Details
Stereochemistry | ACHIRAL |
Molecular Formula | C20H23N |
Molecular Weight | 277.4033 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CN(C)CCC=C1C2=C(CCC3=C1C=CC=C3)C=CC=C2
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 | 277.4033 |
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 |
|
Penetration of amitriptyline, but not of fluoxetine, into brain is enhanced in mice with blood-brain barrier deficiency due to mdr1a P-glycoprotein gene disruption. | 2000 Apr |
|
Antidepressants upregulate messenger RNA levels of the neuroprotective enzyme superoxide dismutase (SOD1). | 2000 Jan |
|
Block of rat brain recombinant SK channels by tricyclic antidepressants and related compounds. | 2000 Jul 28 |
|
Prolonged QT interval and torsades de pointes caused by the combination of fluconazole and amitriptyline. | 2000 Mar |
|
Potent synergism of the combination of fluconazole and cyclosporine in Candida albicans. | 2000 Sep |
|
Activation of cytochrome P450 gene expression in the rat brain by phenobarbital-like inducers. | 2000 Sep |
|
Gender differences in depression associated with neurologic illness: clinical correlates and pharmacologic response. | 2001 |
|
A randomized trial of fluoxetine versus amitriptyline in musculo-skeletal pain. | 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 |
|
Dopaminergic activity in transgenic mice underexpressing glucocorticoid receptors: effect of antidepressants. | 2001 |
|
Amitriptyline versus bupivacaine in rat sciatic nerve blockade. | 2001 Apr |
|
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 |
|
Antidepressive treatment with amitriptyline and paroxetine: comparable effects on heart rate variability. | 2001 Apr |
|
Changes in quantitatively assessed tremor during treatment of major depression with lithium augmented by paroxetine or amitriptyline. | 2001 Apr |
|
[Sensory neuropathy in HIV infection: pathogenesis and therapy]. | 2001 Apr 14 |
|
Review of pharmacokinetic and pharmacodynamic interaction studies with citalopram. | 2001 Aug |
|
Interaction of psychotropic drugs with monoamine oxidase in rat brain. | 2001 Aug |
|
Cytochrome P450 2D6.1 and cytochrome P450 2D6.10 differ in catalytic activity for multiple substrates. | 2001 Aug |
|
Regional potassium distribution in the brain in forensic relevant types of intoxication preliminary morphometric evaluation using a histochemical method. | 2001 Feb |
|
Preventive therapy in pediatric migraine. | 2001 Feb |
|
Antidepressant treatment and global tests of coagulation and fibrinolysis. | 2001 Feb |
|
Amitriptyline v. the rest: still the leading antidepressant after 40 years of randomised controlled trials. | 2001 Feb |
|
The effect of polyelectrolyte counterion specificity, charge density, and conformation on polyelectrolyte-amphiphile interaction: the carrageenan/furcellaran-amitriptyline system. | 2001 Feb |
|
Salmon calcitonin potentiates the analgesia induced by antidepressants. | 2001 Jan |
|
Serum levels of amitriptyline and therapeutic effect in non-delusional moderately to severely depressed in-patients: a therapeutic window relationship. | 2001 Jan |
|
The effects of antidepressants on obstructed and unobstructed gait in healthy elderly people. | 2001 Jan |
|
Amitriptyline enhances the central component of physiological tremor. | 2001 Jan |
|
Late-onset GM2 gangliosidosis presenting as burning dysesthesias. | 2001 Jul |
|
Antinociception by tricyclic antidepressants in the rat formalin test: differential effects on different behaviours following systemic and spinal administration. | 2001 Jul |
|
[Ciguatera: clinical relevance of a marine neurotoxin]. | 2001 Jul 13 |
|
Assessment of DNA damage in C6 glioma cells after antidepressant treatment using an alkaline comet assay. | 2001 Jun |
|
Involvement of adenosine in the effect of antidepressants on glutamate and aspartate release in the rat prefrontal cortex. | 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 |
|
[Comparative studies of adverse effects in patients with refractory depression treated with amitryptyline, mianserin and unilateral ECT]. | 2001 Mar-Apr |
|
Antidepressant drugs in dermatology. | 2001 May |
|
Bipolar disorder after mefloquine treatment. | 2001 May |
|
Treatment of neuropathic pain with venlafaxine. | 2001 May |
|
Advances in the management of neuropathic pain. | 2001 May |
|
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 |
|
Antidepressants as risk factor for ischaemic heart disease: case-control study in primary care. | 2001 Sep 22 |
|
Intersegmental vessel formation in zebrafish: requirement for VEGF but not BMP signalling revealed by selective and non-selective BMP antagonists. | 2010 Sep |
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
Created
by
admin
on
Edited
Thu Jul 06 23:19:45 UTC 2023
by
admin
on
Thu Jul 06 23:19:45 UTC 2023
|
Record UNII |
1806D8D52K
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Systematic Name | English | ||
|
Brand Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
WHO-ATC |
N06CA01
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
||
|
WHO-ESSENTIAL MEDICINES LIST |
24.2.1
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
||
|
FDA ORPHAN DRUG |
288809
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
||
|
WHO-VATC |
QN06AA09
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
||
|
LIVERTOX |
NBK548410
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
||
|
NDF-RT |
N0000175752
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
||
|
FDA ORPHAN DRUG |
739620
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
||
|
WHO-ESSENTIAL MEDICINES LIST |
8.4
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
||
|
NCI_THESAURUS |
C94727
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
||
|
WHO-VATC |
QN06CA01
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
||
|
WHO-ATC |
N06AA09
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
D000639
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
PRIMARY | |||
|
Amitriptyline
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
PRIMARY | |||
|
100000092029
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
PRIMARY | |||
|
AMITRIPTYLINE
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
PRIMARY | |||
|
3007
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
PRIMARY | |||
|
976
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
PRIMARY | |||
|
2160
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
PRIMARY | |||
|
200
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
PRIMARY | |||
|
50-48-6
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
PRIMARY | |||
|
SUB05462MIG
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
PRIMARY | |||
|
2666
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
PRIMARY | |||
|
M1753
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
PRIMARY | Merck Index | ||
|
C62005
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
PRIMARY | |||
|
704
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
PRIMARY | RxNorm | ||
|
CHEMBL629
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
PRIMARY | |||
|
1806D8D52K
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
PRIMARY | |||
|
DTXSID7022594
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
PRIMARY | |||
|
DB00321
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
PRIMARY | |||
|
180
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
PRIMARY | |||
|
1806D8D52K
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
PRIMARY | |||
|
200-041-6
Created by
admin on Thu Jul 06 23:19:47 UTC 2023 , Edited by admin on Thu Jul 06 23:19:47 UTC 2023
|
PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
METABOLIC ENZYME -> SUBSTRATE |
Metabolizing reaction by CYP2D6: N-demethylation
|
||
|
TRANSPORTER -> INHIBITOR | |||
|
BINDER->LIGAND |
BINDING
|
||
|
TARGET -> INHIBITOR | |||
|
METABOLIC ENZYME -> SUBSTRATE | |||
|
SALT/SOLVATE -> PARENT | |||
|
METABOLIC ENZYME -> SUBSTRATE | |||
|
SALT/SOLVATE -> PARENT |
|
||
|
METABOLIC ENZYME -> INHIBITOR |
IC50
|
||
|
TRANSPORTER -> INHIBITOR | |||
|
TARGET -> INHIBITOR | |||
|
BINDING PROTEIN->LIGAND |
Amitriptyline displayed an approximately 2:1 [drug:AGP] binding stoichiometry; DETERMINED BY ITC
BINDING
Kd
|
||
|
TARGET -> INHIBITOR | |||
|
TRANSPORTER -> SUBSTRATE |
Related Record | Type | Details | ||
---|---|---|---|---|
|
METABOLITE -> PARENT |
|
||
|
METABOLITE -> PARENT |
URINE
|
||
|
METABOLITE ACTIVE -> PARENT |
MAJOR
|
||
|
METABOLITE -> PARENT |
|
||
|
METABOLITE -> PARENT |
URINE
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
PARENT -> IMPURITY |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
PARENT -> IMPURITY |
UNSPECIFIED
EP
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |
|
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
---|---|---|---|---|---|---|
Volume of Distribution | PHARMACOKINETIC |
|
|
|||
Volume of Distribution | PHARMACOKINETIC |
|
|
|||
MAXIMUM TOLERATED DOSE | TOXICITY |
|
DEPRESSION, INPATIENTS: 300 MG/DAY |
|
||
Route of Elimination | PHARMACOKINETIC |
|
|
|||
Biological Half-life | PHARMACOKINETIC |
|
|
|||