adverse effects
DESCRIPTION
Antipsychotics used to treat bipolar disorderTRANSCRIPT
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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$in!* e&otional quiet* reduction in initiati#e and tendency to !o off to
sleep% Spontaneous &o#e&ents are &ini&ized* but slurrin! of speech* ataxia or &otor
uncoordination does not occur% his has been referred to as the ;neuroleptic syndro&e<
and is quite different fro& the sedati#e action of barbiturates and other si&ilar dru!s%
he effects are appreciated as ;neutral< and ;unpleasant< by &ost nor&al indi#iduals
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• Catalepsy arises pri&arily fro& acute blocade of postsynaptic 5 receptors in basal
!an!lia%
• Chlorpro&azine lo(ers sei)ure threshold and can precipitate fits in untreated epileptics%
he piperazine side chain co£s ha#e a lo$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%