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November 22, 2009
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Medications and Drugs

GENERIC NAME: lopinavir and ritonavir

BRAND NAME: Kaletra

DRUG CLASS AND MECHANISM: Kaletra is an oral medication that is a combination of lopinavir and ritonavir. It is used for treating infections with the human immunodeficiency virus (HIV). It is in a class of drugs called protease inhibitors which also includes ritonavir (Norvir), nelfinavir (Viracept) and saquinavir (Invirase, Fortovase). Although both lopinavir and ritonavir inhibit the HIV virus, they are combined in Kaletra because ritonavir increases the concentration of lopinavir in the body. In fact, the activity of Kaletra against HIV is due to the lopinavir because the amount of ritonavir in Kaletra is not enough to inhibit the HIV virus. During infection with HIV, the HIV virus multiplies within the body's cells. Viruses are released from the cells and spread throughout the body where they infect other cells. In this manner, HIV infection is perpetuated among new cells that the body produces continually. During the production of the viruses, new proteins for the viruses are made. Some of the proteins are structural proteins, that, is, proteins that form the body of the virus. Other proteins are enzymes which manufacture DNA and other components for the new viruses. Protease is the enzyme that forms the new structural proteins and enzymes. The lopinavir in Kaletra blocks the action of protease and results in the formation of defective viruses that are unable to infect the body's cells. As a result, the number of viruses in the body (the viral load) decreases. Nevertheless, Kaletra does not prevent the transmission of HIV among individuals, and it does not cure HIV infections or AIDS. Kaletra was approved by the FDA in September, 2000.

GENERIC AVAILABLE: No

PRESCRIPTION: Yes

PREPARATIONS: Tablets:  100mg lopinavir and 25 mg ritonavir (100/25), 200 mg lopinavir and 50 mg ritonavir (200/50).  Oral solution:  80 mg lopinavir and 20 mg ritonavir per mL (80/20 mg/mL).

STORAGE: Capsules and solution should be refrigerated at 2-8°C (36-46°F). If stored at room temperature, the capsules and solution should be used within 2 months.

PRESCRIBED FOR: Kaletra is used for the treatment of HIV infection.

DOSING: Kaletra may be administered with or without food.

Therapy-naive adult patients: 200/50 tablets, two twice daily or four, once daily; Oral solution, 5 mL twice daily or 10 mL once daily with food.

Therapy-experienced adult patients:  (Once daily administration of Kaletra is not recommended.)  200/50 tablets, two twice daily; Oral solution 5 mL twice daily.

Children between 6 months and 18 years of age:  The recommended dose is 230/57.5 mg/m2 given twice daily and not to exceed the recommended adult dose..  Kaletra should not be administered once daily in patients less than 18 years of age.

In combination with efavirenz, nevirapine, (fos)amprenavir or nelfinavir:  Once daily administration is not recommended when combined with efavirenz, nevirapine, (fos)amprenavir or nelfinavir.  Adults:  Tablets, two 200/50 tablets and one 100/25 tablet twice daily; Oral solution, 6.5 mL twice daily.  For children the recommended dose is 300/75 mg/m2 not to exceed the adult dose. 

DRUG INTERACTIONS: Kaletra interacts with many drugs. Some of the important interactions are mentioned below. Viewers should consult their healthcare provider before combining any drug with Kaletra.

Kaletra should not be used together with amiodarone (Cordarone), quinidine (Quinaglute, Cardioquin), triazolam (Halcion), midazolam (Versed), pimozide (Orap), ergotamine derivatives (e.g. Ergostat), propafenone (Rythmol) and flecainide (Tambocor) because Kaletra increases the levels of these drugs in the body and as a result may lead to serious adverse effects of these drugs

Kaletra may also prevent the break down of lovastatin (Mevacor), simvastatin (Zocor), atorvastatin (Lipitor) and cerivastatin (Baycol) and cause their levels in the body to rise. This may increase the occurrence of muscle breakdown (rhabdomyolysis) a side effect of these drugs.

The blood concentration of rifabutin (Mycobutin) and sildenafil (Viagra) can be increased by Kaletra. Therefore, the doses of rifabutin and sildenafil should be reduced.

The oral solution contains alcohol, which causes severe side effects when combined with metronidazole (Flagyl) or disulfiram (Antabuse).




Report Problems to the Food and Drug Administration

 

You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.


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Suggested Reading by Our Doctors
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  • Drug Interactions - Learn about potential drug interactions you may be exposed to. Drug interactions can occur with prescription drugs, OTC medication, vitamins, herbs, and supplements.
  • Human Immunodeficiency Virus - Read about HIV (human immunodeficiency virus) causes, symptoms, signs, treatment, prevention, transmission, facts, testing, research (vaccine), statistics and AIDS (acquired immunodeficiency syndrome).
  • Drugs: What You Should Know About Your Drugs - Find out what you should know about your drugs such as side effects, warnings and precautions, storage information, and if a generic version is as good as the brand name.

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lopinavir and ritonavir, Kaletra

When was HIV discovered, and how is it diagnosed?

In 1981, homosexual men with symptoms of a disease that now are considered typical of the acquired immunodeficiency syndrome (AIDS) were first described in Los Angeles and New York. The men had an unusual type of lung infection (pneumonia) called Pneumocystis carinii (now known as Pneumocystis jiroveci) pneumonia (PCP) and rare skin tumors called Kaposi's sarcomas. The patients were noted to have a severe reduction in a type of cell in the blood that is an important part of the immune system, called CD4 cells. These cells, often referred to as CD4 T cells, help the body fight infections. Shortly thereafter, this disease was recognized throughout the United States, Western Europe, and Africa. In 1983, researchers in the United States and France described the virus that causes AIDS, now known as the human immunodeficiency virus (HIV) and belonging to the group of viruses called re...

Read the Human Immunodeficiency Virus article »










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