Generic Name

Methotrexate
Trade Name
Folex

Pharmacologic
Class
Folic acid antagonist

Minimum Dose
7.5 mg 1 tab
BID

Therapeutic Class
Antimetabolite.
Antineoplastic,
Antipsoriatic,
Antirheumatic

Maximum
Dose
15 mg 1 tab q6

Pregnancy Risk
Factor
X

Contents
Methotrexate
Availability
and color

- Tablets- 2.5, 5, 7.5

10, 15mg
- Powder for
injection- 20 mg, 1 g
per vial
- Injection- 25 mg/mL

Routes of
administration
Oral
Intramuscular
Intravenous

Inhibits folic acid reductase,

leading to inhibition of DNA
synthesis and inhibition of
cellular replication; selectively
affects the most rapidly
dividing cells (neoplastic and
psoriatic cells)
Pharmacokinetics
A: Rapidly absorbed from the
GI tract at low doses, higher
doses are less well absorbed.
Rapidly and completely
absorbed after IM doses.
D: Tissues and extracellular
fluids; crosses the blood-brain
barrier and placenta; enters
breast milk. Small amounts in
saliva and breast milk. 50%
bound to plasma proteins.
Bound as polyglutamate
conjugates, bound drug may
remain in the body for several
mth, particularly in the liver.
M: Partly by intestinal flora.
Does not undergo significant
metabolism at low dose
therapy; 7-hydroxy metabolite
is detected at high-doses.
E: Primarily via urine; small
amounts in bile, feces.
Rout
e
Oral
IM
IV

Onse
t
Varie
s
Rapi
d
Rapi
d

Peak
1-2 hr
0.5-1
hr
0.5-1
hr

Drug Half Life

3-15 hr

Duratio
n
Unknow
n
Unknow
n
Unknow
n

General Indications
- Burkitt's lymphoma
- Acute lymphoblastic
leukaemia
- Choriocarcinoma
- Mycosis fungoides
- Psoriasis
- Rheumatoid arthritis
- Crohn's disease
- Osteosarcoma
- Breast cancer
- Advanced
lymphosarcoma
- Acute lymphoblastic
leukaemia
- Choriocarcinoma
- Acute lymphoblastic
leukaemia
- Mycosis fungoides
- Crohn's disease
- Psoriasis
- Meningeal leukaemia
- Hydatidiform mole

Concentrations
- Pregnancy
- Lactation
- Alcoholism
- Chronic liver
disease
- Immune
deficiencies
- Blood dyscrasias
- Hypersensitivity
Precaution
- Renal disease
- Infection
- Peptic ulcer
- Ulcerative colitis
- Debility
Drug interaction
Drug to drug
- Potentially serious
to fatal reactions
when given with
NSAIDs
- Risk for toxicity
with alcohol
- Increased risk of
toxicity with
salicylates,
probenecid,
sulfonamides
- Decreased serum
levels and
therapeutic effects of
digoxin
- May decrease
theophylline
clearance
Drug to food
- none reported

CNS: Headache,
drowsiness, blurred vision,
aphasia, hemiparesis,
paresis, seizures, fatigue,
malaise, dizziness
Dermatologic:
Erythematous rashes,
pruritus, urticaria,
photosensitivity,
depigmentation, alopecia,
ecchymosis, telangiectasia,
acne, furunculosis
GI: Ulcerative stomatitis,
gingivitis, pharyngitis,
anorexia, nausea, vomiting,
diarrhea, hematemesis,
melena, GI ulceration,
bleeding, enteritis, hepatic
toxicity
GU: Renal failure, effects on
fertility
Hematologic: Severe bone
marrow depression,
increased susceptibility to
infection
Hypersensitivity:
Anaphylaxis, sudden death
Respiratory: Interstitial
pneumonitis, chronic
interstitial obstructive
pulmonary disease
Other: Chills and fever,
metabolic changes, cancer

Before
- Observe 15 rights in drug
administration.
- Assess for contraindications of the
drug.
- Arrange for tests to evaluate CBC
urinalysis, renal and liver function
tests, and chest X-ray before
therapy.
- Ensure that patient is not pregnan
before administering.
- Prepare a calendar of treatment
days.

During
- Arrange for tests to evaluate CBC
urinalysis, renal and liver function
tests, and chest X-ray during
therapy.
- Do not administer any other
medications containing alcohol.
- Arrange for adequate hydration
during therapy to reduce risk of
hyperuricemia.
- Arrange to have leucovrin readily
available as antidote for
methotrexate overdose.
- Instruct to use contraceptives
during therapy.

After
- Arrange for tests to evaluate CBC
urinalysis, renal and liver function
tests, and chest X-ray several
weeks after therapy.
- Instruct to report black tarry
stools, fever, chills, sore throat,
unusual bleeding or bruising, cough
or shortness of breath, darkened or
bloody urine, abdominal, flank or
joint pain, jaundice symptoms,
mouth sores.
- Arrange for an antiemetic if
nausea and vomiting is severe.

- Reduce dosage or discontinue if

renal failure occurs.
- Arrange for frequent, regular
medical check-ups.

Source:
Karch, Amy: 2009
Lippincotts Nursing
Drug Guide, p. 767768

Source:
http://www.keele.ac.uk/
Karch, Amy: 2009
Lippincotts Nursing Drug
Guide, p. 767

Source:
http://mims.com.ph/, Karch, Amy: 2009
Lippincotts Nursing Drug Guide, p.
768

Source:
http://mims.com.ph/

Source:
Karch, Amy: 2009
Lippincotts Nursing Drug
Guide, p. 769

Source:
Karch, Amy: 2009 Lippincotts
Nursing Drug Guide, p. 769

Source:
Karch, Amy: 2009 Lippincotts Nursing Drug
Guide, p. 769