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year 2 > CNS drugs > Flashcards

CNS drugs Flashcards

1
Q

chlorpromazine**

A

→ block D2, α-adrenergic, antihistamine & considerable anticholinergic; Jaundice
neg. ionotrpic on heart
(low potency) →↑-

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2
Q

Thioridazine

A

retinal deposits
Chorpromazine→ block D2, α-adrenergic, antihistamine & considerable anticholinergic; Jaundice
neg. ionotrpic on heart
(low potency)

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3
Q

Fluphenazine

A

→ more selective for dopamine, less anticholingeric, ↑ extrapyramidal effects
(high potency)

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4
Q

Perchloroperazine

A

Phenothiazine

→ nausea & vomiting

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5
Q

Trifluoperazine

A

→ less anticholinergic: ↑ extrapyramidal, ↓ hypoTN & sedation

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6
Q

Haloperidol**

A

→ greater potency at D2, some α1 & 5HT2, no anticholinergic; MOST likely to cause pyramidal

  • used for acute psychotic situations;
  • tourettes
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7
Q

Pimozide

A

→ binds ONLY to D2; high extrapyramidal, mod. antichol;

Tourettes syn tics

-prolong QT (risperidone, ziprasidone, pimozide)

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8
Q

Loxapine

A

→ use when others dont work; greater seizure risk than Phenothiazines

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9
Q

Olanzapine**

A

blocks D2, D4* (+ symp), 5-HT2a (neg. symp); anti-ACh (↓ ↓ extrapyramid); (anti-Hist/ACh/alpha 1)
tx Bipolar
→ WEIGHT GAIN (most likely)
(first line drug)

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10
Q

Risperidone*

A

→ inhib D2 & esp 5HT2a; block α; +SSRI for resitant depression & autism (↑ DA in basal gang)

  • Plaiperidone is metabolite
    -prolong QT (risperidone, ziprasidone, pimozide)
    (first line drug)
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11
Q

Ziprasidone*

A

→ similar to risperidone; 5HT1a agonism or inhabit 5HT repute

tx Tourette, acute mania;
-prolong QT (risperidone, ziprasidone, pimozide)
↓ chance weight gain; hyperprolactinemia
-caution w/ pts who have history of seizures

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12
Q

Clozapine

A

→ binds D4 & 5HT2a > affinity than D2 (↓↓ extrapyramidal) binds α1 & histamine & anti-ACh;

  • agranulocytosis; RESERVED;
  • psychosis in Parkisons pts
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13
Q

Quetiapine*

A

→ similar to clozapine; ↑ + & - symp; ↓ ↓ SE;

**-↑ NE via metabolite & 5-HT2c block
-little Prolactin affect
-monotherapy for bipolar
first line drug

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14
Q

Iloperidone

A

→ block D2 & 5HT2a, α1; no muscarinic

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15
Q

Lurasidone

A

→ block D2 5HT2a, partial agonist 5HT1a; NO antihistamine or muscarinic; agranulocytosis & neutropenia

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16
Q

Asenapine

A

→ blocks 5-HT2a & 2c, D3** (not strong D2);

  • blocks histamine & α (not muscarinic)
    tx: PTSD nightmares

-less metabolic effects

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17
Q

Aripiprazole**

A

→ dopamine stabilizer;

  • partial agonist @ D2 & 5-HT1a;
  • blocks 5HT2a, α1, & histamine
  • no affect on prolactin, QT;
  • less weight gain.

SE- ↓ esophageal motility (aspiration pneumonia)
↑ blood glucose (diabetes may develop or worsen)

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18
Q

Lithium**

A

→ ↓ release & turnover of NE & DA;

  • ↑ ACh;
  • ↓ IP3 and DAG
  • may uncouple receptors from G-protein (hypothyroid & polyuria)
  • SLOW onset of action
  • prevent mania and depression

-competes w/ Na in proximal tubule for reabsorption

↓ Lithium clearance:

  • -low Na
  • -Thiazide diuretics
  • -NSAID

SIDE EFFECTS

  • TREMOR (tx w/ βB)
  • Nausea
  • Headache
  • ↓ thyroid function (blocks thyroxine)
  • Renal effects- nephrogenic diabetes insipidus (tx: amiloride)
  • weight gain
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19
Q

Divalproex

Valproic Acid

A

→ blocks Na, ↓ NMDA receptor stim, ↑ GABA synthesis & lvls
-DOC if both seizure types occur together (can be used for all seizure types except infantile spasm);

-LIVER toxicity, pancreatitis; hair loss
several drug interaction

BIPOLAR
→ anticonvulsant; effect >= Lithium; rapid onset;
pts who dont respont to Li; few SE

category D

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20
Q

Phenytoin**

Fosphenytoin

A

→ prolong inactivation of Na channel (prevents spread & inhibits glutamate release)
-no general CNS depression, not very sedating
-Zero order metabolism at therapeutic levels
-↑ [warfarin] (↓metabolism)
-↑ metabolism of oral contraceptives
LOTS OF SE & INTERACTIONS

→ water soluble prodrug (IV use)

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21
Q

Carbamazepine**

A 
→ blocks Na & inhibits NTM (glutamate) release; inhib NE release & reuptake;
-mood stabilizing (bipolar)
-Idosyncratic blod dyscracias:
--aplastic anemia 
--agranulocytosis
--mild leukopenia
(mainly in elderly for trigem)

DOC for partial seizures;
1st drug for tonic-clonic seizures, Trigeminal nerualgia (↑ doses)

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22
Q

Levatiracetam*

A

ANTICONVULSANT
→ binds SV2A (↓ glutamate & ↑ GABA); few drug interactions
-Partial & generalized tonic-clonic seizures
-Myoclonic seizures

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23
Q

Lamotrigine*

A

ANTICONVULSANT
→ inactivates Na, N & P/Q Ca++ channels (absence seizures), ↓ glutamate;
-Dermatitis (life-threatening in children)

–Partial & generalized tonic-clonic seizures

  • Atonic seizures
  • category C
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24
Q

Topiramate**

A

ANTICONVULSANT
→ block Na channels, ↑ GABAa current, ↓ glutamate receptor activation;
-inhibits SPREAD not ↑ threshold;
-secreted unchanged in urie

treatment for:

  • -bipolar
  • -eating disorder & binge eating
  • -weight loss aid
  • -alcoholics (started in teens)

-SE acute myopia & glaucoma

  • Partial & generalized tonic-clonic seizures
  • infantile spasm

-helps ↓ craving in recovering alcoholics

category C

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25
Q

Gabapentin

Pregabalin

A

ANTICONVULSANT
→ GABA analogs, not on receptors, ↑ GABA release; block N-type Ca+ (inhib glutamate release) TMJ
→ fibromyalgia

category C

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26
Q

Vigabatrin

A

ANTICONVULSANT
→ irreversible inhib of GABA transaminase; ↑ GABA levels & tonic inhib of brain;

Irreversible constriction of visual field and/or retinal damage;

CI pre-exisitng mental illness

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27
Q

Tiagabine*

A

ANTICONVULSANT
→ inhib. GABA uptake (forebrain & hippo);
–prolong inhib action of GABA

adjunt tx partial seizures

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28
Q

Ethosuximide**

A

→ DOC for absence seizure; block T-type Ca channels; GI SE; valproic acid ↓ clearance

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29
Q

Carbamazepine ↑ metabolism of

A
  • -phenytoin
  • -primidone
  • -ethosuximide
  • -valproic acid
  • -clonazepam
  • -haloperidol
  • -oral contraceptives
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30
Q

↑ metabolism of Carbamazepine

A
  • -phenobarbital
  • -phenytoin
  • -valproic acid
  • -carbamazepine
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31
Q

↓ Metabolism of Carbamazepine:

A
  • -Cimetidine
  • -Fluoxetine
  • -Isoniazid
  • -erythromycin
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32
Q

Valproic acid ↓ metabolism of:

A
  • Valproic acid
  • Phenytoin (& displaces)
  • Carbamazepine
  • Phenobarbital (coma)
  • ↓ elimination of lamotrigine
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33
Q

Baclofen**

A

GABA-mimetic
→ GABAb agonist brain & spine; ↓ excitatory NTM;
-may ↓ substance P (↓ pain)
-intrathecal administration: better control

tx: chronic spascitiy, back pain, prevent migraines

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34
Q

Diazepam**

A

→ GABAa in spinal cord; required dose causes significant sedation; spasm w/ trauma

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35
Q

Cyclobenzaprine**

A

→ similar structure as TCA; sedative @ brain stem; anti-ACh;

  • significant sedation, confusion –transient visual hallucination
  • spasms from trauma/sprain;
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36
Q

Carisoprodol

A

→ metabolite (meprobamate) is anxiolytic (acts like barbs); addiction potential; ↑ microsomal enz)

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37
Q

Tizanidine**

A 
→ analogue of clonidine; acts at α2; pre/post synaptic inhib;
-inhib pain @ dorsal horn;
-SEDATING 
hypoTN (esp w/ antHTN rx)
-dry mouth, muscle weakness (elderly)
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38
Q

Dantrolene**

A

→ targets excitation contraction coupling not CNS;
-↓ Ca release from SR;

tx: malignant hyperthermia & neuroleptic malignant syndrome (antipsychotics)

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39
Q

Methylphenidate

A

→ ADHD & narcolepsy; ↑ DA & NE in prefrontal ctx → modulate GABA & glutamate

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40
Q

Amphetamine

A

→ ADHD & narcolepsy; ↑ DA & NE in prefrontal ctx → modulate GABA & glutamate

41
Q

Atamoxetine**

A

→ SNRI, potentiate effects of β-agonists, dont use w/ vasopressors
Tx: ADHD in adolescents and children 6+

possible liver toxicity

42
Q

Caffeine

A

→ blocks adenosine receptors & inhib PDE; ↑ contractility dilates coronary aa, constricts cerebral (headache tx) moderate bronchodilation, ↑ gastric acid, diuresis

43
Q

Levodopa**

A

→ able to pass BBB; high doses needed b/c peripheral metabolism; nausea & vomitting esp. effective against bradykinesia; arrhythmias, htpoTN & HTN w/ MAOI, dyskinesia
-On/Off phenomenon

44
Q

Carbidopa

A

→ dopa decarboxylase inhib, doesnt cross BBB; ↓ DA synthesis in periphery

45
Q

Carbidopa/levodopa**

A

→ combo ↑ DA in brain & ↓ in periphery; ↓ nausea & vomiting; food ↓ aborp, taken 3-4x/day; doesnt alter progression of disease; dyskinesa more common

46
Q

Selegiline**

A

→ inhib. MAOb (↓ striatal metab of DA); MAOa at ↑ doses;

  • may ↓ progession (↓ h2o2);
  • amphetamine like metabolite (insomnia)
47
Q

Rasagiline

A

→ irreversibe MAO-B inhib; no amphetamine like metabolites, no tyramine restriction

48
Q

Bromocriptine**

A 
Dopamine Agonist:
→ D2 agonist; 
-effectiveness does not ↓
-↓ prolactin; 
-GI SE, postural hypoTN, arrythmias (same as l-dopa)

-vasospasm SE (erythromelagia, pulmonary fibrosis)

49
Q

Pergolide

A

Dopamine Agonist:

→ D1 & D2 agonist; sudden sleep

50
Q

Pramipexole**

A

Dopamine Agonist:
→ NO erythromelalgia, vasospasm, fibrosis;
-can cause sudden sleep; well tolerated
-on/off less likely

51
Q

Ropinirole**

A

Dopamine Agonist:
→ treatment for RLS
→ NO erythromelalgia, vasospasm, fibrosis; can cause sudden sleep; well tolerated, on/off less likely

52
Q

Amantadine

A

→ antiviral for flu; ↑ release of DA (less potent than L-dopa); toxic psycosis & convulsions (OD) spotting of skin & edema; caution w/ history of seizure or CHF

53
Q

Benztropine**

A

→ ↓ effects of ACh to balance loss of DA;

-improves rigidity & tremor (not bradykinesia)

54
Q

Donepezil**
Rivastigmine
Galantamine

A

Cholinesterase Inhibitors
↓ breakdown of ACh in synaptic cleft
-may slow course of disease
-GI side-effects, ↑ stomach acid & salivation

55
Q

Memantine

A

→ NMDA antagonist; ↓ extra-synaptic NMDA glutamate toxicity;

↑ SE of l-dopa & DA agonists;

-SE agitation, urinary incontinence, UTI,

56
Q

Flumazenil**

A

→ competes w/ benzo for receptor;
-IV admin slowly in series to ↓ risk of seizures (DoA 30 min)

  • reverse effect of: Midazolam, zolpidem, zaleplon, eszopiclone
  • can cause seizure in pts w/ barb or TCA overdose; DO NOT use if signs of seizures
57
Q

Zolpidem**

A

→ bind BZ1 subtype; 2hr half-life

-minor effect on REM

58
Q

Zaleplon

A

→ bind BZ1 subtype; 1hr half-life

-minor effect on REM

59
Q

Eszopiclone

A

→ less selective (more like benzo) 6hr half-life; long term treatment of insomnia
-minor effect on REM

60
Q

Ramelteon**

A

→ MT1 & MT2; shortens delay to sleep onset;
-extensive 1st pass metab. (caution w/ liver diease, dont use w/ severe liver problems)

SIDE EFFECTS

  • ↑ prolactin & ↓ testosterone
  • headache, rash
61
Q

Buspirone**

A

→ partial agonist 5-HT1; relieves anxiety w/o sedation; 2 wks to take affect

  • ↓ serotonin release
  • ↑ noradrenergic & DAnergic pathways
  • no effect on bento or GABA receptors
  • -LOW addiction potential
  • -good for ADDICTS & ELDERLY
  • no sedation**
  • doesnt affect memory**

+ MAOI → severe HTN or serotonin syndrome

62
Q

Chloral hydrate**

A

→ converted to trichloroethanol, binds GABAa

  • acts similar to barbiturates (low safety)
  • -respiratory and vasomotor depression
  • -tolerance and dependance
  • -liver danage & fatal intoxication

-pediatric dental procedures

63
Q

Diphenhydramine**

A

→ blocks H1 receptor, anti-ACh; good choice for insomnia in addicts to alcohol or benzo

64
Q

Naltrexone**

A

→ blocks ability of alcohol to simulate reward pathway (B-endorphin)
↓ craving (↓ rate of relapse by 50%); nausea, large dose → liver damage, opioid wont work

65
Q

Acamprosate

A

→ structural analogue of GABA; restores normal balance of GABA/Glutamte transmission
(NO LIVER TOXICITY → DOC for pts w/ liver disease)

66
Q

Disulfiram**

A

→ blocks ALDEHYDE dehydrogenase; long duration; inhib p450

lots of side-effects and drug interactions; not recommended

67
Q

Drugs most likely to cause Steve Johnson syndrome

A

HLA-B*1502

  • phenytoin, fosphenytoin
  • phenobarbital, primidone
  • lamotrigene
  • ethosuximide
  • valproic acid
68
Q

Phenobarbital

A

→ long lasting; anticonvulsant
↑ duration of GABA action

Contraindicated in:
-porphyria (↑ synthesis)

69
Q

Thiopental

A

ultra-short acting; induction of anesthesia

↑ duration of GABA action

70
Q

Benzodiazepines duration of action

A

Long lasting:

  • Diazepam
  • Chlordiazepoxide
  • flurazepam
  • chlorazepate (inactive)

Intermediate:

  • oxazepam
  • lorazepam

short acting:

  • alprazolam
  • triazolam

very short acting:
-midazolam

71
Q

Diazepam**

A

muscle relax, anticonvulsant (status epilepticus), alcohol/barb withdrawl

-cimetidine ↓ metabolism

-long lasting
↑ actions of GABA

Contraindicated in:

  • pregnancy (category D)
  • children (elderly confusion)
  • sleep apnea
  • w/ alcohol use

-Tolerance and dependance can develop

72
Q

Chlordiazepoxide

A

alcohol/barb withdrawal
-long lasting

↑ actions of GABA

Contraindicated in:

  • pregnancy (category D)
  • children (elderly confusion)
  • sleep apnea
  • w/ alcohol use

-Tolerance and dependance can develop

73
Q

Lorazepam

A

anticonvulsant (Status epilepticus)
-alcohol/barb withdrawal

-intermediate action

Contraindicated in:

  • pregnancy (category D)
  • children (elderly confusion)
  • sleep apnea
  • w/ alcohol use

-Tolerance and dependance can develop

74
Q

Oxazepam

A

alcohol/barb withdrawl if liver damage present

-intermediate action

Contraindicated in:

  • pregnancy (category D)
  • children (elderly confusion)
  • sleep apnea
  • w/ alcohol use

-Tolerance and dependance can develop

75
Q

Clonazepam

A

anticonvulsant
-prevent absence seizures

Contraindicated in:

  • pregnancy (category D)
  • children (elderly confusion)
  • sleep apnea
  • w/ alcohol use

-Tolerance and dependance can develop

76
Q

Midazolam**

A

→ anesthesia prep & short procedures

  • anterograde amnesia
  • very short acting

Contraindicated in:

  • pregnancy (category D)
  • children (elderly confusion)
  • sleep apnea
  • w/ alcohol use

-Tolerance and dependance can develop

77
Q

Flurazepam

A

treat early morning waking

  • long duration of action
  • can accumulate if taken daily

Contraindicated in:

  • pregnancy (category D)
  • children (elderly confusion)
  • sleep apnea
  • w/ alcohol use

-Tolerance and dependance can develop

78
Q

Temazepam

Triazolam*

A

treat insomnia
Triazolam for difficulty falling asleep
-less depression of REM

Contraindicated in:

  • pregnancy (category D)
  • children (elderly confusion)
  • sleep apnea
  • w/ alcohol use

-Tolerance and dependance can develop

79
Q

Anxiety disorders where Benzo are not used

A
  • OCD (SSRI)
  • agoraphobia & panic disorders (SSRI or antidepressant)
  • PTSD (antidepressants)
  • anxiety in children or adolescents (antidepressants)
80
Q

TCA**

A

→ inhibit reuptake of NE & 5HT
–analgesic b/c NE ↑ endorphin release which ↓ substance P

  • **anti-ACh→ impair memory & cognition, dry mouth, vision problems, ↓ sweating
  • **anti-Histamine→ drowsiness & weight gain
  • **α1 blockade→ orthostatic hypoTN and ejaculation difficulties
  • cardiac depression & ↑ irritability (torsade de pointes)
  • -ventricular arryth (flat or inverted T waves)
  • -AVOID if previous MI or BBblock

-SIADH → hypoNA

81
Q

TCA overdose

A
  • cardiac conduction defects & arrhythmias (torsade)
  • -Mg & isoproterenol; phenytoin
  • hypotension
  • respiratory depression
  • agitation, delirum, restlessness
  • seizures (neuromusc. irratability)
  • -phenytoin
  • coma w/ shock & metabolic acidosis
82
Q

Imipramine

A

TCA

  • worst cardiac depression
  • enurisis
  • metabolized to Desipramine
83
Q

Clomipramine

A

only used for OCD

84
Q

Phenelzine**

Tranylcypromine

A

→ both irreversibly inhibit MAO-A (NE & 5HT) & MAO-B (DA);
-anti α & ACh
-effects last 1-3 weeks after stopping
-drug of last choice when others have not worked
+ Tyramine or sympathomimetic → HTN crisis

+ OTC cold meds → HTN or serotonin syn

+TCA or SSRI → serotonin syn

+ Busipirone → sever HTN

85
Q

Fluoxetine**

A

→ inhibits reuptake of 5HT and NE; has active metabolite (LONG DoA); can cause insomnia

  • OCD
  • bulimia
  • PMS
86
Q

Fluvoxamine

A

OCD

87
Q

Paroxetine

A

OCD, social anxiety; causes sedation

  • more selective for 5HT
  • inactive metabolite
  • CI in pregnancy due to cardiac effects
88
Q

Sertraline

A

OCD, social anxiety; causes insomnia

-more selective for 5HT than fluoxetine → less sexual SE

89
Q

Citalopram

Escitalopram

A
  • similar SE to fluoxetine & sertraline

- FEWER pharmacokinetic interactions

90
Q

Vortioxetine

A
  • inhibits serotonin transporters
  • -5HT3a & 5HT7 antagonist
  • -5HT1b partial agonist
  • -5HT1a agonist
91
Q

Vilazodone

A

→ SSRI & 5HT1a partial agonist (like busipirone)

92
Q

Venlafaxine** (longer DOA)

desvenlafaxine (metabolite)

A

→ inhibts repute of 5HT and NE
–depression, hot flashes, neuropathic pain

-may ↑ BP and hypoNA (SIADH)

93
Q

Duloxetine (Cymbalta)

A

SNRI
→ physical symptoms (pain)
-hepatotoxic
-CI in 3rd trimester

94
Q

Milnacipran

Levomilnacipran

A

SNRI
→ fibromyalgia
→ major depressive disorder

95
Q

Bupropion**

A

→ inhib reuptake of DA and NE

  • quit smoking (extended release form), reduce craving for alcohol and weight loss
  • ADHD

-combine w/ SSRI to improve effectivness and decrease sexual side-effects

may produce psychosis
CI w/ history of seizures or head trauma
-dont take w/ drugs that may ↓ seizure threshold (TCA and antipsychotics)

96
Q

Mirtazapine

A

→ blocks presynaptic α2 ( ↑ NE and 5HT), blocks 5HT2a & 5HT3

  • antihistamine
  • eliminates normal SE of SSRI b/c of block at 5HT2a & 5HT3
97
Q

Trazodone**

A

→ partial agonist at 5HT1a and block 5HT2a

  • not good antidepressant
  • SLEEP AID
  • PRIAPISM
98
Q

St. John’s Wort

A

→ block repute of NE, 5HT, and possible DA
-DO NOT USE W/
MAOI, SSRI, TCA, ldopa, selegilline)

99
Q

Ketamine**

A

blocks NMDA receptors

  • general anesthetic
  • rapid and long lasting

-vivid dreams

year 2 (15 decks)

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