Pharm Block 3- Anxiolytic And Hypnotic Drugs

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anxiety

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-generalized persistent anxiety for at least 1 month's time
-tachycardia and palpitations
-complications with alcohol abuse, sedatives, anti-anxiety meds common

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sleep stages

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-more deep sleep (3 and 4) early in night
-longer REM late in night

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neurochemistry of sleep

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-slow-wave sleep= serotonin
-REM sleep= NE

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benzodiazepine and barbiturate action sites

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-different receptors on GABA receptor (Cl- ion channel complex)

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GABA-A receptor

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-associated with Cl- ion channel
-GABA binding increases Cl- conductance --> hyperpolarizatoin
-high concnetration in striatum, hippocampus, spinal cord

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benzodiazepine receptor

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-enhances action of GABA
-increases frequency of GABA-induced Cl- channel openings
-Flumazenil=pure antagonist

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barbiturate receptor

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-enhances action of GABA
-increases duration of Cl- ch being opening

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drug types used to treat anxiety

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-SSRIs
-benzodiazepines
-antihistamines
-alcohol
-barbiturates
-buspirone

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benzodiazepines used primarly as hypnotics

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-flurazepam, triazolam, and lorazepam

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benzodiazepines used for hypnosis pharmacokinetics

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-flurazepam, triazolam, and lorazepam
-lipophilicity determines rate of entry into CNS
-metab=complex and forms active metabolites (x lorazepam and oxazepam)

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most rapidly absorbed benzodiazepine

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-diazepam

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benzodiazepines that do not form active metabolites

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-lorazepam
-oxazepam
(glucuronidation occurs)

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what benzodiazepine is used for muscle relaxation?

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diazepam

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benzodiazepine drug interactions

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-produce additive CNS depression with most other depressant drugs
-CYP2C9, CYP3A4

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what benzodiazepines are used for panic disorder?

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-alprazolam (xanax)
-clonazepam
-SSRIs

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what benzodiazepines are used for seizure treatment

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-IV diazepam or lorazepam

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which benzodiazepines are used for IV sedation/anesthesia

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-diazpema and midazolam

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how do you treat abuse of benzodiazepines

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-gradual dose reduction
-switch to longer acting drug like chlordiazepoxide
(also used in alcohol withdrawal)

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which benzodiazepine do you use for acute manic episodes?

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-clonazepam

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buspirone mech

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-not a benzodiazepine
-partial agonist at 5HT1A
-also binds dopamine-D2 receptors

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buspirone effects

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-short t1/2
-less sedating than benzodiazepines
-no cross-tolerance/ potentiation
-therapeutic effect may take 1-2 weeks to appear

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other anxiety treatments

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-SSRIs: panic attacks and generalized anxiety disorder
-b-blocker: performance anxiety

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drugs to treat insomnia

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-benzodiazepines
-zoplidem, zaleplon, eczopiclone

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benzodiazepine effects on sleep

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-decreased latency to sleep
-inc in stage 1 and 2, dec in stage 3, 4, REM
-rebound insomnia upon withdrawal

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benzodiazepines as sleep aids s/e

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-daytime sedation
-ataxia
-rebound insomnia
-tolerance and dependence
-occassional idiosyncratic excitemetn and stimulation

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zolpidem mech

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-binds omega-1 BDZ receptor
-antagonized by flumazenil
-relative lack of muscle relaxant or anxiolytic effects

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zaleplon

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-works like zoplidem
-benzodiazepine receptor binding

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eszopiclone

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-non-benzodiazepine hypnotic agent
-approved for longterm use

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ramelteon

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-melatonin MT1 and 2 receptor-agonist
-specifically for insomnia with difficulty falling asleep
-not a controlled substance
-used in jet lag

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barbiturates metab and pharmacokinetics

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-weak acids
-highly lipid soluble
-can induce their own metab and that of other drugs
-renal excretion

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barbiturates s/e

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-CNS depression
-anticonvulsant
-resp depression
-acute intermittent porphyria
-tolerance
-physical dependence-- life-threatening seizures
-acute poisoning
-additive with other depressants

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barbiturate uses

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-hypnotic: rarely; pentobarbital
-anticonvulsant: phenobarbital
-induction of anesthesia: thiopental

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chloral hydrate

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-aldehyde hydrate with pungent taste
-sedative hypnotic
-metab to trichloroethanol=active form
-pharm like barbiturates
-less effects on stages of sleep

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spasticity

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-increases in tonic stretch reflexes and flexor muscle spasms
-possibly with muscle weakness
-underlying mech's are in both streth reflex arc itself and higher centers in the brain

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diazepam

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-reduces muscle spasticity via spinal cord
-produces sedation as well

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baclofen

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-treat muscle spasticity
-GABA-mimetic that works at GABA-b receptors
-hyperpolarization--> presynaptic inhibition --> dec excitatory glutamate release
-much less sedation

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tizanidine mech

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-a2 agonist related to clonidine
-may enhance both pre and postsynaptic inhibition
-relieves muscle spasm

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tizanidine s/e

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-drowsiness
-hypoTN
-dry mouth
-astenia (fatigue)

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dantrolene

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-reduces skel muscle contraction by interfering with excitation-contraction coupling
-used for malignany HTN