Neuromodulators Flashcards
indication: anxiety, panic disorder
dosing (1/4, 1/2, 1, 2, mg) - 1 tab tid
alprazolam
Selectively binds to GABA-A-BZD receptors, thereby enhancing GABA effects
alprazolam (benzodiazepine anxiolytic)
gaba pathways are?
inhibitory
competitive drug
drug is competing for same binding site as the endogenous substrate (ex: gaba receptor: gaba)
is benzodiazepine competitive?
no, it binds to a different site than gaba
benzodiazepine + alcohol =
deadly! because they bind the same receptor
- Common:diplopia,drowsiness, anterograde amnesia,confusion,dizziness,hypotension
- Hypersensitivity:StevensJohnson Syndrome, angioedema
alprazolam
- Common: diplopia,drowsiness, anterograde amnesia,confusion,dizziness,hypotension
- Hypersensitivity: Stevens Johnson Syndrome, angioedema
alprazolam
- Cyclosporine, Azoles, and Erythromycins: Reduce this drugs metabolism
- Chlorpheniramine, Diphenhydramine, Opioids –> Additive
alprazolam
CONTRAINDICATIONS/CAUTIONS
• Unstable Myasthenia Gravis
alprazolam
*can cause double vision; mg has dysfunctional acetycholine pathway
zolpidem (ambien), eszopiclone (lunesta), zaleplon (sonata)
non-benzodiazepine
• INDICATION: Insomnia
• DOSING[5/10mg] • 1 tab qhs

zolpidem
• CLINICAL PHARMACOLOGY– Non WBZD Sedative Hypnotic
• Mechanism of Action
– Selective agonist ofG ABAAWBZD-1 receptor
zolpidem
ADVERSE EFFECTS
• Common:headache,sinusitis, pharyngitis
• CNS:amnesia, suicidal ideation, aggression,hallucinations
zolpidem
not as dangerous as other benzadiazepine drugs
zolpidem
DRUG INTERACTIONS
• Cyclosporine, AzoleAntifungals: Reduced#metabolism#of#Zolpidem#
• Classic#An:histaminics,#Opioids:# Addi:ve#
zolpidem
DRUG INTERACTIONS
• Cyclosporine, Azole, Antifungals: Reduced metabolism of drug
• Classic Antihistaminics,Opioids: Additive
zolpidem
which drug has the same moa as amphetamine?
pyramed (hydroxyamphetamine + tropicamide)
– Stimulates#CNS#through#a# sympathomimetic#mechanism#involving#
the#enhanced#release#and#reduced# reuptake#of#norepinephrine#and# dopamine#
amphetamine
what drug blocks the reuptake receptors for NE ?
cocaine
photosensitivity, elevated BP, infection, headache
adverse: dependency, abuse, psychosis, growth suppression, heart failure, stevens johnsons syndrome
amphetamine adverse effects
CAIs (renal excretion decreased in alkaline urine)
Sympathomimetics (hypertensive crisis, arrhythmia)
Ophthalmic Beta-Blockers & Alpha-2 Agonists (hypertensive crisis)
NSAIDs (caffeine-based additive effects)
Decongestants (additive)
drug interactions with amphetamine
pt with adhd and large cups presents at clinic. what do we do?
workup for glaucoma and call pcp –> unusually large cupping is a risk factor for it; the use of amphetamine could be contributing factor
pt with adhd and large cups presents at clinic. what do we do?
workup for glaucoma and call pcp –> unusually large cupping is a risk factor for it; the use of amphetamine could be contributing factor
class of drugs that are often overprescribed
antidepressants
Escitalopram [Lexapro®] Sertraline [Zoloft®] Fluoxetine [Prozac®] Paroxetine [Paxil®] Fluvoxamine [Luvox®] Citalopram [Celexa®]
SSRI ANTIDEPRESSANTS
INDICATION
Major Depressive Disorder, Generalized Anxiety Disorder
DOSING [5/10/20mg]
10-20mg qd
Escitalopram indication
what drug is the “S” enantiomer of citalopram which is a racemic mixture. What does this suggest?
escitalopram; our body responds to S structure
ESCITALOPRAM CLINICAL PHARMACOLOGY Antidepressant: SSRI Mechanism of Action Selective serotonin reuptake inhibitor (SSRI)
escitalopram moa
ADVERSE EFFECTS
Common: dizziness
Distinguishing: suicidal risk, serotonin syndrome, neuroleptic malignant syndrome (NMS), seizures
Ocular: dry eye, blur, diplopia, conjunctivitis, ptosis
adverse effects of escitalopram
ADVERSE EFFECTS
Common: dizziness
Distinguishing: suicidal risk, serotonin syndrome, neuroleptic malignant syndrome (NMS), seizures
Ocular: dry eye, blur, diplopia, conjunctivitis, ptosis
adverse effects of escitalopram
what combo of drugs could result in heme?
escitalopram + nsaid + omega 3
what combo of drugs could result in heme?
escitalopram + nsaid + omega 3
INDICATION
Depression, Anxiety, Neuropathic Pain (DM), Fibromyalgia
DOSING [20/30/60mg]
60mg qd
duloxetine indications
CLINICAL PHARMACOLOGY
Antidepressant, Analgesic: SNRI
Mechanism of Action
Selective Serotonin & Norepinephrine reuptake inhibitor (SNRI)
duloxetine moa
ADVERSE EFFECTS
Common: blurred vision, headache, dizziness, sweating, ED, HTN, orthostatic hypotension, syncope, yawning, constipation
Distinguishing: serotonin syndrome
Hypersensitivity: Angioedema, Stevens-Johnson syndrome
Ocular: Glaucoma
duloxetine adverse effects
DRUG INTERACTIONS
Opioids (additive)
NSAIDs & Omega-3/6 (hemorrhage)
Beta-Blockers (reduced beta-blocker metabolism
duloxetine drug interactions
CAUTIONS
Bleeding risk
Angle closure glaucoma
duloxetine contraindiction
types of antidepressants that arent used as much
tricyclic antidepressant
most prescribed atypical antidepressant
trazadone
INDICATION Major Depressive Disorder*, Insomnia# DOSING [50-300mg] *50-100mg bid-tid #25-50mg qhs
trazadone indication
CLINICAL PHARMACOLOGY
Antidepressant, Anti-Insomnia
Mechanism of Action
Selective Serotonin (5-HT) Reuptake Inhibitor (SSRI); adrenergic α1-blocker & 5-HT2A/C blocker
trazadone moa
TRAZODONE
ADVERSE EFFECTS
Common: headache, dizziness, blurred vision, ocular irritation
Distinguishing: Suicidal ideation, 5-HT syndrome
CVS: hemorrhage
TRAZODONE
ADVERSE EFFECTS
acts similar to tomaxafen used to treat breast cancer
trazadone
DRUG INTERACTIONS
Cyclosporine, Macrolides, Azoles (QT prolongation & impaired hepatic metabolism)
NSAIDs (hemorrhage)
trazadone drug interaction
_______ activity in the mesolimbic system is the pleasure center that is thought to drive psychotic behavior
Dopamine
1st generation antipsychotics initially were relatively selective dopamine receptor inhibitors
Newer antipsychotics have a variety of selectivities accounting for a range of activities and side effects
1st generation antipsychotics initially were relatively selective ____________.
Newer antipsychotics have a ___________ accounting for a range of activities and side effects
most prescribed antipsychotic
quetiapine
most prescribed antipsychotic
quetiapine
INDICATION
Schizophrenia, Bipolar Disorder
DOSING [25-400mg]
200-400 mg bid
quetiapine INDICATION
QUETIAPINE
CLINICAL PHARMACOLOGY
2nd Gen Anti-Psychotic, Bipolar Disorder
Mechanism of Action
Antagonizes D2 receptors & 5-HT2 receptors
Ancillary effects may arise from antagonism of H1 and α1
QUETIAPINE
Mechanism of Action
which antipsychotic drug produces cataracts?
quetiapine
QUETIAPINE ADVERSE EFFECTS Common: headache, anemia Ocular: cataracts Hypersensitivity: Stevens-Johnson syndrome
QUETIAPINE
ADVERSE EFFECTS
which antipsychotic drug can cause stevens johnson synderome?
quetiapine
QUETIAPINE
DRUG INTERACTIONS
Macrolides, Azoles, CsA (Prolonged QT segment)
Classic (sedating) Anti-histaminics (additive CNS depression)
QUETIAPINE
DRUG INTERACTIONS
Patients with Alzheimer disease have a significant loss of cholinergic neurons in the temporal lobe and entorhinal cortex. Most of the drugs available to treat the disease are acetylcholinesterase (AChE) inhibitors
Antagonists of the NMDA-glutamate receptor are often neuro-protective, preventing the loss of neurons following ischemic and other injuries.
Patients with _______ disease have a significant loss of cholinergic neurons in the temporal lobe and entorhinal cortex. Most of the drugs available to treat the disease are ______.
_________ of the NMDA-glutamate receptor are often neuro-protective, preventing the loss of neurons following ischemic and other injuries.
used to treat glaucoma and alzheimers; only drug selective for nmda
memantine
DONEPEZIL INDICATION Alzheimer Dementia DOSING [5/10/23 mg] 1 tabs qhs
DONEPEZIL
INDICATION
DONEPEZIL CLINICAL PHARMACOLOGY Alzheimer Disease / Dementia Mechanism of Action Indirect (central) acting; reversibly binds to and inactivates acetylcholinesterase
DONEPEZIL
CLINICAL PHARMACOLOGY
Mechanism of Action
DONEPEZIL ADVERSE EFFECTS Common: headache, dizziness, arthritis SERIOUS ADVERSE EFFECTS CNS: Seizures, dream disturbances Circulatory: Hemolytic anemia CV: AV block, bradycardia, syncope DONEPEZIL ADVERSE EFFECTS Common: headache, dizziness, arthritis SERIOUS ADVERSE EFFECTS CNS: Seizures, dream disturbances Circulatory: Hemolytic anemia CV: AV block, bradycardia, syncope
donepezil adverse effects
DONEPEZIL ADVERSE EFFECTS Common: headache, dizziness, arthritis SERIOUS ADVERSE EFFECTS CNS: Seizures, dream disturbances Circulatory: Hemolytic anemia CV: AV block, bradycardia, syncope DONEPEZIL ADVERSE EFFECTS Common: headache, dizziness, arthritis SERIOUS ADVERSE EFFECTS CNS: Seizures, dream disturbances Circulatory: Hemolytic anemia CV: AV block, bradycardia, syncope
donepezil adverse effects