Mycology is the study of fungi. The name “fungi” is derived from “mykos” meaning mushroom. The fungi are eukaryotic organisms and they differ from the bacteria, which are prokaryotic organisms, in many ways (Table 71-1). The fungi possess rigid cell walls, which possess two characteristic cell structures: chitin and ergosterol.
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.
Anti-Protozoal drugs/agents/drugs for protozoal infectionakhileshtiwari95
Antiprotozoal drugs are a class of medication used to treat infections caused by protozoa, which are single cell organisms that belong to the type of parasites.
Although Protozoal infections occur throughout the world and are a major cause of morbidity and mortality in some regions such as Africa and South-East Asia.
In the United States and other countries of the temperate zone, protozoal diseases are of minor importance.
Protozoal diseases are highly prevalent in tropical Third World countries,
where they infect both human and animal populations.
anthelmintics Parasitic infections are caused by organisms that live and feed...akhileshtiwari95
Parasitic infections are caused by organisms that live and feed off another organism, known as the host, often causing harm in the process. These parasites can be single-celled organisms like protozoa or multicellular organisms like helminths (worms). Types of Parasitic Infections:
1. Protozoal Infections: Caused by single-celled organisms such as Plasmodium (malaria), Giardia lamblia (giardiasis), Entamoeba histolytica (amebiasis), and Trypanosoma (sleeping sickness, Chagas disease).
2. Helminthic Infections: Caused by parasitic worms including nematodes (roundworms), trematodes (flukes), and cestodes (tapeworms). Examples include Ascaris lumbricoides (roundworm), Schistosoma (schistosomiasis), and Taenia solium (tapeworm).
3. Ectoparasitic Infections: Caused by organisms that live on the external surface of the host's body, such as lice, fleas, ticks, and mites.
Combinatorial chemistry is a technique that allows for the rapid synthesis of large libraries of compounds with similar structures. It works by preparing many similar compounds simultaneously using the same reaction conditions, rather than synthesizing compounds one at a time. The goal is to efficiently build up a large collection of molecules that can then be screened for biological activity against specific targets. Key methods for combinatorial chemistry include solid phase synthesis, solution phase synthesis, and the use of beads, pins, or "tea bags" to track compounds during parallel reactions. This approach has been successful in identifying new lead compounds for conditions like HIV and cancer.
This document provides information about quinolones, a class of urinary tract anti-infective agents. It lists nalidixic acid, norfloxacin, enoxacin, ciprofloxacin, ofloxacin, lomefloxacin, and sparfloxacin as examples of quinolones. Quinolones are chemically classified as naphthyridines, such as nalidixic acid, or cinoxines and quinolines like various floxacins. The document also discusses the mechanisms of phototoxicity of some quinolones and how they interact with topoisomerase enzymes in mammalian cells.
antiviral drugs medicinal chemistry by padala varaprasadVaraprasad Padala
medicinal chemistry of antiviral drugs by padala varaprasad
mainly includes structures, SAR , mechanism of action, uses and toxicity of antiviral drugs
Sulphonamides, MOA, SAR, History of development, Nomenclature of the Sulfonamides, Classification, Spectrum of Action of the Sulfonamides,Structure Activity Relationship, Reducing Toxicity, Cotrimoxazole
Macrolides are a group of antibiotics isolated from actinomycetes bacteria. The first macrolide identified was picromycin in 1950. Erythromycin and carbomycin were reported as new antibiotics in 1952. There are now over 40 known macrolide compounds.
Macrolides share three chemical characteristics - a large lactone ring, a ketone group, and a glycosidically linked amino sugar. The lactone ring typically has 12, 14 or 16 atoms and is often unsaturated with a conjugated olefinic group and ketone. Some macrolides also contain a neutral sugar linked to the lactone ring. They are basic compounds that form salts due to a dimethylamino group
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.
Anti-Protozoal drugs/agents/drugs for protozoal infectionakhileshtiwari95
Antiprotozoal drugs are a class of medication used to treat infections caused by protozoa, which are single cell organisms that belong to the type of parasites.
Although Protozoal infections occur throughout the world and are a major cause of morbidity and mortality in some regions such as Africa and South-East Asia.
In the United States and other countries of the temperate zone, protozoal diseases are of minor importance.
Protozoal diseases are highly prevalent in tropical Third World countries,
where they infect both human and animal populations.
anthelmintics Parasitic infections are caused by organisms that live and feed...akhileshtiwari95
Parasitic infections are caused by organisms that live and feed off another organism, known as the host, often causing harm in the process. These parasites can be single-celled organisms like protozoa or multicellular organisms like helminths (worms). Types of Parasitic Infections:
1. Protozoal Infections: Caused by single-celled organisms such as Plasmodium (malaria), Giardia lamblia (giardiasis), Entamoeba histolytica (amebiasis), and Trypanosoma (sleeping sickness, Chagas disease).
2. Helminthic Infections: Caused by parasitic worms including nematodes (roundworms), trematodes (flukes), and cestodes (tapeworms). Examples include Ascaris lumbricoides (roundworm), Schistosoma (schistosomiasis), and Taenia solium (tapeworm).
3. Ectoparasitic Infections: Caused by organisms that live on the external surface of the host's body, such as lice, fleas, ticks, and mites.
Combinatorial chemistry is a technique that allows for the rapid synthesis of large libraries of compounds with similar structures. It works by preparing many similar compounds simultaneously using the same reaction conditions, rather than synthesizing compounds one at a time. The goal is to efficiently build up a large collection of molecules that can then be screened for biological activity against specific targets. Key methods for combinatorial chemistry include solid phase synthesis, solution phase synthesis, and the use of beads, pins, or "tea bags" to track compounds during parallel reactions. This approach has been successful in identifying new lead compounds for conditions like HIV and cancer.
This document provides information about quinolones, a class of urinary tract anti-infective agents. It lists nalidixic acid, norfloxacin, enoxacin, ciprofloxacin, ofloxacin, lomefloxacin, and sparfloxacin as examples of quinolones. Quinolones are chemically classified as naphthyridines, such as nalidixic acid, or cinoxines and quinolines like various floxacins. The document also discusses the mechanisms of phototoxicity of some quinolones and how they interact with topoisomerase enzymes in mammalian cells.
antiviral drugs medicinal chemistry by padala varaprasadVaraprasad Padala
medicinal chemistry of antiviral drugs by padala varaprasad
mainly includes structures, SAR , mechanism of action, uses and toxicity of antiviral drugs
Sulphonamides, MOA, SAR, History of development, Nomenclature of the Sulfonamides, Classification, Spectrum of Action of the Sulfonamides,Structure Activity Relationship, Reducing Toxicity, Cotrimoxazole
Macrolides are a group of antibiotics isolated from actinomycetes bacteria. The first macrolide identified was picromycin in 1950. Erythromycin and carbomycin were reported as new antibiotics in 1952. There are now over 40 known macrolide compounds.
Macrolides share three chemical characteristics - a large lactone ring, a ketone group, and a glycosidically linked amino sugar. The lactone ring typically has 12, 14 or 16 atoms and is often unsaturated with a conjugated olefinic group and ketone. Some macrolides also contain a neutral sugar linked to the lactone ring. They are basic compounds that form salts due to a dimethylamino group
This document discusses aminoglycoside antibiotics. It describes their structure, including that they contain amino sugars linked to an aminocyclitol ring. Examples are provided such as streptomycin, kanamycin, neomycin, and gentamicin. Their broad-spectrum antibacterial activity against gram-negative bacteria is summarized. Toxicities like nephrotoxicity and ototoxicity limit their clinical use to serious infections.
Viruses are obligate intracellular parasites that invade host cells and hijack their machinery to replicate. Antiviral drugs work by inhibiting viral replication and development inside host cells. There are several classes of antiviral drugs including adamantane derivatives, purine nucleotides, and pyrimidine nucleotides. Acyclovir, a purine nucleotide, gets activated by viral thymidine kinase inside infected cells and competitively inhibits viral DNA polymerase or gets incorporated into viral DNA. Idoxuridine, a pyrimidine nucleotide, is phosphorylated and substitutes for thymidine during viral DNA synthesis, inhibiting the viral DNA polymerase enzyme. Antiviral drugs display specificity against certain viruses by exploiting differences between host and viral polymer
medicinal chemistry of Antiviral drugsFatenAlsadek
medicinal chemistry of antiviral drugs with its chemical structures and how they chemically work
Done by: Faten Al-Sadek , Pharmacy student at Mohammed Al-Mana college for Health Sciences -MACHS
Antiviral Agents,Medicinal Chemistry
•Introduction to Viruses
•Structure of Virus
•Types of Viruses.
•The viral Life cycle.
•Classification of Antiviral Agents
- Tetracyclines are a class of broad spectrum antibiotic drugs derived from bacteria. They work by binding to the bacterial ribosome to inhibit protein synthesis and show bacteriostatic activity.
- Structurally, they contain four cyclic rings. Modifications to the structure can impact their activity. They are classified based on their duration of action as long, intermediate, or short acting.
- Common examples include tetracycline, doxycycline, and minocycline. They are used to treat various bacterial infections but have side effects like nausea, vomiting, and tooth staining when taken.
This document provides information about quinolones, including their classification, mechanism of action, and examples of specific quinolones. It discusses the classification of quinolones as first, second, third, or fourth generation. It also summarizes the mechanisms of action, pharmacokinetic properties, uses, and adverse effects of several common quinolones like ciprofloxacin, norfloxacin, ofloxacin, and moxifloxacin. Finally, it mentions some quinolones currently under clinical trials.
This document discusses various classes of antibiotics - polyenes and polypeptides. It provides details about Amphotericin B, Nystatin, Hamycin in the polyene class and Bacitracin, Polymyxin-B, Colistin/Polymyxin-E, and Dactinomycin/Actinomycin-D in the polypeptide class. It describes their origins, mechanisms of action, therapeutic uses, dosages and adverse effects.
This document provides an overview of antiviral drugs, including their mechanisms of action, classifications, and examples. It discusses how antiviral drugs work by inhibiting viral replication and preventing the virus from multiplying, rather than destroying the pathogen. The main classes covered are nucleoside analogs, including purine and pyrimidine analogs like acyclovir and idoxuridine; non-nucleoside reverse transcriptase inhibitors like nevirapine; protease inhibitors used to treat HIV; and miscellaneous agents like foscarnet sodium. For each drug class, examples are given along with descriptions of their structures, mechanisms of action, therapeutic uses, and dosages.
This document summarizes information about two antiviral drugs - Loviride and Zalcitabine. Loviride is a non-nucleoside reverse transcriptase inhibitor that was tested in clinical trials but failed to receive approval. Zalcitabine is a nucleoside reverse transcriptase inhibitor sold under the brand name Hivid. It works by incorporating into viral DNA and terminating its growth. The document also provides details on the mechanisms of action, pharmacokinetics, side effects and uses of the two drugs.
This document discusses antifungal drugs. It begins by describing common fungal infections that antifungals treat, such as ringworm and athlete's foot. It then discusses the different types of fungal infections including superficial infections of the skin and internal organ infections. The document outlines the main biochemical targets of antifungals and describes the structure and mechanisms of several major classes of antifungal drugs, including azoles, polyenes like amphotericin B and nystatin, and the heterocyclic compound griseofulvin. It provides details on specific antifungals like their structures, mechanisms of action, uses, and side effects.
This document discusses several classes of antibiotics including tetracyclines, macrolides, chloramphenicol, and lincosamides. It describes the chemical structures, mechanisms of action, modes of resistance, and structure-activity relationships for these drug classes. Tetracyclines are broad-spectrum antibiotics derived from Streptomyces fermentation that work by inhibiting bacterial protein synthesis. Macrolides also inhibit bacterial protein synthesis by binding the 50S ribosomal subunit. Resistance to macrolides occurs through methylation of ribosomal RNA. Chloramphenicol obtained from Streptomyces inhibits bacterial protein synthesis. Clindamycin is a lincosamide derived from lincomycin with a chlorine substitution that
The document discusses urinary tract anti-infective agents. It notes that newer quinolones like ciprofloxacin, norfloxacin, and ofloxacin are effective against a wide range of gram-positive and gram-negative bacteria causing urinary tract infections. Some quinolones can also treat infections caused by Chlamydia trachomatis and Ureaplasma urealyticum. Quinolones reach high concentrations in the urine, serum, prostate, and semen. They have been shown to effectively treat uncomplicated cystitis with a single dose and have results similar to or better than other antibiotics for complicated UTIs. Hexamine is mentioned as
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.
This document provides information on various antitubercular agents. It begins with background on tuberculosis (TB) caused by Mycobacterium tuberculosis bacteria. It then discusses first-line antitubercular drugs including isoniazid, rifampicin, pyrazinamide, ethambutol and streptomycin. For each drug, it summarizes uses, mechanisms of action and potential adverse effects. It also discusses second-line drugs including para-amino salicylic acid, ethionamide, cycloserine and thiacetazone. The document aims to inform readers about different drug options for treating TB.
Sulfonamides are antibacterial drugs that work by interfering with bacterial synthesis of folic acid. They are structural analogues of para-aminobenzoic acid (PABA) that bind to and inhibit the enzyme dihydropteroate synthase. This document discusses the mechanism of action, classification, structure-activity relationships, and properties of sulfonamides. It provides examples of commonly used sulfonamides and details their structures, mechanisms, and applications in treatment. The document also addresses issues like ionization, crystalluria, and dissociation constants that are important for understanding sulfonamide properties and use.
Sulfonamides were the first effective antimicrobial agents against bacterial infections but resistance has limited their use. They work by inhibiting the bacterial enzyme involved in folate synthesis. Sulfonamides are classified based on duration of action and include sulfadiazine and sulfamethoxazole. Resistance can develop via decreased drug uptake, decreased enzyme affinity, or increased PABA synthesis. Cotrimoxazole is a fixed dose combination of trimethoprim and sulfamethoxazole that has synergistic antibacterial effects and lower resistance due to sequential folate pathway inhibition. It is commonly used to treat urinary tract, respiratory, and gastrointestinal infections.
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.
synthetic antimicrobials having a quinolone structure that are active primarily against gram-negative bacteria, though newer fluorinated compounds also inhibit gram-positive ones.
This document discusses aminoglycoside antibiotics. Aminoglycosides are natural and semi-synthetic antibiotics containing amino sugars that are used to treat gram-negative bacterial infections. Examples discussed include streptomycin, amikacin, neomycin, kanamycin, gentamicin, and netilmycin. The document provides details on the structure and uses of each drug. Aminoglycosides work by binding to the 30s ribosomal subunit, interfering with protein synthesis and causing the production of defective proteins that inhibit bacterial growth.
Antifungals drugs classification,mechanism of action uses and adverse effectsMuhammad Amir Sohail
Antifungal drugs are used to treat fungal infections by preventing fungal growth and reproduction. The document discusses several classes of antifungal drugs including polyenes like amphotericin B and nystatin, azoles like ketoconazole and fluconazole, and others. It describes the mechanisms of action, spectra of activity, clinical uses, and side effects of some common antifungal drugs used in veterinary medicine to treat superficial and systemic fungal infections.
This document discusses aminoglycoside antibiotics. It describes their structure, including that they contain amino sugars linked to an aminocyclitol ring. Examples are provided such as streptomycin, kanamycin, neomycin, and gentamicin. Their broad-spectrum antibacterial activity against gram-negative bacteria is summarized. Toxicities like nephrotoxicity and ototoxicity limit their clinical use to serious infections.
Viruses are obligate intracellular parasites that invade host cells and hijack their machinery to replicate. Antiviral drugs work by inhibiting viral replication and development inside host cells. There are several classes of antiviral drugs including adamantane derivatives, purine nucleotides, and pyrimidine nucleotides. Acyclovir, a purine nucleotide, gets activated by viral thymidine kinase inside infected cells and competitively inhibits viral DNA polymerase or gets incorporated into viral DNA. Idoxuridine, a pyrimidine nucleotide, is phosphorylated and substitutes for thymidine during viral DNA synthesis, inhibiting the viral DNA polymerase enzyme. Antiviral drugs display specificity against certain viruses by exploiting differences between host and viral polymer
medicinal chemistry of Antiviral drugsFatenAlsadek
medicinal chemistry of antiviral drugs with its chemical structures and how they chemically work
Done by: Faten Al-Sadek , Pharmacy student at Mohammed Al-Mana college for Health Sciences -MACHS
Antiviral Agents,Medicinal Chemistry
•Introduction to Viruses
•Structure of Virus
•Types of Viruses.
•The viral Life cycle.
•Classification of Antiviral Agents
- Tetracyclines are a class of broad spectrum antibiotic drugs derived from bacteria. They work by binding to the bacterial ribosome to inhibit protein synthesis and show bacteriostatic activity.
- Structurally, they contain four cyclic rings. Modifications to the structure can impact their activity. They are classified based on their duration of action as long, intermediate, or short acting.
- Common examples include tetracycline, doxycycline, and minocycline. They are used to treat various bacterial infections but have side effects like nausea, vomiting, and tooth staining when taken.
This document provides information about quinolones, including their classification, mechanism of action, and examples of specific quinolones. It discusses the classification of quinolones as first, second, third, or fourth generation. It also summarizes the mechanisms of action, pharmacokinetic properties, uses, and adverse effects of several common quinolones like ciprofloxacin, norfloxacin, ofloxacin, and moxifloxacin. Finally, it mentions some quinolones currently under clinical trials.
This document discusses various classes of antibiotics - polyenes and polypeptides. It provides details about Amphotericin B, Nystatin, Hamycin in the polyene class and Bacitracin, Polymyxin-B, Colistin/Polymyxin-E, and Dactinomycin/Actinomycin-D in the polypeptide class. It describes their origins, mechanisms of action, therapeutic uses, dosages and adverse effects.
This document provides an overview of antiviral drugs, including their mechanisms of action, classifications, and examples. It discusses how antiviral drugs work by inhibiting viral replication and preventing the virus from multiplying, rather than destroying the pathogen. The main classes covered are nucleoside analogs, including purine and pyrimidine analogs like acyclovir and idoxuridine; non-nucleoside reverse transcriptase inhibitors like nevirapine; protease inhibitors used to treat HIV; and miscellaneous agents like foscarnet sodium. For each drug class, examples are given along with descriptions of their structures, mechanisms of action, therapeutic uses, and dosages.
This document summarizes information about two antiviral drugs - Loviride and Zalcitabine. Loviride is a non-nucleoside reverse transcriptase inhibitor that was tested in clinical trials but failed to receive approval. Zalcitabine is a nucleoside reverse transcriptase inhibitor sold under the brand name Hivid. It works by incorporating into viral DNA and terminating its growth. The document also provides details on the mechanisms of action, pharmacokinetics, side effects and uses of the two drugs.
This document discusses antifungal drugs. It begins by describing common fungal infections that antifungals treat, such as ringworm and athlete's foot. It then discusses the different types of fungal infections including superficial infections of the skin and internal organ infections. The document outlines the main biochemical targets of antifungals and describes the structure and mechanisms of several major classes of antifungal drugs, including azoles, polyenes like amphotericin B and nystatin, and the heterocyclic compound griseofulvin. It provides details on specific antifungals like their structures, mechanisms of action, uses, and side effects.
This document discusses several classes of antibiotics including tetracyclines, macrolides, chloramphenicol, and lincosamides. It describes the chemical structures, mechanisms of action, modes of resistance, and structure-activity relationships for these drug classes. Tetracyclines are broad-spectrum antibiotics derived from Streptomyces fermentation that work by inhibiting bacterial protein synthesis. Macrolides also inhibit bacterial protein synthesis by binding the 50S ribosomal subunit. Resistance to macrolides occurs through methylation of ribosomal RNA. Chloramphenicol obtained from Streptomyces inhibits bacterial protein synthesis. Clindamycin is a lincosamide derived from lincomycin with a chlorine substitution that
The document discusses urinary tract anti-infective agents. It notes that newer quinolones like ciprofloxacin, norfloxacin, and ofloxacin are effective against a wide range of gram-positive and gram-negative bacteria causing urinary tract infections. Some quinolones can also treat infections caused by Chlamydia trachomatis and Ureaplasma urealyticum. Quinolones reach high concentrations in the urine, serum, prostate, and semen. They have been shown to effectively treat uncomplicated cystitis with a single dose and have results similar to or better than other antibiotics for complicated UTIs. Hexamine is mentioned as
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.
This document provides information on various antitubercular agents. It begins with background on tuberculosis (TB) caused by Mycobacterium tuberculosis bacteria. It then discusses first-line antitubercular drugs including isoniazid, rifampicin, pyrazinamide, ethambutol and streptomycin. For each drug, it summarizes uses, mechanisms of action and potential adverse effects. It also discusses second-line drugs including para-amino salicylic acid, ethionamide, cycloserine and thiacetazone. The document aims to inform readers about different drug options for treating TB.
Sulfonamides are antibacterial drugs that work by interfering with bacterial synthesis of folic acid. They are structural analogues of para-aminobenzoic acid (PABA) that bind to and inhibit the enzyme dihydropteroate synthase. This document discusses the mechanism of action, classification, structure-activity relationships, and properties of sulfonamides. It provides examples of commonly used sulfonamides and details their structures, mechanisms, and applications in treatment. The document also addresses issues like ionization, crystalluria, and dissociation constants that are important for understanding sulfonamide properties and use.
Sulfonamides were the first effective antimicrobial agents against bacterial infections but resistance has limited their use. They work by inhibiting the bacterial enzyme involved in folate synthesis. Sulfonamides are classified based on duration of action and include sulfadiazine and sulfamethoxazole. Resistance can develop via decreased drug uptake, decreased enzyme affinity, or increased PABA synthesis. Cotrimoxazole is a fixed dose combination of trimethoprim and sulfamethoxazole that has synergistic antibacterial effects and lower resistance due to sequential folate pathway inhibition. It is commonly used to treat urinary tract, respiratory, and gastrointestinal infections.
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.
synthetic antimicrobials having a quinolone structure that are active primarily against gram-negative bacteria, though newer fluorinated compounds also inhibit gram-positive ones.
This document discusses aminoglycoside antibiotics. Aminoglycosides are natural and semi-synthetic antibiotics containing amino sugars that are used to treat gram-negative bacterial infections. Examples discussed include streptomycin, amikacin, neomycin, kanamycin, gentamicin, and netilmycin. The document provides details on the structure and uses of each drug. Aminoglycosides work by binding to the 30s ribosomal subunit, interfering with protein synthesis and causing the production of defective proteins that inhibit bacterial growth.
Antifungals drugs classification,mechanism of action uses and adverse effectsMuhammad Amir Sohail
Antifungal drugs are used to treat fungal infections by preventing fungal growth and reproduction. The document discusses several classes of antifungal drugs including polyenes like amphotericin B and nystatin, azoles like ketoconazole and fluconazole, and others. It describes the mechanisms of action, spectra of activity, clinical uses, and side effects of some common antifungal drugs used in veterinary medicine to treat superficial and systemic fungal infections.
This document discusses various types of antifungal agents. It begins by stating that antifungal medicines are used to treat fungal infections affecting the skin, hair, nails, and other areas. There are hundreds of fungi that can cause infections ranging from common issues like athlete's foot to more serious infections. The document then covers the various classes of antifungal drugs including polyenes such as amphotericin B and nystatin, antimetabolites like flucytosine, azoles including imidazoles and triazoles, and allylamines. It discusses the mechanisms of action, common uses, and side effects of representative drugs within each class.
Amphotericin B is a polyene antifungal drug produced by Streptomyces nodosus that is used intravenously to treat serious systemic fungal infections. It works by binding to ergosterol in the fungal cell membrane, disrupting the membrane and causing leakage of cell contents. While fungi contain ergosterol in their cell membranes, human cells contain cholesterol and are less affected. Common side effects include nephrotoxicity.
This document provides information about antifungal agents. It begins with an introduction to fungi and fungal infections. It then discusses the classification, mechanisms of action, and clinical uses of various antifungal drug classes, including azoles, polyenes, allylamines, and echinocandins. Side effects and resistance mechanisms are also covered. The document aims to outline the potential targets and modes of action of different antifungal agents used in clinical practice.
Medicinal Chemistry and Pharmacology of Antifungal Agents and how to take care from fungal infections. Useful Course study material for the undergraduate , postgraduate and aspirants of Pharmacy , Pharmacology and Medicinal Chemistry.
Secondary Metabolism is a term for pathways for small molecule and products of metabolism that are not absolutely required for the survival of the organism.
A secondary metabolite has an important ecological function.
Examples include antibiotics, mycotoxins etc.
This document provides an overview of antifungal and anthelminthic drugs. It discusses the structure and types of fungi, classification of antifungal drugs, and drugs used to treat systemic fungal infections. Specifically, it describes the mechanisms of action, clinical uses, and toxicities of amphotericin B and flucytosine, two important drugs for treating systemic fungal infections.
This document provides an overview of anti-fungal drugs. It defines anti-fungal medications as fungicides or fungistatics used to treat mycosis (fungal infections). It classifies anti-fungal drugs into several categories including polyenes, echinocandins, azoles, allylamines, and others. For each category, it describes the mechanisms of action, examples of drugs, pharmacokinetics, adverse effects, and common uses. Key drugs discussed include amphotericin B, griseofulvin, flucytosine, ketoconazole, fluconazole, and terbinafine. The document explains that anti-fungal drugs work by
The ppt covers the following topics-
1. MICROBES
2. MICROBIAL CONTROL
2.1.Reason for microbial control
2.2.Methods of microbial control
3. ANTIBIOTIC
3.1.Definition
3.2.History of antibiotic discovery
4. MAJOR ANTIBIOTIC
4.1.PENICILLINS
4.1.1 Action , organisms and biosynthesis of penicillin
4.2.CEPHALOSPORINS
4.2.1 organism and biosynthesis
4.3.AROMATIC ANTIBIOTICS
4.4.NUCLEOSIDE ANTIBIOTICS
5. APPLICATIONS OF ANTIBIOTIC
6. SIDE EFFECTS OF ANTIBIOTIC
7. CONCLUSION
Fungi have cell walls containing chitin and polysaccharides, as well as cell membranes composed of ergosterol. Their similarity to mammalian cells makes antifungal drugs less selective than antibacterial drugs. There are several classes of antifungal drugs that target different parts of the fungal cell, including the cell wall, membrane, and nucleic acid synthesis. Echinocandins inhibit the synthesis of the essential cell wall component glucan, while azoles like fluconazole inhibit ergosterol synthesis. Amphotericin forms pores in the fungal membrane. Care must be taken with antifungal selection and use due to potential toxicity.
This document discusses anti-fungal drugs. It begins by defining fungi and describing their characteristics. It then discusses the structure of fungi including their cell wall, cell membrane, and intracellular components. It notes that anti-fungal drugs target the fungal cell wall, cell membrane, DNA/RNA synthesis, and mitosis. The document categorizes anti-fungal drugs and describes several major classes - polyenes, azoles, echinocandins, griseofulvin, and flucytosine. It provides details on several important anti-fungal drugs, including their mechanisms of action, pharmacokinetics, clinical uses, and side effects.
This document provides an overview of chemotherapy and antimicrobial agents. It discusses the types of bacteria, classification of antimicrobials, mechanisms of action and resistance. Specific drug classes are covered in detail including penicillins, cephalosporins, tetracyclines, macrolides, aminoglycosides, and fluoroquinolones. Adverse effects and clinical uses are described for each class. The document aims to educate students on the general concepts of antimicrobial therapy and properties of commonly used antibiotic drugs.
This document provides information on antifungal agents, including their targets, mechanisms of action, and clinical uses. It discusses that fungi have cell walls made of chitin and cell membranes containing ergosterol. Major classes of antifungals are described such as azoles which inhibit ergosterol biosynthesis, and polyenes like amphotericin B which bind to ergosterol in the membrane. The development of antifungals over time is summarized, from amphotericin B to newer azoles and echinocandins. Common adverse effects of amphotericin B include fever, renal impairment, and hypotension.
Fungi are eukaryotic organisms that are divided into three main groups: yeasts, molds, and dimorphic fungi. Yeasts are unicellular, oval or rounded organisms that reproduce asexually by budding. Molds are filamentous fungi that form branching hyphae and reproduce sexually through spores. Dimorphic fungi can exist in both yeast and filamentous forms depending on temperature. Candida albicans is a common yeast pathogen of humans that appears gram-positive and oval under the microscope and forms creamy, pasty colonies on Sabouraud's dextrose agar. Aspergillus is a mold that has branching septate hyphae and conidiophores terminating
Antifungal agents can be classified as systemic or topical based on their mode of application. Systemic agents treat internal fungal infections while topical agents treat superficial infections. Major classes of antifungals include polyenes like amphotericin B, azoles like ketoconazole and fluconazole, and allylamines like terbinafine. They have different mechanisms of action, spectra of activity, and side effect profiles. Choosing an antifungal depends on the type and location of infection as well as the safety profile.
Lab 6 isolation of antibiotic producer from soilHama Nabaz
The document outlines steps to isolate antibiotic-producing microorganisms from soil samples and determine their antimicrobial activity. Students will isolate Bacillus, Penicillium, and Actinomyces colonies on agar plates. Colonies will be streaked on plates seeded with Staphylococcus epidermidis or fungi to check for evidence of antibiosis. Colonies showing inhibition will be re-streaked with test pathogens to confirm antimicrobial activity through zone of inhibition assays. The goal is to isolate microbes producing antibiotics that could have clinical significance.
Similar a Anti-fungal agents Medicinal Chemistry-III (20)
A) Carrier linked prodrugs and B) Bioprecursors
A) Carrier linked prodrugs- active drug linked to a carrier group
Carrier group- should be labile, non-toxic, biologically inactive
Further divided to bipartate, tripartate and mutual prodrugs
1. Bipartate- prodrug with carrier
2. Tripartate- carrier + linker + prodrug
3. Mutual prodrug- synergistic drugs connected to each other
Biguanides – biological transformation, SAR, metabolism, effects and side effects
Pyrimidines – site of action, SAR
Sulphones and sulphonamides – Action and toxicity
Mechanism of action of Antimalarials
Synthesis of chloroquine
Synthesis of primaquine
Synthesis of quinacrine
Chloroquine is prepared from 2-nitro aniline
Primaquine is prepared from 1,4-dibromopentane
Quinacrine is prepared from 2,4-dichloro benzoic acid
Etiology (study of the cause/ causation of disease or condition):
Malaria in humans is caused by four species of Plasmodium (protozoan parasite)
Plasmodium Vivax (benign tertian malaria)
Plasmodium falciparum (malignant tertian, sub-tertian malaria)
Plasmodium malariae (quartan malaria)
Plasmodium ovale (mild tertian malaria ovale tertian)
In other mammals, birds and reptiles it is caused by many other species.
Indian pharmaceutical history began from Gupta period which was existed from approximately 320 to 550 CE where people were dependent only on indigenous form of medicine before British rule.
In India Allopathic medication was started in British rule, but production of such medicines was not in the country.
In 1901 Acharya P C Ray started first Indian Pharmaceutical Industry, Bangal Chemical in Calcutta.
The government started to encourage the growth of drug manufacturing by Indian companies in the early 1960s, and with the Patents Act in 1970.
However, economic Liberalization in 90s enabled the industry to become what it is today.
"Exploring Pharmacy as a Career: Pathways, Opportunities, and Impact"akhileshtiwari95
Pharmacists are experts in medicines and their use. They have a unique set of skills and knowledge, they train as scientists and clinicians. They use this scientific knowledge to advise patients how to take their medicines and make recommendations on the best medicine for particular conditions and diseases.
Pharmacists are the third largest healthcare profession in india. They work in a number of different settings, developing new medicines, supplying medicines, providing advice about medicines, and offering health services. Some pharmacists are also prescribers, and like doctors can prescribe medicines on prescriptions. They also work within the wider healthcare team, ensuring that patients receive the best possible care. Pharmacists also work in other roles where there may be less direct contact with patients, for example in universities, regulation, government organisations, research, publishing and the pharmaceutical industry.
Pharmacists must have very good communication skills, as they are required to translate technical medical information to patients. They often work in busy environments and must be organised, logical, be able to manage multiple tasks, and remain calm under pressure. They should also have a good eye for detail and be thorough and accurate in what they do. Pharmacists work in teams and are often involved in education and training others, so good people skills are also essential.
Brief history, classification, Structure, mechanism Interferes with the cell wall synthesis of bacteria
Inhibit the formation of peptidoglycan cross links in bacterial cell wall by binding of ß-lactum ring of penicillin to enzyme DD -transpeptidase
DD-transpeptidase cannot catalyze the formation of cross links causing imbalance in cell wall production, degrades leading to rapid cell death
Beta lactam antibiotics, First antibiotic by Scottish scientist , Alexander Fleming in 1928 (seen fungus and bacteria can not grow together)
PCN was isolated from fungus Penicillium notatum
ß-lactum antibiotics
Active against Gram +ve bacteria (Staphylococci and Streptococci) not against gram –ve except at high dose
Integrating Ayurveda into Parkinson’s Management: A Holistic ApproachAyurveda ForAll
Explore the benefits of combining Ayurveda with conventional Parkinson's treatments. Learn how a holistic approach can manage symptoms, enhance well-being, and balance body energies. Discover the steps to safely integrate Ayurvedic practices into your Parkinson’s care plan, including expert guidance on diet, herbal remedies, and lifestyle modifications.
Hiranandani Hospital in Powai, Mumbai, is a premier healthcare institution that has been serving the community with exceptional medical care since its establishment. As a part of the renowned Hiranandani Group, the hospital is committed to delivering world-class healthcare services across a wide range of specialties, including kidney transplantation. With its state-of-the-art facilities, advanced medical technology, and a team of highly skilled healthcare professionals, Hiranandani Hospital has earned a reputation as a trusted name in the healthcare industry. The hospital's patient-centric approach, coupled with its focus on innovation and excellence, ensures that patients receive the highest standard of care in a compassionate and supportive environment.
8 Surprising Reasons To Meditate 40 Minutes A Day That Can Change Your Life.pptxHolistified Wellness
We’re talking about Vedic Meditation, a form of meditation that has been around for at least 5,000 years. Back then, the people who lived in the Indus Valley, now known as India and Pakistan, practised meditation as a fundamental part of daily life. This knowledge that has given us yoga and Ayurveda, was known as Veda, hence the name Vedic. And though there are some written records, the practice has been passed down verbally from generation to generation.
Muktapishti is a traditional Ayurvedic preparation made from Shoditha Mukta (Purified Pearl), is believed to help regulate thyroid function and reduce symptoms of hyperthyroidism due to its cooling and balancing properties. Clinical evidence on its efficacy remains limited, necessitating further research to validate its therapeutic benefits.
Travel vaccination in Manchester offers comprehensive immunization services for individuals planning international trips. Expert healthcare providers administer vaccines tailored to your destination, ensuring you stay protected against various diseases. Conveniently located clinics and flexible appointment options make it easy to get the necessary shots before your journey. Stay healthy and travel with confidence by getting vaccinated in Manchester. Visit us: www.nxhealthcare.co.uk
These lecture slides, by Dr Sidra Arshad, offer a simplified look into the mechanisms involved in the regulation of respiration:
Learning objectives:
1. Describe the organisation of respiratory center
2. Describe the nervous control of inspiration and respiratory rhythm
3. Describe the functions of the dorsal and respiratory groups of neurons
4. Describe the influences of the Pneumotaxic and Apneustic centers
5. Explain the role of Hering-Breur inflation reflex in regulation of inspiration
6. Explain the role of central chemoreceptors in regulation of respiration
7. Explain the role of peripheral chemoreceptors in regulation of respiration
8. Explain the regulation of respiration during exercise
9. Integrate the respiratory regulatory mechanisms
10. Describe the Cheyne-Stokes breathing
Study Resources:
1. Chapter 42, Guyton and Hall Textbook of Medical Physiology, 14th edition
2. Chapter 36, Ganong’s Review of Medical Physiology, 26th edition
3. Chapter 13, Human Physiology by Lauralee Sherwood, 9th edition
Local Advanced Lung Cancer: Artificial Intelligence, Synergetics, Complex Sys...Oleg Kshivets
Overall life span (LS) was 1671.7±1721.6 days and cumulative 5YS reached 62.4%, 10 years – 50.4%, 20 years – 44.6%. 94 LCP lived more than 5 years without cancer (LS=2958.6±1723.6 days), 22 – more than 10 years (LS=5571±1841.8 days). 67 LCP died because of LC (LS=471.9±344 days). AT significantly improved 5YS (68% vs. 53.7%) (P=0.028 by log-rank test). Cox modeling displayed that 5YS of LCP significantly depended on: N0-N12, T3-4, blood cell circuit, cell ratio factors (ratio between cancer cells-CC and blood cells subpopulations), LC cell dynamics, recalcification time, heparin tolerance, prothrombin index, protein, AT, procedure type (P=0.000-0.031). Neural networks, genetic algorithm selection and bootstrap simulation revealed relationships between 5YS and N0-12 (rank=1), thrombocytes/CC (rank=2), segmented neutrophils/CC (3), eosinophils/CC (4), erythrocytes/CC (5), healthy cells/CC (6), lymphocytes/CC (7), stick neutrophils/CC (8), leucocytes/CC (9), monocytes/CC (10). Correct prediction of 5YS was 100% by neural networks computing (error=0.000; area under ROC curve=1.0).
Osteoporosis - Definition , Evaluation and Management .pdfJim Jacob Roy
Osteoporosis is an increasing cause of morbidity among the elderly.
In this document , a brief outline of osteoporosis is given , including the risk factors of osteoporosis fractures , the indications for testing bone mineral density and the management of osteoporosis
Our backs are like superheroes, holding us up and helping us move around. But sometimes, even superheroes can get hurt. That’s where slip discs come in.
1. Medicinal Chemistry-III
Antifungal agents
Department of Pharmacy, Indira Gandhi National Tribal
University, Lalpur, Amarkantak (M.P.)
Dr. Akhilesh Tiwari
Assistant Professor
Department of Pharmacy,
IGNTU, Amarkantak
4/25/2024 1
2. Mycology is the study of fungi. The name “fungi” is derived from “mykos” meaning mushroom. The fungi are eukaryotic
organisms and they differ from the bacteria, which are prokaryotic organisms, in many ways (Table 71-1). The fungi possess
rigid cell walls, which possess two characteristic cell structures: chitin and ergosterol.
3. Classification of Fungi
The fungi can be classified as follows:
Taxonomical Classification
The fungi are placed in the phylum Thallophyta. There are four classes of fungi: Zygomycetes, Ascomycetes, Basidiomycetes, and Deuteromycetes.
Morphological Classification
The fungi can be classified into the following four main groups based upon the morphology: (a) yeast, (b) yeast-like form, (c) molds, and (d) dimorphic fungi.
4. Chitin:
• The fungi consist primarily of chitin, unlike pepti-doglycan present in cell wall of bacteria.
Hence, fungi are not sensitive to action of penicillin and other antibiotics that inhibit
peptidoglycan synthesis.
• Chitin is a polysaccharide consisting of long chains of N-acetylglucosamine.
Ergosterol:
• The cell membrane of fungus contains ergosterol, unlike human cell membrane which contains
cholesterol.
• The antifungal agents, such as amphotericin B, fluconazole, and ketoconazole have selective
action on the fungi due to this basic difference in membrane sterols.
5. Pathogenesis of Fungal Infection
Most fungi are aerobes.
The natural habitat of most fungi is environment,
C. albicans is exception and is an important fungus, which is a part of the normal human flora.
Fungi are ubiquitous in nature, i.e., they occur as free-living saprobes, hence determining their role in human
infection may sometimes be difficult.
The effects of fungi on humans can be grouped in three major ways as follows: (a) colonization and disease, (b)
hypersensitive diseases, and (c) diseases caused by mycotoxins or fungal toxins.
6. Colonization and Disease
Most fungal infections are mild and self-limited. Intact skin is an effective host defense against certain fungi. But if
the skin is broken, organisms, the fungi enter through that broken skin and initiate the infection.
Fatty acid content, pH, epithelial turnover, and normal bacterial flora of the skin contribute to host resistance
against fungi.
For example, The mucous mem-brane of the nasopharynx traps inhaled fungal spores. Cell-mediated immunity is
much important in conferring protection against fungi. Suppression of cell-mediated immu-nity can lead to
reactivation fungal infection and to diseases caused by opportunistic fungi.
The humoral immunity is mediated by production of IgG and IgM antibody. But their role in protection from
fungal disease is uncertain.
Fungal infection that occurs in the immunocompromised hosts is called as opportunistic mycosis. If such
conditions are not rapidly diagnosed and immediately managed, they can prove to be life-threatening.
7. Hypersensitivity Diseases
Humans are continually exposed to air-borne fungal spores and other fungal elements present in the
environment. These spores can be antigenic stimulants and depending on individual’s
immunological status may induce a state of hypersensitivity by production of immunoglobulin's or
sensitized lymphocytes.
Rhinitis, bronchial asthma, alveolitis, and various forms of atopy are the clinical manifestations of
hypersensitive pneumo-nitis. The clinical manifestations of the hypersensitivity disease are seen
only in sensitized person, after repeated exposure to the fungus, fungal metabolites, or other cross-
reactive materials. Allergies to the fungal spores are manifested primarily by an asthmatic reaction
including rapid bronchial constriction mediated by IgE, eosinophilia, and positive hypersensitivity
skin test reaction. These are caused due to immediate hyper-sensitivity reactions of the host to
fungal spores.
8.
9. Antifungal Drugs
A few drugs are available for therapy of systemic fungal infection, unlike a large number of antibiotics available to treat bacterial infections. The drugs used to treat
bacterial disease have no effect on fungal diseases. Amphotericin B and various azoles are the most effective antifungal drugs. They act on the ergosterol of fungal
cell membrane that is not found in bacterial or human cell membrane. Similarly, caspo-fungin inhibits synthesis of beta-glucan, which is found only in fungal
membrane but not in bacterial or human cell mem-brane. Table 71-3 summarizes the common antifungal agents and their primary sites of activity.
10.
11.
12. Antifungal antibiotics
• Use of the polyenes for the treatment of systemic infections is limited
• toxicities of the drugs,
• Low water solubilities, and
• poor chemical stabilities
• Amphotericin B, the only polyene useful for the treatment of serious systemic
infections, must be solubilized with a detergent
• Other polyenes are indicated only as topical agents for superficial fungal infections
13.
14. Mechanism of action
• In three-dimensional shape,
• a barrel-like nonpolar structure capped by a polar group (sugar)
• penetrate the fungal cell membrane, acting as “false membrane components,”
• bind closely with ergosterol,
• causing membrane disruption,
• cessation of membrane enzyme activity, and loss of cellular constituents, especially
potassium ions
15. Amphotericin B
• Purified from the fermentation beer of a soil culture of the actinomycete
Streptomyces nodosus, which was isolated in Venezuela
• first isolate from the streptomycete was a separable mixture of two compounds,
designated amphotericins A and B
• In test cultures, compound B proved to be more active, and this is the one used
clinically
• Amphotericin B is believed to interact with membrane sterols (ergosterol in fungi) to
produce an aggregate that forms a transmembrane channel
• Intermolecular hydrogen bonding interactions among hydroxyl, carboxyl, and amino
groups stabilize the channel in its open form
16. Amphotericin B
• Fever, headache, anorexia, gastrointestinal distress, malaise, and muscle and joint
pain are common
• Pain at the site of injection and thrombophlebitis are frequent complications of
intravenous administration.
• Drug must never be administered intramuscularly.
• Hemolytic activity of amphotericin B may be a consequence of its ability to leach
cholesterol from erythrocyte cell membranes
• For fungal infections of the CNS (e.g., cryptococcosis), amphotericin B is mixed with
cerebrospinal fluid (CSF) that is obtained from a spinal tap
• Drug is supplied in various topical forms, including a 3% cream, a 3% lotion, a 3%
ointment, and a 100-mg/mL oral suspension
17. • Nystatin
• First isolated in 1951 from a strain of the actinomycete Streptomyces noursei by
Hazen and Brown
• very slightly soluble in water and sparingly soluble in organic solvents
• unstable to moisture, heat, and light
• aglycone portion of nystatin is called nystatinolide
• It consists of a 38-membered macrolide lactone ring containing single tetraene and
diene moieties separated by two methylene groups
• Aglycone also contains eight hydroxyl groups, one carboxyl group, and the lactone
ester functionality
• Entire compound is constructed by linking the aglycone to mycosamine
• not absorbed systemically when administered by the oral route
• It is nearly insoluble under all conditions
• It is also too toxic to be administered parenterally and used only as a topical agent
18. Nystatin
• Valuable agent for the treatment of local and gastrointestinal infections caused by C.
albicans and other Candida species
• For the treatment of cutaneous and mucocutaneous candidiasis, it is supplied as a
cream, an ointment, and a powder
• Oral tablets are used in the treatment of gastrointestinal and oral candidiasis
20. Natamycin
• Polyene antibiotic obtained from cultures of Streptomyces natalensis
• consists of a 26-membered lactone ring containing a tetraene chromophore,
• an α,β-unsaturated lactone carbonyl group, three hydroxyl groups, a carboxyl group,
a trans epoxide, and a glycosidically joined mycosamine
• natamycin is amphoteric
• Mechanism- 26-membered–ring polyenes cause both potassium ion leakage and cell
lysis at the same concentration
• whereas the 38-membered–ring polyenes cause potassium leakage at low,
fungistatic concentrations and cell lysis at high, fungicidal concentrations
• supplied as a 5% ophthalmic suspension intended for the treatment of fungal
conjunctivitis, blepharitis, and keratitis
21. • Griseofulvin
• antibiotic obtained from the fungus Penicillium griseofulvum
• It was isolated originally as a “curling factor” in plants
• drug has been used for many years for its antifungal action in plants and animals
• In 1959, griseofulvin was introduced into human medicine for the treatment of tinea
infections by the systemic route
23. Griseofulvin
• example of a rare structure in nature, a spiro compound
• compound is a white, bitter, heat-stable powder or crystalline solid
• sparingly soluble in water but soluble in alcohol and other nonpolar solvents
• used for a long time for the systemically delivered treatment of refractory ringworm
infections of the body, hair, nails, and feet
• caused by species of dermatophytic fungi including Trichophyton and
Epidermophyton
• Griseofulvin neither possesses antibacterial activity nor is effective against P.
obiculare, the organism that causes tinea versicolor
24. Griseofulvin
• most common ones are allergic reactions such as rash and urticaria, gastrointestinal
upset, headache, dizziness, and insomnia
• oral bioavailability of griseofulvin is very poor
• compound is highly lipophilic with low water solubility
• Several structural derivatives have been synthesized, but they have failed to improve
absorption
• best advice that the pharmacist can give a patient who is about to use griseofulvin is
to take the drug with a fatty meal
25. Synthetic anti-fungal agents
• Clotrimazole, Econazole, Butoconazole, Oxiconazole Tioconozole Ketoconazole,
Terconazole, Itraconazole, Fluconazole, Naftifine hydrochloride
• Synthesis- Miconazole, Tolnaftate
• Azole Antifungal Agents
• Possess a unique mechanism of action
• Can achieve selectivity for the infecting fungus over the host
• Can treat infections ranging from simple dermatophytoses to life-threatening, deep
systemic fungal infections
• First members of the class were highly substituted imidazoles, such as clotrimazole
and miconazole
26. Azole Antifungal Agents
• Structure–activity studies revealed that the imidazole ring could be replaced with a
bioisosteric 1,2,4-triazole ring without adversely affecting the antifungal properties
of the molecule
• Spectrum of activity
• Azoles tend to be effective against most fungi that cause superficial infections of the
skin and mucous membranes, including the dermatophytes such as Trichophyton,
Epidermophyton, and Microsporum spp. and yeasts such as C. albicans
• On the other hand, they also exhibit activity against yeasts that cause systemic
infections, including C. immitis, C. neoformans, Paracoccidioides brasiliensis,
Petriellidium boydii, B. dermatitidis, and H. capsulatum
27. Azole Antifungal Agents- Mechanism of action
• At micromolar, the azoles are fungicidal
• At nanomolar, the azoles are fungistatic
• Fungicidal effect is clearly associated with damage to the cell membrane, with the
loss of essential cellular components such as potassium ions and amino acids
• Fungistatic effect is associated with inhibition of membrane-bound enzymes
• A cytochrome P450-class enzyme, lanosterol 14α-demethylase, is the likely target for
the azoles
• Function of lanosterol 14α-demethylase is to oxidatively remove a methyl group from
lanosterol during ergosterol biosynthesis
29. Azole Antifungal Agents- Mechanism of action
• Lanosterol 14α-demethylase is also required for mammalian biosynthesis of
cholesterol, and the azoles are known to inhibit cholesterol biosynthesis
• Higher concentrations of the azoles are needed to inhibit the mammalian enzyme
• Provides selectivity for antifungal action
• 1,2,4-triazoles appear to cause a lower incidence of endocrine effects and
hepatotoxicity than the corresponding imidazoles
• Possibly because of a lower affinity for the mammalian cytochrome P450 enzymes
involved
30. Clotrimazole
• Broad-spectrum antifungal drug that is used topically for the treatment of tinea
infections and candidiasis
• It occurs as a white crystalline solid that is sparingly soluble in water but soluble in
alcohol and most organic solvents
• It is a weak base that can be solubilized by dilute mineral acids
• Extremely stable, with a shelf life of more than 5 years
• Effective against various pathogenic yeasts and
• Reasonably well absorbed orally, extensively protein bound
• Not considered suitable for the treatment of systemic infections
31. Econazole
• It is only slightly soluble in water and most organic solvents
• Used as a 1% cream for the topical treatment of local tinea infections and cutaneous
candidiasis
32. Butoconazole
• Extremely broad-spectrum antifungal drug that is specifically effective against C.
albicans
• It is intended for the treatment of vaginal candidiasis- 2% of butoconazole nitrate in
the form of cream
33. Oxiconazole
• It is used in cream and lotion dosage forms in 1% concentration for the treatment of
tinea pedis, tinea corporis, and tinea capitis
34. Tioconazole
• Used for the treatment of vulvovaginal candidiasis
• A vaginal ointment containing 6.5% of the free base is available
• More effective against Torulopsis glabrata than are other azoles
35. Miconazole
• Occurs as white crystals that are sparingly soluble in water and most organic solvents
• The free base is available in an injectable form, solubilized with polyethylene glycol
and castor oil, and intended for the treatment of serious systemic fungal infections
• Like candidiasis, coccidioidomycosis, cryptococcosis, petriellidiosis, and
paracoccidioidomycosis
• thrombophlebitis, pruritus, fever, and gastrointestinal upset are relatively common
side effects
36. Ketoconazole
• broad-spectrum imidazole antifungal agent that is administered orally for the
treatment of systemic fungal infections
• It is a weakly basic compound that occurs as a white crystalline solid that is very
slightly soluble in water
37. Ketoconazole
• primary route of excretion is enterohepatic
• It is estimated to be 95% to 99% bound to protein in the plasma
• Hepatotoxicity- most serious adverse effect
• known to inhibit cholesterol biosynthesis in both mammals and fungi
• High doses have also been reported to lower testosterone and corticosterone levels
• Ketoconazole is a racemic compound, consisting of the cis-2S,4R and cis-2R,4S
isomers
• trans-isomers, 2S,4S and 2R,4R, are much less active
38. Ketoconazole
• recommended for the treatment of the following systemic fungal infections:
candidiasis (including oral thrush and the chronic mucocutaneous form),
coccidioidomycosis, blastomycosis, histoplasmosis, chromomycosis, and
paracoccidioidomycosis
• It is also used orally to treat severe refractory cutaneous dermatophytic infections
not responsive to topical therapy or oral griseofulvin
• antifungal actions of ketoconazole and the polyene antibiotic amphotericin B are
reported to antagonize each other
• used topically in a 2% concentration in a cream and in a shampoo for the
management of cutaneous candidiasis and tinea infections
39. Terconazole
• Triazole derivative that is used exclusively for the control of vulvovaginal moniliasis
caused by C. albicans and other Candida species
• It is available in creams containing 0.4% and 0.8% of the free base intended for 7-day
and 3-day treatment periods, respectively
40. Itraconazole
• Unique member of the azole class that contains two triazole moieties in its structure
• A weakly basic 1,2,4-triazole and a non-basic 1,2,4-triazol-3-one
• orally active, broad-spectrum antifungal agent and important alternative to
ketoconazole
41. Itraconazole
• An acidic environment is required for optimum solubilization and oral absorption
• Food greatly enhances the absorption of itraconazole, nearly doubling its oral
bioavailability
• drug is avidly bound to plasma proteins (nearly 99% at clinically effective
concentrations) and extensively metabolized in the liver
• Only one of the numerous metabolites, namely 1-hydroxyitraconazole, has significant
antifungal activity
• terminal elimination half-life of itraconazole ranges from 24 to 40 hours
42. Itraconazole
• Used for the treatment of systemic fungal infections including blastomycosis,
histoplasmosis (including patients infected with [HIV]),
• nonmeningeal coccidioidomycosis, paracoccidioidomycosis, and sporotrichosis
• It may also be effective in the treatment of pergellosis, disseminated and deep organ
candidiasis, coccidioidal meningitis, and cryptococcosis
• Unlike ketoconazole, it is not hepatotoxic and does not cause adrenal or testicular
suppression in recommended therapeutic doses
43. Fluconazole
• Water soluble bis-triazole with broad-spectrum antifungal properties
• Suitable for both oral and intravenous administration as the free base
• Excellent bioavailability in both tablet and suspension dosage forms
• Presence of two weakly basic triazole rings in the molecule confers sufficient
aqueous solubility to balance the lipophilicity of the 2,4-difluorophenyl group
• Has a relatively long elimination half-life, ranging from 27 to 34 hours
• It penetrates well into all body cavities, including the CSF
• Little or no hepatic metabolism and is excreted substantially unchanged in the urine
• Plasma protein binding of fluconazole is less than 10%
44. Fluconazole
• Inhibition of cytochrome P450 oxidases by fluconazole can give rise to clinically
significant interactions involving increased plasma levels of cyclosporine, phenytoin,
and the oral hypoglycemic drugs
• Recommended for the treatment and prophylaxis of disseminated and deep organ
candidiasis
• It is also used to control esophageal and oropharyngeal candidiasis
• Agent of choice for the treatment of cryptococcal meningitis and
for prophylaxis against cryptococcosis in AIDS patients
45. Naftifine Hydrochloride
• White crystalline powder that is soluble in polar solvents such as ethanol and
methylene chloride
• It is supplied in a 1% concentration in a cream and in a gel for the topical treatment
of ringworm, athlete’s foot, and jock itch
• Although unapproved for these uses, naftifine has
shown efficacy for treatment of ringworm of the
beard, ringworm of the scalp, and tinea versicolor
Cl
46. Tolnaftate
• White crystalline solid that is insoluble in water, sparingly soluble in alcohol, and
soluble in most organic solvents
• compound, a thioester of β-naphthol, is fungicidal against dermatophytes, such as
Trichophyton, Microsporum, and Epidermophyton spp., that cause superficial tinea
infections
• Available in a concentration of 1% in creams, powders, aerosols, gels, and solutions
for the treatment of ringworm, jock itch, and athlete’s foot
• Shown to act as an inhibitor of squalene epoxidase
• in susceptible fungi
48. Tolnaftate- Synthesis
2-naphthol and thiophosgene to make a monosubstituted product of thiophosgene,
which is then reacted with N-methyl-3-toluidine to give the desired tolnaftate