Pharmacology Flashcards
Methylphenidate
Ritalin, Concerta
Stimulant; transporter blocker; blocks reuptake of DA and NE
dexmethylphenidate
Focalin
Stimulant; transporter blocker; blocks reuptake of DA and NE
dextroamphetamine
Dexedrine
Stimulant; Transporter reverser; reverses DA, NE transporters
lisdexamfetamine
Vyvanse
Prodrug of dextroamphetamine
Stimulant; Transporter reverser; reverses DA, NE transporters
mixed amphetamine salts
Adderall
Stimulant; Transporter reverser; reverses DA, NE transporters
atomoxetine
Non-Stimulant ADHD medication
blocks reuptake of NE only, not as effective as stimulants. Can block growth.
Carbamazepine
Anticonvulsant
Blocks Na+ channels; prevents action potentials.
Phenytoin
Anticonvulsant
Blocks Na+ channels; prevents action potentials.
Can become very toxic. Variable elimination and dosing between patients.
topiramate
Anticonvulsant
Blocks Na+ channels; prevents action potentials.
Also acts at GABAa receptors (Cl- Channels)
Can also be used for migraine prophylaxis
lamotrigine
Anticonvulsant
Blocks Na+ channels; prevents action potentials.
zonisamide
Anticonvulsant
Blocks Na+ channels; prevents action potentials.
Benzodiazepines
Anticonvulsant
Increases inhibition by acting at GABAa receptors between alpha and gamma subunits
Increases frequency of Cl- channel opening
Barbiturates
Anticonvulsant
Increases inhibition by acting at GABAa receptors at Beta subunit
Gabapentin
Anticonvulsant
GABA breakdown
Tiagabine
Anticonvulsant
Blocks GABA reuptake through Gat-1 transporter
Valproate
Anticonvulsant
Blocks Na+ channels; prevents action potentials.
Prevents GABA breakdown
Blocks T-Type Ca2+ channels
Can also be used for Migraine prophylaxis
Ethosuximide
Blocks T-Type Ca2+ channels
Used for Absence seizures
Y-hydroxybutyrate
GHB, illegal sedative
depresses CNS, interferes with memory
Rohypnol
Roofie, illegal sedative
Benzo
depresses CNS, interferes with memory
Nitrites
Poppers, Inhalant
vasodilates; used as a sexual enhancer
Phencyclidine
Psychedelic, alters sensorium
PCP; NMDA receptor antagonist
Ketamine
Psychedelic, alters sensorium
NMDA receptor antagonist
Dextromethorphan
Psychedelic, alters sensorium
NMDA receptor antagonist
Lysergic acid diethylamide
Psychedelic, alters sensorium
LSD, agonist @ 5-HT2 and 5-HT1a receptors
MDMA
Psychedelic and Psychostimulant, alters sensorium
Ecstasy, increases release of 5-HT via transporter reversal
delta-9-tetrahydrocannabinol
THC, binds to cannabinoid receptors.
Heroin
illegal opioid.
produces euphoria and sedation
activates mu opioid receptors
Morphine
produces euphoria and sedation
activates mu opioid receptors
Oxycodone
produces euphoria and sedation
activates mu opioid receptors
Cocaine
Psychostimulant
blocks reuptake of DA, NE, 5-HT
Methamphetamine
Psychostimulant
increases release of DA, NE, 5-HT via transporter reversal
Opioid Withdrawal
Nausea, vomiting, sweating, tachycardia, hypertension
Won’t actually die
Treat with Clonidine - alpha-2 receptor agonist
Treat with Methadone - long acting mu opioid receptor agonist (given in a clinic)
Treat with Buprenorphine - partial mu opioid receptor agonist (given at home) (comes as Subutex or mixed with naloxone (opioid antagonist) to prevent shooting up.
Naloxone
Opioid antagonist,
used for acute overdose
Alcohol withdrawal
Nausea, vomiting, sweating, tachycardia, seizures
can actually die.
Tx with benzos (short acting like oxazepam are best - oxazepam doesn’t need to be cleared by liver)
long term management:
Disulfuram - blocks aldehyde dehydrogenase which causes a buildup of acetaldehyde which makes you feel crappy if you drink
Acamprosate - GABA analog
Naltrexone - long acting mu opioid receptor antagonist
Varenicline
Chantix
partial agonist to nAChRs with greater affinity than nicotine
more effective than buproprion
can cause or exacerbate psychiatric problems
Sedative
Reduces anxiety
Hypnotic
Makes you sleepy
GABAa receptor agonist
Binds to GABAa receptor (specific for Cl-), increases Cl- concentration and influx which hyper polarizes the neuron
Benzos
Binds to GABAa receptor between alpha and gamma subunits
Increases frequency of Cl- channel opening
low dose = sedative
high dose = hypnotic
Also can shorten sleep latency
safer than the older barbiturates
Can block with Flumazenil
Short acting (half-life < 6 hrs) triazolam
Intermediate acting (half-life 6-24hrs) alprazolam, oxazepam, lorazepam (ativan)
Long acting (half-life >24 hrs) chlordiazepoxide, desmethyldiazepam, flurazepam, diazepam
Chlordiazepoxide
Benzo (binds between alpha and gamma subunits of GABAa receptors)
Enhances effects of GABA binding without being an agonist
Increases frequency of Cl- channel opening
Diazepam
Valium
Benzo (binds between alpha and gamma subunits of GABAa receptors)
Enhances effects of GABA binding without being an agonist
Increases frequency of Cl- channel opening
Desmethyldiazepam
Benzo (binds between alpha and gamma subunits of GABAa receptors)
Enhances effects of GABA binding without being an agonist
Increases frequency of Cl- channel opening
flurazepam
Benzo (binds between alpha and gamma subunits of GABAa receptors)
Enhances effects of GABA binding without being an agonist
Increases frequency of Cl- channel opening
triazolam
Benzo (binds between alpha and gamma subunits of GABAa receptors)
Enhances effects of GABA binding without being an agonist
Increases frequency of Cl- channel opening
alprazolam
Xanax
Benzo (binds between alpha and gamma subunits of GABAa receptors)
Enhances effects of GABA binding without being an agonist
Increases frequency of Cl- channel opening
Thiopental
Barbiturate
Binds to beta subunit of GABAa receptor and increases duration of Cl- channel opening
High doses act as agonist
Secobarbital
Barbiturate
Binds to beta subunit of GABAa receptor and increases duration of Cl- channel opening
High doses act as agonist
phenobarbital
Barbiturate
Binds to beta subunit of GABAa receptor and increases duration of Cl- channel opening
High doses act as agonist
Tolerance and Dependence of Barbs and Benzos
Benzos - down regulated binding site
Barbs - increased metabolism
Zolpidem
Shortens Sleep Latency
Ambien binds to GABAa alpha-1 subunits
Can get amnesia
rebound insomnia when coming off it
Zaleplon
Shortens Sleep Latency
binds to GABAa alpha-1 subunits
Eszopiclone
Shortens Sleep Latency
binds to GABAa alpha-1 subunits
Buspirone
Other Sedative/Hypnotic
Mostly anxiolytic
agonist of 5-HT1a and DA d2 receptors
Ramelteon
Melatonin receptor agonist
Can’t mix with fluvoxamine (SSRI)
Sumatriptan
Migraine Tx
activate 5-HT 1D/1B receptors on trigeminal nerve endings and cerebral/meningeal vessels. Also vasoconstricts
Ergotamine
Migraine Tx
activate 5-HT 1D/1B receptors on trigeminal nerve endings and cerebral/meningeal vessels. Also vasoconstricts
Timolol
Migraine Prophylaxis, beta blocker
propanolol
Migraine Prophylaxis, beta blocker
Opioid Receptors
mu, delta, kappa
g-protein coupled receptors
Opioid binding effects: analgesia euphoria sedation w/out amnesia respiratory depression cough supression miosis truncal rigidity
Morphine
Strong opioid mu agonist
heroine
illegal strong opioid mu agonist
heroine is morphine with 2 acetyl groups added on
oxymorphone
derivative of morphine
strong opioid mu agonist
hydromorphone
Dilaudid
derivative of morphine
strong opioid mu agonist
methadone
strong opioid mu agonist
used to wean people off heroine
fentanyl
short acting strong opioid mu agonist
meperidine
Demerol
strong opioid mu agonist
Also has antimuscarinic effects and blocks 5-ht reuptake
codeine
partial mu agonist
oxycodone
mild mu agonist
derivative of codeine
hydrocodone
mild mu agonist
derivative of codeine
propoxyphene
mild mu agonist
Percocet
(oxycodone + acetaminophen)
Percodan
(oxycodone + aspirin)
Vicodin/Lortab
(hydrocodone + acetaminophen)
Vicoprofen
(hydrocodone + ibuprofen)
naloxone
mu opioid receptor antagonist
naltrexone
mu opioid receptor antagonist
Nalbuphine
strong kappa agonist
mu antagonist
Buprenorphine
long acting partial mu agonist
Butorphanol
kappa agonist
partial mu agonist or antagonist
Pentazocine
kappa agonist
weak mu antagonist or partial agonist
Tramadol
Kind of like meperedine (demerol)
weak mu agonist, antimuscarinic, blocks 5-HT reuptake
Chlorpromazine
Typical antipsychotic
Phenothiazine
strong DA D2 receptor antagonist
Fluphenazine
Typical antipsychotic
Phenothiazine
strong DA D2 receptor antagonist
thioridizine
Typical antipsychotic
Phenothiazine
strong DA D2 receptor antagonist
Thiothixene
Typical antipsychotic
less potent than Phenothiazines
strong DA D2 receptor antagonist
Haloperidol
Typical antipsychotic
more potent than Phenothiazines w/ less side effects
strong DA D2 receptor antagonist
EPS
D2 blockers disrupt basal ganglia indirect vs direct pathway dopamine stimulation
leads to parkinsonian symptoms due to removal of inhibition of indirect pathway
Can result in tardive dyskinesia due to unregulated d2 receptors which causes a decrease in indirect pathway stimulation
Clozapine
Atypical antipsychotic
serotonin-dopamine antagonist
also used as a mood stabilizer
olanzapine
Atypical antipsychotic
serotonin-dopamine antagonist
also used as a mood stabilizer
quetiapine
Atypical antipsychotic
serotonin-dopamine antagonist
also used as a mood stabilizer
ziprasidone
Atypical antipsychotic
serotonin-dopamine antagonist
also used as a mood stabilizer
risperidone
Atypical antipsychotic
serotonin-dopamine antagonist
also used as a mood stabilizer
aripiprazole
Abilify
Atypical antipsychotic
serotonin-dopamine antagonist
also used as a mood stabilizer
asenapine
Atypical antipsychotic
serotonin-dopamine antagonist
also used as a mood stabilizer
Lithium
Bipolar drug
depletes PIP2 in cell membranes thus inhibiting the recycling of inositol substrates
Phenelzine
irreversible MAOI
last resort antidepressant
Tranylcypromine
long acting MAOI
last resort antidepressant
Amitripyline
Tricyclic antidepressant
breaks down to nortriptyline which can be given by itself
both block NE and 5-HT reuptake
lethal in overdose
imipramine
Tricyclic antidepressant
blocks NE and 5-HT reuptake (desipramine doesn’t block 5-HT reuptake)
breaks down to desipramine which can be given by itself
lethal in overdose
Venlafaxine
Effexor
SNRI
Desvenlafaxine
Pristique
SNRI
Duloxetine
Cymbalta
SNRI
selegeline
long acting MAOI
last resort antidepressant
St Johns Wort
reuptake inhibitor of monoamines, GABA, and glutamate
Amoxapine
Blocks NE reuptake and muscarinic receptors
Also blocks D2 receptors
Maprotiline
Blocks NE reuptake and muscarinic receptors
Mirtazapine
Antagonist @ 5-HT2, Alpha 2, and histaminergic receptors
Bupropion
blocks DA reuptake
used for smoking cessation
Trazodone
5-HT2a antagonist
Nefazodone
5-HT2a antagonist
Citalopram
SSRI
Celexa
escitalopram
Lexapro
SSRI
Fluoxetine
Prozac
SSRI
sertraline
Zoloft
SSRI
Paroxetine
Paxil
SSRI
Fluvoxamine
SSRI
Primidone
Barbiturate prodrug of Phenobarbital
Thiopental
Barbiturate IV anesthetic
fast induction due to low solubility
Midazolam
Versed
Benzo
not for full surgical anesthesia
Flumazenil to reverse benzos
Flumazenil
blocks benzos
Propofol
most popular IV anesthetic
Can induce and maintain anesthesia
etomidate
induction but need to give opioid for analgesia
ketamine
NMDA receptor antagonist (can cause dissociative effects)
Amantadine
Prevents release of infectious viral nucleic acid (influenza)
May promote dopamine release from presynaptic fibers or block reuptake of dopamine into presynaptic neurons
Benztropine
Exerts anticholinergic and antihistaminic effects; may prolong action of dopamine by inhibiting its reuptake and storage
modafinil (Provigil)
stimulant; unknown MOA
Ephedrine
Moderate beta-1 & weak alpha effects resulting in alpha- and beta- adrenergic stimulation that increase CO & BP, decrease renal perfusion & variable PVR
Pseudoephedrine
Alpha-adrenergic agonist of receptors present in respiratory mucosa, causing vasoconstriction; directly stimulates beta-adrenergic receptors and causes bronchial relaxation, as well as increased heart rate and contractility.
Phenylpropylamine
Phenylpropanolamine acts as a potent and selective releasing agent of norepinephrine and epinephrine, or as a norepinephrine releasing agent (NRA). It also acts as a dopamine releasing agent (DRA) to a lesser extent.