Drug/Small Molecule:
cinolazepam

PharmGKB contains no dosing guidelines for this drug/small molecule. To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.

PharmGKB contains no drug labels with pharmacogenomic information for this drug/small molecule. To report a drug label with PGx, click here.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • Cinolazepamum [inn-latin]
Trade Names
  • Gerodorm
Brand Mixture Names

PharmGKB Accession Id:
PA164748034

Description

Cinolazepam is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Cinolazepam is not approved for sale in the United States or Canada.

Source: Drug Bank

Indication

For the management of anxiety disorders or for the short-term relief of the symptoms of anxiety or anxiety associated with depressive symptoms.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Cinolazepam binds to central benzodiazepine receptors which interact allosterically with GABA receptors. This potentiates the effects of the inhibitory neurotransmitter GABA, increasing the inhibition of the ascending reticular activating system and blocking the cortical and limbic arousal that occurs following stimulation of the reticular pathways.

Source: Drug Bank

Pharmacology

Cinolazepam is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Cinolazepam is not approved for sale in the United States or Canada.

Source: Drug Bank

Food Interaction

Avoid alcohol.|Avoid excessive quantities of coffee or tea (Caffeine).|Take with food.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic.

Source: Drug Bank

Absorption

Bioavailability following oral administration is 90-100%.

Source: Drug Bank

Half-Life

9 hours

Source: Drug Bank

Toxicity

The onset of impairment of consciousness is relatively rapid in benzodiazepine poisoning. Onset is more rapid following larger doses and with agents of shorter duration of action. The most common and initial symptom is somnolence. This may progress to coma Grade I or Grade II following very large ingestions.

Source: Drug Bank

Chemical Properties

Chemical Formula

C18H13ClFN3O2

Source: Drug Bank

Isomeric SMILES

c1ccc(c(c1)C2=NC(C(=O)N(c3c2cc(cc3)Cl)CCC#N)O)F

Source: OpenEye

Canonical SMILES

OC1N=C(C2=CC=CC=C2F)C2=C(C=CC(Cl)=C2)N(CCC#N)C1=O

Source: Drug Bank

Average Molecular Weight

357.766

Source: Drug Bank

Monoisotopic Molecular Weight

357.068032587

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Drug Targets

Gene Description
GABRA1 (source: Drug Bank)
GABRA2 (source: Drug Bank)
GABRA3 (source: Drug Bank)
GABRA5 (source: Drug Bank)
GABRB1 (source: Drug Bank)
GABRB2 (source: Drug Bank)
GABRB3 (source: Drug Bank)
GABRD (source: Drug Bank)
GABRE (source: Drug Bank)
GABRG1 (source: Drug Bank)
GABRG2 (source: Drug Bank)
GABRG3 (source: Drug Bank)
GABRP (source: Drug Bank)
GABRR1 (source: Drug Bank)
GABRR2 (source: Drug Bank)
GABRR3 (source: Drug Bank)
TSPO (source: Drug Bank)

Drug Interactions

Drug Description
cinolazepam Increased risk of toxicity (source: Drug Bank)
cinolazepam Increased risk of toxicity (source: Drug Bank)
No related diseases are available

Publications related to cinolazepam: 4

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The benzodiazepine site of the GABAA receptor: an old target with new potential?. Sleep medicine. 2004. Bateson Alan N. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Mapping of the benzodiazepine recognition site on GABA(A) receptors. Current topics in medicinal chemistry. 2002. Sigel Erwin. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
New insights into the role of the GABA(A)-benzodiazepine receptor in psychiatric disorder. The British journal of psychiatry : the journal of mental science. 2001. Nutt D J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The benzodiazepine binding site of GABAA receptors. Trends in pharmacological sciences. 1997. Sigel E, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB01594
ChEBI:
59514
PubChem Compound:
3033621
PubChem Substance:
10047721
46508803
ChemSpider:
2298251
Therapeutic Targets Database:
DAP001250

Clinical Trials

These are trials that mention cinolazepam and are related to either pharmacogenetics or pharmacogenomics.

Common Searches

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.