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House Pharmacology > Penicilin Bullshit > Flashcards

Penicilin Bullshit Flashcards

1
Q

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

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

A

β- lactam

Penicillium notatum

1928; Alexander Fleming

halo of inhibition

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2
Q

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

A

C9H11N2O4S

Dorothy Crowfoot Hodgkin

1945

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3
Q

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

A

1957

John Clark Sheehan

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4
Q

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

A

beta-lactam ring

thiazolidine

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5
Q

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

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

A

beta-lactam ring

thiazolidine

β-lactam ring ; 6; dihydrothiazine

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6
Q

Penicillin

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

A

beta lactam ring

5; thiazolidine

monocyclic beta lactams

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7
Q

Penicillin

Different substitution at the _____ position differentiate types of penicillin.

A

R

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8
Q

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

A

penam

246g/mol.

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9
Q

First generation penicillins

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

A

narrow

sensitive

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10
Q

First generation penicillins

Benzyl penicillin (________,________ )

benzathine benzyl penicillin (combination of __________ )

procaine benzyl penicillin (combination of ______ and ________ )

_______________________

A

Penicillin G, crystalline penicillin

2 penicillin G molecules with diphenylethylenediamine

procaine and Penicillin G

phenoxymethylpen icillin.

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11
Q

First generation penicillins

______________ (Penicillin G, crystalline penicillin)

________________(combination of 2 penicillin G molecules with diphenylethylenediamine)

____________(combination of procaine and Penicillin G)

____________________

A

Benzyl penicillin

benzathine benzyl penicillin

procaine benzyl penicillin

phenoxymethylpen icillin.

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12
Q

Example of a tablet first generation penicillin

A

phenoxymethylpen icillin.

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13
Q

Second generation penicillins

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

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

A

narrow

resistant

ineffective against methicillin-resistant bacteria

Cloxa; fluclo; methi

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14
Q

Third generation penicillins

-_______ spectrum

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

A

Extended

Aminopenicillins

Amoxi
Ampi
Pivampi

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15
Q

Fourth generation penicillin

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

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

A

extended

Pseudomonas

negative

Ticarcillin; Piperacillin; Pivmecillinam

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16
Q

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

A

transpeptidase enzyme

penicillin binding protein

inhibiting production of peptidoglycan

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17
Q

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.

A

death

continuous hydrolyses of the peptidoglycan

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18
Q

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

A

syphilis; meningitis

Yaws; pinta; syphilis

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19
Q

Second generation penicillins

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

A

Pneumococci

Streptococci and Staphylococci

Staphylococci

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20
Q

Third generation penicillins

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

A

skin, nose, ear and throat

H. Pylori ulcer

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21
Q

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)

A

Pseudomonas aeruginosa

Proteus vulgaris

negative

tazobactam; pneumonia

Bladder

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22
Q

tazobactam is a _________

A

b-lactamase inhibitor

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23
Q

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.

A

aminoglycosides

peptidoglycan synthesis

aminoglycosides

bacterial protein synthesis

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24
Q

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

A

B-lactamases inhibitors

25
Q

Penicillins + Beta lactamases inhibitors

Examples include ________ with amoxicillin (Augmentin), ______ with ampicillin (Unasyn) and ________ with piperacillin (Zosyn)

A

clavulanic acid

sulbactam

tazobactam

26
Q

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.

A

Common

hypersensitivity; candidiasis

Rare

erythema; dermatitis; angiooedema

27
Q

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, _______ ______

A

icidal

Giuseppe Brotzu

Cephalosporium acremonium.

28
Q

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

A

7 amino-aminocephalosporic acid

cefalotin

29
Q

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.

A

6; dihydrothiazine

5; thiazolidine

30
Q

The basic structure of the cephalosporin is ______________

A

7-amino cephalosporanic acid

31
Q

❑ First generation cephalosporin:
❖Activities

Have _____ spectrum of activity

(High or low?) toxicity.

Very active against gram __ve cocci

A

broad; low

+

32
Q

First generation cephalosporin

Is Effective against gram –ve rods

T/F

A

T

33
Q

First generation cephalosporin

Is Effective against gram +ve rods

T/F

A

T

34
Q

First generation cephalosporin

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

A

Pseudomonas aeruginosa, Proteus vulgaris, Enterobacter, Citrobacter

35
Q

First generation cephalosporin

Is active against anaerobes

T/F

Any exception?

A

T

Yes. It is ineffective against Bacteroides fragillis.

36
Q

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

T/F

A

F

None of them

37
Q

First generation cephalosporins can
be used for treatment of meningitis

T/F

A

F

They can’t because they can’t cross BBB

38
Q

Second generation cephalosporins and First generation cephalosporins

Who is more active against gram+ve bacteria and who is more active against gram -ve bacteria

A

First generation cephalosporins

Second generation cephalosporins

39
Q

Who has more extended spectrum between first and second generation cephalosporins

A

Second

40
Q

Third generation cephalosporin can cross the BBB

T/F

A

T

41
Q

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

A

First, then second, then third

Third, then second, then first

42
Q

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

T/F

A

F

43
Q

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

A

sepsis

immunocompromised

44
Q

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

A

Fourth

45
Q

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

A

zwitterions

outer membrane

negative

46
Q

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

A

Fourth!

47
Q

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

T/F

A

F

Can
Effective

48
Q

Fourth generation cephalosporins are also used against Pseudomonas aeruginosa.

T/F

A

T

49
Q

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

A

Ceftobiprole, ceftaroline & ceftolozane.

50
Q

_______ generation cephalosporins

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

A

Fifth

antipseudomonal

development of resistance.

51
Q

______ generation cephalosporins

❑ Ceftaroline has the antipseudomonal or VRE coverage of ceftobiprole.

T/F

A

Fifth

F
Doesn’t

52
Q

______ generation cephalosporins

Ceftolozane is a new option for treatment of ________ Infections, and Complicated _____ Infections.

Ceftolozane is combined with the β-lactamase inhibitor ______.

A

Fifth

complicated Intra-abdominal

Urinary Tract

tazobactam

53
Q

Cephalosporins disrupt _________ by binding to _________.

A

synthesis of the peptidoglycan

transpeptidases (penicillin-binding proteins (PBPs))

54
Q

PBPs bind to the ________ at the end of ________ (peptidoglycan precursors) to _____ the peptidoglycan.

Beta-lactam antibiotics mimic the _________, thereby irreversibly inhibiting ___________________

A

D-Ala-D-Ala

muropeptides; crosslink

D-Ala-D-Ala site

PBP crosslinking of peptidoglycan

55
Q

Which has broader gray negative coverage between cephalosporins and penicillins

A

Cephalosporins

56
Q

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

A

no one

57
Q

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

A

positive

negative

positive

58
Q

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

T/F

A

T

House Pharmacology (50 decks)

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