Antitubercular Agents Flashcards

1
Q

Mechanism of Action of Streptomycin

A

inhibits CHON synthesis, irreversibly inhibit bacterial protein synthesis and binds to 30s subunit, causing a misreading of tRNA then leaving the bacteria unable to synthesize proteins

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2
Q

Mechanism of Action of Rifampin

S. mediterranei

A

inhibits RNA polymerase, inhibits DNA-dependent RNA polymerase activity by forming a stable complex w/ the enzyme
-suppresses initiation of RNA synthesis and leads to cell death

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3
Q

Mechanism of Action of Para Aminosalicylic Acid

A

Competitive inhibitor for PABA

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4
Q

Mechanism of Action of Ethionamide

A

Structural analogue of isoniazid

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5
Q

Mechanism of Action of Isoniazid

A

inhibits cell wall synthesis

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6
Q

First antibiotic for TB

A

Streptomycin

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7
Q

Most active agent and Enzyme inducer

A

Rifampin

S. mediterranei

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8
Q

For isoniazid resistant TB

A

Ethionamide

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9
Q

First line drug for short term tx

A

Pyrazinamide (Pyrazinecarboxamide)

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10
Q

Active form of Pyrazinamide

A

Pyrazinoic acid

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11
Q

First line

A

Isoniazid

Isonicotinic acid hydrazide

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12
Q

Basic red dye for leprosy, including dapsone resistant forms

A

Clofazimine

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13
Q

Combined with other agents (resistance develops rapidly)

A

Pyrazinamide (Pyrazinecarboxamide)

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14
Q

Streptomyces: S. orchidaceus, S. garyphalus, S. Lavendulus

A

Cycloserine

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15
Q

Streptomyces capreolus

A

Capreomycin

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16
Q

Adverse effects of Streptomycin

A

Ototoxicity, nephrotoxicity

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17
Q

Adverse effects of Rifampin

A

Reddish secretions

+ INH or ethambutol–> higher hepatotoxicity

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18
Q

Adverse effects of Clofazimine

A

Hyperpigmentation

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19
Q

Adverse effects of Para Aminosalicylic Acid

A

Severe GI irritation

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20
Q

Adverse effects of Ethionamide

A

Hepatotoxicity, Peripheral neuritis

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21
Q

Adverse effects of Ethambutol

A

Optic neuritis (red green color blindness)

22
Q

Adverse effects of Pyrazinamide (Pyrazinecarboxamide)

A

Hepatotoxicity

23
Q

Adverse effects of Isoniazid

Isonicotinic acid hydrazide

A
Hepatotoxicity
Peripheral neuritis (TX: pyridoxine)
24
Q

C6H7N3O

25
C5H5N3O
Pyrazinamide
26
C10H24N2O2
Ethambutol
27
C43H58N4O12
Rifampicin
28
C21H39N7O12
Streptomycin
29
C7H7NO3
Aminosalicylic Acid
30
C8H10N2S
Ethionamide
31
C12H12N2O2S
Dapsone
32
absorption and bioavailability decreases when administered with food
Isoniazid
33
active only at a slightly acidic pH
Pyrazinamide
34
Mechanism of Action of Pyrazinamide
decrease pH (making the environment acidic) w/c retards the growth of M.TB and thereby inhibiting fatty acid synthesis
35
Bactericidal and can penetrate human cells and exert lethal effect
Ethambutol
36
Mechanism of Action of Ethambutol
inhibits arabinosyl transferase w/c is involved in cell wall biosynthesis =bacterial cell wall complex production is inhibited leads to the increase of cell wall permeability
37
Additional MOA of ethambutol
this can also inhibit the transfer of mycolic acid into the cell wall
38
semisynthetic and has broad antibacterial spectrum
Rifampin
39
aminoglycoside antibiotic
Streptomycin
40
administered in association w/ isoniazid
aminosalicylic acid
41
Optimal activity of aminosalicylic acid
ortho position
42
can also be used to treat leprosy and may be bacteriostatic and bactericidal
ethionamide
43
Mechanism of action of Dapsone
inhibition of folic acid synthesis in susceptible organisms
44
resistant to isoniazid and rifampin
MDR-TB
45
resistant to isoniazid, rifampin and fluoroquinolones
XDR-TB
46
highly effective during the few months of therapy when inflammation changes are present
pyrazinamide
47
more lethal to sites showing inflammation response ( pH is acidic at these locations
pyrazinamide
48
used as adjunct in the tx of pulmonary TB
ethambutol
49
bactericidal: acts on both intra and extracellular organisms
rifampin
50
used for infections involving aerobic, g- bacteria such as Pseudomonas and Enterobacter
streptomycin