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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
Gabapentin | Pregabalin
ANTICONVULSANT → GABA analogs, not on receptors, ↑ GABA release; block N-type Ca+ (inhib glutamate release) TMJ → fibromyalgia category C
26
Vigabatrin
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
27
Tiagabine*
ANTICONVULSANT → inhib. GABA uptake (forebrain & hippo); --prolong inhib action of GABA adjunt tx partial seizures
28
Ethosuximide**
→ DOC for absence seizure; block T-type Ca channels; GI SE; valproic acid ↓ clearance
29
Carbamazepine ↑ metabolism of
- -phenytoin - -primidone - -ethosuximide - -valproic acid - -clonazepam - -haloperidol - -oral contraceptives
30
↑ metabolism of Carbamazepine
- -phenobarbital - -phenytoin - -valproic acid - -carbamazepine
31
↓ Metabolism of Carbamazepine:
- -Cimetidine - -Fluoxetine - -Isoniazid - -erythromycin
32
Valproic acid ↓ metabolism of:
- Valproic acid - Phenytoin (& displaces) - Carbamazepine - Phenobarbital (coma) - ↓ elimination of lamotrigine
33
Baclofen**
GABA-mimetic → GABAb agonist brain & spine; ↓ excitatory NTM; -may ↓ substance P (↓ pain) -intrathecal administration: better control tx: chronic spascitiy, back pain, prevent migraines
34
Diazepam**
→ GABAa in spinal cord; required dose causes significant sedation; spasm w/ trauma
35
Cyclobenzaprine**
→ similar structure as TCA; sedative @ brain stem; anti-ACh; - significant sedation, confusion --transient visual hallucination - spasms from trauma/sprain;
36
Carisoprodol
→ metabolite (meprobamate) is anxiolytic (acts like barbs); addiction potential; ↑ microsomal enz)
37
Tizanidine**
``` → 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) ```
38
Dantrolene**
→ targets excitation contraction coupling not CNS; -↓ Ca release from SR; tx: malignant hyperthermia & neuroleptic malignant syndrome (antipsychotics)
39
Methylphenidate
→ ADHD & narcolepsy; ↑ DA & NE in prefrontal ctx → modulate GABA & glutamate
40
Amphetamine
→ ADHD & narcolepsy; ↑ DA & NE in prefrontal ctx → modulate GABA & glutamate
41
Atamoxetine**
→ SNRI, potentiate effects of β-agonists, dont use w/ vasopressors Tx: ADHD in adolescents and children 6+ possible liver toxicity
42
Caffeine
→ blocks adenosine receptors & inhib PDE; ↑ contractility dilates coronary aa, constricts cerebral (headache tx) moderate bronchodilation, ↑ gastric acid, diuresis
43
Levodopa**
→ 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
Carbidopa
→ dopa decarboxylase inhib, doesnt cross BBB; ↓ DA synthesis in periphery
45
Carbidopa/levodopa**
→ combo ↑ DA in brain & ↓ in periphery; ↓ nausea & vomiting; food ↓ aborp, taken 3-4x/day; doesnt alter progression of disease; dyskinesa more common
46
Selegiline**
→ inhib. MAOb (↓ striatal metab of DA); MAOa at ↑ doses; - may ↓ progession (↓ h2o2); - amphetamine like metabolite (insomnia)
47
Rasagiline
→ irreversibe MAO-B inhib; no amphetamine like metabolites, no tyramine restriction
48
Bromocriptine**
``` Dopamine Agonist: → D2 agonist; -effectiveness does not ↓ -↓ prolactin; -GI SE, postural hypoTN, arrythmias (same as l-dopa) ``` -vasospasm SE (erythromelagia, pulmonary fibrosis)
49
Pergolide
Dopamine Agonist: | → D1 & D2 agonist; sudden sleep
50
Pramipexole**
Dopamine Agonist: → NO erythromelalgia, vasospasm, fibrosis; -can cause sudden sleep; well tolerated -on/off less likely
51
Ropinirole**
Dopamine Agonist: → treatment for RLS → NO erythromelalgia, vasospasm, fibrosis; can cause sudden sleep; well tolerated, on/off less likely
52
Amantadine
→ 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
Benztropine**
→ ↓ effects of ACh to balance loss of DA; | -improves rigidity & tremor (not bradykinesia)
54
Donepezil** Rivastigmine Galantamine
Cholinesterase Inhibitors ↓ breakdown of ACh in synaptic cleft -may slow course of disease -GI side-effects, ↑ stomach acid & salivation
55
Memantine
→ NMDA antagonist; ↓ extra-synaptic NMDA glutamate toxicity; ↑ SE of l-dopa & DA agonists; -SE agitation, urinary incontinence, UTI,
56
Flumazenil**
→ 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
Zolpidem**
→ bind BZ1 subtype; 2hr half-life | -minor effect on REM
58
Zaleplon
→ bind BZ1 subtype; 1hr half-life | -minor effect on REM
59
Eszopiclone
→ less selective (more like benzo) 6hr half-life; long term treatment of insomnia -minor effect on REM
60
Ramelteon**
→ 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
Buspirone**
→ 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
Chloral hydrate**
→ 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
Diphenhydramine**
→ blocks H1 receptor, anti-ACh; good choice for insomnia in addicts to alcohol or benzo
64
Naltrexone**
→ 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
Acamprosate
→ structural analogue of GABA; restores normal balance of GABA/Glutamte transmission (NO LIVER TOXICITY → DOC for pts w/ liver disease)
66
Disulfiram**
→ blocks ALDEHYDE dehydrogenase; long duration; inhib p450 | lots of side-effects and drug interactions; not recommended
67
Drugs most likely to cause Steve Johnson syndrome
HLA-B*1502 - phenytoin, fosphenytoin - phenobarbital, primidone - lamotrigene - ethosuximide - valproic acid
68
Phenobarbital
→ long lasting; anticonvulsant ↑ duration of GABA action Contraindicated in: -porphyria (↑ synthesis)
69
Thiopental
ultra-short acting; induction of anesthesia | ↑ duration of GABA action
70
Benzodiazepines duration of action
Long lasting: - Diazepam - Chlordiazepoxide - flurazepam - chlorazepate (inactive) Intermediate: - oxazepam - lorazepam short acting: - alprazolam - triazolam very short acting: -midazolam
71
Diazepam**
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
Chlordiazepoxide
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
Lorazepam
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
Oxazepam
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
Clonazepam
anticonvulsant -prevent absence seizures Contraindicated in: - pregnancy (category D) - children (elderly confusion) - sleep apnea - w/ alcohol use -Tolerance and dependance can develop
76
Midazolam**
→ 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
Flurazepam
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
Temazepam | Triazolam*
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
Anxiety disorders where Benzo are not used
- OCD (SSRI) - agoraphobia & panic disorders (SSRI or antidepressant) - PTSD (antidepressants) - anxiety in children or adolescents (antidepressants)
80
TCA**
→ 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
TCA overdose
- cardiac conduction defects & arrhythmias (torsade) - -Mg & isoproterenol; phenytoin - hypotension - respiratory depression - agitation, delirum, restlessness - seizures (neuromusc. irratability) - -phenytoin - coma w/ shock & metabolic acidosis
82
Imipramine
TCA - worst cardiac depression - enurisis - metabolized to Desipramine
83
Clomipramine
only used for OCD
84
Phenelzine** | Tranylcypromine
→ 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
Fluoxetine**
→ inhibits reuptake of 5HT and NE; has active metabolite (LONG DoA); can cause insomnia - OCD - bulimia - PMS
86
Fluvoxamine
OCD
87
Paroxetine
OCD, social anxiety; causes sedation - more selective for 5HT - inactive metabolite - CI in pregnancy due to cardiac effects
88
Sertraline
OCD, social anxiety; causes insomnia | -more selective for 5HT than fluoxetine → less sexual SE
89
Citalopram | Escitalopram
- similar SE to fluoxetine & sertraline | - FEWER pharmacokinetic interactions
90
Vortioxetine
- inhibits serotonin transporters - -5HT3a & 5HT7 antagonist - -5HT1b partial agonist - -5HT1a agonist
91
Vilazodone
→ SSRI & 5HT1a partial agonist (like busipirone)
92
Venlafaxine** (longer DOA) | desvenlafaxine (metabolite)
→ inhibts repute of 5HT and NE --depression, hot flashes, neuropathic pain -may ↑ BP and hypoNA (SIADH)
93
Duloxetine (Cymbalta)
SNRI → physical symptoms (pain) -hepatotoxic -CI in 3rd trimester
94
Milnacipran | Levomilnacipran
SNRI → fibromyalgia → major depressive disorder
95
Bupropion**
→ 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
Mirtazapine
→ blocks presynaptic α2 ( ↑ NE and 5HT), blocks 5HT2a & 5HT3 - antihistamine - eliminates normal SE of SSRI b/c of block at 5HT2a & 5HT3
97
Trazodone**
→ partial agonist at 5HT1a and block 5HT2a - not good antidepressant - SLEEP AID - PRIAPISM
98
St. John's Wort
→ block repute of NE, 5HT, and possible DA -DO NOT USE W/ MAOI, SSRI, TCA, ldopa, selegilline)
99
Ketamine**
blocks NMDA receptors - general anesthetic - rapid and long lasting -vivid dreams

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