Adult Dosing

Treatment of HIV Infection (ONLY indicated in treatment experienced patients)

• 500 mg PO bid with ritonavir 200 mg PO bid

Pediatric Dosing

Treatment of HIV Infection (ONLY indicated in treatment experienced patients)

Child (2-18 yrs)

• 14 mg/kg (MAX: 500 mg/dose) PO bid with ritonavir 6 mg/kg (MAX: 200 mg/dose) PO bid
• Titrate: if intolerance develops, may reduce dose to 12 mg/kg PO bid with ritonavir 5 mg/kg PO bid

[Outline]

• Adult Dosing
• Pediatric Dosing

• Combination therapy with ritonavir in HIV-1 infection in treatment-experienced patients resistant to more than one protease inhibitor

• Hypersensitivity to any of the ingredients of the product
• Moderate or severe (Child-Pugh Class B or C) hepatic impairment
• Concomitant potent CYP 3A inducers
• Concomitant use with drugs highly dependent on CYP3A for clearance (eg, antiarrhythmic agents, antihistamines, cisapride, ergot derivative midazolam, pimozide, triazolam)

• Clinical hepatitis and hepatic decompensation, including some fatalities, reported in patients on tipranavir + ritonavir 200 mg; 2-fold increased risk if chronic HBV or HCV co-infection. Monitor for signs or symptoms of hepatitis, discontinue if asymptomatic elevations in AST or ALT >10 times ULN or asymptomatic elevations in AST or ALT between 5-10 times ULN with increases in total bilirubin >2.5 times the ULN occur. Use with caution in mild hepatic impairment
• Fatal and non-fatal intracranial hemorrhage reported in patients on tipranavir + ritonavir 200 mg; other medical conditions or medications may have caused or contributed to these events. No abnormal pattern of coagulation parameters has been observed, routine monitoring not recommended. Use with caution in patients at increased bleeding risk

Renal Dose Adjustment

• Renal impairment: No dose adjustments

Hepatic Dose Adjustment

• Mild hepatic impairment (Child-Pugh class A): Use with caution
• Moderate or severe hepatic impairment (Child-Pugh Class B or C): Contraindicated

• Risk of hepatotoxicity and intracranial hemorrhage [US Black Box Warning]
• Do not use in patients with pre-treatment liver enzymes levels >5 times the upper limit of normal
• Discontinue if AST/ALT 5-10 times ULN and total bilirubin >2.5 times ULN in asymptomatic patients or if signs/symptoms of clinical hepatitis
• Redistribution/accumulation of body fat including central obesity, dorsocervical fat enlargement, peripheral wasting with increased abdominal girth, and cushingoid appearance have occurred
• New-onset diabetes mellitus, exacerbation of preexisting diabetes, and hyperglycemia has occurred in patients receiving protease inhibitor therapy
• Immune reconstitution syndrome has occurred in patients treated with combination antiretroviral therapy
• Elevations in total cholesterol and triglycerides have been reported
• Rash, including urticarial, maculopapular, possible photosensitivity, and accompanied by joint pain or stiffness, throat tightness, or generalized pruritus, have been reported
• Tipranavir impairs platelet aggregation; increased bleeding events, including spontaneous skin hematomas and hemarthrosis have been reported in patients with hemophilia A and B treated with protease inhibitors
• Oral solution formulation contains vitamin E; additional vitamin E supplements should be avoided
• Monitor for spontaneous bleeding
• Monitor lipids, liver function (baseline and periodically)

Cautions: Use cautiously in

• Intracranial hemorrhage
• Chronic hepatitis B or C co-infection
• Increased bleeding risk (concomitant antiplatelets, anticoagulants, trauma, surgery)
• Diabetes mellitus
• Hepatitis
• Known sulfonamide allergy (contains sulfa moiety)
• Hemophilia
• Elderly patients

Aptivus interacts with :

	Apixaban
	Betrixaban (Bevyxxa)
	Dabigatran
	Digoxin
	Dolutegravir
	Edoxaban
	Eliquis
	Lanoxicaps
	Lanoxin
	Lanoxin pediatric
	Pradaxa
	Rivaroxaban
	Savaysa
	Tivicay
	Xarelto

Pregnancy Category:C

Breastfeeding: Unsafe, women with HIV infection should not breastfeed. Limited published experience with tipranavir during breastfeeding, an alternate drug may be preferred, especially while nursing a newborn or preterm infant. This information is based upon LactMed database (available at http://toxnet.nlm.nih.gov/cgi-bin/sis/htmlgen?LACT last accessed 1 September 2010)

• CNS Fatigue, headache, insomnia, dizziness, intracranial hemorrhage
• GI: Diarrhea, nausea, abdominal pain, vomiting, pancreatitis
• RESP: Dyspnea
• GU: Renal insufficiency
• DERM: Rash, photosensitivity
• HEMA: Anemia, neutropenia, thrombocytopenia
• HEPA: Hepatic failure, hepatitis, hepatotoxicity
• LABTESTS: Increased triglycerides, elevated liver transaminases, elevated amylase
• METABOLIC: Dehydration, diabetes mellitus, hyperlipidemia, weight decreased, fat redistribution
• MUSC: Myalgia
• MISC: Pyrexia, hypersensitivity, immune reconstitution syndrome, mitochondrial toxicity

• Protease inhibitor; prevents formation of mature virions by inhibiting virus-specific processing of the viral Gag and Gag-Pol polyproteins in HIV-1 infected cells
• Primarily metabolized by liver; CYP450: 3A4 inhibitor
• Renally excreted: 4.4%, feces 82.3% (80% unchanged)
• Half-life: 4.8-6 hrs

US Trade Name(s)

• Aptivus

US Availability

Aptivus

• CAPS: 250 mg
• ORAL SOLN: 100 mg/mL

Canadian Trade Name(s)

• Aptivus

Canadian Availability

Aptivus

• CAPS: 250 mg

UK Trade Name(s)

• Aptivus

UK Availability

Aptivus

• CAPS: 250 mg
• ORAL SOLN: 100 mg/mL

Australian Trade Name(s)

• Aptivus

Australian Availability

Aptivus

• CAPS: 250 mg
• ORAL SOLN: 100 mg/mL

[Outline]

Antimicrobials

Antiviral (HIV) Agents

Protease Inhibitors

Infectious Disease

Antiviral (HIV) Agents

Protease Inhibitors

Pricing data from www.DrugStore.com in U.S.A.

• Aptivus 250 MG CAPS [Bottle] (BOEHRINGER INGELHEIM)
  120 mg = $1138.02
  360 mg = $3366.83

Warning: This pricing information is subject to change at the sole discretion of DS Pharmacy. For the most current and up-to-date pricing information, please visit drugstore.com.

Drug Name: Aptivus 250 MG Oral Capsule

Ingredient(s): Tipranavir

Imprint: TPV;250

Color(s): Pink

Shape: Capsule

Size (mm): 22.00

Score: 1

Inactive Ingredient(s): alcohol / polyoxyl 35 castor oil / propylene glycol / caprylic/capric mono/diglycerides / gelatin

Drug Label Author:
Boehringer Ingelheim Pharmaceuticals, Inc.

DEA Schedule:
Non-Scheduled