General anesthetics are drugs used during surgery to induce unconsciousness, analgesia, and muscle relaxation. They work by blocking NMDA receptors or enhancing GABA receptors in the central nervous system. There are two main types - general anesthetics that are gases administered by inhalation (nitrous oxide, xenon), and volatile liquids administered by inhalation (halothane, isoflurane, desflurane, sevoflurane). These drugs work by passing through four stages - analgesia, loss of consciousness, surgical anesthesia with loss of reflexes, and a dangerous stage of respiratory depression. The ideal general anesthetic is potent, inexpensive, minimally soluble in tissues, stable, and lacks side effects like cardiotoxicity.
This document provides information about sympathomimetic agents. It discusses direct-acting, indirect-acting, and mixed-acting agents and how they work. Specific agents are described, including their properties, mechanisms of action, uses, and storage requirements. Sympathomimetic drugs act on adrenergic receptors to increase heart rate and blood pressure. Structure-activity relationships are also covered, explaining how chemical modifications impact receptor selectivity and duration of action.
The document discusses various classes of sedative and hypnotic drugs including benzodiazepines, barbiturates, and miscellaneous agents. It covers their structures, mechanisms of action, uses, and metabolism. Some key points discussed include how benzodiazepines act on GABA receptors to inhibit neuronal activity, the classification of barbiturates based on duration of action, and factors affecting the potency of barbiturates like acidity, lipid solubility, and structural properties.
Anticholinergics are drugs that inhibit the pharmacological response of acetylcholine (Ach) by competitively binding to and blocking muscarinic receptors. Their general structure consists of two carbocyclic or heterocyclic rings (R1 and R2) connected by a chain with an ester or ether group (X) and a basic nitrogen substituent. The R3 group can be hydrogen, hydroxyl, or hydroxymethyl. Maximum potency is seen with 2 carbon units between the ring and nitrogen. Older anticholinergics like atropine and scopolamine are non-selective for muscarinic receptor subtypes, while newer drugs show selectivity. Anticholinergics are used to treat
This document discusses adrenergic blockers, which block the effects of sympathomimetic drugs. It describes alpha-adrenergic blockers and beta-adrenergic blockers. Alpha blockers are classified as non-selective, alpha-1 selective, alpha-2 selective, and ergot alkaloids. They work by competitively inhibiting catecholamines at alpha receptors. Beta blockers are classified as beta-1 selective, beta-2 selective, and non-selective. They competitively inhibit catecholamine effects at beta receptors and are used to treat hypertension, heart disease, and arrhythmias. The document provides examples of specific drugs for each class and discusses their mechanisms and uses.
Adrenergic drugs have many uses. They are used to increase the output of the heart, to raise blood pressure, and to increase urine flow as part of the treatment of shock. Adrenergics are also used as heart stimulants.
it's our aim to provide notes for pharmacy student without any charge.so that we make pharmacy education easier.
किसी भी शुल्क के बिना फार्मेसी छात्र के लिए नोट्स प्रदान करना हमारा लक्ष्य है।ताकि हम फार्मेसी शिक्षा को आसान बना दें।
This ppt covers the classification, structures and IUPAC names, Mechanism of action and uses of individual drugs...under anticonvulsants topic..Side effects/metabolism are also given for few
This document provides information about sympathomimetic agents. It discusses direct-acting, indirect-acting, and mixed-acting agents and how they work. Specific agents are described, including their properties, mechanisms of action, uses, and storage requirements. Sympathomimetic drugs act on adrenergic receptors to increase heart rate and blood pressure. Structure-activity relationships are also covered, explaining how chemical modifications impact receptor selectivity and duration of action.
The document discusses various classes of sedative and hypnotic drugs including benzodiazepines, barbiturates, and miscellaneous agents. It covers their structures, mechanisms of action, uses, and metabolism. Some key points discussed include how benzodiazepines act on GABA receptors to inhibit neuronal activity, the classification of barbiturates based on duration of action, and factors affecting the potency of barbiturates like acidity, lipid solubility, and structural properties.
Anticholinergics are drugs that inhibit the pharmacological response of acetylcholine (Ach) by competitively binding to and blocking muscarinic receptors. Their general structure consists of two carbocyclic or heterocyclic rings (R1 and R2) connected by a chain with an ester or ether group (X) and a basic nitrogen substituent. The R3 group can be hydrogen, hydroxyl, or hydroxymethyl. Maximum potency is seen with 2 carbon units between the ring and nitrogen. Older anticholinergics like atropine and scopolamine are non-selective for muscarinic receptor subtypes, while newer drugs show selectivity. Anticholinergics are used to treat
This document discusses adrenergic blockers, which block the effects of sympathomimetic drugs. It describes alpha-adrenergic blockers and beta-adrenergic blockers. Alpha blockers are classified as non-selective, alpha-1 selective, alpha-2 selective, and ergot alkaloids. They work by competitively inhibiting catecholamines at alpha receptors. Beta blockers are classified as beta-1 selective, beta-2 selective, and non-selective. They competitively inhibit catecholamine effects at beta receptors and are used to treat hypertension, heart disease, and arrhythmias. The document provides examples of specific drugs for each class and discusses their mechanisms and uses.
Adrenergic drugs have many uses. They are used to increase the output of the heart, to raise blood pressure, and to increase urine flow as part of the treatment of shock. Adrenergics are also used as heart stimulants.
it's our aim to provide notes for pharmacy student without any charge.so that we make pharmacy education easier.
किसी भी शुल्क के बिना फार्मेसी छात्र के लिए नोट्स प्रदान करना हमारा लक्ष्य है।ताकि हम फार्मेसी शिक्षा को आसान बना दें।
This ppt covers the classification, structures and IUPAC names, Mechanism of action and uses of individual drugs...under anticonvulsants topic..Side effects/metabolism are also given for few
It contains classification, SAR, MOA, metabolism and usd of hypnotics and sedatives. Barbiturates and benzodiazepines were discussed as per PCI syllabus. This helps B.Pharm students to learn with focus
This document discusses adrenergic antagonists, which are drugs that block adrenergic receptors to inhibit the functions of epinephrine, norepinephrine, and dopamine. It classifies them as alpha or beta blockers and provides examples of each. Key drugs discussed include tolazoline, phentolamine, phenoxybenzamine, prazosin, dihydroergotamine, methysergide, propranolol, metoprolol, atenolol, betaxolol, esmolol, metaprolol, and carvedilol. Their structures, mechanisms of action, and clinical uses for conditions like hypertension and cardiac issues are summarized. The synthesis of tolazoline and
Narcotic and Nonnarcotic analgesic(Medicinal Chemistry)Yogesh Tiwari
Analgesics are agents that relieve pain by acting centrally to elevate pain threshold without disturbing consciousness or altering other sensory modalities.
This document discusses antipsychotic agents used to treat schizophrenia. It begins with an introduction that explains the positive and negative symptoms of schizophrenia and how antipsychotics work by decreasing dopaminergic neurotransmission. The document then covers the classification of typical and atypical antipsychotics, including examples from different drug classes. It discusses the mechanism of action of phenothiazine derivatives and provides structure-activity relationships. Specific phenothiazine derivatives are highlighted, including chlorpromazine. The document also briefly discusses thioxanthene derivatives as bioisosteres of phenothiazines. In summary, the document provides an overview of antipsychotic agents used to treat schizophrenia, focusing on phenothiazine derivatives and structure-activity relationships
General Anaesthesia (Medicinal Chemistry)Yogesh Tiwari
General anaesthetics are group of drugs that produces loss of consciousness, and therefore, loss of all sensations.
The absolute loss of sensation is termed as anaesthesia.
1. The document discusses narcotic analgesics and narcotic antagonists, including their mechanisms of action, examples, and uses.
2. It describes the three main opioid receptors and their roles in pain management. Morphine and its analogues are discussed in terms of important structural features that determine their activity.
3. Individual narcotic analgesics like morphine sulfate, codeine, meperidine hydrochloride, and narcotic antagonists such as nalorphine hydrochloride are explained in terms of their therapeutic uses.
Psychosis is a severe mental disorder characterized by a loss of contact with reality through disturbed perceptions, thoughts, emotions and behavior. Common symptoms include delusions, hallucinations, incoherent speech and inappropriate behavior. The document discusses various types of psychosis and drugs used to treat psychotic illnesses. Antipsychotics like chlorpromazine, haloperidol and sulpiride work by blocking dopamine receptors in the brain to reduce psychotic symptoms. The mechanisms of action and uses of different classes of antipsychotics including phenothiazines, butyrophenones, and benzamides are described.
Medicinal Chemistry of Antihypertensive agents pptxSameena Ramzan
This document provides an overview of antihypertensive agents. It begins with an introduction to hypertension and classifications of hypertension. It then discusses the pharmacological classifications of antihypertensive drugs and provides details on the synthesis, mechanisms of action, adverse effects and dosage of various classes of antihypertensive agents including diuretics, ACE inhibitors, calcium channel blockers, beta-blockers, central sympatholytics, and arterial dilators. It also discusses structure-activity relationships of ACE inhibitors and ARBs. The document aims to inform healthcare professionals about the different types of antihypertensive drugs.
Sedative and hypnotic Drugs/ Medicinal Chemistry III (Part One)NarminHamaaminHussen
Sedative and hypnotic drugs act on the central nervous system by depressing activity. Sedatives decrease excitement without causing drowsiness, while hypnotics produce sleep. The same drugs can act as sedatives at low doses and hypnotics at higher doses in a dose-dependent manner. Most sedatives and hypnotics work by enhancing the effects of the inhibitory neurotransmitter GABA at GABAA receptors. Benzodiazepines are a commonly used class of sedative and hypnotic drugs that work through this GABAergic mechanism of action. Their effects and pharmacokinetic properties depend on their chemical structure and metabolism.
The document discusses neurohumoral transmission and the roles of various neurotransmitters including GABA, glutamate, glycine, serotonin, and dopamine. It explains how each neurotransmitter binds to receptors on target cells and triggers electrical or chemical responses that influence processes like muscle movement, mood, learning, and reward pathways. Abnormalities in the function of these neurotransmitters have also been linked to neurological and psychiatric disorders.
General anesthetic and pre anestheticsGourav Singh
The document discusses different aspects of anesthesia including:
1. Anesthesia refers to reversible loss of sensation and consciousness and is achieved through anesthetic agents that induce loss of pain and sensation along with loss of reflexes.
2. There are two main types of anesthesia - local anesthesia and general anesthesia. General anesthesia involves drug-induced absence of all sensation allowing surgery.
3. Anesthesia works through several stages from initial analgesia to eventual respiratory paralysis if overdosed. Proper pre-anesthesia medications are used to make the anesthesia safer and more comfortable for the patient.
Part II: UNIT cholinergic neurotransmitter - Antagonist DrugsSONALI PAWAR
This document discusses cholinergic neurotransmitters and cholinergic blocking agents. It begins by describing various cholinergic blocking agents including solanaceous alkaloids like atropine, scopolamine, and hyoscyamine as well as synthetic agents like tropicamide, cyclopentolate, dicyclomine, glycopyrrolate, and propantheline. It then discusses the mechanisms of action and medical uses of these drugs, which work by antagonizing acetylcholine at nicotinic or muscarinic receptors. The document also covers structural activity relationships of parasympatholytic agents and their use in treating conditions like smooth muscle spasms, ulcers, overactive bladder, and Parkinson
Biosynthesis and catabolism of acetylcholine by Dheeraj gargDheeraj Aggarwal
Acetylcholine (ACh) is an organic chemical that functions in the brain and body of many types of animals (and humans) as a neurotransmitter—a chemical message released by nerve cells to send signals to other cells, such as neurons, muscle cells and gland cells.
This is the presentation for B. Pharm. IV Semester Students. It includes details like introduction, mechanism of action, classification along with structures and nomenclature, synthesis, uses and adverse effects of General Anaesthetics.
This ppt covers the classification of anti psychotics with structures and IUPAC names, MOA, uses, metabolism and side effects. Dopaminergic pathways also given
This document discusses cholinergic agents, which are drugs that produce effects similar to acetylcholine by directly interacting with cholinergic receptors or increasing acetylcholine availability. It classifies cholinergic agonists and anticholinesterases. Cholinergic agonists include acetylcholine and analogs like methacholine and carbachol. Anticholinesterases reversibly or irreversibly inhibit the enzyme acetylcholinesterase, leading to acetylcholine accumulation. Common anticholinesterases discussed are physostigmine, neostigmine, pyridostigmine, and organophosphates. The document provides examples of clinical uses and synthesis for several cholinergic agents.
1) Barbiturates are derivatives of barbituric acid formed by the reaction of malonic acid with urea. Barbituric acid was first synthesized in 1864.
2) Barbiturates are classified based on their duration of action - long acting (>6 hrs), intermediate acting (3-6 hrs), short acting (<3 hrs), and ultra short acting. Their chemical structures determine duration of action.
3) Extensive testing of barbiturate structures has defined structure-activity relationships. Substitutions that increase lipid solubility, like lower alkyl groups at position 5 and N-methylation at position 3, decrease duration of action by enhancing brain penetration and liver metabolism. Replacing the
General Anesthetics Pdf Medicinal Chemistrycrazyknocker40
General anesthetics work by depressing the central nervous system through various mechanisms of action. They are classified as inhalation anesthetics like sevoflurane, desflurane, and nitrous oxide or intravenous anesthetics like propofol and barbiturates. Inhalation anesthetics produce anesthesia through blocking NMDA receptors, activating GABA receptors, and other targets. Intravenous anesthetics rapidly induce unconsciousness but require other anesthetics for maintenance due to their short duration of action. Common inhalation anesthetics include sevoflurane, desflurane, isoflurane and nitrous oxide while intravenous options are propofol, thiopental, and methohexital. Ketamine is a dissociative anesthetic that blocks NMDA receptors to produce
This document provides an overview of inhalational anesthetic agents. It begins with a brief history of inhaled anesthesia and then outlines the ideal properties of anesthetic agents. The stages of anesthesia are described based on Guedel's criteria. Common inhaled agents like ether, nitrous oxide, and halothane are then discussed in more detail, covering their physical and pharmacologic properties as well as potential toxicities.
It contains classification, SAR, MOA, metabolism and usd of hypnotics and sedatives. Barbiturates and benzodiazepines were discussed as per PCI syllabus. This helps B.Pharm students to learn with focus
This document discusses adrenergic antagonists, which are drugs that block adrenergic receptors to inhibit the functions of epinephrine, norepinephrine, and dopamine. It classifies them as alpha or beta blockers and provides examples of each. Key drugs discussed include tolazoline, phentolamine, phenoxybenzamine, prazosin, dihydroergotamine, methysergide, propranolol, metoprolol, atenolol, betaxolol, esmolol, metaprolol, and carvedilol. Their structures, mechanisms of action, and clinical uses for conditions like hypertension and cardiac issues are summarized. The synthesis of tolazoline and
Narcotic and Nonnarcotic analgesic(Medicinal Chemistry)Yogesh Tiwari
Analgesics are agents that relieve pain by acting centrally to elevate pain threshold without disturbing consciousness or altering other sensory modalities.
This document discusses antipsychotic agents used to treat schizophrenia. It begins with an introduction that explains the positive and negative symptoms of schizophrenia and how antipsychotics work by decreasing dopaminergic neurotransmission. The document then covers the classification of typical and atypical antipsychotics, including examples from different drug classes. It discusses the mechanism of action of phenothiazine derivatives and provides structure-activity relationships. Specific phenothiazine derivatives are highlighted, including chlorpromazine. The document also briefly discusses thioxanthene derivatives as bioisosteres of phenothiazines. In summary, the document provides an overview of antipsychotic agents used to treat schizophrenia, focusing on phenothiazine derivatives and structure-activity relationships
General Anaesthesia (Medicinal Chemistry)Yogesh Tiwari
General anaesthetics are group of drugs that produces loss of consciousness, and therefore, loss of all sensations.
The absolute loss of sensation is termed as anaesthesia.
1. The document discusses narcotic analgesics and narcotic antagonists, including their mechanisms of action, examples, and uses.
2. It describes the three main opioid receptors and their roles in pain management. Morphine and its analogues are discussed in terms of important structural features that determine their activity.
3. Individual narcotic analgesics like morphine sulfate, codeine, meperidine hydrochloride, and narcotic antagonists such as nalorphine hydrochloride are explained in terms of their therapeutic uses.
Psychosis is a severe mental disorder characterized by a loss of contact with reality through disturbed perceptions, thoughts, emotions and behavior. Common symptoms include delusions, hallucinations, incoherent speech and inappropriate behavior. The document discusses various types of psychosis and drugs used to treat psychotic illnesses. Antipsychotics like chlorpromazine, haloperidol and sulpiride work by blocking dopamine receptors in the brain to reduce psychotic symptoms. The mechanisms of action and uses of different classes of antipsychotics including phenothiazines, butyrophenones, and benzamides are described.
Medicinal Chemistry of Antihypertensive agents pptxSameena Ramzan
This document provides an overview of antihypertensive agents. It begins with an introduction to hypertension and classifications of hypertension. It then discusses the pharmacological classifications of antihypertensive drugs and provides details on the synthesis, mechanisms of action, adverse effects and dosage of various classes of antihypertensive agents including diuretics, ACE inhibitors, calcium channel blockers, beta-blockers, central sympatholytics, and arterial dilators. It also discusses structure-activity relationships of ACE inhibitors and ARBs. The document aims to inform healthcare professionals about the different types of antihypertensive drugs.
Sedative and hypnotic Drugs/ Medicinal Chemistry III (Part One)NarminHamaaminHussen
Sedative and hypnotic drugs act on the central nervous system by depressing activity. Sedatives decrease excitement without causing drowsiness, while hypnotics produce sleep. The same drugs can act as sedatives at low doses and hypnotics at higher doses in a dose-dependent manner. Most sedatives and hypnotics work by enhancing the effects of the inhibitory neurotransmitter GABA at GABAA receptors. Benzodiazepines are a commonly used class of sedative and hypnotic drugs that work through this GABAergic mechanism of action. Their effects and pharmacokinetic properties depend on their chemical structure and metabolism.
The document discusses neurohumoral transmission and the roles of various neurotransmitters including GABA, glutamate, glycine, serotonin, and dopamine. It explains how each neurotransmitter binds to receptors on target cells and triggers electrical or chemical responses that influence processes like muscle movement, mood, learning, and reward pathways. Abnormalities in the function of these neurotransmitters have also been linked to neurological and psychiatric disorders.
General anesthetic and pre anestheticsGourav Singh
The document discusses different aspects of anesthesia including:
1. Anesthesia refers to reversible loss of sensation and consciousness and is achieved through anesthetic agents that induce loss of pain and sensation along with loss of reflexes.
2. There are two main types of anesthesia - local anesthesia and general anesthesia. General anesthesia involves drug-induced absence of all sensation allowing surgery.
3. Anesthesia works through several stages from initial analgesia to eventual respiratory paralysis if overdosed. Proper pre-anesthesia medications are used to make the anesthesia safer and more comfortable for the patient.
Part II: UNIT cholinergic neurotransmitter - Antagonist DrugsSONALI PAWAR
This document discusses cholinergic neurotransmitters and cholinergic blocking agents. It begins by describing various cholinergic blocking agents including solanaceous alkaloids like atropine, scopolamine, and hyoscyamine as well as synthetic agents like tropicamide, cyclopentolate, dicyclomine, glycopyrrolate, and propantheline. It then discusses the mechanisms of action and medical uses of these drugs, which work by antagonizing acetylcholine at nicotinic or muscarinic receptors. The document also covers structural activity relationships of parasympatholytic agents and their use in treating conditions like smooth muscle spasms, ulcers, overactive bladder, and Parkinson
Biosynthesis and catabolism of acetylcholine by Dheeraj gargDheeraj Aggarwal
Acetylcholine (ACh) is an organic chemical that functions in the brain and body of many types of animals (and humans) as a neurotransmitter—a chemical message released by nerve cells to send signals to other cells, such as neurons, muscle cells and gland cells.
This is the presentation for B. Pharm. IV Semester Students. It includes details like introduction, mechanism of action, classification along with structures and nomenclature, synthesis, uses and adverse effects of General Anaesthetics.
This ppt covers the classification of anti psychotics with structures and IUPAC names, MOA, uses, metabolism and side effects. Dopaminergic pathways also given
This document discusses cholinergic agents, which are drugs that produce effects similar to acetylcholine by directly interacting with cholinergic receptors or increasing acetylcholine availability. It classifies cholinergic agonists and anticholinesterases. Cholinergic agonists include acetylcholine and analogs like methacholine and carbachol. Anticholinesterases reversibly or irreversibly inhibit the enzyme acetylcholinesterase, leading to acetylcholine accumulation. Common anticholinesterases discussed are physostigmine, neostigmine, pyridostigmine, and organophosphates. The document provides examples of clinical uses and synthesis for several cholinergic agents.
1) Barbiturates are derivatives of barbituric acid formed by the reaction of malonic acid with urea. Barbituric acid was first synthesized in 1864.
2) Barbiturates are classified based on their duration of action - long acting (>6 hrs), intermediate acting (3-6 hrs), short acting (<3 hrs), and ultra short acting. Their chemical structures determine duration of action.
3) Extensive testing of barbiturate structures has defined structure-activity relationships. Substitutions that increase lipid solubility, like lower alkyl groups at position 5 and N-methylation at position 3, decrease duration of action by enhancing brain penetration and liver metabolism. Replacing the
General Anesthetics Pdf Medicinal Chemistrycrazyknocker40
General anesthetics work by depressing the central nervous system through various mechanisms of action. They are classified as inhalation anesthetics like sevoflurane, desflurane, and nitrous oxide or intravenous anesthetics like propofol and barbiturates. Inhalation anesthetics produce anesthesia through blocking NMDA receptors, activating GABA receptors, and other targets. Intravenous anesthetics rapidly induce unconsciousness but require other anesthetics for maintenance due to their short duration of action. Common inhalation anesthetics include sevoflurane, desflurane, isoflurane and nitrous oxide while intravenous options are propofol, thiopental, and methohexital. Ketamine is a dissociative anesthetic that blocks NMDA receptors to produce
This document provides an overview of inhalational anesthetic agents. It begins with a brief history of inhaled anesthesia and then outlines the ideal properties of anesthetic agents. The stages of anesthesia are described based on Guedel's criteria. Common inhaled agents like ether, nitrous oxide, and halothane are then discussed in more detail, covering their physical and pharmacologic properties as well as potential toxicities.
This document discusses general anesthetics, including their stages of anesthesia, characteristics of an ideal anesthetic, mechanisms of action, classifications, and specific anesthetics like halothane, barbiturates, ketamine, cyclopropane, ethyl chloride, and nitrous oxide. It describes the four stages of general anesthesia from analgesia to medullary depression. An ideal anesthetic should be potent, non-irritating, produce smooth anesthesia with muscle relaxation but no side effects. Mechanisms of action include lipid and protein theories. Anesthetics are classified as volatile or non-volatile, with examples like halothane, thiopental, ketamine, cyclopropane, ethyl chloride and nitrous oxide discussed
General anaesthetics (GAs) are drugs which produce reversible loss of all sensation and consciousness.
The cardinal features of general anaesthesia are:
• Loss of all sensation, especially pain.
• Sleep (unconsciousness) and amnesia
• Immobility and muscle relaxation
• Abolition of somatic and autonomic reflexes.
GA was absent until the mid 1800’s
Original discoverer of GA
-Crawford long, physician from Gerogia(1842),
ETHER ANESTHESIA
. NITROUS OXIDE
- Horace wells(1844)
. GASEOUS ETHER by William T.G. Morton(1846)
. CHLOROFORM introduced by
- James simpson (1847)
METHODS OF ADMINISTRATION OF INHALATIONAL GENERAL ANAESTHETICS
OPEN METHOD: This is a simple method of administering a volatile anaesthetic.
A simple mask covered with six to ten layers of gauze, which does not fit the contour of the face is held on the face and an anaesthetic like ether, or ethyl chloride is poured on it in drops. The anaesthetic vapour, diluted with air, is inhaled through the gap between the mask and the face.
SEMI-OPEN METHOD: This method is similar to open method but the dilution with air is prevented by using either a well-fitting mask like Ogston’s mask or layers of gauze between face and the mask. A small carbon dioxide build-up occurs with this method.
SEMI-CLOSED METHOD: This method allows some rebreathing of the anaesthetic drug with the help of a reservoir but in addition, part of the volume of each succeeding inspiration is a new portion from an anaesthetic mixture. This method involves accumulation and rebreathing of carbon dioxide.
• CLOSED METHOD: This method employs the chemical agent soda lime to absorb the carbon dioxide present in the expired air. It requires the use of a special apparatus but is particularly useful when the anaesthetic agent is potentially explosive
STAGES OF ANAESTHESIA
Guedel, in 1920 outlined the four stages of general anaesthesia :
• Stage I: Stage of analgesia
• Stage II: Stage of delirium
• Stage III: Stage of surgical anaesthesia
• Stage IV: Stage of respiratory paralysis
Inadequate anaesthesia is indicated by:
Signs of ANS overactivity, such as tachycardia, rise of BP, sweating and lacrimation.
Grimacing;
Other muscle activity.
Surgical anaesthesia is indicated by:
Loss of eyelash (lid) reflex
Development of rhythmic respiration.
Deep anaesthesia is suggested by :
Depression of respiration.
Hypotension
Asystole
This document discusses general anesthetics, which are drugs that produce unconsciousness and loss of sensation. It defines general anesthesia and describes the four stages of anesthesia: analgesia, delirium/excitement, surgical anesthesia, and medullary paralysis. It classifies general anesthetics as inhalation anesthetics, ultra short-acting barbiturates, and dissociative anesthetics. For each class, it provides examples (e.g. halothane, sevoflurane, ketamine) and summarizes their mechanisms of action, properties, uses and syntheses.
General anaesthetics are CNS depressants that produce partial or total loss of pain sensation through controlled and reversible depression of CNS function. They act by fluidizing neuronal cell membranes, inhibiting ion channel proteins essential for nerve conduction. Various classes include volatile liquids/gases administered via inhalation as well as intravenous barbiturates and dissociatives. While effective, general anaesthetics have varying degrees of toxicity, flammability, and other side effects.
Agents that produces loss of consciousness are anesthetics.
They induce smooth and rapid effect for limited period. There are five stages of anesthesia. They are classified as INHALATION ANESTHETICS, ULTRA SHORT ACTING BARBITURATES and DISSOCIATIVE ANESTHETICS.
General anesthesia Presentation by Muhammad SaeedMuhammad Saeed
General anesthesia involves loss of sensation and consciousness. It is used for surgeries and certain medical procedures. There are three main types: general anesthesia which induces unconsciousness; regional anesthesia which blocks pain in a specific body region; and local anesthesia which blocks pain in a small, localized area. The document then discusses the stages of anesthesia, mechanisms of action involving GABA receptors, and properties of various inhalational anesthetic agents like nitrous oxide, ether, halothane, enflurane, isoflurane, desflurane, and sevoflurane.
This document discusses catecholamines and their mechanisms of action. It describes seven types of actions that catecholamines and sympathomimetic agents can have in the body. It then focuses on the specific catecholamines norepinephrine, epinephrine, and dopamine. It details the synthesis of norepinephrine via tyrosine hydroxylation and other enzymatic steps. It also discusses norepinephrine storage in vesicles, release via calcium influx, and termination of action through reuptake into neurons or nearby cells. Finally, it classifies adrenoceptors and their downstream effects.
Catecholamines and sympathomimetic agents have seven broad types of actions in the body: 1) excitatory effects on smooth muscle and glands, 2) inhibitory effects on smooth muscle, 3) excitatory effects on the heart, 4) metabolic effects, 5) endocrine effects, 6) central nervous system effects, and 7) effects on neurotransmitter release. The three most important catecholamines are norepinephrine, epinephrine, and dopamine. Norepinephrine is a neurotransmitter released by sympathetic nerves, epinephrine is a hormone from the adrenal medulla, and dopamine is a precursor to norepinephrine and epinephrine. Catecholamines exert their
This document describes several inhalational anesthetic agents including halothane, ether, enflurane, isoflurane, desflurane, and sevoflurane. It discusses their physical and chemical properties, mechanisms of action, advantages, and disadvantages. The key points are:
- These agents work by altering the function of ion channels in the central nervous system to produce effects like unconsciousness and amnesia.
- They have various cardiovascular, respiratory, and other systemic effects depending on the specific agent.
- While rapid induction and recovery are advantages for some agents, others have greater risks of toxicity like hepatitis or sensitizing the heart to arrhythmias. Agent selection depends on balancing risks and benefits for each patient.
General anesthesia involves 3 stages:
1) Analgesia - Relief from pain without loss of consciousness
2) Excitement - Potential combative behavior as anesthesia takes effect
3) Surgical anesthesia - Unconsciousness, muscle relaxation, and loss of response to painful stimuli allowing for surgery
The document discusses the history of general anesthesia from ancient times using substances like opium to modern inhalational and intravenous agents. It also covers the pharmacological mechanisms and classes of different anesthetic drugs as well as considerations for their administration and side effects. Pre-anesthetic medications are discussed to reduce anxiety and smooth induction of anesthesia.
General anesthetics were introduced in the 19th century with diethyl ether and chloroform. While effective, they had toxicity issues. In the 1840s-50s, William Morton, Pirogoff, and James Young Simpson successfully used ether and chloroform for surgeries and obstetrics. Modern balanced anesthesia uses combinations of inhaled and injectable anesthetics along with analgesics and muscle relaxants to reduce risks and side effects compared to single agents. Common inhaled agents include desflurane, isoflurane, sevoflurane, and nitrous oxide. Injectables include propofol, etomidate, ketamine, and barbiturates like thiopental.
Anesthesiology involves rendering a patient comfortable and physiologically stable before, during, and after a procedure using reversible anesthesia. General anesthesia is used for surgical procedures to make the patient unaware of painful stimuli. Anesthesia decreases the body's stress response to surgery and is associated with lowering blood pressure and blunting the central sympathetic nervous system. The main targets of inhalational anesthetics are the brain, and there are two main types - inhalational for maintenance of anesthesia and intravenous for induction and short procedures. Inhalational anesthetics like halothane, enflurane, and isoflurane are commonly used but each has specific advantages and disadvantages.
General anesthetics work by depressing the central nervous system starting with the cerebral cortex. They are used during surgery to induce unconsciousness and abolish pain sensation. There are several stages of anesthesia from analgesia to medullary paralysis. General anesthetics are classified as inhalation agents like halothane, dissociative agents like ketamine, and ultra short-acting barbiturates like methohexital. Inhalation agents directly reach the lungs and bloodstream while others must pass the blood brain barrier. These drugs work by potentiating GABA, glycine, or inhibiting NMDA receptors to produce neuronal inhibition.
General and Local Anaesthetics drugs.pptxdrarunsingh4
This document provides information on general and local anaesthetics. It begins by defining general anaesthesia as a reversible condition that renders a patient unaware during a medical procedure, which is produced through general anaesthetic drugs. Local anaesthesia is defined as reversible nerve inhibition in a localized area, produced through local anaesthetic drugs.
The document then discusses the stages of general anaesthesia and compares the key differences between general and local anaesthetics. It provides classifications and examples of different types of general anaesthetics including inhalational and intravenous agents. The mechanisms of action and effects of various general anaesthetics like ether, nitrous oxide, and halothane are summarized.
The document discusses various inhalational anesthetics used in veterinary medicine including their properties, mechanisms of action, advantages, and disadvantages. It describes key terms like MAC and blood:gas partition coefficients. Specific anesthetics covered include ether, halothane, methoxyflurane, enflurane, isoflurane, nitrous oxide, cyclopropane, and chloroform. Their potencies, effects on vital organs, muscle relaxation properties, and appropriate uses are summarized. Contraindications and safety concerns are also mentioned for some agents.
1. Alkylating agents are a class of anticancer drugs that work by introducing alkyl groups onto DNA, interfering with DNA separation and cell division. Common alkylating agents include nitrogen mustards, cyclophosphamide, ifosfamide, busulfan, nitrosoureas, thiotepa, and procarbazine.
2. These drugs are metabolized in the liver and form reactive metabolites that alkylate guanine bases in DNA, forming crosslinks that prevent cell division. Many require metabolic activation and have toxic metabolites that can cause side effects like hemorrhagic cystitis.
3. Co-administration of drugs like mesna and sodium thiosulfate can help detoxify toxic
This document summarizes several protozoal diseases and their treatment with anti-parasitic drugs. It discusses the diseases giardiasis and amebiasis caused by the protozoa Giardia lamblia and Entamoeba histolytica respectively. It also discusses trichomoniasis caused by Trichomonas vaginalis. The main drugs used to treat these diseases are metronidazole, tinidazole, and nitazoxanide. It provides details on the mechanisms of action and metabolism of these drugs. It also briefly discusses diloxanide furoate and leishmaniasis.
This document summarizes various anti-malarial agents. It discusses the classes of drugs used to treat malaria, including cinchona alkaloids, 4-aminoquinolines, 8-aminoquinolines, diaminopyrimidines, amino alcohols, artemisinins, antibiotics, and fixed combinations. Key drugs discussed include chloroquine, primaquine, pyrimethamine, atovaquone-proguanil, and artemisinin derivatives. The document also briefly discusses vaccine development efforts for malaria.
This document discusses antifungal drugs. It begins by describing common fungal infections that antifungals treat, such as ringworm and athlete's foot. It then discusses the different types of fungal infections including superficial infections of the skin and internal organ infections. The document outlines the main biochemical targets of antifungals and describes the structure and mechanisms of several major classes of antifungal drugs, including azoles, polyenes like amphotericin B and nystatin, and the heterocyclic compound griseofulvin. It provides details on specific antifungals like their structures, mechanisms of action, uses, and side effects.
This document provides an overview of anti-cancer drugs, beginning with an introduction to cancer and statistics on cancer cases in Iraq. It then discusses the classification of anti-cancer drugs according to their chemical structure and mechanisms of action. Specifically, it covers alkylating agents including nitrogen mustards, alkyl sulphonates, nitrosoureas, and aziridines. It provides details on the structures, mechanisms of action, uses, and side effects of common alkylating agents like cyclophosphamide, ifosfamide, busulfan, carmustine, and thiotepa. The document focuses on describing the chemical properties and metabolic pathways that allow these drugs to damage cancer cell DNA and induce cell death.
1. The document discusses several classes of anticancer drugs including antimetabolites, anthracyclines, and natural products.
2. It focuses on antimetabolites such as pyrimidine and purine analogs that interfere with DNA synthesis including 5-fluorouracil, capecitabine, cytarabine, gemcitabine, and 6-mercaptopurine.
3. The mechanisms of these drugs and how they inhibit key enzymes like thymidylate synthase and dihydrofolate reductase is explained.
This document summarizes different classes of anthelmintic drugs used to treat helminth infections. It discusses the chemical structures, mechanisms of action, and metabolism of various classes including benzimidazoles (e.g. albendazole, mebendazole), piperazines (e.g. piperazine citrate, diethylcarbamazine citrate), heterocyclics (e.g. oxamniquine, praziquantel), vinyl pyrimidines (e.g. pyrantel palmoate), amides (e.g. niclosamide), and natural products (e.g. ivermectin). It provides details on the
Parkinson's disease is caused by a loss of dopamine-producing neurons in the substantia nigra. Symptoms include tremors, stiffness, and impaired movement. Anti-Parkinsonian drugs work by increasing dopamine levels in the brain. These include dopamine precursors like levodopa, dopamine receptor agonists, MAO-B inhibitors, COMT inhibitors, and anticholinergic agents. Newer treatments include the dopamine releaser amantadine and drugs that target the adenosine A2A receptor like istradefylline. Deep brain stimulation is also used to treat motor symptoms.
Barbiturates are central nervous system depressants that were historically used as sedatives, hypnotics, and anticonvulsants. They work by enhancing the effects of the neurotransmitter GABA. While largely replaced by safer benzodiazepines, barbiturates are still used for certain medical purposes. Their structure is based on barbituric acid, with activity requiring lipophilic 5,5-disubstitutions for blood-brain barrier crossing. Mechanisms of action, classifications by duration, and metabolism pathways are described.
This document provides information about benzodiazepines, including their history, mechanisms of action, structures, and metabolism. Benzodiazepines work by enhancing the effects of the inhibitory neurotransmitter GABA in the brain. They are commonly used to treat anxiety, insomnia, seizures and muscle spasms. The first benzodiazepine developed was chlordiazepoxide in 1955. Key structural features that influence their pharmacological properties include functional groups at the 1st, 2nd, 3rd, 4th, 5th and 7th positions of the benzodiazepine ring system. Metabolism and elimination pathways determine a benzodiazepine's duration of action from short-acting to long-acting
This document provides an overview of β-lactam antibiotics, including penicillins. It begins by classifying common antibiotics and listing their mechanisms of action. It then focuses on β-lactam antibiotics, describing their structure and major subclasses like penicillins, cephalosporins, carbapenems, and monobactams. Specific penicillins are discussed in depth, highlighting their structures, spectra of activity, stability properties, and mechanisms of resistance. β-lactamase inhibitors like clavulanic acid are also introduced.
This document provides information about anti-viral drugs. It begins by defining viruses and their structure. It then discusses different classes of anti-viral drugs, including those that block viral attachment and entry, inhibit penetration, act as uncoating inhibitors, and are nucleic acid inhibitors that target polymerases or reverse transcriptase. Specific drugs are discussed for each class, along with their mechanisms of action, structures, and importance for treating various viral diseases like HIV, hepatitis, herpes, and influenza.
The document discusses various antiepileptic drugs (AEDs) and their mechanisms of action. It covers major classes of AEDs including valproic acid, phenytoin, carbamazepine, lamotrigine, topiramate, and zonisamide. The main mechanisms of AEDs are enhancement of GABA activity, inhibition of sodium channels, and inhibition of calcium channels. The document discusses the metabolism, pharmacokinetics, indications, contraindications and side effects of the various AEDs. It provides details on the chemical structures and metabolic pathways of many commonly used AEDs.
Here is the updated list of Top Best Ayurvedic medicine for Gas and Indigestion and those are Gas-O-Go Syp for Dyspepsia | Lavizyme Syrup for Acidity | Yumzyme Hepatoprotective Capsules etc
Rasamanikya is a excellent preparation in the field of Rasashastra, it is used in various Kushtha Roga, Shwasa, Vicharchika, Bhagandara, Vatarakta, and Phiranga Roga. In this article Preparation& Comparative analytical profile for both Formulationon i.e Rasamanikya prepared by Kushmanda swarasa & Churnodhaka Shodita Haratala. The study aims to provide insights into the comparative efficacy and analytical aspects of these formulations for enhanced therapeutic outcomes.
share - Lions, tigers, AI and health misinformation, oh my!.pptxTina Purnat
• Pitfalls and pivots needed to use AI effectively in public health
• Evidence-based strategies to address health misinformation effectively
• Building trust with communities online and offline
• Equipping health professionals to address questions, concerns and health misinformation
• Assessing risk and mitigating harm from adverse health narratives in communities, health workforce and health system
Integrating Ayurveda into Parkinson’s Management: A Holistic ApproachAyurveda ForAll
Explore the benefits of combining Ayurveda with conventional Parkinson's treatments. Learn how a holistic approach can manage symptoms, enhance well-being, and balance body energies. Discover the steps to safely integrate Ayurvedic practices into your Parkinson’s care plan, including expert guidance on diet, herbal remedies, and lifestyle modifications.
Histololgy of Female Reproductive System.pptxAyeshaZaid1
Dive into an in-depth exploration of the histological structure of female reproductive system with this comprehensive lecture. Presented by Dr. Ayesha Irfan, Assistant Professor of Anatomy, this presentation covers the Gross anatomy and functional histology of the female reproductive organs. Ideal for students, educators, and anyone interested in medical science, this lecture provides clear explanations, detailed diagrams, and valuable insights into female reproductive system. Enhance your knowledge and understanding of this essential aspect of human biology.
Does Over-Masturbation Contribute to Chronic Prostatitis.pptxwalterHu5
In some case, your chronic prostatitis may be related to over-masturbation. Generally, natural medicine Diuretic and Anti-inflammatory Pill can help mee get a cure.
TEST BANK For Community Health Nursing A Canadian Perspective, 5th Edition by...Donc Test
TEST BANK For Community Health Nursing A Canadian Perspective, 5th Edition by Stamler, Verified Chapters 1 - 33, Complete Newest Version Community Health Nursing A Canadian Perspective, 5th Edition by Stamler, Verified Chapters 1 - 33, Complete Newest Version Community Health Nursing A Canadian Perspective, 5th Edition by Stamler Community Health Nursing A Canadian Perspective, 5th Edition TEST BANK by Stamler Test Bank For Community Health Nursing A Canadian Perspective, 5th Edition Pdf Chapters Download Test Bank For Community Health Nursing A Canadian Perspective, 5th Edition Pdf Download Stuvia Test Bank For Community Health Nursing A Canadian Perspective, 5th Edition Study Guide Test Bank For Community Health Nursing A Canadian Perspective, 5th Edition Ebook Download Stuvia Test Bank For Community Health Nursing A Canadian Perspective, 5th Edition Questions and Answers Quizlet Test Bank For Community Health Nursing A Canadian Perspective, 5th Edition Studocu Test Bank For Community Health Nursing A Canadian Perspective, 5th Edition Quizlet Test Bank For Community Health Nursing A Canadian Perspective, 5th Edition Stuvia Community Health Nursing A Canadian Perspective, 5th Edition Pdf Chapters Download Community Health Nursing A Canadian Perspective, 5th Edition Pdf Download Course Hero Community Health Nursing A Canadian Perspective, 5th Edition Answers Quizlet Community Health Nursing A Canadian Perspective, 5th Edition Ebook Download Course hero Community Health Nursing A Canadian Perspective, 5th Edition Questions and Answers Community Health Nursing A Canadian Perspective, 5th Edition Studocu Community Health Nursing A Canadian Perspective, 5th Edition Quizlet Community Health Nursing A Canadian Perspective, 5th Edition Stuvia Community Health Nursing A Canadian Perspective, 5th Edition Test Bank Pdf Chapters Download Community Health Nursing A Canadian Perspective, 5th Edition Test Bank Pdf Download Stuvia Community Health Nursing A Canadian Perspective, 5th Edition Test Bank Study Guide Questions and Answers Community Health Nursing A Canadian Perspective, 5th Edition Test Bank Ebook Download Stuvia Community Health Nursing A Canadian Perspective, 5th Edition Test Bank Questions Quizlet Community Health Nursing A Canadian Perspective, 5th Edition Test Bank Studocu Community Health Nursing A Canadian Perspective, 5th Edition Test Bank Quizlet Community Health Nursing A Canadian Perspective, 5th Edition Test Bank Stuvia
Basavarajeeyam is a Sreshta Sangraha grantha (Compiled book ), written by Neelkanta kotturu Basavaraja Virachita. It contains 25 Prakaranas, First 24 Chapters related to Rogas& 25th to Rasadravyas.
- Video recording of this lecture in English language: https://youtu.be/kqbnxVAZs-0
- Video recording of this lecture in Arabic language: https://youtu.be/SINlygW1Mpc
- Link to download the book free: https://nephrotube.blogspot.com/p/nephrotube-nephrology-books.html
- Link to NephroTube website: www.NephroTube.com
- Link to NephroTube social media accounts: https://nephrotube.blogspot.com/p/join-nephrotube-on-social-media.html
TEST BANK For An Introduction to Brain and Behavior, 7th Edition by Bryan Kol...rightmanforbloodline
TEST BANK For An Introduction to Brain and Behavior, 7th Edition by Bryan Kolb, Ian Q. Whishaw, Verified Chapters 1 - 16, Complete Newest Versio
TEST BANK For An Introduction to Brain and Behavior, 7th Edition by Bryan Kolb, Ian Q. Whishaw, Verified Chapters 1 - 16, Complete Newest Version
TEST BANK For An Introduction to Brain and Behavior, 7th Edition by Bryan Kolb, Ian Q. Whishaw, Verified Chapters 1 - 16, Complete Newest Version
2. Anesthesia
▪ Anesthesia is a way to used to (control pain) blocks the transmission of pain.
▪ General anesthetics are a group of drugs commonly used in major surgery to
produce unconsciousness, analgesia, and depression of reflexes.
▪ General anesthesia: affects your brain and the rest of your body.
▪ Local anesthetics are used to block nerve transmission, to reduce or
eliminate sensation of pain in small area of the body without affecting
consciousness.
▪ Epidural and Spinal Anesthesia
▪ Epidural and spinal blocks are types of anesthesia in which a local
anesthetic is injected near the spinal cord and nerve roots. It blocks pain
from an entire region of the body, such as the belly, the hips, the legs, or
the pelvis. Epidural anesthesia is often used in childbirth
3. Stages of anesthesia produced by general anesthetics:
Stage I - analgesia results from an increase in circulating endorphins.
Stage II - loss of consciousness (secretions are managed by anticholinergic agents)
Stages I and II together are referred to as induction.
Stage III – anesthesia (surgical anesthesia) loss of spinal reflexes and muscle tone
(suitable for surgical procedures).
Stage IV - undesirable stage (characterized by respiratory depression) and ends in death
.
4. Mechanisms of anesthesia
1- Blocking the NMDA and glutamate controlled channels.
▪ Glutamate or NMDA (N-methyl-D-aspartate) receptors in the CNS are activated by the excitatory AA
neurotransmitter glutamic acid.
➢ Agonists: This activation opens the channel, allowing K+ to flow to the extra cellular fluid and Na and
Ca++ to flow into the nerve cell. The increased intracellular [Ca++] activates the liberation of the
(NO), which causes alertness (consciousness).
➢ Antagonists: Ketamine blocks NMDA receptors, causes CNS depression (anesthesia)
2- Activation of the inhibitory GABA receptor controlled channel.
▪ Binding of GABA (inhibitory transmitter) to their receptors will open the Cl- channel, leading to the
influx of Cl- and hyper- polarization of the neuron.
o Halothane and isoflurane inhibit the synaptic destruction of GABA, thereby increasing the GABA-ergic
neurotransmission.
o Benzodiazepines and barbiturates: Enhance GABA opening Cl channels γ-aminobutyric acid (GABA)
o Benzodiazepines and barbiturates produce anesthesia, by enhancing of GABA opening of the chloride
channel
3- Inhaled anesthetics are also known to enhance the major inhibitory receptors in the spinal cord, the
glycine receptors.
5. Classification Of General Anesthetics
Methohexital
Xenon
morphine
Isoflurane
desflurane
sevoflurane
Remimazolam
6. The Ideal Inhaled Anesthetic Drugs:
The ideal inhaled anesthetic will be:
➢ Inexpensive
➢ Potent
➢ Minimally soluble in the blood and tissues
➢ Pleasant to inhale
➢ Stable on the shelf and during administration
➢ Lack undesirable side effects such as:
▪ Cardiotoxicity
▪ Hepatotoxicity
▪ Renal toxicity
▪ Neurotoxicity.
7. Potency (MAC):
▪ The most common way to measure inhaled anesthetic potency is by recording the minimum alveolar
concentration (MAC) needed to prevent movement to a painful stimulus. The MAC concentrations
are recorded at 1 atmosphere and reported as the mean concentration needed to abolish movement
in 50% of subjects.
▪ MAC expressed as the percentage of gas in a mixture required to achieve the effect. Numerically,
MAC is small for potent anesthetics such as methoxyflurane and large for less potent agents such as
nitrous oxide.
▪ Potency α
Properties of the Inhaled Anesthetics
Most potent
Least potent
8. Solubility:
➢ Blood: gas partition coefficient:
▪ Blood : gas partition co-efficient It is a measure of solubility in the blood.
▪ The blood:gas partition coefficient is defined as the ratio of the concentration of the drug in the
blood to the concentration of the drug in the gas phase (in the lung), at equilibrium.
▪ It determines the rate of induction and recovery of Inhalational anesthetics.
▪ Lower the blood : gas co-efficient – faster the induction and recovery (Nitrous oxide)
▪ Higher the blood : gas co-efficient – slower induction and recovery (methoxyflurane )
Rock
9. Properties of the Inhaled Anesthetics
➢ Oil : gas partition coefficient
▪ Oil: gas partition co-efficient It is a measure of lipid solubility.
▪ Lipid solubility correlates strongly with the potency of the anesthetic.
▪ Higher the lipid solubility, more potent anesthetic (e.g., methoxyflurane )
10. ➢ Arteriovenous concentration gradient (ACG)
▪ Difference between concentration of anesthetic drug in artery and veins.
▪ Smaller the ACG value faster will be the onset of action and vice versa.
Example:
Drug A Drug B
Artery = 100mg Artery = 100mg
Vein = 20mg Vein = 80mg
ACG= 80 mg ACG= 20 mg
Blood saturation
Slow onset of action
Blood saturation
Fast onset of action
11. Stability:
▪ The early inhaled anesthetics suffered from stability problems, leading to explosions
and operating room fires.
Example:
▪ Ether (Diethyl ether) is not used now in developed countries because of its
unpleasant and inflammable properties.
▪ By halogenating the ether and hydrocarbon anesthetics, the explosiveness and
flammability of the drugs were diminished, and the number of operating room fires
decreased.
▪ Halogenation clearly stabilizes the inhaled agent and all inhaled anesthetics used
today contain halogens
Diethyl ether
12. Structure–Activity Relationships of the Volatile General Anesthetics
▪ The inhalation anesthetics in use today are nitrous oxide, halothane, isoflurane, desflurane, and
sevoflurane.
1- Alkane/Cycloalkane
▪ The potency of alkanes, cycloalkanes, and aromatic hydrocarbons increases in direct proportion to the
number of carbon atoms in the structure up to a cutoff point.
▪ Within the n-alkane series, the cutoff number is 10, with n-decane showing minimal anesthetic potency.
▪ In the cycloalkane series, the cutoff number in most studies is eight with cyclooctane showing no
anesthetic activity in the rat.
▪ The reduced activity of the compounds beyond their cutoff number could be a result of problems getting
to the site of action (reduced vapor pressure or high blood solubility) or inability to bind to the site of
action and induce the conformational change required for anesthetic action.
▪ The cycloalkanes are more potent anesthetics than the straight chain analog with the same number of
carbons. For example, the MAC of cyclopropane in rats is about one fifth of the MAC of n-propane.
13. 2- Effect of Halogenation/Ether Halogenation :
▪ The first inhaled anesthetics used in the late 1800s, diethyl ether and cyclopropane caused laryngospasms.
These compounds were also explosive and flammable requiring careful handling.
▪ Early studies found that halogenating the ethers decreased the flammability of the compounds, enhanced
their stability and increased their potency. Higher atomic mass halogens increased potency compared to
lower atomic mass halogens.
▪ For example, replacing the fluorine in desflurane (CF2HOCFHCF3) with chlorine to form isoflurane
(CF2HOCClHCF3) increased potency more than fourfold. Replacing the chlorine with bromine in the
investigational agent I-537`(CF2HOCBrHCF3) increased potency threefold further.
▪ Halogenated ether compounds also caused less laryngospasms than unhalogenated compounds.
▪ Unfortunately, halogenation also increased the propensity of the drugs to cause cardiac arrhythmias
and/or convulsions.
▪ Halogenated methyl ethyl ethers were found to be more stable and potent than halogenated diethyl
ethers. The commonly used inhaled anesthetics are ethers or aliphatic hydrocarbons with 2 to 5 carbon
atoms.
14. 3- Alkanol Series:
▪ A similar increase in potency with increase in carbon length was seen in the n- alkanol series. In addition,
the n-alkanol with a given number of carbons is more potent than the n-alkane with the same chain
length.
4- Effect of Saturation:
▪ The addition of double and/or triple bonds to small anesthetic molecules having 6 carbon atoms or
less increases potency.
15. Inhaled anesthetic Products
Gas:
1-Nitrous oxide (laughing gas):
▪ Nitrous oxide is a gas at room temperature and is supplied as a liquid under pressure in metal
cylinders. Nitrous oxide is a“dissociative anesthetic” and causes slight euphoria and
hallucinations.
▪ The low potency of nitrous oxide (MAC= 104%) precludes it from being used alone for surgical
anesthesia.
▪ It is a potent analgesic but a weak general anesthetic. Rapid onset and recovery, does not
depress respiration, and no muscle relaxation.
▪ To use it as the sole anesthetic agent the patient would have to breathe in pure N2O to the
exclusion of oxygen. This situation would obviously cause hypoxia and potentially lead to
death.
➢ Nitrous oxide can inactivate methionine synthase, a B12-dependent enzyme necessary for the
synthesis of DNA and therefore should be used with caution in pregnant and B12-deficient
patients.
16. 2-Xenon(Xe):
▪ Xenon is an interesting anesthetic as it appears to lack negative inotropicy and vasodilatation,
giving great advantages to both patients with limited cardiovascular reserve or those who
require hemodynamic stability.
▪ Xenon is an inert gas that is nonflammable and nonexplosive.
▪ It has low toxicity and is not teratogenic.
▪ Xenon gives rapid induction and recovery, due to its low blood/gas partition coefficient
(0.15), and has a MAC of 63%.
▪ Several vitro studies showed that Xenon may protect neural cells against ischaemic injury
17. Volatile liquids:
1-Halothane:
▪ Halothane is a nonflammable, nonpungent, volatile, liquid, halogenated (F, Cl, and Br) ethane
(bp =50°C). Halothane may increase heart rate, cause cardiac arrhythmias, increase cerebral
blood flow, and increase intracranial pressure.
▪ It can undergo spontaneous oxidation when exposed to ultraviolet light to yield HCl,HBr, Cl-, Br-
, and phosgene (COCl2). To prevent oxidation it is packaged in amber bottles with a low
concentration of thymol (0.01%) as a stabilizer.
▪ The drug has a high potency (MAC= 0.75%), a blood:gas partition coefficient of 2.4, and high
adipose solubility.
18. Synthesis of halothane
1. Hydrogen fluoride is added to trichloroethylene and on
simultaneous substitution of chloride atoms in presence of
antimony(III) chloride at 130oC produces 2-chloro-1,1,1-
trifluoroethane.
2. The above formed compound undergoes bromination at 450oC
to produce halothane.
19. Halothane metabolism
▪ Halothane undergoes both reductive and
oxidative processes with up to 20% of the
dose undergoing metabolism.
▪ The trifluoroacetyl chloride metabolite is
electrophilic and can form covalent bonds
with proteins leading to immune
responses and halothane hepatitis upon
subsequent halothane exposure.
Halothane hepatitis is rare with 1 case
reported for every 6,000 to 35,000
patients exposed.
20. Malignant hyperthermia (MH)
▪ The use of inhaled anesthetics and halothane in particular can produce
malignant hyperthermia (MH) in genetically susceptible individuals. This
results in an increase in body temperature, tachycardia, tachypnea,
acidosis, and rhabdomylolysis. MH is a result of the excessive release of
calcium from the sarcoplasmic reticulum (SR).
▪ Dantrolene is used for the prevention and treatment of malignant
hyperthermia during anesthesia. It achieves this by inhibiting Ca2+ ions
release from sarcoplasmic reticulum stores.
21. 2- Methoxyflurane:
▪ Methoxyflurane is a volatile liquid (bp = 105°C) with a high blood:gas partition coefficient
and thus a slow induction and prolonged recovery. Approximately 75% of the drug
undergoes metabolism yielding dichloroacetate, difluoromethoxy acetate, oxalate, and
fluoride ions.
▪ The intrarenal inorganic fluoride concentration, as a result of renal defluorination, may be
responsible for the nephrotoxicity seen with methoxyflurane.
22. 3-Enflurane:
▪ Enflurane is a volatile liquid (bp =56.5°C) with a blood: gas partition coefficient of 1.8 and an MAC of 1.68%.
▪ Enflurane may increase heart rate, cause cardiac arrhythmias, increase cerebral blood flow, and increase
intracranial pressure but all to a smaller degree than halothane.
▪ Enflurane also causes electroencephalographic (EEG) patterns consistent with electrical seizure activity. It
has caused tonic–clonic convulsive activity in patients when used at high concentrations or during profound
hypocarbic periods. Enflurane is therefore not recommended in patients with seizure disorders.
▪ Approximately 2% to 8% of the drug is metabolized primarily at the chlorofluoromethyl carbon. Little
chlorofluoroacetic acid is produced suggesting minor metabolism at the difluoromethyl carbon.
Difluoromethoxydifluoroacetate and fluoride ion have been reported as metabolites.
23. 4-Isoflurane:
▪ Isoflurane is a volatile liquid (bp = 48.5°C) with an MAC of 1.15, a blood:gas partition coefficient of 1.43
and high solubility in fat.
▪ Isoflurane is a structural isomer of enflurane. It is a known respiratory irritant, but less so than
desflurane. Approximately 0.2% of the administered drug undergoes metabolism, the rest is exhaled
unchanged.
▪ The metabolism of isoflurane yields low levels of the nephrotoxic fluoride ion as well as a potentially
hepatotoxic trifluoroacetylating compound. The relatively low concentrations of these compounds
have resulted in very low risks of hepatotoxicity and nephrotoxicity.
25. 5-Desflurane:
▪ Desflurane is a nonflammable, colorless, very volatile liquid packaged in amber-colored vials. The
boiling point is 22.8°C, and it requires a vaporizer specifically designed for desflurane.
▪ Desflurane has a blood:gas partition coefficient of 0.42, an MAC of 7.3% and an oil:gas partition
coefficient of 18.7. The low blood:gas partition coefficient leads to fast induction times and short
recovery times.
▪ Desflurane is not recommended for induction anesthesia in children because of the high incidence
of laryngospasms (50%), coughing (72%), breath holding (68%), and increase in secretions (21%).
▪ Desflurane can react with desiccated carbon dioxide absorbents to produce carbon monoxide that
may result in elevated levels of carboxyhemoglobin.
▪ Desflurane is metabolized minimally with less than 0.02% of the administered dose recovered as
urinary metabolites.
▪ Desflurane produces minimal free fluoride ion and very little trifluoroacetic acid and has not been
reported to cause either kidney or liver damage.
26. 6-Sevoflurane:
▪ Sevoflurane is a volatile, nonpungent, nonflammable, and nonexplosive liquid with a boiling
point of 58.6°C. The blood:gas partition coefficient is 0.65, the oil:gas partition coefficient is
50, and the MAC is 2.1%.
▪ Sevoflurane reacts with desiccated carbon dioxide adsorbents, to produce compounds (A and
B) with known toxicity.
▪ The major breakdown product, compound A, pentafluoroisopropenyl fluoromethyl ether,
(PIFE, C4H2F6O) has been studied extensively. Compound A is nephrotoxic in rats and
nonhuman primates and remains a theoretical risk to humans.
▪ Approximately 5% to 8% of the administered dose of sevoflurane is metabolized in man by
CYP2E1 to hexafluo roisopropanol, CO2 and the potentially nephrotoxic fluoride ion
27.
28. ▪ Diethyl ether is a potent anesthetic whose actions are accompanied by analgesic and
muscle relaxant activity. It is highly flammable and explosive.
▪ The MAC of ether in humans is around 3.2%.
▪ Ether is sweet smelling and mildly pungent; although it can be used for inhalational
induction, an ether induction is very slow and risks laryngospasm.
▪ Ether is still used as an anesthetic in some developing countries because of its low
cost and high therapeutic index with minimal cardiac and respiratory depression.
▪ Chloroform is a halogenated hydrocarbon that, unlike ether, is not flammable but has
significant toxicity, including carcinogenicity, hepato-, and nephrotoxicity.
▪ chloroform soon emerged as the more widely used, as it took action faster and was
non-flammable.
▪ On the other hand, there were higher risks associated with chloroform than with
ether, and its administration required greater physician skill.
▪ Usage of ether and chloroform later declined after the development of safer, more
effective inhalation anesthetics, and they are no longer used in surgery today.
Ether and Chloroform
Diethyl ether
Chloroform
29. The Injectable General Anesthetics:
1-Propofol:
• Propofol is an injectable sedative–hypnotic used for the induction and
maintenance of anesthesia or sedation.
• The pKa of the propanol hydroxyl is 11 and the injectable emulsion has a pH of 7 to 8.5.
• Formulations contain either disodium ethylenediaminetetraacetic acid (EDTA) (0.005%) or
sodium metabisulfite to retard the growth of microorganisms. EDTA is a metal chelator and
patients on propofol containing EDTA for extended periods of time excrete more zinc and
iron in their urine
• Propofol is quickly and extensively metabolized with 88% of a 14C-labelled intravenous
administered dose appearing in the urine as conjugates. Less than 2% of the dose is found
unchanged in the feces and less than 0.3% found unchanged in the urine. Thirty minutes
after the 14C-labelled dose was administered, 81% of the radioactivity was in the form of
metabolites Propofol has a quick onset of action (arm-to-brain circulation time) and a quick
recovery time.
31. 2- Fospropofol:
▪ Fospropofol is a water soluble prodrug and is converted to propofol in the liver.
▪ Breakdown by phosphatase to release propofol
▪ Fospropofol is a short acting hypnotic/sedative/anesthetic agent.
▪ Unlike propofol, does not cause injection-site pain as it is unable to activate TRPA1.FDA approved in
December 2008.
▪ It is currently approved for use in sedation of adult patients undergoing diagnostic or therapeutic
procedures such as endoscopy.
▪ Fospropofol is administered in conjunction with an opioid such as fentanyl
32. 3-Etomidate:
▪ Etomidate is a carboxylated imidazole intended for the induction of general
anesthesia.
▪ Etomidate is rapidly metabolized in the plasma and liver via esterases. About
75% of the drug is eliminated in the urine as the inactive ester hydrolyzed
carboxylic acid.
▪ It is only used for patients with coronary artery disease or cardiovascular
dysfunction. No effect on heart and circulation. lacks analgesic activity.
Esterases
Carboxylic acid
Ester
33. 4-Ketamine:
▪ Ketamine is formulated as an acidic solution, pH 3.5 to 5.5, available with or without 0.1 mg/mL
benzethonium chloride preservative.
▪ Unlike the proposed mechanism of action for most anesthetics, ketamine does not act at the
GABAA receptor. Ketamine acts as a noncompetitive antagonist at the glutamate, NMDA receptor,
a nonspecific ion channel receptor. The NMDA receptor is located throughout the brain and
contains four well-studied binding sites. The primary binding site binds L-glutamate, NMDA, and
aspartate.
▪ Ketamine is metabolized via N-demethylation to form the main metabolite norketamine.
▪ Norketamine has about one third the potency of the parent compound. Minor metabolic pathways
include hydroxylation of the cyclohexanone ring; hydroxylation followed by glucuronide
conjugation, and hydroxylation followed by dehydration to the cyclohexenone derivative.
35. 5- Fentanyl:
▪ Fentanil, is an opioid used as a pain medication and together with other medications for
anesthesia.
▪ Often used in cardiac surgery because not cause CV toxicity
▪ To maintain anesthesia, inhaled anesthetics and additional fentanyl may be used. These are
often given in 15-30 minute intervals throughout procedures such as endoscopy, surgeries, and
in emergency rooms.
36. 6- Thiopental (pentothal):
▪ It is a rapid-onset short-acting barbiturate general anesthetic. , has a very low analgesic
properties (used by IV as sodium salt).
▪ Induction of the sulfur enhanced lipophilicity.
▪ Onset- 30-60 sec : Peak- 10-30 min : Half-life- 12 min : Duration- 20-30 min
▪ Adverse effects: Can produce severe respiratory depression (Respiratory), apnea, airway
obstruction, depress the myocardium and causes dysrhythmias (Cardiovascular),
hypotension.
▪ Contraindication in liver disease, severe heart disease, severe hypotension and severe
breathing disorder.
37. 7- Midazolam:
▪ Midazolam is used before surgery or a procedure. It helps to cause drowsiness,
decrease anxiety, and to decrease your memory of the surgery or procedure.
▪ This medication may also be used to help with anesthesia or to sedate people who
need a tube or machine to help with breathing. Midazolam works by calming the brain
and nerves. It belongs to a class of drugs known as benzodiazepines.
▪ Advantage: Causes little cardiovascular and respiratory problem compare to other IV
anesthetic drugs.
38. ▪ It acts on GABA receptors, as does midazolam, and exhibits
pharmacokinetic properties common to the ester-based opioid
remifentanil.
▪ In animal studies, remimazolam produced a more rapid onset and
faster recovery than did midazolam.
▪ Remimazolam significantly potentiated the analgesic effect of
remifentanil, without lung irritation, bronchospasm, or other adverse
pulmonary event
▪ Remimazolam was approved for medical use in the United States in
July 2020.
▪ The U.S. Food and Drug Administration (FDA) approved remimazolam
based on evidence from three clinical trials .
▪ remimazolam metabolism: the parent drug remimazolam is hydrolyzed
by carboxylesterase 1 to the inactive metabolite
Remimazolam:
remimazolam
midazolam