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MedChem 2 Hypnotics
Terms in this set (92)
Hypnotics are historically called what?
Sedative Hypnotics and referred to as sleeping pills
ALL HYPNOTICS have _____ and _____ properties
sedative and anxiolytic
Drugs that slow activity in the CNS?
Drugs used to relax, calm, or tranquilize?
Drugs used to induce sleep?
What dose of hypnotics can be prescribed for day-time use to reduce anxiety?
What dose of hypnotics are used for sleeping pills (hypnotics)?
Ideal Hypnotic Drug: The transient ______ in the level of consciousness for the purpose of sleep without lingering effects
Ideal Hypnotic Drug: Have no potential for ______ or ______ respirations
Decreasing or arresting
Ideal Hypnotic Drug: Produce no _____, ______, ______, or _____
Neurotransmitters involved in sleep (8)
GH or Prolactin
Intact transmission system absolutely needed for REM sleep
Inactivation of the system causes sleep
May have involvement in wakefulness and REM
1st system shown to have a role in wakefullness and initiation of REM sleep
Activation causes hypnotic effect
Most important inhibitory transmitter
Linked with sleep as neuro hormones
GH and Prolactin
May have effects on circadian rhythm and sleep processes as neuro hormones
What is used to alleviate jet lag (>5 time zones)?
3 Endogenous peptide sleep substances
______ has a short onset (30 minutes) and 1-2 grams will induce sleep in less than an hour
Suffix __ comes from chloral hydrate
3 Classes of Barbiturates
Absorbed and enters the brain rapidly and also leave the brain rapidly to be metabolized (15 min onset, lasts 2-3 hours)
Onset in about 3 0 minutes duration of 5-6 hours
Take longer to be absorbed and stay longer
Onset about 1 hour and duration of 6-10 hours
3 uses of barbiturates
-Anticonvulsant and anesthetic
Can put someone to sleep and wake up without much grogginess
Can give long acting at low dose to prevent drowsiness
Widely used before the introduction of benzodiazepines
All four hydrogens of barbituric acid are _____
SAR: BOTH hydrgens at positions ___ must be replaced
SAR: If one H is present what happens?
The compound can tautomerize at physiological pH and CANNOT cross the BBB
SAR: _______ substitution at #5 (increased length) will lead to increase in onset and decrease duration
SAR: Branching of the alkyl chain will ______ the activity and _____ the duration
(A branched alkyl chain will be more lipophilic-faster to brain, faster to liver, faster to be metabolized)
SAR: Total number of carbons on both chains should be under __
(If the chain has more than 6, depressant effects will decrease and convulsant effects will increase)
SAR: Introduction of ____ groups will abolish activity
SAR: Replacement of 2-oxygen with SULFUR to form thiobarbiturates will -______ lipid solubility and therefore ______ onset and shorten duration
______-________ of one nitrogen leads to increased onset and decreased duration
2 long acting barbiturates
Has ethyl chain and phenyl group
1 intermediate acting barbiturate
Branched alkyl side-chain _______ lipophilicity and ______ the duration (Amobarbital)
2 Short acting barbtiuates
Same number of carbons as Amobarbital but is metabolized much faster and shorter duration
Substituents in the 5-position which are easily metabolized, alkyl substitution metabolized rapidly
TAKE HOME) Inverse relationship between lipophilicity and duration of action
What are some problems with barbiturates?
What was the first synthesized anti-malaria drug?
_____ at low doses have sedative effects
What does EOH do to BZDs
MOA of BZDs
Bind to specific site on the ionophoric GABAa receptor
BZDs ______ total sleep and _____ nocturnal wakefullness, number of awakenings, sleep latency and NREM sleep
_____ is absorbed the most rapidly of BDZs
How is Flurazepam metabolized?
N-dealkylation and hydroxylation alpha to the imine
What position is Flurazepam metabolized?
_____ has a 41 hours half-life and is metabolized by Oxidative loss of sulfur to oxygen to an active metabolite
_____ has NO active metabolite
How is Temazepam metabolized?
3 second gen BZDs
_____ more rapid elimination with short half-life 8-28 hours
How is Estazolam metabolized?
_____ has a ultra short half-life with a metabolism to an inactive metabolite?
How is triazolam metabolized?
Hydroxylation triazole methyl followed by conjugation
What is similar to BDZs but has reduced ability to cause physical dependence (have withdrawal syndrome)
GABAa, receptor BZ-1
Does Zolpidem induce sleep?
How is Zolpidem metabolized?
Inactive metabolites via hydroxylation of aryl methyl groups
What CYP is responsible from Zolpidem metabolism?
______ is a soft drug, which is a drug designed to be metabolized quickly
______ is a Imidazopyridine
______ is also structurally similar to BDZs and interacts with BZ-1 site and is pharmacologically and pharmacokinetically similar to Zolpidem
Are Zaleplon metabolites active?
No; ALL metabolites are inactive
________ is a Pyrazolopyrimidine
_____ is a GABAa agonist that binds to both BZ-1 and BZ-2 with no selectivity
_______ is a Pyrrolopyrazine
How many melatonin receptors are there?
MT1,2, and 3
What receptors have been cloned?
1 and 2
What type of receptors are Melatonin receptors?
Melatonin receptor agonist
What CYP's are responsible from Ramelteon metabolism
1A2 and 3A4
MT1 and MT2 receptor agonist in the suprachiasmatic nucleus (similar to ramelteon)
What does Tasimelteon do to liver enzymes?
Use of Tasimelteon
Sleep-wake disorder in blind ppl
What regulates sleep-wake cycle
Orexin A and B aka?
Hypocretin 1 and 2
______ are neuropeptides produced in the lateral hypothalamus that promote many aspects of arousal through the OX1 and OX2 receptors
Suvorexant is not recommended for who?
Liver impaired and Strong inhibitors of 3A4
Not recommended in Pg
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