Name of the Hypnotic sedatives Drugs
- Estazolam
- Alprazolam
- Phenobarital
- Pentobarbital
1.Estazolam
| Estazolam |
| Availability tablet: Schedule IV 1mg ,2mg |
| Indications and Dosages To treat insomnia Adults. 1 to 2 mg at bedtime |
Mechanism of Action
May potentiate effects of gamma-aminobutyric acid (GABA) and other inhibitory neurotransmitters by binding to specific benzodiazepine receptors in limbic and cortical areas of CNS. By binding to these receptors, estazolam increases GABA’s inhibitory effects and blocks cortical and limbic arousal.
Pharmacokinetics
- Half-Life: 10-24 hr
- Duration: Variable
- Peak Plasma Time: 0.5-1.6 hr
- Protein Bound: 93%
- Metabolism: Hepatic
- Metabolites: Inactive
- Excretion: Urine
- Half-life elimination: 10-24 h, and peak action is 2 h
Contraindications
Acute angle-closure glaucoma; hypersensitivity to estazolam, other benzodiazepines, or their components; pregnancy; psychosis
Adverse Reactions
- CNS: Amnesia, anxiety, ataxia, confusion, delusions, depression, dizziness, drowsiness, euphoria, headache, hypokinesia, irritability, malaise, nervousness, slurred speech, tremor
- CV: Chest pain, palpitations, tachycardia
- EENT: Blurred vision, dry mouth, increased salivation, photophobia
- GI: Abdominal pain, constipation, diarrhea, nausea, thirst, vomiting
- GU: Libido changes
- RESP: Respiratory depression
- SKIN: Diaphoresis
- Other: Physical or psychological dependence
Nursing Considerations
- Use estazolam with extreme caution in patients with a history of drug or alcohol abuse because of risk of addiction. Expect to give drug for no more than 12 weeks.
- Use cautiously in elderly or debilitated patients and those with depression or impaired hepatic, renal, or respiratory function.
- Expect to stop drug gradually to prevent withdrawal symptoms. Avoid stopping abruptly if patient has history of seizures. • Monitor respiratory status, especially in patients with respiratory compromise, who are at increased risk for respiratory depression.
- If patient takes estazolam for depression,watch for suicidal tendencies, especially when therapy starts or dosage changes
Patient Teaching
- Warn patient not to exceed prescribed time because of risk of addiction.
- Because estazolam can reduce alertness, advise patient to avoid hazardous activities until CNS effects of the drug are known.
- Advise patient not to drink alcohol or take other CNS depressants during therapy because of the risk of additive effects.
- Warn elderly and debilitated patients and those with impaired hepatic or renal function about risk of excessive sedation or mental impairment and need to report them.
- If patient takes 2-mg dosage for a long time, warn against stopping drug abruptly.
3.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 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 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
- Bioavailability: 90%
- Peak serum time: 1-2 hr (immediate release); 9 hr (extended release); 1.5-2 hr (disintegrating tablet)
- Protein bound: 80%
- Metabolized 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.
3.Phenobarital
| Phenobarital |
| Availability Capsules: 16 mg Elixir: 15 mg/5 ml, 20 mg/5 ml Injection: 30 mg/ml and 60 mg/ml in 1-ml prefilled syringes; 65 mg/ml in 1-ml vials; 130 mg/ml in 1-ml prefilled syringes, 1-ml vials, and 1-ml ampules Tablets: 15 mg, 16 mg, 30 mg, 60 mg, 90 mg, 100 mg |
| Indications and dosages ➣ Tonic-clonic (grand mal) and partial seizures; febrile seizures in children Adults: 60 to 100 mg/day P.O. as a single dose or in two or three divided doses; or initially, 100 to 320 mg I.V. p.r.n. (a total of 600 mg I.V. in a 24- hour period). Infants and children: Loading dose of 15 to 20 mg/kg P.O. (produces drug blood level of 20 mcg/ml shortly after dosing). To achieve therapeutic blood level (10 to 25 mcg/ml), children usually need higher dosage/kg than adults. Follow loading dose with 3 to 6 mg/kg/day P.O. Alternatively, 4 to 6 mg/kg/day I.M.or I.V. for 7 to 10 days to achieve blood level of 10 to 15 mcg/ml. ➣ Status epilepticus Adults: 200 to 320 mg I.M. or I.V., repeated q 6 hours p.r.n. Children: 15 to 20 mg/kg I.V. given over 10 to 15 minutes ➣ Sedation or hypnotic effect Adults: For sedation, 30 to 120 mg/day P.O. or 30 to 120 mg/day I.M. or I.V. in two or three divided doses. As a hypnotic, 100 to 200 mg P.O. or 100 to 320 mg I.M. or I.V. at bedtime. Don’t exceed 400 mg in a 24-hour period. ➣ Preoperative sedation Adults: 100 to 200 mg I.M. 60 to 90 minutes before surgery Children: 1 to 3 mg/kg I.M. or I.V., as prescribed |
Mechanism of Action
Inhibits ascending conduction of impulses in the reticular formation, which controls CNS arousal to produce drowsiness, hypnosis, and sedation. Phenobarbital also decreases the spread of seizure activity in cortex, thalamus, and limbic system. It promotes an increased threshold for electrical stimulation in the motor cortex, which may contribute to its anticonvulsant properties.
Pharmacokinetics
- Bioavailability: 70-90%
- Peak plasma time: 8-12 hr
- Protein bound: 20-45%
- Metabolized by hepatic oxidative hydroxylation
- Half-life: 50-140 hr
- Excretion: Urine (major)
Administration
- Inject I.M. deep into large muscle mass; limit volume to 5 ml.
- Give I.V. no faster than 60 mg/ minute. Keep resuscitation equipment at hand.
- Stop injection immediately if patient complains of pain or if circulation at injection site diminishes (indicating inadvertent intra-arterial injection).
- Don’t give by subcutaneous route; severe reactions (such as pain and tissue necrosis) may occur.
- Know that when given I.V. for status epilepticus, drug may take 15 minutes to attain peak blood level in brain. If injected continuously until seizures stop, drug brain level would keep rising and could exceed that required to control seizures. To avoid barbiturateinduced depression, use minimal amount required and wait for anticonvulsant effect to occur before giving second dose.
- Use parenteral route only when patient can’t receive drug P.O.
- Know that drug is intended only for short-term use, losing efficacy after about 2 weeks.
Contraindications
- Hypersensitivity to drug or other barbiturates
- Manifest or latent porphyria
- Nephritis (with large doses)
- Severe respiratory disease with dyspnea or obstruction
- History of sedative-hypnotic abuse
- Subcutaneous or intra-arterial administration
Precautions:
- Hepatic dysfunction, renal impairment, seizure disorder, fever, hyperthyroidism, diabetes mellitus, severe anemia, pulmonary or cardiac disease
- History of suicide attempt or drug abuse
- Chronic phenobarbital use
- Elderly or debilitated patients
- Pregnant or breastfeeding patients
- Children younger than age 6
Adverse reactions
- CNS: headache, dizziness, anxiety, depression, drowsiness, excitation, delirium, lethargy, agitation, confusion, hyperkinesia, ataxia, vertigo, nightmares, nervousness, paradoxical stimulation, abnormal thinking, hallucinations, insomnia, CNS depression
- CV: hypotension, syncope, bradycardia (with I.V. use)
- GI: nausea, vomiting, constipation
- Hematologic: megaloblastic anemia
- Hepatic: hepatic damage
- Musculoskeletal: joint pain, myalgia
- Respiratory: hypoventilation, laryngospasm, bronchospasm, apnea (with I.V. use); respiratory depression
- Skin: rash, urticaria, exfoliative dermatitis, Stevens-Johnson syndrome
- Other: phlebitis at I.V. site, drug dependence, hypersensitivity reactions including angioedema
Patient monitoring
- Monitor vital signs; watch for bradycardia and hypotension.
- In patients with seizure disorders, know that drug withdrawal may cause status epilepticus.
- Assess neurologic status. Institute safety measures as needed.
- Closely monitor respiratory status, especially for respiratory depression and airway spasm.
- Monitor phenobarbital blood level, CBC, and kidney and liver function tests.
- Watch for signs of drug dependence.
Patient teaching
- Instruct patient to promptly report rash, facial and lip edema, syncope, dyspnea, or depression.
- Stress importance of taking exactly as prescribed, with or without food. Caution patient not to stop therapy abruptly, especially if he’s taking drug for seizures.
- Tell patient that prolonged use may lead to dependence.
- Instruct patient to seek medical advice before taking other prescription or over-the-counter drugs.
- Caution patient to avoid driving and other hazardous activities until he knows how drug affects him.
- Advise patient to avoid herbs, alcohol, and other CNS depressants.
- Instruct patient taking hormonal contraceptives to use alternate birthcontrol method.
- As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above.
Nursing Considerations
- Be aware that phenobarbital shouldn’t be given during third trimester of pregnancy because repeated use can cause dependence in neonate. It also shouldn’t be given to breast-feeding women because it may cause CNS depression in infants.
- Use I.V. route cautiously in patients with CV disease, hypotension, pulmonary disease, or shock because drug may cause adverse hemodynamic or respiratory effects.
- Because drug can cause respiratory depression, assess respiratory rate and depth before use, especially in patient with bronchopneumonia, pulmonary disease, respiratory tract infection, or status asthmaticus.
- Give elixir undiluted or mix with water, milk, or fruit juice. Use a calibrated device to measure doses.
- If necessary, crush tablets and mix with food or fluids.
- Reconstitute sterile powder with at least 10 ml sterile water for injection. Don’t use reconstituted solution if it fails to clear within 5 minutes. Further dilute prescribed dose with normal saline solution or D5W and infuse over 30 to 60 minutes.
- Don’t give more rapidly than 60 mg/min by I.V. injection.
- During I.V. use, monitor blood pressure, respiratory rate, and heart rate and rhythm. Anticipate increased risk of hypotension, even at recommended rate. Keep resuscitation equipment readily available.
- During I.M. use, don’t inject more than 5 ml into any one I.M. site to prevent sterile abscess formation.
- Be aware that drug may cause physical and psychological dependence.
- Expect that phenobarbital’s CNS effects may exacerbate major depression, suicidal tendencies, or other mental disorders.
- Take safety precautions for elderly patients, as appropriate, because they’re more likely to experience confusion, depression, and excitement as adverse CNS reactions.
- Anticipate that phenobarbital may cause paradoxical stimulation in children.
- Be aware that drug may trigger signs and symptoms in patients with acute intermittent porphyria.
4.Pentobarbital
| Pentobarbital |
| Availability Injection: 50 mg/ml in 2-ml prefilled syringes |
| Indications and dosages ➣ Preoperative sedation Adults: Initially, 150 to 200 mg I.M., or 100 mg I.V. ➣ Seizures Adults: Initially, 100 mg. I.V.; may give additional doses after 1 minute. Maximum dosage is 500 mg. Children: Initially, 50 mg. I.V.; may give additional doses until desired response occurs. Don’t exceed 100 mg/ dose. |
Mechanism of Action
Inhibits ascending conduction in reticular formation, which controls CNS arousal to produce drowsiness, hypnosis, and sedation. Pentobarbital also decreases spread of seizure activity in cortex, thalamus, and limbic system. It promotes an increased threshold for electrical stimulation in the motor cortex, which may contribute to anticonvulsant effects.
Pharmacokinetics
- Half-Life: 15-50 hr
- Onset: 10-15 min (IM); 3-5 min (IV)
- Duration: 3-4 hr
- Protein bound: 45-70%
- Metabolism: hepatic microsomal enzymes, glucuronidation
- Excretion: Mostly urine
- Enzymes induced: CYP1A2, CYP2C9/10, CYP3A4
Administration
- When giving I.V., make sure resuscitation equipment is available.
- Give I.V. by direct injection no faster than 50 mg/minute.
- Inject I.M. deep into large muscle mass.
- Don’t give by subcutaneous or intra-arterial routes, because severe reactions (such as tissue necrosis and gangrene) may occur.
- Know that drug is for short-term use only, losing efficacy after about 2 weeks.
Contraindications
- Hypersensitivity to drug or other barbiturates
- Nephritis (with large doses)
- Severe hepatic impairment
- Severe respiratory disease with dyspnea or obstruction
- Manifest or latent porphyria
- History of sedative-hypnotic abuse
- Subcutaneous or intra-arterial administration
Precautions:
- Hepatic or renal impairment, increased risk for suicide, alcohol use
- History of drug addiction
- Labor and delivery
- Elderly or debilitated patients.
Adverse reactions
- CNS: drowsiness, agitation, confusion, hyperkinesia, ataxia, nightmares, nervousness, hallucinations, insomnia, anxiety, abnormal thinking
- CV: hypotension, syncope, bradycardia (all with I.V. use)
- GI: nausea, vomiting, constipation
- Hepatic: hepatic damage
- Musculoskeletal: joint pain, myalgia, neuralgia Respiratory: laryngospasm (with I.V. use), bronchospasm, respiratory depression
- Skin: rash, urticaria, exfoliative dermatitis
- Other: phlebitis at I.V. site, physical or psychological drug dependence, fever, hypersensitivity reactions including angioedema
Patient monitoring
- Closely monitor blood pressure and heart and respiratory rates. Watch for evidence of respiratory depression.
- Monitor neurologic status before and during therapy.
- Assess CBC and kidney and liver function tests.
- In long-term therapy, monitor patient for signs of drug dependence.
Patient teaching
- Advise patient to avoid other CNS depressants, alcohol, and herbs.
- Caution patient to avoid driving and other hazardous activities.
- Advise patient taking hormonal contraceptives to use alternate birth control method during therapy.
- As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above.
Nursing Considerations
- Use pentobarbital with extreme caution in patients with depression, a history of drug abuse, or suicidal tendencies.
- Use drug cautiously in elderly or debilitated patients and those with acute or chronic pain because it may induce paradoxical stimulation.
- When using I.V. route, inject drug at 50 mg/min or less to avoid adverse respiratory and circulatory reactions.
- If patient shows premonitory signs of hepatic coma, withhold drug and notify prescriber immediately.
- Monitor I.V. site closely and avoid extravasation. Drug is highly alkaline and may cause local tissue damage and necrosis
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
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