!Neuropharm Antidepressants Flashcards
Selective serotonin reputable inhibitor (SSRI)
For depression, anxiety, OCD, buimia, PTSD
Specific SSRI such as ___ can even be used to improve cognitive recognition post stroke
Escitalopram
Examples of SSRI
Fluozetine, paroxetine, sertraline, citalopram, escitalopram, vilazonone, vortioxetine
MOA SSRI
Selectively inhibiting reputable of serotonin by presynaptic cells leading to an increased availability of serotonin in the synaptic gap, allowing it to repeatedly stimulate the post synaptic receptors
Side effect of SSRI
Sexual dysfunction (erectile dysfunction, anorgasmia, decreased libido) Serotonin syndrome
What is serotonin syndrome
SSRI combined with other medications promoting serotonin availability
How does serotonin syndrome present
Hyperthermia, hypertension, myoclonus, mydriasis, overactive bowels, mental agitation
How can you treat serotonin syndrome
Cyproheptadine
Indications forSSRI
Depression and anxiety (social phobia, panic disorder, PTSD)
MOA SSRI
Inhibit the reputable of the NT serotonin by the presynaptic cells . Serotonin stays in synaptic gap longer and may repeatedly stimulate the receptors of the post synaptic cell
How long do u have to take SSRI before effect
4-8 weeks
Examples of SSRI
Paroxetine, sertraline, escitalopram, fluoxetine, citalopram, vortioxetine, vilazonone
Paroxetine
SSRI for social phobia
Panic attacks, depression OCD and PTSD
Sertraline
SSRI for PTSD(soldier says SIR)
Anxiety disorders, depression, OCD, panic disorder
Escitalopram
Cognitive recovery post stroke also for depression and anxiety treatment
Fluoxetine
SSRI for depression , OCD, bulimia and panic disorder
Side effects SSRI
Sexual dysfunction, serotonin syndrome,
What drugs taken with SSRI cause serotonin syndrome
TCAs, SNRIs, MAOIs (any medication increasing serotonin availability)
How treat serotonin syndrome
Hyperthermia, hypertension, myoclonus, mydriasis, overactive bowels and mental agitation
Treat with cyproheptadine
What does cyproheptadine do
Acts as a serotonergic (5-HT2) receptor antagonist
Fluoxetine (prozac)
SSRI maintains mental balance in the brain by decreasing the reputable of serotonin back into presynaptic cell
increase serotonin in synaptic cleft which bind to postsynaptic receptors and create more transmission
Serotonin
NT involved in transmission of nerve impulses
Indication for fluoxetine (Prozac)
Depression
-believed to be a defiency in freely available serotonin in brain
OCD, panic disorder, premenstrual dysphoric disorder
Side effects fluoxetine
Sexual dysfunction, CNS stimulation, wight gain, serotonin syndrome
What is CNS stimulation
Headache, nervousness, anxiety, insomnia
Contradictions for fluoxetine
Do not take with monoamine oxidase inhibitors (MAO-Is) as it increases the available pool of serotonin int he brain and increases the risk of developing serotonin syndrome
Contradiction 2 for fluoxetine
SSI decrease aggregation of platelets and increase GI bleeding risk up to 3 times . Patients should be advised to avoid anticoagulants and antiplatelets while taking these medication s
Considerations for fluoxetine
Suicide risk
Delayed onset of action
Why SSRI increase suicide risk
Side effects violent behavior , mania or aggression which can increase siucidal thoughts or actions suicide risk increases during the initial phase of starting on the meds
How long does it take SSRI to work
1-3 week weeks
Longer if depression more severe
Serotonin norepinephrine reputable inhibitors (SNRIs)
Class of drug indicated for the use of major depression, diabetic peripheral neuropathy, panic and anxiety.
Examples of SNRI
Duloxetine
Venlafaxine
Duloxetine
SNRI for diabetic peripheral neuropathy and depression
Venlafaxine
Panic and anxiety disorders
MOA SNRI
Inhibiting reputable of the NT serotonin and norepinephrine thus increasing their bioavailability, yielding increased NT
Side effects SNRI
Increase NE
Nausea , vomiting , decreased libido and anorgasmia
Bad compliance
Indications for SNRI
Depression, diabetic peripheral neuropathy, panic and anxiety
Which SNRI for diabetic peripheral neuropathy
Deluxetine
Other indications for duloxetine
Anxiety, chronic pain and fibromyalgia
Which SNRI for panic and anxiety
Venlafaxine
Venlafaxine
Works on serotonergic and noradrenergic receptors
MOS SNRI
Inhibits reputable of serotonin and NE
Increases in NT by increasing availability of extracellular concentrations of serotonin and NE
Side effects SNRI
Hypertension, insomnia, nausea and vomiting, decreased libido
Why get insomnia with SNRI
Increasing circulating NE
Bupropion
Atypical antidepressant for smoking cessation often combined with SSRI for depression therapy
MOA bupropion
Increased availability of dopamine and NE
How does bupropion lead to smoking cessation
Blocking nicotonic acetylcholine receptors in the brain
Side effects bupropion
Insomnia, tachycardia, seizure(lowers seizure threshold)
Indication s for bupropion
Depression and smoking cessation
Smoking cessation and bupropion
Reduce severity of nicotine cravings and ithdrawal symptoms
MOA bupropion
Increase dopamine and NE
Block of nicotonic acetylcholine receptors in brain
Side effects of bupropion
Tachycardia insomnia, seizure , epilepsy
Tricyclics antidepressants (TCAs) overview
Three ring chemical structure
Wide range of presentations, including depression, bed wetting, OCD, fibromyalgia
MOA TCA
Lipi soluble and rapidly absorbed and exhibit their effects by blocking serotonin and NE reputable transporters leading to increased availability of serotonin and NE
Side effects TCA
Convulsion, coma, cardiotoxicity (arrhythmias), anti histamine and anticholinergic effects of this drug , adverse CNS stimulant effects, such as mania, agitation, seizure, confusion and tremor.
Impaired gastric motility, dry mouth, blurry vision, increased temp, urinary impairment
Postural hypotension
MOA TCA
Blocks serotonin and NE reputable by blocking 5-HT and NE
Elevated synaptic concentrations of the neurotransmitters
*no affinity for dopamine transporters thus limited effect on dopamine
TCA is lipid soluble. Significance?
Rapidly absorbed
Side effects TCA
Adverse CNS effects Anticholinergic Antihistamine Tri-c: convulsion, coma, cardiotoxicity Blocks alpha1 receptors
Adverse CNS effects TCA
CNS stimulation
Confusion, mania, agitation, tremor, seizures, sedation
Anticholinergic TCA
Impaired gastric motility, dry mouth, blurry vision, increased temp, and urinary impairment
Cholinergic actions eye
Contraction muscle of iris (miosis)
Contraction of ciliary muscles (accommodation for near vision
Anticholinergic actions eyes
Relaxation of circular muscle of iris (mydriasis)
Relaxation of ciliary muscles (cycloplegia, loss of accommodation)
Cholinergic effects heart
Bradycardia
Decrease HR
Anticholinergic actions heart
Tachycardia increased HR
Cholinergic actions urinalysis bladder
Contraction of muscles in urinary bladder
Relaxation of sphincter bladder
Urination
Anticholinergic actions urinary bladder
Relaxation of muscles
Contraction of sphincter
Urinary retention
TCA antihistamine
Seizures and arrhythmias
Mostly mimic anticholinergic effects
Tri-c : convulsion, coma, cardiotoxicity TCA
Cardiac-na channel block (widening QRS, QT prolongation and torsades de points)hyperpyrexia and respiratoy depression
Tca blocks alpha1 receptors
Postural hypotension
Indications for tCA
Major depression, bed wetting, fibromyalgia, OCD
Suffix of TCA
Iptyline or ipramine
TCA examples
Amitriptyline, desipramine, clomipramine, imipramine, nortiptyline
Amitriptyline
For depression and first line for fibromyalgia and chronic pain
Amitriptyline has more __ effects than other TCA. Causing what
Anticholinergic
Stiffness, nausea, constipation, nervousness, dizziness, tremor, blurred vision, urinary retention and changes in sexual function
Desipramine
TCA for OCD, also depression and anxiety disorders
Imipramine
TCA for nocturnal enuresis (bed wetting)
Why is imipramine used for bed wetting
Decrease the delta wave stage of sleep (when bed wetting occurs)
Nortriptyline
TCA for depression, less side effects than 1st generation TCA medications.
Why does nortriptyline have less influence on hypotension than other TCA
Stilll blocks a1, but less?
Nortriptyline keeps blood pressure NORmal
Tricyclic antidepressants (TCA)
Older generation of antidepressants that block the reputable of norepinephrine and serotonin.
Why aretricyclic antidepressants called dirty drugs
Cause a wide variety of side effects
Side effects of tricyclic antidepressants
Antimuscarinic Alpha blocking Antihistamininc Cardiac arrhythmias Lower seizure threshold Long QQT-lead to torsades
How do we treat tricyclic antidepresssant toxicity
Sodium bicarbonate
How does sodium bicarbonate treat tricyclic antidepressant toxicity
- Alkalinization of the plasma can increase protein binding of them and decrease their bioavailability
- Sodium load is thought to reverse the Na channel blocking effects of TCA
Monoamine oxidase inhibitors (MAOIs)
Group of drugs that work by inhibiting the breakdown of the neurotransmitters serotonin, NE and dopamine, thereby increasing their availability
Indication for MAOI
Atypical depression by also anxiety and panic disorders
___, a monoamine oxidase type B inhibitor, may be effective int he treatment of parkinson disease
Selegiline
What food should u avoid with MAOI
Tyramine-containing foods, such as large amounts of wine and cheese , as the combination of MAOIs with excess tyramine can lead to a hypertensive crisis
Severe increase in bp occurs due to the release of large amounts of amine NT (serotonin, NE and dopamine) triggered by excess tyramine
What drugs should not be used with MAOI
SSRI, TCA< meperidine, dextromethorphan, St. John’s wort, as this may lead to serotonin syndrome
Wine and cheese and MAOI
Tyramine is metabolized by monoamine oxidase, and when foods high in tyramine are combined with therapy that inhibits MAO, excess stored monoamine are released.
What foods are high n tyramine
Wine cheese, red wine, beer, soy, over ripened bananas, cured smoked aged or pickled meats
What will tyramine rich food and MAOI lead to
Hypertensive crisis
-severe bp increase which can lead to stroke
What other drugs should not be given with MAOI
SSRI, TCA, meperidine, and dextromethorphan
What happens when have MAOI and serotonin drug
Risk of serotonin syndrom e
Monoamine oxidase inhibitors (MAO-Is)
Group of drugs that work by inhibiting the breakdown of the NT serotonin, NE and dopamine, thereby increasing their availability
Indication for monoamine oxidase inhibitors
Atypical depression, but have been used for anxiety and panic disorders, bulimia, personality disorders and Parkinson’s disease (selegiline)
MAO “takes pride in shanghai”
MAO-Is meds
Takes Pride in shanghai
Tranylcypromine
Phenelzine
Isocarboxasid
Selegiline
What should we not give MAO-Is with
Tyramine containing food——hypertensive crisis
What happens in hypertensive crisis
Severe increase in bp occurs due to the release of large amounts of amine NT (serotonin, NE and dopamine),triggered by excess tyramine
What drugs should MAO-Is not be given with
SSRI, TCA, meperadine, dextromethorphan, St. John’s wart may lead to serotonin syndrome
Indication for MAO-is
Atypical depression
MOA MAO-Is
Increased levels of amine NT (serotonin, NE, dopamine)
Tranylcyrpomine
Nonselective
Major depression
Mood disorders
Phenelzine
Nonselective
Failed first and second lines of treatments for depression
Isocarboxazid
Non selective MAO-I indicated for depression, anxiety and panic disorders
Selegiline
Selectively inhibits MAO-B at low doses which metabolizes dopamine over NE and serotonin. This leads to increased levels of dopamine availability.
Selegiline is typically used with what
L Dopa for parkinsons treatment as it enhances effects of L dopa treatment and decreases motor complications
At high doses, selegiline loses its selectivity for ___
MAO-B
