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House Pharmacology > Sulfonamides > Flashcards

Sulfonamides Flashcards

1
Q

SULFONAMIDES

The stain sulfonamide is a generic name for derivatives of _________________ (____________).

A

para aminobenzene sulfonamide

sulfanilamide

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2
Q

para aminobenzene sulfonamide (sulfanilamide) was the 1st effective chemotherapeutic agent to be employd systemically for the prevention and cure of bacterial infections in man.

T/F

A

T

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3
Q

SULFONAMIDES
para aminobenzene sulfonamide (sulfanilamide) were the main stay of antibacterial chemotherapy before the __________ become genrally available.

A

penicillin

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4
Q

SULFONAMIDES

Most of them are relatively (soluble or insoluble ?) in H2O but their sodium salts are readily (soluble or insoluble?) .

A

Insoluble

Soluble

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5
Q

SULFONAMIDES

Conc of sulfonamides in body fluids are determined by ________ rather than by _______.

A

chemical techinicals

bioassay

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6
Q

SULFONAMIDES

The minimal structural prerequisites for antibacterial action are in __________________.

The ______________ is not essential as such, but the important feature is that the _________________ is ________________.

A

sulfanilamide itself

SO2 NH2 gaps

sulfur is directly linked to the benzene ring

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7
Q

SULFONAMIDES

The para-__________ is essential.

A

NH2gp (N4)

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8
Q

SULFONAMIDES

_______ of the para –_____ abolishes in-vitro activity; but _______ may occur in vivo with a resulting _________

A

Acylation

NH2

deacylation

return of potency.

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9
Q

SULFONAMIDES

EFFECTS ON MICROBIAL AGENTS
Effective against gram ____________________ microorganisms, they are generally Bacterio________ .

A

both gram – positive & gram negative

static

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10
Q

SULFONAMIDES

MECHANISM OF ACTION
Sulfonamides are __________ and _______ of ________ and prevent normal bacteria
utilization of it for synthesis of ________________, ploA (Folic acid).

A

structural analogues and competitive antagonists

PABA

pteroy/glutanic acid

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11
Q

SULFONAMIDES

MECHANISM OF ACTION

Suphonamides are (competitive or non-competitive?) inhibitors of the bactieral enzyme responsible for the _______ of _______ into ____________

A

competitive

incorporation of PABA

dihydropletroci acid

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12
Q

dihydropletroic acid is the immediate precursor of ________

A

folic acid.

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13
Q

____________ is the immediate precursor of folic acid.

A

dihydropletroic acid

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14
Q

SULFONAMIDES

Sensitive microorganisms are those that _______________, bacteria that can ______________ are not affected.

A

must synthesize their own PHA

utilize proformed PGA

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15
Q

Bacterio______ induced by sulfonamides is counter acted by ______ (competitively or non-competitively?)

A

stasis

PABA

competitively

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16
Q

sulfonamides

Trimethoprim exerts _____ effect with sulfonamides, it is a potent & selective competitive inhibitor of _________

A

synergistic

dihydrofolate reductase

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17
Q

Trimethoprim - inhibitor of dihydrofolate reductase

dihydrofolate reductase Reduces _______ to _________ which is required for _________ reactions, hence sequential blockage.

A

dihydrofolate

tetralydrofolate

one-carbon transfer

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18
Q

Antagonists of sulfonamide are ———-, ___________ e.g. _______

A

PABA

local anesthetic

procain

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19
Q

procaine is an ______ of _______

A

ester of PABA

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20
Q

sulfonamides

Mech of resistance, an altered enzymatic constitution of the _____________ bs(i) an alteration in the _______ that ______ ———-

2) an increased capacity to _______ or ___________

(3) an alternative __________ for ____________

4) an increased production of _________ or ____________

A

bacterial cell

enzyme that utilizes PABA,

destroy or inactivate the drug

metabolic pathway for synthesis of an essential metabolite

an essential metabolite or drug antagonist.

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21
Q

ABSORPTION, FATE & EXCRETION of sulfonamides

•It is rapidly absorbed for ______% of an oral dose except for those _____________.

•In urine ______ after a ingestion, variable & unreliable absorbtion from ______,_______,———

A

70 – 100

designed for their local effect in the GIT

30 mins

vagina, respiratory track, abraded skin.

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22
Q

All sulfonamides are bound to _______ in variable degree particularly _______.

A

plasma protein

albumin

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23
Q

Sulfonamides are distributed throughout _____ tissues and readily _______,______, and _________ fluid up to 50-80% of the simultaneously determined concentration in blood

A

all

outer pleural peritoneal , synovial, ocular

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24
Q

Sulfonamides readily attain concentration in foetal tissues sufficient to cause _______________________

A

both antibacterial and toxic effects

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25
Q

Sulfonamides

The metabolic product, the _______ forms have _____ antibacterial activity but are ________ compared to the ___________ form.

A

acetylated

no

equally toxic

un acetylated

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26
Q

acetylation of sulfonamides is a function of ________ function and time

A

hepatic

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27
Q

Sulfonamides

__________ is a major factor of excretion of both the acettlated and unacetylated form

The rate of excretion ____eases as their pKA ____eases . Tubular reabsorption and secretion also play their role

A

Glomerular filtration

incr; decr

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28
Q

Sulfilsoxazole diolamine in 4% solution or ointment for ______ use in the ____.

Sulfamethoxazole – precautions to avoid ________ because of high % of _______, relatively (soluble or insoluble?) form in the urine.

A

topical; eye

crystallnurial; acetylated ; insoluble

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29
Q

Sulfadiazine – _________ urine to decrease tubular reabsorption and increase renal clearance.

Sulfasalazine – used in _________ and _______ but recurrence in 1/3 of patients, 1 to 3g dly.

A

Alkalinize

ulcerative colitis & regional enlevitis

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30
Q

___________ in 4% solution or ointment for topical use in the eye.

___________– precautions to avoid crystallnurial b/c of high % of acetylated, relatively insoluble form in the uiwine.

A

Sulfilsoxazole diolamine

Sulfamethoxazole

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31
Q

Sulfasalazine – There is evidence that it alters the intestinal microflra of persons with ulcerative colitis.

T/F

A

F

There is no evidence that it alters the intestinal microflra of persons with ulcerative colitis.

32
Q

Sulfacetamide.

It is the ____ - _______ – sublitered derivative

•aqueous solubility (1:140) is 90* that of _________.

• Used in _________ infections.

A

N1 – a cetyl

sulfadiazine

opththalmic

33
Q

Silver sulfadiazine to silver is released (slowly or rapidly?) from the prep in concentrations that are ________ to the microorganism.

•Little ______ is absorbed but _______ concentration may reach toxic levels.

•It is used to decrease microbial colonization &incidence of infections of _______ from ______

A

Slowly

selectively toxic

Silver ; sulfadiazine

wounds from burns.

34
Q

_________ is used to decrease microbial colonization &incidence of infections of wounds from burns.

A

Silver sulfadiazine

35
Q

The trimethoprim- Sulfamethoxazole combination ( ____________)

•Trimethoprim is a ____________.

•Trimethoprim is __________times more potent than Sulfamethoxazole and effective against gram positive and negative microorganisms although resistance can occur if used alone.

A

co-trimoxazole

di-amino pyridine

20 to 100

36
Q

The trimethoprim- Sulfamethoxazole combination

Which is more potent, Trimethoprim or
Sulfamethoxazole

A

Trimethoprim is 20 to 100 times more potent than Sulfamethoxazole and effective against gram positive and negative microorganisms although resistance can occur if used alone.

37
Q

The trimethoprim- Sulfamethoxazole combination ( co-trimoxazole)

the most efficient ratio against the greatest number of microorganisms is ____ parts Sulfamethoxazole to ___ part trimethoprim

A

20

One

38
Q

The trimethoprim- Sulfamethoxazole combination

The combination is bacterio____ for some organisms .

Resistance formation is (lower or higher?) than to either substances alone

A

cidal

Lower

39
Q

The combination(co-trimoxazole ) appears to ______ the absorption of ________,

PPC of trimethoprim in ______ while sulfamethoxazole takes _______

A

slow down

sulfamethoxazole

2 hours; 4 hours

40
Q

Sulphonamides therapy is useful in the following cases

-______
-_________
-_________
-_______

A

UTI

Bacillary Dysentary

Meningococcal

Nocardiosis

41
Q
  • Meningococcal :

N.meningitidis Rx now with ________,________, or _________ ( _________ for some sensitive strains) because of ____________ to sulfonamides except if ———— to sulfonamides

A

Penicillin or ampicillion or Cephalosporins

chloramphenicol

resistance formation

sensitivity

42
Q

PRINCIPLE OF UTI DRUG TREATMENT
Pylonephitis + Bacteremia/septiceamia= ___________, __________.

________ (or other quinolones) or other drugs to which the organisms are sensitive for example ________,_________etc

A

Amoxicill/clavulanic acid

cephalosporins

Ciprofloxacin

gentamicin, sulfonamides

43
Q

PRINCIPLE OF UTI DRUG TREATMENT

____________+ ________/________= Amoxicill/clavulanic acid,
cephalosporins. Ciprofloxacin(or other quinolones) or other drugs to which the organisms are sensitive for example gentamicin, sulfonamides etc

A

Pylonephitis

Bacteremia/septiceamia

44
Q

PRINCIPLE OF UTI DRUG TREATMENT

Mixture of microorganism of organisms can occur also, then sulfonamide may be useful as ________________ when indicated

A

a co- administered drug

45
Q

PRINCIPLE OF UTI DRUG TREATMENT

_________/________ (Re-infectioin or Bacteraemia) in some cases may justify the use of sulfonamides

A

Chronic /Recurrent

46
Q

PRINCIPLE OF UTI DRUG TREATMENT

CHRONIC OR RECURRENT CAN BE CAUSED BY __________,______________ , ABNORMALITY OF ______, _________ AND __________

A

Urolithiasis/Nephrolithiasis,
Obstruction

TRACT, DIABETES

DECREASED URINATION

47
Q

PRINCIPLE OF UTI DRUG TREATMENT

Acute Lower tract INFECTION: pending sensitivity
_____________

__________ especially in pregnancy, for nonpregnant, quinolones, sulfonamide, genticin also when indicated.

A

Amoxicillin/clavulanic acid

cephalosporins

48
Q

Methenamine – URINARY tract antiseptic owes it activity to ________.

____________ of urine promotes its antibacterial action.

A

formaldehyde

Acidification

49
Q

Methenamine –

________ decomposes in the blood & tissues so no ___________ from aminoria or formaldelyde.

Various substances given in addition to keep urine pH _______ e.g _______,_______,_______

A

So little; systemic toxicity

below 5.5

Ascorbic acid, mandelic, lippuric acid.

50
Q

Methenamine –

is a primary drug for UTI

is a secondary drug for chronic suppressive Rx.

T/F

A

F

F

is not a primary drugs for UTI but for chronic suppressive Rx.

51
Q

Microorganisms develop resistance to formaldehyde.

T/F

A

F

Microorganisms do not develop resistance to formaldehyde.

52
Q

The Quinolones: This & _________ inhibit ________ during bacteria replication.

A

Nalidixic acid

DNA synthesis

53
Q

Nalidixic acid is bacteri_____ to most gram-negative bacteria in UTI.

A

cidal

54
Q

Nalidixic acid :

(Poorly or Well?) absorbed from GIT

(high or low ?) conc of Nalidixic acid & metabolite (hydroxynalidixic acid) in urine.

_______ and _______ are necessary if Treatment last longer than 2 weeks.

A

Well

High

LFT & blood tests

55
Q

Nalidixic acid :

ADRs include ____ toxicity, ____ disturbances occasionally

A

CNS

GIT

56
Q

Which is more potent, oxolinic acid or nalidixic acid.

A

Oxolinic acid 2 to 4 x more potent than nalidixic acid.

57
Q

Norfloxacin, ciprofloxacin & perfloxacin good activities against gram-positive and negative orgs.

Norfloxacin, ciprofloxacin & perfloxacin can be used for systemic diseases.

T/F

A

T

T

58
Q

________ acid similar in structure to oxolinic acid.

A

Cinoxacin

59
Q

Nitrofuratoin.

It is a ( natural or synthetic ?) nitrofuran in prevention & treatment of UTI.

It is bacteri______ for most susceptible microorganisms at conc of 32 ug/ml or less.

(Poorly or Well?) absorbed from GIT.

_________ing urine decreases antibacterial activity

A

synthetic; ostatic

Well; Alkalinizing

60
Q

Nitrofuratoin.

Side effects

Nausea, vomiting and diarrhoea.

_________ is uncommon but a serious side effect.

A

Chronic active hepatitis

61
Q

Phenazopyridine HCl – is not a ________ but ________ on the urinary tract & alleviates _____ and _________ (irritation induced)

A

urinary antiseptic

an analgesic

dysuria; frequency of urination

62
Q

Phenazopyridine HCl

It colors the urine _______ or _______.

GIT upset in ____% of patients.

A

orange or red

10

63
Q

Phenazopyridine HCl .

Combination available with __________ and _________

A

sulfisoxazole & sulfamethoxazole.

64
Q

SULPHONES

They are derivatives of ___________________________________ (dapsone, DDS), all of which have certain __________ in commons.

They are related chemically to the ———————. E.g. _______ and _______

A

4, 4-diaminodiphenylsulfone

pharm properties

sulfonamides

Dapsone & sulfoxone sodium.

65
Q

much of action of sulphones are similar to sulfonamides.

T/F

A

T

66
Q

SULPHONES

Secondary resistance can occur to Dapsone by ______ especialy __________ particularly with _____ drug therapy.

Primary resistance also occurs which can be ______________

A

M leprae; lepromatous leprosy; single

partial or complete

67
Q

SULPHONES

UE – ________ is commonest. ___________ deficiency predisposes to _______.

______________ is also common.

A

Hemolysis

Glucose-6-P04 dehydrogenese

hemolysis

Methemoglobineria

68
Q

SULPHONES

UE –
Anorexia, nausea & vomiting, CNS manifestation, exacerbation of lemomatous leprosy “ __________ ” 5 to 6/52 after start therapy in malnourished people.

________ of treatment may be necessary in the course of treatment

A

sulfone syndrome

Stoppage

69
Q

Dapsone is (slowly or rapidly?) and almost ________ absorbed from the GIT.

A

Slowly

completely

70
Q

Sulfoxone is (completely or incompletely ?) absorbed from GIT & (small or large?) amount are excreted in feces.

A

Incompletely; large

71
Q

DAPSONE

A total of ____% of Dapsone is bound to plasma potency.

It is retain in _______ and ______.

They are retained in the circulation for a (short or long?) time because of ______________________ hence __________________ is advisable.

A

70

skin and muscle

Long ; intestinal reabsorption from the bile

periodic interruption of treatment

72
Q

Dapsone is ______ in the line & then is genetically determined

A

acetylated

73
Q

DAPSONE

Dosage: treatment with Dapsone is usually started with (small or large?) amounts & increase, when serious gastric irritation occurs, ________ is given instead.

A

small

sulfoxae Na

74
Q

Sulfones are active against P. faciparium

T/F

A

T

75
Q

Sulfones are active against P. faciparium even used in P falciparium resistant cases combined with __________.

A

pyrimethamine

House Pharmacology (50 decks)

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