Antiretroviral Medication for HIV

If you are pregnant and have HIV, it is essential that you receive treatment with antiretroviral medication. There are two basic reasons for this treatment:

  • it helps prevent transmission of HIV infection to your baby; and
  • it improves the course of your disease.

Current treatment guidelines recommend administration of at least three antiretroviral drugs (see Table 1). If the mother merits treatment for HIV infection for her own disease (recommended at this point if the CD4 cell count is below 200 cells/mL), she should be placed on HIV therapy as soon as her pregnancy is confirmed-if she isn't on therapy already. If the mother doesn't need therapy for her own condition, she will need antiretroviral therapy starting from the second trimester to help prevent transmission of HIV to the baby. Once the baby is delivered, the antiretroviral therapy for the mother can be stopped and restarted whenever the woman needs it for her own HIV infection.

Table 1. Drugs Used for Treatment of HIV Infection*
AGENT USUAL ADULT DOSEREMARKS
Nucleoside Analogues (NRTIs)Abacavir (Ziagen, ABC)300mg BIDMost serious adverse effect is a hypersensitivity reaction (2-5% of patients).
 Didanosine (ddI, Videx)400mg QDMost serious adverse effects are pancreatitis and peripheral neuropathy. Of note, the combination of d4T and ddI is contraindicated during pregnancy because of the increased risk of lactic acidosis.
 Lamivudine (3TC, Epivir)300mg QDAdverse effects are very minimal and include nausea. Drug is eliminated by renal excretion.
 Stavudine (d4T, Zerit)40 mg BIDMain adverse effect is peripheral sensory neuropathy. Of note, the combination of d4T and ddI is contraindicated during pregnancy because of the increased risk of lactic acidosis.
 Zalcitabine (ddC, Hivid)0.75 mg Q8hMost serious adverse effect is peripheral neuropathy. Pancreatitis also can occur. Least potent of the nucleoside analogs and very rarely used in pregnant or non-pregnant patients.
 Zidovudine (AZT, Retrovir)300mg BIDMain adverse effect is marrow suppression, leading to anemia (low red blood cells) or leucopenia (low white blood cells). Can also rarely cause peripheral neuropathy.
 Emtricitabine (FTC, Emtriva)200mg QDVery similar to 3TC and adverse effects are minimal.
 Tenofovir (Viread)`300mg QDMost serious adverse events is renal failure or low phosphate in the bloodstream.
 Various combination of the above NRTIs are manufactured (where the drugs are co-formulated in one pill), including combivir (AZT + 3TC) taken as 1 pill BID, Epzicom (abacavir + 3TC) taken as 1 pill QD, Truvada (Tenofovir + FTC), taken as 1 pill QD, trizivir (AZT+ 3TC + abacavir), taken as 1 pill BID.
Non-Nucleoside Reverse Transcriptase InhibitorsDelavirdine (Rescriptor)400 mg TIDMost common side effect is rash; it usually is less severe than the one associated with nevirapine. Hepatitis also can occur. This medication is rarely used since it is required 3 times a day.
 Nevirapine (Viramune)200 mg BIDMost common adverse effect is rash. If the rash is extensive, the drug should be permanently discontinued. Rashes from nevirapine are more common in women. Liver inflammation with nevirapine is quite common in pregnancy and this drug is rarely used anymore in pregnant women. If this drug is used, liver tests should be carefully monitored.
 Efavirenz (Sustiva)600 mg QDThe drug is teratogenic and should absolutely not be used in pregnancy or in women planning pregnancy. Most common adverse effects for the non-pregnant patient are central nervous system changes and rash.
Protease InhibitorsAmprenavir (Agenerase)1,200 mg BIDMost common adverse effects are rash and gastrointestinal irritation. Since this drug requires the administration of 8 pills twice a day, it is rarely used anymore. Lexiva (see below) has replaced this formulation.
 Indinavir (Crixivan)800 mg Q8h without ritonavir, but most commonly given as 800 mg BID with ritonavir boostingMost serious adverse effect is nephrolithiasis (kidney stones). Most common side effect is gastrointestinal upset. Rarely used anymore in favor of newer protease inhibitors (Lopinavir/ritonavir, Atazanavir, Lexiva).
 Nelfinavir (Viracept)1,250 mg BIDMost common adverse effect is diarrhea. This drug is rarely used because it is not as potent as the newer protease inhibitors. In addition, the levels of nelfinavir are significantly decreased during pregnancy so that virologic failure with this medication can readily occur..
 Ritonavir (Norvir)600 mg Q12h

100 mg QD or 100 mg BID or 200 mg QD or 200 mg BID as booster doses
Ritonavir as a single agent is no longer used because of the frequency of adverse effects, which include gastrointestinal irritation, metallic taste in the mouth, numbness and tingling around the mouth, fatigue, and drug-drug interactions. However, ritonavir is often used to boost the levels of other protease inhibitors at a smaller dose (ranging from 100mg QD to up to 400mg over the day)
 Saquinavir (Invirase,)1,000 mg BID with 100 mg BID of ritonavirMain adverse effect is gastrointestinal irritation. Also not as commonly used as the newer protease inhibitors below.
 Lopinavir/ritonavir (Kaletra)400 mg BID of lopinavir with 100 mg BID of ritonavirMain adverse effect is gastrointestinal irritation, including nausea, vomiting, and diarrhea. Should be taken with a meal or a light snack.
 Atazanavir (Reyataz)Usually given as 300 mg QD with 100 mg QD of ritonavir. More rarely given alone at 400 mg QDMain adverse effect is a benign hyperbilirubinemia (high bilirubin levels), which can lead to jaundice (yellow skin) and scleral icterus (yellow eyes). Can also lead to a rash. Should be taken with a full meal. Cannot give atazanavir without ritonavir if tenofovir is in the regimen).
 Fosamprenavir (Lexiva)Usually given as 1,400 mg QD with 200 mg QD of ritonavir. Can also be given as 700 mg BID with 100 mg BID of ritonavir. More rarely given as 1,400 mg BID alone.Most common adverse effect is gastrointestinal irritation or a rash. Can be taken with or without food.
 Tipranavir (aptivus)500 mg BID along with ritonavir 200 mg BIDAssociated with many adverse effects due to the ritonavir component, including nausea, vomiting, diarrhea, liver damage, and rash. Should be reserved for patients who are resistant to other protease inhibitors and shouldn't be used in combination with other protease inhibitors.

*Highlighted medications are commonly used in pregnant women. Discuss with your doctor the best regimen for you.

Key:

QD = Once a day

BID = Twice a day

TID = Three times a day

Q8h = Every 8 hours

Q12h = Every 12 hours

Did You Know?

When combination therapy is effective (it significantly reduces the patient's viral load), the risk of transmission of HIV infection to the baby appears to be almost zero.

Many combinations of antiretroviral medications are used currently for the treatment of HIV infection and at least three drugs in combination are used. The most common combinations used in pregnancy are two nucleoside analogs (preferably not d4T or ddI and never the two in combination), along with a protease inhibitor, most commonly Kaletra or Atazanavir (with ritonavir). Zidovudine (AZT, Retrovir) should be administered intravenously during labor to the mother and then given orally to the baby for at least six weeks after delivery. Following delivery, the mother should resume her oral antiretroviral medications if she needs them for her current HIV infection or can discontinue them if they were only being administered during pregnancy for prevention of transmission to the fetus.

In addition to specific antiretroviral chemotherapy, patients also should receive preventive medication against the most common opportunistic infections if their CD4 counts are low and render them susceptible to such infections, such as Pneumocystis carinii pneumonia, herpes infections, candidiasis (yeast infection), toxoplasmosis, and tuberculosis. Table 2 lists the drugs used most commonly to protect against opportunistic infections in patients infected with HIV.

Table 2. Prophylactic Antibiotic Regimens for Common Opportunistic Infections
CONDITIONANTIBIOTIC
Candidiasis-oral and vaginal infectionFluconazole (Diflucan)
Cryptococcosis-meningitisFluconazole (Diflucan)
Herpes simplex-oral and genital infectionAcyclovir (Zovirax), valacyclovir (Valtrex), or famciclovir (Famvir)
Mycobacterium avium complex (MAC)-wide-spread, disseminated infectionAzithromycin (Zithromax)-1,200 mg weekly
Pneumocystis carinii pneumoniaTrimethoprim-sulfamethoxazole (Septra, Bactrim), dapsone, or atovaquone
Toxoplasmic encephalitisTrimethoprim-sulfamethoxazole (Septra, Bactrim)
Tuberculosis-pulmonary infectionIsoniazid (Nydrazid) plus pyridoxine (Vitamin B-6)