STARTING HIV MEDICINES FOR THE FIRST TIME

Editing this section begun on 1/5/14

This section deals with beginning the first HIV medicine regimen.  Starting a second medicine regimen or even a third or fourth regimen is different from starting the first regimen, so this subject is given its own section.

The drug companies put out colorful pictures of all the different medicines on one large page.  The pictures are eye-catching and give one the impression that there are lots of medicines to choose from.  This is not true, because some of the medicines pictured are not used very often, if at all, and some are not even considered good choices.  Always keep in mind that there are less choices than you might think and you should be sure to take the medicines correctly so as not to develop resistance to any of the medicines.  Having to change HIV medicines because they no longer work for you is never a good thing.  

Another thing to remember is that your first regimen probably has the fewest pills you will ever take for your HIV.  Each time you have to change medicine because you have become resistant to your medicines, you will most likely need more pills; also, instead of once-a-day, you may need to take medicines twice a day.  So again, take care of this first HIV medicine regimen so that you will get many years of use out of it. Hopefully, it will be the only regimen you will ever need.  

In the olden days of HIV--the 1980’s and the early 1990’s, nearly everyone who had HIV eventually died of AIDS.  There were several HIV drugs, (like AZT--also called zidovudine or retrovir) but the drugs were used one at a time.  Using the drugs one at a time was not powerful enough to hold down the virus, so eventually, the person became resistant to the one drug and eventually died of AIDS.  It wasn’t until 1996 that this deadly trend turned around and doctors began giving patients with HIV three powerful drugs at a time, which kept the virus from multiplying and destroying the immune system.  After 1996, people with AIDS began to survive and today, 18 years after the first HIV 3-drug regimens, or “cocktails”, there are lots more choices to choose from: new two-drug combinations (one pill with 2 drugs) and pills containing 3 and even 4 drugs.  Someday, perhaps, there will be a cure, or there will be one pill a day for everyone with HIV.  Might I go so far as to wish for 1 pill once a week?  Hmmmm. 

HIV infection is managed today just like diseases such as diabetes and high blood pressure.  Once you begin the pills, you will usually stay on them for life.  Your lifespan on HIV medicines should be close to the lifespan you would have without the disease, provided you pay close attention to your general health and to the measurements of the virus in your body.  

The general rule for the HIV medicine is as follows: You want at least 3 active medicines working in your body all the time.  Not one, not two, but at least 3, all the time.  

Making the Perfect Choice for You. 

You and your provider should work together to figure out which first regimen is perfect for you. Some patients come in to the clinic knowing exactly what they want. Usually, they will come in asking for something their friend is taking, or the “one pill a day” option.  Choosing a particular cocktail just because your friend took the medicines or because it’s just one pill a day does not mean that this will be the right medicine for you.   Factors like these will affect your first medicine regimen:

• What is your work and sleep schedule?  Do you work at night and sleep during the day?  Avoid efavirenz (Sustiva), or Atripla, which contains efavirenz.
• Do you have mental health issues like depression, bipolar, and schizophrenia? You may want to consider avoiding efavirenz (Sustiva), or Atripla, which contains efavirenz.
• Do you have stomach issues, like frequent heartburn, a history of ulcers, or a stomach that gets upset very easily?  Avoid atazanavir (Reyataz).
• Have you had a heart attack or angina (heart-related chest pain), or do you have a good chance of having a heart attack in the near future?  In other words, do you smoke, have high blood pressure, have diabetes, or high cholesterol? If so, these put you at high risk for heart disease in the near future.  You may want to avoid abacavir  (Ziagen), and Epzicom, which contains the drug abacavir. Keep in mind that this fact is actually controversial and debated by many HIV/AIDS physicians and researchers.
• Do you have liver problems like Hepatitis B or Hepatitis C or cirrhosis? You will need to take certain drugs, like tenofovir (Viread) and lamivudine (Epivir) or emtricitabine (Emtriva) if you have hepatitis B.
• Do you have kidney problems? Have you had a tendency to get kidney stones?  Do you use cocaine, which causes kidney problems?  Diabetes and high blood pressure also cause kidney problems.  HIV itself can also cause kidney problems.  Your health care provider may want you to avoid indinavir, (Crixivan) and tenofovir (Viread), and Truvada, which contains tenofovir.
• Are you pregnant or is there a chance that you could become pregnant?  To health care providers, this is any woman before the age of around 50 who has not had her fallopian tubes tied (a tubal ligation) or a hysterectomy.  Avoid efavirenz, or Sustiva, and Atripla, which contains efavirenz.  If you are pregnant, you should start HIV medicines during the pregnancy to maintain your health and prevent you from giving your unborn baby HIV. 
• Have you just been diagnosed with one of these three infections: 1) tuberculosis (TB)? 2) mycobacterium avium complex (MAC)? 3) cryptococcosis?  If so, your health care provider may have you wait several weeks after beginning treatment for these infections before you start HIV medicines.   Tuberculosis medicines may also affect your drug choices.
•   What drugs are you taking now?  There may be a potential for some drugs not to get along with each other.  
• Do you have any drug resistance?  Remember the chapter about genotypes?  If not, re-read this section.  
• Are you ready to commit to a long-term medicine relationship?
• Do you have a reliable place to live and reliable transportation to the clinic at least once a month?
• Do you have a way to pay for your medicine and will that plan be for the long haul--in other words, for years?  This will be insurance, paying out of your own pocket (rare, as HIV medicines are quite expensive), or state government funding.  
• What is your CD4 count and viral load?  If your CD4 count is less than 350, or you have symptoms of HIV, like thrush, you should start medicines.  There are also other conditions in which you should start medicines before your CD4 drops below 350.  The CD4 count of 350 may not hold much longer as the time for starting HIV drugs; experts are thinking of changing this number to 500.  The International AIDS Society--USA recommends starting medicine before your CD4 decreases to 350.  
• How likely are you, given your lifestyle, to skip doses of your HIV medicines? Or take them late (or at different times ) every day?  Certain HIV drug regimens are “unforgiving” of missed doses, while other regimens are considered “forgiving.”  The unforgiving medicines cause fast resistance if you skip doses, while the forgiving medicines are less likely to lead to fast resistance.
• It’s easier to get resistance to efavirenz compared to the protease inhibitors.  That’s because it takes just one mutation (change) in the virus before the drug no longer works.  This is a big deal!  If you are the least bit careless about taking your HIV medicines, you will quickly become resistant to this drug and you will have to give up this medicine and, most likely, choose another class of drug.  Also, resistance to efavirenz will give you resistance to other drugs in the class (except for the newer drug, etravirine).
• Efavirenz can, in rare cases, cause problems with your liver.  You will have your labs drawn about 4 weeks after starting the medicine, to check for this problem. 
• Efavirenz can cause a rash.  Sometimes, however, the rash will go away on it’s own and you will be able to stay on the drug.  Be sure to report the rash to your health care provider, who will want you to come in to the clinic to see you and may treat your rash symptoms if there are no other problems other than the rash.  
• Efavirenz can cause what I call the 3 DRs--DRunk, DRowsy, and DReams.  By drunk, I mean that you may feel like you have a mild hangover the next morning after the evening you take your dose.  Some people describe the feeling as dizziness, or that their head feels big.  The drug makes you drowsy, but that’s a good thing if you take it before bed.  Efavirenz can also cause you to have bad dreams.  By this, I mean very vivid and scary dreams.  One person on this drug would wake up and begin to hit his partner because he believed his partner was hitting him.  Other people report dreams about murder and body mutilation. These dreams can be quite disturbing.  In rare cases, the drug can cause disturbing thoughts while you are awake--this is called psychosis.  When you have psychosis, you see, feel, smell or hear things that are not really there.  The good thing is, these side effects usually take anywhere from 1 to 30 days to go away.  It is seldom that the side effects of this drug are enough to stop it for good.  
• Efavirenz also has some drugs that it does not get along with--your pharmacist and health care provider will watch for any type of drug interactions.  
• Efavirenz can cause birth defects in an unborn child.  This drug must not be given to any woman who is capable of bearing a child.  That means any woman before the age of menopause, unless she has had a hysterectomy (her uterus, or womb, removed).  In our clinic, we will prescribe efavirenz for those women who have had a tubal ligation.  That’s the only exception.  It can still be used in young women taking other types of birth control, like the pill and the depo-provera shot; however, we go to great lengths to tell her that if she becomes pregnant on this medicine, the baby will have a high chance of a birth defect. 
• You must take the medicine on an empty stomach, or with a low-fat meal.  High fat meals may cause you to experience worse side effects.  
• Most people must go to sleep after they take efavirenz, because it causes drowsiness.  This will cause a problem for people who work the night shift.  You might not see a problem; after all, you just take the medicine before you go to bed.  What usually happens, however, is that the night-shift worker has business to conduct during the daylight hours and will conduct that business in the morning hours, delaying going to bed.  Several hours may go by while he/she runs errands and by the time the person goes to bed, the drug is 4 hours late.  HIV drugs must be taken on time, within 1-2 hours of when the drugs were taken the day before.  If you go to bed at 8 a.m. and the next day, don’t go to bed until 11 a.m., the drug is late and the level of the drugs in the body is low.  When the drug levels are low, the virus learns how to get around the medicine--that’s called resistance.  
• Some people take efavirenz in the morning.  They say it does not make them sleepy and they are able to function normally.  

It is not true that it is worse to miss a dose of a once-a-day regimen than to miss a dose of a twice-a-day regimen. It just depends on how long the medicine remains in the body.   Experts and patients do agree, however, that taking HIV medicine once-a-day is better than twice-a-day. Patients who are on once-a-day regimens are more satisfied and are more likely to stick to their medicine regimens, thereby leading to a good CD4 count and undetectable virus.  The same is true for the number of pills--the less pills, the better.  Patients feel better if they have to take 4 pills a day rather than 8 pills a day.  This, in turn, leads to sticking to the medicine regimen and good results.  

The best regimen is simple (the least amount of pills and once a day), safe (the drug will cause no major disruptions in body function), tolerable (no or very few side effects), and effective (it works!). 

National Guidelines

Two organizations give your health care provider guidance in choosing the first regimen: The US Department of Health and Human Services--DHHS (nickname “dishes”) and the International AIDS Society (IAS) USA Panel (I guess we need a nickname for this one). Both organizations’ guidelines are pretty much the same, except for some small differences.   

Where do these HIV treatment guidelines come from?  The guidelines are based on expert medical and scientific opinions, research studies using the drug(s) in small groups of people with HIV, and from experience using the HIV drug(s) in the entire population.  In order for a drug or drug combination to make it into the guidelines, it must be shown to be effective, safe, and have few drawbacks.  The guidelines have changed over the years, as we get newer drugs and the drugs are constantly being used.  

Using the guidelines, you and your provider will be able to find a medicine regimen that is simple, safe, tolerable, and effective for you.  In other words, perfect.  It’s just like picking a lifetime partner.   Pick a good partner for you and you will have a happy partnership.   Pick a bad partner, and you will have difficulties and problems, and may even want a divorce from your partner (medicines).  

Before looking at the guidelines, it is necessary to know a little bit about the six different classes of HIV medicine and how the different classes of drugs work.  I have color coded the different classes--pink for the NRTIs, blue for the PIs, purple for the NNRTIs, green for the Integrase Inhibitors, aqua for the Fusion Inhibitors, and red for the Entry Inhibitors. 

Classes of HIV Medicines  

1) NRTIs  Nucleoside and Nucleotide Reverse Transcriptor Inhibitors

Abacavir (Ziagen, ABC)

Didanosine (Videx, ddI)

Emtricitabine (Emtriva, FTC)

Lamivudine (Epivir, 3TC)

Stavudine (Zerit, d4T)

Tenofovir (Viread, TDF)

Zalcitabine (Hivid, ddC)

Zidovudine (Retrovir, AZT/ZDV)

NRTI Drug combinations available:

zidovudine + lamivudine = Combivir

abacavir + lamivudine + zidovudine = Trizivir

abacavir and lamivudine = Epzicom

tenofovir + emtricitabine = Truvada

2) NNRTIs  Non-Nucleoside Reverse Transcriptase Inhibitors

Delavirdine (Rescriptor, DLV)

Efavirenz (EFV, Sustiva)

Etravirine (Intelence, ETV, TMC-125)

Nevirapine (Viramune, NVP)
Rilpivirine (Edurant)

Combinations using this class of drugs:
emtricitabine + tenofovir + efavirenz = Atripla
emtricitabine + tenofovir + rilpivirine = Complera

3) PIs  Protease Inhibitors

Atazanavir (Reyataz, ATV)

Darunavir (Prezista, DRV, TMC-114)

Fosamprenavir (Lexiva, FPV--called Telzir in Canada)

Indinavir (Crixivan, IDV)

Lopinavir/Ritonavir (Kaletra, LPV/RTV)

Nelfinavir (Viracept, NFV)

Ritonavir (Norvir, RTV)

Saquinavir (Invirase, Fortovase, SQV)

Tipranavir (Aptivus, TPV)

4) Entry Inhibitors also called CCR5 co-receptor Antagonists

Maraviroc (Selzentry)                                                              

5) Integrase Inhibitors

Raltegravir (Isentress, RAL)
Dolutegravir (Tivicay)
Elvitegravir (Pending FDA approval)

Combinations using this drug class:
emtricitabine + tenofovir + cobicistat + elvitegravir = Stribild

6) Fusion Inhibitor

Enfurvitide (T20, Fuzeon)

The guidelines recommend two medicines from one class of medicines--nucleoside reverse transcriptase inhibitors,or NRTIs.  These two medicines are put together with either a “boosted” protease inhibitor (PI) or a non-nucleoside reverse transcriptase inhibitor (NNRTI).  Wow.  It sounds complicated, but after a while, you’ll be talking about NRTIs and NNRTIs and PI’s like they were old friends. 

2 NRTIs plus either a NNRTI or a PI

Let’s take this in steps: Step 1--choose from the list of nucleoside reverse transcriptase inhibitors (NRTIs).  The 2 NRTIs are already combined and chosen for you--Choose one combination medicine from the list below:

Step One--Choose # 1 or #2 

1) tenofovir/emtricitabine (Viread and Emtriva available in one tablet as Truvada)

 or 

2) abacavir/lamivudine (Ziagen and Epivir available in one tablet as Epzicom)

Now, in step 2, choose either number (1) efavirenz, or (2) one from the list of protease inhibitors as shown in the following list or (3).

Step 2: Choose from number 1 or number 2 or number 3:

1) Efavirenz (Sustiva) once a day

or 

2) a boosted PI, like these:

atazanavir (Reyataz) with the booster drug ritonavir (Norvir) once a day

darunavir (Prezista) with the booster drug ritonavir (Norvir) once a day

fosamprenavir (Lexiva) with the booster drug ritonavir (Norvir) twice a day

lopinavir with the booster drug ritonavir inside the pill--Kaletra once or twice a day

saquinavir with the booster drug ritonavir (Norvir) twice a day--IAS guidelines only)

or

3) the integrase inhibitor:

Isentress (Raltegravir) twice a day

So, you see, the choices are already set down--you just need to make some choices from the above choices.  

Most likely, the first thing your provider will suggest is the drug combination (2 pills in one) tenofovir/emtricitabine, which is the generic name for the drugs Viread and Emtriva which is available as the blue tablet Truvada.  Everyone likes this medicine.  It’s once a day, and I rarely hear any complaints about side effects.  The big advantage of this drug is that it is combined with the drug efavirenz (Sustiva) in the 3-drug combination pill called Atripla.  

The disadvantage to tenofovir/emtricibine (Viread + Emtriva) is that it should be avoided if you have kidney problems or a chance of developing kidney problems.   On the other hand, if you have hepatitis B, you will want to take Truvada.  

In step one, if you avoid choice number one, tenovovir/emtricitabine, you must pick what is behind door number 2--abacavir/lamivudine, which is Ziagen and Epivir given together in one orange pill called Epzicom.  The only reason this is the second choice is because the abacavir (Ziagen) part of the pill can cause a rare but serious type of allergic reaction.  There is a blood test called HLA-B*5701 to check for the tendency to develop this allergic reaction.  Your health care provider will order this test and if you are HLA-B*5701 positive, you must not take abacavir (Ziagen).  If the test is negative, you can rest easily that you probably won’t have a reaction to this drug.  However, even if you are HLA-B*5701 negative, you will still need to watch for the allergic reaction and report any side effects at once.  Some health care providers may avoid abacavir (Ziagen) if the viral load is more than 100,000 or the person has heart disease (or a high chance of getting heart disease).  Once one gets past these difficulties, the drug is easy to take--it is combined with lamivudine (Epivir), and it’s rare to hear about side effects.  

So that’s it.  That takes care of the first two drugs for your regimen. Wait a minute, you say.  What about other drugs like AZT (zidovudine or retrovir), DDI (Videx or didanosine), and D4T (Zerit or stavudine)?  Those drugs are not on the list, so we don’t even consider them unless we have to. 

AZT (Zidovudine or Retrovir)

The old standby, AZT (zidovudine or Retrovir), might be considered if you are unable to take the drugs on the recommended list.  AZT is a great drug but has fallen out of favor due to these factors: 1) it must be given twice a day; 2) it has a tendency to cause headaches, nausea, and vomiting; 3) it may cause problems with your blood.  The blood problems are: a) anemia, which is a lack of red blood cells that carry oxygen and b) a low white blood cell count, which affects your immune system. 

In my experience, most people get used to zidovudine (AZT) after staying on it for a week or more.  There are drugs to treat the anemia and the low white count, if you need them.  You can take the zidovudine (AZT) with food to help with any nausea.  

There are still some people around who look at you in horror when you mention AZT.  They say to you, “My friend took that drug and he died.”  That may be true, but the friend didn’t die because he took AZT.  He died because he took AZT alone, before medical experts knew you had to take at least 3 drugs to hold down the virus.  

Zerit (also called D4T or stavudine)

Zerit is another drug that has fallen out of favor recently, like it’s friend AZT.  The reasons for this dislike of this drug are listed here:  1) the drug must be given twice a day; 2) the drug has a tendency to cause numbness, tingling, and pain in the feet (sometimes the hands, too); 3) this drug may be more likely than other HIV drugs to cause a shifting of body fat from one place to another.  In some, this may mean loss of fat from the cheeks. In others, fat may shift away from the legs, buttocks, or breasts, and deposit itself in another area, like the upper back and neck; 4) Zerit may cause problems with your lipids--fatty substances in your blood like cholesterol and triglycerides.  Lately, Zerit is used in a lower dose and the tendency to cause these problems is much less.   If you are put on this medicine, watch for the above problems and report them.  However, you can rest easy that you are on a good drug that will do what it’s supposed to do--increase your CD4 count and keep your virus at undetectable levels.  One more thing to remember: Never take Zerit with AZT.  The two drugs are so alike that this will cause problems.  

The Third Choice 

Now, lets look at the next choices on the list.  You have your first two drugs and now you and your health care provider have to choose your third drug. That third drug will be efavirenz (Sustiva) or a “boosted” protease inhibitor.  By boosted, I mean that the drug ritonavir (Norvir) is given to boost the level of the protease inhibitor.  Ritonavir (Norvir) is given with atazanavir (Reyataz), darunavir (Prezista), fosamprenavir (Lexiva), or saquinavir (Invirase).  The ritonavir makes the level of these drugs go up.  That’s a good thing so you will need less pills.  The drug lopinavir/ritonavir (Kaletra) already has the ritonavir inside the pill so you don’t need to take it separately.  

A word about ritonavir (Norvir)

Never take ritonavir (Norvir) alone--it must be taken with another protease inhibitor and you must take them both with food. Ritonavir boosts the level of the other protease inhibitor.   I always tell the patients to take all their HIV medicines at the same time.

Which choice is best for the third drug?

Your health care provider will help you make this choice, and it is a bit more complicated.  Remember the list of questions I asked you at the beginning of this chapter?  Many of those factors must be taken into consideration for the third drug. 

Choosing atazanavir (Reyataz) plus booster drug ritonavir (Norvir)

Atazanavir (Reyataz) is a great drug choice.  It is one capsule given once a day with your breakfast, or another meal of your choosing, as long as it’s at the same time each day.  You must take the atazanavir with ritonavir.  The advantages of this drug are: 1) it does not seem to elevate cholesterol or triglyceride levels; 2) this boosted protease inhibitor has the lowest amount of pills (pill burden) compared to all the other boosted protease inhibitors--all the other protease inhibitors require at least 2 pills a day--not one; 3) it’s given once a day; 4) it requires only one ritonavir capsule to boost it; 5) it works!  

There are two disadvantages to atazanavir with ritonavir:  1) You should avoid this drug if you have a tendency to have acid reflux, or heartburn.  Any drug which you take to reduce stomach acid, like over-the-counter Prilosec, Pepcid, Zantac, and Tagamet, etc., will interfere with the medicine and keep it from working. 2) In some patients, the drug may cause a yellow discoloration to the skin or eyes (jaundice).  It’s nothing to be alarmed about but you must tell your health care provider immediately. Fortunately, this does not happen often, but it’s worth watching for. In most patients, the yellow discoloration will go away. In rare cases, you must stop the drug.   All things considered, let’s give two thumbs up for this choice. 

Choosing darunavir (Prezista) plus booster drug ritonavir (Norvir)

Darunavir (Prezista) with ritonavir.  Darunavir is the newest kid on the block and  this drug is another great choice.  The advantages are: 1) it may be taken just once a day with a meal--it doesn’t matter which meal as long as you take it at the same time every day.  2) you need to take just two tablets darunavir tablets a day combined with just one ritonavir (Norvir), so it has a “low pill burden”--this is one more pill than the atazanavir capsule mentioned in the above paragraph; 3) it does not tend to increase your cholesterol or triglyceride levels. 4) It works great in just about everyone who takes it.  (Even patients who are resistant to other protease inhibitors have success with this drug.)  Disadvantages include: 1) Patients with a sulfa allergy may be allergic to this drug.  Reactions are rare, but watch for a rash.  2) All protease inhibitors have a tendency to cause nausea and diarrhea; however, this drug seems to agree with most people’s stomachs.  Two thumbs up for this drug.   

Choosing fosamprenavir (Lexiva) plus booster drug ritonavir (Norvir)

The drug fosamprenavir, also called Lexiva, is another good choice.  I have an elderly lady in her 70’s who was not able to take any other protease inhibitor and she loves this drug.  Fosamprenavir can be given as two tablets once a day with one ritonavir (Norvir) capsule, or one tablet twice a day with one ritonavir capsule.  Of course, most people prefer once a day; however, the guidelines say that taking it twice a day is better, based on what they know now.  The drug can be taken with or without food but most people take it with their morning meal. 

Advantages to the fosamprenavir (Lexiva) plus ritonavir (Norvir) choice are: 1) A low amount of pills (low pill burden); 2) It is effective.  Disadvantages are: 1) it may worsen cholesterol and triglyceride problems, and  2) The drug may cause a rash. (Again, watch for a rash if you have an allergy to Bactrim, or sulfa drugs.)  This rash is rare, occurring in just about 3 out of every 100 who take this drug;  3) Gastrointestinal side effects like nausea, cramping, and diarrhea. 

Choosing lopinavir/ritonavir (Kaletra)

Notice that I did not say lopinavir plus the booster drug ritonavir.  That’s because the makers of lopinavir and ritonavir happen to be the same drug company and they put the two drugs together combined into one pill.  Lopinavir/ritonavir (Kaletra) is another great drug; as a matter of fact, lopinavir/ritonavir was and is so effective that it is the drug that all the other protease inhibitors are compared with in order to see how they stack up.  In other words, Kaletra is the “gold standard” of the protease inhibitors.  If you think of it like a speed skating race, the skater in the Kaletra suit always comes across the finish line, and all the other skaters (drugs) have to either come across the finish line at the same time, or do better.  If not, the skater (drug) is not good enough to go on the list of winners--or in this case, the HIV drug guidelines.  

Lopinavir/ritonavir (Kaletra) may be taken as four tablets once a day or as two tablets twice a day.

Advantages to lopinavir/ritonavir (Kaletra) are: 1) lopinavir and ritonavir are mixed together into one tablet, so there’s no need to worry about two separate pills--no separate co-pays either;  2) Kaletra has proven effectiveness, and has been, for years, the one to beat.  Most pregnant women are given this drug to protect their unborn baby from getting HIV, so you know it’s safe and effective.  

Disadvantages to lopinavir/ritonavir (Kaletra) are: it may cause cholesterol or triglyceride problems, which is quite common.  These problems can be treated, but it may mean taking extra pills for cholesterol or triglycerides. 2) the drug may cause more stomach and intestinal issues than the other protease inhibitors.  These include nausea, cramping, and diarrhea.  3) There is a higher number of pills one must take--4, more than all the other protease inhibitors I’ve talked about so far--even counting the “booster” drug ritonavir (Norvir) that must be given with the other protease inhibitors.  

Given all the above information, Kaletra gets two thumbs up.  

Choosing saquinavir (Invirase) plus the booster drug ritonavir (Norvir)

Saquinavir (Invirase) plus the booster drug ritonavir is the last protease inhibitor on the guidelines list of protease inhibitors for the first HIV drug regimen.  Saquinavir has been around since 1996 and was used quite a bit in those first years of the HIV cocktail.  

Saquinavir is a perfectly acceptable drug choice and has two advantages: 1) There is no effect on cholesterol or triglyceride levels.  2) As I said above, the drug has been around for a long time, so there are no surprises about the long-term effects.  The disadvantages are: it must be given as two tablets twice daily with the booster drug ritonavir for a total of 3 pills twice a day or 6 pills a day--in other words, there is a high pill burden.  In comparison to all the other choices for the first HIV regimen, this one requires the most pills.  Given that the only disadvantage is the high pill burden, this is a perfectly good choice for a first regimen.  Two thumbs up.

Choosing a non-nucleoside reverse transcriptase inhibitor instead of a protease inhibitor 

People who have never taken HIV medicines can avoid the protease inhibitors and go instead to the non-nucleoside reverse transcriptase inhibitors (the class can also be called NNRTIs or “non-nukes”).  The class is made up of 4 medications--nevirapine (Viramune), efavirenz (Sustiva), delavirdine (Rescriptor), and the new etravirine (Intelence).   The only drug in this class that you need to know about, for now, is efavirenz (Sustiva).  

Efavirenz (Sustiva) is a wonderful medicine and has proven itself to be quite effective.  You don’t need a booster drug with it and it’s just one pill, once a day at bedtime, or before you go to bed.  It has a long half-life and stays in the body a long time. It’s less likely than the protease inhibitors to cause any of your body fat to shift around.   Plus, taking this medicine can save the protease inhibitors for the future, if you should happen to have to change your medicines.  The biggest advantage this drug has is that it has been combined with two other HIV drugs called tenofovir and emtricitabine into one 3-drug pill called Atripla.  All three of your HIV pills are combined into one pill.    

Efavirenz (Sustiva) also has some disadvantages: