Lopinavir & Ritonavir

Lopinavir/ritonavir is a prescription medication used in combination with other medications to treat human immunodeficiency virus (HIV) infection. 

Lopinavir/ritonavir contains 2 medications which belong to a group of drugs called protease inhibitors. These work by stopping the virus from replicating. Ritonavir helps to increase the amount of lopinavir in the body so that the medication will have a greater effect.

This medication comes in capsule, tablet, and oral liquid forms. It is usually taken once or twice daily.

Swallow lopinavir/ritonavir tablets whole.

Common side effects of lopinavir/ritonavir include diarrhea, nausea, and stomach pain.

Lopinavir/ritonavir is a prescription medication that contains two medicines, lopinavir and ritonavir. It is used in combination with other HIV medicines to treat human immunodeficiency virus (HIV) infection.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Lopinavir & Ritonavir may be found in some form under the following brand names:

• Kaletra

Lopinavir/ritonavir may cause serious side effects, including: 

• Interactions with other medicines. It is important to know the medicines that should not be taken with lopinavir/ritonavir. 
• Changes in your heart rhythm and the electrical activity of your heart. These changes may be seen on an EKG (electrocardiogram) and can lead to serious heart problems. Your risk for these problems may be higher if you:
  • already have a history of abnormal heart rhythm or other types of heart disease.
  • take other medicines that can affect your heart rhythm while you take lopinavir/ritonavir.

Tell your doctor right away if you have any of these symptoms while taking lopinavir/ritonavir:

• dizziness
• lightheadedness
• fainting
• sensation of abnormal heartbeats

Liver problems, including death, can happen in people who take lopinavir/ritonavir. Signs and symptoms of liver problems include:

• loss of appetite
• yellow skin and whites of eyes (jaundice)
• dark colored urine
• pale colored stools,
• itchy skin
• abdominal pain (stomach pain)

Lopinavir/ritonavir may cause pancreatitis (inflammation of the pancreas). Tell your doctor if you have nausea, vomiting, or abdominal pain (stomach pain) while taking lopinavir/ritonavir.

Large increases of triglycerides and cholesterol can be seen in blood tests of some people who take lopinavir/ritonavir.

Some people taking lopinavir/ritonavir get new or more serious diabetes or high blood sugar.

Changes in body fat have occurred in people taking lopinavir/ritonavir. 

Some people with hemophilia have increased bleeding while taking lopinavir/ritonavir.

Allergic reactions, including sometimes severe skin rashes, have occurred in people taking lopinavir/ritonavir.

Common side effects of lopinavir/ritonavir include:

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

Serious problems or death can happen if you take these medicines with lopinavir/ritonavir:

• 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 lopinavir/ritonavir since they may make lopinavir/ritonavir 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, Ionsys, Fentora) and methadone
• metronidazole or disulfiram. You can have severe nausea and vomiting if you take these medicines with lopinavir/ritonavir.

Lopinavir/ritonavir may cause serious side effects, including: 

• Interactions with other medicines. See "Drug Interactions" section.
• Changes in your heart rhythm and the electrical activity of your heart. These changes may be seen on an EKG (electrocardiogram) and can lead to serious heart problems. Your risk for these problems may be higher if you:
  • already have a history of abnormal heart rhythm or other types of heart disease.
  • take other medicines that can affect your heart rhythm while you take lopinavir/ritonavir.

Tell your doctor right away if you have any of these symptoms while taking lopinavir/ritonavir:

• dizziness
• lightheadedness
• fainting
• sensation of abnormal heartbeats

Do not take lopinavir/ritonavir if you are taking certain medicines. For more information about medicines you should not take with lopinavir/ritonavir, and consult with your doctor about all other medicines you take.

Do not take lopinavir/ritonavir if you have an allergy to lopinavir/ritonavir or any of its ingredients.

Medicines can interact with certain foods. In some cases, this may be harmful and your doctor may advise you to avoid certain foods. In the case of lopinavir/ritonavir there are no specific foods that you must exclude from your diet when receiving lopinavir/ritonavir.

Lopinavir/ritonavir may not be right for you. Tell your doctor about all your medical conditions, including if you:

• have any heart problems, including if you have a condition called Congenital Long QT Syndrome.
• have liver problems, including Hepatitis B or Hepatitis C.
• have diabetes.
• have hemophilia. People who take lopinavir/ritonavir may have increased bleeding.
• have low potassium in your blood.
• are pregnant or plan to become pregnant. 
• take lopinavir/ritonavir during pregnancy, talk with your doctor about how you can take part in an antiretroviral pregnancy registry. The purpose of the pregnancy registry is to follow the health of you and your baby.
• are breastfeeding. Do not breastfeed if you are taking lopinavir/ritonavir. You should not breastfeed if you have HIV-1. If you are a woman who has or will have a baby while taking lopinavir/ritonavir, talk with your doctor about the best way to feed your baby. If your baby does not already have HIV-1, there is a chance that HIV-1 can be passed to your baby through your breast milk.

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Many medicines interact with lopinavir/ritonavir. Do not start taking a new medicine without telling your doctor or pharmacist. Your doctor can tell you if it is safe to take lopinavir/ritonavir with other medicines. Your doctor may need to change the dose of other medicines while you take lopinavir/ritonavir.

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

Lopinavir/ritonavir falls into category C. It is not known if lopinavir/ritonavir will harm your unborn baby.

To monitor maternal-fetal outcomes of pregnant women exposed to lopinavir/ritonavir, an Antiretroviral Pregnancy Registry has been established. Patients can register by calling 1-800-258-4263.

Birth control pills or patches may not work as well while you take lopinavir/ritonavir. To prevent pregnancy while taking lopinavir/ritonavir, women who take birth control pills or use estrogen patch for birth control should either use a different type of birth control or an extra form of birth control. Talk to your doctor about how to prevent pregnancy while taking lopinavir/ritonavir.

Tell your doctor if you are breastfeeding or planning to breastfeed. You should not breastfeed if you are infected with HIV or if you are taking lopinavir/ritonavir.

• Take lopinavir/ritonavir every day exactly as prescribed by your doctor.
• It is very important to set up a dosing schedule and follow it every day. Do not miss a dose of lopinavir/ritonavir. This could make the virus harder to treat. If you forget to take lopinavir/ritonavir, 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 lopinavir/ritonavir at one time.
• Do not change your treatment or stop treatment without first talking with your doctor.
• Swallow lopinavir/ritonavir tablets whole. Do not chew, break, or crush lopinavir/ritonavir tablets.
• Lopinavir/ritonavir tablets can be taken with or without food.
• Take lopinavir/ritonavir oral solution and capsules with food to help it work better.
• If lopinavir/ritonavir is being used for your child, tell your doctor if your child’s weight changes.
• Lopinavir/ritonavir should not be given one time each day in children. When giving lopinavir/ritonavir to your child, give lopinavir/ritonavir exactly as prescribed.
• Lopinavir/ritonavir oral solution contains propylene glycol and a large amount of alcohol. lopinavir/ritonavir 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 lopinavir/ritonavir.
• When your lopinavir/ritonavir supply starts to run low, get more from your doctor or pharmacy. It is important not to run out of lopinavir/ritonavir. 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 lopinavir/ritonavir and become harder to treat.
• Lopinavir/ritonavir can be taken with acid reducing agents used for heartburn or reflux such as omeprazole (Prilosec) and ranitidine (Zantac ) with no dose adjustment.
• Lopinavir/ritonavir should not be administered once daily in combination with carbamazepine (Tegretol and Epitol), phenobarbital (Luminal), or phenytoin (Dilantin).

If you are taking both Videx (didanosine) and lopinavir/ritonavir:

• Didanosine can be taken at the same time as lopinavir/ritonavir tablets, without food.
• Take didanosine either one hour before or two hours after taking lopinavir/ritonavir oral solution.

Take lopinavir/ritonavir exactly as prescribed by your doctor. Follow the directions on your prescription label carefully. Your doctor will determine the best dosage for you. Tablets may be taken with or without food, swallowed whole and not chewed, broken, or crushed. Oral solution and capsules must be taken with food.

Recommended dosage for:

Adult Patients

• 400/100 mg (two 200/50 mg tablets, 3 capsules, or 5 mL oral solution) twice daily

• Lopinavir/ritonavir 400/100 mg (3 capsules or 5.0 mL) twice-daily taken with food.
• Lopinavir/ritonavir 800/200 mg (6 capsules or 10 mL) once-daily taken with food.
• Lopinavir/ritonavir 800/200 mg (10 mL) once-daily taken with food.
• Lopinavir/ritonavir 800/200 mg (four 200/50 mg tablets) once daily in patients with less than three lopinavir resistance-associated substitutions.

Once-daily administration of lopinavir/ritonavir is not recommended in therapy-experienced patients.

Administer 400/100 mg of lopinavir/ritonavir twice daily in pregnant patients with no documented lopinavir-associated resistance substitutions.  Once daily lopinavir/ritonavir dosing is not recommended in pregnancy.

• There are insufficient data to recommend dosing in pregnant women with any documented lopinavir-associated resistance   substitutions.
• No dosage adjustment of lopinavir/ritonavir is required for patients during the postpartum period.
• Pregnant women should not use lopinavir/ritonavir oral solution.

Pediatric patients (ages 14 days and older)

• Twice daily dose is based on body weight or body surface area.

Concomitant Therapy in Adults and Pediatric Patients 

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

Lopinavir/ritonavir 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 

If you have taken too much lopinavir/ritonavir call your local Poison Control Center or seek emergency medical treatment right away.

Lopinavir/ritonavir tablets:

• Store lopinavir/ritonavir tablets at room temperature, between 59°F to 86°F (15°C to 30°C).
• Do not keep lopinavir/ritonavir tablets out of the container it comes in for longer than 2 weeks, especially in areas where there is a lot of humidity. Keep the container closed tightly.

Lopinavir/ritonavir capsules:

• Store lopinavir/ritonavir capsules at room temperature, between 36°F - 46°F (2°C - 8°C) until dispensed.
• Avoid exposure to excessive heat.
• For patient use, refrigerated lopinavir/ritonavir capsules remain stable until the expiration date printed on the label. If stored at room temperature up to 77°F (25°C), capsules should be used within 2 months.

Lopinavir/ritonavir oral solution:

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