Table 11. Antiretroviral Drug Use in Pregnant People with HIV: Pharmacokinetic and Toxicity Data in Human Pregnancy and Recommendations for Use in Pregnancy

• 300 mg

• 20 mg/mL

• ABC 600 mg/
  3TC 300-mg tablet

• ABC 600 mg/
  DTG 50 mg/
  3TC 300-mg tablet

• ABC 300 mg/3TC 150 mg/ZDV 300 mg tablet

Standard Adult Doses
ABC (Ziagen)

• ABC 300 mg twice daily or ABC 600 mg once daily, without regard to food

ABC/3TC (Epzicom)

• One tablet once daily without regard to food

ABC/DTG/3TC (Triumeq)

• One tablet once daily without regard to food

ABC/3TC/ZDV (Trizivir)

• One tablet twice daily without regard to food

Pregnancy
PKs in Pregnancy

• PKs not significantly altered in pregnancy.

Dosing in Pregnancy

• No change in dose indicated.

For guidance about use of combination products in pregnancy, please see the specific sections on other components (i.e., 3TC, ZDV, DTG).

High placental transfer to fetus.^b

No evidence of human teratogenicity (can rule out 1.5-fold increase in overall birth defects).

HSRs occur in approximately 5% to 8% of nonpregnant individuals. A small percentage of reactions are fatal, and these fatal reactions are usually associated with re-challenge. Rate of reactions during pregnancy is unknown. Testing for HLA-B*5701 identifies patients at risk of reactions, and a patient’s status should be documented as negative before initiating ABC. Patients should be educated regarding symptoms of HSR.

FTC (Emtriva)
Capsule^d

• 200 mg

• 10 mg/mL

• FTC 200 mg/
  EFV 600 mg/
  TDF 300-mg tablet

• FTC 200 mg/
  BIC 50 mg/
  TAF 25 mg- tablet

• FTC 200 mg/
  RPV 25 mg/
  TDF 300-mg tablet

• FTC 200 mg/
  TAF 25-mg tablet

• FTC 200 mg/
  EVG 150 mg/
  COBI 150 mg/
  TAF 10-mg tablet

• FTC 200 mg/
  RPV 25 mg/
  TAF 25-mg tablet

• FTC 200 mg/
  EVG 150 mg/
  COBI 150 mg/
  TDF 300-mg tablet

• FTC 200 mg/
  DRV 800 mg/
  COBI 150 mg/
  TAF 10-mg tablet

• FTC 200 mg/
  TDF 300-mg tablet

Standard Adult Doses
FTC (Emtriva) — Capsule

• FTC 200 mg once daily without regard to food

FTC (Emtriva) — Oral Solution

• FTC 240 mg (24 mL) once daily without regard to food

FTC/EFV/TDF (Atripla)

• One tablet once daily at or before bedtime
• Take on an empty stomach to reduce or mitigate side effects.

FTC/BIC/TAF (Biktarvy)

• One tablet once daily with or without food

FTC/RPV/TDF (Complera)

• One tablet once daily with food

FTC/TAF (Descovy)

• One tablet once daily with or without food

FTC/EVG/c/TAF (Genvoya)

• One tablet once daily with food

FTC/RPV/TAF (Odefsey)

• One tablet once daily with food

FTC/EVG/c/TDF (Stribild)

• One tablet once daily with food

FTC/DRV/c/TAF (Symtuza)

• One tablet once daily with food

FTC/TDF (Truvada)

• One tablet once daily without regard to food

Pregnancy
PKs in Pregnancy

• PKs of FTC are not significantly altered in pregnancy.

Dosing in Pregnancy

• No change in dose indicated.

For guidance about the use of combination products in pregnancy, please see the specific sections on other components (i.e., TDF, TAF, EFV, RPV, DRV, EVG, BIC, COBI).

High placental transfer to fetus.^b

No evidence of human teratogenicity (can rule out 1.5-fold increase in overall birth defects).

If patient has HBV/HIV coinfection, it is possible that an HBV flare may occur if the drug is stopped; see Hepatitis B Virus/HIV Coinfection.

3TC (Epivir)^d
Tablets

• 150 mg
• 300 mg

Oral Solution

• 10 mg/mL

3TC/TDF (Cimduo)

• 3TC 300 mg/
  TDF 300-mg tablet

3TC/ZDV (Combivir)^d

• 3TC 150 mg/
  ZDV 300-mg tablet

3TC/DOR/TDF (Delstrigo)

• 3TC 300 mg/
  DOR 100 mg/
  TDF 300-mg tablet

3TC/DTG (Dovato)

• 3TC 300 mg/
  DTG 50-mg tablet

3TC/ABC (Epzicom)^d

• 3TC 300 mg/
  ABC 600-mg tablet

3TC/EFV/TDF (Symfi)^d

• 3TC 300 mg/
  EFV 600 mg plus TDF 300-mg tablet

3TC/EFV/TDF (SymfiLo)^d

• 3TC 300 mg/
  EFV 400 mg/
  TDF 300-mg tablet

3TC/TDF (Temixys)

• 3TC 300 mg/
  TDF 300-mg tablet

3TC/ABC/DTG (Triumeq)

• 3TC 300 mg/
  ABC 600 mg/
  DTG 50-mg tablet

3TC/ABC/ZDV (Trizivir)^d

• 3TC 150 mg/
  ABC 300 mg/
  ZDV 300-mg tablet

Standard Adult Doses
3TC (Epivir)

• 3TC 150 mg twice daily or 300 mg once daily, without regard to food

3TC/TDF (Cimduo)

• One tablet once daily without regard to food

3TC/ZDV (Combivir)

• One tablet twice daily without regard to food

3TC/DOR/TDF (Delstrigo)

• One tablet once daily without regard to food

3TC/DTG (Dovato)

• One tablet once daily without regard to food

3TC/ABC (Epzicom)

• One tablet once daily without regard to food

3TC/EFV/TDF (Symfi or Symfi Lo)

• One tablet once daily on an empty stomach and preferably at bedtime

3TC/TDF (Temixys)

• One tablet once daily without regard to food

3TC/ABC/DTG (Triumeq)

• One tablet once daily without regard to food

3TC/ABC/ZDV (Trizivir)

• One tablet twice daily without regard to food

Pregnancy
PKs in Pregnancy

• PKs not significantly altered in pregnancy.

Dosing in Pregnancy

• No change in dose indicated.

For guidance about the use of combination products in pregnancy, please see the specific sections on other components (i.e., ABC, DOR, DTG, EFV, TDF, ZDV).

High placental transfer to fetus.^b

No evidence of human teratogenicity (can rule out 1.5-fold increase in overall birth defects).

If patient has HBV/HIV coinfection, it is possible that an HBV flare may occur if the drug is stopped; see Hepatitis B Virus/HIV Coinfection.

3TC products that were developed specifically for treatment of HBV (e.g., Epivir-HBV) contain a lower dose of 3TC that is not appropriate for treatment of HIV.

TAF (Vemlidy)
Tablet

• 25 mg

TAF/BIC/FTC (Biktarvy)

• TAF 25 mg/
  BIC 50 mg/
  FTC 200‑mg tablet

TAF/FTC (Descovy)

• TAF 25 mg/
  FTC 200-mg tablet

TAF/EVG/c/FTC (Genvoya)

• TAF 10 mg/
  EVG 150 mg/
  COBI 150 mg/
  FTC 200-mg tablet

TAF/FTC/RPV (Odefsey)

• TAF 25 mg/
  FTC 200 mg/
  RPV 25­-mg tablet

TAF/DRV/c/FTC (Symtuza)

• TAF 10 mg/
  DRV 800 mg/
  COBI 150 mg/
  FTC 200-mg tablet

Standard Adult Doses
TAF (Vemlidy)

• One tablet once daily with food

TAF/BIC/FTC (Biktarvy)

• One tablet once daily with or without food

TAF/FTC Descovy)

• One tablet once daily with or without food
• Same dose (TAF 25 mg) can be used with or without PK enhancers.

TAF/EVG/c/FTC (Genvoya)

• One tablet once daily with food

TAF/FTC/RPV (Odefsey)

• One tablet once daily with food

TAF/DRV/c/FTC (Symtuza)

• One tablet once daily with food

Pregnancy
PKs in Pregnancy

• Plasma PKs not significantly altered in pregnancy.

Dosing in Pregnancy

• No change in dose indicated.

For guidance about the use of combination products in pregnancy, please see the specific sections on other components (i.e., BIC, COBI, DRV, EVG, FTC, RPV).

Low placental transfer to fetus.^b

Insufficient data to assess for teratogenicity in humans. No evidence of teratogenicity in rats.

Renal function should be monitored because of the potential for renal toxicity.

TDF (Viread)

• Tablet^d
  • 300 mg
• Powder
  • 40 mg/
    1 g oral powder

TDF/EFV/FTC (Atripla)

• TDF 300 mg/
  EFV 600 mg/
  FTC 200 mg tablet

TDF/3TC (Cimduo)

• TDF 300 mg/
  3TC 300 mg tablet

TDF/FTC/RPV (Complera)

• TDF 300 mg/
  FTC 200 mg/
  RPV 25 mg tablet

TDF/DOR/3TC (Delstrigo)

• TDF 300 mg/
  DOR 100 mg/
  3TC 300 mg tablet

TDF/EVG/c/FTC (Stribild)

• TDF 300 mg/
  EVG 150 mg/
  COBI 150 mg/
  FTC 200 mg tablet

TDF/EFV/3TC (Symfi)

• TDF 300 mg/
  EFV 600 mg/
  3TC 300 mg tablet

TDF/EFV/3TC (Symfi Lo)

• TDF 300 mg/
  EFV 400 mg/
  3TC 300 mg tablet

TDF/3TC (Temixys)

• TDF 300 mg/
  3TC 300-mg tablet

TDF/FTC (Truvada)

• TDF 300 mg/
  FTC 200-mg tablet

Standard Adult Doses

TDF (Viread)

• Tablet
  • TDF 300 mg once daily without regard to food
• Powder
  • TDF 8 mg/kg daily (up to a maximum of TDF 300 mg). Take with food.

TDF/EFV/FTC (Atripla)

• One tablet once daily at or before bedtime. Take on an empty stomach to reduce side effects.

TDF/3TC (Cimduo)

• One tablet once daily without regard to food

TDF/FTC/RPV (Complera)

• One tablet once daily with food

TDF/DOR/3TC (Delstrigo)

• One tablet once daily without regard to food

TDF/EVG/c/FTC (Stribild)

• One tablet once daily with food

TDF/EFV/3TC (Symfi or Symfi Lo)

• One tablet once daily on an empty stomach and preferably at bedtime

TDF/3TC (Temixys)

• One tablet once daily without regard to food

TDF/FTC (Truvada)

• One tablet once daily without regard to food

Pregnancy

PKs in Pregnancy

• AUC is lower in third trimester than postpartum, but trough levels are adequate.

Dosing in Pregnancy

• No change in dose is indicated.

For guidance about the use of combination products in pregnancy, please see the specific sections on other components (i.e., 3TC, COBI, DOR, EFV, EVG, FTC, RPV).

High placental transfer to fetus.^b

No evidence of human teratogenicity (can rule out 1.5-fold increase in overall birth defects).

Studies in monkeys (at doses approximately twofold higher than those for human therapeutic use) show decreased fetal growth and reduction in fetal bone porosity within 2 months of starting maternal therapy. Human studies demonstrate no consistent link to low birth weight, but data are conflicting about potential effects on growth outcomes later in infancy.

If patient has HBV/HIV coinfection, an HBV flare may occur if TDF is stopped; see Hepatitis B Virus/HIV Coinfection.

Renal function should be monitored because of potential for renal toxicity.

ZDV (Retrovir)

Capsule

• 100 mg

Tablet

• 300 mg

Oral Solution

• 10 mg/mL

IV Solution

• 10 mg/mL

ZDV/3TC (Combivir)

• ZDV 300 mg/
  3TC 150-mg tablet

ZDV/ABC/3TC (Trizivir)

• ZDV 300 mg/
  ABC 300 mg/
  3TC 150-mg tablet

Standard Adult Doses

ZDV (Retrovir)

• ZDV 300 mg twice daily or ZDV 200 mg three times a day without regard to food
• Patients in active labor should receive ZDV 2 mg/kg IV as a loading dose, followed by ZDV 1 mg/kg/hour continuous infusion from beginning of active labor until delivery

ZDV/3TC (Combivir)

• One tablet twice daily without regard to food

ZDV/ABC/3TC (Trizivir)

• One tablet twice daily without regard to food

Pregnancy

PKs in Pregnancy

• PKs not significantly altered in pregnancy.

Dosing in Pregnancy

• No change in dose indicated.

For guidance about the use of combination products in pregnancy, please see the specific sections on other components (i.e., ABC, 3TC).

High placental transfer to fetus.^b

No evidence of human teratogenicity (can rule out 1.5-fold increase in overall birth defects).

• 100 mg tablet

• DOR 100 mg/
  3TC 300 mg/
  TDF 300 mg tablet

Standard Adult Doses

DOR (Pifeltro)

• DOR 100 mg once daily with or without food

DOR/3TC/TDF (Delstrigo)

• One tablet once daily with or without food

Pregnancy

PKs in Pregnancy

• No PK studies in human pregnancy.

Dosing in Pregnancy

• Insufficient data to make dosing recommendations.

For guidance about the use of combination ARV drug products in pregnancy, please see the specific sections on other drug components (i.e., 3TC, TDF).

No human in vivo data are available on the placental transfer of DOR, but passage is noted in an ex vivo model.

Insufficient data are available to assess for teratogenicity in humans. No evidence exists of teratogenicity in rats or rabbits.

• 50 mg
• 200 mg

• 600 mg

• EFV 600 mg/
  FTC 200 mg/
  TDF 300-mg tablet

• EFV 600 mg/
  3TC 300 mg/
  TDF 300-mg tablet

• EFV 400 mg/
  3TC 300 mg/
  TDF 300-mg tablet

Standard Adult Doses

EFV (Sustiva)

• EFV 600 mg once daily at or before bedtime
• Take on an empty stomach to reduce side effects.

EFV/FTC/TDF (Atripla)

• One tablet once daily at or before bedtime
• Take on an empty stomach to reduce side effects.

EFV/3TC/TDF
(Symfi or Symfi Lo)

• One tablet once daily on an empty stomach and preferably at bedtime

Pregnancy

PKs in Pregnancy

• AUC is decreased during the third trimester compared with postpartum, but nearly all third trimester participants exceeded target exposure.

Dosing in Pregnancy

• No change in dose is indicated.

For guidance about the use of combination products in pregnancy, please see the specific sections on other components (i.e., 3TC, FTC, TDF).

Moderate placental transfer to fetus.^b

The FDA advises women to avoid becoming pregnant while taking EFV and advises health care providers to avoid administration during the first trimester of pregnancy because fetal harm may occur. However, the data on more than 7,900 periconception EFV exposures from Botswana rule out a threefold or greater increased risk of NTDs. As a result, the current Perinatal Guidelines do not restrict the use of EFV in pregnant women or in women who are planning to become pregnant. This is consistent with both the British HIV Association and WHO guidelines for use of ARV drugs in pregnancy.

EFV should be continued in pregnant women who are on a virally suppressive, EFV-based regimen, because ARV drug changes during pregnancy may be associated with loss of viral control and an increased risk of perinatal transmission (see Pregnant People with HIV Who are Currently Receiving Antiretroviral Therapy).

• 25 mg
• 100 mg
• 200 mg

• 200 mg twice daily with food

• PK data in pregnancy suggest 1.2-fold to 1.6-fold increases in ETR exposure during pregnancy.

• No change in dose is indicated.

• 200 mg^d

• 50 mg/5 mL^d

• 100 mg
• 400 mg^d

• NVP 200 mg once daily (using Viramune immediate release) for a 14-day lead-in period; thereafter, NVP 200 mg twice daily or 400 mg (using Viramune XR tablet) once daily, without regard to food.
• Repeat lead-in period if therapy is discontinued for >7 days.
• In patients who develop mild-to-moderate rash without constitutional symptoms during the lead-in period, continue lead-in dosing until rash resolves, but administer for ≤28 days total.

• PKs of immediate-release tablets not significantly altered in pregnancy.
• No data available on extended-release formulations in pregnancy.

• No change in dose indicated.

High placental transfer to fetus.^b

No evidence of human teratogenicity (can rule out 1.5-fold increase in overall birth defects and twofold increase in cardiovascular and genitourinary defects).

An increased risk of symptomatic liver toxicity exists when first initiating therapy in women with CD4 counts ≥250/mm³. Liver toxicity is often associated with a rash and can be fatal. Pregnancy does not appear to increase this risk.

NVP should be initiated in pregnant people with CD4 counts ≥250 cells/mm³ only if benefit clearly outweighs risk. A potential increased risk of life-threatening hepatotoxicity exists in pregnant people with high CD4 counts. Elevated transaminase levels at baseline may increase the risk of NVP toxicity.

Patients who become pregnant while taking NVP-containing regimens and who are tolerating their regimens well can continue taking those regimens, regardless of their CD4 counts.

Rilpivirine
(RPV)
Edurant

(RPV/FTC/TDF)
Complera

(RPV/DTG)
Juluca

(RPV/FTC/TAF)
Odefsey

(CAB and RPV)
Cabenuva

CAB and RPV is a two-drug co-packaged product for IM injection.

• 25 mg

• RPV 25 mg/
  FTC 200 mg/
  TDF 300-mg tablet

• RPV 25 mg/
  DTG 50-mg tablet

• RPV 25 mg/
  FTC 200 mg/
  TAF 25-mg tablet

Standard Adult Doses

RPV (Edurant)

• RPV 25 mg once daily with food

RPV/FTC/TDF (Complera)

• One tablet once daily with food

RPV/DTG (Juluca)

• One tablet once daily with food

RPV/FTC/TAF (Odefsey)

• One tablet once daily with food

CAB and RPV (Cabenuva)

• Refer to Cabotegravir for dosing and instructions.

Pregnancy

PKs in Pregnancy

• RPV PKs are highly variable during pregnancy. RPV AUC and trough concentrations are 20% to 50% lower in pregnancy than postpartum. Although most pregnant women exceeded target exposure, those with detectable viral loads had lower RPV troughs.

Dosing in Pregnancy

• Although RPV plasma concentration is reduced during pregnancy, higher-than-standard doses have not been studied, and not enough data are available to recommend a dosing change during pregnancy. Pregnant women receiving standard dosing should have their viral loads monitored more frequently than women who are not receiving RPV.

For guidance about the use of combination products in pregnancy, please see the specific sections on other components (i.e., DTG, FTC, TAF, TDF).

Moderate-to-high placental transfer to fetus.^b

No evidence of human teratogenicity (can rule out two-fold increase in overall birth defects).

Two-drug regimens (e.g., the RPV/DTG FDC) are not recommended for use in pregnancy.

• 100 mg (generic product only)
• 150 mg^d
• 200 mg^d
• 300 mg^d

• 50-mg packet

• ATV 300 mg/
  COBI 150-mg tablet

• ATV 400 mg once daily with food; ATV without RTV boosting is not recommended when used with TDF, H2-receptor antagonists, PPIs, or during pregnancy.

• ATV/r 300 mg/100 mg once daily with food
• When combined with EFV in ARV-naive patients: ATV/r 400 mg/100 mg once daily with food

• ATV 300 mg plus RTV 100 mg once daily with food
• Do not use with PPIs or EFV.

• ATV/r 300/100 mg once daily with food

• ATV/r 400 mg/100 mg once daily with food

• Oral powder is taken with RTV once daily with food at the same recommended adult dose as the capsules.

• One tablet once daily with food

Pregnancy
PKs in Pregnancy

• ATV (Reyataz)
  • ATV concentrations are reduced during pregnancy, and they are further reduced when ATV is given concomitantly with TDF or an H2-receptor antagonist.
• ATV/c (Evotaz)
  • Use of ATV/c is not recommended during pregnancy, because ATV trough concentrations are 80% to 85% lower than the ATV concentrations seen in nonpregnant adults.

Dosing in Pregnancy

• ATV (Reyataz)
  • Use of unboosted ATV is not recommended during pregnancy.
  • Use of ATV is not recommended for ARV-experienced pregnant women who are taking TDF and an H2-receptor antagonist.
  • Use of an increased dose (ATV/r 400 mg/100 mg once daily with food) during the second and third trimesters results in plasma ATV concentrations equivalent to those seen in nonpregnant adults receiving standard dosing. Although some experts recommend increased ATV dosing in all women during the second and third trimesters, the package insert recommends increased ATV dosing only for ARV-experienced pregnant women in the second and third trimesters who are also receiving either TDF or an H2-receptor antagonist.
• ATV/c (Evotaz)
  • Insufficient data to make dosing recommendation in pregnancy (see COBI).
  • For guidance about the use of combination products in pregnancy, please see the specific sections on other components (i.e., COBI).

• 75 mg
• 150 mg
• 600 mg
• 800 mg

• 100 mg/mL

• DRV/c 800 mg/
  150 mg tablet

• DRV 800 mg/
  COBI 150 mg/
  FTC 200 mg/
  TAF 10 mg tablet

• DRV/r 800 mg/ 100 mg once daily with food
• DRV/c 800 mg/ 150 mg once daily with food

• DRV/r 800 mg/ 100 mg once daily with food
• DRV/c 800 mg/ 150 mg once daily with food

• DRV/r 600 mg/ 100 mg twice daily with food

• One tablet once daily with food

• One tablet once daily with food

• Decreased exposure in pregnancy with use of DRV/r.

• The Panel does not recommend once-daily dosing with DRV/r during pregnancy or the use of DRV/c during pregnancy.
• Twice-daily DRV/r dosing (DRV/r 600 mg/100 mg with food) is recommended for all pregnant women.
• Increased, twice-daily DRV dose (DRV/r 800 mg/100 mg with food) during pregnancy does not result in an increase in DRV exposure and is not recommended.

• LPV/r 200 mg/50 mg
• LPV/r 100 mg/25 mg

• Each 5 mL contains LPV/r 400 mg/100 mg^d

Standard Adult Doses

• LPV/r 400 mg/
  100 mg twice daily, or
• LPV/r 800 mg/
  200 mg once daily

Tablets

• Take without regard to food.

Oral Solution

• Take with a meal.

With EFV or NVP in PI-Naive or PI-Experienced Patients

• LPV/r 500 mg/
  125-mg tablets twice daily without regard to meals (use a combination of two LPV/r 200 mg/50 mg tablets and one LPV/r 100 mg/25-mg tablet), or
• LPV/r 520 mg/
  130 mg oral solution (6.5 mL) twice daily with food

Pregnancy

PKs in Pregnancy

• With twice-daily dosing, LPV exposure is reduced in pregnant women who receive standard adult doses; increasing the dose by 50% results in exposure equivalent to that seen in nonpregnant adults receiving standard doses.
• No PK data are available for once-daily dosing in pregnancy.

Dosing in Pregnancy

• Once-daily dosing is not recommended during pregnancy.
• Some experts recommend that an increased dose (i.e., LPV/r 600 mg/
  150 mg twice daily without regard to meals or LPV/r 500 mg/
  125 mg twice daily without regard to meals) should be used in the second and third trimesters, especially in PI-experienced pregnant women and women who start treatment during pregnancy with a baseline viral load >50 copies/mL.
• When standard dosing is used, monitor virologic response and, if possible, LPV drug levels.

Low placental transfer to fetus.^b

No evidence of human teratogenicity (can rule out 1.5-fold increase in overall birth defects).

Oral solution contains 42% alcohol and 15% propylene glycol and is not recommended for use in pregnancy.

Once-daily LPV/r dosing is not recommended during pregnancy.

FTR (Rukobia)
Extended-Release Tablet

• 600 mg

• FTR 600 mg twice daily with or without food

• No PK studies in human pregnancy.

• Insufficient data to make dosing recommendations.

• 150mg/mL

• IBA 2,000-mg loading dose, followed by IBA 800-mg maintenance doses administered every 2 weeks

• No PK studies in human pregnancy.

• Insufficient data to make dosing recommendations.

No human data are available, but placental transfer of IBA, a monoclonal antibody, is possible and documented in monkeys.

Based on data in cynomologus monkeys with in utero exposure, potential exists for reversible immunosuppression (CD4 T cell and B cell lymphocytopenia) in infants born to mothers exposed to IBA during pregnancy.

The FDA requires collection of prospective data in individuals exposed to IBA during pregnancy to monitor maternal and pregnancy outcomes, including adverse effects on the developing fetus, neonate, and infant.

Insufficient data to assess for teratogenicity in humans.

• 150 mg
• 300 mg

• MVC 300 mg twice daily with or without food
• MVC should be used only for patients with CCR5-tropic virus (and no X4-tropic virus).

• Increase to MVC 600 mg twice daily when used with the potent CYP3A inducers EFV, ETR, and rifampin.
• Decrease to MVC 150 mg twice daily when used with CYP3A inhibitors, which includes all PIs except TPV/r and itraconazole.

• A PK study in human pregnancy demonstrated a 20% to 30% overall decrease in MVC AUC, but C_trough exceeded the recommended minimal concentration of 50 ng/mL.

• Adjusting the standard adult MVC dose for concomitant use with ARV drugs seems appropriate.

Bictegravir/Emtricitabine/ Tenofovir Alafenamide
(BIC/FTC/TAF)
Biktarvy

Note: BIC is available only as part of an FDC tablet.

BIC/FTC/TAF (Biktarvy)

• BIC 50 mg/
  FTC 200 mg/
  TAF 25 mg tablet
• BIC 30 mg/
  FTC 120 mg/
  TAF 15 mg tablet

Standard Adult Doses

• One tablet of BIC 50 mg/FTC 200 mg/TAF 25 once daily with or without food

Pregnancy
PK in Pregnancy

• No PK studies in human pregnancy

Dosing in Pregnancy

• Insufficient data to make dosing recommendations

For guidance about use of combination products in pregnancy, please see the specific sections on other components (i.e., FTC, TAF).

More data are needed to characterize the placental passage of BIC.

Insufficient data exist to assess for teratogenicity in humans. No evidence of teratogenicity in rats or rabbits exists.

BIC can be taken with food at the same time as any preparation containing iron or calcium—including prenatal vitamins—but should not be administered within 2 hours of these preparations when taken on an empty stomach. BIC can be taken at least 2 hours before or 6 hours after antacids containing aluminum or magnesium.

December 30, 2021

Cabotegravir
(CAB)
Vocabria (oral)
Apretude (injection)

(CAB RPV)
Cabenuva

CAB RPV is a two-drug co-packaged product for IM injection.

CAB

• CAB 30-mg tablets for oral administration
• CAB 200 mg/mL suspension for IM injection

CAB RPV

• CAB 200 mg/mL suspension for IM injection

RPV 300 mg/mL suspension for IM injection

Standard Adult Doses

Oral Lead-in Therapy
CAB (Vocabria)

• One 30-mg tablet once daily in combination with RPV (Edurant) 25 mg once daily taken with a meal for 4 weeks

CAB (Apretude)
Initiation

• CAB 600 mg (3 mL) injection given 1 month apart for 2 consecutive months on the last day of an oral lead-in if used or within 3 days

Continuation Therapy

• CAB 600 mg (3 mL) injections every 2 months thereafter

CAB RPV (Cabenuva)
Loading Dose to Be Given on Last Day of Oral Therapy

• CAB 600 mg (3 mL) and RPV 900 mg (3 mL), given as two separate injections in separate ventrogluteal sites

Continuation Therapy

• CAB 400 mg (2 mL) and RPV 600 mg (2 mL), given as two separate injections in separate ventrogluteal sites once a month with allowance for a +/- 7‑day administration window
• Patients should be monitored for ~10 minutes for post-injection reactions. A 23‑gauge, 1.5‑inch IM needle is recommended for the injection and is provided in the packaging. Longer, 2‑inch needles should be used in patients with BMIs >30 kg/m².

Pregnancy
PKs in Pregnancy

• No PK studies in human pregnancy

Dosing in Pregnancy

• Insufficient data to make dosing recommendations

For guidance about the use of combination products in pregnancy, please see the specific sections on other components (i.e., RPV).

No human data are available regarding placental passage.

Insufficient data to assess for teratogenicity in humans. No evidence of teratogenicity in rats or rabbits.

December 30, 2021

Dolutegravir
(DTG)
Tivicay

Tivicay PD

(DTG/3TC)
Dovato

(DTG/RPV)
Juluca

(DTG/ABC/3TC)
Triumeq

DTG (Tivicay)

• DTG 10 mg, 25 mg, and 50 mg film-coated tablets

DTG (Tivicay PD)

• DTG 5 mg dispersible tablet for oral suspension

DTG film-coated tablets and DTG dispersible tablets are not bioequivalent and are not interchangeable.

DTG/3TC (Dovato)

• DTG 50 mg/
  3TC 300 mg tablet

DTG/RPV (Juluca)

• DTG 50 mg/
  RPV 25 mg tablet

DTG/ABC/3TC (Triumeq)

• DTG 50 mg/
  ABC 600 mg/
  3TC 300 mg tablet

Standard Adult Doses
In ARV-Naive or ARV‑Experienced (but INSTI-Naive) Patients

DTG (Tivicay)

• One 50 mg tablet once daily, without regard to food

DTG (Tivicay PD)

• Six 5 mg tablets (30 mg) dissolved in water once daily, without regard to food

DTG/3TC (Dovato)

• One tablet once daily, without regard to food

DTG/RPV (Juluca)

• One tablet once daily, with food

DTG/ABC/3TC (Triumeq)

• One tablet once daily, without regard to food

In ARV-Naive or ARV‑Experienced (but INSTI-Naive) Patients Who Are Also Receiving EFV, FPV/r, TPV/r, or Rifampin
DTG (Tivicay)

• One 50 mg tablet twice daily, without regard to food

DTG (Tivicay PD)

• Six 5 mg tablets (30 mg) dissolved in water twice daily, without regard to food

In INSTI-Experienced Patients
DTG (Tivicay)

• One tablet twice daily, without regard to food

Pregnancy

PKs in Pregnancy

• AUC may be decreased during the third trimester compared with postpartum, but exposures during pregnancy are well above those needed to inhibit viral replication.

Dosing in Pregnancy

• No change in dose indicated.

For guidance about the use of combination products in pregnancy, please see the specific sections on other components (i.e., ABC, 3TC, RPV).

High placental transfer to fetus.^b

No evidence of teratogenicity in rats or rabbits. The most recent data from Botswana indicates the prevalence of NTDs in infants born to pregnant women with HIV receiving DTG at conception is no longer statistically different than in those receiving other antiretrovirals.

DTG is a Preferred antiretroviral drug for use during pregnancy, irrespective of trimester, and for people who are trying to conceive (see Recommendations for Use of Antiretroviral Drugs During Pregnancy and Table 5).

To maximize DTG absorption, doses should not be administered within 2 hours of ingesting any preparation that contains such minerals as iron or calcium, including prenatal vitamins.

December 30, 2021

Elvitegravir
(EVG)

Note: As of October 2017, the single-drug formulation of EVG (Vitekta) is no longer available.

(EVG/c/FTC/TAF)
Genvoya

(EVG/c/FTC/TDF)
Stribild

EVG/c/FTC/TAF (Genvoya)

• EVG 150 mg/
  COBI 150 mg/
  FTC 200 mg/
  TAF 10-mg tablet

EVG/c/FTC/TDF (Stribild)

• EVG 150 mg/
  COBI 150 mg/
  FTC 200 mg/
  TDF 300-mg tablet

Standard Adult Doses
Genvoya and Stribild

• One tablet once daily with food

Pregnancy
PKs in Pregnancy

• PK studies in women who received EVG/c demonstrated significant reduction in EVG plasma exposure during pregnancy.

Dosing in Pregnancy

• EVG plasma concentrations are reduced with use of standard adult doses during pregnancy; however, higher-than-standard doses of EVG have not been studied. Insufficient data are available to recommend a dose for use in pregnancy.

For guidance about use of combination products in pregnancy, please see the specific sections on other components (i.e., COBI, FTC, TAF).

Evidence of high placental transfer of EVG and low transfer of COBI.^b

Insufficient data to assess for teratogenicity in humans. No evidence of teratogenicity in rats or rabbits.

EVG/c is not recommended for use in pregnancy. For persons who become pregnant while taking EVG/c, consider frequent viral load monitoring or switching to a more effective, recommended regimen. If a woman continues taking a regimen that contains EVG/c, doses should be administered with a meal and should not be administered within 2 hours of ingesting any preparation that contains minerals, such as iron or calcium, including prenatal vitamins.

December 30, 2021

Raltegravir
(RAL)
Isentress

Isentress HD

RAL (Isentress)
Film-Coated Tablets

• 400 mg

Chewable Tablets

• 25 mg
• 100 mg

RAL (Isentress HD)
Film-Coated Tablets

• 600 mg

Standard Adult Doses
In Patients Who Are Not Receiving Rifampin

• RAL 400 mg, film-coated tablets twice daily without regard to food
• Two RAL 600 mg, film-coated tablets (1,200 mg) once daily without regard to food for ARV-naive patients or patients who are already virologically suppressed on an initial regimen of RAL 400 mg twice daily
• Chewable tablets and oral suspension doses are not interchangeable with either film-coated tablets or each other.

In Patients Who Are Receiving Rifampin

• Two RAL 400 mg, film-coated tablets (800 mg) twice daily without regard to food.

Pregnancy
PKs in Pregnancy

• Decreased drug concentrations in the third trimester are not of sufficient magnitude to warrant a change in dosing.

Dosing in Pregnancy

• No change in dose is indicated.
• Once-daily dosing (i.e., two RAL 600 mg, film-coated tablets) should not be used in pregnant individuals until more information is available.

High placental transfer to fetus.^b

No evidence of human teratogenicity (can rule out 1.5-fold increase in overall birth defects).

There is a case report of markedly elevated liver transaminases with RAL use in late pregnancy. Severe, potentially life-threatening, and fatal skin and HSRs have been reported in nonpregnant adults.

RAL chewable tablets contain phenylalanine.

To maximize RAL absorption, doses should not be administered within 2 hours of ingestion of any preparation containing minerals—such as iron or calcium—including prenatal vitamins.

December 30, 2021

Cobicistat
(COBI)
Tybost

(ATV/c)
Evotaz

(EVG/c/FTC/TAF)
Genvoya

(DRV/c)
Prezcobix

(EVG/c/FTC/TDF)
Stribild

(DRV/c/FTC/TAF)
Symtuza

COBI (Tybost)
Tablet:

• COBI 150 mg

ATV/c (Evotaz)

• ATV 300 mg/
  COBI 50-mg tablet

EVG/c/FTC/TAF (Genvoya)

• EVG 150 mg/
  COBI 150 mg/
  FTC 200 mg/
  TAF 10-mg tablet

DRV/c (Prezcobix)

• DRV 800 mg/
  COBI 150 mg tablet

EVG/c/FTC/TDF (Stribild)

• EVG 150 mg/
  COBI 150 mg/
  FTC 200 mg/
  TDF 300-mg tablet

DRV/c/FTC/TAF (Symtuza)

• DRV 800 mg/
  COBI 150 mg/
  FTC 200 mg/
  TAF 10-mg tablet

Standard Adult Doses
COBI (Tybost)

• When used as an alternative PK booster with ATV or DRV, the dose is one tablet once daily with food.

ATV/c (Evotaz)

• One tablet once daily with food

EVG/c/FTC/TAF (Genvoya)

• One tablet once daily with food

DRV/c (Prezcobix)

• One tablet once daily with food

EVG/c/FTC/TDF (Stribild)

• One tablet once daily with food

DRV/c/FTC/TAF (Symtuza)

• One tablet once daily with food

Pregnancy
PKs in Pregnancy

• Based on limited data, COBI exposure and its pharmacoenhancing effect on ATV, DRV, and EVG are reduced markedly in pregnancy.
• When coadministered with COBI, TAF exposure is not significantly different between pregnancy and the postpartum period.

Dosing in Pregnancy

• Although COBI exposure is reduced markedly during pregnancy, higher-than-standard doses have not been studied. The Panel recommends RTV as the preferred pharmacoenhancer for PIs and INSTIs during pregnancy until more data are available on COBI activity during pregnancy.

For guidance about the use of combination products in pregnancy, please see the specific sections on other components (i.e., FTC, TAF, TDF, ATV, DRV, EVG).

Low placental transfer to fetus^b

No evidence of human teratogenicity (can rule out two-fold increase in overall birth defects).

Use of COBI-boosted ATV, DRV, or EVG is not recommended in pregnancy.

December 30, 2021

Ritonavir
(RTV)
Norvir

(LPV/r)
Kaletra

RTV (Norvir)
Capsules

• RTV 100 mg

Tablets

• RTV 100 mg

Oral Solution

• RTV 80 mg/mL

Powder

• RTV 100 mg/sachet

LPV/r (Kaletra)

Tablets

• LPV/r 200 mg/
  50 mg
• LPV/r 100 mg/25 mg

Oral Solution

• Each 5 mL contains LPV/r 400 mg/
  100 mg

Standard Adult Dose of RTV (Norvir) When Used as PK Booster for Other PIs

• RTV 100–400 mg per day in one or two divided doses (refer to other PI sections for specific dosing recommendations)

Tablet

• Take with food

Capsule or Oral Solution

• To improve tolerability, take with food, if possible.

Standard Adult Doses of LPV/r (Kaletra)

• LPV/r 400 mg/100 mg twice daily, or
• LPV/r 800 mg/200 mg once daily

Tablets

• Take without regard to food.

Oral Solution

• Take with food.

With EFV or NVP in PI-Naive or PI-Experienced Patients

• LPV/r 500 mg/125 mg tablets twice daily without regard to meals (use a combination of two LPV/r 200 mg/50 mg tablets and one LPV/r 100 mg/25 mg tablet), or
• LPV/r 520 mg/130 mg oral solution (6.5 mL) twice daily with food

Pregnancy

PKs in Pregnancy

• Lower RTV levels are seen during pregnancy than during postpartum, which may reduce the pharmaco-enhancing effect of RTV in pregnancy.

RTV Dosing in Pregnancy

• No dose adjustment is necessary when RTV is used as booster.

LPV/r Dosing in Pregnancy

• Once-daily dosing is not recommended during pregnancy.
• Some experts recommend that an increased dose (i.e., LPV/r 600 mg/150 mg twice daily without regard to meals or LPV/r 500 mg/125 mg twice daily without regard to meals) should be used in the second and third trimesters of pregnancy, especially in patients who are PI-experienced and in those who start treatment during pregnancy with a baseline viral load >50 copies/mL.
• When standard dosing is used, monitor virologic response and, if possible, LPV drug levels.

For guidance about use of combination products in pregnancy, please see the specific sections on other components (i.e., LPV/r).

Low placental transfer to fetus.^b

No evidence of increased risk of human teratogenicity (can rule out 1.5-fold increase in overall birth defects).

RTV should only be used as low-dose booster for other PIs.

RTV oral solution contains 43% alcohol and, therefore, is not recommended for use during pregnancy because no safe level of alcohol exposure during pregnancy is known. LPV/r oral solution contains 42% alcohol and 15% propylene glycol and is not recommended for use in pregnancy.

Once-daily LPV/r dosing is not recommended during pregnancy.

December 30, 2021