, Mood Stabilizer List PHRM 203

Generic Name Trade Name Class/Indication(s)/Notes “Pronunciation” Alprazolam Xanax • C-IV; Benzodiazepine (BZD) “al PRAY zoe lam” • Short-acting with active metabolites, t ½ ~ 12 hours • PO only Diazepam Valium • C-IV; BZD used to treat acute alcohol withdrawal, epilepsy, tremors/spasms, “dye AZ e pam)” athetosis (continuous, involuntary, slow, writhing movements of, usually, hands/feet; part of a continuum of epilepsy mimics with ballismus & chorea). • Long-acting with active metabolites (t ½ up to 10 days) • 3-5% of whites are poor metabolizers due to polymorphism of CYP2C19. High variability in . T ½ 24-60 hrs, usually. • PO, IM, IV, PR Lorazepam Ativan • C-IV; BZD used as a sedative, anxiolytic, amnesiac preanesthetic, status “lor A ze pam” epilepticus • Intermediate-acting without active metabolites • t ½ is around 15 hours • PO, IM, IV Midazolam Hypnovel, • C-IV; BZD used as a sedative, anxiolytic, strong amnesiac preanesthetic, “meh-DAZE-oh-lam” Versed induction of general anesthesia. • Short-acting (t ½ is abour 2.5 hours, but effects on memory may last for days) • IV, IM, PO (syrup) • Boxed warning: Respiratory arrest. Thiopental Pentothal • C-III; Highly lipid soluble Barbiturate used as a Parenteral “thigh-oh-PEN-tahl” • IV/IM • See lecture Phenobarbital Luminal • C-IV; More polar Barbiturate used as a short-term hypnotic for insomnia, “feen oh BAR bit al” long-term anti epileptic, preanesthetic sedative. Off label uses include febrile seizures in kids, hyperbilirubinemia in newborns, and chronic cholestasis. • Not • Long t ½ (53-118 hours) leads to “hangover” sedation on following day • REM rebound (very vivid dreams) on drug withdrawal due to suppression of REM • PO, IM Zolpidem Ambien, • C-IV; non-BZD GABAA agonist; Short-term hypnotic for insomnia “zole PI dem” Zolpimist, • Decrease dose by ½ in the elderly; women take ½ dose of men. Intermezzo • PO (tablets and oral spray). T ½ is 2 – 2.5 hours. • Tolerance, dependence and rebound insomnia a problem. May cause (sublingual “sleepwalking.” tablets) Eszopiclone Lunesta • C-IV; non-BZD GABAA agonist; Short-term hypnotic for insomnia. “es ZOP ih clone” • Note: extremely rapid onset. May cause “sleepwalking.” • PO. T ½ is 5 – 7 hours. • Decrease dose by ½ in the elderly and liver patients

Page 1 of 4 Sedative Hypnotic, Mood Stabilizer Drug List PHRM 203

Generic Name Trade Name Class/Indication(s)/Notes “Pronunciation” Diphenhydramine Benadryl • Sedating 1st generation Antihistamine used for short-term “DYE fen HYE dra treatment of insomnia, motion sickness, Parkinson’s disease and meen” drug-induced extrapyramidal symptoms, and all allergic reactions. • See Autocoids lecture Buspirone BuSpar • Non sedating anxiolytic “byoo SPYE rone” • PO, poor absorption with high 1st pass • See Autocoids lecture Propranolol Inderal • – off label non-sedating anxiolytic. Indicated for HT, “pro PRAN oh lol” angina, migraine, hypertrophic subaortic stenosis and as a class II anti arrhythmic. • See PNS and CV 1 & 2 lectures • Boxed warning: rebound angina/MI. Lithane, Happy • ; . “LITH ee um” Happy, Eskalith, • Note: causes weight gain, lithium-induced tremor, goiter Lithobid, etc. (supresses thyroid hormone release), alopecia etc. • Thiazide or NSAIDs decrease excretion a toxicity • Greatly reduces the risk of suicide (until lithium is no longer taken, then risk is increased) • Boxed warning: narrow therapeutic margin Equetro, Tegretol • AED; Mood stabilizer (Bipolar disorder). “kar ba MAZ e peen” • PO • See ADHD & AEDs lecture • Boxed warnings: (1) SJS in patients with HLA-B1502 gene; (2) Aplastic anemia and (3) Divalproex Depakote • AED; Mood stabilizer (Bipolar disorder). Divalproex also used for “dye val PRO ex” migraine prophylaxis, valproic acid and are AEDs only. Valproic acid is • PO (valproate avail IV). Divalproex is a 1:1 mix of valproic acid Depakene and valproate. • Note: causes weight gain, tremors, alopecia. Shown to reduce Valproate is the cognitive test scores of kids exposed in utero.

Depacon • Boxed warning: (1) hepatotoxic, (2) pancreatitis, (3) Teratogenic Lamictal • AED; Mood stabilizer (Bipolar disorder). “la MOE tri jeen” • PO • Don’t give with valproate • Boxed warning: Serious skin reactions in patients with HLA- B1502 gene.

Page 2 of 4 Sedative Hypnotic, Mood Stabilizer Drug List PHRM 203

Generic Name Trade Name Class/Indication(s)/Notes “Pronunciation” Zyprexa • Atypical with indications to treat in “oh LANZ a peen” Bipolar Disorder Risperdal • Boxed warning: increased mortality risk in the elderly with “ris PER i done” Seroquel • Additional boxed warning for Quetiapine: suicide. “kwe TYE a peen” • See also & Antipsychotics lecture Doxepin Sinequan • Tricyclic with indication to treat depression “DOX e pin” in Bipolar Disorder • Boxed warning: suicide Olanzapine + Symbyax • Combination of an atypical with an SSRI fluoxetine antidepressant with an indication to treat Bipolar Disorder and treatment resistant MDD. • Individualize dose based on gender (females less than males), age (elderly less), nonsmokers (less than smokers), and those with liver disease. • Taper off to avoid discontinuation syndrome. • Boxed warnings: (1) increased mortality risk in the elderly with dementia; (2) suicide

Notes: 1. Benzodiazepines, and other GABAA agonists, have effects similar to alcohol. The BZD are said to “replace” alcohol effects, so they can be used to treat alcohol withdrawal symptoms. 2. In general the BZD have the following effects a. Sedation b. Hypnosis c. Anxiolysis d. AED/ (not a direct effect) e. Amnesiac f. THEY ARE NOT ANTIDEPRESSANT g. THEY ARE NOT ANALGESIC 3. There are substantial individual differences in metabolism and excretion of certain BZD that mainly impacts those with active metabolites like Diazepam. There is polymorphism in CYP2C19 that affects the metabolism of Diazepam such that 3-5% of Caucasians are poor metabolizers. 4. Flumazenil (Romazicon) is the reversal agent for BZD OD. a. It may precipitate withdrawal symptoms (e.g., seizures) in BZD tolerant patients b. It causes seizures (which limits total dose to 3-4 courses), risk greatest with TCA c. It has a shorter t ½ (40-80 minutes) than most BZD and effects aren’t seen until 6-7 minutes after injection. d. If a person has eaten prior to therapy with flumazenil, the t ½ is decreased by up to 50% due to increased flow through the liver (hence greater hepatic clearance). e. It doesn’t reverse other GABA-A agonists (barbiturates, general anesthetics, alcohol)

Page 3 of 4 Sedative Hypnotic, Mood Stabilizer Drug List PHRM 203

5. The sedative generally require individualization in the elderly and in those with liver disease. a. Women (and the elderly) take ½ the dose that men take of i. “Intermezzo,” sublingual tablets of zolpidem ii. “Ambien” iii. Eszopiclone (also decrease dose by ½ in liver patients) 6. Withdrawal syndrome for BZD a. Taper patients off to avoid withdrawal b. Similar to alcohol or barbiturate withdrawal c. Symptoms affect a constellation of systems and occur at varying times, often for months i. Anxiety, fear, agitation, depression, paranoia, , feelings of unreality, thoughts and feelings of persecution or hostility, increased sensitivity to light/noise/taste/smell, confusion, , etc. ii. Sleeplessness, hallucinations, visual disturbances, etc. iii. Paresthesias, , etc. iv. GI upset, headache, muscle pain, etc. v. Seizure, coma, death 7. Other include the neuromodulators (AEDs) a. (Topamax) b. Pregabalin (Lyrica) c. (Neurontin), etc. 8. HLA = Human Leukocyte Antigen, these receptors are involved in self-recognition. 9. Delirium is present in about 20% of hospital patients. It generally consists of: a. and/or hallucinations b. Aggression and mood changes c. Sleep/wake problems d. Limited or absent ability to form new memories (forgetfulness)

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