Antidepressants Flashcards
SSRIs can act on
- serotonin
- norepi
- dopamine
regardless of acting on serotonin, norepi or dopamine ALL SSRIs __________
block the repuptake of serotonin
some of the side effects caused by SSRIs is due to the ________.
Alpha 2 receptor blockade
oldest SSRI that works on serotonin only and also has a very active metabolite
Fluoxetine (Prozac)
has an active metabolite and a shorter elimination half time that fluoxetine
Sertraline (Zoloft)
SSRI with the longest elimination half time. How long is it?
Fluoxetine (Prozac) 3-6 Days
three other SSRIs that only act on serotonin
- Paroxitine (Paxil)
- Fluvoxamine (Luvox)
- Escitalopram (Lexapro)
SSRIs that act on NE and serotonin
- Buproprion (wellbutrin)
- Trazadone (desyrel)
- Nefazadone (serzone)
- Venlafaxine (effexor)
- Duloxetine (cymbalta)
What makes SSRIs have a higher index of safety than other antidepressants
- Minimal effects on blood pressure
- Minimal changes in conduction
- Minimal changes in the seizure threshold
if one antidepressant isn’t working the patient should….
try another one, because they have a high index of safety
Biggest complaint with SSRI see effects
Sexual dysfunction and weight gain
insomnia/fatigue agitation headache N/V rarely orthostatic hypotension
side effects of SSRIs
SSRI constellations with anesthesia
- Inhibits CYP 450 system
- Potential anti platelet activity - increased bleeding risk
- Serotonin Syndrome
Due to excess availability of serotonin in the CNS
Serotonin syndrome
Presents as muscle rigidity, hyperreflexia, diaphoresis, ataxia, shivering, fever and confusion
Serotonin syndrome
drugs that could potentiate a serotonin syndrome
phenylpipridine opioids:
- Methadone
- demerol
- tramadol
Methadone, demeorl and tramadol
weak serotonin repuptake inhibitors that could possibly potentiate a serotonin syndrome
SSRIs at lower doses can be used to treat_________ by inhibiting the overactive inflammatory response systems
chronic pain syndromes
Tricyclics are _________________.
Tertiary of Secondary amines
Tertiary amines inhibit ____________ reuptake while Secondary amines inhibit ____________ reuptake
Serotonin AND Norepi only Norepi
elimination half time of tricyclics
10-80 hours
how are tricyclics metabolized
by the liver
Tricyclics are highly ____________ and strongly _________.
lipid soluble - easily absorbed GI protein bound - to tissue and plasma proteins
_________ should not be given with tricyclics because they can cause CNS toxicity with _________, _________, ___________
MAOI
- hypothermia
- seizure
- coma
Because ___________ cause anticholinerdic side effects caution should be executed with __________. they are highly unpredictable and can cause an increase in ___________. An indirect agent should be aboided because an increase in _________ may be exaggerated due to larger amounts of _________ available at the synapse. Insead a ___________ acting agent should be used and with ________.
Tricyclic Antidepressants
Sympathetomimetics
Blood Pressure
Blood Pressure
Norepi
Direct
lower doses
Tricyclics and the cardiovascular system
- depresses conduction of the atria and ventricals- prolonged PR, Wide QRS and flat or inverted T-waves
- Orthostatic Hypotension - r/t activation of presynaptic Alpha-2 causing vasodilation
- Decreaed seizure threshold
Tricyclic overdose
Cardiotoxic effects, Seizure potential and CNS depression can be fatal
Tricyclics and Volitile anestheisa gasses
May need a higher MAC because more NE is present
Tricyclics and Opioids
Decrese opioid dose
Tricyclics and Induction agents
Most agents are cardiac depressants-
- with conduction changes from tricyclics
- induction agents can cause dangerous arrhythmias
Tricyclics and Barbituates
Decrease barbituate dose
Tricyclics and Anticholonergic
Because of the Anticholinergic side effectspt more likely to have post op delerium
try to use something that does not cross the BBB like glycopyrolate instead of atropine
Flushing, dry mouth and skin, mydriasis,
progressively red hot and dry
treated with physostigmine
Anticholonergic toxicity or Central anticholinergic syndrome wth Tricyclics
life threatening, intractable myocardial debression or ventricular dysrhythmias usually cause of death
Tricyclic Overdose
Tertiary amines
Tricyclics- inhibit serotonin and NE reuptake at presynaptic terminals
- Amytriptyline (elavil)
- Imipramine (tofranil)
- Clomiparime (anafanil)
Secondary amines
Tricyclic antidepressants that inibit NE reuptake at the presynaptic terminals
- Desipramine (norpramin)
- nortruptyline (pamelor)
Presenting features of tricyclic overdose
agitation, excitement, delerium which progresses to seizures, respiratory depression, cardiac dysrhythmias and sudden death.
there are hypotensive anticholinergic effects
how long will someone need to be monitored for a tricyclic overdose?
10 days, they can still have dysrhythmias for 10 days
what is given for anticolonergic psychosis
physostigmine
Levophed
direct acting agent for blood pressure support that can be used with tricyclics
Acidosis and tricyclic overdose
Acidosis may INCREASE unbound drug causing dysrhythmias
Give HCO3- to keep PH normal
Why should tricyclics be weaned
to prevent withdrawl symptoms
MAO is found in the __________________ and functions to _________________ inculding 1._______, 2.__________, 3._________, 4.__________
outer mitochondrial membrane
inactivate monoamines
dpoamine
serotonin
epinepherine
norepinepherine
MAOIs mechanism of action
block the enzyme that metabolizes biogenic amines, thereby increasing neurotransmitters in the CNS and peripheal autonomic nervous system
Deaminate: Serotonin, NE, Epi
MAO A
platelts contain exclusively _________ also 60% of MAO in the brain is ________
MAO A
Type A
Deaminate: Phenylethylamine
MAO B
Selecive MAO-B inhibitor at lower doses and non-selective at higher doses
Selegiline (eldepryl)
dont need to follow tyrosine free diet at lower doses
List to Memorize of MAOIs
- Brofaramine
- selegiline (eldepril)
- Iproniazid
- isocarboxazid (marplan)
- Phenelzine (nardil)
- Meclobemide
- befloxatone
- Tranycupromine (parnate)
Why do MAOIs have such a long duration of action
they bind irreversibly to MAO- the body actually has to form NEW enzymes to continue break down bioamines
MAOIs have NO effect on the ___________ and do NOT produce __________.
Seisure Threshold
Cardiac dysrythmias
Where is the MAO enzyme present?
liver, GI tract, kidneys, lungs
most common side effect with MAOIs
orthostatic hypotension
especially with the elderly
Side effects of MAOIs
- Anticholonergic like effects
- impotancy/anorgasmy
- weight gain
- sedation ir mild stimulate effects
- Orthostatic hypotension
What metabolizes tyramine
MAO A in GI tract and liver
Tyromine is a precursor for ______ and ______ and can act as a _____________________.
- Dopamine
- NE
- catchecholamine releasing agent
What happens when a person on an MAOI eats tyramine
Massive release of endogenous catechacholamines leading to a hypertensive crisis that can be lethal
hyperpyrexia
CVA
MAOI dietary restricions
- Cheese
- Fava beans
- red wine
- avacado
- cured meats, sourcrout
Drug ABSOLUTELY CONTRAINDICATED with MAOI - what do we use it for?
Meperidine (demerol)- used for post op shivering
MAOI drug cautions: Can cause CNS excitation, delerium, seizure, DEATH
- Tricyclic antidepressants
- opioids
- cold-allergy drugs
- sympathomimetics
- nasal decongestants
- SSRIs
- Serious headache
- vomiting
- chest pain
Symtoms to report with MAOI - could be the start of a Catechacholamine surge
Excitatory response may look like serotonin syndrome
MAOI and Meperidine (Demerol)
can inhibit the neuronal serotonin uptake
Meperedine (Demerol)
Agitation, skeletal musle rigidity, hyperpyrexia (high fever)
Excitatory response of MAOI with Meperedine (Demerol)
Type I
Hypotension, Respiratory depression, Coma
Depressive response of MAOI with Meperedine (Demerol)
Type II
Why does Meperedine (Demerol) react with MAOIs
MAOIs inhibits one of the enzymes that breaks down Meperedine (demerol).
Morphine and Opioids with MAOIs
respiratory depressive effects cand be enhanced with MAOIs
Four RULES for MAOIs and Anesthetics
- minimize the possibility of sympathetic nervous system stimulation or drug induced hypotension
- Caution with sympathetomimetics - Use DIRECT acting agents, NO EPHEDRINE
- Caution with opoids- NO Meperidine (Demerol)
- May need a higher MAC- r/t extra biogenic amines circulating
MAOI and Sympathomimetics
- May get an exagerated response from indirect acting drugs- NO EPHEDRINE
- Use direct acting agesnt like Phenylephrine
- Decrease dose by 1/3 an titrate to effect - can always give more, but cant take back what you have given
Hyperthemia, Mydriasis, Tachycardia, Seizure and death
MAOI overdose- only treatable with supportive care.
- Dizziness
- Myalgias - muscle pain
- Paresthesia
- irritability
- insomnia
- visual disturbances
- tremors
- letahrgy
- N/V/D
Discontinuation of antidepressants