PARALDEHYDE INJECTION BP

Paraldehyde

Source of information: Drugbank (External Link). Last updated on: 3rd July 18
*Trade Name used in the content below may not be the same as the HSA-registered product.

Active Ingredient / Synonyms

Paraldehyde | Paraldehyde |

Description

Paraldehyde is the cyclic trimer of acetaldehyde molecules. It was introduced into clinical practice in the UK by the Italian physician Vincenzo Cervello in 1882. It is a central nervous system depressant and was soon found to be an effective anticonvulsant, hypnotic and sedative. It was included in some cough medicines as an expectorant (though there is no known mechanism for this function beyond the placebo effect).

Indication

Paraldehyde was used historically as a sedative and hypnotic [A19735]. It has been used in the treatment of seizures as an anticonvulsant [A19736].

Mechanism of Action

Paraldehyde is believed to reduce the release of acetylcholine in response to neuronal depolarization [A19737]. The exact mechanism of this effect is unknown.

Pharmacodynamics

Paraldehyde blocks neuromuscular transmission [A19737].

Pharmacokinetics

Absorption:

93% of orally administered paraldehyde is absorbed from the gastrointestinal tract.

Distribution:

Not Available

Metabolism:

Paraldehyde is believed to undergo depolymerization to acetaldehyde followed by oxidation by aldehyde dehydrogenase [A19378]. It is thought to ultimately be metabolized to carbon dioxide and water.

Elimination:

70-80% is metabolized to carbon dioxide and subsequently exhaled [A19738]. 11-28% is exhaled as the parent compound. 0.1-2.5% is excreted in the urine as the parent compound.

Half-life

The mean half life is 7.5 hours in a range if 3.5-9.5 hours [A19738].

Clearance

Not Available

Toxicity

Paraldehyde overdosage can produce headache, nausea, drowsiness, unconsciousness, coma, severe hypotension, respiratory depression, pulmonary edema and hemorrhages, and right-side heart failure [A19738]. Inhalation of paraldehyde can produce sore throat, headache, dizziness, nausea, drowsiness and unconsciousness but exposure via this route is rare. Chronic use is dependence forming and withdrawal proceeds similarly to ethanol withdrawal producing hallucinations and convulsions. Toxic hepatitis and nephritis have been observed during chronic use. The acute LD50 values determined for various species are as follows [A19738]: Rabbit - 3.3-5 g/kg (oral) Rat - 1.5-1.65 g/kg (oral), 1.3-1.45 g/kg (i.p.) Dog - 3-4 g/kg (oral) Mouse - 2.75 (oral) Cat - 3.3 (oral)

References

  1. Health Science Authority of Singapore - Reclassified POM
  2. Drugbank

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Approval Information

PARALDEHYDE INJECTION BP was registered with Health Science Authority of Singapore by NOVEM PHARMA PTE LTD. It is marketed with the registration number of SIN00325P with effective from 1988-04-22.

This product contains 5ml/ampoule of Paraldehyde in the form of INJECTION.

The medicine was manufactured by HOSPIRA AUSTRALIA PTY LTD in AUSTRALIA

It is a Presciption Only Medicine which can only be obtained from a doctor or a dentist, or from a pharmacist with a prescription from a Singapore-registered doctor or dentist.

Anatomical Therapeutic Chemical (ATC) Classification

ATC Code: N05CC05

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