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General anesthesia likely involves inhibition of the opening of the ion channel in a

postsynaptic ligand-gated membrane protein. Calculations yield qualitative


agreement with anesthetic potency at clinical anesthetic membrane concentrations
and predict the alkanol cutoff and anomalously low potencies of strongly hydrophobic
molecules with little or no attraction for the aqueous interface, such as
perfluorocarbons.

It was shown that anaesthetics alter the functions of many cytoplasmic


signalling proteins, including protein kinase C. They bind directly only
to small number of targets in CNS mostly ligand (neurotransmitter)gated ion channels in synapse and G-protein coupled receptors altering
their ion flux.

Sevoflurane, isoflurane, propofol. Immobility and cerebral effects


reflect different entities of anaesthetic action. MAC (Minimum Alveolar
Concentration of inhaled anaesthetic) concentration of the vapor in the
lungs that is needed to prevent movement (motor response) due to
surgical stimulus, used to compare strengths or potency of anaesthetic
vapor. Although MAC may not have revealed information on the
cerebral sites of anesthetic action and anesthetic actions on sensory
processing, one of the great benefits of the MAC studies was to define
a set of drug concentrations that are appropriate to induce anesthesia.
CP50i = minimum plasma concentration of intravenous anaesthetic
(non-opioid)

Etomidate, midazolam, propofol (lipofilik), thiopental. Enhancing the


activity of inhibitory neurotransmitter y-aminobutyric acid (GABA) in
the central neuron system. Ketamine, nitrous oxide and xenon inhibit
ionotropic glutamate receptors, with the strongest effects being seen
on the NMDA receptor subtype. Ketamine antagonizes the effect of the
excitatory neurotransmitter N-methyl-D-aspartate (NMDA) on its
receptors. Opioid agonists stimulate opioid receptors. General
anesthetics also have a spectrum of modest to strong effects on other
ion channels, including glycine receptors, neuronal nicotinic receptors,
5-HT3 receptors, glutamate receptors and the two pore potassium
channels. These drugs have rapid action and quickly cleared from the
bloodstream and CNS, facilitating control of anaesthetic state (tirtration
effect). It also protects vital tissue, memiliki efek yg lebih ringan, tidak
mempengaruhi sistem peredaran darah atau mengakibatkan efek
samping lainnya. Bereaksi di otak, berjalan dari tempat injeksi, kurang
lebih 1 menit. Tidak larut dalam darah dan langsung dibersihkan di hati

The transmitter-gated ion channel (TGIC) superfamily and includes gaminobutyric acid type A (GABAA), strychnine-sensitive glycine,
neuronal nicotinic acetylcholine (nAch) and 5-hydroxytryptamine (5HT3) receptors. Activation of GABAA receptors induces inward
movement of mainly chloride ions down their electrochemical gradient
resulting in a hyperpolarization of the cell membrane, whereas
activation of nicotinic receptors produces a net inward movement of
sodium ions and depolarization of the cell membrane. Therefore,
augmenting an inhibitory signal, or inhibiting an excitatory signal,
provides a logical mechanism for general anaesthetic action

Useful effects of general anaesthetic include unconsciousness,


analgesia, suppression of autonomic reflexes (increasing blood
pressure, and heart rate), and muscle relaxation. Movement reflects a
shallow depth of anesthesia and can interfere surgery.

General anestesi adalah proses mendapatkan suatu keadaan otak yang


tidak sadar. Namun jika hanya tidak sadar, surgical stimulus yang
didapatkan pasien dapat mengakibatkan awakening. Untuk mencegah
awakening maka stimulus tersebut di inhibisi agar tidak sampai ke
otak. Hal ini dilakukan dengan menghambat kerja reseptor opioid di
saraf perifer.

At the cellular level, anesthetics alter the behavior of neurons, by


interacting directly with a small number of ion channels. Under normal
conditions, these specialized membrane proteins are activated by
chemical signals or changes in the membrane environment. Upon
activation, channels change the electrical excitability of neurons by
controlling the flow of depolarizing (excitatory) or hyperpolarizing
(inhibitory) ions across the cell membrane via an ion channel that is
integral with the receptor that senses the initial signal. General
anesthetics primarily act by either enhancing inhibitory signals or by
blocking excitatory signals.

Analgesic fentanyl, sufentanil, alfentanil, remifentanil. Hypnotic


isoflurane, desflurane,sevoflurane, propofol. Inhibit kerja enzim, inhibit
ion channel, inhibit pelepasan neurotransmitter, dan inhibit protein
reseptor di terminal post sinaps

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