This is a very useful quick reference guide to first and second-line TB drugs from the WRHI.
This reference is also available as a PDF file.
A Quick Reference to Drugs commonly used in the Management of TB
ORAL AGENTS – 1st line
NAME |
RIFAMPICIN (Bactericidal, Sterilizing) |
DOSE/KG |
10 mg/kg/day |
USUAL DOSE |
600 mg dly |
MAXIMUM DOSE |
600 mg dly |
CAUTION |
Hepatic disease, alcoholism, porphyria, hypersensitivity to Rifampicin |
COMMON SIDE EFFECTS |
↑ ALT, GI , Hypersensitivity, Orange discoloration of body fluids |
PAEDIATRIC DOSE |
10 mg/kg/day (up to 20 mg/kg/day for TBM/Miliary TB) |
RENAL DOSE |
N/A |
LIVER IMPAIRMENT DOSE |
8 mg/kg/day |
PREGNANCY |
Category C |
LACTATION |
Amount excreted too small to harm |
BUILDING A REGIMEN |
High early bactericidal activity. With Isoniazid achieves greater killing than either drug alone. Resistance more rare than Isoniazid resistance |
NAME |
ISONIAZID (Bactericidal) |
DOSE/KG |
5 mg/kg/day (10 mg/kg/day = High dose INH) |
USUAL DOSE |
300 mg dly |
MAXIMUM DOSE |
300 mg dly |
CAUTION |
Hepatic disease, Epilepsy, hypersensitivity to Isoniazid, porphyria |
COMMON SIDE EFFECTS |
Skin rash, peripheral neuropathy, ↑ ALT, neurotoxicity, haematological effects |
PAEDIATRIC DOSE |
5-10 mg/kg/day (up to 15 mg/kg/day for TBM/Miliary TB) |
RENAL DOSE |
N/A |
LIVER IMPAIRMENT DOSE |
N/A |
PREGNANCY |
Category C |
LACTATION |
Monitor infant for adverse effects |
BUILDING A REGIMEN |
Highest early bactericidal activity. With Rifampicin achieves greater killing than either drug alone. Strain of TB may still be susceptible in certain cases of resistance depending on mutation |
NAME |
PYRAZINAMIDE (Sterilizing) |
DOSE/KG |
20-30 mg/kg/day |
USUAL DOSE |
1600 mg dly |
MAXIMUM DOSE |
2 g dly |
CAUTION |
Gout, Hepatic disease, Diabetes, Renal impairment, hypersensitivity to pyrazinamide, isoniazid, ethionamide or niacin, porphyria |
COMMON SIDE EFFECTS |
Hepatotoxicity, arthralgia (hyperuricaemia), GI side effects, skin rash |
PAEDIATRIC DOSE |
15-30 mg/kg/day (up to 40 mg/kg/day for TBM/Miliary TB) |
RENAL DOSE |
Use doses at lower limit of recommended range. GFR<10 ml/min - ↓dose by 50% |
LIVER IMPAIRMENT DOSE |
Avoid drug if possible |
PREGNANCY |
Category C |
LACTATION |
No problems with usage |
BUILDING A REGIMEN |
Good sterilizing activity, contributes to shortening of duration of treatment. Resistance not tested routinely |
NAME |
ETHAMBUTOL (Bacteriostatic, may be bactericidal at high doses) |
DOSE/KG |
15-20 mg/kg/day |
USUAL DOSE |
800 mg dly |
MAXIMUM DOSE |
1000 mg dly |
CAUTION |
Eye defects, renal disease or hyperuricaemia |
COMMON SIDE EFFECTS |
Ocular toxicity, arthralgia (hyperuricaemia), GI side effects |
PAEDIATRIC DOSE |
15-25 mg/kg/day (up to 15 mg/kg/day for TBM/Miliary TB) |
RENAL DOSE |
GFR <10 ml/min – 15 mg/kg every 48 hours |
LIVER IMPAIRMENT DOSE |
N/A |
PREGNANCY |
Max 15 mg/kg/day |
LACTATION |
No known adverse effects |
BUILDING A REGIMEN |
|
ORAL AGENTS – 2nd line
NAME |
ETHIONAMIDE (Bacteriostatic) |
DOSE/KG |
15-20 mg/kg/day |
USUAL DOSE |
1000 mg dly (Split dose 250 mg mane, 750 mg nocte to minimize nausea) |
MAXIMUM DOSE |
1000 mg dly |
CAUTION |
Hepatic disease, previous hypersensitivity to Ethionamide or porphyria. Use with caution in diabetes, alcoholics, psychiatric illness, depression, hypothyroidism and epilepsy |
COMMON SIDE EFFECTS |
GI side effects, CNS toxicity, Hepatotoxicity |
PAEDIATRIC DOSE |
10 mg/kg/day |
RENAL DOSE |
GFR <30 ml/min or on dialysis – Decrease dose by 50% |
LIVER IMPAIRMENT DOSE |
N/A |
PREGNANCY |
Category C. Teratogenic in animals. Avoid |
LACTATION |
Safety not established |
BUILDING A REGIMEN |
|
NAME |
CYCLOSERINE (AND TERIZIDONE – a derivative of Cycloserine) (Bacteriostatic) |
DOSE/KG |
10-20 mg/kg/day. + Pyridoxine to prevent CNS Side effects |
USUAL DOSE |
500-750 mg dly or 250-500 mg bd |
MAXIMUM DOSE |
1000 mg dly |
CAUTION |
Contraindicated in psychiatric conditions, epilepsy, severe renal impairment, alcohol abuse and porphyria. Caution in elderly and those with renal impairment |
COMMON SIDE EFFECTS |
CNS toxicity (more common with Cycloserine), skin rash |
PAEDIATRIC DOSE |
10 mg/kg/day |
RENAL DOSE |
Extend dose interval and adjust by monitoring drug levels (Target – 20-30micromg/ml) GFR 10-50 ml/min – Extend dosing interval to 24 hrs GFR <10 ml/min – Extend dosing interval to 36-48 hrs |
LIVER IMPAIRMENT DOSE |
N/A |
PREGNANCY |
Use only if no alternatives |
LACTATION |
Give infant Pyridoxine |
BUILDING A REGIMEN |
Does not share cross-resistance with other anti-TB drugs |
NAME |
PARA-AMINO SALICYLIC ACID (PAS) |
DOSE/KG |
150 mg/kg/day or 10-12 g/day in 2 divided doses |
USUAL DOSE |
5 g bd |
MAXIMUM DOSE |
12 g/day |
CAUTION |
Allergy to aspirin or PAS. Avoid in advance renal impairment |
COMMON SIDE EFFECTS |
Anorexia, diarrhoea, hypothyroidism. Low risk of hepatitis |
PAEDIATRIC DOSE |
150 mg/kg/day in 2 or 3 divided doses |
RENAL DOSE |
Avoid |
LIVER IMPAIRMENT DOSE |
N/A |
PREGNANCY |
Avoid |
LACTATION |
Concentrations excreted in breast milk are low |
BUILDING A REGIMEN |
|
FLUOROQUINOLONES – 2nd line
NAME |
LEVOFLOXACIN (Bactericidal) |
DOSE/KG |
- |
USUAL DOSE |
750 mg dly |
MAXIMUM DOSE |
750 mg dly |
CAUTION |
As for Ciprofloxacin |
COMMON SIDE EFFECTS |
As for Ciprofloxacin. |
PAEDIATRIC DOSE |
7.5-10 mg/kg/day (Max 750 mg) |
RENAL DOSE |
GFR <30 ml/min – 750-1000mg 3 times/week |
LIVER IMPAIRMENT DOSE |
N/A |
PREGNANCY |
Avoid |
LACTATION |
Avoid |
BUILDING A REGIMEN |
|
NAME |
OFLOXACIN (Bactericidal) |
DOSE/KG |
- |
USUAL DOSE |
800 mg dly or 400 mg bd |
MAXIMUM DOSE |
800 mg dly |
CAUTION |
Avoid in patients with prolonged QT interval. Previous hypersensitivity to fluoroquinolones. Caution in patients with CNS disorders, hepatic or renal involvement and in children |
COMMON SIDE EFFECTS |
GI side effects, Headaches, dizziness, drowsiness, insomnia, arthralgia. Hypersensitivity |
PAEDIATRIC DOSE |
15-20 mg/kg/day |
RENAL DOSE |
GFR <30 ml/min – 800 mg 3 times/week |
LIVER IMPAIRMENT DOSE |
N/A |
PREGNANCY |
Avoid |
LACTATION |
Avoid |
BUILDING A REGIMEN |
|
NAME |
CIPROFLOXACIN (Bactericidal) |
DOSE/KG |
- |
USUAL DOSE |
500-750 mg bd (Doses at higher range preferred in TB) |
MAXIMUM DOSE |
750 mg bd |
CAUTION |
Avoid in patients with prolonged QT interval. Previous hypersensitivity to fluoroquinolones. Caution in patients with CNS disorders, hepatic or renal involvement and in children |
COMMON SIDE EFFECTS |
GI side effects, Headaches, dizziness, drowsiness, insomnia, arthralgia. Hypersensitivity |
PAEDIATRIC DOSE |
20-30 mg/kg/day in 2 divided doses |
RENAL DOSE |
GFR <30 ml/min – 1000-1500 mg 3 times/week |
LIVER IMPAIRMENT DOSE |
N/A |
PREGNANCY |
Avoid |
LACTATION |
Avoid |
BUILDING A REGIMEN |
|
NAME |
MOXIFLOXACIN (Bactericidal) |
DOSE/KG |
- |
USUAL DOSE |
400 mg dly |
MAXIMUM DOSE |
400 mg dly |
CAUTION |
As for Ciprofloxacin |
COMMON SIDE EFFECTS |
As for Ciprofloxacin |
PAEDIATRIC DOSE |
7.5-10 mg/kg/day (Max 400 mg) |
RENAL DOSE |
No dose adjustment |
LIVER IMPAIRMENT DOSE |
N/A |
PREGNANCY |
Avoid |
LACTATION |
Avoid |
BUILDING A REGIMEN |
|
INJECTABLE AGENTS
NAME |
STREPTOMYCIN (Bactericidal) |
DOSE/KG |
15-20 mg/kg/day IMI |
USUAL DOSE |
750 mg dly IMI |
MAXIMUM DOSE |
1000 mg dly IMI |
CAUTION |
Patients with renal failure, impaired hearing or vestibular defects, previous hypersensitivity to Streptomycin. Contraindicated in myasthenia gravis |
COMMON SIDE EFFECTS |
Ototoxicity, renal toxicity, hypersensitivity, skin rash |
PAEDIATRIC DOSE |
20-40 mg/kg/day |
RENAL DOSE |
GFR 10-50 ml/min – 15 mg/kg every 24-72 hours GFR <10 ml/min – 15 mg/kg every 72-96 hours |
LIVER IMPAIRMENT DOSE |
N/A |
PREGNANCY |
Can cause ototoxicity in foetus – avoid |
LACTATION |
No known adverse effects |
BUILDING A REGIMEN |
|
NAME |
KANAMYCIN (Bactericidal) |
DOSE/KG |
15 mg/kg/day IMI |
USUAL DOSE |
750-1000 mg dly IMI |
MAXIMUM DOSE |
1500 mg dly IMI |
CAUTION |
Patients with renal failure, impaired hearing or vestibular defects, previous hypersensitivity to Kanamycin. Contraindicated in myasthenia gravis |
COMMON SIDE EFFECTS |
Ototoxicity, renal toxicity, hypersensitivity, skin rash |
PAEDIATRIC DOSE |
15-30 mg/kg/day |
RENAL DOSE |
GFR <30 ml/min – 12-15 mg/kg 2-3 times/week |
LIVER IMPAIRMENT DOSE |
N/A |
PREGNANCY |
Avoid |
LACTATION |
No known adverse effects |
BUILDING A REGIMEN |
Vs Amikacin - As effective, less well tolerated, cheaper Vs Streptomycin - Streptomycin-resistant strains usually susceptible to Kanamycin and Amikacin |
NAME |
AMIKACIN (Bactericidal) |
DOSE/KG |
15-20 mg/kg/day IMI |
USUAL DOSE |
750-1000 mg dly IMI |
MAXIMUM DOSE |
1500 mg dly IMI |
CAUTION |
Patients with renal failure, impaired hearing or vestibular defects, previous hypersensitivity to Amikacin. Contraindicated in myasthenia gravis. Caution in neonates |
COMMON SIDE EFFECTS |
Ototoxicity, renal toxicity, peripheral neuropathy, hypersensitivity, skin rash |
TARGET DRUG LEVELS |
Peak > 30 mg/L; trough < 1 mg/L |
PAEDIATRIC DOSE |
<10 years – 25 mg/kg dly on first day; then 18 mg/kg dly >10 years – 20 mg/kg dly on first day; then 15 mg/kg dly |
RENAL DOSE |
GFR <60 ml/min – Loading dose 10 mg/kg with further doses guided by drug levels |
LIVER IMPAIRMENT DOSE |
N/A |
PREGNANCY |
Avoid |
LACTATION |
No known adverse effects |
BUILDING A REGIMEN |
Vs Kanamycin – As effective, better tolerated, more expensive Vs Streptomycin - Streptomycin-resistant strains usually susceptible to Kanamycin and Amikacin |
Resources:
Schaaf H, Zumla AI et al. Tuberculosis: A Comprehensive Clinical Reference. Elsevier 2009.
South African Medicines Formulary. Produced by the Division of Clinical Pharmacology, University of Cape Town.