Handbook of experimental pharmacology
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Handb Exp Pharmacol · Jan 2008
ReviewPharmacokinetics and pharmacodynamics of GPI 15715 or fospropofol (Aquavan injection) - a water-soluble propofol prodrug.
Propofol (2,6-diisopropylphenol) is inadequably soluble in water and is therefore formulated as a lipid emulsion. This may have disadvantages when propofol is used to provide total intravenous anaesthesia or especially during long-term sedation. There has been considerable interest in the development of new propofol formulations or propofol prodrugs. ⋯ We found a significantly greater V(c), V(dss), significantly shorter alpha- and beta-half-life and a longer MRT (mean residence time) for propofol(G). The pharmacodynamic potency of propofol(G) appears to be higher than propofol when measured by EEG and clinical signs of hypnosis. In summary, GPI 15715 or fospropofol was well suited to provide anaesthesia or conscious sedation.
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Anesthesia cannot be defined in an unambiguous manner. The essential components of general anesthesia are absence of consciousness and pain. This translates into two particular qualities: (1) sedation and hypnosis, i.e., mental blockade and (2) analgesia/antinociception, i.e., sensory blockade. ⋯ Clinical assessment of analgesia requires a conscious patient, so antinociception is difficult to measure. Several methods of objective quantification on the basis of electrical brain activity are discussed including EEG and evoked potentials. Despite numerous indexes of the hypnotic component of anesthesia, there is no parameter that unambiguously quantifies the level of mental or sensory blockade.
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Asthma is a heterogeneous disorder of unknown etiology that manifests as recurrent episodes of coughing, wheezing, and breathlessness. These symptoms are often debilitating and exacerbations usually are unexpected, resulting in work or school absences, limitations in activity, reduced quality of life, and personal and economic hardships. ⋯ However, asthma remains a global public health problem, and the hope is that newer therapies targeting specific biological mediators of asthma, particularly antibody-mediated therapies, offer exciting new modes to the control of this disease. We will review some of these therapies, with the majority of attention devoted to anti-IgE therapy which has been approved for treatment of adult and childhood asthma by the US Food and Drug Administration (FDA) since 2003.
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Handb Exp Pharmacol · Jan 2008
ReviewHypnotic and opioid anesthetic drug interactions on the CNS, focus on response surface modeling.
This chapter will present the conceptual and applied approaches to capture the interaction of anesthetic hypnotic drugs with opioid drugs, as used in the clinical anesthetic state. The graphic and mathematical approaches used to capture hypnotic/opiate anesthetic drug interactions will be presented. This chapter is not a review article about interaction modeling, but focuses on specific drug interactions within a quite narrow field, anesthesia.
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Handb Exp Pharmacol · Jan 2008
ReviewAdvanced technologies and devices for inhalational anesthetic drug dosing.
Technological advances in micromechanics, optical sensing, and computing have led to innovative and reliable concepts of precise dosing and sensing of modern volatile anesthetics. Mixing of saturated desflurane flow with fresh gas flow (FGF) requires differential pressure sensing between the two circuits for precise delivery. The medical gas xenon is administered most economically in a closed circuit breathing system. ⋯ Delivery of xenon is presented, followed by a discussion of direct injection of volatile anesthetics and of a device designed to conserve anesthetic drugs. Next, innovative sensing technologies are presented for reliable control and precise metering of the delivered volatile anesthetics. Finally, we discuss the technical challenges of automatic control in low-flow and closed circuit breathing systems in anesthesia.