Neuro Modulators Flashcards by Michael Clark

What are the Amphetamine-based stimulants?

Amphetamine
Dextroamphetamine
Methylphenidate

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What are the indications for amphetamine?

ADHD

Narcolepsy

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How does amphetamine treat narcolepsy?

Keeps the CNS running at a high rate of activity

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What is the MOA of amphetamine?

Stimulates CNS via a sympathomimetic mechanism involved the enhanced release and reduced reuptake of norepinephrine and dopamine

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What are the common side effects of amphetamine?

Photosensitivity
Visual disturbance
Elevated BP
Infection
Headache

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What are the serious side effects of amphetamine?

Dependency
Abuse
Psychosis
Growth suppression
Heart failure
Steven's-Johnson syndrome

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Amphetamines increase the release of what at the synaptic cleft?

Biogenic amines

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Why are photosensitivity and visual disturbance common with amphetamine use?

Can cause mydriasis

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What is the effect produced by the interaction of CAIs and amphetamine?

Renal excretion decreased in alkaline urine

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What is the effect produced by the interaction of sympathomimetics and amphetamine?

Hypertensive crisis

Arrhythmia

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What is the effect produced by the interaction of ophthalmic beta-blockers and amphetamine?

Hypertensive crisis

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What is the effect produced by the interaction of NSAIDs and amphetamine?

Caffeine-based additive effects

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When would be a situation in which it might be common to see an issue with amphetamine and sympathomimetic interactions?

A narcoleptic being treated for glaucoma (glaucoma drugs are often sympathomimetics

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When is amphetamine contraindicated?

With glaucoma

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What is the biogenic amine theory for antidepressants?

There is a deficiency in monoamines (norepinephrine and serotonin)

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SSRIs are designed not to influence which monoamine?

Norepinephrine

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Which monoamine is acted on my SNRIs?

Both norepinephrine and serotonin

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What kind of antidepressant is imiparmine?

TCAD

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What is MAO responsible for?

Biogenic amine degradation

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What are the 6 SSRI antidepressants?

Escitalopram
Sertaline
Fluoxetine
Paroxetine
Fluvoxamine
Citalopram

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Which SSRI is the “s” enantiomer of citalopram?

Escitalopram

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The majority of SSRI antidepressants end in what suffix?

-ine

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What is the indication for Excitalopram (SSRI)?

Major depressive disorder

Generalized anxiety disorder

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What is the MOA of escitalopram?

SSRI

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What are the common side effects of escitalopram?

Dizziness

What are the distinguishing side effects of escitalopram?

Suicidal risk Serotonin syndrome Neuroleptic malignant syndrome Siezures

What is neuroleptic malignant syndrome?

High levels of serotonin in the body - life threatening

Why might escitalopram cause dry eye?

Fight and flight turns off all the body's glands, except the sweat glands, causing a lack of tear production

What are the effects of an interaction between NSAIDs and Escitalopram? (Omega-3s as well)

Hemorrhage risk

What are the effects of an interaction between ophthalmic beta blockers and escitalopram?

Reduced beta-blocker metabolism

What are the three SNRI antidepressants?

Duloxetine Venlofoxine Desvenlofoxine

SNRIs aren't selective for which monoamine?

Serotonin

What is the MOA for duloxetine?

SNRI

What are the common side effects of Duloxetine?

``` Blurred vision Headache Dizziness Sweating ED HTN Orthrostatic hypotension Syncope Yawning Constipation ```

What are the distinguishing adverse effects of duloxetine?

Serotonin syndrome

What are the possible hypersensitivity reactions to duloxetine?

Angioedema | Steven's-Johnson syndrome

What are the ocular side effects of duloxetine?

Glaucoma

Angioedema from Duloxetine can masquerade as what?

Preseptal cellulitis

What is the effect of an interaction between opioids and duloxetine?

Additive

What is the effect of an interaction between NSAIDs/omega-3/6s and duloxetine?

Hemorrhage

What is the effect of an interaction between beta-blockers and duloxetine?

Reduced beta-blocker metabolism, causing a toxic build up of beta-blockers

What cautions come with duloxetine?

Bleeding risk | Angle closure glaucoma

What are the three atypical antidepressants?

Trazadone Nefazadone Bupropion

What is the MOA of trazodone?

``` Selective Serotonin (5-HT) Reuptake inhibitor (SSRI) Adrenergic alpha-1blocker and 5-HT_2A/C blocker ```

What are the common adverse effects of trazodone?

Headache Dizziness Blurred vision Ocular irritation

What are the distinguishing side effects of trazodone?

Suicidal ideation | 5-HT syndromw

What are the effects of cyclosporine/macrolides/azoles when they interact with Trazodone?

QT prolongation and impaired hepatic metabolism - rising levels of trazodone

What are the effects of NSAIDs when they interact with trazodone?

Hemorrhage

What causes mania?

Excess of norepinephrine, serotonin, and dopamine

What are the indications for Quetiapine?

Schizophrenia | Bipolar disorder

What is the MOA of quetiapine?

Antagonizes D2 receptors and 5-HT receptors | Ancillary effects may arise from antagonism of H1 and alpha 1

What is H1?

Histamine receptor

What is 5-HT2?

Serotonin type 2 receptors

What is D2?

Dopamine type 2 receptors

Which generation anti-psychotic is quetiapine?

2nd generation

What does quetiapine antagonize?

Both dopamine and serotonin

What are the ocular side effects of Quetiapine?

Cataracts

What are the muscular side effects of quetiapine?

Extrapyramidal symptoms

What are the interactions of Macrolides/azoles, CsA with quetiapine?

Prolonged QT segment

What is the effect of classic anti-histaminics interacting with quetiapine?

Additive CNS depression

What are the 1st generation antipsychotics?

Haloperidol Chlorpromazine Thioridazine

First generation antipsychotics are selective for what?

Which is the more potent 1st generation antipsychotic?

Haloperidol

What are the ocular side effects to 1st generation antipsychotics?

Cataracts | Retinopathy

Chlorpromazine and thioridazine have additional ocular side effects beyond the usual cataracts. What are they?

Night blindness | Salt and pepper fundus

What are the common adverse effects of lithium?

Blurred vision

What are the severe adverse effects of lithium?

Seizures Bradycardia Idiopathic intracranial hypertension Diabetes IN

Why should NSAIDs be taken in conjunction with Lithium?

NSAIDs increase lithium level by reducing renal excretion

What is the effect of the interaction of Lithium with either NSAIDs or tetracyclines?

Increased lithium levels

What is the effect of the interaction of caffeine or CAIs with lithium?

Reduced lithium because of diuresis (caffeine is a diuretic)

Alzheimer's patients have a significant loss of what in the temporal lobe?

Cholinergic neurons

Most of the drugs used to treat Alzheimer's are what?

Acetylcholinesterase inhibitors (AChE)

Why has Tacrine been largely discontinued to treat Alzheimer's?

Severe hepatotoxicity

Most of the Alzheimer therapy drugs have which suffix?

-ine

What is the indication for Donepezil?

Alzheimer Dementia

What is the MOA of Donepezil?

Indirect acting - reversibly binds to and inactivates ACh-ase

What are the common adverse effects of Donepezil?

Headache Dizziness Arthridis

What are the serious side effects of Donepezil?

``` Seizures Dream disturbances Hemolytic anemia AV block Bradycardia Syncope ```

What is the effect of a cholinergic agent interacting with Donepezil?

Additive

If an anticholinergic interacts with Donepezil, what happens?

An antagonistic effect

Donepezil and NSAIDs put you at risk of what?

Hemorrhage

What are the two anti-parkinson therapies?

Carbidopa + Levodopa | Bromocriptine

What is Sinemet?

Levodopa + cabidopa for Parkinson's disease

What is the MOA for levodopa?

Dopamine precursor that crosses the BBB and enhances dopamine synthesis

What is the MOA for carbidopa?

Inhibits dopa decarboxylose, preventing it from degrading levodopa to dopa

The majority of drugs in the anziolytics and hypnotics category act where?

GABAa receptor - the CNS's major inhibitory neurotransmitter

What is the most common type of anxiolytic/hypnotic?

Benzodiazepines

Is a high therapeutic index good or bad?

Bad

Which is short acting, alprazolam, or midazolam?

Midazolam

What is the MOA of Alprazolam?

Selectively binds the BZD site on GABAa receptors, enhancing GABA effects, leading to Cl influx and hyperpolarization

Does Alprazolam actually stimulate the receptor?

No, it enhances GABA effects

What are the common adverse effect of Alprazolam?

``` Diplopia Drowsiness Anterograde amnesia Confusion Dizziness Hypotension ```

What are the possible hypersensitivity reactions to Alprazolam?

Stevens-Johnson syndrome | Angioedema

How does Alprazolam interact with cyclosporine/azoles/erythromycins?

Reduces alprazolam metabolism

What happens with chlorpheniramin, diphendydramine/opioids interact with Alprazolam?

Additive effect

Alprazolam essentially does what to the CNS?

Depresses it

What are the contraindications for Alprazolam?

Unstable Myasthenia Gravis

What is the indication for Zolpidem?

Insomnia (it is Ambien)

What is the MOA of Zolpidem?

Selective agonist of GABAa-BZD-1 receptor

What are the adverse effects of Zolpidem?

``` Headache Sinusitis Pharyngitis Anmesia Suicidal ideation Aggression Hallucinations ```

What happens if you take cyclosporine/azoles with Zolpidem?

Zolpidem metabolizm is reduced, leading to a build up

What happens if you take Zolpidem with opioids or antihistaminics?

Additive effect