RIFAMPICIN SOURCE, STRUCTURES,MECHANISM OF ACTION,SAR,RIFAMYCINS, USES HOW T.B IS TREATED?
BY P. RAVISANKAR
VIGNAN PHARMACY COLLEGE
VADLAMUDI
GUNTUR,
ANDHRA PRADESH
INDIA.
THIS PRESENTATION ABOUT ANTIMALARIAL DRUGS DETAILING THE COMPLETE INFORMATION ABOUT THE DRUGS USED WITH ITS MECHANISM OF ACTION, STRUCTURAL ACTIVITY AND DOSES.
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thank you, all the respected peoples, for giving the information to complete this presentation.
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THIS PRESENTATION ABOUT ANTIMALARIAL DRUGS DETAILING THE COMPLETE INFORMATION ABOUT THE DRUGS USED WITH ITS MECHANISM OF ACTION, STRUCTURAL ACTIVITY AND DOSES.
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.
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watch video:https://www.youtube.com/watch?v=v3rI1lf2TZ8&t=403s
This slide describes the Important Synthesis of Antiviral 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.
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.
It is the presentation for Combinatorial Chemistry. this presentation should be helpful for B. Pharm students. It includes introduction, types, applications, advantages and disadvantages.
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
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.
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.
It is the presentation for Combinatorial Chemistry. this presentation should be helpful for B. Pharm students. It includes introduction, types, applications, advantages and disadvantages.
VLE Data - Selection and Use
0 INTRODUCTION/PURPOSE
1 SCOPE
2 FIELD OF APPLICATION
3 DEFINITIONS
4 DIAGRAMMATIC REPRESENTATION OF IDEAL
AND NON-IDEAL SYSTEMS
4.1 Ideal Mixtures
4.2 Non-Ideal Mixtures
5 REVIEW OF VLE MODELS
5.1 Ideal Behavior in Both Phases
5.2 Liquid Phase Non-Idealities
5.3 High Pressure Systems
5.4 Special Models
6 SETTING UP A VLE MODEL
6.1 Define Problem
6.2 Select Data
6.3 Select Correlation(s)
6.4 Produce Model
7 AVOIDING PITFALLS
7.1 Experimental Data is Better than Estimates
7.2 Check Validity of Fitted Model
7.3 Check Limitations of Estimation Methods
7.4 Know Your System
7.5 Appreciate Errors and Effects
7.6 If in Doubt – Ask
8 A CASE STUDY
8.1 The Problem
8.2 The System
8.3 Data Available
8.4 Selected Correlation
8.5 Simulation
8.6 Selection of Model
9 RECOMMENDED READING
10 VLE EXPERTS IN GBHE
APPENDICES
A USE OF EXTENDED ANTOINE EQUATION
B USE OF WILSON EQUATION
C USEFUL METHODS OF ESTIMATING
D EQUATIONS OF STATE FOR VLE CALCULATIONS
TABLES
1 SUMMARY OF VLE METHODS
2 LIST OF USEFUL REFERENCES
FIGURES
1 VAPOR-LIQUID EQUILIBRIUM - IDEAL SOLUTION
BEHAVIOR
2 VAPOR-LIQUID EQUILIBRIUM - A GENERALISED
Y-X DIAGRAM
3 VAPOR-LIQUID EQUILIBRIUM - MINIMUM BOILING
AZEOTROPE
4 VAPOR-LIQUID EQUILIBRIUM - MAXIMUM BOILING
AZEOTROPE
5 VAPOR-LIQUID EQUILIBRIUM - MINIMUM BOILING
AZEOTROPE -TWO LIQUID PHASES
6 SENSITIVITY TO ERROR IN VLE DATA (BASED ON FENSKE EQUATION)
7(a) FITTING WILSON 'A' VALUES TO VLE DATA - CASE A
7(b) FITTING WILSON 'A' VALUES TO VLE DATA - CASE B
7(c) FITTING WILSON 'A' VALUES TO VLE DATA - CASE C
SUBJECT:-Pharmaceutical engineering 1
CONTENTS
-general study of composition
-properties
factors affecting the selection of material of pharmaceutical plant
-construction with special reference to S.S and glass
Human population and environment chapter 2Nayan Vaghela
Human population and environment chapter 2, variations in population growth, air borne diseases, HIV/AIDS, television, radio, news paper, internet, computer, cancer
Tetracyclines BY Dr. P. Ravisankar M. Pharm., Ph.D.Dr. Ravi Sankar
Tetracyclines by Dr. P. Ravisankar M. Pharm., Ph.D.
Definition
Introduction
Classification
Historical background
Sources
Chemistry
SAR of tetracyclines
Mechanism of action of tetracyclines
Spectrum of activity
Uses of tetracyclines
Side effects of tetracyclines
Leprosy
Tuberculosis
TYB pharmacy
Pharmacology semester VI notes
Pharmacology VI semester
Pharmacology notes
Third year B pharmacy pharmacology notes
Pharmacology unit 3 notes
Pharmacology VI semester notes
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.
Tuberculosis is completely curable disease now a days but one should follow the treatment regimens correctly .so for under graduate MBBS students it is clearly explained with animations.Hope you all this will be helpful.
Anti mycobacterial drugs (tuberculosis drugs)Ravish Yadav
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.
All new antibacterial agents which have been approved after the year 2000 have been described along with their mechanism of action, development of resistance, spectrum of activity and the stage of developmental in case of yet to be approved drugs.
Similar to RIFAMPICIN [MEDICINAL CHEMISTRY] BY P.RAVISANKAR. (20)
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Finally, one of the best ways of reducing cancer is …..
Cancer prevention is an essential component of all cancer control plans because about 40 % of cancers are preventable.
Firstly…Public education campaigns are important in highlighting the dangers of smoking because possibly as many as 22 % (in the UK 30%) of cancers are caused by smoking.
Secondly, another 30% of cancers are diet-related. Decades of research have clearly shown that by living a healthy life, people can reduce the risk of developing the disease.
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2. Rifampicin (Rifampin)
•Refamycins are a group of macrocyclic antibiotics which are
Produced by Streptomyces mediterranei.
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.
•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.
3. Mechanism/mode of action:
Refampin is bactericidal at 0.005-0.2micrograms/ml vs
Micobacterium tuberculosis.
Rifampicin inhibits Grampositive bacteria and works by
Binding non-covalently to DNA-dependent RNA polymerase
and inhibiting the start of RNA synthesis
The DNA-dependent RNA polymerases in eukaryotic cells
are unaffected, since the drug binds to a peptide chain not
Present in the mamalian RNA polymerase. Therefore it is
highlyselective..
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 supression of inhibiting the m-RNA synthesis
4. •Intact macrocyclic molecule is required for antimycobacterial activity.
•Double bonds in macrocyclic ring should not be redcuced ,or opening of the macro ring
results in compounds have decreased activity.
• Free hydroxyl groups should be present at c-1,c-8,c-21,c-23 all lie in a plane and play a
role in acting as binding groups for attachment to DDRP.
• When –OH groups at c-21 and c-23 were completely removed or substituted the
formation of derivatives are devoid of anti-mycrobial activity were obtained.
•Activity of the compounds get diminished when the –OH groups at c21 and c23 are
acetylated.
• The maintenance of drug activity relies on the presence of either –OH or carbonyl
group
both of which should be unsubstituted.
•Refampicin compound is formed by substitution of [(4-methyl-1piperazinyl)imino)methyl]
at 3rd
position in rifamycin-B. It is a bactericidal antibiotic of Refamycin group and it
Flat naphthalene ring and
Several of the –OH groups
Are essential for activity.
It is a zwitterion, and has good
Solubility both lipids and aqueous acid.
7. Uses:-
• Refampicin is used as a first line drug in the treatment of tuberculosis. As
most of the tubercle bacilli develop resistance to rifampicin. It is used in
combination with other anti-tubercular drugs in the multiple drug therapy to
minimize the problum.
• It is also used the treatment of leprosy.
• Infection like endocarditis(inflammation of membrane lining the heart.)
• For prophylaxis in people exposed to meningococcemia or H. influenzae type
B meningitis.
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 an active inducer of hepatic cytochrome P450 oxygenases.
• It is also used in combination with dapsone in Treating leprosy.
• It is a very useful antibiotic, showing a high degre of selectivity
against bacterial cells over mammalian cells.
• Unfortunately, it is so expensive, which discourages its use against a
wide range of infections.
8. How is TB treated?How is TB treated?
Optimal treatment of TB utilizes a combination of 2 to 3 antibiotics taken over a
period of 6 to 9 months. Drug resistant strains of TB are not uncommon, which
is why multiple antibiotics are used together during treatment. Drugs used most
commonly to treat TB include isoniazid, rifampin, ethambutol, and
pyrazinamide7
.
9. Multidrug therapyMultidrug therapy
Most species of bacteria develop resistance to Rifampicin. Use of single drug
Refampicin for tuberculosis will not be effective. That’s why it is used in
Combination with other antitubercular drugs in multidrug therapy.
Each tablet contains
Genarally the following dosage regimen is given
Rifampicin----120mg.
Isoniazid ------50mg.
Pyrimethamine-300mg.
4 tablets/day for patients ≤ 44kg.
6 tablets /day for patients ≥ 55kg.
child dose:- 100mg/kg of body weight as a single dose.
2 phases of drug therapy are genarally 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.
Continuation phase:-
Two drugs i.e. Rifampicin and isoniazid are to be used for a time period of the next
4months. (2 times/week)
Isoniazid---15mg/kg(orally),Rifampicin—10mg/kg (upto60mg/dose).