Saquinavir
When ATH:
J05AE01
Pharmacological action.
Inhibiting HIV protease.
Application.
Combination therapy of HIV infection in combination with antiretroviral agents.
Contraindications.
Hypersensitivity.
Restrictions to the use of.
Severe liver damage (may increase the plasma concentration), severe renal insufficiency, Age to 16 and older 65 years (safety and efficacy in these age groups are not defined).
Pregnancy and breast-feeding.
During pregnancy is possible only in exceptional cases (there is no clinical experience). At the time of treatment should stop breastfeeding.
Side effects.
From the nervous system and sensory organs: headache (8%), peripheral neuropathy (8%), paraesthesia (6%), numbness (5%), dizziness (2%), depression (≥ 2%), weakness (≥ 2%), asthenic syndrome (≥ 2%), confusion, drowsiness, ataxia, convulsions, suicide attempt.
Cardio-vascular system and blood: hypertension, gipotenziya, cyanosis, syncope, tromboflebit, gemoliticheskaya anemia, thrombocytopenia, neutropenia.
From the digestive tract: diarrhea (17%), nausea (8%), ulcerative stomatitis (6%), abdominal discomfort (4%), vomiting (3%), abdominal pain (3%), flatulence (2%), cheilitis, dysphagia, dyspepsia (≥ 5%), constipation (≥ 2%), ileus, hepatitis, jaundice, portal hypertension.
Metabolism: giperglikemiâ, diabetes, ketoacidosis obesity, degidratatsiya.
With the genitourinary system: nephrolithiasis.
For the skin: skin rashes (5%), itch (3%), dermatitis, эritema, Warts, Syndrome Stevens - Johnson.
Other: ossalgia, myalgia (≥ 2%), xerophthalmia, fever, increased activity of transaminases and creatine phosphokinase.
Combined therapy (additionally):
With zalzitabinom: insomnia, vomiting, appetite disorders, gipoglikemiâ.
With zidovudine: tides, violation of skin pigmentation, euphoria, insomnia, irritability, dry mouth, anorexia, gipermotorika intestine, discoloration of feces, glossitis, laringit, dysuria, myelogenous leukemia.
With zalcitabine and zidovudine: insomnia, intellectual impairment, irritability, euphoria, blurred vision and taste sensations, mucous membranes, glossitis, pharyngitis, breathlessness, appetite disorders, pancreatitis, Sweating.
Cooperation.
Combination with ddC and / or zidovudine not affect their absorption, metabolism, excretion and toxicity profile.
Simultaneous treatment with ranitidine during the meal increases AUC by 67% as compared to that when receiving only food. Inhibitors of the enzyme CYP3A4 (clarithromycin, ketoconazole, fluconazole, itraconazole, mikonazol, grapefruit juice) increase plasma concentration, without affecting T1/2.
Hepatic enzyme inducers (rifampicin, rifabutin, phenobarbital, phenytoin, Carbamazepine, Dexamethasone) reduce the concentration and activity.
May increase the plasma concentration and toxicity, etc.. compounds, is a substrate for CYP3A4 (nifedipine, verapamil, diltiazem, dapsone, klindamiцin, quinidine, ergot alkaloids). Simultaneous treatment with benzodiazepines, metabolized by CYP3A4 (midazolam, triazolam), It may be associated with prolongation of sedation.
Increases (mutually) AUC и Cmax Ritonavir, Nevirapine, indinavir, Nelfinavir, clarithromycin, Terfenadine.
Overdose.
Сообщалось об одном случае приема в дозе 8000 mg. Through 2 ч после приема у больного была вызвана рвота, no adverse effects were noted.
Dosing and Administration.
Inside, 1200 mg 3 once a day (саквинавира мезилат — 600 mg 3 once a day), not later than, than 2 hours after meals. Назначение дозы меньше 3600 mg / day (саквинавира мезилата — 1800 mg / day) not recommended. When combined with other protease inhibitors may reduce the dose.
Precautions.
It is recommended to adhere strictly to the reception. In the event of severe toxic effects, treatment should be interrupted. During treatment requires monitoring of blood glucose levels because of the possibility of development of hyperglycemia or diabetes. Dose adjustment in patients with mild to moderate renal and liver is not required. There are cases of liver deterioration and the emergence of portal hypertension in patients with already existing hepatitis B or C, cirrhosis or other liver disease (a causal relationship to saquinavir reception is not installed). When mild to moderate renal and / or hepatic insufficiency treatment is not accompanied by a deterioration in laboratory parameters.
In patients with hemophilia type A and B increases the risk of spontaneous bleeding and bruising.
Perhaps redistribution and accumulation of fat on the type of central obesity, deposition of fat on the back of the neck ("Climacteric hump").
Cautions.
Saquinavir does not cure HIV infection, during treatment, you may experience AIDS-related illnesses, incl. opportunistic infections. Data on the effect of treatment on the risk of HIV transmission are absent.
