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Rotundine
Natural API
Rotundine.jpg
Stephania.jpg

Rotundine

Rotundine (CAS: 10097-84-4) is a tetrahydroisoquinoline alkaloid extracted from the roots of Stephania sinica (a member of the Menispermaceae family). As a natural medicine ingredient independently developed in China, it has dual analgesic and sedative effects, and is non addictive, widely used in the treatment of chronic pain and insomnia. In 2020, it was included in the list of urgently needed overseas new drugs in the Chinese Pharmacopoeia.

Product Name: Rotundine

IUPAC Name: (6S,12aR)-2,3,6,7,12,12a-Hexahydro-6-methyl-1H-[1,3]dioxolo[4',5':4,5]benzo[1,2-b]quinolizin-10-ol

CAS No.​: 10097-84-4

Molecular Formula: C₂₁H₂₅NO₄

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    Rotundine

    Basic information

    Product Name: Rotundine

    IUPAC Name: (6S,12aR)-2,3,6,7,12,12a-Hexahydro-6-methyl-1H-[1,3]dioxolo[4',5':4,5]benzo[1,2-b]quinolizin-10-ol

    CAS No.​: 10097-84-4

    Molecular Formula: C₂₁H₂₅NO₄

    Physicochemical Properties: 

    Parameter

    Value/Description

    ​Appearance​

    White powder

    ​Melting Point​

    140-143°C

    ​Solubility​

    Water solubility: 0.3 mg/mL (25°C); soluble in chloroform/methanol

    ​logP​

    2.8 (moderate lipophilicity)

    ​pKa​

    8.1 (phenolic OH), 9.3 (tertiary amine)

     Quality Standard: CP2020,JP,Customer Made

    Specification

    Test Items

    Standard

    Rotundine (CAS: 10097-84-4)

    98% by HPLC

    Loss on drying

    ≤5.0%

    Ash

    ≤0.1%

    Key Features

    index_10-7

    Natural Source

    Primarily found in Stephania sinica roots (content: 0.1-0.5%).
    index_10-7

    Dual Action

    Non-narcotic analgesia (potency: 1/10 of morphine) + sedative-hypnotic effects.
    index_10-7

    Regulatory Status

    Classified as a Category II psychoactive drug in China (prescription required) but not internationally controlled.

    Pharmacological Mechanisms

    1.Molecular Target Network

    Molecular Target Network

    2. Pharmacokinetics

    Absorption

    Oral bioavailability 35-45% (significant first-pass effect).

    Distribution

    Vd=5.2 L/kg; brain concentration 3× plasma levels.

    Metabolism

    Hepatic CYP2D6-mediated O-demethylation (active metabolite M1).

    Excretion

    Renal elimination predominates (90% clearance in 72 hours).

    Clinical Applications​

    Indications and Efficacy

    Condition​

    ​Regimen​

    ​Evidence​

    ​Chronic Headache​

    60 mg tid (oral)

    VAS score↓45%*

    ​Postoperative Pain​

    60-90 mg IM

    Morphine use↓30%

    ​Insomnia​

    30 mg at bedtime

    PSQI score↓50%

    *Multicenter RCT (n=320)

    Special Populations​

    Hepatic Impairment: Reduce dose by 50% (Child-Pugh B).

    Elderly: Start with half dose (fall risk).

    Dosage and Administration

    Formulations​

    Tablets: 30 mg (standard); 60 mg (extended-release).

    Injection: 60 mg/2 mL (IM only).

    Dosing Guidelines​

    ​Use​

    ​Dose​

    ​Notes​

    Chronic Pain

    30-60 mg tid

    Max 7 days

    Acute Pain

    60 mg IM q6h

    ≤240 mg/day

    Insomnia

    30-60 mg hs

    Avoid alcohol

    Safety Evaluation

    Adverse Reactions​

    ​System​

    ​Incidence​

    ​Management​

    Neurological

    12%

    Drowsiness (reduce dose)

    Gastrointestinal

    5%

    Nausea (take with food)

    Cardiovascular

    <1%

    Orthostatic hypotension

    Contraindications & Interactions​

    Absolute Contraindications:
    Myasthenia gravis (worsens muscle relaxation).
    Pregnancy (teratogenic in animals).

    Caution with:
    CYP2D6 inhibitors (e.g., fluoxetine): AUC↑60%.
    CNS depressants (e.g., benzodiazepines): Synergistic sedation.

    Research Progress Green max

    Novel Formulations​

    Transdermal Patch: Steady plasma levels for 24 hours (Phase II).

    Nasal Spray: Bioavailability ↑75% (for migraine rescue).

    New Indications​

    Fibromyalgia: Modulates central sensitization (Phase II).

    Opioid Withdrawal: Reduces anxiety/pain (preclinical promise).

    Stephania

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