RIMA -
Reversible Inhibitor of MonoAmine oxidase (type A)
(Wiki)
Also
referred to as a reversible MonoAmine Oxidase Inhibitor
(rMAOI)
Please note:
Dosage equivalents are provided for certain drugs below and
are denoted as unit equivalents, i.e. one unit of drug x is
roughly the equivalent as one unit of drug y, where the
dosage equal to one unit varies.
RIMA antidepressants share much of their properties
with MAOI antidepressants, the differences being reversibility
and selectivity.
Whereas MAOI drugs permanently bind with
monoamine oxidase enzymes (thereby preventing them from breaking
down monoamine neurotransmitters, notably serotonin, noradrenaline and dopamine), RIMA drugs bind with the enzymes in a reversible manner and can detach,
thereby reactivating the enzyme.
Monoamine oxidase enzymes are split into two isoforms, MAO-A and MAO-B. MAO-A chiefly breaks down serotonin, melatonin, adrenaline and noradrenaline, whilst MAO-B breaks down phenylethylamine and trace amines; dopamine seems to be pretty evenly spread over
the two of them. RIMA antidepressants preferably inhibit MAO-A rather than MAO-B; moclobemide, for instance, at a dose of 300mg
roughly inhibits 80% of MAO-A enzymes and 25% of MAO-B enzymes.
In terms of effectiveness, RIMA antidepressants are weaker than typical or
irreversible MAOIs as a direct result of their very
nature. However, they are more likely to produce a
positive effect in patients than any reuptake inhibiting
antidepressant family (for example,
NARI drugs, TCA drugs and SSNaRI drugs).
Unlike MAOI antidepressants, dietry restrictions are not strictly
necessary when being treated with RIMA drugs, although eating large amounts
of tyramine rich foods is probably not the
greatest idea in the world; too much tyramine can technically cause a
hypertensive crisis, a spike in blood pressure that leads to headaches and in the worst case a
stroke; the chances of this with
these drugs though is pretty remote.
Monoamine oxidase inhibitors in general aren't
the smartest things to combine with other
antidepressants or for that matter other
drugs in general. In particular, they should
not be mixed with antidepressants that inhibit the reuptake of
serotonin for fear of inducing a potentially
fatal condition known as serotonin syndrome and many antidepressants such as tricyclics can cause, just as tyramine can, a hypertensive crisis. Emergency pain killers aren't good things to be given either,
so you might want to carry a medic alert on your person. Typically, your doctor
will give you a small amount of an antidote that will combat and hopefully avert
any hypertensive crisis by lowering your blood pressure; one example is a drug called nifedipine (marketed as Adalat®) which can be supplied as liquid
capsules; pop one in your mouth, bite it and the
drug will be absorbed extremely quickly
indeed, kind of like an injection. Again, these are not
really needed for RIMA therapy, but they can be reassuring to
have.
Befloxatone
(Wiki)
Brand names:
None known
Formula: Unknown
Half life: ~ 11 hours
Single unit dose: Unknown
Recommended outpatient dose: Unknown
Maximum outpatient dose: Unknown
I have no
information on this drug at this time.
Brofaromine (Wiki)
Brand names:
Consonar®
Formula: C14H16BrNO2
Half life: ~ 12 hours (not a trustworthy
figure)
Single unit dose: Unknown
Recommended outpatient dose: 50mg per day
[Highly
Questionable]
Maximum outpatient dose: 150mg per day
[Highly
Questionable]
Brofaromine is not currently available to patients
worldwide, which is a pity considering the promise it
has shown. Not only does this drug act as a reversible and
selective monoamine oxidase inhibitor, it also exhibits an
ability to act as a selective serotonin reuptake inhibitor; this means that
the drug is likely to be effective in a
comparatively large number of patients. Additionally, brofaromine has been shown to exhibit relatively
few side effects compared with the average
antidepressant at the time of writing.
Cimoxatone
(Wiki)
Brand names:
None known
Formula: C19H18N2O4
Half life: Unknown
Single unit dose: Unknown
Recommended outpatient dose: 40mg per day
[Highly
Questionable]
Maximum outpatient dose: Unknown
I have no
information on this drug at this time.
Moclobemide
(Wiki)
Brand names:
Aurorix®, Manerix®
Formula: C13H17ClN2O2
Half life: ~ 1.5 hours
Single unit dose: Unknown
Recommended outpatient dose: 300mg per day
[Verified]
Maximum outpatient dose: 600mg per day
[Verified]
Currently the
only RIMA available for conventional
treatment, moclobemide lacks the major side effects of its irreversible brethren
(MAOI antidepressants) yet retains a greater chance of
success than conventional antidepressants.
Generally considered to be less effective at
combating depressive symptoms than true (irreversible)
MAOI antidepressants, moclobemide still plays a valuable role as a
compromise medication, one that does not require those
being treated with it to conform to a special
diet or to refrain from most over the
counter medications.
Moclobemide is known to aggravate present
psychotic symptoms in some cases so sufferers should
proceed with caution. The most common side effects are a dry mouth (9.2%), headaches and/or feelings of pressure in the
head (8% chance), insomnia and/or sleep disturbances (7.3%), nausea (5.2%), dizziness (5.1%) and tremor (5.0%).
Toloxatone
(Wiki)
Brand names:
Humoryl®, Perenum®
Formula: C11H13NO3
Half life: ~ 1 to 2 hours
Single unit dose: Unknown
Recommended outpatient dose: 400mg per day
[Not
Verified]
Maximum outpatient dose: 600mg per day
[Not
Verified]
I have no
information on this drug at this time.