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House Pharmacology > Chloramphenicol, Tetracycline, Erythromycin > Flashcards

Chloramphenicol, Tetracycline, Erythromycin Flashcards

1
Q

TETRACYCLINES

History: _________ was 1st introduced in 1948. 2 years later, _________ became available.

A

Chlortetracyline

oxytetracycline

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2
Q

Sources
Chlortetracycline is from ________
Oxytetracycline is from ______

A

Streptomyces
Streptomyces

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3
Q

Tetracycline is created _____________ from _________ and from a species of ________

A

Semi-synthetically

Chlortetracycline

Streptomyces

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4
Q

Demeclocycline is a product of a mutant strain of ____________

A

Streptomyces Aureofaciens

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5
Q

Mention 3 semi synthetic cycline derivatives

A

Metha

Doxy

Mino

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6
Q

Tetracyclines are usually drugs of choice for bacterial infections.

T/F

A

F

They are not

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7
Q

Tetracyclines

The more lipo____ drugs, ______ and ______ usually are the most active by weight, followed by _______.

A

Philic

minocycline and doxycycline

tetracycline

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8
Q

Resistance of a bacterial strain to any one member of the class usually results in __________ to other tetracyclines.

A

cross resistance

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9
Q

Tetracyclines are bacteri_____agents.

A

Ostatic

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10
Q

Tetracyclines

Rapidly multiplying micro-organisms are least affected.

T/F

A

F

Most

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11
Q

Tetracyclines

Order of activity : ??

A

Minocycline

Doxycycline

Tetracycline

Oxytetracycline

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12
Q

In general gram- _____ micro organisms are affected by lower conc. of tetracycline than are grain –______ special agents.

A

positive

negative

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13
Q

Neisseria gonorrhoea and many strains of N.meningititis are still inhibited by tetracyclines

A

F

Neisseria gonorrhoea and many strains of N.meningititis were initially inhibited by tetracyclines though sensitivity patterns changed over the
years.

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14
Q

Tetracyclines

Mechanism of Action: Site of action is the ___________, inhibiting ______

A

bacterial ribosome 30S

protein synthesis.

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15
Q

Absorption, distribution, and Excretion

Most tetracyclines are (adequately or inadequately?) but (completely or incompletely?) absorbed from the GIT.

Most absorption takes place from ________________ and is greater in the ________ state, though more recent studies show that ______ is well absorbed after food and this _______________

A

adequately

incompletely

stomach and upper small intestine

fasting; doxycycline

even prevents or ameliorates the GIT disturbance initially associated with its administration.

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16
Q

Doxycycline

The drug accumulates with resultant high concentrations in the GIT following repetitive dosing such that many aerobic and anaerobic coliform micro-organisms and gram-positive _______ bacteria are _____.

Consequently, the _______ is altered, the stools become ______,______ and acquire a ____,_____ colour.

Diarrhea can also occur and
ocassionally, pseudomembranous colitis may occur.

A

Spore-forming

suppressed

intestinal flora

softer, odourless

yellow-green

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17
Q

Tetracycline

Absorption is impaired by ___ products, _______ gels, Nabicarbonate, ____ salts, ____ preparations.

There is irregularity of absorption from GIT hence a wide range of plasma conc in different individuals ff oral administration.

A

milk

aluminium hydroxide

calcium; iron

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18
Q

They can be divided into 3 groups based on the dosage and frequency of oral administration required to produce effective plasma concentration.

Oxytetracycline and Tetracycline – Adults ___mg 6 hly

methacycline – ___mg 6 hly.

Deoxycycloine and minocycline – ____mg every 12 hours in 1st 24 hours ff by 100mg once a day or twice daily when infection is severe.

A

250

150

100

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19
Q

Food does not interfare with the absorption of doxycycline and minocycline.

T/F

A

T

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20
Q

The volume of distribution of many of the tetracycline is relatively larger than that of the body water.

T/F

A

T

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21
Q

Tetracycline

They are all concentrated in the ____ and
excreted by way of the ____ into the intestine from which they are ___________

A

liver

bile; partially reabsorbed.

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22
Q

Minocycline reaches a sufficient conc in ______ and _____ to eradicate the meningococcal carrier state.

A

tears and saline

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23
Q

High conc of tetracycline is found in fetal circulation and breast milk.

T/F

A

T

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24
Q

Tetracycline

They are stored in _____ cells of the liver, spleen, and bone marrow and in bone and the __________________

main route of excretion is the _____, also in ____.

A

reticuloendothelial

dentine and enamel of unerupted teeth.

kidney; faeces

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25
Q

Tetracycline

Preps, Routes – usually _____ and some by _______.

Topical administration restricted to use on ______ because of a high risk of _____.

Never inject _______ and rarely given ________.

A

oral capsules

I.V injection

the eye; sensitization

intrathecally

intramuscularly

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26
Q

Tetracycline

UNTOWARD EFFECTS

____ irritation, ______ burning and stress, ______ discomfort, nausea, and vomiting.

The larger the dose the greater the likelyhood of an irritative reaction.

__________, ______ toxicity, ______ toxicity.

A

GIT

Epigastric

abdominal

Photocoxicity; hepatic; Renal

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27
Q

Tetracycline

UNTOWARD EFFECTS

_______ then _______ discolouration of teeth if administered up to ___ years, however, generally most authorities agree that it should not be administered to children up to ____ years of age.

The deciduous teeth are at the greatest danger affected if given from ___________ to _______ of the postnatal period, while the greatest danger to the permanent teeth coloration occurs if given between the ages of ______ and _______ . Super infection.

A

Yellowish then Brownish; 8

12

mid- pregnancy to 4/6 months

2 months and 5 years

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28
Q

CHLORAMPHENICOL
History: produced by _________

A

streptomyces venezuelae

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29
Q

Mechanism of action: Chloramphenicol inhibits ______ in bacteria by binding (reversibly or irreversibly?) to the ___S ribosomal subunit near the site of
action of the _______ antibiotics and _______, which it inhibits (competitively or non competitively?) .

It also inhibits _______ protein synthesis in _______ cells

A

protein synthesis

reversibly

50

macrolide; clindamycin

Competitively ; mitochondrial; mammalian

30
Q

Chloramphenicol

Resistance has been growing, in the case of gram negative bacteria it is due to the presence of a specific _____ acquired, a specific _______ inactivates the drug.

A

plasmid

acetyl transferase

31
Q

Absorption, Distribution, Fate and Excretion
Two forms are available for oral administration (1) the _________ and (2) the ___________

Hydrolysis of (2) occurs rapidly and
almost completely by __________ in the ___________.

A

active drug

prodrug chloramphenicol palmitate

pancreatic lipases

duodenum

32
Q

Chloramphenicol

Bioavailability is greater for the proactive drug than active drug

A

F

Active is more than proactive

33
Q

Chloramphenicol

Absorption of I.M. is usually not ________, however, I.V. of the parenteral form succinate is as suitable as
P.O. or I.M.,

Clearance is by the _____ hence ____ insufficiency, poor ______ function in neonates lead to conc. In plasma.

This is well distributed in body fluids and readily reaches therapettic conc in CSF (____% of plasma) in the presence or absence of meningitis.

A

predicable

kidney; renal; renal

60

34
Q

Chloramphenicol

Doesn’t readily traverse the placental barrier and is not secreted in milk.

T/F

A

F

35
Q

The major route of elimination of chloramphenicol is _____ metabolism to the inactive _______.

This metabolite as well as cholamphenicol is excreted in ______.

A

hepatic; glucoromide

Urine

36
Q

THERAPUTIC USES of chloramphenicol

____________ when the strains causing the organism are susceptible though the use of other newer drugs which usually do not possess serious untoward effects and can be administered for shorter periods has overtaken chloramphenicol in this regard.

A

Typhoid fever

37
Q

Chloramphenicol therapeutic uses

It was very valuable against ______ infection especially ______ and ________, but it is now rarely indicated because of the ___________

A

bacterial anaerobic

intra-abdominal and brain abscesses

availability of numerous equally effective and less toxic alternative.

38
Q

Chloramphenicol

Used in _______ diseases when tetracycline cannot be used.

A

Rickettsial

39
Q

Chloramphenicol

Hematological Toxicity: Type A ADVERSE DRUG REACTION presenting as _________

Type B ADVERSE DRUG REACTION presenting as _______

Type C ADVERSE DRUG REACTION presenting as ________

Type D ADVERSE DRUG REACTION presenting as _______. This occurs sometime after the patient has taken the drug.

A

dose related anaemia.

aplastic anemia

anemia after chronic administration

aplastic anaemia

40
Q

Chloramphenicol

In Type B ADVERSE DRUG REACTION

These patients present in ______ fashion. Who develops anemia cannot
be predetermined, the duration of drug use may not be commensurate with _________ or _______

A

an unpredictable

develop of anemia or depth of anemia

41
Q

Gray baby syndrome can occur in adults

T/F

A

T

42
Q

Chronic administration of ____ or acute administration of ______ shortens the t1/2 of chloramphnicol leading to sub-theraputic concentrations of the drug

A

phenobarbital

rifampin

43
Q

Erythromycin is produced by a strain of ______________(formerly _________ ) and belongs to the ________ group of antibiotics.

A

Saccharopolyspora erythraea

Streptomyces erythraeus

macrolide

44
Q

Erythromycin is (acidic or basic?) and readily forms salts with acids.

A

Basic

45
Q

Erythromycin is a white to off-white powder, _______ in water, and _______ in alcohol, chloroform, and ether

A

slightly soluble

soluble

46
Q

The passage of the erythromycin across the blood-brain barrier _____eases in meningitis.

A

Incr

47
Q

Erythromycin crosses the placental barrier

fetal plasma levels of erythromycin are high.

Erythromycin is excreted in human milk.

Erythromycin is removed by peritoneal dialysis or hemodialysis.

T/F

A

T
F(low)
T
F(it’s not)

48
Q

In the presence of normal hepatic function, erythromycin is concentrated in the _____ and is excreted in the _____

A

liver; bile

49
Q

the effect of hepatic dysfunction on biliary excretion of erythromycin is known.

Mention it

A

It’s not known

50
Q

After oral administration, less than ___% of the administered dose can be recovered in the active form in the urine.

A

5

51
Q

Optimal blood levels are obtained when Erythromycin Base Filmtab tablets are given in the _____ state (at least ____________________).

A

fasting

1⁄2 hour and preferably 2 hours before meals

52
Q

Erythromycin acts by inhibition of protein synthesis by binding ___ S ribosomal subunits of susceptible organisms.

A

50

53
Q

Erythromycin does not affect nucleic acid synthesis.

T/F

A

T

54
Q

Many strains of ___________ are resistant to erythromycin alone but are susceptible to erythromycin and _____ used concomitantly.

A

Haemophilus influenzae

sulfonamides

55
Q

Tetracycline is effective against ____,______,______,______

A

Ricketssiae
Chlamydia
Mycoplasma
Atypical Mycobacteria

56
Q

Chloramphenicol can be exerted through the breast milk

Tetracycline can be excreted through the breast milk

Erythromycin can be excreted through the Breast milk

T/F

A

T

T

T

57
Q

Chloramphenicol is mainly used to treat ________

But can also be used to treat _____ when ———- isn’t available

A

Typhoid fever

Ricketssiae; tetracycline

58
Q

Tetracycline- acidic or basic?

Erythromycin- acidic or basic?

A

Acidic

Basic

59
Q

Mention 2 other drug classified with erythromycin?

A

Clarithromycin

Azithromycin

60
Q

Chloramphenicol is effective against anerobic organisms

T/F

A

T

61
Q

Chloramphenicol can inhibit clindamycin competitively because both have similar mechanism of action

T/F

A

F

62
Q

Chloramphenicol may cause hepatotoxicity

T/F

A

F

63
Q

Aminoglycosides = only against gram ____,_____ ; ____- spectrum

Chloramphenicol: ____ spectrum; preferred for ______

A

neg aerobes; narrow

broad; anaerobes

64
Q

Tetracyclines = _____ spectrum; preferred for _______

A

broad

intracellular microbes

65
Q

Chloramphenicol: by ____,___,______

(Poorly or well ?) absorbed; relatively fairly distributed . Loves the ____,____,_____ ; metabolized in the liver; excreted in kidney and breast milk

A

oral, IV, topical

Well

placenta, cns, breast.

66
Q

Tetracycline: by mainly ____ but also ____; good absorption ; poorly distributed, loves the _____, and _______ ; kidney and liver excretes them

A

oral; IV

bones and teeth

67
Q

Macrolide administration: ____ and ——— ; (complete or incomplete?) absorption ; well distribution; well found in placenta; excreted through the kidney

A

oral and IV

Incomplete

68
Q

Aminoglycosides = inhibit ____ stage

Chloramphenicol = inhibits _____

Tetracycline = inhibits _____

Macrolide= inhibits _____

A

initiation

transpeptidation

elongation

translocation

69
Q

Chemistry

Aminoglycosides = ______________

Chemistry of chloramphenicol =_________

Chemistry of tetracycline = ——————

Chemistry of macrolide=_______ + ________

A

2amino sugar + 2 deoxystreptamin

nitrobenzene ring

4 naphthalene carboxamide

lactose ring+ sugar

70
Q

Bacterio____ - Aminoglycosides

Bacterio_____-tetracycline

Bacterio______- chloramphenicol

A

cidal

static

Static

House Pharmacology (50 decks)

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