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What are some physical effects of anxiety states and sleep disorders?
- -Chest Pain
- -Inc. sweating
- -Inc. heart rate
- -Inc. BP
What are examples of psychological symptoms assoc. with anxiety and sleep disorders?
- -Apprehension or dread
- -Trouble concentrating
- -Feeling tense
- -Irritability and Restlessness
What part of the brain regulates the heartbeat and other visceral functions as well as processes the emotion: fear?
What part of the brain is responsible for the establishment of long-term memory in regions of the cerebral cortex?
What do effective sedative drugs do?
Reduce anxiety and exert calmness
What do effective hypnotic drugs do?
Produce drowsiness and encourage sleep
What are sedative-hypnotic drugs used for clinically?
- -Relief of anxiety
- -Sedation and amnesia in medical and surgical procedures
- -Tx of epilepsy and seizures
- -As a component of balanced anesthesia (IV admin)
- -Control of ethanol or other sedative-hypnotic withdrawl states
- -Muscle relaxation - neuromuscular disorders
- -As diagnostic aids/tx in psychiatry
What class of antianxiety/sedative-hypnotic drugs are Benzodiazepines? (end in "pam" or "lam")
What are some examples of Benzodiazepines?
- Diazepam (1/2 = L) -anxiety, withdrawal, m. relax
- alprazolam (S) -insomnia, anxiety
- lorazepam (I) -insomnia, anxiety, m. relax
- midazolam (Ultra S) -pre-anesthetic med
Non-Benzodiazepines and class 2 drugs that interact with BZ receptors...what are some examples of these?
Pentobarbital, Phenobarbital, Amobarbital and Thiopental are examples of what class of drugs?
Barbiturates (end in "barbital")... which were once used extensively for antianxiety and sedation, but have been largely replaced by the BZ
Does increasing the dose of BZ result in general anesthesia or produce an analgesic affect?
NO - but does produce sedation, hypnosis, and stupor
What are the central effects of BZ?
BZs bind to GABAA rec in the limbic system --> enhancement of inhibition of neurons in the limbic system produce anxiolytic effects
What are the functional binding sites of GABAA rec and what is the effect of binding to each of these?
- GABA site - inc. Cl- conductance, hyperpolarization, - neuronal activity
- Barbiturate site - enhances GABA effect
- Benzodiazapine site - enhances GABA effect
- Picrotoxin site - Blocks Cl- channels
What are two examples of GABA antagonists? Which one acts competitively and which one non-competitively?
- Bicuculline (Competitive)
- Picrotoxin (Non-Competitive) - Block Cl- channel
Beta-carbolines are INVERSE AGONISTS which bind at the BZ binding site. what do they do and what symptoms do they cause?
- Dec. Cl- conductance
- Anxiety, irritability, agitation, delirium, convulsions
What is the name of the drug that blocks the effects of both agonists and inverse agonists (antagonist) and has no biological effects by itself, but can prec. withdrawl in BZ or BARB dep. persons?
What action does BZ have at the GABAA rec?
- Binds to rec (Cl- channel) --> enhances inhib effect of GABA by inc. Cl- influf (hyperpolarization)
- Inc. FREQUENCY of Cl- channel opening IN PRESENCE of GABA (no GABA no affect)
TRUE or FALSE: BZ have a low TI and overdose is usually life threatening.
- Acute Toxicity: Support resp and BP, gastric lavage, FLUMAZENIL (antag)
TRUE or FALSE: BZ are preferred over BARBS b/c they are safer.
TRUE or FALSE: Cross-Tolerance is not a problem with BZ
FALSE. Cross-tolerance can dev. w/other BZs and CNS depressants (ex. EtOH, BARBs)
Place the following in order of tolerance acquisition for BZ (lg-sm): Muscle Relaxant, Sedation, Anticonvulsant, Antianxiety
TRUE or FALSE: BZ are known to have several drug interactions
FALSE: BZ cause minimal induction of liver enz. thus produce few drug interactions
What affects are produced by Non-BZ drugs: Zolpidem & Zaleplon?
- Induce Sleep
- Hypnotic dose (no CV or resp effects unless disease state that causes CV dep)
- IV admin - marked CV and resp depressant effects
- *Extra: oral admin (peak plasma w/in 1-2hr) and met by CYP3A4 and partially by hepatic aldehyde oxidase (1/2 life 1/5-3hr)
List some peripheral effects of BARBs.
- Respiratory: dep w/increasing doeses
- CV: dep BP and HR @ sedative/hypnotic doses
- Liver: influence cytochrome P450 (induce drug metabolism and other enzymes)
What is the mechanism of action of BARBs?
- Inc the open time of Cl- channels in presence of GABA (inc. Cl-influx and - effects of GABA)
- At high conc. directly inc. Cl- conductance w/o GABA
What are common side effects assoc w/ BARBs?
drowsiness, confusion, diminished motor skills and impaired judgment
TRUE or FALSE: BARBS are known to have several drug interactions.
- BARBs enhance CNS dep. effects of antipsychotics, antihistamines, and ethanol
- BARBs enhance the metabolism of - beta-blockers, Ca channel blockers, corticosteroids, estrogens, phenothiazines, valproic acid, and theophylline
TRUE or FALSE: Overdose w/BARBs is usually life threatening?
- TRUE. BARB poisoning is a major problem, serious toxicity @ only 10X hypnotic dose
- Resp dep, circulatory collapse, renal failure and pulmonary complications = life threatening
- Tx: support resp and BP, gastric lavage
How long does it take to dev. tolerance to BARBs?
- W/in few days. (dec CNS response w/chronic exp)
- Cross-tolerance to other general CNS dep.
What is propanolol used for in the tx. of antianxiety?
- Used for disabling stituational anxiety ("stage fright")
- (beta-adrenorec blocker - blocks autonomic effects such as palpitations, sweating, shaking)
Buspirone is a partial agonist for SER (5HT1A) rec. What are the benefits and limitations of its use in tx anxiety?
- Benefits: produces only anxiolytic effects
- no CNS dep, no physical dep, no rebound anxiety or withdrawl, no additive dep w/ethanol
- Limitation: onset of action = 1-3 wks
What type of patient is Chloral hydrate commonly used for?
- Sedative for PEDIATRIC pts (painless dental tx)
- *Extra: Low TI, used in combo w/N20 or promethazine), met. in liver, higher dose = sig cardiac and resp side effects, additive CNS dep w/ethanol
What are ex. of mild & severe withdrawl symptoms of BZ and BARBS?
- Mild BZ: anxiety, insomnia, irritability, bad dreams, tremors, anorexia
- Mild BARB: anxiety, insomnia, dizziness, nausea
- Severe BZ: agitation, dep, panic, paranoia, muscle twitches, convulsions
- Severe BARB: vomiting, hyperthermia, tremors, delirium, convulsions, death
BARBs half-life and use
- Phenobarbital (L -oral) -anticonvulsant
- Pentobarbital (I-S -iv) -preop sedation
- Thiopental (Ultra S=immediat, -iv) -anesthsia induction
Therapeutic uses of BZs
- Sedative-Hypnotic: Tx insomnia
- Anxiolytic: Anxiety, (panic, OCD, phobias)
- Muscle Relaxant: Spasticity, dystonias
- Anticonvulsant: absence, status epilepticus, gen. seizures
- Other: pre-op med & endoscopic procedures, withdrawal from chronic use of alcohol and CNS dep