This document discusses various aminoglycoside, macrolide, and chloramphenicol antibiotics. It provides details on streptomycin, an aminoglycoside antibiotic derived from Streptomyces griseus. It describes the chemical structure and classification of aminoglycosides. Common side effects of aminoglycosides include ototoxicity and nephrotoxicity. Macrolides like erythromycin work by binding to bacterial ribosomes and inhibiting protein synthesis. Chloramphenicol is a broad-spectrum antibiotic that works by inhibiting bacterial ribosomes. Rifampicin is a semi-synthetic rifamycin antibiotic used to treat tuberculosis and leprosy by inhibiting bacterial DNA-dependent RNA polymerase.
-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.
These are antibiotics having a macrocyclic
lactone ring with attached sugars. Erythromycin
is the first member discovered in the 1950s,
Roxithromycin, Clarithromycin and Azithromycin
are the later additions. Antimicrobial spectrum is narrow,
includes mostly gram-positive and a few gramnegative
bacteria, and overlaps considerably with
that of penicillin G. Erythromycin is highly active
against Str. pyogenes and Str. pneumoniae, N.
gonorrhoeae, Clostridia, C. diphtheriae and
Listeria, but penicillin-resistant Staphylococci
and Streptococci are now resistant to erythromycin
also.
All cocci readily develop resistance
to erythromycin, mostly by acquiring the
capacity to pump it out. Resistant Enterobacteriaceae
have been found to produce an erythromycin
esterase. Alteration in the ribosomal binding
site for erythromycin by a plasmid encoded
methylase enzyme is an important mechanism of
resistance in gram-positive bacteria. All the above
types of resistance are plasmid mediated. Change
in the 50S ribosome by chromosomal mutation
reducing macrolide binding a
-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.
These are antibiotics having a macrocyclic
lactone ring with attached sugars. Erythromycin
is the first member discovered in the 1950s,
Roxithromycin, Clarithromycin and Azithromycin
are the later additions. Antimicrobial spectrum is narrow,
includes mostly gram-positive and a few gramnegative
bacteria, and overlaps considerably with
that of penicillin G. Erythromycin is highly active
against Str. pyogenes and Str. pneumoniae, N.
gonorrhoeae, Clostridia, C. diphtheriae and
Listeria, but penicillin-resistant Staphylococci
and Streptococci are now resistant to erythromycin
also.
All cocci readily develop resistance
to erythromycin, mostly by acquiring the
capacity to pump it out. Resistant Enterobacteriaceae
have been found to produce an erythromycin
esterase. Alteration in the ribosomal binding
site for erythromycin by a plasmid encoded
methylase enzyme is an important mechanism of
resistance in gram-positive bacteria. All the above
types of resistance are plasmid mediated. Change
in the 50S ribosome by chromosomal mutation
reducing macrolide binding a
This ppt contains information on the classification, structures, uses and SAR related to macrolide antibiotics, lincomycins and chloramphenicol. It was prepared according to PCI syllabus for B.Pharma graduates
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.
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
THIS PRESENTATION ABOUT ANTIMALARIAL DRUGS DETAILING THE COMPLETE INFORMATION ABOUT THE DRUGS USED WITH ITS MECHANISM OF ACTION, STRUCTURAL ACTIVITY AND DOSES.
This ppt contains information on the classification, structures, uses and SAR related to macrolide antibiotics, lincomycins and chloramphenicol. It was prepared according to PCI syllabus for B.Pharma graduates
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.
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
THIS PRESENTATION ABOUT ANTIMALARIAL DRUGS DETAILING THE COMPLETE INFORMATION ABOUT THE DRUGS USED WITH ITS MECHANISM OF ACTION, STRUCTURAL ACTIVITY AND DOSES.
This presentation is ment to train Paramedicals & persons seeking health information. It is enjoyable to learn What & How about Vitamin A & its Role in Human Body. it educate general people in very palatable forms.
Antibiotics,antibiotics resistances,classification of antibiotics,misuse of antibiotics details discussed here. for more information visit my blog helpful for pharmacy and medical student.thanks.
http://mydreamlan.wordpress.com/category/education/
Brief information about Tuberculosis, drugs used for its treatment including recent advances and drug regimen for patients of different categories of TB suggested by WHO (DOTS therapy) including national and international programes for preventing TB.
Anthelmintics | B.Pharm 3rd year 2nd Sem | Medicinal Chemistry-III | History, Classification, Structures & Synthesis of anthelmintics, Synthesis of Diethylcarbamazine citrate, Synthesis of Mebendazole
B.Pharm I Year II Sem. SN1 and SN2 reactions, kinetics, order of reactivity of alkyl halides, stereochemistry and rearrangement of carbocations.
SN1 versus SN2 reactions, Factors affecting SN1 and SN2 reactions.
Structure and uses of ethylchloride, Chloroform, trichloroethylene, tetrachloroethylene,
dichloromethane, tetrachloromethane and iodoform.
Alcohols, Qualitative tests for Alcohol, Structure and uses of Ethyl alcohol, chlorobutanol, Cetosterylalcohol, Benzyl alcohol, Glycerol, Propylene glycol
Classification and Synthesis of Sulpha drugs, Anti Viral Drugs, Anti Fungal Agents, Anti Tubercular Agents, Anti leprotic Agents, Antiamoebic Agents, Anthelmintics, Anti Malarial Drugs, Anti cancer Drugs
Steroid hormones can be grouped into 2 classes, corticosteroids (typically made in the adrenal cortex, hence cortico-) and sex steroids (typically made in the gonads or placenta).
Anticancer Drug, also called Anti-Neoplastic drug, that is effective in the treatment of malignant, or cancerous, disease. There are several major classes of anticancer drugs; these include Alkylating Agents, Anti-metabolites, Plant Alkaloids and Hormones.
- 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
- Link to NephroTube website: www.NephroTube.com
- Link to NephroTube social media accounts: https://nephrotube.blogspot.com/p/join-nephrotube-on-social-media.html
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.
Recomendações da OMS sobre cuidados maternos e neonatais para uma experiência pós-natal positiva.
Em consonância com os ODS – Objetivos do Desenvolvimento Sustentável e a Estratégia Global para a Saúde das Mulheres, Crianças e Adolescentes, e aplicando uma abordagem baseada nos direitos humanos, os esforços de cuidados pós-natais devem expandir-se para além da cobertura e da simples sobrevivência, de modo a incluir cuidados de qualidade.
Estas diretrizes visam melhorar a qualidade dos cuidados pós-natais essenciais e de rotina prestados às mulheres e aos recém-nascidos, com o objetivo final de melhorar a saúde e o bem-estar materno e neonatal.
Uma “experiência pós-natal positiva” é um resultado importante para todas as mulheres que dão à luz e para os seus recém-nascidos, estabelecendo as bases para a melhoria da saúde e do bem-estar a curto e longo prazo. Uma experiência pós-natal positiva é definida como aquela em que as mulheres, pessoas que gestam, os recém-nascidos, os casais, os pais, os cuidadores e as famílias recebem informação consistente, garantia e apoio de profissionais de saúde motivados; e onde um sistema de saúde flexível e com recursos reconheça as necessidades das mulheres e dos bebês e respeite o seu contexto cultural.
Estas diretrizes consolidadas apresentam algumas recomendações novas e já bem fundamentadas sobre cuidados pós-natais de rotina para mulheres e neonatos que recebem cuidados no pós-parto em unidades de saúde ou na comunidade, independentemente dos recursos disponíveis.
É fornecido um conjunto abrangente de recomendações para cuidados durante o período puerperal, com ênfase nos cuidados essenciais que todas as mulheres e recém-nascidos devem receber, e com a devida atenção à qualidade dos cuidados; isto é, a entrega e a experiência do cuidado recebido. Estas diretrizes atualizam e ampliam as recomendações da OMS de 2014 sobre cuidados pós-natais da mãe e do recém-nascido e complementam as atuais diretrizes da OMS sobre a gestão de complicações pós-natais.
O estabelecimento da amamentação e o manejo das principais intercorrências é contemplada.
Recomendamos muito.
Vamos discutir essas recomendações no nosso curso de pós-graduação em Aleitamento no Instituto Ciclos.
Esta publicação só está disponível em inglês até o momento.
Prof. Marcus Renato de Carvalho
www.agostodourado.com
These simplified slides by Dr. Sidra Arshad present an overview of the non-respiratory functions of the respiratory tract.
Learning objectives:
1. Enlist the non-respiratory functions of the respiratory tract
2. Briefly explain how these functions are carried out
3. Discuss the significance of dead space
4. Differentiate between minute ventilation and alveolar ventilation
5. Describe the cough and sneeze reflexes
Study Resources:
1. Chapter 39, Guyton and Hall Textbook of Medical Physiology, 14th edition
2. Chapter 34, Ganong’s Review of Medical Physiology, 26th edition
3. Chapter 17, Human Physiology by Lauralee Sherwood, 9th edition
4. Non-respiratory functions of the lungs https://academic.oup.com/bjaed/article/13/3/98/278874
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.
NVBDCP.pptx Nation vector borne disease control programSapna Thakur
NVBDCP was launched in 2003-2004 . Vector-Borne Disease: Disease that results from an infection transmitted to humans and other animals by blood-feeding arthropods, such as mosquitoes, ticks, and fleas. Examples of vector-borne diseases include Dengue fever, West Nile Virus, Lyme disease, and malaria.
Pulmonary Thromboembolism - etilogy, types, medical- Surgical and nursing man...VarunMahajani
Disruption of blood supply to lung alveoli due to blockage of one or more pulmonary blood vessels is called as Pulmonary thromboembolism. In this presentation we will discuss its causes, types and its management in depth.
HOT NEW PRODUCT! BIG SALES FAST SHIPPING NOW FROM CHINA!! EU KU DB BK substit...GL Anaacs
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We specializes in exporting high quality Research chemical, medical intermediate, Pharmaceutical chemicals and so on. Products are exported to USA, Canada, France, Korea, Japan,Russia, Southeast Asia and other countries.
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.
Ethanol (CH3CH2OH), or beverage alcohol, is a two-carbon alcohol
that is rapidly distributed in the body and brain. Ethanol alters many
neurochemical systems and has rewarding and addictive properties. It
is the oldest recreational drug and likely contributes to more morbidity,
mortality, and public health costs than all illicit drugs combined. The
5th edition of the Diagnostic and Statistical Manual of Mental Disorders
(DSM-5) integrates alcohol abuse and alcohol dependence into a single
disorder called alcohol use disorder (AUD), with mild, moderate,
and severe subclassifications (American Psychiatric Association, 2013).
In the DSM-5, all types of substance abuse and dependence have been
combined into a single substance use disorder (SUD) on a continuum
from mild to severe. A diagnosis of AUD requires that at least two of
the 11 DSM-5 behaviors be present within a 12-month period (mild
AUD: 2–3 criteria; moderate AUD: 4–5 criteria; severe AUD: 6–11 criteria).
The four main behavioral effects of AUD are impaired control over
drinking, negative social consequences, risky use, and altered physiological
effects (tolerance, withdrawal). This chapter presents an overview
of the prevalence and harmful consequences of AUD in the U.S.,
the systemic nature of the disease, neurocircuitry and stages of AUD,
comorbidities, fetal alcohol spectrum disorders, genetic risk factors, and
pharmacotherapies for AUD.
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
How to Give Better Lectures: Some Tips for Doctors
Antibiotics
1. Chilkur Balaji College of Pharmacy
R.V.S Nagar, Aziz Nagar, Moinabad.
S.SEETARAM SWAMY, M.Pharm.,
Asst. professor,
Dept. of Pharmaceutical Chemistry,
Chilkur Balaji College of Pharmacy.
E-mail:seetaram.443@gmail.com
Aminoglycosides, Macrolide, Chloramphenicol
2. Antibiotics are substances produced by microorganisms, which selectively
suppress the growth of or kill other microorganism at very low
concentration.
CONTENTS
1. Aminoglycosides
a) Introduction
b) Mechanism of action
c) Toxicity
d) Therapeutic uses
2. Macrolides
3. Chlorampehenicol
4. Rifampicin
3. o Amino glycoside antibiotics contain an amino cyclitol moiety to which amino sugars
are linked glycosidically.
o They may be more correctly called aminocyclitol antibiotics.
o Aminoglycosides are a group of antibiotics effictive against gram+ve and gram-ve
organisms as well as micoplasma.
o Most of the aminoglycosides antibiotics are dirived from genus streptomycesspecies,
important one is streptomycin.
o Aminoglycoside antibiotics are also referred as aminocyclitol antibiotics, because they
consist of a highly substituted ring called aminocyclitol ring i.e.1,3 di amino cyclohexane
central ring.
o All Aminoglycosides in this class possess one amino hexose sugar. But some antibiotics
like streptomycin, neomycin, paramomycin possess a pentose sugar.
AMINOGLYCOSIDES
5. STREPTOMYCIN
Streptomycin is the first aminoglycoside antibiotic which
was isolated from the actinomycetes bacteria
STREPTOMYCES GRISEUS and several related soil
microorganisms.
Streptomycin was first discovered in 1943 by SELMAN
ABRAHAM WAKESMAN and received a Nobel prize in 1952.
It was introduced primarily for the treatment of
tuberculosis.
Chemistry:
Physico-chemical properties:
Colour : colourless.
Odour : odourless.
State : Streptomycin sulphate and streptomycin chloride
available in the form of white powdery solid.
Solubility : Easily soluble in water insoluble in acetone.
Stability : It is stable at a temp. less than 28 ̊C and solutions
of streptomycin are stable at pH (4.5-7).
6. Streptomycin is made up of 3 basic structural units called…
1. Streptidine(a diguanidino compound)
2. Streptose (a aldose sugar)
3. N-methyl-L-glucosamine.
O
H
OH
H
H
CH2OH
HOH
NHCH3
O
OH
CHO
CH3
H OH
H
H NH.C.NH2
H
H
OHH
OH
HNH.C.NH2
H OH
O
NH
NH
N-methyl-L-glucosamine
Streptose
Streptidine
8. DIHYDROSTREPTOMYCIN
The only difference in the structure of streptomycin and dihydrostreptomycin is
the presence of a hydroxyl alcoholic group(-CH20H) in place of –CHO group of
Streptose moiety (the –CHO group of streptomycin is replaced by –CH2OH group).
It is a semi-synthetic derivative obtained by the catalytic hydrogenation of
Streptomycin.
It has similar mechanism of action, pharmacokinetic aspects and toxicological
properties as that of streptomycin.
9. IMPORTANCE OF DIHYDROSTREPTOMYCIN:
Treatment of tuberculosis in various animals.
It is less neurotoxic than streptomycin but high
frequency of ototoxicity in humans.
It is used in combination with procaine penicillin
to treat systemic infections.
It is not recommended for humans as it is
ototoxic and hence mostly used for veterinary
purposes for the treatment of systemic
infections.
11. • Aminoglycosides binds to specific 30S – 50S subunit ribosomal proteins.
Protein synthesis is inhibited by them in at least three ways:
1.They Block the formation of initiation 70S ribosomal
mRNA complex
2.They induce misreading of the code on the mRNA template
Causes incorporation of incorrect amino acids into peptide
resulting in a nonfunctional or abnormal protein synthesis.
3.Inhibit translocation
11
MECHANISM OF ACTION
12. A. Ototoxicity
Auditory (Loss of hearing) or vestibular
damage(dizziness, vertigo) or both.
Neomycin, kanamycin, and amikacin
are the most ototoxic drugs,
Streptomycin and gentamicin are the
most vestibulo toxic.
B. Nephrotoxicity
Aminoglycosides are mainly excreted by
glomerular filtration and can be stored
up in kidney. It can cause acute renal
insufficiency and tubular necrosis.
Neomycin is the most nephrotoxic drug,
streptomycin is the least one.
C. Neuromuscular blockade
D. Skin reactions (Hypersensitivity
reactions)
Skin rash, fever, eosinophilia and
anaphylactic shock. 12
TOXICITY
14. Macrolide antibiotics are so named as they possess a macrocyclic lactone usually
having 12 to 17 atoms.
3 common chemical features they are:
1. a macro cyclic lactone, usually having 12 to 17 atoms
2. a ketone group.
3. One or two amino-sugars linked to the nucleus.
MACROLIDES
Macrolide antibiotics contain a many-membered lactone ring (14-membered rings for
erythromycin & clarithromycin and a 15-membered ring for azithromycin).
SOURCE:
These are produced by streptomyces
species and the products of
actinomycetes.
The presence of the dimethyl amino moiety on the sugar residue, which explains the
basicity of these compounds and consequently formation salts.
19. Chloramphenicol / Chloromycetin is a broad spectrum antibiotic
isolated from Streptomyces venezuelae.
It has a nitrobenzene moiety that is responsible for antibacterial
activity and the bitter taste.
CHLORAMPHENICOL
SPECTRUM OF ACTIVITY:
Active against S. typhi, H. influenzae, S. pneumoniae, B. fragilis.
Less active against Chlamydia, Spirochetes while more against Klebsiella, B. pertussis.
20. 1. Chloramphenicol is a bacteriostatic by inhibiting protein synthesis.
2. It prevents protein chain elongation by inhibiting the peptidyl transferase
activity of the bacterial ribosome.
3. Inhibits protein synthesis by binding to 50 S ribosomal subunit of the microbe.
MECHANISIM OF ACTION
21. CO2N
O
CH3
Br2/CH3COOH
Bromination
NO2 C
H2
C
O
Br
Hexamine
O2N C
H2
C
O
NH2
O2N C CH2
O HN C CH3
O
Acetylation
(CH3CO)2O
O2N C C
H
O
CH2
HN C CH3
OH
HCHO
O2N
H
C
OH
C
H
HN
CH2
C
OH
CH3
O
Aluminium
isopropoxide
H
C
OH
C
H
NH2
CH2
OH
HCl/H2O
O2N
H2
C C
H
NHCOCHCl2
CH2
OH
O2N
Chloramphenicol
Chloroacetyl
chloride
Hydrolysis
Cl2CHCOCl
O
p-nitro acetophenone
Synthesis of Chloramphenicol
22. 1. Bone marrow toxicity
a) Bone marrow suppression
b) Aplastic anemia
2. Gray baby syndrome
3. Hypersensitivity reactions
4. Neurotoxic reactions
5. Leukemia
ADVERSE EFFECTES
23. THERAPEUTIC USES
1. Chloramphenicol has a wide range activity that includes gram+, gram-, aerobic
and anaerobic bacteria
2. Typhoid Fever ( Salmonella typhi)
3. Bacterial Meningitis (Chloramphenicol is active against the three main bacterial
causes of meningitis: Neisseria meningitidis, Streptococcus pneumoniae, and
Haemophilus influenzae)
4. Anaerobic Infections
5. Rickettsial Diseases
6. Brucellosis
24. Refamycins are a group of macrocyclic antibiotics which are produced by Streptomyces
mediterranei.
Eventually 7 rifamycins were developed they are Rifamycin A,B,C,D,E,S,SV.
Refampicin is a semi-synthetic rifamycin made from Rifamycin-B isolated from
STREPTOMYCES MEDITERRANEI in 1957.
Among the various rifamycins, rifamycin-B was the first Commercial product.
REFAMPICIN
25. It acts by inhibiting DNA-dependent RNA polymerase(DDRP)of mycobacteria and
other microorganisms by binding strongly to their β-subunits viz ( α, α1, β, β1 and
sigma) and there by suppression of inhibiting the m-RNA synthesis
Refamycins inhibit the enzyme RNA polymerase and prevent RNA synthesis. Than in
turn prevent protein synthesis.
So they are useful in treating tuberculosis, leprosy, Mycobacterium avium complex
(MAC) infection and Staphylococcus infections.
MECHANISIM OF ACTION
26. Hepatotoxic - hepatitis, liver failure in severe cases
Respiratory – breathlessness
Abdominal - nausea, vomiting, abdominal cramps.
Flu-like symptoms - with chills, fever, headache.
Certain bodily fluids, such as urine and tears, to become orange-red in color.
ADVERSE EFFECTES
27. Refampicin is used as a first line drug in the treatment of
tuberculosis. As most of the tubercle bacilli develop resistance to
Refampicin. It is used in combination with other anti-tubercular
drugs in the MULTIPLE DRUG THERAPY to minimize the problem.
It is also used the treatment of leprosy.
Infection like endocarditis (inflammation of membrane lining
the heart.)
Oesteomyelitis(inflammation of bone)
It is used in the first-line therapy of brucellosis in combination
with doxycline.
It is also an excellent drug for Pneumonia.
It is also used in combination with dapsone in Treating leprosy.
THERAPEUTIC USES
28. Most species of bacteria develop resistance to Refampicin.
Use of single drug Refampicin for tuberculosis will not be effective.
That’s why it is used in combination with other anti-tubercular drugs in multidrug
therapy.
Drugs used most commonly to treat TB include Isoniazid, Refampicin, Ethambutol and
Pyrazinamide.
MULTI DRUG THERAPY (MDT)
29. Two phases of drug therapy are generally used:
Initial phase: In this phase 3 drugs namely Refampicin, isoniazid, Pyrazinamide are
used. some times ethambutol drug is used .
All these drugs used for 2 months. (e.g: AKT4)
Continuation phase:-Two drugs i.e. Refampicin and isoniazid are to be used for a time
period of the next 4months. (e.g: R-Cinex-600)