1B CNS : Hypnotics and Sedatives Flashcards
- fear response due to an appropriate stimulus
- the fear response is executed in the body by an extensive increase in what neurotransmitter release
anxiety
noradrenalin
the fear response consists of 2 components
CENTRAL COMPONENT - what location?
PERIPHERAL COMPONENT - what system is involved?
Central- locus ceruleus of the CNS
Peripheral- the sympathetic nervous system
a pathological fear response due to an inappropriate stimulus
anxiety disorder
a pathological fear response due to an inappropriate stimulus
anxiety disorder
there are 3 main types of anxiety disorders
- Generalized Anxiety Disorder
- Panic Disorder
- Phobia
MATCHING TYPE:
A. Generalized Anxiety Disorder
B. Panic Disorder
C. Phobia
- extensive repeating attacks of fear response
- chronic fear response without any definite stimulus
- fear response
GENERALIZED ANXIETY DISORDER - **chronic fear **response without any definite stimulus
PANIC DISORDER - extensive repeating attacks of fear response
PHOBIA - fear response
A drug that subdues excitement and calms the subject without inducing sleep, though drowsiness may be produced.
Sedative
refers to decreased responsiveness to any level of stimulation; is associated with some decrease in motor activity and ideation
Sedation
A drug that induces and/or maintains sleep, similar to normal arousable sleep.
Hypnotic
HYPNOTICS OR SEDATIVES?
quicker onset, shorter duration and steeper dose-response curves
hypnotics
HYPNOTICS OR SEDATIVES?
quicker onset, shorter duration and steeper dose-response curves
hypnotics
HYPNOTICS OR SEDATIVES?
**more slowly **acting drugs with **flatter dose-response **curves
sedatives
SLEEP STAGES
- EEG shows θ, δ and spindle activity,
-
K complexes can be evoked with** strong stimuli only. **
* Eye movements are few; subjects are not easily arousable
Comprises 5–8% of sleep time.
Stage 3
(deep sleep transition)
SLEEP STAGES
- From** lying down to falling asleep** and occasional nocturnal awakenings;
- constitutes **1–2% **of sleep time.
- EEG shows** α activity when eyes are closed** and **β activity when eyes are open. **
- Eye movements are irregular or slowly rolling.
Stage 0
(awake)
SLEEP STAGES
- α activity is interspersed with θ waves.
- Eye movements are reduced but there may be **bursts of rolling. **
- **Neck muscles relax. **
- Occupies 3–6% of sleep time
Stage 1
(dozing)
SLEEP STAGES
- * θ waves with interspersed spindles,
- K complexes can be evoked on sensory stimulation;
- * little eye movement;
- subjects are easily arousable
- This comprises **40–50% **of sleep time.
Stage 2
(unequivocal sleep)
SLEEP STAGE
- δ activity predominates in EEG,
- K complexes** cannot be evoked. **
- Eyes are practically fixed; subjects are difficult to arouse.
- Night terror may occur at this time.
- It comprises 10–20% of sleep time.
Stage 4
(cerebral sleep)
TRUE OR FALSE
- During stage 2, 3 and 4 heart rate, BP and respiration are steady and **muscles are relaxed. **
- Stages 3 and 4 together are called slow wave sleep (SWS).
Characteristics of REM sleep / paradoxical sleep
- EEG has waves of all frequency,
2.** K complexes cannot be elicited. **
3.There are marked, irregular
darting eye movements and irregular
darting eye movements; dreams and nightmares occur, which may be recalled if the subject is aroused. - Heart rate and BP fluctuate; respiration is irregular.
-
Muscles are** fully relaxed, but irregular body movements occur occasionally.
6. Erection occurs **in males. - About 20–30% of sleep time is spent in REM.
CLASSIFICATION OF HYPNOTICS
- BARBITURATES (long acting, short acting, ultra short acting)
- Benziodiazepines (hypnotic, antianxiety, anticonvulsant)
- Newer nonbenzodiazepines
Drugs under Barbiturates
1. long acting
2. short acting
3. ultra short acting
Long acting
* Phenobarbitone
Short acting
* Butobarbitone
* Pentobarbitone
Ultra-short acting
* Thiopentone
* Methohexitone
Drugs under Benzodiazepines that are HYPNOTICS
**Diazepam **
Flurazepam
Nitrazepam
Alprazolam
Temazepam
Triazolam
Drugs under Benzodiazepines that are ANTIANXIETY
Diazepam
Chlordiazepoxide
Clorazepate
Oxazepam
Lorazepam
Alprazolam
Drugs under Benzodiazepines that are ANTICONVULSANT
Diazepam
Lorazepam
Clonazepam
Clobazam
Drugs under Newer nonbenzodiazepine hypnotics
Zopiclone
Zolpidem
Zaleplon
Treatment of ____ is the most important use of this class of drugs.
insomnia
other drug classification that can be used in treatment of insomnia
- antihistaminics (promethazine, diphenhydramine)
- some** neuroleptic/ antidepressants** (chlorpromazine, amitriptyline)
- some anticholinergic (hyoscine) and
- opioids (morphine, pethidine)
have significant sedative action, but are not reliable for treatment of insomnia.
- General depressants of the CNS
- Largely obsolete as anxiolytic- and hypnotic drugs
- Are also abuse-drugs
- cause dependence
BARBITURATES
4 mechanisms by which they barbiturates can cause dependence
- POSITIVE REINFORCEMENT
- CONDITIONING
- TOLERANCE- Upregulation of the hepatic cytochrome P450 system (the enzyme system by which they are metabolize
- NEGATIVE REINFORCEMENT- Hallucinations
same as benzodiazepines
3 groups of barbiturates
A) SHORT-ACTING
B) INTERMEDIATE-ACTING
C) LONG-ACTING
3 groups of barbiturates
A) SHORT-ACTING
B) INTERMEDIATE-ACTING
C) LONG-ACTING
Group of barbiturates:
Short, Intermediate or long acting
- Less than 1 hour
- examples are METHOHEXITAL and THIOPENTAL
Short-acting
Indication: Induction of general anesthesia
- administered IV
- lipophilic , thus accumulate in adipose tissue over time
METHOHEXITAL
Side effect of Methohexital
- Euphoria
- Drowsiness (sedation)
- Respiratory depression
- Cardiovascular depression
- Death (if overdosed)
Group of barbiturates:
Short, Intermediate or long acting
- 1-6 hours
- examples are PENTOBARBITAL and BUTOBARBITAL
INTERMEDIATE-ACTING
- This drug is used for treatment of insomnia and treatment of anxiety
- Administered orally
- Not especially lipophilic, thus will not accumulate in adipose tissue
PENTOBARBITAL
Group of barbiturates:
Short, intermediate or long acting
* 6-12 hours
* example is PHENOBARBITAL
LONG-ACTING
Used for treatment of epileptic convulsions
PHENOBARBITAL
to act primarily at the GABA :BZD receptor–Cl¯ channel complex and* potentiate GABAergic inhibition* by increasing the lifetime of Cl¯ channel opening induced by GABA
Barbiturates
