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Ethanol

J01 - Antibacterials for systemic use Small molecule approved 1982 Parenteral Topical Natural product

JFDA label: JECEPT Ethanol 76%

Mechanism of Action

When used to treat ethylene glycol or methanol toxicity, ethyl alcohol competitively inhibits alcohol dehydrogenase, an enzyme which catalyzes the metabolism of ethylene glycol and methanol to their toxic metabolites. In neurolysis, alcohol will destroy nerves at the site of injection.

Indications

Off-label

  • Ethylene glycol overdose (antidote)
  • Hypertrophic obstructive cardiomyopathy (HOCM) (septal ablation)
  • Methanol overdose (antidote)

Contraindications

Source: Lexicomp

  • Hypersensitivity to ethyl alcohol or any component of the formulation Absolute
  • pregnancy (prolonged use or high doses at term) Absolute
  • seizure disorder and diabetic coma Absolute
  • subarachnoid injection of dehydrated alcohol in patients receiving anticoagulants Absolute

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Cardiac disorders (3)

Not Known Flushing · hypotension · phlebitis

Nervous system disorders (12)

Not Known Agitation · alcohol intoxication · brain disease · central nervous system depression · coma · disorientation · drowsiness · headache · neuropathy · sedation · seizure (rare) · vertigo

Renal and urinary disorders (2)

Not Known Polyuria · Urinary retention

Metabolism and nutrition disorders (1)

Not Known Hypoglycemia

Gastrointestinal disorders (3)

Not Known Gastric irritation · nausea · vomiting

General disorders and administration site conditions (1)

Not Known Tissue damage

Dosing

Source: Lexicomp

Antiseptic: Liquid denatured alcohol: Topical: Apply 1-3 times/day as needed Therapeutic neurolysis (nerve or ganglion block): Dehydrated alcohol injection 98%: Intraneural: Dosage variable depending upon the site of injection (eg, trigeminal neuralgia: 0.05-0.5 mL as a single injection per interspace vs subarachnoid injection: 0.5-1 mL as a single injection per interspace); single doses >1.5 mL are seldom required. Note: Administer when pain is from malignant origin only. Replenishment of fluid and carbohydrate calories: Dehydrated alcohol infusion: Alcohol 5% and dextrose 5%: 1-2 L/day by slow infusion Septal ablation for HOCM (off-label use) (Maron, 2003; Sorajja, 2012): Intracoronary (via balloon catheter): Dosage variable depending on septal anatomy and rate of contrast wash-out: 1-3 mL of at least 95% concentration infused slowly into septal perforator. Note: Smaller amounts may reduce the size of the septal infarct and incidence of complications (eg, complete heart block). Treatment of methanol or ethylene glycol overdose (off-label use) (Barceloux 1999; Barceloux 2002): Note: IV administration is the preferred route; continue therapy until ethylene glycol and/or methanol is no longer detected or levels are and the patient is asymptomatic and metabolic acidosis has been corrected. If ethylene glycol and/or methanol levels are not available in a timely manner, continue therapy until the estimated time of clearance of ethylene glycol and/or methanol has elapsed and the patient is asymptomatic with a normal pH. If patient has coingested ethanol, measure the baseline serum ethanol concentration and adjust the ethyl alcohol loading dose based on results to achieve a serum ethanol level of ~100 mg/dL. Absolute ethyl alcohol [98% (196 proof) = 77.4 g EtOH/dL]: IV: Note: Contact the Poison Control Center for options related to compounding IV ethanol. Initial: 600-700 mg/kg [equivalent to 7.6-8.9 mL/kg using a 10% solution] Maintenance: Goal of therapy is to maintain serum ethanol levels >100 mg/dL. Nondrinker: 66 mg/kg/hour [equivalent to 0.83 mL/kg/hour using a 10% solution] Chronic drinker: 154 mg/kg/hour [equivalent to 1.96 mL/kg/hour using a 10% solution] Dosage adjustment for hemodialysis: Maintenance dose: Nondrinker: 169 mg/kg/hour [equivalent to 2.13 mL/kg/hour using a 10% solution] Chronic drinker: 257 mg/kg/hour [equivalent to 3.26 mL/kg/hour using a 10% solution] Oral: Note: Solution must be diluted to a ≤20% concentration (to reduce the risk of gastritis) with water or juice and administered orally or via a nasogastric tube. Due to the pharmacokinetics of alcohol (ethyl) it is critical that oral ethanol be administered precisely at 60-minute intervals. Initial: 600-700 mg/kg [equivalent to 0.78-0.9 mL/kg using a 98% solution] Maintenance: Goal of therapy is to maintain serum ethanol levels >100 mg/dL Nondrinker: 66 mg/kg/hour [equivalent to 0.09 mL/kg/hour using a 98% solution] Chronic drinker: 154 mg/kg/hour [equivalent to 0.20 mL/kg/
(For additional information see "Ethanol (topical and injection): Pediatric drug information") Antiseptic: Liquid denatured alcohol: Refer to adult dosing. Treatment of methanol or ethylene glycol overdose (off-label use) (Barceloux 1999; Barceloux 2002): Refer to adult dosing.
Refer to adult dosing.
Treatment of methanol or ethylene glycol overdose (off-label use; Barceloux 1999; Barceloux 2002): Absolute ethyl alcohol: Dosage adjustment for hemodialysis: Maintenance dose: IV: Nondrinker: 169 mg/kg/hour [equivalent to 2.13 mL/kg/hour using a 10% solution] Chronic drinker: 257 mg/kg/hour [equivalent to 3.26 mL/kg/hour using a 10% solution] Oral: Nondrinker: 169 mg/kg/hour [equivalent to 0.22 mL/kg/hour using a 98% solution] Chronic drinker: 257 mg/kg/hour [equivalent to 0.33 mL/kg/hour using a 98% solution]

Warnings & Precautions

Source: Lexicomp

Diabetes

Use with caution in patients with diabetes mellitus; ethyl alcohol may decrease blood sugar.

Gout

Use with caution in patients with gout.

Hepatic impairment

Use with caution in patients with hepatic impairment.

Shock

Use with caution in patients with shock. Special populations:

Cranial surgery

Use with caution in patients following cranial surgery.

Infants

Minimize dermal exposure of ethyl alcohol in infants as significant systemic absorption and toxicity can occur. Ethyl alcohol passes freely into breast milk at a level approximately equivalent to maternal serum level.

Pregnancy

Use with caution in pregnant women with anticipated postpartum hemorrhage. Other warnings/precautions:

Administration

Proper positioning of the patient for neurolytic administration is essential to control localization of the injection of dehydrated alcohol (which is hypobaric) into the subarachnoid space; avoid extravasation. Not for SubQ administration. Do not administer simultaneously with blood due to the possibility of pseudoagglutination or hemolysis; may potentiate severe hypoprothrombic bleeding. Avoid extravasation during IV administration.

Appropriate use

When used as a topical antiseptic, improper use may lead to product contamination. Although infrequent, product contamination has been associated with reports of localized and systemic infections. To reduce the risk of infection, ensure antiseptic products are used according to the labeled instructions; avoid diluting products after opening; and apply single-use containers only one time to one patient and discard any unused solution (FDA Drug Safety Communication, 2013).

Monitoring

Clinical evaluation and periodic lab determinations, including serum ethanol levels, are necessary to monitor effectiveness, changes in electrolyte concentrations, and acid-base balance (when used as an antidote). Monitor blood glucose closely, particularly in children as treatment of ingestions is associated with hypoglycemia.

Proper storage

Flammable liquid and should be kept cool and away from any heat source.

Pregnancy & Lactation

Pregnancy

FDA category C Teratogenic

Animal reproduction studies have not been conducted with alcohol injection. Ethanol crosses the placenta, enters the fetal circulation, and has teratogenic effects in humans (AAP 2000; Barceloux 1999). The following withdrawal symptoms have been noted in the neonate following maternal ethanol consumption during pregnancy: Crying, hyperactivity, irritability, poor suck, tremors, seizures, poor sleeping pattern, hyperphagia, and diaphoresis (Hudak 2014). Fetal alcohol syndrome (FAS) is a term referring to a combination of physical, behavioral, and cognitive abnormalities resulting from ethanol exposure during fetal development. Since a "safe" amount of ethanol consumption during pregnancy has not been determined, the AAP recommends those women who are pregnant or planning a pregnancy refrain from all ethanol intake (AAP 2000). When used as an antidote during the second or third trimester, FAS is not likely to occur due to the short treatment period; use during the first trimester is cont

Lactation

Avoid

Ethanol is excreted in breast milk in concentrations similar to maternal blood concentrations (Koren 2002). Milk production may be decreased and adverse events to the nursing infant may occur (eg, sleep disturbances, impaired motor development or postnatal growth) (Sachs 2013). The actual clearance of ethanol from breast milk is dependent upon the mother's weight and amount of ethanol consumed (Koren 2002). Guidelines recommend to avoid drinking completely, or limit intake to the equivalent of e

Monitoring

Clinical pearlAntidotal therapy: Blood ethanol levels every 1-2 hours until steady state, then every 2-4 hours; blood glucose, electrolytes (including serum magnesium), arterial pH, blood gases, methanol or ethylene glycol blood levels; heart rate, blood pressure

Chemistry & Properties

2D structure
FormulaC2H6O
Molecular weight46.07 g/mol
IUPAC nameethanol
CAS64-17-5
PubChem CID702
InChIKeyLFQSCWFLJHTTHZ-UHFFFAOYSA-N
logP0.0 (XLogP -0.1)
Polar surface area20.23 Ų
H-bond acceptors / donors1 / 1
Drug-likeness (QED)0.41
Lipinski violations0
SMILESCCO

Biology & Pharmacokinetics

Pharmacokinetics

BBB penetrantYes (logBB -0.2)

Enzyme interactions

EnzymeRoleDetail
CYP1A2Substrate
CYP2B6Inhibitor
CYP2B6Substrate
CYP2C19Substrate
CYP2D6Substrate
CYP3A4Substrate

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Drug–drug interactions (100+, DDInter)

Interacting drugSeverityManagement
Acetaminophen major
Acitretin major
Amobarbital major
Benznidazole major
Buprenorphine major
Butabarbital major
Butalbital major
Cycloserine major
Dextropropoxyphene major
Disulfiram major
Droperidol major
Eluxadoline major
Ethionamide major
Flibanserin major
Fomepizole major
Hydrocodone major
Hydromorphone major
Leflunomide major
Levacetylmethadol major
Lomitapide major
Metformin major
Methohexital major
Methylphenobarbital major
Metronidazole major
Mipomersen major
Morphine major
Nifurtimox major
Pentobarbital major
Pexidartinib major
Phenobarbital major
Primidone major
Secobarbital major
Sodium oxybate major
Teriflunomide major
Thiopental major
Acarbose moderate
Acebutolol moderate
Acetohexamide moderate
Acetylsalicylic acid moderate
Acrivastine moderate

Showing 40 of 100+.

Registered Products (5)

BrandForm / strengthPackAgentCitizen (JOD)
JECEPT Ethanol Solution 76 % 250 ml pack varies الشـــــــــــــركــة الاردنية المصرية لصناعة منتجات البحر الميت
JECEPT Ethanol Solution 76 % 200 ml pack varies الشـــــــــــــركــة الاردنية المصرية لصناعة منتجات البحر الميت
JECEPT Ethanol Tablet 76 % 1 l pack varies الشـــــــــــــركــة الاردنية المصرية لصناعة منتجات البحر الميت
JECEPT Ethanol Tablet 76 % 4 l pack varies الشـــــــــــــركــة الاردنية المصرية لصناعة منتجات البحر الميت
JECEPT Ethanol Solution 76 % 50 ml pack varies الشـــــــــــــركــة الاردنية المصرية لصناعة منتجات البحر الميت