Baclofen
BP
Pharmacology:
Baclofen is an effective muscle relaxant and antispastic agent with a
spinal site of action. Its mode of action is not fully understood. Baclofen
inhibits both monosynaptic and polysynaptic reflexes at the spinal level by
stimulating the GABAB-receptors, which inhibits the release of glutamate and
aspartate. It may also act at intraspinal sites producing CNS depression.
Neuromuscular transmission is not affected by
Baclofen.
Baclofen also exerts antinociceptive effect.
Indication:
Baclofen is indicated for
· Spasm
· Reflex
muscle contractions
· Spasticity
resulting from multiple sclerosis
· Skeletal
muscle spasm resulting from rheumatic disorders
· Flexor
spasms and concomitant pain,clonus and muscular rigidity
· Spinal
cord injuries and other spinal cord diseases
· Cerebrovascular
accidents or neoplastic or degenerative brain disease
· Tension
type headache
Dosage
& administration: Adult The initial dose of baclofen is 5
mg three times daily by mouth preferably with or after food or milk-The total
daily dose is increased by 15 mg every fourth day (i.e. the dosage regimen
is 5
mg 3 times a day for 3 days, then 10 mg 3 times a day for 3 days, then 15 mg 3
times a day for 3 days), until either a dose of 20 mg three times a day is
reached or until the desired therapeutic effect is obtained.
Children:
The usual dosage range for children is 0.75 to 2 mg/kg body weight per day. In
children aged over
10
years a maximum daily dose of 2.5 mg/kg body weight may be given. The usual
starting dose is 2.5 mg given four times daily increased cautiously about every
three days until the desired therapeutic effect is obtained. The recommended
daily maintenance doses are: 12
months
to 2 years of age, 10 to 20 mg; 2 to 6 years, 20 to 30 mg; 6 to 10 years, 30 to
60 mg.
Contraindication:
Baclofen is contraindicated in patients who are hypersensitive to any
component of this product.
Precaution:
Baclofen stimulates gastric acid secretion and should be used with
caution in patients with a history of peptic ulcer and avoided in those with
active peptic ulcer disease, Liver function should be
monitored
in patients with liver disease, patients with renal impairment need a reduced
dose.
Baclofen
should be used with caution in patients with respiratory impairment. Baclofen
may cause
drowsiness,
patients affected should not drive
or
operate machinery.
Side
Effect: The most common side effects include day time
drowsiness, sedation, lethargy, dizziness,
headache,
nausea and diarrhea. Other infrequent side-effects are muscular hypotonia,
urinary
disturbances,
confusion, speech disturbance, insomnia, depression, anxiety, agitation,
myalgia, fever,
respiratory
depression, hypotension, dry mouth, sexual dysfunction, visual disorders, rash,
pruritis, weight
gain,
taste alterations, blood sugar changes.
Drug
Interaction: Alcohol and other CNS depressants may exacerbate
the CNS effects of baclofen and
should
be avoided, severe aggravation of hyperkinetic symptoms may possibly occur in
patients taking lithium,
Ibuprofen
and other drugs that produce renal insufficiency may reduce baclofen excretion
leading to toxicity.
Use
in Pregnancy and Lactation: The safety of baclofen in women who are or who may
become pregnant has
not
been established. Baclofen crosses the placental barrier. Baclofen should be
used during pregnancy only if
the
potential benefit justifies the potential risk to the fetus. Baclofen is
excreted in breast milk however
evidence
to date suggests that the quantities are so small that no undesirable effects
on the infant would be
expected.
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