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84 Cards in this Set
- Front
- Back
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Bioavailability of PCn ranges from 30-75%, how is PCN absoprtioed
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RAPIDLY absorbed-- peak serum in 30-60min
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How are PCN usually administered
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ON empty stomch, becuased acid labile, affect both rate and extend of absorption
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PCN GERNALLY are well distributed into, and what is metabolism
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tissues and lfuids
MIXED renal and hepatic metabolism |
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Generally what is half-life of PCN
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VERY SHORT
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What is absorption of Penicillin G and why
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LOW b/c ACID labilbe 15-30%
ONLY PARENTERALLY |
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Penicllin V is a SEMI-Syntheiss pencillin but more STABLE TO ACID-how is it adminsitered
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ORALLY--
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Orginall PCN have broad spectum of activity NOW ONLY useful against
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Gram + aerobes (Strepococcus, enterococcus, Listeria)
Gram - aerobes--ONLY neisseria meningitides ANAERobes (+/- expect for Bacteroides fragilis) |
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What are Penicllinase-Resistance PCN
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Oxacillin (IV)
Cloxacillin (PO) Dixloxcillin (PO) Nafcillin (IV0 |
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Penicilinase Resistance Pencillins were specfically desgined to overcome resistacne to
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B-lactamases in S. aureus
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The oral absoprtion varies among Pencillinase-Resistance PCN,
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Oxacillin 30-40%
Cloxacillin 50% Dicloxacillin 30-40 MOST COMMON Nafcillin <20% |
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What is half-life of Pencilinase Resistance PCN
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short half time 0.5-1.0hrs
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Metabolism of Methicilin was primary renally, which was why discontinued due to
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nephotoxicity
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What is metabolism of Ox/Clox/Diclox
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mixed renal and hepatic
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What is metabolism of Nafcillin
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primarly hepatically--
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What type of bacteria are Penicllinase Resistance Penicillins effective aginast
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Gram + aerobes
MSSA |
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Pencillinase reistannt PCN, has less activty then PCN G against
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Steoptoccci
and NO activity agasinst enterococci |
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What are the 2 types of Aminopenillcin
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Ampicllin (PO IV)
Amoxicilin (PO) |
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What type of bacteria are Penicllinase Resistance Penicillins effective aginast
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Gram + aerobes
MSSA |
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What were aminopencillins designed to improve
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Gram- activity of natural PCN by adding a amino group
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Pencillinase reistannt PCN, has less activty then PCN G against
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Steoptoccci
and NO activity agasinst enterococci |
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Are aminopenilclin B-lactasmase resistance
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NO
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What are the 2 types of Aminopenillcin
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Ampicllin (PO IV)
Amoxicilin (PO) |
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Aminopencilins have improved oral absoprtion due to increase acid stability, which is best one
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amoxxicillin 75-90%
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What were aminopencillins designed to improve
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Gram- activity of natural PCN by adding a amino group
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How is Aminopenicllin metabolism
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RENALLY
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Are aminopenilclin B-lactasmase resistance
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NO
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Aminopencillin have GOOD acitivty agginst NON-b lactamase organisms
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YES
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Aminopencilins have improved oral absoprtion due to increase acid stability, which is best one
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amoxxicillin 75-90%
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What is spectum of activity of aminopencillins
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Gram+ aerobes similar to PCN G, but better against Enterocooci
Gram- aerobes (KEP , and Haemophlius influnze Anaerobes (+- expect bacteriodes fragolies |
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The extended-spectrum PCN are
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Caroxypenicllins
Ureidopenilclins |
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What is an example of a Carboxypencillin
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Ticarcillin
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What is an example of Ureidopencillin
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mezoliccilin, or piperacillin
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What was the reason for extended spectum penicllin
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improve gram-neatvie actions
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Are the extended spectum pencillins B-lactamase resistance
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NO
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How are extended spectrum pencilins absorbed
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POOR--only pareneteral
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What is elimination of Extneded Spectrum pencillins
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MIXED
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What is the Etended spectrum Spectrum of activity
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Gram + aerobes--strep/enterococci (less than PCN G)
Gram - aerobes--Energic bacilli and PSEDUMONAS aeugrinosea and H. influenze Anaerobes--limited activity simlar to PCN G |
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What are the MORE activty Extended Spetrum Pencillins
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UrediopCN
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PCN have relatively LOW toxicity, and are generally well tolerated in what type of doses
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LOW-moderate doses
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What are the MAIN SE of PCN
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GI
SKIN CNS Hematolgic Hepatic Renal Electroyltes |
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What are the GI sides effect of PCN
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N/V, diarrhea
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GI sides of PCN are due due its poor absroption, what PCN has highest rate of diarrhea
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ampicillin
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Skin rash is most commonly reported with what PCN
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Ampicillin and amoxicllin
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Does a rash with ampicillin mean a hypersenstiivgty reaction
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sometime--becareful
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PCN can also cause hematolgoic effect, such as neutropenia, throbmocyotpenia or prolonged bleeding time with what
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BIG doses---like Pipercillin (IV
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Also PCN do NOT really cross CNS, what are SEs with high doses
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mental status chnages, and seizures
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What are the heaptic effects of PCN
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elevation of transaminases
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Whatare SEs of PCN renally
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intersitial nehpritis, and acute tubular necrossis
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Anaphylactic reations are rare! Half of all allegic drug reaction occur in who
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hospitalized pts receiving high dose parenteral
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Hypersenstivity reactions result from immune system sensization to
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breakdown productions----penicilloyl derivations, that combine with cellular moleucles to form haptens
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Hapten funcution as
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antigens and iniate antibody production
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When does a Type I hypersenstivity reaction occur
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IMMEIDATE
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Type I hypersenstivity--can lead to anaphylaxis which is mediated by
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IgE antibitoides
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Type I hypersenstivyte occur within 2-20minutes, and signs/symptoms include
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urticaria, broconspasma cardiovasclar collapse
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Tpye II hypersenstive reactions are mediated by
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IgG and IgM
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IgG adn IgM antibodies are directed in Type II reactions towards
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cell surface--RBC---or pCN haptens
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What are sign/symtpos of Type II reactions
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hemolytic anemia, luekpenia, thromboyctpenia, and nehpritis
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Type III hypersensitvity reactions to PCN are NOT commonly seen, and occur when
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1-3 weeks are threapy
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Type III hypersenstivity is associated wiwth
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IgG
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Type III hypersenstivity signs/symptoms
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SERUM sickness--rash fever, arthralgia, hymphadeonpaty
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Type IV hypersenstivity is DELAYED involve
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lymphocytes and amcrophages
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What are signs/symptoms of type IV
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pruituts, maculopapular rashes, phtosenstivity, dermattis
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If a invidials has a + Coombs test---it is assoicated with what hypersenstivity
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Type II
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Skin testing is possible in pts with allaegy to PCN, NOT usally performed in clincial seeting risk of what
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Type I reaction
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PCN cross react 100% with other PCN, what is cross reactivity with Cephalosprins or Carapenems
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7-10%
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Cephalosprings and Carabpenems what is risk of cross reactivity with PCN
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7-10%
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What is cross-reactivity of PCN, Cephalospoirns or Carbapenems with Aztreoman
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0%
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Axtreoman other cross reacts with
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Axteoman--100%
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What is % of cross reactivity between Cephalosporins and Carbapenems
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100%
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What are 2 reactions aaociated with Broad-stemum antibotics and B-lactams
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C. difficule
Superinfection |
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What are the 2 MAIN drug interactions with PCN
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Aminoglycosides and Probenecid
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What is reaction between PCN and aminoglycoside
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chemical inactivtion of PCN when mixed in SAME bad with aminoglycosides
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What is reaction between PCN and Probenecid
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INhibition of renal tubular secretion and increase conc and 1/2 life of PCN
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Do B lactamase inhibitor have antimicrobial activity
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NO
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What do B-lactamase inhibitors MOA
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IRREVERSIBLE inbhit B lactamses via acylation of the enzyme
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Are all B-lactamases inhibtited by these agents
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NO
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B-lactamse inhibtiors are MOST effectve against what
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pencillinases and B-balctamses produced by ANAEROBIC organism
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B-lactamse inhibtior has variable activity against B-lactamses produced by what type of bacteria
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Gram- aerobic bacilli
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What are the 4 B-lactamse inhibtior combinations
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Amoxillin/clavulanate
Ticarcilin/cluavulante Ampicllin/sulbactam (IV) Pipercllin/tazobactam |
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All B-lactamse inhibtiors improve activity against
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S. aureus and ANAEROBES
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Amoxcillin/clavulanta have imporved activity against
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S. aureus, Gram - aerobes and anerboes
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Ticarcillin/clavulante has improved activity against
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S. aurerus, Gram - bacilli, Pseudomonas, and anerobes
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Pipercillin/tazobactam (Zosyn) has improved activity against
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S. sures, Gram - aerobes (Pesdumonas and EXCELLENT ANAERBOCIS
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What B-lactam/B lactamse inhibtior combination have best overall activyt than ANY other PCN class
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Piperaccilin/tazobactam
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