Pharmacodynamics and pharmacokinetics of intramuscular dexmedetomidine

Scheinin, Harry; Karhuvaara, Sakari; Olkkola, Klaus T.; Kallio, Antero; Anttila, Markku; Vuorilehto, Lauri; Scheinin, Mika

doi:10.1038/clpt.1992.182

Cited by 64 publications

(31 citation statements)

References 2 publications

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“…These finding are supported by studies examining pharmacokinetics of some drugs administered to various sites. Peak plasma concentration of 0.34 ± 0.1 µg·l -1 of the drug was achieved after 1.6-1.7 h when 1.5 µg·kg -1 dexmedetomidine was injected to the gluteus muscle (Scheinin et al 1992). When 2.0 µg·kg -1 dexmedetomidine was administered to the deltoid muscle, the peak plasma concentration of 0.81 ± 0.27 ng·ml -1 of the drug was achieved after 12 (2-60) min (Dyck et al 1993).…”

Section: Discussionmentioning

confidence: 87%

The effect of site (deltoid or gluteus muscle) of intramuscular administration of anaesthetic drugs on the course of immobilisation in macaque monkeys (Macaca mulatta)

et al. 2012

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The aim of this work was to study the effect of site of intramuscular administration of anaesthetic drugs on the course of immobilisation in macaque monkeys (Macaca mulatta). Twenty macaque monkeys were given medetomidine (25 µg·kg -1 ) and ketamine (3 mg·kg -1 ) intramuscularly to the deltoid (n = 10 animals) or gluteus (n = 10 animals) muscles. Behavioural changes, loss of aggressiveness, immobilisation time and cardiorespiratory changes were recorded. The effect of drugs was reversed after 20 min by i.m. administration of atipamezole at the dose of 250 µg·kg -1 . Highly significant differences (P < 0.001) were found between groups with gluteal or deltoid administration of drugs on the onset of immobilisation effect (71.3 s and 108.3 s, respectively), and immobilisation time (152.7 s and 254.4 s, respectively). In the gluteus muscle group, the grasp reflex was still present at the beginning of immobilisation and slowly wore off in 15-45 s. The same was valid for muscle tone. There were no differences in cardiorespiratory parameters in any of the groups. Animals of both groups recovered in 3-6 min after atipamezole administration. Administration of drugs to the deltoid muscle resulted in a more rapid onset and increased effect of immobilisation than administration to the gluteus muscle. Both in veterinary and human medicine, injection to the deltoid muscle may be more convenient in all cases, when rapid and more prominent effect is desirable as in premedication before surgery or in emergency medicine. The study is the first to compare the effect of administering drugs to different muscles and the results may improve the practice of intramuscular injections in animals and in humans. Medetomidine, ketamine, atipamezole, intramuscular injection

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Section: Discussionmentioning

confidence: 87%

The effect of site (deltoid or gluteus muscle) of intramuscular administration of anaesthetic drugs on the course of immobilisation in macaque monkeys (Macaca mulatta)

et al. 2012

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“…Its pharmacology and mechanism of action have been reviewed elsewhere. 5 Briefly, alpha-2 receptors modulate the activity of the autonomic nervous and cardiovascular systems. Activation of the alpha-2 receptor in peripheral blood vessels causes vasoconstriction and, in the autonomic ganglia, stimulation of the receptor inhibits the release of catecholamines.…”

Section: Objectif : Décrire L'usage De Dexmédétomidine Pour La Sédatimentioning

confidence: 99%

“…Activation of the alpha-2 receptor in peripheral blood vessels causes vasoconstriction and, in the autonomic ganglia, stimulation of the receptor inhibits the release of catecholamines. 5,6 Activation of alpha-2 receptors in the central nervous system, particularly in the locus ceruleus, may cause a significant reduction in central sympathetic flow and result in sedation and increased vagal activity. [7][8][9] Sedation with dexemedetomidine resembles light sleep.…”

Section: Objectif : Décrire L'usage De Dexmédétomidine Pour La Sédatimentioning

confidence: 99%

Dexmedetomidine sedation in a pediatric cardiac patient scheduled for mri

Young

2005

Can J Anesth/J Can Anesth

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P Pu ur rp po os se e: : To describe the use of dexmedetomidine for sedation in a critically ill infant undergoing magnetic resonance imaging (MRI).C Cl li in ni ic ca al l f fe ea at tu ur re es s: : A nine-month-old 5.1 kg infant was to have an MRI study of the thorax. The infant had multiple congenital cardiac anomalies which had been partially corrected surgically. After administration of atropine, 0.1 mg iv, a loading dose of dexmedetomidine (1 µg·kg -1 iv) was administered over ten minutes followed by a continuous infusion of 0.5 µg·kg -1 ·hr -1 for maintenance. Propofol 5 mg iv were administered after the loading dose of dexemedetomidine to produce somnolence. Anesthetic conditions for performing the MRI were excellent. The infant remained motionless, breathing spontaneously. Hemodynamics remained stable throughout the procedure. Recovery was rapid and uneventful.

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“…4,5 In addition, activation of α2 receptors in peripheral blood vessels causes vasoconstriction and, in the autonomic ganglia, stimulation of the receptor inhibits release of catecholamines. 4,6 These features of dexmedetomidine make it a better fit for sedation of TOF patients (particularly small infants) with hypercyanotic spells. We report an 8-day-old patient with TOF in whom dexmedetomidine produced effective sedation and management of hypercyanotic spells.…”

Section: Introductionmentioning

confidence: 99%

O uso de dexmedetomidina na sedação de crises hipercianóticas em um recém-nascido com tetralogia de Fallot

Senzaki¹,

Ishido²,

Iwamoto³

et al. 2008

J. Pediatr. (Rio J.)

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Objective: Sedation is an important step in the management of patients with hypercyanotic spells associated with tetralogy of Fallot (TOF) to ameliorate and prevent recurrence of cyanosis. This case report illustrates the effectiveness of dexmedetomidine-induced sedation in the management of hypercyanotic spells in a neonate with TOF.Description: An 8-day-old term newborn patient with TOF showed hypercyanotic spells, as indicated by an abrupt decrease in arterial saturation (SpO 2 ) level measured by a pulse oximeter from 80% to as low as 50%, when the patient became irritable and agitated. We started continuous infusion of dexmedetomidine at a dose of 0.2 μg/kg/min without a loading bolus injection. About half an hour after commencement of dexmedetomidine infusion, the patient reached an acceptable level of sedation, together with a drop in heart rate by approximately 20 beats/min. There was no apparent respiratory depression or marked change in blood pressure. SpO 2 was also stable during dexmedetomidine infusion.The patient underwent a successful Blalock-Taussig shunt operation on the next day of admission.Comments: Dexmedetomidine may be useful for the management of hypercyanotic spells in pediatric patients with TOF.

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Pharmacodynamics and pharmacokinetics of intramuscular dexmedetomidine

Cited by 64 publications

References 2 publications

The effect of site (deltoid or gluteus muscle) of intramuscular administration of anaesthetic drugs on the course of immobilisation in macaque monkeys (Macaca mulatta)

The effect of site (deltoid or gluteus muscle) of intramuscular administration of anaesthetic drugs on the course of immobilisation in macaque monkeys (Macaca mulatta)

Dexmedetomidine sedation in a pediatric cardiac patient scheduled for mri

O uso de dexmedetomidina na sedação de crises hipercianóticas em um recém-nascido com tetralogia de Fallot

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