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Once a day drugs and boosted PIs are highlighted in green
 

ABACAVIR SULFATE

(Ziagen)

300 mg BID
or
300 mg 2 taken once a day (not FDA-approved)
 

Tablets: 300 mg; Liquid 20 mg/ml
 

Take with/without food

• Headache, malaise

• Nausea, vomiting

• Diarrhea

• Hypersensitivity reaction 2-5% (fever, nausea, vomiting, rash, diarrhea, SOB)
• Rare: lactic acidosis

• Perform HLA-B5701 test prior to using this drug, and administer drug only if the test is nonreactive or negative.
• STOP only if CERTAIN that patient is hypersensitive.

DO NOT RECHALLENGE.

DIDANOSINE (ddI)

(Videx)

wt > 60 kg:  2 x 100 mg BID
 

wt < 60 kg: 125 mg bid

Tablets: 25 mg, 100 mg, 150 mg, 200 mg

Powder: 100 mg, 167 mg, 250 mg packets

Take on empty stomach 1/2 hour ac or 1 hour pc. Must have dose in 2 tabs. Chew tablets or dissolve in H2O.

Dose reduction for renal impairment

• Nausea • Diarrhea

• Headache

• Pancreatitis, possibly fatal

• Peripheral neuropathy
• Rare: lactic acidosis

• Contraindicated in patients with history of alcoholism, pancreatitis (do baseline lipase)

• This form of didanosine has been largely replaced by Videx EC
• No alcohol. Can be taken on an empty stomach with other antiretrovirals.

DIDANOSINE (ddI)

(Videx EC)

400 mg once daily
 

Capsules 125 mg, 200 mg, 250 mg, 400 mg
 

Take on empty stomach. Swallow capsule whole
Dose reduction for renal impairment

• Nausea • Diarrhea

• Headache

• Pancreatitis, possibly fatal

• Peripheral neuropathy
• Rare: lactic acidosis

• No alcohol. Can be taken on an empty stomach with other antiretrovirals.

• Adherence enhanced with use of ddI-EC formulation
• Contraindicated in patients with history of alcoholism, pancreatitis (do baseline lipase or p-amylase)

• Administration with tenofovir results in blunting of CD4 increase or even decreases in CD4

EMTRICITABINE (FTC)

(Emtriva)

200 mg once daily capsules
 

Take with or without food
 

Dose reduction for renal impairment

• Well tolerated

• Skin discoloration

• Possible flare-up of HBV when discontinued
• Rare: lactic acidosis

• Active against HBV 
• Therapy with emtricitabine should not be stopped suddenly unless other potent antiretrovirals are substituted for at least 48-72h

LAMIVUDINE (3TC)

(Epivir)

150 mg BID or 300 mg once a day

<50 kg: 2 mg/kg BID

Tablets 150 mg; Liquid 10 mg/ml

Dose reduction for renal impairment

Take with/without food

• Well tolerated

• Possible flare-up of HBV when discontinued
• Rare: lactic acidosis

• ddC/3TC or ddI/3TC combinations contraindicated

• Active against HBV
• Therapy with lamivudine should not be stopped suddenly unless other potent antiretrovirals are substituted for at least 48-72h

STAVUDINE (d4T)

(Zerit)

40 mg bid

Capsules: 15 mg, 20 mg, 30 mg, 40 mg

wt > 60 kg: 40 mg q 12 hours

wt < 60 kg: 30 mg q 12 hours

Dose reduction for renal impairment

Take with/without food

• Peripheral neuropathy

• Fat redistribution syndrome

 • High potential for mitochondrial toxicity

• Rare: lactic acidosis

• AZT/d4T combination contraindicated

• ddI/d4T contraindicated during pregnancy
• Use other NRTI options if available due to increased risk of mitochondrial toxicity associated with this agent.

TENOFOVIR (TDF)

(Viread)

300 mg daily with food
 

Dose reduction for renal impairment

• Possible nephrotoxicity

• Possible flare-up of HBV on d/c

• Possible bone loss
• Rare: lactic acidosis

• Active against HBV

• Significantly increases DDI levels

• Follow renal function when using multiple nephrotoxins including NSAIDs
• Administration with didanosine may result in blunting of CD4 increase or even decreases in CD4

ZALCITABINE (ddC)

(Hivid)

0.75 mg every 8 hours

Tablets: 0.375 mg, 0.75 mg

Dose reduction for renal impairment

Take with/without food

• Peripheral neuropathy

• Stomatitis
• Rare: lactic acidosis

• Take with/without food

• ddI/ddC, d4T/ddC or 3TC/ddC  combinations contraindicated

• This drug is generally not recommended due to toxicity and lower efficacy 

ZIDOVUDINE (AZT)

(Retrovir)

300 mg twice a day
 

Capsules 100 mg;  Tablets 300 mg; Liquid 50 mg/5 ml

Dose reduction for renal impairment

Take with/without food

• Anemia/neutropenia

• Nausea/myopathy

• Headache/insomnia
• Rare: lactic acidosis

• FDA approved for use in pregnancy to decrease perinatal transmission as part of combination therapy or monotherapy as a minimum
 

 DELAVIRDINE

(Rescriptor)

 600 mg BID or 400 mg 3 times per day

Tablets 100 mg, 200 mg

May drop 4-6 tabs in 3 oz water to produce suspension

• Rash

• Headaches

• Hepatitis

• Antacids and ddI: separate administration by 1 hr

• Multiple drug interactions

• Increases AUC of other PIs

• No data with oral contraceptives
• This NNRTI is not recommended due to higher pill burden, higher dosing frequency, and meal dependence.

EFAVIRENZ

(Sustiva)

600 mg PO at bedtime or once daily
 

Capsules: 50, 100, 200, 600 mg

• Rash 
• CNS symptoms: dizziness, somnolence, insomnia, abnormal dreams, confusion, impaired thinking   
• Increased LFTs in patients with prior history of hepatitis B and/or C

• False positive screening cannabinoid test possible

• Multiple drug interactions

• Pregnancy should be avoided. Barrier contraception should always be used in combination with other methods of contraception (oral or other hormonal contraceptives)

• Not recommended in combination with saquinavir as a sole PI

• Take with/without food. Avoid high fat meals

• Avoid coadministration with clarithromycin

• Therapy with efavirenz should not be stopped suddenly unless other potent antiretrovirals are substituted for at least 2-4 weeks.

 NEVIRAPINE

(Viramune)

200 mg once a day x 14 days,

then 200 mg twice a day

or
2 x 200 mg once a day
 

Tablets: 200 mg

Liquid: 50 mg/5 ml

• Rash, usually mild but possibly severe (Stevens Johnson)

• Hepatitis which may be severe

• Take with/without food

• Discontinue in patient with severe rash or rash with fever, blistering, oral lesions, conjunctivitis, swelling, muscle/joint aches.

• Reduces effectiveness of oral contraceptives

• Multiple drug interactions

• QD dosing slightly more hepatotoxic
• Therapy with nevirapine should not be stopped suddenly unless other potent antiretrovirals are substituted for at least 2-4 weeks.

• Avoid starting this drug in females with CD4 > 250 or males with CD4 > 400

• Diarrhea, N&V
• Rash 10-15%

• Headache

• Hepatitis

• Hyperlipidemia

• Hyperglycemia
• Fat redistribution

• Always taken with ritonavir

• Contains sulfonamide component (use cautiously with sulfonamide allergy)

• Take with food

• Contraindicated with moderate or severe hepatic dysfunction

• Monitor liver enzymes, lipids, serum glucose
• Studied only in salvage situations by the time of approval
• Should not be taken with other protease inhibitors except for ritonavir

Approved by US FDA 6.22.2005

AMPRENAVIR

(Agenerase)

8 x 150 mg twice a day
 

Capsules 50 mg, 150 mg, liquid 15 mg/ml

Capsules and oral solution are not interchangeable on a milligram per milligram basis
 

Administer with/without food (avoid high fat meals) 

• N&V, diarrhea

• Rash

• Circumoral paresthesia

• Not recommended to use with oral contraceptives

• Hyperlipidemia

• Hyperglycemia
• Fat redistribution

• Large capsule size and high pill burden

• Do not take with vitamin E supplement

• Take at least 1 hour before or after use of antacids or ddI

• Patients with impaired hepatic function require dosage adjustment

• Increase dose when combined with efavirenz

Amprenavir has been largely replaced by its prodrug fosamprenavir which is better tolerated and has a much lower pill burden.  GlaxoSmithKline ceased production of amprenavir in October 2007.

Tablets 300 mg

Administer both medications with food.
 

• N&V, diarrhea

• Rash

• Circumoral paresthesia

• Not recommended to use with oral contraceptives

• Hyperlipidemia

• Hyperglycemia
• Fat redistribution

FOSAMPRENAVIR

(Lexiva)

1 x 700 mg BID + 100 mg ritonavir twice a day

for treatment naive pts only:

2 x 700 mg daily + ritonavir 1-2 x 100 mg daily
 

• N&V, diarrhea

• Rash

• Hyperlipidemia?

• Hyperglycemia?
• Fat redistribution?

• Take at least 1 hour before or after use of antacids or ddI?

• Patients with impaired hepatic function require dosage adjustment?

• Increase dose when combined with efavirenz?
• Ritonavir 100 mg + Lexiva 2 x 700 mg approved in late 2007 - for treatment naive patients

Approved 10.20.2003

ATAZANAVIR

(Reyataz)

2 x 200 mg once daily
 

Capsules: 100 mg, 150 mg, 200 mg
Take with food

With concomitant efavirenz and/or tenofovir:

1 x 300 mg or 2 x 150 mg daily + ritonavir 100 mg daily
 

• GI intolerance

• Hepatitis

• Only PI approved for once daily dosing

• Possibly less hyperlipidemia than other PIs

• No significant interaction with oral contraceptives

• Dose adjustment/interaction with efavirenz & tenofovir suggested (nevirapine interaction unknown 10.2003)

INDINAVIR

(Crixivan)

2 x 400 mg every 8 hours
(at least 1 hr ac or 2 hr pc)
 

Capsules: 200 mg, 330 mg, 400 mg
 

May take with skim milk, juice or light meal

Decrease dose to 600 mg q 8 hrs with ketoconazole/itraconazole

• Kidney stones

• Hyperbilirubinemia

• GI intolerance

• Hyperlipidemia

• Hyperglycemia
• Fat redistribution

• Maintain adequate hydration at least 48 oz H₂O/day

• Grapefruit juice decreases indinavir levels by 26%

• Keep in original container with dessicant

• Can use with oral contraceptives

• Separate by 2 hrs from ddI

• Increase dose when combined with efavirenz

LOPINAVIR / RITONAVIR

(Kaletra)

2 film-coated tablets twice a day
Take with or without food
Dosing form of choice!

3 capsules twice a day
or one teaspoon liquid BID

Singe daily dosing for antiretroviral naïve patients

6 capsules once a day with food

Capsules 133/33mg, liquid 400/100 mg

per 5 cc

Take with food

• Diarrhea, N&V

• Headache

• Hepatitis

• Hyperlipidemia

• Hyperglycemia
• Fat redistribution
 

• Many, many drug interactions

• Reduces effects of oral contraceptives

• Liquid form contains ethanol

• Increase dose when combined with efavirenz

• Increased GI side effects with single daily dosing

Single daily dosing approved 4.29.2005

Film-coated tablets approved 8.28.2005

NELFINAVIR

(Viracept)

2 x 625 mg BID or  or 3 x 250 mg TID

with meal or light snack
Tablets 250 mg, 625 mg; 50 mg/g oral powder

With concomitant efavirenz or nevirapine:
6 x 250 mg bid
 

• Diarrhea (reduced with calcium supplement or fiber)

• Hyperlipidemia

• Hyperglycemia
• Fat redistribution

• Reduces effectiveness of oral contraceptives

• Increase dose when combined with efavirenz

RITONAVIR

(Norvir )

6 x 100 mg BID with food

(start with 300 mg BID and dose escalate over next 1-2 weeks).

Caps 100 mg.  Oral solution 600 mg/7.5 ml

Separate by ≥ 2 hrs from didanosine buffered form.

• N&V, diarrhea

• Taste perversion

• Circumoral and peripheral paresthesia

• Hepatitis

• Hyperlipidemia

• Hyperglycemia

• Fat redistribution

• Elevated CPK and uric acid levels
 

• Refrigerate capsules but not liquid

• Has multiple possible drug interactions

• Formulated in alcohol. Do not give to pts taking disulfiram

• Reduces effectiveness of oral contraceptives

• Used to boost other protease inhibitors (see below)

• Increase dose when combined with efavirenz
 

SAQUINAVIR

(Fortovase )

Soft Gel Capsules (SGC)

1600 mg twice a day
or 6 x 200 mg three times per day
 

Take with food containing fat.
 

Capsules: 200 mg

• Diarrhea/nausea

• GI intolerance 

• Elevated transaminase levels

• Headache

• Hyperglycemia

• Fat redistribution and lipid abnormalities
 

• Can use with oral contraceptives

• Grapefruit juice and ketoconazole increase levels

• Stable at room temperature for 3 months

• Increase dose when combined with efavirenz
• Boosting with ritonavir is usually preferable

• Production of this drug will cease in 2006.  Replace with equivalent dose of hard gel cap form of the drug (Invirase)

SAQUINAVIR

(Invirase)

Hard Gel

Capsules

(HGC)

Capsules: 200 mg or 500 mg

Invirase 2 x 500 mg BID with food
+
Ritonavir 100 mg BID with food

Used mainly in boosted regimes (see below)
Take with food.

• Diarrhea/nausea

• GI intolerance 

• Elevated transaminase levels

• Headache

• Hyperglycemia

• Fat redistribution and lipid abnormalities

• Can use with oral contraceptives

• Grapefruit juice and ketoconazole increase levels

• Stable at room temperature for 3 months

• Increase dose when combined with efavirenz

500 mg hard gel cap FDA approved 12.23.2004 and available 2.18.2005

ENFUVIRTIDE

(Fuzeon)

90 mg injected SQ every 12 hours

Vial: 90 mg/1cc

Injection site reactions: erythema, induration, pain/tenderness

Expensive, labor-intensive therapy for deep salvage in highly motivated patient only

Must be used with at least two other active antiretrovirals or resistance develops rapidly

MARAVIROC

(Selzentry)

Orthostatic hypotension

Rare and possibly severe hepatitis

Tropism assay required before use: the results must indicate the absence of X4 virus.

1.  8 x 200 mg saquinavir hard-gel capsule
 +
100 mg ritonavir
both once a day with food

2.  2 x 500  mg saquinavir hard-gel capsule
+
100 mg ritonavir,
both bid with food

3.  5 x 200  mg saquinavir hard-gel capsule
+
100 mg ritonavir,
both bid with food

4.  2 x 200  mg saquinavir hard-gel capsule
+
4x100 mg ritonavir
both bid with food

2 x 400 mg indinavir bid

+
1-2 x 100 mg ritonavir bid
with or without food

Hyperlipidemia, hepatitis, fat redistribution, diarrhea, abdominal pain, chapped lips, nephrolithiasis

Lopinavir/ritonavir
boosted with
ritonavir

Fosamprenavir
boosted with
ritonavir

2 x 700 mg fosamprenavir
+
2 x 100 mg ritonavir
both once a day
or
700 mg fosamprenavir
+
100 mg ritonavir
Both twice a day

Nausea, headache, rash, diarrhea

Newest PI with least experience but appears to be an excellent option anecdotally.

Once a day option is not to be used for antiretroviral-experienced patients

Saquinavir
combined with
lopinavir/ritonavir

Lopinavir/ritonavir
combined with
indinavir

efavirenz 600 mg
emtricitabine 200 mg
tenofovir 300 mg
 

emtricitabine 200 mg
tenofovir 300 mg