MNI DRUGS Flashcards
Isocarboxazid
MAO inhibitor
Phenelzine
MAO inhibitor
Tranylcypromine
MAO inhibitor
Selegiline
MAO inhibitor
Amitryptaline
TCA
Clomipramine
TCA
Desipramine
TCA
Imipramine
TCA
Nortriptyline
TCA
Citalopram
SSRI
Escitalopram
SSRI
Fluoxetine
SSRI
Fluvoxamine
SSRI
Paroxetine
SSRI
Sertraline
SSRI
Venlafaxine
SNRI
Duloxetine
SNRI
Bupropion
NDRI
Nefazodone
SARI
Trazodone
SARI
Mirtazapine
NASSA
Drug for bipolar disorder
Lithium
Alternative drug to Lithium antiepileptics
valproate and carbamazepine
Drug used for hypertension thought to increase depression. Depletes serotonin, norepinephrine and dopamine in rat brains
reserpine
Drug used for TB that is found to lift depression in chronically ill patients
Iproniazid and isoniazid
Signs of serotonin syndrome
hyperthermia, muscle rigidity, myoclonus
Treatment for serotonin syndrome
serotonin antagonist called cyproheptadine
Of the MAO inhibitors which does not react with foods?
Selegiline
What kinds of drugs are involved with depletion of tyramine break down in cheese products?
MAO inhibitors
Over the counter meds for cold contraindicated with MAOI if they contain
pseudoephedrine and phenylpropanolamine
Tricyclic antidepressant more selective for SERT
clomipramine
Tricyclic antidepressant more selective for NET
Desipramine and nortriptyline
Conduction block due to Tricyclic antidepressant can be treated with what?
Due to NA channel blockage, Arrhythmias due to this can be treated with sodium bicarbonate. which are the most common cause of death with these drugs
What is the drug of choice in treating depression?
SSRI
AE of SSRI
Excess serotonin causes GI upset, sexual dys, nausea,vomiting, serotonin syndrome when combined with MAOI
What drug is very dangerous to combine with MAOI
SSRI
What can an overdose of SSRI cause?
seizure
AE of Nefazodone
hepatotoxicity
AE of Trazadone
blocks alpha1 and H1 receptors/ very sedating, it is a hypnotic and can cause priapism.
What drugs are effected in treating depression where SSRI dont work?
SNRI- venlafaxine and duloxetine
What kinds of drug for depression inhibits norepinephrine and dopamine uptake?
bupoprion/ NDRI
What is the only drug not associated with sexual dysfunction
NDRI, bupoprion
AE of Bupoprion when overdosed?
seizures
What kind of drug is useful in a depressed patient with insomnia and agitation?
NASSA/ mirtazapine
What are the AE of mirtazapine
weight gain and sedation
antidepressant discontinuation syndrome can occur in drugs with short half lives what are these?
paroxitine (SSRI)
Venlafaxine (SNRI)
Antidepressant discontinuation syndrome is less likely in drugs with long half life such as…
fluoxetine (SSRI)
what enzyme does lithium inhibit?
inositol polyphosphatase and monophosphatase, blocks PIP2
AE of lithium
hypothyroidism, weight gain, nephrogenic diabetes insipidus, edema, dermatitis, alopecia, leukocytosis, can increase congenital anomalies in new borns,
What treats nephrogenic diabetes insipidus in patients on lithium?
amiloride, thiazides and NSAIDS
What is the DOC for Generalized anxiety?
antidepressants SSRI if not then SNRI ( venlafaxine is next), and TCA ( if didnt respond to other two)
What anxiety disorder can Benzos not be used alone for?
PTSD or OCD
How long does it take for antidepressants to work for GAD?
4-6 weeks, as a result you can give benzodiazepine in unison tapered.
What drug is used for acute management of GAD?
Benzodiazepines
Drug that acts as a second line for GAD does not cause dependacy/ withdrawal no alcohol potentiation or sedative hypnotic effects/ no psychomotor impairment, no dependency
Only used as anxiolytic
Buspirone
What are the DOC for panic disorders?
SSRI> TCA>MAOI
What is used to reduce an acute panic attack?
either Benzodiazepine alone or +SSRI
If patient has cormorbid depression plus panic disorder what is the rule?
only give an SSRI
In a patient with panic disorder what drug can cause rebound anxiety between doses and can cause withdrawal including seizures?
Alprazolam
what is the DOC for social anxiety?
SSRI
How long do SSRIs take to work in patients with social anxiety?
8-12 weeks
What are the DOC for OCD?
clomipramine, fluoxetine, fluoxamine, paroxetine, sertraline
If a patient with OCD has increased anxiousness what do you give plus their normal med?
benzodiazepine
DOC for PTSD?
SSRI ( sertraline)…. venlafaxine, MAOI and TCA work but bad effects.
What drugs do you give for acute treatment of PTSD?
sertraline and paroxitine
what treats performance anxiety?
propranolol/naldolol AE-hypotension
Overactivity of the mesolimbic pathway can cause
positive symptoms (midbrain to limbic system)
What decreases positive symptoms?
blockade of D2 in mesolimbic pathway.
Underactivity of the mesocortical pathway can cause
negative symptoms/ and cognitive symptoms ( blockade of D2 causes this).
projects from midbrain to prefrontal cortex
What pathway is associated with prolactin secretion?
Tuberoinfundibular:
projects from hypothalamus to anterior pituitary
dopamine released here inhibits prolactin
blocked dopamine ( increases prolactin)= galactorrhea
Blockade of D2 in the nigrostriatal pathway leads to
movement disorders/ extrapyramidal rxns
this is from substantial nigra to basal ganglia.
GABA’s primary directive is to fine tune
movement
5HT2 receptor stimulation causes
hallucinations
LSD and Mescaline are
5HT2 agonists that cause hallucinations
What are the classical antipsychotic drugs
Chlorpromazine, fluphenazine, haloperidol, thioridazine
What is the only classical antipsychotic drug that does not have “ zine”
haloperidol
What are the atypical antipsychotic drugs?
clozapine, respiradone, olanzapine, quetiapine, aripiprazole
what is the only drug of the atypical antipsychotics that doesn’t end in done or pine?
aripiprazole
What are the high potency antipsychotic drugs?
fluphenazine, haloperidol
What are the low potency antipsychotic drugs?
chlorpromazine and thioridazine
What is the job of classical antipsychotics?
they block the mesolimbic pathway ( block D2 receptors) to lessen + symptoms
What class of drugs treats negative psychotic symptoms ?
atypical antipsychotics
What is the job of atypical antipsychotics?
block multiple receptors and relieve of negative symptoms via the mesocortical pathway.
What are the receptors that clozapine has a high affinity for?
D1,D4, 5Ht2, muscarinic and alpha adrenergic receptors, also a D2 blocker
What atypical antipsychotic is more like to have EPR?
respiradone
What atypical antipsychotic is considered a partial agonist at D2 and 5HT1A receptor , but antagonist at 5HT2A?
Aripiprazole
The onset of an antipsychotic is how long? aka how long does it take to work?
less than 24 hours
Most antipsychotics are antiemetic except
aripiprazole and thioridazine
What antipsychotics experience the most extrapyramidal reactions?
the high D2 potency ones like Fluphenazine and Haloperidol (FHP).
What drugs are less likely to cause EPRs?
drugs with high anticholinergic activity like chlorpromazine and thioridazine and the atypicals
What are the EPRS?
Parkinsonism, dystonia, akathisia, tardive dyskynesia
What can treat Parkinsonism?
antimuscarinics such as benztropine and trihexyphenidyl, with diphenhydramine or amantadine NO LEVODOPA
what can treat dystonia ( involuntary muscle contractions)?
Treated with benztropine, trihexyphenidyl, diphenhydramine
What can treat Akathisia ( need to be in constant motion?
first change dosage of antipsychotic or the actual drug, clonazepam or propranolol
What can treat Tardive Diskynesia ? ( facial tics, late occurring choreoatheroid movements)
first change dosage of antipsychotic or the actual drug, tetrabenazine or valbenazine they inhibit VMAT
can also use Benzos…
For patiesnt who require antipsychotics and have tardive diskynesia what do you give ?
clozapine
Sedation is an AE of what kind of antipsychotic?
low potency classical or atypical drug
What clinically characterizes Neuroleptic Malignant Syndrome an AE of antipsychotics ?
Rare, life threatening rigidity, tremor, hyperthermia, altered mental status, autonomic instability, increased WBC, increased CK and myoglobinemia with potential nephrotoxicity. myoglobinemia is usually what kills people
What treats Neuroleptic malignant syndrome?
Dantrolene and bromocriptine
What is the AE of clozapine?
causes agranulocytosis
what drug causes a high incidence of QTc and T wave changes and rarely produce ventricular arrhythmias and sudden death?
thioridazine
Patient is female and has amenorrhea, galactorrhea syndrome and infertility what kind of antipsychotic drug is this patient most likely taking?
classical antipsychotic
Male has loss of libido, fertility and potency what antipsychotic drug is he likely taking?
a classical antipsychotic
What antipsychotic drug causes deposits in cornea and lens?
chlorpromazine
what antipsychotic drug causes retinal deposits?
thioridazine
What kind of antipsychotic drugs have the most metabolic effects such as type 2 diabetes, weight gain, hypertension, hyperlipidemia?
atypical agents… on chart aripiprazole had this the least
what are non-psychiatric reasons to take an antipsychotic?
nausea and vomiting, combined with fentanyl in neuroleptic anesthesia
Which involves more CNS effects? hypnosis or sedation?
hypnosis
Gaba is a ______ neurotransmitter of the CNS?
inhibitory
Where does GABA bind to on the Gaba receptor?
between alpha and beta subunits
Where do Benzodiazepines bind on the Gaba receptor?
between alpha and gamma subunits (BZ1 and BZ2)
What forms of anxiolytic drugs are positive allosteric modulators of GABA A receptors?
They increase GABA and increase CL
Benzodiazepines, Barbiturates, and Non-Benzodiazepine benzodiazepine receptor agonists= Z drugs
What are the functions of benzodiazepines ?
they reduce anxiety, sedative and hypnotic, anticonvulsant, and muscle relaxant
What is the onset for benzodiazepines?
30 min to an hour, because they are lipophillic and completely absorbed
Cl channels open more FREQUENTLY IN what allosteric modulator of Gaba A receptors?
Benzodiazepines
Cl channels open for more DURATION in what allosteric modulator of Gaba A receptors?
Barbiturates
What are the Long acting benzodiazepines?
FCD ALOT MT
FCD: Flurazepam, Clonazepam, Diazepam,
What are the intermediate acting Benzodiazepines?
ALOT: Alprazolam, Lorazepam, Oxazepam, Temazepam
What are the short acting Benzodiazepines?
MT: Midazolam, Triazolam
Benzodiazepines and Barbiturates are ________ dependent
dose
Most Benzos undergo phase I reactions by
CYP3A4 they are later conjugated into glucoronides and urinated.
_______is an active metabolite of clinical Benzos and is metabolized to oxazepam
Desmethyldiazepam
What benzodiazepine drugs are conjugated directly and not metabolized by P450 system?
Lorazepam, Oxazepam, Temazepam (LOT)
What benzodiazepine has a half life of 30-100 hours ?
Flurazepam ( long acting) and is metabolize by the liver.
What Benzodiazepine/ anxiolytic drug can treat skeletal muscle spasms, spacity from degenerative disorders like MS and cerebral palsy?
diazepam
What anxiolytic drug/ Benzodiazepine can treat most seizures?
clonazepam
what anxiolytic drug/ Benzodiazepine can treat status epilipticus ?
Midazolam, lorazepam, diazepam
What is the DOC for alcohol withdrawal?
Benzodiazepines
What anxiolytic drug/ Benzodiazepine can treat sleep disorders?
Temazepam- intermediate acting
triazolam- short acting
What are the adverse effects of Benzodiazepines?
Drowsiness and confusion, ataxia, cognitive impairment, psych effects: ( paradoxical/anxiety), irritability, hostility, rage, paranoia, depression, suicidal ideation, dependence ( no coma or death)
what is withdrawal like after benzodiazepines?
confusion, anxiety, agitation, restlessness, insomnia, tension
Name a Benzodiazepine antagonist
Flumazenil
Flumazenil can block the effects of what drugs?
benzodiazepines and Z drugs: reverses the CNS depressant effects of Benzo overdose also for recovery of benzodiazepines as an anesthetic. This drug can precipitate withdrawals and cause seizures
If flumazenil is not working on Benzo overdose patient, what do you do?
apply more drug because it has a short half life
What is the MOA of barbiturates?
activates CL independent of GABA, they block glutamate receptors and inhibit voltage gated sodium and calcium channels. this is the reason for their general anesthetic and CNS depression effects…
1- sedation/hypnosis 2- anesthesia 3- depress respirations and suppress hypoxic chemoreceptor response to CO2= death
what are the AE of Barbiturates?
Drowsiness, impaired concentration, paradoxical excitement, hypersensitivity, hang over, pulmonary depression, worsened pain perception, dependence withdrawal and poisoning to CV and resp
What drugs are the Non-Benzodiazepine Benzodiazepine receptor agonists?
Z drugs: zolpidem, Zaleplon, Eszoplicon
What drug is only approved as a hypnotic and only acts on BZ1 receptor subtype, no muscle relaxing, or anticonvulsant effects… ?
Z drugs
what Z drug is used for short term treatment of insomnia characterized by issues of sleep onset?
Zolpidem ( short acting)
Which is an ultrashort acting Z drug?
zaleplon
which z drug as the shortest half life?
zaleplon ( 20 min) others are 30 min
What drug is a 5HT1A partial agonist?
buspirone
What drug has no hypnotic, anticonvulsant or muscle relaxant properties, it is ONLY an ANXIOLYTIC?
Buspirone
What is the onset time for buspirone?
2-3 weeks
What drug is a melatonin agonist (MT1 and MT2)?
Ramelteon
what does Ramelteon treat?
insomnia with difficulties at sleep onset. can be given long term.
What are the AE of Ramelteon?
dizziness, somnolence, fatigue, endocrine changes, decrease in testosterone, increase in prolactin
What drugs are Orexin receptor antagonist?
Suvorexant, and Lemborexant
What do Orexin A and B do?
promote wakefulness by activating the OX1 and OX2 receptors.
What is the function of Suvorexant/ Lemborexant ( Orexin Receptor antagonists)?
treat insomnia, promote sleepiness in onset or maintenance
Adverse effects of Orexin receptor antagonist ?
daytime somnolence and worsening of depression, suicidal ideation.. contraindicated in narcolepsy
A TCA used to treat insomnia characterized by sleep maintenance. The antagonist of the H1 receptor is responsible for the sedation.
Doxepin
Antihistamine with antiemetic activity approved for symptomatic relief of anxiety
hydroxazine
Nonprescription antihistamine with sedating properties used to treat mild types of insomnia
diphenhydramine and doxylamine
What treats tyramine induced hypertension ?
phentolamine and prazosin
What is the clinical presentation for the Cheese Reaction?
tachycardia, seizures, stroke, arrhythmias and hypertension
What are the main clinical effects of Parkinson’s ?
Resting Tremor, Muscular Rigidity, Bradykinesia, Gait imparment
what amino acid does Dopamine comes from_______
tyrosine
In Parkinson there is a loss of neurons in ______ pathway
the dopaminergic nigrostriatal pathway
D1 receptors ________ adenylyl cyclase
increases
D2 receptors ______ adenylyl cyclase, ____ K conductance, ______ Ca conductance
decrease, increase, decrease
most anti-parkinson drugs work at the D2 receptors
This drug for Parkinsons restores dopamine levels in the extrapyramidal centers. It uses residual dopaminergic neurons during early disease from substantia nigra….
Levodopa
Levodopa crosses the BBB what enzyme turns it into dopamine there?
Dopa decarboxylase
______ delays appearance of levodopa in plasma
food
When Levodopa is converted by dopa decarboxylase at the periphery, what are the AE?
nausea, vomiting, cardiac arrythmias hypotension
What Parkinson’s drug is a Dopa decarboxylase inhibitor?
Carbidopa
What is the function of carbidopa?
given simultaneously to levodopa, increases availability of levodopa to CNS by decreasing metabolism of it in GI tract and peripheral tissues.
Sinemet
Levodopa plus carbidopa
When does the Sinemet ( levodopa+ carbidopa) combo decline in response?
during 3rd to 5th year of therapy. this concoction does not stop the progression of PD
What are the contraindications of Levodopa?
Vit B6 ( cofactor for dopa decarboxylase which will increase peripheral metabolism), nonspecific MAOI can present hypertensive crisis, psychotic patients, people with angle closure glaucoma, cardiac patients at risk of arrythmias, Avoid taking antipsychotics, admin with hypertensive will increase risk of orthostatic hypotension, active peptic ulcer due to risk of GI bleeding on levodopa
What is the ergot dopamine agonist for Parkinson’s?
Bromocriptine, a D2 agonist that is barely used
_________ drugs do not depend on nigrostriatal neurons, and dont need enzymatic conversion for activity
dopamine receptor agonists
What are the non-Ergot dopamine agonists for PD?
pramipexole, Ropinirole, Rotigotine
What drugs are commonly used for initial treatment of younger patients with PD?
Non-ergot dopamine agonist, pramipexole, and ropinirole
These are less effective in treating motor symptoms of PD, they are less likely to cause motor fluctuations or dyskinesia
What Parkinson drug is transdermal once daily use?
Rotigotine
What is a common side of effect of Dopamine receptor antagonist?
compulsive behaviors (ICD)
What Parkinson drugs will cause nasal congestion, headache, increased arousal, pulmonary infiltrations, pleural and retroperitoneal fibrosis and erythromelalgia?
Bromocriptine/ ergot dopamine agonist
what are the AE of the non-ergot dopamine agonists?
uncontrollable somnolence.
What are the contraindications of dopamine receptor agonists?
antipsychotics, CNS depressants ( increase risk of somnolence and confusion), psychotic illness, recent MI, active peptic ulcer.
What drug is used as rescue therapy and is a non-ergot dopamine agonist? what drug must be used together with it and why?
apomorphine is an emetogenic, and you need an anti- emetic together with it like trimethobenzamide
Drug used for rescue therapy treatment of off episodes of akinesia on patients on dopaminergic therapy
apomorphine
What are the AE of apomorphine
Qt prolongation, dyskinesia, drowsiness, sweating, hypotension
What are the inhibitors of dopamine metabolism?
MAO I and COMT I
what are the two MAO I used in the treatment of PD?
selegiline and rasagiline
this drug selectively and irreversible inhibits MAOB ( which metabolizes dopamine) it slows breakdown of dopamine in the brain and can get you to lower the levodopa dose, it enhances the effects of levodopa, used as an adjunct to levodopa
Selegiline
what PD drug is metabolized to methamphetamine and Beta amphetamine?
selegiline
If you take selegiline for PD and you tae it too late in the day what may happen?
insomnia
What MAOB inhibitor is approved for PD besides selegiline?
rasagiline
MAO-B inhibitor drug plus serotonergic drug can cause what?
serotonin syndrome and hypertensive crisis if taken within 14 days together
Concomitant use of MAO B and sympathomimetic can cause…?
severe hypertension
When dopa decarboxylase is inhibited what is increased ?
3-0-methyldopa which competes with levodopa for a carrier that transports across intestinal mucosa and BBB
Tolcapone and entacapone are _________
COMT inhibitors
What is the action of COMT inhibitors?
inhibit comt, allow for decreased metabolism of levodopa and decreased of 3-o methyldopa, increases uptake of levodopa, and increases dopamine levels in the Brain
What is the AE Tolcapone?
Fulminating hepatic necrosis
Does tolcapone or entacapone cross BBB?
Tolcapone does, for this reason entacapone is preferred drug because it is only at the periphery. this drug is concocted with levodopa and carbidopa and sold as fixed dose.
An antiviral drug used for PD that may increase dopamine release and inhibit dopamine reuptake
amantadine
What Parkinson Drug is a NDMA antagonist?
Amantadine
what are the AE if amantadine?
restlessness, confusion agitation, hallucination, ACUTE TOXIC PSYCHOSIS, peripheral edema, orthostatic hypotension, HF
Use with caution with patient with hx of seizure and HF.
What drug has a risk of Livedo reticularis?
Amantadine
What antimuscarinc drugs can be used in PD to treat tremor and rigidity?
Benztropine and trihexyphenidyl.
- also work for drooling
these drugs have sympathetic AE.
Who is contraindicated with antimuscarinic drugs like benztropine and trihexyphenidl for PD?
glaucoma pts, prostatic hypertrophy, pyloric stenosis.
The excessive self administration of any substance for nonmedical purposes
abuse , hallucinogens are drugs of abuse that do not lead to addiction
impaired control over drug use, compulsive use, continued use despite harm
addiction
What can cause drug withdrawal?
Abrupt cessation, rapid dose reduction, admin of antagonist
What is the prime target of addictive drugs?
mesolimbic dopamine system
Drugs that inhibit Gaba and as a result increase dopamine are
Opioids, Cannabinoids, benzodiazepines, ethanol
Drugs that directly stimulate dopaminergic neurons
nicotine and ethanol
Drugs that block or reverse DAT
cocaine, amphetamines, MDMA
What are the CNS depressants?
ethanol, benzodiazepines, barbiturates
Whaty does ethanol cause that makes it a depressant?
it produces sedation and sleep
Channels influenced by alcohol
Gabaa receptor, Kir3/ GIRK channels, Adenosine reuptake, Glycine receptors, NMDA receptors, 5HT3 receptors
Withdrawal associated with tremor, nausea, vomiting, sweating agitation and anxiety followed by hallucinations and seizures 24-48 hours later and then DELIRIUM TREMENS 48-72 hours later. Characterizes withdrawal from what substance?
ethanol
How many hours till delirium tremens kicks in in an alcoholic?
48-72 hours
What are the agents used to treat alcohol WITHDRAWAL?
long acting benzo, Diazepam and chlordiazepoxide
If you have an elderly patient undergoing withdrawal from alcohol or someone with liver failure what would you prescribe?
intermediate acting benzo lorazepam and oxazepam
What drugs are used to treat alcohol addiction?
Disulfram, naltrexone, acamprostate
What drug is an inhibitor of aldehyde dehydrogenase?
disulfiram. It creates an aversion to drinking.
doesnt allow for conversion of atetalaldehyde to acetate
PT takes a tablet that gives them an aversion to alcohol because they experience nausea, headache, flushing, and hypotension as a result of it. what drug is it?
disulfiram
What drug that is a treatment of alcohol addiction is considered an opioid antagonist?
naltrexone
it antagonizes the release of U receptor from the endogenous opioids set out by alcohol that releases dopamine
what drug reduces cravings for alcohol and decreases relapse to heavy drinking?
naltrexone
What alcohol treatment drug works by blocking a hyperglutamatergic state in the alcoholic brain?
acamprostate
what drug of alcohol treatment of addiction is an NMDA receptor antagonist?
acamprostate, it prevents relapse of drinking
what treatment of alcohol addiction prevents relapse drinking?
acamprostate
What drug facilitates Gaba function in alcohol addiction, antagonizes glutamate and may reduce cravings but is not approved by the FDA?
Topiramate
Withdrawal of what drug causes tremors, anxiety, perceptual disturbances, dysphoria, psychosis, and seizures? can be life threatening
Benzodiazepines
How do you manage withdrawal of benzodiazepine?
if the pt is on a short acting drug, you give them a long acting drug. Diazepam is the most used, then the dose is gradually reduced
What are the psychostimulants?
methylxanthines, cocaine, ampthetamines
Methylxanthines include:
Caffeine, theophylline, and theobromine
What is the mechanism of Methylxanthines (ex caffeine) ?
Block presynaptic adenosine receptors
activation of adenosine receptors inhibits norepinephrine release, blocking them increases norepinephrine
100-200 mg of coffee/ 1-2 cups per day
decrease in fatigue and increased mental alertness
1.5g 12-15 cups of coffee
anxiety and tremors
2-5g of caffeine
spinal cord stimulated
What is the withdrawal effect of methylxanthines?
fatigue and sedation.
Cocaine and amphetamines are considered schedule ______ drugs by DEA
II
_______ inhibits dopamine, norepinephrine and serotonin reuptake
cocaine
what causes the euphoria of cocaine
prolongation of dopaminergic effects in the brains limbic system
This drug acts by stimulating the cortex and brainstorm. It increases mental awareness and produces a feeling of well being and euphoria. Paranoia occurs after repeated doses.
At high doses: tremors, convulsions, followed by respiratory and vasomotor depression
Cocaine
What drug potentiates adrenergic stimulation peripherally ?
Cocaine
Patient undergoes withdrawal from a drug and has the following symptoms: dysphoria, depression, sleepiness, fatigue, craving the drug, bradycardia,
Cocaine
What drugs have been tested as treatment for cocaine abuse ?
Antidepressants and dopamine agonists: none have demonstrated clear efficacy
This drug increases release of catecholamines, are weak inhibitors of MAO, and are direct catechilaminergic agonists in the brain
Amphetamines
Amphetamines are taken up into neurons by _______. Once in the neuron, amphetamines interfere with _____ depleting synaptic vesicles
amine transporters.
VMAT
Levels of dopamine in the cytoplasm increase and are released into the synapse by reversal of the DAT.
What are the uses of amphetamine?
attention deficit syndrome ( amphetamine and methylphenidate), narcolepsy ( amphetamine and methylphenidate)
What drug experiences these withdrawal signs? increased appetite, sleepiness, exhaustion, and mental depression
Amphetamines and antidepressants are given
Amphetamine normally causes
increased alertness, decreased fatigue, depressed appetite and insomnia
The rewarding effects of nicotine requires involvement of the ____________ area where nicotinic receptors are expressed on dopamine neurons
ventral tegmental area
what drug is a full agonist of the nicotine receptor?
nicotine
IN low doses what does nicotine cause?
ganglionic stimulation by depolarization- causes euphoria and relaxation, improves attention learning, problem solving and reaction time
in high doses what does nicotine cause?
ganglionic blockade- central respiratory paralysis and severe hypotension caused by medullary paralysis
nicotine is an appetite suppressant
What does nicotine withdrawal consist of?
irritability and sleepiness
what drug is a partial agonist at nicotinic receptors in the CNS and reduces the reward of smoking?
Varenicline and buproprion
what are the opioid drugs?
heroin, morphine, codeine, oxycodone
Patient is withdrawing like this: dysphoria, lacrimation, rhinorrhea, and yawning. What drug was it?
opioid… the withdrawal is actually not life threatening
How do you treat opioid withdrawal with the use of an opioid agonist? what drugs are used?
you give an opioid agonist and slowly reduce it.
Methadone and buprenorphine
What drug is useful for detoxification and maintenance of the chronic relapsing heroin addict?
methadone
How do you treat opioid withdrawal with the use of an opioid antagonist? what drugs are used?
Naltrexone…. high affinity for u opioid receptor. this drug will not satisfy a craving or relieve the withdrawal symptoms. Naltrexone can be used after detox for patient with high motivation to remain opioid free
Marijuana has two receptor subtypes CB1 and CB2. both are G protein linked receptors and couple to Gi. where are each found?
CB1- in the brain and mediate psychological effects of THC ( receptor at Gabaergic neurons in the ventral tegmental area)
CB2- present mainly on immune cells
Binding of THC to CB1 receptors ______ gaba release
decreases…. this decrease of Gaba release disinhibits dopaminergic neurons resulting in increased dopamine release
What drug can produce euphoria, followed by drowsiness and relaxation. affects the short term memory and mental activity. causes impairment of highly skilled motor activity.
other: appetite stimulation, xerostomia, visual hallucinations, delusions, enhancement of sensory activity. At high doses- toxic psychosis
marijuana
what occurs at high doses of marijuana?
toxic psychosis
what are the 3 cannabinoids approved by the FDA for medical use?
nabilone, dronabinol, Cannabidiol (CBD)
Dronabinol is the synthetic form of THC.
Nabilone is a synthetic derivative of THC.
What form of marijuana is approved for nausea and vomiting associated with cancer chemotherapy in patients who have failed to respond to conventional antiemetic treatments ?
Dronabinol and nabilone
What Marijuana based drug is approved for anorexia associated with weight loss in patients with AIDS?
Dronabinol
What marijuana based product is approved for the treatment of seizures associated with Lennox-Gastaut syndrome, Dravet syndrome, or tuberous sclerosis complex
CBD
What are the psychedelic agents?
LSD, Mescaline, Psilocybin, Phenciclidine, MDMA
What drugs affect thought, perception and mood and do not cause marked psychomotor stimulation or depression?
psychedelic agents