Dihydrocodeine

DEA NFLIS-Drug Category -> Narcotic Analgesics

DEA Schedule II Controlled Substance -> Opiates

Pharmaceuticals -> Used in Switzerland

Pharmaceuticals -> Synthetic Cannabinoids or Psychoactive Compounds

Pharmaceuticals -> Listed in ZINC15

Breast Feeding; Lactation; Milk, Human; Analgesics, Opioid; Narcotics; Antitussive Agents

Pharmaceuticals

Danger

H301+H311+H331 (90.7%): Toxic if swallowed, in contact with skin or if inhaled [Danger Acute toxicity, oral; acute toxicity, dermal; acute toxicity, inhalation]

P233, P260, P261, P262, P264, P270, P271, P272, P280, P284, P301+P316, P302+P352, P304+P340, P316, P321, P330, P333+P317, P342+P316, P361+P364, P362+P364, P403, P403+P233, P405, and P501 (click each P-code to see the statement)

Aggregated GHS information provided per 43 reports by companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

DEA schedule II controlled substance

REACH registered substance: Dihydrocodeine (EC: 204-732-3)

Drug-Induced Liver Injury Severity and Toxicity (DILIst)

Dihydrocodeine

DILI Positive

DOI:10.1016/j.drudis.2019.09.022

Dihydrocodeine

3.7

15.8

Dihydrocodeine bitartrate is given in combination with acetaminophen and caffeine in a capsule (as Trezix), with 16 mg dihydrocodeine bitartrate per capsule. The usual adult dosage is 2 Trezix capsules orally every 4 hours, as needed. No more than 5 doses, or 10 capsules should be taken in a 24-hour period.

N - Nervous system

QN - Nervous system

Metabolized in the liver by CYP 2D6 into an active metabolite, dihydromorphine, and by CYP 3A4 into secondary primary metabolite, nordihydrocodeine. A third primary metabolite is dihydrocodeine-6-glucuronide. [1] The time for mean peak concentration in acid metabolites is 1.76h and 1.98h for a 30 and 60mg dose, respectively. The concentrations achieved were 563 ug/1 and 1476 ug/1, respectively. [2]

Dihydrocodeine has known human metabolites that include Desmethyl dihydrocodeine and Paramorfan.

N9I9HDB855

DIHYDROCODEINE

Mechanisms of Action [MoA] - Full Opioid Agonists

Established Pharmacologic Class [EPC] - Opioid Agonist

Dihydrocodeine is an Opioid Agonist. The mechanism of action of dihydrocodeine is as a Full Opioid Agonist.

Bioavailability is low (approximately 20%) if administered orally. This may be due to poor gastrointestinal absorption. It is also likely due to pre-systemic metabolism by the liver and intestinal wall. [2] The AUCs after oral and intravenous administration are similar (3203ug/l/h and 3401ug/l/h, respectively). [2] Time to peak values are 1.6 and 1.8hours for a 30mg and 60mg dose, respectively. The concentrations achieved were 71.8 ug/1 and 146 ug/1, respectively. [2]