BACLOPAR

Main information

  • Trade name:
  • BACLOPAR Tablets 25 Milligram
  • Dosage:
  • 25 Milligram
  • Pharmaceutical form:
  • Tablets
  • Medicine domain:
  • Humans
  • Medicine type:
  • Allopathic drug

Documents

Localization

  • Available in:
  • BACLOPAR Tablets 25 Milligram
    Ireland
  • Language:
  • English

Status

  • Source:
  • HPRA - Health Products Regulatory Authority - Ireland
  • Authorization number:
  • PA0405/029/002
  • Authorization date:
  • 21-11-1989
  • Last update:
  • 14-10-2016

Summary of Product characteristics: dosage, interactions, side effects

PartII

SummaryofProductCharacteristics

1NAMEOFTHEMEDICINALPRODUCT

Baclopar25 mg Tablets

2QUALITATIVEANDQUANTITATIVECOMPOSITION

Each tabletcontains25 mg ofBaclofen

Forexcipients, see6.1.

3PHARMACEUTICALFORM

Tablet

Awhitetablet, marked“BN”breakline“25”on onesideand“G”on thereverse.

4CLINICALPARTICULARS

4.1TherapeuticIndications

4.1.1 Reliefofvoluntary musclespasticity asoccursin conditionssuch asmultiplesclerosisand spinalcord

lesionsincluding syringomelia, transversemyelitisand motorneuronedisease.

4.1.2 Managementofspasticity ofcerebralorigin including meningitis, cerebralpalsy, traumatichead injury,

cerebrovascularaccident.

Baclofenisofmostbenefitin reliefofspasticity which isseriously interfering with activity.

4.2Posologyandmethodofadminstration

Fororaladministration only.

Reliefofvoluntary musclespasticity in spinalcord lesionsand managementofspasticity ofcerebralorigin.

Adults:Agradually increasingdosageregimen ofbaclofen isrecommended which should beadjusted to

achievesatisfactory symptomcontrol.

5mg threetimesaday forthreedays

10mg threetimesaday forthreedays

15mg threetimesaday forthreedays

20mg threetimesaday forthreedays

25mg threetimesaday forthreedays

Symptomsareusually adequately controlled with dosesup to 60mg daily.However, in orderto meet

individualpatientneeds, dosageadjustmentsshould beslowandcareful.Thedoseshould notexceed 100mg

perday unlessthepatientisin hospitalundermedicalsupervision.Iftherapeuticeffectisnotachieved within

6 weeksofreaching themaximumrecommended dose, adecision ofwhetherto continuewith therapy should

betaken.In somecases, mobility isimproved with smallfrequentdoses, especially ifgiven1 hourpriorto

performing manualtasks, ratherthan largerspaced doses.Somepatientsbenefitfromonly takingbaclofen at

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Issued 27/10/2005 CRN 2016159 page number: 1

Elderly:Sideeffectsaremorecommon in theelderly and arenoticed mostparticularly atthebeginning of

baclofen therapy.Elderly patientsshould betreated undercarefulmedicalsupervisionand initially receivea

lowdoseofbaclofen which can gradually betitrated upwardsaccording to thetherapeuticresponse.Most

elderly patientsareableto toleratethesameaveragemaximumdoseasforyoungerpatients.

Children:Adosagerangeof0.75-2mg/kg body weightshould beused.In children over10 yearsofage

however, amaximumdaily dosageof2.5mg/kg body weightmay begiven.Thedosageshould becautiously

raised atthesamerateindicated foradultsuntilsatisfactory symptomcontrolisachieved.Therecommended

daily dosagesformaintenancetherapy areasfollows:-

Children aged, 12 months-2 years: 10-20mg;

2 years-6 years: 20-30mg;

6 years-10 years: 30-60mg

Patientswithimpaired renalfunction:Aparticularly lowdosageofbaclofen should beused in patientswith

impaired renalfunction orthoseundergoing haemodialysis.

Patientswithspasticstatesofcerebralorigin:Such patientsaremorelikely to experienceunwanted side

effectsand should bekeptunderclosesurveillance.Therapy and subsequentdosagechangesshouldbe

initiated with caution.

4.3Contraindications

Hypersensitivity to baclofen and pulmonary insufficiency.

4.4Special warningsandspecialprecautionsforuse

Baclofenshould only beused with greatcaution in patientswith epilepsy, history ofconvulsions, psychotic

disorders, schizophreniaorconfusionalstatessinceexacerbation ofsuch conditionsmay occur.

Patientswith acutecerebrovascularischaemia, ahistoryof/orexistentpepticulcers, orthoseon anti-

hypertensivetherapyorwith renalimpairmentshouldreceivebaclofen only undercarefulsupervision.

Useofthedrug, particularly ifithasbeen prolonged, should notbeterminated abruptly to avoid precipitation

ofparanoia, hallucinations, and withdrawalsyndrome.Treatmentshould begradually discontinued by

reducing thedosageover1-2 weeks.

Baclofenmay interferewith micturition and associated functions.Patientswith neurogenicdisturbances

affecting emptying may showimprovementbutthosewith pre-existing sphincterhypertoniamay experience

acuteurinary retention.

Raised AST, APand blood glucoselevelshavebeen noted rarely.Liverfunction testsshould beperformed in

patientswith liverdiseaseand diabeticpatientsmonitored to ensurethatno underlying drug induced changes

haveoccurred in thesediseases.

Patientswith renalhereditary problemsofgalactoseintolerance, theLapp lactasedeficiency orglucose-

galactosemalabsorption should nottakethismedicine.

4.5Interactionwithothermedicinalproductsandotherformsofinteraction

In concomitantadministration with otherdrugsacting on theCNSorwith alcohol, increased sedation may

occur.

Prolongation offentanylinduced anaesthesiamay occurin patientspre-treated with baclofen.

Theeffectofbaclofen may beprolonged ifco-administered with tricyclicanti-depressantsresulting inmarked

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Issued 27/10/2005 CRN 2016159 page number: 2

Therisk ofhypotension occurring isincreased in patientsreceiving both baclofen and anti-hypertensive

therapy.Adjustmentsto thedosageofanti-hypertensivemedication should bemadeaccordingly.

Mentalconfusion, hallucinationsand agitation hasbeen reported in patientsconcurrently treated with baclofen

and levodopapluscarbidopaforParkinson'sDisease.

Drugswhich may producerenalinsufficiency e.g. ibuprofen may reducebaclofen excretion leading to toxic

effects.

4.6Pregnancyandlactation

Genotoxicity hasnotbeen reported with baclofen.

An increased incidenceofventralherniashasbeen noted in thefoetusesofratsreceiving high dosesof

baclofen during theperiod oforganogenesis.Studiesin ratsand rabbitssuggestthatbaclofen may inhibit

foetalboneossification.

Femalerats, treated with baclofenfor2 yearshavedeveloped enlarged and/orhaemorrhagicadrenalsand a

doserelated increaseofovarian cysts.Theclinicalrelevanceofthesefindingsisnotknown.

Asbaclofen crossestheplacentaitshould beavoided in pregnancy, especially in thefirsttrimester, unlessthe

benefitoftreatmentforthemotheroutweighstherisksto thefoetus. Acaseofwithdrawalin aneonate

manifesting asgeneralised convulsionsfollowing intrauterineBaclofenexposurehasbeen recorded.

Baclofenisexcreted in breastmilk, buttheamountpresentisconsidered to betoo smallto harmtheinfant.

4.7Effectsonabilitytodriveandusemachines

Baclofenmay inducesedation and willaffectvoluntary muscletone.Ifaffected, patientsshould notdriveor

operatemachinery.

4.8Undesirableeffects

Thesearemostcommon atthestartofbaclofen therapy;ifthedoseisraised too rapidly;athigh dosesand

also in theelderly.They areusually temporary and can berelieved orremoved by reducing thedose.Itisrare

forthesideeffectsto requirewithdrawaloftherapy.

Centralnervoussystem:Atthestartoftreatmentfrequenteffectshaveincluded day timesedation,

drowsiness, andnausea.Occasionally drynessofthemouth, respiratory depression, lightheadedness,

lassitude, exhaustion, mentalconfusion, dizziness, retching, vomiting, headacheand insomniaarereported.

Ifnauseapersistsdespitedosagereduction, itisrecommended thatbaclofen betaken with food oramilk

beverage.

Itisoften difficultto distinguish between neurologicaland/orpsychiatricmanifestationsand thoseofthe

diseaseundertreatment.Thosewhich haveoccasionally orrarely been reported include:euphoria, depressive

states, paraesthesiae, myalgia, muscularweakness, ataxia, tremor, nystagmus, accommodation disorders,

hallucinations, nightmares.Lowering oftheconvulsion threshold and seizuresmay possibly occur,

particularly in epilepticpatients.

Gastro-IntestinalTract:Occasionally, mild gastro-intestinaldisturbances(constipation, diarrhoea).

Cardio-vascularSystem:Occasionally, hypotension, diminished cardiovascularfunction.

UrogenitalSystem:Occasionally orrarely, dysuria, frequencyofmicturition, enuresisand impotenceand

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Issued 27/10/2005 CRN 2016159 page number: 3

undertreatment.

MiscellaneousUnwanted Effects:In rareorisolated cases, alterationsin thetastesensation, hyperhidrosis,

skin rash, hepaticdysfunction.

Paradoxicalincreased spasticity hasbeen noted in somepatients.

An undesirabledegreeofmuscularhypotoniamay occur.Thiscan usually berelieved by dosagere-

adjustments(i.e. by reducing thedosesgiven during theday and possibly increasing theevening dose).

4.9Overdose

Symptoms:Centralnervousdepression:drowsiness, impairmentofconsciousness, respiratorydepression and

coma.

Otherpossiblesymptomsare:confusion, hallucinations, agitation, accommodation disorders, absentpupillary

reflex;generalised muscularhypotonia, myoclonia, hyporeflexiaorareflexia:convulsions;peripheral

vasodilatation, hypotension, bradycardia;hypothermia;nausea, vomiting, diarrhoea, hypersalivation;elevated

LDH, ASTand APvalues.

Thecondition may beaggravated ifvarioussubstancesordrugsacting on thecentralnervoussystem(e.g.

alcohol, diazepam, tricyclicantidepressants)weretaken atthesametime.

Treatment:Thereisno specificantidote.

Thedrug should beremoved fromthegastro-intestinaltractby induction ofvomiting, gastriclavage

(comatosepatientsshould beintubated priorto gastriclavage)and administration ofactivated charcoal;if

necessary salineaperient.In respiratory depression, administration ofartificialrespiration, also measuresin

supportofcardiovascularfunctionsshould begiven.Excretion ischiefly viathekidneysso generous

quantitiesoffluid should begiven.In theeventofconvulsions, i.v. diazepammay beadministered cautiously.

5PHARMACOLOGICALPROPERTIES

5.1Pharmacodynamicproperties

Baclofenisachlorophenylanalogueofgamma-aminobutyricacid (GABA)and ischemically unrelated to

otherantispasticagents.Itactsatthespinalleveldepressing monosynapticand polysynapticreflex

transmission, mostprobably by stimulating theGABAreceptors.This, in turn inhibitsthereleaseofthe

excitatory amino acids(glutamateand aspartate).Baclofendoesnotaffectneuromusculartransmission.

5.2Pharmacokineticproperties

Baclofeniswellabsorbed and excreted mostly unmetabolised in theurinewith aT½ofabout5 hours.

5.3Preclinical safetydata

Animalstudiessuggestarelatively lowleveloftoxicity.Repeated dosing schedulesdemonstrated adose-

related increasein theincidenceofovarian cysts.No associated microscopicabnormalitieswerereported with

theincreased incidenceofovarian cysts.Increased levelsofALTwerealso demonstrated butwerenot

associated with histopathologicalchanges.Two yearratstudiesshowno increasesin eitherhyperplasiaor

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Issued 27/10/2005 CRN 2016159 page number: 4

6PHARMACEUTICALPARTICULARS

6.1Listofexcipients

Lactosemonohydrate

Microcrystallinecellulose

Calciumhydrogen phosphate, anhydrous

Sodiumstarch glycolate(TypeA)

Colloidalanhydroussilica

Magnesiumstearate

6.2Incompatibilities

Notapplicable

6.3ShelfLife

3 years

6.4Special precautionsforstorage

Do notstoreabove25 °

6.5Natureandcontentsofcontainer

6.5.1 Securitainers

Polypropylenetabletcontainerswith polyethylenecapsand polyethyleneullagefiller.Pack contentsof50 or

100 tablets.

6.5.2 Blisterstrips

Polyvinylchlorideblisterssealed onto aluminiumfoil.Pack contentsof100 tablets.

Notallpack sizesmay bemarketed.

6.6Instructionsforuseandhandling

No specialrequirements.

7MARKETINGAUTHORISATIONHOLDER

Generics(UK)Limited

12 Station Close

PottersBar

Hertfordshire, EN6 1TL

8MARKETINGAUTHORISATIONNUMBER

PA405/29/2

9DATEOFFIRSTAUTHORISATION/RENEWALOFTHEAUTHORISATION

Dateoffirstauthorisation: 21 st

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Issued 27/10/2005 CRN 2016159 page number: 5

Dateoflastrenewal: 21 st

November2004

10DATEOFREVISIONOFTHETEXT

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Issued 27/10/2005 CRN 2016159 page number: 6