Aptivus
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Aptivus
Aptivus Side Effects Center
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
What is Patient Information in Detail?
Easy-to-read and understand detailed drug information and pill images for the patient or caregiver from Cerner Multum.
Aptivus in Detail - Patient Information: Side Effects
Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.
- unusual bleeding (such as a nosebleed or blood in your urine or stools);
- sudden headache, confusion, problems with vision, speech, or balance;
- low fever, nausea, stomach pain, loss of appetite;
- dark urine, clay-colored stools; or
- jaundice (yellowing of the skin or eyes).
Stop taking tipranavir and call your doctor at once if you have any of these serious side effects:
- severe skin rash, blistering, peeling, or sunburn;
- increased urination or extreme thirst;
- easy bruising or bleeding; or
- signs of a new infection, such as fever or chills, cough, skin lesions, or flu symptoms.
Less serious side effects may include:
- mild nausea, vomiting, diarrhea, stomach pain;
- headache, tired feeling; or
- changes in the shape or location of body fat (especially in your arms, legs, face, neck, breasts, and waist).
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Read the entire detailed patient monograph for Aptivus (Tipranavir) »
What is Patient Information Overview?
A concise overview of the drug for the patient or caregiver from First DataBank.
Aptivus Overview - Patient Information: Side Effects
Diarrhea, nausea, drowsiness, dizziness, headache or vomiting may occur. If any of these effects persist or worsen, notify your doctor or pharmacist promptly.
Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.
Some people may experience worsening of a previous medical condition (such as an old infection) as their immune systems improve, or develop new conditions because their immune systems have become overactive. This reaction may occur at any time (soon after starting HIV treatment or many months later). Tell your doctor right away if you have any serious side effects, including: unexplained weight loss, persistent muscle aches/weakness, joint pain, numbness/tingling of the hands/feet/arms/legs, severe tiredness, vision changes, severe/persistent headaches, signs of infection (such as fever, chills, trouble breathing, cough, non-healing skin sores), signs of an overactive thyroid (such as irritability, nervousness, heat intolerance, fast/pounding/irregular heartbeat, bulging eyes, unusual growth in the neck/thyroid known as a goiter), signs of a certain nerve problem known as Guillain-Barre Syndrome (such as difficulty breathing/swallowing/moving your eyes, drooping face, paralysis, slurred speech).
Tell your doctor immediately if any of these unlikely but serious side effects occur: depression, increased thirst, change in the amount of urine.
Seek immediate medical attention if any of these rare but serious side effects occur: symptoms of a heart attack (such as chest/jaw/left arm pain, shortness of breath, unusual sweating).
Changes in body fat may occur while you are taking this medication (e.g., increased fat in the upper back and stomach areas, decreased fat in the arms and legs). The cause and long-term effects of these changes are unknown. Discuss the risks and benefits of therapy with your doctor, as well as the possible role of exercise to reduce this side effect.
A very serious allergic reaction to this drug is unlikely, but seek immediate medical attention if it occurs. Symptoms of a serious allergic reaction may include: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.
Tipranavir can commonly cause a mild rash that is usually not serious. However, you may not be able to tell it apart from a rare rash that could be a sign of a severe allergic reaction. Therefore, seek immediate medical attention if you develop a rash. Taking estrogen (in birth control or hormone therapy) may increase your risk of developing this rash.
This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.
In the US -
Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
Read the entire patient information overview for Aptivus (Tipranavir)»
What is Prescribing information?
The FDA package insert formatted in easy-to-find categories for health professionals and clinicians.
Aptivus FDA Prescribing Information: Side Effects
(Adverse Reactions)
SIDE EFFECTS
The following adverse reactions are described, in greater detail, in other sections:
- Hepatic Impairment and Toxicity [see WARNINGS AND PRECAUTIONS]
- Intracranial Hemorrhage [see WARNINGS AND PRECAUTIONS]
- Rash [see WARNINGS AND PRECAUTIONS]
Due to the need for co-administration of APTIVUS with ritonavir, please refer to ritonavir prescribing information for ritonavir-associated adverse reactions.
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.
Clinical Trials in Adults
APTIVUS, co-administered with ritonavir, has been studied in a total of 6308 HIV-1 positive adults as combination therapy in clinical studies. Of these, 1299 treatment-experienced patients received the dose of 500/200 mg BID. Nine hundred nine (909) adults, including 541 in the 1182.12 and 1182.48 controlled clinical trials, have been treated for at least 48 weeks [see Clinical Studies].
In 1182.12 and 1182.48 in the APTIVUS/ritonavir arm, the most frequent adverse reactions were diarrhea, nausea, pyrexia, vomiting, fatigue, headache, and abdominal pain. The 48-Week Kaplan-Meier rates of adverse reactions leading to discontinuation were 13.3% for APTIVUS/ritonavir-treated patients and 10.8% for the comparator arm patients.
Adverse reactions reported in the controlled clinical trials 1182.12 and 1182.48, based on treatment-emergent clinical adverse reactions of moderate to severe intensity (Grades 2 - 4) in at least 2% of treatment-experienced subjects in either treatment group are summarized in Table 2 below.
Table 2 : Adverse Reactions Reported in Randomized,
Controlled Clinical Trials (1182.12 and 1182.48) Based on Treatment-Emergent
Clinical Adverse Reactions of Moderate to Severe Intensity (Grades 2 -4) in at
least 2% of Treatment-Experienced Subjects in either Treatment Groupa
(48-week Analyses)
| Percentage of patients (rate per 100 patient-exposure years) | ||
| APTIVUS/ritonavir (500/200 mg BID) + OBRc (n=749; 757.4 patient-exposure years) |
Comparator PI/ritonavirb + OBR (n=737; 503.9 patient-exposure years) |
|
| Blood and Lymphatic Disorders | ||
| Anemia | 3.3% (3.4) | 2.3% (3.4) |
| Neutropenia | 2.0% (2.0) | 1.0% (1.4) |
| Gastrointestinal Disorders | ||
| Diarrhea | 15.0% (16.5) | 13.4% (21.6) |
| Nausea | 8.5% (9.0) | 6.4% (9.7) |
| Vomiting | 5.9% (6.0) | 4.1% (6.1) |
| Abdominal pain | 4.4% (4.5) | 3.4% (5.1) |
| Abdominal pain upper | 1.5% (1.5) | 2.3% (3.4) |
| General Disorders | ||
| Pyrexia | 7.5% (7.7) | 5.4% (8.2) |
| Fatigue | 5.7% (5.9) | 5.6% (8.4) |
| Investigations | ||
| Weight decreased | 3.1% (3.1) | 2.2% (3.2) |
| ALT increased | 2.0% (2.0) | 0.5% (0.8) |
| GGT increased | 2.0% (2.0) | 0.4% (0.6) |
| Metabolism and Nutrition Disorders | ||
| Hypertriglyceridemia | 3.9% (4.0) | 2.0% (3.0) |
| Hyperlipidemia | 2.5% (2.6) | 0.8% (1.2) |
| Dehydration | 2.1% (2.1) | 1.1% (1.6) |
| Musculoskeletal and Connective Tissue Disorders | ||
| Myalgia | 2.3% (2.3) | 1.8% (2.6) |
| Nervous System Disorders | ||
| Headache | 5.2% (5.3) | 4.2% (6.3) |
| Peripheral neuropathy | 1.5% (1.5) | 2.0% (3.0) |
| Psychiatric Disorders | ||
| Insomnia | 1.7% (1.7) | 3.7% (5.5) |
| Respiratory, Thoracic and Mediastinal Disorders | ||
| Dyspnea | 2.1% (2.1) | 1.0% (1.4) |
| Skin and Subcutaneous Tissue Disorders | ||
| Rash | 3.1% (3.1) | 3.8% (5.7) |
| aExcludes laboratory abnormalities that were Adverse Events bComparator PI/ritonavir: lopinavir/ritonavir 400/100 mg BID, indinavir/ritonavir 800/100 mg BID, saquinavir/ritonavir 1000/100 mg BID, amprenavir/ritonavir 600/100 mg BID cOptimized Background Regimen |
||
Less Common Adverse Reactions
Other adverse reactions reported in < 2% of adult patients (n=1474) treated with APTIVUS/ritonavir 500/200 mg in Phase 2 and 3 clinical trials are listed below by body system:
Blood and Lymphatic System Disorders: thrombocytopenia
Gastrointestinal Disorders: abdominal distension, dyspepsia, flatulence, gastroesophageal reflux disease, pancreatitis
General Disorders: influenza-like illness, malaise
Hepatobiliary Disorders: hepatitis, hepatic failure, hyperbilirubinemia, cytolytic hepatitis, toxic hepatitis, hepatic steatosis
Immune System Disorders: hypersensitivity
Investigations: hepatic enzymes increased, liver function test abnormal, lipase increased
Metabolism and Nutrition Disorders: anorexia, decreased appetite, diabetes mellitus, facial wasting, hyperamylasemia, hypercholesterolemia, hyperglycemia, mitochondrial toxicity
Musculoskeletal and Connective Tissue Disorders: muscle cramp
Nervous System Disorders: dizziness, intracranial hemorrhage, somnolence
Psychiatric Disorders: sleep disorder
Renal and Urinary Disorders: renal insufficiency
Skin and Subcutaneous System Disorders: exanthem, lipoatrophy, lipodystrophy acquired, lipohypertrophy, pruritus
Laboratory Abnormalities
Treatment-emergent laboratory abnormalities reported at 48 weeks in the controlled clinical trials 1182.12 and 1182.48 in adults are summarized in Table 3 below.
Table 3 : Treatment-Emergent Laboratory Abnormalities
Reported in ≥ 2% of Adult Patients (48-week Analyses)
| Limit | Randomized, Controlled Clinical Trials 1182.12 and 1182.48 | ||
| Percentage of Patients (rate per 100 patient-exposure years) | |||
| APTIVUS/ritonavir (500/200 mg BID) + OBR (n=738) |
Comparator PI/ritonavir + OBR* (n=724) |
||
| Hematology | |||
| WBC count decrease | |||
| Grade 3 | < 2.0 x 103/μL | 5.4% (5.6) | 4.8% (7.7) |
| Grade 4 | < 1.0 x 103/μL | 0.3% (0.3) | 1.1% (1.7) |
| Chemistry | |||
| Amylase | |||
| Grade 3 | > 2.5 x ULN | 5.7% (5.9) | 6.4% (10.4) |
| Grade 4 | > 5 x ULN | 0.3% (0.3) | 0.7% (1.1) |
| ALT | |||
| Grade 2 | > 2.5-5 x ULN | 14.9% (16.5) | 7.5% (12.4) |
| Grade 3 | > 5-10 x ULN | 5.6% (5.7) | 1.7% (2.6) |
| Grade 4 | > 10 x ULN | 4.1% (4.1) | 0.4% (0.7) |
| AST | |||
| Grade 2 | > 2.5-5 x ULN | 9.9% (10.5) | 8.0% (13.3) |
| Grade 3 | > 5-10 x ULN | 4.5% (4.6) | 1.4% (2.2) |
| Grade 4 | > 10 x ULN | 1.6% (1.6) | 0.4% (0.6) |
| ALT and/or AST | |||
| Grade 2-4 | > 2.5 x ULN | 26.0% (31.5) | 13.7% (23.8) |
| Cholesterol | |||
| Grade 2 | > 300 - 400 mg/dL | 15.6% (17.7) | 6.4% (10.5) |
| Grade 3 | > 400 - 500 mg/dL | 3.3% (3.3) | 0.3% (0.4) |
| Grade 4 | > 500 mg/dL | 0.9% (1.0) | 0.1% (0.2) |
| Triglycerides | |||
| Grade 2 | 400 - 750 mg/dL | 35.9% (49.9) | 26.8% (51.0) |
| Grade 3 | > 750 - 1200 mg/dL | 16.9% (19.4) | 8.7% (14.6) |
| Grade 4 | > 1200 mg/dL | 8.0% (8.4) | 4.3% (7.0) |
| *Comparator PI/ritonavir: lopinavir/ritonavir 400/100 mg BID, indinavir/ritonavir 800/100 mg BID, saquinavir/ritonavir 1000/100 mg BID, amprenavir/ritonavir 600/100 mg BID | |||
In controlled clinical trials 1182.12 and 1182.48 extending up to 96 weeks, the proportion of patients who developed Grade 2-4 ALT and/or AST elevations increased from 26% at week 48 to 32.1% at week 96 with APTIVUS/ritonavir. The risk of developing transaminase elevations is greater during the first year of therapy.
Clinical Trials in Pediatric Patients
APTIVUS, co-administered with ritonavir, has been studied in a total of 135 HIV-1 infected pediatric patients age 2 through 18 years as combination therapy. This study enrolled HIV-1 infected, treatment-experienced pediatric patients (with the exception of 3 treatment-naïve patients), with baseline HIV-1 RNA of at least 1500 copies/mL. One hundred and ten (110) patients were enrolled in a randomized, open-label 48-week clinical trial (Study 1182.14) and 25 patients were enrolled in other clinical studies including Expanded Access and Emergency Use Programs.
The adverse reactions profile seen in Study 1182.14 was similar to adults. Pyrexia (6.4%), vomiting (5.5%), cough (5.5%), rash (5.5%), nausea (4.5%), and diarrhea (3.6%) were the most frequently reported adverse reactions (Grade 2-4, all causes) in pediatric patients. Rash was reported more frequently in pediatric patients than in adults.
The most common Grade 3-4 laboratory abnormalities were increases in CPK (11%), ALT (6.5%), and amylase (7.5%).
Due to previous reports of both fatal and non-fatal intracranial hemorrhage (ICH), an analysis of bleeding events was performed. At 48 weeks of treatment, the frequency of pediatric patients with any bleeding adverse reactions was 7.5%. No drug related serious bleeding adverse reaction was reported. The most frequent bleeding adverse reaction was epistaxis (3.7%). No other bleeding adverse reaction was reported in frequency of > 1%. Additional trial follow-up through 100 weeks showed a cumulative 12% frequency of any bleeding adverse reaction.
Read the entire FDA prescribing information for Aptivus (Tipranavir) »
Additional Aptivus Information
Aptivus - User Reviews
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