WMiranda Pharm Exam 7 - Anxiolytics & Sleep PDF

Benzodiazepines alprazolam (Xanax): works quickly & has a moderate half-life. Xanaxs quick onset = rapid relief of symptoms. These are often the most addictive. lorazepam (Ativan): commonly used for anxiety--it has a slower onset & a shorter half-life. diazepam (Valium): fairly long half-life....

Benzodiazepines alprazolam (Xanax): works quickly & has a moderate half-life. Xanaxs quick onset = rapid relief of symptoms. These are often the most addictive. lorazepam (Ativan): commonly used for anxiety--it has a slower onset & a shorter half-life. diazepam (Valium): fairly long half-life. Used to help reduce spasm & decrease seizure activity. Indications: Anxiety, Seizure disorder, PD. Due to their rapid onset of action, benzos are often used for immediate relief from an acute anxiety attack until a safer anxiolytic agent (SSRI/SNRI or Buspirone) can take effect &/or resolve insomnia. MOA: Boost effect of neurotransmitter GABA prescribe benzos cautiously & for as Safety/Contraindications/D2D: short a time as possible Contraindicated in pregnancy. Caution in people with sleep apnea. Caution in those with history of alcohol or substance abuse. Combining opioids (or alcohol) & benzos can = severe respiratory depression & death. Special: Schedule IV drugs. Routine daily use may = physical dependence & is highly discouraged For a pt who has chronically used benzos, abrupt D/C can = seizures; therefore D/C should be gradually tapered over many weeks.  SSRIs escitalopram (Lexapro) Anxiety paroxetine (Paxil) Both citalopram (Celexa) Depression fluoxetine (Prozac) sertraline (Zoloft) BBW: Suicide risk, especially Indications: Depression & Anxiety early on, may increase. GAD, SAD, PTSD, PD, OCD Antidepressant-induced suicide apply mainly to MOA: SSRIs block reuptake of serotonin resulting in an  concentration of serotonin in the synapse &  activation children, adolescents, & of postsynaptic serotonin receptors. adults under 25 years old. Safety/Contraindications/D2D: Abrupt D/C may result in withdrawal symptoms. Serotonin syndrome is a rare but serious complication. SSRIs & SNRIs: Generally Increased suicidal ideation the first 2-3 weeks. the drugs of choice for May cause n/v, insomnia, weight gain, sexual dysfunction. depression &/or chronic anxiety r/t their low abuse Use caution with elderly. Start low & go slow. potential, lack of lethality Special: with overdose, & Zoloft, Paxil, Fluvox safe & first line in breastfeeding. effectiveness. Avoid Paxil in pregnancy. Prozac NOT first line for breastfeeding. Prozac most studied for children.  SNRIs venlafaxine (Effexor) duloxetine (Cymbalta) desvenlafaxine SR (Pristiq) SSRIs & SNRIs: Generally the drugs of choice for Indications: Depression & Anxiety depression &/or chronic AD, PD, PTSD anxiety r/t their low abuse potential, lack of lethality with overdose, & MOA: effectiveness. Boost serotonin & norepinephrine Safety/Contraindications/D2D: Venlafaxine may cause HTN & must be avoided with MAOI. Special: Venlafaxine can be used for post-menopausal hot flashes.  Anxiolytic buspirone (BuSpar) Indications: Anxiety MOA: Unknown. Is NOT a CNS depressant. Safety/Contraindications/D2D: Takes several wks to work. Not for PRN use. Not for long term TX of anxiety (up to a yr). No abuse potential. D2D: Erythromycin, Ketoconazole & grapefruit juice can greatly  levels of buspirone Side Effects: Dizziness, N/A, HA, drowsiness.  Antihistamine Hydroxyzine (Atarax, Vistaril) Indications: Anxiety Sleep MOA: Antihistamine Safety/Contraindications/D2D: Anticholinergic side effects. Use with caution in elderly. There are NO abuse or addiction concerns with this med. It is a strong antihistamine & will cause side effects consistent with antihistamines but in pts with severe anxiety can offer some relief of anxiety. Special: May use in pregnancy.  Beta Blocker propranalol (Inderal) Take an hour before the event: is typically effective in reducing Indications: symptoms & does Performance anxiety NOT cause sedation. MOA: Decreases symptoms caused by autonomic hyperactivity o Tremors, sweating, tachycardia, palpitations Safety/Contraindications/D2D: Not to be used in patients already taking beta blocker or other cardiac issues.  Herb St. John's Wort Indications: Sleep, anxiety, improves mood Safety/Contraindications/D2D: Many D2D including but not limited to triptans, benzos, contraceptives, digoxin, SSRIs, antibiotics. Risk of severe phototoxic skin reactions.  Sedative Benzodiazepines estazolam (ProSom) flurazepam (Dalmane) temazepam (Restoril) Indications: Sleep Safety/Contraindications/D2D: For short term use only (10 days maximum). Risk for dependence. Contraindicated in elderly r/t risk of cognitive impairment, falls, & fractures Rapid dose decrease can = withdrawal symptoms.  Non-benzodiazepines Eszopiclone (Lunesta): only drug recommended for long-term use. zaleplon (Sonata) to be used for a maximum of 35 days. zolpidem (Ambien) Safety/Contraindications/D2D: Zolpidem (Ambien) has sex-specific dosing: lower doses for women Zolpidem comes in a sublingual form (Edluar) & nasal spray (ZolpiMist). Short term use. Special: Lunesta recommended for long term use. All others to be used for maximum of 35 days.  Melatonin agonist ramelton (Rozerem) Indications: Sleep MOA: Activates receptors for melatonin. Safety/Contraindications/D2D: May increase levels of prolactin & decrease levels of testosterone. D2D- fluvoxamine (Luvox) can increase levels of ramelteon more than 50-fold. Caution or avoid in people with hepatic impairment. Avoid in pregnancy & lactation. Special: Used for difficulty with sleep onset. May be used for long term.  TCAs Amitriptyline Clomipramine The lethality of these drugs Doxepin with overdose made their use risky & pts could only Imipramine be given small amounts of their meds at a time. Indications: Depression MOA: Block reuptake of norepinephrine & serotonin. Safety/Contraindications/D2D: Anticholinergic side effects. Use with caution in elderly. Contraindicated in pts with cardiac issues. Risk of cardiac toxicity. May lead to dysrhythmias & may be fatal with overdose. D2D interactions – MAOI, CNS depressants, sympathomimetics, anticholinergic drugs. Special: Can be helpful for those with sleep issues or chronic pain  MAO Inhibitors Isocarboxazid Phenelzine Indications: Depression MOA:  the amount of norepinephrine & serotonin for release by inhibiting intraneuronal MAO-A. Safety/Contraindications/D2D: Risk for hypertensive crisis. Avoid fermented or aged foods. Tyramine rich foods. Many D2D interactions. Contraindicated in elderly. Typically prescribed by psych. Reserved for pts who have not responded to SSRIs, TCAs & other safer drugs.  Atypical Antidepressant Bupropion (Wellbutrin) Indications: Depression Smoking cessation MOA: Boosts norepinephrine & dopamine. which can be stimulating/energizing. Safety/Contraindications/D2D: May increase frequency & severity of seizures in those with a seizure disorder. Special: Improved focus & concentration can be seen. Decreased appetite, increased libido. Trazodone (triazolopyridine) tends to be very sedating & is helpful in mildly depressed clients with insomnia. Ketamine Indications: Depression MOA: Blocks NMDA receptor, decreasing glutamate binding. Special: Given IV. Effect lasts 1-2 weeks. Esketamine (the S enantiomer of ketamine) was approved for intranasal administration for treatment- resistant depression in conjunction with a conventional oral antidepressant medication. Brexanolone (Zulresso) Indications: Depression first FDA approved treatment specifically for post-partum depression. MOA: Modulates GABA Special: Very expensive. Given IV in a monitored, specialized healthcare setting, over a total period of 60 hours with a specific stepped dosing regimen. Used in postpartum people.  First Generation/Conventional Antipsychotics Haloperidol (Haldol) Chlorpromazine Indications: Antipsychotic Schizophrenia The effects are non-selective & led to pronounced negative EPS side MOA: Block receptors in & out of CNS such as effects such as tardive dyskinesia. dopamine, acetylcholine, histamine & Another concerning side effects norepinephrine. They suppress symptoms of are galactorrhea, amenorrhea, psychosis. sexual dysfunction, & weight gain. Safety/Contraindications/D2D: Contraindicated in pts who are severely depressed or comatose or with Parkinson’s. Prolong QT interval. D2D interactions – anticholinergics, CNS depressants, Levodopa. Special: Blood monitoring – CBC, electrolytes, liver and heart functions.  Second Generation/Atypical Antipsychotics Clozapine Olanzapine Ziprasidone Aripirazole Indications: Schizophrenia BBW: Clozapine can cause life- threatening agranulocytosis MOA: D2 antagonist & serotonin 2A antagonist as well as it has been associated with myocarditis. Safety/Contraindications/D2D: Cardiometabolic risks: weight gain, obesity, dyslipidemia, diabetes, & accelerated cardiovascular disease. o Clozapine & olanzapine have the highest risk for these side effects. o Ziprasidone & aripiprazole have the lowest risk Special: Help with the positive & negative effects of schizophrenia Fewer negative side effects than the conventional antipsychotics  Iminostilbenes Carbamazepine (Tegretol) Indications: Partial seizures & generalized tonic-clonic seizures. Bipolar. BBW: Trigeminal neuralgia. May cause SJS & TEN (Toxic epidermal necrolysis). MOA: Suppress sodium influx Aplastic anemia & agranulocytosis. Safety/Contraindications/D2D: Depression is a concern for all antiseizure drugs. Bone marrow suppression. Many D2D interactions particularly oral contraceptives & folic acid. Grapefruit juice can increase peak & trough of carbamazepine. High incidence SJS in Asian people: should be screened for the variant HLA-B1502 allele prior to initiating therapy. Special: Compatible with breastfeeding.  Hydantoin Phenytoin (Dilantin) Indications: Tonic-clonic or partial seizures. Epilepsy. Seizures after head trauma, neurosurgery and hemorrhagic stroke. MOA: Suppress sodium influx BBW: Rapid IV administration can Safety/Contraindications/D2D: cause severe hypotension & Many D2D interactions. cardiac dysrhythmias. Teratogenic. Pregnancy cat D SJS. Phenytoin induced hepatitis is a common hypersensitivity reaction. contraindicated in pts with sinus bradycardia, SA block, second & third-degree AV block, & Stokes-Adams Syndrome. Special: Compatible with breastfeeding.  Succinimide Ethosuximide (Zarontin) Valproic acid (Depakote) lamotrigine (Lamictal) Indications: preferred meds for absence seizures (generalized seizure resulting in petit mal) MOA: Unknown. May increase GABA concentration in brain or augment inhibitory influence of GABA. Safety/Contraindications/D2D: Valproic acid reduced by 2 carbapenem antibiotics – meropenem & imipenem/cilastatin. Increased fetal neural tube defects. BBW: Valproic acid & lamotrigine have fewer side effects Valproic acid: fatal hepatic & are the preferred meds for absence seizures. failure risk. Fatal & rapidly progressing pancreatitis. Special: Valproate is highly Compatible with breastfeeding. teratogenic. Obtain platelet counts before initiating therapy with valproic acid, & at regular intervals. Any bleeding or bruises should be investigated.  Cholinesterase Inhibitors Donepezil (Aricept) Indications: Mild to moderate symptoms MOA: Prevent the breakdown of actylcholine. 1. Excitatory neurotransmitter 2. Involved in learning and memory formation in hippocampus 3. Also, a role in regulating REM sleep cycles Safety/Contraindications/D2D: D2D: anticholinergic agents, first-generation antihistamines, TCAs, - all can reduce therapeutic effects & should be avoided. Side Effects: Weight loss, N/V, diarrhea, dizziness, muscle cramps, may increase seizure risk (rare). Can prolong Qt Precautions: bradycardia, conduction defects, asthma, COPD Special: Improved cognition (thinking) & function for patients with AD.  NMDA receptor antagonists Memantine (Namenda) Indications: Moderate or severe AD. MOA: Blocks excessive excitation of NMDA receptors by glutamate as overexcitation by glutamate is cytotoxic. Safety/Contraindications/D2D: Side Effect: Dizziness – risk for falls. D2D: Drugs with memantine & sodium bicarb may have undesired additive effect. Use cautiously in patients with renal impairment. Special: Helps treat symptoms of AD but no evidence that it modifies the underlying disease process.  Stimulants Methylphenidate (Ritalin, Concerta) Dextroamphetamine (Dexedrine) Indications: First line treatment of ADHD MOA: Amplify norepinephrine & BBW: dopaminesignals that are low in ADHD. Chronic abuse of methylphenidate can lead to marked tolerance & psychological dependence with Safety/Contraindications/D2D: varying degrees of abnormal May cause insomnia & restlessness, behavior & possible frank psychotic suppress appetite leading to weight loss. episodes. Small increase in heart rate & blood pressure. Amphetamines have a high potential for abuse & dependence. In pts who use amphetamines chronically, withdrawal may occur if use of these meds are suddenly stopped.  Non-Stimulants Atomoxetine (Strattera) Clonidine (Kapvay) Indications: Second line treatment of ADHD MOA: Inhibits norepinephrine reuptake, increasing NE Safety/Contraindications/D2D: Less effective than stimulants. Adverse effects: dyspepsia, n/v, decreased appetite, dizziness, somnolence, mood swings. *Atomoxetine may cause suicidal thinking in children & adolescents but not in adults. Small risk of severe liver injury.  Dopamine replacement Levodopa/Carbidopa Indications: PD MOA: Undergoes conversion to DA in the brain & activates DA receptors (Carbidopa blocks destruction of levodopa in the periphery). Safety/Contraindications/D2D: Good for initial treatment of PD. *Must avoid high protein meals. Side effects: n/v, tremor, hypotension, palpitations, dizziness. Possible psychosis. D2D: first generation antipsychotic drugs, MAOI’s, anticholinergics & pyridoxine. Special: First line drug or used as a supplement to a dopamine agonist. Pt education must include what to expect from the effects of Levodopa, D2D & no high-protein meals as amino acids will compete with levodopa for absorption which can result in a decrease in the amount of Levodopa that is transported to the brain. Dopamine Agonists Nonergot Derivatives: very selective for dopamine receptors Apomorphine Ropinirole Rotigotine Egot Derivatives: less selective Bromocriptine Indications: May be used as supplement to Levodopa MOA: Activate dopamine receptors in the striatum Safety/Contraindications/D2D: Hallucinations, sleep attack, postural hypotension  Anticholinergic Drugs Benztropine (Cogentin) Indications: Supplement to Levodopa MOA: Block cholinergic receptors in the CNS; help restore balance between dopamine & ACh Safety/Contraindications/D2D: Dry mouth, blurred vision, photophobia, urinary retention, constipation, tachycardia. Special: Increase benefits of levodopa