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Drugs/Immuno > Neuro Drugs > Flashcards

Neuro Drugs Flashcards

1
Q

Dantrolene

A
  • decreases muscle contraction by directly interfering with calcium ion release from sarcoplasmic reticulum in skeletal muscle
  • uncoupled excitation-contraction process
  • useful in treating malignant hyperthermia
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2
Q

Baclofen

A
  • GABA-B agonist
  • used to treat spasticity, improve mobility in pts with MS
  • works on spinal cord to block polysynaptic afferent pathways
  • acts as inhibitory neurotransmitter or by hyperpolarizing the primary afferent nerve terminals which inhibit other excitatory neurotransmitters
  • works at supraspinal sites
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3
Q

Cyclobenzaprine

A
  • similar to amitriptyline, effects are similar to tricyclic antidepressants
  • sedation, confusion, visual hallucinations and releases histamine
  • relieves muscle spasms through central action
  • no direct action on NMJ or muscle
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4
Q

Tizanidine

A
  • central acting alpha2-adrenergic agonist acts pre and post synaptically within the cord
  • related to clonidine
  • decreases release of excitatory amino acids and inhibits spinal motor neurons
  • drowsiness and sedation
  • no muscle weakness
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5
Q

Riluzole, Idrocilamide

A
  • inhibits glutamate transmission and improves energy metabolism in muscles
  • inhibits release of glutamate by interfering with sodium channels
  • treats ALS and Huntington’s disease
  • extends survival
  • side effects: asthenia, decreased lung function, pneumonia, vertigo, parasthesia, anorexia, somnolence
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6
Q

Gabapentin

A
  • antiepileptic used for MS patients

- GABA analog works on Ca2+ receptors

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7
Q

Progabide

A

-GABA-A and GABA-B agonist with active metabolites

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8
Q

Morphine

A
  • strong mu agonists
  • chronic and severe pain
  • high intrinsic activity
  • hospice care, fixed-interval administration with regular dose
  • low O/P ratio
  • used for acute pulmonary edema, anxiety, decrease cardiac load
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9
Q

Oxycodone

A
  • chronic and severe pain
  • high intrinsic activity
  • hospice care, fixed-interval administration with regular dose
  • strong mu agonist
  • low O/P ratio
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10
Q

Fentanyl

A
  • strong mu agonist
  • low O/P ratio
  • transdermal patch given over long period if GI transit occurs from oral
  • buccal for short, breakthrough pain
  • low risk of respiratory depression so can be used for adjunct anesthesia
  • decreases heart rate, increase ICP, caution in liver failure
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11
Q

Methadone

A
  • strong mu agonist
  • high O/P ratio
  • synthetic with equal potency to morphine
  • maintenance in rehab programs, withdrawal less severe
  • block NMDA receptors & monoaminergic reuptake transporters
  • metabolized by CYP3A4&CYP2D6, thus liver dysfunction w/overdose
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12
Q

Meperidine

A
  • strong mu agonist
  • medium O/P ratio
  • synthetic with equal potency to morphine
  • less severe resp depression, constipation, biliary colic,& urinary retention
  • strong anti-muscarinic effects - tachycardia is contraindication
  • renal failure can predispose accumulation of metabolite, normeperidine which can cause seizures
  • used for shivering
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13
Q

Codeine

A
  • Full mu agonist
  • high O/P ratio
  • used for cough suppression
  • often combined with other drugs (aspirin, acetaminophen)
  • can antagonize strong agonists
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14
Q

Hydrocodone

A
  • partial mu agonist
  • medium O/P ratio
  • cough suppression
  • often combined with other drugs
  • can antagonize strong agonists
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15
Q

Loperamide

A
  • possibly good for peripheral neuropathic pain because of actions at mu opioid receptors while lacking CNS effects
  • used for anti-diarrhea
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16
Q

Tramadol

A
  • very weak opioid agonist
  • inhibits serotonin and norepinephrine reuptake
  • useful to treat chronic pain
  • avoid issues with tolerance
  • decreases seizure threshold and risk for serotonin syndrome
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17
Q

Buprenorphine

A
  • kappa antagonist and partial mu agonist
  • sublingual route is preferred to avoid 1st pass
  • long acting, slow dissociation from mu receptors
  • resistant to naloxone reversal
  • added with Naloxone as a maintenance program for heroin addicts, as effective as methadone in detox from opioids
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18
Q

Butorphanol

A
  • kappa-opioid agonist and partial mu-opioid agonist
  • causes withdrawal symptoms
  • treats severe pain, greater sedation than buprenorphine
  • not easily reversed with naloxone
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19
Q

Dextromethorphan

A
  • used for cough suppression

- free of addictive properties and leads to less constipation than codeine

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20
Q

Isoflurane

A
  • medium rate of onset and recovery, declining use
  • potentiate GABA-A and glycine receptors, K+ channels
  • inhibit glutamatergic ionotropic receptors and neuronal nicotinic AChR’s
  • decreased peripheral resistance, decreased O2 consumption, resp depression, nausea/vomiting, decreased metabolic rate, increased cerebral flow and IC pressure, decrease blood flow
  • can cause malignant hyperthermia
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21
Q

Nitrous Oxide

A
  • rapid rate of onset and recovery
  • incomplete anesthetic, used as combo
  • blocks NMDA receptor mediated synaptic transmission in spinal cord
  • decrease myocardial function, increase sympathetic outputs, nausea/vomiting, increase cerebral flow and ICP, decrease blood flow
  • may cause malignant hyperthermia, treat with dantrolene
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22
Q

Midazolam

A
  • benzo, facilitate GABA-A
  • used as adjuncts prior to anesthesia to produce anxiolysis, amnesia, sedation
  • water soluble, given IV, no venous irritation, rapid onset, shorter duration of action
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23
Q

Thiopental

A
  • barbs
  • lipophilic agent that rapidly enters and depresses CNS
  • ultra-short acting
  • facilitates GABA-A
  • used during induction of anesthesia and deep sedation
  • decreases cerebral metabolism and blood flow (lowers ICP)
  • nausea, vomiting, decreases CV resistance
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24
Q

What are 4 good analgesics?

A
  • Nitrous oxide
  • Fentanyl
  • Ketamine
  • Dexmetomidine
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25
Q

Propofol

A
  • potentiates GABA-A receptors, used for induction and maintenance
  • onset and recovery are rapid
  • used often for conscious sedation
  • resp depression, decrease peripheral resistance, decrease ICP, antiemetic
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26
Q

Etomidate

A
  • potentiates GABA-A receptor
  • use for induction in pts with hypotension
  • minimal resp depression, minimal CV depression, vomiting, pain with injection, myoclonus, decrease plasma levels of hydrocortisone
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27
Q

Ketamine

A
  • PCP analog, blocks NMDA receptors
  • dissociative anesthesia, catatonia, amnesia and analgesia without loss of consciousness
  • only IV that produces CV stimulation, minimal effects on resp, increases ICP
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28
Q

Dexmetomidine

A
  • short term sedation of intubated and ventilated ICU patients
  • Alpha2-adrenergic receptor agonist
  • analgesia produced by activation of these receptors in spinal cord
  • hypnosis produced by activation of these receptors in locus coeruleus
  • little effect on resp, decreases cerebral blood flow
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29
Q

L-DOPA/Carbidopa (Sinemet)

A
  • L-Dopa is precursor of dopamine, but can cross BBB
  • Carbidopa enhances bioavailability of L-DOPA, prolongs 1/2 life
  • causes nausea by stimulation of D2 receptors in area postrema, tachycardia, nightmares/hallucinations, may produce dyskinesia after long-term treatment
  • contraindicated in: psychotic pts, pts with CV disease
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30
Q

COMT inhibitors (Entacapone)

A
  • inhibition of COMT enhances amount of L-dopa available for CNS, increases bioavailability
  • blocks metabolism to 3-0-methyldopa
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31
Q

Selegiline,Rasagiline, Tranylcypromine, phenelzine, isocarboxid

A
  • Selegiline=specific MAO-B inhibitor
  • nonspecific MAO inhibition increases neurotransmitter levels (NE,5HT,DA)
  • slows metabolism of Dopamine in CNS
  • used in early PD stages prior to L-DOPA or with it
  • used for atypical depression, anxiety
  • may cause CNS stimulation, contraindicated with SSRIs, TCAs, dextromethorphan (serotonin syndrome)
32
Q

Dopamine receptor agonists (Ropinerole,Pramipexole)

A
  • do not depend of nigrostraital dopamine neuron function, bind directly to dopamine receptors
  • longer duration of action, delay need for L-DOPA
  • not as effective as L-DOPA to alleviate symptoms
  • Ropinirole=D2 receptor agonist, causes nausea, orthostatic hypotension, hallucinations
33
Q

Anticholinergics (Benztropine, Trihexyphenidyl)

A
  • Thought to restore ACh:DA balance in corpus striatum
  • anti-Parkinson action
  • parasympathetic side effects
  • used to treat tremor, little effect on bradykinesia
34
Q

Amantadine

A
  • antiviral agent provides mild relief to PD symptoms
  • anticholinergic properties, releases DA, NMDA antagonist
  • causes dizziness, lethargy, sleep disturbances
35
Q

Donepezil (Aricept)

A
  • AChE inhibitor
  • use for mild,moderate,severe dementia/Alzheimer’s
  • decrease appetite, muscle cramps
36
Q

Rivastigmine (Exelon patch)

A
  • AChE inhibitor, BuChE inhibitor
  • mild,moderate dementia
  • decrease appetite, dizziness, nausea, diarrhea
37
Q

Galantamine (Reminyl)

A
  • AChE inhibitor, possible allosteric modulator nACh a7
  • decrease appetite, dizziness
  • mild, moderate dementia
38
Q

Tacrine (Cognex)

A
  • AChE inhibitor
  • decrease appetite, elevated transaminase
  • mild, moderate dementia
39
Q

Memantine (Namenda)

A
  • Glutamate NMDA inhibitor
  • use for moderate or severe dementia
  • headache, confusion, dizziness
40
Q

Phenobarbital, pentobarbital, thiopental, secobarbital

A
  • GABA-A action by increasing duration of Cl channel opening
  • sedative for anxiety, seizures, insomnia
  • respiratory and CV depression, CNS depression, dependence, drug interactions, overdose treatment only supportive care
  • alters sleep cycle
41
Q

Diazepam, lorazepam, triazolam, temazepam, alprazolam, chlordiazepoxide

A
  • GABA-A action by increasing frequency of Cl channel opening
  • decrease REM sleep, alter sleep cycle
  • most are long acting except alprazolam, triazolam, oxazepam
  • anxiety, eclampsia, seizures, sleepwalking, anesthetic, hypnotic
  • dependence, additive with EtOH, treat overdose with Flumazenil
42
Q

Zolpidem, Zaleplon, esZopiclone

A
  • act via BZ subtype of GABA receptor, less sleep cycle effect
  • reverse with flumazenil
  • use for insomnia
  • cause ataxia, headache, confusion, short duration because metabolized by liver, less dependence risk
43
Q

Carbamazepine

A
  • blocks Na channels
  • 1st line for trigeminal neuralgia
  • use for partial and tonic-clonic seizures
  • causes diplopia, ataxia, blood dyscrasias, liver toxicity, teratogenic, Steven-Johnson syndrome
44
Q

Ethosuximide

A
  • blocks thalamic T-type Ca channels
  • use for absence seizures
  • fatigue, GI distress, headache, itching, Steven Johnson syndrome
45
Q

Gabapentin

A
  • inhibits high voltage activated Ca channels, GABA analog
  • use for partial seizures, peripheral neuropathy, postherpetic neuralgia
  • causes sedation, ataxia
46
Q

Lamotrigine

A
  • blocks voltage gated Na channels, inhibits glutamate release
  • use for partial, tonic-clonic, and absence seizures
  • may cause SJ syndrome
47
Q

Phenobarbital

A
  • increases GABA-A action
  • use for partial, tonic-clonic, status epilepticus, 1st line in neonates
  • may cause sedation, tolerance, dependence, cardiorespiratory depression
48
Q

Phenytoin, fosphenytoin

A
  • blocks Na channels
  • use for partial, tonic-clonic, status epilepticus
  • causes P450 induction, hirsutism, enlarged gums, nystagmus, teratogen, osteopenia, neuropathy, inhibited folate absorption, SLE-like syndrome
  • toxicity causes diplopia, ataxia, sedation
49
Q

Tiagabine

A
  • increases GABA by inhibiting reuptake

- use for partial seizures

50
Q

Topiramate

A
  • blocks Na channels, increases GABA action
  • partial seizures, tonic-clonic,migraines
  • causes sedation, mental dulling, kidney stones, glaucoma, weight loss
51
Q

Valproic Acid

A
  • increases Na channel inactivation, increases GABA concentration
  • use for partial, tonic-clonic, absence seizures, bipolar disorder, migraines, myoclonic seizures
  • GI distress, hepatotoxicity, pancreatitis,neural tube defects, tremor, contraindicated for pregnancy
52
Q

Vigabatrin

A
  • increases GABA, irreversible transaminase inhibitor
  • use for partial seizures
  • may cause permanent vision loss
53
Q

Suvorexant

A
  • orexin receptor antagonist
  • use for insomnia
  • cause CNS depression, headache, dizziness, URI, contraindicated in narcoleptics, pts with liver disease
54
Q

Ramelteon

A
  • melatonin receptor agonist, binds MT1 and MT2 in suprachiasmatic nucleus
  • use for insomnia
  • causes dizziness, fatigue, headache, no dependence
55
Q

Sumatriptan

A

5-HT agonist, inhibit trigeminal nerve activation

  • use for acute migraines, cluster headache attacks
  • coronary vasospasm, contraindicated in patients with CAD or Prinzmetal angina
56
Q

Amitriptyline, nortriptyline, imipramine, doxepin, amoxapine

A
  • tricyclic antidepressants
  • inhibit 5HT and NE uptake
  • use for major depression, OCD, peripheral neuropathy, migraines, nocturnal enuresis
  • may cause convulsions, coma, cardiotoxicity, resp depression, contraindicated in the elderly
57
Q

Venlafaxine, desvenlafaxine, duloxetine, levomilnacipran, milnacipran

A
  • SE-NE reuptake inhibitors
  • SNRIs inhibit 5HT and NE reuptake
  • use for depression, anxiety disorder, diabetic neuropathy
  • increase BP, stimulant effects, sedation, nausea
58
Q

Fluoxetine, fluvoxamine, paroxetine, sertraline, escitalopram, citalopram

A
  • SSRIs, inhibit 5HT reuptake
  • use for depression, anxiety disorder, panic disorder, OCD, bulimia, PTSD, premature ejaculation, premenstrual dysphoric disorder
  • fewer than TCAs, cause GI distress, sexual dysfunction
59
Q

Trazodone

A
  • blocks 5HT2A/2C, alpha1 Adrenergic and H1 receptors
  • used for insomnia, and high doses needed for antidepressant
  • toxicity causes sedation, nausea, postural hypotension, male specific side effects
  • use promotes sleep onset and maintenance
  • SERT inhibition could help avoid the tolerability issues
60
Q

Clonidine and Guanfacine

A
  • antihypertensive,alpha 2-Adrenoreceptor agonist
  • used for hypertension and ADHD
  • dry mouth, sedation, weakness, dizziness, constipation, paresthesia, dermatitis, hypotension
61
Q

Methylphenidate (Ritalin, Metadate)

A
  • DAT blocker
  • increases extracellular DA/NE by blocking reuptake
  • use for treatment of narcolepsy and ADHD
62
Q

Dextroamphetamine (Adderall)

A
  • Isomer of amphetamine, potent CNS stimulator

- treat narcolepsy and ADD

63
Q

Modafinil

A
  • psychostimulant developed for narcolepsy
  • increases DA and NE by blocking transporters
  • lower addictive potential
  • rarely can cause SJ syndrome, TEN, and DRESS
64
Q

Atomoxetine

A
  • SNRI and nonstimulant drug approved for ADHD
  • little effect on CV
  • used for ADHD when psychostimulants are not an option
  • nausea, anorexia, headache, ED, urinary dysfunction, dry mouth, vomiting, abdominal pain
  • can increase BP and HR, avoid in pts with closed angle glaucoma
65
Q

Bupropion

A
  • antidepressant drug
  • inhibitor of neuronal uptake of NE, also some SE and DA reuptake
  • avoid in pts on MAOIs
  • used for neuropathic pain, aide for smoking cessation
  • headache, insomnia, sedation, agitation, potential for seizures, sweating, increased HR, confusions, delusions, paranoia, suicidal thoughts
66
Q

Buspirone

A
  • partial 5-HT1A agonist
  • use for generalized anxiety
  • reduces and delays REM sleep
  • tolerance development is minimal, little or no rebound anxiety
67
Q

Chloral hydrate

A
  • sedative-hypnotic adjunct to analgesics

- minor effects on REM

68
Q

Zolpidem

A
  • short-acting, fewer amnesic effects, does not affect sleep architecture
  • increases slow wave sleep
  • additive with ethanol
  • increase GABA activity
69
Q

Doxepin

A
  • sedating tricyclic drug
  • originally for nerve pain, antidepressant and anxiolytic, insomnia
  • sleep maintenance and sleep duration but not initiation
  • contraindicated in narrow angle glaucoma and urinary retention or pts on MAOIs
  • antimuscarinic side effects
70
Q

Sodium oxybate and Gamma hydroxybutyrate

A
  • controlled substance because of abuse
  • can cause cataplexy seizures, trouble breathing, loss of alertness, coma and death
  • used to treat narcolepsy
71
Q

What two drugs are used for restless leg syndrome?

A

Gabapentin and ropinrole

72
Q

Tasimelteon

A
  • melatonin agonist
  • acts at MT1 and MT2
  • side effects are headaches, URI, increase ALT
73
Q

Haloperidol, pimozide, trifluoperazine, fluphenazine, thioridazine, chlorpromazine

A

-Typical antipsychotics
-D2 antagonist, increase cAMP
-use for schizophrenia, psychosis, bipolar, delirium, Tourette, HD, OCD
-High potency: Tri, Fl, H (try to fly high)
-Low potency: Cl, Thi (Cheating thieves are low)
-lipid soluble, dyslipidemia, sedation, orthostatic hypotension
ADAPT: acute dystopia, akathisia, Parkinsonism, tardive dyskinesia

74
Q

Aripiprazole, asenapine, clozapine, olanzapine, quetiapine, iloperidone, paliperidone, risperidone, lurasidone, ziprasidone

A
  • atypical antipsychotics
  • most are D2 antagonists *aripiprazole -D2 partial agonist
  • use for schizophrenia, bipolar, OCD, anxiety, depression, mania, Tourette
  • all prolong the QT interval, “pines” cause metabolic syndromes, clozapine - agranulocytosis, risperidone - hyperprolactinemia
75
Q

Lithium

A
  • mood stabilizer for bipolar disorder, treats acute manic episodes
  • LiTHIUM: low thyroid, heart (Epstein anomaly), Insipidus (nephrogenic diabetes), Unwanted Movements

Drugs/Immuno (9 decks)

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