Note: This document contains side effect information about lopinavir / ritonavir. Some dosage forms listed on this page may not apply to the brand name Kaletra.

Summary

Common side effects of Kaletra include: increased serum cholesterol and increased serum triglycerides. Other side effects include: hyperglycemia and increased serum amylase. Continue reading for a comprehensive list of adverse effects.

Applies to lopinavir / ritonavir: oral solution, oral tablet.

Serious side effects of Kaletra

Along with its needed effects, lopinavir/ritonavir may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur while taking lopinavir / ritonavir:

Less common

• Bloating
• blurred vision
• chills
• constipation
• darkened urine
• dry mouth
• fast heartbeat
• fever
• flushed, dry skin
• fruit-like breath odor
• increased hunger
• increased thirst
• increased urination
• indigestion
• loss of appetite
• loss of consciousness
• nausea
• pains in the stomach, side, or abdomen, possibly moving to the back
• sweating
• troubled breathing
• unexplained weight loss
• vomiting
• yellow eyes or skin

Incidence not known

• Blistering, peeling, or loosening of the skin
• chest pain or discomfort
• cough
• diarrhea
• itching
• joint or muscle pain
• lightheadedness, dizziness, or fainting
• red skin lesions, often with a purple center
• red, irritated eyes
• slow or irregular heartbeat
• sore throat
• sores, ulcers, or white spots in the mouth or on the lips
• unusual tiredness or weakness

Get emergency help immediately if any of the following symptoms of overdose occur while taking lopinavir / ritonavir:

Symptoms of overdose

• Agitation
• confusion
• cool, sweaty skin
• decreased appetite
• decreased awareness or responsiveness
• decreased urine output
• depression
• fast, irregular, or pounding heartbeat
• fast, shallow breathing
• general feeling of discomfort
• headache
• hostility
• irritability
• muscle pain or cramping
• muscle twitching
• pounding, slow heartbeat
• rapid weight gain
• seizures
• severe sleepiness
• stomach discomfort
• swelling of the face, ankles, or hands
• swelling of the feet or lower legs
• unusual drowsiness, dullness, tiredness, weakness, or feeling of sluggishness

Other side effects of Kaletra

Some side effects of lopinavir / ritonavir may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects.

Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

Less common

• Abnormal stools
• belching
• heartburn
• lack or loss of strength
• pain
• skin rash
• trouble with sleeping

Incidence not known

• Redistribution of body fat

For Healthcare Professionals

Applies to lopinavir / ritonavir: oral capsule, oral liquid, oral tablet.

General

In clinical studies, this drug was used with nucleoside reverse transcriptase inhibitors with or without efavirenz or nevirapine. The most common side effects were diarrhea, nausea, vomiting, hypertriglyceridemia, and hypercholesterolemia. Diarrhea, nausea, and vomiting occurred more often at the start of therapy while hypertriglyceridemia and hypercholesterolemia generally occurred later. Diarrhea was reported more often when this drug was used once a day than when it was used twice a day.^[Ref]

Other

Increased total cholesterol (greater than 300 mg/dL) and triglycerides (greater than 750 mg/dL) have been reported in up to 39% and up to 36% of patients, respectively. Decreased inorganic phosphorus (less than 1.5 mg/dL) has been reported in up to 2% of patients.^[Ref]

Very common (10% or more): Increased total cholesterol (up to 39%), increased triglycerides (up to 36%)

Common (1% to 10%): Fatigue, asthenia, pain, decreased weight, pyrexia, chills, decreased inorganic phosphorus

Uncommon (0.1% to 1%): Increased weight

Frequency not reported: Generalized pain, back and abdomen enlargement, chest pain, cyst, edema, peripheral edema, face edema, influenza syndrome, hypertrophy, malaise, drug interaction, increased drug level, bacterial infection, viral infection, otitis media, breast enlargement

Antiretroviral therapy:

-Frequency not reported: Increased weight, increased blood lipid levels^[Ref]

Hepatic

Very common (10% or more): Increased GGT (up to 29%), increased ALT (up to 11%)

Common (1% to 10%): Increased AST, hepatitis (including increased AST, ALT, GGT), increased total bilirubin

Uncommon (0.1% to 1%): Hepatomegaly, cholangitis, hepatic steatosis, hyperbilirubinemia, jaundice

Frequency not reported: Fatty liver deposit, cytolytic hepatitis, liver tenderness, hepatic failure, cholecystitis, hepatic dysfunction

Postmarketing reports: Jaundice, hepatitis^[Ref]

Increased GGT (greater than 300 units/L), ALT (greater than 215 units/L), AST (greater than 180 units/L), and total bilirubin (greater than 3.48 mg/dL) have been reported in up to 29%, up to 11%, up to 10%, and 1% of patients, respectively.

Patients with underlying hepatitis B or C or marked elevations in transaminases before initiation of therapy may be at an increased risk for developing further transaminase elevations or liver decompensation. There have been reports of hepatic dysfunction with some cases leading to death. A causal relationship with this drug has not been proven since these cases have generally occurred in patients with advanced HIV who also had underlying chronic hepatitis or cirrhosis and were taking multiple concomitant medications.^[Ref]

Gastrointestinal

Very common (10% or more): Diarrhea (up to 28%), nausea (up to 16%)

Common (1% to 10%): Increased amylase, vomiting, abdominal pain, upper abdominal pain, lower abdominal pain, increased lipase, gastroenteritis and colitis, dyspepsia, pancreatitis, gastroesophageal reflux disease, hemorrhoids, flatulence, abdominal distention, abnormal feces, constipation, dysphagia

Uncommon (0.1% to 1%): Stomatitis and oral ulcers, duodenitis, gastritis, gastrointestinal hemorrhage (including rectal hemorrhage), dry mouth, gastrointestinal ulcer, fecal incontinence

Frequency not reported: Abdominal discomfort, enteritis, enterocolitis, eructation, esophagitis, gastric disorder, gastric ulcer, hemorrhagic enterocolitis, mouth ulceration, periodontitis, sialadenitis, stomach discomfort, ulcerative stomatitis^[Ref]

Increased amylase (greater than 2 times the upper limit of normal [2 x ULN]) and lipase (greater than 2 x ULN) were reported in up to 8% and up to 5% of patients, respectively.

Pancreatitis, including fatalities, has occurred in patients receiving this drug, including those who developed hypertriglyceridemia. Although a causal relationship has not been established, marked triglyceride elevation is a risk factor for the development of pancreatitis.^[Ref]

Respiratory

Very common (10% or more): Upper respiratory tract infection (up to 13.9%)

Common (1% to 10%): Lower respiratory tract infection, bronchitis

Frequency not reported: Asthma, bronchopneumonia, dyspnea, pulmonary edema, pharyngitis, rhinitis, increased cough, sinusitis, influenza^[Ref]

Metabolic

Increased glucose (greater than 250 mg/dL) and uric acid (greater than 12 mg/dL) have each been reported in up to 5% of patients.

Episodes of hyperglycemia, new onset diabetes mellitus, and exacerbation of preexisting diabetes mellitus have been reported during postmarketing studies in HIV-infected patients receiving protease inhibitors. In some cases, diabetic ketoacidosis has occurred. No causal relationship has been established.^[Ref]

Common (1% to 10%): Hypercholesterolemia, hypertriglyceridemia, increased glucose, increased uric acid, decreased appetite, blood glucose disorders (including diabetes mellitus), anorexia

Uncommon (0.1% to 1%): Lactic acidosis, increased appetite

Frequency not reported: Avitaminosis, hypovitaminosis, dehydration, dyslipidemia, hyperamylasemia, hyperlipasemia, decreased glucose tolerance, lipomatosis, obesity, hyperglycemia, new onset diabetes mellitus, exacerbation of preexisting diabetes mellitus, ketoacidosis, insulin resistance, hyperlactatemia

Postmarketing reports: Redistribution/accumulation of body fat (including central obesity, dorsocervical fat enlargement, peripheral wasting, facial wasting, breast enlargement, "cushingoid appearance")

Combination antiretroviral therapy:

-Frequency not reported: Redistribution of body fat (fat loss or fat gain)

Antiretroviral therapy:

-Frequency not reported: Redistribution/accumulation of body fat, increased glucose levels^[Ref]

Musculoskeletal

Common (1% to 10%): Musculoskeletal pain (including arthralgia, back pain), increased creatine phosphokinase, myalgia, muscle disorders (such as weakness, spasms)

Uncommon (0.1% to 1%): Rhabdomyolysis, osteonecrosis

Frequency not reported: Arthropathy, arthrosis, muscular weakness, joint disorder, osteoarthritis, extremity pain, myasthenia, myositis, perineal abscess^[Ref]

Increased creatine phosphokinase (greater than 4 x ULN) was reported in up to 5% of patients.^[Ref]

Nervous system

Common (1% to 10%): Headache (including migraine), neuropathy (including peripheral neuropathy), dizziness, paresthesia

Uncommon (0.1% to 1%): Ageusia, convulsion, vertigo, tremor, cerebrovascular accident/event, tinnitus, dysgeusia

Frequency not reported: Amnesia, ataxia, balance disorder, abnormal coordination, cerebral infarction, dyskinesia, encephalopathy, facial paralysis/palsy, hypertonia, peripheral neuritis, somnolence, hyperacusis, extrapyramidal disorder^[Ref]

Hematologic

Decreased neutrophils (less than 0.75 x 10[9]/L) and hemoglobin (less than 8 g/dL) have been reported in up to 5% and up to 2% of patients, respectively.^[Ref]

Common (1% to 10%): Decreased neutrophils, anemia, decreased hemoglobin, leukopenia, neutropenia, lymphadenopathy

Rare (less than 0.1%): Hemolytic anemia, spontaneous bleeding in hemophiliacs

Frequency not reported: Splenomegaly^[Ref]

Psychiatric

Common (1% to 10%): Anxiety, insomnia, decreased libido, depression

Uncommon (0.1% to 1%): Abnormal dreams

Frequency not reported: Affect lability, agitation, apathy, confusional state, disorientation, mood swings, nervousness, abnormal thinking^[Ref]

Dermatologic

Common (1% to 10%): Rash (including maculopapular rash), skin infections (including cellulitis, folliculitis, furuncle), acquired lipodystrophy (including facial wasting), dermatitis/rash (including eczema, seborrheic dermatitis), night sweats, pruritus

Uncommon (0.1% to 1%): Alopecia, capillaritis, vasculitis

Rare (0.01% to 0.1%): Stevens-Johnson syndrome, erythema multiforme

Frequency not reported: Acne, dry skin, acneiform dermatitis, allergic dermatitis, exfoliative dermatitis, idiopathic capillaritis, generalized rash, nail disorder, seborrhea, benign skin neoplasm, skin discoloration, skin hypertrophy, skin ulcer, skin striae, swelling face, hyperhidrosis, acute generalized exanthematous pustulosis, furunculosis

Postmarketing reports: Toxic epidermal necrolysis, Stevens-Johnson syndrome, erythema multiforme^[Ref]

Renal

Common (1% to 10%): Decreased calculated CrCl, renal failure

Uncommon (0.1% to 1%): Nephritis

Frequency not reported: Nephrolithiasis, renal disorder

Postmarketing reports: Nephrolithiasis^[Ref]

Decreased calculated CrCl (less than 50 mL/min) was reported in up to 3% of patients.^[Ref]

Hypersensitivity

Common (1% to 10%): Hypersensitivity (including urticaria, angioedema)

Frequency not reported: Drug hypersensitivity, severe skin and mucous hypersensitivity reaction with transient multiorgan failure^[Ref]

Cardiovascular

Common (1% to 10%): Hypertension, vasodilatation

Uncommon (0.1% to 1%): Deep vein thrombosis, atherosclerosis (such as myocardial infarction), atrioventricular (AV) block, tricuspid valve incompetence

Frequency not reported: Distended veins, angina pectoris, atrial fibrillation, chest pain, palpitation, orthostatic hypotension, thrombophlebitis, varicose vein, vasculitis, sinus arrest, bradycardia-tachycardia syndrome

Postmarketing reports: Bradyarrhythmias, first-degree AV block, second-degree AV block, third-degree AV block, QTc interval prolongation, torsades de pointes^[Ref]

Genitourinary

Common (1% to 10%): Erectile dysfunction, menstrual disorders, amenorrhea, menorrhagia

Uncommon (0.1% to 1%): Hematuria

Frequency not reported: Ejaculation disorder, impotence, abnormal urine odor, urine abnormality^[Ref]

Endocrine

Common (1% to 10%): Hypogonadism

Frequency not reported: Cushing's syndrome, hypothyroidism, gynecomastia^[Ref]

Ocular

Uncommon (0.1% to 1%): Visual impairment

Frequency not reported: Visual disturbance, eye disorder^[Ref]

Immunologic

Uncommon (0.1% to 1%): Immune reconstitution syndrome/immune reconstitution inflammatory syndrome

Frequency not reported: Autoimmune disorders in the setting of immune reconstitution (e.g., Graves' disease, polymyositis, Guillain-Barre syndrome, autoimmune hepatitis)

Oncologic

Frequency not reported: Neoplasm, lipoma