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Pharmacology > CNS > Flashcards

CNS Flashcards

1
Q

Anorexiant Use and Mode of Action

A

Short-term (8-12 weeks) drugs used for weight loss
Indicated for tx of morbid exogenous obesity

Mode of action: thought to stimulate the release of NE and/or dopamine from storage sites in nerve terminals in the lateral hypothalamic feeding center, thereby producing a decrease in appetite

Approved for those with a BMI of greater than or equal to 30 or for patients with BMI greater than or equal to 27 who have an obesity related condition such as HTN, type II diabetes, or dyslipidemia

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2
Q

-Anorexiant Pharmacokinetics and Pharmacotherapeutics

A

Lipid soluble, can cross blood-brain barrier
Metabolized by liver, excreted by kidneys; duration of action is 4-6 hours

Have risk of tolerance and dependence so avoid using in patients with hx of dependency
Contraindicated in patients who abuse cocaine, methamphetamine, etc.
Use of anorexiants should be limited to a maximum period of 6 months and discontinued at any sign of tolerance

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3
Q

Anorexiant ADRs

A

CNS overstimulation: agitation, confusion, insomnia dizziness, HTN, HA, palpitations, arrhythmias, dry mouth, N/V
Sudden w/drawal can cause w/drawal symptoms
Cautious use in patients with diabetes due to increased glucose uptake from skeletal muscles
Avoid use in patients with hx of cardiovascular disease

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4
Q

Anorexiant Drug Interactions

A

Careful use with serotonergic meds due to increased risk for serotonin syndrome
Avoid MAOIs due to increased risk of hypertensive crisis
Can cause lithium toxicity
Orlistat decreases level of levothyroxine and increases warfarin levels

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5
Q

Hydantoin Use and Pharmacodynamics

A

Anticonvulsant used for first-line tx for tonic-clonic & partial complex seizures

Pharmacodynamics: works by stabilizing neuronal membranes and decreasing seizure activity by increasing influx of sodium ions across membranes in motor cortex

Onset and duration varies

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6
Q

Hydantoin Pharmacokinetics

A

metabolized in liver: strong cytochrome P2C9 (CYP2C9) effects

Levels will increase with cimetidine, diazepam, acute alcohol intake, valproic acid, and allopurinol

Decreases effects with barbiturates, antacids, calcium, chronic alcohol use

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7
Q

Hydantoin Drug Interactions and ADRs

A

Concurrent administration causes decreased effect of carbamazepine, estrogens, acetaminophen, corticosteroids, levadopa, sulfonylureas, cardiac gylcosides

Many ADRs
Never give IV or IM in primary care setting
Watch patients with liver and renal disease closely
Phenytoin associated with hepatitis
Most Common ADRs:
Nystagmus, dizziness, pruritis, paresthesia, HA, somnolence, ataxia confusion, hypotension, tachycardia, constipation, n/v, anorexia, dry mouth, gingival hyperplasia, urinary retention, urine discoloration

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8
Q

Hydantoin Monitoring and Patient Education

A

Baseline lab values and plasma levels, along with TSH
Need to assess OTC drugs: ibuprofen, antacids
Pregnancy Category D- if pt. has to take it, add 400 IU folic acid daily
Has a Black Box warning for causing blood dyscrasias

Discuss risk factors for seizures, report ADRs, avoid driving if not seizure free for more than 1 year, oral hygiene

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9
Q

Carbamazepine Interactions and ADRs

A

Watch out for intake with grapefruit juice

ADRs:
Depression of bone marrow, liver damage, impairs thyroid function, drowsiness, dizziness, blurred vision, n/v, dry mouth, diplopia, HA

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10
Q

Carbamazepine Monitoring and Pt. Education

A

Baseline lab values: CBC, chemical panel, hepatic panel, TSH

Teach about symptoms of bone marrow depression (fatigue; pale skin, lips, & nail beds, faster HR, easy tiring w/ exertion, dizziness, SOB), careful use of medications, therapeutic dosing, kindling

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11
Q

Succinimide Use and Pharmacodynamics

A

Used for tx of absence seizures in children and adults

Suppresses seizures by delaying calcium influx into neurons
Decreases nerve impulses and transmission in the motor cortex
Absorbed in GI tract

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12
Q

Succinimide Pharmacokinetics and ADRs

A

Metabolized in liver

ADRs:
GI most common
CNS: somnolence, fatigue, ataxia
Agranulocytosis, aplastic anemia, granulocytopenia

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13
Q

Lamotrigine Use & Pharmacokinetics

A

Used in adjunctive tx of primary generalized tonic-clonic seizures and partial seizures in adults and children older than 2 years of age
Concurrent use with valproic acid, phenytoin

Metabolized in liver and kidneys

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14
Q

Lamotrigine ADRs and Pt. Education

A

ADRs:
GI- mostly n/v, constipation; somnolence, fatigue, dizziness, anxiety, insomnia, HA, amblyopia, nystagmus; dermatological- rashes

Patient Education:
Adherence, avoidance of alcohol, avoidance of OTC drugs, adequate hydration, reporting any new drugs, reporting ADRs
Discussion of risk factors that contribute to seizures; driving; controversy about discontinuing medications after a few years of being seizure free: neurologists to make decision

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15
Q

Rufinamide Use, Contraindications, ADRs, and Interactions

A

Adjunctive tx for Lennox-Gastaut Syndrome

Modulates the activity of sodium channels

Contraindicated in familial short QT syndrome

ADRs: increased suicide risk, DRESS (drug rash with eosinophilia & systemic symptoms)

Interactions: carbamazepine, phenobarbital, valproate

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16
Q

Tricyclic Antidepressants (TCA)- Uses & Pharmacodynamics

A

Imipramine (Tofranil)- Prototype: used for depression; can be used for nocturnal enuresis, intractable pain, anxiety disorders

Acts on neurotransmitters, serotonin, and NE, and histamine and acetylcholine

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17
Q

TCAs- Pharmacokinetics & ADRs

A

Have fairly long half-life of 6 to 18 hours
Liver metabolism strong CYP2D6

ADRs:
Paradoxical diaphoresis, causing anticholinergic effects, orthostatic hypotension, sedation, drowsiness

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18
Q

TCAs- Patient Education and Monitoring

A

Patient education:
Do not discontinue abruptly; avoid OTCs
Must let provider know if having MI, glaucoma

Monitoring:
Must report any chest pain
reassess patient after 2-4 weeks of starting medication: suicide, ADRs
Baseline EKG

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19
Q

Monoamine Oxidase Inhibitor (MAOIs) - Mechanism of Action

A

Inhibit monoamine oxidase, the enzyme that terminates the actions of neurotransmitters such as dopamine, NE, epinephrine, & serotonin

Have a low safety margin

Not a first-line drug

Have many drug-drug and food-drug interactions

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20
Q

MAOIs- ADRs, Pharmacodynamics, Pharmacokinetics

A

ADRs:
Orthostatic hypotension, HA, insomnia, diarrhea, hypertensive crisis when used with other antidepressants or sympathomimetic drugs or with drugs containing tyramine

Pharmacodynamics:
They inactivate the enzymes that metabolize NE, 5HT, dopamine
They prevent the breakdown of tyramine found in many foods

Pharmacokinetics:
There is a major first-pass effect of liver metabolism and most have CYP2D6 as a substrate
Quick onset: 1-2 weeks

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21
Q

Selective Serotonin Reuptake Inhibitors (SSRIs)- Pharmacodynamics & Pharmacokinetics

A

Pharmacodynamics:
All SSRIs have selective inhibitory effects on presynaptic serotonin reuptake and weak effects on NE and dopamine neuronal uptake

Pharmacokinetics:
Slow absorption, half-life: 26 hours, has extensive first-pass metabolism
- Fluoxetine half-life: 1-3 days and first metabolite 4 to 16 days
Liver metabolism may involve CYP2C19 and CYP2D6

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22
Q

SSRIs- ADRs, Patient Education, and Monitoring

A

ADRs:
CNS, GI, sexual dysfunction; serotonin syndrome

Patient Education:
Adherence, avoidance of alcohol, avoidance of OTC medications that stimulate, insomnia, or drowsiness, suicide ideation
Pregnancy: Category B, C, or D
Withdrawal symptoms if abruptly discontinued

Monitoring:
Never give more than 4 weeks on first prescription
Monitor target symptoms

23
Q

Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs)- Use & Pharmacodynamics

A

Used for major depressive disorder, GAD, neuropathy pain, fibromyalgia; not FDA approved for use in children

Considered “atypical antidepressants”

Pharmacodynamics:
inhibit reuptake of both NE and serotonin

24
Q

SNRIs- Pharmacokinetics & ADRs

A

Pharmacokinetics:
Half-life: 8-17 hours
Metabolized in liver via CYP1A2 and CYP2D6; forms multiple metabolites
Watch with abx: quinilones

ADRs:
HA, somnolence, dizziness, insomnia, fatigue, dry mouth, constipation, orthostatic hypotension, erectile dysfunction, ejaculation failure

25
Q

SNRIs- Patient Education and Monitoring

A

Patient Edcuation:
Adherence, suicide ideation, avoidance of OTCs

Monitoring:
May increase serum transamine levels: watch in patients with liver disease
Monitor suicide risk, activation of hypomanic or manic symptoms

26
Q

Atypical Antidepressants- MOA, PK, Contraindications

A

Buproprion (Wellbutrin, Zyban), and Mirtazapine (Remeron)

Exact Mechanism of Action unknown
- Mirtazapine is an antagonist of 5-HT2, 5-HT3, and histamine (H1) receptors

Pharmacokinetics:
Both extensively metabolized via CYP2D6

Contraindications:
Bupropion is contraindicated in seizure disorder

27
Q

Atypical Antidepressants- ADRs, Monitoring, Patient Education

A

ADRs:
Bupropion may cause insomnia
Mirtazapine causes drowsiness, greater at 15 mg/day than at 30 mg/day

Monitoring:
Depression and suicidal ideation

Patient Education:
Take Mirtazapine before bedtime because it may cause drowsiness

28
Q

Typical Antipsychotics- Pharmacodynamics

A

Phenothiazines: chlorpromazine (Thorazine)
Nonphenothiazine: Haloperidol (Haldol)

Pharmacodynamics:
Block dopamine receptors in the basal ganglia, hypothalamus, limbic system, and medulla
Side effects: parkinsonism, prolactin elevation, and extrapyramidal symptoms (EPS); concurrent therapy with anticholinergic

29
Q

Typical Antipsychotics- Contraindications & ADRs

A

Contraindications:
Narrow-angle glaucoma, bone marrow depression, and severe liver or cardiovascular disease
Black box: increased mortality in older adult patients

ADRs:
neuroleptic malignant syndrome (NMS), EPS, sedation, weight gain

30
Q

Typical Antipsychotics- Patient Education and Monitoring

A

Patient Education:
drug interactions, avoid sudden withdrawal, sun protection

Monitoring:
Abnormal involuntary movement scale (AIMS), prolactin levels

31
Q

Atypical Antipsychotics- Use and Contraindications

A

Use:
Block serotonin receptors in cortex

Contraindications:
Hepatic or renal disease

32
Q

Atypical Antipsychotics- ADRs, Patient Education, and Monitoring

A

ADRs:
Seizures, weight gain, diabetes, hyperprolactinemia, dizziness, orthostatic hypotension
Clozapine- fatal agranulocytosis

Patient Education:
ADRs; do not abruptly stop taking

Monitoring:
symptoms, ADRs

33
Q

Dopaminergics- MOAs

A

These drugs attempt to restore the functional balance of dopamine and acetylcholine in the corpus striatum of the brain

Tx of choice for Parkinson’s Disease

  • Amantadine (Symmetrel)
  • Bromocriptine (Parlodel)
  • Levodopa (L-Dopa, Larodopa); Carbidopa-levodopa (Sinemet)
  • Pramipexole (mirapex)
  • Ropinirole (Requip)
  • Pergolide (Permax)
  • Tolcapone (Tasmar)
34
Q

Dopaminergics- Pharmacodynamics & ADRs

A

PD:
restore dopamine in areas of the brain
May need up to 6 mos. to achieve maximum therapeutic effects

ADRs:
N/V, hallucinations, dizziness; tolcapone may cause hepatocellular injury

35
Q

Dopaminergics- Drug Interactions, Patient Education, & Monitoring

A

Many drug interactions

Patient education:
Avoidance of abrupt discontinuation
Drug interactions, TCAs, decrease effects, may increase effects of HTN drugs, avoid antacids

Monitoring:
Lab tests- hepatic panels

36
Q

Anxiolytics and Hypnotics- Benzodiazepines & Serotonergic Anxiolytics

A

Benzodiazepines: for anxiety and insomnia (category IV)

  • anxiety: lorazepam (ativan)
  • insomnia: flurazepam (dalmane), temezepam (restoril)

Serotonergic anxiolytics: Buspirone

  • Pharmacokinetics: reduced first-pass affect; has many metabolites; one has noradrenergic effects; NOT used with panic attacks
  • Takes up to 2 weeks for onset to occur and up to 6 weeks for maximum effect
37
Q

Anxiolytics & Hypnotics- Barbiturates Categories II to IV

A

Short-acting: pentobarbital (Nembutal), secobarbital (Seconal)

Intermediate-acting: amobarbital (Amytal), aprobarbital (Alurate), butabarbital sodium (Butisol)

Long-acting: mephobarbital (Mebaral), phenobarbital (Luminal)
- Half-life: in children 30 to 72 hours; in adults 50 to 150 hours

38
Q

Anxiolytics & Hypnotics- Precautions/Contraindications

A

Dependence, withdrawal symptoms (need to be tapered)

Contraindicated in pregnancy and geriatric patients

39
Q

Anxiolytics & Hypnotics- ADRs, Monitoring, Patient Education

A

ADRs:
CNS depression sedation

Monitoring:
Liver function if using long term

Patient Education:
Avoiding alcohol and CNS depressants, safety, driving concerns

40
Q

Serotonergic Anxiolytics- Pharmacokinetics, ADRs, Drug Interactions, Monitoring, Patient Education

A

Busprione

PK: take 1-2 weeks for onset of anxiolytic effects, up to 6 weeks for maximum effects

ADRs: few

Drug interactions: MAOIs, SSRIs may cause serotonin syndrome, atypical antipsychotics

Monitoring: None needed

PE: prolonged onset, drowsiness

41
Q

Barbiturates- Use, MOA, ADRs, Interactions, Monitoring

A

Limited to: preanesthesia sedation, short-term tx of insomnia, status epilepticus

CNS depressants; bing ot GABA receptors

Contraindications: alcohol, hx of depression or suicide attempts

ADRs: CNS depression, agitation, confusion, HA

Drug interactions: CNS depressants

Monitoring: therapeutic levels, narrow therapeutic range

42
Q

Sedative-Hypnotics- Use, Contraindications, ADRs, Patient Education

A

Insomnia
Benzodiazepine hypnotics
Nonbenzodiazepine hypnotics

Contraindications: pregnancy, children, older adults, long-term use

ADRs: somnolence, abnormal behaviors

Patient Education: avoid CNS depressants, take immediately before bedtime, and get 6-7 hours of sleep

43
Q

Mood Stabilizers- Lithium Carbonate (Lithobid, Eskalith): MOA, Half-life, Therapeutic index, ADRs

A

MOA- unknown
Absorbed in GI tract, has no protein-binding, NOT metabolized in liver, excreted by kidney

Long half-life: 15-36 hours; steady state: 5-7 days

Very narrow therapeutic index (0.6-1.5 mEq/L): monitor levels every 10-14 days after initiating, and then every 2-3 mos. thereafter

ADRs
narrow therapeutic index, toxicity, ECG changes

44
Q

Mood Stabilizers- Lithium Carbonate: Monitoring and Patient Education

A

Monitoring:
Blood levels every 14 days after starting, 14 days after dosage changes, and then every 3-6 months

Patient Education:
Maintain adequate salt intake

45
Q

Mood Stabilizers- Valproates: Pharmacodynamics, Pharmacokinetics, Contraindications

A

PD:
Blocks GABA

PK:
metabolized by CYP2C9, 2C19, and 2A6; possibly induces 2C9 and 2C19; and inhibits 2C9, 2D6, and 3A4

Contraindications: pregnancy category D

46
Q

Mood Stabilizers- Valproates: Interactions, Monitoring, Patient Education

A

Many drug interactions

Monitoring:
Monitor plasma levels every 3 months

Patient Education:
Bruising and delayed clotting

47
Q

Nonclassified Mood Stabilizers- Nonbenzdiazepines: ADRs, Patient Education

A

Lamotrigine (Lamictal), Gabapentin (Neurontin), and topiramate (topamax)

ADRs:
somnolence, dizziness, weight changes
topiramate has 1% chance of renal calculi

Patient Education: ADRs

48
Q

Muscle Relaxants & Antispasmodics: Centrally Acting & Direct Acting

A

Centrally acting:
baclofen (Lioresal), carisoprodol (Soma), chloroxazone (Paraflex, Parafon Forte), cyclobenzaprine (Flexeril), metaxalone (Skelaxin), methocarbamol (Robaxin), orphenadrine (Banflex, Norflex), and tizanidine (Zanaflex)

Direct acting:
dantrolene (Dantrium) and botulinum toxin type A (Botox)

49
Q

Centrally Acting Muscle Relaxants and Antispasmodics: MOA, Contraindications, ADRs, Interactions, Patient Education

A

MOA: exact action unknown

Contraindications: specific for each drug; all are contraindicated in pregnancy

ADRs: CNS sedation, respiratory depression; chloroxazone may be hepatotoxic

Drug interactions: additive sedation with CNS depressants

Patient Education: appropriate use, CNS sedation

50
Q

Direct-Acting Antispasmodics: Dantrolene & Botulinum toxin type A

A

Dantrolene: used to treat spasticity associated with upper neuron disorders

  • Contraindications in active liver disease
  • ADRs: CNS depression, confusion
  • Patient Education: titration schedule

Botulinum toxin type A: injected to provide localized reduction in muscle activity
- May spread from site of injection to mimic botulism; may require mechanical ventilation

51
Q

Opioids: Types, Pharmacodynamics, Pharmacokinetics

A

Morphine- prototype
- all opioids rated against morphine

Single agent products: oxycodone, morphine
Combination products: Vicodin, Percocet, Percodan, Tylenol with Codeine

PD: bind to opioid receptors in CNS

PK: vary

52
Q

Opioids: ADRs, Patient Education, Monitoring

A

ADRs:
CNS sedation, constipation, euphoria

Patient Education:
ADRs, drug interactions

Monitoring:
ADRs, withdrawal, refills

53
Q

Stimulants- Amphetamine: Pharmacodynamics, Contraindications, ADRs

A

PD:
CNS stimulation, reward centers

Contraindications:
Heart disease, HTN, pregnancy

ADRs:
Insomnia, weight loss, palpitations, HA

54
Q

Stimulants- Amphetamines: Patient Education, Monitoring; Nonamphetamine

A

Patient Education:
ADRs, drug interactions

Monitoring:
Monitor ADRs, amount of drug used, refills

Nonamphetamine
Atomoxetine (Strattera)

Pharmacology (25 decks)

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