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Saquinavir Disease Interactions

There are 6 disease interactions with saquinavir:

Major

PIs (applies to saquinavir) hemophilia

Major Potential Hazard, Low plausibility. Applicable conditions: Coagulation Defect

There have been postmarketing reports of increased bleeding, including spontaneous skin hematomas and hemarthrosis, in types A and B hemophiliac patients treated with protease inhibitors. However, a causal relationship has not been established. In some patients, additional Factor VIII was given. In more than half of the reported cases, protease inhibitor therapy was continued or reintroduced following an interruption. Hemophiliacs and patients with other coagulation defects should be monitored closely for bleeding during protease inhibitor therapy.

References

  1. "Product Information. Agenerase (amprenavir)." Glaxo Wellcome, Research Triangle Pk, NC.
  2. "Product Information. Crixivan (indinavir)." Merck & Co, Inc, West Point, PA.
  3. "Product Information. Viracept (nelfinavir)." Agouron Pharma Inc, La Jolla, CA.
  4. "Product Information. Kaletra (lopinavir-ritonavir)" Abbott Pharmaceutical, Abbott Park, IL.
  5. "Product Information. Norvir (ritonavir)." Abbott Pharmaceutical, Abbott Park, IL.
  6. "Product Information. Lexiva (fosamprenavir)." GlaxoSmithKline, Research Triangle Park, NC.
  7. "Product Information. Invirase (saquinavir)." Roche Laboratories, Nutley, NJ.
  8. "Product Information. Reyataz (atazanavir)." Bristol-Myers Squibb, Princeton, NJ.
  9. "Product Information. Fortovase (saquinavir)" Roche Laboratories, Nutley, NJ.
  10. "Product Information. Aptivus (tipranavir)." Boehringer-Ingelheim, Ridgefield, CT.
View all 10 references
Major

Saquinavir (applies to saquinavir) QT prolongation

Major Potential Hazard, Moderate plausibility. Applicable conditions: Arrhythmias, Congestive Heart Failure, Hypokalemia, Magnesium Imbalance, Cardiomyopathy

QT and PR interval dose-dependent prolongation and torsades de pointes have been reported with the use of saquinavir (saquinavir should always be used in combination with ritonavir). Saquinavir should not be used in patients with congenital long QT syndrome, patients with refractory hypokalemia or hypomagnesemia, or in combination with other drugs that can both prolong the QT interval and increase the plasma concentration of saquinavir. Saquinavir is also contraindicated in patients with a complete atrioventricular (AV) block without an implanted pacemaker or patients at risk of a complete AV block.
Caution and close EKG and electrolyte monitoring is recommended if therapy is initiated in patients with congestive heart failure, bradyarrhythmias, structural heart disease, cardiomyopathies, ischemic heart disease, hepatic impairment, and electrolyte abnormalities.

Moderate

PIs (applies to saquinavir) hyperglycemia

Moderate Potential Hazard, Moderate plausibility. Applicable conditions: Abnormal Glucose Tolerance, Diabetes Mellitus

New onset diabetes mellitus, exacerbation of preexisting diabetes mellitus, glucose intolerance, hyperglycemia, and some cases of diabetic ketoacidosis have been reported during postmarketing surveillance in HIV-infected patients treated with protease inhibitors (PIs). In some cases, glucose abnormalities/hyperglycemia persisted despite discontinuation of PI therapy. Frequently, insulin resistance may accompany fat redistribution and serum lipid elevations in what is collectively termed the HIV-associated lipodystrophy syndrome. Although a causal relationship has not been established, these metabolic disturbances have most often occurred in HIV-infected patients during treatment with potent antiretroviral regimens containing PIs. Monitoring patients for hyperglycemia, new onset diabetes mellitus, or exacerbation of diabetes mellitus should be considered during PI therapy. Dosage adjustments in insulin or oral hypoglycemic medications may be necessary in patients with diabetes.

References

  1. Hardy H, Esch LD, Morse GD "Glucose disorders associated with HIV and its drug therapy." Ann Pharmacother 35 (2001): 343-51
  2. "Product Information. Viracept (nelfinavir)." Agouron Pharma Inc, La Jolla, CA.
  3. "Product Information. Lexiva (fosamprenavir)." GlaxoSmithKline, Research Triangle Park, NC.
  4. "Product Information. Invirase (saquinavir)." Roche Laboratories, Nutley, NJ.
  5. Kaufman MB, Simionatto C "A review of protease inhibitor-induced hyperglycemia." Pharmacotherapy 19 (1999): 114-7
  6. "Product Information. Agenerase (amprenavir)." Glaxo Wellcome, Research Triangle Pk, NC.
  7. Noor MA, Lo JC, Mulligan K, Schwarz JM, Halvorsen RA, Schambelan M, Grunfeld C "Metabolic effects of indinavir in healthy HIV-seronegative men." Aids 15 (2001): f11-8
  8. "Product Information. Crixivan (indinavir)." Merck & Co, Inc, West Point, PA.
  9. "Product Information. Fortovase (saquinavir)" Roche Laboratories, Nutley, NJ.
  10. Pujol RM, Domingo P, XavierMatiasGuiu, Francia E, Sanbeat MA, Alomar A, Vazquez G "HIV-1 protease inhibitor-associated partial lipodystrophy: Clinicopathologic review of 14 cases." J Am Acad Dermatol 42 (2000): 193-8
  11. "Product Information. Aptivus (tipranavir)." Boehringer-Ingelheim, Ridgefield, CT.
  12. Struble K, Piscitelli SC "Syndromes of abnormal fat redistribution and metabolic complications in HIV-infected patients." Am J Health Syst Pharm 56 (1999): 2343-8
  13. "Product Information. Norvir (ritonavir)." Abbott Pharmaceutical, Abbott Park, IL.
  14. Mauss S, Wolf E, Jaeger H "Impaired glucose tolerance in HIV-positive patients receiving and those not receiving protease inhibitors." Ann Intern Med 130 (1999): 162-3
  15. "Product Information. Reyataz (atazanavir)." Bristol-Myers Squibb, Princeton, NJ.
  16. Qaqish RB, Fisher E, Rublein J, Wohl DA "HIV-associated lipodystrophy syndrome." Pharmacotherapy 20 (2000): 13-22
  17. Tsiodras S, Mantzoros C, Hammer S, Samore M "Effects of protease inhibitors on hyperglycemia, hyperlipidemia, and lipodystrophy - A 5-year cohort study." Arch Intern Med 160 (2000): 2050-6
  18. "Product Information. Kaletra (lopinavir-ritonavir)" Abbott Pharmaceutical, Abbott Park, IL.
  19. Dube MP, Johnson DL, Currier JS, Leedom JM "Protease inhibitor-associated hyperglycaemia." Lancet 350 (1997): 713-4
  20. Carr A "HIV protease inhibitor-related lipodystrophy syndrome." Clin Infect Dis 30 (2000): s135-42
  21. Walli R, Demant T "Impaired glucose tolerance and protease inhibitors." Ann Intern Med 129 (1998): 837-8
  22. Brambilla AM, Novati R, Calori G, et al. "Stavudine or indinavir-containing regimens are associated with an increased risk of diabetes mellitus in HIV-infected individuals." AIDS 17 (2003): 1993-5
View all 22 references
Moderate

PIs (applies to saquinavir) hyperlipidemia

Moderate Potential Hazard, High plausibility. Applicable conditions: Ischemic Heart Disease, History - Myocardial Infarction

Hyperlipidemia has been observed in 10% of patients receiving ritonavir during clinical trials. Increases of 30% to 40% from baseline have been reported for total cholesterol and 200% to 300% or more for triglycerides. These effects have also been reported during postmarketing experience with other protease inhibitors (PIs) but may be the most dramatic with ritonavir. The clinical significance of these elevations is unclear. Severe hyperlipidemia is known to sometimes cause pancreatitis. In addition, some patients have reportedly developed symptomatic atherosclerosis and coronary artery disease after initiating PI treatment. Patients with preexisting hyperlipidemia may require closer monitoring during PI therapy, and adjustments made accordingly in their lipid-lowering regimen. PI therapy should be administered cautiously in patients with coronary artery disease or a history of ischemic heart disease.

References

  1. "Product Information. Agenerase (amprenavir)." Glaxo Wellcome, Research Triangle Pk, NC.
  2. Noor MA, Lo JC, Mulligan K, Schwarz JM, Halvorsen RA, Schambelan M, Grunfeld C "Metabolic effects of indinavir in healthy HIV-seronegative men." Aids 15 (2001): f11-8
  3. "Product Information. Reyataz (atazanavir)." Bristol-Myers Squibb, Princeton, NJ.
  4. "Product Information. Norvir (ritonavir)." Abbott Pharmaceutical, Abbott Park, IL.
  5. Echevarria KL, Hardin TC, Smith JA "Hyperlipidemia associated with protease inhibitor therapy." Ann Pharmacother 33 (1999): 859-63
  6. Struble K, Piscitelli SC "Syndromes of abnormal fat redistribution and metabolic complications in HIV-infected patients." Am J Health Syst Pharm 56 (1999): 2343-8
  7. Sullivan AK, Feher MD, Nelson MR, Gazzard BG "Marked hypertriglyceridaemia associated with ritonavir therapy." AIDS 12 (1998): 1393-4
  8. "Product Information. Kaletra (lopinavir-ritonavir)" Abbott Pharmaceutical, Abbott Park, IL.
  9. Flynn TE, Bricker LA "Myocardial infarction in HIV-infected men receiving protease inhibitors." Ann Intern Med 131 (1999): 548
  10. Tsiodras S, Mantzoros C, Hammer S, Samore M "Effects of protease inhibitors on hyperglycemia, hyperlipidemia, and lipodystrophy - A 5-year cohort study." Arch Intern Med 160 (2000): 2050-6
  11. Karmochkine M, Raguin G "Severe coronary artery disease in a young HIV-infected man with no cardiovascular risk factor who was treated with indinavir." AIDS 12 (1998): 2499
  12. Segerer S, Bogner JR, Walli R, Loch O, Goebel FD "Hyperlipidemia under treatment with proteinase inhibitors." Infection 27 (1999): 77-81
  13. "Product Information. Invirase (saquinavir)." Roche Laboratories, Nutley, NJ.
  14. "Product Information. Lexiva (fosamprenavir)." GlaxoSmithKline, Research Triangle Park, NC.
  15. "Product Information. Crixivan (indinavir)." Merck & Co, Inc, West Point, PA.
  16. "Product Information. Fortovase (saquinavir)" Roche Laboratories, Nutley, NJ.
  17. Costa A, Pulido F, Rubio R, Cepeda C, Torralba M, Costa JR "Lipid changes in HIV-infected patients who started rescue therapy with an amprenavir/ritonavir-based highly active antiretroviral therapy." AIDS 16 (2002): 1983-4
  18. "Product Information. Aptivus (tipranavir)." Boehringer-Ingelheim, Ridgefield, CT.
  19. "Product Information. Viracept (nelfinavir)." Agouron Pharma Inc, La Jolla, CA.
View all 19 references
Moderate

Saquinavir (applies to saquinavir) liver disease

Moderate Potential Hazard, High plausibility. Applicable conditions: Alcoholism

Saquinavir is primarily metabolized by the liver. Patients with liver disease may be at greater risk for adverse effects from saquinavir due to decreased drug clearance, so therapy should be administered cautiously in these patients. Additionally, there have been reports of worsening liver disease in patients with underlying hepatitis B or C, cirrhosis, chronic alcoholism, and other liver abnormalities. Close monitoring is recommended. The use of saquinavir when administered with ritonavir is contraindicated in patients with severe hepatic impairment.

References

  1. Sommadossi JP "HIV protease inhibitors: pharmacologic and metabolic distinctions." AIDS 13 (1999): s29-40
  2. "Product Information. Invirase (saquinavir)." Roche Laboratories, Nutley, NJ.
Moderate

Saquinavir (applies to saquinavir) renal impairment

Moderate Potential Hazard, Moderate plausibility. Applicable conditions: Renal Dysfunction

The principal route of excretion for saquinavir is by hepatic metabolism, therefore no initial dose adjustment is necessary in patients with renal impairment. However, saquinavir has not been studied in patients with severe renal impairment and end-stage renal disease, and caution should be exercised when prescribing this drug to these patients.

Saquinavir drug interactions

There are 625 drug interactions with saquinavir

Saquinavir alcohol/food interactions

There are 2 alcohol/food interactions with saquinavir

Drug Interaction Classification

These classifications are only a guideline. The relevance of a particular drug interaction to a specific individual is difficult to determine. Always consult your healthcare provider before starting or stopping any medication.
Major Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit.
Moderate Moderately clinically significant. Usually avoid combinations; use it only under special circumstances.
Minor Minimally clinically significant. Minimize risk; assess risk and consider an alternative drug, take steps to circumvent the interaction risk and/or institute a monitoring plan.
Unknown No interaction information available.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.