Details
Stereochemistry | ACHIRAL |
Molecular Formula | C10H12N2 |
Molecular Weight | 160.2157 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
C(C1=NCCN1)C2=CC=CC=C2
InChI
InChIKey=JIVZKJJQOZQXQB-UHFFFAOYSA-N
InChI=1S/C10H12N2/c1-2-4-9(5-3-1)8-10-11-6-7-12-10/h1-5H,6-8H2,(H,11,12)
Tolazoline, also known as priscoline, was used in treatment of persistent pulmonary hypertension of the newborn. But that prescription was discontinued. Priscoline given intravenously produces vasodilatation, primarily due to a direct effect on vascular smooth muscle, and cardiac stimulation; the blood pressure response depends on the relative contributions of the two effects. Priscoline usually reduces pulmonary arterial pressure and vascular resistance. The mechanisms of its therapeutic effects are not clear, but is known, that tolazoline is a non-selective competitive α-adrenergic receptor antagonist and it possesses histamine agonist activity.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2094251 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11938943 |
|||
Target ID: CHEMBL231 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8487790 |
|||
Target ID: CHEMBL1941 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8487790 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | PRISCOLINE Approved UseUnknown Launch Date-6.8774402E11 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3.8 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3576663 |
3.2 mg single, intravenous dose: 3.2 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
TOLAZOLINE blood | Homo sapiens population: UNHEALTHY age: NEWBORN sex: FEMALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
0.15 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3576663 |
3.2 mg single, intravenous dose: 3.2 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
TOLAZOLINE blood | Homo sapiens population: UNHEALTHY age: NEWBORN sex: FEMALE food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
2 mg/kg single, intravenous Highest studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
unhealthy, 36 weeks n = 47 Health Status: unhealthy Age Group: 36 weeks Population Size: 47 Sources: |
Other AEs: Erythema, Thrombocytopenia... Other AEs: Erythema (60%) Sources: Thrombocytopenia (45%) Hyponatremia (40%) Gastric acid increased (36%) Seizures (30%) Hematuria (23%) Hypotension (19%) Oliguria (11%) Abdominal distension (9%) Activity motor exaggerated (6%) Tracheal bleeding (6%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Oliguria | 11% | 2 mg/kg single, intravenous Highest studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
unhealthy, 36 weeks n = 47 Health Status: unhealthy Age Group: 36 weeks Population Size: 47 Sources: |
Hypotension | 19% | 2 mg/kg single, intravenous Highest studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
unhealthy, 36 weeks n = 47 Health Status: unhealthy Age Group: 36 weeks Population Size: 47 Sources: |
Hematuria | 23% | 2 mg/kg single, intravenous Highest studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
unhealthy, 36 weeks n = 47 Health Status: unhealthy Age Group: 36 weeks Population Size: 47 Sources: |
Seizures | 30% | 2 mg/kg single, intravenous Highest studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
unhealthy, 36 weeks n = 47 Health Status: unhealthy Age Group: 36 weeks Population Size: 47 Sources: |
Gastric acid increased | 36% | 2 mg/kg single, intravenous Highest studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
unhealthy, 36 weeks n = 47 Health Status: unhealthy Age Group: 36 weeks Population Size: 47 Sources: |
Hyponatremia | 40% | 2 mg/kg single, intravenous Highest studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
unhealthy, 36 weeks n = 47 Health Status: unhealthy Age Group: 36 weeks Population Size: 47 Sources: |
Thrombocytopenia | 45% | 2 mg/kg single, intravenous Highest studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
unhealthy, 36 weeks n = 47 Health Status: unhealthy Age Group: 36 weeks Population Size: 47 Sources: |
Activity motor exaggerated | 6% | 2 mg/kg single, intravenous Highest studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
unhealthy, 36 weeks n = 47 Health Status: unhealthy Age Group: 36 weeks Population Size: 47 Sources: |
Tracheal bleeding | 6% | 2 mg/kg single, intravenous Highest studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
unhealthy, 36 weeks n = 47 Health Status: unhealthy Age Group: 36 weeks Population Size: 47 Sources: |
Erythema | 60% | 2 mg/kg single, intravenous Highest studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
unhealthy, 36 weeks n = 47 Health Status: unhealthy Age Group: 36 weeks Population Size: 47 Sources: |
Abdominal distension | 9% | 2 mg/kg single, intravenous Highest studied dose Dose: 2 mg/kg Route: intravenous Route: single Dose: 2 mg/kg Sources: |
unhealthy, 36 weeks n = 47 Health Status: unhealthy Age Group: 36 weeks Population Size: 47 Sources: |
PubMed
Title | Date | PubMed |
---|---|---|
DDT-induced myoclonus: serotonin and alpha noradrenergic interaction. | 1979 Feb |
|
Hypochloremic metabolic alkalosis following tolazoline-induced gastric hypersecretion. | 1980 Feb |
|
Bolus and continuous infusion of tolazoline in neonates with hypoxemia. | 1986 |
|
Blood flow distribution and brain metabolism during tolazoline-induced hypotension in newborn dogs. | 1990 Aug |
|
Spasms of the hepatic artery following percutaneous transluminal angioplasty and tolazoline administration in a liver transplant patient. | 1996 May-Jun |
|
Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding. | 1998 Apr 1 |
|
Endotracheal tolazoline: pharmacokinetics and pharmacodynamics in dogs. | 1999 Sep |
|
Indirect atomic absorption determination of atropine, diphenhydramine, tolazoline, and levamisole based on formation of ion-associates with potassium tetraiodometrcurate. | 2001 Apr |
|
Reinnervation of the biceps brachii muscle following cotransplantation of fetal spinal cord and autologous peripheral nerve into the injured cervical spinal cord of the adult rat. | 2001 Feb |
|
Pharmacologic therapy of persistent pulmonary hypertension of the newborn. | 2001 Jan |
|
Questionnaire on practices and priorities in neonatal care in Ireland. | 2001 Mar |
|
Persistent pulmonary hypertension of the newborn: experience in a single institution. | 2001 Mar-Apr |
|
[A case of Down syndrome with ventricular septal defect and hemodynamical Eisenmenger syndrome]. | 2001 May |
|
Inhaled nitric oxide applications in paediatric practice. | 2002 Jan |
|
Use of azaperone and zuclopenthixol acetate to facilitate translocation of white-tailed deer (Odocoileus virginianus). | 2002 Jun |
|
[Aggression to the immature kidney]. | 2002 Mar-Apr |
|
Re: Nonlocalized lower gastrointestinal bleeding: provocative bleeding studies with intraarterial tPA, heparin, and tolazoline. | 2002 May |
|
Efficacy and safety of tolazoline for treatment of severe hypoxemia in extremely preterm infants. | 2002 May |
|
Is nebulised tolazoline an effective treatment for persistent pulmonary hypertension of the newborn? | 2003 Jan |
|
Octopaminergic modulation of synaptic transmission between an identified sensory afferent and flight motoneuron in the locust. | 2003 Jul 14 |
|
Comparison of the vasodilating effect of nitroglycerin, verapamil, and tolazoline in hand angiography. | 2003 Jun |
|
Pharmacokinetics of xylazine, 2,6-dimethylaniline, and tolazoline in tissues from yearling cattle and milk from mature dairy cows after sedation with xylazine hydrochloride and reversal with tolazoline hydrochloride. | 2003 Summer |
|
An in vitro study of the effects of Cassia podocarpa fruit on the intestinal motility of rats. | 2004 Feb |
|
The effects of imidazoline agents on the aggregation of human platelets. | 2004 Feb |
|
Effectiveness of antagonists for tiletamine-zolazepam/xylazine immobilization in female white-tailed deer. | 2004 Jul |
|
Persistent pulmonary hypertension of the newborn. | 2004 Jun |
|
Clinically diagnosed nonocclusive mesenteric ischemia after cardiopulmonary bypass: retrospective study. | 2004 Mar |
|
Characterisation of some pharmacological effects of the venom from Vipera lebetina. | 2004 Mar 15 |
|
2-(Anilino)imidazolines and 2-(benzyl)imidazoline derivatives as h5-HT1D serotonin receptor ligands. | 2004 Sep 20 |
|
Bench-to-bedside review: Ventilator strategies to reduce lung injury -- lessons from pediatric and neonatal intensive care. | 2005 Apr |
|
Prevention and management of meconium aspiration syndrome--assessment of evidence based practice. | 2005 May |
|
Antagonism by imidazoline-type drugs of muscarinic and other receptors in the guinea-pig ileum. | 2006 Jul |
|
Reported medication use in the neonatal intensive care unit: data from a large national data set. | 2006 Jun |
|
Antagonism of detomidine sedation in the horse using intravenous tolazoline or atipamezole. | 2006 May |
|
Impaired cognition and attention in adults: pharmacological management strategies. | 2007 Feb |
|
Castration of lambs: a welfare comparison of different castration techniques in lambs over 10 weeks of age. | 2007 May |
|
A diazonium ion cascade from the nitrosation of tolazoline, an imidazoline-containing drug. | 2008 Feb |
|
A comparison of two combinations of xylazine-ketamine administered intramuscularly to alpacas and of reversal with tolazoline. | 2008 May |
|
Effect of vasoactive agents on the dermatopharmacokinetics and systemic disposition of model compounds, salicylate and FITC-dextran 4 kDa, following intracutaneous injection of the compounds. | 2008 May 22 |
|
A novel high-throughput screening assay for putative antidiabetic agents through PPARalpha interactions. | 2008 Oct |
|
Evaluation of intramuscular butorphanol, azaperone, and medetomidine and nasal oxygen insufflation for the chemical immobilization of white-tailed deer, Odocoileus virginianus. | 2008 Sep |
|
Butorphanol-azaperone-medetomidine for immobilization of captive white-tailed deer. | 2009 Apr |
|
The clinical outcomes of transcatheter microcoil embolization in patients with active lower gastrointestinal bleeding in the small bowel. | 2009 Jul-Aug |
|
Physiologic effects of nasal oxygen or medical air administered prior to and during carfentanil-xylazine anesthesia in North American elk (Cervus canadensis manitobensis). | 2009 Mar |
|
Adverse drug effects in hospitalized elderly: data from the healthcare cost and utilization project. | 2010 |
|
Effect of sildenafil on digital ulcers in systemic sclerosis: analysis from a single centre pilot study. | 2010 Aug |
|
Functional and pharmacological characterization of a beta-adrenergic-like octopamine receptor from the silkworm Bombyx mori. | 2010 Jun |
|
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. | 2011 Jul 14 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.drugs.com/pro/priscoline.html
An initial dose of 1 to 2 mg/kg, via scalp vein, followed by an infusion of 1 to 2 mg/kg per hour have usually resulted in significant increases in arterial oxygen. There is very little experience with infusions lasting beyond 36 to 48 hours. Response, if it occurs, can be expected within 30 minutes after the initial dose.
Route of Administration:
Intravenous
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
WHO-VATC |
QM02AX02
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
||
|
WHO-VATC |
QV03AB94
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
||
|
WHO-ATC |
M02AX02
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
||
|
WHO-VATC |
QC04AB02
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
||
|
NCI_THESAURUS |
C29713
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
||
|
WHO-ATC |
C04AB02
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
TOLAZOLINE
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
PRIMARY | |||
|
SUB11148MIG
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
PRIMARY | |||
|
59-98-3
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
PRIMARY | |||
|
DTXSID3023683
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
PRIMARY | |||
|
35110
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
PRIMARY | |||
|
DB00797
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
PRIMARY | |||
|
200-448-9
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
PRIMARY | |||
|
100000077751
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
PRIMARY | |||
|
D014043
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
PRIMARY | |||
|
m10936
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
PRIMARY | Merck Index | ||
|
C66608
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
PRIMARY | |||
|
7310
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
PRIMARY | |||
|
4213
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
PRIMARY | |||
|
CHEMBL770
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
PRIMARY | |||
|
CHH9H12AQ3
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
PRIMARY | |||
|
CHH9H12AQ3
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
PRIMARY | |||
|
5504
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
PRIMARY | |||
|
10634
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
PRIMARY | RxNorm | ||
|
2695
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
PRIMARY | |||
|
28502
Created by
admin on Fri Dec 15 16:38:36 UTC 2023 , Edited by admin on Fri Dec 15 16:38:36 UTC 2023
|
PRIMARY |
ACTIVE MOIETY
SALT/SOLVATE (PARENT)