| |
Invirase™ Roche
saquinavir |
Norvir™ Abbott
ritonavir |
Crixivan® Merck
indinavir |
Viracept® Agouron
nelfinavir |
| Dosage |
600 mg tid |
600 mg bid |
800 mg q8h |
750 mg tid |
Dosage Strength/
Dosage Form |
200 mg capsule |
100 mg capsule
600 mg/7.5 mL oral solution |
200 mg capsule
400 mg capsule |
250 mg tablets
50 mg/g powder |
Number
per Full dose |
3 capsules
(9/day full dose) |
6 capsules
(12/day full dose) |
2 (400 mg) capsules
(6/day full dose) |
3 tablets (9/day full dose)
powder See Table B
|
Volume per
Full Dose |
n/a |
7.5 mL (15 mL/day full dose) See Table A for additional
Pediatric Information
|
n/a |
Variable, oral powder 50 mg/g may be
reconstituted with a small amount of water, milk,
formula, soy formula, soy milk or dietary supplements. (See Table B
for additional Pediatric Information
|
| Relation to Food |
Take on a full stomach, within 2
hours of a high fat meal if possible. (e.g. 48 g protein,
60 g carbohydrate, 57 g fat; 1006 Kcal) (Administration
of saquinavir on an empty stomach dramatically reduces
the drug's absorption) |
Take with food if possible. The
taste of the oral solution may be improved by mixing with
chocolate milk, Ensure or Advera. If the solution is
mixed to improve the taste, it must be taken within 1
hour of mixing. |
Take on an empty stomach with water
1 hour before or 2 hours after a meal. May be
administered with other liquids such as skim milk, juice,
coffee, or tea or with a light meal. (Ingestion of
Crixivan with a meal high in calories, fat, and protein
reduces the drug's absorption.) At least 1.5 liters of
liquids should be taken during the course of 24 hours to
ensure adequate hydration and minimize potential side
effect of nephrolithiasis. |
Take with Food. Maximum plasma
concentrations and AUC were 2 to 3-fold higher under fed
conditions compared to fasting. Meals contained 517-719
Kcal with 153-313 Kcal derived from fat. |
Dosage Initiation/
Adjustments
(Also see drug interactions) |
In combination therapy, dose
adjustment of the nucleoside analogue should be based on
the drug's toxicity profile. Lower Doses
of saquinavir are not recommended due to poor
bioavailability.
|
Dose escalation may provide relief
of nausea when initiating therapy¼. Begin at no
less than 300 mg bid and increase by 100 mg bid
increments up to 600 mg bid.
|
Reduce the dose to 600 mg q8h in
mild-to-moderate hepatic insufficiency due to cirrhosis.
Patients who experience nephrolithiasis my interrupt or
discontinue therapy (e.g. 1-3 days) during the acute
episode. |
If a dose is missed, take the dose
as soon as possible and return to normal schedule. Do not
double the next dose. Pharmaco-
kinetics in patients with
hepatic or renal insufficiency have not been studied.
However, less than 2% of nelfinavir is excreted n the
urine so the impact of renal impairment is minimal.
Caution when administering in patients with hepatic
impairment. |
| Storage Requirements |
Room Temperature
Tightly Closed Bottle |
Store capsules in the refrigerator
at all time and protect from light. Store oral
solution in the refrigerator until dispensed.
Refrigeration by the patient of the oral solution is
recommended but not required if used within 30 days.
Store in original container. Avoid exposure to excessive
heat.
|
Room Temperature, Tightly Closed
Bottle. Capsules are sensitive to moisture and should be
dispensed and stored in the original container. The
desiccant should remain in the original bottle. |
Room Temperature: Tablets and Oral
PowderAdvertisementOral Powder mixed with liquids,
water, milk, formula, etc. should be used within 6 hours.
|
| Combination or Monotherapy |
Combination Use Only |
Combination and Monotherapy
Use |
Combination and Monotherapy
Use |
Combination Use Only |
| Route of Metabolism |
Cytochrome P450, specifically CYP3A4
isoenzyme. |
Cytochrome P450
(CYP3A>>2D6>>
2C>1A2) |
Cytochrome P450, specifically CYP3A4
isoenzyme. |
Cytochrome P-450 (CYP3A) |
| Adverse Effects (Most frequently
reported - check with your physician for
complete information) |
diarrhea, abdominal discomfort and
nausea |
asthenia, diarrhea, nausea,
vomiting, circumoral paresthesia, taste perversion,
peripheral paresthesia |
nephrolithiasis, asymptomatic
hyperbili-
rubinemia, nausea, abdominal pain |
diarrhea, nausea, flatulence;
diarrhea can usually be controlled with non-prescription
drugs, such as Imodium to slow GI motility. |
This article was provided by U.S. Food and Drug Administration. It is a part of the publication Protease Inhibitors Backgrounder.
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