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Unit 6 : Anti-Infective Agents
HCSP 1232 Intro to Pharma
Roszan Sapon
Objective
• Definition, class, mode of action and
example of drug ;
• Anti-infective
• Antibiotic
• Antiviral
• Antifungal
• Antiparasites
Some terminology
• Pathogen: Disease causing microorganism.
• Empiric: Therapy that is started based upon on
experience and precedent in the observation
and treatment of disease.
• Normal flora: Organisms found in various parts
of the body living symbiotically.
• Aerobic: Requires oxygen to survive.
• Anaerobic: Does not require oxygen to survive.
• Gram Stain: Laboratory test used to determine
if an organism is gram-positive or gram-
negative.
• C & S: Culture and sensitivity. Determines the
organism present in the culture and the
antibiotic to which it is sensitive (susceptible to).
• Fungicide / fungistatic: To kill fungus
• Mycosis: Disease cause by fungus
Some terminology - cont
Definition
• Anti-infective : An agent that is capable of
acting against infection, either by inhibiting the
spread of an infectious agent of by killing the
infectious agent outright.
• Antibiotic: Substance that kills microorganism
growth (mostly bacteria).
• Antiviral : Class of medication used for treating
viral infections
• Antifungal : Pharmaceutical fungicide used to
treat and prevent mycosis
• Antiparasites : Drugs used to treat parasitic
diseases.
Classes of Anti-infective Agents
1. Antibiotic
• An antibiotic is a type of anti-infective substance
active against bacteria.
• It is the most important of antibacterial agent for
fighting infection.
• Widely used in treatment and prevention of such
infection.
• Bacteriostatic: Inhibits replication of
microorganisms and prevents growth. Does not
kill bacteria.
• Bacteriocidal: Kills the bacteria.
Antibiotic - Mode of action
• Mode of action :
• They may either kill or inhibit the growth of
bacteria.
• Bacteriostatic: Inhibits replication of
microorganisms and prevents growth. Does
not kill bacteria.
• Bacteriocidal: Kills the bacteria. Its may
attack he structures of the microb including
their nucleus.
Antibiotic - Classes of
Antibiotics
Antibiotics - Types & Example
• Beta Lactams
• penicillins
• cephalosporins (4 generations)
• Broader coverage with each generation.
• Aminoglycosides
• tobramycin
• Vancomycin
• MRSA
• Protein Synthesis Inhibitors
• macrolides
• tetracyclines
• Folate Inhibitors
• metronidazole
Antibiotics - Penicillins
• In 1928, Alexander Fleming noted that mold
belonging to the genus Penicillium inhibited the
growth of bacteria. Fleming called this unknown
antibacterial substance penicillin. Ten years later, a
group at Oxford University began to investigate
penicillin in laboratory mice. Penicillin was hailed as
a miracle drug and saved countless lives in World
War II
• Penicillins are antibiotics used to treat bacterial
infections that are derived from the antibiotic
penicillin.
Uses for Penicillin
• Penicillin antibiotics are used to treat many
types of infections caused by susceptible
bacteria. They are used to treat infections of
the middle ear, sinuses, stomach and
intestines, bladder, and kidney. They also are
used for treating
• pneumonia,
• blood infections (sepsis),
• uncomplicated gonorrhea,
• meningitis,
• endocarditis, and
• other serious infections.
• Penicillin V
• Penicillin G (P
fi
zerpen, Permapen)
• Amoxicillin/clavulonate (Augmentin)
• Ampicillin (Unasyn)
• Nafcillin (Nallpen)
• Oxacillin (Bactocill)
• Dicloxacillin
• Cloxacillin
Example of penicillin antibiotics
Antibiotics - Cephalosporins
• Cephalosporins are a large group of antibiotics derived from
the mold Acremonium (previously called Cephalosporium).
• Cephalosporins are bactericidal (kill bacteria) and work in a
similar way to penicillins.
• They bind to and block the activity of enzymes responsible
for making peptidoglycan, an important component of the
bacterial cell wall.
• They are called broad-spectrum antibiotics because they
are effective against a wide range of bacteria.
Use for Cephalosporins
• Cephalosporins may be used to treat infections
caused by susceptible bacteria, such as:
• Bone infections
• Ear infections (eg, otitis media)
• Skin infections
• Upper respiratory tract infections
• Urinary tract infections.
Cephalosporins are not usually used as a
fi
rst-
choice antibiotic. They tend to be reserved for
use when other antibiotics (often penicillins)
cannot be used.
Example of Cephalosporins
• There are currently five “generations” of
cephalosporins, with each generation
differing slightly in their antibacterial
spectrum (ie, how effective they are at
killing certain types of bacteria).
• Within each generation, there are
differences in terms of administration
(such as oral or intravenous
administration), absorption, excretion,
and how long the activity of the
cephalosporin lasts for in the body.
Example of Cephalosporins - cont
• Ancef and Kefazol (cefazolin)
• Ceclor and Cefaclor (cefaclor)
• Cefdinir.
• Ceftin and Zinacef (cefuroxime)
• Duricef (cefadroxil)
• Keflex and Keftabs (cephalexin)
• Maxipime (cefepime)
• Rocephin (ceftriaxone)
Antibiotics - Macrolides
• Macrolide: One in a class of antibiotics that includes
Biaxin (Clarithromycin), Zithromax (Azithromycin),
Dificid (Fidoximycin), and Erythromycin.
• The macrolides inhibit the growth of bacteria and are
often prescribed to treat rather common bacterial
infections.
• In more technical terms, the macrolides are a group of
antibiotics produced by various strains of
Streptomyces (spore forming bacteria that grow slowly
in soil or water as a branching filamentous mycelium
similar to that of fungi) and have a complex chemical
(macrocyclic) structure. They act by inhibiting protein
synthesis, specifically by blocking the 50S ribosomal
subunit. They are broad spectrum antibiotics.
Antibiotics - Quinolones
• A quinolone antibiotic is a member of a large group
of broad-spectrum bacteriocidals that share a bicyclic
core structure related to the substance 4-quinolone.
• They are used in human and veterinary medicine to
treat bacterial infections, as well as in animal
husbandry.
• Nearly all quinolone antibiotics in use are
fluoroquinolones, which contain a fluorine atom in
their chemical structure and are effective against
both Gram-negative and Gram-positive bacteria.
• One example is ciprofloxacin, one of the most widely
used antibiotics worldwide.
Antibiotics - Tetracyclines
• Tetracyclines have a broad spectrum of activity
against many gram-positive and gram-negative
bacteria as well as Mycoplasma, Chlamydia,
Rickettsiae, Plasmodia, and amoebae.
• They are usually bacteriostatic.
• Tetracyclines bind reversibly to the small subunits of
bacterial (and eukaryotic) ribosomes where they
interfere with binding of charged-tRNA to the
"Acceptor" site.
• Tetracyclines can also inhibit protein synthesis in the
host, but are less likely to reach the concentration
required because eukaryotic cells do not have a
tetracycline uptake mechanism.
Use of Tetracyclines
• Tetracyclines are used widely in both human and veterinary
medicine; for example, tetracyclines have been used:
• For the prevention of malaria
• For the treatment of moderate-to-severe acne or rosacea
• To treat anthrax
• To treat infections of the eye, gastrointestinal tract,
genitourinary tract, gums, respiratory tract, and skin
• To treat infections caused by lice, mites, or ticks (such as
Rocky Mountain spotted fever, typhus fever)
• To treat infections caused by Campylobacter, Chlamydiae,
Yersinia pestis (plague), Vibrio cholerae (cholera) and other
atypical organisms
• To treat respiratory tract infections caused by Mycoplasma
pneumoniae
• As a growth promoter in animals.
Use of Tetracyclines
• Because many strains of microorganisms are now
resistant to some tetracyclines, culture and susceptibility
testing is recommended before beginning treatment.
• Doxycycline is a tetracycline that may be considered
when penicillin is contraindicated.
Antibiotics - Aminoglycosides
• Aminoglycosides are natural or semisynthetic antibiotics
derived from actinomycetes.
• Aminoglycosides are potent, broad-spectrum antibiotics
that act through inhibition of protein synthesis.
• They are commonly used in combination with drugs
such as ampicillin.
• For example, gentamicin, an aminoglycoside antibiotic
that has gram-negative coverage, is used in
combination with both an agent against gram-positive
organisms and one that covers anaerobes. Because of
their potential nephrotoxicity, aminoglycosides should
be reserved as a last resort, for use in resistant or life-
threatening infections.
• In addition, aminoglycosides should be avoided during
pregnancy.
2. Anti-Viral Agents
• Antiviral drugs are a class of medication used for
treating viral infections.
• Most antivirals target specific viruses, while a
broad-spectrum antiviral is effective against a
wide range of viruses.
• Unlike most antibiotics, antiviral drugs do not
destroy their target pathogen; instead they inhibit
its development.
Anti-viral
• Most of the antiviral drugs now available are
designed to help deal with
• HIV,
• herpes viruses,
• COVID-19,
• the hepatitis B and C viruses, and
• influenza A and B viruses.
• Researchers are working to extend the range of
antivirals to other families of pathogens.
Anti-viral
• Mechanism of Action (in combination or single
action)
• Inhibit viral attachment
• Prevent genetic copying of virus
• Prevent viral protein production, vital for
reproduction of virus.
Concept of antiviral surfaces, their action
mechanisms, and the application
Example of Anti-viral
• Antiherpesvirus
• acyclovir and ganciclovir
• Anti-influenza
• Amantadine and rimantadine Zanamivir, peramivir, and
oseltamivir
• Anti-HIV
• zidovudine, didanosine, zalcitabine, lamivudine, and
stavudine
• Anti Respiratory syncytial virus (RSV)
• Ribavirin
• Inteferon
• Represent a group of nonspecific antiviral proteins
produced by host cells in response to viral infections
3. Anti-Fungal Agent
• Pharmaceutical fungicide used to treat and
prevent mycosis
• Fungi include mushrooms, yeasts & molds.
• Fungal infections or mycosis occur in
immunocompromised patients.
• Common examples include athlete's foot, ringworm.
• Histoplasmosis capsulatum, Aspergillosis,
Blastomycosis, & Candida albicans (oral thrush).
• Mode of action;
• killing the fungus
• preventing the fungus from growing
Example of Anti-Fungal drug
• Amphotericin
• Clotrimazole
• Fluconazole
• Griseofulvin
• Itraconazole
• Ketonazole
• Metronidazole
• Micronazole
• Nystatin
• Terbination
4. Anti-parasites agent
• Antiparasitic drugs are a group of medications
used in the management and treatment of
infections by parasites, including protozoa,
helminths, and ectoparasites.
• Antiparasitic drugs include several classes of
drugs that cover a broad range of diseases
caused by parasites.
• Some common protozoa infections are malaria,
leishmaniasis, trypanosomiasis, amebiasis,
gardiasis and trichomoniasis.
•
Mode of action - Anti-parasites
• Anti malarial drugs differ depending on chemical
family to which they belong
• The 4-aminoquinoline deriatives work by inhibiting
deoxyribonucleic acid and ribonucleic acid
polymerase, enzymes essential to DNA and RNA
synthesis by the parasite cells.
NON-AEROSOLIZED ANTI-INFECTIVE
DRUGS ANTI-TUBERCULOSIS AGENTS
• The standard approach to treating tuberculosis
(TB) today consists of multiple first line drugs
for a period of either 6 or 9 months.
• First line drugs are:
• Rifapentine
• Isoniazid
• Rifampin
• Ethambutol
• Pyrazinamide
• Streptomycin used to be a front-line drug, but has been
replaced by Rifapentine.
NON-AEROSOLIZED ANTI-INFECTIVE
DRUGS ANTI-TUBERCULOSIS AGENTS
• 9 Month approach
• Isoniazid and Rifampin are given for 9 months and in an initial
2 to 8 week period these two drugs are supplemented with one
of the other first line drugs.
• 6 Month approach
• Four drugs are used for 2 months followed by 4 months of
Isoniazid and Rifampin.
• There is an association of TB and HIV infection.
• Along with the disturbing increase in the number of TB
cases in conjunction with AIDS, there has been an
emergence of drug resistant strains of TB. The cure
rate is poor in this subset.

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Unit 6 Anti-Infective agent.pdf

  • 1. Unit 6 : Anti-Infective Agents HCSP 1232 Intro to Pharma Roszan Sapon
  • 2. Objective • Definition, class, mode of action and example of drug ; • Anti-infective • Antibiotic • Antiviral • Antifungal • Antiparasites
  • 3. Some terminology • Pathogen: Disease causing microorganism. • Empiric: Therapy that is started based upon on experience and precedent in the observation and treatment of disease. • Normal flora: Organisms found in various parts of the body living symbiotically. • Aerobic: Requires oxygen to survive. • Anaerobic: Does not require oxygen to survive.
  • 4. • Gram Stain: Laboratory test used to determine if an organism is gram-positive or gram- negative. • C & S: Culture and sensitivity. Determines the organism present in the culture and the antibiotic to which it is sensitive (susceptible to). • Fungicide / fungistatic: To kill fungus • Mycosis: Disease cause by fungus Some terminology - cont
  • 5. Definition • Anti-infective : An agent that is capable of acting against infection, either by inhibiting the spread of an infectious agent of by killing the infectious agent outright. • Antibiotic: Substance that kills microorganism growth (mostly bacteria). • Antiviral : Class of medication used for treating viral infections • Antifungal : Pharmaceutical fungicide used to treat and prevent mycosis • Antiparasites : Drugs used to treat parasitic diseases.
  • 7. 1. Antibiotic • An antibiotic is a type of anti-infective substance active against bacteria. • It is the most important of antibacterial agent for fighting infection. • Widely used in treatment and prevention of such infection. • Bacteriostatic: Inhibits replication of microorganisms and prevents growth. Does not kill bacteria. • Bacteriocidal: Kills the bacteria.
  • 8. Antibiotic - Mode of action • Mode of action : • They may either kill or inhibit the growth of bacteria. • Bacteriostatic: Inhibits replication of microorganisms and prevents growth. Does not kill bacteria. • Bacteriocidal: Kills the bacteria. Its may attack he structures of the microb including their nucleus.
  • 9. Antibiotic - Classes of Antibiotics
  • 10. Antibiotics - Types & Example • Beta Lactams • penicillins • cephalosporins (4 generations) • Broader coverage with each generation. • Aminoglycosides • tobramycin • Vancomycin • MRSA • Protein Synthesis Inhibitors • macrolides • tetracyclines • Folate Inhibitors • metronidazole
  • 11. Antibiotics - Penicillins • In 1928, Alexander Fleming noted that mold belonging to the genus Penicillium inhibited the growth of bacteria. Fleming called this unknown antibacterial substance penicillin. Ten years later, a group at Oxford University began to investigate penicillin in laboratory mice. Penicillin was hailed as a miracle drug and saved countless lives in World War II • Penicillins are antibiotics used to treat bacterial infections that are derived from the antibiotic penicillin.
  • 12. Uses for Penicillin • Penicillin antibiotics are used to treat many types of infections caused by susceptible bacteria. They are used to treat infections of the middle ear, sinuses, stomach and intestines, bladder, and kidney. They also are used for treating • pneumonia, • blood infections (sepsis), • uncomplicated gonorrhea, • meningitis, • endocarditis, and • other serious infections.
  • 13. • Penicillin V • Penicillin G (P fi zerpen, Permapen) • Amoxicillin/clavulonate (Augmentin) • Ampicillin (Unasyn) • Nafcillin (Nallpen) • Oxacillin (Bactocill) • Dicloxacillin • Cloxacillin Example of penicillin antibiotics
  • 14. Antibiotics - Cephalosporins • Cephalosporins are a large group of antibiotics derived from the mold Acremonium (previously called Cephalosporium). • Cephalosporins are bactericidal (kill bacteria) and work in a similar way to penicillins. • They bind to and block the activity of enzymes responsible for making peptidoglycan, an important component of the bacterial cell wall. • They are called broad-spectrum antibiotics because they are effective against a wide range of bacteria.
  • 15. Use for Cephalosporins • Cephalosporins may be used to treat infections caused by susceptible bacteria, such as: • Bone infections • Ear infections (eg, otitis media) • Skin infections • Upper respiratory tract infections • Urinary tract infections. Cephalosporins are not usually used as a fi rst- choice antibiotic. They tend to be reserved for use when other antibiotics (often penicillins) cannot be used.
  • 16. Example of Cephalosporins • There are currently five “generations” of cephalosporins, with each generation differing slightly in their antibacterial spectrum (ie, how effective they are at killing certain types of bacteria). • Within each generation, there are differences in terms of administration (such as oral or intravenous administration), absorption, excretion, and how long the activity of the cephalosporin lasts for in the body.
  • 17. Example of Cephalosporins - cont • Ancef and Kefazol (cefazolin) • Ceclor and Cefaclor (cefaclor) • Cefdinir. • Ceftin and Zinacef (cefuroxime) • Duricef (cefadroxil) • Keflex and Keftabs (cephalexin) • Maxipime (cefepime) • Rocephin (ceftriaxone)
  • 18. Antibiotics - Macrolides • Macrolide: One in a class of antibiotics that includes Biaxin (Clarithromycin), Zithromax (Azithromycin), Dificid (Fidoximycin), and Erythromycin. • The macrolides inhibit the growth of bacteria and are often prescribed to treat rather common bacterial infections. • In more technical terms, the macrolides are a group of antibiotics produced by various strains of Streptomyces (spore forming bacteria that grow slowly in soil or water as a branching filamentous mycelium similar to that of fungi) and have a complex chemical (macrocyclic) structure. They act by inhibiting protein synthesis, specifically by blocking the 50S ribosomal subunit. They are broad spectrum antibiotics.
  • 19. Antibiotics - Quinolones • A quinolone antibiotic is a member of a large group of broad-spectrum bacteriocidals that share a bicyclic core structure related to the substance 4-quinolone. • They are used in human and veterinary medicine to treat bacterial infections, as well as in animal husbandry. • Nearly all quinolone antibiotics in use are fluoroquinolones, which contain a fluorine atom in their chemical structure and are effective against both Gram-negative and Gram-positive bacteria. • One example is ciprofloxacin, one of the most widely used antibiotics worldwide.
  • 20. Antibiotics - Tetracyclines • Tetracyclines have a broad spectrum of activity against many gram-positive and gram-negative bacteria as well as Mycoplasma, Chlamydia, Rickettsiae, Plasmodia, and amoebae. • They are usually bacteriostatic. • Tetracyclines bind reversibly to the small subunits of bacterial (and eukaryotic) ribosomes where they interfere with binding of charged-tRNA to the "Acceptor" site. • Tetracyclines can also inhibit protein synthesis in the host, but are less likely to reach the concentration required because eukaryotic cells do not have a tetracycline uptake mechanism.
  • 21. Use of Tetracyclines • Tetracyclines are used widely in both human and veterinary medicine; for example, tetracyclines have been used: • For the prevention of malaria • For the treatment of moderate-to-severe acne or rosacea • To treat anthrax • To treat infections of the eye, gastrointestinal tract, genitourinary tract, gums, respiratory tract, and skin • To treat infections caused by lice, mites, or ticks (such as Rocky Mountain spotted fever, typhus fever) • To treat infections caused by Campylobacter, Chlamydiae, Yersinia pestis (plague), Vibrio cholerae (cholera) and other atypical organisms • To treat respiratory tract infections caused by Mycoplasma pneumoniae • As a growth promoter in animals.
  • 22. Use of Tetracyclines • Because many strains of microorganisms are now resistant to some tetracyclines, culture and susceptibility testing is recommended before beginning treatment. • Doxycycline is a tetracycline that may be considered when penicillin is contraindicated.
  • 23. Antibiotics - Aminoglycosides • Aminoglycosides are natural or semisynthetic antibiotics derived from actinomycetes. • Aminoglycosides are potent, broad-spectrum antibiotics that act through inhibition of protein synthesis. • They are commonly used in combination with drugs such as ampicillin. • For example, gentamicin, an aminoglycoside antibiotic that has gram-negative coverage, is used in combination with both an agent against gram-positive organisms and one that covers anaerobes. Because of their potential nephrotoxicity, aminoglycosides should be reserved as a last resort, for use in resistant or life- threatening infections. • In addition, aminoglycosides should be avoided during pregnancy.
  • 24.
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  • 26. 2. Anti-Viral Agents • Antiviral drugs are a class of medication used for treating viral infections. • Most antivirals target specific viruses, while a broad-spectrum antiviral is effective against a wide range of viruses. • Unlike most antibiotics, antiviral drugs do not destroy their target pathogen; instead they inhibit its development.
  • 27. Anti-viral • Most of the antiviral drugs now available are designed to help deal with • HIV, • herpes viruses, • COVID-19, • the hepatitis B and C viruses, and • influenza A and B viruses. • Researchers are working to extend the range of antivirals to other families of pathogens.
  • 28. Anti-viral • Mechanism of Action (in combination or single action) • Inhibit viral attachment • Prevent genetic copying of virus • Prevent viral protein production, vital for reproduction of virus.
  • 29. Concept of antiviral surfaces, their action mechanisms, and the application
  • 30. Example of Anti-viral • Antiherpesvirus • acyclovir and ganciclovir • Anti-influenza • Amantadine and rimantadine Zanamivir, peramivir, and oseltamivir • Anti-HIV • zidovudine, didanosine, zalcitabine, lamivudine, and stavudine • Anti Respiratory syncytial virus (RSV) • Ribavirin • Inteferon • Represent a group of nonspecific antiviral proteins produced by host cells in response to viral infections
  • 31. 3. Anti-Fungal Agent • Pharmaceutical fungicide used to treat and prevent mycosis • Fungi include mushrooms, yeasts & molds. • Fungal infections or mycosis occur in immunocompromised patients. • Common examples include athlete's foot, ringworm. • Histoplasmosis capsulatum, Aspergillosis, Blastomycosis, & Candida albicans (oral thrush). • Mode of action; • killing the fungus • preventing the fungus from growing
  • 32. Example of Anti-Fungal drug • Amphotericin • Clotrimazole • Fluconazole • Griseofulvin • Itraconazole • Ketonazole • Metronidazole • Micronazole • Nystatin • Terbination
  • 33. 4. Anti-parasites agent • Antiparasitic drugs are a group of medications used in the management and treatment of infections by parasites, including protozoa, helminths, and ectoparasites. • Antiparasitic drugs include several classes of drugs that cover a broad range of diseases caused by parasites. • Some common protozoa infections are malaria, leishmaniasis, trypanosomiasis, amebiasis, gardiasis and trichomoniasis. •
  • 34. Mode of action - Anti-parasites • Anti malarial drugs differ depending on chemical family to which they belong • The 4-aminoquinoline deriatives work by inhibiting deoxyribonucleic acid and ribonucleic acid polymerase, enzymes essential to DNA and RNA synthesis by the parasite cells.
  • 35.
  • 36. NON-AEROSOLIZED ANTI-INFECTIVE DRUGS ANTI-TUBERCULOSIS AGENTS • The standard approach to treating tuberculosis (TB) today consists of multiple first line drugs for a period of either 6 or 9 months. • First line drugs are: • Rifapentine • Isoniazid • Rifampin • Ethambutol • Pyrazinamide • Streptomycin used to be a front-line drug, but has been replaced by Rifapentine.
  • 37. NON-AEROSOLIZED ANTI-INFECTIVE DRUGS ANTI-TUBERCULOSIS AGENTS • 9 Month approach • Isoniazid and Rifampin are given for 9 months and in an initial 2 to 8 week period these two drugs are supplemented with one of the other first line drugs. • 6 Month approach • Four drugs are used for 2 months followed by 4 months of Isoniazid and Rifampin. • There is an association of TB and HIV infection. • Along with the disturbing increase in the number of TB cases in conjunction with AIDS, there has been an emergence of drug resistant strains of TB. The cure rate is poor in this subset.