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Biogenic monoamine neurotransmitters
- Derived from tyrosine, tryptophan, phenylalanine, and thyroid.
- Histamine
- Catecholamines: Dopamine, EPI, NEP
- Tryptamines: Serotonin, melatonin
- Trace amines
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Amphetamine
- Stimulant for ADHD
- MOA: inc DA & NE
Contra: Drug abuser, hyperthyroid, HTN
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Amphetamine salts XR
- Stimulant for ADHD
- MOA: inc DA & NE
Contra: drug abuser, hyperthyroid, HTN
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Lisdexamfetamine
- Stimulant for ADHD
- MOA: inc DA & NE
- Contra: Drug abuser, hyperthyroid, HTN
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Methylphenidate
- Stimulant for ADHD (SR-12hrs)
- MOA: inc DA & NE
- A/E: insomnia (narcolepsy)
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Methylphenidate hydrochloride (transdermal patch)
- Stimulant for ADHD (9 hour wear ~to cocaine)
- MOA: Inc DA & NE
Contra: Not in adults
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Atomoxetine
- Nonstimulant for resistant ADHD (1/day)
- MOA: NE uptake inhibitor/ CYP450 metabolism
CONTRA: tramadol, MAOI, drugs that inhibit CYP450
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Buproprion
- Nonstimulant for resistant ADHD (also antidepressant)
- MOA: inc NE & DA/ inhibits CYP 450
A/E: peripheral NE & DA effects
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Guanfacine
- Nonstimulant for resistant ADHD
- MOA: A-2 receptor agonist in prefrontal cortex --> inc noradrenergic system (for tics and emotional bursts)
CONTRA: sedative drugs, phenobarbital and phenytoin (may dec plasma level)
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Carbamazepine (1st generation)
FOR: All the partial seizures
MOA: Na channel inactivation
Enzyme inducer
best risk/benefit ratio
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Phenytoin (1st generation)
FOR: All partial seizures
- MOA: slows Na channel recovery
- 5-10X enhances GABA
Enzyme inducer
Inhibits Warfarin metabolism
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Phenobarbital (1st generation)
FOR: status epilepticus, Generalized t-c, partial seizures
MOA: Inc GABA
Enzyme inducer
Teratogen
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Ethosuximide (1 st generation)
FOR: Partial Seizures
MOA: Prodrug
Enzyme inducer
No Warfarin interference
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Gabapentin(2nd generation)
FOR: Partial & generalized seizures
MOA: Inc GABA via Ca2+ channel
No enzyme induction
A/E: ataxia & fatigue
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Pregabalin (2nd generation)
FOR: Partial and generalized seizures
MOA: Inc GABA via Ca2+ channel
ataxia & fatigue
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Ezogabine (2nd generation)
FOR: Resistant partial seizures
MOA: K channels
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Valproic acid (1st generation)
FOR: Partial, absence, and myoclonic seizures
- MOA: Na inactivation
- Inc GABA
- Reduces T-type Ca2+ current
Inhibits liver enzymes
Teratogen
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Clonazepam (1st generation) benzodiazepine
FOR: Absence, Lennox-Gastaut syndrome w/ myoclonic seizures
MOA: Inc GABA A opening frequency
A/E: Lethargy Cognitive effects
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Lamotrigine (2nd generation)
FOR: All partial, Lennoz-Gastut syndrome, general T-C, absence
- MOA: Na channel inactivation
- inhibit glutamate release
(used with Valproic in drug resistant epilepsy)
Aggravates myoclonie seizures
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Levetiracetam (2nd generation)
FOR: Partial, generalized, myoclonic seizures
MOA: Unkonwn
No enzyme induction
asthenia
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Topiramate (2nd generation)
FOR: All partial & Lennox-Gastut Syndrome
- MOA: Red Na current
- activate K hyperpolarization
- enhance GABA
- Limits glutamate receptor
- Inhibit Brain Carbonic anhydrase
Enzyme inducer
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Felbamate (2nd generation)
FOR: Partial and generalized & Lennox-Gastut syndrome
- MOA: inhibits NMDA response
- Potentiate GABA response
w/ other anticonvulsants --> rash & toxicities
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Zonisamide
FOR: Partial, generalized T-C(except myoclonic)
- MOA: Inhibits Ca channel
- Prolongs Na channel inactivation
- inhibits Carbonic anhydrase
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Drug for Status epilepticus
- IV lorazepam
- Diazepam followed by phenytoin
- phenobarbital & phenytoin
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Imipramine
Tricyclic for Depression
MOA: inhibits 5-HT and NEP reuptake sites
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Amitriptyline
Tricyclic for Depression
MOA: inhibits 5-HT and NEP reuptake sites
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Clomipramine
Tricyclic for Depression
MOA: inhibits 5-HT and NEP reuptake sites
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Phenelzine
MAOI for depression
MOA: inhibits breakdown of the 3 monoamines
Irreversible nonselesctive MAOI
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Selegiline Patch
MAOI for depression
MOA: inhibits breakdown of the 3 monoamines
Irreversible MAO-B inhibitor
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Fluoxetine
SSRI for depression
MOA: block reuptake sites --> downregulate auto-receptors
inhibits P450 enzymes
can be used in kids
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Paroxitine
SSRI for depression
MOA: Block 5HT reuptake site --> autoreceptor downregulate
inhibits P450 enzyme
Used in kids
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Escitalopram
SSRI for depression
MOA: block reuptake sites-> downregulate auto-receptors
- Strong efficacy
- tolerability
- OK for kids
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citalopram
SSRI for depression
MOA: block reuptake site -> downregulate autoreceptor
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Sertaline
SSRI for depression
MOA: block reuptake site -> downregulate autoreceptor
- Great efficacy
- tolerable
- Ok for kids
TERATOGEN
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Serotonin Syndrome
Hyperkinetic, tremor, clonus, hyper-reflexia, agitation, tachycardia
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Duloxetine
SNRI for depression
Ok For kids
Liver concerns
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Venlafaxine
SNRI for depression
- good efficacy
- ok for kids
No P450 interaction
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Desvenlafaxine
SNRI for depression
- ok for kids
- No P450 interaction
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Trazodone
Atypical for depression
- MOA: presynaptic alpha2 receptor blocker
- block 5-HT2A and 2c autoreceptor
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Buproprion
Atypical for depression
MOA: NE & Da uptake inhibitor
- tolerable
- Ok with kids
- Safe in cardiac patients
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Mirtazapine
Atypical for depression
MOA: H1 antagonism
Blocks 5-HT3 sites -> anti-nausea
- good efficacy
- ok with kids
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Agomelatine
Atypical for depression
MOA: 5-HT2C antagonist & MT1/MT2 agonist
Restores circadian rhythms and improves sleep quality
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First line treatment in Depression
- SSRI
- SNRI
- Buproprion
- CBT
- interpersonal therapy
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Barbituates
1st generation sedative hypnotic (for anxiety)
Inc time channel is open
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Phenobarbital
Barbituate Anxiety (long acting)
MOA: inc time channel is open
- Increased pain perception
- Respiratory depression
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Pentobarbital & secobarbital
Barbituates (intermediate)
MOA: inc time GABA channel is open
For: surgery, anesthesia, & sleep induction
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Thiopental
Barbituate (short acting)
MOA: Inc time GABA channel is open
Supports anesthesia
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Benzodiazepine
2nd generation
MOA: Inc frequency of GABA channel opening
- Teratogen
- No coma or death
- active metabolite accumulation
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Chlordiazapoxide
Benzodiazepine (long acting)
MOA: inc opening frequency of GABA channels
Hypnotic
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Diazepam
Benzodiazepine (long acting)
MOA: inc open frequency of GABA channel
dec sleep latency, inc total sleep time, but dec REM
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