Lisdexamfetamine Dimesylate (lisdexamfetamine dimesylate)
Amphetamines/Anorexiants/Stimulants Oral Capsule; Oral Tablet,Chewable
Last reviewed · Source: First Databank (FDB) drug data
Overview
Lisdexamfetamine dimesylate is a prodrug of dextroamphetamine, a noncatecholamine, sympathomimetic amine with CNS-stimulating activity.
Lisdexamfetamine, a prodrug of dextroamphetamine, is a CNS stimulant. Lisdexamfetamine is inactive until hydrolyzed in vivo to l-lysine and dextroamphetamine, which is responsible for the drug's activity. The exact mechanism of therapeutic action in attention deficit hyperactivity disorder (ADHD) and binge-eating disorder is not known.
Amphetamines block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of the monoamines into the extraneuronal space.
Following single-dose administration of lisdexamfetamine, the pharmacokinetics of dextroamphetamine are linear over the oral dosage range of 30-70 mg in children 6-12 years of age and over the oral dosage range of 50-250 mg in adults. Following single-dose administration of a lisdexamfetamine capsule, peak plasma concentrations of lisdexamfetamine occur in approximately 1 hour; concentrations are low and transient, and become nonquantifiable by 8 hours after administration. Peak plasma concentrations of dextroamphetamine occur in approximately 3.5 hours.
Following administration of the chewable tablets, peak plasma concentrations of lisdexamfetamine occur at about 1 hour and dextroamphetamine at 4.4 hours. Lisdexamfetamine and dextroamphetamine do not accumulate at steady state in adults. Administration of capsules with food (high-fat meal or yogurt) delays time to peak plasma concentrations of dextroamphetamine by about 1 hour; however, administration with a high-fat meal, yogurt, or orange juice does not affect the AUC or magnitude of the peak plasma concentration of dextroamphetamine.
Peak plasma concentrations and AUC of lisdexamfetamine are reduced by about 15% when the chewable tablets are administered versus the capsules; however, exposure to dextroamphetamine is similar between products. Food (high-fat meal) decreases the magnitude of peak plasma concentrations and AUC of dextroamphetamine by about 5-7% and delays the time to peak concentrations by about 1 hour. Lisdexamfetamine is not metabolized by CYP isoenzymes.
Lisdexamfetamine is converted to l-lysine and dextroamphetamine by hydrolytic activity of erythrocytes, which have a high capacity for metabolism of lisdexamfetamine. Lisdexamfetamine is excreted principally in urine. Approximately 96% of a 70-mg radiolabeled oral dose of lisdexamfetamine was recovered in urine; parent drug accounted for about 2% of the recovered radioactivity.
Changes in urinary pH may alter excretion of amphetamines. The elimination half-life of lisdexamfetamine is less than 1 hour in patients >=6 years of age, and is approximately 8.6-9.5 hours in pediatric patients 6-12 years of age and 10-11.3 hours in adults for dextroamphetamine.
USES: Lisdexamfetamine is used to treat attention deficit hyperactivity disorder (ADHD) as part of a total treatment plan, including psychological, social, and other treatments. It may help to increase the ability to pay attention, stay focused, and stop fidgeting. Lisdexamfetamine may also be used to treat binge eating disorder (BED).
It may help to reduce the number of binge eating days. This medication is a stimulant. It is thought to work by restoring the balance of certain natural chemicals (neurotransmitters) in the brain.
This medication is not recommended for use for weight loss due to the risk of serious side effects.
Generic name: lisdexamfetamine dimesylate
Pronunciation: (lis-DEX-am-FET-a-meen)
Drug class: Amphetamines/Anorexiants/Stimulants
Therapeutic class: Central Nervous System Agents
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Lisdexamfetamine Dimesylate
Indications
The following indications are listed for Lisdexamfetamine Dimesylate:
- Attention-Deficit Hyperactivity Disorder
- Binge Eating Disorder
Also known as: Add With Hyperactivity.
Dosing
Available as lisdexamfetamine dimesylate; dosage expressed in terms of the salt.
No dosing information is available for this tab.
| Drug label | Dosing type | Instructions |
|---|---|---|
| Lisdexamfetamine 10 Mg Tb Chew | Maintenance | Chew 1 tablet (10 mg) by oral route once daily in the morning. |
| Lisdexamfetamine 20 Mg Tb Chew | Maintenance | Chew 1 tablet (20 mg) by oral route once daily in the morning. |
| Lisdexamfetamine 30 Mg Tb Chew | Maintenance | Chew 1 tablet (30 mg) by oral route once daily in the morning. |
| Lisdexamfetamine 40 Mg Tb Chew | Maintenance | Chew 1 tablet (40 mg) by oral route once daily in the morning. |
| Lisdexamfetamine 50 Mg Tb Chew | Maintenance | Chew 1 tablet (50 mg) by oral route once daily in the morning. |
| Lisdexamfetamine 60 Mg Tb Chew | Maintenance | Chew 1 tablet (60 mg) by oral route once daily in the morning. |
| Lisdexamfetamine 10 Mg Capsule | Maintenance | Take 1 capsule (10 mg) by oral route once daily in the morning. |
| Lisdexamfetamine 20 Mg Capsule | Maintenance | Take 1 capsule (20 mg) by oral route once daily in the morning. |
| Lisdexamfetamine 30 Mg Capsule | Maintenance | Take 1 capsule (30 mg) by oral route once daily in the morning. |
| Lisdexamfetamine 40 Mg Capsule | Maintenance | Take 1 capsule (40 mg) by oral route once daily in the morning. |
| Lisdexamfetamine 50 Mg Capsule | Maintenance | Take 1 capsule (50 mg) by oral route once daily in the morning. |
| Lisdexamfetamine 60 Mg Capsule | Maintenance | Take 1 capsule (60 mg) by oral route once daily in the morning. |
| Lisdexamfetamine 70 Mg Capsule | Maintenance | Take 1 capsule (70 mg) by oral route once daily in the morning. |
| Drug label | Dosing type | Instructions |
|---|---|---|
| Lisdexamfetamine 20 Mg Capsule | Maintenance | Take 1 capsule (20 mg) by oral route once daily in the morning. |
| Lisdexamfetamine 30 Mg Capsule | Maintenance | Take 1 capsule (30 mg) by oral route once daily in the morning. |
| Lisdexamfetamine 40 Mg Capsule | Maintenance | Take 1 capsule (40 mg) by oral route once daily in the morning. |
| Lisdexamfetamine 50 Mg Capsule | Maintenance | Take 1 capsule (50 mg) by oral route once daily in the morning. |
| Lisdexamfetamine 60 Mg Capsule | Maintenance | Take 1 capsule (60 mg) by oral route once daily in the morning. |
| Lisdexamfetamine 70 Mg Capsule | Maintenance | Take 1 capsule (70 mg) by oral route once daily in the morning. |
| Lisdexamfetamine 10 Mg Capsule | Maintenance | Take 1 capsule (10 mg) by oral route once daily in the morning. |
| Lisdexamfetamine 10 Mg Tb Chew | Maintenance | Chew 1 tablet (10 mg) by oral route once daily in the morning. |
| Lisdexamfetamine 20 Mg Tb Chew | Maintenance | Chew 1 tablet (20 mg) by oral route once daily in the morning. |
| Lisdexamfetamine 30 Mg Tb Chew | Maintenance | Chew 1 tablet (30 mg) by oral route once daily in the morning. |
| Lisdexamfetamine 40 Mg Tb Chew | Maintenance | Chew 1 tablet (40 mg) by oral route once daily in the morning. |
| Lisdexamfetamine 50 Mg Tb Chew | Maintenance | Chew 1 tablet (50 mg) by oral route once daily in the morning. |
| Lisdexamfetamine 60 Mg Tb Chew | Maintenance | Chew 1 tablet (60 mg) by oral route once daily in the morning. |
Drug interactions
There is no enhanced messaging for this drug.
Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient.
Mixed & Indirect Sympathomimetics; Oral Phenylephrine/Maois
SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient.
MECHANISM OF ACTION: Catecholamine stores increased by MAOIs can be released by indirect acting sympathomimetics such as ephedrine and amphetamine. MAO inhibitors also interfere with gut and liver metabolism of direct acting sympathomimetics (e.g oral phenylephrine).
CLINICAL EFFECTS: Concurrent use of MAOIs may result in potentiation of sympathomimetic effects, which may result in headaches, hypertensive crisis, toxic neurological effects, and malignant hyperpyrexia. Fatalities have occurred.
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: Concurrent use of monoamine oxidase inhibitors and sympathomimetics is contraindicated. The manufacturers of sympathomimetic agents recommend waiting 14 days after discontinuation of MAO inhibitors before initiating the sympathomimetic.
DISCUSSION: Indirect acting sympathomimetic amines may cause abrupt elevation of blood pressure when administered to patients taking monoamine oxidase inhibitors, resulting in a potentially fatal hypertensive crisis. Mixed (direct and indirect) acting sympathomimetics have also been shown to interact with monoamine oxidase inhibitors depending on their degree of indirect action. The direct-acting sympathomimetics have not been reported to interact. Dopamine is metabolized by monoamine oxidase, and its pressor effect is enhanced by monoamine oxidase inhibitors. Linezolid is another antibacterial with monoamine oxidase inhibitor properties. Metaxalone is a weak inhibitor of MAO. Foods containing large amounts of tyramine have also been implicated in this interaction. Methylene blue, when administered intravenously, has been shown to reach sufficient concentrations to be a potent inhibitor of MAO-A. At recommended dosages, rasagiline, oral selegiline, and transdermal selegiline up to 6mg/day are selective for MAO-B; however, at higher dosages they have been shown to lose their selectivity. One or more of the drug pairs linked to this monograph have been included in a list of interactions that should be considered "high-priority" for inclusion and should not be inactivated in EHR systems. This DDI subset was vetted by an expert panel commissioned by the U.S. Office of the National Coordinator (ONC) for Health Information Technology.
Serotonergic Agents/Dapoxetine
SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient.
MECHANISM OF ACTION: Concurrent administration of dapoxetine with other serotonergic agents may result in additive effects on serotonin, resulting in serotonin syndrome.(1,2)
CLINICAL EFFECTS: Concurrent use of dapoxetine with other serotonergic agents may result in serotonin syndrome, a potentially life-threatening syndrome which may include one or more of the following symptoms: tremor, agitation, diaphoresis, hyperreflexia, clonus, tachycardia, hyperthermia, and muscle rigidity.(3)
PREDISPOSING FACTORS: Use of multiple drugs which increase serotonin levels is associated with an increased risk for this toxidrome.
PATIENT MANAGEMENT: Dapoxetine should not be administered with other serotonergic agents such as the selective serotonin reuptake inhibitors (SSRIs), serotonin-norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants (TCAs), L-tryptophan, triptans, tramadol, lithium, and/or St. John's Wort.(1,2) Dapoxetine should not be initiated within 14 days of receiving other serotonergic agents. Other serotonergics should not be initiated within 7 days of receiving dapoxetine.(2)
DISCUSSION: This interaction is based on class labeling for these agents. Although there is no clinical documentation for an interaction between dapoxetine and either the elective serotonin reuptake inhibitors (SSRIs), serotonin-norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants (TCAs), L-tryptophan, triptans, tramadol, lithium, and/or St. John's Wort, caution is still warranted. This syndrome has been reported with the selective serotonin reuptake inhibitors and other serotonergic agents, including sumatriptan and dihydroergotamine.
Sympathomimetics/Dihydroergotamine
SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient.
MECHANISM OF ACTION: Concurrent use of dihydroergotamine and sympathomimetics may result in additive or synergistic effect on peripheral blood vessels.(1)
CLINICAL EFFECTS: Concurrent use of dihydroergotamine and sympathomimetics may result in increased blood pressure due to peripheral vasoconstriction.(1)
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: Dihydroergotamine is contraindicated with sympathomimetics because the combination may result in additive or synergistic elevation of blood pressure.(1)
DISCUSSION: Significant elevation in blood pressure has been reported in patients treated with dihydroergotamine.(1) Sympathomimetics can be expected to have additional effects on blood pressure.
Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
Agents That Affect Catecholamines/Iobenguane I 123
SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
MECHANISM OF ACTION: Many compounds that reduce catecholamine uptake or that deplete catecholamine stores may interfere with iobenguane uptake into cells.(1)
CLINICAL EFFECTS: Compounds that reduce catecholamine uptake or that deplete catecholamine stores may interfere with imaging completed with iobenguane.(1)
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: Discuss the use of agents that affect catecholamines. Discontinue drugs that reduce catecholamine uptake or deplete catecholamine stores prior to imaging with iobenguane. Before imaging with iobenguane, discontinue agents that affect catecholamines for at least 5 biological half-lives, as clinically tolerated.(1)
DISCUSSION: Many agents may reduce catecholamine uptake or deplete catecholamine stores.(1) Examples include: - CNS stimulants or amphetamines (e.g. cocaine, methylphenidate, dextroamphetamine) - norepinephrine and dopamine reuptake inhibitors (e.g. phentermine) - norepinephrine and serotonin reuptake inhibitors (e.g. tramadol) - monoamine oxidase inhibitors (e.g. phenelzine, linezolid) - central monoamine depleting drugs (e.g. reserpine) - non-select beta adrenergic blocking drugs (e.g. labetalol) - alpha agonists or alpha/beta agonists (e.g. pseudoephedrine, phenylephrine, ephedrine, phenylpropanolamine, naphazoline) - tricyclic antidepressants or norepinephrine reuptake inhibitors (e.g. amitriptyline, bupropion, duloxetine, mirtazapine, venlafaxine) - botanicals that may inhibit reuptake of norepinephrine, serotonin or dopamine (e.g. ephedra, ma huang, St. John's Wort, yohimbine)
Agents That Affect Catecholamines/Iobenguane I 131
SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
MECHANISM OF ACTION: Many compounds that reduce catecholamine uptake or that deplete catecholamine stores may interfere with iobenguane uptake into cells.(1)
CLINICAL EFFECTS: Compounds that reduce catecholamine uptake or that deplete catecholamine stores may impact the dosimetry calculations or effectiveness of iobenguane.(1)
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: Discuss the use of agents that affect catecholamines. Discontinue drugs that reduce catecholamine uptake or deplete catecholamine stores for at least 5 half-lives before administration of either the dosimetry or a therapeutic dose of iobenguane. Do not administer these drugs until at least 7 days after each iobenguane dose.(1)
DISCUSSION: Many agents may reduce catecholamine uptake or deplete catecholamine stores.(1) Examples include: - CNS stimulants or amphetamines (e.g. cocaine, methylphenidate, dextroamphetamine) - norepinephrine and dopamine reuptake inhibitors (e.g. phentermine) - norepinephrine and serotonin reuptake inhibitors (e.g. tramadol) - monoamine oxidase inhibitors (e.g. phenelzine, linezolid) - central monoamine depleting drugs (e.g. reserpine) - non-select beta adrenergic blocking drugs (e.g. labetalol) - alpha agonists or alpha/beta agonists (e.g. pseudoephedrine, phenylephrine, ephedrine, phenylpropanolamine, naphazoline) - tricyclic antidepressants or norepinephrine reuptake inhibitors (e.g. amitriptyline, bupropion, duloxetine, mirtazapine, venlafaxine) - botanicals that may inhibit reuptake of norepinephrine, serotonin or dopamine (e.g. ephedra, ma huang, St. John's Wort, yohimbine) - calcium channel blockers
Mixed & Indirect Sympathomimet; Oral Phenylephrine/Slt Maois
SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
MECHANISM OF ACTION: Catecholamine stores increased by MAOIs can be released by indirect acting sympathomimetics such as ephedrine and amphetamine. MAO inhibitors also interfere with gut and liver metabolism of direct acting sympathomimetics (e.g oral phenylephrine).
CLINICAL EFFECTS: Concurrent use of MAOIs may result in potentiation of sympathomimetic effects, which may result in headaches, hypertensive crisis, toxic neurological effects, and malignant hyperpyrexia. Fatalities have occurred with combinations of sympathomimetics and MAO-A inhibitors.
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: Concurrent use of MAO-A inhibitors and sympathomimetics is contraindicated. The manufacturers of sympathomimetic agents recommend waiting 14 days after discontinuation of MAO inhibitors before initiating the sympathomimetic. Patients receiving indirect acting sympathomimetics should not receive linezolid unless they are monitored for potential increases in blood pressure. Initial dosages of dopamine should be reduced. At recommended dosages, oral selegiline and transdermal selegiline up to 6mg/day are selective for MAO-B; however, at higher dosages they have been shown to lose their selectivity. Patients receiving higher dosages of selegiline should be considered susceptive to this interaction.
DISCUSSION: Indirect acting sympathomimetic amines may cause abrupt elevation of blood pressure when administered to patients taking monoamine oxidase inhibitors, resulting in a potentially fatal hypertensive crisis. Mixed (direct and indirect) acting sympathomimetics have also been shown to interact with monoamine oxidase inhibitors depending on their degree of indirect action. The direct-acting sympathomimetics have not been reported to interact. Dopamine is metabolized by monoamine oxidase, and its pressor effect is enhanced by monoamine oxidase inhibitors. Foods containing large amounts of tyramine have also been implicated in this interaction. A significant pressor response was observed in normal subjects receiving linezolid and tyramine doses of more than 100 mg. Administration of linezolid (600 mg BID for 3 days) with pseudoephedrine (60 mg q 4 hours for 2 doses) increased blood pressure by 32 mmHg. Administration of linezolid (600 mg BID for 3 days) with phenylpropanolamine (25 mg q 4 hours for 2 doses) increased blood pressure by 38 mmHg. One or more of the drug pairs linked to this monograph have been included in a list of interactions that should be considered "high-priority" for inclusion and should not be inactivated in EHR systems. This DDI subset was vetted by an expert panel commissioned by the U.S. Office of the National Coordinator (ONC) for Health Information Technology.
Mixed & Indirect Sympathomimet;Oral Phenylephrine/Rasagiline
SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
MECHANISM OF ACTION: Catecholamine stores increased by MAOIs can be released by indirect acting sympathomimetics such as ephedrine and amphetamine. MAO inhibitors also interfere with gut and liver metabolism of direct acting sympathomimetics (e.g oral phenylephrine).
CLINICAL EFFECTS: Concurrent use of MAOIs may result in potentiation of sympathomimetic effects, which may result in headaches, hypertensive crisis, toxic neurological effects, and malignant hyperpyrexia. Hypertensive crisis has been reported in patients taking recommended doses of rasagiline with sympathomimetic agents.
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: At recommended dosages, rasagiline is selective for MAO-B; however, at higher dosages it has been shown to lose its selectivity. Patients receiving higher dosages of rasagiline should be considered susceptive to this interaction. Concurrent use should be approached with caution.
DISCUSSION: Indirect acting sympathomimetic amines may cause abrupt elevation of blood pressure when administered to patients taking monoamine oxidase inhibitors, resulting in a potentially fatal hypertensive crisis. Mixed (direct and indirect) acting sympathomimetics have also been shown to interact with monoamine oxidase inhibitors depending on their degree of indirect action. The direct-acting sympathomimetics have not been reported to interact. Dopamine is metabolized by monoamine oxidase, and its pressor effect is enhanced by monoamine oxidase inhibitors.
Select Indirect-Acting Sympathomimetics/Tricyclic Compounds
SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
MECHANISM OF ACTION: Unknown. However, it is speculated that indirect-acting sympathomimetics would have decreased activity due to tricyclic blockage of their uptake into the adrenergic neuron.
CLINICAL EFFECTS: Decreased effect of indirect acting sympathomimetics.
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: Use of tricyclic compounds and indirect-acting sympathomimetics should be approached with caution. Monitor patients receiving concurrent therapy for decreased sympathomimetic efficacy.
DISCUSSION: The pressor effects of the indirect-acting sympathomimetic amines (e.g., amphetamines, ephedrine, and methylphenidate) are antagonized by tricyclic antidepressants.
Sympathomimetics (INDIRECT ACTING)/Guanethidine
SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
MECHANISM OF ACTION: Indirect-acting sympathomimetics may displace guanethidine from adrenergic neurons, thereby antagonizing the clinical effect.
CLINICAL EFFECTS: Blood pressure may be increased.
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: When possible, use an alternative antihypertensive agent or sympathomimetic.
DISCUSSION: This interaction has been demonstrated with concomitant administration of anorexiant-type indirect-acting sympathomimetics and guanethidine. Increased blood pressure has been reported.
Sympathomimetics/Ergot Alkaloids
SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
MECHANISM OF ACTION: Concurrent use of ergot alkaloids and sympathomimetics may result in additive or synergistic effect on peripheral blood vessels.
CLINICAL EFFECTS: Concurrent use of ergot alkaloids and sympathomimetics may result in increased blood pressure due to peripheral vasoconstriction.
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: When possible, avoid the concurrent use of ergot alkaloids and sympathomimetics. If concurrent use is warranted, monitor blood pressure and for signs of vasoconstriction. Decreasing the dose of one or both drugs may be necessary.
DISCUSSION: There have been reports of severe vasoconstriction resulting in gangrene in patients receiving intravenous ergonovine with dopamine or norepinephrine.
Sympathomimetics/Selected Inhalation Anesthetic Agents
SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
MECHANISM OF ACTION: The exact mechanism is unknown. The anesthetics produce conduction changes that increase impulse re-entry into the myocardial tissue.(1) The anesthetics' ability to precipitate arrhythmias is enhanced by elevated arterial blood pressure, tachycardia, hypercapnia, and/or hypoxia, events that stimulate the release of endogenous catecholamines.(1)
CLINICAL EFFECTS: Concurrent use of inhalation anesthetic agents and sympathomimetics may result in ventricular arrhythmias or sudden blood pressure and heart rate increase during surgery.(2)
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: Monitor blood pressure and avoid use of sympathomimetics in patients being treated with anesthetics on the day of surgery.(2) Intravenous use of epinephrine during surgery with halothane and related halogenated general anesthetics should be strongly discouraged. When intravenous epinephrine is necessary, nitrous oxide anesthesia supplemented with ether, muscle relaxants, or opioids should be used instead of halothane.(3,4) Epinephrine may safely be used subcutaneously with the following precautions: the patient is adequately ventilated to prevent hypoxia or respiratory acidosis; the total dose of epinephrine is limited to 100 mcg/10 minute period or 300 mcg/hour in adults, 3.5 mcg/Kg in infants, 2.5 mcg/Kg in children up to two years of age, and 1.45 mcg/Kg in children over two years of age; a minimum effective concentration of anesthetic is maintained; the drugs are not co-administered in patients with hypertension or other cardiovascular disorders; and the cardiac rhythm is continuously monitored during and after injection.(3-10) If arrhythmias occur after the administration of the epinephrine, the drugs of choice are lidocaine or propranolol, depending on the type of arrhythmia.(1)
DISCUSSION: Administration of epinephrine during halothane anesthesia may may lead to serious ventricular arrhythmias.(3-6,11-18) This has occurred when epinephrine was administered intravenously,(6) when it was administered with lidocaine as a dental block,(11,14) or when it was administered supraperiosteally.(5) Norepinephrine has been shown to interact with halothane in a manner similar to epinephrine.(1) In two case reports, patients were given terbutaline (0.25 to 0.35 mg) for wheezing following induction of anesthesia with halothane. One patient's heart rate increased from 68 to 100 beats/minute, and the ECG showed premature ventricular contractions and bigeminy, while the other patient developed multiple unifocal premature ventricular contractions and bigeminy. The arrhythmias resolved in both patients following lidocaine administration.(19) Although not documented, isoproterenol causes effects on the heart similar to terbutaline(20) and would probably interact with halothane in a similar manner. Other inhalation anesthetics that increase the incidence of arrhythmias with epinephrine include chloroform,(20) methoxyflurane,(20) and enflurane.(12) A similar interaction may be expected between the other inhalation anesthetics and sympathomimetics.
Moderate Interaction: Assess the risk to the patient and take action as needed.
Amphetamines/Meperidine
SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed.
MECHANISM OF ACTION: Opioids and stimulants exhibit opposing effects on the CNS.(1) Amphetamines may affect serotonin release and/or reuptake, depending on their molecular structure. Ring substitution tends to increase amphetamine-induced release of endogenous serotonin. However, the effect on serotonin release may also be dose related and is more likely if the amphetamine is taken in doses greater than those approved and generally employed in treating attention-deficit-hyperactivity-disorder, or if abused, especially over long periods of time.(1) Meperidine blocks serotonin reuptake. Concurrent administration of amphetamines with meperidine may produce additive effects on serotonin, resulting in serotonin syndrome.(2,3)
CLINICAL EFFECTS: Opposing CNS effects of opioids and stimulants may compromise the effectiveness of both agents and mask opioid overdose symptoms such as drowsiness and inability to focus. Concurrent use of amphetamines with meperidine may increase the risk of serotonin syndrome, a potentially life-threatening syndrome which may include one or more of the following symptoms: tremor, agitation, diaphoresis, hyperreflexia, clonus, tachycardia, hyperthermia, and muscle rigidity.(4)
PREDISPOSING FACTORS: Concurrent use of alcohol or other CNS depressants may increase the risk of adverse effects. High doses or long-term abuse of amphetamines may increase the risk of this interaction. Renal dysfunction and chronic use of meperidine would also be expected to increase the risk for serotonin toxicity. Use of multiple drugs which increase serotonin levels is associated with an increased risk for this toxidrome.
PATIENT MANAGEMENT: Limit prescribing meperidine with CNS stimulants such as amphetamines to patients for whom alternatives are ineffective, not tolerated, or would be otherwise inadequate to provide sufficient management of pain.(1) Concurrent use of amphetamines with meperidine should be approached with appropriate monitoring, especially during therapy initiation and dose increase. Instruct patients receiving concurrent therapy to report any signs or symptoms of serotonin syndrome immediately. Consider initiating amphetamines or meperidine at lower doses and monitor for signs and symptoms of serotonin syndrome. Discontinue one or both medications if symptoms occur. Respiratory depression can occur at any time during opioid therapy, especially during therapy initiation and following dosage increases. The risk of opioid-related overdose or overdose-related death is increased with higher opioid doses, and this risk persists over the course of therapy. Consider these risks when using concurrently with stimulants. Monitor patients receiving concurrent therapy for unusual dizziness or lightheadedness, extreme sleepiness, slowed or difficult breathing, or unresponsiveness.(1) Discuss opioid reversal agents (e.g., naloxone, nalmefene) to patients when prescribing or renewing an opioid analgesic or medicine to treat opioid use disorder (OUD). Consider prescribing opioid reversal agents (e.g., naloxone, nalmefene) to patients prescribed medicines to treat OUD or opioid analgesics who are at increased risk of opioid overdose (such as those taking CNS depressants) and when a patient has household members/close contacts at risk for accidental overdose. Discuss the options for obtaining an opioid reversal agent (e.g., prescription, over-the-counter, or as part of a community-based program).(1) Monitor patients receiving concurrent therapy for signs of substance abuse.
DISCUSSION: A total of 70,237 persons died from drug overdoses in the United States in 2017; approximately two thirds of these deaths involved an opioid.(2). The CDC analyzed 2016-2017 changes in age-adjusted death rates involving cocaine and psychostimulants by demographic characteristics, urbanization levels, U.S. Census region, 34 states, and the District of Columbia (DC). The CDC also examined trends in age-adjusted cocaine-involved and psychostimulant-involved death rates from 2003 to 2017 overall, as well as with and without co-involvement of opioids. Among all 2017 drug overdose deaths, 13,942 (19.8%) involved cocaine, and 10,333 (14.7%) involved psychostimulants. Death rates increased from 2016 to 2017 for both drug categories across demographic characteristics, urbanization levels, Census regions, and states. In 2017, opioids were involved in 72.7% and 50.4% of cocaine-involved and psychostimulant-involved overdoses, respectively, and the data suggest that increases in cocaine-involved overdose deaths from 2012 to 2017 were driven primarily by synthetic opioids.(7) There was opioid co-involvement in 72.7 percent of cocaine and 50.4 percent of stimulant-involved overdose deaths. This was largely driven by synthetic opioids such as fentanyl. However, stimulant-involved overdose without opioid co-involvement is also increasing.(6)
Amphetamines/Tramadol
SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed.
MECHANISM OF ACTION: Opioids and stimulants exhibit opposing effects on the CNS.(1) Amphetamines may affect serotonin release and/or reuptake, depending on their molecular structure. Ring substitution tends to increase amphetamine-induced release of endogenous serotonin. However, the effect on serotonin release may also be dose related and is more likely if the amphetamine is taken in doses greater than those approved and generally employed in treating attention-deficit-hyperactivity-disorder, or if abused, especially over long periods of time.(2) Concurrent administration of amphetamines with tramadol may result in additive effects on serotonin, resulting in serotonin syndrome.(3,4)
CLINICAL EFFECTS: Opposing CNS effects of opioids and stimulants may compromise the effectiveness of both agents and mask opioid overdose symptoms such as drowsiness and inability to focus. Concurrent use of amphetamines with other serotonergic agents may increase the risk of serotonin syndrome, a potentially life-threatening syndrome which may include one or more of the following symptoms: tremor, agitation, diaphoresis, hyperreflexia, clonus, tachycardia, hyperthermia, and muscle rigidity.(5)
PREDISPOSING FACTORS: Concurrent use of alcohol or other CNS depressants may increase the risk of adverse effects. High doses or long-term abuse of amphetamines may increase the risk of serotonin syndrome. Use of multiple drugs which increase serotonin levels is associated with an increased risk for this toxidrome.
PATIENT MANAGEMENT: Limit prescribing tramadol with CNS stimulants such as amphetamines to patients for whom alternatives are ineffective, not tolerated, or would be otherwise inadequate to provide sufficient management of pain. If concurrent use is necessary, limit the dosages and duration of each drug to the minimum possible while achieving the desired clinical effect. Consider initiating amphetamines or tramadol at lower doses and monitor for signs and symptoms of serotonin syndrome. Concurrent use of amphetamines with tramadol should be approached with appropriate monitoring. Discontinue medication if symptoms occur.(3,4) Instruct patients receiving concurrent therapy to report any signs or symptoms of serotonin syndrome immediately. Monitor patients receiving concurrent therapy for signs of substance abuse. Respiratory depression can occur at any time during opioid therapy, especially during therapy initiation and following dosage increases. The risk of opioid-related overdose or overdose-related death is increased with higher opioid doses, and this risk persists over the course of therapy. Consider these risks when using concurrently with stimulants.(1) Discuss opioid reversal agents (e.g., naloxone, nalmefene) with all patients when prescribing or renewing an opioid analgesic or medicine to treat opioid use disorder (OUD). Consider prescribing opioid reversal agents (e.g., naloxone, nalmefene) to patients prescribed medicines to treat OUD or opioid analgesics who are at increased risk of opioid overdose (such as those taking CNS depressants) and when a patient has household members/close contacts at risk for accidental overdose. Discuss the options for obtaining an opioid reversal agent (e.g., prescription, over-the-counter, or as part of a community-based program).(1)
DISCUSSION: A total of 70,237 persons died from drug overdoses in the United States in 2017; approximately two thirds of these deaths involved an opioid.(2). The CDC analyzed 2016-2017 changes in age-adjusted death rates involving cocaine and psychostimulants by demographic characteristics, urbanization levels, U.S. Census region, 34 states, and the District of Columbia (DC). The CDC also examined trends in age-adjusted cocaine-involved and psychostimulant-involved death rates from 2003 to 2017 overall, as well as with and without co-involvement of opioids. Among all 2017 drug overdose deaths, 13,942 (19.8%) involved cocaine, and 10,333 (14.7%) involved psychostimulants. Death rates increased from 2016 to 2017 for both drug categories across demographic characteristics, urbanization levels, Census regions, and states. In 2017, opioids were involved in 72.7% and 50.4% of cocaine-involved and psychostimulant-involved overdoses, respectively, and the data suggest that increases in cocaine-involved overdose deaths from 2012 to 2017 were driven primarily by synthetic opioids.(7) There was opioid co-involvement in 72.7 percent of cocaine and 50.4 percent of stimulant-involved overdose deaths. This was largely driven by synthetic opioids such as fentanyl. However, stimulant-involved overdose without opioid co-involvement is also increasing.(6)
Amphetamines; Phentermine/Ssris; Snris
SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed.
MECHANISM OF ACTION: Amphetamines may affect serotonin release and/or reuptake, depending on their molecular structure. Ring substitution tends to increase amphetamine-induced release of endogenous serotonin. However, the effect on serotonin release may also be dose related and is more likely if the amphetamine is taken in doses greater than those approved and generally employed in treating Attention-deficit-hyperactivity-disorder, or if abused, especially over long periods of time.(1) Amphetamines, phentermine and serotonin-norepinephrine reuptake inhibitors(SNRIs) may have additive effects on blood pressure.
CLINICAL EFFECTS: Concurrent use of amphetamines with agents that affect serotonin may increase the risk of serotonin syndrome. Symptoms of serotonin syndrome may include tremor, agitation, diaphoresis, hyperreflexia, clonus, tachycardia, hyperthermia, and muscle rigidity.(8) Concurrent use of amphetamines or phentermine and a SNRI may increase the risk for high blood pressure or make hypertension more difficult to control. SSRIs and SNRIs linked to this monograph are: citalopram, desvenlafaxine, duloxetine, escitalopram, fluoxetine, fluvoxamine, levomilnacipran, milnacipran, paroxetine, sertraline, venlafaxine, vilazodone and vortioxetine.
PREDISPOSING FACTORS: High doses or long-term abuse of amphetamines may increase the risk of this interaction.
PATIENT MANAGEMENT: The concurrent use of amphetamines with SSRIs or SNRIs should be approached with appropriate monitoring. Instruct patients receiving concurrent therapy to report any signs or symptoms of serotonin syndrome immediately. Monitor blood pressure during concurrent therapy and adjust dosage or change medication for persistent increases in blood pressure. If concurrent therapy is warranted, patients should be monitored for signs and symptoms of serotonin syndrome. Instruct patients to report muscle twitching, tremors, shivering and stiffness, fever, heavy sweating, heart palpitations, restlessness, confusion, agitation, trouble with coordination, or severe diarrhea.
DISCUSSION: In a case report, a 13 year-old female experienced tachycardia when amphetamine was added to her sertraline regimen.(2) Increased side effects have also been reported in patients maintained on fluoxetine who ingested illicit amphetamines.(3) In a case report, a 22 year-old female had previously been taking phentermine and oral contraceptive agents. The patient stopped taking phentermine and, after an undetermined length of time, started taking fluoxetine (20 mg daily). The patient discontinued her fluoxetine after three months. Eight days later, she took one dose of phentermine (30 mg). Within several hours, she developed jitteriness, stomach cramps, dry eyes, palpitations, and tremors. The patient received once dose of lorazepam (1.5 mg) and her symptoms resolved over night.(4) In a case report, a 32 year-old male developed agitation, anxiety, shivering, tremors, and diaphoresis two weeks after adding venlafaxine to his dexamphetamine.(5) There have also been reports of safe and effective use of amphetamines with fluoxetine,(6) dextroamphetamine and sertraline,(6) and dextroamphetamine with fluoxetine.(7)
Selected Stimulants/Benzodiazepines
SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed.
MECHANISM OF ACTION: Benzodiazepines and stimulants exhibit opposing effects on the CNS.
CLINICAL EFFECTS: Concurrent use of benzodiazepines and stimulants may reduce the clinical effectiveness of both the benzodiazepine and the stimulant. In addition, concurrent use may mask overdose symptoms of the benzodiazepine, such as drowsiness and inability to focus.
PREDISPOSING FACTORS: Concurrent use of alcohol or other CNS depressants may increase the risk of adverse effects.
PATIENT MANAGEMENT: Limit prescribing benzodiazepines with CNS stimulants such as amphetamines to patients for whom alternatives are inadequate. If concurrent use is necessary, limit the dosages and duration of each drug to the minimum possible while achieving the desired clinical effect. Monitor patients receiving concurrent therapy for signs of substance abuse.
DISCUSSION: Analysis of the 2015 and 2016 National Survey on Drug Use and Health found that misuse of benzodiazepines was strongly associated with misuse of or dependences on stimulants.(1) Benzodiazepines are used to reduce the adverse effects of stimulant use, such as insomnia.(2) Patients abusing benzodiazepines in combination with other drugs tend to consume higher dosages of benzodiazepines than patients abusing only benzodiazepines.(3)
Selected Stimulants/Opioids (COUGH & COLD)
SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed.
MECHANISM OF ACTION: Opioids and stimulants exhibit opposing effects on the CNS.
CLINICAL EFFECTS: Opposing CNS effects of opioids and stimulants may compromise the effectiveness of both agents and mask opioid overdose symptoms such as drowsiness and inability to focus.
PREDISPOSING FACTORS: Concurrent use of alcohol or other CNS depressants may increase the risk of adverse effects.
PATIENT MANAGEMENT: Limit prescribing opioid analgesics with CNS stimulants such as amphetamines to patients for whom alternatives are ineffective, not tolerated, or would be otherwise inadequate to provide sufficient management of pain. If concurrent use is necessary, limit the dosages and duration of each drug to the minimum possible while achieving the desired clinical effect. Respiratory depression can occur at any time during opioid therapy, especially during therapy initiation and following dosage increases. The risk of opioid-related overdose or overdose-related death is increased with higher opioid doses, and this risk persists over the course of therapy. Consider these risks when using concurrently with other agents that may cause CNS depression.(1) Monitor patients receiving concurrent therapy for signs of substance abuse. Monitor patients receiving concurrent therapy for unusual dizziness or lightheadedness, extreme sleepiness, slowed or difficult breathing, or unresponsiveness. Discuss opioid reversal agents (e.g., naloxone, nalmefene) with all patients when prescribing or renewing an opioid analgesic or medicine to treat opioid use disorder (OUD). Consider prescribing opioid reversal agents (e.g., naloxone, nalmefene) to patients prescribed medicines to treat OUD or opioid analgesics who are at increased risk of opioid overdose (such as those taking CNS depressants) and when a patient has household members/close contacts at risk for accidental overdose. Discuss the options for obtaining an opioid reversal agent (e.g., prescription, over-the-counter, or as part of a community-based program).
DISCUSSION: A total of 70,237 persons died from drug overdoses in the United States in 2017; approximately two thirds of these deaths involved an opioid.(2). The CDC analyzed 2016-2017 changes in age-adjusted death rates involving cocaine and psychostimulants by demographic characteristics, urbanization levels, U.S. Census region, 34 states, and the District of Columbia (DC). The CDC also examined trends in age-adjusted cocaine-involved and psychostimulant-involved death rates from 2003 to 2017 overall, as well as with and without co-involvement of opioids. Among all 2017 drug overdose deaths, 13,942 (19.8%) involved cocaine, and 10,333 (14.7%) involved psychostimulants. Death rates increased from 2016 to 2017 for both drug categories across demographic characteristics, urbanization levels, Census regions, and states. In 2017, opioids were involved in 72.7% and 50.4% of cocaine-involved and psychostimulant-involved overdoses, respectively, and the data suggest that increases in cocaine-involved overdose deaths from 2012 to 2017 were driven primarily by synthetic opioids.(3) There was opioid co-involvement in 72.7 percent of cocaine and 50.4 percent of stimulant-involved overdose deaths. This was largely driven by synthetic opioids such as fentanyl. However, stimulant-involved overdose without opioid co-involvement is also increasing.(2)
Selected Stimulants/Opioids (EXTENDED RELEASE)
SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed.
MECHANISM OF ACTION: Opioids and stimulants exhibit opposing effects on the CNS.
CLINICAL EFFECTS: Opposing CNS effects of opioids and stimulants may compromise the effectiveness of both agents and mask opioid overdose symptoms such as drowsiness and inability to focus
PREDISPOSING FACTORS: Concurrent use of alcohol or other CNS depressants may increase the risk of adverse effects.
PATIENT MANAGEMENT: Limit prescribing opioid analgesics with CNS stimulants such as amphetamines to patients for whom alternatives are ineffective, not tolerated, or would be otherwise inadequate to provide sufficient management of pain. If concurrent use is necessary, limit the dosages and duration of each drug to the minimum possible while achieving the desired clinical effect. Respiratory depression can occur at any time during opioid therapy, especially during therapy initiation and following dosage increases. The risk of opioid-related overdose or overdose-related death is increased with higher opioid doses, and this risk persists over the course of therapy. Consider these risks when using concurrently with other agents that may cause CNS depression.(1) Monitor patients receiving concurrent therapy for signs of substance abuse. Monitor patients receiving concurrent therapy for unusual dizziness or lightheadedness, extreme sleepiness, slowed or difficult breathing, or unresponsiveness. Discuss opioid reversal agents (e.g., naloxone, nalmefene) with all patients when prescribing or renewing an opioid analgesic or medicine to treat opioid use disorder (OUD). Consider prescribing opioid reversal agents (e.g., naloxone, nalmefene) to patients prescribed medicines to treat OUD or opioid analgesics who are at increased risk of opioid overdose (such as those taking CNS depressants) and when a patient has household members/close contacts at risk for accidental overdose. Discuss the options for obtaining an opioid reversal agent (e.g., prescription, over-the-counter, or as part of a community-based program).
DISCUSSION: A total of 70,237 persons died from drug overdoses in the United States in 2017; approximately two thirds of these deaths involved an opioid.(2). The CDC analyzed 2016-2017 changes in age-adjusted death rates involving cocaine and psychostimulants by demographic characteristics, urbanization levels, U.S. Census region, 34 states, and the District of Columbia (DC). The CDC also examined trends in age-adjusted cocaine-involved and psychostimulant-involved death rates from 2003 to 2017 overall, as well as with and without co-involvement of opioids. Among all 2017 drug overdose deaths, 13,942 (19.8%) involved cocaine, and 10,333 (14.7%) involved psychostimulants. Death rates increased from 2016 to 2017 for both drug categories across demographic characteristics, urbanization levels, Census regions, and states. In 2017, opioids were involved in 72.7% and 50.4% of cocaine-involved and psychostimulant-involved overdoses, respectively, and the data suggest that increases in cocaine-involved overdose deaths from 2012 to 2017 were driven primarily by synthetic opioids.(3) There was opioid co-involvement in 72.7 percent of cocaine and 50.4 percent of stimulant-involved overdose deaths. This was largely driven by synthetic opioids such as fentanyl. However, stimulant-involved overdose without opioid co-involvement is also increasing.(2)
Selected Stimulants/Opioids (IMMEDIATE RELEASE)
SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed.
MECHANISM OF ACTION: Opioids and stimulants exhibit opposing effects on the CNS.
CLINICAL EFFECTS: Opposing CNS effects of opioids and stimulants may compromise the effectiveness of both agents and mask opioid overdose symptoms such as drowsiness and inability to focus.
PREDISPOSING FACTORS: Concurrent use of alcohol or other CNS depressants may increase the risk of adverse effects.
PATIENT MANAGEMENT: Limit prescribing opioid analgesics with CNS stimulants such as amphetamines to patients for whom alternatives are ineffective, not tolerated, or would be otherwise inadequate to provide sufficient management of pain. If concurrent use is necessary, limit the dosages and duration of each drug to the minimum possible while achieving the desired clinical effect. Respiratory depression can occur at any time during opioid therapy, especially during therapy initiation and following dosage increases. The risk of opioid-related overdose or overdose-related death is increased with higher opioid doses, and this risk persists over the course of therapy. Consider these risks when using concurrently with other agents that may cause CNS depression.(1) Monitor patients receiving concurrent therapy for signs of substance abuse. Monitor patients receiving concurrent therapy for unusual dizziness or lightheadedness, extreme sleepiness, slowed or difficult breathing, or unresponsiveness. Discuss opioid reversal agents (e.g., naloxone, nalmefene) with all patients when prescribing or renewing an opioid analgesic or medicine to treat opioid use disorder (OUD). Consider prescribing an opioid reversal agent (e.g., naloxone, nalmefene) to patients prescribed medicines to treat OUD or opioid analgesics who are at increased risk of opioid overdose (such as those taking CNS depressants) and when a patient has household members/close contacts at risk for accidental overdose. Discuss the options for obtaining an opioid reversal agent (e.g., prescription, over-the-counter, or as part of a community-based program).
DISCUSSION: A total of 70,237 persons died from drug overdoses in the United States in 2017; approximately two thirds of these deaths involved an opioid.(2). The CDC analyzed 2016-2017 changes in age-adjusted death rates involving cocaine and psychostimulants by demographic characteristics, urbanization levels, U.S. Census region, 34 states, and the District of Columbia (DC). The CDC also examined trends in age-adjusted cocaine-involved and psychostimulant-involved death rates from 2003 to 2017 overall, as well as with and without co-involvement of opioids. Among all 2017 drug overdose deaths, 13,942 (19.8%) involved cocaine, and 10,333 (14.7%) involved psychostimulants. Death rates increased from 2016 to 2017 for both drug categories across demographic characteristics, urbanization levels, Census regions, and states. In 2017, opioids were involved in 72.7% and 50.4% of cocaine-involved and psychostimulant-involved overdoses, respectively, and the data suggest that increases in cocaine-involved overdose deaths from 2012 to 2017 were driven primarily by synthetic opioids.(3) There was opioid co-involvement in 72.7 percent of cocaine and 50.4 percent of stimulant-involved overdose deaths. This was largely driven by synthetic opioids such as fentanyl. However, stimulant-involved overdose without opioid co-involvement is also increasing.(2)
Serotonergic Agents/Centanafadine
SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed.
MECHANISM OF ACTION: Centanafadine is a norepinephrine, dopamine, and serotonin reuptake inhibitor.(1) Concurrent administration with one or more serotonergic agents may increase serotonin effects, resulting in serotonin toxicity.(1,2)
CLINICAL EFFECTS: Concurrent use of centanafadine with other serotonergic agents may increase the risk of serotonin syndrome, a potentially life-threatening syndrome which may include one or more of the following symptoms: tremor, agitation, diaphoresis, hyperreflexia, clonus, tachycardia, hyperthermia, and muscle rigidity.(1,2)
PREDISPOSING FACTORS: Serotonin syndrome risk is dose-related. Higher systemic concentrations of either drug would be predicted to increase risk for serotonin toxicity.(2) Concomitant therapy with multiple agents which increase brain serotonin concentrations may also increase risk for serotonin syndrome.(2)
PATIENT MANAGEMENT: If concurrent use of centanafadine with other serotonergic agents is clinically warranted, counsel the patient on the increased risk of serotonin syndrome and monitor for symptoms. If symptoms of serotonin syndrome develop, discontinue centanafadine and/or the other serotonergic agents immediately and initiate supportive measures.(1)
DISCUSSION: Centanafadine inhibits reuptake of norepinephrine, dopamine, and serotonin.(1)
Serotonergic Agents/Gepirone
SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed.
MECHANISM OF ACTION: Gepirone is a serotonin receptor agonist. Concurrent administration with one or more serotonergic agents may increase serotonin effects, resulting in serotonin toxicity.(1,2)
CLINICAL EFFECTS: Concurrent use of gepirone with other serotonergic agents may increase the risk of hypertensive crisis and serotonin syndrome, a potentially life-threatening syndrome which may include one or more of the following symptoms: tremor, agitation, diaphoresis, hyperreflexia, clonus, tachycardia, hyperthermia, and muscle rigidity.(1)
PREDISPOSING FACTORS: Serotonin syndrome risk is dose-related. Higher systemic concentrations of either drug would be predicted to increase risk for serotonin toxicity.(2) Concomitant therapy with multiple agents which increase brain serotonin concentrations may also increase risk for serotonin syndrome.(2)
PATIENT MANAGEMENT: If concurrent use of gepirone with other serotonergic agents is clinically warranted, counsel the patient on the increased risk of serotonin syndrome and monitor for symptoms. If symptoms of serotonin syndrome develop, discontinue gepirone and/or the other serotonergic agents immediately and initiate supportive measures.(1)
DISCUSSION: Gepirone and its 3'-OH metabolite act as agonists at 5HT1A receptors. Use with other agents that also increase serotonin in the body must be undertaken with caution and monitored closely due to the risk of serotonin syndrome.(1)
Serotonergic Agents/Ziprasidone
SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed.
MECHANISM OF ACTION: Ziprasidone is a 5-HT1A agonist and serotonin and norepinephrine reuptake inhibitor. Concurrent administration with one or more serotonergic agents may increase serotonin effects, resulting in serotonin toxicity.(1,2)
CLINICAL EFFECTS: Concurrent use of ziprasidone and other serotonergic agents may result in serotonin syndrome, a potentially life-threatening condition with symptoms including altered mental status, hypertension, restlessness, myoclonus, hyperthermia, hyperreflexia, diaphoresis, shivering, and tremor.(1)
PREDISPOSING FACTORS: Serotonin syndrome risk is dose-related. Higher systemic concentrations of either drug would be predicted to increase risk for serotonin toxicity.(2) Concomitant therapy with multiple agents which increase brain serotonin concentrations may also increase risk for serotonin syndrome.(2)
PATIENT MANAGEMENT: Caution patients about the risk of serotonin syndrome with the concomitant use of ziprasidone with other serotonergic drugs. Instruct patients to contact their healthcare provider, or report to the emergency room, should they experience signs or symptoms of serotonin syndrome.(1)
DISCUSSION: Several cases of serotonin syndrome have been reported in patients receiving ziprasidone.(4-6)
Sympathomimetics/Urinary Alkalinizers
SEVERITY LEVEL: 3-Moderate Interaction: Assess the risk to the patient and take action as needed.
MECHANISM OF ACTION: Unionized sympathomimetic amines will be reabsorbed into systemic circulation from the distal tubules of the kidneys.
CLINICAL EFFECTS: Enhanced sympathomimetic activity and increased risk of sympathomimetic toxicity.
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: Watch patient for enhanced sympathomimetic side effects when urinary alkalinizers are concomitantly used. A lower dose of certain sympathomimetics may be required.
DISCUSSION: Signs and symptoms of sympathomimetic toxicity include euphoria, confusion, delirium, hallucinations and nervousness.
Contraindications
*Known hypersensitivity to amphetamines or any ingredient in the formulation of lisdexamfetamine dimesylate. Anaphylactic reactions, hypersensitivity, Stevens-Johnson syndrome, angioedema, and urticaria have been reported during postmarketing surveillance of lisdexamfetamine.
*Concurrent or recent (i.e., within 14 days) therapy with a monoamine oxidase (MAO) inhibitor, including linezolid or IV methylene blue, since hypertensive crisis could result.
- Cardiac arrhythmia
- Congenital heart disease
- Congenital long QT syndrome
- Coronary artery disease
- Prolonged QT interval
- Torsades de pointes
- Valvular heart disease
- Alcohol intoxication
- Alcohol use disorder
- Bipolar disorder
- Cerebrovascular accident
- Chronic heart failure
- Chronic kidney disease stage 4 (severe) GFR 15-29 ml/min
- Chronic kidney disease stage 5 (failure) GFr<15 ml/min
- Depression
- Drug abuse
- Glaucoma
- History of drug abuse
- Hypertension
- Lower seizure threshold
- Manic disorder
- Motor tic disorder
- Pheochromocytoma
- Psychotic disorder
- Seizure disorder
- Suicidal ideation
- Aggressive behavior
- Hyperthyroidism
- Raynaud's phenomenon
Adverse reactions
Adverse effects occurring in >=5% of children, adolescents, or adults receiving lisdexamfetamine for ADHD and at a frequency at least twice that reported with placebo include anorexia, anxiety, decreased appetite, decreased weight, diarrhea, dizziness, dry mouth, irritability, insomnia, nausea, upper abdominal pain, and vomiting.
Adverse effects occurring in >=5% of adults receiving lisdexamfetamine for binge-eating disorder and at a frequency at least twice that reported with placebo include dry mouth, insomnia, decreased appetite, increased heart rate, constipation, jittery feeling, and anxiety.
Less Frequent
- Hypersensitivity drug reaction
Rare or Very Rare
- Acute myocardial infarction
- Anaphylaxis
- Angioedema
- Atrial fibrillation
- Cardiac arrhythmia
- Cardiomyopathy
- Cerebrovascular accident
- Drug-induced psychosis
- Exacerbation of gilles de la tourette's syndrome
- Gastrointestinal vascular ischemia
- Hallucinations
- Hepatitis
- Hypertension
- Priapism
- Rhabdomyolysis
- Seizure disorder
- Stevens-johnson syndrome
- Suicidal ideation
- Toxic epidermal necrolysis
More Frequent
- Anorexia
- False sense of well-being
- Insomnia
- Irritability
- Nausea
- Nervousness
- Symptoms of anxiety
- Upper abdominal pain
- Vomiting
Less Frequent
- Abnormal sexual function
- Acute abdominal pain
- Agitation
- Allergic rhinitis
- Constipation
- Diarrhea
- Dizziness
- Drowsy
- Dysgeusia
- Dyspnea
- Erectile dysfunction
- Fatigue
- Fever
- General weakness
- Headache disorder
- Hostility
- Hyperhidrosis
- Libido changes
- Motor tic disorder
- Palpitations
- Skin rash
- Tachycardia
- Tremor
- Urinary tract infection
- Urticaria
- Weight loss
- Xerostomia
Rare or Very Rare
- Accommodation disorder
- Aggressive behavior
- Alopecia
- Altered mental status
- Blurred vision
- Bruising
- Bruxism
- Chest pain
- Depression
- Diplopia
- Drug dependence
- Dyschromia
- Dysglycemia
- Dyskinesia
- Dysphoric mood
- Epistaxis
- Euphoria
- Excoriation disorder
- Frequent erections
- Livedo reticularis
- Logorrhea
- Manic disorder
- Mood changes
- Muscle spasm
- Mydriasis
- Pain in oropharynx
- Paresthesia
- Peripheral vasoconstriction
- Raynaud's phenomenon
- Syncope
- Tooth disorder
Precautions
No enhanced messaging available.
Safety and efficacy of lisdexamfetamine for the management of ADHD have not been established in children <6 years of age.
Safety and efficacy of lisdexamfetamine for binge-eating disorder have not been established in pediatric patients <18 years of age.
Psychotic (e.g., hallucinations, delusional thinking) or manic symptoms have been reported in children and adolescents receiving stimulants for management of ADHD.
Long-term administration is expected to cause at least a temporary suppression of normal weight and/or height patterns in some children and adolescents.
The National Pregnancy Registry for ADHD Medications monitors outcomes in women exposed to ADHD medications during pregnancy. Clinicians are encouraged to register women who become pregnant while receiving lisdexamfetamine by calling 866-961-2388 or visiting https://womensmentalhealth.org/research/pregnancyregistry/adhd-medications/ .
Data are limited regarding use of lisdexamfetamine dimesylate in pregnant women. Amphetamines may decrease placental perfusion through vasoconstriction, and may stimulate uterine contractions in pregnant women, increasing the risk of premature delivery. Infants born to amphetamine-dependent women have increased risk of prematurity and low birth weight; such infants should be monitored for withdrawal symptoms (e.g., feeding difficulties, irritability, agitation, excessive drowsiness).
In animals, lisdexamfetamine dimesylate had no effects on embryofetal morphology or survival when administered orally to rats and rabbits throughout the period of organogenesis. Prenatal and postnatal studies were not conducted specifically with lisdexamfetamine dimesylate. However, administration of amphetamine to pregnant rats during gestation and lactation resulted in decreased pup survival and body weight that correlated with developmental delays at clinically relevant dosages of amphetamine.
Amphetamine is distributed into human milk based on limited case reports. There are no reports of adverse effects on breast-feeding infants; long-term neurodevelopmental effects from amphetamine exposure are not known. Large dosages of dextroamphetamine may interfere with milk production, especially in women whose lactation is not well established. Because of the potential for serious adverse reactions to lisdexamfetamine in breast-feeding infants (e.g., blood pressure and heart rate increases, growth suppression, peripheral vasculopathy), the manufacturer does not recommend breast-feeding during therapy.
The manufacturer does not provide specific dosage recommendations in geriatric patients; however, dosage in geriatric patients should generally start at the lower end of the dosing range, reflecting the greater incidence of reduced hepatic, renal, or cardiac function, and of concomitant diseases and drug therapies.
Clinical studies of lisdexamfetamine dimesylate did not include sufficient numbers of patients >=65 years of age to determine whether geriatric patients respond differently than younger adults. While other reported clinical experience has not revealed differences in response between geriatric and younger adults, dosage selection in geriatric patients should generally start at the lower end of the dosage range, reflecting the greater frequency of decreased hepatic, renal, and/or cardiac function and of concomitant disease and drug therapy in such patients.
ICD codes
| Code | Type | Description |
|---|---|---|
| Attention-deficit hyperactivity disorder | ||
| F90 | ICD10CM | Attention-deficit hyperactivity disorders |
| F90.0 | ICD10CM | Attention-deficit hyperactivity disorder, predominantly inattentive type |
| F90.1 | ICD10CM | Attention-deficit hyperactivity disorder, predominantly hyperactive type |
| F90.2 | ICD10CM | Attention-deficit hyperactivity disorder, combined type |
| F90.8 | ICD10CM | Attention-deficit hyperactivity disorder, other type |
| F90.9 | ICD10CM | Attention-deficit hyperactivity disorder, unspecified type |
| Binge eating disorder | ||
| F50.020 | ICD10CM | Anorexia nervosa, binge eating/purging type, mild |
| F50.021 | ICD10CM | Anorexia nervosa, binge eating/purging type, moderate |
| F50.022 | ICD10CM | Anorexia nervosa, binge eating/purging type, severe |
| F50.023 | ICD10CM | Anorexia nervosa, binge eating/purging type, extreme |
| F50.024 | ICD10CM | Anorexia nervosa, binge eating/purging type, in remission |
| F50.029 | ICD10CM | Anorexia nervosa, binge eating/purging type, unspecified |
| F50.20 | ICD10CM | Bulimia nervosa, unspecified |
| F50.21 | ICD10CM | Bulimia nervosa, mild |
| F50.22 | ICD10CM | Bulimia nervosa, moderate |
| F50.23 | ICD10CM | Bulimia nervosa, severe |
| F50.24 | ICD10CM | Bulimia nervosa, extreme |
| F50.25 | ICD10CM | Bulimia nervosa, in remission |
| F50.81 | ICD10CM | Binge eating disorder |
| F50.810 | ICD10CM | Binge eating disorder, mild |
| F50.811 | ICD10CM | Binge eating disorder, moderate |
| F50.812 | ICD10CM | Binge eating disorder, severe |
| F50.813 | ICD10CM | Binge eating disorder, extreme |
| F50.814 | ICD10CM | Binge eating disorder, in remission |
| F50.819 | ICD10CM | Binge eating disorder, unspecified |
ICD code information from First Databank (FDB).
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