Paraldehyde


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intramuscular
Seizure
Adult: For cases associated with tetanus, status epilepticus, or poisoning: 5-10 mL via deep inj into the buttocks. Do not give >5 mL/inj site.
Child: For cases associated with status epilepticus: 0.1-0.15 mL/kg 4-8 hourly via deep inj into the buttocks. Do not give >5 mL/inj site.

Intramuscular
Alcohol withdrawal syndrome
Adult: For the management of acute agitation or delirium tremens: 5 mL 4-6 hourly for 24 hours (max: 30 mL on day 1); then 6 hourly thereafter (max: 20 mL/day). Doses are to be given via deep inj into the buttocks. Do not give >5 mL/inj site.

Intramuscular
Hypnotic
Adult: 10 mL via deep inj into the buttocks. Do not give >5 mL/inj site.
Child: 0.3 mL/kg daily via deep inj into the buttocks. Do not give >5 mL/inj site.

Intramuscular
Sedation
Adult: 5 mL via deep inj into the buttocks. Do not give >5 mL/inj site.
Child: 0.15 mL/kg daily via deep inj into the buttocks. Do not give >5 mL/inj site.
Suy gan
Severe: Contraindicated
Tương kỵ
Incompatible with plastic or rubber.
Chống chỉ định
Bronchopulmonary disease. Severe hepatic impairment. Pregnancy. Concomitant administration with other CNS depressants.
Thận trọng
Patient with CV disease, respiratory disease (e.g. asthma); history of drug abuse or acute alcoholism. Not for use as obstetric anaesthesia. For use as an alternative agent when conventional therapy is unavailable, ineffective, or inappropriate. For short-term use only (as hypnotic or sedative). Avoid abrupt withdrawal. Avoid injecting near nerve trunks; may cause severe and permanent nerve damage. Use glass syringes for administration. Mild to moderate hepatic impairment. Children. Lactation.
Tác dụng không mong muốn
Significant: CNS depression, metabolic acidosis. If prolonged use: Nephrosis, toxic hepatitis, tolerance, psychological and physical dependence.
General disorders and administration site conditions: Inj site reaction (e.g. extreme pain, sterile skin abscess, skin sloughing, fat necrosis, muscular irritation, nerve damage [including permanent damage]).
Musculoskeletal and connective tissue disorders: Muscle cramps.
Nervous system disorders: Dizziness, tremor.
Skin and subcutaneous tissue disorders: Rash, diaphoresis.
Potentially Fatal: Corrosive poisoning (administration of decomposed solution).
Thông tin tư vấn bệnh nhân
Avoid contact with eyes, skin and clothing. This drug may cause drowsiness, if affected, do not drive or operate machinery.
Chỉ số theo dõi
Evaluate pregnancy status before initiating therapy.
Quá liều
Symptoms: Short and troubled, rapid breathing; cloudy urine, reduced urination, slow heartbeat, general weakness, odour of the drug on the breath, severe hypotension, metabolic acidosis (with increased anion gap), respiratory depression, pulmonary oedema, impaired renal function (e.g. azotaemia, albuminuria, oliguria), nephrosis, fatty changes in the kidneys or liver, toxic hepatitis, cardiac failure and coma. Management: Symptomatic and supportive treatment. Maintain adequate airway, control respiration and administer oxygen to re-establish adequate respiratory exchange. Administer IV Na bicarbonate or Na lactate to correct metabolic acidosis. Maintain body temperature and support circulation with IV fluids or vasopressors if needed.
Tương tác
May potentiate CNS depression with other CNS depressants (e.g. barbiturates); avoid concomitant use.
Tương tác với thức ăn
May potentiate CNS depression with alcohol.
Tác dụng
Description:
Mechanism of Action: Paraldehyde is a cyclic trimer of acetaldehyde with unknown mechanism of action. It is believed to cause CNS depression, including the ascending reticular activating system leading to hypnosis or sedation and anticonvulsant activity (in sub-hypnotic doses). In sub-anaesthetic doses, it has no analgesic activity and may produce delirium or excitement in the presence of pain.
Onset: Sedation or hypnosis: 5-15 minutes (IM).
Duration: 8 hours.
Pharmacokinetics:
Absorption: Rapidly absorbed from the injection site. Time to peak plasma concentration: within 20-60 minutes.
Distribution: Diffuses into the CSF. Crosses the placenta.
Metabolism: Metabolised (approx 80-90% of the dose) in the liver into acetaldehyde, then oxidised by aldehyde dehydrogenase into acetic acid and further metabolised into CO2 and water.
Excretion: Mainly via the lungs (as unchanged drug); urine (small amounts, as unchanged drug). Elimination half-life: Approx 3.5-9.5 hours.
Đặc tính

Chemical Structure Image
Paraldehyde

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 31264, Paraldehyde. https://pubchem.ncbi.nlm.nih.gov/compound/Paraldehyde. Accessed July 27, 2021.

Bảo quản
Store below 25°C. Do not refrigerate. Protect from light. May crystallise at approx 12°C; warm gently if crystallisation occurs. Use immediately upon opening; do not use if the solution has a brownish colour or has an odour of acetic acid. This is a hazardous drug. Follow applicable procedures for receiving, handling, administration, and disposal.
Phân loại MIMS
Thuốc chống co giật / Thuốc giải lo âu / Thuốc ngủ & thuốc an thần
Phân loại ATC
N05CC05 - paraldehyde ; Belongs to the class of aldehydes and derivatives. Used as hypnotics and sedatives.
Tài liệu tham khảo
Anon. Paraldehyde. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 21/06/2021.

Buckingham R (ed). Paraldehyde. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 21/06/2021.

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