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pharm 586 exam 1 > Antianxiety Agents, Muscle Relaxants, Sedative Hypnotics & Alcohol > Flashcards

Antianxiety Agents, Muscle Relaxants, Sedative Hypnotics & Alcohol Flashcards

0
Q

Chlordiazepoxide (LIBRIUM)

A

Benzodiazepine.
PO, IM, IV
Long acting
Active metabs

Anxiolytic
Anticonvulsant
Withdrawal suppressant

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1
Q

Alprazolam (XANAX)

A

P.P.
Intermediate duration
No active metabolites

Anxiolytic

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2
Q

Diazepam (Valium)

A

A benzodiazepine.
PO, IM, IV
LONG ACTING
active metabs

Anxiolytic 
Anticonvulsant 
Anesthesia supplement
Withdrawal suppressant
Muscle relaxant
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3
Q

Lorazepam (Ativan)

A

A benzodiazepine.
PO, IM, IV
intermediate acting
No active metabs

Hypnotic
Anxiolytic
Anesthesia supplement
Withdrawal suppressant

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4
Q

Midazolam (Versed)

A

A benzodiazepine.
IV
SHORT ACTING
No active metab

Induction or supplement to anesthesia

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5
Q

Termazepam (Restoril)

A

A benzodiazepine.
PO
Intermediate acting
No active metab

Hypnotic

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6
Q

Triazolam (Halicon)

A

A Benzodiazepine.
PO
Short acting
No active metab

Hypnotic

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7
Q

Flumazenil (romazicon)

A

A benzodiazepine antagonist.
Use: reverses the CNS depressant effects of benzodiazepines particularly those use for surgical anesthesia such as Midazolam; Also used to tx benzo poisoning.

SE:
Can trigger seizures esp in epileptic patients or those currently dependent on benzos, barbs, or ETOH.
Can cause sxs of withdrawal in it and addicts.

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8
Q

Butalbital (florinal)

A

A barbiturate.
Intermediate/ short acting

Used mainly as sedative-hypnotics.

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9
Q

Pentobarbital ( Nembutal)

A

A barbiturate.
Intermediate/ short acting

Used mainly as sedative-hypnotics.

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10
Q

Phenobarbital

A

A barbiturate
Long-acting

Used mainly as anticonvulsants.

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11
Q

Thiopental (Pentothal)

A

A barbiturate.

Ultra short acting.

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12
Q

Balcofen (Lioresal)

A

Centrally acting muscle relaxant.
Analog of GABA that acts at GABA-B receptors –> acts in spinal cord to inhibit the release of excitatory transmitters & thus inhibits spasmogenic reflexes.

Use: tx spasticity from MS, spinal cord injuries, etc.

SE: CNS depression, before you, hallucinations, tremors, and seizures. Some degree of dependents me results from chronic use.

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13
Q

Cyclobenzaprine (Flexaril)

A

Centrally acting muscle relaxants.
Tx muscle spasms of local origin (sprains, strains)

SE: CNS depressing effects.

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14
Q

Diazepam (Valium)

A

A centrally acting muscle relaxant.
MOA: act at the levels of the brain stem and spinal cord where they modify the reflex arcs that modulate skull to muscle contraction.

Tx spasticity & acute muscle spasm.

Enhances presynaptic inhibition by facilitating the actions of GABA in the spinal cord.

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15
Q

Metaxalone (Skelaxin)

A

A centrally acting muscle relaxant.

16
Q

Tizanidine (Zanaflex)

A

A centrally acting muscle relaxant.
Alpha 2 agonist.

SE: hypotension, sedation

17
Q

Alcohol

A

Anxiolytic and sedative – hypnotic agent.
Over 90% of consumed alcohol is oxidized in the liver; the rest is excreted through the lungs and kidneys. Alcohol oxidation follows zero order kinetics – a constant amount is oxidized at a constant rate. A typical adult metabolizes 7-10 g of alcohol per hour (one drink).
Alcohol dehydrogenase pathway
ETOH–>acetaldehyde (toxic)

MEOS
ETOH–>acetaldehyde

Acetaldehyde metab
Acetaldehyde –>acetate–>H2O+ CO2
(Aldehyde dehydrogenase)

Graded depression of CNS
Release of inhibitions–> Anxiolytic effect–> sedation–> hypnosis–>anesthesia–> resp depression–> coma–> death

ETOH has a very steep dose response curve.

Depresses respiration and may cause respiratory arrest. And goal is to prevent or treat severe respiratory depression.

Effects on sleep:
Reduces sleep latency. Reduces the time spent in REM sleep and decreases the overall quality of sleep.

Overdosed treated w/ benzodiazepines

More content in notes.

18
Q

Buspirone (Buspar)

A

An anxiolytic and sedative hypnotic agent.
Alleviates mild to moderate anxiety with minimal sedative – hypnotic, muscle relaxant, or respiratory depressant effects. takes one to two weeks to work.

Does not act through GABA mechanisms. May be a partial agonist at serotonin receptors.

Has very low abuse potential. Does not exhibit cross tolerance or cross dependence with the benzo’s, barbiturates, or alcohol. it’s cannot suppress the symptoms of alcohol withdrawal.

The drug of choice for the treatment of anxiety in patients with a history of alcohol or sedative abuse who have been brought through the acute withdrawal face.

19
Q

Eszopiclone (Lunesta)

A 
Long acting (6-8hrs)
Helps to sleep

SEs: CNS depression, complex behaviors while unconscious (sleep driving, sleep eating, etc).

Less suppression of REM sleep & to produce less rebound insomnia (when discontinued) than benzos.

Non-benzo.
Enhances effects of GABA at the benzo receptor – Cl channel complex by interacting with the subtype of the benzo receptor.

Use: Anxiolytic and sedative – hypnotic agent.

Metab by liver- potential for drug interactions.

Drug interactions w/ other CNS depressants.

20
Q

Gammahydroxybutyrate (GHB)

A

Anxiolytic and sedative – hypnotic agent.

Analog of GABA that can cross the BBB.
Use:
1. Ergogenic effect- abused by athletes
2. Date rape drug

High dose use can cause seizures & CNS depression –> coma & death

Chronic use can inducd. State of dependence

21
Q

Melatonin

A

Anxiolytic and sedative – hypnotic agent.

Hormone produced by the pineal gland. Agonist at melatonin receptors.

22
Q

Ramelton (Rozerem)

A

Anxiolytic and sedative-hypnotic agent.

Used w/ caution in Pts w/ impaired lived function.

23
Q

Zolpidem (Ambien)

A 
Long acting (6-8hrs)
Helps to sleep

SEs: CNS depression, complex behaviors while unconscious (sleep driving, sleep eating, etc).

Less suppression of REM sleep & to produce less rebound insomnia (when discontinued) than benzos.

Non-benzo.
Enhances effects of GABA at the benzo receptor – Cl channel complex by interacting with the subtype of the benzo receptor.

Use: Anxiolytic and sedative – hypnotic agent.

Metab by liver- potential for drug interactions.

Drug interactions w/ other CNS depressants.

24
Q

Zaleplon (Sonata)

A

Short acting (2-4 hrs)

SEs: CNS depression, complex behaviors while unconscious (sleep driving, sleep eating, etc).

Less suppression of REM sleep & to produce less rebound insomnia (when discontinued) than benzos.

Non-benzo.
Enhances effects of GABA at the benzo receptor – Cl channel complex by interacting with the subtype of the benzo receptor.

Use: Anxiolytic and sedative – hypnotic agent.

Metab by liver- potential for drug interactions.

Drug interactions w/ other CNS depression.

25
Q

Disulfiram (Antibuse)

A

Treatment of alcoholism.

Inhibitor of aldehyde dehydrogenase. It blocks the conversion of acetyl aldehyde to acetate.

If the patient consumes alcohol they have a severe reaction consisting of flashing, headache, nausea, and confusion. Very unpleasant.

Potentially hepatotoxic.

26
Q

Acamprosate (Campral)

A

Treatment of alcoholism.

27
Q

Naltrexone (ReVIA)

A

Treatment of alcoholism.

28
Q

Benzodiazepines

A

A Benzodiazepine.

A Benzodiazepine.

  1. Anxiolytic
  2. Sedative hypnotic
  3. Anticonvulsant
  4. Muscle relaxation
  5. CNS depressant–> sedation, sleep, surgical anesthesia, resp depression, cardiovascular collapse
    Benzodiazepines have a shallow dose response curve (much less likely to cause fatalities)
  6. TX OF ALCOHOL WITHDRAWAL
  7. Preanesthetic med/ supplement
  8. Induction of anesthesia (Midazolam, Versed)

Effects on sleep–> decreased sleep latency, decrease in duration of REM sleep. May cause REM rebound.

MOA: enhance inhibitory effects of GABA; GABA & GABA-a receptors must be present–> interacts at benzo receptor –> Cl- channel opens & hyper polarizes the membrane –> decreases neuronal firing.
SEs:
1. sedation, drowsiness, lightheadedness
2. Mental clouding, confusion, psychomotor impairment, slurred speech, ataxia
3. Memory impairment-anterograde amnesia
4. Disinhibition of suppressed behaviors
5. Euphoria
6. Hangover
7. Rebound anxiety
8. Resp depression
9. Tolerance
10. Dependence –> withdrawal
11. Possible teratogenicity - don’t use when pregnant.

Major drug interactions:

  1. Additive effects w/ ETOH & other CNS depressants
  2. Cimetidine (Tagamet), disulfiram (Antabuse), & isoniazide can prolong benzo action
  3. Cross tolerance & cross dependence w/ ETOH & barbiturates.
  4. Can inc levels of Digoxin & phenytoin
29
Q

Short acting benzos

A

Triazolam

Better for Pts who have trouble falling to sleep.

May cause rebound anxiety

30
Q

Long acting Benzos

A

Flurazepam

Better for Pts who have trouble staying asleep.

May cause hangover effect.

31
Q

Barbiturates

A

MOA: facilitate the actions of GABA at the GABA – a receptor chloride channel complex. They interact with the site that is different from the GABA or the benzodiazepine binding site. Unlike benzos, barbiturates can cause opening of the chloride channels without GABA. This may be why Barbiturates can produce surgical anesthesia and great CNS depression that occurs in overdose.
Used as:
1. sedative-hypnotics - almost obsolete
2. anxiolytics,
3. anticonvulsants.
4. General anesthetic- Can readily induce a state of surgical anesthesia –> thiopental.
5. Depress respiration - can be fatal
6. Euphoria -abuse potential
Recently replaced by benzodiazepines which have a better margin of safety.
7. Induction of, following head injuries.
Barbs are lipid soluble –> can easily cross blood brain barrier. The more lipid soluble compounds have a rapid onset and a short duration of action.
8. As adjuncts for the Tx of tension HA

Barbs are metab by impaired liver function –> induce microsomal enzymes –> Potential drug interactions.

SEs:

  1. Sedation, drowsiness, lethargy, confusion, ataxia.
  2. Hangover effect
  3. Respiratory depression at high doses
  4. Disinhibition of suppressed behavior
  5. Nausea and G.I. upset
  6. Allergic reactions particularly of the skin
  7. Aggravation of acute intermittent porphyria, due to infection of hepatic enzymes involved in porphyrin synthesis.

Additive effects of the CNS depressants (alcohol, opioids, antihistamines).
MAO inhibitors enhance CNS depression.
Anticoagulants – word from FX can be greatly reduced by phenobarbital.

ADDICTIVE- reduce physical and psychological dependence. Produce from a coconut it and pharmacodynamic tolerance. Can lead to withdrawal –> life threatening!

32
Q

Withdrawal Syndrome

A

A. Insomnia, anxiety, restlessness, irritability, tremors, EEG changes, nausea, vomiting.
B. Grand mal seizures
C. Delirium, hallucinations

Life-threatening emergency!!!!!

Tx: symptomatic support and benzodiazepines to control seizures.

Barbiturates, ETOH, Benzodiazepines

33
Q

Barbiturate Poisoning

A

Severe CNS depression – coma and depressed respiration.
Hypotension, shock, circulatory collapse.
- Treatment is mainly symptomatic – ventilation, hydration, etc.
There is no specific antidote

34
Q

Hydroxyzine

Promethazine

Diphenhydramine

A

Antihistamines used as mild sedatives.

Hydroxyzine- also had Anxiolytic activity. Limited abyss potential.

Diphenhydramine- OTC sleep aid.

Promethazine- mild sedative

35
Q

Beta blockers

A

Ex- propranolol

Anxiolytic activity

Useful in patients with pronounced on an Autonomic sxs such as tachycardia and HTN. Use for tx of some types of situational anxiety- example stage fright

36
Q

Severe alcohol withdrawal syndrome:

A

Anxiety, fear, hallucinations, delirium, tremors (delirium tremens), grand mal seizures, hypertension, tachycardia, arrhythmias.

Can be life-threatening

Tx with benzodiazepines – lorazepam and oxazepam maybe preferred in patients with impaired Liver function.

Phenytoin can be used to control seizures.

Clonidine may reduce tachycardia and hypertension.

Naltrexone may reduce craving for alcohol.

Disulfiram(Antabuse)

Acamprosate decreases craving for alcohol – may help maintain abstinence. Less hepatotoxicity

pharm 586 exam 1 (1 decks)

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