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Anti-Anxiety Agents > Anti-Anxiety Agents > Flashcards

Anti-Anxiety Agents Flashcards

1
Q

Sedatives and Hypnotics

A
  • an effective sedative (anxiolytic) agent should reduce anxiety and exert a calming effect
  • hypnotic (sleep-promoting) effects require more pronounced CNS depression than sedation and can be achieved with many anxiolytic drugs just by increasing the dose
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2
Q

Graded Dose-Dependent CNS Depression

A
  • characteristic of most sedative-hypnotics
  • BRs exhibit linear dose-response relationships and can thus induce anesthesia and coma at higher than hypnotic doses
  • BZs and some of the newer hypnotics (like zolpidem and zaleplon) exhibit flatter non-linear dose-response relationships
  • therefore, BZs safer than BRs
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3
Q
  • benzodiazepine
  • high doses depress the CNS to the point known as stage III general anesthesia
  • intermediate acting
  • sufficiently selective to exert anticonvulsant effects without marked CNS depression
  • clinically useful in the management of seizures
  • used for panic disorder
  • parenteral formulation is used to suppress delirium tremens
A

Lorazepam

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4
Q
  • benzodiazepine
  • sufficiently selective to exert anticonvulsant effects without marked CNS depression
  • clinically useful in the management of seizures
  • used for GAD and social phobia
A

Clonazepam

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5
Q
  • benzodiazepine

- long acting

A

Chlordiazepoxide

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6
Q
  • benzodiazepine

- short acting

A

Oxazepam

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7
Q
  • benzodiazepine

- long acting

A

Clorazepate

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8
Q
  • benzodiazepine
  • long acting
  • prototypical BZ, with most other BZs being structurally related
  • -high doses depress the CNS to the point known as stage III general anesthesia
  • sufficiently selective to exert anticonvulsant effects without marked CNS depression
  • clinically useful in the management of seizures
  • muscle relaxation
  • withdrawal from physiologic dependence on ethanol or other sedative-hypnotics
A

Diazepam

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9
Q
  • benzodiazepine
  • used for GAD, panic disorder, and agoraphobia
  • short acting
A

Alprazolam

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10
Q
  • benzodiazepine
  • has short half-life and used to sedate you and then quickly go away
  • short acting
  • high doses depress the CNS to the point known as stage III general anesthesia
  • sedative and possible amnesic effects during medical or surgical procedures and premedication prior to anesthesia
A

Midazolam

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11
Q
  • newer anxiolytic
  • safe
  • track record is not as long, but has been around for a long time and is looking very good
  • selective anxiolytic effects w/o causing marked sedative, hypnotic, or euphoric effects
  • thought to exert its anxiolytic effects by acting as a partial agonist at brain 5-HT1A receptors, though it also has affinity for brain dopamine D2 receptors
  • does not interact directly with GABAergic systems
  • patients treated with this drug show no rebound anxiety or withdrawal signs on abrupt discontinuance
  • not effective in blocking the acute withdrawal syndrome resulting from abrupt cessation of the use of BZs
  • used in generalized anxiety states, but is less effective in panic disorders
  • unlike the BZs, the anxiolytic effects of this drug may take > 1 week to become established, making the drug unsuitable for acute anxiety states
  • rapidly absorbed after PO admin.
  • t1/2 = 2-4 hrs and liver dysfunction may slow its clearance
  • inhibitors of CYP3A4 can markedly inc. the plasma level
  • causes less psychomotor impairment than BZs and does not affect driving skills
A

Buspirone

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12
Q
  • beta-blocker

- do not reduce anxiety per se, but they do reduce the associated sxs

A

Propranolol

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13
Q
  • beta-blocker

- do not reduce anxiety per se, but they do reduce the associated sxs

A

Atenolol

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14
Q

Pharmacokinetics of BZs (Absorption and Distribution)

A
  • PO absorption rates of the BZs depend on lipophilicity
  • increased lipophilicity leads to increased absorption in blood
  • lipophilicity is major determinant of the rate at which a given BZ enters the CNS
  • the BZs cross the placental barrier during pregnancy and may contribute to the depression of neonatal vital functions when administered pre-delivery
  • also detectable in breast milk and may exert depressant effects in the nursing infant
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15
Q

Pharmacokinetics of BZs (Metabolism)

A
  • metabolic transformation to water-soluble metabolites is critical for clearance from body
  • elimination half-life of the drugs depends mainly on the rate of metabolic transformation
  • most BZs undergo phase I oxidative rxns catalyzed by CYP enzymes
  • resulting metabolites then undergo phase II conjugation reactions to form glucoronides that are excreted in urine
  • fortunately, drugs are metabolized heavily
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16
Q

Metabolites of BZs and desmethyldiazepam (nordiazepam)

A
  • note that many phase I metabolites of BZs are pharmacologically active, some with long half-lives
  • desmethyldiazepam (nordiazepam), which has a half-life of >40 hrs is an active metabolite of chlordiazepoxide, diazepam, and clorazepate
  • therefore, drugs can have accumulative effects, especially in the elderly
17
Q

Half-lives and Peak Concentration of BZs

A
  • most have long half-lives due to long-lasting metabolites
  • only one that has very shor thalf-live (1-7 hrs) is midazolam
  • midazolam has short half-life and used to sedate you and then quickly go away
  • drugs reach peak hours in only a couple hours, so effects come on quick, but then they last long
  • dose sparingly and don’t take them frequently
  • BZs for which parent drug or its active metabolites have long t1/2’s are more likely to cause cumulative effects (e.g. increased drowsiness) with multiple doses
18
Q

Pharmacokinetics of BZs: Factors Affecting Biodisposition

A
  • disease or drug induced increases or decreases in hepatic function
  • age: clearance is generally reduced in elderly
  • long-term exposure to BZs does not alter hepatic drug metabolizing enzyme activity (in contrast to some older sedatives like the barbiturates)
19
Q

Pharmacodynamics of BZs

A
  • bind to the molecular components of the GABAa receptor in neuronal membranes in the CNS
  • this receptor functions as Cl- ion channel
  • GABAa receptor is a heteropentameric glycoprotein assembled from 5 subunits
  • GABA interacts between alpha and beta subunits, triggering Cl- ion channel opening with resulting membrane hyperpolarization
  • BZs potentiate the Cl- ion channel effects of GABA, as well as GABAergic inhibition at all levels of the neuraxis
  • this potentiation take sthe form of an increase in FREQUENCY of GABA-gated channel opening events
20
Q

BZ Organ Level Effects: Sedation

A
  • at low doses, BZs exert calming effects and dec. anxiety
  • anxiolytic actions are accompanied by some depressant effects on psychomotor and cognitive fxns
  • at doses used to manage anxiety, BZs can cause disinhibitory effects like euphoria, impaired judgment, and loss of self-control
  • BZs can also exert dose-dependent anterograde amnestic effects (inability to remember events occurring during the drug’s duration of action)
21
Q

BZ Organ Level Effects: Hypnosis

A

Promotion of Sleep

22
Q

BZ Organ Level Effects: Anesthesia

A
  • high doses of certain BZs (e.g. diazepam, lorazepam, midazolam) depress the CNS to the point known as stage III general anesthesia
  • these BZs are used IV in anesthesia, often in combination with other agents
  • when used as adjuncts to general anesthesia, the BZs can contribute to persistent (although reversible) post-anesthetic respiratory depression
23
Q

BZ Organ Level Effects: Anticonvulsant Effects

A
  • several BZs (clonazepam, lorazepam, and diazepam) are sufficiently selective to exert anticonvulsant effects without marked CNS depression
  • such BZs are clinically useful in the management of seizures
24
Q

BZ Organ Level Effects: Muscle Relaxation

A
  • the BZs (e.g. diazepam) exert inhibitory effects on polysynaptic reflexes and internuncial transmission
  • at high doses, BZs can also depress transmission at the skeletal neuromuscular junction
  • these collective actions lead to muscle relaxation and have proven useful for relaxing contracted voluntary muscle in muscle spasm
25
Q

BZ Organ Level Effects: Respiratory Depression

A
  • at hypnotic doses in health pts, BZs have a comparable effect on respiration to changes that occur during natural sleep
  • however, even at therapeutic doses, these agents can produce significant respiratory depression in pts with pulmonary disease
26
Q

BZ Organ Level Effects: Cardiovascular Depression

A
  • at doses up to those causing hypnosis, no significant effects on the cardiovascular system are observed in healthy people
  • however, normal doses can cause cardiovascular depression in hypovolemic states, heart failure, and other diseases that impair cardiovascular fxn
  • at toxic doses, myocardial contractility and vascular tone may both be depressed leading to circulatory collpase
  • cardiovascular (and respiratory) effects are more pronounced when the BZs are administered IV
27
Q

BZs and Treatment of Anxiety

A
  • anxiety is often secondary to organic disease states (ulcers, acute MI, etc.) or unpleasant situations
  • even though situational anxiety tends to be self-limiting, the short-term use of sedatives may be appropriate for the txt of such anxiety states
  • excessive or unreasonable anxiety about life circumstances (GAD), panic disorders, and agoraphobia are also amenable to drug therapy
  • BZs widely used for the management of acute anxiety states and for rapid control of panic attacks
  • also used (though less commonly) in long-term management of GAD and panic disorders
28
Q

Advantages of BZs in Anxiety Treatment

A
  • rapid onset of action
  • relatively high therapeutic index and availability of flumazenil for treatment of overdose
  • low risk of drug interactions based on liver enzyme induction
  • minimal effects on cardiovascular and autonomic functions
29
Q

Disadvantages of BZs in Anxiety Treatment

A
  • risk of dependence (both physiologically and psychologically)
  • depression of CNS fxns (additive when administered with other drugs, including antihistamines, anticholinergics, and ethanol)
  • amnesic effects
30
Q

Treatment of Anxiety Dosing Considerations

A
  • a dose should be prescribed that does not impair mentation or motor fxns during waking hrs
  • prescriptions should be written for short periods, since there is little justification for long-term therapy
  • b/c the elderly are more sensitive to the effects of BZs, doses 1/2 those used in younger adults are safer and usually effective
  • combinations w/ other anti-anxiety agents, antihistamines, anticholinergies, and ethanol should be avoided
31
Q

BZs: Other Therapeutic Uses

A
  • sedative and possible amnesic effects during medical or surgical procedures and premedication prior to anesthesia (use PO formulations of shorter-acting drugs like midazolam)
  • withdrawal from physiologic dependence on ethanol or other sedative-hypnotics (use longer-acting drugs (e.g. diazepam) administered in progressively decreasing doses)
  • parenteral lorazepam is used to suppress delirium tremens
  • used as central muscle relaxants, though generally with some degree of accompanying sedation
32
Q

BZs: Direct Toxic Actions

A
  • at low doses, BZs can lead to drowsiness, impaired judgment, and diminished motor skills (sometimes with significant impact on driving ability, job performance, and personal relationships)
  • can cause significant dose-related anterograde amnesia and can significantly impair ability to learn new information
  • overuse is a common cause of confusional states in the elderly
  • at high doses, toxicity can present as lethargy or a state of exhaustion or, alternatively, as gross sxs of ethanol intoxication (i.e. behavioral disinhibition)
33
Q

BZs: Tolerance, Psychologic Dependence, and Physiologic Dependence

A
  • can result from extended use of BZs (see sleep note cards)
  • after prolonged use, abrupt cessation can precipitate withdrawal sxs (characterized by states of increased anxiety, insomnia, and CNS excitability that my progress to convulsions)
  • BZs with short half-lives cause more severe withdrawal signs than those with longer half-lives, which are eliminated slowly and achieve gradual withdrawal
  • doses should be tapered slowly to avoid withdrawal sxs
34
Q

BZs: Overdoses

A
  • sedative-hypnotics are the drugs most frequently involved in deliberate overdoses
  • BZs are considered to be safer in this respect, since they have flatter dose-response curves
  • even following ingestion of very high doses, the outcome is rarely fatal if discovery is made early and a conservative txt regimen is started
  • with severe toxicity, respiratory depression can be complicated by aspiration of gastric contents (an even more likely occurrence if ethanol is present)
  • txt consists of ensuring a patent airway (with a ventilator if necessary) and maintenance of plasma volume, renal output, and cardiac fxn
35
Q
  • synthetic BZ derivative that binds to the BZ site on the GABAa receptor
  • antagonizes the actions of the BZs and the newer hypnotics zolpidem, zaleplon, and eszopiclone, but not the barbiturates
  • approved for use in reversing the CNS depressant effects of BZ overdose and hastens recovery after BZ use in medical procedures
  • when given IV, it acts rapidly, but has a short t1/2 (0.7-1.3 hrs)
  • because all BZs have a longer duration of action, sedation commonly recurs, requiring repeated administration of this antagonist
A

Flumazenil

36
Q

Adverse Rxns of Buspirone

A
  • nonspecific chest pain, tachycardia, palpitations, dizziness, nervousness, tinnitus, GI distress, and paresthesias
  • these adverse effects are extremely rare
  • buspirone should not be taken in combination with MAO inhibitors, as significant elevations in blood pressure can result
37
Q

Beta-Blockers

A
  • typically used to treat heart conditions and high BP
  • they are also used in an off-label application to control the physical sxs of anxiety (i.e. trembling, sweating)
  • taken for a short period of time, these agents can help individuals keep physical sxs under control during stressful situations (e.g. when a person with social phobia has to give a speech or attend a meeting)
38
Q

Triazolam

A

short acting BZ

Anti-Anxiety Agents (1 decks)

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