baclofen


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Related to baclofen: Tizanidine

baclofen

 [bak´lo-fen]
an analogue of γ-aminobutyric acid administered orally or intrathecally as a muscle relaxant and antispastic in the treatment of spasticity of spinal origin, such as multiple sclerosis or spinal cord injury. It is also used intrathecally to treat spasticity of cerebral origin, such as trauma to the brain or cerebral palsy.

baclofen

Apo-Baclofen (CA), Baclofen, Gen-Baclofen (CA), Kemstro, Lioresal, Lioresal Intrathecal, Liotec (CA), Lyflex (UK), Nu-Baclo (CA), PMS-Baclofen (CA)Colazal, Colazide (UK)

Pharmacologic class: Skeletal muscle relaxant

Therapeutic class: Antispasmodic

Pregnancy risk category C

Pharmacologic class: GI agent

Therapeutic class: Anti-inflammatory

Pregnancy risk category B

FDA Box Warning

• With intrathecal form, abrupt withdrawal may cause high fever, altered mental status, exaggerated rebound spasticity, and muscle rigidity; in rare cases, patient progresses to rhabdomyolysis, multisystem failure, and death. To prevent abrupt withdrawal, pay careful attention to programming and monitoring of infusion system, refill scheduling and procedures, and pump alarms. Advise patients and caregivers of importance of keeping scheduled refill visits, and teach about early drug withdrawal symptoms. Give special attention to patients at apparent risk (those with spinal cord injuries at T6 or above, communication problems, or history of withdrawal symptoms from oral or intrathecal baclofen).

Action

Relaxes muscles by acting specifically at spinal end of upper motor neurons

Availability

Intrathecal injection: 10 mg/20 ml (500 mcg/ml), 10 mg/5 ml (2,000 mcg/ml)

Tablets: 10 mg, 20 mg

Indications and dosages

Reversible spasticity associated with multiple sclerosis or spinal cord lesions

Adults: Initially, 5 mg P.O. t.i.d. May increase by 5 mg q 3 days to a maximum dosage of 80 mg/day.

Children ages 4 and older: 25 to 1,200 mcg/day by intrathecal infusion; (average is 275 mcg/day); dosage determined by response during screening phase.

Severe spasticity in patients who don't respond to or can't tolerate oral baclofen

Adults:Screening phase-Before pump implantation and intrathecal infusion, give test dose to check responsiveness. Administer 1 ml of 50 mcg/ml dilution over 1 minute by barbotage into intrathecal space. Within 4 to 8 hours, muscle spasms should become less severe or frequent and muscle tone should decrease; if patient's response is inadequate, give second test dose of 75 mcg/1.5 ml 24 hours after first dose. If patient is still unresponsive, may give final test dose of 100 mcg/2 ml 24 hours later. Patients unresponsive to 100-mcg dose aren't candidates for intrathecal baclofen. Following appropriate responsiveness, adjust dosage to twice the screening dose and give over 24 hours. If screening dose efficacy is maintained for 12 hours, don't double the dosage. After 24 hours, increase dosage slowly as needed and tolerated by 10% to 30% daily.

Maintenance therapy-During prolonged maintenance therapy, adjust daily dosage by 10% to 40% as needed and tolerated to maintain adequate control of symptoms. Maintenance dosage ranges from 12 mcg to 2,000 mcg daily.

Dosage adjustment

• Renal impairment
• Seizure disorders
• Elderly patients

Off-label uses

• Cerebral palsy
• Tardive dyskinesia
• Trigeminal neuralgia

Contraindications

• Hypersensitivity to drug
• Rheumatic disorders

Precautions

Use cautiously in:
• renal impairment
• epilepsy
• patients who use spasticity to maintain posture and balance
• elderly patients
• pregnant or breastfeeding patients
• children.

Administration

• Give oral doses with food or milk.
• Dilute only with sterile, preservative-free sodium chloride for injection.
• Know that intrathecal infusion should be performed only by personnel who have been trained in the procedure.

Adverse reactions

CNS: dizziness, drowsiness, fatigue, confusion, depression, headache, insomnia, hypotonia, difficulty speaking, seizures

CV: edema, hypotension, hypertension, palpitations

EENT: blurred vision, tinnitus, nasal congestion

GI: nausea, vomiting, constipation

GU: urinary frequency, dysuria, erectile dysfunction

Metabolic: hyperglycemia

Skin: pruritus, rash, sweating

Other: weight gain, hypersensitivity reactions

Interactions

Drug-drug.CNS depressants: increased baclofen effect

MAO inhibitors: increased CNS depression, hypotension

Tricyclic antidepressants, drugs causing

CNS depression: hypotonia, increased

CNS depression

Drug-diagnostic tests.Alkaline phosphatase, aspartate aminotransferase, glucose: increased levels

Drug-behaviors.Alcohol use: CNS depression

Patient monitoring

• During intrathecal infusion, check pump often for proper functioning and check catheter for patency.
• Monitor patient's response continually to determine appropriate dosage adjustment.

Observe closely for signs and symptoms of overdose (drowsiness, light-headedness, dizziness, respiratory depression), especially during initial screening and titration. No specific antidote exists. Immediately remove any solution from pump; if patient has respiratory depression, intubate until drug is eliminated.

Patient teaching

• Advise patient to take oral dose with food or milk.
• Instruct patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• Caution patient not to discontinue drug therapy abruptly. Doing so may cause hallucinations and rebound spasticity.
• Advise patient to avoid alcohol and other depressants such as sedatives while taking drug.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and behaviors mentioned above.


balsalazide disodium

Colazal, Colazide (UK)


Pharmacologic class: GI agent

Therapeutic class: Anti-inflammatory

Pregnancy risk category B

 

Action

Metabolized in colon to mesalamine and then to 5-aminosalicylic acid, both of which are thought to exert local anti-inflammatory effect by inhibiting prostaglandin and acid metabolites.

Availability

Capsules: 750 mg

Indications and dosages

Mildly to moderately active ulcerative colitis

Adults: Usual dosage, three 750-mg capsules P.O. t.i.d. (6.75 g daily) for up to 8 weeks; some patients may require 12 weeks

Children ages 5 to 17: Usual dosage, either three 750-mg capsules P.O. t.i.d. (6.75 g daily) for up to 8 weeks, or one 750-mg capsule P.O. t.i.d. (2.25 g daily) for up to 8 weeks

Contraindications

• Hypersensitivity to balsalazide, salicylates, or mesalamine

Precautions

Use cautiously in:
• renal impairment
• pyloric stenosis
• breastfeeding patients
• children younger than age 5 (safety and efficacy not established).

Administration

• Advise patient to swallow capsules whole, either always with or always without food.
• For those patients who can't swallow capsules whole, carefully open capsules and sprinkle contents on applesauce and have patient swallow contents immediately without chewing.

Adverse reactions

CNS: headache, insomnia, dizziness, anxiety, confusion, agitation, coma

EENT: blurred vision, eye irritation, tinnitus, earache, epistaxis, sinusitis, sore throat, nasopharyngitis

GI: nausea, vomiting, diarrhea, constipation, abdominal pain, dyspepsia, anorexia, oral blisters, oral candidiasis,

GI hemorrhage

GU: urinary tract infection

Musculoskeletal: arthralgia; myalgia; bone, back, neck, or limb pain

Respiratory: cough, upper respiratory tract infection

Skin: erythema

Other: generalized pain

Interactions

Drug-drug.Oral antibiotics: interference with balsalazide action

Patient monitoring

• Assess character and frequency of stools.
• Monitor CBC and liver and kidney function test results.

Patient teaching

• Instruct patient to take drug only as directed.
• Instruct patient to carefully open capsules and sprinkle contents on applesauce and swallow contents immediately without chewing if patient can't swallow capsules whole.
• Tell patient that teeth and tongue staining may occur when drug is taken by sprinkling on applesauce.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs mentioned above.

baclofen

/bac·lo·fen/ (bak´lo-fen″) an analogue of γ used to treat severe spasticity.

baclofen

(băk′lə-fĕn)
n.
A drug, C10H12ClNO2, that acts as a gamma-aminobutyric acid receptor agonist and is used to treat muscle spasticity, especially in patients with multiple sclerosis and spinal cord injuries.

baclofen

an antispastic agent.
indication It is prescribed to reduce the spasticity associated with multiple sclerosis, cerebral palsy, and spinal cord injury; not effective against spasticity caused by stroke.
contraindication Known hypersensitivity to this drug prohibits its use.
adverse effects Among the more serious adverse reactions are confusion, hypotension, dyspnea, impotence, nausea, and transient drowsiness.

baclofen

A GABA (gamma-aminobutyric acid) antagonist used to decrease recalcitrant spinal spasticity in patients with multiple sclerosis, spinal-cord injury and possibly also Parkinson’s disease.
 
Adverse effects
Vomiting, weakness, drowsiness, slow breathing, seizures, coma.

baclofen

Lioresal® Neurology A GABA antagonist used to ↓ recalcitrant spinal spasticity in Pts with multiple sclerosis, spinal-cord injury, and possibly also Parkinson's disease

baclofen

A drug derived from the NEUROTRANSMITTER GABA that interferes with nerve transmission in the spinal cord and relaxes muscle spasm. It is used to alleviate the effects of conditions such as STROKE and MULTIPLE SCLEROSIS. A brand name is Lioresal.

baclofen 

An analogue of gamma-aminobutyric acid (GABA) used orally to treat skeletal muscle spasm and in the management of nystagmus, particularly periodic alternating nystagmus.

baclofen (bak´lōfen´),

n brand name: Lioresal;
drug class: central-acting skeletal muscle relaxant;
action: inhibits both monosynaptic and polysynaptic reflexes in the spinal cord;
uses: treatment for skeletal muscle spasticity in multiple sclerosis and spinal cord injury.

baclofen

an analog of gamma-aminobutyric acid (GABA) used as a muscle relaxant.
References in periodicals archive ?
The following drugs were used in these experiments: morphine sulfate (TEMAD, Iran), baclofen and CGP35348 (Novartis Basel, Switzerland), Ketamine hydrochloride and Xylazine (Alfasan Worden, Holland).
She has a Baclofen pump inserted into her stomach to control her MS.
Bethany was one of the first patients in the North East to be fitted with the innovative Baclofen pump and her parents said it transformed her life for many years.
Racemic baclofen (mixture of arbaclofen and esbaclofen) is approved by the FDA to treat spasticity and stiff muscles due to cerebral palsy or other forms of brain or spinal cord injury, but arbaclofen, the more active form of baclofen, is not FDA approved.
Bethany Ruff's life had been transformed when she was fitted with a Baclofen pump to treat her cerebral palsy nine years ago.
Implanting a special device -- the Baclofen Pump -- into him could have helped Shamlal move.
Natter suggested that Carol consider undergoing surgery to have a subcutaneous pump implanted that would administer Baclofen continuously and uniformly.
On questioning the family members, it emerged that the patient was taking baclofen, quetiapine, mirtazipine, salicylic acid and gabapentin, and that two weeks' supply of the gamma-aminobutyric acid analogue baclofen (a total of 840 mg) and the atypical antipsychotic quetiapine (8400 mg) were missing, leading to a presumptive diagnosis of deliberate overdose.
Baclofen has been shown to produce presynaptic inhibition of primary afferent terminals [88], and it inhibits the release of the excitatory neurotransmitters glutamate [89] and substance P [90] from the primary afferents.