Murphy 17 N305 Psych And Pain Drugs

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Hi everyone! This will be the last note card set you'll have to study with.
It's on Psych and Pain medication.

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Lets go over some general information about these meds....

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Meds that ______ action potential make the neuron more ______ stimulated.

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Meds that decrease action potential make the neuron more easily stimulated

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Meds that _______ action potential make the neuron more _________ to stimulation

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Meds that increase action potential make the neuron more resistant to stimulation

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Acetylcholine (ACh)

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Involved in arousal, consciousness, memory**, nicotine dependence

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Many conventional antipsychotics interact with (i.e. block) muscarinic AChR...which causes...

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Anticholinergic Effects:
dry mouth
blurred vision
constipation
urinary retention
Delirium

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Dopamine

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DA release controls gross motor skills, sensations of euphoria, prolactin release, and psychotic symptoms
Elevated DA levels seen in pts with psychosis**

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Serotonin (5-HT)

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Responsible for many “housekeeping” functions
(body temperature, sleep-wake cycle, normative eating and mood states, memory, anxiety, panic)

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Decreased 5-HT levels seen in pts with __________

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Decreased 5-HT levels seen in pts with depression

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Norepinephrine (NE)
Decreased NE levels seen in pts with __________

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Norepinephrine (NE)
Decreased NE levels seen in pts with depression

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Glutamate
Major excitatory NT, involved in long-term potentiation (______)

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Glutamate
Major excitatory NT, involved in long-term potentiation (memory)

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PSYCHOSIS

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Management:
Maintain highest level of functioning!

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There are two sorts of meds.

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Different meds effective at reducing different symptoms

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Conventional antipsychotics ~ more effective w/ __________ ________

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Conventional antipsychotics ~ more effective w/ positive symptoms

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Atypical antipsychotics ~ more effective w/ ________ ________

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Atypical antipsychotics ~ more effective w/ negative symptoms

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Conventional Antipsychotics
‘First Generation’ Antipsychotics
Prototype is:

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Chlorpromazine [Thorazine]

Haloperidol [Haldol]

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Chlorpromazine [Thorazine]
Low or high potency?

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Chlorpromazine [Thorazine]
Low potency
2st Chlorpromazine [Thorazine]
Low or high potency?developed antipsychotic (1952)

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Haloperidol [Haldol]
Low or high potency?

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Haloperidol [Haldol]
High Potency

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Conventional Antipsychotics ‘First Generation’ Antipsychotics
Mechanism of action

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Block receptors of dopamine, acetylcholine, histamine, norepinephrine (especially D2 receptors)
Therapeutic effects: reduces or eliminates positive symptoms of psychosis

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Chlorpromazine [Thorazine] and Haloperidol [Haldol]
MAJOR SIDE EFFECTS (a total of 5...)

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~Extrapyramidal side effects: dystonia, pseudoparkinsonism, akathasia, tardive dyskinesia
~High potency conventional antipsychotics display the greatest risk for EPS
~Anticholinergic effects
~Orthostatic hypotension (low potency has greater risk)
~Neuroleptic malignant syndrome

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Atypical Antipsychotic Agents
‘Second Generation Antipsychotics’
Prototype is...

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Clozapine (Clozaril) (1st in class)

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Most commonly prescribed atypicals* (name 3)

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Risperidon (Risperdal)
Olanzapine (Zyprexa)
Quetiapine (Seroquel)

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Clozapine (Clozaril)
Mechanism of Action

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Blocks dopamine (D4) and serotonin receptors

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Versus conventional antipsychotics

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Greater efficacy for negative & cognitive symptoms
Fewer EPS/tardive dyskinesia

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ANTIDEPRESSANTS

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Selective Serotonin Reuptake Inhibitors
Tricyclic Antidepressants
MAO Inhibitors

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Depression caused by decrease in NTs:

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Norepinephrine (NE) and serotonin (5-HT)

Using these drugs will raise the levels of these NT's

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Selective Serotonin Reuptake Inhibitors (SSRIs)

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First-line therapy for depression

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Prototype:
Fluoxetine (Prozac)*

What are other ones that are perscribed?

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Citalopram (Celexa)*
Paroxetine (Paxil)*
Sertaline (Zoloft)*

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Mechanism of Action

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Inhibit presynaptic reuptake of 5-HT

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Tricyclic Antidepressants

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2nd line therapy against depression

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Tricyclic Antidepressants
Prototype is...

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Imipramine (Tofranil)

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Imipramine (Tofranil)
Mechanism of Action

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Blocks reuptake of norepinephrine (NE) and also 5-HT into presynaptic nerve

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Imipramine (Tofranil)
Significant Adverse effects

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Anticholinergic effects
Orthostatic hypotension
Cardiac toxicity
Sedation
Toxicity may be lethal...

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Administering safely...

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Administer at bedtime
Pts should avoid alcohol and tobacco

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Monoamine Oxidase Inhibitors (MAOIs)

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Second or third choice for depression

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MAOI's
Prototype...

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Phenelzine (Nardil)

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MAOIs
Mechanism of action

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Irreversibly inhibits presynaptic MAO
**Prevents monoamine degradation

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MAOIs
Uses

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Atypical depression or TCA/SSRI-resistant
hypersomnia, anxiety, and no neg symptoms
Also for other psych illnesses (e.g. bulimia, OCD, panic attacks)

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MAOI's
Phenelzine (Nardil)
Significant Adverse effects

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Orthostatic hypotension
Hypertensive crisis (from **tyramine foods)
Multiple drug-drug interactions
Multiple drug-food interactions

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MAOI's
Phenelzine (Nardil)
Contraindications

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Cerebrovascular disease, cardiovascular disease, >65, bipolar, diabetes, pregnancy

Dietary restrictions
Necessary to prevent hypertensive crisis

Avoid tyramine-rich foods
Yeast extracts, most cheeses
Aged fish or meat, Figs, bananas
Wine

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Atypical Antidepressants
Bupropion (Wellbutrin)*

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Bupropion (Wellbutrin)*
Inhibits DA and NE reuptake (minimal 5-HT)
Side effects include agitation, headache, seizures, anticholinergic effects

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Atypical Antidepressants
Venlafaxine (Effexor)*

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Venlafaxine (Effexor)*
Serotonin/NE reuptake inhibitor
Lacks TCA anticholinergic SEs
Major SE = GI upset + SSRIs

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Atypical Antidepressants
Trazodone (Desyrel)*

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Trazodone (Desyrel)*
SSRI also blocks 5-HT receptors
Sedative, used for insomnia
Adjunct to SSRIs (counter insomnia)

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Bipolar Disorder

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Lithium
Mood Stabilizing Anticonvulsants

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Acute therapy: manic episode

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Acute therapy: manic episode
Lithium (most effective)
Valproate
Second-generation (atypical) antipsychotics

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Acute therapy: depressive phase

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Acute therapy: depressive phase
Valproate, divalproex (Depakote)*
Mood stabilizer alone +/- antidepressant

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Long-term maintenance

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Lithium, one or more mood stabilizers, other drugs as needed acutely

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Lithium
Drug of choice for _____

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Drug of choice for mania

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Lithium
Therapeutic range

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Narrow therapeutic index
0.8 to ~1.4 mEq/L [serum] acute treatment
0.6-0.8 mEq/L [serum] maintenance level

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Lithium Toxicity

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Lithium serum level—greater than 1.5 mEq/L

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Adverse effects
Most significant is...

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Renal toxicity
SEs often managed with other meds

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Mood-Stabilizing Anticonvulsants

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Valproic acid and valproate, divalproex [Depakote]*
1st line therapy for rapid-cycling bipolar disorders

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Valproic acid and valproate, divalproex [Depakote]*
Mechanism of Action

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Mechanism of Action
Presumably by increasing GABA (inhibitory) neurotransmission

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Valproic acid and valproate
Adverse effects

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Adverse effects
Wider therapeutic range than lithium, less incidence of OD
SEs include sedation, GI upset, tremor (treated with beta-blocker), hepatotoxicity (in young)

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ANXIETY DISORDERS
5 types of anxiety disorders

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Generalized anxiety disorder
Excessive worry, poor concentration, insomnia, >6 mo

Panic disorder
Intense fear, persistent worry, impending doom

Obsessive-compulsive disorder (OCD)
Uncontrollable obsessive or intrusive repetitive thoughts; ritualistic behaviors

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ANXIETY DISORDERS
5 types of anxiety disorders cont.

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Posttraumatic stress disorder (PTSD)
Re-experiencing a traumatic event; avoidance of remindful stimuli
Generalized social phobia (social anxiety disorder)
Disproportionate anxiety/fear of scrutiny or humiliation

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ANXIETY DISORDERS

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antidepressants as first-line therapy
Venlafaxine (Effexor)*
SSRIs e.g. paroxetine (Paxil)
TCAs e.g. imipramine (Tofranil) w/ 5-HT action

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Versus benzodiazepines

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Benefits: **lower abuse potential
Disadvantages: less effective w/ physical/somatic symptoms

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Benzodiazepines
Prototype is...

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diazepam (Valium)

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Mechanism of action

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Potentiate the actions of GABA (major inhibitory NT)

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Benzodiazepines
Uses

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anxiety, insomnia, seizure disorders, muscle spasms, panic disorder, alcohol withdrawal

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Benzodiazepines
Sig. Adverse effects

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High potential for abuse
Paradoxic effects
Category X
Significant DDIs w/ CNS depressants

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OPIOID ANALGESIC

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Morphine
Hyrdocodone
Codeine
Naloxone

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Opioid (poppies) analgesics

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Drugs structurally similar to morphine
Mimic actions of endogenous opioid-like molecules (ex:endorphins)

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Prototype of strong opioid analgesics

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Morphine

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Morphine
MOA:

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Binds to mu opioid receptor as agonist results in analgesia, respiratory depression, euphoria (joy), mental clouding, and sedation

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Used for relief of moderate/severe pain
Adverse effects include:

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Respiratory depression

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Opioid Overdose

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Opioid Overdose
Classic triad:
Coma
Respiratory depression
Pinpoint pupils

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Treatment

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Ventilatory support
Opioid antagonist
Naloxone [Narcan]

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Cyclooxygenase Inhibitors: Nonsteroidal Anti Inflammatory Drugs and Acetaminophen

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Aspirin
Ibuprofen
2nd Generation NSAIDs
Acetominophen ~ (Tylenol)

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Classification of Cyclooxygenase (COX) Inhibitors

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NSAIDs are Drugs with anti-inflammatory properties

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Three Major Uses
Suppress inflammation
Relieve pain
Reduce fever

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Three Major Adverse Effects
Gastric ulceration
Bleeding
Renal impairment

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Mechanism of Action
Inhibiting COX enzymes (thus inhibiting prostaglandin synthesis)

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These are the last drugs you'll be learning! Ready?!

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Cyclooxygenase (COX) Inhibitors
First generation
Inhibit COX-1 and COX-2 enzymes
Prototype is...

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Aspirin

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Aspirin
Therapeutic uses

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Relieves mild-to-moderate pain
Analgesic, antipyretic (prevent fever), anti-inflammatory
1st line therapy for rheumatoid arthritis
Dysmenorrhea – painful menstruation

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Aspirin
Mechanisms of action

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Irreversibly inhibits COX enzymes
COX-2 inhibition = suppresses inflammation, pain, and fever
COX-1 inhibition = protects against MI
Suppression of platelet aggregation
Inhibition of platelet COX = protects against MI

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Aspirin
Contraindications

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Pregnancy (Category D)
Caution in children (Reye’s syndrome)

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Second Generation COX Inhibitors
Prototype is....

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Celecoxib [Celebrex]

Specifically inhibit COX-2 (suppresses inflammation)

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Celecoxib [Celebrex]
what we thought

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fewer adverse effects than first generation COX inhibitors
but
potential for increased risk of cardiovascular (CV) events, gastrointestinal (GI) bleeding

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Celecoxib [Celebrex]
Adverse effects

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Dyspepsia, Abdominal pain, Renal toxicity, Sulfonamide allergy

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Celecoxib [Celebrex]
Therapeutic uses

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Osteoarthritis, Rheumatoid arthritis, Acute pain, Dysmenorrhea, Familial adenomatous polyposis

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Acetaminophen
Also known as....you know it!

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[Tylenol]

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Acetaminophen
Therapeutic Uses

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Analgesic, antipyretic (not useful as anti-inflammatory*)
Permissible in children and during pregnancy (Category B)

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Acetaminophen
Action

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Inhibits prostaglandin synthesis only in *CNS

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Acetaminophen
Adverse effects

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**Hepatotoxicity (Overdose—hepatic necrosis)
**Alcohol consumption increases risk for liver injury
Warfarin may increase bleeding risk