Benzodiazepine

Class Summary
This drug is used to control seizures. View full drug information

Diazepam (Valium)
Depresses all levels of CNS (eg, limbic and reticular formation), possibly by increasing GABA activity. View full drug information

Lorazepam (Ativan)
DOC for treatment of status epilepticus because persists in CNS longer than diazepam. Rate of injection not to exceed 2 mg/min. May be administered IM if IV access not available. View full drug information

Midazolam (Versed)
Alternative to terminate refractory status epilepticus. Because water soluble, takes approximately 3 times longer than diazepam to peak EEG effects. Wait 2-3 min to fully evaluate sedative effects before starting procedure or repeating dose. Has twice the affinity for benzodiazepine receptors than diazepam. May be administered IM if vascular access unavailable. Previous Proceed to Follow-up

Adult Dosing & Uses

Dosing Forms & Strengths
tablet: Schedule IV
2mg 5mg 10mg 5mg/5mL 5mg/mL

oral solution: Schedule IV

rectal solution: Schedule IV

5mg/mL 5mg/mL

injectable solution: Schedule IV

Anxiety
2-10 mg PO BID/QID OR 2-10 mg IV/IM q3-4hr; no more than 30 mg/8 hours

Alcohol Withdrawal
Initial: 10 mg IV, may give additional doses of 5-10 mg IV q1-4hr; if severe may give q2030min

Endoscopy
IV: Titrate dose with 10 mg or less immediately before procedure, not to exceed cumulative dose of 20 mg; reduce dose of narcotic by 1/3 or omit, OR IM: 5-10 mg 30 minutes before procedure

Pre-Op Sedation
10 mg IV 1-2 hours before surgery

Muscle Spasm
2-10 mg PO BID-QID OR 5-10 mg IV/IM q3-4hr PRN

Seizure Disorder
2-10 mg PO BID-QID OR 0.2 mg/kg PR, repeat after 4-12 hours PRN

Status Epilepticus
5-10 mg/dose IV/IM q10-15min; no more than 30 mg OR 0.5 mg/kg PR (using parenteral solution), THEN 0.25 mg/kg in 10 minutes PRN

Geriatric Dosing
2-2.5 mg PO qD or BID initially; increase gradually as needed Due to long-acting metabolite not considered a drug of choice in the elderly; associated with falls

Administration
PO: Dilute oral concentrate with water/juice/carbonated beverages or mix with semisolid foods PR: Gel or parenteral form can be used

Other Indications & Uses

Off-label: Atonic seizures, atypical absence seizures, infantile spasms, myoclonic epilepsy adjunct, neonatal abstinence syndrome, opioid withdrawal symptoms, panic disorder, sedation in pediatrics, tension headache, tremors Geriatric: Initiate with 2-2.5 mg PO qDay/BID; 2-5 mg IV x1, slowly increase if necessary

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Pediatric Dosing & Uses

Dosing Forms & Strengths
tablet: Schedule IV
2mg 5mg 10mg 5mg/5mL 5mg/mL 5mg/mL 5mg/mL

oral solution: Schedule IV

rectal solution: Schedule IV injectable solution: Schedule IV

Sedative/Muscle Relaxant
<6 months old: PO not recommended 0.04-0.2 mg/kg IV/IM q2-4hr; no more than 0.6 mg/kg within 8 hours, OR 0.12-0.8 mg/kg/day divided TID/QID PO

Status Epilepticus
IV
Neonate (<28 days old): 0.3-0.75 mg/kg IV q15-30min x2-3 doses (not firstline treatment because of benzyl alcohol content) >1 month old: 0.2-0.5 mg/kg IV q15-30min x2-3 doses No more than <5 years old: 5 mg; >5 years old: 10 mg 2-5 years old: 0.5 mg/kg; repeat in 4-12 hours PRN 6-11 years old: 0.3 mg/kg; repeat in 4-12 hours PRN >12 years old: 0.2 mg/kg; repeat in 4-12 hours PR PR (using IV form): As adult

PR

Administration
PO: Dilute oral concentrate with water/juice/carbonated beverages or mix with semisolid foods PR: Place patient on side facing you with upper leg bent forward, lubricate rectal applicator tip, gently instert syringe tip in rectum and slowly push plunger

Other Information
Potential toxic dose <6 years old: 0.5 mg/kg
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Drug Interactions
Interaction Checker diazepam and Type a dru

No Results

No Interactions Found Interactions Found Contraindicated Serious - Use Alternative Significant - Monitor Closely Minor Sort by :

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Adverse Effects
1-10%
Ataxia Euphoria (3%, rectal gel ) Incoordination (3%, rectal gel ) Somnolence Rash (3%, rectal gel )

Diarrhea (4%, rectal gel )

Frequency Not Defined

Common
Hypotension Fatigue Muscle weakness Respiratory depression Neutropenia Local Effects: pain, swelling, thrombophlebitis, carpal tunnel syndrome, tissue necrosis Phlebitis if too rapid IV push

Serious

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Contraindications & Cautions

Contraindications
Documented hypersensitivity Acute alcohol intoxication Myasthenia gravis (allowable in limited circumstances) Narrow angle glaucoma (questionable) Severe respiratory depression Depressed neuroses, psychotic reactions IV use in shock, coma, depressed respiration, patients who recently received other respiratory depressants Breastfeeding

Precautions
Use caution in COPD, sleep apnea, renal/hepatic disease, open-angle glaucoma (questionable), depression, suicide ideation May impair ability to perform hazardous tasks
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Pregnancy & Lactation

Pregnancy Category: D Lactation: Enters breast milk/contraindicated (AAP Committee states "of concern") Minor tranquilizers should be avoided in 1st trimester of pregnancy due to increased risk of congenital malformations Maternal use shortly before delivery is associated with floppy infant syndrome (good and consistent evidence) Prenatal benzodiazepine exposure slightly increased oral cleft risk (limited or inconsistent evidence) A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk. B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA:Information not available.
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Pharmacology
Half-Life: 20-70 hr (active metabolite) Onset: 15-45 min (PO, hypnotic action); 1-5 min (IV sedative action) Duration: PO (hypnotic action):7-8 hr; IV (sedative action); 15-60 min

Peak Plasma
Time: 30-90 min (PO), 5-90 min (PR) Concentration: 373 ng/mL (initial at 45 min); 447 ng/mL (second peak at 70 min)

Other Information
Bioavailability: 90% (PR) Protein Bound: 98% Vd: 0.8-1 L/kg Metabolism: hepatic P450 enzyme CYP2C19, CYP3A4

Metabolites: N-desmethyldiazepam, 3-hydroxdiazepam, oxazepam Renal Clearance: 20-30 mL/min Excretion: urine

Mechanism of Action
Modulates postsynaptic effects of GABA-A transmission, resulting in an increase in presynaptic inhibition. Appears to act on part of the limbic system, the thalamus, and hypothalamus, to induce a calming effect.
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IV & IM Information
IV Incompatibilities
Solution: D5W(?), Ringer's(?), LR(?), NS(?)-see preparation Additive: bleomycin, dobutamine, doxorubicin, floxacillin, fluorouracil, furosemide Syringe: doxapram, glycopyrrolate, heparin, hydromorphone, ketorolac(?), nalbuphine(?), ranitidine(?), sufentanil Y-site: amphotericin B cholesteryl SO4, atracurium, bivalirudin, cefepime, dexmedetomidine, diltiazem, fenoldopam, fluconazole, foscarnet, gatifloxacin, heparin, heparin/hydrocortisone, Hextend, hydromorphone, linezolid, meropenem, pancuronium, KCl, propofol, remifentanil(?), tirofiban, vecuronium, vit B/C Not specified: atropine, epinephrine, hydroxyzine, lidocaine, meperidine, morphine, norepinephrine, pentobarbital, Na bicarb

IV Compatibilities
Additive: netilmicin, verapamil Syringe: cimetidine Y-site: cisatracurium (may be incomp at higher conc), dobutamine, fentanyl, hydromorphone (may be incom at higher conc), methadone, morphine sulfate, nafcillin, quinidine, remifentanil (may be incomp at higher conc), sufentanil Not spec: aminophylline, cefazolin

IV Preparation
Compatibility w/ D5W, NS & Ringer's controversial. If infusion is selected, adding the infusion soln to diazepam injection (& not the other way around) may prevent precipitate formation.

IV Administration
Administer over 3 min no more than 5 mg/min Have airway support ready until effects of IV admin are known

Administer directly into a large vein to avoid thrombosis

If this is not feasible, give drug into tubing of a flowing IV soln as close as possible to vein insertion Do not use small veins such as those of wrist or dorsum of hand

Monitor resp's q5-15min and before each IV dose

Storage
Store intact vials at room temp; protect from light
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Dosing Forms & Strengths
tablet: Schedule IV
0.5mg 1mg 2mg 2mg/mL 2mg/mL

oral concentrate: Schedule IV injectable solution: Schedule IV

4mg/mL

Anxiety Disorders
Initial: 2-3 mg PO BID/TID PRN; not to exceed 10 mg/day Maintenance: 2-6 mg/day PO in divided BID/TID

Short-Term Treatment of Insomnia

2-4 mg PO qHS

Preoperative Sedation, Anxiety Relief, & Anterograde Amnesia

0.05 mg/kg IM for 1 dose; 2 hours before surgery; not to exceed 4 mg/dose (2 mg/dose in elderly) OR 0.044 mg/kg IV for 1 dose; 15-20 minutes before surgery; not to exceed 4 mg/dose; (2 mg/dose in elderly)

Status Epilepticus
Usual 4 mg/dose slow IV at a rate of 2 mg/min If seizure persists after 10-15 minutes, administer 4 mg IV again

Anxiolytic/Sedation in Intubated & Mechanically Ventilated Patients in Criticalcare Setting (Off-label)

0.02-0.06 mg/kg intermittent IV q2-6hr PRN OR 0.01-0.1 mg/kg/hr continuous IV

Chemotherapy-Induced Nausea/Vomiting (Off-label)

1-2.5 mg PO/IV 30 minutes prior to chemotherapy & q4hr PRN thereafter

Geriatric Dosing
Preferred agent in elderly because short-acting and has inactive metabolite When higher dose indicated, increase evening dose before daytime doses Anxiety Disorders
Lower initial dose recommended; 1-2 mg PO divided BID/TID Lower initial dose recommended; 0.5-1 mg PO qHS, increase PRN Initial daily dose should not exceed 2 mg to avoid oversedation

Insomnia

Other Information
Monitor: respirations q5-15min & before each repeated IV dose

Other Indications & Uses

Preanesthesia

Off-label
Oral: chronic insomnia Parenteral: delirium (in combination with haloperidol), EtOH withdrawal, psychogenic catatonia, muscle spasm

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Pediatric Dosing & Uses

Dosing Forms & Strengths
tablet: Schedule IV
0.5mg 1mg 2mg 2mg/mL 2mg/mL 4mg/mL

oral concentrate: Schedule IV injectable solution: Schedule IV

Status Epilepticus (Off-label)

Infants and children: 0.05-0.1 mg/kg IV over 2-5 minutes; not to exceed 4 mg/dose; may repeat q10-15min PRN Adolescents: 4 mg slow IV; if seizure persists after 10-15 minutes, administer 4 mg IV again

Anxiolytic/Sedation/Agitation (Off-label)
Children: 0.05 mg/kg/dose PO q4-8hr; not to exceed 2 mg/dose

Chemotherapy-Induced Nausea/Vomiting (Off-label)

Children: 0.05 mg/kg IV q6hr PRN; not to exceed 2 mg/dose

Other Information
Monitor: Respirations q5-15min & before each repeated IV dose
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Drug Interactions
Interaction Checker lorazepam and Type a dru

No Results

No Interactions Found Interactions Found Contraindicated Serious - Use Alternative Significant - Monitor Closely Minor Sort by :

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Adverse Effects
>10%
Sedation (16%)

1-10%
Dizziness (7%) Weakness (4.2%) Unsteadiness (3.4%)

Frequency Not Defined

Fatigue Drowsiness Amnesia Confusion Disorientation Depression Suicidal ideation/attempt Vertigo

Ataxia Sleep apnea Asthenia Extrapyramidal symptoms Respiratory depression Tremor Convulsions/seizures Visual disturbances Dysarthria Hypotension Blood dyscrasias Change in libido Impotence Jaundice Incr bilirubin Incr liver transaminases Incr in ALP Hypersensitivity reactions Nausea Constipation Change in appetite Paradoxical reactions (anxiety, excitation, agitation, hostility, aggression, rage)
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Contraindications & Cautions

Contraindications
Documented hypersensitivity Acute narrow angle glaucoma Intraarterial administration Severe respiratory depression

Sleep apnea Breast feeding

Cautions
Not recommended for use in patients with primary depressive disorder or psychosis Injection contains benzyl alcohol associated with potentially fatal "Gasping Syndrome" in neonates Prolonged use may lead to physical & psychological dependence; use caution in patients with history of suicide attempt or drug abuse Do not withdraw abruptly after prolonged use; terminate dosage gradually May cause CNS depression, impairing physical and mental abilities; caution patients to not operate dangerous machinery or motor vehicles Caution patients that tolerance for alcohol and other CNS depressants will be diminished Pregnancy (use only if no suitable alternatives)
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Pregnancy & Lactation

Pregnancy Category: D Lactation: Avoid if breastfeeding; excreted in human breast milk Risk of serious adverse effects, including CNS and respiratory depression, exist Minor tranquilizers should be avoided in 1st trimester of pregnancy due to increased risk of congenital malformations Maternal use shortly before delivery is associated with floppy infant syndrome (good and consistent evidence) Prenatal benzodiazepine exposure slightly increased oral cleft risk (limited or inconsistent evidence) A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk. B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA:Information not available.
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Pharmacology
Mechanism of Action
Sedative hypnotic with short onset of effects and relatively long half-life By increasing the action of gamma-aminobutyric acid (GABA), which is a major inhibitory neurotransmitter in the brain, may depress all levels of CNS, including limbic and reticular formation

Absorption
Bioavailability: 90% Onset: IV 1-5 min; IM 15-30 min Peak plasma time: 2 hr Peak plasma concentration: 20 ng/mL Duration: 12-24 hr (IV/IM)

Distribution
Protein Bound: 85%

Metabolism
Glucuronic acid conjugation Metabolites: inactive

Elimination
Half-Life: unconjugated lorazepam, 12hr; major metabolite lorazepam glucuronide, 18hr Excretion: Urine
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IV & IM Information
IV Incompatibilities
Additive: buprenorphine, dexamethasone sodium phosphate w/diphenhydramine & metoclopramide Syringe: sufentanil

Y-site: aldesleukin, aztreonam, floxacillin, foscarnet, idarubicin, imipenem/cilastatin, omeprazole, ondansetron, sargramostim, sufentanil

IV Preparation
Parenteral admixture stable for 24 hr at room temp (25C) Usually given IVP Standard IVP dilution: dilute immediately before use with equal amt of NS or SWI Usual dilution for cont infusion: 1 mg in 100 mL D5W Discard if discoloration or precipitate

IV/IM Administration
IM: administer deep into muscle mass IV: prior to use, dilute injection soln with an equal amount of compatible diluent (D5W, NS, SWFI) Administer IV inj slowly, directly into a vein or into tubing of a free-flowing compatible IV infusion (eg, NS, D5W), at NMT 2 mg/min
Validate patent venous cath w/ repeated aspiration during infusion to visualize venous blood return Inadvertent intra-arterial injection may produce arteriospasm resulting in gangrene potentially requiring amputation Rapid IV infusion may result in apnea, bradycardia, hypotension, cardiac arrest

Continuous infusion solutions should have an in-line filter & should be checked frequently for possible precipitation Emergency resuscitative equipment should be available when administering IV

Storage
IV/IM injection: Refrigerate intact vials at 2-8 C (36-46 F) & protect contents from light Tablets: Keep tightly closed; store at 25 C (77 F) Oral concentrate: Store at cold temperature; refrigerate at 2-8 C (36-46 F); discard open bottle after 90 days
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Adult Dosing & Uses

Dosing Forms & Strengths
oral syrup: Schedule IV
2mg/mL 1mg/mL 5mg/mL

injectable solution: Schedule IV

Sedation/Anxiolysis with Anterograde Amnesia

IM: 70-80 mcg/kg (~5 mg) 30-60 minutes before surgery (reduce 50% chronic ill or geriatric) IV
<60 years old: Initial usually 0.5-1 mg (no more than 2.5 mg) >60 years old: Debilitated or chronically ill: Initial no more than 1.5 mg; additional doses at no more than 1 mg/dose Repeat q2-3min PRN, usually no more than 5 mg (<60 years old & healthy), no more than 3.5 mg (>60 years old/ill) Maintenance: 25% of initial effective dose PRN by slow titration Reduce 30% if premedicated with opiate (50% in elderly/ill)

Anesthesia (Used with Other Components)

Induction
300-350 mcg/kg IV injection over 20-30 seconds (without premedication) 150-350 mcg/kg (with premedication)

Usually lower doses for >55 years old or debilitated 25% of induction dose PRN

Maintenance

Sedation of Intubated/Ventilated Patients

Load: 10-50 mcg/kg slow IV injection or infusion over several minutes, repeat q10-15min PRN Maintenance: Initial 20-100 mcg/kg/hr infusion, titrate up or down 25-50% PRN

Seizure Clusters (Orphan)

Rescue treatment of seizures in patients on stable AED regimens who require control of intermittent bouts of increased seizure activity (eg, acute repetitive seizures, seizure clusters) Administered by intranasal route Orphan indication sponsors
Upsher-Smith Laboratories, Inc. 6701 Evenstad Drive Maple Grove, MN 55369-6026 Schwarz Biosciences, Inc. 8010 Arco Corporate Drive Raleigh, NC 27617

Geriatric Dosing
Sedation/Anxiolysis with Anterograde Amnesia
IM: 1-3 mg (~35-40 mcg/kg) IM 30-60 minutes before surgery; some elderly patients may respond to as little as 1 mg; onset is 15 min (peaking at 30-60 minutes) IV (age >60 years): 1.5 mg IV initially; may repeat with 1 mg/dose IV q2-3 min PRN; not to exceed cumulative dose of 3.5 mg; peak effect may be delayed in elderly, so increments should be smaller and rate of injection slower IV Maintenance: 10-15% of initial effective dose PRN by slow titration Age >55 years: Decrease typical adult doses for induction and maintenance doses Induction in unpremedicated patients: 0.3 mg/kg IV; if severe systemic disease of other debilitation, decrease further to 0.15-0.25 mg/kg Induction in premedicated patients: As little as 0.15 mg/kg IV may suffice

Anesthesia (used with Other Components)

Other Information
Monitor: IV: Respiratory & cardiac function

Other Indications & Uses

Off-label: Seizure, status epilepticus
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Pediatric Dosing & Uses

Dosing Forms & Strengths
syrup: Schedule IV
2mg/mL 1mg/mL 5mg/mL

injectable solution: Schedule IV

Sedation
250-1000 mcg/kg PO x1 diluted by juice; no more than 20 mg IM: 100-150 mcg/kg, up to 500 mcg/kg, usually no more than 10 mg IV
6 months old-5 years old: Initial 50-100 mcg/kg IV over 2-3 minutes, repeat q2-3min PRN, usually no more than 6 mg 6-12 years old: Initial 25-50 mcg/kg IV over 2-3 minutes, repeat q2-3min PRN, usually no more than 10 mg

Sedation in Critical Care Settings

50-150 mcg/kg IV q1-2hr PRN 0.001-0.002 mg/kg/min IV infusion <32 weeks gestation: 0.0005 mg/kg/min IV infusion

Other Information
Monitor: IV: Respiratory & cardiac function
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Drug Interactions
Interaction Checker midazolam and Type a dru

No Results

No Interactions Found

Interactions Found Contraindicated Serious - Use Alternative Significant - Monitor Closely Minor Sort by :

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Adverse Effects
>10%
Decr respiratory rate (23%) Apnea (15%)

1-10%
Drowsiness (1-5%) Pediatric
Nystagmus (1-5%)

Frequency Not Defined

Headache Sedation Hiccoughs Nausea Vomiting Injection site reaction Coughing Pediatric
Desaturation Hypotension Seizure-like activity Paradoxical reactions

Hiccoughs Apnea

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Contraindications & Cautions

Black Box Warnings
Respiratory depression/arrest has been associated with use, especially when used for sedation in noncritical care settings. Respiratory depression, airway obstruction, desaturation, hypoxia, and apnea, particularly when used with concomitant CNS depressants (eg,opioids), have been reported. Should only be used in settings (eg hospital, ambulatory care settings, including physicians' or dentists' offices) that can provide continuous monitoring of respiratory and cardiac function. Immediate availability of resuscitative drugs and age- and size- appropriate equipment for ventilation and intubations and personnel trained in their use and skilled in airway management should be ensured. For deeply sedated patients, a dedicated individual other than the practitioner performing the procedure should monitor the patient throughout the procedure. Use of the 1 mg/mL formulation or dilution of the 1 mg/mL or 5 mg/mL formulation is recommended to facilitate slower injection. Adult Dosing: The initial intravenous dose for sedation in adult patients may be as little as 1 mg but should not exceed 2.5 mg in a normal healthy adult. Lower doses are necessary for older (>60 years) or debilitated patients and in patients receiving concomitant narcotics or other central nervous system (CNS) depressants. The initial dose and all subsequent doses should always be titrated slowly; administer over at least 2 minutes and allow an additional 2 or more minutes to fully evaluate the sedative effect. Pediatric Dosing: Doses of sedative medications in pediatric patients must be calculated on a mg/kg basis, and initial doses and all subsequent doses should always be titrated slowly. The initial pediatric dose of midazolam for sedation/anxiolysis/amnesia is age, procedure, and route dependent. Neonates: Midazolam should not be administered by rapid injection in the neonatal population. Severe hypotension and seizures have been reported following rapid IV administration, particularly with concomitant use of fentanyl.

Contraindications
Documented hypersensitivity Acute alcohol intoxication Myasthenia gravis (allowable in limited circumstances) Narrow angle glaucoma (questionable) Severe respiratory depression

Depressed neuroses, psychotic reactions IV use in shock, coma, depressed respiration, patients who recently received other respiratory depressants Not for intrathecal/epidural use due to benzyl alcohol

Cautions
Use caution in COPD, sleep apnea, renal/hepatic disease, open-angle glaucoma (questionable), depression, suicide ideation May impair ability to perform hazardous tasks Do not inject by rapid bolus to neonates or for sedation IV associated with risk of potentially fatal respiratory depression and arrest IV: Wait 2-3 min to evaluate sedation before repeating dose Have resuscitative drugs and equipment handy
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Pregnancy & Lactation

Pregnancy Category: D Lactation: distributed in breast milk, use caution Minor tranquilizers should be avoided in 1st trimester of pregnancy due to increased risk of congenital malformations Maternal use shortly before delivery is associated with floppy infant syndrome (good and consistent evidence) Prenatal benzodiazepine exposure slightly increased oral cleft risk (limited or inconsistent evidence) A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk. B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA:Information not available.

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Pharmacology
Half-Life: 1.2-12.3 hr (IV)

Onset
15 min (IM, PO) 2-3 min IV

Peak Plasma
Time: 0.5 hr (IM) Concentration: 90 ng/mL (IM)

Other Information
Peak Sedation: 30-60 min Duration: 1-4 hr Duration of Anterograde Amnesia: IM: 1 hr; IV: 20-40 min Bioavailability: >90% (IM) Protein Bound: 97% Vd: 1.0-3.1 L/kg Metabolism: hepatic CYP3A4 Metabolites: 1-hydroxymethylmidazolam Total Body Clearance: 0.25-0.54 L/hr/kg Excretion: urine

Mechanism of Action
Binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at several sites within the central nervous system, including the limbic system, reticular formation. Because it is water soluble, takes approximately 3 times longer than diazepam to peak EEG effects. Thus, clinician must wait 2-3 min to fully evaluate sedative effects before initiating procedure or repeating dose. Has twice the affinity for benzodiazepine receptors than diazepam. May be administered IM if unable to obtain vascular access.
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IV & IM Information

IV Incompatibilities
Syringe: dimenhydrinate, heparin, pentobarbital, perphenazine, prochlorperazine, ranitidine Additive: aminophylline(?), amoxicillin Y-site: albumin, amoxicillin, amphotericin B cholSO4, ampicillin, bumetanide, butorphanol, ceftazidime, cefuroxime, clonidine, dexamethasone, dobutamine(?), floxacillin, foscarnet, fosphenytoin, furosemide, hydrocortisone, imipenem-cilastatin, methotrexate, nafcillin, omeprazole, Na bicarb, thiopental, TMP-SMX

IV Compatibilities
Solution: D5W, D5/NS, NS Additive: cefuroxime, cimetidine, ciprofloxacin, furosemide, gentamicin, hydrocortisone, hydromorphone, metronidazole, ranitidine Syringe: alfentanil, atracurium, atropine, buprenorphine, butorphanol, chlorpromazine, cimetidine, diamorphine, diphenhydramine, droperidol, fentanyl, glycopyrrolate, hydromorphne, hydroxyzine, meperidine, metoclopramide, morphine, nalbuphine, ondansetron, promazine, promethazine, scopolamine, sufentanil, thiethylperazine, trimethobenzamide Y-site: abciximab, amikacin, amiodarone, argatroban, atracurium, bivalirudin, Ca-gluconate, cefazolin, cefotaxime, cimetidine, ciprofloxacin, cisatracurium, clindamycin, digoxin, diltiazem, dopamine, epinephrine, erythromycin, esmolol, etomidate, famotidine, fenoldopam, fentanyl, fluconazole, gatifloxacin, gentamicin, haloperidol, heparin, hetastarch, hydromorphone, insulin, labetalol, linezolid, lorazepam, methadone, methylprednisolone, metronidazole, milrinone, morphine, nicardipine, nitroglycerin, norepinephrine, pancuronium, pipieracillin, KCl, propofol, ranitidine, remifentanil, sodium nitroprusside, sufentanil, theophylline, tirofiban, tobramycin, vancomycin, vecuronium

IV Preparation
Solution: 100 mg in 250 mL D5W or NS Administration: via infusion pump

IV/IM Administration
IM: deep into large muscle mass IV: Give slowly over at least 2 min
And wait at least 2 min when adjusting doses to desired effect Excessive dose or too rapid infusion may cause resp arrest Have resuscitation equipment available and monitor pt closely until effects of IV admin are known

May dilute both 1 mg/mL or 5 mg/mL in D5W or NS to facilitate slow inj IVP: Administer through side port of free flowing IV Monitor for irritation and infiltration
Extravasation can cause tissue damage & necrosis

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