Name of the Antidepressants TCA & Others
- Amitriptyline
- Clomipramine
- Doxepin
- Bupropion
1.Amitriptyline
| Amitriptyline |
| Availability: Tablets: 10 mg, 25 mg, 50 mg, 75 mg, 100 mg, 150 mg. |
| Administration/handling: PO • Give with food or milk if GI distress occurs. Administer full dose at bedtime to minimize orthostatic hypotension. Don’t withdraw drug suddenly. Instead, taper dosage gradually.; If patient is scheduled for surgery, discuss dosage tapering with prescriber.; Be aware that drug is often used in conjunction with psychotherapy |
| Depression: PO: Adults: Initially, 25–50 mg/day as a single dose at bedtime, or in divided doses. May gradually increase up to 100–300 mg/day. Titrate to lowest effective dosage. Elderly: 10 mg 3 times/day and 20 mg at bedtime. Adolescents: 10 mg 3 times/day and 20 mg at bedtime. |
| Pain Management: PO: Adults, elderly: 25–50 mg at bedtime. May increase to 150 mg/day. Children: Initially, 0.1 mg/kg. May increase over 2 weeks to 0.5–2 mg/kg at bedtime. |
Mechanism of Action:
Blocks reuptake of neurotransmitters (norepinephrine, serotonin) at presynaptic membranes, increasing synaptic concentration in the CNS. Therapeutic Effect: Antidepressant effect.
Indications:
- To relieve depression, especially when accompanied by anxiety and insomnia
- Pain Management
Cautions & Contraindications:
- Hypersensitivity to amitriptyline.
- Acute recovery period after MI
- Co-administered with or within 14 days of MAOIs
- Cautions: prostatic hypertrophy
- History of urinary retention or obstruction
- Narrow-angle glaucoma
- Diabetes, seizures, hyperthyroidism
- Cardiac/hepatic/renal disease
- Schizophrenia
- Xerostomia, visual problems, constipation or bowel obstruction, elderly, increased intraocular pressure (IOP)
- Hiatal hernia, suicidal ideation.
Metabolism & Half-life:
Rapidly and well absorbed from GI tract. Protein binding: 90%. Metabolized in liver. Primarily excreted in urine. Minimal removal by hemodialysis.
Half-life: 10–26 hours.
Drug Interactions:
- CNS depressants (e.g., alcohol, morphine, zolpidem) may increase CNS depression.
- May increase CNS depressant effect of azelastine.
- May increase arrhythmogenic effect of dronedarone.
- MAOIs (e.g., phenelzine, selegiline) may increase the serotonergic effect.
- May alter ECG readings (flattened T wave), serum glucose (increase or decrease).
Side- Effects:
- Frequent: Dizziness, drowsiness, dry mouth, orthostatic hypotension, headache, increased appetite, weight gain, nausea, unusual fatigue, unpleasant taste.
- Occasional: Blurred vision, confusion, constipation, hallucinations, delayed micturition, eye pain, arrhythmias, fine muscle tremors, parkinsonian syndrome, anxiety, diarrhea, diaphoresis, heartburn, insomnia.
- Rare: Hypersensitivity, alopecia, tinnitus, breast enlargement, photosensitivity.
Nursing Considerations
Baseline assessment
- Observe and record behavior.
- Assess psychological status, thought content, suicidal ideation, sleep patterns, appearance, interest in environment.
- For pts on long-term therapy, hepatic/renal function tests, blood counts should be performed periodically.
Intervention/evaluation
- Supervise suicidal risk pt closely during early therapy (as depression lessens, energy level improves, increasing suicide potential).
- Assess appearance, behavior, speech pattern, level of interest, mood.
- Monitor B/P for hypotension, pulse, arrhythmias.
- Therapeutic serum level: Peak: 120–250 ng/mL; toxic serum level: greater than 500 ng/mL.
Patient/family teaching
- Go slowly from lying to standing.
- Tolerance to postural hypotension, sedative and anticholinergic effects usually develops during early therapy.
- Maximum therapeutic effect may be noted in 2–4 wks.
- Sensitivity to sun may occur.
- Report visual disturbances.
- Do not abruptly discontinue medication.
- Avoid tasks that require alertness, motor skills until response to drug is established.
- Avoid alcohol.
- Sips of water may relieve dry mouth.
2. Clomipramine
| CLOMIPRAMINE |
| Availability: Capsules: 25 mg, 50 mg, 75 mg.; Aerosol foam: 1% |
| Administration/handling: PO: May give with food to decrease risk of GI disturbance. • Recommend bedtime administration. Don’t give with grapefruit juice. Once stabilizing dosage is reached, entire daily dose may be given at bedtime. Following dose titration, may give once-daily dose at bedtime. |
| Obsessive-Compulsive Disorder (OCD): PO: Adults, elderly: Initially, 25 mg/day. May gradually increase to 100 mg/day in divided doses in the first 2 wks. Maintenance: After initial titration, wait 2–3 weeks between dosing. May further increase up to 250 mg/day at bedtime. Maximum: 250 mg/day. Children 10 yrs and older: Initially, 25 mg/day. May gradually increase up to maximum of 3 mg/kg/day or 100 mg in divided doses (whichever is lowest). Maintenance: After initial titration, wait 2–3 weeks between dosing. May further increase to 3 mg/kg or 200 mg/ day at bedtime (whichever is less) |
Mechanism of Action:
Blocks reuptake of neurotransmitters (norepinephrine, serotonin) at CNS presynaptic membranes, increasing availability at postsynaptic receptor sites. Therapeutic Effect: Reduces obsessive-compulsive behavior.
Indications:
- Obsessive-Compulsive Disorder (OCD)
- Off-label uses: Panic disorder
- Depression
Cautions & Contraindications:
- Hypersensitivity to clomipramine, other tricyclic agents.
- Acute recovery period after MI
- Use of maois intended for psychiatric disorders (concurrently or within 14 days of discontinuing either clomipramine or MAOI).
- Initiation in pts receiving linezolid or methylene blue.
- Cautions: pts at high risk for suicide, prostatic hypertrophy, history of urinary retention/obstruction, narrow angle glaucoma, seizures, cardiovascular/ hepatic/renal disease, hyperthyroidism, alcoholism, xerostomia, visual problems, elderly, constipation, history of bowel obstruction. Tumors of the adrenal medulla (e.G., Pheochromocytoma).
Metabolism and Half- Life:
Rapidly absorbed. Metabolized in liver. Eliminated in urine (51%–60%), feces (24%–32%). Half-life: 20–30 hrs.
Drug Interactions:
- Alcohol, other CNS depressants may increase CNS, respiratory depression, hypotensive effect.
- CNS depressants may increase CNS depression.
- Strong CYP2C19, CYP2D6 inhibitors may increase concentration/effect.
- Linezolid, MAOIs (e.g., selegiline, phenelzine) may increase serotonergic effect.
- Anticholinergics may increase anticholinergic effect.
- Grapefruit products may increase concentration, toxicity.
- May alter serum glucose, ECG readings.
Side effects
- Ejaculatory failure
- Dry mouth
- Somnolence
- Tremors
- Dizziness, headache
- Constipation
- Fatigue, nausea.
- Impotence, diaphoresis, dyspepsia, sexual dysfunction, dysmenorrhea, nervousness, weight gain, pharyngitis.
- Rare (less than 5%): diarrhea, myalgia, rhinitis, increased appetite, paresthesia, memory impairment, anxiety, rash, pruritus, anorexia, abdominal pain, vomiting, flatulence, flushing, UTI, back pain
Nursing Considerations
Baseline assessment
Assess psychological status, thought content, level of interest, mood, behavior, suicidal ideation.
Intervention/evaluation
- Supervise suicidal-risk pt closely during early therapy (as depression lessens, energy level improves, increasing suicide potential).
- Assess appearance, behavior, speech pattern, level of interest, mood.
Patient/family teaching
- May cause dry mouth, constipation, blurred vision.
- Avoid tasks that require alertness, motor skills until response to drug is established.
- Tolerance to postural hypotension, sedative, anticholinergic effects usually develop during early therapy.
- Maximum therapeutic effect may be noted in 2–4 wks.
- Do not abruptly discontinue medication.
- Daily dose may be given at bedtime to minimize daytime sedation.
- Avoid alcohol.
•Report worsening depression, suicidal ideation, change in behavior.
3. Doxepin
| Doxepin |
| Availability: Capsules: 10 mg, 25 mg, 50 mg, 75 mg, 100 mg, 150 mg Cream (topical): 5% in 30-g tube; Oral concentrate: 10 mg/ml ; Tablets: 3 mg, 6 mg |
| Administration/handling: PO • Give with food, milk if GI distress occurs. • Dilute concentrate in 4-oz glass of water, milk, or orange, tomato, prune, pineapple juice. Incompatible with carbonated drinks. • Give larger portion of daily dose at bedtime. Topical • Apply thin film of cream on affected areas of skin. • Do not use for more than 8 days. • Do not use occlusive dressing |
| Depression, Anxiety Note: Gradually taper dose upon discontinuation of antidepressant therapy. PO: ADULTS: Initially, 25–50 mg/day at bedtime or in 2–3 divided doses. May increase gradually to usual dose of 100 mg–300 mg/day (single dose should not exceed 150 mg). ELDERLY: Initially 10–25 mg at bedtime. May increase by 10–25 mg/day every 3–7 days. |
| Insomnia: PO: Adults: 3–6 mg (give within 30 min of bedtime). Elderly: 3 mg (give within 30 min of bedtime). May increase to 6 mg once daily. |
| Pruritus Associated with Atopic Dermatitis: Topical: Adults, elderly: Apply thin film 4 times/day at 3- to 4-hr intervals. Not recommended for more than 8 days. |
Mechanism of Action:
Increases synaptic concentrations of norepinephrine, serotonin by inhibiting reuptake. Therapeutic Effect: Produces antidepressant, anxiolytic effects.
Indications:
- Treatment of depression and/or anxiety.
- Treatment of insomnia in pts with difficulty staying asleep.
- Topical: Treatment of pruritus associated with atopic dermatitis.
- OFF-LABEL: Treatment of neurogenic pain, treatment of anxiety
Cautions & Contraindications:
- Hypersensitivity to doxepin.
- Glaucoma
- Hypersensitivity to other tricyclic antidepressants
- Urinary retention
- Use of maois within 14 days.
- Cautions: cardiac/hepatic/renal disease, pts at risk for suicidal ideation, respiratory compromise, sleep apnea, history of bowel obstruction, increased IOP, glaucoma, history of seizures, history of urinary retention/ obstruction, hyperthyroidism, prostatic hypertrophy, hiatal hernia, elderly
Metabolism And Half- Life:
PO: Rapidly absorbed from GI tract. Protein binding: 80%–85%. Metabolized in liver. Primarily excreted in urine. Not removed by hemodialysis.
Half-life: 6–8 hrs. Topical: Absorbed through skin. Distributed to body tissues. Metabolized to active metabolite. Excreted in urine.
Drug Interactions:
- Alcohol, other CNS depressants (e.g., lorazepam, morphine, zolpidem) may increase CNS, respiratory depression.
- MAOIs (e.g., phenelzine, selegiline) may increase risk of seizures, hyperpyrexia, hypertensive crisis (discontinue at least 2 wks prior to starting doxepin).
- Anticholinergic agents (e.g., aclidinium, ipratropium, umeclidinium) may increase anticholinergic effect.
- May increase QT interval-prolonging effect of dronedarone.
- Strong CYP2D6 inhibitors (e.g., bupropion, Paroxetine) may increase concentration/effect.
Side Effects
Frequent:
- PO: Orthostatic hypotension, drowsiness, dry mouth, headache, increased appetite, weight gain, nausea, unusual fatigue, unpleasant taste.
- Topical: Edema, increased pruritus, eczema, burning, tingling, stinging at application site, altered taste, dizziness, drowsiness, dry skin, dry mouth, fatigue, headache, thirst.
Occasional:
- PO: Blurred vision, confusion, constipation, hallucinations, difficult urination, eye pain, irregular heartbeat, fine muscle tremors, nervousness, impaired sexual function, diarrhea, diaphoresis, heartburn, insomnia.
- Silenor: Nausea, upper respiratory infection.
- Topical: Anxiety, skin irritation/cracking, nausea. Rare: PO: Allergic reaction, alopecia, tinnitus, breast enlargement. Topical: Fever, photosensitivity
Nursing Considerations
Baseline assessment
- Assess B/P, pulse, ECG (those with history of cardiovascular disease).
- Perform CBC, serum electrolyte tests before long-term therapy.
- Assess pt’s appearance, behavior, level of interest, mood, suicidal ideation, sleep pattern.
Intervention/evaluation
- Monitor B/P, pulse, weight.
- Perform CBC, serum electrolyte tests periodically to assess renal/hepatic function.
- Monitor mental status, suicidal ideation. Supervise suicidal risk pt closely during early therapy (as depression lessens, energy level improves, increasing suicide potential).
- Assess appearance, behavior, speech pattern, level of interest, mood.
- Therapeutic serum level: 110–250 ng/mL; toxic serum level: greater than 300 ng/mL.
Patient/family teaching
- Do not discontinue abruptly.
- Change positions slowly to avoid dizziness.
- Avoid tasks that require alertness, motor skills until response to drug is established.
- Do not cover affected area with occlusive dressing after applying cream.
- May cause dry mouth.
- Avoid alcohol, limit caffeine.
- May increase appetite.
- Avoid exposure to sunlight/ artificial light source.
- Therapeutic effect may be noted within 2–5 days, maximum effect within 2–3 wks.
- Report worsening depression, suicidal ideation, unusual changes in behavior (esp. at initiation of therapy or with changes in dosage).
4.Bupropion
| Bupropion |
| Availability: Tablets: 75 mg, 100 mg. Tablets, Extended-Release (24 hr): (Aplenzin): 174 mg, 348 mg, 522 mg (Forfivo XL): 450 mg (Wellbutrin XL): 150 mg, 300 mg. Tablets, Sustained-Release (12 hr): (Wellbutrin SR): 100 mg, 150 mg, 200 mg; (Zyban): 150 mg |
| Administration/handling: PO • Give without regard to food (give with food if GI irritation occurs). • Give at least 4-hr interval for immediate onset and 8-hr interval for sustained-release tablet to avoid seizures. • Give Aplenzin once daily in the morning. • Avoid bedtime dosage (decreases risk of insomnia). • Do not break, crush, dissolve, or divide sustained-, extended-release preparations. |
| Depression PO: (Immediate-Release): Adults, elderly: Initially, 100 mg twice daily. May increase to 100 mg 3 times/day no sooner than 3 days after beginning therapy. Maximum: 150 mg 3 times/day. PO: (Sustained-Release): Adults, elderly: Initially, 150 mg/day as a single dose in the morning. May increase to 150 mg twice daily as early as day 4 after beginning therapy. Maximum: 400 mg/ day in 2 divided doses. PO: (Extended-Release): Adults, elderly: 150 mg once daily. May increase to 300 mg once daily as early as day 4. If no clinical improvement after 2 wks, may increase to 450 mg once daily. Maximum: 450 mg/day. (Aplenzin): Initially, 174 mg once daily in morning; may increase as soon as 4 days to 348 mg/day. |
| Smoking Cessation PO: Adults, elderly: (Zyban): Initially, 150 mg/day for 3 days, then 150 mg twice daily for 7–12 wks. |
| SAD PO: Adults, elderly: (Wellbutrin XL): 150 mg/day for 1 wk, then 300 mg/day. Begin in autumn (Sept–Nov). End of treatment begins in spring (Mar–Apr) by decreasing dose to 150 mg/day for 2 wks before discontinuation. (Aplenzin): 174 mg once daily. May increase after 1 wk to 348 mg once daily |
Mechanism of Action:
Blocks reuptake of neurotransmitters, (Dopamine, norepinephrine) at CNS presynaptic membranes.
Therapeutic Effect: Relieves depression. Eliminates nicotine withdrawal symptoms.
Indications:
- Treatment of major depressive disorder (MDD)
- Seasonal affective disorder (SAD)
- Smoking cessation.
- OFF-LABEL: treatment of ADHD in adults, children.
- Depression associated with bipolar disorder.
Cautions & Contraindications:
- Hypersensitivity to bupropion.
- Current or prior diagnosis of anorexia nervosa or bulimia
- seizure disorder
- Use of MAO inhibitors (concurrently or within 14 days of discontinuing either bupropion or the MAOI)
- Pts undergoing abrupt discontinuation of alcohol or sedatives.
- Initiation of bupropion in pts receiving linezolid or IV methylene blue.
- Cautions: history of seizure, cranial or head trauma, cardiovascular disease, history of hypertension or coronary artery disease, elderly, pts at high risk for suicide, renal/hepatic impairment. Concurrent use of antipsychotics, antidepressants, theophylline, steroids, stimulants, hypoglycemic agents, excessive use of alcohol, sedatives/hypnotics, opioids.
Metabolism and Half- Life:
Rapidly absorbed from GI tract. Protein binding: 84%. Crosses the blood-brain barrier. Metabolized in liver. Primarily excreted in urine. Half-life: 14 hrs.
Drug Interactions:
- CNS depressants (e.g., alcohol, morphine, oxycodone, zolpidem) may increase CNS depressant effect.
- MAOIs (e.g., phenelzine, selegiline) may increase hypertensive effect.
- May decrease concentration of tamoxifen.
- May increase concentration of metoclopramide, thioridazine.
- May increase adverse effects of citalopram, vortioxetine.
Side- Effects:
Frequent: Constipation, weight gain or loss, nausea, vomiting, anorexia, dry mouth, headache, diaphoresis, tremor, sedation, insomnia, dizziness, agitation.
Occasional: Diarrhea, akinesia, blurred vision, tachycardia, confusion, hostility, fatigue
Nursing Considerations
Baseline assessment
- Assess psychological status, thought content, suicidal tendencies, appearance.
- For pts on long-term therapy, hepatic/ renal function tests should be performed periodically.
Intervention/evaluation
- Supervise suicidal risk pt closely during early therapy and dose changes (as depression lessens, energy level improves, increasing suicide potential).
- Assess appearance, behavior, speech pattern, level of interest, mood changes.
Patient/family teaching
- Full therapeutic effect may be noted in 4 wks.
- Avoid tasks that require alertness, motor skills until response to drug is established.
- Report signs/symptoms of seizure, worsening depression, suicidal ideation, unusual behavioral changes.
- Avoid alcohol. • Do not chew, crush, dissolve, or divide sustained-, extended-release table
REFERENCES
- Robert Kizior, Keith Hodgson, Saunders Nursing Drug handbook,1st edition 2024, Elsevier Publications. ISBN-9780443116070
- McGraw Hill- Drug Handbook, Seventh Edition, 2013, McGraw Hill Education Publications,9780071799430.
- April Hazard, Cynthia Sanoski, Davi’s Drug Guide for Nurses -Sixteenth Edition 2019, FA Davis Company Publications,9780803669451.
- Jones and Bartlet, Pharmacology for Nurses, Second Edition, 2020, Jones and Bartlet Learning Publications, ISBN 9781284141986.
- Nursebro.com, Search – Nursebro
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