Use of amitriptyline is commonly considered for treating mood shifts due to depression, anxieties, schizophrenia, etc. However, due to a few adverse side effects this drug is not a first-line option of many mental conditions. When all the options have failed, amitriptyline is prescribed as a second-line treatment. At lower doses, the drug is used for treating pains, insomnia as well as conditions such as fibromyalgia, diabetes-induced neuropathy, etc. Given the multiple uses of amitriptyline, it is important to know how this drug works. A basic knowledge of its mechanism of action can always be helpful.

There are multiple applications for which amitriptyline can be of use; this drug is essentially an antidepressant of the tricyclic genre. Key uses include treatment of depression, pains, headaches, migraine and irritation of bowels or related syndromes such as IBS, insomnia or other sleep-related disorders. In some countries, it is widely considered as a treatment option for attention deficit hyperactive disorder – ADHD, especially among children.

The common discomforts experienced by users of amitriptyline are dizziness, dryness of mouth, spells of drowsiness, difficulties to pass stools or constipation. Discomforts such as blurring of eyesight, increase in bodyweight, erratic heartbeats, shakes, enhanced level of appetite, etc. are also observed.

Mechanism of action of amitriptyline

This drug is absorbed directly from the gastric tract; however, this is not a sudden activity. It takes more than 3 hours for the process to be completed. It essentially makes a few neuro-transmitting substances such as serotonin, norepinephrine to be blocked – i.e., avoid them from being reabsorbed. This action makes way for an increased presence of these transmitting substances. Ions of sodium play an important role at a micro-level in the transmission of signals to your brain. Amitriptyline is efficient in inhibiting the channels of sodium ions. This inhibiting action is important for the blocking of feelings of pains as well as other discomforts like migraines, etc.

Shorter half-life and faster actions of amitriptyline

Amitriptyline has a half-life (elimination time) of almost 24 hours. More than 75% of the drug is discharged through urine; less than 1.75% of this drug – in an unaltered form – is eliminated through your urine. However, the discharge through solid waste / stools is not fully studied. Within its short half-life period, it controls the pumping mechanism of amines responsible for intra-membranous transmission of chemicals. Once the reuptake of amines such as serotonin, norepinephrine, etc. is controlled or blocked, the peripheral area of your brain is endowed with an increased presence of such amines.

Elevation of moods and effective control of pains

An increased presence of neuro-transmitting chemicals is directly responsible for regulating your moods and how you feel about things. This drug is essentially an antidote for the reduced availability of such neuro-transmitters. Several medical researches and studies have shown the link between reduced availability of serotonin, norepinephrine and other amines to conditions like depression, anxieties, etc. However, how these actions contribute to its painkilling or analgesic properties is still a matter of serious study. Several theories are being postulated to evidence amitriptyline’s ability to numb painful feelings.


Likely risks of overdose of amitriptyline

A few people may take amitriptyline for a faster relief from depression or other mental discomforts. This is not a safe practice. Those who took more than 750 milligrams (mg) of this drug experienced signs associated with overdose. You need to know that a larger dose (than what is prescribed) may only aggravate your current condition. The typical signs of an overdose include serotonin toxicity, faster heartbeats, lack of coordination, drop in blood pressure levels (hypotension), dilation of pupils, fits, seizures as well as convulsions. In some rare instances, a few people develop cardiac dysfunction, being in a confused state of mind, weird dreams, passing out or slipping into coma.

The mechanism of action of amitriptyline can harm women who are pregnant. It is important to tell your doctor if you are having plans to become pregnant or if you are already pregnant. Those who are planning to get pregnant may be advised to use birth control measures – such as pills, rings, patches, etc. It is recommended to talk to your physician about ways to avoid unplanned pregnancies while you are taking amitriptyline.

The active ingredients of amitriptyline are likely to enter into mother’s milk. Hence, it is not a good practice to take this drug while you are nursing a baby. Mothers who took amitriptyline may witness a few side effects in their baby. Your baby may experience adverse signs like sleeping difficulties, incessant spells of crying, feeding problems, etc. It is very important to tell your treating doctor about nursing your baby prior to starting medication plans involving the intake of amitriptyline.

Mechanism of action of amitriptyline when taken with other drugs

It is a good practice to inform your physician about the other drugs you are presently taking. Not stopping with drugs taken, you need to inform about other treatment plans, if any. It is highly recommended to make a list of all drugs currently consumed. As you make this list, ensure to add prescription meds, over the counter medications, vitamins, dietary supplements, nutraceuticals, herbals aids, etc.

You need to stay aware that drugs such as abacavir may see a loss of efficiency when it is taken along with amitriptyline. This drug is broken down sooner when administered with drugs like acebutolol, abiraterone, abatacept, etc. You are more likely to develop internal bleeding problems when you mix amitriptyline with medications like acemetacin and aceclofenac. Other safety precautions include reduction of caffeine intake; caffeine may intercept in the reuptake inhibiting properties of this drug. It is highly recommended to take amitriptyline along with a meal; this is known to reduce risks of gastrointestinal problems such as internal bruising, bleeding as well as gastric irritation.

In sum, amitriptyline controls the intra-membranous pumping of amines like serotonin, norepinephrine, etc. This action leads to an increased presence of these amines in the peripheral area of your brain. A reduced presence of norepinephrine and serotonin is likely to lead to mental conditions like anxieties, depression, mood swings, etc. In essence, amitriptyline provides for a larger residue of these amines in the peripheral area of your brain. These actions bring about much-needed relief from pains as well as mental health problems. You are advised to talk to your treating physician to know more about the mechanism of action of amitriptyline.

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