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Index
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ORG MED LEC
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ANTIBACTERIAL.ppt
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Level 4
level: Level 4
Questions and Answers List
level questions: Level 4
Question
Answer
Are those which can be obtained directly from penicillium mold and do not require further modification. Many species of bacteria are now resistant to these penicillins It was made available in the form of water-soluble salt of potassium, sodium and calcium poorly absorbed from the intestinal tract, oral doses must be very large its rapid elimination from the bloodstream led to the development of repository forms.
Natural Penicillin
In the repository forms of penicillin 1 Suspension of penicillin in __ 2 Suspension in __
1 Peanut oil or sesame oil with white beeswax 2 Vegetable oil with Aluminum monostearate or Aluminum distearate
Repository FORMS (IM) of penicillin
1 Penicillin G procaine (Crysticillin, Duracillin, Wycillin) 2 Penicillin G benzathine (Permapen)
When phenoxyacetic acid is introduced to the penicillium culture. Adding oxygen, decreases nucleophilicity of the carbonyl group making it acid stable and orally viable
Penicillin V
Acyl side chain of the penicillin can be cleaved using enzyme or chemical methods to produce 6-APA 75% of penicillin is produced is modified in this manner
Semi-synthetic penicillin
Penicillin with bulky side groups can block the Beta-lactamases which hydrolyze the lactam ring
Penicillinase-resistant penicillin - Antistaphylococcal
Beta lactamases are prevalent in what microorganisms?
S aureus S epidermidis
prototype drug -off the market due to high incidence of nephrotoxicity Interstitial nephritis
(Staphcillin) 2,6-dimethoxyphenylpenicillin
1 Methicillin is acid sensitive and has been improved by adding __ 2 This results to drugs such as
1 Electron withdrawing groups 2 Oxacillin, Nafcillin
can be given to patients with renal problems Stable in acid>orally relatively small amounts are excreted through kidneys, with the major portion excreted in the bile
Nafcillin (2-ethoxy-phenylpenicillin) (Unipen)
Better absorbed than other antistaphs
Isoxazoyl Penicillin
Isoxazoyl Penicillins:
Oxacillin, Cloxacillin, Dicloxacillin
Penicillin modified to have more hydrophilic groups allowing to penetrate gram negative bacteria Wider range of activity than natural or antistaphylococcal drugs but without bulky side groups
Aminopenicillin ex. Ampicillin, Amoxicillin
Aminopenicillin hydrophilic groups make gut wall penetration difficult therefore susceptible to infection by __
H pylori
agent of choice against Haemophilus influenzae infections
Ampicillin, 6-(d-α-aminophenylactemidopenicillanic acid) BN: Omniphen, Amcill, Principen
treatment of choice for gonorrhea
Ampicillin + Probenecid
p-hydroxy analog of ampicillin better GI absorption than ampicillin introduced in 1974,
Amoxicillin 6-[d-(-)-α-amino-para-hydroxyphenylacetamido]penicillanic acid BN: Amoxil