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Antibiotics/Antivirals
N/A
24
Pharmacology
Undergraduate 4
11/21/2016

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Cards

Term
penicillin
Definition
MOA - Bactericidal; Inhibit bacterial cell wall synthesis; Bind to penicillin binding proteins (renally eliminated)
Indications - Gram + bacteria; Syphilis (neurosyphilis); Group B Strep
AE -
CNS- Seizure risk, lethargy, depression
GI- N/V/D, Oral candidiasis
Hematologic- Anemia, Bone Marrow Depression, Granulocytopenia
Allergic Reactions (0.4-7% receiving PCN have reaction)DRUG DRUG INTERACTIONS
Probenecid- can delay renal excretion of pencillin
Aminoglycosides- Synergistic- extra bactericidal effects
Book mentions to avoid mixing together in same solution
GUT FLORA
Warfarin- reduced vitamin K in gut
Oral Contraceptives- theoretically decrease absorption
***Safest of all antibiotics; pregnancy category B; require dose adjustments in renal dysfunction
Term
nafcillin
Definition
penicillinase-resistant penicillins
MOA - Bactericidal; Inhibit bacterial cell wall synthesis; Bind to penicillin binding proteins; Modified structure to resist Penicillinase
Indications - only for penicillinase producing Staphylococci; Staph. aureus (MSSA) and Staph. epidermidis; Cellulitis, SSTI, endocarditis
AE - Same as penicillin
Drug/Drug - Same as penicillin
Term
ampicillin/amoxicillin
Definition
aminopenicillins
MOA - Bactericidal; Inhibit bacterial cell wall synthesis; Bind to penicillin binding proteins; Modified structure to add some Gram - Coverage (renally eliminated)
Indications - Upper Respiratory Infections (Sinusitis, Acute Otitis Media), Lyme Disease, Meningitis* (children and geriatric), dental prophlyaxis; same coverage as natural penicillins, but have added coverage for gram negative
HELPS KILL ENTEROCOCCUS (enterococcus faecalis)
H. influenzae
E. coli
Listeria
Proteus mirabilis
Salmonella
AE - ampicillin has highest rate of N/V of penicillins; amoxicillin is associated with rash in peds (10%), but usually not serious
Term
piperacillin
Definition
extended spectrum penicillin
MOA - Bactericidal; Inhibit bacterial cell wall synthesis; Bind to penicillin binding proteins (renally eliminated)
Indications - Similar to aminopenicillins coverage PLUS Pseudomonas aeruginosa, Klebsiella and anaerobes (Bacteroides fragilis); susceptible to beta-lactamases, give with a beta-lactamase inhibitor (which gives it anaerobic coverage); Pneumonia (PNA), Intra-abdominal surgery/wounds, animal bites
AE - Same as penicllin
Drug/Drug - Same as penicillin
Term
tazobactam (piperacillin/tazobactam = Zosyn)
Definition
beta-lactamase inhibitor
MOA - Bind to and inactivate the beta-lactamase inhibitor enzymes
Indications - Never given alone; Usually combined with a penicillinase resistant penicillin; Target bacteria dependant upon the combined therapy; Great for adding anaerobic coverage; with piperacillin- pseudomonas aeruginosa; with amoxicillin- Does NOT cover pseudomonas aeruginosa
AE - Minimal toxicity, usually due to the PCN component
Term
cephalexin/cefazolin
Definition
1st generation cephalosporins
MOA - Bactericidal; Inhibit bacterial cell wall synthesis; Bind to penicillin binding proteins (renal elimination)
Indications - Gram + bacteria; UTI, surgical prophylaxis, Cellulitis, SSTI
AE - Very similar to penicillins
Most common: diarrhea, abdominal cramps, rash, pruritus, redness,edema; Cross Sensitivity- Statistics vary- anywhere from <1-10%; potential for cross-sensitivity
Drug/Drug - Cefazolin- disulfiram like reaction when combined with EtOH; Probenecid- can delay renal excretion of cephalosporins; GUT FLORA; Warfarin- reduced vitamin K in gut; Oral Contraceptives- theoretically decrease absorption/alter metabolism
Pregnancy category B; adjust dose with renal dysfunction
Term
cefoxitin
Definition
2nd generation cephalosporins
MOA - Bactericidal; Inhibit bacterial cell wall synthesis; Bind to penicillin binding proteins (renal elimination)
Indications - Some Gram +/- bacteria, now have anaerobic coverage; Cefoxitin- surgical prophylaxis, intra-abdominal wounds, bites
AE - Same as 1st gen
Drug/drug - same as 1st gen
Term
ceftriaxone/ceftazidime
Definition
3rd gen cepalosporins
MOA - Bactericidal; Inhibit bacterial cell wall synthesis; Bind to penicillin binding proteins
Pharmacokinetics - Ceftriaxone has excellent CSF penetration; Ceftriaxone- Hepatic Metabolism and elimination (safe in renal!); Ceftriaxone- long half life; All others- renal elimination
Indications - Some Gram +/-
Ceftriaxone- PNA, Meningitis (CSF penetration), UTIs
Ceftazidime- Pseudomonas aeruginosa
AE - Same as 1st; increased risk for bleeding ceftriaxone
Drug/Drug - same as 1st; Ceftriaxone and calcium can bind (TPN,Lactated Ringers)
Term
cefepime
Definition
4th gen cephalosporins
MOA - Bactericidal; Inhibit bacterial cell wall synthesis; Bind to penicillin binding proteins (renal elimination; CSF penetration)
Indications - Some Gram +/-
Cefepime: Febrile Neutropenia, Meningitis, Hospital Acquired Pneumonia, Pseudomonas aeruginosa
AE - same as 1st
Drug/drug/ - same as 1st
Term
ceftaroline
Definition
5th gen cephalosporins
MOA - Bactericidal; Inhibit bacterial cell wall synthesis; Bind to penicillin binding proteins (renal elimination)
Indications - Some Gram +/-
Ceftaroline: unique- covers MRSA (CAP, SSTI)
AE - same as 1st
Drug/drug - same as 1st
Term
imipenem/cilastatin (Primaxin) OR ertapenem
Definition
carbapenems
MOA - Bactericidal; Inhibit bacterial cell wall synthesis; Bind to penicillin binding proteins
pharmacokinetics - renal elimination; minimal bioavailability, all are IV; CSF penetration; different half lives
Imipenem and Cilastatin
Cilastatin- dipeptidase inhibitor
Dipeptidase is enzyme in the kidneys that was found to breakdown imipenem
Ertapenem
Less bacterial coverage compared to other three
The exclusive carbapenem that does NOT cover Pseudomonas aeruginosa
Indications - Some Gram +/-, anaerobes, Pseudomonas aeruginosa; LOTS!
AE - Same as PCNs, Cephalosporins; Seizure Risk! Big Carbapenem Class effect; Cross sensitivity to beta lactams, <1%
Drug/drug - Same as PCNs, Cephalosporins; Valproate- can reduce valproate levels (seizure risk)
Term
aztreonam
Definition
monobactams
MOA - Bactericidal; Inhibit bacterial cell wall synthesis; Bind to penicillin binding proteins of aerobic gram negative bacteria (does not bind to anaerobic and gram + PBPs) (renal elimination; CSF penetration)
Indications - Aerobic Gram Negative Bacteria; Pseudomonas aeruginosa; Inhaled form for Cystic Fibrosis; Meningitis, UTIs, sepsis
AE - Relatively Safe; Same as other beta-lactams- mostly GI; Cross sensitivity to beta lactams, <1%
Drug/drug - nothing notable
Term
vancomycin
Definition
miscellaneous/glycopeptide
MOA - Bactericidal; Binds to gram positive bacterial cell wall and immediately causes cell death
pharmacokinetics - PO has very minimal if any systemic absorption; eliminated renally; has some CSF penetration- typically requires higher doses
Indications - Gram + only; MRSA (IV only); Clostridium difficile (C.diff) (PO only); pneumonia, meningitis,osteomyelitis, UTIs, sepsis, etc
AE - Nephrotoxicity- monitor SCr/BUN, vanco levels; rarely ototoxicity?; Red Man Syndrome- Histamine release
Drug/drug - MAJOR: other nephrotic drugs; MINIMIAL: other ototoxic drugs
Monitoring - SCr/BUN; Vancomycin trough levels (10-20mcg/mL); Peaks are no longer necessary
Term
Sulfamethoxazole-Trimethoprim (Bactrim®)- IV,PO
Definition
sulfonamides
MOA - Bacteriostatic; inhibit synthesis of tetrahydrofolate, which is required by bacteria to make DNA,RNA and proteins; similar structure to PABA (1:1 - IV-PO)
Indications - UTIs- E.Coli; Respiratory Tract Infections; coverage for CA-MRSA; HIV patients -prophylactic or active treatment of: Pneumocystis jiroveci/carinii Pneumonia (PJP/PCP)
AE - Blood dyscrasias; Kernicterus in newborns - avoid in pregnancy and infants; excessive bilirubin- neurologic damage; Renal crystallization rare- adequate hydration; Hepatoxicity; Hyperkalemia (trimethoprim component); Hypersensitivty Reactions; Photosensitivity; Rash; Stevens-Johnson Syndrome/TEN (rare)
Drug/drug - Potential hyperkalemia drugs
Inhibitor of hepatic metabolism - Warfarin, phenytoin, sulfonylurea diabetic medications
AVOID - pregnancy; infants; breastfeeding
Term
azithromycin/erythromycin
Definition
macrolides
MOA - Bacteriostatic; Inhibit protein synthesis by binding to the 50s ribosomal subunit (extensive hepatic metabolism)
Indications - Broad Gram +/- coverage; Erythyromycin- GI motility!; Mycobacterium Avium Complex (MAC); Prevention and treatment in patients with HIV; Great for URTI, LRTI, Chlamydia, pelvic inflammatory disease, lots more; Mycoplasma pneumoniae (CAP); Clarithromycin- H.pylori (not on exam)
AE - QT prolongation; N/V/D
Drug/drug - Any QT prolonging drugs; CYP3A4 drugs- macrolides function as inhibitors - azithromycin having least inhibition (Causes elevated levels-Warfarin,Phenytoin, Carbamazepine); Oral Contraceptives- decreased effectivenss
Term
clindamycin
Definition
miscellaneous
MOA - Bacteriostatic; Inhibit protein synthesis; Binds to the 50s subunit of bacterial ribosomes (same site as macrolides, but they have different coverage (hepatic and renal elimination)
Indications - Anaerobes as well as gram + bugs (nice for PCN allergy); intra-abdominal infections, bites; certain SSTI CA-MRSA infections, resistance patterns
AE - BOXED WARNING - pseudomembranous colitis; C.diff associated diarrhea (CDAD)
Term
doxycycline/tigecycline
Definition
tetracyclines
MOA - Broad Spectrum; Bacteriostatic; use transport systems to enter bacteria; Bind to the 30s ribosomal subunit, inhibits binding of transfer RNA to messenger RNA-ribosome complex
pharmacokinetics - renal- tetracycline, demeclocycline, tigecycline; hepatic/bile- doxycycline, minocycline
Indications - Tigecycline only- MRSA!; Acne- topical and oral preparations; Lyme Disease; Mycoplasma pneumoniae (CAP); H. pylori (peptic ulcer disease); Rocky Mountain Spotted Fever (Rickettsial diseases); Chlamydia; lots of uses
AE - very irritating to the G.I. tract- rarely causes ulceration
N/V/D, rash
Bind to cations (divalent and trivalent)
Calcium- Bind to developing teeth-Tooth Discoloration, hypoplasia of the enamel
Avoid Calcium products- Milk,yogurt, antacids
Iron, aluminum, magnesium, zinc products
Can suppress bone growth in developing infants, reversible
Hepatotoxicity with larges doses
Renal Impairment (only with the renally eliminated ones)
PHOTOSENSITIVITY- sunburn very easily
Risk for Super Infection/Overgrowth
Antibiotic pseudomembranous colitis
C.diff associated diarrhea (CDAD)
Candida albicans- oral/vaginal candidiasis
Drug/drug - calcium; iron; magnesium; aluminum products; oral contraceptives; warfarin
AVOID - pregnancy; breastfeeding; children < 8
Term
gentamicin/tobramycin
Definition
aminoglycosides
MOA - Bactericidal; Concentration Dependent; Disrupts protein synthesis by binding to 30S ribosomal subunit, believe to inhibit protein synthesis and promote production of abnormal proteins (renal elimination)
Indications - Gram negative only as a monotherapy; Pseudomonas aeruginosa; used in neonates; Gram positive synergy with Abx that weaken bacterial cell wall; Have a post-antibiotic effect; Conventional Dosing vs. Extended Interval
AE - nephro/ototoxity
Term
levofloxacin/ciprofloxacin
Definition
fluoroquinolones
MOA - Bactericidal; Inhibit bacterial DNA gyrase and topoisomerase IV (IV:PO - 1:1)
Indications - Gram +/- coverage; Pseudomonas aeruginosa; Pneumonia; Urinary Tract Infections; Anthrax; Prostatitis; Not all interchangeable- ciprofloxacin (not for respiratory)
AE - BOXED WARNING- Tendon rupture/tendonitis
BOXED WARNING- Peripheral Neuropathy; QT prolongation; Photosensitivity (phototoxicity); Increased risk for C.Diff; Can exacerbate myasthenia gravis; Pregnancy Class C
Drug/drug - Chelation- zinc, iron, magnesium, calcium, aluminum; increased Warfarin levels; increased theophylline levels
Term
metronidazole
Definition
nitrolmidazoles
MOA - Bactericidal; anaerobic bacteria take up metronidazole into cells and activate the drug. The drug then interacts with DNA, causes strand breakage and loss of helical structure (hepatic elimination IV:PO = 1:1)
Indications - anaerobes only; first line therapy for C.diff; combo therapy for H.pylori; lots of uses (think anaerobic)
AE - box Warning- has been shown to be carcinogenic in mice and rats; Disulfiram like reaction with EtOH; peripheral neuropathy; Headache (most common)
Term
acyclovir/valacyclovir
Definition
non-HIV antiviarls - guanine analogs
MOA - Inhibits viral replication by suppressing synthesis of viral DNA
pharmacokinetics - acyclovir has poor oral bioavailability; acyclovir has CSF penetration; Both renally eliminated
Indications - HSV1, HSV2, VZV (chicken-pox and shingles)
Does NOT work for CMV
AE - GI- N/D; Headache, discomfort; Rarely thrombocytopenia; Neurologic toxicity- hallucinations,tremors,delirium; SUPER RARE- Walking Corpse Syndrome "Cotard Delusion"; Nephrotoxicity- crystallization in renal tubules (STAY HYDRATED); Burning at topical site/Phlebitis at injection site
Drug/drug - probenecid; Other nephrotoxic drugs
Pregnancy category B
Term
ganciclovir
Definition
non-HIV antiviral - acylic nucleoside analogs
MOA - Inhibits viral replication by suppressing synthesis of viral DNA (renal elimination)
Indications - CMV retinitis in AIDS patints; prevent CMV infection in high-risk patients undergoing organ transplant
AE -
BOXED WARNING: Blood dyscrasias
Bone Marrow Toxicity- thrombocytopenia and granulocytopenia
BOXED WARNING:
In animal studies ganciclovir was carcinogenic, teratogenic and caused aspermatogenesis
headaches; N/V
Drug/drug - probenecid
Pregnancy - category C; women/men both advised to use contraceptives
Term
amantadine (not much for test)
Definition
non-HIV antivirals - adamantanes
MOA - Not completely known; believed to interfere with the viral M2 protein and prevent viral release of nucleic acid (renal elimination)
Indications - CDC currently doesn't recommend it to be used at all (resistance); If used, only used for Influenza A, NOT B; Parkinsons!
AE - Anticholingeric properties- orthostatic hypotension, blurred vision; CNS depression; Impulse control disorders; Melanoma; rarely: Neuroleptic Malignant Syndrome
Term
olsetamivir
Definition
non-HIV antiviral - neuramanidase inhibitor
MOA - mimic sialic acid, a target of neuraminidase; prevents cleavage of newly formed viral particles from the host cell (renal elimination)
Indications - prophylactic and active treatment of Influenza A and B; effective in H5N1 (avian flu) and H1N1 (swine flu)
AE - GI- N/V- can be given with food; neuropsychiatric effects(especially in children); hallucinations, delirium, suicide; rarely hypersensitivity reactions- SJS/TEN
Drug/drug - probenecid
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