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(1 / 5 )
( antibacterial )
( antifungal)
(anticancer cell )
( cytotoxic)
( antivirus )
(antibacterial)
-lactam antibiotic
Penicillin
Vancomycin
cephalosporin
Bacitracin
carbapenems
monobactoms
MODE OF ACTION:
It is act on cell wall via : 1) distraction the wall already synthesis : through activation autolysin ( an
enzyme found inside the bacteria that lead to cell wall distraction , cause its inside the cell , the
penicillin must get into the cell ) .
2) inhibit forming of new cell wall : by inhibit the last step of cell wall formation
"transpeptidation"** , through binding protein PBP cell wall loose allowing water to reabsorb
swelling rupture death , So Penicillin is consider as BACTIROCAIDAL .
** "Cell wall synthesis of peptaidoglaycan linked to each other by cross linkage or transpeptidation "
(PREPARATION OF PENICILLIN )
1-natural
2-anti-staph
members
spectrum
GIT stability
Affect by
lactan
enzyme
natural
Penicillin G
Penicillin V
3-extended spectrum
4-anti-pseudomonas
anti-staph
extended spectrum
Cloxacillin
Ampicillin
Flucloxacillin
Amoxicillin
Nafcillin
Gram +ve & -ve COCCI, only +ve Mainly ve BACILLI
BACILLI
also +ve BACILLI &
"narrow spectrum"
cover all previous
one .
Stable
Stable
G unstable
So it can be
So it can take it oral
V stable
taking oral
Yes L
NO
Yes L
anti-pseudomonas
Ticarcillin
Carpencillin
Pipercillin
Resistant gram ve
bactiria
Unstable
So should taking
parenteral
Yes L
* The natural and anti-staph penicillin are considered narrow spectrum antibiotics, cues they don't act
on gram ve bacilli , So the broad spectrum antibiotics are extended spectrum and anti-pseudomonas .
* generally all penicillin depend on KIDNEY execration .
* all penicillin groups can be taken orally except :
1-penicillin G
2- anti-pseudomonas
can take parentally cues they are unstable with high gastric acidity .
# Bacteria succeeded in inhibiting all group of -lactam antibiotics except : Anti-staph penicillin ( by
secreting -lactemase) , so it is considered (-lactemase resistant group) .
*To overcome the effect of -lactemase , -lactemase inhibitors must be added to the antibiotics
Eg : Augmantine = Amoxicillin + Clavulanic acid .
Chemotherapy .. ( 2 / 5 )
CLINICAL USES OF PENCILLIN:
Therapeutic uses:
1-tretment of Meningococcal meningitis "penicillin can't cross BBB in normal states, it can cross
inflamed BBB as in case of meningitis"
2-tretment of streptococcal infection "in form of sore throat, sub acute bacterial endocardaitis
"SABE""
3-tretment of typhoid fever "a fever affecting stomach & GIT"
4-tretment of pneumococcal pneumonia
5- treatment of syphilis and gonorrhea
6-tretment of Tetanus and gas gangrene
PROPHYLACTIC USESE:
1-prevent Recurrence of rheumatic fever
2-prevent occurrence of SABE "sub acute bacterial endocarditis"
*Why should an inflamed tonsil "in form of tonsillitis" more than 3 times per Year , must be removed?
CAUSE Streptococcal bacteria has protein in its wall called M protein which is similar to a protein in
the heart , so the immune system is attacking at the same time the infected pharynx and the heart ,
and with the recurrence of infection many times 'SABE' might develop .
*IF Penicillin is used as prophylaxis, a new preparation of penicillin must be used which is (long acting
penicillin)
Long acting penicillin eg : Benzathine given : once per month for people up to 18-20 years IM
"the muscle act as reservoir, releasing the drug gradually" 1.2 million units used as prophylaxis
taken since childhood to high risk individual till age of 18 or 20 years .
If the patient already have sub acut bacterial endocarditis ?
Amino glycosides can be used (used and reserved for serious cases as sub acute bacterial endocarditis ,
septicemia , Bacteremia , peritonitis, recurrent UTI ,etc) but not used in mild infectious a pharyngitis or
mild UTI, but it might lead to dangerous side effects as deafness and renal failure .
* Amino glycosides when used to treat SABE it needs the presence of peincillin, cause penicillin act on
distruction of cell wall and inhibit it synthesis and Amino glycosides act on inhibition of protein
synthesis, so as if penicillin is opening the way for Amino glycosides to act inside the streptococcus
bacteria .
*Is it allowed to mix both penicillin and Amino glycosides in the same syringe and give it to patient?
NO, its not allowed to avoid precipitation which affect the concentration of the drug, so the solution
for this is by giving the penicillin in one syringe then after 2-3min give the Amino glycosides in another
syringe .
Chemotherapy .. (3 / 5 )
Given :
Act on :
Effect :
Carbapenems
Brood spectrum
IV
GRAM +VE / - VE
Aerobic / Anaerobic
monobactams
Narrow spectrum
IV , IM
GRAM - VE
Aerobic
* when he mention this drugs can effect on anaerobic bacteria that mean can use it for treatment of
dental and bone infection eg : Carbapenems .
Cell wall inhibiters
-lactam antibiotic
Vancomycin
Bacitracin
macroclines
Tetracycline
clindamycin
chloramphenicol
aminoglycoside
Chemotherapy .. ( 4 / 5 )
Drugs dealing with proteins
microclines
Tetracycline
clindamycin
chloramphenicol
aminoglycoside
3- septicemia
4 hepatic coma
microclines
Tetracycline
clindamycin
chloramphenicol
aminoglycoside
microclines
Tetracycline
clindamycin
chloramphenicol
aminoglycoside
microclines
Tetracycline
clindamycin
chloramphenicol
aminoglycoside
Chloramphenicol
Clinical uses :
1) anaerobic brain abseess
2) Haemophilus influenzae meningitis
3) Typhoid
4) Eye infection
Adverse effect of chloramphenical:
1) grey baby syndrome : with baby : hypothermia hypotension renal failure
2) Bone marrow suppression
3) Optic neuritis
4) GIT upset
5) enzyme inhibition.
Chemotherapy .. ( 5 / 5 )
4th generation
Clinafloxacin
---------------------------------Mainly Gram + / less Anaerobic
Sulfonamides :
* clinical uses of sulfonamides:
1- eye infection sulfacetamides
2-burnssulfadiazine
3-colitissulfasalazine
4-malaria sulfadoxine & sulfamethoxazole.
Adverse effects of sulfonamides : CHHIK
1-crystaluria sulfonamideshould be taken with high amount of 2 liter of water 1 day to avoid
sulfonamide deposition .
2-hemolytic anemia in case of G-6P dehydrogenese deficiency .
3- hypersensitivity (due to sulfer group)
4-drug interation (high drug interaction)
*it's an enzyme inhibitor.
*it displace other drugs ( eg :if taken with warfarin it will cause cerebral hemorrhage).
5-kernictrus (which is preventable mental retardation &deafness) .
*drug related to age :
1-sulfonamides forbidden completely in new borns
2-chlorapheicol forbidden completely in new borns
3- tetracycline forbidden below 8
4-ciprofluxacin forbidden<18
Done by : Tariq Elessawi , Reem Darwish , Shiraz Al-Neel , Taqwa Odeh , Ibtesam younes .
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