Details
Stereochemistry | ACHIRAL |
Molecular Formula | C20H23N |
Molecular Weight | 277.4041 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(C)CCC=C1c2ccccc2CCc3ccccc31
InChI
InChIKey=KRMDCWKBEZIMAB-UHFFFAOYSA-N
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
Molecular Formula | C20H23N |
Molecular Weight | 277.4041 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionCurator's Comment:: description was created based on several sources, including
http://www.rxlist.com/elavil-drug.htm
https://www.ncbi.nlm.nih.gov/pubmed/23235671; https://www.ncbi.nlm.nih.gov/pubmed/11157426; http://www.ncbi.nlm.nih.gov/pubmed/16871467; http://www.ncbi.nlm.nih.gov/pubmed/2578912; http://www.ncbi.nlm.nih.gov/pubmed/?term=15943846
Curator's Comment:: description was created based on several sources, including
http://www.rxlist.com/elavil-drug.htm
https://www.ncbi.nlm.nih.gov/pubmed/23235671; https://www.ncbi.nlm.nih.gov/pubmed/11157426; http://www.ncbi.nlm.nih.gov/pubmed/16871467; http://www.ncbi.nlm.nih.gov/pubmed/2578912; http://www.ncbi.nlm.nih.gov/pubmed/?term=15943846
Amitriptyline is a derivative of dibenzocycloheptadiene and a tricyclic antidepressant (TCA) and is mainly used to treat symptoms of depression. It works on the central nervous system (CNS) by inhibiting the membrane pump mechanism responsible for uptake of norepinephrine and serotonin in adrenergic and serotonergic neurons. Amitriptyline has been frequently used as an active comparator in clinical trials on newer antidepressants. It is rarely used as a first-line antidepressant nowadays due to its high degree of toxicity in overdose and generally poorer tolerability than the newer antidepressants.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P23975 Gene ID: 6530.0 Gene Symbol: SLC6A2 Target Organism: Homo sapiens (Human) Sources: http://www.ncbi.nlm.nih.gov/pubmed/14744476 |
3.45 nM [IC50] | ||
Target ID: P31645 Gene ID: 6532.0 Gene Symbol: SLC6A4 Target Organism: Homo sapiens (Human) Sources: http://www.ncbi.nlm.nih.gov/pubmed/14744476 |
13.3 nM [IC50] | ||
Target ID: P28223 Gene ID: 3356.0 Gene Symbol: HTR2A Target Organism: Homo sapiens (Human) Sources: http://www.ncbi.nlm.nih.gov/pubmed/7855217 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Preventing | AMITRIPTYLINE HYDROCHLORIDE Approved UseFor the relief of symptoms of depression. Endogenous depression is more likely to be alleviated than are other depressive states. Launch Date8.7393599E11 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
15.3 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10383563 |
75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered: |
AMITRIPTYLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
593 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10383563 |
75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered: |
AMITRIPTYLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
20.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10383563 |
75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered: |
AMITRIPTYLINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
7.7% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/6125396 |
150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
AMITRIPTYLINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Doses
Dose | Population | Adverse events |
---|---|---|
100 mg 1 times / day single, intravenous Studied dose Dose: 100 mg, 1 times / day Route: intravenous Route: single Dose: 100 mg, 1 times / day Sources: |
healthy, 21 to 70 years n = 5 Health Status: healthy Age Group: 21 to 70 years Sex: M+F Population Size: 5 Sources: |
Disc. AE: Bradycardia... Other AEs: Agitation, Dry mouth... AEs leading to discontinuation/dose reduction: Bradycardia (grade 3, 20%) Other AEs:Agitation (20%) Sources: Dry mouth (20%) Drowsiness (20%) Language disorder (20%) |
10 % 1 times / day single, topical Highest studied dose Dose: 10 %, 1 times / day Route: topical Route: single Dose: 10 %, 1 times / day Sources: |
unhealthy, 57 years n = 1 Health Status: unhealthy Condition: pain Age Group: 57 years Sex: M Population Size: 1 Sources: |
Other AEs: Thought disorder, Mental concentration difficult... Other AEs: Thought disorder Sources: Mental concentration difficult |
520.3 mg 1 times / day single, oral (mean) Studied dose Dose: 520.3 mg, 1 times / day Route: oral Route: single Dose: 520.3 mg, 1 times / day Sources: |
healthy, mean age 22.1 years n = 96 Health Status: healthy Age Group: mean age 22.1 years Sex: M+F Population Size: 96 Sources: |
Other AEs: Mental status changes... |
25 mg 1 times / day multiple, oral Studied dose Dose: 25 mg, 1 times / day Route: oral Route: multiple Dose: 25 mg, 1 times / day Sources: |
unhealthy, mean age 43.2 years n = 16 Health Status: unhealthy Condition: globus pharyngeus Age Group: mean age 43.2 years Sex: M+F Population Size: 16 Sources: |
Other AEs: Dry mouth, Sleepiness... Other AEs: Dry mouth (75%) Sources: Sleepiness (68.8%) Dizziness (25%) Constipation (18.8%) Palpitations (6.3%) Malaise (6.3%) |
75 mg 1 times / day multiple, oral Recommended Dose: 75 mg, 1 times / day Route: oral Route: multiple Dose: 75 mg, 1 times / day Sources: |
unhealthy, mean age 55 years n = 27 Health Status: unhealthy Condition: chronic pain Age Group: mean age 55 years Sex: M+F Population Size: 27 Sources: |
Disc. AE: Drowsiness, Dry mouth... Other AEs: Drowsiness, Nausea... AEs leading to discontinuation/dose reduction: Drowsiness (10%) Other AEs:Dry mouth (10%) Drowsiness (51.8%) Sources: Nausea (7.4%) Headache (7.4%) Dry mouth (63%) Thirst (7.4%) Tiredness (7.4%) Bad taste (18.5%) Attention concentration difficulty (7.4%) Hyperglycaemia (3.7%) |
59 mg 1 times / day multiple, oral (mean) Studied dose Dose: 59 mg, 1 times / day Route: oral Route: multiple Dose: 59 mg, 1 times / day Sources: |
unhealthy, mean age 60.4 years n = 25 Health Status: unhealthy Condition: diabetic peripheral neuropathy pain Age Group: mean age 60.4 years Sex: M+F Population Size: 25 Sources: |
Disc. AE: Ankle edema, Dizziness... Other AEs: Sedation, Dry mouth... AEs leading to discontinuation/dose reduction: Ankle edema (4%) Other AEs:Dizziness (4%) Sedation (32%) Sources: Dry mouth (32%) Postural hypotension (20%) Weight gain (24%) Ataxia (8%) Constipation (12%) Lethargy (20%) Edema (8%) Headache (12%) Pruritus (12%) Bad taste (4%) Nausea (4%) Diarrhea (4%) Blurred vision (8%) |
520.3 mg 1 times / day single, oral (mean) Studied dose Dose: 520.3 mg, 1 times / day Route: oral Route: single Dose: 520.3 mg, 1 times / day Sources: |
healthy n = 96 |
Other AEs: Tachycardia... |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Agitation | 20% | 100 mg 1 times / day single, intravenous Studied dose Dose: 100 mg, 1 times / day Route: intravenous Route: single Dose: 100 mg, 1 times / day Sources: |
healthy, 21 to 70 years n = 5 Health Status: healthy Age Group: 21 to 70 years Sex: M+F Population Size: 5 Sources: |
Drowsiness | 20% | 100 mg 1 times / day single, intravenous Studied dose Dose: 100 mg, 1 times / day Route: intravenous Route: single Dose: 100 mg, 1 times / day Sources: |
healthy, 21 to 70 years n = 5 Health Status: healthy Age Group: 21 to 70 years Sex: M+F Population Size: 5 Sources: |
Dry mouth | 20% | 100 mg 1 times / day single, intravenous Studied dose Dose: 100 mg, 1 times / day Route: intravenous Route: single Dose: 100 mg, 1 times / day Sources: |
healthy, 21 to 70 years n = 5 Health Status: healthy Age Group: 21 to 70 years Sex: M+F Population Size: 5 Sources: |
Language disorder | 20% | 100 mg 1 times / day single, intravenous Studied dose Dose: 100 mg, 1 times / day Route: intravenous Route: single Dose: 100 mg, 1 times / day Sources: |
healthy, 21 to 70 years n = 5 Health Status: healthy Age Group: 21 to 70 years Sex: M+F Population Size: 5 Sources: |
Bradycardia | grade 3, 20% Disc. AE |
100 mg 1 times / day single, intravenous Studied dose Dose: 100 mg, 1 times / day Route: intravenous Route: single Dose: 100 mg, 1 times / day Sources: |
healthy, 21 to 70 years n = 5 Health Status: healthy Age Group: 21 to 70 years Sex: M+F Population Size: 5 Sources: |
Mental concentration difficult | 10 % 1 times / day single, topical Highest studied dose Dose: 10 %, 1 times / day Route: topical Route: single Dose: 10 %, 1 times / day Sources: |
unhealthy, 57 years n = 1 Health Status: unhealthy Condition: pain Age Group: 57 years Sex: M Population Size: 1 Sources: |
|
Thought disorder | 10 % 1 times / day single, topical Highest studied dose Dose: 10 %, 1 times / day Route: topical Route: single Dose: 10 %, 1 times / day Sources: |
unhealthy, 57 years n = 1 Health Status: unhealthy Condition: pain Age Group: 57 years Sex: M Population Size: 1 Sources: |
|
Mental status changes | 520.3 mg 1 times / day single, oral (mean) Studied dose Dose: 520.3 mg, 1 times / day Route: oral Route: single Dose: 520.3 mg, 1 times / day Sources: |
healthy, mean age 22.1 years n = 96 Health Status: healthy Age Group: mean age 22.1 years Sex: M+F Population Size: 96 Sources: |
|
Constipation | 18.8% | 25 mg 1 times / day multiple, oral Studied dose Dose: 25 mg, 1 times / day Route: oral Route: multiple Dose: 25 mg, 1 times / day Sources: |
unhealthy, mean age 43.2 years n = 16 Health Status: unhealthy Condition: globus pharyngeus Age Group: mean age 43.2 years Sex: M+F Population Size: 16 Sources: |
Dizziness | 25% | 25 mg 1 times / day multiple, oral Studied dose Dose: 25 mg, 1 times / day Route: oral Route: multiple Dose: 25 mg, 1 times / day Sources: |
unhealthy, mean age 43.2 years n = 16 Health Status: unhealthy Condition: globus pharyngeus Age Group: mean age 43.2 years Sex: M+F Population Size: 16 Sources: |
Malaise | 6.3% | 25 mg 1 times / day multiple, oral Studied dose Dose: 25 mg, 1 times / day Route: oral Route: multiple Dose: 25 mg, 1 times / day Sources: |
unhealthy, mean age 43.2 years n = 16 Health Status: unhealthy Condition: globus pharyngeus Age Group: mean age 43.2 years Sex: M+F Population Size: 16 Sources: |
Palpitations | 6.3% | 25 mg 1 times / day multiple, oral Studied dose Dose: 25 mg, 1 times / day Route: oral Route: multiple Dose: 25 mg, 1 times / day Sources: |
unhealthy, mean age 43.2 years n = 16 Health Status: unhealthy Condition: globus pharyngeus Age Group: mean age 43.2 years Sex: M+F Population Size: 16 Sources: |
Sleepiness | 68.8% | 25 mg 1 times / day multiple, oral Studied dose Dose: 25 mg, 1 times / day Route: oral Route: multiple Dose: 25 mg, 1 times / day Sources: |
unhealthy, mean age 43.2 years n = 16 Health Status: unhealthy Condition: globus pharyngeus Age Group: mean age 43.2 years Sex: M+F Population Size: 16 Sources: |
Dry mouth | 75% | 25 mg 1 times / day multiple, oral Studied dose Dose: 25 mg, 1 times / day Route: oral Route: multiple Dose: 25 mg, 1 times / day Sources: |
unhealthy, mean age 43.2 years n = 16 Health Status: unhealthy Condition: globus pharyngeus Age Group: mean age 43.2 years Sex: M+F Population Size: 16 Sources: |
Drowsiness | 10% Disc. AE |
75 mg 1 times / day multiple, oral Recommended Dose: 75 mg, 1 times / day Route: oral Route: multiple Dose: 75 mg, 1 times / day Sources: |
unhealthy, mean age 55 years n = 27 Health Status: unhealthy Condition: chronic pain Age Group: mean age 55 years Sex: M+F Population Size: 27 Sources: |
Dry mouth | 10% Disc. AE |
75 mg 1 times / day multiple, oral Recommended Dose: 75 mg, 1 times / day Route: oral Route: multiple Dose: 75 mg, 1 times / day Sources: |
unhealthy, mean age 55 years n = 27 Health Status: unhealthy Condition: chronic pain Age Group: mean age 55 years Sex: M+F Population Size: 27 Sources: |
Bad taste | 18.5% | 75 mg 1 times / day multiple, oral Recommended Dose: 75 mg, 1 times / day Route: oral Route: multiple Dose: 75 mg, 1 times / day Sources: |
unhealthy, mean age 55 years n = 27 Health Status: unhealthy Condition: chronic pain Age Group: mean age 55 years Sex: M+F Population Size: 27 Sources: |
Hyperglycaemia | 3.7% | 75 mg 1 times / day multiple, oral Recommended Dose: 75 mg, 1 times / day Route: oral Route: multiple Dose: 75 mg, 1 times / day Sources: |
unhealthy, mean age 55 years n = 27 Health Status: unhealthy Condition: chronic pain Age Group: mean age 55 years Sex: M+F Population Size: 27 Sources: |
Drowsiness | 51.8% | 75 mg 1 times / day multiple, oral Recommended Dose: 75 mg, 1 times / day Route: oral Route: multiple Dose: 75 mg, 1 times / day Sources: |
unhealthy, mean age 55 years n = 27 Health Status: unhealthy Condition: chronic pain Age Group: mean age 55 years Sex: M+F Population Size: 27 Sources: |
Dry mouth | 63% | 75 mg 1 times / day multiple, oral Recommended Dose: 75 mg, 1 times / day Route: oral Route: multiple Dose: 75 mg, 1 times / day Sources: |
unhealthy, mean age 55 years n = 27 Health Status: unhealthy Condition: chronic pain Age Group: mean age 55 years Sex: M+F Population Size: 27 Sources: |
Attention concentration difficulty | 7.4% | 75 mg 1 times / day multiple, oral Recommended Dose: 75 mg, 1 times / day Route: oral Route: multiple Dose: 75 mg, 1 times / day Sources: |
unhealthy, mean age 55 years n = 27 Health Status: unhealthy Condition: chronic pain Age Group: mean age 55 years Sex: M+F Population Size: 27 Sources: |
Headache | 7.4% | 75 mg 1 times / day multiple, oral Recommended Dose: 75 mg, 1 times / day Route: oral Route: multiple Dose: 75 mg, 1 times / day Sources: |
unhealthy, mean age 55 years n = 27 Health Status: unhealthy Condition: chronic pain Age Group: mean age 55 years Sex: M+F Population Size: 27 Sources: |
Nausea | 7.4% | 75 mg 1 times / day multiple, oral Recommended Dose: 75 mg, 1 times / day Route: oral Route: multiple Dose: 75 mg, 1 times / day Sources: |
unhealthy, mean age 55 years n = 27 Health Status: unhealthy Condition: chronic pain Age Group: mean age 55 years Sex: M+F Population Size: 27 Sources: |
Thirst | 7.4% | 75 mg 1 times / day multiple, oral Recommended Dose: 75 mg, 1 times / day Route: oral Route: multiple Dose: 75 mg, 1 times / day Sources: |
unhealthy, mean age 55 years n = 27 Health Status: unhealthy Condition: chronic pain Age Group: mean age 55 years Sex: M+F Population Size: 27 Sources: |
Tiredness | 7.4% | 75 mg 1 times / day multiple, oral Recommended Dose: 75 mg, 1 times / day Route: oral Route: multiple Dose: 75 mg, 1 times / day Sources: |
unhealthy, mean age 55 years n = 27 Health Status: unhealthy Condition: chronic pain Age Group: mean age 55 years Sex: M+F Population Size: 27 Sources: |
Constipation | 12% | 59 mg 1 times / day multiple, oral (mean) Studied dose Dose: 59 mg, 1 times / day Route: oral Route: multiple Dose: 59 mg, 1 times / day Sources: |
unhealthy, mean age 60.4 years n = 25 Health Status: unhealthy Condition: diabetic peripheral neuropathy pain Age Group: mean age 60.4 years Sex: M+F Population Size: 25 Sources: |
Headache | 12% | 59 mg 1 times / day multiple, oral (mean) Studied dose Dose: 59 mg, 1 times / day Route: oral Route: multiple Dose: 59 mg, 1 times / day Sources: |
unhealthy, mean age 60.4 years n = 25 Health Status: unhealthy Condition: diabetic peripheral neuropathy pain Age Group: mean age 60.4 years Sex: M+F Population Size: 25 Sources: |
Pruritus | 12% | 59 mg 1 times / day multiple, oral (mean) Studied dose Dose: 59 mg, 1 times / day Route: oral Route: multiple Dose: 59 mg, 1 times / day Sources: |
unhealthy, mean age 60.4 years n = 25 Health Status: unhealthy Condition: diabetic peripheral neuropathy pain Age Group: mean age 60.4 years Sex: M+F Population Size: 25 Sources: |
Lethargy | 20% | 59 mg 1 times / day multiple, oral (mean) Studied dose Dose: 59 mg, 1 times / day Route: oral Route: multiple Dose: 59 mg, 1 times / day Sources: |
unhealthy, mean age 60.4 years n = 25 Health Status: unhealthy Condition: diabetic peripheral neuropathy pain Age Group: mean age 60.4 years Sex: M+F Population Size: 25 Sources: |
Postural hypotension | 20% | 59 mg 1 times / day multiple, oral (mean) Studied dose Dose: 59 mg, 1 times / day Route: oral Route: multiple Dose: 59 mg, 1 times / day Sources: |
unhealthy, mean age 60.4 years n = 25 Health Status: unhealthy Condition: diabetic peripheral neuropathy pain Age Group: mean age 60.4 years Sex: M+F Population Size: 25 Sources: |
Weight gain | 24% | 59 mg 1 times / day multiple, oral (mean) Studied dose Dose: 59 mg, 1 times / day Route: oral Route: multiple Dose: 59 mg, 1 times / day Sources: |
unhealthy, mean age 60.4 years n = 25 Health Status: unhealthy Condition: diabetic peripheral neuropathy pain Age Group: mean age 60.4 years Sex: M+F Population Size: 25 Sources: |
Dry mouth | 32% | 59 mg 1 times / day multiple, oral (mean) Studied dose Dose: 59 mg, 1 times / day Route: oral Route: multiple Dose: 59 mg, 1 times / day Sources: |
unhealthy, mean age 60.4 years n = 25 Health Status: unhealthy Condition: diabetic peripheral neuropathy pain Age Group: mean age 60.4 years Sex: M+F Population Size: 25 Sources: |
Sedation | 32% | 59 mg 1 times / day multiple, oral (mean) Studied dose Dose: 59 mg, 1 times / day Route: oral Route: multiple Dose: 59 mg, 1 times / day Sources: |
unhealthy, mean age 60.4 years n = 25 Health Status: unhealthy Condition: diabetic peripheral neuropathy pain Age Group: mean age 60.4 years Sex: M+F Population Size: 25 Sources: |
Bad taste | 4% | 59 mg 1 times / day multiple, oral (mean) Studied dose Dose: 59 mg, 1 times / day Route: oral Route: multiple Dose: 59 mg, 1 times / day Sources: |
unhealthy, mean age 60.4 years n = 25 Health Status: unhealthy Condition: diabetic peripheral neuropathy pain Age Group: mean age 60.4 years Sex: M+F Population Size: 25 Sources: |
Diarrhea | 4% | 59 mg 1 times / day multiple, oral (mean) Studied dose Dose: 59 mg, 1 times / day Route: oral Route: multiple Dose: 59 mg, 1 times / day Sources: |
unhealthy, mean age 60.4 years n = 25 Health Status: unhealthy Condition: diabetic peripheral neuropathy pain Age Group: mean age 60.4 years Sex: M+F Population Size: 25 Sources: |
Nausea | 4% | 59 mg 1 times / day multiple, oral (mean) Studied dose Dose: 59 mg, 1 times / day Route: oral Route: multiple Dose: 59 mg, 1 times / day Sources: |
unhealthy, mean age 60.4 years n = 25 Health Status: unhealthy Condition: diabetic peripheral neuropathy pain Age Group: mean age 60.4 years Sex: M+F Population Size: 25 Sources: |
Ankle edema | 4% Disc. AE |
59 mg 1 times / day multiple, oral (mean) Studied dose Dose: 59 mg, 1 times / day Route: oral Route: multiple Dose: 59 mg, 1 times / day Sources: |
unhealthy, mean age 60.4 years n = 25 Health Status: unhealthy Condition: diabetic peripheral neuropathy pain Age Group: mean age 60.4 years Sex: M+F Population Size: 25 Sources: |
Dizziness | 4% Disc. AE |
59 mg 1 times / day multiple, oral (mean) Studied dose Dose: 59 mg, 1 times / day Route: oral Route: multiple Dose: 59 mg, 1 times / day Sources: |
unhealthy, mean age 60.4 years n = 25 Health Status: unhealthy Condition: diabetic peripheral neuropathy pain Age Group: mean age 60.4 years Sex: M+F Population Size: 25 Sources: |
Ataxia | 8% | 59 mg 1 times / day multiple, oral (mean) Studied dose Dose: 59 mg, 1 times / day Route: oral Route: multiple Dose: 59 mg, 1 times / day Sources: |
unhealthy, mean age 60.4 years n = 25 Health Status: unhealthy Condition: diabetic peripheral neuropathy pain Age Group: mean age 60.4 years Sex: M+F Population Size: 25 Sources: |
Blurred vision | 8% | 59 mg 1 times / day multiple, oral (mean) Studied dose Dose: 59 mg, 1 times / day Route: oral Route: multiple Dose: 59 mg, 1 times / day Sources: |
unhealthy, mean age 60.4 years n = 25 Health Status: unhealthy Condition: diabetic peripheral neuropathy pain Age Group: mean age 60.4 years Sex: M+F Population Size: 25 Sources: |
Edema | 8% | 59 mg 1 times / day multiple, oral (mean) Studied dose Dose: 59 mg, 1 times / day Route: oral Route: multiple Dose: 59 mg, 1 times / day Sources: |
unhealthy, mean age 60.4 years n = 25 Health Status: unhealthy Condition: diabetic peripheral neuropathy pain Age Group: mean age 60.4 years Sex: M+F Population Size: 25 Sources: |
Tachycardia | 520.3 mg 1 times / day single, oral (mean) Studied dose Dose: 520.3 mg, 1 times / day Route: oral Route: single Dose: 520.3 mg, 1 times / day Sources: |
healthy n = 96 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
yes [IC50 14 uM] | ||||
yes [IC50 6.99 uM] | ||||
yes [IC50 8.8 uM] | ||||
yes [Inhibition 200 uM] | ||||
yes [Ki 31 uM] | ||||
yes [Ki 37.7 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
yes | ||||
yes | ||||
yes | ||||
yes | ||||
yes | ||||
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
[Cardiac arrest following amitriptylin and adrenaline]. | 1975 Jun 16 |
|
Fatal cholestatic jaundice associated with amitriptyline. | 2000 Jul-Aug |
|
Near fatal case of atrio-ventricular block induced by amitriptyline at therapeutic dose. | 2000 Sep |
|
Smoking in patients receiving psychotropic medications: a pharmacokinetic perspective. | 2001 |
|
Gender differences in depression associated with neurologic illness: clinical correlates and pharmacologic response. | 2001 |
|
Tianeptine: a review of its use in depressive disorders. | 2001 |
|
Long-term effects of tricyclic antidepressants on norepinephrine kinetics in humans. | 2001 |
|
The concentration of three anti-seizure medications in hair: the effects of hair color, controlling for dose and age. | 2001 |
|
Hyposecretion of the adrenal androgen dehydroepiandrosterone sulfate and its relation to clinical variables in inflammatory arthritis. | 2001 |
|
Involvement of potassium channels in amitriptyline and clomipramine analgesia. | 2001 |
|
Evidence for the use of gabapentin in the treatment of diabetic peripheral neuropathy. | 2001 Apr |
|
The effects of amitriptyline, citalopram and reboxetine on autonomic nervous system. A randomised placebo-controlled study on healthy volunteers. | 2001 Apr |
|
Noradrenergic dysfunction and antidepressant treatment response. | 2001 Apr |
|
Antidepressive treatment with amitriptyline and paroxetine: comparable effects on heart rate variability. | 2001 Apr |
|
Application of the relative activity factor approach in scaling from heterologously expressed cytochromes p450 to human liver microsomes: studies on amitriptyline as a model substrate. | 2001 Apr |
|
[Sensory neuropathy in HIV infection: pathogenesis and therapy]. | 2001 Apr 14 |
|
Controlling phantom limb pain in Sierra Leone. | 2001 Apr 21 |
|
Postherpetic neuralgia. Treatment with amitriptyline is cheaper than with aciclovir. | 2001 Apr 7 |
|
Review of pharmacokinetic and pharmacodynamic interaction studies with citalopram. | 2001 Aug |
|
Combined pharmacotherapy for nocturnal enuresis. | 2001 Aug |
|
Interaction of psychotropic drugs with monoamine oxidase in rat brain. | 2001 Aug |
|
Adherence to treatment regimen in depressed patients treated with amitriptyline or fluoxetine. | 2001 Aug |
|
Preventive therapy in pediatric migraine. | 2001 Feb |
|
Antidepressant treatment and global tests of coagulation and fibrinolysis. | 2001 Feb |
|
Amitriptyline: still efficacious, but at what cost? | 2001 Feb |
|
Salmon calcitonin potentiates the analgesia induced by antidepressants. | 2001 Jan |
|
Mirtazepine: heir apparent to amitriptyline? | 2001 Jan-Feb |
|
Isolated sural neuropathy presenting as lateral ankle pain. | 2001 Jul |
|
Cyclobenzaprine and back pain: a meta-analysis. | 2001 Jul 9 |
|
Efficacy of amitriptyline as a pharmacological adjunct to behavioral modification in the management of aggressive behaviors in dogs. | 2001 Jul-Aug |
|
The effect of amitriptyline on pain intensity and perception of stress in bruxers. | 2001 Jun |
|
Acute eosinophilic pneumonia associated with amitriptyline in a hemodialysis patient. | 2001 Jun |
|
Retro-orbital tumour--an uncommon cause of headache in pregnancy. | 2001 Jun |
|
Involvement of adenosine in the effect of antidepressants on glutamate and aspartate release in the rat prefrontal cortex. | 2001 Jun |
|
Pharmacological modulation of SK3 channels. | 2001 Jun |
|
Corticotropin-releasing hormone perturbations in interstitial cystitis patients: evidence for abnormal sympathetic activity. | 2001 Jun |
|
Ring flexibility within tricyclic antidepressant drugs. | 2001 Jun |
|
In vitro reaction of formaldehyde with fenfluramine: conversion to N-methyl fenfluramine. | 2001 Mar |
|
Cyclobenzaprine hydrochloride is a commonly prescribed centrally acting muscle relaxant, which is structurally similar to tricyclic antidepressants (TCAs) and differs from amitriptyline by only one double bond. | 2001 Mar |
|
Discovery of a novel member of the histamine receptor family. | 2001 Mar |
|
Effects of amitriptyline on diurnal variations of oxidation-reduction enzyme activities in rat lymphocytes during experimental desynchronosis. | 2001 May |
|
Antidepressant drugs in dermatology. | 2001 May |
|
Treatment of neuropathic pain with venlafaxine. | 2001 May |
|
Advances in the management of neuropathic pain. | 2001 May |
|
High-performance liquid chromatographic method combining radiochemical and ultraviolet detection for determination of low activities of uridine 5'-diphosphate-glucuronosyltransferase. | 2001 May 15 |
|
Inverse agonist actions of typical and atypical antipsychotic drugs at the human 5-hydroxytryptamine(2C) receptor. | 2001 Oct |
|
Efficacy of spinal manipulation for chronic headache: a systematic review. | 2001 Sep |
|
Drug use and five-year incidence of age-related cataracts: The Beaver Dam Eye Study. | 2001 Sep |
|
HPLC of basic drugs on microparticulate strong cation-exchange materials - a review. | 2001 Sep 15 |
|
Antidepressants as risk factor for ischaemic heart disease: case-control study in primary care. | 2001 Sep 22 |
Sample Use Guides
For outpatients, 75 mg of amitriptyline HCl a day in divided doses. If necessary, this may be increased to a total of 150 mg per day. An alternate method of initiating therapy in outpatients is to begin with 50 to 100 mg amitriptyline HCl at bedtime. This may be increased by 25 or 50 mg as necessary in the bedtime dose to a total of 150 mg per day. Hospitalized patients may require 100 mg a day initially. This can be increased gradually to 200 mg a day if necessary up to 300 mg a day. Not recommended for patients under 12 years of age
Route of Administration:
Oral
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/26504754
Amitriptyline was used at 40 uM in isolated rat hepatocytes for 60,120,180 min.
Substance Class |
Chemical
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1806D8D52K
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WHO-ATC |
N06CA01
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WHO-ESSENTIAL MEDICINES LIST |
24.2.1
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FDA ORPHAN DRUG |
288809
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WHO-VATC |
QN06AA09
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LIVERTOX |
44
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NDF-RT |
N0000175752
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FDA ORPHAN DRUG |
739620
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WHO-ESSENTIAL MEDICINES LIST |
8.4
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NCI_THESAURUS |
C94727
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WHO-VATC |
QN06CA01
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WHO-ATC |
N06AA09
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D000639
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Amitriptyline
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AMITRIPTYLINE
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3007
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2160
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200
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50-48-6
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SUB05462MIG
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M1753
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C62005
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704
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CHEMBL629
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1806D8D52K
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50-48-6
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DB00321
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180
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200-041-6
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Related Record | Type | Details | ||
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METABOLIC ENZYME -> SUBSTRATE |
Metabolizing reaction by CYP2D6: N-demethylation
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BINDER->LIGAND |
BINDING
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TARGET -> INHIBITOR | |||
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TRANSPORTER -> INHIBITOR | |||
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METABOLIC ENZYME -> SUBSTRATE | |||
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SALT/SOLVATE -> PARENT | |||
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SALT/SOLVATE -> PARENT | |||
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METABOLIC ENZYME -> INHIBITOR |
IC50
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BINDING PROTEIN->LIGAND |
Amitriptyline displayed an approximately 2:1 [drug:AGP] binding stoichiometry; DETERMINED BY ITC
BINDING
Kd
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TARGET -> INHIBITOR | |||
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TARGET -> INHIBITOR | |||
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TRANSPORTER -> SUBSTRATE | |||
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TRANSPORTER -> INHIBITOR | |||
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METABOLIC ENZYME -> SUBSTRATE |
Related Record | Type | Details | ||
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METABOLITE -> PARENT |
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METABOLITE -> PARENT |
URINE
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METABOLITE ACTIVE -> PARENT |
MAJOR
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METABOLITE -> PARENT | |||
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METABOLITE -> PARENT |
URINE
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Related Record | Type | Details | ||
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PARENT -> IMPURITY |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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PARENT -> IMPURITY |
UNSPECIFIED
EP
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Volume of Distribution | PHARMACOKINETIC |
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Volume of Distribution | PHARMACOKINETIC |
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MAXIMUM TOLERATED DOSE | TOXICITY |
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DEPRESSION, INPATIENTS: 300 MG/DAY |
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Route of Elimination | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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