adverse effects

18
7/21/2019 Adverse Effects http://slidepdf.com/reader/full/adverse-effects 1/18 Antipsychotics used to treat bipolar disorder include: Abilify (aripiprazole) Clozaril (clozapine) Geodon (ziprasidone) Latuda (lurasidone) Risperdal (risperidone) Saphris (asenapine) Seroquel (quetiapine) Zyprexa (olanzapine) ru! "nteractions Additi#e effects $ith sedati#es% Additi#e effects $ith anticholiner!ics% Additi#e effects $ith antihista&iner!ics% Additi#e effects $ith α'AR blocin! dru!s% Additi#e effects $ith dru!s $ith quinidine'lie action (thioridazine)%

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Antipsychotics used to treat bipolar disorder

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Page 1: Adverse Effects

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Antipsychotics used to treat bipolar disorder  include:

• Abilify (aripiprazole)

• Clozaril (clozapine)

• Geodon (ziprasidone)

• Latuda (lurasidone)

• Risperdal (risperidone)

• Saphris (asenapine)

• Seroquel (quetiapine)

• Zyprexa (olanzapine)

ru! "nteractions

• Additi#e effects $ith sedati#es%

• Additi#e effects $ith anticholiner!ics%

• Additi#e effects $ith antihista&iner!ics%

• Additi#e effects $ith α'AR blocin! dru!s%

• Additi#e effects $ith dru!s $ith quinidine'lie action (thioridazine)%

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Side ffects of Antipsychotic ru!s

Certain antipsychotic dru!s cause si!nificant $ei!ht !ain and hi!h cholesterol le#els* and they&ay increase the ris of  diabetes% +eople considerin! an antipsychotic for bipolar disorder should

 be screened for their ris of heart disease* stroe* and diabetes* accordin! to a study published

in Diabetes Care%

Co&&on side effects of antipsychotic &edications include:

• ,lurred #ision

• ry &outh

• ro$siness

• -uscle spas&s or tre&ors

• .ei!ht !ain

• +seudodepression and Schizophrenia'lie syndro&e%

• Seizures%

• Cardiac toxicity and endocrine effects%

• /ther side'effects (dry &outh* constipation* blurred #ision* hypotension* etc%) are due to

 bloc of other receptors* particularly 01adrenoceptors and &uscarinic ACh receptors%

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•   Contact der&atitis* blood dyscrasias* obstructi#e 2aundice so&eti&es occurs $ith

 phenothiazines%

• Sedation ' initially considerable3 tolerance usually de#elops after a fe$ $ees of therapy3

dysphoria

• Postural hypotension ' results pri&arily fro& adrener!ic blocade3 tolerance can

de#elop

• Anticholinergic effects ' include blurred #ision* dry &outh* constipation* urinary

retention3 results fro& &uscarinic choliner!ic blocade

• Endocrine effects ' increased prolactin secretion can cause !alactorhea3 results fro&

antidopa&ine effect

• Hypersensitivity reactions ' 2aundice* photosensiti#ity* rashes* a!ranulocytosis can

occur 

• Idiosyncratic reactions ' &ali!nant neuroleptic syndro&e

• Weight gain

•  4eurolo!ical side effects

• ) cause anorexia%

• (5) precipitate &ania or hypo&ania%

• (6) result in nausea* ner#ousness* headache* and inso&nia%

• (7) cause 8'9 syndro&es (hyperpyrexia* con#ulsions* and co&a) $hen co&binated $ith

and -A/ inhibitor%

• EFFECTS OF ANTIPSCHOPTIC !"#$S

• %&Central Nervous Syste' 

• ffects of antipsychotic dru!s differ in nor&al and psychotic indi#iduals%

• In nor'al individuals they produce indifference to surroundin!* paucity of thou!ht*

 psycho&otor slo$in!* e&otional quiet* reduction in initiati#e and tendency to !o off to

sleep% Spontaneous &o#e&ents are &ini&ized* but slurrin! of speech* ataxia or &otor

uncoordination does not occur% his has been referred to as the ;neuroleptic syndro&e<

and is quite different fro& the sedati#e action of barbiturates and other si&ilar dru!s%

he effects are appreciated as ;neutral< and ;unpleasant< by &ost nor&al indi#iduals

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• Catalepsy arises pri&arily fro& acute blocade of postsynaptic 5 receptors in basal

!an!lia%

• Chlorpro&azine lo(ers sei)ure threshold and can precipitate fits in untreated epileptics%

he piperazine side chain co&pounds ha#e a lo$er property for this action% he

te&perature control is noced off at relati#ely hi!her doses renderin! the indi#idual

 poiilother&ic 1 body te&perature falls if surroundin! are cold% he &edullary

respiratory and other #ital centers are not affected* except at hi!h doses% "t is #ery difficult

to produce co&a $ith these dru!s% 4euroleptics* except thioridazine* ha#e potent

antie'etic action exerted throu!h the central tri!!er zone% 9o$e#er* they are ineffecti#e

in &otion sicness% 

• *&+ocal anaesthetic 

• Chlorpro&azine is as potent a local anaesthetic as procaine% 9o$e#er* it is not used for

this purpose because of its irritant action% /thers ha#e $eaer &e&brane stabilizin!

action% 

• ,&S-eletal 'uscle •  4euroleptics ha#e no effects on &uscle fibers or neuro&uscular trans&ission% hey

reduce certain types of spasticity: the site of action bein! in the basal !an!lia or &edulla

oblon!ata% Spinal reflexes are not affected%

• ANWANTE! EFFECTS 

•  4euroleptic dru!s are replete $ith side effects% -any side effects occur early

durin! treat&ent and result fro& neuroleptic blocade of receptors in the central and

 peripheral ner#ous syste&s3 others appear later in the course of treat&ent (fi!%=5)% 

• 1.”Extrapyramidal” reactions include

• Par-insonis'* $hich can &i&ic idiopathic +arinson>s disease but is usually of &ild

de!ree% "t responds to anticholiner!ic dru!s or a&antadine3 • A-atisia is a sub2ecti#e sense of restlessness usually acco&panied by $ild to &oderate

&otor hyperacti#ity% "t is a&on! the &ost co&&on of side effects and usually responds to

0'adrener !ic receptor anta!onists* anticholiner!ics* antihista&ines or a&antadine%

Aathisia is so&eti&es &isinterpreted as increased a!itation* leadin! to increased

neuroleptic dosin!* resultin! in !reater aathisia% 

• 2.Endocrine effects 

•   A* released in the &edian e&inence by neurons of the tuberohypophyseal path$ay

acts physiolo!ically #ia 5 receptors as an inhibitor of prolactin secretion% he result of

 blocin! 5 receptors by antipsychotic dru!s is therefore to increase the plas&a prolactin

concentration* resultin! .reast s(elling/ pain and lactation* $hich can occur in &en as

$ell as $o&en% /ther less pronounced endocrine chan!es includin! a decrease of !ro$th

hor&one secretion* but these* unlie the prolactin response* are uni&portant clinically% 

•  Sedation, $hich tends to decrease $ith continued use* occurs $ith &any antypsychotic

dru!s% Antihista&ine (9=) acti#ity is a property of phenothiazines and contributes to their 

sedati#e and antie&etic properties* but not to their antipsychotic action%

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"EACTION FEAT#"ES TI0E OF

0A1I0A+"IS2 

P"OPOSE!

0ECHANIS0

T"EAT0ENT

Acute dystonia Spas& of &uscles

of ton!ue* face*

nec* bac3 &ay

&i&ic seizures3

not  hysteria

= to 8 days ?nno$n Antiparinsonian

a!ents are

dia!nostic and

curati#e

Aathisia -otor restlessness3

not  anxiety or

@a!itation@

8 to B days ?nno$n Reduce dose or

chan!e dru!:

antiparinsoniana!ents*b

 benzodiazepines

or propranololc

&ay help

+arinsonis& ,radyinesia*

ri!idity* #ariable

tre&or* &as

facies* shufflin!

!ait

8 to 6B days Anta!onis& of

dopa&ine

Antiparinsonian

a!ents helpful

 4euroleptic &ali!nant

syndro&e

Catatonia* stupor*

fe#er* unstable

 blood pressure*

&yo!lobine&ia3

can be fatal

.ees3 can

 persist for

days after

stoppin!

neuroleptic

Anta!onis& of

dopa&ine &ay

contribute

Stop neuroleptic

i&&ediately:

dantrolene or

 bro&ocriptined

&ay help:

antiparinsonian

a!ents not

effecti#e

+erioral tre&or (@rabbit@syndro&e)

+erioral tre&or(&ay be a late

#ariant of p

arinsonis&)

After&onths or

years of

treat&ent

?nno$n Antiparinsoniana!ents often help

ardi#e dysinesia /ral'facial

dysinesia3

$idespread

After

&onths or

years of

xcess function

of dopa&ine

hypothesized

+re#ention

crucial3 treat&ent

unsatisfactory

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choreoathetosis or

dystonia

treat&ent

($orse on

$ithdra$al)

 -any dru!s ha#e been clai&ed to be helpful for acute dystonia% A&on! the &ost co&&only e&ployed

treat&ents are diphenhydra&ine hydrochloride* 58 or 8B &! intra&uscularly* or benztropine &esylate* = or&! intra&uscularly or slo$ly intra#enously* follo$ed by oral &edication $ith the sa&e a!ent for a period

days to perhaps se#eral $ees thereafter% .& or details re!ardin! the use of oral antiparinsonian a!ents* s

the rest of slides c& +ropranolol often is effecti#e in relati#ely lo$ doses (5B'DB &! per day)% Selecti#e beta

adrener!ic receptor anta!onists are less effecti#e% d& espite the response to dantrolene* there is no e#idenc

of an abnor&ality of Ca5E transport in seletal &uscle3 $ith lin!erin! neuroleptic effects* bro&ocriptine

&ay be tolerated in lar!e doses (=B'7B &! per day)%

6.Various idiosyncratic and hypersensitivity reaction can occur, the most important being. 

3aundice* $hich occurs $ith older phenothi)ines* such as chlorpro'a)ine& he 2aundice is

usually &ild* and of obstructi#e ori!in3 it disappears quicly $hen the dru! is stopped of

substituded by an antipsychotic of different class% 

etails on t$o &ain extrapyra&idal disturbances (+S):

F +arinson'lie sy&pto&s

 1 tre&or* ri!idity

 1 direct consequence of bloc of ni!rostriatal A5 R 

 1 re#ersible upon cessation of antipsychotics

F ardi#e dysinesia

F in#oluntary &o#e&ent of face and li&bs

F less liely $ith atypical antipsychotics (A+)

F appears &onths or years after start of A+

F result of proliferation of A R in striatu&

H presynaptic

treat&ent is !enerally unsuccessful

+henothiazines ' Side effects

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.ei!ht !ain 1 7BI ' $ei!ht !ain no$ attributed to ratio of bindin! to 5 and 8'95 receptors3

 possibly also hista&ine (for ne$er antipsychotics any$ay)

Sexual dysfunction

F result fro& 4 and S blocade

F erectile dysfunction in 56'87I of &en

F retro!rade e2aculation in

F loss of libido and anor!as&ia in &en and $o&en

Seizures ' J=I for !eneralized !rand &al

S"-A -A4 ."G9 GA"4 A =B .KS

F A co&prehensi#e literature search identified D studies that included data on $ei!htchan!e in patients treated $ith a specific antipsychotic%

F or each a!ent a &eta'analysis and rando& effects re!ression esti&ated the chan!e in

$ei!ht at =B $ees of treat&ent%

+henothiazines ' Side effects

 4euroleptic &ali!nant syndro&e (='5I early in trt)

F co&bination of &otor ri!idity* hyperther&ia* and autono&ic dysre!ulation of blood

 pressure and heart rate (both !o up)

F can be fatal in 8'5BI of cases if untreated

F treat&ent 1 discontinue &eds3 !i#e trts for fe#er and cardiac proble&s

Sensiti#ity to sun

F so&e phenothiazines collect in sin (chlorpro&azine)

F sunli!ht causes pi!&entation chan!es 1 !rayish'purple splotchin! (loo bruised)

F can also occur in eye and cause bro$n in cornea

F this produces a bro$nish cloud to #ision and possibly per&anent i&pair&ent

A!ranulocytosis ' J=I

F reduced $hite blood cell count

F lo$ered resistance to infection

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F can be fatal

Maundice 1 ele#ated bilirubin in li#er ' J NI

 4euroleptic -ali!nant Syndro&e

"s a rare but serious side effect of neuroleptic (antipsychotic) therapy that can be lethal% "t can

arise at any ti&e in the course of treat&ent and sho$s no predilection for a!e* duration of

treat&ent* antipsychotic &edication* or dose%

• /ccurs in pts% hypersensiti#e to the x%+y% effects of antipsychotics%

• ue to excessi#ely rapid blocade of postsynaptic dopa&ine receptors%

• he syndro&e be!ins $ith &ared &uscle ri!idity%

• "f s$eatin! is i&paired* a fe#er &ay ensue% he stress leuocytosis and hi!h fe#er

associated $ith this syndro&e &ay be &istaen for an infection%

• Autono&ic instability $ith altered blood pressure and heart rate is another &idbrain

&anifestation%

• Creatineinaseisozy&es are usually ele#ated* reflectin! &uscle da&a!e%

ranquilizer effects* both ad#erse and therapeutic* are !enerally less extre&e than those of

 barbiturates% olerance &ay de#elop $ithin a fe$ $ees if the dru! is continually ept in the

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 bloodstrea& by three'ti&es'a'day in!estion% Side effects &ay include apathy* lo$ blood pressure*

 blurred #ision rashes* disorientation* confusion* &uscle $eaness* head aches* upset sto&ach*

faintin!* lac of coordination* dizziness3 &enstrual* bladder* and o#ulary irre!ularities3: anxiety*

and hallucinations% So&e users experience sti&ulation rather than sedation* $hich results in

hyperex citability* inso&nia* hostility* and ra!e% Lar!e doses can lead to tre&ors* loss of &uscular 

coordination* and con#ulsions $ith ti&e and hea#y dosa!e* habituation* psycholo!ical

dependence* and $ithdra$al sy&pto&s &ay occur%

ranquilizers can ill $hen potentiated by other central ner#ous'syste& depressants such as

alcohol* barbiturates* opiates* hypnotic'sedati#es* and synthetic narcotics% Accidental poisonin!

or suicide is al&ost i&possible $ith tranquilizer unless the dru! is co&bined $ith anon

depressant%

Alcohol and tranquilizers ha#e a syner!istic effect on eachother* creatin! an additi#e result $hen

they are to!ether% Since the li#er processes alcohol first* the tranquilizer &ust $ait its turn*

circulatin! throu!h the syste& &any ti&es o#er* da&a!in! or!ans $ith each #isit% ,ody func

tions* includin! breathin!* heartbeat* and &u& ' ad reasonin! po$ers* slo$ do$n and &ay

e#entually stop* causin! death%

"n addition to alcohol* &inor tranquilizers should not be used $ith anti'depressants or

antihista&ines and &ay decrease the effecti#eness of birth'control pills3 -a2or tranquilizers

should be a#oided $hen usin! anti'depressants*

antihista&ines* barbiturates* other tranquilizers and sedati#es* blood'pressure &edication* or 

diuretics% hese sub stances* alon! $ith anti'con#ulsants* anti'coa!ulants* and -A/ inhibitors*

should also be a#oided in co&bination $ith try'cyclic anti'depressants* $hich re&ain in thesyste& for t$o $ees after their use is discontinued% All dru!s should be te&porarily a#oided

after the user has stopped tain! tri'cyclics%

Since tranquilizers depress the central ner#ous syste& and relax &uscles* they cause the userOs

reaction ti&e to increase /peratin! &achinery or po$er tools* dri#in! a car* or ridin! a bie in

traffic &ay all be hazardous to the health of the user* as alteration of #ision and ti&e* and' space

 2ud!&ent !reatly &ultiplies the chance of accident%

+re!nant $o&en should a#oid use of tranquilizers* $hich penetrate the placental barrier% ,irth

defects* fetal death* con!enital heart disease* and seletal l abnor&alities ha#e all been attributedto use of the dru!* $hich also infiltrates the &otherOs &il% he &ost publicized case of

tranquilizer3

dan!er to fetal de#elop&ent $as that of halido&ide* a non' barbiturate sleepin! pill* ori!inally

thou!ht har&less* $hich resulted in se#ere birth defects% ranquilizers are also raned third

a&on! dru!s causin! da&a!e to the sto&ach linin!* trailin! only aspirin and alcohol%

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Street tranquilizers are e#en &ore dan!erous* since they are so&eti&es cut $ith unno$n

substances* or crudely &anufactured in a&ateur laboratories* addin! to the unpredictability of an

already unpredictable dru!% ranquilizersO shelf li#es $ith so&e pills beco&in! i&potent $hile

others beco&e &ore toxic $ith the passa!e of ti&e%

Addiction* both physical and psycholo!ical* &ay occur $ith prolon!ed hea#y use% Self'

&edication is often the culprit $hen tranquilizers 'are abused% he need to increase dosa!e to

achie#e the sa&e effect si!nifies tolerance has set in%

An addicti#e personality &ay find the dru! to be a<le!iti&ate@ source to feed'his'habit* not

realizin! that $ithdra$al fro& tranquilizers &aybe as difficult as fro& alcohol* opiates* or

 barbiturates% Sedati#e* users should tae precautions% o 'not use tranquilizers for &inor

te&porary proble&s or refill prescriptions $ithout consultin! your doctor% o not use the dru!

o#er lon! periods of ti&e* follo$ directions exactly* and do not self'&edicate%

+rolon!ed &edication'Oshould not be stopped abruptly%O ranquilizer use &ust be !radually

discontinued to a#oid unpleasant $ithdra$al sy&pto&s% A dependent user &ay experience such

sy&pto&s $ithin four to ei!ht hours after cessation% 9yperexcitability and anxiety* inso&nia*

Orespiration and pulse reductions* coordination i&pair&ent* 'slurredO speech* nausea* #o&itin!*

tre&ors* and con#ulsions &ay occur* dependin! on the dru!Os potency* the #icti&Os &etabolis&*

and the len!th and frequency of use%

-edical super#ision is necessary for safe $ithdra$al fro& tranquilizers% Get the o#erdoser to a

hospital* or* if he is conscious* induce #o&itin!% o not force an unconscious person to thro$ up*

 but turn hi& on his side in case he does% o not !i#e hi& a&pheta&ines or coffee% KeepP hi&a$ae and $alin!% ind out exactly $hat he too* ho$ &uch* and $hat it looed lie* if

 possible%

ranquilizers are re!ulated under Schedule "Q of the Controlled Substances Act% +rescriptions

are not refillable &ore than fi#e ti&es $ithin six &onths* and the dru!Os production and

distribution O&ust be recorded and super#ised by &anufacturers%

Tran4uili)er Effects

?nfortunately* an addiction to tranquilizers $ill be costly to you or your lo#ed one% .hile the

 physical si!ns of addiction &ay be the &ost e#ident* the ra&ification of tranquilizer abuse does

not stop there% An addiction to tranquilizers can i&pact your life in the follo$in! $ays:

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Physically5 he recreational use of tranquilizers can har& your body physically as it interferes

$ith the nor&al &echanis&s% "n se#ere cases* death can occur* especially in the instance of 

o#erdose% hese are possible physical effects that &ay result fro& a tranquilizer addiction:

• "rre!ular sleep patterns

• isorientation* confusion

• Restlessness

• "nability to relax

• Respiratory distress or arrest

• Cardiac arrest

• Gastrointestinal distress

• ?nconsciousness or sedation

Psychologically5 A tranquilizer addiction can confuse an abuser>s perception of reality as $ell as

disturb their &ental and e&otional $ell bein!% he follo$in! are so&e psycholo!ical effects that

&ay result fro& the abuse of tranquilizers:

• Ris of anxiety or paranoia attacs

• -ood disorders* personality shifts

• eelin!s of ra!e or a!!ressi#eness

• ulled e&otional responses

• elusions or 9allucinations

Social I'pact5 he prolon!ed use of tranquilizers $ill ha#e a ne!ati#e i&pact on an indi#idual>s

social life% "f you or a lo#ed one is abusin! tranquilizers* you &ay obser#e these social effects:

• stran!ed relationships $ith fa&ily and friends

• ifficulty en!a!in! in social functions

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• "solation and increased seclusion fro& lo#ed ones

• Seclusion fro& lo#ed ones

-en and $o&en abusin! tranquilizers $ill incur da&a!e to the other facets of their li#es as $ell*

such as in their financial responsibilities* career* and $or and fa&ilial duties% or the duration of 

ti&e that tranquilizers are abused* addicts $ill continually experience these consequences until

 professional help is sou!ht and appropriate treat&ent is recei#ed%

Tran4uili)er Withdra(al

he $ithdra$al fro& tranquilizers can be a dan!erous process as the body has beco&e dependent

on the dru! and a #ariety of unpleasant sy&pto&s can be induced once the dru! is no lon!er in

the body>s syste&s% Sy&pto&s can #ary fro& person to person dependin! on ho$ lon!

tranquilizers ha#e been abused% ,ecause of the se#erity of the sy&pto&s that can result* it is

i&portant that the $ithdra$al process tae place under &edical super#ision% .ithdra$alsy&pto&s $ill usually be!in any$here fro& '6 hours after the last use of the dru! and can

include the follo$:

• Seizures

• Con#ulsions

• +sychotic episodes

• Chills

• 9ot flashes

• Loss of appetite

•  4i!ht s$eats

• Rapid breathin!

• Confusion* altered reality

• -uscle aches

• "rritability* Ra!e

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"t is usually expected that sy&pto&s $orsen and reach the pea of disco&fort around the first to

second day of the $ithdra$al process% "n certain situations* physicians &ay be able to prescribe a

&edication to help ease the disco&fort that is experienced $hile $ithdra$in! fro& tranquilizers%

reat&ent pro!ra&s tailored specifically for tranquilizer addictions $ill ha#e the necessary

resources to help indi#iduals safely $ithdra$ fro& these substances* and ha#in! this support is

in#aluable durin! the reco#er process%

Tran4uili)er Treat'ent And Help

.ith adequate support and $ith the proper resources* you can be $ell on your $ay to$ards

reco#ery fro& a tranquilizer addiction% "f you or a lo#ed one is stru!!lin! $ith a tranquilizer 

addiction* tae co&fort in no$in! that you are not alone% here is nothin! &ore #aluable than

your life* $ellness* and peace and you are deser#in! of the freedo& that is experienced apart

fro& dependence on a dru!% hou!h it &i!ht feel painfully difficult or i&possible to brea your 

addiction* tae hope in no$in! that reco#ery is al$ays an achie#able option% ou should find

treat&ent centers that $or $ith a tranquilizers addiction% ou $ill ulti&ately ha#e the ability too#erco&e this addiction by recei#in! the help you%

ANTIPSCHOTICS

6Called 0a7or Tran4uili)ers or Neuroleptics8

9"AN! NA0ES5 6Older Antipsychotics8

A&idate

Ar#ynol

al&ane

e&erol

epaote

oriden

or&alin

Geodon

9aldol

Lar!on

Lidone

Loxitane

-ellaril

-oban

 4a#ane 4e&butal

 4eurontin

 4ozinan

/rap

+er&itil

+hener!an

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+roetazine

+rolixin

+rosco&

uide

Repoise

Serlect

Seroquel

Sparine

Stelazine

aractan

e!retol

horazine

indal

opa&ax

rancopalriclos

rilafon

Qersed

Qesprin

9"AN! NA0ES5 6Ne(er Antipsychotics8

Abilify

A&bien

Clozaril

Co&pazine

La&ictalReserpine

Risperdal

Serentil

Zyprexa

Side Effects5

AathisiaT

Abnor&al !ait (&anner of $alin!)

,irth defects

,lindness

,lood disorders

,lood'su!ar 

abnor&alities

,lurred #ision

Cardiac arrest

Confusion

eath fro& li#er failure

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epression

iabetes

ro$siness

xtre&e inner'anxiety

atal blood clots

9eadache

9eart arrhyth&ia

9eart failure

9eart palpitation

9eat stroe

9e&orrha!e

9ostility

9yper!lyce&ia (abnor&ally hi!h blood su!ar)

9ypo!lyce&ia (abnor&ally lo$ blood su!ar)

"&potence"nso&nia

"n#oluntary &o#e&ents

Li!ht'headedness

-anic reaction

-uscle ri!idity

 4ausea

 4er#ousness

 4euroleptic &ali!nant

Syndro&eT

 4i!ht&ares+ainful sin rashes

+ancreatitis (infla&&ation of pancreas* a !land near the sto&ach that helps di!estion)

+oor concentration

Restlessness

Seizures

Sexual dysfunction

Sleepiness

Spas&s

Suicidal thou!hts

S$ollen and leain! breasts

achycardia (heart irre!ularity)

ardi#e dysinesiaT

re&ors

Qiolence

Qo&itin!

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.eaness

.ei!ht !ainD

TAathisia: A* &eanin! ;$ithout< and athisia* &eanin! ;sittin!*< an inability to eep still%

+atients pace about uncontrollably% he side effect has been lined to assaulti#e*

#iolent beha#ior%U

T4euroleptic &ali!nant syndro&e: A potentially fatal toxic reaction $here patients brea into

fe#ers and beco&e confused* a!itated* and extre&ely ri!id% An esti&ated =BB*BBB A&ericans

ha#e died fro& it after tain! the older antipsychotics%B

Tardi#e ysinesia: ardi#e* &eanin! ;late< and dysinesia &eanin!* ;abnor&al &o#e&ent of

&uscles%< ardi#e ysinesia is a per&anent i&pair&ent of the po$er of #oluntary &o#e&ent of 

the lips* ton!ue* 2a$* fin!ers* toes* and other body parts%=

Tran4uili)ers5 Physiological effects

Last &odified: Saturday* 5B% Mune 5BBU ' 6:7 p&

,eneficial +hysiolo!ical effects of the &a2or and &inor tranquilizers include:

F anesthesia

F anticon#ulsant effects

F blood #essel dilation

F decreased contrasctability of the heart

F decreased hyperacti#ity* i&pulsi#ity* and a!!ression

F &uscle relaxation

F pain relief 

F reduced &uscle spas&s

F relaxation

F sedation

F slo$ed heart rate

 Harmful side effects

At hi!h doses* both the &a2or and &inor tranquilizers are se#erely toxic and &ay cause co&a*

respiratory arrest* con#ulsions* acute renal failure* speech i&pair&ent* or death% 9o$e#er* at

therapeutic doses* the neu'roleptics ha#e been associated $ith &ore

Atypical antipsychotic a!ent istincti#e features Aripiprazole F partial a!onist at 5 and 8'

9=A receptor F "t is &ini&ally sedatin!* &ay e#en cause inso&nia F -etabolized by C+5

and C+6A7% F AR: nausea* dyspepsia* constipation and li!ht'headedness%

hyperprolactinae&ia* hypotension and ' prolon!ation are not frequent% Ziprasidone F 5 E 8'

95AV5C E 9= E 0= receptor blocin! acti#ity% F fficacy in schizophrenia has been related

equi#alent to haloperidol A&isulpiride F Con!ener of sulpiride (typical antipsychotic) F 9i!h

affinity to 5 (and 6) receptor and has lo$ affinity for 8' 95 receptor% F 4ot sedati#e%

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Zotepine F =E5 and 8'95* 0= receptor blocin! acti#ity% F "t also inhibits 4A reuptae% F

,oth positi#e and ne!ati#e sy&pto&s of schizophrenia appear to be benefited% F "t has lo$er

seizure threshold% F AR: .ei!ht !ain* hyper!lyce&ia%

67%  Ad#erse e#ents F C4S: ro$siness* lethar!y* &ental confusion* $ei!ht !ain (not $ith

haloperidol)* a!!ra#ation of seizures in epileptics% F CQS: +ostural hypotension* palpitation*

inhibition of e2aculation (especially $ith thioridazine) are due to a adrener!ic blocade3 '

 prolon!ation and cardiac arrhyth&ias are ris of o#erdose $ith thioridazine* pi&ozide and

ziprasidone% F Anticholiner!ic ry &outh* blurrin! of #ision* constipation* urinary hesitancy

in elderly &ales% F ndocrine 9yperprolactine&ia (due to 5 blocade) is co&&on $ith

typical neuroleptics and risperidone% his can lo$er G9 le#els* but a&enorrhoea* infertility*

!alactorrhoea and !ynaeco&astia occur infrequently after prolon!ed treat&ent% F -etabolic

effect: le#ation of blood su!ar and tri!lyceride%

68%  Ad#erse e#ents F xtrapyra&idal disturbances: ose'li&itin! side effects% 1 he inhibitory

effects of dopa&iner!ic neurons are nor&ally balanced by the excitatory actions of choliner!ic

neurons in the striatu&% ,locin! dopa&ine receptors alters this balance* causin! a relati#eexcess of choliner!ic influence* $hich results in extrapyra&idal &otor effects% 1 +arinson'lie

sy&pto&s of bradyinesia* ri!idity* and tre&or usually occur $ithin $ees to &onths of

initiatin! treat&ent% ardi#e dysinesia* $hich can be irre#ersible* &ay occur after &onths or

years of treat&ent% F 9ypersensiti#ity reaction: Chlestatic 2aundice* &yocarditis* a!ranulocytosis%

F -iscellaneous: .ei!ht !ain often occurs $ith lon! ter& antipsychotic therapy3 blood su!ar and

lipids &ay tend to rise% Ris of $orsenin! of diabetes and blue pi!&entation of exposed sin* and

retinal de!eneration% ardi#e dysinesia is a disorder that in#ol#es in#oluntary &o#e&ents*

especially of the lo$er face (ton!ue* lips* face* trun* and extre&ities)%

=% 6%  herapeutic uses F reat&ent of schizophrenia F +re#ention of se#ere nausea and

#o&itin! F /ther uses: 1 reat&ent of &ania* or!anic brain syndro&es* anxiety% 1Chlorpro&azine is used to treat intractable hiccups% 1 Risperidone and haloperidol are

also co&&only prescribed for this tic disorder% Also* risperidone and aripiprazole are no$

appro#ed for the &ana!e&ent of the disrupti#e beha#ior and irritability secondary to

autis& (is a disorder of neural de#elop&ent characterized by i&paired social interaction)%

"EFE"ENCES 

=% +har&acolo!y* ourth dition* 9%+%Ran!* -%-%ale* M%-%Ritter* C9?RC9"LL

L"Q"4GS/4* 5BB=%

5% 9u&an +har&acolo!y* -olecular to Clinical* hird dition* %,rody* M%Larner*

K%-inne&an* -osby* =UUD by -osby'ear ,oo*"nc%

6% ,asic W Clinical +har&acolo!y% A LA4G &edical boo% D ""/4* ,%G%Katzun!*

5BB=* -cGra$'9ill Co&p%

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4. Lippincott>s "llustrated Re#ie$s: +har&acolo!y* 5nd dition* -%M%-yce* R%A%9ar#ey W

+%C%Cha&pe* L"++"4C/ ."LL"A-S W ."LK"4S* 5BBB%