Name: PAJARO, Lara Nicole F.

Section: 2NU08 Topic: CNS

Generic Classification Action Indication Contraindication Side effects Nsx

Name (Brand Action/ Responsibilities
Name)

CNS stimulant Amphetamine is a central Anaphylaxis, Hypotension Amphetamine is contraindicated in insomnia, headache, dry mouth, • Keep in mind that when symptoms of
nervous (CNS) system associated with septic shock, patients with hypersensitivity to tachycardia, increase in systolic ADHD occur with acute stress reactions,
Amphetamine stimulant that functions by Asthma, Cardiac resuscitation any component of the drug blood pressure, restlessness, treatment with amphetamines usually isn’t
increasing the amounts of formulation. Amphetamine is also and irritability. indicated.
dopamine, norepinephrine, contraindicated during or within 14 WARNING To prevent hypertensive crisis,
and serotonin (to a lesser days of MAOI therapy, e.g., don’t give amphetamine during or for up
Route & Dosage: to 14 days after MAO therapy.
extent) in the synaptic cleft phenelzine, due to the risk of
• Give first dose when patient awakens and
through a variety of ADHD: 5 to 40 mg daily divided hypertensive crisis. Additional
additional doses at 4- to 6-hour intervals.
mechanisms. Amphetamine from one to three doses - divided contraindications include • Be aware that 5 ml of oral solution contains
enters the presynaptic axon doses should be at 4 to 6-hour symptomatic cardiovascular 5 mg of dexamphetamine.
terminal through diffusion intervals. Doses exceeding 40 mg disease, advanced arteriosclerosis, • If patient has bothersome adverse reactions,
or uptake by the are rarely more effective. glaucoma, hyperthyroidism, severe such as insomnia and anorexia,
monoamine transporters Narcolepsy: 5 to 60 mg daily hypertension, agitated states, and a expect to decrease dosage. To minimize
DAT, NET, and SERT. Once divided from one to three doses; history of drug misuse. insomnia, administer drug earlier in day.
inside the presynaptic start with 10 mg each morning, • Be alert for evidence of long-term
terminal, amphetamine increasing dose by 10 mg daily amphetamine abuse, such as severe dermatoses,
increases the amounts of each week; divided doses should marked insomnia, irritability,
monoamine be at 4 to 6-hour intervals. hyperactivity, and personality changes. If
neurotransmitters in the Prolonged, high-dose use should patient suddenly stops drug after long-term,
be stopped. high-dose regimen, watch for
cytosol through the
extreme fatigue and depression.
inhibition of vesicular
monoamine transporter 2 Obesity (short-term treatment):
(VMAT2) as well as through 15 to 30 mg daily divided into • Instruct breast-feeding patient to avoid
disruption of the three doses, given 30 to 60 breast-feeding during amphetamine therapy
minutes before meals. because drug is excreted in breast milk.
electrochemical gradients
Discontinuation should be • Teach patient to take first dose on awakening
necessary for vesicular
tapered. Discontinue prolonged and subsequent doses at 4- to 6-hour
transporter function.
high-dose use. intervals. Tell him not to take last dose late
Amphetamine also inhibits in evening because insomnia may occur.
the metabolism of • Inform patient or caregiver that each 5 ml
monoamine of oral solution contains 5 mg of dexamphetamine.
neurotransmitters by Advise patient to use a calibrated
inhibiting monoamine measuring device for accurate dose.
oxidase (MAO). At the same • Urge patient to avoid hazardous activities
time, amphetamine until drug’s effects are known.
stimulates the intracellular • Advise patient not to take amphetamine
receptor TAAR1, which with acidic fruit juice because doing so
induces internalization or decreases drug absorption.
• Explain drug’s abuse potential, and caution
transporter reversal of DAT.
against altering dosage unless prescribed
The effects of TAAR1 on
DAT may also extend to NET
and SERT, although co-
localization of TAAR1 with
these two transporters has
only been indirectly
evidenced in studies thus
 far. The net result of this
activity is increased efflux of
dopamine into the synaptic
cleft and reuptake inhibition
in the synaptic cleft through
DAT internalization and
direct competition.

Sympathomimetic drug Theophylline competitively  Symptomatic relief or Hypersensitivity to dopamine,  Frequent: Headache,  History: Hypersensitivity to any xanthines; peptic ulcer,
blocks phosphodiesterase prevention of sulfites. Pheochromocytoma, Nausea, vomiting, active gastritis; status asthmaticus; cardiac arrhythmias,
Theophylline which increases cAMP bronchial asthma and ventricular fibrillation. Uncorrected abdominal pain, acute myocardial injury, CHF, cor pulmonale; severe
tissue concentrations reversible tachyarrhythmias. diarrhea, headache, hypertension; severe hypoxemia; renal or hepatic disease;
causing bronchodilatation, bronchospasm insomnia, dizziness, hyperthyroidism; pregnancy, lactation
diuresis, CNS and cardiac associated with anxiety, restlessness,  Physical: Skin color, texture, lesions; reflexes, bilateral grip
(100 mg, 125 mg, stimulation, and gastric acid chronic bronchitis and tremor, palpitations. strength, affect; P, auscultation, BP, perfusion; R,
200 mg, 250 mg, secretion. emphysema  Potentially adventitious sounds; bowel sounds, normal output;
300 mg tablets;
 Unlabeled use of 2 Fatal: Convulsions, frequency, voiding pattern, normal urinary output; ECG;
100 mg, 200 mg
mg/kg/day to maintain cardiac arrhythmias, EEG; LFTs, renal and thyroid function tests
capsules; 80
serum concentrations hypotension and
mg/15 mL, 150
between 3 and 5 sudden death after  Caution patient not to chew or crush enteric-coated timed-
mg/15 mL liquid; release preparations.
mcg/mL: Treatment of too rapid IV injection
100 mg, 200 mg,
apnea and bradycardia  Give immediate release, liquid dosage forms with food if GI
250 mg, 300 mg,
of prematurity effects occur.
450 mg, 500 mg,
600 mg  Do not give timed-release preparations with food; these
sustained-release should be given on an empty stomach, 1 hr before or 2 hr
tablets; 50 mg, 75 Route & Dosage: after meals.
mg, 100 mg, 125
mg, 200 mg, 250 Adult/Child: PO/IV Loading
 Advise patients that this drug should not be used during
mg, 260 mg, 300 Dose 5 mg/kg
pregnancy; using barrier contraceptives is recommended.
mg sustained- Adult: PO/IV Maintenance
release capsules; Dose* Nonsmoker, 0.4 mg/kg/h  WARNING: Monitor results of serum theophylline level
200 mg, 400 mg, [*IV by continuous infusion, PO determinations carefully, and reduce dosage if serum levels
800 mg injection) divided q6h (immediate release) exceed therapeutic range of 10–15 mcg/mL.
or q8–12h (sustained
release)]; Smoker, 0.6  Monitor carefully for clinical signs of adverse effects,
mg/kg/h; with CHF or particularly if serum theophylline levels are not available.
cirrhosis, 0.2 mg/kg/h
Child: PO/IV Maintenance  WARNING: Keep diazepam readily available to treat
Dose* 1–9 y, 0.8 mg/kg/h; 10–12 seizures.
y, 0.6 mg/kg/h
Infant: PO/IV Maintenance  Take this drug exactly as prescribed. If a timed-release
Dose* 2–6 mo, 0.4 mg/kg/h; 6– product is prescribed, take it on an empty stomach, 1 hour
11 mo, 0.7 mg/kg/h before or 2 hours after meals. Do not chew or crush timed-
Neonate: PO/IV Maintenance release preparations; it may be necessary for you to take
Dose* 0.13 mg/kg/h this drug around-the-clock for adequate control of asthma
attacks.
  Avoid excessive intake of coffee, tea, cocoa, cola
beverages, and chocolate. These contain theophylline-
related substances that may increase your side effects.

 Smoking cigarettes or other tobacco products may

markedly influence the effects of theophylline. It is
preferable not to smoke while you are taking this drug.
Notify your health care provider if you change your
smoking habits while you are taking this drug; it may be
necessary to change your drug dosage.

 Do not use this drug during pregnancy; using barrier

contraceptives is advised.
 You may experience these side effects: Nausea, loss of
appetite (take drug with food if taking immediate-release
or liquid dosage forms); difficulty sleeping, depression,
emotional lability.

 Report nausea, vomiting, severe GI pain, restlessness,

seizures, irregular heartbeat.

 Have frequent blood tests to monitor drug effects and

ensure safe and effective dosage

Barbiturate Depresses sensory cortex, Seizure control (maintenance), Hypersensitivity to Phenobarbital, Occasional (3%–1%):  Assess B/P, heart rate, respirations imme-diately
decreases motor activity, Status Epilepticus and other barbiturates, porphyria, Drowsiness. Rare (less than before administration. Hypnotic: Raise bed rails,
Phenobarbital alters cerebellar function. renal/hepatic impairment dyspnea or airway obstruction, use 1%): Confusion, paradoxical CNS provide environment conducive to sleep (back rub,
in nephritic pts (large doses), severe reactions (hyperactivity, anxiety quiet environment, low lighting). Seizures: Review
hepatic impairment. History of in children; excitement, history of seizure disorder (length, presence of auras,
sedative/hypnotic addiction. Intra- restlessness in elderly, generally
Elixir: 20 mg/5 LOC). Observe for recurrence of seizure activity.
Routes and Dosage: arterial or SQ administration.
mL. Oral noted during first 2 weeks of Initiate seizure precautions.
Solution: 20 mg/5 therapy, particularly in presence  Monitor CNS status, seizure activity, hepatic/renal
mL. Injection of uncontrolled pain). function, respiratory rate, heart rate, B/P. Monitor for
Solution: 65 Status Epilepticus therapeutic serum level. Neurologic assessments may
mg/mL, 130 IV: ADULTS, ELDERLY, CHILDREN: be inaccurate until drug has properly cleared the body.
mg/mL. Tablets: 15 mg/kg as a single dose. Therapeutic serum level: 10–40 mcg/ mL; toxic serum
15 mg, 30 mg, 60 CHILDREN: 15–20 mg/ kg level: greater than 40 mcg/mL.
mg, 100 mg. (Maximum: 1,000 mg) over 10  PATIENT/FAMILY TEACHING
min; may repeat with an  • Avoid alcohol, limit caffeine. • May be habit-forming.
additional 5–10 mg/ kg dose 10 • Do not discontinue abruptly. • May cause
min after loading dose. dizziness/drowsiness; avoid tasks that require
alertness, motor skills until response to drug is
Note: Maintenance dose usually established.
starts 12 hrs after loading dose.
PO, IV: ADULTS, ELDERLY: 2
mg/kg/day in divided doses.
ADOLESCENTS, CHIL- DREN 6 YRS
AND OLDER: 2–3 mg/kg/day in 1–
2 divided doses. CHILDREN 5 YRS
OR YOUNGER, INFANTS,
 NEONATES: 3–5 mg/ kg/day in 1–
2 divided doses.

Dosage in Renal/Hepatic
Impairment

No dose adjustment.

Diazepam Benzodiazepine Depresses all levels of CNS Anxiety, Anxiety Disorders, Hypersensitivity to diazepam. Acute IV route may produce pain, BASELINE ASSESSMENT
by enhancing action of Muscle spasm, spasticity/rigidity, narrow-angle glaucoma, untreated swelling, thrombophlebitis, Assess B/P, pulse, respirations immediately before administration.
gamma-aminobutyric acid alcohol withdrawal, status open-angle glaucoma, severe carpal tunnel syndrome. Abrupt Assess risk of drug abuse, misuse, drug-seeking behavior. Anxiety:
(GABA), a major inhibitory epilepticus, acute active seizures, respiratory depression, severe or too-rapid withdrawal may Assess autonomic response (cold, clammy hands; diaphoresis),
Injection, neurotransmitter in the Control of Increased Seizure hepatic insufficiency, sleep apnea result in pronounced rest- motor response (agitation, trembling, tension). Musculoskeletal
Solution: 5 brain. Activity (Breakthrough Seizures) syndrome, myasthenia gravis. lessness, irritability, insomnia, spasm: Record onset, type, location, duration of pain. Check for
mg/mL. Nasal: 5
in Pts With Refractory Epilepsy Children younger than 6 mos (oral). hand tremor, abdominal/muscle immobility, stiffness, swelling. Seizures: Review his- tory of seizure
mg/0.1 mL, 7.5
mg/0.1 mL, 10 Who Are on Stable Regimens of cramps, diaphoresis, vomiting, disorder (length, intensity, frequency, duration, LOC). Observe fre-
mg/0.1 mL. Oral Anticonvulsants, renal/hepatic seizures. Abrupt withdrawal in quently for recurrence of seizure activity. Assess for potential of
Concentrate: impairment pts with epilepsy may produce abuse/misuse (e.g., drug-seeking behavior, mental health
(DiazePAM Inten- increase in frequency/severity conditions, history of substance abuse).
sol): 5 mg/mL. of seizures. Overdose results in
Oral Solution: 5 drowsiness, confusion,
mg/5 mL. Rectal diminished reflexes, CNS
Gel: (Diastat): 2.5 INTERVENTION/EVALUATION
depression, coma. Antidote:
mg, 10 mg, 20 Flumazenil (see Appendix J for Monitor heart rate, respiratory rate, B/P, mental status. Assess
mg. Tablet:
dosage). children, elderly for paradoxical reaction, par- ticularly during
(Valium): 2 mg, 5
mg, 10 mg. early therapy. Evaluate for therapeutic response (decrease in
intensity/frequency of seizures; calm
Routes and Dosage:

Anxiety (Acute/Severe)
M, IV, PO: ADULTS: 2–10 mg q3–
6hrs PRN up to 40 mg/day based
on response and tolerability.

Anxiety Disorders

PO: Initially, 2–5 mg once or twice

daily. May gradually increase
based on response and
tolerability up to 40 mg/ day in 2–
4 divided doses.

Muscle spasm, spasticity/rigidity

PO: ADULTS: Initially,2mg twice

daily or 5 mg at bedtime. May
gradually increase up to 40–60
mg/day in 3–4 divided doses
based on response and
tolerability. ADOLESCENTS,
CHILDREN, INFANTS 6 MOS AND
OLDER: Initially, 1–2.5 mg 3–4
times daily. May gradually
increase as needed and tolerated.

Alcohol Withdrawal

IV, PO: ADULTS: 5–20 mg PRN

until appropriate sedation
achieved. Dose and frequency
determined by severity of
withdrawal symptoms.

Status Epilepticus
IV: ADULTS: 5–10 mg as a single
dose given at a maximum
infusion rate of 5 mg/ min. May
repeat in 3–5 min if seizures do
not subside. INFANTS, CHILDREN:
0.15–0.2 mg/kg over 2 min; may
repeat after 5–10 min.
Maximum: 10 mg/dose.

Acute Active Seizures

IV: ADULTS: 5–10 mg as a single

dose. May repeat at 3- to 5-min
intervals up to a total dose of 30
mg. Intranasal: 0.2 mg/kg as a
single dose. May repeat once
based on response and
tolerability after 4 or more hrs.
Maximum dose: 2 doses/episode.
Do not use for more than 1
episode q5days or more than 5
episodes/mo.

Control of Increased Seizure

Activity (Breakthrough Seizures)
in Pts With Refractory Epilepsy
Who Are on Stable Regimens of
Anticonvulsants
Note: Do not use gel for more
 than 5 epi- sodes/mo or more
than 1 episode q5days. PO:
ADULTS, ELDERLY: 2–10 mg 2–4
times/day.

Rectal gel: ADULTS, CHILDREN 12

YRS AND OLDER: 0.2–0.5 mg/kg;
may be repeated in 4–12 hrs.
CHILDREN 6–11 YRS: 0.3 mg/ kg;
may be repeated in 4–12 hrs.
Maxi- mum: 20 mg. CHILDREN 2–
5 YRS: 0.5 mg/ kg; may be
repeated in 4–12 hrs. Maxi-
mum: 20mg.

Dosage in Renal Impairment

Use caution.

Dosage in Hepatic Impairment

Use caution. Oral tablets

contraindicated in severe hepatic
impairment.

Anticonvulsant Stabilizes neuronal Status epilepticus, Focal Partial- Hypersensitivity to phenytoin, other Frequent: Drowsiness, BASELINE ASSESSMENT
membranes in motor Onset Seizures, Generalized- hydantoins. Concurrent use of lethargy, confusion, slurred Anticonvulsant: Review history of seizure disorder (intensity,
Phenytoin cortex. Decreases influx of Onset Seizures delavirdine. History of acute speech, irritability, gingival frequency, duration, LOC). Initiate seizure precautions. LFT, CBC
sodium during generation of phenytoin therapy–induced hyperplasia, hypersensitivity should be performed before beginning therapy and periodically
nerve impulses. hepatotoxicity. IV (additional): reaction (fever, rash, during therapy.
Second- and third-degree AV block, lymphadenopathy),
Capsules: 30 mg, Routes and Dosage: sinoatrial block, sinus brady- cardia, constipation, dizziness, nausea.
100 mg, 200 mg, Adams-Stokes syndrome. Occasional: Headache,
300 mg. Injection Status Epilepticus hirsutism, coarsening of facial INTERVENTION/EVALUATION
Solution: 50 features, insomnia, muscle
mg/mL. Sus- IV: ADULTS, ELDERLY, twitching. Repeat CBC 2 wks following initiation of therapy and 2 wks
pension, Oral: ADOLESCENTS: Loading dose: 20 following admin- istration of maintenance dose. Observe
125 mg/5 mL. mg/kg at maximum rate of 25–50 frequently for recurrence of seizure ac- tivity. Monitor ECG for
Tablets, mg/min. May repeat in 10 min cardiac arrhyth- mia. Assess for clinical improvement (decrease in
Chewable: 50 mg. after loading dose with dose of 5– intensity/frequency of sei- zures). Monitor for depression, suicidal
10 mg/kg. Maintenance: (IV, tendencies, unusual behavior. Monitor CBC with differential, renal
Oral): Initially, 4–7 mg/kg/day function, LFT, B/P (with IV use). Assist with ambulation if
(usual 300–400 mg/day) in 2–4 drowsiness, lethargy occurs. Monitor for therapeutic serum level
divided doses. INFANTS, (10–20 mcg/ mL). Therapeutic serum level: 10–20 mcg/mL; toxic
CHILDREN: Loading dose: 20 serum level: greater than 20 mcg/mL. Free unbound levels:
mg/kg in a single dose or divided
 doses. Maxi- Therapeutic: 1–2 mcg/mL; toxic: more than 2 mcg/mL.
mum:1,000mg/dose. May give
additional dose of 5–10 mg/kg
after loading dose. Maintenance:
PATIENT/FAMILY TEACHING
Initially, 5 mg/kg/day in divided
doses. Usual Range: 4–8 mg/kg/ • Pain may occur with IV injection. • To prevent gingival
day. Maximum daily dose: 300 hyperplasia (bleeding, tenderness, swelling of gums), maintain
mg/day. good oral hygiene, gum massage, regular dental visits. • Report
Focal Partial-Onset Seizures, sore throat, fever, glandular swelling, skin reaction (hema- tologic
Generalized-Onset Seizures toxicity). • Drowsiness usually diminishes with continued therapy.
PO: ADULTS, ELDERLY: Loading
Dose: 1 g divided into 3 doses
given at 2-hr inter- vals.
Maintenance (begins 24 hrs after
loading dose): Initially 100 mg 3
times/ day; adjust at no less than
7–10-day inter- vals. Usual dose:
100 mg 3–4 times/day up to 200
mg 3 times/day (may consider
300 mg once daily in pts
established on 100 mg 3
times/day). CHILDREN: Load- ing
dose: IV/PO: 15–20 mg/kg
divided into 3 doses and
administered q2–4h.
Maintenance: Initially, 5
mg/kg/day in 2–3 divided doses.
Adjust dose at 7- to 10-day
intervals. Usual range: 4–8 mg/
kg/day. Maximum: 300 mg/day.

Dosage in Renal/Hepatic
Impairment

No dose adjustment.

Bethanechol Parasympathomimetic Stimulates parasympathetic Nonobstructive Urinary Hypersensitivity to bethanechol. Occasional: Belching, changes in  Ensure patient has emptied bladder prior to
choline ester nervous system, increasing Retention, Neurogenic Bladder, Mechanical obstruction of GI/ GU vision, blurred vision, diarrhea, procedure.
bladder muscle tone and Renal/Hepatic impairment tract, GI or bladder wall instability, urinary urgency or frequency.  Monitor urine output. Palpate bladder for evidence of
causing contractions, which hyperthyroidism, asthma, peptic Rare: Dyspnea, chest tight- ness, urinary retention.
5mg,10mg,25mg,
initiates urination. Also ulcer disease, epilepsy, pronounced bronchospasm.  Report nausea, vomiting, diarrhea, diaphoresis,
50mg. tablets
stimulates gastric motility, bradycardia or hypotension, increased salivary secretions, irregular heartbeat,
increasing gastric tone, and parkinsonism, CAD, vasomotor muscle weakness, severe abdominal pain, difficulty
may restore peristalsis. instability, bladder neck breathing.
obstruction, spastic GI disturbances,
acute inflammatory lesions of the
GI tract, peritonitis, marked
vagotonia.
Gabapentin Anticonvulsants Unknown. Structurally Adjunctive treatment of partial Hypersensitivity to Gabapentin Frequent (19%–10%): Fatigue, BASELINE ASSESSMENT
related to GABA but doesn't seizures with or without drowsiness, dizziness, ataxia. Review history of seizure disorder (type, onset, intensity,
interact with GABA secondary generalization in Occasional (8%–3%): frequency, duration, LOC). Assess lo- cation, intensity of
receptors, isn't converted patients with epilepsy (excluding Nystagmus, tremor, diplopia, neuralgia/neuropathic pain. Question history of renal impairment.
Capsules: 100 mg, into GABA or GABA agonist, Gralise and Horizant), Adjunctive rhinitis, weight gain, peripheral
300 mg, 400 mg doesn't inhibit GABA treatment to control partial INTERVENTION/EVALUATION
edema.
Oral solution: 250 reuptake, and doesn't seizures in children (excluding
mg/5 mL prevent degradation. Gralise and Horizant), Moderate Provide safety measures as needed. Monitor seizure
Rare (less than 2%): Anxiety,
Tablets: 100 mg, to severe primary restless legs frequency/duration, renal function, weight, behavior in children.
dysarthria, memory loss,
300 mg, 400 mg, syndrome (Horizant), Monitor for signs/symptoms of depression, suicidal tendencies,
600 mg, 800 mg dyspepsia, pharyngitis, myalgia.
Postherpetic neuralgia other unusual behavior; hypersensitivity reaction.
Tablets (immediate-release),
(extended- Postherpetic neuralgia (Gralise) PATIENT/FAMILY TEACHING
release): 300 mg,
600 mg • Use only as prescribed; do not abruptly stop taking drug (may
Routes and Dosage:
Adjunctive Therapy for Seizure increase seizure frequency).
Control
• Avoid tasks that require alertness, motor skills until response to
PO: ADULTS, ELDERLY, CHILDREN
drug is established.
13 YRS AND OLDER: (Immediate-
Re- lease): Initially, 300 mg 3
• Avoid alcohol.
times/day. May titrate dosage.
Range: 900–1,800 mg/ day in 3 • Report suicidal ideation, depression, unusual behavioral changes
divided doses. Maximum: 3,600
(esp. with changes in dosage), worsening of seizure activity or loss
mg/day. CHILDREN 3–12 YRS:
of seizure control.
Initially, 10–15 mg/kg/day in 3
divided doses. May titrate up to
• Seek medical attention for allergic reactions including difficulty
25–35 mg/kg/day (for children 5–
breathing, coughing, wheezing, throat tightness, swelling of face
12 yrs) and 40 mg/kg/day (for
or tongue.
children 3–4 yrs). Maximum: 50
mg/kg/day.

Adjunctive Therapy for

Neuropathic Pain
PO: ADULTS, ELDERLY:
(Immediate-Re- lease): Initially,
100–300 mg 1–3 times/ day. May
increase up to 1,200 mg 3 times/
day. (Extended-Release): Initially,
300 mg at bedtime. May increase
up to target dose of 900–3,600
mg once daily.

Postherpetic Neuralgia
PO: ADULTS, ELDERLY:
(Immediate-Re- lease): 300 mg
once on day 1, 300 mg twice daily
on day 2, and 300 mg 3 times/
day on day 3 as needed. Range:
1,800– 3,600 mg/day. (Extended-
Release): 300 mg once on day 1;
600 mg once on day 2; 900 mg
 once daily on days 3–6; 1,200 mg
once daily on days 7–10; 1,500
mg once daily on days 11–14;
then 1,800 mg once daily.
(Horizant): 600 mg once daily in
AM for 3 days, then increase to
600 mg twice daily.
RLS
PO: ADULTS, ELDERLY:
(Horizant): 600 mg once daily at
about 5 PM.
Dosage in Renal Impairment
Dosage and frequency are
modified based on creatinine
clearance.
Dosage in Hepatic Impairment
No dose adjustment.

Levodopa- Dopamine precursor. Levodopa is converted to Parkinsonism, renal/hepatic Hypersensitivity to Frequent (80%–50%): BASELINE ASSESSMENT
Carbidopa Decarboxylase Dopamine in basal ganglia, impairment carbidopa/levodopa. Concurrent Involuntary movements of face, Assess symptoms of Parkinson’s disease (e.g., muscular rigidity,
inhibitor. increasing Dopamine con- use with MAOIs or use within 14 tongue, arms, upper body; pen rolling motion, gait disturbance, tremors), emotional state.
centration in brain, days. (Tablets only): Narrow-angle nausea/vomiting; anorexia. Receive full medication his- tory and screen for interactions.
inhibiting hyperactive glaucoma. Occasional: Depression, anxiety,
cholinergic activity. Route & Dosage: confusion, nervousness, urinary INTERVENTION/EVALUATION
retention, palpitations, dizziness,
Carbidopa prevents
Availability: Parkinsonism light-headedness, decreased ap-
peripheral breakdown of petite, blurred vision, constipation, Be alert to neurologic effects (headache, lethargy, mental
levodopa, making more PO: ADULTS, ELDERLY: dry mouth, flushed skin, headache, confusion, agitation). Monitor for evidence of dyskinesia (difficulty
levodopa available for (Immediate- Release Orally insomnia, diarrhea, unusual fatigue, with movement). Assess for clinical reversal of symptoms
transport into brain. Disintegrating Tablet): Initially, darkening of urine and sweat.
Enteral Rare: Hypertension, ulcer, hemolytic
(improvement of tremor of head and hands at rest, mask-like
25/100 mg 3 times/day. May in- anemia (marked by fatigue). facial ex- pression, shuffling gait, muscular rigidity). Monitor B/P
Suspension:
crease daily or every other day by (standing, sitting, supine).
(Duopa): 100-mL
1 tablet up to 200/2,000 mg daily.
cassette
containing 4.63 (Extended- Release): 50/200 mg PATIENT/FAMILY TEACHING
mg carbidopa and 2 times/day at least 6 hours
apart. Intervals between doses of • Avoid tasks that require alertness, motor skills until response to
20 mg levodopa
per mL. Tablets: Sinemet CR should be 4–8 hours drug is established.
(Immediate- while awake, with smaller doses
• Take with food to minimize GI upset.
Release at end of day if doses are not
[Sinemet]): 10 mg equal. May adjust q3days. Maxi-
carbidopa/100 mg mum: 8 tablets/day. (Rytary):
levodopa, 25 mg Initially, 23.75/95 mg 3 times/day • Effects may be delayed from several weeks to months.
carbidopa/100 mg for 3 days, then to 36.25/145 mg
levodopa, 25 mg 3 times/day. Frequency may be • May cause darkening of urine or sweat(not harmful).
carbidopa/250 mg increased to maximum of 5
levodopa. • Report any uncontrolled movement of face, eyelids, mouth,
times/day if needed and
Tablets: (Orally tongue, arms, hands, legs; mental changes; palpitations; severe or
tolerated. Maximum daily dose:
Disintegrating persistent nausea/vomiting; difficulty urinating.
612.5/2450 mg/day. (Enteral Sus-
Immediate-
pension): Maximum: 2000 mg (1 • Report exacerbations of asthma, underlying depression,
Release): 10 mg
carbidopa/100 mg container) over 16 hours through psychosis.
levodopa, 25 mg NJ or PEG tube via infusion pump.
carbidopa/100 mg Also take oral immediate-release
levodopa, 25 mg in evening after disconnecting
carbidopa/250 mg pump. Refer to manufacturer’s
levodopa. guidelines for morning dose,
continuous dose escalation,
titration instructions.

Dosage in Renal/Hepatic
Impairment

Use caution.

Baclofen Skeletal muscle Inhibits transmission of Spasticity, Intrathecal Dose, Renal Hypersensitivity to Baclofen Frequent (greater than 10%): BASELINE ASSESSMENT
relaxant monosynaptic or Impairment, Hepatic Impairment Transient drowsiness, asthenia, Record onset, type, location, duration of muscular spasm, pain.
polysynaptic reflexes at dizziness, nausea, vomiting. Check for immobility, stiffness, swelling.
spinal cord level possibly by Occasional (10%–2%): Head-
Intrathecal hyperpolarization of ache, paresthesia, constipation, INTERVENTION/EVALUATION
Injection primary afferent fiber Route & Dosage: anorexia, hypotension,
Solution: 500 terminals. confusion, nasal congestion. For pts on long-term therapy, BMP, LFT, CBC should be performed
mcg/ mL, 1,000 Spasticity Rare (less than 1%): Paradoxical periodically. Assess for paradoxical reaction. Observe for
mcg/mL, 2,000 PO: ADULTS, CHILDREN 12 YRS CNS excitement or restlessness, drowsiness, dizziness, ataxia. Assist with ambulation at all times.
mcg/mL. Oral AND OLDER: Initially, 5 mg 3 slurred speech, tremor, dry Evaluate for therapeutic response: decreased intensity of skeletal
Solution: times daily. May increase by 15 mouth, diarrhea, nocturia, muscle spasm, pain.
5mg/5mL.Tablets mg/day (5 mg/dose) at 3-day impotence.
: 5mg,10mg, 20 intervals until optimal response PATIENT/FAMILY TEACHING
mg. achieved. Range: 40–80 mg/day.
Maximum: 80 mg/day. ELDERLY: • Drowsiness usually diminishes with continued therapy.
Initially, 5 mg 2–3 times daily.
• Avoid tasks that require alertness, motor skills until response to
May gradually in- crease dosage.
drug is established.

• Do not abruptly withdraw medication after long- term therapy

Intrathecal Dose (may result in muscle rigidity, rebound spasticity, high fever,
altered mental status).
ADULTS, ELDERLY, CHILDREN 4
YRS AND OLDER: Initially, 50 mcg • Avoid alcohol, CNS depressants.
as screening dose (25 mcg in very
small pediatric pts) for 1 dose;
observe pt for 4–8 hrs for positive
response (decrease in muscle
tone and/ or frequency and/or
severity of spasm). If response is
inadequate, give 75 mcg 24h after
1st dose. If response is still
inadequate, give 100 mcg 24h
after 2nd dose. Initial pump dose:
give double screening dose
(unless efficacy of bolus
maintained greater than 8 hrs,
then screening dose). After 24h,
dose may be increased/de-
creased only once q24h until
satisfactory response.

Dosage in Renal Impairment

Use caution.

Dosage in Hepatic Impairment

No dose adjustment.