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Pharmacology > Pharmacology Chapter 12 (Unit 1) > Flashcards

Pharmacology Chapter 12 (Unit 1) Flashcards

1
Q
  • A drug that has a calming effect or that depresses the central nervous system(CNS)
  • Drugs that have an inhibitory effect on the CNS to the degree that they reduce:

-Nervousness
-Excitability
-Irritability without causing sleep

  • Can become a hypnotic if given in a large enough dose
A

Sedative

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2
Q
  • This drug causes sleep

-Much more potent effect on CNS than sedatives

  • A sedative can become this if it is given in large doses
  • These drugs are regularly prescribed for insomnia and other sleep disorders and are habit forming

-Ex: Diphenhydramine, trazodone, and amitriptyline

A

Hypnotics

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3
Q

-Can act as either a sedative or a hypnotic depending on the dose

-At low doses, calm the CNS without inducing sleep

  • At high doses, calm the CNS to the point of causing sleep

Classified into three main groups: Barbiturates, Benzodiazepines, and miscellaneous drugs

A

Sedative- Hypnotics

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4
Q
  • Transient, reversible, and periodic state of rest in which there is a decrease in physical activity and consciousness

-Cyclic and repetitive

  • A persons response to sensory stimuli are markedly reduced during this
A

Sleep

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5
Q

Sleep research involves study of the patterns of sleep

  • Consist of two basic elements that occur cyclically: rapid eye movement(REM) and non rapid eye movement(non-REM)
A

Sleep Architecture

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6
Q

The prolonged sedative hypnotic use may reduce the cumulative amount of REM sleep

  • Can result in daytime fatigue because REM sleep provides a certain component of the “restfulness” of sleep
A

REM interference

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7
Q

This happens when a patient has an abnormally large amount of REM sleep, and often leading to frequent and vivid dreams

  • The discontinuance of a sedative hypnotic drug
A

REM rebound

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8
Q
  • These kinds of drugs were the most commonly prescribed sedative hypnotic drugs Favorable adverse effect profiles, efficacy, and safety when used appropriately

-Classified as either sedative-hypnotics or anxiolytics (depending on their primary use)

-Are prescription drugs only and are a schedule 4 controlled substances

Mechanism of Action
- Depresses CNS activity
- Affects the hypothalamic, thalamic, and limbic systems of the brain
- Thought to have gamma-aminobutyric acid receptors (GABA)
- Does not suppress rapid eye movement (REM)
- Does not increase metabolism of other drugs

Indications
- Used for: Sedation, Sleep induction, skeletal muscle relaxation, anxiety relief, anxiety related depression, treatment of acute seizure disorders, treatment of alcohol withdrawal, agitation relief, balanced anesthesia, moderate or conscious sedation
- Combined with anesthetics, analgesics, and neuromuscular blocking drugs in balanced anesthesia and also moderate sedation for their amnestic properties to reduce memory of painful procedures
-recommended for short term use

Contraindications
include: Drug allergy, narrow angle glaucoma, and pregnancy

Adverse Effects include mild and infrequent
-Headache
-Drowsiness
-Dizziness
Cognitive impairment
-Vertigo
-Lethargy
-Fall hazard for older adults
- “Hangover” effect or daytime sleepiness

Toxicity and Overdose includes the following:
- Somnolence
-Confusion
-Coma
-Diminished reflexes
- Does not cause hypertension and respiratory depression unless taken with other CNS depressants
-rarely results in death

Treatment is symptomatic and supportive
- Flumazenil Can be used to acutely reverse the sedative effects of this
- It antagonizes the action of this on the CNS by directly competing with the (blank) for binding at the receptors
- Flumazenil Is used in the cases of oral overdose or excessive intravenous sedation

Interactions
-Azole antifungals, verapamil, diltiazem, protease inhibitors, macrolide antibiotics, and grapefruit juice
- CNS depressants (Alcohol, opioids)
-Olanzapine
-Rifampin
-Herbal interactions
-Food- drug interactions
- Opioids

effects include: Reduced blood pressure, reduced respiratory rate, sedation, confusion, and diminished reflexes, and the supplements cava and Valerian
- black box warning

A

CNS depressants: Benzodiazepines

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9
Q
A

Nonbenzodiazepine drugs

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10
Q
  • These drugs are used to reduce the intensity of feelings of anxiety
  • These drugs can function along a continuum as a sedative and or hypnotic and or this depending on the dosage and patient sensitivity

-There are 5 benzodiazepines used as sedative-hypnotic drugs

A

Anxiolytic Drugs

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11
Q
  • These drugs functions like benzodiazepines but are chemically distinct

these drugs include: Ramelteon, Suvorexant (belsomra), and Tasimelteon (Hetlioz)

A

Miscellaneous Hypnotic drugs

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12
Q
  • A hypnotic drug not related to any other hypnotics

-Non- Benzodiazepine

  • Structurally similar to the hormone melatonin works as an agonist at melatonin receptors in the CNS

-Technically, it is not a CNS depressant; used as a hypnotic

  • Not classified as a controlled substance
  • Indicated for patients who have difficulty with sleep onset rather than sleep maintenance

-Has a shorter duration of action

-Contraindicated in cases of severe liver dysfunction

  • Avoid in patients receiving fluconazole or ketoconazole, both of which can impede its metabolism
A

Ramelteon

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13
Q
  • This drug is in a new class of drugs called selective orexin receptor antagonists
  • Neuropeptides involved in the regulation of the sleep-wake cycle
A

Suvorexant (Belsomra)

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14
Q
  • This drug is used only for disturbance of sleep wake cycle and patients who are totally blind

-Limited Use

A

Tasimelteon (Hetlioz)

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15
Q
  • These receptors are the primary inhibitor neurotransmitter of the brain and it serves to modulate CNS activity by inhibiting overstimulation
A

GABA receptors

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16
Q
  • This drug is used to treat benzodiazepine intoxication
A

Flumazenil

17
Q
  • An herbal product that is used to relieve anxiety, stress, and restlessness, and promote sleep
  • May cause temporary yellow skin discoloration with extended intake, visual disturbance, and the hepatotoxicity
  • Potential interactions with alcohol, barbiturates, and psychoactive drugs
  • Contra indicated in liver disease, alcoholism, and other conditions
  • Patients should not operate heavy machinery during use
A

Kava

18
Q
  • A herbal product that is used to relieve anxiety, restlessness, and insomnia

-May cause CNS depression, hepatotoxicity, nausea, vomiting, anorexia, restlessness, insomnia

-Many interactions, including with CNS depressants, MAOIs, phenytoin, warfarin, and alcohol

-Contraindicated in cardiac, renal, and liver disease

-Patients should not operate heavy machinery during use

A

Valerian

19
Q
  • This drug is the first clinically available benzodiazepine drug. It has varied uses
    -Treatment of anxiety
    -Procedural sedation and anesthesia adjunct
  • Anticonvulsant therapy
    -Skeletal muscle relaxation
  • This drug is available orally, rectally, and injectable
A

Diazepam (Valium)

20
Q
  • This drug is most commonly used preoperatively and for moderate sedation
  • Can cause amnesia and anxiolysis (reduce anxiety) as well as sedation
  • Normally administered by injection in adults
  • Liquid oral dosage form is also available for children
  • High alert medication
A

Midazolam

21
Q
  • This drug is an intermediate acting benzodiazepine (Most commonly used as a hypnotic)
  • One of the metabolites of diazepam
  • Normally induces sleep within 20 to 40 minutes
  • Has a long onset of action, so it is recommended that patients take it approximately 1 hour before going to bed
  • Still an effective hypnotic, it has been replaced by the newer drugs
A

Temazepam (Restoril)

22
Q
  • This drug is a Non-Benzodiazepine
  • The first hypnotic to be FDA approved for long term use
  • Designed to provide a full 8 hours of sleep
  • Considered a short- to intermediate acting agent
  • Patients should allot 8 hours of sleep time and should avoid taking hypnotics when they must awaken in less than 6 to 8 hours
A

Eszopiclone (Lunesta)

23
Q

This is thought to regulate circadian rhythms (day-night sleep cycles) in the body

A

Melatonin

24
Q
  • This drug is a short acting non benzodiazepine hypnotic

-Short half-life, lack of active metabolites, And has lower incidence of daytime sleepiness compared with benzodiazepine hypnotics

  • FDA recommends a max dose of 5 mg for women and 5 to 10 mg for men

Ambien CR- Is a longer acting form with two separate drug reservoirs

-Concerns about somnambulation (sleep-walking)

Only one of the two hypnotics to be FDA approved for long term use; the other is eszopiclone (Lunesta)

A

Zolpidem (Ambien)

25
Q
  • This drug class is hypothalamic neuropeptides that play a key role in promoting wakefulness and regulating the sleep wake cycle
A

Orexin A and B

26
Q
  • This drug is the first drug in a new class called orexin receptor antagonist

-Oral dual orexin receptor antagonist with a 12-hour half-life

-safety concerns: daytime somnolence and unconscious nighttime behaviors

-Adverse effects: Drowsiness, headache, dizziness, diarrhea, dry mouth, cough, and increased serum cholesterol

-Adverse side effects are commonly found in women

A

Suvorexant (Belsomra)

27
Q
  • These types of drugs were first introduced in 1903; were the standard drugs for insomnia and sedation
  • Chemically they are derivatives of barbituric acid
  • Only if you are commonly used today partially because of the safety and efficacy of benzodiazepines
  • Can produce many unwanted adverse effects
  • Physiologically habit forming and have a low therapeutic index

Mechanism of Action

  • CNS depressants that act primarily on the brainstem (reticular formation)

-Sedative and hypnotic effects are dose related, and they act by reducing the nerve impulses traveling to the cerebral cortex

  • By potentiating the action of GABA, nerve impulses traveling in the cereal cortex are inhibited
  • Raise the seizure threshold and can be used to treat seizures

Indications

-No longer recommended for sleep induction

-Ultrashort acting: Anesthesia for short surgical procedures, anesthesia induction, control of convulsions, reduction of intracranial pressure in neurologic patients

-Short acting: Sedation and control of convulsive conditions

-Intermediate acting: Sedation and control of convulsive conditions

-Long acting: Epileptic seizure prophylaxis

Contraindications

-Must not be taken if: Drug allergy, pregnancy, significant respiratory difficulties, severe kidney or liver disease

-Caution in older adults: Their sedative properties and increased fall risk

Adverse Effects

  • effects include: Drowsiness, lethargy, dizziness, hangover, and paradoxical restlessness or excitement

-Deprive people of REM sleep, which can result in agitation

  • Rebound phenomenon may occur which can cause sleep increase and nightmares often ensue
  • If this is recommended for older adults the usual dosage is reduced by half whenever possible

Toxicity and Overdose
- Overdose frequently leads to respiratory depression and subsequent respiratory arrest

  • Overdose produces CNS depression (sleep to coma and death)

-Can be therapeutic: Anesthesia induction, Uncontrollable seizures “phenobarbital coma”

Drug Interactions

  • Enzyme inducers which means that they increase metabolism of other drugs
  • Additive effects: Alcohol, Antihistamines, benzodiazepines, opioids, and tranquilizers
  • Drugs most likely to have marked interactions with these kinds of drugs include monoamine oxidase inhibitors (MAOIs), tricyclic antidepressants, anticoagulants, glucocorticoids, and oral contraceptives

-Inhibited metabolism: MAOIs prolong the effects of these drugs

-Increased metabolism: Reduces Anticoagulant response, leading to possible clot formation

  • Co administration of these drugs with oral contraceptives can result in accelerated metabolism of the contraceptive drug and possible unintended pregnancy
A

Barbiturates

28
Q
  • This drug is a short acting barbiturate
  • Used preoperatively to relieve anxiety and provide sedation
  • Also used occasionally to control status epilepticus
  • May be used to treat withdrawal symptoms in patients who are physically dependent on barbiturates or barbiturate hypnotics

-Available in oral, injectable, and rectal dosage forms

  • No longer used as a sedative hypnotic drug for insomnia
A

Pentobarbital (Nembutal)

29
Q
  • This drug is considered the Pro typical barbecue and is classified as a long-acting drug
  • Available in oral and injectable forms
  • Used for the following:
  • Prevention of generalized tonic- colonic seizures and febrile convulsions

-Hyperbilirubinemia in neonates

  • Raely used as a sedative

No longer recommended as a hypnotic

A

Phenobarbital

30
Q
  • Non-prescription sleeping aids often contain antihistamines, which have CNS depressant effect

-Ex: Doxylamine (Unisom) and Diphenhydramine (Sominex) and acetaminophen/ diphenhydramine (Extra strength Tylenol PM); melatonin

  • As with other CNS depressants, concurrent use of alcohol can cause respiratory depression or arrest
A

Over the Counter Hypnotics

31
Q
  • A group of compounds that act predominantly with the CNS to relieve pain associated with skeletal muscle spasms

-Known as Centrally acting
-CNS is the site of action
-Similar in structure and action to other CNS depressants

-Direct acting
-Act directly on skeletal muscle
- Closely resemble GABA

Indications

  • relief of painful musculoskeletal conditions
    -Muscle spasms
    -Management of spasticity of severe chronic disorders (multiple sclerosis, cerebral palsy)
    -IV dantrolene used for malignant hyperthermia
  • Works best when used along with physical therapy

Adverse Effects
- An extension of their effects on the CNS and skeletal muscles
- effects include: Euphoria, lightheadedness, dizziness, drowsiness, fatigue, confusion, and muscle weakness
- These adverse effects are generally short lived because patients grow tolerant to them overtime

Toxicity and Management of Overdose
- Primarily involve the CNS

  • No specific antidote or medication or reversal
  • Best treated with conservative supportive measures
  • If taken along with other CNS depressants
  • Adequate airway must be maintained
  • EKG monitoring
    -Administer fluids to avoid crystalluria

Interactions
-Caution with other CNS depressants such as Benzodiazepines, and alcohol

Mental confusion, anxiety, tremors, an additive hypoglycemic activity also have been reported with this combination. A dosage reduction and/or discontinuance of one or both drugs is recommended

A

Muscle Relaxants

32
Q

-Baclofen (Lioresal)
-Cyclobenzaprine (Flexeril)
- Dantrolene (Dantrium)
-Metaxalone (Skelaxin)
-Tizanidine (Zanaflex)
- Carisoprodol (Soma)
- Chlorzoxazone (Paraflex)
-Methocarbamol (Robaxin)

The two most commonly used drugs in this classification are Baclofen and Cyclobenzaprine

A

Common Muscle Relaxants

33
Q

When combining Carisoprodol, an opioid, and a benzodiazepine It is known as this. Combination produces a heroin like effect

A

The Holy Trinity

34
Q
  • This drug is available in both oral and injectable dosage forms. Injectable form is for use with an implantable this pump device
  • Used to treat chronic spastic muscular conditions
  • A test dose is administered to confirm a positive response
  • The injection is diluted before infusion. Oral and injectable doses are titrated to a desired response
A

Baclofen (Lioresal)

35
Q

-This drug is available in a five milligram and 10 milligram dose and an extended-release formulation (Amrix)

  • Centrally acting muscle relaxant that is structurally and pharmacologically related to the tricyclic depressants
  • Most commonly used muscle relaxer to reduce spasms after musculoskeletal injuries
  • Can cause marked sedation
A

Cyclobenzaprine (Flexeril)

Pharmacology (4 decks)

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