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Pharmacology > CNS > Flashcards

CNS Flashcards

1
Q

Barbiturates

A
  • Hypnotic/Anxiolytic(now anesthesia)
  • Enhance GABA response, inhibit Glutamate response
  • Strong CNS depressant-> anesthesia
  • High risk of dependence-> severe withdrawal symptoms
  • High dose-> respiratory (inhibit hypoxic and CO2 chemoreceptors) and cardiovascular depression-> little use as hypnotic (Epilepsy and Anesthesia)
  • Potent inducer of P450-> Drug interaction (Contraceptive Failure)
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2
Q

Phenobarbital

A
  • Long acting barbiturate

- Used as anti-convulsant

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3
Q

Thiopental

A
  • Short acting barbiturate
  • Highly lipophylic-> (brain-> fat) hangover
  • Administered via IV-> anesthesia
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4
Q

Amobarbital

A
  • Barbiturate used to treat epilepsy

- Also Pentobarbital, secobarbital

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5
Q

Benzodiazepines

A
  • Anxiolytic
  • 7 member ring fused to benzene ring
  • Strictly GABA modifier-> enhance GABA affinity
  • Treat phobias, anxiety, myocardial infarcon(reduce stress)
  • Safer than barbiturates
  • Anterograde amnesia-> preoperative administration
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6
Q

Chlordiazepoxide

A

-First benzodiazepine(Librium) 1960

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7
Q

Diazepam

A
  • Valium, benzodiazepine

- Strong anti convulsant

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8
Q

Lorazepam

A

-Ativan, Benzodiazepine

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9
Q

Flunitrazopam

A
  • Rohypnol, Benzodiazepine
  • Disinhibition, date rape drug
  • Risk of dependence
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10
Q

Alprazolam

A
  • Xanax, Benzodiazepine

- Antidepressive properties

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11
Q

Triazolam

A

-Benzodiazepine, Paradoxical irritability-> withdrawn use in UK

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12
Q

MAO inhibitor effects

A
  • Increase in Norepinephrine, serotonin, dopamine
  • Last resort, Side effects
  • Food interaction(Cheese), Tyramine is metabolized by MAO, when MAO is inhibited tyramine builds up and displaces NE in storage vesicles-> NE release-> hypertension and arrythmias
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13
Q

Tranylcypromine

A
  • MAO inhibitor

- Also: Phenelzine

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14
Q

Imipramine

A
  • Tricyclic antidepressants, NSRI, dibenzepine
  • Strong interaction with alcohol
  • Side effect: Sedation(H1 blocker)
  • Desipramine, Clomipramine
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15
Q

Amitriptyline

A
  • Tricyclic antidepressant, NSRI, Dibenzcycloheptene

- Norttiptyline

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16
Q

Fluoxetine

A
  • SSRI, same efficacy as TCAs but fewer side effects
  • Side effects: inhibition of sexual climax, (rare) aggression, violence
  • Paroxetine, Sertraline, Citalopram
17
Q

What causes depression?

A
  • “Amine hypothesis”

- Functional decrease in Norepinephrine and serotonin in the brain

18
Q

What cause Schizophrenia?

A
  • “Dopamine Hypothesis”
  • Increase In dopamine (possibly serotonin) in the brain
  • Anti-psychotic-> D2 and 5-HT receptor antagonists
19
Q

2 Types of Neuroleptics

A
  • Typical (classical)->Phenothiazines, Butyrophenones->releives posative symptoms
  • Atypical-> Relieves positive and negative symptoms-> action primarily in the limbic system not striatum-> fewer extra pyramidal effects
20
Q

Classical neuroleptic side effects

A
  • Extrapyramidal effects due to dopamine blockage in the striatum->acute dystonia, Pseudo-parkinsonism, Tardive Dyskinesia (irreversible)
  • (H1 blockage) Sedation
  • (Muscarinic and Alpha-adrenergic) dry mouth, constipation, urinary retention
  • Lactation
  • Strong interaction with alcohol
21
Q

Chlorpromazine

A
  • Classical neuroleptic, Phenothiazine

- Triflupromazine, Fluphenazine

22
Q

Halopridol

A
  • Classical neuroleptic, Buterophenones

- Trifluperidol, Spiroperidol

23
Q

Olanzapine

A
  • 5-HT and D2 receptors
  • Same efficacy as clozapine, but no agranulocytosis
  • Risperadone
24
Q

Parkinson’s Pathology

A

-Loss of dopaminergic neurons in the Pars compact of Substantia nigra-> ACh excitation goes unopposed in corpus striatum->Increase GABA inhibition to thalamus-> less excitatory input to motor cortex-> Tremors, stiffness, rigid posture, mask-like face, pill rolling (early)

25
Q

Dopamine replacement

A
  • Levodopa (L-Dopa)

- Carbidopa (L-Dopa decarboxylase inhibitor)

26
Q

Bromocriptine

A
  • Derived from Ergot Alkaloid (Rye fungus, LSD)
  • Potent D2 agonist
  • Initially used to treat Galactorrhea (inhibit Prl release)
  • Pergolide, Pramipexole
27
Q

Selegiline

A
  • MAOb inhibitor (mostly CNS, no cheese rxn at low dosage)

- Extends half-life of Dopamine

28
Q

Carbamazepine

A
  • Anti-Epileptic

- Benzodiazepine-> GABA modulation-> counteracts depolarization

29
Q

Tiagabin

A

-Anti-epileptic, prevents GABA re-uptake

30
Q

Phenytoin

A
  • Anti-epileptic, Block Na channels in refractory stage-> only blocks high frequency excitation
  • Eliminated by zero order Kinetics
  • Convulsive seizures only(not absent)
  • Side effect: Gingival hyperplasia
31
Q

Ethosuximide

A
  • Anti-epileptic, blocks T-type Ca channels

- Drug of choice for absent seizures

32
Q

Valproate

A
  • Anti-epileptic, Increase GABA in the brain(mechanism unclear)
  • Useful for convulsive or absent seizures
  • Teratogenic (birth defects)
  • Heptatoxic
33
Q

Disulfiram

A
  • Treat alcoholism
  • Aldehyde-dehydrogenase inhibitor->Increase Acetaldehyde-> nausea, vomiting, hang over
  • Side effect: Also inhibits dopamine hydroxyls-> Blocks conversion of Dopamine to NE-> rise in dopamine-> schizophrenic symptoms
34
Q

Naltrexone

A
  • Alcoholism treatment, Opioid receptor antagonist-> blocks reward response
  • Urge diminishes over time, 80% success rate

Pharmacology (10 decks)

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