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67 Cards in this Set
- Front
- Back
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What are vericosities and how do they play a role im MDD?
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Vesical mediated release systems which release large amounts of NT's into the diffuse extracellular space causing global effects in the brain. Serotonergic and adrenergic systems are examples of vericosities which are abnormal in MDD.
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what controls the release of -HT and NE?
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they autoregulate themselves
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what is serotonin synthesized from?
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tryptophan
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what is the rate limiting step in serotonin production?
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the step mediate by tryptophan hydroxylase
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why is NE synthesized from?
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tyrosine
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what is the rate limiting step in the formation of NE?
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the conversion of tyrosine into L-DOPA by tyrosine hydroxylase
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what regulates the activity of the the rate limiting enzymes in the formation of NE and serotonin?
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autoregulatory receptors which bind serotonin or NE
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how do monoamines get into the vesicles of the vericosity systems?
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monoamine transporter (VMAT) which is powered by a proton gradient
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describe the frequency of release of NE and 5-HT in the neuron over time?
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they are released tonically and the frequency of release is determined by autoregulation
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what happens to the monoamines which are not repackaged into vesicles after the re-uptake from the extracellular space?
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they are degraded by monoamine oxidase
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receptors for serotonin and NE are all what type of receptor except for one?
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G-coupled
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what are the 4 monoamine receptors what are important in MDD?
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1. 5-HT1A
2. 5-HT1D 3. 5-HT2A 4. 5-HT2C |
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which of the important receptor types in MDD is responsible for autoinhibitory action of 5-HT neurotransmission?
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5-HT1D receptors
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which of the adrenergic receptors is responsible for the autoinhibitory actions of NE or NE neurotransmission?
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alpha-2 receptora
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Why does the antihypertensive drug reserpine cause depression?
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it inhibits the uptake of NE, 5-HT, and dopamine into synaptic vesicles
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what is the effect of imipramine and iproniazid?
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increase neurotransmission of monoamines
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what is the monoamine hypothesis for depression?
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that it is a deficiency in the central monoamine systems that causes depression
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what is the limitation of the monoamine hypothesis?
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that despite drugs which increase the level of monoamine neurotransmission, 33% of MDD patients do not get well
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how do tricyclic antidepressants work to increase the neurotransmission of monoamines?
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the block re-uptake
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the inhibition of which MAO enzyme is responsible for the anti-depressant effects of MAO inhibitors?
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MAO-A
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the side effects of MAOI's are mainly due to what?
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blockade of alpha-adrenergic receptors causing hypotension and lightheadedness
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what is the specific opioid that you want to avoid if a patient is taking MAOI's?
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Meperidine
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TCA's with secondary amines primarily effect which NT system?
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NE
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TCA's with tertiary amines primarily effect which NT system?
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5-HT
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what are the 4 TCA drugs which are representative of the TCA class?
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1. Imipramine
2. Desipramine 3. Amitriptyline 4. Nortiiptyline |
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which antidepressants are most likely to cause conduction-delays such as first-degree atrioventricular and bundle branch blocks?
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TCA's
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Why are TCA's rarely used?
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they have a very narrow therapeutic window and a 7-10 day supply can be enough to kill
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the side effects of TCA's are caused by their high affinity for what 3 receptors?
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1. H1
2. M1 3. alpha-1 |
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which of the TCA's has the highest side effect profile?
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Amitriptyline
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which of the TCA's has the lowest side effect profile?
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1. Desipramine
2. Nortyiptyline |
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In addition to depression what other disorders are SSRI's efficacious treatments?
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1. OCD
2. Panic Disorder 3. PTSD 4. Social Phobia |
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Why are SSRI's the DOC in the treatment of depression?
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the have a mild side effect profile
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what are the four SSRI's we should know?
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1. Flouxetine
2. Paroxetine 3. Sertraline 4. Citalopram |
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why must precaution be taken when perscribing other medications with SSRI's?
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they inhibit cytochrome P450 isoenzymes thus may effect metabolism of some drugs
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The following side effects are caused by SSRI activity at which receptor?
anxiety (limbic system), akathisia (basal ganglia), myoclonus(brainstem sleep centers), sexual dysfunction—orgasm and ejaculation (spinal cord), apathy and decreased libido (mesocortical pleasure centers) |
HT2A
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The following side effects are caused by SSRI activity at which receptor?
anxiety and panic attacks (limbic system) |
5HT2C
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The following side effects are caused by SSRI activity at which receptor?
nausea and vomiting (hypothalamus and brainstem), gastrointestinal cramps and diarrhea (GI tract) |
5HT3
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The following side effects are caused by SSRI activity at which receptor?
increased bowel motility, cramps and diarrhea (GI tract) |
5HT4
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what are the mixed NE-5HT reuptake inhibitors?
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1. Venlafaxine
2. Duloxetine |
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What must always be monitered in patients on the mixed reuptake inhibitor Venlafaxine?
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diastolic BP
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what is the most effective treatment for the painful symptoms of depression?
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TCA's
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Which drug does the following describe?
Mechanism unclear: Augments NE release; dopamine (DA) reuptake inhibition Side Effects Increased risk of seizures in up to 0.4% of patients, esp. if positive history of seizures or bulimia nervosa, so contra-indicated in those patients. There is a very low incidence of sexual dysfunction, and is weight neutral—probably because it lacks a significant serotonergic component in its mechanism of action. Also useful in decreasing the craving associated with smoking cessation. |
Bupropion
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Which drug does the following describe?
Mechanism: 5HT2a antagonist, weak 5HT reuptake inhibition Side Effects Is associated with Priaprism (estimated risk of 1:6,000-8,000 men, needing surgical treatment in about a third of cases). Extremely sedating, so difficult to dose adequately for antidepressant effects, therefore primarily prescribed in lower dosages for purpose of treating insomnia. |
Trazodone
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Which drug does the following describe?
Mechanism: alpha-2adrenegic antagonist that enhances noradrenergic neurotransmission. Additionally, increases transmission of serotonin and is a 5HT2A and 5HT3 blocker Side Effects Marked sedation and weight gain (antihistamine effects) are common, usually decreasing after the first weeks of treatment and at higher doses, which may provide more activation due to greater noradrenergic enhancement. There is a very low incidence of sexual dysfunction. |
Mirtazapine
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what happens when you give antidepressants to the bi-polar patient?
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can induce mania
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what might you see with chronic antidepressant use in bi-polar patients?
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increase in the speed of the mood cycling
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which two antidepressants decrease seizure levels to a clinically significant degree?
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1. Bupropion
2. TCA's |
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what is the only antidepressant with no associated sexual dysfunction of weight gain?
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buproprion
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what are the important OD effects seen with MAOI's?
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1. Hypertensive crisis
2. Hyperexia |
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Explain the way lithium gets into cells and its mechanism of action?
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Lithium enters the cells via Na+ channels and blocks phosphatidylinositol signaling via inositol phosphatase. This blocks regeneration of PIP2 thus inhibiting central adrenergic, muscarinic, and serotonergic neurotransmission via IP3 and DAG
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what is the only medicine known to reduce the chance of suicide in bipolar disorder?
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lithium
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what is the first line of treatment for bipolar disorder?
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lithium
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explain the effects of lithium on 5-HT, NE, and dopamine neurotransmission?
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increases 5-HT, decreases NE and dopamine
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what component of the diet effects levels of lithium in the body?
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salt content - higher salt content means better clearence of lithium
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what should be minotored closely over time with lithium use?
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thyroid function
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severe OD of lithium (greater than 2.5 mEq/L) will be treated how?
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hemodialysis
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what is the diuretic which is most notorius for causing lithium levels to rise above therapeutic levels?
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thiazide
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what OTC drugs elevate lithium levels?
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NSAIDs
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what blood pressure medication elevates lithium levels?
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ACE inhibitors
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describe the mechanism of action for valproic acid in the treatment of bipolar disorder?
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increases GABA levels in the CNS by either blocking re-uptake or blocking degredation
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what patient population are valproic acid and carbamazepine not appropriate for?
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women of child-bearing age
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what is the mechanism of action for lamotrigine?
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it is a neuronal membrane stabalizer by its effects on voltage-sensitive sodium channels - reduces presyntaptic release of glutamate and apartate
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what is stevens-johnson syndrome and how is it caused?
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pervasive and dangerous rash formation brought on by the use of lamotrigine
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describe the perscribing precautions and uses for lamotrigine?
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it needs to be perscribed in slowly increasing incriments to avoid stevens-johnson syndrome and is best for treatment of depression in bipolar disorder
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what are the two anticonvulsants that are effective in treating bipolar disorder?
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1. topiramate
2. Gabapentin |
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which of the anticonvulsant treatments should be avoided in women of childbearing age?
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topiramate
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explain why atypical antipsychotics are effective for treatment of bipolar disorder?
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blockade of D2 receptors and antagonism of other monoamine receptors
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