Term
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Definition
BNZ - approved for insomnia;
Modify the response of GABA receptor to GABA (shift dose response curve left);
Require GABA to act;
Morning after symptoms (sedation, cognitive impair);
Withdrawl - anxiety, OSA, ventilatory impairment;
Hepatic metabolism with active intermediates;
Pregnancy category X, schedule IV;
Drug-drug interactions at CYP-P450s |
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Term
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Definition
BNZ - approved for insomnia;
Modify the response of GABA receptor to GABA (shift dose response curve left);
Require GABA to act;
Morning after symptoms (sedation, cognitive impair);
Withdrawl - anxiety, OSA, ventilatory impairment;
Hepatic metabolism with active intermediates;
Pregnancy category X, schedule IV;
Drug-drug interactions at CYP-P450s;
METABOLIC ACCUMULATION |
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Term
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Definition
BNZ - approved for insomnia;
Modify the response of GABA receptor to GABA (shift dose response curve left);
Require GABA to act;
Morning after symptoms (sedation, cognitive impair);
Withdrawl - anxiety, OSA, ventilatory impairment;
Hepatic metabolism with active intermediates;
Pregnancy category X, schedule IV;
Drug-drug interactions at CYP-P450s;
METABOLIC ACCUMULATION |
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Term
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Definition
BNZ - approved for insomnia;
Modify the response of GABA receptor to GABA (shift dose response curve left);
Require GABA to act;
Morning after symptoms (sedation, cognitive impair);
Withdrawl - anxiety, OSA, ventilatory impairment;
Hepatic metabolism with active intermediates;
Pregnancy category X, schedule IV;
Drug-drug interactions at CYP-P450s |
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Term
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Definition
BNZ - approved for insomnia;
Modify the response of GABA receptor to GABA (shift dose response curve left);
Require GABA to act;
Morning after symptoms (sedation, cognitive impair);
Withdrawl - anxiety, OSA, ventilatory impairment;
Hepatic metabolism with active intermediates;
Pregnancy category X, schedule IV;
Drug-drug interactions at CYP-P450s |
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Term
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Definition
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Term
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Definition
BRA - approved for insomnia;
Modify the response of GABA receptor to GABA (shift dose response curve left);
Require GABA to act;
Specific for BZ-1 receptor at approved doses;
No clinically crucial lethality;
Pregnancy category C (Okay, but caution), schedule IV; |
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Term
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Definition
BRA - approved for insomnia;
Modify the response of GABA receptor to GABA (shift dose response curve left);
Require GABA to act;
Specific for BZ-1 receptor at approved doses;
No clinically crucial lethality;
Pregnancy category C (Okay, but caution), schedule IV;
ETHNIC VARIABILITY - Asians, must dec the dose |
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Term
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Definition
BRA - approved for insomnia;
Modify the response of GABA receptor to GABA (shift dose response curve left);
Require GABA to act;
Specific for BZ-1 receptor at approved doses;
No clinically crucial lethality;
Pregnancy category C (Okay, but caution), schedule IV; |
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Term
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Definition
BNZ and BRA antagonist !;
Reversal of sedation or overdose;
IV admin- short duration calls for re-dose to cover the longer-acting BNZs;
Effects: Abrupt awakening, dysphoria, agitation;
Doesn’t reverse effects of barbiturates, opiate agonists, TCAs |
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Term
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Definition
Barbiturate - Approved for insomnia;
Adverse effects - porphyria, metabolic enzyme induction;
Caution w/ COPD, CNS depressants, operating machinery;
Fallen from favor due to toxic profile;
Lethal at high doses;
EXTENSIVE HEPATIC METABOLISM |
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Term
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Definition
Barbiturate - Approved for insomnia;
Adverse effects - porphyria, metabolic enzyme induction;
Caution w/ COPD, CNS depressants, operating machinery;
Fallen from favor due to toxic profile;
Lethal at high doses;
(NO extensive hepatic metabolism) |
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Term
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Definition
Barbiturate - Approved for insomnia;
Adverse effects - porphyria, metabolic enzyme induction;
Caution w/ COPD, CNS depressants, operating machinery;
Fallen from favor due to toxic profile;
Lethal at high doses;
EXTENSIVE HEPATIC METABOLISM |
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Term
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Definition
Barbiturate - Approved for insomnia;
Adverse effects - porphyria, metabolic enzyme induction;
Caution w/ COPD, CNS depressants, operating machinery;
Fallen from favor due to toxic profile;
Lethal at high doses;
(NO extensive hepatic metabolism) |
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Term
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Definition
Barbiturate - Approved for insomnia;
Adverse effects - porphyria, metabolic enzyme induction;
Caution w/ COPD, CNS depressants, operating machinery;
Fallen from favor due to toxic profile;
Lethal at high doses;
EXTENSIVE HEPATIC METABOLISM |
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Term
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Definition
Melatonin receptor agonist;
Not a schedule drug;
No residual effects (morning after);
Drug interactions with substrates of CYP1A2 (2C9, 3A4);
No metabolic accumulation;
Adverse effects - HA, nausea, URI, Somnolence, insomnia (paradox);
No MT3 activity;
Higher receptor specificity than melatonin, ↘ dose |
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Term
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Definition
| Attenuation of SCN activity, induces sleep |
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Term
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Definition
| Maintenance of circadian rhythm |
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Term
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Definition
TC-Antidepressant;
Induce sedation;
Use doses lower than those from primary indication;
Not schedule drug;
Large toxic profile (slide 82) |
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Term
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Definition
Heterocyclic Antidepressant;
Induce sedation;
Use doses lower than those from primary indication;
Not schedule drug;
CYP metabolism and possible interactions;
Suicidal ideation (BB WARNING);
SEs on endocrine |
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Term
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Definition
Heterocyclic Antidepressant;
Induce sedation;
Use doses lower than those from primary indication;
Not schedule drug;
CYP metabolism and possible interactions;
Suicidal ideation (BB WARNING);
SEs on endocrine |
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Term
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Definition
Anticonvulsant used for off-label insomnia;
Unknown mechanism; not GABA, not Na channel blocker;
SE - Fatigue, weight gain, dizziness, ataxia, nystagmus |
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Term
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Definition
Antipsychotic used for off-label insomnia;
Mech – sedation via H1 receptors;
SE - QT prolongation, orthostatic hypotension, weight gain, constipation, xerostomia |
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Term
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Definition
1st Generation antihistamine;
cross BBB for H1 antagonism;
SE - Xerostomia, blurred vision, urinary retention, inc intraocular pressure (think glaucoma!);
Rapid tolerance with rebound insomnia;
Caution in elderly |
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