Antidepressant Drugs PDF

Anti-Depressants Drugs  Definition Antidepressants are substances used to treat depression, elevate mood and improve sense of well being.  Action  Elevate mood.  Improve sleep.  Increase appetite.  Increase activity.  Help patient to become more sociable. ...

Anti-Depressants Drugs  Definition Antidepressants are substances used to treat depression, elevate mood and improve sense of well being.  Action  Elevate mood.  Improve sleep.  Increase appetite.  Increase activity.  Help patient to become more sociable.  Decrease anxiety.  Classifications 1. Tricyclic & tetracyclic antidepressants (TCAs). 2. Monoamine oxidase inhibitors (MAOIs). 3. Selective serotonin reuptake inhibitors (SSRIs). 4. Novel or atypical antidepressants (post SSRIs).  Tricyclic & tetracyclic antidepressants (TCAs).  Action of TCAs: Depressed patients have decrease in serotonin, dopamine and norepinephrine.  1-Tri and Tetracyclic antidepressant (TCAs)  therapeutic action: Inhibit the reuptake of the neurotransmitters 5HT & NE by block reuptake site in pre synapse, so the drugs allow 5HT & NE to remain active in the synapse longer, thereby correcting a presumed deficit in the activity of these neurotransmitters.  Non therapeutic action :  Block alpha receptor lead to vasodilation and orthostatic hypotension.  Block histamine receptor lead to sedation and weight gain.  Block acetylcholine receptor lead to anticholinergic side effect.  : Indications of TCAs  Treatment & prophylaxis of major depressive disorder.  postpartum depression.  Treatment of premenstrual dysphoric disorder, is characterized by debilitating mood and behavioral changes in the week preceding menstruation that interfere with normal functioning.  Depressive episode of bipolar disorder.  Anxiety disorder (Generalized anxiety disorder, Obsessive compulsive disorder, Panic disorder, post traumatic stress disorder, specific and social phobia)  Eating disorders (Bulimia & anorexia nervosa)  Pain disorder  Other disorders: Sleep walking disorder, Childhood enuresis, Nightmare disorder.  Side effects of TCAs  Anticholinergic effects: Dry mouth, Constipation, Urinary retention, Blurred vision.  Cardiac effects: ECG changes, Tachycardia & arrhythmias, orthostatic hypotension  Endocrine and sexual effects: Impotence, hyperprolactenmia, anorgasmia, amenorrhea & ejaculatory disturbances.  Neurological effects: Sedation, dizziness, drowisness, Tremors & Myoclonic twitches of the tongue & upper extremities.  GIT : Weight gain, nausea, vomiting.  Name of TCAs  Tofranil  Anafranil  Tryptizol  Elavil  Vivactil 2-Monoamine Oxidase Inhibitors (MAOIs)  Monoamine(MA): such as neurotransmitter (norepinephrine, dopamine or serotonin) , food, drug.  Monoamine Oxidase(MAO): enzyme responsible for metabolism of monoamine and tyramine (end metabolite of protein).  Monoamine Oxidase Inhibitors(MAOI) : inhibit the effect of enzyme so inhibit metabolism of monoamine and tyramine.  : Action of MAOIs  This drugs inhibits the activity of monoamine oxidase enzyme (MAO), that metabolite neurotransmitters (norepinephrine, dopamine or serotonin) in synapses. The inhibition of this enzyme allows these neurotransmitters to remain active in the brain longer, thereby correcting a presumed deficit in monoamine function.  Indications of MAOIs:  For patient who not respond to TCAs.  Treatment of atypical depression, which manifested by ( hyperphagia, hypersomnia, phobic anxiety).  Treatment of acute depression as they have a rapid action in a short duration.  Treatment of anxiety disorder panic disorder, social phobia, generalized, obsessive compulsive disorder, post traumatic stress disorder.  Treatment of bulimia nervosa.  : Side effects of MAOIs  Liver: heptocellular damage , severe liver necrosis.  Psychotic: a retarded depression may converted into agitated one.  Hypomania may result.  Peripheral neuropathy may occur.  Hypertensive crisis: the "cheese effect".  Mechanism of hypertensive crisis  Some foods contain monoamine. These amines are normally deactivated by MAO enzyme that is present in the blood. This crisis occurs when a person treated with MAO inhibitors eats food containing amines. These amines accumulate and stimulate the sympathetic nervous system, increasing heart rate and blood pressure. This reaction can cause blood pressure to increase enough to produce intracranial bleeding or cardiovascular collapse.  Hypertensive crisis is triggered by:  Food contains tyramine: Aged cheese, beans, yeast products, Smoked salmon, Pickles, Chocolate, Coffee, Chicken liver, bananas.  Certain medications containing ephedrine such as Cough mixtures, antipyretic, antitussive, antibiotic.  Symptoms of hypertensive crises  Blood pressure over than 180/90.  dilated pupils.  Sever occipital headache.  Stiff neck.  Nausea & vomiting.  Sever nose bleeding.  Tachycardia.  Chest pain, coma, death.  Management of Hypertensive crisis  Preventive measures Avoid intake of food or medications contains tyramine.  Curative measures Stop the medication. Administer antihypertensive. Close monitoring of the patient.  Name of MAOIs  Nardil  Parnate  Marplan  Emsam 3-Selective Serotonin Reuptake Inhibitors (SSRIs)  Action of SSRIs:  Inhibit the reuptake of 5HT only by block reuptake site present in pre synapse. So allowing 5HT to remain active and available in the synapse longer, thereby correcting a presumed deficit in the activity of this neurotransmitter.  This drug highly safety margin(difference between toxic dose and therapeutic dose high).  : Indications of SSRIs  Treatment of depression during pregnancy and postpartum.  Depression in the elderly and medically ill, behavioral disturbance in the elderly because it has no cognitive side effect.  Treatment of major depressive disorder.  Effective in the treatment of anxiety disorders.  Treatment of eating disorders.  Chronic pain disorder.  Side effects of SSRIs  serotonin syndrome: concurrent administration of SSRIS and MAOI can raise plasma serotonin concentrations to toxic level, this serious and fatal syndrome. Symptoms include: diarrhea, restlessness, extreme agitation, hyperreflexia, rapid fluctuation in vital signs, hyperthermia, shivering, rigidity, delirium, coma, cardiovascular collapse and death.  Serotonin withdrawal : this caused by sudden stoppage of serotonin. Symptom includes: dizziness, weakness, nausea, headache, rebound depression, anxiety, insomnia, poor concentration, upper respiratory symptoms and migraine like symptoms  Sexual dysfunction: anorgasmia, impotence, delayed impotence.  GIT: Nausea, vomiting, anorexia, dyspepsia, diarrhea.  CNS: Nervousness, insomnia, anxiety, drowsiness.  Name of SSRIS  Prozac  Felozac  Zoloft  cipram  Celexa  Cetalo  Post selective serotonin reuptake inhibitors  Advantage Rapid improvement Less side effect  Disadvantage very expensive  Post selective serotonin reuptake inhibitors  Action: Some drug act as SSRIS inhibit the reuptake of 5HT this results in an increase of available serotonin in the synapse. Some drug act as tricyclic antidepressant but don’t have effect alpha, histamine or ACH. Name of Post selective serotonin reuptake inhibitors  Effexor  Trittico  Trazodone Why patient take antidepressant high risk to suicide  Antidepressant drug improve mood before improve thinking.  patient have energy to commit suicide.