Peringatan Keamanan

The oral LD50 of saquinavir in both rats and mice is >5 g/kg.L14354 Data regarding overdose with saquinavir are limited.L3450 No acute toxicities or sequelae were noted in a patient ingesting 8 grams of saquinavir as a single dose, and a second subject ingesting 2.4 grams as a single dose experienced throat pain that lasted for 6 hours and subsequently resolved.L3450 Treatment of overdose should consist of symptomatic and supportive measures. Dialysis is unlikely to be of benefit given saquinavir's extensive protein-binding.L3450

Saquinavir

DB01232

small molecule approved investigational

Deskripsi

Saquinavir is an HIV-1 protease inhibitor used in combination with ritonavir and other antiretrovirals for the treatment of human immunodeficiency virus-1 (HIV-1) infection. In 1995 it became the first protease inhibitor approved by the FDA, followed shortly by ritonavir in 1996, and remains in clinical use today due to a relatively benign adverse effect profile as compared to other antiretroviral therapies.A214382 While its efficacy was initially limited by exceptionally poor oral bioavailability (approximately 4%),L3450 its current indications require the co-administration of ritonavir - a potent enzyme inhibitor - that increases the bioavailability and subsequent serum concentrations of saquinavir, thus dramatically improving antiviral activity.A214382,L3450,L14351

Struktur Molekul 2D

Berat 670.8408
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) -
Volume Distribusi The steady-state volume of distribution of saquinavir is approximately 700 L, suggesting extensive distribution into tissues.[L3450]
Klirens (Clearance) The systemic clearance of saquinavir is approximately 1.14 L/h/kg following intravenous administration.[L3450]

Absorpsi

The absolute bioavailability of orally administered saquinavir is only ~4%,L3450 thought to be a consequence of incomplete absorption and extensive first-pass metabolism. It is co-administered with ritonavir, another protease inhibitor and a potent inhibitor of the enzymes responsible for saquinavir's first-pass metabolism, in order to dramatically boost its serum concentrations and, by extension, its therapeutic efficacy. Following administration of saquinavir 1000mg twice daily with ritonavir 100mg twice daily the AUC24h at steady-state was 39026 ng.h/mL.L3450

Metabolisme

Saquinavir is extensively metabolized in the liver following oral administration, and in vitro studies have shown that >90% of its biotransformation is mediated by the CYP3A4 isoenzyme. Saquinavir is rapidly metabolized to a number of inactive mono- and di-hydroxylated compounds.L3450

Rute Eliminasi

The primary means of elimination of saquinavir appears to be extensive hepatic metabolism followed by fecal excretion of both the parent drug and metabolic products.L3450 Following the administration of radiolabeled saquinavir (both orally and intravenously), approximately 81-88% of radioactivity is recovered in the feces within 5 days of dosing while only 1-3% is recovered in the urine. Mass balance studies indicate that only 13% of orally-administered plasma radioactivity is attributed to unchanged parent drug, with the remainder comprising metabolic products of saquinavir's hepatic metabolism. In contrast, intravenous administration resulted in approximately 66% of the circulating plasma radioactivity being attributed to unchanged parent drug, suggesting a high degree of first-pass metabolism with oral administration.L3450

Interaksi Makanan

2 Data
  • 1. Avoid grapefruit products. Co-administration with grapefruit-containing products inhibits the metabolism of saquinavir.
  • 2. Take after a meal.

Interaksi Obat

1385 Data
Ivabradine Ivabradine may increase the QTc-prolonging activities of Saquinavir.
Afatinib The serum concentration of Afatinib can be increased when it is combined with Saquinavir.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Saquinavir.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Saquinavir.
Reserpine Reserpine may decrease the excretion rate of Saquinavir which could result in a higher serum level.
Ursodeoxycholic acid Ursodeoxycholic acid may decrease the excretion rate of Saquinavir which could result in a higher serum level.
Cholic Acid Cholic Acid may decrease the excretion rate of Saquinavir which could result in a higher serum level.
Valinomycin Valinomycin may decrease the excretion rate of Saquinavir which could result in a higher serum level.
Olmesartan Olmesartan may decrease the excretion rate of Saquinavir which could result in a higher serum level.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Saquinavir.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Saquinavir.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Saquinavir.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Saquinavir.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Saquinavir.
Silodosin The excretion of Silodosin can be decreased when combined with Saquinavir.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Saquinavir.
Pravastatin The serum concentration of Pravastatin can be decreased when it is combined with Saquinavir.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Saquinavir.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Saquinavir.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Saquinavir.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Saquinavir.
Dofetilide The risk or severity of adverse effects can be increased when Saquinavir is combined with Dofetilide.
Omeprazole The serum concentration of Saquinavir can be increased when it is combined with Omeprazole.
Lansoprazole The serum concentration of Saquinavir can be increased when it is combined with Lansoprazole.
Esomeprazole The serum concentration of Saquinavir can be increased when it is combined with Esomeprazole.
Rabeprazole The serum concentration of Saquinavir can be increased when it is combined with Rabeprazole.
Dexlansoprazole The metabolism of Dexlansoprazole can be decreased when combined with Saquinavir.
Dexrabeprazole The serum concentration of Saquinavir can be increased when it is combined with Dexrabeprazole.
Ilaprazole The serum concentration of Saquinavir can be increased when it is combined with Ilaprazole.
Vonoprazan The metabolism of Vonoprazan can be decreased when combined with Saquinavir.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Saquinavir.
Cisapride The serum concentration of Cisapride can be increased when it is combined with Saquinavir.
Clarithromycin The serum concentration of Clarithromycin can be increased when it is combined with Saquinavir.
Cyclophosphamide The serum concentration of the active metabolites of Cyclophosphamide can be increased when Cyclophosphamide is used in combination with Saquinavir.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Saquinavir.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Saquinavir.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Saquinavir.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Saquinavir.
Nevirapine The serum concentration of Saquinavir can be decreased when it is combined with Nevirapine.
Alprazolam The serum concentration of Alprazolam can be increased when it is combined with Saquinavir.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Saquinavir.
Cimetidine Cimetidine can cause an increase in the absorption of Saquinavir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Nizatidine Nizatidine can cause an increase in the absorption of Saquinavir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Ranitidine Ranitidine can cause an increase in the absorption of Saquinavir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Famotidine Famotidine can cause an increase in the absorption of Saquinavir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Methantheline Methantheline can cause an increase in the absorption of Saquinavir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Promethazine Promethazine can cause an increase in the absorption of Saquinavir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Doxepin Doxepin can cause an increase in the absorption of Saquinavir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Asenapine Asenapine can cause an increase in the absorption of Saquinavir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Metiamide Metiamide can cause an increase in the absorption of Saquinavir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Roxatidine acetate Roxatidine acetate can cause an increase in the absorption of Saquinavir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Lafutidine Lafutidine can cause an increase in the absorption of Saquinavir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Lavoltidine Lavoltidine can cause an increase in the absorption of Saquinavir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Niperotidine Niperotidine can cause an increase in the absorption of Saquinavir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Olanzapine Olanzapine can cause an increase in the absorption of Saquinavir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Epinastine Epinastine can cause an increase in the absorption of Saquinavir resulting in an increased serum concentration and potentially a worsening of adverse effects.
Bosentan The serum concentration of Bosentan can be increased when it is combined with Saquinavir.
Rifabutin The serum concentration of the active metabolites of Rifabutin can be increased when Rifabutin is used in combination with Saquinavir.
Efavirenz Saquinavir may increase the hepatotoxic activities of Efavirenz.
Clorazepic acid The serum concentration of Clorazepic acid can be increased when it is combined with Saquinavir.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Saquinavir.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Saquinavir.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Saquinavir.
Flurazepam The serum concentration of Flurazepam can be increased when it is combined with Saquinavir.
Diazepam The serum concentration of Diazepam can be increased when it is combined with Saquinavir.
Triazolam The serum concentration of Triazolam can be increased when it is combined with Saquinavir.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Saquinavir.
Quinidine The metabolism of Quinidine can be increased when combined with Saquinavir.
Ketoconazole The serum concentration of Ketoconazole can be increased when it is combined with Saquinavir.
Rifampin The serum concentration of Saquinavir can be decreased when it is combined with Rifampicin.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Saquinavir.
Itraconazole The serum concentration of Saquinavir can be increased when it is combined with Itraconazole.
Bepridil Bepridil may increase the QTc-prolonging and arrhythmogenic activities of Saquinavir.
Darunavir The serum concentration of Darunavir can be decreased when it is combined with Saquinavir.
Lopinavir The serum concentration of Saquinavir can be increased when it is combined with Lopinavir.
Eluxadoline The serum concentration of Eluxadoline can be increased when it is combined with Saquinavir.
Vincristine The excretion of Vincristine can be decreased when combined with Saquinavir.
Doxorubicin The serum concentration of Doxorubicin can be increased when it is combined with Saquinavir.
Garlic Garlic can cause a decrease in the absorption of Saquinavir resulting in a reduced serum concentration and potentially a decrease in efficacy.
Insulin human The therapeutic efficacy of Insulin human can be decreased when used in combination with Saquinavir.
Insulin lispro The therapeutic efficacy of Insulin lispro can be decreased when used in combination with Saquinavir.
Insulin glargine The therapeutic efficacy of Insulin glargine can be decreased when used in combination with Saquinavir.
Insulin pork The therapeutic efficacy of Insulin pork can be decreased when used in combination with Saquinavir.
Glimepiride The therapeutic efficacy of Glimepiride can be decreased when used in combination with Saquinavir.
Acarbose The therapeutic efficacy of Acarbose can be decreased when used in combination with Saquinavir.
Acetohexamide The therapeutic efficacy of Acetohexamide can be decreased when used in combination with Saquinavir.
Miglitol The therapeutic efficacy of Miglitol can be decreased when used in combination with Saquinavir.
Chlorpropamide The therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Saquinavir.
Tolazamide The therapeutic efficacy of Tolazamide can be decreased when used in combination with Saquinavir.
Phenformin The therapeutic efficacy of Phenformin can be decreased when used in combination with Saquinavir.
Gliclazide The therapeutic efficacy of Gliclazide can be decreased when used in combination with Saquinavir.
Gliquidone The therapeutic efficacy of Gliquidone can be decreased when used in combination with Saquinavir.
Mitiglinide The therapeutic efficacy of Mitiglinide can be decreased when used in combination with Saquinavir.
Exenatide The therapeutic efficacy of Exenatide can be decreased when used in combination with Saquinavir.
Mecasermin The therapeutic efficacy of Mecasermin can be decreased when used in combination with Saquinavir.
Pramlintide The therapeutic efficacy of Pramlintide can be decreased when used in combination with Saquinavir.
Glisoxepide The therapeutic efficacy of Glisoxepide can be decreased when used in combination with Saquinavir.
Insulin aspart The therapeutic efficacy of Insulin aspart can be decreased when used in combination with Saquinavir.
Insulin detemir The therapeutic efficacy of Insulin detemir can be decreased when used in combination with Saquinavir.
Insulin glulisine The therapeutic efficacy of Insulin glulisine can be decreased when used in combination with Saquinavir.

Target Protein

Gag-Pol polyprotein gag-pol
Pol polyprotein pol

Referensi & Sumber

Artikel (PubMed)
  • PMID: 11483925
    Forestier F, de Renty P, Peytavin G, Dohin E, Farinotti R, Mandelbrot L: Maternal-fetal transfer of saquinavir studied in the ex vivo placental perfusion model. Am J Obstet Gynecol. 2001 Jul;185(1):178-81.
  • PMID: 19714702
    De Clercq E: The history of antiretrovirals: key discoveries over the past 25 years. Rev Med Virol. 2009 Sep;19(5):287-99. doi: 10.1002/rmv.624.
  • PMID: 9578182
    Kupferschmidt HH, Fattinger KE, Ha HR, Follath F, Krahenbuhl S: Grapefruit juice enhances the bioavailability of the HIV protease inhibitor saquinavir in man. Br J Clin Pharmacol. 1998 Apr;45(4):355-9. doi: 10.1046/j.1365-2125.1998.t01-1-00687.x.
  • PMID: 22762019
    Sundquist WI, Krausslich HG: HIV-1 assembly, budding, and maturation. Cold Spring Harb Perspect Med. 2012 Jul;2(7):a006924. doi: 10.1101/cshperspect.a006924.
  • PMID: 19108994
    De Clercq E: Anti-HIV drugs: 25 compounds approved within 25 years after the discovery of HIV. Int J Antimicrob Agents. 2009 Apr;33(4):307-20. doi: 10.1016/j.ijantimicag.2008.10.010. Epub 2008 Dec 23.

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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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