BZD Flashcards
Short acting bzd for favorable asa hypnotic than sedative drug
Triazolam
Use for anxiety and more toxic in overdose than other bzd
Alprazolam
Drugs for epilepticus
Lorazepam
Diazepam
Bzd drug for seizures
Clonazepam
⚬ muscular disorders,old first-line tmt for status epilepticus
Diazepam
Aka nordiazepam
Desmethydiazepam
• ↓REM sleep
Zolpidem
Newer gen of sedative and hypnotic drug with a Short half life and ↓latency of sleep onset
Zaleplon
a hypnotic drug which ↑sleep time, stage 2 NREM sleep
ESZOPICLONE
non-24hour sleep-wake disorder
Tasimelteon
Concurrent use with fluvoxamine increases the peak plasma conc of ramelteon over 50-fold
RAMELTEON
relieves anxiety without causing marked sedative, hypnotic, or euphoric effects
BUSPIRONE
Medical term of pins and needes
Paresthesias
Bzd drug for amnesia with a duration of action of 3-8hrs
Midazolam
Intermediate acting Bzd drug for insomia
Temazepam
Long acting bzd which administered indecreasing doses to px with withdrawal
Chlordiazepoxide
Date rape drug
Flunitrazepam
Knock out drops
Mickey finn
active metabolite of chlordiazepoxide, diazepam, prazepam, and clorazepate
Desmethyldiazepam
structurally unrelated to benzodiazepines, share a similar mechanism of action
ZOLPIDEM
slow-onset anxiolytic agent
BUSPIRONE
may take 3-4weeks to develop anxiolytic effects
Not for acute anxiety
BUSPIRONE
2 bzd blokers
Flumazenil,
B-carbolines
Has a a/e of paradoxical reactions
Bzd blokers ( flumazenil, B-carbolines)
In the tmt of GAD and phobias
Bzd
increase in the frequency of channel-opening events
Benzodiazepines
do not substitute for GABA but appear to enhance GABA’s effects allosterically without directly activating GABA-A receptors
Benzodiazepines
negative allosteric modulators of GABA-receptor function
INVERSE AGONISTS
OREXIN RECEPTOR ANTAGONISTS FDA-approved:
Suvorexant
line tmt for febrile seizure
Phenobarbital
INTERMEDIATE-ACTING
• Amobarbital • Butabarbital
Barbiturates for anesthetic
Thiopental
increase the duration of the GABA-gated chloride channel openings
Barbiturates
AMPA
α-amino-3-hydroxy-5- methylisoxazole-4- propionic acid
ULTRA SHORT-ACTING
• Thiopental
• Thioamylal
• Methohexital
LONG-ACTING DOA
4-5 days
As a component if balanced anesthesia (IV)
Thiopental
For sedation and amnesia before and during medical and surgical procedures
Thiopental
Midazolam
Triazolam
For sedation and amnesia before and during medical and surgical procedures
Thiopental
Triazoalam
Midazolam
INTERMEDIATE-ACTING barbiturates
• Amobarbital • Butabarbital
tonic-clonic seizure
• Phenobarbital
OREXIN RECEPTOR ANTAGONISTS Use for mgt insomia and slepig disorders
Almorexant & Suvorexant
Notable barbiturates available in the market
Phenobarbital
also depress the actions of glutamic acid via binding to the AMPA receptor
Barbiturates
Previously known as grand mal seizure
tonic-clonic seizure
T/F drugs must either be highly hydrophobic or engage specific transport mechanisms
True
respond to changes in the membrane potential of the cell
VOLTAGE-GATED CHANNELS
responsible for fast synaptic transmission typical of hierarchical pathways in the CNS (ms)
LIGAND-GATED CHANNELS
reduce the amount of transmitter released from the terminals of sensory fibers
Axoaxonic synapses
causes the release of the peptide substance P from sensory neurons
Reserpine
Capsaicin
retrograde signaling
Endocannabinoids
seven-transmembrane G protein-coupled receptors
METABOTROPIC RECEPTORS
highly concentrated on the initial segment of the axon, which initiates the all-or-nothing fast action potential
VOLTAGE-GATED CHANNELS
cAMP, block metabolism, prolong action
methylxanthines
blocks NMDA subtype of glutamate receptors = anesthesia
ketamine
all the pathways directly involved in sensory perception and motor control
HIERARCHICAL SYSTEMS
blocks glycine = convulsant action
strychnine
form the interconnecting pathways that transmit signals over long distances
projection neurons
axons arborize in the immediate vicinity of the cell body
local circuit neurons
neurotransmitters are produced by only a limited number of neurons whose cell bodies are located in small discrete nuclei, often in the brainstem
NONSPECIFIC OR DIFFUSE NEURONAL SYSTEMS
GLUTAMATE receptors
AMPA
kainic acid
N-methyl-D-aspartate
GABA & Glycine receptors
GABA -A and GABA-B
first compound to be identified pharmacologically as a transmitter in the CNS
ACETYLCHOLINE
no orexin
narcolepsy
may affect memory, cognition, and pain perception by this mechanism
Endocannabinoids
hypothesized to be a retrograde messenger
Nitric oxide
inhibit release of both amino acid and monoamine transmitters
Purines
established for vascular smooth muscle
Nitric oxide