Pet Scanning and Propofol Action

 

Positron Emission Tomography (PET) and functional Magnetic Resonnance Imaging (fMRI) allow researchers to study brain function in vivo. Those techniques are used to refine our understanding of the nature of anesthetic effects as well as of the influence of anesthetic drugs on sensory and pain transmission.

 

How they work.

 

PET.

 

PET uses a combination of scintigraphic and computerized tomography techniques. A biological compound labeled with a radioactive tracer (11C, 13N, 15O, 18F) is injected into a subject so that its distribution in the target tissue can be determined. Depending on the information desired, a variety of compounds can be labeled. For functional brain studies, 15O labeled water is often used for determination of regional Cerebral Blood Flow (rCBF) based on the assumption that changes in rCBF are coupled with those of neuronal activity. Cerebral metabolic rate studies are performed with labeled glucose or oxygen. It is also possible to study neurotransmission by looking at the displacement of a labeled ligand from its binding sites 1. For example, 11C benztropine, an M1 and M2 non-specific antagonist, is used by our group to study cholinergic muscarinic transmission under anesthesia. 

 

PET has been used for more than a decade for localization of human cognitive operations 2. The basis of PET studies is to submit a group of individuals to a series of different conditions and to statistically compare the images to determine the physiologic changes induced by a given condition. Examples of conditions are: increasingly painful stimuli, increasing levels of drug sedation, or a more complex pattern mixing painful stimuli at increasing levels of sedation.

 

fMRI.

 

fMRI  uses a different principle. Again, the basis of the studies is to compare changes in brain activation induced between conditions in a strictly controlled experimental environment, but there is no need for radioactive tracers, and the temporal resolution is much better than with PET.

 

 

Brain imaging and Anesthesia.

 

 

Brain imaging offers unique possibilities for improving our knowledge of anesthetic effects. Anesthesia induces a host of dose-specific and controllable changes in CNS function. Our knowledge of propofol pharmacology and the availability of powerful tools to achieve and maintain stable drug concentrations allow us to use propofol as a prototypical anesthetic drug and as modulators of consciousness. Stable levels, or conditions in the brain imaging vocabulary, can be obtained that correspond to specific levels of sedation. Dose specific changes in brain activity can be measured, and the neurophysiological correlates of the regional changes can be explored. Brain imaging allows us to have a systems approach to the investigation of mechanisms of anesthesia based on the premise that, propofol, and by extension anesthetic drugs, possibly has a dose-dependant effect on specific neural systems.

 

 

PET studies on propofol and regional cerebral effects.

 

Michael Alkire and his group (U.C. Irvine) have done a series of propofol studies in human volunteers using 18fluorodeoxyglucose (FDG). They studied the glucose metabolic rate in human volunteers3 and showed that it was not uniform. Cortical metabolism was depressed more than sub-cortical and marked differences in regional cortical changes were seen. In another study, they correlated EEG changes with the cerebral metabolic reduction caused by propofol and isoflurane and proposed that a physiologic link exists between those variables.

 

Our group has studied the effects of propofol on the CNS using PET. In a first study, we have determined the effect of different levels of propofol sedation, from light sedation to unconsciousness, on rCBF using 15H2O. We found a significant decrease in rCBF of the thalamus, the orbito-frontal cortices, and a large area of the medial parieto-occipital cortex extending bilaterally to the parieto-occipital sulcus area4. These anatomical sites are involved in the control of consciousness5 and in various integrative and associative tasks. In particular, given the importance of the thalamic function in conscious processes, this study, as well as others show that “the level of functional thalamic activity occurring in a brain during anesthesia is likely to be related in some manner to a person’s level of consciousness”[a]. These results support the hypothesis that propofol has regional effects and that certain brain structures might have a specific sensitivity to anesthetic effect.

 

The neural pathways for conducting and perceiving pain and vibro-tactile stimulation are well known and their activation following a stimulus can be clearly and accurately shown using PET 6; 7. It is the very nature of anesthesia to alter the perception of external stimuli thus allowing the performance of noxious operations but very little is known on the exact mechanism by which such a disruption of neural conduction happens. Is the stimulus blocked at the level of the dorsal horn, the thalamus, the primary or secondary sensory cortex? Are we only modulating the associative and affective functions related to pain perception? Do these areas of the CNS show a dose-dependant sensitivity to anesthetics?

 

To try answering those questions, we have conducted a study on the influence of the level of propofol sedation on vibro-tactile stimulation. Volunteers were submitted to increasing target concentrations of propofol and presented with standardized vibratory stimuli. We found a significant decrease in activation of the primary sensory cortex at very low sedative doses of propofol (0.5 mg·ml-1). A more profound effect is seen at higher levels of sedation, with an almost complete abolition of activation at in the thalamus when pharmacological unconsciousness is reached. This suggests that even when a patient in only mildly sedated, a rather significant effect on cortical activation might explain a relative indifference to external tactile stimuli 8. 

           

PET allows us to explore another aspect of propofol action related to neurotransmission. There are reports in the literature of reversal of anesthetic effects with physostigmine, an anticholinesterase drug that crosses the blood-brain barrier. In fact Antilirium® has been used for years to “speed up awakening”. It is also common knowledge that scopolamine, an antimuscarinic drug also crossing the blood-brain barrier induces sedation and potentiates anesthetic effect. These facts, coupled with the extensive knowledge on the modulatory effect of the central cholinergic system on sleep-wake states, suggest that the central muscarinic system has a role to play in the generation of anesthetic effect 9. We have used 11C-Benztropine, a non-specific M1 and M2 antagonist, to study muscarinic receptor occupancy during propofol-induced unconsciousness. Preliminary results show an increase in benztropine binding (reflecting a decrease in acetyl choline binding) under anesthesia in areas rich in M1 receptors. 

 

   

Conclusion:

 

Brain imaging is a window on the working brain. It offers tremendous possibilities for understanding the neural processes involved in all aspects of consciousness. Data from research in this field in the past 5 years suggest that anesthetics are not simply general depressant of brain activity, but rather act on specific structures of the CNS in a dose-dependant fashion.

 

 

 

 

 

 

 

 

 

 

 

 

Reference List

 

   1.   Saha GB, MacIntyre WJ, Go RT: Radiopharmaceuticals for brain imaging.  Seminars in Nuclear Medicine 24:324-349, 1994

   2.   Posner MI, Petersen SE, Fox PT, Raichle ME: Localization of cognitive operations in the human brain.  Science 240:1627-1631, 1988

   3.   Alkire MT, Haier RJ, Barker SJ, Shah NK, Wu JC, Kao J: Cerebral metabolism during propofol anesthesia in humans studied with positron emission tomography.  Anesthesiology 82:393-403, 1995

   4.   Fiset P, Paus T, Daloze T, Plourde G, Meuret P, Bonhomme V, Hajj-Ali N, Backman SB, Evans AC: Brain mechanisms of propofol-induced loss of consciousness in humans: a Positron Emission Tomography study.  Journal of neuroscience 19:5506-5513, 1999

   5.   Alkire MT, Haier RJ, Fallon JH: Toward a unified theory of narcosis: brain imaging evidence for a thalamocortical switch as the neurrophysiologic basis of anesthetic-induced unconsciousness.  Consciousness and Cognition 9:370-386, 2000

   6.   Coghill RC, Talbot JD, Evans AC, Meyer E, Gjedde A, Bushnell MC, Duncan GH: Distributed processing of pain and vibration by the human brain.  Journal of neuroscience 14:4095-4108, 1994

   7.   Talbot JD, Marret S, Evans AC, Meyer E, Bushnell MC, Duncan GH: Multiple representations of pain in human cerebral cortex.  Science 251:1355-1357, 1991

   8.   Bonhomme V, Fiset P, Meuret P, Backman SB, Plourde G, Paus T, Bushnell C, Evans A: Effect of propofol-induced general anesthesia on changes in regional cerebral blood flow elicited by vibrotactile stimulation: a positron emission tomography (PET) study.  Journal of Neurophysiology Accepted:2000

   9.   Meuret P, Backman SB, Bonhomme V, Plourde G, Fiset P: Physostigmine reverses propofol-induced unconsciousness and attenuation of the auditory steady state response and bispectral index in human volunteers.  Anesthesiology 93:708-717, 2000

 



[a] M.T Alkire, Proceedings of the 9th Annual SIVA meeting, October 13th, San Francisco, CA, USA