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General anesthetics-Medicinal Chemistry

General anesthetics are CNS depressant drugs that induce the absence of sensation and loss of pain. They can be classified into inhalation and non-inhalation categories, with various agents such as halothane, methohexital, and ketamine, each having specific mechanisms of action and clinical applications. The document also outlines the mechanisms of action, uses, and therapeutic properties of various anesthetics.

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Mechanism of Action•Medicinal Chemistry•
General anesthetics Dr. Gopal Krishna Padhyp y 16-04-2020
DefinitionDefinition General anesthetics are CNS depressant drugs that inducep g absence of perception of all sensations and loss of pain. They depress the CNS non selectively but reversibly.y p y y 16-04-2020
Classification DefinitionInhalation anesthetics Halogenated Halothane Enflurane Isoflurane M h fl D fl S flMethoxyflurane Desflurane Sevoflurane 16-04-2020
Non-Halogenatedg Cyclopropane DiethyletherCyclopropane Diethylether N ON2O Nitrous oxide 16-04-2020
Non-Inhalation anesthetics Barbituric acid derivatives 2 5 2 3 23 3 Thiopental Sodium Methohexital Sodium 22 2 3 23 Thiamylal sodium 16-04-2020
Miscellaneous Ketamine Hydrochloride 16-04-2020
Halothane MOA: Halothane causes anesthesia due to its actions on multiple ion channels, which ultimately depresses nerve conduction, breathing, cardiac contractility. Its effects haveg y been attributed to its binding to potassium channels in cholinergic neurons. Halothane's effect are also likely due tog y binding to NMDA receptor and calcium channels, causing hyperpolarization.yp p Uses: Halothane is a modern and widely used inhalation anesthetic. It is used in both short and long-lasting surgical operations. It acts very quickly, which is pleasing to patients, and it is very safe. 16-04-2020
Methohexital Sodium 16-04-2020
Mechanism of action of methohexital It is believed that methohexital decreases the electrical Mechanism of action of methohexital It is believed that methohexital decreases the electrical nerve activity in the CNS that leads to general anesthetic actionaction. Methoxehital binds to GABA-BZD receptors-Chloride ion channel complex This binding increases affinity of GABAchannel complex. This binding increases affinity of GABA for the GABAA receptor. It leads to increase in chloride ion conduction via anIt leads to increase in chloride ion conduction via an increase in the frequency of the chloride channel opening. At higher dose it directly increase conductance of Cl- ion andhigher dose, it directly increase conductance of Cl ion and inhibit calcium dependant release of neurotransmitter. 16-04-2020
I ddi i b i l d l i d dIn addition to above it also depress glutamate induced neuronal depolarization through AMPA receptor. At very high d b bi d N + d K+ i h l ldose barbiturates depress Na+ and K+ ion channels also. Uses: I i i il d i d h i I i l d iIt is primarily used to induce anesthesia. It is only used in hospital under strict supervision. It has been used to induce d d ti f d d t l ddeep sedation for surgery and dental procedure. 16-04-2020
Ketamine Hydrochloride 16-04-2020
Reaction mechanism for step-5 16-04-2020
Ketamine show multiple therapeutic properties like Mechanism of Action Ketamine show multiple therapeutic properties like analgesic, anesthetic and sympathomimetic effects by acting on different sites.on different sites. N-methyl-D-aspartate (NMDA)-receptor antagonism is the most important neuropharmacological mechanism for themost important neuropharmacological mechanism for the analgesic effects of ketamine. Effects on opiate receptors may contribute to the analgesicects o op ate ecepto s ay co t ute to t e a a ges c proporties as well as to dysphoric reactions.  Sympathomimetic properties are mediated by enhancedy p p p y central and peripheral monoaminergic transmission. 16-04-2020
Inhibition of central and peripheral cholinergic transmission may contribute to the induction of anaesthetic state andy hallucinations. Uses: Ketamine is a specific drug for non-inhalation anesthesia. It is used in brief surgical procedures. It is indicated as the soleg p anesthetic agent for diagnostic and surgical procedures. 16-04-2020
Enflurane Isoflurane MOA: Enflurane acts as a positive allosteric modulator ofp the GABAA receptor. It also inhibits receptor activity in they NMDA glutamate receptor subtypes. These yield a decreased MOA: Similar to enflurane. Uses: Used for the depolarization and therefore, tissue excitability which results induction and maintenance of general anaesthesia in anesthesia. Uses: Used for the induction during surgery and cesarean section and also used for and maintenance of general anaesthesia during surgery and as analgesia during child delivery. analgesia during child delivery. 16-04-2020
Methoxyflurane Desflurane MOA: Similar to enflurane. MOA: Similar to enflurane. Uses: Used for the induction and maintenance of general Uses: Used for the induction and maintenance of generalg anaesthesia during surgery and for analgesia during child g anaesthesia during surgery and cesarean section and alsog g delivery. used for analgesia during child delivery.y 16-04-2020
Sevoflurane Thiopental Sodium NC2H5 O SNa NH CH O CH2 CH3 CH2H3C lMOA: Similar to enflurane. Uses: Used for the induction MOA: Similar to methohexital sodium. h land maintenance of general anesthesia during surgery Uses: Thiopental is an extremely short acting b b h k g g y and also as analgesia during child delivery. barbiturate that makes anesthesia pleasant and h f h y smooth for the patient. It has been used to induce d d fdeep sedation for surgery and dental procedure.16-04-2020
Thiamylal sodium CH O CHH C NH NCH2 CH SNa CH2 CHH2C CH2CH3 MOA: Similar to CH O CH2 CH3 CH2CH3 methohexital sodium. Uses: It has sedative, hypnotic and anticonvulsant properties and is used as a short acting sedative. It is used primarily for induction of surgical hanesthesia or as an anticonvulsant to counteract d ff f hside effects from other anesthetics. 16-04-2020
BOOKS FOR FURTHER READING Wil d Gi ld T b k f i M di i l BOOKS FOR FURTHER READING Wilson and Gisvold,Text book of organic, Medicinal and Pharmaceutical Chemistry. Foyes Principles of medicinal chemistry byWilliams O. Foye.y AText book of medicinal chemistry (Synthetic and Biochemical Approach) vol I& II by SN PandeyaBiochemical Approach) vol. I& II by SN Pandeya. Synthesis of Essential Drugs by R.S.Vardanyan and VJ H bV.J. Hruby 16-04-2020