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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

P450 inhibitors include

fluvoxamine, fluoxetine, paroxetine, duloxetine, sertraline
-- all the OCD SSRIs + duloxetine