Week 3 - Drugs Flashcards

(38 cards)

1
Q

Depression-related neurotransmitters in the brain

A
Norepinephrine= starts in Locus coeruleus and projects all over
Serotonin= starts in raphe nuclei and projects everywhere (incl spinal cord)
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2
Q

Tricyclic antidepressant actions

A

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

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3
Q

SSRI antidepressants

A

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

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4
Q

Mirtazapine

A

atypical antidepressant
blocks a2 presynaptic receptors on NE and serotonin neurons
thus increases release of neurotransmitter which has similar result to tricyclics
increases appetite

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5
Q

MAO inhibitor actions

A
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
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6
Q

SSRI drugs

A

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=

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7
Q

SNRI antidepressants

A

block both 5-HT and NE reuptake

side effects similar to SSRIs

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8
Q

SNRI drugs

A
Duloxetine= also for nauropathic pain, caution with liver ds
Venlafaxine= for depression and anxiety
Milnacipran= for fibromyalgia
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9
Q

Bupropion

A

atypical antidepressant
blocks NE and dopamine uptake
also for nicotine withdrawal and SAD
no weight gain or sex dysfxn

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10
Q

Trazodone

A

atypical antidepressant
SSRI-like, sedating
used for insomnia
can cause priapism (long erections)

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11
Q

Tricyclic drugs

A
Imipramine= for enuresis in kids
amitriptyline= also for chronic pain
Trimipramine=
Doxepin=
Desipramine=
Nortriptyline= 
Protriptyline
Clomipramine= for OCD
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12
Q

MAO inhibitor drugs

A
Phenelzine= irreversible
Tranylcypromine= reversible
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13
Q

St John’s Wort

A

Hypericum perforatum
MAOI activity
maybe good for mild depression
has drug interactions (with birth control)

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14
Q

Buspirone

A
anti-anxiety
partial 5-HT1a agonist
less sedating, no cross-tolerance with benzodiazepines
treat GAD
takes 2wk to work
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15
Q

Benzodiazepine actions

A

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

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16
Q

Benzodiazepine drugs

A
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
17
Q

Benzodiazepines for sleep

A

cause decreased latency, decreased stage3/4/REM
rebound insomnia on withdrawal
tolerance and dependence, occasional idiosyncratic excitement

18
Q

Zolpidem and Zaleplon

A

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

19
Q

Flumazenil

A

benzodiazepine antagonist

20
Q

Eszopiclone

A

hypnotic

similar to zolpidem, but maybe at a different GABA site

21
Q

Ramelteon

A

hypnotic
melatonin MT1 and MT2 receptor agonist
used to help fall asleep (not so much for staying asleep)

22
Q

Barbiturates

A

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

23
Q

Skeletal muscle relaxants

A

Diazepam: also sedation, benzodiazepine
Baclofen: GABA-mimetic at GABA-B, much less sedation
Tizanidine: a2-adrenergic agonist, sides are drowsiness, hypotension, dry mouth

24
Q

Dopamine receptors

A

D1-like (D1 and D5)= activate adenylyl cyclase
D2-like (D2,3,4)= inhibit adenylyl cyclase

D2 is the important one in schizophenia drugs

25
Typical antipsychotics
D2 blockers mostly variable absorption, lipid soluble, complex metabolism sides: sedation, extrapyramidal effects (dystonia, parkinsonism, akathisia, tardive dyskenesia) more sides: anticholinergic, orthostatis hypotension, neuroendocrine effects, cardiac effects (thioridazine), weight gain, seizures Neuroleptic Malignant Syndrome- lethal hypodopaminergic side effect- hyperthermia, parkinson-like
26
Typical antipsychotic drugs
Phenothiazines: - chlorpromazine, triflupromazine: low/med potency, sedative, anticholinergic - thioridazine, Mesoridazine: low potency, sedative, less extrapyramidal, anticholinergic - Trifluoperazine, fluphenazine, perphenazine, prochlorperazine: high potency, less sedative, more EPS, less anticholinergic Chlorprothixene, thiothixene: similar to phenothiazines Haloperidol: similar to high-potency piperazine Pimozide: potent, tx of Tourette's
27
Atypical antipsychotics
Block D2 and 5-HT2 usually less EPS side effects, less tardive dyskinesia better at improving negative sx
28
Atypical antipsychotic drugs
Clozapine= D4 and 5-HT2 blocker, muscarininc antagonist,, seizures, fatal agranulocytosis Olanzepine= fewer EPS sx, less seizures,, weight gain and diabetes Risperidone= less seizures and less antimuscarinic, available as IM inj,, metabolized to Paliperidone Quetiapine= shorter half-life, also for depression Ziprasidomne= may also be anxiolytic Aripiprazole= also for depression Asenapine, Iloperidone, Lurasidone
29
Lithium
for Bipolar, blocks manic behavior no effect in normals inhibits IP2 to IP1, which blocks PIP2/IP3 recycling narrow therapeutic window, concentration influenced by Na concentration (inc Na excretion= inc Li levels) Sides: fatigue, tremor, GI, slurred speech, ataxia, serious toxicity at higher levels
30
Other drugs for bipolar
Valproic acid / divalproex sodium: first line, sedating Carbamazepine: acts at Na channel Lamotrigine, topiramate: antiseizure Haloperidol (for initial control)
31
Buprenorphine
(Suboxone) used for treating opiate addiction,, also for pain mu partial agonist often mixed with naloxone to reduce abuse potential blocks cravings and prevents receptor activation (sets new baseline) highly safe
32
Marijuana
contains THC, cannabidiol, cannabinol, many more reaches brain in 30sec when smoked, 30min when ingested metabolized and distributed in fat duration of action is 1-6hrs, half life of 20-50hrs CB1 receptor- Gi inhibits transmitter release effects: memory impairment, worsens driving, tachycardia, orthostatic hypotension, bronchodilation, lowers testosterone, sperm ct anxiety, paranoia, worse schizophrenia, amotivational has tolerance and dependence- restlessness, irrability, craving Therapeutic use: control nausea (Dronabinol), AIDS wasting syndrome
33
Phencyclidine (PCP) and Ketamine
NMDA antagonists autonomic and CV sympathomimetic- tachycardia, hypertension, potentiates catecholamines tolerance, no physical dependence Ketamine is less potent, shorter lasting than PCP numbness of extremities, analgesia, anaesthesia, resembles sensory isolation, cateleptoid motor PCP: anxiety, aggression, hallucinations, convulsions
34
Indoleamines and Phenethylamines
Indoleamines: LSD, psilocybin, 5M-DMT Phenethylamines: MDMA (ecstasy), mescaline, amphetamines
35
LSD
highly potent, 12hr duration sympatheomimetic- tachycardia, inc BP, psychomotor stim visual hallucinations, lability of mood, impaired judgement action at 5-HT receptor flashbacks, possible neurotoxicity tolerance and cross-tolerance
36
MDMA- Ecstasy
``` feelings of well being and connection less potent onset 30min, duration 4hrs psychomotor stimulation, restlessness, bruxism, sweating, tremor hangover, maybe neurotoxicity ```
37
Gamma-Hydroxybutyrate (GHB)
``` related to GABA, but doesn't act on GABA receptor duration 3hrs primarily a depressant interacts with ethanol drowsiness, ataxia, nausea amnesia at high doses ```
38
Salvia Divinorum
psychedelic, unpleasant to many 20-40min duration, dream-like Salvinorin-A= kappa opioid agonist