THIS PRESENTATION ABOUT ANTIMALARIAL DRUGS DETAILING THE COMPLETE INFORMATION ABOUT THE DRUGS USED WITH ITS MECHANISM OF ACTION, STRUCTURAL ACTIVITY AND DOSES.
THIS PRESENTATION ABOUT ANTIMALARIAL DRUGS DETAILING THE COMPLETE INFORMATION ABOUT THE DRUGS USED WITH ITS MECHANISM OF ACTION, STRUCTURAL ACTIVITY AND DOSES.
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.
The all the content in this profile is completed by the teachers, students as well as other health care peoples.
thank you, all the respected peoples, for giving the information to complete this presentation.
this information is free to use by anyone.
Natural compounds from the bark of the cinchona tree, most notably quinine was observed to exhibit antimalarial activity.
Until the development of synthetic derivatives (ie. 4-aminoquinoline antimalarials), quinine continued to be the first choice to treat malaria.
Quinine is associated with side effects such as diarrhœa.
4-aminoquinoline antimalarials such as amodiaquine and chloroquine largely replaced quinine because of reduced unpleasant side effects.
The life cycle of the parasite and the immunological defence mechanisms against the parasite are complex.
Part of the parasite’s life cycle involves invasion of red blood cells (erythrocytes).
The haemoglobin within the red blood cell is broken down by the parasite and is used as a source of amino acids.
The 4-aminoquinolines act at the erythrocytic stage of the parasite.
Doxycycline is a compound used in prophylaxis against plasmodial parasites.
Other compounds associated with treating malaria include halofantrine and lumefantrine, often used in combination with other drugs.
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.
Definition: Antiviral agents are substances used in the treatment and prophylaxis of disease caused by viruses.
Classification:
A] Agents involves the inhibition of early stage of viral replication (Adamantane derivatives)
Admantane
Amantadine
Rimantadine
Tromantadine
B] Interferon:
Tilorane
ABPP (Bromopirimine)
CP20,961
-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.
Sulphonamides, MOA, SAR, History of development, Nomenclature of the Sulfonamides, Classification, Spectrum of Action of the Sulfonamides,Structure Activity Relationship, Reducing Toxicity, Cotrimoxazole
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.
The all the content in this profile is completed by the teachers, students as well as other health care peoples.
thank you, all the respected peoples, for giving the information to complete this presentation.
this information is free to use by anyone.
Natural compounds from the bark of the cinchona tree, most notably quinine was observed to exhibit antimalarial activity.
Until the development of synthetic derivatives (ie. 4-aminoquinoline antimalarials), quinine continued to be the first choice to treat malaria.
Quinine is associated with side effects such as diarrhœa.
4-aminoquinoline antimalarials such as amodiaquine and chloroquine largely replaced quinine because of reduced unpleasant side effects.
The life cycle of the parasite and the immunological defence mechanisms against the parasite are complex.
Part of the parasite’s life cycle involves invasion of red blood cells (erythrocytes).
The haemoglobin within the red blood cell is broken down by the parasite and is used as a source of amino acids.
The 4-aminoquinolines act at the erythrocytic stage of the parasite.
Doxycycline is a compound used in prophylaxis against plasmodial parasites.
Other compounds associated with treating malaria include halofantrine and lumefantrine, often used in combination with other drugs.
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.
Definition: Antiviral agents are substances used in the treatment and prophylaxis of disease caused by viruses.
Classification:
A] Agents involves the inhibition of early stage of viral replication (Adamantane derivatives)
Admantane
Amantadine
Rimantadine
Tromantadine
B] Interferon:
Tilorane
ABPP (Bromopirimine)
CP20,961
-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.
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.
Sulfonamides are synthetic antibacterial agents that contain the sulfonamide group. Classification, Chemistry and SAR, Mechanism of action, Side effects and Marketed preparations.....
Presentation gives details of Sulphonamides, its medicinal Chemistry and pharmacology , useful for the undergraduate and postgraduate students of Pharmacy , Medicinal Chemistry, Pharmaceutical Chemistry, Pharmacology, Medicine, Nursing and allied Health Sciences. Undergraduate and Postgraduate Course work
Sulphonamides Pharmacology For Pharmacy studentsMalay Pandya
This is the PowerPoint presentation of the Antimicrobial drug - SULPHOANMIDE.
Sulphonamide is the first antimicrobial agent
It Can be employed for suppressive therapy of chronic urinary tract infection, streptococcal pharyngitis and gum infection.
Combined with trimethoprim (cotrimoxazole) sulfamethoxazole is used for many bacterial infections.
This will be useful to all Pharmacy Student ...
The sulfonylamide tragedy refers to a historical event that occurred in the 1930s, which resulted in the deaths of many patients who were treated with certain medications containing sulfa drugs.
Sulfa drugs were discovered in the early 20th century and were considered a revolutionary breakthrough in the treatment of bacterial infections. They were widely used during World War II and saved countless lives.
However, in the 1930s, the pharmaceutical industry was still in its infancy and drug safety regulations were not as stringent as they are today. This led to the production and distribution of poorly tested and inadequately regulated drugs.
One such drug was Elixir Sulfanilamide, which contained the sulfa drug sulfanilamide and diethylene glycol as a solvent. The drug was marketed as a safe and effective treatment for streptococcal infections.
Unfortunately, the solvent used in Elixir Sulfanilamide was highly toxic, causing severe liver and kidney damage. This led to the deaths of over 100 people, including many children.
The tragedy resulted in the passing of the Federal Food, Drug, and Cosmetic Act in 1938, which established new safety requirements for drugs and food additives. It also highlighted the need for thorough testing and regulation of pharmaceutical products before they are released to the market.
Today, sulfa drugs are still used in the treatment of bacterial infections, but they are much safer and undergo rigorous testing and regulation before being approved for use.
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.
Sulphonamide and cotrimoxazole pptx-Dr.Jibachha SahDr. Jibachha Sah
Lecturer notes on veterinary pharmacology and toxicology for B.V.Sc & A.H Seventh semester student for educational purpose.This lecturer notes will be useful for all the veterinary students.Plesae send your comments,jibachhashah@gmail.com,mob.9845024121
Sulphonamides and their combination with trimethoprim - by Dr.Jibachha SahDr. Jibachha Sah
Sulphonamides and their combination with trimethoprim is lecturer notes on Veterinary Pharmacology & Toxicology(Chemotherapy) for B.V.Sc & A.H students of veterinary college.
New Drug Discovery and Development .....NEHA GUPTA
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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.
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.
- Video recording of this lecture in English language: https://youtu.be/lK81BzxMqdo
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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
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Tom Selleck Health: A Comprehensive Look at the Iconic Actor’s Wellness Journeygreendigital
Tom Selleck, an enduring figure in Hollywood. has captivated audiences for decades with his rugged charm, iconic moustache. and memorable roles in television and film. From his breakout role as Thomas Magnum in Magnum P.I. to his current portrayal of Frank Reagan in Blue Bloods. Selleck's career has spanned over 50 years. But beyond his professional achievements. fans have often been curious about Tom Selleck Health. especially as he has aged in the public eye.
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Introduction
Many have been interested in Tom Selleck health. not only because of his enduring presence on screen but also because of the challenges. and lifestyle choices he has faced and made over the years. This article delves into the various aspects of Tom Selleck health. exploring his fitness regimen, diet, mental health. and the challenges he has encountered as he ages. We'll look at how he maintains his well-being. the health issues he has faced, and his approach to ageing .
Early Life and Career
Childhood and Athletic Beginnings
Tom Selleck was born on January 29, 1945, in Detroit, Michigan, and grew up in Sherman Oaks, California. From an early age, he was involved in sports, particularly basketball. which played a significant role in his physical development. His athletic pursuits continued into college. where he attended the University of Southern California (USC) on a basketball scholarship. This early involvement in sports laid a strong foundation for his physical health and disciplined lifestyle.
Transition to Acting
Selleck's transition from an athlete to an actor came with its physical demands. His first significant role in "Magnum P.I." required him to perform various stunts and maintain a fit appearance. This role, which he played from 1980 to 1988. necessitated a rigorous fitness routine to meet the show's demands. setting the stage for his long-term commitment to health and wellness.
Fitness Regimen
Workout Routine
Tom Selleck health and fitness regimen has evolved. adapting to his changing roles and age. During his "Magnum, P.I." days. Selleck's workouts were intense and focused on building and maintaining muscle mass. His routine included weightlifting, cardiovascular exercises. and specific training for the stunts he performed on the show.
Selleck adjusted his fitness routine as he aged to suit his body's needs. Today, his workouts focus on maintaining flexibility, strength, and cardiovascular health. He incorporates low-impact exercises such as swimming, walking, and light weightlifting. This balanced approach helps him stay fit without putting undue strain on his joints and muscles.
Importance of Flexibility and Mobility
In recent years, Selleck has emphasized the importance of flexibility and mobility in his fitness regimen. Understanding the natural decline in muscle mass and joint flexibility with age. he includes stretching and yoga in his routine. These practices help prevent injuries, improve posture, and maintain mobilit
2. Inhibition of synthesis of essential
metabolites
Antimicrobials in this class;
• Sulfonamides
• Trimethoprim
Bacteriostatic
Mode of actions;
• inhibit the production of folic acid required for synthesis of purines
and nucleic acid
• does not affect human cells or certain bacteria
3. Gerhard Domagk
• German bacteriologist and pathologist who was
awarded the 1939 Nobel Prize for Physiology or
Medicine for his discovery of the antibacterial effects
of Prontosil, the first of the sulfonamide drugs.
• beginning of the concept of prodrug
• used greatly as antibiotic in the 1940’s, then
replaced by cheaper and less toxic penicillins.
• Sulfa drugs were discovered when a red dye called
prontosil has shown in-vivo antibacterial activity
while it was in-vitro inactive.
• This supports the idea that prontosil to exert its
action, it has to be activated by the host metabolic
pathways to give the active form.
H 2 N N
N H 2
N S
O
O
N H 2
H 2 N S
O
O
N H 2
S u lfa n ila m id e o r S u lfa n am id e
H 2 N N
N H 2
N S
O
O
N H 2
P ro n to sil
In v iv o
A zo d y e ac tiv e in
viv o b u t n o t o n
b ac teria l c u ltu res
H 2 N S
O
O
N H 2
4. Antibacterial sulfonamides
Mechanism of Action;
Step 1;
• Inhibited by Sulfonamides which
act by competing with PABA
here.
Step 3;
• Inhibited by Trimethoprim
S O 2 N H 2
H 2 N
C O O H
H 2 N
P-amino-benzoic acid (PABA) Sulfanilamide
5. Mechanism of action
• Sulfonamides are a competitive inhibitors of dihydropteroate synthetase
which is a vital enzyme for the synthesis of tetrahydrofolate ( Coenzyme
F).
• Tetrahydrofolate is important for pyrimidine nucleic acid synthesis so the
bacteria can no longer grow and divide which gives time for the host
immune system to destroy the bacterial cells.
• Sulfonamide is not recommended in patients with weak or impaired
immune system.
• This binding is reversible.
• Because of that sulfonamides have bacteriostatic effect not bactericidal.
6. Mechanism of action
• Sulfonamides mimic P-aminobenzoic acid (PABA) which is the
normal substrate for dihydropteroate synthetase. This means
that sulfonamide will bind in the same manner as PABA:
7. Mechanism of action
• Because sulfonamides are competitive inhibitors for the enzyme, the bacteria can
increase the production of PABA to compete with sulfonamide at the active site
and become resistant to sulfa drugs.
• In such case, the dose of sulfonamide agents should be increased to overcome this
resistant mechanism. But this high dose is accompanied with an increase in side
effects especially the crystalluria.
• In human, the cell synthesized tetrahydrofolate from folic acid that obtained from
food sources. This folic acid is normally transported to inside the cell by special
transport system.
• Bacterial cell does not have such transport system and they should synthesize
tetrahydrofolate using PABA.
• For that reason, human cells do not need dihydropteroate synthetaze enzyme
which means sulfonamides have selective antibacterial activity.
8. Structure-Activity Relationships (SAR)
• The p-amino group is essential for activity and must be unsubstituted (i.e. R
= H).
• The only exception is when R = acyl (i.e. amides). The amides themselves
are inactive but can be metabolized in the body to regenerate the active
compound
• The aromatic ring and the sulfonamide functional group are both required.
• The aromatic ring must be para-substituted only.
• The sulfonamide nitrogen must be secondary.
• R" is the only possible site that can be varied in sulfonamides.
9. Sulfonamides antibacterial agents
• They are the first synthetic antibacterial agents.
• They have good antibacterial activity mainly on gram +ve
bacteria.
• limitation of the sulfa drugs use:
– Sulfa allergic reactions.
– The formation of crystalluria.
– They give toxic metabolites after the oxidation of the
aromatic amine:
10. The problem of crystalluria
• Sulfonamides are mostly excreted in urine as acetylated metabolite.
• They are relatively water insoluble mainly due to the formation of
the acetylated metabolites.
• The acetylated metabolite is non-ionizable under the pH conditions
of the urine (≈ 7) that increase the possibility of precipitation and
the formation of crystals in the urine (crystalluria)
11. The problem of crystalluria
• How to minimize the possibility of crystalluria formation with
sulfonamides:
– Increase the urine flow.
– Increase the pH of the urine to increase the ionization of
sulfonamides and the formation of water soluble salts (this can
be done by taking sodium bicarbonate or potassium citrate.
– Lowering the pKa of the sulfonamide group which will help to
increase the ionization under the acidic conditions. This can be
done by adding electron withdrawing group on the sulfonamide
side chain
13. Sulfonamide derivatives
• Differ mainly in the substitution at the sulfonamide side chain…
derivatives with heterocyclic or aromatic ring. This was done to:
– Reduce the pKa of the sulfonamide... Reduce crystalluria.
– Increase protein binding by adding lipophilic heterocycles….
Long lasting derivatives.
• Few derivatives have the amino group at the P position being
derivatized except in sulfonamide prodrugs
14. Nomenclature of sulfonamides
• The sulfonamide termination is used for p-aminobenzene
sulfonamide (sulfanilamide) derivatives. The generic nomenclature is
made by combining the N1- residue together with the sulphate prefix.
such as Sulfapyridine, Sulfaguanidine.
15. 15
General Synthesis of Sulfonamides
NH2 NH CO R
+ ClSO2OH
NH COR
SO2Cl
HNH2
RNH2
veya
NHCOR
SO2NH2
SO2NHR
-
veya
Hid.
SO2 NHR
H2N
sübstitüe sulfamid
1)
2)
anilin
HCOOH H
R
Ac2O CH3
ClCOOEt OEt
Cl
HONO2
Cl
NO2
HOSO3H
SO3
(oleum)
SO3H
NO2
PCl5
K2CO3
SO2Cl
NO2
klorobenzen
RNH2
Red.
1)
2)
16. 16
Classification by Therapeutic
Effect
*Systemic sulfonamides (used in systemic infections, especially in urinary
infections)
-Short-acting sulfonamides
-Moderately active sulfonamides
-Long acting sulfonamides
*Sulfonamides used in GI infections
*Sulfonamides used in ophthalmic infections
*Sulfonamides used in urinary infections
*Sulfonamides used in burn treatment
*Sulfonamides used in the treatment of vaginal infections
17. N H 2
S O 2 N H
O
N
C H 3
C H 3
Sulfisoxazole
A- Short-Acting Sulfonamides
They are absorbed fast. Their half-lives
are 4-7 hours. They are preferred for
systemic infections
N1- (3,4-dimethyl-5-isoxazolyl) sulfanilamide
5- (4-aminobenzensülfonamido) -2,3-dimethyl-isoxazole
19. B- Moderate Effect Sulfonamides
orta etki süreliler
Bileşik R Müstahzarlar
Sülfametoksazol
N1-(5-metil-3-
izoksazolil)sülfanilamit
Gantanol(roche)
Sülfadiazin
N1-(2-primidinil)sülfanilamit
Silvadiazin,Sulfatrim,Silvadene
Silverdin,Sulfadiazin,Ultradiazin
Pedidiyazin
Sülfafenazol
N1-(1-fenil-1H-1-pirazol-5-
il)sülfanilamit
Sülfamoksol
N1-(4,5-dimetil-1,3-oksazol-2-
il)sülfanilamit
They are absorbed and
discarded more slowly
than short-acting
sulfonamides.
Their half-lives are 10-
12 hours.
They are given twice a
day.
Use for long-term
treatment and
especially for urinary
infections.
20. C- Long Acting Sulfonamides
Stevens-Johnson syndrome is a rare serious complaint in which the skin and mucous membrane reacts
severely to the drug or infection
• Absorption of these derivatives is fast and their breakthrough is slow (More
lipophilic).
• Their half-lives are 35-40 hours
• Long-acting sulfonamides are given once or twice a day.
• These compounds are used only in special cases. Because;
-They do not have a clinical advantage over short acting sulfonamides.
-They can not pass blood-brain barrier as easily as short-acting sulfonamides
• They can reach dangerous concentration because they are slowly taken away.
• Therefore, attention should be paid especially to patients with poor renal
function.
• Due to these reasons and some side effects such as Stevens-Johnson syndrome, it
has been removed from U.S. therapy today.
21. Uzun etki süreliler
Bileşik R Müstahzarlar
Sülfadimetoksin
N1-(2,6-dimetoksi-
4-
primidinil)sülfanila
mit
Duramid(Dev
a)
Sülfadoksin
N1-(5,6-dimetoksi-
4-
primidinil)sülfanila
mit
Fanasil(roche)
Sülfametoksidiazin
N1-(5-metoksi-2-
primidinil)sülfanila
mit
Sülfametomidin
N1-(6-metoksi-2-
metil-4-
primidinil)sülfanila
mit
Sülfametoksipiridaz
in
N1-(6-metoksi-3-
pridizanil)sülfanila
mit
Depo-
sulfon(Öztürk)
Metamit(Yavu
z)
Sülfaperin
N1-(5-metil2-
primidinil)sülfanila
mit
Sülfalen
N1-(4-
metoksiprimidin-5-
il)sülfanilamit
C- Long Acting Sulfonamides
22. Sulfonamides Used in Gastrointestinal Infection
• Hydrophilic groups are attached to the free amino group to increase water solubility
of these drugs.
• Due to the presence of hydrophilic groups such as maleyl, succinyl, it is less
absorbed from the gastrointestinal tract.
• This leads to a high concentration in the colon lumen. Bacterial hydrolysis occurs in
the colon lumen resulting in active sulphonamide structure.
23. Sulfonamides Used in Gastrointestinal Infection
Sulfasalazine
Composed of salicylic acid
and sulpyridine.
In the intestine,
sulphapyridine and 5-
aminosalicylic acid are
separated.
Therefore, both anti-
inflammatory and
antibacterial effects occur.
Use for thick intestinal
inflammation.
24. Sulfonamides Used in Ophthalmic Infections
They are used topically in conjunctivitis and similar ocular
infections.
Sülfadikramit
3-Metil-N-sülfanililkrotonamit
H 2 N SO 2 N COCH 3
Na
N
1
-A se tilsü lfa nila m it so d yum
Sulfacetamide Sodium:
Sodium salt is used in ophthalmic
infections as it is in good solubility at
physiological pH (7.4)
25. Sulfonamides Used in Burn Treatment
Mafenit
Since it is not a true sulfonamide type, it is not inhibited by PABA.
Therefore, the mechanism of antibacterial action differs from the
others. It is not used orally. It is used alone or in combination with
antibiotics in the treatment of infected burns.
Silver Sulphadiazine
•4-amino-N-pyrimidin-2-yl-benzenesulfonamide
Silver [(4-aminophenyl) sulfonyl]
(pyrimidin-2-yl) azanide
4- (aminomethyl) benzenesulfonamide
It is used topically in the form of water-miscible cream, especially for
the treatment of infections caused by pseudomonas species. This is
very important in the treatment of burns because, if it fails,
pesudomonas infection is often developing.
26. Sulfonamides Used in Urinary Infection
• The sulfonamides in this group are preferred because of their rapid absorption
and slow release from the kidneys, which leads to high concentrations in the
kidneys.
• Sulfacytin, sulfamethoxazole, sulfamethisole, sulfisoxazole are preferred because
they are relatively reliable, well tolerated, highly concentrated in urine, and
therefore low in crystallinity risk.
4-Amino-N- (5-methylisoxazole-3-yl) -benzenesulfonamide
Sulphamethoxazole
27. 27
Sulfamethoxazole with trimethoprim in 5: 1
Tablets contain 400 mg of sulfamethoxazole plus 80 mg of trimethoprim.
Trimetoprim inhibits the enzyme dihydrofolic acid reductase and exhibits
bacteriostatic activity.
Ko-trimoxazole Baktrim / Bakton / Septrin
(Gantanol) Trimetoprim
Sulfametoxazol
+
OCH3
H3CO
H3CO
N
N NH2
NH2
N
O
CH3
H2N SO2NH
Baktrisid/Kemoprim/Sulfatrim
5- (3,4,5-trimethoxybenzyl)
-2,4-diaminopyrimidine
CO-TRİMOXAZOLE
28. CO-TRİMOXAZOLE
Since the biochemical event necessary for the bacteria is blocked from two separate
points, the synthesis of purine in the bacteria is disrupted. This results in a
bactericidal effect.
This compound is used in urinary tract, respiratory tract and prostate infections.
Ca-trimoxazole users should not be given sodium bicarbonate (Sulfametoxazole is
acidic, Trimetoprim is basic) because urine chalevilization changes the outcome of
the compound in the opposite direction.
30. Sulfonamides Used in the Treatment of Vaginal
Infections
• Sulfabenzamide + Sulfacetamide + Sulfathiazole used in mixture.
Sulfathiazole
Sulfabenzamide
Sulfacetamide
4-Amino-N-benzoyl-benzenesulphonamide
N1-Benzoilsülfanilamit