Indinavir (Sulphate)

Indinavir (Sulphate) is a protease inhibitor with antiretroviral activity. Indinavir (Sulphate) is used in combintion with other antiretroviral agents for the treatment of HIV infection and with advanced ae progressive immunedefiency.


Brands
Adult Dose
Dose: 800 mg
Single Dose: 800 (800)
Frequency: 8 hourly
Route: PO
Instructions:
Neonatal
Paedriatic
Dose: 500 mg/m2
Single Dose: 500 (500)
Frequency: 8 hourly
Route: PO
Instructions: child under 4 year safety not establish
Characteristics
Indinavir (Sulphate) also known as Sulfatoindinavir. . It is of Synthetic origin and belongs to Indanes, pherylpropylamine. . The Molecular Weight of Indinavir (Sulphate) is 711.90. Its pKa is 6.2.
Contraindications
Indinavir (Sulphate) is contraindicated in conditions like Diabetes mellitus,Haemophilia,Hypersensitivity.
Effects
The severe or irreversible adverse effects of Indinavir (Sulphate), which give rise to further complications include Nausea, Vomiting, Anorexia, Hyperglycemia, Diarrhea, Renal stones, Hyperglycemia, Renal insufficiency, Diabetes mellitus.Indinavir (Sulphate) produces potentially life-threatening effects which include Anemia, Thrombocytopenia, Bleeding, Anemia, Acute hemolytic anemia, Skin hematomas, Hemarthrosis, Hemarthrosis. which are responsible for the discontinuation of Indinavir (Sulphate) therapy.The symptomatic adverse reactions produced by Indinavir (Sulphate) are more or less tolerable and if they become severe, they can be treated symptomatically, these include Abdominal distension, Hematuria, Acute renal failure, Weight LossX, Liver dysfunction, Hyperpigmentation, Crystalluria, Hepatitis, Proteinuria, Nephrolithiasis including flank pain, Hepatic failure, Hypertriglyceridemia, Hyperbilirubinemia, Hypercholesterolemia.
Indications
Indinavir (Sulphate) is primarily indicated in conditions like AIDS, HIV infection, and can also be given in adjunctive therapy as an alternative drug of choice in Prophylaxis after occupational exposure to HIV.
Interactions
Indinavir (Sulphate) is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementAbacavirAbacavir possibly reduces plasma concentration of methadone.AmobarbitalBarbiturates possibly reduces plasma concentration of indinavir.MajorCarbamazepineCarbamazepine increases the plasma concentration of 9indinavir by induces its hepatic metabolismModerateAdjust the dose of indinavir if necessary. Closely monitor for antiretroviral responsesCisaprideIndinavir increases the plasma concentration of cisapride by inhibiting its metabolic clearence. Increased level of cisapide results in prolongation of QT interval on ECG, ventricular arrythmia, cardiac arrest and sudden death.MajorCoadministration should be avoided.Clorazepate (K)DexamethasoneDidanosineErgotamine (Tartrate)Co administration increases the plasma concentrations of ergot derivatives by inhibiting the enzyme responsible for metabolic clearance.MajorCo administration is considered contraindicated.ErlotinibThis CYP3A4 inhibitor increases levels/toxicity of erlotinibItraconazoleKetoconazoleketoconazole enhances the mean area under the plasma concentration-time curve of indinavir by 68% by inhibiting CYP450 3A4 hepatic metabolism.ModerateReduce the dose in case of liver disease. Closely monitor the adverse and therapeutic effects of indinavir.MethadoneMidazolamIndinavir increases the plasma concentration and pharmacological effect of midazolamby inhibiting intestinal and hepatic metabolism.MajorConcomitant use is considered contraindicated.NevirapinePhenobarbitonePhenytoin (Na)RifabutinSalmeterolConcurrent use may potentiate the risk of cardiovascular adverse events.SaquinavirSunitinibMay increases sunitinib concentrations.TerfenadineCo administration increases the plasma concentrations by inhibiting the enzyme responsible for metabolic clearance.MajorCo administration is considered contraindicated.Loratadine,Cetirizine or Fexofenadine may be the safer alternatives during therapy.VORICONAZOLEVoriconazole may increase the serum concentration of indinavir by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects Warfarin (Na)ZidovudineIndinavir enhances AUC of zidovudine upto 36%. During concomitant administration plasma concentration of indinavir is increased upto 13% by acting on its hepatic enzyme.MinorAdjust dose if necessary. Closely monitor the patient for toxicity of zidovudine. 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 cholesterolIncreased serum triglycerides
Risks
Drug should not be given to Paediatrics, Pregnant Mothers, patients suffering from Kidney dysfunction, patients suffering from Liver Malfunction, and Neonates.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
Caps Store at room temperature, Between 15°C-30°C. Protect from Moisture.
Warnings
Caution is required in diabetic patient, patients with hemophilia who may experienced increased bleeding . Indinavir should be used with caution and possible dose reduction is needed in hepatic impairment. Adequate hydration is recommended to avoid any risk of nephrolithiasis. Monitoring is required in case of renal impairment. Avoid in porphyrid hepatic impairment , Preexisting livered disease or chronic hepatitis B&C treatment may need to be stopped or temperature interupted in patient developing nephrolithasis cuation in a eating pateint with hemeophilis A&B as report of spotaneous Bleeding with use of HIV use of the HIV protease inhibitor
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