Test 1 Flashcards
Deprescribing Anti-Depressives
"Titration" Helps Avoid Withdrawal like Symptoms -Flu like Symptoms -Insomnia -Nausea -Poor Balance -Sensory Disturbance -Hyperarousal
Bupropion
Treats Nicotine Withdrawal
NDRI
Imipramine
Treats Enuresis
Duloxetine
Treats: Diabetic Neuropathy, Fibromyalgia, MSK pain, stress incontinence
-SNRI
What is an anti-depressant that treats stress incontinence?
Duloxetine
Fluvoxamine
SSRI only for OCD
Amoxapine
SSNRI+ Dopamine Antagonis
SARAs (Sertonin Adrenergic Receptor Antagonist)
Nefazodone
Trazodone
Mirtazapine
MAOI
Isoscarboxazid
Phenelzine
Segeline
Trancyclopromine
NDRI (Nadi/DA reuptake inhibitor)
Bupropion
enhanced pre-synaptic release of NE and DA via VMAT
selectively inhibits pre-synaptic reuptake of NE via NET and DA via DAT
SSRIs
Citalopram Escitalopram Sertiline Fluoxetine Paroxetine Valazodone Vortioxetine
less impact on histamine/ muscarinic/ adrinergic receptors
SNRIs
TCAs Desvenlafaxine Duloxtine Venalfaxine Lenomilnacipran
SSRI MOA
inhibit presynaptic re-uptake of serotonin via SERT
SSRI Side effects
sexual dysfunction CNS sedation/insomnia withdrawal rxns QT Prolongation Hyponatremia (esp in old people) Sertonin Syndrome Suicidality esp in young adults
Why should you be very cautious giving SSRIs to old people?
Risk of hyponatremia
Serotonin Syndrome
Sweating, Hyperreflexia***, Myoclonus, Tremors, Dilated pupils, hyperactive bowel sounds
-HTN, Tachycardia, Tachypnea, Hyperthermia
Neuroepileptic Malignant Syndrome
-HTN, Tachycardia, Tachypnea, Hyperthermia
hyporeflexia***, normal pupils, normal bowel sounds
Why should you be cautious with using opioids and antidepressants?
Increased risk of serotonin syndrome
Fluoxetine
broad and strong inhibitor of CYP (most powerful)
Least CYP inhibition form SSRI
Vortioxetine
Escitalopram
secondary amines
amoxapine
desipramine
nortriptyline
inhibit NE>5HT
Tertiary amines
Amytriptyline
Clomipramine
Doxepin
Imipramine
generally inhibit NE and 5HT equally except clomipramine and amytriptyiline
What is unique about Amitriptyline and Clomipramine?
Tertiary amines that inhibit 5HT more than NE
TCAs
amitriptline clomipramine doxepine imipramine amoxapine desipramine Nortriptyline
**Blocks other receptors (histamine, muscarinic, adrinergic)
Side effects of TCAs
Tachycardia Orthostatic hypotension Dysrythmia Dry mouth Urinary Retention Blurred Vision Sedation/Fatigue
TCA overdose
coma, cardiotoxicity, convulsions
TCA effects in cardio cells
slows conductions
changes QRS
blocks sodium channels
(quinedien like)
Non-TCA SNRI
Desvenlafaxine,
Duloxetine
Venlafaxine
Levomilnacipran
*less risk of sexual dysfunction
Mirtazapine
Blocks alpha 2 receptors on NE and 5-HT presynaptically and blocks post-synaptic 5-HT 2/3
- No SERT/NET actvity
- *H1 blockade (Sedation)
**weight gain
Nefazodone & Trazodone
**H1 blockade (sedation)
block post-synaptic alpha one receptor and post synaptic 5-HT2
Orthostatic Hypotension
NDRI side effects
Stimulating Agitation/Insomnia HTN, Tachycardia Weight loss Seizures
MAOI MOA
Increase level of monoamines in neuronal vesicles to increase serotonin, 5-HT, and DA released
-Oral—>irreversible
(non-selective except segeline)
Segeline
MAOI
transdermal patch
selective at low doses
non-selective MAOa in GI inhibits Tyramine metabolism
MAOI Side Effects
Orthostatic hypotension Sexual dysfunction Insomnia/Agitation Drug interactions (SSRIS, TCA)--->2 week washout **Risk of HTN crisis risk of serotonin syndrome
What is the major concern with MAOI?
Hypertensive Crisis due to increased tyramine
Why is Tyramine of Concern?
causes a HTN crisis
levels increased with MAOA (when inhibited by MAOI)
age cheese, soy, beer
Esketamine
NMDA (glutamate) antagonist
treatment resistant depression
Nasal Spray
–must watch for 2 hours post
Brexanolone
GABA allosteric modulator (endogenous to allopregnenalone)
indicated for post partum depression
60 hour IV infusion
Mood Stabilizers (Anti-seizure meds)
Carbamazepine
Lamotrigine
Valporic Acid
Lithium
Mood stabilizer -neuroprotective -neuroproliferative Inhibits dopamine neurotransmission downregulates NMDA **increases GABA levels in CSF handled by kidneys like sodium **narrow therapeutic index
Lithium Side Effects
Polyuria like Diabetes Insipidus
tremor
goiters
serotonin syndrome
Lithium Drug Interactions
Diuretics
ACE inhibitors
NSAIDS
Lithium Therapeutic Index
Narrow
0.6-1.2 mEq/L
Indications for Lithium
- acute& maintance of bipolar 1/ mania
- reduced risk of suicide
- augment unipolar depressive treatment with poor response
Carbamazpiene
major CYP inducer
acute and maintance of Bipolar 1
Lamotrigine
maintance of bipolar 1 and 2
antiseizures
Valporic Acid
acute bipolar 1
Flumazenil
Benzodiazapene antagonist esp if benzo overdose
associated with seizures
Long Acting Barbiturates
Phenobarbital
Short Acting Barbiturates
Secobarbital
Ultra-Short Acting Barbiturate
Thiopental
Sedatives
Drug that decreases CNS activity, moderates excitement, and calms recipient
-Anxiolytic
Hypnotic
Drug that produces drowsiness and facilitates onset and maintenance of sleep
-More pronounced CNS depression
Benzodiazapines
acts on Gaba A receptor enhances Gaba activity
—hyperpolarization with CL- influx
(sedation and hypnotic effects, relaxation, anxiolytic, anticonvulsant)
-wide distribution throughout body: breast milk
-dependence and tolerance
-“LAMS and “PAMS”
-high therapeautic index
-cumulative toxicity
Barbiturates
acts on GabaA receptor
widely distributed throughout the body (placenta/breastmilk)
-mild sedation and anesthsia
-treats seizures, insomnia, tension HA with acetominophen and caffeine
can counteract the effects of stimulants
induces CYP450
Contraindications to Diazepam
Myasthenia Gravis
Respiratory Insuffiency
Hepatic 3 Insufficiency
Sleep Apnea Syndrome
**don’t use with alcohol or other CNS depressant
Alprazolam
CYP3A -management of anxiety disorders -panic disorder CI: acute narrow angle glaucoma, ketoconazole, itraconazole Dependence & withdrawal: seizures
Midazolam
given IM or IV
pre-op anxiolytic/ sedation/ amnesia
given before other anesthesia
BBW: respiratory depression
Diazepam
anxiolytic, sedative, muscle relaxant, anticonvulsant
prolonged half life: 48 hours (increased in cirrhosis)
active metabolite
-rapid rate of oral onset
–management of anxiety disorders
–treat for acute alcohol withdrawal syndrome
Triazolam
short term treatment of insomnia
BBW: profound sedation, respiratory depression, coma, death
Chlordiazepoxide
BENZODIAZEPINE
- pre-op apprehension/anxiety
- short relief of anxiety
- withdrawal symptom of alcoholism
BBW: sedation, respiratory depression, coma, death esp with opiods
Lorazepam
Treatment of seizure disorder**
pre-op anxiety
Flurazepam
long acting hypnotic for insomnia treatment
Thiopental
ultrashort acting barbiturate
- IV only
- used for brief procedures
- first anesthesia given before “big anesthesia”
- controls anesthesia induced convulsions
- decreases intracranial pressure
AE: cardiac arrythmias, laryngospasm, bronchospasm
Secobarbital
preanesthetic
**short term treatment for insomnia (loss of effect after 2 weeks)
Secobarbital Contraindications
latent porphyria impaired liver functions test respiratory disease (obstruction/dyspnea)
Phenobarbital Cautions
depressed patients with/without suicidal ideations
Phenobarbital
used as sedative/hypnotic
Induces liver enzymes****
Phenobarbital Contraindications
latent porphyria
Good insomnia drugs
Zolpidem (sustained sleep maintenance) Zalpelon Ezopicalone -CYP3A4 -Short half life -binds alpha 1 subunit of GABAa subunit
Zolpidem (ambien)
barbituate
sustained sleep
Rameleton
MT1 and MT2 agonist
AE: dizziness, somnolence, fatigue, endocrine changes
Avoid coadministration with fluvoxamine (an SSRI)
**treats disorder of sleep onset
Buspirone
generalized anxiety disorder
CYP3A4
–no sedation/hypnosis/euphoria
MOA unknown
Zaleplon
non benzo hypnontic
short term tx of insomnia
GabaBZ receptor
short term insomnia treatment
Chloral Hydrate
short term sedative
treat alcohol withdrawal syndrome
relieves anxiety with other drug withdrawal
Meprobramate
short term anxiety relief
slows activity of brain
Ezopicalone
treatment for insomnia
improve sleep maintanence
risk of morning impairment and CNS depression
AE: dry mouth, hallucination, anxiety, infection
