GENERIC NAME: alteplase
BRAND NAME: Activase; TPA
DRUG CLASS AND MECHANISM: Alteplase is an injectable drug,
given directly into a vein, that is used to treat conditions
caused by arterial blood clots including heart attacks,
strokes, chest pain at rest (unstable angina), blood clots
in the lungs (pulmonary thrombosis), and other less common
conditions involving blood clots. Alteplase is an enzyme
that occurs naturally in man and causes blood clots to
dissolve. It is a man-made protein manufactured by recombinant
DNA technology. The naturally occurring protein, known
as tissue plasminogen activator (TPA), is made by ovarian
cells from the Chinese hamster. The amount that is given
to patients is far greater than the amount naturally made
by the body itself. Alteplase was first approved for heart
attacks in 1987. In 1996, it was approved for strokes.
GENERIC AVAILABLE: no
PRESCRIPTION: yes
PREPARATIONS: Powder to be mixed with sterile water
for injection at concentrations of 50 mg/50 mL and 100mg/100
mL.
STORAGE: The vials are stored at room temperature up
to 80癋 (30癈) or under refrigeration at 2-8 癈 (36-46
癋). Once mixed with sterile water, it must be used immediately.
Any drug not used must be thrown away.
PRESCRIBED FOR: Alteplase is used to treat persons
with heart attacks (acute myocardial infarctions), strokes,
chest pain at rest (unstable angina), blood clots in
the lungs (pulmonary thrombosis or embolism), and other
less common conditions involving blood clots.
DOSING: Alteplase is injected intravenously. Depending
on the condition being treated, it is given once quickly
or as a brief infusion over 30 to 60 minutes.
DRUG INTERACTIONS: Alteplase breaks down clots and
thereby interferes with the body's ability to stop bleeding.
Therefore, drugs which also interfere with the body's
ability to form blood clots (or the clot-promoting effects
of platelets) increase the risk of bleeding in patients
receiving alteplase. Such medicines include warfarin
(Coumadin), aspirin, and nonsteroidal anti-inflammatory
drugs (NSAIDs) such as ibuprofen (Motrin), naproxen
(Naprosyn), and nabumetone (Relafen). Specific platelet
inhibitors, for example, clopidogrel (Plavix) do not
appear to interact with alteplase and increase the risk
of bleeding.
PREGNANCY: Alteplase has been shown to cause damage
to embryos of rabbits. No damage has been reported in
humans. Physicians must carefully balance potential
risks and possible benefits when prescribing alteplase
to pregnant women.
NURSING MOTHERS: It is not known whether alteplase
passes into breast milk.
SIDE EFFECTS: The most common and serious side effect
with alteplase is bleeding. Most commonly, such bleeding
is minor, but significant, even fatal bleeding has been
reported.
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