LEUCOVORIN CALCIUM tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

LEUCOVORIN CALCIUM (UNII: RPR1R4C0P4) (LEUCOVORIN - UNII:Q573I9DVLP)

Available from:

Teva Pharmaceuticals USA, Inc.

INN (International Name):

LEUCOVORIN CALCIUM

Composition:

LEUCOVORIN 5 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Leucovorin calcium tablets are indicated to diminish the toxicity and counteract the effects of impaired methotrexate elimination and of inadvertent overdosages of folic acid antagonists. Leucovorin is improper therapy for pernicious anemia and other megaloblastic anemias secondary to the lack of vitamin B12 . A hematologic remission may occur while neurologic manifestations continue to progress.

Product summary:

Leucovorin Calcium Tablets USP, 5 mg are available as white, round, unscored, biconvex tablets, debossed with b on one side and 484 on the other side, packaged in bottles of 30 (NDC 0555-0484-01), 100 (NDC 0555-0484-02) and 1000 (NDC 0555-0484-05) tablets. Leucovorin Calcium Tablets USP, 25 mg are available as pale green, round, unscored, biconvex tablets, debossed with b on one side and 485 on the other side, packaged in bottles of 25 (NDC 0555-0485-27) and 500 (NDC 0555-0485-04) tablets. Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]. Dispense in a tight, light-resistant container as defined in the USP, with a child-resistant closure (as required). Protect from light and moisture. KEEP THIS AND ALL MEDICATIONS OUT OF THE REACH OF CHILDREN.

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

LEUCOVORIN CALCIUM- LEUCOVORIN CALCIUM TABLET
TEVA PHARMACEUTICALS USA, INC.
----------
LEUCOVORIN CALCIUM TABLETS USP
RX ONLY
DESCRIPTION
Leucovorin Calcium Tablets USP contain either 5 mg or 25 mg leucovorin
as the calcium
salt of _N_-[4-[[(2-amino-5-formyl-1, 4, 5, 6, 7,
8-hexahydro-4-oxo-6-pteridinyl)methyl]
amino]benzoyl]-_L_-glutamic acid. This is equivalent to 5.4 mg or
27.01 mg of anhydrous
leucovorin calcium, respectively. In addition, each tablet contains
the following inactive
ingredients: colloidal silicon dioxide, croscarmellose sodium, lactose
monohydrate,
magnesium stearate, and microcrystalline cellulose. The 25 mg tablet
also contains D&C
yellow no. 10 aluminum lake and FD&C blue no. 1 aluminum lake.
Leucovorin is a water soluble form of reduced folate in the folate
group; it is useful as an
antidote to drugs which act as folic acid antagonists. These tablets
are intended for oral
administration only.
The structural formula is as follows:
C
H
CaN O M.W. 511.5
CLINICAL PHARMACOLOGY
Leucovorin is a racemic mixture of the diastereoisomers of the
5-formyl derivative of
tetrahydrofolic acid. The biologically active compound of the mixture
is the (-)-_L_-isomer,
known as _Citrovorum factor_, or (-)-folinic acid. Leucovorin does not
require reduction by
the enzyme dihydrofolate reductase in order to participate in
reactions utilizing folates as
a source of “one-carbon” moieties. Following oral administration,
leucovorin is rapidly
absorbed and enters the general body pool of reduced folates. The
increase in plasma
and serum folate activity (determined microbiologically with
_Lactobacillus casei_) seen
20
21
7
7
after oral administration of leucovorin is predominantly due to
5-methyltetrahydrofolate.
Twenty normal men were given a single, oral 15 mg dose (7.5 mg/m ) of
leucovorin
calcium and serum folate concentrations were assayed with _L. casei_.
Mean values
observed (± one standard error) were:
a. Time to peak serum folate concentration: 1.72 ± 0.08 hours,
b. Peak serum folate concentration achi