APPENDIX: CHARACTERISTICS OF AVAILABLE ANTIRETROVIRAL DRUGS
Nucleoside Analogue Reverse Transcriptase Inhibitors*
Nucleoside Analogue Reverse Transcriptase Inhibitors*
*Information in this appendix is not all inclusive. Complete and detailed prescribing and toxicity information on these drugs is available from the drug companies and should be reviewed by the healthcare provider before prescribing these drugs.
Adolescents in early puberty (Tanner I-II) should be dosed using pediatric schedules, whereas those in late puberty (Tanner Stage V) should be dosed using adult schedules. Youth who are in the midst of their growth spurt (Tanner III females and Tanner IV males) should be closely monitored for medication efficacy and toxicity when choosing adult or pediatric dosing guidelines.
Didanosine (dideoxyinosine) (ddI), VIDEX ®
Preparations: Pediatric powder for oral solution (when reconstituted as solution containing antacid): 10 mg/mL; Chewable tablets with buffers: 25, 50, 100, and 150 mg; Buffered powder for oral solution: 100, 167, and 250 mg
Dosage: Neonatal dose (infants aged <90 days): 50 mg per m 2 of body surface area every 12 hours.
Pediatric usual dose: In combination with other antiretrovirals: 90 mg per m 2 of body surface area every 12 hours.
Pediatric dosage range: 90 to 150 mg per m 2 of body surface area every 12 hours. (Note: may need higher dose in patients with central nervous system disease.) Adolescent/Adult dose: Body weight >60 kg: 200 mg twice daily. Body weight <60 kg: 125 mg twice daily.
Major toxicities
Most frequent: Diarrhea, abdominal pain, nausea, and vomiting. Unusual (more severe): Peripheral neuropathy (dose related), electrolyte abnormalities, and hyperuricemia. Uncommon: Pancreatitis (dose related, less common in children than adults), increased liver enzymes, and retinal depigmentation.
Drug interactions
Special instructions
Lamivudine (3TC), EPIVIR ®
Preparations: Solution: 10 mg/mL; Tablets: 150 mg
Dosage Neonatal dose (infants aged <30 days): 2 mg per kg of body weight twice daily.
Pediatric dose: 4 mg per kg of body weight twice daily.
Adolescent/Adult dose: Body weight >50 kg: 150 mg twice daily. Body weight <50 kg: 2 mg per kg body weight twice daily.
Major toxicities Most frequent: Headache, fatigue, nausea, diarrhea, skin rash, and abdominal pain. Unusual (more severe): Pancreatitis (primarily seen in children with advanced HIV infection receiving multiple other medications), peripheral neuropathy, decreased neutrophil count, and increased liver enzymes.
Drug interactions
Special instructions
Stavudine (d4T), ZERIT ®
Preparations: Solution: 1 mg/mL; Capsules: 15, 20, 30, and 40 mg
Dosage Neonatal dose: Under evaluation in Pediatric AIDS Clinical Trial Group protocol 332.
Pediatric dose: 1 mg per kg of body weight every 12 hours (up to weight of 30 kg).
Adolescent/Adult dose: Body weight >60 kg: 40 mg twice daily. Body weight <60 kg: 30 mg twice daily.
Major toxicities
Most frequent: Headache, gastrointestinal disturbances, and skin rashes. Uncommon (more severe): Peripheral neuropathy and pancreatitis. Other: Increased liver enzymes.
Drug interactions
Special instructions
Zalcitabine (ddC), HIVID ®
Preparations: Syrup: 0.1 mg/mL (investigational); Tablets: 0.375 and 0.75 mg
Dosage Neonatal dose: Unknown.
Pediatric usual dose: 0.01 mg per kg of body weight every 8 hours.
Pediatric dosage range: 0.005 to 0.01 mg per kg of body weight every 8 hours.
Adolescent/Adult dose: 0.75 mg three times a day.
Major toxicities
Most frequent: Headache, gastrointestinal disturbances, and malaise. Unusual (more severe): Peripheral neuropathy, pancreatitis, hepatic toxicity, oral ulcers, esophageal ulcers, hematologic toxicity, and skin rashes.
Drug interactions
Zidovudine (ZDV, AZT), RETROVIR ®
Preparations: Syrup: 10 mg/mL; Capsules: 100 mg; Tablets: 300 mg; Concentrate for injection/for intravenous infusion: 10 mg/mL
Dosage Dose for premature infants: (Standard neonatal dose may be excessive in premature infants.) Under study in Pediatric AIDS Clinical Trial Group protocol 331: 1.5 mg per kg of body weight every 12 hours from birth to 2 weeks of age; then increase to 2 mg per kg of body weight every 8 hours after 2 weeks of age.
Neonatal dose: Oral: 2 mg per kg of body weight every 6 hours. Intravenous: 1.5 mg per kg of body weight every 6 hours.
Pediatric usual dose: Oral: 160 mg per m 2 of body surface area every 8 hours. Intravenous (intermittent infusion): 120 mg per m 2 of body surface area every 6 hours. Intravenous (continuous infusion): 20 mg per m 2 of body surface area per hour.
Pediatric dosage range: 90 mg per m 2 of body surface area to 180 mg per m 2 of body surface area every 6-8 hours.
Adolescent/Adult dose: 200 mg three times a day or 300 mg twice daily.
Major toxicities
Most frequent: Hematologic toxicity, including granulocytopenia and anemia, and headache. Unusual: Myopathy, myositis, and liver toxicity.
Drug interactions
Special instructions
*Information in this appendix is not all inclusive. Complete and detailed prescribing and toxicity information on these drugs is available from the drug companies and should be reviewed by the healthcare provider before prescribing these drugs.
Adolescents in early puberty (Tanner I-II) should be dosed using pediatric schedules, whereas those in late puberty (Tanner Stage V) should be dosed using adult schedules. Youth who are in the midst of their growth spurt (Tanner III females and Tanner IV males) should be closely monitored for medication efficacy and toxicity when choosing adult or pediatric dosing guidelines.
§ Drugs metabolized by the hepatic cytochrome P450 enzyme system have the potential for significant interactions with multiple drugs, some of which may be life threatening. These interactions are outlined in detail in prescribing information available from the drug companies. These interactions will not be reiterated in this document, and the healthcare provider should review those documents for detailed information. Before therapy with these drugs is initiated, the patients medication profile should be carefully reviewed for potential drug interactions.
Nonnucleoside Reverse Transcriptase Inhibitors*
*Information in this appendix is not all inclusive. Complete and detailed prescribing and toxicity information on these drugs is available from the drug companies and should be reviewed by the healthcare provider before prescribing these drugs.
Adolescents in early puberty (Tanner I-II) should be dosed using pediatric schedules, whereas those in late puberty (Tanner Stage V) should be dosed using adult schedules. Youth who are in the midst of their growth spurt (Tanner III females and Tanner IV males) should be closely monitored for medication efficacy and toxicity when choosing adult or pediatric dosing guidelines.
§ Drugs metabolized by the hepatic cytochrome P450 enzyme system have the potential for significant interactions with multiple drugs, some of which may be life nthreatening.These interactions are outlined in detail in prescribing information available from the drug companies.These interactions will not be reiterated in this document, and the healthcare provider should review those documents for detailed information. Before therapy with these drugs is initiated, the patients medication profile should be carefully reviewed for potential drug interactions.
Delavirdine (DLV), RESCRIPTOR ®
Preparations: Tablets: 100 mg
Dosage Neonatal dose: Unknown.
Pediatric dose: Unknown.
Adolescent/Adult dose: 400 mg three times a day.
Major toxicities
Most frequent: Headache, fatigue, gastrointestinal complaints, and rash (may be severe).
Drug interactions
Special instructions
Nevirapine (NVP), VIRAMUNE ®
Preparations: Suspension: 10 mg/mL (investigational); Tablets: 200 mg
Dosage Neonatal dose (through age 3 months): Under study in Pediatric AIDS Clinical Trial Group protocol 356: 5 mg per kg of body weight once daily for 14 days, followed by 120 mg per m 2 of body surface area every 12 hours for 14 days, followed by 200 mg per m 2 of body surface area every 12 hours.
Pediatric dose: 120 to 200 mg per m 2 of body surface area every 12 hours. Note: Initiate therapy with 120 mg per m 2 of body surface area administered once daily for 14 days. Increase to full dose administered every 12 hours if there are no rash or other untoward effects.
Adolescent/Adult dose: 200 mg every 12 hours. Note: Initiate therapy at half dose for the first 14 days. Increase to full dose if there is no rash or other untoward effects.
Major toxicities
Most frequent: Skin rash (some severe and life threatening, including Stevens-Johnson syndrome), sedative effect, headache, diarrhea, and nausea. Unusual: Elevated liver enzymes and, rarely, hepatitis.
Drug interactions
*Drugs metabolized by the hepaticsystem have the potential for significant interactions with multiple drugs, some of which may be life threatening. These interactions are outlined in detail in prescribing information available from the drug companies. These interactions will not be reiterated in this document, and the healthcare provider should review those documents for detailed information. Before therapy with these drugs is initiated, the patients medication profile should be carefully reviewed for potential drug interactions.
Special instructions
Protease Inhibitors*§¶
*Information in this appendix is not all inclusive. Complete and detailed prescribing and toxicity information on these drugs is available from the drug companies and should be reviewed by the healthcare provider before prescribing these drugs.
Adolescents in early puberty (Tanner I-II) should be dosed using pediatric schedules, whereas those in late puberty (Tanner Stage V) should be dosed using adult schedules. Youth who are in the midst of their growth spurt (Tanner III females and Tanner IV males) should be closely monitored for medication efficacy and toxicity when choosing adult or pediatric dosing guidelines.
§ Data in children is limited, and doses may change as more information is obtained about the pharmacokinetics of these drugs in children.
¶ Drugs metabolized by the hepatic cytochrome P450 enzyme system have the potential for significant interactions with multiple drugs, some of which may be life threatening. These interactions are outlined in detail in prescribing information available from the drug companies. These interactions will not be reiterated in this document, and the healthcare provider should review those documents for detailed information. Before therapy with these drugs is initiated, the patients medication profile should be carefully reviewed for potential drug interactions.
Indinavir, CRIXIVAN®
Preparations: Capsules: 200 and 400 mg
Dosage Neonatal Dose: Unknown. Due to side effect of hyperbilirubinemia, should not be given to neonates until further information is available.
Pediatric Dose: Under study in clinical trials: 500 mg per m 2 of body surface area every 8 hours. Adolescent/Adult dose: 800 mg every 8 hours.
Major toxicities
Most frequent: Nausea, abdominal pain, headache, metallic taste, dizziness, and asymptomatic hyperbilirubinemia (10%). Unusual (more severe): Nephrolithiasis (4%) and exacerbation of chronic liver disease. Rare: Spontaneous bleeding episodes in hemophiliacs, hyperglycemia, ketoacidosis, diabetes, and hemolytic anemia.
Drug interactions
*Drugs metabolized by the hepaticsystem have the potential for significant interactions with multiple drugs, some of which may be life threatening. These interactions are outlined in detail in prescribing information available from the drug companies. These interactions will not be reiterated in this document, and the healthcare provider should review those documents for detailed information. Before therapy with these drugs is initiated, the patients medication profile should be carefully reviewed for potential drug interactions.
Special instructions
Nelfinavir , VIRACEPT ®
Preparations: Powder for oral suspension: 50 mg per 1 level gram scoopful (200 mg per 1 level teaspoon); Tablets: 250 mg tablet
Dosage Neonatal dose: Under study in Pediatric AIDS Clinical Trial Group protocol 353: 10 mg per kg of body weight three times a day. (Note: no preliminary data available, investigational.)
Pediatric dose: 20 to 30 mg per kg of body weight three times a day.
Adolescent/Adult dose: 750 mg three times a day.
Major toxicities
Most frequent: Diarrhea. Less common: Asthenia, abdominal pain, rash, and exacerbation of chronic liver disease. Rare: Spontaneous bleeding episodes in hemophiliacs, hyperglycemia, ketoacidosis, and diabetes.
Drug interactions
*Drugs metabolized by the hepaticsystem have the potential for significant interactions with multiple drugs, some of which may be life threatening. These interactions are outlined in detail in prescribing information available from the drug companies. These interactions will not be reiterated in this document, and the healthcare provider should review those documents for detailed information. Before therapy with these drugs is initiated, the patients medication profile should be carefully reviewed for potential drug interactions.
Special instructions
Ritonavir, NORVIR®
Preparations: Oral solution: 80 mg/mL; Capsules: 100 mg
Dosage Neonatal dose: Under study in Pediatric AIDS Clinical Trial Group protocol 354 (single dose pharmacokinetics).
Pediatric usual dose: 400 mg per m 2 of body surface area every 12 hours. To minimize nausea/vomiting, initiate therapy starting at 250 mg per m 2 of body surface area every 12 hours and increase stepwise to full dose over 5 days as tolerated.
Pediatric dosage range: 350 to 400 mg per m 2 of body surface area every 12 hours.
Adolescent/Adult dose: 600 mg twice daily. To minimize nausea/vomiting, initiate therapy starting at 300 mg twice daily and increase stepwise to full dose over 5 days as tolerated.
Major toxicities
Most frequent: Nausea, vomiting, diarrhea, headache, abdominal pain, and anorexia. Less common: Circumoral paresthesias and increase in liver enzymes. Rare: Spontaneous bleeding episodes in hemophiliacs, pancreatitis, increased levels of triglycerides and cholesterol, hyperglycemia, ketoacidosis, diabetes, and hepatitis.
Drug interactions
*Drugs metabolized by the hepaticsystem have the potential for significant interactions with multiple drugs, some of which may be life threatening. These interactions are outlined in detail in prescribing information available from the drug companies. These interactions will not be reiterated in this document, and the healthcare provider should review those documents for detailed information. Before therapy with these drugs is initiated, the patients medication profile should be carefully reviewed for potential drug interactions.
Special instructions
Saquinavir, INVIRASE (hard gel capsule) and FORTOVASE (soft gel capsule)
Preparations: Hard gel capsules: 200 mg; Soft gel capsules: 200 mg
Dosage Neonatal dose: Unknown.
Pediatric dose: Unknown (will be studied in Pediatric AIDS Clinical Trials Group protocol 397).
Adolescent/Adult dose: Hard gel capsules: 600 mg three times a day; Soft gel capsules: 1200 mg three times a day.
Major toxicities
Most frequent: Diarrhea, abdominal discomfort, headache, nausea, paresthesias, and skin rash. Less common: Exacerbation of chronic liver disease. Rare: Spontaneous bleeding episodes in hemophiliacs, hyperglycemia, ketoacidosis, and diabetes.
Drug interactions
* Drugs metabolized by the hepatic cytochrome P450 enzyme system have the potential for significant interactions with multiple drugs, some of which may be life threatening. These interactions are outlined in detail in prescribing information available from the drug companies. These interactions will not be reiterated in this document, and the healthcare provider should review those documents for detailed information. Before therapy with these drugs is initiated, the patient's medication profile should be carefully reviewed for potential drug interactions.
Special instructions
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