Disease relevance of Caroverine

• The findings suggest that local application of caroverine on the RWM for the treatment of excitotoxicity-related inner ear diseases, such as tinnitus and noise-induced hearing loss, might be both safe and more efficacious while avoiding high blood and CSF caroverine levels seen with systemic administration [1].
• Caroverine was well tolerated, showed no sedative side effects, and no epileptic seizures were observed [2].
• On the cerebro-protective effects of caroverine, a calcium-channel blocker and antiglutamatergic drug: double-blind, placebo-controlled, EEG mapping and psychometric studies under hypoxia [3].
• Caroverine was found to offer significant protection of the cochlear function against noise-induced hearing loss [4].
• Ubiquinol and the papaverine derivative caroverine prevent the expression of tumour- promoting factors in adenoma and carcinoma colon cancer cells induced by dietary fat [5].

Psychiatry related information on Caroverine

• In 4 cases of manifest delirium tremens the infusional application of caroverine was openly tested with dose ranges of 2.5-5.0 mg/kg (24 h) [6].
• We present a randomized double-blind study on the efficacy of caroverine in the treatment of alcohol withdrawal symptoms [6].
• Therefore the clinically available quinoxaline dione caroverine provides a new approach to a successful treatment of tinnitus, sudden hearing loss and speech discrimination disorders in presbyacusis [7].

High impact information on Caroverine

• The antioxidant activity of caroverine [8].
• Caroverine exhibits competitive AMPA antagonism, and at higher concentrations, noncompetitive NMDA antagonism [8].
• Lipid peroxidation of liposomal membranes was suppressed in the presence of caroverine [8].
• Since glutamate is likely to be the major mediator of neurotoxicity in the central nervous system, the selective glutamate-antagonism of caroverine is of particular interest, due to its putative neuroprotective competence [9].
• Diltiazem also depressed the ventral root potential (DR-VRP), whereas caroverine augmented both the polysynaptic component in the ventral root reflex and the size of the DR-VRP [10].

Chemical compound and disease context of Caroverine

• Magnesium and the quinoxaline derivative Caroverine, which have already been tested in humans, exhibit a statistically significant otoneuroprotective action in noise-induced hearing loss and tinnitus [11].

Biological context of Caroverine

• Pharmacokinetics of caroverine in the inner ear and its effects on cochlear function after systemic and local administrations in Guinea pigs [1].
• In spontaneously firing SA node cells, caroverine (1 X 10(-7) M-1 X 10(-5) M) decreased the action potential amplitude (APA) and the maximal rate of depolarization (MRD) in a concentration-dependent manner [12].
• Caroverine as well as verapamil had a frequency-dependent inhibitory action on atrial DT, which indicates that both of the drugs have an influence on the kinetics of slow channel of cardiac fibers [12].

Anatomical context of Caroverine

• Since reactive oxygen species are supposed to be involved in the pathogenesis of inner ear diseases in which caroverine shows beneficial effects, the present study aimed to investigate the antioxidant properties of caroverine [8].
• Local administration of caroverine on the round window membrane (RWM) could be a more effective means of administration to avoid systemic side/adverse effects [1].
• Our results show much higher caroverine concentrations in the perilymph with lower concentrations in CSF and plasma following local applications compared with systemic administration [1].
• The effects of caroverine on electrical activity of isolated rabbit sinoatrial (SA) node cells and atrial muscle fibers and on contractile force of atrial muscle preparations were examined [12].
• Results. It was shown that caroverine could significantly protect the cochlea against impulse noise trauma [13].

Associations of Caroverine with other chemical compounds

• The group B Ca2+ channel blocking agent caroverine was tested against meprobamate in inpatient treatment of alcohol withdrawal [6].
• In order to understand the mechanism of this antioxidant action of Caroverine we studied the interaction of Caroverine with superoxide radicals, hydroxyl radicals and peroxynitrite [14].
• Different action of memantine and caroverine on glutamatergic transmission in the mammalian cochlea [15].

Gene context of Caroverine

• This prospective study, which conformed with good clinical practice (GCP-conform), tested the concept that the topical transtympanic administration of the quinoxaline derivative Caroverine promises a new approach to the treatment of tinnitus [16].

Analytical, diagnostic and therapeutic context of Caroverine

• 1. In a double-blind, placebo-controlled study, the acute antihypoxidotic properties of the calcium-channel blocking and antiglutamatergic caroverine were investigated utilizing blood gas analysis, EEG mapping and psychometry under a transient, reversible, hypoxic hypoxidosis [3].
• Two different doses of caroverine were applied onto the round window membrane with gelfoam, followed by one-third-octave band noise centered at 6.3 kHz (110 dB SPL) for 1 h [4].
• Multivariate analysis of EEG mapping data demonstrated that caroverine exerted a significant action on human brain function, as compared with placebo, at all given dosages, as early as in the 1st and as late as in the 8th hour after both intravenous and oral administration during resting (R-EEG) and vigilance-controlled recording (V-EEG) [17].
• Topical administration of Caroverine in somatic tinnitus treatment: proof-of-concept study [16].

References