Six 200 mg capsules three times daily

Brand name: Fortovase

Common name: saquinavir soft-gel

Class: HIV protease inhibitor (PI)

Standard dose: Six 200 mg soft-gel capsules three times a day with food, or within two hours after a meal; or five 200 mg Fortovase with 100 mg Norvir, twice-a-day with food. Take missed dose as soon as possible, but do not double up on your next dose.

AWP: $257 / month

Manfacturer contact: Roche Pharmaceuticals, www.fortovase.com, 1 (800) 910–4687

AIDS Treatment Information Service: 1 (800) HIV–0440 (448–0440)

Potential side effects and toxicity: Most common include diarrhea, nausea, stomach pain, gas, indigestion, vomiting, headaches, insomnia, fatigue, body aches, anxiety, depression and taste alteration.

As seen with all other protease inhibitors are increased levels of cholesterol and triglycerides, except possibly unboosted Reyataz (atazanavir) and these increased levels may be associated with heart disease. Other possible side effects are lipodystrophy (body fat changes, including thinning of the face, arms and legs, with or without fat accumulation in the stomach, breasts and sometimes the upper back), onset of new cases or worsening of diabetes (see your doctor promptly) and increased bleeding in hemophiliacs.

Potential drug interactions: Do not take with Tambocor (flecainide), Rythmol (propafenone), Versed, Halcion, Hismanol, Seldane, rifampin, ergot derivatives (such as Cafergot, Wigraine and Methergine, D.H.E. 45, in any form—serious interactions seen with dilation during gynecological exams), garlic supplements, or the herb St. John’s wort. Do not use Zocor (simvastatin) or Mevacor (lovastatin); lipid-lowering alternatives are Lipitor (atorvastatin), Lescol, and Pravachol (pravastatin), but they should be used with caution due to potential for liver toxicity. Rifampin and Fortovase should not be used together.

Increased blood levels when taken with Crixivan, Norvir and Viracept. Blood levels are decreased significantly by Sustiva and Viramune, but can be taken together if Norvir is included. Other drugs that may also reduce Fortovase blood levels are Decadron and Tegretol, Dilantin, and phenobarbital. High incidence of liver problems, and severe ones, when taken with Rescriptor. The side effects of calcium channel blockers, clindamycin, dapsone and quinidine may be increased if taken with saquinavir.

Protease inhibitors increase blood levels of Viagra (sidenafil citrate), Cialis (tadalafil) and Levitra (vardenafil). Use with caution. Initially the Viagra dose should be 12.5 mg (1/2 of 25 mg tablet) and increased as needed and tolerated. It’s recommended that people on PIs do not exceed 25 mg of Viagra in a 48-hour period because of potential for serious reaction. Use Cialis at reduced doses of 10 mg every 72 hours and Levitra at reduced doses of no more than 2.5 mg every 72 hours, with increased monitoring for adverse events.

Tips: Must be taken with food or within two hours after a meal. Keep capsules at room temperature if they will be used up within three months. Zantac, Pepcid, Tagamet or antacids may be necessary to treat Fortovase heartburn (which is common). Refrigerated (36–46° F or 2–8° C) capsules remain stable until the expiration date printed on the manufacture bottle. Once brought to room temperature capsules should be used within 3 months. Avoid direct sunlight. Dosings of Fortovase boosted with Norvir—five 200 mg Fortovase with one 100 mg Norvir twice-a-day or eight 200 mg Fortovase with one 100 mg Norvir once-a-day or five 200 mg Fortovase with three 133 mg Kaletra (lopinavir/ritonavir) twice-a-day.

Doctor
Saquinavir, the first protease inhibitor approved by the FDA, comes in two versions: Invirase (soft-gel) and Fortovase (hard-gel). Fortovase has better bioavailability—that is, more of it is absorbed after ingestion. With better absorption, there are more side effects, mainly diarrhea. Recently, however, Invirase has made a comeback because it has fewer side effects, even when combined with Norvir, which significantly boosts blood levels. When taken alone, Fortovase must be given in whopping doses, six pills three times daily! If boosted with Norvir it can be taken in smaller quantities; but diarrhea remains a problem for some people.
Activist
More than once, I’ve watched the eyes of people making their first treatment decision fill with terror when they look at the HIV drug chart for the first time. Usually, their gaze has fallen on Fortovase and its ant parade of 18 big, shiny capsules (the daily dose!). To add to its charms, it lacks potency on its own, has a reputation for gut disturbance, is dosed every eight hours—shall I go on? Last year it was approved for twice daily dosing at 1,000 mg, with 100 mg of ritonavir. Whew. This reduces pill count, of course, but makes GI matters worse. If you use this drug do an inventory of the other medications you take—the list of possible drug interactions covers a lot of ground. One place Fortovase actually comes recommended is in pregnancy—it’s one of two PIs listed in the U.S. treatment guidelines as recommended agents.

Nukes | Retrovir / AZT / zidovudine | Videx, Videx EC / ddI / didanosine |
| Hivid / ddC / zalcitabine | Zerit / d4T / stavudine | Epivir / 3TC / lamivudine |
| Ziagen / abacavir sulfate | Combivir (Retrovir, Epivir) |
| Trizivir (Retrovir, Epivir, Ziagen) | Emtriva / emtricitabine / FTC |
| Viread / tenofovir disoproxil fumarate | Epzicom (Epivir, Ziagen) |
| Truvada (Viread, Emtriva) |

Non-Nukes | Rescriptor / delavirdine | Viramune / nevirapine |
| Sustiva / efavirenz |

HIV Protease Inhibitors | Invirase / saquinavir hard-gel | Crixivan / indinavir | Norvir / ritonavir | Viracept / nelfinavir | Fortovase / saquinavir soft-gel |
| Agenerase / amprenavir | Kaletra (lopinavir/ritonavir) |
| Reyataz / atazanavir | Lexiva / fos-amprenavir | tipranavir |

Fusion Inhibitor | Fuzeon / T-20 / enfuvirtide |

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