Lexiva Side Effects

Please note - some side effects for Lexiva may not be reported. Always consult your doctor or healthcare specialist for medical advice. You may also report side effects to the FDA.

Side Effects of Lexiva - for the Consumer

Lexiva

All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome when using Lexiva:

Diarrhea; headache; nausea; tiredness; vomiting.

Seek medical attention right away if any of these SEVERE side effects occur when using Lexiva:

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue; unusual hoarseness); loss of appetite; signs of infection (eg, fever, chills, sore throat); swollen, reddened, or blistered skin; symptoms of a heart attack (eg, chest pain; fainting; numbness of an arm or leg; sudden, severe headache or vomiting); symptoms of kidney stones (eg, lower back or side pain, blood in the urine, painful urination); unusual increase in thirst or urination; unusual tiredness or weakness; weight loss; yellowing of the skin or eyes.

This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.

Lexiva Suspension

All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome when using Lexiva Suspension:

Diarrhea; headache; nausea; tiredness; vomiting.

Seek medical attention right away if any of these SEVERE side effects occur when using Lexiva Suspension:

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue; unusual hoarseness); loss of appetite; signs of infection (eg, fever, chills, sore throat); swollen, reddened, or blistered skin; symptoms of a heart attack (eg, chest pain; fainting; numbness of an arm or leg; sudden, severe headache or vomiting); symptoms of kidney stones (eg, lower back or side pain, blood in the urine, painful urination); unusual increase in thirst or urination; unusual tiredness or weakness; weight loss; yellowing of the skin or eyes.

This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.

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Lexiva Side Effects - for the Professional

Lexiva

• Severe or life-threatening skin reactions have been reported with the use of Lexiva [see Warnings and Precautions (5.2)].
• The most common moderate to severe adverse reactions in clinical studies of Lexiva were diarrhea, rash, nausea, vomiting, and headache.
• Treatment discontinuation due to adverse events occurred in 6.4% of patients receiving Lexiva and in 5.9% of patients receiving comparator treatments. The most common adverse reactions leading to discontinuation of Lexiva (incidence ≤1% of patients) included diarrhea, nausea, vomiting, AST increased, ALT increased, and rash.

Clinical Trials

Adults

  The data for the 3 active-controlled clinical trials described below reflect exposure of 700 HIV-1 infected patients to Lexiva Tablets, including 599 patients exposed to Lexiva for >24 weeks, and 409 patients exposed for >48 weeks. The population age ranged from 17 to 72 years. Of these patients, 26% were female, 51% Caucasian, 31% black, 16% American Hispanic, and 70% were antiretroviral-naive. Sixty-one percent received Lexiva 1,400 mg once daily plus ritonavir 200 mg once daily, 24% received Lexiva 1,400 mg twice daily, and 15% received Lexiva 700 mg twice daily plus ritonavir 100 mg twice daily.

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.

Selected adverse reactions reported during the clinical efficacy studies of Lexiva are shown in Tables 2 and 3. Each table presents adverse reactions of moderate or severe intensity in patients treated with combination therapy for up to 48 weeks.

Table 2. Selected Moderate/Severe Clinical Adverse Reactions Reported in ≥2% of Antiretroviral-Naive Adult Patients

Adverse Reaction	APV30001a		APV30002a
	Lexiva 1,400 mg b.i.d. (n = 166)	Nelfinavir 1,250 mg b.i.d. (n = 83)	Lexiva 1,400 mg q.d./ Ritonavir 200 mg q.d. (n = 322)	Nelfinavir 1,250 mg b.i.d. (n = 327)
Gastrointestinal
Diarrhea	5%	18%	10%	18%
Nausea	7%	4%	7%	5%
Vomiting	2%	4%	6%	4%
Abdominal pain	1%	0%	2%	2%
Skin
Rash	8%	2%	3%	2%
General disorders
Fatigue	2%	1%	4%	2%
Nervous system
Headache	2%	4%	3%	3%

aAll patients also received abacavir and lamivudine twice daily.

Table 3. Selected Moderate/Severe Clinical Adverse Reactions Reported in ≥2% of Protease Inhibitor-Experienced Adult Patients (Study APV30003)

Adverse Reaction	Lexiva 700 mg b.i.d./ Ritonavir 100 mg b.i.d.a (n = 106)	Lopinavir 400 mg b.i.d./ Ritonavir 100 mg b.i.d.a (n = 103)
Gastrointestinal
Diarrhea	13%	11%
Nausea	3%	9%
Vomiting	3%	5%
Abdominal pain	<1%	2%
Skin
Rash	3%	0%
Nervous system
Headache	4%	2%

aAll patients also received 2 reverse transcriptase inhibitors.

Skin rash (without regard to causality) occurred in approximately 19% of patients treated with Lexiva in the pivotal efficacy studies. Rashes were usually maculopapular and of mild or moderate intensity, some with pruritus. Rash had a median onset of 11 days after initiation of Lexiva and had a median duration of 13 days. Skin rash led to discontinuation of Lexiva in <1% of patients. In some patients with mild or moderate rash, dosing with Lexiva was often continued without interruption; if interrupted, reintroduction of Lexiva generally did not result in rash recurrence.

The percentages of patients with Grade 3 or 4 laboratory abnormalities in the clinical efficacy studies of Lexiva are presented in Tables 4 and 5.

Table 4. Grade 3/4 Laboratory Abnormalities Reported in ≥2% of Antiretroviral-Naive Adult Patients in Studies APV30001 and APV30002

Laboratory Abnormality	APV30001a		APV30002a
	Lexiva 1,400 mg b.i.d. (n = 166)	Nelfinavir 1,250 mg b.i.d. (n = 83)	Lexiva 1,400 mg q.d./ Ritonavir 200 mg q.d. (n = 322)	Nelfinavir 1,250 mg b.i.d. (n = 327)
ALT (>5 x ULN)	6%	5%	8%	8%
AST (>5 x ULN)	6%	6%	6%	7%
Serum lipase (>2 x ULN)	8%	4%	6%	4%
Triglyceridesb (>750 mg/dL)	0%	1%	6%	2%
Neutrophil count, absolute (<750 cells/mm3)	3%	6%	3%	4%

aAll patients also received abacavir and lamivudine twice daily.

bFasting specimens.

ULN = Upper limit of normal.

The incidence of Grade 3 or 4 hyperglycemia in antiretroviral-naive patients who received Lexiva in the pivotal studies was <1%.

Table 5. Grade 3/4 Laboratory Abnormalities Reported in ≥2% of Protease Inhibitor-Experienced Adult Patients in Study APV30003

Laboratory Abnormality	Lexiva 700 mg b.i.d./ Ritonavir 100 mg b.i.d.a (n = 104)	Lopinavir 400 mg b.i.d./ Ritonavir 100 mg b.i.d.a (n = 103)
Triglyceridesb (>750 mg/dL)	11%c	6%c
Serum lipase (>2 x ULN)	5%	12%
ALT (>5 x ULN)	4%	4%
AST (>5 x ULN)	4%	2%
Glucose (>251 mg/dL)	2%c	2%c

aAll patients also received 2 reverse transcriptase inhibitors.

bFasting specimens.

cn = 100 for Lexiva plus ritonavir, n = 98 for lopinavir plus ritonavir.

ULN = Upper limit of normal.

Pediatric Patients: Lexiva with and without ritonavir was studied in 144 pediatric patients 2 to 18 years of age in 2 open-label studies. Safety information from 75 pediatric patients receiving Lexiva twice daily with or without ritonavir follows.

All adverse events regardless of causality, all drug-related adverse events, and all laboratory events occurred with similar frequency in pediatrics compared with adults, with the exception of vomiting. Vomiting, regardless of causality, occurred more frequently among pediatric patients receiving Lexiva twice daily with ritonavir ([30%] all between 2 and 18 years of age) and without ritonavir ([56%] all between 2 and 5 years of age) compared with adults receiving Lexiva twice daily with ritonavir (10%) and without ritonavir (16%). The median duration of drug-related vomiting episodes was 1 day (range: 1 to 62 days). Vomiting required temporary dose interruptions in 4 pediatric patients and was treatment-limiting in 1 pediatric patient, all of whom were receiving Lexiva twice daily with ritonavir.

Postmarketing Experience

In addition to adverse reactions reported from clinical trials, the following reactions have been identified during post-approval use of Lexiva. Because they are reported voluntarily from a population of unknown size, estimates of frequency cannot be made. These reactions have been chosen for inclusion due to a combination of their seriousness, frequency of reporting, or potential causal connection to Lexiva. 

Cardiac Disorders

Myocardial infarction.

Metabolism and Nutrition Disorders

Hypercholesterolemia.

Nervous System Disorders

Oral paresthesia.

Skin and Subcutaneous Tissue Disorders

Angioedema.

Urogenital

Nephrolithiasis.

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Side Effects by Body System - for Healthcare Professionals

General

Diarrhea, rash, nausea, vomiting, and headache were the most frequent moderate to severe side effects in clinical trials of fosamprenavir. Discontinuations due to side effects were 6.4% in patients receiving fosamprenavir compared to 5.9% in those receiving comparator therapies. The most common side effects leading to fosamprenavir discontinuation (incidence of 1% or less) included diarrhea, nausea, vomiting, increased AST, increased ALT, and rash.

Dermatologic

Dermatologic side effects of moderate to severe intensity have included rash (up to 8%) in patients treated with combination therapy. Skin rash, regardless of causality, occurred in approximately 19% of patients treated with fosamprenavir in studies. Rashes were generally maculopapular and of mild or moderate intensity, some with pruritus. Severe or life-threatening skin reactions, including at least 1 case of Stevens-Johnson syndrome, have been reported during clinical trials. Erythema multiforme has been reported in at least 1 patient receiving fosamprenavir with ritonavir, zidovudine, and lamivudine. Angioedema has been reported during postmarketing experience.

Skin rash, regardless of causality, had a median onset and duration of 11 and 13 days, respectively, and led to discontinuation of fosamprenavir in less than 1% of patients.

Gastrointestinal

Gastrointestinal side effects of moderate to severe intensity have included diarrhea (up to 13%), nausea (up to 7%), vomiting (up to 6%), and abdominal pain (up to 2%) in patients treated with combination therapy.

Metabolic

Metabolic side effects have included increased serum lipase (greater than 2 times ULN; up to 8%), triglycerides (greater than 750 mg/dL; up to 11%), glucose (greater than 251 mg/dL; 2%), and amylase. Redistribution/accumulation of body fat, including central obesity, dorsocervical fat enlargement, peripheral wasting, facial wasting, breast enlargement, and "cushingoid appearance," have been observed in patients receiving antiretroviral therapy, including fosamprenavir. Hypercholesterolemia has been reported during postmarketing experience. New onset diabetes mellitus, exacerbation of preexisting diabetes mellitus, and hyperglycemia have been reported during postmarketing experience in HIV-infected patients receiving protease inhibitor therapy; however, causality has not been established.

The mechanism and long-term consequences of body fat redistribution/accumulation are currently unknown and a causal relationship has not been established.

Hepatic

Hepatic side effects have included elevated ALT (greater than 5 times ULN; up to 8%) and AST (greater than 5 times ULN; up to 6%). Liver toxicity has been reported in patients receiving fosamprenavir with ritonavir, zidovudine, and lamivudine.

Nervous system

Nervous system side effects of moderate to severe intensity have included headache (up to 4%) in patients treated with combination therapy. Oral paresthesia has been reported during postmarketing experience.

Other

Other side effects of moderate to severe intensity have included fatigue (up to 4%) in patients treated with combination therapy. Elevated creatine kinase has been reported.

Hematologic

Hematologic side effects have included neutropenia (less than 750 cells/mm3; 3%). Acute hemolytic anemia has been associated with amprenavir. Hematologic side effects associated with protease inhibitors have included spontaneous bleeding in patients with hemophilia A and B. In many of the reported cases, treatment with protease inhibitors was continued or restarted and some patients required additional factor VIII. A causal relationship between protease inhibitor therapy and these episodes has not been established.

Psychiatric

Psychiatric side effects have included depressive/mood disorders.

Cardiovascular

Cardiovascular side effects have included myocardial infarction during postmarketing experience.

Genitourinary

Genitourinary side effects have included nephrolithiasis during postmarketing experience.

Immunologic

Immunologic side effects have included immune reconstitution syndrome during the initial phase of treatment. Patients responding to antiretroviral therapy may develop an inflammatory response to indolent or residual opportunistic infections.

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