Raltegravir Side Effects

Some side effects of raltegravir may not be reported. Always consult your doctor or healthcare specialist for medical advice. You may also report side effects to the FDA.

For the Consumer

Applies to raltegravir: oral tablet, oral tablet chewable

Get emergency medical help if you have any of these signs of an allergic reaction while taking raltegravir: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

In rare cases, raltegravir can cause a condition that results in the breakdown of skeletal muscle tissue, leading to kidney failure. Call your doctor right away if you have unexplained muscle pain, tenderness, or weakness especially if you also have fever, unusual tiredness, and dark colored urine.

Call your doctor at once if you have a serious side effect such as:

• pale skin, easy bruising or bleeding;

• signs of a new infection, such as fever or chills, cough, or flu symptoms;

• drowsiness, confusion, increased thirst, lower back pain, urinating less than usual or not at all;

• depressed mood, unusual thoughts about hurting yourself;

• nausea, upper stomach pain, itching, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes);

• muscle pain, tenderness, or weakness with fever or flu symptoms and dark colored urine; or

• severe skin reaction -- fever, sore throat, swelling in your face or tongue, burning in your eyes, skin pain, followed by a red or purple skin rash that spreads (especially in the face or upper body) and causes blistering and peeling.

Less serious side effects of raltegravir may include:

• headache; sleep problems (insomnia);

• mild stomach pain, vomiting, diarrhea;

• tired feeling;

• dizziness; or

• changes in the shape or location of body fat (especially in your arms, legs, face, neck, breasts, and trunk).

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects.

For Healthcare Professionals

Applies to raltegravir: oral tablet, oral tablet chewable

General

The safety report of raltegravir is based on 281 treatment-naive and 462 treatment-experienced HIV-infected patients receiving the indicated twice daily dosing regimen in combination with emtricitabine plus tenofovir and optimized background therapy, respectively. The most common side effects of moderate to severe intensity which occurred in treatment-naive patients at a higher rate compared to efavirenz were insomnia, headache, nausea, and fatigue. The most common side effect of moderate to severe intensity which occurred in treatment-experienced patients at a higher rate compared to placebo was headache. The rates of discontinuation due to side effects were 5% and 9% in treatment-naive subjects receiving raltegravir and efavirenz, respectively, and 4% and 5% in treatment-experienced subjects receiving raltegravir and placebo, respectively.

Gastrointestinal

Gastrointestinal side effects of moderate to severe intensity have included nausea (3%). Abdominal pain, gastritis, dyspepsia, and vomiting have been reported in less than 2% of patients. At least one case each of mouth ulceration and peritonitis (including perihepatitis) have been reported. Diarrhea has been reported during postmarketing experience.

Nervous system

Nervous system side effects of moderate to severe intensity have included insomnia (4%) and headache (up to 4%). Dizziness has been reported in less than 2% of patients. Cerebellar ataxia has been reported during postmarketing experience.

Metabolic

Metabolic side effects have included acquired lipodystrophy and elevated serum glucose (Grade 2: up to 10%, Grade 3: up to 3%), alkaline phosphatase (Grade 2: up to 2%, Grade 3: less than 1%, Grade 4: up to 1%), pancreatic amylase (Grade 2: 2%, Grade 3: 4%, Grade 4: less than 1%), and lipase (Grade 2: 5%, Grade 3: 2%). Elevated triglycerides, fasting cholesterol, and low density lipoprotein cholesterol have been reported.

Hepatic

Hepatic side effects have included hepatitis (less than 2%) and elevated aspartate transaminase (AST; Grade 2: up to 9%, Grade 3: up to 4%, Grade 4: up to 1%), alanine transaminase (ALT; Grade 2: up to 10%, Grade 3: up to 4%, Grade 4: up to 1%), and total bilirubin (Grade 2: up to 6%, Grade 3: up to 3%, Grade 4: up to 1%). The rates of AST and ALT abnormalities were higher in patients with hepatitis B and/or hepatitis C virus coinfection. Hepatic failure (with and without associated hypersensitivity) has been reported during postmarketing experience in patients with underlying liver disease and/or concomitant medications.

In treatment-naive patients, Grade 2 or higher laboratory abnormalities indicating a worsening Grade from baseline of AST, ALT, or total bilirubin occurred in 17%, 33%, and 17%, respectively, of coinfected patients treated with raltegravir as compared to 8%, 10%, and 5% of all other patients treated with raltegravir. In treatment-experienced patients, Grade 2 or higher laboratory abnormalities indicating a worsening Grade from baseline of AST, ALT, or total bilirubin occurred in 29%, 34%, and 13%, respectively, of coinfected patients treated with raltegravir as compared to 11%, 10%, and 9% of all other patients treated with raltegravir.

Hematologic

Hematologic side effects have included decreased hemoglobin (Grade 2: up to 1%, Grade 3: up to 1%, Grade 4: less than 1%), absolute neutrophil count (Grade 2: up to 4%, Grade 3: up to 3%, Grade 4: up to 1%), and platelet count (Grade 2: up to 3%, Grade 3: up to 1%, Grade 4: up to 1%). Thrombocytopenia has been reported during postmarketing experience.

Other

Other side effects of moderate to severe intensity have included fatigue (2%). Asthenia, genital herpes, and herpes zoster have been reported in less than 2% of patients. Pyrexia and diaphoresis have been reported.

Musculoskeletal

Musculoskeletal side effects have included myopathy and rhabdomyolysis; however, relationship of raltegravir to these events is unknown. Elevated creatine kinase (Grade 2: 2%, Grade 3: 4%, Grade 4: 3%) has been reported. Rhabdomyolysis has been reported during postmarketing experience.

Cardiovascular

Cardiovascular side effects have included myocardial infarction.

Renal

Renal side effects have included nephrolithiasis (less than 2%), renal failure (less than 2%), toxic nephropathy, chronic renal failure, and renal tubular necrosis.

Hypersensitivity

Hypersensitivity side effects have included hypersensitivity (less than 2%). Hypersensitivity reactions have been reported and were characterized by rash, constitutional findings, and sometimes, organ dysfunction, including hepatic failure.

Oncologic

Oncologic side effects have included Kaposi's sarcoma, lymphoma, squamous cell carcinoma, skin cancer, hepatocellular carcinoma, rectal adenocarcinoma, and anal cancer, regardless of causality. The types and rates of specified cancers were expected in a highly immunodeficient population and most patients had other risk factors for cancer, including tobacco use, papillomavirus, and active hepatitis B virus infection. It is unknown if these cancer diagnoses were related to raltegravir use.

Immunologic

Immunologic side effects have included immune reconstitution syndrome. Autoimmune disorders (e.g., Graves' disease, polymyositis, and Guillain-Barre syndrome) have been reported in the setting of immune reconstitution.

Dermatologic

Dermatologic side effects have included skin rash and pruritus. Severe, potentially life-threatening, and fatal skin reactions (including Stevens-Johnson syndrome and toxic epidermal necrolysis) have been reported.

Rashes considered drug related were mild to moderate in severity and did not limit treatment.

Psychiatric

Psychiatric side effects have included depression (particularly in patients with a history of psychiatric illness), including suicidal ideation and behaviors, in less than 2% of patients. Abnormal dreams and exacerbation of depression have been reported. Anxiety and paranoia have been reported during postmarketing experience.

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