ALPROX

Main information

  • Trade name:
  • ALPROX Tablets 0.5 Milligram
  • Dosage:
  • 0.5 Milligram
  • Pharmaceutical form:
  • Tablets
  • Medicine domain:
  • Humans
  • Medicine type:
  • Allopathic drug

Documents

Localization

  • Available in:
  • ALPROX Tablets 0.5 Milligram
    Ireland
  • Language:
  • English

Status

  • Source:
  • HPRA - Health Products Regulatory Authority - Ireland
  • Authorization number:
  • PA1327/001/001
  • Authorization date:
  • 30-06-2006
  • Last update:
  • 14-10-2016

Summary of Product characteristics: dosage, interactions, side effects

PartII

SummaryofProductCharacteristics

1NAMEOFTHEMEDICINALPRODUCT

Alprox0.5mgTablets

2QUALITATIVEANDQUANTITATIVECOMPOSITION

Eachtabletcontains0.5mgofAlprazolam.

Forexcipients,seesection6.1.

3PHARMACEUTICALFORM

Tablet

Whiteoralmostwhite,flat,roundscoredtabletswithadiameterof7mm.

4CLINICALPARTICULARS

4.1TherapeuticIndications

Intheshort-termmanagementofanxietystates.

Benzodiazepinesareonlyindicatedwhenthedisorderissevere,disablingorsubjectingtheindividualtoextreme

distress.

4.2Posologyandmethodofadministration

Fororaladministrationonly.

Anxiety

Thedurationoftreatmentshouldbeasshortaspossiblebutnotlongerthan8-12weeks,includingtaperingoffprocess.

Itisusualtocommencewithadoseof500micrograms(0.5mg)to1mgdailyindivideddoses,withincrements(ofno

greaterthan1mgevery3-4days)tothelevelofoptimalcontrol,usually3to4mgdaily.

Intheelderlyordebilitatedpatientaregimenof250micrograms(0.25mg)twicedailyshouldbeusedinitiallywith

gradualincrementsifrequiredandtoleranceisassured.

Initialdosesmaybegivenatbedtimetominimisedaytimelethargy.Ifside-effectsoccurwiththestartingdose,the

doseshouldbelowered.

Incertaincasesextensionbeyondthemaximumtreatmentperiodmaybenecessary;ifso,itshouldnottakeplace

withoutre-evaluationofthepatient’sstatus.

Treatmentshouldbestartedwiththelowestrecommendeddose.Themaximumdoseshouldnotbeexceeded.

4.3Contraindications

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 30/09/2006 CRN 2028462 page number: 1

Hypersensitivitytobenzodiazepinesortoanyoftheexcipients.

Severerespiratoryinsufficiency.

Sleepapnoeasyndrome.

Severehepaticinsufficiency.

4.4Specialwarningsandprecautionsforuse

Tolerance:

Somelossofefficacytothehypnoticeffectsofshort-actingbenzodiazepinesmaydevelopafterrepeateduseforafew

weeks.

Dependence:

Useofbenzodiazepinesmayleadtothedevelopmentofphysicalandpsychicdependenceupontheseproducts.Therisk

ofdependenceincreaseswithdoseanddurationoftreatment;itisalsogreaterinpatientswithahistoryofalcoholor

drugabuse.

Oncephysicaldependencehasdeveloped,abruptterminationoftreatmentwillbeaccompaniedbywithdrawal

symptoms.Thesemayconsistofheadaches,musclepain,extremeanxiety,tension,restlessness,confusionand

irritability.Inseverecasesthefollowingsymptomsmayoccur:derealisation;depersonalisation;hyperacusis;numbness

andtinglingoftheextremities;hypersensitivitytolight,noiseandphysicalcontact;hallucinationsorepilepticseizures.

Reboundinsomniaandanxiety:

Atransientsyndromewherebythesymptomsthatledtotreatmentwithabenzodiazepinerecurinanenhancedform

mayoccuronwithdrawaloftreatment.Itmaybeaccompaniedbyotherreactionsincludingmoodchanges,anxietyor

sleepdisturbancesandrestlessness.

Sincetheriskofwithdrawalphenomena/reboundphenomenaisgreaterafterabruptdiscontinuationoftreatment,itis

recommendedthatthedosageisdecreasedgradually.

Durationoftreatment:

Thedurationoftreatmentshouldbeasshortaspossible(seePosology)dependingontheindication,butshouldnot

exceedeighttotwelveweeksincaseofanxietyincludingtaperingoffprocess.Extensionbeyondthisperiodshouldnot

takeplacewithoutre-evaluationofthesituation.

Itmaybeusefultoinformthepatientwhentreatmentisstartedthatitwillbeoflimiteddurationandtoexplain

preciselyhowthedosagewillbeprogressivelydecreased.Moreover,itisimportantthatthepatientshouldbeawareof

thepossibilityofreboundphenomena,therebyminimisinganxietyoversuchsymptomsshouldtheyoccurwhilethe

medicinalproductisbeingdiscontinued.

Thereareindicationsthat,inthecaseofbenzodiazepineswithashortdurationofaction,withdrawalphenomenacan

becomemanifestwithinthedosageinterval,especiallywhenthedosageishigh.

Whenbenzodiazepineswithalongdurationofactionarebeinguseditisimportanttowarnagainstchangingtoa

benzodiazepinewithashortdurationofactionaswithdrawalsymptomsmaydevelop.

Amnesia:

Benzodiazepinesmayinduceanterogradeamnesia.Theconditionoccursmostoftenseveralhoursafteringestingthe

product,andthereforetoreducetherisk,patientsshouldensurethattheywillbeabletohaveanuninterruptedsleepof

7-8hours(seealsoUndesirableEffects).

Psychiatricandparadoxicalreactions:

Reactionslikerestlessness,agitation,irritability,aggressiveness,delusion,rages,nightmares,hallucinations,psychoses,

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 30/09/2006 CRN 2028462 page number: 2

thisoccur,useoftheproductshouldbediscontinued.

Thesereactionsaremorelikelytooccurinchildrenandtheelderly.

Specificpatientgroups:

Benzodiazepinesshouldnotbegiventochildrenwithoutcarefulassessmentoftheneedtodoso;thedurationof

treatmentshouldbekepttoaminimum.Elderlyshouldbegivenareduceddose(seePosology).Alowerdoseisalso

recommendedforpatientswithchronicrespiratoryinsufficiencyduetotheriskofrespiratorydepression.

Benzodiazepinesarenotindicatedtotreatpatientswithseverehepaticinsufficiencyasitmayprecipitate

encephalopathy.

Benzodiazepinesarenotrecommendedfortheprimarytreatmentofpsychoticillness.

Benzodiazepinesshouldnotbeusedalonetotreatdepressionoranxietyassociatedwithdepression(suicidemaybe

precipitatedinsuchpatients).

Benzodiazepinesshouldbeusedwithextremecautioninpatientswithahistoryofalcoholordrugabuse.

PatientswithrarehereditaryproblemsofgalactoseintolerancetheLapplactosedeficiencyorglucosegalactose

malabsorptionshouldnottakethismedicine.

4.5Interactionwithothermedicinalproductsandotherformsofinteraction

Notrecommended:

Concomitantintakewithalcohol.Thesedativeeffectmaybeenhancedwhentheproductisusedincombinationwith

alcohol.Thisaffectstheabilitytodriveorusemachines.

Takeintoaccount:

CombinationwithCNSdepressants.Enhancementofthecentraldepressiveeffectmayoccurincasesofconcomitant

usewithantipsychotics(neuroleptics),hypnotics,anxiolytics/sedatives,antidepressantagents,narcoticanalgesics,

antiepilepticdrugs,anaestheticsandsedativeantihistamines.

Inthecaseofnarcoticanalgesicsenhancementoftheeuphoriamayalsooccurleadingtoanincreaseinpsychic

dependence.

Compoundswhichinhibitcertainenzymes(particularlycytochromeP450)mayenhancetheactivityof

benzodiazepines.Toalesserdegreethisalsoappliestobenzodiazepinesthataremetabolisedonlybyconjugation.

4.6Pregnancyandlactation

Iftheproductisprescribedtoawomanofchildbearingpotential,sheshouldbewarnedtocontactherphysician

regardingdiscontinuanceoftheproductifsheintendstobecomeorsuspectsthatsheispregnant.

If,forcompellingmedicalreasons,theproductisadministeredduringthelatephaseofpregnancy,orduringlabour,

effectsontheneonate,suchashypothermia,hypotoniaandmoderaterespiratorydepressioncanbeexpectedduetothe

pharmacologicalactionoftheproduct.

Moreover,infantsborntomotherswhotookbenzodiazepineschronicallyduringthelatterstagesofpregnancymay

havedevelopedphysicaldependenceandmaybeatsomeriskofdevelopingwithdrawalsymptomsinthepostnatal

period.

Sincebenzodiazepinesarefoundinthebreastmilk,benzodiazepinesshouldnotbegiventobreastfeedingmothers.

4.7Effectsonabilitytodriveandusemachines

Sedation,amnesia,impairedconcentrationandimpairedmuscularfunctionmayadverselyaffecttheabilitytodriveor

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 30/09/2006 CRN 2028462 page number: 3

Interactions).

4.8Undesirableeffects

Drowsiness(whentheproductisusedasahypnoticitshouldbestatedexplicitly:drowsinessduringtheday),numbed

emotions,reducedalertness,confusion,fatigue,headache,dizziness,muscleweakness,ataxia,ordoublevision.These

phenomenaoccurpredominantlyatthestartoftherapyandusuallydisappearwithrepeatedadministration.

Othersideeffectslikegastrointestinaldisturbances,changesinlibidoorskinreactionshavebeenreportedoccasionally.

Amnesia:

Anterogradeamnesiamayoccurusingtherapeuticdosages,theriskincreasingathigherdosages.Amnesiceffectsmayb

associatedwithinappropriatebehaviour(seeWarningsandprecautions).

Depression:

Pre-existingdepressionmaybeunmaskedduringbenzodiazepineuse.

Psychiatricandparadoxicalreactions:

Reactionslikerestlessness,agitation,irritability,aggressiveness,delusion,rages,nightmares,hallucinations,psychoses,

inappropriatebehaviourandotheradversebehaviouraleffectsareknowntooccurwhenusingbenzodiazepinesor

benzodiazepine-likeagents.Theymaybequiteseverewiththisproduct.

Theyaremorelikelytooccurinchildrenandtheelderly.

Dependence:

Use(evenattherapeuticdoses)mayleadtothedevelopmentofphysicaldependence:discontinuationofthetherapymay

resultinwithdrawalorreboundphenomena(seeWarningsandprecautions).Psychicdependencemayoccur.Abuseof

benzodiazepineshasbeenreported.

4.9Overdose

Aswithotherbenzodiazepines,overdoseshouldnotpresentathreattolifeunlesscombinedwithotherCNSdepressants

(includingalcohol).

Inthemanagementofoverdosewithanymedicinalproduct,itshouldbeborneinmindthatmultipleagentsmayhave

beentaken.

Followingoverdosewithoralbenzodiazepines,vomitingshouldbeinduced(withinonehour)ifthepatientisconscious

gastriclavageundertakenwiththeairwayprotectedifthepatientisunconscious.Ifthereisnoadvantageinemptyingth

stomach,activatedcharcoalshouldbegiventoreduceabsorption.Specialattentionshouldbepaidtorespiratoryand

cardiovascularfunctionsinintensivecare.

Overdoseofbenzodiazepinesisusuallymanifestedbydegreesofcentralnervoussystemdepressionrangingfrom

drowsinesstocoma.Inmildcases,symptomsincludedrowsiness,mentalconfusionandlethargy,inmoreserious

cases,symptomsmayincludeataxia,hypotonia,hypotension,respiratorydepression,rarelycomaandveryrarelydeath.

Flumazenilmaybeusefulasanantidote.

5PHARMACOLOGICALPROPERTIES

5.1Pharmacodynamicproperties

Pharmacodynamicgroup:Anxiolytics,Benzodiazepinederivatives.

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 30/09/2006 CRN 2028462 page number: 4

Alprazolam,likeotherbenzodiazepines,hasahighaffinityforthebenzodiazepinebindingsiteinthebrain.Itfacilitates

theinhibitoryneurotransmitteractionofgammaaminobutyricacidwhichmediatesbothpre-andpostsynapticinhibition

inthecentralnervoussystem(CNS).

5.2Pharmacokineticproperties

Followingoraladministration,peakplasmaconcentrationsarereachedinabout1.7hours.Afterasingleoraldoseof

0.5mg,theaveragemaximalconcentrationwas7.1ng/ml.Thereisalinearrelationshipbetweenthedoseandplasma

concentration.Atleast80%oftheoraldoseisabsorbed.About70%oftheabsorbeddoseisboundtoplasmaproteins.

Alprazolamisextensivelymetabolisedintheliver,primarilytohydroxylatedmetabolites,butabout20%ofthedoseis

excretedasunchangedalprazolam.Eliminationoccursmostlyviathekidneys;80%ofthedoseisexcretedintothe

urineandonly7%intothefaeces.Themeaneliminationhalflifeis10-12hours.

5.3Preclinicalsafetydata

Thereisnopreclinicaldataofrelevancetotheprescriberwhichisadditionaltothatalreadyincludedinothersections

oftheSummaryofProductCharacteristics.

PreclinicaldatarevealsnospecialhazardforhumansbasedonconventionalstudiesofSafetyPharmacology,repeated

dosetoxicity,genotoxicity,carcinogenicpotentialandtoxicitytoreproduction.

6PHARMACEUTICALPARTICULARS

6.1Listofexcipients

Lactose

MaizeStarch

Gelatin

MagnesiumStearate

6.2Incompatibilities

Notapplicable.

6.3ShelfLife

3years.

6.4Specialprecautionsforstorage

Donotstoreabove25°C.

6.5Natureandcontentsofcontainer

Amberglassbottles(TypeIIIPh.Eur.)

Packsizes:100tablets.

6.6Specialprecautionsfordisposalofausedmedicinalproductorwastematerialsderivedfrom

suchmedicinalproductandotherhandlingoftheproduct

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 30/09/2006 CRN 2028462 page number: 5

7MARKETINGAUTHORISATIONHOLDER

OrionCorporation

Orionintie1

FIN-02200Espoo

Finland

8MARKETINGAUTHORISATIONNUMBER

PA1327/1/1

9DATEOFFIRSTAUTHORISATION/RENEWALOFTHEAUTHORISATION

Dateoffirstauthorisation:03January1995

Dateoflastrenewal:03January2005

10DATEOFREVISIONOFTHETEXT

Irish Medicines Board

______________________________________________________________________________________________________________________

Date Printed 30/09/2006 CRN 2028462 page number: 6