Activase

• Generic Name: alteplase
• Brand Name: Activase

Activase (Alteplase) side effects drug center

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• Drug Comparison
  Streptase vs. Activase

 

PROFESSIONAL

CONSUMER

SIDE EFFECTS

• Overview
• Professional Information

 

Activase Side Effects Center

What Is Activase?

Activase (alteplase) is an enzyme, which works to break up and dissolve blood clots that can block arteries, used in the treatment of an acute heart attack or pulmonary embolism.

What Are Side Effects of Activase?

The most common side effect of Activase is bleeding, including gastrointestinal bleeding, genitourinary bleeding, bruising, nosebleed, and bleeding gums. Other side effects of Activase include:

• nausea,
• vomiting,
• low blood pressure (hypotension),
• dizziness,
• mild fever, or
• allergic reactions (swelling, rash, hives).

Dosage for Activase?

The recommended total dose of Activase is based upon patient weight, not to exceed 100 mg.

What Drugs, Substances, or Supplements Interact with Activase?

Activase may interact with blood thinners, or aspirin. Tell your doctor all medications and supplements you use.

Activase During Pregnancy and Breastfeeding

During pregnancy, Activase should be used only if prescribed. It is unknown if this drug is passes into breast milk. Consult your doctor before breastfeeding.

Additional Information

Our Activase (alteplase) Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication.

 

Activase Consumer Information

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Alteplase increases your risk of bleeding, which can be severe or fatal. Call your doctor or seek emergency medical attention if you have bleeding that will not stop. Bleeding may occur from a surgical incision, or from the skin where a needle was inserted during a blood test or while receiving injectable medication. You may also have bleeding on the inside of your body, such as in your stomach or intestines, kidneys or bladder, brain, or within the muscles.

Call your doctor or get emergency medical help if you have signs of bleeding, such as:

• sudden headache, feeling very weak or dizzy;
• bleeding gums, nosebleeds;
• easy bruising;
• bleeding from a wound, incision, catheter, or needle injection;
• bloody or tarry stools, coughing up blood or vomit that looks like coffee grounds;
• red or pink urine;
• heavy menstrual periods or abnormal vaginal bleeding; or
• sudden numbness or weakness (especially on one side of the body), slurred speech, problems with vision or balance.

Also call your doctor at once if you have:

• chest pain or heavy feeling, pain spreading to the jaw or shoulder, nausea, sweating, general ill feeling;
• swelling, rapid weight gain, little or no urination;
• severe stomach pain, nausea, and vomiting;
• darkening or purple discoloration of your fingers or toes;
• very slow heartbeats, shortness of breath, feeling light-headed;
• sudden severe back pain, muscle weakness, numbness or loss of feeling in your arms or legs;
• increased blood pressure--severe headache, blurred vision, pounding in your neck or ears, anxiety, nosebleed; or
• pancreatitis--severe pain in your upper stomach spreading to your back, nausea and vomiting.

Bleeding is the most common side effect of alteplase.

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 Activase (Alteplase)

 

Activase Professional Information

SIDE EFFECTS

The following adverse reactions are discussed in greater detail in the other sections of the label:

• Bleeding [see CONTRAINDICATIONS, WARNINGS AND PRECAUTIONS]
• Orolingual Angioedema [see WARNINGS AND PRECAUTIONS]
• Cholesterol Embolization [see WARNINGS AND PRECAUTIONS]
• Reembolization of Deep Venous Thrombi during Treatment for Acute Massive Pulmonary Embolism [see WARNINGS AND PRECAUTIONS].

Clinical Trials Experience

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.

The most frequent adverse reaction associated with Activase in all approved indications is bleeding.

Bleeding

Acute Ischemic Stroke (AIS)

In clinical studies in patients with AIS (Studies 1 and 2) the incidence of intracranial hemorrhage, especially symptomatic intracranial hemorrhage, was higher in Activase-treated patients than in placebo patients. A dose-finding study of Activase suggested that doses greater than 0.9 mg/kg may be associated with an increased incidence of intracranial hemorrhage.

The incidence of all-cause 90-day mortality, intracranial hemorrhage, and new ischemic stroke following Activase treatment compared to placebo are presented in Table 3 as a combined safety analysis (n=624) for Studies 1 and 2. These data indicate a significant increase in intracranial hemorrhage following Activase treatment, particularly symptomatic intracranial hemorrhage within 36 hours. There was no increase in the incidences of 90-day mortality or severe disability in Activasetreated patients compared to placebo.

Table 3 : Combined Safety Outcomes for Studies 1 and 2


	Placebo (n= 312)	Activase (n=312)	p-Value*
All-Cause 90-day Mortality	64 (20.5%)	54 (17.3%)	0.36
Total ICH†	20 (6.4%)	48 (15.4%)	<0.01
Symptomatic	4 (1.3%)	25 (8.0%)	<0.01
Asymptomatic	16 (5.1%)	23 (7.4%)	0.32
Symptomatic Intracranial Hemorrhage within 36 hours	2 (0.6%)	20 (6.4%)	<0.01
New Ischemic Stroke (3-months)	17 (5.4%)	18 (5.8%)	1.00
*Fisher's Exact Test. †Within trial follow-up period. Symptomatic intracranial hemorrhage was defined as the occurrence of sudden clinical worsening followed by subsequent verification of intracranial hemorrhage on CT scan. Asymptomatic intracranial hemorrhage was defined as intracranial hemorrhage detected on a routine repeat CT scan without preceding clinical worsening.

Bleeding events other than intracranial hemorrhage were noted in the studies of AIS and were consistent with the general safety profile of Activase. In Studies 1 and 2, the frequency of bleeding requiring red blood cell transfusions was 6.4% for Activase-treated patients compared to 3.8% for placebo (p = 0.19).

Although exploratory analyses of Studies 1 and 2 suggest that severe neurological deficit (National Institutes of Health Stroke Scale [NIHSS > 22]) at presentation was associated with an increased risk of intracranial hemorrhage, efficacy results suggest a reduced but still favorable clinical outcome for these patients.

Acute Myocardial Infarction (AMI)

For the 3-hour infusion regimen in the treatment of AMI, the incidence of significant internal bleeding (estimated as > 250 mL blood loss) has been reported in studies in over 800 patients (Table 4). These data do not include patients treated with the Activase accelerated infusion.

Table 4 : Incidence of Bleeding in 3-Hour Infusion in AMI Patients


	Total Dose ≤100 mg
Gastrointestinal	5%
Genitourinary	4%
Ecchymosis	1%
Retroperitoneal	<1%
Epistaxis	<1%
Gingival	<1%

The incidence of intracranial hemorrhage in AMI patients treated with Activase is presented in Table 5.

Table 5 : Incidence of Intracranial Hemorrhage in AMI Patients


Dose	Number of Patients	Intracranial Hemorrhage (%)
100 mg, 3-hour	3272	0.4
≤ 100 mg, accelerated	10,396	0.7
150 mg	1779	1.3
1-1.4 mg/kg	237	0.4

A dose of 150 mg or greater should not be used in the treatment of AMI because it has been associated with an increase in intracranial bleeding.

Pulmonary Embolism (PE)

For acute massive pulmonary embolism, bleeding events were consistent with the general safety profile observed with Activase treatment of AMI patients receiving the 3-hour infusion regimen.

Allergic Reactions

Allergic-type reactions, e.g., anaphylactoid reaction, laryngeal edema, orolingual angioedema, rash, and urticaria have been reported. When such reactions occur, they usually respond to conventional therapy.

Post-Marketing Experience

The following adverse reactions have been identified during post-approval use of Activase. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. These reactions are frequent sequelae of the underlying disease, and the effect of Activase on the incidence of these events is unknown.

Acute Ischemic Stroke

Cerebral edema, cerebral herniation, seizure, new ischemic stroke. These events may be life threatening and may lead to death.

Acute Myocardial Infarction

Arrhythmias, AV block, cardiogenic shock, heart failure, cardiac arrest, recurrent ischemia, myocardial reinfarction, myocardial rupture, electromechanical dissociation, pericardial effusion, pericarditis, mitral regurgitation, cardiac tamponade, thromboembolism, pulmonary edema. These events may be life threatening and may lead to death. Nausea and/or vomiting, hypotension and fever have also been reported.

Pulmonary Embolism

Pulmonary reembolization, pulmonary edema, pleural effusion, thromboembolism, hypotension. These events may be life threatening and may lead to death. Fever has also been reported.

Read the entire FDA prescribing information for Activase (Alteplase)



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