LOPINAVIR AND RITONAVIR (Systemic)

Some commonly used brand names are:

In the U.S.?

• Kaletra

In Canada?

• Kaletra

Category

• Antiviral, systemic

Description

The combination of lopinavir and ritonavir (low-PIN-a-veerand ri-TOE-na-veer) is used in the treatment of the infectioncaused by the human immunodeficiency virus (HIV). HIV is the virus responsiblefor acquired immune deficiency syndrome (AIDS). It is used to slow the progressionof disease in patients infected with HIV who have advanced symptoms, earlysymptoms, or no symptoms at all.

Lopinavir and ritonavir will not cure or prevent HIV infection or AIDS;however, it helps keep HIV from reproducing and appears to slow down the destructionof the immune system. This may help delay the development of problems usuallyrelated to AIDS or HIV disease. Lopinavir and ritonavir will not keep youfrom spreading HIV to other people. People who receive this medicine may continueto have other problems usually related to AIDS or HIV disease.

This medicine is available only with your doctor's prescription, in thefollowing dosage forms:

Oral
• Capsules (U.S. and Canada)
• Oral solution (U.S. and Canada)
• Tablets (U.S.)

Before Using This Medicine

In deciding to use a medicine, the risks of takingthe medicine must be weighed against the good it will do. This is a decisionyou and your doctor will make. For lopinavir and ritonavir, the followingshould be considered:

Allergies?Tell your doctor if you have ever had any unusualor allergic reaction to lopinavir or ritonavir. Also tell your health careprofessional if you are allergic to any other substances, such as foods, preservatives,or dyes.

Pregnancy?Lopinavir and ritonavir has not been studied inpregnant women. However, it has been found to cause birth defects and otherproblems in animals at doses many times the human dose. Before taking thismedicine, make sure your doctor knows if you are pregnant or if you may becomepregnant.

Breast-feeding?It is not known whether lopinavir and ritonavirpass into breast milk. However, because of the possibility that this medicinecould cause unwanted effects in nursing babies and the risk of passing HIVon to the infant, breast-feeding is usually not recommended.

Children?The twice-daily dose of this medicine has beentested in children 6 months of age and older and, in effective doses, hasnot been shown to cause different side effects or problems than it does inadults.

The once-daily dose of this medicine have been tested only in adult patientsand there is no specific information comparing use in children with use inother age groups.

Older adults?Many medicines have not been studied specificallyin older people. Therefore, it may not be known whether they work exactlythe same way they do in younger adults or if they cause different side effectsor problems in older people. There is no specific information comparing useof lopinavir and ritonavir in the elderly with use in other age groups.

Other medicines?Although certain medicines should not be used together at all, in other casestwo different medicines may be used together even if an interaction mightoccur. In these cases, your doctor may want to change the dose, or other precautionsmay be necessary. When you are taking lopinavir and ritonavir, it is especiallyimportant that your health care professional knows if you are taking any ofthe following:

• Amiodarone (e.g., Cordarone) or
• Bepridil (e.g., Vascor) or
• Quinidine (e.g., Quinidex)?Levels of these medicines in thebody may be increased and cause toxic effects to the heart.

• Amprenavir (e.g., Agenerase)?Amprenavir should not be usedwith the lopinavir and ritonavir once-daily dosing regimen

• Astemizole (e.g. Hismanal) or
• Cisapride (e.g., Propulsid) or
• Flecainide (e.g., Tambocor) or
• Pimozide (e.g., Orap) or
• Propafenone (e.g., Rythmol) or
• Terfenadine (e.g., Seldane)?These medicines should not be takenwith lopinavir and ritonavir due to the chance of serious heart rhythm problems.

• Atorvastatin (e.g., Lipitor) or
• Lovastatin (e.g., Mevacor) or
• Simvastatin (e.g., Zocor)?Simvastatin and lovastatin shouldnot be taken with lopinavir and ritonavir due to the risk of serious effectson muscle tissue; atorvastatin dose should be as low as possible to avoidadverse effects

• Carbamazepine (e.g., Tegretol) or
• Dexamethasone (e.g., Decadron) or
• Phenobarbital (e.g., Luminal) or
• Phenytoin (e.g., Dilantin)?These medicines may reduce the effectivenessof lopinavir and ritonavir by lowering the amount of lopinavir present inthe body. Carbamazepine, phenobarbital, and phenytoin should not be used withthe lopinavir and ritonavir once-daily dosing regimen.

• Clarithromycin (e.g., Biaxin)?Use of lopinavir and ritonavirmay increase the amount of clarithromycin in the body; patients with abnormalkidney function may need to have their dose adjusted

• Cyclosporine (e.g., Sandimmune, Neoral) or
• Felodipine (e.g., Plendil) or
• Nelfinavir (e.g., Viracept) or
• Nicardipine (e.g., Cardene) or
• Nifedipine (e.g., Procardia) or
• Sirolimus (e.g., Rapamune) or
• Tacrolimus (e.g., Prograf) or
• Trazodone (e.g., Desyrel)?Use of lopinavir and ritonavir mayincrease the amount of these medicines in the body, which may lead to increasedside effects. Nelfinavir should not be used with the lopinavir and ritonavironce-daily dosing regimen.

• Dihydroergotamine (e.g. D.H.E., Migranal) or
• Ergonovine (e.g., Ergotrate) or
• Ergotamine (e.g., Ergostat) or
• Methylergonovine (e.g., Methergine) or
• Midazolam (e.g., Versed) or
• Triazolam (e.g., Halcion)?These medicines should not be takenwith lopinavir and ritonavir because serious side effects could occur.

• Efavirenz (e.g., Sustiva) or
• Nevirapine (e.g., Viramune)?The dose of lopinavir and ritonavirmight need to be increased when taken with these medicines. Efavirenz andnevirapine should not be used with the lopinavir and ritonavir once-dailydosing regimen.

• Ethinyl estradiol?Lopinavir and ritonavir may cause this medicineto be less effective; therefore, alternative or additional birth control methodsshould be used when birth control pills containing ethinyl estradiol are takenwith lopinavir and ritonavir.

• Fluticasone, inhaled or nasal (e.g., Flonase, Flovent)?Lopinavirand ritonavir may increase the amount of this medicine in your body. Theyshould not be used together, if possible.

• Indinavir (e.g., Crixivan) or
• Saquinavir (e.g., Fortovase)?Lopinavir and ritonavir may decreasethe amount of these medicines in your body.

• Ketoconazole (e.g., Nizoral) or
• Itraconazole (e.g., Sporanox)?High doses are not recommendedwhen taken with lopinavir and ritonavir

• Rifabutin (e.g., Mycobutin)?Doses of this medicine should bedecreased and patients should be monitored more closely when this medicineis taken with lopinavir and ritonavir.

• Rifampin (e.g., Rifadin) or
• St. John's wort?Lopinavir and ritonavir may not work properlyif taken with these medicines.

• Sildenafil (e.g., Viagra) or
• Tadalafil (e.g., Cialis) or
• Vardenafil (e.g., Levitra)?Use of lopinavir and ritonavir mayincrease the amount of this medicine in the body, which may lead to increasedside effects; your doctor may decrease your dose of these medicines.

• Warfarin (e.g., Coumadin)?The amount of warfarin in the bloodmay be affected; bleeding times should be closely watched by your doctor.

Other medical problems?The presence of other medical problems may affect the use of lopinavirand ritonavir. Make sure you tell your doctor if you have any other medicalproblems, especially:

• Diabetes mellitus (sugar diabetes)?Lopinavir and ritonavirmay increase blood sugar; it may be necessary to adjust your dose of insulinor oral diabetes medicine.

• Hemophilia?Lopinavir and ritonavir may increase the risk ofmajor bleeding.

• Liver problems or
• Hepatitis B or
• Hepatitis C?Effects of lopinavir and ritonavir may be increasedbecause of slower removal of the medicines from the body.

• Pancreatitis (history of)?The chance that this condition willreturn is increased.

Proper Use of This Medicine

A paper with information about lopinavir and ritonavirwill be given to you with your filled prescription. Read this paper carefullyand ask your health care professional if you need additional information orexplanation.

It is important that lopinavir and ritonavir capsulesand oral solution be taken with food.

Lopinavir and ritonavir tablets may be taken with or without food.

For oral solution dosage form, use calibrated dosing syringe to measuredose.

For tablet dosage form, swallow whole and do not crush or chew.

Take this medicine exactly as directed by your doctor. Do not take it more often and do not take it for a longer time thanyour doctor ordered. Also, do not stop taking this medicine without checkingwith your doctor first.

Dosing?The doseof lopinavir and ritonavir will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of lopinavirand ritonavir. If your dose is different, do not changeit unless your doctor tells you to do so.

The number of capsules, tablets, or milliliters (mL) of lopinavir andritonavir that you take depends on the strength of the medicine.

• For oral dosage form (capsules):
  • For treatment of HIV infection:
    • Adults: 400 milligrams (mg) of lopinavir and 100 mg of ritonavir(3 capsules) twice a day with food or 800 mg of lopinavir and 200 mg of ritonavir(6 capsules) one time a day with food.
    • Children: This dosage form is usually not used for children. Pleaserefer to the oral solution dosage form.
• For oral dosage form (oral solution):
  • For treatment of HIV infection:
    • Adults and adolescents: 400 mg of lopinavir and 100 mg of ritonavir(5 milliliters [mL]) twice a day with food or 800 mg of lopinavir and 200mg of ritonavir (10 mL) one time a day with food.
    • Children 6 months to 12 years of age: Dose is based on body weightand must be determined by your doctor.
    • Children less than 6 months of age: Use and dose must be determinedby your doctor.
    • Use and dose must be determined by a doctor for all children receivingthe once-daily dose
• For oral dosage form (tablets):
  • For treatment of HIV infection:
    • Adults: 400 milligrams (mg) of lopinavir and 100 mg of ritonavir(2 tablets) twice a day with food or 800 mg of lopinavir and 200 mg of ritonavir(4 tablets) one time a day with or without food.
    • Children: This dosage form is usually not used for children. Pleaserefer to the oral solution dosage form.

Missed dose?If you miss a dose of this medicine, take itas soon as possible. However, if it is almost time for your next dose, skipthe missed dose and go back to your regular dosing schedule. Do not doubledoses.

Storage?To store this medicine:

• Keep out of the reach of children.
• Store in the refrigerator. However, keep the medicine from freezing.
• Avoid high heat.
• Do not keep outdated medicine or medicine no longer needed. Ask yourhealth care professional how you should dispose of any medicine you do notuse. Be sure that any discarded medicine is out of the reach of children.

Precautions While Using This Medicine

It is very important that yourdoctor check your progress at regular visits to make sure this medicineis working properly and to check for unwanted effects.

If you are taking the oral solution form of this medicine, you should limitthe amount of alcohol you drink. The oral solution contains 42% alcohol.

It is very important that you use a second type of birth control if youare currently using an estrogen-containing form of birth control

If you are taking sildenafil, tadalafil, or vardenafil, it is very importantto report any side effects, especially dizziness, fainting, or changes inyour vision

Side Effects of This Medicine

Along with its needed effects, a medicinemay cause some unwanted effects. Although not all of these side effects mayoccur, if they do occur they may need medical attention.

Less common

Bloating; blurred vision; chills ; constipation; darkened urine; dry mouth; fast heart beat; fatigue; fever; flushed, dry skin; fruit-like breath odor; increased hunger; increased thirst; increasedurination; indigestion; loss of appetite; loss of consciousness; nausea; pains in stomach, side, or abdomen,possibly moving to the back; sweating ; troubled breathing; unexplained weightloss; vomiting; yellow eyesor skin

Frequency not determined

Blistering, peeling, loosening of skin ; chest pain or discomfort; cough; diarrhea; itching ; jointor muscle pain; lightheadedness, dizziness or fainting; red irritated eyes; shortness of breath; slow or irregular heartbeat; sore throat; sores, ulcers,or white spots in mouth or on lips; ; unusual tiredness

Other sideeffects may occur that usually do not need medical attention. These side effectsmay go away during treatment as your body adjusts to the medicine. However,check with your doctor if any of the following side effects continue or arebothersome.

More common

Diarrhea

Less common

Abnormal stools; acid or sour stomach; belching; headache; heartburn; lack or loss of strength; pain; skin rash; stomach discomfort, upset, or pain; trouble in sleeping

Other side effects may occur that do not require medicalattention.

Frequency not determined

Other side effects not listed above may also occur in some patients. If younotice any other effects, check with your doctor.