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111 Cards in this Set
- Front
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Alprazolam
class prescribed for |
Commonly Prescribed For
(bold for FDA approved) Generalized anxiety disorder (IR) Panic disorder (IR and XR) non-fda Other anxiety disorders Anxiety associated with depression Premenstrual dysphoric disorder Irritable bowel syndrome and other somatic symptoms associated with anxiety disorders Insomnia Acute mania (adjunctive) Acute psychosis (adjunctive) |
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Alprazolam
how the drug works |
Binds to benzodiazepine receptors at the GABA-A ligand-gated chloride channel complex
Enhances the inhibitory effects of GABA Boosts chloride conductance through GABA-regulated channels Inhibits neuronal activity presumably in amygdala-centered fear circuits to provide therapeutic benefits in anxiety disorders |
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Alprazolam
how long until it works |
Some immediate relief with first dosing is common; can take several weeks with daily dosing for maximal therapeutic benefit
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Alprazolam
if it works |
For short-term symptoms of anxiety – after a few weeks, discontinue use or use on an “as-needed” basis
For chronic anxiety disorders, the goal of treatment is complete remission of symptoms as well as prevention of future relapses For chronic anxiety disorders, treatment most often reduces or even eliminates symptoms, but not a cure since symptoms can recur after medicine stopped For long-term symptoms of anxiety, consider switching to an SSRI or SNRI for long-term maintenance If long-term maintenance with a benzodiazepine is necessary, continue treatment for 6 months after symptoms resolve, and then taper dose slowly If symptoms reemerge, consider treatment with an SSRI or SNRI, or consider restarting the benzodiazepine; sometimes benzodiazepines have to be used in combination with SSRIs or SNRIs for best results |
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Alprazolam
best augmenting combos for partial response or treatment resistance |
Benzodiazepines are frequently used as augmenting agents for antipsychotics and mood stabilizers in the treatment of psychotic and bipolar disorders
Benzodiazepines are frequently used as augmenting agents for SSRIs and SNRIs in the treatment of anxiety disorders Not generally rational to combine with other benzodiazepines Caution if using as an anxiolytic concomitantly with other sedative hypnotics for sleep |
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Alprazolam
notable side effects |
Notable Side Effects
Sedation, fatigue, depression Dizziness, ataxia, slurred speech, weakness Forgetfulness, confusion Hyperexcitability, nervousness Rare hallucinations, mania Rare hypotension Hypersalivation, dry mouth |
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Alprazolam
dosage |
Anxiety: alprazolam IR: 1–4 mg/day
Panic: alprazolam IR: 5–6 mg/day Panic: alprazolam XR: 3–6 mg/day |
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Alprazolam
dosage forms |
Alprazolam IR tablet 0.25 mg scored, 0.4 mg (Japan), 0.5 mg scored, 0.8 mg (Japan), 1 mg scored, 2 mg multi-scored
Alprazolam IR orally disintegrating tablet 0.25 mg, 0.5 mg, 1 mg, 2 mg Alprazolam IR solution, concentrate 1 mg/mL Alprazolam XR (extended-release) tablet 0.5 mg, 1 mg, 2 mg, 3 mg |
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Alprazolam
how to dose |
For anxiety, alprazolam IR should be started at 0.75–1.5 mg/day divided into 3 doses; increase dose every 3–4 days until desired efficacy is reached; maximum dose generally 4 mg/day
For panic, alprazolam IR should be started at 1.5 mg/day divided into 3 doses; increase 1 mg or less every 3–4 days until desired efficacy is reached, increasing by smaller amounts for dosage over 4 mg/day; may require as much as 10 mg/day for desired efficacy in difficult cases For panic, alprazolam XR should be started at 0.5–1 mg/day once daily in the morning; dose may be increased by 1 mg/day every 3–4 days until desired efficacy is reached; maximum dose generally 10 mg/day |
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Alprazolam
how to stop |
Seizures may rarely occur on withdrawal, especially if withdrawal is abrupt; greater risk for doses above 4 mg and in those with additional risks for seizures, including those with a history of seizures
Taper by 0.5 mg every 3 days to reduce chances of withdrawal effects For difficult to taper cases, consider reducing dose much more slowly after reaching 3 mg/day, perhaps by as little as 0.25 mg per week or less For other patients with severe problems discontinuing a benzodiazepine, dosing may need to be tapered over many months (i.e., reduce dose by 1% every 3 days by crushing tablet and suspending or dissolving in 100 ml of fruit juice and then disposing of 1 ml while drinking the rest; 3–7 days later, dispose of 2 ml, and so on). This is both a form of very slow biological tapering and a form of behavioral desensitization Be sure to differentiate reemergence of symptoms requiring reinstitution of treatment from withdrawal symptoms Benzodiazepine-dependent anxiety patients and insulin-dependent diabetics are not addicted to their medications. When benzodiazepine-dependent patients stop their medication, disease symptoms can reemerge, disease symptoms can worsen (rebound), and/or withdrawal symptoms can emerge |
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Alprazolam
pharmacokinetics |
Metabolized by CYP450 3A4
Inactive metabolites Elimination half-life 12–15 hours |
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Alprazolam
drug interactions |
Increased depressive effects when taken with other CNS depressants
Inhibitors of CYP450 3A, such as nefazodone, fluvoxamine, fluoxetine, and even grapefruit juice, may decrease clearance of alprazolam and thereby raise alprazolam plasma levels and enhance sedative side effects; alprazolam dose may need to be lowered Thus, azole antifungal agents (such as ketoconazole and itraconazole), macrolide antibiotics, and protease inhibitors may also raise alprazolam plasma levels Inducers of CYP450 3A, such as carbamazepine, may increase clearance of alprazolam and lower alprazolam plasma levels and possibly reduce therapeutic effects |
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Alprazolam
do not use if |
If patient has narrow angle-closure glaucoma
If patient is taking ketoconazole or itraconazole (azole antifungal agents) If there is a proven allergy to alprazolam or any benzodiazepine |
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Alprazolam
special populations |
Renal Impairment
Drug should be used with caution Hepatic Impairment Should begin with lower starting dose (0.5–0.75 mg/day in 2 or 3 divided doses) Cardiac Impairment Benzodiazepines have been used to treat anxiety associated with acute myocardial infarction Elderly Should begin with lower starting dose (0.5–0.75 mg/day in 2 or 3 divided doses) and be monitored clo |
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Alprazolam
pregnancy |
Risk Category D [positive evidence of risk to human fetus; potential benefits may still justify its use during pregnancy]
Possible increased risk of birth defects when benzodiazepines taken during pregnancy Because of the potential risks, alprazolam is not generally recommended as treatment for anxiety during pregnancy, especially during the first trimester Drug should be tapered if discontinued Infants whose mothers received a benzodiazepine late in pregnancy may experience withdrawal effects Neonatal flaccidity has been reported in infants whose mothers took a benzodiazepine during pregnancy Seizures, even mild seizures, may cause harm to the embryo/fetus |
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Alprazolam
art of psychopharmacology advantages/disadvantages target symptoms |
Potential Advantages
Rapid onset of action Less sedation than some other benzodiazepines Availability of an XR formulation with longer duration of action Potential Disadvantages Euphoria may lead to abuse Abuse especially risky in past or present substance abusers Primary Target Symptoms Panic attacks Anxiety |
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Alprazolam
pearls |
One of the most popular benzodiazepines for anxiety, especially among primary care physicians and psychiatrists
Is a very useful adjunct to SSRIs and SNRIs in the treatment of numerous anxiety disorders Not effective for treating psychosis as a monotherapy, but can be used as an adjunct to antipsychotics Not effective for treating bipolar disorder as a monotherapy, but can be used as an adjunct to mood stabilizers and antipsychotics May both cause depression and treat depression in different patients Risk of seizure is greatest during the first 3 days after discontinuation of alprazolam, especially in those with prior seizures, head injuries, or withdrawal from drugs of abuse Clinical duration of action may be shorter than plasma half-life, leading to dosing more frequently than 2–3 times daily in some patients, especially for immediate release alprazolam Adding fluvoxamine, fluoxetine, or nefazodone can increase alprazolam levels and make the patient very sleepy unless the alprazolam dose is lowered by half or more When using to treat insomnia, remember that insomnia may be a symptom of some other primary disorder itself, and thus warrant evaluation for comorbid psychiatric and/or medical conditions Alprazolam XR may be less sedating than immediate release alprazolam Alprazolam XR may be dosed less frequently than immediate release alprazolam, and lead to less inter-dose breakthrough symptoms and less “clock-watching” in anxious patients Slower rises in plasma drug levels for alprazolam XR have the potential to reduce euphoria/abuse liability, but this has not been proven Slower falls in plasma drug levels for alprazolam XR have the potential to facilitate drug discontinuation by reducing withdrawal symptoms, but this has not been proven Alprozolam XR generally has longer biological duration of action than clonazepam If clonazepam can be considered a “long-acting alprazolam-like anxiolytic”, then alprazolam XR can be considered “an even longer-acting clonazepam-like anxiolytic” with the potential of improved tolerability features in terms of less euphoria, abuse, dependence, and withdrawal problems, but this has not been proven |
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Ativan
class used for |
Class
Benzodiazepine (anxiolytic, anticonvulsant) Commonly Prescribed For (bold for FDA approved) Anxiety disorder (oral) Anxiety associated with depressive symptoms (oral) Initial treatment of status epilepticus (injection) Preanesthetic (injection) non-fda Insomnia Muscle spasm Alcohol withdrawal psychosis Headache Panic disorder Acute mania (adjunctive) Acute psychosis (adjunctive) Delirium (with haloperidol) |
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Ativan
how the drug works |
How The Drug Works
Binds to benzodiazepine receptors at the GABA-A ligand-gated chloride channel complex Enhances the inhibitory effects of GABA Boosts chloride conductance through GABA-regulated channels Inhibits neuronal activity presumably in amygdala-centered fear circuits to provide therapeutic benefits in anxiety disorders Inhibitory actions in cerebral cortex may provide therapeutic benefits in seizure disorders |
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ativan
how long until it works |
Some immediate relief with first dosing is common; can take several weeks for maximal therapeutic benefit with daily dosing
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ativan
if it works |
For short-term symptoms of anxiety – after a few weeks, discontinue use or use on an “as-needed” basis
For chronic anxiety disorders, the goal of treatment is complete remission of symptoms as well as prevention of future relapses For chronic anxiety disorders, treatment most often reduces or even eliminates symptoms, but not a cure since symptoms can recur after medicine stopped For long-term symptoms of anxiety, consider switching to an SSRI or SNRI for long-term maintenance If long-term maintenance with a benzodiazepine is necessary, continue treatment for 6 months after symptoms resolve, and then taper dose slowly If symptoms reemerge, consider treatment with an SSRI or SNRI, or consider restarting the benzodiazepine; sometimes benzodiazepines have to be used in combination with SSRIs or SNRIs for best results |
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ativan
if it doesn't work |
Consider switching to another agent or adding an appropriate augmenting agent
Consider psychotherapy, especially cognitive behavioral psychotherapy Consider presence of concomitant substance abuse Consider presence of lorazepam abuse Consider another diagnosis such as a comorbid medical condition |
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Ativan
best augmenting combos for partial response or treatment resistance |
Best Augmenting Combos for Partial Response or Treatment-Resistance
Benzodiazepines are frequently used as augmenting agents for antipsychotics and mood stabilizers in the treatment of psychotic and bipolar disorders Benzodiazepines are frequently used as augmenting agents for SSRIs and SNRIs in the treatment of anxiety disorders Not generally rational to combine with other benzodiazepines Caution if using as an anxiolytic concomitantly with other sedative hypnotics for sleep |
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Ativan
tests |
In patients with seizure disorders, concomitant medical illness, and/or those with multiple concomitant long-term medications, periodic liver tests and blood counts may be prudent
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ativan
side effects |
How Drug Causes Side Effects
Same mechanism for side effects as for therapeutic effects – namely due to excessive actions at benzodiazepine receptors Long-term adaptations in benzodiazepine receptors may explain the development of dependence, tolerance, and withdrawal Side effects are generally immediate, but immediate side effects often disappear in time Notable Side Effects Sedation, fatigue, depression Dizziness, ataxia, slurred speech, weakness Forgetfulness, confusion Hyper-excitability, nervousness Pain at injection site Rare hallucinations, mania Rare hypotension Hypersalivation, dry mouth weight gain unusual sedation common |
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ativan
life threatening side effects |
Life Threatening or Dangerous Side Effects
Respiratory depression, especially when taken with CNS depressants in overdose Rare hepatic dysfunction, renal dysfunction, blood dyscrasias |
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Ativan
dose dose forms |
Usual Dosage Range
Oral: 2–6 mg/day in divided doses, largest dose at bedtime Injection: 4 mg administered slowly Dosage Forms Tablet 0.5 mg, 1 mg, 2 mg Liquid 0.5 mg/5mL, 2 mg/mL Injection 1 mg/0.5mL, 2 mg/mL, 4 mg/mL |
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Ativan
how to dose |
How to Dose
Oral: Initial 2–3 mg/day in 2–3 doses; increase as needed, starting with evening dose; maximum generally 10 mg/day Injection: Initial 4 mg administered slowly; after 10–15 minutes may administer again Take liquid formulation with water, soda, applesauce or pudding |
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ativan
dosing tips |
One of the few benzodiazepines available in an oral liquid formulation
One of the few benzodiazepines available in an injectable formulation Lorazepam injection is intended for acute use; patients who require long-term treatment should be switched to the oral formulation Use lowest possible effective dose for the shortest possible period of time (a benzodiazepine-sparing strategy) Assess need for continued treatment regularly Risk of dependence may increase with dose and duration of treatment For inter-dose symptoms of anxiety, can either increase dose or maintain same total daily dose but divide into more frequent doses Can also use an as-needed occasional “top up” dose for inter-dose anxiety Because panic disorder can require doses higher than 6 mg/day, the risk of dependence may be greater in these patients Some severely ill patients may require 10 mg/day or more Frequency of dosing in practice is often greater than predicted from half-life, as duration of biological activity is often shorter than pharmacokinetic terminal half-life |
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ativan
long term use |
Long-Term Use
Evidence of efficacy up to 16 weeks Risk of dependence, particularly for treatment periods longer than 12 weeks and especially in patients with past or current polysubstance abuse |
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ativan
how to stop |
Patients with history of seizure may seize upon withdrawal, especially if withdrawal is abrupt
Taper by 0.5 mg every 3 days to reduce chances of withdrawal effects For difficult to taper cases, consider reducing dose much more slowly once reaching 3 mg/day, perhaps by as little as 0.25 mg per week or less For other patients with severe problems discontinuing a benzodiazepine, dosing may need to be tapered over many months (i.e., reduce dose by 1% every 3 days by crushing tablet and suspending or dissolving in 100 ml of fruit juice and then disposing of 1 ml while drinking the rest; 3–7 days later, dispose of 2 ml, and so on). This is both a form of very slow biological tapering and a form of behavioral desensitization Be sure to differentiate reemergence of symptoms requiring reinstitution of treatment from withdrawal symptoms Benzodiazepine-dependent anxiety patients and insulin-dependent diabetics are not addicted to their medications. When benzodiazepine-dependent patients stop their medication, disease symptoms can reemerge, disease symptoms can worsen (rebound), and/or withdrawal symptoms can emerge |
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ativan
pharmacokinetics |
harmacokinetics
Elimination half-life 10–20 hours No active metabolites |
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Ativan
drug interactions |
Drug Interactions
Increased depressive effects when taken with other CNS depressants Valproate and probenecid may reduce clearance and raise plasma concentrations of lorazepam Oral contraceptives may increase clearance and lower plasma concentrations of lorazepam Flumazenil (used to reverse the effects of benzodiazepines) may precipitate seizures and should not be used in patients treated for seizure disorders with lorazepam |
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ativan
do not use if |
Do Not Use
If patient has narrow angle-closure glaucoma If patient has sleep apnea (injection) Must not be given intra-arterially because it may cause arteriospasm and result in gangrene If there is a proven allergy to lorazepam or any benzodiazepine |
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Ativan
special populations |
Renal Impairment
1–2 mg/day in 2–3 doses Hepatic Impairment 1–2 mg/day in 2–3 doses Because of its short half-life and inactive metabolites, lorazepam may be a preferred benzodiazepine in some patients with liver disease Cardiac Impairment Benzodiazepines have been used to treat anxiety associated with acute myocardial infarction Lorazepam may be used as an adjunct to control drug-induced cardiovascular emergencies Elderly 1–2 mg/day in 2–3 doses May be more sensitive to sedative or respiratory effects |
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ativan
pregnancy |
Pregnancy
Risk Category D [positive evidence of risk to human fetus; potential benefits may still justify its use] Possible increased risk of birth defects when benzodiazepines taken during pregnancy Because of the potential risks, lorazepam is not generally recommended as treatment for anxiety during pregnancy, especially during the first trimester Drug should be tapered if discontinued Infants whose mothers received a benzodiazepine late in pregnancy may experience withdrawal effects Neonatal flaccidity has been reported in infants whose mothers took a benzodiazepine during pregnancy Seizures, even mild seizures, may cause harm to the embryo/fetus |
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Ativan
the art of psychopharmacology advantages and disadvantages |
Potential Advantages
Rapid onset of action Availability of oral liquid as well as injectable dosage formulations Potential Disadvantages Euphoria may lead to abuse Abuse especially risky in past or present substance abusers Possibly more sedation than some other benzodiazepines commonly used to treat anxiety |
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Ativan
primary target symptoms |
Primary Target Symptoms
Panic attacks Anxiety Muscle spasms Incidence of seizures (adjunct) |
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Ativan
Pearls |
Pearls
One of the most popular and useful benzodiazepines for treatment of agitation associated with psychosis, bipolar disorder, and other disorders, especially in the inpatient setting; this is due in part to useful sedative properties and flexibility of administration with oral tablets, oral liquid, or injectable formulations, which is often useful in treating uncooperative patients Is a very useful adjunct to SSRIs and SNRIs in the treatment of numerous anxiety disorders Not effective for treating psychosis as a monotherapy, but can be used as an adjunct to antipsychotics Not effective for treating bipolar disorder as a monotherapy, but can be used as an adjunct to mood stabilizers and antipsychotics Because of its short half-life and inactive metabolites, lorazepam may be preferred over some benzodiazepines for patients with liver disease Lorazepam may be preferred over other benzodiazepines for the treatment of delirium When treating delirium, lorazepam is often combined with haloperidol, with the haloperidol dose 2 times the lorazepam dose Lorazepam is often used to induce pre-operative anterograde amnesia to assist in anesthesiology May both cause depression and treat depression in different patients Clinical duration of action may be shorter than plasma half-life, leading to dosing more frequently than 2–3 times daily in some patients When using to treat insomnia, remember that insomnia may be a symptom of some other primary disorder itself, and thus warrant evaluation for comorbid psychiatric and/or medical conditions |
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Klonopin
class use |
Class
Benzodiazepine (anxiolytic, anticonvulsant) Commonly Prescribed For (bold for FDA approved) Panic disorder, with or without agoraphobia Lennox-Gastaut syndrome (petit mal variant) Akinetic seizure Myoclonic seizure Absence seizure (petit mal) non-fda Atonic seizures Other seizure disorders Other anxiety disorders Acute mania (adjunctive) Acute psychosis (adjunctive) Insomnia |
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Klonopin
how the drug works |
How The Drug Works
Binds to benzodiazepine receptors at the GABA-A ligand-gated chloride channel complex Enhances the inhibitory effects of GABA Boosts chloride conductance through GABA-regulated channels Inhibits neuronal activity presumably in amygdala-centered fear circuits to provide therapeutic benefits in anxiety disorders Inhibitory actions in cerebral cortex may provide therapeutic benefits in seizure disorders |
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Klonopin
how long until it works |
Some immediate relief with first dosing is common; can take several weeks with daily dosing for maximal therapeutic benefit
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Klonopin
if it works |
For short-term symptoms of anxiety – after a few weeks, discontinue use or use on an “as-needed” basis
For chronic anxiety disorders, the goal of treatment is complete remission of symptoms as well as prevention of future relapses For chronic anxiety disorders, treatment most often reduces or even eliminates symptoms, but not a cure since symptoms can recur after medicine stopped For long-term symptoms of anxiety, consider switching to an SSRI or SNRI for long-term maintenance If long-term maintenance with a benzodiazepine is necessary, continue treatment for 6 months after symptoms resolve, and then taper dose slowly If symptoms reemerge, consider treatment with an SSRI or SNRI, or consider restarting the benzodiazepine; sometimes benzodiazepines have to be used in combination with SSRIs or SNRIs for best results For long-term treatment of seizure disorders, development of tolerance dose escalation and loss of efficacy necessitating adding or switching to other anticonvulsants is not uncommon |
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Klonopin
if it doesn't work |
Consider switching to another agent or adding an appropriate augmenting agent
Consider psychotherapy, especially cognitive behavioral psychotherapy Consider presence of concomitant substance abuse Consider presence of clonazepam abuse Consider another diagnosis such as a comorbid medical condition |
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Klonopin
best augmenting combos for partial response or treatment resistance |
Benzodiazepines are frequently used as augmenting agents for antipsychotics and mood stabilizers in the treatment of psychotic and bipolar disorders
Benzodiazepines are frequently used as augmenting agents for SSRIs and SNRIs in the treatment of anxiety disorders Not generally rational to combine with other benzodiazepines Caution if using as an anxiolytic concomitantly with other sedative hypnotics for sleep Clonazepam is commonly combined with other anticonvulsants for the treatment of seizure disorders |
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Klonopin
tests |
In patients with seizure disorders, concomitant medical illness, and/or those with multiple concomitant long-term medications, periodic liver tests and blood counts may be prudent
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Klonopin
side effects |
How Drug Causes Side Effects
Same mechanism for side effects as for therapeutic effects – namely due to excessive actions at benzodiazepine receptors Long-term adaptations in benzodiazepine receptors may explain the development of dependence, tolerance, and withdrawal Side effects are generally immediate, but immediate side effects often disappear in time Notable Side Effects Sedation, fatigue, depression Dizziness, ataxia, slurred speech, weakness Forgetfulness, confusion Hyper-excitability, nervousness Rare hallucinations, mania Rare hypotension Hypersalivation, dry mouth weight gain unusual sedation not usual |
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Klonopin
life threatening |
Respiratory depression, especially when taken with CNS depressants in overdose
Rare hepatic dysfunction, renal dysfunction, blood dyscrasias Grand mal seizures |
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Klonopin
what to do about side effects |
Wait
Wait Wait Lower the dose Take largest dose at bedtime to avoid sedative effects during the day Switch to another agent Administer flumazenil if side effects are severe or life-threatening |
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Klonopin
dosage range for seizures and panic forms |
Usual Dosage Range
Seizures: dependent on individual response of patient, up to 20 mg/day Panic: 0.5–2 mg/day either as divided doses or once at bedtime Dosage Forms Tablet 0.5 mg scored, 1 mg, 2 mg Disintegrating (wafer): 0.125 mg, 0.25 mg, 0.5 mg, 1 mg, 2 mg |
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Klonopin
how to dose seizures, panic |
Seizures – 1.5 mg divided into 3 doses, raise by 0.5 mg every 3 days until desired effect is reached; divide into 3 even doses or else give largest dose at bedtime; maximum dose generally 20 mg/day
Panic – 1 mg/day; start at 0.25 mg divided into 2 doses, raise to 1 mg after 3 days; dose either twice daily or once at bedtime; maximum dose generally 4 mg/day |
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Klonopin
dosing tips |
For anxiety disorders, use lowest possible effective dose for the shortest possible period of time (a benzodiazepine sparing strategy)
Assess need for continuous treatment regularly Risk of dependence may increase with dose and duration of treatment For inter-dose symptoms of anxiety, can either increase dose or maintain same daily dose but divide into more frequent doses Can also use an as-needed occasional “top-up” dose for inter-dose anxiety Because seizure disorder can require doses much higher than 2 mg/day, the risk of dependence may be greater in these patients Because panic disorder can require doses somewhat higher than 2 mg/day, the risk of dependence may be greater in these patients than in anxiety patients maintained at lower doses Some severely ill seizure patients may require more than 20 mg/day Some severely ill panic patients may require 4 mg/day or more Frequency of dosing in practice is often greater than predicted from half-life, as duration of biological activity is often shorter than pharmacokinetic terminal half-life Clonazepam is generally dosed half the dosage of alprazolam Escalation of dose may be necessary if tolerance develops in seizure disorders Escalation of dose usually not necessary in anxiety disorders, as tolerance to clonazepam does not generally develop in the treatment of anxiety disorders Available as an oral disintegrating wafer |
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Klonopin
how to stop |
Patients with history of seizures may seize upon withdrawal, especially if withdrawal is abrupt
Taper by 0.25 mg every 3 days to reduce chances of withdrawal effects For difficult to taper cases, consider reducing dose much more slowly after reaching 1.5 mg/day, perhaps by as little as 0.125 mg per week or less For other patients with severe problems discontinuing a benzodiazepine, dosing may need to be tapered over many months (i.e., reduce dose by 1% every 3 days by crushing tablet and suspending or dissolving in 100 ml of fruit juice and then disposing of 1 ml while drinking the rest; 3–7 days later, dispose of 2 ml, and so on). This is both a form of very slow biological tapering and a form of behavioral desensitization Be sure to differentiate reemergence of symptoms requiring reinstitution of treatment from withdrawal symptoms Benzodiazepine-dependent anxiety patients and insulin-dependent diabetics are not addicted to their medications. When benzodiazepine-dependent patients stop their medication, disease symptoms can reemerge, disease symptoms can worsen (rebound), and/or withdrawal symptoms can emerge |
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Klonopin
half life |
Long half-life compared to other benzodiazepine anxiolytics (elimination half-life approximately 30–40 hours)
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Klonopin
drug interactions |
Increased depressive effects when taken with other CNS depressants
Inhibitors of CYP450 3A4 may affect the clearance of clonazepam, but dosage adjustment usually not necessary Flumazenil (used to reverse the effects of benzodiazepines) may precipitate seizures and should not be used in patients treated for seizure disorders with clonazepam Use of clonazepam with valproate may cause absence status |
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Klonopin
warnings and precautions |
Dosage changes should be made in collaboration with prescriber
Use with caution in patients with pulmonary disease; rare reports of death after initiation of benzodiazepines in patients with severe pulmonary impairment History of drug or alcohol abuse often creates greater risk for dependency Clonazepam may induce grand mal seizures in patients with multiple seizure disorders Use only with extreme caution if patient has obstructive sleep apnea Some depressed patients may experience a worsening of suicidal ideation Some patients may exhibit abnormal thinking or behavioral changes similar to those caused by other CNS depressants (i.e., either depressant actions or disinhibiting actions) |
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Klonopin
do not use |
If patient has narrow angle-closure glaucoma
If patient has severe liver disease If there is a proven allergy to clonazepam or any benzodiazepine |
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Klonopin
special populations |
Renal Impairment
Dose should be reduced Hepatic Impairment Dose should be reduced Cardiac Impairment Benzodiazepines have been used to treat anxiety associated with acute myocardial infarction Elderly Should receive lower doses and be monitored |
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Klonopin
pregnancy |
Pregnancy
Risk Category D [positive evidence of risk to human fetus; potential benefits may still justify its use during pregnancy, especially for seizure disorders] Possible increased risk of birth defects when benzodiazepines taken during pregnancy Because of the potential risks, clonazepam is not generally recommended as treatment for anxiety during pregnancy, especially during the first trimester Drug should be tapered if discontinued Infants whose mothers received a benzodiazepine late in pregnancy may experience withdrawal effects Neonatal flaccidity has been reported in infants whose mothers took a benzodiazepine during pregnancy Seizures, even mild seizures, may cause harm to the embryo/fetus |
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Klonopin
The art of psychopharm advantages and disadvanteges |
Potential Advantages
Rapid onset of action Less sedation than some other benzodiazepines Longer duration of action than some other benzodiazepines Availability of oral disintegrating wafer Potential Disadvantages Development of tolerance may require dose increases, especially in seizure disorders Abuse especially risky in past or present substance abusers |
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Klonopin
target symptoms |
Primary Target Symptoms
Frequency and duration of seizures Spike and wave discharges in absence seizures (petit mal) Panic attacks Anxiety |
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Klonopin
Pearls |
Pearls
One of the most popular benzodiazepines for anxiety, especially among psychiatrists Is a very useful adjunct to SSRIs and SNRIs in the treatment of numerous anxiety disorders Not effective for treating psychosis as a monotherapy, but can be used as an adjunct to antipsychotics Not effective for treating bipolar disorder as a monotherapy, but can be used as an adjunct to mood stabilizers and antipsychotics Generally used as second-line treatment for petit mal seizures if succinimides are ineffective Can be used as an adjunct or as monotherapy for seizure disorders Clonazepam is the only benzodiazepine that is used as a solo maintenance treatment for seizure disorders Easier to taper than some other benzodiazepines because of long half-life May have less abuse potential than some other benzodiazepines May cause less depression, euphoria, or dependence than some other benzodiazepines Clonazepan is often considered a “longer-acting alprazolam-like anxiolytic” with improved tolerability features in terms of less euphoria, abuse, dependence, and withdrawal problems, but this has not been proven When using to treat insomnia, remember that insomnia may be a symptom of some other primary disorder itself, and thus warrant evaluation for comorbid psychiatric and/or medical conditions |
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Diazepam
class use |
Class
Benzodiazepine (anxiolytic, muscle relaxant, anticonvulsant) Commonly Prescribed For (bold for FDA approved) Anxiety disorder Symptoms of anxiety (short-term) Acute agitation, tremor, impending or acute delirium tremens and hallucinosis in acute alcohol withdrawal Skeletal muscle spasm due to reflex spasm to local pathology Spasticity caused by upper motor neuron disorder Athetosis Stiffman syndrome Convulsive disorder (adjunctive) Anxiety during endoscopic procedures (adjunctive) (injection only) Pre-operative anxiety (injection only) Anxiety relief prior to cardioversion (intravenous) Initial treatment of status epilepticus (injection only) non -fda Insomnia |
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Diazepam
how the drug works |
Binds to benzodiazepine receptors at the GABA-A ligand-gated chloride channel complex
Enhances the inhibitory effects of GABA Boosts chloride conductance through GABA-regulated channels Inhibits neuronal activity presumably in amygdala-centered fear circuits to provide therapeutic benefits in anxiety disorders Inhibiting actions in cerebral cortex may provide therapeutic benefits in seizure disorders Inhibitory actions in spinal cord may provide therapeutic benefits for muscle spasms |
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Diazepam
how long until it works |
Some immediate relief with first dosing is common; can take several weeks with daily dosing for maximal therapeutic benefit
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Diazepam
if it works |
For short-term symptoms of anxiety or muscle spasms – after a few weeks, discontinue use or use on an “as-needed” basis
Chronic muscle spasms may require chronic diazepam treatment For chronic anxiety disorders, the goal of treatment is complete remission of symptoms as well as prevention of future relapses For chronic anxiety disorders, treatment most often reduces or even eliminates symptoms, but not a cure since symptoms can recur after medicine stopped For long-term symptoms of anxiety, consider switching to an SSRI or SNRI for long term maintenance If long-term maintenance with a benzodiazepine is necessary, continue treatment for 6 months after symptoms resolve, and then taper dose slowly If symptoms reemerge, consider treatment with an SSRI or SNRI, or consider restarting the benzodiazepine; sometimes benzodiazepines have to be used in combination with SSRIs or SNRIs for best results |
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Diazepam
best augmenting combos for partial or treatment resistance |
Benzodiazepines are frequently used as augmenting agents for antipsychotics and mood stabilizers in the treatment of psychotic and bipolar disorders
Benzodiazepines are frequently used as augmenting agents for SSRIs and SNRIs in the treatment of anxiety disorders Not generally rational to combine with other benzodiazepines Caution if using as an anxiolytic concomitantly with other sedative hypnotics for sleep |
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Diazepam
labs or tests |
In patients with seizure disorders, concomitant medical illness, and/or those with multiple concomitant long-term medications, periodic liver tests and blood counts may be prudent
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Diazepam
side effects |
How Drug Causes Side Effects
Same mechanism for side effects as for therapeutic effects – namely due to excessive actions at benzodiazepine receptors Long-term adaptations in benzodiazepine receptors may explain the development of dependence, tolerance, and withdrawal Side effects are generally immediate, but immediate side effects often disappear in time Notable Side Effects Sedation, fatigue, depression Dizziness, ataxia, slurred speech, weakness Forgetfulness, confusion Hyper-excitability, nervousness weight gain unusual, sedation common Pain at injection site Rare hallucinations, mania Rare hypotension Hypersalivation, dry mouth |
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Diazepam
life threatening side effects |
Respiratory depression, especially when taken with CNS depressants in overdose
Rare hepatic dysfunction, renal dysfunction, blood dyscrasias |
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Diazepam
usual dose and dose forms |
Oral: 4–40 mg/day in divided doses
Intravenous (adults): 5 mg/minute Tablet 2 mg scored, 5 mg scored, 10 mg scored Liquid 5 mg/5 mL, concentrate 5 mg/mL Injection vial 5 mg/mL; 10 mL, boxes of 1; 2 mL boxes of 10 Rectal gel 5 mg/mL; 2.5 mg, 5 mg, 10 mg, 15 mg, 20 mg |
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Diazepam
how to dose |
Oral (anxiety, muscle spasm, seizure): 2–10 mg, 2–4 times/day
Oral (alcohol withdrawal): Initial 10 mg, 3–4 times/day for 1 day; reduce to 5 mg, 3–4 times/day; continue treatment as needed Liquid formulation should be mixed with water or fruit juice, applesauce, or pudding Because of risk of respiratory depression, rectal diazepam treatment should not be given more than once in 5 days or more than twice during a treatment course, especially for alcohol withdrawal or status epilepticus |
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Diazepam
dosing tips |
Only benzodiazepine with a formulation specifically for rectal administration
One of the few benzodiazepines available in an oral liquid formulation One of the few benzodiazepines available in an injectable formulation Diazepam injection is intended for acute use; patients who require long-term treatment should be switched to the oral formulation Use lowest possible effective dose for the shortest possible period of time (a benzodiazepine-sparing strategy) Assess need for continued treatment regularly Risk of dependence may increase with dose and duration of treatment For inter-dose symptoms of anxiety, can either increase dose or maintain same total daily dose but divide into more frequent doses Can also use an as-needed occasional “top up” dose for inter-dose anxiety Because some anxiety disorder patients and muscle spasm patients can require doses higher than 40 mg/day or more, the risk of dependence may be greater in these patients Frequency of dosing in practice is often greater than predicted from half-life, as duration of biological activity is often shorter than pharmacokinetic terminal half-life |
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Diazepam
long term use |
Evidence of efficacy up to 16 weeks
Risk of dependence, particularly for treatment periods longer than 12 weeks and especially in patients with past or current polysubstance abuse Not recommended for long-term treatment of seizure disorders |
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Diazepam
how to stop |
Patients with history of seizure may seize upon withdrawal, especially if withdrawal is abrupt
Taper by 2 mg every 3 days to reduce chances of withdrawal effects For difficult to taper cases, consider reducing dose much more slowly after reaching 20 mg/day, perhaps by as little as 0.5–1 mg every week or less For other patients with severe problems discontinuing a benzodiazepine, dosing may need to be tapered over many months (i.e., reduce dose by 1% every 3 days by crushing tablet and suspending or dissolving in 100 mL of fruit juice and then disposing of 1 mL while drinking the rest; 3–7 days later, dispose of 2 mL, and so on). This is both a form of very slow biological tapering and a form of behavioral desensitization Be sure to differentiate reemergence of symptoms requiring reinstitution of treatment from withdrawal symptoms Benzodiazepine-dependent anxiety patients and insulin-dependent diabetics are not addicted to their medications. When benzodiazepine-dependent patients stop their medication, disease symptoms can reemerge, disease symptoms can worsen (rebound), and/or withdrawal symptoms can emerge |
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Diazepam
pharmacokinetics |
Elimination half-life 20–50 hours
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Diazepam
warnings and precautions |
Dosage changes should be made in collaboration with prescriber
Use with caution in patients with pulmonary disease; rare reports of death after initiation of benzodiazepines in patients with severe pulmonary impairment History of drug or alcohol abuse often creates greater risk for dependency Some depressed patients may experience a worsening of suicidal ideation Some patients may exhibit abnormal thinking or behavioral changes similar to those caused by other CNS depressants (i.e., either depressant actions or disinhibiting actions) |
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Diazepam
do not use in or if |
If narrow angle-closure glaucoma
If there is a proven allergy to diazepam or any benzodiazepine |
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Diazepam
special populations |
Renal Impairment
Initial 2–2.5 mg, 1–2 times/day; increase gradually as needed Hepatic Impairment Initial 2–2.5 mg, 1–2 times/day; increase gradually as needed Cardiac Impairment Benzodiazepines have been used to treat anxiety associated with acute myocardial infarction Diazepam may be used as an adjunct during cardiovascular emergencies Elderly Initial 2–2.5 mg, 1–2 times/day; increase gradually as needed |
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Diazepam
pregnancy |
Risk Category D [positive evidence of risk to human fetus; potential benefits may still justify its use during pregnancy]
Possible increased risk of birth defects when benzodiazepines taken during pregnancy Because of the potential risks, diazepam is not generally recommended as treatment for anxiety during pregnancy, especially during the first trimester Drug should be tapered if discontinued Infants whose mothers received a benzodiazepine late in pregnancy may experience withdrawal effects Neonatal flaccidity has been reported in infants whose mothers took a benzodiazepine during pregnancy Seizures, even mild seizures, may cause harm to the embryo/fetus |
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Diazepam
art of psychopharmacology advantages and disadvantages primary target |
Potential Advantages
Rapid onset of action Availability of oral liquid, rectal, and injectable dosage formulations Potential Disadvantages Euphoria may lead to abuse Abuse especially risky in past or present substance abusers Can be sedating at doses necessary to treat moderately severe anxiety disorders Primary Target Symptoms Panic attacks Anxiety Incidence of seizures (adjunct) Muscle spasms |
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Diazepam
pearls |
Pearls
Can be a useful adjunct to SSRIs and SNRIs in the treatment of numerous anxiety disorders, but not used as frequently as other benzodiazepines for this purpose Not effective for treating psychosis as a monotherapy, but can be used as an adjunct to antipsychotics Not effective for treating bipolar disorder as a monotherapy, but can be used as an adjunct to mood stabilizers and antipsychotics Diazepam is often the first choice benzodiazepine to treat status epilepticus, and is administered either intravenously or rectally Because diazepam suppresses stage 4 sleep, it may prevent night terrors in adults May both cause depression and treat depression in different patients Was once one of the most commonly prescribed drugs in the world and the most commonly prescribed benzodiazepine Remains a popular benzodiazepine for treating muscle spasms A commonly used benzodiazepine to treat sleep disorders Remains a popular benzodiazepine to treat acute alcohol withdrawal Not especially useful as an oral anticonvulsant Multiple dosage formulations (oral tablet, oral liquid, rectal gel, injectable) allow more flexibility of administration compared to most other benzodiazepines When using to treat insomnia, remember that insomnia may be a symptom of some other primary disorder itself, and thus warrant evaluation for comorbid psychiatric and/or medical conditions |
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Oxazepam (Serax)
class and use |
benzodiazepine
FDA anxiety anxiety associated with depression alcohol withdrawal |
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Oxazepam (Serax)
how the drug works |
Binds to benzodiazepine receptors at the GABA-A ligand-gated chloride channel complex
Enhances the inhibitory effects of GABA Boosts chloride conductance through GABA-regulated channels Inhibits neuronal activity presumably in amygdala-centered fear circuits to provide therapeutic benefits in anxiety disorders |
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Oxazepam (Serax)
how long until it works |
Some immediate relief with first dosing is common; can take several weeks with daily dosing for maximal therapeutic benefit
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Oxazepam (Serax)
best augmenting for partial response or treatment resistance |
Benzodiazepines are frequently used as augmenting agents for antipsychotics and mood stabilizers in the treatment of psychotic and bipolar disorders
Benzodiazepines are frequently used as augmenting agents for SSRIs and SNRIs in the treatment of anxiety disorders Not generally rational to combine with other benzodiazepines Caution if using as an anxiolytic concomitantly with other sedative hypnotics for sleep |
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Oxazepam (Serax)
tests |
n patients with seizure disorders, concomitant medical illness, and/or those with multiple concomitant long-term medications, periodic liver tests and blood counts may be prudent
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Oxazepam (Serax)
side effects |
Same mechanism for side effects as for therapeutic effects – namely due to excessive actions at benzodiazepine receptors
Long-term adaptations in benzodiazepine receptors may explain the development of dependence, tolerance, and withdrawal Side effects are generally immediate, but immediate side effects often disappear in time Notable Side Effects Sedation, fatigue, depression Dizziness, ataxia, slurred speech, weakness Forgetfulness, confusion Hyper-excitability, nervousness Rare hallucinations, mania Rare hypotension Hypersalivation, dry mouth unusual weight gain, sedation common |
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Oxazepam (Serax)
dosage range for mild to moderate anxiety and severe anxiety or associated with ETOH withdrawal |
Usual Dosage Range
Mild to moderate anxiety: 30–60 mg/day in 3–4 divided doses Severe anxiety, anxiety associated with alcohol withdrawal: 45–120 mg/day in 3–4 divided doses Dosage Forms Capsule 10 mg, 15 mg, 30 mg Tablet 15 mg |
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Oxazepam (Serax)
how to dose |
Titration no necessary
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Oxazepam (Serax)
dosing tips |
Use lowest possible effective dose for the shortest possible period of time (a benzodiazepine-sparing strategy)
15 mg tablet contains tartrazine, which may cause allergic reactions in certain patients, particularly those who are sensitive to aspirin For inter-dose symptoms of anxiety, can either increase dose or maintain same total daily dose but divide into more frequent doses Can also use an as-needed occasional “top up” dose for inter-dose anxiety Because anxiety disorders can require higher doses, the risk of dependence may be greater in these patients Some severely ill patients may require doses higher than the generally recommended maximum dose Frequency of dosing in practice is often greater than predicted from half-life, as duration of biological activity is often shorter than pharmacokinetic terminal half-life |
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Oxazepam (Serax)
long term use |
Risk of dependence, particularly for treatment periods longer than 12 weeks and especially in patients with past or current polysubstance abuse
Habit Forming Oxazepam is a Schedule IV drug Patients may develop dependence and/or tolerance with long-term use |
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Oxazepam (Serax)
how to stop |
Patients with history of seizure may seize upon withdrawal, especially if withdrawal is abrupt
Taper by 15 mg every 3 days to reduce chances of withdrawal effects For difficult to taper cases, consider reducing dose much more slowly once reaching 45 mg/day, perhaps by as little as 10 mg per week or less For other patients with severe problems discontinuing a benzodiazepine, dosing may need to be tapered over many months (i.e., reduce dose by 1% every 3 days by crushing tablet and suspending or dissolving in 100 ml of fruit juice and then disposing of 1 ml while drinking the rest; 3–7 days later, dispose of 2 ml, and so on). This is both a form of very slow biological tapering and a form of behavioral desensitization Be sure to differentiate reemergence of symptoms requiring reinstitution of treatment from withdrawal symptoms Benzodiazepine-dependent anxiety patients and insulin-dependent diabetics are not addicted to their medications. When benzodiazepine-dependent patients stop their medication, disease symptoms can reemerge, disease symptoms can worsen (rebound), and/or withdrawal symptoms can emerge |
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Oxazepam (Serax)
pharmacokinetics |
Pharmacokinetics
Elimination half-life 3–21 hours No active metabolites |
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Oxazepam (Serax)
warnings and precautions |
Dosage changes should be made in collaboration with prescriber
Use with caution in patients with pulmonary disease; rare reports of death after initiation of benzodiazepines in patients with severe pulmonary impairment History of drug or alcohol abuse often creates greater risk for dependency Some depressed patients may experience a worsening of suicidal ideation Some patients may exhibit abnormal thinking or behavioral changes similar to those caused by other CNS depressants (i.e., either depressant actions or disinhibiting actions) |
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Oxazepam (Serax)
do not use |
If patient has narrow angle-closure glaucoma
If there is a proven allergy to oxazepam or any benzodiazepine |
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Oxazepam (Serax)
special populations |
enal Impairment
Use with caution; oxazepam levels may be increased Hepatic Impairment Use with caution; oxazepam levels may be increased Because of its short half-life and inactive metabolites, oxazepam may be a preferred benzodiazepine in some patients with liver disease Cardiac Impairment Benzodiazepines have been used to treat anxiety associated with acute myocardial infarction Elderly Initial 30 mg in 3 divided doses; can be increased to 30–60 mg/day in 3–4 divided doses |
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Oxazepam (Serax)
The art of psychopharm pros and cons target symptoms |
Potential Advantages
Rapid onset of action Potential Disadvantages Euphoria may lead to abuse Abuse especially risky in past or present substance abusers Primary Target Symptoms Panic attacks Anxiety Agitation |
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Oxazepam (Serax)
target symptoms pearls |
Can be a very useful adjunct to SSRIs and SNRIs in the treatment of numerous anxiety disorders
Not effective for treating psychosis as a monotherapy, but can be used as an adjunct to antipsychotics Not effective for treating bipolar disorder as a monotherapy, but can be used as an adjunct to mood stabilizers and antipsychotics Because of its short half-life and inactive metabolites, oxazepam may be preferred over some benzodiazepines for patients with liver disease Oxazepam may be preferred over some other benzodiazepines for the treatment of delirium Can both cause and treat depression in different patients When using to treat insomnia, remember that insomnia may be a symptom of some other primary disorder itself, and thus warrant evaluation for comorbid psychiatric and/or medical conditions |
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Gabapentin (Neurontin)
Class |
Anticonvulsant, antineuralgic for chronic pain, alpha 2 delta ligand at voltage-sensitive calcium channels
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Gabapentin (Neurontin)
used for |
Commonly Prescribed For
(bold for FDA approved) Partial seizures with or without secondary generalization (adjunctive) Postherpetic neuralgia non-fda Neuropathic pain/chronic pain Anxiety (adjunctive) Bipolar disorder (adjunctive) |
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Gabapentin (Neurontin)
best augmenting combos for partial or treatment resistance |
Gabapentin is itself an augmenting agent to numerous other anticonvulsants in treating epilepsy; and to lithium, atypical antipsychotics and other anticonvulsants in the treatment of bipolar disorder
For postherpetic neuralgia, gabapentin can decrease concomitant opiate use For neuropathic pain, gabapentin can augment tricyclic antidepressants and SNRIs as well as tiagabine, other anticonvulsants and even opiates if done by experts while carefully monitoring in difficult cases For anxiety, gabapentin is a second-line treatment to augment SSRIs, SNRIs, or benzodiazepines |
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Gabapentin (Neurontin)
side effects |
How Drug Causes Side Effects
CNS side effects may be due to excessive blockade of voltage-sensitive calcium channels Notable Side Effects Sedation, dizziness, ataxia, fatigue, nystagmus, tremor Vomiting, dyspepsia, diarrhea, dry mouth, constipation, weight gain Blurred vision Peripheral edema Additional effects in children under age 12: hostility, emotional lability, hyperkinesia, thought disorder, weight gain Life-Threatening or Dangerous Side Effects Sudden unexplained deaths have occurred in epilepsy (unknown if related to gabapentin use) Rare activation of suicidal ideation and behavior(suicidality) weight gain not usual sedation common |
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Gabapentin (Neurontin)
dose range |
900–1800 mg/day in 3 divided doses
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Gabapentin (Neurontin)
how to dose |
Postherpetic neuralgia: 300 mg on day 1; on day 2 increase to 600 mg in 2 doses; on day 3 increase to 900 mg in 3 doses; maximum dose generally 1800 mg/day in 3 doses
Seizures (ages 12 and older): Initial 900 mg/day in 3 doses; recommended dose generally 1800 mg/day in 3 doses; maximum dose generally 3600 mg/day; time between any 2 doses should usually not exceed 12 hours |
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Gabapentin (Neurontin)
dosing tips |
Gabapentin should not be taken until 2 hours after administration of an antacid
If gabapentin is added to a second anticonvulsant, the titration period should be at least a week to improve tolerance to sedation Some patients need to take gabapentin only twice daily in order to experience adequate symptomatic relief for pain or anxiety At the high end of the dosing range, tolerability may be enhanced by splitting dose into more than 3 divided doses For intolerable sedation, can give most of the dose at night and less during the day To improve slow-wave sleep, may need to take gabapentin only at bedtime |
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Gabapentin (Neurontin)
pharmacokinetics |
Gabapentin is not metabolized but excreted intact renally
Not protein bound Elimination half-life approximately 5–7 hours |
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Gabapentin (Neurontin)
special populations |
Renal Impairment
Gabapentin is renally excreted, so the dose may need to be lowered Dosing can be adjusted according to creatinine clearance, such that patients with clearance below 16 mL/min should receive 100–300 mg/day in 1 dose, patients with clearance between 16–29 mL/min should receive 200–700 mg/day in 1 dose, and patients with clearance between 30–59 mL/min should receive 400–1400 mg/day in 2 doses Can be removed by hemodialysis; patients receiving hemodialysis may require supplemental doses of gabapentin Use in renal impairment has not been studied in children under age 12 Hepatic Impairment No available data but not metabolized by the liver and clinical experience suggests normal dosing Cardiac Impairment No specific recommendations Elderly Some patients may tolerate lower doses better Elderly patients may be more susceptible to adverse effects Pregnancy C |
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Gabapentin (Neurontin)
The art of psychopharmacology |
Potential Advantages
Chronic neuropathic pain Has relatively mild side effect profile Has few pharmacokinetic drug interactions Treatment-resistant bipolar disorder Potential Disadvantages Usually requires 3 times a day dosing Poor documentation of efficacy for many off-label uses, especially bipolar disorder |
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Gabapentin (Neurontin)
primary target symptoms |
Primary Target Symptoms
Seizures Pain Anxiety |
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Gabapentin (Neurontin)
Pearls |
Pearls
Gabapentin is generally well-tolerated, with only mild adverse effects Well-studied in epilepsy and postherpetic neuralgia Most use is off-label Off-label use for first-line treatment of neuropathic pain may be justified Off-label use for second-line treatment of anxiety may be justified Off-label use as an adjunct for bipolar disorder may not be justified Misperceptions about gabapentin’s efficacy in bipolar disorder have led to its use in more patients than other agents with proven efficacy, such as lamotrigine Off-label use as an adjunct for schizophrenia may not be justified May be useful for some patients in alcohol withdrawal One of the few agents that enhances slow-wave delta sleep, which may be helpful in chronic neuropathic pain syndromes May be a useful adjunct for fibromyalgia Drug absorption and clinical efficacy may not necessarily be proportionately increased at high doses, and thus response to high doses may not be consistent |
