CNS pharmacology Flashcards by Brock rose

What are indications for antipsychotic drugs

Schizophrenia
tourettes syndrome
Huntingtons Chorea
OCD and others

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What is the widely accepted cause of psychosis

hyperactive dopamine pathway

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what are antipsychotic drugs

Dopamine Antagonists

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What are typical antipsychotic drugs, and what are common ones

1st generation dopamine antagonists

phenothiazines
haloperidol
Thiothixene

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what are atypical antipsychotic drugs, and what are the common ones

2nd generation dopamine antagonists
more specific than 1st gen antagonists = less tardive dyskinesia
- Clozapine
- Olanzipine
- Quetiapine
- Risperidone
- Ziprasidone
- Arpiprazole
- paliperidone

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what is the most commonly prescribed 1st gen antipsychotic

Haloperidol

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What are the side effects of dopamine receptor antagonists (antipsychotics)

tardive dyskinesias
parkinsons like symptoms
Dystonias (spasms)
Perioral tremor

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what is the problem with the side effects of antipsychotics (dopamine antagonists)

the patients struggle to live with them so they stop taking their medications

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What type of drug is used to manage the extrapyrimidal motor effects of antipsychotics (dopamine antagonists)

Antimuscarinic drugs

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what is Neuroleptic Malignant syndrome

a life threatening neurological disorder from an adverse reaction to antipsychotic drugs. symptoms include: muscle rigidity, fever, autonomic instability, delerium.

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adverse effects of antipsychotic use

otrhostatic hypotension
convulsions
photosensitivity
cardiac arrythmias (long QT
galactorrhea

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what are the two types of depression

unipolar

bipolar

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what is the monoamine theory of depression

depression is a result of low monoamine transmitters (Norepinephrine and 5-HT (serotonin)

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what is the desired action of antidepressants

block the reuptake of monoamines

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What are tricyclic antidepressants? and what are the common drugs

NE and 5-HT reuptake inhibitors (More NE)

Amitryptiline
Desipramine
Doxepin
Imipramine
Protryptiline
Maprotiline

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What are SSRIs? and what are the common drugs

Selective serotonin reuptake inhibitors

prozac (Fluoxetine)
paroxetine
Sertraline
Fluvoxamine
Citalopram

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what are SNRIs? and what are the common drugs

mixed NE and Serotonin (5-ht) reuptake inhibitors

Effexor (Venlafaxine)
Cymbalta (Duloxetine)

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What is the drug that is an NE only reuptake inhibitor

Wellbutrin (bupropion)

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What are MAOIs. what are the most common drugs

monoamine oxidase inhibitors

Phenelazine
tranylcypromine
selegiline

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why are MAOIs and other antidepressants contraindicated

because it leads to excessive amounts of monoamines (seratonin and NE)

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What is Mirtazapine

monoamine receptor agonist
(a2 adrenergic receptor blocker)

another antidepressant

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What is Trazodone

antidepressant thought to potentiate 5-HT

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What is St. Johns Wort

weak monoamine uptake inhibitor

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What are other uses of TCA’s, SSRis?

TCA = neuropathic pain
TCA + SSRI = fibromyalgia
SSRI = anxiety disorders, ADHD
Buproprion = addiction

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Why aren't typical antidepressants used to treat bipolar disorder

they can induce the manic phase

What is the drug used to prophylactially prevent manic-depressive episodes

Lithium

what is the problem with lithium in treating bipolar disorder

it has a narrow TI which requires plasma monitoring. | causes nasuea, convulsions, coma, arrythmias

what are other options besides lithium in treating bipolar disorder

antiepileptic drugs: Valproate, carbamazepine, lamotrigine | Atypical antipsychotics: Zyprexa (Olanzapine)

What is the common method of action for sedative hypnotics

activating or enhancing Cl channels | GABA-A receptors

What are the uses for sedative hypnotics

``` antianxiety anticonvulsants amnesia insomnia panic disorders sedation skeletal muscle relaxation ```

Adverse effects of sedative hypnotics

``` Ataxia Amnesia Altered sleep patterns confusion Excessive sedation ```

What are the two main classes of sedative hypnotics and what is their mode of action

barbiturates and benzodiazepines | they are both modulators of GABA receptors that enhance the effect of GABA on them

what are the subclasses of barbiturates and their drugs

long acting - phenobarbital intermediate acting - pentobarbital, amobarbital short acting - thiopental

What is the long acting barbiturate and what is it used for

phenobarbital = antiepileptic

what are the intermediate acting barbiturate and what are they for

pentobarbital, amobarbital = sleep induction

what is the short acting barbiturate and what is it used for

thiopental = induction anesthetic

what is a contraindication for barbiturates

Certain types of porphyria

What is it about benzodiazepines that gives them a longer half life

they have active metabolites

What are the benzodiazepines and what are their half lives

``` triazolam - 1,5 hrs midazolam - 4 hours oxazepam - 8 hrs lorazepam - 14 hrs diazepam - 48-100 hrs flurazepam - 100 hrs ```

What is a common sedative hypnotic used for conscious sedation in dentistry that is not a barbiturate or benzodiazepine

chloral hydrate

what should you know about chloral hydrate before using it

that repetitive doses of it shouldn't be used since toxicities can be very serious

what is zolpidem and zalepon?

a sedative hypnotic that acts on GABAA receptors, has low risk of dependence and is used to treat insomnia

what is the sleep hypnotic Buspirone used for and what is its mechanism

it is a 5HT1A agonist, | it is used for anxiety

What is Baclophen, what is it used for

agonist at GABAB | its a muscle relaxant used to treat trigeminal neuralgia

What is Diphenhydramine

Benadryl | its an antihistamine that causes sedation

Ethanol can be used as a sedative narcotic but isn't

yep, it affects multiple targets and one of them is GABAA

What is Flumazenil, and what is it used for

its a GABA A receptor antagonist | it is used to reverse sedation drugs

Methocarbamol, Carisprodol, and Cyclobenzaprine are used for what

sedative hypnotics (their mechanism of action isn't fully understood)

What are seizures, what different types are there

they are excessive and innapropriate activity of CNS neurons they can be partial or generalized they can be tonic-clonic or absence

What are the 4 mechanisms of action in antiepileptics

Na v channel antagonists Ca channel antagonists Glutamate receptor antagonists (AMPA, NMDA) Cl channel agonists

What are the different drugs used to treat epilepsy, and what is their method of action

``` phenobarbital - GABA A modulator phenytoin - Na v antagonist Primidone - metabolized to phenobarbital Carbamazepine - Na v antagonist Gabapentin - unknown (not GABA) Valproic acid (valproate) - GABA, Na v and Ca v antagonist Ethosuxamide - Ca v antagonist ```

What are the adverse effects of using phenobarbital as an antiepileptic

potential for drug-drug interactions sedation osteomalacia respiratory depression

What are the adverse effects of using phenytoin as an antiepileptic

eliminated by zero order kinetics = potential for overdose gingival hyperplasia osteomalacia

What are the adverse effects of using primidone as an antiepileptic

acute systemic and CNS toxicity sedation ataxia nystagmus

What are the adverse effects of using carbamazepine as an antiepileptic

induces liver enzymes - drug drug interactions diziness ataxia

What is carbamazepine used for besides as an antiepileptic

bipolar disorder and trigeminal neuralgia

what is the antiepileptic with an unknown mechanism of action that is FDA approved for partial seizures

Gabapentin

what is Gabapentin used for more often that epilepsy

neuralgia

what is the antiepileptic that increases GABA and is an NA v and Ca V antagonist. and is approved by the FDA for partial seizures

valproic acid (valproate)

what else is valproate (valproic acid) used for besides epilepsy

bipolar disorder

What are the adverse effects of using valproate (valproic acid) as an antiepileptic

hair loss hyperglycemia hyperuricemia teratogenic

What is the antiepileptic drug that blocks Ca v and is approved by the FDA for absence seizures

Ethosuxamide

What is the characteristic of parkinsons disease

``` progressive hypokinesia loss of voluntary movement tremor at rest involuntary hyperkinesia progresses to muscle rigidity ```

What causes parkinsons disease

a defect in signaling in the basal ganglia loss of DA cells leads to less GABA action leads to increased excitatory output to motor cortex

What are the 3 treatment strategies for parkinsons

increase dopamine receptor activation in basal ganglia block muscarinic receptors in basal ganglia block NMDA glutamate receptors

why does blocking muscarinic receptors in basal ganglia help with parkinsons

cholinergic function in the basal ganglia inhibits dopamine action

What is the main drug used for parkinsons disease that is a prodrug for dopamine

levadopa (once it gets past the BBB it is converted into dopamine

What is the drug used for to prevent levadopa from being converted into dopamine in the periphery due to its action as a dopa carboxylase inhibitor

carbidopa (it can't cross the BBB but help L-dopa stay until L-dopa crosses the BBB) reduces L-dopa needed by 90% and decreases side effects

What drugs are used as DA receptor agonists that help dopamine bind more readily

Pramipexole Ropinirole Apomorphine Bromocriptine

What are the drugs that block COMT (catecholectamine O-methyl tranferase) from breaking down dopamine in CNS

tolcapone | Entacapone

What are the drugs that block MAO-B from breaking down dopamine in the CNS

``` Rasagiline Selegiline (don't use with antidepressants) ```

How is diphenhydramine used to treat parkinsons

it blocks the H1 receptor and treats extrapyrimidal side effects

What is the drug that used to be used as an antiflu but now is used for parkinsons

amantidine (blocks NMDA)

how does benztropine help with parkinsons

it is an anticholinergic and tries to restore cholinergic and dopamine balance

CNS pharmacology Flashcards

(74 cards)