Lopinavir and Ritonavir (Oral)

By preventing the multiplication of the HIV virus, lopinavir and ritonavir strengthens the immune system and helps delay the development of opportunistic infections associated with AIDS or HIV disease.

Overview

Lopinavir and ritonavir is a combination medication used to treat infections caused by the human immunodeficiency virus (HIV). HIV is the virus that causes acquired immune deficiency syndrome (AIDS). This medication is used to slow the progression of the disease in HIV positive patients who exhibit early symptoms, advanced symptoms, or no symptoms at all.

Sold under the brand name Kaletra, lopinavir and ritonavir belongs to a class of medications called protease inhibitors which, among others, includes nelfinavir, ritonavir, and saquinavir. When the HIV virus affects the cell, it takes control of that cell, forcing it to generate multiple copies of the virus. To generate these copies, the cell uses an enzyme called protease. Lopinavir and ritonavir works by inhibiting the activity of protease enzyme, which is used by HIV infected cells to generate new viruses. This way, the medication reduces or inhibits the activity of protease, hence the name œprotease inhibitor.

The purpose of small doses of ritonavir in Kaletra is to boost the levels of lopinavir in the blood. In addition, ritonavir also helps ensure that lopinavir levels in the blood are high for several hours after medication. This is why this medication can be taken once or twice per day. Lopinavir and ritonavir is available only with the healthcare provider's prescription and comes in the following dosage forms:

  • Tablet
  • Solution
  • Liquid filled capsule

Conditions treated

lopinavir and ritonavir

  • Infection caused by human immunodeficiency virus (HIV)

Type Of Medicine

  • Antiretroviral Agent

Side effects of lopinavir and ritonavir

Along with its intended effects, lopinavir and ritonavir may cause some unwanted side effects. Some side effects are not life-threatening and will often go away as the body gets used to the medication. In addition, your healthcare provider will advise you on how to manage these side effects and reduce their severity. However, other side effects tend to be severe and may require medical attention. Check with your healthcare immediately when you experience the following lopinavir and ritonavir side effects.

  • Bloating
  • Chills
  • Blurred vision
  • Darkened urine
  • Constipation
  • Dry mouth
  • Fruit-like breath odor
  • Fever
  • Fast heartbeat
  • Flushed, dry skin
  • Increased thirst
  • Increased hunger
  • Indigestion
  • Increased urination
  • Loss of consciousness
  • Loss of appetite
  • Nausea
  • Profuse sweating
  • Pain in the abdomen, side, or back
  • Breathing difficulty
  • Weight loss
  • Vomiting
  • Yellowing of the skin and eyes
  • Chest pain and discomfort
  • Blistering, peeling, or loosening of the skin
  • Itching
  • Cough
  • Diarrhea
  • Joint and muscle pain
  • Red, irritated eyes
  • Lightheadedness, dizziness, or fainting
  • Sore throat
  • Unusual tiredness or general body weakness
  • Sores, ulcers, or white spots on the lips and around the mouth

Seek emergency help immediately if you experience any of the following symptoms of lopinavir and ritonavir overdose:

  • Confusion
  • Agitation
  • Cool, sweaty skin
  • Decreased responsiveness or awareness
  • Reduced appetite
  • Reduced urine output
  • Depression
  • Persistent headache
  • Irritability
  • Fast, irregular and pounding heartbeat
  • General feeling of discomfort
  • Fast, shallow breathing
  • Muscle pain and cramping
  • Seizures
  • Rapid weight gain
  • Rapid heartbeat
  • Stomach discomfort
  • Severe sleepiness
  • Swelling of the feet and ankles
  • Unusual drowsiness, tiredness, dullness, weakness, or feeling of sluggishness
  • Swelling of the face, hands, and ankles

Some lopinavir and ritonavir side effects occur that do not require medical attention. These side effects tend to go away as the body adjusts to treatment. Also, your healthcare provider may be able to advise you how on how to reduce or manage these side effects. However, you may check with your healthcare provider if any of the following side effects persist or become bothersome if you have questions about them:

  • Constant belching
  • Abnormal bowel movement
  • Heartburn
  • Lack or loss of strength
  • Skin rashes
  • Pain
  • Trouble with sleeping
  • Redistribution of body fat

Call your healthcare provider for advice about these side effects. You may also report the side effects to the FDA at 1-800-FDA-1088.

Lopinavir and ritonavir dosage

It is important that you take lopinavir and ritonavir exactly as directed by your healthcare provider. Do not change the dosage or stop taking this medication without first checking with your healthcare provider. Contact your pharmacist or healthcare provider ahead of time when your lopinavir and ritonavir supply is running low.

Lopinavir and ritonavir comes with a Medication Guide. Be sure to read and understand the instructions therein before starting your medication and each time you go for a refill. Ask your healthcare provider or pharmacist if you have any questions.

Lopinavir and ritonavir works well when there is a constant amount of medication in the blood. To help maintain the right levels of medication in your blood, ensure that you take your medication as scheduled without fail. Your nurse or doctor may help you plan the best dosing schedule.

Lopinavir and ritonavir should be taken in combination with other medications that are used to treat HIV. It is important that you take all the medications prescribed by your healthcare provider at the right time of day, and in the correct order. Do not stop taking this medication unless advised to do so by your healthcare provider.

It is important that you take lopinavir and ritonavir with food. If you are taking the tablet form of this medication, do not crush or chew the medicine. Swallow them whole.

Dosing schedule

Lopinavir and ritonavir dosing varies from patient to patient. Follow your healthcare provider's prescription or the directions on the drug's label. The following is only the average dosing information for lopinavir and ritonavir. If your healthcare provider has recommended a different dose, do not change it unless with their approval.

The amount of medication you take also depends on the strength of the medication, the number of daily doses, and the time recommended in between the doses.

Dosing for treating HIV infection

Oral dosing form ' solution

Adult dosage' Take 400 mg of lopinavir and 100 mg of ritonavir orally two times per day with food, or 800 mg of lopinavir and 200 mg of ritonavir once per day with food. Your healthcare provider may adjust the dosage if there is need.

Children (6 months and older) dosage ' the dosage is based on body weight or body size and must be determined by your child's healthcare provider. The recommended dosage is 10 mg to 12 mg of lopinavir and 2.5 mg to 3 mg of ritonavir per kilogram of body weight. The medication should be administered once per day with food. The doctor may adjust dosage as necessary.

Children (14 days to 6 months old) dosage ' The dosage is based on the child's body weight or body size and must be determined by the child's healthcare provider. The recommended dosage is 16 mg of lopinavir and 4 mg ritonavir per kilogram of body weight administered twice per day with food.

Children younger than 14 days '“ the use of lopinavir and ritonavir is not recommended unless the doctor determines that it is safe to be given.

Tablet forms

Adult dosage' 400 mg of lopinavir and 100 mg of ritonavir taken twice per day, or 800 mg of lopinavir and 200 mg of ritonavir taken once per day. The dosage can be adjusted as needed.

Children 6 months and older' It is important that the patient swallows the medicine whole. The dosage is based on the child's body weight and must be determined by the child's healthcare provider. Average dosing is 200 mg to 400 mg of lopinavir and 50 mg to 100 mg ritonavir administered twice per day. The doctor may recommend adjustment of the dosage as necessary.

Children 14 days to 6 months old ' this dosage form is not recommended for infants.

Overdose

If there is lopinavir and ritonavir overdose, with serious symptoms like passing out or breathing difficulty, call the emergency room immediately. You may also report lopinavir and ritonavir overdose to the poison control center at 1-800-222-1222. Some of the symptoms of lopinavir and ritonavir overdose include change in the amount of urine and numbness or tingling in the hands, arms, legs and ankles.

Missed dose

If you have missed your lopinavir and ritonavir dosage, take it as soon as you remember. However, if it is almost time for your next dose, skip the missed dose and resume your regular dosing schedule. Do not make up for the missed dose by double dosing.

Important notes on dosing

Do not share this medication with other HIV positive patients.

Keep all your medical as well as laboratory appointments. It is important that you are tested for the following on a regular basis: liver function, blood cholesterol, blood sugar, or blood triglyceride levels, and blood count.

Lopinavir and ritonavir comes in capsular, tablets, and oral solution forms. Never switch types of this medication without approval from your healthcare provider.

Lopinavir and ritonavir interactions

Although certain medications should not be used in combination, in other cases two or more medications may be combined even if an interaction might occur. In such cases, your healthcare provider may recommend a change of dosage for one of the medications or recommend appropriate precautions. Tell your healthcare provider about the medications you are currently taking, including over-the-counter medications, supplements, and herbal drugs, before using lopinavir and ritonavir.

  • Efavirenz
  • Elbasvir
  • Eletriptan
  • Encainide
  • Isavuconazonium Sulfate
  • Ivabradine
  • Ketoconazole
  • Lomitapide
  • Lovastatin
  • Lurasidone
  • Primidone
  • Propafenone
  • Sildenafil
  • Silodosin
  • Maraviroc
  • Mesoridazine
  • Methylergonovine
  • Phenytoin
  • Pimozide
  • Piperaquine
  • Posaconazole
  • Ethinyl Estradiol
  • Everolimus
  • Flecainide
  • Flibanserin
  • Fluconazole
  • Eplerenone
  • Ergoloid Mesylates
  • Ergonovine
  • Ergotamine
  • Fosphenytoin
  • Grazoprevir
  • Conivaptan
  • Crizotinib
  • Dihydroergotamine
  • Doxorubicin
  • Bepridil
  • Carbamazepine
  • Cisapride
  • Colchicine
  • Doxorubicin Hydrochloride Liposome
  • Dronedarone
  • Alfuzosin
  • Amifampridine
  • Amiodarone
  • Amisulpride
  • Astemizole
  • Atorvastatin
  • Simvastatin
  • Sirolimus
  • Quinidine
  • Ranolazine
  • Rifampin
  • Riociguat
  • Naloxegol
  • Nelfinavir
  • Nimodipine
  • Phenobarbital
  • Romidepsin
  • Methysergide
  • Midazolam
  • Sparfloxacin
  • Venetoclax
  • Voriconazole
  • Ziprasidone
  • St John's Wort
  • Tacrolimus
  • Terfenadine
  • Thioridazine
  • Tolvaptan
  • Triazolam

Combining lopinavir or ritonavir with any of the following medications is usually not recommended but may be necessary in some cases. Should both medications be prescribed together, your healthcare provider may change the dosage or how you use the drugs.

  • Acalabrutinib
  • Amiodarone
  • Amitriptyline
  • Amoxapine
  • Anagrelide
  • Arsenic Trioxide
  • Artemether
  • Asenapine
  • Atorvastatin
  • Atovaquone
  • Azithromycin
  • Bedaquiline
  • Bepridil
  • Betrixaban
  • Axitinib
  • Boceprevir
  • Bosentan
  • Bosutinib
  • Brexpiprazole
  • Ceritinib
  • Chloroquine
  • Chlorpromazine
  • Codeine
  • Copanlisib
  • Cyclophosphamide
  • Cyclosporine
  • Ado-Trastuzumab Emtansine
  • Afatinib
  • Apixaban
  • Buprenorphine
  • Bupropion
  • Buserelin
  • Cabazitaxel
  • Cabozantinib
  • Calcifediol
  • Carbamazepine
  • Cariprazine
  • Cilostazol
  • Ciprofloxacin
  • Citalopram
  • Dabrafenib
  • Daclatasvir
  • Darunavir
  • Dasatinib
  • Deferasirox
  • Deflazacort
  • Degarelix
  • Delamanid
  • Desipramine
  • Deslorelin
  • Droperidol
  • Eluxadoline
  • Enzalutamide
  • Erlotinib
  • Everolimus
  • Fosaprepitant
  • Foscarnet
  • Fosphenytoin
  • Fusidic Acid
  • Ifosfamide
  • Iloperidone
  • Inotuzumab Ozogamicin
  • Irinotecan
  • Irinotecan Liposome
  • Ibutilide
  • Idelalisib
  • Lapatinib
  • Leuprolide
  • Levofloxacin
  • Levomilnacipran
  • Apomorphine
  • Aprepitant
  • Aripiprazole
  • Aripiprazole Lauroxil
  • Avanafil
  • Brigatinib
  • Bromocriptine
  • Budesonide
  • Clarithromycin
  • Clomipramine
  • Clozapine
  • Cobicistat
  • Cobimetinib
  • Dabigatran Etexilate
  • Deutetrabenazine
  • Dexamethasone
  • Doxorubicin Hydrochloride Liposome
  • Methylenedioxymethamphetamine
  • Erythromycin
  • Escitalopram
  • Eszopiclone
  • Etravirine
  • Fentanyl
  • Fingolimod
  • Fluconazole
  • Fluoxetine
  • Fluticasone
  • Haloperidol
  • Hemin
  • Histrelin
  • Hydrocodone
  • Hydroxychloroquine
  • Isavuconazonium Sulfate
  • Ivacaftor
  • Ixabepilone
  • Ketoconazole
  • Lacosamide
  • Lamotrigine
  • Lumacaftor
  • Lumefantrine
  • Macimorelin
  • Macitentan
  • Manidipine
  • Mefloquine
  • Piperaquine
  • Pitolisant
  • Pixantrone
  • Ponatinib
  • Temsirolimus
  • Tetrabenazine
  • Thiotepa
  • Ticagrelor
  • Promethazine
  • Propafenone
  • Protriptyline
  • Quetiapine
  • Quinidine
  • Tipranavir
  • Triamcinolone
  • Trifluoperazine
  • Trimipramine
  • Triptorelin
  • Rifabutin
  • Rifapentine
  • Rivaroxaban
  • Rosuvastatin
  • Ribociclib
  • Ruxolitinib
  • Salmeterol
  • Saquinavir
  • Sertraline
  • Sevoflurane
  • Omeprazole
  • Ondansetron
  • Orlistat
  • Oxycodone
  • Procainamide
  • Quinine
  • Reboxetine
  • Regorafenib
  • Retapamulin
  • Vinblastine
  • Vincristine
  • Vincristine Sulfate Liposome
  • Digoxin
  • Docetaxel
  • Dofetilide
  • Dolasetron
  • Domperidone
  • Donepezil
  • Doxorubicin
  • Garlic
  • Gatifloxacin
  • Gemifloxacin
  • Glecaprevir
  • Gonadorelin
  • Goserelin
  • Granisetron
  • Halofantrine
  • Hydroxyzine
  • Ibrutinib
  • Lidocaine
  • Metformin
  • Methadone
  • Metronidazole
  • Midostaurin
  • Mifepristone
  • Morphine
  • Morphine Sulfate Liposome
  • Norfloxacin
  • Nortriptyline
  • Octreotide
  • Ofloxacin
  • Olaparib
  • Palbociclib
  • Paliperidone
  • Panobinostat
  • Paritaprevir
  • Pasireotide
  • Pazopanib
  • Phenobarbital
  • Phenytoin
  • Pibrentasvir
  • Pimavanserin
  • Posaconazole
  • Pravastatin
  • Prednisolone
  • Prednisone
  • Solifenacin
  • Sonidegib
  • Sorafenib
  • Tadalafil
  • Tamoxifen
  • Tamsulosin
  • Telaprevir
  • Telavancin
  • Telithromycin
  • Valbenazine
  • Vandetanib
  • Vardenafil
  • Vemurafenib
  • Voriconazole
  • Voxilaprevir
  • Zolpidem
  • Zuclopenthixol
  • Vinflunine
  • Vorapaxar
  • Topotecan
  • Toremifene
  • Trabectedin
  • Trazodone
  • Moxifloxacin
  • Nafarelin
  • Venlafaxine
  • Vilanterol
  • Vilazodone
  • Sotalol
  • Sulpiride
  • Sunitinib
  • Suvorexant
  • Simeprevir
  • Neratinib
  • Netupitant
  • Nifedipine
  • Nilotinib
  • Sodium Phosphate
  • Sodium Phosphate, Dibasic
  • Sodium Phosphate, Monobasic

Combining lopinavir and ritonavir with any of the following medications may increase the risk of certain side effects. However, both drugs may be the best treatment combination for you. If both medications are prescribed together, your healthcare provider may recommend a change in the dosage or the frequency of using one or both medications.

  • Acenocoumarol
  • Amitriptyline
  • Amprenavir
  • Aripiprazole Lauroxil
  • Delavirdine
  • Desipramine
  • Desogestrel
  • Dutasteride
  • Efavirenz
  • Estradiol Cypionate
  • Estradiol Valerate
  • Ethynodiol Diacetate
  • Eltrombopag
  • Etonogestrel
  • Fosamprenavir
  • Gemfibrozil
  • Levothyroxine
  • Medroxyprogesterone Acetate
  • Meperidine
  • Mestranol
  • Methamphetamine
  • Mexiletine
  • Didanosine
  • Dienogest
  • Disopyramide
  • Drospirenone
  • Norgestimate
  • Norgestrel
  • Olanzapine
  • Paroxetine
  • Prasugrel
  • Quinupristin
  • Valproic Acid
  • Warfarin
  • Risperidone
  • Tenofovir Disoproxil Fumarate
  • Theophylline
  • Trazodone
  • Nefazodone
  • Nelfinavir
  • Nevirapine
  • Norelgestromin
  • Norethindrone
  • Imipramine
  • Indinavir
  • Itraconazole
  • Lamotrigine
  • Levonorgestrel

Interactions with food, tobacco, and alcohol

Certain foods should be avoided while on some medications since this might cause interaction. Using alcohol and tobacco products with certain medications may also trigger an interaction. Discuss with your healthcare provider the use of lopinavir and ritonavir with food, alcohol and tobacco products. Specifically, avoid using alcohol while on this medication as it might affect the efficiency of the medication.

Other Medical Problems

affecting the use and effectiveness of lopinavir and ritonavir

Certain pre-existing medical conditions may affect the use, and efficiency, of lopinavir and ritonavir. Be sure to inform your healthcare provider if you have any of the following medical conditions, especially:

  • A history of liver disease (cirrhosis)
  • A history of diabetes mellitus
  • A history of bleeding problem (hemophilia)
  • Hyperglycemia (high blood sugar)
  • Hyperlipidemia (high fat or cholesterol in the blood)
  • Hepatitis B or C
  • A history of pancreatitis
  • A history of heart attack or other cardiovascular condition
  • Heart rhythm problems including prolonged QT or PR interval or congenital long QT syndrome
  • Hypokalemia (low blood potassium levels)

Lopinavir and ritonavir warnings

If you are combining lopinavir and ritonavir with didanosine, take didanosine at least 1 hour before or 2 hours after taking lopinavir and ritonavir.

Lopinavir and ritonavir contains alcohol. Do not take alcohol while on this medication

Taking this medication does NOT prevent you from double infection or passing the HIV virus to other people. Do not have unprotected sex or share toothbrushes or razors. Talk to your healthcare provider about safe sex and how to prevent HIV transmission during sex. Sharing personal effects like drugs and needles is never safe even for healthy people.

Lopinavir and ritonavir oral solution should not be administered in preterm neonates in the immediate postnatal period because of the risk of toxicities. An effective and safe dosage of lopinavir and ritonavir oral solution in this population group is yet to be established. However, if the benefits of using this medication for managing HIV infection in infants immediately after birth outweighs potential risks and side effects, then the infant should be closely monitored for increase in serum creatinine and serum osmolality, as well as for toxicities related to this medication such as renal toxicity, hyperosmolality, CNS depression, seizures, cardiac arrhythmias and ECG changes, hypotonia, and hemolysis.

Pancreatitis

Pancreatitis has been reported in patients on lopinavir and ritonavir therapy, including those who developed marked elevations of triglyceride. Fatalities have been reported in some cases. Patients with advanced HIV-1 as well as those with a history of pancreatitis are specifically at an increased risk of pancreatitis and elevated triglycerides.

Hepatotoxicity

Patients with a history of hepatitis B or C or marked elevations in transaminase before starting lopinavir and ritonavir therapy, may be at risk of developing complications when on lopinavir and ritonavir therapy.

QT interval prolongation

Lopinavir and ritonavir should be used with caution in patients with congenital long QT syndrome as well as those with hypokalemia.

PR Interval prolongation

Lopinavir and ritonavir should be used with caution in patients with pre-existing conduction system abnormalities, underlying structural heart disease, cardiomyopathies, or ischemic heart disease.

Diabetes mellitus and hyperglycemia

Patients on protease inhibitor therapy like lopinavir and ritonavir are at a greater risk of developing diabetes or experiencing an exacerbation of preexisting diabetes mellitus as well as hyperglycemia. Some patients may require an initiation or adjustment of insulin dosage or oral hypoglycemic agents while on lopinavir and ritonavir treatment.

Immune reconstruction syndrome

Immune reconstruction syndrome has been reported in patients on combination antiretroviral medications such as lopinavir and ritonavir. Additionally, autoimmune disorders such as Guillain-Barre syndrome, polymyositis, and Grave's disease have been reported in patients on this medication.

Lipid elevations

Long term lopinavir and ritonavir therapy can increase the concentration of total cholesterol and triglycerides in the patient's body. Cholesterol and triglyceride levels should be tested at the onset of the treatment and at periodic intervals during the treatment period.

Fat redistribution

Accumulation/ redistribution of body fat including dorsocervical fat enlargement (buffalo hump), central obesity, facial wasting, peripheral wasting, breast enlargement and œcushingoid appearance' have been reported in patients on long term anti-retroviral therapy.

Patients with pre-existing hemophilia

Increased bleeding, including hemarthrosis and hematomas have been reported in patients with type A and type B hemophilia who are on protease inhibitor therapy. Combination of lopinavir and ritonavir with factor VIII is recommended in some patients.

Lopinavir and ritonavir storage

Lopinavir and ritonavir tablets should be stored at room temperature (20 to 25 degrees C). Keep the medication away from pets and children in the original or USP equivalent tight container to avoid accidental administration.

Lopinavir and ritonavir oral solution should be stored at 2 degrees C to 8 degrees C. This formation should not be stored at room temperature for more than 2 weeks before use.

Keep the medication away from direct sunlight, heat and moisture for longer than 2 weeks before use. Additionally, keep the medicine from freezing.

Do not flush the medication down the sink or toilet unless advised to do so. Consult your pharmacist on how to properly dispose of expired medications or medications that you no longer use.

Summary

Lopinavir and ritonavir is a combination medicine used together with other drugs in the treatment of infections caused by the human immunodeficiency virus (HIV). It works by slowing down the progression of disease in HIV patients who have early symptoms, advanced symptoms, or no symptoms at all.

Lopinavir and ritonavir does not cure or prevent HIV infections or AIDS. It helps prevent multiplication of the HIV virus, thus appearing to slow down the degradation of the patient's immune system. In return, this helps delay the development of opportunistic complications associated with HIV and AIDS. Additionally, it is important to understand that this drug cannot prevent you from spreading HIV virus to other people. Patients on lopinavir and ritonavir therapy may continue to experience some of the health problems related to AIDS or HIV.

Lopinavir and ritonavir combination is only available with the healthcare provider's prescription. The combination comes as a solution or as a tablet to be taken orally. It should be taken two times per day but may also be taken once per day based on your healthcare provider's prescription and medical condition. The solution form must be taken with food while the tablet form may be taken with or without food. It is important that you follow the directions on the prescription or your doctor's recommendation.

Do not take this medication more often or less often than as prescribed by your healthcare provider. The tablet forms should be swallowed whole without splitting, chewing, or crushing. If you are using the solution form, be sure to shake the bottle to properly mix the medicine before taking. Always use a dose-measuring cup or spoon to measure accurate amounts of medicine for each dose. Do not measure the medicine with a regular household spoon.

For patients who have never been on any anti-retroviral medication, also referred to as treatment naïve patients with HIV, lopinavir and ritonavir should be taken once or twice per day. Your healthcare provider should help you determine the best schedule for you. For treatment-experienced patients, lopinavir and ritonavir dosing is often more frequent. This ensures that these patients do not develop resistance to the medication.

It is important that you continue taking this medication even if you feel well. Do not discontinue the medication without the knowledge and approval of your healthcare provider. If you miss multiple doses, take less than the prescribed amount, or discontinue the medication, your condition may become more difficult to treat.

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