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    PenicillinBy : abdelmnaem elgelia

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    Classification:

    Cell wall synthesis inhibitorsBeta-lactams (penicillins, cephalosporins,

    aztreonam, imipenem)Poly-peptides (bacitracin, vancomycin) Protein synthesis inhibitorsAminoglycosidesTetracyclinsMacrolidesChloramphenicol

    Clindamycin Folate antagonistsSulfonamidesTrimethoprim Quinolones

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    BACTERIAL CELL WALL

    Gram-negative (e.g. E.coli, Salmonella)Few peptidoglycan

    layers(Lipopolysaccheride)

    Gram-positive (e.g. Staphylococci,Listeria)

    Many peptidoglycan layers(Lipoteichoicacid)

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    Resistance to PenicillinsResistance to Penicillins

    1)Production of -lactamases

    2)

    3)The occurrence of modified penicillin-

    binding sites4)

    5)Decreased permeability to the drug

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    Narrow spectrum penicillinase sensitive

    Narrow spectrum penicillinase resistant

    Broad spectrum penicillins

    Extended-spectrum penicillins

    PenicillinsPenicillins

    classificationclassification

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    Narrow spectrum penicillinase (=Narrow spectrum penicillinase (= --

    lactamase) sensitivelactamase) sensitive

    Benzylpenicillin

    Naturally occuring

    Poor oral availability (sensitive to stomach

    acid)

    given by injection

    Active against gram-positive bacteria

    Phenoxymethylpenicillin

    Better oral availability (acid resistant)

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    Narrow spectrum penicillinase (=Narrow spectrum penicillinase (=

    -- lactamase) resistantlactamase) resistant

    Methicillin

    Semisynthetic

    Poor oral availability (only parenteral)

    Active against gram-pos bacteria

    Mostly used for Staphylococcus aureus

    Oxacillin

    Good oral availability

    Cloxacillin

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    Broad spectrum penicillinase (=Broad spectrum penicillinase (= --

    lactamase) sensitive(= Aminopenicillins)lactamase) sensitive(= Aminopenicillins)

    Ampicillin

    Semisynthetic

    Good oral availability

    Active against gram-pos and gram-neg

    bacteria

    Active against enterobacteria

    Amoxicillin

    Excellent oral availability

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    Extended spectrum penicillinase (= -Extended spectrum penicillinase (= -

    lactamase) sensitivelactamase) sensitive (=(=

    Carboxypenicillins)Carboxypenicillins) Carbenicillin

    Semisynthetic

    Poor oral availability Active against gram-pos and gram-neg bacteria

    Active against Pseudomonas aeruginosa,

    Klebsiella

    Ticarcillin

    Mezlocillin

    Pipercillin

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    PHARMACOKINETIC:

    bsorbtion orallyDistrubutionBBBPlacentaenal execretion

    etabolizetion

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    Therapeutic useTherapeutic use

    Treatment of:Treatment of:+r a m o c c i _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ S t a p h, >>>>t r e p t o a b c e s sr a m _ o c c i _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ n i s s e r i a>>>> e n i n g i t i s+r a m a c i l l i _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ a n t h r a x, ,e t a n u s g a s g a n g r e n e>>>>p i r o c h e t e s s y p h i l i s>>>>c t i n o m y c e s e a c t i n o m y c o s i sr a m ,a c i l l i _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ U T I. ,P y l o r i t y p h o i d f e v e r

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    impairment ofplatelet aggregation.

    irritative responses to penicillin at site

    of injection

    phlebitis or thrombophlebitis

    nausea, with or without vomiting

    Intrathecal injection of penicillin G

    may produce arachnoiditis

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    PROBENECID

    Probenecid is an oral drug used for reducingblood uric acid levels in patients with

    hyperuricemia (high uric acid)

    Probenecid prevents attacks of gout by

    reducing uric acid levels in the blood.

    It does this by preventing the reabsorption of

    uric acid by the kidney and increasing its

    excretion from the body in the urine.

    Probenecid also blocks excretion by thekidney of penicillin and related antibiotics

    and is used for increasing the levels of the

    antibiotics in the blood and increasing

    their effectiveness when treating

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    PRESCRIBED FOR:PRESCRIBED FOR:

    Probenecid is used for the treatment

    ofhyperuricemia associated with

    gout. It also is used for increasing

    blood levels of penicillin-type

    antibiotics (for example, ampicillin

    and amoxicillin).

    http://www.medicinenet.com/script/main/art.asp?articlekey=693http://www.medicinenet.com/script/main/art.asp?articlekey=692http://www.medicinenet.com/script/main/art.asp?articlekey=692http://www.medicinenet.com/script/main/art.asp?articlekey=693
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    SIDE EFFECTS:

    Common side effects of probenecid include

    headache, dizziness, nausea, vomiting, skin

    rash, sore gums, and fever.

    Probenecid may cause a flare of gout and

    kidney stones, and it is not started during an

    acute attack of gout.Serious but rare side effects include reduced

    red blood cell counts (anemia), liver damage

    and severe allergic reactions.

    http://www.medicinenet.com/script/main/art.asp?articlekey=20628http://www.medicinenet.com/script/main/art.asp?articlekey=97800http://www.medicinenet.com/script/main/art.asp?articlekey=24732http://www.medicinenet.com/script/main/art.asp?articlekey=1992http://www.medicinenet.com/script/main/art.asp?articlekey=361http://www.medicinenet.com/script/main/art.asp?articlekey=2015http://www.medicinenet.com/script/main/art.asp?articlekey=2015http://www.medicinenet.com/script/main/art.asp?articlekey=361http://www.medicinenet.com/script/main/art.asp?articlekey=1992http://www.medicinenet.com/script/main/art.asp?articlekey=24732http://www.medicinenet.com/script/main/art.asp?articlekey=97800http://www.medicinenet.com/script/main/art.asp?articlekey=20628