Antibacterial Antibiotics Flashcards
Lincomycin came from the microorganism called
Streptomyces Lincolensis
Cycloserine came from microorganisms called
Streptomyces orchidaceus
Streptomyces lavendulus
Streptomyces garyphalus
Vancomycin came from the microorganism called
Streptomyces orientalis
Chloramphenicol came from the microorganism called
Streptomyces venezulae
Streptomycin came from the microorganism called
Streptomyces griseus
Neomycin came from the microorganism called
Streptomyces fradiae
Chlortetracycline came from the microorganism called
Streptomyces aureofaciens
Oxytetracycline came from the microorganism called
Streptomyces rimosus
Erythromycin came from the microorganism called
Streptomyces erythreus
Rifampicin came from the microorganism called
Streptomyces mediterranei
Natamycin came from the microorganism called
Streptomyces natalensis
Capreomycin came from the microorganism called
Streptomyces capreolin
Amphotericin B came from the microorganism called
Streptomyces nodosus
Nystatin came from the microorganism called
Streptomyces noursei
Penicillin came from the microorganism called
Penicillium notatum
Penicillinase-resistant pens came from the microorganism called
Penicillium chrysogenium
Cephalosporin came from the microorganism called
Cephalosporium acremonium
Bacitracin came from the microorganism called
Bacillus subtilis
Colistin came from the microorganism called
Bacillus colistinus
Polymixin came from the microorganism called
Bacillus polymyxa
Gentamicin came from the microorganism called
Micromonospora purpurea
equivalent units of 1 mg Pen G Na
1,667 U
equivalent units of 1 mg Pen G
1,530 U
equivalent units of 1 mg Pen Procaine
1,009 U
Beta lactam ring is acid….
sensitive
Benzyl Penicillin
Pen G
Gold standard penicillin
Pen G
Phenoxymethylpenicillin
Pen V
the active component of penicillin
beta lactam
ring present in penicillin
Thiazolidine ring
responsible for the solubility of penicillin
carboxylic acid
responsible for the spectrum of activity of penicillin
acylamino group
Pen G is acid labile/instable unless given with
antacids
Pen G is rapidly eliminated thus _ forms were made - _, _
Pen G is rapidly eliminated thus REPOSITORY forms were made, Pen G Procaine, Pen G Benzathine
Penicillin which has a uniform concentration with blood
Pen V
Differentiate Pen G and Pen V based on its SAR
Pen V has an additional of electron withdrawing electron, oxygen which makes it acid STABLE thus can be given ORALLY. Unlike Pen G which is acid SENSITIVE/LABILE thus given parenterally.
In penicillinase-resistant drugs its SAR is the substitution of BULKIER groups which are
Isoxazolyl
Di-ortho substituted aromatic ring
Naphthyl ring
Which among the group describes methicillin:
a. 2,6-DImethoxyphenylpenicillin
b. 2-ETHOXYL-1-phenylpenicillin
2,6-dimethoxyphenylpenicillin
Nafcillin is 2-ETHOXYL-1-phenylpenicillin
prototype penicillinase resistant drug
methicillin
What group is present in Methicillin
Di-ortho substituted ring
What group is present in Nafcillin
Naphthyl ring
Penicillins with Isoxazolyl ring
Oxacillin
Cloxacillin
Dicloxacillin
Flucoxacillin
Which among the following describes Cloxacillin
a. 5-Methyl-3-phenyl-4-isoxazolylpenicillin
b. 5-Methyl-3-(2-chlorophenyl)-4-isoxazolylpenicillin
c. 5-Methyl-3-(2,6-dichlorophenyl)-4-isoxazolylpenicillin
5-Methyl-3-(2-chlorophenyl)-4-isoxazolylpenicillin
Cloxacillin has only 1 chlorine
Dicloxacillin has 2 chlorine
Which among the following describes Cloxacillin
a. 5-Methyl-3-phenyl-4-isoxazolylpenicillin
b. 5-Methyl-3-(2-chlorophenyl)-4-isoxazolylpenicillin
c. 5-Methyl-3-(2,6-dichlorophenyl)-4-isoxazolylpenicillin
5-Methyl-3-(2-chlorophenyl)-4-isoxazolylpenicillin
Cloxacillin has only 1 chlorine
Dicloxacillin has 2 chlorine
Which among the following describes Oxacillin
a. 5-Methyl-3-phenyl-4-isoxazolylpenicillin
b. 5-Methyl-3-(2-chlorophenyl)-4-isoxazolylpenicillin
c. 5-Methyl-3-(2,6-dichlorophenyl)-4-isoxazolylpenicillin
5-Methyl-3-phenyl-4-isoxazolylpenicillin
Electron withdrawing group present in cloxacillin and dicloxacillin
Chlorine
Electron withdrawing group present in Pen V
Oxygen
Aminopenicillins have antibac spectrum similar to pen g but more effective against
gram negative bacilli
Which among describes ampicillin
a. alpha-amino benzylpenicillin
b. alpha-amino-para-hydroxybenzylpenicillin
alpha-amino benzylpenicillin
Give the 2 aminopenicillins
Ampicillin
Amoxicillin
The only aminopenicillin who can penetrate the GI tract thus given orally
Amoxicillin
Give the IV prodrugs of ampicillin
Hetacillin
Bacampicillin
Cyclacillin
Pivampicillin
Electron withdrawing group present in amoxicillin
Hydroxyl
Amoxicillin is administered orally or parenterally?
orally because of the presence of an electron withdrawing group - hydroxyl
Extended Spectrum Penicillins are also known as
Antipseudomonal
Give the 2 extended spectrum penicillins and examples of it
Carboxypenicillins
-Carbenicillin
-Ticarcillin
Ureidopenicillin
-Mezlocillin
-Piperacillin
prototype of antipseudomonal drugs
carbenicillin (under carboxypenicillin)
are carboxypenicillins, carbenicillin and ticarcillin acid stable?
no, they are administered parenterally
An acylureidopenicillin recommended for serious infections
Mezlocillin
Most potent, generally useful extended-spectrumn
Piperacillin
Piperacillin is acid…
unstable given IV/IM
first widely used amine salt of pen G was made with
Procaine
units/mg of Pen G Benzathine
1,211 units/mg
units/mg of Pen V
1,695 units/mg
prodrug of ampicilillin with no antibacterial activity
Bacampicillin
agent of choice against Haemophilus influenzae infections
Ampicillin
penicillins interfere with the last step of cell wall synthesis which is called
transpeptidation
Route of administration of Pen G
PO, IV, IM
True or False
Pen G is used for RHD and Syphilis
True
What class of penicillins are narrow, broad and extended spectrum?
Narrow - Penicillinase-resistant/Antistaphylococcal
Broad - Aminopenicillins
Extended - Antipseudomonal
most potent anti-pseudomonal penicillin
piperacillin
True or False
Probenecid is also sometimes given together with penicillin antibiotics
True
Type of Beta-Lactamase inhibitors which only:
1. protect the beta-lactam ring
2. prolong duration of action of penicillin
3. extend the spectrum of activity of penicillins
Type I Beta-Lactamase inhibitors
Give the class I beta-lactamase inhibitors
Clavulanic Acid
Sulbactam
Tazobactam
Give the class II beta-lactamase inhibitors
Carbapenems
-Imipenem
Newer carbapenems
-meropenem
-biapenem
Cilastatin
Thienamycin
Monobactam
-aztreonam
1st carbapenem
Imipenem
Impinem and Thienamycin are inactivated by DHP
True
DHP inhibitor
Cilastatin
Monobactam
_ methoxy group was responsible for B-lactamase stability series, contributed to the low antibacterial potency and poor chemical stability
3
are newer carbapenems stable to DHP? name the 2 of them
Meropenem
Biapenem
Nucleus of penicillins
6-APA (6-aminopenicillanic acid)
Nucleus of cephalosporins
7-ACA or 7-APDA
7-aminocephalosporanic acid or 7-aminodeacetoxycephalosporanic acid
Name the ring that is present in cephalosporin
Dihydrothiazine ring
Most reactive site in cephalosporin
Acetoxylmethyl
Addition of dihydrothiazine ring in cephalosporin makes it more or less strained and reactive?
less
if your solvent is _ (acid/base) cephalosporin hydrolyzes with a hydrolytic product of:
acid, 7-ACA or 7-ADCA
If you are allergic to penicillin, then you are also allergic to cephalosporin
True because they both have beta lactam ring
Adverse reaction of Cephalosporin
Allergic and hypersensitivity
Mild rashes
Anaphylaxis
a close congener of Pen N which contains the dihydrothiazine ring
Cephalosporin C