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136 Cards in this Set

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Competitively inhibit enzyme dihydropteroate synthetase
PABA Antagonists
Bacteria cannot absorb
folic acid
Simplest sulfonamide structure, topical use
Sulfanilamide
Prodrug. Azo compound reduced in vivo to
sulfapyridine (PABA antagonist) and mesalamine (antiinflamatory)
Sulfasalazine
Indicated for Crohn’s Disease
Sulfasalazine
Prodrug. Metabolised in vivo to Cycloguanil (the inhibitor)
Proguanil
Mechanism of Isoniazid
Mycolic acid synthesis inhibitor
Undesired side effect - forms Shiff base with Vitamin B6
Isoniazid
Mechanism of Pyrazinamide
lowers pH
Mechanism of Ethambutol
Unknown, inhibits RNA synthesis
Mechanism of Aminosalicylic Acid
PABA competitive inhibitor
Mechanism of Ethionamide
Unknown, bacterial protein synthesis inhibitor
Mechanism of Cycloserine
Bacterial cell wall synthesis inhibitor, competes with D-alanine
Mechanism of Capreomycin
Unknown, protein synthesis inhibitor, binds 30S ribosome(?)
Cross-resistance with aminoglycoside antibiotics
Capreomycin
Mechanism of Rifapentine
Inhibitor of DNA-dependent RNA polymerase
10x more potent than rifampin for TB
Rifapentine
Treatment for TB which induces CYP3A4. Many drug interactions
Rifapentine
Mechanism of Dapsone
PABA competative inhibitor
Mechanism of Clofazimine
Binds preferentially to mycobacterial DNA
Mechanism of Rifampin
DNA-dependent RNA polymerase inhibitor
Mechanism of Thalidomide
Tumor necrosis factor (TNF) inhibitor
Red color - tan or black in human tissue
Clofazimine
Treated with Dapsone
Leprosy
Treated with Clofazimine
Leprosy
Treated with Rifampin
Leprosy
Treated with Thalidomide
Leprosy
Treated with Ethionamide
Leprosy and Tuberculosis
Treated with Isoniazid
Tuberculosis
Treated with Pyrazinamide
Tuberculosis
Treated with Ethambutol
Tuberculosis
Treated with Aminosalicylic Acid
Tuberculosis
Treated with Cycloserine
Tuberculosis
Treated with Capreomycin
Tuberculosis
Treated with Rifapentine
Tuberculosis
Drugs which treat fungi and disrupt the cell membrane
Amphotericin-B
Nystatin
Micafungin
Treats fungi; selective for ergosterol-containing membranes, increases cell potassium loss, and is orally active
Amphotericin-B
Treats fungi; selective for ergosterol-containing membranes, increases cell potassium loss, and is NOT orally active
Nystatin
Inhibits synthesis of 1-3-beta D-glucan,
a component of fungal cell wall
Micafungin
Echinocandin lipopeptide
Micafungin
Mechanism of Ketoconazole
Inhibits ergosterol synthesis
Mechanism of Econazole
Inhibits ergosterol synthesis
Mechanism of Clotrimazole
Inhibits ergosterol synthesis
Mechanism of Fluconazole
Inhibits ergosterol synthesis
Mechanism of Itraconazole
Inhibits ergosterol synthesis
Mechanism of Terconazole
Inhibits ergosterol synthesis
Mechanism of Voriconazole
Inhibits ergosterol synthesis
Mechanism of Terbinafine
Inhibits ergosterol synthesis
Mechanism of Butenafine
Inhibits ergosterol synthesis
Mechanism of Naftifine
Inhibits ergosterol synthesis
Imidazoles, P450 inhibitors, orally active
Miconazole
Ketoconazole
Econazole
Imidazole, P450 inhibitor, topical, NOT orally active with extra benzene ring
Clotrimazole
Triazoles, P450 inhibitors, orally active
Fluconazole
Itraconazole
Terconazole
Voriconazole
Non-P450 mechanism, Squalene epoxidase inhibitor, oral
Terbinafine
Non-P450 mechanisms, Squalene epoxidase inhibitors, NOT oral
Butenafine
Naftifine
Anti-fungal drug which is converted to 5-fluorouracil by a fungal enzyme
Flucytosine
Anti-fungal drug which disrupts mitotic spindle which inhibits mitosis
Griseofulvin
Anti-worm drug which inhibit ATP synthesis and oxidative phosphorylation
Niclosamide
Drugs which treat Cestodes
Niclosamide and Oxamniquine
Treats beef, fish, and dwarf tapeworm
Niclosamide
Works against shistosomes
Oxamniquine
Known mechanism of Oxamniquine
Makes female worms unable to lay eggs and they explode
Unknown mechanism of Oxamniquine
kills males
Treatments for trematodes
Praziquantel
Bithional
Increase cell calcium loss leading to worm paralysis
Praziquantel
Treatment for tapeworm
Praziquantel
Treatment for lung or liver flukes
Bithional
Treatment for pin, whip, round, or hookworms
Mebendazole
Treatment for threadworms or trichinosis
Thiabendazole
Treatment for round worm
Pyrantel
Treatment for filariasis
Diethycarbamazine
Treatment for adult filariasis
Suramin
Treatment for river blindness
Ivermectin
Damages protective cuticle and inhibits worm egg formation
Bithional
Three drugs which lead to worm paralysis
Praziquantel, Ivermectin and Pyrantel
Blocks worm glucose and nutrient uptake and kills selectively
Mebendazole
Mitochondrial fumurate reductase inhibitor which kills selectively
Thiabendazole
Cholinesterase inhibitor which releases acetylcholine and works in gi tract toparalyzes worms
Pyrantel
Utilizes an unknown mechanism to immobilize worms and make their surface membranes more susceptible to host defense mechanisms
Diethycarbamazine
Worm treatment which binds GABA receptors leading to worm paralysis
Ivermectin
Drug which is worm selective
Mebendazole
Inhibits oxidative phosphorylation which inhibit DNA and RNA synthesis in protozoa
Pentamidine
Inhibits ornithine decarboxylase
which inhibit polyamine synthesis in protozoa
Eflornithine
Blockades electron transport by unknown mechanism in protozoa
Atovaquone
dihydrofolate reductase inhibitor in protozoa; selective antidote
Trimetrexate / Leucovorin
Prodrug, reduced form binds DNA
increases DNA breakage in protozoa
Metronidazole
Have unknown mechanisms to treat Amoebiasis
Diloxanide, Iodoquinol and Emetine / Dehydroemetine
Poorly absorbed drug which treats Amoebiasis
Iodoquinol
Prodrug to diloxanide
Diloxanide Furoate
Aminoglycoside, poorly absorbed
40S ribosome binder, inhibits protein synthesis, treats Amoebiasis
Paramomycin
All drugs which treat Giardiasis have this mechanism
The mechanism is unknown
Treatments for Giardiasis with reversible yellowing of skin, resembles clofazimine
Quinacrine and Acranil
Treatment for Giardiasis which forms a Shiff base, used for children
Furazolidine
Treatment for Giardiasis with unknown antiinflammatory action
Tinidazole
Treatment for Giardiasis in Treatments for Giardiasis
Paramomycin
Treatment for Lishmaniasis with Pentavalent antimony and unknown mechanism
Sodium Stibogluconate
Two treatments for Lishmaniasis which inhibits
oxidative phosphorylation of and interfers with the incorporation of nucleic acids into RNA and
DNA in protozoa
Pentamidine and Stibamidine
Effective for treatment of lishmiasis resistent to antimonial drugs
Pentamidine and Stibamidine
Arsenic drug which treats Trypanosomiasis
Melarsoprol
Treatment for Trypanosomiasis which inhibits energy metabolism enzymes
Suramin
Treatment for Trypanosomiasis which works just like Pentamidine and Stibamidine
Eflornithine
Treatment for Trypanosomiasis which forms a Shiff base, like furazolidine, for cardiac muscle
Nifurtimox / cortisone
Treatment for Trypanosomiasis which is antiinflamatory, and works like tinidazole
Benznidazole
Two treatments for Malaria which raises internal pH, inhibits DNA synthesis
Chloroquine and Mefloquine
Treatment for Malaria which inhibits oxygen uptake and
metabolism disturbs calcium distribution
Quinine
Chloroquine, Quinine and Mefloquine treat
blood shizonts
Treatment for malaria which disrupts mitochondria, binds DNA G6PD
Primaquine
Treatment for malaria with hemolysis side effect
Primaquine
Treatment for malaria which is good to prevent relapses
Primaquine
Treatment for malaria which is a prodrug to dihydrofolate reductase inhibitor
Proguanil
Treatment for malaria which is a dihydrofolate reductase inhibitorwhich inhibits thymidine synthesis
Pyrimethamine
Tetracycline-like, IV only, not used during tooth development
Glycylcycline class
Anti-metabolites
such as folate antagonists are classified as
Protein synthesis inhibitors
It deactivates and is deactivated by vitamin B6
Isoniazid
Acts by inhibiting
mycolic acid synthesis, a unique mechanism
Isoniazid
Similar to amphotericin B but lacks double bond and folds up in water
Nystatin
Inhibits glucan synthesis, made of six peptides cyclized, given by injection only
Echinocandin lipopeptide
Kill parasites while they
reproduce asexually in the liver, before entry into the red blood cells
Tissue schizonticides
Destroy parasite in the red blood cells and can cure or prevent relapse of malaria
Blood schizonticides
Basis for selectivity of PABA inhibitors
Inability of bacteria to absorb folic acid
Selectively toxic because major cell membrane sterol
is cholesterol in humans and not ergosterol in fungi
Amphotericin B
Converted in fungal cells, but not in human cells,
into 5-fluorouracil (5-FU)
Flucytosine
Competitive inhibitors of dihydropteroate synthetase
Sulfonamides
Pharmacodynamically selective
Sulfonamides
Required for activity of sulfonamides
Proton on the sulfonamide nitrogen
Sulfonamides exhibit optimal activity when the pKa of the sulfonamide N hydrogen is between
6 and 8
The haptophore of sulfonamides minic PABA while the toxophile
competes with PABA for a binding site
For sulfonamides the haptophore is equal to the
toxophile
Sulfamethoxazole is used with
Trimethoprim because
They both have similar pattern of distribution and rate of elimination
Sulfamethoxazole with
Trimethoprim is marketed as
Co-trimoxazole
Drugs which inhibit the synthesis or utilization of folic acid are called
Antimetabolites
The most common predisposing factors to fungal growth in humans
Use of broad-spectrum
antibiotics
Upon biting the mosquito sporozites enter the body and infect the
Liver
Symptoms of malaria are present about every 48 hours due to
bursting of red blood cells
dormant parasites are called
hypnozoites
The depolarizing
neuromuscular blocking action of this drug overwhelms the worm’s nicotinic receptors and causes paralysis.
Pyrantel pamoate