what was the name??
To Life!
Thread Starter
Join Date: Oct 2003
Location: Rhode Island
Posts: 9,293
what was the name??
Someone posted here about an antidepressant that was different from an SSRI. Instead of being a reuptake, it allowed more seretonin to stay in the brain. The function of the medication was just the opposit of the SSRI types.
I'm interested in looking into it, in case I want another antidepressant next winter. I didn't do well on the SSRIs and Welbutrin gave me panic attacks. So, I want a plan in place just in case. But, I can't remember the name of it. I know I looked it up on the web at the time, and didn't book mark it. So, now, I don't know the name.
Can anyone help me remember? Thanks.
Shalom!
I'm interested in looking into it, in case I want another antidepressant next winter. I didn't do well on the SSRIs and Welbutrin gave me panic attacks. So, I want a plan in place just in case. But, I can't remember the name of it. I know I looked it up on the web at the time, and didn't book mark it. So, now, I don't know the name.
Can anyone help me remember? Thanks.
Shalom!
Member
Join Date: May 2005
Location: Nowhere
Posts: 889
Hm I found this:
Tianeptine
From Wikipedia, the free encyclopedia
Jump to: navigation, search
Tianeptine chemical structure
Tianeptine
Systematic (IUPAC) name
7-((3-Chloro-6,11-dihydro-6-methyldibenzo(c,f)
(1,2)thiazepin-11-yl)amino)heptanoic acid S,S-dioxide
Identifiers
CAS number 66981-73-5
ATC code N06AX14
PubChem 68870
Chemical data
Formula C21H25ClN2O4S
Mol. weight 436.953 g/mol
Pharmacokinetic data
Bioavailability 99 +/- 29%[1]
Metabolism hepatic
Half life 2.5 hours (2.5 +/- 1.1 h)[1]
Excretion Renal[1]
Therapeutic considerations
Pregnancy cat.
?
Legal status
℞ Prescription only
Routes oral
Tianeptine (INN) (Stablon®, Coaxil®, Tatinol®), is described as an Selective Serotonin Reuptake Enhancer (SSRE), structurally similar to the tricyclic antidepressants. Unlike the tricyclics, however, it enhances the reuptake of serotonin instead of blocking it. Interestingly, tianeptine along with its two metabolites (S8849, S3139) does not affect uptake of monoamines (i.e. DA, 5-HT, and noradrenaline) in vitro. Results from in vivo studies show that monoamine reuptake is indeed enhanced, suggesting a mechanism independent of SERT. [2] No data is available regarding effects of the drug on postsynaptic receptors.
Tianeptine has strong antidepressant and anxiolytic properties with a relative lack of sedative, anticholinergic and cardiovascular adverse effects, making it particularly suitable for use in elderly patients and in those following alcohol withdrawal as these patients are known to be more sensitive to the adverse effects of psychotropic drugs.
Currently, tianeptine is approved in France. The manufacturer there is Servier. It is also marketed to a host of countries in Europe, Asia and Latin America.
Contents
[hide]
* 1 Uses
o 1.1 Approved
o 1.2 Investigational/Off-Label/Unapproved
* 2 Contraindications
* 3 Side effects
* 4 Drug Interactions
* 5 Usual Doses
* 6 Coping with suicide risks
* 7 Abuse Potential
* 8 References and End Notes
* 9 See also
* 10 External links
[edit]
Uses
[edit]
Approved
Tianeptine shows efficacy against serious depressive episodes (major depression), comparable to amitriptyline, imipramine and fluoxetine, but with fewer side effects. It was even more effective than maprotiline in a group of patients with coexisting depression and anxiety. Tianeptine also displays significant anxiolytic properties and is useful in treating a spectrum of anxiety disorders including panic disorder, as evidenced by a study in which those administered 35% CO2 gas on paroxetine (Paxil) or tianeptine (Stablon) therapy showed equivalent panic-blocking effects.[3]
[edit]
Investigational/Off-Label/Unapproved
Tianeptine has been reported to be very effective for asthma starting in August of 1998, when Dr. Fuad Lechin and colleagues at the Central University of Venezuela Institute of Experimental Medicine in Caracas published the results of a 52-week randomized controlled trial of asthmatic children; the children in the groups that received tianeptine had a sharp decrease in clinical rating and increased lung function.[4] Two years earlier, they had found a close, positive association between free serotonin in plasma and severity of asthma in symptomatic patients.[5] As tianeptine was the only agent known to reduce both free serotonin in plasma and enhance uptake in platelets, they decided to use it to see if reducing free serotonin levels in plasma would help.[4] By November of 2004, there had been two double-blind placebo-controlled crossover trials, and a 25,000+ patient open-label study lasting over seven years, all showing effectiveness.[6]
A 2005 study in Egypt demonstrated tianeptine to be effective in men with depression and erectile dysfunction.[7]
Tianeptine is also being studied in the treatment of ADD/ADHD.
[edit]
Contraindications
According to Servier International, tianeptine is contraindicated in children under 15 years of age, people taking MAOIs, and pregnant or lactating women.[8] However, as of 2005, there are no studies published showing increased risk of birth defects.[9]
[edit]
Side effects
Tianeptine was both studied for short-term (3 month) and long-term treatment (12 months) and equally well tolerated. The studies encompassed 1,300 to nearly 3,000 patients each.
Side effects are as follows (Amitriptyline vs Tianeptine):
* dry mouth (38 vs 20%)
* constipation (19 vs 15%)
* dizziness/syncope (23 vs 13%)
* drowsiness (17 vs 10%)
* postural hypotension (8 vs 3%)
* Insomnia and nightmares occur more often in tianeptine than in amitriptyline recipients (7 vs 20%)
Costa e Silva and colleagues at the Jardim Botanico in Rio de Janeiro, Brazil reported a greater frequency of headaches in the tianeptine group as compared with placebo.[10]
So far neither seizures nor kidney or bone marrow damage have been noted.
Liver toxicity has been observed very rarely, as is the case with amineptine, however, this is thought to be due to genetic predisposition and is often preceded by rash, itching, fever, and/or abdominal pain.
Sema Gülen Yıldırım and colleagues reported in 2004 of a case of hypomania caused by tianeptine.[11]
[edit]
Drug Interactions
No sufficient data available at present date.
[edit]
Usual Doses
Although Servier's official recommendation is 12.5mg three times per day before the main meals of the day, lower or higher doses may be used as determined by your prescribing physician.
[edit]
Coping with suicide risks
As is generally true for activating/nonsedating antidepressants, particularly agitated patients or those developing increase of energy together with suicidal thoughts before remission occurs will normally need initial comedication (1 to 4 weeks) with an effective sedating drug such as a benzodiazepine or the neuroleptic chlorprothixene. Additionally, hospitalisation of these patients is desirable (close observation possible). These measures to lower the risk of suicide should be continued until remission of depression is stable.
[edit]
Abuse Potential
Relatively rare and only seen thus far in a few patients with previous or pre-existing multi-substance abuse disorders. One patient reportedly consumed a total of 240 tablets per day for several months and was later successfully detoxified in an inpatient setting. Singapore has restricted the prescription of tianeptine to psychiatrists. Bahrain has designated tianeptine a controlled substance.
[edit]
References and End Notes
* Tianeptine: a review of its use in depressive disorders. Retrieved on 7 October 2005.
1. ^ a b c Royer RJ, Albin H, Barrucand D, Salvadori-Failler C, Kamoun A (1988). "Pharmacokinetic and metabolic parameters of tianeptine in healthy volunteers and in populations with risk factors.". Clinical Neuropharmacology 11 (Suppl 2): S90-6. PMID 3180120. List of Library Holdings Worldwide
2. ^ Mennini T, Mocaer E, Garattini S (1987). "Tianeptine, a selective enhancer of serotonin uptake in rat brain.". Naunyn-Schmiedeberg's Archives of Pharmacology 336 (5): 478-82. PMID 3437921. List of Library Holdings Worldwide
3. ^ Schruers K, Griez E (2004). "The effects of tianeptine or paroxetine on 35% CO2 provoked panic in panic disorder.". Journal of Psychopharmacology 18 (4): 553-8.
4. ^ a b Lechin F, van der Dijs B, Orozco B, Jara H, Rada I, Lechin ME, Lechin AE (1998). "The serotonin uptake-enhancing drug tianeptine suppresses asthmatic symptoms in children: a double-blind, crossover, placebo-controlled study.". Journal of Clinical Pharmacology 38 (10): 918-25. PMID 9807972. Fulltext options (subscription required) List of Library Holdings Worldwide
5. ^ Lechin F, van der Dijs B, Orozco B, Lechin M, Lechin AE (1996). "Increased levels of free serotonin in plasma of symptomatic asthmatic patients.". Annals of Allergy, Asthma & Immunology : Official Publication of the American College of Allergy, Asthma, & Immunology 77 (3): 245-53. PMID 8814052. List of Library Holdings Worldwide
6. ^ Lechin F, van der Dijs B, Lechin AE (2004). "Treatment of bronchial asthma with tianeptine.". Methods and Findings in Experimental and Clinical Pharmacology 26 (9): 697-701.
7. ^ El-Shafey, Hany, Ahmad Atteya, Samir Abu el-Magd, Ahmad Hassanein, Ahmad Fathy, and Rany Shamloul (2005). "Tianeptine Can Be Effective in Men with Depression and Erectile Dysfunction". Journal of Sexual Medicine 0 (0). DOI:10.1111/j.1743-6109.2005.00141.x.
8. ^ Les Labotoires Servier (2005). STABLON (Tianeptine) - Summary of Product Characteristics. STABLON (Tianeptine) - OVERVIEW. Servier International. Retrieved on 8 October 2005.
9. ^ Google search of The National Center for Biotechnology Information website for articles containing "tianeptine" and "prenatal". Retrieved on 20 October 2005.
10. ^ Costa e Silva JA, Ruschel SI, Caetano D, Rocha FL, da Silva Lippi JR, Arruda S, Ozun M (1997). "Placebo-controlled study of tianeptine in major depressive episodes.". Neuropsychobiology 35 (1): 24-9. PMID 9018020. List of Library Holdings Worldwide
11. ^ Yıldırım, Sema Gülen, Ayşe Devrim Başterzi and Erol Göka (2004). "Tianeptinin Neden Olduğu Hipomani; Bir Olgu Sunumu / Tianeptine Induced Mania: A Case Report". Klinik Psikiyatri Dergisi 7 (4): 177-180.
[edit]
See also
From Wikipedia, the free encyclopedia
Jump to: navigation, search
Tianeptine chemical structure
Tianeptine
Systematic (IUPAC) name
7-((3-Chloro-6,11-dihydro-6-methyldibenzo(c,f)
(1,2)thiazepin-11-yl)amino)heptanoic acid S,S-dioxide
Identifiers
CAS number 66981-73-5
ATC code N06AX14
PubChem 68870
Chemical data
Formula C21H25ClN2O4S
Mol. weight 436.953 g/mol
Pharmacokinetic data
Bioavailability 99 +/- 29%[1]
Metabolism hepatic
Half life 2.5 hours (2.5 +/- 1.1 h)[1]
Excretion Renal[1]
Therapeutic considerations
Pregnancy cat.
?
Legal status
℞ Prescription only
Routes oral
Tianeptine (INN) (Stablon®, Coaxil®, Tatinol®), is described as an Selective Serotonin Reuptake Enhancer (SSRE), structurally similar to the tricyclic antidepressants. Unlike the tricyclics, however, it enhances the reuptake of serotonin instead of blocking it. Interestingly, tianeptine along with its two metabolites (S8849, S3139) does not affect uptake of monoamines (i.e. DA, 5-HT, and noradrenaline) in vitro. Results from in vivo studies show that monoamine reuptake is indeed enhanced, suggesting a mechanism independent of SERT. [2] No data is available regarding effects of the drug on postsynaptic receptors.
Tianeptine has strong antidepressant and anxiolytic properties with a relative lack of sedative, anticholinergic and cardiovascular adverse effects, making it particularly suitable for use in elderly patients and in those following alcohol withdrawal as these patients are known to be more sensitive to the adverse effects of psychotropic drugs.
Currently, tianeptine is approved in France. The manufacturer there is Servier. It is also marketed to a host of countries in Europe, Asia and Latin America.
Contents
[hide]
* 1 Uses
o 1.1 Approved
o 1.2 Investigational/Off-Label/Unapproved
* 2 Contraindications
* 3 Side effects
* 4 Drug Interactions
* 5 Usual Doses
* 6 Coping with suicide risks
* 7 Abuse Potential
* 8 References and End Notes
* 9 See also
* 10 External links
[edit]
Uses
[edit]
Approved
Tianeptine shows efficacy against serious depressive episodes (major depression), comparable to amitriptyline, imipramine and fluoxetine, but with fewer side effects. It was even more effective than maprotiline in a group of patients with coexisting depression and anxiety. Tianeptine also displays significant anxiolytic properties and is useful in treating a spectrum of anxiety disorders including panic disorder, as evidenced by a study in which those administered 35% CO2 gas on paroxetine (Paxil) or tianeptine (Stablon) therapy showed equivalent panic-blocking effects.[3]
[edit]
Investigational/Off-Label/Unapproved
Tianeptine has been reported to be very effective for asthma starting in August of 1998, when Dr. Fuad Lechin and colleagues at the Central University of Venezuela Institute of Experimental Medicine in Caracas published the results of a 52-week randomized controlled trial of asthmatic children; the children in the groups that received tianeptine had a sharp decrease in clinical rating and increased lung function.[4] Two years earlier, they had found a close, positive association between free serotonin in plasma and severity of asthma in symptomatic patients.[5] As tianeptine was the only agent known to reduce both free serotonin in plasma and enhance uptake in platelets, they decided to use it to see if reducing free serotonin levels in plasma would help.[4] By November of 2004, there had been two double-blind placebo-controlled crossover trials, and a 25,000+ patient open-label study lasting over seven years, all showing effectiveness.[6]
A 2005 study in Egypt demonstrated tianeptine to be effective in men with depression and erectile dysfunction.[7]
Tianeptine is also being studied in the treatment of ADD/ADHD.
[edit]
Contraindications
According to Servier International, tianeptine is contraindicated in children under 15 years of age, people taking MAOIs, and pregnant or lactating women.[8] However, as of 2005, there are no studies published showing increased risk of birth defects.[9]
[edit]
Side effects
Tianeptine was both studied for short-term (3 month) and long-term treatment (12 months) and equally well tolerated. The studies encompassed 1,300 to nearly 3,000 patients each.
Side effects are as follows (Amitriptyline vs Tianeptine):
* dry mouth (38 vs 20%)
* constipation (19 vs 15%)
* dizziness/syncope (23 vs 13%)
* drowsiness (17 vs 10%)
* postural hypotension (8 vs 3%)
* Insomnia and nightmares occur more often in tianeptine than in amitriptyline recipients (7 vs 20%)
Costa e Silva and colleagues at the Jardim Botanico in Rio de Janeiro, Brazil reported a greater frequency of headaches in the tianeptine group as compared with placebo.[10]
So far neither seizures nor kidney or bone marrow damage have been noted.
Liver toxicity has been observed very rarely, as is the case with amineptine, however, this is thought to be due to genetic predisposition and is often preceded by rash, itching, fever, and/or abdominal pain.
Sema Gülen Yıldırım and colleagues reported in 2004 of a case of hypomania caused by tianeptine.[11]
[edit]
Drug Interactions
No sufficient data available at present date.
[edit]
Usual Doses
Although Servier's official recommendation is 12.5mg three times per day before the main meals of the day, lower or higher doses may be used as determined by your prescribing physician.
[edit]
Coping with suicide risks
As is generally true for activating/nonsedating antidepressants, particularly agitated patients or those developing increase of energy together with suicidal thoughts before remission occurs will normally need initial comedication (1 to 4 weeks) with an effective sedating drug such as a benzodiazepine or the neuroleptic chlorprothixene. Additionally, hospitalisation of these patients is desirable (close observation possible). These measures to lower the risk of suicide should be continued until remission of depression is stable.
[edit]
Abuse Potential
Relatively rare and only seen thus far in a few patients with previous or pre-existing multi-substance abuse disorders. One patient reportedly consumed a total of 240 tablets per day for several months and was later successfully detoxified in an inpatient setting. Singapore has restricted the prescription of tianeptine to psychiatrists. Bahrain has designated tianeptine a controlled substance.
[edit]
References and End Notes
* Tianeptine: a review of its use in depressive disorders. Retrieved on 7 October 2005.
1. ^ a b c Royer RJ, Albin H, Barrucand D, Salvadori-Failler C, Kamoun A (1988). "Pharmacokinetic and metabolic parameters of tianeptine in healthy volunteers and in populations with risk factors.". Clinical Neuropharmacology 11 (Suppl 2): S90-6. PMID 3180120. List of Library Holdings Worldwide
2. ^ Mennini T, Mocaer E, Garattini S (1987). "Tianeptine, a selective enhancer of serotonin uptake in rat brain.". Naunyn-Schmiedeberg's Archives of Pharmacology 336 (5): 478-82. PMID 3437921. List of Library Holdings Worldwide
3. ^ Schruers K, Griez E (2004). "The effects of tianeptine or paroxetine on 35% CO2 provoked panic in panic disorder.". Journal of Psychopharmacology 18 (4): 553-8.
4. ^ a b Lechin F, van der Dijs B, Orozco B, Jara H, Rada I, Lechin ME, Lechin AE (1998). "The serotonin uptake-enhancing drug tianeptine suppresses asthmatic symptoms in children: a double-blind, crossover, placebo-controlled study.". Journal of Clinical Pharmacology 38 (10): 918-25. PMID 9807972. Fulltext options (subscription required) List of Library Holdings Worldwide
5. ^ Lechin F, van der Dijs B, Orozco B, Lechin M, Lechin AE (1996). "Increased levels of free serotonin in plasma of symptomatic asthmatic patients.". Annals of Allergy, Asthma & Immunology : Official Publication of the American College of Allergy, Asthma, & Immunology 77 (3): 245-53. PMID 8814052. List of Library Holdings Worldwide
6. ^ Lechin F, van der Dijs B, Lechin AE (2004). "Treatment of bronchial asthma with tianeptine.". Methods and Findings in Experimental and Clinical Pharmacology 26 (9): 697-701.
7. ^ El-Shafey, Hany, Ahmad Atteya, Samir Abu el-Magd, Ahmad Hassanein, Ahmad Fathy, and Rany Shamloul (2005). "Tianeptine Can Be Effective in Men with Depression and Erectile Dysfunction". Journal of Sexual Medicine 0 (0). DOI:10.1111/j.1743-6109.2005.00141.x.
8. ^ Les Labotoires Servier (2005). STABLON (Tianeptine) - Summary of Product Characteristics. STABLON (Tianeptine) - OVERVIEW. Servier International. Retrieved on 8 October 2005.
9. ^ Google search of The National Center for Biotechnology Information website for articles containing "tianeptine" and "prenatal". Retrieved on 20 October 2005.
10. ^ Costa e Silva JA, Ruschel SI, Caetano D, Rocha FL, da Silva Lippi JR, Arruda S, Ozun M (1997). "Placebo-controlled study of tianeptine in major depressive episodes.". Neuropsychobiology 35 (1): 24-9. PMID 9018020. List of Library Holdings Worldwide
11. ^ Yıldırım, Sema Gülen, Ayşe Devrim Başterzi and Erol Göka (2004). "Tianeptinin Neden Olduğu Hipomani; Bir Olgu Sunumu / Tianeptine Induced Mania: A Case Report". Klinik Psikiyatri Dergisi 7 (4): 177-180.
[edit]
See also
Member
Join Date: May 2005
Location: Nowhere
Posts: 889
Oh and I also found this one, which is a newer anti depressant but it wasn't specifically what you were looking for (opposite working of a SSRI would be SSRE):
Marte
Mirtazapine
From Wikipedia, the free encyclopedia
Jump to: navigation, search
Mirtazapine chemical structure
Mirtazapine
Systematic (IUPAC) name
1,2,3,4,10,14b-hexahydro-2-methylpyrazino[2,1-a] pyrido [2,3-c] benzazepine
Identifiers
CAS number 61337-67-5
ATC code N06AX11
PubChem 4205
Chemical data
Formula C17H19N3
Mol. weight 265.36
Pharmacokinetic data
Bioavailability 50%
Metabolism Liver
Half life 37 hours (females), 26 hours (males)
Excretion ?
Therapeutic considerations
Pregnancy cat.
C
Legal status
?
Routes ?
Mirtazapine is an antidepressant introduced by Organon International in 1996 used for the treatment of mild to severe depression. Although Mirtazapine has a tetracyclic chemical structure it is classified as a noradrenergic and specific serotonergic antidepressant (NaSSA). Mirtazapine may be used in preference to an SSRI due to the fact that it causes fewer sexual dysfunction problems. Due to its unique pharmacologic profile, mirtazapine is virtually devoid of anticholinergic, adrenolytic, and serotonin-related side effects[1]. Mirtazapine is relatively safe if an overdose is taken.[2]
Contents
[hide]
* 1 Trade Names
* 2 Indications
o 2.1 Approved
o 2.2 Unapproved/Off-label/Investigational
* 3 Mechanism of action
* 4 Side effects
o 4.1 Side effects occurring commonly:
o 4.2 Side effects occurring rarely:
o 4.3 Side effects to tell your doctor about and stop taking mirtazapine immediately
* 5 Dosage
* 6 Pregnancy and Lactation
* 7 Drug-Drug Interactions
* 8 External links
* 9 References
[edit]
Trade Names
Mirtazapine is marketed under the tradenames Remeron® in the U.S. and Finland, Avanza® and Axit® in Australia, Zispin® in the UK & Ireland, Norset® in France, Remergon® in Belgium, Remergil® in Germany and Mirtabene® in Austria.
[edit]
Indications
[edit]
Approved
Mirtazapine is primarily used to treat the symptoms of mild to severe depression.[3]
[edit]
Unapproved/Off-label/Investigational
There is also eveidence that mirtazapine can be used to treat panic disorder (PD)[4], generalized anxiety disorder (GAD)[5], obsessive-compulsive disorder (OCD)[6], post traumatic stress disorder (PTSD)[7] and pruritus[8]. Mirtazapine is thought to be effective in the prophylactic treatment of chronic tension-type headache[9].
[edit]
Mechanism of action
It is thought to work by blocking presynaptic alpha-2 adrenergic receptors that normally inhibit the release of the neurotransmitters norepinephrine (noradrenaline) and serotonin, thereby increasing active levels in the synapse. Mirtazapine also blocks post-synaptic 5-HT2 and 5-HT3 receptors—an action which is thought to enhance serotonergic neurotransmission while causing a low incidence of side effects.
[edit]
Side effects
The side effects that do occur are thought to be primarily related to the blockage of histamine receptors, which decreases with higher dosages.
[edit]
Side effects occurring commonly:
* Increased appetite
* weight gain
* Drowsiness, especially at lower doses during the first few weeks of treatment
* Dizziness
* Headache
* General or local swelling
* Visual hallucinations (when taken during the day)
[edit]
Side effects occurring rarely:
* Mania
* nightmares and vivid dreams
* Seizures
* Tremor
* Muscle twitching and Restless Legs Syndrome
* Pins and needles
* Rash and skin eruptions
* Pain in the joints or muscles
* Low blood pressure
* Agranulocytosis
[edit]
Side effects to tell your doctor about and stop taking mirtazapine immediately
* An allergic reaction; signs of swelling of the lips, face and tongue, difficulty in breathing, rash or itching (especially affecting the whole body) or feeling faint.
* Signs of infection such as fever, sore throat, mouth ulcers or stomach upset.
* Jaundice (yellowing of the skin and/or eyes).
Interestingly, its side effect profile can be used for benefit in certain clinical situations. The drowsiness, increased appetite, and weight gain it causes are useful in patients with depressive disorders with prominent sleep and appetite disturbances. In addition, it is quite useful in inpatient situations in which patients suffer from nausea since it also antagonizes the 5-HT3 receptor, the target of the popular anti-emetic ondansetron (Zofran®).
[edit]
Dosage
The usual starting dose for mirtazapine is 7.5 - 15 mg once daily, usually at bedtime (Due to the sedative nature and disturbed visual perception). Doses may be increased every 1-2 weeks up to a dose of 45 mg, the maxium daily dose is 90 mg. It may be taken with or without food. Dissolving tablets can even be taken without water.
[edit]
Pregnancy and Lactation
* Pregnancy : Sufficient data in humans is lacking. The use should be justified by the severity of the condition to be treated.
* Lactation : Sufficient data in humans is also lacking. Additionally, Mirtazapine may be found in the maternal milk in significant concentrations. The use in breastfeeding women should be carefully weighed against possible risks.
[edit]
Drug-Drug Interactions
Due to the sedative effects of Mirtazapine, alcohol should not be taken. Excessive sedation may result when it is used with other sedating drugs, such as benzodiazepines. Mirtazapine should not be used within 14 days of the use of a monoamine oxidase inhibitor because of the possibility that a hypertensive emergency will be triggered.
[edit]
External links
* Patient Information Leaflet (pdf)
[edit]
References
1. ↑ Burrows GD, Kremer CM. (1997). "Mirtazapine: clinical advantages in the treatment of depression.". Journal of Clinical Psychopharmacology 17 (2S): 34S-39S. PMID 9090576.
2. ↑ Velazquez C, Carlson A, Stokes KA, Leikin JB. (2001). "Relative safety of mirtazapine overdose.". Veterinary and Human Toxicology 43 (6): 342-344. PMID 11757992.
3. ↑ Gorman JM (1999). "Mirtazapine: clinical overview.". Journal of Clinical Psychiatry 60 (17): 9-13. PMID 10446735.
4. ↑ Baldwin DS, Anderson IM, Nutt DJ, Bandelow B, Bond A, Davidson JR, den Boer JA, Fineberg NA, Knapp M, Scott J, Wittchen HU (2005). "Evidence-based guidelines for the pharmacological treatment of anxiety disorders: recommendations from the British Association for Psychopharmacology.". Journal of Psychopharmacology 19 (6): 567-596. PMID 16272179.
5. ↑ Goodnick PJ, Puig A, DeVane CL, Freund BV (1999). "Mirtazapine in major depression with comorbid generalized anxiety disorder". Journal of Clinical Psychiatry 60 (7): 446-448. PMID 10453798.
6. ↑ Koran LM, Gamel NN, Choung HW, Smith EH, Aboujaoude EN (2005). "Mirtazapine for obsessive-compulsive disorder: an open trial followed by double-blind discontinuation". Journal of Clinical Psychiatry 66 (4): 515-520. PMID 15816795.
7. ↑ Baldwin DS, Anderson IM, Nutt DJ, Bandelow B, Bond A, Davidson JR, den Boer JA, Fineberg NA, Knapp M, Scott J, Wittchen HU (2005). "Evidence-based guidelines for the pharmacological treatment of anxiety disorders: recommendations from the British Association for Psychopharmacology.". Journal of Psychopharmacology 19 (6): 567-596. PMID 16272179.
8. ↑ Davis MP, Frandsen JL, Walsh D, Andresen S, Taylor S. (2003). "Mirtazapine for pruritus.". Journal of pain and symptom management 25 (3): 288-291. PMID 12614964.
9. ↑ Bendtsen L, Jensen R (2004). "Mirtazapine is effective in the prophylactic treatment of chronic tension-type headache.". Neurology 62 (10): 1706-1711. PMID 15159466.
From Wikipedia, the free encyclopedia
Jump to: navigation, search
Mirtazapine chemical structure
Mirtazapine
Systematic (IUPAC) name
1,2,3,4,10,14b-hexahydro-2-methylpyrazino[2,1-a] pyrido [2,3-c] benzazepine
Identifiers
CAS number 61337-67-5
ATC code N06AX11
PubChem 4205
Chemical data
Formula C17H19N3
Mol. weight 265.36
Pharmacokinetic data
Bioavailability 50%
Metabolism Liver
Half life 37 hours (females), 26 hours (males)
Excretion ?
Therapeutic considerations
Pregnancy cat.
C
Legal status
?
Routes ?
Mirtazapine is an antidepressant introduced by Organon International in 1996 used for the treatment of mild to severe depression. Although Mirtazapine has a tetracyclic chemical structure it is classified as a noradrenergic and specific serotonergic antidepressant (NaSSA). Mirtazapine may be used in preference to an SSRI due to the fact that it causes fewer sexual dysfunction problems. Due to its unique pharmacologic profile, mirtazapine is virtually devoid of anticholinergic, adrenolytic, and serotonin-related side effects[1]. Mirtazapine is relatively safe if an overdose is taken.[2]
Contents
[hide]
* 1 Trade Names
* 2 Indications
o 2.1 Approved
o 2.2 Unapproved/Off-label/Investigational
* 3 Mechanism of action
* 4 Side effects
o 4.1 Side effects occurring commonly:
o 4.2 Side effects occurring rarely:
o 4.3 Side effects to tell your doctor about and stop taking mirtazapine immediately
* 5 Dosage
* 6 Pregnancy and Lactation
* 7 Drug-Drug Interactions
* 8 External links
* 9 References
[edit]
Trade Names
Mirtazapine is marketed under the tradenames Remeron® in the U.S. and Finland, Avanza® and Axit® in Australia, Zispin® in the UK & Ireland, Norset® in France, Remergon® in Belgium, Remergil® in Germany and Mirtabene® in Austria.
[edit]
Indications
[edit]
Approved
Mirtazapine is primarily used to treat the symptoms of mild to severe depression.[3]
[edit]
Unapproved/Off-label/Investigational
There is also eveidence that mirtazapine can be used to treat panic disorder (PD)[4], generalized anxiety disorder (GAD)[5], obsessive-compulsive disorder (OCD)[6], post traumatic stress disorder (PTSD)[7] and pruritus[8]. Mirtazapine is thought to be effective in the prophylactic treatment of chronic tension-type headache[9].
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Mechanism of action
It is thought to work by blocking presynaptic alpha-2 adrenergic receptors that normally inhibit the release of the neurotransmitters norepinephrine (noradrenaline) and serotonin, thereby increasing active levels in the synapse. Mirtazapine also blocks post-synaptic 5-HT2 and 5-HT3 receptors—an action which is thought to enhance serotonergic neurotransmission while causing a low incidence of side effects.
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Side effects
The side effects that do occur are thought to be primarily related to the blockage of histamine receptors, which decreases with higher dosages.
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Side effects occurring commonly:
* Increased appetite
* weight gain
* Drowsiness, especially at lower doses during the first few weeks of treatment
* Dizziness
* Headache
* General or local swelling
* Visual hallucinations (when taken during the day)
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Side effects occurring rarely:
* Mania
* nightmares and vivid dreams
* Seizures
* Tremor
* Muscle twitching and Restless Legs Syndrome
* Pins and needles
* Rash and skin eruptions
* Pain in the joints or muscles
* Low blood pressure
* Agranulocytosis
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Side effects to tell your doctor about and stop taking mirtazapine immediately
* An allergic reaction; signs of swelling of the lips, face and tongue, difficulty in breathing, rash or itching (especially affecting the whole body) or feeling faint.
* Signs of infection such as fever, sore throat, mouth ulcers or stomach upset.
* Jaundice (yellowing of the skin and/or eyes).
Interestingly, its side effect profile can be used for benefit in certain clinical situations. The drowsiness, increased appetite, and weight gain it causes are useful in patients with depressive disorders with prominent sleep and appetite disturbances. In addition, it is quite useful in inpatient situations in which patients suffer from nausea since it also antagonizes the 5-HT3 receptor, the target of the popular anti-emetic ondansetron (Zofran®).
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Dosage
The usual starting dose for mirtazapine is 7.5 - 15 mg once daily, usually at bedtime (Due to the sedative nature and disturbed visual perception). Doses may be increased every 1-2 weeks up to a dose of 45 mg, the maxium daily dose is 90 mg. It may be taken with or without food. Dissolving tablets can even be taken without water.
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Pregnancy and Lactation
* Pregnancy : Sufficient data in humans is lacking. The use should be justified by the severity of the condition to be treated.
* Lactation : Sufficient data in humans is also lacking. Additionally, Mirtazapine may be found in the maternal milk in significant concentrations. The use in breastfeeding women should be carefully weighed against possible risks.
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Drug-Drug Interactions
Due to the sedative effects of Mirtazapine, alcohol should not be taken. Excessive sedation may result when it is used with other sedating drugs, such as benzodiazepines. Mirtazapine should not be used within 14 days of the use of a monoamine oxidase inhibitor because of the possibility that a hypertensive emergency will be triggered.
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External links
* Patient Information Leaflet (pdf)
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References
1. ↑ Burrows GD, Kremer CM. (1997). "Mirtazapine: clinical advantages in the treatment of depression.". Journal of Clinical Psychopharmacology 17 (2S): 34S-39S. PMID 9090576.
2. ↑ Velazquez C, Carlson A, Stokes KA, Leikin JB. (2001). "Relative safety of mirtazapine overdose.". Veterinary and Human Toxicology 43 (6): 342-344. PMID 11757992.
3. ↑ Gorman JM (1999). "Mirtazapine: clinical overview.". Journal of Clinical Psychiatry 60 (17): 9-13. PMID 10446735.
4. ↑ Baldwin DS, Anderson IM, Nutt DJ, Bandelow B, Bond A, Davidson JR, den Boer JA, Fineberg NA, Knapp M, Scott J, Wittchen HU (2005). "Evidence-based guidelines for the pharmacological treatment of anxiety disorders: recommendations from the British Association for Psychopharmacology.". Journal of Psychopharmacology 19 (6): 567-596. PMID 16272179.
5. ↑ Goodnick PJ, Puig A, DeVane CL, Freund BV (1999). "Mirtazapine in major depression with comorbid generalized anxiety disorder". Journal of Clinical Psychiatry 60 (7): 446-448. PMID 10453798.
6. ↑ Koran LM, Gamel NN, Choung HW, Smith EH, Aboujaoude EN (2005). "Mirtazapine for obsessive-compulsive disorder: an open trial followed by double-blind discontinuation". Journal of Clinical Psychiatry 66 (4): 515-520. PMID 15816795.
7. ↑ Baldwin DS, Anderson IM, Nutt DJ, Bandelow B, Bond A, Davidson JR, den Boer JA, Fineberg NA, Knapp M, Scott J, Wittchen HU (2005). "Evidence-based guidelines for the pharmacological treatment of anxiety disorders: recommendations from the British Association for Psychopharmacology.". Journal of Psychopharmacology 19 (6): 567-596. PMID 16272179.
8. ↑ Davis MP, Frandsen JL, Walsh D, Andresen S, Taylor S. (2003). "Mirtazapine for pruritus.". Journal of pain and symptom management 25 (3): 288-291. PMID 12614964.
9. ↑ Bendtsen L, Jensen R (2004). "Mirtazapine is effective in the prophylactic treatment of chronic tension-type headache.". Neurology 62 (10): 1706-1711. PMID 15159466.
Reach Out and Touch Faith
Join Date: Jul 2005
Location: On a Sailboat
Posts: 3,871
There is also one drug that is not in any family called Desyrel(Trazodone)
http://www.nlm.nih.gov/medlineplus/d...r/a681038.html
Have you ever tried the tricyclic antidepressants? These are the ones that were around before SSRIs. For years, I was on one of them, Tofranil (Imipramine). This was before the SSRI's and it worked wonders for 6 years for me. If I ever get that depressed again I will ask to be put back on that one, over the SSRIs (I'm on paxil for my anxiety now).
Tofranil worked so well that through the 80s it was the drug that they used in clinical trials to determine whether another drug was worth pursusing financially. If it didn't work as well as Tofranil studies were stopped.
Also in this family is Sinequan (doxepin) and Elavil.
Originally Posted by NIH
Trazodone is used to treat depression. Trazodone is in a class of medications called serotonin modulators. It works by increasing the amount of serotonin, a natural substance in the brain that helps maintain mental balance.
Have you ever tried the tricyclic antidepressants? These are the ones that were around before SSRIs. For years, I was on one of them, Tofranil (Imipramine). This was before the SSRI's and it worked wonders for 6 years for me. If I ever get that depressed again I will ask to be put back on that one, over the SSRIs (I'm on paxil for my anxiety now).
Tofranil worked so well that through the 80s it was the drug that they used in clinical trials to determine whether another drug was worth pursusing financially. If it didn't work as well as Tofranil studies were stopped.
Also in this family is Sinequan (doxepin) and Elavil.
One Day At A Time
Join Date: Jul 2006
Location: West Vancouver, BC
Posts: 405
Just wanted to say how good it makes me feel to see people being Pro-active in their treatment...
When I was initially so Ill I was unable to keep track of what they tried on me - what worked and what didn't and my memory in the depths or depression was non-existant..not that it is the greatest now..but I really wished I had kept a record...I changed Doctors several times to finally find the one (I call my Guru - He's excellent) I have now...I really can't remember the combinations I was on before ..10 yrs is a long time...
A good doctor is open to suggestions and questions about potential medications..when I come up with something and research it - He will definately consider it as long as it isn't contraindicated for me,.
When I was initially so Ill I was unable to keep track of what they tried on me - what worked and what didn't and my memory in the depths or depression was non-existant..not that it is the greatest now..but I really wished I had kept a record...I changed Doctors several times to finally find the one (I call my Guru - He's excellent) I have now...I really can't remember the combinations I was on before ..10 yrs is a long time...
A good doctor is open to suggestions and questions about potential medications..when I come up with something and research it - He will definately consider it as long as it isn't contraindicated for me,.
To Life!
Thread Starter
Join Date: Oct 2003
Location: Rhode Island
Posts: 9,293
I agree, upanddownjj;
It's important to be responsible for ourselves. I went through what you did with multiple meds and being stoned out of my mind. I won't go there again!
I believe my doc and I are partners in my health care. He has expertise on meds and health; I have expertise on ME. Neither of us works effectively without the other.
And I, too, feel like I have the best doc in the world!
Shalom!
It's important to be responsible for ourselves. I went through what you did with multiple meds and being stoned out of my mind. I won't go there again!
I believe my doc and I are partners in my health care. He has expertise on meds and health; I have expertise on ME. Neither of us works effectively without the other.
And I, too, feel like I have the best doc in the world!
Shalom!
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