Naloxone


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
Reversal of central depression from opioid use during surgery
Adult: As naloxone hydrochloride: 100-200 mcg, may give additional 100 mcg if necessary at 2-3 minute intervals until adequate response is obtained. Dose may be repeated within 1-2 hours depending on the dose, type and time interval of last opioid administration.
Child: As naloxone hydrochloride: 10-20 mcg/kg at 2-3 minute intervals until adequate response is obtained. May give additional dose if necessary at 1-2 hours interval depending on the dose, type and time interval of last opioid administration.

Intravenous
Opioid overdosage
Adult: As naloxone hydrochloride: 0.4-2 mg repeated if necessary at 2-3 minute intervals. If there is no response after a total of 10 mg has been given, consider the possibility of overdosage with other drugs.
Child: As naloxone hydrochloride: Initially, 10 mcg/kg followed by 100 mcg/kg , if necessary. Alternatively, may be given via IM inj, if IV admin is not possible.

Oral
Opioid dependence
Adult: As hydrochloride: 200 mg to 3 g daily.

Parenteral
Opioid-induced respiratory depression in neonates due to obstetric analgesia
Child: As naloxone hydrochloride: 10 mcg/kg via IV or IM inj, may be repeated at 2-3 minute intervals if necessary.
Hướng dẫn pha thuốc
Intravenous:
Opioid overdosage: Stable in 0.9% sodium chloride and 5% dextrose ing at 4 mcg/ml for 24 hr.
Reversal of central depression from opioid use dur...: Stable in 0.9% sodium chloride and 5% dextrose inj at 4 mcg/ml for 24 hr.
Parenteral:
Stable in 0.9% sodium chloride and 5% dextrose inj at 4 mcg/ml for 24 hr.
Tương kỵ
Preparations containing bisulfite, metabisulfite, long-chain or high-molecular wt anions, or solutions with an alkaline pH.
Thận trọng
Patients physically dependent on opioids, or who have received large doses of opioids (acute withdrawal syndrome may be precipitated). Pregnancy and lactation.
Tác dụng không mong muốn
Occur secondarily to reversal (withdrawal) of narcotic analgesia and sedation. Mental depression, apathy, inability to concentrate, sleepiness, irritability, anorexia, nausea, and vomiting in high oral doses during initial treatment of opiate addiction.
Potentially Fatal: Severe cardiopulmonary effects (e.g. hypotension, hypertension, ventricular tachycardia and fibrillation, dyspnoea, pulmonary oedema, cardiac arrest) in postoperative patients, most frequently in those with preexisting CV disease. Recurrence of respiratory depression in long-acting opioids.
IM/IV/Nasal/Parenteral/SC: C
Tương tác
Decreased effect of opioid analgesics.
Potentially Fatal: Acute withdrawal reaction in physically dependent patients may occur with opioid analgesics. Severe cardiopulmonary effects may occur with cardiotoxic drugs.
Tác dụng
Description:
Mechanism of Action: Naloxone is a pure opioid antagonist that acts competitively at opioid receptors.
Onset: 2 min (IV); 2-5 min (endotracheal, IM, SC).
Duration: 30-120 min depending on route; IV has a shorter duration than IM.
Pharmacokinetics:
Distribution: Crosses placenta.
Metabolism: Extensively hepatic via glucuronidation.
Excretion: Urine (as metabolites); elimination half-life: 0.5-1.5 hr (adult); 3-4 hr (neonates).
Bảo quản
Store at 25°C. Protect from light.
Phân loại MIMS
Thuốc giải độc & khử độc
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