Nalodeine

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An opioid analgesic drug


Nalodeine
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Nalodeine is an opioid analgesic drug that is derived from codeine. It is used primarily for its pain-relieving properties. Nalodeine is a semi-synthetic opioid, meaning it is chemically modified from naturally occurring opiates found in the opium poppy.

Chemical Structure and Properties

Chemical structure of Nalodeine

Nalodeine has the chemical formula C18H21NO3 and a molecular weight of 299.37 g/mol. It is structurally similar to codeine, with the primary difference being the presence of a methoxy group at the 3-position of the morphinan skeleton. This modification affects its pharmacological activity and potency.

Pharmacology

Nalodeine acts on the central nervous system by binding to opioid receptors, which are part of the body's natural pain control system. It primarily targets the mu-opioid receptor, which is responsible for its analgesic effects. The drug's action at these receptors leads to a decrease in the perception of pain, an increase in pain tolerance, and, in some cases, a sense of euphoria.

Metabolism

Nalodeine is metabolized in the liver by the cytochrome P450 enzyme system. It undergoes O-demethylation to produce active metabolites, which contribute to its analgesic effects. The metabolites are then excreted by the kidneys.

Medical Uses

Nalodeine is used in the management of moderate to severe pain. It is often prescribed when other pain relief measures are insufficient. Due to its potential for addiction and abuse, its use is typically limited to short-term management of pain.

Side Effects

Common side effects of Nalodeine include nausea, vomiting, constipation, drowsiness, and dizziness. More serious side effects can include respiratory depression, hypotension, and allergic reactions.

Legal Status

The legal status of Nalodeine varies by country. In many jurisdictions, it is classified as a controlled substance due to its potential for abuse and dependence. Prescriptions are typically required for its use.

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Contributors: Prab R. Tumpati, MD