Pharm - Sedatives & Alcohol Flashcards
What are examples of the Benzodiazepines?
MIDAZOLAM
ALPRAZOLAM (Xanax ®)
TRIAZOLAM (Halcion®)
DIAZEPAM (Valium®)
FLURAZEPAM
NITRAZEPAM
LORAZEPAM
FLUNITRAZEPAM (Rohypnol® Date rape drug)
OXAZEPAM
CHLORDIAZEPOXIDE
What is the Mechanism of Action for Benzodiazepines ?
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.
What are examples of Non - Benzodiazepine ?
ZOLPIDEM
ZALEPLON
What are the clinical applications of Benzodiazepines ?
- Acute Anxiolytic
- Hypnotic
- Muscle Relaxation
- Anticonvolustants
- Alcohol Withdrawal
Which Benzodiazepines are excreted by Glucorodination?
Lorazepam
Temazepam
By what process are all other Benzodiazepines eliminated ?
Oxidation by CYP450/ CYP3A4/2C19
True or False? Phase I metabolites are usually active.
TRUE!!
What is an examples of a Long acting BZD?
Diazepam
What is an example of a short acting BZD?
Midazolam, Triazolam
What is an example of an Intermediate acting BZD?
Alprazolam
What type of BZD is preferred as a sedative?
Short- acting preferred
What type of BZD is preferred as a Hypnotic?
Long-acting preferred for maintaining sleep,
short-acting for inducing sleep
Which BZD’s are Only useful for Hypnosis?
Zolpidem & Zaleplon
What is the Antagonist used for Benzodiazepines?
FLUMAZENIL
Which drug is a competitive antagonist of Orexin (OX)) 1& 2 receptors - shutting down the release of Histamine ?
Suvorexant
Which drugs is a Melatonin 1& 2 receptor against- reducing neuronal firing to the Suprachiasmatic nucleus ?
Ramelteon
Which drug is an Unclear- partial agonist of 5HT1A receptors and can be used to treat general anxiety?
Buspirone
What is the main inhibitory neurotransmitter in the Ventrolateral Preoptic Nucleus ( VLPO)?
GABA
What can be used in the treatment of Methanol , Ethylene glycol and Diethylene glycol poisoning?
Ethanol
What type of Alcohols are used as antifreeze formations in automobile radiators, solvent for pharmaceuticals, cosmetics?
Ethylene glycol(EG)
Diethylene glycol(DEG)
True or False? Methanol is used for embalming fluid, common industrial solvent: paint, paint remover.
TRUE!!
Fill in the blanks. “ Ethanol is metabolised by ___________.”
Enzymes in the liver & intestines.
What is the Average rate of elimination for Ethanol?
100mg/kg per hr (10-15 ml/hr)
What are some of the CNS effects of Ethanol?
- Inhibition of Glutamate NMDA channel activity.
- Inhibits Glutamate AMPA channel activity.
- Increase beta-endorphin release.
- Inhibition of adenosine transport.
- Increases
GABA-A channel activity
Which enzyme is blocked by the drug Disulfiram ?
Acetyaldehyde dehydrogenase.
Which drug is a Beta-endorphin antagonist found to inhibit the desire to drink EtOH?
Naltrexone
Which drug is an Alcohol dehydrogenase inhibitor?
Fomepizole
Alcohol consumption with drug causes Acetaldehyde accumulation ?
Metronidizale
Alcohol consumption with drug potentiates GI bleeds?
Aspirin
Which drugs while consuming alcohol can cause of Synergism of CNS depression?
Sedative- Hypnotics & Anti-histamines
