POWERPOINT+Chapter+20+for+4th+Edition.pptx

Theraputic Drugs for the Nervous System

1. Chapter 20 Therapeutic Drugs for the Nervous System Jahangir Moini , The Pharmacy Technician A Comprehensive Approach, Second Edition. © 2011 Cengage . All Rights Reserved. May not be scanned, copied or duplicated, or posted to a publicly accessible website, in whole or in part.

2. Overview The nervous system consists of the interconnected neurons of the: Brain Spinal cord Nerves Neurons carry electrical impulses for: Control and regulation of body activities

3. Nervous System The nervous system is divided into two sections: Central nervous system (CNS) Peripheral nervous system (PNS)

4. Anatomy and physiology of the nervous system

5. Central Nervous System The CNS is located in the dorsal cavity, including the: Brain (in the cranium) Spinal cord (in the spinal cavity) It receives information from: The afferent division of the peripheral nervous system It sends instructions to the body via The efferent division of the PNS

6. The Brain (1 of 2) Cerebrum – largest portion: With two hemispheres connected by the corpus callosum Diencephalon – contains the: Thalamus, which relays incoming impulses, Hypothalamus, which maintains homeostasis

7. The Brain (2 of 2) Brainstem – consists of the: Midbrain Pons Medulla oblongata; the major autonomic control center of blood pressure, heart rate, breathing, and digestion Cerebellum – consists of: Two hemispheres coordinating: Skeletal muscle movements Equilibrium

8. cerebrum, diencephalon, brain stem, cerebellum

9. Peripheral Nervous System The PNS is outside the CNS: Connecting it to the remainder of the body Consists of 12 pairs of cranial and 31 pairs of spinal nerves, which branch to all body parts Subdivided into the: Autonomic nervous system Somatic nervous systems

10. Subdivisions of the PNS and CNS

11. Cranial and spinal nerves

12. Primary functions of the cranial and spinal nerves Table 20.1 Classifications of Cranial Nerves and Their Functions Name, Number Functions Olfactory (I) Sensory (special sensory: smell). Mucous membranes in the nose send information to part of the cerebral cortex, which processes it, then sends responses resulting from the information Optic (II) Sensory (special sensory: vision). The optic nerves receive images captured by the retinas. They travel through the thalamus to the visual cortex for processing Oculomotor (III) Motor (eye movements). Related muscles are involved in movement of parts of the eyes and eyelids Trochlear (IV) Motor (eye movements). Control other areas of the eyes related to eye movements Trigeminal (V) Mixed (sensory and motor, to face). Located in the brainstem, providing sensations to the scalp, face, eyes, nasal mucous membranes, and mouth; also responsible for sensations in the skin and muscles of the jaw Abducens (VI) Motor (eye movements). Provides even more control of eye movements Facial (VII) Mixed (sensory and motor, to face). Involved in taste sensation at the front of the tongue. Connected to face and head muscles, controls facial expressions Vestibulocochlear (VIII) Sensory (special sensory: balance and equilibrium via vestibular nerve, and hearing via cochlear nerve). Connected to inner ear Glossopharyngeal (IX) Mixed (sensory and motor, to head and neck). Connected to sinuses, back of tongue, soft palate, parotid glands, and reflexive control of the heart; also involved in swallowing Vagus (X) Mixed (sensory and motor, widely distributed in thorax, abdomen). Extends from brainstem through the neck to reach final locations. Involved in swallowing, breathing, heartbeat, speaking, and digestion. Connected to nerves that receive messages from the ears, pharynx, chest, esophagus, and abdominal areas Accessory (XI) Motor (to muscles of neck and upper back). There are two divisions. Cranial branch controls pharynx, larynx, and palate muscles, helping in swallowing and digestive tract movements. Spinal branch assists in muscle movements of the head, neck, and upper shoulders Hypoglossal (XII) Motor (controls the movements of the muscles of the tongue)

13. Autonomic Nervous System The ANS: Controls homeostasis With no conscious effort It is subdivided into the: Sympathetic nervous system – Responds to stress and emergency situations Parasympathetic nervous system – Most active under ordinary conditions

14. Sympathetic nervous system

15. Parasympathetic nervous system

16. Somatic Nervous System Voluntary control of body movements Reception of external stimuli Made up of fibers of motor neurons: Supply skeletal muscles Under voluntary control; however: Many skeletal muscle activities used in balance, posture: Are subconsciously controlled

17. Neurons Neuron : basic cell of the nervous system It carries nerve impulses between body parts A neuron has a cell body, and: Dendrites – Receptors carrying information to the cell body Axons – Which carry nerve information away from the cell body

18. Parts of a neuron

19. Neurotransmitters At neuron junctions, continuation of messages: Via acetylcholine (ACh) and other neurotransmitters ACh stimulates nerve endings Cholinesterase inhibits ACh Neurohormones are different neurotransmitters: Norepinephrine Epinephrine Dopamine Serotonin Endorphins

20. Disorders of the Nervous System and Their Treatments Migraine headache - Stroke Epilepsy - Parkinson’s disease Bell’s palsy - Tic douloureux Multiple sclerosis - Alzheimer’s disease Schizophrenia - Bipolar disorder Anxiety disorders - Sleep disorders Major depressive disorder

21. Migraine Headache (1 of 2) Involves periodic, severe pain Can totally incapacitate the patient Usually accompanied by: Nausea Vomiting Visual signs and symptoms

22. Migraine Headache (2 of 2) Treatment often involves bed rest in a dark room Also, analgesics Disease-modifying immunotherapies: Such as interferon

23. Stroke Arterial blockage of blood to the brain Most are ischemic : from blockage or narrowing Some are hemorrhagic : with actual bleeding Outcomes: Limb weakness Paralysis of one side of the body Loss of speech

24. Epilepsy (1 of 2) A chronic brain disorder Sudden, abnormally intense electrical activity Results in seizures There are 30+ types Partial seizures: Often arise from the cerebral cortex or another local area Generalized seizures: Have multiple foci that may cause loss of consciousness

25. Epilepsy (2 of 2) Convulsions: Involuntary muscle contractions Treatments: Anticonvulsants Rarely, surgical intervention: To remove identified brain lesions

26. Partial seizures

27. International classification of seizures Table 20.2 Classifications of Seizures Type Description Generalized Seizures Absence (petit mal) Level of consciousness is changed briefly; there is eye blinking or rolling, a blank stare, and slight movements of the mouth. It takes about 10 seconds, and it is seen more in children Tonic- clonic (grand mal) Usually begins with a loud cry due to air that rushes from the lungs through the vocal cords; the patient falls, losing consciousness; the body stiffens and then experiences spasms and relaxations Akinetic More common in children: there is an overall loss of postural tone, and temporary loss of consciousness; also called a drop attack Myoclonic Clinically described as bilateral massive epileptic myoclonus ; involves brief and involuntary muscular jerks of the body or extremities Status epilepticus Continuous seizures; may be related to all other forms, and accompanied by loss of consciousness with respiratory distress—may be life-threatening; can be due to an abrupt withdrawal of anticonvulsants, encephalopathy, head trauma, or septicemia (because of meningitis) Partial Seizures Complex partial Have varied effects, sometimes with behaviors that are without purpose; an aura occurs immediately before the seizure—nausea, pungent smells, dream-like sensations, unusual tastes, or visual disturbances; behavioral changes include “picking” at clothing, glassy stare, wandering, unintelligible speech, lip-smacking, or lip-chewing; symptoms last from seconds to 20 minutes; after these seizures, there may be mental confusion Simple partial motor Jerking or stiffening in one extremity, followed by tingling sensations in the same area; consciousness usually retained, but seizure may progress to a generalized seizure Simple partial sensory Involves hallucinations and other perceptual distortions

28. Examples of anti-epileptic drugs Table 20.3 Examples of Antiepileptic Drugs (Anticonvulsants) Generic Name Trade Name Route of Administration Average Adult Dosage carbamazepine Tegretol ® , Tegretol XR ® PO 200 mg bid, gradually increased to 800 to 1200 mg/day in three to four divided doses. Tegretol XR dosed bid ethosuximide Zarontin ® PO 250 mg bid, may increase q4 to 7d prn (maximum 1.5 g/day) lamotrigine Lamictal ® PO 25 mg/day, may increase up to 375 mg/day levetiracetam Keppra ® PO Initial: 1000 mg/day, in two divided doses, may increase up to maximum 3000 mg/day lorazepam Ativan ® IV for status epilepticus 4 mg injected slowly at 2 mg/min, may repeat dose once if inadequate response after 10 minutes oxcarbazepine Trileptal ® PO Initial: 600 mg/day, bid. May be increased by up to 600 mg/day in weekly intervals (maximum 1200 mg/day) phenobarbital Luminal ® PO, IM. IV PO: 100 to 300 mg/day; IV/IM: 200 to 600 mg up to 20 mg/kg phenytoin Dilantin ® PO, IV PO: 15 to 18 mg/kg or 1 g loading dose, then 300 mg/day in one to three divided doses; IV: 15 to 18 mg/kg or 1g loading dose, then 100 mg tid tiagabine hydrochloride Gabitril ® PO Start with 4 mg every day, may increase dose by 4 to 8 mg/day q week valproic acid Depakene ® PO, IV PO and IV: Start with 10 to 15 mg/kg/day; increase by 5 to 10 mg/kg/week to achieve optimal clinical response

29. Parkinson’s Disease (1 of 2) A slowly progressive degenerative disorder Affects motor function Through loss of extrapyramidal activity Muscle tremor Rigidity Bradykinesia Posture and equilibrium disturbances “Pill-rolling” movements of thumb and forefinger

30. Parkinson’s Disease (2 of 2) Substantia nigra mostly affected Inadequate amounts of dopamine secreted Bowed head; body flexed forward; shuffling gait Treatments are supportive: Levodopa Carbidopa Antidepressants Anticholinergics Selegiline Rasagiline Pramipexole Ropinirole Physical therapy

31. Signs of Parkinson’s disease

32. Acetylcholine and dopamine imbalance

33. Drugs used for Parkinson’s disease (1 of 2) Table 20.4 Examples of Anti-Parkinson Drugs Generic Name Trade Name Route of Administration Average Adult Dosage amantadine Symmetrel ® PO 100 mg 1 to 2 times/day, start with 100 mg/day if patient is on other anti-Parkinsonism medications benztropine Cogentin ® PO 0.5 to 1 mg/day, may be gradually increased prn up to 6 mg/day carbidopa / levodopa Sinemet ® PO If not currently receiving levodopa: 1 tablet containing 10 mg carbidopa /100 mg levodopa or 25 mg carbidopa /100 mg levodopa tid , increased by 1 tablet every day to every other day up to 6 tablets/day If currently receiving levodopa: 1 tablet of the 25/250 mixture tid to qid , adjusted by ½ to 1 tablet prn up to 8 tablets/day (start at 20% to 25% of initial dose of levodopa) entacapone Comtan ® PO 200 mg with each dose of carbidopa /levodopa to a maximum of 8 times/day (maximum 1600 mg/day) levodopa Larodopa ® PO 500 mg to 1 g daily in two or more equally divided doses, may increase by 100 to 750 mg q3 to 7d (maximum 8 g/day); if used in combination with carbidopa , decrease levodopa dose by 75% to 80%

34. Drugs used for Parkinson’s disease (2 of 2) Table 20.4 Examples of Anti-Parkinson Drugs Generic Name Trade Name Route of Administration Average Adult Dosage pramipexole Mirapex ® PO Initial: 0.375 mg/day in three divided doses, not to be increased more frequently than q5 to 7d Maintenance: 1.5 to 4.5 mg/day in three divided doses, with or without levodopa at 800 mg/day rasagiline Azilect ® PO 1 mg/day; may need to be started at 0.5 mg/day initially and then increased; may be used with or without levodopa ropinirole Requip ® PO Initial: 0.25 mg tid , increased in weekly increments as follows: Week two: 0.5 mg tid Week three: 0.75 mg tid Week four: 1 mg tid Increases continue similarly up to maximum dose of 24 mg/day selegiline Zelapar ® Eldepryl ® PO Initial: 1.25 mg/day for at least six weeks; then may increase to 2.5 mg/day trihexyphenidyl Artane ® PO Trihexy ®: 1 mg on day 1, 2 mg on day 2, then increase by 2 mg q3 to 5d up to 6 to 10 mg/day in three or more divided doses (maximum 15 mg/day); Artane ®: 2 to 5 mg in three divided doses taken with meals

35. Bell’s Palsy Paralysis of the facial nerve on one side Causing that side of the face to temporarily “droop” Early treatment required, to prevent permanent effects Treatments: Massage - Heat applications Facial exercises - Prednisone Analgesics - Artificial tears Eye patches - Electrotherapy

36. Tic Douloureux (Trigeminal Neuralgia) Pain in the area innervated by the trigeminal nerve May affect: Forehead - Eyes Nose - Lips Cheeks - Tongue Areas near the ears Treatments: Massage - Heat applications Facial exercises - Prednisone Analgesics - Artificial tears Eye patches - Electrotherapy

37. Multiple Sclerosis Progressive demyelination of nerve cells of CNS: Usually in early adulthood Causes lesions leading to sclerosis of fatty myelin sheaths: Reducing nerve impulse conduction Causing muscle weakness Treatments: Interferon Glatiramer Later, mobility-assisting devices

38. Alzheimer’s Disease (1 of 3) Also known as senile disease complex Common in people older than age 65 Progressive brain atrophy Senile plaques from beta amyloid deposits Most common cause of dementia May be genetically linked in families

39. Alzheimer’s Disease (2 of 3) Progressive short-term memory failure Impaired cognition Inability to learn or reason Confusion Personality changes Difficult to accurately diagnose

40. Alzheimer’s Disease (3 of 3) Treatments are supportive: Cholinesterase inhibitors N-methyl-D-aspartate inhibitors Tacrine Antipsychotics Neuroleptics Antianxiety agents Selective serotonin reuptake inhibitors

41. Alzheimer’s patient

42. Drugs used for Parkinson’s disease Table 20.5 Examples of Drugs Used to Treat Alzheimer’s Disease Generic Name Trade Name Route of Administration Average Adult Dosage Acetylcholinesterase Inhibitors donepezil Aricept ® PO 5 to 23 mg/day galantamine Razadyne ® PO Immediate release: 4 to 12 mg bid; extended release: 8 to 24 mg/day rivastigmine Exelon ® PO, transdermal path PO: 3 to 6 mg bid; patch: 4.6 to 13.3 mg/day N -Methyl-D-aspartate Receptor Antagonist memantine Namenda ® PO Immediate release: 10 mg bid (initial: 5 mg/day, titrating weekly to 10 mg bid); extended release: 14 to 28 mg/day (initial: 7 mg/day titrating up to 28 mg/day)

43. Schizophrenia (1 of 2) Devastating mental illness characterized by: Distortion of reality Disorganized thoughts Social withdrawal Hallucinations Poor judgment May be genetic, causing: Physical brain mass changes Excessive dopamine secretion Decreased blood flow to the front of the brain

44. Schizophrenia (2 of 2) Onset is in late adolescence or early adulthood Treatments: Atypical antipsychotics - Psychotherapy Family counseling - Ziprasidone Quetiapine - Chlorpromazine Haloperidol - Fluphenazine

45. Bipolar Disorder Characterized by: Periods of extreme excitation or mania Periods of deep depression Also called manic-depressive illness Treatments: Hospitalization - Lithium Anticonvulsants - Antipsychotics Antidepressants - Benzodiazepines Substance abuse treatment (if related)

46. Examples of antipsychotic medications (1 of 2) Table 20.6 Examples of Antipsychotic Drugs Generic Name Trade Name Route of Administration Average Adult Dosage lithium Eskalith ® PO 900 to 1800 mg/day in three or four divided doses haloperidol Haldol ® PO,IM PO: 0.2 to 5 mg bid to tid ; IM: 2 to 5 mg repeated q4h prn thiothixene Navane ® PO, IM PO: 2 mg tid , may increase up to 15 mg/day prn or tolerated (maximum 60 mg/day); IM: 4 mg bid to qid (maximum 30 mg/day) trifluoperazine Stelazine ® PO, IM PO: 1 to 2 mg bid, may increase up to 20 mg/day in hospitalized patients; IM: 1 to 2 mg q4 to 6h (maximum 10 mg/day) cariprazine Vraylar ® PO Initial dose is 1.5 mg once daily; may be increased to 3 mg once daily loxapine Loxitane ® PO, IM PO: Start with 10 mg bid and rapidly increase to maintenance levels of 60 to 100 mg/day in two to four divided doses (maximum 250 mg/day); IM: 12.5 to 50 mg q4 to 6h

47. Examples of antipsychotic medications (2 of 2) Table 20.6 Examples of Antipsychotic Drugs Generic Name Trade Name Route of Administration Average Adult Dosage perphenazine Perphenazine ® PO,IM, IV PO: 4 to 16 mg bid to qid ; 8 to 32 mg sustained release bid (maximum 64 mg/day); IM: 5 mg q6h (maximum 15 to 30 mg/day); IV: Dilute to 0.5 mg/mL in NS, administer at not more than 1 mg q1 to 2 min or 5 mg by slow infusion chlorpromazine Thorazine ® PO,IM, IV PO: 25 to 100 mg tid to qid , may need up to 1000 mg/day; IM/IV: 25 to 50 mg up to 600 mg q4 to 6h thioridazine Mellaril ® PO 50 to 100 mg tid , may be increased up to 800 mg/day prn or as tolerated clozapine Clozaril ® PO Initial: 25 to 50 mg/day, titrate to target dose of 350 to 450 mg/day in three divided doses at 2-week intervals; increase prn (maximum 900 mg/day) olanzapine Zyprexa ® PO Initial: 5 to 10 mg/day, may be increased by 2.5 to 5 mg q week until desired response (usual range: 10 to 15 mg/day, maximum 20 mg/day) quetiapine Seroquel® PO Initial: 25 mg bid, may be increased by 25 to 50 mg bid to tid on second or third day as tolerated to target a dose of 300 to 400 mg/day in divided doses bid to tid , may adjust dose by 25 to 50 mg bid every day prn (maximum 800 mg/day)

48. Major Depressive Disorder Mood disorder characterized by: One or more major depressive episodes Major depression (unipolar disorder): A chemical deficit within the brain Treatments: Psychotherapy Antidepressants (with SSRIs used first) Serotonin-norepinephrine reuptake inhibitors (SNRIs) Atypical antidepressants Family education Electroconvulsive therapy

49. Examples of antidepressants (1 of 3) Table 20.7 Examples of Antidepressants Generic Name Trade Name Route of Administration Average Adult Dosage Selective Serotonin Reuptake Inhibitors (SSRIs) citalopram Celexa ® PO 20 mg/day, increased to maximum dose of 40 mg/ day at an interval of no less than one week escitalopram Lexapro ® PO 10 mg/day fluoxetine Prozac ® PO 20 to 80 mg/day, in the morning fluvoxamine Luvox ® PO Initial: 50 mg/day at bedtime; Maint : 100 to 300 mg/day paroxetine Paxil ® PO 20 mg/day, in the morning sertraline Zoloft ® PO 50 mg/day Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs) desvenlafaxine Pristiq ® PO 50 mg/day duloxetine Cymbalta ® PO 40 to 60 mg/day, in two divided doses venlafaxine Effexor ® PO 75 mg/day, in two to three divided doses, with food Atypical Antidepressants bupropion Wellbutrin ® PO Initial: 150 mg/day, in the morning; Maint : if tolerated, increase to 300 mg/day on day 4, in the morning mirtazapine Remeron ® PO 15 mg/day, at bedtime (maximum 45 mg/day, at bedtime) trazodone Desyrel ® PO 150 mg/day; may be increased by 75 mg/day q3d (maximum 375 mg/day)

50. Examples of antidepressants (2 of 3) Table 20.7 Examples of Antidepressants Generic Name Trade Name Route of Administration Average Adult Dosage Tricyclic and Tetracyclic Antidepressants amitriptyline Elavil ® PO, IM PO (initial): 25 to 100 mg/day in three to four divided doses, or 50 to 100 mg at bedtime; PO ( maint ): 25 to 150 mg/day in one dose or three to four divided doses; IM: 20 to 30 mg up to qid ; switch to PO therapy as soon as possible clomipramine Anafranil ® PO 25 mg/day; if tolerated, increase gradually to 100 mg at end of week 2 (maximum 250 mg/day) desipramine Norpramin ® PO 100 to 200 mg/day (maximum 300 mg/day) doxepin Silenor ® PO Initial: 25 to 150 mg/day in one to three divided doses; Maint : 25 to 300 mg/day in one to three divided doses imipramine Tofranil ® PO PO (initial): 30 to 100 mg/day in divided doses, gradually increase to 200 mg/day prn ; IM: up to 100 mg/day in divided doses; switch to PO dosage as soon as possible nortriptyline Pamelor ® PO 25 mg tid to qid (maximum 150 mg/day) protriptyline Vivactil ® PO, IM 15 to 40 mg/day in three to four divided doses (maximum 60 mg/day) trimipramine Surmontil ® PO Initial: 75 mg/day in divided doses, increased to 150 mg/day; Maint : 50 to 150 mg/day

51. Examples of antidepressants (3 of 3) Table 20.7 Examples of Antidepressants Generic Name Trade Name Route of Administration Average Adult Dosage Monoamine Oxidase Inhibitors (MAOIs) isocarboxazid Marplan ® PO Initial: 10 mg bid, increase by 10 mg increments q2 to 4d up to 40 mg/day by end of week 1; then increase by up to 20 mg/week prn (maximum 60 mg/day); divide daily dosage into two to four doses phenelzine Nardil ® PO 15 mg tid , may increase prn (maximum 90 mg/day) selegiline Emsam ® Transdermal patch One patch (6 mg) q24h tranylcypromine Parnate ® PO 30 mg/day in divided doses; increase prn in 10 mg/day increments at intervals of one to three weeks (maximum 60 mg/day)

52. Anxiety Disorders Anxiety : A common psychological disorder Usually temporary, not chronic The most common psychiatric illnesses in the USA Treatments: Behavior therapy - Psychotherapy Physical activity - Relaxation exercises SSRIs - Amitriptyline/nortriptyline Short-term benzodiazepines

53. Generalized Anxiety Disorder Chronic condition Characterized by uncontrollable worrying Often accompanied by: Depression or another psychiatric disorder Worrying is unrealistic or excessive May last for six months or longer

54. Panic Disorder Recurrent, uncomfortable panic attacks Symptoms peak in 10 minutes: Trembling - Shortness of breath Palpitations - Chest tightness Sweating - Nausea May mimic symptoms of heart attacks Usually resolve on their own: May cause the patient to go to the emergency department

55. Obsessive-Compulsive Disorder Potentially disabling Uncontrolled, persistent obsessions, compulsions Obsessions: Recurrent, persistent impulses Compulsions: Ritualized behaviors performed in response to obsessions

56. Social Anxiety Disorder Formerly called social phobia Extremely common Irrational fear of being scrutinized by others Symptoms: Blushing - Stuttering Sweating - Palpitations Dry throat - Muscle tension The most common anxiety disorder Usually beginning in adolescence If untreated at that time, it usually continues for life

57. Post-Traumatic Stress Disorder PTSD develops after a traumatic event causing: An immediate reaction of fear, helplessness, or horror Including assault, rape, or torture Treatments: Counseling - Cognitive behavior training Benzodiazepines - Antianxiety agents SSRIs If indicated, medications for sleep disturbances

58. Sleep Disorders Insomnia: inability to fall or stay asleep, due to: Emotional problems - Pain Physical disorders - Drugs Treatments: Removing causes - Stress reduction Regular sleep schedules - Increased daily activities Avoidance stimulants - Hypnotic benzodiazepines Bedroom changes

59. Attention Deficit and Hyperactivity Disorder Inability to focus Loss of attention Inability to remain quiet and passive Boys affected 3 times more often Can also affect older children, adults

60. Sedatives, Hypnotics, and Antianxiety Drugs Sedatives and hypnotic drugs: Treat anxiety and sleep disorders Sedation : Decreased anxiety, motor activity, mental acuity Hypnosis : an increased tendency to sleep

61. Examples of antianxiety drugs Table 20.8 Examples of Antianxiety Drugs Generic Name Trade Name Route of Administration Average Adult Dosage Benzodiazepines alprazolam Xanax ® PO 0.25 to 0.5 mg tid (maximum 4 mg/day) chlordiazepoxide Librium ® PO, IM, IV PO: 5 to 10 mg tid to qid ; IM/IV: 50 to 100 mg 1 hour before surgery diazepam Valium ® PO, IM, IV PO: 2 to 10 mg bid to qid or 15 to 30 mg/day sustained release; IV/IM: 2 to 10 mg, repeat if needed in 3 to 4 hours estazolam Prosom ® PO 1 mg at bedtime, may be increased up to 2 mg if necessary lorazepam Ativan ® PO, IM, IV PO: 2 to 6 mg/day in divided doses; IM: 2 to 4 mg (0.05 mg/kg) at least 2 hours before surgery; IV: 0.044 mg/kg up to 2 mg 15 to 20 minutes before surgery oxazepam Oxazepam ® PO 10 to 30 mg tid to qid Nonbenzodiazepines buspirone BuSpar ® PO 7.5 to 15 mg/day in divided doses secobarbital Seconal ® PO 100 to 300 mg/day in three divided doses zolpidem Ambien ® PO 5 to 10 mg at bedtime, limited to 7 to 10 days

62. Narcotic Analgesics (1 of 2) Also called opioids Have morphine-like activity: Reduce pain Induce tolerance and physical dependence Opiates are made from opium: Morphine Heroin

63. Narcotic Analgesics (2 of 2) High potential for addiction and abuse Tightly controlled Very dangerous if used with: Benzodiazepines Other CNS depressants Alcohol

64. Examples of common narcotic analgesics Table 20.9 Examples of Narcotic Analgesics Generic Name Trade Name Route of Administration Average Adult Dosage codeine (generic only) PO, IM, SC 15 to 60 mg qid fentanyl Subsys ®, Abstral ®, Actiq ® , Fentora ®, Lazanda ® , Duragesic ®, Ionsys ® , Sublimaze ® Sublingual, Buccal , Intranasal, Transdermal patch, IM, IV Transmucosal products: varied dosages; transdermal patch: 25 mcg/h q72h; IM: 50 to 100 mcg q1 to 2h; IV: 25 to 50 mcg/h hydrocodone (oral IR only available with acetaminophen: Lorcet ® , Lortab ® , Norco ®, Vicodin ® , Verdrocet ® , Xodol ® ); Hysingla ER ® , Zohydro ER ® PO Immediate-release: 5 to 10 mg q4 to 6h (in combination with 300 to 325 mg acetaminophen per tablet); extended- release: 10 to 20 mg q12 to 24h hydrocodone and homatropine Hycodan ® PO 5 to 10 mg q4 to 6h prn (maximum 15 mg/ dose) hydromorphone Dilaudid ® PO, IM, IV, rectal, SC PO/IM/IV/SC: 1 to 4 mg q4 to 6h prn; extended release: 12 to 32 mg q24h; rectal: 3 mg q4 to 6h meperidine Demerol ® PO, IM, IV, SC 50 to 150 mg q3 to 4h prn methadone Dolophine ® , Methadone ® PO, IM, SC 2.5 to 10 mg q3 to 4h prn morphine MS Contin ® , Kadian ® , Arymo ER ® , MorphaBond ER ® , Infumorph ® , Mitigo ® PO, IM, IV PO: 15 to 30 mg q4h; extended- release: 15 to 30 mg q8 to 12h; IM/IV: 5 to 15 mg q4h oxycodone Oxaydo ® , Roxicodone ® , RoxyBond ® , OxyContin ® , Xtampza ER ® PO Immediate-release: 5 to 15 mg q4 to 6h; extended- release: 10 to 20 mg q12h (for OxyContin ), 9 to 18 mg q12h (for Xtampza ER) oxymorphone Opana ® , generic PO Immediate-release: 5 to 10 mg q4 to 6h; extended-release: 5 to 10 mg q12h pentazocine Talwin ® PO, IM, IV, SC PO: 50 to 100 mg q3 to 4h (maximum 600 mg/day); IM/IV/SC: 30 mg q3 to 4h (maximum 360 mg/day) pentazocine and naloxone Talwin NX ® PO One tablet (50 mg pentazocine /0.5 mg naloxone q3 to 4h); dosage may be doubled when needed; maximum 12 tablets/day tapentadol Nucynta ® , Nucynta ER ® PO Immediate-release: 50 to 100 mg q4 to 6h prn ; extended- release: 50 to 250 mg q12h tramadol Ultram ® , ConZip ® PO Immediate- release: 50 to 100 mg q4 to 6h prn ; extended- release: 100 to 300 mg/day

65. Naloxone Opioid antagonist Blocks or temporarily reverse effects of opioids Used for emergency treatment of overdose All 50 states have laws increasing access Most allow pharmacists to provide it without a prescription

66. Anesthetics Anesthesia: Reversible unconsciousness or a loss of sensation Characterized by analgesia, immobility, and amnesia General anesthetics affect the entire body Local anesthetics: loss of sensation in a local area

67. Examples of common narcotic analgesics (1 of 3) Table 20.10 The Four Stages of General Anesthesia Stage Characterized By Stage I Analgesia Euphoria Perceptual distortions Amnesia Stage II Delirium Hypertension Tachycardia Stage III Surgical anesthesia Stage IV Medullary depression begins with cessation of respiration and circulatory collapse

68. Examples of common narcotic analgesics (2 of 3) Table 20.11 Examples of Local Anesthetics Generic Name Trade Name Route of Administration Average Adult Dosage Amides bupivacaine Sensorcaine ® IM (local infiltration, sympathetic block, lumbar epidural, caudal block, peripheral nerve block, retrobulbar block) 0.25% to 0.75% solution, depending on how administered lidocaine Xylocaine ® Caudal, Epidural, Infiltration, Nerve Block, Saddle Block, Spinal, Topical (jelly, ointment, cream, or solution) 0.5% to 2% solution (infiltration, nerve block, epidural, caudal); spinal: 5% with glucose; saddle block: 1.5% with dextrose; topical: 2.5% to 5% Esters benzocaine Americaine ® Topical Lowest effective dose procaine Novocain ® SC, Peripheral nerve block SC: 10% solution diluted with NS at 1 mL/5 seconds; PNB: 0.5% solution (up to 200 mL), 1% solution (up to 100 mL), or 2% solution (up to 50 mL)

69. Examples of common narcotic analgesics (3 of 3) Table 20.12 Examples of Currently Used General Anesthetics Generic Name Trade Name Route of Administration Average Adult Dosage diazepam Valium ® IV, IM 5 to 10 mg, repeat if needed in 2 to 4 hours propofol (a benzodiazepine) Diprivan ® IV Induction: 2 to 2.5 mg/kg q10s until induction onset; Maint : 100 to 200 mcg/kg/min thiopental sodium (a barbiturate) Pentothal ® IV IV test dose: 25 to 75 mg, then 50 to 75 mg at 20 to 40 seconds intervals; an additional 50 mg may be given prn