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

[3S] Antimycobacterials Flashcards

(102 cards)

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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
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)
Ethambutol
26
1ST LINE DRUGS TOXICITIES ● Dose-dependent visual disturbances ● Headache, confusion, hyperuricemia
Ethambutol
27
1ST LINE DRUGS TOXICITIES ● Eyes : Retrobulbar neuritis, loss of visual acuity, red-green color- blindness
Ethambutol
28
1ST LINE DRUGS PKINETICS Pyrazinamide metabolism
Metabolized by the liver Partly to pyrazinoic acid
29
1ST LINE DRUGS ROA Pyrazinamide
PO
30
1ST LINE DRUGS MOA ● Bacteriostatic ● Inhibits tubercle bacilli ● Converted to **pyrazinoic acid** ● Encoded by **pncA** ● Disrupts mycobacterial cell membrane metabolism and transport functions
Pyrazinamide
31
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
Pyrazinamide
32
1ST LINE DRUGS CLINICAL APPLICATIONS ● MTB (combination therapy) ● Sterilizing agent with INH or RIF that deals with intracellular mycobacteria
Pyrazinamide
33
1ST LINE DRUGS TOXICITIES ● Joint pains, myalgia, GI irritation, rash ● Nausea, vomiting, fever, photosensitivity ● Hepatotoxicity
Pyrazinamide
34
1ST LINE DRUGS TOXICITIES ● Hyperuricemia (gout) ● Contraindicated in pregnant women
Pyrazinamide
35
2ND LINE DRUGS PKINETICS Can cross the BBB
Streptomycin
36
2ND LINE DRUGS PKINETICS Streptomycin excretion
Renal
37
2ND LINE DRUGS ROA Streptomycin
IV
38
2ND LINE DRUGS MOA ● Mainly affects extracellular tubercle bacilli ● Irreversible inhibition of protein synthesis via the binding to the 30S subunit
Streptomycin
39
2ND LINE DRUGS CLINICAL APPLICATIONS ● Life-threatening TB disease (meningitis, miliary dissemination, severe organ TB) ● Pott’s disease, extracellular TB
Streptomycin
40
2ND LINE DRUGS TOXICITIES ● Ototoxicity & nephrotoxicity ● Vertigo and hearing loss
Streptomycin & Rifabutin
41
2ND LINE DRUGS PKINETICS Ethionamide metabolism
Liver
42
2ND LINE DRUGS ROA Ethionamide
PO
43
2ND LINE DRUGS MOA ● INH derivative; also inhibits mycolic acids. ● Low-level cross resistance between isoniazid and ethionamide
Ethionamide
44
2ND LINE DRUGS CLINICAL APPLICATIONS ● PTB treatment regimen for INH-intolerant patients ● Can be used for leprosy treatment
Ethionamide
45
2ND LINE DRUGS TOXICITIES Hepatotoxicity, GI irritation, and neurotoxicity
Ethionamide
46
2ND LINE DRUGS PKINETICS Capreomycin excretion
Urin
47
2ND LINE DRUGS ROA Capreomycin
PO/IV
48
2ND LINE DRUGS MOA ● Binds to 70S ribosomal subunit. ● Cross-resistance with amikacin and kanamycin ● Resistance occurs due to **rrs, eis, tlyA** gene mutations
Capreomycin
49
2ND LINE DRUGS CLINICAL APPLICATIONS Treatment of drug- resistant tuberculosis
Capreomycin
50
2ND LINE DRUGS TOXICITIES ● [Ototoxicity] tinnitus, deafness, vestibular disturbances ● Nephrotoxicity
Capreomycin
51
2ND LINE DRUGS PKINETICS Cycloserine excretion & ROA
Renal & PO
52
2ND LINE DRUGS MOA Inhibits cell-wall synthesis (peptidoglycans)
Cycloserine
53
2ND LINE DRUGS CLINICAL APPLICATIONS Used in combination treatment for Mycobacterium avium complex and TB
Cycloserine
54
2ND LINE DRUGS TOXICITIES ● Peripheral neuropathy, ● CNS dysfunction (depression and psychoses)
Cycloserine
55
2ND LINE DRUGS PKINETICS Aminosalicylic Acid excretion & ROA
Renal & PO
56
2ND LINE DRUGS MOA Inhibits folic acid synthesis and mycobactin synthesis
Aminosalicylic Acid
57
2ND LINE DRUGS CLINICAL APPLICATIONS Anti-mycobacterial agent used in combination to treat active tuberculosis
Aminosalicylic Acid
58
2ND LINE DRUGS TOXICITIES ● High concentrations can cause crystalluria ● Gastrointestinal symptoms, hypersensitivity, hemorrhage ● Hepato-, nephro-, and thyroid toxicities
Aminosalicylic Acid
59
2ND LINE DRUGS PKINETICS Kanamycin & Amikacin excretion & ROA
Renal & IV/IM
60
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
Kanamycin & Amikacin
61
2ND LINE DRUGS CLINICAL APPLICATIONS Used in combination for Treatment of streptomycin- resistant or MDR-TB
Kanamycin & Amikacin
62
2ND LINE DRUGS TOXICITIES ● Ototoxicity ● Nephrotoxicity
Kanamycin & Amikacin
63
2ND LINE DRUGS PKINETICS Fluoroquinones excretion & ROA
● Renal excretion ● Partial biliary excretion ● PO/IV
64
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
Fluoroquinones
65
2ND LINE DRUGS CLINICAL APPLICATION MTB resistant to first-line agents
Fluoroquinones
66
2ND LINE DRUGS TOXICITIES ● Nausea, vomiting, diarrhea, abnormal liver function, headache, dizziness. ● Peripheral neuropathy and central neurotoxicities (agitation, impaired memory etc.)
Fluoroquinones
67
2ND LINE DRUGS PKINETICS Linezolid excretion & ROA
Renal & PO
68
2ND LINE DRUGS MOA ● Point mutations causes linezolid resistance ● Inhibitor of monoamine oxidase enzymes and binds to the 50S subunit to prevent bacterial division
Linezolid
69
2ND LINE DRUGS CLINICAL APPLICATIONS Used in combination with pyroxidone for treatment of MDR tuberculosis
Linezolid
70
2ND LINE DRUGS TOXICITIES ● Bone marrow suspension, irreversible peripheral and optic neuropathy ● Serotonin syndrome
Linezolid
71
2ND LINE DRUGS PKINETICS ● 20% bioavailability ● 53% of oral dose
Rifabutin
72
2ND LINE DRUGS PKINETICS Rifabutin excretion, metabolism, ROA
Excreted in urine & feces Hepatic metabolism PO
73
2ND LINE DRUGS MOA ● Inhibition of DNA- dependent polymerase RNA ● Cross-resistance with rifampin
Rifabutin
74
2ND LINE DRUGS CLINICAL APPLICATIONS ● Equally effective as anti- mycobacterial agent ● For HIV/AIDS patients taking ARVs ● MAC, MTB, M. fortuitum
Rifabutin
75
2ND LINE DRUGS PKINETICS Rifapentine excretion & ROA
Renal & fecal + PO
76
2ND LINE DRUGS MOA ● Same drug interaction profile as Rifampin (Inhibiting of DNA-dependent RNA polymerase)
Rifapentine
77
2ND LINE DRUGS CLINICAL APPLICATIONS ● Active against Mycobacterium avium complex and M tuberculosis ● Used in combination with isoniazid to LTBI in PLHIVs
Rifapentine
78
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
Rifabutin
79
2ND LINE DRUGS PKINETICS Not absorbed from the GI tract
Rifaximin
80
2ND LINE DRUGS ROA Rifaximin
PO
81
2ND LINE DRUGS CLINICAL APPLICATIONS Traveler’s diarrhea
Rifaximin
82
2ND LINE DRUGS TOXICITIES Nausea, headache, dizziness, joint pain, muscle tightening
Rifaximin
83
2ND LINE DRUGS PKINETICS Bedaquiline excretion & ROA
Feces & PO
84
2ND LINE DRUGS MOA Inhibits a bacteria’s generation of energy by interfering with their proton pump of mycobacterial ATP
Bedaquiline
85
2ND LINE DRUGS CA Treats isoniazid and rifampin tuberculosis
Bedaquiline
86
2ND LINE DRUGS TOXICITIES Nausea, arthralgia, headache, hepatotoxicity, cardiac toxicity
Bedaquiline
87
DRUGS FOR LEPROSY PKINETICS Penetrates tissues well
Dapsone
88
DRUGS FOR LEPROSY PKINETICS Dapsone elimination & ROA
Urine & PO
89
DRUGS FOR LEPROSY MOA ● Mainly affects extracellular tubercle bacilli ● Irreversible inhibition of protein synthesis via the binding to the 30S subunit
Dapsone (same w/ Strep)
90
DRUGS FOR LEPROSY CA Most active drug for M. leprae
Dapsone
91
DRUGS FOR LEPROSY TOXICITIES GI irritation, fever, skin rashes, methemoglobinemia, hemolysis in patients with G6PD
Dapsone & Sulfones (Acedeapsone)
92
DRUGS FOR LEPROSY TOXICITIES Requires folic acid supplements
Dapsone & Sulfones (Acedeapsone)
93
DRUGS FOR LEPROSY PKINETICS ● Acetylated dapsone ● Distributed in all tissues
Sulfones
94
DRUGS FOR LEPROSY PKINETICS Sulfones excretion & ROA
Renal & IM
95
DRUGS FOR LEPROSY CA ● Alternative drug for P. carinii pneumonia in HIV patients; ● Possible antimalarial activity
Sulfones
96
DRUGS FOR LEPROSY PKINETICS Stored widely in reticuloendothelial tissue and skin
Clofazimine
97
DRUGS FOR LEPROSY ROA Clofazimine
PO
98
DRUGS FOR LEPROSY MOA Not clearly established
Clofazimine
99
DRUGS FOR LEPROSY CA Phenazine dye for multibacillary leprosy
Clofazimine
100
DRUGS FOR LEPROSY TOXICITIES Discoloration of the skin and conjunctivae
Clofazimine
101
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
Rifampin
102
Erythema nodosum leprosum may be suppressed by ______
thalidomide

[MT 6314] Pharmacology & Toxicology (20 decks)

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