Name of the Adjuvant Benzodiazepine Drugs
- Lorazepam
- alprazolam
1.Lorazepam
| Lorazepam |
| Availability Injection: 2 mg/ml, 4 mg/ml Solution (concentrated): 2 mg/ml Tablets: 0.5 mg, 1 mg, 2 mg |
| Indications and dosages Anxiety Adults: 2 to 3 mg P.O. daily in two or three divided doses. Maximum dosage is 10 mg daily. Insomnia Adults: 2 to 4 mg P.O. at bedtime Premedication before surgery (as antianxiety agent, sedative-hypnotic, or amnestic) Adults: 0.05 mg/kg (not to exceed 4 mg) deep I.M. injection at least 2 hours before surgery, or 0.044 mg/kg (not to exceed 2 mg) I.V. 15 to 20 minutes before surgery. For greater amnestic effect, give up to 0.05 mg/kg (not to exceed 4 mg) I.V. 15 to 20 minutes before surgery. Status epilepticus Adults: 4 mg I.V. given slowly (no faster than 2 mg/minute). If seizures continue or recur after 10 to 15 minutes, repeat dose. If seizure control isn’t established after second dose, other measures should be used. Don’t exceed 8 mg in 12 hours. |
Mechanism of Action
May potentiate the effects of gamma aminobutyric acid (GABA) and other inhibitory neurotransmitters by binding to specific benzodiazepine receptors in limbic and cortical areas of CNS. GABA inhibits excitatory stimulation, which helps control emotional behavior. Limbic system contains a highly dense area of benzodiazepine receptors, which may explain drug’s antianxiety effects. Also, lorazepam hyperpolarizes neuronal cells, thereby interfering with their ability to generate seizures.
Pharmacokinetics
- Peak plasma time: 2 hr (tablets); 14 hr (capsules); <3 hr (IM)
- Protein bound: 85-93%
- Vd: 1.9 L/kg (adolescents); 1.3 L/kg (adults); 0.78 L/kg (neonates); 177 L (capsules)
- Metabolism: Inactive
- Undergoes glucuronic acid conjugation
- Half-life: 18 hr (children 2-12 years); 42 hr (neonates); 28 hr (adolescents); 18 hr (end stage renal disease); 12 hr (tablets, adults); 20.2 hr (capsules, adults)
- Excretion: Urine (88% mainly as inactive metabolites); feces (7%)
Administration
- For I.V. use, dilute with equal volume of compatible diluent, such as normal saline solution or dextrose 5% in water. Keep resuscitation equipment and oxygen at hand. 2Give each 2 mg of I.V. dose slowly, over 2 to 5 minutes. Don’t exceed rate of 2 mg/minute.
- Don’t give parenteral form to children younger than age 18.
Adverse reactions
- CNS: amnesia, agitation, ataxia, depression, disorientation, dizziness, drowsiness, headache, incoordination, asthenia
- CV (with too rapid I.V. administration): hypotension, bradycardia, tachycardia, apnea, cardiac arrest, cardiovascular collapse
- EENT: blurred vision, diplopia, nystagmus GI: nausea, abdominal discomfort
- Other: increased or decreased appetite
Contraindications
- Hypersensitivity to drug, other benzodiazepines, polyethylene or propylene glycol, or benzyl alcohol
- Acute angle-closure glaucoma
- Coma or CNS depression
- Hepatic or renal failure
Precautions Use cautiously in:
- Hepatic or renal impairment
- History of suicide attempt, drug abuse, depressive disorder, or psychosis
- Elderly patients
- Pregnant or breastfeeding patients.
Patient monitoring
- During I.V. administration, monitor ECG
- Monitor vital signs closely.
- Evaluate for amnesia.
- Watch closely for CNS depression. Institute safety precautions as needed to prevent injury.
- Monitor for signs and symptoms of overdose (such as confusion, hypotension, coma, and labored breathing).
- Assess liver function tests and CBC.
Patient teaching
- Tell patient and family about drug’s possible CNS effects. Recommend appropriate safety precautions.
- Explain that with long-term use, drug must be discontinued slowly (typically over 8 to 12 weeks).
- Instruct patient to avoid alcohol, because it increases drowsiness and other CNS effects.
- Caution patient to avoid smoking, because it speeds drug breakdown in body.
- Advise female patient to inform prescriber if she is pregnant or breastfeeding.
- As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, herbs, and behaviors mentioned above.
Nursing Considerations
- Before starting lorazepam therapy in a patient with depression, make sure he already takes an antidepressant because of increased risk of suicide in patients with untreated depression.
- Use extreme caution when giving lorazepam to elderly patients, especially those with compromised respiratory function, because drug can cause hypoventilation, sedation, unsteadiness, and respiratory depression.
- Use drug cautiously in patients with a history of alcohol or drug abuse or a personality disorder because of an increased risk of physical and psychological dependence. Also use cautiously in patients with severe hepatic insufficiency or encephalopathy because drug may worsen hepatic encephalopathy.
- For I.M. use, inject lorazepam deep into large muscle mass, such as gluteus maximus.
- For I.V. use, dilute lorazepam with equal amount of sterile water for injection, sodium chloride for injection, or D5W. Give diluted lorazepam slowly, at no more than 2 mg/min.
- During I.V. use, monitor patient’s respirations every 5 to 15 minutes and keep emergency resuscitation equipment readily available.
- Because stopping drug abruptly increases risk of withdrawal symptoms, expect to taper dosage gradually, especially in epileptic patients.
2.Alprazolam
| Alprazolam |
| Availability Tablet: Schedule IV 0.25mg ,0.5mg,1mg,2mg tablet, extended release: Schedule IV,0.5mg,1mg,2mg,3mg tablet, orally disintegrating: Schedule IV 0.25mg,0.5mg,1mg,2mg oral solution: Schedule IV 1mg/mL |
| Indications and dosages To control anxiety disorders, relieve anxiety (short-term therapy), or treat anxiety associated with depression TABLETS Adults. Initial: 0.25 to 0.5 mg t.i.d., adjusted to patient’s needs. Maximum: 4 mg daily in divided doses. To treat panic attack ORALLY DISINTEGRATING TABLETS, TABLETS Adults. Initial: 0.5 mg t.i.d., increased every 3 to 4 days by no more than 1 mg daily, based on patient response. Maximum: 10 mg daily in divided doses. E.R. TABLETS Adults. Initial: 0.5 to 1 mg daily in morning, increased every 3 to 4 days by no more than 1 mg daily, based on patient response. Maximum: 10 mg daily as single dose in morning |
Mechanism of Action
May increase effects of gamma-aminobutyric acid (GABA) and other inhibitory neurotransmitters by binding to specific benzodiazepine receptors in limbic and cortical areas of the CNS. GABA inhibits excitatory stimulation, which helps control emotional behavior. The limbic system contains many benzodiazepine receptors, which may help explain drug’s antianxiety effects
Pharmacokinetics
- Peak plasma time: 1-2 hr (immediate release); 9 hr (extended release); 1.5-2 hr (disintegrating tablet)
- Protein bound: 80%
- Metabolism: by hepatic P-450 enzyme CYP3A4
- Half-life: 11 hr average for immediate release, 13 hr average for extended release, and 13 hr average for disintegrating tablets (adults); 16.3 hr (elderly); 21.8 hr (obesity)
- Excretion: Urine
Contraindications
Acute angle-closure glaucoma; hypersensitivity to alprazolam, its components, or other benzodiazepines; itraconazole or ketoconazole therapy
Adverse Reactions
- CNS: Agitation, akathisia, confusion, depression, dizziness, drowsiness, fatigue, hallucinations, headache, insomnia, irritability, lack of coordination, light-headedness, memory loss, nervousness, paresthesia, rigidity, speech problems, syncope, tremor, weakness
- CV: Chest pain, edema, hypotension, nonspecific ECG changes, palpitations, tachycardia
- EENT: Blurred vision, altered salivation, dry mouth, nasal congestion, tinnitus
- ENDO: Galactorrhea, gynecomastia, hyperprolactinemia
- GI: Abdominal discomfort, anorexia, constipation, diarrhea, elevated liver function test results, hepatitis, hepatic failure, nausea, vomiting
- GU: Altered libido, urinary hesitancy
- MS: Dysarthria, muscle rigidity and spasms
- RESP: Hyperventilation, upper respiratory tract infection
- SKIN: Dermatitis, diaphoresis, pruritus, rash, Stevens-Johnson syndrome
- Other: Weight gain or loss
Nursing Considerations
- Expect to give a higher dosage if patient’s panic attacks occur unexpectedly or during such activities as driving.
- Because use can lead to dependency, expect to reduce dosage gradually when stopping drug. To prevent withdrawal symptoms, don’t stop drug abruptly.
Patient Teaching
- Warn against stopping drug abruptly because withdrawal symptoms may occur.
- Instruct patient never to increase prescribed dose because of risk of dependency.
- Urge patient to avoid drinking alcohol during alprazolam therapy.
- Advise patient to avoid driving and activities that require alertness until alprazolam’s effects are known.
- Instruct female patient of childbearing age to notify prescriber immediately if she becomes or might be pregnant. Drug isn’t recommended during pregnancy.
REFERENCES
- Robert Kizior, Keith Hodgson, Saunders Nursing Drug handbook,1st edition 2024, Elsevier Publications. ISBN-9780443116070
- McGraw Hill- Drug Handbook, Seventh Edition, 2013, McGraw Hill Education Publications,9780071799430.
- April Hazard, Cynthia Sanoski, Davi’s Drug Guide for Nurses -Sixteenth Edition 2019, FA Davis Company Publications,9780803669451.
- Jones and Bartlet, Pharmacology for Nurses, Second Edition, 2020, Jones and Bartlet Learning Publications, ISBN 9781284141986.
- Nursebro.com, Search – Nursebro
Stories are the threads that bind us; through them, we understand each other, grow, and heal.
JOHN NOORD
Connect with “Nurses Lab Editorial Team”
I hope you found this information helpful. Do you have any questions or comments? Kindly write in comments section. Subscribe the Blog with your email so you can stay updated on upcoming events and the latest articles.