Ativan Injection

— THERAPEUTIC CATEGORIES —
  • Anesthetics
  • Seizure disorders

Ativan Injection Generic Name & Formulations

General Description

Lorazepam 2mg/mL, 4mg/mL; soln for IV inj after dilution or IM inj; contains polyethylene glycol 400 in propylene glycol, benzyl alcohol.

Pharmacological Class

Benzodiazepine.

How Supplied

Single-use vials—10, 25; Multiple-dose vials (10mL)—10, 25

Manufacturer

Generic Availability

YES

Mechanism of Action

Lorazepam interacts with the γ-aminobutyric acid (GABA)-benzodiazepine receptor complex, which is widespread in the brain of humans as well as other species. This interaction is presumed to be responsible for lorazepam’s mechanism of action. Lorazepam exhibits relatively high and specific affinity for its recognition site but does not displace GABA. Attachment to the specific binding site enhances the affinity of GABA for its receptor site on the same receptor complex. The pharmacodynamic consequences of benzodiazepine agonist actions include antianxiety effects, sedation, and reduction of seizure activity.

Ativan Injection Indications

Indications

Preanesthetic to produce sedation, anxiety relief, and diminished recall of events related to surgery.

Ativan Injection Dosage and Administration

Adult

Individualize. ≥18yrs: IM: Give 2 hours prior to surgery. 0.05mg/kg, max 4mg. IV: Give 15–20 minutes prior to surgery. 0.044mg/kg or 2mg total, whichever is lower, may increase dose to 0.05mg/kg up to max 4mg if diminished recall of events related to surgery is desired; >50yrs: max IV dose of 0.044mg/kg or 2mg total, whichever is lower.

Children

<18yrs: not established.

Ativan Injection Contraindications

Contraindications

Acute narrow-angle glaucoma. Sleep apnea. Severe respiratory insufficiency (except as preanesthetic during mechanical ventilation). Intra-arterial injection. Premature infants.

Ativan Injection Boxed Warnings

Boxed Warning

Risks from concomitant use with opioids. Abuse, misuse, and addiction. Dependence and withdrawal reactions.

Ativan Injection Warnings/Precautions

Warnings/Precautions

Risks from concomitant use with opioids; see Interactions. Monitor for respiratory depression and level of sedation; ensure availability of resuscitative equipment for ventilatory support. Fall risk. Critically ill. Limited pulmonary reserve. Assess patient's risk for abuse, misuse, addiction prior to and during therapy. Avoid abrupt cessation. Drug or alcohol abuse. Hepatic or renal failure: not recommended; mild to moderate hepatic/renal disease: use with caution. Avoid extravasation. Outpatient endoscopy. Pediatric neurotoxicity. Elderly. Premature neonates/infants: gasping syndrome (due to benzyl alcohol content). Neonatal sedation and withdrawal syndrome; monitor neonates exposed during pregnancy or labor. Pregnancy (esp. late stage). Labor & delivery: not recommended. Nursing mothers: monitor infants.

Ativan Injection Pharmacokinetics

Absorption

IV: A 4mg dose provides an initial concentration of ~70 ng/mL. IM: Peak concentrations within 3 hours; a 4mg dose provides a Cmax of ~48 ng/mL.

Distribution

Plasma protein bound: 91±2%. Volume of distribution: ~1.3 L/kg.

Metabolism

Hepatic.

Elimination

Renal (88±4%), fecal (7±2%). Terminal half-life: 14±5 hours. 

Ativan Injection Interactions

Interactions

Increased sedation, respiratory depression, coma, and death with concomitant opioids; reserve use in those for whom alternative treatment options are inadequate; if needed, limit dosages/durations to minimum and monitor. Additive CNS effects with alcohol, phenothiazines, barbiturates, antidepressants, and MAOIs. Caution with concomitant scopolamine, loxapine, clozapine, haloperidol, or other CNS depressant drugs. May be antagonized by oral contraceptives (may need to increase lorazepam dose). May be potentiated by probenecid or valproate (reduce lorazepam dose by 50%).

Ativan Injection Adverse Reactions

Adverse Reactions

Respiratory depression/failure, hypotension, somnolence, headache, apnea, excessive sleepiness and drowsiness, inj site reaction, paradoxical reactions; withdrawal reactions.

Ativan Injection Clinical Trials

See Literature

Ativan Injection Note

Not Applicable

Ativan Injection Patient Counseling

See Literature

Ativan Injection Generic Name & Formulations

General Description

Lorazepam 2mg/mL, 4mg/mL; soln for IV inj after dilution or IM inj; contains polyethylene glycol 400 in propylene glycol, benzyl alcohol.

Pharmacological Class

Benzodiazepine.

How Supplied

Single-use vials—10, 25; Multiple-dose vials (10mL)—10, 25

Manufacturer

Generic Availability

YES

Mechanism of Action

Lorazepam interacts with the γ-aminobutyric acid (GABA)-benzodiazepine receptor complex, which is widespread in the brain of humans as well as other species. This interaction is presumed to be responsible for lorazepam’s mechanism of action. Lorazepam exhibits relatively high and specific affinity for its recognition site but does not displace GABA. Attachment to the specific binding site enhances the affinity of GABA for its receptor site on the same receptor complex. The pharmacodynamic consequences of benzodiazepine agonist actions include antianxiety effects, sedation, and reduction of seizure activity.

Ativan Injection Indications

Indications

Status epilepticus.

Ativan Injection Dosage and Administration

Adult

Individualize. ≥18yrs: Give by IV inj. 4mg at a rate of 2mg/min; may repeat dose once in 10–15 minutes if seizures continue or recur.

Children

<18yrs: not established.

Ativan Injection Contraindications

Contraindications

Acute narrow-angle glaucoma. Sleep apnea. Severe respiratory insufficiency (except as preanesthetic during mechanical ventilation). Intra-arterial injection. Premature infants.

Ativan Injection Boxed Warnings

Boxed Warning

Risks from concomitant use with opioids. Abuse, misuse, and addiction. Dependence and withdrawal reactions.

Ativan Injection Warnings/Precautions

Warnings/Precautions

Risks from concomitant use with opioids; see Interactions. Monitor for respiratory depression and level of sedation; ensure availability of resuscitative equipment for ventilatory support. Fall risk. Critically ill. Limited pulmonary reserve. Assess patient's risk for abuse, misuse, addiction prior to and during therapy. Avoid abrupt cessation. Drug or alcohol abuse. Hepatic or renal failure: not recommended; mild to moderate hepatic/renal disease: use with caution. Avoid extravasation. Outpatient endoscopy. Pediatric neurotoxicity. Elderly. Premature neonates/infants: gasping syndrome (due to benzyl alcohol content). Neonatal sedation and withdrawal syndrome; monitor neonates exposed during pregnancy or labor. Pregnancy (esp. late stage). Labor & delivery: not recommended. Nursing mothers: monitor infants.

Ativan Injection Pharmacokinetics

Absorption

IV: A 4mg dose provides an initial concentration of ~70 ng/mL. IM: Peak concentrations within 3 hours; a 4mg dose provides a Cmax of ~48 ng/mL.

Distribution

Plasma protein bound: 91±2%. Volume of distribution: ~1.3 L/kg.

Metabolism

Hepatic.

Elimination

Renal (88±4%), fecal (7±2%). Terminal half-life: 14±5 hours. 

Ativan Injection Interactions

Interactions

Increased sedation, respiratory depression, coma, and death with concomitant opioids; reserve use in those for whom alternative treatment options are inadequate; if needed, limit dosages/durations to minimum and monitor. Additive CNS effects with alcohol, phenothiazines, barbiturates, antidepressants, and MAOIs. Caution with concomitant scopolamine, loxapine, clozapine, haloperidol, or other CNS depressant drugs. May be antagonized by oral contraceptives (may need to increase lorazepam dose). May be potentiated by probenecid or valproate (reduce lorazepam dose by 50%).

Ativan Injection Adverse Reactions

Adverse Reactions

Respiratory depression/failure, hypotension, somnolence, headache, apnea, excessive sleepiness and drowsiness, inj site reaction, paradoxical reactions; withdrawal reactions.

Ativan Injection Clinical Trials

See Literature

Ativan Injection Note

Not Applicable

Ativan Injection Patient Counseling

See Literature