Class: SSRI (anti-depressant)

Name(s): Fluoxetine (Prozac), Citalopram (Celexa),

Paroxetine (Paxil), Sertraline (Zoloft)
Effects: selective inhibition of !" transporter
PK: t# $ %-&'hrs (Fluo &'-()hrs)
Uses: %
st
line - *epression, +C*, panic disorder,
eatin, disorder
Early SE: -I" . nausea, anorexia, diarrhoea/ C0S .
tremour, headache, fati,ue, irritabilit1, insomnia,
anxiet1/ Sexual . dec libido/ other . inc 2ei,ht, fever,
s2eatin,, palpitations
Cautions: earl1 anxio,enic effects ma1 a,,ravate
suicidal ideation (dec dose or add anxiol1tic)
Class: 0RI (0oradrenaline reupta3e inhibitor)
Name(s): Reboxetine
Effects: inhibits reupta3e of 04, no !" effects, can
be combined 2ith SSRI
PK: hepatic metab b1 C5Ps
Uses: ma6or depression, panic disorder, 4*!*, social
phobia
SE: dr1 mouth, constipation, headache, dro2siness,
dizziness, excessive s2eatin,, insomnia
Cautions: some dru, interactions sertraline,
paroxetine, fluoxetine, fluvoxamine, benzos,
3etoconazole, tacrolimus (P-,l1coprotein)
Class: 0aSS4 (anti-depressant)
Name(s): 7irtazapine
Effects: anta,onises 8
&
, !"
&a, &c, 9
, !% receptor:
PK: lon, half-life
Uses: Ist line - If depressed pt re;uires sedation or if
SSRI induced insomnia, sexual d1sfx are an issue
SE: dro2siness, dizziness, dr1 mouth, constipation,
2ei,ht ,ain, mild visual hallucinations
Cautions: do not combine 2ith C0S depressants
Class: RI74 (anti-depressant)
Name(s): 7oclobemide
Effects: reversible selective inhibition of 74+a
PK: short-actin,, half-life %:hrs, metab in liver b1
C5P, renal excretion
Uses: %
st
line - if depressed pt is severel1 fati,ued or
sexual d1sfx from SSRIs is a problem
SE: nausea, dizziness, a,itation, insomnia, headaches
Cautions: dru, interactions clomipramine, recent
SSRI use, dextromethorphan
Class: S0RIs (anti-depressant)
Name(s): <enlafaxine (=ffexor), *uloxetine
(c1mbaltz), *oxepin (sine;uan)
Effects: &
nd
line - non-selective inhibitor of !",
0a (> dopamine) reupta3e
PK: <enlafaxine . liver metab b1 C5Ps, renal
excretion, short half-life
Uses: severe depression, -4*
SE: 0ausea, somnolence, dr1 mouth, dizziness,
!"0
Cautions? abrupt cessation discontinuation
s1ndrome nausea, somnolence, insomnia
Class: "C4 (anti-depressant)
Name(s): Clomipramine, Imipramine, 0ortript1line,
*esipramine
Effects: anta,onism of muscarinic, 8
%
, !% receptors inc
CR=@ > @*0F inc neuro,enesis enhancement of
neuronal connectivit1 alleviate depressive Sx
PK: +/ bind to plasma albumin/ metabolized in liver/ t# $
%A-&Ahrs/
Uses: 9
rd
line - 7**
SE: 7usc . dr1 mouth, blurred vision, constipation, urinar1
retention/ 8
%
. postural !o"0, sedation, sexual d1sfx/ !% .
sedation, 2ei,ht ,ain: +B* respirator1 depression,
impaired cardiac conduction, seizures death
Contraindication: 74+I, C0S depressant
Class: 74+I (anti-depressant)
Name(s): Phenelzine, tran1lc1poramine
Effects: irreversible inhibition of 74+a > 74+b
2hich selectivel1 inactivates !", 04
PK: acet1lated in liver, renal excretion of metabolites
Uses: 9
rd
line . hi,hl1 effective, but rarel1 used
SE: "1ramine induced !"0 ( deaths) > harmful *Is
Cautions: man1 dru, interactions, must have dietar1
restriction or can induce !"0 crisis b1 inhibitin,
catabolism of dietar1 amines
Class: Lithium
Effects: un3no2n . inhibits dopamine release, enhances
serotonin releases, decreases formation of intracellular &
nd
messen,ers
PK: rapidl1 absorbed in -I", rapid pea3s in plasma but slo2 to
cross @@@, renall1 excreted unchan,ed
Uses: %
st
line . acute mania, rapid c1clin,, bipolar depressive
episodes, maintenance of bipolar
SE: common . 2ei,ht ,ain, fati,ue, headache, verti,o, tremor,
acne, psoriasis, leucoc1tosis, pol1uria, hair loss/ rare .
arrh1thmias, h1perth1roidism
Cautions: acute h1ponatraemia (increases 0a and Li
reabsorption . toxicit1), psoriasis, renal impairment, sur,er1,
elderl1, pre,nanc1, breast feedin,, has narro2 therapeutic
ratio
7ust ,raduall1 decrease unless toxicit1 occurs
Class: 4nti-convulsant
Name(s): Sodium <alproate (=pilim)
Effects: unclear . 2ea3 inhibitor of -4@4
transaminase/ 2ea3 bloc3ade of volta,e ,ated 0a
channels
PK: oral/ t# $ %&-%hrs/ excreted in urine
Uses: %
st
line - mood stabilizer in bipolar
SE: nausea, 2t ,ain, hair loss, rare severe hepatic
toxicit1, terato,enic (spina bifida)
Class: 4nti-convulsant
Name(s): Carbamazepine
Effects: bloc3ade of volta,e ,ated 0a channels
PK: t# $ 9Ahrs %hrs 2ith use/ induces hepatic enz
C5Ps
Uses: &
nd
line - mood stabilizer in bipolar, behavioural
sx in *ementia
SE: s3in rashes, bone marro2 depression (
leucopenia), liver failure
Cautions: inc metabolism of other dru,s (2arfarin,
phen1toin, +CP), interaction 2ith <alproic acid
Class: S-4
Name(s): Cuetiapine (Sero;uel), 4misulpride (Solian),
4ripriprazole
Effects: interact 2ith !"&4 RD > *& RD clinicall1 effective
2hen 'A-)AE of *& RD occupied
PK: 4rip .hepatic metab b1 C5Ps
Uses: F%
st
line - schizophrenia
SE: C . sedation, dr1 mouth, postural !o"0, a3athisia, 2ei,ht
,ain, ma1 Gseizure threshold/ 4mi . dose related =PS=, PRL
induction, nausea, insomnia/ 4rip . partial a,onism of *& RD,
a3athisia, headache, nausea, vomitin,
Cautions: Rare but serious S= - neuroleptic mali,nant
s1ndrome (muscle ri,idit1, fever, autonomic instabilit1,
delirium)
Class: S-4
Name(s): +lanzapine
Effects: interact 2ith !"&4 RD > *& RD clinicall1
effective 2hen 'A-)AE of *& RD occupied
PK: 2afer, I7 in6ection, linear 3inetics, C5P metab
Uses: &
nd
line . schizophrenia if pt refuses +ral meds/
9
rd
line . acute mania, ps1chotic depression
SE: sedation (!%RD), 2ei,ht ,ain, metabolic
s1ndrome, tardive d1s3inesia, neuroleptic mali,nant
s1ndrome
Cautions: not for elderl1 2ith dementia (inc ris3 of
stro3e)
Class: S-4
Name(s): Risperidone
Effects: interact 2ith !"&4 RD > *& RD clinicall1
effective 2hen 'A-)AE of *& RD occupied
PK: +ral > depot (for non-adherant pts)
Uses: &
nd
line . schizophrenia if pt refuses oral meds
SE: dizzinessBfaintin,, postural !o"0, PRL
menstrual problems, impotence, breast enlar,ement
> lactation, dose related =PS=
Class: F-4
Name(s): Chlorpromazine
Effects: 4nta,onism of *& > *9 RD effective 2hen HA-IAE of *& RD
occupied (=PS= 2ith JIAE occupied), also anticholiner,ic,
antihistamine effects, 4R anta,onism
PK: +ralBIn6ection/ erratic abs/ hepatic metabolism b1 C5Ps, lo2 oral
bioavail due to %
st
pass metab
PD: lo2 potenc1
Uses: &
nd
line . (after S-4s) schizophrenia
SE: antimuscarinic effects - sedation, !o"0, constipation, dr1
mouth, antiemetic, obstructive 6aundice, photosensitivit1
Cautions: earl1 =PS= (da1s) . acute d1stonias? par3insonism,
a3athisia (respond to benxtropine)/ dela1ed =PS= ()-&'mo) . tardive
d1s3inesias? can be irreversible, neuroleptic mali,nant s1ndrome,
rare . leu3openia K a,ranuloc1tosis
Intensifies C0S depressants, S= of anti!"0 dru,s, man1 dru,
interactions ("ramadol, SSRIs, barbituates)
Class: F-4
Name(s): !aloperidol
Effects: 4nta,onism of *& > *9 RD effective 2hen HA-IAE of
*& RD occupied (=PS= 2ith JIAE occupied)
PK: oralBin6ectionBdepot, hepatic metabolism
PD: hi,h potenc1, minor antihistamine K anticholiner,ic
Uses: &
nd
line . (after S-4s) schizophrenia
SE: minimal sedation, !o"0, antimuscarinic effects
Cautions: earl1 =PS= (da1s) . acute d1stonias? par3insonism,
a3athisia (respond to benxtropine)/ dela1ed =PS= ()-&'mo) .
tardive d1s3inesias? can be irreversible
Interactions: C0S depressants, Par3insonian dru,s, "C4s,
Carbamazepine, Li, 4drenaline
Contraindications: coma, stro3e, alcohol K C0S depressants,
heart disease
Class: S-4
Name(s): Clozapine
Effects: interact 2ith !"&4 RD > *& RD clinicall1 effective 2hen
'A-)AE of *& RD occupied
PK: +ral, extensive %
st
pass metab, hepatic metab b1 C5Ps
Uses: Last choice Rx for Schizophrenia > 9
rd
line mood stabilizer in
bipolar
SE: droolin,, sedation, 2ei,ht ,ain, !o"0, seizure, nausea, Serious?
agranulocytosis (%E), m1ocarditis, leu3opaenia, lo2er seizure
threshold, ps1chotic sx on discontinuation
Indications: treatment resistant schizo, lo2er =PS= ris3
Cautions: s1ner,ism 2ith sedatin, dru,s, diabetes . ris3 of
h1per,l1caemia
Contraindications: epileps1, a,ranuloc1tosis
7onitorin,? @aseline =C-, F@-, F@C, @P, L>=s, LF"s, @7I etc
F@C 2ee3l1 for %I 2ee3s, monthl1 thereafter, increased monitorin,
2hen re;uired: Stop if neutrophils M%:x%A
(
L, =C- at %' da1s, echo
at )mths, "roponin at H, then %'da1s:
Class: @enzodiazepines
Name(s): Short? oxazepam, temazepam, 7od? alprazolam, nitrazepam,
Lon,? clonazepam, diazepam
Effects: bind selectivel1 to -4@44 RD, Cl- channels open h1perpolarization
and neuronal inhibition: -4@44 mediates inhibitor1 transmission in C0S,
2hich is potentiated b1 @enzos
PK: oral, lipid soluble (accum in bod1 fats), hepatic metab, renal excretion,
Uses: 4nxiol1tic (acute anxiet1), social phobia, anticonvulsant, sedation,
alcohol 2ithdra2al sx
SE: acute toxicit1 . extended sleep, dro2siness, poor coordination
Rare? behavioural chan,es . mania, schizophrenia, an,er, impulsivit1,
h1pomania
Cautions: Combination 2ith C0S depressants lifethreatenin, respirator1
depression
Tolerance/Dependence: tolerance not P* therefore mild, dependence?
cessation causes inc anxiet1 or insomnia, sometimes convulsions
Class: 4cet1lcholinesterase inhibitors
Name(s): Rivasti,mine, *onepezil
Effects: Inhibits cholinesterases (brea3do2n
acet1lcholine)
PK: R-oral, de,raded b1 tar,et enz1mes
(cholinesterase-mediated h1drol1sis), renal excretion,
crosses @@@, *- %AAE oral bioavail, crosses @@@ easil1
Uses: alzheimerDs disease, Le21 @od1 *ementia,
m1asthenia ,ravis, antivenom
SE: autonomic . brad1cardia, h1potension,
h1persecretion, bronchoconstriction, -I"
h1permotilit1, decreased I+P
Wernicke Korsakoff Syndrome amnesic s1ndrome (alcohol
or thiamine deficienc1)
Dementia (ischaemic dama,e in brainstem)! ata"ia! #aryin$
op%t%almople$ia! nysta$mus&
'e#ersi(le if promptly treated
=1e Si,ns? n1sta,mus, bilateral lateral rectus palsies, con6u,ate
,aze palsies, fixed pupils and rarel1 papilloedema
4taxia? broad based ,ait, cerebellar si,ns and vestibular
paral1sis
Co,nitive chan,e? amnestic s1ndrome (confabulation),
restlessness, stupor, coma
!1pothermia and h1potension . due to h1pothalamic
involvement (rare)
Treatment? thiamine
Name(s): -abapentin, Pre,abalin
Effects: similar structure to -4@4, acts on volta,e-
dependent Ca channel
Uses: anticonvulsant, mi,raine, neuropathic pain,
n1sta,mus, bipolar disorder, social phobia, +C*,
treatment-resistant depression, -4*
SE: dizziness, dro2siness, peripheral oedema,
Cautions: rare adverse effects .neutropenia, %
st
de,ree heart bloc3, h1potension, h1pertension,
pancreatitis, d1spha,ia, oli,uria, rhabdom1ol1sis
Class: Serotonin receptor a,onist
Name(s): @uspirone
Effects: -!"%a pres1n RD a,onist, also *RD effects
PK: lo2 bioavail orall1, ta3es %-923s to 2or3, less
efficac1 than benzos
Uses: -4*, +C*, au,mentin, SSRIs in depression
SE: verti,o, headache, nervousness, dizziness,
a,itation, nausea, dro2siness, insomnia, rare? =PS=,
ps1chosis, hallucinations, ataxia, epileptic seizures
Contraindications: not 2ith 74+I, ,laucoma,
liverBrenal d1sfx, heart conditions
Class: -opioid receptor an,ta,onist
Name(s): 0aloxone (0arcan, 0alone), 0almefene
Effects: competitive anta,onist of -receptor, bloc3s effects of
opioids, produces rapid onset of 2ithdra2al sx
PK: 0aloxone . I<, t # )A-(Amin, rapid effects, 0almefene .
oralBI<, t # %Ahr, hepatic metab
Uses: counteract opioid overdose, 0almefene? alcohol
dependence, lon,er-actin, :? ,ood for overdose of 7ethadone
SE: Common? dro2siness, !"0, tach1cardia, dizziness, nausea,
vomitin,: +ccasional? fever, !o"0, vasodilation, chills,
headache: Rare? arrh1thmia, brad1cardia, confusion,
hallucinations, m1oclonus, itchin,
Cautions: dru, interactions . methadone, codeine, man1
others
Class: Partial a,onist and anta,onist of -receptor
Name(s): @uprenorphine (Subutex)
Effects: po2erful anal,esic properties, anta,onist properties,
hi,her bindin, affinit1 than other opioids therefore bloc3s
their activit1
PK: I7, I<, transdermal, sublin,ual tablet .hi,h %
st
pass
metab, hepatic metab b1 C5Ps
PD: hi,h-bindin, affinit1 for -receptor . 0aloxone onl1
partiall1 reverses effects
Uses: moderate to severe chronic pain, opioid 2ithdra2al
SE: dro2siness, vomitin,, respirator1 depression, orthostatic
!o"0, urinar1 retention:
Cautions: avoid C0S depressants
Class: +pioid a,onist
Name(s): 7ethadone
Effects: -receptor a,onist
PK: oral and parenteral, lon,er plasma t # than morphine, metab b1
C5Ps
Uses: moderate to severe unresponsive pain, detoxification of
opioid addiction, maintenance Rx of opioid addiction
SE: too rapid titration is more li3el1 to induce S=, respirator1
depression, !o"0, respirator1 arrest, cardiac arrest, more common?
li,htheadedness, dizziness, sedation, nausea, vomitin,, s2eatin,
Cautions: hi,h interpatient variabilit1 . titrate to effect, pre,nanc1,
hi,h potential for abuseBaddiction
Interactions? C5P inducersBinhibitors, 74+I, desipramine,
phen1toin , Carbamazepine, anti-retroviral a,ents, opioid
anta,onistsBmixedBpartial a,onists
Class: +pioid receptor anta,onist
Name(s): 0altrexone (Revia, *epade)
Effects: competitive anta,onist of and N receptor, reversibl1
bloc3s effects of opioids, does not induce dependence or
tolerance
PK: +ral, depot in trials, extensive %
st
pass metab, hepatic
metab, renal excretion, t # '-%9hrs dependin, on preparation
Uses: alcohol and opioid dependence, trials for impulse-
control disorders (e:,: self harm, ,amblin,)
SE: nausea, headache, dizziness, fati,ue, insomnia, vomitin,,
anxiet1, somnolence, sleep disturbance
Cautions: contraindicated in acute hepatitis or hepatic failure
Class: Combination of @uprenorphine and 0aloxone
Name(s): Suboxone
Effects: addition of 0aloxone prevents abuse of
@uprenorphine
PK: sublin,ual, hepatic metab b1 C5PS
Uses: opiate dependence
SE: coldBflu-li3e sx, headache, s2eatin,, sleep disturbance,
nausea, mood s2in,s, respirator1 depression
Cautions: should not be combined 2ith C0S depressants,
dru, interaction 2ith certain C5P inducersBinhibitors,
pre,nanc1 . neonatal 2ithdra2al can occur
Class:
Name(s): *isulfiram (4ntabuse)
Effects: inhibits aldeh1de deh1dro,enase accumulation of
acetaldeh1de after consumption of alcohol causin, flushin,,
nausea, vomitin,, palpitations, S+@
PK: oral, hepatic metab
Uses: aids sobriet1 in alcoholism
SE: initial dro2siness, fati,ue, metallic taste, rare? rash,
peripheral neuropath1, headache, sexual d1sfunction
Cautions: administered after pt has abstained from alcohol for
%& hrs, Contra? 3no2n cardiac disease, severe liver disease,
ma6or coexistin, ps1ch disorder, pre,nanc1 (terato,enic)
Interactions? phen1toin, 2arfarin, diazepam, anti-"@ meds
Name(s): 4camprosate (Campral)
Effects: mechanism of action not identified . thou,ht to
stabilize chemical balance that 2ould be disrupted b1 alcohol
modification of Ca ion flux, reduction of 07*4 receptor
activit1 and -4@4 a,onist activit1, does not interact 2ith
alcohol if ta3en concurrentl1
PK:
Uses: prevents alcohol relapse post 2ithdra2al, can be ,iven
2ith disulfiram
SE: diarrhoea, headache, nausea, itch
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