Baclofen, Uses, Dosage, Side Effects, Interactions ,Pregnancy

Baclofen
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Baclofen’s mechanism of action is not fully understood, but it is believed that the drug works mainly at the level of the spinal cord to block polysynaptic afferent pathways and, to a lesser extent, monosynaptic afferent pathways. Baclofen may inhibit the transmission of impulses through these pathways by acting as an inhibitory neurotransmitter itself or by hyperpolarizing the primary afferent nerve terminals, which inhibits the release of excitatory neurotransmitters such as glutamate and aspartic acids. Because of large doses of baclofen cause CNS depression, it is postulated that the drug works at supraspinal sites as well. Baclofen has been described as a gamma-aminobutyric acid (GABA) agonist; the drug stimulates the GABA-B receptor. This leads to a decreased release of the neurotransmitters aspartate and glutamate and decreased excitatory input into alpha-motor neurons.

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Baclofen is a direct agonist at GABAB receptors. The precise mechanism of action of Baclofen is not fully known. It is capable of inhibiting both monosynaptic and polysynaptic reflexes at the spinal level, possibly by hyperpolarization of afferent terminals, although actions at supraspinal sites may also occur and contribute to its clinical effect.

Baclofen is a muscle relaxant and antispastic. Baclofen is useful for the alleviation of signs and symptoms of spasticity resulting from multiple sclerosis, particularly for the relief of flexor spasms and concomitant pain, clonus, and muscular rigidity. Although Baclofen is an analog of the putative inhibitory neurotransmitter gamma-aminobutyric acid (GABA), there is no conclusive evidence that actions on GABA systems are involved in the production of its clinical effects. In studies with animals, Baclofen has been shown to have general CNS depressant properties as indicated by the production of sedation with tolerance, somnolence, ataxia, and respiratory and cardiovascular depression. Baclofen is rapidly and extensively absorbed and eliminated. Absorption may be dose-dependent, being reduced with increasing doses. Baclofen is excreted primarily by the kidney in unchanged form and there is relatively large intersubject variation in absorption and/or elimination.
Baclofen is a synthetic chlorophenyl-butanoic acid derivative used to treat spasms due to spinal cord damage and multiple sclerosis, muscle-relaxing Baclofen acts as a gamma-aminobutyric acid (GABA) agonist specific for GABA-B receptors. It acts at spinal and supraspinal sites, reducing excitatory transmission. 

Indications of Baclofen

These medicines work by acting on the central nervous system and may be used for the relief of muscle spasms, cramping or tightness caused by diseases such as

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Contra Indications of Baclofen

Dosage of Baclofen

Strengths : 10 mg; 20 mg; 0.05 mg/mL; 0.5 mg/mL;

Spasticity

  • Initial dose: The following gradually increasing dosage regimen is suggested, but should be adjusted to suit individual patient requirements:
  • 5 mg orally 3 times a day for 3 days, then 10 mg orally 3 times a day for 3 days, then 15 mg orally 3 times a day for 3 days, then 20 mg orally 3 times a day for 3 days
  • Maintenance dose: Should be individualized.
  • Maximum dose: 80 mg/day (20 mg orally 4 times a day)

Cerebral Spasticity

  • First Screening Dose: 50 mcg (in a volume of 1 mL) administered into the intrathecal space by barbotage over at least 1 minute; observe patient for 4 to 8 hours for a positive response
  • Second Screening Dose: (if no positive response to first screening dose): 75 mcg (in a volume of 1.5 mL) bolus dose administered 24 hours after the first screening dose; observe the patient for 4 to 8 hours for a positive response
  • Third Screening Dose: (if no positive response to second screening dose): 100 mcg (in a volume of 2 mL) bolus dose administered 24 hours after the second screening dose; observe patient for 4 to 8 hours for a positive response; if no positive response to third screening dose, the patient should not be considered for chronic intrathecal therapy.
  • No dose increases should be given in the first 24 hours (i.e., until a steady state is achieved).
  • After the first 24 hours, the daily dosage should be increased slowly by 10% to 30% increments and only once every 24 hours, until the desired effect is achieved.
  • After the first 24 hours, the daily dose should be increased slowly by 5% to 15% only once every 24 hours, until the desired effect is achieved.

Intrathecal mainteinance dosing

  • During periodic refills of the pump, the daily dose may be increased by 10% to 40%, but no more than 40%, to maintain adequate symptom control.
  • The daily dose may be reduced by 10% to 20% if patients experience side effects; most patients require gradual increases in dose to maintain optimal response during chronic therapy
  • Maintenance dosage for long-term continuous infusion: 12 to 2003 mcg/day, with most patients, adequately maintained on 300 to 800 mcg/day; there is limited experience with daily doses greater than 1000 mcg/day.

Intrathecal mainteinance dosing for spasticity of cerebral origin

  • During periodic refills of the pump, the daily dose may be increased by 5% to 20%, but no more than 20%, to maintain adequate symptom control.
  • The daily dose may be reduced by 10% to 20% if patients experience side effects; most patients require gradual increases in dose to maintain optimal response during chronic therapy.
  • Maintenance dosage for long term continuous infusion: 22 to 1400 mcg/day, with most patients adequately maintained on 90 to 703 mcg/day; there is limited experience with daily doses greater than 1000 mcg/day.

Potential need for dosage adjustment in chronic use

  • During long term treatment, approximately 5% of patients become refractory to increasing doses. There is not sufficient experience to make recommendations for tolerance treatment; however, tolerance has been treated on occasion, in hospital, by a “drug holiday” consisting of the gradual reduction of intrathecal dosing over a 2 to 4-week period and switching to alternative methods of spasticity management
  • After the “drug holiday,” intrathecal dosing may be restarted at the initial continuous infusion dose.

Spinal Spasticity

Intrathecal screening phase

  • Prior to pump implantation for chronic infusion, patients must show a positive response to an intrathecal bolus dose in a screening trial.
  • First Screening Dose: 50 mcg (in a volume of 1 mL) administered into the intrathecal space by barbotage over at least 1 minute; observe patient for 4 to 8 hours for a positive response.
  • Second Screening Dose: (if no positive response to first screening dose): 75 mcg (in a volume of 1.5 mL) bolus dose administered 24 hours after the first screening dose; observe patient for 4 to 8 hours for a positive response
  • Third Screening Dose: (if no positive response to second screening dose): 100 mcg (in a volume of 2 mL) bolus dose administered 24 hours after the second screening dose; observe patient for 4 to 8 hours for a positive response; if no positive response to third screening dose, the patient should not be considered for chronic intrathecal therapy
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Intrathecal Post implant dose titration period

  • The screening dose that received a positive response should be doubled and administered over 24 hours, unless the efficacy of the bolus dose was maintained for more than 8 hours, in which case the starting daily dose should be the screening dose delivered over 24 hours.
  • No dose increases should be given in the first 24 hours (i.e., until steady state is achieved).
  • After the first 24 hours, the daily dosage should be increased slowly by 10% to 30% increments and only once every 24 hours, until the desired effect is achieved.
  • After the first 24 hours, the daily dose should be increased slowly by 5% to 15% only once every 24 hours, until the desired effect is achieved.

Intrathecal maintenance dosing for spasticity of spinal cord

  • During periodic refills of the pump, the daily dose may be increased by 10% to 40%, but no more than 40%, to maintain adequate symptom control.
  • The daily dose may be reduced by 10% to 20% if patients experience side effects; most patients require gradual increases in dose to maintain optimal response during chronic therapy
  • Maintenance dosage for long term continuous infusion: 12 to 2003 mcg/day, with most patients adequately maintained on 300 to 800 mcg/day; there is limited experience with daily doses greater than 1000 mcg/day.
Maintenance dosing for spasticity of cerebral origin
  • During periodic refills of the pump, the daily dose may be increased by 5% to 20%, but no more than 20%, to maintain adequate symptom control.
  • The daily dose may be reduced by 10% to 20% if patients experience side effects; most patients require gradual increases in dose to maintain optimal response during chronic therapy.
  • Maintenance dosage for long term continuous infusion: 22 to 1400 mcg/day, with most patients adequately maintained on 90 to 703 mcg/day; there is limited experience with daily doses greater than 1000 mcg/day.

Potential need for dose adjustment in chronic use

  • During long term treatment, approximately 5% of patients become refractory to increasing doses.
  • There is not sufficient experience to make recommendations for tolerance treatment; however, tolerance has been treated on occasion, in hospital, by a “drug holiday” consisting of the gradual reduction of intrathecal dosing over a 2 to 4-week period and switching to alternative methods of spasticity management.After the “drug holiday,” intrathecal dosing may be restarted at the initial continuous infusion dose.

Spasticity

12 years and older

  • Initial dose: The following gradually increasing dosage regimen is suggested, but should be adjusted to suit individual patient requirements:
  • 5 mg orally 3 times a day for 3 days, then 10 mg orally 3 times a day for 3 days, then 15 mg orally 3 times a day for 3 days, then 20 mg orally 3 times a day for 3 days
  • Maintenance dose: Should be individualized.
  • Maximum dose: 80 mg/day (20 mg orally 4 times a day)

For Hiccup

  • If the hiccup are reached the severe condition the beclofen 5 mg tab  twich daily for 7 day. It must be come in control gradually

Pediatric Cerebral Spasticity

4 years and older ; The starting screening dose for pediatric patients is the same as in adult patients, (50 mcg); however, for very small patients, a screening dose of 25 mcg may be tried first

Intra thecal screening

  • Prior to pump implantation for chronic infusion, patients must show a positive response to an intrathecal bolus dose in a screening trial.
  • First Screening Dose: 25 to 50 mcg (in a volume of 1 mL) administered into the intrathecal space by barbotage over at least 1 minute; observe patient for 4 to 8 hours for a positive response
  • Second Screening Dose: (if no positive response to first screening dose): 75 mcg (in a volume of 1.5 mL) bolus dose administered 24 hours after the first screening dose; observe patient for 4 to 8 hours for a positive response
  • Third Screening Dose: (if no positive response to second screening dose): 100 mcg (in a volume of 2 mL) bolus dose administered 24 hours after the second screening dose; observe patient for 4 to 8 hours for a positive response; if no positive response to third screening dose, the patient should not be considered for chronic intrathecal therapy.
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Maintenance dose
The same dosing recommendations for adults with spasticity of cerebral origin are used in pediatric patients 4 years and older

  • During periodic refills of the pump, the daily dose may be increased by 5% to 20%, but no more than 20%, to maintain adequate symptom control.
  • The daily dose may be reduced by 10% to 20% if patients experience side effects.

Maintenance dosage for long term continious infusion

  • Pediatric patients 4 to under 12 years may require a lower daily dose: 274 mcg/day, with a range of 24 to 1199 mcg/day
  • Age 12 years and older: 22 to 1400 mcg/day, with most patients adequately maintained on 90 to 703 mcg/day; there is limited experience with daily doses greater than 1000 mcg/day

Side effects of Baclofen

More common

Common

Rare

Drug Interactions of Baclofen

Baclofen may interact with following drugs, supplyments, & may change the efficacy of drugs

Pregnancy & Lactation of 

FDA Pregnancy Category C

Pregnancy

It is not known if baclofen is safe and effective for use in pregnant women. Tell your doctor if you’re pregnant or plan to become pregnant. Baclofen should be used during pregnancy only if the potential benefit justifies the potential risk.Call your doctor right away if you become pregnant while taking this drug.

Lactation

It isn’t known if baclofen passes into breast milk. If it does, it may cause side effects in a child who is breastfed. Talk to your doctor if you breastfeed your child. You may need to decide whether to stop breastfeeding or stop taking this medication.

References

    1. https://pubchem.ncbi.nlm.nih.gov

     

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