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424 Pharmacology > CNS & ANS > Flashcards

CNS & ANS Flashcards

1
Q

Anticonvulsants

Phenytoin (Dilantin)

Indications and MOA

A

Indications: first-line treatment for tonic-clonic and partial complex seizures

MOA: inhibit and stabilize electrical discharges in the motor cortex of the brain by affecting the influx of sodium ions during generation of nerve impulses

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2
Q

Anticonvulsants

Phenytoin (Dilantin)

Avoid, caution

A
  • Avoid: sinus bradycardia, second and third degree AV block and Stocks-Adams syndrome (syncope with heart block)
  • Caution: hypotension and myocardial insufficiency, elderly
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3
Q

What is one significant effect of rapid withdrawal from anticonvulsants/seizure medications?

A

Rebound status epilepticus can occur with sudden withdrawal

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4
Q

Anticonvulsants

Phenytoin (Dilantin)

Interactions

A
  • Increase level of phenytoin: cimetidine, diazepam, alcohol intake, valproic acid, allopurinol
  • Decrease level of phenytoin: barbiturates, antacids, calcium, chronic alcohol use
  • Phenytoin decreases the effects of: carbamazepine, estrogens, acetaminophen, corticosteroids, levodopa, sulfonylureas, cardiac glycosides
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5
Q

Anticonvulsants

Phenytoin (Dilantin)

Adverse fx (17)

A
  • Most common: Nystagmus, dizziness, pruritus, paresthesia, headache, somnolence, ataxia, confusion
  • Cardiovascular effects: hypotension, tachycardia
  • Gastrointestinal (GI) effects: n/v, anorexia, constipation, dry mouth, gingival hyperplasia
  • Genitourinary effects: urinary retention, urine discoloration
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6
Q

Anticonvulsants

Phenytoin (Dilantin)

Monitoring

A
  • baseline lab and plasma levels
  • TSH
  • drug levels
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7
Q

What should patients with seizure disorders keep in mind in regards to driving?

A

avoid driving if not seizure free for more than 1 year

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8
Q

Anticonvulsants

Phenytoin (Dilantin)

Patient education

A
  • keep up good oral hygiene
  • Monitor for phenytoin hypersensitivity syndrome = fever, skin rash, lymphadenopathy which occurs at 3-8 weeks of tx
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9
Q

Anticonvulsants

Carbamazepine (Tegretol)

Indications & MOA

A

Indications: focal and generalized onset seizures, bipolar disorder

MOA: exact unclear but thought to affect the sodium channels, slowing influx of sodium in the cortical neurons, which slows the spread of abnormal activity

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10
Q

Anticonvulsants

Carbamazepine (Tegretol)

Black box warning - in which population does this issue occur most frequently?

A

development of Stevens Johnson syndrome and toxic epidermal necrolysis in chinese patients - strong association with HLA-B 1202 allele variant in development of these conditions; blood dyscrasias; dermatologic toxicity

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11
Q

Anticonvulsants

Carbamazepine (Tegretol)

Caution

A

Caution: elderly

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12
Q

Anticonvulsants

Carbamazepine (Tegretol)

Drug interactions

A
  • grapefruit juice
  • Levels increased: propoxyphene, cimetidine, erythromycin, clarithromycin, verapamil, hydantoins
  • Levels decreased: beta blockers, warfarin, doxycycline, succinimides, haloperidol
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13
Q

Anticonvulsants

Carbamazepine (Tegretol)

Adverse fx (10)

A
  • Depression of bone marrow
  • Liver damage, impairs thyroid function
  • Drowsiness, dizziness, blurred vision, n/v, dry mouth, diplopia, headache (HA)
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14
Q

Anticonvulsants

Carbamazepine (Tegretol)

Symptoms of toxicity

A
  • hypertension
  • tachycardia
  • stupor
  • agitation
  • respiratory depression
  • nystagmus
  • urinary retention
  • seizures
  • coma
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15
Q

Anticonvulsants

Lamotrigine (Lamictal)

Indications & MOA

A
  • Indications: adjunctive treatment of partial seizures, primary generalized tonic-clonic seizures in adults and children 2+
    • Use with valproic acid and phenytoin
  • MOA: affects voltage-sensitive sodium channels and inhibits presynaptic release of glutamate and aspartate in the neuron
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16
Q

Anticonvulsants

Lamotrigine (Lamictal)

Interactions

A

Levels decreased: barbiturates, estrogens, phenytoin, mefloquine

Levels increased: alcohol, carbamazepine, CNS depressants, valproic acid

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17
Q

Anticonvulsants

Lamotrigine (Lamictal)

Black box warning

A

serious skin reactions

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18
Q

Anticonvulsants

Lamotrigine (Lamictal)

Adverse fx (13)

A
  • GI: n/v, constipation
  • cardiovascular: chest pain, peripheral edema
  • CNS: somnolence, fatigue, dizziness, anxiety, insomnia, headache, amblyopia, nystagmus
  • dermatological: rashes
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19
Q

Anticonvulsants

Lamotrigine (Lamictal)

Patient education

A
  • report any new onset of rash
  • avoid alcohol & OTC drugs
  • stay well hydrated
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20
Q

Anticonvulsants

Zonisamide (Zonegran)

Indications & MOA

A

Indications: partial seizures

MOA: blocks voltage-dependent sodium and chloride channels

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21
Q

Anticonvulsants

Zonisamide (Zonegran)

Avoid

A

Avoid: allergy to sulfa drugs

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22
Q

Anticonvulsants

Pregnancy/lactation and pediatric considerations

A
  • Pregnancy/lactation
    • Avoid – Phenytoin, Carbamazepine, Lamotrigine, zonisamide, valproic acid
    • Succinimides: Pregnancy ok with close monitoring, avoid in lactation
    • Gabapentin: Pregnancy/lactation: if benefits outweigh risks
    • Topiramate: Pregnancy: avoid; lactation: only if benefits outweigh the risks
    • Levetiracetam: Pregnancy: caution; lactation: avoid
  • Peds
    • All ages – phenytoin, carbamazepine
    • 1month+: levetiracetam
    • 3months+: topiramate
    • 2+: lamotrigine, valproic acid
    • 3+: succinimides, gabapentin
    • 16+: zonisamide
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23
Q

Anticonvulsants

Succinimides: Ethosuximide, Methsuximide

Indication & MOA

A

Indication: absence seizures

MOA: delays calcium influx into neurons; decrease nerve impulses and transmission in the motor cortex

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24
Q

Anticonvulsants

Succinimides: Ethosuximide, Methsuximide

Other considerations, symptoms of toxicity

A
  • Other considerations: Do not take with alcohol, decreases effectiveness of birth control
  • Narrow TI - toxicity = CNS depression, respiratory depression, acute nausea/vomiting
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25
Q

Which anticonvulsants should you be cautious of with patients with renal & hepatic impairment?

Renal impairment only?

A
  • phenytoin
  • carbamazepine
  • lamotrigine
  • zonisamide
  • succinimides
  • topiramate
  • Renal only: levetiracetam & gabapentin
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26
Q

Anticonvulsants

Succinimides: Ethosuximide, Methsuximide

Adverse fx (5)

A

GI most common

CNS: somnolence, fatigue, ataxia

Blood dyscrasias

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27
Q

Anticonvulsants

Valproic Acid (Depakote)

Indications & MOA

A

Indications: focal (partial) onset seizures, generalized onset seizures, focal onset impaired awareness and absence seizures

MOA: increases GABA availability, enhances the action of GABA, mimics its action at postsynaptic sites, blocks voltage gated sodium channels - results in suppression of high-frequency repetitive neuronal firing

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28
Q

Anticonvulsants

Valproic Acid (Depakote)

Caution, black box warning, sx of toxicity

A
  • Caution: elderly - BEERS
  • BBW: hepatotoxicity in severe pancreatitis
  • toxicity = CNS depression, confusion, jaundice
29
Q

Anticonvulsants

Valproic Acid (Depakote)

Adverse fx

A
  • CNS fx: headache, drowsiness, dizziness, tremor, visual disturbance, behavioral changes, SI, brain atrophy
  • GI fx: nausea, vomiting, weight gain,
  • Other: hypersensitivity reactions
30
Q

Anticonvulsants

Gabapentin

Indications & MOA

A

Indications: focal seizures

MOA: GABA analogue that binds to unknown receptors in the brain

31
Q

Anticonvulsants

Gabapentin

Pharmacokinetics, caution

A
  • Food increases absorption, not metabolized by the liver, excreted in the urine
  • Caution: elderly (BEERS), patients with substance abuse history
32
Q

Anticonvulsants

Gabapentin

Adverse fx

A
  • CNS fx: ataxia, paresthesia, dizziness, somnolence, difficulty concentrating, mood changes, SI
  • Other: weight loss, decreased sweating & hyperthermia
33
Q

Anticonvulsants

Levetiracetam (Keppra)

Indications & MOA

A

Indications: adjunct for partial onset seizures in children and adults

MOA: may inhibit burst firing without affecting normal neuronal excitability

34
Q

Anticonvulsants

Levetiracetam (Keppra)

What is a benefit of keppra over other anticonvulsants?

Caution, patient education

A
  • Fewer drug interactions
  • Caution: elderly
  • Patient education: somnolence, dizziness or balance issues when starting
35
Q

Anticonvulsants

Levetiracetam (Keppra)

Adverse fx

A
  • CNS fx:somnolence, dizziness, nervousness, mood disturbances, SI
  • Other: dermatologic reactions, blood dyscrasias
36
Q

Dopaminergics

Carbidopa-Levodopa (Sinemet)

Indication & MOA

A

Indication: Parkinson Disease

MOA

Levodopa: circulates in the plasma to the BBB where it crosses to be converted by enzymes to dopamine

Carbidopa: inhibits peripheral plasma breakdown of levodopa, thereby increasing the availability of levodopa at the BBB

37
Q

Dopaminergics

Carbidopa-Levodopa (Sinemet)

Avoid, caution, interactions, other considerations

A
  • Avoid: narrow-angle glaucoma, major psych dx, malignant melanoma
  • Caution: CVD, elderly - more sensitive to CNS fx
  • Interactions: TCAs decrease fx; may increase fx of HTN drugs; avoid with antacids
  • Other considerations: Risk for neuroleptic malignant syndrome if abruptly stopped; should be taken on a schedule without food
38
Q

Dopaminergics

Carbidopa-Levodopa (Sinemet)

Adverse fx

A
  • CNS fx: somnolence, dizziness, HA, depression, dyskinesia, insomnia, abnormal dreams, neuroleptic malignant syndrome, peripheral neuropathy
  • CV fx: orthostatic hypotension, HTN
  • GI fx: nausea, constipation, hepatocellular injury
39
Q

Muscle relaxants - general considerations

A
  • short term use, may be habit forming and sedating
  • may consider long-term use for MS or ALS; avoid alcohol use
  • Not for pregnant women - will relax the uterus
  • Use baclofen in caution with lactating women
40
Q

Muscle relaxants

Baclofen

Indications & MOA

A

Indications: severe muscle spasms with pain

MOA: inhibits transmission of both monosynaptic and polysynaptic reflex reflexes at the spinal cord level, possibly by hyperpolarization of primary afferent fiber terminals, which results in the relief of muscle spasticity

41
Q

Muscle relaxants

Baclofen

Caution, interaction, adverse fx

A
  • Caution: renal impairment, elderly (BEERS), seizure disorder
  • Interaction: additive sedation with CNS depressants
  • Adverse fx: drowsiness, confusion, HA, NV, hypotension, seizures
42
Q

Muscle relaxants

Cyclobenzaprine (Flexeril)

MOA

A

MOA: acts on monosynaptic and polysynaptic spinal reflexes; inhibits synaptic reflex arcs affecting the messages that are producing and maintaining the skeletal muscle spasm

43
Q

Muscle relaxants

Cyclobenzaprine (Flexeril)

Avoid, caution, peds, interaction

A
  • Avoid: hyperthyroidism, heart failure, arrythmias, heart block or conduction disturbances, acute recovery phase of MI
  • Caution: urinary retention, angle closure glaucoma, increased ocular pressure, hepatic impairment. elderly
  • Peds: 12+
  • Interaction: additive sedation with CNS depressants
44
Q

Muscle relaxants

Cyclobenzaprine (Flexeril)

Adverse fx

A
  • Anticholinergic fx: dry mouth, constipation, blurred vision
  • drowsiness, fatigue, N/V, hallucinations, serotonin syndrome
45
Q

Muscle relaxants

Tizanadine

MOA

A

MOA: centrally acting alpha-2 adrenergic agonist; presynaptic inhibition of motor neurons

46
Q

Muscle relaxants

Tizanadine

Avoid, caution, other considerations

A
  • Avoid: hepatic impairment
  • Caution: renal impairment, elderly
  • Other considerations: Do not abruptly stop - may cause rebound tachycardia; P450 drug
47
Q

Muscle relaxants

Tizanadine

Adverse fx

A
  • Anticholinergic fx: dry mouth,constipation
  • CV fx: hypotension, bradycardia
  • hepatotoxicity, anaphylaxis, angioedema, weakness, fatigue
48
Q

Cholinesterase inhibitors

Donepezil (Aricept), Rivastigmine (Exelon)

Indications & MOA

A

Indication: Alzheimers disease

MOA: reversibly and noncompetitively inhibits centrally active acetylcholinesterase which results in increased levels of acetylcholine available for synaptic transmission in the CNS - indirect cholinergic agonists

49
Q

Cholinesterase inhibitors

Donepezil (Aricept), Rivastigmine (Exelon)

S/s of toxicity, caution, Donepezil specific considerations

A
  • S/S of toxicity = constricted pupils, excessive salivation, diarrheaAvoid: with anticholinergic drugs
  • Caution: renal and hepatic impairment, seizure disorders
  • Donepezil - metabolized by the P450 system. risk of QT prolongation
50
Q

Cholinesterase inhibitors

Donepezil (Aricept), Rivastigmine (Exelon)

Adverse fx

A
  • CNS fx: dizziness, HA, agitation, insomnia, tremor, exacerbation of extrapyramidal side fx if patient has parkinson’s
  • GI fx: wt loss, N/V, diarrhea
  • Other: falls
51
Q

Cholinesterase inhibitors

Memantine (Namenda)

Indications & MOA

A
  • Indications: Often used in combo with aricept or exelon when alzheimers behavioral symptoms becomes more moderate to severe
  • MOA: noncompetitive antagonist at NMDA receptors
52
Q

Cholinesterase inhibitors

Memantine (Namenda)

Caution, adverse fx

A
  • Caution: CVD, renal impairment, seizure disorder
  • Adverse fx
    • CNS fx: confusion, dizziness, HA, somnolence
    • GI fx: constipation, diarrhea
    • CV fx: HTN
    • Other: hypersensitivity reaction
53
Q

Alpha-1 selective antagonists

Zosins - doxazosin, tamsulosin, terazosin

Indications & MOA

A
  • Indication: HTN, BPH, raynaud’s disease, migraines
  • MOA
    • HTN: competitively inhibits postsynaptic alpha-1 receptors which results in vasodilation
    • BPH: competitively inhibits postsynaptic alpha-1 receptors in prostatic stromal and bladder neck tissues - reduces sympathetic tone-induced urethral stricture causing BPH symptoms; relieve outflow obstruction
54
Q

Alpha-1 selective antagonists

Zosins - doxazosin, tamsulosin, terazosin

Avoid, caution, pregnancy/lactation, peds, patient education

A
  • Avoid: presence of volume depletion
  • Caution: heart failure, angina, recent MI, renal & hepatic impairment, elderly (BEERS)
    • Tamsulosin is an option that does not cause orthostatic hypotension
  • Pregnancy/lactation: avoid
  • Peds: limited data
  • Patient education: Risk for first-dose or reinitiation orthostatic hypotension - take at night
55
Q

Alpha-1 selective antagonists

Zosins - doxazosin, tamsulosin, terazosin

Adverse fx

A
  • Anticholinergic fx: fluid retention, blurred vision, dry mouth, constipation
  • CNS fx: HA, dizziness, fatigue
  • GU fx: impotence, urinary frequency, priapism
  • Other: allergic reactions, nasal congestion
56
Q

Alpha 2 agonists

Clonidine (Catapres)

Indications & MOA

A
  • Indications: HTN, ADHD
  • MOA
    • HTN: stimulates alpha-2 receptors in the brain stem, activating the inhibitory neuron, resulting in reduced sympathetic outflow from the CNS, decreasing peripheral resistance, heart rate, blood pressure and renal vascular resistance
    • ADHD: possibly regulates activity in the prefrontal cortex responsible for emotions, attention and behaviors
57
Q

Alpha 2 agonists

Clonidine (Catapres)

Avoid, caution, pregnancy, peds, patient education

A
  • Avoid: at risk or hx of bradycardia
  • Caution: renal impairment, cerebrovascular disease, severe coronary insufficiency, elderly (BEERS orthostatic hypotension, bradycardia)
  • Pregnancy: caution; lactation: avoid
  • Peds: approved
  • Patient education: do not stop abruptly - can lead to severe increase in blood pressure
58
Q

Alpha 2 agonists

Clonidine (Catapres)

Adverse fx

A

CNS fx: drowsiness, HA, fatigue, dizziness, nightmares

skin rash, dry mouth, bradycardia, constipation, impotence

59
Q

Alpha 2 agonists

Methyldopa

Indications & MOA

A

Indications: HTN

MOA: stimulates central alpha-2 receptors by methyldopa’s metabolite alpha-methylnorepinephrine which produces a decrease in sympathetic outflow to the heart kidneys and blood vessels

60
Q

Alpha 2 agonists

Methyldopa

Avoid, caution, pregnancy, peds, interactions

A
  • Avoid: at risk or history of bradycardia, active liver disease
  • Caution: severe coronary insufficiency, renal impairment, cerebrovascular disease, elderly
  • Pregnancy: compatible; lactation avoid
  • Peds: not recommended
  • Interactions: avoid with beta-blockers, clonidine
61
Q

Alpha 2 agonists

Methyldopa

Adverse fx

A
  • CV fx: edema, bradycardia, hypotension
  • GI: elevated LFTs, hemolytic anemia, hepatotoxicity
  • Other: sedation, skin rash, myalgias
62
Q

Beta-adrenergic antagonists (beta blockers)

Selective beta-blockers: metoprolol, atenolol

Indications & MOA

A

Indications: heart failure, HTN, a fib, angina, treatment post-acute MI

MOA: block beta-1 receptors at the SA node to decrease heart rate, decrease contractility in the atria and ventricles and conduction velocity and slow conduction at the AV node

63
Q

Beta-adrenergic antagonists (beta blockers) & combined alpha & beta adrenergic agonists and antagonists

Selective beta-blockers: metoprolol, atenolol, Non-selective beta blockers: Propranolol (Inderal), Carvedilol & Labetalol

Avoid, caution, pregnancy/lactation, peds, patient education

A
  • Avoid: bronchospasms, second or third degree AV block
    • Carvedilol, Labetolol: also severe hepatic impairment, NYHA Class IV HF
  • Caution: peripheral vascular disease, diabetes - will mask hypoglycemia s/s except diaphoresis, hyperlipidemia, elderly - bradycardia & orthostatic hypotension
  • Pregnancy/lactation: others preferred, contraindicated in first trimester
    • Labetolol: compatible after first trimester; caution in lactation
  • Peds: propranolol approved
  • Patient education: Do not abruptly withdraw
64
Q

Beta-adrenergic antagonists (beta blockers)

Selective beta-blockers: metoprolol, atenolol & Non-selective beta blockers: Propranolol (Inderal)

Adverse fx

A
  • CNS fx: fatigue, insomnia, depression, dizziness
  • CV fx: HTN, bradycardia
  • GU fx: impotence, decreased libido
  • Other: anaphylaxis, pruritis
65
Q

Beta-adrenergic antagonists (beta blockers)

Non-selective beta blockers: Propranolol (Inderal)

Indications & MOA

A

Indications: a. fib, essential tremor, migraine prophylaxis, HTN, stable angina, thyroid storm, anxiety

MOA: competitively block response to beta-1 and beta-2 stimulation resulting in decreased HR, myocardial contractility, BP and myocardial O2 demand

66
Q

Combined alpha & beta adrenergic agonists and antagonists

Carvedilol

Indications & MOA

A

Indications: HTN, HF with reduced EF, left ventricular dysfunction following MI

MOA: nonselective beta receptor blocker and alpha-1 receptor blocker - decreases BP and peripheral resistance to decrease myocardial O2 demand and lower cardiac workload

67
Q

Epinephrine

Indications & MOA

A

Indications: emergency treatment of type 1 allergic reaction, including anaphylaxis

MOA: decreases vasodilation and vascular permeability that occur during anaphylaxis; relaxes smooth muscles, relieves bronchospasm, wheezing, dyspnea, pruritis, angioedema, urticaria

68
Q

Epinephrine

Caution, pregnancy/lactation, peds

A

Caution: cardiac disease

Pregnancy/lactation: compatible

Peds: approved

69
Q

Epinephrine

Adverse fx

A
  • CNS fx: apprehensiveness, tremor, anxiety, HA, disorientation, weakness
  • CV fx: palpitations, angina, HTN
  • Other: alterations in blood sugar

424 Pharmacology (12 decks)

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