Cryptenamine

Identification

Generic Name
Cryptenamine
DrugBank Accession Number
DB00785
Background

Cryptenamine is a mixture of closely related hypotensive alkaloids from Veratrum album (Liliaceae). It has been used in the treatment of hypertension but has largely been replaced by drugs with fewer adverse effects. Cryptenamine has a marked and re-producible depressor effect when given intravenously to hypertensive patients, however the mechanism of action is not known.

Type
Small Molecule
Groups
Approved
Synonyms
Not Available

Pharmacology

Indication

For the treatment of hypertension.

Pharmacology
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Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Cryptenamine is a mixture of closely related hypotensive alkaloids from Veratrum album (Liliaceae). It has been used in the treatment of hypertension but has largely been replaced by drugs with fewer adverse effects.

Mechanism of action

Cryptenamine has a marked and re-producible depressor effect when given intravenously to hypertensive patients, however the mechanism of action is not known. Some evidence has suggested that cryptenamine acts in a similar fashion to atropine, which lowers the "rest and digest" activity of all muscles and glands regulated by the parasympathetic nervous system. This occurs because atropine is a competitive inhibitor of the muscarinic acetylcholine receptors (acetylcholine is the neurotransmitter used by the parasympathetic nervous system). Therefore muscarinic acetylcholine receptors will be listed as experimental targets for cryptenamine.

TargetActionsOrganism
AMuscarinic acetylcholine receptor M2
antagonist
Humans
UBeta adrenergic receptor
inhibitor
potentiator
Humans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AcebutololAcebutolol may increase the hypotensive activities of Cryptenamine.
AceclofenacThe therapeutic efficacy of Cryptenamine can be decreased when used in combination with Aceclofenac.
AcemetacinThe therapeutic efficacy of Cryptenamine can be decreased when used in combination with Acemetacin.
Acetylsalicylic acidAcetylsalicylic acid may decrease the antihypertensive activities of Cryptenamine.
AlclofenacThe therapeutic efficacy of Cryptenamine can be decreased when used in combination with Alclofenac.
AldesleukinAldesleukin may increase the hypotensive activities of Cryptenamine.
AlfentanilAlfentanil may decrease the antihypertensive activities of Cryptenamine.
AlfuzosinAlfuzosin may increase the hypotensive activities of Cryptenamine.
AliskirenAliskiren may increase the hypotensive activities of Cryptenamine.
AlmotriptanAlmotriptan may decrease the antihypertensive activities of Cryptenamine.
Interactions
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Food Interactions
Not Available

Products

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International/Other Brands
Unitensen (MEDA AB)

Categories

Drug Categories
Classification
Not classified
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
QVO4N8484O
CAS number
1356-18-9
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

References

Synthesis Reference

Cavallito ,C.J.; US. Patent 2,789,977; April 23,1957; assigned to Innrin, Neisler and Company.

General References
Not Available
PubChem Substance
46507822
RxNav
42618
Therapeutic Targets Database
DAP000479
PharmGKB
PA164749510
Wikipedia
Cryptenamine

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

Pharmacoeconomics

Manufacturers
  • Medpointe pharmaceuticals medpointe healthcare inc
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
Not Available
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Drugtargets
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
G-protein coupled acetylcholine receptor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM2
Uniprot ID
P08172
Uniprot Name
Muscarinic acetylcholine receptor M2
Molecular Weight
51714.605 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Jandhyala ML, Buckley JP: Mechanisms of action of cryptenamine. J Pharm Sci. 1968 Sep;57(9):1576-82. [Article]
  4. Jandhyala BS, Buckley JP: Pharmacology and mechanism of action of cryptenamine. J Pharm Sci. 1966 Sep;55(9):888-93. [Article]
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Potentiator
Curator comments
Literature suggests that either potentiation or inhibition may be observed depending on location of receptor and organism studied.
General Function
Receptor signaling protein activity
Specific Function
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately e...

Components:
References
  1. Jandhyala ML, Buckley JP: Mechanisms of action of cryptenamine. J Pharm Sci. 1968 Sep;57(9):1576-82. [Article]

Drug created on June 13, 2005 13:24 / Updated on April 03, 2021 09:38