Practical Aspects of Practical Aspects of Antiretroviral TherapyAntiretroviral Therapy
Nancy R. Calles,R.N.,B.S.N.Nancy R. Calles,R.N.,B.S.N.
Treatment Goals for Treatment Goals for ChildrenChildren
Promote or restore normal growth Promote or restore normal growth and developmentand development
Prevent complicating infections Prevent complicating infections and cancersand cancers
Improve quality of lifeImprove quality of life Prolong survivalProlong survival
Objectives of this Objectives of this PresentationPresentation
List the names and formulations of List the names and formulations of antiretroviralsantiretrovirals
Describe the dosing of antiretroviralsDescribe the dosing of antiretrovirals Discuss the side effects of Discuss the side effects of
antiretroviralsantiretrovirals List drug interactions of antiretroviralsList drug interactions of antiretrovirals Discuss practical approaches to Discuss practical approaches to
administration of antiretroviralsadministration of antiretrovirals
Nucleoside Reverse Nucleoside Reverse Transcriptase InhibitorsTranscriptase Inhibitors
AZT, zidovudine (RETROVIR)AZT, zidovudine (RETROVIR) d4T, stavudine (ZERIT)d4T, stavudine (ZERIT) ddI, didanosine (VIDEX)ddI, didanosine (VIDEX) ddC, zalcitabine (HIVID)ddC, zalcitabine (HIVID) 3TC, lamivudine (EPIVIR)3TC, lamivudine (EPIVIR) ABC, abacavir (ZIAGEN)ABC, abacavir (ZIAGEN)
Zidovudine (RETROVIR): Zidovudine (RETROVIR): FormulationsFormulations
100 mg capsules100 mg capsules 300 mg tablets300 mg tablets 10 mg/ml yellow liquid, strawberry 10 mg/ml yellow liquid, strawberry
flavoredflavored Intravenous formulationIntravenous formulation
Zidovudine (RETROVIR): Zidovudine (RETROVIR): DosingDosing
Neonatal: Oral: 2 mg/kg q6hNeonatal: Oral: 2 mg/kg q6h
Neonatal: Intravenous: 1.5 mg/kg Neonatal: Intravenous: 1.5 mg/kg q6hq6h
Pediatric: Oral: Pediatric: Oral: 90-180 mg/m90-180 mg/m22 body surface area body surface area tid or bid ( 200 max. qid)tid or bid ( 200 max. qid)
Zidovudine (RETROVIR): Zidovudine (RETROVIR): Side EffectsSide Effects
Most Frequent:Most Frequent:Hematological, including anemia Hematological, including anemia and neutropeniaand neutropenia
Less common:Less common:Myopathy, myositis, and liver Myopathy, myositis, and liver toxicitytoxicity
Zidovudine (RETROVIR):Zidovudine (RETROVIR):Drug InteractionsDrug Interactions
Drugs which can be associated Drugs which can be associated with bone marrow suppression with bone marrow suppression should be avoidedshould be avoided
Drugs which may increase ZDV Drugs which may increase ZDV concentration should be avoided concentration should be avoided (probenecid, atovaquone, (probenecid, atovaquone, methadone, valproic acid, and methadone, valproic acid, and fluconazole)fluconazole)
Zidovudine (RETROVIR):Zidovudine (RETROVIR): Tips for Caregivers Tips for Caregivers
Tablets and capsules should be Tablets and capsules should be stored at room temperaturestored at room temperature
Protect capsules from moistureProtect capsules from moisture May be taken with or without foodMay be taken with or without food
Stavudine (ZERIT):Stavudine (ZERIT):FormulationsFormulations
15 mg, 20 mg, 30 mg, and 40 mg 15 mg, 20 mg, 30 mg, and 40 mg capsulescapsules
1 mg/ml cloudy solution1 mg/ml cloudy solution
Stavudine (ZERIT):Stavudine (ZERIT):DosingDosing
Neonatal:Neonatal:Under investigationUnder investigation
Pediatric: Oral:Pediatric: Oral:1 mg/kg bid (max. 40 mg bid)1 mg/kg bid (max. 40 mg bid)
Stavudine (ZERIT):Stavudine (ZERIT):Side EffectsSide Effects
Most frequent:Most frequent:Headache, gastrointestinal Headache, gastrointestinal complaints, skin rashcomplaints, skin rash
Less common:Less common:Pancreatitis, peripheral Pancreatitis, peripheral neuropathy, increased liver neuropathy, increased liver enzymesenzymes
Stavudine (ZERIT):Stavudine (ZERIT):Drug InteractionsDrug Interactions
Should not be administered with Should not be administered with ZDV because of potential ZDV because of potential antagonismantagonism
Drugs which decrease renal Drugs which decrease renal function can decrease clearance function can decrease clearance and should be avoidedand should be avoided
Stavudine (ZERIT):Stavudine (ZERIT):Tips for CaregiversTips for Caregivers
Can be given with or without foodCan be given with or without food Shake oral solution, keep Shake oral solution, keep
refrigerated, good for 30 daysrefrigerated, good for 30 days Capsules can be opened and Capsules can be opened and
sprinkled on mashed potatoes, sprinkled on mashed potatoes, applesauce or other soft foodsapplesauce or other soft foods
Didanosine (VIDEX): Didanosine (VIDEX): FormulationsFormulations
25 mg, 50 mg, 100 mg, and 150 25 mg, 50 mg, 100 mg, and 150 mg orange flavored, chewable mg orange flavored, chewable tabletstablets
10 mg/ml white suspension10 mg/ml white suspension
Didanosine (VIDEX): Didanosine (VIDEX): Dosing Dosing
Neonatal: Oral: (infants <90 days Neonatal: Oral: (infants <90 days old)old)50 mg/m50 mg/m22 of body surface area of body surface area
Pediatric: Oral: Dose range: Pediatric: Oral: Dose range: 90-150 mg/m90-150 mg/m22 body surface area body surface area bidbid
Didanosine (VIDEX):Didanosine (VIDEX):Side EffectsSide Effects
Most frequent:Most frequent:Abdominal pain, nausea, vomiting, Abdominal pain, nausea, vomiting, diarrhea, constipationdiarrhea, constipation
Less common:Less common:Peripheral neuropathy, Peripheral neuropathy, pancreatitis, retinal pancreatitis, retinal depigmentation, electrolyte depigmentation, electrolyte abnormalitiesabnormalities
Didanosine (VIDEX):Didanosine (VIDEX):Drug InteractionsDrug Interactions
May decrease the absorption of May decrease the absorption of ketaconazole, itraconazole, and ketaconazole, itraconazole, and dapsone if administered concomitantlydapsone if administered concomitantly
Tetracycline and fluoroquinolone Tetracycline and fluoroquinolone antibiotic absorption are significantly antibiotic absorption are significantly decreaseddecreased
Concomitant administration of ddI and Concomitant administration of ddI and DLV decreases the absorption of bothDLV decreases the absorption of both
Didanosine (VIDEX):Didanosine (VIDEX): Tips for Caregivers Tips for Caregivers
Give on an empty stomach 1 hour Give on an empty stomach 1 hour before or 2 hours after a mealbefore or 2 hours after a meal
Shake suspension well, keep Shake suspension well, keep refrigeratedrefrigerated
Give two tablets to ensure adequate Give two tablets to ensure adequate buffering, may be dissolved in waterbuffering, may be dissolved in water
Do not give at the same time as Do not give at the same time as indinavir, ritonavir, or delavirdineindinavir, ritonavir, or delavirdine
Lamivudine (EPIVIR):Lamivudine (EPIVIR):FormulationsFormulations
150 mg white tablets150 mg white tablets 10 mg/ml clear solution10 mg/ml clear solution
Lamivudine (EPIVIR):Lamivudine (EPIVIR):DosingDosing
Neonatal: Oral: (< 30 days old)Neonatal: Oral: (< 30 days old)2 mg/kg bid2 mg/kg bid
Pediatric: Oral:Pediatric: Oral:4 mg/kg bid (max. 150 mg bid)4 mg/kg bid (max. 150 mg bid)
Lamivudine (EPIVIR):Lamivudine (EPIVIR):Side EffectsSide Effects
Most frequent:Most frequent:Headache, fatigue, nausea, Headache, fatigue, nausea, diarrhea, skin rash, abdominal paindiarrhea, skin rash, abdominal pain
Less common:Less common:Pancreatitis, peripheral Pancreatitis, peripheral neuropathy, increased liver neuropathy, increased liver enzymesenzymes
Lamivudine (EPIVIR):Lamivudine (EPIVIR):Drug InteractionsDrug Interactions
No known negative drug No known negative drug interactionsinteractions
Lamivudine (EPIVIR):Lamivudine (EPIVIR):Tips for CaregiversTips for Caregivers
Can be given with or without foodCan be given with or without food Store oral solution at room Store oral solution at room
temperaturetemperature Dosage should be decreased in Dosage should be decreased in
patients with impaired renal patients with impaired renal functionfunction
Abacavir (ZIAGEN):Abacavir (ZIAGEN):FormulationsFormulations
300 mg yellow, capsule-shaped 300 mg yellow, capsule-shaped tabletstablets
20 mg/ml yellow oral solution20 mg/ml yellow oral solution
Abacavir (ZIAGEN):Abacavir (ZIAGEN):DosingDosing
Neonatal: Oral:Neonatal: Oral:Not approved for children < 3 Not approved for children < 3 months of agemonths of age
Pediatric: Oral:Pediatric: Oral:8 mg/kg bid (max. 300 mg bid)8 mg/kg bid (max. 300 mg bid)
Abacavir (ZIAGEN):Abacavir (ZIAGEN):Side EffectsSide Effects
Most frequent:Most frequent:Nausea, fever, vomiting, headache, Nausea, fever, vomiting, headache, rash, anorexia, and fatiguerash, anorexia, and fatigue
Less common:Less common:Hypersensitivity reaction, diarrhea, Hypersensitivity reaction, diarrhea, pancreatitis, increased liver enzymes, pancreatitis, increased liver enzymes, elevated blood glucose, elevated elevated blood glucose, elevated triglycerides, and lactic acidosistriglycerides, and lactic acidosis
Abacavir (ZIAGEN):Abacavir (ZIAGEN):Drug InteractionsDrug Interactions
No known significant drug No known significant drug interactions interactions
Abacavir (ZIAGEN):Abacavir (ZIAGEN):Tips for CaregiversTips for Caregivers
Give with or without foodGive with or without food Store at room temperatureStore at room temperature Teach the signs and symptoms of a Teach the signs and symptoms of a
hypersensitivity reactionhypersensitivity reaction Instruct parents to call immediately Instruct parents to call immediately
if rash occursif rash occurs Provide a medication guide and Provide a medication guide and
warning card warning card
Non-Nucleoside Reverse Non-Nucleoside Reverse Transcriptase InhibitorsTranscriptase Inhibitors
NVP, nevirapine (VIRAMUNE)NVP, nevirapine (VIRAMUNE) EFV, efavirenz (SUSTIVA)EFV, efavirenz (SUSTIVA) DLV, delavirdine (RESCRIPTOR)DLV, delavirdine (RESCRIPTOR)
Nevirapine (VIRAMUNE):Nevirapine (VIRAMUNE):FormulationsFormulations
200 mg white, oval tablets200 mg white, oval tablets 50 mg/5 ml solution50 mg/5 ml solution
Nevirapine (VIRAMUNE):Nevirapine (VIRAMUNE):DosingDosing
Neonatal: Oral:Neonatal: Oral:Under investigationUnder investigation
Pediatric: Oral:Pediatric: Oral:(>3 months - 8 years of of age)(>3 months - 8 years of of age)7 mg/kg bid7 mg/kg bid(> 8 years of age)(> 8 years of age)4 mg/kg bid (max. 200 mg bid)4 mg/kg bid (max. 200 mg bid)
Nevirapine (VIRAMUNE):Nevirapine (VIRAMUNE):Side EffectsSide Effects
Most frequent:Most frequent:Skin rash, sedative effect, Skin rash, sedative effect, headache, diarrhea, nauseaheadache, diarrhea, nausea
Less common:Less common:Elevated liver enzymesElevated liver enzymes
Nevirapine (VIRAMUNE):Nevirapine (VIRAMUNE):Drug InteractionsDrug Interactions
Lowers the levels of rifampin and Lowers the levels of rifampin and rifabutinrifabutin
Should not be administered with Should not be administered with ketoconazole or oral ketoconazole or oral contraceptivescontraceptives
Decreases levels of indinavir Decreases levels of indinavir (recommended indinavir dose in (recommended indinavir dose in adults is 1000 mg q8h)adults is 1000 mg q8h)
Nevirapine (VIRAMUNE):Nevirapine (VIRAMUNE):Tips for CaregiversTips for Caregivers
Give with or without foodGive with or without food Tablets may be broken in halfTablets may be broken in half Shake solution wellShake solution well Discuss potential for rashDiscuss potential for rash Medication profile should be Medication profile should be
reviewed carefully prior to starting reviewed carefully prior to starting NVP for potential of multiple drug NVP for potential of multiple drug interactions interactions
Efavirenz (SUSTIVA):Efavirenz (SUSTIVA):FormulationsFormulations
50 mg, 100 mg and 200 mg 50 mg, 100 mg and 200 mg capsulescapsules
Efavirenz (SUSTIVA):Efavirenz (SUSTIVA):DosingDosing
Neonatal: Oral:Neonatal: Oral:Not approved for children < 3 Not approved for children < 3 years oldyears old
Pediatric: Oral:Pediatric: Oral:200-600 mg qd (exact dose is 200-600 mg qd (exact dose is dependent on weight)dependent on weight)
Efavirenz (SUSTIVA):Efavirenz (SUSTIVA):Side EffectsSide Effects
Most frequent:Most frequent:Rash, CNS symptoms (somnolence, Rash, CNS symptoms (somnolence, insomnia, abnormal dreams, insomnia, abnormal dreams, confusion, abnormal thinking, confusion, abnormal thinking, impaired concentration, impaired concentration, hallucinations, euphoria)hallucinations, euphoria)
Less common:Less common:Elevated liver enzymes, hepatitisElevated liver enzymes, hepatitis
Efavirenz (SUSTIVA):Efavirenz (SUSTIVA):Drug InteractionsDrug Interactions
Should not be taken with Should not be taken with midazolam, triazolam, cisapride, midazolam, triazolam, cisapride, and ergot derivativesand ergot derivatives
Reduces levels of clarithromycin Reduces levels of clarithromycin and rifampinand rifampin
Reduces level of rifabutinReduces level of rifabutin Decreases levels of saquinavir, Decreases levels of saquinavir,
indinavir, lopinavirindinavir, lopinavir
Efavirenz (SUSTIVA): Efavirenz (SUSTIVA): Tips for CaregiversTips for Caregivers
Give with or without food, but Give with or without food, but avoid high fat mealavoid high fat meal
Capsules may be opened and Capsules may be opened and sprinkled on foodsprinkled on food
Tolerability of CNS side effects can Tolerability of CNS side effects can be improved by bedtime dosingbe improved by bedtime dosing
Delavirdine (RESCRIPTOR):Delavirdine (RESCRIPTOR):FormulationsFormulations
100 mg white, capsule-shaped 100 mg white, capsule-shaped tabletstablets
Delavirdine (RESCRIPTOR):Delavirdine (RESCRIPTOR):DosingDosing
Neonatal: Oral:Neonatal: Oral:Not approved for use in neonatesNot approved for use in neonates
Pediatric: Oral:Pediatric: Oral:Not approved for use in children Not approved for use in children less than 16 years oldless than 16 years old
Protease InhibitorsProtease Inhibitors
NFV, nelfinavir (VIRACEPT)NFV, nelfinavir (VIRACEPT) RTV, ritonavir (NORVIR)RTV, ritonavir (NORVIR) IDV, indinavir (CRIXIVAN)IDV, indinavir (CRIXIVAN) SQV, saquinavir (FORTOVASE)SQV, saquinavir (FORTOVASE) APV, amprenavir (AGENERASE)APV, amprenavir (AGENERASE) LPV, lopinavir/r (KALETRA)LPV, lopinavir/r (KALETRA)
Nelfinavir (VIRACEPT):Nelfinavir (VIRACEPT):FormulationsFormulations
250 mg blue, capsule-shaped 250 mg blue, capsule-shaped tabletstablets
50 mg/scoop white powder50 mg/scoop white powder
Nelfinavir (VIRACEPT):Nelfinavir (VIRACEPT):DosingDosing
Neonatal: Oral:Neonatal: Oral:Under investigationUnder investigation
Pediatric: Oral:Pediatric: Oral:30 mg/kg tid30 mg/kg tid
Nelfinavir (VIRACEPT):Nelfinavir (VIRACEPT):Side EffectsSide Effects
Most frequent:Most frequent:DiarrheaDiarrhea
Less common:Less common:Abdominal pain, rash, Abdominal pain, rash, exacerbation of liver disease, exacerbation of liver disease, hyperglycemia, diabetes, hyperglycemia, diabetes, metabolic abnormalitiesmetabolic abnormalities
Nelfinavir (VIRACEPT):Nelfinavir (VIRACEPT):Drug InteractionsDrug Interactions
Do not give with simvastatin, Do not give with simvastatin, lovastatin, rifampin, cisapride, lovastatin, rifampin, cisapride, midazolam, triazolam, midazolam, triazolam, dihydroergotamine, ergotaminedihydroergotamine, ergotamine
Concominant Rifabutin should be Concominant Rifabutin should be reduced to 150 mg qd and nelfinavir reduced to 150 mg qd and nelfinavir increased to 1000 mg tidincreased to 1000 mg tid
Decreases level of oral contraceptivesDecreases level of oral contraceptives
Nelfinavir (VIRACEPT):Nelfinavir (VIRACEPT):Tips for CaregiversTips for Caregivers
Give with a meal or light snackGive with a meal or light snack Tablets can be crushed or pulverizedTablets can be crushed or pulverized Do not give with citrus juice or apple Do not give with citrus juice or apple
saucesauce Powder may be put on food or in liquidsPowder may be put on food or in liquids Improve taste by mixing with milk, Improve taste by mixing with milk,
chocolate milk, pudding or vanilla ice chocolate milk, pudding or vanilla ice creamcream
Ritonavir (NORVIR):Ritonavir (NORVIR):FormulationsFormulations
100 mg white, soft-gelatin capsule100 mg white, soft-gelatin capsule 80 mg/ml orange colored solution80 mg/ml orange colored solution
Ritonavir (NORVIR):Ritonavir (NORVIR): Dosing Dosing
Neonatal: Oral:Neonatal: Oral:Under investigationUnder investigation
Pediatrics: Oral:Pediatrics: Oral:400 mg/m400 mg/m22 body surface area bid body surface area bid (max. 600 mg bid)(max. 600 mg bid)
Ritonavir (NORVIR):Ritonavir (NORVIR):Side EffectsSide Effects
Most frequent:Most frequent:Nausea, vomiting, diarrhea, Nausea, vomiting, diarrhea, abdominal pain, anorexiaabdominal pain, anorexia
Less common:Less common:Paresthesias, increased liver Paresthesias, increased liver enzymes, pancreatitis, increased enzymes, pancreatitis, increased triglycerides and cholesterol, triglycerides and cholesterol, hyperglycemia, diabetes, metabolic hyperglycemia, diabetes, metabolic abnormalitiesabnormalities
Ritonavir (NORVIR):Ritonavir (NORVIR):Drug InteractionsDrug Interactions
Should not be used with bepridil, Should not be used with bepridil, amiodarone, flecainide, amiodarone, flecainide, propafenone, quinidine, propafenone, quinidine, simvastatin, lovastatin, cisapride, simvastatin, lovastatin, cisapride, clozapine, midazolam, ergotamineclozapine, midazolam, ergotamine
Lowers the level of oral Lowers the level of oral contraceptivescontraceptives
Ritonavir (NORVIR):Ritonavir (NORVIR):Tips for CaregiversTips for Caregivers
Give with or without food, but food Give with or without food, but food seems to make it more tolerableseems to make it more tolerable
Keep refrigeratedKeep refrigerated Tips for making it more palatable: mix Tips for making it more palatable: mix
with milk or chocolate milk, or vanilla with milk or chocolate milk, or vanilla or chocolate pudding, dull taste buds or chocolate pudding, dull taste buds by giving ice or popsicles prior to by giving ice or popsicles prior to dosing, coat the mouth with peanut dosing, coat the mouth with peanut butter butter
Ritonavir (NORVIR):Ritonavir (NORVIR):Tips for CaregiversTips for Caregivers
Give gradually increasing amounts Give gradually increasing amounts over 5 days until the full dose is over 5 days until the full dose is achieved to help prevent nausea achieved to help prevent nausea and vomitingand vomiting
Obtain a medication history prior Obtain a medication history prior to starting therapyto starting therapy
Indinavir (CRIXIVAN):Indinavir (CRIXIVAN):FormulationsFormulations
200 mg, 400 mg capsules200 mg, 400 mg capsules
Indinavir (CRIXIVAN):Indinavir (CRIXIVAN):DosingDosing
Neonatal: Oral:Neonatal: Oral:Not recommendedNot recommended
Pediatric: Oral:Pediatric: Oral:500 mg/m500 mg/m22 body surface area q8h body surface area q8h(max. 800 mg q8h)(max. 800 mg q8h)
Indinavir (CRIXIVAN):Indinavir (CRIXIVAN):Side EffectsSide Effects
Most frequent:Most frequent:Nausea, abdominal pain, Nausea, abdominal pain, headache, metallic taste, dizziness, headache, metallic taste, dizziness, asymptomatic hyperbilirubinemiaasymptomatic hyperbilirubinemia
Less common:Less common:Nephrolithiasis, hyperglycemia, Nephrolithiasis, hyperglycemia, ketoacidosis, diabetes, metabolic ketoacidosis, diabetes, metabolic abnormalitiesabnormalities
Indinavir (CRIXIVAN):Indinavir (CRIXIVAN):Drug InteractionsDrug Interactions
Do not give with cisapride, Do not give with cisapride, triazolam, midazolam, ergot triazolam, midazolam, ergot derivatives, simvastatin, lovastatinderivatives, simvastatin, lovastatin
Reduce to 800 mg tid when used in Reduce to 800 mg tid when used in combination with ketoconazolecombination with ketoconazole
Reduce rifabutin 50% when used Reduce rifabutin 50% when used togethertogether
Indinavir (CRIXIVAN):Indinavir (CRIXIVAN):Tips for CaregiversTips for Caregivers
Give 1 hour before or 2 hours after Give 1 hour before or 2 hours after a meala meal
Encourage 48 ounces of fluid q24hEncourage 48 ounces of fluid q24h Do not take with grapefruit juice;Do not take with grapefruit juice;
may take with water, skim milk, or may take with water, skim milk, or apple juiceapple juice
Keep capsules moisture freeKeep capsules moisture free
Indinavir (CRIXIVAN):Indinavir (CRIXIVAN):Tips for CaregiversTips for Caregivers
Decrease dose in patients with Decrease dose in patients with hepatic insufficiencyhepatic insufficiency
Give 1 hour apart from ddI on an Give 1 hour apart from ddI on an empty stomachempty stomach
Saquinavir (FORTOVASE):Saquinavir (FORTOVASE):FormulationsFormulations
200 mg beige, soft-gel capsules200 mg beige, soft-gel capsules
Saquinavir (FORTOVASE):Saquinavir (FORTOVASE):DosingDosing
Neonatal: Oral:Neonatal: Oral:Not approvedNot approved
Pediatric: Oral:Pediatric: Oral:50 mg/kg tid50 mg/kg tid
Saquinavir (FORTOVASE):Saquinavir (FORTOVASE):Side EffectsSide Effects
Most frequent:Most frequent:Diarrhea, abdominal discomfort, Diarrhea, abdominal discomfort, headache, nausea, paresthesias, skin headache, nausea, paresthesias, skin rashrash
Less common:Less common:Exacerbation of chronic liver disease, Exacerbation of chronic liver disease, hyperglycemia, ketoacidosis, hyperglycemia, ketoacidosis, diabetes, metabolic abnormalitiesdiabetes, metabolic abnormalities
Saquinavir (FORTOVASE):Saquinavir (FORTOVASE):Drug InteractionsDrug Interactions
Should not be taken with cisapride, Should not be taken with cisapride, triazolam, midazolam, ergot, triazolam, midazolam, ergot, simvastatin, lovastatin, rifampin, simvastatin, lovastatin, rifampin, rifabutin, efavirenz, indinavir, rifabutin, efavirenz, indinavir, ketoconazole, clarithromycinketoconazole, clarithromycin
Ritonavir increases levels of Ritonavir increases levels of saquinavir by 3 fold or greatersaquinavir by 3 fold or greater
Saquinavir (FORTOVASE):Saquinavir (FORTOVASE):Tips for CaregiversTips for Caregivers
Give with a meal or up to 2 hours Give with a meal or up to 2 hours after a mealafter a meal
Avoid grapefruit juiceAvoid grapefruit juice Sunscreen or protective clothing is Sunscreen or protective clothing is
recommended recommended Review the patient’s medication Review the patient’s medication
profile for potential drug profile for potential drug interactionsinteractions
Amprenavir (AGENERASE):Amprenavir (AGENERASE):FormulationsFormulations
50 mg and 150 mg cream-white, 50 mg and 150 mg cream-white, soft-gelatin capsulessoft-gelatin capsules
Yellow colored oral solutionYellow colored oral solution
Amprenavir (AGENERASE):Amprenavir (AGENERASE):DosingDosing
Neonatal: Oral:Neonatal: Oral:Not approved for children < 4 years Not approved for children < 4 years oldold
Pediatric: Oral:Pediatric: Oral:Capsule: 20 mg/kg bid or 15 mg/kg Capsule: 20 mg/kg bid or 15 mg/kg tidtidSolution: 22.5 mg/kg bid or Solution: 22.5 mg/kg bid or 17 mg/kg tid17 mg/kg tid(max. 2,800 mg daily)(max. 2,800 mg daily)
Amprenavir (AGENERASE):Amprenavir (AGENERASE):Side EffectsSide Effects
Most frequent:Most frequent:Headache, nausea, upset stomach, Headache, nausea, upset stomach, tirednesstiredness
Less common:Less common:Hyperglycemia, Stevens-Johnson Hyperglycemia, Stevens-Johnson syndromesyndrome
Amprenavir (AGENERASE):Amprenavir (AGENERASE):Drug InteractionsDrug Interactions
Should not be given with bepridil, Should not be given with bepridil, cisapride, dihydroergotamine, cisapride, dihydroergotamine, ergotamine, midazolam, triazolam, ergotamine, midazolam, triazolam, rifampin, simvastatin, lovastatinrifampin, simvastatin, lovastatin
Reduce concomitant Rifabutin by Reduce concomitant Rifabutin by 50% 50%
Give 1 hour before ddIGive 1 hour before ddI Interacts with other antiretroviralsInteracts with other antiretrovirals
Amprenavir (AGENERASE):Amprenavir (AGENERASE):Tips for CaregiversTips for Caregivers
Give with or without foodGive with or without food Do not give supplemental vitamin Do not give supplemental vitamin
EE Solution is bitter but well toleratedSolution is bitter but well tolerated Get comprehensive medication Get comprehensive medication
history prior to starting treatmenthistory prior to starting treatment
Lopinavir/r (KALETRA):Lopinavir/r (KALETRA):FormulationsFormulations
133.3 mg lopinavir/ 33.3 mg 133.3 mg lopinavir/ 33.3 mg ritonavir orange, soft gelatin ritonavir orange, soft gelatin capsulecapsule
80 mg lopinavir/ 20 mg ritonavir/ 80 mg lopinavir/ 20 mg ritonavir/ ml light, yellow/orange oral ml light, yellow/orange oral solutionsolution
Lopinavir/r (KALETRA) Lopinavir/r (KALETRA) DosingDosing
Neonatal: oral: Not approved for Neonatal: oral: Not approved for children less than 6 months of agechildren less than 6 months of age
Pediatric: oral: Pediatric: oral: 12 mg LPV/ 3 mg RTV/kg for children 12 mg LPV/ 3 mg RTV/kg for children
7-15 kg bid with food7-15 kg bid with food10 mg LPV/ 2.5 mg RTV/kg for 10 mg LPV/ 2.5 mg RTV/kg for
children 15-40 kg bid with foodchildren 15-40 kg bid with food
Lopinavir/r (KALETRA)Lopinavir/r (KALETRA)Side EffectsSide Effects
Most frequent:Most frequent: Diarrhea, nausea, vomiting, Diarrhea, nausea, vomiting,
headache, fatigueheadache, fatigue Less Common:Less Common: Pancreatitis, hyperglycemia, Pancreatitis, hyperglycemia,
diabetes, diabetes, metabolic abnormalitiesmetabolic abnormalities
Lopinavir/r (KALETRA)Lopinavir/r (KALETRA)Drug InteractionsDrug Interactions
Should not be taken with ergotamine, Should not be taken with ergotamine, triazolam, astemizole, pinozide, triazolam, astemizole, pinozide, cisapride, propafenone, terfenadine, cisapride, propafenone, terfenadine, flecainide, midazolam, rifampin, flecainide, midazolam, rifampin, lovastatin, simvastatin, St. John’s Wortlovastatin, simvastatin, St. John’s Wort
May reduce effectiveness of oral May reduce effectiveness of oral contraceptivescontraceptives
Increase dose if used with NNRTI’sIncrease dose if used with NNRTI’s
Lopinavir/r (KALETRA):Lopinavir/r (KALETRA):Tips for CaregiversTips for Caregivers
Give with foodGive with food Stable unrefridgerated for 2 Stable unrefridgerated for 2
monthsmonths Review patients medication profile Review patients medication profile
for potential drug interactionsfor potential drug interactions
Drug Interactions of NRTIsDrug Interactions of NRTIsDrug Interactions
AZT Drugs associated with bone marrowsuppressionDrugs which increase ZDVconcentration
d4T Should not be administered with AZTbecause of potential antagonism
ddI Decreases the absorption ofketaconazole, itraconazole, anddapsone
3TC No known drug interactions
ABC No known drug interactions
Drug Interactions of Drug Interactions of NNRTIsNNRTIs
Drug Interactions
NVP Lowers levels of rifampinShould not be administeredwith ketoconazole or oralcontraceptives
EFV Decreases levels of rifampin,rifabutin, clarithromycin,saquinavir, indinavir, lopinavir
Drug Interactions of PIsDrug Interactions of PIsDrug Interactions*
NFV Decreases level of oralcontraceptives
RTV Decreases level of oralcontraceptivesIncreases metabolism oftheophylline
IDV Reduces rifabutin 50% when usedconcomitantly
*All PIs have multiple drug interactions because they are metabolized by ctyochrome
P450 3A
Drug Interactions of PIsDrug Interactions of PIs
Drug InteractionsSQV Levels are increased 3 fold
or greater by RitonavirAPV Reduces Rifabutin 50%
when used concomitantly
Serious Side Effects of Serious Side Effects of NRTIs in ChildrenNRTIs in Children
Drug Side Effects
3TC Pancreatitis, peripheral neuropathy
ABC Hypersensitivity reactions, pancreatitis
AZT Bone marrow suppression
d4t Pancreatitis, peripheral neuropathy
ddC Peripheral neuropathy
ddI Pancreatitis, peripheral neuropathy, retinaldepigmentation
Serious Side Effects of Serious Side Effects of NNRTIsNNRTIs
Drug Side Effects
NVP Rash, fever, nausea, headache,diarrhea
EFV Rash, diarrhea, fever, cough, nausea
DLV Not approved for use in children
Side Effects of PIsSide Effects of PIsDrug Side Effects
NFV Diarrhea
RTV Nausea, vomiting
IDV Nausea, vomiting, hematuria,kidney stones, hyperbilrubinemia
SQV Diarrhea
APV Nausea, vomiting, diarrhea
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