Labeling for FDA-approved Antiretrovirals Used in the Treatment of Infants and Children with HIV Infection

Following is a list of antiretroviral drugs with their current pediatric use labeling, as well as notations from U.S. Food and Drug Administration (FDA) regarding special information about use of these drugs in infants and children.

Nucleoside Reverse Transcriptase Inhibitors (NRTIs)

Brand Name	Generic Name(s)	Manufacturer Name	Pediatric Use Labeling	Special Information
Combivir	lamivudine [3TC] and zidovudine [AZT]	GlaxoSmithKline	>12 yr: Tablet: 1 tablet (300 mg zidovudine/ 150 mg lamivudine) twice daily	Use is contraindicated in children <12 yr. due to fixed dosage form that cannot be adjusted for this population
Emtriva	emtricitabine; FTC	Gilead Sciences	0-3 months: Solution: 3 mg/kg/day 3 months-17 yr. Solution: 6 mg/kg once daily >33 kg: Capsule: 200 mg once daily Solution: 6 mg/kg once daily	Maximum dosage: Solution: 240 mg/day
Epivir	lamivudine, 3TC	GlaxoSmithKline	3 months-16 yr: Solution or tablet: 4 mg/kg twice daily >16yr: Refer to adult dosing	Maximum dosage: 150 mg twice daily
Epzicom	abacavir and lamivudine	GlaxoSmithKline	Safety and effectiveness in pediatric patients not established	Use is contraindicated in children <12 yr. due to fixed dosage form that cannot be adjusted for this population
Hivid	zalcitabine; dideoxycytidine; ddC	Hoffmann-La Roche	Safety and effectiveness in patients <13 years not established
Retrovir	Zidovudine; azidothymidine; AZT	GlaxoSmithKline	6 weeks-12 yr: Tablet/capsule/solution: 160 mg/m² every 8 hours^† For prevention of maternal-fetal neonatal transmission <12 hours after birth-6 weeks: Solution: 2 mg/kg every 6 hours until 6 weeks of age IV: 1.5 mg/kg infused over 30 minutes every 6 hours until 6 weeks of age	Maximum dosage: 200 mg every 8 hours Note different dosages for treatment vs. prevention of maternal-fetal transmission IV form used if neonate unable to receive oral form
Trizivir	abacavir, zidovudine, and lamivudine	GlaxoSmithKline	Safety and efficacy not established in pediatric patients, and should not be administered to adolescents weighing < 40 kg
Truvada	tenofovir disoproxil/emtricitabine	Gilead Sciences, Inc.	Safety and efficacy not established in pediatric patients <18 years
Videx EC	enteric coated didanosine	Bristol Myers-Squibb	Safety and efficacy not established in pediatric patients
Videx	didanosine, ddI, dideoxyinosine	Bristol Myers-Squibb	2 weeks-8 months: Powder for oral solution: 100 mg/m² twice daily; 50 mg/m² may be used for infants 2 weeks-4 months ^† >8 months: recommended 120 mg/m² twice daily; dosing range 90-150 mg/m^{2 †}	Dosing recommendations for patients less than 2 weeks of age cannot be made because the pharmacokinetics in these children are too variable to determine appropriate dose. Patients with CNS disease may require higher doses
Viread	tenofovir disoproxil fumarate	Gilead	Safety and effectiveness in patients <18 years not established	No pediatric studies have been documented to date
Zerit	stavudine; d4T	Bristol Myers-Squibb	Birth-13 days: Tablet/oral solution: 0.5 mg/kg/dose every 12 hours >14 days and <30 kg: Tablet/oral solution: 1 mg/kg/dose every 12 hours >30 kg to < 60 kg: 30 mg every 12 hours >60 kg: 40 mg every 12 hours
Ziagen	abacavir	GlaxoSmithKline	3 months-16 yr: Tablet/oral solution: 8 mg/kg twice daily	Maximum dosage: 300 mg twice daily

Non-nucleoside Reverse Transcriptase Inhibitors (NNRTIs)

Brand Name	Generic Name	Manufacturer Name	Pediatric Use Labeling	Special Information
Rescriptor	delavirdine	Pfizer	Safety and effectiveness not established in HIV-1–infected individuals <16 years
Sustiva	efavirenz	Bristol Myers-Squibb	>3 yr.: Tablet/capsule: 10-<15 kg: 200 mg once daily 15-<20 kg: 250 mg once daily 20-<25 kg: 300 mg once daily 25-<32.5 kg: 350 once daily 32.5-<40 kg: 400 mg once daily >40 kg: 600 mg once daily	Dosing recommended at bedtime to limit CNS effects
Viramune	nevirapine	Boehringer Ingelheim	2 months-<8 yr: Tablet/oral suspension: 4 mg/kg once daily for 14 days, then 7 mg/kg twice daily >8 yr: Tablet/oral suspension: 4 mg/kg once daily for 14 days, then 4 mg/kg twice daily	Maximum dosage 2 months-<8 yr.: 400 mg/day (200 mg twice daily) >8 yr.: 400 mg/day (200 mg twice daily)

Protease Inhibitors (PIs)

Brand Name	Generic Name(s)	Manufacturer Name	Pediatric Use Labeling	Special Information
Agenerase	amprenavir	GlaxoSmithKline	4-16 yr. weighing <50 kg: Capsule: 20 mg/kg twice daily or 15 mg/kg three times daily Solution: 22.5 mg/kg twice daily or 17 mg/kg three times daily >13 yrs. weighing >50 kg: Capsule: 1200 mg twice daily Solution: 1400 mg twice daily	Maximum dosage: Capsule: 2400 mg/day Solution: 2800 mg/day Capsules and oral solution are not interchangeable on a mg per mg basis
Aptivus	tipranavir	Boehringer Ingelheim	Safety and effectiveness in pediatric patients not established.
Invirase	saquinavir	Hoffmann-La Roche	Safety and effectiveness in patients <16 years not established
Kaletra	lopinavir and ritonavir	Abbott Laboratories	Patients receiving nevirapine or efavirenz with Kaletra should have their dose of Kaletra increased. 6 months-12 yr: Tablet/capsule/solution: 7-<15 kg: 12 mg/kg twice daily (13/3.25 mg/kg with nevirapine) 15-40 kg: 10 mg/kg twice daily (11/2.75 mg/kg with nevirapine) >40 kg or >12 yr: lopinavir 400 mg/ ritonavir 100 mg twice daily (533/133 mg with nevirapine)	Maximum dosage: lopinavir 400 mg/ ritonavir 100 mg for patients who are not receiving nevirapine or efavirenz
Lexiva	fosamprenavir	GlaxoSmithKline	Therapy-Naïve 2 to 5 Years of Age: Lexiva Oral Suspension 30 mg/kg twice daily, not to exceed the adult dose of LEXIVA 1,400 mg twice daily. Therapy-Naïve > 6 Years of Age: Either Lexiva Oral Suspension 30mg/kg twice daily not to exceed the adult dose of Lexiva 1,400 mg twice daily or Lexiva Oral Suspension 18 mg/kg plus ritonavir 3 mg/kg twice daily not to exceed the adult dose of Lexiva 700 mg plus ritonavir 100 mg twice daily. Therapy-Experienced > 6 Years of Age: Lexiva Oral Suspension 18 mg/kg plus ritonavir 3 mg/kg administered twice daily not to exceed the adult dose of LEXIVA 700 mg plus ritonavir 100 mg twice daily. Lexiva Oral Suspension 18 mg/kg plus ritonavir 3 mg/kg administered twice daily not to exceed the adult dose of Lexiva 700 mg plus ritonavir 100 mg twice daily. When administered without ritonavir, the adult regimen of Lexiva Tablets 1,400 mg twice daily may be used for pediatric patients weighing at least 47 kg. When administered in combination with ritonavir, Lexiva Tablets may be used of pediatric patients weighing at least 39 kg; ritonavir capsules may be used for pediatric patients weighing at least 33 kg.	The recommended dosage of Lexiva in patients > 2 years of age should be calculated based on body weight (kg) and should not exceed the recommended adult dose. The data are insufficient to recommend: (1) once-daily dosing of Lexiva alone or in combination with ritonavir, and (2) any dosing of Lexiva in therapy-experienced patients 2 to 5 years of age.
Norvir	ritonavir	Abbott Laboratories	>1 month: 350-400 mg/m² twice daily ^† Initiate dose at 250 mg/m² twice daily and titrate upward every 2-3 days by 50 mg/m² twice daily ^†	Maximum dosage: 600 mg twice daily Lower doses have been used to boost other protease inhibitors but the RTV doses used for boosting haven't been specifically approved in children
Prezista	darunavir	Tibotec, Inc.	Safety and effectiveness in pediatric patients not established
Reyataz	atazanavir	Bristol-Myers Squibb	Safety and efficacy not established in pediatric patients
Viracept	nelfinavir	Agouron Pharmaceuticals	2-13 yr: Tablets/powder for: 45-55 mg/kg twice daily or 25-35 mg/kg three times daily	Maximum dosage: 2500 mg/day 250 mg tablets are interchangeable with oral powder (625 mg tablets are not) Reliable dosing recommendations could not be determined in patients < 2 years of age

Fusion Inhibitors

Brand Name	Generic Name	Manufacturer Name	Pediatric Use Labeling	Special Information
Fuzeon	enfuvirtide	Hoffmann-La Roche & Trimeris	6-16 yr: Subcutaneous injection: 2 mg/kg twice daily	Maximum dosage: 90 mg twice daily Rotate injection sites

* "While some of these drugs may, in practice, be used in the treatment of children of various ages, the sponsors have not submitted adequate data to support a labeled pediatric indication at this time." -- FDA Statement

†Body surface area can be calculated using the following equation:

08/21/07

Source
US Food and Drug Administration (FDA).