Home' Australian Pharmacist : Australian Pharmacist August 2016 Contents Australian Pharmacist August 2016 I © Pharmaceutical Society of Australia Ltd.
Taken in high doses, the stimulating
effects of tranylcypromine, an M AOI,
leads to abuse. Its amphetamine-like
structure promotes this while other
drugs in its class not sharing its structure
display no potential for abuse. Either
through overdose of or withdrawal from
tranylcypromine, it has been reported
that delirium or thrombocytopenia have
developed. These effects may be more
pronounced as dosages grow higher.
When non-selective MAOIs are
combined with certain foods that are
high in tyramine, there exists a risk of
hypertensive crisis. This risk is highest
for tranylcypromine. Individuals who are
unaware of the recommended dietary
restrictions or those taking high doses of
MAOIs are most at risk.
TCAs (tricyclic antidepressants) with
anticholinergic or sedative properties
display the greatest potential for abuse.
High doses of amitriptyline produce
contentment, euphoria, giddiness, and
relaxation. There is a move to caution
against prescribing TCAs to methadone
patients as about 25% were abusing
amitriptyline in the desire to become
euphoric. Dothiepan has been similarly
used in Europe.
Many patients attending drug treatment
clinics admitted using TCAs to produce
euphoria and pleasant auditory/visual
hallucinations. Many addicts not having
TCAs prescribed had TCA or metabolites
in their urine. Patients abusing narcotics
can take advantage of the synergistic
interaction of opiates and TCAs
enhancing and prolonging opiate effects.
Oral abuse of bupropion is highly
unlikely. Nasal insufflations produce a
cocaine-like effect by bypassing first-
pass metabolism, producing a quicker,
higher plasma concentration that an
oral intake. Structurally it resembles
amphetamine and endogenous
monoamines. It inhibits dopamine and
nor-epinephrine reuptake. It potentiates
Fluoxetine – is a selective serotonin
reuptake inhibitor (SSRI) which
selectively blocks the reuptake of
serotonin. However, while they are more
selective at the serotonin receptor, all
SSRIs impact other neurotransmitter
systems, including nor-epinephrine and
dopamine reuptake blockade.
Reports indicate that high doses of
fluoxetine have amphetamine-like
effects. One patient took 80 mg with two
beers to produce extra energy, mood
elevation and jitteriness, but unlike speed
he felt ‘numb and calm’. A handful of
medication led to amphetamine effects
and insomnia. Taking up to 280 mg/
day, an abuser developed tolerance,
dependence and withdrawal. One case
described an anorexic woman taking up
to 120 mg/day of fluoxetine for appetite
suppression and weight loss.
In overdose, they are thought to be
relatively safe. Rarely fatalities have
involved co-ingestion of alcohol or
drugs dependent on the cytochrome
P450 2D6 system, such as TCAs.
A combination of fluoxetine with
MDMA (ecstasy), either with or without
sertraline, will result in a prolonged
effect of MDMA.
Venlafaxine – is a serotonin and nor-
epinephrine reuptake inhibitor (SNRI).
A report for venlafaxine found that an
individual experienced amphetamine-
like effects while averaging 2100 mg/
day with doses rising to 3750 mg/day.
He took it to feel ‘more empathic and
sociable’ and for the purpose of ‘elating’
his mood. Presenting with profound
weight loss, tremor, dizziness, and
muscle weakness, he was hospitalised
for detoxification with significant
withdrawal, he later resumed abuse.
Another 38 year old man with a history
of depression and amphetamine use
ingested doses up to 4050 mg to
achieve an ‘amphetamine-like high’.
Since the maximum recommended
dose is 375 mg it is not surprising that
he presented for medical attention with
Venlafaxine can cause a sustainable
elevation of blood pressure in certain
people while on therapeutic levels.
For them, regular blood pressure
checking is recommended. Higher
doses likely place someone at greater
risk of hypertension and hypertensive
crisis. At recommended doses, SNRIs do
not affect cardiac conduction or lower
seizure threshold; however, in overdose
may occur. A combination of venlafaxine
and other drugs with or without alcohol
have been involved in fatal overdoses.
Most anticonvulsants have not
demonstrated significant potential
for abuse except for pregabalin and
Recently, ER physicians in Belfast have
witnessed an increase in the number of
patients presenting after recreational
abuse of pregabalin.
Patients, state that the medication
induces a state similar to drunkenness,
hence the street name ‘Budweiser’s’.
To our knowledge this is the first case
series detailing the recreational abuse
of pregabalin, a drug which has become
popular in primary care. All were
aged between 20 and 35 years of age.
Dosages ranged from 500–1400 mg.
Seizures and admissions to ICU
Patients are either taking tablets whole
or cutting and snorting them.
Gabapentin is approved for the
treatment of epilepsy and post-herpetic
neuralgia. It is an anticonvulsant and
is able to treat seizures by decreasing
‘abnormal activity in the brain.’ It also
changes the way the body senses pain.
It is often prescribed off-label for other
pain syndromes, anxiety and mood
disorders, restless legs syndrome,
and alcohol withdrawal among other
conditions. Most recently, it has
been used in some capacity to treat
individuals suffering from marijuana
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