ANTIDEPRESSANTS -An antidepressant is a psychiatric medication used to alleviate mood disorders, such as major depression and dysthymia and anxiety disorders such as social anxiety disorder. – They can improve your mood, sleep, appetite and concentration. It may take several weeks for them to help. – Antidepressant agents act by increasing the levels of excitatory neurostransmitters. Excitatory neurotransmitters are not necessarily exciting – they are what stimulate the brain.
Those that calm the brain and help create balance are called inhibitory. Inhibitory neurotransmitters balance mood and are easily depleted when the excitatory neurotransmitters are overactive. The main types of antidepressant drugs in use today are: 1. Tricyclic antidepressants (TCAs) – are the oldest class of antidepressant drugs – block the reuptake of certain neurotransmitters such as norepinephrine (noradrenaline) and serotonin -tricyclic antidepressants have been used to treat mental depression.
Like other antidepressant drugs, they reduce symptoms such as extreme sadness, hopelessness, and lack of energy. Some tricyclic antidepressants are also used to treat bulimia, cocaine withdrawal, panic disorder, obsessive-compulsive disorders, certain types of chronic pain, and bed-wetting in children. 2. selective serotonin reuptake inhibitors (SSRIs or serotonin boosters) – are said to work by preventing the reuptake of serotonin -they help reduce the extreme sadness, hopelessness, and lack of interest in life that are typical in people with depression.
Selective serotonin reuptake inhibitors also are used to treat panic disorder, obsessive compulsive disorder (OCD), and have shown promise for treating a variety of other conditions, such as premenstrual syndrome, eating disorders, obesity, self-mutilation, and migraine headache. 3. monoamine oxidase inhibitors (MAO inhibitors) – may be used if other antidepressant medications are ineffective – work by blocking the enzyme monoamine oxidase which breaks down the neurotransmitters dopamine, serotonin, and norepinephrine (noradrenaline). help reduce the extreme sadness, hopelessness, and lack of interest in life that are typical in people with depression. MAO inhibitors are especially useful in treating people whose depression is combined with other problems such as anxiety, panic attacks, phobias, or the desire to sleep too much. 4. tetracyclic compounds and atypical antidepressants – ay be prescribed when SSRIs or TCAs have not worked. DRUGINDICATIONMECHANISM OF ACTIONCONTRAINDICATIONSIDE EFFECTS /ADVERSE EFFECTSUSUAL DOSE TCAs Imipamine (Tofranil, Janimine) -For the relief of symptoms of depression. -temporary adjunctive therapy in reducing enuresis (bedwetting or involuntary urination) in children aged 5 years and older-Imipramine works by inhibiting the neuronal re-uptake of the neurotransmitters norepinephrine and serotonin-convulsive disorders or glaucoma -acute recovery phase following a myocardial infarction -hypersensitivity to the drug hepatic or renal damage, and those with a history of blood dyscrasias -should not be given in conjunction with, or within 14 days of treatment with a MAO inhibitor (Combined therapy of this type could lead to the appearance of serious interactions such as hypertensive crises, hyperactivity, hyperpyrexia, spasticity, severe convulsions or coma and death may occur. )-Dizziness, drowsiness, confusion, seizures, headache, anxiety, tremors, stimulation, weakness, insomnia, nightmares -Orthostatic hypotension, EKG changes, tachycardia, hypertension, palpitations, dysrhythmias -Blurred vision, tinnitus, mydriasis Diarrhea, Dry mouth, nausea, vomiting, paralytic ileus, increased appetite, cramps, epigastric distress, jaundice, hepatitis, stomatitis, constipation, taste change -Urinary retention, acute renal failure? Hospitalized patients: starting with 3 times 25 mg, increasing to 125 mg ? Ambulatory patients: starting with 25 to 75 mg daily, increasing up to a maximum of 200 mg daily ? Pediatric patients: starting with 10 mg daily AVAILABILITY: Tablets: 10mg, 25mg, 50mg. Sustained- release capsules: 75, 100, 125 or 150 mg. ?Nortriptyline ( Aventyl, Pamelor)-relief of symptoms of depression for treating nocturnal enuresis -for the treatment of panic disorder, irritable bowel syndrome, migraine prophylaxis and chronic pain or neuralgia modification -inhibits the activity of such diverse agents as histamine, 5-hydroxytryptamine, and acetylcholine. It increases the pressor effect of norepinephrine but blocks the pressor response of phenethylamine-acute recovery phase after myocardial infarction -As for all tricyclic antidepressants, concurrent use, or failure to allow a two week gap, with monoamine oxidase inhibitors (MAO inhibitors, e. g. phenelzine, tranylcypromine, etc. ) may precipitate hyperpyretic crisis and/or severe convulsions; fatalities have occurred-heart rate, blurred vision, urinary retention, dry mouth, constipation, weight gain or loss, and low blood pressure on standing -rash, hives, hepatitis and seizures are rare -Overdoses of nortriptyline can cause life-threatening abnormal heart rhythms or seizures.? For adults is 25 mg given 3 to 4 times daily. ?In children, doses usually are 30 to 50 mg once daily or in divided doses – It is advisable to begin at a low dose and increase the dose slowly.
AVAILABILITY: Capsules: 10, 25, 50, and 75mg. Oral solution: 10 mg/teaspoon ? Protriptyline ( Vivactil)All types of mental depression. Suitable for apathetic, withdrawn, depressed patients. acts by decreasing the reuptake of norepinephrine and serotonin (5-HT) in the brain-hypersensitivity to protriptyline – it has anticholinergic activity, protriptyline is contraindicated in glaucoma and when there is predisposition to urinary retention. – dry mouth, constipation, urinary retention, increased heart rate, sedation, irritability, dizziness, and decreased coordination Ambulatory patients, 15 to 30 mg daily in divided doses ? Hospitalized patients, 30 to 60 mg daily in divided doses ? If insomnia is present, do not give last daily dose later than midafternoon. SSRIs ?Citalopram (Celexa)- for the treatment of depression- The ability of citalopram to potentiate serotonergic activity in the central nervous system via inhibition of the neuronal reuptake of serotonin is thought to be responsible for its antidepressant action- Concomitant use in patients taking monoamine oxidase inhibitors – Concomitant use in patients taking pimozide patients with a hypersensitivity to citalopram or any of the inactive ingredients in Citalopram. – Feeling or being sick, diarrhea – Sleepiness, dizziness, weakness -dry mouth -headache – Increased sweating, shakiness, difficulty focusing, difficulty sleeping, agitation, nervousness, constipation, loss of appetite, weight changes? 10 mg, 20 mg, and 40 mg tablets, as well as 10 mg/5 mL peppermint flavor oral solution AVAILABILITY: Tablets: 10, 20, and 40 mg. Solution: 10 mg/5 ml ?Fluoxetine Prozac)-treatment of major depression, obsessive compulsive disorder, bulimia nervosa and panic disorder – primarily that of an SSRI although it may produce some of its effects through 5-HT2C antagonism in a manner similar to the novel antidepressant agomelatine. Other psychopharmacological substances that exhibit 5-HT2C antagonism are mirtazapine, trazodone, some tricyclic antidepressants and various (mainly atypical) antipsychotics. – People who have taken a monoamine-oxidase inhibitor antidepressant (MAOI) in the last 14 days. Manic episodes. -Uncontrolled epilepsy. -Uncontrolled seizure disorders, eg due to brain injury -Prozac liquid contains sucrose and should not be used by people with rare hereditary problems of fructose intolerance- nausea, headaches, anxiety, insomnia, drowsiness, and loss of appetite – skin rashes and vasculitis (inflammation of small blood vessels) – Increased blood pressure -seizures ?adults is treated with 20-80 mg of fluoxetine daily. ?depression in children is 10-20 mg daily AVAILABILITY: Capsules: 10, 20, and 40 mg.
Capsules (delayed release): 90 mg. Tablets: 10, 15, and 20 mg. Oral suspension: 20mg/5ml ? Setrakine ( Zoloft): major depression, obsessive-compulsive disorder (OCD), posttraumatic stress disorder (PTSD), premenstrual dysphoric disorder (PMDD), panic disorder and social phobia (social anxiety disorder). – Acts as an antidepressant by inhibiting CNS neuronal uptake of serotonin; which raises serotonin levels in the CNS with little effect on norepinephrine, muscarinic, histaminergic, and alpha1-adrenergic or dopaminergic receptors. Concomitant use in patients taking monoamine oxidase inhibitors (MAOIs) is contraindicated – patients with a hypersensitivity to Sertraline or any of the inactive ingredients in Sertraline hydrochloride. – ANTABUSE (disulfiram) due to the alcohol content of the concentrate. – sleepiness, nervousness, insomnia, dizziness, nausea, tremor, skin rash, upset stomach, loss of appetite, headache, diarrhea, abnormal ejaculation, dry mouth and weight loss. Important side effects are irregular heartbeats, allergic reactions and activation of mania in patients with bipolar disorder. recommended dose of sertraline is 25-200 mg once daily AVAILABILITY: Tablets: 25, 50, and 100 mg; oral concentrate: 20 mg/ml MAOIs ?Isocarboxazid ( marplan)- treatment of panic disorder and the phobic disorders- works by irreversibly blocking the action of a chemical substance known as monoamine oxidase (MAO) in the nervous system – Children -Decreased liver function -Disease of the blood vessels in and around the brain (cerebrovascular disease) -Severe cardiovascular disease -Tumour of the adrenal gland (phaeochromocytoma) -Manic phase of manic depression. most common are dizziness, headaches, and nausea – insomnia, dry mouth, and shakiness ?PO Start with 10 mg twice daily ?increased by 10 mg increments every 2 to 4 days to achieve a dosage of 40 mg by the end of the first week ? Phenelzine ( nardil)- Anxiety, Depression, Obsessive-compulsive disorders, Pain, Phobias. – causes an increase in the levels of serotonin, norepinephrine, and dopamine in the neuron, relieving depressive symptoms. – Epilepsy, Phaeochromocytoma, Blood dyscrasias, Liver diseases, Cardiovascular disease, Cerebrovascular disease. – weight gain, dizziness, and fatigue Drowsiness, constipation, and weakness – difficulty urinating, jitteriness, and blurred vision, although these are rare? 15 mg of phenelzine three times per day ? increased to a maximum of 90 mg per day if lower doses are not effective ? tranylcypromine ( Parnate)- For the treatment of major depressive episode without melancholia. – act by increasing free serotonin and norepinephrine concentrations and/or by altering the concentrations of other amines in the CNS- In patients with cerebrovascular defects or cardiovascular disorders – In the presence of pheochromocytoma In combination with MAO inhibitors or with dibenzazepine-related entities – In combination with selective serotonin reuptake inhibitors (SSRIs-Blurred vision; decreased amount of urine and sexual ability; dizziness or lightheadedness (mild); drowsiness; headache (mild); increased appetite (especially for sweets) or weight gain; increased sweating; muscle twitching during sleep; restlessness; shakiness or trembling; tiredness and weakness; trouble in sleeping-in adults is 10 mg taken twice per day. -increased to 30 mg per day after a two-week period. -The maximum recommended amount is 60 mg per day.
The elderly (over age 60) are usually started on a dose of 2. 5 mg per day. Atypical Antidepressants ?Bupropion ( wellbutrin ) – treatment of depression and anxiety disorders; smoking cessation- inhibit neuronal uptake of serotonin, norepinephrine, and dopamine in the central nervous system – patients with a seizure disorder – patients treated with ZYBANO – patients with a current or prior diagnosis of bulimia or anorexia nervosa – patients undergoing abrupt discontinuation of alcohol or sedatives – patients who have shown an allergic response to bupropion or the other ingredients that make up Bupropion Tablets. Weight loss, nausea, and headaches -hair loss, bladder infections, and acne -suicidal thoughts or behavior, seizures, and any signs of an allergic reaction. ?300 mg/day, given as 150 mg twice daily. ?Maprotiline ( ludiomil)- For treatment of depression, including the depressed phase of bipolar depression, psychotic depression, and involutional melancholia, and may also be helpful in treating certain patients suffering severe depressive neurosis. inhibition of presynaptic uptake of catecholamines, thereby increasing their concentration at the synaptic clefts of the brain- hypersensitive to Maprotiline – with known or suspected seizure disorders – not recommended for use during the acute phase of myocardial infarction. – Anxiety or nervousness; blurred vision; constipation; dizziness; drowsiness; dry mouth; headache; nausea; tiredness; upset stomach; weakness.? Initial Dose: 75 mg orally as a single or divided daily dose. ?100 mg to 150 mg orally as a single or divided daily dose. Maintenance Dose: May be reduced to 75 to 150 mg orally