Anxiety and Its Control Flashcards

1
Q

Immediate Acting Antianxiety Agents

A

Benzodiazepines, Barbiturates, Alcohol, Beta Blockers (ex. Panic attacks)

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2
Q

Delayed Action Antianxiety Agents

A

Antidepressant drugs, Buspirone (ex. Medical anxiety)

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3
Q

Benzodiazepine Effects

A

Diazepam (Valium)
Relief of Anxiety (Tame animals), Sedation, Hypnosis (Large TI 70+) > Limited REM suppression, Amnesia, Anticonvulsant (Medically induced), Muscle Relaxant, Controls gagging and vomiting, Minimal effect on heart and respiration (Lost safety margin with combination of drugs; Exception = Midazolam - Between Benzodiazepine and Barbiturate), Treatment of alcohol withdrawal - chlordiazepoxide, May contribute to mild analgesia, Adjunct treatment in psychiatry

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4
Q

Diazepam

A

(Valium); Benzodiazepine; Very Fast onset; Single dose, behavioral, 6hr, multidose, blood level up to 200; Long active metabolites; Used for antianxiety, anticonvulsant, sedation and hypnotic, muscle relaxant, amnesia; Mild respiratory depression - may be lethal when combined with other depressants, Amesia; Class D pregnancy

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5
Q

Triazolam

A

(Halcion); Benzodiazepine; Fast onset; 2-3hr duration half-life; Short active metabolites; Hypnotic, Used for antianxiety, anticonvulsant, sedation and hypnotic, muscle relaxant, amnesia; Amnesia; Class X pregnancy

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6
Q

Midazolam

A

(Versed); Benzodiazepine; Fast onset; 1-12hr duration; Short active metabolites; Pre-anesthesia and conscious sedation, given parenterally; Overdose can cause respiratory depression and result in death; Amnesia; Class D pregnancy; pH4 - water/lipid soluble, More efficacy binds to receptor than Diazepam, Possible platelet aggregation, Status epilepticus/Local anesthetic induced seizures, IV, IM, Intranasal, Intrabuccal

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7
Q

Flurazepam

A

(Dalmane); Benzodiazepine; Inter med. onset; Multidose, Up to 100hr duration; Long active metabolites; Hypnotic (Similar to diazepam); Amnesia, Class X pregnancy

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8
Q

Alprazolam

A

(Xanax); Benzodiazepine; Rapid onset; 12-15hr duration; Short active metabolites; May have antidepressant properties; Not much amnesia; Class D pregnancy

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9
Q

Clonazepam

A

(Klonopin); Benzodiazepine; Slow onset; 24hr duration; Used as anticonvulsant; Partial agonist; Class D pregnancy

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10
Q

Chlordiazepoxide

A

(Librium); Benzodiazepine; Inter med. onset; 5-30hr duration; Long active metabolites; Withdrawal; Minimal respiratory depression, Amnesia

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11
Q

Lorazepam

A

(Ativan); Benzodiazepine; Int. (2hrs) onset; 10-18hr duration; Pre-op sedation in elderly; Mild respiratory depression; Amnesia, Class D pregnancy

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12
Q

Oxazepam

A

(Serax); Benzodiazepine; Int.Slow onset; 5-13hr onset; Pre-op sedation in elderly; Mild respiratory depression; Amnesia; Class D pregnancy

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13
Q

Benzodiazepine Warnings and Contraindications

A

Sedation, Amnesia, Paradoxical excitation, Allergy, Avoid use in pregnancy class - D,X, Venous thrombosis (IV - Diazepam), Increase drug metabolizing enzymes, Altered kinetics in liver or kidney failure (Black box warning), Pulmonary disease (COPD, Myesthinia gravis, Sleep Apnea), Respiratory depression - Midazolam, Narrow angle glaucoma BB, Tolerance and dependence, Drug interactions

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14
Q

Benzodiazepine Drug Interactions - Physiologic Stimulants and Depressants

A

Stimulants: Nicotine, Caffiene, Methylphenidate, Amphetamine, Cocaine
Depressants: Sedatives, Anesthetics, Opiates, Neurologics (decrease Benzodiazepine safety)

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15
Q

Benzodiazepine Drug Interactions - Drugs Inhibiting Metabolism of Benzodiazepines

A

Erythromycins (Midazolam, Alprazolam, Triazolam), Diltiazam and Verapamil (Substrates for CYP3A4), Azole Antifungals (Diazepam + Fluconazole = 2.5XDiazepam); Grapefruit juice (Midazolam, Alprazolam, Triazolam); Cimetidine, Oral contraceptive, Fluoxetine (SSRI); Propoxyphene, Propranolol; Isoniazd, Vaproic acid

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16
Q

Smoking with Benzodiazepine

A

(Antagonizes sedation)

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17
Q

Flumazenil

A

(Romazicon); Benzodiazepine Antagonist; Reverses actions (Blocks BZ receptor) (exception - Antagonizes zolpidem, Z drugs), Reverses sedation and amnesia better than respiratory depression, Relatively short acting (t1/2 =1hrs), Some use in epilepsy; 5mg/min up to 3mg/hr; May precipitate withdrawal in BZ dependent individuals or overdosed cyclic antidepressants

18
Q

Zolpidem

A

(Ambien); Hypnotic Drug; Act on BZ1 (Omega 1), Anticonvulsant, Amnesia like Triazolam, Issues with sleep driving, eating and sex; 10mg men/5mg women; Max effect in 1.6hrs, Half life in 2.5hrs, Ambien CR; Metabolized CYP3A4 in liver (Reduce in hepatic disease, elder, no active metabolites), Absorption reduced by meals; Side effects: Drowsiness, Dizziness, Allergy, Hallucinations (Combine with SSRI), Risk of dependence; Interaction reverse by Flumazenil

19
Q

ZZZ Drugs

A

Zolpidem, Zaleplon (Sonata), esZopiclone (Lunesta); Behaviorally similar to BZs; Pregnancy Class C; Flumazenil reverses;

20
Q

Buspirone

A

(Buspar); Long acting Anti-anxiety; Don’t prescribe for dental anxiety; Proposed action partial agonist at serotonin 5HT receptors, Minor antagonist action on dopaminergic receptors, Increased use in psychiatry; Min sedation, Not anticonvulsant, Little risk of dependence; Drug interaction - MAO inhibitors (hypertension), RX 5-10mg

21
Q

Melatonin agonists

A

Natural pineal hormone, OTC, Remelteon (Rozerem) - Sleep onset insomnia, MT1, MT2, MT3 agonist; Shorten sleep latency, Hormone associated with circadian rhythm, Side effects (Tasimelteon - Hetlioz - 24hr sleep-wake disorder in blind)

22
Q

Suvorexant

A

(Belsomra CIV); Orexin antagonist, Marginally effective, Hangover sleepiness, Expensive

23
Q

Phenobarbital

A

Barbiturate; 3 Partition coefficient, Slow absorption from stomach, Slow entry into CNS, 30% renal excretion, Terminate liver and kidney, Long duration of action, Anticonvulsant and sedative, Soluble in oil/water

24
Q

Pentobarbital

A

Barbiturate; 50 Partition coefficient, Rapid absorption from stomach, Rapid entry into CNS, Negligible renal excretion, Termination of action in liver; Short duration of action; Hypnotic use

25
Q

Thiopental

A

580 Partition coefficient, Rapid absorption from stomach (Not oral); Very rapid rate of entry into CNS, Negligible renal excretion, Redistribution and liver termination of action, Ultrashort duration of action, Induction anesthetic use, Moves out of brain into mass of body down concentration gradient

26
Q

Barbiturate Pharmacology

A

Hypnotics, Sedatives, Anesthetic, Muscle relaxants, Anticonvulsant, Not analgesic (May be hyperalgesic)

27
Q

Barbiturate Side Effects and Toxicity

A

Hangover, Paradoxical excitement (Inhibitory neurons more, Occurs before anesthesia), Decreased REM sleep, Dependence (Related to dose and duration - Severe withdrawl), Induce drug metabolizing enzymes of liver (P450, UGT) - Metabolic intolerance (Pharmacokinetic intolerance, Some pharmacodynamic, Less and less drug effect), Drug interactions (Sedation), Porphyria (ALA synthetase increase contraindication), Respiratory and cardiac depression (High dose), Allergies, Birth defects Class D

28
Q

Barbiturate Examples

A

Nembutal = Pentobarbital, CII, Hypnotic; Luminal = Phenobarbital, CIV, Raise seizure threshold; Pentothal = Thiopental, CIII, Through paradox excitation to anesthesia; Presate = Hexobarbital, CII, Preop Sedative that is rapid

29
Q

Selected Non-Barbiturate Sedative - Hypnotics

A

Examples: Quaaludes (CI), Glutethimide (CII), Thalidomide - Sedative, Antiinflammatory, Immunosuppressant (Apthous ulcers, leprosy, brain malignancy, major teratogen); Similar to barbiturate and toxicity

30
Q

Chloral Hydrate

A

Short, mild sedative; Metabolized to trichoral ethanol; Used in elder and children (Diazepam or antihistamines are safer); Eliminated by liver and kidney (ONE PURPOSE) - Induce hepatic enzymes P450; Drug interaction with alcohol (Micky finn); Irritation of GI tract and poor taste; Tolerance and dependence; Possibly carcinogenic; Active metabolite - Trichloroethanol, Inactive metabolite - Trichloroacetic acid

31
Q

Date Rape Drugs

A

Canada - Triazolam (Halcion); Outside US - Flunitrazepam (Rhoypnol), Ketamine (Ketalar) - sedation and analgesic and Phencylidine, TX - Gamma-Hydroxbutyrate (GHB) - Release of GH - Severe withdrawl

32
Q

Centrally Acting Muscle Relaxants (CAMRs)

A

Acts on CNS poly-snaptic reflexes, Effectiveness is proportional to sedative, Important to warn patient of drowsiness, Used with NSAID analgesic in pain, Adjunct in TMJ treatment, Large TI than barbiturates (~20) but less safe than Diazepam (~70), Similar side effect and toxicity to barbiturates, Can induce liver enzymes, Tolerance and dependence, Beers list (problem in elder)

33
Q

CAMR Examples

A

Mephenisin like - Carisoprodol (Soma), CIV; Chlorozoxazone (Paraflex); Methocarbamol (Robaxin); Pregnancy Class C

Non-Mephenisn like - Orphenadrine (Norflex); Cyclobenzaprine (Flexeril) - Antihistamine like, Structurally dissimilar, Tricyclic antidepressant - Blocks reuptake of NE and 5HT; Pregnancy Class C and B

34
Q

Agents for Relief or Spasticity

A

MS or spasticity

Baclofen (Lioresal), Dantrolene (Dantrium), Tizanidine (Zanaflex)

35
Q

Baclofen

A

(Lioresal); GABA-B receptor to decrease spasticity, MS or spinal cord injury, Intrathecal (spinal) route; Side effects - CNS depression, Tolerance and dependence, Teratogenic (Pregnancy Class C), Trigeminal neuralgia, Cerebral palsy, Tardive dyskinesia, Titrated dose

36
Q

Dantrolene

A

(Dantrium); Acts in muscle - Contractile response; Used in upper spinal cord lesions that induce spasticity - Used in malignant hyperthermia; Side effects - Serious heptatoxicity, Sedation, Weakness, Respiratory depression, Diarrhea; Titrate dose, Pregnancy Class C

37
Q

Tizanidine

A

(Zanaflex); Alpha 2 agonist - Reduce cardiac tone and relax muscles, Treats spasticity associated with MS and spinal cord injury; Flutripine - alpha 2 agonist and NMDA inhibitor; May cause pQT; Side effects - Drowsiness, PROFOUND DRY MOUTH, Mydriasis, Asthenia, Dizziness, Hypotension (Orthostatic as well), Pregnancy Class C

38
Q

Natureceutical Agents with Sedative Property

A

Valarian, Kava Kava, Melatonin

39
Q

Agents with Sedation as Side Effect

A

Opiates, Anticonvulsants, Antipsychotics, Tranquilizers, Tricyclic Antidepressants, Anticholinergics, Beta receptor blockers, Diuretics, Anesthetics

40
Q

Agents Antagonizing Sedation Stimulants

A

Caffeine, Nicotine, Amphetamines, Cocaine

41
Q

CNS Depressants

A

Alcohol, Chloral Hydrate (CIV); Solvents and glues - General - Hydrocarbons; Barbiturates (CII - Phenobarbital=IV), Nonbarbiturate Sedatives (CII), Muscle relaxants - CIV, Benzodiazepines (CIV), Cannabis (CI)