Saquinavir

Drug #1521

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.

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Primary Characteristics

It is of Synthetic origin.

Molecular Weight: 766.95 · pK_a: 7 · Solubility in Water: 1 in 450 · Solubility in Alcohol: 1 in 392 · Non-proprietary name: Saquinavir.

Pharmacokinetics

Distribution: Saquinavir has a volume of distribution is 10.0l/kg. plasma protein binding is 98%.

Elimination: it is metabolised via > 90 % ( Liver), plasma half-life is 7-12hr, renal excretion is <1%.

Indications

Saquinavir is primarily indicated in conditions like HIV infection.

Contraindications

Saquinavir is contraindicated in conditions like Hepatic impairment, Hypersensitivity to any component of product.

Dosage

Saquinavir's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
1000 mg	1000 mg	Every 12h	PO	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.
Paediatric Dosage (20kg)
No data.
Neonatal Dosage (3kg)
No data.

Drug Interactions

Unknown9 interactions

8 interactions

Major3 interactions

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Saquinavir is known to cause more or less tolerable side effects which are usually transient. These include Abdominal discomfort, Diarrhea, Headache, Hemolytic anemia, Nausea, Nephrolithiasis , Skin RashX, Thrombocytopenia, Thrombophlebitis .

Warnings / Precautions

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.

Interference in Pathology

Saquinavir may interfere in the diagnosis of Increased serum triglycerides.

Available Brands

None recorded.

Storage Conditions

Saquinavir should be stored Hard Gelatin Caps. Soft Gelatin Caps.

Drug Classification

1.6.5.2 — Antiretroviral drugs