Saquinavir

Saquinavir is an agent for treatment of HIV infection. It was the first protease inhibitor to be approved and is the result of a project begun in 1986 to design by computer, molecules that would fit into the active site of the HIV protease enzyme. Synthesis of Saquinavir is a long, 17-step process that has hindered the development of this agent, limiting its commercial availability. Although protease inhibitors are potent antiretroviral agents, resistance to it has been noted following several months of administration.

Brands
Adult Dose
Dose: 1000 mg
Single Dose: 1000 (1000)
Frequency: 12 hourly
Route: PO
Instructions: Saquinavir is given as Saquinavir mesylate in combination with ritonavir 100-mg bid. Ritonavir should be taken at the same time as Saquinavir mesylate. Saquinavir mesylate and ritonavir should be taken within 2 hours after a meal.
Neonatal
Paedriatic
Characteristics
. It is of Synthetic origin. . The Molecular Weight of Saquinavir is 766.95. Its pKa is 7.
Contraindications
Saquinavir is contraindicated in conditions like Hepatic impairment,Hypersensitivity to any component of product.
Effects
The symptomatic adverse reactions produced by Saquinavir are more or less tolerable and if they become severe, they can be treated symptomatically, these include Headache, Nausea, Diarrhea, Skin RashX, Thrombophlebitis, Hemolytic anemia, Thrombocytopenia, Nephrolithiasis, Abdominal discomfort.
Indications
Saquinavir is primarily indicated in conditions like HIV infection.
Interactions
Saquinavir is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementAfatinibmay increase the level of afatinib use alterntive or reduced doseAmobarbitalBarbiturates possibly reduces plasma concentration of indinavir.MajorCarbamazepinePlasma concentration of Carbamazepine possibly increased by Saquinavir.MajorDexamethasoneErlotinibThis CYP3A4 inhibitor increases levels/toxicity of erlotinibIndinavir (Sulphate)MethylergonovineCoadministration with protease inhibitors (PIs), particularly ritonavir, may significantly increase the plasma concentrations of ergot derivatives. The mechanism is PI inhibition of CYP450 3A4, the isoenzyme responsible for the metabolic clearance of ergotamine and related drugs. Clinical ergotism, occasionally resulting in surgical amputation or death, has been reported in patients receiving ergotamine tartrate with ritonavir, indinavir, and/or nelfinavir. Even small, single doses of ergotamine have been involved in clinically significant interactions.MajorGiven the potential for ergot toxicity characterized by peripheral vasospasm, ischemia, thrombosis, tachycardia and hypertension, concomitant use of ergot derivatives with protease inhibitors is considered contraindicated. NelfinavirNevirapineNevirapinePhenytoin (Na)RifabutinRifampicinRitonavirSalmeterolConcurrent use may potentiate the risk of cardiovascular adverse events.SunitinibMay increases sunitinib concentrations.VemurafenibSaquinavir inhibits P-gp, glucuronidation and CYP3A4, and increases plasma concentration of Vemurafenib.VORICONAZOLEVoriconazole may increase the serum concentration of saquinavir by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Interfrence
Increased serum triglycerides
Risks
Drug should not be given to patients suffering from Kidney dysfunction, and patients suffering from Liver Malfunction.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.
Storage
Hard Gelatin Caps Store at room temperature. Soft Gelatin Caps Store in refrigerator.
Warnings
Caution is required in diabetic patient, patients with hemophilia who may experienced increased bleeding. It should be used with caution and possible dose reduction is needed in hepatic impairment. Adequate hydration is recommended to avoid any risk of nephrolithiasis. Monotoring is required in case of renal impairment.
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