Professional Documents
Culture Documents
Antidepressants
SSRI(1stline for panic dso, social anxiety dso, Paroxetine, sertraline, escitalopram
OCD,GAD,PTSD)
SNRI(line for GAD; 2 line for panic dso, social Venlafaxine
anxiety dso, OCD,PTSD)
TCA(2 line for panic dso, OCD,GAD,PTSD) Clomipramine
NaSSA(2 line for panic dso, GAD, PTSD) Mirtazapine
MAOI(3 line for panic dso, social anxiety Phenelzine
dso,PTSD)
Anticonvulsants
GABA analogs (2 line for social anxiety disorder, Gabapentin, pregabalin)
GAD)
Phenyltriazine (2 line for PTSD) Lamotrigine
Benzodiazepines (2 line for panic dso, social Gabapentin, pregabalin
anxiety disorder, GAD)
Phenyltriazine (2 line for PTSD) Lamotrigine
Benzodiazepines (2 line for panic dso, social Alprazolam, diazepam, lorazepam
anxiety disorder, GAD)
Azaspirone(2 line for GAD) Buspirone
OTHER INDICATIONS
INDICATIONS
The potency of benzodiazepine is the affinity of the parent drug or its active metabolites.
Most helpful during the beginning phase of treatment and not recommended long-term.
PHARMACOLOGY
GABAA-receptor subtypes containing an 1 subunit are associated with sedation, ataxia and
amnesia
Those containing 2 and/or 1 subunits generally have greater anxiolytic activity
DOSING
Majority are for short-term (<2months) treatment although many have extended treatment
Clinicians should discuss the risk of long-term treatment with patients
Can cause physical and psychological dependence, tolerance and withdrawal symptoms
IM use is discouraged with diazepam because absorption is slow, erratic and possibly
incomplete; local pain often occurs.
Following IV administration of diazepam, local pain and thrombophelbitis may occur due to
precipitation of the drug or due to irritant effect of propylene glycol. A saline flush following IV
admin.
Age, liver, disease, physical disorders as well as concurrent use of other drugs may influence
parameters by changing the volume of distribution , metabolism and elimination half-life
Lipid solubility is positively correlated with enhancing the following properties of benzodiazepines:
Affinity for peripheral adipose tissue, resulting in redistribution from the vascular
compartment, causing increase in volume of distribution
Passage across BBB, facilitating its CNS activity
Duration of action is dependent on dose, rate of absorption, arte and extent of drug distribution,
and rate of elimination
Renal impairment may increase free unbound plasma concentration of benzo and reduce its
clearance
Benzodiazepine with long half-life (diazepam) may have short duration of action if dose is
small or if it undergoes rapid and extensive distribution
Short half-life benzodiazepine(lorazepam) may have long duration of action if dose is large
or if it has limited peripheral distribution
Generally, short-acting drugs can be used as hypnotics and for acute problems relating to anxiety
Long-acting ones can be used for chronic conditions where a continuous drug effect is needed
The longer the half-life, the greater the likelihood it will have an adverse effect on daytime
functioning
The short half-life ones are often associated with interdose withdrawal, rebound anxiety
between doses and anterograde amnesia
ADVERSE EFFECTS
CNS
Most common are extensions of the generalized sedative effect like fatigue and drowsiness
Impaired mental speed, central cognitive processing ability, memory and performance
Chronic use: impaired visuospatial and visuomotor abilities, such as decreased motor
coordination, psychomotor speed and response time, concentration , speed of processing
info processing and verbal learning
Paradoxical irritability, impulsivity and agitation
Confusion and disorientation primarily in the elderly
Excessive doses can result in respiratory depression and apnea
Dysarthria, muscle weakness, incoordination, ataxia, nystagmus
Headache
Sexual dysfunction such as decreased libido, erectile dysfunction, anorganism, ejaculatory,
disturbance and gynecomastia
Dizziness with higher doses of clonazepam
Increased salivation in clonazepam
Few reports of allergies
DISCONTINUATION SYNDROME
Withdrawal: Occur 1-2 days with short-acting agents, up to 5-10 days with long-acting agents after
discontinuation
PRECAUTION
At risk of being abused by susceptible individuals; they prefer those with rapid peak effects such as
diazepam, lorazepam and alprazolam
TOXICITY
PEDIATRIC
Probable indications include seizure disorders, insomnia, night terrors and somnambulism
Metabolizes faster in children than in adults so may require small divided doses to maintain
blood levels
GERIATRIC
Caution when using it with those drugs that can cause CNS effects; excessive sedation can
cause confusion and disorientation
Increases incoordination and risks of falls three-fold
USE IN PREGNANCY
Benzodiazepines and metabolites freely cross the placenta and accumulate in fetal
circulation
Excreted into breast milk in levels sufficient to produce effects in the newborn
Associated with increased risk of congenital anomalies in the first trimester esp. and
neonatal withdrawal with chronic doses
If used in last week of pregnancy, may produce neonatal CNS, depression, poor feeding,
hypothermia, flaccidity and respiratory depression
Metabolism in infants is slower esp. during first six weeks
Long-acting drugs may accumulate
Use of grapefruit and pomegranate juice while taking benzodiazepines can result in
increased blood levels and result in more pronounced effect of the benzodiazepines
Antacids delay absorption of benzodiazepines in the intestines
Separate their administration
BUSPIRONE
INDICATIONS
GAD
Alternative to benzodiazpines when sedation and psychomotor impairment may be
dangerous
In patients with history of alcohol or substance abuse
OCD: for relief of anxiety
Depression: augment effects of antidepressants
Agitation: aggression, antisocial behaviors
Social phobia
Premenstrual syndrome
Bruxism caused by antidepressants
PHARMACOLOGY - not fully understood, it has affinity for central D2 receptors and 5-HT1A receptor
as partial agonist
PHARMACOKINETIC
ADVERSE EFFECTS
Because of its binding to central dopamine receptors, it potentially increases risk of dystonia,
pseudoparkinsonism
Has been reported to precipitate mania and hypomania primarily in the elderly; high doses may
worsen psychosis
Excessive dose may just produce extension of pharmacologic effects such as dizziness,
nausea, vomiting
Monitor vital signs and give supportive therapy
PRECAUTIONS
PEDIATRIC
Geriatric