DRUG STUDY: CNS STIMULANTS AND CNS DEPRESSANTS

Submitted by: Kate Submitted to: Mr.

Roque Barcellus Belisario
 DRUGS AFFECTING THE CNS: DRUG CLASSIFICATION
CNS STIMULANTS
CLASS DRUGS ACTIONS INDICATIONS
1. Amphetamines dextroamphetamine Promotes release of dopamine ➢ Narcolepsy
sulfate and norepinephrine from nerve ➢ ADHD
Dexedrine, terminals in the brain and, to a
ProCentra, Zenzedi lesser extent, the reuptake of
catecholamines.
lisdexamfetamine Increases the release of ➢ Adjust-a-dose (for all indications): For
dimesylate norepinephrine and dopamine patients with severe renal impairment
from nerve terminals and blocks (GFR of 15 mL to less than 30
their reuptake into the presynaptic mL/minute/1.73 m2), maximum dose is
neuron. 50 mg/day. For those with ESRD (GFR
less than 15 mL/minute/1.73 m2),
maximum dose is 30 mg/day.
➢ ADHD
➢ Moderate to severe binge eating
disorder
dextroamphetamine Promotes release of dopamine ➢ Narcolepsy
sulfate– and norepinephrine from nerve ➢ ADHD
dextroamphetamine terminals in the brain and, to a
saccharate– lesser extent, the reuptake of
amphetamine catecholamines.
aspartate–
amphetamine
sulfate,
 Adderall XR,
Mydayis
2. Anorexiants Phentermine Unknown. Phentermine is a ➢ Short-term adjunct in exogenous
hydrochloride sympathomimetic amine with obesity for patients with an initial
pharmacologic properties similar BMI of 30 kg/m2 or more, or of 27
to amphetamines. The kg/m2 or more in the presence of
mechanism of action in reducing other risk factors (e.g., controlled
appetite may be secondary to HTN, diabetes, hyperlipidemia)
CNS effects, including stimulation Adults and children age 17 and
of the hypothalamus to release older: 15 to 37.5 mg PO daily as a
norepinephrine. single dose before breakfast or 1 to 2
hours after breakfast. Or, 8 mg
(Lomaira) PO t.i.d. 30 minutes before
meals. Individualize dose to obtain
an adequate response with the
lowest effective dose.
➢ Adjust-a-dose: Maximum dose of
Adipex-P is 15 mg daily for patients
with severe renal impairment (eGFR
15 to 29 mL/minute/1.73 m2). To
achieve 15 mg of Adipex-P, split
37.5-mg scored tablets. Avoid use in
patients with eGFR less than 15
mL/minute/1.73 m2 or ESRD requiring
dialysis. Use caution when
administering Lomaira to patients
with renal
impairment.
3. Analeptics Modafinil Unknown. Similar to action of ➢ To improve wakefulness in patients
sympathomimetics, including with excessive daytime sleepiness
amphetamines, but drug is caused by narcolepsy, obstructive
structurally distinct from sleep apnea-hypopnea syndrome,
amphetamines and doesn't alter and shift-work sleep disorder
 release of dopamine or Adults: 200 mg PO daily, as a single
norepinephrine. dose in the morning. Patients with
shift-work sleep disorder should take
dose about 1 hour before the start of
their shift. Maximum dose is 400 mg
PO daily as a single dose.
➢ Adjust-a-dose: In patients with severe
hepatic impairment, give 100 mg PO
daily as a single dose in the morning.
Consider lower doses and close
monitoring in elderly patients.
CNS DEPRESSANTS
CLASS DRUGS ACTIONS INDICATIONS
1. Sedative- ALPRAZolam Unknown. Probably ➢ Adjust-a-dose (for all indications): For
hypnotics potentiates the effects of debilitated patients or those with advanced
(Anxiolytics) GABA, depresses the CNS, hepatic disease, usual first dose is 0.25 mg
and suppresses the spread of PO b.i.d. or t.i.d. For extended-release
seizure activity. tablets, 0.5 mg PO once daily.
➢ Anxiety
➢ Panic disorders
busPIRone May inhibit neuronal firing and ➢ Anxiety disorders
hydrochloride reduce serotonin turnover in
cortical, amygdaloid, and
septohippocampal tissue.
diazePAM Potentiates the effects of Adjust-a-dose (for all indications): For elderly or
GABA, depresses the CNS, debilitated patients, give 2 to 2.5 mg PO daily
and suppresses the spread of or b.i.d. initially; increase gradually as needed
seizure activity. and tolerated. Or, when using injection, use
lower doses (2 to 5 mg) and increase dosage
more gradually.
➢ Anxiety
➢ Acute alcohol withdrawal
➢ Before endoscopic procedures
➢ Muscle spasm
 ➢ Preoperative sedation
➢ Adjunctive treatment for seizure disorders
➢ Status epilepticus, severe recurrent seizures
➢ Patients on stable regimens of antiepileptic
drugs who need diazepam intermittently to
control bouts of increased seizure activity.
➢ Tetanus Adults
LORazepam Potentiates the effects of ➢ Anxiety
GABA, depresses the CNS, ➢ Insomnia from anxiety or transient situational
and suppresses the spread of stress
seizure activity. ➢ Preoperative sedation
➢ Status epilepticus
2. Analgesics Opioid analgesics Opioids act as agonists at ➢ Moderate to severe pain from acute and
codeine, fentaNYL specific opioid-receptor some chronic disorders; management of
citrate, binding sites in the CNS and pain severe enough to require daily, around-
HYDROmorphone other tissues, altering the-clock, long-term opioid treatment; dry,
hydrochloride, perception of pain. nonproductive cough (codeine);
meperidine management of opioid dependence
hydrochloride, (methadone); anesthesia support; sedation
methadone
hydrochloride,
morphine sulfate,
nalbuphine
hydrochloride,
oxyCODONE
hydrochloride,
oxyMORphone
hydrochloride,
pentazocine lactate
acetaminophen Thought to produce analgesia ➢ Mild pain or fever PO
(APAP, by inhibiting prostaglandin ➢ Adjust-a-dose: For adults with GFR of 10 to 50
paracetamol) and other substances that mL/minute/1.73 m2, give every 6 hours; if
sensitize pain receptors. Drug GFR is less than 10 mL/minute/1.73 m2, give
may relieve fever through every 8 hours. For patients receiving
 central action in the continuous renal replacement therapy, give
hypothalamic heat-regulating every 6 hours. For infants, children, and
center adolescents with GFR less than 10
mL/minute/1.73 m2, give every 8 hours. For
infants, children, and adolescents receiving
hemodialysis or peritoneal dialysis, give
every 8 hours.
➢ Rectal
➢ Mild to moderate pain; mild to moderate
pain with adjunctive opioid analgesics; fever
➢ Adjust-a-dose: Longer dosing intervals and a
reduced total daily dose may be warranted
in patients with CrCl of 30 mL/minute or less.
Buprenorphine, Unknown. Binds with opioid ➢ Maintenance treatment of opioid
buprenorphine receptors in the CNS, altering dependence in patients who have
hydrochloride perception of and emotional achieved and sustained prolonged clinical
response to pain. stability on low to moderate doses (8
mg/day or less) of a transmucosal
buprenorphine-containing product for 3
months or longer with no need for
supplemental dosing or adjustments
➢ Moderate to severe pain
➢ Opioid dependence
➢ Moderate to severe opioid use disorder in
patients who have initiated treatment with a
transmucosal buprenorphine-containing
product, followed by dosage adjustment for
a minimum of 7 days (Sublocade)
butorphanol tartrate May bind with opioid ➢ Moderate to severe pain
receptors in the CNS, altering ➢ Adjust-a-dose: For patients with renal or
perception of and emotional hepatic impairment, increase dosage
response to pain. interval to 6 to 8 hours and give 50% of the
normal dose. For elderly patients, give 1 mg
IM or 0.5 mg IV; wait 6 hours before
 repeating dose. For nasal use, 1 mg (1 spray
in one nostril). May give another 1 mg in 1.5
to 2 hours. Wait 6 hours before repeating
sequence.
➢ Labor for patients at full term; early labor
(without signs of fetal distress)
➢ Preoperative anesthesia or preanesthesia
➢ Adjunct to balanced anesthesia
codeine Codeine may bind with opioid ➢ Adjust-a-dose (for all indications): Consider
phosphate– receptors in the CNS, altering decreased dosage in patients with renal
acetaminophen perception and emotional impairment, elderly patients, and patients
response to pain. overly sensitive to effects of opioids. For
Acetaminophen is thought to patients with hepatic impairment, maximum
produce analgesia by total daily acetaminophen dose is 2,000 mg.
inhibiting prostaglandin and ➢ Mild to moderately severe pain
other substances that sensitize
pain receptors.
codeine sulfate May bind with opioid ➢ Mild to moderately severe pain
receptors in the CNS, altering
perception of and emotional
response to pain. Also
suppresses the cough reflex
by direct action on the cough
center in the medulla.
fentaNYL citrate, Binds with opioid receptors in ➢Adjunct to general anesthetic.
fentaNYL nasal the CNS, altering perception ➢Adjunct to regional anesthesia
spray, fentaNYL of and emotional response to ➢ To induce and maintain anesthesia
sublingual spray, pain. ➢Postoperative pain, restlessness, tachypnea,
fentaNYL and emergence delirium
transdermal system, ➢ Preoperative medication
fentaNYL ➢ To manage persistent, moderate to severe
transmucosal chronic pain in opioidtolerant patients who
require around-the-clock opioid analgesics
for an extended time
 ➢ To manage breakthrough cancer pain in
patients already receiving and tolerating an
opioid
➢ Switching from Actiq to Fentora to manage
breakthrough cancer pain in opioid-tolerant
patients
➢ Adjust-a-dose: For patients with renal or
hepatic impairment, use lowest possible
dose.
HYDROcodone Acts as a full agonist primarily ➢ Management of pain severe enough to
bitartrate at the mu opioid receptor, require daily, around-the-clock, long-term
binding to and activating opioid treatment and for which alternative
opioid receptors at various treatment options are inadequate
sites in the CNS to produce ➢ Adjust-a-dose: In patients with moderate
analgesia. renal impairment to ESRD, start with 50% of
the Hysingla ER or initial dose or with low
Zohydro ER dose, and monitor closely.
HYDROcodone Inhibits synthesis of ➢ Moderate to moderately severe pain
bitartrate– prostaglandins and binds to ➢ Adjust-a-dose: Adjust dosage according to
acetaminophen opiate receptors in CNS and severity of pain and patient response. Use a
peripherally blocks pain low initial dose in elderly patients and in
impulse generation; produces patients with hepatic or renal impairment;
antipyresis by direct action on monitor closely for adverse events, such as
hypothalamic heat-regulating respiratory depression and sedation. Total
center; causes cough acetaminophen intake shouldn't exceed
suppression by direct central 4,000 mg/day in adults and in children age
action in medulla; may 14 and older.
produce generalized CNS
depression.
HYDROmorphone Unknown. Binds with opioid ➢ Management of pain severe enough to
hydrochloride receptors in the CNS, altering require opioid treatment and for which
(dihydromorphinone perception of and emotional alternative treatment options are
hydrochloride) response to pain. Also inadequate
suppresses the cough reflex
 by direct action on the cough ➢ Adjust-a-dose: For elderly patients, use
center in the medulla. cautiously and reduce initial oral starting
dose. Initial IV starting dose for elderly or
debilitated patients should be 0.2 mg. For
those with moderate renal impairment,
reduce dose to 50% of usual starting dose.
For those with renal or hepatic impairment,
reduce dose to 25% to 50% of usual starting
dose of immediate-acting forms. For
extended-release forms, give patients with
moderate hepatic impairment 25% of usual
starting dose; give patients with moderate
renal impairment 50%, and patients with
severe renal impairment 25% of usual starting
dose. Use an alternative analgesic for those
with severe hepatic impairment.
meperidine Unknown. Binds with opioid ➢ Adjust-a-dose (for all indications): Reduce
hydrochloride receptors in the CNS, altering meperidine dosage by 25% to 50% when
(pethidine perception of and emotional administered with phenothiazines or other
hydrochloride) response to pain. tranquilizers because they potentiate the
action of meperidine. Use cautiously and
initiate at the lower end of the dosage
range in elderly patients and in those with
hepatic and renal impairment; if needed,
titrate dosage slowly.
➢ Moderate to severe pain that requires an
opioid analgesic and for which alternative
treatments are inadequate
➢ Preoperative analgesia
➢ Adjunct to anesthesia
➢ Obstetric analgesia
3. Anticonvulsants brivaracetam, Anticonvulsants include six Seizure disorders; acute, isolated seizures not
carBAMazepine, classes of drugs: selected caused by seizure disorders; status epilepticus;
cloBAZam, hydantoin derivatives, prevention of seizures after trauma or
clonazePAM, barbiturates, craniotomy; neuropathic pain; adjunctive
diazePAM, benzodiazepines, therapy in treatment of seizures
eslicarbazepine succinimides, iminostilbene
acetate, felbamate, derivatives (carbamazepine),
fosphenytoin and valproic/carboxylic acid
sodium, derivatives. Magnesium
gabapentin, sulfate is a miscellaneous
lacosamide, anticonvulsant. Some
lamoTRIgine, hydantoin derivatives and
levETIRAcetam, carbamazepine inhibit the
magnesium sulfate, spread of seizure activity in
OXcarbazepine, the motor cortex. Some
phenytoin sodium, barbiturates and succinimides
primidone, limit seizure activity by
rufinamide, increasing the threshold for
tiaGABine motor cortex stimuli. Selected
hydrochloride, benzodiazepines and
topiramate, valproic/carboxylic acid
valproate sodium, derivatives may increase
valproic acid, inhibition of GABA in brain
vigabatrin, neurons. Magnesium sulfate
zonisamide. interferes with the release of
acetylcholine at the
myoneural junction.
clonazePAM Unknown. Probably acts by ➢ Lennox-Gastaut syndrome, atypical
facilitating the effects of the absence seizures, akinetic and myoclonic
inhibitory neurotransmitter seizures
GABA. ➢ Panic disorder
brivaracetam Exact mechanism unknown. ➢ Adjunctive therapy or monotherapy for
Anticonvulsant effect may be partial-onset seizures in patients with epilepsy
related to affinity for synaptic ➢ Adjust-a-dose: Refer to manufacturer's
vesicle protein 2A in the brain. instructions for dosage adjustments in adults
and children with hepatic impairment. In
patients also taking rifampin, increase
 brivaracetam dosage by up to 100%
(double the dose).
carBAMazepine Thought to stabilize neuronal ➢ Generalized tonic-clonic and complex
membranes and limit seizure partial seizures, mixed seizure patterns
activity by either increasing ➢ Acute manic and mixed episodes
efflux or decreasing influx of associated with bipolar I disorder
sodium ions across cell ➢ Trigeminal neuralgia
membranes in the motor
cortex during generation of
nerve impulses.
fosphenytoin sodium May stabilize neuronal ➢ Adjust-a-dose (for all indications): Phenytoin
membranes and limit seizure clearance is decreased slightly in elderly
activity either by increasing patients; lower or less frequent dosing may
efflux or decreasing influx of be required.
sodium ions across cell ➢ Status epilepticus
membranes in the motor ➢ To prevent and treat seizures during
cortex during generation of neurosurgery (nonemergent loading or
nerve impulses. maintenance dosing)
➢ Traumatic brain injury; prevention of early
posttraumatic seizure (alternative agent)
gabapentin , Unknown. Structurally related ➢ Adjust-a-dose (for all indications): For
gabapentin to GABA but doesn't interact immediate-release formulation in patients
enacarbil with GABA receptors, isn't age 12 and older with CrCl of 30 to 59
converted into GABA or GABA mL/minute, give 400 to 1,400 mg daily
agonist, doesn't inhibit GABA divided into two doses. For CrCl of 15 to 29
reuptake, and doesn't prevent mL/minute, give 200 to 700 mg daily in a
degradation. single dose. For CrCl of less than 15
mL/minute, give 100 to 300 mg daily in a
single dose. Reduce daily dosage in
proportion to CrCl (patients with a CrCl of
7.5 mL/minute should receive half the daily
dosage of those with a CrCl of 15
mL/minute). For patients receiving
hemodialysis, maintenance dosage is based
 on estimates of CrCl. Give supplemental
dose of 125 to 350 mg after each 4 hours of
hemodialysis
➢ Adjunctive treatment of partial seizures with
or without secondary generalization in
patients with epilepsy (excluding Gralise and
Horizant)
➢ Adjunctive treatment to control partial
seizures in children (excluding Gralise and
Horizant)
➢ Moderate to severe primary restless legs
syndrome (Horizant)
➢ Postherpetic neuralgia (immediate-release)
➢ Postherpetic neuralgia (Gralise)
➢ Adjust-a-dose: For patients with reduced
renal function, initiate Gralise at a daily dose
of 300 mg. For patients with CrCl of 30 to 60
mL/minute, titrate dosage to 600 to 1,800 mg
daily as tolerated. Don't give Gralise to
patients with CrCl of less than 30 mL/minute
or to those receiving hemodialysis.
➢ Postherpetic neuralgia (Horizant)
➢ Adjust-a-dose: If CrCl is 30 to 59 mL/minute,
give 300 mg in the morning for 3 days; then
increase to 300 mg b.i.d. (may increase to
600 mg b.i.d. as needed). If CrCl is 15 to 29
mL/minute, give 300 mg in the morning on
days 1 and 3, then 300 mg daily in the
morning (increase to 300 mg b.i.d. if
needed). If CrCl is less than 15 mL/minute,
give 300 mg in the morning every other day
(increase to 300 mg daily in the morning if
needed). If CrCl is less than 15 mL/minute
and patient is on hemodialysis, give 300 mg
 after each dialysis treatment (increase to
600 mg after every dialysis treatment if
needed).
➢ Neuropathic pain (immediate-release)
lacosamide May selectively enhance slow ➢ Adjust-a-dose (for all indications): In patients
inactivation of sodium with mild or moderate hepatic impairment,
channels, stabilizing ESRD, or severe renal impairment (CrCl of 30
hyperexcitable neuronal mL/minute or less), reduce maximum
membranes and inhibiting recommended daily dosage by 25%.
repetitive neuronal firing Withhold drug in patients with severe
hepatic impairment. Dosage
supplementation of up to 50% should be
considered following a 4-hour hemodialysis
treatment. Reduce dosage as needed in
patients with hepatic or renal impairment
who are taking strong CYP3A4 and CYP2C9
inhibitors because of increased lacosamide
exposure.
➢ Adjunctive therapy for partial-onset seizures
➢ Monotherapy for partial-onset seizures
lamoTRIgine Inhibits release of glutamate ➢ Adjust-a-dose (for all indications): No
(an excitatory dosage adjustment is needed in patients
neurotransmitter) in the brain with mild hepatic impairment. Generally,
via action at voltage-sensitive reduce initial, escalation, and maintenance
sodium channels. Is a weak doses by approximately 25% in patients with
inhibitor of the 5-HT3 receptor. moderate and severe hepatic impairment
without ascites and 50% in patients with
severe hepatic impairment with ascites. May
adjust escalation and maintenance doses
according to clinical response. In patients
with renal impairment, base initial doses on
patients’ concomitant medications;
reduced maintenance doses may be
 effective for patients with significant renal
impairment. Use cautiously in such patients.
➢ Conversion to monotherapy using
extended-release formula in patients with
partial seizures who are receiving treatment
with a single enzyme-inducing AED
➢ Conversion to monotherapy using
extended-release formula in patients with
partial seizures who are receiving adjunctive
treatment with valproate
➢ Conversion to monotherapy using
extended-release formula in patients with
partial seizures who are receiving treatment
with a single drug other than an enzyme-
inducing AED or valproate
➢ Adjunctive treatment of partial seizures or
primary generalized tonicclonic seizures
caused by epilepsy or generalized seizures
of LennoxGastaut syndrome
➢ To convert patients from therapy with a
hepatic enzyme-inducing AED alone to
lamotrigine therapy
➢ To convert patients with partial seizures from
adjunctive therapy with valproate to
therapy with lamotrigine alone
➢ Bipolar disorder for maintenance treatment
to delay time to occurrence of mood
episodes (depression, mania, hypomania,
mixed episodes) in patients treated for
acute mood episodes with standard therapy