Lopinavir/ritonavir

What is Lopinavir/ritonavir?

• Lopinavir/ritonavir(Kaletra) is an HIV-1 protease inhibitor used with other antiretroviral agents for the treatment of HIV-1 infection.

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Lopinavir and ritonavir

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What are the uses of this medicine?

• KALETRA (Lopinavir/ritonavir) is a prescription anti-human immunodeficiency virus (HIV) medicine that contains two medicines: lopinavir and ritonavir. KALETRA is called a protease inhibitor that is used with other anti-HIV-1 medicines to treat people with HIV-1 infection. HIV-1 is the virus that causes AIDS (Acquired Immune Deficiency Syndrome).

How does this medicine work?

Lopinavir:

• Lopinavir is an antiviral drug.
• Lopinavir, an inhibitor of the HIV-1 protease, prevents cleavage of the Gag-Pol polyprotein, resulting in the production of immature, non-infectious viral particles.

Ritonavir:

• Ritonavir (ri toe' na vir) is peptidomimetic HIV protease inhibitor that acts by binding to the catalytic site of the viral protease, thereby preventing the cleavage of viral polyprotein precursors into mature, functional proteins that are necessary for viral replication.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• are allergy to KALETRA or any of its ingredients, including ritonavir and lopinavir.

are taking fallowing medicines:

• ergot containing medicines, including:
• ergotamine tartrate (Cafergot®, Migergot, Ergomar, Ergostat, Medihaler Ergotamine, Wigraine, Wigrettes)
• dihydroergotamine mesylate (D.H.E. 45®, Embolex, Migranal®)
• ergonovine, ergonovine and methylergonovine (Ergotrate, Methergine), ergotamine and methylergonovine
• Ergotrate Maleate, methylergonovine maleate (Methergine)
• triazolam (Halcion®), midazolam hydrochloride oral syrup
• pimozide (Orap®)
• the cholesterol lowering medicines lovastatin (Mevacor®) or simvastatin (Zocor®)
• sildenafil (Revatio®) only when used for the treatment of pulmonary arterial hypertension.
• alfuzosin (Uroxatral®)
• the herbal supplement St. John's Wort (hypericum perforatum)
• rifampin (Rimactane®, Rifadin®, Rifater®, or Rifamate®)

What drug interactions can this medicine cause?

• Medicines you should not take with KALETRA.

Serious problems or death can happen if you take these medicines with KALETRA: ergot containing medicines, including:

• ergotamine tartrate (Cafergot®, Migergot, Ergomar, Ergostat, Medihaler Ergotamine, Wigraine, Wigrettes)
• dihydroergotamine mesylate (D.H.E. 45®, Embolex, Migranal®)
• ergonovine, ergonovine and methylergonovine (Ergotrate, Methergine), ergotamine and methylergonovine
• Ergotrate Maleate, methylergonovine maleate (Methergine)
• triazolam (Halcion®), midazolam hydrochloride oral syrup
• pimozide (Orap®)
• the cholesterol lowering medicines lovastatin (Mevacor®) or simvastatin (Zocor®)
• sildenafil (Revatio®) only when used for the treatment of pulmonary arterial hypertension.
• alfuzosin (Uroxatral®)

Medicines that you should not take with KALETRA since they may make KALETRA not work as well: the herbal supplement St. John's Wort (hypericum perforatum) rifampin (Rimactane®, Rifadin®, Rifater®, or Rifamate®)

Medicines that may need changes:

• birth control pills that contain estrogen ("the pill") or the birth control (contraceptive) patches
• certain anticancer medicines, such as nilotinib (Tasigna®) and dasatinib (Sprycel®)
• certain cholesterol lowering medicines, such as atorvastatin (Lipitor®) or rosuvastatin (Crestor®)
• certain other antiretroviral medicines, such as efavirenz (Atripla® and Sustiva®), nevirapine (Viramune®), amprenavir (Agenerase®) and nelfinavir (Viracept®)
• anti-seizure medicines, such as phenytoin (Dilantin®) carbamazepine, (Tegretol®), phenobarbital
• medicines for erectile problems, such as sildenafil (Viagra®), tadalafil (Cialis®), or vardenafil (Levitra®)
• medicines for tuberculosis (TB), such as rifabutin (Mycobutin®)
• inhaled steroid medicines, such as fluticasone propionate (Flonase®)
• inhaled medicines such as salmeterol (Serevent®) or salmeterol in combination with fluticasone propionate (Advair®). Your doctor may need to change to a different medicine
• medicines for gout, such as colchicine (Colcrys®)
• medicines to treat pulmonary arterial hypertension (PAH), such as bosentan (Tracleer®) or tadalafil (Adcirca®)
• pain medicines, such as fentanyl (Duragesic®, IonsysTM, Fentora®) and methadone

Is this medicine FDA approved?

• Lopinavir/ritonavir as a single medication was approved for use in the United States in 2000.

How should this medicine be used?

Recommended dosage: Adult Patients:

• 400/100 mg (two 200/50 mg tablets or 5 mL oral solution) twice daily or
• 800/200 mg (four 200/50 mg tablets or 10 mL oral solution) once daily in patients with less than three lopinavir resistance-associated substitutions.

Pediatric Patients (ages 14 days and older):

• Twice daily dose is based on body weight or body surface area.
• KALETRA oral solution should not be administered to neonates before a postmenstrual age (first day of the mother’s last menstrual period to birth plus the time elapsed after birth) of 42 weeks and a postnatal age of at least 14 days has been attained.

Concomitant Therapy in Adults and Pediatric Patients:

• Dose adjustments of KALETRA may be needed when co-administering with efavirenz, nevirapine, amprenavir, or nelfinavir.

Administration:

• Swallow KALETRA tablets whole. Do not chew, break, or crush KALETRA tablets.
• KALETRA tablets can be taken with or without food.
• If you are taking both Videx® (didanosine) and KALETRA:
• didanosine can be taken at the same time as KALETRA tablets, without food.
• take didanosine either one hour before or two hours after taking KALETRA oral solution.
• Do not miss a dose of KALETRA. This could make the virus harder to treat. If you forget to take KALETRA, take the missed dose right away. If it is almost time for your next dose, do not take the missed dose. Instead, follow your regular dosing schedule by taking your next dose at its regular time. Do not take more than one dose of KALETRA at one time.
• If you take more than the prescribed dose of KALETRA, call your local poison control center or emergency room right away.
• Take KALETRA oral solution with food to help it work better.
• If KALETRA is being used for your child, tell your doctor if your child’s weight changes.
• KALETRA should not be given one time each day in children. When giving KALETRA to your child, give KALETRA exactly as prescribed.
• KALETRA oral solution contains propylene glycol and a large amount of alcohol. KALETRA oral solution should not be given to babies younger than 14 days of age unless your doctor thinks it is right for your baby.
• If a young child drinks more than the recommended dose, it could make them sick. Contact your local poison control center or emergency room right away.
• Talk with your doctor if you take or plan to take metronidazole or disulfiram. You can have severe nausea and vomiting if you take these medicines with KALETRA.
• When your KALETRA supply starts to run low, get more from your doctor or pharmacy. It is important not to run out of KALETRA. The amount of HIV-1 virus in your blood may increase if the medicine is stopped for even a short time. The virus may become resistant to KALETRA and become harder to treat.
• KALETRA can be taken with acid reducing agents used for heartburn or reflux such as omeprazole (Prilosec®) and ranitidine (Zantac®) with no dose adjustment.
• KALETRA should not be administered once daily in combination with carbamazepine (Tegretol® and Epitol®), phenobarbital (Luminal®), or phenytoin (Dilantin®).

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Film-coated tablets: 200 mg lopinavir and 50 mg ritonavir
• Film-coated tablets: 100 mg lopinavir and 25 mg ritonavir
• Oral solution: 80 mg lopinavir and 20 mg ritonavir per milliliter

This medicine is available in fallowing brand namesː KALETRA

What side effects can this medication cause?

The most common side effects of this medicine include:

• diarrhea
• nausea
• stomach area (abdominal) pain
• feeling weak
• vomiting
• headache
• upset stomach

KALETRA can cause serious side effects including:

• Changes in your heart rhythm and the electrical activity of your heart
• Interactions with other medicines
• Liver problems
• pancreatitis
• Increases in certain fat (triglycerides and cholesterol) levels in your blood
• hyperglycemia
• Changes in body fat
• Increased bleeding for hemophiliacs
• Allergic reactions

What special precautions should I follow?

• Higher plasma concentrations of concomitant medications may occur; consider drug-drug interaction potential to reduce risk of serious or life-threatening adverse reactions.
• KALETRA oral solution should not be used in preterm neonates in the immediate postnatal period because of possible toxicities. A safe and effective dose of KALETRA oral solution in this patient population has not been established.
• Pancreatitis has been observed in patients receiving KALETRA therapy, including those who developed marked triglyceride elevations. Fatalities have occurred; suspend therapy as clinically appropriate
• Patients with underlying hepatitis B or C or marked elevations in transaminase prior to treatment may be at increased risk for developing or worsening of transaminase elevations or hepatic decompensation with use of KALETRA. Fatalities have occurred. Monitor liver function before and during therapy, especially in patients with underlying hepatic disease, including hepatitis B and hepatitis C, or marked transaminase elevations.
• New onset diabetes mellitus, exacerbation of pre-existing diabetes mellitus, and hyperglycemia have been reported.
• PR interval prolongation may occur in some patients. Cases of second and third degree heart block have been reported. Use with caution in patients with pre-existing conduction system disease, ischemic heart disease, cardiomyopathy, underlying structural heart disease or when administering with other drugs that may prolong the PR interval.
• QT interval prolongation and isolated cases of torsade de pointes have been reported although causality could not be established. Avoid use in patients with congenital long QT syndrome, those with hypokalemia, and with other drugs that prolong the QT interval.
• Immune reconstitution syndrome has been reported in patients treated with combination antiretroviral therapy, including KALETRA.
• Redistribution/accumulation of body fat including central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, facial wasting, breast enlargement, and "cushingoid appearance" have been observed in patients receiving antiretroviral therapy.
• Treatment with KALETRA has resulted in large increases in the concentration of total cholesterol and triglycerides. Monitor prior to therapy and periodically thereafter.
• Increased bleeding, including spontaneous skin hematomas and hemarthrosis have been reported in patients with hemophilia type A and B treated with protease inhibitors. Additional factor VIII may be required.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• cardiogenic shock
• complete AV block
• cardiomyopathy
• lactic acidosis
• acute renal failure

Treatment of overdosage:

• Treatment of overdose with KALETRA should consist of general supportive measures including monitoring of vital signs and observation of the clinical status of the patient.
• There is no specific antidote for overdose with KALETRA.
• If indicated, elimination of unabsorbed drug should be achieved by gastric lavage.
• Administration of activated charcoal may also be used to aid in removal of unabsorbed drug.
• Since lopinavir is highly protein bound, dialysis is unlikely to be beneficial in significant removal of the drug.
• However, dialysis can remove both alcohol and propylene glycol in the case of overdose with KALETRA oral solution.

Can this medicine be used in pregnancy?

• There are, however, no adequate and well-controlled studies in pregnant women.
• KALETRA should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Can this medicine be used in children?

• The safety, efficacy, and pharmacokinetic profiles of KALETRA in pediatric patients below the age of 14 days have not been established.
• KALETRA once daily has not been evaluated in pediatric patients.

What are the active and inactive ingredients in this medicine?

Active ingredient: lopinavir and ritonavir

Inactive ingredients:

• KALETRA 200 mg lopinavir and 50 mg ritonavir tablets: copovidone, sorbitan monolaurate, colloidal silicon dioxide, and sodium stearyl fumarate. The film coating contains: hypromellose, titanium dioxide, polyethylene glycol 400, hydroxypropyl cellulose, talc, colloidal silicon dioxide, polyethylene glycol 3350, yellow ferric oxide 172, and polysorbate 80.

• KALETRA 100 mg lopinavir and 25 mg ritonavir tablets: copovidone, sorbitan monolaurate, colloidal silicon dioxide, and sodium stearyl fumarate. The film coating contains: polyvinyl alcohol, titanium dioxide, talc, polytheylene glycol 3350, and yellow ferric oxide E172.

• KALETRA oral solution: acesulfame potassium, alcohol, artificial cotton candy flavor, citric acid, glycerin, high fructose corn syrup, Magnasweet-110 flavor, menthol, natural and artificial vanilla flavor, peppermint oil, polyoxyl 40 hydrogenated castor oil, povidone, propylene glycol, saccharin sodium, sodium chloride, sodium citrate, and water.

Who manufactures and distributes this medicine?

• Manufactured by Abbott Pharmaceuticals PR Ltd., Barceloneta, PR

for Abbott Laboratories, North Chicago, IL USA

What should I know about storage and disposal of this medication?

• Store KALETRA oral solution in a refrigerator, between 36°F to 46°F (2°C to 8°C). KALETRA oral solution that is kept refrigerated may be used until the expiration date printed on the label.
• KALETRA oral solution that is stored at room temperature (less than 77°F or 25°C) should be used within 2 months.
• Keep KALETRA away from high heat.
• Throw away any medicine that is out of date or that you no longer need.

• Dailymed label info on Lopinavir/ritonavir
• FDA Lopinavir/ritonavir

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