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Propofol Sale

(Synonyms: 丙泊酚; 2,6-Diisopropylphenol) 目录号 : GC39424

Propofol 有效直接地激活 GABAA 受体和抑制谷氨酸受体介导的兴奋性突触传递。Propofol 具有抗伤害感受特性,可用于镇静和催眠。

Propofol Chemical Structure

Cas No.:2078-54-8

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100mg
¥495.00
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产品描述

Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic[1].

[1]. R Nadeson, et al. Antinociceptive Properties of Propofol: Involvement of Spinal Cord Gamma-Aminobutyric acid(A) Receptors. J Pharmacol Exp Ther . 1997 Sep;282(3):1181-6.

Chemical Properties

Cas No. 2078-54-8 SDF
别名 丙泊酚; 2,6-Diisopropylphenol
Canonical SMILES OC1=C(C(C)C)C=CC=C1C(C)C
分子式 C12H18O 分子量 178.27
溶解度 DMSO: 100 mg/mL (560.95 mM); Water: 1 mg/mL (5.61 mM) 储存条件 Store at 2-8°C
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1 mM 5.6095 mL 28.0473 mL 56.0947 mL
5 mM 1.1219 mL 5.6095 mL 11.2189 mL
10 mM 0.5609 mL 2.8047 mL 5.6095 mL
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Research Update

Propofol

J Pain Symptom Manage 2010 Sep;40(3):466-70.PMID:20816571DOI:10.1016/j.jpainsymman.2010.07.001.

Therapeutic Reviews aim to provide essential independent information for health professionals about drugs used in palliative and hospice care. The content is also available on www.palliativedrugs.com and will feature in future editions of the Hospice and Palliative Care Formulary USA and its British and Canadian counterparts. The series editors welcome feedback on the articles (hq@palliativedrugs.com).

Is Propofol the optimal sedative in gastrointestinal endoscopy?

Acta Gastroenterol Belg 2018 Oct-Dec;81(4):520-524.PMID:30645922doi

Propofol is a sedative agent commonly used for sedation in gastrointestinal endoscopy. Its pharmacologic properties render Propofol an almost ideal drug to achieve and maintain the targeted level of sedation in even complex gastrointestinal procedures. When compared with other sedative agents, Propofol is associated with better patient and endoscopist satisfaction and shorter recovery times. Furthermore, Propofol can be combined with other sedatives to reduce the total dosage required to achieve the targeted sedation. Its safety is demonstrated by multiple studies, in which adverse events occurred very rarely. Nevertheless, the use of Propofol by non-anesthesiologists is illegal in many countries and in those permitted, a structured curriculum with clinical training must first be successfully completed. However, various studies have shown that non-anesthesiologist administration of Propofol is comparable in efficacy and safety to administration by an anesthesiologist and more cost-effective. The results of numerous studies indicate that Propofol is superior in many aspects compared with traditional sedative agents.

Propofol: Milk of Amnesia

Cell 2018 Sep 20;175(1):10-13.PMID:30217361DOI:10.1016/j.cell.2018.08.031.

This year's Lasker Clinical Research Award goes to James Baird Glen for the discovery and development of the anesthetic Propofol. Patients benefit from its fast onset and rapid systemic clearance, eliminating the prolonged sedation effects experienced with earlier agents. In just 30 years, Propofol has been adopted around the world for safe and controlled induction of anesthesia.

Effects of Propofol on ischemia-reperfusion and traumatic brain injury

J Crit Care 2020 Apr;56:281-287.PMID:32001426DOI:10.1016/j.jcrc.2019.12.021.

Oxidative stress exacerbates brain damage following ischemia-reperfusion and traumatic brain injury (TBI). Management of TBI and critically ill patients commonly involves use of Propofol, a sedation medication that acts as a general anesthetic with inherent antioxidant properties. Here we review available evidence from animal model systems and clinical studies that Propofol protects against ischemia-reperfusion injury. However, evidence of Propofol toxicity in humans exists and manifests as a rare complication, "Propofol infusion syndrome" (PRIS). Evidence in animal models suggests that brain injury induces expression of the p75 neurotrophin receptor (p75NTR), which is associated with proapoptotic signaling. p75NTR-mediated apoptosis of neurons is further exacerbated by Propofol's superinduction of p75NTR and concomitant inhibition of neurotrophin processing. Propofol is toxic to neurons but not astrocytes, a type of glial cell. Evidence suggests that Propofol protects astrocytes from oxidative stress and stimulates astroglial-mediated protection of neurons. One may speculate that in brain injury patients under sedation/anesthesia, Propofol provides brain tissue protection or aids in recovery by enhancing astrocyte function. Nevertheless, our understanding of neurologic recovery versus long-term neurological sequelae leading to neurodegeneration is poor, and it is also conceivable that Propofol plays a partial as yet unrecognized role in long-term impairment of the injured brain.

Propofol anesthesia

Vet Clin North Am Small Anim Pract 1999 May;29(3):747-78.PMID:10332821DOI:10.1016/s0195-5616(99)50059-4.

Although questions may still remain regarding the use of this unique sedative-hypnotic drug with anesthetic properties in high-risk patients, our studies have provided cardiopulmonary and neurological evidence of the efficacy and safety of Propofol when used as an anesthetic under normal and selected impaired conditions in the dog. 1. Propofol can be safely and effectively used for the induction and maintenance of anesthesia in normal healthy dogs. Propofol is also a reliable and safe anesthetic agent when used during induced cardiovascular and pulmonary-impaired conditions without surgery. The Propofol requirements to induce the safe and prompt induction of anesthesia prior to inhalant anesthesia with and without surgery have been determined. 2. The favorable recovery profile associated with Propofol offers advantages over traditional anesthetics in clinical situations in which rapid recovery is important. Also, Propofol compatibility with a large variety of preanesthetics may increase its use as a safe and reliable i.v. anesthetic for the induction and maintenance of general anesthesia and sedation in small animal veterinary practice. Although Propofol has proven to be a valuable adjuvant during short ambulatory procedures, its use for the maintenance of general anesthesia has been questioned for surgery lasting more than 1 hour because of increased cost and marginal differences in recovery times compared with those of standard inhalant or balanced anesthetic techniques. When Propofol is used for the maintenance of anesthesia in combination with a sedative/analgesic, the quality of anesthesia is improved as well as the ease with which the practitioner can titrate Propofol; therefore, practitioners are able to use i.v. anesthetic techniques more effectively in their clinical practices. 3. Propofol can induce significant depression of respiratory function, characterized by a reduction in the rate of respiration. Potent alpha 2 sedative/analgesics (e.g., xylazine, medetomidine) or opioids (e.g., oxymorphone, butorphanol) increase the probability of respiratory depression during anesthesia. Appropriate consideration of dose reduction and speed of administration of Propofol reduces the degree of depression. Cardiovascular changes induced by Propofol administration consist of a slight decrease in arterial blood pressures (systolic, mean, diastolic) without a compensatory increase in heart rate. Selective premedicants markedly modify this characteristic response. 4. When coupled with subjective responses to painful stimuli, EEG responses during Propofol anesthesia provide clear evidence that satisfactory anesthesia has been achieved in experimental dogs. When Propofol is used as the only anesthetic agent, a higher dose is required to induce an equipotent level of CNS depression compared with the situation when dogs are premedicated. 5. The Propofol induction dose requirement should be appropriately decreased by 20% to 80% when Propofol is administered in combination with sedative or analgesic agents as part of a balanced technique as well as in elderly and debilitated patients. As a general recommendation, the dose of Propofol should always be carefully titrated against the needs and responses of the individual patient, as there is considerable variability in anesthetic requirements among patients. Because Propofol does not have marked analgesic effects and its metabolism is rapid, the use of local anesthetics, nonsteroidal anti-inflammatory agents, and opioids to provide postoperative analgesia improves the quality of recovery after Propofol anesthesia. 6. The cardiovascular depressant effects of Propofol are well tolerated in healthy animals, but these effects may be more problematic in high-risk patients with intrinsic cardiac disease as well as in those with systemic disease. In hypovolemic patients and those with limited cardiac reserve, even small induction doses of Propofol (0.75-1.5 mg/kg i.v.) can produce profound hypotens