Benzodiazepines are a class of psychoactive drugs whose core structure is derived from fusing a benzene and diazepine ring. They were discovered in 1955 and are primarily used to treat anxiety, panic disorders, insomnia, seizures and muscle spasms. Benzodiazepines produce their effects by enhancing the action of the inhibitory neurotransmitter GABA at GABA-A receptors in the brain. They are classified based on their duration of action as short, intermediate or long acting. While generally safe and effective, benzodiazepines can cause side effects like sedation and dependence with long term use.
Reviews the uses for benzodiazepines and barbiturates, the signs of intoxication and withdrawal, impact on sports performance. Continuing Education for mental health and substance abuse counselors and therapists.
Sedatives and Hypnotics
Pharmacology
Clinical uses
Sedation
Coping with stress and anxiety
Smoothing effects of stimulants
Potentiation of narcotics
Treatment of serious mental disorders
Pleasurable sensations, including intoxication
Classifications
Benzodiazepines
Diazepam, Clonazepam, Oxazepam, Clobazam, Clordiazepoxide, Midazolam
Barbiturates
Phenobarbitone, Amobarbital, Thiopental-Na
Newer drugs
Zolpidem, Zaleplon, Buspirone
Chloral hydrate
Paraldehyde
Diphenhydramine
Benzodiazepines
Properties
High therapeutic index (high LD50)
Relatively safe in overdose
Develop tolerance slowly
Less addiction liability
Benzodiazepines
Benzodiazepines
Most commonly prescribed Benzodiazepines
All Benzodiazepines are classified as Controlled Drugs in some countries.
Most are CD Schedule 4
Diazepam (Valium,Anxicalm)
Alprazolam (Xanax)
Bromazepam (Lexotan)
Clobazam (Frisium)
Lormetazepam (Noctamid)
Nitrazepam (Mogadon)
Clonazepam
Two are CD Schedule 3
Flurazepam (Rohypnol)
Temazepam (Nortem)
Structure Activity Relationship
In ring A an electron – withdrawing group such as Cl, Br, NO2 or CN at position 7.
A methyl Group is attached to the nitrogen atom in position 1 in ring B. However, substituents at position 1 that are metabolically are still clinically useful e.g. Flurazepam.
Replacement of the carbonyl function with two hydrogens in position 2 gives medazepam, less potent than diazepam.
Replacement of one of the hydrogen with a OH group on position 3 lower the activity on the one hand and aids elimination on the other.
Introduction of a carbonyl function in the 3 position increases the duration of action and also favours formation of water soluble salts.
e) α-pyridyl derivative and cycloalkyl substituent at 5 position give potent compounds.
f) Electronegative substituents such as Cl or F at the ortho and disubstituted in both ortho positions in ring C.
g) Derivatives with additional rings joining the diazepine nucleus at the 1 and 2 positions are generally more active than the corresponding 1-methylbenzodiazepines.
h) Replacement of the benzene ring by heteroaromatic (e.g. pyrazole) resulted in compounds with interesting anxiolytic properties ( e.g. ripazepam).
i) Saturation of the 4,5- double bond reduces potency, as does a shift of the unsaturation into the 3,4-position.
Barbiturates
Barbiturates
Barbiturates
Barbiturate poisoning
Treatment of Barbiturate poisoning
Buspirone
Reviews the uses for benzodiazepines and barbiturates, the signs of intoxication and withdrawal, impact on sports performance. Continuing Education for mental health and substance abuse counselors and therapists.
Sedatives and Hypnotics
Pharmacology
Clinical uses
Sedation
Coping with stress and anxiety
Smoothing effects of stimulants
Potentiation of narcotics
Treatment of serious mental disorders
Pleasurable sensations, including intoxication
Classifications
Benzodiazepines
Diazepam, Clonazepam, Oxazepam, Clobazam, Clordiazepoxide, Midazolam
Barbiturates
Phenobarbitone, Amobarbital, Thiopental-Na
Newer drugs
Zolpidem, Zaleplon, Buspirone
Chloral hydrate
Paraldehyde
Diphenhydramine
Benzodiazepines
Properties
High therapeutic index (high LD50)
Relatively safe in overdose
Develop tolerance slowly
Less addiction liability
Benzodiazepines
Benzodiazepines
Most commonly prescribed Benzodiazepines
All Benzodiazepines are classified as Controlled Drugs in some countries.
Most are CD Schedule 4
Diazepam (Valium,Anxicalm)
Alprazolam (Xanax)
Bromazepam (Lexotan)
Clobazam (Frisium)
Lormetazepam (Noctamid)
Nitrazepam (Mogadon)
Clonazepam
Two are CD Schedule 3
Flurazepam (Rohypnol)
Temazepam (Nortem)
Structure Activity Relationship
In ring A an electron – withdrawing group such as Cl, Br, NO2 or CN at position 7.
A methyl Group is attached to the nitrogen atom in position 1 in ring B. However, substituents at position 1 that are metabolically are still clinically useful e.g. Flurazepam.
Replacement of the carbonyl function with two hydrogens in position 2 gives medazepam, less potent than diazepam.
Replacement of one of the hydrogen with a OH group on position 3 lower the activity on the one hand and aids elimination on the other.
Introduction of a carbonyl function in the 3 position increases the duration of action and also favours formation of water soluble salts.
e) α-pyridyl derivative and cycloalkyl substituent at 5 position give potent compounds.
f) Electronegative substituents such as Cl or F at the ortho and disubstituted in both ortho positions in ring C.
g) Derivatives with additional rings joining the diazepine nucleus at the 1 and 2 positions are generally more active than the corresponding 1-methylbenzodiazepines.
h) Replacement of the benzene ring by heteroaromatic (e.g. pyrazole) resulted in compounds with interesting anxiolytic properties ( e.g. ripazepam).
i) Saturation of the 4,5- double bond reduces potency, as does a shift of the unsaturation into the 3,4-position.
Barbiturates
Barbiturates
Barbiturates
Barbiturate poisoning
Treatment of Barbiturate poisoning
Buspirone
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Hello friends. In this PPT I am talking about CNS drugs. If you like it, please do let me know in the comments section. A single word of appreciation from you will encourage me to make more of such videos. Thanks. Enjoy and welcome to the beautiful world of pharmacology where pharmacology comes to life. This video is intended for MBBS, BDS, paramedical and any person who wishes to have a basic understanding of the subject in the simplest way.
Flu Vaccine Alert in Bangalore Karnatakaaddon Scans
As flu season approaches, health officials in Bangalore, Karnataka, are urging residents to get their flu vaccinations. The seasonal flu, while common, can lead to severe health complications, particularly for vulnerable populations such as young children, the elderly, and those with underlying health conditions.
Dr. Vidisha Kumari, a leading epidemiologist in Bangalore, emphasizes the importance of getting vaccinated. "The flu vaccine is our best defense against the influenza virus. It not only protects individuals but also helps prevent the spread of the virus in our communities," he says.
This year, the flu season is expected to coincide with a potential increase in other respiratory illnesses. The Karnataka Health Department has launched an awareness campaign highlighting the significance of flu vaccinations. They have set up multiple vaccination centers across Bangalore, making it convenient for residents to receive their shots.
To encourage widespread vaccination, the government is also collaborating with local schools, workplaces, and community centers to facilitate vaccination drives. Special attention is being given to ensuring that the vaccine is accessible to all, including marginalized communities who may have limited access to healthcare.
Residents are reminded that the flu vaccine is safe and effective. Common side effects are mild and may include soreness at the injection site, mild fever, or muscle aches. These side effects are generally short-lived and far less severe than the flu itself.
Healthcare providers are also stressing the importance of continuing COVID-19 precautions. Wearing masks, practicing good hand hygiene, and maintaining social distancing are still crucial, especially in crowded places.
Protect yourself and your loved ones by getting vaccinated. Together, we can help keep Bangalore healthy and safe this flu season. For more information on vaccination centers and schedules, residents can visit the Karnataka Health Department’s official website or follow their social media pages.
Stay informed, stay safe, and get your flu shot today!
ARTIFICIAL INTELLIGENCE IN HEALTHCARE.pdfAnujkumaranit
Artificial intelligence (AI) refers to the simulation of human intelligence processes by machines, especially computer systems. It encompasses tasks such as learning, reasoning, problem-solving, perception, and language understanding. AI technologies are revolutionizing various fields, from healthcare to finance, by enabling machines to perform tasks that typically require human intelligence.
Knee anatomy and clinical tests 2024.pdfvimalpl1234
This includes all relevant anatomy and clinical tests compiled from standard textbooks, Campbell,netter etc..It is comprehensive and best suited for orthopaedicians and orthopaedic residents.
Acute scrotum is a general term referring to an emergency condition affecting the contents or the wall of the scrotum.
There are a number of conditions that present acutely, predominantly with pain and/or swelling
A careful and detailed history and examination, and in some cases, investigations allow differentiation between these diagnoses. A prompt diagnosis is essential as the patient may require urgent surgical intervention
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Testicular torsion results from inadequate fixation of the testis to the tunica vaginalis producing ischemia from reduced arterial inflow and venous outflow obstruction.
The prevalence of testicular torsion in adult patients hospitalized with acute scrotal pain is approximately 25 to 50 percent
Prix Galien International 2024 Forum ProgramLevi Shapiro
June 20, 2024, Prix Galien International and Jerusalem Ethics Forum in ROME. Detailed agenda including panels:
- ADVANCES IN CARDIOLOGY: A NEW PARADIGM IS COMING
- WOMEN’S HEALTH: FERTILITY PRESERVATION
- WHAT’S NEW IN THE TREATMENT OF INFECTIOUS,
ONCOLOGICAL AND INFLAMMATORY SKIN DISEASES?
- ARTIFICIAL INTELLIGENCE AND ETHICS
- GENE THERAPY
- BEYOND BORDERS: GLOBAL INITIATIVES FOR DEMOCRATIZING LIFE SCIENCE TECHNOLOGIES AND PROMOTING ACCESS TO HEALTHCARE
- ETHICAL CHALLENGES IN LIFE SCIENCES
- Prix Galien International Awards Ceremony
Title: Sense of Smell
Presenter: Dr. Faiza, Assistant Professor of Physiology
Qualifications:
MBBS (Best Graduate, AIMC Lahore)
FCPS Physiology
ICMT, CHPE, DHPE (STMU)
MPH (GC University, Faisalabad)
MBA (Virtual University of Pakistan)
Learning Objectives:
Describe the primary categories of smells and the concept of odor blindness.
Explain the structure and location of the olfactory membrane and mucosa, including the types and roles of cells involved in olfaction.
Describe the pathway and mechanisms of olfactory signal transmission from the olfactory receptors to the brain.
Illustrate the biochemical cascade triggered by odorant binding to olfactory receptors, including the role of G-proteins and second messengers in generating an action potential.
Identify different types of olfactory disorders such as anosmia, hyposmia, hyperosmia, and dysosmia, including their potential causes.
Key Topics:
Olfactory Genes:
3% of the human genome accounts for olfactory genes.
400 genes for odorant receptors.
Olfactory Membrane:
Located in the superior part of the nasal cavity.
Medially: Folds downward along the superior septum.
Laterally: Folds over the superior turbinate and upper surface of the middle turbinate.
Total surface area: 5-10 square centimeters.
Olfactory Mucosa:
Olfactory Cells: Bipolar nerve cells derived from the CNS (100 million), with 4-25 olfactory cilia per cell.
Sustentacular Cells: Produce mucus and maintain ionic and molecular environment.
Basal Cells: Replace worn-out olfactory cells with an average lifespan of 1-2 months.
Bowman’s Gland: Secretes mucus.
Stimulation of Olfactory Cells:
Odorant dissolves in mucus and attaches to receptors on olfactory cilia.
Involves a cascade effect through G-proteins and second messengers, leading to depolarization and action potential generation in the olfactory nerve.
Quality of a Good Odorant:
Small (3-20 Carbon atoms), volatile, water-soluble, and lipid-soluble.
Facilitated by odorant-binding proteins in mucus.
Membrane Potential and Action Potential:
Resting membrane potential: -55mV.
Action potential frequency in the olfactory nerve increases with odorant strength.
Adaptation Towards the Sense of Smell:
Rapid adaptation within the first second, with further slow adaptation.
Psychological adaptation greater than receptor adaptation, involving feedback inhibition from the central nervous system.
Primary Sensations of Smell:
Camphoraceous, Musky, Floral, Pepperminty, Ethereal, Pungent, Putrid.
Odor Detection Threshold:
Examples: Hydrogen sulfide (0.0005 ppm), Methyl-mercaptan (0.002 ppm).
Some toxic substances are odorless at lethal concentrations.
Characteristics of Smell:
Odor blindness for single substances due to lack of appropriate receptor protein.
Behavioral and emotional influences of smell.
Transmission of Olfactory Signals:
From olfactory cells to glomeruli in the olfactory bulb, involving lateral inhibition.
Primitive, less old, and new olfactory systems with different path
- Video recording of this lecture in English language: https://youtu.be/lK81BzxMqdo
- Video recording of this lecture in Arabic language: https://youtu.be/Ve4P0COk9OI
- Link to download the book free: https://nephrotube.blogspot.com/p/nephrotube-nephrology-books.html
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micro teaching on communication m.sc nursing.pdfAnurag Sharma
Microteaching is a unique model of practice teaching. It is a viable instrument for the. desired change in the teaching behavior or the behavior potential which, in specified types of real. classroom situations, tends to facilitate the achievement of specified types of objectives.
Explore natural remedies for syphilis treatment in Singapore. Discover alternative therapies, herbal remedies, and lifestyle changes that may complement conventional treatments. Learn about holistic approaches to managing syphilis symptoms and supporting overall health.
Report Back from SGO 2024: What’s the Latest in Cervical Cancer?bkling
Are you curious about what’s new in cervical cancer research or unsure what the findings mean? Join Dr. Emily Ko, a gynecologic oncologist at Penn Medicine, to learn about the latest updates from the Society of Gynecologic Oncology (SGO) 2024 Annual Meeting on Women’s Cancer. Dr. Ko will discuss what the research presented at the conference means for you and answer your questions about the new developments.
3. History :
• A benzodiazepine is a psychoactive drug whose core
chemical structure is the fusion of a benzene ring and
a diazepine ring.
• The first benzodiazepine, chlordiazepoxide (Librium),
was discovered accidentally by Leo Sternbach in 1955,
and made available in 1960 by Hoffmann–La Roche,
which has also marketed diazepam (Valium) since 1963.
4. Benzodiazepines are used primarily in the treatment of :-
Generalized anxiety
Panic disorders
As sedative hypnotics
As muscle relaxants
As anticonvulsants
They largely replaced barbiturates because they're are shown to
have much wider safety margins than barbiturates, thus safer.
Traditionally they are considered to have a less potential for
addiction and dependence..
6. Intermediate Acting
Half life is 6-24 hours
• Alprazolam
• Estazolam
• Chlordiazepoxide
• Temazepam
Long Acting
Half life is more than 24
hours
• Diazepam
• Quazepam
• Nitrazepam
7. Sites of BZDs in brain
• The targets for BZDs in brains are the GABA receptors
• GABA receptors are primarily composed of
• 2 α subunits
• 2 β subunits
• 1 γ subunit
• BZDs modulate GABA effects by binding to a specific, high
affinity site located at interface of the
α & γ2 subunits
8.
9.
10. Binding of GABA to its receptors triggers an opening of
chloride channel, which leads to an increase in chloride
conductance.
BZDs increase the frequency of channel opening
produces by GABA.
The influx of chloride ions causes hyperpolarization that
moves the postsynaptic potential away from its firing
threshold , and ,thus inhibits the formation of action
potentials.
Mechanism of Action
11.
12.
13.
14. PHARMACOKINETICS:
• Absorption and distribution :-
BZDs are lipophilic they are rapidly and completely
absorbed after oral administration and distribute
throughout the body .
Binding:-
Strongly bound to plasma proteins
16. Metabolism:-
Most BZDs including Chlordiazepoxide and diazepam are
metabolized by the hepatic microsomal system to compound that
are also active.
Excretion:-
BZDs are excreted in urine as glucoronides metabolites.
17.
18. Actions
• Reduction of anxiety:-
At low doses BZDs anxiolytic by inhibiting neuronal circuits in limbic system of
brain.. Alprazolam, Lorazepam, Oxazepam, Chlordiazepoxide..
• Sedative & hypnotic actions:-
All of BZDs used to treat anxiety have some sedative properties, and some can
produces hypnosis at high doses.. Diazepam, Flurazepam,
Nitrazepam,Midazolam..
• Anterograde amnesia:-
The temporary loss of memory with the use of benzodiazepam is also mediated
by the α1-GABAa receptors this also impairs a person’s ability to learn and form
a new memory.
19. • Anticonvulsant:-
Several of BZDs have anticonvulsant activity & some are use
to treat epilepsy & seizures disorder
Clonazepam , Diazepam, Clobazam
• Muscle relaxant:-
At high doses, the BZDs relax the spasticity of skeletal
muscle, probably by increasing presynaptic inhibition in spinal
cord, where the α2 GABAa receptors are largely located
21. Acute toxicity: Benzodiazepines in acute overdose are
considerably less dangerous than other sedative-hypnotic drugs.
Cause prolonged sleep, without serious depression of
respiration or cardiovascular system.
Severe and even life threatening respiratory depression may
occur in BZD combination with other CNS depressants
particularly ALCOHOL.
Acute overdose can b counteracted by effective antagonist,
flumazenil.
22. • Side-effects during therapeutic use: Influence of
manual skills: (i.e driving performance) due to drowsiness,
confusion, amnesia, impaired coordination. Main disadvantages
are interaction with alcohol, long-lasting hangover and the
development of dependence.
• Tolerance and dependence: Tolerance may occur with all
BZD.
• Stopping BZD treatment after weeks or months causes an
increase in symptoms of anxiety, together with tremor n
dizziness.
23. Precautions
These drugs should be used cautiously in
treating patients with liver disease
These drugs should be avoided in patients
With acute narrow angle glaucoma…
EFFECTS ON PREGNANCY:-
All the BZD cross the placental
barrier N may depress the CNS of the newborn , can result
In fetal abnormalities n fetal dependence If given before
birth.
Nursing infants can also suffer as BZD are excreted in breast
Milk.
24. Because of their muscle relaxant action, benzodiazepines may
cause respiratory depression in susceptible individuals. For that reason,
they are contraindicated in people with myasthenia gravis,sleep
apnea, bronchitis, and COPD.
Caution is required when benzodiazepines are used in people
with personality disorders or mental retardation because of
frequent paradoxical reactions.
In major depression, they may precipitate suicidal tendencies and are
sometimes used for suicidal overdoses.
Individuals with a history of alcohol, opioid and barbiturate abuse should
avoid benzodiazepines, as there is a risk of life-threatening interactions
with these drugs