Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C18H22N2S.ClH |
| Molecular Weight | 334.907 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CC(CN(C)C)CN1C2=CC=CC=C2SC3=C1C=CC=C3
InChI
InChIKey=QUVSTPKPFAPBQU-UHFFFAOYSA-N
InChI=1S/C18H22N2S.ClH/c1-14(12-19(2)3)13-20-15-8-4-6-10-17(15)21-18-11-7-5-9-16(18)20;/h4-11,14H,12-13H2,1-3H3;1H
Trimeprazine (also known as Alimemazine), a phenothiazine used as antipsychotic drug. This drug is used in Russia under brand name TERALIGEN and has anti-histamine, sedative, and anti-emetic (anti-nausea) effects. Teraligen is used to treat neurosis, depression and anxiety of different origins. It prevents and relieves allergic conditions, which cause pruritus and urticaria by blocking histamine produced by the body during an allergic reaction. Trimeprazine competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding. Trimeprazine is not approved for use in humans in the United States. Nevertheless, combination of alimemazine and prednisolone (commonly sold under the brand name Temaril-P) is licensed as an antipruritic and antitussive in dogs.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL231 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | TERALIGEN Approved Useis a drug combining tranquilizing, vegetostabilizing, timoanaleptic, antihistamine and antispasmodic properties. Due to these properties Teraligen has a wide range of use. It is highly effective in treating mental, neurologic and somatic diseases such as neuroses of different origin, allergies, pruritus (itching) and urticaria. Teraligen is used to prevent and relieve allergic conditions as well as to treat sleep disorders. |
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| Primary | TERALIGEN Approved Useis a drug combining tranquilizing, vegetostabilizing, timoanaleptic, antihistamine and antispasmodic properties. Due to these properties Teraligen has a wide range of use. It is highly effective in treating mental, neurologic and somatic diseases such as neuroses of different origin, allergies, pruritus (itching) and urticaria. Teraligen is used to prevent and relieve allergic conditions as well as to treat sleep disorders. |
|||
| Primary | TERALIGEN Approved Useis a drug combining tranquilizing, vegetostabilizing, timoanaleptic, antihistamine and antispasmodic properties. Due to these properties Teraligen has a wide range of use. It is highly effective in treating mental, neurologic and somatic diseases such as neuroses of different origin, allergies, pruritus (itching) and urticaria. Teraligen is used to prevent and relieve allergic conditions as well as to treat sleep disorders. |
|||
| Primary | TERALIGEN Approved Useis a drug combining tranquilizing, vegetostabilizing, timoanaleptic, antihistamine and antispasmodic properties. Due to these properties Teraligen has a wide range of use. It is highly effective in treating mental, neurologic and somatic diseases such as neuroses of different origin, allergies, pruritus (itching) and urticaria. Teraligen is used to prevent and relieve allergic conditions as well as to treat sleep disorders. |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
0.357 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2255680/ |
3 mg/kg single, oral dose: 3 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
TRIMEPRAZINE plasma | Homo sapiens population: UNKNOWN age: CHILD sex: UNKNOWN food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
2758 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2255680/ |
3 mg/kg single, oral dose: 3 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
TRIMEPRAZINE plasma | Homo sapiens population: UNKNOWN age: CHILD sex: UNKNOWN food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
6.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2255680/ |
3 mg/kg single, oral dose: 3 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
TRIMEPRAZINE plasma | Homo sapiens population: UNKNOWN age: CHILD sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
80 mg 1 times / day multiple, oral Highest studied dose Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: pruritic dermatoses Age Group: adult Sex: M+F Population Size: 62 Sources: |
Disc. AE: Insomnia... AEs leading to discontinuation/dose reduction: Insomnia Sources: |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Insomnia | Disc. AE | 80 mg 1 times / day multiple, oral Highest studied dose Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: |
unhealthy, adult n = 62 Health Status: unhealthy Condition: pruritic dermatoses Age Group: adult Sex: M+F Population Size: 62 Sources: |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| weak | ||||
| yes | yes (co-administration study) Comment: A similar effect as for the CYP2D6 inhibitors was observed when aripiprazole was coadministered with alimemazine (TRIMEPRAZINE) |
Sample Use Guides
In Vivo Use Guide
Sources: http://rupharma.com/teraligen/
Teraligen is administrated orally 3-4 times a day. Hypnotic effect for adults: initial dose is 5-10 mg/day. Anxiolytic effect: initial dose is 60-80 mg/day. Antipsychotic effect: initial dose 200-400 mg/day.
Sedative effect for chidren: initial dose 2.5-5 mg/day
Symptomatic treatment of allergic reactions: initial dose 5-20 mg/day
Anxiolytic effect: initial dose 20-40 mg/day
Route of Administration:
Oral
Trimeprazine (TMP), a phenothiazine used as antipsychotic drug, was previously shown to induce a decrease in thyroid hormone serum levels in rats. Different mechanisms might be involved, mainly (i) a central mechanism, involving a reduction of thyroid-stimulating hormone (TSH) secretion; (ii) a peripheral mechanism, acting upon the synthesis of thyroid hormones, by inhibition of thyroperoxidase (TPO) or trapping of molecular iodine present in the thyroid gland. In vitro studies concerned TMP, and its three main metabolites: trimeprazine sulphoxide (TSO), N-desmethyl trimeprazine (NDT), and 3-hydroxy-trimeprazine (3-OHT). TMP and TSO expressed a high affinity for iodine in vitro, contrary to NDT, which did not complex iodine. Only 3-OHT inhibited TPO in vitro.
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1936-51-2
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100000127666
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ACTIVE MOIETY
SUBSTANCE RECORD
