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Pharm Exam 4 > Module 7 - Motion Disorders > Flashcards

Module 7 - Motion Disorders Flashcards

1
Q

What type of drug is Phenytoin (Dilantin) and what is its MOA?

A
  • Type: Anti-epileptic drug
  • MOA: Causes selective inhibition of sodium channels; it only causes a blockade of sodium channels in neurons that are hyperactive while leaving the healthy neurons unaffected.
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2
Q

What are the adverse affects associated with Phenytoin (Dilantin)?

A
  • Verry narrow therapeutic range (10-20mcg/mL)
  • Nystagmus is common
  • Gingival hyperplasia (Swelling, tenderness, and bleeding of the gums)
  • Hyperglycemia and glycosuria are due to inhibition of insulin secretion.
  • Rash or Stevens-Johnson syndrome
  • Teratogen, Preg. Cat. D
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3
Q

What are the indications for using Phenytoin (Dilantin)?

A
  • Is used to treat all major forms of epilepsy except absence seizures. Especially effective against tonic-clonic seizures.
  • Can be used for certain types of dysrhythmias.
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4
Q

What are the drug interactions associated with Phenytoin (Dilantin)?

A
  • Phenytoin stimulates synthesis of hepatic drug enzymes, it thus can decrease the effects of other drugs including Oral contraceptives, warfarin, glucocorticoids
  • Diazepam, isoniazid, cimetidine, alcohol, Valproic acid increase levels of Phenytoin
  • Carbamezepine, phenobarbitol, and alcohol (when used chornically) can decrease levels of Phenytoin.
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5
Q

What type of drug is Carbamazepine [Tegretol] and what is its MOA?

A
  • Type: Anticonvulsant
  • MOA: Suppresses high-frequency neuronal discharge in and around seizure foci. MOA appears to be the same as that of phenytoin.
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6
Q

What are the indications for using Carbamazepine [Tegretol]?

A
  • It is used in the treatment of manic patients resistant to lithium therapy
  • Affective against tonic-clonic, simple partial, and complex partial seizures
  • Provides symptomatic control in patients w/ Biopolar Disorder
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7
Q

What are the s/x of using Carbamazepine [Tegretol]?

A
  • It may cause sedation, confusion, and ataxia but adverse effects are often less than associated with lithium.
  • Hyponatremia has been associated with carbamazepine and oxcarbazepine.
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8
Q

What are the drug interactions associated with Carbamazepine [Tegretol]?

A
  • Carbamazepine induces hepatic drug-metabolizing enzymes and increases the rate at which ir and other drugs are inactivated
    • Such as oral contraceptives & warfarin
    • Decreased effects of phenytoin and phenobarbital
  • Grapefruit juice inhibits the metabolism of this drug and causes an increase in peak and through levels.
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9
Q

What are the adverse effects of Carbamazepine [Tegretol]?

A
  • Minimal effect on cognitive function, but may cause nystagmus, blurred vision, vertigo, and headache
  • Drug induced bone marrow suppresion can cause leukopenia, anemia, and thrombocytopenia
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10
Q

What type of drug is Ethosuximide [Zarontin] and what is its MOA?

A
  • Type: Succinimides
  • MOA: Little is known about the mechanism of action of ethosuximide but it probably involves calcium channels, reducing T-type currents. T-type calcium currents may be responsible for rhythmic cortical discharge of an absence attack. It does not inhibit voltage-gated sodium channels (like phenytoin) nor does it enhance postsynaptic actions of GABA (as with clonazepam). It “reduces spread of abnormal electrical activity in the brain.”
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11
Q

What are the indications for using Ethosuximide [Zarontin]?

A

Primary drug for the treatment of absence seizures, although valproic acid, clonazepam & lamotrigine are also useful.

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12
Q

What are the s/x associated with Ethosuximide [Zarontin]?

A
  • Ethosuximide is usually well tolerated.
  • Most common side effects are GI (nausea, vomiting, anorexia) and CNS (drowsiness [warn patient], lethargy, euphoria, dizziness, headache).
  • Aplastic anemia & abnormal liver function have been reported.
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13
Q

What is the MOA of Lamotrigine [Lamictal]?

A

Its mechanism is unknown but in animals it prevented seizure spread, supposedly by an effect on sodium channels stabilizing neuronal membranes (similar to phenytoin & carbamazepine). It also inhibits calcium channels which would account for its effectiveness in absence attacks

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14
Q

What are the indications for using Lamotrigine [Lamictal]?

A

It is used as adjunctive therapy in the treatment of partial seizures, generalized tonic-clonic, absence, or myoclonic seizures and in the treatment of bipolar disorder.

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15
Q

What are the drug interactions associated with Lamotrigine [Lamictal]?

A
  • Lamotrigine metabolism is affected by coadministration of anticonvulsant enzyme inducers (half-life reduced from 24 hours to 7 hours with coadministration of phenobarbital; phenytoin; carbamazepine)
  • & inhibitors (valproic acid, which increases half-life to 59 hours.).
  • Lamotrigine has been reported to increase carbamazepine epoxide levels and decrease valproic acid serum concentrations by 25%
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16
Q

What blackbox warnings are associated with Lamotrigine [Lamictal]?

A
  • Black box warning of serious skin rashes (including Stevens-Johnson Syndrome) requiring hospitalization. Patients develop skin rash usually within 2 to 8 weeks of initiation of therapy.
  • The incidence of severe, potentially life-threatening rash occurs more commonly in pediatric patients (1%) than adults (0.3%).
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17
Q

What are the s/x associated with Lamotrigine [Lamictal]?

A

dizziness, diplopia, ataxia, blurred vision, N/V, somnolence, headache & rash.

18
Q

What type of drug is Levodopa/carbidopa (Sinemet) and what is its MOA?

A

Type: Dopamine Enhancer / Anti-parkinson drug

MOA: It is the immediate metabolic precursor of dopamine and is metabolized to dopamine within the brain

19
Q

What are the s/x associated with Levodopa/carbidopa (Sinemet)?

A
  • Most common early in therapy are anorexia, nausea, and vomiting (80% of patients on levodopa; 20% of patients on Sinemet), caused by stimulation of medullary emetic center by dopamine.
  • Minimize by giving in divided doses with or immediately after meals. (Warning: high protein meals interfere with the transport of levodopa).
  • Abnormal involuntary dystonic movements (dyskinesia) are common in 50%-80% of patients after 1-4 months of treatment. They include faciolingual tics, grimacing, & rocking movements of arms, legs, or trunk
  • Behavioral disturbances, characterized by anxiety, depression, confusion and delirium, occur in 15% of patients taking levodopa. Elderly patients receiving levodopa & anticholinergic drugs are particularly vulnerable.
  • Urinary metabolites cause a false-positive test for ketoacidosis.
  • Can cause orthostatic hypotension in 30% of patients
20
Q

What are the drug interactions associated with associated with Levodopa/carbidopa (Sinemet)?

A
  • Antipsychotic drugs (e.g., phenothiazines) antagonize effects of dopamine. Levodopa should not be given to psychotic patients as it may exacerbate the mental disturbance. If psychosis occurs during therapy, some references suggest continuing therapy and give the patient an atypical antipsychotic (Zahodne LB CNS Spectrum 2008;13(3 Suppl 4): 26)
  • (2) Monoamine oxidase inhibitors (MAOI) may exaggerate peripheral & central effects of levodopa (hypertension; hyperpyrexia).
  • (3) Anticholinergic drugs act synergistically to improve certain symptoms of Parkinson’s but they also slow gastric emptying & decrease absorption of levodopa.
21
Q

What is the benefit of using levodopa + carbidopa vs either drug independently?

A

Concurrent administration of carbidopa with levodopa results in increased peripheral availability of levodopa and decreased peripheral dopamine, hence reducing many of the side effects resulting from plasma concentrations of dopamine

  • Reduces dose of levodopa 75%,
  • Nausea & vomiting are largely eliminated,
  • Cardiac effects are largely eliminated,
  • Levodopa serum concentrations are higher and half-life longer,
  • The effective levodopa dosage is achieved more rapidly, antagonism by pyridoxine is eliminated, and the
  • Percent of patients improved is higher.
22
Q

What type of drug is Benztropine [Cogentin] and what is its MOA?

A
  • Type: Anticholinergic drug
  • MOA: These agents by blocking acetylcholine receptors, blunting the effects of this excitatory neurotransmitter. They also may inhibit uptake of dopamine into neurons. ​
23
Q

What are the s/x associated with Benztropine [Cogentin]?

A
  • Side effects are mydriasis, cycloplegia, dry mouth, tachycardia, adynamic ileus, etc which occur in 30-50% of patients. Central side effects include confusion and agitation, memory loss, hallucinations, and drowsiness (not well tolerated by elderly subjects).
  • The diminished food intake and physical activity of the elderly patient plus the anticholinergic effect increases the risk of constipation and urinary retention.
  • As with other anticholinergics, they should not be used in patients with glaucoma, prostatic hyperplasia, or pyloric stenosis
24
Q

What type of drug is Levetiracetam [Keppra] and what is its MOA?

A

Type: Anti-epileptic Drug

MOA: Unclear MOA, however it does not bind to GABA receptors or any other known neurotransmitter

25
Q

What are the indications for using Levetiracetam [Keppra]?

A
  • indicated for treatment of myoclonic seizures in adults
  • partial-onset seizures in adults & children
  • primary generalized tonic-clonic seizures in adults and children.
  • Unlabeled uses include migraine and bipolar disorder.
26
Q

What are the drug interactions associated with Levetiracetam [Keppra]?

A

It is rapidly & completely absorbed and not affected by food. Metabolism is not mediated by hepatic P450 enzymes and is excreted largely (66%) unchanged in the urine.

Unlike many other AEDs, it does not interact with other drugs.

27
Q

What are the s/x associated with Levetiracetam [Keppra]?

A
  • Adverse effects are generally mild to moderate (drowsiness; asthenia [loss of strength]).
  • In contrast to other AEDs, Levetiracetam does not impair speech or other cognitive functions.
28
Q

What type of drug is Pramipexole [Mirapex] and what is its MOA?

A
  • Type: Dopamine Agonist
  • MOA: The precise mechanism of their action is unknown but they are direct dopamine receptor agonists. Given with levodopa, they may permit the dose of levodopa to be reduced and smooth out response fluctuations.​
29
Q

What are the indications for using Pramipexole [Mirapex]?

A
  • Treatment of Parkinson’s disease where they mimic the actions of dopamine.
  • Some authorities suggest these drugs are preferred to levodopa in younger patients.
  • Pramipexole, rotigotine, and ropinirole are also indicated for the treatment of restless legs syndrome.
30
Q

What are the s/x associated with Pramipexole [Mirapex]?

A
  • Primary side effects include nausea (minimize by taking with meals), dizziness, both somnolence & insomnia, dyspepsia, constipation, and dizziness, with hallucinations and low blood pressure occurring less often. However, they produce less dyskinesia than levodopa.
  • Warning about dangerous narcolepsy-like side effects called “sleep attacks,” - irresistible sleepiness that comes on without warning.
  • An increasingly recognized serious adverse effect of dopamine agonists is an impulse-control disorder, manifested by pathologic gambling, excessive shopping, binge eating, or hypersexuality
31
Q

What type of drug is Ropinirole [Requip] and what is it indicated for?

A
  • Type: Dopamine agonist
  • Indication: Restless leg syndrome (Gold Standard)
32
Q

What are the s/x of using Ropinirole [Requip]?

A

The most common adverse effects were nausea (40%), somnolence, vomiting, dizziness and fatigue.

Ropinirole is given 0.25 mg once daily 1 to 3 hours before bedtime.

33
Q

What type of drug is Diazepam [Valium] and what is its MOA?

A
  • Type: Benzodiazepine
  • MOA: It appears to enhance the efficiency of GABA transmission presynaptically on the motor neuron.​
34
Q

What are the indications for using Diazepam [Valium]?

A

indicated for both spasticity & acute muscle spasms. For relief of muscle spasms, 2 to 10 mg 3 or 4 times

35
Q

What type of drug is Pregabalin [Lyrica] and what is its MOA?

A
  • Type: Antiepileptic
  • MOA: It is unknown. It selectively binds to the (2) subunit of voltage-gated calcium channels.
36
Q

What are the indications for using Pregabalin [Lyrica]?

A
  • Pregabalin is approved for partial onset seizures and for the management of neuropathic pain including diabetic peripheral neuropathy, postherpetic neuralgia, neuropathic pain associated with spinal cord injury, and fibromyalgia.
  • It may be useful in anxiety disorders.
37
Q

What are the s/x associated with Pregabalin [Lyrica]?

A
  • Blurred vision, dizziness (38%), dry mouth, edema, somnolence (20%), headache and weight gain.
  • About 12% of patients reported euphoria, consequently, it is a DEA Schedule V.
38
Q

What type of drug is Dantrolene [Revonto] and what is its MOA?

A
  • Type: Muscle relaxant
  • MOA: reduces contraction of skeletal muscle by direct action on excitation-contraction coupling inside the skeletal muscle fibers apparently by decreasing the amount of calcium released from the sarcoplasmic reticulum. (Cardiac & smooth muscle are minimally depressed because these tissues have a different calcium channel)
39
Q

What are the indications for using Dantrolene [Revonto]?

A
  • It is useful (PO) in the reduction of spasticity (cerebral palsy, multiple sclerosis) but the muscle weakness makes it major utility in nonambulatory patients.
  • It is used in the treatment of malignant hyperthermia (IV) or to prevent the development of signs of malignant hyperthermia in susceptible patients (PO).
40
Q

What are the s/x associated with Dantrolene [Revonto]?

A
  • It has a serious potential to cause hepatotoxicity (Warning Box).
    • AST and ALT liver function tests should be done frequently.
  • The most common major side effect is muscle weakness.
  • Patients should be told to report abdominal pain, jaundiced sclera, dark urine or clay colored stools.
41
Q

What type of drug is Cyclobenzaprine [Flexeril] and what is its MOA?

A
  • Type: Centrally acting Muscle relaxant
  • MOA: Unclear
42
Q

What are the s/x associated with Cyclobenzaprine [Flexeril]?

A
  • CNS depression: Drowsiness, dizziness, and lightheadedness. Tell patients to not drive while taking this medication
  • This medication has significant anticholinergic properties (may cause dry mouth, blurred vision, photophobia, urinary retention, and constipation)

Pharm Exam 4 (3 decks)

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