Buy Protriptyline (Vivactil) Cas 438-60-8

Protriptyline, sold under the brand name Vivactil among others, is a tricyclic antidepressant (TCA), specifically a secondary amine. Uniquely among most of the TCAs, protriptyline tends to be energizing instead of sedating, and is sometimes used for narcolepsy to achieve a wakefulness-promoting effect.^[3]

TCAs including protriptyline are also used to reduce the incidence of recurring headaches such as migraine, and for other types of chronic pain.^[4]

Medical uses

Protriptyline is used primarily to treat depression and to treat the combination of symptoms of anxiety and depression.^[5] Like most antidepressants of this chemical and pharmacological class, protriptyline has also been used in limited numbers of patients to treat panic disorder, obsessive-compulsive disorder, attention-deficit/hyperactivity disorder, enuresis, eating disorders such as bulimia nervosa, cocaine dependency, and the depressive phase of bipolar disorder (manic-depressive) disorder. It has also been used to support smoking cessation programs.^[6]

Protriptyline is available as 5 mg and 10 mg tablets.^[7] Doses range from 15 to 40 mg per day and can be taken in one daily dose or divided into up to four doses daily.^[7] Some people with severe depression may require up to 60 mg per day.^[7]

In adolescents and people over age 60, therapy should be initiated at a dose of 5 mg three times a day and increased under the supervision of a physician as needed.^[7] Patients over age 60 who are taking daily doses of 20 mg or more should be closely monitored for side effects such as rapid heart rate and urinary retention.^[7]

Like all TCAs, protriptyline should be used cautiously and with close physician supervision. This is especially so for persons with glaucoma, especially angle-closure glaucoma (the most severe form) or urinary retention, for men with benign prostatic hyperplasia (enlarged prostate gland), and for the elderly. Before starting treatment, people should discuss the relative risks and benefits of treatment with their doctors to help determine if protriptyline is the right antidepressant for them.

Buy Protriptyline (Vivactil) Cas 438-60-8

Contraindications

Protriptyline may increase heart rate and stress on the heart.^[9] It may be dangerous for people with cardiovascular disease, especially those who have recently had a heart attack, to take this drug or other antidepressants in the same pharmacological class.^[9] In rare cases in which patients with cardiovascular disease must take protriptyline, they should be monitored closely for cardiac rhythm disturbances and signs of cardiac stress or damage.^[9]

When protriptyline is used to treat the depressive component of schizophrenia, psychotic symptoms may be aggravated. Likewise, in manic-depressive psychosis, depressed patients may experience a shift toward the manic phase if they are treated with an antidepressant drug. Paranoid delusions, with or without associated hostility, may be exaggerated.^[7] In any of these circumstances, it may be advisable to reduce the dose of protriptyline or to use an antipsychotic drug concurrently.^[7]

Side effects

Protriptyline shares side effects common to all TCAs.^[5] The most frequent of these are dry mouth, constipation, urinary retention, increased heart rate, sedation, irritability, decreased coordination, anxiety, blood disorders, confusion, decreased libido, dizziness, flushing, headache, impotence, insomnia, low blood pressure, nightmares, rapid or irregular heartbeat, rash, seizures, sensitivity to sunlight, stomach and intestinal problems.^[7] Other more complicated side effects include; chest pain or heavy feeling, pain spreading to the arm or shoulder, nausea, sweating, general ill feeling; sudden numbness or weakness, especially on one side of the body; sudden headache, confusion, problems with vision, speech, or balance; hallucinations, or seizure (convulsions); easy bruising or bleeding, unusual weakness; restless muscle movements in your eyes, tongue, jaw, or neck; urinating less than usual or not at all; extreme thirst with headache, nausea, vomiting, and weakness; or feeling light-headed or fainting.

PROTRIPTYLINE

PROTRIPTYLINE structure

CAS No.: 438-60-8

Chemical Name:: PROTRIPTYLINE

Synonyms: Triptil;Vivactil;Amimetilina;Protriptylin;PROTRIPTYLINE;Protryptyline;Protriptyline-d6;Protriptyline 13CD3;DIBENZO(A,D)CYCLOHEPTENE-5-PROPYLAMINE,N-METHYL-;3-(dibenzo(a,d)cyclohepten-5-yl)propylmethylamine

CBNumber:: CB0774981

Molecular Formula:: C19H21N

Molecular Weight:: 263.38

MDL Number:: MFCD00242993

MOL File:: 438-60-8.mol

MSDS File:: SDS

Last updated:2026-05-11 16:31:51

Product description	Number	Pack Size	Price
PROTRIPTYLINE-D6 95.00%	RDL0007077	5MG	$499.57
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PROTRIPTYLINE Properties

Boiling point	396.62°C (rough estimate)
Density	0.9076 (rough estimate)
refractive index	1.7500 (estimate)
pka	8.2(at 25℃)
FDA UNII	4NDU154T12
ATC code	N06AA11
EPA Substance Registry System	Protriptyline (438-60-8)

SAFETY

Risk and Safety Statements

Hazardous Substances Data	438-60-8(Hazardous Substances Data)

PROTRIPTYLINE price

Manufacturer	Product number	Product description	CAS number	Packaging	Price	Updated	Buy
American Custom Chemicals Corporation	RDL0007077	PROTRIPTYLINE-D6 95.00%	438-60-8	5MG	$499.57	2021-12-16	Buy

PROTRIPTYLINE Chemical Properties, Uses, Production

Uses

Antidepressant.

Uses

Protriptyline is a powerful antidepressant, the mechanism of action of which is not known. It is not a MAO inhibitor and does not stimulate the CNS. It begins to act much faster and acts much longer than imipramine or amitriptyline. Protriptyline does not possess sedative tranquilizing properties. It is used in clinical conditions for treating severe depression.

Definition

ChEBI: Protriptyline is a carbotricyclic compound. It has a role as an antidepressant. It derives from a hydride of a dibenzo[a,d][7]annulene.

brand name

Vivactil (Odyssey).

Mechanism of action

Protriptyline exhibits high selectivity for the NE transporter, but with less potency than desipramine. Its mechanism of action is similar to that of desipramine. Minimal effect on 5-HT reuptake has been observed.

Synthesis

Protriptyline, N-methyl-5-H-dibenzo[a,d]cyclohepten-5-propylamine (7.1.22), differs from all of the drugs described above in that there is present a double bond at the C10¨CC11 position of the central 7-membered ring of the tricyclic part of the molecule. At the same time, a free electron pair on C5 belonging to either a nitrogen atom or an exocyclic double bond are excluded, which undoubtedly changes both the architecture of the whole molecule as well as, the collocation of pharmacophore groups.
Protriptyline is synthesized by alkylation of 5-H-dibenzo[a,d]cycloheptene with 3-(Nphormyl-N-methylamino)propylchloride (7.1.20), which is synthesized from compound (7.1.19). The resulting intermediate product (7.1.21) undergoes alkaline hydrolysis, which leads to the formation of protriptyline (7.1.21) [33¨C38].

Synthesis_438-60-8

Metabolism

Protriptyline is a dibenzocycloheptriene TCA that differs from the other tricyclics by having an unsaturated ethylene bridge joining the two aromatic rings and a secondary aminopropyl side chain. Protriptyline is completely absorbed from the GI tract and slowly eliminated. Metabolism data are limited for protriptyline, but it is most likely to be metabolized via the same pathways as the other TCAs are. Very little drug is excreted in the feces via the bile.

PROTRIPTYLINE Preparation Products And Raw materials

Raw materials

Preparation Products

PROTRIPTYLINE Suppliers

Global Suppliers ( 30)

Supplier	Tel	Email	Country	ProdList	Advantage
Shaanxi Didu New Materials Co. Ltd	+86-86-17392712779 +86-13289823923	1090@dideu.com	China	8651	58
TargetMol Chemicals Inc.	13564774135	marketing@targetmol.com	United States	19950	58
DAYANG CHEM (HANGZHOU) CO.,LTD	+86-88938639 +86-17705817739	info@dycnchem.com	China	53736	58
Shenzhen Polymeri Biochemical Technology Co., Ltd.	+86-400-002-6226	sales@rrkchem.com	China	57336	58
Shaanxi DIDU pharmaceutical and Chemical Co., Ltd	029-029-029-81148696 18161915376	1027@dideu.com	China	9989	58
TargetMol Chemicals Inc.	4008200310 15002144251	marketing@tsbiochem.com	China	24951	58

View Latest Price from PROTRIPTYLINE manufacturers

Image	Update time	Product	Price	Min. Order	Purity	Supply Ability	Manufacturer
	2026-05-11	Protriptyline 438-60-8	$1520.00-2500.00			10g	TargetMol Chemicals Inc.

438-60-8 (PROTRIPTYLINE) Related Search:

Amitriptyline hydrochloride Amitriptyline Cetirizine Bumetanide Paroxetine

Tiopronin Cyclobenzaprine HCl Protriptyline hydrochloride PROTRIPTYLINE PROTRIPTYLINE-D3,100/MLINMETHANOL,PROTRIPTYLINE-D3

5H-dibenzo[a,d]cycloheptene

PROTRIPTYLINEHYDROCHLORIDE,1.0MG/ML(FREEBASE)INMETHANOL DIBENZO(A,D)CYCLOHEPTENE-5-PROPYLAMINE,N-METHYL- N-Methyl-5H-dibenzo[a,d]cycloheptene-5-propan-1-amine Protriptyline-d6 PROTRIPTYLINE 3-(5H-Dibenzo[a,d]cyclohepten-5-yl)-N-methyl-1-propanamine 5-(3-Methylaminopropyl)-5H-Dibenzo[a,d]cycloheptene 5H-Dibenzo[a,d]cycloheptene-5-propanamine, N-methyl- 5H-Dibenzo[a,d]cycloheptene-5-propylamine, N-methyl- 7-(3-Methylaminopropyl)-1,2:5,6-dibenzocycloheptatriene Amimetilina N-3-(5H-Dibenzo(a,d)cyclohepten-5-yl)propyl-N-methylamine N-Methyl-5H-dibenzo[a,d]cycloheptene-5-propylamine Protryptyline Triptil Vivactil 3-(dibenzo(a,d)cyclohepten-5-yl)propylmethylamine 3-(5H-dibenzo[a,d][7]annulen-5-yl)-N-methylpropan-1-amine Protriptylin Protriptyline 13CD3 438-60-8

CAS 438-60-8 Protriptyline | Products & Prices & Suppliers

Antidepressant.

Product Name: Protriptyline
Molecular Weight: 263.384
Molecular Formula: C₁₉H₂₁N
Synonyms: 3-(5H-Dibenzo[a,d]cyclohepten-5-yl)-N-methyl-1-propanamine; 3-(dibenzo(a,d)cyclohepten-5-yl)propylmethylamine; 5-(3-Methylaminopropyl)-5H-Dibenzo[a,d]cycloheptene; 5H-Dibenzo[a,d]cycloheptene-5-propanamine, N-methyl-; 5H-Dibenzo[a,d]cycloheptene-5-propylamine,N-methyl; Amimetilina

Protriptyline | CAS No: 438-60-8 – aquigenbio.com
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Protriptyline

Catalog No.

S561175

CAS No.

438-60-8

M.F

C19H21N

M. Wt

263.4 g/mol

Availability

In Stock

* This item is exclusively intended for research purposes and is not designed for human therapeutic applications or veterinary use.

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General Information

Avoid sedative artifacts in NET studies. Protriptyline (CAS 438-60-8) is a secondary amine TCA with >13-fold selectivity for NET over SERT and minimal H1/M1 binding, ensuring clean noradrenergic data. Key attributes: • 74-198 h half-life, low first-pass metabolism (10-25%) for stable steady-state in chronic dosing. • Reference standard for FIASMA and lysosomal trapping assays. • Supplied with comprehensive QC documentation. In stock for immediate shipment.

CAS Number

438-60-8

Product Name

Protriptyline

IUPAC Name

N-methyl-3-(2-tricyclo[9.4.0.03,8]pentadeca-1(15),3,5,7,9,11,13-heptaenyl)propan-1-amine

Molecular Formula

C19H21N

Molecular Weight

263.4 g/mol

InChI

InChI=1S/C19H21N/c1-20-14-6-11-19-17-9-4-2-7-15(17)12-13-16-8-3-5-10-18(16)19/h2-5,7-10,12-13,19-20H,6,11,14H2,1H3

InChI Key

BWPIARFWQZKAIA-UHFFFAOYSA-N

solubility

SOL: 1 G IN ABOUT 2 ML WATER, ABOUT 2 ML METHANOL, ABOUT 2.3 ML CHLOROFORM, ABOUT 4 ML ALCOHOL; PRACTICALLY INSOL IN ETHER /HYDROCHLORIDE/
Freely sol in water /hydrochloride/
2.31e-04 g/L

Synonyms

Hydrochloride, Protriptyline, Protriptyline, Protriptyline Hydrochloride, Vivactil

Canonical SMILES

CNCCCC1C2=CC=CC=C2C=CC3=CC=CC=C13

The exact mass of the compound Protriptyline is unknown and the complexity rating of the compound is unknown. The solubility of this chemical has been described as 1.04 mg/l2.31e-04 g/l. The storage condition is unknown. Please store according to label instructions upon receipt of goods.Use and application categories indicated by third-party sources: Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients. However, this does not mean our product can be used or applied in the same or a similar way.

Purity

≥98%

Package Size

10 mg, 25 mg, 50 mg, 1 g

Protriptyline: Baseline Overview

Protriptyline is a secondary amine tricyclic antidepressant (TCA) distinguished by its highly potent, preferential inhibition of the norepinephrine transporter (NET) and an exceptionally prolonged pharmacokinetic half-life[1]. Unlike tertiary amine TCAs, protriptyline lacks significant sedative properties, making it a highly activating compound with a distinct neuropharmacological profile [2]. Its high lipophilicity (LogP ~4.7) and basicity (pKa > 8.5) further define its utility as a reliable reference standard in monoamine transporter assays, long-duration pharmacokinetic benchmarking, and lysosomal trapping models [3].

Research Fit

✓NET-selective secondary amine TCA; supports norepinephrine pathway studies

✓Non-sedating profile may reduce confound in behavioral research models

✓Distinct transporter selectivity profile vs. tertiary amine TCAs

References

Why Generic Protriptyline Substitution Fails

Substituting protriptyline with more common TCAs like amitriptyline or nortriptyline compromises experimental integrity in both pharmacokinetic and behavioral models [1]. Tertiary amines like amitriptyline exhibit high off-target affinity for histaminergic (H1) and muscarinic (M1) receptors, introducing profound sedative and anticholinergic artifacts that confound neurobehavioral data [1]. Furthermore, protriptyline’s unique pharmacokinetic profile—featuring a half-life of 74 to over 100 hours and exceptionally low first-pass hepatic metabolism (10-25%)—cannot be replicated by nortriptyline, which clears much faster and requires completely different steady-state dosing regimens [2]. Procurement of exact protriptyline is therefore mandatory for long-duration in vivo studies and highly selective NET-inhibition assays where baseline activation and stable plasma levels are critical.

Substitution Risk

Transporter selectivitySwitching to a tertiary amine TCA may shift NET/SERT balance, altering monoaminergic endpoints

Pharmacokinetic profileExceptionally long half-life (54–198 h) requires different protocol timing than shorter-acting TCAs

Endpoint profileSedation and psychomotor endpoints differ; protriptyline reported no impairment in human performance studies, while comparators showed deficits

References

Protriptyline Evidence Guide

NET Selectivity Profile

Protriptyline demonstrates highly potent and preferential binding to the norepinephrine transporter (NET) over the serotonin transporter (SERT)[1]. In competitive radioligand binding assays, protriptyline exhibits a Ki of 1.41 nM for NET, compared to a significantly weaker Ki of 19.6 nM for SERT[1]. This >13-fold selectivity for NET differentiates it from tertiary amine TCAs like amitriptyline, which have a more balanced or SERT-skewed profile, making protriptyline a superior reference standard for isolating noradrenergic pathways[2].

Evidence Dimension	Transporter Binding Affinity (Ki)
Target Compound Data	Protriptyline: NET Ki = 1.41 nM, SERT Ki = 19.6 nM
Comparator Or Baseline	Tertiary amine TCAs (e.g., Amitriptyline)
Quantified Difference	>13-fold selectivity for NET over SERT
Conditions	In vitro competitive radioligand binding assay (e.g.,[³H]nisoxetine displacement)

Procuring protriptyline ensures highly selective NET inhibition, eliminating the confounding serotonergic and sedative effects typical of broader-spectrum TCAs in neurochemical assays.

NET Binding

Head-to-head

NET Kd 1.41 nM, SERT Kd 19.6 nM (ratio ~13.9) vs. desipramine NET Ki 0.37 nM, nortriptyline NET Ki 4.37 nM

Supports NET pathway study context; high selectivity margin aids norepinephrine-focused research

Human cloned transporters, radioligand displacement

Extended Half-Life and Low First-Pass Metabolism

Protriptyline possesses an exceptionally long elimination half-life compared to other in-class substitutes, averaging 74 hours and ranging up to 198 hours in long-term models [1]. Additionally, it undergoes limited presystemic first-pass hepatic metabolism (only 10-25%), whereas other TCAs like doxepin or amitriptyline can experience up to 87% first-pass degradation [2]. This distinct pharmacokinetic stability makes protriptyline highly valuable for extended in vivo efficacy studies and steady-state modeling without the need for frequent redosing [1].

Evidence Dimension	Elimination Half-Life & First-Pass Metabolism
Target Compound Data	Protriptyline: ~74-198 hours half-life; 10-25% first-pass metabolism
Comparator Or Baseline	Standard TCAs (e.g., Doxepin, Amitriptyline) with 1-2 day half-lives and up to 87% first-pass metabolism
Quantified Difference	3x to 5x longer half-life; >60% reduction in first-pass degradation
Conditions	In vivo pharmacokinetic profiling (oral administration)

Allows researchers to achieve stable, long-duration steady-state plasma concentrations with minimal first-pass loss, reducing dosing frequency in chronic animal models.

Half-Life

Head-to-head

54–198 h (max >2× nortriptyline, >4× amitriptyline)

Long half-life requires protocol adjustment; may support extended-duration PK/PD models

Human pharmacokinetic data; steady-state may take weeks

ASM Inhibition via Physicochemical Properties

Beyond monoamine reuptake, protriptyline’s specific physicochemical properties—namely a high pKa (≥8.5) and high lipophilicity (LogP ~4.7)—enable it to act as a Functional Inhibitor of Acid Sphingomyelinase (FIASMA) [1]. Structure-property-activity relationship models demonstrate that only compounds meeting these strict pKa and LogP thresholds can successfully accumulate in lysosomes and reduce ASM activity by >50% in H4 cell assays [1]. Protriptyline meets these criteria perfectly, unlike less lipophilic or less basic structural analogs [2].

Evidence Dimension	Lysosomal Trapping and ASM Inhibition
Target Compound Data	Protriptyline: pKa ≥ 8.5, LogP ~4.7, >50% ASM inhibition
Comparator Or Baseline	Low pKa (<8.5) / Low LogP (<3.0) analogs
Quantified Difference	Achieves >50% functional inhibition of ASM, whereas comparators fail to inhibit
Conditions	In vitro H4 cell assay for acid sphingomyelinase activity

Provides a validated, dual-action reference compound for researchers studying lysosomal storage disorders or sphingolipid metabolism pathways.

Sedation Endpoints

Reported

No impairment vs. placebo; amitriptyline 12.5 mg and nortriptyline 25 mg showed significant deficits

Reported endpoint context suggests non-sedating profile; may reduce behavioral confound

Double-blind crossover, healthy volunteers; context-dependent

Arrhythmia Incidence

Reported

No arrhythmias in conscious rabbit model; amitriptyline/doxepin provoked severe arrhythmias

Reported model context shows absence of arrhythmias; supports lower-risk selection for CV studies

Rabbit model, subacute pretreatment; safety endpoint context

Anticholinergic Effect

Class-level

Rated +++ (marked) vs. nortriptyline/desipramine + (mild)

Reported class-level context; higher anticholinergic activity may confound cognition or GI models

Approximation from compiled studies; review for specific model

Protriptyline Application Scenarios

NET Inhibition Reference Standard

Due to its >13-fold selectivity for NET over SERT and lack of tertiary-amine-associated off-target receptor binding (H1/M1), protriptyline is the preferred reference standard for in vitro and in vivo assays designed to isolate noradrenergic signaling pathways without sedative artifacts [1].

Long-Duration PK and Steady-State Modeling

Protriptyline’s exceptionally long half-life (74-198 hours) and low first-pass metabolism (10-25%) make it an ideal candidate for chronic in vivo dosing models. It allows researchers to maintain stable steady-state plasma concentrations with less frequent administration compared to shorter-acting TCAs like nortriptyline or amitriptyline [2].

Lysosomal Trapping and Sphingolipid Research

Driven by its high pKa and LogP, protriptyline is utilized as a Functional Inhibitor of Acid Sphingomyelinase (FIASMA). It is procured for cellular assays investigating lysosomal trapping mechanisms, sphingomyelin accumulation, and the repurposing of highly lipophilic basic amines in neurodegenerative or infectious disease models [3].

Application Fit Matrix

Behavioral depression models

Non-sedating psychomotor profile

Sedation-free behavioral endpoints

Extended-duration PK/PD studies

Exceptionally long half-life

Steady-state and washout protocol validation

Cardiovascular comparator studies

Lower arrhythmia incidence in preclinical models

Arrhythmia endpoint monitoring

Arousal and narcolepsy pathway studies

NET inhibition without sedation

Noradrenergic modulation of wakefulness endpoints

References

Specification

Physical Description

Solid

XLogP3

4.4

Hydrogen Bond Acceptor Count

Hydrogen Bond Donor Count

Exact Mass

263.167399674 Da

Monoisotopic Mass

263.167399674 Da

Heavy Atom Count

LogP

4.7
log Kow= 1.18 @ 25 °C

Decomposition

When heated to decomposition it emits toxic fumes of nitroxides.

Others

Melting Point

169-171 °C (Protriptyline HCl)
Max absorption 290 nm (e= 13,311); MP: 169-171 °C; crystals from isopropanol- ethyl ether /hydrochloride/
169 – 171 °C (protriptyline hydrochloride)

UNII

4NDU154T12

Related CAS

1225-55-4 (hydrochloride)

Drug Indication

For the treatment of depression.
Protriptyline hydrochloride is a tricyclic antidepressant used to improve mood in people with depression. It is also used for anxiety. Protriptyline was first patented in 1962, and it is sold under many brand names. It is an amine with the empirical formula of CHN. It is a more potent antidepressant and has fewer sedative and tranquilizing effects than other TCAs.

Livertox Summary

Protriptyline is a tricyclic antidepressant that was previously widely used in the therapy of major depression. Most of the tricyclic antidepressants have been shown to cause a low rate of mild and transient serum enzyme elevations and rare cases of clinically apparent acute cholestatic liver injury. The potential hepatotoxicity specifically of protriptyline, however, has not been well defined.

Drug Classes

Breast Feeding; Lactation; Milk, Human; Antidepressive Agents; Antidepressive Agents, Tricyclic
Antidepressant Agents

Therapeutic Uses

Adrenergic Uptake Inhibitors; Antidepressive Agents, Tricyclic
TRICYCLIC (DIBENZOCYCLOHEPTENE) ANTIDEPRESSANT DRUG USEFUL IN MGMNT OF ENDOGENOUS & EXOGENOUS DEPRESSIONS. IT ALSO INCR PSYCHOMOTOR ACTIVITY; THIS PROPERTY ENHANCES ITS USE IN WITHDRAWN & ANERGIC PT. /HYDROCHLORIDE/
…MAY BE PARTICULARLY USEFUL IN TREATING DEPRESSED PT WHOSE PREDOMINANT MANIFESTATIONS OF ILLNESS ARE PSYCHOMOTOR RETARDATION, APATHY, & FATIGUE… /HYDROCHLORIDE/
…BECAUSE OF THEIR SEDATIVE PROPERTY. …MAY BE USEFUL IN INITIAL THERAPY OF DEPRESSED PT WITH SLEEP LOSS… DRUGS DO DECR NUMBER OF AWAKENINGS, INCR STAGE-4 SLEEP, & MARKEDLY DECR REM TIME. /TRICYCLIC ANTIDEPRESSANTS/
For more Therapeutic Uses (Complete) data for PROTRIPTYLINE (8 total), please visit the HSDB record page.

Mechanism of Action

Protriptyline acts by decreasing the reuptake of norepinephrine and serotonin (5-HT).
ACTION OF TRICYCLIC ANTIDEPRESSANTS ON METAB OF CATECHOLAMINES & INDOLEAMINES IN BRAIN HAS CONTRIBUTED SIGNIFICANTLY TO “BIOGENIC AMINE HYPOTHESIS” OF DEPRESSION. … /ALL/ BLOCK RE-UPTAKE OF NOREPINEPHRINE BY ADRENERGIC NERVE TERMINALS. /DEMETHYLATED ANALOGS ARE MORE POTENT IN THIS ACTION/ /TRICYCLIC ANTIDEPRESSANTS/

Other CAS

438-60-8

Absorption Distribution and Excretion

Protriptyline is reported to undergo cumulative urinary excretion during 16 days, which accounts for approximately 50% of the total drug administered. The fecal excretion pathway seems to play a minimal role in drug elimination.
EXCRETION…IS RAPID, IN CONTRAST TO LONG LATENCY OF ONSET OF ACTION OF DRUGS. /TRICYCLIC ANTIDEPRESSANTS/
…WELL ABSORBED FROM GI TRACT. … RAPIDLY DISTRIBUTED & METABOLIZED BY DEMETHYLATION, OXIDATION, & AROMATIC HYDROXYLATION. /IMIPRAMINE/
IN URINE OF RATS TREATED WITH PROTRIPTYLINE… THERE WAS TWICE AS MUCH 10,11-DIHYDRO-10,11-EPOXY-5-(3-METHYLAMINOPROPYL)-5H-DIBENZO[A,D]CYCLOHEPTENE AS 10,11-DIHYDRO-10,11-EPOXY-5-(3-AMINOPROPYL)-5H-DIBENZO[A,D]CYCLOHEPTENE EXCRETED &…/BOTH/ ACCOUNTED FOR 40% OF DOSE OF PROTRIPTYLINE.
MEAN PLASMA LEVELS FOR PROTRIPTYLINE IN PT ALSO ADMIN NITRAZEPAM INDISTINGUISHABLE FROM PT RECEIVING NO NITRAZEPAM. MEAN PLASMA LEVELS FOR PT RECEIVING SODIUM AMYLOBARBITONE SIGNIFICANTLY DECR. EARLY VALUES MAY BE OF PREDICTIVE IMPORTANCE TO PERMIT EARLY DOSE ADJUSTMENT.

Metabolism Metabolites

KNOWN OXIDATION OF 10,11 DOUBLE BOND OF PROTRIPTYLINE IN MAN, MINIATURE PIG, & DOG… 2 METABOLITES HAVE BEEN DETECTED WHICH DEMONSTRATE EPOXIDE INTERMEDIATE, NAMELY, DIHYDRODIOL & REARRANGEMENT PRODUCT WHOSE FORMATION IS…CATIONIC INTERMEDIATE…REARRANGING TO DIHYDROANTHRACENIC STRUCTURE.
IN DOGS, MINIATURE PIGS, & MAN, 3 URINARY METABOLITES HAVE NOW BEEN FOUND 10-HYDROXY-N-METHYL-5H-DIBENZO(AD)CYCLOHEPTENE-5-PROPYLAMINE, 10,11-DIHYDROXY-N-METHYL-5H-DIBENZO(AD)CYCLOHEPTENE-5-PROPYLAMINE & 5,10-DIHYDRO-10-FORMYLANTHRACENE-5-PROPYLAMINE.
…PROTRIPTYLINE…AFFORDS URINARY 10,11-OXIDE.
IN URINE OF RATS TREATED WITH PROTRIPTYLINE…2 METABOLITES HAVE BEEN IDENTIFIED…AS 10,11-DIHYDRO-10,11-EPOXY-5-(3-M ETHYLAMINOPROPYL)-5H-DIBENZO[A,D]CYCLOHEPTENE & 10,11-DIHYDRO-10,11-EPOXY-5-(3-AMINOPROPYL)-5H-DIBENZO[A,D]CYCLOHEPTENE.
Route of Elimination: Cumulative urinary excretion during 16 days accounted for approximately 50% of the drug. The fecal route of excretion did not seem to be important.

Associated Chemicals

Protriptyline hydrochloride;1225-55-4

Wikipedia

Protriptyline

FDA Medication Guides

VIVACTIL
PROTRIPTYLINE HYDROCHLORIDE
TABLET;ORAL
TEVA WOMENS
07/17/2014

Drug Warnings

…POSSESSES ANTICHOLINERGIC PROPERTIES &, HENCE, SHOULD NOT BE USED IN PT WITH PYLORIC OBSTRUCTION, GLAUCOMA, OR URINARY RETENTION. /HYDROCHLORIDE/
…THOSE WITH SYMPTOMS OF AGITATION, ANXIETY, & TENSION FREQUENTLY BECOME MORE DISTURBED WITH USE OF PROTRIPTYLINE.
DRUG MAY AGGRAVATE ANXIETY, & IT SHOULD NOT BE USED IN ANXIOUS DEPRESSED PT UNLESS IT IS GIVEN WITH SEDATIVE DRUG, SUCH AS PHENOTHIAZINE WITH SEDATIVE EFFECTS…OR MORE CONVENTIONAL SEDATIVE DRUG… /HYDROCHLORIDE/
TACHYCARDIA & POSTURAL HYPOTENSION OCCUR MORE FREQUENTLY…THAN WITH OTHER ANTIDEPRESSANT DRUGS; HENCE, PT WITH CARDIOVASCULAR DISORDERS & ELDERLY PT SHOULD BE OBSERVED CLOSELY FOR THESE UNTOWARD EFFECTS. /HYDROCHLORIDE/
For more Drug Warnings (Complete) data for PROTRIPTYLINE (28 total), please visit the HSDB record page.

Biological Half Life

AFTER A SINGLE ORAL DOSE OF 30 MG TO 8 SUBJECTS, PEAK LEVELS RANGED FROM 10.4-22.3 NG/ML, 6-12 HR AFTER ADMIN. MEAN T/2 WAS 74.3 HR & RANGED FROM 53.6-91.7 HR IN INDIVIDUAL SUBJECTS.
SINGLE ORAL DOSE OF HCL-SALT ADMIN TO 8 PERSONS. EST 1ST PASS METAB WAS RELATIVELY SMALL, 10-25% OF DOSE, ASSUMING COMPLETE ABSORPTION. MEAN VOL OF DISTRIBUTION 22.5 L/KG & RANGED FROM 15.0-31.2 L/KG. CONCLUSION WAS THAT LONG T/2 IS CORRELATED WITH SMALL 1ST PASS METABOLISM.
PLASMA LEVELS IN 30 PT. AFTER 3.5 WK TREATMENT @ 40 MG/DAY, PLASMA LEVELS RANGED FROM 430-1430 NMOL/L. SINGLE DOSE STUDIES IN 5 VOLUNTEERS SUGGEST THAT VOL OF DISTRIBUTION OF PROTRIPTYLINE SHOWS LITTLE INTERSUBJECT VARIATION. HOWEVER, T/2 MAY VARY, RANGING FROM 54-198 HR.

Use Classification

Pharmaceuticals

Methods of Manufacturing

Engelhardt, Christy, Belgian patent 617,967 (1962 to Merck & Co) CA 59, 517f (1963); Tishler et al, US patent 3,244,748 & 3,271,451 (both 1966 to Merck & Co); Engelhardt et al, J Med Chem 11, 325 (1968).

Analytic Laboratory Methods

…MAY BE EXTRACTED FROM ALKALINIZED SAMPLE BY ORGANIC SOLVENT. REEXTRACTED INTO DILUTE ACID YIELDS SOLN WHOSE PORTRIPTYLINE CONTENT CAN BE ASSAYED BY SPECTROFLUOROMETRY.

Clinical Laboratory Methods

GAS CHROMATOGRAPHY METHOD USING EITHER A CONVENTIONAL PACKED COLUMN OR A CAPILLARY COLUMN FOR MEASUREMENT OF THERAPEUTIC PLASMA CONCN OF TRICYCLIC ANTIDEPRESSANT DRUGS & THEIR DEMETHYLATED METABOLITES.
HIGH PRESSURE LIQUID CHROMATOGRAPHIC PROCEDURES REPORTED FOR DETERMINATION OF AMITRIPTYLINE & NORTRIPTYLINE. SEPARATIONS & QUANTITATIONS WERE CARRIED OUT @ AMBIENT TEMP USING A SILICA COLUMN WITH A VARIABLE WAVELENGTH UV DETECTOR. ANALYSIS PERFORMED ON 0.25 ML SERUM.

Interactions

Other interactions that also may potentiate the effects of tricyclic antidepressants can result from interference with their metabolism in the liver. This effect has been associated with neuroleptic drugs, methylphenidate, and certain steroids, including oral contraceptives. /Tricyclic antidepressants/
TRICYCLIC ANTIDEPRESSANTS MAY ENHANCE EFFECTS OF ORAL ANTICOAGULANTS. /TRICYCLIC ANTIDEPRESSANTS/
A PARTICULARLY SEVERE, BUT RARE, DRUG-DRUG INTERACTION HAS BEEN NOTED FOLLOWING THE CONCURRENT ADMINISTRATION OF AN MAO INHIBITOR AND A TRICYCLIC ANTIDEPRESSANT. /TRICYCLIC ANTIDEPRESSANTS/
THIS AGENT IS ALSO CONTRAINDICATED IN PT TAKING ANY OF MAO INHIBITOR ANTIDEPRESSANTS, SUCH AS NIALAMIDE, ISOCARBOXAZID, TRANYLCYPROMINE, OR PHENELZINE. /HYDROCHLORIDE/
For more Interactions (Complete) data for PROTRIPTYLINE (32 total), please visit the HSDB record page.

Stability Shelf Life

REASONABLY STABLE IN LIGHT, STABLE IN AIR, & STABLE IN HEAT UNDER USUAL PREVAILING TEMP /HYDROCHLORIDE/

Reference

Effect of Protriptyline on [Ca²⁺]i and Viability in MDCK Renal Tubular Cells

He-Hsiung Cheng, Chiang-Ting Chou, Wei-Zhe Liang, Chun-Chi Kuo, Pochuen Shieh, Jue-Long Wang, Chung-Ren Jan
PMID: 28468029 DOI: 10.4077/CJP.2017.BAF459

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