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| Name | Amitriptyline | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Accession Number | DB00321 (APRD00227) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Type | small molecule | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Groups | approved | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Description | Amitriptyline hydrochloride is a dibenzocycloheptene-derivative tricyclic antidepressant (TCA). TCAs are structurally similar to phenothiazines. They contain a tricyclic ring system with an alkyl amine substituent on the central ring. In non-depressed individuals, amitriptyline does not affect mood or arousal, but may cause sedation. In depressed individuals, amitriptyline exerts a positive effect on mood. TCAs are potent inhibitors of serotonin and norepinephrine reuptake. Tertiary amine TCAs, such as amitriptyline, are more potent inhibitors of serotonin reuptake than secondary amine TCAs, such as nortriptyline. TCAs also down-regulate cerebral cortical β-adrenergic receptors and sensitize post-synaptic serotonergic receptors with chronic use. The antidepressant effects of TCAs are thought to be due to an overall increase in serotonergic neurotransmission. TCAs also block histamine-H1 receptors, α1-adrenergic receptors and muscarinic receptors, which accounts for their sedative, hypotensive and anticholinergic effects (e.g. blurred vision, dry mouth, constipation, urinary retention), respectively. See toxicity section below for a complete listing of side effects. Amitriptyline may be used to treat depression, chronic pain (unlabeled use), irritable bowel syndrome (unlabeled use), diabetic neuropathy (unlabeled use), post-traumatic stress disorder (unlabeled use), and for migraine prophylaxis (unlabeled use). |
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| Structure |
Download: MOL | SDF | SMILES | InChI Display: 2D Structure | 3D Structure |
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| CAS number | 50-48-6 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Weight |
Average: 277.4033 Monoisotopic: 277.183049741 |
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| Chemical Formula | C20H23N | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
| InChI Key | InChIKey=KRMDCWKBEZIMAB-UHFFFAOYSA-N | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
| InChI |
InChI=1S/C20H23N/c1-21(2)15-7-12-20-18-10-5-3-8-16(18)13-14-17-9-4-6-11-19(17)20/h3-6,8-12H,7,13-15H2,1-2H3
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| IUPAC Name |
dimethyl(3-{tricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-ylidene}propyl)amine
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| SMILES |
CN(C)CCC=C1C2=C(CCC3=C1C=CC=C3)C=CC=C2
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| Mass Spec | show (7.5 KB) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Taxonomy | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Kingdom | Organic | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Pharmacology | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Indication | For the treatment of depression, chronic pain, irritable bowel syndrome, sleep disorders, diabetic neuropathy, agitation and insomnia, and migraine prophylaxis. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Pharmacodynamics | Amitriptyline, a tertiary amine tricyclic antidepressant, is structurally related to both the skeletal muscle relaxant cyclobenzaprine and the thioxanthene antipsychotics such as thiothixene. It is extremely sedating, and thus improvement of sleep patterns can be the first benefit of treatment. Amitriptyline exhibits strong anticholinergic activity, cardiovascular effects including orthostatic hypotension, changes in heart rhythm and conduction, and a lowering of the seizure threshold. As with other antidepressants, several weeks of therapy may be required in order to realize the full clinical benefit of amitriptyline. Although not a labelled indication, amitriptyline is widely used in the management of chronic nonmalignant pain (e.g., post-herpetic neuralgia, fibromyalgia). | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Mechanism of action | Amitriptyline is metabolized to nortriptyline which inhibits the reuptake of norepinephrine and serotonin almost equally. Amitriptyline inhibits the membrane pump mechanism responsible for uptake of norepinephrine and serotonin in adrenergic and serotonergic neurons. Pharmacologically this action may potentiate or prolong neuronal activity since reuptake of these biogenic amines is important physiologically in terminating transmitting activity. This interference with the reuptake of norepinephrine and/or serotonin is believed by some to underlie the antidepressant activity of amitriptyline. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Absorption | Rapidly and well absorbed following oral administration (bioavailability is 30-60% due to first pass metabolism). Peak plasma concentrations occur 2-12 hours following oral or intramuscular administration. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Volume of distribution | Not Available | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Protein binding | Very highly protein bound (90% or more) in plasma and tissues | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Metabolism |
Exclusively hepatic, with first pass effect. Amitriptyline is demethylated in the liver to its primary active metabolite, nortriptyline.
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| Route of elimination | Virtually the entire dose is excreted as glucuronide or sulfate conjugate of metabolites, with little unchanged drug appearing in the urine. 25-50% of a single orally administered dose is excreted in urine as inactive metabolites within 24 hours. Small amounts are excreted in feces via biliary elimination. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Half life | 10 to 50 hours, with an average of 15 hours | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Clearance | Not Available | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Toxicity | LD50=350 mg/kg (in mice). Symptoms of overdose include abnormally low blood pressure, confusion, convulsions, dilated pupils and other eye problems, disturbed concentration, drowsiness, hallucinations, impaired heart function, rapid or irregular heartbeat, reduced body temperature, stupor, and unresponsiveness or coma. Side effects include: sedation, hypotension, blurred vision, dry mouth, constipation, urinary retention, postural hypotension, tachycardia, hypertension, ECG changes, heart failure, impaired memory and delirium, and precipitation of hypomanic or manic episodes in bipolar depression. Withdrawal symptoms include gastrointestinal disturbances, anxiety, and insomnia. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Pathways | Not Available | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Patents | Not Available | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Properties | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| State | solid | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Melting point | 196-197 oC | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Synthesis Reference | Not Available | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
| General Reference |
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| PDB Entries | Not Available | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
| FDA label | Not Available | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
| MSDS | show (73.6 KB) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Drug Interactions | Not Available | |||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Targets |
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1. Sodium-dependent noradrenaline transporter Pharmacological action: yesActions: inhibitor Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals Organism class: humanUniProt ID: P23975  Gene: SLC6A2 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
2. Sodium-dependent serotonin transporter Pharmacological action: yesActions: inhibitor Terminates the action of serotonine by its high affinity sodium-dependent reuptake into presynaptic terminals Organism class: humanUniProt ID: P31645 Gene: SLC6A4 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
3. 5-hydroxytryptamine 2A receptor Pharmacological action: yesActions: antagonist This is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. This receptor is involved in tracheal smooth muscle contraction, bronchoconstriction, and control of aldosterone production Organism class: humanUniProt ID: P28223 Gene: HTR2A Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
4. 5-hydroxytryptamine 1A receptor Pharmacological action: unknownActions: unknown This is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that inhibit adenylate cyclase activity Organism class: humanUniProt ID: P08908 Gene: HTR1A Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
Pharmacological action: unknown
Actions: agonist Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Highly stereoselective. receptor for enkephalins Organism class: humanUniProt ID: P41143 Gene: OPRD1 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
Pharmacological action: unknown
Actions: agonist Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Receptor for dynorphins. May play a role in arousal and regulation of autonomic and neuroendocrine functions Organism class: humanUniProt ID: P41145 Gene: OPRK1 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
7. High affinity nerve growth factor receptor Pharmacological action: unknownActions: agonist Required for high-affinity binding to nerve growth factor (NGF), neurotrophin-3 and neurotrophin-4/5 but not brain- derived neurotrophic factor (BDNF). Known substrates for the Trk receptors are SHC1, PI 3-kinase, and PLC-gamma-1. Has a crucial role in the development and function of the nociceptive reception system as well as establishment of thermal regulation via sweating. Activates ERK1 by either SHC1- or PLC-gamma-1-dependent signaling pathway Organism class: humanUniProt ID: P04629 Gene: NTRK1 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
8. BDNF/NT-3 growth factors receptor Pharmacological action: unknownActions: agonist Receptor for brain-derived neurotrophic factor (BDNF), neurotrophin-3 and neurotrophin-4/5 but not nerve growth factor (NGF). Involved in the development and/or maintenance of the nervous system. This is a tyrosine-protein kinase receptor. Known substrates for the TRK receptors are SHC1, PI-3 kinase, and PLC- gamma-1 Organism class: humanUniProt ID: Q16620 Gene: NTRK2 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
9. Alpha-1A adrenergic receptor Pharmacological action: noActions: antagonist This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins Organism class: humanUniProt ID: P35348 Gene: ADRA1A Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
10. Alpha-1D adrenergic receptor Pharmacological action: noActions: antagonist This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium Organism class: humanUniProt ID: P25100 Gene: ADRA1D Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
11. Alpha-2A adrenergic receptor Pharmacological action: noActions: antagonist Alpha-2 adrenergic receptors mediate the catecholamine- induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianserine > chlorpromazine = spiperone = prazosin > propanolol > alprenolol = pindolol Organism class: humanUniProt ID: P08913 Gene: ADRA2A Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
Pharmacological action: no
Actions: antagonist In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system Organism class: humanUniProt ID: P35367 Gene: HRH1 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
13. Muscarinic acetylcholine receptor M1 Pharmacological action: noActions: antagonist The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover Organism class: humanUniProt ID: P11229 Gene: CHRM1 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
14. Muscarinic acetylcholine receptor M2 Pharmacological action: noActions: antagonist The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is adenylate cyclase inhibition Organism class: humanUniProt ID: P08172 Gene: CHRM2 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
15. Muscarinic acetylcholine receptor M3 Pharmacological action: noActions: antagonist The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover Organism class: humanUniProt ID: P20309 Gene: CHRM3 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
16. Muscarinic acetylcholine receptor M4 Pharmacological action: noActions: antagonist The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is inhibition of adenylate cyclase Organism class: humanUniProt ID: P08173 Gene: CHRM4 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
17. Muscarinic acetylcholine receptor M5 Pharmacological action: noActions: antagonist The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover Organism class: humanUniProt ID: P08912 Gene: CHRM5 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
18. Potassium voltage-gated channel subfamily KQT member 2 Pharmacological action: noActions: inhibitor Probably important in the regulation of neuronal excitability. Associates with KCNQ3 to form a potassium channel with essentially identical properties to the channel underlying the native M-current, a slowly activating and deactivating potassium conductance which plays a critical role in determining the subthreshold electrical excitability of neurons as well as the responsiveness to synaptic inputs. KCNQ2/KCNQ3 current is blocked by linopirdine and XE991, and activated by the anticonvulsant retigabine. Muscarinic agonist oxotremorine-M strongly suppress KCNQ2/KCNQ3 current in cells in which cloned KCNQ2/KCNQ3 channels were coexpressed with M1 muscarinic receptors Organism class: humanUniProt ID: O43526 Gene: KCNQ2 Protein Sequence: FASTA SNPs: SNPJam Report References:
19. Potassium voltage-gated channel subfamily A member 1 Pharmacological action: noActions: inhibitor Mediates the voltage-dependent potassium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a potassium-selective channel through which potassium ions may pass in accordance with their electrochemical gradient Organism class: humanUniProt ID: Q09470 Gene: KCNA1 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
20. Potassium voltage-gated channel subfamily D member 2 Pharmacological action: noActions: inhibitor Pore-forming (alpha) subunit of voltage-gated rapidly inactivating A-type potassium channels. May contribute to I(To) current in heart and I(Sa) current in neurons. Channel properties are modulated by interactions with other alpha subunits and with regulatory subunits Organism class: humanUniProt ID: Q9NZV8 Gene: KCND2 Protein Sequence: FASTA SNPs: SNPJam Report References:
21. Potassium voltage-gated channel subfamily D member 3 Pharmacological action: noActions: inhibitor Pore-forming (alpha) subunit of voltage-gated rapidly inactivating A-type potassium channels. May contribute to I(To) current in heart and I(Sa) current in neurons. Channel properties are modulated by interactions with other alpha subunits and with regulatory subunits Organism class: humanUniProt ID: Q9UK17 Gene: KCND3 Protein Sequence: FASTA SNPs: SNPJam Report References:
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| Enzymes |
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Actions: substrate, inhibitor
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants UniProt ID: P10635Gene: CYP2D6 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
Actions: substrate
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N3-demethylation. Also acts in the metabolism of aflatoxin B1 and acetaminophen UniProt ID: P05177Gene: CYP1A2 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
Actions: substrate, inhibitor
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine UniProt ID: P33261Gene: CYP2C19 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
Actions: substrate
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S- warfarin, diclofenac, phenytoin, tolbutamide and losartan UniProt ID: P11712Gene: CYP2C9 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
Actions: substrate
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4- hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. The enzyme also hydroxylates etoposide UniProt ID: P08684Gene: CYP3A4 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
Actions: substrate
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics UniProt ID: P20815Gene: CYP3A5 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
Actions: substrate
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics UniProt ID: P20813Gene: CYP2B6 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
Actions: substrate, inhibitor
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme responsible for the metabolism the anti- cancer drug paclitaxel (taxol) UniProt ID: P10632Gene: CYP2C8 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
Actions: substrate, inhibitor
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic or carcinogenic forms UniProt ID: P05181Gene: CYP2E1 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
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1. Multidrug resistance protein 1 Actions: substrate, inhibitorEnergy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells UniProt ID: P08183Gene: ABCB1 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
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Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood UniProt ID: P02768Gene: ALB Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
2. Alpha-1-acid glycoprotein 1 Appears to function in modulating the activity of the immune system during the acute-phase reaction UniProt ID: P02763Gene: ORM1 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:
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This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.