快樂小藥師
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Dexmedetomidine(Precedex®


機轉:

Selective alpha2-adrenoceptor agonist with anesthetic and sedative properties thought to be due to activation of G-proteins by apha2a-adrenoceptors in the brainstem resulting in inhibition of norepinephrine release; peripheral alpha2b-adrenoceptors are activated at high doses or with rapid I.V. administration resulting in vasoconstriction.

DEXDOMITOR機轉 

 


長相:

這是人用的

Precedex.gif 

這是動物用的:

DEXDOMITOR盒裝 

DEXDOMITOR vial 


用途:

Sedation of initially intubated and mechanically ventilated patients during treatment in an intensive care setting; sedation prior to and/or during surgical or other procedures of nonintubated patients

 

對於加護病房中,剛插管的病患或是使用呼吸器的病患的鎮靜劑。

非核准用途:

Unlabeled uses include premedication prior to anesthesia induction with thiopental; relief of pain and reduction of opioid dose following laparoscopic tubal ligation; as an adjunct anesthetic in ophthalmic surgery; treatment of shivering; premedication to attenuate the cardiostimulatory and postanesthetic delirium of ketamine; use in children


使用方式:

 

Dosing: Adults 

Individualized and titrated to desired clinical effect. Manufacturer recommends duration of infusion should not exceed 24 hours; however, randomized clinical trials have demonstrated efficacy and safety comparable to lorazepam and midazolam with longer-term infusions of up to approximately 5 days. (Pandharipande, 2007; Riker, 2009).

ICU sedation: I.V.: Initial: Loading infusion (optional; see "Note" below) of 1 mcg/kg over 10 minutes, followed by a maintenance infusion of 0.2-0.7 mcg/kg/hour; adjust rate to desired level of sedation; titration no more frequently than every 30 minutes may reduce the incidence of hypotension (Gerlach, 2009)

Note: Loading infusion: Administration of a loading infusion may increase the risk of hemodynamic compromise. For this indication, the loading dose may be omitted. Maintenance infusion: Dosing ranges between 0.2-1.4 mcg/kg/hour have been reported during randomized controlled clinical trials (Pandharipande, 2007; Riker, 2009). Although infusion rates as high as 2.5 mcg/kg/hour have been used, it is thought that doses >1.5 mcg/kg/hour do not add to clinical efficacy (Venn, 2003).

Procedural sedation: I.V.: Initial: Loading infusion of 1 mcg/kg (or 0.5 mcg/kg for less invasive procedures [eg, ophthalmic]) over 10 minutes, followed by a maintenance infusion of 0.6 mcg/kg/hour, titrate to desired effect; usual range: 0.2-1 mcg/kg/hour

Fiberoptic intubation (awake): I.V. Initial: Loading infusion of 1 mcg/kg over 10 minutes, followed by a maintenance infusion of 0.7 mcg/kg/hour until endotracheal tube is secured.

Dosing: Elderly

ICU sedation: I.V.: Refer to adult dosing. Dosage reduction may need to be considered. No specific guidelines available. Dose selections should be cautious, at the low end of dosage range; titration should be slower, allowing adequate time to evaluate response.

Procedural sedation: I.V.: Refer to adult dosing: Initial: Loading infusion of 0.5 mcg/kg over 10 minutes; Maintenance infusion: Dosage reduction should be considered.

 



獸醫使用狀況可以參照以下範例:


Examples of actual uses of DEXDOMITOR as a sedative and analgesic in dogs include:
Oral exam, treatment
Radiographs
Skin treatments (biopsies, scrapings, etc.)
Ear exam, treatment
Grooming (bathing, nail trims)
Ophthalmic exam, treatment
Anal gland treatment
Other (orthopedic, bandage change, enemas)


Examples of actual uses of DEXDOMITOR as a sedative and analgesic in cats include:
Oral exam, treatment
Grooming and bathing
Abscess treatment, suture removal, or skin biopsy
Radiography and ultrasound
Ear examination and treatment of otitis
Other diagnostic procedures or treatment

除此之外,也可以用在貓貓狗狗的麻醉:


FDA-approved for sedation and analgesia in dogs
Proven safe and effective in dogs as young as 16 weeks of age
Effects observed within 5 minutes
Peak effects observed at 15 minutes (IV) and 30 minutes (IM)
Recovery without ANTISEDAN® (atipamezole hydrochloride) occurred by 180 minutes (IV) and +180 minutes (IM)


FDA-approved for sedation and analgesia in cats
Proven safe and effective in cats as young as 12 weeks of age
Effects observed within 5 minutes
Peak effects observed at 15 - 60 minutes
Recovery occurred by 180 minutes


FDA-approved as a preanesthetic in dogs
Approved for concurrent use with commonly used induction and anesthetic agents
Markedly reduces anesthetic requirements (30% – 60%)
based on DEXDOMITOR dose and type of induction or inhalant agent
The concurrent use of DEXDOMITOR prior to or with an anesthetic or its use in the presence of other sedatives has not been evaluated in cats


Reversible with ANTISEDAN
Reversible with equal volume of ANTISEDAN administered IM
ANTISEDAN is FDA-approved for use in dogs only


這邊我們看到另外一個藥物了:ANTISEDAN(atipamezole hydrochloride)

雖然不是今天的主角,不過就順便介紹一下:為了避免混淆,這個藥物的敘述會用綠色標起來

antisedan.jpg 


ANTISEDAN is administered intramuscularly, regardless of the route used for DEXDOMITOR or DOMITOR. The concentration of ANTISEDAN has been formulated so that the volume of injection is the same (mL for mL) as the recommended dose volume of DEXDOMITOR or DOMITOR. Although injection volumes are the same, the concentration of ANTISEDAN (5.0 mg/mL) is 10 times that of DEXDOMITOR (0.5 mg/mL) and 5 times that of DOMITOR (1.0 mg/mL). 


ANTISEDAN may be given any time following DEXDOMITOR or DOMITOR administration. Dogs that are sedated but ambulatory may be treated with ANTISEDAN if warranted.)

重要資訊:Do not use DEXDOMITOR or DOMITOR in dogs and DEXDOMITOR in cats with cardiovascular disease, respiratory disorders, liver or kidney diseases, or in conditions of shock, severe debilitation, or stress due to extreme heat, cold or fatigue. As with all a2-adrenoceptor agonists, the potential for isolated cases of hypersensitivity, including paradoxical response (excitation), exists. Arrhythmias, bradycardia, emesis were observed in the DEXDOMITOR and DOMITOR clinical field studies in dogs. DEXDOMITOR has not been evaluated for use in breeding, pregnant, or lactating dogs and cats. In cats, vomiting, urinary incontinence and hypersalivation were observed with DEXDOMITOR. Refer to the full prescribing information for more safety information.


好的,我們現在回到本來的藥

 

腎功能不全時:不需調整劑量

懷孕分級:C


給藥方式:

Administer using a controlled infusion device. Must be diluted in 0.9% sodium chloride solution to achieve the required concentration (4 mcg/mL) prior to administration. Advisable to use administration components made with synthetic or coated natural rubber gaskets. Parenteral products should be inspected visually for particulate matter and discoloration prior to administration. If loading dose used, administer over 10 minutes; may extend to 20 minutes to further reduce vasoconstrictive effects. Titration no more frequently than every 30 minutes may reduce the incidence of hypotension when used for ICU sedation (Gerlach, 2009).

 

 

其他溶劑相容性

Stable in D5W, LR, 0.9% NS, 20% mannitol, plasma substitute

 

 

旁插(Y-site)可以使用的藥物:

Alfentanil, amikacin, aminophylline, amiodarone, ampicillin, ampicillin and sulbactam, atracurium, atropine, azithromycin, aztreonam, bumetanide, butorphanol, calcium gluconate, cefazolin, cefepime, cefotaxime, cefotetan, cefoxitin, ceftazidime, ceftizoxime, ceftriaxone, cefuroxime, chlorpromazine, cimetidine, ciprofloxacin, cisatracurium, clindamycin, dexamethasone, digoxin, diltiazem, diphenhydramine, dobutamine, dolasetron, dopamine, doxycycline, droperidol, enalaprilat, ephedrine, epinephrine, erythromycin, esmolol, etomidate, famotidine, fenoldopam, fentanyl, fluconazole, furosemide, gentamicin, glycopyrrolate, granisetron, haloperidol, heparin, hydrocortisone sodium succinate, hydromorphone, hydroxyzine, inamrinone, isoproterenol, ketorolac, labetalol, levofloxacin, lidocaine, linezolid, lorazepam, magnesium sulfate, meperidine, methylprednisolone sodium succinate, metoclopramide, metronidazole, midazolam, milrinone, mivacurium, morphine, nalbuphine, nitroglycerin, nitroprusside, norepinephrine, ofloxacin, ondansetron, pancuronium, phenylephrine, piperacillin, piperacillin and tazobactam, potassium chloride, procainamide, prochlorperazine, promethazine, propofol, ranitidine, rapacuronium, remifentanil, rocuronium, sodium bicarbonate, succinylcholine, sufentanil, sulfamethoxazole and trimethoprim, theophylline, thiopental, ticarcillin and clavulanate, tobramycin, vancomycin, vecuronium, verapamil.

不能旁插的藥物:

Amphotericin B, diazepam

 

主要藥理交互作用:

Antidepressants (Alpha2-Antagonist): May diminish the hypotensive effect of Alpha2-Agonists. Risk D: Consider therapy modification

Beta-Blockers: May enhance the rebound hypertensive effect of Alpha2-Agonists. This effect can occur when the alpha2-agonist is abruptly withdrawn. Exceptions: Levobunolol; Metipranolol. Risk D: Consider therapy modification

CYP2A6 Inhibitors (Moderate): May decrease the metabolism of CYP2A6 Substrates. Risk C: Monitor therapy

CYP2A6 Inhibitors (Strong): May decrease the metabolism of CYP2A6 Substrates. Risk D: Consider therapy modification

Hypotensive Agents: May enhance the adverse/toxic effect of other Hypotensive Agents. Risk C: Monitor therapy

Iobenguane I 123: Alpha2-Agonists may diminish the therapeutic effect of Iobenguane I 123. Risk X: Avoid combination

MAO Inhibitors: May enhance the orthostatic effect of Orthostasis Producing Agents. Risk C: Monitor therapy

Serotonin/Norepinephrine Reuptake Inhibitors: May diminish the antihypertensive effect of Alpha2-Agonists. Risk C: Monitor therapy

Tricyclic Antidepressants: May diminish the antihypertensive effect of Alpha2-Agonists. Risk D: Consider therapy modification

 

 


延伸閱讀:如果你對這個藥物很有興趣,可以參考一下這篇:

Treating Agitation With Dexmedetomidine in the ICU (Dimensions of Critical Care Nursing:May/June 2009 - Volume 28 - Issue 3 - pp 102-109)

這是antisedan的仿單:點我以PDF開啟

這是Dexmedetomidine的仿單:點我以PDF開啟

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  • 您好!想請問一下此藥物Dexmedetomidine只能靜脈注射嘛? 是否可貼服.口服?
  • 目前看到的劑型都是針劑

    快樂小藥師 於 2011/07/03 23:06 回覆

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