No extra Final Drug - Sheet1 Flashcards
penicillin (beta-lactam), bactericidal, gram + cocci, syphilis, meningitides, cell wall synthesis inhibitor, inhibits transpeptidase the enzyme responsible for cell wall crosslinking, drug allergy
penicillin V
penicillin (beta lactam), bactericidal, greater against gram -, susceptible to beta lactamases, cell wall synthesis inhibitor, inhibits transpeptidase the enzyme responsible for cell wall crosslinking, drug allergy
amoxicillin
penicillin (beta lactam), bactericidal, cell wall synthesis inhibitor, inhibits transpeptidase the enzyme responsible for cell wall crosslinking, drug allergy
methicillin
first gen cephalosporin (beta lactam), bactericidal, most active against gram + cocci, cell wall synthesis inhibitor, inhibits transpeptidase the enzyme responsible for cell wall crosslinking, drug allergy
cephalexin
cephalosporin (beta lactam), bactericidal, cell wall synthesis inhibitor, inhibits transpeptidase the enzyme responsible for cell wall crosslinking, drug allergy
cefdinir
third gen cephalosporin (beta lactam), bactericidal, more active against gram - bacteria, increased resistance to beta lactamases, not eliminated by kidney, good CNS, cell wall synthesis inhibitor, inhibits transpeptidase the enzyme responsible for cell wall crosslinking, drug allergy
ceftriaxone
fourth gen cephalosporin (beta lactam), bactericidal, broadest spectrum, used to treat serious infections, resistant to man beta lactamases, good CNS, cell wall synthesis inhibitor, inhibits transpeptidase the enzyme responsible for cell wall crosslinking, drug allergy
cefepime
fifth gen cephalosporin (beta lactam), bactericidal, broad spectrum with resistance to many beta-lactamase, used for MRSA, cell wall synthesis inhibitor, inhibits transpeptidase the enzyme responsible for cell wall crosslinking, drug allergy
ceftaroline
bactericidal cell wall synthesis inhibitor, inhibits cell wall cross-linking by binding D-Ala-D-Ala within the peptidoglycan monomer subunit, only effective at killing gram + bacteria, effective for MRSA, not absorbed orally, used for c. diff, nephrotoxicity, infusion reaction, “red man”
vancomycin
bacteriostatic macrolide, protein synthesis inhibitor, prevents peptide elongation, CYP3A4 inhibitor, QT prolongation, e
erythromycin
bacteriostatic macrolide, protein synthesis inhibitor, prevents peptide elongation, CYP3A4 inhibitor, QT prolongation
clarithromycin
bacteriostatic macrolide, protein synthesis inhibitor, prevents peptide elongation, QT prolongation
azithromycin
bacteriostatic protein synthesis inhibitor, binds to same site as the macrolides, drug allergy, c. diff infection
clindamycin
bacteriostatic tetracycline, protein synthesis inhibitor, zoonotic pathogens, atypicals, and MRSA, bone and tooth development, tooth staining, photosensitivity
doxycycline
bactericidal, anaerobic bacteria (including c. diff) metabolize drug to a DNA damaging agent thereby interfering with DNA synthesis, alcohol (like disulfiram) interactions, potentially mutagenic (avoid in pregnant and nursing women)
metrodinazole
bactericidal aminoglycoside, protein synthesis inhibitor (clock initiation, cause premature termination of elongation, cause misincorporation of amino acids, bactericidal for aerobes only, prolonged post-antibiotic effect, ototoxicity, nephrotoxicity
gentamicin
bascteriostatic (bactericidal for e. coli) sulfonamide and trimethoprim, antimetabolites, inhibit folate synthesis, hypersensitivity, photosensitivity, hemolytic anemia in GGP deficiency
bactrim
bactericidal fluoroquinolone, inhibit DNA gyrase (gram -) and/or topo IV (gram +)leading to inhibition of DNA synthesis and DNA damage, use for UTI, tendon rupture, QT prolongation, peripheral neuropathy, CNS effects
ciprofloxacin
bactericidal fluoroquinolone, inhibit DNA gyrase (gram -) and/or topo IV (gram +), ised for UTIs, enahnced gram + activity, leading to inhibition of DNA synthesis and DNA damage, tendon rupture, QT prolongation, peripheral neuropathy, CNS effects
levofloxacin
bactericidal, anti-TB, mycobacterium cell wall synthesis inhibitor, inhibits biosynthesis of mycolic acid, peripheral neuropathy, hepatotoxicity (B6)
isoniazid
bactericidal, anti-TB, bacterial RNA polymerase inhibitor, induce p450 enzymes, hepatotoxicity
rifampin
topical polyene for yeast infections, fungicidal, binds to ergosterol and disrupts fungal cell membranes creating pores and leaks, well tolerated
nystatin
systemic polyene, fungicidal, binds to ergosterol and disrupts fungal cell membranes creating pores and leaks, broad spectrum against many yeasts and molds, renal toxicity, fever and chills (shake and bake), nephrotoxicity
amphotericin B
imidazole, inhibit ergosterol synthesis - lanosterol 14-a demethylase - fungal cell membranes integrity decreases, for mycoses except meningitis b/c no CNS, well tolerated topically, potent inhibitor of many CYPs
ketoconazole
imidazole, inhibit ergosterol synthesis - lanosterol 14-a demethylase - fungal cell membranes integrity decreases, well tolerated topically, variety of dosage forms
clotrimazole
imidazole, inhibit ergosterol synthesis - lanosterol 14-a demethylase - fungal cell membranes integrity decreases, well tolerated topically
miconazole
systemic triazole, inhibit ergosterol synthesis, fungal membrane integrity decreases, narrow spectrum, prevent yeast infections in patients with lowered immunity (Candida), CNS penetration, elimination kidney dependent, inhibits p450, hepatotoxicity, QT prolongation, pregnancy
fluconazole
systemic triazole, inhibit ergosterol synthesis, fungal membrane integrity decreases, CNS penetration, broader spectrum against molds, elimination in liver, broader spectrum, visual disturbances, inhibits p450, hepatotoxicity, QT prolongation, pregnancy
voriconazole
systemic triazole, no CNS, inhibit ergosterol synthesis, fungal membrane integrity decreases, with food, negative inotropic, inhibits p450, absorption pH dependent, hepatotoxicity, QT prolongation
itraconazole
echinocandin, inhibits beta-D-glucan synthase fungal ecll wall synthesis, systemic, no CNS, candida and aspergillis infections, infusion reactions, hypersensitivity
caspofungin
echinocandins, inhibits beta-D-glucan synthase cell wall synthesis, systemic, no CNS, candida and aspergillis infections, infusion reactions, hypersensitivity
micafungin
inhibits viral DNA synthesis, only effective on replicating viruses, converted by virally encoded thymidine kinase, competitive inhibitor of DNA polymerase, chain thermination, first drug for herpes and shingles, rare nephrotoxicity
acyclovir
inhibits viral DNA synthesis, for herpes and shingles, longer half-life than acyclovir, better bioavailability, rare nephrotoxicity
valacyclovir
inhibits viral DNA synthesis, IV only, nucleoside analog selectively phosphorylated by CMV kinase in human and CMV, resistance from mutation of kinase, for CMV, bone marrow suppression, teratogenic
ganciclovir
inhibits viral DNA synthesis, prodrug taken orally, nucleoside analog selectively phosphorylated by CMV kinase in human and CMV, resistance from mutation of kinase, for CMV, bone marrow suppression, teratogenic
valganciclovir
NRTI ‘nuke’, guanosine analog, inhibits HIV reverse transcriptase by incorporating into viral DNA cuaising chain termination, little activity towards our DNA polymerase, anemia and neutropenia, muscle weakness, peripheral neuropathy, lactic acidosis
abacavir
NRTI ‘nuke’, cytosine analog, inhibits HIV reverse transcriptase by incorporating into viral DNA causing chain termination, little activity towards our DNA polymerase, anemia and neutropenia, muscle weakness, peripheral neuropathy, lactic acidosis
lamivudine
NRTI ‘nuke’, adenosine analog, inhibits HIV reverse transcriptase by incorporating into viral DNA cuaising chain termination, little activity towards our DNA polymerase, anemia and neutropenia, muscle weakness, peripheral neuropathy, lactic acidosis
tenofovir
NRTI ‘nuke’, also cytosine analog, inhibits HIV reverse transcriptase by incorporating into viral DNA cuaising chain termination, little activity towards our DNA polymerase, anemia and neutropenia, muscle weakness, peripheral neuropathy, lactic acidosis
emtricitabine
non-nuke’, inhibits HIV reverse transcriptase, allosteric inhibitor, CNS effects, neurological effects, hepatotoxicity, induce p450s
efavirenz
PI, inhibit viral protease necessary for processing viral proteins and maturation or viral particles, for HIV, pharmacokinetic booster, altered glucose and lipid metabolism, altered fat distribution, with PK booster with drug interactions
ritonavir
PI, inhibit viral protease necessary for processing viral proteins and maturation or viral particles, for HIV, altered glucose and lipid metabolism, altered fat distribution, p450 metabolized, a
atazanavir
PI, inhibit viral protease necessary for processing viral proteins and maturation or viral particles, for HIV, altered glucose and lipid metabolism, altered fat distribution, p450 metabolized
darunavir
INSTI, blocks integration of the HIV cDNA into the human genome, relatively few
raltegravir
INSTI, blocks integration of the HIV cDNA into the human genome, relatively few, d
dolutegravir
cytotoxic DNA alkylating agent, metabolized by p450 to active form that forms crosslink with DNA, phase non-specific, myelosuppression, bladder toxicity (treat with MESNA)
cyclophosphamide
cytotoxic DNA platinating agent, react with H2O to form active platinum compounds that react with DNA forming crosslinks with DNA, phase non-specific, nephrotoxicity, ototoxicity, peripheral neuropathy
cisplatin
cytotoxic DNA platinating agent, react with H2O to form active platinum compounds that react with DNA forming crosslinks with DNA, phase non-specific, myelosuppression
carboplatin
cytotoxic DNA platinating agent, react with H2O to form active platinum compounds that react with DNA forming crosslinks with DNA, phase non-specific, peripheral neuropathy, acute cold sensitivity, nephrotoxicity, ototoxicity, myelosuppression
oxaliplatin
cytotoxic antimetabolite, inhibits human dihydrofolate reductase, deprives cells of tetrahydrofolate needed for dTMP, S phase specificmyelosuppression, GI mucositis, nephrotoxicity
methotrexate
cytotoxic antimetabolite, inhibits thymidylate synthesis, metabolized to FdUMP, S phase specific, myelosuppression and GI mucositis, palmar-plantar erythrodysesthesia
5-fluorouracil
cytotoxic microtubule inhibitor, vinblastine and vincristine, inhibit assembly, mitosis specific, peripheral neuropathy, myelosuppression (not vincristine), extravasation reactions, interactions with p450
vinca alkaloids
cytotoxic microtubule inhibitor, stabilizes microtubules, stops depolymerization, mitosis specific, peripheral neuropathy, myelosuppression, extravasation, interacts with p450s
paclitaxel
cytotoxic topo 2 inhibitor, causes double strand breaks, traps topo 2, S/G2 phase specific, myelosuppression, cardiotoxicity, vesicant
doxorubicin
cytotoxic topo 1 inhibitor, cause replication associated double strand breaks, traps topo 1, S phase specific, myelosuppression, acute diarrhea, late onset diarrhea
irinotecan
BCR-ABL tyrosine kinase that causes CML inhibitor, first protein kinase inhibitor for cancer
imatinib
EGFR tyrosine kinase inhibitor, first generation, ATP competitive inhibitor, primarily for non-small cell lung cancer, acneiform rash
erlotinib and osimertinib
monoclonal antibody targeting, EGFR (HER1), binds to receptor and prevents ligand binding, promotes EGFR degradation, triggers antibody-dependent cell cytotoxicity, acneiform rash
cetuximab
monoclonal human antibody, HER2, prevents dimerization, cardiotoxicity
trastuzumab
monoclonal that reverse brakes on the immune system, CTLA inhibitor, allows signal 2 to activate T cells, autoimmunity
ipilimumab
monoclonal that reverse brakes on the immune system, PD1 inhibitor, PD1 would prevent T cells from killing cancer cells, autoimmunity
pembrolizumab
