Psychopharm Flashcards
(109 cards)
Presynaptic 5HT: function and targets
- reuptake channels
- TCAs and SSRIs
~ clomipramine
~ fenfluramine
Sumatriptan receptors
- vasoactive
- presynaptic: 1B, 1D
- postsynaptic: 1F; 1B,1D
5HT-3 receptors
- most clinically active
- ondansterone
- 5HT-2C/2A receptor
- active site of atypical antipsychotics and LSD
Mesolimbic pathway
- decreased DA
- increased DA
- increase: antipsychotic, anti-anxiety, anti-agitation
- decrease: inhales pleasure; increases psychosis, mania, agitation
- note: nucleus acumbens is center for addiction and pleasure
Meso-cortical path
- increased DA
- decreased DA
- decrease: negative symptoms of schizophrenia, depression, cog. Impairment, inattention (hypofrontality, ADD)
- increased: opposite of above
Nigro-striatal pathway
- increased DA
- decreased DA
Decreased: 4 extra-pyramidal symptoms
~ dystonia, akinesia, Parkinsonism, NMS (fever, AMS, autonomic instability and increased CK)
Increased: tardive dyskinesia, chorea, Tourette’s
Tuberinfundibular pathway
- decreased DA
- increased DA
- decreased: increased prolactin
~ results in -> galactorrhea, amenorrhea, gynecomastia,
infertility, impotence - increased: decreased prolactin
Chemoreceptive trigger zone for DA
- decreased: antiemetic
- increased: N/V
5HT/NE synthesis
5HT - tryptophan derived - tryptophan hydroxylase - rate limiter NE - Tyrosine derived - tyrosine hydroxylase (first step) - rate limiter
Selective monamine transporters (3)
- 5HTT
- NET
- DAT
VMAT
- recycling of monoamines int vesicles
5HT N2K receptors
- 5HT3 is the only non-G protein receptor
- 5HT1D,1A, 2A, 2C (involved in depression)
5HT1A
- in raphe nuclei and post synaptic cell bodies hippocampus
5HT1D
- auto-inhibitors of 5HT release at axon terminals
alpha adrenergic receptors
- a1, 2 and B1, 2 most relevant
- a2: auto inhibitory
MAO-A, B
- anti depressant is primarily MAO-A
Phenelzine (selegiline): MAOI, use, side effects
- MOA: MAOB inhibitor (Parkinson’s, dermal patch depression)
- SE: result from a-adrenergic blockade
~ orthostatic hypotension
~ weight gain
~ sexual dysfunction
~ potentially lethal drug interaction (carbidopa, meperidine,
linezolide, St. John wort, SSRIs)
Tricyclic antidepressants: effects, examples
- TCAs With secondary amines preferentially affect NE systems
- TCAs With tertiary amines preferentially affect 5HT systems
- don’t effect DA
- can also trt neuropathic pain
- amytriptyline, nortriptyline, desipramine, imipramine
Tricyclics specs
- MOA: non-selective 5HT and NE uptake inhibition
- SE: cardio-conduction delays, first degree blocks
~ also blocks: 5HT, NE, a-1, hist, ACh
Histamine blockade SE
- sedation
- weight gain
- impaired coordination
- orthostatic hypotension
- cognitive impairment
Muscarinic blockade
Anti-parasympathetic
- dry mouth
- constipation
- urinary hesitancy
- decreased visual acuity (loss of accommodation)
- aggravation of glaucoma
- tachycardia
- cognative impairment
- impotence
A adrenergic blockade SE
- orthostatic hypotension
- reflex tachycardia
- ejaculation
- cognitive impairment
5HT blockade SE
- anxiety
- anorexia
- N/V
- insomnia
- sedation
- sexual SE: arousal
- weight gain
- serotonin