antibiotics mod 2 Flashcards
Beta-Lactamase inhibitor combinations
Ampicillin-sulbactam
Amoxicillin-clavulanic acid (Augmentin)
Ticarcillin-clavulanic acid (Timentin)
Piperacillin-tazobactam (Zosyn)
Ceftazidime-avibactam (Avycaz)
penicillin
MOA:
- Disrupt the synthesis of the cell wall
- Bacteria must be growing and dividing
- Inhibit transpeptidases
- —Essential for cell wall synthesis
- Activates autolysis
Works against many different organisms
Low toxicity
Adverse effects: urticaria, pruritis, angioedema
penicillin: uses and SE/AE
Different Types of PCNS
Natural Penicillins:
- PCN G & PCN V
Penicillinase-Resistant Penicillins:
- nafcillin
Aminopenicillins:
- amoxicillin & ampicillin
Extended-Spectrum Penicillins:
- Piperacillin
Natural pcns:
penicillin g& V
Indications: Gram +, gram – cocci, anaerobic bacteria, spirochetes
Can be used with aminoglycosides
- gets into the cell and disrupts protein synthesis
½ life about 30 minutes (unless kidney dysfunction)
Least toxic
SE:
Rash to anaphylaxis allergy to 1 PCN, allergy to ALL
Usually given IV/IM (PO forms available)
Penicillanse resistant PCNs:
nafcillin (iv)
Nafcillin is the drug of choice for this class of PCNs
Nafcillin is IV only
Cloxacillin & oxacillin are the oral formulations
Resist breakdown by the penicillanse enzyme
Aminopenicillins:
ampicillin (Augmentin) & amoxicillin
ampicillin (Augmentin)
- 1st broad spectrum
AE: Diarrhea and rash
Given PO or IV
If oral, amoxicillin usually better option
Renal sensitive
ampicillin/sulbactam (Unasyn)
amoxicillin
- Indications: Common for ear, nose, throat, genitourinary and skin infections
- Less SE compared to ampicillin
- Very common in pediatric patients
- Doses are sometimes higher because of strep resistant organisms
- ONLY PO
Extended-spectrum:
piperacillin (Zosyn)
liver and renal function monitor
Wider spectrum than other penicillins
Both ticarcillin & piperacillin ALWAYS given with a beta-lactamase inhibitor
Anti-pseudomonal
Ticarcillin unique side effect: sodium overload & interferes with platelet function
Piperacillin very good for pseudomonas infection
Also affects platelet function
Watch for patients with renal dysfunction
Cephalosporins
1-5 generations
bacterial infections, bacterial cell wall
NO ETOH
Structurally similar to PCNs
Inhibit cell wall synthesis through same penicillin-binding protein - activate autolysis
Often resistant to beta-lactamase - cephalosprinase
Low-toxicity
Some cross-sensitivity with PCN allergy
Avoid if PCN anaphylaxis
5 generations:
Increase the spectrum/activity/and ability to penetrate CSF
Cephalosporins
Most common adverse effects of all: mild diarrhea, abdominal cramps, rash, pruritis, redness, edema
ok for pregnancy
same indications as PCN
1st generation cephalosporin:
cefazolin & cephalexin (Keflex)
Works well for gram + bacteria
Staph and non-enterococcal strep infections
Given PO or IV
Cefazolin is only IV
Cefazolin common for surgical prophylaxis
**no BBB crossing
2nd generation: cephalosporin
cefuroxime& cefotetan
More gram – coverage AND the gram + coverage
IV and PO forms available
Cefuroxime does not kill anerobic bacteria
No BBB or pseudomonas
3rd generation: cephalosporins
ceftriaxone
ceftazidime
Cefotaxine
NO LIVER
Most potent in fighting gram – bacteria BUT much less activity against gram +
These 2 drugs are IV/IM only
Ceftriaxone is EXTREMELY long-acting (once per day dosing benefit)
BBB - effective in treating meningitis and other infections within the CNS
NO LIVER FAILURE
Ceftazidime works well for pseudomonas
4th generation: cephalosporin
cefepime
Works against gram - & + (very broad spectrum)
Uncomplicated/complicated UTIs, skin infections and pneumonia
Also crosses the BBB
5th generation: cephalosporins
ceftaroline
Treats MRSA and MSSA works again some VRSA/VISA
***No Enterobacter, Pseudomonas, ESBL, Klebsiella coverage
Needs to be renally dosed
Only IV form
Ceftolozane/tazobactam (Zerbaxa) NEWEST cephalosporin
Treats complicated infections
Carbapenems
imipenem/cilastin (Primaxin)
meropenem
**potential seizure activity infused over 60 mins
BROADEST spectrum of ALL antibiotics
Bactericidal & cell wall inhibitor (same as previous two classes)
Typically used as a ‘last resort’ medication
Biggest AE: drug-induced seizure activity (not super common)
ALL are IV and must be INFUSED OVER 60 MINUTES
carbapenems
Imipenem/cilastin (primaxin)
what for seizures
Combo of the carbapenem with an inhibitor of enzyme that breaks down imipenem
MOST broad spectrum
Binds to penicillin-binding proteins
VERY RESISTANT TO BETA-LACTAMASE
IV administration only
Can penetrate BBB and meninges
WATCH FOR SEIZURES especially in elderly and with other meds that can induce seizures
Used for complicated infections
carbapenems:
meropenem
A little less coverage than imipenem; but still gram + and – aerobes and anaerobes
Doesn’t degrade in kidneys
Less seizure activity
Rash and diarrhea most common side effects
Ertapenem- less spectrum; but only have to give once a day
Doripenem- newest; less seizure activity; NOT FOR PNEUMONIA
carbapenems
imipenem/cilastin (Primaxin)
meropenem
Imipenem/cilastin (primaxin)
Meropenem
Vancomycin
gram + ; no BBB; kidney dosing
Glycopeptide antibiotic
Destroys by binding to bacterial cell wall, producing immediate inhibition of cell wall synthesis and death
Works on gram + infections - including MRSA and PCN resistant pneumococcus
Oral vancomycin is given to treat clostridium difficile and pseudomembranous colitis
Doesn’t work for CNS infections
Kidneys eliminate drug; decrease doses for renal dysfunction
Vancomycin
red man syndrome
the red man drives the van, listening to music too loudly (ototoxicity) and not drinking enough water (kidney damage)
Toxic side effects:
Ototoxicity with high levels (can be reversible)
Immune-mediated thrombocytopenia
Nephrotoxic watch when using with other drugs (aminoglycosides, cyclosporin’s, IV contrast) that affect kidneys
Watch with neuromuscular blockades (paralyzers)
Red Man Syndrome: usually related to rapid infusion
Flushing, rash, pruritis, urticaria, tachycardia, hypotension
Infuse slowly and over longer time periods
Usually NOT harmful
Monobactam:
aztreonam (Azactam)
Most commonly used for gram – bacteria
Still uses the penicillin binding protein; inhibits cell wall synthesis and cell lysis
Can work for CNS infections- crosses the BBB
Side effects: thrombophlebitis/pain at injection site
Televancin(Vibativ)
gram +
Inhibits cell wall sysnthesis
IV only: usually for skin infections r/t gram + bacteria (works for MRSA)
Adverse effects: renal toxicity, infusion-related reactions, prolonged QT interval
Dalbavancin & oritavancin are newest and are derivatives of televancin (REALLY long half lives)
TEICOPLANIN
Semisynthetic glycopeptide
MOA: Inhibits peptidoglycan polymerization, results in inhibition of cell wall synthesis and cell death
Can be give PO to treat C Diff and pseudomembranous colitis
LONG half-life
Treats gram-positive bacterial infections like MRSA and Enterococcus [similar to Vanc]
Aminoglycosides Lincosamides: clindamycin Macrolides Oxazolindinones Streptogramins Tetracyclines Glycylcycline Fluoroquinolones Cycliclipopeptides Sulfonamides Metronidazole
All of these Drugs Work by Inhibiting/Altering Protein Synthesis: transcription - Nucleus - Messenger RNA - Cytoplasm
translation
- Cytoplasm
- Ribosomes
- mRNA
- Add amino acids
- —-In a specific sequence
- Protein synthesis
Aminoglycosides:
gentamycin
amikacin
tobramycin
gram - and + with combo therapy
Potent antibiotics that work well on gram (–) bacteria
Also work on gram + but need other anti-biotics for synergistic effect
UTIs/pyelonephritis, gynecological infections, peritonitis, endocarditis, PNA, osteomyelitis (DM related infections)
Severe side effect profile:
Nephrotoxicity- 5-25%, usually reversible
Ototoxicity- 3-14%, usually permanent
Therapeutic drug monitoring - peak/trough levels
Transitioned from 3x/day dosing to 1x/day dosing
Aminoglycosides:
gentamycin
** respiratory distress, cochlear damage
Neuromuscular blockade - can cause PROFOUND respiratory distress [myasthenia gravis]
Central nervous system side effects: confusion, depression, disorientation, numbness, and tingling
Cochlear damage– ototoxicity, high-frequency hearing loss, high-pitched tinnitus
Aminoglycosides uses and indications
gentamycin:
IV; intrathecal for meningitis
Also available in ophthalmic drops, and topical ointments
amikacin:
Only IV
Used for infections resistant to tobramycin and gentamycin
tobramycin:
Inhalation for pulmonary infections (esp. CF patients)
Topical and ophthalmic solutions available
Lincosamides:
clindamycin
Bactericidal or bacteriostatic– depending on drug concentration
**anaerobic infections – will develop c-diff and pseudomembranous colitis from usage
MOA: binds to ribosomes and inhibits protein synthesis
Indications: chronic bone infections, GU tract infections, intraabdominal infections, anaerobic pneumonia, septicemia, serious skin infections; prophylaxis for endocarditis
PO & IV available
Primarily used to treat: pseudomembranous colitis
Monitor use with neuromuscular blockade medications
Very toxic- monitor levels - peaks and troughs
Macrolides
erythromycin
azithromycin
Legionnaire’s, Listeria, mycoplasma pneumonia can all be treated with macrolides
Bacteriostatic in general, bactericidal in high enough concentrations
YUCK drugs - GI side effect profile intense (esp. erythromycin)
MOA: inhibit protein synthesis by binding to ribosomes
Indications: various infections of upper and lower respiratory infections, skin infections, soft tissue infections; STIs
macrolides
erythromycin
GI issues; no BBB
Used to treat MANY infections
Has hypomotility benefits for diabetic gastroparesis & increase gastric motility and emptying
Does not cross BBB
PO & IV– IV is painful, oral absorption isn’t great
Topical and ophthalmic also available
Don’t take oral on empty stomach– lots of GI upset
Lots of drug-drug interactions
Macrolides:
azithromycin (Z-pack)
no with food, decr absorption
Differs structurally from other macrolides - has some advantages in coverage compared to erythromycin
Less GI upset, still some
Very good tissue penetration & long duration of action
Taking food with drug decreases absorption, so try to take without food
Oxazolidinones
linezolid
Indicated for healthcare-associated pneumonias and infections
MOA: inhibits protein synthesis through non-selective monoamine oxidase (MAO) inhibitors
Initially created to treat MRSA and VRE
Use with caution: Hypertension Untreated thyroid disease Severe cardiac disease Cerebrovascular disease Pheochromocytoma
Oxazolidinones
linezolid
side effects **serotonin
Common adverse effects: headache, nausea, vomiting
Watch platelet count thrombocytopenia
Available PO and IV
Can cause serotonin syndrome with use of SSRIs
Avoid foods high in tyramine: wines, smoked meats, aged cheese, soy sauce
Streptogramins
quinupristin/dafopristin
**pot. anaphylaxic shock, need D5W with IV infusion
Newest class for ‘superbugs’ quinupristin/dalfopristin used in combination alone bacteriostatic, combination=bactericidal 16x the activity used alone
Use for serious, life-threatening infections caused by VRE and complicated skin and skin structures, including MRSA
IV only
Adverse effects: arthralgias, myalgias (muscle pains); painful/erythema/inflammation at IV site in 75%
Tetracyclines
tetracycline
doxycycline
minocycline
Broad spectrum; major resistance has developed
Contraindications: Pregnant and nursing women, children younger than 8 (teeth)
MOA: bacteriostatic drugs that inhibit protein synthesis by binding to ribosomes
Some infections still commonly treated with tetracyclines: Rickettsia (rocky mountain spotted fever) Chlamydia and trichomonas Lyme disease Cholera Pelvic inflammatory disease Mycoplasma pneumonia Acne
Adverse effects: discoloration of the permanent teeth and tooth enamel hypoplasia in fetuses and children, photosensitivity, many others
tetracycline
Concentrates in bone, liver, tumor, spleen & TEETH
Causes damage to teeth < 8 years
Bacteriostatic Inhibits or retards the growth Not available parenterally Fasting – 75% - 77% absorbed Giving more decreases % absorption
Adverse effects: N/V/D, headache, photosensitivity, dizziness
Rare: anaphylaxis and angioedema
tetracyclines
doxycycline
minocycline
acne primary use
doxycycline
Chlamydial and mycoplasmal infections
Prophylaxis for STIs
Acne and other non-dangerous skin infections
minocycline
Neisseria meningitides
Decreases symptoms of rheumatoid arthritis
Solodyn is an extended release (ER) formula - acne
tetracycline
Glycylcyline: tigecycline
**skin infection
Newest form of tetracyclines
Effective against many organisms resistant to the other tetracyclines
Treats complicated skin and skin structure infections- MRSA, VRE, extended-spectrum beta lactamases
Peritonitis and other complicated abdominal infections
Nausea and vomiting occur in 20-30% of patients
Fluoroquinolones
ciprofloxacin, levofloxacin
***GREAT ORAL ABSORPTION
gram -
Very potent, broad-spectrum antibiotics
Very good oral absorption
1st & 2nd generations not used anymore due to abx resistance
MOA: destroy bacteria by altering their DNA
Interfere with the bacterial enzymes DNA gyrase and topoisomerase
Mostly gram-negative and some gram-positive coverage
Fluroquinolone:
ciprofloxacin
**anthrax, UTI primary,
causes joint disease
Used to treat UTIs, some STIs, upper and lower respiratory tract infections, gonorrhea, and other infections
Also treats anthrax infection with Bacillus anthracis
PO, IV, and topical
Works well on rapid and slow growing organisms
Prolonged post-antibiotic effects concentrated in the neutrophils
Adverse effects: arthropathy (joint disease), often irreversible
Avoid in patients under 18 and over 60
Fluroquinolone:
levofloxacin (Levaquin)
100% bioavailable; respiratory infections,
**give no seizure or kidney failure
Most widely used quinolones
Broad-spectrum of activity like cipro but advantages is once-daily dosing
PO or IV- 100% bioavailability orally
Less resistance
More activity against pneumococcal and other ‘atypical’ respiratory infections
Side effects: CNS disorders that predispose to seizures, kidney failure, can cause prolongation of QT interval, photosensitivity
Cyclic Lipopeptides:
daptomycin
MOA: Not completely understood; binds to gram + cells in calcium-dependent process, disrupts the cell membrane potential
Long post-antibiotic effect
Given IV once per day
Used to treat: MRSA, VRE bacteremia, right-sided endocarditis, complicated skin & skin structure infections
Sulfonamides:
sulfamethoxale + trimethoprim
MOA: don’t actually destroy bacteria but inhibit their growth= bacteriostatic by preventing the synthesis of folic acid needed for DNA synthesis
Indications: uncomplicated UTIs, respiratory infections, salmonella, shigellosis
‘Sulfa allergies’; photosensivity
metronidazole (Flagyl)
NO ETOH, crohn’s disease and c-diff
Antiprotozoal & antibacterial
Crohn’s disease
Antibiotic-associated diarrhea
Anaerobic activity only
MOA: inhibits DNA synthesis, similar to fluroquinolones
DO NOT TAKE WITH ALCOHOL
Adverse effects: N/V, xerostomia, vaginal candidiasis
inhibit cell wall growth
penicillins cephalosporins carbapenems vancomycin aztreonam telavancin
abx classes
class
abx moa
gram coverage
inhibit/alter protein synthesis
aminoglycosides lincosamides macrolides oxazolindinones streptogramins tetracyclines glycylcycline flouroquinolones cycliclipopeptides sulfonamides metronidazole
inhibit cell wall synthesis
penicillin cephalosporins carbapenems vancomycin Monobactam - aztreonam telavancin Teicoplanin
peak
taken 30 minute after medication infusion is complete
trough
taken 8-12 hrs after dose is complete
