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Kaletra Capsules
Human Immunodeficiency Virus »
HIV facts
- The human immunodeficiency virus (HIV) is a type of virus called a retrovirus, which infects humans when it comes in contact with tissues such as those that line the vagina, anal area, mouth, or eyes, or through a break in the skin.
- HIV infection is generally a slowly progressive disease in which the virus is present throughout the body at all stages of the disease.
- Three stages of HIV infection have been described.
- The initial stage of infection (primary infection), which occurs within weeks of acquiring the virus, and often is characterized by a flu- or mono-like illness that generally resolves within weeks.
- The stage of chronic asymptomatic infection (meaning a long duration of infection without symptoms) lasts an average of eight to 10 years.
- The stage of symptomatic infection, in which the body's immune (or defense) system has...
Kaletra Capsules
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SIDE EFFECTS
Adults
Treatment-Emergent Adverse Events
KALETRA has been studied in 891 patients as combination therapy in Phase I/II and Phase III clinical trials. The most common adverse event associated with KALETRA therapy was diarrhea, which was generally of mild to moderate severity. Rates of discontinuation of randomized therapy due to adverse events were 5.8% in KALETRA-treated and 4.9% in nelfinavir-treated patients in Study 863. The incidence of diarrhea was greater for KALETRA once-daily compared to KALETRA twice-daily in Study 418 (see Table 12 and INDICATIONS AND USAGE).
Treatment-Emergent clinical adverse events of moderate or severe intensity in ≥ 2% of patients treated with combination therapy for up to 48 weeks (Phase III) and for up to 360 weeks (Phase I/II) are presented in Table 12. For other information regarding observed or potentially serious adverse events, please see WARNINGS and PRECAUTIONS.
Table 12: Percentage of Patients with Selected Treatment-Emergent1
Adverse Events of Moderate or Severe Intensity Reported in ≥ 2% of Adult
Antiretroviral-Naïve Patients
| Study 863 (48 Weeks) | Study 418 (48 Weeks) | Study 720 (360 Weeks) | |||
| KALETRA
400/100 mg BID + d4T + 3TC (N=326) |
Nelfinavir
750mg TID + d4T + 3TC (N=327) |
KALETRA
800/200 mg QD + TDF + FTC (N=115) |
KALETRA
400/100 mg BID + TDF + FTC (N=75) |
KALETRA BID2 + d4T + 3TC (N=100) |
|
| Body as a Whole | |||||
| Abdominal | 4% | 3% | 3% | 3% | 11% |
| Pain | |||||
| Asthenia | 4% | 3% | 0% | 0% | 9% |
| Headache | 2% | 2% | 3% | 3% | 6% |
| Cardiovascular System | |||||
| Vein distended | 0% | 0% | 0% | 0% | 3% |
| Digestive System | |||||
| Anorexia | 1% | <1% | <1% | 1% | 2% |
| Diarrhea | 16% | 17% | 16% | 5% | 28% |
| Dyspepsia | 2% | <1% | 0% | 1% | 6% |
| Flatulence | 2% | 1% | 2% | 1% | 4% |
| Nausea | 7% | 5% | 9% | 8% | 16% |
| Vomiting | 2% | 2% | 3% | 4% | 6% |
| Metabolic and Nutritional | |||||
| Weight Loss | 1% | < 1% | 0% | 0% | 2% |
| Musculoskeletal | |||||
| Myalgia | 1% | 1% | 0% | 0% | 2% |
| Nervous System | |||||
| Depression | 1% | 2% | 1% | 0% | 0% |
| Insomnia | 2% | 1% | 0% | 0% | 3% |
| Libido decreased | < 1% | < 1% | 0% | 1% | 2% |
| Paresthesia | 1% | 1% | 0% | 0% | 2% |
| Respiratory | |||||
| Bronchitis | 0% | 0% | 0% | 0% | 2% |
| Skin and Appendages | |||||
| Rash | 1% | 2% | 1% | 0% | 5% |
| Urogenital | |||||
| Hypogonadism male | 0% | 0% | 0% | 0% | 2% |
| 1 Includes adverse events of possible,
probable, or unknown relationship to study drug. 2 Includes adverse event data from dose group I (200/100 mg BID [N=16] and 400/100 mg BID [N=16]) and dose group II (400/100 mg BID [N=35] and 400/200 mg BID [N=33]). Within dosing groups, moderate to severe nausea of probable/possible relationship to KALETRA occurred at a higher rate in the 400/200 mg dose arm compared to the 400/100 mg dose arm in group II. |
|||||
Table 13: Percentage of Patients with Selected Treatment-Emergent1
Adverse Events of Moderate or Severe Intensity Reported in ≥ 2% of Adult
Protease Inhibitor-Experienced Patients
| Study 888 (48 Weeks) | Study 9572 and Study 7653 (84-144 Weeks) | ||
| KALETRA 400/100 mg BID + NVP + NRTIs (N=148) |
Investigator-selected protease inhibitor(s) + NVP + NRTIs (N=140) |
KALETRA BID + NNRTI + NRTIs (N=127) |
|
| Body as a Whole | |||
| Abdominal Pain | 2% | 2% | 4% |
| Asthenia | 3% | 6% | 9% |
| Chills | 2% | 0% | 0% |
| Fever | 2% | 1% | 2% |
| Headache | 2% | 3% | 2% |
| Cardiovascular | |||
| Hypertension | 0% | 0% | 2% |
| Digestive System | |||
| Anorexia | 1% | 3% | 0% |
| Diarrhea | 7% | 9% | 23% |
| Dyspepsia | 1% | 1% | 2% |
| Dysphagia | 2% | 1% | 0% |
| Flatulence | 1% | 2% | 2% |
| Nausea | 7% | 16% | 5% |
| Vomiting | 4% | 12% | 2% |
| Metabolic and Nutritional | |||
| Weight loss | 0% | 1% | 3% |
| Musculoskeletal | |||
| Myalgia | 1% | 1% | 2% |
| Nervous System | |||
| Depression | 1% | 2% | 2% |
| Insomnia | 0% | 2% | 2% |
| Paresthesia | 1% | 0% | 2% |
| Skin and Appendages | |||
| Rash | 2% | 1% | 2% |
| 1 Includes adverse events of possible,
probable, or unknown relationship to study drug. 2 Includes adverse event data from patients receiving 400/100 mg BID (n=29) or 533/133 mg BID (n=28) for 84 weeks. Patients receiving KALETRA in combination with NRTIs and efavirenz. 3 Includes adverse event data from patients receiving 400/100 mg BID (n=36) or 400/200 mg BID (n=34) for 144 weeks. Patients received KALETRA in combination with NRTIs and nevirapine. |
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Treatment-emergent adverse events occurring in less than 2% of adult patients receiving KALETRA in all phase II/III clinical trials and considered at least possibly related or of unknown relationship to treatment with KALETRA and of at least moderate intensity are listed below by body system.
Body as a Whole
Allergic reaction, back pain, chest pain, chest pain substernal, cyst, drug interaction, drug level increased, face edema, flu syndrome, hypertrophy, infection bacterial, malaise, neoplasm, and viral infection.
Cardiovascular System
Atrial fibrillation, cerebral infarct, deep thrombophlebitis, deep vein thrombosis, migraine, myocardial infarct, palpitation, postural hypotension, thrombophlebitis, varicose vein, and vasculitis.
Digestive System
Cholangitis, cholecystitis, constipation, dry mouth, enteritis, enterocolitis, eructation, esophagitis, fecal incontinence, gastritis, gastroenteritis, hemorrhagic colitis, hepatitis, hepatomegaly, increased appetite, jaundice, liver fatty deposit, liver tenderness, mouth ulceration, pancreatitis, periodontitis, sialadenitis, stomatitis, and ulcerative stomatitis.
Endocrine System
Cushing's syndrome, diabetes mellitus, and hypothyroidism.
Hemic and Lymphatic System Anemia, leukopenia, and lymphadenopathy.
Metabolic and Nutritional Disorders
Avitaminosis, dehydration, edema, glucose tolerance decreased, lactic acidosis, obesity, peripheral edema, and weight gain.
Musculoskeletal System
Arthralgia, arthrosis, bone necrosis, joint disorder, and myasthenia.
Nervous System
Abnormal dreams, agitation, amnesia, anxiety, apathy, ataxia, confusion, convulsion, dizziness, dyskinesia, emotional lability, encephalopathy, extrapyramidal syndrome, facial paralysis, hypertonia, nervousness, neuropathy, peripheral neuritis, somnolence, thinking abnormal, tremor, and vertigo.
Respiratory System
Asthma, cough increased, dyspnea, lung edema, pharyngitis, rhinitis, and sinusitis.
Skin and Appendages
Acne, alopecia, dry skin, eczema, exfoliative dermatitis, furunculosis, maculopapular rash, nail disorder, pruritis, seborrhea, skin benign neoplasm, skin discoloration, skin striae, skin ulcer, and sweating.
Special Senses
Abnormal vision, eye disorder, otitis media, taste loss, taste perversion, and tinnitus.
Urogenital System
Abnormal ejaculation, amenorrhea, breast enlargement, gynecomastia, impotence, kidney calculus, nephritis, and urine abnormality.
Post-marketing Experience
The following adverse reactions have been reported during post-marketing use of KALETRA. Because these reactions are reported voluntarily from a population of unknown size, it is not possible to reliably estimate their frequency or establish a causal relationship to KALETRA exposure.
Body as a Whole
Redistribution/accumulation of body fat has been reported (see PRECAUTIONS – Fat Redistribution ).
Cardiovascular
Bradyarrhythmias.
Skin and Appendages
Stevens Johnson Syndrome and erythema multiforme.
Laboratory Abnormalities
The percentages of adult patients treated with combination therapy with Grade 3-4 laboratory abnormalities are presented in Table 14 and Table 15.
Table 14: Grade 3-4 Laboratory Abnormalities Reported in
≥ 2% of Adult Antiretroviral-Naïve Patients
| Study 863 (48 Weeks) | Study 418 (48 Weeks) | Study 720 (360 Weeks) | ||||
| Variable | Limit1 | KALETRA
400/100 mg BID + d4T + 3TC (N=326) |
Nelfinavir
750 mg TID + d4T + 3TC (N=327) |
KALETRA
800/200 mg QD + TDF + FTC (N=115) |
KALETRA
400/100 mg BID + TDF + FTC (N=75) |
KALETRA BID + d4T + 3TC (N=100) |
| Chemistry | High | |||||
| Glucose | > 250mg/dL | 2% | 2% | 3% | 1% | 4% |
| Uric Acid | > 12mg/dL | 2% | 2% | 0% | 3% | 5% |
| SGOT/AST | > 180U/L | 2% | 4% | 5% | 3% | 10% |
| SGPT/ALT | > 215U/L | 4% | 4% | 4% | 3% | 11% |
| GGT | > 300U/L | N/A | N/A | N/A | N/A | 10% |
| Total Cholesterol | > 300mg/dL | 9% | 5% | 3% | 3% | 27% |
| Triglycerides | > 750mg/dL | 9% | 1% | 5% | 4% | 29% |
| Amylase | > 2 x ULN | 3% | 2% | 7% | 5% | 4% |
| Hematology | Low | |||||
| Neutrophils | 0.75 x109/L | 1% | 3% | 5% | 1% | 5% |
| 1 ULN = upper limit of the normal range; N/A = Not Applicable. | ||||||
Table 15: Grade 3-4 Laboratory Abnormalities Reported in
≥ 2% of Adult Protease Inhibitor-Experienced Patients
| Study888 (48 Weeks) | Study 9572 and Study 7653 (84-144 Weeks) | |||
| Variable | Limit1 | KALETRA
400/100 mg BID + NVP + NRTIs (N=148) |
Investigator-
selected protease inhibitor(s) + NVP + NRTIs (N=140) |
KALETRA BID
+ NNRTI
+ NRTIs (N=127) |
| Chemistry | High | |||
| Glucose | > 250 mg/dL | 1% | 2% | 5% |
| Total Bilirubin | > 3.48mg/dL | 1% | 3% | 1% |
| SGOT/AST | > 180 U/L | 5% | 11% | 8% |
| SGPT/ALT | > 215 U/L | 6% | 13% | 10% |
| GGT | > 300 U/L | N/A | N/A | 29% |
| Total Cholesterol | > 300mg/dL | 20% | 21% | 39% |
| Triglycerides | > 750mg/dL | 25% | 21% | 36% |
| Amylase | > 2 xULN | 4% | 8% | 8% |
| Chemistry | Low | |||
| Inorganic Phosphorus | < 1.5mg/dL | 1% | 0% | 2% |
| Hematology | Low | |||
| Neutrophils | 0.75 x 109/L | 1% | 2% | 4% |
| 1 ULN = upper limit of the normal
range; N/A = Not Applicable. 2 Includes clinical laboratory data from patients receiving 400/100 mg BID (n=29) or 533/133 mg BID (n=28) for 84 weeks. Patients received KALETRA in combination with NRTIs and efavirenz. 3 Includes clinical laboratory data from patients receiving 400/100 mg BID (n=36) or 400/200 mg BID (n=34) for 144 weeks. Patients received KALETRA in combination with NRTIs and nevirapine. |
||||
Pediatrics
Treatment-Emergent Adverse Events
KALETRA has been studied in 100 pediatric patients 6 months to 12 years of age. The adverse event profile seen during a clinical trial was similar to that for adult patients.
Taste aversion, vomiting, and diarrhea were the most commonly reported drug related adverse events of any severity in pediatric patients treated with combination therapy including KALETRA for up to 48 weeks in Study 940. A total of 8 children experienced moderate or severe adverse events at least possibly related to KALETRA. Rash (reported in 3%) was the only drug-related clinical adverse event of moderate to severe intensity observed in ≥ 2% of children enrolled.
Laboratory Abnormalities
The percentages of pediatric patients treated with combination therapy including KALETRA with Grade 3-4 laboratory abnormalities are presented in Table 16.
Table 16: Grade 3-4 Laboratory Abnormalities Reported in
≥ 2% Pediatric Patients
| Variable | Limit1 | KALETRA BID + RTIs (N = 100) |
| Chemistry | High | |
| Sodium | > 149 mEq/L | 3% |
| Total Bilirubin | 3.0 x ULN | 3% |
| SGOT/AST | > 180 U/L | 8% |
| SGPT/ALT | > 215 U/L | 7% |
| Total Cholesterol | > 300 mg/dL | 3% |
| Amylase | > 2.5 x ULN | 7%2 |
| Chemistry | Low | |
| Sodium | < 130 mEq/L | 3% |
| Hematology | Low | |
| Platelet Count | < 50 x 109/L | 4% |
| Neutrophils | < 0.40 x 109/L | 2% |
| 1 ULN = upper limit of the normal
range. 2 Subjects with Grade 3-4 amylase confirmed by elevations in pancreatic amylase. |
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DRUG INTERACTIONS
KALETRA is an inhibitor of CYP3A (cytochrome P450 3A) both in vitro and in vivo. Coadministration of KALETRA and drugs primarily metabolized by CYP3A (e.g., dihydropyridine calcium channel blockers, HMG-CoA reductase inhibitors, immunosuppressants and PDE5 inhibitors) may result in increased plasma concentrations of the other drugs that could increase or prolong their therapeutic and adverse effects (see Table 11. Established and Other Potentially Significant Drug Interactions). Agents that are extensively metabolized by CYP3A and have high first pass metabolism appear to be the most susceptible to large increases in AUC ( > 3-fold) when co-administered with KALETRA.
KALETRA does not inhibit CYP2D6, CYP2C9, CYP2C19, CYP2E1, CYP2B6 or CYP1A2 at clinically relevant concentrations.
KALETRA has been shown in vivo to induce its own metabolism and to increase the biotransformation of some drugs metabolized by cytochrome P450 enzymes and by glucuronidation.
KALETRA is metabolized by CYP3A. Co-administration of KALETRA and drugs that induce CYP3A may decrease lopinavir plasma concentrations and reduce its therapeutic effect (see Table 11. Established and Other Potentially Significant Drug Interactions).
Although not noted with concurrent ketoconazole, co-administration of KALETRA and other drugs that inhibit CYP3A may increase lopinavir plasma concentrations.
Drugs that are contraindicated and not recommended for co-administration with KALETRA are included in Table 10. Drugs That Should Not Be Co-administered With KALETRA. These recommendations are based on either drug interaction studies or predicted interactions due to the expected magnitude of interaction and potential for serious events or loss of efficacy.
Table 10: Drugs That Should Not Be Co-administered With KALETRA
| Drug Class: Drug Name | Clinical Comment |
| Alpha 1-Adrenoreceptor antagonist: Alfuzosin | CONTRAINDICATED due to potentially increased alfuzosin concentrations that can result in hypotension. |
| Antihistamines: astemizole, terfenadine | CONTRAINDICATED due to potential for serious and/or life-threatening reactions such as cardiac arrhythmias. |
| Antimycobacterial: rifampin | May lead to loss of virologic response and possible resistance to KALETRA or to the class of protease inhibitors or other co-administered antiretroviral agents. (See Table 10 for further details). |
| Ergot Derivatives: dihydroergotamine, ergonovine, ergotamine, methylergonovine | CONTRAINDICATED due to potential for serious and/or life-threatening reactions such as acute ergot toxicity characterized by peripheral vasospasm and ischemia of the extremities and other tissues. |
| GI Motility Agent: cisapride | CONTRAINDICATED due to potential for serious and/or life-threatening reactions such as cardiac arrhythmias. |
| Herbal Products: St. John's wort (hypericum perforatum) | May lead to loss of virologic response and possible resistance to KALETRA or to the class of protease inhibitors. |
| HMG-CoA Reductase Inhibitors: lovastatin, simvastatin |
Potential for serious reactions such as risk of myopathy including rhabdomyolysis. |
| Neuroleptic: pimozide | CONTRAINDICATED due to the potential for serious and/or life-threatening reactions such as cardiac arrhythmias. |
| PDE5 enzyme inhibitor: Sildenafil* (Revatio®) | CONTRAINDICATED as a safe and effective dose has not been established when used with KALETRA. There is an increased potential for sildenafil-associated adverse events, including visual abnormalities, hypotension, prolonged erection, and syncope. |
| Sedative/Hypnotics: midazolam, triazolam | CONTRAINDICATED due to potential for serious and/or life-threatening reactions such as prolonged or increased sedation or respiratory depression. |
| * see WARNINGS – DRUG INTERACTIONS and PRECAUTIONS – Table 11. Established and Other Potentially Significant Drug Interactions: Alteration in Dose or Regimen May Be Recommended Based on Drug Interaction Studies or Predicted Interaction for co-administration of sildenafil in patients with erectile dysfunction. | |
Table 11: Established and Other Potentially Significant Drug
Interactions: Alteration in Dose or Regimen May Be Recommended Based on Drug
Interaction Studies or Predicted Interaction See CLINICAL PHARMACOLOGY for Magnitude
of Interaction – Table 3 and Table 4
| Concomitant Drug Class: Drug Name | Effect on Concentration of lopinavir or Concomitant Drug | Clinical Comment |
| HIV-Antiviral Agents | ||
| Non-nucleoside Reverse Transcriptase Inhibitors: efavirenz*, nevirapine* | ↓ Lopinavir | A dose increase of KALETRA to 533/133 mg (4 capsules or 6.5 mL) twice daily taken with food is recommended when used in combination with efavirenz or nevirapine (see DOSAGE AND ADMINISTRATION ). KALETRA should not be administered once-daily in combination with efavirenz or nevirapine. NOTE: Efavirenz and nevirapine induce the activity of CYP3A and thus have the potential to decrease plasma concentrations of other protease inhibitors when used in combination with KALETRA. |
| Non-nucleoside Reverse Transcriptase Inhibitor: delavirdine | ↑Lopinavir | Appropriate doses of the combination with respect to safety and efficacy have not been established. |
| Nucleoside Reverse Transcriptase Inhibitor: didanosine | It is recommended that didanosine be administered on an empty stomach; therefore, didanosine should be given one hour before or two hours after KALETRA (given with food). | |
| Nucleoside Reverse Transcriptase Inhibitor: tenofovir | ↑Tenofovir | KALETRA increases tenofovir concentrations. The mechanism of this interaction is unknown. Patients receiving KALETRA and tenofovir should be monitored for tenofovir-associated adverse events. |
| HIV-Protease Inhibitor: amprenavir* | ↑Amprenavir (amprenavir 750 mg BID + KALETRA produces ↑AUC, similar Cmax, ↑Cmin, relative to amprenavir 1200 mg BID ↓ Lopinavir | Increase KALETRA dose to 533/133 mg and decrease amprenavir dose to
amprenavir 750 mg BID, when coadministered (see DOSAGE AND ADMINISTRATION and CLINICAL PHARMACOLOGY - Table 3 and Table 4). KALETRA should not be administered once-daily in combination with amprenavir. Appropriate doses of the combination of fosamprenavir and KALETRA have not been established. |
| HIV-Protease Inhibitor: fosamprenavir | ↓ Amprenavir ↓ Lopinavir |
An increased rate of adverse events has been observed with co-administration of these medications. Appropriate doses of the combinations with respect to safety and efficacy have not been established. |
| HIV-Protease Inhibitor: indinavir* | ↑Indinavir (indinavir 600 mg BID + KALETRA produces similar AUC, ↓ Cmax, ↑Cmin relative to indinavir 800 mg TID | Decrease indinavir dose to 600 mg BID, when coindinavir administered with KALETRA 400/100 mg BID (see CLINICAL PHARMACOLOGY - Table 4). KALETRA once-daily has not been studied in combination with indinavir. |
| HIV-Protease Inhibitor: nelfinavir* | ↑Nelfinavir (nelfinavir 1000 mg BID + KALETRA produces similar AUC, similar Cmax, ↑Cmin relative to nelfinavir 1250 mg BID) ↑M8 metabolite of nelfinavir ↓ Lopinavir | Increase KALETRA dose to 533/133 mg and decrease nelfinavir dose to 1000 mg BID, when co-administered (see DOSAGE AND ADMINISTRATION and CLINICAL PHARMACOLOGY - Table 3 and Table 4). KALETRA should not be administered once-daily in combination with nelfinavir. |
| HIV-Protease Inhibitor: saquinavir* | ↑Saquinavir (saquinavir 800 mg BID + KALETRA produces ↑AUC, ↑Cmax, ↑Cmin relative to saquinavir 1200 mg TID) | Decrease saquinavir dose to 800 mg BID, when co-administered with KALETRA 400/100 mg BID (see CLINICAL PHARMACOLOGY - Table 4). KALETRA once-daily has not been studied in combination with saquinavir. |
| HIV-Protease Inhibitor: tipranavir | ↓ Lopinavir AUC and Cmin | KALETRA should not be administered with tipranavir (500 mg twice-daily) co-administered with ritonavir (200 mg twice-daily). |
| HIV-Protease Inhibitor: ritonavir* | ↑Lopinavir | Appropriate doses of additional ritonavir in combination with KALETRA with respect to safety and efficacy have not been established. |
| Other Agents | ||
| Antiarrhythmics: amiodarone, bepridil, lidocaine (systemic), and quinidine | ↑Antiarrhythmics | Caution is warranted and therapeutic concentration monitoring is recommended for antiarrhythmics when co-administered with KALETRA, if available. |
| Anticoagulant: warfarin | Concentrations of warfarin may be affected. It is recommended that INR (international normalized ratio) be monitored. | |
| Anticonvulsants: carbamazepine, phenobarbital, phenytoin | ↓ Lopinavir | Use with caution. KALETRA may be less effective due to decreased lopinavir plasma concentrations in patients taking these agents concomitantly. KALETRA should not be administered once-daily in combination with carbamazepine, phenobarbital, or phenytoin. |
| Antidepressant: trazodone | ↑Trazodone | Concomitant use of trazodone and KALETRA may increase concentrations of trazodone. Adverse events of nausea, dizziness, hypotension and syncope have been observed following co-administration of trazodone and ritonavir. If trazodone is used with a CYP3A4 inhibitor such as ritonavir, the combination should be used with caution and a lower dose of trazodone should be considered. |
| Anti-infective: clarithromycin | ↑Clarithromycin | For patients with renal impairment, the following dosage adjustments
should be considered: For patients with CLCR 30 to 60 mL/min the dose of clarithromycin should be reduced by 50%. For patients with CLCR < 30 mL/min the dose of clarithromycin should be decreased by 75%. No dose adjustment for patients with normal renal function is necessary. |
| Antifungals: ketoconazole*, itraconazole, voriconazole | ↑Ketoconazole ↑Itraconazole Voriconazole effect is unknown. |
High doses of ketoconazole or itraconazole ( > 200 mg/day) are not
recommended. Coadministration of voriconazole with KALETRA has not been studied. However, administration of voriconazole with ritonavir 400 mg every 12 hours decreased voriconazole steady-state AUC by an average of 82%. The effect of lower ritonavir doses on voriconazole is not known at this time. Until data are available, voriconazole should not be administered to patients receiving KALETRA. |
| Anti-gout colchicine | ↑Colchicine | Patients with renal or hepatic impairment should not be given colchicine
with KALETRA. Treatment of gout flares - co-administration of colchicine in patients on KALETRA: 0.6 mg (1 tablet) x 1 dose, followed by 0.3 mg (half tablet) 1 hour later. Dose to be repeated no earlier than 3 days. Prophylaxis of gout flares - co-administration of colchicine in patients on KALETRA: If the original colchicine regimen was 0.6 mg twice a day, the regimen should be adjusted to 0.3 mg once a day. If the original colchicine regimen was 0.6 mg once a day, the regimen should be adjusted to 0.3 mg once every other day. Treatment of familial Mediterranean fever (FMF) - coadministration of colchicine in patients on KALETRA: Maximum daily dose of 0.6 mg (may be given as 0.3 mg twice a day). |
| Antimycobacterial: rifabutin* | ↑Rifabutin and rifabutin metabolite | Dosage reduction of rifabutin by at least 75% of the usual dose of 300 mg/day is recommended (i.e., a maximum dose of 150 mg every other day or three times per week). Increased monitoring for adverse events is warranted in patients receiving the combination. Further dosage reduction of rifabutin may be necessary. |
| Antimycobacterial: Rifampin | ↓ Lopinavir | May lead to loss of virologic response and possible resistance to KALETRA or to the class of protease inhibitors or other co-administered antiretroviral agents. A study evaluated combination of rifampin 600 mg QD, with KALETRA 800/200 mg BID or KALETRA 400/100 mg + ritonavir 300 mg BID. Pharmacokinetic and safety results from this study do not allow for a dose recommendation. Nine subjects (28%) experienced a . grade 2 increase in ALT/AST, of which seven (21%) prematurely discontinued study per protocol. Based on the study design, it is not possible to determine whether the frequency or magnitude of the ALT/AST elevations observed is higher than what would be seen with rifampin alone. (See CLINICAL PHARMACOLOGY for Magnitude of Interaction . Table 3). |
| Antiparasitic: atovaquone | ↓ Atovaquone | Clinical significance is unknown; however, increase in atovaquone doses may be needed. |
| Calcium Channel Blockers, Dihydropyridine: e.g., felodipine, nifedipine, nicardipine | ↑Dihydropyridine calcium channel blockers | Caution is warranted and clinical monitoring of patients is recommended. |
| Corticosteroid: Dexamethasone | ↓ Lopinavir | Use with caution. KALETRA may be less effective due to decreased lopinavir plasma concentrations in patients taking these agents concomitantly. |
| Disulfiram/metronidazole | KALETRA oral solution contains alcohol, which can produce disulfiram-like reactions when co-administered with disulfiram or other drugs that produce this reaction (e.g., metronidazole). | |
| Endothelin receptor antagonists: bosentan | ↑Bosentan | Co-administration of bosentan in patients on KALETRA: In patients who have been receiving KALETRA for at least 10 days, start bosentan at 62.5 mg once daily or every other day based upon individual tolerability. Co-administration of KALETRA in patients on bosentan: Discontinue use of bosentan at least 36 hours prior to initiation of KALETRA. After at least 10 days following the initiation of KALETRA, resume bosentan at 62.5 mg once daily or every other day based upon individual tolerability. |
| PDE5 inhibitors: sildenafil, tadalafil, vardenafil | ↑Sildenafil ↑Tadalafil ↑Vardenafil |
Particular caution should be used when prescribing sildenafil, tadalafil,
or vardenafil in patients receiving KALETRA. Co-administration of KALETRA
with these drugs is expected to substantially increase their concentrations
and may result in an increase in PDE5 inhibitor associated adverse reactions
including hypotension, syncope, visual changes, and prolonged erection.
Use of PDE5 inhibitors for pulmonary arterial hypertension (PAH): Sildenafil (Revatio®) is contraindicated when used for the treatment of pulmonary arterial hypertension (PAH) because a safe and effective dose has not been established when used with KALETRA [see CONTRAINDICATIONS]. The following dose adjustments are recommended for use of tadalafil (Adcirca™) with KALETRA: Co-administration of ADCIRCA in patients on KALETRA: In patients receiving KALETRA for at least one week, start ADCIRCA at 20 mg once daily. Increase to 40 mg once daily based upon individual tolerability. Co-administration of KALETRA in patients on ADCIRCA: Avoid use of ADCIRCA during the initiation of KALETRA. Stop ADCIRCA at least 24 hours prior to starting KALETRA. After at least one week following the initiation of KALETRA, resume ADCIRCA at 20 mg once daily. Increase to 40 mg once daily based upon individual tolerability. Use of PDE5 inhibitors for the treatment of erectile dysfunction: It is recommended not to exceed the following doses: Sildenafil: 25 mg every 48 hours Tadalafil: 10 mg every 72 hours Vardenafil: 2.5 mg every 72 hours Use with increased monitoring for adverse events. |
| HMG-CoA Reductase Inhibitors: atorvastatin* rosuvastatin | ↑atorvastatin ↑rosuvastatin |
Use lowest possible dose of atorvastatin or rosuvastatin with careful monitoring, or consider other HMG-CoA reductase inhibitors such as pravastatin or fluvastatin in combination with KALETRA. |
| Immunosuppressants: cyclosporine, tacrolimus, rapamycin | ↑Immunosuppressants | Therapeutic concentration monitoring is recommended for immunosuppressant agents when co-administered with KALETRA. |
| Inhaled Steroid: fluticasone | ↑Fluticasone | Concomitant use of fluticasone propionate and KALETRA may increase plasma concentrations of fluticasone propionate, resulting in significantly reduced serum cortisol concentrations. Co-administration of fluticasone propionate and KALETRA is not recommended unless the potential benefit to the patient outweighs the risk of systemic corticosteroid side effect (see WARNINGS ) |
| Long-acting betaadrenoceptor agonist: salmeterol |
↑salmeterol | Concurrent administration of salmeterol and KALETRA is not recommended. The combination may result in increased risk of cardiovascular adverse events associated with salmeterol, including QT prolongation, palpitations and sinus tachycardia. |
| Narcotic Analgesic: Methadone* | ↓ Methadone | Dosage of methadone may need to be increased when co-administered with KALETRA. |
| Oral Contraceptive: ethinyl estradiol* | ↓ Ethinyl estradiol | Because contraceptive steroid concentrations may be altered when KALETRA is co-administered with oral contraceptives or with the contraceptive patch, alternative methods of nonhormonal contraception are recommended. |
| * See CLINICAL PHARMACOLOGY for Magnitude of Interaction -Table 3 and Table 4. | ||
Other Drugs
Drug interaction studies reveal no clinically significant interaction between KALETRA and desipramine (CYP2D6 probe), pravastatin, stavudine, lamivudine, omeprazole or ranitidine.
Based on known metabolic profiles, clinically significant drug interactions are not expected between KALETRA and fluvastatin, dapsone, trimethoprim/sulfamethoxazole, azithromycin, erythromycin, or fluconazole.
Zidovudine and Abacavir: KALETRA induces glucuronidation; therefore, KALETRA has the potential to reduce zidovudine and abacavir plasma concentrations. The clinical significance of this potential interaction is unknown.
Last reviewed on RxList: 5/25/2010
This monograph has been modified to include the generic and brand name in many instances.
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