Sedative-Hypnotic Drugs Flashcards
Compare Older Sedatives (barbituates) with Newer (benzos)
Older sedative-hypnotics (barbiturates) show a linear dose-response curve [no ceiling]
An increase in dose above that needed for hypnosis may lead to a state of general anesthesia.
At still higher doses they may depress respiratory and vasomotor centers in the medulla, leading to coma and death.
Benzodiazepines show a non-linear dose- response relationship. They are safer drugs. (have a plateu), overdose will not kill you.
Name the BARBITURATES
Phenobarbital
Pentobarbital
Thiopental
name the NON-BENZODIAZEPINE BENZODIAZEPINE-RECEPTOR AGONISTS (NBBRA)
“Z drugs”
Zolpiden
Zaleplon
EsZopiclone
name the only 5-HT1A PARTIAL AGONISTS
Buspirone
name the only MELATONIN RECEPTOR AGONISTS
Ramelteon
name the OLDER SEDATIVE-HYPNOTICS (3)
Meprobamate
Chloral hydrate
Paraldehyde
name the ANTIHISTAMINICS
Hydroxyzine
Diphenhydramine
Doxylamine
name the only α2-AGONISTS in this lecture
Clonidine
bind to GABAa receptors(which functions as a chloride channel, and is activated by the inhibitory neurotransmitter GABA) in neuronal membranes in the CNS.
is the MOA for which class of drugs
Benzos
Do benzos DIRECTLY activate GABAa receptors?
NO!
Benzodiazepines potentiate GABAergic inhibition. Benzodiazepines don’t directly activate GABAA receptors: they enhance GABA’s effects allosterically. This enhancement takes the form of an increase in frequency of channel opening events.
name the benzo ANTAGONIST (1)
flumazenil
list the 3 benzos that fit the following description
are conjugated directly to their glucuronides, mainly in the liver, and are not metabolized by the P450 system. Their plasma levels are not significantly affected in liver disease. Other benzodiazepines may need dose adjustment in liver disease.
“L-O-T”
lorazepam
oxazepam
temazepam
Benzos good for: MUSCULAR DISORDERS
Diazepam is useful in the treatment of skeletal muscle spasms such as occur in muscle strain, and in treating spasticity from degenerative disorders, like multiple sclerosis and cerebral palsy.
Benzos good for SEIZURES
which one is specifically good for status epilepticus.
Clonazepam: used for some types of epileptic seizures.
Lorazepam : drug of choice in status epilepticus.
benzos good for DRUG WITHDRAWAL
“C-C-O-D”
Chlordiazepoxide
clorazepat
oxazepam
diazepam
*useful in the management of withdrawal states in persons physiologically dependent on ethanol.
which benzos are used for ANESTHESIA
diazepam, midazolam
are used as components of anesthesia protocols.
which benzos are commonly used for SLEEP DISORDERS
The three most prescribed for sleep disorders are
- long-acting flurazepam
- intermediate-acting temazepam
- short-acting triazolam
which barbituate is being described:
acts within seconds and has a duration of action of about 30 min is used in the IV induction of anesthesia.
Thiopental
which barbituate is being described
has a duration of action of >1 day is useful in treatment of seizures.
Phenobarbital
Do barbituates induce or inhibit CYP450 enzymes
ENZYME INDUCTION
Barbiturates induce P-450 microsomal enzymes in the liver. Therefore, chronic barbiturate administration diminishes the action of many drugs that are dependent on P- 450 metabolism to reduce their concentration.
Because hepatic glucuronyl transferase and the bilirubin-binding Y protein are increased by the barbiturates, (this barbituate) has been used successfully to treat hyperbilirubinemia and kernicterus in the neonate.
phenobarbital
this class of drugs is absolutely contraindicated if pts have acute intermittent porphyria, variegate porphyria, hereditary coproporphyria or symptomatic porphyria.
BARBITUATES
These drugs act only on the BZ1 subtype of benzodiazepine receptors
THE NON-BENZODIAZEPINE BENZODIAZEPINE- RECEPTOR AGONISTS (NBBRA)
No hypnotic, anticonvulsant or muscle relaxant properties. Only anxiolytic.
Doesn’t interact with GABA receptors.
Indicated for the management of anxiety disorders or the short-term relief of the symptoms of anxiety.
5-HT1A partial agonist.
BUSPIRONE
mainly metabolized by CYP1A2.
should not be concurrently given with fluvoxamine, which inhibits CYP1A2.
Indicated for the treatment of insomnia characterized by difficulty with sleep onset.
Ramelteon
Temazepam, triazolam, and flurazepam are category ______in pregnancy
category X.
Most barbiturates are category_____ in pregnancy
D
Eszopiclone, zaleplon, zolpidem and ramelteon are category__________ in pregnancy
C
Buspirone is category________ in pregnancy
B
B for B!!!
