Amitriptylin
Amitriptylin Uses, Dosage, Side Effects, Food Interaction and all others data.
Amitriptylin HCl is an antidepressant with sedative effects. Its mechanism of action in man is not known. It is not a monoamine oxidase inhibitor and it does not act primarily by stimulation of the central nervous system.
Amitriptylin inhibits the membrane pump mechanism responsible for uptake of norepinephrine and serotonin in adrenergic and serotonergic neurons. Pharmacologically, this action may potentiate or prolong neuronal activity since reuptake of these biogenic amines is important physiologically in terminating transmitting activity. This interference with reuptake of norepinephrine and/or serotonin is believed by some to underlie the antidepressant activity of Amitriptylin.
Effects in pain and depression
Amitriptylin is a tricyclic antidepressant and an analgesic. It has anticholinergic and sedative properties .Clinical studies have shown that oral amitriptyline achieves, at a minimum, good to moderate response in up to 2/3 of patients diagnosed with post-herpetic neuralgia and 3/4 of patients diagnosed with diabetic neuropathic pain, and neurogenic pain syndromes that are frequently unresponsive to narcotic analgesics. Amitriptylin has also shown efficacy in diverse groups of patients with chronic non-malignant pain. There have also been some studies showing efficacy in managing fibromyalgia (an off-label use of this drug) , .
Cardiovascular and Anticholinergic Effects
Trade Name | Amitriptylin |
Availability | Prescription only |
Generic | Amitriptyline |
Amitriptyline Other Names | Amitriptilina, Amitriptylin, Amitriptyline, Amitriptylinum |
Related Drugs | Rexulti, Buprenex, aspirin, prednisone, ibuprofen, acetaminophen, sertraline, tramadol, trazodone, fluoxetine |
Type | |
Formula | C20H23N |
Weight | Average: 277.4033 Monoisotopic: 277.183049741 |
Protein binding | Very highly protein bound (95%) in plasma and tissues . |
Groups | Approved |
Therapeutic Class | Tricyclic Anti-depressant |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
![Amitriptylin Amitriptylin](https://www.medicinesfaq.com/media/png/amitriptylin.png)
Uses
Amitriptylin is used for depressive illness, particularly with anxiety and nocturnal enuresis in children.
Amitriptylin is also used to associated treatment for these conditions: Acute Depression, Anorexia Nervosa (AN), Attention Deficit Hyperactivity Disorder (ADHD), Bulimia Nervosa, Depression, Diabetic Neuropathies, Insomnia, Irritable Bowel Syndrome (IBS), Major Depressive Disorder (MDD), Migraine, Moderate Depression, Neuropathic Pain, Nocturnal Enuresis, Severe Depression, Sleep disorders and disturbances, Tension Headache, Moderate Agitation, Moderate Anxiety, Severe Anxiety, Severe agitation
How Amitriptylin works
The mechanism of action of this drug is not fully elucidated. It is suggested that amitriptyline inhibits the membrane pump mechanism responsible for the re-uptake of transmitter amines, such as norepinephrine and serotonin, thereby increasing their concentration at the synaptic clefts of the brain , . These amines are important in regulating mood. The monoamine hypothesis in depression, one of the oldest hypotheses, postulates that deficiencies of serotonin (5-HT) and/or norepinephrine (NE) neurotransmission in the brain lead to depressive effects . This drug counteracts these mechanisms, and this may be the mechanism of amitriptyline in improving depressive symptoms.
Whether its analgesic effects are related to its mood-altering activities or attributable to a different, less obvious pharmacological action (or a combination of both) is unknown .
Dosage
Amitriptylin dosage
Depression :
- Adults: Initially 50-70 mg a day in divided dose or as a single dose at night at bed time.
- Elderly and adolescents: 25-50 mg daily in divided doses or as single dose at bed time. Dose can be increased gradually as necessary to a maximum of 150-200 mg. Usual maintenance dose is 50-100 mg daily.
Nocturnal enuresis:
- 6-10 years: 10-20 mg at bed time.
- 11-16 years: 25-50 mg at bed time for up to 3 months and gradually withdrawn.
Side Effects
- Cardiovascular reactions: Hypotension, syncope, postural hypotension, hypertension, tachycardia, palpitations, myocardial infarction, arrythmias, and heart block stroke.
- CNS and neuromuscular: Confusional states, disturbed concentration disorientation, delusions, and hallucinations.
- Anticholinergic: Dry mouth, blurred vision, mydriasis, increased intraoccular pressure, hyperplasia.
- Allergic: Skin rash, urticaria, and photosensitization.
- Haematological: Bone-marrow depression including agranulocytosis, leukopenia, eosinophilia, and thrombocytopenia.
- Gastrointestinal: Nausea, epigastric distress, vomiting anorexia, diarrhoea.
- Endocrine: Testicular swelling, gynaecomastia; breast enlargement, galactorrhoea.
- Other reaction: Dizziness, weakness, fatigue, headache, weight loss
Toxicity
Toxicity Data: Oral TDLO (child): 4167 μg/kg; Oral TDLO (man): 714 μg/kg/1D (intermittent); Oral TDLO (woman): 10 mg/kg .
Ingestion of 750 mg or more by an adult may result in severe toxicity. The effects in overdose are further increased by simultaneous ingestion of alcohol and another psychotropic agent . Symptoms of overdose include abnormally low blood pressure, confusion, convulsions, dilated pupils and other eye problems, disturbed concentration, drowsiness, hallucinations, impaired heart function, rapid or irregular heartbeat, reduced body temperature, stupor, and unresponsiveness or coma, among others , .
Use in pregnancy
For amitriptyline, only limited clinical data are available regarding its use in pregnancy. Amitriptylin is not recommended during pregnancy unless clearly required and only after careful consideration of both risks and benefits .
Use in breastfeeding
Amitriptylin and its metabolites are excreted into breast milk (corresponding to 0.6 % - 1 % of the maternal dose). A risk to the suckling child must be considered. A decision should be made as to whether it is appropriate to discontinue breastfeeding or to discontinue/abstain from the therapy of this medicinal product, considering the benefit of breastfeeding for the child and the benefit of therapy for the woman.
Effects on fertility
Animal studies have shown reproductive toxicity. No data on the effects of amitriptyline on human fertility are available .
Mutagenesis and carcinogenesis
The genotoxic potential of amitriptyline has been investigated in various in vitro and in vivo studies. Although these investigations showed some contradictory results, a potential of amitriptyline to lead to chromosome abnormalities cannot be excluded. Long-term carcinogenicity studies have not been performed to this date .
Precaution
Schizophrenic patients may develop increased symptoms of psychosis; patients with paranoid symptomatology may have an exaggeration of such symptoms. Depressed patients, particularly those with known manic-depressive illness, may experience a shift to mania or hypomania. In these circumstances the dose of Amitriptylin may be reduced or a major tranquilizer such as perphenazine may be administered concurrently.
The possibility of suicide in depressed patients remains until significant remission occurs. Potentially suicidal patients should not have access to large quantities of this drug. Prescriptions should be written for the smallest amount feasible.
Concurrent administration of Amitriptylin hydrochloride and electroshock therapy may increase the hazards associated with such therapy. Such treatment should be limited to patients for whom it is essential.
When possible, the drug should be discontinued several days before elective surgery. Both elevation and lowering of blood sugar levels have been reported. Amitriptylin hydrochloride should be used with caution in patients with impaired liver function.
Interaction
Monoamine oxidase inhibitors can potentiate the effects of Amitriptylin.
Anticholinergic agents: Amitriptylin should not be given with symptomatic agents such as adrenaline, epinephrine, isoprenaline, noradrenaline.
CNS depressant: Amitriptylin may enhance the response to alcohol, barbiturates.
Cemitidine: Cemitidine is reported to reduce hepatic metabolism of certain tricyclic antidepressants.
Food Interaction
- Avoid alcohol.
- Avoid St. John's Wort.
- Limit caffeine intake.
- Take with food. Food reduces irritation.
Amitriptylin Alcohol interaction
[Moderate] GENERALLY AVOID:
Concomitant use of ethanol and a tricyclic antidepressant (TCA) may result altered TCA plasma levels and efficacy, and additive impairment of motor skills, especially driving skills.
Acute ethanol ingestion may inhibit TCA metabolism, while chronic ingestion of large amounts of ethanol may induce hepatic TCA metabolism.
Patients should be advised to avoid alcohol during TCA therapy.
Alcoholics who have undergone detoxification should be monitored for decreased TCA efficacy.
Dosage adjustments may be required.
Amitriptylin Drug Interaction
Major: duloxetine, duloxetine, cyclobenzaprine, cyclobenzaprine, topiramate, topiramateModerate: pregabalin, pregabalin, levothyroxine, levothyroxine, alprazolam, alprazolamUnknown: omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, cyanocobalamin, cyanocobalamin, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol
Amitriptylin Disease Interaction
Major: anticholinergic effects, cardiovascular disease, pheochromocytoma, acute myocardial infarction recovery, cardiovascular disease, depression, seizure disordersModerate: bone marrow suppression, diabetes, renal/liver disease, schizophrenia/bipolar disorder, tardive dyskinesia, acute alcohol intoxication, bipolar disorder screening, glaucoma, hyper/hypoglycemia, liver/renal disease, neutropenia, schizophrenia, thyroid disorders, urinary retention
Volume of Distribution
The apparent volume of distribution (Vd)β estimated after intravenous administration is 1221 L±280 L; range 769-1702 L (16±3 L/kg) . It is found widely distributed throughout the body . Amitriptylin and the main metabolite nortriptyline pass across the placental barrier and small amounts are present in breast milk .
Elimination Route
Rapidly absorbed following oral administration (bioavailability is 30-60% due to first pass metabolism). Peak plasma concentrations are reached 2-12 hours after oral or intramuscular administration . Steady-state plasma concentrations vary greatly and this variation may be due to genetic differences .
Half Life
The elimination half-life (t1⁄2 β) amitriptyline after peroral administration is about 25 hours (24.65 ± 6.31 hours; range 16.49-40.36 hours) .
Clearance
The mean systemic clearance (Cls) is 39.24 ± 10.18 L/h (range: 24.53-53.73 L/h) . No clear effect of older age on the pharmacokinetics of amitriptyline has been determined, although it is possible that clearance may be decreased .
Elimination Route
Amitriptylin and its metabolites are mainly excreted in the urine. Virtually the entire dose is excreted as glucuronide or sulfate conjugate of metabolites, with approximately 2% of unchanged drug appearing in the urine . 25-50% of a single orally administered dose is excreted in urine as inactive metabolites within 24 hours . Small amounts are excreted in feces via biliary elimination .
Pregnancy & Breastfeeding use
Pregnancy Category C. Amitriptylin is not recommended during pregnancy, especially during the first and third trimester because the safety of Amitriptylin has not been established yet.
Amitriptylin is detectable in breast milk. Because of the serious adverse reactions in infants from Amitriptylin, a decision should be made whether to continue breast feeding or discontinue the drug
Contraindication
Amitriptylin is contraindicated in myocardial infarction; arrythmias, particularly heartblock of any degree; mania; severe liver disease. Initially sedation may effect the ability to drive or operate machinery. It should be used with caution in patients with a history of epilepsy, glaucoma, urinary retention, prostatic hypertrophy, constipation, cardiac disease, diabetes, pregnancy, hepatic impairment, thyroid disease, increased intraoccular pressure, psychoses (may aggravate mania).
Storage Condition
Keep containers well closed and stored below 25˚ C, protected from light.
Innovators Monograph
You find simplified version here Amitriptylin
Amitriptylin contains Amitriptyline see full prescribing information from innovator Amitriptylin Monograph, Amitriptylin MSDS, Amitriptylin FDA label
FAQ
What is Amitriptylin used for?
Amitriptylin is a tricyclic antidepressant primarily used to treat major depressive disorder and a variety of pain syndromes from neuropathic pain to fibromyalgia to migraine and tension headaches.
Amitriptylin is a medicine used for treating pain. You can also take it Amitriptylin to treat nerve pain (neuralgia) and back pain.
How safe is Amitriptylin?
Amitriptylin is safe to take for a long time. There do not seem to be any lasting harmful effects from taking it for many months or years.
How does Amitriptylin work?
Amitriptylin work by increasing a chemical called serotonin in your brain.
What are the common side effects of Amitriptylin?
Common side effects of Amitriptylin are include:
- constipation.
- dizziness.
- dry mouth.
- feeling sleepy.
- difficulty peeing.
- headache.
Is Amitriptylin safe during pregnancy?
Amitriptylin is generally not recommended in pregnancy. This is because it has been linked to a small risk of problems for your baby if you take it in early or late pregnancy.
Is Amitriptylin safe during breastfeeding?
Amitriptylin is not usually recommended if you're breastfeeding. Amitriptylin gets into breast milk. It's been linked with side effects like sleepiness in breastfed babies.
Can I drink alcohol with Amitriptylin?
You can drink alcohol while taking Amitriptylin but it may make you feel sleepy. It's usually best to stop drinking alcohol until you see how the medicine makes you feel.
Can I drive after taking Amitriptylin ?
Some people feel sleepy while they're taking Amitriptylin. It is best to stop driving and cycling for the first few days of treatment until you know how this medicine makes you feel.
When should be taken of Amitriptylin?
It's best to take it before bedtime because it can make you feel sleepy. If you find that you are still feeling drowsy in the morning you could try taking it earlier in the evening.
Can I take Amitriptylin on an empty stomach?
Amitriptylin may be taken on an empty or full stomach.
How many time can I take Amitriptylin daily?
Amitriptylin is usually taken one to four times a day.
How long does Amitriptylin take to work?
You may start to feel better after 1 to 2 weeks but it can take 4 to 6 weeks for Amitriptylin to work fully.
How long does Amitriptylin take to work?
So Amitriptylin will stay in your system for about 2 to 6 days after your last dose.
How much Amitriptylin can I take daily?
Adults, At first 75 milligrams (mg) per day given in divided doses, or 50 to 100 mg at bedtime.
How long can I take Amitriptylin?
Some people take it for many months and even for years. You should take this medication for at least 3-6 months.
Who should not take Amitriptylin?
You should not use Amitriptylin if you have recently had a heart attack. Do not use Amitriptylin if you have used an MAO inhibitor in the past 14 days, such as isocarboxazid, linezolid, methylene blue injection, phenelzine, rasagiline, selegiline, or tranylcypromine.
What happens if I miss a dose?
Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.
What happens if I overdose?
Seek emergency medical attention. An overdose of amitriptyline can be fatal. Overdose symptoms may include irregular heart rhythm, feeling like you might pass out, seizures, or coma.
What happen If I stop taking Amitriptylin?
Amitriptylin is not addictive but you can get extra side effects if you stop taking it suddenly. You may have flu-like symptoms like feeling sick, muscle pain and feeling tired or restless.
Will Amitriptylin affect my fertility?
There is no clear evidence that Amitriptylin affects either male or female fertility.
Does Amitriptylin cause heart attacks?
Amitriptylin induced toxic myocarditis and dilated cardiomyopathy have been reported only once in the literature after autopsy.
Can Amitriptylin affect my kidneys?
Amitriptylin has many side effects on rat liver and kidney, it induced liver and kidney toxicity and tissue injury were it metabolized to nortriptyline which inhibits the reuptake of norepinephrine and serotonin almost equally.
Can Amitriptylin increase blood pressure?
Amitriptylin works to cause very high blood pressure.
Can Amitriptylin gain my weight?
Brand can causes weight gain also with other side effects.