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Baclofen Tablets USP Revised: January 2004 Rx only | Baclofen [Preferred Pharmaceuticals, Inc] | BioPortfolio

13:34 EST 27th January 2019 | BioPortfolio

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Baclofen USP is a muscle relaxant and antispastic, available as 10 mg and 20 mg tablets for oral administration. Its chemical name is 4-amino-3-(4-chlorophenyl)-butanoic acid.

Baclofen USP is a white to off-white, odorless or practically odorless crystalline powder. It is slightly soluble in water, very slightly soluble in methanol, and insoluble in chloroform. The structural formula is represented below:

Baclofen Tablets USP 10 mg and 20 mg contain the following inactive ingredients: magnesium stearate, microcrystalline cellulose, povidone and starch (corn).

The precise mechanism of action of baclofen is not fully known. Baclofen 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. 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 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.

Patients should have reversible spasticity so that baclofen treatment will aid in restoring residual function.

Baclofen may also be of some value in patients with spinal cord injuries and other spinal cord diseases.

Baclofen is not indicated in the treatment of skeletal muscle spasm resulting from rheumatic disorders.

The efficacy of baclofen in stroke, cerebral palsy, and Parkinson’s disease has not been established and, therefore, it is not recommended for these conditions.

Hypersensitivity to baclofen.

Safe use of baclofen in pediatric patients under age 12 has not been established, and it is, therefore, not recommended for use in pediatric patients.

Because of the possibility of sedation, patients should be cautioned regarding the operation of automobiles or other dangerous machinery, and activities made hazardous by decreased alertness. Patients should also be cautioned that the central nervous system effects of baclofen may be additive to those of alcohol and other CNS depressants.

Baclofen should be used with caution where spasticity is utilized to sustain upright posture and balance in locomotion or whenever spasticity is utilized to obtain increased function.

In patients with epilepsy, the clinical state and electroencephalogram should be monitored at regular intervals, since deterioration in seizure control and EEG have been reported occasionally in patients taking baclofen.

It is not known whether this drug is excreted in human milk. As a general rule, nursing should not be undertaken while a patient is on a drug since many drugs are excreted in human milk.

A dose-related increase in incidence of ovarian cysts and a less marked increase in enlarged and/or hemorrhagic adrenal glands was observed in female rats treated chronically with baclofen.

Ovarian cysts have been found by palpation in about 4% of the multiple sclerosis patients that were treated with baclofen for up to one year. In most cases these cysts disappeared spontaneously while patients continued to receive the drug. Ovarian cysts are estimated to occur spontaneously in approximately 1% to 5% of the normal female population.

The most common is transient drowsiness (10-63%). In one controlled study of 175 patients, transient drowsiness was observed in 63% of those receiving baclofen compared to 36% of those in the placebo group. Other common adverse reactions are dizziness (5-15%), weakness (5-15%) and fatigue (2-4%). Others reported:

Neuropsychiatric: Confusion (1-11%), headache (4-8%), insomnia (2-7%); and, rarely, euphoria, excitement, depression, hallucinations, paresthesia, muscle pain, tinnitus, slurred speech, coordination disorder, tremor, rigidity, dystonia, ataxia, blurred vision, nystagmus, strabismus, miosis, mydriasis, diplopia, dysarthria, epileptic seizure.

Cardiovascular: Hypotension (0-9%). Rare instances of dyspnea, palpitation, chest pain, syncope.

Gastrointestinal: Nausea (4-12%), constipation (2-6%); and, rarely, dry mouth, anorexia, taste disorder, abdominal pain, vomiting, diarrhea, and positive test for occult blood in stool.

Genitourinary: Urinary frequency (2-6%); and, rarely, enuresis, urinary retention, dysuria, impotence, inability to ejaculate, nocturia, hematuria.

Other: Instances of rash, pruritus, ankle edema, excessive perspiration, weight gain, nasal congestion.

Some of the CNS and genitourinary symptoms may be related to the underlying disease rather than to drug therapy. The following laboratory tests have been found to be abnormal in a few patients receiving baclofen: increased SGOT, elevated alkaline phosphatase, and elevation of blood sugar.

Signs and symptoms: Vomiting, muscular hypotonia, drowsiness, accommodation disorders, coma, respiratory depression, and seizures.

Treatment: In the alert patient, empty the stomach promptly by induced emesis followed by lavage. In the obtunded patient, secure the airway with a cuffed endotracheal tube before beginning lavage (do not induce emesis). Maintain adequate respiratory exchange, do not use respiratory stimulants.

The determination of optimal dosage requires individual titration. Start therapy at a low dosage and increase gradually until optimum effect is achieved (usually between 40-80 mg daily).

The following dosage titration schedule is suggested:

5 mg t.i.d. for 3 days

10 mg t.i.d. for 3 days

15 mg t.i.d. for 3 days

20 mg t.i.d. for 3 days

Thereafter additional increases may be necessary but the total daily dose should not exceed a maximum of 80 mg daily (20 mg q.i.d.).

The lowest dose compatible with an optimal response is recommended. If benefits are not evident after a reasonable trial period, patients should be slowly withdrawn from the drug (see WARNINGS, Abrupt Drug Withdrawal).

Baclofen Tablets USP 10 mg are scored, round, white tablets imprinted DAN 5730 and 10 supplied in:

Bottles of 30 tablets, NDC 68788-0522-3Bottles of 60 tablets, NDC 68788-0522-6Bottles of 90 tablets, NDC 68788-0522-9Bottles of 100 tablets, NDC 68788-0522-1Bottles of 120 tablets, NDC 68788-0522-8

Dispense in a tight container with a child-resistant closure.

Store at controlled room temperature 15°-30°C (59°-86°F).

Watson Laboratories, Inc.

Corona, CA 92880 USA

Rev: January 2004

Manufacturer

Preferred Pharmaceuticals, Inc

Active Ingredients

Source

Clinical Trials [55 Associated Clinical Trials listed on BioPortfolio]

A Study of Baclofen Formulations in Healthy Adults

The purpose of this study is to determine the pharmacokinetics, safety, and tolerability of different baclofen formulations.

Baclofen in Managing Acute Alcohol Withdrawal

The study goal is to investigate whether administration of oral baclofen forms an adequate treatment option in the management of acute alcohol withdrawal. We will compare placebo with dose...

Baclofen as a Perioperative Analgesic Adjuvant

The purpose of this study is to determine whether a single, oral dose of baclofen alters postoperative opioid requirements.

Effect of Low-Dose Baclofen Administration on the GH-IGF1 Axis

Insulin-like growth factor I (IGF-I) is used as a measure of the body's ability to produce growth hormone. Growth hormone is important for muscle tissue as well as many other tissues in th...

Baclofen in the Treatment of Alcoholic Liver Disease

To explore the effectiveness and biobehavioural basis of baclofen in improving treatment outcomes for alcohol dependence in people with alcoholic cirrhosis in a double-blind randomised pla...

PubMed Articles [36 Associated PubMed Articles listed on BioPortfolio]

Pharmacokinetics and toxicity of high-dose baclofen in ICU patients.

High-dose baclofen could prove beneficial in patients with unhealthy alcohol use in intensive care units (ICU). However, the pharmacokinetic properties of baclofen are unknown in this population. Our ...

An intoxication mimicking brain death: baclofen.

Baclofen is a derivative of gamma-aminobutyric acid, used mainly for the treatment of muscle spasticity. Baclofen overdose can result in severe respiratory depression, autonomic disturbances, seizures...

Interactions between Baclofen and DC-Induced Plasticity of Afferent Fibers within the Spinal Cord.

The aims of the study were to compare effects of baclofen, a GABA receptor agonist commonly used as an antispastic drug, on direct current (DC) evoked long-lasting changes in the excitability of affer...

Subcutaneous dexmedetomidine for baclofen withdrawal during palliative sedation.

Sudden cessation of baclofen can produce a withdrawal syndrome even if it was previously orally administered. We present the case of a man who exhibited signs of baclofen withdrawal syndrome during pa...

Baclofen-loaded PLGA nanoparticles for neuropathic pain management: In-vitro and In-vivo Evaluation.

In the present work, PLGA nanoparticles of baclofen (Bcf-PLGA-NPs) were developed and optimized using nanoprecipitation method. The average particle size of the Bcf-PLGA-NP was found to be 124.8 nm, p...

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