imipramine
Dictionary:
i·mip·ra·mine (ĭ-mĭp'rə-mēn') 
|
n.
A tricyclic compound, C19H24N2, used to treat depression and enuresis.
| 5min Related Video: imipramine |
| Drug Info: Imipramine |
Brand names: Tofranil®Tofranil-PM®
Chemical formula:
- Drug Forms:
- Imipramine tablets (below)
- Imipramine injection
- Imipramine Pamoate Oral capsule
- Imipramine Hydrochloride Oral tablet
- Español:
- Tabletas de imipramina
- Inyección de imipramina
- Imipramina Pamoato, Cápsula oral
- Clorhidrato de Imipramina, Tableta oral
Imipramine tablets
What are imipramine tablets?
IMIPRAMINE (Tofranil®) is an antidepressant. Imipramine can help to lift your spirits by treating your depression. Imipramine can help children who have a nighttime bed-wetting problem. Generic imipramine tablets are available.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
• an alcohol problem
• asthma, difficulty breathing
• blood disorders or disease
• diabetes
• difficulty passing urine, prostate trouble
• glaucoma
• having intramuscular injections
• heart disease, or recent heart attack
• liver disease
• over active thyroid
• Parkinson's disease
• schizophrenia
• seizures (convulsions)
• stomach disease
• an unusual or allergic reaction to imipramine, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding
How should I take this medicine?
Take imipramine tablets by mouth. Follow the directions on the prescription label. Swallow the tablets with a drink of water. Take your doses at regular intervals. Do not take your medicine more often than directed. Do not stop taking except on your prescriber's advice.
Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.
Elderly patients over 65 years old and adolescents may have a stronger reaction to this medicine and need smaller doses.
What drug(s) may interact with imipramine?
Imipramine can interact with many other medicines. Some interactions can be very important. Make sure your prescriber or health care professional knows about all other medicines you are taking. Many important interactions are listed below:
Do not take Imipramine with any of the following medications:
• astemizole (Hismanal®)
• cisapride (Propulsid®)
• probucol
• terfenadine (Seldane®)
• thioridazine (Mellaril®)
• medicines called MAO inhibitors-phenelzine (Nardil®), tranylcypromine (Parnate®), isocarboxazid (Marplan®), selegiline (Eldepryl®)
• other medicines for mental depression (may be duplicate therapies or cause additive side effects)
Imipramine may also interact with any of the following medications:
• alcohol
• antacids
• atropine and related drugs like hyoscyamine, scopolamine, tolterodine and others
• barbiturate medicines for inducing sleep or treating seizures (convulsions), such as phenobarbital
• blood thinners, such as warfarin
• bromocriptine
• bupropion
• cimetidine
• clonidine
• cocaine
• delavirdine
• diphenoxylate
• disulfiram
• donepezil
• drugs for treating HIV infection
• female hormones, including contraceptive or birth control pills and estrogen
• galantamine
• herbs and dietary supplements like ephedra (Ma huang), kava kava, SAM-e, St. John's wort, valerian, or others
• imatinib, STI-571
• kaolin; pectin
• labetalol
• levodopa and other medicines for movement problems like Parkinson's disease
• lithium
• medicines for anxiety or sleeping problems
• medicines for colds, flu and breathing difficulties, like pseudoephedrine
• medicines for hay fever or allergies (antihistamines)
• medicines for weight loss or appetite control
• medicines used to regulate abnormal heartbeat or to treat other heart conditions (examples: amiodarone, bepridil, disopyramide, dofetilide, encainide, flecainide, ibutilide, mibefradil, procainamide, propafenone, quinidine, and others)
• metoclopramide
• muscle relaxants, like cyclobenzaprine
• other medicines for mental or mood problems and psychotic disturbances
• prescription pain medications like morphine, codeine, tramadol and others
• procarbazine
• seizure (convulsion) or epilepsy medicine such as carbamazepine or phenytoin
• stimulants like dexmethylphenidate or methylphenidate
• some antibiotics (examples: erythromycin, gatifloxacin, levofloxacin, linezolid, moxifloxacin, sotalol, sparfloxacin)
• tacrine
• thyroid hormones such as levothyroxine
Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.
What should I watch for while taking imipramine?
Visit your prescriber or health care professional for regular checks on your progress. It can take several days or weeks before you feel the full effect of imipramine. If you have been taking imipramine regularly for some time, do not suddenly stop taking it. You must gradually reduce the dose or you may get severe side effects. Ask your prescriber or health care professional for advice. Even after you stop taking imipramine it can still affect your body for several days.
You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how imipramine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol can increase dizziness and drowsiness. Avoid alcoholic drinks.
Do not treat yourself for coughs, colds or allergies without asking your prescriber or health care professional for advice. Some ingredients can increase possible side effects.
Your mouth may get dry. Chewing sugarless gum or sucking hard candy, and drinking plenty of water will help.
Imipramine may cause dry eyes and blurred vision. If you wear contact lenses you may feel some discomfort. Lubricating drops may help. See your ophthalmologist if the problem does not go away or is severe.
Imipramine may make your skin more sensitive to the sun. Keep out of the sun, or wear protective clothing outdoors and use a sunscreen. Do not use sun lamps or sun tanning beds or booths.
Imipramine can affect blood glucose (sugar) levels. If you are a diabetic, check your blood sugar more often than usual, especially during the first few weeks of imipramine treatment. Call your prescriber or health care professional for advice if you notice a change in the results of blood or urine glucose tests.
If you are going to have surgery or will need an x-ray procedure that uses contrast agents, tell your prescriber or health care professional that you are taking this medicine.
What side effects may I notice from taking imipramine?
Side effects that you should report to your prescriber or health care professional as soon as possible:
• abnormal production of milk in females
• blurred vision or eye pain
• breast enlargement in both males and females
• confusion, hallucinations (seeing or hearing things that are not really there)
• difficulty breathing
• fainting spells
• fever
• irregular or fast, pounding heartbeat, palpitations
• muscle stiffness, or spasms
• pain or difficulty passing urine, loss of bladder control
• seizures (convulsions)
• sexual difficulties (decreased sexual ability or desire, difficulty ejaculating)
• stomach pain
• swelling of the testicles
• tingling, pain, or numbness in the feet or hands
• tremor (shaking)
• unusual weakness or tiredness
• yellowing of the eyes or skin
Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• anxiety
• constipation, or diarrhea
• drowsiness or dizziness
• dry mouth
• headache
• increased sensitivity of the skin to sun or ultraviolet light
• loss of appetite
• nausea, vomiting
• skin rash or itching
• weight gain or loss
Where can I keep my medicine?
Keep out of the reach of children in a container that small children cannot open.
Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Throw away any unused medicine after the expiration date.
Last updated: 7/1/2002
Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.
| Veterinary Dictionary: imipramine |
A tricyclic antidepressant used in the treatment of behavior disorders and urinary incontinence in dogs.
| Wikipedia: Imipramine |
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|
| Systematic (IUPAC) name | |
|---|---|
| 3-(10,11-dihydro-5H-dibenzo[b,f]azepin-5-yl)-N,N-dimethylpropan-1-amine | |
| Identifiers | |
| CAS number | 50-49-7 |
| ATC code | N06AA02 |
| PubChem | 3696 |
| DrugBank | APRD00672 |
| ChemSpider | 3568 |
| Chemical data | |
| Formula | C19H24N2 |
| Mol. mass | 280.407 |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | Hepatic Main active metabolite desipramine |
| Half life | 11-25 hours |
| Excretion | Renal |
| Therapeutic considerations | |
| Pregnancy cat. |
D(US) |
| Legal status |
℞ Prescription only |
| Routes | Oral |
 (what is this?) (verify) |
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Imipramine (sold as Antideprin, Deprimin, Deprinol, Depsonil, Dynaprin, Eupramin, Imipramil, Irmin, Janimine, Melipramin, Surplix, Tofranil) is an antidepressant medication, a tricyclic antidepressant of the dibenzazepine group. Imipramine is mainly used in the treatment of major depression and enuresis (inability to control urination).
It has also been evaluated for use in panic disorder.[1]
Contents |
History
Imipramine was, in the late 1950s, the first tricyclic antidepressant to be developed (by Ciba-Geigy). It was first tried against psychotic disorders, such as 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[citation needed]. It is not surprising, therefore, that 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 less tolerable. Therefore, it became 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.
Mechanisms Of Action
Imipramine, a tertiary amine, affects numerous neurotransmitter systems known 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. Imipramine has been shown to interact with opioid systems in the central nervous system, possibly explaining some of its pain-relieving properties. [3] It is also becoming apparent that at least some of Imipramine's effects are epigenetic and related to its promotion of histone acetylation of the BDNF promotor in the hippocampus and also downregulation of histone deacetylase (HDAC5).[4]
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 with the exception of Clomipramine, 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. Regarding dopamine uptake, imipramine is far less potent than most other antidepressants (for example, it is 1/20 the 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.
BDNF Brain derived neurotrophic factor (BDNF) is implicated in neurogenesis in the hippocampus, and studies suggest that depressed patients have decreased levels of BDNF and reduced hippocampal neurogenesis. It is not clear how neurogenesis restores mood, as ablation of hippocampal neurogenesis in murine models do not show anxiety related or depression related behaviours. Chronic Imipramine administration results in increased histone acetylation (which is associated with transcriptional activation and decondensed chromatin) at the hippocampal BDNF promotor, and also reduced expression of hippocampal histone deacetylase (hdac5).[5]
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.[6]
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 |
Metabolism
Imipramine is converted to desipramine, another TCA, in the body.
Contraindications and precautions
(See Tricyclic antidepressants)
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This section requires expansion. |
Side-effects
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This section does not cite any references or sources. Please help improve this article by adding citations to reliable sources. Unsourced material may be challenged and removed. (September 2009) |
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.
Dosage
- Hospitalized patients: starting with 3 times 25 mg, increasing to 125 mg. Up to 300 mg may be given in resistant cases. After remission dose is often reduced to 50 to 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.
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.
References
- ^ Lepola U, Arató M, Zhu Y, Austin C (June 2003). "Sertraline versus imipramine treatment of comorbid panic disorder and major depressive disorder". J Clin Psychiatry 64 (6): 654–62. PMID 12823079. http://www.psychiatrist.com/privatepdf/2003/v64n06/v64n0606.pdf.
- ^ Bottlender R, Rudolf D, Strauss A, Möller HJ (1998). "Antidepressant-associated maniform states in acute treatment of patients with bipolar-I depression". European Archives of Psychiatry and Clinical Neuroscience 248 (6): 296–300. doi:. PMID 9928908.
- ^ Effects of imipramine administration on mu-opioid receptor immunostaining in the rat forebrain. de Gandarias JM, Echevarria E, Acebes I, Silio M, Casis L. 1: Arzneimittelforschung. 1998 Jul;48(7):717-9 http://www.ncbi.nlm.nih.gov/pubmed/9706370
- ^ Tsankova NM, Berton O, Renthal W, Kumar A, Neve RL, Nestler EJ (April 2006). "Sustained hippocampal chromatin regulation in a mouse model of depression and antidepressant action". Nature Neuroscience 9 (4): 519–25. doi:. PMID 16501568.
- ^ Krishnan V, Nestler EJ (October 2008). "The molecular neurobiology of depression". Nature 455 (7215): 894–902. doi:. PMID 18923511.
- ^ Richelson E (May 2001). "Pharmacology of antidepressants". Mayo Clinic Proceedings. Mayo Clinic 76 (5): 511–27. doi:. PMID 11357798.
External links
- Imipramine - Medicinenet.com
- Neurotransmitter - Neurotransmitter.net
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Mentioned in
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