DRUG NAME

DRUG CATEGORY

AVAILABLE DOSAGE FORMS

NORMAL DOSE

DOSING INSTRUCTIONS

ADVERSE EFFECTS

LAB MONITORING

DRUG INTERACTION POTENTIAL

NUCLEOSIDE/NUCLEOTIDE REVERSE TRANSCRIPTASE INHIBITORS (NRTI/NtRTI)

abacavir
(Ziagen, ABC)
GlaxoSmithKline

nucleoside reverse transcriptase inhibitor (NRTI)

Tablet: 300mg
Oral solution: 20mg/ml (strawberry- banana flav) 240ml

Trizivir is 300mg AZT, 150mg 3TC and 300mg abacavir.

Adult: 300mg bid

Children: 3mos-16yrs 8mg/kg bid (max 300mg bid)

Infants (<3mo): investigational, 8mg/kg po bid

With or without food.

Pregnancy Category:C

Hypersensitivity reactions (~5%) -fever, skin rash, fatigue, GI (N/V, diarrhea, abdominal pain), pharyngitis, dyspnea, cough, abnormal labs (creat kinases, LFT). D/C immediately.
Rechallenge is contraindicated- can cause hypotension and death.
Other: nausea, vomiting, malaise, fatigue, HA, diarrhea, anorexia.
Lab abnormalities: anemia, neutropenia, LFT, CPK, blood glucose, trig.
General NRTI: Lactic acidosis, hepatomegaly w/ steatosis, lipodystrophy.

LFT, CBC

- Metabolized through glucoronyl transferase and alcohol dehydrogenase.
- Ethanol increases abacavir levels.
- Renal excretion of metabolites 82%

- Tipranavir decreases abacavir AUC 40%

- Cases of hepatic decompensation with ribavirin

didanosine (Videx, Videx EC, ddl)
Bristol -Myers Squibb

nucleoside reverse transcriptase inhibitor (NRTI)

Buffered pwdr for oral soln: packets of 100, 167, and 250mg.
DR capsules: 125 (Videx EC only), 200, 250, 400mg capsules.

Peds: 10mg/ml pwdr for oral soln: 2g, 4g.

>60kg
Tablets: 200mg bid or 400mg qd.
Powder: 250mg bid.
EC: 400mg qd

<60kg
Tablets: 125mg bid or 250mg qd.
Powder: 167mg bid.
Peds: 90-150mg/m2 q12

Renal dose adjustment for CrCl<60ml/min

Take on an empty stomach.
Do not crush or break open EC capsules.
Chewable tabs can be dissolved in water or apple juice (no acidic juices). Drink immediately.

Ped susp. Must add Maalox to conc. Of 10mg/mL before dispensing., stable 30d under refrigeration.

Pregnancy Category: B

Most common: diarrhea, neuropathy, chills, fever, rash, abd pain, weakness, HA, N/V.
Other: Vision changes, dyslipidemia, lipodystrophy.

Warning: Pancreatitis, peripheral neuropathy, lactic acidosis, severe hepatomegally w/ steatosis. Pacreatitis more common in pts w/ renal disease, alcohol use, treatment w/ stavudine or hydroxyurea.

CBC, LFT, amylase, lipase

- Each packet of buff pwdr has 1380mg sodium. Chew. tab has 264.5mg sodium.
- Chew. tab has 36.5mg phenylalanine (caution PKU pts)
- Renal excretion 50%
- Didanosine IR contains antacids. Separate from drugs needing acidic pH (itraconazole)
- Buffer will chelate with antibiotics (quinolones, tetracycine, etc)
- Methadone decreases didanosine levels. Allopurinol increases didanosine levels.

- additive peripheral neuropathy with zalcitabine, ddC

- use w/delavirdine dec AUC20%

-Use w/tipranavir results in decreased ddI conc. Separate by 2 hours.

- buffered form decreases indinavir AUV 84%

- ddI + d4T increases risk of pancreatitis, neuropathy, and hepatic dysfunction

Emtricitabine (Emtriva)

Gilead

nucleoside reverse transcriptase inhibitor (NRTI)

Capsule: 200mg

Oral Soln : 10mg/mL

Adults: 200mg po qd, 240mg oral soln (24ml) po qd

Peds (3mo-17y): 6mg/kg oral soln po qd, wt > 33kg à 200mg po qd,

Decrease dose in renal impairment

Take with or without food.

Use calibrated syringe for oral son

Screen patients for HBV

Pregnancy category: B

Common: N/D, HA, insomnia, rash, skin discoloration

More Severe: neutropenia, lactic acidosis, hepatomegally with steatosis, HBV exacerbations when d/c’d

CBC and platelet count, creatine kinase

Not metabolized by CYP enzyme system

Mainly excreted unchanged in the urine (caution with renal eliminated competitors)

Undergoes minimal glucuronidation

Cases of hepatic decompensation with ribavirin

lamivudine
(Epivir, 3TC, Epivir-HBV, for chronic hep B)
GlaxoSmithKline

nucleoside reverse transcriptase inhibitor (NRTI) Also active against Hepatitis B.

Tablet: 150mg, 300mg
Oral Soln: 10mg/ml (strawberry-banana flav.) 240ml

Epivir-HBV: 100mg tabs, 5mg/ml oral soln

Combivir is 300mg AZT, 150mg 3TC.

Trizivir is 300mg AZT, 150mg 3TC and 300mg abacavir.

Adult: 300mg daily as either 150mg bid or 300mg qd

12-16yo, <50kg: 2mg/kg po bid
Peds: 4mg/kg bid (max 150mg bid)

Neonates (investigational): 2mg/kg po bid

Renal impaired: see package insert. Dose adjustment based on ClCr

Take with or without food.

Lamivudine is also used for hepatitis B (HBV).

Do not use Epivir and Epivir-HBV interchangeably

Pregnancy Category: C

Generally well tolerated.
Minor: fatigue, N/V, diarrhea, anorexia, HA, insomnia, dizziness, arthralgia, myalgia, fever, chills, skin rash, asthenia, lipodystrophy. Possible flares of Hep B upon discontinuation.
General NRTI: Lactic acidosis, severe hepatomegaly w/ steatosis, pancreatitis (especially children).

LFTs, sCr

- Metabolized through renal excretion unchanged.
- Lamivudine and zalcitabine may inhibit intracellular phosphorylation of one another (co-administration not recommended).
- TMP/SMX may increase lamivudine AUC.

- Use with ribavirin increases risk of lactic acidosis.

stavudine
(Zerit, d4T)
Bristol -Myers Squibb

nucleoside reverse transcriptase inhibitor (NRTI)

Capsules: 15, 20, 30, 40mg
Oral soln: 1mg/ml powder (must be mixed)

Adult (>60kg): 40mg bid
Adult (<60kg): 30mg bid
Peds: 1mg/kg/ dose q12h., birth à 13 days: 0.5mg/kg bid

If Ped is 30kg or greater use adult dosing.

Dose adjustment for renal impair, dialysis, or prior peripheral neur. - see package insert

Take with or without food.

Pregnancy Category: C

Solution should appear hazy

Mild: HA, skin rash, fever, chills, N/V, diarrhea, anorexia, lipodystrophy.
Rare: anemia, hepatotoxicity, pancreatitis
Major: Peripheral neuropathy (incr. risk w/ didanosine)
General NRTI: Lactic acidosis, severe hepatomegaly w/ steatosis, pancreatitis (incr. risk w/ didanosine).

LFT

- Renal excretion 50%
- Didanosine incr risk of peripheral neuropathy and pancreatitis.

- Increased risk of neuropathy with zalcitabine, ddC

- Zidovudine may inhibit intracellular phosphorylation of stavudine (co-administration not recommended).
- Oral soln has 50mg sucrose per ml (caution diabetics)

tenofovir
(Viread, TDF)
Gilead Sciences

nucleotide reverse transcriptase inhibitor (NtRTI)

Tablet: 300mg

Adult: 300mg qd

Safety and effectiveness in pediatrics not yet established

Take with a meal to increase oral bioavailability

Pregnancy. Category: B

Most common: GI events (nausea, diarrhea, vomiting, flatulence).
Other: SOB, rash, asthenia, dizziness, weakness; renal insufficiency/ failure. Lab abnormalities similar to placebo. Bone abnormalities in animals.
General NRTI: pancreatitis, lipodystrophy, lactic acidosis, hepatomegaly w/ steatosis.

Creatinine in pts with renal dysfunction

- Small reduction in metabolism of CYP1A.
- Primarily excreted by the kidneys (glomerular filtration & tubular secretion), therefore caution with nephrotoxic agents.
- Take tenofovir 2hrs before or 1hr after didanosine (ddI)

zalcitabine
(Hivid, ddC)
Roche

nucleoside reverse transcriptase inhibitor (NRTI)

Tablet: 0.375, 0.750 mg

Planned production into 2006.

No longer recommended for HIV.

13yo-Adult: 0.750 mg q8h
Peds: 0.01mg/kg q 8 h (not approved)

Dose adjust: pts w/ dec renal fxn (CrCl<40ml/min) or hx of toxicities

Take with or without food.

Do not take with antacids or didanosine.

Pregnancy Category: C

Minor: diarrhea, N/V, anorexia, myalgia, HA, confusion, dementia, depression, arthralgia, lipodystrophy, oral and esophageal ulcers, leukopenia.
Major: Peripheral neuropathy
General NRTI: pancreatitis, lactic acidosis, hepatomegaly w/ steatosis.

CBC, LFTs, amylase, trigs, renal fx

- Renal excretion 70%
- Antacids and metoclopramide decrease absorption of zalcitabine .
- Combination with didanosine , stavudine , atazanavir or lamivudine not recommended due to inc risk of neuropathy.

- pentamidine inc pancreatitis
- Increased toxicity: Amphotericin, cimetidine , probenecid , aminoglycosides, and others that may increase risk for side effects.

zidovudine
(Retrovir, AZT, ZDV)
GlaxoSmithKline

nucleoside reverse transcriptase inhibitor (NRTI)

Tablet: 300mg
Capsules: 100mg
Syrup: 50mg/5ml (strawberry flav) 240ml

Solution for inj: 10mg/ml

Combivir is 300mg AZT, 150mg 3TC.

Trizivir is 300mg AZT, 150mg 3TC and 300mg abacavir.

Adults: 200mg tid or 300mg bid, 1mg/kg iv 5-6x/d ATC
Peds: 6wks to 12yrs- 160mg/m2 q8h (max of 200mg q8h), 120mg/m2 iv q6h 180-240mg/m2 po bid may inc compliance

Neonates- 6wks: 2mg/kgpo q6h, 1.5mg/kg iv q6h

Premature neonates (investigational): 2 mg/kg po q12h; increase to 2 mg/kg po q8h at 2 weeks for neonates >= 30 wks gestation or at 4 wks for neonates < 30 wks gestation

Take with or without food.

Dilute iv solution with D5W, infuse over 60min or civi

Pregnancy Category: C

Minor: N/V, diarrhea, anorexia, HA, insomnia, mild rash, fingernail discoloration, lipodystrophy.
Other: Myopathy w/ incr CPK, hepatitis w/ incr transaminases, hepatic failure, cardiomyopathy, neurotoxicity.
Major: Bone marrow suppression w/ anemia and/or neutropenia. Malaise, GI intolerance, asthenia.
General NRTI: Lactic acidosis, hepatomegaly w/ steatosis.

CBC and platelet count, serum creat kinase

- Metabolized to AZT glucuronide (GAZT). Renal excretion of GAZT.
- Incr zidovudine levels: fluconazole , probenecid , valproic acid , atovaquone .
- Decr zidovudine levels: nelfinavir , rifampin , ritonavir .
- Incr Hematologic toxicity: ganciclovir , interferon-alpha, bone marrow suppressants/ cytotoxic agents (dapsone, adriamycin , etc).
- Other: zidovudine may decr plasma levels of phenytoin . Doxorubicin and AZT use together should be avoided b/c of antagonistic relationship. , zidovudine inhibits phosphorylation of stavudine

lamivudine/ zidovudine
(Combivir)
GlaxoSmithKline

combination of two nucleoside reverse transcriptase inhibitors (NRTI)

Tablet: each tablet contains 150mg lamivudine and 300mg zidovudine.

Adults: one tablet bid. Peds: not recommended for pts under 12 y/o

Take with or without food.

Pregnancy Category: C

Lamivudine:
generally well tolerated.
Minor: HA, Nausea, diarrhea, abd pain, lipodystrophy, insomnia, flares of hep B when d/c. Pancreatitis in children.

Zidovudine:
Minor or rare: Myopathy w/ incr CPK, hepatitis w/ incr transaminases, hepatic failure, cardiomyopathy, fingernail discoloration, lipodystrophy, neurotoxicity
Major: Bone marrow Supression w/ anemia or neutropenia. Malaise, GI intolerance, asthenia.
General NRTI: Lactic acidosis, hepatomegaly w/ steatosis.

CBC and platelet count, serum creat kinase

See lamivudine and zidovudine

lamivudine/ zidovudine/ abacavir
(Trizivir)
GlaxoSmithKline

combination of three nucleoside reverse transcriptase inhibitors (NRTI)

Tablet: each tablet contains 150mg lamivudine, 300mg zidovudine, and 300mg abacavir

Adults: one tablet bid. Peds: Trizivir is not recommended in children who weigh less than 40kg

Take with or without food.

Pregnancy Category:C

Lamivudine:
generally well tolerated.
Minor: HA, Nausea, diarrhea, abd pain, lipodystrophy, insomnia, flares of hep B when d/c. Pancreatitis-children.

Zidovudine:
Minor or rare: Myopathy w/ incr CPK, hepatitis w/ incr transaminases, hepatic failure, cardiomyopathy, fingernail discoloration, lipodystrophy, neurotoxicity
Major: Bone marrow suppression w/ anemia or neutropenia. Malaise, GI intolerance, asthenia.

Abacavir:
Hypersensitivity reactions (~5%) -fever, skin rash, fatigue, GI (N/V, diarrhea, abdominal pain), pharyngitis, dyspnea, cough, abnormal labs (creat kinase, LFT). D/C immediately.
Other: nausea, vomiting, malaise, fatigue, HA, diarrhea, anorexia. Lab abnormalities: anemia, neutropenia, LFT, CPK, blood glucose, trigs.
General NRTI: Lactic acidosis, hepatomegaly w/ steatosis.

CBC with platelet count, serum creat kinase, LFT, amylase, lipase

See lamivudine, zidovudine and abacavir

Emtricitabine/tenofovir (Truvada)

Gilead

Combination of nucleoside reverse transcriptase inhibitor (NRTI) and nucleotide reverse transcriptase inhibitor (NtRTI)

Tablet: 200mg emtricitabine + 300mg tenofovir

Adults: 200/300mg emtricitabine/tenofovir po qd

Take with or without food.

Pregnancy Category: B

See Emtricitabine and tenofovir

Creatinine, BUN, LFTs

See Emtricitabine and tenofovir

Abacavir/lamivudine (Epzicom)

GlaxoSmithKline

combination of two nucleoside reverse transcriptase inhibitors (NRTI)

Tablet: 300mg 3TC/ 600mg ABC

Adults >40kg: 300/600 mg po qd

Not for use in patients with CrCl<50ml/min

Take with or without food.

Pregnancy Category: C

See abacavir and lamivudine AE

LFT, CBC

See abacavir and lamivudine DI

NON NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS (NNRTI'S)

delavirdine
(Rescriptor, DLV)
Agouron

Non nucleoside reverse transcriptase inhibitor (NNRTI)

Tablet: 100, 200mg

Adults: 400mg tid. The 100mg tab may be dispersed in water prior to consumption.
Peds: Safety and effectiveness in children less than 16 y/o not established.

Take with or without food.

Achlorhydric patients: take with acidic beverage

Pregnancy Category: C

Most Common: Skin rash (can usually treat through rash but sometimes will be serious)
Minor: N/V/D, HA, fatigue.

LFT if given with saquinavir

- Metabolized through CYP3A. Inhibits CYP3A and its own metabolism.
- May also be metabolized by CYP2D6.
- Has been shown in vitro to inhibit CYP2C9, 2D6, and 2C19 activity.
- Separate didanosine buffered tabs and antacids by at least one hour.

See package insert for complete list.

efavirenz
(Sustiva, EFV)
Bristol -Myers Squibb

Non nucleoside reverse transcriptase inhibitor (NNRTI)

Capsules: 50, 100, 200mg
Tablets: 600mg

Adults: 600mg qd
Peds: >40kg= 600mg qd.

If <40kg see chart in package insert

Take on an empty stomach preferably at bedtime.

Pregnancy Category: C

Most Common: CNS side effects (insomnia, depression, abnormal dreams, euphoria, confusion, agitation, amnesia, hallucinations, stupor, abnormal thinking) Minor: diarrhea, vomiting, GI complaints, dizziness, fatigue, rash (can usually treat through rash but sometimes will be serious).
Other: Incr LFT, incr triglycerides and cholesterol, lipodystrophy. Efavirenz can cause a false positive urine test for marijuana.

LFT in hepatitis pts, cholesterol, triglycerides

- Metabolized through CYP3A
- Induces CYP3A4.
- Shown in vitro to inhibit CYP2C9, 2C19, ad 3A4

See package insert for complete list.

nevirapine
(Viramune, NVP)
Boehringer-Ingelheim

Non nucleoside reverse transcriptase inhibitor (NNRTI)

Tablets: 200mg Oral Susp: 50mg/5ml (240ml)

Adults: 200mg qd x14 days then 200mg bid
Peds: 4mg/kg qd x14 days then 7mg/kg bid (pts 2mos - 8yrs). 4mg/kg qd x14days then 4mg/kg bid (pts >8yrs) MDD=400mg

Neonates-2mos:5mg/kg or 120mg/m2 qd x 14days, then 120mg/m2 bid x 14days, then 200mg/m2 bid

*start low and titrate up to account for possible autoinduction

Take with or without foods. High fat meals increase bioavailability (avoid)

Pregnancy Category: C

Most Common: Rash (can usually treat through but may be serious).
Minor: nausea, diarrhea, HA, abd pain, mouth sores, somnolence, arthralgia, lipodystrophy.
Major: Hepatotoxicity, hepatic necrosis, hepatic failure. Permanently d/c if hepatitis occurs.

LFTs

- Metabolized through CYP3A3/4
- Induces CYP3A (possible autoinduction)

-CYP3A4 substrate/inducer

- Rifampin

- Rifapentine

- OCs

- dec conc of amprenavir, indinavir, saquinavir

See package insert for complete list.

PROTEASE INHIBITORS (PI's)

amprenavir (Agenerase, APV) GlaxoSmithKline

Protease Inhibitor (PI)

Capsules: 50,.
Oral soln: 15mg/ml (240ml)

Tablets and liquid are not interchangeable on a mg per mg basis. Liquid is 14% less bioavailable

Adult: 1200mg bid or 1200mg with ritonavir 200mg qd or 600mg with ritonavir 100mg bid
Peds caps: 1200mg bid (13-16y/o, >=50kg), 20mg/kg bid or 15mg/kg tid (4-12y/o or <50kg) MDD=2400mg
Peds soln: 22.5mg/kg bid or 17mg/kg tid (4-12 or <50kg) MDD=2800mg

1400mg po bid

(13-16y/o, >=50kg),

Take with or without food. Do not take with a high-fat meal.
- 1200mg bid contains 1744IU vit E; ped soln contains 46 IU/ml
- Oral soln is contraindicated in pregnancy, infants and children <4y/o, and hepatic failure due to risk of toxicity from the large amounts of the excipient, propylene glycol.

Pregnancy Category: C

Most Common: Rash (can usually treat through but may be serious). Amprenavir is a sulfonamide and may have cross sensitivity with other dysguesia.
Minor: N/V/D, HA,circumoral paresthesia, lipodystrophy, abd pain, milk skin rash, itching, change in taste.
General PIs: diabetes/hyperglycemia, increased cholesterol and triglycerides, hemolytic anemia, increased bleeding in hemophiliacs.

Trigs, cholesterol, AST, ALT, glucose

- Metabolized through CYP3A4
- Inhibits CYP3A4

-possible inducer of 3A4

- not for use with RTV oral soln- excipient competes for elimination

- tipranavir decreases amprenavir concentrations 44-55%

- increases PDE5 inhibitor AUC

- use with delavirdine dec delavirdine con and inc amprenavir conc

-Rifampin decr amprenavir AUC 82%

-OCs

See package insert for complete list.

atazanavir (Reyataz, ATV) Bristol -Myers Squibb

Protease Inhibitor (PI)

Capsules: 100mg, 150mg, 200mg

ADULTS: 400mg po qd (ARV naïve), 300mg +100mg ritonavir (ARV-experienced, +EFV or TDF) decrease dose in hepatic impairment

-with food in enhance absorption - requires acidic pH for ATV solubility therefore separate from H2R antagonists, ppi, antacids and buffered ddI by 2hrs

-Pregnancy category B

Common: increased bilirubin, jaundice, HA, fever, arthralgia, depression, insomnia, dizziness, N/V/D, paresthesias

More Severe : prolonged PR interval, first degree AVB, rash, fat redistribution/lipid alterations (less than other PIs)

Rare : 2nd degree AVB, Stevens-Johnson syndrome, DM, spontaneous bleeding (hemophiliacs), inc LFTs

LFTs in patients with hepatitis Hx

- CYP3A4 inhibitor/substrate - CYP1A2 inhibitor

- CYP2C9 inhibitor - UGT1A1 inhibitor -tenofovir/ efavirenz decrease ATV conc -abs decreased by inc pH

see package insert for complete list

fosamprenavir (lexiva, f-APV)

GlaxoSmithKline

Protease Inhibitor (PI)

Tablets: 700mg (equivalent to 600mg APV) Suspension: 50mg/mL (INVESTIGATIONAL)

Adults: (ARV naïve) 1400mg po bid, 1400mg + 200mg RTV po qd, 700mg + 100mg po bid; (PI experienced) 700mg + 100mg RTV po bid

With EFV: 700mg + 100mg RTV bid + 600mg EFV qd or 1400mg + 300mg RTV + 600mg EFC qd

With or without food

Potential cross reaction with sulfonamide allergy

separate from H2R antagonists, ppi, antacids and buffered ddI by 2hrs

Common: N/V/D, HA, perioral paresthesias, rash

More Severe : Steven-Johnson syndrome, fat redistribution, neutropenia

Rare: DM, spontaneous bleed (hemophiliacs), hemolytic anemia, inc LFTs,

Blood glucose , lipids, LFTs

See parent drug, APV

3A4 inhibitor/substrate/possible inducer

See package insert for complete list

indinavir
(Crixivan, IDV)
Merck

Protease Inhibitor (PI)

Capsules: 100, 200, 333, 400mg

Adult: 800mg q8h
Peds: optimal dose not established., Investigational: 4-15yo: 500mg/m2 q8h
Dose adjust: when hepatic insufficiency or when given with delavirdine, itraconazole, ketoconazole, rifabutin.

Take on an empty stomach. May be given with skim milk, juice, coffee, tea or with a light snack.
- Drink at least 48 oz of water daily to prevent nephrolithiasis.
- Store in original bottle w/ desiccant.

Pregnancy Category: C

Mild: N/V/D, mild rash, heartburn, insomnia, HA, myalgia, metallic taste, blurred vision, dry skin, lipodystrophy.
Other: incr hepatic transaminases, thrombocytopenia.
Major: nephrolithiasis, Increase in bilirubin.
General PIs: diabetes/hyperglycemia, increased cholesterol and triglycerides, hemolytic anemia, increased bleeding in hemophiliacs.

bilirubin, glucose, trigs, cholesterol

- Metabolized though CYP3A4
- Inhibits CYP3A4
- Separate dose from didanosine

- Rifampin dec indinavir AUC 89%

- increases PDE5 inhibitor AUC

See package insert for complete list.

lopinavir/ ritonavir
(Kaletra, LPV/r)
Abbott

Protease Inhibitor (PI)

Capsules: each capsule contains 133.3mg lopinavir and 33.3mg ritonavir.
Tablets: contains 200mg lopinavir and 50mg ritonavir.

Oral soln: 400mg lopinavir/100mg ritonavir per 5ml (80/20mg per ml) 160ml

Adult: Pts NOT receiving NVP, APV, EFV:400/100mg (3caps, 2 tabs, or 5ml) bid

Treatment Naïve adults: 800/200 po qd

Pts receiving NVP or EFV or APV: 533/133mg bid

Treatment Naïve adults:400/100mg po bid
Peds:

6mos- 12yrs - Pts NOT receiving NVP, APV, EFV:

12/3 mg/kg (7-<15kg) bid; 10/2.5 mg/kg (15-40kg) bid. Or 230/57.5mg/m2 bid

Pts receiving NVP or EFV or APV:

13/3.25mg/kg bid (7-<15kg); 11/2.75mg/kg bid (15-50kg) or 300/75mg/m2 po bid
Investigational:

<6mos: 300/75mg/m2
MDD=400/100mg bid.

Take with food. Store capsules and liquid in refrigerator (can be at room temp for up to 2 mos.

Pregnancy Category: C

Most common: diarrhea, asthenia, fatigue, HA, nausea, skin rash (children)
Other: worsening liver disease in patients with hepatic impairment, lipodystrophy.
General Pis: diabetes/hyperglycemia, increased cholesterol and triglycerides, hemolytic anemia, increased bleeding in hemophiliacs.

LFTs, lipids, glucose

- Metabolized through CYP3A4
- Inhibits CYP3A and 2D6 (lesser extent)
- Oral solution contains alcohol (caution with metronidazole and disulfiram)

- Induces glucuronidation

- increases PDE5 inhibitor AUC

See package insert for complete list.

nelfinavir
(Viracept, NFV)
Agouron

Protease Inhibitor (PI)

Tablets: 250mg, 625mg
Oral powder: 50mg/g (5 scoops = 250mg)

Adult: 750mg tid or 1250mg bid.
Peds (2-13yo): 45-55mg/kg bid, 25-35mg/kg tid tid

Take with a meal or a light snack.
- Tablet may be dissolved in water or crushed and mixed with food.

- Pwd should be mixed with water, milk, soy milk, baby formula, or dietary supp drink. Measure using scoop provided. Do not mix with acidic beverages.

Pregnancy Category: B

Most Common: Diarrhea, soft stools.
Minor: HA, fatigue, N/V, flatulence, anorexia, myalgia, arthralgia, asthenia, rash, lipodystrophy, mood changes.
General PIs: diabetes/hyperglycemia, increased cholesterol and triglycerides, hemolytic anemia, increased bleeding in hemophiliacs.

Lipids, glucose

- Metabolized through CYP3A4 and CYP2C19
- Inhibits CYP3A4

- increases PDE5 inhibitor AUC

See package insert for complete list.

ritonavir
(Norvir, RTV)
Abbott

Protease Inhibitor (PI)

Capsule: 100mg

Oral soln: 600mg/7.5ml (43% alcohol)

Adult: 600mg bid (dose titration starting at 300mg bid inc over 5d may help reduce AE).
Peds:

>1mo

350- 400mg/m2 q12h (start at 250mg/m2 and titrate up q3-3d by 50mg/m2).
- Often used in combination with other ARV at doses of 100-400mg bid

Take with food
- Store capsules in refrigerator (room temp ok for 30 days); store oral soln at room temp (shake well)
- Soln can be mixed with choc milk or nutritional drink supplement.

Pregnancy Category: B

Most Common: GI events (N/V/D)
Other: abd pain, anorexia, change in taste, myalgias, throat irritation, dizziness, somnolence, rash diaphoresis, lipodystrophy, paresthesias, HA, hyperlipidemia, increased CPK and uric acid, liver toxicity.
General PIs: diabetes/hyperglycemia, increased cholesterol and triglycerides, hemolytic anemia, increased bleeding in hemophiliacs.

Trigs, cholesterol, LFTs, CPK, uric acid, glucose

- Extensively metabolized by CYP3A (high first pass metabolism)
- Inhibits CYP3A and 2D6 (lesser extent)
- May induce CYP3A, glucuronosyl transferase, CYP1A2, and 2C9.

- increases PDE5 inhibitor AUC

- Liquid contains alcohol (caution with metronidazole and disulfiram)

saquinavir
(Invirase, SQV)
Roche

Protease Inhibitor (PI)

Capsules: 200mg (Invirase- saquinavir mesylate);

Adult: Invirase- 1000 mg bid(use w/RTV 100mg boost or w/2 Kaletra tabs)

Peds: safety and efficacy in children <16 not established

Take within 2 hours of a full meal

Most common: GI events (N/V/D)
Other: HA, heartburn, anxiety, somnolence, mild rash, paresthesias, myalgia, depression, dysguesia, mouth ulcers or sores, lipodystrophy, liver damage, pancreatitis.
General PIs: diabetes/hyperglycemia, increased cholesterol and triglycerides hemolytic anemia, increased bleeding in hemophiliacs.

Trigs, cholesterol, glucose

- Metabolized by CYP3A
- Inhibits CYP3A personnel

-P-glycoprotein substrate

-ritonavir inc SQV conc 20-fold

- increases PDE5 inhibitor AUC

tipranavir (Aptivus, TPV) Boehinger Ingelheim Pharmaceuticals, Inc.

Nonpeptide Protease Inhibitor (PI)

Capsules : 250mg

Adults : 500mg po bid (boosted with 200mg ritonavir bid)

- take with food - bioavailability increase with high fat meal -cross sensitivity in sulfonamide allergic patients -Pregnancy Category C

Common: D/N/V, fatigue, HA, rash More Severe: fat redistribution, hepatitis/hepatic decompensation (inc risk in chronic hep pts) Rare: DM onset/exacerbations Lab Alterations: inc LFTs, cholesterol, TGs

LFTs (baseline and routine monitoring), lipids, TG

- metabolized by CYP 3A4 -3A4 inducer -CYP2D6 inhibitor (clinical significance unknown) -P-glycoprotein substrate/weak inhibitor/possible inducer -caps contain alcohol See package insert for complete list

FUSION INHIBITORS

enfuvirtide (Fuzeon, T-20) Roche Laboratories

Fusion Inhibitors

Single use powder for injection vials: 108mg resulting in 90mg/mL (60vials/box, kit contains SWFI, lyophilized powder, syringes, alcohol wipes)

ADULTS: 90 mg SQ bid PEDS (6-16yo): 2mg/kg SQ bid (approval is for treatment-experienced pts)

-reconstitute with 1.1ml SWFI, may take up to 45min to dissolve, reconstituted product must be used w/in 24h -SQ injection: upper arm, anterior thigh, abdomen. Rotate site

Common : injection site reaction, N/D, fatigue More Severe: increased rate of pneumonia (association unclear) Rare: hypersensitivity reaction, immune-mediated reactions Lab Alterations: eosinophilia, inc LFTs, incTG, inc amylase/lipase, inc creatinine phosphokinase

CBC + diff, LFTs

no CYP metabolism, no interactions currently available, (patel et al Clinical Pharmacokinetics 2005)