anti depressant drugs

Presented by:Zafreen chaudary

Definition of Depression

“An affective disorder characterized by loss of interest or pleasure in almost all a person’s usual activities or pastimes.”

Symptoms Associated With Depression Sadness, Despair,

Guilt, Pessimism Decrease in energy Decrease in sex

drive Insomnia and fatigue Thoughts of death

and suicide Mental slowing, lack

of concentration

Treatment of Depression

Antidepressant Pharmacology First introduced 40 years ago Also used for treatment of other

disorders including:Anxiety disorders, dysthymia, chronic pain and behavioral problems

Treatment

Evolution of drug therapy Antidepressants discovered accidentally while

investigating antipsychotic efficacy of modifications of phenothiazines

Imipramine - first antidepressant discovered Around the same time, monoamine oxidase

inhibitors were identified Late 1980’s- SSRI’s were developed Now working on other antidepressant treatments

Serotonin - Specific Reuptake Inhibitors (SSRI’s) Available for the past 15 years Allows for more serotonin to be

available to stimulate postsynaptic receptors

Available to treat depression, anxiety disorders, ADHD, obesity, alcohol abuse, childhood anxiety, etc.

Citalopram

Citalopram (Celexa) – well absorbed orally, few drug interactions, treats major depression, social phobia, panic disorder and OCD its side effects are as follow:

drowsiness, tired feeling; sleep problems

(insomnia); mild nausea, diarrhea,

upset stomach, dry mouth;

cold symptoms such as stuffy nose, sneezing, sore throat, cough;

increased sweating or urination, weight changes; or.

decreased sex drive, impotence, or difficulty having an orgasm.

Escitalopram

It prevents the reuptake of one neurotransmitter, serotonin, an action which results in more serotonin in the brain to attach to receptors. The FDA approved escitalopram in August 2002. But it has some side effects drowsiness, dizziness; sleep problems (insomnia);mild nausea, gas, heartburn, upset stomach, constipation; weight changes; decreased sex drive, impotence, or difficulty having an orgasm; or. dry mouth, yawning, ringing in your ears

Fluoxetine

Fluoxetine (Prozac) – first SSRI available, long half life, slow onset of action, can cause sexual dysfunction, anxiety, insomnia and agitation

Fluvoxamine (Luvox) – structural derivative of Prozac, became available for OCD, also treats PTSD, dysphoria, panic disorder, and social phobia

SSRI’s

Paroxetine (Paxil) – third SSRI available, more selective than Prozac, highly effective in reducing anxiety and posttraumatic stress disorder (PTSD) as well as OCD, panic disorder, social phobia, premenstrual dysphoric disorder, and chronic headache

Sertraline (Zoloft) – second SSRI approved, low risk of toxicity, few interactions, more selective and potent than Prozac

SSRI’s

Serotonin syndrome At high doses or combined with other drugs an

exaggerated response can occur This is due to increased amounts of serotonin Alters cognitive function, autonomic function and

neuromuscular function Potentially fatal

Serotonin withdrawal syndrome With discontinuation of any SSRI onset of withdrawal

symptoms occur within a few days and can persist 3-4 weeks

Symptoms: disequilibrium, gastrointestinal problems, flu-like symptoms, sensory disturbances, sleep disturbances

SEROTONIN/NOREPINEPHRINE REUPTAKTE INHIBITORS SNRIs

SNRIs may be effective in treating depression in patient in whom SSRIs are ineffective

Depression is often accompanied by chronic painful symptoms such as, backache, and muscle ache. Both SNRIs and TCAs with their dual inhibition of both serotonin and norepinephrine reuptake are effective in relieving such pains.

VENLAFAXINE

Venlafaxine (VEN-la-fax-een) is potent inhibitor of serotonin reuptake.

The most common side effects of venlafaxine are nausea, headache, sexual dysfunction, dizziness, insomnia, sedation and constipation.

High doses may be increase blood pressure and heart rate.

DULOXETINE

Duloxetine (doo-LOX-e-teen) inhibit serotonin and norepinephrine reuptake at all doses.

G1 side effects are common with duloxetine.

Overdose may increase blood pressure and heart rate.

LEVONMILNAXCIPRAN

Levonmilnacipran (leevo-mil-NA-si-pran) use for treatment of depression and its side effects are same as the other SNRIs.

Second Generation (Atypical) Antidepressants Developed in the late 1970’s and 1980’s Bupropion – selectively inhibits Dopamine reuptake,

used for ADHD, side effects include: anxiety, restlessness, tremors, and insomnia

Mirtazapine- it enhances serotonin and norepinephrine neurotransmitter. Mirtazapine is used to treat Major depressive disorder, side effect includes: Dizziness, Drowsiness ,Dry Mouth, Feeling Weak, High Cholesterol, Incomplete or Infrequent Bowel Movements, Increased hunger, Weight Gain.

Trazodone

Trazodone probably improves symptoms of depression by inhibiting the uptake of serotonin by nerves in the brain. This results in more serotonin to stimulate other nerves. Trazodone also may increase directly the action of serotonin.

Side effects including: Headache, Muscle ache, Nausea, vomiting, loss of appetite, or stomachache.Constipation or diarrhea, Loss of interest in sex (erectile dysfunction in men) Dizziness or loss of balance, Dry mouth or dry eyes, Numbness, burning, or tingling sensations.

It will not cause of weight gain.

Tricyclic Antidepressants Effectively relieve depression with anxiolytic (used to

reduce anxiety) and analgesic action (a remedy that relieves pain)

First choice for treatment of depression Pharmacological properties

Block presynaptic norepinephrine reuptake transporter Block presynaptic serotonine reuptake transporter Block postsynaptic histamine receptors Block postsynaptic acytalcholine receptors

Imipramine and Amitriptyline Prototypical Tricyclic Antidepressants Desipramine (Norpramin) –

pharmacologically active intermediate metabolite of imipramine (tofranil)

Nortriptyline (Pamelor) – an active intermediate metabolite of amitriptyline (elavil)

Clinical Limitations of Tricyclic Antidepressants Slow onset of action Wide variety of effects on CNS (adverse side effects):

Can directly impair attention, motor speed, dexterity (learning skills), and memory

Cardiotoxic and potentially fatal in overdoses

Pharmacological Effects of Tricyclic Antidepressants In CNS: blocks presynaptic serotonin, norepinephrine

receptors Blocking of Acetylcholine receptors leads to dry mouth,

confusion, blurry vision and mental confusion Blocking of histamine receptors leads to drowsiness and

sedation Effects on the Peripheral nervous system include: cardiac

depression, increased electrical irritability, can be life threatening with over dosages

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