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thiamylal

Trade name: surital

Small moleculeapproved

Approved

Jul 9, 1954

Thiamylal is a barbiturate that is administered intravenously for the production of complete anesthesia of short duration, for the induction of general anesthesia, or for inducing a hypnotic state. Thiamylal, a barbiturate, is used in combination with acetaminophen or aspirin and caffeine for its sedative and relaxant effects in the treatment of tension headaches, migraines, and pain. Barbiturates act as nonselective depressants of the central nervous system (CNS), capable of producing all levels of CNS mood alteration from excitation to mild sedation, hypnosis, and deep coma. In sufficiently high therapeutic doses, barbiturates induce anesthesia. Thiamylal binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged. — NCATS

Clinical trial activity

0 trials · 0 clinical orgs · 1 marketing orgs

Phase 1
0
Phase 2
0
Phase 3
0
Phase 4
0

Timeline

1940s

  1. May 18, 1948

    Parke-Davis — First NDA Organization

  2. May 18, 1948

    Parke-Davis — NDA Organization

1950s

  1. Jul 9, 1954

    Earliest FDA Approval

  2. Jul 9, 1954

    Parke-Davis — Marketing Organization

Indications

Approved for

Mechanism of action

Approval history

  • approvedJul 9, 1954

Chemistry & pharmacology

Loading structure…

SMILES

C=CCC1(C(C)CCC)C(=O)NC(=S)NC1=O
Mol. weight
254.35 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Racemic Mixture
Inorganic
No
Polymer
No
Delivery
Parenteral
Availability
Discontinued

Oral

No

Parenteral

Yes

Topical

No

Sources

Also known as

  • 5-allyl-5-(1-methylbutyl)-2-thiobarbituric acid
  • 5-allyl-5-(1-methylbutyl)-2-thiobarbituric acid
  • 5-allyl-5-(1-methylbutyl)-2-thioxodihydro-4,6(1h,5h)-pyrimidinedione
  • 5-allyl-5-(1-methylbutyl)-2-thioxodihydro-4,6(1h,5h)-pyrimidinedione
  • 5-allyl-5-(1-methylbutyl)-2-thioxodihydropyrimidine-4,6(1h,5h)-dione
  • 5-allyl-5-(1-methylbutyl)-2-thioxodihydropyrimidine-4,6(1h,5h)-dione
  • dihydro-5-(1-methylbutyl)-5-(2-propenyl)-2-thioxo-4,6(1h,5h)-pyrimidinedione
  • dihydro-5-(1-methylbutyl)-5-(2-propenyl)-2-thioxo-4,6(1h,5h)-pyrimidinedione
  • surital
  • surital
  • surital
  • surital
  • thiamylal
  • thiamylal
  • thiamylal
  • thiamylal
  • thiamylal
  • thiamylal
  • thiamylal
  • thiamylal sodium
  • thiamylal sodium
  • thiamylal sodium
  • thiamylal sodium
  • thiamylal sodium
  • thiamylal sodium
  • thiamylal sodium
  • thiamylal sodium
  • thioquinalbarbitone
  • thioseconal
  • thioseconal
  • thioseconal

Organizations

Marketing (2)

OrganizationOrg typeRelationshipDate
Parke-DavisFor profitNDAMay 18, 1948
Parke-DavisFor profitMKTGJul 9, 1954