Neuro Drugs Flashcards

(51 cards)

1
Q

TCA: Despiramine and Nortriptyline

A

MOA: block reuptake of NE

- Treat depression

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

TCA: Imipramine, Amitryptyline

A

MOA: block NE/5HT reuptake

- Treat depression

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Dual-action: Venlafaxine, Desvenlafaxine

A

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

- Treat depression

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Anticonvulsants: Valproic acid and Sodium Valproate

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

- Tx for seizures

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Anticonvulsants: Carbamazepine

A
  • Used for prophylactic tx of bipolar disorder

- Tx for seizures

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Lurasidone

A

MOA: D2 and 5HT2A antagonist; precise unknown

  • Used to treat major depression in bipolar patients
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Benzodiazepines

A

Diazepam, Lorazepam, Flurazepam, Triazolam, Alprazolam

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

  • Treats anxiety
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Flumazenil

A

MOA: reverses effects of benzos, zolidem, zapelon

  • Used to treat benzodiazepine OD
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Propanolol

A

MOA: blocks autonomic signs

  • Used to treat anxiety
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Atomoxetine (Strattera)

A

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

  • Used to treat ADHD
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
What are some features of sevoflurane?
- MAC = 1.71 - High potency, rapid onset (5-10 minutes) and recovery - Commonly used for day surgery
26
Nitrous Oxide
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
What does 'second gas effect' mean?
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
Barbiturates (as anesthetics)
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
Benzodiazepines (as anesthetics)
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
Propofol
- Rapid induction (50 seconds); recovery (4-8 minutes) - May result in pain at injection site - Respiratory apnea (22-45%)
31
Ketamine (as an anesthetic)
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
Etomidate
- Used as a general anesthetic for emergency intubations | - Has a safe CV risk profile
33
Opioids: fentanyl, sufentanyl (used for general anesthesia)
- CNS effects: hemodynamic instability | - Respiratory airway must be maintained artificially as it may be depressed post-operatively
34
Carbamazepine
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
Ethosuximide
MOA: Reduces low threshold Ca2+ currents (T-type) in thalamic neurons - Treats absence seizures
36
Levetiracetam
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
Phenytoin
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
Tiagabine
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
Topiramate
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
Valproate
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
What are some treatments for methanol and ethylene glycol poisoning?
Administer: - Ethanol - Fomepizole - Bicarbonate - acidify urine to promote excretion (methanol)
42
How does one treat an amphetamine OD?
Give antipsychotics (FGAs or SGAs) and/or acidify the patient's urine if have acute OD
43
Pentamidine
MOA: Binds DNA minor groove, mitochondrial as well as nuclear genome replication is affected • Effective against: Trypanosoma brucei
44
Suramin
* Unknown mechanism, highly toxic | * Effective against: Trypanosoma brucei
45
Melarsaprol
• An arsenical, crosses BBB, so will treat stage 2 T. brucei infection. Super toxic!!!!
46
Eflornithine
MOA: ornithine decarboxylase inhibitor, crosses BBB, - Treats stage 2 T. brucei infection.
47
Nifurtimox and Benznidazole
MOA: oxidative stress, impairment of membrane potential • Trypanosoma cruzi or T. brucei co-treatment with eflornithine
48
Sodium Stibugluconate, Meglumine antimoniate
MOA: targets glycolysis and fatty acid beta-oxidation in mitochondria - Treats leishmanial infections
49
Miltefosine
MOA: unknown - Treats leishmanial infections
50
Sulfadiazine + Pyrimethamine
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
Albendazole
MOA: microtubule inhibitor | - Treats: Taenia solium- cysticercosis, Echinococcus granulosis, Toxocara cati roundworms, tapeworms