ANXIOLYTICS
sedative/hypnotics (e.g. benzodiazepine)
BUSPIRONE
Brand Name: Buspar
Generic Name: Buspirone
General Action: Anxiolytic
Mechanism of Action: Buspirone, an
azaspirodecanedione, is an anxioselective
drug w/ only little sedative effect but w/o
anticonvulsant and muscle relaxant
properties. It has high affinity for serotonin
(5-HT1A and 5-HT2), moderate affinity for
dopamine (D2), and no affinity for GABA
receptors.
Side Effects: CNS: dizziness, drowsiness,
headache, nervousness, insomnia, light-
headedness,
fatigue, numbness, excitement, confusion,
depression, anger, decreased concentration,
paresthesia, incoordination, tremor,
hostility. CV: tachycardia, nonspecific chest
pain.
EENT: blurred vision. GI: dry mouth,
nausea, diarrhea, abdominal distress,
constipation, vomiting. Musculoskeletal:
aches and pains. Skin: rash, sweating or
clamminess.
Drug-Drug Interaction: Increased serum
concentration when used w/ CYP3A4
enzyme inhibitors (e.g. erythromycin,
itraconazole, nefazodone, ritonavir,
diltiazem, verapamil). Decreased
metabolism and therapeutic effect when
used w/ CYP3A4 enzyme inducers (e.g.
rifampicin). Enhanced sedative effect w/
baclofen, lofexidine, nabilone,
antihistamines. May increase serum
concentration of haloperidol. Buspirone
does not exhibit cross-tolerance w/
and will not block symptoms of their
withdrawal, gradually withdraw such agents
prior to initiation of buspirone.
Potentially Fatal: Increased BP when taken
w/ MAOIs.
Time best given: May be taken with or
without food. Take consistently either
always w/ or always w/o meals.
ALPRAZOLAM
muscle cramps, muscle twitch.
Brand Name: Alprazolam Intensol, Apo-
Alpraz (CAN), Novo Alprazol (CAN),
Xanax, Xanax TS (CAN), Xanax
XR
Generic Name: Alprazolam
Pharmacologic class: Benzodiazepine
General Action: Anxiolytic, antipanic
Mechanism of Action: May increase
effects of gamma-aminobutyric acid
(GABA) and other inhibitory
neurotransmitters by binding to specific
benzodiazepine receptors in cortical and
limbic areas of the CNS. GABA inhibits
excitatory stimulation, which helps
control emotional behavior. The limbic
system contains many benzodiazepine
receptors, which may help explain drug’s
antianxiety effects.
Side Effects: CNS: insomnia, irritability,
dizziness, headache, anxiety, confusion,
drowsiness, lightheadedness, sedation,
somnolence, difficulty speaking, impaired
coordination, memory
impairment, fatigue, depression, suicide,
mental impairment, ataxia, paresthesia,
dyskinesia, hypoesthesia, lethargy, vertigo,
malaise, tremor, nervousness, restlessness,
agitation, nightmare, syncope, akathisia,
mania. CV: palpitations, chest pain,
hypotension. EENT: blurred vision, tinnitus,
allergic rhinitis, nasal congestion. GI:
diarrhea, dry mouth, constipation, nausea,
increased or decreased appetite, anorexia,
vomiting, dyspepsia, abdominal pain,
increased or decreased salivation. GU:
dysmenorrhea, sexual dysfunction,
premenstrual syndrome, difficulty urinating.
Metabolic: increased or decreased weight.
Musculoskeletal: arthralgia, myalgia,
arm or leg pain, back pain, muscle rigidity,
Respiratory: URI, dyspnea,
hyperventilation. Skin: pruritus, increased
sweating,
dermatitis. Other: influenza, injury,
emergence of anxiety between doses,
dependence,
feeling warm, increased or decreased libido.
Drug to Drug Interaction: amiodarone,
cyclosporine, diltiazem, ergotamine,
isoniazid, macrolide
antibiotics (clarithromycin, erythromycin),
nicardipine, nifedipine, paroxetine,
sertraline: Possible alteration in alprazolam
plasma levels antacids: Altered
alprazolam absorption rate
anticonvulsants; antidepressants;
antihistamines; other benzodiazepines, CNS
depressants, and psychotropics: Possibly
increased CNS depressant effects
carbamazepine: Decreased plasma level of
alprazolam and potential decreased
effectiveness
cimetidine, fluoxetine, oral contraceptives,
propoxyphene: Decreased alprazolam
elimination and increased effects
Time Best Given: Adults—At first, 0.5 to 1
milligram (mg) taken in the morning once a
day. Your doctor may increase your dose as
needed. However, the dose is usually not
more than 10 mg per day. Older adults—At
first, 0.5 mg taken in the morning once a
day.

CHLORDIAZEPOXIDE
Brand Name: Librium
Generic Name: chlordiazepoxide
Pharmacologic class: Benzodiazepine
General Action: Anxiolytic
Mechanism of Action: May potentiate the
effects of gamma-aminobutyric acid
(GABA) and other
inhibitory neurotransmitters by binding to
specific benzodiazepine receptors in cortical
and limbic areas of the CNS. By binding to
these receptors, chlordiazepoxide increases
GABA’s inhibitory effects and blocks
cortical and limbic arousal, which helps
control emotional behavior. It also helps
relieve symptoms of alcohol withdrawal by
causing CNS depression.
Side Effects: CNS: Ataxia, confusion,
depression, drowsiness, suicidal ideation
CV: ECG changes, hypotension,
GI: Elevated liver enzymes, hepatic
dysfunction, jaundice
HEME: Agranulocytosis
Other: Injection-site pain, redness, and
swelling
Drug to Drug Interaction: antacids:
Delayed absorption of chlordiazepoxide
cimetidine, disulfiram: Increased blood
chlordiazepoxide level
CNS depressants, opioids, other
benzodiazepines, sedating antihistamines,
tricyclic antidepressants: Increased risk of
sedation and somnolence and other
CNS effects
digoxin, phenytoin: Increased blood level
and risk of toxicity with digoxin and
phenytoin RESP: Bronchitis, cough, respiratory
levodopa: Decreased efficacy of levodopa’s depression
CLONAZEPAM Other: Allergic reaction
antiparkinsonian effects
Brand Name: Clonapam (CAN), Rivotril
opioids: Increased risk of significant
(CAN) Drug to Drug Interaction:
respiratory depression
Generic Name: clonazepam antianxiety drugs, antipyschotics
Pharmacologic class: Benzodiazepine (butyrophenone and thioxanthene classes),
Time Best Given: Initial: 50 to 100 mg,
General Action: Anticonvulsant, antipanic barbiturates, CNS depressants, MAO
usually given I.V. or I.M. Repeated in 2 to 4
hr inhibitors, narcotics, nonbarbiturate
Mechanism of Action: Although unknown, hypnotics, other benzodiazepines,
followed by individualized oral dosage if
drug is thought to prevent panic and phenothiazines, sedating antihistamines,
needed to control symptoms. I.V. given
seizures by potentiating tricyclic antidepressants: Increased risk of
slowly no faster than 50 mg/min.
the effects of gamma-aminobutyric acid CNS depression including significant
Maximum: 300 mg daily.
(GABA), which is an inhibitory sedation and somnolence
5 to 10 mg P.O. three or four times daily
neurotransmitter. This action is also thought carbamazepine, lamotrigine, phenobarbital,
several days before surgery; 50
to suppress the spread of seizure activity phenytoin: Possibly decreased
to 100 mg I.M. 1 hr before surgery
caused by seizure-producing foci in the plasma clonazepam levels with potential for
cortex, limbic, and thalamus structures. interference with its effectiveness
fluconazole: Possibly impaired clonazepam
Side Effects: CNS: Abnormal dreams, metabolism with potential for
aggression, agitation, amnesia, anxiety,
exaggerated concentrations and effects
apathy, ataxia,
opioids: Increased risk of severe respiratory
attention disturbance, confusion,
depersonalization, depression, dizziness, depression
phenytoin: Possibly altered plasma
drowsiness, emotional lability, excessive
dreaming, fatigue, hallucinations, concentrations of phenytoin
headache, hostility, hysteria, insomnia,
Time Best Given: Adults and children over
irritability, memory loss, nervousness,
nightmares, organic disinhibition, age 10. 1.5 mg daily in divided doses three
psychosis, reduced intellectual ability, sleep times daily.
disturbances, suicidal ideation Increased by 0.5 to 1 mg every 3 days, if
CV: Palpitations needed, until seizures are controlled.
EENT: Blurred vision, eyelid spasm,
increased salivation, loss of taste,
pharyngitis, rhinitis, sinusitis, yawning
GI: Abdominal pain, anorexia, constipation,
increased appetite
GU: Altered libido, difficult ejaculation,
dysmenorrhea, dysuria, enuresis,
impotence, nocturia, urine retention, UTI
HEME: Anemia, eosinophilia, leukopenia,
thrombocytopenia
MS: Dysarthria, myalgia

DIAZEPAM
Brand Name: Diastat, Diazepam Intensol,
Dizac, Valium
Generic Name: diazepam
Pharmacologic class: Benzodiazepine
General Action: Anticonvulsant,
anxiolytic, sedative-hypnotic, skeletal
muscle relaxant
Mechanism of Action: May potentiate
effects of gamma-aminobutyric acid
(GABA) and other
inhibitory neurotransmitters by binding to
specific benzodiazepine receptors in cortical
and limbic areas of CNS. GABA inhibits
excitatory stimulation, which helps control
emotional behavior. Limbic system contains
a dense area of benzodiazepine receptors,
which may explain drug’s antianxiety
effects.
Diazepam suppresses spread of seizure
activity caused by seizure-producing foci in
cortex, limbic, and thalamus structures.
Side Effects: CNS: drowsiness, dysarthria,
slurred speech, tremor, transient amnesia,
fatigue, ataxia,
headache, insomnia, paradoxical anxiety,
hallucinations, minor changes in EEG
patterns, pain, vertigo, confusion,
depression. CV: CV collapse, bradycardia,
hypotension. EENT: diplopia, blurred
vision, nystagmus. GI: nausea, constipation,
diarrhea with rectal form, dry mouth. GU:
incontinence, urine retention. Hematologic:
neutropenia. Hepatic: jaundice. Respiratory:
respiratory depression, apnea,
hiccups. Skin: rash, phlebitis at injection
site. Other: altered libido, physical or
psychological dependence.
Drug- Drug Interaction: antacids: Altered
rate of diazepam absorption
cimetidine, fluoxetine, fluvoxamine,
ketoconazole, omeprazole Decreased
diazepam metabolism, increased blood level
and risk of adverse effects including
prolonged sedation
CNS depressants including anesthetics,
anticonvulsants, antipsychotics,
anxiolytics, barbiturates, hypnotics, MAO
inhibitors, narcotics, phenothiazines,
sedatives including sedative antihistamines,
and other antidepressants:
Increased CNS depression and risk of falls
and fractures
opioids: Increased risk of severe respiratory
depression
phenytoin: Decreased metabolic elimination
of phenytoin, increased risk of
adverse reactions
Time Best Given: When using oral
solution, dilute dose just before giving with
liquid or semisolid food,
such as water, juices, soda or sodalike
beverages, applesauce, or pudding.
Adults: Depending on severity, 2 to 10 mg
PO b.i.d. to q.i.d. Or, 2 to 10 mg IM or IV.
May repeat in 3 to 4 hours if needed.
Children age 6 months and older: 1 to 2.5
mg PO t.i.d. or q.i.d., increased gradually, as
needed and tolerated.
nausea, thirst, vomiting
GU: Libido changes
HEME: Agranulocytosis, pancytopenia,
LORAZEPAM thrombocytopenia
RESP: Apnea, respiratory depression,
Brand Name: Ativan, Lorazepam Intensol,
worsening of obstructive pulmonary
Nu-Loraz (CAN)
disease or sleep apnea
Generic Name: lorazepam
SKIN: Diaphoresis
Pharmacologic class: Benzodiazepine
Other: Anaphylaxis, injection-site pain
General Action: Anxiolytic
(I.M.) or phlebitis (I.V.), physical and
psychological dependence, withdrawal
Mechanism of Action: May potentiate the
symptoms
effects of gamma-aminobutyric acid
(GABA) and other
Drug- Drug Interaction: aminophylline,
inhibitory neurotransmitters by binding to
theophylline: Possibly reduced sedative
specific benzodiazepine receptors in cortical
effects of lorazepam
and limbic areas of CNS. GABA inhibits
clozapine: Increased risk of ataxia, delirium,
excitatory stimulation, which
excessive salivation, hypotension,
helps control emotional behavior. Limbic
marked sedation, and respiratory arrest
system contains a highly dense area of
CNS depressants: Additive CNS depression,
benzodiazepine receptors, which may
potentially fatal respiratory
explain drug’s antianxiety effects. Also,
depression
lorazepam hyperpolarizes neuronal cells,
fentanyl: Possibly decreased therapeutic
thereby interfering with their ability to
effects of fentanyl
generate seizures.
probenecid, valproate: Possibly increased
therapeutic and adverse effects of lorazepam
Side Effects: CNS: Amnesia, anxiety, other benzodiazepines, sedating
ataxia, coma, confusion, delusions, antihistamines, opioids, tricyclic
depression, antidepressants: Increased risk of profound
dizziness, drowsiness, euphoria, respiratory depression, sedation, and
extrapyramidal symptoms, fatigue, somnolence
headache,
hypokinesia, irritability, malaise, Time Best Given: 2 to 4 mg at bedtime
nervousness, seizures, slurred speech,
suicidal
ideation, tremor, unsteadiness, vertigo
CV: Chest pain, palpitations, tachycardia
EENT: Blurred vision, diplopia, dry mouth,
increased salivation, photophobia
ENDO: Syndrome of inappropriate ADH
GI: Abdominal pain, constipation, diarrhea,
elevated liver enzymes, jaundice,
 Potentially Fatal: Increased sleep duration
Time Best Given: Hypnotic and CNS depression w/ Na oxybate.
Adult: 65-200 mg via IM inj (should not
exceed 5 mL at any single site) or IV inj Time Best Given: Phenobarbital is given by
AMOBARBITAL (should not exceed 50 mg/min) at bedtime. mouth in the form of a tablet, capsule, liquid
Max: 1,000 mg as a single dose. May be PENTOBARBITAL solution, paste, or chewable. It may be
Brand Name: Amytal Sodium or Tuinal
taken with or without food. Brand Name: Nembutal. given with or without food.
Generic Name: Amobarbital
Generic Name: Pentobarbital
Pharmacologic class: Barbiturates
Pharmacologic class: Barbiturate Oral
General Action:
General Action: sedative-hypnotics Hypnotic
Adult: 100-200 mg at bedtime.
Mechanism of Action: Amobarbital
Mechanism of Action: Pentobarbital is a
interferes w/ the transmission of impulses
barbiturate mainly used as a sedative and Sedation
from the thalamus to the cortex of the brain
hypnotic. It has been suggested that its Adult: 20-40 mg 2-4 times daily.
which develops an imbalance in central
pharmacologic effect is due to its property Child: 2-6 mg/kg daily in 3 divided doses.
inhibitory and facilitatory mechanisms.
to enhance the activity of GABA by altering Max: 100 mg.
GABA receptor-mediated inhibitory
Side Effects: Bradycardia, syncope,
synaptic transmissions
hypotension; apnoea, atelectasis (post-op),
hypoventilation; agitation, anxiety, ataxia,
Side Effects: Drowsiness, somnolence,
confusion, CNS depression, dizziness,
dizziness, anxiety, insomnia; hypotension,
fever, hallucinations, headache, insomnia,
apnoea, resp depression, bronchospasm,
nightmares, nervousness, psychiatric
laryngospasm, bradycardia, CNS
disturbances, somnolence, abnormal
depression, physical and psychological
thinking; hyperkinesias; nausea, vomiting,
dependence, psychiatric disturbance,
constipation; liver damage; megaloblastic
confusion, hallucinations, nightmares,
anaemia (following chronic phenobarbital
thinking abnormality, syncope,
use); angioedema, rash; inj site reaction.
hyperkinesias, ataxia, agitation,
nervousness, nausea, vomiting, constipation,
Drug- Drug Interaction: May reduce plasma
pain at inj site.
levels of oral anticoagulants (e.g. warfarin,
Potentially Fatal: Stevens-Johnson
dicoumarol, acenocoumarol,
syndrome.
phenprocoumon), corticosteroids,
griseofulvin, doxycycline, Na valproate and
Drug- Drug Interaction: Additive effect w/
valproic acid. Constant monitoring of blood
other CNS depressants. Increased plasma
levels when concomitantly used w/
concentrations w/ MAO inhibitors. May
phenytoin. May increase CNS depressant
decrease serum levels of phenytoin,
effect w/ antihistamines, sedative/hypnotics,
carbamazepine, valproic acid. May increase
tranquilisers. May prolong the effect w/
metabolism of anticoagulants,
MAOIs. May reduce the effect of estradiol,
corticosteroids, griseofulvin, doxycycline
progesterone, estrone and other steroidal
and hormonal contraceptives.
hormones.
 Hepatobiliary disorders: Hepatitis, amprenavir, darunavir, lopinavir, indinavir,
cholestasis. nelfinavir, saquinavir), clonazepam,
Musculoskeletal and connective tissue aprepitant, β-blockers (e.g. metoprolol,
disorders: Dupuytren's contracture, timolol), Ca channel blockers (e.g.
PHENOBARBITAL arthralgia, frozen shoulder, osteomalacia, felodipine, diltiazem, verapamil,
rickets; osteopenia, osteoporosis (prolonged nifedipine), digoxin, ciclosporin, tacrolimus,
Brand Name: Luminal Sodium®,
use). corticosteroids, etoposide, irinotecan,
Solfoton®, Tedral®
Nervous system disorders: Drowsiness, eplerenone, haloperidol, gestrinone,
Generic Name: Phenobarbital
ataxia, nystagmus. toremifene, methadone, montelukast,
Pharmacologic class: Barbiturates
Psychiatric disorders: Mental depression, theophylline, sodium oxybate, thyroid
General Action: Anticonvulsants /
hallucination; confusion, restlessness (in hormones, tibolone, tropisetron, vitamin D.
Hypnotics & Sedatives
elderly); memory and cognitive impairment; May reduce the effect of oral contraceptives
behavioural disturbances (in children). containing estrogen and/or progestogen.
Mechanism of Action: Phenobarbital is a
Skin and subcutaneous tissue disorders: May increase the metabolism of
long-acting barbiturate that has hypnotic,
Maculopapular, morbilliform or paracetamol which may lead to reduced
sedative, and anticonvulsant activities. The
scarlatiniform rashes. effect and increased risk of hepatotoxicity.
exact mechanism of action is unknown, but
Vascular disorders: Hypotension, syncope.
it may be related to its ability to enhance
Time Best Given:
and/or mimic the synaptic action of GABA.
Drug- Drug Interaction: Concurrent use Phenobarbital is given by mouth in the form
It depresses the sensory cortex, reduces
with MAOIs, SSRIs, and TCAs may of a tablet, capsule, liquid solution, paste, or
motor activity, changes cerebellar function,
antagonise antiepileptic activity of chewable. It may be given with or without
and produces drowsiness, sedation, and
phenobarbital by reducing the convulsive food.
hypnosis. Its anticonvulsant property is
threshold. May result in additive CNS Sedation
exhibited at high doses.
depressant effects when used concomitantly Adult: 30-120 mg daily in 2-3 divided doses
with other CNS depressants (e.g. via deep IM inj or slow IV inj at a rate of no
Side Effects: ignificant: Respiratory
antihistamines, narcotics, tranquilisers). more than 60 mg/min. Max: 400 mg daily.
depression (particularly IV use), suicidal
Increased plasma concentration with
ideation and behaviour; paradoxical
oxcarbazepine, phenytoin, methylphenidate, Oral
responses (including agitation,
chloramphenicol, valproic acid or Na Sedation
hyperactivity); drug dependence, decreased
valproate. May decrease plasma Adult: 30-120 mg daily in 2-3 divided
BMD, increased risk of fractures (prolonged
concentration with vigabatrin or folic acid. doses. Max: 400 mg daily.
use).
May decrease efficacy with memantine.
Blood and lymphatic system disorders:
May reduce the plasma concentrations of
Agranulocytosis, megaloblastic anaemia,
disopyramide, quinidine, chloramphenicol,
thrombocytopenia.
doxycycline, metronidazole, rifampicin,
Cardiac disorders: Bradycardia.
anticoagulants (e.g. dicoumarol),
Gastrointestinal disorders: Nausea,
chlorpromazine, paroxetine, mianserin,
vomiting.
TCAs, carbamazepine, lamotrigine,
General disorders and administration site
tiagabine, zonisamide, primidone,
conditions: Lethargy, hangover effect; inj
ethosuximide, antifungals (e.g. itraconazole,
site reactions (IV/IM).
posaconazole, griseofulvin, voriconazole),
aripiprazole, antivirals (e.g. abacavir,