Flashcards in export_psychopharm 2 Deck (140)
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1
Typical Antipsychotics Mechanism of Action
D2 antagonism
-- secondary = blockage of muscarinic, a adrenergic, and histamine 1 receptors
2
mesolimbic pathway blockade responsible for
positive symptoms (delusions, hallucinations)
3
nigrostriatal pathway responsible for
EPS
4
tuberoinfundibular pathway responsible for
hyperprolactinemia
5
mesocortical pathway responsible for
worsening negative symptoms (alogia, avolition) and cognitive symptoms
6
side effects of high v. low potency
high - worse EPS
low - worse anticholinergic, anti-histaminergic, anti-adrenergic
7
indications for typical antipsychotics
schizophrenia, schizoaffective, brief psychotic disorder, substance and medication induced psychosis
- depression w/ psychotic features, acute manic, depressed and mixed manic states of bipolar disorder
- Tourette's and Huntington's
8
Adverse effects of typical antipsychotics
* EPS (akathisia, dystonia, parkinsonism)
* hyperprolactinemia
* sedation, weight gain, anticholinergic (dry mouth, constipation, blurry vision)
* tardive dyskinesia
* NMS (hyperpyrexia, autonomic instability, muscle rigidity, delirium)
9
treatment of akathisia
anticholinergics, beta blockers or benzos
10
treatment of dystonia
PO or IM anticholinergics
11
treatment of parkinsonism
anticholinergics, dopaminergic agents (amantidine) or beta blockers
12
anticholinergic side effects of typical antipsychotics
dry mouth, constipation, blurry vision, urine retention, confusion, EKG changes, orthostatic hypotension, decreased seizure threshold, sex dysfunction, dermatitis/photosensitivity
13
high potency typical antipsychotics
* haloperidol (PO, IM, depot)
* fluphenazine (prolixin) - PO, IM and depot
* pimozide (orap)
* thithixene (navane)
* trifluoperazine (stelazine)
14
mid potency typical antipsychotics
* perphenazine (trilafom) - PO, IM
* molindone (moban)
* loxapine (loxitane)
15
low potency typical antipsychotics
* chlorpromazine (thorazine) - highly sedating, significant hypotension and anticholinergic effects but low EPS
* mesoridazine (serentil)
* thioridazine (mellaril) - least EPS of all typicals, QT prolongation, retinitis pigmentosa at high doses
16
atypical antipsychotics mechanism of action
D2 antagonism and serotonin 2A antagonism
- also muscarinic, alpha adrenergic and histamine 1 to varying degrees
17
side effects of atypical antipsychotics
* metabolic problems (hyperglycemia, DM II, hyperlipidemia)
* lower incidence of TD, NMS and EPS (except risperidone)
* olanzapine/clozapine have highest risk of metabolic syndrome
18
indications for atypical antipsychotics
* all except clozapine - acute mania
* olanzapine and aripiprazole - prophylaxis of recurrent mania and bipolar maintenance
19
Clozapine mechanism of action
- 5HT2A, D1, D2, D4, H1, muscarinic and a1 antagonism
- most efficacious antipsychotic
20
clozapine indications/contraindications
* typical antipsychotic indications
* treatment of refractory schizophrenia
* schizophrenia concurrent with TD
* contra: granulocytopenia, diabetes/hyperlipidemia
21
clozapine adverse effects/toxicities
sedation, anticholinergic side effects, orthostatic hypotension, weigh gain, hypersalivation, seizures, metabolic problems, agranulocytosis
22
risperidone mechanism of action
5HT2A, D2 and a1 antagonism
- PO, dissolvable tab and IM forms
23
risperidone indications/contraindications
* typical antipsychotic indications
* acute mania
24
risperidone adverse effects/toxicities
* orthostatic hypotension, reflex tachy, dizziness, metabolic probs
* insomnia, agitation, weight gain, hyperprolactinemia
* at higher doses ( >6mg), EPS
25
olanzapine (zyprexa) mechanism of action
5HT2A, D1, D2, D4, H1, muscarinic and a1 antagonism
26
olanzapine indications
* typical antipsychotic indications
* acute mania
* bipolar maintenance
* contra: diabetes/hyperlipidemia
27
olanzapine adverse effects/toxicities
anticholinergic SE, orthostatic hypotension and dizziness, weight gain (SUBSTANTIAL), hyperglycemia, DM II, hyperlipidemia, DKA
28
quetiapine (seroquel) mechanism of action
5HT2A, D2, a1, a2 and H1
29
quetiapine indications/contraindications
* typical antipsychotic indications
* acute mania
* bipolar depression
* adjunctive - unipolar depression
30
quetiapine adverse effects/toxicities
orthostatic hypotension, and dizziness, sedation, weight gain, metabolic problems
31
ziprasidone (Geodon) mechanism of action
* HGT1, 5HT2, D2, D3, and monoamine (NE, 5HT, DA) reuptake pumps
* PO and fast acting IM
32
ziprasidone indications/contraindications
* typical antipsychotic indications
* acute mania
33
ziprasidone adverse effects/toxicities
* sedation, weight gain (less than others)
* metabolic probs (DM, hyperlipidemia, less than others)
* increased risk for QT prolongation -EKG!
34
aripiprazole (abilify) mechanism of action
* 5HT2A, partial agonist of D2 and 5HT1A
35
aripiprazole indications/contraindications
* typical antipsychotic indications
* acute mania
* bipolar maintenance
* adjunct - unipolar depression
36
aripiprazole adverse effects/toxicities
* sedation, weight gain, metabolic problems
37
paliperidone
metabolite of risperidone
38
paliperidone indications/contraindications
typical antipsychotic indications
39
paliperidone adverse effects/toxicities
possibly less EPS than risperidone
40
iloperidone indications/contraindications, adverse effects/toxicities
* typical antipsychotic indications
* possibly less weight gain than other atypicals, increased risk of QT prolongation
41
asenapine
* typical antipsychotic indications
* ?novel mechanism of action
42
lurasidone
* typical antipsychotic indications
* possibly less weight gain tan other atypicals
43
Amitriptyline
TCA - tertiary amine
* wide use for pain, headache or insomnia
44
Clomipramine
TCA - tertiary amine
* highly serotinergic
* indicated for OCD
45
doxepin
TCA - tertiary amine
* used for pain, insomnia and anxiety
46
imipramine
TCA - tertiary amine
* useful for panic, enuresis
47
desipramine
TCA - secondary amine
* demethylated imipramine
* least anticholinergic
48
nortriptyline
TCA - secondary amine
* demethylated amitriptyline
* least orthostasis
49
TCA mechanism of action
* antagonism of 5HT and NE presynaptic re-uptake pumps
* also known to block muscarinic, a-adrenergic, and histamine-1 receptors
* therapeutic effect after 3-4 wks
* secondary amines are less sedating and safer in overdose
50
TCA indications/contraindications
* MDD, Bipolar Depression, Dysthymia, panic disorder, generalized social phobia, GAD, OCD (clomipramine), pain disorders (migraines/neuralgia)
* cardiac conduction delays, arrhythmias, BPH, excoriations on hands
51
TCA adverse effects
* anticholinergic: sedation, weight gain, orthostatic hypotension, sex dysfunction, mania in BPD, seizures
* cardiotoxicity - slows conduction, EKG changes, arrhythmias, AV block
* neurotoxicity - tremor and ataxia, overdose = agitation, delerium, coma and death
52
MAOi mechanism of action
irreversible monoamine oxidase inhibitors (5HT, DA, NE)
* also block some alpha-1 adrenergic receptors and H1 receptors
* use for people with chronic pain/atypical depression
* do not use with sickle cell or migraine --> hypertensive crisis
53
MAOi adverse effects
* severe orthostatic hypotension
* weight gain, sex dysfunction, insomnia, myoclonus, muscle pains and paresthesias, mania
* tyramine induced hypertensive crisis (no aged cheese, fava beans, liver)
* minimal anticholinergic effects
54
phenalzine (Nardil)
MAOi
55
tranylcypromine (Parnate)
MAOi
56
transdermal Selegiline (Emsam)
patch MAOi with lower dietary restrictions at lower dose
57
SSRIs
mechanism of action: antagonism of 5HT presynaptic reuptake pumps
threrapeutic effect in 3-4 wks
sage, well tolerated and widely indicated, blood thinning capabilities
58
SSRI indications
MDD, PMDD, PTSD, Bulimia, Panic Disorder, Social Phobia, OCD
x coadministration with MAOIs
59
SSRI Adverse Effects
- 5HT3: diarrhea, nausea, vomiting
- 5HT2C: anxiety and mental agitation
- 5HT2A: anxiety and mental agitation, akathisia, insomnia, myoclonus and sex dysfunction
- weigh gain, mania, serotonin discontinuation syndrome (headache, dizziness, irritability and fatigue)
- serotonin syndrome: HARM - hyperthermia, autonomic instability, rigidity, myoclonus, coma and death
60
fluoxetine
Prozac
- longest half life, efficacy in bullimia
- if pregnant, use this
61
paroxetine
Paxil
- more sedating than fluoxetine or sertraline
- do not use in patients with constipation or diarrhea
62
sertraline
Zoloft
- less sedating than paroxetine
- if breast feeding, use this
- cleared mainly by the liver so use in pts with renal failure
63
fluvoxamine
Luvox, SSRI for OCD
64
citalopram, escitalopram
SSRIs
65
SNRIs
selective antagonists of NE and 5HT reuptake
-- no alpha, histamine-1 or muscarinic blockade (avoids TCA side effects)
-- additional dopamine reuptake inhibition at higher doses --> curvilinear dose response
66
SNRI indications
MDD, GAD, Panic Disorder, Generalized Social Phobia
x coadministration with MAOis
67
SNRI adverse effects
tremor, agitation, tachycardia, HTN, diarrhea, n/v, anxiety and mental agitation, akathisia, insomnia, myoclonus, sex dysfunction, seizures, mania and discontinuation syndrome
68
venlafaxine
SNRI - Effexor - superior efficacy for depression among new antidepressants
69
duloxetine
SNRI, Cymbalta, nausea common, approved for diabetic neuropathy
70
NaSSAs
antagonism of central a2 autoreceptors (disinhibition of NE and 5HT release), stimulation of a1 somatodendritic receptors on serotonin neurons, boosting 5HT release
71
NaSSA indications
MDD
x coadmin with MAOis
72
NaSSA adverse effects
sedation (significant, often used as sleep aid), increased appetite and weight gain
agranulocytosis and other blood dyscrasias
73
mirtazepine
NaSSA
Remeron
also blocks 5HT2A, 2c, 3, and H1 receptors
74
Noradrenergic and Dopamine Reuptake inhibitors mech of action and indications
antagonists of presynaptic NE and DA reuptake
- MDD, Bipolar Depression, ADHD, Smoking Cessation
x MAOIs, anorexia, bulimia, seizure disorder
75
Bupropion - class and SE
Wellbutrin - Noradrenergic and Dopamine Reuptake inhibitor
- side effects: activation, insomnia, nausea, tremor, seizure at higher doses
76
SARIs mechanism and indications
mech of action: selective antagonism of 5HT reuptake and simultaneous 5HT2A blockade
- indications: MDD, dysthymia
x coadmin with MAOI
77
trazodone
SARI, might cause priapism
78
SARI side effects
sedation, nausea, dizziness and mania
-- due to 5HT2A blockade, sexual dysfunction is avoided
79
nefazodone
SARI
may have liver toxicity (black box warning)
80
vilazodone
* selective serotonin reuptake inhibitor and serotonin partial agonist
* indications: MDD, no coadmin with MAOIs
* adverse effects: similar to SSRI (less sex dysfunction and weight gain maybe)
81
Benzodiazepines
* full agonism of benzo binding site to the GABAa receptor, potentiating GABA by causing increased freq of Cl channel openings
* high potency - more efficacious and addictive, shorter half-life - more rapid in onset addictive
* cross-tolerant with alcohol and barbiturates, allowing their use in detox in sedative and alcohol addiction
82
indications/contraindications of benzos
- GAD, situational anxiety/phobias, panic disorder, epilepsy, muscle spasms, akathisia, alcohol withdrawal, agitation, anxiety associated with other psychiatric disorders, substance dependence
83
benzos that are safe in liver disease
lorazepam, oxazepam, temazepam (LOT)
-- these are all short half life
84
adverse effects of benzos
drowsiness, dizziness or ataxia, cognitive impairment and/or amnesia, tolerance, dependence, withdrawal symptoms include anxiety, insomnia, restlessness, agitation, irritability, and muscle tension
- overdose can be treated with flumazenil
85
alprazolam
benzo - xanax
* short half-life
* greatest addictive potential but very effective for panic
86
lorazepam
benzo - ativan
* short half-life
* available in PO, IM and IV forms, widely used
* Haldol and ativan if agitated
87
oxazepam
benzo - serax
* short half life
88
temazepam
benzo - restoril
* short half-life
* effective short-term sleep aid
89
clonazepam
benzo - Klonipin
* long half life
90
diazepam
benzo - Valium
* long half life
* fast onset but with active metabolite
91
chlordiazepoxide
benzo - librium
* long half life
* alcohol detox
92
bispirone
* 5HT1a agonist, onset of action at least 2 weeks
* indications: GAD, adjunctive use in MDD
* adverse effects: dizziness, HA, fatigue, GI distress
* does not have sedation or addictive potential of benzos
93
hydroxyzine
* sedating antihistamine - non benzo anxiolytic
* indications: situational anxiety
* adverse effects: sedation and weight gain, anticholinergic SE
94
propranolol
* b blocker
* indications: performance anxiety
* contraindications: asthma
* adverse effects: dizziness, fatigue, bradycardia and HTN
95
zolpidem
ambien
* GABAergic
* indication: insomnia
* adverse effects: dizziness, nausea, vomiting, GI distress
96
zaleplon
sonata
* GABAergic, suggested to not yield tolerance
* indication: insomnia
* adverse effects: headache
97
dephenhydramine
benadryl
* sedating antihistamine
* indications: insomnia
* adverse effects: sedation, weight gain, anticholinergic SE
98
ramelteon
rozerem
* agonist at melatonin MT-1 and MT-2 receptors, thought to normalize cardiac rhythms
* indications: insomnia
* adverse effects: dizziness, fatigue
99
Lithium
* cleared almost entirely by the kidney
* indications: BP I, BP II, Bipolar maintenance, intermittent explosive disorder, adjunct to antidepressants
* contra: preggo --> Ebstein, caution with diuretics (all except mannitol and acetazolamide), ACE-inhibitors, and NSAIDS, all of which can raise levels (caffeine and theophylene can lower)
100
Lithium adverse effects
* GI irritation
* polyuria, polydypsia, nephrogenic diabetes insipidus
* tremor, subtle incoordination, cognitive blunting
* benign leukocytosis
101
lithium toxicity
* nausea, diarrhea, vomiting, oliguria, ataxia, coarse tremor, increased DTRs, obtundation, seizure and death
* thyrotoxic, nephrotoxic, cardiac arrhythmias and T wave flattening
102
when do you check lithium?
5 days after starting, 5 days after dose change, then 1 mo., 3 mo. and every 6 mo.
103
carbamezapine
tegretol
* effects on Na/K channels
* known to decrease the effect of other drugs (like birth control)
104
carbamezapine indications
* BP I, mixed mania and rapid cycling, BP II, epilepsy and neuralgias, alcohol withdrawal
* pregnant women - can cause craniofacial abnormalities like cleft lip and paalte, neural tube defects and learning disorders
105
carbamezapine adverse effects
* n/v, diarrhea
* sedation, lightheadedness, tremor, cognitive blunting
* hyponatremia (SIADH), anticholinergic side effects, SJS, hepatotoxicity
* blood dyscrasias (aplastic anemia, agranulocytosis, thrombocytopenia)
* overdose --> coarse tremor, coma, death
106
valproic acid
depakote
* inhibits Na/Ca channels, boosting GABA and decreasing glutamate
* cab ne rapidly loaded for quicker therapeutic effect
107
valproic acid indications/contraindications
* BP I, mixed mania, rapid cycling, BP II, epilepsy, neuralgias, alcohol withdrawal
* pregnant women - can cause neural tube defects to a greater degree than carbamezapine
* PCOS
* lamotrigine stimulates the metabolism of depakote
108
valproic acid adverse effects
* n/v, diarrhea
* sedation, lightheadedness, tremor, cognitive blunting
* weight gain
* hair loss
* thrombocytopenia, pancretitis, hepatotoxicity, polycystic ovaries
* overdose can cause coarse tremor, coma and death
109
oxcarbazepine
trileptal
* has effects at Na/K/Ca channels, possibly enhances GABA
* structurally related to carbamezapine
* more likely to cause hyponatremia (CPM!)
110
oxcarmezapine indications/contraindications
* BP I, adjunctive treatment
* epilepsy and neuralgias
111
oxcarbazepine adverse effects
* n/v, diarrhea
* sedation, lightheadedness, tremor
* cognitive blunting
* rash
* therapeutic blood monitoring necessary
112
lamotrigine
lamictal
* has effects at Na, possibly inhibits glutamate
* FDA for bipolar maintenance
113
lamotrigine indications/contraindications
* BP maintenance, epilepst and neuralgias
* caution when given with valproic acid, valproic acid boosts the blood levels of lamotrigine by decreasing metabolism of lamotrigine
114
lamotrigine adverse effects
* n/v, diarrhea
* sedation, lightheadedness, tremor
* cognitive blunting
* weight gain
* rash (common), may --> SJS
115
gabapentin
neurontin
* GABAergic, excreted renally
* ineffective as monotherapy for mania
* also off label use in GAD and social anxiety
116
gabapentin indications
* BP I, adjunctive treatment
* epilepsy and neuralgias
* caution in renal disease
117
gabapentin adverse effects
sedation, lightheadedness, tremor, n/v, diarrhea
118
topiramate indications
topamax
- ineffective monotherapy for mania
- epilepsy and neuralgias
119
topiramate adverse effects
* sedation, lightheadedness, cognitive dulling
* nausea
* nephrolithiasis
* anorexia and weight loss -- causes taste aversion
120
SSRIs for PTSD
Please See
Paroxetine, Sertraline
121
SSRIs for OCD
Fresh Frozen Plasma and Serum
Fluoxetine, Fluvoxamine, Paroxetine, Sertraline
122
SSRIs for Social Phobia
St. Vincent Paul
Sertraline, Venlafaxine, paroxetine
123
SSRIs for Panic Disorder
RSVP
fluvoxamine XR, sertraline, venlafaxine, paroxetine
124
SSRIs for GAD
Dr Poag East Village
Duloxetine, paroxetine, escitalopram, venlafaxine
125
risperidone OD symptoms
EPS, long QTc, NMS (rigid with fever)
126
which atypical antipsychotics are more weight neutral?
ziprasidone, abilify
127
TCA overdose signs and treatment
anticholinergic, delirium
--treat with Na bicarb
128
which SSRI do you give to terminally ill/cancer patients and why?
mirtazepine (NaSSA) because it has a parenteral formulation and causes increased appetite and weight gain
129
what does OD on benzos look like?
delerium, sedation
130
what does Li overdose look like, what level leads to death and how do you treat OD?
- n/v, diarrhea, oliguria, atadia, coarse tremor, increased DTRs, obtundation, seizure and death
- >4 --> death
- in OD, give kahexalate and do dialysis, charcoal does not help
131
old stimulant indications/contraindications
Ritalin: ADD, Narcolepsy
- do not give with MAOis, or narrow angle glaucoma
132
what are the old stimulants?
methylphenidate (Ritalin), dexmethylphenidate (Focalin), Dextromethamphetamine (Dexidrine), Dextromethamphetamine/amphetamine (Adderall), Pemoline (Cylert)
133
what are the adverse effects of old stimulants?
anxiety, insomnia (decreased appetite), tachy, drug dependence, HTN, cardiac arrhythmias, cardiovascular collapse
134
Modafinil indications/contrindications
stimulant (Provigil)
- narcolepsy, ADD, primary and seconday hyperinsomnia
- do not coadminister with MAOis
135
Modafinil adverse effects
headache, nausea, rhinitis, anxiety, insomnia
136
Atomoxetine
Straterra
- ADD
- do not coadminister with MAOis, or narrow angle glaucoma
137
Atomoxetine adverse effects
dyspepsia, n/v, anorexia, dizziness, insomnia, sexual dysfunction, SI (black box warning), severe liver injury
138
P450 inducers
smoking, carbamezapine, St. John's wart, barbiturates
139
treat EPS with (drug of choice)
benzotropine
140
