Antibiotics * Flashcards
Penicillin *
Drugs- amoxicillin (amoxil), ampicillin, dicloxacillin, nafcillin, oxacillin, penicillin G (pfizerpen), pencilling G benzathine (bicillin L-A), pencillin G benzathine and pencilin G procaine (bicillin C-R), penicillin V
MOA- cell wall inhibitor, interferes with the last step of bacteria wall synthesis, we can sell wall of cell death, bacterialcidal
Spectrum- Good for gram-positive bacteria, more difficult for grab negative as they have an extra polysaccharide cell wall, see other slide
Admin- IV, IM, PO
ADE- hypersensitivity, Diarrhea, nephritis, neurotoxicity, hematologic toxicity usually with high doses
Cephalosporins*
Drugs- cefaclor, cefadroxil, cefazolin (ancef, kefzol), cefdinir (omnicef), cefepime (maxipime), cefiderocol (fetroja), cefixime (suprax), cefotetan (cefotan), cefoxutin (mefoxin), cefpodoxime (vantin), cefotaximine (claforan), cefprozil (cefzil), ceftaroline (fortaz), ceftriaxone, cefuroxime (ceftin, zinacef), cephalexin (keflex)
MOA-disrupt cell wall synthesis
First generation- act as a penicillin G substitute,
5 generations-see other slides
ADE- generally well tolerated, anaphylaxis, Steve Johnson syndrome, toxic epidermal necrolysis, use with caution and individuals with penicillin allergies
Carbapenems *
Drugs- doripenem (doribax), ertapenem (invanz), imipenem/cilastatin (primaxin), meropenem (merrem)
Synthetic
MOA- cell wall inhibitor
Spectrum- empiric, beta lactamase producing gram positive and negative, anaerobes, pseudomonas, entrapenem lacks pseudomonas, enterococcus and acinetibacter
Pharm- IV
ADE- n/v/d, seizures (imipenem high dose), use caution With PCN allergy
Monobactams *
Drug- azetreonam (azactam)
MOA-cell wall inhibitor
Against gram negative like enterobacteria and pseudomonas, lacks activity against gram positive and anaerobes
IV/IM
Use in caution with renal failure
ADE-phlebitis, skin rash, abnormal LFT
Safe alternative for those with PCN allergy, cephalosporins and carbapenems
Cephalosporin + beta lactamase inhibitor *
Drug- ceftolazone + tazobactan (zerbaxa)
-3rd generation cephalosporins
Ceftazimide + avibactam (avycaz)
Spectrum- resistant enterobacterales, MDR pseudomonas, some ESBLs, narrow gram + and anaerobes, good for intra abdominal infection, complicated UTI, MDR
Vancomycin*
MOA- cell wall inhibitor
Spectrum- active against aerobic and anaerobic gram positive bacteria like MRSA, MRSE, enterococcus, c.diff
Uses- skin and soft tissue infections infective endocarditis nosocomial pneumonia
Dose- dependent on renal function monitoring of creatinine clearance is required with the use of trough as well
ADE- nephro toxicity, and infusion related reactions like Redman syndrome, phlebitis, and ototoxicity
Resistance is now a problem with strep and staph and enterococcus
Lipoglycopeptides *
Drugs- dalbavancin (dalvance), oritavancin (orbactiv), telavancin (vibativ)
MOA- cell wall inhibitor
Spectrum- active against gram positive bacteria. Similar to vancomycin, affects strep, staph and enterococci
Telavancin is an alternative for vancomycin for the treatment of acute bacterial skin and skin structure infections hospital acquired pneumonia caused by resistant gram positive bacteria like MRSA
ADE- includes nephrotoxicity fetal harm interactions with medication at prolong QT, monitor, renal function, pregnancy status, and current medication’s before using
For oritavancin and dalbavancin have a long half life alone for single-dose Ivy administration for bacterial skin and skin structure infections, stable. Patient can be used as outpatient
Oritavancin and telavancin are known to interfere with phospholipid regents that are used in assessing coagulation. Alternative therapy should be considered with concurrent use of heparin.
Daptomycin *
MOA- cell wall inhibitor
Indicated as an alternative for other agents, such as vancomycin or linezolid
Spectrum- gram + organisms, MRSA, VRE
Uses-complicated skin, and skin structure infections and caused by staph aureus and infective endocarditis on the right side
DO NOT USE TO TREAT PNEUMONIA
Fosfomycin (monurol) *
MOA- cell wall inhibitor
Uses- UTIs caused by E. coli or e. faecalis, first line therapy for acute cystitis
One time dose
ADE-diarrhea, vaginitis, nausea and headache
Polymyxins*
Drugs- polymyxin B and colistin (polymyxin E)
MOA- cell wall inhibitor with Detergent like affect
Spectrum- gram negative bacteria
Active against pseudomonas, E. coli, klebisella, enterbacteria, acinetobacter
Dosage- B can be given IV optic Otic and topical, Colistin is a pro drug, can we get an IV or via nebulizer
ADE- Limited due to increase risk of nephrotoxicity and neurotoxicity when systemically- in the setting of gram negative resistance they may be used a salvage therapy for patient with multi drug resistant infections and limited alternative therapeutic options
Tetracycline *
Drugs- demeclocycline (declomycin), doxycycline (doryx, vibrmycin), eravacycline (xerava), minocycline (minocin), omadacycline (nuzyra), tetracycline
MOA- protein synthesis inhibitor
Spectrum- effective against a wide variety of organisms, including gram positive and negative bacteria, spirocytes, mycobacteria, atypical species
Uses- chlamydia infections and acne
Resistance can happen but nontransferable to others in this group
Tetracycline and omadacyline should not be administered with dairy products
ADE-gastric discomfort, effects on calcified tissues, can deposit on the bone and teeth, causing discoloration, hepatotoxicity, phototoxicity, benign intra cranial hypertension
Contraindications -should not be used in those pregnant or breast-feeding or in children less than eight years of age
Glycyclines *
Drugs- tigecycline (tygacil)
MOA- derivative of minocycline, protein synthesis inhibitor
Uses- treatment of complicated skin and soft tissue infections, complicated intra-abdominal infections and community acquired pneumonia. MRSA, VRE, acinetobacter, anaerobic organisms, gram - organisms
IV infusion, poor option for bloodstream infections
ADE- nausea, vomiting, pancreatitis, fatality, elevation, and liver enzymes and creatinine all mortality and and patience treated with this drug is higher than other agents, similar to Tetracycline
BLACK BOX WARNING- the drug should be reserved for use in situations when alternative units are not suitable
D-D- may decrease clearance of warfarin monitor INR levels closely
Aminoglycosides *
Drugs- Amikacin, gentamycin, neomycin, plazomicin (zemdri), streptomycin, tobramycin (tobi, tobrex)
MOA- protein synthesis inhibitor, bacteriacidal
Spectrum- effective from majority of aerobic gram negative bacilli, including those drug resistant, such as pseudomonas, klebsiella, enterobacter, often combined with beta lactate antibiotics for a synergistic effect especially for enterococcus bacteria in endocarditis
Resistance is known
ADE-ototoxicity, nephrotoxicity, neuromuscular blockade, allergic reaction, such as contact dermatitis
Macrolides *
Drugs- azithromycin (Zithromax), clarithromycin (biaxin), erthyromycin (EES, ery-tab)
MOA- protein synthesis inhibitor, bacteriostatic
Spectrum- erythromycin is effective against many as the same organism as penicillin G good alternative for those with a penicillin allergy, clarithryomycin has activities similar to erythromycin, but is also effective against HI, chlamydia, legionella, h pylori, mycobacterium, moraxella, ureaplasma, azithromycin is less effective than erythromycin against strep and staph, azithromycin is more active against respiratory pathogens such as HI and moraxella
Resistance for azithromycin against strep pneumonia
Does not crossover to CSF
ADE- gastric distress and motility, can even lead to ileus, or gastroparesis, jaundice, oto toxicity, prolong QT
Patient with hepatic dysfunction should be treated cautiously with erythromycin and azithromycin
D-D- erythromycin and clarithyromycin inhibit the hepatic metabolism of a number of drugs, which can lead to toxicity, both agents are inhibitors of CYP3A4, it interferes with statins, alprazolam, alfuzosin
Fidaxomicin *
Similar to the macrolides
MOA- inhibit protein synthesis
Spectrum- very narrow limited to gram positive aerobes and anaerobes, good for c. Diff stays in GI tract
ADE- nausea, vomiting, abdominal pain, anemia, and neutropenia are rare, be cautious in those with macrolide allergy
Clindamycin (cleocin) *
Similar to macrolides
MOA- protein synthesis inhibitor
Spectrum- gram positive organisms including MRSA, strep and anaerobic bacteria
Resistance mechanisms are the same same erythromycin, c. Diff resistance
Available an IV oral topical or vaginal formulations use of oral is limited due to G.I. issues
It does not cross into the CSF not useful for UTIs
Accumulation has been reported in patient with either severe renal impairment or liver failure
ADE-skin rash, diarrhea, pseudomembranous colitis due to c. Diff
Oxazilidinones *
Drugs- linezolid (zyvox), tedizolid (sivextro)
MOA- protein synthesis inhibitor
Spectrum- gram positive organisms, including those with resistant, including MRSA, VRE, penicillin resistant strep, corynebacterium, listeria, mycobacterium
Linezolid is alternative for daptomycin for VRE
These agents are not recommended as first line agents for MRSA
ADE- gastrointestinal issues- n/v/d, headache, and rash, thrombocytopenia, usually reported for those who take it longer than 10 days, can lead to serotonin syndrome taken with large quantities of mean containing foods SSRI or MAOIs, peripheral neuropathy optic neuritis, causing blindness, has been associated with greater than 28 days use
Limited utility for extended duration treatments
Lefamulin (Xenleta) *
MOA-protein synthesis inhibitor
Uses- approved for a treatment for community acquired pneumonia
Spectrum- staph aureus, strep pyogenes, s pneumoniae, mycoplasma, HI
Resistance is known
Is available in both IV and oral concentrations
D-D-Primary metabolize by CYP3A4 So drugs are strongly, induce, or inhibit this enzyme or contraindicated
ADE-G.I. issues
Not be used in pregnancy
Chloramphenicol *
MOA-protein synthesis inhibitor
at high circulating chloramphenicol concentration producing bone marrow toxicity oral formulation was removed by the US market due to this
Spectrum- restricted to life threatening infections in which there is no alternative- active against many organisms, including chlamydia, rickettsiae, spirochetes, anaerobes
ADE- anemia, including hemolytic or aplastic, bone marrow toxicity, gray baby syndrome
D-D- another CYP3A4 metabolite interacts with alprazolam, warfarin, phenytoin and may potentiate their effects
Do not give in breast feeding
Quinupristin/dalfopristin (synercid) *
MOA- protein synthesis inhibitor
Spectrum- active against gram positive cocci, resistance, primary treatment is those with enterococcus faecium (VRE)
Resistance is known
Does not achieve therapeutic concentrations in CSF
ADE- significant, that’s why it’s usually reserved for severe infections of VRE, venous irritation when administered through a peripheral line, hyperbilirubinemia, arthralgia and myalgia
D-D-CYP3A4 metabolism
Fluroquinolones *
Drugs- ciprofloxacin (cipro 2nd gen), delafloxacin (baxdela, 4th gen), gemifloxacin (factive, 4th gen), levofloxacin (3rd gen), moxifloxacin (avelox, moxeza, vigamox, 4th gen), ofloxacin
MOA-interferes with DNA ligation, increases the number of permanent chromosomal breaks triggering cell lysis
Four generations spectrum coverage
1st- narrow, aerobic gram negative bacilli, enterobacteriaceae
2nd- better, enterobacteriaceae, pseudomonas, HI, neiserria, chlamydia, legionella
3rd- above plus strep, MSSA, mycobacterium, stenotrophomonas
4th- enhanced gram positive, staph, strep, MRSA, enterococcus
ADE-n/v, dizzy, HA, hepatotoxicity, prolong QT, phototoxic
BLACK BOX WARNING FOR TENDINITIS, TENDON RUPTURE, PERIPHERAL NEUROPATHY, CNS EFFECTS
Limit use in peds
D-D- CYP3A4, CYP1A2, alprazolam, tizanidine; warfarin; ropirinole; duloxetine; caffeine; sildenafil; zolpidem
Sulfonamides *
Drugs- mafenide (sulfamylon), silver sulfadiazine (silvadene, SSD, thermazene), sulfadiazide, sulfasalazine (azulfidine)
MOA-inhibit genesis of bacteria dihydrofolic acid, bacteria status
Spectrum -gram negative and positive including ecoli, klebsiella, enterobacter, HI, strep, staph, toxoplasmosis
Crosses BBB/placenta
Known resistance, if organisms are resistance to one member of this drug family, they are resistant to all
ADE- crystalluria, hypersensitivity, hemolytic anemia, thrombocytopenia, kernicterus
D-D- warfare methotrexate, phenytoin
Contraindications -avoiding newborns and infants, less than two months as well as in pregnant woman at term
Inhibitors of folate reduction *
Drugs- pyrimethamine (daraprim), trimethoprim
MOA- inhibitor of bacterial dihydrofolate inhibition of this enzyme, prevent formation of metabolically, active forms of folic acid and interferes with normal bacterial self function
Spectrum - similar to the sulfas, maybe be used alone in the treatment of UTIs and bacterial prostatitis
Known resistance to gram negative bacteria
ADE- folic acid deficiency, which can cause anemia leukopenia, especially in those pregnant, potassium sparing affects using caution with those already taking spironolactone or any ace inhibitors
Combination of inhibitors of folate synthesis and reduction*
Drug-cotrimocazole (trimethoprim + sulfamethoxazole)(bactrim, septra)
MOA- synergistic effect results in inhibition of two sequential steps in the synthesis of tetrahydrofolic acid
Spectrum -more effective as combination can get PCJ, listeria, salmonella, toxoplasmosis, MRSA, UTI, URI
Resistance is known but less common
ADE- same as a standalone drugs, but most common or nausea, vomiting, skin rash, hematologic, toxicity, and hyperkalemia
Urinary track antiseptics*
Drugs-methenamine (hiprex, urex),
MOA- methenamine salts are hydrolyzed to ammonia and formaldehyde in acidic urine which denatures proteins, resulting in bacterial death
Spectrum - methanamine is mainly used for chronic suppressive therapy to reduce frequency of UTIs active against E. coli, enterococcus, staph, some gram negative coverage like pseudomonas or proteus but urine has to be kept acidic
ADE- gastrointestinal distress, albuminuria hematuria and rash may develop contraindicated in those with renal/hepatic insufficiency
Amphotericin B *
For the treatment of subcutaneous and systemic mycoses, remains drug of choice for the treatment of life threatening mycoses
MOA- binds to ergosterol in the plasma membrane of fungal cells forms, pores that disrupt membrane function, allowing electrolytes to leak from the cell resulting in death
Spectrum - Candida albicans, histoplasma, crypotoccus, coccidiodes, blastomyces, aspergillus, also for leishmaniasis’s
Pharm- can be given IV extensively bound of plasma protein
ADE- very toxic drug has a low therapeutic index and can cause fever and chills, renal impairment shock like hypotension thrombophlebitis
