Penicilin Bullshit Flashcards by Iseoluwa Ojo

Penicillins are _____ antibiotics originally derived from a mould ( ______________ ).

It was discovered in ____ by ________ (Scottish microbiologist) after he observed __________ around the mould.
Dorothy

β- lactam

Penicillium notatum

1928; Alexander Fleming

halo of inhibition

How well did you know this?

Not at all

Perfectly

The chemical structure (R-__________) of penicillin was determined by _____________________ (British chemist) in _____.

C9H11N2O4S

Dorothy Crowfoot Hodgkin

1945

How well did you know this?

Not at all

Perfectly

First chemical synthesis of penicillin:
_____ by _________ (American organic chemist

1957

John Clark Sheehan

How well did you know this?

Not at all

Perfectly

Penicillins are β-lactam antibiotics consisting of a ________ joined to a _______ ring.

beta-lactam ring

thiazolidine

How well did you know this?

Not at all

Perfectly

Penicillins are β-lactam antibiotics consisting of a ________ joined to a _______ ring.

Cephalosporins has its ________ joined to a ___-member _________ ring

beta-lactam ring

thiazolidine

β-lactam ring ; 6; dihydrothiazine

How well did you know this?

Not at all

Perfectly

Penicillin

The ________ is essential for their antibacterial activity and its fusion to the ___-membered ______ ring makes the penicillins more reactive than _______________.

beta lactam ring

5; thiazolidine

monocyclic beta lactams

How well did you know this?

Not at all

Perfectly

Penicillin

Different substitution at the _____ position differentiate types of penicillin.

How well did you know this?

Not at all

Perfectly

The core penicillin structure without the R is known as _____ which has a molecular weight of _______

penam

246g/mol.

How well did you know this?

Not at all

Perfectly

First generation penicillins

-__________ spectrum
-beta lactamase (sensitive or resistant?)

narrow

sensitive

How well did you know this?

Not at all

Perfectly

First generation penicillins

Benzyl penicillin (________,________ )

benzathine benzyl penicillin (combination of __________ )

procaine benzyl penicillin (combination of ______ and ________ )

_______________________

Penicillin G, crystalline penicillin

2 penicillin G molecules with diphenylethylenediamine

procaine and Penicillin G

phenoxymethylpen icillin.

How well did you know this?

Not at all

Perfectly

First generation penicillins

______________ (Penicillin G, crystalline penicillin)

________________(combination of 2 penicillin G molecules with diphenylethylenediamine)

____________(combination of procaine and Penicillin G)

____________________

Benzyl penicillin

benzathine benzyl penicillin

procaine benzyl penicillin

phenoxymethylpen icillin.

How well did you know this?

Not at all

Perfectly

Example of a tablet first generation penicillin

phenoxymethylpen icillin.

How well did you know this?

Not at all

Perfectly

Second generation penicillins

-_____ spectrum
-beta lactamase (sensitive or resistant?) but ____________________:

Examples: ____cillin, _____xacillin,_____ cillin (phased out), nafcillin, oxacillin

narrow

resistant

ineffective against methicillin-resistant bacteria

Cloxa; fluclo; methi

How well did you know this?

Not at all

Perfectly

Third generation penicillins

-_______ spectrum

Examples :_________ (____cillin, ____cillin, and _____cillin).

Extended

Aminopenicillins

Amoxi
Ampi
Pivampi

How well did you know this?

Not at all

Perfectly

Fourth generation penicillin

-_______ spectrum
-active against ________ spp and other gram-_______ bacteria

Carboxypenicillin (______); ureidopenicillins (_______); and Mecillinam (________)

extended

Pseudomonas

negative

Ticarcillin; Piperacillin; Pivmecillinam

How well did you know this?

Not at all

Perfectly

Penicillins make use of their beta-lactam ring to bind to ____________ (________) thereby ______________________ which is responsible for maintenance of the integrity of bacteria cell wall.

transpeptidase enzyme

penicillin binding protein

inhibiting production of peptidoglycan

How well did you know this?

Not at all

Perfectly

Penicillins mechanism of action

Imbalance in degradation and production of the peptidoglycan cell wall causes _____ of bacteria.

In addition cell death is also enhanced by the _______________ while production of peptidoglycan cross links has stopped due to inhibition of the activities of the transpeptidases by Penicillins.

death

continuous hydrolyses of the peptidoglycan

How well did you know this?

Not at all

Perfectly

First generation penicillins

Benzyl penicillin injection: ____ , ______ , endocarditis, septicaemia, pneumonia, lung abscess

Benzathine penicillin injections:___, bejel, ____, _____ and upper RTI. oPenicillin V tablets: pneumonia, ear, skin, gum and throat infections

syphilis; meningitis

Yaws; pinta; syphilis

How well did you know this?

Not at all

Perfectly

Second generation penicillins

Cloxacillin: Infections caused by ____, _______ and _______ species including
penicillinase producing ________ spp.

Pneumococci

Streptococci and Staphylococci

Staphylococci

How well did you know this?

Not at all

Perfectly

Third generation penicillins

Amoxycillin: ____________ infections, in triple regimen to combat _______, typhoid fever, pneumonia, tonsilitis, bronchitis and UTI.

skin, nose, ear and throat

H. Pylori ulcer

How well did you know this?

Not at all

Perfectly

Fourth generation penicillins

Ticarcillin: As injectable antibiotic mainly for infections caused by _______, ________ and other gram ____ bacteria infections. Also for UTIs, bone and joint infections.

Piperacillin: Combines with _______ as injectable antibiotic to treat ______ and skin, gynecological, and abdominal bacteria infections.

Pivmecillinam: ——— infection (Cystitis)

Pseudomonas aeruginosa

Proteus vulgaris

negative

tazobactam; pneumonia

Bladder

How well did you know this?

Not at all

Perfectly

tazobactam is a _________

b-lactamase inhibitor

How well did you know this?

Not at all

Perfectly

Penicillin shows a synergistic effect with __________, since the inhibition of ________ allows _______ to penetrate the bacterial cell wall more easily, allowing disruption of _________ within the cell.

aminoglycosides

peptidoglycan synthesis

aminoglycosides

bacterial protein synthesis

How well did you know this?

Not at all

Perfectly

• Combining Penicillins with ____________ extend their antibacterial spectrum even though they have little or no antibiotic activity of their own.

B-lactamases inhibitors

Penicillins + Beta lactamases inhibitors Examples include ________ with amoxicillin (Augmentin), ______ with ampicillin (Unasyn) and ________ with piperacillin (Zosyn)

clavulanic acid sulbactam tazobactam

Penicillins (Adverse effects) • (Common or rare?) (≥ 1% of patients): _________, rash, urticarial, neurotoxicity, diarrhoea, nausea and superinfection including _________. • (common or Rare?) (0.1–1% of patients): fever, _____, ______ , ______, seizures, pseudomembranous colitis and vomiting.

Common hypersensitivity; candidiasis Rare erythema; dermatitis; angiooedema

The cephalosporins are bacter___ and broad spectrum β-lactam antibiotics first discovered in 1948, by __________ (Italian Pharmacologist) in form of antibacterial substance obtained from a mould, _______ ______

icidal Giuseppe Brotzu Cephalosporium acremonium.

the basic nucleus of cephalosporin (____________________________) and developed it until the first cephalosporin ( _______ ) was synthesized in 1964.

7 amino-aminocephalosporic acid cefalotin

Cephalosporins has structurally similarity with Penicillins except that the β-lactam ring is joined to a __-member ________ ring compared to the ___-member ________ ring structure of the Penicillins.

6; dihydrothiazine 5; thiazolidine

The basic structure of the cephalosporin is ______________

7-amino cephalosporanic acid

❑ First generation cephalosporin: ❖Activities Have _____ spectrum of activity (High or low?) toxicity. Very active against gram __ve cocci

broad; low +

First generation cephalosporin Is Effective against gram –ve rods T/F

First generation cephalosporin Is Effective against gram +ve rods T/F

First generation cephalosporin have very little activity against some gram negative bacteria such as ________,_______,_______,_______ , Serratia and Acinetobacter.

Pseudomonas aeruginosa, Proteus vulgaris, Enterobacter, Citrobacter

First generation cephalosporin Is active against anaerobes T/F Any exception?

T Yes. It is ineffective against Bacteroides fragillis.

Some of the 1st generation cephalosporin can cross blood brain barrier. T/F

F None of them

First generation cephalosporins can be used for treatment of meningitis T/F

F They can’t because they can’t cross BBB

Second generation cephalosporins and First generation cephalosporins Who is more active against gram+ve bacteria and who is more active against gram -ve bacteria

First generation cephalosporins Second generation cephalosporins

Who has more extended spectrum between first and second generation cephalosporins

Second

Third generation cephalosporin can cross the BBB T/F

Second generation cephalosporins ,First generation cephalosporins and third generet cephalosporins Who is most active against gram+ve bacteria and who is most active against gram -ve bacteria

First, then second, then third Third, then second, then first

Third generation cephalosporins are not useful against meningitis caused by meningococci. T/F

Third generation cephalosporins are usually used in treatment of ______ of unknown origin especially in ________ patients in in those individuals where cephalosporin possess least toxicity

sepsis immunocompromised

______-generation cephalosporins have similar activity against G+ve organisms as first-generation cephalosporins.

Fourth

Fourth generation cephalosporins are __________ that can penetrate the ________ of Gram- ______ bacteria.

zwitterions outer membrane negative

Which generation of cephalosporins have a greater resistance to β-lactamases than the third-generation cephalosporins?

Fourth!

Fourth generation cephalosporins can’t cross the blood–brain barrier and are therefore ineffective in meningitis. T/F

F Can Effective

Fourth generation cephalosporins are also used against Pseudomonas aeruginosa. T/F

Fifth-generation cephalosporins ❑Examples: ___________ ,________,_______

Ceftobiprole, ceftaroline & ceftolozane.

_______ generation cephalosporins Ceftobiprole has powerful _______ characteristics and appears to be less susceptible to _______

Fifth antipseudomonal development of resistance.

______ generation cephalosporins ❑ Ceftaroline has the antipseudomonal or VRE coverage of ceftobiprole. T/F

Fifth F Doesn’t

______ generation cephalosporins Ceftolozane is a new option for treatment of ________ Infections, and Complicated _____ Infections. Ceftolozane is combined with the β-lactamase inhibitor ______.

Fifth complicated Intra-abdominal Urinary Tract tazobactam

Cephalosporins disrupt _________ by binding to _________.

synthesis of the peptidoglycan transpeptidases (penicillin-binding proteins (PBPs))

PBPs bind to the ________ at the end of ________ (peptidoglycan precursors) to _____ the peptidoglycan. Beta-lactam antibiotics mimic the _________, thereby irreversibly inhibiting ___________________

D-Ala-D-Ala muropeptides; crosslink D-Ala-D-Ala site PBP crosslinking of peptidoglycan

Which has broader gray negative coverage between cephalosporins and penicillins

Cephalosporins

Which one of of the cephalosporins is active against MRSA and enterococci.

no one

First-generation cephalosporins are active predominantly against Gram- _________ bacteria, and successive generations have increased activity against Gram- _______ bacteria often with reduced activity against Gram- ________ organisms

positive negative positive

Cephalosporins have No activity against Gram-positive organism such as methicillin-resistant staphylococci or enterococci T/F