NEODOSE

INDICATIONS

FDA APPROVED INDICATION

Lopinavir/ritonavir is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in patients 14 days of age or older.

CONTRAINDICATIONS

• Concomitant use with the following alpha 1-adrenoreceptor antagonist: Alfuzosin
• Concomitant use with the following antianginal agent: Ranolazine
• Concomitant use with the following antiarrhythmic agent: Dronedarone
• Concomitant use with the following anti-gout agent: Colchicine
• Concomitant use with the following antimycobacterial agent: Rifampin
• Concomitant use with the following antipsychotics: Lurasidone, pimozide
• Concomitant use with the following ergot derivatives: Dihydroergotamine, ergotamine, methylergonovine
• Concomitant use with the following GI motility agent: Cisapride
• Concomitant use with the following hepatitis C direct-acting antiviral agent: Elbasvir/grazoprevir
• Concomitant use with the following herbal product: St. John’s wort (Hypericum perforatum)
• Concomitant use with the following HMG-CoA reductase inhibitors: Lovastatin, simvastatin
• Concomitant use with the following microsomal triglyceride transfer protein (MTTP)inhibitor: Lomitapide
• Concomitant use with the following phosphodiesterase type-5 (PDE5) inhibitor: Sildenafil (when used for the treatment of pulmonary arterial hypertension)
• Concomitant use with the following sedative/hypnotic agents: Triazolam, oral midazolam

PRECAUTIONS

• Cardiovascular:
  • Avoid use in patients with congenital long QT syndrome or hypokalemia, as QT interval prolongation and torsade de pointes have been reported.
  • PR interval prolongation and 2nd or 3rd degree atrioventricular block have been reported.
  • Underlying structural heart disease, conduction system abnormalities, ischemic heart disease, or cardiomyopathies; increased risk of conduction abnormalities.
• Concomitant Use:
  • Avoid once-daily use with carbamazepine, efavirenz, nevirapine, nelfinavir, phenobarbital, or phenytoin.
  • Avoid use with avanafil, boceprevir, rivaroxaban, salmeterol, simeprevir, tipranavir, amiodarone, or rifapentine.
  • Avoid use with fluticasone or other glucocorticoids, budesonide (systemic, inhaled, or intranasal), or prednisone unless benefit outweighs risk of systemic corticosteroid side effects.
  • Avoid use with QT interval-prolonging drugs.
  • Avoid use with voriconazole unless benefit outweighs risk of decreased voriconazole efficacy.
• Endocrine & Metabolic:
  • New onset diabetes mellitus, exacerbation of preexisting diabetes mellitus, hyperglycemia, and diabetic ketoacidosis have been reported with protease inhibitor use; consider monitoring for hyperglycemia and new onset or exacerbation of diabetes mellitus.
  • Large elevations of triglycerides and cholesterol have been reported; monitoring recommended.
• Gastrointestinal:
  • Pancreatitis has been reported, especially in patients with marked triglyceride elevations and in patients with a history of pancreatitis.
• Hematologic:
  • Hemophilia type A or B; increased bleeding (eg, skin hematomas, hemarthrosis) has been reported.
• Hepatic:
  • New or worsening of transaminase elevations or hepatic decompensation may occur in patients with hepatitis B or C or with marked transaminase elevation; monitoring recommended.
  • Hepatic dysfunction, including some fatalities, has been reported; monitoring recommended.
• Immunologic:
  • Autoimmune disorders (eg, Graves disease, polymyositis, Guillain-Barre syndrome) have been reported in the setting of immune reconstitution and may occur many months after initiation of therapy.
  • Immune reconstitution syndrome may occur, leading to an inflammatory response in patients with indolent or residual opportunistic infections.
• Preterm Neonates:
  • Use of the oral solution in preterm neonates in the immediate postnatal period is not recommended due to potential adverse effects caused by propylene glycol accumulation (complete AV block, bradycardia, cardiomyopathy, lactic acidosis, acute renal failure, CNS depression, and respiratory complications); if use is required, monitoring recommended.

ADVERSE EFFECTS

In a study of pediatric patients 6 months to 12 years of age (n=100), taste aversion (22%), vomiting (21%), and diarrhea (12%) were the most commonly reported events in patients treated for up to 48 weeks. Rash of moderate to severe intensity was reported in 3% of patients. Premature infants experience increased risk of toxicity, including life-threatening cardiotoxicity.

ADMINISTRATION

Administer with a feeding. Use a calibrated dosing syringe to administer the oral solution dose. If coadministered with didanosine, give didanosine 1 hour before or 2 hours after lopinavir/ritonavir dose. Oral solution not recommended for use with polyurethane feeding tubes due to ethanol and propylene glycol content and potential for incompatibility. Compatible feeding tubes include silicone and polyvinyl chloride (PVC).

MONITORING

Consider monitoring for hyperglycemia or new onset or worsening diabetes mellitus during treatment with lopinavir/ritonavir.