BACLOFEN by Palmetto Pharmaceuticals Inc. BACLOFEN solution

BACLOFEN by

Drug Labeling and Warnings

BACLOFEN by is a Prescription medication manufactured, distributed, or labeled by Palmetto Pharmaceuticals Inc.. Drug facts, warnings, and ingredients follow.

Drug Details [pdf]

  • 1 INDICATIONS AND USAGE

    Baclofen Oral Solution is indicated for the treatment of spasticity resulting from multiple sclerosis, particularly for the relief of flexor spasms and concomitant pain, clonus, and muscular rigidity.

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

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

  • 2 DOSAGE AND ADMINISTRATION

    2.1 Recommended Dosage

    Initiate Baclofen Oral Solution with a low dosage, preferably in divided doses, administered orally. The following gradually increasing dosage regimen is suggested, but should be adjusted based on clinical response and tolerability:

    5 mL (5 mg) three times a day for three days

    10 mL (10 mg) three times a day for three days

    15 mL (15 mg) three times a day for three days

    20 mL (20 mg) three times a day for three days

    Additional increases may be necessary up to the maximum recommended dosage of 80 mg daily (20 mg four times a day).

    2.2 Discontinuation of Baclofen Oral Solution

    When discontinuing Baclofen Oral Solution, reduce the dosage slowly and avoid abrupt withdrawn from the drug to help minimize the risk of adverse reactions [see Warnings and Precautions ( 5.1)].

  • 3 DOSAGE FORMS AND STRENGTHS

    Oral Solution: 5 mg/5 mL baclofen as a clear, colorless solution with a grape aroma

  • 4 CONTRAINDICATIONS

    Baclofen Oral Solution is contraindicated in patients with hypersensitivity to baclofen.

  • 5 WARNINGS AND PRECAUTIONS

    5.1 Adverse Reactions from Abrupt Withdrawal of Baclofen Oral Solution

    Abrupt discontinuation of baclofen, regardless of the cause, has resulted in adverse reactions that include hallucinations, seizures, high fever, altered mental status, exaggerated rebound spasticity, and muscle rigidity, that in rare cases has advanced to rhabdomyolysis, multiple organ-system failure, and death. Therefore, reduce the dosage slowly when Baclofen Oral Solution is discontinued, unless the clinical situation justifies a rapid withdrawal.

    5.2 Neonatal Withdrawal Symptoms

    Withdrawal symptoms in neonates whose mothers were treated with oral baclofen throughout pregnancy have been reported starting hours to days after delivery. The symptoms of withdrawal in these infants have included increased muscle tone, tremor, jitteriness, and seizure. If the potential benefit justifies the potential risk to the fetus and Baclofen Oral Solution is continued during pregnancy, gradually reduce the dosage and discontinue Baclofen Oral Solution before delivery. If slow withdrawal is not feasible, advise the parents or caregivers of the exposed neonate of the potential for neonatal withdrawal.

    5.3 Drowsiness and Sedation

    Drowsiness and sedation have been reported in up to 63% of patients taking baclofen, the active ingredient in Baclofen Oral Solution  [see Adverse Reactions ( 6.1)] . Patients should avoid operation of automobiles or other dangerous machinery and activities made hazardous by decreased alertness when starting Baclofen Oral Solution or increasing the dose until they know how the drug affects them. Advise patients that the central nervous system depressant effects of Baclofen Oral Solution may be additive to those of alcohol and other CNS depressants.

    5.4 Poor Tolerability in Stroke Patients

    Baclofen Oral Solution should be used with caution in patients who have had a stroke. Baclofen has not significantly benefited patients with stroke. These patients have also shown poor tolerability to the drug.

    5.5 Exacerbation of Psychotic Disorders, Schizophrenia, or Confusional States

    Baclofen Oral Solution should be used with caution in patients suffering from psychotic disorders, schizophrenia, or confusional states. If treated with Baclofen Oral Solution, these patients should be kept under careful surveillance because exacerbations of these conditions have been observed with oral baclofen administration.

    5.6 Exacerbation of Autonomic Dysreflexia

    Baclofen Oral Solution should be used with caution in patients with a history of autonomic dysreflexia. The presence of nociceptive stimuli or abrupt withdrawal of Baclofen Oral Solution may cause an autonomic dysreflexic episode.

    5.7 Exacerbation of Epilepsy

    Baclofen Oral Solution should be used with caution in patients with epilepsy. Deterioration in seizure control has been reported in patients taking baclofen.

    5.8 Posture and Balance Effects

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

    5.9 Ovarian Cysts

    A dose-related increase in incidence of ovarian cysts was observed in female rats treated chronically with oral baclofen. Ovarian cysts have been found by palpation in about 4% of the multiple sclerosis patients who were treated with oral 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.

  • 6 ADVERSE REACTIONS

    The following clinically significant adverse reactions are described elsewhere in the labeling:

    • Adverse Reactions from Abrupt Withdrawal of Baclofen Oral Solution  [see Warnings and Precautions ( 5.1)]
    • Neonatal Withdrawal Symptoms [see Warnings and Precautions ( 5.2)]
    • Drowsiness and Sedation [see Warnings and Precautions ( 5.3)]
    • Poor Tolerability in Stroke Patients [see Warnings and Precautions ( 5.4)]
    • Exacerbation of Psychotic Disorders, Schizophrenia, or Confusional States [see Warnings and Precautions ( 5.5)]
    • Exacerbation of Autonomic Dysreflexia [see Warnings and Precautions ( 5.6)]
    • Exacerbation of Epilepsy [see Warnings and Precautions ( 5.7)]
    • Posture and Balance Effects [see Warnings and Precautions ( 5.8)]
    • Ovarian Cysts [see Warnings and Precautions ( 5.9)]

    6.1 Clinical Trials Experience

    Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

    The most common adverse reaction is transient drowsiness. 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 (up to 15%) are dizziness and weakness. Adverse reactions with a frequency of ≥1% are listed in Table 1.

    Table 1. Common (≥1%) Adverse Reactions in Patients Treated with Baclofen for Spasticity

    ADVERSE REACTION

    PERCENT

    Drowsiness

    10-63%

    Dizziness

    5-15%

    Weakness

    5-15%

    Nausea

    4-12%

    Confusion

    1-11%

    Hypotension

    0-9%

    Headache

    4-8%

    Insomnia

    2-7%

    Constipation

    2-6%

    Urinary Frequency

    2-6%

    Fatigue

    2-4%

    The following adverse reactions not included in Table 1, classified by body system, were also reported:

    Neuropsychiatric: 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: dyspnea, palpitation, chest pain, syncope

    Gastrointestinal: dry mouth, anorexia, taste disorder, abdominal pain, vomiting, diarrhea, and positive test for occult blood in stool

    Genitourinary: enuresis, urinary retention, dysuria, impotence, inability to ejaculate, nocturia, hematuria

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

    The following laboratory tests have been found to be abnormal in patients receiving baclofen: increased SGOT, elevated alkaline phosphatase, and elevation of blood sugar.

  • 7 DRUG INTERACTIONS

    7.1 CNS Depressants and Alcohol

    Baclofen Oral Solution can cause CNS depression, including drowsiness and sedation, which may be additive when used concomitantly with other CNS depressants or alcohol [see Warnings and Precautions ( 5.3)].

  • 8 USE IN SPECIFIC POPULATIONS

    8.1 Pregnancy

    Risk Summary
    There are no adequate data on the developmental risk associated with the use of Baclofen Oral Solution in pregnant women. Oral administration of baclofen to pregnant rats resulted in an increased incidence of fetal structural abnormalities at a dose which was also associated with maternal toxicity. The background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively.

    Clinical Considerations
    Fetal/Neonatal adverse reactions
    Baclofen Oral Solution may increase the risk of late-onset neonatal withdrawal symptoms [see Warnings and Precautions ( 5.2)] .

    Data

    Animal Data
    Baclofen given orally has been shown to increase the incidence of omphaloceles (ventral hernias) in fetuses of rats given approximately 13 times on a mg/kg basis, or 3 times on a mg/m 2 basis, the maximum oral dose recommended for human use; this dose also caused reductions in food intake and weight gain in the dams. This abnormality was not seen in mice or rabbits.

    8.2 Lactation

    Risk Summary
    At recommended oral doses, baclofen is present in human milk. There are no human data on the effects of baclofen on milk production. There are no adequate data on the effects of baclofen on the breastfed infant. Withdrawal symptoms can occur in breastfed infants when maternal administration of Baclofen Oral Solution is stopped, or when breastfeeding is stopped [see Warnings and Precautions ( 5.2)] .

    The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for Baclofen Oral Solution and any potential adverse effects on the breastfed infant from Baclofen Oral Solution or from the underlying maternal condition.

    8.4 Pediatric Use

    Safety and effectiveness in pediatric patients below the age of 12 have not been established.

    8.5 Geriatric Use

    In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

    8.6 Renal Impairment

    Because baclofen is primarily excreted unchanged through the kidneys, Baclofen Oral Solution should be given with caution to patients with renal impairment, and it may be necessary to reduce the dosage.

  • 10 OVERDOSAGE

    10.1 Symptoms of Baclofen Overdose

    Patients may present in coma or with progressive drowsiness, lightheadedness, dizziness, somnolence, accommodation disorders, respiratory depression, seizures, or hypotonia progressing to loss of consciousness.

    10.2 Treatment for Overdose

    The treatment of baclofen overdose includes gastric decontamination, maintaining an adequate airway and respirations.

  • 11 DESCRIPTION

    Baclofen Oral Solution is a gamma-aminobutyric acid (GABA-ergic) agonist available as 5 mg/5 mL solution for oral administration. Its chemical name is 4-amino-3-(4-chlorophenyl)-butanoic acid, and its structural formula is:

    image description

    Molecular formula is C 1OH 12CINO 2.

    Molecular Weight is 213.66.

    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 Baclofen Oral Solution inactive ingredients are: citric acid anhydrous, glycerin, natural grape flavor, methylparaben, propylparaben, purified water, sodium citrate dihydrate, and sucralose. May also contain sodium hydroxide or hydrochloric acid for pH adjustment.

  • 12 CLINICAL PHARMACOLOGY

    12.1 Mechanism of Action

    The precise mechanism of action of baclofen is not fully understood. Baclofen inhibits both monosynaptic and polysynaptic reflexes at the spinal level, possibly by decreasing excitatory neurotransmitter release from afferent terminals, although actions at supraspinal sites may also occur and contribute to its clinical effect. Baclofen is a structural analog of the inhibitory neurotransmitter gamma- aminobutyric acid (GABA), and may exert its effects by stimulation of the GABA B receptor subtype.

    12.2 Pharmacodynamics

    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 [see Warnings and Precautions ( 5.3), Adverse Reactions ( 6.1), and Overdosage ( 10.1)].

    12.3 Pharmacokinetics

    A pharmacokinetic study in heathy adult male subjects under fasting conditions at 20 mg dose level demonstrated similar bioavailability for baclofen oral solution and oral tablets. The peak plasma concentrations were achieved in about 0.75 hours from oral solution and the apparent elimination half-life is about 5.7 hours. Baclofen is excreted primarily by the kidney in unchanged form, and there is relatively large intersubject variation in absorption and/or elimination.

  • 13 NONCLINICAL TOXICOLOGY

    13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility

    Carcinogenesis

    No increase in tumors was seen in rats receiving baclofen orally for two years at approximately 30 to 60 times on a mg/kg basis, or 10 to 20 times on a mg/ m 2 basis, the maximum oral dose recommended for human use.

    Mutagenesis

    Genetic toxicology assays have not been conducted for baclofen.

    Impairment of Fertility

    Studies to evaluate the effects of baclofen on fertility have not been conducted.

  • 14 CLINICAL STUDIES

    The efficacy of Baclofen Oral Solution is based upon a bioavailability study in healthy adults comparing baclofen oral tablets to Baclofen Oral Solution  [see Clinical Pharmacology ( 12.3)].

  • 16 HOW SUPPLIED/STORAGE AND HANDLING

    16.1 How Supplied

    Baclofen Oral Solution contains 5 mg/5 mL baclofen. It is a clear, colorless solution with a grape aroma and is supplied in bottles of 473 mL, NDC: 68134-401-16.

    16.2 Storage and Handling

    Must be refrigerated. Store at 2°C to 8°C (36°F to 46°F). Dispense in a tight, light-resistant container with a child-resistant closure.

  • 17 PATIENT COUNSELING INFORMATION

    Administration Instructions

    Instruct patients or caregivers to use an oral dosing syringe to correctly measure the prescribed amount of medication. Inform patients that oral dosing syringes may be obtained from their pharmacy.

    Risks Related to Sudden Withdrawal of Baclofen Oral Solution

    Advise patients and caregivers not to discontinue use of Baclofen Oral Solution without consulting with their healthcare provider because sudden withdrawal of Baclofen Oral Solution can result in serious complications that include hallucinations, seizures, high fever, confusion, muscle stiffness, multiple organ-system failure, and death [see Warnings and Precautions ( 5.1)]. Inform patients that early symptoms of Baclofen Oral Solution withdrawal may include increased spasticity, itching, and tingling of extremities.

    Neonatal Withdrawal Symptoms

    Advise patients to notify their healthcare provider if they are pregnant, plan to become pregnant, or plan to breastfeed [see Warnings and Precautions ( 5.2) and Use in Specific Populations ( 8.2)].

    Increased Risk of Drowsiness with Alcohol and Other CNS Depressants

    Advise patients that Baclofen Oral Solution may cause drowsiness, and that they should avoid the operation of automobiles or other dangerous machinery, or activities made hazardous by decreased alertness when starting Baclofen Oral Solution or increasing the dose until they know how the drug affects them [see Warnings and Precautions ( 5.3)]. Inform patients and their caregivers that the drowsiness associated with Baclofen Oral Solution use can be worsened by alcohol and other CNS depressants. Advise patients to read all medicine labels carefully, and to tell their healthcare provider about all prescription and nonprescription drugs they may use.

    Storage

    Instruct patients to store Baclofen Oral Solution in the refrigerator [see How Supplied/Storage and Handling ( 16.2)].

    Manufactured by:
    Entreprises Importfab, Inc.
    50 Hymus Blvd.
    Pointe-Claire, QC, Canada H9R 1C9

    Distributed by:
    Palmetto Pharmaceuticals, Inc.

    Greenville, SC 29615.

    U.S. Patent No. 10,610,502

    02/2022

  • PACKAGE LABEL. PRINCIPAL DISPLAY PANEL

    NDC: 68134-401-16

    Baclofen Oral Solution

    5 mg / 5 mL

    Grape flavored,
    clear liquid solution

    Rx only

    16 fl. oz. (473 mL)

    baclofen_16oz

  • INGREDIENTS AND APPEARANCE
    BACLOFEN 
    baclofen solution
    Product Information
    Product TypeHUMAN PRESCRIPTION DRUGItem Code (Source)NDC: 68134-401
    Route of AdministrationORAL
    Active Ingredient/Active Moiety
    Ingredient NameBasis of StrengthStrength
    BACLOFEN (UNII: H789N3FKE8) (BACLOFEN - UNII:H789N3FKE8) BACLOFEN5 mg  in 5 mL
    Inactive Ingredients
    Ingredient NameStrength
    ANHYDROUS CITRIC ACID (UNII: XF417D3PSL)  
    GLYCERIN (UNII: PDC6A3C0OX)  
    METHYLPARABEN (UNII: A2I8C7HI9T)  
    PROPYLPARABEN (UNII: Z8IX2SC1OH)  
    TRISODIUM CITRATE DIHYDRATE (UNII: B22547B95K)  
    SUCRALOSE (UNII: 96K6UQ3ZD4)  
    WATER (UNII: 059QF0KO0R)  
    Product Characteristics
    Color    Score    
    ShapeSize
    FlavorGRAPEImprint Code
    Contains    
    Packaging
    #Item CodePackage DescriptionMarketing Start DateMarketing End Date
    1NDC: 68134-401-16473 mL in 1 BOTTLE; Type 0: Not a Combination Product03/15/2022
    Marketing Information
    Marketing CategoryApplication Number or Monograph CitationMarketing Start DateMarketing End Date
    NDA authorized genericNDA20819303/15/2022
    Labeler - Palmetto Pharmaceuticals Inc. (963291864)
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