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All about: Lopinavir/Ritonavir

Big Image Pronouncation: (loe-PIN-a-vir/rit-OH-na-vir)
Class: Protease inhibitor combination

Trade Names:
Kaletra
- Capsules lopinavir 133.3 mg/ritonavir 33.3 mg
- Solution, oral lopinavir 80 mg/ritonavir 20 mg/mL

Mechanism of Action

Pharmacology

Lopinavir inhibits HIV protease, the enzyme required to form functional proteins in HIV-infected patients. Ritonavir inhibits the CYP-450 3A–mediated metabolism of lopinavir, increasing lopinavir plasma concentrations.

Indications and Usage

Treatment of HIV infection in combination with other antiviral agents.

Contraindications

Coadministration with drugs that are highly dependent on CYP3A for Cl and for which elevated plasma levels are associated with serious and/or life-threatening reactions (eg, astemizole, cisapride, conivaptan, dihydroergotamine, ergonovine, ergotamine, methylergonovine, midazolam, pimozide, ranolazine, sulfasalazine, terfenadine, triazolam); hypersensitivity to any of the ingredients.

Dosage and Administration

Therapy-Naive Patients
Adults

PO 400/100 mg twice daily or 800/200 mg once daily.

Therapy-Experienced Patients
Adults

PO 400/100 mg twice daily.

Concomitant Therapy
Adults

PO A dose increase in lopinavir/ritonavir to 533/133 mg twice daily with food is recommended when combined with amprenavir, efavirenz, nelfinavir, or nevirapine.

Children 6 mo to 12 yr of age

Dose based on lopinavir component of combination.

With Amprenavir, Efavirenz, or Nevirapine
  • Children weighing 7 to 14 kg: PO 13 mg/kg twice daily.
  • Children weighing 15 to 45 kg: PO 11 mg/kg twice daily.
  • Children weighing more than 45 kg: PO Adult dose.
Without Amprenavir, Efavirenz, or Nevirapine
  • Children weighing 7 to 14 kg: PO 12 mg/kg twice daily.
  • Children weighing 15 to 40 kg: PO 10 mg/kg twice daily.
  • Children weighing more than 40 kg: PO Adult dose.

General Advice

  • Lopinavir/ritonavir capsules and oral solution must be taken with food.
  • Once-daily administration of lopinavir/ritonavir is not recommended in therapy-experienced patients.
  • Do not administer lopinavir/ritonavir as a once-daily regimen in combination with amprenavir, efavirenz, nelfinavir, or nevirapine.
  • When possible, administer child dose using a calibrated dosing syringe.

Storage/Stability

Store capsules and oral solution at 36° to 46°F until dispensed. Avoid excessive heat.

Under refrigeration, capsules and oral solution are stable until the expiration date. If stored at 77°F, use within 2 mo.

Drug Interactions

Abacavir, amprenavir, atovaquone, lamotrigine, methadone, oral contraceptives, phenytoin, zidovudine

Levels of these agents may be reduced, decreasing the efficacy.

Antiarrhythmic agents (eg, amiodarone, bepridil, lidocaine [systemic], quinidine), antifungal agents (eg, itraconazole, ketoconazole), atorvastatin, buspirone, calcium channel blockers (eg, amlodipine, diltiazem, felodipine, nicardipine, nifedipine), cetirizine, clarithromycin, cyclosporine, dihydropyridine, fexofenadine, fluticasone, phosphodiesterase type 5 inhibitors (eg, sildenafil, tadalafil, vardenafil), protease inhibitors (eg, amprenavir, indinavir, nelfinavir, saquinavir), rifabutin, tacrolimus, tenofovir, trazodone

Levels of these agents may be elevated, increasing the pharmacologic and adverse reactions.

Astemizole, cisapride, conivaptan, ergot derivatives (eg, dihydroergotamine, ergonovine, ergotamine, methylergonovine), HMG-CoA reductase inhibitors (eg, lovastatin, simvastatin), midazolam, pimozide, ranolazine, rifampin, St. John's wort, sulfasalazine, terfenadine, triazolam

Contraindicated because of potentially serious or life-threatening reactions.

Carbamazepine, dexamethasone, NNRTIs (eg, efavirenz, nevirapine), phenobarbital, phenytoin, protease inhibitors (amprenavir, fosamprenavir, nelfinavir), rifampin

Lopinavir concentrations may be reduced, decreasing efficacy.

Delavirdine, ritonavir

Lopinavir concentrations may be elevated, increasing the pharmacologic and adverse reactions.

Didanosine

Because didanosine should be given on an empty stomach, and lopinavir/ritonavir capsules and oral solution should be taken with food, give didanosine 1 h before or 2 h after lopinavir/ritonavir capsules or oral solution.

Disulfiram/Metronidazole

A disulfiram-like reaction may occur when coadministered with the oral solution, which contains alcohol.

Warfarin

Because warfarin concentrations may be altered, monitor INR.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Atrial fibrillation, deep vein thrombosis, hypertension, palpitation, thrombophlebitis, varicose vein, vasculitis (less than 2%); bradyarrhythmias (postmarketing).

CNS

Asthenia, depression, headache, insomnia (at least 2%); abnormal dreams, abnormal thinking, agitation, amnesia, anxiety, apathy, ataxia, confusion, decreased libido, dizziness, dyskinesia, emotional lability, encephalopathy, facial paralysis, hypertonia, malaise, migraine, neuropathy, paresthesia, peripheral neuritis, seizure, somnolence, tremor (less than 2%).

Dermatologic

Rash (at least 2%); acne, alopecia, benign skin neoplasm, dry skin, eczema, exfoliative dermatitis, furunculosis, maculopapular rash, nail disorder, pruritus, seborrhea, skin discoloration, skin ulcer, sweating (less than 2%).

EENT

Abnormal vision, eye disorder, otitis media, taste perversion, tinnitus (less than 2%).

Endocrine

Cushing syndrome, diabetes mellitus, hypothyroidism (less than 2%).

GI

Abdominal pain, anorexia, diarrhea, dyspepsia, dysphagia, flatulence, nausea, vomiting (at least 2%); cholangitis, constipation, dry mouth, enlarged abdomen, enteritis, enterocolitis, eructation, esophagitis, fecal incontinence, gastritis, gastroenteritis, hemorrhagic colitis, increased appetite, mouth ulceration, pancreatitis, sialadenitis, stomatitis, ulcerative colitis (less than 2%).

Genitourinary

Abnormal ejaculation, gynecomastia, hypogonadism, kidney calculus, urine abnormality (less than 2%).

Hematologic-Lymphatic

Anemia, leukopenia, lymphadenopathy (less than 2%).

Hepatic

Cholecystitis, jaundice (less than 2%).

Lab Tests

ALT, amylase, AST, glucose elevated, glucose tolerance test, inorganic phosphorus and neutrophils decreased, total bilirubin, total cholesterol, triglycerides, uric acid (at least 2%).

Metabolic-Nutritional

Avitaminosis, decreased glucose tolerance, dehydration, edema, face edema, lactic acidosis, obesity, peripheral edema, weight gain, weight loss (less than 2%).

Musculoskeletal

Arthralgia, arthrosis, back pain, myalgia (less than 2%).

Respiratory

Bronchitis (at least 2%); asthma, dyspnea, lung edema, pharyngitis, rhinitis, sinusitis (less than 2%).

Miscellaneous

Chills, fever (at least 2%); allergic reaction, bacterial infection, chest pain (including substernal), cyst, flu syndrome, hypertrophy, viral infection (less than 2%); accumulation/redistribution of body fat (postmarketing).

Precautions

Monitor

Baseline tests

Assess serum transaminases, cholesterol, and triglyceride levels before starting therapy and periodically during therapy.

Blood sugar

Monitor blood sugar in diabetic patients when drug is started or dose is changed.

Fasting blood sugar

Assess fasting blood glucose before starting therapy and periodically thereafter during therapy in patient with risk factors for diabetes mellitus (eg, obesity, family history of diabetes).


Pregnancy

Category C .

Lactation

HIV-infected mothers should not breast-feed infants.

Children

Safety and efficacy not established in children younger than 6 mo of age.

Elderly

Select dose with caution, reflecting greater frequency of cardiac, hepatic, or renal function impairment, and of comorbidity.

Hepatic Function

Use with caution; decreased lopinavir/ritonavir Cl may occur.

Cross-resistance

Various degrees of cross-resistance among protease inhibitors have been observed.

Diabetes mellitus

New-onset diabetes mellitus, exacerbation of preexisting diabetes mellitus, and hyperglycemia have been reported.

Fat redistribution

Redistribution and accumulation of body fat has been observed.

Hemophilia

Increased bleeding, including spontaneous skin hematomas and hemarthrosis, has been reported in patients with hemophilia type A and B treated with protease inhibitors.

Immune reconstitution syndrome

Has been reported in patient receiving combination antiretroviral therapy, including lopinavir/ritonavir.

Lipid elevations

Large increases in total cholesterol and triglycerides have resulted with treatment.

Pancreatitis

Fatalities have been associated with use.

Overdosage

Symptoms

Alcohol-related toxicity caused by 42.4% alcohol content of oral solution.

Patient Information

  • Advise patient to review patient information leaflet before starting therapy and with each refill of the medication.
  • Review list of medications that must not be taken with lopinavir/ritonavir because of risk of very serious reactions.
  • Instruct patient to continue to take other HIV medications as prescribed by health care provider while taking this medication.
  • Advise patient taking didanosine to take didanosine 1 h before or 2 h after lopinavir/ritonavir.
  • Caution patient not to change the dose or stop taking any medications unless advised by health care provider.
  • Advise patient or caregiver to use measuring cup, dosing spoon, or syringe to measure prescribed dose of oral solution.
  • Advise patient to take capsules and oral solution with food to increase absorption and efficacy of the medication.
  • Advise patient that if a dose is missed, to take it as soon as possible and then return to the normal schedule. However, if it is almost time for the next dose, instruct patient to skip the missed dose and take the next dose at the regularly scheduled time. Instruct patient not to double the dose to catch up.
  • Instruct diabetic patient to monitor blood glucose more frequently when drug is started or dose is changed and to inform health care provider of significant changes in readings.
  • Instruct patient to report persistent abdominal pain, nausea, and vomiting, or frequent hunger, thirst, and urination to health care provider. Advise patient these symptoms could indicate a serious problem that will need medical care.
  • Inform patient that drug does not completely eliminate HIV virus and, therefore, does not reduce risk of transmitting HIV. Appropriate precautions must still be followed.
  • Advise patient that drug is not a cure for HIV infection and that illnesses associated with HIV infection, including opportunistic infections, may be acquired. Advise patient to remain under the care of health care provider.
  • Caution patient taking sildenafil, tadalafil, or vardenafil of increased risk of sildenafil-, tadalafil-, or vardenafil-induced adverse reactions (eg, low BP, sustained erection, visual changes) and to promptly report any symptoms to health care provider. Caution patient that an erection lasting longer than 4 h requires immediate medical help to prevent permanent damage to the penis.
  • Advise patient that the medication may cause changes in body fat distribution and to inform health care provider if noted.
  • Advise women using estrogen-based hormonal contraceptive to use additional or alternative nonhormonal contraceptive measures while taking this medication.
  • Advise HIV-infected mothers not to breast-feed infants to avoid risk of HIV transmission to the infant.

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