Sympathomimetics Classification and SAR.ppt
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This document discusses the classification, structure-activity relationships, and mechanisms of action of sympathomimetic and adrenergic drugs. It categorizes these drugs based on their chemical nature, mode of action, receptor selectivity, and therapeutic effects. Key points include: 1) Sympathomimetics are classified as catecholamines which contain a catechol nucleus, or non-catecholamines which do not. 2) They can act directly on receptors, indirectly by releasing norepinephrine, or by both mechanisms. 3) Drugs show selectivity for alpha-1, alpha-2, beta-1, or beta-2 adrenergic receptors. 4) Ther
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Agonists at adrenergic receptors are either direct-acting or indirect-acting. Catecholamines, norepinephrine, and epinephrine are direct-acting and nonselective adrenergic agonists. Indirect-acting agonists cause the release of the neurotransmitter norepinephrine from sympathetic nerve terminal
Barbiturates
Sedatives and hypnotics work by calming agitation, inducing sleep, and reducing anxiety. Barbiturates are central nervous system depressants that produce their effects by potentiating the inhibitory neurotransmitter GABA. Their mechanism of action, uses, synthesis, and structure-activity relationships are described. While formerly widely used, barbiturates have largely been replaced by benzodiazepines due to risks of addiction and tolerance. Other sedative-hypnotics discussed include paraldehyde, chloral hydrate, alcohols, ethchlorvynol, and glutarimide derivatives.
Sympathomimetics or Adrenergic Agonists (Introduction, Classification, Adenor...
Sympathomimetics or adrenergic agonists (introduction, classification, adenoreceptors, neurtransmission, direct acting, indirect acting, mixed action agonists, summary)
Drugs that partially or completely mimic the effects of transmitter substances of the sympathetic nervous system. On the basis of chemical structure we divide Sympathomimetics into
1. Catecholamine
2. Non-Catecholamine
Adrenergic drugs that activate adrenergic receptors are termed
as sympathomimetics, Some sympathomimetics directly activate
adrenergic receptors (direct-acting agonists), while others act
indirectly by enhancing release or blocking reuptake of norepinephrine (indirect-acting agonists). Adrenergic transmission is restricted to the sympathetic division of the ANS. There are three closely related endogenous catecholamine's (CAs).
1. Noradrenaline (NA): It acts as transmitter at postganglionic sympathetic sites (except sweat glands, hair follicles and some vasodilator fibers) and in certain areas of brain.
2. Adrenaline (Adr) It is secreted by adrenal medulla and may have a transmitter role in the brain.
3. Dopamine (DA) It is a major transmitter in basal ganglia, limbic system, CTZ, anterior pituitary, etc. and in a limited manner in the periphery
Mechanism of Action , Therapeutic uses and adverse effects of Adrenergic Agonists
1. Direct-acting agonists:
These drugs act directly on α or β receptors, producing effects similar to those that occur following stimulation of sympathetic nerves or release of epinephrine from the adrenal medulla.
Examples of direct-acting agonists include epinephrine,
norepinephrine, isoproterenol, and phenylephrine.
2. Indirect-acting agonists:
These agents may block the reuptake of norepinephrine or cause the release of norepinephrine from the cytoplasmic pools or vesicles of adrenergic neuron. The norepinephrine then traverses the synapse and binds to α or β receptors.
Examples of reuptake inhibitors and agents that cause norepinephrine release include cocaine and amphetamines,
respectively.
3. Mixed-action agonists:
Ephedrine and its stereoisomer, pseudoephedrine, both stimulate adrenoceptors directly and release norepinephrine
from the adrenergic neuron.
Adrenergic agents lady ann
The document discusses the biosynthesis, mechanisms of action, receptors, and pharmacological properties of catecholamines and various adrenergic drugs. It describes the steps involved in catecholamine biosynthesis, the types of adrenergic receptors (alpha and beta), and the functions of endogenous catecholamines like epinephrine, norepinephrine, and dopamine. It also provides details on various adrenergic drugs including agonists, antagonists, inhibitors of biosynthesis, depleters of neurotransmitters, and their uses and mechanisms of action.
Protein metabolism
1. Protein metabolism involves the breakdown of amino acids into ammonia and carbon skeletons, and the reuse of these components for new protein synthesis or energy production. Amino acids undergo transamination, deamination, and are metabolized through the urea cycle to dispose of ammonia.
2. The urea cycle is a series of chemical reactions that converts ammonia into urea for excretion. It occurs primarily in the liver and involves five enzymatic steps to incorporate ammonia and carbon into the relatively non-toxic urea molecule.
3. Defects in protein metabolism can cause inborn errors such as phenylketonuria, maple syrup urine disease, and defects in the urea cycle, which
Systemic Pharmacology Of Autonomic Nervous System. Sympathomimetics Agents
Dive into the Intriguing World of Sympathomimetics! Unravel the secrets of Systemic Pharmacology in our exploration of the Autonomic Nervous System. Join us on a journey through the dynamic realm of Sympathomimetic Agents, where science meets adrenaline. From their roles in medicine to the intricacies of their impact, this presentation is your gateway to understanding the pharmacological dance within the Autonomic Nervous System. #Pharmacology #AutonomicNervousSystem #Sympathomimetics
Characteristics and Properties of Amino Acids (AA)
Amino acids have several key properties:
1. They are amphoteric, taking on positive, negative, or neutral charges depending on pH. Their isoelectric point is when the net charge is neutral.
2. They have acidic and basic groups that allow them to undergo various chemical reactions like esterification, acylation, and reactions with carbonyl compounds.
3. When heated to high temperatures during cooking, amino acids can form mutagenic and potentially toxic compounds like acrylamide or heterocyclic amines. The Maillard reaction and Strecker degradation play important roles in these processes.
classification adrenergic.pdf of automatic nervous system
This document classifies sympathomimetic drugs according to their:
1. Chemical structure as catecholamines or non-catecholamines
2. Mode of action as direct acting, indirect acting, or mixed acting
3. Duration of action as short, intermediate, or long acting
Some examples of classifications include epinephrine as a catecholamine, direct acting, and short acting drug and amphetamine as a non-catecholamine, indirect acting, and long acting drug. The document also discusses classification by receptor selectivity and therapeutic use.
ANTI-HYPERTENSIVE%20DRUGS%20123.pptx
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Adrenergic Drugs II
This document summarizes the actions and clinical applications of major adrenergic drugs, including:
1) Sympathomimetics like amphetamine and ephedrine act indirectly by releasing catecholamines from neurons, while direct-acting drugs interact directly with adrenoceptors.
2) Sympatholytics include direct-acting antagonists that block adrenoceptors and indirect-acting drugs that interfere with norepinephrine release or synthesis.
3) Adrenergic drugs have applications for conditions like hypotension, shock, asthma, and hypertension. Common side effects include hypotension, tachycardia, and sedation.
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This ppt contains the description about opoidal analgesic drugs with their Receptors, MOA and Chemical Classification.
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- 2. ACCORDING TO CHEMICAL NATURE Catecholamines: possess catechol nucleus e.g. Adrenaline, Nor-Adr, Dopamine Non-catecholamines: no catechol nucleus e.g. Ephedrine, Metaraminol
- 3. ACCORDING TO MODE OF ACTION Direct acting: Act directly on receptors. E.g. Adr, Nor-Adr, Isoprenaline and Salbutamol Indirect acting: Act on adrenergic neurons to release Nor-Adr. E.g. Tyramine, Amphetamine. Mixed acting: Can act in both ways. E.g. Ephedrine
- 4. ACCORDING TO RECEPTOR SELECTIVITY α1 selective: Phenyl ephrine α2 selective: Clonidine Both α1 and α2 selective: Adr and Nor Adr
- 5. β1 selective: Dobutamine β2 selective: Salbutamol Both β1 and β2 selective: Adr, Nor Adr, Isoproterenol
- 6. ACCORDING TO THERAPEUTIC EFFECT Vasoconstrictor: Adr, Nor-Adr, Ephedrine, Phenylephrine Bronchodilator: Salbutamol, Terbutaline, Isoprenaline Cardiac stimulant: Adr, Isoprenaline CNS stimulant: Amphetamine, Methamphetamine Nasal decongestant: Ephedrine, Naphazoline, Oxymetazoline, Xylometazoline Anorectics- Fenfluramine, Sibutramine (But banned due to serious side effects like heart attack)
- 7. ADRENORECEPTORS G-protein coupled receptor. Located throughout the body on neuronal and non- neuronal tissues. 2 types- α and β receptors α receptor is further of 2 subtypes – α1 and α2 β receptor is further of 3 subtypes –β1, β2 and β3
- 8. ADRENORECEPTOR, DISTRIBUTION, ACTION Receptor Location Action Use Agonist Antagonis t α1 Blood vessels Contraction Hypotension, Shock Phenylephrin e Prazosin (Antihypert ensive) Eye Dilation Mydriatics Mucus memb Vasoconstriction Nasal decongestant Prostate gland Contraction α2 CNS Decrease neurotransmitter release Antihypertens ive Clonidine (Antihyperten sive) Yohimbine Pancreatic cells Decrease insulin release
- 9. Receptor Location Action Use Agonist Antagonist β1 Heart muscle Muscle contraction Increase heart rate and force Dobutamine Metoprolol (Antihyperte nsive) Kidney Increase renin secretion Increase BP β2 Smooth muscle (Bronchus) Relaxation (Bronchodialation) Asthma and COPD Salbutamol Butoxamine β3 Adipose tissue Lipolysis BRL 37344
- 10. SAR OF SYMPATHOMIMETIC DRUGS Parent structure of most of adrenergic drugs is β-phenylethylamine. Modifications of β-phenylethylamine influence not only the mechanism of action, the receptor selectivity, but also their absorption, oral activity, metabolism, and thus duration of action (DOA). For the direct-acting sympathomimetic amines, maximal activity is seen in β-phenylethylamine derivatives containing (a) catechol (b) OH group on the ethylamine portion of the molecule.
- 11. High adrenergic activity occurs when two carbon atoms separate the aromatic ring from the amino group. Primary and secondary amines have good adrenergic activity, whereas tertiary amines and quaternary ammonium salts do not. The nature of the amino substituent also affects the receptor selectivity of the compound. As the size of the nitrogen substituent increases, α-receptor agonist activity generally decreases and β-receptor agonist activity increases. Substitution by small alkyl group at α- carbon (e.g., CH3- or C2H5-) slows metabolism by MAO. So, addition of small alkyl group increases the resistance to metabolism and lipophilicity, so such compounds often exhibit enhanced oral effectiveness and greater CNS activity than other compounds that do not contain an α-alkyl group. Substitution at β- C by OH greatly enhances agonist activity at both α- and β-receptors.
- 12. Compounds with 3,4-dihydroxy group in phenyl nucleus act as direct acting drugs whereas without catechol nucleus act as indirect acting drugs. Compounds without one or both phenolic OH substituents are not metabolized by COMT, and they are orally active and have longer duration of action.