Dihydrocodeine 60 mg tablets

Product Beschrijving

Dihydrocodeine 60 mg oral tablets deliver a semi-synthetic morphinan opioid analgesic designed for the continuous management of moderate to severe pain refractory to non-opioid therapies. Frequently utilized in oncological palliative care, severe musculoskeletal disorders, and post-operative recovery, this 60 mg modified-release formulation provides consistent 12-hour analgesia positioned clinically between weak opioids (such as codeine) and strong $\mu$-agonists (such as morphine or oxycodone).

Clinical Profile & Physical Properties

• Active Ingredient: Dihydrocodeine tartrate (60 mg per tablet).

• Dosage Form: Typically manufactured as a modified-release / continuous-release matrix tablet (e.g., round, off-white to pale yellow, debossed with identifiers such as “DHC 60”) engineered to provide steady systemic absorption.

• Mechanism of Action: Acts as an agonist at central and spinal $\mu$-opioid receptors ($\text{MOR}$). A significant portion of its analgesic efficacy is mediated through O-demethylation into dihydromorphine, which displays roughly 100-fold higher affinity for $\mu$-receptors than the parent drug. Receptor activation triggers inhibitory $G_i$-protein signaling, decreasing intracellular cyclic AMP, closing voltage-gated calcium channels, and stimulating potassium efflux to attenuate nociceptive neurotransmission.

Pharmacokinetics & Metabolism

• Bioavailability & Absorption: Well absorbed via the gastrointestinal tract with an oral bioavailability of approximately 20% due to first-pass hepatic metabolism. Modified-release tablets flatten peak-to-trough plasma variations over a 12-hour dosing interval.

• Hepatic Biotransformation: Extensively metabolized in the liver via three primary pathways:

  • Glucuronidation to dihydrocodeine-6-glucuronide (predominant pathway).

  • $N$-demethylation via CYP3A4 to nordihydrocodeine.

  • $O$-demethylation via polymorphic CYP2D6 to the active metabolite dihydromorphine.

• Elimination: Excreted predominantly through the renal system as unchanged drug and polar conjugated metabolites, with an elimination half-life averaging 3.5 to 5 hours.

Prescribing Protocols & Administration

• Tablet Integrity: Modified-release tablets must be swallowed whole with water. Crushing, chewing, breaking, or dissolving the tablet destroys the polymer release matrix, precipitating rapid drug release (“dose dumping”) and acute systemic toxicity.

• Dose Individualization: Must be titrated to the minimum effective dose required to achieve clinical pain endpoints. Discontinuation after prolonged use requires a structured tapering schedule to avoid autonomic withdrawal symptoms.

Important Safety Information & Boxed Warnings

• Addiction, Abuse, and Misuse: Dihydrocodeine is a controlled substance with significant potential for psychological dependence, tolerance, misuse, and diversion.

• Life-Threatening Respiratory Depression: Serious, potentially fatal respiratory depression can occur, with highest susceptibility during initial therapy or following dosage increases.

• Risks with CNS Depressants & Alcohol: Concurrent administration with benzodiazepines, barbiturates, other sedatives, or alcohol significantly increases the risk of profound sedation, respiratory arrest, coma, and death.

• Contraindications: Contraindicated in patients with acute respiratory depression, severe obstructive pulmonary disease, acute asthma, or known paralytic ileus.