Sulphonamides are among the oldest antibacterial agents used to treat infections. They work by competitively inhibiting the enzyme dihydropteroate synthase, blocking folic acid synthesis in bacteria. This makes them bacteriostatic rather than bactericidal. Chemical modifications of the sulphonamide structure have led to important drug classes like diuretics, hypoglycemics, and anti-mycobacterials. Sulphonamides are commonly used to treat urinary tract, respiratory, and other bacterial infections. When combined with trimethoprim, they have broad-spectrum activity against many pathogens and are used as co-trimoxazole. Adverse effects can include allergic reactions and bone marrow suppression.
Aminoglycosides(medicinal chemistry by p.ravisankar)Dr. Ravi Sankar
Aminoglycosides,Aminocyclitols,Source,Structures of streptomycin,Dihydrostreptomycin,A mention of other aminoglycoside antibiotics,Acid hydrolysis,Mechanism of action,SAR,Dihydrostreptomycin and its importance,therapeutic uses, toxicity.
Sulfonamide (also called sulphonamide, sulfa drugs or sulpha drugs) is the basis of several groups of drugs. The original antibacterial sulfonamides are synthetic antimicrobial agents that contain the sulfonamide group.
-a broad-spectrum antibiotics.
-It is commonly used to treat acne, infection, and other infections caused by bacteria.
-The first of these compounds was chlortetracycline followed by oxytetracycline and tetracycline.
Tetracycline is a broad-spectrum polyketide antibiotic produced by the Streptomyces genus of Actinobacteria, indicated for use against many bacterial infections. It is a protein synthesis inhibitor. It is commonly used to treat acne today, and, more recently, rosacea, and is historically important in reducing the number of deaths from cholera. Tetracycline is marketed under the brand names Sumycin, Tetracyn, and Panmycin, among others. Actisite is a thread-like fiber formulation used in dental applications. It is also used to produce several semisynthetic derivatives, which together are known as the tetracycline antibiotics. The term "tetracycline" is also used to denote the four-ring system of this compound; "tetracyclines" are related substances that contain the same four-ring system.
Aminoglycosides(medicinal chemistry by p.ravisankar)Dr. Ravi Sankar
Aminoglycosides,Aminocyclitols,Source,Structures of streptomycin,Dihydrostreptomycin,A mention of other aminoglycoside antibiotics,Acid hydrolysis,Mechanism of action,SAR,Dihydrostreptomycin and its importance,therapeutic uses, toxicity.
Sulfonamide (also called sulphonamide, sulfa drugs or sulpha drugs) is the basis of several groups of drugs. The original antibacterial sulfonamides are synthetic antimicrobial agents that contain the sulfonamide group.
-a broad-spectrum antibiotics.
-It is commonly used to treat acne, infection, and other infections caused by bacteria.
-The first of these compounds was chlortetracycline followed by oxytetracycline and tetracycline.
Tetracycline is a broad-spectrum polyketide antibiotic produced by the Streptomyces genus of Actinobacteria, indicated for use against many bacterial infections. It is a protein synthesis inhibitor. It is commonly used to treat acne today, and, more recently, rosacea, and is historically important in reducing the number of deaths from cholera. Tetracycline is marketed under the brand names Sumycin, Tetracyn, and Panmycin, among others. Actisite is a thread-like fiber formulation used in dental applications. It is also used to produce several semisynthetic derivatives, which together are known as the tetracycline antibiotics. The term "tetracycline" is also used to denote the four-ring system of this compound; "tetracyclines" are related substances that contain the same four-ring system.
Anti Malarial Drugs of medicinal chemistryPranjal Saxena
This slide contain information about Anti Malarial Drugs and their description with the synthesis of Chloroquine and pamaquine
SAR of quinolines
Miscellaneous agents of anti Malarial
THIS PRESENTATION ABOUT ANTIMALARIAL DRUGS DETAILING THE COMPLETE INFORMATION ABOUT THE DRUGS USED WITH ITS MECHANISM OF ACTION, STRUCTURAL ACTIVITY AND DOSES.
sulfonamides are the antimicrobial agents.It's act by folic acid synthesis inhibitors.It is PABA analogue competitive antagonist. first synthesised drug is prontosil.
In this slide contents history, mechanism of action, SAR, classification of drugs, some structure of important drugs, choice of drugs in different purpose, side effect, adverse effect.
subscribe the channel :Work&Life Hobbies
watch video:https://www.youtube.com/watch?v=v3rI1lf2TZ8&t=403s
This slide describes the Important Synthesis of Antiviral Drugs
Malignancy is most familiar as a characterization of cancer.Chemotherapy is a category of cancer treatment that uses one or more anti-cancer drugs as part of a standardized chemotherapy regimen
Anti Malarial Drugs of medicinal chemistryPranjal Saxena
This slide contain information about Anti Malarial Drugs and their description with the synthesis of Chloroquine and pamaquine
SAR of quinolines
Miscellaneous agents of anti Malarial
THIS PRESENTATION ABOUT ANTIMALARIAL DRUGS DETAILING THE COMPLETE INFORMATION ABOUT THE DRUGS USED WITH ITS MECHANISM OF ACTION, STRUCTURAL ACTIVITY AND DOSES.
sulfonamides are the antimicrobial agents.It's act by folic acid synthesis inhibitors.It is PABA analogue competitive antagonist. first synthesised drug is prontosil.
In this slide contents history, mechanism of action, SAR, classification of drugs, some structure of important drugs, choice of drugs in different purpose, side effect, adverse effect.
subscribe the channel :Work&Life Hobbies
watch video:https://www.youtube.com/watch?v=v3rI1lf2TZ8&t=403s
This slide describes the Important Synthesis of Antiviral Drugs
Malignancy is most familiar as a characterization of cancer.Chemotherapy is a category of cancer treatment that uses one or more anti-cancer drugs as part of a standardized chemotherapy regimen
Sulphonamides, MOA, SAR, History of development, Nomenclature of the Sulfonamides, Classification, Spectrum of Action of the Sulfonamides,Structure Activity Relationship, Reducing Toxicity, Cotrimoxazole
Sulphonamides are a group of synthetic antimicrobial agents that contain the sulfonamide group (-SO2NH2). These drugs were among the first antimicrobial agents to be widely used in clinical medicine, and they paved the way for the antibiotic revolution in the mid-20th century. Sulphonamides are primarily bacteriostatic, meaning they inhibit the growth and multiplication of bacteria rather than directly killing them.
Sulphonamides are the first effective chemotherapeutic agents used for bacterial infection in humans. Sulfonamides have a wide range of pharmacological activities such as Oral hypoglycemic, antileprotic, anti epileptic, anti-hypertensive, anti-bacterial, anti-protozoal, anti-fungal, anti retroviral, anti cancer, antiinflammatory, and used as diuretic. This review consists of a discussion on the various pharmacological effects of sulfonamides
Sulfonamides are synthetic antibacterial agents that contain the sulfonamide group. Classification, Chemistry and SAR, Mechanism of action, Side effects and Marketed preparations.....
Sulfonamides (sulphonamides) are a group of man-made (synthetic) medicines that contain the sulfonamide chemical group. They may also be called sulfa drugs. Many people use the term sulfonamide imprecisely to refer only to antibiotics that have a sulfonamide functional group in their chemical structure.
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
Testicular torsion refers to twisting of the spermatic cord, causing ischaemia of the testicle.
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
Ozempic: Preoperative Management of Patients on GLP-1 Receptor Agonists Saeid Safari
Preoperative Management of Patients on GLP-1 Receptor Agonists like Ozempic and Semiglutide
ASA GUIDELINE
NYSORA Guideline
2 Case Reports of Gastric Ultrasound
New Directions in Targeted Therapeutic Approaches for Older Adults With Mantl...i3 Health
i3 Health is pleased to make the speaker slides from this activity available for use as a non-accredited self-study or teaching resource.
This slide deck presented by Dr. Kami Maddocks, Professor-Clinical in the Division of Hematology and
Associate Division Director for Ambulatory Operations
The Ohio State University Comprehensive Cancer Center, will provide insight into new directions in targeted therapeutic approaches for older adults with mantle cell lymphoma.
STATEMENT OF NEED
Mantle cell lymphoma (MCL) is a rare, aggressive B-cell non-Hodgkin lymphoma (NHL) accounting for 5% to 7% of all lymphomas. Its prognosis ranges from indolent disease that does not require treatment for years to very aggressive disease, which is associated with poor survival (Silkenstedt et al, 2021). Typically, MCL is diagnosed at advanced stage and in older patients who cannot tolerate intensive therapy (NCCN, 2022). Although recent advances have slightly increased remission rates, recurrence and relapse remain very common, leading to a median overall survival between 3 and 6 years (LLS, 2021). Though there are several effective options, progress is still needed towards establishing an accepted frontline approach for MCL (Castellino et al, 2022). Treatment selection and management of MCL are complicated by the heterogeneity of prognosis, advanced age and comorbidities of patients, and lack of an established standard approach for treatment, making it vital that clinicians be familiar with the latest research and advances in this area. In this activity chaired by Michael Wang, MD, Professor in the Department of Lymphoma & Myeloma at MD Anderson Cancer Center, expert faculty will discuss prognostic factors informing treatment, the promising results of recent trials in new therapeutic approaches, and the implications of treatment resistance in therapeutic selection for MCL.
Target Audience
Hematology/oncology fellows, attending faculty, and other health care professionals involved in the treatment of patients with mantle cell lymphoma (MCL).
Learning Objectives
1.) Identify clinical and biological prognostic factors that can guide treatment decision making for older adults with MCL
2.) Evaluate emerging data on targeted therapeutic approaches for treatment-naive and relapsed/refractory MCL and their applicability to older adults
3.) Assess mechanisms of resistance to targeted therapies for MCL and their implications for treatment selection
Couples presenting to the infertility clinic- Do they really have infertility...Sujoy Dasgupta
Dr Sujoy Dasgupta presented the study on "Couples presenting to the infertility clinic- Do they really have infertility? – The unexplored stories of non-consummation" in the 13th Congress of the Asia Pacific Initiative on Reproduction (ASPIRE 2024) at Manila on 24 May, 2024.
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
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
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.
Title: Sense of Taste
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 structure and function of taste buds.
Describe the relationship between the taste threshold and taste index of common substances.
Explain the chemical basis and signal transduction of taste perception for each type of primary taste sensation.
Recognize different abnormalities of taste perception and their causes.
Key Topics:
Significance of Taste Sensation:
Differentiation between pleasant and harmful food
Influence on behavior
Selection of food based on metabolic needs
Receptors of Taste:
Taste buds on the tongue
Influence of sense of smell, texture of food, and pain stimulation (e.g., by pepper)
Primary and Secondary Taste Sensations:
Primary taste sensations: Sweet, Sour, Salty, Bitter, Umami
Chemical basis and signal transduction mechanisms for each taste
Taste Threshold and Index:
Taste threshold values for Sweet (sucrose), Salty (NaCl), Sour (HCl), and Bitter (Quinine)
Taste index relationship: Inversely proportional to taste threshold
Taste Blindness:
Inability to taste certain substances, particularly thiourea compounds
Example: Phenylthiocarbamide
Structure and Function of Taste Buds:
Composition: Epithelial cells, Sustentacular/Supporting cells, Taste cells, Basal cells
Features: Taste pores, Taste hairs/microvilli, and Taste nerve fibers
Location of Taste Buds:
Found in papillae of the tongue (Fungiform, Circumvallate, Foliate)
Also present on the palate, tonsillar pillars, epiglottis, and proximal esophagus
Mechanism of Taste Stimulation:
Interaction of taste substances with receptors on microvilli
Signal transduction pathways for Umami, Sweet, Bitter, Sour, and Salty tastes
Taste Sensitivity and Adaptation:
Decrease in sensitivity with age
Rapid adaptation of taste sensation
Role of Saliva in Taste:
Dissolution of tastants to reach receptors
Washing away the stimulus
Taste Preferences and Aversions:
Mechanisms behind taste preference and aversion
Influence of receptors and neural pathways
Impact of Sensory Nerve Damage:
Degeneration of taste buds if the sensory nerve fiber is cut
Abnormalities of Taste Detection:
Conditions: Ageusia, Hypogeusia, Dysgeusia (parageusia)
Causes: Nerve damage, neurological disorders, infections, poor oral hygiene, adverse drug effects, deficiencies, aging, tobacco use, altered neurotransmitter levels
Neurotransmitters and Taste Threshold:
Effects of serotonin (5-HT) and norepinephrine (NE) on taste sensitivity
Supertasters:
25% of the population with heightened sensitivity to taste, especially bitterness
Increased number of fungiform papillae
2. Description
• One of the oldest antibacterial agents used to
combat infection
• Used for coccal infection in 1935
• They are bacteriostatic because it inhibits
bacterial synthesis of folic acid
• Clinical usefulness has decreased because of the
effectiveness of other antibiotics and penicillin
2
3. Presence of free amino group
Antibacterial action
Prontosil red Prodrug
In vitro Inactive
In vivo Active
SO2NH2
N N NH2
NH2
SO2NH2
NH2
NH2
NH2
NH2
Metablic cleavage
+
Prontosil Red Sulphonamide
3
4. Chemical modification of the sulphonamide structure
has given rise to several important group of drugs.
Gloucoma – Acetazolamide
Diuretic – Thiazides
Anti-mycobacterial – Sulphones
Oral hypoglycemic – Sulphonyl ureas
NH2SO2
NH2
Substitution gives
prodrug
1) Sodium salt-- water soluble
2)Substitution on these group gives
different molecules having different
pharmacokinetic properties
4
5. Mechanism of action
• Competitive inhibitor to dihydropteroate synthase
enzyme due to resemblance with para-amino benzoic
acid.
• Sulfonamides therefore are reversible inhibitors of
folic acid synthesis and bacteriostatic not
bactericidal.
• Inhibit bacterial growth without affecting normal
cells
5
7. Antibacterial activityAntibacterial activity
• Gram-positive and gram negative.
• Nocardia, chlamydia trachomatis, some protozoa.
ClassificationClassification
A. Sulphonamides employed for treatment of
systemic infection. Depending upon duration , they
can be further subdivided into
7
8. a) Short to intermediate acting sulphonamides.
NH2 SO2N
H
O
N
CH3
CH3
NH2 SO2N
H
N
N
NH2 SO2N
H
O
N
CH3
NH2 SO2N
H
N
N
Sulphamethoxazole Sulphadiazine
Slpfisoxazole
Sulphaphenazole
8
9. B. Long acting sulphonamides
C. Extra long acting sulphonamides
NH2 SO2N
H
N
N
CH3
CH3
NH2 SO2N
H
N N
OMe
Sulphamethoxypyridazine
Sulphadimethoxine
N SO2N
H
N
NOH
HOOC
NH2 SO2N
H
N
N
MeO
Sulphasalazine
Sulphadiazine
9
10. 2. Poorly absorbed sulphonamides
3. Topically used sulphonamides
NH2 SO2N
H
NH2
NH
SO2N
H
N
H
O
CH2
C
H2
OH
O
N
S
SO2N
H
N
H
OO
OH
N
S
Sulphaguanidine
Succinyl Sulphathiazole
Phthalyl Sulphathiazole
NH2 SO2N
H
COCH3
NH2 SO2N
N
N
Ag
+
S
O O
N
H
O CH3
ONH2
Sulphacetamide
Silver Sulphadiazine
Mafenide acetate
10
11. Structure activityStructure activity
relationShiprelationShip
GeneralGeneral
1.Sulphonamide skeleton is the minimum structural
requirement for antibacterial activity.
2.The active form of sulphonamide is the ionized form.
Maximum activity is observed bretween the pka value
6.6-7.4.
3. Sulphonamides competes for binding site on plasma
albumin with causes increased action of drugs like
Aspirin, Phenylbutazone, methotrexate etc. 11
12. RHN SO2NHR'
1 4
Sulphur atom should be directly
linked to the benzene ring
The free aromatic amino group should
reside para to the sulphonamide group
Substituents at these positions results
in devoid of antibacterial activity
Substitution at this position activity varies with the nature of
substituents.
1) Electron donating substituents to SO2 leads to increase in
antibacterial activity.
2) Heterocyclic substituents leads to highly potent derivatives.
3) Substitution of free Sulphonic acid (-SO3H) group for
sulphonamide function destroys activity.
4) Replacement by a sulfinic acid group (-SO2H) an acetylation
of N1 positio retains activity.
Structure activity relationship of sulphonamide 12
13. Therapeutic usesTherapeutic uses
• Urinary tract infections
• Upper respiratory tract infections
• Nocardiosis
• Sulfasalazine in IBD.
• Sulfacetamide in bacterial conjunctivitis & trachoma
• Silver sulfadiazine for prevention of infection of
burn wounds .
13
14. Adverse effectsAdverse effects
• Hypersensitivity reactions
• Crystalluria,hematuria,renal obstruction.
• Allergic nephritis
• Haemolytic anaemia, aplastic anaemia, thrombocytopenia.
• Kernicterus in new born
14
15. Trimethoprim - Sulfamethoxazole combinationTrimethoprim - Sulfamethoxazole combination
(Co-trimoxazole(Co-trimoxazole)
N
N
NH2
NH2
C
H2
CH3
CH3
CH3
NH2 SO2N
H
O
N
CH3
TrimethoprimSulphamethoxazole
15
16. Mechanism of action:
• Sequential blocking of purine synthesis
(synergism).
• Trimethoprim inhibits dihydrofolate reductase
enzyme so inhibits tetrahydrofolic acid synthesis
• The combination is bactericidal
16
20. Adverse effects
• Megaloblastic anemia, leukopenia & granulocytopenia
(can be prevented by administration of folic acid )
• All side effects associated with sulfonamides
20