Norvir

Antiviral agent ritonavir, a peptide inhibitor of HIV-1 and HIV-2 proteases. Enzymatic cleavage of the protease prevents the activation of the protein precursor and leads to the synthesis of immature HIV particles which are unable to initiate further development of the infection. Proteolysis of polypeptides of HIV stops the life cycle of its replication. It binds C2-symmetric part of the active area of HIV protease, has a high selective affinity for it and has a weak inhibitory effect on the protease of a human. It also increases the number of CD4+cells in the blood and reduces the concentration of viral RNA. It increases the overall number of white blood cells, lymphocytes and platelets.

 


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Description

Norvir: Pharmacological action.

Antiviral agent ritonavir, a peptide inhibitor of HIV-1 and HIV-2 proteases. Enzymatic cleavage of the protease prevents the activation of the protein precursor and leads to the synthesis of immature HIV particles which are unable to initiate further development of the infection. Proteolysis of polypeptides of HIV stops the life cycle of its replication. It binds C2-symmetric part of the active area of HIV protease, has a high selective affinity for it and has a weak inhibitory effect on the protease of a human. It also increases the number of CD4+cells in the blood and reduces the concentration of viral RNA. It increases the overall number of white blood cells, lymphocytes and platelets.

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Norvir: Indications for use

HIV (adults and children) as a part of combination therapy.

Norvir: Drug Contraindications

Hypersensitivity.

Norvir: Side effects.

Nausea, vomiting, diarrhea, loss of appetite, abdominal pain, dryness of the mucous membrane of the mouth, dyspepsia, eructation, flatulence, irritation of the larynx, loss of taste sensations; fever, allergic reactions; fear, insomnia, paresthesia, asthenia, headache, dizziness, drowsiness; weight loss; myalgia; cough, pharyngitis; rash papular, itchy skin, excessive sweating; hyperglycemia, anemia, decreased hematocrit, erythropenia, leukopenia, neutropenia, eosinophilia, hyperuricaemia, hypokalaemia, increased activity of “liver” transaminases, hypertriglyceridemia.

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Method of application and doses.

The drug is taken inside, during the meal, 600 mg 2 times a day (as the sole protease inhibitor). The initial dose for reducing the side effects is 300 mg 2 times a day, then you should increase the dose by 100 mg at each meal every day to achieve the dose of 600 mg 2 times a day. The drug is prescribed in combination with saquinavir at the dosage of 300 mg 2 times a day, with indinavir – 200 mg 2 times per day with subsequent increase of dose (within 2 weeks) by 100 mg to 400 mg 2 times per day. Children – 400 mg/sq m body surface 2 times a day; when poor tolerability of the initial dose – 250 mg/sq m, with a further increase by 50 mg/sq m at each reception every 2-3 days, until you reach the dose of 400 mg/m 2 times a day. If you take ritonavir in combination with saquinavir, the treatment starts with a dose of 300 mg 2 times a day; in combination with indinavir – with a dose of 200 mg 2 times per day, which is increased gradually (by 100 mg), to 400 mg 2 times a day for 2 weeks.

Norvir: Special instructions.

During treatment, it is necessary to regularly monitor the clinical and biochemical analysis of the blood activity of “liver” transaminases in addition to specific immunological and virological analysis. During the treatment of patients with hemophilia A and B, it may increase the likelihood of bleeding (cutaneous and articular hematomas); after specific treatment, the therapy can be continued under the regular control of blood parameters.

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Interaction with other drugs

It increases the concentration of drugs metabolized by isoenzymes of cytochrome P450 (including amiodarone, astemizole, Itraconazole, ketoconazole, bepridil, cisapride, clozapine, dihydroergotamine, ergotamine, encainide, flecainide, piroxicam, propafenon, clonidine, rifabutin, terfenadine). The drug reduces effectiveness of oral contraceptives, theophylline. It increases the AUC of saquinavir, indinavir, clarithromycin, trimethoprim, rifabutin and its metabolite. The medicine decreases AUC of zidovudine (26%), theophylline (45%), ethinyl estradiol (41%), sulfamethoxazole (20%). Lorazepam, flurazepam, diazepam, estazolam, midazolam, triazolam, zolpidem increase the risk of developing respiratory disorders, asthenia. Phenobarbital, carbamazepine, dexamethasone, phenytoin, rifampicin, rifabutin and smoking reduce the effectiveness of the drug. It is not recommended to carry out the simultaneous reception (in connection with a possible change in the concentration) of analgesics, antihistamines, antiarrhythmic and sedative drugs, antidepressants, antipsychotic drugs, CCBA.

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