Flashcards
Sedatives
Flashcards do conjunto (38)
- 1Thalidomideanti-emetic
toxic
immunosuppressant (for cancer and leprosy) - 2—Buspirone
Anxiolytic but not sedative
1 week to establish
partial agonist (5-HT1a receptors)
No rebound/withdrawal effects - 3—(S) Ramelteon
Indane
melatonin receptor agonist
for insomnia (but doesn't maintain sleep)
S-configuration + ether-->affinity for MT1-MT2
orally but rapid metabolism-->short half life (no drug accumulation)
No depression of cognitive function/memory/...
No abuse/withdrawal/tolerance...
- 4—Melatonin
Indole
- 5—MI
- 6—M II
major metabolite of Ramelteon by CYP1A2
active
higher bioavailability but less potent
- 7—M III
- 8—M IV
from M II or M III with CYP3A4
- 9—Doxylamine
ethanolamine
antihistamine
for acute insomnia
CNS hypnotic
OTC
- 10—Diphenhydramine
ethanolamine
antihistamine
for acute insomnia
CNS hypnotic
OTC
- 11—Barbituric acid
no sedative/hypnotic, anxiolytic
no anticonvulant
keto-enol tautomerization
- 12—Pentobarbital
short act (10-15mins)-short DOA (3-4 hr)
sedative/hypnotic - orally
more potent and faster onset than butabarbital
from thiopentobarbital
branched-->increased potency, less DOA
inactive metabolites
- 13—Secobarbital
short acting (3-4 hr)
rapid onset (10-15 mins)
sedative/hypnotic
orally available
- 14—Butethal
- 15—Methohexital
IV anesthetic
lipophilic
ultra-short acting and very short DOAt
- 16—Thiopental
sulfuration at C2
ultra-short acting
immediate onset but shorter DOA than pentobarbital
anesthetic
by injection (as salt)
- 17—Phenobarbital
long-acting
anticonvulsant
slow onset (30-60 mins)
orally available
half life: 80-120 hr
inactive metabolites
- 18—Mephobarbital
long-acting
anticonvulsant
slow onset (30-60 mins)
orally available
half life: 10-70 hr
- 19—Amobarbital
intermediate acting (6-8 hr)
sedative/hypnotic
slow onset (45-60 mins)
orally available
- 20—Butabarbital
intermediate acting (6-8 hr)
sedative/hypnotic
slow onset (45-60 mins)
orally available
- 21—Chloral hydrate
barbiturate-like
acts on GABA-->sedative/hypnotic
synergizes with alcohol-no analgesia
weak acid-->prodrug (no GI disturbance)
from chloral which is metabolized to trichloroacetic acid (cardiotoxic) and trichloroethanol (CNS depressant)
- 22—Chlordiazepoxide
- 23—Midazolam
imidazobenzodiazepine
- 24—Alprazolam
triazolobenzodiazepine
removal of methyl-->estazolam
- 25—Triazolam
triazolobenzodiazepine
from alprazolam
short DOA (4 hours)
onset of action: 1-2 hr after oral
- 26Benzodiazepines promoted as sleep inducersOnset of action after oral 30 mins:
Flurazepam
Quazepam
Estazolam
Onset of action after oral 1-2h:
Triazolam
Temazepam - 27—Flurazepam
half life 2 hr but very long DOA
Metabolites by CYP3A4: N-desalkyl (47-100hr) and N-hydroxyethyl (2-4hr)
-->efficacious for 1-2 nights (residual hypnotic effect)
onset of action: 30 mins after oral
2 active metabolites with higher t1/2
- 28—Quazepam
onset of action: 30 mins after oral
2 active metabolites with long t1/2-->residual hypnotic effects
- 29—2-oxoquazepam
active metabolite of quazepam
slow elimination
residual hypnotic effect
- 30—N-desalkyl-2-oxo-quazepam
active metabolite of quazepam
slow elimination
residual hypnotic effect
- 31—Estazolam
triazolobenzodiazepine
metabolites have short half-lives and more hydrophilic because of triazolo ring that prevents oxidation-->low/no activity
minor metabolite: 4-hydroxyestazolam
major metabolite: 4'-hydroxyestazolam
onset of action: 30 mins after oral
- 32—α-hydroxytriazolam
major urine metabolite of triazolam
short DOA
sleep inducer in elderly
slow onset of action orally (1-2 hr)
- 33—Temazepam
3-OH prevents phase I
Phase II-->conjugated temazepam-->rapid urine excretion
no active metabolite
short half life (0.4-0.6h)
onset of action: 1-2 hr after oral
- 34—Diazepam
gives: temazepam and nordiazepam-->oxazepam (all active)
- 35—Flumazenil
BZD receptor antagonist for treatment of overdose with BZD
low dose to treat BZP dependence
rapid administration may precipitate withdrawal
IV metabolism only-->inactive acid and N-demethylation, short half life (<1 hr)
- 36—Zolpidem
Imidazopyridine
selective GABA agonist at α1 subunit of Cl channel (BZ1 receptor)
highly bound to plasma proteins
lipophilic-->rapid absorption orally-->rapid onset
metabolism in liver-->inactive metabolites (no accumulation, no addiction)
short acting (2h, less than Eszopiclone but more than Zaleplon)
Administration with heavy metals (high fat foods) delay time to peak plasma concentration
Activity reversed by flumanezil
Sedative/hypnotic for pregnant women
- 37—Zaleplon
Pyrazolopyrimidine
selective GABA agonist at α1 subunit of Cl channel (BZ1 receptor)
lipophilic-->rapid absorption orally-->rapid onset (more than Zolpidem)
metabolism in liver-->inactive metabolites (no accumulation, no addiction)
short acting (1h, less than Eszopiclone and Zolpidem)
Administration with heavy metals (high fat foods) delay time to peak plasma concentration
Activity reversed by flumanezil
- 38—Eszopiclone: (S)-Zopiclone
cyclopyrrolone
less selective GABA agonist at α1 subunit of Cl channel (BZ1 receptor): hypnotic and other CNS activities
lipophilic-->rapid absorption orally-->rapid onset
metabolism in liver-->inactive metabolites (no accumulation/addiction)
short acting (3-6h but more than Zaleplon and Zolpidem)
Administration with heavy metals (high fat foods) delay time to peak plasma [ ]
Activity reversed by flumanezil
racemic mixture: next day residual sedation and cognitive effects
Informações
- Descrição
- Pharmacy FlashCards sobre Sedatives, criado por Cyrielle Saba em 03-12-2020.
- Criado por
- Cyrielle Saba
- Visualizações
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- Avaliação