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
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
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
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
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
6
Q
Gabapentin
A
- antiepileptic used for MS patients
- GABA analog works on Ca2+ receptors
7
Q
Progabide
A
-GABA-A and GABA-B agonist with active metabolites
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
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
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
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
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
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
14
Q
Hydrocodone
A
- partial mu agonist
- medium O/P ratio
- cough suppression
- often combined with other drugs
- can antagonize strong agonists
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
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
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
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
19
Q
Dextromethorphan
A
- used for cough suppression
- free of addictive properties and leads to less constipation than codeine
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
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
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
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
24
Q
What are 4 good analgesics?
A
- Nitrous oxide
- Fentanyl
- Ketamine
- Dexmetomidine
25
Propofol
- 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
26
Etomidate
- 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
27
Ketamine
- 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
28
Dexmetomidine
- 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
29
L-DOPA/Carbidopa (Sinemet)
- 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
30
COMT inhibitors (Entacapone)
- inhibition of COMT enhances amount of L-dopa available for CNS, increases bioavailability
- blocks metabolism to 3-0-methyldopa
31
Selegiline,Rasagiline, Tranylcypromine, phenelzine, isocarboxid
- 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
Dopamine receptor agonists (Ropinerole,Pramipexole)
- 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
Anticholinergics (Benztropine, Trihexyphenidyl)
- Thought to restore ACh:DA balance in corpus striatum
- anti-Parkinson action
- parasympathetic side effects
- used to treat tremor, little effect on bradykinesia
34
Amantadine
- antiviral agent provides mild relief to PD symptoms
- anticholinergic properties, releases DA, NMDA antagonist
- causes dizziness, lethargy, sleep disturbances
35
Donepezil (Aricept)
- AChE inhibitor
- use for mild,moderate,severe dementia/Alzheimer’s
- decrease appetite, muscle cramps
36
Rivastigmine (Exelon patch)
- AChE inhibitor, BuChE inhibitor
- mild,moderate dementia
- decrease appetite, dizziness, nausea, diarrhea
37
Galantamine (Reminyl)
- AChE inhibitor, possible allosteric modulator nACh a7
- decrease appetite, dizziness
- mild, moderate dementia
38
Tacrine (Cognex)
- AChE inhibitor
- decrease appetite, elevated transaminase
- mild, moderate dementia
39
Memantine (Namenda)
- Glutamate NMDA inhibitor
- use for moderate or severe dementia
- headache, confusion, dizziness
40
Phenobarbital, pentobarbital, thiopental, secobarbital
- 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
Diazepam, lorazepam, triazolam, temazepam, alprazolam, chlordiazepoxide
- 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
Zolpidem, Zaleplon, esZopiclone
- 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
Carbamazepine
- 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
Ethosuximide
- blocks thalamic T-type Ca channels
- use for absence seizures
- fatigue, GI distress, headache, itching, Steven Johnson syndrome
45
Gabapentin
- inhibits high voltage activated Ca channels, GABA analog
- use for partial seizures, peripheral neuropathy, postherpetic neuralgia
- causes sedation, ataxia
46
Lamotrigine
- blocks voltage gated Na channels, inhibits glutamate release
- use for partial, tonic-clonic, and absence seizures
- may cause SJ syndrome
47
Phenobarbital
- increases GABA-A action
- use for partial, tonic-clonic, status epilepticus, 1st line in neonates
- may cause sedation, tolerance, dependence, cardiorespiratory depression
48
Phenytoin, fosphenytoin
- 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
Tiagabine
- increases GABA by inhibiting reuptake
| - use for partial seizures
50
Topiramate
- blocks Na channels, increases GABA action
- partial seizures, tonic-clonic,migraines
- causes sedation, mental dulling, kidney stones, glaucoma, weight loss
51
Valproic Acid
- 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
Vigabatrin
- increases GABA, irreversible transaminase inhibitor
- use for partial seizures
- may cause permanent vision loss
53
Suvorexant
- orexin receptor antagonist
- use for insomnia
- cause CNS depression, headache, dizziness, URI, contraindicated in narcoleptics, pts with liver disease
54
Ramelteon
- melatonin receptor agonist, binds MT1 and MT2 in suprachiasmatic nucleus
- use for insomnia
- causes dizziness, fatigue, headache, no dependence
55
Sumatriptan
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
Amitriptyline, nortriptyline, imipramine, doxepin, amoxapine
- 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
Venlafaxine, desvenlafaxine, duloxetine, levomilnacipran, milnacipran
- SE-NE reuptake inhibitors
- SNRIs inhibit 5HT and NE reuptake
- use for depression, anxiety disorder, diabetic neuropathy
- increase BP, stimulant effects, sedation, nausea
58
Fluoxetine, fluvoxamine, paroxetine, sertraline, escitalopram, citalopram
- 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
Trazodone
- 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
Clonidine and Guanfacine
- antihypertensive,alpha 2-Adrenoreceptor agonist
- used for hypertension and ADHD
- dry mouth, sedation, weakness, dizziness, constipation, paresthesia, dermatitis, hypotension
61
Methylphenidate (Ritalin, Metadate)
- DAT blocker
- increases extracellular DA/NE by blocking reuptake
- use for treatment of narcolepsy and ADHD
62
Dextroamphetamine (Adderall)
- Isomer of amphetamine, potent CNS stimulator
| - treat narcolepsy and ADD
63
Modafinil
- psychostimulant developed for narcolepsy
- increases DA and NE by blocking transporters
- lower addictive potential
- rarely can cause SJ syndrome, TEN, and DRESS
64
Atomoxetine
- 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
Bupropion
- 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
Buspirone
- partial 5-HT1A agonist
- use for generalized anxiety
- reduces and delays REM sleep
- tolerance development is minimal, little or no rebound anxiety
67
Chloral hydrate
- sedative-hypnotic adjunct to analgesics
| - minor effects on REM
68
Zolpidem
- short-acting, fewer amnesic effects, does not affect sleep architecture
- increases slow wave sleep
- additive with ethanol
- increase GABA activity
69
Doxepin
- 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
Sodium oxybate and Gamma hydroxybutyrate
- controlled substance because of abuse
- can cause cataplexy seizures, trouble breathing, loss of alertness, coma and death
- used to treat narcolepsy
71
What two drugs are used for restless leg syndrome?
Gabapentin and ropinrole
72
Tasimelteon
- melatonin agonist
- acts at MT1 and MT2
- side effects are headaches, URI, increase ALT
73
Haloperidol, pimozide, trifluoperazine, fluphenazine, thioridazine, chlorpromazine
-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
Aripiprazole, asenapine, clozapine, olanzapine, quetiapine, iloperidone, paliperidone, risperidone, lurasidone, ziprasidone
- 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
Lithium
- mood stabilizer for bipolar disorder, treats acute manic episodes
- LiTHIUM: low thyroid, heart (Epstein anomaly), Insipidus (nephrogenic diabetes), Unwanted Movements
