Pharm Winter FInal Flashcards
Polyene macrolides
Amphotericin B
Nystatin
Liposomal membrane
Amphotericin B
Amphotericin B mechanism
Binds to sterols in fungal cell membrane
Must give parenterally
Amphotericin B
Causes nephrotoxicity and anemia from decreased erythropoietin release
Amphotericin B
Treats leishmaniasis, amebic meningoencephalitis and other protozoal infxns
Amphotericin B
Imidazoles
Miconazole
Ketoconazole
Triazoles
Itraconazole
Fluconazole
Azole mechanism of action
Inhibit sterol 14 alpha demethylase (a cytochrome p450 enzyme) in ergosterol synthesis causing buildup of lanosterol
Side effect from inhibiting steroid biosynthesis resulting in gynecomastia
Ketoconazole
Drug interactions by inhibiting P450 3A4 enzyme
Ketoconazole
Inhibits Cyt P450 thus affeting metabolism of cyclosporine, rifampin, and warfarin
Fluconazole and Itraconazole
Treats cryptococcal meningitis and oropharyngeal and vaginal candidiasis
Fluconazole
No parenteral formulation available
Itraconazole
Griseofulvin
Griseofulvin MOA
Disrupts mitotic spindle structure arresting metaphase of cell division
Deposited in keratin precursor cells
Griseofulvin
Ultramicrosize absorbed better
Griseofulvin
Only used for dermatophytoses (tineas) except tinea versicolor
Griseofulvin
Nystatin MOA
Binds to sterols in the fungal cell membrane
Too toxic for parenteral use
Nystatin
Nystatin is used for what
Candidal infxns
Tolnaftate MOA
Inhibits squalene monooxygenase leading to squalene accumulation
Mainly used against dermatophytoses (doesn’t say onnly for this though…)
Tolnaftate
Terbinafine
Terbinafine MOA
Inhibits squalene monooxygenase leading to squalene accumulation
Echinocandin
Caspofungin
Caspofungin MOA
Inhibits synthesis of Beta 1,3 D glucan into polysaccharite cell wall
Use of casponfungin
Aspergilloma and Esophageal Candidiasis
If given with cyclosporine, increased plasma levels
If given withinducers of drug clearance, decreased plasma levels
Caspofungin
Alternative to Ketoconazole since less toxic
Fluconazole
Alkylating agents
Mechlorethamine
Cyclophosphamide
Carmustine
Cisplatin
Antimetabolites
Methotrexate
Mercaptopurine
Fluorouracil
Cytarabine
Natural products
Daunorubicin Doxorubicin Vinblastine Vincristine Etoposide Paclitaxel
Hormonal agents
Prednisone
Dexamethasone
Tamoxifen
Kinase inhibitors
Imatinib
Monoclonal antibodies
Trastuzumab
Developed from mustard gas
Mechlorethamine
Cyclophosphamide
Nitrosureas
Carmustine
Platinum complexes
Cisplatin
Alkylating agents MOA
Damage DNA by transfering reactive alkyl groups to N7 guanine position
Causes DNA breaks and crosslinking of DNA
Requires metabolic activation by Cyt P450
Cyclophosphamide
Used for brain tumors
Carmustine
Nephro and Ototoxic
Cisplatin
Folic acid analog
Methotrexate
Methotrexate MOA
Inhibits dihydrofolate reductase
Cell cycle specific agents
Antimetabolites
What phase does Methotrexate effect
S phase
Used for psoriasis and RA
Methotrexate
Purine analogs
Mercaptopurine
Inhibits a number of enzymes of purine interconversion
Mercaptopurine
Converted to nucleotide form by HGPRT
Mercaptopurine
Metabolized by xanthine oxidase
Mercaptopurine
Inhibits xanthine oxidase
Allopurinol
Pyrimidine analogs
Fluorouracil
Cytarabine
Fluorouracil MOA
Inhibits Thimidylate synthetase in DNA synthesis
Cytarabine MOA
Inhibits DNA polymerase
Cancer antibiotic drugs/Anthracyclines
Daunorubicin
Doxorubicin
Daunorubicin and Doxorubicin MOA
ind to DNA between adjacent strands uncoiling DNA helix
Tetracycline ring gives antitumor activity
Daunorubicin
Doxorubicin
Dilated cardiomyopathy side effect
Daunorubicin
Doxorubicin
Used for acute non lymphocytic leukemia
Daunorubicin
How does vinblastine differ from vincristine
Vinblastine has methyl group
Vincristine has formyl group
What cell cycle stage is targeted by vinblastine and vincristine
Mitosis
Vinblastine/Vincristine MOA
Bind to tubulin of Microtubules leading to metaphase arrest
Etoposide MOA
Complexes with Topoisomerase 2 resulting in DNA breaks