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Antimycobacterials
anti mycobacs
74
Pharmacology
Graduate
09/03/2012

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Cards

Term
First Line antimycobaterials
Definition

Isoniazid

Rifampacin

Pyrinizinamide

Ethambutol

Term
INH- MOA
Definition
Inhibits mycolic acid synthesis
Term
INH activation
Definition
KatG- only in Mb
Term
INH & liver enzymes
Definition
p450 inhibitor
metabolized in liver
various rates of acetylation
Term
INH distribution
Definition
All tissues- w/ high intracellular concentrations
Term
INH MOR
Definition
katG mutation
Term
INH- AE
Definition
Hepatitis
B6 defficiency- peripheral neuropathy, give pyridoxine
Inhibition of Phenytoin metabolism- ataxma
Term
INH method of admin
Definition
Oral
Term
INH Tmax
Definition
1-2 hr
Term
INH 1/2 life
Definition
.75-5h
Term
INH excretion
Definition
Kidney
Term
Rifampin- MOA
Definition
binds to beta subunit of Mb RNA pol --> inhibits transcription
Term
RIF method of admin
Definition
Oral- well absorbed
Term
RIF T1/2
Definition
2.5-5hr
Term
RIF- distribution
Definition
all tissues
Term
RIF & liver enzymes
Definition
CYP450 inducer
Term
RIF excretion
Definition
mostly feces, some urine
Term
RIF AE
Definition
Reddish/ brown Urine
Hepatitis
Abdominal discomfort
fever
skin eruptions
Term
RIF drug interactions
Definition
inc elimination of other drugs esp Birth control and HIV proteases- monitor the level
Term
RIfabutin
Definition
doesn't affect CYP450 so use in AIDs patients so don't inc elimination of PI
Term
Rifampimicin
Definition
Used for leprosy
Term
Pyrizinamide (PZA)- MOA
Definition
Pyrizinamidase converts it to pyrizinmatoic acid --> unknown MOA
Term
PZA method of admin
Definition
Oral
Term
PZA 1/2 life
Definition
9 hr
Term
PZA- distribution
Definition
well distributed in tissues but concentrates in cells
Term
PZA activity
Definition
active in acidic environments ie lysozomes inside of macropahges
Term
PZA metabolism
Definition
Liver
Term
PZA excretion
Definition
Kidney
Term
PZA AE
Definition
Hyperuricemia- Pyrazinoic acid inhibits renal secretion of Uric acid --> Gout monitor SGOT (liver enzyme) and uric acid
Heptatitis
Arthralgia, fever, skin rashes
Term
Ethambutol MOA
Definition
inhibits arabinosyl tranferase --> inhibits bac wall synthesis
Bacerial static
Term
Ethambutol admin
Definition
Oral
Term
Ethambutol 1/2 life
Definition
10 -15 h
Term
Ethambutol distribution
Definition
most tissues, including CNS --> used for TB meningitis
Term
Ethambutol excretion
Definition
Unchanged in urine
Term
Ethambutol AE
Definition
Retrobulbar neuritis- Optic neuritis w/o swelling of optic disc. R/G color blindness- Monthly tests for visual acuity
Peripheral neuritis
HA
Rash
Term
Streptomycin (SM)- use
Definition
occationally used in conjunction with first line tx
Term
SM- admin
Definition
IV/ IM
Term
SM- tissue distribution
Definition
distributes to tissues, but doens't concentrate in cells
Term
SM- excretion
Definition
Excreted unchanged in urine, no liver metabolism
Term
SM- AE
Definition
Ototoxicity- vistibular and auditory
renal injury
hypersensitivity
Term
SM- MOA
Definition
binds 30s subunit of bac ribosome- prevents initiation complex formation.
Inhibits translation
Term
Paraminosalicylic Acid- PSA- MOA
Definition
competes with PABA for Mb dihyropterase synthase, interferes with folic acid and thus DNA synthesis
bacteriastatic
Term
PSA- admin
Definition
oral
well absorbed
always with food
Term
PSA- T1/2
Definition
2 hr
Term
PSA metabolism
Definition
Liver
Term
PSA excretion
Definition
Kidney
Term
PSA toxicity
Definition
GI- nausea, abdominal pain, diarrhea, nausea if not given w/ food
Goiter, hypothyroidism
Anemia
Term
Ethionamide- MOA
Definition
Inhibits mycolic acid synthesis
Term
Ethionamide- admin
Definition
Oral- well absorbed
Term
Ethionamide- distribution
Definition
wide
Term
Ethionamide- metabolism
Definition
Liver metabolizes it to ethionamide sulphoxide
Term
Ethionamide excretion
Definition
ethionamide sulphoxide- kidney excretion
Term
Ethionamide - AE
Definition
pyridoxine deficiency
GI- N/D/ pain
hepatotoxicity
allergic reactions
Term
Clofazamine- uses
Definition
Leprosy and Tb
Term
Clofazoamine- MOA
Definition
inhibits DNA synthesis
Term
Clofazamine- Admin
Definition
Oral
Term
Clofazamine T1/2
Definition
10 days
Term
Clofazamine distribution
Definition
widely
concentrates in reticuloendothelil system and is slowly let out, partially accounts for long half life
Term
Clofazamine- excretion
Definition
metabolized to several inactive metabolites and excreted in the feces and urine
Term
Clofazamine - AE
Definition
Drug accumulation in tissues turns- skin, urine, and feces a red brown color, so people with leprosy don't like it b/c it marks them
GI disturbances
Term
Cycloserine/ kanamycin- MOA
Definition
inhibits cell wall synthesis
Term
Cycloserine/ Kanmycin- use
Definition
rarely used due to poor efficacy and adverse eventes
Term
Fluroquinolones-
Definition
Ciprofloxacin
Moxifloxacin
Levofloxacin
Term
Fluroquinolones- MOA
Definition
inhibit topoisomerase II
Term
Fluroquinolones- disrtibution
Definition
Low intracellular concentration
Term
Dapsone- use
Definition
Tx leprosy
Term
Dapsone- MOA
Definition
inhibits folate synthesis
Term
Dapsone- excretion
Definition
excreted into bile, reabsorbed, excreted in urine
Term
Dapsone- AE
Definition
well tolerated
Fever, GI, rash, exoliative dermatitis
Term
Dapsone Contratindications
Definition
Don't give to someone with sulfa drug allergies
Term
Second line Tb tx
Definition
Streptomyocin
Paramino Salacylic Acid
Ethionamide
Clofazamine
Cyloserine/ Kanomycin
Fluroquinolones, capreomycin
Term
Paucibacillary Tb- Tx
Definition
Rifampin& Dapsone for 6 mnths
Single lesion- Rifampin, ofloxacin, Minocycline
Term
Lepromatous MB- Tx
Definition
Rifampin, Dapsone, Clofazamine- 12 mos
Term
M. avium Tx
Definition
Azithromycin
Ethambutol
Rifabutin
Fluroquinolones
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