Medicine composition and application thereof

Abstract

Medicine composition is characterized by comprising an effective medicine component comprising dexmedetomidine hydrochloride and ketamine hydrochloride. The medicine composition has a synergistic effect, is particularly used for sedation before examination of a child and has a significant effect, and various examinations can be performed on the sick child safely and effectively. The successful sedation rate can reach 96% or higher, the medicine takes effect quickly, and the analepsia controllability is high. Meanwhile, the medicine composition has little side effect and has no obvious adverse reactions, the child taking the medicine composition is normal in heart rate, blood pressure and the like and has no emergence agitation phenomena and the like, and the medicine has high safety.

Description

technical field [0001] The invention relates to a pharmaceutical composition, in particular to a sedative pharmaceutical composition. Background technique [0002] Pre-examination sedation, especially for children, is a clinical problem that needs to be solved urgently. The use of safe and effective drugs is the key to ensure that children can successfully complete various examinations. [0003] At present, the commonly used sedative drugs before examination in China are oral chloral hydrate or midazolam, and intramuscular injection of sodium lumina. The efficacy and use of these sedatives have the following problems: (1) chloral hydrate oral agent: it is the most commonly used sedative agent for children before examination in outpatient clinics. Because its mouthfeel is very bitter, many children refuse to take it or cause vomiting after taking it. Increased risk of aspiration, even life threatening. In addition, the metabolites of chloral hydrate are active and sometimes...

AI Technical Summary

Problems solved by technology

The efficacy and use of these sedatives have the following problems: (1) chloral hydrate oral agent: it is the most commonly used sedative agent for children before examination in outpatient clinics. Because its mouthfeel is very bitter, many children refuse to take it or cause vomiting after taking it. Increased risk of aspiration, even life-threatening

In addition, the metabolites of chloral hydrate are active and sometimes cause delayed awakening; at the same time, the first-pass effect of the drug is obvious, and the sedative effect is uncertain, which often leads to sedation failure, and many children often need repeated medications

(2) Oral midazolam: the sedative effect is not good, and the success rate is only 60-75%

(3) Lumin sodium intramuscular injection: the success rate of sedation is about 80%, but it is accompanied by painful stimulation, which will cause harm to children

[0004] Dexmedetomidine hydrochloride is the dextro isomer of medetomidine, which is a derivative of imidazoles and is a highly selective α2 receptor agonist. The chemical name is: (+)-4-(S) -[1-(2,3-Dimethylphenyl)ethyl]-1H-imidazole hydrochloride acts on the α2 receptor in the locus coeruleus nucleus of the brainstem to produce a good sedative effect. The bioavailability of medetomidine is 81.8% (72.6-92.1%), so adults and children can produce obvious sedative effect after nasal instillation of dexmedetomidine, and it has no inhibitory effect on the respiratory center; but 2ug alone After sedation with dexmedetomidine / kg, it is easy to be awakened by external stimuli, and the awakening rate can reach about 50%, resulting in failure of sedation; large doses of dexmedetomidine hydrochloride (>2ug / kg) intranasally can produce heartbeat Brady phenomenon

[0005] Ketamine is an NMDA receptor antagonist, which has analgesic, sedative and sympathetic stimulation effects, but generally its use requires a large dose, which can easily cause blood pressure to rise and there is agitation during the recovery period

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