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Amitriptyline

Amitriptyline (Elavil, Endep, Saroten, Sarotex, Redomex, Adepril, Amineurin, Domical, Euplit, Laroxyl, Lentizol, Miketorin, Triptizol, Tryptanol, Tryptizol) is one of the most frequently used tricyclic antidepressants. Its effects are mediated notably by increasing serotonin and norepinephrine concentrations in the brain. However, other modes of action are likely to contribute to its antidepressant effects as well. This pharmacological profile is also why, beyond its use for treating mood disorders, it can be beneficial for the treatment of certain types of pain. It has practically no value as a recreational drug.

Contents




[top]Introduction to Amitriptyline



[top]Using Amitriptyline

[top]Ways of Administration

[top]Oral Amitriptyline

Oral use is the most common form of administration for Amitryptyline, and it is normally provided in 10mg, 25mg, or 50mg pills. Other routes of administration would appear to be pointless, as it has no recreational value.

[top]Insufflating Amitriptyline

[top]Injecting Amitriptyline

[top]Plugging Amitriptyline

[top]Effects of Amitriptyline

[top]Combinations with Amitriptyline

[top]Different Uses for Amitriptyline

Amitryptyline is sometimes prescribed for sleep disorders in the UK when other drugs have been found to be ineffective.


[top]Pharmacology of Amitriptyline

[top]General


Amitriptyline is a Serotonin-Norepinephrine reuptake inhibitor. It also is a negative allosteric modulator at the PCP site of the NMDA receptor.

LD50 (mg/kg) :
Mice : 350 orally, 65 intraperitoneal
Rat : 380 orally, 75 intraperitoneal

[top]Targets, Enzymes, and Transporters

[top]Targets

Target
Action
Sodium-dependent noradrenaline transporter Inhibitor[1][2]
Sodium-dependent serotonin transporter Inhibitor[3][4][1][5][6][2][7]
5-hydroxytryptamine receptor 1A Inhibitor[8]
5-hydroxytryptamine receptor 2A Inhibitor[8]
Delta-type opioid receptor Agonist[9]
Kappa-type opioid receptor Agonist[9]
High affinity nerve growth factor receptor Agonist[10]
BDNF/NT-3 growth factors receptor Agonist[10]
Alpha-1A adrenergic receptor Antagonist[8][11]
Alpha-1D adrenergic receptor Antagonist[11]
Alpha-2A adrenergic receptor Antagonist[8][12]
Histamine H1 receptor Antagonist
Muscarinic acetylcholine receptor M1 Antagonist[8]
Muscarinic acetylcholine receptor M2 Antagonist[8]
Muscarinic acetylcholine receptor M3 Antagonist[8]
Muscarinic acetylcholine receptor M4 Antagonist[8]
Muscarinic acetylcholine receptor M5 Antagonist[8]
Potassium voltage-gated channel subfamily KQT member 2 Inhibitor[13]
Potassium voltage-gated channel subfamily A member 1 Inhibitor[13]
Potassium voltage-gated channel subfamily D member 2 Inhibitor[14]
Potassium voltage-gated channel subfamily D member 3 Inhibitor[14]
Histamine H2 receptor Blocker[15]
Histamine H4 receptor Binder[16]
Sigma non-opioid intracellular receptor 1 Agonist[17][7]
5-hydroxytryptamine receptor 2C Binder[18]
Alpha-1B adrenergic receptor Antagonist[11]
5-hydroxytryptamine receptor 7 Antagonist[19]
5-hydroxytryptamine receptor 1D Binder[7]
Mu-type opioid receptor Binder[20][21]
5-hydroxytryptamine receptor 1B Binder[7]
5-hydroxytryptamine receptor 6 Antagonist[22][23]
Potassium voltage-gated channel subfamily KQT member 3 Blocker[13]
Beta-1 adrenergic receptor Binder[7]
Beta-2 adrenergic receptor Binder[7]
Beta-3 adrenergic receptor Binder[7]
[24]

[top]Enzymes

Enzyme
Short Name
Action
Action
Cytochrome P450 1A2[25][26][27][28][29][30] CYP1A2 Substrate 
Cytochrome P450 2B6[29][30] CYP2B6 Substrate 
Cytochrome P450 2C8[29][30] CYP2C8 Substrate Inhibitor
Cytochrome P450 2C9[31][26][27][29][30] CYP2C9 Substrate 
Cytochrome P450 2C19[28][26][27][29][30] CYP2C19 Substrate Inhibitor
Cytochrome P450 2D6[32][25][31][26][27][29][30] CYP2D6 Substrate Inhibitor
Cytochrome P450 2E1[29] CYP2E1 Substrate Inhibitor
Cytochrome P450 3A4[25][31][26][29][30] CYP3A4 Substrate 
Cytochrome P450 3A5[25] CYP3A5 Substrate 
[24]

[top]Transporters

Transporter
Action
TBC To Be Continued (WIP)


[top]Chemistry of Amitriptyline

Property
Values
Systematic(IUPAC) name:3-(10,11-dihydro-5H-dibenzo[a,d]cycloheptene-5-ylidene)-N,N-dimethyl-1-propanamine
Synonyms: 5-(3-dimethylaminopropylidene)dibenzo[a,d][1,4]cycloheptadiene, 10,11-dihydro-N,N-dimethyl-5H-dibenzo[a,d]cycloheptene-[Delta]^5,[gamma]-propylamine, 5-([gamma]-dimethylaminopropylidene)-5H-dibenzo[a,d]-10,11-dihydrocycloheptene, 10,11-dihydro-5-([gamma]-dimethylaminopropylidene)-5H-dibenzo[a,d]cycloheptene ; Elavil, Endep, Saroten, Sarotex, Redomex, Adepril, Amineurin, Domical, Euplit, Laroxyl, Lentizol, Miketorin, Triptizol, Tryptanol, Tryptizol (hydrochloride)
Molecular Formula:C20H23N
Molar mass:277.403 g/mol; 313.87 g/mol (hydrochloride)
CAS Registry Number:50-48-6; 549-18-8 (hydrochloride)
Melting Point:196-197℃ (hydrochloride)
Boiling Point: no data
Flash Point: no data
Solubility: Freely soluble in water, chloroform, alcohol (ethanol). Insoluble in ether.
Additionnal data: pKa 9.4
[33]


[top]The Dangers of Amitriptyline

[top]General Warnings

[top]Side Effects and Interactions

[top]Potential Side Effects

[top]Potential Drug Interactions

Note this is not a comprehensive list of potential interactions, but commonly known interactions. You should check with your medical provider for additional information.
AS OF DATE: 22 April 2015

Drug
Effects
AltretamineRisk of severe hypotension
Artemether Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
Atazanavir Atazanavir may increase the effect and toxicity of the tricyclic antidepressant, amitriptyline, by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of amitriptyline if atazanavir if initiated, discontinued or dose changed.
Butabarbital Barbiturates like butabarbital may increase the metabolism of tricyclic antidepressants like amitriptyline. Monitor for decreased therapeutic effects of tricyclic antidepressants if a barbiturate is initiated/dose increased, or increased effects if a barbiturate is discontinued/dose decreased. The tricyclic antidepressant dosage will likely need to be increased during concomitant barbiturate therapy, and reduced upon barbiturate discontinuation.
Butalbital Barbiturates such as butalbital may increase the metabolism of tricyclic antidepressants such as amitriptyline. Monitor for decreased therapeutic effects of tricyclic antidepressants if a barbiturate is initiated/dose increased, or increased effects if a barbiturate is discontinued/dose decreased. The tricyclic antidepressant dosage will likely need to be increased during concomitant barbiturate therapy, and reduced upon barbiturate discontinuation.
Carbamazepine Carbamazepine may decrease the serum concentration of the tricyclic antidepressant, amitriptyline, by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of amitriptyline if carbamazepine is initiated, discontinued or dose changed.
Cimetidine Cimetidine may increase the effect of the tricyclic antidepressant, amitriptyline, by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of amitriptyline if cimetidine is initiated, discontinued or dose changed.
Cisapride Increased risk of cardiotoxicity and arrhythmias
Clonidine The tricyclic antidepressant, amitriptyline, decreases the effect of clonidine.
DesvenlafaxineIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
Dihydroquinidinebarbiturate Dihydroquinidine barbiturate increases the effect of the tricyclic antidepressant, amitriptyline.
Dobutamine The tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect, dobutamine.
Donepezil Possible antagonism of action
DopamineThe tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect, dopamine.
Duloxetine Possible increase in the levels of this agent when used with duloxetine
Ephedra The tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of ephedra.
Ephedrine The tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of ephedrine.
EpinephrineThe tricyclic antidepressant, amitriptyline, may increase the sympathomimetic effect of epinephrine.
Fenoterol The tricyclic antidepressant, amitriptyline, may increase the sympathomimetic effect of fenoterol.
FluconazoleFluconazole may increase the effect and toxicity of the tricyclic antidepressant, amitriptyline, by decreasing its metabolism. Additive QTc-prolonging effects may also occur. Monitor for changes in the therapeutic and adverse effects of amitriptyline if fluconazole is initiated, discontinued or dose changed. Monitor for the development of torsades de pointes during concomitant therapy.
Fluoxetine The SSRI, fluoxetine, may increase the serum concentration of the tricyclic antidepressant, amitriptyline, by decreasing its metabolism. Additive modulation of serotonin activity also increases the risk of serotonin syndrome. Monitor for development of serotonin syndrome during concomitant therapy. Monitor for changes in the therapeutic and adverse effects of amitriptyline if fluoxetine is initiated, discontinued or dose changed.
FluvoxamineThe SSRI, fluvoxamine, may increase the serum concentration of the tricyclic antidepressant, amitriptyline, by decreasing its metabolism. Additive modulation of serotonin activity also increases the risk of serotonin syndrome. Monitor for development of serotonin syndrome during concomitant therapy. Monitor for changes in the therapeutic and adverse effects of amitriptyline if fluvoxamine is initiated, discontinued or dose changed.
GalantaminePossible antagonism of action
Grepafloxacin Increased risk of cardiotoxicity and arrhythmias
Guanethidine The tricyclic antidepressant, amitriptyline, decreases the effect of guanethidine.
IndacaterolConcomitant therapy with monoamine oxidase inhibitors, tricyclic antidepressants, or other drugs that prolong the QTc interval should be monitored closely. These drugs may potentiate the effect of adrenergic agonist on the cardiovascular system.
Iobenguane May diminish the therapeutic effect and increase chances of producing a false negative imaging result of Iobenguane as it inhibits noradrenaline transporter function
Isocarboxazid Possibility of severe adverse effects
Isoprenaline The tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of isoproterenol.
Ketoconazole Ketoconazole, a moderate CYP2D6 inhibitor, may increase the serum concentration of amitriptyline by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of amitriptyline if ketoconazole is initiated, discontinued or dose changed.
Lumefantrine Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
Mephentermine The tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of mephentermine.
Mesoridazine Increased risk of cardiotoxicity and arrhythmias
MetaraminolThe tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of metaraminol.
MethoxamineThe tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of methoxamine.
MoclobemidePossible severe adverse reaction with this combination
NorepinephrineThe tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of norepinephrine.
Orciprenaline The tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of orciprenaline.
Phenelzine Possibility of severe adverse effects
Phenylephrine The tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of phenylephrine.
Phenylpropanolamine The tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of phenylpropanolamine.
Pirbuterol The tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of pirbuterol.
Procaterol The tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of procaterol.
Pseudoephedrine The tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of pseudoephedrine.
Quinidine Additive QTc-prolonging effects may occur. Quinidine may also increase the serum concentration of the tricyclic antidepressant, amitriptyline, by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of amitriptyline if quinidine is initiated, discontinued or dose changed. Monitor for the development of torsades de pointes during concomitant therapy.
Quinidinebarbiturate Quinidine barbiturate increases the effect of tricyclic antidepressant, amitriptyline.
Rasagiline Possibility of severe adverse effects
Rifabutin The rifamycin, rifabutin, may decrease the effect of the tricyclic antidepressant, amitriptyline, by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of amitriptyline if rifabutin is initiated, discontinued or dose changed.
Rifampicin The rifamycin, rifampin, may decrease the effect of the tricyclic antidepressant, amitriptyline, by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of amitriptyline if rifampin is initiated, discontinued or dose changed.
Ritonavir Ritonavir may increase the effect and toxicity of the tricyclic antidepressant, amitriptyline, by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of amitriptyline if ritonavir if initiated, discontinued or dose changed.
Rivastigmine Possible antagonism of action
Salbutamol The tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of salbutamol.
SibutramineIncreased risk of CNS adverse effects
Sparfloxacin Increased risk of cardiotoxicity and arrhythmias
Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Amitriptyline, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.
Tacrolimus Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
TerbinafineTerbinafine may reduce the metabolism and clearance of Amitryptyline. Consider alternate therapy or monitor for therapeutic/adverse effects of Amytriptyline if Terbinafine is initiated, discontinued or dose changed.
TerbutalineThe tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of terbutaline.
TerfenadineIncreased risk of cardiotoxicity and arrhythmias
Thioridazine Increased risk of cardiotoxicity and arrhythmias
ThiothixeneMay cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
Toremifene Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
TramadolTramadol increases the risk of serotonin syndrome and seizures.
Tranylcypromine Increased risk of serotonin syndrome. Concomitant therapy should be avoided. A significant washout period, dependent on the half-lives of the agents, should be employed between therapies.
Trazodone Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
TrimethobenzamideTrimethobenzamide and Amitriptyline, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Trimipramine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome. Additive QTc-prolongation may also occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
Triprolidine Triprolidine and Amitriptyline, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
TrospiumTrospium and Amitriptyline, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
VenlafaxineIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
Vilazodone Monitor for toxic effects of tricyclic antidepressants if a selective serotonin reuptake inhibitor (SSRI) is initiated or the dose is increased. The influence of the SSRI may take several days or weeks to be fully realized or resolved.
Voriconazole Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Vorinostat Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
ZiprasidoneAdditive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
Zolmitriptan Use of two serotonin modulators, such as zolmitriptan and amitriptyline, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
ZuclopenthixolAdditive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
[24]

[top]Potential Food Interactions and Precautions

  • Avoid taking with alcohol.
  • Avoid excessive quantities of coffee or tea (caffeine).
  • Avoid St. John's Wort.
  • Take with food to reduce irritation.
[24]


[top]Producing Amitriptyline



[top]Forms of Amitriptyline



[top]Legal Status of Amitriptyline

[top]United Nations

[top]Austrailia

Available only by prescription, known as Endep.

[top]EU

[top]Norway

Available only by prescription.

[top]USA

Amitriptyline (Elavil) is unscheduled in the United States. Available only by prescription. This means that sales and distribution are allowed only by those with a license and only to those with a prescription (according to FDA regulations). Possession of Amitriptyline is not illegal without prescription.


[top]History of Amitriptyline

[top]Popularity of Amitriptyline over time



[top]More Amitriptyline Sections



[top]The Latest Amitriptyline Threads


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[top]References

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Last edited by Damocles, 23-04-2015 at 10:08
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