Term
| What do Barbiturates and benzodiazipines demonstrate in reference to their mode of action |
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Definition
Dose dependent CNS depression..
Barbiturates being more toxic at higher doses - causing Coma & medullary depression
Benzo's being less toxic.. |
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Term
|
Definition
Clonazepam, Nitrazepam, Lorazepam (zepams)
Or
Diazepam, Flurazepam, Alprazolam (zolams)
Chlordiazepoxide
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Term
|
Definition
•Zolpidem
•Zaleplon
•Eszopiclone
•Ramelteon- melatonin receptor agonist
•Buspirone- anxiolytic agent
|
|
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Term
|
Definition
uses melatonion
to regulate sleep |
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Term
|
Definition
| GAD - generalised anxiety disorders |
|
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Term
| what is the MOA of BZD's ? |
|
Definition
BZD bind to BZ1 receptor on GABAa
Increases the FREQUENCY of CL- channel (GABAa agonist)
CNS depression
(does not mimic GABA thus less CNS depression) |
|
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Term
| what is the MOA of barbiturates? |
|
Definition
Act on the GABAa receptor
PROLONG the DURATION of CL- channel opening
CNS depression
(inhibitory affect to glutamate receptors)
they mimmic GABA thus you get more CNS depression |
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Term
| What is the MOA of non BZD drugs.. |
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Definition
Act on the BZ1 site of the GABAa
causing CNS depression |
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Term
Which barbiturate has a large effect on the CNS?
why?
Use?
what BZD has a similar effect? |
|
Definition
Thiopentone
Highly lipid soluble - unionized
RAPID ONSET OF ACTION
used in induction of general ansthesia
Triazolam |
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|
Term
Name the short acting BZD's
Why are they short acting? |
|
Definition
Lorazepam
Tamazepam
Oxazepam
Alprazolam
Midazolam
Triazolam
They do not produce an active metabolites in the body.. they are conjugated with glucuronide & excreted out of the body |
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Term
Name the long acting BZD's
why are they long acting?
when would they be contraindicated? |
|
Definition
Clordiazepoxide
Clorazepate
Diazepam
Halazepam
Prazepam
Flurazepam
Quazepam
Estrazolam
They are metabolised in the body via hydrolysis before conjugation thus producing an active metabolite that has longer duration of action
contraindicated in elderly |
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Term
What is the duration of action of non BZD's
why is this advantageous? |
|
Definition
Non BZD's are rapidly metabolised by the liver enzymes thus they have a very short t 1/2,
thus good in use of ppl with short term insomnia.. low potential to cause dependance/tolerance
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Term
How are BZD's excreted?
what increases BARBITURATE excretion & why? |
|
Definition
Excreated by kidney
they are acidic thus alkylating the urine will enhance excretion |
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Term
| WHat are the effects of BZD's on sleep pattern? |
|
Definition
•Shortens time taken for onset of sleep
• Increases sleep duration
•REM sleep is decreased
•On discontinuation (barbiturates, triazolam)
rebound increase in REM sleep
hangover (irritability, dizziness, mood upset)
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Term
| Uses of BZD's at different doses |
|
Definition
1. low does - anti anxiety
2. high dose - general anaesthesia |
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Term
| What drugs are used as inducing anaesthesia? |
|
Definition
|
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Term
| WHich BZD's are used as IV anaesthesia |
|
Definition
Diazepam
Lorazepam
Midazolam |
|
|
Term
| WHat BZD's are used as anticonvulsants? |
|
Definition
Clonazepam
Nitrazepam
Lorazepam
Diazepam
Phenobarbitol |
|
|
Term
| What are the effects of BZD's on RS & CVS |
|
Definition
Respiratory depression
Fall in BP |
|
|
Term
| What are the uses of BZD's? |
|
Definition
1. Anxiety disorders - sedation
2. Causes hypnosis - treats insomnia as they are drugs that induce sleep
3. Eclampsia - antiemmetic in pregnancy
4. Alcohol withdrawal
5. DOC for status epilepticus (diazepam)
6. muscle spasm
7. febrile convulsions in children |
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|
Term
| what is the DOC for status epilepticus (prolonged seizure fro more than 20 mins) |
|
Definition
|
|
Term
| diazepam is the DOC for what? |
|
Definition
statys epilepticus
Febrile convulsions
alcohol withdrawl |
|
|
Term
| what is the DOC for panic disorders/phobias |
|
Definition
|
|
Term
| What is Alprazolam used for? |
|
Definition
| Panic disorders & agrophobias |
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|
Term
| What is Midazolam used for |
|
Definition
| Preanesthatic med.. given via IV |
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|
Term
| What BDZ is used for insomnia |
|
Definition
|
|
Term
| What is Triazolam used for? |
|
Definition
|
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Term
| Which BZD's drugs are safer to use in older pts & why? |
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Definition
| Oxazepam & lorazepam as they do not form active metabolites thus have a shorter duration of action |
|
|
Term
| what is the date rape drug? |
|
Definition
|
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Term
| WHen & Why are oxazepam and lorazepam used? |
|
Definition
| Insomnia in older patients as it does not produce active metabolites |
|
|
Term
What is used for BZD overdose?
when is it contraindicated? |
|
Definition
Flumazenil
contraindicated in BZD abusive mother as it increases the risk for seizures in newborn |
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|
Term
| When is phenobarbitone used? |
|
Definition
|
|
Term
| When an individual has tolerance to alcohol how will they react to BZD's |
|
Definition
| cross tolerance thus a higher dose is required |
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|
Term
| What are the major ADR of BZD's? |
|
Definition
Tolerance
Psychological & physiological dependance
CYP 450 inducer
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|
|
Term
Buspirone
1.MOA
2.Use
3. advantages over BDZ's? |
|
Definition
1. partial agonist of 5HT1a (serotonin)
2.GAD - generalized anxiety disorder
3. No rebound anxiety or rebound symptoms on abrupt discontiunance
No physical dependance
DOES NOT AFFECT DRIVING SKILLS! |
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Term
| What is used to treat GAD? (geeralised anxiety disorder?) |
|
Definition
|
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Term
|
Definition
1. affects melatonion - circadian rhythem agonist at the MT1 and MT2 receptors
2. INSOMNIA (DOC) |
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Term
|
Definition
Induce metabolism (enzyme inducers)
oral contraceptives
Phenytoin
Warfarin |
|
|
Term
| BDZ's have a synergistic effect with what? |
|
Definition
other BZD's (general ansthetics)
alcohol
antihistaminics
opiates |
|
|
Term
|
Definition
Phenobarbitol
Pentobarbitol
Secobarbitol
Thiopentone |
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