Pooja drugs ppt
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this presentation is based on anticonvulsants which are used to cure or to control the disturbance created in brain by abnormal discharging of neurons which is termed as epilepsy.
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Neurotransmitters
Neurotransmitters are chemical messengers that transmit signals between neurons. There are four main neurotransmitter systems: monoamines like dopamine and serotonin which regulate movement, mood, and reward; acetylcholine which is involved in memory, attention, and muscle control; amino acids like glutamate and GABA which are excitatory or inhibitory; and neuropeptides which modulate various functions. Disorders like Parkinson's, Alzheimer's, epilepsy, depression, and others have been linked to imbalances in specific neurotransmitters.
Acetylcholine metabolism by Dr. Ashok Kumar J
The document discusses acetylcholine (ACh), a neurotransmitter that is secreted by neurons in the nervous system. ACh acts at neuromuscular junctions and is involved in functions like muscle contraction. It is broken down by the enzyme acetylcholinesterase. There are two main types of ACh receptors: nicotinic and muscarinic. Disorders like myasthenia gravis and glaucoma involve issues with ACh signaling. Inhibitors of acetylcholinesterase are used to treat conditions by prolonging the actions of ACh.
Acetylcholine
Acetylcholine is a neurotransmitter that functions in both the peripheral and central nervous systems. It is synthesized from choline and acetyl-CoA by the enzyme cholinesterase and is broken down by acetylcholinesterase. Acetylcholine is distributed throughout the body, including in muscles, nerves, the brain, and at neuromuscular junctions. It is stored in vesicles and released into the synaptic cleft upon arrival of an action potential.
Parasympathomimetic drugs
Parasympathomimetic or cholinergic drugs act on cholinergic receptors in the parasympathetic nervous system to produce effects similar to parasympathetic stimulation. They have two types of activities: muscarinic and nicotinic. Examples include direct-acting drugs like acetylcholine and indirect-acting anticholinesterases. Anticholinesterases inhibit the enzyme cholinesterase, leading to accumulation of acetylcholine at receptor sites. They are used to treat conditions like glaucoma, myasthenia gravis, Alzheimer's disease, and organophosphate poisoning.
Para sympathomimetics
Para-sympathomimetics can directly activate cholinergic receptors as agonists or indirectly increase acetylcholine levels by inhibiting acetylcholinesterase. Direct agonists include natural alkaloids like muscarine and synthetic ones like carbachol. Indirect anticholinesterases prevent acetylcholine degradation, either reversibly like neostigmine or irreversibly like organophosphates. Their effects are mediated through muscarinic and nicotinic receptors in the autonomic ganglia, neuromuscular junction and central nervous system. They have therapeutic uses for conditions like glaucoma and myasthenia gravis but overdose can cause toxic effects that require atropine and oxime
Skeletal muscle relaxants (or) Neuromuscular blockers
Skeletal muscle relaxants (or) Neuromuscular blockers
Classification and Mechanism of action of drugs.
Cholinergic drugs thea
This document discusses cholinergic drugs and related agents. It defines cholinergic drugs as those that mimic or block the action of acetylcholine. The document outlines the cholinergic system including acetylcholine as a neurotransmitter, cholinergic receptors (nicotinic and muscarinic), and receptor subtypes. It also discusses cholinergic agonists, antagonists, stereochemistry, and inhibitors of the acetylcholinesterase enzyme. Specific drugs are provided as examples within each category.
central nervous system
The central nervous system (CNS) is the part of the nervous system consisting of the brain and spinal cord. The CNS is so named because it integrates the received information and coordinates and influences the activity of all parts of the bodies of bilaterally symmetric animals
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Neurotransmitters
Neurotransmitters are chemical messengers that transmit signals between neurons. There are four main neurotransmitter systems: monoamines like dopamine and serotonin which regulate movement, mood, and reward; acetylcholine which is involved in memory, attention, and muscle control; amino acids like glutamate and GABA which are excitatory or inhibitory; and neuropeptides which modulate various functions. Disorders like Parkinson's, Alzheimer's, epilepsy, depression, and others have been linked to imbalances in specific neurotransmitters.
Acetylcholine metabolism by Dr. Ashok Kumar J
The document discusses acetylcholine (ACh), a neurotransmitter that is secreted by neurons in the nervous system. ACh acts at neuromuscular junctions and is involved in functions like muscle contraction. It is broken down by the enzyme acetylcholinesterase. There are two main types of ACh receptors: nicotinic and muscarinic. Disorders like myasthenia gravis and glaucoma involve issues with ACh signaling. Inhibitors of acetylcholinesterase are used to treat conditions by prolonging the actions of ACh.
Acetylcholine
Acetylcholine is a neurotransmitter that functions in both the peripheral and central nervous systems. It is synthesized from choline and acetyl-CoA by the enzyme cholinesterase and is broken down by acetylcholinesterase. Acetylcholine is distributed throughout the body, including in muscles, nerves, the brain, and at neuromuscular junctions. It is stored in vesicles and released into the synaptic cleft upon arrival of an action potential.
Parasympathomimetic drugs
Parasympathomimetic or cholinergic drugs act on cholinergic receptors in the parasympathetic nervous system to produce effects similar to parasympathetic stimulation. They have two types of activities: muscarinic and nicotinic. Examples include direct-acting drugs like acetylcholine and indirect-acting anticholinesterases. Anticholinesterases inhibit the enzyme cholinesterase, leading to accumulation of acetylcholine at receptor sites. They are used to treat conditions like glaucoma, myasthenia gravis, Alzheimer's disease, and organophosphate poisoning.
Para sympathomimetics
Para-sympathomimetics can directly activate cholinergic receptors as agonists or indirectly increase acetylcholine levels by inhibiting acetylcholinesterase. Direct agonists include natural alkaloids like muscarine and synthetic ones like carbachol. Indirect anticholinesterases prevent acetylcholine degradation, either reversibly like neostigmine or irreversibly like organophosphates. Their effects are mediated through muscarinic and nicotinic receptors in the autonomic ganglia, neuromuscular junction and central nervous system. They have therapeutic uses for conditions like glaucoma and myasthenia gravis but overdose can cause toxic effects that require atropine and oxime
Skeletal muscle relaxants (or) Neuromuscular blockers
Skeletal muscle relaxants (or) Neuromuscular blockers
Classification and Mechanism of action of drugs.
Cholinergic drugs thea
This document discusses cholinergic drugs and related agents. It defines cholinergic drugs as those that mimic or block the action of acetylcholine. The document outlines the cholinergic system including acetylcholine as a neurotransmitter, cholinergic receptors (nicotinic and muscarinic), and receptor subtypes. It also discusses cholinergic agonists, antagonists, stereochemistry, and inhibitors of the acetylcholinesterase enzyme. Specific drugs are provided as examples within each category.
central nervous system
The central nervous system (CNS) is the part of the nervous system consisting of the brain and spinal cord. The CNS is so named because it integrates the received information and coordinates and influences the activity of all parts of the bodies of bilaterally symmetric animals
Parasympathomimetcs ; Cholinomimetics , Parasympathomimetics ;Anti-Choliester...
Cholinomimetics , Parasympathomimetics ;Anti-Choliesterases ; Parasympatholytics,Cholinergic transmission.
General Anaesthetics
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.
Medicinal chemistry
This document contains 15 sections written by Mr. Manojkumar K. Munde on various topics related to pharmaceutical chemistry and medicinal chemistry. The sections discuss neurotransmitters like acetylcholine and catecholamines, the synthesis of drugs like diazepam and insulin, classes of receptors and drug-receptor interactions. Specific agents discussed include ganglion blockers, ACE inhibitors, beta blockers, antimigraine drugs, and anticonvulsants.
Skeletal muscle relaxant
Skeletal muscle relaxants can act peripherally at the neuromuscular junction, centrally in the central nervous system, or directly on muscle contractile mechanisms. Peripherally acting drugs include competitive blockers like tubocurarine and depolarizing agents like succinylcholine. Centrally acting drugs like diazepam and baclofen reduce muscle tone by depressing spinal reflexes. Dantrolene acts directly on muscle to inhibit calcium release and contraction. These drugs are used to reduce muscle spasms and tone in various neurological and orthopedic conditions as well as in anesthesia and electroconvulsive therapy.
Cholinergic ramesh
This document discusses cholinergic drugs, which act on the parasympathetic nervous system. It describes two main types: direct-acting cholinergics (acetylcholine and related agonists) and indirect-acting cholinergics (cholinesterase inhibitors). The direct-acting drugs include acetylcholine, pilocarpine, and muscarine. The indirect-acting drugs inhibit the enzyme acetylcholinesterase, increasing cholinergic activity. Examples given are physostigmine, neostigmine, pyridostigmine, and organophosphate nerve agents. The document outlines the mechanisms and uses of these drugs in conditions like glaucoma, myasthenia gravis,
Drugs acting on neuromuscular junnction and Muscle Relaxants
It covers all related info about drugs acting at NMJ and centrally as well as locally acting muscle relaxants.
Ajay
This document discusses convulsants and anticonvulsant medications. It begins by defining convulsions as a serious neurological disorder characterized by paroxysmal cerebral dysrhythmias and changes in sensation, stress, emotions and behavior that can cause muscle spasms, loss of consciousness and death if not treated. It then lists several common medications used to treat generalized convulsions such as phenytoin, mephobarbital, carbamazepine and valproic acid. Medications used for partial convulsions include ethosuximide and clonazepam. The document goes on to classify different types of anticonvulsant medications and discusses the structure-activity relationship of pheny
Parasympathomimetic agents
This document provides an overview of parasympathomimetic agents or cholinergic drugs. It discusses the organization of the nervous system and types of cholinergic receptors. Cholinergic drugs are classified as directly acting or indirectly acting. Directly acting drugs like choline esters and pilocarpine directly bind to muscarinic and nicotinic receptors. Indirectly acting drugs like physostigmine and neostigmine inhibit acetylcholinesterase and prolong the action of acetylcholine. These drugs have therapeutic uses in conditions like myasthenia gravis and glaucoma. Organophosphate poisoning is also discussed which occurs due to inhibition of acetylcholinesterase.
Actylcholine part 2
Cholinergic drugs, inhibit, enhance, or mimic the action of the neurotransmitter acetylcholine, the primary transmitter of nerve impulses within the parasympathetic nervous system
Pharmacology parasympathetic nervous system- in brief
The parasympathetic nervous system functions to conserve energy and promote rest. It decreases heart rate and promotes secretions from glands. Acetylcholine is the primary neurotransmitter and binds to nicotinic receptors in the autonomic ganglia and muscarinic receptors in effector tissues. Parasympathetic stimulation contracts the iris sphincter muscle to accommodate vision.
Parasympathomimetics (Cholinergic drugs)
The document discusses the parasympathetic nervous system and parasympathomimetic drugs. It provides details on:
- The parasympathetic nervous system originates from the brainstem and sacral region and uses acetylcholine as a neurotransmitter.
- Parasympathomimetic drugs like acetylcholine, muscarine, and anticholinesterases act to stimulate parasympathetic responses. Direct acting drugs activate cholinergic receptors while indirect drugs inhibit acetylcholinesterase.
- These drugs have therapeutic uses for conditions like glaucoma, urinary retention, and myasthenia gravis. Combinations of drugs are sometimes used to achieve optimal effects while minimizing side effects.
Local anaesthetics
Local anaesthetics reversibly block nerve impulse conduction. They provide temporary loss of sensation in a localized area without loss of consciousness. Local anaesthetics are classified as injectable or surface anaesthetics. The mechanism of action involves blocking voltage-gated sodium channels, inhibiting the influx of sodium and preventing the generation of action potentials. Individual local anaesthetics vary in potency, duration of action, metabolism and excretion. Commonly used local anaesthetics include lidocaine, bupivacaine and cocaine.
Mechanism of general anaesthesia at molecular level.
This document discusses the mechanism of general anesthesia at the molecular level. It begins by introducing general anesthetics and their historical use. While anesthetics have been used for over 160 years, their exact mechanism of action is still unknown. The document then examines various theories for how anesthetics act, including affecting ion channels such as GABA, glutamate, and calcium channels. It also discusses the Meyer-Overton hypothesis that anesthetic potency correlates with lipid solubility. While research continues, no single theory can fully explain anesthesia and its effects are thought to involve multiple molecular targets in the brain and nervous system.
Cholinergic receptors,funtion and its clinical application
This document discusses the history and functions of acetylcholine and cholinergic receptors. It begins with the 1936 Nobel Prize-winning discovery of acetylcholine as a neurotransmitter by Dale and Loewi. It describes the two main cholinergic receptor classes - muscarinic and nicotinic - and provides details on cholinergic drugs that act as agonists or antagonists at these receptors. These include parasympathomimetic and anticholinergic drugs used to treat various conditions like asthma, glaucoma, peptic ulcers, and Parkinson's disease. The document also discusses organophosphate poisoning and nerve agents that act by inhibiting acetylcholinesterase.
Adrenergic antagonists
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
THEORIES OF GENERAL ANAESTHESIA
This document discusses theories of general anesthesia. It begins by introducing general anesthesia and its uses. It then classifies theories into three main categories: lipid theory, protein theory, and biochemical theory. The lipid theory section describes several specific lipid theories, including the Mayer and Overton theory, Pauling and Miller hydrate theory, membrane expansion theory, and membrane fluidization theory. The protein theory suggests anesthetics act on membrane proteins. The biochemical theory notes theories involving inhibition of glucose metabolism and interference with cellular respiration. In closing, it lists references used.
Autonomic nervous system and cholinomimetics
It deals with the basics of autonomic nervous system and cholinergic drugs / cholinomimetics / parasympathomimetic drugs
parasympathomimetic drugs or agents
This document discusses parasympathomimetic drugs, which mimic the effects of the parasympathetic nervous system. It describes how these drugs activate parasympathetic receptors, especially muscarinic and nicotinic acetylcholine receptors. It provides details on the mechanisms of different parasympathomimetic drugs, including how they stimulate receptors to produce various effects in the body. Specific drugs discussed include acetylcholine, carbachol, and their therapeutic uses and side effects.
SAR and Synthesis of adrenergic blockers
This document discusses drugs that act on the autonomic nervous system, specifically adrenergic antagonists and beta blockers. It provides information about Propranolol and Tolazoline, including their uses and syntheses. It also summarizes the structure-activity relationships of beta blockers, noting that most are aryloxypropanolamines, the S-configuration of the hydroxyl group is important for receptor affinity, and lipophilicity affects central nervous system effects.
Anti convulsant drugs
Anticonvulsant drugs, also known as antiepileptic drugs, are used to control seizures and epilepsy. The document discusses various types of anticonvulsant drugs including barbiturates, hydantoins, oxazolidinediones, succinimides, benzodiazepines, and miscellaneous drugs. It provides details on the classification, mechanism of action, structural activity relationships, synthesis, uses, and adverse effects of these anticonvulsant drugs. The main mechanisms of action include enhancement of GABA action, inhibition of sodium channels, and inhibition of calcium channels. Phenobarbital, phenytoin, carbamazepine, and valproic acid are some of the
02.Anticonvulsant and H1 and H2 receptor antagonist.pptx
1) The document discusses anti-convulsant drugs and H1 and H2 receptor antagonists. It defines epilepsy and seizures, describes types of seizures and anti-convulsant drugs.
2) It also discusses the mechanisms of action of barbiturates, benzodiazepines, and gabapentin as anti-convulsants.
3) For H1 and H2 receptor antagonists, it describes histamine receptors and classifications of H1 and H2 receptor antagonists. It covers the mechanisms of action and structure-activity relationships of these drugs.
Anticonvulsant ppt.pptx
This document discusses anticonvulsant drugs, which are used to treat epilepsy and seizures. It describes the types of epilepsy including partial and generalized seizures. The major classes of anticonvulsant drugs are then outlined - barbiturates, hydantoin derivatives, oxazolidinediones, succinimides, benzodiazepines, and GABA analogues. The mechanisms of action are explained for each class, such as potentiation of GABA receptors or blocking voltage-gated calcium channels. Examples are given of specific drugs from each class along with their chemical structures. The structure-activity relationships are also summarized for some classes.
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General Anaesthetics
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.
Medicinal chemistry
This document contains 15 sections written by Mr. Manojkumar K. Munde on various topics related to pharmaceutical chemistry and medicinal chemistry. The sections discuss neurotransmitters like acetylcholine and catecholamines, the synthesis of drugs like diazepam and insulin, classes of receptors and drug-receptor interactions. Specific agents discussed include ganglion blockers, ACE inhibitors, beta blockers, antimigraine drugs, and anticonvulsants.
Skeletal muscle relaxant
Skeletal muscle relaxants can act peripherally at the neuromuscular junction, centrally in the central nervous system, or directly on muscle contractile mechanisms. Peripherally acting drugs include competitive blockers like tubocurarine and depolarizing agents like succinylcholine. Centrally acting drugs like diazepam and baclofen reduce muscle tone by depressing spinal reflexes. Dantrolene acts directly on muscle to inhibit calcium release and contraction. These drugs are used to reduce muscle spasms and tone in various neurological and orthopedic conditions as well as in anesthesia and electroconvulsive therapy.
Cholinergic ramesh
This document discusses cholinergic drugs, which act on the parasympathetic nervous system. It describes two main types: direct-acting cholinergics (acetylcholine and related agonists) and indirect-acting cholinergics (cholinesterase inhibitors). The direct-acting drugs include acetylcholine, pilocarpine, and muscarine. The indirect-acting drugs inhibit the enzyme acetylcholinesterase, increasing cholinergic activity. Examples given are physostigmine, neostigmine, pyridostigmine, and organophosphate nerve agents. The document outlines the mechanisms and uses of these drugs in conditions like glaucoma, myasthenia gravis,
Drugs acting on neuromuscular junnction and Muscle Relaxants
It covers all related info about drugs acting at NMJ and centrally as well as locally acting muscle relaxants.
Ajay
This document discusses convulsants and anticonvulsant medications. It begins by defining convulsions as a serious neurological disorder characterized by paroxysmal cerebral dysrhythmias and changes in sensation, stress, emotions and behavior that can cause muscle spasms, loss of consciousness and death if not treated. It then lists several common medications used to treat generalized convulsions such as phenytoin, mephobarbital, carbamazepine and valproic acid. Medications used for partial convulsions include ethosuximide and clonazepam. The document goes on to classify different types of anticonvulsant medications and discusses the structure-activity relationship of pheny
Parasympathomimetic agents
This document provides an overview of parasympathomimetic agents or cholinergic drugs. It discusses the organization of the nervous system and types of cholinergic receptors. Cholinergic drugs are classified as directly acting or indirectly acting. Directly acting drugs like choline esters and pilocarpine directly bind to muscarinic and nicotinic receptors. Indirectly acting drugs like physostigmine and neostigmine inhibit acetylcholinesterase and prolong the action of acetylcholine. These drugs have therapeutic uses in conditions like myasthenia gravis and glaucoma. Organophosphate poisoning is also discussed which occurs due to inhibition of acetylcholinesterase.
Actylcholine part 2
Cholinergic drugs, inhibit, enhance, or mimic the action of the neurotransmitter acetylcholine, the primary transmitter of nerve impulses within the parasympathetic nervous system
Pharmacology parasympathetic nervous system- in brief
The parasympathetic nervous system functions to conserve energy and promote rest. It decreases heart rate and promotes secretions from glands. Acetylcholine is the primary neurotransmitter and binds to nicotinic receptors in the autonomic ganglia and muscarinic receptors in effector tissues. Parasympathetic stimulation contracts the iris sphincter muscle to accommodate vision.
Parasympathomimetics (Cholinergic drugs)
The document discusses the parasympathetic nervous system and parasympathomimetic drugs. It provides details on:
- The parasympathetic nervous system originates from the brainstem and sacral region and uses acetylcholine as a neurotransmitter.
- Parasympathomimetic drugs like acetylcholine, muscarine, and anticholinesterases act to stimulate parasympathetic responses. Direct acting drugs activate cholinergic receptors while indirect drugs inhibit acetylcholinesterase.
- These drugs have therapeutic uses for conditions like glaucoma, urinary retention, and myasthenia gravis. Combinations of drugs are sometimes used to achieve optimal effects while minimizing side effects.
Local anaesthetics
Local anaesthetics reversibly block nerve impulse conduction. They provide temporary loss of sensation in a localized area without loss of consciousness. Local anaesthetics are classified as injectable or surface anaesthetics. The mechanism of action involves blocking voltage-gated sodium channels, inhibiting the influx of sodium and preventing the generation of action potentials. Individual local anaesthetics vary in potency, duration of action, metabolism and excretion. Commonly used local anaesthetics include lidocaine, bupivacaine and cocaine.
Mechanism of general anaesthesia at molecular level.
This document discusses the mechanism of general anesthesia at the molecular level. It begins by introducing general anesthetics and their historical use. While anesthetics have been used for over 160 years, their exact mechanism of action is still unknown. The document then examines various theories for how anesthetics act, including affecting ion channels such as GABA, glutamate, and calcium channels. It also discusses the Meyer-Overton hypothesis that anesthetic potency correlates with lipid solubility. While research continues, no single theory can fully explain anesthesia and its effects are thought to involve multiple molecular targets in the brain and nervous system.
Cholinergic receptors,funtion and its clinical application
This document discusses the history and functions of acetylcholine and cholinergic receptors. It begins with the 1936 Nobel Prize-winning discovery of acetylcholine as a neurotransmitter by Dale and Loewi. It describes the two main cholinergic receptor classes - muscarinic and nicotinic - and provides details on cholinergic drugs that act as agonists or antagonists at these receptors. These include parasympathomimetic and anticholinergic drugs used to treat various conditions like asthma, glaucoma, peptic ulcers, and Parkinson's disease. The document also discusses organophosphate poisoning and nerve agents that act by inhibiting acetylcholinesterase.
Adrenergic antagonists
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
THEORIES OF GENERAL ANAESTHESIA
This document discusses theories of general anesthesia. It begins by introducing general anesthesia and its uses. It then classifies theories into three main categories: lipid theory, protein theory, and biochemical theory. The lipid theory section describes several specific lipid theories, including the Mayer and Overton theory, Pauling and Miller hydrate theory, membrane expansion theory, and membrane fluidization theory. The protein theory suggests anesthetics act on membrane proteins. The biochemical theory notes theories involving inhibition of glucose metabolism and interference with cellular respiration. In closing, it lists references used.
Autonomic nervous system and cholinomimetics
It deals with the basics of autonomic nervous system and cholinergic drugs / cholinomimetics / parasympathomimetic drugs
parasympathomimetic drugs or agents
This document discusses parasympathomimetic drugs, which mimic the effects of the parasympathetic nervous system. It describes how these drugs activate parasympathetic receptors, especially muscarinic and nicotinic acetylcholine receptors. It provides details on the mechanisms of different parasympathomimetic drugs, including how they stimulate receptors to produce various effects in the body. Specific drugs discussed include acetylcholine, carbachol, and their therapeutic uses and side effects.
SAR and Synthesis of adrenergic blockers
This document discusses drugs that act on the autonomic nervous system, specifically adrenergic antagonists and beta blockers. It provides information about Propranolol and Tolazoline, including their uses and syntheses. It also summarizes the structure-activity relationships of beta blockers, noting that most are aryloxypropanolamines, the S-configuration of the hydroxyl group is important for receptor affinity, and lipophilicity affects central nervous system effects.
Anti convulsant drugs
Anticonvulsant drugs, also known as antiepileptic drugs, are used to control seizures and epilepsy. The document discusses various types of anticonvulsant drugs including barbiturates, hydantoins, oxazolidinediones, succinimides, benzodiazepines, and miscellaneous drugs. It provides details on the classification, mechanism of action, structural activity relationships, synthesis, uses, and adverse effects of these anticonvulsant drugs. The main mechanisms of action include enhancement of GABA action, inhibition of sodium channels, and inhibition of calcium channels. Phenobarbital, phenytoin, carbamazepine, and valproic acid are some of the
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Pooja drugs ppt
- 1. CHEMISTRY OF SYNTHETIC DRUGS POOJA CHAUHAN B.SC CHEMISTRY 2015017009
- 2. EPILEPSY AND ITS TREATEMENT SEIZURE- Seizure is a sudden discharge, sudden attack or sudden symptoms which could be due to outburst of abnormal synchronous discharging caused by a network of neurons. Electrical discharge of neurons which may results into the type of attacks or fits.
- 3. EPILEPSY Two or more seizures occurring at intervals of 24 hours apart is termed to be epilepsy. It can result into lack or awareness or unconsciousness, major convulsions. Types of epilepsy: there are two types of epilepsy a) Grand mal epilepsy – it is the type of epilepsy in which a patient leads to complete unconsciousness stage. b) Petit mal epilepsy- it is the type of epilepsy in which only a part of body or organ is affected.
- 4. CURE: DRUGS used to cure epilepsy are called as anticonvulsants. Anticonvulsants are basically the drugs that are used for controlling and managing CNS disorders characterised by transient attacks of disturbed brain function. These drug basically having ureide structure (UREA like structure)
- 5. TYPES OF CONVULSANTS: BARBITURATES having cyclic ureides structure. MODE OF ACTION: They impair the synaptic transmission and cause a distinct enhancement of GABA ergic inhibitory response. Barbiturates acts on the picrotoxin unit of GABA.(Y- amino butyric acid) eg. Barbital , phenobarbital.
- 6. a) Barbital b) phenobarbital Powerful hypnotic drug > it is used for both sedative and hypnosis. Therapeutic index is low >On metabolism it changes into para hydroxyl phenLy derivative (65%) and rest (35%) exerted as such.
- 7. SAR OF BARBITEURATES The number of carbon atoms in the side change should be between 4 to 10 for optimal therapeutic results. One of the substituents at the side chain may be a close chain. Inclusion of halogen atom in the side alkyl chain enhances the activity. Inclusion of polar groups like hydroxyl, carbonyl, carboxylic ,amino and sulphonic in the side chain reduces potency considerably. Replacement of c=o group by c=s shows rapid action of drug but for short duration. Inclusion for more sulphur atom decreases the activity. Stereoisomers have more and same potencies. Aromatic and alicyclic moieties exerts greater potency than corresponding aliphatic moiety having same number of carbon atoms.
- 8. HYDANTOINS Phenytoin sodium >mephenytoin Dosage: 50 to 100 mg can give per day. it exerts its action on motor cortex where it stabilises neuronal membrane and thereby inhibits the spread of seizure discharge.
- 9. OXAZOLIDINEDIONES A) trimethadione. B) paramethadione It is used in grand mal epilepsy and petit mal epilepsy. It is useful when given in conjunction with phenytoin sodium or phenobarbital. It is metabolised by conversion to N-dimethylated compound which is more soluble and in excreted as such without further degration.
- 10. SUCCINIMIDES A) phensuximide b) methsuximide • Used in petit mal epilepsy >used for curing petit mal epilepsy. >more effective than phensuxinimide.
- 12. CHEMOTHERAPY OF EPILEPSY it is very old disease and 1850s inorganic bromides were used for treating epilepsy. In 1920s phenobarbital gave a meaningful treatment to epilepsy and again after 20 years 5 substituted hydantoins was found to substituted. Salient structural features of anticonvulsants include the following: a) Uriede type moiety structural variants. b) Hydantoins having imidazole. 2-4 moieties moiety c) Bezodiazepams having epoxide ring at c10-c11 position gives rise to active metabolite.