Antiretroviral Treatments
| ANTIRETROVIRAL TREATMENTS | ||||
|---|---|---|---|---|
| Generic & Class | Brand & Company | Strength | Formulations | Usual Dose |
| CCR5 Co-receptor Antagonists | ||||
| maraviroc (MVC) | Selzentry
(Pfizer) |
150mg, 300mg | tabs | Adults: Swallow whole. ≥16yrs: Concomitant CYP3A inhibitors
(eg, PIs except tipranavir/ritonavir, delavirdine, ketoconazole, itraconazole,
clarithromycin, nefazodone, telithromycin) (with or without a CYP3A inducer): 150mg twice
daily. Concomitant tipranavir/ritonavir, nevirapine, raltegravir, NRTIs, enfuvirtide: 300mg
twice daily. Concomitant CYP3A inducers (efavirenz, rifampin, etravirine, carbamazepine,
phenobarbital, phenytoin) (without a strong CYP3A inhibitor): 600mg twice daily.
ESRD (CrCl <30mL/min) (without potent CYP3A inhibitors or inducers): reduce dose from
300mg twice daily to 150mg twice daily if postural hypotension occurs.
Children: <16yrs: not recommended. |
| Fusion Inhibitors | ||||
| enfuvirtide (ENF, T |
Fuzeon
(Roche) |
90mg/mL | pwd for SC inj after reconstitution | Adults: Give by SC inj into upper arm, anterior thigh, or abdomen
(not into moles, scar tissue, bruises, or navel). ≥16yrs: 90mg twice daily.
Children: 6–16yrs: limited data available; doses of 2mg/kg (max 90mg) twice daily have been used. |
| HIV-1 Integrase Strand Transfer Inhibitors | ||||
| raltegravir potassium (RAL) | Isentress
(Merck) |
25mg, 100mg+ | chew tabs | Adults: >16yrs: 400mg twice daily (avoid dosing prior to
dialysis). Concomitant rifampin: 800mg twice daily.
Children: <2yrs: not recommended. 2–<6yrs (and ≥10kg): use chew tabs and base dose on weight. 6–<12yrs: one 400mg film-coated tab twice daily or use chew tabs and base dose on weight; if 10–<14kg: 75mg twice daily; 14–<20kg: 100mg twice daily; 20–<28kg: 150mg twice daily; 28–<40kg: 200mg twice daily; ≥40kg: 300mg twice daily. Chew tab max dose: 300mg twice daily. ≥12yrs: one 400mg film-coated tab twice daily. |
| 400mg | tabs | |||
| Non-nucleoside Reverse Transcriptase Inhibitors (NNRTIs) | ||||
| delavirdine mesylate (DLV) | Rescriptor
(Pfizer) |
100mg, 200mg | tabs | Adults: Swallow whole or may disperse 100mg tabs in ≥3oz
water and drink. ≥16yrs: 400mg 3 times daily.
Children: <16yrs: not recommended. |
| efavirenz (EVF) | Sustiva
(Bristol Myers-Squibb) |
50mg, 200mg | caps | Adults and Children: Give once daily on an empty stomach, preferably at bedtime. Consider pretreating with antihistamine (for children) or steroid to minimize rash. <3yrs: not recommended. ≥3yrs (10kg to <15kg): 200mg; (15kg to <20kg): 250mg; (20kg to <25kg): 300mg; (25kg to <32.5kg): 350mg; (32.5kg to <40kg): 400mg; (≥40kg) and adults: 600mg. Concomitant voriconazole: increase voriconazole maintenance dose to 400mg every 12 hours and decrease efavirenz dose to 300mg once daily using capsule form. Concomitant rifampin (patient >50kg): increase efavirenz dose to 800mg once daily. |
| 600mg | tabs | |||
| etravirine (ETR) | Intelence
(Tibotec) |
25mg+, 100mg, 200mg | tabs | Adults: Take after meals. May disperse tabs in water and drink.
200mg twice daily.
Children: Take after meals. May disperse tabs in water and drink. <6yrs or <16kg: not established. ≥6yrs: ≥16kg–<20kg: 100mg twice daily. ≥20kg–<25kg: 125mg twice daily. ≥25kg–<30kg: 150mg twice daily. ≥30kg: 200mg twice daily. |
| nevirapine (NVP) | Viramune
(Boehringer Ingelheim) |
200mg+ | tabs | Adults: ≥16yrs: Initially 200mg once daily for
14 days. If no rash occurs, increase to 200mg twice daily. If mild-to-moderate rash
occurs during the 14 Children: <15days: not recommended. For oral susp: use dosing syringe or cup: ≥15days: initially 150mg/m² once daily for 14 days; if no rash occurs increase to 150mg/m² twice daily. If mild-to-moderate rash occurs during the 14 |
| 50mg/5mL | oral susp | |||
| Viramune XR
(Boehringer Ingelheim) |
400mg | ext-rel tabs | Adults: Swallow whole. Initially Viramune 200mg once daily for 14 days, then
Viramune XR 400mg once daily. If mild-to-moderate rash develops during the 14 Children: Not recommended. |
|
| rilpivirine | Edurant
(Janssen) |
25mg | tabs | Adults: 25mg once daily with a meal.
Children: Not recommended. |
| Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs) | ||||
| abacavir sulfates (ABC) | Ziagen
(GlaxoSmithKline) |
300mg | tabs | Adults: >16yrs: 300mg twice daily or 600mg once
daily. Mild hepatic impairment: 200mg twice daily.
Children: <3 months: not recommended. ≥3 months–16yrs: 8mg/kg twice daily; max 300mg twice daily. |
| 20mg/mL | oral soln1 | |||
| abacavir sulfate (ABC)/ lamivudine (3TC) |
Epzicom
(GlaxoSmithKline) |
ABC/3TC: 600mg/300mg |
tabs | Adults: >18yrs: 1 tab daily. Hepatic or renal impairment (CrCl
<50mL/min): not recommended.
Children: ≤18yrs: not recommended. |
| abacavir sulfate (ABC)/ lamivudine (3TC)/ zidovudine (ZDV) |
Trizivir
(GlaxoSmithKline) |
ABC/3TC/ZDV: 300mg/150mg/300mg |
tabs | Adults: <40kg: not recommended. ≥40kg: 1 tab twice daily. |
| didanosine (ddI) | Videx EC
(Bristol Myers-Squibb) |
125mg, 200mg, 250mg, 400mg | e-c del-rel caps | Adults and Children: Take once daily on an empty stomach; swallow whole. <20kg: use oral soln. 20kg to <25kg: 200mg. 25kg to <60kg: 250mg. ≥60kg: 400mg. Renal impairment (CrCl 30–59mL/min): <60kg: 125mg. ≥60kg: 200mg. CrCl 10–29mL/min: 125mg. CrCl <10mL/min or dialysis: <60kg: use oral soln; ≥60kg: 125mg. |
| Videx Pediatric Pwd for Oral Soln
(Bristol Myers-Squibb) |
4g | pediatric pwd for oral soln after reconstitution | Adults: Take on an empty stomach. <60kg: 125mg twice daily.
≥60kg: 200mg twice daily. If once daily dosing required: <60kg: 250mg. ≥60kg: 400mg.
Renal impairment (CrCl 30–59mL/min): <60kg: 150mg once daily or 75mg twice daily;
≥60kg: 200mg once daily or 100mg twice daily; CrCl 10–29mL/min: <60kg: 100mg once
daily; ≥60kg: 150mg once daily; CrCl <10mL/min or dialysis: <60kg: 75mg once
daily; ≥60kg: 100mg once daily.
Children: See literature. Take on empty stomach. <2 weeks: not recommended. 2 weeks–8 months: 100mg/m² twice daily. ≥8 months: 120mg/m² twice daily. Renal impairment: consider reducing dose and/or increasing dosing interval. |
|
| emtricitabine (FTC) | Emtriva
(Gilead Sciences) |
200mg | caps | Adults: ≥18yrs: 200mg once daily. Renal impairment (CrCl
30–49mL/min): 200mg every 48hrs; (CrCl 15–29mL/min): 200mg every 72hrs; (CrCl
<15mL/min or dialysis): 200mg every 96hrs.
Children: <3months: not recommended. 3months–17yrs: ≤33kg: use soln form. >33kg: 200mg once daily. Renal impairment: reduce dose or prolong dosing interval (see literature). |
| 10mg/mL | oral soln | Adults: ≥18yrs: 240mg (24mL) once daily. Renal impairment:
(CrCl 30–49mL/min): 120mg (12mL) once daily; (CrCl 15–29mL/min): 80mg (8mL) once
daily; (CrCl <15mL/min): 60mg (6mL) once daily.
Children: <3months: 3mg/kg once daily. 3months–17yrs: 6mg/kg [max 240mg (24mL)] once daily. >33kg: may use cap form. Renal impairment: reduce dose or prolong dosing interval (see literature). |
||
| emtricitabine (FTC)/ tenofovir disoproxil fumarate (TDF) | Truvada
(Gilead Sciences) |
FTC/TDF:
200mg/300mg |
tabs | Adults: ≥18yrs (CrCl ≥50mL/min): 1 tab once daily.
Renal impairment: CrCl 30–49mL/min: 1 tab every 48hrs; CrCl <30mL/min,
hemodialysis: not recommended.
Children: <18yrs: not recommended. |
| lamivudine (3TC) | Epivir
(GlaxoSmithKline) |
150mg+, 300mg | tabs | Adults and Children: ≤3months: not recommended. 3months–16yrs: 4mg/kg (max 150mg) twice daily; renal impairment: reduce dose or prolong dosing interval. ≥16yrs, CrCl ≥50mL/min: 300mg once daily or 150mg twice daily; CrCl 30–49mL/min: 150mg once daily; CrCl 15–29mL/min: 150mg for 1st dose then 100mg once daily; CrCl 5–14mL/min: 150mg for 1st dose then 50mg once daily; CrCl <5mL/min: 50mg for 1st dose then 25mg once daily. |
| 10mg/mL | oral soln | |||
| lamivudine (3TC)/ zidovudine (ZDV) | Combivir
(GlaxoSmithKline) |
3TC/ZDV:
150mg/300mg |
tabs | Adults: 1 tab twice daily. Hepatic or renal impairment (CrCl
<50mL/min): not recommended.
Children: Not recommended. |
| stavudine (d4T) | Zerit
(Bristol Myers-Squibb) |
15mg, 20mg, 30mg, 40mg | caps | Adults: ≥60kg: 40mg every 12hrs; <60kg: 30mg every
12hrs. Withdraw drug if peripheral neuropathy occurs; after complete resolution, may
restart at 20mg every 12hrs for patients ≥60kg, or 15mg every 12hrs for patients
<60kg; if neuropathy recurs consider discontinuing permanently. Renal impairment:
≥60kg (CrCl 26–50mL/min): 20mg every 12hrs; (CrCl 10–25mL/min): 20mg every 24hrs.
<60kg (CrCl 26–50mL/min): 15mg every 12hrs; (CrCl 10–25mL/min): 15mg every 24hrs.
Hemodialysis: ≥60kg: 20mg every 24hrs; <60kg: 15mg every 24hrs. Coincide dose for
end of dialysis and give at same time of day on non-dialysis days.
Children: ≤13 days: 0.5mg/kg every 12hrs. ≥14 days: (<30kg): 1mg/kg every 12hrs. ≥30kg: as adult. Withdraw drug if peripheral neuropathy occurs; after complete resolution, may restart at ½ recommended dose; if neuropathy recurs consider discontinuing permanently. Renal impairment: reduce dose or increase dosing interval. |
| 1mg/mL | pwd for oral soln after reconstitution | |||
| tenofovir disoproxil fumarate (TDF) | Viread
(Gilead Sciences) |
150mg, 200mg, 250mg, 300mg | tabs | Adults: ≥12yrs (≥35kg): 300mg once daily. Renal impairment: CrCl 30–49mL/min: 300mg every 48hrs; CrCl 10–29mL/min: 300mg every 72–96hrs; hemodialysis: 300mg once per week or after a total of 12hrs of dialysis; CrCl <10mL/min: not recommended. |
| 40mg/g | oral pwd | Children: <2yrs: not recommended. Mix oral pwd with 2–4oz of soft food not requiring chewing (eg, applesauce, baby food, yogurt). ≥2yrs: 8mg/kg once daily; max 300mg/day. ≥17kg: may use tablets if able to swallow. 17–<22kg: 150mg once daily. 22–<28kg: 200mg once daily. 28–<35kg: 250mg once daily. ≥35kg: 300mg once daily. | ||
| zidovudine (ZDV) | Retrovir
(GlaxoSmithKline) |
100mg | caps | Adults: ≥18yrs: 600mg daily in divided doses. End-stage renal disease on dialysis: 100mg every 6–8hrs. Vertical transmission, severe anemia and/or neutropenia: see literature. |
| 300mg | tabs | Children: <6 weeks and/or for vertical transmission: see literature. 6 weeks to <18yrs: (4 to <9kg): 24mg/kg/day (12mg/kg twice daily or 8mg/kg 3 times daily); (≥9 to <30kg): 18mg/kg/day (9mg/kg twice daily or 6mg/kg 3 times daily); (≥30kg): 600mg/day (300mg twice daily or 200mg 3 times daily). Alternative dosing based on BSA: 480mg/m²/day (240mg/m² twice daily or 160mg/m² 3 times daily). | ||
| 50mg/5mL | syrup | |||
| 10mg/mL | soln for IV inj after dilution | Adults: Give by IV infusion over 1 hour; use only until oral
therapy can be given. 1mg/kg 5–6 times daily. End-stage renal disease on dialysis: 1mg/kg
every 6–8hrs. Vertical transmission, severe anemia and/or neutropenia: see literature.
Children: Vertical transmission: see literature. |
||
| Protease Inhibitors (PIs) | ||||
| atazanavir sulfate (ATV) | Reyataz
(Bristol Myers-Squibb) |
100mg, 150mg, 200mg, 300mg | caps | Adults: Take with food. Therapy naive: atazanavir 300mg +
ritonavir 100mg both once daily; atazanavir 400mg once daily if unable to tolerate
ritonavir. Therapy experienced: atazanavir 300mg + ritonavir 100mg both once daily.
Concomitant efavirenz (must also give ritonavir, not for therapy-experienced): atazanavir
400mg + ritonavir 100mg both once daily + efavirenz 600mg (on an empty stomach at bedtime);
Concomitant tenofovir (must also give ritonavir): may give atazanavir 300mg + ritonavir
100mg + tenofovir 300mg all once daily. ESRD with hemodialysis: therapy-naive: atazanavir
300mg + ritonavir 100mg. Moderate hepatic impairment: 300mg once daily.
Pregnancy (2nd or 3rd trimester): treatment-experienced plus concomitant H2-blocker or tenofovir:
atazanvir 400mg + ritonavir 100mg, both once daily. All other pregnant patients: no dose adjustments needed.
Postpartum period: no dose adjustments needed; monitor for adverse events during first 2 months after delivery.
Children: See literature. Take with food. <6yrs: not recommended. 6–18yrs: (15–<20kg): atazanavir 150mg + ritonavir 100mg; (20–<40kg): atazanavir 200mg + ritonavir 100mg; (≥40kg): atazanavir 300mg + ritonavir 100mg; all: single daily dose. Treatment-naive: ≥13yrs and ≥40kg who are unable to tolerate ritonavir: atazanavir 400mg once daily. For patients ≥13yrs and ≥40kg receiving concomitant tenofovir, H2-blockers, or PPIs: give atazanavir with ritonavir. |
| darunavir ethanolate (DRV) | Prezista
(Tibotec) |
75mg, 150mg, 400mg, 600mg, 800mg | tabs | Adults: Take with food. ≥18yrs: Treatment-naive and treatment-experienced
with no darunavir resistance associated substitutions: 800mg once daily with ritonavir 100mg once
daily. Treatment-experienced with at least one darunavir resistance associated substitution: 600mg
twice daily with ritonavir 100mg twice daily. Severe hepatic impairment: not recommended.
Children: <3yrs: not recommended. Take with food. Use oral susp if unable to swallow tabs. Treatment-experienced: ≥3yrs to <18yrs: ≥10kg–<11kg: 200mg twice daily with ritonavir 32mg twice daily; ≥11kg–<12kg: 220mg twice daily with ritonavir 32mg twice daily; ≥12kg–<13kg: 240mg twice daily with ritonavir 40mg twice daily; ≥13kg–<14kg: 260mg twice daily with ritonavir 40mg twice daily; ≥14kg–<15kg: 280mg twice daily with ritonavir 48mg twice daily; ≥15–<30kg: 375mg (3.8mL of susp) twice daily with ritonavir 50mg twice daily; ≥30kg–<40kg: 450mg (4.6mL of susp) twice daily with ritonavir 60mg twice daily; ≥40kg: 600mg twice daily with ritonavir 100mg twice daily. Severe hepatic impairment: not recommended. |
| 100mg/mL | oral susp | |||
| fosamprenavir calcium (FOS-APV) | Lexiva
(GlaxoSmithKline) |
700mg | tabs | Adults: Oral susp: take without food; if emesis occurs within 30
minutes after dosing, re-dose. Therapy-naive: 1.4g twice daily; or fosamprenavir 1.4g +
ritonavir 200mg once daily; or fosamprenavir 1.4g + ritonavir 100mg once daily; or
fosamprenavir 700mg + ritonavir 100mg twice daily. Protease-inhibitor-experienced:
fosamprenavir 700mg + ritonavir 100mg twice daily. Hepatic dysfunction: see literature for
dose adjustments.
Children: <4wks: not recommended. Oral susp: take with food; if emesis occurs within 30 minutes after dosing, re-dose. Therapy-naïve (≥4wks): <11kg: fosamprenavir 45mg/kg + ritonavir 7mg/kg; 11kg–<15kg: fosamprenavir 30mg/kg + ritonavir 3mg/kg; 15kg–<20kg fosamprenavir 23mg/kg + ritonavir 3mg/kg; ≥20kg: fosamprenavir 18mg/kg + ritonavir 3mg/kg; or 2–5yrs: fosamprenavir 30mg/kg twice daily. Therapy-experienced (≥6mos): <11kg: fosamprenavir 45mg/kg + ritonavir 7mg/kg; 11kg–<15kg: fosamprenavir 30mg/kg + ritonavir 3mg/kg; 15kg–<20kg fosamprenavir 23mg/kg + ritonavir 3mg/kg; ≥20kg: fosamprenavir 18mg/kg + ritonavir 3mg/kg. For all: do not exceed the adult dosage (see literature). Alternative oral tabs regimen: see literature. |
| 50mg/mL | oral susp | |||
| indinavir sulfate (IDV) | Crixivan
(Merck) |
100mg, 200mg, 400mg | caps | Adults: Take with water on an empty stomach or with a light meal.
800mg every 8hrs. Concomitant rifabutin: 1g every 8hrs and reduce rifabutin dose by
½. Concomitant ketoconazole, itraconazole, delavirdine, or hepatic insufficiency:
600mg every 8hrs.
Children: Not recommended. Take with water on an empty stomach or with a light meal. 3–18yrs: 500mg/m² every 8hrs has been used; see literature. |
| lopinavir (LPV)/ ritonavir (RTV) | Kaletra
(AbbVie) |
LPV/RTV: 100mg/25mg, 200mg/50mg | tabs | Adults: Swallow tabs whole; take oral soln with food.
Treatment-naive: Lopinavir/ritonavir 400mg/100mg twice daily or lopinavir/ritonavir
800mg/200mg once daily. Treatment-experienced: Lopinavir/ritonavir 400mg/100mg twice daily.
Concomitant efavirenz, nevirapine, fosamprenavir (without ritonavir) or nelfinavir in
treatment-experienced patients when reduced susceptibility to lopinavir is suspected:
600mg/150mg twice daily. Concomitant efavirenz, nevirapine, amprenavir or nelfinavir:
533mg/133mg (6.5mL) twice daily.
Children: May use tabs if able to swallow whole and ≥15kg. <14days: not recommended. Take twice daily. 14days–6mo: soln: lopinavir/ritonavir 16mg/4mg per kg. ≥6mo–18yrs: (<15kg): 12mg/3mg per kg; (15–40kg): 10mg/2.5mg per kg; tabs: (15–25kg): 200mg/50mg (2 tabs); (25–35kg): 300mg/75mg (3 tabs); (>35kg): 400mg/100mg twice daily (max). Concomitant efavirenz, nevirapine or fosamprenavir: (<15kg): 13mg/3.25mg per kg; (15–45kg): 11mg/2.75mg per kg; (>45kg): max oral soln: 533mg/133mg; max tabs 400mg/100mg or 600mg/150mg twice daily. |
| LPV/RTV: 80mg/20mg per mL | oral soln2,5 | |||
| nelfinavir mesylate (NFV) | Viracept
(Agouron) |
250mg, 625mg | tabs | Adults and Children: Take with food. May dissolve tab and mix in small amount of water; powder may be mixed with a small amount of non-acidic food or beverage. <2yrs: not recommended. 2–13yrs: 45–55mg/kg twice daily or 25–35mg/kg 3 times daily; max 2.5g/day. >13yrs: 1.25g twice daily or 750mg 3 times daily. Reduce concomitant rifabutin dose by ½ and give nelfinavir 1.25g twice daily. |
| 50mg/g | oral pwd3 | |||
| ritonavir (RTV) | Norvir
(AbbVie) |
100mg | tabs, soft gel caps2,5 | Adults: Take with meals. Initially at least 300mg twice daily, increase every 2–3 days by 100mg twice daily to 600mg twice daily. Concomitant other PIs (eg, amprenavir, atazanavir, darunavir, fosamprenavir, saquinavir, tipranavir); reduce ritonavir dose. See literature. |
| 80mg/mL | oral soln2 | Children: Give with food. <1month: not recommended. >1month: initially 250mg/m² twice daily; increase every 2–3 days by 50mg/m² twice daily to 350–400mg/m² twice daily; max 600mg twice daily. | ||
| saquinavir mesylate (SQV) | Invirase
(Genentech) |
500mg | tabs | Adults: Take within 2hrs after a meal. ≥16yrs: saquinavir 1g twice daily + ritonavir 100mg twice daily (taken at same time). |
| 200mg | hard gel caps | Children: <16yrs: not recommended. | ||
| tipranavir (TPV) | Aptivus
(Boehringer Ingelheim) |
250mg | soft gel caps2 | Adults: Swallow caps whole. Tipranavir 500mg +
ritonavir 200mg twice daily.
Children: <2yrs: not recommended. Use oral soln if unable to swallow caps. 2–18yrs: Tipranavir 14mg/kg + ritonavir 6mg/kg (or 375mg/m² + ritonavir 150mg/m²) twice daily; max tipranavir 500mg + ritonavir 200mg twice daily. Intolerance or toxicity (if virus not resistant to multiple PIs): may reduce dose to tipranavir 12mg/kg + ritonavir 5mg/kg (or 290mg/m² + ritonavir 115mg/m²) twice daily. |
| 100mg/mL | oral soln4 | |||
| Multiclass Fixed-Dose Combination | ||||
| efavirenz (EVF)/ emtricitabine (FTC)/ tenofovir disoproxil fumarate (TDF) |
Atripla
(Bristol-Myers Squibb and Gilead) |
EVF/FTC/TDF: 600mg/200mg/300mg |
tabs | Adults: ≥18yrs: Take on empty stomach. 1 tablet once daily
(preferably at bedtime).
Children: <18yrs: not recommended. |
| emtricitabine (FTC)/ rilpivirine/ tenofovir disoproxil fumarate (TDF) |
Complera
(Gilead Sciences) |
FTC/rilpivirine/TDF: 200mg/25mg/300mg |
tabs | Adults: ≥18yrs: Take with a meal. 1 tablet once daily. Renal
(impairment CrCl<50mL/min): not recommended.
Children: <18yrs: not recommended. |
| elvitegravir/ cobicistat/ emtricitabine (FTC)/ tenofovir disoproxil fumarate (TDF) |
Stribild
(Gilead Sciences) |
elvitegravir/ cobicistat/FTC/TDF: 150mg/150mg/ 200mg/300mg |
tabs | Adults: ≥18yrs: Take 1 tablet once daily with food. Renal
impairment (CrCl <70mL/min): do not initiate; if CrCl declines to <50mL/min during
therapy: discontinue.
Children: <18yrs: not recommended. |
| NOTES | ||||
|
+scored; ext-rel: extended release 1Contains parabens, propylene glycol 2Contains alcohol 3Contains phenylalanine 11.2mg/g 4Contains Vit. E 116 IU/mL 5Keep in refrigerator (Rev. 4/2013) |
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