Pharmacology Test 2 - Antianxiety Agents, Hypnotics, Antipsychotics

Front 1

Benzodiazepines

Back 1

Scheduled treatment for anxiety disorders - increases GABA effects

Action: binds to specific receptor sites in GABA receptor-channel complex and amplifies GABA action. Do no mimick GABA, but simply intensify its effects.

Lipid soluble - crosses quickly, euphoria shortly after administration

Front 2

Benzodiazepine Examples

Back 2

1. Alprazolem (Xanax) - most addictive, short acting
2. Lorazepan (Ativan) - lacks active metabolites, less addictive than xanax
3. Clonazepam (Klonipin) - rapid absorption
4. diazepam (Valium) - rapid absorption

Front 3

Benzodiazepine Adverse Effects

Back 3

1. CNS depression - lack coordination
2. Respiratory depression - higher risk with IV administration
3. Anterograde Amnesia - loss of memory from time they take the med.
4. Paradoxical Psychologic Effects
5. Tolerance, dependence, toxicity - not if given for anxiety, but will for seizures even with short term (6-12 wks.)
6. Abuse (schedule IV)- readily crosses placenta and enters breast milk (babies reach toxic level quick because of underdeveloped BBB)

Front 4

Advantages of Benzodiazepines

Back 4

1. Rapid onset
2. Well-tolerated
3. Few drug-drug interactions - CNS depression (opiods, barbiturates causes severe resp. depression)
4. Little effects on cardiovascular system - quickly IV
5. Generics available

Front 5

Barbiturates

Back 5

Schedule II-III

Uses: seizure disorders, sedation (rare), pre-anesthesia; generally not used to anxiety because there are safer options available

- Effects GABA, binds to GABA-Chloride channels

Accelerates the metabolism of some drugs (including themselves); REPIRATORY DEPRESSION (RR < 12, usually lower)

Front 6

Barbiturates - S/S of toxicity

Back 6

Early:
1. Restlessness
2. Insomnia
3. Confusion

Late:
1. Convulsions
2. Psychosis
3. Cardiac collapse
4. Death

Front 7

Barbiturates - S/S of overdose

Back 7

1.Hypotension
2. Respiratory Depression
3. Hypothermia
4. Pin point pupils
5. Coma

Treatment: gastric lavage, multi-system support

Front 8

Benzodiazepine Like Drugs

Back 8

1. Zolpidem (Ambien)
2. Zalwpion (Sonata)
3. Exzopiclone (Lunesta)

Mechanism: selective benzodiazepine agonist qualities (GABA receptor chloride channel)

Uses: initial insomnia

SE: drowsiness, dizziness, headache, dry mouth, controlled substance schedule IV

Front 9

Other Meds used to treat insomnia

Back 9

1. Ramelteon (Rozerem) - melotonin agonist - activates specific receptor sybtypes of melatonin

Adverse Effects: drowsiness, dizziness, fatigue, neuroendocrine effects secondary to increased levels of prolactin and decreased levels of testosterone

Interactions: Fluvoxamine (Luvox) - increases effects x50.
- Antihistamines
- Trazodone (Desyrel)

Front 10

Busiprone (Buspar)

Back 10

Mechanism: not clearly established; affinity ro seotonin receptors and lower affinity to dopamine receptors. Does not bind to GABA receptors or benzodiazepine sites

should be taken with food for better absorption

Lag time to peak effectiveness - patients continue on other med until therapeutic levels are met. Effec in about 1 week, peak in 2-3 weeks.

Front 11

Buspirone - Adverse Effects

Back 11

1. Dizziness
2. Nausea
3. Headache
4. Nervousness
5. Excitement

Front 12

Antipsychotic Agents

Back 12

- entirely romove or make psychotic symptoms considerably less intense
- Maximum relief: several wekks or months (effects after first few doses
- Maintanence doses: 6-12 months gradual taper to lower dose
- chronic persistent illness (long term)

Front 13

Low potency

Back 13

Prototype: Chorpromazine (throrazine)

Target symptoms:
1. Schizophrenia and psychosis
2. Suppresion of vomiting (phenergan)
3. Relief of intractable hiccoughs

Front 14

High potency

Back 14

Prototype: Haloperidol (Haldol)

Target symptoms:
1. Schizophrenia and psychosis
2. Agitation or aggression

Front 15

Antipsychotic Mechanism of Action

Back 15

- Blocks D2 receptor sites in mesolimbic pathway (poitive symptoms)
- also block other D2 receptors (causing EPS or muscular side effects)
- Other actions/ effects - partial histamine antagonism, partial acetylcholine blockage, antagonism of alpha-adrenergic system