Patient meds … more important than you think

Dental Assistant, The, Sept-Oct, 2002 by Diane Chandler, Michael Palmer

FDA APPROVED ANTIRETROVIRAL AGENTS FOR THE TREATMENT OF HIV INFECTION

Drug                  Dosage Forms               Usual Dose

Nucleoside Reverse Transcriptase Inhibitors (NRTIs)

zidovudine (ZDV,      100 mg capsule,            200 mg tid or
AZT) (Retrovir[R]);   300 mg tablet; 10 mg/ml    300 mg bid
with lamivudine as    syrup; 10 mg/ml IV;        (500-600 mg/day);
Combivir[R] or        Combivir[R] and            Combivir[R] or
lamivudine and        Trizivir[R] are tablets    Trizivir[R]: one
abacavir as           [double dagger]            tab bid
Trizivir[R]

didanosine (ddl)      25, 50, 100, 150, 200 mg   200 mg bid (> 60 kg)
(Videx[R],            chewable tablets           125 mg bid (< 60 kg)
Videx EC[R])          buffered powder for oral   250 mg bid (> 60 kg)
                      solution [dagger]: 100,    167 mg bid (< 60 kg)
                      167, 250 mg packets
                      250, 400 mg enteric        400 mg qd (> 60 kg)
                      coated capsules            250 mg qd (< 60 kg)

zalcitabine (ddC)     0.375, 0.75 mg tablets;    0.75 mg tid (> 60kg)
(Hivid[R])            0.1 mg/ml solution         0.375 mg tid (< 60 kg)
                      (investigational)

stavudine (d4T)       15, 20, 30, 40 mg          20-40 mg bid (> 60 kg)
(Zerit[R])            capsules;                  15-30 mg bid (< 60 kg)
                      1 mg/ml solution

lamivudine (3TC)      150 mg tablets;            150 mg bid
(Epivir[R]) or with   10 mg/ml syrup             2 mg/kg bid if < 50 kg
zidovudine                                       Combivir[R]: one
as Combivir[R]                                   tab bid
[double dagger]

abacavir (ABC,        300 mg tablets;            300 mg bid
1592) (Ziagen[R])     20 mg/ml solution
or with lamivudine                               Trizivir[R]: one
and zidovudine as                                tab bid
Trizivir[R]
[double dagger]

Nonnucleoside Reverse Transcriptase Inhibitors (NNRTIs)

nevirapine (NVP)      200 mg tablets;            200 mg daily for 14
(Viramune[R])         10 mg/ml suspension        days, then if no rash
                      (investigational)          [up arrow] to 200 mg
                                                 bid

delavirdine (DLV)     100, 200 mg tablets        400 mg tid (2x200 mg
(Rescriptor[R])                                  tabs in > 3oz of water
                                                 to produce a slurry)

efavirenz (EFV)       50, 100, 200 mg capsules   600 mg qd
(Sustiva[R])

Protease Inhibitors (Doses listed are for use as the sole PI) [section]

saquinavir *,         200 mg hard gel capsules   600 mg tid *
** (HG-SAQ)
(Invirase[R])
saquinavir **                                    1200 mg tid
(SG-SAQ)
(Fortovase[R])        200 mg soft-gel capsules

ritonavir (RTV)       100 mg capsules or         titration schedule:
(Norvir[R])           80 mg/ml oral solution     300 mg bid (1 day);
                      (43% alcohol; both         400 mg bid (2 days);
                      contain a significant      500 mg bid (1 day);
                      amount of alcohol)         then 600 mg bid
                                                 thereafter

indinavir (IDV)       200, 400 mg capsules       800 mg q 8h (dose
(Crixivan[R])                                    adjustment required
                                                 for liver disease)
                                                 [up arrow] to 1000 mg
                                                 q 8h if given with NVP
                                                 or EFV

nelfinavir (NFV)      250 mg tablets             750 mg tid
(Viracept[R])         50 mg/gm oral powder       or 1250 mg bid

amprenavir (APV)      150 mg tablets             1200 mg bid
(Agenerase[R])        [double dagger]            solution: 15 mg/kg tid
                      15 mg/ml oral solution     or 20 mg/kg bid
                                                 (< 50 kg)

lopinavir/ritonavir   133.3 mg lopinavir and     3 capsules bid or
(LPV/RTV)             33.3 mg ritonavir/         5 ml of solution bid
(Kaletra[R])          capsule oral solution:
                      80 mg lopinavir/
                      20 mg ritonavir per ml
                      (42% alcohol)

Nonnucleotide Reverse Transcriptase Inhibitor

tenofovir             300 mg tablet              300 mg qd
disoproxil
[subsection]
fumurate (DF)

                      Common/Serious          Patient Instruction/
Drug                  Adverse Effects            Administration

Nucleoside Reverse Transcriptase Inhibitors (NRTIs)

zidovudine (ZDV,      Headache, nausea,       Nausea and vomiting
AZT) (Retrovir[R]);   vomiting, diarrhea,     is self-limiting and
with lamivudine as    insomnia, anemia        will resolve within a
Combivir[R] or        (decrease dose to       few weeks. Take with
lamivudine and        100 mg tid if           meals to minimize
abacavir as           needed), hepatitis;     nausea and vomiting.
Trizivir[R]           lactic acidosis and
                      hepatomegaly

didanosine (ddl)      Diarrhea, nausea,       Chew two buffered
(Videx[R],            vomiting, peripheral    tablets/dose on empty
Videx EC[R])          neuropathy,             stomach (1 hour
                      pancreatitis; lactic    before meals or 2
                      acidosis and            hours after meals);
                      hepatomegaly            bid dosing preferable
                                              to once daily dosing
                                              with the buffered
                                              formulation. Swallow
                                              one EC capsule daily
                                              on empty stomach.

zalcitabine (ddC)     Nausea, peripheral      Can be given with
(Hivid[R])            neuropathy, apthous     meals. See Patient
                      ulcer, pancreatitis;    Instructions/
                      lactic acidosis and     Administration under
                      hepatomegaly            ZDV.

stavudine (d4T)       Headache, peripheral    Can be given with
(Zerit[R])            neuropathy; lactic      meals. See Patient
                      acidosis and            Instructions/
                      hepatomegaly            Administration under
                                              ZDV.

lamivudine (3TC)      Headache, fatigue,      Can be given with
(Epivir[R]) or with   nausea, pancreatitis    meals. See Patient
zidovudine            in children, lactic     Instructions/
as Combivir[R]        acidosis and            Administration under
[double dagger]       hepatomegaly            ZDV.

abacavir (ABC,        Nausea, vomiting,       Can be given with
1592) (Ziagen[R])     headache, malaise,      meals.
or with lamivudine    diarrhea, abdominal
and zidovudine as     pain. 3-5%
Trizivir[R]           hyper-sensitivity
[double dagger]       reaction which can
                      be life threatening
                      (DO NOT rechallenge),
                      lactic acidosis and
                      hepatomegaly

Nonnucleoside Reverse Transcriptase Inhibitors (NNRTIs)

nevirapine (NVP)      Skin rash can be        Can be given with
(Viramune[R])         severe, headache,       meals and with ddl.
                      nausea, hepatitis       Instruct patients
                                              about warning
                                              symptoms for rash and
                                              hepatitis during the
                                              first 6-8 weeks of
                                              NVP use.

delavirdine (DLV)     Rash, headaches,        Can be given with
(Rescriptor[R])       hepatitis               meals; separate
                                              administration from
                                              ddl or antacids by
                                              > 1 hour.

efavirenz (EFV)       Headaches, dizziness,   Can be given with
(Sustiva[R])          "disconnected"          meals. CNS symptoms
                      light-headedness,       are transient and
                      rash, hepatitis         usually resolve
                                              within 4 weeks.

Protease Inhibitors (Doses listed are for use as the sole PI) [section]

saquinavir *,         GI (diarrhea, nausea,   Use of HG-SAQ is not
** (HG-SAQ)           abdominal pain),        recommended, except
(Invirase[R])         headache, elevated      in combination with
saquinavir **         LFTs, hyperlipidemia,   ritonavir. Take 6
(SG-SAQ)              hyperglycemia,          soft gel capsules per
(Fortovase[R])        lipodystrophy           dose tid with large
                      Generally well          meal. Grapefruit
                      tolerated.              juice may [up arrow]
                                              saquinavir
                                              absorption.

ritonavir (RTV)       GI (nausea, diarrhea,   Take 6 capsules/dose
(Norvir[R])           vomiting, anorexia,     bid with meals to
                      abdominal pain);        minimize GI symptoms;
                      neurologic: fatigue,    can mix oral solution
                      weakness, numbness,     with Advera[R],
                      tingling around the     chocolate milk, or
                      lips, headache,         Ensure[R].
                      dizziness, antabuse
                      reactions (alcohol
                      content),
                      hyperlipidemia,
                      hyperglycemia,
                      lipodystrophy,
                      hepatitis

indinavir (IDV)       Kidney stones, GI       Take 2 capsules/dose
(Crixivan[R])         (nausea, diarrhea,      q 8h on an empty
                      vomiting, abdominal     stomach (1 hr before
                      pain); neurologic:      or 2 hours after a
                      headaches, insomnia,    meal) or with a light
                      change in taste, dry    meal (skim milk,
                      skin, hair loss,        juice, coffee, tea,
                      hyperlipidemia,         dry toast, corn
                      hyperglycemia,          flakes). Avoid high
                      lipodystrophy,          fat, protein, caloric
                      hepatitis               meal which [down
                                              arrow] s absorption.
                                              Drink [greater than
                                              or equal to] 6
                                              glasses [H.sub.2]O
                                              per day to prevent
                                              kidney stones.

nelfinavir (NFV)      Diarrhea, nausea,       Take 3 tablets per
(Viracept[R])         hyperlipidemia,         dose with meals tid
                      hyperglycemia,          or 5 tablets per dose
                      lipodystrophy,          with meals bid.
                      hepatitis

amprenavir (APV)      Diarrhea, nausea,       Take 8 tablets per
(Agenerase[R])        vomiting, rash,         dose bid with a low
                      perioral                fat meal.
                      paresthesias,
                      hyperlipidemia,
                      hyperglycemia,
                      lipodystrophy,
                      hepatitis

lopinavir/ritonavir   Diarrhea, nausea,       Take 3 capsules per
(LPV/RTV)             fatigue, headache,      dose or 5mL/dose with
(Kaletra[R])          hyperlipidemia,         food bid. If
                      hyperglycemia,          co-administered with
                      lipodystrophy,          NVP or EFV, increase
                      pancreatitis,           to 4 capsules/dose or
                      hepatitis               6.7 mL/dose bid.

Nonnucleotide Reverse Transcriptase Inhibitor

tenofovir             No renal toxicity       Available by expanded
disoproxil            reported; generally     access from Gilead
[subsection]          well tolerated.         Sciences:
fumurate (DF)                                 1-800-GILEAD-5

[dagger] Available as a pediatric powder 2 gm/200 ml or 4 gm/400 ml
(dilute with antacid 10 mg/ml).

** Do not administer as sole protease inhibitor with efavirenz or
nevirapine.

[double dagger] Combivir[R] tablets contain 150 mg lamivudine / 300 mg
zidovudine, Trizivir[R] tablets contain 300 mg abacavir, 150 mg
lamivudine, 300 mg zidovudine.

[double daggers] Each 150 mg tablet contains 109 IU vitamin E. Each 1
mL contains 46 IU vitamin E.

* Doses of 3200-7200 mg/day are more effective but not FDA approved.

[section] See Table 1 for examples of dual PI dosing.

[subsection] Investigational agent; new drug application submitted to
FDA 5/1/2001.