Term
|
Definition
| -Levodopa/Carbidopa (Sinemet) |
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Term
| Levodopa/Carbidopa (Sinemet) |
|
Definition
-Dopamine's immediate precursor (L-Dopa)
-Readily transported across BBB
-prevents conversion of LDopa to dop. in the periphery
-allows L-Dopa to reach CNS in bigger amts.
-reduces rigidity and tremors
-causes "On/Off" Phenomenon |
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Term
| Adverse effects of Levodopa/Carbidopa (Sinemet) |
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Definition
-CNS: dyskinesia, visual/audio hallucinations
-Peripheral: N/V, Tachy, Hypo, mydriasis, brown saliva/urine |
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Term
| Levodopa/Carbidopa (Sinemet) interaction drugs |
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Definition
-Pyridoxine (B6): increases breakdown
-MAOI: increase catecholamine stim = HTN crisis
-Antipsychotic agents: parkinsonian syndr. |
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Term
| Dopamine Receptor Agonists |
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Definition
-Pramipexole (Mirapex)
-Ropinirole (Requip) |
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Term
Pramipexole (Mirapex)
Ropinirole (Requip) |
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Definition
-Dopamine Receptor Agonists
-req. frequent dosing
-eliminated renally
-Adverse Effects: dyskinesia, orthostatic hypo, hallucination, somnolence, dizziness |
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Term
|
Definition
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Term
|
Definition
-MAO-B inhibitors
-inhibits breakdown of dopamine (MAO-B)
-Does NOT inhibit MAO-A
-improves motor function in parkinson's
-Seligine forms Amphetamine at metabolite, VERY limited use |
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Term
|
Definition
-Tolcapone (Tasmar)
-Entacapone (Comtan) |
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Term
Tolcapone (Tasmar)
Entacapone (Comtan) |
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Definition
-COMT Inhibitors
-Decrease the peripheral metabolism of L-Dopa
-Reduces "off" periods
-used in combo w/ levodopa/carbidopa
-Have to monitor Liver Enzymes b/c Tolcapone can cause fulminant hepatic necrosis |
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Term
|
Definition
-Nondopaminergic agents
-helpful for levodopa-induced dyskinesia
-blockade of excitatory NMDA receptors |
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Term
Benztropine (Cogentin)
Trihexyphenidyl |
|
Definition
-Antimuscarinic agents
-Adjuvant role in reducing tremor
-anticholinergic side effects |
|
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Term
| Typical Antipsychotic Agents (Low Potency) |
|
Definition
-Chlorpromazine (Thorazine)
-Procholorperazine (Compazine)
-Promethazine (Phengren)
Thioridazine (Mellaril) |
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Term
|
Definition
-Aripiprazole (Abilify)
-Clozapine (Clozaril)
-Olanzapine (Zyprexa)
-Quetiapine (Seroquel)
-Risperidone (Risperdal)
-Ziprasidone (Geodon) |
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Term
| Typical Antipsychotics (High Potency) |
|
Definition
-Fluphenazine (Prolixin)
-Haloperidol (Haldol)
-Pimozide (Orap)
-Thiothixene (Navaine) |
|
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Term
| Typical Antipsychotics Mechanism |
|
Definition
-block dopamine receptors in brain and periphery
-antipsychotic activity involves antagonism of mesolimbic system |
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Term
|
Definition
-Block dopamine receptors in brain and periphery (lower affinity for D2)
-antipsychotic activity involves antag of mesolimbic system
-unique action through inhibition of serotonin receptors |
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Term
|
Definition
-reduce positive symptoms of halluc and delusions
-Negative s/s of blunted affect, anhedonia, apathy, and impaired attention not as responsive to typical antipsychotics
-actions take several weeks |
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Term
| Antipsychotic Therapeutic Uses |
|
Definition
-Schizophrenia
-Prevention of severe N/V
-Tranquilizers
-Chronic p! w/severe anxiety
-Intractable hiccups
-Motor and phonic tics of Tourette's disorder |
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Term
|
Definition
-GABA meatab inhibitor
-competitive inhibitor of GABA transporters in neurons and glia
-Selective for GAT-1
-inc GABA conc. for receptor binding
-enhances inhibitory activity
-anticonvulsant
-used for Epilepsy
-metab by CYP450 enzymes(liver) |
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Term
|
Definition
GABA Metab Inhibitor
-irreversibly inhibits GABA-transaminase
-inhibition results in inc levels of GABA in CNS
-used for Epilepsy
-eliminated unchanged in urine
-BLACK BOX WARNING: permanent vision loss! |
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Term
| GABA Metabolism Inhibitors |
|
Definition
-Vigabatrin (Sabril)
-Tiagabine (Gabitril) |
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Term
|
Definition
-most widely used anxiolytic drugs
-targets GABA-A (high aff/selective)
-results in freq opening of adjacent chloride channels = enhanced hyperpol=further inhibits neuronal firing
-used as anticonvulsant, anterograde amnesia, sedative, mm relaxant, alcohol withdrawals, sleep disorders |
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Term
Short Acting Benzo's
(3-8 hours) |
|
Definition
-Midazolam = preanesthetic, IV general anesthetic
-Clorazepate = anxiety disorders, seizures
-Triazolam = insomnia |
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Term
Intermediate Acting Benzo's
(11-20 Hours) |
|
Definition
-Alprazolam = anxiety, phobias
-Lorazepan = anxiety, epilepsy, IV general anesthetic
-Estazolam = insomnia
-Temazepam = insomnia |
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|
Term
Long Acting Benzo's
(1-3 days) |
|
Definition
-Chlordiazepoxide = anxiety, EtOH withdrawl
-Clonazepam = seizures
-Diazepam = anxiety, epilepsy, mm relaxant, IV anesth, EtOH w/drawal
-Flurazepam = insomnia
-Quazepam = insomnia |
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Term
|
Definition
Benzo ANTAGonist (GABA-A)
-rapidly reverses benzo effects
-IV only -Short half life (1hour)
-may precipitate withdrawal or cause seizures |
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Term
|
Definition
Hypnotic Agent
-used to treat insomnia
-no anticonvulsant/mm relaxing properties
-rapid onset/shorter half life (2-3hrs)
-metab by CYP450 (liver)
-causes severe drowsiness that can last |
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Term
|
Definition
Hypnotic Agent
-similar to Zolpidem
-treat insomnia
-fewer residual effects on psychomotor and cognitive funct
-rapid elim
-half life= <1hour |
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Term
|
Definition
Anxiolytic Agent
-used for generalized anxiety
-mediated through serotonin recept.
-lacks mm relaxant and anticonvulsant props
-minimal sedation, dependence unlikely
-slow onset of action |
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Term
|
Definition
Hypnotic Agent
-treat insomnia -GABA-A AGONIST
-rapidly absorbed, extensively metab
-6 hour half life |
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Term
|
Definition
Hypnotic Agent
-antihistamine and antiemetic
-low tendency for habituation
-used for allergice reaction but can be used to treat insomnia |
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Term
Ultrashort Acting Barbituates
(5-15 minutes) |
|
Definition
-Thiopental = Anesth. induction, emergency seizure Tx
-Methohexital = Anesth. induction and short term maintenance |
|
|
Term
Short Acting Barbituates
(3-8 hours) |
|
Definition
-Pentobarbital
-Secobarbital
-Amobarbital
= insomnia, preop sedation, emerg seizure Tx |
|
|
Term
Long Acting Barbituates
(days) |
|
Definition
| Phenobarbital - Tx of seizures, epilepsy |
|
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Term
|
Definition
-Barbituate (short acting 1-4 hrs)
-suppression of neuronal activity
-inc efficacy of GABA by inc open time of Cl channel
-direct GABA-A activation
-noncompetitive ANTAG at AMPA recep |
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Term
|
Definition
-Barbituate (Long acting days)
-minimal neuronal suppresion
-inc efficacy of GABA-A by inc open time of Cl channels --> dec. excitability
-noncompetitve ANTAG at AMPA rec
-Used for: partial Seizures (simple), tonic clonic, absence seizures |
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Term
|
Definition
GABA-A AGONIST
-Tx of spasticity assoc w/motor neuron diseases (MS)
-modest vol of distribution
-does not cross BBB
-half life = 5 hours
-renal clearance
-can give an intrathecal line of it
-withdrawal can cause hyperspasticity or Rhabdo |
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Term
|
Definition
-CNS depressant produces sedation and hypnosis
-inc GABA-A Cl channels and inhibits excitatory effects of glutamate at NMDA receptors
-metab by liver
-synergistic w/ sedatives
-Benzo's used to tx withdrawals |
|
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Term
|
Definition
used to treat alcoholism
-makes patient feel sick when they drink but have to take chronically |
|
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Term
|
Definition
Noncompetitive NMDA receptor ANTAGonist
-may slow Ca2+ influx and nerve damage
-used in Tx of Alzheimer's
-min metab via liver, excreted mainly in urine |
|
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Term
|
Definition
Noncompetitive NMDA receptor ANTAGonist
-blocks glutamate's effect=inhibition
-used in combo with levodopa to tx dyskinesias in parkinson disease
-excreted in urine |
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Term
| Serotonin Storage Inhibitors |
|
Definition
Dextroamphetamine/ Amphetamine (Adderall)
-Methylphenidate (Ritalin)
-Modafinil (Provigil) |
|
|
Term
Serotonin Degradation Inhibitor
(MAOI's) |
|
Definition
-Phenelzine (Nardil)
-Tranylcypromine (Parnate) |
|
|
Term
| Serotonin Reuptake Inhibitors |
|
Definition
Tricyclic Antidepressants
-Imipramine (Toranil)
-Amitriptyline (Elavil)
-Nortriptyline (Pamelor) |
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|
Term
| Selective Serotonin Reuptake Inhibitors (SSRI's) |
|
Definition
-Fluoxetine (Prozac)
-Citalopram (Celexa)
-Paroxetine (Paxil)
-Sertraline (Zoloft)
-Escitalopram (Lexapro) |
|
|
Term
| Serotonin-Norepinephrine Reuptake Inhibitors (SNRI's) |
|
Definition
-Venlafaxine (Effexor)
-Desvenlafaxine (Pristiq)
-Duloxetine (Cymbalta) |
|
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Term
|
Definition
-Bupropion (Wellbutrin or Zyban)
-Mirtazapine (Remeron)
-Trazodone (Desyrel) |
|
|
Term
| Bupropion (Wellbutrin or Zyban) |
|
Definition
-Inhibits DA & NE reuptake' min 5HT effects
-used for major depressive disorder and smoking cessation |
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Term
|
Definition
Atypical Antidepressant
-Inhibits 5HT and A andrenergic receptors
-Increase 5HT/NE neurotransmission
-used for major depressive disorder, appetite stim |
|
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Term
|
Definition
Atypical Antidepressant
-Inhibits 5HT reuptake transporter and blocks 5HT2a receptors
-used for insomnia, major depressive disorder |
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Term
| Serotonin Receptor Agonists |
|
Definition
Triptans:
-Sumatriptan (Imitrex)
-Zolmitriptan (Zomig)
-Rizatriptan (Maxalt)
Activate 5HT1D and 1B receptors
-->vasoconstr of intracranial vasc
--used for migraines |
|
|
Term
| Serotonin Receptor Antagonist |
|
Definition
5HT3 receptor antag
-Ondansetron (Zofran)
-Granisetron (Kytril)
-Dolasetron (Anzemet)
-Anti emetic: used for cancer chemo and refractory nausea |
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Term
|
Definition
| Lithium Carbonate (Lithobid or Eskalith) |
|
|
Term
Dextroamphetamine/ Amphetamine (Adderall)
-Methylphenidate (Ritalin)
-Modafinil (Provigil) |
|
Definition
Serotonin Storage Inhibitors
-Displace 5HT from storage vesicles
-used for Atypical depression, depression in elderly, narcolepsy |
|
|
Term
-Phenelzine (Nardil)
-Tranylcypromine (Parnate) |
|
Definition
MAOI
-Inhibits breakdown of DA, 5HT, NE
-used for atypical depression, not considered 1st line therapy
-Adverse effects: HTN crisis, Serotonin syndr. |
|
|
Term
Imipramine (Toranil)
Amitriptyline (Elavil)
Nortriptyline (Pamelor) |
|
Definition
Tricyclic Antidepressants
-Inhibit reuptake of NE and 5HT from cleft by inhibiting transporters
-increase levels of 5HT/NE in cleft
-used for MDD, panic disorder, bed wetting |
|
|
Term
Fuoxetine (Prozac)
Citalopram (Celexa)
Paroxetine (Paxil)
Sertraline (Zoloft)
Escitalopram (Lexapro) |
|
Definition
SSRI's
-selectively inhibit reuptake of 5HT by inhibiting transporter
-used for MDD (1st line), panic, anxiety, OCD, PTSD |
|
|
Term
Venlafaxine (Effexor)
Desvenlafaxine (Pristiq)
Duloxetine (Cymbalta) |
|
Definition
SNRI's
-Venlaf. & Desvenl. block NE/5HT tranporters in conc dependent manner
-Duloxetine blocks NE/5HT reuptake transporters
-used for MDD, anxiety, diabetic neruo, fibromyalgia |
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Term
| Enhance Na+ Channel-Mediated Inhibition |
|
Definition
Phenytoin (Dilantin)
Carbamazepine (Tegretol)
Oxcarbazepine (Trileptal)
Lamotrigine (Lamictal) |
|
|
Term
| Inhibition of Calcium Channels |
|
Definition
Ethosuximide
Valproic Acid
Gabapentin (Neurontin) |
|
|
Term
| Enhance GABA-mediated Inhibition |
|
Definition
Benzodiazapines
Phenobarbital |
|
|
Term
|
Definition
Enhance Na+ Cahnnel-mediated inhibition
-stabilizes neuronal mem. to depol. by dec. flux of Na+ in resting/depol state
-reduces inlfux of Ca2+ during depol. & suppresses repetitive firing neurons
-reduces propagation of abnormal impulses in brain |
|
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Term
| Phenytoin (Dilantin) continued |
|
Definition
-Slow oral absorption; rapid distribution; high brain concentrations
-Highly protein bound (90%)
-CYP450 substrate and inducer
-IV administration (fosphenytoin)
-Used for: partial seizures (simple), tonic clonic seizures, epilepsy |
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Term
|
Definition
Enhance Na+ Channel-mediated inhibition
-Na+ blocker that slows recovery rt of Na+ channels from inactivated to closed
-Suppresses seizure focus and prevents rapid spread of seizure activity
-Metab by CYP450
-CYP450 Inducer; autoinduction
-Used for: partial seizures (simple/complex), tonic clonic seizures, mood stabilization |
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Term
| Oxcarbazepine (Trileptal) |
|
Definition
Enhance Na+ channell-mediated inhibition
-Na+ blocker that slows recovery rt of Na+ channels from inactivated to closed
-CYP450 inducer; NO autoinduction
-used for: partial seizures (simple/complex) |
|
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Term
|
Definition
Enhance Na+ channel-mediated inhibition
-Stabilizes neuronal mem by blocking Na+ channels & Ca2+ channels
-metab by CYP450
-Decreased by Carbamazepine/phenytoin
-increased by Valproic acid
-used for: absence seizures, tonic-clonic, mood stabilization |
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Term
|
Definition
Calcium Channel Inhbitor
-reduces low threshold T-type Ca2+ currents in voltage dependent manner
-metab by CYP450
-used for: absence seizures |
|
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Term
|
Definition
Calcium Channel Inhibitor
-Slows rate of Na+ channel recovery from inactivated state
-Limits activity of low threshold T-type Ca2+ channels
-Inc GABA production
-Metab by CYP450; enzyme inhibitor
-used for: absence seizures, tonic clonic seizures |
|
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Term
|
Definition
Calcium Channel Inhibitor
-inhibits high volt. activated Ca2+ chann
-Inc. GABA content in neurons and glia
-NOT metabolized; renally eliminated
-Used for: simple partial seizures, tonic-clonic, neuropathic pain |
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Term
|
Definition
Enhance GABA mediated inhibition
-targets GABA-A receptor and inhibits neuronal firing
-used for: epilepsy (first line), tonic clonic, infantile spasms |
|
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Term
|
Definition
-Prevents hypersynchronization of epileptiform burst firing
-Does not affect normal neuronal excitability
-renal dosing required
-Used for: partial seizures (adjunct) |
|
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Term
|
Definition
-Inhibits volt. gated Na+ channels
-Inc GABA activity
-Reduces high volt Ca2+ channels
-ANTAG AMPA
-Induced by phenytoin/carbamazepine
-Used for: partial seizures, tonic clonic, mood stabilzation |
|
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Term
|
Definition
-blocks volt gated Na+ channels
-Blocks T-type Ca2+ currents
-sulfonamide derivative
-Used for: partial epilepsy |
|
|
Term
|
Definition
-Binds to a2-d site of volt gated Ca2+
-->inhibits excitatory neurotrans release
-Renally eliminated
-Used for: Partial onset seizures |
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