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162 Cards in this Set
- Front
- Back
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What are the three main treatments for ADHD?
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Methyphenidate, Amphetamines, Amoxetine
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What are two major difference between Methyphenidate and Amphetamines in MOA?
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Methyphenidate blocks reuptake of NE, DA while Amphetamine increases release of NE, DA AND 5HT via transporter reversal.
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What makes Amoxetine so attractive?
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For ADHD, only NE selective transporter blockade and does not cause SNS or reward center stimulation.
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What drug in the treatment of ADHD can cause decreased growth, nausea, sedation and facial tics?
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Amoxetine
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What treatments for ADHD can cause facial tics and tachycardia while causing possible dependence?
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Methyphenidate and Amphetamines
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Why is amoxetine not a stimulant?
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No effects on DA
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This should always be avoided in any ADHD treatment.
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MAOI (At least 2 weeks between) can cause hypertensive crisis.
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This conventional antiseizure drug can be used on ANY type of seizure (super drug).
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Valproate (Valproic Acid)
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Utilized in partial seizures because it inhibits GAT-1
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Tiagabine
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Drug increases GABA release and decreases uptake and is used for partial seizures and postherpetic neuralgia.
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Gabapentin
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This barbituate is used for treating tonic-clonic sezures and partial with secondary generalization and has an active antiseizure metabolite.
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Primidone (Phenobarbital metabolite)
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This conventional antiseizure can be utilized for all partial seizures and tonic-clonic. It purportedly induces its own metabolism.
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Carbamazepine
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This recent anitseizure is a super drug utilized for all partial and generalized seizures (including absence).
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Lamotrigine
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This AS blocks NA, Ca, Glu but not GABA and can be used for Bipolar I
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Lamotrigine
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This recent AS can be used for all seizures except absence because its MOA does not include Ca T channel. It can also blocks carbonic anhydrase activity and can cause migraines and kidney stones.
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Topiramate
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What are the three AS's used for absence seizures?
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Ethosuximide, Valproate, Lamotrigine
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What two AS drugs should you not give to a pregnant woman? What is an acceptable alternative?
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Valproate and Phenytoin; Phenobarbital
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What two major AS drug classes are best for Tonic-Clonic.
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Barbituates or Benzodiazepams
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This AS is good for all seizure disorders except absence and myoclonic.
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Carbemazepine
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What are the only three AS used for myoclonic seizures?
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Valproate, Lamotrigine, topiramate.
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Why can't you predict the plasma level of phenytoin? What should you do? What is a negative outcome?
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Metabolism is first order at low doses then at patient determined saturation, it becomes zero order. Must monitor levels of phenytoin to prevent hepatotoxicity.
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These two AS compete for albumin binding in the blood.
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Phenytoin and Valproate
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This drug induces the metabolism of carbamazepine and can increase warfarin concentration.
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Phenytoin
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What is the main metabolic problem with many of the older AS drugs?
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Can negate oral contraceptives.
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This AS can cause aplastic anemia.
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Carbemazepine
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These two AS can cause Steven Johnson's disease.
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Lamotrigine and Ethosuximide (phenytoin can too)
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Name four typical antipsychotics.
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Chlorpromazine, Fluphenazine, Thioridizine, Haloperidol (Think Halo-zines)
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This typical antipsychotic has high cardiotoxicity.
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Thioridizine (Sulfur in the heart would be bad...)
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What types of blockade are produced by the typical antipsychotics?
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D2, Muscarinic, A1, H1 (Negative symptoms, drymouth, orthostatic hypotension, sedation)
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What is counterindicated in typical antipsychotics?
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Opiods can lead to hyperexic coma (u/k moa)
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What are the hormonal side effects of typical antipsychotics?
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DA block prevents Prolactin inhibition resulting in galactorrhea and amenorrhea in women; hypogonadism and gynomastia in men.
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What are three anticholinergic drugs used to assist with EPS symptoms from typical antipsychotics?
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Benztropine, trihexyphenidyl, diphenydramine (Think psychotics and PD patients Dying to Tri the Mercedes Benz)
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What is the mechanism of action for atypical antipsychotics including clozapine, olanzipine, quetapine, ziprasidone, risperidone, aripiprazole.
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Serotonin-dopamine antagonists (Greater potency for 5HT2A than D2) Note: aripiprazole is a partial D2 agonist
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This atypical antipsychotic actually has D2 agonist properties.
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Aripiprazole (Pip is D2ifferent)
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This antipsychotic can produce agranulocytosis.
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Clozapine
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This antipsychotic should not be used to treat Bipolar (unlike others).
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Clozapine
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This antipsychotic can be used for depression.
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Quetiapine
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This antipsychotic is bad for the heart because it produces and increase it QTc interval.
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Ziprasidone
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What is responsible for the positive symptoms in SZ?
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Increased DA activity in the mesolimbic system producing hallucinations, delusions, hyperactivity, etc.
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What is responsible for the negative symptoms of SZ?
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Decreased DA activity in mesocortical system causing flat affect, avolition, abulia, etc.
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What is the overall control of DA in the mesolimbic and mesocortical sytems?
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The Ventral Tegmental Area (VTA increases DA in the nucleus accumbens (mesolimbic) and decreases DA in the cortex
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How does 5HT2A antagonism help with SZ?
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5HT2A is Gq; HT from Raphe nuclie tonically inhibits DA release from nigrostriatal pathway; MOA = disinhibition
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How does DA increase from atypical overcome their D2 antagonism in the cortex?
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High D2 off rate and increased DA allow DA dominance in caudate-putament and cortex.
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These atypical AP produce weight gain and metabolic syndrome.
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Olanzipine and Clozapine
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Name three MAOIs.
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Phenelzine, Tranylcypromine, Selgeline
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This MAOI is an irreversible inhibitor of -A and -B and causes orthostatic hypertension, weight gain, insomnia and sexual dysfunction.
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Phenelzine
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This MAOI is a nearly irreversible inhibitor of -A and -B and causes orthostatic hypotension, weight gain, insomnia, sexual dysfunction less than its counterpart.
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Tranycypromine
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What four monoamines are increased by MAOI's?
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5HT, NE, Tyramine, DA)
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What are the antidepressants of last resort?
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MAOIs
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MAOI + sympathomimetics can cause what condition?
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Hypertensive Crisis
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MAOI + SSRI can cause what?
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Serotonin Syndrome
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What are some major C/I of MAOI's?
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SSRI, or any serotonin increase (cocaine, MDMA, Meth, meperidine & tramodol opiod inhibitors
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MAOI + opiods can cause what?
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Hyperpyrexic coma (u/k moa)
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This MAOI solely works on MAO-B for inhibition and has less dietary restrictions tha its counterparts.
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Selegeline
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What are some side effects for selegeline?
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Insomnia, Dry mouth, Bad dreams (u/k MOA)
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Demethylation of Tricyclic AD reduces their ability to do what?
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Effectively block 5HT reuptake.
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What is the MOA for tricyclics?
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Block NE and 5HT reuptake (except for desipramine has no 5HT activity)
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Which tricyclic has no 5HT reuptake blocking activity?
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Desipramine (think no CH3)
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What is the major problem with tricyclics?
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Cardiotoxicity; don't prescribe to suicidal patients
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What common beverage is counterindicated in tricyclic administration?
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Alcohol (impaired driving due to massive sedation)
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Name the four major first generation tricyclics.
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Amitriptyline, nortiriptyline, imipramine, desipramine (PRAMINE = presynatipc reuptake of amine, MI = mixed inhibitor)
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This trycyclic can be used to treat enuresis in kids?
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Imipramine
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These two tricyclcs can treat ADHD too.
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Imipramine, desipramine
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Name three 2nd generation heterocyclics.
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Amoxapine, buprioprion, trazodone (TABs on 2nd generation)
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This 2nd heterocyclic has the same MOA as 1st with the addition of D2 and muscarinic receptor blockade, which allows its treatment of depressed psychotics.
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Amoxapine
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This 2nd generation heterocyclic only blocks DA reuptake with very little traditional activity. It is also used for Nicotine cessation.
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Buproprion
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This 2nd heterocyclic blocks 5HT2 receptors but activates 5HT1 receptors. It also causes massive priaprism.
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Trazadone
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Name four 3rd generation heterocyclics.
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Mirtazapine, venlafaxine, nefazodone, Duloxetine (MNDV ine, one)
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This 3rd generation has no reuptake activity, is an antagonist at 5HT2 and alpha receptors and has anihistamine activity resulting in sedation. The good part is it has no sexual dysfunction.
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Mirtazapine (think miracle)
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This 3rd heterocyclic inhibits serotonin reuptake but not so much NE. It causes sexual dysfunction but since it doesn't interact with CYP, it has few drug interactions.
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Venlafaxine (No Ven diagram of interactions)
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This 3rd heterocyclic has less sexual dysfunction that SSRIs, is a 5HT2 antagonist & anti-muscarinic.
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Nefazodone (Napz from antimuscarinic but rest for sex over SSRIs)
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This 3rd generation hast traditional activity but is very useful because of little sedative effects.
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Duloxetine
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Name 5 important SSRIs.
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citalopram, escitalopram, fluoxetine, paroxetine, sertraline
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What is so attractive about the SSRI MOA.
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Specific for 5HT without as many adrenergic, histaminergic and muscarinic effects.
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What are the only two SSRIs not metabolized by P450 resulting in few drug interactions?
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Citalopram, Escitalopram (Escape CITochromes)
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This CAM inhibits MAO-A, B at high doses, reduces IL-6 and is used as a antidepressant and antiviral; however, make sure you stay out of the sun and watch for drug interactions like birth control.
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St. John's Wort
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This migraine drug decreases vasopeptide release by activating 5HT1D/1B but is very short acting and cannot be utilized in cardiac patients.
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Sumatriptan
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This migraine drug decreases vasopeptide release by activating 5HT1D/1B; is usually given with caffeine to increase absorption but only effective during prodrome. Can cause longstanding vasoconstriction if repeatedly taken.
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Ergotamine
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This migraine drug decreases vasopeptide release by activating 5HT1D/1B; is a safer alternative to ergotamine but is ineffective during active episodes.
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Methysergide
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This migraine drug has no effect on serotonin receptors, but blocks calcium channels for an unknown MOA.
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Propranolol
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The greatest degree of opiod analgesia is associate with which receptor?
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Mu opiod receptor
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Euphoria, respiratory depression, and physical dependence of opiods are due to which receptor?
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Mu opiod receptor
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This opiod receptor only has spinal effects (vs. supraspinal).
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K opiod receptor
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Which CNS effect of opiods does not develop tolerance?
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Miosis
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This strong mu opiod receptor agonsist is more effective than morphine because of less first pass effects and ease of BBB crossing.
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Heroin
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This strong mu opiod receptor is often used in the treatment of heroin because of its long term action.
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Methadone
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This strong mu opioid receptor agonist has very short, but very potent action and is often used as a anesthetic adjunct.
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Fentanyl
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This strong mu opioid receptor agonist has antimuscarinic effects and blocks 5-HT receptors, so don't give it with MAOIs.
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Meperidine
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This mild mu opioid receptor agonist is often used with acetomenaphin due to cough suppression.
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Codeine
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This mild mu opioid receptor agonist has low analgesic activity, but its effect is additive.
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Propoxyphene (Think proportionate increase)
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Most opioids with mixed receptor actions have what pattern? Why is this significant?
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Kappa receptor agonist/with partial agonist or antagonist activity for mu Kappa activity has less tolerance and dependence, but too much kappa can lead to dysphoria.
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This mixed receptor opioid, used in treatment, has long lasting partial mu agonist activity and is a good exception to the rule.
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Buprenorphine
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This mixed receptor agonist follows the rule but has significant first pass effect.
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Butorphanol
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This opioid mixed receptor drug has weak mu opioid receptor agonism, but also blocks serotonin and is an antimuscarinic, so don't use with MAOIS.
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Tramadol
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Giving opioids with sedative-hypnotics (such as benz. or barbs.) can cause what interaction?
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Increased CNS and respiratory depression.
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Giving opioids with antipsychotics leads to what effects?
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Increased sedation and enhancement of cariovascular effects via alpha 2 blockade
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Giving opioids with MAOi's can cause what?
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Hyperpyrexic coman (u/k MOA)
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Name four drugs used in the Tx of AD.
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Donepezil, Rivastigmine, Galantamine, Memantine
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What do donepezil, rivastigmine and galantamine have in common?
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All three are AchE inhibitors to increase time to institutionalization in AD.
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This drugs in an uncompetitive NMDA receptor agonist that relies upon an open Glu activated channel to bind and stops low level excitotoxicity of Glu.
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Memantine
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This drugs is often paired with memantine to increase cognfitive function.
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Donepezil
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This CAM is often used for AD and to decrease free radical damage, but its cholinergic and sympathomimetic activity produces insomnia and anxiety as well as exacerbation of seizure disorders.
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Ginkgo Biloba
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This CAM drug is often used to boost mental performance, but causes vaginal bleeding and mastalgia and should not bee used in psychiatric patients.
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Ginseng
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These two illegal sedatives are CNS depressants that interfere with memory formation, but are not considered addictive.
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GHB, Rohypnol
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These illegal substances are not considered addictive, but alter mood via direct, quick action on CNS and can often cause neuronal death.
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Inhalants
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These substances, while not addictive, are often used in sexual activity by causing transient hypotension.
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Nitrites
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This substance increases serotonin release along with some DA, NE, is considered a psychostimulant; often a designer drug.
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MDMA (Ecstasy)
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This drug, while not considered addictive, causes psychodelic experiences via agonism at 5HT2 and 5HT1A receptors.
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LSD
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These two drugs, while not addictive, cause paralysis without unconsciousness (often associate with violence) via NMDA receptor antagonism.
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PCP, Ketamine
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This drug is used to treat the symptoms of opioid withdrawal and is an a2 adrenergic agonist.
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Clonidine
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This is the MOA for opioid withdrawal.
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SNS outflow from loss of opiod inhibition at the locus coeruleus
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This drugs is used for long term opioid intervention because it is a full agonist at mu with a long half life. It causes cross tolerance with heroin so relapse can often become fatal.
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Methadone
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This drug is used for the long term management of opioid intervention because it is a partial mu agonist and is given orally. Giving with orally inactive naloxone can prevent abuse by injection.
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Buprenorphine
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This family of drugs is used in the treatment of alcohol detox.
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Benzodiazepines
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Name three drugs used in the long-term management of alcohol withdrawal.
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Disulfuram, Naltrexone, Acamprosate
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This drug is used to block aldehyde dehydrogenase.
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Disulfuram (Antibuse)
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This drug is use to treat alcohol dependence by blocking desire; it is a long acting mu opioid receptor antagonist.
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Naltrexone
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This GABA analog competes with alcohol to treat alcohol dependence.
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Acamprosate
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This drug is used for smoking cessation because it binds as a partial agonist with greater affinity than nicotine to AChR. While more effective that buproprion, it does not protect against weight gain.
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Varenicline (Think NICOTINE)
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What are the four stages of anesthesia?
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Analgesia; Excitement; Surgical Anesthesia; Medullary Depression
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What stage of anesthesia do you want to limit in duration?
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Excitement II
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What stage of anesthesia do you want to avoid?
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Medullary Depression IV
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These are the five factors that determine the rate at which a therapeutic concentration in the brain is achieved by general anesthetic.
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Solubility; Concentration in inspired air; Volume of pulmonary ventilation; Pulmonary Blood Flow; PP gradient between AV anesthetic concentrations
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What is the relationship between Partition Coefficient and Solubility for general anesthesia?
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Correlated (Low PC = low solubility)
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What is the relationship between blood solubility of inhaled anesthetic and onset of action?
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Inverse b/c blood partial pressure is inverse of solubility and directly related to onset of action.
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What is the function of anesthetic concentration in inspired air?
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Direct correlation to rate of induction (per Fick's law). Moderately soluble anesthetics can be give with less soluble to increase their rate of induction.
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How does pulmonary ventilation affect rate of anesthetic induction?
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Increases for anesthetics with normally slow onset, but a ceiling exists per the blood:gas coefficient; also, will only slightly speed up induction in low soluble anesthetics (they're already pretty fast).
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How does pulmonary blood flow affect rate of anesthetic induction?
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As flow increases, rate of induction actually decreases (inverse relationship). This is due to dispersement of anesthetic throughout the blood system reduces the tension of the anesthetic between the blood and brain compartments.
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How does the AV concentration affect rate of anesthetic induction?
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Inverse relationship. If gradient exists (i.e. little anesthetic in venous blood), then tissue are stealing (heart, liver, kidneys, GI, etc) anesthetic and it will take longer to reach equilibrium for tension at the blood:brain barrier.
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This measurement is defined as the median concentration that results in the immobility in 50% of patients when exposed to a noxious stimulus.
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Minimum Alveolar Anesthetic Concentration (MAC)
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How do we measure anesthetic doses as individual units?
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Multiples of MAC; 1 MAC=immobility in 50% of patients
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What is a limitation of MAC, especially with nitrious oxide?
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Even if MAC value is > 100%, nitrous oxide limitations at the alveoli result in MAC less than 1.
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How do anesthetic adjuncts (e.g. opioids, etc.) affect MAC?
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Decrease in a dose-dependent fashion (i.e. less anesthetic required if adjuncts available).
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If using two anesthetics, how do MAC values interrelate?
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They are additive with inhaled anesthetics.
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How are potency and MAC related?
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Inverse: Potency = 1/MAC; higher the MAC, lower the potency (e.g. nitrous oxide MAC higher than halothane and less potent)
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What is the general affect of inhaled anesthetics on cerebral blood flow and vascular resistance?
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Decreased vascular resistance from anesthetics results in increased CBF.
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This inhaled anesthetic has the highest potency; however, it does risk heavy hepatotoxicity and hepatitis.
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Halothane
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This IV anesthetic is a highly soluble barbituate that reaches plasma equilibrium quickly, but soon diffuses to other tissues. It is a potent respiratory depressant and decreases CO, but is ok for pts with high ICP.
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Thiopental
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What blood syndrome are all barbituates contraindicated in?
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Porphyrias
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This benzodiazepine is water soluble (decrease injection pain) and therefore is used as an IV anesthetic.
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Midazolam
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What is the antidote treatment for benzodiazepine overdose? What is a major warning regarding this drug?
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Flumazenil; short duration of action may require multiple dose
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This is the most popular iv anesthetic (rapid onset and action like benzos) that probably involves GABA receptors and is used for the induction and maintenance (once stop) of anesthesia.
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Propofol (Milk of Amnesia)
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This iv anesthetic is used for induction because of its rapid, short duration of action; it has no analgesic effects so opioids should be give also. It probably has GABA activity, but has minimal cardiac and respiratory effects.
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Etomidate
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This iv anesthetic is an antagonist of NMDA and produces dissociative anesthesia. It also has analgesic properties and CV stimulation (so don't use when ICP is high). While popular because of limited ventilatory depression, it produces very serious emergence delirium.
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Ketamine (the only way to fly)
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This word describes intense analgesia and amnesia brought on by the combination of a neuroleptic (droperidol) and analgesic (fentanyl)
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Neuroleptanalgesia
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This term indicates unconsciousness produced by adding nitrous oxide to a neuroleptic (droperidol) and analgesic (fentany)
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Neuroleptanesthesia
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What is the mechanism of action of lithium in bipolar treatment?
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All about inositol and decreasing excitatory intracellular singalling.
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What drugs should be avoided when giving lithium because of EPS?
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Typical antipsychotics
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What is the difference between a sedative and a hypnotic?
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Sedative reduces anxiety and hypnotics induce onset and maintenance of sleep.
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What is the difference between high doses of barbiutates versus benzodiazepines?
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Lower doses are anxiolytic and higher doses are hypnotic, but benzodiazepines plateau and do not lead to anesthesia and coma (safer).
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What is the difference between binding sites of benzodiazepines and barbiutates?
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Both bind to GABA receptors (not at GABA site); Benzo = Freq = Alpha; Barbs = Beta = duration
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What are the longest acting benzodiazepines? Why? What are the shortest?
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Chlordiazepoxide and Diazepam because the break down into Desmethydiazepam and then to Oxazepam (both active metabolites). Triazolam is the shortest at 6hr half life.
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What are the mechanisms (different) for barb and benzo tolerance?
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Barbs: increased rate of metabolism; Benzos: down-regulation of BZ binding site
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What two withdrawals can be fatal?
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Alcohol (Delirium Tremens) and Barb/Benzos (convulsions)
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How do benzos affect sleep?
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Decrease time in slow wave; increase stage 2; increase REM cycles but decrease REM duration.
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This hypnotic that increases slow wave sleep, but decreases time in REM; however, it shortens sleep latency and prolongs sleep.
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Zolpidem (Ambien)
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This hypnotic decreases latency of sleep onset but has little effect on sleep architecture. It acts rapidly with a short half life.
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Zaleplon (Sonota)
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This hypnotic increases sleep time and stage 2 sleep, but little other effects at low doses. It will affect REM as dose increases. It has a long half life.
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Eszopiclone (Lunesta)
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This drug does not interact with GABA, but is used as a sedative-hypnotic because of its 5HT1A and D2 agonist properties.
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Buspirone
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This sedative-hypnotic has no action on GABA, but is a melatonin receptor agonist. It should not be used with fluvoxamine because it of interactions. Its active metabolite has a long half life.
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Ramelteon (think MEL)
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This benzo can be used for the elderly because of its extrahepatic metabolism.
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Oxazepan
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This drug is safe for viral hepatitis.
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Olanzapine
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