Sustiva
- Generic Name: efavirenz
- Brand Name: Sustiva
- Drug Class: HIV, NNRTIs
Sustiva (Efavirenz) side effects drug center
Sustiva Side Effects Center
What Is Sustiva?
Sustiva (efavirenz) is an antiviral medication used to treat HIV, which causes the acquired immunodeficiency syndrome (AIDS). Sustiva is not a cure for HIV or AIDS.
What Are Side Effects for Sustiva?
Common side effects of Sustiva include:
- dizziness,
- trouble sleeping (insomnia),
- drowsiness,
- unusual dreams,
- trouble concentrating,
- nausea,
- vomiting,
- stomach pain,
- diarrhea,
- constipation,
- cough,
- blurred vision,
- headache,
- tired feeling,
- spinning sensation,
- problems with balance or coordination,
- muscle or joint pain, or
- changes in the shape or location of body fat (especially in your arms, legs, face, neck, breasts, and waist).
Many of these side effects may begin 1-2 days after starting Sustiva and usually go away in 2-4 weeks. Tell your doctor if you have rare but serious side effects of Sustiva including signs of liver problems such as:
- persistent nausea or vomiting,
- stomach or abdominal pain,
- severe tiredness,
- yellowing eyes or skin, or
- dark urine
Dosage for Sustiva
The recommended adult dosage of Sustiva is 600 mg orally, once daily, in combination with a protease inhibitor and/or nucleoside analogue reverse transcriptase inhibitors (NRTIs).
What Drugs, Substances, or Supplements Interact with Sustiva?
Sustiva may interact with:
- cyclosporine,
- itraconazole,
- sirolimus,
- tacrolimus,
- St. John's wort,
- voriconazole,
- blood thinners,
- cholesterol medications,
- antibiotics,
- heart or blood pressure medications,
- other HIV medicines, or
- seizure medications
Tell your doctor all medications you use.
Sustiva During Pregnancy and Breastfeeding
Sustiva is not recommended for use during pregnancy. It may harm a fetus, especially if taken during the first 3 months of pregnancy. Women of childbearing age should have a pregnancy test before starting this medication. Consult your doctor about using at least 2 forms of birth control (such as condoms with birth control pills) during treatment and for 3 months after the end of treatment. If you become pregnant or think you may be pregnant, tell your doctor immediately. It is unknown if Sustiva passes into breast milk. Because breast milk can transmit HIV, do not breastfeed.
Additional Information
Our Sustiva (efavirenz) Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication.
Sustiva Consumer Information
Get emergency medical help if you have signs of an allergic reaction (hives, difficult breathing, swelling in your face or throat) or a severe skin reaction (fever, sore throat, burning eyes, skin pain, red or purple skin rash with blistering and peeling).
Call your doctor at once if you have:
- a seizure;
- hallucinations, trouble concentrating, trouble speaking or moving (these symptoms may occur months or years after you start taking efavirenz);
- nervous system problems--dizziness, drowsiness, confusion, trouble concentrating, strange dreams, insomnia, or problems with speech, balance, or muscle movement;
- serious psychiatric symptoms--anxiety, paranoia, unusual behavior, feeling sad or hopeless, hallucinations, suicidal thoughts; or
- liver problems--nausea, stomach pain, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes);
Psychiatric symptoms or nervous system problems may happen even months or years after you have been taking efavirenz.
Efavirenz affects your immune system, which may cause certain side effects (even weeks or months after you've taken this medicine). Tell your doctor if you have:
- signs of a new infection--fever, night sweats, swollen glands, cold sores, cough, wheezing, diarrhea, weight loss;
- trouble speaking or swallowing, problems with balance or eye movement, weakness or prickly feeling; or
- swelling in your neck or throat (enlarged thyroid), menstrual changes, impotence.
Common side effects may include:
- nausea, vomiting;
- dizziness, drowsiness, trouble concentrating;
- rash;
- headache, tired feeling;
- sleep problems (insomnia), strange dreams; or
- changes in the shape or location of body fat (especially in your arms, legs, face, neck, breasts, and waist).
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Read the entire detailed patient monograph for Sustiva (Efavirenz)
Sustiva Professional Information
SIDE EFFECTS
The most significant adverse reactions observed in patients treated with SUSTIVA are:
- psychiatric symptoms [see WARNINGS AND PRECAUTIONS],
- nervous system symptoms [see WARNINGS AND PRECAUTIONS],
- rash [see WARNINGS AND PRECAUTIONS].
- hepatotoxicity [see WARNINGS AND PRECAUTIONS]
Clinical Trials Experience
Because clinical studies are conducted under widely varying conditions, the adverse reaction rates reported cannot be directly compared to rates in other clinical studies and may not reflect the rates observed in clinical practice.
Adverse Reactions In Adults
The most common (>5% in either efavirenz treatment group) adverse reactions of at least moderate severity among patients in Study 006 treated with SUSTIVA in combination with zidovudine/lamivudine or indinavir were rash, dizziness, nausea, headache, fatigue, insomnia, and vomiting.
Selected clinical adverse reactions of moderate or severe intensity observed in ≥2% of SUSTIVA-treated patients in two controlled clinical trials are presented in Table 2.
Table 2: Selected Treatment-Emergenta Adverse Reactions of Moderate or Severe Intensity Reported in ≥2% of SUSTIVATreated Patients in Studies 006 and ACTG 364
| Adverse Reactions | Study 006 LAM-, NNRTI-, and Protease Inhibitor-Naive Patients |
Study ACTG 364 NRTI-experienced, NNRTI-, and Protease Inhibitor-Naive Patients |
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| SUSTIVAb + ZDV/LAM (n=412) 180 weeksc |
SUSTIVAb + Indinavir (n=415) 102 weeksc |
Indinavir + ZDV/LAM (n=401) 76 weeksc |
SUSTIVAb + Nelfinavir + NRTIs (n=64) 71.1 weeksc |
SUSTIVAb + NRTIs (n=65) 70.9 weeksc |
Nelfinavir + NRTIs (n=66) 62.7 weeksc |
|
| Body as a Whole | ||||||
| Fatigue | 8% | 5% | 9% | 0 | 2% | 3% |
| Pain | 1% | 2% | 8% | 13% | 6% | 17% |
| Central and Peripheral Nervous System | ||||||
| Dizziness | 9% | 9% | 2% | 2% | 6% | 6% |
| Headache | 8% | 5% | 3% | 5% | 2% | 3% |
| Insomnia | 7% | 7% | 2% | 0 | 0 | 2% |
| Concentration impaired | 5% | 3% | <1% | 0 | 0 | 0 |
| Abnormal dreams | 3% | 1% | 0 | — | — | — |
| Somnolence | 2% | 2% | <1% | 0 | 0 | 0 |
| Anorexia | 1% | <1% | <1% | 0 | 2% | 2% |
| Gastrointestinal | ||||||
| Nausea | 10% | 6% | 24% | 3% | 2% | 2% |
| Vomiting | 6% | 3% | 14% | — | — | — |
| Diarrhea | 3% | 5% | 6% | 14% | 3% | 9% |
| Dyspepsia | 4% | 4% | 6% | 0 | 0 | 2% |
| Abdominal pain | 2% | 2% | 5% | 3% | 3% | 3% |
| Psychiatric | ||||||
| Anxiety | 2% | 4% | <1% | — | — | — |
| Depression | 5% | 4% | <1% | 3% | 0 | 5% |
| Nervousness | 2% | 2% | 0 | 2% | 0 | 2% |
| Skin & Appendages | ||||||
| Rashd | 11% | 16% | 5% | 9% | 5% | 9% |
| Pruritus | <1% | 1% | 1% | 9% | 5% | 9% |
| a Includes adverse events at least possibly related to study drug or of unknown relationship for Study 006. Includes all adverse events regardless of relationship to study drug for Study ACTG 364. b SUSTIVA provided as 600 mg once daily. c Median duration of treatment. d Includes erythema multiforme, rash, rash erythematous, rash follicular, rash maculopapular, rash petechial, rash pustular, and urticaria for Study 006 and macules, papules, rash, erythema, redness, inflammation, allergic rash, urticaria, welts, hives, itchy, and pruritus for ACTG 364. — = Not Specified. ZDV = zidovudine, LAM = lamivudine. |
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Pancreatitis has been reported, although a causal relationship with efavirenz has not been established. Asymptomatic increases in serum amylase levels were observed in a significantly higher number of patients treated with efavirenz 600 mg than in control patients (see Laboratory Abnormalities).
Nervous System Symptoms
For 1008 patients treated with regimens containing SUSTIVA and 635 patients treated with a control regimen in controlled trials, Table 3 lists the frequency of symptoms of different degrees of severity and gives the discontinuation rates for one or more of the following nervous system symptoms: dizziness, insomnia, impaired concentration, somnolence, abnormal dreaming, euphoria, confusion, agitation, amnesia, hallucinations, stupor, abnormal thinking, and depersonalization [see WARNINGS AND PRECAUTIONS]. The frequencies of specific central and peripheral nervous system symptoms are provided in Table 2.
Table 3: Percent of Patients with One or More Selected Nervous System Symptomsa,b
| Percent of Patients with: | SUSTIVA 600 mg Once Daily (n=1008) % |
Control Groups (n=635) % |
| Symptoms of any severity | 52.7 | 24.6 |
| Mild symptomsc | 33.3 | 15.6 |
| Moderate symptomsd | 17.4 | 7.7 |
| Severe symptomse | 2.0 | 1.3 |
| Treatment discontinuation as a result of symptoms | 2.1 |
1.1 |
| a Includes events reported regardless of causality. b Data from Study 006 and three Phase 2/3 studies. c “Mild” = Symptoms which do not interfere with patient’s daily activities. d “Moderate” = Symptoms which may interfere with daily activities. e “Severe” = Events which interrupt patient’s usual daily activities. |
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Psychiatric Symptoms
Serious psychiatric adverse experiences have been reported in patients treated with SUSTIVA. In controlled trials, psychiatric symptoms observed at a frequency greater than 2% among patients treated with SUSTIVA or control regimens, respectively, were depression (19%, 16%), anxiety (13%, 9%), and nervousness (7%, 2%).
Rash
In controlled clinical trials, the frequency of rash (all grades, regardless of causality) was 26% for 1008 adults treated with regimens containing SUSTIVA and 17% for 635 adults treated with a control regimen. Most reports of rash were mild or moderate in severity. The frequency of Grade 3 rash was 0.8% for SUSTIVA-treated patients and 0.3% for control groups, and the frequency of Grade 4 rash was 0.1% for SUSTIVA and 0 for control groups. The discontinuation rates as a result of rash were 1.7% for SUSTIVA-treated patients and 0.3% for control groups [see WARNINGS AND PRECAUTIONS].
Experience with SUSTIVA in patients who discontinued other antiretroviral agents of the NNRTI class is limited. Nineteen patients who discontinued nevirapine because of rash have been treated with SUSTIVA. Nine of these patients developed mild-to-moderate rash while receiving therapy with SUSTIVA, and two of these patients discontinued because of rash.
Laboratory Abnormalities
Selected Grade 3-4 laboratory abnormalities reported in ≥2% of SUSTIVA-treated patients in two clinical trials are presented in Table 4.
Table 4: Selected Grade 3-4 Laboratory Abnormalities Reported in ≥2% of SUSTIVA-Treated Patients in Studies 006 and ACTG 364
| Study 006 LAM-, NNRTI-, and Protease Inhibitor-Naive Patients |
Study ACTG 364 NRTI-experienced, NNRTI-, and Protease Inhibitor-Naive Patients |
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| Variable | Limit | SUSTIVAa + ZDV/LAM (n=412) 180 weeksb |
SUSTIVAa + Indinavir (n=415) 102 weeksb |
Indinavir + ZDV/LAM (n=401) 76 weeksb |
SUSTIVAa + Nelfinavir + NRTIs (n=64) 71.1 weeksb |
SUSTIVAa + NRTIs (n=65) 70.9 weeksb |
Nelfinavir + NRTIs (n=66) 62.7 weeksb |
| Chemistry | |||||||
| ALT | >5 × ULN | 5% | 8% | 5% | 2% | 6% | 3% |
| AST | >5 × ULN | 5% | 6% | 5% | 6% | 8% | 8% |
| GGTc | >5 × ULN | 8% | 7% | 3% | 5% | 0 | 5% |
| Amylase | >2 × ULN | 4% | 4% | 1% | 0 | 6% | 2% |
| Glucose | >250 mg/dL | 3% | 3% | 3% | 5% | 2% | 3% |
| Triglyceridesd | ≥751 mg/dL | 9% | 6% | 6% | 11% | 8% | 17% |
| Hematology Neutrophils |
<750/mm3 | 10% | 3% | 5% | 2% | 3% | 2% |
| a SUSTIVA provided as 600 mg once daily. b Median duration of treatment. c Isolated elevations of GGT in patients receiving SUSTIVA may reflect enzyme induction not associated with liver toxicity. d Nonfasting. ZDV = zidovudine, LAM = lamivudine, ULN = upper limit of normal, ALT = alanine aminotransferase, AST = aspartate aminotransferase, GGT = gamma-glutamyltransferase. |
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Patients Coinfected with Hepatitis B or C
Liver function tests should be monitored in patients with a history of hepatitis B and/or C. In the long-term data set from Study 006, 137 patients treated with SUSTIVA-containing regimens (median duration of therapy, 68 weeks) and 84 treated with a control regimen (median duration, 56 weeks) were seropositive at screening for hepatitis B (surface antigen positive) and/or C (hepatitis C antibody positive). Among these coinfected patients, elevations in AST to greater than five times ULN developed in 13% of patients in the SUSTIVA arms and 7% of those in the control arm, and elevations in ALT to greater than five times ULN developed in 20% of patients in the SUSTIVA arms and 7% of patients in the control arm. Among coinfected patients, 3% of those treated with SUSTIVA-containing regimens and 2% in the control arm discontinued from the study because of liver or biliary system disorders [see WARNINGS AND PRECAUTIONS].
Lipids
Increases from baseline in total cholesterol of 10-20% have been observed in some uninfected volunteers receiving SUSTIVA. In patients treated with SUSTIVA + zidovudine + lamivudine, increases from baseline in nonfasting total cholesterol and HDL of approximately 20% and 25%, respectively, were observed. In patients treated with SUSTIVA + indinavir, increases from baseline in nonfasting cholesterol and HDL of approximately 40% and 35%, respectively, were observed. Nonfasting total cholesterol levels ≥240 mg/dL and ≥300 mg/dL were reported in 34% and 9%, respectively, of patients treated with SUSTIVA + zidovudine + lamivudine; 54% and 20%, respectively, of patients treated with SUSTIVA + indinavir; and 28% and 4%, respectively, of patients treated with indinavir + zidovudine + lamivudine. The effects of SUSTIVA on triglycerides and LDL in this study were not well characterized since samples were taken from nonfasting patients. The clinical significance of these findings is unknown [see WARNINGS AND PRECAUTIONS].
Adverse Reactions In Pediatric Patients
Because clinical studies are conducted under widely varying conditions, the adverse reaction rates reported cannot be directly compared to rates in other clinical studies and may not reflect the rates observed in clinical practice.
Assessment of adverse reactions is based on three clinical trials in 182 HIV-1 infected pediatric patients (3 months to 21 years of age) who received SUSTIVA in combination with other antiretroviral agents for a median of 123 weeks. The adverse reactions observed in the three trials were similar to those observed in clinical trials in adults except that rash was more common in pediatric patients (32% for all grades regardless of causality) and more often of higher grade (ie, more severe). Two (1.1%) pediatric patients experienced Grade 3 rash (confluent rash with fever, generalized rash), and four (2.2%) pediatric patients had Grade 4 rash (all erythema multiforme). Five pediatric patients (2.7%) discontinued from the study because of rash [see WARNINGS AND PRECAUTIONS].
Postmarketing Experience
The following adverse reactions have been identified during postapproval use of SUSTIVA. Because these reactions are reported voluntarily from a population of unknown size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
Body as a Whole: allergic reactions, asthenia, redistribution/accumulation of body fat [see WARNINGS AND PRECAUTIONS]
Central and Peripheral Nervous System: abnormal coordination, ataxia, encephalopathy, cerebellar coordination and balance disturbances, convulsions, hypoesthesia, paresthesia, neuropathy, tremor, vertigo
Endocrine: gynecomastia
Gastrointestinal: constipation, malabsorption
Cardiovascular: flushing, palpitations
Liver and Biliary System: hepatic enzyme increase, hepatic failure, hepatitis.
Metabolic and Nutritional: hypercholesterolemia, hypertriglyceridemia
Musculoskeletal: arthralgia, myalgia, myopathy
Psychiatric: aggressive reactions, agitation, delusions, emotional lability, mania, neurosis, paranoia, psychosis, suicide, catatonia
Respiratory: dyspnea
Skin and Appendages: erythema multiforme, photoallergic dermatitis, Stevens-Johnson syndrome
Special Senses: abnormal vision, tinnitus
DRUG INTERACTIONS
Potential For SUSTIVA To Affect Other Drugs
Efavirenz has been shown in vivo to induce CYP3A and CYP2B6. Other compounds that are substrates of CYP3A or CYP2B6 may have decreased plasma concentrations when coadministered with SUSTIVA.
Potential For Other Drugs To Affect SUSTIVA
Drugs that induce CYP3A activity (eg, phenobarbital, rifampin, rifabutin) would be expected to increase the clearance of efavirenz resulting in lowered plasma concentrations [see DOSAGE AND ADMINISTRATION].
QT Prolonging Drugs
There is limited information available on the potential for a pharmacodynamic interaction between SUSTIVA and drugs that prolong the QTc interval. QTc prolongation has been observed with the use of efavirenz [see CLINICAL PHARMACOLOGY]. Consider alternatives to SUSTIVA when coadministered with a drug with a known risk of Torsade de Pointes.
Established And Other Potentially Significant Drug Interactions
Drug interactions with SUSTIVA are summarized in Table 5. For pharmacokinetics data, [see CLINICAL PHARMACOLOGY] Tables 7 and 8. This table includes potentially significant interactions, but is not all inclusive.
Table 5: Established and Other Potentially Significant Drug Interactions: Alteration in Dose or Regimen May Be Recommended Based on Drug Interaction Studies or Predicted Interaction
| Concomitant Drug Class: Drug Name | Effect | Clinical Comment |
| HIV antiviral agents | ||
| Protease inhibitor: Fosamprenavir Calcium |
↓ amprenavir | Fosamprenavir (unboosted): Appropriate doses of the combinations with respect to safety and efficacy have not been established. Fosamprenavir/ritonavir: An additional 100 mg/day (300 mg total) of ritonavir is recommended when SUSTIVA is administered with fosamprenavir/ ritonavir once daily. No change in the ritonavir dose is required when SUSTIVA is administered with fosamprenavir plus ritonavir twice daily. |
| Protease inhibitor: Atazanavir |
↓ atazanavir* | Treatment-naive patients: When coadministered with SUSTIVA, the recommended dose of atazanavir is 400 mg with ritonavir 100 mg (together once daily with food) and SUSTIVA 600 mg (once daily on an empty stomach, preferably at bedtime). Treatment-experienced patients: Coadministration of SUSTIVA and atazanavir is not recommended. |
| Protease inhibitor: Indinavir |
↓ indinavir* | The optimal dose of indinavir, when given in combination with SUSTIVA, is not known. Increasing the indinavir dose to 1000 mg every 8 hours does not compensate for the increased indinavir metabolism due to SUSTIVA. |
| Protease inhibitor: Lopinavir/ritonavir | ↓ lopinavir* | Lopinavir/ritonavir once daily dosing is not recommended when coadministered with SUSTIVA. The dose of lopinavir/ritonavir must be increased when coadministered with SUSTIVA. See the lopinavir/ritonavir prescribing information for dose adjustments of lopinavir/ritonavir when coadministered with efavirenz in adult and pediatric patients. |
| Protease inhibitor: Ritonavir |
↑ ritonavir* ↑ efavirenz* |
Monitor for elevation of liver enzymes and for adverse clinical experiences (e.g., dizziness, nausea, paresthesia) when SUSTIVA is coadministered with ritonavir. |
| Protease inhibitor: Saquinavir |
↓ saquinavir* | Appropriate doses of the combination of SUSTIVA and saquinavir/ritonavir with respect to safety and efficacy have not been established. |
| NNRTI: Other NNRTIs |
↑ or ↓ efavirenz and/or NNRTI | Combining two NNRTIs has not been shown to be beneficial. SUSTIVA should not be coadministered with other NNRTIs. |
| CCR5 co-receptor antagonist: Maraviroc | ↓ maraviroc* | Refer to the full prescribing information for maraviroc for guidance on coadministration with efavirenz. |
| Hepatitis C antiviral agents | ||
| Boceprevir | ↓ boceprevir* | Concomitant administration of boceprevir with SUSTIVA is not recommended because it may result in loss of therapeutic effect of boceprevir. |
| Elbasvir/Grazoprevir | ↓ elbasvir ↓ grazoprevir |
Coadministration of SUSTIVA with elbasvir/grazoprevir is contraindicated [see CONTRAINDICATIONS] because it may lead to loss of virologic response to elbasvir/grazoprevir. |
| Pibrentasvir/Glecaprevir | ↓ pibrentasvir ↓ glecaprevir |
Coadministration of SUSTIVA is not recommended because it may lead to reduced therapeutic effect of pibrentasvir/glecaprevir. |
| Simeprevir | ↓ simeprevir* ↔ efavirenz* |
Concomitant administration of simeprevir with SUSTIVA is not recommended because it may result in loss of therapeutic effect of simeprevir. |
| Velpatasvir/ Sofosbuvir | ↓ velpatasvir | Coadministration of SUSTIVA and sofosbuvir/velpatasvir is not recommended because it may result in loss of therapeutic effect of sofosbuvir/velpatasvir. |
| Velpatasvir /Sofosbuvir/ /Voxilaprevir | ↓ velpatasvir ↓ voxilaprevir |
Coadministration of SUSTIVA and sofosbuvir/velpatasvir/voxilaprevir is not recommended because it may result in loss of therapeutic effect of sofosbuvir/velpatasvir/voxilaprevir. |
| Other agents | ||
| Anticoagulant: Warfarin |
↑ or ↓ warfarin | Monitor INR and adjust warfarin dosage if necessary. |
| Anticonvulsants: Carbamazepine | ↓ carbamazepine* ↓ efavirenz* | There are insufficient data to make a dose recommendation for efavirenz. Alternative anticonvulsant treatment should be used. |
| Phenytoin Phenobarbital | ↓ anticonvulsant ↓ efavirenz |
Potential for reduction in anticonvulsant and/or efavirenz plasma levels; periodic monitoring of anticonvulsant plasma levels should be conducted. |
| Antidepressants: Bupropion |
↓ bupropion* | Increases in bupropion dosage should be guided by clinical response. Bupropion dose should not exceed the maximum recommended dose. |
| Sertraline | ↓ sertraline* | Increases in sertraline dosage should be guided by clinical response. |
| Antifungals: Voriconazole |
↓ voriconazole* ↑ efavirenz* |
SUSTIVA and voriconazole should not be coadministered at standard doses. When voriconazole is coadministered with SUSTIVA, voriconazole maintenance dose should be increased to 400 mg every 12 hours and SUSTIVA dose should be decreased to 300 mg once daily using the capsule formulation. SUSTIVA tablets must not be broken. [See DOSAGE AND ADMINISTRATION and CLINICAL PHARMACOLOGY.] |
| Itraconazole | ↓ itraconazole* ↓ hydroxyitraconazole* |
Consider alternative antifungal treatment because no dose recommendation for itraconazole can be made. |
| Ketoconazole | ↓ ketoconazole | Consider alternative antifungal treatment because no dose recommendation for ketoconazole can be made. |
| Posaconazole | ↓ posaconazole* | Avoid concomitant use unless the benefit outweighs the risks. |
| Anti-infective: Clarithromycin |
↓ clarithromycin* ↑ 14-OH metabolite* |
Consider alternatives to macrolide antibiotics because of the risk of QT interval prolongation. |
| Antimycobacterials: Rifabutin |
↓ rifabutin* | Increase daily dose of rifabutin by 50%. Consider doubling the rifabutin dose in regimens where rifabutin is given 2 or 3 times a week. |
| Rifampin | ↓ efavirenz* | Increase SUSTIVA to 800 mg once daily when coadministered with rifampin to patients weighing 50 kg or more. |
| Antimalarials: Artemether/lumefantrine | ↓ artemether* ↓ dihydroartemisinin* ↓ lumefantrine* |
Consider alternatives to artemether/ lumefantrine because of the risk of QT interval prolongation. |
| Atovaquone/proguanil | ↓ atovaquone ↓ proguanil |
Concomitant administration is not recommended. |
| Calcium channel blockers: Diltiazem |
↓ diltiazem* ↓ desacetyl diltiazem* ↓ N-monodesmethyl diltiazem* |
Diltiazem dose adjustments should be guided by clinical response (refer to the full prescribing information for diltiazem). No dose adjustment of efavirenz is necessary when administered with diltiazem. |
| Others (eg, felodipine, nicardipine, nifedipine, verapamil) | ↓ calcium channel blocker | When coadministered with SUSTIVA, dosage adjustment of calcium channels blocker may be needed and should be guided by clinical response (refer to the full prescribing information for the calcium channel blocker). |
| HMG-CoA reductase inhibitors: Atorvastatin Pravastatin Simvastatin |
↓ atorvastatin* ↓ pravastatin* ↓ simvastatin* |
Plasma concentrations of atorvastatin, pravastatin, and simvastatin decreased. Consult the full prescribing information for the HMG-CoA reductase inhibitor for guidance on individualizing the dose. |
| Hormonal contraceptives: Oral Ethinyl estradiol/ Norgestimate |
↓ active metabolites of norgestimate* | A reliable method of barrier contraception should be used in addition to hormonal contraceptives. |
| Implant Etonogestrel | ↓ etonogestrel | A reliable method of barrier contraception should be used in addition to hormonal contraceptives. Decreased exposure of etonogestrel may be expected. There have been postmarketing reports of contraceptive failure with etonogestrel in efavirenz-exposed patients. |
| Immunosuppressants: Cyclosporine, tacrolimus, sirolimus, and others metabolized by CYP3A | ↓ immunosuppressant | Dose adjustments of the immunosuppressant may be required. Close monitoring of immunosuppressant concentrations for at least 2 weeks (until stable concentrations are reached) is recommended when starting or stopping treatment with efavirenz. |
| Narcotic analgesic: Methadone | ↓ methadone* | Monitor for signs of methadone withdrawal and increase methadone dose if required to alleviate withdrawal symptoms. |
| * The interaction between SUSTIVA and the drug was evaluated in a clinical study. All other drug interactions shown are predicted. This table is not all-inclusive. |
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Drugs Without Clinically Significant Interactions With SUSTIVA
No dosage adjustment is recommended when SUSTIVA is given with the following: aluminum/magnesium hydroxide antacids, azithromycin, cetirizine, famotidine, fluconazole, lorazepam, nelfinavir, nucleoside reverse transcriptase inhibitors (abacavir, emtricitabine, lamivudine, stavudine, tenofovir disoproxil fumarate, zidovudine), paroxetine, and raltegravir.
Cannabinoid Test Interaction
Efavirenz does not bind to cannabinoid receptors. False-positive urine cannabinoid test results have been reported with some screening assays in uninfected and HIV-infected subjects receiving efavirenz. Confirmation of positive screening tests for cannabinoids by a more specific method is recommended.
Read the entire FDA prescribing information for Sustiva (Efavirenz)
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