2nd gen > Cephamycins >
Cefoxitin, cefotetan, cefametazole
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spectrum, bacteria
narrow spectrum, Gram p+ , does not pass gram N- well
narrow spectrum, gram positive
narrow spectrum, gram positive
Active against MSSA
Enterococci and MRSA strains are resistant
These extended agents retain spectrum of activity of Penicillin G, Differ in having greater activity against gram-negative bacteria.
the extended agents retain spectrum of activity of Penicillin G, Differ in having greater activity against gram-negative bacteria.
These extended agents retain spectrum of activity of Penicillin G, Differ in having greater activity against gram-negative bacteria.
These extended agents retain spectrum of activity of Penicillin G, Differ in having greater activity against gram-negative bacteria.
spectrum similar to the extended spectrum penicillins (amoxicillin )
narrow spectrum (similar to antistaph )
negative aerobic primarily
positive aerobic as well
negative aerobic primarily
positive aerobic as well
Expanded gram negative coverage
Expanded gram negative coverage
Expanded gram negative coverage
Has activity against gram-positive and gram-negative, especially against P. aeruginosa; and gram-negative organisms with multiple-drug resistance patterns
It has a broad gram-negative spectrum activity
only gram negative aerobic
no activity against gram positive bacteria or anaerobes.
gram positive cocci, gram negative rods and anaerobes
gram- positive bacteria. No activity against gram-negative organisms.
active against anaerobes
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DOC, disease
1.diphtheriae ( crystalline penicillin G)
2.Penicillin G is commonly used as the drug of choice for prophylactic antibiotic during labor to prevent group B Streptococcus (GBS) infection in newborns
syphilis (sexually transmitted infection)
it is replaced by amoxicillin clinically
1.certain Staphylococcus infections
2. clean surgical sites ( brain ) as a prophylaxis
the gram-positive bacillus Listeria monocytogenes,
enterococcaal species
prophylactically by dentists in high-risk patients for the prevention of bacterial endocarditis.
gram-negative bacilli, including Pseudomonas aeruginosa (common cause of healthcare-associated infections )
gram-negative bacilli, including Pseudomonas aeruginosa + klibsella pneumonia
It is the drug of choice for surgical prophylaxis , altervative to antistyphlococcual AB, can be used in clean surgical sites ( brain ) as a prophylaxis
treats :
1. Gonorrhea
2. streptopneumococci ( meningitis )
3.meningiococci ( meningitis )
4. H influenza ( meningitis )
but not Listeria monocytogens meningitis
+ when we suspect meningitis after physical examination it is used as an empirical therapy cause it is dangerous to wait for he results
we add ampicillin for extreme ages cause it may be Listeria
treats :
1. Gonorrhea
2. streptopneumococci ( meningitis )
3.meningiococci ( meningitis )
4. H influenza ( meningitis )
but not Listeria monocytogens meningitis
+ when we suspect meningitis after physical examination it is used as an empirical therapy cause it is dangerous to wait for he results
we add ampicillin for extreme ages cause it may be Listeria
combined with aminglycoside to treat meningitis caused by P aeurginosa
we add ampicillin for extreme ages cause it may be Listeria
1.combined with aminoglycosides
to treat psuedomonus areuginosa
2.active against bacteria with multidrug resistance
methicillin resistance styphalococcus aures ( MRSA )
especially pneumonial infections
It is considered an
alternative to 3rd generation alternative to aminoglycosides
The drug of choice for enterobacter infections
The combination of vancomycin and Aminoglycoside as GENTAMYCIN
is synergistic against
1. Sepsis or endocarditis caused by MRSA
2. MSSA in patients who are allergic to penicillins or cephalosporins ( last option )
3. antibiotic-associated enterocolitis caused by Clostridium difficile ( when we give so many antibiotics we kill the flora which will cause C.diff to grow freely and cause "antibiotic pseudomembranous colitis " distinct by yellowish membrane
4. Vancomycin in combination with gentamicin is an alternative regimen for treatment of enterococcal endocarditis in a patient with serious penicillin allergy.
prophylaxis of rich flora sites
Surgery in vagina for example(Rich in microflora) we use the one of anaerobic activity
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mechanism
inhibit transpeptidase enzyme that catalyze formation of the cross-linkages between peptidoglycan chains of the cell wall
inhibit transpeptidase enzyme that catalyze formation of the cross-linkages between peptidoglycan chains of the cell wall
inhibit transpeptidase enzyme that catalyze formation of the cross-linkages between peptidoglycan chains of the cell wall
inhibit transpeptidase enzyme that catalyze formation of the cross-linkages between peptidoglycan chains of the cell wall
inhibit transpeptidase enzyme that catalyze formation of the cross-linkages between peptidoglycan chains of the cell wall
inhibit transpeptidase enzyme that catalyze formation of the cross-linkages between peptidoglycan chains of the cell wall
inhibit transpeptidase enzyme that catalyze formation of the cross-linkages between peptidoglycan chains of the cell wall
inhibit transpeptidase enzyme that catalyze formation of the cross-linkages between peptidoglycan chains of the cell wall
inhibit transpeptidase enzyme that catalyze formation of the cross-linkages between peptidoglycan chains of the cell wall
inhibit transpeptidase enzyme that catalyze formation of the cross-linkages between peptidoglycan chains of the cell wall
inhibit transpeptidase enzyme that catalyze formation of the cross-linkages between peptidoglycan chains of the cell wall
inhibit transpeptidase enzyme that catalyze formation of the cross-linkages between peptidoglycan chains of the cell wall
inhibit transpeptidase enzyme that catalyze formation of the cross-linkages between peptidoglycan chains of the cell wall
inhibit transpeptidase enzyme that catalyze formation of the cross-linkages between peptidoglycan chains of the cell wall
inhibit transpeptidase enzyme that catalyze formation of the cross-linkages between peptidoglycan chains of the cell wall
inhibit transpeptidase enzyme that catalyze formation of the cross-linkages between peptidoglycan chains of the cell wall
inhibit transpeptidase enzyme that catalyze formation of the cross-linkages between peptidoglycan chains of the cell wall
Inhibits the cell wall synthesis by binding to PBP3(transpeptidase).
Inhibits the cell wall synthesis by binding to PBP3(transpeptidase).
cephalosporins must be administered parentally because of their poor oral absorption.
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charactersitics
weak , penicillinase sensitive
acid labile , Widely distributed, Rapid renal excretion ( dose adjusment in renal failure
penecillins Can not penetrate BBB , unless we have active acute inflammation(not chronic)
used for prolonged actions, even if the patient is sensitive for penicillin (we make desensitization…)
Rapid renal excretion ( dose adjusment in renal failure
penecillins Can not penetrate BBB , unless we have active acute inflammation(not chronic)
resist acid degredation, absorbed in the upper respiratory tract
Rapid renal excretion ( dose adjusment in renal failure
penecillins Can not penetrate BBB , unless we have active acute inflammation(not chronic)
Penicillinase-resistant Penicillins (B LACTAMASE RESISTANT) ,
Nafcillin (by biliary secretion), oxacillin and dicloxacillin (by both kidney and biliary) so no need for dose adjustment in renal failure
penecillins Can not penetrate BBB , unless we have active acute inflammation(not chronic)
water soluble
less excreted from the intestine ( may cause diarrhoea
used as an empirical therapy for listeria
ampicillin is inactivated by b-lactamase , need to be protected by b-lactamase inhibitor
(ampicillin-sulbactam)
penecillins Can not penetrate BBB , unless we have active acute inflammation(not chronic)
Rapid renal excretion ( dose adjusment in renal failure
They are inactivated by β -lactamases so they need to be protected by beta lactamase inhibitor
Amoxicillin-clavulanic acid
more excreted by GI tract
better oral absorbstion
Rapid renal excretion ( dose adjusment in renal failure
penecillins Can not penetrate BBB , unless we have active acute inflammation(not chronic)
They are inactivated by β -lactamases so they need to be protected by beta lactamase inhibitor
ticarcillin-clavulanic acid
used in combination with an aminoglycoside for a Pseudomonal infection
Rapid renal excretion ( dose adjusment in renal failure
penecillins Can not penetrate BBB , unless we have active acute inflammation(not chronic)
They are inactivated by β -lactamases so they need to be protected by beta lactamase inhibitor
Piperacillin-tazobactam
Usually an antipseudomonal penicillins are used in combination with an aminoglycoside for a Pseudomonal infection
Rapid renal excretion ( dose adjusment in renal failure
penecillins Can not penetrate BBB , unless we have active acute inflammation(not chronic)
absorbed similar to amoxicillin cross placenta , eliminated renally Adjust dose in case of renal failure
cross allergenicity with penecillin 3%-5%
penetrates well into most tissues. cross placenta , eliminated renally Adjust dose in case of renal failure
cross allergenicity with penecillin 3%-5%
More stable, wider spectrum , more towards gram negative
cross placenta , eliminated renally Adjust dose in case of renal failure
cross allergenicity with penecillin 3%-5%
More stable, wider spectrum , more towards gram negative
the only 2nd generation AB that penetrates well the BBB , but cant cure meningitis
cross placenta , eliminated renally Adjust dose in case of renal failure
cross allergenicity with penecillin 3%-5%
Active against B-lactamase producing strains
Able to cross the BBB and treat meningitis
cross placenta , eliminated renally Adjust dose in case of renal failure
cross allergenicity with penecillin 3%-5%
Active against B-lactamase producing strains
Able to cross the BBB and treat meningitis
excreted through the bile into the feces.
crosses placenta
cross allergenicity with penecillin 3%-5%
Active against B-lactamase producing strains
Able to cross the BBB and treat meningitis
cross placenta , eliminated renally Adjust dose in case of renal failure
cross allergenicity with penecillin 3%-5%
more resistant to hydrolysis by β-lactamases
cross placenta , eliminated renally Adjust dose in case of renal failure
cross allergenicity with penecillin 3%-5%
cross placenta , eliminated renally Adjust dose in case of renal failure
cross allergenicity with penecillin 3%-5%
It resists β-lactamases
Eliminated renally
No cross-allerginicity with penicillin
mono=one b lactam ring , no fused one
no cross allergenicity with penicillins
It has low susceptibility to β-lactamses
carbapenem: all ring members are carbons
Mixed with cliastatin: dehydropeptidase 1 inhibitor ,which convert it rapidly to its metabolite , which is toxic, causing nephrotoxicity ---just mixing it to make the drug safer
partial cross allergenicity with penecillin
non b lactam
Glycopetide big structure
Bactericidal against most gram-positive organisms (except enterococci).
Poorly absorbed from GIT.
Widely distributed in body tissues, thus not removed by hemodialysis So no need to adjust the dose in case of hemodialysis but It is very important to adjust the dose in renal dysfunction .
Cephamycins are not cephalosporins , just structurally related . Functionally related .
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adminstraition
not orally ( acide labile )
intramuscular
oral formulation , Absorption of most oral penicillins (except Amoxicillin) is impaired by food.
AB should be administered at least 1-2 hours before or after a meal.
Absorption of most oral penicillins (except Amoxicillin) is impaired by food.
AB should be administered at least 1-2 hours before or after a meal.
Absorption of most oral penicillins (except Amoxicillin) is impaired by food.
AB should be administered at least 1-2 hours before or after a meal.
Absorption of Amoxicillin is not impaired by food.
Absorption of most oral penicillins (except Amoxicillin) is impaired by food.
AB should be administered at least 1-2 hours before or after a meal.
Absorption of most oral penicillins (except Amoxicillin) is impaired by food.
AB should be administered at least 1-2 hours before or after a meal.
cephalosporins must be administered parentally because of their poor oral absorption.
The only antibiotic in 1st generation the is given parenterally, no oral
cephalosporins must be administered parentally because of their poor oral absorption.
cephalosporins must be administered parentally because of their poor oral absorption.
cephalosporins must be administered parentally because of their poor oral absorption.
cephalosporins must be administered parentally because of their poor oral absorption.
cephalosporins must be administered parentally because of their poor oral absorption.
cephalosporins must be administered parentally because of their poor oral absorption.
cephalosporins must be administered parentally because of their poor oral absorption.
give IV
parenterally
Absorption in GI is difficult , so not active orally
Local infections –can be given orally (Administered orally only for the treatment of antibiotic-associated enterocolitis caused by Clostridium difficile.)
Highly water soluble , limited absorption, coclea of the ear and kidneys– concentrated causing Ototoxicity and nephrotoxicity
cephalosporins must be administered parentally because of their poor oral absorption.
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adverse effect
1. Hypersensitivity reactions are the most common including:
anaphylactic shock (very rare)
Urticaria
fever
joint swelling
angioneurotic edema : edematous episodes of cutaneous and mucosal tissues such as lips, eyes, oral cavity, larynx, and gastrointestinal system (GIS)
pruritus
skin rashes.
2. Diarrhea: disruption of the normal balance of intestinal flora
3. Nephritis: methicillin
4. Neurotoxicity
5. Hematologic toxicities:
- Decreased coagulation (piperacillin, ticarcillin, and nafcillin)
- Cytopenias: treatment for longer than 2 weeks.
1. Hypersensitivity reactions are the most common including:
anaphylactic shock (very rare)
Urticaria
fever
joint swelling
angioneurotic edema : edematous episodes of cutaneous and mucosal tissues such as lips, eyes, oral cavity, larynx, and gastrointestinal system (GIS)
pruritus
skin rashes.
2. Diarrhea: disruption of the normal balance of intestinal flora
3. Nephritis: methicillin
4. Neurotoxicity
5. Hematologic toxicities:
- Decreased coagulation (piperacillin, ticarcillin, and nafcillin)
- Cytopenias: treatment for longer than 2 weeks.
1. Hypersensitivity reactions are the most common including:
anaphylactic shock (very rare)
Urticaria
fever
joint swelling
angioneurotic edema : edematous episodes of cutaneous and mucosal tissues such as lips, eyes, oral cavity, larynx, and gastrointestinal system (GIS)
pruritus
skin rashes.
2. Diarrhea: disruption of the normal balance of intestinal flora
3. Nephritis: methicillin
4. Neurotoxicity
5. Hematologic toxicities:
- Decreased coagulation (piperacillin, ticarcillin, and nafcillin)
- Cytopenias: treatment for longer than 2 weeks.
1. Hypersensitivity reactions are the most common including:
anaphylactic shock (very rare)
Urticaria
fever
joint swelling
angioneurotic edema : edematous episodes of cutaneous and mucosal tissues such as lips, eyes, oral cavity, larynx, and gastrointestinal system (GIS)
pruritus
skin rashes.
2. Diarrhea: disruption of the normal balance of intestinal flora
3. Nephritis: methicillin
4. Neurotoxicity
5. Hematologic toxicities:
- Decreased coagulation (piperacillin, ticarcillin, and nafcillin)
- Cytopenias: treatment for longer than 2 weeks.
1. Hypersensitivity reactions are the most common including:
anaphylactic shock (very rare)
Urticaria
fever
joint swelling
angioneurotic edema : edematous episodes of cutaneous and mucosal tissues such as lips, eyes, oral cavity, larynx, and gastrointestinal system (GIS)
pruritus
skin rashes.
2. Diarrhea: disruption of the normal balance of intestinal flora
3. Nephritis: methicillin
4. Neurotoxicity
5. Hematologic toxicities:
- Decreased coagulation (piperacillin, ticarcillin, and nafcillin)
- Cytopenias: treatment for longer than 2 weeks.
6. enterocolitis caused by Clostridium difficile.
1. Hypersensitivity reactions are the most common including:
anaphylactic shock (very rare)
Urticaria
fever
joint swelling
angioneurotic edema : edematous episodes of cutaneous and mucosal tissues such as lips, eyes, oral cavity, larynx, and gastrointestinal system (GIS)
pruritus
skin rashes.
2. Diarrhea: disruption of the normal balance of intestinal flora
3. Nephritis: methicillin
4. Neurotoxicity
5. Hematologic toxicities:
- Decreased coagulation (piperacillin, ticarcillin, and nafcillin)
- Cytopenias: treatment for longer than 2 weeks.
6.enterocolitis caused by Clostridium difficile.
1. Hypersensitivity reactions are the most common including:
anaphylactic shock (very rare)
Urticaria
fever
joint swelling
angioneurotic edema : edematous episodes of cutaneous and mucosal tissues such as lips, eyes, oral cavity, larynx, and gastrointestinal system (GIS)
pruritus
skin rashes.
2. Diarrhea: disruption of the normal balance of intestinal flora
3. Nephritis: methicillin
4. Neurotoxicity
5. Hematologic toxicities:
- Decreased coagulation (piperacillin, ticarcillin, and nafcillin)
- Cytopenias: treatment for longer than 2 weeks.
1. Hypersensitivity reactions are the most common including:
anaphylactic shock (very rare)
Urticaria
fever
joint swelling
angioneurotic edema : edematous episodes of cutaneous and mucosal tissues such as lips, eyes, oral cavity, larynx, and gastrointestinal system (GIS)
pruritus
skin rashes.
2. Diarrhea: disruption of the normal balance of intestinal flora
3. Nephritis: methicillin
4. Neurotoxicity
5. Hematologic toxicities:
- Decreased coagulation (piperacillin, ticarcillin, and nafcillin)
- Cytopenias: treatment for longer than 2 weeks.
6. enterocolitis caused by Clostridium difficile.
Allergy
Identical to penicillins- cross allergenicity 3-5 %
Toxicity
Severe pain (IM)
Thrombophlebitis (IV)
Renal toxicity
Hypoprothrombinemia (some cephalosporins)
Disulfiram like reaction
Stevens-Johnson syndrome
Superinfection
Allergy
Identical to penicillins- cross allergenicity 3-5 %
Toxicity
Severe pain (IM)
Thrombophlebitis (IV)
Renal toxicity
Hypoprothrombinemia (some cephalosporins)
Disulfiram like reaction
Stevens-Johnson syndrome
Superinfection
Allergy
Identical to penicillins- cross allergenicity 3-5 %
Toxicity
Severe pain (IM)
Thrombophlebitis (IV)
Renal toxicity
Hypoprothrombinemia (some cephalosporins)
Disulfiram like reaction
Stevens-Johnson syndrome
Superinfection
Allergy
Identical to penicillins- cross allergenicity 3-5 %
Toxicity
Severe pain (IM)
Thrombophlebitis (IV)
Renal toxicity
Hypoprothrombinemia (some cephalosporins)
Disulfiram like reaction
Stevens-Johnson syndrome
Superinfection
2. enterocolitis caused by Clostridium difficile.
Allergy
Identical to penicillins- cross allergenicity 3-5 %
Toxicity
Severe pain (IM)
Thrombophlebitis (IV)
Renal toxicity
Hypoprothrombinemia (some cephalosporins)
Disulfiram like reaction
Stevens-Johnson syndrome
Superinfection
Allergy
Identical to penicillins- cross allergenicity 3-5 %
Toxicity
Severe pain (IM)
Thrombophlebitis (IV)
Renal toxicity
Hypoprothrombinemia (some cephalosporins)
Disulfiram like reaction
Stevens-Johnson syndrome
Superinfection
2, enterocolitis caused by Clostridium difficile.
Allergy
Identical to penicillins- cross allergenicity 3-5 %
Toxicity
Severe pain (IM)
Thrombophlebitis (IV)
Renal toxicity
Hypoprothrombinemia (some cephalosporins)
Disulfiram like reaction
Stevens-Johnson syndrome
Superinfection
Allergy
Identical to penicillins- cross allergenicity 3-5 %
Toxicity
Severe pain (IM)
Thrombophlebitis (IV)
Renal toxicity
Hypoprothrombinemia (some cephalosporins)
Disulfiram like reaction
Stevens-Johnson syndrome
Superinfection
Allergy
Identical to penicillins- cross allergenicity 3-5 %
Toxicity
Severe pain (IM)
Thrombophlebitis (IV)
Renal toxicity
Hypoprothrombinemia (some cephalosporins)
Disulfiram like reaction
Stevens-Johnson syndrome
Superinfection
AD.E: GI upset, superinfection, vertigo, rarely hepatotoxicity
GI distress, skin rash and at very high plasma levels CNS toxicity (confusion, encephalopathy and seizures).
Partial cross allergenicity with penicillins. (20-30%)
It is irritating to tissues phlebitis at site of injection.
Chills and fever may occur.
Ototoxicity and nephrotoxicity are rare with current preparations. However, coadministration with aminoglycosides will increase this toxicity.
Red man or red neck syndrome: infusion related flushing due to histamine release.
Allergy
Identical to penicillins- cross allergenicity 3-5 %
Toxicity
Severe pain (IM)
Thrombophlebitis (IV)
Renal toxicity
Hypoprothrombinemia (some cephalosporins)
Disulfiram like reaction
Stevens-Johnson syndrome
Superinfection
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mnemonics
vk: very acidic , keep resisting acid
nafcillin ( nafci : نفسية )
the only one undergoes biliary secretion
a(p)micillin is an em(p)irical therapy for (lis)teria the (less) excectred bacteria from intestine , if it will stay longer in the intestine then it is perfect to cure enterococcal bac
(p)e(p)iracillin 2p's treats (p)suedomonus areginosa and klibsella (p)neumonia
special mnemonic:
if your name is (hal)a, cap(hal)exine , you are always in the first place ( 1st G )
cefa(zol)ine , zol زول = واحد بالسوداني
1st generation
cefa(clor) , (chlor)ide molecule is written Cl(2) , 2nd generation
the only sec gen that penetrate BBB
and still can not treat meningitis
the pure example of " خالف تُعرف "
a sentence of 2 words = 2nd gen
third gen are the family of 3
cefotaxi(me) = me
ceftrix(one) = one cute child
ceftazi(dime) = di me, my other half
+ (cefo)tax(i)(m)(e) = (cefo) (i)s (m)eningitis (e)mpirical therapy
third gen are the family of 3
cefotaxi(me) = me
ceftrix(one) = one cute child
ceftazi(dime) = di me, my other half
cef(tri)xone : tri = third gen
ceftrix(on)e : g(on)orrhea
third gen are the family of 3
cefotaxi(me) = me
ceftrix(one) = one cute child
ceftazi(dime) = di me, my other half
areuginosa is pronounced ( areuginoza ) :
ceft(a)(z)id(i)(m)e treats psuedomonus (a)reugino(z)a caused (m)eningitis
Four pieces of apple (pi)e
all 4th gen AB have pi
cefe(pi)me
all 5th gen AB have (rol)
rola 2005
"IMI(P)(EN)EM"
(P)otent Against (E)verything
given (p)arenetrally to treat (en)terococci
vancomycin
v : (v)ery water soluble
a : (a)lternative to penicillin and cephalosporins (a)llergic patients
n: nephroitis
c : Clostridium difficile
o : otoitis
m : MSSA , MRSA
y : yellow membrane
c : cause pseudomembranous (c)olitis
(i)(n) : (i)mpossible for (n)egative bacteria
Cefoxitin : 2 i = 2nd generation
Cefo(teta)n : 2 t + we are the sec generation to our teta = sec gen
Cefametazole : meta is the sec step of cell division