Neuro Modulators Flashcards
What are the Amphetamine-based stimulants?
Amphetamine
Dextroamphetamine
Methylphenidate
What are the indications for amphetamine?
ADHD
Narcolepsy
How does amphetamine treat narcolepsy?
Keeps the CNS running at a high rate of activity
What is the MOA of amphetamine?
Stimulates CNS via a sympathomimetic mechanism involved the enhanced release and reduced reuptake of norepinephrine and dopamine
What are the common side effects of amphetamine?
Photosensitivity Visual disturbance Elevated BP Infection Headache
What are the serious side effects of amphetamine?
Dependency Abuse Psychosis Growth suppression Heart failure Steven's-Johnson syndrome
Amphetamines increase the release of what at the synaptic cleft?
Biogenic amines
Why are photosensitivity and visual disturbance common with amphetamine use?
Can cause mydriasis
What is the effect produced by the interaction of CAIs and amphetamine?
Renal excretion decreased in alkaline urine
What is the effect produced by the interaction of sympathomimetics and amphetamine?
Hypertensive crisis
Arrhythmia
What is the effect produced by the interaction of ophthalmic beta-blockers and amphetamine?
Hypertensive crisis
What is the effect produced by the interaction of NSAIDs and amphetamine?
Caffeine-based additive effects
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
When is amphetamine contraindicated?
With glaucoma
What is the biogenic amine theory for antidepressants?
There is a deficiency in monoamines (norepinephrine and serotonin)
SSRIs are designed not to influence which monoamine?
Norepinephrine
Which monoamine is acted on my SNRIs?
Both norepinephrine and serotonin
What kind of antidepressant is imiparmine?
TCAD
What is MAO responsible for?
Biogenic amine degradation
What are the 6 SSRI antidepressants?
Escitalopram Sertaline Fluoxetine Paroxetine Fluvoxamine Citalopram
Which SSRI is the “s” enantiomer of citalopram?
Escitalopram
The majority of SSRI antidepressants end in what suffix?
-ine
What is the indication for Excitalopram (SSRI)?
Major depressive disorder
Generalized anxiety disorder
What is the MOA of escitalopram?
SSRI
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?
D2
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