Antimycobacteria Flashcards

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1
Q
  • Rod-shaped, aerobic bacteria
  • Cell wall with peptidoglycolipids, fatty acids, waxes, and mycolic acid
  • Slow growth, fast acid stain,resistsant to detergents/antibiotics
A

Mycobacteria

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2
Q

Mycobacteria infecting humans

Pulmonary tuberculosis,
extrapulmonary TB

A

Mycobacteria Tuberculosis

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3
Q

Mycobacteria infecting humans

Leprosy

A

Mycobacteria Leprae

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4
Q

Mycobacteria infecting humans

Tuberculosis-like illness

A

Mycobacteria Bovis

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5
Q

Mycobacteria infecting humans

Disseminated infection, pulmonary
infections, common in
immunocompromised states/HIV

A

Mycobacterium
Avium complex

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6
Q

Mycobacteria infecting humans

Mycobacteria Properties

A
  • Intrinsically resistant to most antibiotics
  • Slow growing
  • Cell wall is impermeable to many agents
  • Intracellular pathogens, inaccessible to drugs
    that penetrate these cells poorly
  • Can also be dormant, resistant to many drugs or killed very slowly
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7
Q

Mycobacteria infecting humans

USE OF DRUG COMBINATIONS is for ?

A
  • To delay emergence of **resistance **
  • To enhance antimycobacterial efficacy
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8
Q

Mycobacteria infecting humans

What are the complications of chemotheraphy ?

A
  • Limited information about the MOA
  • Development of resistance (easily)
  • Intracellular location of mycobacteria
  • Chronic nature of the disease (protracted therapy and drug toxicities)
  • Patient compliance ( minimum of 6 months cannot miss a day )
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9
Q
  • Commonly involves the lungs but can also infect other organs
  • Liver, CNS, Bone, GI, Kidneys
  • 6th leading cause of death in the Philippines
A

M. Tuberculosis

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10
Q

Drugs for M. tuberculosis

First Line Drugs

A

Isoniazid (H)
Rifampicin (R)
Pyrazinamide (Z)
Ethambutol (E)

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11
Q
  • Structural congener of pyridoxine
  • Inhibition of enzymes required for the synthesis
    of mycolic acid
  • Bactericidal
  • Resistance can emerge **rapidly if used alone **
    1. katG gene -catalase peroxidase bioactivation of
    INH
    2. inhA gene – enzyme acyl carrier reductase
  • **Oral **
  • Metabolized by acetylation in the liver
  • Affected by genetic control of acetylation (“fast” or “slow”)
  • Majority of filipinos are SLOW
A

Isoniazid

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12
Q

Clinical Use of Isoniazid

A

Single most important drug used for TB

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13
Q

Toxicity of Isoniazid

A
  • Peripheral neuritis, Restlessness, Muscle twitches, Insomnia
  • CYP 450 enzyme inhibitor
  • Hemolysis in G6PD deficient patients
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14
Q
  • Bactericidal
  • Inhibits DNA-dependent RNA polymerase
  • Resistance – from changes in drug sensitivity of polymerase
  • can also be bacteriostatic
  • side effect : turns every bodily fluid of patient into orange color
A

Rifampin / Rifampicin

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15
Q

Clinical uses of Rifampin / Rifampicin

A
  • Used in combination with drugs
  • Can be used as sole drug in LTBI or close contacts
    with INH-resistanc strains
  • In leprosy – it delays resistance to dapsone
  • Used for MRSA, PRSP ( Penicillin Resistant Strepto Pseumoniae)
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16
Q

Toxicities and Interactions of Rifampicin / Rifampin

A
  • Can impair antibody responses
  • Skin rashes, Thrombocytopenia, Nephritis, liver
    dysfunction
  • Flu-like symptoms, anemia
  • Induces liver drug-metabolizing enzymes
17
Q
  • Equally effective as anti mycobacterial agent;
    less drug interactions
  • Preferred over Rifampin in AIDS patients taking
    some antiretrovirals
A

Rifabutin

18
Q
  • Not absorbed from GI tract, used in Traveler’s Diarrhea
A

Rifaximin

19
Q
  • Inhibits arabinosyltransferase enzyme needed for cell wall synthesis
  • Resistance due to mutation in emb gene if drug is used alone
  • Orally
  • Distributed most tissues
  • Excrited in Urine
  • Have Dose reduction in renal impairment
A

Ethambutol

20
Q

Uses for Ethambutol

A

Mainly for TBn, in combinatin with other drugs

21
Q

Toxicity of Ethambutol

A
  • Dose-dependent visual disturbances
  • Decrease in acuity, color blindness, optic
    neuritis
    , retinal damage
  • Headache, confusion, hyperuricemia, peripheral neuritis
22
Q
  • Not well known mechanism;
  • Bacteriostatic action – through pyrazinamidases
  • Resistance due to mutations in genes that encode
    enzymes; drug-efflux systems esp. when used
    alone
  • Oral
  • Penetrate most body tissues, including CNS
  • Recomendation “Don’t use alone”
A

Pyrazinamide

23
Q

Clinical use of Pyrazinamide

A
  • In combination with other drugs for MTB
24
Q

Toxicity of Pyrazinamide

A
  • Joint pains
  • **Asymptomatic hyperuricemia **
  • Myalgia, GI irritation, rash,** hepatic dysfunction**
  • Should be avoided in pregnancy
25
Q

Second-line drugs for MTB

Used in combination for life-threatening TB (meningitis, miliary TB, other EPTB)

A

Streptomycin

26
Q

Second-line drugs for MTB

For TB caused by streptomycinresistant or MDR-TB

A

Amikacin

27
Q

Second-line drugs for MTB

Active against strains of MTB resistant
to first-line agents; used in combination

A

Ciprofloxacin
and Ofloxacin

28
Q

Second-line drugs for MTB

Congener of INH; major effect – severe
GI irritation & neurologic toxicity

A
29
Q

Treatment of TB

Intensive phase:

A

2 Months

30
Q

Treatment of TB

Continuation or maintenance phase:

A

more than 4 Months

31
Q

refers to MTB
strains in which resistance to both isoniazid and
rifampicin
has been confirmed in vitro

A

Multidrug-resistant TB (MDR-TB)

32
Q

anti TB pills containing 2 or
more drugs

A

Fixed-dose combination

33
Q
  • Diagnostic and therapeutic unit that caters patients diagnosed with TB or suspected of having TB
  • Is the most effective approach in the diagnosis, treatment, and control of TB
A

TB-DOTS ( Direct Observe Treatment Strategy )

34
Q

Drugs for Leprosy

Drug of Choice is ?

A

DAPSONE (Diaminodiphenylsulfone)

35
Q
  • Most active drug against M. leprae
  • Resistance can develop if low doses
  • usually in combination with
    Rifampin and / or Cloafazimine
  • Oral
  • Eliminated in Urine
A

DAPSONE

36
Q

Dapsone of Toxicity

A
  • GI irritation
  • Fever
  • Skin rashes
  • Methemoglobinemia
  • Hemolysis in patients with G-6PD
37
Q
  • Repository form of dapsone
  • Provides inhibitory plasma concentrations
    for several months
  • Alternative drug for P. carinii pneumonia
    in HIV patients
A

Sulfones (ACEDAPSONE)

38
Q

Other drugs for Leprosy

*phenazine dye for used for multibacillary leprosy
*MOA not clearly established
*Stored widely in reticuloendothelial tissues and
skin
*T1/2 can be as long as 2 months
*Most prominent adverse effect – discoloration of
skin and conjunctivae

A

Clofazimine

39
Q

Drugs for Non-Tuberculous Mycobacteria (NTM)

Active for NTM

NTM’s are less susceptible to anti-TB drugs

A

Tetracyclines, Macrolides, Sulfonamides