Kaletra Capsules

DRUG DESCRIPTION

KALETRA (lopinavir/ritonavir) is a co-formulation of lopinavir and ritonavir. Lopinavir is an inhibitor of the HIV protease. As co-formulated in KALETRA, ritonavir inhibits the CYP3A?­mediated metabolism of lopinavir, thereby providing increased plasma levels of lopinavir.

Lopinavir is chemically designated as [1S-[1R*,(R*), 3R*, 4R*]]-N-[4-[[(2,6?­dimethylphenoxy)acetyl]amino]-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl]tetrahydro?­alpha-(1-methylethyl)-2-oxo-1(2H)-pyrimidineacetamide. Its molecular formula is C37H48N4O5, and its molecular weight is 628.80. Lopinavir has the following structural formula:

Lopinavir Structural Formula Illustration

Ritonavir is chemically designated as 10-Hydroxy-2-methyl-5-(1-methylethyl)-1- [2-(1?­methylethyl)-4-thiazolyl]-3,6-dioxo-8,11-bis(phenylmethyl)-2,4,7,12-tetraazatridecan-13-oic acid, 5-thiazolylmethyl ester, [5S-(5R*,8R*,10R*,11R*)]. Its molecular formula is C37H48N6O5S2, and its molecular weight is 720.95. Ritonavir has the following structural formula:

  Proprietary name: Kaletra
  Established name: lopinavir and ritonavir
  Route of administration: ORAL (C38288)
  Active ingredients (moiety): Lopinavir (Lopinavir), Ritonavir (Ritonavir)
# Strength Form Inactive ingredients
1 133.3 MILLIGRAM,
33.3 MILLIGRAM
CAPSULE, LIQUID FILLED (C42954) FD&C Yellow No. 6, gelatin, glycerin, oleic acid, polyoxyl 35 castor oil, propylene glycol, sorbitol special, titanium dioxide, water
2 80 MILLIGRAM,
20 MILLIGRAM
SOLUTION (C42986) Acesulfame potassium, alcohol, artificial cotton candy flavor, citric acid ,glycerin, high fructose corn syrup, Magnasweet-110 flavor, menthol, natural & artificial vanilla flavor, peppermint oil, polyoxyl 40 hydrogenated castor oil, povidone, propylene glycol, saccharin sodium, sodium chloride, sodium citrate, water

Lopinavir is a white to light tan powder. It is freely soluble in methanol and ethanol, soluble in isopropanol and practically insoluble in water.

KALETRA capsules (lopinavir, ritonavir capsules) are available for oral administration in a strength of 133.3 mg lopinavir and 33.3 mg ritonavir with the following inactive ingredients: FD&C Yellow No. 6, gelatin, glycerin, oleic acid, polyoxyl 35 castor oil, propylene glycol, sorbitol special, titanium dioxide, and water.

KALETRA oral solution is available for oral administration as 80 mg lopinavir and 20 mg ritonavir per milliliter with the following inactive ingredients: Acesulfame potassium, alcohol, artificial cotton candy flavor, citric acid, glycerin, high fructose corn syrup, Magnasweet-110 flavor, menthol, natural & artificial vanilla flavor, peppermint oil, polyoxyl 40 hydrogenated castor oil, povidone, propylene glycol, saccharin sodium, sodium chloride, sodium citrate, and water.

KALETRA oral solution contains 42.4% alcohol (v/v).

What are the possible side effects of lopinavir and ritonavir (Kaletra)?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Stop taking ritonavir and call your doctor at once if you have any of these serious side effects:

  • fever, sore throat, and headache with a severe blistering, peeling, and red skin rash;
  • increased urination or extreme thirst;
  • easy bruising or bleeding;
  • signs of a new infection, such as fever or chills, cough, or flu...

Read All Potential Side Effects and See Pictures of Kaletra Capsules »

What are the precautions when taking lopinavir, ritonavir capsules (Kaletra Capsules)?

Before taking this product, tell your doctor or pharmacist if you are allergic to either lopinavir or ritonavir; or to other HIV protease inhibitors such as amprenavir, indinavir or saquinavir; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease, diabetes, pancreatitis, high blood fat levels (cholesterol/triglycerides), heart problems (coronary artery disease, heart attack), bleeding problems (e.g., hemophilia), previous infection with certain diseases (e.g., hepatitis B infection, hepatitis C infection, tuberculosis).

Lopinavir/ritonavir...

Read All Potential Precautions of Kaletra Capsules »


Kaletra Capsules Consumer (continued)

SIDE EFFECTS: Diarrhea, nausea, vomiting, stomach upset, gas, headache, and trouble sleeping may occur. If any of these effects persist or worsen, notify your doctor or pharmacist promptly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor immediately if any of these unlikely but serious side effects occur: joint/muscle pain, increased thirst, increased urination, blurred vision, confusion, persistent nausea/vomiting, severe stomach pain, yellowing of skin/eyes, dark urine, persistent fever, unusual tiredness.

Seek immediate medical attention if any of these rare but very serious side effects occur: symptoms of a heart attack (such as chest/jaw/left arm pain, shortness of breath, unusual sweating), severe dizziness, fainting, slow/fast/irregular heartbeat.

Changes in body fat may occur while you are taking this medication (e.g., increased fat in the upper back and stomach areas, decreased fat in the arms and legs). The cause and long-term effects of these changes are unknown. Discuss the risks and benefits of therapy with your doctor, as well as the possible role of exercise to reduce this side effect.

This medication may cause an increase in blood fat levels (cholesterol and triglycerides). Cholesterol and triglyceride testing should be done before and occasionally during treatment with this medication. Consult your doctor or pharmacist for more information.

A very serious allergic reaction to this drug is unlikely, but seek immediate medical attention if it occurs. Symptoms of a serious allergic reaction may include: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US -

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

PRECAUTIONS: Before taking this product, tell your doctor or pharmacist if you are allergic to either lopinavir or ritonavir; or to other HIV protease inhibitors such as amprenavir, indinavir or saquinavir; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease, diabetes, pancreatitis, high blood fat levels (cholesterol/triglycerides), heart problems (coronary artery disease, heart attack), bleeding problems (e.g., hemophilia), previous infection with certain diseases (e.g., hepatitis B infection, hepatitis C infection, tuberculosis).

Lopinavir/ritonavir may cause a condition that affects the heart rhythm (QT prolongation). QT prolongation can infrequently result in serious (rarely fatal) fast/irregular heartbeat and other symptoms (such as severe dizziness, fainting) that require immediate medical attention. The risk of QT prolongation may be increased if you have certain medical conditions or are taking other drugs that may affect the heart rhythm (see also Drug Interactions section). Before using lopinavir/ritonavir, tell your doctor or pharmacist if you have any of the following conditions: certain other heart problems (heart failure, slow heartbeat, QT prolongation in the EKG), family history of certain heart problems (QT prolongation in the EKG, sudden cardiac death).

Low levels of potassium or magnesium in the blood may also increase your risk of QT prolongation. This risk may increase if you use certain drugs (such as diuretics/"water pills") or if you have conditions such as severe sweating, diarrhea, or vomiting. Talk to your doctor about using lopinavir/ritonavir safely.

This medication should be used only when clearly needed during pregnancy. Discuss the risks and benefits with your doctor.

It is not known if this medication passes into breast milk. Because breast milk can transmit HIV, do not breast-feed.


Kaletra Capsules Patient Information Including Side Effects

Brand Names: Kaletra

Generic Name: lopinavir and ritonavir (Pronunciation: loe PIN a veer and ri TOE na veer)

  • What is lopinavir and ritonavir (Kaletra Capsules)?
  • What are the possible side effects of lopinavir and ritonavir (Kaletra Capsules)?
  • What is the most important information I should know about lopinavir and ritonavir (Kaletra Capsules)?
  • What should I discuss with my healthcare provider before taking lopinavir and ritonavir (Kaletra Capsules)?
  • How should I take lopinavir and ritonavir (Kaletra Capsules)?
  • What happens if I miss a dose (Kaletra Capsules)?
  • What happens if I overdose (Kaletra Capsules)?
  • What should I avoid while taking lopinavir and ritonavir (Kaletra Capsules)?
  • What other drugs will affect lopinavir and ritonavir (Kaletra Capsules)?
  • Where can I get more information?

What is lopinavir and ritonavir (Kaletra Capsules)?

Lopinavir and ritonavir is a combination of two antiviral medications in a group of HIV medicines called protease (PRO-tee-ayz) inhibitors. This medication prevents human immunodeficiency virus (HIV) cells from multiplying in your body.

Lopinavir and ritonavir is used to treat HIV, which causes acquired immunodeficiency syndrome (AIDS). Lopinavir and ritonavir is not a cure for HIV or AIDS.

Lopinavir and ritonavir may also be used for other purposes not listed in this medication guide.

What are the possible side effects of lopinavir and ritonavir (Kaletra Capsules)?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Stop taking ritonavir and call your doctor at once if you have any of these serious side effects:

  • fever, sore throat, and headache with a severe blistering, peeling, and red skin rash;
  • increased urination or extreme thirst;
  • easy bruising or bleeding;
  • signs of a new infection, such as fever or chills, cough, or flu symptoms;
  • severe pain in your upper stomach spreading to your back, nausea and vomiting, fast heart rate; or
  • low fever, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes).

Less serious side effects may include:

  • mild nausea, vomiting, diarrhea, stomach pain, bloating;
  • numbness or tingling, especially around your mouth;
  • mild skin rash;
  • headache, weakness, mood changes; or
  • changes in the shape or location of body fat (especially in your arms, legs, face, neck, breasts, and waist).

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What is the most important information I should know about lopinavir and ritonavir (Kaletra Capsules)?

Do not take lopinavir and ritonavir with lovastatin (Mevacor, Altocor), oral midazolam (Versed), pimozide (Orap), rifampin (Rifadin, Rimactane, Rifater), simvastatin (Zocor), St. John's wort, triazolam (Halcion), or an ergot medicine such as Ergomar, Cafergot, Wigraine, D.H.E. 45, Migranal, Methergine.

These drugs can cause life-threatening side effects if you use them while you are taking lopinavir and ritonavir.

There are many other medicines that can interact with lopinavir and ritonavir. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor. Keep a list with you of all the medicines you use and show this list to any doctor or other healthcare provider who treats you.

HIV/AIDS is usually treated with a combination of different drugs. To best treat your condition, use all of your medications as directed by your doctor. Do not change your doses or medication schedule without advice from your doctor. Every person with HIV or AIDS should remain under the care of a doctor.

Taking lopinavir and ritonavir will not prevent you from passing HIV to other people through unprotected sex or sharing of needles. Talk with your doctor about safe methods of preventing HIV transmission during sex, such as using a condom and spermicide. Sharing drug or medicine needles is never safe, even for a healthy person.

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