Adrenergic drugs act on the sympathetic nervous system by mimicking neurotransmitters like epinephrine and norepinephrine. They can be classified as direct-acting, indirect-acting, or mixed-acting. Direct-acting drugs like dopamine directly stimulate adrenergic receptors. Indirect-acting drugs like pseudoephedrine stimulate the release of neurotransmitters. Mixed-acting drugs like ephedrine have both direct and indirect effects. These drugs are used to treat conditions like asthma, hypertension, shock, and congestion by increasing heart rate, relaxing bronchial muscles, and constricting blood vessels.
A condition in which the heart is unable to pump sufficient blood
to meet the metabolic demand of the body and also unable to receive it back because every time after a systole.
A condition in which the heart is unable to pump sufficient blood
to meet the metabolic demand of the body and also unable to receive it back because every time after a systole.
Introduction.
Classification .
Drugs used in Coagulant and Anticoagulant Agents
Mechanism of action .
Structure
Synthesis
Adverse Drug Reactions .
Uses.
Reference
Neurohumoral transmission in CNS-
The term neurohumoral transmission designates the transfer of a nerve impulse from a presynaptic to a postsynaptic neuron by means of a humoral agent e.g. a biogenic amine, an amino acid or a peptide.
Introduction of Steroids
Nomenclature
Sex Hormones
Biosynthesis of sex hormones
Structure, synthesis of Testosterone, Oestriol, Oestradiol, Diethyl stilbestrol, Progesterone
Reference
Parasympatholytics are the drugs that block or inhibit the actions of acetylcholine at postganglionic nerve endings and cholinergic receptors. They are also referred to as anticholinergics or cholinergic blocking agents or antispasmodics.
Anticholinergic drugs include atropine and related drugs- atropine is the prototype. Atropine is obtained from the plant Atropa belladonna. Atropine and scopolamine (hyoscine) are the belladonna alkaloids. They compete with acetylcholine for muscarinic receptors and block this receptors-they are muscarinic antagonists.
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.
Histamine is a biogenic amine present in many animal and plant tissues that function as neurotransmitters and are also found in non-neural tissues, have complex physiologic and pathologic effects through multiple receptor subtypes, and are often released locally.
It is also present in venoms and stinging secretions. It is synthesized by decarboxylation of the amino acid, histidine. Histamine is mainly present in storage granules of mast cells in tissues like skin, lungs, liver, gastric mucosa, placenta, etc. It is one of the mediators involved in inflammatory and hypersensitivity reactions.
The medicinal chemistry aspect of Adrenergic (Sympathetic) Nervous System and drugs (Sympathomimetics & sympatholytics) are briefly explained in these slides.
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.
Introduction.
Classification .
Drugs used in Coagulant and Anticoagulant Agents
Mechanism of action .
Structure
Synthesis
Adverse Drug Reactions .
Uses.
Reference
Neurohumoral transmission in CNS-
The term neurohumoral transmission designates the transfer of a nerve impulse from a presynaptic to a postsynaptic neuron by means of a humoral agent e.g. a biogenic amine, an amino acid or a peptide.
Introduction of Steroids
Nomenclature
Sex Hormones
Biosynthesis of sex hormones
Structure, synthesis of Testosterone, Oestriol, Oestradiol, Diethyl stilbestrol, Progesterone
Reference
Parasympatholytics are the drugs that block or inhibit the actions of acetylcholine at postganglionic nerve endings and cholinergic receptors. They are also referred to as anticholinergics or cholinergic blocking agents or antispasmodics.
Anticholinergic drugs include atropine and related drugs- atropine is the prototype. Atropine is obtained from the plant Atropa belladonna. Atropine and scopolamine (hyoscine) are the belladonna alkaloids. They compete with acetylcholine for muscarinic receptors and block this receptors-they are muscarinic antagonists.
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.
Histamine is a biogenic amine present in many animal and plant tissues that function as neurotransmitters and are also found in non-neural tissues, have complex physiologic and pathologic effects through multiple receptor subtypes, and are often released locally.
It is also present in venoms and stinging secretions. It is synthesized by decarboxylation of the amino acid, histidine. Histamine is mainly present in storage granules of mast cells in tissues like skin, lungs, liver, gastric mucosa, placenta, etc. It is one of the mediators involved in inflammatory and hypersensitivity reactions.
The medicinal chemistry aspect of Adrenergic (Sympathetic) Nervous System and drugs (Sympathomimetics & sympatholytics) are briefly explained in these slides.
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.
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
The French Revolution, which began in 1789, was a period of radical social and political upheaval in France. It marked the decline of absolute monarchies, the rise of secular and democratic republics, and the eventual rise of Napoleon Bonaparte. This revolutionary period is crucial in understanding the transition from feudalism to modernity in Europe.
For more information, visit-www.vavaclasses.com
Francesca Gottschalk - How can education support child empowerment.pptxEduSkills OECD
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Macroeconomics- Movie Location
This will be used as part of your Personal Professional Portfolio once graded.
Objective:
Prepare a presentation or a paper using research, basic comparative analysis, data organization and application of economic information. You will make an informed assessment of an economic climate outside of the United States to accomplish an entertainment industry objective.
Honest Reviews of Tim Han LMA Course Program.pptxtimhan337
Personal development courses are widely available today, with each one promising life-changing outcomes. Tim Han’s Life Mastery Achievers (LMA) Course has drawn a lot of interest. In addition to offering my frank assessment of Success Insider’s LMA Course, this piece examines the course’s effects via a variety of Tim Han LMA course reviews and Success Insider comments.
Acetabularia Information For Class 9 .docxvaibhavrinwa19
Acetabularia acetabulum is a single-celled green alga that in its vegetative state is morphologically differentiated into a basal rhizoid and an axially elongated stalk, which bears whorls of branching hairs. The single diploid nucleus resides in the rhizoid.
Read| The latest issue of The Challenger is here! We are thrilled to announce that our school paper has qualified for the NATIONAL SCHOOLS PRESS CONFERENCE (NSPC) 2024. Thank you for your unwavering support and trust. Dive into the stories that made us stand out!
Synthetic Fiber Construction in lab .pptxPavel ( NSTU)
Synthetic fiber production is a fascinating and complex field that blends chemistry, engineering, and environmental science. By understanding these aspects, students can gain a comprehensive view of synthetic fiber production, its impact on society and the environment, and the potential for future innovations. Synthetic fibers play a crucial role in modern society, impacting various aspects of daily life, industry, and the environment. ynthetic fibers are integral to modern life, offering a range of benefits from cost-effectiveness and versatility to innovative applications and performance characteristics. While they pose environmental challenges, ongoing research and development aim to create more sustainable and eco-friendly alternatives. Understanding the importance of synthetic fibers helps in appreciating their role in the economy, industry, and daily life, while also emphasizing the need for sustainable practices and innovation.
Embracing GenAI - A Strategic ImperativePeter Windle
Artificial Intelligence (AI) technologies such as Generative AI, Image Generators and Large Language Models have had a dramatic impact on teaching, learning and assessment over the past 18 months. The most immediate threat AI posed was to Academic Integrity with Higher Education Institutes (HEIs) focusing their efforts on combating the use of GenAI in assessment. Guidelines were developed for staff and students, policies put in place too. Innovative educators have forged paths in the use of Generative AI for teaching, learning and assessments leading to pockets of transformation springing up across HEIs, often with little or no top-down guidance, support or direction.
This Gasta posits a strategic approach to integrating AI into HEIs to prepare staff, students and the curriculum for an evolving world and workplace. We will highlight the advantages of working with these technologies beyond the realm of teaching, learning and assessment by considering prompt engineering skills, industry impact, curriculum changes, and the need for staff upskilling. In contrast, not engaging strategically with Generative AI poses risks, including falling behind peers, missed opportunities and failing to ensure our graduates remain employable. The rapid evolution of AI technologies necessitates a proactive and strategic approach if we are to remain relevant.
2. Adrenergic Drug :
Adrenergic drugs are the agents which acts directly on the
Symphathetic nervous system and these drugs are also known as
symphatomimetic drugs as these agents mimics (copy) the action of
symphathetic nervous system.
On stimulation of symphathetic nervous system following response
are produced :
1. Cardiac stimulation results in increase in heart rate and force of
contraction
2. Stimulation of CNS
3. Relaxation of bronchial muscle
4. Increase in rate of glycogenolysis
5. Liberation of free fatty acids
3. Neurotransmitters-
Epinephrine(Adrenaline), Norepinephrine ( Noradrenaline) and
Dopamine are the naturally occurring Catecholamines and controla
various response of “ Fight, Fiight, Fear” System
Biosynthesis of neurotransmitter ( Catecholamines)
The biosynthesis take place in adrenergic and Dopaminergic neurons in
the CNS, in symphathetic neurons in the ANS and in the adrenal medulla.
Various enzymes which are responsible for biosynthesis are:
1. Tyrosine Hydroxylase ( tyrosine-3-monooxygenase)
2. DOPA Decarboxylase
3. Dopamine- Beta-hydroxylase
4. Phenylethanolamine-N-methyl transfer
6. SAR of adrenergic drug
1. Symathomimatic drug are considered as derivative of beta
– Phenylethylamine. Structurally, Substitution is possible on
-Substitution on Aromatic ring of Phenylethylamine
- substitution on beta –Carbon
- substitution on alpha- carbon
- substitution on the amino group
7. A. Substitution on the aromatic Ring of Beta-phenylethylamine
1. The presence of –OH group in the benzene ring at 3 and 4 positions
givves maximum alpha and beta activity. If –OH group is absent overall
potency get decreased. For example, Phenylephrine is less potent than
Adrenaline
8. 2. The presence of – OH group at 3 and 5 position with bulky Substituents on
the amino nitrogen gives beta2 selective drug.
For example, Orciprenaline and Terbutaline relaxes bronchial muscle without
effecting cardiac muscle.
3. The Unsubstituted or alkyl substituted Adrenergic amines easily cross the
BBB and have more CNS activity. For ex. Amphetamine & Ephedrine
9. B. Substitution on the beta- carbon
A – OH group on the beat carbon decrease the central stimulant action
due to lower lipid solubility of the drug ( OH give polar effect) This increase
agonist activity of the drug at alpha and beta receptor. For ex. Ephedrine
has less central stimulant effe than amphetamine but more bronchial Dilating
effect
10. C. Substitution on the alpha- carbon
Drug having Substituents on the alpha- carbon block the metabolism
and these have longer duration of action. For ex. Amphetamine resists
degradation by MOA.
D. Substitution on the amino group
1. Lesser the substitution on the amino group, higher wiill be selectivity for
alpha- receptor.
2. More the size of alkyl Substituent, higher will be beta 2 -selective action.
For ex . Isoprenaline, Turbutaline and Salbutamol have selective Beta 2
activity
12. Direct acting Drugs 💊💉
These agents produce a Symphathetic response by
interacting directly with Adrenergic receptors The action
produced are of rapid onset and of short duration. This
drugs effect both alpha & beta receptor.
13. 1. Norepinephrine
IUPAC name: R -2-Amino-1-(3, 4-dihydroxyphenyl) -2-methylaminoethanol
MOA : It is potent agonist at alpha receptor and no effect on beta
receptor.
Uses: 1. it is used to reduced the absorption and effects of local
Anaesthetics
2. It decrease chance of hemorrhage during operation
3. It has strong Vasoconstriction property
14. 2. Epinephrine
IUPAC name : R - 1-(3, 4Dihydroxyphenyl) -2-methylaminoethanol
MOA:
Uses : 1. Vasoconstrictor
2. It is mainly used in treatment of anaphylaxis and anaphylactic
shock in the cardiopulmonary disease.
3. It is used in the management of glaucoma as it decreases
Intraocular pressure.
4. It relaxes bronchial muscle and is used in treatment of asthma.
15. 3. Phenylephrine
IUPAC name : ®-2-methylamino-1-(3-hydroxyphenyl) ethanol
Synthesis : it is prepared by reaction of m-chloroacetylphenol and Methylamine
followed by the reduction of the intermediate formed
MOA: activation of alpha-1 receptors causes Vasoconstriction of the Arterioles, iris,
and contraction of uterus.
Uses : 1. it is mainly used in decongestant in rhinitis and sinusitis.
2. Used in the eye for production Mydriasis when Cycloplegia is not required
16. 4. Dopamine
IUPAC name: 4-(2-aminoethyl)-1, 2-diol
MOA: it interacts directly on beta- adrenergic receptors ( agonist at beta
receptor) and indirectly on alpha –adrenergic receptors.
uses : 1. Dopamine is used in patient of shock
2. Used in server CHF where increase BP and urine output.
3. It is used in myocardial infraction, trauma, septic shock and cardiac
surgery.
17. 5. Methyldopa
IUPAC name : 3-(3, 4-dihydroxyphenyl-2-methyl-L-alanine
MOA : it’s competitive inhibitor of enzyme DOPA Decarboxylase which
results lower BP and CNS effect
Uses: 1. used in treatment of hypertension in combination with a diuretics
2. It’s prefered in Gestational hypertension by given orally.
18. 6. Salbutamol
IUPAC name : (2-butylamino-1[hydroxymethyl-4-hydroxy) phenyl]
MOA: It is strong beta-2 adrenergic agonist. It’s directly acting on
symathomimatic drug having strong action on beta- 2 receptors.
Synthesis :salbutamol is prepared from 4,3-dihydroxy methyl Benzaldehyde
which is acetylated and kept for 10 days in ether with cyanide and acetic
acid.
Uses: used in treatment of bronchitis and obstructive pulmonary disease
19. 7. Clonidine
IUPAC name : 2-[(2, 6-Dichlorophenyl)amino]-2-imidazoline
MOA : it’s centrally acting alpha alpha-2 receptor agonist leading to
reduction in sympathetic outflow from CNS
Uses: 1. Clonidine has mild sedative action
2. used in treatment of Tourette syndrome ( Neuropsychiatric
disorder With onset of childhood ) And ADHD
3. Clonidine may be used to ease withdrawal symptoms associated
with long term use of alcohol, narcotics, nicotine ( smoking)
20. 8. Dobutamine:
IUPAC name: 4-(2-[4-(4-hydroxyphenyl) butane-2-yl] amino)ethyl)
benzene 1,2- diol
MOA: it directly stimulate beta- 1 receptor Sympathetic nervous system and
alpha-1 receptor.
Uses : 1. used in treatment of of CHF because of positive inotropic effect
21. 9. Terbutaline
IUPAC name : ( 2- t-butylamino-1-[3, 5-dihydroxyphenyl] ethanol-1-ol)
MOA : it’s a selective beta-2 agonist
Uses : 1. It is very effective as Bronchodilator and is used in treatment of
asthma.
2. Used to arrest premature labour.
23. 1. Hydroxyamphetamine
IUPAC name : 4-hydroxy-alpha-Methylphenethylamine
MOA : derivative of amphetamine lacks CNS stimulant action. It release of
noradrenaline from nerve synapses and cause dilation of pupil.
Uses : 1. it is used as an eye drops to dilate the pupill.
2. It’s used as a diagnostic agent for testing Hornets syndrome ( damage of
nerves of eyes)
24. 2. Propylhexeridine
IUPAC name : 1- Cyclohexyl-N-methylpropan-2-amine
Uses : 1. It has symathomimatic, adrenergic, Vasoconstrictive
and Psychostimulant effect.
2. Used medicinally for relief of congestion due to colds,
allergies and rhinitis.
25. 3. Pseudoephedrine
It is an optically active isomer of Ephedrine. Ephedrine occurs naturally in
Ephedra
IUPAC name : ( 1S , 2S) -2-methylamino-1-phenylpropane-1-ol
MOA : it has both alpha and beta adrenergic activity. It stimulates CNS. It
increases the BP by Increasing cardiac output.
Uses : 1. mainly used as a nasal and bronchial decongestant.
2. It causes Vasoconstriction si results in hypertension
26. Mixed acting drugs💊💉
These drug indicates they act directly on the adrenergic
receptors and also effect the release of noradrenaline.
This drug at both directly and indirectly acting drugs.
27. 1. Ephedrine
IUPAC name : (1R, 2S) -2-methylamino-1-phenylpropan-1-ol
MOA : it has alpha and beta Adrenergic activity.It has high stimulating effect on the
CNS. It has both direct and indirect effect on adrenergic receptor.
Uses : 1. used to control bronchial spasm in asthma
2. Used as a CNS stimulant in narcolepsy
3. Used ias a nasal decongestant in the form of nasal drops and nasal sprays
28. 2. Metaraminol
IUPAC name : ( 1R, 2S)-2-amino-1(3-hydroxyphenyl) -propan-1-ol
MOA : Same like to ephidrine
Uses : 1. It is used as a pressor agent in various hypotensive states
2. It is used in the treatment of Hypotension which is due to
complication of anesthesia.