Drug info - imipramine for ADHD???

[Donmeka]

ok SWIM has done a little googling on imipramine because his doctor in his anger management classes recommended he try it because of his ADHD/depression/GAD or w/e ADHD mainly, he currently has RXs to Adderall and Xanax which he is perfectly happy with and takes perfectly fine with no tolerance or addiction whatsoever, SWIM does not even take it everyday.

anyway this Dr. said he should stop his meds(he has for a couple weeks, has 4 weeks of class left and will get his RX again NP lol) and try the imipramine. Now...SWIM has had an anti depressant and anti psychotic RXd before he had his current combo that works for him. and has gone through a couple psychs that would only suggest ADs and would not respect that SWIM has tried them, hates them and refuses any type of AD because of his experience which was while on Celexa and Rsiperdal(lowest doeses i believe, 10mg and 0.25mg) SWIM experienced a seizure and he also experiences ticks and twitches now he believes from the experience(which was maybe 2/3yrs ago). they also did not work very well for his "mental problem" at all. SWIM did his research and knows his information and after that has told psych/Dr.s and brought in paperwork to back up SWIMs claims.

SWIM finally found a psych that is chill and understands SWIMs issue with Anti Depressants and respects his wish not to use them. He takes Adderall and Xanax and told his doc to try them because they are very well researched and known chemicals and do not take weeks to see an effect. They also do not have as serious side effects as ADs besides addiction potential. SWIM has told his psych that if addiction is the only reason why someone would not RX it to him, he trusts himself with a possibly addictive medication that CAN be controlled easily if SWIM is responsible than some "mystery medication" that MIGHT work in 2 weeks and MAY cause seizures and suicidal thoughts.

Now SWIMs anger doc wants SWIM 100% sober for now(to note SWIM had a fight with his father and is NOT an angry person it is just a court formality he is in the class) and asked him to get on the imipramine. Although SWIM is not an angry person this does irritate him because this Dr. knows very little about SWIM and his mental and general history and constantly acts like he knows everything and he is always right. He is a Dr. yes but SWIM knows what he takes, how to take it and what he does not like to take because of his past experience.

Can anyone tell SWIM any personal experiences with imipramine? or any additional information beyond the usual information on wikipedia and medical guides? if Celexa/Risperdal caused a seizure with SWIM should he stay clear of imipramine?

SWIM will most likely just bullshit his way through the next 4 weeks and get back on his adderall/xanax. this guy is a total prick lol and SWIM will rejoice when he is out of SWIMs life.

any information is greatly appreciated and SWIM may give it a try if he is convinced it might be helpful, though because of the past he may not.

Donmeka added 0 Minutes and 48 Seconds later...

damn there is NO help on this POS chemical here is some info SWIM FOUND ON GOOGLE! since DF for once doesntr have anything, this is so rare it scares SWIM. this is from wikipedia


History

Imipramine was, in the late 1950s, the first tricyclic antidepressant to be developed (by Ciba-Geigy). Initially, it was tried against psychotic disorders (e.g. schizophrenia), but proved insufficient. During the clinical studies its antidepressant qualities were unsurpassed by other antidepressants. To this day, Imipramine is often considered the "gold standard" antidepressant as its ability to lift the most severe depressive episodes is unsurpassed. Not surprisingly, Imipramine is also known to cause a high rate of manic and hypomanic reactions, especially in patients with preexisting bipolar disease. It is estimated that up to 25% of such patients maintained on Imipramine will switch into mania or hypomania.[2] Such powerful antidepressant properties have made it favorable in the treatment of treatment-resistant depression.

At the advent of SSRIs, its sometimes intolerable side effect profile became evident. Subsequently, it was extensively used as a standard antidepressant and later served as a prototypical drug for the development of the later released tricyclics. It is not as commonly used today, but is sometimes used to treat major depression as a second-line treatment. It has also seen limited use in the treatment of migraines, ADD and post concussive syndrome. Imipramine has additional indications for the treatment of panic attacks, chronic pain, and Kleine-Levin syndrome. In pediatric patients it is relatively frequently used to treat pavor nocturnus and nocturnal enuresis.

[edit] Mechanisms Of Action

Imipramine, a tertiary amine, affects numerous neurotransmitter systems know to be involved in the etiology of depression, anxiety , ADD/ADHD, enuresis and numerous other mental and physical conditions. Imipramine is similar in structure to some muscle relaxants, and has a significant analgesic effect and thus is very useful in some pain conditions.

The mechanisms of Imipramine's medicinal action include, but are not limited to, effects on: norepinephrine, serotonin, dopamine, epinephrine, sigma receptor, enkephalinase, histamine, muscarine, and acetylcholine.

Effects on:

Norepinephrine (NE) Reuptake inhibition (strong).

Serotonin (SE) Reuptake inhibition (moderate to strong). The reuptake inhibition is almost comparable but still less than Imipramine's potency of reuptake inhibition on norepinephrine. Stronger SERT inhibition than most other tricyclic antidepressants, making it more akin to the SSRI class of antidepressants (e.g. Prozac (fluoxetine), Zoloft (sertraline)) than its metabolite desipramine, which has almost purely noradrenergic effects.

Acetylcholine (ACh) Imipramine is an anticholinergic. Thus, it is prescribed with caution to the elderly and with extreme caution to those with pyschosis, as the general brain activity enhancement in combination with the "dementing" effects of anticholinergics increases the potential of Imipramine to cause hallucinations, confusion and delirium in this population. Imipramine is an antagonist at M2 muscarinic acetylcholine receptors (see external links). The blockade of cholinergic (muscarine) receptors is known to cause euphoria, potentially contributing to the mood lifting effects of Imipramine as well. Antimuscarinic effect is also responsible for rapid heart rate (tachycardia).

Epinephrine Imipramine antagonizes adreno-receptors (II), thus sometimes causing increased heart rate (contributed to by other effects as well), orthostatic hypotension, and a general decrease in the responsiveness of the central nervous system (hence, a contribution to its potent anti-anxiety properties).

Dopamine Reuptake and release at D1 and D2 receptors, similar to, but less potent than, psychostimulants, dopamine agonists and atypical antidepressant buproprion on dopaminergic mechanisms (increase in release and blockade of reuptake inhibition). While this effect is much less than the primary effects on NE, SE and ACe, it is nonetheless significant and is partially responsible for the therapeutic benefits of treatment with Imipramine. Enhancement of brain dopamine activity has been implicated in Imipramine's ability to stimulate motor activity and prolong time spent in escape in mice. In regards of dopamine uptake, imipramine is far less potent then most of other antidepressants (for example, it's 1/20 in potency of amitryptiline and paroxetine, see references).

Sigma receptor and Enkephalinase Activity on sigma receptors (sigma ligands) is present, but it is very low (Ki of 520 nM on sigma receptors, see references) and it is about half the power of amitryptiline (300 nM).

Histamine Imipramine is an antagonist at histamine H1 receptors. This contributes to the acute sedative effect that it has in most people. In turn, its anti-histaminergic and general calming effects take place immediately and thus, Imiparmine is sometimes prescribed as a sleep aid in low doses.

[edit] Comparison with other antidepressants

The potency (affinity) of imipramine and other antidepressant on various transporters and receptors are summarized below. Data are from "Pharmacology of antidepressant", Mayo Clin Proc, May 2001, Vol 76.[3]

Potency (affinity) data are expressed as the inverse of equilibrium dissocation constant multiplied by a factor of 10^-7. So, the higher the number, the higher the blocking power.
Drug NE Transporter SE Transporter DE transporter alpha1 blockade D2 blockade H1 blockade muscarinic blockade 5HT2 blockade
imipramine 2.7 70 0.012 1.5 0.05 9.1 1.1 1.2
desipramine (also an imipramine metabolite) 128 5.7 0.024 0.77 0.03 0.91 0.5 0.38
amitriptyline 2.9 23 0.023 3.7 0.1 91 5.6 3.4
clomipramine 2.7 360 0.045 2.6 0.53 3.2 2.7 3.7
paroxetine 2.5 800 0.2 0.025 0.003 0.03 0.93 0.005
citalopram 0.035 98 0.0038 0.053 0 0.21 0.045 0.34

[edit] Metabolism

Imipramine is converted to desipramine, another TCA, in the body.

[edit] Contraindications and precautions

(See Tricyclic antidepressants)

Imipramine should not be given in conjunction with, or within 14 days of treatment with a MAO inhibitor. Combined therapy of this type could lead to the appearance of serious interactions such as hypertensive crises, hyperactivity, hyperpyrexia, spasticity, severe convulsions or coma and death may occur.

Imipramine is contraindicated in patients with existing severe hepatic or renal damage, and those with a history of blood dyscrasias.

Imipramine is contraindicated in patients who have shown hypersensitivity to the drug or hypersensitivity to tricyclic antidepressants belonging to the dibenzazepine group.

Imipramine is contraindicated for use during the acute recovery phase following a myocardial infarction.

It should not be used in patients with convulsive disorders or glaucoma.

(http://www.mentalhealth.com/drug/p30-t03.html#Head_3)

[edit] Side effects

After taking the medicine this drug may cause some side effects in some patients, particularly with the first few doses.

Allergy: isolated cases of pneumonitis (fever, chills, cough, difficulty with breathing, unusual weight loss, feeling sick, puffy, swollen face, tongue or body) have been reported. These reactions may be severe, causing shortness of breath, swelling, shock and collapse.

Isolated changes in blood cells.

Arrhythmias: irregular heart rhythms.

Weight gain has been reported frequently. Disturbances in sexual function have been reported occasionally. Isolated cases of enlarged mammary glands, production or over-production of breast milk, increased or decreased blood sugar levels and weight loss have been reported. Low levels of salt in the blood have been reported, usually in elderly patients.

Tremor has been reported frequently. Headache, confusion, orthostatic hypotension (resulting in dizziness upon standing), numbness/tingling, agitation, anxiety, restlessness, mood swings, exaggerated behaviour, delusions and hallucinations have been reported occasionally and are more common in the elderly or in patients on high doses. Aggressiveness, weakness, lack of co-ordination, sudden muscle spasms, difficulty speaking have been reported in isolated cases.

Imipramine also enhances the CNS effects of both stimulants and alcohol, and blocks the parasympathomimetic effects of stimulants while enhancing the cortical excitation. This can be dangerous in some cases and result in seizures and coma.

Ringing or buzzing in the ears.

Feeling or being sick and loss of appetite have been reported occasionally. Isolated cases of tongue lesions and inflammation of the mucus membranes in the mouth have been reported. Extreme dry mouth or "cotton mouth" has been reported. Mild to severe constipation has also been reported.

Changes in liver function have been reported occasionally. Hepatitis and jaundice (yellowing of the skin and/or whites of the eyes) have been reported in isolated cases.

Allergic reactions such as an itchy skin rash have been reported occasionally. Isolated cases of swelling, sensitivity to the sun or sun lamps, hair loss, small purple red spots and itching have been reported.

If the medicine is stopped too quickly, there is the possibility the user may suffer from feeling or being sick, stomach pains, diarrhea, headache, sleeplessness, nervousness, anxiety, irritability and increased sweating.

[edit] Dosage

* Hospitalized patients: starting with 3 time 25 mg, increasing to 200 mg. Up to 300 mg may be given in resistant cases. After remission dose is often reduced to 50–100 mg daily.
* Ambulatory patients: starting with 25 to 75 mg daily, increasing up to a maximum of 200 mg daily, after remission dose is often reduced to 50–100 mg daily.
* Pediatric patients: starting with 10 mg daily the dose is adjusted according to the severity of the symptoms to be treated, the side-effects encountered and the weight of the patient.

[edit] Overdose
Main article: Tricyclic antidepressant overdose

The symptoms and the treatment of an overdose are largely the same as for the other tricyclic antidepressants. Cardinal symptoms are cardiac (tachycardia, widened QRS complex) and neurological disturbances. Any ingestion by children should be considered as serious and potentially fatal.