Pharm - Sedatives & Alcohol Flashcards

1
Q

What are examples of the Benzodiazepines?

A

MIDAZOLAM
ALPRAZOLAM (Xanax ®)
TRIAZOLAM (Halcion®)
DIAZEPAM (Valium®)
FLURAZEPAM
NITRAZEPAM
LORAZEPAM
FLUNITRAZEPAM (Rohypnol® Date rape drug)
OXAZEPAM
CHLORDIAZEPOXIDE

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1
Q

What is the Mechanism of Action for Benzodiazepines ?

A

Bind to a receptor site on the GABA channel; different from the GABA binding site. This increases the binding of GABA resulting in increased frequency of channel opening.

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2
Q

What are examples of Non - Benzodiazepine ?

A

ZOLPIDEM
ZALEPLON

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3
Q

What are the clinical applications of Benzodiazepines ?

A
  • Acute Anxiolytic
  • Hypnotic
  • Muscle Relaxation
  • Anticonvolustants
  • Alcohol Withdrawal
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4
Q

Which Benzodiazepines are excreted by Glucorodination?

A

Lorazepam
Temazepam

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5
Q

By what process are all other Benzodiazepines eliminated ?

A

Oxidation by CYP450/ CYP3A4/2C19

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6
Q

True or False? Phase I metabolites are usually active.

A

TRUE!!

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7
Q

What is an examples of a Long acting BZD?

A

Diazepam

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8
Q

What is an example of a short acting BZD?

A

Midazolam, Triazolam

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9
Q

What is an example of an Intermediate acting BZD?

A

Alprazolam

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10
Q

What type of BZD is preferred as a sedative?

A

Short- acting preferred

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11
Q

What type of BZD is preferred as a Hypnotic?

A

Long-acting preferred for maintaining sleep,
short-acting for inducing sleep

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12
Q

Which BZD’s are Only useful for Hypnosis?

A

Zolpidem & Zaleplon

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13
Q

What is the Antagonist used for Benzodiazepines?

A

FLUMAZENIL

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14
Q

Which drug is a competitive antagonist of Orexin (OX)) 1& 2 receptors - shutting down the release of Histamine ?

A

Suvorexant

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15
Q

Which drugs is a Melatonin 1& 2 receptor against- reducing neuronal firing to the Suprachiasmatic nucleus ?

A

Ramelteon

16
Q

Which drug is an Unclear- partial agonist of 5HT1A receptors and can be used to treat general anxiety?

A

Buspirone

17
Q

What is the main inhibitory neurotransmitter in the Ventrolateral Preoptic Nucleus ( VLPO)?

A

GABA

18
Q

What can be used in the treatment of Methanol , Ethylene glycol and Diethylene glycol poisoning?

A

Ethanol

19
Q

What type of Alcohols are used as antifreeze formations in automobile radiators, solvent for pharmaceuticals, cosmetics?

A

Ethylene glycol(EG)
Diethylene glycol(DEG)

20
Q

True or False? Methanol is used for embalming fluid, common industrial solvent: paint, paint remover.

A

TRUE!!

21
Q

Fill in the blanks. “ Ethanol is metabolised by ___________.”

A

Enzymes in the liver & intestines.

22
Q

What is the Average rate of elimination for Ethanol?

A

100mg/kg per hr (10-15 ml/hr)

23
Q

What are some of the CNS effects of Ethanol?

A
  • Inhibition of Glutamate NMDA channel activity.
  • Inhibits Glutamate AMPA channel activity.
  • Increase beta-endorphin release.
  • Inhibition of adenosine transport.
  • Increases
    GABA-A channel activity
24
Q

Which enzyme is blocked by the drug Disulfiram ?

A

Acetyaldehyde dehydrogenase.

25
Q

Which drug is a Beta-endorphin antagonist found to inhibit the desire to drink EtOH?

A

Naltrexone

26
Q

Which drug is an Alcohol dehydrogenase inhibitor?

A

Fomepizole

27
Q

Alcohol consumption with drug causes Acetaldehyde accumulation ?

A

Metronidizale

28
Q

Alcohol consumption with drug potentiates GI bleeds?

A

Aspirin

29
Q

Which drugs while consuming alcohol can cause of Synergism of CNS depression?

A

Sedative- Hypnotics & Anti-histamines

30
Q
A