Antibacterials Flashcards
Gram- Antibacterials
B-Lactams:
*Aztreonam
Other Cell Wall inhibitors:
*Isoniazid (Cell Wall Synthesis Inhibitor)
Protein Synthesis Inhibitors:
- Aminoglycosides (Streptomycin, Amikacin)
- Rifampin
Other: *Methenamine (Urinary Tract Antiseptic)
Gram+ Antibacterials
*Linezolid (Protein Synthesis Inhibitor)
*Vancomycin (Cell Wall Formation inhibitor D-ala D-ala)
Some Gram-:
*Extended Penicillins (some Gram-)
Positives and ANaerobic bacteria Antibacterials
B-Lactams:
*Penicillin G (G-rated, so doesn’t get too deep…)
Protein Synthesis Inhibitors:
- Macrolides (Erythromycin)
- Clindamycin
DNA Synthesis Inhibition:
*Metronidazole (Flagyl)
Name the B-Lactams
- Penicillin G
- Extended Penicillin
Monobactams:
*Aztreonam
Carbapenems:
- Ertapenem
- Iminpenem (with Cilastatin)
- Meropenem
Cephalosporins:
- 1st gen: Cefazolin, Cephalexin
- 2nd gen: Cefoxitin, Cefuroxime, CEfaclor
- 3rd gen: Ceftriaxone, Cefixime, Ceftazidime, Cefoperzone
- 4th gen:__
Name the Cephalosporins
1st gen: Cefazolin, Cephalexin
2nd gen: Cefoxitin, Cefuroxime, Cefaclor
3rd gen: CefTRIaxone, Cefixime, Ceftazidime, Cefoperazone
4th gen: ___
Name all the Broad-Spectrum Antibacterial drugs
B-lacs:
- Cephalosporin 3rd gen (Ceftriaxone, Ceixime, Ceftadizime, Cefoperazone)
- Iminpenem (with Cilastatin)
Protein Synthesis Inhibitors:
- Chloramphenicol
- Fluoroquinolones and Quinolones 2nd gen (Norflaxin, Ciproflaxin)
- Tetracyclines (Tetra~, Doxy~, Tige~)
Folic Acid Synthesis Inhibitors:
- Dapsone
- Sulfonamides (Sulfisoxale, Sulfamethoxazole)
- Trimethoprim
Name the Cell Wall Inhibitor Classes and Drugs
B-Lacs:
- Penicillin G and Extended
- Monobactams - Axtreonam
- Carbapenem - Ertepenem, Meropenem, Iminpenem WITH Cilastatin
- Cephalosporins -
- *1st Gen: Cefazolin, Cefalexin
- *2nd Gen: Cefoxitin, Cefuroxime, Cefaclor
- *3rd Gen: CefTRIaxone, Cefixime, Ceftazidime, Cefoperazone
- Other: Ethambutol, Isoniazid, Pyrazinamide, Vancomycin
Name the DNA Synthesis Inhibitors
- Quinolones
- Fluoroquinones
- Metronizadole
- Folic Acid Synthesis inhibitors:
- *Dapsone
- *Sulfanamides
- *Trimethroprim
Name Protein Synthesis Inhibitors
30S Inhibitors:
- Tetracycline (Tetra, Doxy, Tige) (Reversible)
- Aminoglycosides (Streptomycin and Amikacin) (Irreverisible)
50S:
- Macrolides (Azithro, Erythro, and Clarithro)
- Chloramphenicol
- Linezolid
- Daptomycin (Dapsone)
- Clindamycin
- Metronizadole
RNApoly:
- Rifampin
- Rifabutin
Metronizadole
** “NO ETOH WHILE ON METRO OR DURING FIRST TRIMESTER OF PREGNANCY.” **
*DNA and Protein Synth Inh by forming covalent bonds
Metabolized in liver that then has further activity that limits aldehyde dehydrogenase, which metabolizes ETOH.
Metallic taste, reddish-brown urine
SUPERINFECTION possible
Erythromycin
- Macrolide (50S inh)
- Gram+ Rods and Cocci (v. few Gram-)
- Alternate to penicillin allergy
- *INHIBITS p450
- GI intolerance, Liver toxicity at high doses, HEARING LOSS (reversible), Ventricular Tachy with QT lengthening
- Per the gut, stimulates Gut motility and makes things go Ery-THROUGH-YOU
Clarithromycin
- Macrolide (50S inh)
- Similar to Erythro
- MORE HEARING LOSS than erythro
- TERATOGENIC - NOT during PREGNANCY
- INHIBITS p450
Azithro
- Macrolide (50S inh)
- Similar to Clarithro
- Oral, excellent tissue penetration and CNS and long half life, easy to take home!
Clindamycin
- SIMILAR TO MACROLIDE, but NOT A MACROLIDE
- Treat MRSA!!
- Oral, SUPERINFECTION side effect
Linezolid
- For Vanc-resistant
- MOSTLY Gram+
- 23S RNA moiety of 50S subunit to prevent 70S formation
- MYELOSUPPRESSION and Peripheral and Optic Neuropathy from long use
- Mild Inh of Monoamine Oxidase, which makes hard for body to metabolize some nutrients like tyramine (BP rises)
- *DOES NOT INHIBIT p450
Daptomycin
- ONLY FOR VANC-RESISTANT STAPH INFECTIONS
- Forms a pore allowing ions in and cell burst
- IV only
- Muscle weakness
- STOP STATINS and agents with rhabdomyolysis because can be significant muscle breakdown
Tetracyclines
- Tetra, Doxy, Mino, Tige
- Gram+ and Gram-
- usually not first choice, except MINOCYCLINE for acne and Lyme and DOXY for STDs and tick-related vectors
- REVERSIBLE bind to 30S and cannot accept new AAs
- ORAL except Tige
- CHELATES with METALS, so don’t take with food, also like to settle in bones and teeth because of the calcium there
- BILE and URINE excre.
- Mech of resistance: influx/efflux, ribosome change, enzyme metabolism
- SUPERINFECTION is possible bc affects gut 1st, Some heart (vestibular) dysfunction, can cause aciduria
- NOT FOR KIDS or MOMS
Aminoglycosides
- 30S binding IRREVERSIBLE so will KILL, RNApoly cannot start translation, will end early, or will incorporate incorrect AAs
- Streptomycin and Amikacin
- IV, does not penetrate
- Concentration-dependent, will build up
- Gram-, Plague, TB
- *NOT ANAEROBES bc **OXYGEN-DEPENDENT TRANSPORT across inner cell membrane means will only act on bacteria that like O2
- OTOTOXICITY and RENAL impairment (because concentration builds), also vestibular and auditory
- Works with b-lacs
What type of bacteria do Aminoglycosides NOT work well against, and why?
- Anaerobes
* OXYGEN-DEPENDENT TRANSPORT across inner cell membrane means will only act on bacteria that like O2
Chloramphenicol
Gram+/- Aerobic and Anaerobic
- 50S binding to inhibit peptidyltransferase between A and P sites
- Can interfere with mitochondrial Ribosomes
- INHIBITS p450!!!
- MYELOSUPPRESSION - anemia, GREY BABY SYNDROME
Drugs that cause Myelosuppression
Chloramphenicol
Linezolid
Benzimidazoles
Dapsone
- Folic Acid Metabolism Inh
- PABA analog
- Inhibits Dihydropteroate Synthase, like the Sulfonamides
- BROAD spectrum, including Anaerobes
Sulfonamides
- Folic Acid Metabolism Inh
- PABA analog
- Inhibits Dihydropteroate Synthase
- UROCRYSTAL FORMATION
Rifampin
- Gram+/-, MYCOBACTERIA, CHLAMYDIA
- Protein Synthesis inhibition
- Beta subunit of RNApoly to inhibit RNA synth
- ACTIVATES p450
Rifambutin
Similar to Rifampin but LESS ACTIVATION OF p450
Isoniazid
- Cell Wall Inhibitor
- MYCOBACTERIA treatment first choice
- Inhibits Mycolic acid synthesis, hence the treatment of mycobacteria
- Oral
- Kidney excre.
- Some immun reactions, liver loxicities with clinical hepatitis
50S DNA Synthesis Inhibitors
- Macrolides (Azithro, Erythro, and Clarithro)
- Chloramphenicol
- Metronizadole
- Linezolid
- Clindamycin
30S DNA Synthesis Inhibitors
- Tetracycline (Tetra, Doxy, Tige) (Reversible)
* Aminoglycosides (Streptomycin and Amikacin) (Irreverisible)
VRE Trio
- Linezolid
- Clindamycin
- Daptomycin (forms pore)
Drugs that act on RNApolymerase
- Rifampin
* Rifabutin
Drugs that act on TB and Mycobacteria
REPuBLIC
- Rifampin
- Ethambutol
- Pyrazinamide
- Bedaquiline
- Levofloxacin
- Isoniazid
- Cycloserine
p450 INDUCERS
p450 must think that something is RIGged against it:
- Rifampin
- Isoniazid (only one CYP that importantly metabolizes Aceteminophen, otherwise inhibits many other CYPs)
- Griseofulvin (antifungal)
p450 INHIBITORS
These put p450 on ICCE-T: *Isoniazid *Ciproflaxin *Clarithromycin *Erythromycin *Trimethoprim+Sulfonamide *Fluconazole *Itraconazole *Metronidazole (*Ritonavir and Cobisistant BOOSTERS for other drugs, and they inhibit p450)
TB drug Cell Wall Formation Inhibitors
EPIC:
- Ethambutol
- Pyrazanimide
- Isoniazid
- Cycloserine
Abx that are dangerous during Pregnancy
Tetra, Amino, Metro, and Chlor: Mamas-to-be like CLARIce can’t have them no more!
The 30S inhibitors, Chloramphenicol, Clarithromycin, and Metronidazole
Special use for Erythromycin
Stimulate gut motility post-surgery
