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Coformulations of Antiretroviral Therapy |
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Effectiveness, Tolerability, Adherence, Simplicity |
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The Leading Edge of HIV Treatment |
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Atripla A combination of emtricitabine + efavirenz + tenofovir Approved 7/12/2006 |
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| Forms Available | 300 mg tenofovir / 200 mg emtricitabine / 600 mg efavirenz in tablet form | ||
| Dosing |
1 tablet once a day without food Dosing at bedtime may improve tolerability to the efavirenz component. |
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| Renal dosing |
Dosing interval Ccr 30-49 cc/min |
Dosing interval Ccr < 30 cc/min |
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| Not recommended | Not recommended | ||
| Hepatic dosing: no data available | |||
| Food dependence |
Food increases
efavirenz absorption and
therefore may produce increased CNS side effects. Take Atripla on an empty stomach. |
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| Adverse Effects |
Same as
tenofovir and
emtricitabine
and
efavirenz
(see above or click on the drug name) Efavirenz may cause CNS stimulation, restlessness, nightmares, depression, exacerbation of underlying mental health problems, rash or chemical hepatitis. Tenofovir may cause nephropathy, Fanconi-like syndrome, or loss of bone mineralization. Emtricitabine rarely causes discoloration of palms or soles. |
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| Interactions |
Same as
tenofovir and
emtricitabine
and
efavirenz (see above or click on the drug name) If Atripla is used with didanosine, reduce the dose of didanosine EC to 250 mg daily maximum. Atripla should be used cautiously if at all with atazanavir as the triple interaction of efavirenz, tenofovir, and atazanavir has not been well studied. |
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Laboratory Monitoring |
Monthly CBC for 3 months, then every 3 months if
stable Consider monthly creatinine measurements in lean individuals or those with renal insufficiency Monthly liver profile for 3 months, then every 3 months and as indicated if stable Monitor urine glucose and protein at baseline and periodically |
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| Warning |
Rare lactic acidosis and hepatic
steatosis. Fanconi syndrome (bone pain, glycosuria, hypophosphatemia, elevated serum creatinine) has been observed with tenofovir. Monitor serum phosphorous, urine glucose and protein at baseline and periodically. |
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| Contraindication | None | ||
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Suggested Usage |
In general Atripla should be used in persons who
are naive to treatment as most persons who are treatment experienced may
harbor resistance mutations to lamivudine/emtricitabine and/or NNRTIs. Resistance testing should be done prior to using Atripla. Do not use in combination with Sustiva, lamivudine, emtricitabine, Epzicom, Combivir, or Trizivir due to identical mechanism of action or duplication of efavirenz or emtricitabine dosing. Encourage exercise and calcium intake to minimize bone loss. Advise patient to avoid dehydration. Do not discontinue abruptly in patients with chronic hepatitis B without consideration of continuation of lamivudine or some other agent active against hepatitis B. |
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Complete prescribing information |
Atripla Prescribing Info Also see http://www.atripla.com for further info as it becomes available. Patient handout for this drug HERE. |
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Complera A combination of emtricitabine + rilpivirine + tenofovir Approved 8/102011 |
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| Forms Available | 300 mg tenofovir / 200 mg emtricitabine / 50 mg rilpivirine, in tablet form | ||
| Dosing |
1 tablet once a day with food This coformulation, Complera, should be taken with a least 400 calories of food, preferably a meal. |
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| Renal dosing |
Dosing interval Ccr 30-49 cc/min |
Dosing interval Ccr < 30 cc/min |
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| Not recommended | Not recommended | ||
| Hepatic dosing: no data available | |||
| Food dependence |
Food increases
rilpivirine absorption and is essential for absorption. Take Complera with a meal, at least 400 calories |
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| Adverse Effects |
Same as
tenofovir and
emtricitabine
and
rilpivirine
(see above or click on the drug name) Rilpivirine does not usually produce any side effects but rash, liver dysfunction, and depression may occur. Tenofovir may cause nephropathy, Fanconi-like syndrome, or loss of bone mineralization. Emtricitabine rarely causes discoloration of palms or soles. |
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| Interactions |
Same as
tenofovir and
emtricitabine
and
rilpivirine
(see above or click on the drug name) Complera should not be used with proton pump inhibitors (e.g., omeprazole) and histamine-2 (H2) blockers should be separated by at least 12 hours from Complera or rilpivirine dosing Use
concomitant agents with nephrotoxic potential cautiously |
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Laboratory
Monitoring |
When initiating therapy with Complera, check HIV
RNA measurements at frequent intervals to assess effectiveness and adherence
[e.g., week 2-3, week 4-6, and monthly until HIV RNA is undetectable]
Monthly CBC for 3 months, then every 3 months if
stable Monitor urine glucose and protein at baseline and periodically |
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| Warning |
Rare lactic acidosis and hepatic
steatosis. Do not used fixed dose combination in persons with renal insufficiency. Severe acute exacerbations of chronic hepatitis B may be observed with sudden discontinuation of lamivudine, emtricitabine, Truvada, Trizivir, Epzicom, Atripla, Complera, Stribild. Use Complera and rilpivirine cautiously in patients with moderate to severe depression. Fanconi syndrome (bone pain, glycosuria, hypophosphatemia, elevated serum creatinine) has been observed with tenofovir. Monitor serum phosphorous, urine glucose and protein at baseline and periodically. |
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| Contraindication | See prescribing info below | ||
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Suggested Usage |
In general Complera should be used in persons who
are naive to treatment as most persons who are treatment experienced may
harbor resistance mutations to lamivudine/emtricitabine and/or NNRTIs. Resistance testing should be done prior to using Complera, even in persons naive to antiretroviral therapy. Do not use with other antiretroviral agents. Encourage exercise and calcium intake to minimize bone loss. Advise patient to avoid dehydration. Do not discontinue abruptly in patients with chronic hepatitis B without consideration of continuation of lamivudine or some other agent active against hepatitis B. |
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Complete prescribing information |
Complera prescribing info Also see http://www.complera.com for further info as it becomes available. Patient handout for this drug HERE. |
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Stribild A combination of emtricitabine + elvitegravir + cobicistat + tenofovir Approved 8/27/2012 |
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| Forms Available | 300 mg tenofovir / 200 mg emtricitabine / 150 mg elvitegravir / 150 mg cobicistat, in tablet form | ||
| Dosing | 1 tablet once a day with food | ||
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Renal dosing at initiation
(see below for adjustments during treatment) |
Dosing interval Ccr 30-69 cc/min |
Dosing interval Ccr < 30 cc/min |
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| Not recommended | Not recommended | ||
| Hepatic dosing: no data available | |||
| Food dependence | Take Stribild with food | ||
| Adverse Effects |
Same as
tenofovir and
emtricitabine
and
elvitegravir
and
cobicistat
(see above or click on the drug name) Elvitegravir does not usually produce any side effects but some nausea or diarrhea may occur. Rash is also possible.
Cobicistat usually does not produce side effects
but nausea or diarrhea may occur. Rash is also possible. |
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| Interactions |
Same as
tenofovir and
emtricitabine
and
elitegravir/cobicistat.
Use concomitant agents with nephrotoxic
potential cautiously. |
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Laboratory Monitoring |
When initiating therapy with Stribild, check HIV
RNA measurements at frequent intervals to assess effectiveness and adherence
[e.g., week 2-3, week 4-6, and monthly until HIV RNA is undetectable] Check baseline urine glucose and protein and monitor periodically thereafter.
Monthly CBC, metabolic profile for 3 months, then every 3 months if
stable |
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| Warning |
Rare lactic acidosis and hepatic
steatosis (obesity and prolonged exposure to NRTI medications may be risk
factors) Do not used fixed dose combination in persons with renal insufficiency. Severe acute exacerbations of chronic hepatitis B may be observed with sudden discontinuation of lamivudine, emtricitabine, Truvada, Trizivir, Epzicom, Atripla, Complera, Stribild. Use Stribild cautiously in patients who are taking other nephrotoxic agents or who are at risk of dehydration (e.g., diarrhea diseases, esophagitis, nausea and vomiting). Renal dysfunction: monitor renal function closely if serum creatinine increases by greater than 0.4 mg per dL and stop Stribild if the creatinine clearance drops below 50 mL/minute. Fanconi syndrome (bone pain, glycosuria, hypophosphatemia, elevated serum creatinine) has been observed with tenofovir. Monitor serum phosphorous, urine glucose and protein at baseline and periodically. |
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| Contraindication |
alfuzosin: potential for increased level of
alfuzosin levels and hypotension rifampin: levels of elvitegravir and cobicistat may be decreased, resulting in subtherapeutic concentrations dihydroergotamine, ergotamin, methylergonovine: potential for serious and/or life-threatening events such as acute ergot toxicity (vasospasm and ischemia of tissues or extremities) cisapride: potential for serious and/or life-threatening events such as cardiac arrhythmias St. John's wort (hypericum perforatum): levels of elvitegravir and cobicistat may be decreased, resulting in subtherapeutic concentrations lovastatin, simvastatin: increased levels of statin drug which might result in myopathy, including rhabdomyolysis pimozide: potential to cause life-threatening events such as cardiac arrhythmias sildenafil: when dosed as Revatio (20 mg three times a day) as there is an increased risk for visual disturbances, hypotension, syncope triazolam, oral-administered midazolam: there may be large increases in the concentrations of these benzodiazapines which may results in sedation or respiratory depression |
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Suggested Usage |
In general Stribild should be used in persons who
are naive to treatment as most persons who are treatment experienced may
harbor resistance mutations to lamivudine/emtricitabine and/or integrase
inhibitors. Stribild should not be used
in persons with creatinine clearance of less than 70 cc/min. |
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Complete prescribing information |
Stribild Prescribing Info Also see http://www.stribild.com for further info as it becomes available. Patient handout for this drug HERE. |
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| Next Page | Click HERE for Antiretroviral Summary Information |
| Links to Antiretroviral Sections |
| Nucleoside & Nucleotide Reverse Transcriptase Inhibitors (NRTI) |
| AZT | ddI | d4T | 3TC | ABC | FTC | TDF ||| Coformulation NRTI: Combivir | Trizivir | Epzicom | Truvada |
| Nonnucleoside Reverse Transcriptase Inhibitors (NNRTI) |
| efavirenz | nevirapine | delavirdine | etravirine | rilpivirine |
| Protease Inhibitors (PI) | Boosted Protease Inhibitors |
| saquinavir | indinavir | ritonavir | nelfinavir | lopinavir + ritonavir | atazanavir | fosamprenavir | tipranavir |
| Co-receptor Inhibitors |
| maraviroc |
| Fusion Inhibitors |
| enfuvirtide |
| Integrase Inhibitors |
| raltegravir | elvitegravir | dolutegravir |
| Antiretroviral Metabolic Inhibitors |
| cobicistat | ritonavir |
| Coformulations |
| Atripla (efavirenz/tenofovir/emtricitabine) | Complera (rilpivirine/tenofovir/emtricitabine) | Stribild (elvitegravir/cobicistat/tenofovir/emtricitabine) |
Updated 3/5/2013
1. Renal dosing information from: Ian R.
McNicholl & Rudolph A. Rodriguez, MD, Dosing of Antiretroviral Drugs in Renal
Insufficiency and Hemodialysis, May 2004
http://hivinsite.ucsf.edu/InSite?page=md-rr-18