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Drugs which can Elevate Mood (Mood Elevators)
Definitions
 Affective disorders - mental illnesses characterized by
pathological changes in mood (not thought – compare
with schizophrenia)
1. Unipolar disorders
 Depression – pathologically depressed mood.
 Mania – excessive elation and accelerated
psychomotor activity (rare)
2. Bipolar disorder (manic-depressive illness) – „cycling
mood“
 severe highs (mania) and lows (depressive
episodes)
It is common & normal emotion in which people
becoming depressed as a result of unfortunate
domestic and social conditions, sometimes the
depression is disproportionate to precipitating
factors or there may be no obvious cause at all.
 Clinical presentation:
 Emotional symptoms:
Sadness.
Hopelessness.
Loss of interest in usual activities.
Feeling of guilt.
 Physical symptoms
Fatigue
Sleep disturbance
Pain (especially headache)
Appetite disturbance ↑or ↓
 Intellectual or cognitive symptoms
Decreased ability to concentrate or slow thinking
Confusion
Poor memory for recent events.
 Reduced self-esteem & self-confidence.
 Ideas or acts of self harm or suicide.
What is the cause of depression?
Monoamine theory
Suggests that depression results from functionally
deficient monoamine neurotransmitters
(Norepinephrine (NE) &/or Serotonin (5-HT)) in
the CNS.
Therefore, in the treatment we try to ↑ the level of
these neurotransmitters
Major classes of anti-depressants:
1.Reuptake inhibitors
A. Selective serotonin(5-HT) reuptake inhibitors
(SSRIs)
e.g. Fluoxitine
B. Selective norepinephrine(NE) reuptake
inhibitors
e.g. Reboxitine
C. None Selective NE/5-HT reuptake
inhibitors(TCAs)
e.g. Imipramine ,Amitriptyline
2. Monoamine oxidase inhibitors
e.g. Phenelzine
3. Atypical antidepressants
e.g. Mirtazapine
Tricyclic antidepressants (TCAs)
 MOA
Inhibit reuptake mechanism which is responsible for
termination of the synaptic action of NE & 5-HT in
the brain
Blocking of receptors:TCAs also block
muscarinic,serotonin,histamine,
α-adrenergic responsible of S/Es
 Examples: Imipramine, Amitriptyline
Therapeutic uses
1.Major depression
2.Some panic disorder respond to TCAs
3.Imipramine has been used to control bed-wetting
in children (older than 6 years).
Advantages
Disadvantages / Side Effects
• Often effective in reducing
panic attacks and elevating
depressed mood.
•Usually a single daily dose
Anticholinergic : dry mouth, blurred
vision
constipation,
urinary retension
Antihistaminergic : Sedation
Alpha blockade : Postural hypotension
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 S/Es
 Antimuscarinic: constipation, blurred vision,
urinary retention, dry mouth
 Sedation
 Postural hypotension
 Arrhythmias
 Weight gain
 Selective Serotonin Reuptake Inhibitors
(SSRIs)
 MOA :Blocks serotonin reuptake only
 Examples: Fluoxetine
SSRIs have little activity
to block muscarinic,
histamine H1,
α-adrenergic receptors
& relatively safe in
over dose
 Therapeutic uses
1.Primary indication is depression
2.Obsessive compulsive disorders
3.Fluoxetine is effective in treating bulimia nervosa.
Unwanted effects:
In combination with MAOIs ,SSRIs can result in
“serotonin syndrome”
Monoamine Oxidase Inhibitors (MAOIs)
MOA: Inactivate monoamine oxidase A & B
enzymes, permitting neurotransmitter molecules
to escape degradation (↑ NE & 5-HT levels)
MAO is a mitochondrial enzymein the brain,
gut and liver.
Example: phenelzine
MOA of MAO inhibitors
 Indicated for depressed patients who are
unresponsiveness or allergic to TCAs
 Because of their risk for drug & drug food
interaction, MAOIs are considered
to be the last line agents.
 S/Es:
Hypertensive reaction may occur in patients taking
MAO inhibitors and consume Tyramine
containing food (“cheese reaction”)
(as aged cheeses, beer, red wines)
Pharmacology of theTyramine Reaction
Tyramine
Non-Selective MAO Inhibitor
Tyramine
Hydroxyphenylacetic acid
(inactive)
MAO-A
X
MAO-A
Norepinephrine (NE)
displacement
NE
NE NE
(
NE
NE
NE
Sympathomimetic
Response
NE
NE NE
Blood Pressure)
A persistent headache is often a warning
of rising blood pressure in patients on
MAOIs..
Drug Choice
 Comparisons of the antidepressants showed
that they are roughly equivalent in efficacy.
 Individual patients may respond better to one
drug than to another.
 SSRIs are not sedative, safe in overdose and
have mild adverse effects so they are widely
prescribed.
 Finding the right drug and the right dose must
be accomplished empirically.
Bipolar Disorder - image
Bipolar Disorder - image
Drugs used in Mania – Mood Stabilizers
The main goal of pharmacological
treatment of bipolar disorder is to reduce
the frequency & severity of fluctuations in
mood.
Lithium Carbonate
Alternative Drugs:
Carbamazepine
Sodium Valproate
Mood stabilizing drugs
 e.g Lithium salts
 Therapeutic uses: used prophylactically for treating
manic-depressive disorder & in the treatment of
mania.
It is Teratogenic.
Has a narrow therapeutic index, frequency &
severity of adverse reactions is directly related to
the serum levels.
Monitoring plasma concentration is essential,
especially in presence of renal disease.
Main unwanted effects: tremor, hypothyroidism,
thirst & polyuria.
Different preparations of lithium vary in
their bioavailability and patients should
receive only one preparation. they should
maintain a reasonable fluid intake.
Record cards are available for patients
taking lithium.
Think Positive!
Thank You