DRUGS & SUPPLEMENTS
Amitriptyline hydrochloride is a dibenzocycloheptene-derivative tricyclic antidepressant (TCA). TCAs are structurally similar to phenothiazines. They contain a tricyclic ring system with an alkyl amine substituent on the central ring. In non-depressed individuals, Amitriptyline does not affect mood or arousal, but may cause sedation. In depressed individuals, Amitriptyline exerts a positive effect on mood. TCAs are potent inhibitors of serotonin and norepinephrine reuptake. Tertiary amine TCAs, such as Amitriptyline, are more potent inhibitors of serotonin reuptake than secondary amine TCAs, such as nortriptyline. TCAs also down-regulate cerebral cortical β-adrenergic receptors and sensitize post-synaptic serotonergic receptors with chronic use. The antidepressant effects of TCAs are thought to be due to an overall increase in serotonergic neurotransmission. TCAs also block histamine-H1 receptors, α1-adrenergic receptors and muscarinic receptors, which accounts for their sedative, hypotensive and anticholinergic effects (e.g. blurred vision, dry mouth, constipation, urinary retention), respectively. See toxicity section below for a complete listing of side effects. Amitriptyline may be used to treat depression, chronic pain (unlabeled use), irritable bowel syndrome (unlabeled use), diabetic neuropathy (unlabeled use), post-traumatic stress disorder (unlabeled use), and for migraine prophylaxis (unlabeled use).
Indication: For the treatment of depression, chronic pain, irritable bowel syndrome, sleep disorders, diabetic neuropathy, agitation and insomnia, and migraine prophylaxis.
Amitriptyline, a tertiary amine tricyclic antidepressant, is structurally related to both the skeletal muscle relaxant cyclobenzaprine and the thioxanthene antipsychotics such as thiothixene. It is extremely sedating, and thus improvement of sleep patterns can be the first benefit of treatment. Amitriptyline exhibits strong anticholinergic activity, cardiovascular effects including orthostatic hypotension, changes in heart rhythm and conduction, and a lowering of the seizure threshold. As with other antidepressants, several weeks of therapy may be required in order to realize the full clinical benefit of Amitriptyline. Although not a labelled indication, Amitriptyline is widely used in the management of chronic nonmalignant pain (e.g., post-herpetic neuralgia, fibromyalgia).
Amitriptyline is an antidepressant tricyclic group of compounds derived dibenzocycloheptadiene.
The mechanism of antidepressant action is associated with an increased concentration of norepinephrine in the synapses and / or serotonin in the central nervous system depression due to reverse neuronal capture of these mediators. When anxiety and depressive states this medication reduces anxiety, agitation and depressive symptoms.
Also this drug has some analgesic effect, which is believed to be associated with changes in the concentrations of monoamines in the central nervous system, especially serotonin, and the influence on the endogenous opioid system.
It has distinct peripheral and central anticholinergic action, due to a high affinity for m-cholinergic receptors, a strong sedative effect connected with affinity for histamine H1-receptors and alpha-adrenoceptor blocking action.
Has antiulcer effect mechanism is due to the ability to block histamine H2-receptors in parietal cells of the stomach and provide a sedative and m-anticholinergic action. Its efficiency in the bed-wetting is caused, apparently, anticholinergic activity, which leads to an increase in the ability of the bladder to stretch, direct beta-adrenergic stimulation, the activity of alpha-adrenergic agonists, accompanied by increased tone of the sphincter and the central blockade of serotonin reuptake.
The mechanism of therapeutic action for bulimia nervosa is not installed (possibly similar to that for depression). It shown a clear efficacy of Amitriptyline in bulimia patients without depression, as well as in its presence, and the reduction of bulimia can be observed without a concomitant weakening of the most depressed.
With general anesthesia reduces blood pressure and body temperature. Amitriptyline does not inhibit MAO.
The antidepressant effect develops within 2-3 weeks after application.
The bioavailability of Amitriptyline is 30-60%. The plasma protein binding is 82-96%. Vd is 5-10 L / kg. This medicine is metabolized to the active metabolite nortriptyline. T1/2 is 31-46 hours. Amitriptyline excreted primarily by the kidneys.
Why is Amitriptyline prescribed?
Depression, schizophrenic psychoses, mixed emotional disorders, behavioral disorders (activity and attention), nocturnal enuresis (except in patients with hypotonia of the bladder), bulimia nervosa, chronic pain syndrome (chronic pain in cancer patients, migraine, rheumatic pain, atypical facial pain, postherpetic neuralgia, posttraumatic neuropathy, diabetic neuropathy, peripheral neuropathy), prophylaxis of migraine, peptic ulcer and duodenal ulcer.
Dosage and administration
For oral administration the initial dose is 25-50 mg at night. Then, within 5-6 days the dose was increased to an individual 150-200 mg / day (most of the dose taken at night). If, during the second week of the improvement has not come, the daily dose increased to 300 mg. With the disappearance of symptoms of depression to reduce the dose of 50-100 mg / day and continue therapy for at least 3 months. In elderly patients with lung disorders the dose is 30-100 mg / day is usually 1 time / at night, after achieving the therapeutic effect switching to the minimum effective dose - 25-50 mg / day.
When nocturnal enuresis in children aged 6-10 years - 10-20 mg / overnight; at the age of 11-16 years - 25-50 mg / day.
For IM injections the initial dose is 50-100 mg / injection in 2-4 injections. If necessary, the dose can be gradually increased to 300 mg / day, in exceptional cases up to 400 mg / day.
Amitriptyline side effects, adverse reactions
CNS and peripheral nervous system: drowsiness, fatigue, fainting, anxiety, confusion, agitation, hallucinations, anxiety, restlessness, mania, hypomania state, aggression, memory impairment, depersonalization, increased depression, decreased ability to concentrate, insomnia, nightmares, yawning, activation of psychosis symptoms, headache, myoclonus, dysarthria, tremor (especially of hands, head and tongue), peripheral neuropathy (paresthesia), myasthenia gravis, myoclonus, ataxia, extrapyramidal syndrome, acceleration and intensification of epileptic seizures, EEG changes.
Cardiovascular system: orthostatic hypotension, tachycardia, conduction disturbances, dizziness, nonspecific ECG changes (ST interval or spike T), arrhythmias, blood pressure lability, impaired intraventricular conduction (widening complex QRS, change the interval PQ, block bundle-branch block).
Digestive system: nausea, heartburn, vomiting, gastralgia, increase or decrease in appetite (increase or decrease in body weight), disease, change in taste, diarrhea, darkening of the tongue, rarely - liver dysfunction, cholestatic jaundice, hepatitis.
Endocrine: testicular swelling, gynecomastia, breast enlargement, galactorrhea, changes in libido, reduced potency, hypo-or hyperglycemia, hyponatremia (decreased production of vasopressin), a syndrome of inappropriate secretion of ADH.
Hematopoietic system: agranulocytosis, leukopenia, thrombocytopenia, purpura, eosinophilia.
Allergic reactions: skin rash, itching, rash, photosensitivity, swelling of the face and tongue.
Effects due to the anticholinergic activity: dry mouth, tachycardia, accommodation disturbances, blurred vision, mydriasis, increased intraocular pressure (only those with a narrow anterior chamber angle), constipation, paralytic ileus, urinary retention, decreased sweating, confusion, delirium or hallucinations.
Other: Hair loss, tinnitus, edema, hyperpyrexia, swollen lymph nodes, pollakiuria, hypoproteinemia.
The acute period and early recovery period after myocardial infarction, acute alcohol intoxication, acute poisoning with soporific, analgesic and psychotropic drugs, angle-closure glaucoma, severe AV- and intraventricular conduction (bundle branch block feet, AV-block II degree), lactation, children under 6 years of age (for oral administration), children under 12 years (for IV and IM injections), simultaneous treatment with inhibitors and a period of 2 weeks prior to their use, increased sensitivity to Amitriptyline Actavis.
Using during pregnancy and breastfeeding
Amitriptyline should not be used during pregnancy, especially in the I and III trimester, except in cases of extreme necessity. Adequate and well controlled clinical studies on the safety of Amitriptyline during pregnancy was not conducted.
This drug excreted in breast milk and may cause drowsiness in infants.
Taking of Amitriptyline should be phased out, at least 7 weeks prior to delivery to avoid the development of withdrawal syndrome in the newborn.
In experimental studies this medicine exerted teratogenic effects.
Use Amitriptyline with caution in coronary artery disease, arrhythmias, heart block, heart failure, myocardial infarction, hypertension, stroke, chronic alcoholism, thyrotoxicosis, against the background of therapy with thyroid cancer.
The therapy Amitriptyline it needed a caution when sharp transition in the vertical position of the "lying" or "sitting".
With a sharp stop taking may develop withdrawal symptoms.
Amitriptyline in doses of 150 mg / day lowers the threshold of convulsive readiness; it possible a risk of epileptic seizures in susceptible patients, as well as the presence of other factors that increase the risk of seizures.
It should be noted that patients with depression may attempt suicide.
In conjunction with electroconvulsive therapy it should only be used with careful medical supervision.
In predisposed patients and elderly patients may provoke the development of drug psychosis, mainly at night (after the withdrawal of the drug are within a few days).
Amitriptyline can cause paralytic ileus, mainly in patients with chronic constipation who are elderly or in patients who have to comply with bed rest.
Prior to the general or local anesthesia, the anesthesiologist it should be warned that patients taking Amitriptyline.
With prolonged use, an increase the frequency of dental caries. May increase the need for riboflavin.
Amitriptyline may be taken no earlier than 14 days after discontinuation of MAO inhibitors.
The drug should not be used in combination with adrenergic and sympathomimetic, including with epinephrine, ephedrine, isoprenaline, norepinephrine, phenylephrine, phenylpropanolamine.
Use Amitriptyline with caution in conjunction with other drugs, which have anticholinergic action.
While receiving Amitriptyline to avoid drinking alcohol.
During the period of treatment you should refrain from potentially hazardous activities requiring increased attention and rapid psychomotor reactions.
Amitriptyline drug interactions
When this drug applied simultaneously with:
- drugs have a depressing effect on the central nervous system, it is possibly a significant increase in inhibitory action on the central nervous system, hypotensive effect, respiratory depression.
- drugs with anticholinergic activity may increase anticholinergic effects.
- it may be enhance the action of sympathomimetic funds for the cardiovascular system and increase the risk of cardiac arrhythmia, tachycardia, severe hypertension.
- antipsychotic drugs (neuroleptics) are relatively suppressed metabolism, with a reduction in the threshold of convulsive readiness.
- antihypertensive drugs (except clonidine, guanethidine and their derivatives) may increase the antihypertensive action and the risk of orthostatic hypotension.
- with MAO inhibitors may been developed a hypertensive crisis; with clonidine, guanethidine it may be decreased the hypotensive effect of clonidine or guanethidine; with barbiturates, carbamazepine it may be decreased the action of Amitriptyline by increasing its metabolism.
- with sucralfate decreases absorption of Amitriptyline; with fluvoxamine - increases the concentration of Amitriptyline in blood plasma and the risk of toxic effects; with fluoxetine - increased concentration of Amitriptyline in plasma and develop toxic reactions due to inhibition of isoenzyme CYP2D6 under the influence of fluoxetine; with quinidine - may slow metabolism of Amitriptyline; with cimetidine - may slow metabolism of Amitriptyline, increasing its concentration in blood plasma and the development of toxic effects.
While taking alcohol the action of ethanol increases, especially during the first few days of therapy.
There was described a case of serotonin syndrome with simultaneously use with sertraline.
Amitriptyline pharmaceutical active ingredients containing related brand and generic drugs:
Active ingredient is the part of the drug or medicine which is biologically active. This portion of the drug is responsible for the main action of the drug which is intended to cure or reduce the symptom or disease. The other portions of the drug which are inactive are called excipients; there role is to act as vehicle or binder. In contrast to active ingredient, the inactive ingredient's role is not significant in the cure or treatment of the disease. There can be one or more active ingredients in a drug.
Amitriptyline available forms, composition, doses:
Form of the medicine is the form in which the medicine is marketed in the market, for example, a medicine X can be in the form of capsule or the form of chewable tablet or the form of tablet. Sometimes same medicine can be available as injection form. Each medicine cannot be in all forms but can be marketed in 1, 2, or 3 forms which the pharmaceutical company decided based on various background research results.
Composition is the list of ingredients which combinedly form a medicine. Both active ingredients and inactive ingredients form the composition. The active ingredient gives the desired therapeutic effect whereas the inactive ingredient helps in making the medicine stable.
Doses are various strengths of the medicine like 10mg, 20mg, 30mg and so on. Each medicine comes in various doses which is decided by the manufacturer, that is, pharmaceutical company. The dose is decided on the severity of the symptom or disease.
Amitriptyline destination | category:
Destination is defined as the organism to which the drug or medicine is targeted. For most of the drugs what we discuss, human is the drug destination.
Drug category can be defined as major classification of the drug. For example, an antihistaminic or an antipyretic or anti anginal or pain killer, anti-inflammatory or so.
Amitriptyline Anatomical Therapeutic Chemical codes:
A medicine is classified depending on the organ or system it acts [Anatomical], based on what result it gives on what disease, symptom [Therapeutical], based on chemical composition [Chemical]. It is called as ATC code. The code is based on Active ingredients of the medicine. A medicine can have different codes as sometimes it acts on different organs for different indications. Same way, different brands with same active ingredients and same indications can have same ATC code.
Amitriptyline pharmaceutical companies:
Pharmaceutical companies are drug manufacturing companies that help in complete development of the drug from the background research to formation, clinical trials, release of the drug into the market and marketing of the drug.
Researchers are the persons who are responsible for the scientific research and is responsible for all the background clinical trials that resulted in the development of the drug.
Frequently asked QuestionsCan i drive or operate heavy machine after consuming Amitriptyline?
Depending on the reaction of the Amitriptyline after taken, if you are feeling dizziness, drowsiness or any weakness as a reaction on your body, Then consider Amitriptyline not safe to drive or operate heavy machine after consumption. Meaning that, do not drive or operate heavy duty machines after taking the capsule if the capsule has a strange reaction on your body like dizziness, drowsiness. As prescribed by a pharmacist, it is dangerous to take alcohol while taking medicines as it exposed patients to drowsiness and health risk. Please take note of such effect most especially when taking Primosa capsule. It's advisable to consult your doctor on time for a proper recommendation and medical consultations.Is Amitriptyline addictive or habit forming?
Medicines are not designed with the mind of creating an addiction or abuse on the health of the users. Addictive Medicine is categorically called Controlled substances by the government. For instance, Schedule H or X in India and schedule II-V in the US are controlled substances.
Please consult the medicine instruction manual on how to use and ensure it is not a controlled substance.In conclusion, self medication is a killer to your health. Consult your doctor for a proper prescription, recommendation, and guidiance.
ReviewsDrugs.com conducted a study on Amitriptyline, and the result of the survey is set out below. It is noteworthy that the product of the survey is based on the perception and impressions of the visitors of the website as well as the views of Amitriptyline consumers. We, as a result of this, advice that you do not base your therapeutic or medical decisions on this result, but rather consult your certified medical experts for their recommendations.
One visitor reported frequency of useHow often in a day do you take the medicine?
Are you taking the Amitriptyline drug as prescribed by the doctor?
Few medications can be taken Once in a day more than prescribed when the doctor's advice mentions the medicine can be taken according to frequency or severity of symptoms. Most times, be very careful and clear about the number of times you are taking the medication. The report of sDrugs.com website users about the frequency of taking the drug Amitriptyline is mentioned below.
Three visitors reported dosesWhat is the dose of Amitriptyline drug you are taking?
According to the survey conducted among sDrugs.com website users, the maximum number of people are using the following dose 101-200mg. Few medications come in only one or two doses. Few are specific for adult dose and child dose. The dose of the medicine given to the patient depends on the severity of the symptom/disease. There can be dose adjustments made by the doctor, based on the progression of the disease. Follow-up is important.
One visitor reported time for resultsWhat is the time duration Amitriptyline drug must be taken for it to be effective or for it to reduce the symptoms?
Most chronic conditions need at least some time so the dose and the drug action gets adjusted to the body to get the desired effect. The stastistics say sDrugs.com website users needed 1 month to notice the result from using Amitriptyline drug. The time needed to show improvement in health condition after using the medicine Amitriptyline need not be same for all the users. It varies based on other factors.
Two visitors reported age
The information was verified by Dr. Arunabha Ray, MD Pharmacology