Psych Pharm Flashcards
What is the preferred drug for alcohol withdrawal?
Benzodiazepines
What is the preferred treatment for anxiety?
SSRIs, SNRIs, buspirone
What is the preferred treatment for ADHD?
Methylphenidate
Amphetamines
Atomoxetine (non-stimulant: NE selective reuptake inhibitor)
What is the preferred drug for bipolar disorder?
Lithium
Valproate
Carbamazepine
Atypical antipsychotic
What is the preferred drug for bulimia?
SSRIs
What is the preferred drug for depression?
SSRIs, SNRIs, TCAs, buspirone, mirtazapine
What is the preferred drug for obsessive compulsive disorder?
SSRIs, clomipramine
What is the preferred drug for panic disorder?
SSRIs, venlafaxine, benzodiazepines
What is the preferred drug for PTSD?
SSRIs
What is the preferred drug for schizophrenia?
Antipsychotic
What is the preferred drug for social phobias?
SSRIs
What is the preferred drug for Tourette’s?
Antipsychotics - haloperidol, risperidone
What are the CNS stimulants?
Methylphenidate, dextroamphetamine, meth
What is the MOA of CNS stimulants?
Increase catecholamines at the synaptic cleft, especially NE and DA
What is the clinical use of CNS stimulants?
ADHD, narcolepsy, appetite control
What are the antipsychotics?
Haloperidol, trifluoperazine, fluphenazine, thioridazine, chlorpromazine
What is the MOA of antipsychotic?
Block D2 receptors (inc. camp)
What are the high potency antipsychotics?
Trifluoperazine
Fluphenazine
Haloperidol
These have extra pyramidal effects
What is the clinical use of antipsychotics?
Schizophrenia
Psychosis
Acute mania
Tourette’s
What are the low potency antipsychotics?
Chlorpromazine
Thioridazine
These cause anticholinergic, antihistamine and alpha 1 blockade effects
What is the toxicity of antipsychotics?
Slow to be removed from body because lipid soluble.
Extrapyramidal effects - dyskinesia, dystopia, Parkinsonian effects
Endocrine: hyperprolactinemia, galactorrhea
Antimuscarinic: dry mouth, constipation
AntiHistamine receptors: sedation
Neuroepileptic malignant syndrome
Tardive dyskinesia
Alpha 1 blockade: hypotension, vasodilation – reflex tachycardia
What is neuroepileptic malignant syndrome?
Rigidity, myoglobinuria, autonomic instability, hyperprexia
What is the treatment for neuroepileptic malignant syndrome?
Dantrolene
d2 agonist - bromocriptine
What is tardive dyskinesia?
Stereotypic oral-facial movements as a result of long term antipsychotic use
Often irreversible
What is the acronym for remembering what happens with NMS?
Fever Encephalopathy Vitals unstable Elevated enzymes Rigidity of muscles
What are the atypical antipsychotics?
Olanzapine Clozapine Quetiapine Risperidone Aripiprazole Ziprasidone
What is the MOA of atypical antipsychotics?
Varied effects on 5-HT, dopamine, alpha, and histamine receptors
What is the clinical use of atypical antipsychotics?
Schizophrenia Bipolar OCD Anxiety Depression Mania Tourette's
What is the toxicity of olanzapine?
Weight gain
What is the toxicity of clozapine?
Weight gain
Agranulocytosis
Seizure
What is the toxicity of ziprasidone?
Prolonged QT interval
What is the MOA of lithium?
Inhibitor of phosphoinositol cascade?
MOA unclear
What is the clinical use of lithium?
Bipolar disorder
Blocks relapse and acute mania events and SIADH
What is the toxicity of lithium?
LMNOP: Movement (tremor). Nephrogenic diabetes insipidus HypOthyroidism Pregnancy problems (teratogenicity)
Where is the lithium excreted?
In the kidney
Mostly reabsorbed at the PCT
What is the MOA of buspirone?
Stimulates 5HT1A receptors
What is the clinical use of buspirone?
Generalized anxiety disorder
1-2 weeks to take effect
Does not interact with alcohol
What is the advantage of buspirone?
Does not cause Sedation, addiction, tolerance
What are the SSRIs?
Fluoxetine, paroxetine, sertraline, citalopram
What is the clinical use of SSRIs?
Depression Bulimia Anxiety disorder Panic disorder OCD Social phobias PTSD
What is the toxicity of SSRIs?
GI
Sexual dysfunction
Serotonin syndrome
What is serotonin syndrome?
Hyperthermia, confusion, myoclonus, CV collapse, flushing, diarrhea, seizures
What it the tx for serotonin syndrome?
Cyproheptadine - 5HT2 receptor antagonist
What are the SNRIs?
Venlafaxine
Duloxetine
What is the MOA of SNRIs?
Inhibit serotonin and NE uptake
What is the clinical use of SNRIs?
Depression
What is the clinical use of venlafaxine?
Generalized anxiety and panic disorder
What is the clinical use of duloxetine?
Diabetic peripheral neuropathy
Has greater effect of NE
What is the toxicity of SNRIs?
elevated BP
Sedation
Nausea
Stimulant effects
What are the TCAs?
Amitryptyline, nortriptyline, imipramine, desipramine, doxepin, clomipramine, amoxapine
What is the MOA of TCAs?
Block reuptake of NE and serotonin
What is the clinical use of TCAs?
Major depression
Bed wetting (imipramine)
OCD (clomipramine)
Fibromyalgia
What is the toxicity of TCAs?
Sedation Alpha 1 blockade effects Anticholinergic effects Convulsions Coma Cardio toxicity Respiratory depression Hyperprexia In elderly: hallucinations, confusion
What is the treatment for cardio toxicity from TCA?
NaHCO3
What are the MAOi’s?
Tranylcypromine
Phenelzine
Isocarboxazid
Selegiline
What is the MOA of MAOi’s?
Nonselective MAO inhibition
Increase amine NTs (NE, serotonin, dopamine)
What is the clinical use of MAOi’s?
Atypical depression
Anxiety
Hypochondriasis
What is the toxicity of MAOi’s?
Hypertensive crisis
CNS stimulation
What is contraindicated with the use of MAOi’s?
SSRIS TCAS St. John's Wort Meperidine Dextromethorphan
What are the atypical antidepressants?
Bupropion
Mirtazapine
Maprotiline
Trazodone
What is trazadone used for?
Insomnia
What is the MOA of trazadone?
Primarily inhibits serotonin reuptake
What is the toxicity of trazadone?
Sedation
Nausea
Priapism
Postural hypotension
What is the MOA of maprotiline?
Blocks NE reuptake
What is the toxicity of maprotiline?
Sedation
Ortho static hypotension
What is the MOA of mirtazapine?
Alpha 2 antagonist, potent 5-HT2/3 receptor antagonist
What is the toxicity of mirtazapine?
Sedation
Increased appetite
Weight gain
Dry mouth
What is the MOA of bupropion?
Increases NE and DA
What is the toxicity of bupropion?
Tachycardia
Insomnia
Headache
Seizure
What is bupropion used for?
Smokin cessation
What is the advantage of bupropion?
No sexual side effects
What is the MOA of memantine?
Uncompetitive NMDA receptor antagonist
Competes with Mg2+ after calcium influx thereby preventing over excitation
What is the toxicity of memantine?
Dizziness, confusion, hallucinations, constipation, H/A
What is the treatment of choice for Alzheimer’s?
Anti-acetylcholinesterases
What are the anti-acetylcholinesterases?
Donezapil
Galantamine
Rivastigmine
What is the disadvantage to using rivastigmine?
It also inhibits butyrylcholinesterase thereby inhibiting the breakdown of succinylcholine and giving it longer duration of action. Patients on this drug can’t go under surgery.
What are the side effects of anti-AchEs?
Diarrhea, incontinence, N/V, dizziness, insomnia, miosis
What anti-AchE treats all forms of Alzheimer’s?
Donezapil
What is the toxicity of tacrine?
Liver toxicity
When are galantamine and rivastigmine used?
In mild to moderate Alzheimer’s
What is the tx for Lewy Body disease?
Low dose anti-AchE and Parkinson drugs
What do all anti-psychotics do?
Block dopamine receptors
Where are the dopamine tracts in the brain?
Ventral tegmental area –> nucleus accumbens, prefrontal cortex
Substantia nigra –> striatum
Hypothalamus –> pituitary
Medulla
What are the effects of dopamine?
Euphoria, psychosis, reinforcement
Voluntary motor activity
Prolactinemia
Eating, hiccups, vom
Why do schizophrenics get negative symptoms?
From decrease DA in the nucleus accumbens and prefrontal cortex
What accounts for the positive sx in schizophrenia?
Excess dopamine in the Mesolimbic system
What drugs can cause psychotic episodes in normal individuals?
Dopaminergic agonists:
Amphetamines
PCP
Cocaine
What do the typical antipsychotics do?
Block DA receptors, especially D2
These are usually messy and also block histamine, muscarinic and cholinergic receptors –> lots of side effects
What are the general effects of antipsychotics?
Control bizarre behavior and calm agitation, impulsivity, aggression
Improve the core thought disorders
Tx: Tourette’s, hiccups, and nausea
What are the typical psychotics?
Phenothiazines: chlorpromazine, prochlorperazine, promethazine
Butyrophenomes: haloperidol
What is the prototype typical antipsychotic?
Chlorpromazine
What are the side effects of chlorpromazine?
Urinary retention, dry mouth - from anti muscarinic effects
Ortho static hypotension - from alpha blockade
What is the risk of taking haloperidol?
Cleaner D2 antagonist so it causes more extra pyramidal side effects: dystonias, Parkinsonism, neuroleptic malignant syndrome
What is the tx for the extrapyramidal side effects of haloperidol?
Reduce the dose of the antipsychotic
Give anticholinergics
What is the tx of neuroleptic malignant syndrome?
Stop antipsych and anticholinergics!
Give antipyretic
Give DA agonist
What are the general side effects of antipsychotics?
Dysphoria, hyperprolactinemia: galactorrhea, gynecomastia, menstrual disturbances Impotence Sexual dysfunction Poikilothermia Weight gain Hypotension
What is the major long term side effect of antipsychotics?
Tardive dyskinesia
What is the tx for tardive dyskinesia?
Decrease the dose of anti-psychotics –> will get worse initially but then it will be ok
What are the atypical antipsychotics?
Olanzapine Clozapine Quetiapine Risperidone Aripiprazole
What is the advantage of atypical antipsychotics?
Greater efficacy for negative sx
Less likely to cause tardive dyskinesia
What are the side effects of olanzapine?
Weight gain
Somnolence
Type II diabetes
What is the MOA of atypical antipsychotics?
Block DA receptors and 5HT2 receptors
What is the FDA warning against atypical antipsychotics?
They cause hyperglycemia, type II diabetes
What atypical antipsychotic is more efficacious than other antipsychotics?
Clozapine
What are the advantages to clozapine?
Better efficacy
No extrapyramidal side effects
What is the major side effect of clozapine?
Agranulocytosis
What are the other side effects of clozapine?
Strong Sedation
Anticholinergic effects: urinary retention
Hypotension
What is the most prescribed atypical antipsychotic?
Quetiapine
What other disorder is quetiapine used for?
Bipolar disorder
Why do you give quetiapine at night?
Because it is slightly more sedative
What is the disadvantage of risperidone?
It has a higher affinity for D2 receptors so it is more likely to cause tardive dyskinesia and extrapyramidal sx
What are the side effects of risperidone?
Anxiety Somnolence Extrapyramidal sx Dizziness Type II diabetes
What is the MOA of aripiprazole?
Partial DA agonist and partial 5HT1 agonist
5HT2 antagonist.
What is the aripiprazole?
Used for depression and schizophrenia
What are the advantages of aripiprazole?
Causes less weight gain than olanzapine
No incidence of Type II diabetes
And can be used for schizophrenia and depression
How can aripiprazole be used for schizophrenia when it’s a dopamine agonist?
As a weak partial agonist it inhibits the full agonist
What drugs may cause depression by lowering bio genic amines?
Reserpine Propranolol Methyldopa and clonidine Amphetamines OCs Drugs of abuse
What is the MOA of TCAs?
Block mono amine reuptake with more effect on 5HT
Down regulate norepinephrine and/or 5HT receptor
What are the side effects of TCAs?
Anti muscarinic: blurred vision, dry mouth, constipation, confusion Weight gain Sexual disturbance Tremor Insomnia Ortho static hypotension Arrhythmias
What is the danger of TCAs?
Patients OD easily
What other conditions are TCAs used for?
Chronic pain and panic disorder
What’s the drug of choice for chronic pain?
Amitryptiline
Which TCA has the most sedative and strongest anti muscarinic side effects?
Amitryptiline
What are the TCAs?
All the -pramines, amitryptiline, nortriptyline, doxepin, protripyline
What are the second generation antidepressants?
Venlafaxine Bupropion Trazadone Duloxetine Mirtazapine
What is the MOA of venlafaxine?
SSNRI a selective serotonin and NE reuptake inhibitor
More potent at 5ht
What are the side effects of venlafaxine?
HTN
Tachycardia
What are th disadvantages of venlafaxine compared to SSRIs?
More intense withdrawal
Greater toxicity in OD
What second generation is used for physical pain symptoms of depression and diabetic neuropathic pain?
Duloxetine
What is the MOA of bupropion?
Occupies 25% of DA uptake sites
What is the advantage of bupropion?
Causes little to no sexual dysfunction
What is bupropion used for?
Smoking cessation
What is the contraindication to using bupropion?
Seizure disorder
What is the MOA of trazadone?
5HT-2 antagonist
Weak selective 5HT reuptake inhibitor
What are the side effects of trazodone.?
Priapism
Sedation
What is the advantage to trazodone?
Less toxic in OD
What is the MOA of mirtazapine?
Selective stimulation of 5Ht1 receptors due to blockade of 5HT2/3
Increase 5HT cell firing due to increase in NE and blockade of alpha2 adrenergic receptors.
What are the side effects of mirtazapine?
Significant sedation
Increased appetite
Weight gain
Why are SSRIs the first choice for depression?
Much safer in OD
What is another advantage of SSRIs?
Little action at other receptors so little side effects
Longer half life
What is the most common side effect of SSRIs?
Sexual dysfunction
What is discontinuation syndrome?
Flu like syndrome from stopping SSRIs abruptly
Most pronounced with paroxetine
Sx: agitation, anxiety, anorexia, insomnia, sweating, tremor, vom
Why don’t you ever give an SSRIS with an MAOi?
Can cause serotonin syndrome
What are the sx of serotonin syndrome?
Altered mental status, fever, agitation, sweating, myoclonus, tremor, hyperprexia, ataxia, GI
What are the SSRIs?
Fluoxetine Sertraline Paroxetine Citalopram Fluvoxamine
Which SSRI has the longest half life?
Fluoxetine
What are the side effects of fluoxetine?
Nausea Insomnia Weight loss Agitation Sexual dysfunction
Which SSRIs have the potential for drug interactions because they inhibit CYP2D6?
Fluoxetine
Paroxetine
Which SSRI is most likely to cause a discontinuation syndrome?
Paroxetine
Which SSRI is most likely to cause GI upset as a side effect?
Sertraline
Which SSRI causes the most sexual dysfunction?
Paroxetine
Which SSRI is less likely to produce mania?
Citalopram
What disorder is fluvoxamine usually prescribed for?
Obsessive compulsive disorder
Which SSRI is the most selective?
Citalopram
What is the mechanism of action of MAOi’s?
Block the deamination of tyramine which results in increased norepinephrine release and therefore a deadly increase in bp
What foods contain tyramine?
Aged cheese Wine Beer Pickled herring Liver Yeast extract Fava beans
What are the MAOi’s?
Phenelzine
Tranylcypromine
Which MAOi is irreversible?
Phenelzine
What are antipsychotics useful for in the treatment of bipolar disorder?
Acute mania
Not good for depressive episodes
Use for rapid correction of a manic episode then add a mood stabilizer
What is the tx for lithium OD?
Dialysis
What are the side effects of lithium?
Most common = tremor Decreased thyroid fxn Mild cognitive impairment Acne eruptions Leukocytosis Polydipsia/polyuria Chronic interstitial nephritis Minimal change glomerulopathy GI Edema Weight gain
What condition is a contraindication to using lithium?
Sick sinus syndrome because lithium suppresses the sinus node
Why do patients get polydipsia/polyuria on lithium?
Lithium makes the collecting tubule unresponsive to ADH
What is the MOA of lithium?
Substitutes for Na in generating action potentials and in the Na/K pump (causes seizures)
Also decreased PIP2 therefore decreasing the responsiveness to synaptic transmission (decreased calcium influx)
Is lithium contraindicated in pregnancy?
N
What is th leading cause of death in bipolar disorder if left untreated?
Suicide
How long does it take before lithium effects are seen?
2-3 weeks
What can cause the concentration of lithium to go up in the body?
NSAIDs
Diuretics
What are the mood stabilizing drugs?
Lithium Valproate Lamotrigine Carbamazepine Oxycarbazepine
What is the advantage to using valproate over lithium?
Faster onset (4-5 days)
What are the side effects of valproate?
GI upset Hepatotoxicity Neural tube defects Alopecia Increases appetite and weight gain
What is the MOA of carbamazepine?
Blocking of voltage gated sodium channels
What are the side effects of carbamazepine?
Agranulocytosis -stop if you see a rash Diplopia Ataxia GI upset Sedation Weight gain
What is lamotrigine not effective for?
Acute mania
What is the MOA of lamotrigine?
Blocks sodium and calcium channels
What is the side effect of lamotrigine?
Steven-Johnson syndrome
Raise levels very slowly
When are atypical antipsychotics or benzodiazepines used?
During an acute manic episode
What are the first choice drugs for treating anxiety?
SSRI
Venlafaxine
TCAs
Why are these the first drugs of choice for anxiety?
Because they have no potential for abuse/dependence
What is the timing of onset for the first choice drugs for anxiety?
Slow - 2-4 weeks which is considered a negative for the patient
How many subunits make up the GABA receptor complex?
5
Which unit binds GABA?
Alpha
What is the binding site for BZD?
Alpha/beta
What subunit must be present for BZDs to modulate GABA?
Gamma
What happens when GABA binds the receptor complex?
The channel opens up to chloride ions causing the cell to become more negative inside making it harder to depolarize - decreased neural firing
What is the endpoint of the using the GABA receptor?
Coma and death
What do inverse agonists of BZDs do?
They decrease chloride conductance by inhibiting GABA in a non-competitive way
What are the overall effects of BZDs?
Anxiolytix Hypnotic Anticonvulsant Amnestic Produce confusion DO NOT produce coma
What is the major problem with BZDs?
Dependency
Don’t use more than 3 days at a time
Shorter half-lives have worse withdrawal effects
Longer half-lives have less severe withdrawal effects but they effects are longer
How can death ensue with BZDs and anoth CNS depressant?
Respiratory depression
What are the uses of diazepam?
Anxiolytic Hypnotic Muscle relaxant Amnestic Pre-anesthetic Terminates status epilepticus Block convulsions of withdrawal from BZD or EtOH
What is the half-life of diazepam?
50+ hours
What is the half life of alprazolam?
12-15 hours
More rapid oral absorption
What are the advantages to alprazolam?
Shorter half life
Faster absorption
Less sedative
What is the BZD of choice for anxiety?
Alprazolam
What is a potential side effect of alprazolam ?
Early morning wakening
Which BZD has a longer duration of action then diazepam?
Lorazepam
What is oxazepam used for?
Anxiolytic
Sleep induction
Who do you give oxazepam to?
The elderly because of more reliable pharmacokinetics
What are the properties of midolazam?
Very short acting
Water soluble
What is midolazam used for?
Pre-op anesthesia
Anxiolytics and muscle relaxant
Amnestic
What is flumazenil?
It is an antagonist of BZD receptor.
No action without BZD in the system
What is flumazenil used for?
Post anesthesia
BZD overdose
What is the thing you should watch out for with flumazenil?
Precipitated withdrawal from the BZD – seizures!
What do inverse agonist?
Anxiety then seizures
What drugs can cause lethality if combined with a BZD?
EtOH Opioids Antipsychotics TCAs Antihistamines
What is the action of cimetidine?
Inhibits liver oxidase so prolonged the action of BZDs.
What BZDs would you prescribe for someone on cimetidine?
Alprazolam
Lorazepam
Oxazepam
Because of shorter duration of action
What are the signs of BZD withdrawal?
Tremors
Seizures
What are the sx of withdrawal sx?
Anxiety
Insomnia
Nausea
Malaise
What is the MOA of 5-HT1a agonists?
Increase K conductance via same channels as GABAb receptors
What is the MOA of buspirone?
5-HT1a agonist
What is the advantage to using buspirone over a BZD?
No sedation
No motor impairment
What is the use of buspirone?
Anxiety
What are the disadvantages to buspirone?
Takes 3-6 weeks to work
Can cause anxiety
What are the side effects of buspirone?
Dizziness, nausea, vomiting
No dependence or tolerance
No cross tolerance with BZDs
Does not alleviate BZD or EtOH withdrawal
What are the drug interactions of buspirone?
Increase bp with MAOi
Better effects against obsessive-compulsive behavior with SSRI
What are the signs of TCA toxicity?
QRS prolongation Anticholinergic effects Agitation Seizures Coma
Why should you wait 2 weeks to switch a patient from an MAOi to an SSRI?
Because it takes up to 2 weeks to resynthesize MAO and without normal levels, catecholamines will not be degraded. Add an SSRI and we have even more catecholamines in the synapse –> serotonin syndrome
What should people on levodopa avoid?
Vitamin B6 because it catalyzes peripheral metabolism of levidopa and decreases its effectiveness
What is infused with IV lorazepam to reduce recurrence of seizures?
Phenytoin
What is the MOA of phenytoin?
Increase sodium channel inactivation in cortical neurons
What is infused if status epilepticus does not stop with lorazepam?
Phenobarbital
Why is methadone effective in treating heroin addiction?
It is a mu agonist with a long half life so it allows for continuous suppression of withdrawal sx
What are the high potency antipsychotics?
Haloperidol
Fluphenazine
Pimozide
What are the high potency antipsychotics more likely to cause?
Extrapyramidal sx - increased skeletal muscle tone
What are the higher potency antipsychotics less likely to cause?
Anticholinergic and antihistamine effects
What are the lower potency typical antipsychotics?
Chlorpromazine and thioridazine
What antipsychotic causes retinitis pigmentosa?
Thioridazine - typical, low potency
What is chlorpromazine associated with?
Corneal deposits
What is ziprasidone associated with?
Prolonged QT interval
What is the MOA of varenicline?
Partial agonist at nicotine receptor - competes with nicotine for binding.
Causes limited downstream dopamine release resulting in less stimulation of the reward pathway.
Decreases withdrawal sx, reduces craving and reduces pleasure from other tobacco products
What is the MOA of reserpine?
Inhibits dopamine entry into synaptic vesicles - reduces heart rate and bp
What are beta blockers used for?
Performance anxiety
Use where sympathetic outflow is high and serves no purpose
Treat alcoholism in someone that needs a deterrent?
Disulfiram
causes aldehyde syndrome = hangover
What do you treat the initial phases of DTs with?
benzodiazepines
*just supportive care if already enter true DT’s
What is the treatment for SSRI toxicity?
Cyproheptadine
5-HT2 receptor antagonist
What are the common SNRI’s?
Venlafaxine & Duloxetine
MOA of SNRI’S?
Inhibits serotonin and NE reuptake
Use of Venlafaxine?
Depression
Generalized anxiety and panic disorder
Use of Duloxetine?
Depression
Diabetic peripheral neuropathy
How do you treat TCA toxicity?
NaHCO3
Treats cardiotoxicity/ arrhythmia
Use of Imipramine?
Sleep enuresis
DOC for sleep enuresis?
DDAVP (desmopressin)
2DOC- Imipramine (TCA)
What to you treat night terrors and sleep walking with?
Benzodiazepines
What do you treat narcolepsy with?
Aronodafinil & Modafinil
Amphetamines
(day-time stimulants)
and night time Sodium oxybate (GHB)
What do you treat restless leg syndrome with?
Dopamine agonists (Ropinirole & Gabapentin)
What do you treat REM-behavioral disorder with?
Clonazepam
What do you treat acute insomnia with?
BZD’s- short term
What do you treat chronic insomnia with?
CBT w/ pyschophysiologic treatment
sleep hygiene
What drug may cause an exaggerated response to ADH?
Carbamazepine
What does an exaggerated response to ADH cause?
Hyponatremia because of increased volume - dilution
What is primidone?
An anti epileptic drug that is metabolized to phenobarbital