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[MT 6314] Pharmacology & Toxicology > [3S] Antimycobacterials > Flashcards

[3S] Antimycobacterials Flashcards

1
Q

1ST LINE DRUGS PKINETICS

● Orally absorbed
● NO BBB Penetration

A

Isoniazid

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2
Q

1ST LINE DRUGS PKINETICS

Isoniazid acetylation & excretion

A

● Acetylated by the liver
● Renally excreted

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3
Q

1ST LINE DRUGS ROA

Isoniazid

A

PO/IV

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4
Q

1ST LINE DRUGS MOA

● Bactericidal
● Inhibits mycolic acid synthesis
● Activated by KatG
● Forms a covalent complex with AcpM and KasA
● Drug interactions:
o Phenytoin,Mcarbamazepine, benzodiazepines

A

Isoniazid

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5
Q

1ST LINE DRUGS RESISTANCE MECHANISM

  1. Overexpression of inhA gene
  2. Mutation or deletion of katG gene
  3. Promotermutationsresulting in overexpression of ahpC
  4. Mutations in kasA
A

Isoniazid

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6
Q

1ST LINE DRUGS CLINICAL APPLICATIONS

● Single most important drug for TB
o PTB (Combination Therapy)
● Sole - LTBI, Close contact, prophylaxis

A

Isoniazid

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7
Q

1ST LINE DRUGS TOXICITIES

● Peripheral neuritis
● Restlessness, Muscle twitches, Insomnia
● CNS toxicity: Memory loss, Psychosis, Ataxia Seizures

A

Isoniazid

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8
Q

1ST LINE DRUGS TOXICITIES

● Hemolysis (G6PD)
● CYP 450 inhibitor (↑ conc)
● Fever and skin rashes

A

Isoniazid

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9
Q

1ST LINE DRUGS TOXICITIES

Isoniazid most common toxicity

A

Hepatitis

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10
Q

1ST LINE DRUGS TOXICITIES

● Drug-induced lupus erythematosus
● Peripheral neuropathy
● Miscellaneous: Hematologic abnormalities, Pyridoxine deficiency anemia, Tinnitus, GI discomfort

A

Isoniazid

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11
Q

1ST LINE DRUGS PKINETICS

● Distributed to most tissues including CNS
● Enterohepatic cycling
o Liver into bile
● High protein binding

A

Rifampin/Rifampicin

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12
Q

1ST LINE DRUGS PKINETICS

Rifampin excretion

A

Feces, urine

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13
Q

1ST LINE DRUGS ROA

Rifampin

A

PO/IV

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14
Q

1ST LINE DRUGS MOA

● Bactericidal
● Inhibits DNA-dependent RNA polymerase
● Binds to beta-subunit of bacterial DNA-dependent
RNA polymerase
● Inhibits RNA synthesis
● Drug interactions:
o Methadone, Anticoagulants, Cyclosporine

A

Rifampin

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15
Q

1ST LINE DRUGS RM

  1. Any one of several possible point mutations in rpoB
  2. These mutations result in reduced binding of rifampin to NA polymerase
A

Rifampin

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16
Q

1ST LINE DRUGS CLINICAL APPLICATIONS

● PTB (combination therapy)
● (Sole) INH-resistant TB or INH-intolerant LTBI
● Atypical mycobacterial infections

A

Rifampin

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17
Q

1ST LINE DRUGS CLINICAL APPLICATIONS

● Leprosy - delays resistance to dapsone
● MRSA, PRSP
● Meningococcal & Staphylococcal carriage
● Prophylaxis against H. influenzae type b disease

A

Rifampin

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18
Q

1ST LINE DRUGS TOXICITIES

Orange color

A

Rifampin

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19
Q

1ST LINE DRUGS TOXICITIES

● Skin rashes, Thrombocytopenia, Nephritis
● Cholestatic jaundice, Light- chain proteinuria, Flu-like syndrome
● Acute tubular necrosis (associated)

A

Rifampin

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20
Q

1ST LINE DRUGS PKINETICS

● Orally absorbed
● Distributed to most tissues including CNS

A

Ethambutol & Pyrazinamide

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21
Q

1ST LINE DRUGS PKINETICS

Ethambutol excretion

A

Urine

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22
Q

1ST LINE DRUGS ROA

Ethambutol

A

PO

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23
Q

1ST LINE DRUGS MOA

● Bactericidal or Bacteriostatic depending on the bacteria’s reproductive activity
● Inhibits arabinosyltransferase enzyme needed for cell wall synthesis (polymerization of arabinoglycan)
● Encoded by embCAB operon

A

Ethambutol

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24
Q

1ST LINE DRUGS RM

  1. Mutation in embB gene if drug is used alone.
  2. Results in overexpression of emb gene products or within the embB strucutral gene.
A

Ethambutol

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25
Q

1ST LINE DRUGS CLINICAL APPLICATIONS

● TB (combination therapy); usually EMB + INH, RIF, or PZA
● Combination with other agents for nontuberculous mycobacterial infections (MAC and M. kansasii)

A

Ethambutol

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26
Q

1ST LINE DRUGS TOXICITIES

● Dose-dependent visual disturbances
● Headache, confusion, hyperuricemia

A

Ethambutol

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27
Q

1ST LINE DRUGS TOXICITIES

● Eyes : Retrobulbar neuritis, loss of visual acuity, red-green color- blindness

A

Ethambutol

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28
Q

1ST LINE DRUGS PKINETICS

Pyrazinamide metabolism

A

Metabolized by the liver
Partly to pyrazinoic acid

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29
Q

1ST LINE DRUGS ROA

Pyrazinamide

A

PO

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30
Q

1ST LINE DRUGS MOA

● Bacteriostatic
● Inhibits tubercle bacilli
● Converted to pyrazinoic acid
● Encoded by pncA
● Disrupts mycobacterial cell membrane metabolism and transport functions

A

Pyrazinamide

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31
Q

1ST LINE DRUGS RM

  1. Impaired uptake of pyrazinamide
  2. Mutations in pncA that impair conversion of PZA to its active form
  3. Drug-efflux systems, especially when used alone
A

Pyrazinamide

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32
Q

1ST LINE DRUGS CLINICAL APPLICATIONS

● MTB (combination therapy)
● Sterilizing agent with INH or RIF that deals with intracellular mycobacteria

A

Pyrazinamide

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33
Q

1ST LINE DRUGS TOXICITIES

● Joint pains, myalgia, GI irritation, rash
● Nausea, vomiting, fever, photosensitivity
● Hepatotoxicity

A

Pyrazinamide

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34
Q

1ST LINE DRUGS TOXICITIES

● Hyperuricemia (gout)
● Contraindicated in pregnant women

A

Pyrazinamide

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35
Q

2ND LINE DRUGS PKINETICS

Can cross the BBB

A

Streptomycin

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36
Q

2ND LINE DRUGS PKINETICS

Streptomycin excretion

A

Renal

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37
Q

2ND LINE DRUGS ROA

Streptomycin

A

IV

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38
Q

2ND LINE DRUGS MOA

● Mainly affects extracellular tubercle bacilli
● Irreversible inhibition of protein synthesis via the binding to the 30S subunit

A

Streptomycin

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39
Q

2ND LINE DRUGS CLINICAL APPLICATIONS

● Life-threatening TB disease (meningitis, miliary dissemination, severe organ TB)
● Pott’s disease, extracellular TB

A

Streptomycin

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40
Q

2ND LINE DRUGS TOXICITIES

● Ototoxicity & nephrotoxicity
● Vertigo and hearing loss

A

Streptomycin & Rifabutin

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41
Q

2ND LINE DRUGS PKINETICS

Ethionamide metabolism

42
Q

2ND LINE DRUGS ROA

Ethionamide

43
Q

2ND LINE DRUGS MOA

● INH derivative; also inhibits mycolic acids.
● Low-level cross resistance between isoniazid and ethionamide

A

Ethionamide

44
Q

2ND LINE DRUGS CLINICAL APPLICATIONS

● PTB treatment regimen for INH-intolerant patients
● Can be used for leprosy treatment

A

Ethionamide

45
Q

2ND LINE DRUGS TOXICITIES

Hepatotoxicity, GI irritation, and neurotoxicity

A

Ethionamide

46
Q

2ND LINE DRUGS PKINETICS

Capreomycin excretion

47
Q

2ND LINE DRUGS ROA

Capreomycin

48
Q

2ND LINE DRUGS MOA

● Binds to 70S ribosomal subunit.
● Cross-resistance with amikacin and kanamycin
● Resistance occurs due to rrs, eis, tlyA gene mutations

A

Capreomycin

49
Q

2ND LINE DRUGS CLINICAL APPLICATIONS

Treatment of drug- resistant tuberculosis

A

Capreomycin

50
Q

2ND LINE DRUGS TOXICITIES

● [Ototoxicity] tinnitus, deafness, vestibular disturbances
● Nephrotoxicity

A

Capreomycin

51
Q

2ND LINE DRUGS PKINETICS

Cycloserine excretion & ROA

A

Renal & PO

52
Q

2ND LINE DRUGS MOA

Inhibits cell-wall synthesis (peptidoglycans)

A

Cycloserine

53
Q

2ND LINE DRUGS CLINICAL APPLICATIONS

Used in combination treatment for Mycobacterium avium complex and TB

A

Cycloserine

54
Q

2ND LINE DRUGS TOXICITIES

● Peripheral neuropathy,
● CNS dysfunction (depression and psychoses)

A

Cycloserine

55
Q

2ND LINE DRUGS PKINETICS

Aminosalicylic Acid excretion & ROA

A

Renal & PO

56
Q

2ND LINE DRUGS MOA

Inhibits folic acid synthesis and mycobactin synthesis

A

Aminosalicylic Acid

57
Q

2ND LINE DRUGS CLINICAL APPLICATIONS

Anti-mycobacterial agent used in combination to treat active tuberculosis

A

Aminosalicylic Acid

58
Q

2ND LINE DRUGS TOXICITIES

● High concentrations can cause crystalluria
● Gastrointestinal symptoms, hypersensitivity, hemorrhage
● Hepato-, nephro-, and thyroid toxicities

A

Aminosalicylic Acid

59
Q

2ND LINE DRUGS PKINETICS

Kanamycin & Amikacin excretion & ROA

A

Renal & IV/IM

60
Q

2ND LINE DRUGS MOA

● No cross-resistance with streptomycin and amikacin
● Binds to 30S subunit
● Interferes with mRNA binding and tRNA acceptor
sites
o to cause misreading of t-RNA
o disrupting protein synthesis

A

Kanamycin & Amikacin

61
Q

2ND LINE DRUGS CLINICAL APPLICATIONS

Used in combination for Treatment of streptomycin- resistant or MDR-TB

A

Kanamycin & Amikacin

62
Q

2ND LINE DRUGS TOXICITIES

● Ototoxicity
● Nephrotoxicity

A

Kanamycin & Amikacin

63
Q

2ND LINE DRUGS PKINETICS

Fluoroquinones excretion & ROA

A

● Renal excretion
● Partial biliary excretion
● PO/IV

64
Q

2ND LINE DRUGS MOA

● Class-resistance (resistance to one fluoroquinolone indicates resistance to others)
● Inhibits DNA gyrase and topoisomerase IV to block bacterial DNA synthesis, inhibiting cell division

A

Fluoroquinones

65
Q

2ND LINE DRUGS CLINICAL APPLICATION

MTB resistant to first-line agents

A

Fluoroquinones

66
Q

2ND LINE DRUGS TOXICITIES

● Nausea, vomiting, diarrhea, abnormal liver function, headache, dizziness.
● Peripheral neuropathy and central neurotoxicities (agitation, impaired memory etc.)

A

Fluoroquinones

67
Q

2ND LINE DRUGS PKINETICS

Linezolid excretion & ROA

A

Renal & PO

68
Q

2ND LINE DRUGS MOA

● Point mutations causes linezolid resistance
● Inhibitor of monoamine oxidase enzymes and binds to the 50S subunit to prevent bacterial division

69
Q

2ND LINE DRUGS CLINICAL APPLICATIONS

Used in combination with pyroxidone for treatment of MDR tuberculosis

70
Q

2ND LINE DRUGS TOXICITIES

● Bone marrow suspension, irreversible peripheral and optic neuropathy
● Serotonin syndrome

71
Q

2ND LINE DRUGS PKINETICS

● 20% bioavailability
● 53% of oral dose

72
Q

2ND LINE DRUGS PKINETICS

Rifabutin excretion, metabolism, ROA

A

Excreted in urine & feces
Hepatic metabolism
PO

73
Q

2ND LINE DRUGS MOA

● Inhibition of DNA- dependent polymerase RNA
● Cross-resistance with rifampin

74
Q

2ND LINE DRUGS CLINICAL APPLICATIONS

● Equally effective as anti- mycobacterial agent
● For HIV/AIDS patients taking ARVs
● MAC, MTB, M. fortuitum

75
Q

2ND LINE DRUGS PKINETICS

Rifapentine excretion & ROA

A

Renal & fecal + PO

76
Q

2ND LINE DRUGS MOA

● Same drug interaction profile as Rifampin (Inhibiting of DNA-dependent RNA polymerase)

A

Rifapentine

77
Q

2ND LINE DRUGS CLINICAL APPLICATIONS

● Active against Mycobacterium avium complex and M tuberculosis
● Used in combination with isoniazid to LTBI in PLHIVs

A

Rifapentine

78
Q

2ND LINE DRUGS TOXICITIES

● Should NOT be used to treat ACTIVE tuberculosis in HIV patients due to risk of relapse
● Can cause subtherapeutic levels of ARVs

79
Q

2ND LINE DRUGS PKINETICS

Not absorbed from the GI tract

80
Q

2ND LINE DRUGS ROA

Rifaximin

81
Q

2ND LINE DRUGS CLINICAL APPLICATIONS

Traveler’s diarrhea

82
Q

2ND LINE DRUGS TOXICITIES

Nausea, headache, dizziness, joint pain, muscle tightening

83
Q

2ND LINE DRUGS PKINETICS

Bedaquiline excretion & ROA

A

Feces & PO

84
Q

2ND LINE DRUGS MOA

Inhibits a bacteria’s generation of energy by interfering with their proton pump of mycobacterial ATP

A

Bedaquiline

85
Q

2ND LINE DRUGS CA

Treats isoniazid and rifampin tuberculosis

A

Bedaquiline

86
Q

2ND LINE DRUGS TOXICITIES

Nausea, arthralgia, headache, hepatotoxicity, cardiac toxicity

A

Bedaquiline

87
Q

DRUGS FOR LEPROSY PKINETICS

Penetrates tissues well

88
Q

DRUGS FOR LEPROSY PKINETICS

Dapsone elimination & ROA

A

Urine & PO

89
Q

DRUGS FOR LEPROSY MOA

● Mainly affects extracellular tubercle bacilli
● Irreversible inhibition of protein synthesis via the binding to the 30S subunit

A

Dapsone (same w/ Strep)

90
Q

DRUGS FOR LEPROSY CA

Most active drug for M. leprae

91
Q

DRUGS FOR LEPROSY TOXICITIES

GI irritation, fever, skin rashes, methemoglobinemia, hemolysis in patients with G6PD

A

Dapsone & Sulfones (Acedeapsone)

92
Q

DRUGS FOR LEPROSY TOXICITIES

Requires folic acid supplements

A

Dapsone & Sulfones (Acedeapsone)

93
Q

DRUGS FOR LEPROSY PKINETICS

● Acetylated dapsone
● Distributed in all tissues

94
Q

DRUGS FOR LEPROSY PKINETICS

Sulfones excretion & ROA

A

Renal & IM

95
Q

DRUGS FOR LEPROSY CA

● Alternative drug for P. carinii pneumonia in HIV patients;
● Possible antimalarial activity

96
Q

DRUGS FOR LEPROSY PKINETICS

Stored widely in reticuloendothelial tissue and skin

A

Clofazimine

97
Q

DRUGS FOR LEPROSY ROA

Clofazimine

98
Q

DRUGS FOR LEPROSY MOA

Not clearly established

A

Clofazimine

99
Q

DRUGS FOR LEPROSY CA

Phenazine dye for multibacillary leprosy

A

Clofazimine

100
Q

DRUGS FOR LEPROSY TOXICITIES

Discoloration of the skin and conjunctivae

A

Clofazimine

101
Q

DRUGS FOR LEPROSY CA

● 600 mg daily as a sole agent or 600 mg per month in combination therapy for leprosy
● Given with other drugs to prevent resistance

102
Q

Erythema nodosum leprosum may be suppressed by ______

A

thalidomide

[MT 6314] Pharmacology & Toxicology (20 decks)

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