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Details

Stereochemistry ACHIRAL
Molecular Formula C23H16O6.2C20H23N
Molecular Weight 943.1762
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of AMITRIPTYLINE PAMOATE

SMILES

CN(C)CCC=C1C2=CC=CC=C2CCC3=C1C=CC=C3.CN(C)CCC=C4C5=CC=CC=C5CCC6=C4C=CC=C6.OC(=O)C7=CC8=C(C=CC=C8)C(CC9=C%10C=CC=CC%10=CC(C(O)=O)=C9O)=C7O

InChI

InChIKey=HBFZQWHVSYYTGA-UHFFFAOYSA-N
InChI=1S/C23H16O6.2C20H23N/c24-20-16(14-7-3-1-5-12(14)9-18(20)22(26)27)11-17-15-8-4-2-6-13(15)10-19(21(17)25)23(28)29;2*1-21(2)15-7-12-20-18-10-5-3-8-16(18)13-14-17-9-4-6-11-19(17)20/h1-10,24-25H,11H2,(H,26,27)(H,28,29);2*3-6,8-12H,7,13-15H2,1-2H3

HIDE SMILES / InChI

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

Molecular Formula C23H16O6
Molecular Weight 388.3695
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
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.

Originator

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P23975
Gene ID: 6530.0
Gene Symbol: SLC6A2
Target Organism: Homo sapiens (Human)
3.45 nM [IC50]
Target ID: P31645
Gene ID: 6532.0
Gene Symbol: SLC6A4
Target Organism: Homo sapiens (Human)
13.3 nM [IC50]
Target ID: P28223
Gene ID: 3356.0
Gene Symbol: HTR2A
Target Organism: Homo sapiens (Human)
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Preventing
AMITRIPTYLINE HYDROCHLORIDE

Approved Use

For the relief of symptoms of depression. Endogenous depression is more likely to be alleviated than are other depressive states.

Launch Date

1997
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
15.3 ng/mL
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

AUC

ValueDoseCo-administeredAnalytePopulation
593 ng × h/mL
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

T1/2

ValueDoseCo-administeredAnalytePopulation
20.4 h
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

Funbound

ValueDoseCo-administeredAnalytePopulation
7.7%
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

Doses

DosePopulationAdverse 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%)
Dry mouth (20%)
Drowsiness (20%)
Language disorder (20%)
Sources:
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
Mental concentration difficult
Sources:
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...
Other AEs:
Mental status changes
Sources:
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%)
Sleepiness (68.8%)
Dizziness (25%)
Constipation (18.8%)
Palpitations (6.3%)
Malaise (6.3%)
Sources:
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%)
Dry mouth (10%)
Other AEs:
Drowsiness (51.8%)
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%)
Sources:
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%)
Dizziness (4%)
Other AEs:
Sedation (32%)
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%)
Sources:
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
Health Status: healthy
Sex: M+F
Population Size: 96
Sources:
Other AEs: Tachycardia...
Other AEs:
Tachycardia
Sources:
AEs

AEs

AESignificanceDosePopulation
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
Health Status: healthy
Sex: M+F
Population Size: 96
Sources:
Overview

OverviewOther

Drug as perpetrator​Drug as victimTox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
[Cardiac arrest following amitriptylin and adrenaline].
1975 Jun 16
Smoking in patients receiving psychotropic medications: a pharmacokinetic perspective.
2001
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
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
[Sensory neuropathy in HIV infection: pathogenesis and therapy].
2001 Apr 14
Controlling phantom limb pain in Sierra Leone.
2001 Apr 21
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
Cytochrome P450 2D6.1 and cytochrome P450 2D6.10 differ in catalytic activity for multiple substrates.
2001 Aug
Serum levels and cardiovascular effects of tricyclic antidepressants and selective serotonin reuptake inhibitors in depressed patients.
2001 Aug
Regional potassium distribution in the brain in forensic relevant types of intoxication preliminary morphometric evaluation using a histochemical method.
2001 Feb
Mirtazepine: heir apparent to amitriptyline?
2001 Jan-Feb
Late-onset GM2 gangliosidosis presenting as burning dysesthesias.
2001 Jul
Isolated sural neuropathy presenting as lateral ankle pain.
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
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
Assessment of DNA damage in C6 glioma cells after antidepressant treatment using an alkaline comet assay.
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
[Comparative studies of adverse effects in patients with refractory depression treated with amitryptyline, mianserin and unilateral ECT].
2001 Mar-Apr
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
Bipolar disorder after mefloquine treatment.
2001 May
Treatment of neuropathic pain with venlafaxine.
2001 May
Advances in the management of neuropathic pain.
2001 May
Inhibition of synovial plasma extravasation by preemptive administration of an antiinflammatory irrigation solution in the rat knee.
2001 May
Combining psychotherapy and antidepressants in the treatment of depression.
2001 May
[St. John's wort: a pharmaceutical with potentially dangerous interactions].
2001 May 10
High-performance liquid chromatographic method combining radiochemical and ultraviolet detection for determination of low activities of uridine 5'-diphosphate-glucuronosyltransferase.
2001 May 15
Management of chronic tension-type headache with tricyclic antidepressant medication, stress management therapy, and their combination: a randomized controlled trial.
2001 May 2
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
Patents

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
Amitriptyline was used at 40 uM in isolated rat hepatocytes for 60,120,180 min.
Substance Class Chemical
Created
by admin
on Fri Dec 15 18:18:09 GMT 2023
Edited
by admin
on Fri Dec 15 18:18:09 GMT 2023
Record UNII
YX6VNM127F
Record Status Validated (UNII)
Record Version
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Name Type Language
AMITRIPTYLINE PAMOATE
WHO-DD  
Common Name English
2-NAPHTHALENECARBOXYLIC ACID, 4,4'-METHYLENEBIS(3-HYDROXY-, COMPD. WITH 3-(10,11-DIHYDRO-5H-DIBENZO(A,D)CYCLOHEPTEN-5-YLIDENE)-N,N-DIMETHYL-1-PROPANAMINE) (1:2)
Common Name English
2-NAPHTHOIC ACID, 4,4'-METHYLENEBIS(3-HYDROXY-, COMPD. WITH 10,11-DIHYDRO-N,N-DIMETHYL-5H-DIBENZO(A,D)CYCLOHEPTENE-.DELTA.5,.GAMMA.-PROPYLAMINE) (1:2)
Common Name English
1-PROPANAMINE, 3-(10,11-DIHYDRO-5H-DIBENZO(A,D)CYCLOHEPTEN-5-YLIDENE)-N,N-DIMETHYL-, 4,4'-METHYLENEBIS(3-HYDROXY-2-NAPHTHALENECARBOXYLATE)(2:1)
Common Name English
Amitriptyline pamoate [WHO-DD]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C94727
Created by admin on Fri Dec 15 18:18:09 GMT 2023 , Edited by admin on Fri Dec 15 18:18:09 GMT 2023
Code System Code Type Description
RXCUI
235737
Created by admin on Fri Dec 15 18:18:09 GMT 2023 , Edited by admin on Fri Dec 15 18:18:09 GMT 2023
PRIMARY RxNorm
NCI_THESAURUS
C96201
Created by admin on Fri Dec 15 18:18:09 GMT 2023 , Edited by admin on Fri Dec 15 18:18:09 GMT 2023
PRIMARY
SMS_ID
100000127498
Created by admin on Fri Dec 15 18:18:09 GMT 2023 , Edited by admin on Fri Dec 15 18:18:09 GMT 2023
PRIMARY
FDA UNII
YX6VNM127F
Created by admin on Fri Dec 15 18:18:09 GMT 2023 , Edited by admin on Fri Dec 15 18:18:09 GMT 2023
PRIMARY
CAS
17086-03-2
Created by admin on Fri Dec 15 18:18:09 GMT 2023 , Edited by admin on Fri Dec 15 18:18:09 GMT 2023
PRIMARY
ECHA (EC/EINECS)
241-145-1
Created by admin on Fri Dec 15 18:18:09 GMT 2023 , Edited by admin on Fri Dec 15 18:18:09 GMT 2023
PRIMARY
EPA CompTox
DTXSID60168958
Created by admin on Fri Dec 15 18:18:09 GMT 2023 , Edited by admin on Fri Dec 15 18:18:09 GMT 2023
PRIMARY
PUBCHEM
76965204
Created by admin on Fri Dec 15 18:18:09 GMT 2023 , Edited by admin on Fri Dec 15 18:18:09 GMT 2023
PRIMARY
DRUG BANK
DBSALT001193
Created by admin on Fri Dec 15 18:18:09 GMT 2023 , Edited by admin on Fri Dec 15 18:18:09 GMT 2023
PRIMARY
EVMPD
SUB33535
Created by admin on Fri Dec 15 18:18:09 GMT 2023 , Edited by admin on Fri Dec 15 18:18:09 GMT 2023
PRIMARY
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