2 - Neuromodulators Flashcards
what are 3 amphetamine-based stimulants (psychomotor stimulants)?
amphetamine (Adderall), dextroamphertamine (Dexedrine), methylphenidate (Ritalin, Concerta)
what are the indications for amphetamine?
ADHD and narcolepsy
what is the mechanism of action for amphetamine?
stimulates CNS through sympathomimetic mechanism - enhanced release and reduced re-uptake of NE and E
what are some common side effects for amphetamine?
sympathomimetic = photosensitivity, visual disturbance, elevated BP, infection, headaches
what are some serious side effects for amphetamine?
dependency, abuse, psychosis, growth suppression, heart failure, stevens-johnson syndrome
which two types of drugs will have an additive effect with amphetamine?
NSAIDs (caffeine based) and decongestants
what three types of drugs when combined with amphetamine create hypertensive crisis?
sympathomimetics, ophthalmic beta-blockers and alpha2 agonists
what happens when CAIs are taken with amphetamine?
renal excretion decreased in alkaline urine
Ex: you have a patient with ADHD and is taking Visine. If you need to dilate them what drug should you use?
tropicamide - not phenylephrine (decongestant)
what is a contraindication for amphetamine?
glaucoma (glaucoma is treated with drugs that block sympathetic activity and amphetamine enhances sympathetic activity)
what are the 5 antidepressant drug classes?
SSRIs, SNRIs, TCADs, atypical and MAOIs
what are TCADs inhibiting?
very non-selective = inhibit re-uptake of NE, serotonin and dopamine
what are the 6 SSRI antidepressants?
Excitalopram (Lexapro), Sertraline (zoloft), fluozetine (prozac), paroxetine (paxil), fluvoxamine (luvox), citalopram (celexa)
what is escitalopram indicated for?
major depressive disorder and generalized anxiety disorder
what is the mechanism for escitalopram?
selective serotonin re-uptake inhibitor (SSRI)
what are the distinguishing side effects for escitalopram (SSRIs)?
suicidal risk, serotonin syndrom, neuroleptic malignant syndrome (NMS), seizures
what are the ocular side effects for escitalopram (SSRIs)?
dry eye, blur, diplopia, conjunctivitis, ptosis = all due to sympathomimetic effect
what causes 5-HT syndrome in SSRIs?
the excessive serotonin overwhelms the effects of dopamine and the body doesn’t recognize dopamine like it normally would
what symptoms can occur with low levels of dopamine (or with 5-HT syndrome, NMS)?
parkinson like symptoms = life-threatening, bradykinesia/muscle rigidity (elevated CPK) and leukocytosis
what happens if you take escitalopram with NSAIDs and omega-3?
hemorrhage risk = reduced serotonin reduces platelet clotting (patient may have sub-conjunctival hemorrhage)
what happens if you take escitalopram with ophthalmic beta-blockers?
reduced metabolism of beta-blockers = side effects will be enhanced, may need to reduce dose/concentration
what are 3 SNRI antidepressants?
duloxetine (cymbalta), venlafaxine (effexor), and desyenlafaxine (pristiq)
what is the indication for duloxetine?
depression, anxiety, nueropathic pain (DM) and fibromyalgia
what is the pharmacology for duloxetine?
antidepressant, analgesic: SNRI
what is the mechanism of action for duloxetine?
selective serotonin and norepinephrine re-uptake inhibitor (SNRI)
what are the common side effects for duloxetine?
sympathomimetic effects = blurred vision, headache, dizziness, sweating, ED, HTN, orthostatic hypotension, syncope, yawning, constipation
what is the distinguishing side effect for duloxetine?
serotonin syndrome
what hypersensitivities may occur with duloxetine?
angioedema and stevens-johnson syndrome
what is the ocular side effect for duloxetine?
glaucoma
what happens if you take opioids with duloxetine?
there is an additive effect = risk of 5-HT syndrome/NMS increases
what happens if you take NSAIDs and omega-3,6 with duloxetine?
hemorrhages = there is reduced clotting with reduced serotonin
what happens if you take oral beta-blockers with duloxetine?
reduced metabolism of beta-blockers = AV block and hypotension, bradycardia (used for high BP)
what are 2 cautions for duloxetine?
bleeding risk and angle closure glaucoma
what are 3 atypical antidepressants?
trazodone (desyrel), nefazadone (serzone), bupropion (wellbutrin, zyban)
what are the indications for trazodone?
major depressive disorder and insomnia
what is the mechanism of action for trazodone?
selective serotonin re-uptake inhibitor (SSRI) and adrenergic alpha1 blocker
what are the common side effects for trazodone?
headache, dizziness, blurred vision, ocular irritation (sympathomimetic effects)
what are the distinguishing side effects for trazodone?
suicidal ideation and 5-HT syndrome
what is a CVS side effect for trazodone?
hemorrhage (platelets depend on serotonin for clotting)
what happens if you take cyclosporine, macrolides, and azoles with trazodone?
QT prolongation and imparied hepatic metabolism
what happens if you take NSAIDs with trazodone?
hemorrhage risk is increased
what are 4 anti-psychotic/neuroleptics?
Quetiapine (seroquel), Halloperidol (haldol), Chlorpromazine (thorazine), Thioridazine (mellaril)
what are the indications for quetiapine?
schizophrenia and bipolar disorder
what is the pharmacology for quetiapine?
2nd generation anti-psychotic and bipolar disorder
what is the mechanism of action for quetiapine?
antagonizes dopamine receptors and 5-HT receptors (ancillary effects may arise from antagonism of histamine and alpha1 receptors)
what are the common side effects for quetiapine?
headache and anemia
what is an ocular side effect for quetiapine?
cataracts
what is a hypersensitivity connected to quetiapine?
stevens-johnson syndrome
what happens if you take macrolides, azoles and cyclosporine with quetiapine?
prolonged QT segment
what happens if you take classic (sedating) anti-histamines with quetiapine?
additive CNS depression
Ex: if a patient has an allergic conjunctivitis due to sinusitis and is taking quetiapine, what do you prescribe for an oral/topical anti-histamine?
needs to be 2nd generation and non-drowsy (non-CNS depressant)
what happens to patients with Alzheimer’s disease?
there is a significant loss of cholinergic neurons in temporal lobe and entorhinal cortex
what are two classes of drugs used to treat Alzheimer’s disease?
acetylcholinesterase inhibitors (AChEI) and NMDA-glutamate receptor antagonists
what are 5 drugs used to treat Alzheimer’s disease?
Donepezil (aricept), Galantamine (razadyne), Rivastigmine (exelon), Tacrine (cognex), Memantine (namenda)
which of the Alzheimer’s drugs is the NMDA receptor agonist (neuro-protective)?
Memantine (namenda) - may be used to treat glaucoma
what is the mechanism of action for donepezil?
indirect (central) acting - reversibly binds to and inactivates acetylcholinesterase (AChE) = produces excessive ACh (rest/digest symptoms)
what are the common side effects for donepezil?
headache, dizziness, arthritis (relaxes vascular tone)
what are some serious side effects of donepezil?
CNS (seizures, dream disturbances), hemolytic anemia, CV (AV block, bradycardia, syncope)
what happens if you take cholinergic agents with donepezil?
additive effect (ex: pilocarpine use punctal occlusion)
what happens if you take NSAIDs and donepezil?
hemorrhagic risk (hemolytic anemia produced by donepezil)
what happens if you take anti-cholinergics with donepezil?
antagonism occurs
what happens if you take macrolides and azoles with donepezil?
reduced metabolism of donepezil
what happens if you take dexamethasone with donepezil?
enhanced metabolism of donepezil (patients may show Alzheimer’s symptoms even if taking medication)
what happens if you take Brimonidine (alpha2 agonist) and timolol (beta-blocker) ophthalmics with donepezil?
both ophthalmic drugs reduce sympathetic activity + donepezil reduced sympathetic activity = bradycardia and bronchospasm
what happens if you take ester anesthetics with donepezil?
reduced metabolism of anesthetics (proparacaine and benzocaine are esters)
what causes Parkinson’s disease?
imbalance between excitatory cholinergic neurons and diminished inhibitory dopaminergic neurons
what is the goal of Parkinson’s disease therapy?
restoring dopamine in basal ganglia and antagonizing the excitatory effect of cholinergic neurons (restores D/ACh balance)
what are 2 anti-parkinson drugs?
Carbidopa + Levodopa (sinemet) and Bromocriptine (Parlodel)
what is the mechanism of action for sinemet (carbidopa and levodopa)?
carbidopa = inhibits dopa decarboxylase (which degrades levodopa to dopa) levodopa = dopamine precursor that can cross BBB to enhance DA synthesis in substantia nigra
what are the common side effects for sinemet?
headache and confusion
what are the serious CNS side effects for sinemet?
psychosis, suicidal ideation, hallucinations
what are the drug interactions for sinemet?
there are no ophthalmic drug interactions
where do the majority of anxiolytics and hypnotics act?
at the GABAa receptor = CNS’s major inhibitory neurotransmitter
what are the 3 long lasting benzodiazepines?
diazepam (valium), chlordiazepoxide (librium), Flurazepam (dalmane)
what are the 2 short acting benzodiazepines?
midazolam (versed), triazolam (halcion)
what are the indications for alprazolam?
anxiety and panic disorder
what is the mechanism of action for alprazolam?
selectively binds to GABAa-BZD receptors - enhancing GABA effects = inhibitory effect on CNS (ligand gated ion channel)
what are the common adverse effects for alprazolam?
diplopia, drowsiness, anterograde amnesia, confusion, dizziness, hypotension
what are the 2 hypersensitivities for alprazolam?
stevens johnson syndrome and angioedema
what happens if you take alprazolam with cyclosporine, Azoles, or erythromycins?
reduced alprazolam metabolism
what happens if you take alprazolam with chlorpheniramine, diphenhydramine or opioids?
there is an additive effect
what are the contraindications/cautions for alprazolam?
unstable myasthenia gravis
what are the 3 non-benzodiazepines?
zolpidem (ambien), eszopiclone (lunesta) and zaleplon (sonata)
what is the indication for zolpidem?
insomnia (only short term)
what is the pharmacology for zolpidem?
non-BZD sedative hypnotic
what is the mechanism of action for zolpidem?
selective agonist of GABAa-BZD-1 receptors
what are the common side effects for zolpidem?
headache, sinusitis, and pharyngitis
what are the CNS side effects seen with zolpidem?
amnesia, suicidal ideation, agression, and hallucinations
what happens if you take zolpidem with cyclosporine or azoles?
reduced metabolism of zolpidem
what happens if you take zolpidem with classic antihistiminics or opioids?
there is an additive effect
