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Advanced Pharm-McNeese > CNS PART 1 > Flashcards

CNS PART 1 Flashcards

1
Q

NSAIDS for migraines

A

OTC, Rapid onset, useful in early migraines
-Marked lack of potency for most migraine headaches
-Must be taken early in the migraine attack; delayed administration of these drugs will be ineffective.

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2
Q

Acetaminophen

A

blocks the synthesis of prostaglandins in the brain
- Has analgesic effect for some migraine headaches if used early in the attack.
- Food does not inhibit oral absorption
- No “cross-sensitivity” with aspirin or the NSAIDs
Hepatotoxicity; especially in patients with pre-existing liver disease. Contraindicated in patients with severe liver dysfunction (i.e., cirrhosis)
- Precautions in patients with renal disease; does have some nephrotoxicity
- Must be taken early in the attack to be effective at all
-NSAIDS are more potent

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3
Q

Aspirin-Caffeine-Butalbital (Fiorinal)

A

-Very rapid onset of action; 15-30 minutes
-three drugs provides greater potency for migraine relief than the aspirin, NSAIDs, or acetaminophen do alone
-schedule III drug
-Contraindicated in pregnancy; barbiturates are teratogenic
-Precaution in pts with resp diseases
-Risk for addiction, causes hangover effect, contains ASA

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4
Q

Serotonin Agonists;
ergotamine (Ergomar)

A

long track record of success
-Rapid onset
-sup, sublingual, supp, inhaled
-Can be effective for mild, moderate, and some severe migraine headaches
-Can cause physical dependence- rebound headache
-Most effective if used early
- May cause peripheral vasospasm
- Contraindicated in patients with peripheral vascular disease, coronary occlusive disease, hypertension, or severe renal or hepatic disease
- no for pregos; they cause uterine contractions
- Contraindicated with several drugs;antifungals (such as itraconazole), erythromycin-type antibiotics and HIV protease inhibitors
- Precaution required in children

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5
Q

Serotonin Agonists;DIHYDROERGOTAMINE

A

-IV, IM ,spray for nausea
-rapid onset
-No risk of physical dependence or abuse
- Causes less nausea and peripheral vasospasm than ergotamine
- May be effective in some patients who do not respond to triptans
-Same contraindications as ergotamine
- Effectiveness decreases the later in the attack the drug is administered
- Not available orally
- Can cause -numbness of the fingers and toes, muscle aches, tachycardia or bradycardia, increase or decrease in blood pressure

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6
Q

Serotonin Agonists; SUMATRIPTAN and the other “Triptans”

A
  • Most effective of all the anti-migraine medications
  • Cerebral vasoconstriction is the predominant effect; less peripheral vasoconstriction
  • Less nausea
  • Still effective if administered late in the attack
  • Minimal CNS sedation;
    Can be used (with precaution) in pregnancy
    Use limited per 24 hrs
  • Commonly causes tightness in the chest, jaw, and neck; also causes a warm, tingling sensation
  • Contraindicated in coronary artery disease, ischemic heart disease, or angina
    -May cause dizziness, drowsiness and fatigue
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7
Q

Adjunctive Drugs for the Abortive Treatment of Migraine

A

Antimedics- metoclopramide (Reglan), prochlorperazine (Compazine), promethazine (Phenergan)
sedatives- butalbital (as in Fiorinal)
narcotics - meperidine (Demerol),codeine (various combinations), butorphanol (Stadol)

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8
Q

Prophylactic Drugs Used for Migraine

A

Tricyclic Antidepressants
- amitriptyline (Elavil)
Beta Blockers
- propranolol (Inderal)
- atenolol (Tenormin)
Anticonvulsants
- divalproex/valproate (Depakote)
- topiramate (Topamax)
SSRI’s
- fluoxetine (Prozac)
- sertraline (Zoloft)
Monoamine Oxidase Inhibitors
- phenelzine (Nardil)
Calcium Channel Blockers
- nimodipine (Nimotop)
- verapamil (Calan

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9
Q

Calcitonin Gene-Related Peptide (CGRP) Receptor Antagonists- new migraine med

A

Additional option for prophylaxis for those currently not controlled on more traditional prophylactic medications. (Aimovig, Ajovy, Emgality, Vyepti)
-Convenient dosing depending on the drug
-Ubrelvy offers another option for abortive therapy
Expensive
- Antibody development (humanized monoclonal antibody)
-Injection site reactions (for those that are not oral)

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10
Q

new Serotonin Agonists-lasmiditan (Reyvow)

A

Acute TREATMENT med-PO
- Can only take one dose (suppose migraine doesn’t go away?)

-Warnings for driving impairment, CNS depression, Serotonin syndrome, medication overuse headache.

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11
Q

PARKINSONS MEDS

A

Dopamine Agonists (including inhaled versions), Anticholinergics, Monoamine Oxidase B Inhibitors, COMT Inhibitors, and adenosine receptor antagonists.

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12
Q

DOPAMINE AGONIST DRUGS
For Parkinson’s Disease
amantadine (Symmetrel) (Gocovri) (Osmolex ER)
bromocriptine (Parlodel)
levodopa-carbidopa (Sinemet)
pramipexole (Mirapex)
ropinirole (Requip)

A

-They mimic actions of dopamine; replace in the brain what the brain is lacking which comes close to a specific correction of the basic pathophysiology.
-useful as monotherapy
-Most require BID to QID dosing
Most require frequent titration of doses; exact dose difficult to establish and it constantly changes
- Most are relatively expensive
- Commonly produce hallucinations

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13
Q

DOPAMINE AGONIST DRUGS
LEVODOPA-CARBIDOPA, LEVODOPA

A

Levodopa is metabolized into dopamine; carbidopa blocks an enzyme responsible for the peripheral (non-brain) metabolism of levodopa
-. Available in sustained-release
-Only small amounts actually enter the brain because of extensive peripheral metabolism before the drug can get across the blood brain barrier
-over 50% of patients) causes involuntary skeletal muscle movements
May cause orthostatic hypotension
- Can cause a variety of CNS adverse effects; inattention, memory loss, agitation, anxiety, confusion, depression, delirium, inappropriate or excessive sexual behavior, etc.
- Can cause visual problems; blurring, miosis, mydriasis, staring
-May cause excessive nasal discharge
- In general, has a narrow margin of safety.
- Contraindicated in glaucoma and in cases of suspected melanoma; levodopa can stimulate the growth rate of melanoma.

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14
Q

DOPAMINE AGONIST DRUGS-CONT LEVODOPA-CARBIDOPA DISADVANTAGES

A

less peripheral conversion before entry into the brain.
- Tolerance possible with continuous use
Commonly associated with an “On-Off” Phenomenon; relatively rapid fluctuations (within hours) of poor control of bradykinesia with period of dyskinesia (i.e., periods of muscle rigidity fluctuating with period of involuntary excessive muscle activity

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15
Q

DOPAMINE AGONIST DRUGS-BROMOCRIPTINE

A

Adjunctive benefit when given concurrently with levodopa-carbidopa; allows a reduction in the dose
- Prevents fluctuations in the patient’s response to levodopa-carbidopa
- May cause drowsiness and headache, and Nausea
- Possible hypotension (orthostatic);in older adults
- Not useful as monotherapy; only effective when used as an adjunct to levodopa - carbidopa

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16
Q

DOPAMINE AGONIST DRUGS-AMANTADINE

A

Stimulates the release of the body’s natural dopamine from the remaining dopamine-producing neurons; a direct correction of the basic pathophysiology of the disease.
- Dual therapeutic actions; useful as a dopamine agonist in Parkinson’s Disease and, by a different pharmacodynamic mechanism, as an anti-viral agent in influenza.
- No specific contraindications.
- Useful as initial monotherapy; can reduce bradykinesia effectively by itself in many early cases of the disease.
-Has anticholinergic adverse effects, lack potency,
- May cause dizziness, insomnia, ataxia, confusion
- Has a beneficial psychotomimetic effect; improves mood and sense of well-being in Parkinson’s patients
- Minimal adverse effects-Not metabolized

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17
Q

Anticholinergic Drugs: benztropine (Cogentin)
trihexyphenidyl (Artane)

A

decrease acetylcholine, to balance out the production of dopamine and acetylcholine.
Most useful for the treatment of Parkinsonian tremor; no effect on bradykinesia
- Has anticholinergic effect of producing dry mouth
- Inexpensive
- Useful as adjuncts to the dopamine agonist drugs
- Can be used as initial monotherapy
- Not effective for the bradykinesia or muscle rigidity of Parkinson’s Disease
- Use of these drugs is usually limited to early Parkinsonism; lack potency for severe, advanced cases.
- Contraindicated in glaucoma.

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18
Q

MAO-B Inhibitors-IRREVERSIBLY BOUND
rasagiline (Azilect)
selegiline (Eldepryl) (Deprenyl) (Zelapar)

A

-May delay the progression of Parkinson’s Disease
-Useful as an adjunct to the dopamine agonist drug
-Not effective as monotherapy
-Cause nausea
- May cause nervousness and anxiety; these are effects of the amphetamine metabolites
- May rarely cause abdominal pain, dry mouth, insomnia, hallucinations, dyskinesias, mood swings.

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19
Q

MAO-B Inhibitors – REVERSIBLY BOUND
safinamide (Xadago)

A

Specifically approved by the FDA for the adjunctive treatment with levodopa/carbidopa in patients with Parkinson’s disease experiencing OFF episodes.
-not effective as monotherapy.
- contraindicated in severe hepatic impairment and when administered with any other MAO inhibitor, opioids, (SNRIs), tricyclic, tetracyclic, or triazolopyridine antidepressants, cyclobenzaprine, methylphenidate, amphetamine derivatives, St. John’s Wort, and dextromethorpha

20
Q

COMT Inhibitors;
entacapone (Comtan)
tolcapone (Tasmar)

A
  • Not useful as monotherapy; only effective when given as an adjunct to levodopa - carbidopa.
    Tolcapone can cause liver failure; its use is limited to those patients who have exhausted other treatment options. If no benefit is evident within 3 weeks of initiating treatment the drug should be withdrawn.
  • Can cause diarrhea, orthostatic hypotension and hallucinations.
21
Q

inhaled Dopamine Agonists-Levodopa (Inbrija)

A

Specifically FDA approved for the intermittent treatment of OFF episodes of Parkinson’s disease in patients treated with carbidopa/levodopa (not approved as monotherapy)
-Need to take upwards of 5 times daily
-Not effective as monotherapy

22
Q

Adenosine Receptor Antagonists-istradefylline (Nourianz)

A

-Specifically FDA approved for adjunctive therapy with carbidopa/levodopa in patients with Parkinson’s disease experiencing OFF episodes.
-expensive $2,000 per month
-Can’t be used as monotherapy.

23
Q

Drugs Used to Treat Epilepsy

A

phenytoin (Dilantin)
carbamazepine (Tegretol)
oxcarbazepine (Trileptal) (Oxtellar XR)
ethosuximide (Zarontin)
divalproex sodium (Depakote)
valproate (Depakene)
lamotrigine (Lamictal)
phenobarbital (Luminal)
topiramate (Topamax)
rufinamide (Banzel)

24
Q

Phenytoin (Dilantin)

A

-Effective in partial and generalized tonic-clonic seizures
-Least sedating drug to treat seizures of any type.
- May cause a variety of CNS adverse reactions; dizziness, ataxia, slurred speech, confusion, insomnia, nystagmus.
- Can produce a rash
-Cannot be abruptly discontinued
- Totally ineffective for absence seizures
Long-term therapy can produce cosmetic problems; acne, hirsutism, coarsening of facial features, gingival hyperplasia
- Can produce lymphadenopathy
- Can cause hyperglycemia
- Teratogenic in pregnancy (Pregnancy category D)
- Narrow therapeutic window
-Baseline CBC, urinalysis and liver function tests should be complete prior to beginning therapy.

24
Q

Phenytoin (Dilantin)

A

-Effective in partial and generalized tonic-clonic seizures
-Least sedating drug to treat seizures of any type.

25
Q

Carbamazepine (Tegretol)

A

Useful for partial and generalized tonic-clonic seizures including mixed seizure patterns. [Note: Not effective in absence seizures]
- Useful in pain management of trigeminal neuralgia
- Does not produce sedation in normal dosages
- May also be used in treatment of bipolar disorder

26
Q

Disadvantages of Carbamazepine (Tegretol)

A
  • Commonly causes dizziness, diplopia, and ataxia;
  • Rare but serious cases of aplastic anemia and agranulocytosis; requires baseline hematological studies including white cell and platelet count before beginning therapy and periodically throughout treatment.
  • Can provoke nausea, vomiting, erythematous skin rash
  • May decrease the serum levels of other anticonvulsants since it is a P-450 enzyme inducer.
  • Cannot be abruptly discontinued
  • Classified as a Pregnancy Category D drug

-Boxed warning for serious dermatological reactions (Steven Johnson and toxic epidermal necrolysis). Particularly among the Asian population. Very strong association with the HLA-B*1202 gene. Patients in at risk populations should be screened.
-monitor drug levels

27
Q

Advantages of Oxcarbazepine

A

-Useful in partial onset seizures in adults and children.
-Useful in pain management of trigeminal neuralgia
-very few contraindications.
-no need to monitor serum drug levels

28
Q

Disadvantages of Oxcarbazepine

A

-Pregnancy Category C
-May decrease the efficacy of hormonal contraceptives containing ethinyestradiol and levonorgestrel.
-could cause hyponatremia in first few months (monitor sodium levels)
- Cannot be abruptly discontinued

29
Q

Ethosuximide (Zarontin)

A
  • Very effective in control of absence seizures
  • Very safe drug with a long track record of success
    -Can cause headache, nausea and vomiting
  • May cause agranulocytosis and thrombocytopenia (rare)
30
Q

Advantages- Valproate/Divalproex sodium (Depakene/Depakote)

A

-Can be used for both urgent control of seizures as well as for chronic suppressive therapy
- Useful for a wide variety of seizure types including generalized tonic-clonic, partial, myoclonic, and absence seizures
-Can be effective as monotherapy
- Generally safe drug
- May also be used in treatment of bipolar disorder with both immediate release and extended release formulations

31
Q

Disadvantages of Valproate/Divalproex

A
  • nausea, vomiting, abdominal pain and heartburn.
  • Can produce hepatotoxicity; contraindicated in patients with known liver disease. Monitoring of liver function studies required
  • Teratogenic in pregnancy (Pregnancy category D
  • Is a weak P-450 enzyme inhibitor; will increase the serum concentration and the potential toxicity of the other drugs.
  • Cannot be discontinued abruptly;
  • May produce increased appetite and weight gain, especially in female patients
32
Q
A
33
Q

Lamotrigine

A
  • Commonly causes dizziness and drowsiness
  • Can produce a life-threatening rash (Steven’s Johnson Syndrome or toxic epidermal necrolysis) administration with valproate can increase chances of rash
  • Cannot be abruptly withdrawn;
  • Immediate release: Not approved as monotherapy for patients under 16 years of age;combination therapy in children as young as 2
    -extended release: adjunctive therapy for primary generalized tonic-clonic seizures and partial-onset seizures with or without secondary generalization in patients aged 13 years and older.
  • Classified as a Pregnancy Category C drug but considered possibly teratogenic
34
Q

Phenobarbital (Luminal) Advantages

A

Can be used for therapy of all types of seizures (generalized and partial)
- Can be administered I.V. for emergency control of status epilepticus (generalized tonic-clonic seizures)
- Can be used in combination therapy with other anticonvulsants
- Useful in infants, especially for febrile seizures

35
Q

Disadvantages of Phenobarbital (Luminal)

A
  • Contraindicated in patients with severe liver disease and severe respiratory disease associated with dyspnea
  • Riak for tolerance and physical and dependence
  • Causes hepatic drug metabolizing enzyme induction; leads to increased metabolism of itself as well as other drugs metabolized by the same enzymes
  • Can produce paradoxical CNS excitation
  • teratogenic drug (Pregnancy category D drug)
  • Can produce severe respiratory depression
36
Q

Advantages of topiramate (Topamax)

A
  • initial monotherapy patients 2 years + with partial or generalized tonic-clonic seizures
  • Indicated as adjunctive therapy for adults and pediatric patients ages 2 - 16 years with partial onset seizures, or primary generalized tonic-clonic seizures as well as seizures associated with Lennox-Gastaut.
  • Indicated for adults for the prophylaxis of migraine headache
37
Q

Disadvantages of topiramate (Topamax)

A
  • Decreased serum bicarbonate levels as a manifestation of hyperchloremic, non-anion gap, metabolic acidosis. Measurement of baseline and periodic serum bicarbonate during topiramate treatment is recommended
  • Acute myopia
  • Decreased sweating and an elevation in body temperature above normal, especially in children
  • cognitive-related adverse effects, including confusion, psychomotor slowing,
    -Can cause depression or mood problems
    -Somnolence or fatigue
    -Pregnancy category D; increased incidence of cleft lip
38
Q

rufinamide (Banzel)

A

-indicated for adjunctive treatment of seizures associated with Lennox-Gastaut Syndrome in pediatric patients 1 year of age and older and in adults.
-although not approved, may have efficacy in focal seizures.
-relatively well tolerated with somnolence and vomiting as the most common adverse events.
-no monitoring of therapeutic levels.
-pregnancy category C

39
Q

INSOMNIA - Benzodiazepine Hypnotic Drugs

A

estazolam (Prosom)
flurazepam (Dalmane)
quazepam (Doral)
temazepam (Restoril)
triazolam (Halcion

40
Q

Advantages of Using the Benzodiazepine Drugs for Insomnia

A
  • little risk of respiratory depression
  • Overdose potential is very low
  • useful for sleep and anxiolysis
  • Most have a rapid onset of action -
  • Flurazepam and quazepam have rapid-onset and a long duration of action
  • Triazolam has rapid-onset and is slow-acting
  • Temazepam and estazolam have delayed-onset and intermediate duration of action
41
Q

Disadvantages of Using the Benzodiazepine Drugs for Insomnia

A
  • Risk of dependence and tolerance
    -should not exceed two to three weeks
    -peak effect may take 2-3 days
  • May cause allergic reaction
  • May cause complex sleep-related behaviors such as sleep-eating and sleep driving
  • May produce amnesic effects; are used as “date-rape” drugs because they create amnesia about the criminal act.
  • May produce “hang-over” effects;
  • Not recommended for children.
  • They are Pregnancy Category D or X
  • They are controlled substances.
  • Flurazepam =hang-over effect
  • Triazolam has prominent amnesic effects and prominent hang-over effects. It also commonly produces a paradoxical CNS stimulant effect manifested as hyperexcitability, insomnia, and even rage.
42
Q

Miscellaneous Hypnotic Drugs

A

eszopiclone (Lunesta)- only sedative hypnotic approved by the FDA for chronic use up to 6 months
ramelteon (Rozerem)
zaleplon (Sonata)
zolpidem (Ambien) (Edluar) (Intermezzo)

43
Q

Miscellaneous Hypnotic Drugs in Insomnia Pros and cons

A
  • Rapid onset and good duration
    -Can cause hangover effect
  • Can cause nausea and diarrhea
  • Patient should be advised to get at least 4 hours sleep and to use caution
  • May cause complex sleep-related behaviors
  • May cause allergic reactions
  • Additive CNS depression if combined with alcohol, benzodiazepines or over-the-counter sleeping aids
  • Overdose can cause possible severe CNS depression and hypotension
  • Not recommended for children or pregod
  • therapy should be limited to 1-2 wk
  • Controlled substances
44
Q

Ramelteon Cons

A

May cause elevation of prolactin levels
-Should not be taken in combination with fluvoxamine
- May cause complex sleep-related behaviors

Advanced Pharm-McNeese (5 decks)

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