Week 3 - Drugs Flashcards
(38 cards)
Depression-related neurotransmitters in the brain
Norepinephrine= starts in Locus coeruleus and projects all over Serotonin= starts in raphe nuclei and projects everywhere (incl spinal cord)
Tricyclic antidepressant actions
Blocks NE and serotonin reuptake
thus after a period of a few weeks downregulates post-synaptic receptors
sides: decreases REM, increases stage 4, anticholinergic, sedating, orthostatic hypotension, cardiac abns
Overdose: hyperpyrexia, seizures, cardiac conduction probs
SSRI antidepressants
block serotonin reuptake (SERT)
action similar to TCAs, but less side effects
sides: nausea, insomnia, sexual dysfxn
potential dangerous “serotonin reaction” if with MAOIs
also warning about neuroleptic malignant syndrome
and danger for suicide in kids
Withdrawl: dizziness, insomnia, nausea, visual disturbance, etc
Mirtazapine
atypical antidepressant
blocks a2 presynaptic receptors on NE and serotonin neurons
thus increases release of neurotransmitter which has similar result to tricyclics
increases appetite
MAO inhibitor actions
non-selective as antidepressants 3rd line blocks breakdown of NE and serotonin may cause hypomania in bipolar, corrects sleep disorders, may produce stimulation orthostatic hypotension toxicity: agitation, hallucinations Risk of HTN crisis if ingests tyramine from food also can be used for narcolepsy
SSRI drugs
Fluoxetine= long half-life, has drug interactions
Sertraline= shorter half life, less drug rxns, also for OCD, PTSD, panic
Paroxetine= also for hot flashes
Fluvoxamine= for OCD
Citalopram/Excitalopram=
SNRI antidepressants
block both 5-HT and NE reuptake
side effects similar to SSRIs
SNRI drugs
Duloxetine= also for nauropathic pain, caution with liver ds Venlafaxine= for depression and anxiety Milnacipran= for fibromyalgia
Bupropion
atypical antidepressant
blocks NE and dopamine uptake
also for nicotine withdrawal and SAD
no weight gain or sex dysfxn
Trazodone
atypical antidepressant
SSRI-like, sedating
used for insomnia
can cause priapism (long erections)
Tricyclic drugs
Imipramine= for enuresis in kids amitriptyline= also for chronic pain Trimipramine= Doxepin= Desipramine= Nortriptyline= Protriptyline Clomipramine= for OCD
MAO inhibitor drugs
Phenelzine= irreversible Tranylcypromine= reversible
St John’s Wort
Hypericum perforatum
MAOI activity
maybe good for mild depression
has drug interactions (with birth control)
Buspirone
anti-anxiety partial 5-HT1a agonist less sedating, no cross-tolerance with benzodiazepines treat GAD takes 2wk to work
Benzodiazepine actions
anti-anxiety and pro-sleep
Potentiate GABA receptor
many have active metabolites which affect duration of action
CNS: decrease anxiety, sedation, hypnosis, muscle relax, anterograde amnesia
minimal CV and respiratory actions
Withdrawal: anxiety, insomnia, hallucinations, seizures
can have bad effects with alcohol
Benzodiazepine drugs
Diazepam= fast onset, long duration, also muscle relaxant, has active metabolites Chlordiazepoxide= used for alcohol withdrawal Alprazolam= short duration, anti-panic Lorazepam= slower onset, longer duration Clonazepam= used for acute manic episodes
Benzodiazepines for sleep
cause decreased latency, decreased stage3/4/REM
rebound insomnia on withdrawal
tolerance and dependence, occasional idiosyncratic excitement
Zolpidem and Zaleplon
bind to BDZ receptor (but not actually benzodiazepines)
hypnotics
preserve stage 3/4 sleep, minor effect on REM
Zaleplon has faster onset and shorter half life
can have sleep-walking
Flumazenil
benzodiazepine antagonist
Eszopiclone
hypnotic
similar to zolpidem, but maybe at a different GABA site
Ramelteon
hypnotic
melatonin MT1 and MT2 receptor agonist
used to help fall asleep (not so much for staying asleep)
Barbiturates
hypnotics: pentobarbital, phenobarbital, thiopental
rapidly absorbed, highly lipid
can induce drug metabolism
also act on GABA receptor (likle benzodiazepines)
sedation, anesthesia, respiratory depression
tolerance and dependence
toxicity= resp depression and death
Skeletal muscle relaxants
Diazepam: also sedation, benzodiazepine
Baclofen: GABA-mimetic at GABA-B, much less sedation
Tizanidine: a2-adrenergic agonist, sides are drowsiness, hypotension, dry mouth
Dopamine receptors
D1-like (D1 and D5)= activate adenylyl cyclase
D2-like (D2,3,4)= inhibit adenylyl cyclase
D2 is the important one in schizophenia drugs