kwin´vir mes´ilāt´),drug class: antiviral;
action: inhibits human immunodeficiency virus (HIV) protease important for viral replication;
use: used in combination with nucleoside analogues, zidovudine, or zalcitabine in the treatment of acquired immunodeficiency syndrome (AIDS).
saquinavir mesylate
Invirase
Pharmacologic class: Protease inhibitor
Therapeutic class: Antiretroviral
Pregnancy risk category B
Action
Inhibits human immunodeficiency virus (HIV) protease, preventing cleavage of HIV polyproteins and blocking virus replication and maturation
Availability
saquinavir mesylate
Capsules: 200 mg
⊘Indications and dosages
➣ Advanced HIV infection in selected patients
Adults older than age 16: 1,000 mg P.O. b.i.d. given only in combination with ritonavir b.i.d.
Contraindications
• Hypersensitivity to drug or its components
• Concurrent use of antiarrhythmics (amiodarone, bepridil, flecainide, propafenone, quinidine); astemizole, cisapride, or terfenadine (not available in United States); ergot derivatives; midazolam; pimozide; rifampin; or triazolam
• Severe hepatic impairment
• Monotherapy
Precautions
Use cautiously in:
• hepatic disease, hemophilia types A and B, diabetes mellitus
• pregnant or breastfeeding patients
• children younger than age 16.
Administration
• Give around the clock without missing doses, within 2 hours of a full meal.
• If prescribed in combination with ritonavir, give both drugs at same time.
• Know that drug is given only in combination with ritonavir, which inhibits its metabolism.
☞ Don't give concurrently with antiarrhythmics (amiodarone, bepridil, flecainide, propafenone, quinidine); astemizole, cisapride, terfenadine, ergot derivatives, midazolam, pimozide, rifampin, or triazolam. Life-threatening reactions may occur.
| Route | Onset | Peak | Duration |
| P.O. | Unknown | Unknown | Unknown |
Adverse reactions
CNS: headache, dizziness, paresthesia, asthenia, depression, insomnia, anxiety, confusion, ataxia, seizures, suicidal ideation, intracranial hemorrhage
CV: chest pain, peripheral vasoconstriction, thrombophlebitis
GI: nausea, vomiting, diarrhea, constipation, abdominal pain, flatulence, dyspepsia, buccal mucosal ulcers, pancreatitis
GU: urinary retention, nephrolithiasis, oliguria, acute renal insufficiency
Hematologic: hemolytic anemia, pancytopenia, thrombocytopenia, acute myeloblastic leukemia
Hepatic: jaundice, portal hypertension , exacerbation of chronic hepatic disease (with grade 4 elevated liver function test results)
Metabolic: hyperglycemia, diabetes mellitus (exacerbation or new onset), hypercalcemia, hyperkalemia, hypoglycemia
Musculoskeletal: musculoskeletal pain
Respiratory: bronchitis, cough
Skin: rash, Stevens-Johnson syndrome
Other: altered taste, drug fever
Interactions
Drug-drug. Antiarrhythmics (amiodarone, bepridil, flecainide, propafenone, quinidine), astemizole, cisapride, pimozide, terfenadine: increased blood levels of these drugs, life-threatening arrhythmias
Benzodiazepines, calcium channel blockers: increased blood levels of these drugs
Carbamazepine, dexamethasone, nevirapine, phenobarbital, phenytoin, rifabutin, rifampin: reduced saquinavir steady-state level
Clarithromycin, indinavir, ketoconazole, nelfinavir, ritonavir: increased saquinavir blood level
Ergot derivatives: elevated blood level of these drugs, life-threatening reactions such as acute ergot toxicity (peripheral vasospasm and ischemia of extremities and other tissues)
HMG-CoA reductase inhibitors: increased risk of myopathy (including rhabdomyolysis)
Midazolam, triazolam: increased risk of life-threatening prolonged or increased sedation or respiratory depression
Nonnucleoside reverse transcriptase inhibitors (delavirdine, nevirapine): increased saquinavir blood level
Sildenafil, tadalafil, tricyclic antidepressants, vardenafil: increased blood levels of these drugs
Warfarin: altered International Normalized Ratio
Drug-diagnostic tests. Alanine aminotransferase (ALT), amylase, aspartate aminotransferase (AST), bilirubin, calcium, creatinine phosphokinase, potassium: increased levels
Blood glucose: increased or decreased level
Phosphate: decreased level
Platelets, red blood cells, white blood cells: decreased counts
Drug-food. Any food: increased drug absorption
Grapefruit juice: elevated drug blood level, increased pharmacologic and adverse effects
Drug-herbs. Garlic capsules: decreased saquinavir blood level
St. John's wort: 50% reduction in saquinavir blood level
Patient monitoring
• Monitor platelet count, CBC, liver function tests, electrolytes, and uric acid and bilirubin levels. Watch for evidence of life-threatening blood dyscrasias and portal hypertension.
• Assess nutritional status and hydration.
• Monitor neurologic status. Stay alert for depression, suicidal ideation, seizures, and signs or symptoms of intracranial hemorrhage.
Patient teaching
• Tell patient to take with food (but not grapefruit juice) or within 2 hours of a full meal. Stress importance of taking doses around the clock on a regular schedule.
☞ Inform patient (and significant other as appropriate) that drug may cause depression and suicidal thoughts, which should be reported immediately.
• Advise patient to notify prescriber if rash occurs.
☞ Teach patient to recognize and immediately report signs and symptoms of liver disorder or bleeding tendency.
• Tell patient drug interacts with many other drugs, causing serious reactions. Advise him to discuss all drug use with prescriber before therapy starts.
• Caution patient to avoid St. John's wort and garlic capsules during therapy.
• Instruct female patient not to breastfeed, because she may transmit drug effects and HIV to infant.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, and herbs mentioned above.
saquinavir mesylate
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