Name of the CNS Stimulants drugs
- Dextroamphetamine
- Doxapram
- Methylphenidate hydrochloride
- Pemoline
1.Dextroamphetamine
| Dextroamphetamine |
| Availability: Capsules (sustained release): 5 mg, 10 mg, 15 mg; Oral solution: 5 mg/ml; Tablets: 5 mg, 10 mg transdermal system: Schedule II : 4.5mg/9hr, 9mg/9hr, 13.5mg/9hr, 18mg/9hr |
| Administration and Handling: Administer amphetamines at lowest effective dosage and adjust dosage individually Administer initial dose upon awakening; avoid late evening doses because of resulting insomnia Do not crush or chew extended-release formulations. Make sure patient swallows sustained- release capsules whole without chewing or crushing. Before starting therapy, perform complete cardiac evaluation, including ECG and echocardiogram. Give last daily dose at least 6 hours before patient’s bedtime. Don’t give within 14 days of MAO inhibitor, because potentially fatal reaction may occur. |
| Transdermal Administration : Apply 1 patch at a time for ≤9 hr; use only 1 patch/24 hr. Apply to clean (void of lotions, oils, or gels), dry (not wet), and intact skin at selected application site; Application sites include hip, upper arm, chest, upper back, or flank; Select a different application site each time a new transdermal system is applied; Avoid touching adhesive side to avoid absorption of amphetamine; If adhesive side is touched, immediately wash hands with soap and water; If patch lifts at edges, reattach patch by pressing firmly and smoothing down edges of patch; If patch comes off completely, apply a new patch; Do not apply or reapply with dressings, tape, or other common adhesives Avoid exposing application site to direct external heat sources (eg., hair dryers, heating pads, electric blankets, heated water beds) while wearing transdermal system; heat to application site increases both rate and extent of absorption |
| Attention deficit hyperactivity disorder: Adults: 5 to 60 mg P.O. daily in divided doses until optimal response is obtained. Children ages 6 and older: 5 mg (capsules, oral solution, or tablets) P.O. once or twice daily, increased by 5 mg at weekly intervals until optimal response is obtained; Children ages 3 to 5: 2.5 mg (oral solution) P.O. daily, increased by 2.5 mg at weekly intervals until optimal response is obtained. |
| Narcolepsy: Adults: 5 to 60 mg P.O. daily as a single dose or in divided doses Children ages 12 and older: 10 mg P.O. daily, increased by 10 mg at weekly intervals until desired response occurs or adult dosage is reached. Children ages 6 to 11: 5 mg P.O. daily, increased by 5 mg at weekly intervals until desired response occurs or adult dosage is reached. |
Mechanism of Action
Sympathomimetic amine that promotes release of dopamine and norepinephrine from their storage sites in the presynaptic nerve terminals; may also block reuptake of catecholamines by competitive inhibition.
Indications:
- Narcolepsy
- Attention Deficit Hyperactivity Disorder
Cautions & Contraindications:
- Hypersensitivity to drug or tartrazine
- Glaucoma
- Psychotic disorders, agitated states
- Advanced arteriosclerosis, symptomatic cardiovascular disease, moderate to severe hypertension
- Hyperthyroidism
- MAO inhibitor use within past 14 days
- Pregnancy or breastfeeding
Use cautiously in:
- cardiovascular disease, hypertension, diabetes mellitus
- history of substance abuse
- elderly patients
Black Box Warning
- Drug has high abuse potential. Prolonged use may lead to drug dependence. Stay alert for possibility of patient obtaining drug for nontherapeutic use or distribution. Drug should be prescribed sparingly.
- Misuse may cause sudden death and serious cardiovascular events.
Metabolism and Half- life:
- Onset of action: 1-1.5 hr
- Metabolism: Hepatic via glucuronidation and monooxygenase
- Half-life elimination: 10-13 hr (adults); Excretion: Urine
Drug Interactions:
- MAO inhibitors: hypertensive crisis
- Acetazolamide, sodium bicarbonate: urine alkalization, leading to increased dextroamphetamine effects
- Adrenergic blockers: additive effects
- Caffeine: increased stimulant effect
Side- Effects:
- Hyperactivity, insomnia, restlessness, tremor, depression, dizziness, headache, irritability
- Palpitations, tachycardia, hypertension, hypotension, arrhythmias
- Nausea, vomiting, constipation, diarrhea, abdominal cramps, dry mouth
- Erectile dysfunction, increased libido
- Urticaria
- Metallic taste,
- Decreased appetite
- Physical or psychological drug dependence
Nursing Considerations
Monitor:
- Cardiovascular: Blood pressure, heart rate, changes in fingers and toes
- General: Signs of abuse/dependence
- Musculoskeletal: Growth (height, weight, appetite)
Psychiatric: New or worsening psychiatric disorders, including aggressive behavior/hostility, depression, psychosis, mania, and suicidal thoughts or behavior
- Interrupt therapy or reduce dosage periodically to assess drug efficacy in patients with behavior disorders
- Monitor patient for new or worsening aggressive behavior.
- Monitor blood and urine glucose levels carefully in diabetic patient. Drug may alter regular insulin requirements.
Patient teaching
- Tell patient to swallow sustained- release capsules whole with liquid without chewing or crushing.
- Advise patient to take drug early in day to avoid insomnia.
- Instruct patient to immediately notify prescriber if chest pain, irregular pulse, or worsening aggressive behavior occurs.
- Instruct patient to avoid driving and other hazardous activities until he knows how drug affects him.
- Caution patient not to stop therapy abruptly but to taper dosage gradually.
2.Doxapram
| Doxapram |
| Availability: Injection: 20 mg/ml |
| Administration and Handling: IV Preparation : Add 250 mg doxapram to 250 mL D5W, D10W or NS to obtain a 1 mg/mL solution; For COPD: add 400 mg doxapram to 180 mL D5W, D10W or NS to a final concentration of 2 mg/mL IV Administration: COPD : Initial infusion at 1-2 mg/min; may incr to NMT 3 mg/min; No more than 2 hr; ABG should be determined before administering doxapram & q30min during 2 hr of infusion; Discontinue if ABG show evidence of deterioration. Anesthesia: If infusing, use 1 mg/mL at an initial rate of 5 mg/min; When the desired response is obtained or if adverse effects appear, may be reduce to 1-3 mg/min; Do not increase infusion rate in debilitated patients in an attempt to lower pCO2 because of associated increased work in breathing CNS Depression: If infusing, infuse at 1-3 mg/min until patient begins to awaken, but NMT 2 hr; May repeat after a 30 min-2 hr rest period, provided max daily dose of 3 g has not been exceeded Storage : Store at 20-25°C |
| Respiratory depression after anesthesia : Adults and adolescents: 5 mg/minute by I.V. infusion until desired response occurs; then reduce to 1 to 3 mg/minute, to a maximum cumulative dosage of 4 mg/kg (or 300 mg). Or 0.5 to 1 mg/kg I.V. injection, repeated q 5 minutes, if needed, to a maximum total dosage of 1.5 mg/kg. |
| Chronic pulmonary disease related to acute hypercapnia : Adults: 1 to 2 mg/minute by I.V. infusion, using a concentration of 2 mg/ml, to a maximum of 3 mg/minute. Infusion shouldn’t exceed 2 hours |
| Drug-induced CNS depression : Adults: Initially, 2 mg/kg I.V., repeated in 5 minutes and then q 1 to 2 hours until patient awakens, to a maximum daily dosage of 3 g. For infusion, priming dose of 2 mg/kg I.V.; if no response occurs, continue for 1 to 2 hours as needed; if some response occurs, give I.V. infusion of 250 mg in 250 ml of saline solution or dextrose 5% in water at 1 to 3 mg/minute until patient awakens. Don’t infuse longer than 2 hours or give more than 3 g/day. |
Mechanism of Action
Activates peripheral carotid, aortic, and other chemoreceptors to stimulate respiration, resulting in increased tidal volume and respiratory rate. Doxapram also may increase respiratory rate and tidal volume by directly stimulating the respiratory center in the medulla oblongata.
Indications:
- Respiratory depression after anesthesia
- Chronic pulmonary disease related to acute hypercapnia
- Drug-induced CNS depression
Cautions & Contraindications:
- Hypersensitivity to drug
- Cardiovascular disorders, severe hypertension
- Cerebrovascular accident
- Head injury, seizures
- Respiratory failure, restrictive respiratory disease
- Neonates
Use cautiously in:
- bronchial asthma, arrhythmias,
- increased intracranial pressure, hyperthyroidism, pheochromocytoma, metabolic disorders
- concurrent use of mechanical ventilation
- pregnant or breastfeeding patients.
Metabolism and Half- life:
Onset: 20-40 sec; Duration: 5-12 min (single IV injection)
Peak Plasma Time: 1-2 min;
Half-life: 3.4 hr (2.4-4.1 hr)
Drug Interactions:
- General anesthetics: increased risk of self-limiting arrhythmias
- MAO inhibitors, sympathomimetics: potentiation of adverse cardiovascular effects
- Skeletal muscle relaxants: masking of residual effects of these drugs
Side- Effects:
- CNS: Disorientation, dizziness, headache
- CV: Arrhythmias, including sinus tachycardia; hypertension
- GI: Diarrhea, hiccups, nausea, vomiting
- GU: Urine retention
- RESP: Bronchospasm, cough, dyspnea
- SKIN: Diaphoresis
- Other: Injection site pain, redness, swelling, and thrombophlebitis
Nursing Considerations
- Avoid giving doxapram to patients receiving mechanical ventilation.
- Maintain a patent airway and assess for optimal oxygenation before giving drug.
- Monitor I.V. insertion site for extravasation and signs of thrombophlebitis or local skin irritation.
- If hypertension or dyspnea develops suddenly, stop infusion as directed.
- Assess patient for early signs and symptoms of overdose, including enhanced deep tendon reflexes, skeletal muscle hyperactivity, and tachycardia.
Monitoring / evaluation:
- Assess blood pressure, pulse, deep tendon reflexes, airway, and arterial blood gas values before starting therapy and frequently during infusion.
- Monitor I.V. site frequently for irritation and thrombophlebitis.
Patient teaching
- Instruct patient to report adverse reactions promptly.
- Explain the need for frequent pulse and blood pressure monitoring
3.Methylphenidate hydrochloride
| Methylphenidate hydrochloride |
| Availability : Capsules (extended-release): 10 mg, 20 mg, 30 mg, 40 mg, 50 mg, 60 mg Solution (oral): 5 mg/5 ml, 10 mg/ 10 ml; Tablets (chewable): 2.5 mg, 5 mg, 10 mg; Tablets (extended-release): 10 mg,18 mg, 20 mg, 27 mg, 36 mg, 54 mg; Tablets (prompt-release): 5 mg, 10 mg,20 mg Tablets (sustained-release): 20 mg; Transdermal patch: 10 mg/9 hours, 15 mg/9 hours, 20 mg/9 hours,30 mg/9 hours |
| Administration and Handling: Sustained-release, extended-release tablets may be given in place of regular tablets once the daily dose is titrated using regular tablets and the titrated dosage corresponds to sustained-release or extended-release tablet strength. |
| PO: Do not give in afternoon or evening (may cause insomnia). Do not crush, break extended-release capsules, extended- or sustained-release tablets. • Immediate- release tablets may be crushed. • Give dose 30–45 min before meals. |
| Patch: To be worn daily for 9 hrs. • Replace daily in morning. • Apply to dry, clean area of hip. • Avoid applying to waistline (clothing may cause patch to rub off). • Alternate application site daily. • Press firmly in place for 30 sec to ensure patch is in good contact with skin. • Do not cut patch. |
| ADHD: PO: Adults: (Immediate-Release): 5 mg twice daily, before breakfast and lunch. May increase by 5–10 mg/day at weekly intervals. Maximum: 60 mg/day in 2–3 divided doses. Children 6 yrs and older: Initially, 2.5–5 mg before breakfast and lunch. May increase by 5–10 mg/day at weekly intervals. Usual dose: 20–30 mg/day in 2–3 divided doses. Maximum: 60 mg/day. Patch: Children 6–12 yrs, adolescents: Initially, 10 mg daily (applied and worn for 9 hrs). Dosage is titrated to desired effect. May increase dose no more frequently than every wk. |
| Narcolepsy: PO: Adults, elderly: (Immediate-Release): Initially, 5 mg twice daily, before breakfast and lunch. May increase by 5–10 mg/day at weekly intervals. Maximum: 60 mg/day in 2–3 divided doses. (Extended-Release): May be given once the immediate-release dose is titrated and the titrated 8-hr dose corresponds to sustained-release or extended-release tablet strength. Maximum: 60 mg/day |
Mechanism of Action
Blocks the reuptake mechanism of dopaminergic neurons in the cerebral cortex and subcortical structures of the brain, including the thalamus, decreasing motor restlessness and improving concentration.
Methylphenidate also may trigger sympathomimetic activity. This action produces increased motor activity, alertness, mild euphoria, and decreased fatigue in patients with narcolepsy.
Indications:
- Treatment of attention-deficit hyperactivity disorder (ADHD).
- Management of narcolepsy.
- OFF-LABEL: Depression in ill, elderly patients (such as those with cerebrovascular accident)
- To enhance analgesia and sedation in patients receiving opioids
Cautions & Contraindications:
- Hypersensitivity to methylphenidate.
- Use during or within 14 days following MAOI therapy
- Marked anxiety, tension, agitation, motor tics
- Family history or diagnosis of tourette’s syndrome, glaucoma.
- Severe hypertension, HF, arrhythmia
- Hyperthyroidism
- Recent MI or angina.
- Cautions: Hypertension, seizures, acute stress reaction, emotional instability, history of drug dependence, HF, recent MI, hyperthyroidism or thyrotoxicosis, known structural cardiac abnormality, bipolar disorder, cardiomyopathy, arrhythmias, alcohol abuse.
Metabolism & Half- Life:
Slowly, incompletely absorbed from GI tract. Protein binding: 15%. Metabolized in liver. Primarily excreted in urine. Unknown if removed by hemodialysis. Half-life: 2–4 hrs.
Drug Interactions:
- MAOIs (e.g., phenelzine, selegiline) may increase hypertensive effects.
- Other CNS stimulants (e.g., caffeine, dextroamphetamine, phentermine) may have additive effect.
- May inhibit metabolism of warfarin, anticonvulsants, antidepressants.
- Alcohol may increase adverse effects.
Side –Effects:
- Anxiety
- Insomnia
- Anorexia
- Dizziness
- Drowsiness
- Headache
- Nausea, abdominal pain
- Fever, rash, arthralgia, vomiting.
- Rare: blurred vision, tourette’s syndrome (uncontrolled vocal outbursts, repetitive body movements, tics), palpitations, priapism
Nursing Considerations:
Baseline assessment
- DHD: Assess attention span, impulsivity, interaction with others, distractibility.
- Narcolepsy: Observe/assess frequency of episodes. Question history of seizures.
Intervention/evaluation
- Monitor B/P, pulse, changes in ADHD symptoms.
- CBC with differential should be performed routinely during therapy.
- If paradoxical return of attention-deficit occurs, dosage should be reduced or discontinued. Monitor growth
Patient/family teaching
- Avoid tasks that require alertness, motor skills until response to drug is established.
- Sugarless gum, sips of water may relieve dry mouth.
- Report any increase in seizures.
- Take daily dose early in morning to avoid insomnia.
- Report anxiety, palpitations, fever, vomiting, skin rash.
- Report new or worsened symptoms (e.g., behavior, hostility, concentration ability).
- Avoid caffeine.
- Do not stop taking abruptly after prolonged use.
4. Pemoline
| Pemoline |
| Availability: tablets: 18.75 mg, 37.5 mg or 75 mg of pemoline. chewable tablets containing 37.5 mg of pemoline. |
| Administration and Handling: chewable tablet: must be chewed before swallowing. Do not swallow whole. administered as a single oral dose each morning. The recommended starting dose is 37.5 mg/day. This daily dose should be gradually increased by 18.75 mg at one-week intervals until the desired clinical response is obtained. The effective daily dose for most patients will range from 56.25 to 75 mg. The maximum recommended daily dose of pemoline is 112.5 mg. Storage: Store below 86° F (30° C). |
| ADHD: oral or chewable dosage forms (tablets): Children 6 years of age and over—To start, 37.5 milligrams (mg) every morning. Your doctor may increase your dose if needed. However, the dose is usually not more than 112.5 mg a day. Adult: Initial dose: 37.5 mg orally every morning. Maintenance dose: May increase by 18.75 mg a day at one- week intervals, up to a maximum of 112.5 mg/day. |
Mechanism of Action:
The pharmacologic actions of pemoline are qualitatively similar to those of the amphetamines and methylphenidate and include CNS and respiratory stimulation and weak sympathomimetic activity. Pemoline may produce an increase in motor activity, mental alertness, diminished sense of fatigue, and mild euphoria. In usual therapeutic dosage, pemoline exhibits no substantial effects on the peripheral circulatory system.
Indications:
Attention Deficit Hyperactivity Disorder (ADHD)
Pemoline has been associated with life-threatening hepatic failure and should not ordinarily be considered as first line drug therapy for Attention Deficit Hyperactivity Disorder (ADHD).
Cautions & Contraindications:
- Liver Impairment
- Children < 6 year
- Tourette’s syndrome
- Psychosis
Metabolism and Half- Life:
Onset: Peak effect: 4 hours
Duration: 8 hours-life: children 7-8.6 hour; adults: 12 hours.
Readily absorbed from the GI tract and Metabolized in Liver.
Excretion Via Urine, feces
Drug Interactions:
- Hypertensive crisis with MAOIs.
- Reduced seizure threshold in epileptic patients on antiepileptics.
Side- Effects:
- Insomnia
- Nervousness
- Headache
- Drowsiness
- Mild depression
- Nausea
- Abdominal discomfort
- Diarrhea
- Decreased appetite
- Weight loss
- Rapid heart rate
- Rash
Nursing Considerations:
- Administered with caution to patients with significantly impaired renal function.
- This drug should be initiated only in individual without liver disease and with normal baseline liver function tests.
- Periodic liver function tests should be done. Should be discontinued if clinically significant liver function test abnormalities are revealed at any time during therapy with this drug.
- Patients who are receiving CYLERT (pemoline) concurrently with other drugs, especially drugs with CNS activity, should be monitored carefully.
- Decrements in the predicted growth (i.E., Weight gain and/or height) rate have been reported with the long- term use of stimulants in children. Therefore, patients requiring long-term therapy should be carefully monitored.
Patient / family teaching:
- Avoid alcohol.
- Limit caffeine intake.
- Take with or without food. Food does not significantly affect absorption.
- To avoid insomnia and to provide its greatest benefits during waking hours, pemoline should be taken in the morning. Have your child take pemoline exactly as directed. Your child should not take more or less of it or take it more often than prescribed by the doctor.
- This medicine may cause some people to become dizzy or less alert than they are normally. Make sure you know how you react to this medicine before you ride a bicycle or do anything else that could be dangerous if you are dizzy or are not alert.
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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