Block 3 Bolded Drugs Part 2 Flashcards
Amikacin
Aminoglycoside: binds to 30S ribosome to stop initiation of protein synthesis.
Used for tobramycin and gentamicin ressistant strain.
Amoxicillin
1 choice for pediatric otitis media and an alternate choice for lyme disease
B-lactam that treats gram + and gram - that don’t make B lactamases: listeria, strep, enterococcus.
Oral only
Ampicillin
B lactam that treats gram + and - that don’t make B lactamases such as listeria, strep, and enterococcus.
Oral or IV
Treats meningitis and GI infections (amox doesnt)
Azithromycin
Macrolide: binds to 50S ribosome to block translocation
Common for outpatient respiratory tract infections and genital infections.
Aztreonam
Used against gram - aerobic rods; no cross allergic reactions with B-lactams
Bacitracin
Topical use only
Interferes with carrier that moves early cell wall components through the cell membrane
Bacteriocidal
Inhibits bacterial growth
Effective at the minimal inhibitory concentration (MIC)
Bacteriostatic
Kills the bacteria
Effective at minimal bacteriocidal concentration (MBC)
Cefazolin
1st generation cephalosporin
Best gram + activity of the 1st gens
Longer half life: 1-2 hrs
Cefepime
4th generation cephalosporin
Spectrum like ceftazidime except more B-lactamase resistant
Used to treat severe inpatient infections
Cefoxitin
2nd generation cephalosporin with good tolerance to many gram - B-lactamases
Good for anaerobes and some strains of bacteroides fragilis
Ceftazidime
3rd generation cephalosporin
Most active 3rd gen against pseudomonas aeruginosa, poorest for gram +
Short half life: ~90 min
Ceftriaxone
3rd gen cephalosporin good for types of meningitis and drug of choice for gonorrhea.
Half life: 6-9 hrs
Cefuroxime
2nd generation cephalosporin; only second generation to penetrate the CSF
Best against haemophilus
Good tolerance to many gram - B-lactamases
Cephalexin
1st generation cephalosporin
Oral, half life of 50 minutes
Chloramphenicol
Interferes with binding of aminoacyl tRNA to 50S subunit and inhibits peptide pond formation.
Very restricted use due to serious side effects
Ciprofloxacin
Fluoroquinolone - inhibits DNA gyrase
Good for UTIs, infectious diarrhea, bone/joint/skin infections.
Not good for gram + or respiratory infections
Clarithromycin
Macrolide - binds 50S to block translocation
Less freq dosing and less effects on GI motility than erythromycin
Clavulanic acid
B-lactamase inhibitor
B-lactamase analog that binds irreversibly to B-lactamase
Works with ampicillin, amoxicillin, ticarcillin, and pipercillin
Clindamycin
Binds 50S ribosomal subunit to block translocation
Significant cause of enterocolitis
Concentration-dependent killin
Peak concentration (Cmax) must be met
Aminoglycosides use this killing - as long as they hit a peak concentration, they can still have their effects below the MIC
Daptomycin
Binds bacterial cytoplasmic membrane causing rapid depolarization
Gram + spectrum
Doxycycline
Tetracycline used for PenG sensitive syphilis and uncomplicated N. gonorrhoeae
Least affinity for Ca2+
Erythromycin
Macrolide - binds to 50S to block translocation
Treats unusual bugs such as chlamydia, mycoplasma, legionella, campylobacter, and bordetella.
Mostly treats gram +
Fidamoxicin
Inhibitor of RNA polymerase and inhibits RNA synthesis
1st line therapy for C. diff
Oral admin with poor absorption (this is good for treatment of C. diff).
Fosfomycin
Blocks N-acetylmuramic acid from being made (needed for PG synthesis)
Treats uncomplicated UTI’s caused by E. coli or enterococcus.
Gentamicin
Aminoglycoside
Binds 30S ribosome to stop initiation of protein synthesis
Imipenem
Carbapenem with broad spectrum, resistant to many B-lactamases including extended spectrum beta lactamases
Killing dependent on concentration x time
AUC/MIC is most important for effectiveness
Generally want >125 hours for effectiveness
Quinolones
Linezolid
Inhibits protein synthesis by binding to the 50S subunit and preventing formation of the 70S initiation complex
Metronidazole
Anaerobes reduce nitro group to make product that damages DNA (cidal)
Minocycline
Tetracycline
For penG sensitive syphilis and uncomplicated gonorrhea.
Ca2+ binding < tetracycline and >doxycycline
Moxifloxacin
Fluoroquinolone - Inhibits DNA gyrase
Better at killing gram + than ciprofloxacin. Also treats respiratory infections.
Nitrofurantoin
Nitroreductase enzyme converts drug to reactive compound that damages DNA
Used for lower UTIs from e. coli, enterococcus, and staphylococcus
Norfloxacin
Fluoroquinolone inhibits DNA gyrase
Prototype for UTIs but NO LONGER used as 1st line for UTIs
Oxacillin
Methicillin-type drug used to treat B-lactamase + staphylococci
IV/IM
penicillin G and V
Anaerobes (esp gram +), gram positives that don’t make B lactamase like staph, a few gram negatives: neisseria meningitidis and spirochetes (syphilis).
V is oral
G is IV/IM
Piperacillin
Gram - spectrum like ticarcillin but also some pseudomonas and klebsiella, including those that are ticarcillin resistant.
Polymyxin B
Cationic detergent binds LPB in the OM of gram negatives
Topical use only
Rifampin
Binds/inhibits RNA pol B to inhibit RNA synthesis
Bactericidal
Treats TB and prophylaxis for meningitis from neisseria and haemophilus
Silver Sulfadiazine
Sulfonamide antibiotic
Competitive analog of p-aminobenzoic acid, a precursor in folate synthesis
Used topically for infection prevention in burn pts
Sulfamethoxazole
Sulfonamide antibiotic
Competitive analog of p-aminobenzoic acid, a precursor in folate synthesis
Often used with trimethoprim
Tazobactam
B-lactamase inhibitor
B-lactamase analog that binds irreversibly to B-lactamse
Works with ampicillin, amoxicillin, ticarcillin, and pipercillin.
Ticarcillin
Antibiotic with some gram + coverage, some anaerobes, and extended gram negative including pseudomonas aeruginosa.
Susceptible to B-lactamases
Tigecycline
Like tetracyclines, but also binds to additional unique sites of the ribosome and doesn’t have cross-resistance.
Last line drug due to increased risk of death.
Time dependent killing
Amount (%) of time above the minimal inhibitory concentration is what’s important for effectiveness
Works best at 4x above the MIC for 50% of the time
Tobramycin
Aminoglycoside antibiotic
Binds 30S ribosome to stop initiation of protein synthesis
Trimethoprim
Inhibits folate synthesis.
It’s a dihydrofolate analog that competitively inhibits dihydrofolate reductase.
Often used in combo with sulfamethoxazole (TMP/SMX)
Vancomycin
Bactericidal antibiotic
Binds free D-ala-D-ala of pentapeptide to inhibit cross-linking and elongation of PG chains.
Works on gramp positives only.
First line for C. diff.
Amphotericin B
Effective broad spectrum antifungal for most serious systemic mycoses.
Gold standard for effectiveness.
Binds ergosterol to cause membrane instability. Can be used topically.
Caspofungin
Inhibits fungal cell wall synthesis by non-competitively blocking synthesis of B(1,3)-D-glucan
Treats invasive aspergillus and esophageal and systemic candida.
Ciclopirox
Used to treat fungal nail infections topically
Clarithromycin (what can it treat in AIDs pts)?
Antimycobacterial used in multi-drug treatment of M. avium intracellulare in AIDs pts
Clofazimine
Binds DNA and interferes with reproduction and growth; can cause red-brown skin/sclera
Antimycobacterial used in combination therapy
Clotrimazole
Mechanism similar to fluconazole (inhibits 14a-sterol demethylase, a fungal p450 that converts lanosterol to ergosterol)
Can be given as oral troches, in creams for vaginal infections, or topically for dermatophyte s
Dapsone
Antimycobacterial
Analog of para-aminobenzoic acid (PABA) that inhibits folic acid synthesis
Static drug used in combination with other drugs for prophylaxis and treatment of pneumocystis jiroveci in AIDs pts.
Ethambutol
1st line TB (tuberculostatic)
Interferes with arabinosyl transferase, thereby blocking cell wall synthesis.
Fluconazole
Inhibits 14a-sterol demethylase, a fungal p450 that converts lanosterol to ergosterol
Treats cryptococcus, candida infections in the CNS and urinary tract, most C. albicans, some C. glabrata, but NOT C. krusei.
Flucytosine (5-FC)
Fungi have cytosine deaminase that converts 5-FC to 5-FU and metabolites of 5-FU block nucleic acid synthesis.
Treats candida and cryptococcus infections.
Used with amphotericin B.
Griseofulvin
Oral antifungal that interferes with microtubule function, mitotic spindles, and mitosis.
Treats stubborn dermatophytic infections of the hair, skin, and nails, including tinea capitis.
Isoniazid
1st line TB
Cidal drug for actively growing cells.
Activated by KatG protein and inhibits mycolic acid synthesis by targeting enoyl-acyl carrier protein reductase (InhA protein).
Itraconazole
inhibits 14a-sterol demethylase, a fungal p450 that converts lanosterol to ergosterol.
Treats blastomyces, histoplasma, and candida: more C. albicans than glabrata, but not CNS or urinary.
Do not give to pts taking drugs with CYP3A4 metabolism.
Miconazole
Same mechanism as fluconazole
Topical cream or suppositories for vaginal candida.
Natamycin
Similar mechanism to amphotericin B
Used for ophthalmic fungal infections, especially fusarium, cephalosporium, and aspergillus.
Nystatin
Mechanism like amphotericin B
Works on azole resistant strains
Topically for candida or oral for GI candida (but causes GI distress)
Pyrazinamide
Cidal drug, 1st line for TB
Blocks mycolic acid synthesis by inhibiting fatty acid synthase 1
Good for CNS involvement
Rifabutin
Prophylaxis for M. avium celllulare (MAC) in AIDs pts
Alternate to rifampin for multi-drug treatment of MAC
Rifampin (what severe infection does this treat)?
1st line drug for TB
Streptomycin
1st line for TB
Binds several ribosome sites to stop initiation and cause misreading
Reserved for most severe TB
Terbinafine
Topical antifungal for dermatophytes or oral for 12 wk therapy for nail infections
Causes squalene to accumulate, causing lipid droplets that disrupt fungal cell membranes
Tolnaftate
Topical treatment for dermatophyte fungal infection
Voriconazole
Inhibits 14a-sterol demethylase, a fungal p450 that converts lanosterol to ergosterol
Treats aspergillus, candida glabrata and krusei but NOT urinary.
Albendazole
Treats echinococcos, cutaneous larval migrans, and neurocysticercosis.
Well distributed,
Causes increased hepatic enzymes, headache, nausea, vomiting, and abdominal pain.
Atovaquone
Selectively inhibits malarial mitochondrial electron transport (cytochrome bc1) and thereby disrupts pyrimidine synthesis.
Treats toxoplasma gondii
Atovaquone + proguanil
Proguanil is a prodrug that inhibits malarial dihydrofolate reductase to block folate synthesis.
Atovaquone selectively inhibits malarial mitochondrial electron transport (cytochrome bc1).
Both drugs disrupt pyrimidine synthesis.
Chloroquine
Blood schizonticide
Parasitized RBCs concentrate drug >25 fold by a pH dependent mechanism into acidic vacuoles.
It inhibits heme polymerization, causing heme to accumulate at toxic levels.
Doxycycline (antimalarial)
Treats multi-drug resistant P. falciparum and can be used for prophylaxis for chloroquine resistant P. falciparum
Idodoquinol
Luminal amebicide
Used alone for asymptomatic infection or with a tissue amebicide for symptomatic infections.
Contraindication in those hypersensitive to iodine.
Mebendazole
Treats many intestinal roundworms and some ova.
Poorly absorbed, which means there low systemic toxicity.
Mefloquine
Similar MOA to chloroquine; Blood schizonticide
Can be used for prophylaxis in chloroquine-resistant areas; treats chloroquine-resistant P. falciparum and P. vivax.
Black box warning for psych effects.
Metronidazole (amebicide)
Cidal tissue amebicide for symptomatic entamoeba infections.
Nitazoxanide
Inhibits pyruvate: ferredoxin oxidoreductase and disrupts anaerobic energy metabolism.
Treats giardia lamblia and cryptosporidium parvum
Paromomycin sulfate
3rd choice for tapeworm infections, for those that don’t tolerate praziquantel or albendazole
Luminal amebicide used alone for asymptomatic infection or with tissue amebicide for symptomatic infection.
Praziquantel
Treats trematodes (flukes)
Drug of choice for schistosoma; some activity on other flukes; treats many cestodes including taenia solium (And its eggs).
Causes abdominal discomfort and nausea.
Primaquine
Kills liver hypnozoites
Cure/terminal prophylaxis of P. vivax and ovale (in combo with blood schizonticide).
Used with clindamycin for pneumocystic jiroveci in AIDs pts.
Pyrantel pamoate
Treats hookworm, pinworm, and roundworm but NOT whipworm (trichuris).
Poorly absorbed; mild GI symptoms
Quinine
MOA like chloroquine
Blood schizonticide for all four malarial parasites; for acute attacks
Treats chloroquine resistant P. falciparum
Thiabendazole
Treats strongyloides and cutaneous larval migrans from disseminated dog or cat hookworm.
Rapidly absorbed; causes nausea, vomiting, and dizziness.
Abacavir
Nucleoside analog, triphosphate form inhibits reverse transcriptase and causes DNA chain termination.
Treats HIV
Hypersensitivity rxn can occur with HLA-B* 5701 allele
Acyclovir
Phosphorylated form is made 40-100x faster in infected cells by herpes thymidine kinase.
Inhibits herpes DNA Pol 10-30x better than host DNA Pol
Competes with deoxy-GTP for DNA polymerase.
What are the three ways that acyclovir can be given and what does each treat?
IV: severe genital herpes, systemic HSV, HSV encephalitis, and disseminated neonatal HSV
Oral: Genital herpes, herpetic gingivostomatitis
Topical: Genital herpes
Amantadine
Prophylaxis and treatment for influenza A (NOT B); Blocks viral uncoating by interfering with influenza A M2 protein (an ion channel)
Best when given within 48 hrs of symptom onset
Can cause CNS effects
Efavirenz
1 anti-HIV drug in 2005
Non-nucleoside inhibitor of reverse transcriptase that binds different sites than NRTI’s and disrupts RT active site.
Can cause rash and psych effects
Emtricitabine
Analog of lamivudine with same MOA.
Treats HIV and some HepB
Enfuvirtide
Binds gp41 subunit of HIV glycoprotein to block membrane fusion to CD4+ cells
Treats HIV-1 only, and only used for pts who failed other regimens.
Bad side effects: severe injection site rxn, diarrhea, nausea, fatigue
Famciclovir
Prodrug activated to penciclovir-triP
Inhibits viral DNA pol
Treats acute herpes zoster(shingles), and recurrent genital herpes
Foscarnet
Inhibits cytomegalovirus DNA pol by binding to its pyrophosphate binding site.
Does not need to be converted to a triphosphate form to be active
Treats CMV retinitis and acyclovir-resistant herpes simplex
Ganciclovir
Cytomegalovirus prophylaxis and treatment
Same MOA as acyclovir except the mono-phosphorylated by CMV protein kinase.
Treats CMV retinitis and is used in transplant prophylaxis
Interferon-alpha
Treats condyloma accuminata (genital warts), HepB, and HepB (in combo with other drugs).
Pegylation decreases clearance which is beneficial for treatment.
Not used long term due to side effects: flu-like, BM suppression, neurotoxicity, and myalgia.
Lamivudine (3TC)
Nucleoside analog activated to tri-P form
Competitively inhibits RT of hepatitis B virus polymerase, causing chain termination
Treats HepB, HIV, and AZT-resistant HIV strains
Synergistic with AZT (zidovudine) for HIV.
Ledipasvir
Inhibits NS5A phosphorylation
Given with sofosbuvir for HSV types 1, 4, 5, and 6
Avoid use with p-glycoprotein inducers
Lopinavir
Prevents viral aspartic protease from cleaving Gag-pol polypeptide into functional viral proteins, resulting in non-infectious viral particles.
Protease inhibitor; Treats HIV
Causes redistribution of fat, diabetes, and is a potent CYP3A inhibitor
Maraviroc
Antagonist of chemokine co-receptor CCR5 (only HIV drug that targets human protein)
Treats CCR5-tropic HIV strains and strains that are resistant to other drugs
CCRV-tropic infections typically predominate early in the infection.
Oseltamivir
Prodrug, competitively inhibits influenza neuraminidases and interferes with viral release and penetration.
Prophylaxis and treatment of influenza A and B
Give within 48 hours of symptom onset
Palivizumab
Humanized monoclonal Ab that binds to fusion protein of RSV to prevent fusion to host cells.
Prevents severe RSV in high risk peds patients.
Penciclovir
MOA like acyclovir
Treats recurrent herpes of lips and faec (topical)
Raltegravir
Inhibits HIV-1 integrase, preventing integration of HIV-1 FNA into host genome.
Common 1st line drug
Treats HIV-1 and strains that are resistant to other drugs.
Ribavirin
Monophosphate form inhibits inosine-5’-phosphate dehydrogenase and thus GMP/GTP synthesis
Triphosphate form inhibits GTP-dependent capping of viral mRNA
Both forms interfere with viral mRNA syntehsis
Aerosol used for severe RSV, oral for HepC (in combo with PEG-IFN-alpha)
Ritonavir
Used to BOOST levels of other protease inhibitors by blocking their metabolism by CYP3A
Avoid using with other drugs that are metabolized by CYP3A
Simeprevir
Reversibly inhibits hepC NS3/NS4A protease and blocks cleavage of polyprotein and thus formation of infectious virus.
Treats HepC genotype 1
Metabolized by CYP3A
Sofosbuvir
Prodrug nucleoside analog; in triphosphate form it inhibits HIV NS5B RNA pol causing chain termination.
Treats all Hep C genotypes
Avoid taking P-glycoprotein inducers with this
Tenofovir
Monophosphate prodrug converted to Tri-P form and competitively inhibits RT domain of hepatitis B virus polymerase, causing chain termination
Treats HepB and HIV
Trifluridine
Thymidine analog that interferes with DNA synthesis
Ophthalmic use; treats HSV 1 and HSV2
Zidovudine (AZT)
Nucleoside reverse transcriptase inhibitor
Triphosphate form competitively inhibits reverse transcriptase and acts as a chain terminator
Anti-HIV drug that can treat 3TC resistant strains. Avoid use with glucuronyltransferase inhibitors (as they can increase the hematologic toxicity)
