Antipsychotics, antidepressants, opioids, drugs of abuse, endocrine Flashcards
target action of typical antipsychotics
D2 receptors in caudate putamen, nucleus accumbens, cerebral cortex, hypothalamus
dopaminergic tract-regulating mentation and mood
meso-cortical, meso-limbic
dopaminergic tract-extrapyramidal function
nigrostriatal
dopaminergic tract-control of prolactin relace
tuberoinfundibular
dopaminergic tract-eating behavior
medullary-periventricular
dopaminergic tract-anticipatory motivational phase of copulatory behavior
incertohypothalamic
antipsychotic of choice for drug resistance
clozapine
caused by supersensitivity of dopamine receptors
tardive dyskinesia
tx for acute dystonia
diphenhydramine
tx for parkinsonism
benztropine
tx for rabbit syndrome
benztropine
tx for tardive dyskinesia
nonerome
tx for akathisia
decrease dose, diphenhydramine
tx for neuroleptic malignant syndrome
withdraw drug, dantrolene, diazepam, dopamine agonist
typical antipsychotic; SE: corneal and lens deposits, neuroleptic malignant syndrome, contact dermatitis
chlorpromazine
typical antipsychotic; SE: retinal deposits, cardiotoxicity, w/ strongest autonomic effects, fatal ovedose
thoridazine
typical antipsychotic known for major EPS, also used for Huntington’s and Tourette’s, least sedating among typicals
haloperidol/droperidol
only antipsychotic that reduces the risk of suicide
clozapine
weight gain attributed to atypical antipsychotics
probably from H1 and 5-HT2 blockade
atypical antipsychotic also used for manic episodes; SE: cataracts, hypnagogic hallucinations, priapism
quetiapine
only antipsychotic approved in the youth
risperidone
atypical antipsychotic; SE: QT prolongation, increased mortality in elderly with dementia-related psychosis
ziprasidone
least sedating among atypical anti-psychotics
aripiprazole
atypical antipsychotics with no atropine like effects, do not cause hypergly, hyperprolactinemia or weight gain
ziprasidone, aripiprazole
features of neuroleptic malignant syndrome
FEVER: fever, encephalopathy, vitals unstable, elevated CPK, rigidity`
MOA of lithium
decreases cAMP, inhibits inositol-1-phosphatase
SE of lithium; Tx
LITH: leukocytosis, insipidus, teratogen (Ebstein’s anomaly), thyroid enlargement, tremors, heart (bradycardia); also acneiform skin eruptions; hemodialysis
threshold for lithium toxicity
2 mEq/L
NTs responsible for mood
NE and serotonin
back-up drug for MDD
TCAs: imipramine (clomipramine, desipramine, amitryptyline, nortryptiline)
toxic dose of TCAs; lethal dose
7mg/kg; 15 mg/kg
ECG findings in TCA overdose
abnormal QRS morphology, prolonged QRS, abnormal R and S waves in AVR
features of TCA overdose; Tx
coma, convulsions, cardiotoxicity; bicarbonate (for QRS>100msec)
first line for MDD
SSRI (fluoxetine, paroxetine, citalopram, escitalopram, sertraline, fluvoxamine)
notable SE of SSRIs
erectile dysfunction
tx for serotonin syndrome
cyproheptadine
inhibits neuronal reuptake of serotonin and NE
SNRIs (venlafaxine, duloxetine, desvenlafaxine)
SNRI with hepatotoxicity SE
duloxetine
SNRI with cardiotoxicity and CYP450 inhibitio
venlafaxine
weak 5-HT reuptake inhibitors that blocks 5-HT2 receptors to make serotonin available to other receptors, SE: priapism; SE: hepatotoxicity
trazodone and nefazodone; trazodone; nefazodone
tetracyclic antidepressant which causes amenorrhea-galactorrhea syndrome and lowers seizure threshold
amoxapine
tetracyclic antidepressant which can be used as appetite stimulant; can cause nightmares
mirtazapine
tetracyclic antidepressant which can also be used for smoking cessation; also causes priapism, aggravation of psychosis, lower seizure threshold
bupropion
inhibits monoamine oxidase type A and B, increases NE and serotonin
MAOIs (phenelzine, tranylcypromine, selegiline)
causes hypertensive crisis when taken with tyramine (indirect acting sympathomimetic in cheese)
MAOIs
features of serotonin syndrome
FAT CHD; fever, agitation, tremors, clonus, hyperreflexia, diaphoresis
features of malignant hyperthermia
FCHART; fever, acidosis, rhabdomyolysis, trismus, clonus, HPN
precipitating drugs for serotonin syndrome
SSRIs, MAOIs, TCAs, meperidine, MDMA, St. John’s wort
opioids with shortest and longest half-lives
remifentanil; buprenorphine
mu opioid receptor (function, affinity)
inhibition of respiration, endorphins
delta opioid receptor (function, affinity)
dev’t of tolerance, enkephalin
kappa opioid receptor (function, affinity)
slowed GI transit, dynorphin
opioid analgesic which may be given trandermally or via lollipop
fentanyl
most potent opioid
ohmefentanyl
opioid of choice for relief in pancreatitis and labor pains
meperidine
opioid which causes serotonin syndrome w/ SSRIs or MAOIs
meperidine
agonist of mu and kappa receptors
meperidinethadone
opioid used for opioid dependence/withdrawal, can cause drug-induced hyperthyroidism, currently being investigated as a novel treatment for leukemia
methadone
partial opioid agonist; SE: hypogonadism, hearing loss
hydrocodone/oxycodone
partial opioid agonist which depresses medullary cough center through sigma receptor stimulation
dextrometorphan/ codeine
weak opioid agonist withdrawn due to fatal cardiotoxicity
propoxyphene
opioid which is a strong agonist of kappa receptors but weak antagonist of mu receptors
nalbuphine, buprenorphine, butorphanol, pentazocine
effects resistant to naloxone reversal
nalbuphine, buprenorphine, butorphanol, pentazocine
systemic opioid antagonist
naloxone
systemic opioid antagonist which also reduces alcohol dependence
naltrexone
dual-acting opioid analgesic, weak agonist of mu receptor, also inhibits reuptake of serotonin and NE, lowers seizure threshold and may cause serotonin syndrome
tramadol
CI of tramadol use
epilepsy
triad of opioid overdose
PRC: pupillary constriction, respiratory depression, coma
NT believed to cause addiction
excessive dopaminergic stimulation
antidepressants with limited benefit against amphetamine withdrawal symptoms
amineptine, mirtazapine
congeners of amphetamines
dimethoxymethylamphetamine (DOM), methylene dioxyamphetamine (MDA), methylene dioxymethamphetamine (MDMA/ ecstacy)
electrolyte imbalance which may be caused by ecstacy
profound hyponatremia
“speed”, “superspeed”
methamphetamine, cocaine
causes crack lung (hemorrhagic alveolitis), mydriasis, HPN, vasoconstriction, psychomotor agitation, hyperthermia, dyspnea, bowel ischemia, thrombus formation
cocaine overdose
presents with agitation, hypertension, tachycardia, delusions, hallucinations, hyperthermia, seizures
methamphetamine overdose
teratogenic, causes cystic cortical lesions on CT
cocaine
psychotomimetic effect
phencyclidine/ ketamine
most dangerous hallucinogenic agent
phencyclidine
“angel dust”
phencyclidine
causes nystagmus, hypertension and seizures; tx
phencyclidine; IV diazepam/lorazepam
no actions on dopaminergic neurons unlike most drugs of abuse
phencyclidine
psychedelic effects
lysergic acid diethylamide (LSD), mescaline, psilocybin