These highlights do not include all the information needed to use zidovudine safely and effectively. See full prescribing information for zidovudine tablets, USP. Zidovudine Tablets, USP Initial U.S. Approval: 1987 | Zidovudine
| Body Weight (kg) | Total Daily Dose | Dosage Regimen and Dose | |
|---|---|---|---|
| b.i.d. | t.i.d. | ||
| 4 to <9 |
24 mg/kg/day |
12 mg/kg |
8 mg/kg |
| ≥9 to <30 |
18 mg/kg/day |
9 mg/kg |
6 mg/kg |
| ≥30 |
600 mg/day |
300 mg |
200 mg |
| Adverse Reaction | Zidovudine 500 mg/day (n = 453) |
Placebo (n = 428) |
|---|---|---|
|
*Reported in ≥5% of study population. †Not statistically significant versus placebo. |
||
|
Body as a whole
|
||
| Asthenia |
9%†
|
6% |
| Headache |
63% |
53% |
| Malaise |
53% |
45% |
|
Gastrointestinal
|
||
| Anorexia |
20% |
11% |
| Constipation |
6%†
|
4% |
| Nausea |
51% |
30% |
| Vomiting |
17% |
10% |
| Test (Abnormal Level) |
Zidovudine 500 mg/day (n = 453) |
Placebo (n = 428) |
|---|---|---|
| ULN = Upper limit of normal. |
||
| Anemia (Hgb<8 g/dL) |
1% |
<1% |
| Granulocytopenia (<750 cells/mm3) |
2% |
2% |
| Thrombocytopenia (platelets<50,000/mm3) |
0% |
<1% |
| ALT (>5 x ULN) |
3% |
3% |
| AST (>5 x ULN) |
1% |
2% |
| Adverse Reaction | EPIVIR plus Zidovudine (n = 236) |
Didanosine (n = 235) |
|---|---|---|
|
*Includes pain, discharge, erythema, or swelling of an ear. |
||
|
Body as a whole
|
|
|
| Fever |
25% |
32% |
|
Digestive
|
|
|
| Hepatomegaly |
11% |
11% |
| Nausea & vomiting |
8% |
7% |
| Diarrhea |
8% |
6% |
| Stomatitis |
6% |
12% |
| Splenomegaly |
5% |
8% |
|
Respiratory
|
|
|
| Cough |
15% |
18% |
| Abnormal breath sounds/wheezing |
7% |
9% |
|
Ear, Nose, and Throat
|
|
|
| Signs or symptoms of ears*
|
7% |
6% |
| Nasal discharge or congestion |
8% |
11% |
|
Other
|
|
|
| Skin rashes |
12% |
14% |
| Lymphadenopathy |
9% |
11% |
| Test (Abnormal Level) | EPIVIR plus Zidovudine | Didanosine |
|---|---|---|
| ULN = Upper limit of normal. ANC = Absolute neutrophil count. |
||
| Neutropenia (ANC<400 cells/mm3) |
8% |
3% |
| Anemia (Hgb<7 g/dL) |
4% |
2% |
| Thrombocytopenia (platelets<50,000/mm3) |
1% |
3% |
| ALT (>10 x ULN) |
1% |
3% |
| AST (>10 x ULN) |
2% |
4% |
| Lipase (>2.5 x ULN) |
3% |
3% |
| Total amylase (>2.5 x ULN) |
3% |
3% |
| Parameter | Mean ± SD (except where noted) |
|---|---|
|
*Median [range]. †Approximate range. |
|
| Oral bioavailability (%) |
64 ± 10 (n = 5) |
| Apparent volume of distribution (L/kg) |
1.6 ± 0.6 (n = 8) |
| Plasma protein binding (%) |
<38 |
| CSF:plasma ratio*
|
0.6 [0.04 to 2.62] (n = 39) |
| Systemic clearance (L/hr/kg) |
1.6 ± 0.6 (n = 6) |
| Renal clearance (L/hr/kg) |
0.34 ± 0.05 (n = 9) |
| Elimination half-life (hr)†
|
0.5 to 3 (n = 19) |
| Parameter | Control Subjects (Normal Renal Function) (n = 6) |
Patients With Renal Impairment (n = 14) |
|---|---|---|
|
*Data are expressed as mean ± standard deviation. |
||
| CrCl (mL/min) |
120 ± 8 |
18 ± 2 |
| Zidovudine AUC (ng•hr/mL) |
1,400 ± 200 |
3,100 ± 300 |
| Zidovudine half-life (hr) |
1 ± 0.2 |
1.4 ± 0.1 |
| Parameter | Birth to 14 Days of Age | 14 Days to 3 Months of Age | 3 Months to 12 Years of Age |
|---|---|---|---|
|
*Data presented as mean ± standard deviation except where noted. †Median [range]. |
|||
| Oral bioavailability (%) |
89 ± 19 (n = 15) |
61 ± 19 (n = 17) |
65 ± 24 (n = 18) |
| CSF:plasma ratio |
no data |
no data |
0.68 [0.03 to 3.25] †
(n = 38) |
| CL (L/hr/kg) |
0.65 ± 0.29 (n = 18) |
1.14 ± 0.24 (n = 16) |
1.85 ± 0.47 (n = 20) |
| Elimination half-life (hr) |
3.1 ± 1.2 (n = 21) |
1.9 ± 0.7 (n = 18) |
1.5 ± 0.7 (n = 21) |
| Note: ROUTINE DOSE MODIFICATION OF ZIDOVUDINE IS NOT WARRANTED WITH COADMINISTRATION OF THE FOLLOWING DRUGS. | |||||
|---|---|---|---|---|---|
| Coadministered Drug and Dose |
Zidovudine Dose |
n | Zidovudine Concentrations |
Concentration of Coadministered Drug |
|
| AUC | Variability | ||||
| ↑= Increase; ↓= Decrease; ↔= no significant change; AUC = area under the concentration versus time curve; CI = confidence interval. * This table is not all inclusive. † Estimated range of percent difference. |
|||||
| Atovaquone 750 mg q 12 hr with food |
200 mg q 8 hr |
14 |
↑AUC 31% |
Range 23% to 78%† |
↔ |
| Clarithromycin 500 mg twice daily |
100 mg q 4 hr x 7 days |
4 |
↓AUC 12% |
Range ↓34% to ↑14% |
Not Reported |
| Fluconazole 400 mg daily |
200 mg q 8 hr |
12 |
↑AUC 74% |
95% CI: 54% to 98% |
Not Reported |
| Lamivudine 300 mg q 12 hr |
single 200 mg |
12 |
↑AUC 13% |
90% CI: 2% to 27% |
↔ |
| Methadone 30 to 90 mg daily |
200 mg q 4 hr |
9 |
↑AUC 43% |
Range 16% to 64%† |
↔ |
| Nelfinavir 750 mg q 8 hr x 7 to 10 days |
single 200 mg |
11 |
↓AUC 35% |
Range 28% to 41% |
↔ |
| Probenecid 500 mg q 6 hr x 2 days |
2 mg/kg q 8 hr x 3 days |
3 |
↑AUC 106% |
Range 100% to 170%† |
Not Assessed |
| Rifampin 600 mg daily x 14 days |
200 mg q 8 hr x 14 days |
8 |
↓AUC 47% |
90% CI: 41% to 53% |
Not Assessed |
| Ritonavir 300 mg q 6 hr x 4 days |
200 mg q 8 hr x 4 days |
9 |
↓AUC 25% |
95% CI: 15% to 34% |
↔ |
| Valproic acid 250 mg or 500 mg q 8 hr x 4 days |
100 mg q 8 hr x 4 days |
6 |
↑AUC 80% |
Range 64% to 130%† |
Not Assessed |
| Endpoint | EPIVIR plus Zidovudine (n = 236) |
Didanosine (n = 235) |
|---|---|---|
| HIV disease progression or death (total) |
15 (6.4%) |
37 (15.7%) |
| Physical growth failure |
7 (3%) |
6 (2.6%) |
| Central nervous system deterioration |
4 (1.7%) |
12 (5.1%) |
| CDC Clinical Category C |
2 (0.8%) |
8 (3.4%) |
| Death |
2 (0.8%) |
11 (4.7%) |
Manufacturer
Greenstone LLC
Active Ingredients
Source
- U.S. National Library of Medicine
- DailyMed
- Last Updated: 18 May 2013
Drugs and Medications
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Clinical Trials
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Bioequivalency Study of Zidovudine Under Fed Conditions
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PubMed Articles
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Abstract The evolution of hematological parameters in HIV-1-exposed uninfected infants according to various durations of perinatal zidovudine exposure was studied. We used data prospectively collected...
Background: Advent of the HIV/AIDS pandemic has led to a dramatic increase in the number of TB cases worldwide. Availability of highly active antiretroviral therapy (HAART) has significantly improved...
OBJECTIVES: Oral complications associated with HIV infection and with the antiretroviral drugs used to treat it are of increasing concern in HIV-infected patients. Protease inhibitors have been shown...
A new fluorescence-based detection method was developed to visualize zidovudine-incorporated DNA using click chemistry. This bio-orthogonal detection method was used to quantify the relative susceptib...
