Sinequan 100mg (hundred Mg) Capsule
WARNING: Drugs like this one have raised the chance of suicidal thoughts or actions in children and young adults. The risk may be greater in people who have had these thoughts or actions in the past. All people who take this drug need to be watched closely. Call the doctor right away if signs like depression, nervousness, restlessness, grouchiness, panic attacks, or changes in mood or actions are new or worse. Call the doctor right away if any thoughts or actions of suicide occur.This drug is not approved for use in children. Talk with the doctor. @ COMMON USES: It is used to treat depression.It is used to treat anxiety.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Antidepressant; Anxiolytic; Hypnotic; Antipruritic
Pharmacologic Class
Tricyclic Antidepressant (TCA); Histamine H1 Receptor Antagonist
Pregnancy Category
C
FDA Approved
Sep 1969
DEA Schedule
Not Controlled
Overview
What is this medicine?
Doxepin is a medication used to treat depression and anxiety. At lower doses, it can also be used to help with sleep problems (insomnia) or severe itching. It works by affecting certain natural chemicals in the brain that help regulate mood, sleep, and other body functions. It belongs to a group of medicines called tricyclic antidepressants.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, it's essential to follow your doctor's instructions carefully. Read all the information provided with your medication and follow the instructions closely. If you're taking this medication once a day, take it at bedtime. Continue taking your medication as directed by your doctor or healthcare provider, even if you're feeling well.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication, store it at room temperature, protected from light, and in a dry place. Avoid storing it in a bathroom. Keep all medications in a secure location, out of the reach of children and pets. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless instructed to do so. Instead, check with your pharmacist for guidance on the best disposal method. You may also want to explore local drug take-back programs in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
To get the most benefit from your medication, it's essential to follow your doctor's instructions carefully. Read all the information provided with your medication and follow the instructions closely. If you're taking this medication once a day, take it at bedtime. Continue taking your medication as directed by your doctor or healthcare provider, even if you're feeling well.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication, store it at room temperature, protected from light, and in a dry place. Avoid storing it in a bathroom. Keep all medications in a secure location, out of the reach of children and pets. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless instructed to do so. Instead, check with your pharmacist for guidance on the best disposal method. You may also want to explore local drug take-back programs in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for the missed one.
Lifestyle & Tips
- Avoid alcohol and other CNS depressants (e.g., sedatives, tranquilizers) as they can increase drowsiness and dizziness.
- Be cautious when driving or operating machinery until you know how this medication affects you, as it can cause significant drowsiness and blurred vision.
- To minimize dizziness or lightheadedness when standing up, especially at the start of treatment, get up slowly from a sitting or lying position.
- Maintain good oral hygiene and use sugar-free candies or gum to help with dry mouth.
- Increase fiber and fluid intake to help prevent constipation.
- Do not stop taking this medication suddenly, especially if you have been on it for a long time, as it can cause withdrawal symptoms. Your doctor will guide you on how to slowly reduce the dose.
- Inform your doctor about all other medications, supplements, and herbal products you are taking to avoid potential drug interactions.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Depression/Anxiety: 75-150 mg/day orally, typically divided or as a single bedtime dose. Insomnia (low-dose): 3-6 mg orally once daily at bedtime. Pruritus: 10-30 mg orally at bedtime.
Dose Range:
3 - 300 mg
Condition-Specific Dosing:
depression_anxiety:
Initial: 25-75 mg/day, gradually increase to 75-150 mg/day. Max: 300 mg/day for severe cases.
insomnia:
3-6 mg once daily at bedtime (low-dose formulation, e.g., Silenor).
pruritus:
10-30 mg once daily at bedtime.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not generally recommended for depression/anxiety in children <12 years. Safety and efficacy not established for insomnia in children <18 years.
Adolescent:
Not generally recommended for depression/anxiety in adolescents <18 years due to increased risk of suicidality. Safety and efficacy not established for insomnia in adolescents <18 years.
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment recommended, but monitor for increased side effects.
Moderate:
Consider lower initial doses and slower titration. Monitor for increased side effects.
Severe:
Consider lower initial doses (e.g., 50% of usual starting dose) and slower titration. Monitor closely for adverse effects.
Dialysis:
Doxepin is highly protein-bound and has a large volume of distribution, making it unlikely to be significantly removed by dialysis. No specific recommendations, but monitor for increased side effects.
Hepatic Impairment:
Mild:
No specific dose adjustment recommended, but monitor for increased side effects.
Moderate:
Consider lower initial doses and slower titration. Monitor for increased side effects due to reduced metabolism.
Severe:
Significant dose reduction (e.g., 50-75% of usual dose) is likely necessary. Avoid use if possible. Monitor plasma levels if available and clinically indicated.
Pharmacology
Mechanism of Action
Doxepin is a tricyclic antidepressant (TCA) that primarily inhibits the reuptake of norepinephrine and serotonin at the presynaptic neuronal membrane, thereby increasing the concentration of these neurotransmitters in the synaptic cleft. It also possesses potent antihistaminic (H1), anticholinergic (muscarinic), and alpha-1 adrenergic blocking properties, which contribute to its sedative, anticholinergic, and orthostatic hypotensive side effects, respectively. Its H1 antagonism is particularly strong, contributing to its use in insomnia and pruritus.
Pharmacokinetics
Absorption:
Bioavailability:
Variable, approximately 13-45% due to extensive first-pass metabolism.
Tmax:
Approximately 2-4 hours for doxepin; 2-10 hours for active metabolite (nordoxepin).
FoodEffect:
Food may delay absorption and slightly decrease peak concentrations, but overall extent of absorption is not significantly affected.
Distribution:
Vd:
Large (approximately 9-33 L/kg), indicating extensive tissue distribution.
ProteinBinding:
High (approximately 80-95%), primarily to albumin.
CnssPenetration:
Yes, readily crosses the blood-brain barrier.
Elimination:
HalfLife:
Doxepin: 10-25 hours; Nordoxepin: 28-51 hours.
Clearance:
Not readily available as a single rate, but extensive hepatic metabolism is the primary clearance mechanism.
ExcretionRoute:
Primarily renal (as metabolites).
Unchanged:
<3% (doxepin) and <6% (nordoxepin) excreted unchanged in urine.
Pharmacodynamics
OnsetOfAction:
Antidepressant effects: May take 2-4 weeks. Sedative/Hypnotic effects: Within 30-60 minutes. Antipruritic effects: Within hours to days.
PeakEffect:
Antidepressant effects: 4-6 weeks. Sedative/Hypnotic effects: 1-3 hours after dose.
DurationOfAction:
Sedative/Hypnotic effects: 6-8 hours (low dose). Antidepressant effects: Sustained with daily dosing due to long half-life of parent drug and active metabolite.
Confidence:
Medium
Safety & Warnings
BLACK BOX WARNING
Antidepressants increased the risk compared to placebo of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults in short-term studies of Major Depressive Disorder (MDD) and other psychiatric disorders. Anyone considering the use of doxepin or any other antidepressant in a child, adolescent, or young adult must balance this risk with the clinical need. Short-term studies did not show an increase in the risk of suicidality with antidepressants compared to placebo in adults beyond age 24; there was a reduction in risk with antidepressants compared to placebo in adults aged 65 and older. Depression and certain other psychiatric disorders are themselves associated with increases in the risk of suicide. Patients of all ages who are started on antidepressant therapy should be monitored appropriately and observed closely for clinical worsening, suicidality, or unusual changes in behavior. Families and caregivers should be advised of the need for close observation and communication with the prescriber.
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high or low blood pressure, including:
+ Severe headache or dizziness
+ Passing out
+ Changes in eyesight
Fast heartbeat
Difficulty urinating
Feeling extremely nervous or excitable
Fever, chills, or sore throat
Unexplained bruising or bleeding
Feeling very tired or weak
Yellowing of the skin or eyes (jaundice)
Ringing in the ears (tinnitus)
Changes in sex drive
Enlarged breasts or nipple discharge
Swelling of the testicles
Important Warning for Asthma Patients
If you have asthma, use this medication with caution. Worsening of asthma symptoms has occurred in people taking this medication. If your asthma symptoms worsen while taking this medication, contact your doctor immediately.
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people experience no side effects or only mild ones. However, if you notice any of the following side effects or if they bother you or do not go away, contact your doctor or seek medical help:
Feeling dizzy, sleepy, tired, or weak
Constipation, diarrhea, stomach pain, upset stomach, vomiting, or decreased appetite
Dry mouth
Changes in taste
Mouth irritation or mouth sores
Weight gain
Excessive sweating
Flushing
Hair loss
* Headache
Reporting Side Effects
This is not a comprehensive list of all possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high or low blood pressure, including:
+ Severe headache or dizziness
+ Passing out
+ Changes in eyesight
Fast heartbeat
Difficulty urinating
Feeling extremely nervous or excitable
Fever, chills, or sore throat
Unexplained bruising or bleeding
Feeling very tired or weak
Yellowing of the skin or eyes (jaundice)
Ringing in the ears (tinnitus)
Changes in sex drive
Enlarged breasts or nipple discharge
Swelling of the testicles
Important Warning for Asthma Patients
If you have asthma, use this medication with caution. Worsening of asthma symptoms has occurred in people taking this medication. If your asthma symptoms worsen while taking this medication, contact your doctor immediately.
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people experience no side effects or only mild ones. However, if you notice any of the following side effects or if they bother you or do not go away, contact your doctor or seek medical help:
Feeling dizzy, sleepy, tired, or weak
Constipation, diarrhea, stomach pain, upset stomach, vomiting, or decreased appetite
Dry mouth
Changes in taste
Mouth irritation or mouth sores
Weight gain
Excessive sweating
Flushing
Hair loss
* Headache
Reporting Side Effects
This is not a comprehensive list of all possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Worsening depression or anxiety
- New or worsening thoughts of self-harm or suicide
- Unusual changes in behavior (e.g., agitation, restlessness, panic attacks, irritability, aggression, impulsivity, severe insomnia, hypomania, mania)
- Severe dizziness or fainting spells
- Fast or irregular heartbeat
- Difficulty urinating
- Severe constipation or abdominal pain
- Blurred vision or eye pain
- Muscle stiffness, fever, sweating, confusion (signs of Serotonin Syndrome or Neuroleptic Malignant Syndrome)
- Unexplained fever, sore throat, or other signs of infection (may indicate blood dyscrasia)
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Describe the allergic reaction you experienced, including the symptoms that occurred.
Certain health conditions, including:
+ Difficulty urinating
+ Glaucoma
Current or recent use of specific medications, such as:
+ Linezolid or methylene blue
+ Certain antidepressants or Parkinson's disease medications taken within the last 14 days, including isocarboxazid, phenelzine, tranylcypromine, selegiline, or rasagiline, as they may cause very high blood pressure
Use of other medications that can cause drowsiness, as there are many drugs with this potential effect. If you are unsure, consult your doctor or pharmacist for guidance.
* If you are breastfeeding, as you should not breastfeed while taking this medication.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Describe the allergic reaction you experienced, including the symptoms that occurred.
Certain health conditions, including:
+ Difficulty urinating
+ Glaucoma
Current or recent use of specific medications, such as:
+ Linezolid or methylene blue
+ Certain antidepressants or Parkinson's disease medications taken within the last 14 days, including isocarboxazid, phenelzine, tranylcypromine, selegiline, or rasagiline, as they may cause very high blood pressure
Use of other medications that can cause drowsiness, as there are many drugs with this potential effect. If you are unsure, consult your doctor or pharmacist for guidance.
* If you are breastfeeding, as you should not breastfeed while taking this medication.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Before engaging in activities that require alertness, such as driving, wait until you understand how this drug affects you.
Please note that it may take several weeks to experience the full effects of this medication. Do not abruptly stop taking this drug without consulting your doctor, as this may increase your risk of side effects. If you need to discontinue this medication, your doctor will instruct you on how to gradually stop taking it to minimize potential side effects.
While taking this medication, avoid consuming alcohol and consult your doctor before using marijuana, other forms of cannabis, or prescription or over-the-counter (OTC) drugs that may cause drowsiness or impair your reactions.
Some individuals may be at a higher risk of developing eye problems while taking this medication. Your doctor may recommend an eye exam to assess your risk. If you experience eye pain, changes in vision, or swelling and redness in or around the eye, contact your doctor immediately.
This medication may increase your sensitivity to the sun, making you more prone to sunburn. Take necessary precautions when spending time outdoors, and inform your doctor if you experience excessive sunburn while taking this medication.
If you have diabetes (high blood sugar), closely monitor your blood sugar levels. Be aware of the signs of high or low blood sugar, which may include fruity-smelling breath, dizziness, rapid breathing, rapid heartbeat, confusion, drowsiness, weakness, flushing, headache, unusual thirst or hunger, frequent urination, shaking, or sweating. If you experience any of these symptoms, notify your doctor.
Older adults (65 years and older) should use this medication with caution, as they may be more susceptible to side effects.
Certain medications, including this one, may affect fertility and the ability to conceive. If you have concerns or questions, discuss them with your doctor.
If you are pregnant or plan to become pregnant, consult your doctor to weigh the benefits and risks of taking this medication during pregnancy. Taking this drug in the third trimester may lead to health problems in the newborn, so it is crucial to discuss this with your doctor.
Please note that it may take several weeks to experience the full effects of this medication. Do not abruptly stop taking this drug without consulting your doctor, as this may increase your risk of side effects. If you need to discontinue this medication, your doctor will instruct you on how to gradually stop taking it to minimize potential side effects.
While taking this medication, avoid consuming alcohol and consult your doctor before using marijuana, other forms of cannabis, or prescription or over-the-counter (OTC) drugs that may cause drowsiness or impair your reactions.
Some individuals may be at a higher risk of developing eye problems while taking this medication. Your doctor may recommend an eye exam to assess your risk. If you experience eye pain, changes in vision, or swelling and redness in or around the eye, contact your doctor immediately.
This medication may increase your sensitivity to the sun, making you more prone to sunburn. Take necessary precautions when spending time outdoors, and inform your doctor if you experience excessive sunburn while taking this medication.
If you have diabetes (high blood sugar), closely monitor your blood sugar levels. Be aware of the signs of high or low blood sugar, which may include fruity-smelling breath, dizziness, rapid breathing, rapid heartbeat, confusion, drowsiness, weakness, flushing, headache, unusual thirst or hunger, frequent urination, shaking, or sweating. If you experience any of these symptoms, notify your doctor.
Older adults (65 years and older) should use this medication with caution, as they may be more susceptible to side effects.
Certain medications, including this one, may affect fertility and the ability to conceive. If you have concerns or questions, discuss them with your doctor.
If you are pregnant or plan to become pregnant, consult your doctor to weigh the benefits and risks of taking this medication during pregnancy. Taking this drug in the third trimester may lead to health problems in the newborn, so it is crucial to discuss this with your doctor.
Overdose Information
Overdose Symptoms:
- Severe drowsiness or coma
- Confusion, disorientation, hallucinations
- Severe dry mouth, blurred vision, dilated pupils
- Fast, irregular, or pounding heartbeat (tachycardia, arrhythmias)
- Low blood pressure (hypotension)
- Seizures
- Respiratory depression (slow, shallow breathing)
- Urinary retention
- Hypothermia
- Muscle rigidity, hyperreflexia
What to Do:
Seek immediate medical attention. Call 911 or your local emergency number. For poison control, call 1-800-222-1222. Treatment is supportive and symptomatic, including gastric lavage, activated charcoal, and monitoring of cardiac function (ECG) and vital signs. Physostigmine may be used for severe anticholinergic toxicity, but with caution due to potential for cardiac effects.
Drug Interactions
Contraindicated Interactions
- Monoamine Oxidase Inhibitors (MAOIs) - risk of serotonin syndrome, hyperpyretic crises, convulsions, and death.
- Cisapride - risk of QT prolongation and arrhythmias.
- Pimozide - risk of QT prolongation and arrhythmias.
- Linezolid - weak MAOI activity, risk of serotonin syndrome.
- Methylene blue (IV) - weak MAOI activity, risk of serotonin syndrome.
Major Interactions
- Other CNS depressants (e.g., alcohol, benzodiazepines, opioids, sedatives, hypnotics) - additive CNS depression.
- Anticholinergic agents (e.g., atropine, benztropine, diphenhydramine, oxybutynin) - additive anticholinergic effects (e.g., severe constipation, urinary retention, blurred vision, delirium).
- Adrenergic neuron blocking agents (e.g., guanethidine, clonidine, reserpine) - may block antihypertensive effects.
- Sympathomimetics (e.g., epinephrine, norepinephrine, phenylephrine) - potentiate pressor response.
- CYP2D6 inhibitors (e.g., fluoxetine, paroxetine, quinidine, bupropion) - significantly increase doxepin and nordoxepin plasma concentrations, increasing risk of toxicity.
- Thyroid hormones - increased risk of cardiac arrhythmias and toxicity.
- Cimetidine - inhibits doxepin metabolism, increasing plasma levels.
- Tramadol - increased risk of seizures and serotonin syndrome.
- Serotonergic drugs (e.g., SSRIs, SNRIs, triptans, fentanyl, lithium, St. John's Wort) - increased risk of serotonin syndrome.
Moderate Interactions
- Anticoagulants (e.g., warfarin) - TCAs may potentiate anticoagulant effects, monitor INR.
- Anticonvulsants - TCAs may lower seizure threshold; anticonvulsant levels may be altered.
- Disulfiram - may inhibit doxepin metabolism.
- Oral contraceptives - may alter TCA metabolism.
- Tobacco smoking - may induce CYP1A2, potentially reducing doxepin levels.
Minor Interactions
- Not specifically categorized as minor, but general caution with any drug affecting CNS or hepatic metabolism.
Monitoring
Baseline Monitoring
Complete Blood Count (CBC) with differential
Rationale: To establish baseline and monitor for rare but serious blood dyscrasias (e.g., agranulocytosis, thrombocytopenia).
Timing: Prior to initiation
Electrocardiogram (ECG)
Rationale: To assess for pre-existing cardiac conduction abnormalities, especially in elderly patients or those with cardiac disease, due to risk of QT prolongation and other arrhythmias.
Timing: Prior to initiation, especially in patients >40 years old or with cardiac risk factors
Liver Function Tests (LFTs)
Rationale: To establish baseline and monitor for hepatic dysfunction, as doxepin is extensively metabolized by the liver.
Timing: Prior to initiation
Renal Function Tests (BUN, Creatinine)
Rationale: To assess baseline renal function, as metabolites are renally excreted and dose adjustments may be needed in severe impairment.
Timing: Prior to initiation
Blood Pressure (BP) and Heart Rate (HR)
Rationale: To establish baseline and monitor for orthostatic hypotension and tachycardia.
Timing: Prior to initiation (supine and standing BP)
Mental Status Examination (MSE) / Suicidality Assessment
Rationale: To establish baseline mood, thought content, and assess for suicidal ideation, especially in young adults.
Timing: Prior to initiation and at each visit during early treatment
Routine Monitoring
Mental Status Examination (MSE) / Suicidality Assessment
Frequency: Weekly for first 4 weeks, then every 2 weeks for next 4 weeks, then monthly for 3 months, then periodically as clinically indicated, especially during dose changes.
Target: Improvement in target symptoms without emergence or worsening of suicidal ideation/behavior.
Action Threshold: Any new or worsening suicidal ideation, agitation, or unusual changes in behavior require immediate assessment and intervention.
Blood Pressure (BP) and Heart Rate (HR)
Frequency: Periodically, especially during dose titration and in elderly patients or those prone to orthostatic hypotension.
Target: Maintain within patient's normal range, minimize orthostatic drop.
Action Threshold: Significant orthostatic hypotension (e.g., >20 mmHg systolic drop) or persistent tachycardia.
Anticholinergic side effects (e.g., dry mouth, constipation, urinary retention, blurred vision)
Frequency: At each visit, especially during dose titration.
Target: Minimize discomfort.
Action Threshold: Severe or intolerable symptoms, or signs of urinary retention/ileus.
Sedation/Drowsiness
Frequency: At each visit, especially during dose titration.
Target: Acceptable level of sedation, not interfering with daily activities (unless used for insomnia).
Action Threshold: Excessive sedation, impaired alertness, or falls.
Therapeutic Drug Monitoring (TDM) - Doxepin and Nordoxepin levels
Frequency: Not routinely recommended for all patients, but may be useful in cases of suspected non-adherence, poor response, or toxicity, especially in elderly or renally/hepatically impaired patients.
Target: Combined plasma levels of doxepin and nordoxepin for antidepressant effect: 100-250 ng/mL. (Note: Therapeutic ranges are not definitively established for all indications and can vary by lab).
Action Threshold: Levels significantly outside therapeutic range, or signs of toxicity despite 'normal' levels.
Symptom Monitoring
- Worsening depression
- Emergence of suicidal thoughts or behavior
- Unusual changes in behavior (e.g., agitation, irritability, aggression, panic attacks, insomnia, impulsivity, akathisia, hypomania, mania)
- Orthostatic hypotension (dizziness upon standing)
- Dry mouth
- Constipation
- Urinary retention
- Blurred vision
- Sedation/Drowsiness
- Confusion or delirium (especially in elderly)
- Tremor
- Nausea/Vomiting
- Weight gain
- Cardiac symptoms (e.g., palpitations, chest pain, syncope)
Special Patient Groups
Pregnancy
Doxepin is Pregnancy Category C. Use during pregnancy should only be considered if the potential benefit justifies the potential risk to the fetus. Neonates exposed to TCAs during the third trimester have developed withdrawal symptoms (e.g., respiratory distress, cyanosis, apnea, seizures, feeding difficulties, hypotonia, hypertonia, tremor, jitteriness, irritability, constant crying).
Trimester-Specific Risks:
First Trimester:
Limited human data, but animal studies show some evidence of embryotoxicity/teratogenicity at high doses. Risk of major birth defects is generally considered low, but caution is advised.
Second Trimester:
Risk of withdrawal symptoms in neonates increases with exposure later in pregnancy.
Third Trimester:
Increased risk of neonatal withdrawal syndrome and persistent pulmonary hypertension of the newborn (PPHN) if exposed close to delivery. Monitor neonate for symptoms.
Lactation
Doxepin and its active metabolite (nordoxepin) are excreted into breast milk. Due to the potential for serious adverse reactions in breastfed infants (e.g., sedation, poor feeding, irritability, anticholinergic effects), a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. If breastfeeding, monitor the infant closely for sedation, poor feeding, and weight gain.
Infant Risk:
Moderate to High (L3/L4) - Potential for sedation, poor feeding, irritability, and anticholinergic effects in the infant. Long half-life of active metabolite increases concern.
Pediatric Use
Not approved for depression or anxiety in children and adolescents due to increased risk of suicidality. Safety and efficacy for insomnia (low-dose) not established in children <18 years. Use in pediatric patients should be approached with extreme caution and only after careful consideration of risks vs. benefits.
Geriatric Use
Elderly patients are more sensitive to the anticholinergic, sedative, and orthostatic hypotensive effects of doxepin. Start with lower doses (e.g., 10-25 mg/day for depression/anxiety, 3 mg for insomnia) and titrate slowly. Monitor closely for falls, confusion, urinary retention, and cardiac effects. The Beers Criteria recommend avoiding TCAs in older adults due to highly anticholinergic properties, risk of orthostatic hypotension, and sedation.
Clinical Information
Clinical Pearls
- Doxepin is one of the most sedating TCAs due to its potent H1 antagonism, making it useful for insomnia and pruritus at lower doses.
- The 100mg capsule is typically used for depression/anxiety, while very low doses (3mg, 6mg) are specifically formulated for insomnia (Silenor). Ensure correct formulation and dose for the intended indication.
- Due to its anticholinergic properties, doxepin can worsen conditions like benign prostatic hyperplasia (BPH), narrow-angle glaucoma, and severe constipation.
- Orthostatic hypotension is a common side effect, especially in the elderly; advise patients to rise slowly.
- Full antidepressant effects may take several weeks to develop, but sedative effects are immediate. Manage patient expectations.
- Withdrawal symptoms can occur if discontinued abruptly; taper dose gradually over several weeks.
- Monitor for signs of serotonin syndrome, especially if co-administered with other serotonergic agents.
Alternative Therapies
- For Depression/Anxiety: SSRIs (e.g., fluoxetine, sertraline, escitalopram), SNRIs (e.g., venlafaxine, duloxetine), Atypical Antidepressants (e.g., bupropion, mirtazapine), other TCAs (e.g., amitriptyline, imipramine, nortriptyline).
- For Insomnia: Other hypnotics (e.g., zolpidem, eszopiclone, ramelteon), benzodiazepines (short-term), trazodone, mirtazapine, cognitive behavioral therapy for insomnia (CBT-I).
- For Pruritus: Antihistamines (e.g., hydroxyzine, diphenhydramine), topical corticosteroids, other antipruritics.
Cost & Coverage
Average Cost:
Varies widely, typically $10-$50 per 30 capsules (100mg)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (Generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication.
This medication is accompanied by a Medication Guide, which provides crucial information about its use. Please read this guide carefully and review it again whenever you receive a refill. If you have any questions or concerns about this medication, don't hesitate to consult with your doctor, pharmacist, or other healthcare provider.
In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When reporting the incident, be prepared to provide details about the medication taken, the amount, and the time it occurred.
This medication is accompanied by a Medication Guide, which provides crucial information about its use. Please read this guide carefully and review it again whenever you receive a refill. If you have any questions or concerns about this medication, don't hesitate to consult with your doctor, pharmacist, or other healthcare provider.
In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When reporting the incident, be prepared to provide details about the medication taken, the amount, and the time it occurred.