Neuropsych drugs

Question 1

chlorpromazine (Thorazine)

Answer 1

Class: Low potency 1st gen antipsychotic (FGA, typical)

MoA: Blocks many receptors in CNS and PNS: dopamine, AcH, H1, NE & Alpha 1 & 2

Uses: Mainly schizophrenia, schizoaffective disorder, manic BPD episodes, intractable hiccups, emesis, behavioral problems in kids, delirium

Admin: PO, IM, IV.

Considerations: incr r/f CNS depression w benzos, benadryl, ETOH, opioids, barbiturates, some antidepressants. Incr r/f hypotension w/ antihypertensives d/t effect on NE.

AEs: Extrapyramidal symptoms: Acute dystonia. Parkinsonism. Akathisia. Tardive dyskinesia.
NMS.
Anticholinergic effects.
Orthostatic hypotension d/t blockade of Alpha receptors causing vasodilation.
Cardiac dysrhythmias.
Sedation (1st week).
Agranulocytosis.
Sexual dysfunction, gynecomastia, galactorrhea, menstrual irregularity, incr. sensitivity to sunlight, sunburns, seizures, r/f death in elderly.

Question 2

Parkinsonism symptoms

Answer 2

bradykinesia, drooling, rigidity, shuffling gait, stooped posture

Question 3

Akathisia

Answer 3

uncontrollable need to move

Question 4

Tardive dyskinesia

Answer 4

twisting/worm-like
movements of the tongue/face, lip smacking
& tongue darting. Can interfere with chewing which can result in malnutrition/ weight loss. Sometimes irreversible even after stopping treatment.

Question 5

NMS

Answer 5

(Neuroleptic Malignant Syndrome)
“lead pipe” rigidity, sweating, dysrhythmias, fever,
confusion & restlessness. Rare but can be fatal.

Question 6

Anticholinergic effects of chlorpromazine (Thorazine)

Answer 6

Due to blockade of AcH: dry mouth, constipation, urinary frequency/retention, tachycardia & blurred vision

Question 7

Cardiac dysrhythmias side effect of chlorpromazine (Thorazine) considerations

Answer 7

prolong QT interval. Check ECG and check K+ before starting drug.

Question 8

Agranulocytosis SE of chlorpromazine (Thorazine)

Answer 8

rare but serious AE
characterized by ↓ WBC ct. → ↑’d R/F infx. Check WBC ct. before starting treatment

Question 9

Acute dystonia

Answer 9

severe muscle spasms of the tongue, face, neck & back. Medical emergency; can affect breathing. Requires immediate admin of Benadryl.

Question 10

Extrapyramidal symptoms (EPS)

Answer 10

likely d/t blockage of DA receptor sites in the EPS of the brain:
Acute Dystonia
Parkinsonism
Akathisia
Tardive dyskinesia

Question 11

haloperidol (Haldol)

Answer 11

Class: High potency FGA (typical)

MoA: Same as thorazine

Uses: Schizophrenia, acute psychosis, Tourette’s, severe behavioral issues in kids. The most often used drug of the FGA’s.

Admin: PO, IV, IM

Considerations: incr. r/f dysrhythmias with amiodarone, erythromycin & quinidine. Check ECG & K+ before starting. Use caution in pts w/ hx of dysrhythmias, K+ imbalance, heart disease & elderly

AEs: Early EPS reactions. More likely to occur w/ high potency than low potency FGAs.

Sedation, hypotension & anticholinergic effects uncommon

Gynecomastia, galactorrhea & menstrual irregularity

Fatal arrhythmias

Question 12

risperidone (Risperdal)

Answer 12

Class: Second generation antipsychotic (SGA, atypical)

MoA: Blocks 5-HT2 (serotonin), DA, H1 & Alpha-adrenergic receptors

Uses: Schizophrenia & bipolar mania. Approved for autistic kids w/ severe behavioral problems.

Admin: PO & IM. Rapidly absorbed and long lasting. Decrease dose w/ renal or hepatic impairment.

Considerations: ↑ R/F CNS depression w/ benzo’s, 1st gen. antihistamines, ETOH, opioids, barbiturates, FGA’s & some antidepressants.
↑ R/F hypotension w/antihypertensives

AEs: Metabolic Symptoms: Wt. gain, diabetes & dyslipidemia. Check fasting blood glucose and lipid panel before starting therapy.

EPS risk very low with low doses

May cause agitation, tremors, dizziness, sedation, fatigue

↑ R/F death in elderly

Question 13

clozapine (Clozaril) or aripiprazole (Abilify)

Answer 13

Class: Second generation antipsychotic (SGA, atypical)

MoA: Same as risperidone.

Uses: Schizophrenia, bipolar mania, major depressive disorder, agitation & irritability a/w autism. Adjunctive Tx for OCD. Safest SGA.

Admin: PO & IM,

Considerations: ↓ drug levels w/ barbiturates, rifampin, Tegretol & Dilantin

↑ drug levels w/ many antifungals, erythromycin, quinidine, Paxil & Prozac

AEs: HA, agitation, nervousness, anxiety, insomnia, n/v, dizziness & somnolence

Incidence of wt. gain, diabetes & dyslipidemia lowest of all SGA’s

R/F EPS & orthostatic hypotension low

NMS (Neuroleptic Malignant Syndrome) very rare

↑ R/F death in elderly same as other antipsychotics

Question 14

Serotonin syndrome

Answer 14

a serious and can be fatal reaction with hypertensive crisis, hyperpyrexia, extreme agitation progressing to delirium and coma, muscle rigidity and seizures. (Altered mental status, dyscoordination, myoclonus hyperreflexia, overactive sweating, tremors & fever)

Question 15

fluoxetine (Prozac)

Answer 15

Class: SSRI

MoA: Blocks reuptake of serotonin (5-HT) resulting in increased serotonin availability at synapses

Uses: MDD, BPD, OCD, panic disorder, bulimia, PMDD

Off label: PTSD, social phobia, alcoholism, ADHD, migraines, obesity, tourette’s

Admin: PO.

Considerations: Use w/ MAOIs increases r/f serotonin syndrome. Increases TCAs and Lithium drug levels. Incr. r/f bleeding w antiplatelets & anticoags

AEs: Sexual dysfunction, nausea, diarrhea, HA, excessive sweating, weight gain, & insomnia most common

Serotonin syndrome.

Withdrawal syndrome w/ abrupt DC (dizziness, HA, n/v sensory disturbances, tremors, anxiety & dysphoria)

If taken during last part of pregnancy, may cause AE’s in the newborn

Bruxism- clenching/grinding of teeth

Hyponatremia in older pts taking diuretics

Bleeding Disorders- R/F GI bleed increased 3-fold. Teach to avoid ASA/NSAIDS

As w/ all antidepressants, initially ↑ r/f suicide

Question 16

venlafaxine (Effexor)

Answer 16

Class: SNRI

MoA: Blocks reuptake of 5-HT & NE + weak block of DA reuptake, resulting in increased availability at synapses

Uses: MDD, GAD, social phobia, panic disorder

Admin: PO, should be taken w food.

Considerations: Inrc. r/f serotonin syndrome w/ other antidepressants. Contraindicated w/ MAOIs.

AEs: Nausea, HA, anorexia, nervousness, excessive sweating, somnolence, insomnia & sexual dysfunction most common

Dose-Dependent Wt. Loss & HTN

Hyponatremia in older pts on diuretics

If used late in pregnancy, can cause neonatal withdrawal syndrome

Withdrawal syndrome with abrupt DC- Avoid by slowly tapering over several weeks

As w/ all antidepressants, initially ↑’d r/f suicide

Question 17

imipramine/amitriptyline (Elavil)

Answer 17

Class: Tricyclic Antidepressant (TCA)

MoA: Blocks reuptake of 5-HT and NE resulting in increased availability at synapses

Also causes blockade of H1 and Alpha 1 and AcH receptors

Uses: Depression, BPD depressive symptoms, fibromyalgia, neuropathic pain, chronic insomnia, ADHD, panic disorder, OCD

Admin: PO at bedtime. Therapeutic effect in 1-3 weeks, mac effect in 1-2 months.

Considerations: Use w/ MAOIs = incr. risk for severe HTN.
Inhibition of Indirect-Acting Sympathomimetics (e.g. amphetamines, cocaine, tyramine)
Potentiation of Direct-Acting Sympathomimetics (e.g. epinephrine/NE, dopamine)
Potentiation of Anticholinergics
Potentiation of CNS Depressants

AEs: Sedation & orthostatic hypotension most common

Anticholinergic effects: dry mouth, constipation, tachycardia, blurred vision

Excessive sweating & hypomania

Dysrhythmias: obtain ECG before starting therapy

Seizures

As w/ all antidepressants, initially ↑’d r/f suicide

Question 18

Monoamine oxidase inhibitor (MAOI)

Answer 18

Class: MAOI

MoA: Blocks enzyme that breaks down NE, 5-HT and DA to inactive substances, resulting in increased availability at synapses

Uses: Depression when all else has failed

Admin: PO & transdermal.

Considerations: Interacts w/ Most Meds & Tyramine-rich Foods & Drinks (most fermented foods, cheeses, cured meats, figs, avocados, soy & ETOH)

AEs: CNS Stimulation (anxiety, insomnia, agitation & mania)—d/t more availability of NE
Orthostatic Hypotension
Hypertensive Crises from Dietary Tyramine… severe HA, tachycardia, n/v, confusion, sweating—medical emergency!

Question 19

bupropion (Wellbutrin)

Answer 19

Class: atypical antidepressant

MoA: Possibly blocks DA and/or NE reuptake resulting in increased availability at synapses

Does not affect serotonin, AcH or H1

Uses: MDD, SAD & smoking cessation

Off label: Neuropathic pain, BPD depressive symptoms & ADHD

Admin: PO.

Considerations: ↑ R/F Seizures w/ some SSRI’s: Zoloft, Prozac & Paxil

MAOI’s can ↑ r/f Wellbutrin toxicity

AEs: Agitation, HA, dry mouth, GI symptoms, dizziness, tremor, insomnia, blurred vision, tachycardia most common

Don’t use in pts w/psychotic disorders-can cause hallucinations & delusions

IMPROVES sexual function for many pts

In high doses → seizures

As w/ all antidepressants, initially ↑ r/f suicide

Question 20

lithium (Lithobid)

Answer 20

Class: heavy metal & in-organic ion found naturally in body

MoA: Possibly helps prevent neuronal atrophy and/or promote neuronal growth

Uses: BPD: drug of choice to control acute mania & provide long-term prevention against recurrence

Admin: PO in 3-4 doses daily d/t short half life.

Considerations: Lithium excretion is ↓’d when serum NA is Low: teach importance of avoiding NA loss & staying well hydrated

Very Low Therapeutic Index (narrow therapeutic range) makes Toxicity a Big Concern: keep Plasma Drug levels within Therapeutic Range of 0.4-1 Not to Exceed 1.5

Interactions:
* ↑ R/F Lithium Toxicity w/ Diuretics
* ↑ R/F Lithium Toxicity w/ NSAIDS x ASA
* Avoid Anticholinergics d/t → urinary hesitancy & ↑↑ discomfort

AEs: When Lithium Levels WNL:
GI Effects (nausea, diarrhea, abd bloating & anorexia)
Transient fatigue, muscle weakness HA, confusion & ↓ memory
Tremors
Polyuria & thirst- Avoid excessive activity that would result in fluid loss.
Renal Injury
Goiter & Hypothyroidism
Teratogenesis

when Lithium Levels > 1.5:
Persistent GI upset, course hand tremors, ECG changes, confusion, muscle hyperirritability, tinnitus, blurred vision, seizures, ↓ BP, coma → death

Question 21

valproate (Depakote)

Answer 21

Class: antiepeleptic/anticonvulsant

MoA: Unknown how it helps BPD. Possibly neuroprotective effects. Similar effectiveness as lithium with less AEs.

Uses: BPD: controls symptoms in acute manic episodes & prevents relapse of mania

Also used to treat migraines and seizures

Admin: PO & IV

Considerations: Incr. levels of dilantin and phenobarbital

AEs: GI upset (n/v/d & indigestion) & weight gain most common

Thrombocytopenia, pancreatitis, liver failure

Teratogenic: do not use in pregnancy

Question 22

lorazepam (Ativan)

Answer 22

Class: benzo - anxiolytic, hypnotic

MoA: Potentiates action of GABA (the main inhibitory NT in the brain). Endogenous GABA causes decreased neuron firing resulting in decreased anxiety, increased sleep and muscle relaxation

Uses: Anxiety, insomnia, seizures, preop sedation, ETOH withdrawal, panic disorder, GAD

Valium (diazepam) often prescribed for muscle spasms

Admin: PO, IM, IV (be v cautious w/ IV admin). High lipid solubility–crosses BBB.

Considerations:
Tolerance Develops to Some but Not All Effects

Physical Dependence is Possible but Low

Interactions: ↑ R/F CNS Depression W/ CNS Depressants

AEs: CNS depression
Anterograde amnesia if not desired
Sleep driving/walking/talking
Paradoxical effects
Respiratory depression

Low Abuse Potential- Schedule IV of the CSA

Avoid in pregnancy & Nursing Moms

Withdrawal Syndrome often Mild (Anxiety, insomnia, sweating & tremors), but more Severe w/ Prolonged Use at High Doses (Panic attacks, paranoia, delirium, HTN & convulsions). Best to taper slowly

Question 23

zolpidem (Ambien)

Answer 23

Class: benzo-like drug - hypnotic

MoA: Same as benzo

Uses: Short term tx of insomnia

Admin: PO & sublingual. Peaks in 2 hrs.

Considerations: Avoid taking w/ ETOH or other CNS depressants

AEs: Daytime drowsiness & dizziness most common

Sleep driving/talking/walking

Safety in pregnancy not established

Low abuse potential- Schedule IV of the CSA

Question 24

zaleplon (Sonata)

Answer 24

Class: Benzodiazepine-like drug–Hypnotic
MoA: Same as benzo
Uses: Same as Ambien
Admin: PO - peak in 1 hour

Considerations: Avoid taking w/ ETOH or other CNS depressants

↑ R/F Toxicity w/ Tagamet

AEs: HA, Nausea, drowsiness, dizziness, myalgia & abd pain most common

Sleep driving/talking/walking

Low abuse potential- Schedule IV of the CSA

Question 25

methylphenidate (Ritalin)

Answer 25

Class: CNS stimulant

MoA: Promotes NE & DA release & blocks reuptake, resulting in CNS stimulation. Chemically nearly identical to amphetamine

Uses: ADHD & narcolepsy

Admin: PO - IR/SR

Considerations: Cautious use w other CNS stimulants like caffeine, sudafed, adderall.

Decr. BP control w anti-HTN drugs

AEs: CNS Stimulant & CV Stimulant Effects:
Insomnia
Anorexia, weight loss
Restlessness
Tremors
Hyperactivity
Hypertension
Palpitations
Tachycardia
Emotional lability & psychosis

Physical & Psychological dependence- taper off slowly to avoid withdrawal syndrome

High abuse potential (Schedule II drug)