Brand names: Kaletra®
Chemical formula:


Lopinavir; Ritonavir tablets
What are lopinavir; ritonavir tablets?
LOPINAVIR; RITONAVIR is an antiretroviral drug. It is used with other medicines to treat HIV. This medicine is not a cure for HIV. It will not stop the spread of HIV to others.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
diabetes mellitus or high blood sugar
hemophilia
high cholesterol levels
high triglyceride levels
liver disease, including hepatitis
an unusual or allergic reaction to lopinavir, ritonavir, other medicines, foods, dyes, or preservatives
breast-feeding
pregnancy or recent attempts to get pregnant
How should I take this medicine?
Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. You can take this medicine with or without food. Do not crush, break, or chew the tablets. Take your medicine at regular intervals. Do not take your medicine more often than directed. For your anti-HIV therapy to work as well as possible, take each dose exactly as prescribed. Do not skip doses or stop your medicine even if you feel better. Skipping doses may make the HIV virus resistant to this medicine and other medicines. Do not stop taking except on your doctor's advice.
Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.
What drug(s) may interact with lopinavir; ritonavir?
Many medicines may interact with lopinavir; ritonavir, if you have a question concerning other medicines you may be taking, talk with your pharmacist, prescriber or other health care professional.
Do not take lopinavir; ritonavir with any of these medicines:
alfuzosin (UroXatral®)
amiodarone (Cordarone®)
astemizole (Hismanal®)
bepridil (Vascor®)
cisapride (Propulsid®)
dofetilide (Tykosin®)
ergotamine medicines (Cafergot®, Migranal®, D.H.E. 45®, and others)
lovastatin (Mevacor®)
midazolam (Versed®)
pimozide (Orap®)
quinidine (Quinaglute®, Cardioquin®, Quinidex®, and others)
red yeast rice
simvastatin (Zocor®)
St. John's wort or products containing St. John's Wort
terfenadine (Seldane®)
triazolam (Halcion®)
zolpidem (Ambien®)
Other medicines that may interact with lopinavir; ritonavir:
atovaquone
birth control pills or other hormonal birth control medicines (like the patch, ring, or injections)
bosentan
certain medicines for anxiety or difficulty sleeping
certain medicines for fungal infections
certain medicines for high cholesterol (e.g., atorvastatin or cerivastatin)
certain medicines for high blood pressure
certain pain medicines
doxercalciferol
medicines for seizures
medicines for depression
medicines for diabetes
other antiviral medicines such as didanosine, ddI, saquinavir, or zidovudine
clarithromycin
cyclosporine
erythromycin
imatinib, STI-571
paricalcitol
rifabutin
rifampin
rifapentine
theophylline
sildenafil
warfarin
Tell your prescriber or health care professional about all other medicines you are taking, including nonprescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.
Tell your prescriber or health care professional about all other medicines you are taking, including nonprescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.
What should I watch for while taking lopinavir; ritonavir?
You must visit your prescriber or health care professional for regular checks on your progress. Lopinavir; ritonavir will not cure HIV infection, and you can still get other illnesses associated with HIV.
Lopinavir; ritonavir may cause abnormal liver function tests, changes in your cholesterol or triglyceride levels, and may increase the level of your blood sugar. Visit your health care professional or prescriber regularly to check for any of these side effects. Some of these effects may become serious.
Taking lopinavir; ritonavir does not reduce the risk of passing HIV infection to others through sexual or blood contact. It is best to avoid sexual contact so that you do not spread the disease to others. For any sexual contact, use a condom. Be careful about cuts, abrasions, and other possible sources of blood contact. Never share a needle or syringe with anyone.
If you are a woman of childbearing age and are using hormone contraceptives, then you should use another form of birth control while taking lopinavir; ritonavir. Lopinavir; ritonavir may decrease the effectiveness of hormone birth control agents, including birth control pills and injections. Do not breast-feed your infant if you have HIV.
What side effects might I notice from taking lopinavir; ritonavir?
Side effects that you should report to your prescriber or health care professional as soon as possible:
abdominal pain
increases in your blood sugar
redness, blistering, peeling or loosening of the skin, including inside the mouth
signs of a severe allergic reaction including difficulty breathing, tightness in throat, or swelling of your tongue
skin rash, hives
unusual tiredness or weakness
Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
abnormal bowel movements
changes in taste
changes in body fat
diarrhea
difficulty sleeping
dizziness
headache
heartburn
loss of appetite
nausea, vomiting
tingling or numbness in the hands or feet or around the mouth
tiredness or weakness
Where can I keep my medicine?
Keep out of the reach of children.
Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Keep in original container. Do not store this medicine outside the original container for longer than 2 weeks. Protect from moisture. Throw away any unused medicine after the expiration date.
Last updated: 11/14/2005 5:32:00 PM
Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.
| Systematic (IUPAC) name | |
|---|---|
| (2S)-N-[(2S,4S,5S)-5-[2-(2,6-dimethylphenoxy)acetamido]-4-hydroxy-1,6-diphenylhexan-2-yl]-3-methyl-2-(2-oxo-1,3-diazinan-1-yl)butanamide | |
| Clinical data | |
| AHFS/Drugs.com | International Drug Names |
| MedlinePlus | a602015 |
| Pregnancy cat. | C (US) |
| Legal status | POM (UK) ℞-only (US) |
| Routes | Oral |
| Pharmacokinetic data | |
| Bioavailability | Unknown |
| Protein binding | 98-99% |
| Metabolism | Hepatic |
| Half-life | 5 to 6 hours |
| Excretion | Mostly fecal |
| Identifiers | |
| CAS number | 192725-17-0 |
| ATC code | J05AE06 |
| PubChem | CID 92727 |
| DrugBank | DB01601 |
| ChemSpider | 83706 |
| UNII | 2494G1JF75 |
| KEGG | D01425 |
| ChEMBL | CHEMBL729 |
| Chemical data | |
| Formula | C37H48N4O5 |
| Mol. mass | 628.810 g/mol |
| SMILES | eMolecules & PubChem |
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Lopinavir (ABT-378) is an antiretroviral of the protease inhibitor class. It is used as a fixed-dose combination with another protease inhibitor, ritonavir, under the trade names Kaletra (high-income countries) and Aluvia (low-income countries).
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Contents
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Lopinavir is highly bound to plasma proteins (98–99%).[1]
There are contradictory reports regarding lopinavir penetration into the cerebrospinal fluid (CSF). Anecdotal reports state that lopinavir cannot be detected in the CSF; however, a study of paired CSF-plasma samples from 26 patients receiving lopinavir/ritonavir found lopinavir CSF levels above the IC50 in 77% of samples.[2]
Side effects, interactions and contraindications have only be evaluated in the drug combination lopinavir/ritonavir.
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