PCL200 FInal Flashcards
Synthetic THC/dronabinol (Marinol)
Target: CB1 + CB2 (agonist)
Used for: Anorexia from AIDS & Cancer, chemo nausea, muscle spasticity, neuropathic pain
Side effects: increased appetite, hallucinations, memory/motor impairment, sleepiness, psychosis/delusions at high dose.
CBD (cannabidiol)
Target: GPR55, 5HT1A, CB1 (questionable)
Used for: Dravet syndrome (severe epilepsy, development delays), Childhood epilepsy
Being tested for chronic pain/inflammatory disorder
No side effects discussed
THC:CBD Nabiximol (Sativex)
CB1/CB2 agonist, GPR55, 5HT1A
Used for: Anorexia in AIDS/Cancer, chemo nausea, muscle spasticity, neuropathic pain, Dravet system
Side effects: increased appetite, hallucinations, memory/motor impairment, sleepiness, psychosis/delusions at high dose.
1st gen anti-psychotics (neuroleptics): Chlorpromazine + Haloperidol
Target: D2R dopamine receptor (antagonist)
Used for: Schizophrenia, Psychosis
Side effects: anhedonia, sleepiness, Parkinson symptoms, dyskinesia (involuntary muscle movement), increased lactation, disrupts menstrual, fertility issues, weight gain
Clozapine - 2nd gen Atypical antipsychotics
Target: 5HT2A/2C, D2 (antagonist), multiple others
Used for: Schizophrenia, Psychosis
Side effects: anhedonia, sleepiness, metabolic syndrome: (type2 diabetes, weight gain, blood lipid changes, increase cardiovascular disease), Rare/fatal blood disorder.
2nd gen Atypical antipsychotic: Olanzapine/Risperidone
Target: 5HT2A (partial agonist), D2 antagonist
Used for: Schizophrenia, Psychosis
Side Effects: anhedonia, sleepiness, metabolic syndrome: type2, weight gain, blood lipid changes, increase cardiovascular disease.
Anti-depressant: Ketamine
Target: NMDA receptor antagonist
Used for: Depression (rapid acting, thru IV infusion)
Side Effects: hallucinations during treatment
TCA: Imipramine, Amitriptyline
Target: TCA (tricyclic antidepressant) - Inhibit SERT/NET,
Antagonist: 5HT2A/2C/6/7, A1 adrenergic receptor, muscarinic acetylcholine / histamine receptor
Used For: Depression, neuropathic pain
Imipramine: First TCA discovered based off chlorpromazine structure!
1st line SSRI: Fluoxetine (Prozac - for adolescents),
Paroxetine (Paxil) - anti-cholinergic + weight gain
Citalopram (Celexa) - SERT selective
Sertraline (Zoloft) - DAT antagonist
Target: SSRI (selective serotonin reuptake inhibitor) - SERT antagonist, elevate serotonin
Used For: depressive mood disorders, anxiety disorders, bulimia, neuropathic pain
Side effects: headache, insomnia, GI disturbance, less sexual, weight gain, dizzy, weak, tired, tremor, agitate, anxiety.
TCA: Venlafaxine (Effexor)
Duloxetine (Cymbalta)
Target: SNRI (serotonin - norepinephrine reuptake inhibitor) - SERT & NET antagonist
More effective for depression than SSRI
Used For: depressive mood disorders, anxiety disorders, bulimia, neuropathic pain
Lithium - Mood stabilizer
Target unknown: reduces signal events downstream of dopamine receptor
Used For: Bipolar disorder - mood stabilizer
Side Effects: dry mouth/thirst, tremor, fequent urination, kidney toxicity with long-term use/ high dose. Narrow therapeutic window
Pharmacotherapy: Mood stabilizer - Lamotrigine/carbamazepine
Target: Multiple: glutamate receptor (antagonist) & calcium channel (antagonist)
Used For: Epilepsy and bipolar disorder (MOA unknown)
Mood stabilizer: Pharmacotherapy Valproate/valporic acid
Target: Multiple - Chromatin (makes DNA available for gene expression = increase GABA), voltage-gated sodium channel antagonist
Used For: epilepsy and bipolar disorder (unknown MOA)
Hallucinogen (natural): Psilocybin
Mescaline Dimethyltryptamine (DMT)
Semi-synthetic: Lysergic acid diethylamide (LSD)
Target: Serotonin 5HT2A agonist
Used For: psilocybin assisted psychotherapy (still in clinical trials; not approved yet)
Reserpine
VMAT2 antagonist (vesicular monoamine transporter)
Used to be anti-hypertension, no longer used for brain disease, causes depression
Phenytoin
Target: antagonist for voltage-gated sodium channels
Used For: Epilepsy
Nerve stabilizer - Phenobarbital
Target: agonist of GABA chloride channel
Used For: epilepsy, status epilepticus
Ethosuximide
Target: antagonist of T-type calcium channel
Used For: absence seizures - brief, sudden laps of of unconsciousness (first line treatment for absence)
SERT
Serotonin epinephrine reuptake transporter
Endocannabinoids (eCB’s)
Post-synaptic neuron by enzymes that convert membrane lipid into eCB. Diffuse + bind to close Cb1 receptor on presynaptic neuron
Quick degrade = fast acting modulators to correct level of neurotransmission.
CB1 activation causes pre-s neuron to release less neuro-T.
Appetite stimulant, reduces pain in descending pathway, helps learning/memory, helps bone formation
Environmental risk factors that may cause Schizophrenia
Maternal infection (2nd tri),
Maternal starvation,
plasmodium gondii (parasite),
birth complications,
physical/psychological trauma in childhood,
low socioeconomic status
Urbanicity
Drug exposure
Borderline Personality Disorder (BPD) - Causes/Triggers
Genetic component: 70-80% (no single gene causes BPD), prevalence 1-2%, Onset
Treatment mix: mood stabilizers, antipsychotics, antidepressants
Triggers: sleep-deprivation, sleep/day schedule change, amphetamine, stress (positive and negative)
Monoamines: (DA) dopamine, (NE) norepinephrine, (5HT) serotonin. Melatonin, histamine, trace amines
MOA: packaged in synaptic vesicles by vesicular monoamine transporter 2 (VMAT2)
Used for: mood, sleep, appetite, arousal, sexual function, cognition, motivation, aggression, peristalsis
Monoamine Oxidase Inhibitor: Phenelzine
Degrades serotonin, NE, adrenaline, DA, tyramine (regulates blood pressure -amino acid)
MOA: HIGHLY EFFECTIVE binds to enzyme = permanently inactive until cell makes more.
Not used unless all options are exhausted: cause hypertensive crisis (adrenaline)/serotonin syndrome = fatal
MOAI: Phenelzine substitute
moclobemide: effective and safer
TCA: Bupropion (Wellbutrin)
Inhibits DAT + NET (own class not SSRI/SNRI)
Common effects and adverse - serotonergic hallucinogens
Serotonin syndrome: excessive activation of serotonin receptors
Adverse at hallucinogenic doses: nausea/vomit, clenched teeth, sweating, dry mouth, muscle twitch/convulse
Overdose: from hyperthermia (internal temp very high), high blood pressure = cardiovascular events
Hallucinogen: MDMA
Similar to methamphetamine/amphetamine
More selective on SERT
