Alteplase, Recombinant (Intravenous)

Alteplase Recombinant is a purified and sterile glycoprotein comprising of 527 amino acids and is used to dissolve blood clots that may have formed in blood vessels. Here is more information about it.

Overview

Alteplase is synthesized by recombinant DNA technology and is available in the U.S. under the brand name Activase and Cathflo Activase. The drug dissolves blood clots in catheters placed in large blood vessels. It is administered soon after symptoms of a heart attack and a stroke and when blood clots are suspected to have formed in the lungs (Pulmonary Embolism).

It is a drug of the therapeutic class, thrombolytic and the pharmacologic class, tissue plasminogen activator. It is a white to off-white, sterile, freeze-dried powder used to make a solution for intravenous administration. It is administered only by a trained healthcare professional.

Conditions Treated

Type of Medicine

  • Thrombolytic

Side Effects

The following are side effects of taking Alteplase, recombinant that are common and of which a doctor should be notified immediately if they occur.

  • Bleeding from wounds and puncture sites
  • Coughing up blood
  • Difficulties breathing
  • Dizziness
  • Bleeding gums
  • Headache
  • Vaginal bleeding or increased menstrual flow
  • Prolonged bleeding from cuts
  • Nosebleeds
  • Paralysis
  • Black or red tarry stools
  • Dark brown or red urine

The following are rarely seen adverse effects and should be reported to a doctor as soon as they occur.

  • Confusion
  • Chills
  • Fainting: at times this may happen suddenly
  • Racing heartbeat
  • Redness, pain or swelling in the legs or arms
  • Pain in the groin, chest, and legs, especially the calves
  • Shallow and rapid breathing
  • Slurred speech
  • A severe headache that starts suddenly
  • Loss of coordination which happens suddenly
  • Sudden and severe numbness or weakness in the arms and legs which occurs suddenly
  • Shortness of breath that is sudden and unexplainable
  • Changes in vision

The incidence of the following symptoms is not known, but a doctor should be notified immediately if they are observed.

  • Anxiety
  • The patient's skin may turn blue and pale, at times on the fingernails and lips
  • Blurred vision
  • Discomfort or pain in the chest. The patient may also experience chest pain that feels like it is moving to the left arm, neck or shoulder
  • Convulsions
  • Sweaty, cool skin
  • A cough, at times producing frothy, pink sputum
  • Neck veins that are dilated
  • The patient may notice a decrease in urine output and loss of bladder control
  • Extreme fatigue
  • Welts or hives, itching or skin rash
  • Hoarseness
  • Increased sweating
  • The patient may notice hive-like swellings that are large on the lips, mouth or tongue
  • The patient may experience jerking of extremities and muscle spasms
  • Vomiting or nausea
  • Swelling or puffiness around the eyes, or on the eyelids, lips, face or tongue
  • The skin may be seen to redden
  • Irregular or slow heartbeat or breathing
  • Sweating
  • Weight gain

All of the above are by no means all the unwanted effects that may occur after the use of Alteplase. A doctor should be informed of all the side effects experienced for proper medical advice. Adverse effects can also be reported to the FDA on 1-800-FDA-1088.

Dosage

  1. Acute Ischemic Stroke dosing

Alteplase should be administered as soon as is possible after symptoms are seen but at least within 3 hours of the onset of symptoms.

The maximum dose given should not exceed 90mg, though the recommended dosage is 0.9mg/Kg. 10% of the entire dose should be administered within 1 minute as the initial intravenous bolus. The remaining drug should be given within 60 minutes.

Blood pressure should frequently be measured and monitored during this treatment.

  1. Acute Myocardial Infarction

Alteplase should be administered as soon as symptoms are observed. Dosage is determined by the weight of the patient but must not exceed 100mg, irrespective of the selected administration regime. For this condition, the drug can be administered in two ways:

  • Accelerated Infusion
  • 3-Hour Infusion

In accelerated infusion, the doses are as follows:

For patients greater than or equal to 67kgs in weight, the first intravenous bolus of 15mg should be administered as soon as possible. This should be followed by 50mg in the next 30 minutes and 35mg within the next 60 minutes.

For patients less or equal to 67kgs of body weight, the first intravenous bolus should be 15mg administered as soon as possible. The second should be at a ratio of 0.75mg/kg, delivered within 30 minutes and the third at a rate of 0.5mg/kg administered within 60 minutes.

For the 3-Hour infusion:

For patients greater than 65kg, the dosage should be 100mg. 60mg should be administered in the first hour, with 6-10mg administered as a bolus. 20mg should be administered in the second hour and the remainder in the third hour.

Patients who weigh less than 65kgs should have a dose of 1.25mg/kg administered over 3 hours. A bolus should be administered first at the ratio of 0.075mg/kg. During the rest of the first hour, the patient should get 0.675mg/kg and 0.25mg/kg in the second and third hours.

  1. Pulmonary Embolism

Using the intravenous infusion method of administration, 100mg of the drug should be given over a two hour period.

No data is available for the dose adjustments required when administering Alteplase for patients with liver or renal impairments and those undergoing dialysis.

Interactions

Alteplase interacts with 226 drugs (899 generic and brand names). 92 generic and brand names, which are 40 distinct drugs, have major interactions with alteplase. Of 801 generic and brand names, 180 different drugs have moderate interactions with alteplase. 6 drugs have minor interactions with alteplase.

The type of interactions mentioned above can be explained as follows:

  • Major interactions are highly clinically significant. The risks of combining the drugs outweigh the benefits, and such drugs should never be used together.
  • Medications with moderate interactions should not be combined unless under exceptional circumstances. Such interactions are moderately clinically significant.
  • Medicines with minor interactions can be used together if steps are taken to reduce such interactions, or if a monitoring plan is instituted. Their interactions are minimally clinically significant.

The following drugs are often checked when in use with alteplase:

  • Acetylsalicylic acid (Aspirin)
  • Adrenalin (Epinephrine)
  • Amoxil (amoxicillin)
  • Ativan (Loraxepam)
  • Atrovent (Ipratropium)
  • Cardizem (Diltiazem)
  • Decadron (dexamethasone)
  • Dilaudid (hydromorphone)
  • Haldol (haloperidol)
  • Lasix (furosemide)
  • Lipitor (atorvastatin)
  • Lovenox (enoxaparin)
  • Normal Saline Flush (Sodium Chloride)
  • Paracetamol (acetaminophen)
  • Plavix (clopidogrel)
  • Protonix (pantoprazole)
  • Toradol (ketorolac)
  • Tylenol (acetaminophen)
  • Vicodin (acetaminophen/hydrocodone)
  • Zofran (Ondansetron)

Disease interactions

Alteplase should not be used if a patient has any one of the following medical conditions:

  • A history of bleeding from any body part or any bleeding problems
  • Arteriovenous malformation or an aneurysm or any other blood vessel problems
  • Brain disease or tumor
  • Uncontrolled high blood pressure (hypertension)
  • A history of strokes
  • Brain or spine injury or surgery within the last three months

If a patient has any one of the following, the chances of severe bleeding are increased:

  • A history of blood clots
  • Diabetic eye problems such as hemorrhagic retinopathy
  • Heart infections
  • Blood vessel injections
  • Severe kidney or liver disease
  • If the patient has a catheter in any part of their body.
  • Major, recent surgery or injury

Patients with a history of high cholesterol, deep venous thrombosis (blood clots in the leg) or a catheter infection have an increased risk of severe side effects.

Alteplase may also make heart rhythm problems worse.

Warnings

The patient should inform their doctor of any allergies to alteplase, or any other drugs.

The doctor should also be informed of any medical conditions that the patient may be suffering as well as therapies they may be undergoing. All OTC drugs, vitamins, mineral supplements and any other natural products that the patient may be using should also be listed for the doctor. This will help the doctor determine the safety of giving this medication.

There is the possibility of severe bleeding in some people after using this drug. The advice of the patient's doctor should be followed to help prevent any serious blood loss. Movement should also be reduced to a minimum and the patient should only get out of bed when informed it is safe to do so by his or her doctor.

Pregnancy Warning

Animal studies have shown adverse effects to the fetus after administering alteplase, or such studies have not been done. There are no adequate, well-controlled studies on pregnant women.

Breastfeeding Warnings

There are no adequate studies done on breastfeeding women to determine if this drug is passed in milk and if it poses a risk to a nursing infant. Most medicines are passed into human milk. The potential benefits of this drug to nursing women should be weighed against the dangers it poses to the child.

Storage

Alteplase should be stored at room temperature not exceeding 30 degrees C (86 degrees F) or under refrigeration between 2-8 degrees C (36-46 degrees F).

It should be protected from excessive exposure to light. When it is reconstituted, it must be used within 8 hours, and any unused portion discarded.

The expiry date is always stamped on the vial, and it should not be used after this.

Summary

Alteplase is useful for the conditions it is indicated for. However, after administration of this drug, the patient runs a risk of internal as well as external bleeding. The patient should be on the lookout for signs that might indicate bleeding, and a doctor notified immediately if any symptoms appear. Any other side effects that the patient experiences, as well health issues they may be suffering or begin to suffer from, must also be reported to the doctor.

The patient must not attempt to medicate themselves especially when they begin to experience adverse reactions. A doctor must be notified of all products the patient takes including natural products which might otherwise be deemed safe. Only a doctor can determine all possible interactions and assess safety of use.

All the information available on Alteplase is not contained here. The preceding information must be used for general purposes only and must not replace the advice of a doctor.

Resources
Last Reviewed:
December 10, 2017
Last Updated:
April 04, 2018