Term
| All sedative/hypnotics except for ______ are general CNS _________ capable of producing _________ that can progress to _________ |
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Definition
1. Benzodiazepines
2. depressants
3. dose-dependant CNS depression
4. medulla oblongata depression, coma, death |
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Term
| Mechanism of action: BDZs |
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Definition
| positive allosteric modulators of GABA-operated chloride channels. Straddles the alpha and gamma subunit. Increaes the frequency at which chloride channels are opened by GABA sothat they increase synaptic inhibition (but they NEED GABA) |
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Term
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Definition
| oral, sometimes i.m. or iv for more rapid onset |
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Term
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Definition
| lipid soluble but bound to plasma proteins so get lower Vd than expected |
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Term
| Metabolism/Excretion: BDZ |
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Definition
| b/c lipd, must be metab by liver before excreted by kidney |
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Term
| what are the 3 classes of BDZ |
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Definition
| Long, intermediate, short T 1/2 lives |
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Term
| Which BDZs are in the long T1/2 life class? (> 1 day) |
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Definition
| flurazepam, chlordizepoxide, clorzepate, diazepam |
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Term
| What BDZs are in the intermediate T1/2? (6-24hr) |
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Definition
| temazepam, estazolam, lorzepam, oxazepam |
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Term
| What BDZs are in the short T1/2 (less than 6 hrs) |
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Definition
| triazolam, zolpidem, midazopam |
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Term
| Flurazepam is what kind of drug? |
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Definition
|
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Term
| chlordiazepoxid is what kind of drug? |
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Definition
|
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Term
| clorazepate is what kind of drug? |
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Definition
|
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Term
| diazepam is what kind of drug? |
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Definition
|
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Term
| Temazepam is what kind of drug? |
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Definition
|
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Term
| estazolam is what kind of drug? |
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Definition
|
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Term
| lorazepam is what kind of drug? |
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Definition
|
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Term
| Oxazepam is what kind of drug? |
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Definition
|
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Term
| triazolam is what kind of drug? |
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Definition
|
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Term
| Zolipdem is what kind of drug? |
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Definition
| a non BDZ (alpha1 subunit selective on GABA) with short T1/2 |
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Term
| Midazopam is what kind of drug? |
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Definition
|
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Term
| Where are the GABA reecptors that are not potentiated by BDZs located? |
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Definition
|
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Term
| T or F. BDZs are analgesic? |
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Definition
| F except in some forms of neuropathic pain |
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Term
|
Definition
Anxiolytic
SEdation, muscle relaxation, anticonvulsant
Hypnosis, anterograde amnesia
Ataxia, confusion
Suptor |
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Term
| What are the two parameters that the intensity of withdrawal sx depend on? |
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Definition
the higher the dosage the more severe
the longer the T1/2 the less severe |
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Term
|
Definition
excessive sedation and impaired motor performance
additive effects w/ other CNS depressants
adversely affect breathing in people with compromised respiration |
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Term
| What type of BDZ (long, intermediate, short T1/2) is good for tx generalized or non-specific anxiety? |
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Definition
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Term
| What type of BDZ (long, intermediate, short T1/2) is good for preanesthetic med? |
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Definition
| Intermediate (lorazepam) or short (midazolam) i.v. |
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Term
| What BDZ is useful for absence seizures? |
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Definition
|
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Term
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Definition
insomnia (hypnotic effect),
anxeity (sedative effect),
preanesthetic med
absence seizures
staus epilepticus
suppress dangerous sx of withdrawal from CNS depressants (esp ethanol) |
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Term
| What is the drug that bind to the same sites of GABA receptors as BDZs but produces no effect of its own? |
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Definition
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Term
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Definition
A BDZ antagonist, it can be used to reverse sedative effects of BDZ
Reverse BDZ overdose |
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Term
| Mechanism of Action: Busprione |
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Definition
| partial agonist acitivty at 5HT1A receptors; does not interact with GABA-gated Cl- channels |
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Term
| What type of drug is buspirone? |
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Definition
| anxiolytic (but not a sedative hypnotic) |
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Term
| How is buspirone different from BDZs? |
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Definition
doesn't use GABA channels
lacks BDZ side effects (sedation)
free of tolerance/dependence/withdrawal
less effective tx severe anxiety
lacks sedative/ataxic, anticonvulsant, or muscle relaxant effects
no "rebound" anxiety upon withdrawal |
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Term
| What are the sedative/hypnotic drug categories? |
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Definition
| BDZs, barbituates, alcohol, miscellaneous (antihistamine, alpha 2 agonist, archeodrugs) |
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Term
| Why can't non-BDZs be use to produce surgical anesthesia? |
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Definition
| there is too small a gap between anesthetic doses and those that cause cardiovascular collapse |
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Term
| Pharmacodyanmic tolerance: nonBDZ sedative/hypnotics |
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Definition
| develops rapidly to all CNS despressant effects EXCEPT to lethal respiratory and cardiovascular depression with cross tolerance between all members of the group |
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Term
| PHysical dependance: nonBDZ sedative/hypnotics |
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Definition
| major physical dependence and withdrawal can be lethal |
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Term
| physical dependence of BDZ sedative/hypnotics |
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Definition
| usually mild and depedence on dosage and T1/2 of drug |
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Term
| What are the barbituates sedative/hypnotics? |
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Definition
| phenobarbital, thiopental, secobarbital |
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Term
| Which barbituate can be used as an anticonvulsant? |
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Definition
|
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Term
| what are the effects of barbituates on microsomal enzymes? |
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Definition
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Term
| which barbituate is esp good at inducing microsomal enzymes? |
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Definition
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Term
| What short acting barbituate can be used for anesthesia |
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Definition
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Term
| Mechanism of action: barbituates (low and high dose) |
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Definition
low dose: potentiate GABAergic transmission
high dose: promote Cl-influx trhough GABA gated channels independently of GABA. |
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Term
| mechanism of action: alcohol as sedative/hypnotic |
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Definition
| increases GABA receptor/CL- channel function |
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Term
| Side effect profile of alcohol: |
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Definition
liver damage as acetaldehyde depletes hepatic glutathione
disruptes nl sleep patterns
exacerbates sleep apnea
produces cutaneous vasodilation but overall increases vasoconstriction and increases BP
Decrease release of ADH (anti diuretic) and oxytocin -> diuresis |
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Term
| Physical dependencd: alcohol |
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Definition
| severe and life threatening |
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Term
| How to tx alcohol withdrawal |
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Definition
| administer a BDZ, rehydrate, check electrolytes |
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Term
|
Definition
| Disulfiram, naltrexone, acamprosate |
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Term
| Mechanism of action: disulfiram |
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Definition
| inhibits aldehyde dehydrogenase leading to increased acetic acid and aversive side effects - supposed to discourage drinking |
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Term
| Mechanism of action: naltrexone |
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Definition
| orally active opaite receptor antagonist that attenuates rewarding effects of alcohol within the limbic forbrain. |
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Term
| Mechanism of action: acamprosate |
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Definition
| unclear. Attenuates alcohol craving and modestly reduces rate of relapse after detox. |
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Term
| Beneficial uses of alcohol? |
|
Definition
increase HDL/LDL ratio
tx of methanol or ehtylene glycol poisoning |
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