TINNEX INJECTION
(CAROVERINE IINJECTION 160 mg/8 ml)
Caroverine [1-(diethylaminoethyl) -3 – (p-methoxybenzyl) – 1, 2 – hydroquinoxaline-2-one] is a quinoxaline derivative developed in the 1960s. Caroverine, an N-methyl-D-aspartate and α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor antagonist together with antioxidant activity, has been shown to protect the inner ear from excitotoxicity and to be effective in the treatment of tinnitus, sudden hearing loss and speech discrimination disorders in presbyacusis.
In recent years, it is on grounds of its quinoxline-dione structure, glutamate antagonism of him excitatory, afferent synapses of the cochlear inner hair cells and its neuroprotective properties that caroverine has been investigated as a new drug in the pharmacological treatment of tinnitus.
Pharmacodynamic:
Caroverine also acts as a reversible glutamate antagonist in afferent cochlear synapse. Theoretical justification for the introduction of caroverine in the pharmacotherapy of tinnitus is that glutamate, as a key neurotransmitter in the central nervous system, is the most likely transmitter-substance in the afferent cochlear synapse (Ehrenberger-K eta al., 1992; Ehrenberger-K et al., 1995a; Ehrenberger-K et al., 1995b). A frequent type of inner ear tinnitus, the cochlear-synaptic tinnitus, is caused by a dysfunction of the synapse between inner hair cells and afferent dendrites of the auditory nerve. On the subsynaptic membrane, two different types of receptors, working as a dual receptor system, arte actually stimulated by glutamate. The NMDA (N-methyl-D-asparatate) receptors and the non-NMDA quisqualate and kainite receptors. The dual receptor system is responsible for a typical pattern of depolarization: non-NMDA receptors generate fast depolarizing response, where as NMDA receptors generate a current of longer duration. Under normal synapse function conditions, the typical interplay of the two different time courses of depolarization are observed. They result in an irregular spontaneous fiber activity. Under pathological conditions, spontaneous receptor-dependent depolarization patterns mimic sound- induced patterns differing from the normally irregular pattern. They are perceived as tinnitus by the patient. This may occur under excessive sitmualtion of the receptors, when glutamate develops a neurotoxic activity.
Pharmacokinetic:
Metabolism of caroverine depends to a considerable extent on individual genetic polymorphis such that quantitative evaluations are impossible. Caroverine is chiefly metabolized into glucuronic acid conjugates including demethyl caroverine and other as yet unidentified quinoxaline derivatives which are excreted in the urine (up to approx 33%). Non-metabolized caroverine is not detected in urine.Caroverine is mainly excreted in feces.
Caroverine has a half-life of approx 25 mins. The highest levels of identified metabolites are reached within about 75 mins with an approx half-life of 2 hrs. no data regarding the efficacy of the principal metabolites are available
Indication:
In case of cochlear- synaptic tinnitus (Of any duration) have shown favorable results
Dosages & Administration:
1 ampoule in 100 ml of saline slow infusion under experts observation with gradation system
In case of tinnitus: Dosage is determined on an individual basis. Maximum up to160 mg of Caroverine in 100 ml of physiological saline as slow controlled intravenous infusion (2 - 3 ml/minute) up till maximum improvement of the tinnitus ,Before tinnitus disappear totally, it should be stopped- Further dosage can lead to worsening of the symptoms.
Side effect:
The signs and symptoms that are produced after the acute overdosage of Caroverine include Dizziness, Headache.
The symptomatic adverse reactions produced by Caroverine are more or less tolerable and if they become severe, they can be treated symptomatically, these include Tachycardia,Dry mouth, Blurred vision, Urinary retention, Dry mouth.
Contraindicated:
Hypersensitivity to Caroverine, acute stomach and intestinal ulcers, children under 3 years. To be administered in children of above 3 years only in case of strong indications. For Adult it is safe
Precaution:
Intravenous administration should be done slowly. Vascular damage should be expected in case of intra-arterial dosage.
Normal Saline & Caroverine has to be used in infusion
Drug Interaction:
None
Presentation:
1 Ampoule in box containing patient booklet ,user manual & gradation card.