Exam 1 Drug, classes etc Flashcards

1
Q

Amitriptyline (Elavil)

A

TCA: tertiary amine

  • blocks reuptake of 5HT, NE
  • also blocks a adrenergic, Histamine and Muscarinic R
  • depression, TMJ, fibromyalgia, enuresis
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2
Q

Imipramine (Tofranil)

A

TCA: tertiary amine

  • inhibits reuptake of 5HT, NE
  • also blocks a adrenergic, Histamin, and Muscarinic R
  • depression, TMJ, fibromyalgia, enuresis
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3
Q

Nortriptyline (Pamelor)

A

TCA: secondary amine

  • inhibits reuptake primarily of NE
  • also blocks a adrenergic, Histamine and Muscarinic R
  • depression, TMJ, fibromyalgia, enuresis
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4
Q

Despiramine (Norpramin)

A

TCA: secondary amine

*blocks reuptake primarily of NE

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5
Q

Fluoxetine (Prozac)*

A

SSRI: selectively inhibits 5-HT reuptake

*Depression, mosty likely to inhibit CYP450 - 2D6, 3A4

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6
Q

Sertraline (Zoloft)

A

SSRI: selectively inhibits 5-HT reuptake

*depression, preferred in elderly bc least likely to interact w/ drug

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7
Q

Citalopram (Celexa)

A

SSRI: selectively inhibits 5-HT reuptake

current DOC for depression

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8
Q

Venlafaxine (Effexor)

A

SNRI: inhibit NE and 5-HT reuptake

  • depression, neuropathic pain, postmenopausal hot flashes
  • may increase BP, cardiac toxicity
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9
Q

Duloxetine (Cymbalta)

A

SNRI: inhibits NE and 5-HT reuptake

  • depression, neuropathic pain, post meno hot flashes
  • may cause hepatotoxicity
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10
Q

Phenelzine (Nardil)

A

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

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11
Q

Selegiline (Deprenyl)

A

MAOI: selectively inhibits MAO-B, increases DA

  • used for depression which doesn’t respond to other drugs
  • also used for Parkinsons
  • fewer SE
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12
Q

Bupropion (wellbutrin)

A

Preferentially inhibits DA reuptake

  • sometimes used with SSRI
  • ADHD, alcoholism (decreases craving), extended release for smoking cessation (Zyban)
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13
Q

Mirtazapine (Remeron)

A

NaSSA: noreadrenergic and specific serotonergic antidepressant
*blocks presynaptic a2, increases release of NE and 5-HT, blocks 5-HT2a and 5-HT3 receptors

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14
Q

Atomoxetine (Strattera)

A

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
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15
Q

Trazodone (Desyrel)

A

5-HT2a receptor antagonist

  • antianxiety, antipsychotic, antidepressant, sedating effects
  • MOST COMMON USE is off label HYPNOTIC or SLEEP aid
  • also used for pain mgmt
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16
Q

St Johns Wort (hpericin)

A

uncertain MOA

  • may be effective in mild depression
  • do not comb with other antidepressants –> serotonin syndrome
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17
Q

Chlorpromazine (Thorazine)

A

Classical antipsychotic: blocks DA D2 receptors

*use for psychosis associated with mania and drugs of abuse, antiemetic (prochlorperazine), pre-anesthetic

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18
Q

Fluphenazine (Prolixin)

A

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
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19
Q

Haloperidol (Haldol)

A

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
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20
Q

Clozapine (Clozaril)

A

Atypical antipsychotic: Blocks 5-HT2a and DA D4 receptors, some DA D2

  • alleviate +/- sx
  • Drug of last choice due to Agranulocytosis (monitor CBC)
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21
Q

Olanzapine (Zyprexa)

A

Atypical Antipsychotic: Blocks 5-HT2a, DA D4 and D2 receptors

  • improves +/- sx
  • similar to clozapine but no agranulocytosis
  • also used for bipolar
22
Q

Risperidone (Risperdal)

A

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
23
Q

Ziprisadone (Geodon)

A

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
24
Q

Quetiapine (seroquel)

A

Atypical antipsychotic:*blocks 5-HT2a and DA D2 receptors

  • Similar to clozapine, no agranulocytosis, no PRL
  • used to promote sleep onset and maintenance, SEDATING
25
Q

Aripriprazole (abilify)

A

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
26
Q

Lithium, anticonvulsants and antipsychotics (Olanzapine) combined for

A

bipolar disorder

27
Q

Lithium Li

A

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

28
Q

Valproic acid (depakene)

A

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)

29
Q

Gabapentin (Neurontin)

A

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
30
Q

Carbamazepine (Tegretol)

A

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
31
Q

Lamotrigine (Lamictal)

A

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
32
Q

Naltrexone (ReVia)

A

Opioid R antagonist

Blocks ability of alcohol to stim reward pathway

33
Q

Acamprostate (Campral EC)

A

Structural Analogues of Gaba

Restores normal balance of GABA and glutamate to increase abstinence in alcoholism

34
Q

Disulfaram (Antabuse)

A

Inhiits aldehyde dehyrdogenase (help tx alcoholism) but acetaldehyde build up = dangerous)

35
Q

Fomepizole (antizole)

A

Alcohol dehydrogenase inhibitor

  • used to treat Methanol poisoning
  • note that ethanol can also be used
36
Q

Chloral Hydrate (Noctec)

A

Sedative hypnotic

  • converted to trichloroethanol which causes sedation, acts similarly to Barbs on GABA recetpor
  • ped dental procedure and nursing homes, cheap, low MOS
37
Q

Pentobarbital (Nembutal Na)

A

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
38
Q

Phenobarbital (Luminal)

A

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
39
Q

Secobarbital (Seconal)

A

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
40
Q

Thiopental (Pentothal)

A

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)
41
Q

Diazepam (Valium)

A

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
42
Q

Flurazepam (Dalmane)

A

BZ (long action metabolites, 74hr half life)

*Commonly used as hypnotics for INSOMNIA (less depression of REM sleep than Barbs)

43
Q

Midazolam (Versed)

A

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),

44
Q

Temazepam (Restoril)

A

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,
45
Q

Alprazolam (Xanax)

A

BZ, bind site on GABA r to prolong action of GABA (anxiolytic, sedative-hypnotic)
*short action (<6hr) converted to short acting metabolites

46
Q

Lorazepam (Ativan)

A

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
47
Q

Flumazinel (Mazicon)

A

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
48
Q

Zolpidem (ambien)

A

Bind BZ1 of GABA R

  • strong and rapid sedative activity, high MOS
  • sleep relate behaviors, rebound insomnia
49
Q

Zaleplon (sonata)

A

Bind BZ1 subtype of GABA R, increase GABA

  • very strong, rapid sedation, high MOS
  • sleep related behaviors, rebound insomnia
50
Q

Eszopiclone (lunesta)

A

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)

51
Q

Ramelteon (Rozerem)

A

Melatonin analogue

*resets sleep-wake cycle (promotes sleep indep of GABA); additive sedation with ETOH and other sedative hypnotics

52
Q

Buspirone (BuSpar)

A

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