Study sets matching "nucleic acid inhibitors"

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Study sets matching "nucleic acid inhibitors"

57 terms
Nucleic Acid Inhibitors
TRUE
anaerobes
chronic inflammatory bowel disease (an…
Pradofloxacin
3rd and 4th generation drugs are characterized by less resist…
3rd and 4th generation drugs will add this to spectrum
A (probable) non bacterial indication for metronidazole
A 3rd generation FQ recently approved in the USA for cats
TRUE
3rd and 4th generation drugs are characterized by less resist…
anaerobes
3rd and 4th generation drugs will add this to spectrum
11 terms
Nucleic Acid Inhibitors
What are the 3 classes of antibiotics…
Are nucleic acid inhibitors bacteriost…
From what class are the antibiotics Ci…
From what class is the drug Metronidaz…
1. Fluoroquinolones... 2. Nitromidazoles... 3. Rifmycins
Cidal
"-floxacin " indicates Fluroquinolone Nucleic Acid inhibitors
"-dazole" indicates Nitromidazole, also think Metro similar t…
What are the 3 classes of antibiotics…
1. Fluoroquinolones... 2. Nitromidazoles... 3. Rifmycins
Are nucleic acid inhibitors bacteriost…
Cidal
Metabolic Inhibitors and Nucleic Acid Inhibitors
Trimethoprim ... Sulfamethoxazole... Dapsone
they all act on certain metabolic step…
1 to 5
Sulfonamides are competitive inhibitor…
what are the three metabolic inhibitors we need to know?
what is the MOA of the metabolic inhibitors?
what is the ratio of trimethoprim to sulfamethoxazole ratio i…
where specifically in the pathway do the sulfonamides act on…
Trimethoprim ... Sulfamethoxazole... Dapsone
what are the three metabolic inhibitors we need to know?
they all act on certain metabolic step…
what is the MOA of the metabolic inhibitors?
48 terms
Antibiotics: Nucleic Acid Inhibitors
Nucleic Acid Synthesis Inhibitors: (2)
__________ inhibit enzymes that mainta…
________ block prokaryotic RNA polymer…
Quinolones and Fluoroquinolines: table
1. Fluoroquinolones... 2. Rifamycin
Fluoroquinolones
Rifamycin
Nucleic Acid Synthesis Inhibitors: (2)
1. Fluoroquinolones... 2. Rifamycin
__________ inhibit enzymes that mainta…
Fluoroquinolones
39 terms
Nucleic Acid Synthesis Inhibitors
Objectives slide
Target of Nucleic Acid Synthesis Inhib…
What is folic acid?
Introduction
DNA
Humans need folic acid in our DIET... Important in the formatio…
Objectives slide
Target of Nucleic Acid Synthesis Inhib…
DNA
Nucleic Acid Inhibitors
T/F: 3rd and 4th generation drugs are…
3rd and 4th generation drugs will add…
A (probable) non bacterial indication…
A 3rd generation FQ recently approved…
True
anaerobes
chronic inflammatory bowel disease and giardia
Pradofloxacin
T/F: 3rd and 4th generation drugs are…
True
3rd and 4th generation drugs will add…
anaerobes
10 terms
Nucleic Acid Synthesis Inhibitors
Fluoroquinolones
Antifolates
Sulfonamides
Trimethoprim
Inhibit the action of Topoisomerase II in G- bacteria ... Topois…
Sulfonamides, Folate reductase inhibitors (trimethoprim)
Acts by inhibiting dihydropteroate synthetase... Absorbed and e…
Inhibitor of bacterial dihydrofolate reductase ... It s used in…
Fluoroquinolones
Inhibit the action of Topoisomerase II in G- bacteria ... Topois…
Antifolates
Sulfonamides, Folate reductase inhibitors (trimethoprim)
Nucleic acid synthesis inhibitors
Name 5 Nucleic Acid Synthesis inhibitors
MOA of quinolones. Example of a drug
MOA of Nitroimidazoles. Example
MOA of Nitrofuran. Example
Quinolones... Nitroimidazoles... Nitrofurans... Sulfonamides... Dihydrofo…
Inhibitors DNA gyrase (unwinds DNA) and Topoisomerase IV (sep…
Metronidazole interacts with the anaerobic bacterial oxidored…
Nitrofurantoin is reduced by Nitrofuran reductase to form a t…
Name 5 Nucleic Acid Synthesis inhibitors
Quinolones... Nitroimidazoles... Nitrofurans... Sulfonamides... Dihydrofo…
MOA of quinolones. Example of a drug
Inhibitors DNA gyrase (unwinds DNA) and Topoisomerase IV (sep…
7 terms
Nucleic Acid Synthesis Inhibitors
Nucleic Acid Synthesis Inhibitors
Trimethoprim/Sulfamethoxazole Mechanis…
Trimethoprim/SulfamethoxazoleToxicities
Trimethoprim/Sulfamethoxazole Antibiot…
Trimethoprim/Sulfamethoxazole... Quinolones (-floxacin)
Inhibit Dihydrofolate Reductase, inhibiting the production of…
Rash --> Steven Johnson Syndrome... Interstitial Nephritis
MRSA, MSSA
Nucleic Acid Synthesis Inhibitors
Trimethoprim/Sulfamethoxazole... Quinolones (-floxacin)
Trimethoprim/Sulfamethoxazole Mechanis…
Inhibit Dihydrofolate Reductase, inhibiting the production of…
23 terms
Nucleic acid synthesis inhibitors
Fluoroquinolone
Fluoroquinolone
Fluoroquinolone
Nitroimidazoles
Synthetic agents that inhibit DNA gyrase
Antibacterial
Ciprofloxacin
anaerobic conditions reduce the molecule which damages DNA an…
Fluoroquinolone
Synthetic agents that inhibit DNA gyrase
Fluoroquinolone
Antibacterial
7 terms
Nucleic Acid Synthesis Inhibitors
Fluoroquinolones
Rifamycin
Nalidixic Acid
Ciprofloxacin
Inhibit enzymes that maintain the supercoiling of closed circ…
Block prokaryotic RNA polymerase from inhibiting transcription
A quinolone used for treatment of UTI E.coli. Klebsiella, Ent…
A Fluroquinolone useful for treatment of many systemic infect…
Fluoroquinolones
Inhibit enzymes that maintain the supercoiling of closed circ…
Rifamycin
Block prokaryotic RNA polymerase from inhibiting transcription
Nucleic Acid Synthesis Inhibitors
Topoisomerase Inhibitors
Quinolones/Fluoroquinolones (FQs) MOA
FQs Spectrum
FQ 1st Generation EXAMPLE
Quinolones... Fluoroquinolones (FQs)
MOA - inhibit DNA replication by interfering with the action…
Broad G- coverage... Newer, "respiratory" FQs with improved G+…
Nalidixic acid - not used now
Topoisomerase Inhibitors
Quinolones... Fluoroquinolones (FQs)
Quinolones/Fluoroquinolones (FQs) MOA
MOA - inhibit DNA replication by interfering with the action…
15 terms
Nucleic Acid Inhibitors
Sulfonamides Mechanism of Action
Activity
Toxicities
Drug interactions
They are a structural analogue for PABA, so inhibit bacteria…
Many gram positive and negatives, a Actinomyces, Chlamydia, P…
1. Less soluble sulfonamides (sulfadiazine, sulfathiazole) ar…
Displaces warfarin, methotrexate, chlorpropamide, and tolbuta…
Sulfonamides Mechanism of Action
They are a structural analogue for PABA, so inhibit bacteria…
Activity
Many gram positive and negatives, a Actinomyces, Chlamydia, P…
17 terms
Nucleic Acid Inhibitors
Sulfacytine
Sulfisoxazole
Sulfamethizole
Sulfadiazine
Sulfonamide.
Sulfonamide
Sulfonamide
Sulfonamide
Sulfacytine
Sulfonamide.
Sulfisoxazole
Sulfonamide
28 terms
Nucleic Acid Synthesis Inhibitors
Naldixic Acid
Norfloxacin
Ofloxacin
Topoisomerase I
1st generation quinolone... Urinary infxn (mostly G-, minor effe…
2nd generation quinolone (similar to Cipro)... - Treat UTIs... - Ac…
2nd generation quinolone
Cuts ONE strand of DNA, opens up negative supercoil in bacter…
Naldixic Acid
1st generation quinolone... Urinary infxn (mostly G-, minor effe…
Norfloxacin
2nd generation quinolone (similar to Cipro)... - Treat UTIs... - Ac…
27 terms
Nucleic Acid Inhibitors
Sulfonamides
Sulfonamide Drug Type
Sulfonamide Mechanism
Sulfonamide Resistance
Sulfamethoxazole, Sulfadiazine, Sulfasalazine, Sulfacetamide,…
Bacteriostatic, until combined with Trimethoprim
Inhibits dihydropteroate synthetase
Neiserraie, Strep, Staph, Shigella, E. coli
Sulfonamides
Sulfamethoxazole, Sulfadiazine, Sulfasalazine, Sulfacetamide,…
Sulfonamide Drug Type
Bacteriostatic, until combined with Trimethoprim
34 terms
Nucleic Acid Synthesis Inhibitors
Agents
Cellular targets
DNA gyrase (Topoisomerase II) function
Topoisomerase IV function
Rifamycin... Fidaxomycin... Fluoroquinolone... Metronidazole
DNA gyrase (Topoisomerase II)... Topoisomerase IV
Forms (-) supercoil by cutting, passing through, and reanneal…
Unknots by cutting and reannealing
Agents
Rifamycin... Fidaxomycin... Fluoroquinolone... Metronidazole
Cellular targets
DNA gyrase (Topoisomerase II)... Topoisomerase IV
22 terms
Nucleic Acid Inhibitors
sulfonamides: mechanism of action
sulfonamides: selective toxicity
sulfonamide activity
antimicrobial activity
inhibits bacterial folic acid synthesis... - folic acid consists…
- mammalian cells are unable to synthesize folic acid, but ca…
- usually bacteriostatic, exerting effect after several cell…
- active against many gram negative and gram positive organis…
sulfonamides: mechanism of action
inhibits bacterial folic acid synthesis... - folic acid consists…
sulfonamides: selective toxicity
- mammalian cells are unable to synthesize folic acid, but ca…
Nucleic Acid Synthesis Inhibitors
Fluoroquinolones
fluoroquinolone pharma
cipro
cipro use
ciprofloxacin (older)... levofloxacin, moxifloxacin (advanced or…
well absorbed in small intestine. but like tetracyclines: bin…
greatest ability against aerobic gram- bacilli.
UTI, osteomyelitis, chronic prostatitis/epididymitis, infecti…
Fluoroquinolones
ciprofloxacin (older)... levofloxacin, moxifloxacin (advanced or…
fluoroquinolone pharma
well absorbed in small intestine. but like tetracyclines: bin…
10 terms
Nucleic acid inhibitors
Sulfonamides
short half-life sulfonamides
intermediate half-life sulfonamides
long half-life sulfonamides
- class of nucleic acid inhibitors... - have free NH2 groups tha…
- sulfacytine... - sulfaoxazole... - sulfamethizole
- sulfadiazine... - sulfamethoxazole... - sulfapyridine
- sulfadoxine
Sulfonamides
- class of nucleic acid inhibitors... - have free NH2 groups tha…
short half-life sulfonamides
- sulfacytine... - sulfaoxazole... - sulfamethizole
19 terms
Bacterial Nucleic Acid inhibitors
Trimethoprim MOA
Trimethoprim Use
Trimethoprim Toxicity
Sulfonamides
-Inhibits bacterial dihydrofolate reductase. Bacteriostatic.
-Used in combination with sulfonamides (trimethoprim-sulfamet…
" TMP Treats Marrow Poorly."... -Megaloblastic anemia... -leukopeni…
-Sulfamethoxazole (SMX)... -Sulfisoxazole... -Sulfadiazine.
Trimethoprim MOA
-Inhibits bacterial dihydrofolate reductase. Bacteriostatic.
Trimethoprim Use
-Used in combination with sulfonamides (trimethoprim-sulfamet…
Nucleic Acid Synthesis Inhibitors
fluoroquinolones
fluoroquinolone moa
ciprofloxacin use
fluoroquinolone pharma
ciprofloxacin, levofloxacin, moxifloxacin
inhibits DNA gyrase and type IV topoisomerase
aerobic, gram-. UTI (E. coli), Osteomyelitis (P. aeruginosa),…
oral, IV, topical. absorbed in SI. like tetracyclines: bind d…
fluoroquinolones
ciprofloxacin, levofloxacin, moxifloxacin
fluoroquinolone moa
inhibits DNA gyrase and type IV topoisomerase
11 terms
Nucleic acid synthesis inhibitors
Topoisomerase inhibitors
FQ's
Second generation FQ
3rd generation FQ
Quinolones/Fluoroquinolones (FQs)... They inhibit DNA replicati…
Bactericidal and CONCENTRATION DEPENDENT killing ... Has broad…
Ciprofloxacin - UTI, GI and DOC for anthrax!
Levofloxacin - UTI, GI, URI and skin
Topoisomerase inhibitors
Quinolones/Fluoroquinolones (FQs)... They inhibit DNA replicati…
FQ's
Bactericidal and CONCENTRATION DEPENDENT killing ... Has broad…
7 terms
Nucleic Acid Inhibitors
Rifampin - Rifamycin group
Quinolones/ Fluoroquinolones
Norfloxacin (noroxin)
Ciprofloxacin (cipro)
Blocks transcription of DNA into RNA (inhibition of mRNA)... Can…
Block DNA replication in bacteria... Bind to enzyme called DNA g…
Broad spectrum... Blocks DNA replication
fights anthrax... Blocks DNA replication
Rifampin - Rifamycin group
Blocks transcription of DNA into RNA (inhibition of mRNA)... Can…
Quinolones/ Fluoroquinolones
Block DNA replication in bacteria... Bind to enzyme called DNA g…
22 terms
Nucleic Acid Synthesis Inhibitors
Nucleic Acid Synthesis Inhibitors
Fluoroquinolones Mechanism
Topoisomerase II
Topoisomerase IV
Target enzymes required for nucleic acid synthesis... Quinolone…
ENTER HOST CELLS (active against intracellular pathogens),…
DNA Gyrase... Relieves tension in ds DNA, relaxes supercoils
Separates & unlinks DNA for the next DNA replication
Nucleic Acid Synthesis Inhibitors
Target enzymes required for nucleic acid synthesis... Quinolone…
Fluoroquinolones Mechanism
ENTER HOST CELLS (active against intracellular pathogens),…
56 terms
Antimetabolites/Nucleic Acid Inhibitors
sulfonamides
trimethoprim
antimetabolites mimic substrates of
sulfonamides mimic and compete with
antimetabolite
antimetabolite
metabolic pathways
PABA (p-aminobenzoic acid)
sulfonamides
antimetabolite
trimethoprim
antimetabolite
57 terms
Nucleic Acid Inhibitors
3rd and 4th generation drugs are chara…
3rd and 4th generation drugs will add…
A (probable) non-bacterial indication…
A 3rd generation FQ recently approved…
TRUE
anaerobes
chronic inflammatory bowel disease (and giardia)
Pradofloxacin
3rd and 4th generation drugs are chara…
TRUE
3rd and 4th generation drugs will add…
anaerobes
57 terms
Nucleic Acid Inhibitors
3rd and 4th generation drugs are chara…
3rd and 4th generation drugs will add…
A (probable) non bacterial indication…
A 3rd generation FQ recently approved…
TRUE
anaerobes
chronic inflammatory bowel disease (and giardia)
Pradofloxacin
3rd and 4th generation drugs are chara…
TRUE
3rd and 4th generation drugs will add…
anaerobes
57 terms
Nucleic Acid Inhibitors
3rd and 4th generation drugs are chara…
3rd and 4th generation drugs will add…
A (probable) non bacterial indication…
A 3rd generation FQ recently approved…
TRUE
anaerobes
chronic inflammatory bowel disease (and giardia)
Pradofloxacin
3rd and 4th generation drugs are chara…
TRUE
3rd and 4th generation drugs will add…
anaerobes
57 terms
Nucleic Acid Inhibitors
3rd and 4th generation drugs are chara…
3rd and 4th generation drugs will add…
A (probable) non bacterial indication…
A 3rd generation FQ recently approved…
TRUE
anaerobes
chronic inflammatory bowel disease (and giardia)
Pradofloxacin
3rd and 4th generation drugs are chara…
TRUE
3rd and 4th generation drugs will add…
anaerobes
57 terms
Nucleic Acid Inhibitors
3rd and 4th generation drugs are chara…
3rd and 4th generation drugs will add…
A (probable) non bacterial indication…
A 3rd generation FQ recently approved…
TRUE
anaerobes
chronic inflammatory bowel disease (and giardia)
Pradofloxacin
3rd and 4th generation drugs are chara…
TRUE
3rd and 4th generation drugs will add…
anaerobes
57 terms
Nucleic Acid Inhibitors
3rd and 4th generation drugs are chara…
3rd and 4th generation drugs will add…
A (probable) non bacterial indication…
A 3rd generation FQ recently approved…
TRUE
anaerobes
chronic inflammatory bowel disease (and giardia)
Pradofloxacin
3rd and 4th generation drugs are chara…
TRUE
3rd and 4th generation drugs will add…
anaerobes
57 terms
Nucleic Acid Inhibitors
TRUE
anaerobes
chronic inflammatory bowel disease (an…
Pradofloxacin
3rd and 4th generation drugs are characterized by less resist…
3rd and 4th generation drugs will add this to spectrum
A (probable) non bacterial indication for metronidazole
A 3rd generation FQ recently approved in the USA for cats
TRUE
3rd and 4th generation drugs are characterized by less resist…
anaerobes
3rd and 4th generation drugs will add this to spectrum
Nucleic Acid Inhibitors
3rd and 4th generation drugs are chara…
3rd and 4th generation drugs will add…
A (probable) non bacterial indication…
A 3rd generation FQ recently approved…
TRUE
anaerobes
chronic inflammatory bowel disease (and giardia)
Pradofloxacin
3rd and 4th generation drugs are chara…
TRUE
3rd and 4th generation drugs will add…
anaerobes
15 terms
Nucleic Acid Inhibitors
Sulfonamides MOA
Trimethoprim MOA
1. Sufonamides are bacteriostatic or b…
How are sulfonamides selective for bac…
competitively inhibit the incorporation of para-aminobenzoic…
inhibitor of DHFR--blockade of synthesis of tetrahydrofolate
1. bacteriostatic... 2. bacterial killing is inhibited... 3. such…
-mammalian cells unable to synthesize folic acid but can abso…
Sulfonamides MOA
competitively inhibit the incorporation of para-aminobenzoic…
Trimethoprim MOA
inhibitor of DHFR--blockade of synthesis of tetrahydrofolate
57 terms
Nucleic Acid Inhibitors
3rd and 4th generation drugs are chara…
3rd and 4th generation drugs will add…
A (probable) non bacterial indication…
A 3rd generation FQ recently approved…
TRUE
anaerobes
chronic inflammatory bowel disease (and giardia)
Pradofloxacin
3rd and 4th generation drugs are chara…
TRUE
3rd and 4th generation drugs will add…
anaerobes
57 terms
Nucleic Acid Inhibitors
T/F: 3rd and 4th generation drugs are…
3rd and 4th generation drugs will also…
Non-bacterial indications for metronid…
A 3rd generation FQ recently approved…
True
anaerobes
1. chronic inflammatory bowel disease... 2. giardia
Pradofloxacin
T/F: 3rd and 4th generation drugs are…
True
3rd and 4th generation drugs will also…
anaerobes
101 terms
Nucleic Acid Synthesis Inhibitors
quinolones, metronidazole, rifampin
inhibit enzymes required for DNA repli…
dna gyrase
topoisomerase 4
nucleic acid synthesis inhibitors
quinolones mechanism of action
where do quinolones bind to in gram negative organisms
where do quinolones bind to in gram positive organisms
quinolones, metronidazole, rifampin
nucleic acid synthesis inhibitors
inhibit enzymes required for DNA repli…
quinolones mechanism of action
Inhibitors of nucleic acid synthesis
Rifamycin
Anti-tuberculosis
Ciprofloxacin and norfloxacin
Quinolones,fluoroquinolones,DNA Gyrase
Inhibits RNA synthesis:
Medication rifamycin
Examples of quinolones and fluoroquinolones:
__and__inhibits__.
Rifamycin
Inhibits RNA synthesis:
Anti-tuberculosis
Medication rifamycin
57 terms
Nucleic Acid Inhibitors
3rd and 4th generation drugs are chara…
3rd and 4th generation drugs will add…
A (probable) non bacterial indication…
A 3rd generation FQ recently approved…
TRUE
anaerobes
chronic inflammatory bowel disease (and giardia)
Pradofloxacin
3rd and 4th generation drugs are chara…
TRUE
3rd and 4th generation drugs will add…
anaerobes
10 terms
Nucleic Acid Inhibitors / Fluoroquinolones
Fluoroquinolones
Which ones accumulate in neutrophils a…
What are the important toxic effects.
We can use these antibiotics to treat
Nucleic Acid Inhibitors ... Type I ... Bacteriocidal ... Inhibit bacte…
1) Enrofloxcin... 2) Marbofloxicin ... 3) Orbifloxcin... (also Rifampi…
Photosensitvity in dogs and cats ... ARTHROPATHY ... Ocular Toxicit…
Mycoplasma and Rickettsia
Fluoroquinolones
Nucleic Acid Inhibitors ... Type I ... Bacteriocidal ... Inhibit bacte…
Which ones accumulate in neutrophils a…
1) Enrofloxcin... 2) Marbofloxicin ... 3) Orbifloxcin... (also Rifampi…
Nucleic acid synthesis inhibitors
what are the abx classes of nucleic ac…
what is the MOA for nucleic acid synth…
fluoroquinolones inhibit what two enzy…
Cipro... infection
fluoroquinolones... metronidazole
prevent DNA replication by inhibiting key enzymes involved in…
DNA gyrase... type IV topoisomerase
UTI's... osteomyelitis... chronic prostatitis/epididymitis... infectio…
what are the abx classes of nucleic ac…
fluoroquinolones... metronidazole
what is the MOA for nucleic acid synth…
prevent DNA replication by inhibiting key enzymes involved in…
57 terms
Nucleic Acid inhibitors
3rd and 4th generation drugs are chara…
3rd and 4th generation drugs will add…
A (probable) non bacterial indication…
A 3rd generation FQ recently approved…
TRUE
anaerobes
chronic inflammatory bowel disease (and giardia)
Pradofloxacin
3rd and 4th generation drugs are chara…
TRUE
3rd and 4th generation drugs will add…
anaerobes
6 terms
inhibitors of nucleic acid synthesis
inhibitors of nucleic acid synthesis
quinolones (nalidixic acid) and fluoro…
rifampin
metronidazole
competitive inhibition of essential nucleic acid precursor or…
inhibit bacterial DNA gyrase (the enzyme that controls DNA co…
inhibits transcription by binding to RNA polymerase and inhib…
causes breakage of microbial DNA (bacterial and parasitic DNA)
inhibitors of nucleic acid synthesis
competitive inhibition of essential nucleic acid precursor or…
quinolones (nalidixic acid) and fluoro…
inhibit bacterial DNA gyrase (the enzyme that controls DNA co…
Inhibitors of Nucleic Acid Synthesis
Sulfamethoxazole
Sulfadiazine
Sulfasalazine
Sulfacetamide
Sulfonamides... MOA: stops dihydropteroate synthase (PABA). com…
Sulfonamides... MOA: stops dihydropteroate synthase (PABA). com…
Sulfonamides... MOA: stops dihydropteroate synthase (PABA). com…
Sulfonamides... MOA: stops dihydropteroate synthase (PABA). com…
Sulfamethoxazole
Sulfonamides... MOA: stops dihydropteroate synthase (PABA). com…
Sulfadiazine
Sulfonamides... MOA: stops dihydropteroate synthase (PABA). com…
6 terms
Inhibitors of nucleic acid synthesis
Nalidixic acid- bacteriocidal
Nalidixic acid- mechanism of action
Ciproflaxacin- bacteriacidal
Ciproflaxacin-mechanism of action
Nalidixic acid is a quinolone antibacterial agent,it has mark…
Evidence exists for Nalidixic acid that its active metabolite…
Ciprofloxacin is a broad-spectrum antiinfective agent of the…
The mechanism of action of ciprofloxacin results from inhibit…
Nalidixic acid- bacteriocidal
Nalidixic acid is a quinolone antibacterial agent,it has mark…
Nalidixic acid- mechanism of action
Evidence exists for Nalidixic acid that its active metabolite…
54 terms
Inhibitors of nucleic acid synthesis
Can humans synthesize folate?
Can bacteria synthesize folate?
Where do antibiotics compete with...
Folate is utilized for DNA synthesis b…
No... - Must be provided in the diet
Yes... - From precursors like p-aminobenzoic acid (PABA)
PABA for active site on enzyme (dihydropteroate synthase)
Humans & Bacteria
Can humans synthesize folate?
No... - Must be provided in the diet
Can bacteria synthesize folate?
Yes... - From precursors like p-aminobenzoic acid (PABA)
nucleic acid synthesis inhibitors
what is the mechanism of nucleic acid…
will NASI harm the host?
which is the indication for NASI?
are NASI broad or narrow spectrum?
binds to DNA dependent RNA polymerase so it blocks initiation…
no, because of the differences between prokaryotic and eukary…
TB, leprosy and MAC pneumonia
broad
what is the mechanism of nucleic acid…
binds to DNA dependent RNA polymerase so it blocks initiation…
will NASI harm the host?
no, because of the differences between prokaryotic and eukary…
Antimetabolites (and Nucleic Acid Inhibitors)
Sulfonamides
Sulfonamides - resistance
Sulfonamides - pharmacokinetics
Sulfonamides - toxicities
-sulfisoxazole, sulfamethoxazole-trimethoprim (*co-trimoxaz…
-increased concentrations of pABA (outcompetes the drug)... -al…
-well absorbed orally... -distributes everywhere, *including CNS…
-allergy: 5% of patients, mostly rash & not severe... -nausea, s…
Sulfonamides
-sulfisoxazole, sulfamethoxazole-trimethoprim (*co-trimoxaz…
Sulfonamides - resistance
-increased concentrations of pABA (outcompetes the drug)... -al…
inhibitors of nucleic acid synthesis
Rifampin
Fidoxamin
Fluoroquinolones
Sulfonamides
RNA polymerase inhibitor... Induces metabolism of other drugs... Us…
RNA polymerase inhibitor... narrow spectrum... C. diff
Ciprofloxacin, levofloxacin, moxifloxacin... Inhibit DNA replica…
Indirect inhibition of DNA synthesis... Competitive inhibitor in…
Rifampin
RNA polymerase inhibitor... Induces metabolism of other drugs... Us…
Fidoxamin
RNA polymerase inhibitor... narrow spectrum... C. diff
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