Amitriptyline 75mg Tablets

Amitriptyline is a tertiary amine tricyclic antidepressant (TCA). It primarily inhibits the reuptake of norepinephrine (NE) and serotonin (5-HT) into presynaptic neurons, thereby increasing the concentrations of these neurotransmitters in the synaptic cleft. It also has significant anticholinergic (muscarinic), antihistaminic (H1), and alpha1-adrenergic blocking properties, which contribute to its side effect profile.

Serious Side Effects: Seek Medical Help Right Away

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you experience any of the following symptoms, contact your doctor or seek medical attention immediately:

Signs of an allergic reaction: 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, or swelling of the mouth, face, lips, tongue, or throat
Signs of high or low blood pressure: severe headache, dizziness, fainting, or changes in vision
Signs of liver problems: dark urine, fatigue, decreased appetite, stomach pain or upset, light-colored stools, vomiting, or yellowing of the skin or eyes
Weakness on one side of the body, difficulty speaking or thinking, balance problems, drooping on one side of the face, or blurred vision
Chest pain or pressure, rapid or irregular heartbeat
Confusion, difficulty focusing, or changes in behavior
Urination problems
Fever, chills, sore throat, unexplained bruising or bleeding, or excessive fatigue or weakness
Swelling, shakiness, seizures, or hallucinations (seeing or hearing things that are not there)
Abnormal sensations such as burning, numbness, or tingling
Changes in sex drive
Erectile dysfunction
Swelling of the testicles, enlarged breasts, or nipple discharge
Severe constipation or stomach pain, which may be signs of a serious bowel problem
Inability to sweat during physical activity or in warm temperatures
Sleep disturbances, bad dreams, ringing in the ears, or changes in tongue color
Excessive sweating, joint pain, or hair loss

Other Possible Side Effects

Like all medications, this drug can cause side effects. Many people experience no side effects or only mild ones. If you experience any of the following side effects or any other unusual symptoms, contact your doctor for advice:

Constipation, diarrhea, stomach pain, upset stomach, vomiting, or decreased appetite
Dizziness, drowsiness, fatigue, or weakness
Dry mouth, headache, anxiety, or nervousness
* Changes in taste, weight gain or loss, or mouth sores

Reporting Side Effects

This list is not exhaustive, and you may experience other 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.

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. Be sure to describe the allergic reaction you experienced.
If you have recently had a heart attack.
If you have taken certain medications for depression or Parkinson's disease within the last 14 days, including isocarboxazid, phenelzine, tranylcypromine, selegiline, or rasagiline, as this may lead to very high blood pressure.
If you are currently taking linezolid, methylene blue, or cisapride, as these medications may interact with this drug.

This list is not exhaustive, and it is crucial to disclose all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, as well as any health problems you may have. Your doctor and pharmacist need this information to ensure it is safe for you 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.

Important Warnings and Precautions

Before taking this medication, inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are using this drug. Your doctor may advise you to stop taking this medication before certain surgical procedures. If you need to stop taking this drug, your doctor will provide guidance on when to resume taking it after your surgery or procedure.

Caution with Daily Activities

Until you know how this medication affects you, avoid driving and other activities that require alertness. To minimize the risk of dizziness or fainting, get up slowly from a sitting or lying down position. Be cautious when climbing stairs.

Discontinuing the Medication

Do not stop taking this medication abruptly without consulting your doctor, as this may increase the risk of withdrawal symptoms. If you need to discontinue this drug, your doctor will instruct you on how to gradually stop taking it.

Monitoring Blood Sugar Levels

If you have diabetes (high blood sugar), closely monitor your blood sugar levels while taking this medication. Notify your doctor if you experience symptoms of high or low blood sugar, such as:

Fruity-smelling breath
Dizziness
Rapid breathing
Rapid heartbeat
Confusion
Drowsiness
Weakness
Flushing
Headache
Increased thirst or hunger
Frequent urination
Shaking
Sweating

Interactions with Other Substances

Before consuming alcohol, marijuana, or other forms of cannabis, or taking prescription or over-the-counter medications that may cause drowsiness, consult your doctor.

Eye Problems

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. Immediately report any eye pain, changes in vision, or swelling and redness around the eye to your doctor.

Sun Sensitivity

This medication may increase your risk of sunburn. Take precautions when exposed to sunlight, and inform your doctor if you experience excessive sunburn.

Heat and Fluid Loss

Be cautious in hot weather or during physical activity, and drink plenty of fluids to prevent dehydration.

Muscle Problems

There is a risk of developing a severe muscle condition called tardive dyskinesia, which may be irreversible. This risk is higher in individuals with diabetes, older adults, especially older females, and those taking higher doses or using the medication for an extended period. Notify your doctor immediately if you experience:

Uncontrolled body movements
Tongue sticking out
Puffing cheeks
Mouth puckering
Chewing problems

Special Considerations

If you are 65 years or older, use this medication with caution, as you may be more susceptible to side effects.

Pregnancy and Breastfeeding

Inform your doctor if you are pregnant, plan to become pregnant, or are breastfeeding. Discuss the potential benefits and risks of this medication to you and your baby.

• Monoamine Oxidase Inhibitors (MAOIs) (concurrent use or within 14 days of MAOI discontinuation)
• Cisapride
• Pimozide
• Thioridazine
• Linezolid (reversible MAOI)

• Other CNS depressants (e.g., alcohol, benzodiazepines, opioids, sedatives) - increased CNS depression
• Anticholinergic agents (e.g., atropine, benztropine, diphenhydramine) - increased anticholinergic effects (e.g., urinary retention, severe constipation, paralytic ileus, delirium)
• QT-prolonging drugs (e.g., antiarrhythmics like quinidine, procainamide; antipsychotics like ziprasidone; certain antibiotics like moxifloxacin) - increased risk of arrhythmias
• Sympathomimetics (e.g., epinephrine, norepinephrine, phenylephrine) - potentiated pressor response
• Thyroid hormones - increased risk of arrhythmias
• CYP2D6 inhibitors (e.g., fluoxetine, paroxetine, quinidine) - increased amitriptyline levels
• CYP2C19 inhibitors (e.g., omeprazole, fluoxetine) - increased amitriptyline levels

• Antihypertensives (e.g., guanethidine, clonidine) - may antagonize hypotensive effects
• Cimetidine - increased amitriptyline levels
• Oral anticoagulants (e.g., warfarin) - may alter anticoagulant effect (monitor INR)
• Tramadol - increased risk of seizures and serotonin syndrome
• St. John's Wort - increased risk of serotonin syndrome
• Tobacco smoking - may decrease amitriptyline levels (CYP1A2 induction)

• Grapefruit juice - may increase amitriptyline levels (CYP3A4 inhibition)
• Valerian - increased sedation

• Orthostatic hypotension (dizziness, lightheadedness upon standing)
• Anticholinergic effects (dry mouth, blurred vision, constipation, urinary retention)
• Sedation/Drowsiness
• Cardiac symptoms (palpitations, chest pain, shortness of breath, fainting)
• Changes in mood or behavior (agitation, irritability, anxiety, mania/hypomania)
• Suicidal ideation or worsening depression (especially in young adults)
• Seizures
• Serotonin syndrome symptoms (agitation, hallucinations, rapid heart rate, fever, sweating, muscle rigidity, tremor, incoordination, nausea, vomiting, diarrhea)
• Neuroleptic Malignant Syndrome (NMS) symptoms (fever, severe muscle rigidity, altered mental status, autonomic instability)

Amitriptyline is Pregnancy Category C. Studies in animals have shown adverse effects on the fetus, but there are no adequate and well-controlled studies in pregnant women. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Neonatal withdrawal symptoms (e.g., respiratory distress, cyanosis, apnea, seizures, feeding difficulties, hypotonia, hypertonia, tremor, jitteriness, irritability, constant crying) have been reported in neonates exposed to TCAs during the third trimester.

Amitriptyline and its active metabolite, nortriptyline, are excreted into breast milk. The American Academy of Pediatrics considers amitriptyline to be a drug for which the effect on the nursing infant is unknown but may be of concern. Monitor infants for sedation, poor feeding, and weight gain. Nortriptyline may be preferred if a TCA is needed during lactation due to lower levels in milk and less active metabolites.

Amitriptyline has a Black Box Warning regarding increased risk of suicidal thoughts and behaviors in children, adolescents, and young adults. Use for depression in pediatric patients is generally not recommended. It is approved for nocturnal enuresis in children 6 years and older. Off-label use for neuropathic pain or migraine prophylaxis in adolescents should be carefully considered with close monitoring.

Elderly patients are more sensitive to the anticholinergic, sedative, and hypotensive effects of amitriptyline. They are also at increased risk for cardiac conduction abnormalities and falls. Lower starting doses and slower titration are recommended. Monitor closely for adverse effects, especially orthostatic hypotension, urinary retention, constipation, and cognitive impairment.

• Amitriptyline is a highly sedating TCA; therefore, it is often dosed at bedtime to minimize daytime drowsiness and leverage its sedative properties for sleep improvement.
• Due to its significant anticholinergic effects, it should be used with extreme caution or avoided in patients with benign prostatic hyperplasia (BPH), narrow-angle glaucoma, or severe constipation.
• The antidepressant effects may take 2-4 weeks to manifest, but sedative and anticholinergic side effects often appear sooner.
• Therapeutic drug monitoring (TDM) for amitriptyline and nortriptyline levels can be useful in cases of non-response, suspected toxicity, or drug interactions.
• Withdrawal symptoms (e.g., nausea, headache, malaise, vivid dreams, irritability) can occur if discontinued abruptly; taper dose gradually over several weeks.
• Amitriptyline is often used off-label for chronic neuropathic pain (e.g., diabetic neuropathy, postherpetic neuralgia) and migraine prophylaxis at lower doses than those used for depression.

• Other Tricyclic Antidepressants (TCAs): Nortriptyline (less sedating, less anticholinergic), Imipramine, Desipramine, Doxepin.
• Selective Serotonin Reuptake Inhibitors (SSRIs): Fluoxetine, Sertraline, Paroxetine, Citalopram, Escitalopram (for depression).
• Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs): Duloxetine, Venlafaxine (for depression and neuropathic pain).
• Other Neuropathic Pain Agents: Gabapentin, Pregabalin, Duloxetine, Venlafaxine.
• Migraine Prophylaxis: Beta-blockers (e.g., Propranolol), Topiramate, CGRP inhibitors (e.g., Erenumab, Fremanezumab).

If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe use, never share your medication with others or take someone else's medication. This medication is accompanied by a Medication Guide, which provides crucial information for patients. Please read this guide carefully and review it again whenever you receive a refill of this medication. If you have any questions or concerns about this medication, consult 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 quantity, and the time it occurred.