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Found. Pharm > Anxiolytic, Tranquilizing and Muscle Relaxant Medications > Flashcards

Anxiolytic, Tranquilizing and Muscle Relaxant Medications Flashcards

1
Q

Tranquilizer

A

Medication that produces emotional calming, reduces anxiety, tension, agitation and other related emotional states
* “Major tranquilizers” –antipsychotics
* “Minor tranquilizers” –anxiolytics

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2
Q

Anxiolytic

A

Reduces or relieves anxiety, fear, apprehension

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3
Q

Sedative

A

eneral slowing down of cognitive function, reduction of restlessness, impairment of memory formation

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4
Q

Hypnotic

A

induction of sleep

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5
Q

Myorelaxant

A

causing relaxation of the muscles

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6
Q

Antiepileptic/anticonvulsant

A

Used to treat epilepsy/convulsions
- Preferred term is antiseizure medication

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7
Q

Epilepsy

A

Chronic neurological disorder characterized by sudden recurrent episodes (seizures) of sensory disturbance, loss of consciousness, or convulsions, associated with abnormal electrical activity in the brain

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8
Q

Status Epilepticus

A

A seizure lasting longer than 5 minutes, or repeated seizures without returning to normal consciousness between seizures

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9
Q

Mania

A

ood episode associated with bipolar disorder, characterized by periods of great excitement or euphoria, increased psychomotor activity, racing thoughts and attention difficulties

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10
Q

Neurosis

A

An outdated term for any long-term psychiatric disorder in which contact with reality is retained and the condition is recognized by the patient as abnormal
* Typically referring to anxiety disorders

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11
Q

Neuralgia

A

Severe burning or stabbing pain along the course of a
nerve, e.g., post-herpetic neuralgia

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12
Q

Neuropathy

A

Any disease of the peripheral nerves, usually causing
weakness and numbness

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13
Q

Tolerance

A

A person no longer responds to a drug in the way they did at first, need a higher dose to achieve the same effect

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14
Q

Dependence

A

When a person taking a substance every day over a long period stops using the substance, their body goes through withdrawal

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15
Q

Withdrawal

A

Group of physical and mental symptoms that occur when stopping a substance; can range from mild (caffeine) to life-threatening (alcohol)

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16
Q

Addiction

A

Person taking a substance regularly and has difficulty stopping, despite negative consequences from using the substance
- Preferred term is substance use disorder

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17
Q

Barbiturates

A

Minor Tranquilizers
- Became popular for their anxiolytic, sedative and hypnotic effects
- First truly effective antiseizure medications
- Opened up the field for IV anesthesia

Ex. Amobarbital(Amytal®), Pentobarbital (Nembutal®),
Phenobarbital (Luminal®)

18
Q

Barbiturates Problems

A
  • Physical and psychologic dependence
  • Tolerance and withdrawal
  • Respiratory depression in overdose
19
Q

Meprobomate (Miltown®, Equanil®)

A

First drug marketed specifically as an anxiolytic
- Anxiolytic, sedative and myorelaxant properties
– Binds to GABA-A receptor

Schedule IV
- Tolerance/dependence
- Dangerous withdrawal –hallucinations, seizures
- Lethal in overdose

20
Q

Benzodiazepines

Azo, Azep, Azepam, Azolam

A
  • Versatile in their use
  • Generally safer, less respiratory depression/toxicity than barbiturates
21
Q

Benzodiazepine Indications

A
  • Anxiolytic: anxiety disorders, procedural anxiety, acute agitation
  • Antiseizure: Typically adjunctively
  • Myorelaxant
  • Sedative hypnotic: insomnia
  • Management of Alcohol Withdrawal Syndrome (AWS)
22
Q

Benzodiazepine Mechanism of Action

A

Potentiate the effects of Gamma Aminobutyric Acid (GABA)
- Main inhibitory chemical in the brain

Schedule IV controlled substances
- Euphoria
- Tolerance/dependence
- Withdrawal syndrome
- Tremors
- Seizures

23
Q

Benzodiazepine
Contraindications/Precautions

A
  • Myasthenia gravis
  • Respiratory insufficiency
  • Liver disease
  • Acute narrow angle glaucoma
  • Pregnancy –premature birth, low birth weight, “floppy infant syndrome”
  • History of substance use disorder
24
Q

Benzodiazepine Adverse Effects

A
  • Sedation
  • Ataxia
  • Impaired cognitive and motor function
  • Confusion, delirium
  • Amnesia
  • Paradoxical excitation/disinhibition
  • Rebound anxiety
  • Depression –with long-term use
  • Older patients –falls, fractures; Reduced metabolism and clearance
  • Fatal overdose is uncommon, except when mixed with other CNS depressant
25
Q

Buspirone(Buspar®)

A

Miscellaneous Antianxiety Agent
Indication:
- Generalized Anxiety Disorder
- Augmentation of Major Depressive Disorder
- No potential for misuse, no tolerance/dependence, favorable safety profile
- Dosed 2-3 times per day, no immediate effect, significant drug interactions (major substrate CYP3A4)

MOA:
- No direct effect on GABA receptors, high affinity for serotonin receptors and moderate affinity for dopamine receptors

26
Q

Skeletal Muscle Relaxants

A
  • Cyclobenzaprine (Flexeril®)
  • Methocarbamol (Robaxin®)
  • Baclofen (Gablofen®, Lioresal®)
  • Metaxolone(Skelaxin®)
  • Chlorzoxazone (Lorzone®)
  • Dantrolene (Dantrium®, Ryanodex®)
  • Orophenadrine(Norflex®)
  • Tizanidine (Zanaflex®)
  • Carisoprodol (Soma®) –metabolized to meprobomate, C-IV
27
Q

Skeletal Muscle Relaxants Indications

A
  • Spasticity associated with neurologic diseases (Multiple Sclerosis, cerebral palsy) or spinal injury
  • Musculoskeletal pain –short term use
  • Fibromyalgia
  • Malignant hyperthermia
  • Neuroleptic Malignant Syndrome
28
Q

Skeletal Muscle Relaxants Indications

A
  • Spasticity associated with neurologic diseases (Multiple Sclerosis, cerebral palsy) or spinal injury
  • Musculoskeletal pain –short term use
  • Fibromyalgia
  • Malignant hyperthermia
  • Neuroleptic Malignant Syndrome
29
Q

Muscle Relaxant Adverse Effects

A
  • Confusion
  • Drowsiness
  • Headache
  • Dizziness
  • Nausea/vomiting
  • Anticholinergic effects
    – Constipation
    – Dry mouth
    – Blurred Vision
30
Q

Non-Benzodiazepine Antiseizure
Medications (Azepine)

A

Carbamazepine (Tegretol®, Carbatrol®, Equetro®)
- Seizure disorders
- Bipolar disorder
- Neuropathic pain

Oxcarbazepine (Trileptal®, Oxtellar®)
Eslicarbazepine(Aptiom®)

Suicidal ideation -warning for all antiseizure medications
- Increased risk of suicidal thoughts/behavior
- Monitor for behavior changes, especially early in treatment

31
Q

Antiseizure Medication Adverse Effect

A
  • Dizziness
  • Drowsiness
  • Headache
  • Double or blurry vision
  • Ataxia –slurred speech, stumbling, falling, incoordination
  • Nausea
32
Q

Carbamazepine
Contraindications/Precautions

A
  • Bone marrow suppression–anemia, low white blood cell count
  • Severe rash –Stevens-Johnson Syndrome, Toxic Epidermal Necrolysis
    – Asian ancestry –HLA-B 1502 allele
  • Liver disease
  • Hyponatremia
  • Use with certain HIV medications –MANY drug interactions
  • Pregnancy –spina bifida, craniofacial defects, cardiovascular malformations
33
Q

Oxcarbazepine

A

Structural derivative of carbamazepin: contraindicated with carbamazepine allergy

Less potential for several adverse effects
- Liver disease
- Bone marrow suppression

Less drug interaction

Novartis charged with marketing for unapproved uses –neuropathic pain, bipolar disorder

34
Q

Eslicarbazepine

A

Derivative of the active metabolite of oxcarbazepine

Contraindications:
- Severe heart rhythm disorders (Atrioventricular block)
- Allergy to carbamazepine or oxcarbazepine

Expensive: brand only

35
Q

Non-Benzodiazepine (BZD)
Sedative-Hypnotics

A

Non-benzodiazepine receptor agonists –“Z drugs”
- Zolpidem (Ambien®)
- Zaleplon (Sonata®)
- Eszopiclone (Lunesta®)

Ramelteon (Rozerem®)
Low-dose doxepin (Silenor®)
Orexin receptor antagonists
- Suvorexant (Belsomra®)
- Lemborexant (Dayvigo®)
- Daridorexant(Quviviq®)

36
Q

Non-Benzodiazepine Receptor Agonists
(NBRAs)

A

Enchance GABA activity by binding to BZD-1 receptors
- No effect on BZD-2
- Minimal anxiolytic, myorelaxant, anticonvulsant properties

C-IV –potential for misuse, tolerance, dependence
Warnings/Precautions
- Complex sleep behaviors
- May worsen depression
- Caution with sleep apnea, COPD

37
Q

Ramelteon (Rozerem®)

A

Melatonin receptor agonist
- Indicated for sleep onset insomnia
- No concern for misuse

Adverse effects
- Headache
- Dizziness
- Somnolence

38
Q

Low-dose Doxepin
(Silenor®)

A

Tricyclic Antidepressant (TCA)
- At low doses acts as an antihistamine
- Indicated for sleep maintenance insomnia
- No concern for misuse

Adverse effects
- Drowsiness
- Headache
- Dry mouth

39
Q

Orexin Antagonists

A

Effective for both sleep onset and sleep maintenance
C-IV: precaution

Warnings
- Narcolepsy-like symptoms
-Daytime somnolence and next-day driving impairment –ensure at least 7-8 hours of sleep

Adverse effects
- Abnormal dreams
- Headache
- Somnolence

40
Q

OTC Sedative-Hypnotics

A

Antihistamines
- Diphenhydramine (Benadryl®)
- Doxylamine (Unisom®, Sleep Aid®)
- Adverse effects – dry mouth, daytime hangover, tolerance in 7-10 days

Melatonin: may be helpful in children with autism, ADHD
Valerian: withdrawal concerns, potential drug interactions
Kava:liver toxicity

41
Q

Summary

A

Some of the earliest psychotropic/neurologic medications, known as “tranquilizers” had a wide array of clinical effects
- Anxiolytic
- Sedative
- Hypnotic
- Myorelaxant

Barbiturates and meprobomate largely fell out of favor due to their lethality in overdose

Benzodiazepines have largely replaced these older medications due to their improved safety profile, but still have significant risks
- Newer medications have a narrower spectrum of activity but improved safety profile

Found. Pharm (14 decks)

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