Exam 1 Drug, classes etc Flashcards
Amitriptyline (Elavil)
TCA: tertiary amine
- blocks reuptake of 5HT, NE
- also blocks a adrenergic, Histamine and Muscarinic R
- depression, TMJ, fibromyalgia, enuresis
Imipramine (Tofranil)
TCA: tertiary amine
- inhibits reuptake of 5HT, NE
- also blocks a adrenergic, Histamin, and Muscarinic R
- depression, TMJ, fibromyalgia, enuresis
Nortriptyline (Pamelor)
TCA: secondary amine
- inhibits reuptake primarily of NE
- also blocks a adrenergic, Histamine and Muscarinic R
- depression, TMJ, fibromyalgia, enuresis
Despiramine (Norpramin)
TCA: secondary amine
*blocks reuptake primarily of NE
Fluoxetine (Prozac)*
SSRI: selectively inhibits 5-HT reuptake
*Depression, mosty likely to inhibit CYP450 - 2D6, 3A4
Sertraline (Zoloft)
SSRI: selectively inhibits 5-HT reuptake
*depression, preferred in elderly bc least likely to interact w/ drug
Citalopram (Celexa)
SSRI: selectively inhibits 5-HT reuptake
current DOC for depression
Venlafaxine (Effexor)
SNRI: inhibit NE and 5-HT reuptake
- depression, neuropathic pain, postmenopausal hot flashes
- may increase BP, cardiac toxicity
Duloxetine (Cymbalta)
SNRI: inhibits NE and 5-HT reuptake
- depression, neuropathic pain, post meno hot flashes
- may cause hepatotoxicity
Phenelzine (Nardil)
MAOI: irreversibly inhibits MAOs which metabolize NE, DA, 5-HT
*inhibits both MAO-A and MAO-B, increases NE, 5-HT and DA
drug of LAST CHOICE for depression
Selegiline (Deprenyl)
MAOI: selectively inhibits MAO-B, increases DA
- used for depression which doesn’t respond to other drugs
- also used for Parkinsons
- fewer SE
Bupropion (wellbutrin)
Preferentially inhibits DA reuptake
- sometimes used with SSRI
- ADHD, alcoholism (decreases craving), extended release for smoking cessation (Zyban)
Mirtazapine (Remeron)
NaSSA: noreadrenergic and specific serotonergic antidepressant
*blocks presynaptic a2, increases release of NE and 5-HT, blocks 5-HT2a and 5-HT3 receptors
Atomoxetine (Strattera)
Selective inhibitor of NE reuptake
- first non stimulant for ADHD tx
- may increase memory and attention; some antipsychotic properties (DA D2 antag)
- typ drug of last choice for depression
Trazodone (Desyrel)
5-HT2a receptor antagonist
- antianxiety, antipsychotic, antidepressant, sedating effects
- MOST COMMON USE is off label HYPNOTIC or SLEEP aid
- also used for pain mgmt
St Johns Wort (hpericin)
uncertain MOA
- may be effective in mild depression
- do not comb with other antidepressants –> serotonin syndrome
Chlorpromazine (Thorazine)
Classical antipsychotic: blocks DA D2 receptors
*use for psychosis associated with mania and drugs of abuse, antiemetic (prochlorperazine), pre-anesthetic
Fluphenazine (Prolixin)
Classical antipsychotic: selective for DA D2 receptors
- used for psychosis associated with mania and drugs of abuse, pre-anesthetic
- less antichol activity than Chlorpromazine thus more EPS
Haloperidol (Haldol)
Classical antipsychotic: potent DA D2 receptor blocker “Vit H”
- also affinity for DA D1, 5-HT2 and a1 receptors
- used in acute situations (inj), no antichol acitivity so lots of EPS
Clozapine (Clozaril)
Atypical antipsychotic: Blocks 5-HT2a and DA D4 receptors, some DA D2
- alleviate +/- sx
- Drug of last choice due to Agranulocytosis (monitor CBC)
Olanzapine (Zyprexa)
Atypical Antipsychotic: Blocks 5-HT2a, DA D4 and D2 receptors
- improves +/- sx
- similar to clozapine but no agranulocytosis
- also used for bipolar
Risperidone (Risperdal)
atypical antipsychotic: blocks 5-HT2a and DA D2 receptors
- improves +/- sx
- no sig effect on DA in nigrostriatal pathway (thus EPS &TD sx rare)
- FIRST LINE DRUG psychosis
Ziprisadone (Geodon)
Atypical Antipsychotic: Blocks DA D2 and 5HT-2a receptors
- some antidepressant activity (5-HT1a receptor agonist, inhibition of 5-HT reuptake)
- used for Tourettes, acute mania
- SE: prolong QTI, sedation, hyperPRL, lowers seizure threshold
Quetiapine (seroquel)
Atypical antipsychotic:*blocks 5-HT2a and DA D2 receptors
- Similar to clozapine, no agranulocytosis, no PRL
- used to promote sleep onset and maintenance, SEDATING
Aripriprazole (abilify)
Atypical antipsychotic: DA system stabilizer (activates DA receptors if DA tone low, blocks receptors if tone high)
- Partial agonsit for DA D2 and 5-HT1a, antagonist for 5-HT2a
- depression and schizophrenia
Lithium, anticonvulsants and antipsychotics (Olanzapine) combined for
bipolar disorder
Lithium Li
Mood stabilizer: No metabolism,
Suppresses 2nd messengers (IP3), may increase ACh, NE and DA
*60% success at calming effect in manic pt
*small therapeutic window, toxicity, hyponatremia, hypothyroidism, diabetes insipidus, preg cat
Valproic acid (depakene)
Anticonvulsant with antidepressants uses: Unknown antipsychotic MOA (for anticonvulsant, blocks Na channels, increases syn and levels of GABA)
- used for rapid cycling manic/depressive phases
- effective in pt who do not respond to lithium
*as anticonvulsant: used for absence or generalized tonic clonic seizures (DOC if both present)
Gabapentin (Neurontin)
Anticonvulsant with mood stabilizing uses: GABA analogue
- used for rapid cycling in bipolar
- as anticonvulsant used as supplemental tx for partial seizures and gen tonic-clonic; also for neuropathic pain
Carbamazepine (Tegretol)
Anticonvulsant with mood stabilizing uses: inhibits Na channels and decreases transmitter release
- DOC partial seizures; also used for gen tonic clonic
- REFRACTORY bipolar in combo with Lithium
Lamotrigine (Lamictal)
Anticonvulsant with mood stabilizing uses: Inactivates voltage dependent Na channels
- used for absense seizures
- Approved for prevention of relapse, depressive state following mania and acute mania
Naltrexone (ReVia)
Opioid R antagonist
Blocks ability of alcohol to stim reward pathway
Acamprostate (Campral EC)
Structural Analogues of Gaba
Restores normal balance of GABA and glutamate to increase abstinence in alcoholism
Disulfaram (Antabuse)
Inhiits aldehyde dehyrdogenase (help tx alcoholism) but acetaldehyde build up = dangerous)
Fomepizole (antizole)
Alcohol dehydrogenase inhibitor
- used to treat Methanol poisoning
- note that ethanol can also be used
Chloral Hydrate (Noctec)
Sedative hypnotic
- converted to trichloroethanol which causes sedation, acts similarly to Barbs on GABA recetpor
- ped dental procedure and nursing homes, cheap, low MOS
Pentobarbital (Nembutal Na)
Barbiturate: (sedative hypnotic)
- Binds to GABAa R and increases duration of GABA action, prolongs opening of Cl channels to produce inhibition independent of GABA (no ceiling)
- marked CNS depression/hypnosis; euphoria
Phenobarbital (Luminal)
Barbiturate - long acting: (sedative hypnotic and anticonvulsant)
- binds GABA a receptor and prolongs opening of Cl channels to produce inhibition independent of GABA (no ceiling)
- marked CNS depression/hypnosis; cuphoria
Secobarbital (Seconal)
Barbiturate (sedative hypnotic)
- binds GABAa R to increase duration of GABA action, prolongs opening of Cl channels to produce inhibition independent of GABA (no celing)
- CNS depression/hypnosis; euphorai
Thiopental (Pentothal)
Babitruate (sedative hypnotic)
- binds GABAa R to increase duration of GABA action, prolongs opening of Cl channels to produce inhibition independent of GABA (no ceiling)
- *ultra short acting barb used for induction of anesthesia)
Diazepam (Valium)
BZ - long acting 75 hr combined t1/2(sedative hypnotic, anticonvulsant)
- Diazepam (43h) - dismethyldiazepam (24) to Oxazepam (8h)
- Bind specific site on GABA receptor to prolong action of GABA
- used to prevent alcohol withdrawal seizures and DT (same with chlorodiazepoxide)
- standard tx for anxiety, DOC epilepsy, tx of muscle spasm, withdrawal from BARB
Flurazepam (Dalmane)
BZ (long action metabolites, 74hr half life)
*Commonly used as hypnotics for INSOMNIA (less depression of REM sleep than Barbs)
Midazolam (Versed)
BZ short acting, bind site on GABA receptor to prolong action of GABA (sedative hypnotic)
*Commonly used in prep for anesthesia for short surg procedures given IV (anterograde amnesia),
Temazepam (Restoril)
BZ, bind site on GABA receptor to prolong action of GABA (sedative hypnotic)
- commonly used as hypnotic for INSOMNIA
- less depression of REM than barbs,
Alprazolam (Xanax)
BZ, bind site on GABA r to prolong action of GABA (anxiolytic, sedative-hypnotic)
*short action (<6hr) converted to short acting metabolites
Lorazepam (Ativan)
BZ, bind site on GABA r to prolong action of GABA (sedative hypnotic, anticonvulsant)
- half life 6-24 hr, conjugated to INACTIVE metabolites
- longer acting used to provide tapered withdrawal from alcohol and barbs; used to tx seizures from withdrawal
- 2nd line epilepsy
Flumazinel (Mazicon)
BZ antagonist
- competes with BZ for GABA R
- DOA 30 min, reverse CNS depressant effects and effect of Midzaolam
- also reverses Z drugs
- triggers withdrawal and seizures in pt physically dependent on BZd
Zolpidem (ambien)
Bind BZ1 of GABA R
- strong and rapid sedative activity, high MOS
- sleep relate behaviors, rebound insomnia
Zaleplon (sonata)
Bind BZ1 subtype of GABA R, increase GABA
- very strong, rapid sedation, high MOS
- sleep related behaviors, rebound insomnia
Eszopiclone (lunesta)
Bind BZ1 subtype of GABA R, increase GAB
*Very strong and rapid sedation
*high MOS and approved for long term insomnia?
longer half life of 6 hr compared to others (withdrawal if abrupt cessation –> rebound insomnia)
Ramelteon (Rozerem)
Melatonin analogue
*resets sleep-wake cycle (promotes sleep indep of GABA); additive sedation with ETOH and other sedative hypnotics
Buspirone (BuSpar)
Partial agonist at 5HT1a serotonin R to DECREASE release of serotonin and increase activity of NE and DA –> anxiolytic effects in 2 wk
- very low addiction potential, good for anxiety in recovering addicts
- GAD, anxiety with depression, PMS, ADHD
