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Neurological Medicine > Neuro Drugs > Flashcards

Neuro Drugs Flashcards

1
Q

TCA: Despiramine and Nortriptyline

A

MOA: block reuptake of NE

- Treat depression

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2
Q

TCA: Imipramine, Amitryptyline

A

MOA: block NE/5HT reuptake

- Treat depression

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3
Q

SSRIs: Citalopram, Escitalopram, Sertaline, Fluoxetine

A

MOA: block 5HT reuptake at all seven 5HT subtypes

- Treat depression & bipolar disorder (should never be used alone to treat though)

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4
Q

Dual-action: Venlafaxine, Desvenlafaxine

A

MOA: selective 5HT and NE reuptake inhibitor (SNRI)

- Treat depression

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5
Q

Lithium Carbonate

A

MOA: unknown, three possible:

  • Interferes with IP3 and DAG production and release
  • May uncouple receptor recognition site from GPCR by competing with Mg2+
  • May affect several cell or nuclear regulatory factors
  • Treats bipolar disorder
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6
Q

Anticonvulsants: Valproic acid and Sodium Valproate

A
  • Used for rapid-cycling of bipolar disorder (acute tx)

- Tx for seizures

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7
Q

Anticonvulsants: Carbamazepine

A
  • Used for prophylactic tx of bipolar disorder

- Tx for seizures

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8
Q

First Generation Antipsychotics: Chlorpromazine, Haloperidol

A

MOA: block all D2 receptors in limbic system –> lowers DA levels
- Used for schizophrenia (+ psychoses symptoms - nigrostriatal pathway)

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9
Q

Second Generation Antipsychotics: CROQA

A

Clozapine, Risperidone, Olanzapine, Quetiapine, Aripiprazole

MOA: blocks D2 and 5HT receptors (5HT regulates D2 release…)

  • Used for schizophrenia, bipolar disorder
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10
Q

Lurasidone

A

MOA: D2 and 5HT2A antagonist; precise unknown

  • Used to treat major depression in bipolar patients
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11
Q

Vortioxetine

A

MOA: 5HT3A and 5HT7 antagonist, 5HT1B partial agonist, 5HT1A agonist –> together this results in increases in NE, DA, and Glu transmission

  • Used to treat major depression in bipolar patients
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12
Q

Barbiturates

A

Thiopental, Pentobarbital, Phenobarbital

MOA: facilitates GABA binding to GABAa receptors to increase duration of channel opening

  • Treats anxiety and used as a general anesthetic
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13
Q

Benzodiazepines

A

Diazepam, Lorazepam, Flurazepam, Triazolam, Alprazolam

MOA: facilitates GABA binding to GABAa receptors to increase frequency of channel opening

  • Treats anxiety
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14
Q

Methylphenidate

A

Immediate: Ritalin, XR: Concerta

MOA: enhances DA release and blocks reuptake

  • Used to treat ADHD
    This drug is a sympathomimetic (stimulant) - can be abused
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15
Q

Flumazenil

A

MOA: reverses effects of benzos, zolidem, zapelon

  • Used to treat benzodiazepine OD
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16
Q

Propanolol

A

MOA: blocks autonomic signs

  • Used to treat anxiety
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17
Q

Non-benzo benzodiazepine agonists

A

Zolpidem, Zaleplon, Eszoplicone

MOA: bind to GABAa receptors, but are selective to which receptor subtypes they bind

  • Used for sleeping aids
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18
Q

Ramelteon

A

MOA: melatonin MT1 & MT2 receptor agonists; these receptors are located in suprachiasmatic nucleus (body’s master clock)

  • Used for sleeping aid
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19
Q

Amphetamines

A

(d)-amphetamine (Ritalin, Concerta)
(d,l)-amphetamine (Dexedrine, Adderall)

MOA:

  • (d & d,l): enhances DA release, blocks DA reuptake
  • (d,l only): enhances NE release
  • Used to treat ADHD
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20
Q

Atomoxetine (Strattera)

A

MOA: elevates DA levels in prefrontal cortex (not nucleus accumbens!!)

  • Used to treat ADHD
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21
Q

Eugeroics: Modafinil, Armodafinil

A

MOA: increase release of NE and DA; elevates hypothalamic histamine levels

  • Used to treat narcolepsy (once treated ADHD)

DEA schedule IV drug - low abuse potential

22
Q

Halogenated hydrocarbons: halothane, isoflurane, sevoflurane, desflurane

A

Inhaled general anesthetics

MOA: amount of undissolved drug in the blood is related to clinical effect (Henry’s law)

23
Q

What are some features of halothane?

A
  • MAC: 0.77 (most potent)
  • Rapid induction & recovery
  • Potential for hepatic toxicity due to liver metabolism
  • Can cause malignant hyperthermia - sensitizes myocardium to catecholamines
24
Q

What are some features of isoflurane?

A
  • MAC = 1.15
  • Potent, induction < 10 minutes
  • Less renal and hepatotoxicity than halothane
  • rare arrhythmias, pungent odor, potential for malignant hyperthermia
25
Q

What are some features of sevoflurane?

A
  • MAC = 1.71
  • High potency, rapid onset (5-10 minutes) and recovery
  • Commonly used for day surgery
26
Q

Nitrous Oxide

A

Inhaled general anesthetic

  • MAC = 104!!! - can’t use alone
  • Low blood solubility (rapid onset)
  • No muscle relaxing effect
  • Diffusion hypoxia if rapidly discontinued (recovery)
  • Use for second gas effect
27
Q

What does ‘second gas effect’ mean?

A

It involves use of two anesthetics. The first one (usually Nitrous oxide) is administered which is then followed by a second inhaled anesthetic which is taken up faster. This decreases the time for induction (skip over stage 2) and recovery!

28
Q

Barbiturates (as anesthetics)

A

Thiopental, methohexital, phenobarbital

MOA: facilitates GABA binding to GABAa receptors to increase the duration of channel opening

  • Rapid onset (seconds), short action (minutes)
  • Anesthetic dose is 50-75% of LD50 –> monitor patients!!!
29
Q

Benzodiazepines (as anesthetics)

A

Midazolam, Diazapam

MOA: facilitates GABA binding to GABAa receptors to increase frequency of channel opening

  • Cannot be given alone
  • Has amnestic effect
  • Less CV and respiratory depression compared to barbs
30
Q

Propofol

A
  • Rapid induction (50 seconds); recovery (4-8 minutes)
  • May result in pain at injection site
  • Respiratory apnea (22-45%)
31
Q

Ketamine (as an anesthetic)

A

MOA: NMDA glutamate agonist

  • Dissociate anesthetic = patient appears to be awake, but unaware
  • Rapid onset (1-2 min), short duration (20 min)
  • Principle drawback = emergence reactions (delerium, hallucinations)
  • Currently abused in US
32
Q

Etomidate

A
  • Used as a general anesthetic for emergency intubations

- Has a safe CV risk profile

33
Q

Opioids: fentanyl, sufentanyl (used for general anesthesia)

A
  • CNS effects: hemodynamic instability

- Respiratory airway must be maintained artificially as it may be depressed post-operatively

34
Q

Carbamazepine

A

MOA: limits firing of APs, slows recover of VG Na+ channels from inactivation

  • Used for focal, secondary generalized tonic-clonic seizures
  • Note: this drug can reduce the amount of Topiramate due to hepatic metabolism.
35
Q

Ethosuximide

A

MOA: Reduces low threshold Ca2+ currents (T-type) in thalamic neurons

  • Treats absence seizures
36
Q

Levetiracetam

A

MOA: inhibits neuronal burst firing (unknown), but possibly related to SV2A protein

  • Treats focal, both types of generalized tonic-clonic seizures; myoclonic seizures (convulsive types)
37
Q

Phenytoin

A

MOA: slows rate of recovery of VG Na+ channel from inactivation

  • Treats focal and secondary generalized tonic-clonic seizures
  • Note, rate of elimination is nonlinear - [drug] increases disproportionally as dosage increases
38
Q

Tiagabine

A

MOA: Inhibits GAT-1 (reduces GABA uptake into neurons and glia)

  • Treats focal seizures

Used as adjuvant therapy and should not be used as a monotherapy!

39
Q

Topiramate

A

MOA: reduces VG Na+ currents; activates hyperpolarizing K+ current; enhances GABAa receptor currents; limits activation of AMPA-kainate receptors (post)

  • Treats focal and generalized tonic-clonic seizures
40
Q

Valproate

A

MOA: inhibits repetitive firing by mediated VG Na+ channels; produces small reduction of T-type Ca2+ channels; increased GABA levels

  • Treats for most types of seizures!! Less effective for complex focal seizures
41
Q

What are some treatments for methanol and ethylene glycol poisoning?

A

Administer:

  • Ethanol
  • Fomepizole
  • Bicarbonate - acidify urine to promote excretion (methanol)
42
Q

How does one treat an amphetamine OD?

A

Give antipsychotics (FGAs or SGAs) and/or acidify the patient’s urine if have acute OD

43
Q

Pentamidine

A

MOA: Binds DNA minor groove, mitochondrial as well as nuclear genome replication is affected

• Effective against: Trypanosoma brucei

44
Q

Suramin

A
  • Unknown mechanism, highly toxic

* Effective against: Trypanosoma brucei

45
Q

Melarsaprol

A

• An arsenical, crosses BBB, so will treat stage 2 T. brucei infection. Super toxic!!!!

46
Q

Eflornithine

A

MOA: ornithine decarboxylase inhibitor, crosses BBB,

  • Treats stage 2 T. brucei infection.
47
Q

Nifurtimox and Benznidazole

A

MOA: oxidative stress, impairment of membrane potential

• Trypanosoma cruzi or T. brucei co-treatment with eflornithine

48
Q

Sodium Stibugluconate, Meglumine antimoniate

A

MOA: targets glycolysis and fatty acid beta-oxidation in mitochondria

  • Treats leishmanial infections
49
Q

Miltefosine

A

MOA: unknown

  • Treats leishmanial infections
50
Q

Sulfadiazine + Pyrimethamine

A

MOA: folate synthesis inhibitors, dangerous to use in pregnancy.

The macrolide Spiramycin may be more appropriate in certain pregnancy situations but not approved in US so must acquire from FDA

• Treats: Toxoplasmosis

51
Q

Albendazole

A

MOA: microtubule inhibitor

- Treats: Taenia solium- cysticercosis, Echinococcus granulosis, Toxocara cati
roundworms, tapeworms

Neurological Medicine (5 decks)

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