FIRST-LINE ANTITUBERCULOSIS MEDICATIONS FOR ACTIVE DISEASE

Generic Name Dosage/Administration Drug Indication Contraindication Mechanism of Action Nursing Responsibility

Isoniazid PO, IM (Adults): First-line therapy of active Hypersensitivity; Acute liver Inhibits mycobacterial cell wall Mycobacterial studies and
300 mg/day (5 mg/kg) or 15 tuberculosis, in combination disease; Previous hepatitis from synthesis and interferes with susceptibility tests should be
mg/kg (up to 900 mg) 2– 3 with other agents. Prevention isoniazid. metabolism. performed prior to and
times weekly. of tuberculosis in patients periodically throughout therapy
exposed to active disease Use Cautiously in: Therapeutic Effects: to detect possible resistance.
PO, IM (Children < 40 kg): (alone). -History of liver damage or chronic Bacteriostatic or bactericidal About 50% to 65% of
Latent TB infection— 10– 20 alcohol ingestion action against susceptible Caucasians, Black, South
Brand Name mg/kg/day (up to 300 mg/day) -Malnourished patients, patients mycobacteria. Indians and Mexicans are slow
or 20– 40 mg/kg (up to 900 with diabetes, or chronic alcoholics acetylators at risk for toxicity,
mg) 2 times weekly (qrisk of while 80 to 90% of Eskimos,
INH Active TB infection— 10– 15 neuropathy); Japanese, and Chinese are
mg/kg/day (up to 300 mg/day) rapid acetylators at risk for
or 20– 40 mg/kg (up to 900 OB, Lactation: Although safety is decreased levels and
mg) 2 times weekly. not established, isoniazid has been treatment failure.
used with ethambutol to treat
tuberculosis in pregnant women Lab Test Considerations:
without harm to the fetus Hepatic function should be
evaluated prior to and monthly
throughout therapy.

Toxicity and Overdose: If

Classification isoniazid overdosage occurs,
treatment with pyridoxine
(vitamin B) is instituted.
Therapeutics:
antituberculars Advise patient to notify health
care professional promptly if
signs and symptoms of
hepatitis (yellow eyes and
skin, nausea, vomiting,
anorexia, dark urine, unusual
tiredness, or weakness) or
peripheral neuritis (numbness,
tingling, paresthesia) occur.
 Generic Name Dosage/Administration Drug Indication Contraindication Mechanism of Action Nursing Responsibility

Rifampin PO, IV (Adults): Active tuberculosis (with other Hypersensitivity; Concurrent use of Inhibits RNA synthesis by Perform mycobacterial studies
600 mg/day or 10 mg/kg/day agents). Elimination of atazanavir, darunavir, blocking RNA transcription in and susceptibility tests prior to
(up to 600 mg/day) single meningococcal carriers. fosamprenavir, saquinavir, susceptible organisms. and periodically during therapy
dose; may also be given twice tipranavir, or ritonavir-boosted to detect possible resistance.
weekly. Unlabeled Use: Prevention of saquinavir. Therapeutic Effects:
disease caused by Bactericidal action against Assess lung sounds and
PO, IV (Children and Infants): Haemophilus influenzae type B Use Cautiously in: History of liver susceptible organisms. character and amount of
Brand Name 10– 20 mg/kg/day single dose in close contacts. Synergy with disease; Diabetes; Concurrent use sputum periodically during
or divided q 12 h (not to other antimicrobial agents for S. of other hepatotoxic agents; Spectrum: Broad spectrum therapy.
exceed 600 mg/day); may also aureusinfections. notable for activity against:
Rifadin be given twice weekly. OB, Lactation: Pregnancy or Mycobacterium spp, Lab Test Considerations:
lactation. Staphylococcus aureus, H. Evaluate renal function, CBC,
influenzae,Legionella and urinalysis periodically and
pneumophila, Neisseria during therapy
meningitidis.
Do not confuse rifampin with
rifabutin.

PO: Administer medication on

an empty stomach at least 1 hr
before or 2 hr after meals with
Classification a full glass (240 mL) of water.

Therapeutics:
antituberculars

Pharmacologic:
Rifamycins
 Generic Name Dosage/Administration Drug Indication Contraindication Mechanism of Action Nursing Responsibility

Rifabutin PO (Adults): Prevention of disseminated Hypersensitivity. Cross-sensitivity Appears to inhibit DNA- Monitor patient for signs of
300 mg once daily. If GI upset Mycobacterium avium complex with other rifamycins (rifampin) may dependent RNA polymerase in active tuberculosis (purified
occurs, may give as 150 mg (MAC) disease in patients with occur; Active tuberculosis; susceptible organisms. protein derivative [PPD],
twice daily with food. H. pylori advanced HIV infection. Concurrent ritonavir or delavirdine. chest x-ray, sputum culture,
— 300 mg/day (unlabeled). Therapeutic Effects: blood culture, urine culture,
Unlabeled Use: Treatment of Use Cautiously in: OB, Lactation, Antimycobacterial action biopsy of suspicious lymph
Helicobacter pylori ulcer Pedi: Safety not established. against susceptible organisms. nodes) prior to and throughout
Brand Name disease which has failed on therapy. Rifabutin must not be
other regimens (with Spectrum: Active againstM. administered to patients with
pantoprazole and amoxicillin). avium and most strains of M. active tuberculosis.
Mycobutin tuberculosis.
Monitor bowel function.
Diarrhea, abdominal cramping,
fever, and bloody stools should
be reported to health care
professional promptly as a sign
of pseudomembranous colitis.
May begin up to several weeks
following cessation of therapy.

Lab Test Considerations:

Classification Monitor CBC periodically
during therapy. May cause
neutropenia and
Therapeutics: thrombocytopenia.
agents for atypical
mycobacterium Do not confuse rifabutin with
rifampin.
 Generic Name Dosage/Administration Drug Indication Contraindication Mechanism of Action Nursing Responsibility

Rifapentine Must be used in combination Treatment of pulmonary Hypersensitivity to rifapentine or Inhibits DNA-dependent RNA Mycobacterial studies and
with other antituberculars. tuberculosis: Must be used in other rifamycins (rifampin or polymerase. susceptibility tests should be
combination with other agents. rifabutin). performed prior to and
PO (Adults): Therapeutic Effects: periodically throughout therapy
Intensive phase—600 mg Use Cautiously in: History of liver Bactericidal action against to detect possible resistance.
twice weekly (not less than 72 disease intracellular and extracellular
hr between doses) for 2 mo; susceptible strains of Assess lung sounds and
Brand Name continuation phase—600 mg OB, Lactation, Pedi: Pregnancy, Mycobacterium tuberculosis. character and amount of
once weekly for 4 mo. Lactation, or children 12 yr (safety sputum periodically throughout
not established). therapy.
Priftin
Exercise Extreme Caution in: Monitor bowel function.
Concurrent protease inhibitor Diarrhea, abdominal cramping,
therapy. fever, and bloody stools should
be reported to health care
professional promptly as a sign
of pseudomembranous colitis.
May begin up to several weeks
following cessation of therapy.

Rifapentine is not administered

Classification alone. When used with
isoniazid, pyridoxine (vitamin
B) is administered concurrently
Therapeutics: in patients who are
antituberculars malnourished, predisposed to
neuropathy (patients with
alcoholism or diabetes), or
adolescents to prevent
neuropathy.
 Generic Name Dosage/Administration Drug Indication Contraindication Mechanism of Action Nursing Responsibility

Pyrazinamide PO (Adults and Children): Used in combination with other Hypersensitivity; Cross-sensitivity Converted to pyrazinoic acid in Perform mycobacterial studies
15– 30 mg/kg/day as a single agents in the treatment of with ethionamide, isoniazid, niacin, susceptible strains of and susceptibility tests before
dose. Up to 60 mg/kg/day has active tuberculosis. or nicotinic acid may exist; Severe Mycobacterium which lowers and periodically during therapy
been used in isoniazid- liver impairment. the pH of the environment. to detect possible resistance.
resistant tuberculosis (not to
exceed 2 g/day as a single Use Cautiously in: Gout; Renal Therapeutic Effects: Lab Test Considerations:
dose or 3 g/day in divided failure; Diabetes mellitus; Acute Bacteriostatic action against Evaluate hepatic function
Brand Name doses). May also be given as intermittent porphyria; susceptible mycobacteria. before and every 2–4 wk
50– 70 mg/kg 2– 3 times during therapy. Increased AST
weekly (not to exceed 2 g/dose OB:Safety not established. Spectrum: Active against and ALT may not be predictive
on daily regimen, 3 g/dose for mycobacteria only. of clinical hepatitis and may
3-times-weekly regimen, or 4 return to normal levels during
g/dose for twice-weekly treatment. Patients with
regimen). impaired liver function should
receive pyrazinamide therapy
Patients with HIV—20– 40 only if crucial to treatment
mg/kg/day for first 2 mo of
therapy (maximum: 2 g/day); May be given concurrently with
further dosing depends on isoniazid
regimen employed.
Inform diabetic patients that
Classification pyrazinamide may interfere
with urine ketone
measurements
Therapeutics:
antituberculars
 Generic Name Dosage/Administration Drug Indication Contraindication Mechanism of Action Nursing Responsibility

Ethambutol PO (Adults and Children 13 Active tuberculosis or other Hypersensitivity; Optic neuritis. Inhibits the growth of Mycobacterial studies and
yr): mycobacterial diseases (with mycobacteria. susceptibility tests should be
15– 25 mg/kg/day (maximum at least one other drug). Use Cautiously in: Renal and performed before and
2.5 g/day) or 50 mg/kg (up to severe hepatic impairment Therapeutic Effects: periodically during therapy to
2.5 g) twice weekly or 25– 30 (dosage reduction required); Tuberculostatic effect against detect possible resistance.
mg/kg (up to 2.5 g) 3 times susceptible organisms.
weekly. OB: Although safety not Assess lung sounds and
Brand Name established, ethambutol has been character and amount of
PO (Children 1 mo — 13 yr): used with isoniazid in pregnant sputum periodically during
HIV negative– 15-20 women without fetal adverse therapy
Myambutol mg/kg/day once daily effects;
(maximum: 1 g/day) or 50 PO: Administer with food or
mg/kg/dose twice weekly Lactation: Usually compatible with milk to minimize GI irritation.
(maximum: 2.5 g/dose) HIV- breast feeding (AAP). PO: Tablets may be crushed
exposed/-infected– 15-25 and mixed with apple juice or
mg/kg/day once daily apple sauce.
(maximum: 2.5 g/day) MAC,
secondary prophylaxis, or Instruct patient to take
treatment in HIV-exposed/- medication as directed. Take
infected– 15-25 mg/kg/day missed doses as soon as
once daily (maximum: 2.5 possible unless almost time
Classification g/day) with clarithromycin (or for next dose; do not double
azithromycin) with or without up on missed doses. A full
rifabutin Nontuberculous course of therapy may take
Therapeutics: mycobacterial infection– 15- months to yr. Do not
antituberculars 25 mg/kg/day once daily discontinue without consulting
(maximum: 2.5 g/day). health care professional, even
though symptoms may
disappear.

Advise patient to notify health

care professional if pregnancy
is suspected