Basic
Informations
Aptivus is an HIV medication.
It is in a category of HIV medicines called protease inhibitors
(PIs). Aptivus prevents cells infected by HIV from producing new
virus. This reduces the amount of virus in your body.
Aptivus must be used in combination with Norvir (ritonavir) and
other HIV drugs.
Aptivus, manufactured by Boehringer Ingelheim, was approved for the
treatment of HIV by the U.S. Food and Drug Administration (FDA) in
June 2005. Aptivus/ritonavir is only approved for HIV-infected
people who have tried and failed HIV drug regimens (including those
containing protease inhibitors) in the past. It is not approved for
HIV-infected people starting HIV treatment, or a protease inhibitor,
for the first time (unless they were infected with a strain of HIV
resistant to multiple protease inhibitors).
Drugs
Interactions
Because of the ways Aptivus
and ritonavir are metabolized (broken down) in the body, they can
interact with many other medications used to treat HIV, AIDS-related
complications, and other diseases. Aptivus/ritonavir may cause blood
levels of other medications to be become too low (which can decrease
their effectiveness) or high (which can increase the risk of side
effects). Similarly, other medications may cause blood levels of
Aptivus and/or ritonavir to become too low or high.
Tell your doctors and pharmacists about all medicines you take. This
includes those you buy over-the-counter and herbal or natural
remedies, such as St. John's wort. Bring all your medicines when you
see a doctor, or make a list of their names, how much you take, and
how often you take them. Your doctor can then tell you if you need
to change the dosages of any of your medications.
The following medications should not be taken while you are being
treated with Aptivus/ritonavir:
-
Acid reflux/heartburn
medications: Propulsid (cisapride)
-
Antibiotics: Rifadin
(rifampin)
-
Antimigraine medications:
Methergine, Methylergometrine (methylergonovine); Ergostat,
Cafergot, Ercaf, Wigraine (ergotamine); Ergotrate, Methergine
(ergonovine); or D.H.E. 45, Migranal (dihydroergotamine)
-
Heart medications:
Cordarone (amiodarone), Vascor (bepridil), Tambocor
(flecainide), Rythmol (propafenone), or Quinaglute/Quinidex
(quinidine)
-
Cholesterol-lowering drugs
(statins): Zocor (simvastatin) and Mevacor (lovastatin)
-
Antipsychotics: Orap
(pimozide)
-
Sedatives: Versed
(midazolam) and Halcion (triazolam)
-
Enlarged Prostate:
UroXatral (alfuzosin)
-
Pulmonary Hypertension:
sildenafil, used as Revatio
-
Herbal products: St.
John's wort
Aptivus/ritonavir can greatly
decrease the levels of other protease inhibitors—including Lexiva (fosamprenavir),
Kaletra (lopinavir), Reyataz (atazanavir) and Invirase (saquinavir)—in
the blood. It is currently recommended that Aptivus/ritonavir not be
taken with other protease inhibitors, until adequate
drug-interaction and dosing studies have been completed.
Aptivus/ritonavir can interact with HIV nucleoside reverse
transcriptase inhibitors (NRTIs). Aptivus/ritonavir decreases Ziagen
(abacavir) levels in the blood by 40% and Retrovir (zidovudine)
levels by 35%. It might be necessary to increase the doses of Ziagen
or Retrovir, if they are combined with Aptivus/ritonavir. However,
no dosing recommendations have been made. Aptivus/ritonavir can also
decrease levels of Videx EC (didanosine) in the blood. In turn,
Aptivus/ritonavir should be taken at least two hours before or two
hours after taking Videx/Videx EC.
Aptivus/ritonavir can interact with some medications used to treat
thrush (candidiasis) and other fungal infections. Diflucan (fluconazole)
can increase Aptivus levels in the blood, but dose adjustments are
not necessary. Aptivus/ritonavir may increase Sporanox (itraconazole)
or Nizoral (ketoconazole) levels in the bloodstream (total daily
doses of Sporanox and Nizoral should not exceed 200mg). It is also
possible that Aptivus/ritonavir either increases or decreases Vfend
(voriconazole) levels in the blood.
Aptivus/ritonavir can interact with some medications used to treat
TB, MAC, and other bacterial infections. Aptivus/ritonavir raises
Biaxin (clarithromycin) levels in the bloodstream. Similarly, Biaxin
raises Aptivus levels in the bloodstream. The dose of Biaxin does
not need to be decreased, although this may be necessary in people
with altered kidney function. Aptivus/ritonavir can also increase
Mycobutin (rifabutin) levels in the bloodstream. If Mycobutin is
taken at the same time as Aptivus/ritonavir, it is recommended that
the Mycobutin dose be reduced to 150mg every other day.
Aptivus/ritonavir may interact with calcium channel blockers,
medications used to treat heart disease. Studies of Aptivus/ritonavir
combined with calcium channel blockers have not yet been conducted.
Healthcare providers should be cautious when prescribing Aptivus/ritonavir
with either Cardizem (diltiazem), Plendil/Lexxel (felodipine),
Cardene (nicardipine), Sular (nisoldipine), or Calan/Verelan (verapamil).
Aptivus/ritonavir should not be combined with Vascor (bepridil).
Aptivus/ritonavir may also effect the blood levels of Coumadin (warfarin),
and anti-coagulating drug used to treat people at risk of blood
clots. Providers should frequently check blood levels of Coumadin,
known as the international normalization ratio (INR).
Aptivus/ritonavir may alter the blood levels of drugs used to treat
diabetes, including: Amaryl (glimepiride), Glucotrol (glipizide),
Micronase (glyburide), Actos (pioglitazone), Prandin (repaglinide)
and Tol-Tab (tolbutamide). The effect on blood levels of these drugs
varies. People should monitor their blood sugar carefully.
Aptivus/ritonavir can interact with drugs used to treat depression.
Aptivus/ritonavir may increase blood levels of Norpramin
(desipramine). The dose of Norpramin may need to be decreased.
Similarly, Aptivus/ritonavir can increase blood levels of Desyrel (trazadone),
making Desyrel side effects more likely. Prozac (fluoxetine), Paxil
(paroxetine) and Zoloft (sertraline) blood levels may also be
increased by Aptivus/ritonavir, though no changes in dosing are
recommended.
Antabuse (disulfiram) is a medication taken by people with an
alcohol-dependency problem. This medication can make people very
sick if they consume even small amounts of alcohol. Because Aptivus/ritonavir
contains small amounts of alcohol, it should not be combined with
Antabuse.
Flagyl (metronidazole) is used to treat some types of parasitic
infections. People should not drink alcohol—or take medications that
contain alcohol (such as Aptivus/ritonavir)—while taking this drug.
The combination of alcohol and Flagyl can cause someone to become
very ill. In turn, HIV-positive people taking Aptivus/ritonavir
should not take Flagyl.
Cholesterol-lowering drugs, also known as "statins," can interact
with Aptivus/ritonavir. There are two statins that should not be
used with Aptivus/ritonavir: Zocor (simvastatin) and Mevacor
(lovastatin). Levels of these two drugs can become significantly
increased in the bloodstream if they are combined with Aptivus/ritonavir,
which increases the risk of side effects. The two statins that are
believed to be the safest in combination with Aptivus/ritonavir are
Pravachol (pravastatin) and Lescol (fluvastatin). It is also
possible to take Aptivus/ritonavir with Lipitor (atorvastatin) or
Crestor (rosuvastatin) although Aptivus/ritonavir can increase the
levels of these drugs in the bloodstream. If Lipitor or Crestor is
prescribed, it's best to begin treatment with the lowest possible
dose of the drug and then increase the dose if necessary.
Aptivus/ritonavir may have an unpredictable effect on the blood
levels of drugs used to suppress the immune system, including
Sandimmune (cyclosporine), Rapamune (sirolimus, rapamycin) and
Prograf (tacrolimus). It is recommended that blood levels of the
immune suppressants be checked regularly.
Aptivus/ritonavir can significantly increase blood levels of the
inhaled steroid, Flonase (fluticasone), used to treat allergies.
This may increase the risk of side effects from Flonase, including
Cushing's syndrome. Combining these drugs is not recommended unless
the possible benefits from Flonase outweigh the risks. Prezista can
increase blood levels of an asthma medication called Serevent (salmeterol),
a drug that is used to open the air passages in the lungs during an
asthma attack. This can result in heart rhythm problems. Use of the
two drugs together is not recommended.
Aptivus/Norvir may interact with calcium channel blockers,
medications used to treat heart disease. Studies of Aptivus/Norvir
combined with calcium channel blockers have not yet been conducted.
Healthcare providers should be cautious when prescribing Aptivus/Norvir
with either Cardizem (diltiazem), Plendil/Lexxel (felodipine),
Cardene (nicardipine), Sular (nisoldipine), or Calan/Verelan (verapamil).
Tracleer (bosenstan) is another type of drug used to treat pulmonary
arterial hypertension, called an endothelin receptor antagonist.
Kaletra can increase Tracleer blood levels, so the dose of Tracleer
should be reduced.
Aptivus/ritonavir may decrease blood levels of the stomach-acid
reducer Prilosec (omeprazole). The dose of Prilosec may need to be
increased.
People taking anti-seizure medication may need to use caution when
combining these medications with Aptivus/ritonavir. Tegretol
(carbamazepine), Luminal (phenobarbital) and Dilantin (phenytoin)
can all decrease blood levels of Aptivus, making the Aptivus less
effective. Aptivus/ritonavir may decrease blood levels of Depakote (valproic
acid), making the Depakote less effective.
Prezista can increase blood levels of cochicine, which is used to
treat gout. Lower doses of colchicine are recommended, and the two
drugs should not be used together in people with liver or kidney
impairment.
Demerol (meperidine) is a powerful analgesic (painkiller). Aptivus/ritonavir
can decrease meperidine, but can increase the amount of
normeperidine (an active byproduct of Demerol), in the bloodstream.
In turn, Demerol should be used cautiously if it must be combined
with Aptivus/ritonavir.
Another painkiller, methadone, commonly used to treat drug heroin
addiction, can interact with Aptivus/ritonavir. Methadone levels in
the bloodstream can decrease when combined with Aptivus/ritonavir.
Because of this, it might be necessary to increase the dose of
methadone.
Aptivus/ritonavir may increase or decrease blood levels of the drugs
Suboxone (buprenorphine) and Narcan (naloxone), which are commonly
used to treat opioid addiction or overdose. These drugs may also
reduce blood levels of Aptivus. No dosing changes are yet
recommended.
Aptivus/ritonavir decreases the amount of oral contraceptives (taken
by women to help avoid pregnancy) in the bloodstream. This means
that there may be a higher risk of becoming pregnant if Aptivus/ritonavir
and oral contraceptives are taken at the same time. To reduce the
risk of pregnancy, barrier protection (e.g., condoms) should be
used.
Children (or adults) using the liquid version of Aptivus should not
take vitamin E supplements in excess of the amount found in a single
multivitamin. This is because liquid Aptivus already contains
vitamin E.
Viagra (sildenafil), Levitra (vardenafil) and Cialis (tadalafil)
levels in the bloodstream may increase when combined with Aptivus/ritonavir.
In turn, it is best to use a lower dose of these drugs in order to
reduce the risk of side effects.
Side
Effects
The most common short-term
side effects noticed in clinical trials involving HIV-positive
people taking Aptivus/ritonavir were: nausea, vomiting, diarrhea,
stomach pain, tiredness, and headache.
Aptivus/ritonavir may increase the risk of intracranial hemorrhage (ICH)—bleeding
in the brain due to ruptured blood vessels in the head—that can lead
to stroke or death. Aptivus/ritonavir should be used with caution in
patients who may have other risk factors for excessive bleeding from
trauma, surgery or other medical conditions, or who are receiving
medications known to increase the risk of bleeding (e.g.,
anticoagulants or antiplatelets used to prevent or treat heart
attacks).
Aptivus/ritonavir has been associated with reports of hepatitis and
significant liver damage (hepatic decompensation), including some
fatal cases. Extra caution is recommended for HIV-positive patients
with chronic hepatitis B or hepatitis C, who are at the highest risk
of liver-related side effects. Aptivus/ritonavir is not recommended
for people with moderate to severe liver impairment (Child-Pugh
Class B or C).
All HIV-positive people receiving Aptivus/ritonavir should be
carefully monitored. Liver function tests should be performed prior
to starting treatment with Aptivus/ritonavir and rechecked
frequently throughout the duration of treatment. HIV-positive people
who develop symptoms of liver problems, such as fatigue, loss of
appetite, yellowing of the eyes or skin, or liver tenderness, should
consult their healthcare providers to discuss stopping Aptivus/ritonavir
treatment. HIV-positive people with moderate to severe liver
problems should not take Aptivus/ritonavir.
Aptivus, a sulfa-containing drug, should be used with caution in
patients with a known sulfa allergy. Mild to moderate rashes and
increased sensitivity to the sun (photosensitivity) have been
reported in HIV-positive people taking Aptivus/ritonavir. In
clinical trials, rash was seen in 10 percent of females and in 8
percent of males receiving Aptivus/ritonavir. Additionally, in one
drug interaction trial involving HIV-study female study volunteers
who were administered a single dose of an oral contraceptive (ethinyl
estradiol) followed by Aptivus/ritonavir, 33% developed a rash. Rash
accompanied by joint pain or stiffness, throat tightness, or itching
has been reported in both men and women receiving Aptivus/ritonavir.
Women taking Aptivus/ritonavir with medications that contain
estrogen have an increased risk of developing a rash.
Some people may have large increases in their lipid levels
(triglycerides and cholesterol). The long-term chance of getting
complications such as heart attacks or stroke due to increases in
blood lipids caused by protease inhibitors is not known at this
time. Click here for our lesson called "Risks To Your Heart
(Hyperlipidemia)".
Diabetes and high blood sugar may occur in people who take Aptivus/ritonavir
or other protease inhibitors.
HIV drug regimens containing protease inhibitors, including Aptivus/ritonavir,
can cause abnormal body-shape changes (lipodystrophy; including
increased fat around the abdomen, breasts, and back of the neck, as
well as decreased fat in the face, arms, and legs).
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