Term
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Definition
Inhibits presynaptic a2-adrenoceptors (autoR), which normally inhibits further NE release
Blockade amplifies the amount of NE released
(Also has indirect effects on 5HT transmission) |
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Term
| Tertiary amine TCAs, SNRIs: MOA |
|
Definition
Non-selectively block NE/5HT reuptake
-Clomipramine: 5HT>NE
-Imipramine: NE>5HT
-Venlafaxine: dose dependent = 5HT at low doses, both at high doses |
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Term
| Secondary amine TCAs: MOA |
|
Definition
| Selectively block NE reuptake |
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Term
|
Definition
| Selectively block 5HT reuptake |
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Term
|
Definition
Irreversibly inhibit MAO (effects last long after they're no longer present in the body, can take 10-14 days to resynthesize MAO to pre-drug levels after discontinuation)
Cytoplasmic NE rises
Transporter may work in reverse direction now, and dump NE from inside the cell into the synapse
(Also inhibits metabolism of 5HT and so increases cytoplasmic and thus synaptic concentrations in a similar manner) |
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Term
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Definition
|
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Term
| People with MDD need ___ with ADs to prevent relapse |
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Definition
| Long-term treatment with ADs |
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Term
|
Definition
Muscarinic: dry mouth, blurred vision, constipation and urinary retention, memory impairment, sexual dysfunction
H1: sedation, weight gain (chronic use)
A1 (non-cardio): sexual dysfunction |
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Term
|
Definition
Tachycardia (due to anticholinergic properties)
Orthostatic hypotension (due to A1-blocker properties)
Changes in conduction: flattened/inverted T waves, increased PR interval (normal? not really an issue; pre-existing heart disease? increased risk of AV block)
OD: severe arrhythmias |
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Term
|
Definition
Ataxia or fine, rapid tremor in extremities, especially in elderly receiving high doses
Initiation of manic episodes in bipolar
Lower seizure threshold |
|
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Term
|
Definition
Hepatic toxicity
CNS excitation (like amphetamines): tremors, insomnia, agitation, hypomanic/manic reaction in bipolar
Orthostatic hypotension due to increased stimulation of central A2-# or accumulation of false transmitter "octopamine" in PNS |
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Term
|
Definition
Ingestion of indirectly-acting sympathomimetic amines
Normally metabolized by MAO-A in GI tract
Inhibition allows things like tyramine to enter circulation
Means that there's an unusually high amount of NE released
Stimulation of A1-R raises BP causing a hypertensive crisis |
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Term
| SSRIs, venlafaxine: S/E (4) |
|
Definition
N/V
Sexual dysfunction
Asthenia: apathy, concentration problems, decreased motivation, fatigue
Late weight gain
No inhibition of MAO = no hypertensive crisis
No anticholinergic properties = no heart conduction abnormalities or muscarinic symptoms
No anti-A1 properties = no orthostatic hypotension |
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Term
|
Definition
|
|
Term
|
Definition
| Weight gain due to blockage of H1-R |
|
|
Term
| The overall efficacy of different ADs is ___ |
|
Definition
|
|
Term
| Autoreceptors are always ___ |
|
Definition
|
|
Term
| The presynaptic transporter is the ___ |
|
Definition
| Primary means for biogenic amine inactivation/removal from the synaptic cleft |
|
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Term
|
Definition
| No, it's sloppy medicine and marketing |
|
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Term
|
Definition
Clomipramine (3)
Imipramine (3)
Desipramine (2) |
|
|
Term
| SSRIs: drugs (6) "Some Patients Can Feel Fine Eventually" |
|
Definition
Sertraline
Paroxetine
Citalopram
Fluoxetine
Fluvoxamine
Escitalopram
"Some Patients Can Feel Fine Eventually" |
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|
Term
|
Definition
Bupropion
Duloxetine
Mirtazapine
Venlafaxine |
|
|
Term
|
Definition
|
|
Term
|
Definition
| Alprazolam Clomipramine Clonazepam Diazepam Lorazepam Oxazepam Triazolam |
|
|
Term
| Flumazenil: MOA, indications |
|
Definition
Competitive BZ-R antagonist
Indicated for rapid reversal of BZ effects when BZs are used as an anethesia adjunct in outpatient surgery |
|
|
Term
| GAD is most commonly treated using ___ b/c ___ |
|
Definition
Benzos
Efficacy and favorable S/E |
|
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Term
|
Definition
| BZs SSRIs Venlafaxine Buspirone |
|
|
Term
| Benzos produce a ___ of neuronal systems with more potent effects at ___ |
|
Definition
General depression
Polysynaptic connections |
|
|
Term
| BZs: pharmacologic effects (instant) |
|
Definition
Sedative-hypnotic
Anti-anxiety
Anti-convulsant
Muscle relaxant (spinal cord level)
Anterograde amnesia (surgery) |
|
|
Term
| BZs: MOA "Barbie stays longer" |
|
Definition
Bind to GABA-R between alpha-gamma subunits
Enhance chloride-channel opening
More chloride flows into the cell
Hyperpolarization and thus inhibition
They are not direct GABA-R agonists! |
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Term
|
Definition
Sedative hypnotics that produce super amnesia
Have no anti-anxiety, anti-convulsant, or skeletal muscle relaxant effects |
|
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Term
|
Definition
Eszopiclone
Zaleplon
Zolpidem |
|
|
Term
| Z-drugs: pharmacologic effects (6) |
|
Definition
BZ-R agonists
Short t1/2 (which make them good sedative hypnotics)
Little effect on sleep stages
Mild S/E: drowsiness, dizziness, headache
Less abuse potential
No alcohol potentiation |
|
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Term
| Ramelteon: MOA, indications |
|
Definition
Melatonin-1 and Melatonin-2-R agonist in suprachiasmatic nucleus
Helps maintain circadian rhythm and normal sleep/wake cycle
Indicated for insomnia with difficulty with onset of sleep |
|
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Term
| Ramelteon: pharmacologic effects (4) |
|
Definition
No affinity for GABA-A-R
Short t1/2
Mild S/E: drowsiness, dizziness, headache
No abuse potential |
|
|
Term
|
Definition
Primarily metabolized in liver via oxidation
In the case of ozazepam, it's conjugated to glucoronic acid, rendering it inactive, and excreted in urine (this process is unaffected by aging, unlike oxidation) |
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Term
|
Definition
Sedation
Dizziness
Uncoordination
Impaired cognitive function
Paradoxical agitation
Addictive with continued usage (>8mo)
Minimal OD potential on their own, but effects are potentiated with alcohol (both are depressants)
Little organ toxicity, minimal capacity to induce hepatic enzymes |
|
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Term
|
Definition
Usually in patients taking high doses or using BZs for >8mo, but can occur at clinically accepted doses
Avoided by slowly tapering the dose
Usually a flu-like syndrome: muscle cramps, ab discomfort, diarrhea
Can cause seizures (more frequent with short t1/2) |
|
|
Term
| Buspirone: MOA, pharmacologic effects (4) |
|
Definition
Directly activates 5HT1A-R, which increases K conductance, thus hyperpolarizing the neuron and inhibiting firing
Slower onset of action (need a BZ to fill in while the buspirone has yet to "take")
S/E: dizziness, nausea
No interaction with alcohol
No dependence or withdrawal |
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|
Term
| Benzos may help ___ anticipatory anxiety associated with panic attacks but may be ___ against the condition itself |
|
Definition
Minimize
Relatively ineffective |
|
|
Term
| Panic Disorder: BZ usage, risks of alprazolam |
|
Definition
High potency preferred b/c lower potency BZs cause too much sedation
May need higher doses of alprazolam than would be used for GAD
Run the risk of seizures and severe withdrawal upon cessation |
|
|
Term
| Panic Disorder: drug classes (4) |
|
Definition
|
|
Term
| Panic Disorder: TCA/MAOI/SSRI usage |
|
Definition
| Use the same doses for the same periods of time (as depression) to obtain effective control of PD symptoms |
|
|
Term
|
Definition
|
|
Term
| OCD-effective drugs must ___ |
|
Definition
|
|
Term
| OCD: Clomipramine has ___ but it's most distinctive among the TCAs for ___ |
|
Definition
NE-reuptake blocking effects
Potent inhibition of 5HT reuptake |
|
|
Term
|
Definition
SSRIs for women suffering from PTSD due to sexual/physical assault
No drug has proved effective for combat vets |
|
|
Term
|
Definition
SSRIs
TCAs are ineffective! |
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