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Beta-Lactam Antibacterials
Penicillins, Cephaloporins & other drugs Chapter 29
36
Pharmacology
Undergraduate 1
03/07/2013

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Term
Beta-lactam Antibacterials
Definition
Several gram negative & gram positive bacteria produce beta-lactam.
They inhibit synthesis of bacterial walls.
Allows contents to leak out destroying the microb.
Term
Penicillin(P)
Definition
Most effective in infection caused by Gram positive bacteria.
skin/soft tissue
Respiratory
Gastrointestinal
GU (Genitourinary infections)syphilis
Usually given IM or IV
Cross allergies to drugs with similar structures
Term
Cross allergenicity(allergies)
Definition
allergy to a drug of another class with similar chemical structures.
Ex; cephalosporins/carbapenems should be avoided w/ pts w life threatening allergic reactions.
Term
Penicillin G (Pfizerpen, Bicillin, Wycillin)

are resistant to what type of strains?

Penicillin V (Veetids)
Definition
1st drug of choice in many infections
staphylococcal & gonococci
treat: pharyngitis, rheumatic fever.
Not effective orally, inactivated by gastic acid.

Route: IV, IM can NOT be used interchangeably.

BBB: inadvertent IV result in cardiopulmonary arrest or death.
Term
What is the drug of choice for streptococcal pharyngitis?
Definition
Penicillin G
Term
Can you give penicillin G orally and why?
Definition
not effective orally because it is inactivated by gastric acid.
Term
Nafcillin is the drug of choice for ____?
Definition
MRSA =Methicillin resistant staphylococcal aureus
Term
Aminopenicillins (Ampicillin) are used for what types of gram stains?
Definition
both positive and negative
Term
Aminopenicillins (Ampicillin) are excreted mainly by kidneys(some in bile) and useful in what type of infections?
Definition
UTI's
Term
Aminopenicillins (Ampicillin) are used to treat what three things?
Definition
bronchitis, sinusitis, otitis media.
Term
Aminopenicillins (Ampicillin)
Definition
-is a broad spectrum semisynthetic for gram +/- bacteria.
-Effective against; enterococci, proteus mirabilis, salmonella, shigella, escherichia coli.
-Resistant to; penicillinase producing staphylococci & gonococci.
-Excreted by kidney (some in bile) but usefull for UTI's.
-Treatment for; bronchitis, sinusitis, otitis media.
Term
Penicillins G* (Pfizerpen, Bicillin, Wycillin)
Definition
-Remains effective for limited use.
-Many strains of staphylococci & gonococci are resistance
-Drug of choice for treatment of streptococcal pharyngitis/prevent recurrent attacks acute rheumatic fever due to group A streptococcus and neurosyphilis.
-Not effective orally, inactivated by gastric acid.
-Route is IV, IM (can NOT be used interchangeably)
-BBB: inadvertent IV result in cardiopulmonary arrest or death
Term
Amoxicillin(P)*(Amoxil, Trimox)
Definition
-Similar to ampicillin
-Except available only ORALLY
-Better absorbed & produce therapeutic blood levels more rapidly than oral ampicillin, causes less GI distress
-TREAT: Endocarditis that produce bacteremia.
Term
Ampicillin-sulbactam (Unasyn)*
Definition
-Combined w/penicillin may be effective in infections caused by bacteria that are resistant to a beta-lactam antibiotic alone.
-Unasyn; combined w ampicillin & sulbactam available in vials with;
-1g ampicillin & 1.5g sulbactam
-2g ampicillin & 1g sulbactam
Term
Piperacillin-tazobactam (Zosyn)
Definition
-Combined with piperacillin and tazobactam in an IV formulation
-3 dosage strengths;
-2g, 3g,4g of piperacillin to
-0.25g,0.375g, 0.5g tazobactam (match up)
Term
What are the Contranindications for use for Penicillins (P)?
Definition
Hypersensitivity or allergic reaction
Cross allergies(allergy to a drug of another class w/ similar chemcal structure)
Admin of cephalosporins/carbapenems should be avoided with life threating allergic reactions to penicillins.
Anaphylaxis, laryngeal swelling, angioedema or hives.
Term
Penicillin V
Definition
Derived from Penicillin G. It is not destroyed by gastric acid and given only by oral route.
Well absorbed & produces therapeutic blood levels.
Term
Cephalosporins
Definition
-Broad spectrum, cousin to pencillin, made from fungus.
-May be used alone for treatment of infections.
Activity against both gram +/- bacteria
-Drugs used fro pre-op surgery, prosthetic implants.
-URI & UTI
Skin/soft tissue
Brain, septicemia, brain & spinal cord.
Similar to PCN(watch for allergy)
Excreted thru kidneys.
Term
What are the indications for use in Cephalosporins?
Definition
-1st & 2nd Gen; Used for surgical prophylaxis, prosthetic implants
-2nd Gen; Used for surgical prophylaxis; gynecologic & colorectal surgery also treatment of intra-abdominal infections, pelvic inflammatory disease, diverticulitis, wounds of abdomen.
-respiratory tract
-skin/soft tissue
- bones, joints
-UTI
-brain, spinal cord
-bloodstream (septicemia)
Term
What are the contraindications for Cephalosporins?
Definition
o anaphylactic reaction/skin rash/drug fever, eosinophilia
o cephalosporin allergy
o bronchospasm
o urticarial
Term
What are the Pt. teaching guidelines for Cephalosporins?
Definition
o Report; skin rash, hives, itching, diarrhea, do not take if allergy
o Complete full course of antibiotics, try not to miss a dose, take at regular times ATC
o Take on empty stomach 1hr before or 2 hours after
Term
What is the name of the 1st Generation of Oral Cephalosporin?
Definition
Cephalexin (Keflex)
Term
Oral CEPHALOSPORINS/ 1st Gen
Cephalexin (Keflex)
Definition
First oral cephalosporin; still used extensively.
Term
What is the name of the 2nd Generation of Oral Cephalosporin?
Definition
Cefuroxime (Ceftin)
Term
What is the name of the 3rd Generation of Oral Cephalosporin?
Definition
Cefdinir (Omnicef)
Term
Oral CEPHALOSPORINS/ 2nd Gen
Cefdinir (Omnicef)
Definition
o Indicated for bronchitis, pharyngitis, otitis media caused by streptococci or H. influenza
Term
Oral CEPHALOSPORINS/ 3rd Gen
Cefuroxime (Ceftin)
Definition
o Can also be give parenterally
o Tablet can be crushed & added to a food(applesause) but leaves a strong bitter persistent aftertaste.
o Exception; reach therapeutic levels in CSF
o Excretion; undergoes dual elimination via the biliary tract & kidneys
Term
What is the name of the two 2nd Generation of Parenteral Cephalosporin?
Definition
Cefotaxime (Claforan) & Ceftriaxone (Rocephin)
Term
PARENTERAL CEPHALOSPORINS/ 2nd Gen
Cefotaxime (Claforan)
Definition
o Antibacterial avtivity against most gram +/- bacteria, including several strains resistant to other antibiotics
o Recommended for serious infections caused by susceptible microorganisms
o Metabolized in the liver to an active metabolite desacetylcefotaxime, which is eliminated by the kidneys.
Term
PARENTERAL CEPHALOSPORINS/ 2nd Gen
Ceftriaxone (Rocephin)
Definition
o First 3rd generation cephalosporin approved for once daily dosing.
o Antibacterial activity against most gram +/- bacteria, including several strains resistant to other antibiotics.
Term
What is the name of the four 4th Generation of Parenteral Cephalosporin?
Definition
Cfepime (Maxipime)
Carbapenems
Meropenem (Merrem)
Monobactam
Term
PARENTERAL CEPHALOSPORINS/ 4th Gen
Cefepime (Maxipime)
Definition
o Indicated for UTI caused by Escherichia coli or Klebsiella pneumoniae;
o skin/soft tissue infections caused by susceptible streptococci, staphylococci; pneumonia caused by Streptococcus pneumoniae or P. aeruginosa; complicated intraabdominal infection and empiric therapy of fevrile, neutropenic clients.
o Dosage must be reduced with renal impairment
Term
PARENTERAL CEPHALOSPORINS/4th Gen
Carbapenems
Definition
o Broad spectrum, bactericidal, beta-lactam antimicrobials
o Inhibits cell wall synthesis by binding w/penicillin binding proteins.
Term
PARENTERAL CEPHALOSPORINS/ 4th Gen
Meropenem (Merrem)
Definition
o Used as a single drug for empiric therapy.
o Used for intra abdominal infections and bacterial meningitis.
o Adverse effects; cross sensitivity w/ hypersensitivity, CNS toxicity/seizures
o IM injections; use lidocaine local anesthetic for decreased pain.
o Contraindications; pts. Allergic to local anesthetic/severe shock/ heart block.
Term
PARENTERAL CEPHALOSPORINS/ 4th Gen
Monobactam
Definition
o Active against many strains that are resistant to multiple antibiotics
o UTI
o Skin
o Lower respiratory tract
o Abdominal
o Gynecological
Term
PARENTERAL CEPHALOSPORINS/ 4th Gen
Monobactam
Definition
-Active against many strains that are resistant to multiple antibiotics.
-UTI
-Skin
-Lower respiratory tract
-Abdominal
-Gynecological
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