LOPINAVIR/RITONAVIR

LOPINAVIR/RITONAVIR
(lop-i-na'ver/rit-o-na'ver)
Kaletra
Classifications: antiretroviral agent; protease inhibitor;
Therapeutic: antiretroviral agent
; protease inhibitor
Prototype: Saquinavir mesylate
Pregnancy Category: C

Availability

200 mg lopinavir/50 mg ritonavir tablets; 400 mg lopinavir/100 mg ritonavir/5 mL suspension

Action

Lopinavir, an HIV protease inhibitor that inhibits the activity of HIV protease and prevents the cleavage of viral polyproteins essential for the maturation of HIV. Ritonavir inhibits the CYP3A metabolism of lopinavir, thereby, increasing the blood level of lopinavir.

Therapeutic Effect

Decreases plasma HIV RNA level; reduces viral load as a result of the combined therapy of the two drugs in HIV infected patients.

Uses

Treatment of HIV infection in combination with other antiretroviral agents.

Contraindications

Hypersensitivity to lopinavir or ritonavir; concurrent administration with drugs that utilize CYP3A or CYP2D6 for metabolism (e.g., ergotamine, pimozide); pregnancy (category C), lactation. Safety and efficacy in children <6 mo are not established.

Cautious Use

Hepatic impairment, patients with hepatitis B or C, older adults; diabetes mellitus.

Route & Dosage

HIV Infection—Treatment Na?ve
Adult: PO 800/200 mg q.d.

HIV Infection—Treatment Experienced
Adult: PO 400/100 mg (3 capsules or 5 mL suspension) b.i.d., increase dose to 533/133 mg (4 capsules or 6.5 mL) b.i.d., with concurrent efavirenz or nevirapine
Child: PO 6 mo–12 y, 7–15 kg, 12/3 mg/kg; 15–40 kg, 10/2.5 mg/kg; >40 kg, 400/100 mg b.i.d., increase dose 7–15 kg, 13/3.25 mg/kg; 15–40 kg, 1?.75 mg/kg; >40 kg, 533/133 mg b.i.d., with concurrent efavirenz or nevirapine

Administration

Note: Take with food.

Oral
  • Give with a meal or light snack.
  • Note: If didanosine is concurrently ordered, give didanosine 1 h before or 2 h after lopinavir/ritonavir.
  • Store refrigerated at 2°–8° C (36°–46° F). If stored at room temperature ≤25° C (77° F), discard after 2 mo.

Adverse Effects (≥1%)

Body as a Whole: Asthenia, pain. GI: Abdominal pain, abnormal stools, diarrhea, nausea, vomiting. CNS: Headache, insomnia. Skin: Rash.

Interactions

Drug: Flecainide, propafenone, pimozide may lead to life-threatening arrhythmias; rifampin may decrease antiretroviral response; dihydroergotamine, ergonovine, ergotamine, methylergonovine may lead to acute ergot toxicity; hmg-coa reductase inhibitors may increase risk of myopathy and rhabdomyolysis; benzodiazepines may have prolonged sedation or respiratory depression; efavirenz, nevirapine, anticonvulsants, steroids may decrease lopinavir levels; delavirdine, ritonavir may increase lopinavir levels; may increase levels of amprenavir, indinavir, saquinavir, ketoconazole, itraconazole, midazolam, triazolam, rifabutin, sildenafil, atorvastatin, cerivastatin, immunosuppressants; may decrease levels of atovaquone, methadone, ethinyl estradiol. Also see INTERACTIONS in ritonavir monograph. Herbal: St. John's wort, garlic may decrease antiretroviral activity.

Pharmacokinetics

Absorption: Increased absorption when taken with food. Peak: 4 h. Distribution: 98–99% protein bound. Metabolism: Extensively metabolized by CYP3A. Elimination: Primarily in feces. Half-Life: 5–6 h lopinavir.

Nursing Implications

Assessment & Drug Effects

  • Monitor for S&S of: Pancreatitis, especially with marked triglyceride elevations; new onset diabetes or loss of glycemic control; hypothyroidism or Cushing's syndrome.
  • Lab test: Periodically monitor fasting blood glucose, AST & ALT, total cholesterol & triglycerides, serum amylase, inorganic phosphorus, CBC with differential, and thyroid functions.

Patient & Family

  • Report all prescription and nonprescription drugs being taken. Do not use herbal products, especially St. John's wort, without first consulting the physician.
  • Become familiar with the potential adverse effects of this drug; report those that are bothersome to physician.
  • Concurrent use of sildenafil (Viagra) increases risk for adverse effects such as hypotension, changes in vision, and sustained erection; promptly report any of these to the physician.
  • Use additional or alternative contraceptive measures if estrogen-based hormonal contraceptives are being used.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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