Neuro Drugs Flashcards
TCA: Despiramine and Nortriptyline
MOA: block reuptake of NE
- Treat depression
TCA: Imipramine, Amitryptyline
MOA: block NE/5HT reuptake
- Treat depression
SSRIs: Citalopram, Escitalopram, Sertaline, Fluoxetine
MOA: block 5HT reuptake at all seven 5HT subtypes
- Treat depression & bipolar disorder (should never be used alone to treat though)
Dual-action: Venlafaxine, Desvenlafaxine
MOA: selective 5HT and NE reuptake inhibitor (SNRI)
- Treat depression
Lithium Carbonate
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
Anticonvulsants: Valproic acid and Sodium Valproate
- Used for rapid-cycling of bipolar disorder (acute tx)
- Tx for seizures
Anticonvulsants: Carbamazepine
- Used for prophylactic tx of bipolar disorder
- Tx for seizures
First Generation Antipsychotics: Chlorpromazine, Haloperidol
MOA: block all D2 receptors in limbic system –> lowers DA levels
- Used for schizophrenia (+ psychoses symptoms - nigrostriatal pathway)
Second Generation Antipsychotics: CROQA
Clozapine, Risperidone, Olanzapine, Quetiapine, Aripiprazole
MOA: blocks D2 and 5HT receptors (5HT regulates D2 release…)
- Used for schizophrenia, bipolar disorder
Lurasidone
MOA: D2 and 5HT2A antagonist; precise unknown
- Used to treat major depression in bipolar patients
Vortioxetine
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
Barbiturates
Thiopental, Pentobarbital, Phenobarbital
MOA: facilitates GABA binding to GABAa receptors to increase duration of channel opening
- Treats anxiety and used as a general anesthetic
Benzodiazepines
Diazepam, Lorazepam, Flurazepam, Triazolam, Alprazolam
MOA: facilitates GABA binding to GABAa receptors to increase frequency of channel opening
- Treats anxiety
Methylphenidate
Immediate: Ritalin, XR: Concerta
MOA: enhances DA release and blocks reuptake
- Used to treat ADHD
This drug is a sympathomimetic (stimulant) - can be abused
Flumazenil
MOA: reverses effects of benzos, zolidem, zapelon
- Used to treat benzodiazepine OD
Propanolol
MOA: blocks autonomic signs
- Used to treat anxiety
Non-benzo benzodiazepine agonists
Zolpidem, Zaleplon, Eszoplicone
MOA: bind to GABAa receptors, but are selective to which receptor subtypes they bind
- Used for sleeping aids
Ramelteon
MOA: melatonin MT1 & MT2 receptor agonists; these receptors are located in suprachiasmatic nucleus (body’s master clock)
- Used for sleeping aid
Amphetamines
(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
Atomoxetine (Strattera)
MOA: elevates DA levels in prefrontal cortex (not nucleus accumbens!!)
- Used to treat ADHD
Eugeroics: Modafinil, Armodafinil
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
Halogenated hydrocarbons: halothane, isoflurane, sevoflurane, desflurane
Inhaled general anesthetics
MOA: amount of undissolved drug in the blood is related to clinical effect (Henry’s law)
What are some features of halothane?
- MAC: 0.77 (most potent)
- Rapid induction & recovery
- Potential for hepatic toxicity due to liver metabolism
- Can cause malignant hyperthermia - sensitizes myocardium to catecholamines
What are some features of isoflurane?
- MAC = 1.15
- Potent, induction < 10 minutes
- Less renal and hepatotoxicity than halothane
- rare arrhythmias, pungent odor, potential for malignant hyperthermia
What are some features of sevoflurane?
- MAC = 1.71
- High potency, rapid onset (5-10 minutes) and recovery
- Commonly used for day surgery
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
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!
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!!!
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
Propofol
- Rapid induction (50 seconds); recovery (4-8 minutes)
- May result in pain at injection site
- Respiratory apnea (22-45%)
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
Etomidate
- Used as a general anesthetic for emergency intubations
- Has a safe CV risk profile
Opioids: fentanyl, sufentanyl (used for general anesthesia)
- CNS effects: hemodynamic instability
- Respiratory airway must be maintained artificially as it may be depressed post-operatively
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.
Ethosuximide
MOA: Reduces low threshold Ca2+ currents (T-type) in thalamic neurons
- Treats absence seizures
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)
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
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!
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
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
What are some treatments for methanol and ethylene glycol poisoning?
Administer:
- Ethanol
- Fomepizole
- Bicarbonate - acidify urine to promote excretion (methanol)
How does one treat an amphetamine OD?
Give antipsychotics (FGAs or SGAs) and/or acidify the patient’s urine if have acute OD
Pentamidine
MOA: Binds DNA minor groove, mitochondrial as well as nuclear genome replication is affected
• Effective against: Trypanosoma brucei
Suramin
- Unknown mechanism, highly toxic
* Effective against: Trypanosoma brucei
Melarsaprol
• An arsenical, crosses BBB, so will treat stage 2 T. brucei infection. Super toxic!!!!
Eflornithine
MOA: ornithine decarboxylase inhibitor, crosses BBB,
- Treats stage 2 T. brucei infection.
Nifurtimox and Benznidazole
MOA: oxidative stress, impairment of membrane potential
• Trypanosoma cruzi or T. brucei co-treatment with eflornithine
Sodium Stibugluconate, Meglumine antimoniate
MOA: targets glycolysis and fatty acid beta-oxidation in mitochondria
- Treats leishmanial infections
Miltefosine
MOA: unknown
- Treats leishmanial infections
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
Albendazole
MOA: microtubule inhibitor
- Treats: Taenia solium- cysticercosis, Echinococcus granulosis, Toxocara cati
roundworms, tapeworms
