as the preferable safer-to-use alternative to amiodarone for inhibiting TcdA/B in the (supportive) therapy of CDADs.

show abstract

A Review of Structure Activity Relationship of Amiodarone and Its Derivatives

Cited by 3 publications

References 19 publications

Drugs Associated with Adverse Effects in Vulnerable Groups of Patients

Drugs Associated with Adverse Effects in Vulnerable Groups of Patients

Photoredox‐Catalyzed Decarboxylative Oxidation of Arylacetic Acids

Inhibition of Clostridioides difficile toxins TcdA and TcdB by the amiodarone derivative dronedarone

Contact Info

Product

Resources

About