| 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, NRTIs, enfuvirtide: 300mg twice daily.
Concomitant CYP3A inducers (efavirenz, rifampin, carbamazepine, phenobarbital, phenytoin)
(without a strong CYP3A inhibitor): 600mg twice daily.
Children: <16yrs: not recommended. |
| Fusion Inhibitors |
| enfuvirtide (ENF, T-20) |
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) |
400mg |
tabs |
Adults: >16yrs: 400 mg twice daily (avoid dosing prior to
dialysis). Concomitant rifampin: 800mg twice daily.
Children: <16yrs: not recommended. |
| 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, 100mg, 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): 200 mg;
(15kg to <20kg): 250mg; (20kg to <25kg): 300mg; (25kg to <32.5kg): 350mg; (32.5kg
to <40kg): 400mg; (≥40kg) and adults: 600mg. |
| 600mg |
tabs |
| etravirine (ETR) |
Intelence
(Tibotec) |
100mg |
tabs |
Adults: Take after meals. May disperse tabs in water and drink.
200mg twice daily.
Children: Not recommended. |
| 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-day lead in period, do not give twice-daily regimen until
rash has resolved; lead-in dosing regimen should not be continued beyond
28 days, consider alternative regimen. If severe rash or hepatic event occurs,
discontinue permanently. Max 400mg/day. Retitrate if stopped for >7 days.
Hemodialysis: give additional nevirapine 200mg dose after dialysis.
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-day lead in period, do not give twice-daily regimen until rash has
resolved; lead-in dosing regimen should not be continued beyond 28 days,
consider alternative regimen. If severe rash or hepatic event occurs, discontinue
permanently. Max 400mg/day. Retitrate if stopped for >7 days. |
| 50mg/5mL |
oral susp |
| 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.
Children: Not recommended. |
| 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) |
300mg |
tabs |
Adults: ≥18yrs: 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.
Children: <18yrs: not recommended. |
| 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.
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). |
| 300mg |
tabs |
| 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.
Children: <6yrs: not recommended. 6–18yrs: Therapy-naive: 15–25kg:
atazanavir 150mg + ritonavir 80mg; 25–32kg: atazanavir 200mg + ritonavir 100mg; 32–39kg:
atazanavir 250mg + ritonavir 100mg; ≥39kg: atazanavir 300mg + ritonavir 100mg. If
≥13yrs and ≥39kg and unable to tolerate ritonavir: atazanavir 400mg once daily.
Therapy experienced: <25kg: not recommended. 25–32kg: atazanavir 200mg + ritonavir 100mg;
32–39kg: atazanavir 250mg + ritonavir 100mg; ≥39kg: atazanavir 300mg + ritonavir
100mg. All: single daily dose. |
| darunavir ethanolate (DRV) |
Prezista
(Tibotec) |
75mg, 300mg, 400mg, 600mg |
tabs |
Adults: Take with food. ≥18yrs: Treatment-naive: 800mg
once daily with ritonavir 100mg once daily. Treatment-experienced: 600mg twice daily with
ritonavir 100mg twice daily. Severe hepatic impairment: not recommended.
Children: <6yrs: not recommended. Take with food.
Treatment-experienced: ≥6yrs to <18yrs: ≥20kg–<30kg: 375mg twice daily
with ritonavir 50mg twice daily; ≥30kg–<40kg: 450mg twice daily with ritonavir
60mg twice daily; ≥40kg: 600mg twice daily with ritonavir 100mg twice daily. Severe
hepatic impairment: not recommended. |
| 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: <2yrs: not recommended. Oral susp: take with food; if emesis
occurs within 30 minutes after dosing, re-dose. Therapy-naive: 2–5yrs: 30mg/kg twice daily.
≥6yrs: fosamprenavir 30mg/kg twice daily; or fosamprenavir 18mg/kg + ritonavir 3mg/kg
twice daily. Therapy-experienced: ≥6yrs: fosamprenavir 18mg/kg + ritonavir 3mg/kg
twice daily. 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, 333mg, 400mg |
caps |
Adults: Take with water on an empty stomach or with a light meal.
800mg every 8hrs. Concomitant efavirenz: 1g 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
(Abbott) |
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. |
| 50mg/g |
oral pwd3 |
<2yrs: not recommended. 2–13yrs: 20–30mg/kg
3 times daily; max 750mg 3 times daily. >13yrs: 1.25g twice daily or 750mg
3 times daily. Reduce concomitant rifabutin dose by ½ and give nelfinavir 1.25g
twice daily. |
| ritonavir (RTV) |
Norvir
(Abbott) |
100mg |
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. May initiate alone, then
add nucleoside analogues before completing 2 weeks of ritonavir monotherapy. Concomitant
saquinavir: reduce ritonavir dose to 400mg twice daily. |
| 80mg/mL |
oral soln2 |
Children: Give with food. <2yrs: not
recommended. ≥2yrs: initially 250mg/m2 twice daily; increase every
2–3 days by 50mg/m2 twice daily to 400mg/m2 twice daily;
max 600mg twice daily. |
| saquinavir mesylate (SQV) |
Invirase
(Roche) |
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.<2yrs: not recommended. Use oral soln if unable to swallow caps. 2–18yrs:
Tipranavir 14mg/kg + ritonavir 6mg/kg 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 twice daily. |
| 100mg/mL |
oral soln4 |