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Pharmacology > Antianxiety and Antipsychotics > Flashcards

Antianxiety and Antipsychotics Flashcards

1
Q

Antianxiety medications are also called what 2 things?

A
  1. Sedative hyponotics
  2. Minor tranquilizers

**These are low potency compounds used to treat anxiety and neurosis

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2
Q

Which drugs account for 75% of 100 million prescriptions written for sedatives/tranquilizers?

A

1. dizepam (Valium)

  1. chlordizepoxide (Librium)
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3
Q

All benzodiazepines (BDZ) have same basic structure:

A
  • 2 nitrogens “diazo”
  • Benzene ring = binds to GABA receptors
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4
Q

Popular BDZ drugs =

A
  1. chlordiazepoxide (Librium)

2. diazepam (Valium)

3. lorazepam (Ativan)

  1. oxazepam (Serax)

5. alprazolam (Xanax)

  1. triazolam (Halcion)

7. midazolam (Versed) = “dazzle”

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5
Q

Which popular BDZ drug is used for preoperative sedation and inudction of general anesthesia?

A

midazolam (Versed)

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6
Q

T or F, Benzodiazepines were originally not thought of to be addictive. Now, these are known to be highly addictive

A

True

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7
Q

What schedule are Benzodiazepines?

A

Schedule IV/V opiates in the U.S. due to their abuse potential.

  • Complicated by the fact that tolearnce develops to these drugs requiring increasingly higher doses = contributes to addiction
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8
Q

Benzodiazepines produce 3 distinct effects:

A

1. Effects on behavior

2. Anticonvulsant effects

3. Muscle relaxation

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9
Q

How do Benzodiazepines effect behavior

A
  1. Reduces aggression and hostility
  2. Reduce other symptoms of non-specific CNS depression

(Anxiety reduction, Drowsiness/depression)

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10
Q

Low doses of Benzodiazepines have what effect on behavior? High doses?

A

Anxiety reduction at low doses

Drowsiness/depression at high doses

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11
Q

Which two drugs prevent and arrest local anesthetic-induced seizures in dentistry?

A

1. diazepam (Valium)

2. midazolam (Versed)

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12
Q

How is diazepam and midazolam administered?

A

Slowly by IV (diazepam 5 mg/minute or midazolam 1 mg/minute)

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13
Q

Which drugs are most potent at muscle relaxation?

A

1. diazepam (Valium)

2. chlordiazepoxide (Librium)

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14
Q

Describe how Benzos cause muscle relaxation

A

Depresses motor nerve and muscle function in both healthy persons and in patients suffering from skeletal muscle disorders

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15
Q

Where are the receptor sites for BDZ found?

A

In the CNS

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16
Q

Describe the mechanism of action of BDZs

A

BDZ affect the concentration of most neurotransmitters, including GABA.

  • When GABA receptor is activated, the Cl- channel opens, allowing Cl- influx, membrane hyperpolarization and neuronal inhibition. BDZ facilitate GABA action and “indirectly” increase inhibitory neurotransmission resulting from GABA

**Extra: BDZ increase frequency at which Cl- channels open in response to GABA

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17
Q

T or F, GABA receptor embedded in neuronal plasma membranes, locate at synapse = binds both GABA and BDZ

A

True - Presence of GABA enhances binding of BDZ

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18
Q

Binding to GABA receptor sites is:

A
  1. Rapid
  2. Reversible
  3. Stereospecific
  4. Saturable
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19
Q

Describe the body’s handling of BDZs

A

1. Most have very long half-lives

2. Most are metabolized to active compounds

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20
Q

BDZs have long half-lives so repeated dosing results in accumulation of the drug in the body. However, there is one drug that is metabolized rapidly to INACTIVE compounds = no significant accumulation. Which drug is it?

A

lorazepam (Ativan)

** A good choice for dentistry

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21
Q

Use of BDZs in Medicine

A
  1. Relief of anxiety
  2. Skeletal muscle relaxation = muscle strains
  3. Hypnotic to treat insomnia = induces sleep
  4. Treat withdrawal symptoms of alcoholism = helps alcoholic through initial withdrawal effects
  5. Pre-operative medication = used to decrease apprehension
22
Q

Use of BDZs in Dentistry

A
  1. Reduce pre-operative anxiety
    - diazepam (Valium), lorazepam (Ativan), alprazolam (Xanax), triazolam (Halcion)
  2. IV sedative and amnesiac
  3. Emergency intervention for seizures
23
Q

Adverse Effects of BDZs

A
  1. CNS depression (Fatigue, drowsiness
  2. Xerostomia
  3. Abuse and addiction
  4. Additive effects with other CNS depressants especially alcohol
  5. Dangerous drug interaction (Alcohol and BDZ)
24
Q

If a patient is taking BDZs, how does this affect your dosage of opiates?

A

Reduce dose of opiates by 1/3 of normal dose when a BDZ is added (diazepam)

25
Q

T or F, There is no drug interaction between BDZ and Alcohol. Patients are safe in consuming alcohol while on these medications

A

False, This is a dangerous drug interaction! Results in severe CNS depression that may be DEADLY. Results in significant respiratory depression.

  • Because of the long half-life, teach your patients to avoid alcohol when using these medications.
26
Q

What is buspirone (BuSpar) used for and its mechanism of action

A
  • Used for management of generalized anxiety disorder
  • Mechanism is unknown –> Binds serotonin receptors without affecting BDZ-GABA receptors
27
Q

Many dental drug interactions increase the concentration of buspirone - what drugs should you avoid with concurrent use?

A
  1. ciprofloxacin
  2. clarithromycin
  3. erythromycin
  4. doxycycline
  5. systemic antifungals
    - RED Flag Drugs in dentistry
28
Q

Anti-anxiety medications together with what other drug class causes xerostomia?

A

Antidepressant

29
Q

Older term for major tranquilizers or antipsychotic medications

A

neuroleptic drugs

30
Q

Major Tranquilizers are used in the treatment of: (6)

A
  1. Psychotic disorders (Schizophrenia, paranoia)
  2. Acute delirium and dementia
  3. Manic episodes during induction of lithium
  4. Movement disorders - Huntington’s disease, Tourette’s syndrome, Ballismus
  5. Intractable hiccups
  6. Severe nausea and vomiting
31
Q

Major Tranquilizers bind to a variety of receptors and act as what?

A

Antagonists

32
Q

Name the 6 receptors that Major Tranquilizers bind to

A
  1. dopaminergic
  2. alpha1 and alpha2 adrenergic
  3. serotonergic (5-HT)
  4. muscarinic
  5. H1 histamine
  6. sigma opioid
33
Q

Name the three major effects of major tranquilizers and how their effects are believed to occur?

A
  1. Antipsychotic action = blockage in prefrontal cortex and limbic areas
  2. Extrapyramidal side effects = blockade in basal ganglia
  3. Antiemetic effects = blockade in chemoreceptor trigger zone of the medulla

**Blockade of dopaminergic transmission in various areas of brain is thought to be responsible for their major effects

34
Q

What is the Dopaminergic hypothesis of Schizophrenia?

A

Overactivity of dopaminergic system - thus, antipsychotic medications reduce dopaminergic activity by blocking D2 receptors

35
Q

T or F, All major tranquilizers are strong D2 dopamine receptor antagonists and effective doses (potency) are indirectly proportional to their D2 antagonism

A

False, directly proportional

  • Exception: cloxapine (Clozaril) = low D2 antagonism; effective dose is lower than is expected
36
Q

Primary site for dopaminergic neurons

A

Striatum - Most tranquilizer drugs work here

  • Antipsychotics occupy >70% of striatal D2 sites
  • clozapine occupies only 30%
  • **Also in Limbic system and prefrontal cortex - likely sites for curative actions of clozapine, where this drug occupies the same high percentage of D2 receptors as other antipsychotics.
37
Q

What are the problems with the Dopaminergic Hypothesis of Schizophrenia

A
  • Receptors are blocked within 2-4 hours after drug administration, but therapeutic activity requires several weeks of treatment to achieve full effect
  • Therapeutic effects is related to slow-developing depolarization block of dopaminergic neurons
  • Schizophrenia is also associated with alterations in structure of neurons in prefrontal cortex and limbic system
38
Q

Dopamine is involved in:

A
  1. Neurotransmission
  2. Regulation of neuronal morpholoy
39
Q

How are Major Tranquilizers administered?

A

Administered orally or by IM

40
Q

Maximal concentration in blood for major tranquilizers occurs when? What is the half-life?

A
  • Maximal concentration in blood is achieved 2-4 hours after oral adminsitration and within 30-4- minutes after IM
  • Half-life = 18-40 hours
  • Once daily dosing
  • All durgs have similar efficacy
41
Q

Side Effects of Major Tranquilizers:

A
  1. Akathisia = restless legs syndrome - caused by D2 receptor blockage in basal ganglia
  2. Dystonia = sustained muscular contraction
  3. Tardive Dyskinesia - abnormal movements, particularly of face and tongue, but may also be of trunk and limbs
42
Q

Sedation and autonimc side effects of major tranquilizers are caused by what?

A

blockade of histamine, cholinergic and adrenergic receptors

  • orthostatic hypotension, blurred vision, dry mouth, nasal congestion, constipation, urinary retention
43
Q

T or F, Most extrapyramidal side effects of major tranquilizers are treatable with antiadrenergic drugs

A

False, anticholinergic drugs

44
Q

Extrapyramidal side effects of antipsychotics

A

Parkinsonism - akinesia (difficulties in initiating movment), tremor, rigidity

Caused by blockage of D2 receptors in basal ganglia

45
Q

T or F, Antipsychotics are highly addictive and have a low therapeutic index

A

False, Not addictive and have a HIGH therapeutic index

46
Q

Antipsychotics potentiate CNS effects of :

A

Sedatives

Analgesics

Antihistamines

47
Q

T or F, Antipsychotics potentiate the respiratory depression caused by opioids

A

True

48
Q

Which other drug classes have this drug interaction with antipsychotics:

  • Decrease absorption of antipsychotics
  • Decrease plasma levels of antipsychotics
  • Antipyschotics may alter efficacy of this medication
A
  • Antacids
  • Anticonvulsants
  • Antihypertensive
49
Q

Typical Antipsychotics:

A

clorpromazine (Thorazine)

haloperidol (Haldol)

prochlorperazine (Compro, Compazine)

50
Q

Atypical Antipsychotics

A

- aripiprazole (Abilify)

- clozapine (Clozaril)

- risperdone (Risperdal)

51
Q

3 Critical points for dentist regarding antipsychotics

A
  1. May cause hematologic disturbances = check white blood cell counts
  2. May alter QT interval of heart (caution with epinephrine; risk for arrhythmias)
  3. Cause extrapyramidal effects (movement disorders) - bruxism, Tardive dyskinesia

Pharmacology (24 decks)

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